AR112227A2 - Sal de hemifumarato del ácido 1-(4-{1-[(e)-4-ciclohexil-3-trifluorometil-benciloxi-imino]-etil}-2-etil-bencil)-azetidin-3-carboxílico, y otras formas cristalinas de la misma - Google Patents
Sal de hemifumarato del ácido 1-(4-{1-[(e)-4-ciclohexil-3-trifluorometil-benciloxi-imino]-etil}-2-etil-bencil)-azetidin-3-carboxílico, y otras formas cristalinas de la mismaInfo
- Publication number
- AR112227A2 AR112227A2 ARP180101916A AR112227A2 AR 112227 A2 AR112227 A2 AR 112227A2 AR P180101916 A ARP180101916 A AR P180101916A AR 112227 A2 AR112227 A2 AR 112227A2
- Authority
- AR
- Argentina
- Prior art keywords
- ethyl
- trifluoromethyl
- cyclohexyl
- benzyl
- benzyloxy
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title abstract 3
- 239000002253 acid Substances 0.000 title abstract 2
- -1 4- {1 - [(E) -4-CYCLOHEXYL-3-TRIFLUORomethyl-BENZYLOXY-IMINO] -ETHYL} -2-ETHYL-BENZYL Chemical class 0.000 title 1
- 239000013078 crystal Substances 0.000 title 1
- 238000000034 method Methods 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- KIHYPELVXPAIDH-HNSNBQBZSA-N 1-[[4-[(e)-n-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-c-methylcarbonimidoyl]-2-ethylphenyl]methyl]azetidine-3-carboxylic acid Chemical compound CCC1=CC(C(\C)=N\OCC=2C=C(C(C3CCCCC3)=CC=2)C(F)(F)F)=CC=C1CN1CC(C(O)=O)C1 KIHYPELVXPAIDH-HNSNBQBZSA-N 0.000 abstract 1
- UJXFWRARCPDBIX-UZWMFBFFSA-N C1CN(CC2=C(CC)C=C(C=C2)C(\C)=N\OCC2=CC=C(C3CCCCC3)C(=C2)C(F)(F)F)C1 Chemical compound C1CN(CC2=C(CC)C=C(C=C2)C(\C)=N\OCC2=CC=C(C3CCCCC3)C(=C2)C(F)(F)F)C1 UJXFWRARCPDBIX-UZWMFBFFSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
- C07C57/13—Dicarboxylic acids
- C07C57/15—Fumaric acid
-
- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Esta solicitud se refiere a una sal de hemi-fumarato del ácido 1-(4-{1-[(E)-4-ciclohexil-3-trifluorometil-benciloxi-imino]-etil}-2-etil-bencil)-azetidin-3-carboxílico, a composiciones farmacéuticas que comprenden esta sal, a procesos para formar esta sal, y a su uso en un tratamiento médico. En adición, la presente también se refiere a formas polimórficas de la forma de sal de hemi-fumarato del compuesto [formas A, B, C y D], así como a composiciones farmacéuticas que comprenden estas formas polimórficas, a procesos para obtenerlas, y a su uso en un tratamiento médico. Reivindicación 1: Forma cristalina A del ácido 1-(4-{1-[(E)-4-ciclohexil-3-trifluorometil-benciloxiimino]-etil}-2-etil-bencil)-azetidin-3-carboxílico, ácido (E)-but-2-endioico, caracterizado porque la forma cristalina tiene un patrón de difracción en polvo de rayos X que tiene por los menos un pico específico a aproximadamente 2-q = 20.7º.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US20305308P | 2008-12-18 | 2008-12-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR112227A2 true AR112227A2 (es) | 2019-10-02 |
Family
ID=42236293
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090104917A AR074694A1 (es) | 2008-12-18 | 2009-12-16 | Sal de hemifumarato del acido 1-(4-{1-[(e)-4-ciclohexil-3-trifluoro-metil-benciloxi-imino]-etil}-2-etil-bencil)-azetidin-3-carboxilico, y otras formas cristalinas de la misma. |
| ARP180101916 AR112227A2 (es) | 2008-12-18 | 2018-07-10 | Sal de hemifumarato del ácido 1-(4-{1-[(e)-4-ciclohexil-3-trifluorometil-benciloxi-imino]-etil}-2-etil-bencil)-azetidin-3-carboxílico, y otras formas cristalinas de la misma |
| ARP210100712A AR121635A2 (es) | 2008-12-18 | 2021-03-22 | Nueva sal y formas cristalinas |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090104917A AR074694A1 (es) | 2008-12-18 | 2009-12-16 | Sal de hemifumarato del acido 1-(4-{1-[(e)-4-ciclohexil-3-trifluoro-metil-benciloxi-imino]-etil}-2-etil-bencil)-azetidin-3-carboxilico, y otras formas cristalinas de la misma. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP210100712A AR121635A2 (es) | 2008-12-18 | 2021-03-22 | Nueva sal y formas cristalinas |
Country Status (35)
| Country | Link |
|---|---|
| US (7) | US20120115840A1 (es) |
| EP (2) | EP2379497B1 (es) |
| JP (1) | JP5627597B2 (es) |
| KR (5) | KR101885052B1 (es) |
| CN (2) | CN102256943A (es) |
| AR (3) | AR074694A1 (es) |
| AU (1) | AU2009335924B2 (es) |
| BR (1) | BRPI0923176B8 (es) |
| CA (2) | CA2747437C (es) |
| CL (1) | CL2011001490A1 (es) |
| CO (1) | CO6390104A2 (es) |
| CY (2) | CY1114662T1 (es) |
| DK (2) | DK2676953T3 (es) |
| EC (1) | ECSP11011210A (es) |
| ES (2) | ES2436197T3 (es) |
| HR (2) | HRP20131106T1 (es) |
| HU (1) | HUE034819T2 (es) |
| IL (3) | IL253845B (es) |
| JO (1) | JO2894B1 (es) |
| LT (1) | LT2676953T (es) |
| MA (1) | MA32961B1 (es) |
| MX (1) | MX2011006609A (es) |
| MY (1) | MY152669A (es) |
| NZ (1) | NZ593061A (es) |
| PE (2) | PE20120336A1 (es) |
| PL (2) | PL2676953T3 (es) |
| PT (2) | PT2676953T (es) |
| RS (2) | RS53041B (es) |
| RU (1) | RU2518114C3 (es) |
| SG (1) | SG171785A1 (es) |
| SI (2) | SI2676953T1 (es) |
| TW (2) | TWI591055B (es) |
| UY (1) | UY32330A (es) |
| WO (1) | WO2010080409A1 (es) |
| ZA (1) | ZA201103709B (es) |
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| PL3129006T3 (pl) | 2014-04-10 | 2021-07-05 | Novartis Ag | Formulacja immunosupresanta |
| SG11201607894RA (en) * | 2014-04-10 | 2016-10-28 | Novartis Ag | S1p modulator immediate release dosage regimen |
| US20180042895A1 (en) | 2015-02-26 | 2018-02-15 | Novartis Ag | Treatment of autoimmune disease in a patient receiving additionally a beta-blocker |
| EP3400211A1 (en) | 2016-01-04 | 2018-11-14 | Auspex Pharmaceuticals, Inc. | Azetidine modulators of the sphingosine 1-phosphate receptor |
| US11434200B2 (en) | 2017-03-09 | 2022-09-06 | Novartis Ag | Solid forms comprising an oxime ether compound and a coformer, compositions and methods of use thereof |
| US11629124B2 (en) | 2017-03-09 | 2023-04-18 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
| US11958805B2 (en) * | 2017-03-09 | 2024-04-16 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
| AU2018341136A1 (en) * | 2017-09-27 | 2020-03-12 | Novartis Ag | Parenteral formulation comprising siponimod |
| CN111405897A (zh) | 2017-09-27 | 2020-07-10 | 雷迪博士实验室有限公司 | 辛波莫德、其盐及其固态形式的制备方法 |
| AU2018343239A1 (en) | 2017-09-29 | 2020-03-12 | Novartis Ag | Dosing regimen of siponimod |
| AU2018341154A1 (en) * | 2017-09-29 | 2020-03-12 | Novartis Ag | Dosing regimen of siponimod |
| US11673860B2 (en) * | 2018-01-22 | 2023-06-13 | Teva Pharmaceuticals International Gmbh | Crystalline siponimod fumaric acid and polymorphs thereof |
| CN110776450B (zh) * | 2018-07-27 | 2022-09-27 | 广东东阳光药业有限公司 | 一种辛波莫德晶型及其制备方法 |
| KR20200072795A (ko) | 2018-12-13 | 2020-06-23 | 고려대학교 산학협력단 | 옥시이미노메틸벤젠 유도체를 유효성분으로 포함하는 일주기 연관성 질환의 예방 또는 치료용 약학적 조성물 |
| CN111484434A (zh) * | 2019-01-29 | 2020-08-04 | 东莞市东阳光仿制药研发有限公司 | 一种辛波莫德晶型及其制备方法 |
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| US20220144768A1 (en) * | 2019-02-27 | 2022-05-12 | Dr. Reddy's Laboratories Limited | Solid state forms of siponimod |
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| KR20220093330A (ko) | 2019-10-31 | 2022-07-05 | 이도르시아 파마슈티컬스 리미티드 | Cxcr7 안타고니스트와 s1p1 수용체 조절인자의 조합 |
| GB202002560D0 (en) * | 2020-02-24 | 2020-04-08 | Johnson Matthey Plc | Crystalline forms of voxelotor, and processes for the preparation thereof |
| US20230212115A1 (en) * | 2020-05-29 | 2023-07-06 | Cipla Limited | Methods for the preparation of sphingosine 1-phosphate receptor modulators and solid forme thereof |
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2009
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