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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Abandoned
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JP2012556199A
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JP2013521301A5 (enExample
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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
Abandoned legal-status Critical Current

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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • 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
    • A61P25/00—Drugs for disorders of the nervous 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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

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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)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Transplantation (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • 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

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JP2013521301A true JP2013521301A (ja) 2013-06-10
JP2013521301A5 JP2013521301A5 (enExample) 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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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

Country Status (8)

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US (2) US9085581B2 (enExample)
EP (1) EP2542554B1 (enExample)
JP (2) JP2013521301A (enExample)
CN (2) CN105503882B (enExample)
CA (1) CA2789480A1 (enExample)
ES (1) ES2558087T3 (enExample)
SG (2) SG10201501575VA (enExample)
WO (1) WO2011109471A1 (enExample)

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
HRP20161133T1 (hr) 2008-07-23 2016-12-02 Arena Pharmaceuticals, Inc. DERIVATI SUSPSTITUIRANE 1,2,3,4-TETRAHIDROCIKLOPENTA[b]INDOL-3-IL-OCTENE KISELINE KORISNI U LIJEČENJU AUTOIMUNIH I UPALNIH POREMEĆAJA
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
CA2786994C (en) 2010-01-27 2018-01-16 Arena Pharmaceuticals, 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
CN105503882B (zh) * 2010-03-03 2019-07-05 艾尼纳制药公司 制备s1p1受体调节剂及其晶体形式的方法
AU2016205361C1 (en) 2015-01-06 2021-04-08 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
PL3310760T3 (pl) 2015-06-22 2023-03-06 Arena Pharmaceuticals, Inc. Krystaliczna sól L-argininy kwasu (R)-2-(7-(4-cyklopentylo-3-(trifluorometylo)benzyloksy)- 1,2,3,4-tetrahydrocyklo-penta[b]indol-3-ilo)octowego do zastosowania w zaburzeniach związanych z receptorem S1P1
KR20190116416A (ko) 2017-02-16 2019-10-14 아레나 파마슈티칼스, 인크. 원발 담즙성 담관염을 치료하기 위한 화합물 및 방법
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
AU2019280822A1 (en) 2018-06-06 2021-01-07 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the S1P1 receptor
EP3847158A1 (en) 2018-09-06 2021-07-14 Arena Pharmaceuticals, Inc. Compounds useful in the treatment of autoimmune and inflammatory disorders
CA3117695A1 (en) * 2018-10-26 2020-04-30 Keros Therapeutics, Inc. Crystal forms of an alk2 inhibitor

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 (145)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL293572A (enExample) * 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
IL145922A0 (en) 1999-04-28 2002-07-25 Aventis Pharma Gmbh Di-aryl acid derivatives as ppar receptor ligands
US6410583B1 (en) 2000-07-25 2002-06-25 Merck Frosst Canada & Co. Cyclopentanoindoles, compositions containing such compounds and methods of treatment
WO2002039987A2 (en) 2000-11-14 2002-05-23 Neurosearch A/S Use of malaria parasite anion channel blockers for treating malaria
EP1383778B1 (en) 2001-01-30 2009-10-21 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
US7179817B2 (en) 2001-05-10 2007-02-20 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
ATE441654T1 (de) 2002-01-18 2009-09-15 Merck & Co Inc Edg-rezeptoragonisten
US20050070506A1 (en) 2002-01-18 2005-03-31 Doherty George A. Selective s1p1/edg1 receptor agonists
JP2005516967A (ja) 2002-01-18 2005-06-09 ザ ジェネティクス カンパニー インコーポレーティッド β−セクレターゼインヒビター
JP2005531506A (ja) 2002-03-01 2005-10-20 メルク　エンド　カムパニー　インコーポレーテッド Ｅｄｇ受容体作動薬としてのアミノアルキルホスホネートおよび関連化合物
EP1482896A4 (en) 2002-03-01 2005-11-23 Merck & Co Inc AMINO ALKYL PHOSPHONATES 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
AU2003252478A1 (en) 2002-07-10 2004-02-02 Ono Pharmaceutical Co., Ltd. Ccr4 antagonist and medicinal use thereof
US7241790B2 (en) 2002-07-30 2007-07-10 University Of Virginia Patent Foundation Compounds active in spinigosine 1-phosphate signaling
EP1559422B1 (en) 2002-11-08 2014-04-30 Takeda Pharmaceutical Company Limited Receptor function controlling agent
JP4516430B2 (ja) 2002-12-20 2010-08-04 メルク・シャープ・エンド・ドーム・コーポレイション １−（アミノ）インダン並びに（１，２−ジヒドロ−３−アミノ）−ベンゾフラン、ベンゾチオフェン及びインドール
JP4505449B2 (ja) 2003-02-11 2010-07-21 アイアールエム・リミテッド・ライアビリティ・カンパニー 新規二環式化合物および組成物
DK1602660T3 (da) 2003-02-18 2011-05-23 Kyorin Seiyaku Kk Aminophosphonsyrederivater, additionssalte deraf og S1P-receptormodulatorer
ATE547395T1 (de) 2003-04-30 2012-03-15 Novartis Pharma Gmbh Aminopropanol-derivate als modulatoren des sphingosin-1-phosphat-rezeptors
JP2006525366A (ja) 2003-04-30 2006-11-09 ジ インスチチュート フォー ファーマシューティカル ディスカバリー、エルエルシー 複素環式カルボン酸置換基
ES2392167T3 (es) 2003-04-30 2012-12-05 Novartis Ag Derivados aminopropanol como moduladores del receptor esfingosina-1-fosfato
CA2524867A1 (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
CN1787817B (zh) 2003-05-19 2011-09-07 Irm责任有限公司 免疫抑制剂化合物及组合物
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
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.
US7825109B2 (en) 2003-08-29 2010-11-02 Ono Pharmaceutical Co., Ltd. Compound capable of binding S1P receptor and pharmaceutical use thereof
US7732442B2 (en) 2003-09-05 2010-06-08 Ono Pharmaceutical Co., Ltd. Chemokine receptor antagonist and medical use thereof
CN1859908A (zh) 2003-10-01 2006-11-08 默克公司 作为s1p受体激动剂的3,5－芳基、杂芳基或环烷基取代的－1,2,4－噁二唑类化合物
WO2005041899A2 (en) 2003-11-03 2005-05-12 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
AU2004299456B2 (en) 2003-12-17 2010-10-07 Merck Sharp & Dohme Corp. (3,4-disubstituted)propanoic carboxylates as S1P (Edg) receptor agonists
JP4766384B2 (ja) 2003-12-19 2011-09-07 小野薬品工業株式会社 リゾホスファチジン酸受容体拮抗作用を有する化合物およびその用途
GB0329498D0 (en) 2003-12-19 2004-01-28 Novartis Ag Organic compounds
GB0401332D0 (en) 2004-01-21 2004-02-25 Novartis Ag Organic compounds
TW200538433A (en) 2004-02-24 2005-12-01 Irm Llc Immunosuppressant compounds and compositiions
TWI355934B (en) 2004-02-24 2012-01-11 Sankyo Co Pharmaceutical composition for treatment or prophy
US7718704B2 (en) 2004-02-24 2010-05-18 Irm Llc Immunosuppressant compounds and compositions
EP1726585A4 (en) 2004-03-05 2009-07-15 Banyu Pharma Co Ltd DIARYLSUBSTITUTED FIVE-GLOSS HETEROCYCLUS DERIVAT
GB0405289D0 (en) 2004-03-09 2004-04-21 Novartis Ag Organic compounds
CA2561632A1 (en) 2004-04-02 2005-10-20 Merck & Co., Inc. Asymmetric hydrogenation process useful for the preparation of cycloalkanoindole derivatives
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
JP5315611B2 (ja) 2004-06-23 2013-10-16 小野薬品工業株式会社 Ｓ１ｐ受容体結合能を有する化合物およびその用途
ATE502630T1 (de) 2004-07-16 2011-04-15 Kyorin Seiyaku Kk Verfahren zur effektiven anwendung eines medikaments und verfahren zur prävention von nebenwirkungen
JP2007284350A (ja) 2004-07-27 2007-11-01 Takeda Chem Ind Ltd 糖尿病治療剤
WO2006010379A1 (en) 2004-07-29 2006-02-02 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives as immunosuppressive agents
TW200611687A (en) 2004-07-29 2006-04-16 Sankyo Co Pharmaceutical compositions used for immunosuppressant
RU2383536C2 (ru) 2004-08-04 2010-03-10 Тайсо Фармасьютикал Ко., Лтд. Производное триазола
US20060223866A1 (en) 2004-08-13 2006-10-05 Praecis Pharmaceuticals, Inc. Methods and compositions for modulating sphingosine-1-phosphate (S1P) receptor activity
AU2005272619A1 (en) 2004-08-13 2006-02-23 Praecis Pharmaceuticals, Inc. Methods and compositions for modulating sphingosine-1-phosphate (SIP) receptor activity
US7250441B2 (en) 2004-09-23 2007-07-31 Wyeth Carbazole and cyclopentaindole derivatives to treat infection with Hepatitis C virus
CA2583947A1 (en) 2004-10-12 2006-04-20 Forbes Medi-Tech (Research) Inc. Compounds and methods of treating insulin resistance and cardiomyopathy
EP1650186B1 (en) 2004-10-22 2008-06-04 Bioprojet Novel dicarboxylic acid derivatives
JP2008517915A (ja) 2004-10-22 2008-05-29 メルク エンド カムパニー インコーポレーテッド Ｓ１ｐ受容体アゴニストとしての２−（アリール）アザシクリルメチルカルボキシレート、スルホネート、ホスホネート、ホスフィネート及びヘテロ環
AU2005307718A1 (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
JP2008522977A (ja) 2004-12-06 2008-07-03 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 スフィンゴシン＝１−リン酸のアリールアミドアナログ
JP4318087B2 (ja) 2004-12-13 2009-08-19 小野薬品工業株式会社 アミノカルボン酸誘導体およびその医薬用途
WO2006079406A1 (en) 2005-01-25 2006-08-03 Merck Patent Gmbh Mesogenic compounds, liquid crystal medium and liquid crystal display
MX2007009848A (es) 2005-02-14 2008-03-10 Univ Virginia Agonistas de esfingosina 1-fosfato comprendiendo cicloalcanos y heterociclos de 5 miembros substituidos por grupos amino y fenilo.
AU2006226018B2 (en) 2005-03-23 2012-07-12 Idorsia Pharmaceuticals Ltd Hydrogenated benzo (C) thiophene derivatives as immunomodulators
KR20080002850A (ko) 2005-03-23 2008-01-04 액테리온 파마슈티칼 리미티드 신규한 티오펜 유도체
BRPI0609668A2 (pt) 2005-03-23 2011-10-18 Actelion Pharmaceuticals Ltd composto, composição farmacêutica, e, uso de um composto
JP2008545767A (ja) 2005-06-08 2008-12-18 ノバルティス アクチエンゲゼルシャフト 多環式オキサジアゾールまたはイソキサゾールおよびｓｉｐ受容体リガンドとしてのそれらの使用
AU2006260573A1 (en) 2005-06-24 2006-12-28 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives
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
US20070060573A1 (en) 2005-08-10 2007-03-15 Lars Wortmann Acyltryptophanols
JP2009506046A (ja) 2005-08-23 2009-02-12 アイアールエム・リミテッド・ライアビリティ・カンパニー 免疫抑制剤化合物および組成物
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
AU2006317689B2 (en) 2005-11-23 2013-07-25 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
AU2007212193A1 (en) 2006-02-09 2007-08-16 University Of Virginia Patent Foundation Bicyclic sphingosine 1-phosphate analogs
US20070191371A1 (en) 2006-02-14 2007-08-16 Kalypsys, Inc. Heterocyclic modulators of ppar
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
CA2642668C (en) 2006-02-15 2013-01-08 Allergan, Inc. Indole-3-carboxylic acid amide and ester compounds bearing phenyl groups having sphingosine-1-phosphate (s1p) receptor antagonist biological activity
BRPI0707957A2 (pt) 2006-02-21 2011-05-17 Univ Virginia Patent Found composto, e, método para prevenção ou tratamento de uma condição ou sintoma patológico em um mamìfero
US7649098B2 (en) 2006-02-24 2010-01-19 Lexicon Pharmaceuticals, Inc. Imidazole-based compounds, compositions comprising them and methods of their use
CA2646430A1 (en) 2006-03-14 2007-09-20 Amgen Inc. Bicyclic carboxylic acid derivatives useful for treating metabolic disorders
US7790707B2 (en) 2006-03-21 2010-09-07 Epix Pharmaceuticals Inc. S1P receptor modulating compounds and use thereof
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
MX2008012738A (es) 2006-04-03 2009-02-06 Astellas Pharma Inc Heterocompuesto.
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
MX2008013990A (es) 2006-05-09 2009-01-29 Pfizer Prod Inc Derivados de cicloalquilamino acidos.
EP2017263A4 (en) 2006-05-09 2011-11-30 Daiichi Sankyo Co Ltd Heteroarylamide derivative of a lower carboxylic acid
AR062156A1 (es) 2006-08-01 2008-10-22 Praecis Pharm Inc Compuestos agonistas y selectivos del receptor s1p-1
US20080070866A1 (en) 2006-08-01 2008-03-20 Praecis Pharmaceuticals Incorporated Chemical compounds
EP2099768A2 (en) 2006-08-04 2009-09-16 Praecis Pharmaceuticals Incorporated Agonists of the sphingosine-1-phosphate receptor
US8232319B2 (en) 2006-08-08 2012-07-31 Kyorin Pharmaceutical Co., Ltd. Amino phosphate derivative and S1P receptor modulator having same as an active ingredient
EP2054377A1 (en) 2006-08-24 2009-05-06 Praecis Pharmaceuticals Incorporated Chemical compounds
JP2009269819A (ja) 2006-08-25 2009-11-19 Asahi Kasei Pharma Kk アミン化合物
AR061841A1 (es) 2006-09-07 2008-09-24 Actelion Pharmaceuticals Ltd Derivados de tiofen-oxadiazoles, agonistas del receptor s1p1/edg1, composiciones farmaceuticas que los contienen y usos como agentes inmunomoduladores.
CA2662852A1 (en) 2006-09-07 2008-03-13 Allergan, Inc. Heteroaromatic compounds having sphingosine-1-phosphate (s1p) receptor agonist and/or antagonist biological activity
CL2007002593A1 (es) 2006-09-07 2008-06-13 Actelion Pharmaceuticals Ltd Compuestos derivados de 4-heteroaril-piridina; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como rechazo de organos transplantados, sindromes autoinmunes y cancer.
CA2662091A1 (en) 2006-09-08 2008-03-13 Novartis Ag N-biaryl (hetero) arylsulphonamide derivatives useful in the treatment of diseases mediated by lymphocytes interactions
EP2069318B1 (en) 2006-09-21 2012-09-12 Actelion Pharmaceuticals Ltd. Phenyl derivatives and their use as immunomodulators
CN101562977A (zh) 2006-12-15 2009-10-21 艾博特公司 新的二唑化合物
CA2672727A1 (en) 2006-12-21 2008-07-03 Abbott Laboratories Sphingosine-1-phosphate receptor agonist and antagonist compounds
JO2701B1 (en) * 2006-12-21 2013-03-03 جلاكسو جروب ليميتد Vehicles
GB0625648D0 (en) 2006-12-21 2007-01-31 Glaxo Group Ltd Compounds
JP2010515750A (ja) 2007-01-11 2010-05-13 アラーガン インコーポレイテッド スフィンゴシン−１−ホスフェート（ｓ１ｐ）受容体アンタゴニスト生物活性を有する６−置換インドール−３−カルボン酸アミド化合物
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
JP2010521450A (ja) 2007-03-16 2010-06-24 アクテリオン ファーマシューティカルズ リミテッド Ｓ１ｐ１／ｅｄｇ１受容体アゴニストとしてのアミノ−ピリジン誘導体
JP5191497B2 (ja) 2007-03-21 2013-05-08 エピックス ファーマシューティカルズ，インコーポレイテッド Ｓ１ｐ受容体調節化合物およびその使用
CL2008001099A1 (es) 2007-04-19 2008-10-24 Glaxo Group Ltd Compuestos derivados de indazol; y su uso para tratar enfermedades mediadas por los receptores s1p1, tales como esclerosis multiple, enfermedad autoinmune, trastornos inflamatorios, diabetes, entre otras.
EP2014653A1 (en) 2007-06-15 2009-01-14 Bioprojet Novel dicarboxylic acid derivatives as S1P1 receptor agonists
US20090069288A1 (en) 2007-07-16 2009-03-12 Breinlinger Eric C 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
UY31468A1 (es) 2007-11-15 2009-07-17 Derivados bis-(sulfonilamino) en terapia 065
AU2008338965A1 (en) 2007-12-18 2009-06-25 Arena Pharmaceuticals, Inc. Tetrahydrocyclopenta[b]indol-3-yl carboxylic acid derivatives useful in the treatment of autoimmune and inflammatory disorders
AR070398A1 (es) 2008-02-22 2010-03-31 Gruenenthal Chemie Derivados sustituidos de indol
HUE025984T2 (hu) 2008-05-14 2016-05-30 Scripps Research Inst Szfingozin foszfát receptor új modulátorai
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
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
HRP20161133T1 (hr) 2008-07-23 2016-12-02 Arena Pharmaceuticals, Inc. DERIVATI SUSPSTITUIRANE 1,2,3,4-TETRAHIDROCIKLOPENTA[b]INDOL-3-IL-OCTENE KISELINE KORISNI U LIJEČENJU AUTOIMUNIH I UPALNIH POREMEĆAJA
AU2010213794A1 (en) 2009-02-10 2011-09-01 Abbott Laboratories Agonists and antagonists of the S1P5 receptor, and methods of uses thereof
WO2011005290A1 (en) 2009-06-23 2011-01-13 Arena Pharmaceuticals, Inc. Disubstituted oxadiazole derivatives useful in the treatment of autoimmune and inflammatory disorders
CN102686571B (zh) 2009-10-29 2015-11-25 百时美施贵宝公司 三环杂环化合物
CA2786994C (en) 2010-01-27 2018-01-16 Arena Pharmaceuticals, 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
CN105503882B (zh) * 2010-03-03 2019-07-05 艾尼纳制药公司 制备s1p1受体调节剂及其晶体形式的方法
EP2598126A2 (en) 2010-07-30 2013-06-05 Saint Louis University Methods of treating pain

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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