- ISOINDOLINONE COMPOUNDS
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Disclosed herein is a compound or pharmaceutically acceptable salts or stereoisomers thereof of of formula I wherein X1 is linear or branched C1-6 alkyl, C3-6 cycloalkyl, -C1-6 alkyl C3-6 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, C1-6 alkyl C6-10 aryl, C1-6 alkyl 5-10 membered heteroaryl, wherein X1 is unsubstituted or substituted with one or more of halogen, linear or branched C1-6 alkyl, linear or branched C1-6 heteroalkyl, CF3, CHF2, -O-CHF2, -O-(CH2)2-OMe, OCF3, C1-6 alkylamino, -CN, -N(H)C(O)-C1- 6alkyl, -OC(O)-C1-6alkyl, -OC(O)-C1-4alkylamino, -C(O)O-C1-6alkyl, -COOH, - CHO, -C1-6alkylC(O)OH, -C1-6alkylC(O)O-C1-6alkyl, NH2, C1-6 alkoxy or C1-6 alkylhydroxy; X2 is hydrogen, C6-10 aryl, 5-10 membered heteroaryl, -O-(5-10 membered heteroaryl), 4-8 membered heterocycloalkyl, C1-4 alkyl 4-8 membered heterocycloalkyl, -O-(4-8 membered heterocycloalkyl), -O-C1-4 alkyl-(4-8 membered heterocycloalkyl), -OC(O)-C1-4alkyl-4-8 membered heterocycloalkyl or C6 aryloxy, wherein X2 is unsubstituted or substituted with one or more of linear or branched C1-6 alkyl, NH2, NMe2 or 5-6 membered heterocycloalkyl; n is 0, 1 or 2.
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- COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
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Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are
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Page/Page column 60
(2012/02/06)
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- Discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB2 agonists
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Recently sulfamoyl benzamides were identified as a novel series of cannabinoid receptor ligands. Replacing the sulfonamide functionality and reversing the original carboxamide bond led to the discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB2 agonists. Selective CB2 agonist 31 (Ki = 2.7; CB1/CB2 = 190) displayed robust activity in a rodent model of postoperative pain.
- Worm, Karin,Weaver, Damian G.,Green, Rosalyn C.,Saeui, Christopher T.,Dulay, Doreen-Marie S.,Barker, William M.,Cassel, Joel A.,Stabley, Gabriel J.,DeHaven, Robert N.,LaBuda, Christopher J.,Koblish, Michael,Brogdon, Bernice L.,Smith, Steven A.,Dolle, Roland E.
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scheme or table
p. 5004 - 5008
(2010/03/24)
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- 3 , 5-SUBSTITΓUED PIPERIDINE COMPOUNDS AS RENIN INHIBITORS
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The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3, 5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The preferred compounds (which can also be present as salts) have the formula (I'), wherein R1 , R2, T, R3 and R4 are as defined in the specification.
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Page/Page column 212
(2008/06/13)
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- INDOLE DERIVATIVES
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Indole derivatives of the following formula: wherein R1 is carboxy(lower)alkyl or protected carboxy(lower)alkyl, R2 is hydrogen, lower alkyl or halogen, R3 and R4 are each hydrogen or lower alkyl, R5 is ar(lower)alkyl which may have suitable substituent(s), and A is carbonyl, sulfonyl or lower alkylene, or a pharmaceutically acceptable salt thereof, which are useful as a testosterone 5alpha-reductase inhibitor
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