Lactam-containing compounds and derivatives thereof as factor Xa inhibitors

• US 6,967,208 B2
• Filed: 09/17/2002
• Issued: 11/22/2005
• Est. Priority Date: 09/21/2001
• Status: Active Grant

• Current Assignee: Bristol-Myers Squibb Company
• Original Assignee: Bristol-Myers Squibb Pharma Company (Bristol-Myers Squibb Company)
• Inventors: Li, Yun-Long, Quan, Mimi L., Han, Wei, Qiao, Jennifer X., Lam, Patrick Y. S., Pinto, Donald J. P., Orwat, Michael J., Koch, Stephanie L.
• Primary Examiner(s): Kifle, Bruck
• Application Number:
  US10/245,122
• Publication Number:
  US 20030191115A1
• Time in Patent Office: 1,162 Days
• Field of Search: 514/303, 546/119, 546/120
• US Class Current: 514/303
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/4365 the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
• CPC Class Codes: A61K 31/616 by carboxylic acids, e.g. acetylsalicylic acid
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 7/02 Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
• CPC Class Codes: C07D 211/40 Oxygen atoms
• CPC Class Codes: C07D 211/76 attached in position 2 or 6
• CPC Class Codes: C07D 213/64 attached in position 2 or 6
• CPC Class Codes: C07D 213/75 Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
• CPC Class Codes: C07D 213/81 Amides; Imides
• CPC Class Codes: C07D 213/82 in position 3
• CPC Class Codes: C07D 239/10 Oxygen or sulfur atoms
• CPC Class Codes: C07D 241/08 with oxygen atoms directly attached to ring carbon atoms
• CPC Class Codes: C07D 265/10 with oxygen atoms directly attached to ring carbon atoms
• CPC Class Codes: C07D 401/10 linked by a carbon chain containing aromatic rings
• CPC Class Codes: C07D 401/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 401/14 containing three or more hetero rings
• CPC Class Codes: C07D 403/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 403/14 containing three or more hetero rings
• CPC Class Codes: C07D 405/14 containing three or more hetero rings
• CPC Class Codes: C07D 409/12 : linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 409/14 : containing three or more hetero rings
• CPC Class Codes: C07D 413/12 : linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 413/14 : containing three or more hetero rings
• CPC Class Codes: C07D 417/14 : containing three or more hetero rings
• CPC Class Codes: C07D 471/04 : Ortho-condensed systems
• CPC Class Codes: C07D 495/04 : Ortho-condensed systems

Abstract

The present application describes lactam-containing compounds and derivatives thereof of Formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Claims

1. A compound of Formula I:

or a stereoisomer or pharmaceutically acceptable salt thereof, wherein;

ring M, including P₁, P₂, and M₁, and M₂ is substituted with 0-2 R^1a and is

ring P, including P₁, P₂, and P₃, is

P₄ is —

G₁—

G;

G is a group of Formula IIa or IIb;

ring D, including the two atoms of Ring E to which it is attached, is a 5-6 membered ring consisting of;

carbon atoms and 0-2 heteroatoms selected from the group consisting of N, O, and S(O)_p;

ring D is substituted with 0-2 R and there are 0-3 ring double bonds;

E is selected from phenyl, pyridyl, pyrimidyl, pyrazinyl, and pyridazinyl, and is substituted with 1-2 R;

alternatively, ring D is absent and ring E is selected from phenyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, pyrrolyl, pyrazolyl, imidazolyl, isoxazolyl, oxazolyl, triazolyl, thienyl, and thiazolyl, and ring E is substituted with 1-2 R;

alternatively, ring D is absent and ring E is selected from phenyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, pyrrolyl, pyrazolyl, imidazolyl, isoxazolyl, oxazolyl, triazolyl, thienyl, and thiazolyl, and ring E is substituted with 1 R and with a 5-6 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, wherein the 5-6 membered heterocycle is substituted with 0-1 carbonyl and 1-2 R and there are 0-3 ring double bonds;

R is selected from H, C_1-4 alkyl, F, Cl, Br, I, OH, OCH₃, OCH₂CH₃, OCH(CH₃)₂, OCH₂CH₂CH₃, CN, C(═

NR⁸)NR⁷R⁹, NHC(═

NR⁸)NR⁷R⁹, ONHC(═

NR⁸)NR⁷R⁹, NR⁸CH(═

NR⁷), NH₂, NH(C_1-3 alkyl), N(C_1-3 alkyl)₂, C(═

NH)NH₂, CH₂NH₂, CH₂NH(C_1-3 alkyl), CH₂N(C_1-3 alkyl)₂, CH₂CH₂NH₂, CH₂CH₂NH(C_1-3 alkyl), CH₂CH₂N(C_1-3 alkyl)₂, (CR⁸R⁹)_tC(O)H, (CR⁸R⁹)_tC(O)R^2c, (CR⁸R⁹)_tNR⁷R⁸, (CR⁸R⁹)_tC(O)NR⁷R⁸, (CR⁸R⁹)_tNR⁷C(O)R⁷, (CR⁸R⁹)_tOR³, (CR⁸R⁹)_tS(O)_pNR⁷R⁸, (CR⁸R⁹)_tNR⁷S(O)_pR⁷, (CR⁸R⁹)_tSR³, (CR⁸R⁹)_tS(O)R³, (CR⁸R⁹)_tS(O)₂R³, and OCF₃;

alternatively, when 2 R groups are attached to adjacent atoms, they combine to form methylenedioxy or ethylenedioxy;

A is selected from;

C_3-10 carbocycle substituted with 0-2 R⁴,

B is

 

provided that Z and B are attached to different atoms on A and that the A—

X—

N moiety forms other than a N—

N—

N group;

Q₁ is C═

O;

ring Q is a 6 4-8 membered monocyclic ring, wherein;

0-2 double bonds are present within the ring and the ring is substituted with 0-2 R^4a;

X is absent;

G₁ is absent or is selected from (CR³R^3a)_1-5, (CR³R^3a)_0-2CR³═

CR³(CR³R^3a)_0-2, (CR³R^3a)_0-2C≡

C(CR³R^3a)_0-2, (CR³R^3a)_uC(O)(CR³R^3a)_w, (CR³R^3a)_uC(O)O(CR³R^3a)_w, (CR³R^3a)_uOC(O)(CR³R^3a)_w, (CR³R^3a)_uO(CR³R^3a)_w, (CR³R^3a)_uN^3b(CR³R^3a)_w, (CR³R^3a)_uC(O)N^3b(CR³R^3a)_w, (CR³R^3a)_uN^3bC(O)(CR³R^3a)_w, (CR³R^3a)_uOC(O)N^3b(CR³R^3a)_w, (CR³R^3a)_uN^3bC(O)O(CR³R^3a)_w, (CR³R^3a)_uN^3bC(O)N^3b(CR³R^3a)_w, (CR³R^3a)_uN^3bC(S)N^3b(CR³R^3a)_w, (CR³R^3a)_uS(CR³R^3a)_w, (CR³R^3a)_uS(O)(CR³R^3a)_w, (CR³R^3a)_uS(O)₂(CR³R^3a)_w, (CR³R^3a)_uS(O)N^3b(CR³R^3a)_w, (CR³R^3a)_uN^3bS(O)₂(CR³R^3a)_w, (CR³R^3a)_uS(O)₂N^3b(CR³R^3a)_w, (CR³R^3a)_uN^3bS(O)₂N^3b(CR³R^3a)_w, (CR³R^3a)_uNR^3e(CR³R^3a)_w, (CR³R^3a)_uC(O)(CR³R^3a)_uC(O)(CR³R^3a)_w, (CR³R^3a)_uNR^3b(CR³R^3a)_uC(O)NR^3b(CR³R^3a)_w, (CR³R^3a)_uNR^3bC(O)(CR³R^3a)_uC(O)(CR³R^3a)_w, (CR³R^3a)_uC(O)(CR³R^3a)_uC(O)NR^3b(CR³R^3a)_w, (CR³R^3a)_uNR^3bC(O)(CR³R^3a)_uC(O)NR^3b(CR³R^3a)_w, (CR³R^3a)_uS(O)NR^3bC(O)(CR³R^3a)_w, (CR³R^3a)_uC(O)NR^3bS(O)₂(CR³R^3a)_w, and (CR³R^3a)_uS(O)₂NR^3bC(O)NR^3bCR³R^3a)_w, wherein u+w total 0, 1, 2, 3, or 4, provided that G₁ does not form an N—

S, NCH₂N, NCH₂O, or NCH₂S bond with either group to which it is attached;

R^1a, at each occurrence, is selected from H, —

(CR³R^3a)_r—

R^1b, —

(CR³R^3a)_r—

CR³R^1bR^1b, —

(CR³R^3a)_r—

O—

(CR³R^3a)_rR^1b, —

C_2-6 alkenylene-R^1b, —

C_2-6 alkynylene-R^1b, —

(CR³R^3a)_rC(═

NR^1b)NR³R^1b, NR³CR³R^3aR^1c, OCR³R^3aR^1c, SCR³R^3aR^1c, NR³(CR³R^3a)₂(CR³R^3a)_tR^1b, C(O)NR²(CR³R^3a)₂(CR³R^3a)_tR^1b, CO₂(CR³R^3a)₂(CR³R^3a)_tR^1b, O(CR³R^3a)₂(CR³R^3a)_tR^1b, S(CR³R^3a)₂(CR³R^3a)_tR^1b, S(O)_p(CR³R^3a)_rR^1d, O(CR³R^3a)_rR^1d, NR³(CR³R^3a)_rR^1d, OC(O)NR³(CR³R^3a)_rR^1d, NR³C(O)NR³(CR³R^3a)_rR^1d, NR³C(O)O(CR³R^3a)_rR^1d, and NR³C(O)(CR³R^3a)_rR^1d, provided that R^1a forms other than an N-halo, N—

S, O—

O, or N—

CN bond;

alternatively, when two R^1a groups are attached to adjacent atoms, together with the atoms to which they are attached they form a 5-7 membered ring consisting of;

carbon atoms and 0-2 heteroatoms selected from the group consisting of N, O, and S(O)_p, this ring being substituted with 0-2 R^4b and 0-3 ring double bonds;

R^1b is selected from H, C_1-3 alkyl, F, Cl, Br, I, —

CN, —

NO₂, —

CHO, (CF₂)_rCF₃, (CR³R^3a)_rOR², NR²R^2a, C(O)R^2b, CO₂R^2b, OC(O)R², (CF₂)_rCO₂R^2a, S(O)_pR^2b, NR²(CH₂)_rOR², C(═

NR^2c)NR²R^2a, NR²C(O)R^2b, NR^2c(O)NHR², NR²C(O)₂R^2a, OC(O)NR²R^2a, C(O)NR²R^2a, C(O)NR²(CH₂)_rOR², SO₂NR²R^2a, NR²SO₂R², C(O)NR²SO₂R², C_3-6 carbocycle substituted with 0-2 R^4b, and 5-10 membered heterocycle consisting of carbon atoms and from 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b, provided that R^1b forms other than an O—

O, N-halo, N—

S, or N—

CN bond;

R^1c is selected from H, CH(CH₂OR²)₂, C(O)R^2c, C(O)NR²R^2a, S(O)R², S(O)₂R², and SO₂NR²R^2a;

R^1d is selected from C_3-6 carbocycle substituted with 0-2 R^4b and 5-10 membered heterocycle consisting of carbon atoms and from 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b, provided that R^1d forms other than an N—

S bond;

R², at each occurrence, is selected from H, CF₃, C_1-6 alkyl, benzyl, —

(CH₂)_r—

C_3-10 carbocycle substituted with 0-2 R^4b, and —

(CH₂)_r-5-10 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b;

R^2a, at each occurrence, is selected from H, CF₃, C_1-6 alkyl, benzyl, —

(CH₂)_r—

C_3-10 carbocycle substituted with 0-2 R^4b, and —

(CH₂)_r-5-10 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b;

alternatively, R² and R^2a, together with the atom to which they are attached, combine to form a 5 or 6 membered saturated, partially saturated or unsaturated ring substituted with 0-2 R^4b and consisting of;

0-1 additional heteroatoms selected from the group consisting of N, O, and S(O)_p;

R^2b, at each occurrence, is selected from CF₃, C_1-4 alkoxy substituted with 0-2 R^4b, C_1-6 alkyl substituted with 0-2 R^4b, —

(CH₂)_r—

C_3-10 carbocycle substituted with 0-2 R^4b, and —

(CH₂)_r-5-10 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b;

R^2c, at each occurrence, is selected from CF₃, OH, C_1-4 alkoxy, C_1-6 alkyl, —

(CH₂)_r—

C_3-10 carbocycle substituted with 0-2 R^4b, and —

(CH₂)_r-5-10 membered heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b;

R³, at each occurrence, is selected from H, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, benzyl, and phenyl;

R^3a, at each occurrence, is selected from H, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, benzyl, and phenyl;

alternatively, R³ and R^3a, together with the nitrogen atom to which they are attached, combine to form a 5 or 6 membered saturated, partially unsaturated, or unsaturated ring consisting of;

carbon atoms, the nitrogen atom to which R³ and R^3a are attached, and 0-1 additional heteroatoms selected from the group consisting of N, O, and S(O)_p;

R^3b, at each occurrence, is selected from H, C_1-6 alkyl substituted with 0-2 R^1a, C_2-6 alkenyl substituted with 0-2 R^1a, C_2-6 alkynyl substituted with 0-2 R^1a, —

(C_0-4 alkyl)-5-10 membered carbocycle substituted with 0-3 R^1a, and —

(C_0-4 alkyl)-5-10 membered heterocycle substituted with 0-3 R^1a and consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p;

R^3c, at each occurrence, is selected from CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, benzyl, and phenyl;

R^3d, at each occurrence, is selected from H, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C_1-4 alkyl-phenyl, and C(═

O)R^3c;

R^3e, at each occurrence, is selected from H, SO₂NHR³, SO₂NR³R³, C(O)R³, C(O)NHR³, C(O)OR^3f, S(O)R^3f, S(O)₂R^3f, C_1-6 alkyl substituted with 0-2 R^1a, C_2-6 alkenyl substituted with 0-2 R^1a, C_2-6 alkynyl substituted with 0-2 R^1a, —

(C_0-4 alkyl)-5-10 membered carbocycle substituted with 0-3 R^1a, and —

(C_0-4 alkyl)-5-10 membered heterocycle substituted with 0-3 R^1a and consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p;

R^3f, at each occurrence, is selected from;

C_1-6 alkyl substituted with 0-2 R^1a, C_2-6 alkenyl substituted with 0-2 R^1a, C_2-6 alkynyl substituted with 0-2 R^1a, —

(C_0-4 alkyl)-5-10 membered carbocycle substituted with 0-3 R^1a, and —

(C_0-4 alkyl)-5-10 membered heterocycle substituted with 0-3 R^1a and consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p;

R⁴, at each occurrence, is selected from H, ═

O, (CR³R^3a)_rOR², F, Cl, Br, I, C_1-4 alkyl, (CR³R^3a)_rCN, (CR³R^3a)_rNO₂, (CR³R^3a)_rNR²R^2a, (CR³R^3a)_rC(O)R^2c, (CR³R^3a)_rNR²C(O)R^2b, (CR³R^3a)_rC(O)NR²R^2a, (CR³R^3a)_rNR²C(O)NR²R^2a, (CR³R^3a)_rC(═

NR²)NR²R^2a, (CR³R^3a)_rC(═

NS(O)₂R⁵)NR²R^2a, (CR³R^3a)_rNHC(═

NR²)NR²R^2a, (CR³R^3a)_rC(O)NHC(═

NR²)NR²R^2a, (CR³R^3a)_rSO₂NR²R^2a, (CR³R^3a)_rNR²SO₂NR²R^2a, (CR³R^3a)_rNR²SO₂—

C_1-4 alkyl, (CR³R^3a)_rNR²SO₂R⁵, (CR³R^3a)_rS(O)_pR^5a, (CR³R^3a)_r(CF₂)_rCF₃, NHCH₂R^1c, OCH₂R^1c, SCH₂R^1c, NH(CH₂)₂(CH₂)_tR^1b, O(CH₂)₂(CH₂)_tR^1b, S(CH₂)₂(CH₂)_tR^1b, (CR³R^3a)_r-5-6 membered carbocycle substituted with 0-1 R⁵, and a (CR³R^3a)_r-5-6 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-1 R⁵;

R^4a, at each occurrence, is selected from H, ═

O, (CR³R^3a)_rOR², (CR³R^3a)_rF, (CR³R^3a)_rBr, (CR³R^3a)_rCl, C_1-4 alkyl, (CR³R^3a)_rCN, (CR³R^3a)_rNO₂, (CR³R^3a)_rNR²R^2a, (CR³R^3a)_rC(O)R^2c, (CR³R^3a)_rNR²C(O)R^2b, (CR³R^3a)_rC(O)NR²R^2a, (CR³R^3a)_rN═

CHOR³, (CR³R^3a)_rC(O)NH(CH₂)₂NR²R^2a, (CR³R^3a)_rNR²C(O)NR²R^2a, (CR³R^3a)_rC(═

NR²)NR²R^2a, (CR³R^3a)_rNHC(═

NR²)NR²R^2a, (CR³R^3a)_rSO₂NR²R^2a, (CR³R^3a)_rNR²SO₂NR²R^2a, (CR³R^3a)_rNR²SO₂—

C_1-4 alkyl, (CR³R^3a)_rC(O)NHSO₂—

C_1-4 alkyl, (CR³R^3a)NR²SO₂R⁵, (CR³R^3a)_rS(O)_pR^5a, (CR³R^3a)_r(CF₂)_rCF₃, (CR³R^3a)_r-5-6 membered carbocycle substituted with 0-1 R⁵, and a (CR³R^3a)_r-5-6 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-1 R⁵;

R^4b, at each occurrence, is selected from H, ═

O, (CH₂)_rOR³, (CH₂)_rF, (CH₂)_rCl, (CH₂)_rBr, (CH₂)_rI, C_1-4 alkyl, (CH₂)_rCN, (CH₂)_rNO₂, (CH₂)_rNR³R^3a, (CH₂)_rC(O)R³, (CH₂)_rC(O)OR^3c, (CH₂)_rNR³C(O)R^3a, (CH₂)_r—

C(O)NR³R^3a, (CH₂)_rNR³C(O)NR³R^3a, (CH₂)_r—

C(═

NR³)NR³R^3a, (CH₂)_rNR³C(═

NR³)NR³R^3a, (CH₂)_rSO₂NR³R^3a, (CH₂)_rNR³SO₂NR³R^3a, (CH₂)_rNR³SO₂—

C_1-4 alkyl, (CH₂)_rNR³SO₂CF₃, (CH₂)_rNR³SO₂-phenyl, (CH₂)_rS(O)_pCF₃, (CH₂)_rS(O)_p—

C_1-4 alkyl, (CH₂)_rS(O)_p-phenyl, and (CH₂)_r(CF₂)_rCF₃;

R^4c, at each occurrence, is selected from H, C_1-4 alkyl (CR³R^3a)_r1OR², (CR³R^3a)_r1F, (CR³R^3a)_r1Br, (CR³R^3a)_r1Cl, (CR³R^3a)_r1CN, (CR³R^3a)_r1NO₂, (CR³R^3a)_r1NR²R^2a, (CR³ R^3a)_rC(O)R^2c, (CR³R^3a)_r1NR²C(O)R^2b, (CR³R^3a)_rC(O)NR²R^2a, (CR³R^3a)_r1N═

CHOR³, (CR³R^3a)_rC(O)NH(CH₂)₂NR²R^2a, (CR³R^3a)_r1NR²C(O)NR²R^2a, (CR³R^3a)_r1C(═

NR²)NR²R^2a, (CR³R^3a)_r1NHC(═

NR²)NR²R^2a, (CR³R^3a)_rSO₂NR²R^2a, (CR³R^3a)_r1NR²SO₂NR²R^2a, (CR³R^3a)_r1NR²SO₂—

C_1-4 alkyl, (CR³R^3a)_rC(O)NHSO₂—

C_1-4 alkyl, (CR³R^3a)_r1NR²SO₂R⁵, (CR³R^3a)_rS(O)_pR^5a, (CR³R^3a)_r(CF₂)_rCF₃, (CR³R^3a)_r-5-6 membered carbocycle substituted with 0-1 R⁵, and a (CR³R^3a)_r-5-6 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-1 R⁵;

R⁵, at each occurrence, is selected from H, C_1-6 alkyl, ═

O, (CH₂)_rOR³, F, Cl, Br, I, —

CN, NO₂,(CH₂)_rNR³R^3a, (CH₂)_rC(O)R³, (CH₂)_rC(O)OR^3c, (CH₂)_rNR³C(O)R^3a,(CH₂)_rC(O)NR³R^3a, (CH₂)_rNR³C(O)NR³R^3a, (CH₂)_rCH(═

NOR^3d), (CH₂)_rC(═

NR³)NR³R^3a, (CH₂)_rNR³C(═

NR³)NR³R^3a, (CH₂)_rSO₂NR³R^3a, (CH₂)_rNR³SO₂NR³R^3a, (CH₂)_rNR³SO₂C_1-4 alkyl, (CH₂)_rNR³SO₂CF₃, (CH₂)_rNR³SO₂-phenyl, (CH₂)_rS(O)_pCF₃, (CH₂)_rS(O)_p—

C_1-4 alkyl, (CH₂)_rS(O)_p-phenyl, (CF₂)_rCF₃, phenyl substituted with 0-2 R⁶, naphthyl substituted with 0-2 R⁶, and benzyl substituted with 0-2 R⁶;

R^5a, at each occurrence, is selected from C_1-6 alkyl, (CH₂)_rOR³, (CH₂)_rNR³R^3a, (CH₂)_rC(O)R³, (CH₂)_rC(O)OR^3c, (CH₂)_rNR³C(O)R^3a, (CH₂)_rC(O)NR³R^3a, (CF₂)_rCF₃, phenyl substituted with 0-2 R⁶, naphthyl substituted with 0-2 R⁶, and benzyl substituted with 0-2 R⁶, provided that R^5a does not form a S—

N or S(O)_p—

C(O) bond;

R⁶, at each occurrence, is selected from H, OH, (CH₂)_rOR², halo, C_1-4 alkyl, CN, NO₂, (CH₂)_rNR²R^2a, (CH₂)_rC(O)R^2b, NR²C(O)R^2b, NR²C(O)NR²R^2a, C(═

NH)NH₂, NHC(═

NH)NH₂, SO₂NR²R^2a, NR²SO₂NR²R^2a, and NR²SO₂C_1-4 alkyl;

R⁷, at each occurrence, is selected from H, OH, C_1-6 alkyl, C_1-6 alkyl-C(O)—

, C_1-6 alkyl-O—

, (CH₂)_n-phenyl, C_1-4 alkyl-OC(O)—

, C_6-10 aryl-O—

, C_6-10 aryl-OC(O)—

, C_6-10 aryl-CH₂—

C(O)—

, C_1-4 alkyl-C(O)O—

C_1-4 alkyl-OC(O)—

, C_6-10 aryl-C(O)O—

C_1-4 alkyl-OC(O)—

, C_1-6 alkyl-NH₂—

C(O)—

, phenyl-NH₂—

C(O)—

, and phenyl-C_1-4 alkyl-C(O)—

;

R⁸, at each occurrence, is selected from H, C_1-6 alkyl, and (CH₂)_n-phenyl;

alternatively, R⁷ and R⁸, when attached to the same nitrogen, combine to form a 5-10 membered heterocyclic ring consisting of carbon atoms and 0-2 additional heteroatoms selected from the group consisting of N, O, and S(O)_p;

R⁹, at each occurrence, is selected from H, C_1-6 alkyl, and (CH₂)_n-phenyl;

n, at each occurrence, is selected from 0, 1, 2, and 3;

p, at each occurrence, is selected from 0,1, and 2;

r, at each occurrence, is selected from 0, 1, 2, 3, 4, 5, and 6;

r1, at each occurrence, is selected from 1, 2, 3, 4, 5, and 6;

t, at each occurrence, is selected from 0, 1, 2, and 3.

2. A compound according to claim 1, wherein:

G is a group of Formula IIa or IIb;

ring D, including the two atoms of Ring E to which it is attached, is a 5-6 membered ring consisting of;

carbon atoms and 0-2 heteroatoms selected from the group consisting of N, O, and S(O)_p;

ring D is substituted with 0-2 R and there are 0-3 ring double bonds;

E is selected from phenyl, pyridyl, pyrimidyl, pyrazinyl, and pyridazinyl, and is substituted with 1-2 R;

alternatively, ring D is absent, and ring E is selected from phenyl, pyridyl, pyrimidyl, and thienyl, and ring E is substituted with 1-2 R;

alternatively, ring D is absent, ring E is selected from phenyl, pyridyl, and thienyl, and ring E is substituted with 1 R and substituted with a 5 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, wherein the 5 membered heterocycle is substituted with 0-1 carbonyl and 1-2 R and there are 0-3 ring double bonds;

R is selected from H, C_1-4 alkyl, F, Cl, OH, OCH₃, OCH₂CH₃, OCH(CH₃)₂, CN, C(═

NH)NH₂, C(═

NH)NHOH, C(═

NH)NHOCH₃, NH₂, NH(C_1-3 alkyl), N(C_1-3 alkyl)₂, C(═

NH)NH₂, CH₂NH₂, CH₂NH(C_1-3 alkyl), CH₂N(C_1-3 alkyl)₂, (CR⁸R⁹)_tNR⁷R⁸, C(O)NR⁷R⁸, CH₂C(O)NR⁷R⁸, S(O)_pNR⁷R⁸, CH₂S(O)_pNR⁷R⁸, SO₂R³, and OCF₃;

alternatively, when 2 R groups are attached to adjacent atoms, they combine to form methylenedioxy or ethylenedioxy;

A is selected from;

C_5-10 carbocycle substituted with 0-2 R⁴;

R^1a is selected from H, —

(CH₂)_r—

R^1b, —

(CH(CH₃))_r—

R^1b, —

(C(CH₃)₂)_r—

R^1b, NHCH₂R^1c, OCH₂R^1c, SCH₂R^1c, NH(CH₂)₂(CH₂)_tR^1b, and O(CH₂)₂(CH₂)_tR^1b, provided that R^1a forms other than an N-halo, N—

S, or N—

CN bond;

alternatively, when two R^1a groups are attached to adjacent atoms, together with the atoms to which they are attached they form a 5-7 membered ring consisting of;

carbon atoms and 0-2 heteroatoms selected from the group consisting of N, O, and S(O)_p, this ring being substituted with 0-2 R^4b and 0-3 ring double bonds;

R^1b is selected from H, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, F, Cl, Br, I, —

CN, —

CHO, CF₃, OR², NR²R^2a, C(O)R^2b, CO₂R^2b, OC(O)R², CO₂R^2a, S(O)_pR², NR²(CH₂)_rOR², NR²C(O)R^2b, NR²C(O)NHR², NR²C(O)₂R^2a, OC(O)NR²R^2a, C(O)NR²R^2a, C(O)NR²(CH₂)_rOR², SO₂NR²R^2a, NR²SO₂R², C_5-6 carbocycle substituted with 0-2 R^4b, and 5-6 membered heterocycle consisting of carbon atoms and from 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b, provided that R^1b forms other than an O—

O, N-halo, N—

S, or N—

CN bond;

R^1c is selected from H, CH(CH₂OR²)₂, C(O)R^2c, C(O)NR²R^2a, S(O)R², S(O)₂R², and SO₂NR²R^2a;

R², at each occurrence, is selected from H, CF₃, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)_{2, CH2}CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, benzyl, C_5-6 carbocycle substituted with 0-2 R^4b, a C_5-6 carbocyclic-CH₂-group substituted with 0-2 R^4b, and 5-6 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b;

R^2a, at each occurrence, is selected from H, CF₃, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)_{2, CH2}CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, benzyl, C_5-6 carbocycle substituted with 0-2 R^4b, and 5-6 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b;

alternatively, R² and R^2a, together with the atom to which they are attached, combine to form a 5 or 6 membered saturated, partially saturated or unsaturated ring substituted with 0-2 R^4b and consisting of;

0-1 additional heteroatoms selected from the group consisting of N, O, and S(O)_p;

R^2b, at each occurrence, is selected from CF₃, C_1-4 alkoxy, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, benzyl, C_5-6 carbocycle substituted with 0-2 R^4b, and 5-6 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b;

R^2c, at each occurrence, is selected from CF₃, OH, C_1-4 alkoxy, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, benzyl C_5-6 carbocycle substituted with 0-2 R^4b, and 5-6 membered heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b;

R³, at each occurrence, is selected from H, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, benzyl, and phenyl;

R^3a, at each occurrence, is selected from H, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, benzyl, and phenyl;

alternatively, R³ and R^3a, together with the nitrogen atom to which they are attached, combine to form a 5 or 6 membered saturated, partially unsaturated, or unsaturated ring consisting of;

carbon atoms and the nitrogen atom to which R³ and R^3a are attached;

R^3c, at each occurrence, is selected from CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, benzyl phenyl;

R^3d, at each occurrence, is selected from H, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂-phenyl, CH₂CH₂-phenyl, and C(═

O)R^3c;

R⁴, at each occurrence, is selected from H, ═

O, OR², CH₂OR², (CH₂)₂OR², F, Cl, Br, I, C_1-4 alkyl, —

CN, NO₂, NR²R^2a, CH₂NR²R^2a, (CH₂)₂NR²R^2a, C(O)R^2c, NR²C(O)R^2b, C(O)NR²R^2a, SO₂NR²R^2a, S(O)_pR^5a, CF₃, CF₂CF₃, 5-6 membered carbocycle substituted with 0-1 R⁵, and a 5-6 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-1 R⁵;

R^4a, at each occurrence, is selected from H, ═

O, CH₂OR², OR², CH₂F, F, CH₂Br, Br, CH₂Cl, Cl, C_1-4 alkyl, CH₂—

CN, —

CN, CH₂NO₂, NO₂, CH₂NR²R^2a, NR²R^2a, CH₂—

C(O)R^2c, C(O)R^2c, NR²C(O)R^2b, (CH₂)_rC(O)NR²R^2a, NR²C(O)NR²R^2a, (CH₂)_rSO₂NR²R^2a, NR²SO₂NR²R^2a, NR²SO₂—

C_1-4 alkyl, NR²SO₂R⁵, (CH₂)_rS(O)_pR^5a, CH₂CF₃, CF₃, CH₂-5-6 membered carbocycle substituted with 0-1 R⁵, 5-6 membered carbocycle substituted with 0-1 R⁵, and a CH₂-5-6 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-1 R⁵, and 5-6 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-1 R⁵;

R^4b, at each occurrence, is selected from H, ═

O, OR³, CH₂OR³, F, Cl, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, —

CN, NO₂, NR³R^3a, CH₂NR³R^3a, C(O)R³, CH₂—

C(O)R³, C(O)OR^3c, CH₂C(O)OR^3c, NR³C(O)R^3a, CH₂NR³C(O)R^3a, C(O)NR³R^3a, CH₂C(O)NR³R^3a, NR³C(O)NR³R^3a, CH₂NR³C(O)NR³R^3a, C(═

NR³)NR³R^3a, CH₂C(═

NR³)NR³R^3a, NR³C(═

NR³)NR³R^3a, CH₂NR³C(═

NR³)NR³R^3a, SO₂NR³R^3a, CH₂SO₂NR³R^3a, NR³SO₂NR³R^3a, CH₂NR³SO₂NR³R^3a, NR³SO₂—

C_1-4 alkyl, CH₂NR³SO₂—

C_1-4 alkyl NR³SO₂CF₃, CH₂NR³SO₂CF₃, NR³SO₂-phenyl, CH₂NR³SO₂-phenyl, S(O)_pCF₃, CH₂S(O)_pCF₃, S(O)_p—

C_1-4 alkyl, CH₂S(O)_p—

C_1-4 alkyl, S(O)_p-phenyl, CH₂S(O)_p-phenyl, CF₃, and CH₂—

CF₃;

R^4c, at each occurrence, is selected from H, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, CH₂OR², CH₂F, CH₂Br, CH₂Cl, CH₂CN, CH₂NO₂, CH₂NR²R^2a, C(O)R^2c, CH₂C(O)R^2c, CH₂NR²C(O)R^2b, C(O)NR²R^2a, CH₂C(O)NR²R^2a, CH₂NR²C(O)NR²R^2a, SO₂NR²R^2a, CH₂SO₂NR²R^2a, CH₂NR²SO₂NR²R^2a, CH₂NR²SO₂—

C_1-4 alkyl, C(O)NHSO₂—

C_1-4 alkyl, CH₂C(O)NHSO₂—

C_1-4 alkyl, CH₂NR²SO₂R⁵, S(O)_pR^5a, CH₂S(O)_pR^5a, CF₃, CH₂CF₃, 5-6 membered carbocycle substituted with 0-1 R⁵, CH₂-5-6 membered carbocycle substituted with 0-1 R⁵, 5-6 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-1 R⁵, and a CH₂-5-6 membered heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-1 R⁵;

R⁵, at each occurrence, is selected from H, ═

O, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, OR³, CH₂OR³, F, Cl, —

CN, NO₂, NR³R^3a, CH₂NR³R^3a, C(O)R³, CH₂C(O)R³, C(O)OR^3c, CH₂C(O)OR^3c, NR³C(O)R^3a, C(O)NR³R^3a, NR³C(O)NR³R^3a, CH(═

NOR^3d), C(═

NR³)NR³R^3a, NR³C(═

NR³)NR³R^3a, SO₂NR³R^3a, NR³SO₂NR³R^3a, NR³SO₂—

C_1-4 alkyl, NR³SO₂CF₃, NR³SO₂-phenyl, S(O)_pCF₃, S(O)_p—

C_1-4 alkyl, S(O)_p-phenyl, CF₃, phenyl substituted with 0-2 R⁶, naphthyl substituted with 0-2 R⁶, and benzyl substituted with 0-2 R⁶; and

,

R⁶, at each occurrence, is selected from H, OH, OR², F, Cl, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, CN, NO₂, NR²R^2a, CH₂NR²R^2a, C(O)R^2b, CH₂C(O)R^2b, NR²C(O)R^2b, NR²C(O)NR²R^2a, C(═

NH)NH₂, NHC(═

NH)NH₂, SO₂NR²R^2a, NR²SO₂NR²R^2a, and NR²SO₂C_1-4 alkyl.

3. A compound according to claim 2, wherein;

G is selected from the group;

G₁ is absent or is selected from (CR³R^3a)_1-3, (CR³R^3a)_uC(O)(CR³R^3a)_w, (CR³R^3a)_uO(CR³R^3a)_w, (CR³R^3a)_uNR^3b(CR³R^3a)_w, (CR³R^3a)_uC(O)NR^3b(CR³R^3a)_w, (CR³R^3a)_uNR^3bC(O)(CR³R^3a)_w, (CR³R^3a)_uNR^3bC(O)(CR³R^3a)_uC(O)NR^3b(CR³R^3a)_w, (CR³R^3a)_uS(CR³R^3a)_w, (CR³R^3a)_uS(O)(CR³R^3a)_w, (CR³R^3a)_uS(O)₂(CR³R^3a)_w, (CR³R^3a)_uS(O)NR^3b(CR³R^3a)_w, (CR³R^3a)_uNR^3bS(O)₂(CR³R^3a)_w, and (CR³R^3a)_uS(O)₂NR^3b(CR³R^3a)_w, wherein u+w total 0, 1, or 2, provided that G₁ does not form a N—

S, NCH₂N, NCH₂O, or NCH₂S bond with either group to which it is attached;

A is phenyl substituted with 0-2 R⁴;

R^1a is selected from H, R^1b, CH(CH₃)R^1b, C(CH₃)₂R^1b, CH₂R^1b, and CH₂CH₂R^1b, provided that R^1a forms other than an N-halo, N—

S, or N—

CN bond;

alternatively, when two R^1a groups are attached to adjacent atoms, together with the atoms to which they are attached they form a 5-6 membered ring consisting of;

carbon atoms and 0-2 heteroatoms selected from the group consisting of N, O, and S(O)_p, this ring being substituted with 0-2 R^4b and 0-3 ring double bonds;

R^1b is selected from H, CH₃, CH₂CH₃, F, Cl, Br, —

CN, —

CHO, CF₃, OR², NR²R^2a, C(O)R^2b, CO₂R^2b, OC(O)R², CO₂R^2a, S(O)_pR², NR²(CH₂)_rOR², NR²C(O)R^2b, C(O)NR²R^2a, SO₂NR²R^2a, NR²SO₂R², phenyl substituted with 0-2 R^4b, and 5-6 membered aromatic heterocycle consisting of carbon atoms and from 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b, provided that R^1b forms other than an O—

O, N-halo, N—

S, or N—

CN bond;

R², at each occurrence, is selected from H, CF₃, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, phenyl substituted with 0-2 R^4b, a benzyl substituted with 0-2 R^4b, and a 5-6 membered aromatic heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b;

R^2a, at each occurrence, is selected from H, CF₃, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, benzyl, phenyl substituted with 0-2 R^4b, and 5-6 membered aromatic heterocycle consisting of;

carbon atoms and 1-4 hetero atoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b;

alternatively, R² and R^2a, together with the atom to which they are attached, combine to form a 5 or 6 membered saturated, partially saturated or unsaturated ring substituted with 0-2 R^4b and consisting of;

0-1 additional heteroatoms selected from the group consisting of N, O, and S(O)_p;

R^2b, at each occurrence, is selected from CF₃, C_1-4 alkoxy, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, benzyl, phenyl substituted with 0-2 R^4b, and 5-6 membered aromatic heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b;

R^2c, at each occurrence, is selected from CF₃, OH, OCH₃, OCH₂CH₃, OCH₂CH₂CH₃, OCH(CH₃)₂, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, benzyl, phenyl substituted with 0-2 R^4b, and 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b;

R⁴, at each occurrence, is selected from H, CH₂OR², (CH₂)₂OR², OR², F, Cl, Br, I, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, —

CN, NO₂, NR²R^2a, CH₂NR²R^2a, (CH₂)₂NR²R^2a, C(O)R^2c, NR²C(O)R^2b, C(O)NR²R^2a, SO₂NR²R^2a, CF₃, and CF₂CF₃;

R^4a at each occurrence, is selected from H, ═

O, CH₂OR², OR², F, Br, Cl, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, —

CN, NO₂, CH₂NR²R^2a, NR²R^2a, C(O)R^2c, NR²C(O)R^2b, C(O)NR²R^2a, NR²C(O)NR²R^2a, SO₂NR²R^2a, and —

CF₃;

R^4b, at each occurrence, is selected from H, ═

O, OR³, CH₂OR³, F, Cl, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, —

CN, NO₂, NR³R^3a, CH₂NR³R^3a, C(O)R³, CH₂—

C(O)R³, C(O)OR^3c, CH₂—

C(O)OR^3c, NR³C(O)R^3a, CH₂NR³C(O)R^3a, C(O)NR³R^3a, CH₂—

C(O)NR³R^3a, SO₂NR³R^3a, CH₂SO₂NR³R^3a, NR³SO₂—

C₁₄ alkyl, CH₂NR³SO₂—

C_1-4 alkyl, NR³SO₂-phenyl, CH₂NR³SO₂-phenyl, S(O)_pCF₃, CH₂S(O)_pCF₃, S(O)_p—

C_1-4 alkyl, CH₂S(O)_p—

C_1-4 alkyl, S(O)_p-phenyl, CH₂S(O)_p-phenyl, and CF₃;

R^4c, at each occurrence, is selected from H, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, CH₂OR², CH₂F, CH₂Br, CH₂Cl, CH₂CN, CH₂NO₂, CH₂NR²R^2a, C(O)R^c, CH₂C(O)R^2c, CH₂NR²C(O)R^2b, C(O)NR²R^2a, CH₂C(O)NR²R^2a, SO₂NR²R^2a, CH₂SO₂NR²R^2a, S(O)_pR^5a, CH₂S(O)_pR^5a, CF₃, phenyl substituted with 0-1 R⁵, and benzyl substituted with 0-1 R⁵;

R⁵, at each occurrence, is selected from H, ═

O, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, OR³, CH₂OR³, F, Cl, —

CN, NO₂, NR³R^3a, CH₂NR³R^3a, C(O)R³, CH₂C(O)R³, C(O)OR^3c, CH₂C(O)OR^3c, NR³C(O)R^3a, C(O)NR³R^3a, SO₂NR³R^3a, NR³SO₂—

C_1-4 alkyl, NR³SO₂CF₃, NR³SO₂-phenyl, S(O)_pCF₃, S(O)_p—

C_1-4 alkyl, S(O)_p-phenyl, CF₃, phenyl substituted with 0-2 R⁶, naphthyl substituted with 0-2 R⁶, and benzyl substituted with 0-2 R⁶; and

,

R⁶, at each occurrence, is selected from H, OH, OR², F, Cl, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, —

CN, NO₂, NR²R^2a, CH₂NR²R^2a, C(O)R^2b, CH₂C(O)R^2b, NR²C(O)R^2b, SO₂NR²R^2a, and NR²SO₂C_1-4 alkyl.

4. A compound according to claim 3, wherein;

G is selected from the group;

G₁ is absent or is selected from CH₂, CH₂CH₂, CH₂O, OCH₂, NH, CH₂NH, NHCH₂, CH₂C(O), C(O)CH₂, C(O)NH, NHC(O), CH₂S(O)₂, S(O)₂(CH₂), SO₂NH, and NHSO₂, provided that G₁ does not form a N—

S, NCH₂N, NCH₂O, or NCH₂S bond with either group to which it is attached;

R^1a is selected from H, R^1b, C(CH₃)₂R^1b, and CH₂R^1b, provided that R^1a forms other than an N-halo, N—

S, or N—

CN bond;

R^1b is selected from CH₃, CH₂CH₃, F, Cl, Br, —

CN, CF₃, OR², NR²R^2a, C(O)R^2b, CO₂R^2b, CO₂R^2a, S(O)_pR², C(O)NR²R^2a, SO₂NR²R^2a, NR²SO₂R², and 5-6 membered aromatic heterocycle consisting of carbon atoms and from 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-2 R^4b, provided that R^1b forms other than an O—

O, N-halo, N—

S, or N—

CN bond;

R², at each occurrence, is selected from H, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, phenyl substituted with 0-1 R^4b, benzyl substituted with 0-1 R^4b, and 5-6 membered aromatic heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-1 R^4b;

R^2a, at each occurrence, is selected from H, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, benzyl, phenyl substituted with 0-1 R^4b, and 5-6 membered aromatic heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-1 R^4b;

alternatively, R² and R^2a, together with the atom to which they are attached, combine to form a 5 or 6 membered saturated, partially saturated or unsaturated ring substituted with 0-1 R^4b and consisting of;

0-1 additional heteroatoms selected from the group consisting of N, O, and S(O)_p;

R^2b, at each occurrence, is selected from OCH₃, OCH₂CH₃, OCH₂CH₂CH₃, OCH(CH₃)₂, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, benzyl, phenyl substituted with 0-1 R^4b, and 5-6 membered aromatic heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-1 R^4b;

R^2c, at each occurrence, is selected from OH, OCH₃, OCH₂CH₃, OCH₂CH₂CH₃, OCH(CH₃)₂, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, benzyl, phenyl substituted with 0-1 R^4b, and 5-6 membered aromatic heterocycle containing from 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-1 R^4b;

R⁴, at each occurrence, is selected from OH, OR², CH₂OR², (CH₂)₂OR², F, Br, Cl, I, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, NR²R^2a, CH₂NR²R^2a, (CH₂)₂NR²R^2a, CF₃, and CF₂CF₃;

R^4a, at each occurrence, is selected from H, ═

O, CH₂OR², OR², F, Br, Cl, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, C(CH₃)₃, CH₂NR²R^2a, NR²R^2a, C(O)R^2c, NR²C(O)R^2b, C(O)NR²R^2a, SO₂NR²R^2a, and CF₃;

R^4b, at each occurrence, is selected from H, ═

O, OR³, CH₂OR³, F, Cl, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, —

CN, NO₂, NR³R^3a, CH₂NR³R^3a, C(O)R³, C(O)OR^3c, NR³C(O)R^3a, C(O)NR³R^3a, SO₂NR³R^3a, NR³SO₂—

C_1-4 alkyl, NR³SO₂-phenyl, S(O)_p—

C_1-4 alkyl, S(O)_p-phenyl, and CF₃;

R^4c, at each occurrence, is selected from H, CH₃, CH₂CH₃, phenyl substituted with 0-1 R⁵, and benzyl substituted with 0-1 R⁵;

R⁵, at each occurrence, is selected from H, ═

O, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, OR³, CH₂OR³, F, Cl, —

CN, NO₂, NR³R^3a, CH₂NR³R^3a, C(O)R³, C(O)OR^3c, NR³C(O)R^3a, C(O)NR³R^3a, SO₂NR³R^3a, NR³SO₂—

C_1-4 alkyl, NR³SO₂-phenyl, S(O)_p—

C_1-4 alkyl, S(O)_p-phenyl, CF₃, phenyl substituted with 0-2 R⁶, naphthyl substituted with 0-2 R⁶, and benzyl substituted with 0-2 R⁶; and

,

R⁶, at each occurrence, is selected from H, OH, OR², F, Cl, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, —

CN, NO₂, NR²R^2a, CH₂NR²R^2a, C(O)R^2b, CH₂C(O)R^2b, CH₂c(O)R^2b, NR²C(O)R^2b, and SO₂NR²R^2a.

5. A compound according to claim 4, wherein;

G is selected from;

A is selected from the group;

phenyl, 2-Cl-phenyl, 3-Cl-phenyl, 2-F-phenyl, 3-F-phenyl, 2-methylphenyl, 2-aminophenyl, and 2-methoxyphenyl;

B is attached to a different atom on A than M and is selected from the group;

R^1a is selected from H, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH₂F, CH₂Cl, Br, CH₂Br, —

CN, CH₂CN, CF₃, CH₂CF₃, OCH₃, CH₂OH, C(CH₃)₂OH, CH₂OCH₃, NH₂, CH₂NH₂, NHCH₃, CH₂NHCH₃, N(CH₃)₂, CH₂N(CH₃)₂, CO₂H, COCH₃, CO₂CH₃, CH₂CO₂CH₃, SCH₃, CH₂SCH₃, S(O)CH₃, CH₂S(O)CH₃, S(O)₂CH₃, CH₂S(O)₂CH₃, C(O)NH₂, CH₂C(O)NH₂, SO₂NH₂, CH₂SO₂NH₂, NHSO₂CH₃, CH₂NHSO₂CH₃, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridin-2-yl-N-oxide, pyridin-3-yl-N-oxide, pyridin-4-yl-N-oxide, imidazol-1-yl, CH₂-imidazol-1-yl, 4-methyl-oxazol-2-yl, 4-N,N-dimethylaminomethyl-oxazol-2-yl, 1,2,3,4-tetrazol-1-yl, 1,2,3,4-tetrazol-5-yl, CH₂-1,2,3,4-tetrazol-1-yl, and CH₂-1,2,3,4-tetrazol-5-yl, provided that R^1a forms other than an N-halo, N—

S, or N—

CN bond;

R², at each occurrence, is selected from H, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, phenyl substituted with 0-1 R^4b, benzyl substituted with 0-1 R^4b, and 5 membered aromatic heterocycle consisting of;

carbon atoms and 1-4 heteroatoms selected from the group consisting of N, O, and S(O)_p, and substituted with 0-1 R^4b;

R^2a, at each occurrence, is selected from H, CH₃, and CH₂CH₃;

alternatively, R² and R^2a, together with the atom to which they are attached, combine to form a 5 or 6 membered saturated, partially saturated or unsaturated ring substituted with 0-1 R^4b and consisting of;

0-1 additional heteroatoms selected from the group consisting of N, O, and S(O)_p;

R^2b, at each occurrence, is selected from OCH₃, OCH₂CH₃, CH₃, and CH₂CH₃;

R^2c, at each occurrence, is selected from OH, OCH₃, OCH₂CH₃, CH₃, and CH₂CH₃;

R^4a, at each occurrence, is selected from H, ═

O, CH₃, CH₂CH₃, CH₂CH₂CH₃, CH(CH₃)₂, CH₂CH₂CH₂CH₃, CH₂CH(CH₃)₂, CH(CH₃)CH₂CH₃, and C(CH₃)₃;

R^4b, at each occurrence, is selected from H, ═

O, OR³, CH₂OR³, F, Cl, CH₃, CH₂CH₃, NR³R^3a, CH₂NR³R^3a, C(O)R³, C(O)OR^3c, NR³C(O)R^3a, C(O)NR³R^3a, SO₂NR³R^3a, NR³SO₂-phenyl, S(O)₂CH₃, S(O)₂-phenyl, and CF₃;

R⁵, at each occurrence, is selected from H, ═

O, CH₃, CH₂CH₃, OR³, CH₂OR³, F, Cl, NR³R^3a, CH₂NR³R^3a, C(O)R³, C(O)OR^3c, NR³C(O)R^3a, C(O)NR³R^3a, SO₂NR³R^3a, NR³SO₂—

C_1-4 alkyl, NR³SO₂-phenyl, S(O)₂—

CH₃, S(O)_p-phenyl, CF₃, phenyl substituted with 0-2 R⁶, naphthyl substituted with 0-2 R⁶, and benzyl substituted with 0-2 R⁶; and

,

R⁶, at each occurrence, is selected from H, OH, OR², F, Cl, CH₃, CH₂CH₃, NR²R^2a, CH₂NR²R^2a, C(O)R^2b, CH₂C(O)R^2b, NR²C(O)R^2b, and SO₂NR²R²a.

6. A compound according to claim 5, wherein the compound is

P₄ is —

G;

G is selected from;

 

and,

A—

B is selected from;

7. A compound according to claim 6, wherein:

A—

B is selected from;

8. A compound according to claim 1, wherein the compound is selected from the group:

3-methoxy-1-(4-methoxyphenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-1,4,5,6-tetrahydro-7-H-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxyphenyl)-3-[(methylamino)methyl]-6-[4-(2-oxo-1-piperidinyl)phenyl]-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-(3-chloro-4-fluorophenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridine-7-one;

1-[3-(aminomethyl)-4-fluorophenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridine-7-one;

1-(3-amino-1,2-benzisoxazol-5-yl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridine-7-one;

1-(4-methoxyphenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carbonitrile;

1-(4-methoxyphenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(1H-tetraazol-5-yl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl-4,5,6,7-tetrahydro-1H-pyrazole-[3,4-c]pyridine-3-carboxamide;

3-bromo-1-(4-methoxyphenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxyphenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(4-pyridinyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxyphenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(4-pyridinyl-N-oxide)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxyphenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(3-pyridinyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxyphenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(3-pyridinyl-N-oxide)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxyphenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(2-pyridinyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]-7-one;

1-(4-methoxyphenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1(2H)-pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide;

1-(4-methoxyphenyl)-3-(methylsulfonyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxyphenyl)-6-(4-(2-oxo-1(2H)-pyridinyl)phenyl]-3-(2-pyridinyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-[3-(aminomethyl)phenyl]-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

3-[7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide;

1-(3-chlorophenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide;

1-(3-chlorophenyl)-7-oxo-6-[4-(2-oxo-1(2H)pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide;

1-(3-chlorophenyl)-N,N-dimethyl-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide;

1-(3-chloro-4-fluorophenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide;

1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1(2H)-pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carbonitrile;

1-(3-amino-1H-indazol-5-yl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide;

1-(3-amino-1,2-benzisoxazol-5-yl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide;

1-(2,3-dihydro-1H-indol-6-yl)-6-[4-(2-oxo-1(2H)-pyridinyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-(2,3-dihydro-1H-indol-6-yl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-(2,3-dihydro-1H-isoindol-5-yl)-6-[4-(2-oxo-2H-pyridin-1-yl)phenyl]-3-trifluoromethyl-1,4,5,6-tetrahydropyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxyphenyl)-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-3-(2-pyrrolidin-1-ylmethyl-phenyl)-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one;

ethyl 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1(2H)-pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylate;

1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1(2H)-pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid;

1-(4-methoxyphenyl)-N,N-dimethyl-7-oxo-6-[4-(2-oxo-1(2H)-pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide;

N-({1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1(2H)-pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-3-yl}carbonyl)methanesulfonamide;

1-(4-hydroxy-phenyl)-7-oxo-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid amide;

1-(4-methoxyphenyl)-6-[4-(2-oxo-1(2H)-pyridinyl)phenyl]-3-(1H-tetraazol-5-yl)-1,4,5,6,-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

3-{4-[dimethylamino)methyl]-1,3-oxazol-2-yl}-1-(4-methoxyphenyl)-6-[4-(2-oxo-1(2H)-pyridinyl)phenyl]-1,4,5,6,-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

3-{4-[dimethylamino)methyl]-1,3-oxazol-2-yl }-1-(4-methoxyphenyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-1,4,5,6,-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxy-phenyl)-3-(4-methyl-oxazol-2-yl)-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxy-phenyl)-3-(4-methyl-oxazol-2-yl)-6-[4-(2-oxo-2H-1-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one;

3-acetyl-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one;

3-(4,5-dihydro-1H-imidazol-2-yl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxy-phenyl)-3-(1-methyl-4,5-dihydro-1H-imidazol-2-yl)-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxy-phenyl)-3-(1-methyl-1H-imidazol-2-yl)-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one;

1-(4-methoxy-phenyl)-3-methyl-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one;

3-hydroxymethyl-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one;

3-(1-hydroxy-1-methyl-ethyl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-1,4,5,6-tetrahydropyrazolo[3,4-c]pyridin-7-one;

3-(1-hydroxy-1-methyl-ethyl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one;

2-dimethylamino-N-{1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-3-ylmethyl}-N-methylacetamide;

2-dimethylamino-N-{1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-3-ylmethyl}acetamide;

N-{1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-3-ylmethyl}-2-pyridin-2-yl-acetamide;

N-{1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-3-ylmethyl}-2-(1-oxypyridin-2-yl)acetamide;

N-hydroxy-3-{7-oxo-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridin-1-yl}-benzamidine;

N-methoxy-3-{7-oxo-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridin-1-yl}-benzamidine;

1-(3-cyano-4-fluorophenyl-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridine-3-carboxamide;

1-(3-aminomethyl-4-fluoro-phenyl)-7-oxo-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid amide;

2-{7-oxo-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridin-1-yl}-benzenesulfonamide;

2-{7-oxo-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridin-1-yl}-benzenesulfonamide;

N-acetyl-2-{7-oxo-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridin-1-yl}-benzenesulfonamide;

1-(3-chloro-phenyl)-3-methanesulfonyl-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one;

1-(3-chloro-phenyl)-3-methanesulfonyl-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one;

1-(3-chloro-phenyl)-3-(1-hydroxy-1-methyl-ethyl)-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one; and

,

3-{7-oxo-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridin-1-yl}-benzamide;

or a pharmaceutically acceptable salt form thereof.

9. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt form thereof.

10. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt form thereof.

11. A method according to claim 10, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

12. A method according to claim 10, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

13. A compound according to claim 8, wherein the compound is:

1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl-4,5,6,7-tetrahydro-1H-pyrazole-[3,4-c]pyridine-3-carboxamide

or a pharmaceutically acceptable salt form thereof.

14. A compound according to claim 8, wherein the compound is:

1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1(2H)-pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide

or a pharmaceutically acceptable salt form thereof.

15. A compound according to claim 8, wherein the compound is:

1-(4-methoxyphenyl)-3-(methylsulfonyl)-6-[4-(2-oxo-1-piperidinyl)phenyl]-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one

or a pharmaceutically acceptable salt form thereof.

16. A compound according to claim 8, wherein the compound is:

1-(3-chlorophenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide

or a pharmaceutically acceptable salt form thereof.

17. A compound according to claim 8, wherein the compound is:

1-(3-chlorophenyl)-7-oxo-6-[4-(2-oxo-1(2H)pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide

or a pharmaceutically acceptable salt form thereof.

18. A compound according to claim 8, wherein the compound is:

1-(4-methoxyphenyl)-N,N-dimethyl-7-oxo-6-[4-(2-oxo-1(2H)-pyridinyl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide

or a pharmaceutically acceptable salt form thereof.

19. A compound according to claim 8, wherein the compound is:

3-(1-Hydroxy-1-methyl-ethyl)-1-(4-methoxy-phenyl)-6-[4-(2-oxo-2H-pyridin-1-yl)-phenyl]-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one

or a pharmaceutically acceptable salt form thereof.

20. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 2 or a pharmaceutically acceptable salt form thereof.

21. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 3 or a pharmaceutically acceptable salt form thereof.

22. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 4 or a pharmaceutically acceptable salt form thereof.

23. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 5 or a pharmaceutically acceptable salt form thereof.

24. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 6 or a pharmaceutically acceptable salt form thereof.

25. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 7 or a pharmaceutically acceptable salt form thereof.

26. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 8 or a pharmaceutically acceptable salt form thereof.

27. A pharmaceutical composition, comprising;

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 13 or a pharmaceutically acceptable salt form thereof.

28. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 14 or a pharmaceutically acceptable salt form thereof.

29. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 15 or a pharmaceutically acceptable salt form thereof.

30. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 16 or a pharmaceutically acceptable salt form thereof.

31. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 17 or a pharmaceutically acceptable salt form thereof.

32. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 18 or a pharmaceutically acceptable salt form thereof.

33. A pharmaceutical composition, comprising:

a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 19 or a pharmaceutically acceptable salt form thereof.

34. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 2 or a pharmaceutically acceptable salt form thereof.

35. A method according to claim 34, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

36. A method according to claim 34, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

37. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 3 or a pharmaceutically acceptable salt form thereof.

38. A method according to claim 37, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

39. A method according to claim 37, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

40. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 4 or a pharmaceutically acceptable salt form thereof.

41. A method according to claim 40, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

42. A method according to claim 40, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

43. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 5 or a pharmaceutically acceptable salt form thereof.

44. A method according to claim 43, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

45. A method according to claim 43, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

46. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 6 or a pharmaceutically acceptable salt form thereof.

47. A method according to claim 46, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

48. A method according to claim 46, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism. kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

49. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 7 or a pharmaceutically acceptable salt form thereof.

50. A method according to claim 49, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

51. A method according to claim 49, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

52. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 8 or a pharmaceutically acceptable salt form thereof.

53. A method according to claim 52, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

54. A method according to claim 52, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

55. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 13 or a pharmaceutically acceptable salt form thereof.

56. A method according to claim 55, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

57. A method according to claim 55, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

58. A method according to claim 55, wherein the thromboembolic disorder is an acute coronary syndrome.

59. A method according to claim 55, wherein the thromboembolic disorder is stroke.

60. A method according to claim 55, wherein the thromboembolic disorder is deep vein thrombosis.

61. A method according to claim 55, wherein the thromboembolic disorder is pulmonary embolism.

62. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 14 or a pharmaceutically acceptable salt form thereof.

63. A method according to claim 62, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

64. A method according to claim 62, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

65. A method according to claim 62, wherein the thromboembolic disorder is an acute coronary syndrome.

66. A method according to claim 62, wherein the thromboembolic disorder is stroke.

67. A method according to claim 62, wherein the thromboembolic disorder is deep vein thrombosis.

68. A method according to claim 62, wherein the thromboembolic disorder is pulmonary embolism.

69. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 15 or a pharmaceutically acceptable salt form thereof.

70. A method according to claim 69, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

71. A method according to claim 69, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

72. A method according to claim 69, wherein the thromboembolic disorder is an acute coronary syndrome.

73. A method according to claim 69, wherein the thromboembolic disorder is stroke.

74. A method according to claim 69, wherein the thromboembolic disorder is deep vein thrombosis.

75. A method according to claim 69, wherein the thromboembolic disorder is pulmonary embolism.

76. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 16 or a pharmaceutically acceptable salt form thereof.

77. A method according to claim 76, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

78. A method according to claim 76, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial, embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass;

(e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

79. A method according to claim 76, wherein the thromboembolic disorder is an acute coronary syndrome.

80. A method according to claim 76, wherein the thromboembolic disorder is stroke.

81. A method according to claim 76, wherein the thromboembolic disorder is deep vein thrombosis.

82. A method according to claim 76, wherein the thromboembolic disorder is pulmonary embolism.

83. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 17 or a pharmaceutically acceptable salt form thereof.

84. A method according to claim 83, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

85. A method according to claim 83, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and Thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

86. A method according to claim 83, wherein the thromboembolic disorder is an acute coronary syndrome.

87. A method according to claim 83, wherein the thromboembolic disorder is stroke.

88. A method according to claim 83, wherein the thromboembolic disorder is deep vein thrombosis.

89. A method according to claim 83, wherein the thromboembolic disorder is pulmonary embolism.

90. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 18 or a pharmaceutically acceptable salt form thereof.

91. A method according to claim 90, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

92. A method according to claim 90, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

93. A method according to claim 90, wherein the thromboembolic disorder is an acute coronary syndrome.

94. A method according to claim 90, wherein the thromboembolic disorder is stroke.

95. A method according to claim 90, wherein the thromboembolic disorder is deep vein thrombosis.

96. A method according to claim 90, wherein the thromboembolic disorder is pulmonary embolism.

97. A method for treating a thromboembolic disorder, comprising:

administering to a patient in need thereof a therapeutically effective amount of a compound of claim 19 or a pharmaceutically acceptable salt form thereof.

98. A method according to claim 97, wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders, venous cardiovascular thromboembolic disorders, and thromboembolic disorders in the chambers of the heart.

99. A method according to claim 97, wherein the thromboembolic disorder is selected from unstable angina, an acute coronary syndrome, first myocardial infarction, recurrent myocardial infarction, ischemic sudden death, transient ischemic attack, stroke, atherosclerosis, peripheral occlusive arterial disease, venous thrombosis, deep vein thrombosis, thrombophlebitis, arterial embolism, coronary arterial thrombosis, cerebral arterial thrombosis, cerebral embolism, kidney embolism, pulmonary embolism, and thrombosis resulting from (a) prosthetic valves or other implants, (b) indwelling catheters, (c) stents, (d) cardiopulmonary bypass, (e) hemodialysis, or (f) other procedures in which blood is exposed to an artificial surface that promotes thrombosis.

100. A method according to claim 97, wherein the thromboembolic disorder is an acute coronary syndrome.

101. A method according to claim 97, wherein the thromboembolic disorder is stroke.

102. A method according to claim 97, wherein the thromboembolic disorder is deep vein thrombosis.

103. A method according to claim 97, wherein the thromboembolic disorder is pulmonary embolism.