SG10201501575VA - 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

Info

Publication number
SG10201501575VA
SG10201501575VA SG10201501575VA SG10201501575VA SG10201501575VA SG 10201501575V A SG10201501575V A SG 10201501575VA SG 10201501575V A SG10201501575V A SG 10201501575VA SG 10201501575V A SG10201501575V A SG 10201501575VA SG 10201501575V A SG10201501575V A SG 10201501575VA
Authority
SG
Singapore
Prior art keywords
processes
preparation
crystalline forms
receptor modulators
modulators
Prior art date
Application number
SG10201501575VA
Inventor
Robert M Jones
Daniel J Buzard
Tawfik Gharbaoui
Benjamin R Johnson
Michelle Kasem
Thomas O Schrader
Scott Stirn
Original Assignee
Arena Pharm Inc
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 Arena Pharm Inc filed Critical Arena Pharm Inc
Publication of SG10201501575VA publication Critical patent/SG10201501575VA/en

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Classifications

    • 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
SG10201501575VA 2010-03-03 2011-03-02 Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof SG10201501575VA (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US33936210P 2010-03-03 2010-03-03

Publications (1)

Publication Number Publication Date
SG10201501575VA true SG10201501575VA (en) 2015-04-29

Family

ID=43838192

Family Applications (2)

Application Number Title Priority Date Filing Date
SG2012061685A SG183416A1 (en) 2010-03-03 2011-03-02 Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof
SG10201501575VA SG10201501575VA (en) 2010-03-03 2011-03-02 Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof

Family Applications Before (1)

Application Number Title Priority Date Filing Date
SG2012061685A SG183416A1 (en) 2010-03-03 2011-03-02 Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof

Country Status (9)

Country Link
US (2) US9085581B2 (en)
EP (1) EP2542554B1 (en)
JP (2) JP2013521301A (en)
CN (2) CN102884064B (en)
CA (1) CA2789480A1 (en)
ES (1) ES2558087T3 (en)
HK (1) HK1179627A1 (en)
SG (2) SG183416A1 (en)
WO (1) WO2011109471A1 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE030424T2 (en) 2008-07-23 2017-05-29 Arena Pharm Inc SUBSTITUTED 1,2,3,4- TETRAHYDROCYCLOPENTA[b]INDOL-3-YL) ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
SI2342205T1 (en) * 2008-08-27 2016-09-30 Arena Pharmaceuticals, Inc. Substituted tricyclic acid derivatives as s1p1 receptor agonists useful in the treatment of autoimmune and inflammatory disorders
ES2937386T3 (en) 2010-01-27 2023-03-28 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 of same
WO2011109471A1 (en) 2010-03-03 2011-09-09 Arena Pharmaceuticals, Inc. Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof
CA2965449C (en) * 2014-10-27 2020-11-10 Cellix Bio Private Limited Three component salts of fumaric acid monomethyl ester with piperazine or ethylene diamine for the treatment of multiple sclerosis
EP3242666A1 (en) 2015-01-06 2017-11-15 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
JP6838744B2 (en) 2015-06-22 2021-03-03 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 (R) -2- (7- (4-cyclopentyl-3- (trifluoromethyl) benzyloxy) -1,2,3,4-tetrahydrocyclopenta [b] indole-for use in S1P1 receptor-related disorders Crystalline L-arginine salt of 3-yl) acetic acid (Compound 1)
CN110545848A (en) 2017-02-16 2019-12-06 艾尼纳制药公司 Compounds and methods for treating inflammatory bowel disease with extra-intestinal manifestations
KR20190116416A (en) 2017-02-16 2019-10-14 아레나 파마슈티칼스, 인크. Compounds and Methods for Treating Primary Bile Cholangitis
WO2020051378A1 (en) 2018-09-06 2020-03-12 Arena Pharmaceuticals, Inc. Compounds useful in the treatment of autoimmune and inflammatory disorders

Family Cites Families (149)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL293572A (en) * 1962-06-07
DE2226703A1 (en) 1972-05-25 1973-12-13 Schering Ag NEW TETRAHYDROCARBAZOLE DERIVATIVES AND THE PROCESS FOR THEIR PRODUCTION
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 (en) 1989-10-27 1991-09-13 American Home Prod PROCESS FOR THE PREPARATION OF INDOLE-, INDENO-, PYRANOINDOLE- AND TETRA-HYDROCARBAZOLE-ALCANOIC ACID DERIVATIVES, OR WHICH ARE USEFUL AS PLA2 INHIBITORS AND 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
EP1177187B1 (en) 1999-04-28 2007-07-25 Sanofi-Aventis Deutschland 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
JP2004529100A (en) 2001-01-30 2004-09-24 ユニバーシティ オブ バージニア パテント ファウンデーション Agonists and antagonists of sphingosine-1-phosphate receptor
WO2002079131A1 (en) 2001-03-29 2002-10-10 Kansai Research Institute, Inc. Optically active compound and photosensitive resin composition
ATE416762T1 (en) 2001-05-10 2008-12-15 Ono Pharmaceutical Co CARBOXIC ACID DERIVATIVES AND MEDICINAL PRODUCTS CONTAINING THESE AS ACTIVE INGREDIENTS
MXPA04002679A (en) 2001-09-27 2004-07-30 Kyorin Seiyaku Kk Diaryl sulfide derivative, addition salt thereof, and immunosuppressant.
US7479504B2 (en) 2002-01-18 2009-01-20 Merck & Co., Inc. Edg receptor agonists
EP1469863A2 (en) 2002-01-18 2004-10-27 Merck & Co., Inc. Selective s1p1/edg1 receptor agonists
US20050239899A1 (en) 2002-01-18 2005-10-27 Wolfgang Fecke 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
CA2488117A1 (en) 2002-06-17 2003-12-24 Merck & Co., Inc. 1-((5-aryl-1,2,4-oxadiazol-3-yl)benzyl)azetidine-3-carboxylates and 1-((5-aryl-1,2,4-oxadiazol-3-yl)benzyl)pyrrolidine-3-carboxylates as edg receptor agonists
JPWO2004007472A1 (en) 2002-07-10 2005-11-17 小野薬品工業株式会社 CCR4 antagonist and pharmaceutical use thereof
EP1546110A4 (en) 2002-07-30 2008-03-26 Univ Virginia Compounds active in sphingosine 1-phosphate signaling
AU2003277576A1 (en) 2002-11-08 2004-06-07 Takeda Pharmaceutical Company Limited Receptor function controlling agent
AU2003297232B2 (en) 2002-12-20 2010-02-04 Merck Sharp & Dohme Corp. 1-(amino)indanes and (1,2-dihydro-3-amino)-benzofurans, benzothiophenes and indoles
AU2004210697B2 (en) 2003-02-11 2007-10-18 Irm Llc Novel bicyclic compounds and compositions
KR101005171B1 (en) 2003-02-18 2011-01-04 교린 세이야꾸 가부시키 가이샤 Aminophosphonic acid derivatives, addition salts thereof and s1p receptor modulators
MXPA05011539A (en) 2003-04-30 2006-01-23 Inst For Pharm Discovery Inc Heterocycle substituted carboxylic acids as inhibitors of protein tyrosine phosphatase-1b.
ES2383298T3 (en) 2003-04-30 2012-06-20 Novartis Ag Amino-propanol derivatives as sphingosine-1-phosphate receptor modulators
CA2523677A1 (en) 2003-04-30 2004-11-11 Novartis Ag Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators
US20060252741A1 (en) 2003-05-15 2006-11-09 Colandrea Vincent J 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
JP4728962B2 (en) 2003-05-19 2011-07-20 アイアールエム・リミテッド・ライアビリティ・カンパニー Immunosuppressive compounds and compositions
EP1638551B1 (en) 2003-05-19 2011-12-21 Irm Llc Immunosuppressant compounds and compositions
CA2524048C (en) 2003-05-19 2013-06-25 Irm Llc Immunosuppressant compounds and compositions
GB0313612D0 (en) 2003-06-12 2003-07-16 Novartis Ag Organic compounds
JPWO2005012221A1 (en) 2003-08-04 2006-09-14 小野薬品工業株式会社 Diphenyl ether compound, its production method and use
WO2005021503A1 (en) 2003-08-28 2005-03-10 Novartis Ag Aminopropanol derivatives
CN101407471A (en) 2003-08-29 2009-04-15 小野药品工业株式会社 Compound capable of binding S1P receptor and pharmaceutical use thereof
WO2005023771A1 (en) 2003-09-05 2005-03-17 Ono Pharmaceutical Co., Ltd. Chemokine receptor antagonist and medical use thereof
CN1859908A (en) 2003-10-01 2006-11-08 默克公司 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 (en) 2003-11-10 2005-05-19 Kyorin Pharmaceutical Co., Ltd. Aminocarboxylic acid derivative, addition salt thereof, and s1p receptor control agent
JP4773972B2 (en) 2003-12-17 2011-09-14 メルク・シャープ・エンド・ドーム・コーポレイション (3,4-Disubstituted) propanecarboxylic acids as S1P (Edg) receptor agonists
JP4766384B2 (en) 2003-12-19 2011-09-07 小野薬品工業株式会社 Compound having lysophosphatidic acid receptor antagonistic activity and use 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
TW200538433A (en) 2004-02-24 2005-12-01 Irm Llc Immunosuppressant compounds and compositiions
JP4740884B2 (en) 2004-02-24 2011-08-03 アイアールエム・リミテッド・ライアビリティ・カンパニー Immunosuppressive compounds and compositions
KR20110136901A (en) 2004-02-24 2011-12-21 상꾜 가부시키가이샤 Amino alcohol compound
AU2005219791B2 (en) 2004-03-05 2011-06-09 Msd K.K. Diaryl-substituted five-membered heterocycle derivative
GB0405289D0 (en) 2004-03-09 2004-04-21 Novartis Ag Organic compounds
JP5239071B2 (en) 2004-04-02 2013-07-17 メルク・シャープ・アンド・ドーム・コーポレーション Asymmetric hydrogenation methods 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
EP1760071A4 (en) 2004-06-23 2008-03-05 Ono Pharmaceutical Co Compound having s1p receptor binding potency and use thereof
PL1772145T3 (en) 2004-07-16 2011-08-31 Kyorin Seiyaku Kk Method of effectively using medicine and method concerning prevention of side effect
JP2007284350A (en) 2004-07-27 2007-11-01 Takeda Chem Ind Ltd Therapeutic agent for diabetes
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
CN1993333B (en) 2004-08-04 2012-08-01 大正制药株式会社 Triazole derivative
US20060223866A1 (en) 2004-08-13 2006-10-05 Praecis Pharmaceuticals, Inc. Methods and compositions for modulating sphingosine-1-phosphate (S1P) receptor activity
WO2006020951A1 (en) 2004-08-13 2006-02-23 Praecis Pharmaceuticals, Inc. Methods and compositions for modulating sphingosine-1-phosphate (s1p) receptor activity
US7250441B2 (en) 2004-09-23 2007-07-31 Wyeth Carbazole and cyclopentaindole derivatives to treat infection with Hepatitis C virus
MX2007004262A (en) 2004-10-12 2008-03-04 Forbes Medi Tech Res Inc Compounds and methods of treating insulin resistance and cardiomyopathy.
DK1650186T3 (en) 2004-10-22 2008-10-13 Sun Pharmaceutical Ind Ltd New dicarboxylic acid derivatives
WO2006047195A2 (en) 2004-10-22 2006-05-04 Merck & Co., Inc. 2-(aryl)azacyclylmethyl carboxylates, sulfonates, phosphonates, phosphinates and heterocycles as s1p receptor agonists
JP2008520692A (en) 2004-11-18 2008-06-19 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 Heterocyclic substituted carboxylic acids
WO2006057448A1 (en) 2004-11-26 2006-06-01 Takeda Pharmaceutical Company Limited Arylalkanoic acid derivative
WO2006063033A2 (en) 2004-12-06 2006-06-15 University Of Virginia Patent Foundation Aryl amide sphingosine 1-phosphate analogs
PL1826197T3 (en) 2004-12-13 2012-06-29 Ono Pharmaceutical Co Aminocarboxylic acid derivative and medicinal use thereof
JP5798282B2 (en) 2005-01-25 2015-10-21 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ Mesogenic compound, liquid crystal medium and liquid crystal display
MX2007009848A (en) 2005-02-14 2008-03-10 Univ Virginia Sphingosine 1- phos phate agonists comprising cycloalkanes and 5 -membered heterocycles substituted by amino and phenyl groups.
CN101180050B (en) 2005-03-23 2011-07-27 埃科特莱茵药品有限公司 Novel thiophene derivatives as sphingosine-1-phosphate-1 receptor agonists
RU2404178C2 (en) 2005-03-23 2010-11-20 Актелион Фармасьютиклз Лтд Novel thiophene derivatives as sphingosine-1-phosphate-1 receptor agonists
JP5047941B2 (en) 2005-03-23 2012-10-10 アクテリオン ファーマシューティカルズ リミテッド Hydrogenated benzo (C) thiophene derivatives as immunomodulators
AU2006256968A1 (en) 2005-06-08 2006-12-14 Novartis Ag Polycyclic oxadiazoles or I soxazoles and their use as SIP receptor ligands
AU2006260573A1 (en) 2005-06-24 2006-12-28 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives
TWI418350B (en) 2005-06-24 2013-12-11 Sankyo Co Use of pharmaceutical compositions comprising ppar modulator
US20070060573A1 (en) 2005-08-10 2007-03-15 Lars Wortmann Acyltryptophanols
AU2006283175A1 (en) 2005-08-23 2007-03-01 Irm Llc Immunosuppressant compounds and compositions
WO2007037196A1 (en) 2005-09-29 2007-04-05 Yamamoto Chemicals, Inc. Indoline compound and method for producing same
AR057894A1 (en) 2005-11-23 2007-12-26 Actelion Pharmaceuticals Ltd THIOPHEN DERIVATIVES
AU2006317689B2 (en) 2005-11-23 2013-07-25 Epix Delaware, Inc. S1P receptor modulating compounds and use thereof
TWI404706B (en) 2006-01-11 2013-08-11 Actelion Pharmaceuticals Ltd Novel thiophene derivatives
TW200736234A (en) 2006-01-17 2007-10-01 Astrazeneca Ab Chemical compounds
EP1979345B1 (en) 2006-01-24 2009-11-04 Actelion Pharmaceuticals Ltd. Novel pyridine derivatives
GB0601744D0 (en) 2006-01-27 2006-03-08 Novartis Ag Organic compounds
TWI389683B (en) 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
CA2641718A1 (en) 2006-02-09 2007-08-16 University Of Virginia Patent Foundation Bicyclic sphingosine 1-phosphate analogs
TW200806611A (en) 2006-02-09 2008-02-01 Daiichi Seiyaku Co Novel amidopropionic acid derivatives and medicine containing the same
US20070191371A1 (en) 2006-02-14 2007-08-16 Kalypsys, Inc. Heterocyclic modulators of ppar
CN101460458A (en) 2006-02-15 2009-06-17 阿勒根公司 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
WO2007095561A2 (en) 2006-02-15 2007-08-23 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
EP1991535A1 (en) 2006-02-21 2008-11-19 University Of Virginia Patent Foundation Phenyl-cycloalkyl and phenyl-heterocyclic derivatives as sip receptor agonists
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
CA2646469A1 (en) 2006-03-21 2007-09-27 Epix Delaware, Inc. S1p receptor modulating compounds
JP2007262009A (en) 2006-03-29 2007-10-11 Dai Ichi Seiyaku Co Ltd Heteroaryl lower carboxylic acid derivative
ES2453372T3 (en) 2006-04-03 2014-04-07 Astellas Pharma Inc. Oxadiazole derivatives as S1P1 agonists
GB0607389D0 (en) 2006-04-12 2006-05-24 Novartis Ag Organic compounds
WO2007132307A1 (en) 2006-05-09 2007-11-22 Pfizer Products Inc. Cycloalkylamino acid derivatives and pharmaceutical compositions thereof
US20090324581A1 (en) 2006-05-09 2009-12-31 Daiichi Sankyo Company Limited Heteroarylamide lower carboxylic acid derivative
WO2007129473A1 (en) 2006-05-09 2007-11-15 Daiichi Sankyo Company, Limited Bicyclic aryl derivative
JP2009545597A (en) 2006-08-01 2009-12-24 プリーシス・ファーマシューティカルズ・インコーポレイテッド Sphingosine-1-phosphate receptor (SLP) agonist
AR062156A1 (en) 2006-08-01 2008-10-22 Praecis Pharm Inc S1P-1 RECEPTOR AGONIST AND SELECTIVE COMPOUNDS
JP2009545630A (en) 2006-08-04 2009-12-24 プリーシス・ファーマシューティカルズ・インコーポレイテッド Compound
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 (en) 2006-08-25 2009-11-19 Asahi Kasei Pharma Kk Amine compound
AU2007292993B2 (en) 2006-09-07 2013-01-24 Idorsia Pharmaceuticals Ltd Pyridin-4-yl derivatives as immunomodulating agents
BRPI0716815A2 (en) 2006-09-07 2013-11-05 Allergan Inc HETEROATOMATIC POST HAVING AGONIST AND / OR ANTAGONIST BIOLOGICAL ACTIVITY OF SPINPHOSINE-1-PHOSPHATE (S1P) RECEIVER
AR061841A1 (en) 2006-09-07 2008-09-24 Actelion Pharmaceuticals Ltd DERIVATIVES OF THIOFEN-OXADIAZOLS, AGONISTS OF THE S1P1 / EDG1 RECEPTOR, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USES AS IMMUNOMODULATING AGENTS.
CN101511783A (en) 2006-09-08 2009-08-19 诺瓦提斯公司 N-biaryl (hetero) arylsulphonamide derivatives useful in the treatment of diseases mediated by lymphocytes interactions
RU2442780C2 (en) 2006-09-21 2012-02-20 Актелион Фармасьютиклз Лтд Phenyl derivatives and their application as immunomodulators
AU2007334436A1 (en) 2006-12-15 2008-06-26 Abbott Laboratories Novel oxadiazole compounds
TW200838497A (en) 2006-12-21 2008-10-01 Abbott Lab 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 Compounds
KR20090101307A (en) 2007-01-11 2009-09-24 알러간, 인코포레이티드 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 (en) 2007-03-16 2014-02-10 Actelion Pharmaceuticals Ltd AMINOPYRIDINE DERIVATIVES AS S1P1 / EDG1 RECEPTOR AGONISTS
EP2121648A2 (en) 2007-03-21 2009-11-25 EPIX Pharmaceuticals, Inc. S1p receptor modulating compounds and use thereof
KR20090130062A (en) 2007-04-19 2009-12-17 글락소 그룹 리미티드 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
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
JP5508265B2 (en) 2007-08-08 2014-05-28 メルク セローノ ソシエテ アノニム 6-amino-pyrimidine-4-carboxamide derivatives and related compounds that bind to the sphingosine 1-phosphate (S1P) receptor for the treatment of multiple sclerosis
TW200930368A (en) 2007-11-15 2009-07-16 Astrazeneca Ab Bis-(sulfonylamino) derivatives in therapy
EP2222668B1 (en) 2007-12-18 2011-11-02 Arena Pharmaceuticals, Inc. Tetrahydrocyclopenta[b]indol-3-yl carboxylic acid derivatives useful in the treatment of autoimmune and inflammatory disorders
AU2009206733A1 (en) * 2008-01-25 2009-07-30 Arena Pharmaceuticals, Inc. Dihydro- 1H- pyrrolo [1,2-a] indol-1-yl carboxylic derivatives which act as S1P1 agonists
AR070398A1 (en) 2008-02-22 2010-03-31 Gruenenthal Chemie INDOL SUBSTITUTED DERIVATIVES
NZ589617A (en) 2008-05-14 2012-06-29 Scripps Research Inst 3-(Inden-4-yl)-5-(phenyl)-1,2,4-oxadiazole and 3-(tetralin-5-yl)-5-(phenyl)-1,2,4-oxadiazole derivatives
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
HUE030424T2 (en) 2008-07-23 2017-05-29 Arena Pharm Inc SUBSTITUTED 1,2,3,4- TETRAHYDROCYCLOPENTA[b]INDOL-3-YL) ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS
SI2342205T1 (en) * 2008-08-27 2016-09-30 Arena Pharmaceuticals, Inc. Substituted tricyclic acid derivatives as s1p1 receptor agonists useful in the treatment of autoimmune and inflammatory disorders
BRPI0922135B1 (en) * 2008-12-05 2021-07-13 Astellas Pharma Inc 2H-CROMENE COMPOUND OR A SALT THEREOF, PHARMACEUTICAL COMPOSITION COMPRISING SUCH COMPOUND AND USE OF THE SAME TO PREVENT OR TREAT A DISEASE INDUCED BY UNDESIRABLE LYMPHOCYTE INFILTRATION ASSOCIATED WITH S1P1
CA2749960A1 (en) 2009-02-10 2010-08-19 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
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
EP2597089A1 (en) 2009-10-29 2013-05-29 Bristol-Myers Squibb Company Tricyclic heterocyclic compounds
ES2937386T3 (en) 2010-01-27 2023-03-28 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 of same
WO2011109471A1 (en) * 2010-03-03 2011-09-09 Arena Pharmaceuticals, Inc. Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof
WO2012015758A2 (en) 2010-07-30 2012-02-02 Saint Louis University Methods of treating pain

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