2287-10-7Relevant academic research and scientific papers
Synthesis and SAR study of pyrrolo[3,4-b]pyridin-7(6H)-one derivatives as melanin concentrating hormone receptor 1 (MCH-R1) antagonists
Lim, Chae Jo,Kim, Ji Young,Lee, Byung Ho,Oh, Kwang-Seok,Yi, Kyu Yang
, p. 1736 - 1739 (2013/04/10)
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.
BI-ARYL META-PYRIMIDINE INHIBITORS OF KINASES
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Page/Page column 161-162, (2008/06/13)
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.
Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists
Balavoine, Fabrice,Malabre, Patrice,Alleaume, Thierry,Rey, Astrid,Cherfils, Valerie,Jeanneton, Olivier,Seigneurin-Venin, Sophie,Revah, Frederic
, p. 3754 - 3759 (2008/02/10)
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.
NOVEL AMINO ALCOHOL-SUBSTITUTED ARYLTHIENOPYRIMIDINONES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS
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Page/Page column 97, (2008/06/13)
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
NOVEL MCH RECEPTOR ANTAGONISTS
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Page/Page column 26, (2008/06/13)
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.
NOVEL AMINOALCOHOL-SUBSTITUTED ARYLDIHYDROISOQUINOLINONES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS
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Page/Page column 87, (2008/06/13)
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.
SAR of biphenyl carboxamide ligands of the human melanin-concentrating hormone receptor 1 (MCH R1): Discovery of antagonist SB-568849
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.
, p. 4865 - 4871 (2007/10/03)
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
Carboxamide compounds and their use as antagonists of a human 11cby receptor
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, (2008/06/13)
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.
