CN102875413A - 免疫抑制剂化合物及组合物 - Google Patents

免疫抑制剂化合物及组合物 Download PDF

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CN102875413A
CN102875413A CN2012103237490A CN201210323749A CN102875413A CN 102875413 A CN102875413 A CN 102875413A CN 2012103237490 A CN2012103237490 A CN 2012103237490A CN 201210323749 A CN201210323749 A CN 201210323749A CN 102875413 A CN102875413 A CN 102875413A
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ethyl
benzyl
amino
propionic acid
trifluoromethyl
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潘世风
高文奇
N·S·格雷
米媛
范毅
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IRM LLC
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IRM LLC
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Publication of CN102875413A publication Critical patent/CN102875413A/zh
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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111107837A (zh) * 2017-09-27 2020-05-05 诺华股份有限公司 包含西普尼莫德的肠胃外制剂
CN119564675A (zh) * 2024-12-25 2025-03-07 合肥工业大学 一种小分子化合物在制备细胞焦亡抑制剂中的应用
WO2025077706A1 (zh) * 2023-10-08 2025-04-17 华东师范大学 用于肌病治疗的s1pr4调节剂化合物及其应用

Families Citing this family (105)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2533587A1 (en) 2002-07-30 2004-02-05 University Of Virginia Patent Foundation Compounds active in sphingosine 1-phosphate signaling
AU2011224085B2 (en) * 2003-05-19 2013-03-07 Novartis Ag Immunosuppressant compounds and compositions
MY150088A (en) * 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
BRPI0413923A (pt) * 2003-08-29 2006-11-07 Ono Pharmaceutical Co composto capaz de ligar o receptor de s1p e uso farmacêutico do mesmo
US7638637B2 (en) 2003-11-03 2009-12-29 University Of Virginia Patent Foundation Orally available sphingosine 1-phosphate receptor agonists and antagonists
GB0500020D0 (en) 2005-01-04 2005-02-09 Novartis Ag Organic compounds
CN1922135B (zh) * 2004-02-24 2011-07-06 Irm责任有限公司 免疫抑制剂化合物和组合物
TW200538433A (en) * 2004-02-24 2005-12-01 Irm Llc Immunosuppressant compounds and compositiions
NZ554720A (en) 2004-11-29 2011-04-29 Novartis Ag Compositions and uses of fingolimod (2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol)
JP2008530135A (ja) 2005-02-14 2008-08-07 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 アミノ基およびフェニル基で置換されたシクロアルカンならびに5員の複素環を含むスフィンゴシン=1−リン酸アゴニスト
GB0504544D0 (en) * 2005-03-04 2005-04-13 Novartis Ag Organic compounds
RU2382781C2 (ru) * 2005-04-22 2010-02-27 Дайити Санкио Компани, Лимитед Гетероциклическое соединение
GB0510390D0 (en) * 2005-05-20 2005-06-29 Novartis Ag Organic compounds
CA2640366A1 (en) 2006-01-27 2007-08-09 University Of Virginia Patent Foundation Method for treatment of neuropathic pain
WO2007092638A1 (en) 2006-02-09 2007-08-16 University Of Virginia Patent Foundation Bicyclic sphingosine 1-phosphate analogs
WO2007112322A2 (en) 2006-03-28 2007-10-04 Allergan, Inc. Indole compounds having sphingosine-1-phosphate (s1p) receptor agonist and/or antagonist biological activity
GB0612721D0 (en) 2006-06-27 2006-08-09 Novartis Ag Organic compounds
KR101339976B1 (ko) 2006-08-08 2013-12-10 교린 세이야꾸 가부시키 가이샤 아미노인산에스테르 유도체 및 그들을 유효성분으로 하는 s1p 수용체 조절제
KR20090041424A (ko) 2006-08-08 2009-04-28 교린 세이야꾸 가부시키 가이샤 아미노알코올 유도체 및 그것들을 유효성분으로 하는 면역 억제제
JP2009269819A (ja) * 2006-08-25 2009-11-19 Asahi Kasei Pharma Kk アミン化合物
AU2007323557A1 (en) 2006-11-21 2008-05-29 University Of Virginia Patent Foundation Benzocycloheptyl analogs having sphingosine 1-phosphate receptor activity
CA2669104A1 (en) 2006-11-21 2008-05-29 University Of Virginia Patent Foundation Hydrindane analogs having sphingosine 1-phosphate receptor agonist activity
CA2669102A1 (en) 2006-11-21 2008-05-29 University Of Virginia Patent Foundation Tetralin analogs having sphingosine 1-phosphate agonist activity
US8524917B2 (en) 2007-01-11 2013-09-03 Allergan, Inc. 6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
JP2010526116A (ja) 2007-05-04 2010-07-29 ノバルティス アーゲー S1p受容体調節因子の使用
JP2010540543A (ja) 2007-09-24 2010-12-24 アラーガン インコーポレイテッド スフィンゴシン‐1‐リン酸(s1p)レセプター生物学的活性を有するアリールまたはヘテロアリール基を担持するインドール化合物
HUE027696T2 (en) 2007-10-12 2016-10-28 Novartis Ag Preparations containing sphingosine-1-phosphate (S1P) receptor modulators
GB0725101D0 (en) * 2007-12-21 2008-01-30 Glaxo Group Ltd Compounds
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
RU2519660C2 (ru) 2008-03-17 2014-06-20 Актелион Фармасьютиклз Лтд Режим дозировки селективного агониста рецептора s1p1
GB0807910D0 (en) * 2008-04-30 2008-06-04 Glaxo Group Ltd Compounds
RU2010149311A (ru) 2008-05-08 2012-06-20 Аллерган, Инк. (Us) ТЕРАПЕВТИЧЕСКИ ПОЛЕЗНЫЕ ЗАМЕЩЕННЫЕ 1,7-ДИФЕНИЛ-1,2,3,5,6,7-ГЕКСАГИДРОПИРИДО [3,2,1-ij]ХИНОЛИНОВЫЕ СОЕДИНЕНИЯ
US8143291B2 (en) 2008-05-09 2012-03-27 Allergan, Inc. Indole compounds bearing aryl or heteroaryl groups having sphingosine-1-phosphate (S1P) receptor biological activity
PT2300013T (pt) 2008-05-21 2017-10-31 Ariad Pharma Inc Derivados de fósforo como inibidores de cinases
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
DK2307007T3 (da) * 2008-07-23 2014-11-10 Novartis Ag Sphingosin-1-phosphat-receptormodulatorer samt deres anvendelse til behandling af muskelinflammation
AU2013209344B2 (en) * 2008-07-23 2015-12-24 Novartis Ag Sphingosine 1 phosphate receptor modulators and their use to treat muscle inflammation
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
EP2326325B1 (en) 2008-08-18 2014-11-12 Novartis AG Azetidine derivative for the treatment of peripheral neuropathies
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
BRPI0922457A2 (pt) * 2008-12-18 2015-12-15 Novartis Ag forma polimórfica de ácido 1-(4-{1-[(e)-4-ciclo-hexil-3-trifluormetil-benziloxi-imino]-etil)-2-etil-benzil)-azetidino-3-carboxílico"
ES2478842T3 (es) 2008-12-18 2014-07-23 Novartis Ag Sal clorhidrato del ácido 1-(4-(1-((E)-4-ciclohexil-3-trifluorometil-benziloxiimino)-etil)-2-etil-benzil)-azetidina-3-carboxílico
US20120115840A1 (en) 2008-12-18 2012-05-10 Lech Ciszewski Hemifumarate salt of 1-[4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl]-azetidine-3-carboxylic acid
CA2981830A1 (en) * 2008-12-22 2010-07-01 Novartis Ag Dosage regimen of an s1p receptor agonist
US8399451B2 (en) 2009-08-07 2013-03-19 Bristol-Myers Squibb Company Heterocyclic 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
CA2789480A1 (en) 2010-03-03 2011-09-09 Arena Pharmaceuticals, Inc. Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof
WO2011116091A1 (en) 2010-03-17 2011-09-22 Novartis Ag Dispenser
EP2560969B1 (en) 2010-04-23 2015-08-12 Bristol-Myers Squibb Company 4-(5-isoxazolyl or 5-pyrrazolyl-1,2,4-oxadiazol-3-yl)-mandelic acid amides as sphingosin-1-phosphate 1 receptor agonists
ES2548258T3 (es) 2010-09-24 2015-10-15 Bristol-Myers Squibb Company Compuestos de oxadiazol sustituidos y su uso como agonistas de S1P1
EP2646018B1 (en) 2010-12-03 2014-10-22 Allergan, Inc. Novel oxime azetidine derivatives as sphingosine 1-phosphate (s1p) receptor modulators
AU2011336970A1 (en) 2010-12-03 2013-07-11 Allergan, Inc. Novel oxime derivatives as sphingosine 1-phosphate (S1P) receptor modulators
JP5617799B2 (ja) 2010-12-07 2014-11-05 信越化学工業株式会社 化学増幅レジスト材料及びパターン形成方法
KR101951966B1 (ko) 2011-01-07 2019-02-25 노파르티스 아게 면역억제제 제제
WO2012095853A1 (en) 2011-01-10 2012-07-19 Novartis Pharma Ag Modified release formulations comprising sip receptor modulators
EA201391626A1 (ru) 2011-05-04 2014-03-31 Ариад Фармасьютикалз, Инк. Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака
CN103889408A (zh) 2011-10-21 2014-06-25 诺华股份有限公司 S1p受体调节剂或激动剂的剂量方案
CA2862375A1 (en) 2012-02-03 2013-08-08 Novartis Ag Process for preparing n-(4-cyclohexyl-3-trifluoromethyl-benzyloxy)-acetimidic acid ethyl ester
AU2013204563B2 (en) 2012-05-05 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
US20160046573A1 (en) * 2013-04-04 2016-02-18 Novartis Ag Identifying patient response to s1p receptor modulator administration
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
WO2014175287A1 (ja) * 2013-04-26 2014-10-30 国立大学法人 京都大学 脳動脈瘤の形成および/または増大の抑制若しくは縮小用医薬組成物
EP2862574A1 (en) 2013-10-15 2015-04-22 Sanofi {4-[5-(3-chloro-phenoxy)-oxazolo[5,4 d]pyrimidin-2-yl]-2,6-dimethyl-phenoxy}-acetic acid for use in the prevention or treatment of acute kidney injury
WO2015109391A1 (en) 2014-01-24 2015-07-30 Children's Hospital Of Eastern Ontario Research Institute Inc. Smc combination therapy for the treatment of cancer
DK3102576T3 (da) 2014-02-03 2019-07-22 Vitae Pharmaceuticals Llc Dihydropyrrolopyridininhibitorer af ror-gamma
MX371304B (es) 2014-10-14 2020-01-24 Vitae Pharmaceuticals Llc Dihidropirrolopiridinas inhibidoras del receptor huérfano-gamma.
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
US9845308B2 (en) 2014-11-05 2017-12-19 Vitae Pharmaceuticals, Inc. Isoindoline inhibitors of ROR-gamma
WO2016112075A1 (en) 2015-01-06 2016-07-14 Arena Pharmaceuticals, Inc. Methods of treating conditions related to the s1p1 receptor
WO2016135644A1 (en) 2015-02-26 2016-09-01 Novartis Ag Treatment of autoimmune disease in a patient receiving additionally a beta-blocker
KR102603199B1 (ko) 2015-06-22 2023-11-16 아레나 파마슈티칼스, 인크. S1p1 수용체-관련 장애에서의 사용을 위한 (r)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[b]인돌-3-일)아세트산 (화합물 1)의 결정성 l-아르기닌 염
WO2017024018A1 (en) 2015-08-05 2017-02-09 Vitae Pharmaceuticals, Inc. Modulators of ror-gamma
AU2016355710B2 (en) 2015-11-20 2021-03-25 Vitae Pharmaceuticals, Llc Modulators of ROR-gamma
US20190047951A1 (en) 2016-01-04 2019-02-14 Auspex Pharmaceuticals, Inc. Azetidine modulators of the sphingosine 1-phosphate receptor
TW202220968A (zh) 2016-01-29 2022-06-01 美商維它藥物有限責任公司 ROR-γ調節劑
US9481674B1 (en) 2016-06-10 2016-11-01 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
MA47503A (fr) 2017-02-16 2021-04-21 Arena Pharm Inc Composés et méthodes pour le traitement de maladies inflammatoires chroniques de l'intestin avec manifestations extra-intestinales
MA47504A (fr) 2017-02-16 2019-12-25 Arena Pharm Inc Composés et méthodes de traitement de l'angiocholite biliaire primitive
US11629124B2 (en) 2017-03-09 2023-04-18 Novartis Ag Solid forms comprising an oxime ether compound, compositions and methods of use thereof
US11958805B2 (en) 2017-03-09 2024-04-16 Novartis Ag Solid forms comprising an oxime ether compound, compositions and methods of use thereof
US11434200B2 (en) 2017-03-09 2022-09-06 Novartis Ag Solid forms comprising an oxime ether compound and a coformer, compositions and methods of use thereof
UA126583C2 (uk) 2017-07-24 2022-11-02 Вітае Фармасьютікалс, Ллс ІНГІБІТОРИ ROR<font face="Symbol">g</font>
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
US11390583B2 (en) 2017-09-27 2022-07-19 Dr. Reddy's Laboratories Limited Process for preparation of Siponimod, its salts and solid state forms thereof
WO2019064212A1 (en) 2017-09-29 2019-04-04 Novartis Ag DOSAGE DIAGRAM OF SIPONIMOD
CA3074416A1 (en) 2017-09-29 2019-04-04 Novartis Ag Dosing regimen of siponimod
WO2019144094A1 (en) 2018-01-22 2019-07-25 Teva Pharmaceuticals International Gmbh Crystalline siponimod fumaric acid and polymorphs thereof
CN112601516A (zh) 2018-06-06 2021-04-02 艾尼纳制药公司 治疗与s1p1受体相关的病况的方法
US11555015B2 (en) 2018-09-06 2023-01-17 Arena Pharmaceuticals, Inc. Compounds useful in the treatment of autoimmune and inflammatory disorders
CN111630029B (zh) * 2018-12-06 2021-04-30 上海济煜医药科技有限公司 作为免疫调节剂的化合物及其制备方法和应用
US12410126B2 (en) 2019-03-29 2025-09-09 Synthon B.V. Process for making Siponimod and intermediate thereof
WO2020208167A1 (en) 2019-04-11 2020-10-15 Synthon B.V. Solid forms of siponimod
EP3972954A1 (en) 2019-05-21 2022-03-30 Synthon B.V. Siponimod maleic acid and fumaric acid salt
CN112745244B (zh) * 2019-10-30 2024-05-03 苏州科伦药物研究有限公司 一种辛波莫德的中间体及其合成方法
EP4051250A1 (en) 2019-10-31 2022-09-07 Idorsia Pharmaceuticals Ltd Combination of a cxcr7 antagonist with an s1p1 receptor modulator
EP4483960A3 (en) 2020-02-06 2025-03-05 Mitsubishi Tanabe Pharma Corporation Therapeutic agent for myalgic encephalomyelitis/chronic fatigue syndrome
WO2021158838A1 (en) 2020-02-07 2021-08-12 Argentum Pharmaceuticals Llc Dosage regimen of an s1p receptor modulator
WO2021214717A1 (en) 2020-04-23 2021-10-28 Novartis Ag Dosing regimen for the use of siponimod for the treatment of acute respiratory distress syndrome
WO2021240547A2 (en) 2020-05-29 2021-12-02 Cipla Limited Methods for the preparation of sphingosine 1-phosphate receptor modulators and solid forms thereof
IT202000019897A1 (it) 2020-08-10 2022-02-10 Olon Spa Procedimento per la preparazione di un intermedio chiave del siponimod
CA3197026A1 (en) 2020-09-25 2022-03-31 Bohumil Dymacek Siponimod salts and cocrystals
EP4313941A1 (en) 2021-03-26 2024-02-07 OLON S.p.A. Novel crystalline compound of siponimod hemifumarate
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
WO2024126409A1 (en) 2022-12-12 2024-06-20 Synthon B.V. Pharmaceutical composition of siponimod
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

Family Cites Families (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR901228A (fr) 1943-01-16 1945-07-20 Deutsche Edelstahlwerke Ag Système d'aimant à entrefer annulaire
CH540247A (de) * 1967-04-21 1973-09-28 Ciba Geigy Ag Verfahren zur Herstellung von heterocyclischen, Asthylendoppelbindungen enthaltenden Verbindungen
US3872113A (en) * 1972-05-30 1975-03-18 Endo Lab Hydroxy- and acetoxy-phthalaldehydric acid, O-(substituted) oximes
IL86632A0 (en) 1987-06-15 1988-11-30 Ciba Geigy Ag Derivatives substituted at methyl-amino nitrogen
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
DK0528762T3 (da) 1991-08-15 1997-08-25 Ciba Geigy Ag N-acyl-N-heterocyclyl- eller naphthylalkyl-aminosyrer som angiotensin II antagonister
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
TW225528B (enExample) 1992-04-03 1994-06-21 Ciba Geigy Ag
JP3398382B2 (ja) 1992-10-28 2003-04-21 ジェネンテク,インコーポレイテッド 血管内皮細胞増殖因子アンタゴニスト
IL109161A0 (en) 1993-03-31 1994-06-24 Cell Therapeutics Inc Amino alcohol derivatives, methods for the preparation thereof, and pharmaceutical compositions containing the same
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
IL110172A (en) 1993-07-22 2001-10-31 Lilly Co Eli Bicyclic compounds and pharmaceutical compositions containing them
US5362718A (en) 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
CA2198242A1 (en) 1994-08-24 1996-02-29 Eli Lilly And Company Pyrrolidinyl di-carboxylic acid derivatives as metabotropic glutamate receptor antagonists
EP0817775B1 (en) 1995-03-30 2001-09-12 Pfizer Inc. Quinazoline derivatives
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
HUP9900330A3 (en) 1995-07-06 2001-08-28 Novartis Ag Pyrrolopyrimidines and processes for the preparation thereof
US5688798A (en) 1995-10-10 1997-11-18 Hoffmann-La Roche Inc. Pyrimidine compounds
HU222986B1 (hu) * 1995-12-22 2004-01-28 Warner-Lambert Co. A mátrix metalloproteinázok működését gátló aromás ketosavak és azok származékai
IL125033A0 (en) 1995-12-29 1999-01-26 Smithkline Beecham Corp Vitronectin receptor antagonists
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
CN1145614C (zh) 1996-04-12 2004-04-14 沃尼尔·朗伯公司 酪氨酸激酶的不可逆抑制剂,其制药用途及药物组合物
CA2258548C (en) 1996-06-24 2005-07-26 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
US6258823B1 (en) 1996-07-12 2001-07-10 Ariad Pharmaceuticals, Inc. Materials and method for treating or preventing pathogenic fungal infection
JPH11209277A (ja) 1998-01-19 1999-08-03 Yoshitomi Pharmaceut Ind Ltd 医薬組成物
DE19638745C2 (de) 1996-09-11 2001-05-10 Schering Ag Monoklonale Antikörper gegen die extrazelluläre Domäne des menschlichen VEGF - Rezeptorproteins (KDR)
AU4342997A (en) 1996-09-13 1998-04-02 Sugen, Inc. Use of quinazoline derivatives for the manufacture of a medicament in the reatment of hyperproliferative skin disorders
EP0837063A1 (en) 1996-10-17 1998-04-22 Pfizer Inc. 4-Aminoquinazoline derivatives
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
DK1002792T3 (da) 1997-04-04 2004-11-22 Mitsubishi Pharma Corp 2-aminopropan-1,3-diolforbindelser, medicinsk anvendelse deraf og mellemprodukter til syntese af disse
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
TW557297B (en) 1997-09-26 2003-10-11 Abbott Lab Rapamycin analogs having immunomodulatory activity, and pharmaceutical compositions containing same
GB9721069D0 (en) 1997-10-03 1997-12-03 Pharmacia & Upjohn Spa Polymeric derivatives of camptothecin
WO1999036415A1 (en) * 1998-01-16 1999-07-22 Centaur Pharmaceuticals, Inc. Thioether furan nitrone compounds
JP2002505868A (ja) * 1998-03-09 2002-02-26 スミスクライン・ビーチャム・コーポレイション ヒトEDG−1cポリヌクレオチドおよびポリペプチドおよびその使用法
ES2342240T3 (es) 1998-08-11 2010-07-02 Novartis Ag Derivados de isoquinolina con actividad que inhibe la angiogenia.
US6630998B1 (en) * 1998-08-13 2003-10-07 Acushnet Company Apparatus and method for automated game ball inspection
UA71587C2 (uk) 1998-11-10 2004-12-15 Шерінг Акцієнгезелльшафт Аміди антранілової кислоти та їхнє застосування як лікарських засобів
GB9824579D0 (en) 1998-11-10 1999-01-06 Novartis Ag Organic compounds
EP1133467B1 (en) * 1998-12-04 2004-09-15 Neurosearch A/S Ion channel modulating agents
IL143596A0 (en) 1998-12-22 2002-04-21 Genentech Inc Vascular endothelial cell growth factor antagonists and uses thereof
AU766081B2 (en) 1999-03-30 2003-10-09 Novartis Ag Phthalazine derivatives for treating inflammatory diseases
TR200102810T2 (tr) 1999-04-01 2002-01-21 Pfizer Products Inc. Sorbitol dehidrojenaz inhibitörleri olarak aminopirimidinler
UA73307C2 (uk) 1999-08-05 2005-07-15 Куміаі Кемікал Індастрі Ко., Лтд. Похідна карбамату і фунгіцид сільськогосподарського/садівницького призначення
EP1212331B1 (en) 1999-08-24 2004-04-21 Ariad Gene Therapeutics, Inc. 28-epirapalogs
JP2001151771A (ja) 1999-09-10 2001-06-05 Kyowa Hakko Kogyo Co Ltd 含窒素芳香族複素環誘導体
AU8533101A (en) 2000-08-31 2002-03-13 Merck & Co Inc Phosphate derivatives as immunoregulatory agents
JP2002167371A (ja) * 2000-09-21 2002-06-11 Sankyo Co Ltd フェニルプロピオン酸誘導体
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
TWI311133B (en) 2001-04-20 2009-06-21 Eisai R&D Man Co Ltd Carboxylic acid derivativeand the salt thereof
EP1391199B1 (en) 2001-05-10 2008-12-10 Ono Pharmaceutical Co., Ltd. Carboxylic acid derivatives and drugs containing the same as the active ingredient
JP3714205B2 (ja) 2001-07-10 2005-11-09 ソニー株式会社 非水電解液二次電池
WO2003018578A1 (en) 2001-08-27 2003-03-06 Aurobindo Pharma Ltd. Method for producing beta form of crystalline anhydrous aztreonam
JP2003073357A (ja) 2001-09-03 2003-03-12 Mitsubishi Pharma Corp アミド化合物を含有するRhoキナーゼ阻害剤
US20040235866A1 (en) 2001-09-05 2004-11-25 Takahisa Hanada Lymphocytic activation inhibitor and remedial agent for autoimmune disease
WO2003037271A2 (en) 2001-10-30 2003-05-08 Millennium Pharmaceuticals,Inc. Compounds, pharmaceutical compositions and methods of use therefor
DE60329073D1 (de) 2002-01-18 2009-10-15 Merck & Co Inc Edg-rezeptoragonisten
AU2003216054B2 (en) 2002-01-18 2007-01-04 Merck & Co., Inc. Selective S1P1/Edg1 receptor agonists
US20030207924A1 (en) 2002-03-07 2003-11-06 Xue-Min Cheng Compounds that modulate PPAR activity and methods of preparation
KR100681585B1 (ko) 2002-04-26 2007-02-09 에프. 호프만-라 로슈 아게 아이소퀴놀린 유도체
WO2003099769A1 (en) * 2002-05-24 2003-12-04 Pharmacia Corporation Anilino liver x-receptor modulators
WO2003099192A2 (en) * 2002-05-27 2003-12-04 Novartis Ag Bis-aromatic alkanols
US6846832B2 (en) 2002-08-07 2005-01-25 Hoffman-La Roche Inc. 2,3-dihydro-isoindol-1-one derivatives
JP4691988B2 (ja) 2002-10-03 2011-06-01 小野薬品工業株式会社 Lpa受容体拮抗剤
EP1594508B1 (en) * 2003-02-11 2012-08-08 Irm Llc Novel bicyclic compounds and compositions
AU2004251146A1 (en) * 2003-05-19 2005-01-06 Irm, Llc Immunosuppressant compounds and compositions
MY150088A (en) * 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
BRPI0413923A (pt) 2003-08-29 2006-11-07 Ono Pharmaceutical Co composto capaz de ligar o receptor de s1p e uso farmacêutico do mesmo
BRPI0510664B8 (pt) 2004-05-07 2021-05-25 Warner Lambert Co derivados de fenol e tiofenol 3 ou 4-monosubstituído, composição farmacêutica, combinação e uso dos compostos para tratamento de doenças relacionadas ao h3, incluindo transtornos do sistema nervoso central e transtornos inflamatórios
HRP20100298T1 (hr) 2004-08-26 2010-06-30 Pfizer Inc. Enantiomerno čisti aminoheteroarilni spojevi kao inhibitori proteinskih kinaza
PT2415873E (pt) 2006-12-14 2015-03-31 Sangamo Biosciences Inc Proteínas com dedos de zinco não canónicas optimizadas

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111107837A (zh) * 2017-09-27 2020-05-05 诺华股份有限公司 包含西普尼莫德的肠胃外制剂
WO2025077706A1 (zh) * 2023-10-08 2025-04-17 华东师范大学 用于肌病治疗的s1pr4调节剂化合物及其应用
CN119564675A (zh) * 2024-12-25 2025-03-07 合肥工业大学 一种小分子化合物在制备细胞焦亡抑制剂中的应用

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