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 |
|---|---|---|---|
| EP16195431.8 | 2016-10-25 | ||
| EP16195431 | 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 (enExample) | 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 (enExample) |
| EP (1) | EP3532458B1 (enExample) |
| JP (1) | JP7050797B2 (enExample) |
| CN (1) | CN110088089B (enExample) |
| WO (1) | WO2018077699A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10919859B2 (en) * | 2017-01-26 | 2021-02-16 | Boehringer Ingelheim International Gmbh | Benzylaminopyridylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof |
| CN110198928B (zh) * | 2017-01-26 | 2023-08-29 | 勃林格殷格翰国际有限公司 | 苄氧基吡啶基环丙烷甲酸、其药物组合物和用途 |
| US10793530B2 (en) | 2017-01-26 | 2020-10-06 | Boehringer Ingelheim International Gmbh | Benzylaminopyrazinylcyclopropanecarboxylic 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 |
| CR20200347A (es) | 2018-02-13 | 2020-09-23 | Gilead Sciences Inc | Inhibidores pd-1/pd-l1 |
| TWI712412B (zh) | 2018-04-19 | 2020-12-11 | 美商基利科學股份有限公司 | Pd‐1/pd‐l1抑制劑 |
| SG11202012425QA (en) | 2018-07-13 | 2021-01-28 | Gilead Sciences Inc | Pd-1/pd-l1 inhibitors |
| WO2020086556A1 (en) | 2018-10-24 | 2020-04-30 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| KR20220150270A (ko) | 2019-10-07 | 2022-11-10 | 칼리오페, 인크. | Gpr119 효능제 |
| 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 |
| 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 |
| CA2505322A1 (en) * | 2002-11-08 | 2004-05-21 | Takeda Pharmaceutical Company Limited | Receptor function regulator |
| EP1630152A4 (en) | 2003-05-30 | 2009-09-23 | Takeda Pharmaceutical | CONDENSED CYCLIC COMPOUND |
| US7834013B2 (en) | 2003-11-19 | 2010-11-16 | Glaxosmithkline Llc | Aminophenylcyclopropyl carboxylic acids and derivatives as agonists to GPR40 |
| JP4875978B2 (ja) | 2004-03-15 | 2012-02-15 | 武田薬品工業株式会社 | アミノフェニルプロパン酸誘導体 |
| 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 |
| PE20061127A1 (es) | 2005-02-15 | 2006-10-21 | Glaxo Group Ltd | Derivados de propanosulfonamida que potencian el receptor de glutamato |
| EP1866278A1 (en) | 2005-03-28 | 2007-12-19 | Pfizer, 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 |
| EP1916234B1 (en) * | 2005-07-29 | 2014-11-12 | Takeda Pharmaceutical Company Limited | Cyclopropanecarboxylic acid compound |
| EP1924546A1 (en) | 2005-09-14 | 2008-05-28 | Amgen, Inc | Conformationally constrained 3- (4-hydroxy-phenyl) - substituted-propanoic acids useful for treating metabolic disorders |
| WO2007104717A1 (en) | 2006-03-15 | 2007-09-20 | Neurosearch A/S | Quinazolinones and their use as potassium channels activators |
| 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 |
| KR20110027657A (ko) | 2008-06-25 | 2011-03-16 | 다이이찌 산쿄 가부시키가이샤 | 카르복실산 화합물 |
| 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 |
| AU2011256444B2 (en) | 2010-05-18 | 2014-07-10 | Merck Sharp & Dohme Corp. | Spiro isoxazoline compounds as SSTR5 antagonists |
| JP5945545B2 (ja) | 2011-02-17 | 2016-07-05 | 武田薬品工業株式会社 | 光学活性なジヒドロベンゾフラン誘導体の製造法 |
| US8633182B2 (en) | 2012-05-30 | 2014-01-21 | Boehringer Ingelheim International Gmbh | Indanyloxyphenylcyclopropanecarboxylic acids |
| CN104684907A (zh) * | 2012-08-02 | 2015-06-03 | 默沙东公司 | 抗糖尿病的三环化合物 |
| RU2015106909A (ru) | 2012-08-02 | 2016-09-27 | Мерк Шарп И Доум Корп. | Антидиабетические трициклические соединения |
| 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 WO PCT/EP2017/076618 patent/WO2018077699A1/en not_active Ceased
- 2017-10-18 CN CN201780078329.1A patent/CN110088089B/zh active Active
- 2017-10-18 US US16/340,151 patent/US10538490B2/en active Active
- 2017-10-18 JP JP2019542787A patent/JP7050797B2/ja active Active
- 2017-10-18 EP EP17784652.4A patent/EP3532458B1/en active Active