JPWO2020168143A5 - - Google Patents
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- Publication number
- JPWO2020168143A5 JPWO2020168143A5 JP2021547528A JP2021547528A JPWO2020168143A5 JP WO2020168143 A5 JPWO2020168143 A5 JP WO2020168143A5 JP 2021547528 A JP2021547528 A JP 2021547528A JP 2021547528 A JP2021547528 A JP 2021547528A JP WO2020168143 A5 JPWO2020168143 A5 JP WO2020168143A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- alkoxy
- cycloalkyl
- independently
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 93
- -1 cyano, hydroxyl Chemical group 0.000 claims 73
- 125000003545 alkoxy group Chemical group 0.000 claims 44
- 125000000623 heterocyclic group Chemical group 0.000 claims 34
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 30
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 27
- 229910052739 hydrogen Inorganic materials 0.000 claims 19
- 239000001257 hydrogen Substances 0.000 claims 18
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 17
- 125000004043 oxo group Chemical group O=* 0.000 claims 16
- 150000001875 compounds Chemical class 0.000 claims 13
- 150000002431 hydrogen Chemical class 0.000 claims 13
- 239000012453 solvate Substances 0.000 claims 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims 12
- 125000005843 halogen group Chemical group 0.000 claims 11
- 125000004076 pyridyl group Chemical group 0.000 claims 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000004452 carbocyclyl group Chemical group 0.000 claims 8
- 125000004122 cyclic group Chemical group 0.000 claims 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 7
- 125000004438 haloalkoxy group Chemical group 0.000 claims 6
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 claims 5
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 5
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 5
- 206010016654 Fibrosis Diseases 0.000 claims 4
- 230000004761 fibrosis Effects 0.000 claims 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 4
- 125000002971 oxazolyl group Chemical group 0.000 claims 4
- 125000003566 oxetanyl group Chemical group 0.000 claims 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 125000000335 thiazolyl group Chemical group 0.000 claims 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 125000002393 azetidinyl group Chemical group 0.000 claims 3
- 150000001602 bicycloalkyls Chemical group 0.000 claims 3
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000006431 methyl cyclopropyl group Chemical group 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 2
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims 2
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 2
- 125000005873 benzo[d]thiazolyl group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000006419 fluorocyclopropyl group Chemical group 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 230000001575 pathological effect Effects 0.000 claims 2
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 1
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 210000000013 bile duct Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 230000001587 cholestatic effect Effects 0.000 claims 1
- 208000020832 chronic kidney disease Diseases 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 125000005043 dihydropyranyl group Chemical group O1C(CCC=C1)* 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 1
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962806066P | 2019-02-15 | 2019-02-15 | |
| US62/806,066 | 2019-02-15 | ||
| PCT/US2020/018203 WO2020168143A1 (en) | 2019-02-15 | 2020-02-14 | Substituted bicyclic compounds as farnesoid x receptor modulators |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022519770A JP2022519770A (ja) | 2022-03-24 |
| JP2022519770A5 JP2022519770A5 (https=) | 2022-12-22 |
| JPWO2020168143A5 true JPWO2020168143A5 (https=) | 2022-12-22 |
| JP7476216B2 JP7476216B2 (ja) | 2024-04-30 |
Family
ID=69811921
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021547528A Active JP7476216B2 (ja) | 2019-02-15 | 2020-02-14 | 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 |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US11254663B2 (https=) |
| EP (1) | EP3924336A1 (https=) |
| JP (1) | JP7476216B2 (https=) |
| KR (1) | KR102927636B1 (https=) |
| CN (1) | CN113710656B (https=) |
| AR (1) | AR118050A1 (https=) |
| AU (1) | AU2020223316A1 (https=) |
| BR (1) | BR112021015689A2 (https=) |
| CA (1) | CA3129492A1 (https=) |
| CL (1) | CL2021002093A1 (https=) |
| CO (1) | CO2021010611A2 (https=) |
| EA (1) | EA202192276A1 (https=) |
| IL (1) | IL285246B2 (https=) |
| MX (1) | MX2021009694A (https=) |
| PE (1) | PE20211701A1 (https=) |
| SG (1) | SG11202108792WA (https=) |
| TW (1) | TWI808305B (https=) |
| WO (1) | WO2020168143A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| IL293892A (en) | 2020-01-15 | 2022-08-01 | Inserm Institut National De La Sant? Et De La Rech M?Dicale | Use of fxr agonists for treating an infection by hepatitis d virus |
| WO2022152773A1 (en) | 2021-01-14 | 2022-07-21 | Enyo Pharma | Method for treating chronic kidney diseases |
| JP2024502673A (ja) | 2021-01-14 | 2024-01-22 | ウエヌイグレックオ・ファーマ | Hbv感染の処置のためのfxrアゴニストとifnの相乗効果 |
| JP2024517181A (ja) | 2021-04-28 | 2024-04-19 | ウエヌイグレックオ・ファーマ | 組合せ治療としてfxrアゴニストを使用するtlr3アゴニストの効果の強い増強 |
| AU2023261809A1 (en) * | 2022-04-29 | 2024-12-05 | Asieris Pharmaceuticals (Shanghai) Co., Ltd. | Pyrimidine compound, method for preparing same, and pharmaceutical use thereof |
| CN115057996B (zh) * | 2022-06-24 | 2023-06-02 | 河南工程学院 | 4CzIPN型多孔有机聚合物的制备方法及其应用 |
| WO2025012422A1 (en) * | 2023-07-13 | 2025-01-16 | Enyo Pharma | L-arginine salt of 4-chloro-5-[4-(2,6-dichlorophenyl)sulfonylpiperazin-1-yl]-1-benzofuran-2-carboxylic acid and various forms thereof |
| AU2024295030A1 (en) * | 2023-07-13 | 2026-01-15 | Enyo Pharma | L-lysine salt of 4-chloro-5-[4-(2,6-dichlorophenyl)sulfonylpiperazin-1-yl]-1-benzofuran-2-carboxylic acid and various forms thereof |
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| WO1993013101A1 (fr) | 1991-12-27 | 1993-07-08 | Yoshitomi Pharmaceutical Industries, Ltd. | Compose de pyridonecarboxylate, son utilisation pharmaceutique et compose spiro |
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| US7319104B2 (en) | 2002-03-01 | 2008-01-15 | Smithkline Beecham Corporation | hPPARs activators |
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| WO2004046162A2 (en) | 2002-11-14 | 2004-06-03 | The Scripps Research Institute | Non-steroidal fxr agonists |
| WO2006006490A1 (ja) | 2004-07-08 | 2006-01-19 | Ono Pharmaceutical Co., Ltd. | スピロ化合物 |
| PL2402002T3 (pl) | 2005-04-08 | 2018-11-30 | Ptc Therapeutics, Inc. | Kompozycje zawierające kwas 1,2,4-oksadiazolobenzoesowy i ich zastosowania do leczenia chorób związanych z przedwczesnym kodonem stop |
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| CL2007003035A1 (es) | 2006-10-24 | 2008-05-16 | Smithkline Beechman Corp | Compuestos derivados de isoxazol sustituidos, agonistas de receptores farnesoid x; procedimiento de preparacion; composicion farmaceutica que lo comprende; y uso del compuesto en el tratamiento de la obesidad, diabetes mellitus, fibrosis en organos, |
| EP2108017A2 (en) | 2007-01-30 | 2009-10-14 | Biogen Idec MA, Inc. | Imidazolone compounds as tgf-beta family type i receptors, alk5 and/or alk4 antagonists |
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| EP3917516A4 (en) * | 2019-01-28 | 2022-10-12 | Flatley Discovery Lab, LLC | COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS |
| CN113727973B (zh) * | 2019-02-15 | 2025-08-29 | 百时美施贵宝公司 | 可用作类法尼醇x受体调节剂的取代酰胺化合物 |
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| KR102932313B1 (ko) | 2019-02-15 | 2026-02-26 | 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 | Nrf2 활성화제로서 히드록시피리드옥사제핀 |
-
2020
- 2020-02-11 AR ARP200100360A patent/AR118050A1/es not_active Application Discontinuation
- 2020-02-13 US US16/789,551 patent/US11254663B2/en active Active
- 2020-02-14 PE PE2021001326A patent/PE20211701A1/es unknown
- 2020-02-14 KR KR1020217029597A patent/KR102927636B1/ko active Active
- 2020-02-14 BR BR112021015689-5A patent/BR112021015689A2/pt unknown
- 2020-02-14 CA CA3129492A patent/CA3129492A1/en active Pending
- 2020-02-14 JP JP2021547528A patent/JP7476216B2/ja active Active
- 2020-02-14 TW TW109104696A patent/TWI808305B/zh not_active IP Right Cessation
- 2020-02-14 IL IL285246A patent/IL285246B2/en unknown
- 2020-02-14 AU AU2020223316A patent/AU2020223316A1/en not_active Abandoned
- 2020-02-14 MX MX2021009694A patent/MX2021009694A/es unknown
- 2020-02-14 CN CN202080029369.9A patent/CN113710656B/zh active Active
- 2020-02-14 WO PCT/US2020/018203 patent/WO2020168143A1/en not_active Ceased
- 2020-02-14 EA EA202192276A patent/EA202192276A1/ru unknown
- 2020-02-14 SG SG11202108792WA patent/SG11202108792WA/en unknown
- 2020-02-14 EP EP20711418.2A patent/EP3924336A1/en active Pending
-
2021
- 2021-08-10 CL CL2021002093A patent/CL2021002093A1/es unknown
- 2021-08-12 CO CONC2021/0010611A patent/CO2021010611A2/es unknown
- 2021-12-07 US US17/544,490 patent/US11713312B2/en active Active
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