Pyrazole Derivatives as Modulators of the 5-Ht2a Serotonin Receptor Useful for the Treatment of Disorders Related Thereto
First Claim
Patent Images
1. A compound of Formula (Ia):
-
or a pharmaceutically acceptable salt thereof, wherein;
R1 is selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl and C3-7 cycloalkyl;
R2 is selected from the group consisting of H, C2-6 alkenyl, C1-6 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, C1-6 alkylsulfonamide, carbo-C1-6-alkoxy, carboxamide, carboxy, cyano, C3-7 cycloalkyl, C2-8 dialkylcarboxamide, and halogen;
R3 is selected from the group consisting of H, C1-6 acyl, C1-6 acyloxy, C2-6 alkenyl, C1-6 alkoxy, C1-6 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, C1-6 alkylsulfonamide, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, C1-6 alkylthio, C1-6 alkylureyl, amino, C1-6 alkylamino, C2-8 dialkylamino, carbo-C1-6-alkoxy, carboxamide, carboxy, cyano, C3-7 cycloalkyl, C2-8 dialkylcarboxamide, C2-8 dialkylsulfonamide, halogen, C1-6 haloalkoxy, C1-6 haloalkyl, C1-6 haloalkylsulfinyl, C1-6 haloalkylsulfonyl, C1-6 haloalkylthio, hydroxyl, thiol, nitro and sulfonamide;
R4, R5, R6, and R7 are each independently selected from the group consisting of H, C1-6 acyl, C1-6 acyloxy, C2-6 alkenyl, C1-6 alkoxy, C1-6 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, C1-6 alkylsulfonamide, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, C1-6 alkylthio, C1-6 alkylureyl, amino, C1-6 alkylamino, C2-8 dialkylamino, carbo-C1-6-alkoxy, carboxamide, carboxy, cyano, C3-7 cycloalkyl, C2-8 dialkylcarboxamide, C2-8 dialkylsulfonamide, halogen, C1-6 haloalkoxy, C1-6 haloalkyl, C1-6 haloalkylsulfinyl, C1-6 haloalkylsulfonyl, C1-6 haloalkylthio, hydroxyl, thiol, nitro and sulfonamide;
X is —
NR8C(═
O)—
, —
C(═
O)NR8, —
NR9—
, —
C(═
O)—
, —
O—
, —
S—
, —
S(═
O)—
or —
S(═
O)2—
;
wherein R8 is H or C1-6 alkyl; and
R9 is selected from the group consisting of H, C1-6 acyl, C2-6 alkenyl, C1-6 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, C1-6 alkylsulfonyl, carbo-C1-6-alkoxy, and C3-7 cycloalkyl, each optionally substituted with halogen;
Y is —
NR10C(═
O)—
, —
C(═
O)NR10, —
NR10S(═
O)2—
, —
S(═
O)2NR10—
, —
NR10C(═
O)NR11—
, —
NR10C(═
O)O—
, —
OC(═
O)NR10—
, —
NR12—
, —
C(═
O)—
, —
O—
, —
S—
, —
S(═
O)—
, —
S(═
O)2—
or absent;
wherein R10 and R11 are each independently H or C1-6 alkyl; and
R12 is selected from the group consisting of H, C1-6 acyl, C2-6 alkenyl, C1-6 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, C1-6 alkylsulfonyl, carbo-C1-6-alkoxy, and C3-7 cycloalkyl, each optionally substituted with halogen;
Ar is aryl or heteroaryl each optionally substituted with R13 to R17 substituents selected independently from the group consisting of C1-6 acyl, C1-6 acyloxy, C2-6 alkenyl, C1-6 alkoxy, C1-8 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, C1-6 alkylsulfonamide, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, C1-6 alkylthio, C1-6 alkylureyl, amino, C1-6 alkylamino, C2-8 dialkylamino, carbo-C1-6-alkoxy, carboxamide, carboxy, cyano, C3-7 cycloalkyl, C2-8 dialkylcarboxamide, C2-8 dialkylsulfonamide, halogen, C1-6 haloalkoxy, C1-6 haloalkyl, C1-6 haloalkylsulfinyl, C1-6 haloalkylsulfonyl, C1-6 haloalkylthio, hydroxyl, thiol, nitro and sulfonamide;
or two adjacent substituents together with said aryl or said heteroaryl form a C5-7 cycloalkyl optionally comprising 1 to 2 oxygen atoms.
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Abstract
The present invention relates to certain pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette'"'"'s syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
82 Citations
55 Claims
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1. A compound of Formula (Ia):
-
or a pharmaceutically acceptable salt thereof, wherein;
R1 is selected from the group consisting of C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl and C3-7 cycloalkyl;
R2 is selected from the group consisting of H, C2-6 alkenyl, C1-6 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, C1-6 alkylsulfonamide, carbo-C1-6-alkoxy, carboxamide, carboxy, cyano, C3-7 cycloalkyl, C2-8 dialkylcarboxamide, and halogen;
R3 is selected from the group consisting of H, C1-6 acyl, C1-6 acyloxy, C2-6 alkenyl, C1-6 alkoxy, C1-6 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, C1-6 alkylsulfonamide, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, C1-6 alkylthio, C1-6 alkylureyl, amino, C1-6 alkylamino, C2-8 dialkylamino, carbo-C1-6-alkoxy, carboxamide, carboxy, cyano, C3-7 cycloalkyl, C2-8 dialkylcarboxamide, C2-8 dialkylsulfonamide, halogen, C1-6 haloalkoxy, C1-6 haloalkyl, C1-6 haloalkylsulfinyl, C1-6 haloalkylsulfonyl, C1-6 haloalkylthio, hydroxyl, thiol, nitro and sulfonamide;
R4, R5, R6, and R7 are each independently selected from the group consisting of H, C1-6 acyl, C1-6 acyloxy, C2-6 alkenyl, C1-6 alkoxy, C1-6 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, C1-6 alkylsulfonamide, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, C1-6 alkylthio, C1-6 alkylureyl, amino, C1-6 alkylamino, C2-8 dialkylamino, carbo-C1-6-alkoxy, carboxamide, carboxy, cyano, C3-7 cycloalkyl, C2-8 dialkylcarboxamide, C2-8 dialkylsulfonamide, halogen, C1-6 haloalkoxy, C1-6 haloalkyl, C1-6 haloalkylsulfinyl, C1-6 haloalkylsulfonyl, C1-6 haloalkylthio, hydroxyl, thiol, nitro and sulfonamide;
X is —
NR8C(═
O)—
, —
C(═
O)NR8, —
NR9—
, —
C(═
O)—
, —
O—
, —
S—
, —
S(═
O)—
or —
S(═
O)2—
;
wherein R8 is H or C1-6 alkyl; and
R9 is selected from the group consisting of H, C1-6 acyl, C2-6 alkenyl, C1-6 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, C1-6 alkylsulfonyl, carbo-C1-6-alkoxy, and C3-7 cycloalkyl, each optionally substituted with halogen;
Y is —
NR10C(═
O)—
, —
C(═
O)NR10, —
NR10S(═
O)2—
, —
S(═
O)2NR10—
, —
NR10C(═
O)NR11—
, —
NR10C(═
O)O—
, —
OC(═
O)NR10—
, —
NR12—
, —
C(═
O)—
, —
O—
, —
S—
, —
S(═
O)—
, —
S(═
O)2—
or absent;
wherein R10 and R11 are each independently H or C1-6 alkyl; and
R12 is selected from the group consisting of H, C1-6 acyl, C2-6 alkenyl, C1-6 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, C1-6 alkylsulfonyl, carbo-C1-6-alkoxy, and C3-7 cycloalkyl, each optionally substituted with halogen;
Ar is aryl or heteroaryl each optionally substituted with R13 to R17 substituents selected independently from the group consisting of C1-6 acyl, C1-6 acyloxy, C2-6 alkenyl, C1-6 alkoxy, C1-8 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, C1-6 alkylsulfonamide, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, C1-6 alkylthio, C1-6 alkylureyl, amino, C1-6 alkylamino, C2-8 dialkylamino, carbo-C1-6-alkoxy, carboxamide, carboxy, cyano, C3-7 cycloalkyl, C2-8 dialkylcarboxamide, C2-8 dialkylsulfonamide, halogen, C1-6 haloalkoxy, C1-6 haloalkyl, C1-6 haloalkylsulfinyl, C1-6 haloalkylsulfonyl, C1-6 haloalkylthio, hydroxyl, thiol, nitro and sulfonamide;
or two adjacent substituents together with said aryl or said heteroaryl form a C5-7 cycloalkyl optionally comprising 1 to 2 oxygen atoms.- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 55)
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3. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein Y is bonded at the 4-position on said phenyl ring.
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4. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein R1 is CH3.
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5. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein R2 is H, F, Cl or Br.
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6. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein R3 is H.
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7. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein R4, R5, R6, and R7 are each independently selected from the group consisting of H, C1-6 alkoxy, C1-6 alkyl, and halogen.
-
8. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein X is —
- NH—
.
- NH—
-
9. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein Y is absent.
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10. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein Ar is aryl or heteroaryl each optionally substituted with R13 to R17 substituents selected independently from the group consisting of C1-6 acyl, C1-6 alkoxy, C1-8 alkyl, C1-6 alkylcarboxamide, C2-6 alkynyl, C1-6 alkylsulfonyl, C2-8 dialkylamino, carbo-C1-6-alkoxy, carboxamide, carboxy, cyano, C3-7 cycloalkyl, halogen, C1-6 haloalkoxy, C1-6 haloalkyl, C1-6 haloalkylsulfonyl, hydroxyl, and sulfonamide;
- or two adjacent substituents together with said aryl or said heteroaryl form a C5-7 cycloalkyl optionally comprising 1 to 2 oxygen atoms.
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11. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein Ar is selected from the group consisting of phenyl, 2-fluoro-phenyl, 3-fluoro-phenyl, 4-fluoro-phenyl, 3-chloro-phenyl, 4-chloro-phenyl, 4-methyl-phenyl, 4-n-propyl-phenyl, 4-tert-butyl-phenyl, 4-heptyl-phenyl, 4-methoxy-phenyl, 2-trifluoromethyl-phenyl, 3-trifluoromethyl-phenyl, 4-trifluoromethyl-phenyl, 3-trifluoromethoxy-phenyl, 4-trifluoromethoxy-phenyl, 3-acetyl-phenyl, 4-nitro-phenyl, 3-amino-phenyl, 2,3-difluoro-phenyl, 3,5-difluoro-phenyl, 3,4-difluoro-phenyl, 4-fluoro-2-methyl-phenyl, 3-fluoro-4-methyl-phenyl, 4-fluoro-3-methyl-phenyl, 3-fluoro-4-methoxy-phenyl, 3,4-dichloro-phenyl, 2-chloro-4-methyl-phenyl, 3-chloro-4-trifluoromethyl-phenyl, 2,4-bis-trifluoromethyl-phenyl, benzo[1,3]dioxol-5-yl and 2,6-dimethoxy-phenyl.
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12. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein Ar is selected from the group consisting of thiophen-2-yl, thiophen-3-yl, 3,5-dimethyl-isoxazol-4-yl, pyridin-3-yl, 6-methoxy-pyridin-3-yl, pyridin-4-yl and quinolin-8-yl.
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13. The compound according to claim 1 having Formula (Im):
wherein;
R1 is CH3;
R2 is H, F, Cl or Br;
R3 is H;
R4, R5, R6, and R7 are each independently selected from the group consisting of H, OCH3, CH3 and F; and
Ar is aryl or heteroaryl each optionally substituted with R13 to R17 substituents selected independently from the group consisting of C(═
O)CH3, OCH3, CH3, amino, F, Cl, Br, OCF3, CF3 and nitro;
or two adjacent substituents together with said aryl form a C5 cycloalkyl comprising 2 oxygen atoms;
or a pharmaceutically acceptable salt thereof.
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14. The compound according to claim 1 having Formula (Im):
wherein;
R1 is CH3;
R2 is H, F, Cl or Br;
R3 is H;
R4, R5, R6, and R7 are each independently selected from the group consisting of H, OCH3, CH3 and F; and
Ar is phenyl, thiophen-2-yl, thiophen-3-yl, isoxazol-4-yl, pyridin-3-yl, pyridin-4-yl or quinolin-8-yl each optionally substituted with R13 to R17 substituents selected independently from the group consisting of C(═
O)CH3, OCH3, CH3, amino, F, Cl, Br, OCF3, CF3 and nitro;
or two adjacent substituents together with said aryl form a C5 cycloalkyl comprising 2 oxygen atoms;
or a pharmaceutically acceptable salt thereof.
-
15. The compound according to claim 1 wherein the compound is selected from the group consisting of:
-
Biphenyl-4-yl-(4-bromo-2-methyl-2H-pyrazol-3-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(2′
-fluoro-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(3′
-fluoro-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-fluoro-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(2-fluoro-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(2-methyl-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(3′
-chloro-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-chloro-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-methyl-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-propyl-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-tert-butyl-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-heptyl-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-methoxy-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(2′
-trifluoromethyl-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(3′
-trifluoromethyl-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-trifluoromethyl-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(3′
-trifluoromethoxy-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-trifluoromethoxy-biphenyl-4-yl)-amine;
1-[4′
-(4-Bromo-2-methyl-2H-pyrazol-3-ylamino)-biphenyl-3-yl]-ethanone;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-nitro-biphenyl-4-yl)-amine;
N4′
-(4-Bromo-2-methyl-2H-pyrazol-3-yl)-biphenyl-3,4′
-diamine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(2′
,3′
-difluoro-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(3′
,5′
-difluoro-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(3′
,4′
-difluoro-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(3,3′
,4′
-trifluoro-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-fluoro-2′
-methyl-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(3′
-fluoro-4′
-methyl-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-fluoro-3′
-methyl-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(3′
-fluoro-4′
-methoxy-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(3′
,4′
-dichloro-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(2′
-chloro-5′
-methyl-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(5′
-chloro-2′
-methyl-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(3′
-chloro-4′
-trifluoromethyl-biphenyl-4-yl)-amine;
(2′
,4′
-Bis-trifluoromethyl-biphenyl-4-yl)-(4-bromo-2-methyl-2H-pyrazol-3-yl)-amine;
(4′
-Fluoro-biphenyl-4-yl)-(2-methyl-2H-pyrazol-3-yl)-amine;
(2,5-Dimethyl-2H-pyrazol-3-yl)-(4′
-fluoro-biphenyl-4-yl)-amine;
(4-Bromo-1-methyl-1H-pyrazol-3-yl)-(4′
-fluoro-biphenyl-4-yl)-amine;
(4-Benzo[1,3]dioxol-5-yl-phenyl)-(4-bromo-2-methyl-2H-pyrazol-3-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4-phenoxy-phenyl)-amine;
[4-(4-Bromo-2-methyl-2H-pyrazol-3-ylamino)-phenyl]-phenyl-methanone;
1-[4-(4-Bromo-2-methyl-2H-pyrazol-3-ylamino)-phenyl]-3-(4-chloro-phenyl)-urea;
Biphenyl-2-yl-(4-bromo-2-methyl-2H-pyrazol-3-yl)-amine;
Biphenyl-3-yl-(4-bromo-2-methyl-2H-pyrazol-3-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(2′
-fluoro-biphenyl-3-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-methoxy-biphenyl-3-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4′
-trifluoromethoxy-biphenyl-3-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(3-methoxy-4′
-trifluoromethoxy-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(3′
-fluoro-3-methoxy-biphenyl-4-yl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(2′
,6′
-dimethoxy-biphenyl-3-yl)-amine;
Biphenyl-4-carboxylic acid (4-bromo-2-methyl-2H-pyrazol-3-yl)-amide;
4′
-Fluoro-biphenyl-4-carboxylic acid (4-bromo-2-methyl-2H-pyrazol-3-yl)-amide;
4′
-Trifluoromethoxy-biphenyl-4-carboxylic acid (4-bromo-2-methyl-2H-pyrazol-3-yl)-amide;
4′
-Fluoro-biphenyl-3-carboxylic acid (4-bromo-2-methyl-2H-pyrazol-3-yl)-amide; and
4′
-Trifluoromethyl-biphenyl-3-carboxylic acid (4-bromo-2-methyl-2H-pyrazol-3-yl)-amide;
or a pharmaceutically acceptable salt thereof.
-
-
16. The compound according to claim 1 wherein the compound is selected from the group consisting of:
-
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4-thiophen-2-yl-phenyl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4-thiophen-3-yl-phenyl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-[4-(3,5-dimethyl-isoxazol-4-yl)-phenyl]-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4-pyridin-3-yl-phenyl)-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-[4-(6-methoxy-pyridin-3-yl)-phenyl]-amine;
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4-pyridin-4-yl-phenyl)-amine; and
(4-Bromo-2-methyl-2H-pyrazol-3-yl)-(4-quinolin-8-yl-phenyl)-amine;
or a pharmaceutically acceptable salt thereof.
-
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17. A pharmaceutical composition comprising a compound according to any one of claims 1 to 16, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
-
18. A method for treating a 5-HT2A mediated disorder in an individual comprising administering to said individual in need thereof a therapeutically effective amount of a compound according to any one of claims 1 to 16, or a pharmaceutically acceptable salt thereof.
-
19. The method according to claim 18, wherein said 5-HT2A mediated disorder is selected from the group consisting of coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, and atrial fibrillation.
-
20. A method for treating a condition associated with platelet aggregation in an individual comprising administering to said individual in need thereof a therapeutically effective amount of a compound according to any one of claims 1 to 16, or a pharmaceutically acceptable salt thereof.
-
21. A method for reducing the risk of blood clot formation in an angioplasty or coronary bypass surgery individual comprising administering to said individual in need thereof a therapeutically effective amount of a compound according to any one of claims 1 to 16, or a pharmaceutically acceptable salt thereof.
-
22. A method for reducing the risk of blood clot formation in an individual suffering from atrial fibrillation, comprising administering to said individual in need thereof a therapeutically effective amount of a compound according to any one of claims 1 to 16, or a pharmaceutically acceptable salt thereof.
-
23. A method for treating a sleep disorder in an individual comprising administering to said individual in need thereof a therapeutically effective amount of a compound according to any one of claims 1 to 16, or a pharmaceutically acceptable salt thereof.
-
24. The method according to claim 23, wherein said sleep disorder is a dyssomnia.
-
25. The method according to claim 23, wherein said sleep disorder is a parasomnia.
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26. A method for treating a diabetic-related disorder in an individual comprising administering to said individual in need thereof a therapeutically effective amount of a compound according to any one of claims 1 to 16, or a pharmaceutically acceptable salt thereof.
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27. A method for treating progressive multifocal leukoencephalopathy in an individual comprising administering to said individual in need thereof a therapeutically effective amount of a compound according to any one of claims 1 to 16, or a pharmaceutically acceptable salt thereof.
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28. A method for treating hypertension in an individual comprising administering to the individual in need thereof a therapeutically effective amount of a compound according to any one of claims 1 to 16, or a pharmaceutically acceptable salt thereof.
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29. A method for treating pain in an individual comprising administering to the individual in need thereof a therapeutically effective amount of a compound according to any one of claims 1 to 16, or a pharmaceutically acceptable salt thereof.
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55. A process for preparing a composition comprising admixing a compound according to any one of claims 1 to 16, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
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30-54. -54. (canceled)
Specification
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Current AssigneeArena Pharmaceuticals Incorporated
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Original AssigneeArena Pharmaceuticals Incorporated
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InventorsUnett, David, Teegarden, Bradley, Strah-Pleynet, Sonja
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Application NumberUS11/792,163Publication NumberTime in Patent OfficeDaysField of SearchUS Class Current514/314CPC Class CodesA61P 25/00 Drugs for disorders of the ...A61P 43/00 Drugs for specific purposes...A61P 9/00 Drugs for disorders of the ...C07D 231/38 Nitrogen atoms nitro radica...C07D 401/12 linked by a chain containin...C07D 405/12 linked by a chain containin...C07D 409/12 linked by a chain containin...C07D 413/12 linked by a chain containin...
