[EN] SUBSTITUTED INDANONE COMPOUNDS AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS [FR] COMPOSÉS INDANONE SUBSTITUÉS UTILES EN TANT QUE MODULATEURS DE GPR119 POUR LE TRAITEMENT DU DIABÈTE, DE L'OBÉSITÉ, DE LA DYSLIPIDÉMIE ET DE TROUBLES ASSOCIÉS
Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13
摘要:
Explorations in the pyrimidinetrione series of MMP-13 inhibitors led to the discovery of a series of spiro-fused compounds that are potent and selective inhibitiors of MMP-13. While other spiro-fused motifs are hydrolytically unstable, presumably due to electronic destabilization of the pyrimidinetrione ring, the spiropyrrolidine series does not share this liability. Greater than 100-fold selectivity versus other MMP family members was achieved by incorporation of an extended aryl-heteroaryl P1' group. When dosed as the sodium salt, these compounds displayed excellent oral absorption and pharmacokinetic properties. Despite the selectivity, a representative of this series produced fibroplasia in a 14 day rat study. (c) 2007 Elsevier Ltd. All rights reserved.
AZETIDINE COMPOUNDS AS GRP119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS
申请人:SANOFI
公开号:US20180237419A1
公开(公告)日:2018-08-23
The present disclosure relates to azetidine compounds. The azetidine compounds are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The present disclosure furthermore relates to the use of azetidine compounds as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
[EN] ISOINDOLINONE COMPOUNDS AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS<br/>[FR] COMPOSÉS D'ISOINDOLINONE UTILISÉS COMME MODULATEURS DE GPR119 POUR LE TRAITEMENT DU DIABÈTE, DE L'OBÉSITÉ ET DE TROUBLES ASSOCIÉS
申请人:SANOFI SA
公开号:WO2015150565A1
公开(公告)日:2015-10-08
The present invention relates to isoindolinone compounds. The isoindolinone compounds are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of isoindolinone compounds as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
PYRROLIDINONE DERIVATIVES AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS
申请人:SCHWINK Lothar
公开号:US20140099333A1
公开(公告)日:2014-04-10
The present invention relates to pyrrolidinone derivatives. The pyrrolidinone derivatives are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
[EN] PYRROLIDINONE DERIVATIVES AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS<br/>[FR] DÉRIVÉS DE PYRROLIDINONE À TITRE DE MODULATEURS DE GPR119 POUR LE TRAITEMENT DU DIABÈTE, DE L'OBÉSITÉ, DE LA DYSLIPIDÉMIE ET AUTRES AFFECTIONS APPARENTÉES
申请人:SANOFI SA
公开号:WO2014056938A1
公开(公告)日:2014-04-17
The present invention relates to pyrrolidinone derivatives of formula (I). The pyrrolidinone derivatives of formula (I) are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
[EN] SUBSTITUTED FUSED HETEROCYCLES AS GPR119 MODULATORS FOR THE TREATMENT OF DIABETES, OBESITY, DYSLIPIDEMIA AND RELATED DISORDERS<br/>[FR] HÉTÉROCYCLES SUBSTITUÉS LIÉS PAR FUSION EN TANT QUE MODULATEURS GPR119 POUR LE TRAITEMENT DU DIABÈTE, DE L'OBÉSITÉ, DE LA DYSLIPIDÉMIE ET DE TROUBLES ASSOCIÉS
申请人:SANOFI SA
公开号:WO2015150564A1
公开(公告)日:2015-10-08
The present invention relates to substituted fused heterocyclic compounds. The substituted fused heterocyclic compounds are GPR1 19 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of substituted fused heterocyclic compounds as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.