JPWO2019213470A5 - - Google Patents
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- Publication number
- JPWO2019213470A5 JPWO2019213470A5 JP2020560186A JP2020560186A JPWO2019213470A5 JP WO2019213470 A5 JPWO2019213470 A5 JP WO2019213470A5 JP 2020560186 A JP2020560186 A JP 2020560186A JP 2020560186 A JP2020560186 A JP 2020560186A JP WO2019213470 A5 JPWO2019213470 A5 JP WO2019213470A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cycloalkyl
- group
- aryl
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 77
- 125000000753 cycloalkyl group Chemical group 0.000 claims 74
- 125000003118 aryl group Chemical group 0.000 claims 67
- 125000001072 heteroaryl group Chemical group 0.000 claims 65
- 125000000623 heterocyclic group Chemical group 0.000 claims 62
- 125000003545 alkoxy group Chemical group 0.000 claims 60
- -1 cyano, amino, hydroxy Chemical group 0.000 claims 54
- 125000003342 alkenyl group Chemical group 0.000 claims 53
- 229910052736 halogen Inorganic materials 0.000 claims 39
- 150000002367 halogens Chemical class 0.000 claims 39
- 229910052739 hydrogen Inorganic materials 0.000 claims 34
- 239000001257 hydrogen Substances 0.000 claims 34
- 150000002431 hydrogen Chemical class 0.000 claims 31
- 125000001188 haloalkyl group Chemical group 0.000 claims 28
- 150000001875 compounds Chemical class 0.000 claims 21
- 125000000304 alkynyl group Chemical group 0.000 claims 20
- 239000000203 mixture Substances 0.000 claims 18
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 14
- 239000000651 prodrug Substances 0.000 claims 14
- 229940002612 prodrug Drugs 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 14
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 239000012453 solvate Substances 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 5
- 206010061218 Inflammation Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 125000004438 haloalkoxy group Chemical group 0.000 claims 4
- 230000004054 inflammatory process Effects 0.000 claims 4
- 125000006193 alkinyl group Chemical group 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 208000011580 syndromic disease Diseases 0.000 claims 3
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 2
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 2
- 108091008773 RAR-related orphan receptors γ Proteins 0.000 claims 2
- 201000002661 Spondylitis Diseases 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 206010003246 arthritis Diseases 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 230000001363 autoimmune Effects 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 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
- 239000002904 solvent Substances 0.000 claims 2
- 230000001256 tonic effect Effects 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 208000002874 Acne Vulgaris Diseases 0.000 claims 1
- 208000031212 Autoimmune polyendocrinopathy Diseases 0.000 claims 1
- BTBUEUYNUDRHOZ-UHFFFAOYSA-N Borate Chemical compound [O-]B([O-])[O-] BTBUEUYNUDRHOZ-UHFFFAOYSA-N 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 206010012442 Dermatitis contact Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013774 Dry eye Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 208000001204 Hashimoto Disease Diseases 0.000 claims 1
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000011200 Kawasaki disease Diseases 0.000 claims 1
- 208000019693 Lung disease Diseases 0.000 claims 1
- 208000009525 Myocarditis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 208000034189 Sclerosis Diseases 0.000 claims 1
- 206010000496 acne Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 201000011385 autoimmune polyendocrine syndrome Diseases 0.000 claims 1
- 208000010928 autoimmune thyroid disease Diseases 0.000 claims 1
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003054 catalyst Substances 0.000 claims 1
- 208000019069 chronic childhood arthritis Diseases 0.000 claims 1
- 208000010247 contact dermatitis Diseases 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 208000001725 mucocutaneous lymph node syndrome Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 208000005987 polymyositis Diseases 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 206010043778 thyroiditis Diseases 0.000 claims 1
- 238000002054 transplantation Methods 0.000 claims 1
- 230000009278 visceral effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862666312P | 2018-05-03 | 2018-05-03 | |
| US62/666,312 | 2018-05-03 | ||
| PCT/US2019/030526 WO2019213470A1 (en) | 2018-05-03 | 2019-05-03 | Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (rorϒ) and pharmaceutical uses thereof |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021522262A JP2021522262A (ja) | 2021-08-30 |
| JP2021522262A5 JP2021522262A5 (https=) | 2022-05-12 |
| JPWO2019213470A5 true JPWO2019213470A5 (https=) | 2022-05-12 |
| JP7351851B2 JP7351851B2 (ja) | 2023-09-27 |
Family
ID=68386171
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020560186A Active JP7351851B2 (ja) | 2018-05-03 | 2019-05-03 | レチノイド関連オルファン受容体ガンマ（ＲＯＲγ）のモジュレーターとしてのベンジイミダゾール誘導体およびそれらの医薬品用途 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US11512055B2 (https=) |
| EP (1) | EP3781161B1 (https=) |
| JP (1) | JP7351851B2 (https=) |
| KR (1) | KR102709804B1 (https=) |
| CN (2) | CN116514722A (https=) |
| AU (1) | AU2019262169B2 (https=) |
| BR (1) | BR112020021967A2 (https=) |
| CA (1) | CA3097519A1 (https=) |
| ES (1) | ES2949366T3 (https=) |
| HR (1) | HRP20230643T1 (https=) |
| HU (1) | HUE062273T2 (https=) |
| MX (1) | MX2020011405A (https=) |
| MY (1) | MY208400A (https=) |
| PL (1) | PL3781161T3 (https=) |
| RS (1) | RS64348B1 (https=) |
| SM (1) | SMT202300212T1 (https=) |
| TW (1) | TWI818985B (https=) |
| UA (1) | UA128161C2 (https=) |
| WO (1) | WO2019213470A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY208400A (en) * | 2018-05-03 | 2025-05-07 | Shanghai hengrui pharmaceutical co ltd | Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (ror) and pharmaceutical uses thereof |
| US20220411380A1 (en) * | 2019-10-31 | 2022-12-29 | Jiangsu Hengrui Medicine Co., Ltd. | ACID ADDITION SALT OF RORy REGULATOR |
| CN112745268B (zh) * | 2019-10-31 | 2022-09-16 | 江苏恒瑞医药股份有限公司 | 苯并咪唑衍生物的晶型及制备方法 |
| TW202136238A (zh) * | 2020-01-06 | 2021-10-01 | 大陸商廣東東陽光藥業有限公司 | RORγt抑制劑及其製備方法和用途 |
| TW202136237A (zh) * | 2020-01-06 | 2021-10-01 | 大陸商廣東東陽光藥業有限公司 | RORγt抑制劑及其製備方法和用途 |
| CN111269126B (zh) * | 2020-03-12 | 2023-04-07 | 北京理工大学重庆创新中心 | 一种熔铸载体1,2-二氟-4,5-二硝基苯的制备方法 |
| CA3179686A1 (en) * | 2020-04-07 | 2021-10-14 | UCB Biopharma SRL | Difluorocyclohexyl derivatives as il-17 modulators |
| TW202146381A (zh) * | 2020-05-15 | 2021-12-16 | 大陸商上海輝启生物醫藥科技有限公司 | 可用作RORγ調節劑的聯芳基類化合物 |
| WO2022245067A1 (ko) * | 2021-05-17 | 2022-11-24 | 서울대학교 산학협력단 | RORα의 활성자 JC1-40을 포함하는 근감소증 예방, 개선, 또는 치료를 위한 약학적 조성물 |
| CN121045325A (zh) * | 2024-05-31 | 2025-12-02 | 中国科学院广州生物医药与健康研究院 | 磺酰胺基乙酰胺类化合物及其制备方法和应用 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3075991A (en) * | 1960-01-20 | 1963-01-29 | Dow Chemical Co | Benzimidazolylalkylbenzene-sulfonamide compounds |
| DE60023920T2 (de) * | 1999-08-27 | 2006-07-20 | Sugen, Inc., South San Francisco | Phosphatmimetika und Verfahren zur Behandlung mit Phosphataseinhibitoren HIBITOREN |
| US7951829B2 (en) | 2006-05-03 | 2011-05-31 | Janssen Pharmaceutica Nv | Benzimidazole modulators of VR1 |
| CN102906074A (zh) * | 2010-05-24 | 2013-01-30 | 东亚荣养株式会社 | 稠合咪唑衍生物 |
| WO2012027965A1 (en) | 2010-09-01 | 2012-03-08 | Glaxo Group Limited | Novel compounds |
| CN102060780B (zh) | 2010-12-27 | 2014-11-05 | 雅本化学股份有限公司 | 2-(n-取代)-氨基苯并咪唑衍生物的制备方法 |
| WO2013029338A1 (en) | 2011-09-01 | 2013-03-07 | Glaxo Group Limited | Novel compounds |
| US9550737B2 (en) * | 2012-06-11 | 2017-01-24 | Ucb Biopharma Sprl | TNF -α modulating benzimidazoles |
| EP3089963A1 (en) | 2013-10-30 | 2016-11-09 | Novartis AG | 2-benzyl-benzimidazole complement factor b inhibitors and uses thereof |
| KR102410076B1 (ko) | 2014-04-14 | 2022-06-22 | 베링거 인겔하임 인터내셔날 게엠베하 | Ror 감마의 조절제로서의 화합물 |
| US9718817B2 (en) | 2014-04-16 | 2017-08-01 | Glenmark Pharmaceuticals S.A. | Aryl and heteroaryl ether compounds as ROR gamma modulators |
| WO2015196335A1 (en) * | 2014-06-23 | 2015-12-30 | Tocopherx, Inc. | Pyrazole compounds as modulators of fshr and uses thereof |
| US20160024052A1 (en) * | 2014-07-25 | 2016-01-28 | Innov17 Llc | Benzimidazole retinoic acid receptor-related orphan receptor modulators and uses thereof |
| FR3030516B1 (fr) * | 2014-12-19 | 2019-12-27 | Galderma Research & Development | Derives sulfonamides bicycles en tant qu'agonistes inverses du recepteur gamma orphelin associe aux retinoides ror gamma (t) |
| TW202220968A (zh) * | 2016-01-29 | 2022-06-01 | 美商維它藥物有限責任公司 | ＲＯＲ－γ調節劑 |
| MY208400A (en) * | 2018-05-03 | 2025-05-07 | Shanghai hengrui pharmaceutical co ltd | Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (ror) and pharmaceutical uses thereof |
-
2019
- 2019-05-03 MY MYPI2020005364A patent/MY208400A/en unknown
- 2019-05-03 ES ES19796430T patent/ES2949366T3/es active Active
- 2019-05-03 UA UAA202007544A patent/UA128161C2/uk unknown
- 2019-05-03 EP EP19796430.7A patent/EP3781161B1/en active Active
- 2019-05-03 SM SM20230212T patent/SMT202300212T1/it unknown
- 2019-05-03 CN CN202310017171.4A patent/CN116514722A/zh active Pending
- 2019-05-03 BR BR112020021967-3A patent/BR112020021967A2/pt unknown
- 2019-05-03 CN CN201980027956.1A patent/CN112135611B/zh active Active
- 2019-05-03 AU AU2019262169A patent/AU2019262169B2/en active Active
- 2019-05-03 CA CA3097519A patent/CA3097519A1/en active Pending
- 2019-05-03 HR HRP20230643TT patent/HRP20230643T1/hr unknown
- 2019-05-03 RS RS20230505A patent/RS64348B1/sr unknown
- 2019-05-03 WO PCT/US2019/030526 patent/WO2019213470A1/en not_active Ceased
- 2019-05-03 HU HUE19796430A patent/HUE062273T2/hu unknown
- 2019-05-03 JP JP2020560186A patent/JP7351851B2/ja active Active
- 2019-05-03 MX MX2020011405A patent/MX2020011405A/es unknown
- 2019-05-03 KR KR1020207032236A patent/KR102709804B1/ko active Active
- 2019-05-03 TW TW108115438A patent/TWI818985B/zh active
- 2019-05-03 US US17/052,451 patent/US11512055B2/en active Active
- 2019-05-03 PL PL19796430.7T patent/PL3781161T3/pl unknown
-
2022
- 2022-11-21 US US18/057,537 patent/US12187684B2/en active Active
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