CA2789480A1 - Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof - Google Patents
Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof Download PDFInfo
- Publication number
- CA2789480A1 CA2789480A1 CA2789480A CA2789480A CA2789480A1 CA 2789480 A1 CA2789480 A1 CA 2789480A1 CA 2789480 A CA2789480 A CA 2789480A CA 2789480 A CA2789480 A CA 2789480A CA 2789480 A1 CA2789480 A1 CA 2789480A1
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- Prior art keywords
- salt
- trifluoromethyl
- isopropoxy
- benzyloxy
- pyrrolo
- Prior art date
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- ONDSBJMLAHVLMI-UHFFFAOYSA-N trimethylsilyldiazomethane Chemical compound C[Si](C)(C)[CH-][N+]#N ONDSBJMLAHVLMI-UHFFFAOYSA-N 0.000 description 1
- FIQMHBFVRAXMOP-UHFFFAOYSA-N triphenylphosphane oxide Chemical compound C=1C=CC=CC=1P(C=1C=CC=CC=1)(=O)C1=CC=CC=C1 FIQMHBFVRAXMOP-UHFFFAOYSA-N 0.000 description 1
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- 210000005166 vasculature Anatomy 0.000 description 1
- 206010047470 viral myocarditis Diseases 0.000 description 1
- 239000011345 viscous material Substances 0.000 description 1
- 239000003039 volatile agent Substances 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
- DJWUNCQRNNEAKC-UHFFFAOYSA-L zinc acetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O DJWUNCQRNNEAKC-UHFFFAOYSA-L 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
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- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
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- Chemical Kinetics & Catalysis (AREA)
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- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| US33936210P | 2010-03-03 | 2010-03-03 | |
| US61/339,362 | 2010-03-03 | ||
| PCT/US2011/026806 WO2011109471A1 (en) | 2010-03-03 | 2011-03-02 | Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof |
Publications (1)
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| CA2789480A1 true CA2789480A1 (en) | 2011-09-09 |
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| CA2789480A Withdrawn CA2789480A1 (en) | 2010-03-03 | 2011-03-02 | Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof |
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| EP (1) | EP2542554B1 (enExample) |
| JP (2) | JP2013521301A (enExample) |
| CN (2) | CN105503882B (enExample) |
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| SG (2) | SG183416A1 (enExample) |
| WO (1) | WO2011109471A1 (enExample) |
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| MX354134B (es) | 2008-07-23 | 2018-02-14 | Arena Pharm Inc | Derivados de acido 1,2,3,4-tetrahidrociclopenta [b] indol-3-il) acetico sustituidos utiles en el tratamiento de enfermedades autoinmune e inflamatorias. |
| NZ591001A (en) * | 2008-08-27 | 2012-11-30 | Arena Pharm Inc | Substituted tricyclic acid derivatives as s1p1 receptor agonists useful in the treatment of autoimmune and inflammatory disorders |
| EP4148045A1 (en) | 2010-01-27 | 2023-03-15 | Arena Pharmaceuticals, Inc. | Intermediate compounds for the preparation of (r)-2-(7-(4-cyclopentyl-3- (trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b] indol-3-yl)acetic acid and salts thereof |
| SG183416A1 (en) * | 2010-03-03 | 2012-09-27 | Arena Pharm Inc | Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof |
| EP3212626B1 (en) * | 2014-10-27 | 2018-11-07 | Cellix Bio Private Limited | Three component salts of fumaric acid monomethyl ester with piperazine or ethylene diamine for the treatment of multiple sclerosis |
| KR102595163B1 (ko) | 2015-01-06 | 2023-10-30 | 아레나 파마슈티칼스, 인크. | S1p1 수용체와 관련된 상태의 치료 방법 |
| EA201890096A1 (ru) | 2015-06-22 | 2018-08-31 | Арена Фармасьютикалз, Инк. | КРИСТАЛЛИЧЕСКАЯ L-АРГИНИНОВАЯ СОЛЬ (R)-2-(7-(4-ЦИКЛОПЕНТИЛ-3-(ТРИФТОРМЕТИЛ)БЕНЗИЛОКСИ)-1,2,3,4-ТЕТРАГИДРОЦИКЛОПЕНТА[b]ИНДОЛ-3-ИЛ)УКСУСНОЙ КИСЛОТЫ (СОЕДИНЕНИЯ 1) ДЛЯ ПРИМЕНЕНИЯ ПРИ РАССТРОЙСТВАХ, СВЯЗАННЫХ С S1P-РЕЦЕПТОРОМ |
| CA3053418A1 (en) | 2017-02-16 | 2018-08-23 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of primary biliary cholangitis |
| CN110545848A (zh) | 2017-02-16 | 2019-12-06 | 艾尼纳制药公司 | 用于治疗具有肠外表现的炎症性肠病的化合物和方法 |
| CN112601516A (zh) | 2018-06-06 | 2021-04-02 | 艾尼纳制药公司 | 治疗与s1p1受体相关的病况的方法 |
| WO2020051378A1 (en) | 2018-09-06 | 2020-03-12 | Arena Pharmaceuticals, Inc. | Compounds useful in the treatment of autoimmune and inflammatory disorders |
| EP3870181B1 (en) * | 2018-10-26 | 2024-08-14 | Keros Therapeutics, Inc. | Crystal forms of an alk2 inhibitor |
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-
2011
- 2011-03-02 SG SG2012061685A patent/SG183416A1/en unknown
- 2011-03-02 EP EP11707330.4A patent/EP2542554B1/en active Active
- 2011-03-02 CN CN201510932844.4A patent/CN105503882B/zh active Active
- 2011-03-02 SG SG10201501575VA patent/SG10201501575VA/en unknown
- 2011-03-02 US US13/581,846 patent/US9085581B2/en active Active
- 2011-03-02 ES ES11707330.4T patent/ES2558087T3/es active Active
- 2011-03-02 JP JP2012556199A patent/JP2013521301A/ja not_active Abandoned
- 2011-03-02 CN CN201180022490.XA patent/CN102884064B/zh active Active
- 2011-03-02 CA CA2789480A patent/CA2789480A1/en not_active Withdrawn
- 2011-03-02 WO PCT/US2011/026806 patent/WO2011109471A1/en not_active Ceased
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2015
- 2015-06-15 US US14/739,341 patent/US20150284399A1/en not_active Abandoned
- 2015-07-17 JP JP2015142650A patent/JP2015180706A/ja not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN105503882A (zh) | 2016-04-20 |
| JP2013521301A (ja) | 2013-06-10 |
| ES2558087T3 (es) | 2016-02-01 |
| HK1179627A1 (zh) | 2013-10-04 |
| CN102884064B (zh) | 2016-01-13 |
| CN105503882B (zh) | 2019-07-05 |
| EP2542554B1 (en) | 2015-11-04 |
| US9085581B2 (en) | 2015-07-21 |
| WO2011109471A1 (en) | 2011-09-09 |
| US20120329848A1 (en) | 2012-12-27 |
| CN102884064A (zh) | 2013-01-16 |
| EP2542554A1 (en) | 2013-01-09 |
| US20150284399A1 (en) | 2015-10-08 |
| SG183416A1 (en) | 2012-09-27 |
| SG10201501575VA (en) | 2015-04-29 |
| JP2015180706A (ja) | 2015-10-15 |
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