JP2019532110A5 - - Google Patents
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- Publication number
- JP2019532110A5 JP2019532110A5 JP2019542787A JP2019542787A JP2019532110A5 JP 2019532110 A5 JP2019532110 A5 JP 2019532110A5 JP 2019542787 A JP2019542787 A JP 2019542787A JP 2019542787 A JP2019542787 A JP 2019542787A JP 2019532110 A5 JP2019532110 A5 JP 2019532110A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- cycloalkyl
- heterocyclyl
- replaced
- 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
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 44
- 229910052731 fluorine Inorganic materials 0.000 claims description 36
- -1 NC- Chemical group 0.000 claims description 30
- 125000001072 heteroaryl group Chemical group 0.000 claims description 30
- 229910052801 chlorine Inorganic materials 0.000 claims description 28
- 150000001875 compounds Chemical class 0.000 claims description 25
- 150000003839 salts Chemical class 0.000 claims description 25
- 125000000623 heterocyclic group Chemical group 0.000 claims description 20
- 229910052799 carbon Inorganic materials 0.000 claims description 17
- 125000000217 alkyl group Chemical group 0.000 claims description 14
- 125000001153 fluoro group Chemical group F* 0.000 claims description 12
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 10
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 10
- 125000006704 (C5-C6) cycloalkyl group Chemical group 0.000 claims description 9
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 8
- 125000003566 oxetanyl group Chemical group 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 8
- 125000004632 tetrahydrothiopyranyl group Chemical group S1C(CCCC1)* 0.000 claims description 8
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 238000011282 treatment Methods 0.000 claims description 5
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 4
- 208000008589 Obesity Diseases 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- 125000005842 heteroatom Chemical group 0.000 claims description 4
- 235000020824 obesity Nutrition 0.000 claims description 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 125000001424 substituent group Chemical group 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 3
- 208000032928 Dyslipidaemia Diseases 0.000 claims description 3
- 208000017170 Lipid metabolism disease Diseases 0.000 claims description 3
- 239000000969 carrier Substances 0.000 claims description 3
- 230000002265 prevention Effects 0.000 claims description 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 2
- 206010022489 Insulin Resistance Diseases 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 201000010099 disease Diseases 0.000 description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 4
- 239000003795 chemical substances by application Substances 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 102100026148 Free fatty acid receptor 1 Human genes 0.000 description 2
- 101000912510 Homo sapiens Free fatty acid receptor 1 Proteins 0.000 description 2
- 206010012601 diabetes mellitus Diseases 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 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 description 2
- 208000030159 metabolic disease Diseases 0.000 description 2
- 125000003373 pyrazinyl group Chemical group 0.000 description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 206010019280 Heart failures Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 102000004877 Insulin Human genes 0.000 description 1
- 108090001061 Insulin Proteins 0.000 description 1
- 206010033307 Overweight Diseases 0.000 description 1
- 239000003472 antidiabetic agent Substances 0.000 description 1
- 229940125708 antidiabetic agent Drugs 0.000 description 1
- 229940125396 insulin Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16195431 | 2016-10-25 | ||
| EP16195431.8 | 2016-10-25 | ||
| PCT/EP2017/076618 WO2018077699A1 (en) | 2016-10-25 | 2017-10-18 | Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019532110A JP2019532110A (ja) | 2019-11-07 |
| JP2019532110A5 true JP2019532110A5 (https=) | 2020-11-19 |
| JP7050797B2 JP7050797B2 (ja) | 2022-04-08 |
Family
ID=57189967
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019542787A Active JP7050797B2 (ja) | 2016-10-25 | 2017-10-18 | ベンジルアミノピリジルシクロプロパンカルボン酸、その医薬組成物および使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US10538490B2 (https=) |
| EP (1) | EP3532458B1 (https=) |
| JP (1) | JP7050797B2 (https=) |
| CN (1) | CN110088089B (https=) |
| WO (1) | WO2018077699A1 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110177773B (zh) * | 2017-01-26 | 2023-08-25 | 勃林格殷格翰国际有限公司 | 苄基氨基吡啶基环丙烷羧酸、其药物组合物及其用途 |
| EP3573959B1 (en) | 2017-01-26 | 2021-07-28 | Boehringer Ingelheim International GmbH | Benzylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof |
| US10913720B2 (en) * | 2017-01-26 | 2021-02-09 | Boehringer Ingelheim International Gmbh | Benzyloxypyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof |
| 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 |
| JP2022552655A (ja) | 2019-10-07 | 2022-12-19 | キャリーオペ，インク． | Ｇｐｒ１１９アゴニスト |
| 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 |
| WO2024211164A2 (en) * | 2023-04-03 | 2024-10-10 | Trustees Of Dartmouth College | Fatty acid mimetics as modulators of gpr40 and/or gpr120 |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US628476A (en) | 1898-03-18 | 1899-07-11 | Joseph Howard Kirk | Junction of cycle, motor-car, or other frames, &c. |
| EP1236723A1 (en) | 2001-03-01 | 2002-09-04 | Pfizer Products Inc. | Sulfamide derivatives useful as beta3 agonists and pharmaceutical uses thereof |
| AU2003277576A1 (en) | 2002-11-08 | 2004-06-07 | Takeda Pharmaceutical Company Limited | Receptor function controlling agent |
| EP1630152A4 (en) | 2003-05-30 | 2009-09-23 | Takeda Pharmaceutical | CONDENSED CYCLIC COMPOUND |
| WO2005051890A1 (en) * | 2003-11-19 | 2005-06-09 | Smithkline Beecham Corporation | Aminophenylcyclopropyl carboxylic acids and derivatives as agonists to gpr40 |
| US7786165B2 (en) * | 2004-03-15 | 2010-08-31 | Takeda Pharmaceutical Company Limited | Aminophenylpropanoic acid derivative |
| DE102004017930A1 (de) | 2004-04-14 | 2005-11-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Alkin-Verbindungen mit MCH-antagonistischer Wirkung und diese Verbindungen enthaltende Arzneimittel |
| JP2008530162A (ja) | 2005-02-15 | 2008-08-07 | グラクソ グループ リミテッド | グルタミン酸受容体を増強する化合物および医薬におけるそれらの使用 |
| WO2006103503A1 (en) | 2005-03-28 | 2006-10-05 | Pfizer Japan Inc. | Substituted aryloxoethyl cyclopropanecarboxamide compounds as vr1 receptor antagonists |
| EP1741708A1 (en) | 2005-06-28 | 2007-01-10 | Sanofi-Aventis Deutschland GmbH | Heteroaryl-substituted amides comprising an unsaturated or cyclic linker group, and their use as pharmaceuticals |
| 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 |
| JP2009530237A (ja) | 2006-03-15 | 2009-08-27 | ノイロサーチ アクティーゼルスカブ | キナゾリノン及びカリウムチャネル活性化剤としてのその使用 |
| TW200838526A (en) * | 2006-12-01 | 2008-10-01 | Astellas Pharma Inc | Carboxylic acid derivatives |
| JP2011016722A (ja) * | 2007-10-23 | 2011-01-27 | Astellas Pharma Inc | チアゾリジンジオン化合物 |
| NZ588983A (en) | 2008-06-25 | 2011-11-25 | Daiichi Sankyo Co Ltd | Carboxylic acid compound |
| WO2010051819A1 (en) | 2008-11-10 | 2010-05-14 | Neurosearch A/S | Novel 2,3-diamino-quinazolinone derivatives and their medical use |
| WO2011094890A1 (en) | 2010-02-02 | 2011-08-11 | Argusina Inc. | Phenylalanine derivatives and their use as non-peptide glp-1 receptor modulators |
| CA2799414A1 (en) | 2010-05-18 | 2011-11-24 | Merck Sharp & Dohme Corp. | Spiro isoxazoline compounds as sstr5 antagonists |
| WO2012111849A1 (en) | 2011-02-17 | 2012-08-23 | Takeda Pharmaceutical Company Limited | Production method of optically active dihydrobenzofuran derivative |
| US8633182B2 (en) | 2012-05-30 | 2014-01-21 | Boehringer Ingelheim International Gmbh | Indanyloxyphenylcyclopropanecarboxylic acids |
| US9527875B2 (en) * | 2012-08-02 | 2016-12-27 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| CN104684907A (zh) * | 2012-08-02 | 2015-06-03 | 默沙东公司 | 抗糖尿病的三环化合物 |
| JP2015026445A (ja) | 2013-07-24 | 2015-02-05 | 株式会社オートネットワーク技術研究所 | コネクタ用端子 |
| WO2015051496A1 (en) | 2013-10-08 | 2015-04-16 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| AU2015220427B2 (en) | 2014-02-19 | 2017-09-21 | Piramal Enterprises Limited | Compounds for use as GPR120 agonists |
-
2017
- 2017-10-18 CN CN201780078329.1A patent/CN110088089B/zh active Active
- 2017-10-18 EP EP17784652.4A patent/EP3532458B1/en active Active
- 2017-10-18 JP JP2019542787A patent/JP7050797B2/ja active Active
- 2017-10-18 US US16/340,151 patent/US10538490B2/en active Active
- 2017-10-18 WO PCT/EP2017/076618 patent/WO2018077699A1/en not_active Ceased