JP2020514333A5 - - Google Patents
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- JP2020514333A5 JP2020514333A5 JP2019547662A JP2019547662A JP2020514333A5 JP 2020514333 A5 JP2020514333 A5 JP 2020514333A5 JP 2019547662 A JP2019547662 A JP 2019547662A JP 2019547662 A JP2019547662 A JP 2019547662A JP 2020514333 A5 JP2020514333 A5 JP 2020514333A5
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- JP
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- Prior art keywords
- substituted
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- unsubstituted
- alkyl
- och
- 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.)
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- -1 dioxolyl Chemical group 0.000 claims 27
- 229910052739 hydrogen Inorganic materials 0.000 claims 27
- 229910052805 deuterium Inorganic materials 0.000 claims 26
- 150000001875 compounds Chemical class 0.000 claims 24
- 150000003839 salts Chemical class 0.000 claims 24
- 239000012453 solvate Substances 0.000 claims 24
- PNZXMIKHJXIPEK-UHFFFAOYSA-N cyclohexanecarboxamide Chemical compound NC(=O)C1CCCCC1 PNZXMIKHJXIPEK-UHFFFAOYSA-N 0.000 claims 20
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 14
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 7
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 6
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 6
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 208000019425 cirrhosis of liver Diseases 0.000 claims 5
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 4
- 208000007082 Alcoholic Fatty Liver Diseases 0.000 claims 4
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 4
- 208000018522 Gastrointestinal disease Diseases 0.000 claims 4
- 241000711549 Hepacivirus C Species 0.000 claims 4
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 4
- 208000026594 alcoholic fatty liver disease Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 3
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 3
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 208000006454 hepatitis Diseases 0.000 claims 3
- 210000004185 liver Anatomy 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 3
- 208000015943 Coeliac disease Diseases 0.000 claims 2
- 208000004232 Enteritis Diseases 0.000 claims 2
- 241000700721 Hepatitis B virus Species 0.000 claims 2
- 206010019799 Hepatitis viral Diseases 0.000 claims 2
- 208000002972 Hepatolenticular Degeneration Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 208000025865 Ulcer Diseases 0.000 claims 2
- 208000018839 Wilson disease Diseases 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 230000001684 chronic effect Effects 0.000 claims 2
- 125000004976 cyclobutylene group Chemical group 0.000 claims 2
- 125000004980 cyclopropylene group Chemical group 0.000 claims 2
- 208000021302 gastroesophageal reflux disease Diseases 0.000 claims 2
- 231100000283 hepatitis Toxicity 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 208000019423 liver disease Diseases 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000003566 oxetanyl group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000004817 pentamethylene group Chemical group [H]C([H])([*:2])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[*:1] 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 2
- 125000004632 tetrahydrothiopyranyl group Chemical group S1C(CCCC1)* 0.000 claims 2
- 201000001862 viral hepatitis Diseases 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- GVNVAWHJIKLAGL-UHFFFAOYSA-N 2-(cyclohexen-1-yl)cyclohexan-1-one Chemical compound O=C1CCCCC1C1=CCCCC1 GVNVAWHJIKLAGL-UHFFFAOYSA-N 0.000 claims 1
- 206010004659 Biliary cirrhosis Diseases 0.000 claims 1
- GBGWXZSKWIMHFY-IYYHFTIWSA-N C(#N)C=1C=C(C=CC=1OC)[C@@H]1CC[C@H](CC1)CN(C(=O)[C@@H]1CC[C@H](CC1)O)C1=CC(=CC=C1)C=1C=NN(C=1)CC Chemical compound C(#N)C=1C=C(C=CC=1OC)[C@@H]1CC[C@H](CC1)CN(C(=O)[C@@H]1CC[C@H](CC1)O)C1=CC(=CC=C1)C=1C=NN(C=1)CC GBGWXZSKWIMHFY-IYYHFTIWSA-N 0.000 claims 1
- SVFJFOBEINLCKB-IYYHFTIWSA-N C1(CC1)N1N=CC(=C1)C=1C=C(C=CC=1)N(C(=O)[C@@H]1CC[C@H](CC1)O)C[C@@H]1CC[C@H](CC1)C=1C=NC(=CC=1)N(C)C Chemical compound C1(CC1)N1N=CC(=C1)C=1C=C(C=CC=1)N(C(=O)[C@@H]1CC[C@H](CC1)O)C[C@@H]1CC[C@H](CC1)C=1C=NC(=CC=1)N(C)C SVFJFOBEINLCKB-IYYHFTIWSA-N 0.000 claims 1
- 208000005623 Carcinogenesis Diseases 0.000 claims 1
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 1
- 206010008635 Cholestasis Diseases 0.000 claims 1
- 101150065749 Churc1 gene Proteins 0.000 claims 1
- 206010009657 Clostridium difficile colitis Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 206010010774 Constipation Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 208000004930 Fatty Liver Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 208000007882 Gastritis Diseases 0.000 claims 1
- 208000005577 Gastroenteritis Diseases 0.000 claims 1
- 206010019708 Hepatic steatosis Diseases 0.000 claims 1
- 206010019728 Hepatitis alcoholic Diseases 0.000 claims 1
- 102100038239 Protein Churchill Human genes 0.000 claims 1
- 208000003100 Pseudomembranous Enterocolitis Diseases 0.000 claims 1
- 206010037128 Pseudomembranous colitis Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 208000002353 alcoholic hepatitis Diseases 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000004069 aziridinyl group Chemical group 0.000 claims 1
- 210000000941 bile Anatomy 0.000 claims 1
- 230000036952 cancer formation Effects 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 231100000504 carcinogenesis Toxicity 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 230000007870 cholestasis Effects 0.000 claims 1
- 231100000359 cholestasis Toxicity 0.000 claims 1
- 230000007882 cirrhosis Effects 0.000 claims 1
- 230000001079 digestive effect Effects 0.000 claims 1
- 125000004852 dihydrofuranyl group Chemical group O1C(CC=C1)* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 201000006549 dyspepsia Diseases 0.000 claims 1
- 208000009866 extrahepatic cholestasis Diseases 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 1
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 230000000968 intestinal effect Effects 0.000 claims 1
- 208000001024 intrahepatic cholestasis Diseases 0.000 claims 1
- 230000007872 intrahepatic cholestasis Effects 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 208000018191 liver inflammation Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 208000037931 necrotizing enteritis Diseases 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 230000002980 postoperative effect Effects 0.000 claims 1
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 125000003944 tolyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 231100000397 ulcer Toxicity 0.000 claims 1
- 0 **=IC=C*N Chemical compound **=IC=C*N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762471517P | 2017-03-15 | 2017-03-15 | |
| US62/471,517 | 2017-03-15 | ||
| PCT/US2018/022489 WO2018170166A1 (en) | 2017-03-15 | 2018-03-14 | Farnesoid x receptor agonists and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020514333A JP2020514333A (ja) | 2020-05-21 |
| JP2020514333A5 true JP2020514333A5 (enExample) | 2021-04-15 |
| JP7174709B2 JP7174709B2 (ja) | 2022-11-17 |
Family
ID=63522667
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019547662A Active JP7174709B2 (ja) | 2017-03-15 | 2018-03-14 | ファルネソイドｘ受容体アゴニストおよびその使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US10961198B2 (enExample) |
| EP (1) | EP3596053B1 (enExample) |
| JP (1) | JP7174709B2 (enExample) |
| CN (1) | CN110637011B (enExample) |
| AR (1) | AR111284A1 (enExample) |
| CA (1) | CA3055990A1 (enExample) |
| DK (1) | DK3596053T3 (enExample) |
| IL (1) | IL269068B (enExample) |
| TW (1) | TWI803482B (enExample) |
| WO (1) | WO2018170166A1 (enExample) |
Families Citing this family (25)
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| EP3350166A4 (en) | 2015-09-16 | 2019-05-01 | Metacrine, Inc. | FARNESOID-X RECEPTOR AGONISTS AND USES THEREOF |
| US10626081B2 (en) | 2015-09-16 | 2020-04-21 | Metacrine, Inc. | Farnesoid X receptor agonists and uses thereof |
| EP3350165B1 (en) | 2015-09-16 | 2023-07-26 | Organovo, Inc. | Farnesoid x receptor agonists and uses thereof |
| AU2018236275B2 (en) | 2017-03-15 | 2022-05-12 | Eli Lilly And Company | Farnesoid X receptor agonists and uses thereof |
| DK3596053T3 (da) | 2017-03-15 | 2023-09-25 | Organovo Inc | Farnesoid-x-receptoragonister og anvendelser deraf |
| US11286252B2 (en) | 2017-11-01 | 2022-03-29 | Bristol-Myers Squibb Company | Alkene spirocyclic compounds as farnesoid X receptor modulators |
| KR102731925B1 (ko) | 2017-11-01 | 2024-11-18 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 멀티시클릭 화합물 |
| JP7478142B2 (ja) | 2018-06-07 | 2024-05-02 | ディスアーム セラピューティクス， インコーポレイテッド | Ｓａｒｍ１阻害剤 |
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| JP7465883B2 (ja) * | 2019-02-15 | 2024-04-11 | ブリストル－マイヤーズ スクイブ カンパニー | ファルネソイドｘ受容体モジュレータとしての置換二環式化合物 |
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| JP7664278B2 (ja) * | 2020-03-18 | 2025-04-17 | オルガノボ，インク． | ファルネソイドｘ受容体アゴニストの結晶質形態 |
| KR20220154801A (ko) * | 2020-03-18 | 2022-11-22 | 메타크린, 인크. | 질환의 치료를 위한 파르네소이드 x 수용체 작용제 |
| WO2021188690A1 (en) * | 2020-03-18 | 2021-09-23 | Metacrine, Inc. | Farnesoid x receptor agonists for the treatment of disease |
| CN120227340A (zh) * | 2020-03-18 | 2025-07-01 | 伊莱利利公司 | 法尼醇x受体激动剂的制剂 |
| MX2023008365A (es) | 2021-01-14 | 2023-10-04 | Enyo Pharma | Efecto sinérgico de un agonista de fxr e ifn para el tratamiento de infección por hbv. |
| TW202308629A (zh) | 2021-04-28 | 2023-03-01 | 法商Ｅｎｙｏ製藥公司 | 使用fxr激動劑作為組合治療以增強tlr3激動劑之療效 |
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| AU2016233579A1 (en) | 2015-03-13 | 2017-10-12 | Salk Institute For Biological Studies | Treating latent autoimmune diabetes of adults with farnesoid X receptor agonists to activate intestinal receptors |
| WO2017018751A1 (ko) | 2015-07-24 | 2017-02-02 | 동국대학교 산학협력단 | Blt 저해 활성을 갖는 신규 화합물 및 이를 유효성분으로 포함하는 염증성 질환 예방 또는 치료용 조성물 |
| EP3350166A4 (en) | 2015-09-16 | 2019-05-01 | Metacrine, Inc. | FARNESOID-X RECEPTOR AGONISTS AND USES THEREOF |
| EP3350165B1 (en) * | 2015-09-16 | 2023-07-26 | Organovo, Inc. | Farnesoid x receptor agonists and uses thereof |
| US10626081B2 (en) | 2015-09-16 | 2020-04-21 | Metacrine, Inc. | Farnesoid X receptor agonists and uses thereof |
| WO2017049176A1 (en) | 2015-09-16 | 2017-03-23 | Metacrine, Inc. | Farnesoid x receptor agonists and uses thereof |
| KR102316645B1 (ko) | 2016-03-31 | 2021-10-25 | 가부시키가이샤 아데카 | 감광성 조성물 및 신규 화합물 |
| WO2018170173A1 (en) | 2017-03-15 | 2018-09-20 | Metacrine, Inc. | Farnesoid x receptor agonists and uses thereof |
| AU2018236275B2 (en) | 2017-03-15 | 2022-05-12 | Eli Lilly And Company | Farnesoid X receptor agonists and uses thereof |
| DK3596053T3 (da) * | 2017-03-15 | 2023-09-25 | Organovo Inc | Farnesoid-x-receptoragonister og anvendelser deraf |
| WO2018170165A1 (en) | 2017-03-15 | 2018-09-20 | Metacrine, Inc. | Farnesoid x receptor agonists and uses thereof |
| US20200131132A1 (en) | 2017-03-15 | 2020-04-30 | Metacrine, Inc. | Farnesoid x receptor agonists and uses thereof |
| WO2020060007A1 (ko) * | 2018-09-17 | 2020-03-26 | 엘지전자 주식회사 | 5g 이동통신에서 pdu 세션을 핸들링하는 방법 및 무선 기기 |
| EP3852748B1 (en) | 2018-09-18 | 2025-09-03 | Eli Lilly and Company | Farnesoid x receptor agonists and uses thereof |
| CN113056264A (zh) | 2018-09-18 | 2021-06-29 | 梅塔科林公司 | 法尼醇x受体激动剂及其用途 |
| WO2020061117A1 (en) | 2018-09-18 | 2020-03-26 | Metacrine, Inc. | Farnesoid x receptor agonists and uses thereof |
| WO2020061116A1 (en) | 2018-09-18 | 2020-03-26 | Metacrine, Inc. | Farnesoid x receptor agonists and uses thereof |
| WO2020061118A1 (en) | 2018-09-18 | 2020-03-26 | Metacrine, Inc. | Farnesoid x receptor agonists and uses thereof |
-
2018
- 2018-03-14 DK DK18767094.8T patent/DK3596053T3/da active
- 2018-03-14 US US16/494,264 patent/US10961198B2/en active Active
- 2018-03-14 CA CA3055990A patent/CA3055990A1/en active Pending
- 2018-03-14 IL IL269068A patent/IL269068B/en unknown
- 2018-03-14 JP JP2019547662A patent/JP7174709B2/ja active Active
- 2018-03-14 WO PCT/US2018/022489 patent/WO2018170166A1/en not_active Ceased
- 2018-03-14 EP EP18767094.8A patent/EP3596053B1/en active Active
- 2018-03-14 CN CN201880032220.9A patent/CN110637011B/zh active Active
- 2018-03-15 AR ARP180100608A patent/AR111284A1/es not_active Application Discontinuation
- 2018-03-15 TW TW107108918A patent/TWI803482B/zh active
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2020
- 2020-05-28 US US16/886,642 patent/US10927082B2/en active Active
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2021
- 2021-01-19 US US17/152,548 patent/US20210300875A1/en not_active Abandoned
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