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 |
|---|---|---|---|---|
| SG11201503556PA (en) * | 2012-11-16 | 2015-06-29 | Bristol Myers Squibb Co | Dihydropyrazole gpr40 modulators |
| CA2928097A1 (en) | 2013-11-14 | 2015-07-02 | Cadila Healthcare Limited | Novel heterocyclic compounds |
| BR112016025188A2 (pt) * | 2014-05-07 | 2017-08-15 | Bristol Myers Squibb Co | moduladores de pirrolidina gpr40 para o tratamento de doenças tal como diabetes |
| BR112016024936A2 (pt) | 2014-05-07 | 2017-08-15 | Bristol Myers Squibb Co | moduladores de gpr40 à base de pirrolidina para tratamento de doenças como diabetes |
| WO2016019587A1 (en) | 2014-08-08 | 2016-02-11 | Merck Sharp & Dohme Corp. | [7, 6]-fused bicyclic antidiabetic compounds |
| WO2016022448A1 (en) | 2014-08-08 | 2016-02-11 | Merck Sharp & Dohme Corp. | Antidiabetic bicyclic compounds |
| WO2016022742A1 (en) | 2014-08-08 | 2016-02-11 | 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 |
| CN110719903A (zh) | 2017-03-31 | 2020-01-21 | 武田药品工业株式会社 | 芳族环化合物 |
| SI3752501T1 (sl) | 2018-02-13 | 2023-08-31 | Gilead Sciences, Inc. | Inhibitorji pd-1/pd-l1 |
| CA3093130C (en) | 2018-04-19 | 2023-10-17 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| SI3820572T1 (sl) | 2018-07-13 | 2023-12-29 | Gilead Sciences, Inc. | Inhibitorji pd-1/pd-l1 |
| JP7158577B2 (ja) | 2018-10-24 | 2022-10-21 | ギリアード サイエンシーズ, インコーポレイテッド | Pd-1/pd-l1阻害剤 |
| 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 |
| KR20060135815A (ko) * | 2004-02-17 | 2006-12-29 | 라보라토리오스 델 드라. 에스테브.에스.에이. | 혈중 트리글리세리드를 감소시키기 위한 치환된 피라졸린화합물 |
| EP1637522A1 (en) * | 2004-09-16 | 2006-03-22 | Laboratorios Del Dr. Esteve, S.A. | Substituted pyrazoline compounds for reducing triglycerides in blood |
| US7816367B2 (en) | 2004-02-27 | 2010-10-19 | Amgen Inc. | Compounds, pharmaceutical compositions and methods for use in treating metabolic disorders |
| US7517910B2 (en) | 2004-03-30 | 2009-04-14 | 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 |
| WO2007013689A1 (ja) | 2005-07-29 | 2007-02-01 | Takeda Pharmaceutical Company Limited | シクロプロパンカルボン酸化合物 |
| CA2621949A1 (en) | 2005-09-14 | 2007-03-22 | Amgen Inc. | Conformationally constrained 3- (4-hydroxy-phenyl) - substituted-propanoic acids useful for treating metabolic disorders |
| JP2009530281A (ja) | 2006-03-14 | 2009-08-27 | アムジエン・インコーポレーテツド | 代謝障害の治療に有用である二環式カルボン酸誘導体 |
| CL2007001873A1 (es) | 2006-06-27 | 2008-01-04 | Takeda Pharmaceutical | Acido((3s))-6-((¨2,6-dimetil-4-(3-(metilsulfonil)-propoxi)bifenil-3-il)metoxi-2,3-dihidro-1-benzofuran-3-il)acetico o una sal del mismo |
| EP2064193A1 (en) | 2006-09-07 | 2009-06-03 | Amgen, Inc | Heterocyclic gpr40 modulators |
| WO2008054675A2 (en) | 2006-10-31 | 2008-05-08 | Merck & Co., Inc. | Antidiabetic bicyclic compounds |
| ES2446419T3 (es) | 2007-04-16 | 2014-03-07 | Amgen, Inc | Moduladores de GPR40 de ácidos bifenilfenoxi, tiofenil y aminofenilpropanoico sustituidos |
| WO2009048527A1 (en) | 2007-10-10 | 2009-04-16 | Amgen Inc. | Substituted biphenyl gpr40 modulators |
| MX2010004435A (es) | 2007-10-26 | 2010-05-13 | Japan Tobacco Inc | Compuestos espiro y uso farmaceutico de los mismos. |
| 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 |
| EP2486005B1 (en) * | 2009-10-06 | 2014-06-18 | 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 |
| JP5946192B2 (ja) * | 2010-11-18 | 2016-07-05 | ジェンリン ディスカバリーJenrin Discovery | 肥満症及び糖尿病を含む代謝性疾患の処置に有用なカンナビノイド受容体拮抗薬/逆作動薬 |
| WO2012069917A1 (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 |
| SG11201503556PA (en) * | 2012-11-16 | 2015-06-29 | Bristol Myers Squibb Co | Dihydropyrazole gpr40 modulators |
| US8962660B2 (en) * | 2013-03-14 | 2015-02-24 | Bristol-Myers Squibb Company | Oxabicyclo [2.2.2] acid GPR120 modulators |
-
2013
- 2013-11-15 EA EA201590954A patent/EA026913B1/ru not_active IP Right Cessation
- 2013-11-15 RS RS20161061A patent/RS55363B1/sr unknown
- 2013-11-15 CA CA2891574A patent/CA2891574A1/en not_active Abandoned
- 2013-11-15 SI SI201330340T patent/SI2920165T1/sl unknown
- 2013-11-15 LT LTEP13811645.4T patent/LT2920165T/lt unknown
- 2013-11-15 EP EP13811645.4A patent/EP2920165B1/en active Active
- 2013-11-15 KR KR1020157015541A patent/KR102204804B1/ko not_active Expired - Fee Related
- 2013-11-15 UY UY0001035143A patent/UY35143A/es not_active Application Discontinuation
- 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 DK DK13811645.4T patent/DK2920165T3/en active
- 2013-11-15 ES ES13811645.4T patent/ES2606685T3/es active Active
- 2013-11-15 AU AU2013344604A patent/AU2013344604B2/en not_active Ceased
- 2013-11-15 PL PL13811645T patent/PL2920165T3/pl unknown
- 2013-11-15 WO PCT/US2013/070215 patent/WO2014078610A1/en not_active Ceased
- 2013-11-15 JP JP2015542798A patent/JP6322203B2/ja not_active Expired - Fee Related
- 2013-11-15 HR HRP20161631TT patent/HRP20161631T1/hr unknown
- 2013-11-15 HU HUE13811645A patent/HUE032401T2/en unknown
- 2013-11-15 PT PT138116454T patent/PT2920165T/pt unknown
- 2013-11-15 SG SG11201503558SA patent/SG11201503558SA/en unknown
- 2013-11-15 MX MX2015005735A patent/MX358499B/es active IP Right Grant
- 2013-11-15 CN CN201380059799.5A patent/CN104812748B/zh not_active Expired - Fee Related
- 2013-11-15 TW TW102141762A patent/TW201427971A/zh unknown
-
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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