JP2017511357A5 - - Google Patents
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- Publication number
- JP2017511357A5 JP2017511357A5 JP2016562565A JP2016562565A JP2017511357A5 JP 2017511357 A5 JP2017511357 A5 JP 2017511357A5 JP 2016562565 A JP2016562565 A JP 2016562565A JP 2016562565 A JP2016562565 A JP 2016562565A JP 2017511357 A5 JP2017511357 A5 JP 2017511357A5
- Authority
- JP
- Japan
- Prior art keywords
- cycloalkyl
- alkyl
- optionally substituted
- compound
- halo
- 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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- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 32
- 125000000217 alkyl group Chemical group 0.000 claims 31
- 150000001875 compounds Chemical class 0.000 claims 29
- 125000001475 halogen functional group Chemical group 0.000 claims 21
- 150000003839 salts Chemical class 0.000 claims 18
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 5
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 2
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 2
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims 1
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims 1
- 206010003267 Arthritis reactive Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010012434 Dermatitis allergic Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 208000034189 Sclerosis Diseases 0.000 claims 1
- 208000006045 Spondylarthropathies Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 208000019069 chronic childhood arthritis Diseases 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 208000002574 reactive arthritis Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000005671 spondyloarthropathy Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- OOKODUAJINEEGT-UHFFFAOYSA-N CC(C1CC1)N(c(nc(-c1c(C2CC2)ncnc1OC)nc1)c1N=C1NCc(nc2)ccc2S(NC)(=O)=O)C1=O Chemical compound CC(C1CC1)N(c(nc(-c1c(C2CC2)ncnc1OC)nc1)c1N=C1NCc(nc2)ccc2S(NC)(=O)=O)C1=O OOKODUAJINEEGT-UHFFFAOYSA-N 0.000 description 1
- WUSKTXFSBDEUDC-CQSZACIVSA-N CC[C@@H](C)N(c(nc(-c1c(C2CC2)ncnc1OC)nc1)c1N=C1NCc(cc2)ccc2S(N)(=O)=O)C1=O Chemical compound CC[C@@H](C)N(c(nc(-c1c(C2CC2)ncnc1OC)nc1)c1N=C1NCc(cc2)ccc2S(N)(=O)=O)C1=O WUSKTXFSBDEUDC-CQSZACIVSA-N 0.000 description 1
- FSTZQZLACCJSSK-INIZCTEOSA-N CCc1ncnc(C2CC2)c1-c(nc1)nc(N([C@@H](C)C2CC2)C2=O)c1N=C2NCc(cc1)ncc1S(CC)(=O)=O Chemical compound CCc1ncnc(C2CC2)c1-c(nc1)nc(N([C@@H](C)C2CC2)C2=O)c1N=C2NCc(cc1)ncc1S(CC)(=O)=O FSTZQZLACCJSSK-INIZCTEOSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461979231P | 2014-04-14 | 2014-04-14 | |
| US61/979,231 | 2014-04-14 | ||
| PCT/US2015/025328 WO2015160654A1 (en) | 2014-04-14 | 2015-04-10 | Compounds as modulators of ror gamma |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018009384A Division JP6463855B2 (ja) | 2014-04-14 | 2018-01-24 | Ｒｏｒガンマのモジュレーターとしての化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017511357A JP2017511357A (ja) | 2017-04-20 |
| JP2017511357A5 true JP2017511357A5 (enExample) | 2017-08-31 |
| JP6282759B2 JP6282759B2 (ja) | 2018-02-21 |
Family
ID=52998264
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016562565A Active JP6282759B2 (ja) | 2014-04-14 | 2015-04-10 | Ｒｏｒガンマのモジュレーターとしての化合物 |
| JP2018009384A Active JP6463855B2 (ja) | 2014-04-14 | 2018-01-24 | Ｒｏｒガンマのモジュレーターとしての化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018009384A Active JP6463855B2 (ja) | 2014-04-14 | 2018-01-24 | Ｒｏｒガンマのモジュレーターとしての化合物 |
Country Status (35)
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015160654A1 (en) | 2014-04-14 | 2015-10-22 | Boehringer Ingelheim International Gmbh | Compounds as modulators of ror gamma |
| FR3030518B1 (fr) * | 2014-12-19 | 2018-03-23 | Galderma Research & Development | Derives sulfonamides en tant qu'agonistes inverses du recepteur gamma orphelin associe aux retinoides ror gamma (t) |
| MX394388B (es) | 2015-05-15 | 2025-03-21 | Aurigene Discovery Tech Ltd | Compuestos de tetrahidroquinolinona sustituidos como moduladores de ror gamma |
| JP6778259B2 (ja) | 2015-10-01 | 2020-10-28 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｒｏｒガンマのモジュレーターとしてのプテリジン誘導体 |
| CN109071516B (zh) | 2015-12-15 | 2021-08-31 | 阿斯利康(瑞典)有限公司 | 新颖的化合物 |
| EP3405470B1 (en) * | 2016-01-20 | 2020-07-15 | Boehringer Ingelheim International GmbH | Pyrazinedihydropyrimidinone or pyridazinedihydropyrimidinone compounds as modulators of ror gamma |
| AR110481A1 (es) | 2016-12-05 | 2019-04-03 | Lead Pharma Holding Bv | MODULADORES DE ROR g (RORg) |
| US20200031753A1 (en) | 2017-04-06 | 2020-01-30 | Boehringer Ingelheim International Gmbh | Cyclopropyl alkyl amines and process for their preparation |
| WO2018229155A1 (en) | 2017-06-14 | 2018-12-20 | Astrazeneca Ab | 2,3-dihydroisoindole-1-carboxamides useful as ror-gamma modulators |
| CN109206346A (zh) * | 2017-07-01 | 2019-01-15 | 复旦大学 | 叔胺类衍生物或其盐及其制备方法和用途 |
| CN107903263B (zh) * | 2017-12-28 | 2019-11-12 | 山东铂源药业有限公司 | 一种帕布昔利布中间体的合成方法 |
| AU2019262169B2 (en) | 2018-05-03 | 2024-05-02 | Jiangsu Hengrui Medicine Co., Ltd. | Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (RORy) and pharmaceutical uses thereof |
| US20210395185A1 (en) | 2018-10-18 | 2021-12-23 | Boehringer Ingelheim International Gmbh | Scalable synthesis of optically active 1-cyclopropylalkyl-1-amines |
| US20230014730A1 (en) | 2019-09-23 | 2023-01-19 | Nanjing Zhengxiang Pharmaceuticals Co., Ltd. | Phosphodiesterase inhibitors and use |
| US20220411380A1 (en) | 2019-10-31 | 2022-12-29 | Jiangsu Hengrui Medicine Co., Ltd. | ACID ADDITION SALT OF RORy REGULATOR |
| WO2022106548A1 (en) | 2020-11-19 | 2022-05-27 | Boehringer Ingelheim International Gmbh | Solid forms of a ror gamma inhibitor |
| WO2022106549A1 (en) | 2020-11-19 | 2022-05-27 | Boehringer Ingelheim International Gmbh | Crystalline salts of a ror gamma inhibitor |
| WO2022106550A1 (en) | 2020-11-19 | 2022-05-27 | Boehringer Ingelheim International Gmbh | Crystalline polymorphic form of a ror gamma inhibitor |
| WO2022106551A1 (en) | 2020-11-19 | 2022-05-27 | Boehringer Ingelheim International Gmbh | Co-crystals of a ror gamma inhibitor |
| WO2022106547A1 (en) | 2020-11-19 | 2022-05-27 | Boehringer Ingelheim International Gmbh | Process for synthesising a ror gamma inhibitor |
| WO2023216910A1 (zh) * | 2022-05-07 | 2023-11-16 | 苏州浦合医药科技有限公司 | 取代的双环杂芳基化合物作为usp1抑制剂 |
| WO2023232870A1 (en) | 2022-05-31 | 2023-12-07 | Immunic Ag | Rorg/rorgt modulators for the treatment of virus infections like covid-19 |
| CN116178279A (zh) * | 2023-03-15 | 2023-05-30 | 上海药坦药物研究开发有限公司 | 一种5-溴-4-环丙基-6-甲氧基嘧啶及其中间体的制备方法 |
| AU2024267864A1 (en) * | 2023-05-09 | 2025-11-06 | 11949098 Canada Inc. | Inverse agonists of rar related orphan receptors (rors) |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE0102716D0 (sv) * | 2001-08-14 | 2001-08-14 | Astrazeneca Ab | Novel compounds |
| WO2009022185A2 (en) * | 2007-08-16 | 2009-02-19 | Astrazeneca Ab | 6, 6-fused heterocycles, their pharmaceutical compositions and methos of use |
| CA2737472A1 (en) | 2008-09-26 | 2010-04-01 | Boehringer Ingelheim International Gmbh | Azaindazole compounds as ccr1 receptor antagonists |
| WO2011049917A1 (en) | 2009-10-21 | 2011-04-28 | Boehringer Ingelheim International Gmbh | Indazole and pyrazolopyridine compounds as ccr1 receptor antagonists |
| CN103717070A (zh) * | 2011-06-01 | 2014-04-09 | 贾纳斯生物治疗有限公司 | 新型免疫系统调节剂 |
| DE112013002484B4 (de) * | 2012-05-14 | 2023-05-04 | Shanghai Yidian Pharmaceutical Technology Development Co., Ltd. | Pteridinketon-Derivat und Anwendungen desselben als EGFR-, BLK- und FLT3-Inhibitor |
| WO2015160654A1 (en) * | 2014-04-14 | 2015-10-22 | Boehringer Ingelheim International Gmbh | Compounds as modulators of ror gamma |
| JP6778259B2 (ja) * | 2015-10-01 | 2020-10-28 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｒｏｒガンマのモジュレーターとしてのプテリジン誘導体 |
| EP3405470B1 (en) * | 2016-01-20 | 2020-07-15 | Boehringer Ingelheim International GmbH | Pyrazinedihydropyrimidinone or pyridazinedihydropyrimidinone compounds as modulators of ror gamma |
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2015
- 2015-04-10 WO PCT/US2015/025328 patent/WO2015160654A1/en not_active Ceased
- 2015-04-10 BR BR112016021962A patent/BR112016021962A2/pt not_active IP Right Cessation
- 2015-04-10 KR KR1020167031654A patent/KR102410069B1/ko active Active
- 2015-04-10 NZ NZ723530A patent/NZ723530A/en unknown
- 2015-04-10 UA UAA201803569A patent/UA121255C2/uk unknown
- 2015-04-10 DK DK15718330.2T patent/DK3131902T3/da active
- 2015-04-10 MX MX2016013342A patent/MX370780B/es active IP Right Grant
- 2015-04-10 PT PT15718330T patent/PT3131902T/pt unknown
- 2015-04-10 KR KR1020207010364A patent/KR102410076B1/ko active Active
- 2015-04-10 CA CA2944787A patent/CA2944787C/en active Active
- 2015-04-10 BR BR122020020657-8A patent/BR122020020657B1/pt active IP Right Grant
- 2015-04-10 UA UAA201610804A patent/UA120094C2/uk unknown
- 2015-04-10 EP EP18177902.6A patent/EP3418280B1/en active Active
- 2015-04-10 RS RSP20191083 patent/RS59170B1/sr unknown
- 2015-04-10 HR HRP20191579 patent/HRP20191579T1/hr unknown
- 2015-04-10 CN CN201580016630.0A patent/CN106132965B/zh active Active
- 2015-04-10 PE PE2016001963A patent/PE20161572A1/es unknown
- 2015-04-10 MA MA046373A patent/MA46373A/fr unknown
- 2015-04-10 EA EA201890329A patent/EA035063B1/ru not_active IP Right Cessation
- 2015-04-10 PE PE2020001484A patent/PE20211002A1/es unknown
- 2015-04-10 SG SG11201608537SA patent/SG11201608537SA/en unknown
- 2015-04-10 EP EP15718330.2A patent/EP3131902B1/en active Active
- 2015-04-10 ME MEP-2019-233A patent/ME03513B/me unknown
- 2015-04-10 EA EA201691978A patent/EA031351B1/ru not_active IP Right Cessation
- 2015-04-10 US US14/683,682 patent/US9242989B2/en active Active
- 2015-04-10 PL PL15718330T patent/PL3131902T3/pl unknown
- 2015-04-10 AP AP2016009403A patent/AP2016009403A0/en unknown
- 2015-04-10 CN CN201710445827.7A patent/CN107266450B/zh active Active
- 2015-04-10 CN CN201710445005.9A patent/CN107266454B/zh active Active
- 2015-04-10 AU AU2015247983A patent/AU2015247983B2/en not_active Ceased
- 2015-04-10 HU HUE15718330A patent/HUE045847T2/hu unknown
- 2015-04-10 JP JP2016562565A patent/JP6282759B2/ja active Active
- 2015-04-10 MY MYPI2016001598A patent/MY182834A/en unknown
- 2015-04-10 SI SI201530865T patent/SI3131902T1/sl unknown
- 2015-04-10 LT LTEP15718330.2T patent/LT3131902T/lt unknown
- 2015-04-10 ES ES15718330T patent/ES2744299T3/es active Active
- 2015-04-13 TW TW104111832A patent/TWI655192B/zh not_active IP Right Cessation
- 2015-04-13 UY UY0001036077A patent/UY36077A/es not_active Application Discontinuation
- 2015-04-13 AR ARP150101103A patent/AR100058A1/es not_active Application Discontinuation
- 2015-04-13 TW TW107130729A patent/TWI652268B/zh not_active IP Right Cessation
- 2015-11-20 US US14/946,873 patent/US20160075706A1/en not_active Abandoned
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2016
- 2016-08-22 IL IL247419A patent/IL247419B/en active IP Right Grant
- 2016-09-20 US US15/270,029 patent/US9598415B2/en active Active
- 2016-09-27 CL CL2016002421A patent/CL2016002421A1/es unknown
- 2016-10-11 PH PH12016502019A patent/PH12016502019B1/en unknown
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2017
- 2017-02-07 US US15/426,208 patent/US20180022749A1/en not_active Abandoned
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2018
- 2018-01-24 JP JP2018009384A patent/JP6463855B2/ja active Active
- 2018-09-06 US US16/123,139 patent/US20190002465A1/en not_active Abandoned
- 2018-12-20 IL IL26387818A patent/IL263878B/en active IP Right Grant
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2019
- 2019-04-30 AU AU2019203027A patent/AU2019203027B2/en not_active Ceased
- 2019-09-09 CY CY20191100942T patent/CY1122012T1/el unknown
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2020
- 2020-02-04 PH PH12020500252A patent/PH12020500252A1/en unknown
- 2020-07-21 AR ARP200102050A patent/AR119454A2/es unknown