JP2010519260A5 - - Google Patents
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- Publication number
- JP2010519260A5 JP2010519260A5 JP2009550652A JP2009550652A JP2010519260A5 JP 2010519260 A5 JP2010519260 A5 JP 2010519260A5 JP 2009550652 A JP2009550652 A JP 2009550652A JP 2009550652 A JP2009550652 A JP 2009550652A JP 2010519260 A5 JP2010519260 A5 JP 2010519260A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- compound
- acceptable salt
- pharmaceutical composition
- formula
- 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
- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 8
- 239000011780 sodium chloride Substances 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 239000000969 carrier Substances 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- XEYBRNLFEZDVAW-ARSRFYASSA-N (5Z)-7-[(1R,2R,3R)-3-hydroxy-2-[(1E,3S)-3-hydroxyoct-1-en-1-yl]-5-oxocyclopentyl]hept-5-enoic acid Chemical compound CCCCC[C@H](O)\C=C\[C@H]1[C@H](O)CC(=O)[C@@H]1C\C=C/CCCC(O)=O XEYBRNLFEZDVAW-ARSRFYASSA-N 0.000 claims 2
- 101710011551 PTGER4 Proteins 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 229960002986 dinoprostone Drugs 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000001404 mediated Effects 0.000 claims 2
- 208000005298 Acute Pain Diseases 0.000 claims 1
- 206010002556 Ankylosing spondylitis Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 206010006811 Bursitis Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- HPNMFZURTQLUMO-UHFFFAOYSA-N Diethylamine Chemical compound CCNCC HPNMFZURTQLUMO-UHFFFAOYSA-N 0.000 claims 1
- 206010013935 Dysmenorrhoea Diseases 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 125000001176 L-lysyl group Chemical class [H]N([H])[C@]([H])(C(=O)[*])C([H])([H])C([H])([H])C([H])([H])C(N([H])[H])([H])[H] 0.000 claims 1
- 206010027599 Migraine Diseases 0.000 claims 1
- 208000008085 Migraine Disorders Diseases 0.000 claims 1
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 201000001320 atherosclerosis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 1
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 1
- 201000005569 gout Diseases 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims 1
- 229910052700 potassium Inorganic materials 0.000 claims 1
- 239000011591 potassium Substances 0.000 claims 1
- KEAYESYHFKHZAL-UHFFFAOYSA-N sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
Claims (11)
- 式Ｉ：
Ｘは、−ＣＯＯＨ又はテトラゾリルであり；
Ｒ１及びＲ２は、独立して、ハロ、Ｃ１−４アルキル、Ｃ１−４フルオロアルキル、Ｃ１−４アルコキシ、Ｃ１−４フルオロアルコキシ、及びアセチルからなる群より選択される］
で示される化合物、又はその薬学的に許容され得る塩。 - 式Ｉａ：
で示される請求項１に記載の化合物又はその薬学的に許容され得る塩。 - 式Ｉｂ：
で示される請求項２に記載の化合物又はその薬学的に許容され得る塩。 - 式Ｉｃ：
で示される請求項３に記載の化合物又はその薬学的に許容され得る塩。 - 以下：
- 請求項５に記載の化合物のジエチルアミン、ナトリウム、カリウム、又はＬ−リジン塩。
- １種又はそれ以上の生理学的に許容され得る担体又は賦形剤と混合した、請求項１ないし６のいずれか１項に記載の化合物又はその薬学的に許容され得る塩を含む医薬組成物。
- ヒト又は動物医薬において使用するための、請求項１ないし６のいずれか１項に記載の化合物又は薬学的に許容され得るその誘導体。
- ＥＰ４受容体におけるＰＧＥ２の作用により媒介される症状を治療するための医薬組成物であって、１種又はそれ以上の生理学的に許容され得る担体又は賦形剤と混合した、請求項１ないし６のいずれか１項に記載の化合物又はその薬学的に許容され得る塩を含む前記医薬組成物。
- ＥＰ４受容体におけるＰＧＥ２の作用により媒介される症状を治療するための治療薬製造のための、請求項１に記載の化合物の使用。
- 急性又は慢性疼痛、偏頭痛、変形性関節症、関節リウマチ、若年性関節リウマチ、痛風、滑液包炎、強直性脊椎炎、原発性月経困難症、癌、又はアテローム性動脈硬化症を治療するための医薬組成物であって、１種又はそれ以上の生理学的に許容され得る担体又は賦形剤と混合した、請求項１ないし６のいずれか１項に記載の化合物又はその薬学的に許容され得る塩を含む前記医薬組成物。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US90349407P | 2007-02-26 | 2007-02-26 | |
| US60/903,494 | 2007-02-26 | ||
| PCT/CA2008/000351 WO2008104055A1 (en) | 2007-02-26 | 2008-02-22 | Indole and indoline cyclopropyl amide derivatives as ep4 receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010519260A JP2010519260A (ja) | 2010-06-03 |
| JP2010519260A5 true JP2010519260A5 (ja) | 2011-03-31 |
| JP5301469B2 JP5301469B2 (ja) | 2013-09-25 |
Family
ID=39720805
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009550652A Expired - Fee Related JP5301469B2 (ja) | 2007-02-26 | 2008-02-22 | Ｅｐ４受容体アンタゴニストとしてのインドール及びインドリンシクロプロピルアミド誘導体 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US8158671B2 (ja) |
| EP (1) | EP2114877B1 (ja) |
| JP (1) | JP5301469B2 (ja) |
| CN (1) | CN101622230B (ja) |
| AU (1) | AU2008221194B2 (ja) |
| CA (1) | CA2679175C (ja) |
| ES (1) | ES2400293T3 (ja) |
| WO (1) | WO2008104055A1 (ja) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2141150B1 (en) | 2007-04-26 | 2013-12-11 | Takeda Pharmaceutical Company Limited | Bicyclic compound and pharmaceutical use thereof |
| PT2565191E (pt) | 2008-05-14 | 2014-12-04 | Astellas Pharma Inc | Derivados do ácido 4-(indol-7- ilcarbonilaminometil)ciclo-hexanocarboxílico como antagonistas de receptores ep4, úteis no tratamento de insuficiência renal crónica ou de nefropatia diabética |
| EP2320906B1 (en) * | 2008-08-14 | 2016-02-24 | Beta Pharma Canada Inc. | Heterocyclic amide derivatives as ep4 receptor antagonists |
| US20110287112A1 (en) | 2009-01-30 | 2011-11-24 | Ono Pharmaceutical Co., Ltd. | Prostate cancer progression inhibitor and progression inhibition method |
| WO2010121382A1 (en) * | 2009-04-21 | 2010-10-28 | Merck Frosst Canada Ltd. | Process for making indole cyclopropyl amide derivatives |
| US8536179B2 (en) * | 2010-05-07 | 2013-09-17 | Glaxosmithkline Llc | Indoles |
| HUE031408T2 (en) | 2010-09-21 | 2017-07-28 | Eisai R&D Man Co Ltd | Pharmaceutical preparation |
| US8828987B2 (en) | 2010-12-10 | 2014-09-09 | Rottapharm Biotech S.R.L. | Pyridine amide derivatives as EP4 receptor antagonists |
| RU2565596C2 (ru) | 2011-07-04 | 2015-10-20 | Роттафарм Биотек С.Р.Л. | Производные циклических аминов в качестве антагонистов рецептора ер4 |
| WO2013004291A1 (en) | 2011-07-04 | 2013-01-10 | Rottapharm S.P.A. | Cyclic amine derivatives as ep4 receptor agonists |
| UA115576C2 (uk) | 2012-12-06 | 2017-11-27 | Байєр Фарма Акцієнгезелльшафт | Похідні бензимідазолу як антагоністи ер4 |
| US9295665B2 (en) | 2013-03-12 | 2016-03-29 | Allergan, Inc. | Inhibition of neovascularization by simultaneous inhibition of prostanoid IP and EP4 receptors |
| SG11201510121RA (en) | 2013-06-12 | 2016-01-28 | Kaken Pharma Co Ltd | 4-alkynyl imidazole derivative and medicine comprising same as active ingredient |
| TW201607943A (zh) | 2013-12-19 | 2016-03-01 | 拜耳製藥公司 | 作為ｅｐ４配體之新穎苯并咪唑衍生物 |
| BR112018007664B1 (pt) | 2015-10-16 | 2023-12-19 | Eisai R&D Management Co., Ltd | Compostos antagonistas de ep4, composição compreendendo o composto e uso dos mesmos para tratar câncer |
| CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
| PL3482760T3 (pl) | 2016-07-07 | 2022-02-07 | Ono Pharmaceutical Co., Ltd. | Kombinacja zawierająca antagonistę EP4 i inhibitor immunologicznego punktu kontrolnego |
| WO2018162562A1 (en) | 2017-03-10 | 2018-09-13 | Bayer Pharma Aktiengesellschaft | Use of an ep4 antagonist for the treatment of inflammatory pain |
| AU2018255300B2 (en) | 2017-04-18 | 2021-10-28 | Tempest Therapeutics, Inc. | Bicyclic compounds and their use in the treatment of cancer |
| US11066405B2 (en) * | 2017-04-18 | 2021-07-20 | Tempest Therapeutics, Inc. | Bicyclic compounds and their use in the treatment of cancer |
| KR102612649B1 (ko) | 2017-05-18 | 2023-12-11 | 이도르시아 파마슈티컬스 리미티드 | Pge2 수용체 조절제로서의 벤조푸란 및 벤조티오페논 유도체 |
| PE20191814A1 (es) | 2017-05-18 | 2019-12-27 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores del receptor de pge2 |
| TW201900180A (zh) | 2017-05-18 | 2019-01-01 | 瑞士商愛杜西亞製藥有限公司 | 嘧啶衍生物 |
| HRP20211532T1 (hr) | 2017-05-18 | 2022-01-07 | Idorsia Pharmaceuticals Ltd | N-supstituirani derivati indola |
| JP7159215B2 (ja) | 2017-05-18 | 2022-10-24 | イドーシア ファーマシューティカルズ リミテッド | Ｐｇｅ２レセプター調節剤としてのピリミジン誘導体 |
| WO2019038156A1 (en) | 2017-08-22 | 2019-02-28 | Bayer Pharma Aktiengesellschaft | USE OF AN EP4 ANTAGONIST FOR THE TREATMENT OF ARTHRITIS |
| AU2019229130B2 (en) * | 2018-03-02 | 2021-11-25 | Foshan Ionova Biotherapeutics Co., Inc. | Heterobicyclic carboxylic acids and salts thereof |
| SG11202010153WA (en) | 2018-04-17 | 2020-11-27 | Tempest Therapeutics Inc | Bicyclic carboxamides and methods of use thereof |
| AU2019300449A1 (en) * | 2018-07-12 | 2021-03-04 | Rottapharm Biotech S.R.L. | (R)-4-(1-(1-(4-(trifluoromethyl)benzyl)pyrrolidine-2-carboxamide)cyclopropyl)-benzoic acid as EP4 receptor antagonist |
| AU2020212111A1 (en) | 2019-01-22 | 2021-08-05 | Keythera (Suzhou) Pharmaceuticals Co. Ltd. | Compound for inhibiting PGE2/EP4 signaling transduction inhibiting, preparation method therefor, and medical uses thereof |
| EP3722319A1 (en) | 2019-04-09 | 2020-10-14 | Rottapharm Biotech S.r.l. | Pharmaceutical combination of an ep4 antagonist and immune checkpoint inhibitors for the treatment of tumours |
| EP3827828A1 (en) | 2019-11-29 | 2021-06-02 | Rottapharm Biotech S.r.l. | (r)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)-cyclopropyl) benzoic acid or its salt also in polymorphic form a for use in the prevention of heterotopic ossification |
| WO2021115560A1 (en) | 2019-12-09 | 2021-06-17 | Rottapharm Biotech S.R.L. | New fyn and vegfr2 kinase inhibitors |
| EP3885339A1 (en) | 2020-03-27 | 2021-09-29 | Rottapharm Biotech S.r.l. | Process for the preparation of (r)-4-(1-(6-(4-(trifluoromethyl)benzyl)-6-azaspiro[2.5]octane-5-carboxamido)-cyclopropyl) benzoic acid or a salt thereof |
| JPWO2022102731A1 (ja) | 2020-11-13 | 2022-05-19 | ||
| WO2022247881A1 (zh) * | 2021-05-28 | 2022-12-01 | 凯复(苏州)生物医药有限公司 | 治疗肿瘤的联合疗法 |
| WO2022257960A1 (zh) * | 2021-06-08 | 2022-12-15 | 武汉人福创新药物研发中心有限公司 | 用于治疗ep2、ep4受体介导的疾病的双环化合物 |
| KR20240087749A (ko) * | 2021-08-27 | 2024-06-19 | 키테라 (쑤저우) 바이오-파마슈티컬스 컴퍼니 리미티드 | 인돌 화합물의 고체 형태, 이의 제조 방법 및 이의 용도 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6743793B2 (en) | 2000-03-09 | 2004-06-01 | Ono Pharmaceutical Co., Ltd. | Indole derivatives, process for preparation of the same and use thereof |
| AU2000234451B2 (en) * | 2000-03-24 | 2005-09-29 | Asterand Uk Acquisition Limited | Use of prostanoid ep4 receptor antagonists for the treatment of headache and assays for such antagonists |
| ATE362468T1 (de) | 2000-07-25 | 2007-06-15 | Merck & Co Inc | N-substituierte indole mit anwendung in der behandlung von diabetes |
| WO2005021508A1 (en) * | 2003-09-03 | 2005-03-10 | Pfizer Inc. | Phenyl or pyridyl amide compounds as prostaglandin e2 antagonists |
| EP1885722B1 (en) * | 2005-05-19 | 2011-11-16 | Merck Canada Inc. | Quinoline derivatives as ep4 antagonists |
| US7968578B2 (en) * | 2006-04-24 | 2011-06-28 | Merck Frosst Canada Ltd. | Indole amide derivatives as EP4 receptor antagonists |
| JP5183628B2 (ja) * | 2006-06-12 | 2013-04-17 | メルク カナダ インコーポレイテッド | Ｅｐ４受容体リガンドとしてのインドリンアミド誘導体 |
-
2008
- 2008-02-22 ES ES08714673T patent/ES2400293T3/es active Active
- 2008-02-22 AU AU2008221194A patent/AU2008221194B2/en not_active Ceased
- 2008-02-22 EP EP08714673A patent/EP2114877B1/en active Active
- 2008-02-22 CA CA2679175A patent/CA2679175C/en not_active Expired - Fee Related
- 2008-02-22 WO PCT/CA2008/000351 patent/WO2008104055A1/en active Application Filing
- 2008-02-22 US US12/527,736 patent/US8158671B2/en active Active
- 2008-02-22 CN CN2008800061949A patent/CN101622230B/zh not_active Expired - Fee Related
- 2008-02-22 JP JP2009550652A patent/JP5301469B2/ja not_active Expired - Fee Related
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