- The discovery of novel 3-aryl-indazole derivatives as peripherally restricted pan-Trk inhibitors for the treatment of pain
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The design, synthesis, and biological evaluation of novel 3-aryl-indazole derivatives as peripherally selective pan-Trk inhibitors are described. Three strategies were used to obtain a potent compound exhibiting low central nervous system (CNS) penetratio
- Shirahashi, Hiromitsu,Toriihara, Eisuke,Suenaga, Yoshihito,Yoshida, Hideyuki,Akaogi, Kensuke,Endou, Yukiko,Wakabayashi, Makoto,Takashima, Misato
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supporting information
p. 2320 - 2326
(2019/06/25)
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- P2X7 MODULATORS
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The present invention is directed to a compound of Formula (I) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
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Paragraph 0531; 0532
(2014/09/30)
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- PYRROLO[2,3-B]PYRIDINE CDK9 KINASE INHIBITORS
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Disclosed are compounds of Formula (IIa), wherein R1, R2, R3A, R3B, R3C, R3D, R3E, and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIa)
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Page/Page column 403
(2014/09/29)
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- N-ACYL PYRIDINE BIARYL COMPOUNDS AND THEIR USES
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The present invention provides a compound of general formula:wherein Z2-Z6 include one or two nitrogen atoms as described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
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Page/Page column 143-144
(2012/08/08)
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- N-ACYL PYRIMIDINE BIARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS
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The present invention provides a compound of the general formula (1): wherein one of X and Y is N and the other is an optionally substituted carbon atom, and Z2-Z5 represent one or two nitrogen atoms, as further described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals and as components of pharmaceutical compositions. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds described herein or pharmaceutical compositions comprising such compounds.
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Page/Page column 185
(2012/08/08)
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- Spiro Compounds As NPY Y5 Receptor Antagonists
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The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R is an aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano;Z1 is H, C1-C4 alkyl or F;Z is CH2, CH(C1-C4 alkyl), C(C1-C4 alkyl)2 or a bond;A is a 6-10 membered aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or —C(═O)—X; or —O(CH2)0-1R1;B is hydrogen or is a 5-6 membered heteroaryl, or a 4-6 membered heterocycle, or phenyl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, hydroxyl, cyano; A and B being linked via any atom;R1 is —(C1-C4)alkyl(C1-C4)alkoxy; or C3-C8 cycloalkyl; or R1 is an aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or R1 is a 4-6 membered heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano;X is OR2 or NR3R4;R2 is C1-C4 alkyl;R3 is hydrogen or together with R4 and the nitrogen form a 5-6 saturated membered ring;R4 is C3-C8 cycloalkyl; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.
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Page/Page column 43
(2009/08/18)
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