JP2020530848A5 - - Google Patents
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- Publication number
- JP2020530848A5 JP2020530848A5 JP2020508398A JP2020508398A JP2020530848A5 JP 2020530848 A5 JP2020530848 A5 JP 2020530848A5 JP 2020508398 A JP2020508398 A JP 2020508398A JP 2020508398 A JP2020508398 A JP 2020508398A JP 2020530848 A5 JP2020530848 A5 JP 2020530848A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- membered
- group selected
- pharmaceutically acceptable
- 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.)
- Ceased
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 90
- 150000001875 compounds Chemical class 0.000 claims description 54
- 125000003118 aryl group Chemical group 0.000 claims description 52
- 150000003839 salts Chemical class 0.000 claims description 51
- 125000000623 heterocyclic group Chemical group 0.000 claims description 46
- 125000001072 heteroaryl group Chemical group 0.000 claims description 44
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 39
- 125000001475 halogen functional group Chemical group 0.000 claims description 36
- UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical compound [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 claims description 26
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 25
- 229910052739 hydrogen Inorganic materials 0.000 claims description 25
- 239000001257 hydrogen Substances 0.000 claims description 25
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 24
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims description 24
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 16
- 229910052799 carbon Inorganic materials 0.000 claims description 16
- 150000002431 hydrogen Chemical class 0.000 claims description 15
- 125000003342 alkenyl group Chemical group 0.000 claims description 11
- 208000023275 Autoimmune disease Diseases 0.000 claims description 10
- 125000000304 alkynyl group Chemical group 0.000 claims description 10
- 208000027866 inflammatory disease Diseases 0.000 claims description 10
- 230000002757 inflammatory effect Effects 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 9
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims description 7
- 238000000034 method Methods 0.000 claims description 7
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims description 6
- 206010013774 Dry eye Diseases 0.000 claims description 6
- 201000004681 Psoriasis Diseases 0.000 claims description 6
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 6
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 4
- 241000124008 Mammalia Species 0.000 claims description 3
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 3
- 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 description 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 3
- -1 -OR 6 Chemical group 0.000 claims description 2
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 2
- 206010012689 Diabetic retinopathy Diseases 0.000 claims description 2
- 206010046851 Uveitis Diseases 0.000 claims description 2
- 125000006193 alkinyl group Chemical group 0.000 claims description 2
- 208000026935 allergic disease Diseases 0.000 claims description 2
- 208000004631 alopecia areata Diseases 0.000 claims description 2
- 229910052805 deuterium Inorganic materials 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 3
- 229910052757 nitrogen Inorganic materials 0.000 description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 3
- 238000007792 addition Methods 0.000 description 2
- 125000005103 alkyl silyl group Chemical group 0.000 description 2
- JXLHNMVSKXFWAO-UHFFFAOYSA-N azane;7-fluoro-2,1,3-benzoxadiazole-4-sulfonic acid Chemical compound N.OS(=O)(=O)C1=CC=C(F)C2=NON=C12 JXLHNMVSKXFWAO-UHFFFAOYSA-N 0.000 description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 description 1
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 description 1
- 150000003463 sulfur Chemical class 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762545331P | 2017-08-14 | 2017-08-14 | |
| US62/545,331 | 2017-08-14 | ||
| PCT/US2018/046532 WO2019036374A1 (en) | 2017-08-14 | 2018-08-13 | 3,4-DISUBSTITUTED 3-CYCLOBUTENE-1,2-DIONES AND THEIR USE |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020530848A JP2020530848A (ja) | 2020-10-29 |
| JP2020530848A5 true JP2020530848A5 (OSRAM) | 2021-09-30 |
Family
ID=63405487
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020508398A Ceased JP2020530848A (ja) | 2017-08-14 | 2018-08-13 | ３，４−二置換３−シクロブテン−１，２−ジオンおよびその使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US11208377B2 (OSRAM) |
| EP (1) | EP3668832A1 (OSRAM) |
| JP (1) | JP2020530848A (OSRAM) |
| KR (1) | KR20200037857A (OSRAM) |
| CN (1) | CN111225900A (OSRAM) |
| AU (1) | AU2018318075B2 (OSRAM) |
| BR (1) | BR112020003245A2 (OSRAM) |
| CA (1) | CA3072671A1 (OSRAM) |
| RU (1) | RU2020106383A (OSRAM) |
| WO (1) | WO2019036374A1 (OSRAM) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112679328B (zh) * | 2019-10-17 | 2023-09-15 | 南京药石科技股份有限公司 | 一种3-三氟甲基-2-环己烯-1-酮的工业化生产方法 |
| KR20210100259A (ko) * | 2020-02-05 | 2021-08-17 | 주식회사 에피바이오텍 | 3,4-디아미노-3-시클로부텐-1,2-디온 유도체를 포함하는 탈모의 예방 또는 치료용 조성물 |
| EP4143179B1 (en) | 2020-04-30 | 2025-10-22 | Idorsia Pharmaceuticals Ltd | Azetidin-3-ylmethanol derivatives as ccr6 receptor modulators for the treatment of cancer |
| US11945788B2 (en) * | 2021-06-07 | 2024-04-02 | Nuray Chemicals Private Limited | Process for preparing pitolisant hydrochloride and solid-state forms thereof |
| WO2023057548A1 (en) | 2021-10-07 | 2023-04-13 | Idorsia Pharmaceuticals Ltd | Ccr6 receptor modulators |
| WO2023072924A1 (en) | 2021-10-26 | 2023-05-04 | Idorsia Pharmaceuticals Ltd | Ccr6 receptor modulators |
| KR20240090693A (ko) | 2021-10-28 | 2024-06-21 | 이도르시아 파마슈티컬스 리미티드 | Ccr6 수용체 조절인자 |
| WO2025092968A1 (zh) * | 2023-11-03 | 2025-05-08 | 武汉朗来科技发展有限公司 | 作为ccr6拮抗剂的化合物、其药物组合物和用途 |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5354763A (en) | 1993-11-17 | 1994-10-11 | American Home Products Corporation | Substituted N-heteroaryl and N-aryl-1,2-diaminocyclobutene-3,4-diones |
| US5506252A (en) | 1993-11-17 | 1996-04-09 | American Home Products Corporation | Substituted N-heteroaryl and N-aryl-1,2-diaminocyclobutene-3,4-diones |
| CN1454204A (zh) | 2000-05-30 | 2003-11-05 | 史密丝克莱恩比彻姆公司 | Il－8受体拮抗剂 |
| US6897231B2 (en) | 2000-07-31 | 2005-05-24 | Signal Pharmaceuticals, Inc. | Indazole derivatives as JNK inhibitors and compositions and methods related thereto |
| ATE346043T1 (de) | 2001-01-16 | 2006-12-15 | Smithkline Beecham Corp | Il-8-rezeptorantagonisten |
| IL156793A0 (en) * | 2001-02-02 | 2004-02-08 | Schering Corp | 3,4-di-substituted cyclobutene-1,2-diones as cxc chemokine receptor antagonists |
| HUP0500644A3 (en) | 2001-03-30 | 2005-11-28 | Smithkline Beecham Corp | Method of synthesizing phenol-containing compounds |
| CA2444031C (en) * | 2001-04-16 | 2012-02-21 | Schering Corporation | 3,4-di-substituted cyclobutene-1,2-diones as cxc-chemokine receptor ligands |
| US7132445B2 (en) * | 2001-04-16 | 2006-11-07 | Schering Corporation | 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands |
| US20040106794A1 (en) | 2001-04-16 | 2004-06-03 | Schering Corporation | 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands |
| US20040097547A1 (en) * | 2001-04-16 | 2004-05-20 | Taveras Arthur G. | 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands |
| WO2003080053A1 (en) | 2002-03-18 | 2003-10-02 | Schering Corporation | Combination treatments for chemokine-mediated diseases |
| DE102005001053A1 (de) | 2005-01-07 | 2006-07-20 | Merck Patent Gmbh | Quadratsäurederivate |
| BRPI0812222A2 (pt) | 2007-06-06 | 2014-12-16 | Novartis Ag | Compostos ciclobutenodiona substituídos anti-inflamatórios. |
| US8563527B2 (en) | 2007-08-20 | 2013-10-22 | Pharmain Corporation | Oligonucleotide core carrier compositions for delivery of nucleic acid-containing therapeutic agents, methods of making and using the same |
| EP2217242A1 (en) | 2007-11-15 | 2010-08-18 | Eisai R&D Management Co., Ltd. | Methods of use |
| US20090156459A1 (en) | 2007-11-16 | 2009-06-18 | Pharmain Corporation | Cationic-Core Carrier Compositions for Delivery of Therapeutic Agents, Methods of Making and Using the Same |
| MX2010007833A (es) | 2008-01-18 | 2010-08-11 | Oxagen Ltd | Compuestos que tienen actividad antagonista de crth2. |
| JP2011509990A (ja) | 2008-01-22 | 2011-03-31 | オキサジェン リミテッド | Ｃｒｔｈ２アンタゴニスト活性を有する化合物 |
| EP2240444A1 (en) | 2008-01-22 | 2010-10-20 | Oxagen Limited | Compounds having crth2 antagonist activity |
| EP2254592B1 (en) | 2008-02-28 | 2019-06-05 | Dako Denmark A/S | Mhc multimers in borrelia diagnostics and disease |
| UA103198C2 (en) | 2008-08-04 | 2013-09-25 | Новартис Аг | Squaramide derivatives as cxcr2 antagonists |
| WO2010063802A1 (en) * | 2008-12-05 | 2010-06-10 | Novartis Ag | 3, 4-di-substituted cyclobutene- 1, 2 -diones as cxcr2 receptor antagonists |
| FR2961695B1 (fr) | 2010-06-29 | 2012-07-06 | Galderma Res & Dev | Utilisation de composes dans le traitement ou la prevention de troubles cutanes |
| WO2012047630A2 (en) | 2010-09-27 | 2012-04-12 | Martin Teintze | N-alkyl or n-aryl substituted guanide and biguanide compounds and methods of their use |
| US8648070B2 (en) * | 2010-12-17 | 2014-02-11 | Boehringer Ingelheim International Gmbh | Bicyclic ring system substituted sulfonamide functionalised phenols as medicaments |
| FR2981934B1 (fr) * | 2011-10-28 | 2013-12-20 | Galderma Res & Dev | Nouveaux composes di-substitues de la diamino-3,4-cyclobutene-3-dione-1,2 utiles dans le traitement de pathologies mediees par des chimiokines. |
| FR2981935B1 (fr) | 2011-10-28 | 2015-08-07 | Galderma Res & Dev | Nouveaux composes di-substitues de la diamino-3,4-cyclobutene-3-dione-1,2 utiles dans le traitement de pathologies mediees par des chimiokines. |
| KR102331833B1 (ko) | 2013-12-02 | 2021-11-25 | 케모센트릭스, 인크. | Ccr6 화합물 |
| US9618513B2 (en) | 2014-01-27 | 2017-04-11 | The Regents Of The University Of Michigan | Compositions and methods for detecting and treating colorectal cancer |
| TWI734715B (zh) | 2015-11-19 | 2021-08-01 | 美商卡默森屈有限公司 | 趨化因子受體調節劑 |
| TWI724056B (zh) | 2015-11-19 | 2021-04-11 | 美商卡默森屈有限公司 | Ｃｘｃｒ２抑制劑 |
-
2018
- 2018-08-13 RU RU2020106383A patent/RU2020106383A/ru unknown
- 2018-08-13 EP EP18760225.5A patent/EP3668832A1/en not_active Withdrawn
- 2018-08-13 BR BR112020003245-0A patent/BR112020003245A2/pt not_active Application Discontinuation
- 2018-08-13 WO PCT/US2018/046532 patent/WO2019036374A1/en not_active Ceased
- 2018-08-13 CA CA3072671A patent/CA3072671A1/en active Pending
- 2018-08-13 JP JP2020508398A patent/JP2020530848A/ja not_active Ceased
- 2018-08-13 KR KR1020207007312A patent/KR20200037857A/ko not_active Ceased
- 2018-08-13 CN CN201880066725.7A patent/CN111225900A/zh active Pending
- 2018-08-13 AU AU2018318075A patent/AU2018318075B2/en not_active Expired - Fee Related
- 2018-08-14 US US16/103,607 patent/US11208377B2/en active Active
-
2021
- 2021-12-08 US US17/545,940 patent/US20220402866A1/en not_active Abandoned
-
2024
- 2024-03-11 US US18/601,679 patent/US20240400501A1/en active Pending
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