- HEPATITIS B ANTIVIRAL AGENTS
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The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
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Page/Page column 211; 212
(2013/07/05)
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- Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists
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Melanin concentrating hormone (MCH) is an important mediator of energy homeostasis and plays a role in metabolic and CNS disorders. The modeling-supported design, synthesis and multi-parameter optimization (biological activity, solubility, metabolic stability, hERG) of novel quinazoline derivatives as MCHR1 antagonists are described. The in vivo proof of principle for weight loss with a lead compound from this series is exemplified. Clusters of refined hMCHR1 homology models derived from the X-ray structure of the β2-adrenergic receptor, including extracellular loops, were developed and used to guide the design.
- Sasmal, Sanjita,Balaji, Gade,Kanna Reddy, Hariprasada R.,Balasubrahmanyam,Srinivas, Gujjary,Kyasa, Shivakumar,Sasmal, Pradip K.,Khanna, Ish,Talwar, Rashmi,Suresh,Jadhav, Vikram P.,Muzeeb, Syed,Shashikumar, Dhanya,Harinder Reddy,Sebastian,Frimurer, Thomas M.,Rist, ?ystein,Elster, Lisbeth,H?gberg, Thomas
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scheme or table
p. 3157 - 3162
(2012/06/04)
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- 4-ARYLMORPHOLIN-3-ONE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC USE THEREOF
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The invention relates to compounds corresponding to formula (I): in which: Ar represents a mono- or disubstituted phenyl; R1 represents an unsubstituted or substituted phenyl; R2 represents: a pyridyl; an unsubstituted or substituted phenyl; a benzyl that is unsubstituted or substituted on the phenyl; R2 may moreover represent: a heterocyclic radical; R3 represents various values. The invention also comprises methods for the compounds preparation, formulations comprising them and therapeutic applications thereof.
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Page/Page column 20
(2008/06/13)
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- INDOLE DERIVATIVE AND USE FOR TREATMENT OF CANCER
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The present invention relates to a compound represented by the formula (I’) wherein A is a benzene ring optionally having substituents, R1, R2a and R3 are each a hydrogen atom, a hydrocarbon group optionally having substituents or a heterocyclic group optionally having substituents, R1 and R2a may form a ring via X, when R1 and R2a form a ring via X, R1 and R2a are each a bond or a divalent C1-5 acyclic hydrocarbon group optionally having substituents, and X is a bond, an oxygen atom, an optionally oxidized sulfur atom or an imino group optionally having a substituent, provided that R1, R2a and X are not bonds at the same time, or a salt thereof, and an agent for inhibiting kinase (phosphorylation enzyme), which contains this compound or a prodrug thereof. The compound of the present invention has an inhibitory activity against kinase such as a vascular endothelial growth factor receptor (VEGFR) and the like, and is useful as an agent for the prophylaxis or threatment of cancer and the like.
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Page/Page column 212
(2010/02/15)
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- Piperidine derivatives having renin inhibiting activity
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Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I wherein R1, R2, R3, R4, Q, X, Z, m and n are as described herein.
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- 1,3,8-TRIAZASPIRODECANE-4-ONES, PHARMACEUTICAL COMPOSITIONS THEREOF AND METHOD OF USE THEREOF
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Compounds of the formula STR1 where Q is defined hereinafter and X and Y are hydrogen, halogen, lower alkyl, nitro are useful as neuroleptics.
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- Studies on Psychotropic Agents. VI. Synthesis of 1'-Methylspiro-3-one and Related Compounds
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The title compounds (19) were synthesized by rearrangement of the 1-ethoxycarbonyl-4-aryl-3,4-epoxypiperidines (7) to give the 3-aryl-3-formylpyrrolidine derivatives (12) for pharmacological testing.Compound (19b) exhibited moderate central nervous system
- Nagai, Yasutaka,Hino, Katsuhiko,Uno, Hitoshi,Minami, Shinsaku
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p. 1387 - 1393
(2007/10/02)
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