JP2010526146A5 - - Google Patents
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- Publication number
- JP2010526146A5 JP2010526146A5 JP2010507529A JP2010507529A JP2010526146A5 JP 2010526146 A5 JP2010526146 A5 JP 2010526146A5 JP 2010507529 A JP2010507529 A JP 2010507529A JP 2010507529 A JP2010507529 A JP 2010507529A JP 2010526146 A5 JP2010526146 A5 JP 2010526146A5
- Authority
- JP
- Japan
- Prior art keywords
- aryl
- alkyl
- heteroaryl
- cycloalkyl
- independently
- 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.)
- Withdrawn
Links
- 125000003118 aryl group Chemical group 0.000 claims 88
- 125000000217 alkyl group Chemical group 0.000 claims 87
- 125000001072 heteroaryl group Chemical group 0.000 claims 86
- 125000000623 heterocyclic group Chemical group 0.000 claims 56
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 37
- 125000000753 cycloalkyl group Chemical group 0.000 claims 32
- 125000005843 halogen group Chemical group 0.000 claims 32
- 229910052739 hydrogen Inorganic materials 0.000 claims 32
- 239000001257 hydrogen Substances 0.000 claims 32
- 125000004093 cyano group Chemical group *C#N 0.000 claims 29
- 150000002431 hydrogen Chemical class 0.000 claims 26
- 229910052760 oxygen Inorganic materials 0.000 claims 25
- 229910052717 sulfur Inorganic materials 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 17
- -1 —NH 2 Chemical group 0.000 claims 17
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 15
- 125000005842 heteroatom Chemical group 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 10
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 125000000304 alkynyl group Chemical group 0.000 claims 8
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000001188 haloalkyl group Chemical group 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 2
- 239000013543 active substance Substances 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 229940089838 Glucagon-like peptide 1 receptor agonist Drugs 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
- 239000003877 glucagon like peptide 1 receptor agonist Substances 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91595207P | 2007-05-04 | 2007-05-04 | |
| PCT/US2008/061930 WO2008137436A1 (en) | 2007-05-04 | 2008-04-30 | [6,5]-bicyclic gpr119 g protein-coupled receptor agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010526146A JP2010526146A (ja) | 2010-07-29 |
| JP2010526146A5 true JP2010526146A5 (enExample) | 2011-05-12 |
Family
ID=39691096
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010507529A Withdrawn JP2010526146A (ja) | 2007-05-04 | 2008-04-30 | ［６，５］−二環式ｇｐｒ１１９ｇタンパク質結合受容体アゴニスト |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US8093257B2 (enExample) |
| EP (1) | EP2152707B1 (enExample) |
| JP (1) | JP2010526146A (enExample) |
| CN (1) | CN101668759A (enExample) |
| AR (1) | AR066438A1 (enExample) |
| CL (1) | CL2008001270A1 (enExample) |
| ES (1) | ES2388315T3 (enExample) |
| PE (1) | PE20090213A1 (enExample) |
| TW (1) | TW200848047A (enExample) |
| WO (1) | WO2008137436A1 (enExample) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US7910583B2 (en) | 2007-05-04 | 2011-03-22 | Bristol-Myers Squibb Company | [6,6] and [6,7]-bicyclic GPR119 G protein-coupled receptor agonists |
| EA016595B1 (ru) * | 2007-07-17 | 2012-06-29 | Бристол-Маерс Сквибб Компани | Способ модулирования рецептора gpr119, сопряженного с g-белком, и используемые при этом соединения |
| 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 |
| US8188098B2 (en) * | 2008-05-19 | 2012-05-29 | Hoffmann-La Roche Inc. | GPR119 receptor agonists |
| CA2730606A1 (en) | 2008-07-16 | 2010-01-21 | Schering Corporation | Bicyclic heterocycle derivatives and methods of use thereof |
| JP2011528368A (ja) * | 2008-07-16 | 2011-11-17 | シェーリング コーポレイション | 二環式ヘテロ環誘導体およびｇｐｃｒモジュレーターとしてのその使用 |
| EP2358736A1 (en) * | 2008-10-15 | 2011-08-24 | Intermune, Inc. | Therapeutic antiviral peptides |
| US20110160222A1 (en) * | 2008-11-26 | 2011-06-30 | Metabolex, Inc. | Modulators of glucose homeostasis for the treatment of diabetes and metabolic disorders |
| US20120016119A1 (en) * | 2009-01-22 | 2012-01-19 | Yasunori Tsuboi | NOVEL PYRROLO(2,3-d)PYRIMIDINE COMPOUND |
| WO2010088518A2 (en) * | 2009-01-31 | 2010-08-05 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| EP2399914A4 (en) | 2009-02-18 | 2012-08-29 | Takeda Pharmaceutical | FUSED HETEROCYCLIC CORE COMPOUND |
| CA2759843A1 (en) * | 2009-05-08 | 2010-11-10 | Pfizer Inc. | Gpr 119 modulators |
| US20120052130A1 (en) * | 2009-05-08 | 2012-03-01 | Pfizer Inc. | Gpr 119 modulators |
| NZ596467A (en) | 2009-06-05 | 2014-01-31 | Pfizer | L- ( piperidin-4-yl) -pyrazole derivatives as gpr 119 modulators |
| AR077214A1 (es) | 2009-06-24 | 2011-08-10 | Neurocrine Biosciences Inc | Heterociclos nitrogenados y composiciones farmaceuticas que los contienen |
| AU2010264720A1 (en) | 2009-06-24 | 2011-12-08 | Boehringer Ingelheim International Gmbh | New compounds, pharmaceutical composition and methods relating thereto |
| CA2772188A1 (en) * | 2009-09-23 | 2011-03-31 | Pfizer Inc. | Gpr 119 modulators |
| IN2012DN02693A (enExample) * | 2009-09-28 | 2015-09-04 | Intermune Inc | |
| JP5909185B2 (ja) | 2009-10-01 | 2016-04-26 | シマベイ セラピューティクス， インコーポレーテッド | 置換テトラゾール−１−イルフェノキシメチルチアゾール−２−イルピペリジニルピリミジン塩 |
| TW201116540A (en) * | 2009-10-01 | 2011-05-16 | Intermune Inc | Therapeutic antiviral peptides |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| EP2547339A1 (en) | 2010-03-18 | 2013-01-23 | 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 |
| SG184168A1 (en) | 2010-04-08 | 2012-10-30 | Bristol Myers Squibb Co | Pyrimidinylpiperidinyloxypyridinone analogues as gpr119 modulators |
| US8940716B2 (en) | 2010-05-06 | 2015-01-27 | Bristol-Myers Squibb Company | Bicyclic heteroaryl compounds as GPR119 modulators |
| US8729084B2 (en) | 2010-05-06 | 2014-05-20 | Bristol-Myers Squibb Company | Benzofuranyl analogues as GPR119 modulators |
| US20130096141A1 (en) * | 2010-06-18 | 2013-04-18 | Bernard R. Neustadt | Bicyclic heterocycle derivatives and methods of use thereof |
| 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 |
| TW201204733A (en) | 2010-06-25 | 2012-02-01 | Kowa Co | Novel condensed pyridine or condensed pyrimidine derivative, and medicinal agent comprising same |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| 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 |
| KR20120011357A (ko) * | 2010-07-23 | 2012-02-08 | 현대약품 주식회사 | 치환된 피리디논 유도체 및 이의 제조방법 |
| UY33805A (es) * | 2010-12-17 | 2012-07-31 | Boehringer Ingelheim Int | ?Derivados de dihidrobenzofuranil-piperidinilo, aza-dihidrobenzofuranilpiperidinilo y diaza-dihidrobenzofuranil-piperidinilo, composiciones farmacéuticas que los contienen y usos de los mismos?. |
| CN103328482A (zh) * | 2011-01-03 | 2013-09-25 | 韩美药品株式会社 | 用于调节g蛋白-偶联受体的新双环化合物 |
| CN102617548A (zh) * | 2011-01-31 | 2012-08-01 | 北京赛林泰医药技术有限公司 | 作为gpr受体激动剂的双环杂芳基化合物及其组合物和应用 |
| CA2836487A1 (en) | 2011-06-09 | 2012-12-13 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of gpr-119 |
| 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 |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| TW201348231A (zh) * | 2012-02-29 | 2013-12-01 | Amgen Inc | 雜雙環化合物 |
| WO2013173198A1 (en) | 2012-05-16 | 2013-11-21 | Bristol-Myers Squibb Company | Pyrimidinylpiperidinyloxypyridone analogues as gpr119 modulators |
| WO2013182612A1 (en) | 2012-06-07 | 2013-12-12 | Bayer Pharma Aktiengesellschaft | Glucose transport inhibitors |
| HK1210825A1 (en) | 2012-07-11 | 2016-05-06 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| AU2017305392A1 (en) | 2016-08-03 | 2019-02-21 | Cymabay Therapeutics, Inc. | Oxymethylene aryl compounds for treating inflammatory gastrointestinal diseases or gastrointestinal conditions |
| CR20190119A (es) | 2016-09-09 | 2019-06-03 | Novartis Ag | Compuestos y composiciones como inhibidores de los receptores endosomales tipo peaje |
| TW202140440A (zh) | 2020-02-28 | 2021-11-01 | 美商克力歐普股份有限公司 | Gpr40激動劑 |
| WO2021236617A1 (en) | 2020-05-19 | 2021-11-25 | Kallyope, Inc. | Ampk activators |
| CN116390925A (zh) | 2020-06-26 | 2023-07-04 | 卡尔优普公司 | Ampk活化剂 |
Family Cites Families (30)
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|---|---|---|---|---|
| US3826643A (en) * | 1967-08-07 | 1974-07-30 | American Cyanamid Co | Method of controlling undesirable plant species using 3-nitropyridines |
| US5776983A (en) * | 1993-12-21 | 1998-07-07 | Bristol-Myers Squibb Company | Catecholamine surrogates useful as β3 agonists |
| US5488064A (en) * | 1994-05-02 | 1996-01-30 | Bristol-Myers Squibb Company | Benzo 1,3 dioxole derivatives |
| US5612359A (en) * | 1994-08-26 | 1997-03-18 | Bristol-Myers Squibb Company | Substituted biphenyl isoxazole sulfonamides |
| US5491134A (en) * | 1994-09-16 | 1996-02-13 | Bristol-Myers Squibb Company | Sulfonic, phosphonic or phosphiniic acid β3 agonist derivatives |
| US5541204A (en) * | 1994-12-02 | 1996-07-30 | Bristol-Myers Squibb Company | Aryloxypropanolamine β 3 adrenergic agonists |
| US5620997A (en) | 1995-05-31 | 1997-04-15 | Warner-Lambert Company | Isothiazolones |
| AU6966696A (en) | 1995-10-05 | 1997-04-28 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
| US5770615A (en) * | 1996-04-04 | 1998-06-23 | Bristol-Myers Squibb Company | Catecholamine surrogates useful as β3 agonists |
| US6566384B1 (en) * | 1996-08-07 | 2003-05-20 | Darwin Discovery Ltd. | Hydroxamic and carboxylic acid derivatives having MMP and TNF inhibitory activity |
| TW536540B (en) * | 1997-01-30 | 2003-06-11 | Bristol Myers Squibb Co | Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe |
| UA57811C2 (uk) | 1997-11-21 | 2003-07-15 | Пфайзер Продактс Інк. | Фармацевтична композиція, що містить інгібітор альдозоредуктази та інгібітор глікогенфосфорилази (варіанти), комплект, який її включає, та способи лікування ссавців зі станом інсулінорезистентності |
| HUP0104634A3 (en) | 1998-07-06 | 2002-11-28 | Bristol Myers Squibb Co | Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists |
| CA2348740A1 (en) | 1998-12-23 | 2000-07-06 | Ruth R. Wexler | Thrombin or factor xa inhibitors |
| AU2001275857A1 (en) | 2000-06-29 | 2002-01-14 | Bristol-Myers Squibb Pharma Company | Thrombin or factor xa inhibitors |
| EP1338651B9 (en) | 2000-12-01 | 2007-05-09 | Astellas Pharma Inc. | Method of screening remedy for diabetes |
| US7482366B2 (en) * | 2001-12-21 | 2009-01-27 | X-Ceptor Therapeutics, Inc. | Modulators of LXR |
| EP1465869B1 (en) * | 2001-12-21 | 2013-05-15 | Exelixis Patent Company LLC | Modulators of lxr |
| MXPA05007485A (es) | 2003-01-14 | 2006-01-30 | Arena Pharm Inc | Derivados de arilo y heteroarilo 1,2,3-trisubstituidos como moduladores del metabolismo y la profilaxis y tratamiento de trastornos relacionados con ello tales como diabetes e hiperglicemia. |
| WO2004076413A2 (en) | 2003-02-24 | 2004-09-10 | Arena Pharmaceuticals, Inc. | Phenyl- and pyridylpiperidine-derivatives as modulators of glucose metabolism |
| SE0301010D0 (sv) | 2003-04-07 | 2003-04-07 | Astrazeneca Ab | Novel compounds |
| AR045047A1 (es) | 2003-07-11 | 2005-10-12 | Arena Pharm Inc | Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos |
| RS20060018A (sr) | 2003-07-14 | 2007-12-31 | Arena Pharmaceuticals Inc., | Derivati spojenih arila i heteroarila kao modulatori metabolizma u profilaksi i lečenju sa njima povezanih stanja |
| WO2005025504A2 (en) | 2003-09-12 | 2005-03-24 | Kemia, Inc. | Modulators of calcitonin and amylin activity |
| EP2060266B1 (en) | 2004-03-17 | 2011-08-10 | 7TM Pharma A/S | Y4 selective receptor agonist PP2-36 for therapeutic interventions |
| DE602005015962D1 (de) * | 2004-05-03 | 2009-09-24 | Hoffmann La Roche | Indolylderivate als liver-x-rezeptormodulatoren |
| PL1756084T3 (pl) | 2004-06-04 | 2009-06-30 | Arena Pharm Inc | Podstawione pochodne arylowe i heteroarylowe jako modulatory metabolizmu oraz profilaktyka i leczenie zaburzeń z metabolizmem związanych |
| EP1838706A1 (en) | 2004-12-24 | 2007-10-03 | Prosidion Limited | G-protein coupled receptor agonists |
| MY148521A (en) | 2005-01-10 | 2013-04-30 | Arena Pharm Inc | Substituted pyridinyl and pyrimidinyl derivatives as modulators of metabolism and the treatment of disorders related thereto |
| CA2612187C (en) * | 2005-06-23 | 2013-05-07 | Emory University | Stereoselective synthesis of amino acid analogs for tumor imaging |
-
2008
- 2008-04-30 ES ES08747131T patent/ES2388315T3/es active Active
- 2008-04-30 CN CN200880013802A patent/CN101668759A/zh active Pending
- 2008-04-30 WO PCT/US2008/061930 patent/WO2008137436A1/en not_active Ceased
- 2008-04-30 PE PE2008000776A patent/PE20090213A1/es not_active Application Discontinuation
- 2008-04-30 JP JP2010507529A patent/JP2010526146A/ja not_active Withdrawn
- 2008-04-30 EP EP08747131A patent/EP2152707B1/en not_active Not-in-force
- 2008-04-30 US US12/112,053 patent/US8093257B2/en active Active
- 2008-05-02 TW TW097116366A patent/TW200848047A/zh unknown
- 2008-05-02 CL CL200801270A patent/CL2008001270A1/es unknown
- 2008-05-02 AR ARP080101888A patent/AR066438A1/es not_active Application Discontinuation
-
2011
- 2011-11-30 US US13/307,698 patent/US8476283B2/en active Active
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