144465-94-1Relevant articles and documents
Disubstituted 1-aryl-4-aminopiperidine library synthesis using computational drug design and high-throughput batch and flow technologies
Bryan, Marian C.,Hein, Christopher D.,Gao, Hua,Xia, Xiaoyang,Eastwood, Heather,Bruenner, Bernd A.,Louie, Steven W.,Doherty, Elizabeth M.
, p. 503 - 511 (2013/09/24)
A platform that incorporates computational library design, parallel solution-phase synthesis, continuous flow hydrogenation, and automated high throughput purification and reformatting technologies was applied to the production of a 120-member library of 1-aryl-4-aminopiperidine analogues for drug discovery screening. The application described herein demonstrates the advantages of computational library design coupled with a flexible, modular approach to library synthesis. The enabling technologies described can be readily adopted by the traditional medicinal chemist without extensive training and lengthy process development times.
4- (4-CYANOPHENYL) -1- (3-TRIFLUOROMETHYLPHENYL) -3,4, 6, 7-TETRAHYDRO-1H-PYRROLO [3, 4- D] PYRIMIDINE-2, 5-DIONE DERIVATIVES AND THEIR USE AS HUMAN NEUTROPHIL ELASTASE INHIBITORS
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Page/Page column 15-16, (2009/06/27)
Thirty six specific compounds having human neutrophil elastase inhibitory activity are disclosed, one of which has the structural formula (1). The compounds are useful inter alia for the treatment of inflammatory respiratory disease, and may be administer
Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
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, (2008/06/13)
The present invention relates to compounds that inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclero
Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
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, (2008/06/13)
The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atheroscler
PHARMACEUTICAL COMPOSITIONS AS INHIBITORS OF DIPEPTIDYL PEPTIDASE-IV (DPP-IV)
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Page 60, (2010/11/30)
The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
Inhibitors of factor Xa
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, (2008/06/13)
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.
NEW COMPOUNDS
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Page/Page column 39, (2008/06/13)
The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.
Phenoxylpropanolamines, method for the production thereof and pharmaceutical compositions containing the same
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, (2008/06/13)
The invention concerns compounds of formula (Ia) wherein R1arepresents hydrogen, an —S(O)z—(C1-C4)Alk group, a —CO(C1-C4)Alk group, an —NHSO2—(C1-C4)Alk group, an NCHl (C1-C4) Alk group, a 2-furyl group or a halogen; R2represents hydrogen or a (C1-C4)Alk group, a (C1-C4) alkoxyl group, a halogen, —COOH, —COO(C1-C4)Alk, —CN, —CONR3R4, —NO2, —SO2NH2, —NHSO2(C1-C4)Alk; m and n are independently 0, 1 or 2; R3and R4independently represent hydrogen or a (C1-C4)Alk group; Z is 1 or 2 and their salts or solvates, the pharmaceutical compositions that contain them, the process for their preparation, and intermediate synthesis products.
Inhibitors of factor Xa
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, (2008/06/13)
Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.