- NOVEL CHEMICAL COMPOUNDS
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This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with hYAK3 activity.
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Page/Page column 35
(2010/11/25)
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- 2-(4-Alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists
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With the aim of identifying structurally novel, centrally acting histamine H3 antagonists, a series of 2-(4-alkylpiperazin-1-yl)quinolines was prepared. Systematic variation of the substituents led to highly potent histamine H3 antagonists with low polar surface area and appropriate log P for blood-brain barrier penetration.
- Zaragoza, Florencio,Stephensen, Henrik,Peschke, Bernd,Rimvall, Karin
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p. 306 - 311
(2007/10/03)
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- Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
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The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
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- 6-Substituted 1H-quinolin-2-ones and 2-methoxy-quinolines: Synthesis and evaluation as inhibitors of steroid 5α reductases types 1 and 2
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A Negishi-type coupling reaction between 6-bromo-2-methoxyquinoline. (1a) and various 4-bromo-N,N'dialkyl-benzamides gave access to 6-substituted 2-methoxy-quinolines 1-3 and 1H-quinolin-2-ones 4-12. Most of these compound proved to be inhibitors of steroid 5α reductases with activity arid selectivity both being strongly dependent on the features of the heterocycle and the size of the N,N-dialkylamide substituent. The most active inhibitor for the human type 2 isozyme was 6-[4-(N,N-diisopropylcarbamoyl)phenyl]-1H-quinolin-2-one 4 (K(i) 800 ± 85 nM), showing mostly competitive inhibitory patterns. A type 1 selective inhibitor could be identified with 6-[4-(N,N-diisopropylcarbamoyl)phenyl]-N-methyl-quinolin-2-one (5, IC50 510 nM). (C) 2000 Editions scientifiques et medicales Elsevier SAS.
- Baston, Eckhard,Palusczak, Anja,Hartmann, Rolf W.
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p. 931 - 940
(2007/10/03)
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