JP2011516428A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- cor
- 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.)
- Granted
Links
- 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 (https=) | 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 (https=) |
| EP (1) | EP2280704B1 (https=) |
| JP (1) | JP5711655B2 (https=) |
| KR (1) | KR20100134659A (https=) |
| CN (1) | CN102026636B (https=) |
| AR (1) | AR072352A1 (https=) |
| AU (1) | AU2009231906A1 (https=) |
| BR (1) | BRPI0909469A2 (https=) |
| CA (1) | CA2719507C (https=) |
| CL (1) | CL2009000782A1 (https=) |
| DK (1) | DK2280704T3 (https=) |
| ES (1) | ES2543358T3 (https=) |
| IL (1) | IL208230A0 (https=) |
| MX (1) | MX2010010562A (https=) |
| PL (1) | PL2280704T3 (https=) |
| SM (1) | SMP201000118B (https=) |
| TW (1) | TW201002705A (https=) |
| WO (1) | WO2009123992A1 (https=) |
| ZA (1) | ZA201006687B (https=) |
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 |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| PE20110235A1 (es) | 2006-05-04 | 2011-04-14 | Boehringer Ingelheim Int | Combinaciones farmaceuticas que comprenden linagliptina y metmorfina |
| KR101452915B1 (ko) | 2006-05-04 | 2014-10-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 다형태 |
| 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 |
| AU2008279447A1 (en) | 2007-07-19 | 2009-01-29 | Metabolex, Inc. | N-azacyclic substituted pyrrole, pyrazole, imidazole, triazole and tetrazole derivatives as agonists of the RUP3 or GPR119 receptor 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 |
| PE20091730A1 (es) | 2008-04-03 | 2009-12-10 | Boehringer Ingelheim Int | Formulaciones que comprenden un inhibidor de dpp4 |
| 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 |
| UY32030A (es) | 2008-08-06 | 2010-03-26 | Boehringer Ingelheim Int | "tratamiento para diabetes en pacientes inapropiados para terapia con metformina" |
| KR20190016601A (ko) | 2008-08-06 | 2019-02-18 | 베링거 인겔하임 인터내셔날 게엠베하 | 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료 |
| CA2736421A1 (en) | 2008-09-10 | 2010-03-18 | Boehringer Ingelheim International Gmbh | Combination therapy for the treatment of diabetes and related conditions |
| 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 |
| CN102281919A (zh) * | 2008-11-19 | 2011-12-14 | 先灵公司 | 二酰基甘油酰基转移酶的抑制剂 |
| US20110160222A1 (en) * | 2008-11-26 | 2011-06-30 | Metabolex, Inc. | Modulators of glucose homeostasis for the treatment of diabetes and metabolic disorders |
| JP2012512848A (ja) | 2008-12-23 | 2012-06-07 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 有機化合物の塩の形態 |
| TW201036975A (en) | 2009-01-07 | 2010-10-16 | Boehringer Ingelheim Int | Treatment for diabetes in patients with inadequate glycemic control despite metformin therapy |
| BRPI1008560B1 (pt) | 2009-02-13 | 2021-08-31 | Boehringer Ingelheim International Gmbh | Composição farmacêutica compreendendo um inibidor de sglt2, um inibidor de dpp-iv e opcionalmente um outro agente antidiabético e usos dos mesmos |
| 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 |
| EA201200046A1 (ru) | 2009-06-24 | 2012-08-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Новые соединения, фармацевтическая композиция и связанные с ними способы |
| US8410127B2 (en) * | 2009-10-01 | 2013-04-02 | Metabolex, Inc. | Substituted tetrazol-1-yl-phenoxymethyl-thiazol-2-yl-piperidinyl-pyrimidine salts |
| KR20240090632A (ko) | 2009-11-27 | 2024-06-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 리나글립틴과 같은 ｄｐｐ－ｉｖ 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료 |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| JP2013522279A (ja) * | 2010-03-18 | 2013-06-13 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 糖尿病及び関連状態の治療で用いるｇｐｒ１１９作動薬とｄｄｐ−ｉｖ阻害薬リナグリプチンの組合せ |
| 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 |
| CA3070513C (en) | 2010-05-05 | 2023-01-03 | Boehringer Ingelheim International Gmbh | A dpp-4 inhibitor for use in treatment of skin-alterations or necrosis |
| 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 |
| CN109674753A (zh) * | 2010-06-23 | 2019-04-26 | 希玛贝治疗股份有限公司 | 固态分散体 |
| KR20130093012A (ko) | 2010-06-24 | 2013-08-21 | 베링거 인겔하임 인터내셔날 게엠베하 | 당뇨병 요법 |
| 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 |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| EP3485878A1 (en) | 2010-09-01 | 2019-05-22 | Arena Pharmaceuticals, Inc. | Modified-release dosage forms of 5-ht2c agonists useful for weight management |
| AU2011296027A1 (en) | 2010-09-01 | 2013-04-04 | Arena Pharmaceuticals, Inc. | Fast-dissolve dosage forms of 5-HT2C agonists |
| JP2013536859A (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アゴニストの非吸湿性塩 |
| KR20130138770A (ko) | 2010-09-01 | 2013-12-19 | 아레나 파마슈티칼스, 인크. | 광학적으로 활성 산을 갖는 로르카세린의 염 |
| AR083878A1 (es) | 2010-11-15 | 2013-03-27 | Boehringer Ingelheim Int | Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento |
| SG189830A1 (en) * | 2010-11-23 | 2013-06-28 | Pfizer | 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 |
| KR101913619B1 (ko) | 2011-06-09 | 2018-12-28 | 리젠 파마슈티컬스 소시에떼 아노님 | Gpr-119의 조절제로서의 신규한 화합물 |
| DK2731947T3 (en) | 2011-07-15 | 2019-04-23 | Boehringer Ingelheim Int | SUBSTITUTED DIMERIC QUINAZOLINE DERIVATIVE, PREPARATION AND USE thereof IN PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF TYPE I AND TYPE 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 |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| 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 |
| EP2760862B1 (en) | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| US9555001B2 (en) | 2012-03-07 | 2017-01-31 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition and uses thereof |
| WO2013163244A1 (en) | 2012-04-26 | 2013-10-31 | Bristol-Myers Squibb Company | Imidazothiadiazole derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation |
| LT2841437T (lt) | 2012-04-26 | 2017-09-11 | Bristol-Myers Squibb Company | Imidazotiadiazolo ir imidazopirazino dariniai, kaip proteazės aktyvuotų receptorių 4 (par4) inhibitoriai, skirti trombocitų agregacijos gydymui |
| BR112014026651A8 (pt) | 2012-04-26 | 2018-01-16 | Bristol Myers Squibb Co | derivados de imidazotiadiazol e de imidazopiridazina como inibidores do receptor ativado por proteases 4 (par4) para o tratamento de agregação plaquetária |
| WO2013171167A1 (en) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome |
| WO2013171166A1 (en) | 2012-05-14 | 2013-11-21 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp-4 inhibitor for use in the treatment of sirs and/or sepsis |
| WO2013174767A1 (en) | 2012-05-24 | 2013-11-28 | Boehringer Ingelheim International Gmbh | A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference |
| CA2878625A1 (en) | 2012-07-11 | 2014-01-16 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| EP3110449B1 (en) | 2014-02-28 | 2023-06-28 | Boehringer Ingelheim International GmbH | Medical use of a dpp-4 inhibitor |
| JP2017119628A (ja) * | 2014-05-09 | 2017-07-06 | 日産化学工業株式会社 | 置換アゾール化合物及び糖尿病治療薬 |
| US10414723B2 (en) * | 2015-05-08 | 2019-09-17 | Vertellus Holdings Llc | Processes for converting carboxamides to thiocarboxamides |
| US10526345B2 (en) | 2016-04-08 | 2020-01-07 | Mankind Pharma Ltd. | Compounds as GPR119 agonists |
| US10208030B2 (en) * | 2016-04-08 | 2019-02-19 | Mankind Pharma Ltd. | GPR119 agonist compounds |
| US10954229B2 (en) | 2016-04-08 | 2021-03-23 | Mankind Pharma Ltd. | GPR119 agonist compounds |
| CN109890814B (zh) * | 2016-06-09 | 2023-04-18 | 普拉马纳制药公司 | 包含苯并[d][1,3]氧硫杂环戊烯3-氧化物的化合物及其方法/用途 |
| EP4233840A3 (en) | 2016-06-10 | 2023-10-18 | Boehringer Ingelheim International GmbH | Combinations of linagliptin and metformin |
| AU2017305392A1 (en) | 2016-08-03 | 2019-02-21 | Cymabay Therapeutics, Inc. | Oxymethylene aryl compounds for treating inflammatory gastrointestinal diseases or gastrointestinal conditions |
| BR112021026809A2 (pt) * | 2019-07-08 | 2022-02-22 | Mankind Pharma Ltd | Terapia de combinação de agonistas de gpr119 e inibidores de dpp-4 |
| IL295825A (en) | 2020-02-28 | 2022-10-01 | Kallyope Inc | gpr40 agonists |
| WO2021236617A1 (en) | 2020-05-19 | 2021-11-25 | Kallyope, Inc. | Ampk activators |
| CA3183575A1 (en) | 2020-06-26 | 2021-12-30 | Iyassu Sebhat | Ampk activators |
Family Cites Families (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3778443A (en) * | 1969-02-13 | 1973-12-11 | Ciba Geigy Ag | 4-tetrahydro pyridyl,hydroxy alkyl pyrazoles |
| US3536809A (en) * | 1969-02-17 | 1970-10-27 | Alza Corp | Medication method |
| US3845770A (en) * | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US3916899A (en) * | 1973-04-25 | 1975-11-04 | Alza Corp | Osmotic dispensing device with maximum and minimum sizes for the passageway |
| US4008719A (en) * | 1976-02-02 | 1977-02-22 | Alza Corporation | Osmotic system having laminar arrangement for programming delivery of active agent |
| CA1146866A (en) * | 1979-07-05 | 1983-05-24 | Yamanouchi Pharmaceutical Co. Ltd. | Process for the production of sustained release pharmaceutical composition of solid medical material |
| DE3438830A1 (de) * | 1984-10-23 | 1986-04-30 | Rentschler Arzneimittel | Nifedipin enthaltende darreichungsform und verfahren zu ihrer herstellung |
| US5013556A (en) * | 1989-10-20 | 1991-05-07 | Liposome Technology, Inc. | Liposomes with enhanced circulation time |
| KR0182801B1 (ko) * | 1991-04-16 | 1999-05-01 | 아만 히데아키 | 고체 분산체의 제조방법 |
| US5817667A (en) * | 1991-04-17 | 1998-10-06 | University Of Georgia Research Foudation | Compounds and methods for the treatment of cancer |
| US5340591A (en) * | 1992-01-24 | 1994-08-23 | Fujisawa Pharmaceutical Co., Ltd. | Method of producing a solid dispersion of the sparingly water-soluble drug, nilvadipine |
| JP3265680B2 (ja) * | 1992-03-12 | 2002-03-11 | 大正製薬株式会社 | 経口製剤用組成物 |
| AU4444393A (en) * | 1992-09-01 | 1994-03-10 | Zeneca Limited | Pyrrolidine derivatives |
| ES2229259T3 (es) * | 1995-01-12 | 2005-04-16 | Glaxo Group Limited | Derivados de piperidina con actividad antagonista de taquiquinina. |
| DE19504832A1 (de) * | 1995-02-14 | 1996-08-22 | Basf Ag | Feste Wirkstoff-Zubereitungen |
| RU2167865C2 (ru) * | 1995-09-07 | 2001-05-27 | Ф. Хоффманн-Ля Рош Аг | Производные пиперидина, способ их получения, фармацевтическая композиция на их основе и промежуточные вещества |
| EP0858457A1 (de) * | 1995-10-20 | 1998-08-19 | Dr. Karl Thomae GmbH | 5-gliedrige heterocyclen, diese verbindungen enthaltende arzneimittel und deren verwendung sowie verfahren zu ihrer herstellung |
| US5880138A (en) * | 1996-10-01 | 1999-03-09 | Eli Lilly And Company | NMDA receptor selective antagonists |
| US6274735B1 (en) * | 1998-08-10 | 2001-08-14 | Hoffmann-La Roche Inc. | Process and intermediates for preparation of substituted piperidines |
| IT1303737B1 (it) * | 1998-11-11 | 2001-02-23 | Smithkline Beecham Spa | Derivati fenilpiperidinici procedimento per la loro preparazione eloro uso come ligandi del recettore orl-1. |
| US20030017528A1 (en) * | 1998-11-20 | 2003-01-23 | Ruoping Chen | Human orphan G protein-coupled receptors |
| US6221660B1 (en) * | 1999-02-22 | 2001-04-24 | Synaptic Pharmaceutical Corporation | DNA encoding SNORF25 receptor |
| GB9912416D0 (en) * | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| US7084145B2 (en) * | 2002-10-25 | 2006-08-01 | Pfizer Inc. | Triazole compounds useful in therapy |
| US7132426B2 (en) * | 2003-07-14 | 2006-11-07 | Arena Pharmaceuticals, Inc. | Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
| US8710232B2 (en) * | 2004-04-22 | 2014-04-29 | Sanofi-Aventis Deutschland Gmbh | Imidazole derivatives used as TAFIa inhibitors |
| 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 |
| WO2007003960A1 (en) * | 2005-06-30 | 2007-01-11 | Prosidion Limited | Gpcr agonists |
| WO2007003961A2 (en) * | 2005-06-30 | 2007-01-11 | Prosidion Limited | Gpcr agonists |
| JP2009509988A (ja) * | 2005-09-29 | 2009-03-12 | サノフィ−アベンティス | フェニル−及びピリジニル−１，２，４−オキサジアゾロン誘導体、その製造方法、及び医薬品としてのその使用 |
| ATE552245T1 (de) * | 2006-05-15 | 2012-04-15 | Merck Sharp & Dohme | Antidiabetische bicyclische verbindungen |
| 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 |
| TWI414523B (zh) * | 2006-12-28 | 2013-11-11 | Metabolex Inc | 用於治療糖尿病及代謝病症之雜環受體促效劑 |
| EP2134704B1 (en) * | 2007-03-08 | 2010-09-22 | Irm Llc | Compounds and compositions as modulators of gpr119 activity |
| EP2014656A3 (en) * | 2007-06-11 | 2011-08-24 | High Point Pharmaceuticals, LLC | New heteocyclic h3 antagonists |
| AU2008279447A1 (en) * | 2007-07-19 | 2009-01-29 | Metabolex, Inc. | N-azacyclic substituted pyrrole, pyrazole, imidazole, triazole and tetrazole derivatives as agonists of the RUP3 or GPR119 receptor for the treatment of diabetes and metabolic disorders |
| MX2010013876A (es) * | 2008-06-20 | 2011-03-04 | Metabolex Inc | Agonistas de arilo grpr119 y sus usos . |
| US8536176B2 (en) * | 2008-08-01 | 2013-09-17 | Nippon Chemiphar Co., Ltd. | GPR119 agonist |
| CA2736421A1 (en) * | 2008-09-10 | 2010-03-18 | Boehringer Ingelheim International Gmbh | Combination therapy for the treatment of diabetes and related conditions |
| US8410127B2 (en) * | 2009-10-01 | 2013-04-02 | Metabolex, Inc. | Substituted tetrazol-1-yl-phenoxymethyl-thiazol-2-yl-piperidinyl-pyrimidine salts |
| US20110313160A1 (en) * | 2010-06-04 | 2011-12-22 | Metabolex, Inc. | Preparation of 5-ethyl-2--pyrimidine |
| CN109674753A (zh) * | 2010-06-23 | 2019-04-26 | 希玛贝治疗股份有限公司 | 固态分散体 |
| US20120184572A1 (en) * | 2011-01-13 | 2012-07-19 | Metabolex, Inc. | Aryl gpr119 agonists and uses thereof |
-
2009
- 2009-03-30 BR BRPI0909469A patent/BRPI0909469A2/pt not_active Application Discontinuation
- 2009-03-30 AU AU2009231906A patent/AU2009231906A1/en not_active Abandoned
- 2009-03-30 CL CL2009000782A patent/CL2009000782A1/es unknown
- 2009-03-30 ES ES09727673.7T patent/ES2543358T3/es active Active
- 2009-03-30 TW TW098110577A patent/TW201002705A/zh unknown
- 2009-03-30 EP EP20090727673 patent/EP2280704B1/en not_active Not-in-force
- 2009-03-30 DK DK09727673.7T patent/DK2280704T3/en active
- 2009-03-30 CA CA2719507A patent/CA2719507C/en not_active Expired - Fee Related
- 2009-03-30 CN CN200980110894.7A patent/CN102026636B/zh not_active Expired - Fee Related
- 2009-03-30 US US12/414,639 patent/US20090270404A1/en not_active Abandoned
- 2009-03-30 PL PL09727673T patent/PL2280704T3/pl unknown
- 2009-03-30 KR KR1020107022940A patent/KR20100134659A/ko not_active Withdrawn
- 2009-03-30 MX MX2010010562A patent/MX2010010562A/es not_active Application Discontinuation
- 2009-03-30 WO PCT/US2009/038847 patent/WO2009123992A1/en not_active Ceased
- 2009-03-30 JP JP2011502137A patent/JP5711655B2/ja not_active Expired - Fee Related
- 2009-03-31 AR ARP090101153A patent/AR072352A1/es unknown
-
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
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2011516428A5 (https=) | ||
| JP2014500295A5 (https=) | ||
| AR072352A1 (es) | Compuestos de oximetilen arilo y usos de estos | |
| CA2717948C (en) | 5imidazoquinolines and pyrimidine derivatives as potent modulators of vegf-driven angiogenic processes | |
| RU2010151352A (ru) | Арильные агонисты grp119 и их применения | |
| JP2015511638A5 (https=) | ||
| JP2013512903A5 (https=) | ||
| JP2015506348A5 (https=) | ||
| JP2017527532A5 (https=) | ||
| RU2013121788A (ru) | Ингибиторы репликации вич | |
| JP2020505407A5 (https=) | ||
| JP2020510015A5 (https=) | ||
| ES3053660T3 (en) | Pharmaceutical combination comprising ponesimod and its use in the treatment of multiple sclerosis | |
| JP2011529474A (ja) | ｃｄｋ阻害剤および抗悪性腫瘍剤を含む治療用組合せ | |
| RU2013148922A (ru) | Три- и тетрациклические пиразоло[3,4-в]пиридины в качестве антинеопластического средства | |
| RU2012146194A (ru) | Мультизамещенные ароматические соединения в качестве ингибиторов тромбина | |
| RU2009132188A (ru) | Режим дозирования ингибиторов комт | |
| JP2007529528A5 (https=) | ||
| JP2012522841A5 (https=) | ||
| RU2013108348A (ru) | Конденсированные гетероарилы и их применение | |
| JP2011509302A5 (https=) | ||
| JP2016525104A5 (https=) | ||
| ES2755303T3 (es) | Composición medicinal para potenciar la síntesis de protoporfirina IX | |
| RU2013136895A (ru) | Новое бициклическое соединение или его соль | |
| JP2011518168A5 (https=) |