CN102164891B - 可用于治疗自身免疫性疾病和炎性疾病的经取代的1,2,3,4-四氢环戊并[b]吲哚-3-基乙酸衍生物 - Google Patents

可用于治疗自身免疫性疾病和炎性疾病的经取代的1,2,3,4-四氢环戊并[b]吲哚-3-基乙酸衍生物 Download PDF

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CN102164891B
CN102164891B CN200980137275.7A CN200980137275A CN102164891B CN 102164891 B CN102164891 B CN 102164891B CN 200980137275 A CN200980137275 A CN 200980137275A CN 102164891 B CN102164891 B CN 102164891B
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trifluoromethyl
tetrahydrocyclopenta
cyano
acetic acid
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CN102164891A (zh
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罗伯特.M.琼斯
丹尼尔.J.布扎德
韩相敦
金善姬
朱尔格.莱曼
布雷特.厄尔曼
珍妮.V.穆迪
朱秀文
斯科特.斯特恩
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Arena Pharmaceuticals Inc
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CN200980137275.7A 2008-07-23 2009-07-22 可用于治疗自身免疫性疾病和炎性疾病的经取代的1,2,3,4-四氢环戊并[b]吲哚-3-基乙酸衍生物 Active CN102164891B (zh)

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CN201410403616.3A CN104311472B9 (zh) 2008-07-23 2009-07-22 经取代的1,2,3,4-四氢环戊并[b]吲哚-3-基乙酸衍生物

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US13567208P 2008-07-23 2008-07-23
US61/135,672 2008-07-23
US20937409P 2009-03-06 2009-03-06
US61/209,374 2009-03-06
PCT/US2009/004265 WO2010011316A1 (en) 2008-07-23 2009-07-22 SUBSTITUTED 1,2,3,4- TETRAHYDROCYCLOPENTA[b]INDOL-3-YL) ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104311472A (zh) * 2008-07-23 2015-01-28 艾尼纳制药公司 经取代的1,2,3,4-四氢环戊并[b]吲哚-3-基乙酸衍生物

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE531711T1 (de) * 2007-12-18 2011-11-15 Arena Pharm Inc Für die behandlung von autoimmunerkrankungen und entzündlichen erkrankungen geeignete tetrahydrocyclopentaäbüindol-3- ylcarbonsäurederivate
US20100292233A1 (en) * 2008-01-25 2010-11-18 Arena Pharmaceuticals, Inc. Dihydro-1h-pyrrolo[1,2-a]indol-1-yl carboxylic acid derivatives which act as s1p1 agonists
US8415484B2 (en) * 2008-08-27 2013-04-09 Arena Pharmaceuticals, Inc. Substituted tricyclic acid derivatives as S1P1 receptor agonists useful in the treatment of autoimmune and inflammatory disorders
ES2759949T3 (es) 2009-10-29 2020-05-12 Bristol Myers Squibb Co Compuestos heterocíclicos tricíclicos
SG10201500639TA (en) * 2010-01-27 2015-03-30 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
EP2542554B1 (en) 2010-03-03 2015-11-04 Arena Pharmaceuticals, Inc. Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof
US8987307B2 (en) 2011-03-03 2015-03-24 Hoffmann-La Roche Inc. 3-amino-pyridines as GPBAR1 agonists
HK1200821A1 (en) 2012-04-04 2015-08-14 霍夫曼-拉罗奇有限公司 1,2- pyridazine, 1,6- pyridazine or pyrimidine - benzamide derivatives as gpbar1 modulators
KR102173963B1 (ko) 2012-12-06 2020-11-04 쓰리엠 이노베이티브 프로퍼티즈 컴파니 점성 액체의 정밀 코팅 및 라미네이트 형성에서의 사용
JP6430955B2 (ja) 2012-12-06 2018-11-28 スリーエム イノベイティブ プロパティズ カンパニー 液体コーティングされた基材上の液体の離散的コーティング、及び積層体の形成における使用
ES2995737T3 (en) * 2015-01-06 2025-02-11 Arena Pharm Inc Compound for use in treating conditions related to the s1p1 receptor
MA42807A (fr) 2015-06-22 2018-07-25 Arena Pharm Inc Sel l-arginine cristallin d'acide (r)-2-(7-(4-cyclopentyl-3-(trifluorométhyl)benzyloxy)-1,2,3,4-tétrahydrocyclo-penta[b]indol-3-yl)acétique (composé 1) pour une utilisation dans des troubles associés au récepteur de s1p1
WO2017004609A1 (en) 2015-07-02 2017-01-05 Exelixis, Inc. Thiadiazole modulators of s1p and methods of making and using
WO2017004608A1 (en) 2015-07-02 2017-01-05 Exelixis, Inc. Oxadiazole modulators of s1p methods of making and using
JP7029445B2 (ja) 2016-09-02 2022-03-03 ブリストル－マイヤーズ スクイブ カンパニー 置換された三環式ヘテロ環化合物
WO2018151873A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of primary biliary cholangitis
CA3053416A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of inflammatory bowel disease with extra-intestinal manifestations
AU2018257917B2 (en) * 2017-04-24 2023-05-04 University Of Massachusetts Diagnosis and treatment of vitiligo
CN110730767B (zh) 2017-07-13 2022-06-24 东丽精细化工株式会社 环烷基(三氟甲基)苯的制造方法
US11059784B2 (en) 2017-08-09 2021-07-13 Bristol-Myers Squibb Company Oxime ether compounds
WO2019032632A1 (en) 2017-08-09 2019-02-14 Bristol-Myers Squibb Company ALKYLPHENYL COMPOUNDS
EP3801459B1 (en) 2018-06-06 2024-08-07 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
WO2020051378A1 (en) 2018-09-06 2020-03-12 Arena Pharmaceuticals, Inc. Compounds useful in the treatment of autoimmune and inflammatory disorders
US20210386706A1 (en) * 2018-10-03 2021-12-16 Arena Pharmaceuticals, Inc. Methods for the treatment of scleroderma
KR102824401B1 (ko) * 2018-11-30 2025-06-25 아레나 파마슈티칼스, 인크. S1p1 수용체와 관련된 병태의 치료 방법
TWI846774B (zh) * 2018-12-06 2024-07-01 大陸商上海濟煜醫藥科技有限公司 作為免疫調節的芳環衍生物及其製備方法和應用
WO2020146529A1 (en) 2019-01-08 2020-07-16 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
MX2022003982A (es) * 2019-10-01 2022-07-12 Arena Pharm Inc Metodos de tratamiento de enfermedades relacionadas con el receptor s1p1.
PH12022551043A1 (en) 2019-10-31 2023-05-03 Idorsia Pharmaceuticals Ltd Combination of a cxcr7 antagonist with an s1p1 receptor modulator
KR20220103750A (ko) * 2019-11-20 2022-07-22 아레나 파마슈티칼스, 인크. S1p1 수용체와 관련된 상태를 치료하는 방법
CN115066242A (zh) * 2020-01-06 2022-09-16 艾尼纳制药公司 治疗与s1p1受体相关的病症的方法
US20230055568A1 (en) 2020-02-06 2023-02-23 Mitsubishi Tanabe Pharma Corporation Therapeutic agent for myalgic encephalomyelitis/chronic fatigue syndrome
US12486229B2 (en) * 2020-07-03 2025-12-02 Shanghai Medicilon Inc. Indole derivative and application thereof
JP2023548474A (ja) * 2020-11-09 2023-11-17 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受容体に関連する状態を処置する方法
CN112812052B (zh) * 2021-02-02 2023-12-01 成都阿奇生物医药科技有限公司 一种治疗溃疡性结肠炎的化合物及其制备方法和用途
WO2023109931A1 (zh) * 2021-12-17 2023-06-22 上海济煜医药科技有限公司 一种芳环衍生物的晶型及其制备方法和应用
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
US20250152556A1 (en) 2022-01-13 2025-05-15 Arena Pharmaceuticals, Inc. Etrasimod for use in treating s1p1 receptor-associated disorders in combination with hormone treatment
KR20240158969A (ko) * 2022-03-09 2024-11-05 아레나 파마슈티칼스, 인크. 새로운 s1p1 수용체 작용제, 결정질 염, 제조 방법, 및 이에 관한 용도
WO2023214312A1 (en) 2022-05-06 2023-11-09 Arena Pharmaceuticals, Inc. Methods of treating atopic dermatitis with etrasimod
WO2025007928A1 (zh) * 2023-07-05 2025-01-09 苏州湃芮生物科技有限公司 一种吲哚类化合物及其制备方法和用途
CN116854622A (zh) * 2023-07-10 2023-10-10 青岛科技大学 一种多取代的2,4-二氢环戊二烯并[b]吲哚类化合物的合成方法
WO2025083549A1 (en) 2023-10-16 2025-04-24 Sun Pharma Advanced Research Company Limited Methods and combinations of inhibitors of il-23 pathway and modulators of s1p signaling pathway for the treatment of autoimmune disorders
CN119330873B (zh) * 2024-11-08 2025-07-11 成都克莱蒙医药科技有限公司 一种依曲莫德中间体的制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1436893A (en) * 1972-05-25 1976-05-26 Schering Ag Tetrahydrocarbazole derivatives and process for their manufa cture
WO1991006537A2 (en) * 1989-10-27 1991-05-16 American Home Products Corporation Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole- alkanoic acid derivatives as inhibitors of pla2 and lipoxygenase
EP0468785A2 (en) * 1990-07-26 1992-01-29 Merck Frosst Canada Inc. (Quinolin-2-ylmethoxy)tetrahydrocarbazoles as inhibitors of the biosynthesis of leukotrienes
CN101035528A (zh) * 2004-09-23 2007-09-12 惠氏公司 治疗丙型肝炎病毒感染的咔唑和环戊二烯并吲哚衍生物

Family Cites Families (146)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL293572A (enExample) 1962-06-07
US3843681A (en) * 1971-06-01 1974-10-22 American Home Prod 1-carboxamido pyrano(thiopyrano)(3,4-6)indole derivatives
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
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
JP4038266B2 (ja) * 1998-02-17 2008-01-23 オイレス工業株式会社 粘性せん断型ダンパー
RU2267484C2 (ru) 1999-04-28 2006-01-10 Авентис Фарма Дойчланд Гмбх Производные диариловой кислоты и фармацевтическая композиция на их основе
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
WO2002079131A1 (en) 2001-03-29 2002-10-10 Kansai Research Institute, Inc. 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
CA2461212C (en) 2001-09-27 2010-08-17 Kyorin Pharmaceutical Co., Ltd. Diaryl sulfide derivatives, salts thereof and immunosuppressive agents using the same
WO2003061567A2 (en) 2002-01-18 2003-07-31 Merck & Co., Inc. Selective s1p1/edg1 receptor agonists
EP1467729A1 (en) 2002-01-18 2004-10-20 The Genetics Company Inc. Beta-secretase inhibitors
WO2003062252A1 (en) 2002-01-18 2003-07-31 Merck & Co., Inc. Edg receptor agonists
EP1482895A4 (en) 2002-03-01 2005-04-27 Merck & Co Inc AMINO ALKYL PHOSPHONATES AND RELATED COMPOUNDS AS EDG RECEPTOR AGONISTS
AU2003218056A1 (en) 2002-03-01 2003-09-16 Merck & Co., Inc. Aminoalkylphosphonates and related compounds as edg receptor agonists
AU2003276043A1 (en) 2002-06-17 2003-12-31 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
EP1541563A4 (en) 2002-07-10 2007-11-07 Ono Pharmaceutical Co ANTAGONIST OF CCR4 AND CORRESPONDING MEDICINAL USE
AU2003259296A1 (en) 2002-07-30 2004-02-16 University Of Virginia Patent Foundation Compounds active in spinigosine 1-phosphate signaling
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
US7256206B2 (en) 2003-02-11 2007-08-14 Irm Llc Bicyclic compounds and compositions
CN100344638C (zh) 2003-02-18 2007-10-24 杏林制药株式会社 氨基膦酸衍生物、其加成盐以及s1p受体调节剂
ATE547395T1 (de) 2003-04-30 2012-03-15 Novartis Pharma Gmbh Aminopropanol-derivate als modulatoren des sphingosin-1-phosphat-rezeptors
CA2523677A1 (en) 2003-04-30 2004-11-11 Novartis Ag Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators
CA2523743A1 (en) 2003-04-30 2004-11-18 The Institutes For Pharmaceutical Discovery, Llc Heterocycle substituted carboxylic acids as inhibitors of protein tyrosine phosphatase-1b
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
JP4728962B2 (ja) 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 免疫抑制化合物および組成物
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
BRPI0410454A (pt) 2003-05-19 2006-06-13 Irm Llc composições e compostos imunossupressores
PE20050158A1 (es) 2003-05-19 2005-05-12 Irm Llc Compuestos inmunosupresores y composiciones
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
ATE449069T1 (de) 2003-08-28 2009-12-15 Novartis Pharma Gmbh Aminopropanolderivate
CN101407471A (zh) 2003-08-29 2009-04-15 小野药品工业株式会社 能够结合s1p受体的化合物及其药物用途
EP1661889A4 (en) 2003-09-05 2009-08-05 Ono Pharmaceutical Co ANTAGONIST OF THE CHEMOKINE RECEPTOR AND ITS USE FOR MEDICAL PURPOSES
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
CA2547198A1 (en) 2003-12-17 2005-06-30 Merck & Co., Inc. (3,4-disubstituted)propanoic carboxylates as s1p (edg) receptor agonists
GB0329498D0 (en) 2003-12-19 2004-01-28 Novartis Ag Organic compounds
ATE528276T1 (de) 2003-12-19 2011-10-15 Ono Pharmaceutical Co Lysophosphatidylsäurerezeptor-antagonistische verbindungen und ihre anwendungen
GB0401332D0 (en) 2004-01-21 2004-02-25 Novartis Ag Organic compounds
JP2005272453A (ja) 2004-02-24 2005-10-06 Sankyo Co Ltd アミノアルコール化合物
EP1718604A4 (en) 2004-02-24 2008-02-13 Irm Llc COMPOUNDS AND COMPOSITIONS OF IMMUNOSUPPRESSANTS
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
AU2005230897B2 (en) 2004-04-02 2011-03-03 Merck Sharp & Dohme Corp. 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
EP1760071A4 (en) 2004-06-23 2008-03-05 Ono Pharmaceutical Co COMPOUND WITH S1P RECEPTOR BINDING ABILITY AND USE THEREOF
EP1772145B1 (en) 2004-07-16 2011-03-23 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
EP1798226A4 (en) 2004-08-04 2009-06-17 Taisho Pharmaceutical Co Ltd TRAIZOL DERIVATIVE
US20060223866A1 (en) 2004-08-13 2006-10-05 Praecis Pharmaceuticals, Inc. Methods and compositions for modulating sphingosine-1-phosphate (S1P) receptor activity
JP2008509931A (ja) 2004-08-13 2008-04-03 プレーシス ファーマスーティカルズ 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）レセプター活性を調節するための方法および組成物
BRPI0515992A (pt) 2004-10-12 2008-08-19 Forbes Medi Tech Res Inc compostos e métodos para o tratamento de resistência à insulina e cardiomiopatia
WO2006047195A2 (en) 2004-10-22 2006-05-04 Merck & Co., Inc. 2-(aryl)azacyclylmethyl carboxylates, sulfonates, phosphonates, phosphinates and heterocycles as s1p receptor agonists
DE602004014277D1 (de) 2004-10-22 2008-07-17 Bioprojet Soc Civ Neue Dicarbonsäurederivate
AU2005307718A1 (en) 2004-11-18 2006-05-26 The Institutes For Pharmaceutical Discovery, Llc Heterocycle substituted carboxylic acids for the treatment of diabetes
WO2006057448A1 (ja) 2004-11-26 2006-06-01 Takeda Pharmaceutical Company Limited アリールアルカン酸誘導体
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
EP2371811B1 (en) 2004-12-13 2014-10-08 Ono Pharmaceutical Co., Ltd. Azetidinecarboxylic acid derivative and medicinal use thereof
JP5798282B2 (ja) 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 メソゲン性化合物、液晶媒体および液晶ディスプレイ
US7754703B2 (en) 2005-02-14 2010-07-13 University Of Virginia Patent Foundation Cycloalkane-containing sphingosine 1-phosphate agonists
CN101146529B (zh) 2005-03-23 2012-08-29 埃科特莱茵药品有限公司 新颖噻吩衍生物作为鞘氨醇-1-磷酸酯-1受体激动剂
EP1863787B1 (en) 2005-03-23 2011-05-25 Actelion Pharmaceuticals Ltd. Hydogrenated benzo[c]thiophene derivatives as immunomodulators
US7846964B2 (en) 2005-03-23 2010-12-07 Actelion Pharmaceuticals Ltd. Thiophene derivatives as spingosine-1-phosphate-1 receptor agonists
EP1893591A1 (en) 2005-06-08 2008-03-05 Novartis AG POLYCYCLIC OXADIAZOLES OR I SOXAZOLES AND THEIR USE AS SlP RECEPTOR LIGANDS
CA2612661A1 (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
WO2007024922A1 (en) 2005-08-23 2007-03-01 Irm Llc Immunosuppressant compounds and compositions
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
AR057894A1 (es) 2005-11-23 2007-12-26 Actelion Pharmaceuticals Ltd Derivados de tiofeno
JP2009520688A (ja) 2005-11-23 2009-05-28 エピックス デラウェア， インコーポレイテッド Ｓ１ｐ受容体調節化合物およびそれらの使用
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
JP5063615B2 (ja) 2006-01-24 2012-10-31 アクテリオン ファーマシューティカルズ リミテッド 新規ピリジン誘導体
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
WO2007092638A1 (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
AU2007214434B2 (en) 2006-02-15 2012-06-14 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
CN101384566A (zh) 2006-02-21 2009-03-11 弗吉尼亚大学专利基金会 作为s1p受体激动剂的苯基-环烷基和苯基-杂环衍生物
US7649098B2 (en) 2006-02-24 2010-01-19 Lexicon Pharmaceuticals, Inc. Imidazole-based compounds, compositions comprising them and methods of their use
JP2009530281A (ja) 2006-03-14 2009-08-27 アムジエン・インコーポレーテツド 代謝障害の治療に有用である二環式カルボン酸誘導体
TW200806633A (en) 2006-03-21 2008-02-01 Epix Pharm 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
EP2003132B1 (en) 2006-04-03 2014-03-05 Astellas Pharma Inc. Oxadiazole derivatives as S1P1 agonists
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
BRPI0711358A2 (pt) 2006-05-09 2011-09-27 Pfizer Prod Inc derivados do ácido cicloalquilamino e suas composições farmacêuticas
US20090324581A1 (en) 2006-05-09 2009-12-31 Daiichi Sankyo Company Limited Heteroarylamide lower carboxylic acid derivative
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
US20090318389A1 (en) 2006-08-04 2009-12-24 Praecis Pharmaceuticals Incorporated Agonists of the sphingosine-1 phosphate receptor
PL2058317T3 (pl) 2006-08-08 2014-03-31 Kyorin Seiyaku Kk Aminowa pochodna estru kwasu fosforowego i modulator receptora S1P zawierający ją jako składnik aktywny
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
CA2662852A1 (en) 2006-09-07 2008-03-13 Allergan, Inc. Heteroaromatic compounds having sphingosine-1-phosphate (s1p) receptor agonist and/or antagonist biological activity
MY149853A (en) 2006-09-07 2013-10-31 Actelion Pharmaceuticals Ltd Pyridin-4-yl derivatives as immunomodulating agents
TWI408139B (zh) 2006-09-07 2013-09-11 Actelion Pharmaceuticals Ltd 新穎噻吩衍生物
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
KR20090051774A (ko) 2006-09-21 2009-05-22 액테리온 파마슈티칼 리미티드 페닐 유도체 및 면역조절제로서 이들의 용도
EP2109364A4 (en) 2006-12-15 2010-04-14 Abbott Lab NOVEL OXADIAZONE COMPOUNDS
UY30829A1 (es) 2006-12-21 2008-07-31 Abbott Lab Compuestos agonistas y antagonistas del receptor de esfinfosina-1-fosfato
JO2701B1 (en) 2006-12-21 2013-03-03 جلاكسو جروب ليميتد Vehicles
GB0625648D0 (en) 2006-12-21 2007-01-31 Glaxo Group Ltd Compounds
CA2674946A1 (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
MX2009010060A (es) 2007-03-21 2010-01-20 Epix Pharm Inc Compuestos moduladores del receptor de esfingosin-1-fosfato y uso de los mismos.
CA2684385A1 (en) 2007-04-19 2008-10-30 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
WO2009019167A1 (en) 2007-08-08 2009-02-12 Merck Serono S.A. 6-amino-pyrimidine-4-carboxamide derivatives and related compounds which 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
ATE531711T1 (de) 2007-12-18 2011-11-15 Arena Pharm Inc Für die behandlung von autoimmunerkrankungen und entzündlichen erkrankungen geeignete tetrahydrocyclopentaäbüindol-3- ylcarbonsäurederivate
US20100292233A1 (en) 2008-01-25 2010-11-18 Arena Pharmaceuticals, Inc. Dihydro-1h-pyrrolo[1,2-a]indol-1-yl carboxylic acid derivatives which act as s1p1 agonists
AR070398A1 (es) 2008-02-22 2010-03-31 Gruenenthal Chemie Derivados sustituidos de indol
DK2291080T3 (en) 2008-05-14 2015-12-07 Scripps Research Inst Novel modulator of sphingosinphosphatreceptorer
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
CN104311472B9 (zh) 2008-07-23 2020-03-17 艾尼纳制药公司 经取代的1,2,3,4-四氢环戊并[b]吲哚-3-基乙酸衍生物
US8415484B2 (en) 2008-08-27 2013-04-09 Arena Pharmaceuticals, Inc. Substituted tricyclic acid derivatives as S1P1 receptor agonists 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
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
ES2759949T3 (es) 2009-10-29 2020-05-12 Bristol Myers Squibb Co Compuestos heterocíclicos tricíclicos
SG10201500639TA (en) 2010-01-27 2015-03-30 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
EP2542554B1 (en) 2010-03-03 2015-11-04 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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1436893A (en) * 1972-05-25 1976-05-26 Schering Ag Tetrahydrocarbazole derivatives and process for their manufa cture
WO1991006537A2 (en) * 1989-10-27 1991-05-16 American Home Products Corporation Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole- alkanoic acid derivatives as inhibitors of pla2 and lipoxygenase
EP0468785A2 (en) * 1990-07-26 1992-01-29 Merck Frosst Canada Inc. (Quinolin-2-ylmethoxy)tetrahydrocarbazoles as inhibitors of the biosynthesis of leukotrienes
CN101035528A (zh) * 2004-09-23 2007-09-12 惠氏公司 治疗丙型肝炎病毒感染的咔唑和环戊二烯并吲哚衍生物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Discovery of a Potent and Selective Prostaglandin D2 Receptor Antagonist, [(3R)-4-(4-Chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic Acid (MK-0524);Claudio F. Sturino, et al.;《J. Med. Chem》;20070120;第50卷(第4期);第794-806页 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104311472A (zh) * 2008-07-23 2015-01-28 艾尼纳制药公司 经取代的1,2,3,4-四氢环戊并[b]吲哚-3-基乙酸衍生物

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