- ISOQUINOLINONE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER
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The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt and/or solvate thereof, notably for use as a drug, notably in the treatment of cancer, as well as pharmaceutical compositions containing such a
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- Synthesis and SAR study of pyrrolo[3,4-b]pyridin-7(6H)-one derivatives as melanin concentrating hormone receptor 1 (MCH-R1) antagonists
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The discovery and optimization of novel pyrrolo[3,4-b]pyridin-7(6H)-one MCH-R1 antagonists are described. A systematic SAR study probing the effects of aryl-, benzyl- and arylthio-substituents at the 2-position of the pyrrolo[3,4-b]pyridin-7(6H)-ones led to identification of the 2-[(4-fluorophenyl)thio] derivative 7b as a highly potent MCH-R1 antagonist. This compound also has favorable pharmacokinetic properties along with a high metabolic stability and a minimal impact on CYP isoforms and hERG.
- Lim, Chae Jo,Kim, Ji Young,Lee, Byung Ho,Oh, Kwang-Seok,Yi, Kyu Yang
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p. 1736 - 1739
(2013/04/10)
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- NOVEL AMINOALCOHOL-SUBSTITUTED ARYLDIHYDROISOQUINOLINONES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS
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The invention relates to aminoalcohol-substituted aryldihydroisoquinolinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one aminoalcohol-substituted aryldihydroisoquinolinone of the invention or its derivative, and the use of the aminoalcohol- substituted aryldihydroisoquinolinones of the invention and their derivatives as MCH antagonists.
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Page/Page column 87
(2008/06/13)
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- NOVEL AMINO ALCOHOL-SUBSTITUTED ARYLTHIENOPYRIMIDINONES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS
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The invention relates to amino alcohol-substituted arylthienopyrimidinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one amino alcohol-su
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Page/Page column 96
(2008/06/13)
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- NOVEL MCH RECEPTOR ANTAGONISTS
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The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
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Page/Page column 27
(2008/06/13)
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- Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists
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We report here new chemical series acting as antagonists of melanin-concentrating hormone receptor 1 (MCHR-1). Synthesis and structure-activity relationships are described leading to the identification of compounds with optimized in vitro pharmacological and in vitro ADME profiles. In vivo activity has been demonstrated in animal models of food intake and depression.
- Balavoine, Fabrice,Malabre, Patrice,Alleaume, Thierry,Rey, Astrid,Cherfils, Valerie,Jeanneton, Olivier,Seigneurin-Venin, Sophie,Revah, Frederic
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p. 3754 - 3759
(2008/02/10)
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- BI-ARYL META-PYRIMIDINE INHIBITORS OF KINASES
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The invention provides biaryl meta-pyrimidine compounds having the general structure (A). The pyrimidine compounds of the invention are capable of inhibiting kinases, such as members of the Jak kinase family, and various other specific receptor and non receptor kinases.
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Page/Page column 162
(2008/06/13)
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- THIAZOLOPYRIDINONE DERIVATES AS MCH RECEPTOR ANTAGONISTS
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The present invention relates to a melanin concentrating hormone antagonist compound of formula (I); wherein w, R1, q, p, R2, t, Ar1, L1, R3 and R4 are as defined, or a pharmaceutically acceptable salt, solvate, or enantiomer thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.
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Page/Page column 60
(2008/06/13)
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- SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): Discovery of antagonist SB-568849
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We report here the discovery of a class of MCH R1 ligands based on a biphenyl carboxamide template. A docked-in model is presented indicating key interactions in the putative binding site of the receptor. Parallel high throughput synthetic techniques were
- Witty, David R.,Bateson, John H.,Hervieu, Guillaume J.,Jeffrey, Phillip,Johnson, Christopher N.,Muir, Alison I.,O'Hanlon, Peter J.,Stemp, Geoffrey,Stevens, Alex J.,Thewlis, Kevin M.,Wilson, Shelagh,Winborn, Kim Y.
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p. 4865 - 4871
(2007/10/03)
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- Carboxamide compounds and their use as antagonists of a human 11cby receptor
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Compounds of formula (I) in which: each A is independently hydrogen, C1-6alkyl optionally substituted by hydroxyl, C1-6alkoxy, C1-6alkenyl or C1-6acyl group or a halogen atom or hydroxyl, CN or CF3 group; R3 is hydrogen, methyl or ethyl; R4 is an optionally substituted aromatic carbocyclic or heterocyclic ring; Z is an O or S atom, or an NH or CH2 group, or a single bond, at the 3 or 4 position of R4 relative to the carbonyl group; R5 is an optionally substituted aromatic carbocyclic or heterocyclic ring, or an optionally substituted, saturated or unsaturated, carbocyclic or heterocyclic ring; and Q is (a) Where X, Y, R1 and R2 are as defined in claim 1; are antagonists of a human 11CBy receptor.
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