CN101370496B - 作为s1p1/edg1受体促效剂的新型噻吩衍生物 - Google Patents

作为s1p1/edg1受体促效剂的新型噻吩衍生物 Download PDF

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Publication number
CN101370496B
CN101370496B CN2007800022066A CN200780002206A CN101370496B CN 101370496 B CN101370496 B CN 101370496B CN 2007800022066 A CN2007800022066 A CN 2007800022066A CN 200780002206 A CN200780002206 A CN 200780002206A CN 101370496 B CN101370496 B CN 101370496B
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China
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methyl
isobutyl
hydroxy
dimethyl
thiophen
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Expired - Fee Related
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CN101370496A (zh
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马丁·博利
大卫·莱曼
博里斯·马蒂斯
克劳斯·米勒
奥利弗·内勒
比特·斯蒂内
约尔格·韦尔克
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Actelion Pharmaceuticals Ltd
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Actelion Pharmaceuticals Ltd
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    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
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CN2007800022066A 2006-01-11 2007-01-10 作为s1p1/edg1受体促效剂的新型噻吩衍生物 Expired - Fee Related CN101370496B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IBPCT/IB2006/050103 2006-01-11
IB2006050103 2006-01-11
WOPCT/IB2006/050103 2006-01-11
PCT/IB2007/050070 WO2007080542A1 (en) 2006-01-11 2007-01-10 Novel thiophene derivatives as s1p1/edg1 receptor agonists

Publications (2)

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CN101370496A CN101370496A (zh) 2009-02-18
CN101370496B true CN101370496B (zh) 2012-07-04

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CN2007800022066A Expired - Fee Related CN101370496B (zh) 2006-01-11 2007-01-10 作为s1p1/edg1受体促效剂的新型噻吩衍生物

Country Status (17)

Country Link
US (1) US8003800B2 (https=)
EP (1) EP1976512B1 (https=)
JP (1) JP5114430B2 (https=)
KR (1) KR101382710B1 (https=)
CN (1) CN101370496B (https=)
AR (1) AR058956A1 (https=)
AU (1) AU2007204121B2 (https=)
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Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2007209051A1 (en) * 2006-01-24 2007-08-02 Actelion Pharmaceuticals Ltd Novel pyridine derivatives
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.
PT2069336E (pt) * 2006-09-07 2013-03-07 Actelion Pharmaceuticals Ltd Derivados de piridin-4-ilo como agentes imunomoduladores
PL2069335T3 (pl) * 2006-09-08 2013-05-31 Actelion Pharmaceuticals Ltd Pochodne pirydyn-3-ylu jako środki immunomodulujące
EP2109364A4 (en) 2006-12-15 2010-04-14 Abbott Lab NOVEL OXADIAZONE COMPOUNDS
BRPI0808789A2 (pt) * 2007-03-16 2014-08-12 Actelion Pharmaceuticals Ltd Compostos e composição farmacêutica de derivados aminopiridina e uso destes
KR101547705B1 (ko) * 2007-05-22 2015-08-26 와이어쓰 엘엘씨 히드라지드의 개선된 제조 방법
PT2195311E (pt) * 2007-08-17 2011-05-25 Actelion Pharmaceuticals Ltd Derivados de piridina como moduladores do receptor s1p1/edg1
CN104478821B (zh) * 2007-10-04 2016-09-28 默克雪兰诺有限公司 噁二唑二芳基化合物
KR20100092473A (ko) * 2007-11-01 2010-08-20 액테리온 파마슈티칼 리미티드 신규한 피리미딘 유도체
MX2010005889A (es) * 2007-12-10 2010-06-22 Actelion Pharmaceuticals Ltd Derivados de tiofeno como agonistas de s1p1/edg1.
EP2262799B1 (en) * 2008-03-06 2012-07-04 Actelion Pharmaceuticals Ltd. Pyridine compounds
CA2715317A1 (en) * 2008-03-07 2009-09-11 Actelion Pharmaceuticals Ltd Novel aminomethyl benzene derivatives
WO2009109872A1 (en) * 2008-03-07 2009-09-11 Actelion Pharmaceuticals Ltd Pyridin-2-yl derivatives as immunomodulating agents
PL2278960T5 (pl) 2008-03-17 2020-06-29 Actelion Pharmaceuticals Ltd. Schemat dawkowania dla selektywnego agonisty receptora sip1
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
HRP20160890T1 (hr) 2008-08-27 2016-09-23 Arena Pharmaceuticals, Inc. Derivati supstituirane tricikličke kiseline kao agonisti s1p1-receptora korisni u liječenju autoimunih i upalnih poremećaja
CA2767585C (en) 2009-07-16 2017-09-26 Actelion Pharmaceuticals Ltd Pyridin-4-yl derivatives
US8399451B2 (en) 2009-08-07 2013-03-19 Bristol-Myers Squibb Company Heterocyclic compounds
TW201120016A (en) * 2009-12-08 2011-06-16 Abbott Lab Novel oxadiazole compounds
JP5856980B2 (ja) 2010-01-27 2016-02-10 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−シクロペンチル−３−（トリフルオロメチル）ベンジルオキシ）−１，２，３，４−テトラヒドロシクロペンタ［ｂ］インドール−３−イル）酢酸およびその塩の調製のためのプロセス
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
ES2548683T3 (es) 2010-04-23 2015-10-20 Bristol-Myers Squibb Company Amidas del ácido 4-(5-isoxazolil o 5-pirrazolil-1,2,4-oxadiazol-3-il)-mandélico como agonistas de receptor de esfingosina-1-fosfato 1
TW201206429A (en) * 2010-07-08 2012-02-16 Merck Serono Sa Substituted oxadiazole derivatives
EP2619190B1 (en) 2010-09-24 2015-08-12 Bristol-Myers Squibb Company Substituted oxadiazole compounds and their use as s1p1 agonists
MA34910B1 (fr) * 2011-01-19 2014-02-01 Actelion Pharmaceuticals Ltd Dérivés de 2-methoxy-pyridin-4-yl
SMT202000298T1 (it) 2012-08-17 2020-07-08 Actelion Pharmaceuticals Ltd Processo per la produzione di (2z,5z)-5-(3-cloro-4((r)-2,3-diidrossipropossi) benziliden)-2-(propilimmino)-3-(o-tolil)tiazolidin-4-one e intermedio usato in detto processo
PL3242666T3 (pl) 2015-01-06 2025-02-17 Arena Pharmaceuticals, Inc. Związek do zastosowania w leczeniu dolegliwości związanych z receptorem s1p1
CN107406437B (zh) * 2015-03-06 2021-01-05 Ａｇｃ株式会社 制备1,2,4-噁二唑衍生物的方法
PH12017502097B1 (en) 2015-05-20 2023-05-05 Idorsia Pharmaceuticals Ltd Crystalline form of the compound (s)-3-{4-[5-(2-cyclopentyl-6-methoxy-pyridin-4-yl)-[1,2,4]oxadiazol-3-yl]-2-ethyl-6-methyl-phenoxy}-propane-1,2-diol
US10111841B2 (en) 2015-06-19 2018-10-30 University Of South Florida Stabilization of alcohol intoxication-induced cardiovascular instability
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
MX2019009841A (es) 2017-02-16 2020-01-30 Arena Pharm Inc Compuestos y metodos para el tratamiento de la colangitis biliar primaria.
MX2019009843A (es) 2017-02-16 2020-01-30 Arena Pharm Inc Compuestos y metodos para el tratamiento de la enfermedad inflamatoria intestinal con manifestaciones extraintestinales.
CA3102136A1 (en) 2018-06-06 2019-12-12 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
CN112955431A (zh) 2018-09-06 2021-06-11 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
US11186556B1 (en) 2018-10-16 2021-11-30 Celgene Corporation Salts of a thiazolidinone compound, solid forms, compositions and methods of use thereof
US11014940B1 (en) 2018-10-16 2021-05-25 Celgene Corporation Thiazolidinone and oxazolidinone compounds and formulations
US11013723B1 (en) 2018-10-16 2021-05-25 Celgene Corporation Solid forms of a thiazolidinone compound, compositions and methods of use thereof
US11014897B1 (en) 2018-10-16 2021-05-25 Celgene Corporation Solid forms comprising a thiazolidinone compound, compositions and methods of use thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003062248A2 (en) * 2002-01-18 2003-07-31 Merck & Co., Inc. N-(benzyl)aminoalkylcarboxylates, phosphinates, phosphonates and tetrazoles as edg receptor agonists
WO2005014525A2 (en) * 2003-08-12 2005-02-17 Mitsubishi Pharma Corporation Bi-aryl compound having immunosuppressive activity
WO2005032465A2 (en) * 2003-10-01 2005-04-14 Merck & Co., Inc. 3,5-aryl, heteroaryl or cycloalkyl substituted-1,2,4-oxadiazoles as s1p receptor agonists
WO2005058848A1 (en) * 2003-12-17 2005-06-30 Merck & Co., Inc. (3,4-disubstituted)propanoic carboxylates as s1p (edg) receptor agonists

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU7686891A (en) 1990-04-05 1991-10-30 American National Red Cross, The A protein family related to immediate-early protein expressed by human endothelial cells during differentiation
DE19643037A1 (de) * 1996-10-18 1998-04-23 Boehringer Ingelheim Kg Neue Oxadiazole, Verfahren zu ihrer Herstellung sowie deren Verwendung als Arzneimittel
US6423508B1 (en) 1998-03-09 2002-07-23 Smithkline Beecham Corporation Polynucleotide sequences of human EDG-1c
RU2233839C1 (ru) * 2000-07-13 2004-08-10 Санкио Компани, Лимитед Производные аминоспиртов, фармацевтическая композиция, способ профилактики или лечения, промежуточные соединения и способ получения промежуточных соединений
WO2003061567A2 (en) * 2002-01-18 2003-07-31 Merck & Co., Inc. Selective s1p1/edg1 receptor agonists
JP4430941B2 (ja) 2002-01-18 2010-03-10 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
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
WO2004035538A1 (en) 2002-10-15 2004-04-29 Merck & Co., Inc. Process for making azetidine-3-carboxylic acid
AU2004240586A1 (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
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
WO2006010379A1 (en) 2004-07-29 2006-02-02 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives as immunosuppressive agents
CA2602474C (en) 2005-03-23 2014-06-10 Actelion Pharmaceuticals Ltd Hydrogenated benzo (c) thiophene derivatives as immunomodulators
KR20080002850A (ko) 2005-03-23 2008-01-04 액테리온 파마슈티칼 리미티드 신규한 티오펜 유도체
US7605269B2 (en) 2005-03-23 2009-10-20 Actelion Pharmaceuticals Ltd. Thiophene derivatives as Sphingosine-1-phosphate-1 receptor agonists
WO2006131336A1 (en) 2005-06-08 2006-12-14 Novartis Ag POLYCYCLIC OXADIAZOLES OR I SOXAZOLES AND THEIR USE AS SlP RECEPTOR LIGANDS
US7951794B2 (en) 2005-06-24 2011-05-31 Actelion Pharmaceuticals Ltd. Thiophene derivatives
GB0601744D0 (en) 2006-01-27 2006-03-08 Novartis Ag Organic compounds
EP2109364A4 (en) 2006-12-15 2010-04-14 Abbott Lab NOVEL OXADIAZONE COMPOUNDS
WO2008091967A1 (en) 2007-01-26 2008-07-31 Smithkline Beecham Corporation Chemical compounds
MX2010005889A (es) 2007-12-10 2010-06-22 Actelion Pharmaceuticals Ltd Derivados de tiofeno como agonistas de s1p1/edg1.

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003062248A2 (en) * 2002-01-18 2003-07-31 Merck & Co., Inc. N-(benzyl)aminoalkylcarboxylates, phosphinates, phosphonates and tetrazoles as edg receptor agonists
WO2005014525A2 (en) * 2003-08-12 2005-02-17 Mitsubishi Pharma Corporation Bi-aryl compound having immunosuppressive activity
WO2005032465A2 (en) * 2003-10-01 2005-04-14 Merck & Co., Inc. 3,5-aryl, heteroaryl or cycloalkyl substituted-1,2,4-oxadiazoles as s1p receptor agonists
WO2005058848A1 (en) * 2003-12-17 2005-06-30 Merck & Co., Inc. (3,4-disubstituted)propanoic carboxylates as s1p (edg) receptor agonists

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AR058956A1 (es) 2008-03-05
WO2007080542A1 (en) 2007-07-19
NO20083462L (no) 2008-10-09
BRPI0706476A2 (pt) 2011-04-05
KR20080083010A (ko) 2008-09-12
CA2635047A1 (en) 2007-07-19
RU2008132802A (ru) 2010-02-20
KR101382710B1 (ko) 2014-04-08
MY154909A (en) 2015-08-28
US8003800B2 (en) 2011-08-23
CA2635047C (en) 2014-07-29
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IL192657A0 (en) 2009-02-11
AU2007204121A1 (en) 2007-07-19
IL192657A (en) 2015-09-24
RU2437877C2 (ru) 2011-12-27
EP1976512A1 (en) 2008-10-08
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US20100240717A1 (en) 2010-09-23

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