JPWO2019204523A5 - - Google Patents
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- Publication number
- JPWO2019204523A5 JPWO2019204523A5 JP2020555164A JP2020555164A JPWO2019204523A5 JP WO2019204523 A5 JPWO2019204523 A5 JP WO2019204523A5 JP 2020555164 A JP2020555164 A JP 2020555164A JP 2020555164 A JP2020555164 A JP 2020555164A JP WO2019204523 A5 JPWO2019204523 A5 JP WO2019204523A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- heterocyclyl
- haloalkyl
- aryl
- 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 107
- 125000001188 haloalkyl group Chemical group 0.000 claims 77
- 125000000623 heterocyclic group Chemical group 0.000 claims 69
- 125000000753 cycloalkyl group Chemical group 0.000 claims 66
- 125000003118 aryl group Chemical group 0.000 claims 61
- 229910052736 halogen Inorganic materials 0.000 claims 55
- 150000002367 halogens Chemical class 0.000 claims 55
- 239000000203 mixture Substances 0.000 claims 52
- 150000003839 salts Chemical class 0.000 claims 52
- 125000001072 heteroaryl group Chemical group 0.000 claims 49
- 239000012453 solvate Substances 0.000 claims 46
- 229910052739 hydrogen Inorganic materials 0.000 claims 42
- 239000001257 hydrogen Substances 0.000 claims 42
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 42
- 150000002431 hydrogen Chemical class 0.000 claims 33
- 150000001875 compounds Chemical class 0.000 claims 30
- 229940002612 prodrug Drugs 0.000 claims 26
- 239000000651 prodrug Substances 0.000 claims 26
- 125000004429 atom Chemical group 0.000 claims 13
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims 7
- 229910052805 deuterium Inorganic materials 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 4
- -1 isotope variants Substances 0.000 claims 4
- 125000006574 non-aromatic ring group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 150000004677 hydrates Chemical class 0.000 claims 3
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 208000005440 Basal Cell Neoplasms Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 208000005016 Intestinal Neoplasms Diseases 0.000 claims 1
- 208000003445 Mouth Neoplasms Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 230000036571 hydration Effects 0.000 claims 1
- 238000006703 hydration reaction Methods 0.000 claims 1
- 201000002313 intestinal cancer Diseases 0.000 claims 1
- 230000000155 isotopic effect Effects 0.000 claims 1
- 210000003292 kidney cell Anatomy 0.000 claims 1
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862659068P | 2018-04-17 | 2018-04-17 | |
| US62/659,068 | 2018-04-17 | ||
| US201862746843P | 2018-10-17 | 2018-10-17 | |
| US62/746,843 | 2018-10-17 | ||
| PCT/US2019/027992 WO2019204523A1 (en) | 2018-04-17 | 2019-04-17 | Bicyclic carboxamides and methods of use thereof |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021521128A JP2021521128A (ja) | 2021-08-26 |
| JP2021521128A5 JP2021521128A5 (https=) | 2022-04-11 |
| JPWO2019204523A5 true JPWO2019204523A5 (https=) | 2022-04-11 |
| JP7361713B2 JP7361713B2 (ja) | 2023-10-16 |
Family
ID=66625250
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020555164A Active JP7361713B2 (ja) | 2018-04-17 | 2019-04-17 | 二環式カルボキサミドおよびその使用方法 |
Country Status (14)
| Country | Link |
|---|---|
| US (5) | US10968201B2 (https=) |
| EP (1) | EP3781550B1 (https=) |
| JP (1) | JP7361713B2 (https=) |
| KR (1) | KR102815312B1 (https=) |
| CN (1) | CN112313208B (https=) |
| AU (2) | AU2019255717B2 (https=) |
| BR (1) | BR112020021042A2 (https=) |
| CA (1) | CA3096894A1 (https=) |
| DK (1) | DK3781550T3 (https=) |
| ES (1) | ES3010282T3 (https=) |
| IL (1) | IL277963B2 (https=) |
| MX (1) | MX2020010879A (https=) |
| SG (1) | SG11202010153WA (https=) |
| WO (1) | WO2019204523A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| IL277963B2 (en) | 2018-04-17 | 2024-09-01 | Tempest Therapeutics Inc | Bicyclic carboxamides and methods of use thereof |
| CN115448882A (zh) * | 2021-06-08 | 2022-12-09 | 武汉人福创新药物研发中心有限公司 | 用于治疗ep2、ep4受体介导的疾病的苯并杂环化合物 |
| CN115448913A (zh) * | 2021-06-08 | 2022-12-09 | 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 |
| CN114085167A (zh) * | 2021-12-13 | 2022-02-25 | 华中药业股份有限公司 | 一种杂质ts-3a的制备方法 |
| WO2024102968A1 (en) * | 2022-11-10 | 2024-05-16 | Tempest Therapeutics, Inc. | Uses of ep2/ep4 antagonist compounds for treating familial adenomatous polyposis (fap) |
| CN118164967A (zh) * | 2022-12-08 | 2024-06-11 | 武汉人福创新药物研发中心有限公司 | 一种ep2、ep4受体拮抗剂 |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR036993A1 (es) | 2001-04-02 | 2004-10-20 | Wyeth Corp | Uso de agentes que modulan la interaccion entre pd-1 y sus ligandos en la submodulacion de respuestas inmunologicas |
| CN1753912B (zh) | 2002-12-23 | 2011-11-02 | 惠氏公司 | 抗pd-1抗体及其用途 |
| WO2005080367A1 (en) | 2004-02-12 | 2005-09-01 | Pharmagene Laboratories Limited | Ep2 receptor agonists |
| RU2494107C2 (ru) | 2005-05-09 | 2013-09-27 | Оно Фармасьютикал Ко., Лтд. | Моноклональные антитела человека к белку программируемой смерти 1 (pd-1) и способы лечения рака с использованием анти-pd-1-антител самостоятельно или в комбинации с другими иммунотерапевтическими средствами |
| JP2007023028A (ja) * | 2005-06-16 | 2007-02-01 | Ono Pharmaceut Co Ltd | 内耳疾患治療剤 |
| CN104356236B (zh) | 2005-07-01 | 2020-07-03 | E.R.施贵宝&圣斯有限责任公司 | 抗程序性死亡配体1(pd-l1)的人单克隆抗体 |
| EP2035376B1 (en) * | 2006-06-12 | 2014-08-27 | Merck Canada Inc. | Indoline amide derivatives as ep4 receptor ligands |
| JP5301469B2 (ja) | 2007-02-26 | 2013-09-25 | メルク カナダ インコーポレイテッド | 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 |
| HRP20131167T1 (hr) | 2007-06-18 | 2014-01-03 | Merck Sharp & Dohme B.V. | Antitijela za humani receptor programirane smrti pd-1 |
| JP5408434B2 (ja) * | 2007-07-03 | 2014-02-05 | アステラス製薬株式会社 | アミド化合物 |
| EP2565191B1 (en) * | 2008-05-14 | 2014-10-08 | Astellas Pharma Inc. | 4-(Indol-7-ylcarbonylaminomethyl)cyclohexanecarboxylic acid derivatives as EP4 receptor antagonists useful for the treatment of chronic renal failure or diabetic nephropathy |
| WO2010014784A2 (en) | 2008-08-01 | 2010-02-04 | Bristol-Myers Squibb Company | Combination of anti-ctla4 antibody with diverse therapeutic regimens for the synergistic treatment of proliferative diseases |
| KR101814408B1 (ko) | 2008-09-26 | 2018-01-04 | 다나-파버 캔서 인스티튜트 인크. | 인간 항-ｐｄ-１, ｐｄ-ｌ１, 및 ｐｄ-ｌ2 항체 및 그의 용도 |
| KR101050829B1 (ko) | 2008-10-02 | 2011-07-20 | 서울대학교산학협력단 | 항 ｐｄ-1 항체 또는 항 ｐｄ-ｌ1 항체를 포함하는 항암제 |
| AU2009333580B2 (en) | 2008-12-09 | 2016-07-07 | Genentech, Inc. | Anti-PD-L1 antibodies and their use to enhance T-cell function |
| WO2010121382A1 (en) * | 2009-04-21 | 2010-10-28 | Merck Frosst Canada Ltd. | Process for making indole cyclopropyl amide derivatives |
| RU2560818C2 (ru) | 2009-04-21 | 2015-08-20 | Эппл Инк | Способ и устройство для определения индикатора качества канала в сетях связи, работающих в режиме mu-mimo |
| EP3375791A1 (en) | 2009-09-30 | 2018-09-19 | Memorial Sloan Kettering Cancer Center | Combination immunotherapy for the treatment of cancer |
| CN103167875A (zh) * | 2010-08-17 | 2013-06-19 | 阿勒根公司 | 用于治疗角膜浑浊的ep2或ep4激动剂 |
| EP2760862B1 (en) * | 2011-09-27 | 2015-10-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| US9655887B2 (en) | 2013-05-23 | 2017-05-23 | Bayer Pharma Aktiengesellschaft | Pharmaceutical composition and the use thereof, and application regime of said pharmaceutical composition for on-demand contraception |
| TWI695831B (zh) * | 2014-09-13 | 2020-06-11 | 香港商南北兄弟藥業投資有限公司 | Ｃｒｔｈ２拮抗劑化合物及其用途 |
| CN108430992A (zh) * | 2015-12-17 | 2018-08-21 | 阿斯特克斯医疗公司 | 作为h-pgds抑制剂的喹啉-3-甲酰胺 |
| TWI730032B (zh) * | 2016-01-13 | 2021-06-11 | 美商必治妥美雅史谷比公司 | 作為ｒｏｃｋ抑制劑之螺庚烷水楊酸醯胺及相關化合物 |
| HUE057799T2 (hu) | 2016-07-07 | 2022-06-28 | Ono Pharmaceutical Co | EP4 antagonistát és immunellenõrzõpont gátlót tartalmazó kombináció |
| 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 |
| IL277963B2 (en) | 2018-04-17 | 2024-09-01 | Tempest Therapeutics Inc | Bicyclic carboxamides and methods of use thereof |
| CN115448882A (zh) | 2021-06-08 | 2022-12-09 | 武汉人福创新药物研发中心有限公司 | 用于治疗ep2、ep4受体介导的疾病的苯并杂环化合物 |
| CN119487006A (zh) | 2022-02-24 | 2025-02-18 | 广东新契生物医药科技有限公司 | 作为pge2受体拮抗剂的酰胺化合物 |
-
2019
- 2019-04-17 IL IL277963A patent/IL277963B2/en unknown
- 2019-04-17 WO PCT/US2019/027992 patent/WO2019204523A1/en not_active Ceased
- 2019-04-17 MX MX2020010879A patent/MX2020010879A/es unknown
- 2019-04-17 DK DK19725441.0T patent/DK3781550T3/da active
- 2019-04-17 CA CA3096894A patent/CA3096894A1/en active Pending
- 2019-04-17 KR KR1020207032916A patent/KR102815312B1/ko active Active
- 2019-04-17 SG SG11202010153WA patent/SG11202010153WA/en unknown
- 2019-04-17 CN CN201980040841.6A patent/CN112313208B/zh active Active
- 2019-04-17 JP JP2020555164A patent/JP7361713B2/ja active Active
- 2019-04-17 US US16/387,294 patent/US10968201B2/en active Active
- 2019-04-17 BR BR112020021042-0A patent/BR112020021042A2/pt active IP Right Grant
- 2019-04-17 EP EP19725441.0A patent/EP3781550B1/en active Active
- 2019-04-17 ES ES19725441T patent/ES3010282T3/es active Active
- 2019-04-17 AU AU2019255717A patent/AU2019255717B2/en active Active
-
2020
- 2020-10-14 US US17/070,554 patent/US11472789B2/en active Active
-
2022
- 2022-06-23 US US17/847,811 patent/US11795156B2/en active Active
-
2023
- 2023-02-28 AU AU2023201228A patent/AU2023201228A1/en not_active Abandoned
- 2023-09-14 US US18/467,022 patent/US12215093B2/en active Active
-
2024
- 2024-12-19 US US18/988,376 patent/US20250353829A1/en active Pending
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