BRPI0514316A - métodos e composições para modulação de atividade de receptor de esfingosina-1-fosfato (s1p) - Google Patents

métodos e composições para modulação de atividade de receptor de esfingosina-1-fosfato (s1p)

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Publication number
BRPI0514316A
BRPI0514316A BRPI0514316-0A BRPI0514316A BRPI0514316A BR PI0514316 A BRPI0514316 A BR PI0514316A BR PI0514316 A BRPI0514316 A BR PI0514316A BR PI0514316 A BRPI0514316 A BR PI0514316A
Authority
BR
Brazil
Prior art keywords
compositions
receptor activity
phosphate
methods
modulating sphingosine
Prior art date
Application number
BRPI0514316-0A
Other languages
English (en)
Inventor
Ashis K Saha
Malcom J Kavarana
Ghotas Evindar
Alexander L Satz
Barry Morgan
Original Assignee
Praecis 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 Praecis Pharm Inc filed Critical Praecis Pharm Inc
Publication of BRPI0514316A publication Critical patent/BRPI0514316A/pt

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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
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    • 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
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    • A—HUMAN NECESSITIES
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    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
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    • C07C237/08—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
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    • C07F9/6536—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6539—Five-membered rings
    • C—CHEMISTRY; METALLURGY
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
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    • C07F9/65517—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms the oxygen atom being part of a five-membered ring condensed with carbocyclic rings or carbocyclic ring systems
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
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    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/6574—Esters of oxyacids of phosphorus
    • C07F9/65742—Esters of oxyacids of phosphorus non-condensed with carbocyclic rings or heterocyclic rings or ring systems
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    • C07C2601/00—Systems containing only non-condensed rings
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    • C07C2601/14—The ring being saturated

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Abstract

MéTODOS E COMPOSIçõES PARA MODULAçãO DE ATIVIDADE DE RECEPTOR DE ESFINGOSINA-1-FOSFATO (S1P) A presente invenção refere-se a compostos que modulam a atividade do receptor de S1P1, o emprego destes compostos para tratamento de condições associadas com sinalização através do receptor de S1P1, e composições farmacêuticas compreendendo estes compostos.
BRPI0514316-0A 2004-08-13 2005-08-12 métodos e composições para modulação de atividade de receptor de esfingosina-1-fosfato (s1p) BRPI0514316A (pt)

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PCT/US2005/028914 WO2006020951A1 (en) 2004-08-13 2005-08-12 Methods and compositions for modulating sphingosine-1-phosphate (s1p) receptor activity

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Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003259296A1 (en) * 2002-07-30 2004-02-16 University Of Virginia Patent Foundation Compounds active in spinigosine 1-phosphate signaling
WO2005041899A2 (en) * 2003-11-03 2005-05-12 University Of Virginia Patent Foundation Orally available sphingosine 1-phosphate receptor agonists and antagonists
CN101905023B (zh) * 2004-07-16 2012-07-11 杏林制药株式会社 有效的医药使用方法及与副作用发生的防御相关的方法
US20060223866A1 (en) * 2004-08-13 2006-10-05 Praecis Pharmaceuticals, Inc. Methods and compositions for modulating sphingosine-1-phosphate (S1P) receptor activity
PL1806338T3 (pl) 2004-10-12 2016-07-29 Kyorin Seiyaku Kk Sposób wytwarzania chlorowodorku 2-amino-2-[2-[4-(3-benzyloksyfenylotio)-2-chlorofenyio]etylo]-1,3-propanodioiu i jego hydratów oraz produkty pośrednie w ich wytwarzaniu
CA2590748A1 (en) * 2004-12-06 2006-06-15 University Of Virginia Patent Foundation Aryl amide sphingosine 1-phosphate analogs
CA2596990A1 (en) 2005-02-14 2006-08-24 University Of Virginia Patent Foundation Sphingosine 1-phosphate agonists comprising cycloalkanes and 5 -membered heterocycles substituted by amino and phenyl groups
GB0513431D0 (en) * 2005-06-30 2005-08-10 Kherion Technology Ltd Prophylactic compositions and uses
SI1932522T1 (sl) * 2005-10-07 2012-08-31 Kyorin Seiyaku Kk Terapevtsko sredstvo za jetrno bolezen, ki vsebuje 2-amino-1,3- propandiolni derivat kot aktivno sestavino
US7919519B2 (en) * 2005-11-23 2011-04-05 Epix Pharmaceuticals Inc. S1P receptor modulating compounds and use thereof
CA2630714C (en) * 2005-11-23 2014-01-14 Epix Delaware, Inc. S1p receptor modulating compounds and use thereof
KR20080086546A (ko) 2006-01-27 2008-09-25 유니버시티 오브 버지니아 페이턴트 파운데이션 신경병증성 통증의 치료 방법
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
WO2007092638A1 (en) * 2006-02-09 2007-08-16 University Of Virginia Patent Foundation Bicyclic sphingosine 1-phosphate analogs
WO2007109330A2 (en) * 2006-03-21 2007-09-27 Epix Delaware, Inc. S1p receptor modulating compounds
US20100016260A1 (en) * 2006-08-01 2010-01-21 Praecis Pharmaceuticals Incorporated Agonists of sphingosine-1 phosphate receptor (slp)
TW200823182A (en) * 2006-08-01 2008-06-01 Praecis Pharm Inc Chemical compounds
JP2009545630A (ja) * 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 化合物
RU2430925C2 (ru) 2006-08-08 2011-10-10 Киорин Фармасьютикал Ко., Лтд. Производное аминофосфата и модулятор рецептора s1p, содержащий его в качестве активного ингредиента
CA2659599C (en) 2006-08-08 2014-06-17 Kyorin Pharmaceutical Co., Ltd. Amino alcohol derivative and immunosuppressive agent having same as an active ingredient
WO2008024196A1 (en) * 2006-08-24 2008-02-28 Praecis Pharmaceuticals Incorporated Chemical compounds
JP2010510250A (ja) 2006-11-21 2010-04-02 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−燐酸受容体アゴニスト活性を有するヒドリンダンアナログ
AU2007323618A1 (en) 2006-11-21 2008-05-29 University Of Virginia Patent Foundation Tetralin analogs having sphingosine 1-phosphate agonist activity
JP2010510251A (ja) 2006-11-21 2010-04-02 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−燐酸受容体活性を有するベンゾシクロヘプチルアナログ
EP1969934A1 (de) * 2007-03-12 2008-09-17 Bayer CropScience AG 4-Cycloalkyl-oder 4-arylsubstituierte Phenoxyphenylamidine und deren Verwendung als Fungizide
ATE505454T1 (de) * 2007-09-20 2011-04-15 Amgen Inc 1-(4-(4-benzylbenzamid)-benzyl)-azetidin-3- carboxylsäurederivate und entsprechende verbindungen als s1p-rezeptor-modulatoren zur behandlung von immunerkrankungen
GB0802227D0 (en) * 2008-02-06 2008-03-12 Glaxo Group Ltd Compound
JP5452237B2 (ja) 2008-02-07 2014-03-26 杏林製薬株式会社 アミノアルコール誘導体を有効成分とする炎症性腸疾患の治療剤又は予防剤
US8212010B2 (en) * 2008-02-25 2012-07-03 Expression Drug Designs, Llc Sphingosine 1-phosphate antagonism
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
PL2342205T4 (pl) 2008-08-27 2016-12-30 Podstawione tricykliczne pochodne kwasowe jako antagoniści receptora S1P1 użyteczni w leczeniu zaburzeń autoimmunologicznych i zapalnych
EP2354134B1 (en) * 2008-12-05 2016-02-24 Astellas Pharma Inc. 2h-chromene derivatives as stimulators of sphingosine 1-phosphate receptor
RU2505539C2 (ru) 2008-12-23 2014-01-27 Эбботт Лэборетриз Антивирусные соединения
CN102264737A (zh) 2008-12-23 2011-11-30 雅培制药有限公司 抗病毒化合物
WO2010120935A1 (en) 2009-04-15 2010-10-21 Abbott Laboratories Anti-viral compounds
US8937150B2 (en) 2009-06-11 2015-01-20 Abbvie Inc. Anti-viral compounds
US8716454B2 (en) 2009-06-11 2014-05-06 Abbvie Inc. Solid compositions
US9394279B2 (en) 2009-06-11 2016-07-19 Abbvie Inc. Anti-viral compounds
EP2853531A3 (en) 2009-06-11 2015-08-12 AbbVie Bahamas Ltd. Antiviral compounds
JP5773585B2 (ja) * 2009-06-29 2015-09-02 日東電工株式会社 発光性トリアリール
WO2011008560A1 (en) 2009-06-29 2011-01-20 Nitto Denko Corporation Emissive aryl-heteroaryl compounds
EP2528894A1 (en) 2010-01-27 2012-12-05 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
NZ605440A (en) 2010-06-10 2014-05-30 Abbvie Bahamas Ltd Solid compositions comprising an hcv inhibitor
US10201584B1 (en) 2011-05-17 2019-02-12 Abbvie Inc. Compositions and methods for treating HCV
US9073881B2 (en) 2011-09-23 2015-07-07 Hoffmann-La Roche Inc. Benzoic acid derivatives
US9034832B2 (en) 2011-12-29 2015-05-19 Abbvie Inc. Solid compositions
EP2842937B1 (en) 2012-04-23 2018-01-17 Mitsubishi Tanabe Pharma Corporation Amine compound and use thereof for medical purposes
US11484534B2 (en) 2013-03-14 2022-11-01 Abbvie Inc. Methods for treating HCV
WO2015103490A1 (en) 2014-01-03 2015-07-09 Abbvie, Inc. Solid antiviral dosage forms
CA3002540C (en) 2015-01-06 2023-11-07 Arena Pharmaceuticals, Inc. Use of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid for treating conditions related to the s1p1 receptor
JP6838744B2 (ja) 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 S1P1レセプター関連障害における使用のための(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(化合物1)の結晶性L−アルギニン塩
EP3352753A4 (en) * 2015-09-24 2019-03-13 The Regents of The University of California SYNTHETIC SPHINGOLIPIDE-SIMILAR MOLECULES, MEDICAMENTS, METHODS FOR THEIR SYNTHESIS AND TREATMENT PROCEDURES
CN110520124A (zh) 2017-02-16 2019-11-29 艾尼纳制药公司 用于治疗原发性胆汁性胆管炎的化合物和方法
KR20190113955A (ko) 2017-02-16 2019-10-08 아레나 파마슈티칼스, 인크. 장-외 증상을 갖는 염증성 장질환의 치료를 위한 화합물 및 방법
CN107540623B (zh) * 2017-08-29 2020-02-07 河南大学 一种高对映选择性C-5位α-立体中心4-硝基异恶唑醇类化合物、其制备方法及应用
GB201715786D0 (en) 2017-09-29 2017-11-15 Univ College Cardiff Consultants Ltd Compounds
JP7397011B2 (ja) 2018-06-06 2023-12-12 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 S1p1受容体に関連する状態を治療する方法
CN112351969A (zh) 2018-06-21 2021-02-09 塞莱斯蒂亚生物技术股份公司 用于制备氨基二芳基醚和氨基二芳基醚盐酸盐的方法
EP3847158B1 (en) 2018-09-06 2026-06-24 Arena Pharmaceuticals, Inc. Compounds useful in the treatment of autoimmune and inflammatory disorders
AU2019387370A1 (en) 2018-11-30 2021-06-10 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
CN113966324B (zh) * 2019-04-10 2024-09-03 塞莱斯蒂亚生物技术股份公司 Notch信号传导途径抑制剂及其在癌症治疗的用途
JP2024510435A (ja) 2021-03-18 2024-03-07 シージェン インコーポレイテッド 生体活性化合物の内部移行複合体からの選択的薬物放出

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2406366A (en) * 1942-07-31 1946-08-27 John N Graef Camera
US2423579A (en) * 1945-02-02 1947-07-08 Asa J Buren Corrugated belting
KR0155015B1 (ko) * 1992-10-21 1998-12-01 고우야 마사시 2-아미노-1,3-프로판디올 화합물 및 면역 억제제
US5948820A (en) * 1994-08-22 1999-09-07 Yoshitomi Pharmaceutical Industries, Ltd. Benzene compound and pharmaceutical use thereof
ES2240868T3 (es) * 1997-04-04 2005-10-16 Mitsubishi Pharma Corporation Compuesto de 2-aminopropano -1,3-diol, su uso farmaceutico e intermedios en su sintesis.
US6288105B1 (en) * 1997-04-30 2001-09-11 Eli Lilly And Company Antithrombotic agents
JPH1180026A (ja) * 1997-09-02 1999-03-23 Yoshitomi Pharmaceut Ind Ltd 新規免疫抑制剤、その使用方法およびその同定方法
US6830916B2 (en) * 2000-03-02 2004-12-14 Sarah Spiegel Sphingosine kinase, cloning, expression and methods of use
CA2402038C (en) * 2000-03-17 2011-03-15 The University Of Tennessee Research Corporation Lpa receptor agonists and antagonists and methods of use
WO2002018395A1 (en) 2000-08-31 2002-03-07 Merck & Co., Inc. Phosphate derivatives as immunoregulatory agents
US20020072502A1 (en) * 2000-09-01 2002-06-13 Neuronyx, Inc. Novel synthetic gangliosides
EP1361872A4 (en) * 2000-10-03 2004-05-19 Univ Virginia NEW LYSOPHOSPHIC ACID RECEPTOR AGONISTS AND ANTAGONISTS
US6881546B2 (en) * 2000-12-22 2005-04-19 Medlyte, Inc., Sdsu Heart Institute Compositions and methods for the treatment and prevention of cardiovascular diseases and disorders, and for identifying agents therapeutic therefor
WO2002057311A2 (en) * 2000-12-22 2002-07-25 University Of South Florida Sphingosine 1-phosphate receptor gene, sppr
JP2004529100A (ja) 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 スフィンゴシン−1−ホスフェートレセプターのアゴニストおよびアンタゴニスト
MXPA03008755A (es) 2001-03-26 2004-02-18 Novartis Ag Derivados de 2-amino-propanol.
KR100913269B1 (ko) 2001-09-27 2009-08-21 교린 세이야꾸 가부시키 가이샤 디아릴 황화물 유도체, 그의 염 및 이를 이용한 면역억제제
DE60329073D1 (de) 2002-01-18 2009-10-15 Merck & Co Inc Edg-rezeptoragonisten
EP1469863A2 (en) 2002-01-18 2004-10-27 Merck & Co., Inc. Selective s1p1/edg1 receptor agonists
JP5227492B2 (ja) 2002-05-16 2013-07-03 ノバルティス アーゲー 癌におけるedgレセプター結合剤の使用
WO2003099192A2 (en) * 2002-05-27 2003-12-04 Novartis Ag Bis-aromatic alkanols
WO2003105840A2 (en) * 2002-06-17 2003-12-24 The Pennsylvania State Research Foundation Sphingosine kinase inhibitors
GB0217152D0 (en) 2002-07-24 2002-09-04 Novartis Ag Organic compounds
AU2003259296A1 (en) 2002-07-30 2004-02-16 University Of Virginia Patent Foundation Compounds active in spinigosine 1-phosphate signaling
US6969692B2 (en) * 2002-08-28 2005-11-29 Albemarle Netherlands B.V. Process for the preparation of doped pentasil-type zeolites using a doped reactant
CN100516024C (zh) 2002-09-13 2009-07-22 诺瓦提斯公司 氨基-丙醇衍生物
JP4571497B2 (ja) 2002-09-19 2010-10-27 杏林製薬株式会社 アミノアルコール誘導体とその付加塩及び免疫抑制剤
ATE496024T1 (de) 2002-12-20 2011-02-15 Merck Sharp & Dohme 1-(amino)indane als edg-rezeptoragonisten
WO2004061107A1 (ja) 2002-12-27 2004-07-22 The New Industry Research Organization スフィンゴシンキナーゼ2を利用した細胞増殖抑制剤、その核移行シグナルを持つ融合タンパク質の作製方法、及び薬剤候補物質のスクリーニング方法、並びにスクリーニングキット
DK1602660T3 (da) 2003-02-18 2011-05-23 Kyorin Seiyaku Kk Aminophosphonsyrederivater, additionssalte deraf og S1P-receptormodulatorer
AU2004234067B2 (en) 2003-04-30 2008-02-28 Novartis Ag Aminopropanol derivatives as sphingosine-1-phosphate receptor modulators
AU2004234066B2 (en) 2003-04-30 2008-02-21 Novartis Ag Amino-propanol derivatives as sphingosine-1-phosphate receptor modulator
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
EP1628967B1 (en) 2003-05-19 2014-04-09 Irm Llc Immunosuppressant compounds and compositions
GB0313612D0 (en) 2003-06-12 2003-07-16 Novartis Ag Organic compounds
WO2005041899A2 (en) 2003-11-03 2005-05-12 University Of Virginia Patent Foundation Orally available sphingosine 1-phosphate receptor agonists and antagonists
BRPI0416752B8 (pt) 2003-11-21 2021-05-25 Actelion Pharmaceuticals Ltd composição farmacêutica, uso de um ou mais compostos, e, compostos
GB0405289D0 (en) 2004-03-09 2004-04-21 Novartis Ag Organic compounds
EP1750722A4 (en) 2004-05-06 2010-03-10 Univ Virginia NEW LYSOPHOSPHIC ACID RECEPTORSELECTIVE ANTAGONISTS
GB0411929D0 (en) 2004-05-27 2004-06-30 Novartis Ag Organic compounds
CN101905023B (zh) 2004-07-16 2012-07-11 杏林制药株式会社 有效的医药使用方法及与副作用发生的防御相关的方法
WO2006010379A1 (en) 2004-07-29 2006-02-02 Actelion Pharmaceuticals Ltd. Novel thiophene derivatives as immunosuppressive agents
CA2583681A1 (en) 2004-10-22 2006-05-04 Merck & Co., Inc. 2-(aryl)azacyclylmethyl carboxylates, sulfonates, phosphonates, phosphinates and heterocycles as s1p receptor agonists
US8440627B2 (en) 2004-11-04 2013-05-14 Tufts Medical Center, Inc. G protein coupled receptor agonists and antagonists and methods of use
EP2384749A1 (en) 2004-11-29 2011-11-09 Novartis AG Dosage regimen of an S1P receptor agonist
CA2590748A1 (en) 2004-12-06 2006-06-15 University Of Virginia Patent Foundation Aryl amide sphingosine 1-phosphate analogs
CA2591399C (en) 2004-12-13 2014-05-20 Ono Pharmaceutical Co., Ltd. Aminocarboxylic acid derivative and medicinal use thereof

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WO2006020951A1 (en) 2006-02-23
MX2007001661A (es) 2007-04-23
KR20070058455A (ko) 2007-06-08
US20080064662A1 (en) 2008-03-13
JP2008509931A (ja) 2008-04-03
RU2007109207A (ru) 2008-09-20
CA2576388A1 (en) 2006-02-23
EP1781595A1 (en) 2007-05-09
AU2005272619A1 (en) 2006-02-23
US20060135786A1 (en) 2006-06-22
US7241812B2 (en) 2007-07-10
NO20071054L (no) 2007-05-10

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