JP2017514865A5 - - Google Patents
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- Publication number
- JP2017514865A5 JP2017514865A5 JP2016566729A JP2016566729A JP2017514865A5 JP 2017514865 A5 JP2017514865 A5 JP 2017514865A5 JP 2016566729 A JP2016566729 A JP 2016566729A JP 2016566729 A JP2016566729 A JP 2016566729A JP 2017514865 A5 JP2017514865 A5 JP 2017514865A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- alkoxy
- independently
- independently selected
- 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 54
- 125000003545 alkoxy group Chemical group 0.000 claims 31
- 229910052736 halogen Inorganic materials 0.000 claims 22
- 150000002367 halogens Chemical class 0.000 claims 22
- 229910052799 carbon Inorganic materials 0.000 claims 16
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 15
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 14
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 10
- 125000004432 carbon atom Chemical group C* 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 239000003814 drug Substances 0.000 claims 9
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 229940079593 drug Drugs 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 150000001721 carbon Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 125000001624 naphthyl group Chemical group 0.000 claims 5
- 125000003831 tetrazolyl group Chemical group 0.000 claims 5
- 125000004414 alkyl thio group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 3
- 102000007330 LDL Lipoproteins Human genes 0.000 claims 3
- 108010007622 LDL Lipoproteins Proteins 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 3
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- 206010060378 Hyperinsulinaemia 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
- 239000002830 appetite depressant Substances 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 201000008980 hyperinsulinism Diseases 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 150000002632 lipids Chemical class 0.000 claims 2
- 208000031225 myocardial ischemia Diseases 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000003003 spiro group Chemical group 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 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
- 208000015943 Coeliac disease Diseases 0.000 claims 1
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic 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
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010021519 Impaired healing Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease 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
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 206010033645 Pancreatitis Diseases 0.000 claims 1
- 201000004681 Psoriasis 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
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 201000011040 acute kidney failure Diseases 0.000 claims 1
- 230000000879 anti-atherosclerotic effect Effects 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
- 230000002253 anti-ischaemic effect Effects 0.000 claims 1
- 230000003063 anti-neuropathic effect Effects 0.000 claims 1
- 230000003579 anti-obesity Effects 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 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
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 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
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 208000004104 gestational diabetes Diseases 0.000 claims 1
- 230000004217 heart function Effects 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 201000008383 nephritis Diseases 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
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 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
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 0 CC(C*)CNC Chemical compound CC(C*)CNC 0.000 description 3
- SWJCAXOOHHKUPF-UHFFFAOYSA-N CC1CCN(C)CCC1 Chemical compound CC1CCN(C)CCC1 SWJCAXOOHHKUPF-UHFFFAOYSA-N 0.000 description 1
- ILBZSNOGPTUKHC-UHFFFAOYSA-N CC1CN(C)C1 Chemical compound CC1CN(C)C1 ILBZSNOGPTUKHC-UHFFFAOYSA-N 0.000 description 1
- MAQVWJNXXNOORL-ORSLSVGZSA-N CCOc(cc1)cc(N(CC2)C[C@@H](C)[C@@H]2Oc(nc2)cnc2N(C2)C(CCC(O)=O)[C@H](C)[C@H]2OC)c1F Chemical compound CCOc(cc1)cc(N(CC2)C[C@@H](C)[C@@H]2Oc(nc2)cnc2N(C2)C(CCC(O)=O)[C@H](C)[C@H]2OC)c1F MAQVWJNXXNOORL-ORSLSVGZSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461989560P | 2014-05-07 | 2014-05-07 | |
| US61/989,560 | 2014-05-07 | ||
| PCT/US2015/029422 WO2015171733A1 (en) | 2014-05-07 | 2015-05-06 | Pyrrolidine gpr40 modulators for the treatment of diseases such as diabetes |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017514865A JP2017514865A (ja) | 2017-06-08 |
| JP2017514865A5 true JP2017514865A5 (https=) | 2018-06-14 |
| JP6488320B2 JP6488320B2 (ja) | 2019-03-20 |
Family
ID=53181360
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016566729A Expired - Fee Related JP6488320B2 (ja) | 2014-05-07 | 2015-05-06 | 糖尿病などの疾患の治療用のピロリジンｇｐｒ４０モジュレータ |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US10017497B2 (https=) |
| EP (1) | EP3140297B1 (https=) |
| JP (1) | JP6488320B2 (https=) |
| KR (1) | KR20170002543A (https=) |
| CN (1) | CN106458987B (https=) |
| AU (1) | AU2015256038B2 (https=) |
| BR (1) | BR112016025188A2 (https=) |
| CA (1) | CA2948175A1 (https=) |
| EA (1) | EA032290B1 (https=) |
| ES (1) | ES2671402T3 (https=) |
| IL (1) | IL248670B (https=) |
| MX (1) | MX2016014118A (https=) |
| SG (1) | SG11201609167RA (https=) |
| WO (1) | WO2015171733A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| TWI707849B (zh) | 2018-02-13 | 2020-10-21 | 美商基利科學股份有限公司 | Pd‐1/pd‐l1抑制劑 |
| KR102591947B1 (ko) | 2018-04-19 | 2023-10-25 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| EP3820572B1 (en) | 2018-07-13 | 2023-08-16 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| US11236085B2 (en) | 2018-10-24 | 2022-02-01 | Gilead Sciences, Inc. | PD-1/PD-L1 inhibitors |
Family Cites Families (9)
| 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 |
| US6995183B2 (en) | 2003-08-01 | 2006-02-07 | Bristol Myers Squibb Company | Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods |
| KR20120104534A (ko) * | 2009-10-06 | 2012-09-21 | 브리스톨-마이어스 스큅 컴퍼니 | 피롤리딘 ｇｐｒ40 조절제 |
| JP5864177B2 (ja) | 2011-09-15 | 2016-02-17 | 船井電機株式会社 | プロジェクタおよびプロジェクタシステム |
| CA2891535A1 (en) * | 2012-11-16 | 2014-05-22 | Bristol-Myers Squibb Company | Dihydropyrazole gpr40 modulators |
| BR112015010649A2 (pt) * | 2012-11-16 | 2017-07-11 | Bristol Myers Squibb Co | moduladores de gpr40 à base de pirrolidina |
| WO2014078610A1 (en) * | 2012-11-16 | 2014-05-22 | Bristol-Myers Squibb Company | Dihydropyrazole gpr40 modulators |
| JP6322204B2 (ja) * | 2012-11-16 | 2018-05-09 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | ジヒドロピラゾールのｇｐｒ４０モジュレーター |
| DK3140296T3 (en) * | 2014-05-07 | 2018-07-23 | Bristol Myers Squibb Co | PYRROLIDIN GPR40 MODULATORS FOR TREATMENT OF DISEASES SUCH AS DIABETES |
-
2015
- 2015-05-06 AU AU2015256038A patent/AU2015256038B2/en not_active Ceased
- 2015-05-06 BR BR112016025188A patent/BR112016025188A2/pt not_active Application Discontinuation
- 2015-05-06 ES ES15723096.2T patent/ES2671402T3/es active Active
- 2015-05-06 EP EP15723096.2A patent/EP3140297B1/en not_active Not-in-force
- 2015-05-06 CN CN201580023783.8A patent/CN106458987B/zh not_active Expired - Fee Related
- 2015-05-06 JP JP2016566729A patent/JP6488320B2/ja not_active Expired - Fee Related
- 2015-05-06 SG SG11201609167RA patent/SG11201609167RA/en unknown
- 2015-05-06 KR KR1020167033864A patent/KR20170002543A/ko not_active Withdrawn
- 2015-05-06 EA EA201692216A patent/EA032290B1/ru not_active IP Right Cessation
- 2015-05-06 WO PCT/US2015/029422 patent/WO2015171733A1/en not_active Ceased
- 2015-05-06 CA CA2948175A patent/CA2948175A1/en not_active Abandoned
- 2015-05-06 MX MX2016014118A patent/MX2016014118A/es unknown
- 2015-05-06 US US15/308,428 patent/US10017497B2/en active Active
-
2016
- 2016-11-01 IL IL248670A patent/IL248670B/en not_active IP Right Cessation
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