JP2016500063A5 - - Google Patents
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- Publication number
- JP2016500063A5 JP2016500063A5 JP2015542798A JP2015542798A JP2016500063A5 JP 2016500063 A5 JP2016500063 A5 JP 2016500063A5 JP 2015542798 A JP2015542798 A JP 2015542798A JP 2015542798 A JP2015542798 A JP 2015542798A JP 2016500063 A5 JP2016500063 A5 JP 2016500063A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently
- compound according
- drugs
- pharmaceutically acceptable
- 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 13
- 150000001875 compounds Chemical class 0.000 claims 11
- 239000003814 drug Substances 0.000 claims 11
- 229940079593 drug Drugs 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 230000001548 androgenic effect Effects 0.000 claims 3
- 206010019280 Heart failures Diseases 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- 208000017442 Retinal disease Diseases 0.000 claims 2
- 206010038923 Retinopathy Diseases 0.000 claims 2
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 208000031225 myocardial ischemia Diseases 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 229940126585 therapeutic drug Drugs 0.000 claims 2
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 208000009304 Acute Kidney Injury Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000004990 Cardiorenal syndrome Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 229940124213 Dipeptidyl peptidase 4 (DPP IV) inhibitor Drugs 0.000 claims 1
- 208000032928 Dyslipidaemia Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 208000005764 Peripheral Arterial Disease Diseases 0.000 claims 1
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 1
- 208000033626 Renal failure acute Diseases 0.000 claims 1
- 108091006269 SLC5A2 Proteins 0.000 claims 1
- 102000058081 Sodium-Glucose Transporter 2 Human genes 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010052428 Wound Diseases 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 201000011040 acute kidney failure Diseases 0.000 claims 1
- 229940005524 anti-dementia drug Drugs 0.000 claims 1
- 230000003178 anti-diabetic effect Effects 0.000 claims 1
- 230000002058 anti-hyperglycaemic effect Effects 0.000 claims 1
- 230000001315 anti-hyperlipaemic effect Effects 0.000 claims 1
- 230000003276 anti-hypertensive effect Effects 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 1
- 230000002253 anti-ischaemic effect Effects 0.000 claims 1
- 230000003063 anti-neuropathic effect Effects 0.000 claims 1
- 239000000883 anti-obesity agent Substances 0.000 claims 1
- 230000002946 anti-pancreatic effect Effects 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 239000002830 appetite depressant Substances 0.000 claims 1
- 230000000747 cardiac effect Effects 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000001149 cognitive effect Effects 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 239000003603 dipeptidyl peptidase IV inhibitor Substances 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- 208000004104 gestational diabetes Diseases 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 230000035876 healing Effects 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 230000006883 memory enhancing effect Effects 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 239000002664 nootropic agent Substances 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261727262P | 2012-11-16 | 2012-11-16 | |
| US61/727,262 | 2012-11-16 | ||
| US201361777294P | 2013-03-12 | 2013-03-12 | |
| US61/777,294 | 2013-03-12 | ||
| PCT/US2013/070215 WO2014078610A1 (en) | 2012-11-16 | 2013-11-15 | Dihydropyrazole gpr40 modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016500063A JP2016500063A (ja) | 2016-01-07 |
| JP2016500063A5 true JP2016500063A5 (enExample) | 2016-11-17 |
| JP6322203B2 JP6322203B2 (ja) | 2018-05-09 |
Family
ID=49876965
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015542798A Expired - Fee Related JP6322203B2 (ja) | 2012-11-16 | 2013-11-15 | ジヒドロピラゾールｇｐｒ４０モジュレーター |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US9133163B2 (enExample) |
| EP (1) | EP2920165B1 (enExample) |
| JP (1) | JP6322203B2 (enExample) |
| KR (1) | KR102204804B1 (enExample) |
| CN (1) | CN104812748B (enExample) |
| AU (1) | AU2013344604B2 (enExample) |
| BR (1) | BR112015010779A2 (enExample) |
| CA (1) | CA2891574A1 (enExample) |
| CY (1) | CY1118365T1 (enExample) |
| DK (1) | DK2920165T3 (enExample) |
| EA (1) | EA026913B1 (enExample) |
| ES (1) | ES2606685T3 (enExample) |
| HR (1) | HRP20161631T1 (enExample) |
| HU (1) | HUE032401T2 (enExample) |
| IL (1) | IL238741A0 (enExample) |
| LT (1) | LT2920165T (enExample) |
| MX (1) | MX358499B (enExample) |
| PL (1) | PL2920165T3 (enExample) |
| PT (1) | PT2920165T (enExample) |
| RS (1) | RS55363B1 (enExample) |
| SG (1) | SG11201503558SA (enExample) |
| SI (1) | SI2920165T1 (enExample) |
| SM (1) | SMT201600410B (enExample) |
| TW (1) | TW201427971A (enExample) |
| UY (1) | UY35143A (enExample) |
| WO (1) | WO2014078610A1 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2015005858A (es) * | 2012-11-16 | 2015-09-24 | Bristol Myers Squibb Co | Moduladores del receptor acoplado a proteina g (gpr40) de dihidropirazol. |
| AU2014372114A1 (en) | 2013-11-14 | 2016-06-09 | Cadila Healthcare Limited | Novel heterocyclic compounds |
| AR100328A1 (es) | 2014-05-07 | 2016-09-28 | Bristol Myers Squibb Co | Moduladores pirrolidina de gpr40 |
| US10017497B2 (en) * | 2014-05-07 | 2018-07-10 | Bristol-Myers Squibb Company | Pyrrolidine GPR40 modulators for the treatment of diseases such as diabetes |
| WO2016019587A1 (en) | 2014-08-08 | 2016-02-11 | Merck Sharp & Dohme Corp. | [7, 6]-fused bicyclic antidiabetic compounds |
| US10968193B2 (en) | 2014-08-08 | 2021-04-06 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| US10100042B2 (en) | 2014-08-08 | 2018-10-16 | Merck Sharp & Dohme Corp. | [5,6]—fused bicyclic antidiabetic compounds |
| EP3177282B1 (en) | 2014-08-08 | 2021-10-06 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| JPWO2018181847A1 (ja) | 2017-03-31 | 2020-03-05 | 武田薬品工業株式会社 | 芳香環化合物 |
| WO2019160882A1 (en) | 2018-02-13 | 2019-08-22 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| WO2019204609A1 (en) | 2018-04-19 | 2019-10-24 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| BR112020026746A2 (pt) | 2018-07-13 | 2021-03-30 | Gilead Sciences, Inc. | Composto, composição farmacêutica, métodos para inibir pd-1, pd-l1 e/ou a interação de pd-1/pd-l1 e para tratar câncer, e, kit para tratar ou prevenir câncer ou uma doença ou condição. |
| CN112955435B (zh) | 2018-10-24 | 2024-09-06 | 吉利德科学公司 | Pd-1/pd-l1抑制剂 |
| CN115490638A (zh) * | 2022-09-22 | 2022-12-20 | 哈尔滨理工大学 | 5-官能团化吡唑啉及其制备方法 |
| CN115671105B (zh) * | 2022-11-22 | 2023-10-27 | 北京箭牧科技有限公司 | Ly2922470在制备预防或治疗肾脏疾病药物中的应用 |
| CN119431272B (zh) * | 2024-11-13 | 2025-07-25 | 北京斯利安药业有限公司 | （s）-3-甲基-（2-哌啶基苯基）-1-丁胺乙酰谷氨酸盐的制备方法 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5614492A (en) | 1986-05-05 | 1997-03-25 | The General Hospital Corporation | Insulinotropic hormone GLP-1 (7-36) and uses thereof |
| WO2003099793A1 (en) | 2002-05-24 | 2003-12-04 | Takeda Pharmaceutical Company Limited | 1,2-azole derivatives with hypoglycemic and hypolipidemic activity |
| WO2004004665A2 (en) | 2002-07-09 | 2004-01-15 | Bristol-Myers Squibb Company | Substituted heterocyclic derivatives useful as antidiabetic and antiobesity agents and method |
| US7501440B2 (en) | 2003-03-07 | 2009-03-10 | Sanofi-Aventis Deutschland Gmbh | Substituted benzoylureidopyridylpiperidine-and-pyrrolidinecarboxylic acid derivatives, processes for preparing them and their use |
| US6995183B2 (en) | 2003-08-01 | 2006-02-07 | Bristol Myers Squibb Company | Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods |
| EP1637522A1 (en) | 2004-09-16 | 2006-03-22 | Laboratorios Del Dr. Esteve, S.A. | Substituted pyrazoline compounds for reducing triglycerides in blood |
| RU2006133260A (ru) * | 2004-02-17 | 2008-04-10 | Лабораториос Дель Др. Эстеве С.А. (Es) | Соединения замещенного пиразолина, их получение и применение в качестве лекарственных средств |
| EA011010B1 (ru) | 2004-02-27 | 2008-12-30 | Эмджен, Инк. | Соединения, модулирующие рецептор gpr40, фармацевтическая композиция, способ лечения заболеваний, чувствительных к модулированию рецептора gpr40 (варианты), способ модулирования функции gpr40 (варианты) и способ модулирования циркулирующей концентрации инсулина |
| EP1731505B1 (en) | 2004-03-30 | 2015-01-14 | Takeda Pharmaceutical Company Limited | Alkoxyphenylpropanoic acid derivatives |
| JP2007284350A (ja) | 2004-07-27 | 2007-11-01 | Takeda Chem Ind Ltd | 糖尿病治療剤 |
| US7465804B2 (en) | 2005-05-20 | 2008-12-16 | Amgen Inc. | Compounds, pharmaceutical compositions and methods for their use in treating metabolic disorders |
| EP1743894A1 (en) * | 2005-07-15 | 2007-01-17 | Laboratorios Del Dr. Esteve, S.A. | Heterocyclyl-substituted pyrazoline compounds, their preparation and use as medicaments |
| JP5084503B2 (ja) | 2005-07-29 | 2012-11-28 | 武田薬品工業株式会社 | シクロプロパンカルボン酸化合物 |
| WO2007033002A1 (en) | 2005-09-14 | 2007-03-22 | Amgen Inc. | Conformationally constrained 3- (4-hydroxy-phenyl) - substituted-propanoic acids useful for treating metabolic disorders |
| CA2646430A1 (en) | 2006-03-14 | 2007-09-20 | Amgen Inc. | Bicyclic carboxylic acid derivatives useful for treating metabolic disorders |
| ES2379661T3 (es) | 2006-06-27 | 2012-04-30 | Takeda Pharmaceutical Company Limited | Compuestos cíclicos condensados |
| CA2662305C (en) | 2006-09-07 | 2012-04-17 | Amgen Inc. | Heterocyclic gpr40 modulators |
| US8039484B2 (en) | 2006-10-31 | 2011-10-18 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| US7572934B2 (en) | 2007-04-16 | 2009-08-11 | Amgen Inc. | Substituted biphenyl GPR40 modulators |
| BRPI0818253A2 (pt) | 2007-10-10 | 2015-04-07 | Amgen Inc | Moduladores de gpr40 bifenil substituídos |
| AR071055A1 (es) | 2007-10-26 | 2010-05-26 | Japan Tobacco Inc | Compuestos espiro, composiciones farmaceuticas y medicamentos que los comprenden, agente promotor de la secrecion de insulina y usos para la preparacion de medicamentos y composiciones farmaceuticas |
| AR070898A1 (es) * | 2008-03-18 | 2010-05-12 | Solvay Pharm Bv | Derivados de arilsulfonil pirazolin carboxamidina como antagonistas de 5-ht6 |
| US8236821B2 (en) * | 2008-05-19 | 2012-08-07 | Jenrin Discovery, Inc. | Substituted N-phenyl-5-phenyl-pyrazolin-3-yl amides as cannabinoid receptor antagonists/inverse agonists useful for treating obesity |
| AU2010303670A1 (en) * | 2009-10-06 | 2012-03-29 | Bristol-Myers Squibb Company | Pyrrolidine GPR40 modulators |
| AR078522A1 (es) | 2009-10-15 | 2011-11-16 | Lilly Co Eli | Compuesto de espiropiperidina, composicion farmaceutica que lo comprende, su uso para preparar un medicamento util para tratar diabetes y compuesto intermediario para su sintesis |
| US8580768B2 (en) * | 2010-11-18 | 2013-11-12 | Jenrin Discovery, Inc. | Cannabinoid receptor antagonists-inverse agonists useful for treating metabolic disorders, including obesity and diabetes |
| CA2818050A1 (en) * | 2010-11-26 | 2012-05-31 | Lupin Limited | Bicyclic gpr119 modulators |
| US8791091B2 (en) | 2011-12-02 | 2014-07-29 | Bristol-Myers Squibb Company | Aryl dihydropyridinone and piperidinone MGAT2 inhibitors |
| US9326218B2 (en) * | 2012-11-02 | 2016-04-26 | Telefonaktiebolaget L M Ericsson (Publ) | Base-station-to-base-station gateway and related devices, methods, and systems |
| MX2015005858A (es) * | 2012-11-16 | 2015-09-24 | Bristol Myers Squibb Co | Moduladores del receptor acoplado a proteina g (gpr40) de dihidropirazol. |
| US8962660B2 (en) * | 2013-03-14 | 2015-02-24 | Bristol-Myers Squibb Company | Oxabicyclo [2.2.2] acid GPR120 modulators |
-
2013
- 2013-11-15 PT PT138116454T patent/PT2920165T/pt unknown
- 2013-11-15 HU HUE13811645A patent/HUE032401T2/en unknown
- 2013-11-15 HR HRP20161631TT patent/HRP20161631T1/hr unknown
- 2013-11-15 MX MX2015005735A patent/MX358499B/es active IP Right Grant
- 2013-11-15 KR KR1020157015541A patent/KR102204804B1/ko not_active Expired - Fee Related
- 2013-11-15 AU AU2013344604A patent/AU2013344604B2/en not_active Ceased
- 2013-11-15 EP EP13811645.4A patent/EP2920165B1/en active Active
- 2013-11-15 ES ES13811645.4T patent/ES2606685T3/es active Active
- 2013-11-15 UY UY0001035143A patent/UY35143A/es not_active Application Discontinuation
- 2013-11-15 EA EA201590954A patent/EA026913B1/ru not_active IP Right Cessation
- 2013-11-15 JP JP2015542798A patent/JP6322203B2/ja not_active Expired - Fee Related
- 2013-11-15 CN CN201380059799.5A patent/CN104812748B/zh not_active Expired - Fee Related
- 2013-11-15 RS RS20161061A patent/RS55363B1/sr unknown
- 2013-11-15 TW TW102141762A patent/TW201427971A/zh unknown
- 2013-11-15 DK DK13811645.4T patent/DK2920165T3/en active
- 2013-11-15 US US14/081,094 patent/US9133163B2/en active Active
- 2013-11-15 BR BR112015010779A patent/BR112015010779A2/pt not_active Application Discontinuation
- 2013-11-15 LT LTEP13811645.4T patent/LT2920165T/lt unknown
- 2013-11-15 SG SG11201503558SA patent/SG11201503558SA/en unknown
- 2013-11-15 PL PL13811645T patent/PL2920165T3/pl unknown
- 2013-11-15 SI SI201330340T patent/SI2920165T1/sl unknown
- 2013-11-15 WO PCT/US2013/070215 patent/WO2014078610A1/en not_active Ceased
- 2013-11-15 CA CA2891574A patent/CA2891574A1/en not_active Abandoned
-
2015
- 2015-05-11 IL IL238741A patent/IL238741A0/en not_active IP Right Cessation
-
2016
- 2016-11-14 SM SM201600410T patent/SMT201600410B/it unknown
- 2016-12-16 CY CY20161101309T patent/CY1118365T1/el unknown
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