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
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 239000000969 carrier Substances 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 208000002193 Pain Diseases 0.000 claims 2
- 101150109738 Ptger4 gene Proteins 0.000 claims 2
- XEYBRNLFEZDVAW-ARSRFYASSA-N dinoprostone 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
- 229960002986 dinoprostone Drugs 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- XEYBRNLFEZDVAW-UHFFFAOYSA-N prostaglandin E2 Natural products CCCCCC(O)C=CC1C(O)CC(=O)C1CC=CCCCC(O)=O XEYBRNLFEZDVAW-UHFFFAOYSA-N 0.000 claims 2
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010006811 Bursitis Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 206010013935 Dysmenorrhoea Diseases 0.000 claims 1
- 201000005569 Gout Diseases 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 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
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 208000019069 chronic childhood arthritis Diseases 0.000 claims 1
- HPNMFZURTQLUMO-UHFFFAOYSA-N diethylamine Chemical compound CCNCC HPNMFZURTQLUMO-UHFFFAOYSA-N 0.000 claims 1
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 1
- 125000003709 fluoroalkyl group Chemical group 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
- 206010027599 migraine Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 229910052700 potassium Inorganic materials 0.000 claims 1
- 239000011591 potassium Substances 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 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
- 229940124597 therapeutic agent Drugs 0.000 claims 1
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 (enExample) | 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 (enExample) |
| EP (1) | EP2114877B1 (enExample) |
| JP (1) | JP5301469B2 (enExample) |
| CN (1) | CN101622230B (enExample) |
| AU (1) | AU2008221194B2 (enExample) |
| CA (1) | CA2679175C (enExample) |
| ES (1) | ES2400293T3 (enExample) |
| WO (1) | WO2008104055A1 (enExample) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8110585B2 (en) | 2007-04-26 | 2012-02-07 | Takeda Pharmaceutical Company Limited | Bicyclic compound and pharmaceutical use thereof |
| SI2565191T1 (sl) | 2008-05-14 | 2014-12-31 | Astellas Pharma Inc. | Derivati 4-(indol-7-ilkarbonilaminometil)cikloheksan karboksilne kisline kot EP4 receptorski antagonisti, uporabni za zdravljenje kronične ledvične odpovedi ali diabetične nefropatije |
| EP2320906B1 (en) * | 2008-08-14 | 2016-02-24 | Beta Pharma Canada Inc. | Heterocyclic amide derivatives as ep4 receptor antagonists |
| WO2010087425A1 (ja) | 2009-01-30 | 2010-08-05 | 国立大学法人京都大学 | 前立腺癌の進行抑制剤および進行抑制方法 |
| WO2010121382A1 (en) * | 2009-04-21 | 2010-10-28 | Merck Frosst Canada Ltd. | Process for making indole cyclopropyl amide derivatives |
| EA023788B1 (ru) * | 2010-05-07 | 2016-07-29 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | Производные индола и фармацевтические композиции на их основе |
| PH12013500467A1 (en) | 2010-09-21 | 2013-04-29 | Eisai R&D Man Co Ltd | Pharmaceutical composition |
| CA2820109C (en) | 2010-12-10 | 2018-01-09 | Rottapharm S.P.A. | Pyridine amide derivatives as ep4 receptor antagonists |
| EP2729141B1 (en) | 2011-07-04 | 2015-12-09 | Rottapharm Biotech S.r.l. | Cyclic amine derivatives as ep4 receptor agonists |
| US9181279B2 (en) | 2011-07-04 | 2015-11-10 | Rottapharm Biotech S.R.L. | Cyclic amine derivatives as EP4 receptor antagonists |
| 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 |
| PT3009426T (pt) | 2013-06-12 | 2018-06-08 | Kaken Pharma Co Ltd | Derivado de 4-alquinilimidazole e medicamento compreendendo o mesmo como ingrediente ativo |
| 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 |
| MX390051B (es) | 2015-10-16 | 2025-03-20 | Eisai R&D Man Co Ltd | Antagonistas de ep4. |
| CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
| TWI795362B (zh) | 2016-07-07 | 2023-03-11 | 日商小野藥品工業股份有限公司 | 拮抗藥與免疫核查點阻礙藥而成之組合 |
| WO2018162562A1 (en) | 2017-03-10 | 2018-09-13 | Bayer Pharma Aktiengesellschaft | Use of an ep4 antagonist for the treatment of inflammatory pain |
| US11066405B2 (en) * | 2017-04-18 | 2021-07-20 | Tempest Therapeutics, Inc. | Bicyclic compounds and their use in the treatment of cancer |
| AU2018255300B2 (en) * | 2017-04-18 | 2021-10-28 | Tempest Therapeutics, Inc. | Bicyclic compounds and their use in the treatment of cancer |
| MX388257B (es) | 2017-05-18 | 2025-03-19 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores del receptor de pge2. |
| AR111941A1 (es) | 2017-05-18 | 2019-09-04 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores del receptor de pge2 |
| JP7093791B2 (ja) | 2017-05-18 | 2022-06-30 | 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ベンゾフラン及びベンゾチオフェン誘導体 |
| US20200069686A1 (en) | 2017-05-18 | 2020-03-05 | Idorsia Pharmaceuticals Ltd | N-substituted indole derivatives |
| EP3625223B1 (en) | 2017-05-18 | 2021-08-11 | Idorsia Pharmaceuticals Ltd | Pyrimidine derivatives |
| WO2019038156A1 (en) | 2017-08-22 | 2019-02-28 | Bayer Pharma Aktiengesellschaft | USE OF AN EP4 ANTAGONIST FOR THE TREATMENT OF ARTHRITIS |
| CA3092310C (en) | 2018-03-02 | 2024-01-02 | Shenzhen Ionova Life Science Co., Ltd. | Heterobicyclic carboxylic acids and salts thereof |
| KR102815312B1 (ko) | 2018-04-17 | 2025-05-30 | 템페스트 테라퓨틱스, 인크. | 비시클릭 카르복스아미드 및 그의 사용 방법 |
| ES2948293T3 (es) | 2018-07-12 | 2023-09-07 | Rottapharm Biotech Srl | Acido (R)-4-(1-(1-(4-(trifluorometil)bencil)pirrolidina-2-carboxamida)ciclopropil)-benzoico como antagonista del receptor EP4 |
| KR102861190B1 (ko) * | 2019-01-22 | 2025-09-17 | 키테라 (쑤저우) 바이오-파마슈티컬스 컴퍼니 리미티드 | Pge2/ep4 신호 전달을 억제하기 위한 화합물, 이의 제조 방법, 및 이의 의약적 용도 |
| 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 |
| EP4245301A4 (en) | 2020-11-13 | 2024-08-21 | ONO Pharmaceutical Co., Ltd. | TREATMENT OF CANCER BY COMBINED USE OF AN EP4 ANTAGONIST AND AN IMMUNE CHECKPOINT INHIBITOR |
| CN117377471A (zh) * | 2021-05-28 | 2024-01-09 | 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 |
| EP4393906A4 (en) * | 2021-08-27 | 2026-03-04 | Keythera Suzhou Bio Pharmaceuticals Co Ltd | Solid form of an indole compound, method of manufacture thereof and use thereof |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA02008801A (es) * | 2000-03-09 | 2003-07-07 | Ono Pharmaceutical Co | Derivados de indol, proceso para la preparacion de los mismos y su uso. |
| JP2003528144A (ja) * | 2000-03-24 | 2003-09-24 | ファーマジーン ラボラトリーズ リミテッド | 頭痛治療のためのプロスタノイドｅｐ４受容体アンタゴニストの使用およびそのアンタゴニストについてのアッセイ |
| CA2415742A1 (en) * | 2000-07-25 | 2002-01-31 | Merck & Co., Inc. | N-substituted indoles useful in the treatment of diabetes |
| RS20060143A (sr) * | 2003-09-03 | 2008-06-05 | Pfizer Inc., | Jedinjenja fenil ili piridil amida kao antagonisti prostaglandina e2 |
| ATE533766T1 (de) * | 2005-05-19 | 2011-12-15 | Merck Canada Inc | Chinolinderivate als ep4-antagonisten |
| CA2648729A1 (en) * | 2006-04-24 | 2007-11-01 | Merck Frosst Canada Ltd. | Indole amide derivatives as ep4 receptor antagonists |
| US7705035B2 (en) * | 2006-06-12 | 2010-04-27 | Merck Frosst Canada Ltd. | Indoline amide derivatives as EP4 receptor ligands |
-
2008
- 2008-02-22 US US12/527,736 patent/US8158671B2/en active Active
- 2008-02-22 AU AU2008221194A patent/AU2008221194B2/en not_active Ceased
- 2008-02-22 CA CA2679175A patent/CA2679175C/en not_active Expired - Fee Related
- 2008-02-22 EP EP08714673A patent/EP2114877B1/en active Active
- 2008-02-22 JP JP2009550652A patent/JP5301469B2/ja not_active Expired - Fee Related
- 2008-02-22 CN CN2008800061949A patent/CN101622230B/zh not_active Expired - Fee Related
- 2008-02-22 WO PCT/CA2008/000351 patent/WO2008104055A1/en not_active Ceased
- 2008-02-22 ES ES08714673T patent/ES2400293T3/es active Active