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(12) Patent Application Publication (10) Pub. No.: US 2014/0099333 A1 SCHWINK Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2014/0099333 A1 SCHWINK Et Al US 2014.0099333A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2014/0099333 A1 SCHWINK et al. (43) Pub. Date: Apr. 10, 2014 (54) PYRROLIDINONE DERVATIVES AS GPR119 Publication Classification MODULATORS FOR THE TREATMENT OF DLABETES, OBESITY, DYSLIPIDEMIA AND (51) Int. C. RELATED DSORDERS A 6LX3L/2197 (2006.01) A613 L/405 (2006.01) (71) Applicants: Lothar SCHWINK, Frankfurt am Main C07D 40/12 (2006.01) (DE); Martin BOSSART, Frankfurt am A613 L/4439 (2006.01) Main (DE); Heiner GLOMBIK, A613 L/4545 (2006.01) Frankfurt am Main (DE); Matthias C07D 405/4 (2006.01) GOSSEL, Frankfurt am Main (DE); C07D40 L/4 (2006.01) Dieter KADEREIT, Frankfurt am Main A61K3I/444 (2006.01) (DE); Thomas KLABUNDE, Frankfurt C07D 413/4 (2006.01) am Main (DE); Thomas MAIER, A6II 45/06 (2006.01) Frankfurt am Main (DE); Siegfried C07D 207/12 (2006.01) STENGELIN, Frankfurt am Main (DE) C07D 417/4 (2006.01) (52) U.S. C. (72) Inventors: Lothar SCHWINK, Frankfurt am Main CPC ............ A6IK3I/497 (2013.01); C07D 207/12 (DE); Martin BOSSART, Frankfurt am (2013.01); A61 K3I/4015 (2013.01); C07D Main (DE); Heiner GLOMBIK, 401/12 (2013.01); A61 K3I/4439 (2013.01); Frankfurt am Main (DE); Matthias C07D 417/14 (2013.01); C07D405/14 GOSSEL, Frankfurt am Main (DE); (2013.01); C07D 401/14 (2013.01); A61 K Dieter KADEREIT, Frankfurt am Main 3 1/444 (2013.01); C07D 413/14 (2013.01); (DE); Thomas KLABUNDE, Frankfurt A61K 45/06 (2013.01); A61 K3I/4545 am Main (DE); Thomas MAIER, (2013.01) Frankfurt am Main (DE); Siegfried USPC ..... 424/184.1: 548/544: 514/425; 546/278.7; STENGELIN, Frankfurt am Main (DE) 514/343:546/270.4: 514/342:546/275.4; 514/341; 546/256; 514/333; 546/272.1; 544/405; 514/255.05:546/208: 514/6.5; (73) Assignee: SANOFI, Paris (FR) 514/20.6; 514/210.02; 514/61; 514/318 (57) ABSTRACT (21) Appl. No.: 14/048,425 The present invention relates to pyrrolidinone derivatives. The pyrrolidinone derivatives are GPR119 modulators and (22) Filed: Oct. 8, 2013 useful for the prevention and/or treatment of diabetes, obe sity, dyslipidemia and related disorders. The invention fur (30) Foreign Application Priority Data thermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical Oct. 9, 2012 (EP) .................................. 12306231.7 compositions comprising them. US 2014/0099333 A1 Apr. 10, 2014 PYRROLIDINONE DERVATIVES AS GPR119 0004. Several modulators of GPR119 are known. For MODULATORS FOR THE TREATMENT OF example WO2011 146335 and WO2012037393 describe pip DLABETES, OBESITY, DYSLIPIDEMIA AND eridinyl-substituted lactams as GPR119 modulators. RELATED DSORDERS WO2010048149 describes heterocyclic modulators of GPR119 for the treatment of disease and their preparation. 0001. The present invention relates to pyrrolidinone WO2004110994 describes the preparation of piperazinyl derivatives of the formula I aryloxy and piperazinyl-heteroaryloxy-N-aryl lactams as 5-HT1B ligands. 0005. It was an aim of the invention to provide novel (I) compounds as active ingredients in pharmaceuticals. R1a R1b O R2c 0006. It was an aim of the invention to provide novel (RS)R O s compounds which will lower blood glucose in mammals and N which are suitable for prevention and/or treatment of diabe X 2 tes, obesity, dyslipidemia and related disorders. R2b 2Y 0007. A further aim was to provide novel GPR119 modu lators, especially agonists, which can be used therapeutically Ric R2a for the prevention and/or treatment of diabetes, obesity, dys O lipidemia and related disorders. 0008 Accordingly a subject of the invention is a com 0002 in which R', R', R', R,R,R, X, Y and Y pound of the formula I are defined as indicated below. The pyrrolidinone derivatives Iare GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related dis (I) orders. The invention furthermore relates to the use of pyrro R1a R1b O R2c lidinone derivatives of the formula I as active ingredients in RS). O pharmaceuticals, and pharmaceutical compositions compris (RS) n N ing them. X Y2 0003 GPR119 is a G-protein coupled receptor which is R2b 2 expressed predominantly in the beta cells of the pancreas and RIC R2a in the K- and L-cells of the intestine. In vitro studies have shown, that agonists of GPR119, via activation of the cAMP O pathway in gut and pancreas derived cell lines, mediate the secretion of GLP-1 and insulin respectively. This supports the in which hypothesis, that modulators of GPR119, agonists in particu 0009 X is selected from the series consisting of CH and lar, may have utility to treat diabetes and related disorders by CH, CH: augmenting the secretion of insulin and intestinal hormones I0010) R' is selected from the series consisting of H, F, Cl, like GIP, GLP-1 and PYY. As the secretion of insulin was Br, (C-C)-alkyl and ON: found to be strictly glucose-dependent, induction of hypogly 10011) R' is selected from the series consisting of H, F, Cl cemic episodes may largely be avoided. Furthermore benefi and (C-C)-alkyl; cial effects like reduced food intake may be expected from the (0012) R' is selected from the series consisting of H, F, Cl release of intestinal peptides. Stimulation of the beta cell by and (C-C)-alkyl: activation of GPR119 may also improve beta cell function 0013 R’ is selected from the series consisting of H, F, Cl, and beta cell mass. Studies of GPR119 agonists in rodents Br, (C-C)-alkyl, CN, CO.R and CONRR: showed the predicted glucose lowering effects. For some Such (0014) R' is selected from the series consisting of H, F, Cl animal studies decreased food intake and weight loss was and (C-C)-alkyl; reported. Recently clinical trials with GPR119 agonists 0015 R is selected from the series consisting of H, F, Cl added evidence for a positive impact on lipid parameters i.e. and (C-C)-alkyl; elevation of HDL together with lowering of LDL and triglyc (0016 R, R are independently of each other selected erides in humans. WO2013/070463A2 discloses that from the series consisting of H and (C-C)-alkyl; GPR119 agonists may be used to treat abnormalities in blood 0017 one of the groups Y' and Y is N,N-oxide or CR, lipids. In Summary, modulators of GPR119, agonists in par the other is C Z-R R: ticular, may have therapeutic utility in the prevention and/or 10018 R is selected from the series consisting of H, F, Cl treatment of metabolic disorders in mammals and especially and (C-C)-alkyl; in humans. Examples of Such disorders and diseases include 0019 Z is selected from the series consisting of a bond, O, type 2 diabetes mellitus, type 1 diabetes mellitus, impaired CO, COO, S, SO and SO; glucose tolerance, insulin resistance, loss of beta cell func (0020 R is selected from the series consisting of a bond tion, hyperglycemia, hypercholesterolemia, dyslipidemia, and (CRR), hypertriglyceridemia, Syndrome X, metabolic syndrome, (0021 R, R are independently of each other selected obesity, fatty liver, Steatosis, Steatohepatitis, cirrhosis, micro from the series consisting of Hand (C-C)-alkyl, which is and marcovascular disorders, high blood pressure, chronic unsubstituted or monofluorinated; low grade inflammation, retinopathy, neuropathy, nephropa 0022 n is selected from the series consisting of 1, 2, 3, 4 thy, atherosclerosis, coronary heart disease, endothelial dys and 5; function and bone-related diseases such as osteoporosis, I0023 R is selected from the series consisting of (C-C)- rheumatoid arthritis or osteoarthritis. alkyl, mono-, di- or trifluorinated (C-C)-alkyl, (C-C)- US 2014/0099333 A1 Apr. 10, 2014 alkenyl, (C-C)-alkynyl, COR, OR, NR'R'', SR, (C- 0062) R, R are independently of each other H or (C- Cs)-cycloalkyl, a 4- to 6-membered Saturated or partially C)-alkyl, and the overall number of carbon atoms in a unsaturated heterocycle, which comprises one or two iden (CRR), group is below or equal to eight (8). tical or different ring heteroatoms selected from the series 0063. In another group of embodiments consisting of N and O, phenyl, a 5- to 6-membered het 0064 R is a bond. eroaryl, which comprises one, two or three identical or 0065. In another group of embodiments different ring heteroatoms selected from the series consist I0066 R is selected from the series consisting of CH and ing of N, O and S, wherein all cyclic groups within Rare CH-CH. unsubstituted or substituted by one to three identical or 0067. In another group of embodiments different substituents selected from the series consisting of I0068 R is selected from the series consisting of (C-C)- (C-C)-alkyl, (C-C)-alkanoyl, hydroxy-(Co-C)-alkyl, alkyl, mono-, di- or trifluorinated (C-C)-alkyl, O(C-C)- (C-C)-alkoxy-(Co-C)-alkyl, oxo (=O), F and CI; alkyl, (C-C)-cycloalkyl, a 4- to 6-membered heterocycle, 0024 R7 is selected from the series consisting of H. (C- which comprises one or two ring oxygen atoms, wherein C)-alkyl, hydroxy-(C-C)-alkyl and (C-C)-alkoxy all cyclic groups within Rare unsubstituted or substituted (C-C)-alkyl, by (C-C)-alkyl. 0025 R, R are independently of each other selected 0069. In another group of embodiments from the series consisting of H and (C-C)-alkyl and I0070 R is (C-C)-cycloalkyl, which is unsubstituted or 0026 R is (C-C)-alkyl: substituted by methyl. 0027 in any of its stereoisomeric forms, or a mixture of stereoisomeric forms in any ratio, or a physiologically 0071.
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