JP2020517616A5 - - Google Patents
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- Publication number
- JP2020517616A5 JP2020517616A5 JP2019556633A JP2019556633A JP2020517616A5 JP 2020517616 A5 JP2020517616 A5 JP 2020517616A5 JP 2019556633 A JP2019556633 A JP 2019556633A JP 2019556633 A JP2019556633 A JP 2019556633A JP 2020517616 A5 JP2020517616 A5 JP 2020517616A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cancer
- aryl
- haloalkyl
- heteroaryl
- 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 20
- 125000003118 aryl group Chemical group 0.000 claims 18
- 125000001072 heteroaryl group Chemical group 0.000 claims 16
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 14
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 12
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 150000002367 halogens Chemical class 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- 239000012453 solvate Substances 0.000 claims 12
- 239000000203 mixture Substances 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 229940002612 prodrug Drugs 0.000 claims 6
- 239000000651 prodrug Substances 0.000 claims 6
- KJUGUADJHNHALS-UHFFFAOYSA-N 1H-tetrazole Chemical compound C=1N=NNN=1 KJUGUADJHNHALS-UHFFFAOYSA-N 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 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
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- -1 heteroaryl aryl Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 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
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- LZTSCEYDCZBRCJ-UHFFFAOYSA-N 1,2-dihydro-1,2,4-triazol-3-one Chemical compound OC=1N=CNN=1 LZTSCEYDCZBRCJ-UHFFFAOYSA-N 0.000 claims 1
- JXBKZAYVMSNKHA-UHFFFAOYSA-N 1h-tetrazol-1-ium-5-olate Chemical compound OC=1N=NNN=1 JXBKZAYVMSNKHA-UHFFFAOYSA-N 0.000 claims 1
- LYGLYFUBLZCHCT-UHFFFAOYSA-N 2h-1,2,4-oxadiazole-5-thione Chemical compound SC1=NC=NO1 LYGLYFUBLZCHCT-UHFFFAOYSA-N 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
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 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
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 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
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 201000002313 intestinal cancer Diseases 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
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762486765P | 2017-04-18 | 2017-04-18 | |
| US62/486,765 | 2017-04-18 | ||
| PCT/US2018/028034 WO2018195123A1 (en) | 2017-04-18 | 2018-04-17 | Bicyclic compounds and their use in the treatment of cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020517616A JP2020517616A (ja) | 2020-06-18 |
| JP2020517616A5 true JP2020517616A5 (https=) | 2021-04-08 |
| JP7264060B2 JP7264060B2 (ja) | 2023-04-25 |
Family
ID=62111266
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019556633A Active JP7264060B2 (ja) | 2017-04-18 | 2018-04-17 | 二環式化合物および癌の処置におけるそれらの使用 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US11738009B2 (https=) |
| EP (1) | EP3612517B1 (https=) |
| JP (1) | JP7264060B2 (https=) |
| KR (1) | KR102588955B1 (https=) |
| CN (1) | CN110891935B (https=) |
| AU (1) | AU2018255300B2 (https=) |
| CA (1) | CA3060554A1 (https=) |
| DK (1) | DK3612517T3 (https=) |
| EA (1) | EA038381B1 (https=) |
| ES (1) | ES2914311T3 (https=) |
| IL (1) | IL270021B (https=) |
| MX (1) | MX393318B (https=) |
| SG (1) | SG11201909730PA (https=) |
| WO (1) | WO2018195123A1 (https=) |
| ZA (1) | ZA201906947B (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11066405B2 (en) | 2017-04-18 | 2021-07-20 | Tempest Therapeutics, Inc. | Bicyclic compounds and their use in the treatment of cancer |
| WO2018195123A1 (en) | 2017-04-18 | 2018-10-25 | Tempest Therapeutics, Inc. | Bicyclic compounds and their use in the treatment of cancer |
| US10968201B2 (en) * | 2018-04-17 | 2021-04-06 | Tempest Therapeutics, Inc. | Bicyclic carboxamides and methods of use thereof |
| EP3876939A4 (en) | 2018-11-07 | 2022-08-10 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| EP3877371A4 (en) | 2018-11-07 | 2022-07-27 | Dana-Farber Cancer Institute, Inc. | IMIDAZOPYRIDINE DERIVATIVES AND AZA-IMIDAZOPYRIDINE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND USES THEREOF |
| US12522583B2 (en) | 2018-11-07 | 2026-01-13 | Dana-Farber Cancer Institute, Inc. | Benzimidazole derivatives and aza-benzimidazole derivatives as Janus kinase 2 inhibitors and uses thereof |
| US12240812B2 (en) | 2019-01-22 | 2025-03-04 | Keythera (Suzhou) Pharmaceuticals Co. Ltd. | Compound for inhibiting PGE2/EP4 signaling transduction inhibiting, preparation method therefor, and medical uses thereof |
| WO2020251957A1 (en) * | 2019-06-11 | 2020-12-17 | Teon Therapeutics, Inc. | Prostaglandin e2 receptor 4 antagonists and uses thereof |
| US11691963B2 (en) | 2020-05-06 | 2023-07-04 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors |
| CN113512025B (zh) * | 2020-07-31 | 2023-01-06 | 四川大学 | 一种吲唑酯类化合物及其制药用途 |
| TWI854147B (zh) * | 2020-08-21 | 2024-09-01 | 南韓商治納輔醫藥科技有限公司 | 對前列腺素e2受體具有抑制活性的新穎化合物及其用途 |
| US20230390303A1 (en) | 2020-11-13 | 2023-12-07 | Ono Pharmaceutical Co., Ltd. | Cancer treatment by combination of ep4 antagonist and immune checkpoint inhibitor |
| US12043632B2 (en) | 2020-12-23 | 2024-07-23 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors |
| TW202241909A (zh) * | 2021-01-28 | 2022-11-01 | 大陸商深圳晶泰科技有限公司 | 雜環醯胺衍生物及其製備方法和應用 |
| CN113264843B (zh) * | 2021-04-15 | 2022-09-27 | 台州学院 | 一种3-氨基二环[1.1.1]戊烷-1-羧酸酯类衍生物的合成方法 |
| 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 |
| WO2022257961A1 (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受体介导的疾病的苯并杂环化合物 |
| 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 |
| US12162881B2 (en) | 2021-11-09 | 2024-12-10 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of JAK2 |
| WO2023086319A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | 6-he tero aryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| CN119013017A (zh) * | 2022-02-15 | 2024-11-22 | 治纳辅医药科技有限公司 | 包含抗癌剂和对前列腺素e2受体具有抑制活性的新化合物的用于治疗癌症的药物组合物 |
| 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 |
| CN114886892B (zh) * | 2022-05-07 | 2023-09-12 | 四川大学 | 氧化吲哚螺双环[2,2,1]庚烷类化合物在制备治疗胃癌药物中的应用 |
| WO2024120512A1 (zh) * | 2022-12-08 | 2024-06-13 | 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 (24)
| 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 |
| CN101899114A (zh) | 2002-12-23 | 2010-12-01 | 惠氏公司 | 抗pd-1抗体及其用途 |
| DK2439273T3 (da) | 2005-05-09 | 2019-06-03 | Ono Pharmaceutical Co | Humane monoklonale antistoffer til programmeret død-1(pd-1) og fremgangsmåder til behandling af cancer ved anvendelse af anti-pd-1- antistoffer alene eller i kombination med andre immunterapeutika |
| JP2007023028A (ja) | 2005-06-16 | 2007-02-01 | Ono Pharmaceut Co Ltd | 内耳疾患治療剤 |
| PT1907424E (pt) | 2005-07-01 | 2015-10-09 | Squibb & Sons Llc | Anticorpos monoclonais humanos para o ligando 1 de morte programada (pd-l1) |
| WO2007143825A1 (en) | 2006-06-12 | 2007-12-21 | Merck Frosst Canada Ltd. | Indoline amide derivatives as ep4 receptor ligands |
| CA2679175C (en) | 2007-02-26 | 2015-01-13 | Merck Frosst Canada Ltd. | Indole and indoline cyclopropyl amide derivatives as ep4 receptor antagonists |
| BR122017025062B8 (pt) | 2007-06-18 | 2021-07-27 | Merck Sharp & Dohme | anticorpo monoclonal ou fragmento de anticorpo para o receptor de morte programada humano pd-1, polinucleotídeo e composição compreendendo o referido anticorpo ou fragmento |
| 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 |
| US8552154B2 (en) | 2008-09-26 | 2013-10-08 | Emory University | Anti-PD-L1 antibodies and uses therefor |
| KR101050829B1 (ko) | 2008-10-02 | 2011-07-20 | 서울대학교산학협력단 | 항 ｐｄ-1 항체 또는 항 ｐｄ-ｌ1 항체를 포함하는 항암제 |
| EP3255060A1 (en) | 2008-12-09 | 2017-12-13 | F. Hoffmann-La Roche AG | Anti-pd-l1 antibodies and their use to enhance t-cell function |
| KR101664517B1 (ko) | 2009-04-21 | 2016-10-11 | 애플 인크. | 다중 사용자-ｍｉｍｏ 통신 네트워크에서의 채널 품질 지수를 결정하는 방법 및 장치 |
| WO2010121382A1 (en) * | 2009-04-21 | 2010-10-28 | Merck Frosst Canada Ltd. | Process for making indole cyclopropyl amide derivatives |
| EP2482849B1 (en) | 2009-09-30 | 2018-06-06 | Memorial Sloan-Kettering Cancer Center | Combination immunotherapy for the treatment of cancer |
| BR112013003600A2 (pt) | 2010-08-17 | 2016-08-16 | Allergan Inc | agonistas ep2 ou ep4 para o tratamento de névoa da córnea |
| 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 |
| PT3482760T (pt) * | 2016-07-07 | 2021-12-15 | Ono Pharmaceutical Co | Combinação compreendendo antagonista de ep4 e inibidor de ponto de verificação imunitário |
| US11066405B2 (en) | 2017-04-18 | 2021-07-20 | Tempest Therapeutics, Inc. | Bicyclic compounds and their use in the treatment of cancer |
| WO2018195123A1 (en) | 2017-04-18 | 2018-10-25 | Tempest Therapeutics, Inc. | Bicyclic compounds and their use in the treatment of cancer |
| US10968201B2 (en) | 2018-04-17 | 2021-04-06 | Tempest Therapeutics, Inc. | Bicyclic carboxamides and methods of use thereof |
-
2018
- 2018-04-17 WO PCT/US2018/028034 patent/WO2018195123A1/en not_active Ceased
- 2018-04-17 AU AU2018255300A patent/AU2018255300B2/en active Active
- 2018-04-17 DK DK18722359.9T patent/DK3612517T3/da active
- 2018-04-17 SG SG11201909730P patent/SG11201909730PA/en unknown
- 2018-04-17 KR KR1020197033510A patent/KR102588955B1/ko active Active
- 2018-04-17 JP JP2019556633A patent/JP7264060B2/ja active Active
- 2018-04-17 MX MX2019012541A patent/MX393318B/es unknown
- 2018-04-17 ES ES18722359T patent/ES2914311T3/es active Active
- 2018-04-17 IL IL270021A patent/IL270021B/en unknown
- 2018-04-17 CN CN201880040801.7A patent/CN110891935B/zh active Active
- 2018-04-17 EP EP18722359.9A patent/EP3612517B1/en active Active
- 2018-04-17 EA EA201992418A patent/EA038381B1/ru unknown
- 2018-04-17 CA CA3060554A patent/CA3060554A1/en active Pending
- 2018-04-17 US US16/605,408 patent/US11738009B2/en active Active
-
2019
- 2019-10-22 ZA ZA2019/06947A patent/ZA201906947B/en unknown
-
2021
- 2021-06-22 US US17/354,010 patent/US11638704B2/en active Active
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