CN103204794A - 新的盐 - Google Patents

新的盐 Download PDF

Info

Publication number
CN103204794A
CN103204794A CN2013101141799A CN201310114179A CN103204794A CN 103204794 A CN103204794 A CN 103204794A CN 2013101141799 A CN2013101141799 A CN 2013101141799A CN 201310114179 A CN201310114179 A CN 201310114179A CN 103204794 A CN103204794 A CN 103204794A
Authority
CN
China
Prior art keywords
compound
ethyl
crystallized form
benzyl
salt
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.)
Pending
Application number
CN2013101141799A
Other languages
English (en)
Chinese (zh)
Inventor
M·德拉克鲁兹
P·H·卡比恩斯基
刘玉刚
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Novartis AG
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Novartis AG filed Critical Novartis AG
Publication of CN103204794A publication Critical patent/CN103204794A/zh
Pending legal-status Critical Current

Links

Images

Classifications

    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/06—Antibacterial agents for tuberculosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A61P31/08—Antibacterial agents for leprosy
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN2013101141799A 2008-12-18 2009-12-17 新的盐 Pending CN103204794A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US20305108P 2008-12-18 2008-12-18
US61/203,051 2008-12-18

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN2009801504811A Division CN102256941A (zh) 2008-12-18 2009-12-17 新的盐

Publications (1)

Publication Number Publication Date
CN103204794A true CN103204794A (zh) 2013-07-17

Family

ID=42316715

Family Applications (2)

Application Number Title Priority Date Filing Date
CN2013101141799A Pending CN103204794A (zh) 2008-12-18 2009-12-17 新的盐
CN2009801504811A Pending CN102256941A (zh) 2008-12-18 2009-12-17 新的盐

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN2009801504811A Pending CN102256941A (zh) 2008-12-18 2009-12-17 新的盐

Country Status (12)

Country Link
US (2) US8486930B2 (https=)
EP (1) EP2379499B1 (https=)
JP (1) JP2012512885A (https=)
KR (1) KR20110101159A (https=)
CN (2) CN103204794A (https=)
AU (1) AU2009335887A1 (https=)
BR (1) BRPI0922466A2 (https=)
CA (1) CA2747558A1 (https=)
ES (1) ES2478842T3 (https=)
MX (1) MX2011006622A (https=)
RU (1) RU2011129229A (https=)
WO (1) WO2010080455A1 (https=)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013535480A (ja) * 2010-08-05 2013-09-12 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 ２−［２−［［（４−メトキシ−２，６−ジメチルフェニル）スルホニル］−（メチル）アミノ］エトキシ］−ｎ−メチル−ｎ−［３−（４−メチルピペラジン−１−イル）シクロヘキシル］アセトアミドの酸付加塩及びそのブラジキニンｂ１受容体アンタゴニストとしての使用
BR112013017302B1 (pt) 2011-01-07 2021-12-07 Novartis Ag Composição farmacêutica em fase sólida
WO2012095853A1 (en) 2011-01-10 2012-07-19 Novartis Pharma Ag Modified release formulations comprising sip receptor modulators
WO2016135644A1 (en) 2015-02-26 2016-09-01 Novartis Ag Treatment of autoimmune disease in a patient receiving additionally a beta-blocker
WO2017120124A1 (en) 2016-01-04 2017-07-13 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
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
MX2020007268A (es) 2017-09-29 2020-08-17 Novartis Ag Regimen de dosificacion de siponimod.
EP3743405B1 (en) 2018-01-22 2023-11-15 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
JP7604387B2 (ja) * 2019-03-28 2024-12-23 ファースト・バイオセラピューティクス・インコーポレイテッド ベンゾチアゾール化合物の薬学的塩、多形体及びその製造方法
EP3972954A1 (en) 2019-05-21 2022-03-30 Synthon B.V. Siponimod maleic acid and fumaric acid salt
AU2020372647B2 (en) 2019-10-31 2026-02-05 Idorsia Pharmaceuticals Ltd Combination of a CXCR7 antagonist with an S1P1 receptor modulator
WO2021158838A1 (en) * 2020-02-07 2021-08-12 Argentum Pharmaceuticals Llc Dosage regimen of an s1p receptor modulator
WO2022064007A1 (en) 2020-09-25 2022-03-31 Synthon B.V. Siponimod salts and cocrystals
CN112402610A (zh) * 2020-11-20 2021-02-26 睿阜隆(杭州)生物医药有限公司 1-磷酸鞘氨醇受体调节剂在制备治疗糖尿病的药物中的新用途
EP4212156A1 (en) 2022-01-13 2023-07-19 Abivax Combination of 8-chloro-n-(4-(trifluoromethoxy)phenyl)quinolin-2-amine and its derivatives with a s1p receptor modulator

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1791395A (zh) * 2003-05-19 2006-06-21 Irm责任有限公司 免疫抑制剂化合物及组合物
CN101068536A (zh) * 2004-11-29 2007-11-07 诺瓦提斯公司 S1p受体激动剂的剂量方案
CN101237852A (zh) * 2005-08-09 2008-08-06 诺瓦提斯公司 液体制剂

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL86632A0 (en) 1987-06-15 1988-11-30 Ciba Geigy Ag Derivatives substituted at methyl-amino nitrogen
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
TW225528B (https=) 1992-04-03 1994-06-21 Ciba Geigy Ag
BR9207175A (pt) 1992-10-28 1995-12-12 Genentech Inc Composição contendo antagonista de fator de crescimento de célula endotelial vascular sequência aminoácida de anticorpo monoclonal polipeptídeo e método de tratamento de tumor em mamífero
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
US5362718A (en) 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
MX9707453A (es) 1995-03-30 1997-12-31 Pfizer Derivados de quinazolina.
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
MX9800215A (es) 1995-07-06 1998-03-31 Novartis Ag Pirrolopirimidas y procesos para su preparacion.
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
HU228446B1 (en) 1996-04-12 2013-03-28 Warner Lambert Co Kinazoline derivatives as irreversible inhibitors of protein-kinase, pharmaceutical compositions containing these compounds and use thereof
EP0907642B1 (en) 1996-06-24 2005-11-02 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
US6258823B1 (en) 1996-07-12 2001-07-10 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
DE19638745C2 (de) 1996-09-11 2001-05-10 Schering Ag Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR)
CA2265630A1 (en) 1996-09-13 1998-03-19 Gerald Mcmahon Use of quinazoline derivatives for the manufacture of a medicament in the treatment of hyperproliferative skin disorders
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
TW557297B (en) 1997-09-26 2003-10-11 Abbott Lab Rapamycin analogs having immunomodulatory activity, and pharmaceutical compositions containing same
GB9721069D0 (en) 1997-10-03 1997-12-03 Pharmacia & Upjohn Spa Polymeric derivatives of camptothecin
ATE459616T1 (de) 1998-08-11 2010-03-15 Novartis Ag Isochinoline derivate mit angiogenesis-hemmender wirkung
GB9824579D0 (en) 1998-11-10 1999-01-06 Novartis Ag Organic compounds
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
WO2000037502A2 (en) 1998-12-22 2000-06-29 Genentech, Inc. Vascular endothelial cell growth factor antagonists and uses thereof
WO2000059509A1 (en) 1999-03-30 2000-10-12 Novartis Ag Phthalazine derivatives for treating inflammatory diseases
AU783158B2 (en) 1999-08-24 2005-09-29 Ariad Pharmaceuticals, Inc. 28-epirapalogs
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
GB0612721D0 (en) 2006-06-27 2006-08-09 Novartis Ag Organic compounds

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1791395A (zh) * 2003-05-19 2006-06-21 Irm责任有限公司 免疫抑制剂化合物及组合物
CN101068536A (zh) * 2004-11-29 2007-11-07 诺瓦提斯公司 S1p受体激动剂的剂量方案
CN101237852A (zh) * 2005-08-09 2008-08-06 诺瓦提斯公司 液体制剂

Also Published As

Publication number Publication date
CN102256941A (zh) 2011-11-23
US20110257150A1 (en) 2011-10-20
AU2009335887A1 (en) 2011-06-30
EP2379499B1 (en) 2014-04-09
JP2012512885A (ja) 2012-06-07
US20130225550A1 (en) 2013-08-29
EP2379499A1 (en) 2011-10-26
MX2011006622A (es) 2011-07-12
CA2747558A1 (en) 2010-07-15
US8486930B2 (en) 2013-07-16
WO2010080455A1 (en) 2010-07-15
BRPI0922466A2 (pt) 2018-10-23
RU2011129229A (ru) 2013-01-27
KR20110101159A (ko) 2011-09-15
ES2478842T3 (es) 2014-07-23
US8697682B2 (en) 2014-04-15

Similar Documents

Publication Publication Date Title
CN103204794A (zh) 新的盐
US20240239743A1 (en) 1-(4-{1-[(e)-4-cyclohexyl-3-trifluoromethylbenzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid, (e)-but-2-enedioic acid
CN102256942B (zh) 1-(4-{1-[(e)-4-环己基-3-三氟甲基-苄氧基亚氨基]-乙基}-2-乙基-苄基)-氮杂环丁烷-3-甲酸的多晶型物
AU2013231122A1 (en) New Salts
HK1159631B (en) Hemifumarate salt of 1-(4-{1-[4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-a zetidine-3-carboxylic acid
HK1189588B (en) Hemifumarate salt of 1-[4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl]-azetidine-3-carboxylic acid for use in the treatment of lymphocyte mediated diseases

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20130717