- 3-PIPERIDIN-4-YL-INDOLE ORL-1 RECEPTOR MODULATORS
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The present invention is directed to novel 3-piperidin-4-yl-indole derivatives of formula (I) and forms thereof, wherein X, R1, R2, R3, R4 and R5 are as herein defined, pharmaceutical compositions thereof and use as ORL-1 receptor modulators for treating, preventing or ameliorating ORL-1 receptor mediated disorders and conditions.
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Page/Page column 50
(2008/06/13)
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- Pyrazole-based cathepsin S inhibitors with improved cellular potency
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High potency pyrazole-based noncovalent inhibitors of human cathepsin S (CatS) were developed by modification of the benzo-fused 5-membered ring heterocycles found in earlier series of CatS inhibitors. Although substitutions on this heterocyclic framework
- Wei, Jianmei,Pio, Barbara A.,Cai, Hui,Meduna, Steven P.,Sun, Siquan,Gu, Yin,Jiang, Wen,Thurmond, Robin L.,Karlsson, Lars,Edwards, James P.
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p. 5525 - 5528
(2008/03/11)
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- 3-SUBSTITUTED 3,4-DIHYDRO-THIENO[2,3-D]PYRIMIDINE-4-ONE-DERIVATIVES, PRODUCTION AND USE THEREOF
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The invention relates to 3,4-dihydro-thieno[2,3-d]pyrimidinde-4-one-derivatives which are substituted at 3-position with 5-membered heteroaryl which can be condensed with an aryl or heteroaryl radical. The heteroaryl and, optionally, the condensed aryl or heteroaryl radical 1,2 or 3 can independently include selected substitutents from C1-5-alkyl, C1-5-alkoxy, C1-5-alkylthio, halogen, CN, halogen-C1-5-alkyl, halogen-C1-5alkoxy, hydroxy, -NH2, -N(R6)2, -NH(R6), aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl, the substituents aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl 1,2 or 3 independently include selected substituents from C1-5-alkythio, halogen, CN, halogen-C1-5-alkyl, halogen-C1-5alkoxy, hydroxy, -NH2, -N(R6)2 and -NH(R6). The invention also relates to the production and use of said derivatives, especially for therapeutical purposes, e.g. in the treatment of depression.
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(2008/06/13)
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- AZAINDOLYLPIPERIDINE DERIVATIVES AS ANTIHISTAMINIC AND ANTIALLERGIC AGENTS
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This invention is directed to new potent and selective antagonists of H1 histamine receptors having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
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Page/Page column 22-23
(2008/06/13)
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