JP2013521301A - S1p1受容体修飾物質およびその結晶形の調製のためのプロセス - Google Patents

S1p1受容体修飾物質およびその結晶形の調製のためのプロセス Download PDF

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JP2013521301A
JP2013521301A JP2012556199A JP2012556199A JP2013521301A JP 2013521301 A JP2013521301 A JP 2013521301A JP 2012556199 A JP2012556199 A JP 2012556199A JP 2012556199 A JP2012556199 A JP 2012556199A JP 2013521301 A JP2013521301 A JP 2013521301A
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isopropoxy
trifluoromethyl
salt
pyrrolo
dihydro
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JP2013521301A5 (OSRAM
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ロバート エム. ジョンズ,
ダニエル ジェイ. バザード,
タウフィック ガルバウイ,
ベンジャミン アール. ジョンソン,
ミッシェル カセム,
トーマス オー. シュレイダー,
スコット スティルン,
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アリーナ ファーマシューティカルズ, インコーポレイテッド
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Publication of JP2013521301A publication Critical patent/JP2013521301A/ja
Publication of JP2013521301A5 publication Critical patent/JP2013521301A5/ja
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
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  • Virology (AREA)
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  • Biomedical Technology (AREA)
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  • Rheumatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2012556199A 2010-03-03 2011-03-02 S1p1受容体修飾物質およびその結晶形の調製のためのプロセス Abandoned JP2013521301A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
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

Related Child Applications (1)

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JP2015142650A Division JP2015180706A (ja) 2010-03-03 2015-07-17 S1p1受容体修飾物質およびその結晶形の調製のためのプロセス

Publications (2)

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JP2013521301A true JP2013521301A (ja) 2013-06-10
JP2013521301A5 JP2013521301A5 (OSRAM) 2014-04-17

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JP2012556199A Abandoned JP2013521301A (ja) 2010-03-03 2011-03-02 S1p1受容体修飾物質およびその結晶形の調製のためのプロセス
JP2015142650A Abandoned JP2015180706A (ja) 2010-03-03 2015-07-17 S1p1受容体修飾物質およびその結晶形の調製のためのプロセス

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Country Status (8)

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US (2) US9085581B2 (OSRAM)
EP (1) EP2542554B1 (OSRAM)
JP (2) JP2013521301A (OSRAM)
CN (2) CN102884064B (OSRAM)
CA (1) CA2789480A1 (OSRAM)
ES (1) ES2558087T3 (OSRAM)
SG (2) SG10201501575VA (OSRAM)
WO (1) WO2011109471A1 (OSRAM)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017533954A (ja) * 2014-10-27 2017-11-16 セリックス バイオ プライヴェート リミテッドCellix Bio Private Limited 多発性硬化症の治療のための、フマル酸モノメチルエステルとピペラジン又はエチレンジアミンとの3つの成分の塩

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8580841B2 (en) 2008-07-23 2013-11-12 Arena Pharmaceuticals, Inc. Substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives useful in the treatment of autoimmune and inflammatory disorders
CN105816453B (zh) * 2008-08-27 2021-03-05 艾尼纳制药公司 用于治疗自身免疫性病症和炎性病症的作为s1p1受体激动剂的经取代的三环酸衍生物
SG182610A1 (en) 2010-01-27 2012-08-30 Arena Pharm Inc Processes 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
CA2789480A1 (en) * 2010-03-03 2011-09-09 Arena Pharmaceuticals, Inc. Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof
US11007175B2 (en) 2015-01-06 2021-05-18 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
BR112017027656B1 (pt) 2015-06-22 2023-12-05 Arena Pharmaceuticals, Inc. Hábito cristalino de placa livre de sal de l-arginina de ácido (r)-2-(7-(4- ciclopentil-3-(trifluorometil)benzilóxi)- 1,2,3,4-tetra-hidrociclo-penta[b]indol-3- il)acético, composição farmacêutica que o compreende, seus usos e método de preparação do mesmo
CA3053418A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
JP2020507610A (ja) 2017-02-16 2020-03-12 アリーナ ファーマシューティカルズ, インコーポレイテッド 腸管外症状を伴う炎症性腸疾患の治療のための化合物および方法
BR112020024762A2 (pt) 2018-06-06 2021-03-23 Arena Pharmaceuticals, Inc. métodos de tratamento de condições relacionadas ao receptor s1p1
CN119751336A (zh) 2018-09-06 2025-04-04 艾尼纳制药公司 可用于治疗自身免疫性病症和炎性病症的化合物
JP7504880B2 (ja) * 2018-10-26 2024-06-24 ケロス セラピューティクス インコーポレイテッド Alk2阻害剤の結晶形

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010064707A1 (ja) * 2008-12-05 2010-06-10 アステラス製薬株式会社 2h-クロメン化合物及びその誘導体
WO2011005295A1 (en) * 2009-06-24 2011-01-13 Arena Pharmaceuticals, Inc. Modulators of the sphingosine-1-phosphate (s1p) receptor useful for the treatment of disorders related thereto
JP2011510073A (ja) * 2008-01-25 2011-03-31 アリーナ ファーマシューティカルズ, インコーポレイテッド S1P1アゴニストとして作用するジヒドロ−1H−ピロロ[1,2−a]インドール−1−イルカルボン酸誘導体
JP2012501327A (ja) * 2008-08-27 2012-01-19 アリーナ ファーマシューティカルズ, インコーポレイテッド 自己免疫障害および免疫性障害の治療において有用なs1p1受容体のアゴニストとしての置換三環式酸誘導体

Family Cites Families (146)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL293572A (OSRAM) * 1962-06-07
DE2226703A1 (de) 1972-05-25 1973-12-13 Schering Ag Neue tetrahydrocarbazolderivate und verfahren zu ihrer herstellung
US4057559A (en) 1973-10-01 1977-11-08 American Home Products Corporation Carbazole acetic acid derivatives
US4810699A (en) 1987-02-20 1989-03-07 American Home Products Corporation Substituted 1,3,4,9-tetrahydropyrano[3,4,-b]indole-1-acetic acids, pharmaceutical compositions containing them, and methods for treating inflammatory conditions and for analgesic purposes using them
US4782076A (en) 1988-03-01 1988-11-01 American Home Products Corporation Substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid derivatives, composition and use
PT95692A (pt) 1989-10-27 1991-09-13 American Home Prod Processo para a preparacao de derivados de acidos indole-,indeno-,piranoindole- e tetra-hidrocarbazole-alcanoicos, ou quais sao uteis como inibidores de pla2 e da lipoxigenase
US5221678A (en) 1990-07-26 1993-06-22 Merck Frosst Canada, Inc. (quinolin-2-ylmethoxy)tetrahydrocarbazoles as inhibitors of the biosynthesis of leukotrienes
US5998499A (en) 1994-03-25 1999-12-07 Dentsply G.M.B.H. Liquid crystalline (meth)acrylate compounds, composition and method
US5776967A (en) 1996-07-26 1998-07-07 American Home Products Corporation Pyranoindole inhibitors of COX--2
US5830911A (en) 1996-08-14 1998-11-03 American Home Products Corporation Pyranoindole and tetrahydrocarbazole inhibitors of COX-2
US6861448B2 (en) 1998-01-14 2005-03-01 Virtual Drug Development, Inc. NAD synthetase inhibitors and uses thereof
CN101070316A (zh) 1999-04-28 2007-11-14 萨诺费-阿文蒂斯德国有限公司 作为ppar受体配体的二芳基酸衍生物
US6410583B1 (en) 2000-07-25 2002-06-25 Merck Frosst Canada & Co. Cyclopentanoindoles, compositions containing such compounds and methods of treatment
AU2002223492A1 (en) 2000-11-14 2002-05-27 Neurosearch A/S Use of malaria parasite anion channel blockers for treating malaria
AU2002237988B2 (en) 2001-01-30 2008-01-03 University Of Virginia Patent Foundation Agonists and antagonists of sphingosine-1-phosphate receptors
US7534547B2 (en) 2001-03-29 2009-05-19 Osaka Gas Company Limited Optically active compound and photosensitive resin composition
EP1391199B1 (en) 2001-05-10 2008-12-10 Ono Pharmaceutical Co., Ltd. Carboxylic acid derivatives and drugs containing the same as the active ingredient
AU2002332289B2 (en) 2001-09-27 2007-05-10 Kyorin Pharmaceutical Co., Ltd. Diaryl sulfide derivative, addition salt thereof, and immunosuppressant
AU2003207567B2 (en) 2002-01-18 2008-01-24 Merck Sharp & Dohme Corp. Edg receptor agonists
AU2003216054B2 (en) 2002-01-18 2007-01-04 Merck & Co., Inc. Selective S1P1/Edg1 receptor agonists
EP1467729A1 (en) 2002-01-18 2004-10-20 The Genetics Company Inc. Beta-secretase inhibitors
AU2003218056A1 (en) 2002-03-01 2003-09-16 Merck & Co., Inc. Aminoalkylphosphonates and related compounds as edg receptor agonists
CA2477423A1 (en) 2002-03-01 2003-09-12 Merck & Co., Inc. Aminoalkylphosphonates and related compounds as edg receptor agonists
JP2005533058A (ja) 2002-06-17 2005-11-04 メルク エンド カムパニー インコーポレーテッド Edg受容体アゴニストとしての1−((5−アリール−1,2,4−オキサジアゾール−3−イル)ベンジル)アゼチジン−3−カルボキシラートおよび1−((5−アリール−1,2,4−オキサジアゾール−3−イル)ベンジル)ピロリジン−3−カルボキシラート
WO2004007472A1 (ja) 2002-07-10 2004-01-22 Ono Pharmaceutical Co., Ltd. Ccr4アンタゴニストおよびその医薬用途
EP1546110A4 (en) 2002-07-30 2008-03-26 Univ Virginia COMPOUNDS WITH EFFECT ON SIGNAL TRANSMISSION BY SPHINGOSINE-1-PHOSPHATE
US7960369B2 (en) 2002-11-08 2011-06-14 Takeda Pharmaceutical Company Limited Receptor function regulator
EP1581509B1 (en) 2002-12-20 2011-01-19 Merck Sharp & Dohme Corp. 1-(amino)indanes as edg receptor agonists
MXPA05008531A (es) 2003-02-11 2005-11-17 Irm Llc Compuestos biciclicos novedosos y composiciones.
WO2004074297A1 (ja) 2003-02-18 2004-09-02 Kyorin Pharmaceutical Co., Ltd. アミノホスホン酸誘導体とその付加塩及びs1p受容体調節剤
EP1628970A2 (en) 2003-04-30 2006-03-01 The Institutes of Pharmaceutical Discovery, LLC Heterocycle substituted carboxylic acids as inhibitors of protein tyrosine phosphatase-1b
EP1622866B1 (en) 2003-04-30 2012-07-25 Novartis AG Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators
CN1777575B (zh) 2003-04-30 2010-05-12 诺瓦提斯公司 作为1-磷酸-鞘氨醇受体调节剂的氨基-丙醇衍生物
WO2004103279A2 (en) 2003-05-15 2004-12-02 Merck & Co., Inc. 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists
WO2004104205A2 (en) 2003-05-16 2004-12-02 Merck & Co., Inc. Enzymatic preparation of chiral indole esters
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
WO2004113330A1 (en) 2003-05-19 2004-12-29 Irm Llc Immunosuppressant compounds and compositions
ATE537825T1 (de) 2003-05-19 2012-01-15 Irm Llc Immunosuppressive verbindungen und zusammensetzungen
AU2004251146A1 (en) 2003-05-19 2005-01-06 Irm, Llc Immunosuppressant compounds and compositions
GB0313612D0 (en) 2003-06-12 2003-07-16 Novartis Ag Organic compounds
WO2005012221A1 (ja) 2003-08-04 2005-02-10 Ono Pharmaceutical Co., Ltd. ジフェニルエーテル化合物、その製造方法および用途
MXPA06002349A (es) 2003-08-28 2006-05-22 Novartis Ag Derivados de aminopropanol.
ES2754221T3 (es) 2003-08-29 2020-04-16 Ono Pharmaceutical Co Compuesto capaz de unirse al receptor de S1P y uso farmacéutico del mismo
US7825109B2 (en) 2003-08-29 2010-11-02 Ono Pharmaceutical Co., Ltd. Compound capable of binding S1P receptor and pharmaceutical use thereof
JPWO2005023771A1 (ja) 2003-09-05 2006-11-02 小野薬品工業株式会社 ケモカインレセプターアンタゴニストおよびその医薬用途
EP1670463A2 (en) 2003-10-01 2006-06-21 Merck & Co., Inc. 3,5-aryl, heteroaryl or cycloalkyl substituted-1,2,4-oxadiazoles as s1p receptor agonists
US7638637B2 (en) 2003-11-03 2009-12-29 University Of Virginia Patent Foundation Orally available sphingosine 1-phosphate receptor agonists and antagonists
WO2005044780A1 (ja) 2003-11-10 2005-05-19 Kyorin Pharmaceutical Co., Ltd. アミノカルボン酸誘導体とその付加塩及びs1p受容体調節剤
CN1894225A (zh) 2003-12-17 2007-01-10 默克公司 作为鞘氨醇1-磷酸(内皮分化基因)受体激动剂的(3,4-二取代)丙酸酯
US7875745B2 (en) 2003-12-19 2011-01-25 Ono Pharmaceutical Co., Ltd. Compounds having lysophosphatidic acid receptor antagonism and uses thereof
GB0329498D0 (en) 2003-12-19 2004-01-28 Novartis Ag Organic compounds
GB0401332D0 (en) 2004-01-21 2004-02-25 Novartis Ag Organic compounds
CN1921847B (zh) 2004-02-24 2010-06-16 三共株式会社 氨基醇化合物
WO2005082841A1 (en) 2004-02-24 2005-09-09 Irm Llc Immunosuppressant compounds and compositions
TW200538433A (en) 2004-02-24 2005-12-01 Irm Llc Immunosuppressant compounds and compositiions
CN1934094A (zh) 2004-03-05 2007-03-21 万有制药株式会社 二芳基取代杂环5元环衍生物
GB0405289D0 (en) 2004-03-09 2004-04-21 Novartis Ag Organic compounds
TWI344954B (en) 2004-04-02 2011-07-11 Merck Sharp & Dohme Asymmetric hydrogenation process
WO2005123677A1 (en) 2004-06-16 2005-12-29 Actelion Pharmaceuticals Ltd 4-carbonyl substituted 1,1,2-trimethyl-1a,4,5,5a-tetrahydro-1h-4-aza-cyclopropa'a!pentalene derivatives as agonists for the g-protein-coupled receptor s1p1/edg1 and immunosuppressive agents
WO2006001463A1 (ja) 2004-06-23 2006-01-05 Ono Pharmaceutical Co., Ltd. S1p受容体結合能を有する化合物およびその用途
AU2005264431B2 (en) 2004-07-16 2010-08-19 Kyorin Pharmaceutical Co., Ltd. Method of effectively using medicine and method concerning prevention of side effect
JP2007284350A (ja) 2004-07-27 2007-11-01 Takeda Chem Ind Ltd 糖尿病治療剤
TW200611687A (en) 2004-07-29 2006-04-16 Sankyo Co Pharmaceutical compositions used for immunosuppressant
WO2006010379A1 (en) 2004-07-29 2006-02-02 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives as immunosuppressive agents
JP4993407B2 (ja) 2004-08-04 2012-08-08 大正製薬株式会社 トリアゾール誘導体
US20060223866A1 (en) 2004-08-13 2006-10-05 Praecis Pharmaceuticals, Inc. Methods and compositions for modulating sphingosine-1-phosphate (S1P) receptor activity
BRPI0514316A (pt) 2004-08-13 2008-06-10 Praecis Pharm Inc métodos e composições para modulação de atividade de receptor de esfingosina-1-fosfato (s1p)
BRPI0515596A (pt) 2004-09-23 2008-07-29 Wyeth Corp composição farmacêutica usada para o tratamento e/ou prevenção de hcv, e, métodos de inibir rna polimerase ns5b de hepatite c de tratar ou prevenir infecção por hepatite c em um mamìfero
CA2583947A1 (en) 2004-10-12 2006-04-20 Forbes Medi-Tech (Research) Inc. Compounds and methods of treating insulin resistance and cardiomyopathy
CN101043887A (zh) 2004-10-22 2007-09-26 默克公司 用作s1p受体激动剂的2-(芳基)氮杂环甲基羧酸酯、磺酸酯、膦酸酯、次膦酸酯和杂环化合物
SI1650186T1 (sl) 2004-10-22 2008-12-31 Bioprojet Soc Civ Novi derivati dikarboksilne kisline
WO2006055708A2 (en) 2004-11-18 2006-05-26 The Institutes For Pharmaceutical Discovery, Llc Heterocycle substituted carboxylic acids for the treatment of diabetes
US20080051418A1 (en) 2004-11-26 2008-02-28 Tsuyoshi Maekawa Arylalkanoic Acid Derivative
US7888527B2 (en) 2004-12-06 2011-02-15 University Of Virginia Patent Foundation Aryl amide sphingosine 1-phosphate analogs
EP2371811B1 (en) 2004-12-13 2014-10-08 Ono Pharmaceutical Co., Ltd. Azetidinecarboxylic acid derivative and medicinal use thereof
WO2006079406A1 (en) 2005-01-25 2006-08-03 Merck Patent Gmbh Mesogenic compounds, liquid crystal medium and liquid crystal display
JP2008530135A (ja) 2005-02-14 2008-08-07 ユニバーシティ オブ バージニア パテント ファンデーション アミノ基およびフェニル基で置換されたシクロアルカンならびに5員の複素環を含むスフィンゴシン=1−リン酸アゴニスト
DE602006003642D1 (en) 2005-03-23 2008-12-24 Actelion Pharmaceuticals Ltd Neue thiophen-derivate als sphingosin-1-phosphat-1-rezeptorantagonisten
HRP20110613T1 (hr) 2005-03-23 2011-09-30 Actelion Pharmaceuticals Ltd. Hidrogenizirani derivati benzo[c] tiofena kao imunomodulatori
CN101180050B (zh) 2005-03-23 2011-07-27 埃科特莱茵药品有限公司 作为鞘氨醇-1-磷酸盐-1受体激动剂的新颖噻吩衍生物
BRPI0612028A2 (pt) 2005-06-08 2010-10-13 Novartis Ag oxadiazóis ou isodiazóis policìclicos e uso dos mesmos como ligantes de receptor s1p
TWI418350B (zh) 2005-06-24 2013-12-11 Sankyo Co 含有ppar調節劑之醫藥組成物的用途
US7951794B2 (en) 2005-06-24 2011-05-31 Actelion Pharmaceuticals Ltd. Thiophene derivatives
US20070060573A1 (en) 2005-08-10 2007-03-15 Lars Wortmann Acyltryptophanols
RU2008110949A (ru) 2005-08-23 2009-09-27 Айрм Ллк (Bm) Соединения и композиции-иммуносупрессанты
WO2007037196A1 (ja) 2005-09-29 2007-04-05 Yamamoto Chemicals, Inc. インドリン系化合物及びその製造方法
CA2630714C (en) 2005-11-23 2014-01-14 Epix Delaware, Inc. S1p receptor modulating compounds and use thereof
AR057894A1 (es) 2005-11-23 2007-12-26 Actelion Pharmaceuticals Ltd Derivados de tiofeno
TWI404706B (zh) 2006-01-11 2013-08-11 Actelion Pharmaceuticals Ltd 新穎噻吩衍生物
TW200736234A (en) 2006-01-17 2007-10-01 Astrazeneca Ab Chemical compounds
KR20080092385A (ko) 2006-01-24 2008-10-15 액테리온 파마슈티칼 리미티드 신규한 피리딘 유도체
GB0601744D0 (en) 2006-01-27 2006-03-08 Novartis Ag Organic compounds
TWI389683B (zh) 2006-02-06 2013-03-21 Kyorin Seiyaku Kk A therapeutic agent for an inflammatory bowel disease or an inflammatory bowel disease treatment using a 2-amino-1,3-propanediol derivative as an active ingredient
TW200806611A (en) 2006-02-09 2008-02-01 Daiichi Seiyaku Co Novel amidopropionic acid derivatives and medicine containing the same
JP2009526073A (ja) 2006-02-09 2009-07-16 ユニバーシティ オブ バージニア パテント ファンデーション 二環式スフィンゴシン−1−リン酸受容体アナログ
US20070191371A1 (en) 2006-02-14 2007-08-16 Kalypsys, Inc. Heterocyclic modulators of ppar
EP1984334B1 (en) 2006-02-15 2014-04-09 Allergan, Inc. Indole-3-carboxylic acid amide, ester, thioamide and thiol ester compounds bearing aryl or heteroaryl groups having sphingosine-1-phosphate (s1p) receptor antagonist biological activity
CN101460458A (zh) 2006-02-15 2009-06-17 阿勒根公司 具有1-磷酸-鞘氨醇(s1p)受体拮抗剂生物活性的带芳基或者杂芳基基团的吲哚-3-羧酸的酰胺、酯、硫代酰胺和硫羟酸酯化合物
JP2009527501A (ja) 2006-02-21 2009-07-30 ユニバーシティ オブ バージニア パテント ファンデーション S1p受容体アゴニストとしてのフェニル−シクロアルキル誘導体およびフェニル−複素環誘導体
US7649098B2 (en) 2006-02-24 2010-01-19 Lexicon Pharmaceuticals, Inc. Imidazole-based compounds, compositions comprising them and methods of their use
WO2007106469A2 (en) 2006-03-14 2007-09-20 Amgen Inc. Bicyclic carboxylic acid derivatives useful for treating metabolic disorders
CA2646469A1 (en) 2006-03-21 2007-09-27 Epix Delaware, Inc. S1p receptor modulating compounds
JP2007262009A (ja) 2006-03-29 2007-10-11 Dai Ichi Seiyaku Co Ltd ヘテロアリール低級カルボン酸誘導体
AU2007236707C1 (en) 2006-04-03 2012-05-24 Astellas Pharma Inc. Hetero compound
GB0607389D0 (en) 2006-04-12 2006-05-24 Novartis Ag Organic compounds
WO2007129473A1 (ja) 2006-05-09 2007-11-15 Daiichi Sankyo Company, Limited 二環性アリール誘導体
EP2258700A1 (en) 2006-05-09 2010-12-08 Pfizer Products Inc. Cycloalkylamino acid derivatives and pharmaceutical compositions thereof
JPWO2007129745A1 (ja) 2006-05-09 2009-09-17 第一三共株式会社 ヘテロアリールアミド低級カルボン酸誘導体
EP2046766A1 (en) 2006-08-01 2009-04-15 Praecis Pharmaceuticals Incorporated Agonists of the sphingosine- 1- phosphate receptor (slp)
TW200823182A (en) 2006-08-01 2008-06-01 Praecis Pharm Inc Chemical compounds
EP2099768A2 (en) 2006-08-04 2009-09-16 Praecis Pharmaceuticals Incorporated Agonists of the sphingosine-1-phosphate receptor
NZ574011A (en) 2006-08-08 2011-10-28 Kyorin Seiyaku Kk Aminophosphoric acid ester derivative and s1p receptor modulator containing the same as active ingredient
WO2008024196A1 (en) 2006-08-24 2008-02-28 Praecis Pharmaceuticals Incorporated Chemical compounds
JP2009269819A (ja) 2006-08-25 2009-11-19 Asahi Kasei Pharma Kk アミン化合物
BRPI0716815A2 (pt) 2006-09-07 2013-11-05 Allergan Inc Co posto heteroatomáticos tendo atividade biológia agonista e/ou antagonista de receptor de esfinfosina-1-fosfato (s1p)
TWI408139B (zh) 2006-09-07 2013-09-11 Actelion Pharmaceuticals Ltd 新穎噻吩衍生物
MY149853A (en) 2006-09-07 2013-10-31 Actelion Pharmaceuticals Ltd Pyridin-4-yl derivatives as immunomodulating agents
AU2007293653B2 (en) 2006-09-08 2011-02-17 Novartis Ag N-biaryl (hetero) arylsulphonamide derivatives useful in the treatment of diseases mediated by lymphocytes interactions
JP5250556B2 (ja) 2006-09-21 2013-07-31 アクテリオン ファーマシューティカルズ リミテッド フェニル誘導体及びそれらの免疫調節薬としての使用
AU2007334436A1 (en) 2006-12-15 2008-06-26 Abbott Laboratories Novel oxadiazole compounds
AU2007338700A1 (en) 2006-12-21 2008-07-03 Abbott Laboratories Sphingosine-1 -phosphate receptor agonist and antagonist compounds
GB0625648D0 (en) 2006-12-21 2007-01-31 Glaxo Group Ltd Compounds
JO2701B1 (en) 2006-12-21 2013-03-03 جلاكسو جروب ليميتد Vehicles
AU2008206495A1 (en) 2007-01-11 2008-07-24 Allergan, Inc. 6-substituted indole-3-carboxylic acid amide compounds having Sphingosine-1-Phosphate (S1P) receptor antagonist biological activity
WO2008091967A1 (en) 2007-01-26 2008-07-31 Smithkline Beecham Corporation Chemical compounds
WO2008097819A2 (en) 2007-02-05 2008-08-14 Smithkline Beecham Corporation Chemical compounds
DK2125797T3 (da) 2007-03-16 2014-02-10 Actelion Pharmaceuticals Ltd Aminopyridinderivater som s1p1/edg1-receptoragonister
CA2679980A1 (en) 2007-03-21 2007-09-27 Epix Pharmaceuticals, Inc. S1p receptor modulating compounds and use thereof
US8324254B2 (en) 2007-04-19 2012-12-04 Glaxo Group Limited Oxadiazole substituted indazole derivatives for use as sphingosine 1-phosphate (S1P) agonists
EP2014653A1 (en) 2007-06-15 2009-01-14 Bioprojet Novel dicarboxylic acid derivatives as S1P1 receptor agonists
WO2009011850A2 (en) 2007-07-16 2009-01-22 Abbott Laboratories Novel therapeutic compounds
WO2009019506A1 (en) 2007-08-03 2009-02-12 Astrazeneca Ab Heterocyclyc sulfonamides having edg-1 antagonistic activity
BRPI0814975A2 (pt) 2007-08-08 2015-02-03 Merck Serono Sa Derivados de 6-amino-pirimidina-4-carboxamida e compostos relacionados que se ligam ao receptor de 1-fosfato de esfingosina (s1p) para o tratamento de esclerose múltipla
TW200930368A (en) 2007-11-15 2009-07-16 Astrazeneca Ab Bis-(sulfonylamino) derivatives in therapy
JP2011506600A (ja) 2007-12-18 2011-03-03 アリーナ ファーマシューティカルズ, インコーポレイテッド 自己免疫性障害および炎症性障害の治療において有用なテトラヒドロシクロペンタ[b]インドール−3−イルカルボン酸誘導体
AR070398A1 (es) 2008-02-22 2010-03-31 Gruenenthal Chemie Derivados sustituidos de indol
PL2291080T3 (pl) 2008-05-14 2015-12-31 Scripps Research Inst Nowe modulatory receptorów sfingozyno-1-fosforanu
WO2009151626A1 (en) 2008-06-13 2009-12-17 Arena Pharmaceuticals, Inc. Substituted (1, 2, 4-0xadiaz0l-3-yl) indolin-1-yl carboxylic acid derivatives useful as s1p1 agonists
WO2009151621A1 (en) 2008-06-13 2009-12-17 Arena Pharmaceuticals, Inc. Substituted (1, 2, 4-0xadiaz0l-3-yl) indolin-1-yl carboxylic acid derivatives useful as s1p1 agonists
US8580841B2 (en) 2008-07-23 2013-11-12 Arena Pharmaceuticals, Inc. Substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives useful in the treatment of autoimmune and inflammatory disorders
PE20120578A1 (es) 2009-02-10 2012-06-17 Abbott Lab Agonistas y antagonistas del receptor de s1p5, y metodos de uso de los mismos
WO2011005290A1 (en) 2009-06-23 2011-01-13 Arena Pharmaceuticals, Inc. Disubstituted oxadiazole derivatives useful in the treatment of autoimmune and inflammatory disorders
ES2759949T3 (es) 2009-10-29 2020-05-12 Bristol Myers Squibb Co Compuestos heterocíclicos tricíclicos
SG182610A1 (en) 2010-01-27 2012-08-30 Arena Pharm Inc Processes 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
CA2789480A1 (en) * 2010-03-03 2011-09-09 Arena Pharmaceuticals, Inc. Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof
JP2013533286A (ja) 2010-07-30 2013-08-22 セントルイス ユニバーシティ 疼痛を治療する方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011510073A (ja) * 2008-01-25 2011-03-31 アリーナ ファーマシューティカルズ, インコーポレイテッド S1P1アゴニストとして作用するジヒドロ−1H−ピロロ[1,2−a]インドール−1−イルカルボン酸誘導体
JP2012501327A (ja) * 2008-08-27 2012-01-19 アリーナ ファーマシューティカルズ, インコーポレイテッド 自己免疫障害および免疫性障害の治療において有用なs1p1受容体のアゴニストとしての置換三環式酸誘導体
WO2010064707A1 (ja) * 2008-12-05 2010-06-10 アステラス製薬株式会社 2h-クロメン化合物及びその誘導体
WO2011005295A1 (en) * 2009-06-24 2011-01-13 Arena Pharmaceuticals, Inc. Modulators of the sphingosine-1-phosphate (s1p) receptor useful for the treatment of disorders related thereto

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017533954A (ja) * 2014-10-27 2017-11-16 セリックス バイオ プライヴェート リミテッドCellix Bio Private Limited 多発性硬化症の治療のための、フマル酸モノメチルエステルとピペラジン又はエチレンジアミンとの3つの成分の塩

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