JP2011516428A5 - - Google Patents
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- JP2011516428A5 JP2011516428A5 JP2011502137A JP2011502137A JP2011516428A5 JP 2011516428 A5 JP2011516428 A5 JP 2011516428A5 JP 2011502137 A JP2011502137 A JP 2011502137A JP 2011502137 A JP2011502137 A JP 2011502137A JP 2011516428 A5 JP2011516428 A5 JP 2011516428A5
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- Japan
- Prior art keywords
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- alkyl
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- conr
- substituted
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 125000000217 alkyl group Chemical group 0.000 claims description 156
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims description 122
- 239000008280 blood Substances 0.000 claims description 121
- 210000004369 blood Anatomy 0.000 claims description 121
- 125000003118 aryl group Chemical group 0.000 claims description 90
- 150000001875 compounds Chemical class 0.000 claims description 88
- 229910052739 hydrogen Inorganic materials 0.000 claims description 72
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 72
- 239000003112 inhibitor Substances 0.000 claims description 70
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims description 67
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims description 67
- 125000001072 heteroaryl group Chemical group 0.000 claims description 66
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims description 61
- 102000004877 Insulin Human genes 0.000 claims description 61
- 108090001061 Insulin Proteins 0.000 claims description 61
- 239000008103 glucose Substances 0.000 claims description 61
- 229940125396 insulin Drugs 0.000 claims description 61
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 60
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 60
- 239000001257 hydrogen Substances 0.000 claims description 60
- 239000003814 drug Substances 0.000 claims description 54
- 125000000304 alkynyl group Chemical group 0.000 claims description 48
- 229910052736 halogen Inorganic materials 0.000 claims description 48
- 125000001475 halogen functional group Chemical group 0.000 claims description 48
- 150000002367 halogens Chemical class 0.000 claims description 48
- 238000004519 manufacturing process Methods 0.000 claims description 43
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims description 42
- 150000003839 salts Chemical class 0.000 claims description 40
- 229910052760 oxygen Inorganic materials 0.000 claims description 36
- 150000002431 hydrogen Chemical class 0.000 claims description 33
- MGXWVYUBJRZYPE-YUGYIWNOSA-N incretin Chemical class C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1C=CC(O)=CC=1)[C@@H](C)O)[C@@H](C)CC)C1=CC=C(O)C=C1 MGXWVYUBJRZYPE-YUGYIWNOSA-N 0.000 claims description 33
- 239000000859 incretin Substances 0.000 claims description 33
- 230000001419 dependent effect Effects 0.000 claims description 31
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 30
- 206010012601 diabetes mellitus Diseases 0.000 claims description 30
- 125000001188 haloalkyl group Chemical group 0.000 claims description 30
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims description 30
- 150000002148 esters Chemical class 0.000 claims description 28
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 27
- 125000001931 aliphatic group Chemical group 0.000 claims description 24
- 229910052799 carbon Inorganic materials 0.000 claims description 24
- 229910052757 nitrogen Inorganic materials 0.000 claims description 24
- 229960004034 sitagliptin Drugs 0.000 claims description 24
- MFFMDFFZMYYVKS-SECBINFHSA-N sitagliptin Chemical compound C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F MFFMDFFZMYYVKS-SECBINFHSA-N 0.000 claims description 24
- 229910052717 sulfur Inorganic materials 0.000 claims description 24
- 229960001254 vildagliptin Drugs 0.000 claims description 24
- SYOKIDBDQMKNDQ-XWTIBIIYSA-N vildagliptin Chemical compound C1C(O)(C2)CC(C3)CC1CC32NCC(=O)N1CCC[C@H]1C#N SYOKIDBDQMKNDQ-XWTIBIIYSA-N 0.000 claims description 24
- 125000001424 substituent group Chemical group 0.000 claims description 18
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims description 12
- URRAHSMDPCMOTH-LNLFQRSKSA-N Denagliptin Chemical compound C=1C=C(F)C=CC=1C([C@H](N)C(=O)N1[C@@H](C[C@H](F)C1)C#N)C1=CC=C(F)C=C1 URRAHSMDPCMOTH-LNLFQRSKSA-N 0.000 claims description 12
- -1 NR 8 Inorganic materials 0.000 claims description 12
- 150000001336 alkenes Chemical class 0.000 claims description 12
- 150000001345 alkine derivatives Chemical class 0.000 claims description 12
- 229960001667 alogliptin Drugs 0.000 claims description 12
- ZSBOMTDTBDDKMP-OAHLLOKOSA-N alogliptin Chemical compound C=1C=CC=C(C#N)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 ZSBOMTDTBDDKMP-OAHLLOKOSA-N 0.000 claims description 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 12
- 229950010300 denagliptin Drugs 0.000 claims description 12
- 229940079593 drug Drugs 0.000 claims description 12
- 125000000623 heterocyclic group Chemical group 0.000 claims description 12
- 229960004937 saxagliptin Drugs 0.000 claims description 12
- QGJUIPDUBHWZPV-SGTAVMJGSA-N saxagliptin Chemical compound C1C(C2)CC(C3)CC2(O)CC13[C@H](N)C(=O)N1[C@H](C#N)C[C@@H]2C[C@@H]21 QGJUIPDUBHWZPV-SGTAVMJGSA-N 0.000 claims description 12
- 108010033693 saxagliptin Proteins 0.000 claims description 12
- 239000000203 mixture Substances 0.000 claims description 10
- 102100025101 GATA-type zinc finger protein 1 Human genes 0.000 claims description 2
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 claims description 2
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims description 2
- 238000009472 formulation Methods 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 238000000034 method Methods 0.000 description 33
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 description 12
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 description 6
- NFTMKHWBOINJGM-UHFFFAOYSA-N CCc1cnc(N(CC2)CCC2c2nc(COc(cc3)ccc3-[n]3nnnc3)c[s]2)nc1 Chemical compound CCc1cnc(N(CC2)CCC2c2nc(COc(cc3)ccc3-[n]3nnnc3)c[s]2)nc1 NFTMKHWBOINJGM-UHFFFAOYSA-N 0.000 description 2
- 0 CC(*CC1=*=*C(C2CCN(*)CC2)=*1)*[U] Chemical compound CC(*CC1=*=*C(C2CCN(*)CC2)=*1)*[U] 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4119608P | 2008-03-31 | 2008-03-31 | |
| US61/041,196 | 2008-03-31 | ||
| PCT/US2009/038847 WO2009123992A1 (en) | 2008-03-31 | 2009-03-30 | Oxymethylene aryl compounds and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011516428A JP2011516428A (ja) | 2011-05-26 |
| JP2011516428A5 true JP2011516428A5 (enExample) | 2013-05-02 |
| JP5711655B2 JP5711655B2 (ja) | 2015-05-07 |
Family
ID=40668739
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011502137A Expired - Fee Related JP5711655B2 (ja) | 2008-03-31 | 2009-03-30 | オキシメチレンアリール化合物およびその使用 |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20090270404A1 (enExample) |
| EP (1) | EP2280704B1 (enExample) |
| JP (1) | JP5711655B2 (enExample) |
| KR (1) | KR20100134659A (enExample) |
| CN (1) | CN102026636B (enExample) |
| AR (1) | AR072352A1 (enExample) |
| AU (1) | AU2009231906A1 (enExample) |
| BR (1) | BRPI0909469A2 (enExample) |
| CA (1) | CA2719507C (enExample) |
| CL (1) | CL2009000782A1 (enExample) |
| DK (1) | DK2280704T3 (enExample) |
| ES (1) | ES2543358T3 (enExample) |
| IL (1) | IL208230A0 (enExample) |
| MX (1) | MX2010010562A (enExample) |
| PL (1) | PL2280704T3 (enExample) |
| SM (1) | SMP201000118B (enExample) |
| TW (1) | TW201002705A (enExample) |
| WO (1) | WO2009123992A1 (enExample) |
| ZA (1) | ZA201006687B (enExample) |
Families Citing this family (75)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| US7501426B2 (en) | 2004-02-18 | 2009-03-10 | Boehringer Ingelheim International Gmbh | 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions |
| DE102004054054A1 (de) | 2004-11-05 | 2006-05-11 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine |
| DOP2006000008A (es) * | 2005-01-10 | 2006-08-31 | Arena Pharm Inc | Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1 |
| DE102005035891A1 (de) | 2005-07-30 | 2007-02-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel |
| PE20080251A1 (es) | 2006-05-04 | 2008-04-25 | Boehringer Ingelheim Int | Usos de inhibidores de dpp iv |
| SG174054A1 (en) | 2006-05-04 | 2011-09-29 | Boehringer Ingelheim Int | Polymorphs |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| US7638541B2 (en) | 2006-12-28 | 2009-12-29 | Metabolex Inc. | 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
| CA2693169C (en) * | 2007-07-19 | 2016-01-12 | Metabolex, Inc. | N-linked heterocyclic receptor agonists for the treatment of diabetes and metabolic disorders |
| PE20090938A1 (es) | 2007-08-16 | 2009-08-08 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo |
| AR071175A1 (es) | 2008-04-03 | 2010-06-02 | Boehringer Ingelheim Int | Composicion farmaceutica que comprende un inhibidor de la dipeptidil-peptidasa-4 (dpp4) y un farmaco acompanante |
| EP2108960A1 (en) | 2008-04-07 | 2009-10-14 | Arena Pharmaceuticals, Inc. | Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY |
| KR20190016601A (ko) | 2008-08-06 | 2019-02-18 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| KR20110067096A (ko) | 2008-09-10 | 2011-06-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 및 관련 상태를 치료하기 위한 병용 요법 |
| US20200155558A1 (en) | 2018-11-20 | 2020-05-21 | Boehringer Ingelheim International Gmbh | Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug |
| US8716312B2 (en) * | 2008-11-19 | 2014-05-06 | Merck Sharp & Dohme Corporation | Inhibitors of diacylglycerol acyltransferase |
| US20110160222A1 (en) * | 2008-11-26 | 2011-06-30 | Metabolex, Inc. | Modulators of glucose homeostasis for the treatment of diabetes and metabolic disorders |
| EA022310B1 (ru) | 2008-12-23 | 2015-12-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Солевые формы органического соединения |
| AR074990A1 (es) | 2009-01-07 | 2011-03-02 | Boehringer Ingelheim Int | Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina |
| SG173619A1 (en) | 2009-02-13 | 2011-09-29 | Boehringer Ingelheim Int | Pharmaceutical composition comprising a sglt2 inhibitor, a dpp-iv inhibitor and optionally a further antidiabetic agent and uses thereof |
| NZ596467A (en) * | 2009-06-05 | 2014-01-31 | Pfizer | L- ( piperidin-4-yl) -pyrazole derivatives as gpr 119 modulators |
| US8481731B2 (en) | 2009-06-24 | 2013-07-09 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical composition and methods relating thereto |
| US8293729B2 (en) | 2009-06-24 | 2012-10-23 | Boehringer Ingelheim International Gmbh | Compounds, pharmaceutical composition and methods relating thereto |
| EP2483281B1 (en) | 2009-10-01 | 2014-06-04 | Cymabay Therapeutics, Inc. | Substituted tetrazol-1-yl-phenoxymethyl-thiazol-2-yl-piperidinyl-pyrimidine salts |
| BR112012012641A2 (pt) | 2009-11-27 | 2020-08-11 | Boehringer Ingelheim International Gmbh | TRATAMENTO DE PACIENTES DIABÉTICOS GENOTIPADOS COM INIBIDORES DE DPP-lVTAL COMO LINAGLIPTINA |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| US20130109703A1 (en) * | 2010-03-18 | 2013-05-02 | Boehringer Ingelheim International Gmbh | Combination of a GPR119 Agonist and the DPP-IV Inhibitor Linagliptin for Use in the Treatment of Diabetes and Related Conditions |
| GB201006167D0 (en) * | 2010-04-14 | 2010-05-26 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| GB201006166D0 (en) * | 2010-04-14 | 2010-05-26 | Prosidion Ltd | Compounds for the treatment of metabolic disorders |
| KR101927068B1 (ko) | 2010-05-05 | 2018-12-10 | 베링거 인겔하임 인터내셔날 게엠베하 | 체중 감소 치료에 후속하는 dpp-4 억제제에 의한 순차적 병용 요법 |
| GB2488360A (en) * | 2011-02-25 | 2012-08-29 | Prosidion Ltd | Heterocyclic GPCR agonists |
| TW201209054A (en) | 2010-05-28 | 2012-03-01 | Prosidion Ltd | Novel compounds |
| US20110313160A1 (en) * | 2010-06-04 | 2011-12-22 | Metabolex, Inc. | Preparation of 5-ethyl-2--pyrimidine |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| CA2802541A1 (en) | 2010-06-23 | 2011-12-29 | Metabolex, Inc. | Compositions of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine |
| CA2803504C (en) | 2010-06-24 | 2022-08-30 | Boehringer Ingelheim International Gmbh | A combination for diabetes therapy comprising linagliptin and a long-acting insulin |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| SG188361A1 (en) | 2010-09-01 | 2013-04-30 | Arena Pharm Inc | Non-hygroscopic salts of 5-ht2c agonists |
| WO2012030938A1 (en) | 2010-09-01 | 2012-03-08 | Arena Pharmaceuticals, Inc. | Salts of lorcaserin with optically active acids |
| JP6272695B2 (ja) | 2010-09-01 | 2018-01-31 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 体重管理のために有用な５−ｈｔ２ｃアゴニストの改変放出剤形 |
| JP2013536858A (ja) | 2010-09-01 | 2013-09-26 | アリーナ ファーマシューティカルズ， インコーポレイテッド | ５−ｈｔ２ｃアゴニストの速く溶解する剤形 |
| US9034883B2 (en) | 2010-11-15 | 2015-05-19 | Boehringer Ingelheim International Gmbh | Vasoprotective and cardioprotective antidiabetic therapy |
| EP2643310A1 (en) * | 2010-11-23 | 2013-10-02 | Pfizer Inc | 4- (5-cyano-pyrazol-1-yl) -piperidine derivatives as gpr 119 modulators |
| AR085689A1 (es) | 2011-03-07 | 2013-10-23 | Boehringer Ingelheim Int | Composiciones farmaceuticas de metformina, linagliptina y un inhibidor de sglt-2 |
| WO2012170867A1 (en) | 2011-06-09 | 2012-12-13 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of gpr-119 |
| EP3517539B1 (en) | 2011-07-15 | 2022-12-14 | Boehringer Ingelheim International GmbH | Substituted dimeric quinazoline derivative, its preparation and its use in pharmaceutical compositions for the treatment of type i and ii diabetes |
| CN102898400B (zh) * | 2011-07-28 | 2015-04-29 | 北京韩美药品有限公司 | Gpr119激动剂及其应用 |
| EP2567959B1 (en) | 2011-09-12 | 2014-04-16 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
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2009
- 2009-03-30 PL PL09727673T patent/PL2280704T3/pl unknown
- 2009-03-30 KR KR1020107022940A patent/KR20100134659A/ko not_active Withdrawn
- 2009-03-30 US US12/414,639 patent/US20090270404A1/en not_active Abandoned
- 2009-03-30 CA CA2719507A patent/CA2719507C/en not_active Expired - Fee Related
- 2009-03-30 DK DK09727673.7T patent/DK2280704T3/en active
- 2009-03-30 CL CL2009000782A patent/CL2009000782A1/es unknown
- 2009-03-30 CN CN200980110894.7A patent/CN102026636B/zh not_active Expired - Fee Related
- 2009-03-30 ES ES09727673.7T patent/ES2543358T3/es active Active
- 2009-03-30 WO PCT/US2009/038847 patent/WO2009123992A1/en not_active Ceased
- 2009-03-30 MX MX2010010562A patent/MX2010010562A/es not_active Application Discontinuation
- 2009-03-30 TW TW098110577A patent/TW201002705A/zh unknown
- 2009-03-30 AU AU2009231906A patent/AU2009231906A1/en not_active Abandoned
- 2009-03-30 EP EP20090727673 patent/EP2280704B1/en not_active Not-in-force
- 2009-03-30 JP JP2011502137A patent/JP5711655B2/ja not_active Expired - Fee Related
- 2009-03-30 BR BRPI0909469A patent/BRPI0909469A2/pt not_active Application Discontinuation
- 2009-03-31 AR ARP090101153A patent/AR072352A1/es unknown
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2010
- 2010-09-17 ZA ZA2010/06687A patent/ZA201006687B/en unknown
- 2010-09-19 IL IL208230A patent/IL208230A0/en unknown
- 2010-10-28 SM SM201000118T patent/SMP201000118B/it unknown
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