Compounds for the treatment of Alzheimer's disease

• US 20060211860A1
• Filed: 03/07/2006
• Published: 09/21/2006
• Est. Priority Date: 06/30/2000
• Status: Active Grant

• Current Assignee: Elan Pharmaceuticals Incorporated (Perrigo Company PLC)
• Original Assignee: Elan Pharmaceuticals Incorporated (Perrigo Company PLC)
• Inventors: John, Varghese, Fang, Lawrence Y.
• Granted Patent: US 7,432,389 B2
• Time in Patent Office: Days
• US Class Current: 540/544
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 7/04 Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: C07C 215/28 and containing six-membered aromatic rings
• CPC Class Codes: C07C 233/78 with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
• CPC Class Codes: C07C 235/84 with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
• CPC Class Codes: C07C 239/20 having oxygen atoms of hydroxylamino groups etherified
• CPC Class Codes: C07C 243/22 having nitrogen atoms of hydrazine groups bound to carbon atoms of six-membered aromatic rings
• CPC Class Codes: C07C 243/28 to hydrogen atoms or to carbon atoms of a saturated carbon skeleton
• CPC Class Codes: C07C 271/16 to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
• CPC Class Codes: C07C 271/18 to carbon atoms of hydrocarbon radicals substituted by doubly-bound oxygen atoms
• CPC Class Codes: C07C 275/24 containing six-membered aromatic rings
• CPC Class Codes: C07C 311/03 having the nitrogen atoms of the sulfonamide groups bound to hydrogen atoms or to acyclic carbon atoms
• CPC Class Codes: C07C 311/05 to acyclic carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups
• CPC Class Codes: C07C 311/08 having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
• CPC Class Codes: C07C 311/13 the carbon skeleton containing six-membered aromatic rings
• CPC Class Codes: C07C 311/16 having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
• CPC Class Codes: C07C 311/37 : having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
• CPC Class Codes: C07C 317/44 : having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
• CPC Class Codes: C07C 323/60 : with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
• CPC Class Codes: C07D 211/60 : Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• CPC Class Codes: C07D 215/12 : with substituted hydrocarbon radicals attached to ring carbon atoms
• CPC Class Codes: C07D 277/04 : having no double bonds between ring members or between ring members and non-ring members
• CPC Class Codes: C07D 295/13 : to an acyclic saturated chain
• CPC Class Codes: C07D 303/36 : with hydrocarbon radicals, substituted by nitrogen atoms nitro, nitroso radicals C07D303/08
• CPC Class Codes: C07D 307/52 : Radicals substituted by nitrogen atoms not forming part of a nitro radical
• CPC Class Codes: C07D 307/54 : Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• CPC Class Codes: C07D 333/24 : Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Abstract

The present invention is substituted amines of formula (XV) useful in treating Alzheimer'"'"'s ease and other similar dise

Claims

1-30. -30. (canceled)

31. A protected compound of the formula (II)

32. A protected compound according to claim 31

where R₁ is:

—

(CH₂)_0-1—

(R_1-aryl), or

(CH₂)_n1—

(R_1-heteroaryl);

where R_N is;

R_N-1—

X_N—

, where X_N is selected from the group consisting of;

—

CO—

, and

—

SO₂—

,

where R_N-1 is selected from the group consisting of;

—

R_N-aryl, and

—

R_N-heteroaryl, or

—

CO—

CH(—

(CH₂)_0-2—

O—

R_N-1-10)—

(CH₂)_0-2—

R_N-aryl/R_N-heteroaryl);

where R_A is;

—

C₁-C₈ alkyl,

(CH₂)_0-3—

(C₃-C₇) cycloalkyl,

(CR_A-xR_A-y)_0-4—

R_A-aryl,

(CR_A-xR_A-y)_0-4—

R_A-heteroaryl,

(CR_A-xR_A-y)_0-4—

R_{A-heterocycle},

cyclopentyl or -cyclohexyl ring fused to R_A-aryl or R_A-heteroaryl or R_{A-heterocycle};

where R_B is;

—

C₁-C₈ alkyl,

—

(CH₂)_0-3—

(C₃-C₇) cycloalkyl,

—

(CR_A-xR_A-y)_0-4—

R_A-aryl,

—

(CR_A-xR_A-y)_0-4—

R_A-heteroaryl,

—

(CR_A-xR_A-y)_0-4—

R_{A-heterocycle},

-cyclopentyl or -cyclohexyl ring fused to R_A-aryl or R_A-heteroaryl or R_{A-heterocycle}.

33. A protected compound according to claim 31

where R₁ is:

—

(CH₂)—

(R_1-aryl), or

—

(CH₂)—

(R_1-heteroaryl);

where R₂ is —

H;

.

where R₃ is —

H;

where R_N is;

R_N-1—

X_N—

where X_N is;

—

CO—

,

where R_N-1 is selected from the group consisting of;

—

R_N-aryl, and

—

R_N-heteroaryl;

where R_A is;

—

C₁-C₈ alkyl,

—

(CH₂)_0-3—

(C₃-C₇) cycloalkyl,

—

(CR_A-xR_A-y)_0-4-R_A-aryl,

—

(CR_A-xR_A-y)_0-4—

R_A-heteroaryl,

—

(CR_A-xR_A-y)_0-4—

R_{A-heterocycle}, or

-cyclopentyl or -cyclohexyl ring fused to R_A-aryl or R_A-heteroaryl or R_{A-heterocycle};

where R_B is;

—

C₁-C₈ alkyl,

—

(CH₂)_0-3—

(C₃-C₇) cycloalkyl,

—

(CR_B-xR_B-y)_0-4—

R_B-aryl, or

—

(CR_B-xR_B-y)_0-4—

R_B-heteroaryl.

—

(CR_B-xR_B-y)_0-4—

R_{B-heterocycle},

-cyclopentyl or -cyclohexyl ring fused to R_B-aryl or R_B-heteroaryl or R_{B-heterocycle}.

34. A protected compound according to claim 31 where PROTECTING GROUP is t-butoxycarbonyl.

35. A protected compound according to claim 31 where PROTECTING GROUP is benzyloxycarbonyl.

36-147. -147. (canceled)