HRP20161156T1 - Spojevi i sastavi imunosupresiva - Google Patents

Spojevi i sastavi imunosupresiva Download PDF

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Publication number
HRP20161156T1
HRP20161156T1 HRP20161156TT HRP20161156T HRP20161156T1 HR P20161156 T1 HRP20161156 T1 HR P20161156T1 HR P20161156T T HRP20161156T T HR P20161156TT HR P20161156 T HRP20161156 T HR P20161156T HR P20161156 T1 HRP20161156 T1 HR P20161156T1
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HR
Croatia
Prior art keywords
inhibitor
family
kinase
rapamycin
inflammatory
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HRP20161156TT
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English (en)
Croatian (hr)
Inventor
Shifeng Pan
Wenqi Gao
Nathanael S. Gray
Yuan Mi
Yi Fan
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Novartis Ag
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33479305&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20161156(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of HRP20161156T1 publication Critical patent/HRP20161156T1/hr

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Families Citing this family (108)

* 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
EP1661881B1 (en) * 2003-08-29 2014-12-17 Ono Pharmaceutical Co., Ltd. Compound capable of binding s1p receptor and pharmaceutical use thereof
WO2005041899A2 (en) 2003-11-03 2005-05-12 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
JP4740884B2 (ja) * 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 免疫抑制性化合物および組成物
TW200538433A (en) * 2004-02-24 2005-12-01 Irm Llc Immunosuppressant compounds and compositiions
KR20140095109A (ko) 2004-11-29 2014-07-31 노파르티스 아게 Ｓ１ｐ 수용체 효능제의 투여 용법
AU2006214314B2 (en) 2005-02-14 2012-02-09 University Of Virginia Patent Foundation Sphingosine 1- phos phate agonists comprising cycloalkanes and 5 -membered heterocycles substituted by amino and phenyl groups
GB0504544D0 (en) * 2005-03-04 2005-04-13 Novartis Ag Organic compounds
CN101203512A (zh) * 2005-04-22 2008-06-18 第一三共株式会社 杂环化合物
GB0510390D0 (en) * 2005-05-20 2005-06-29 Novartis Ag Organic compounds
KR20080086546A (ko) 2006-01-27 2008-09-25 유니버시티 오브 버지니아 페이턴트 파운데이션 신경병증성 통증의 치료 방법
AU2007212193A1 (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
MX2009001457A (es) 2006-08-08 2009-02-19 Kyorin Seiyaku Kk Derivados de aminoalcohol e inmunosupresores que contienen lo mismo como ingrediente activo.
JP5188972B2 (ja) 2006-08-08 2013-04-24 杏林製薬株式会社 アミノリン酸エステル誘導体及びそれらを有効成分とするｓ１ｐ受容体調節剤
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
CA2669102A1 (en) 2006-11-21 2008-05-29 University Of Virginia Patent Foundation Tetralin analogs having sphingosine 1-phosphate agonist activity
CA2669104A1 (en) 2006-11-21 2008-05-29 University Of Virginia Patent Foundation Hydrindane analogs having sphingosine 1-phosphate receptor 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
ES2707576T3 (es) 2007-05-04 2019-04-04 Novartis Ag Uso de modulador del receptor S1P
CN101918360A (zh) 2007-09-24 2010-12-15 阿勒根公司 具有1-磷酸-鞘氨醇(s1p)受体生物学活性的带芳基或者杂芳基基团的吲哚化合物
AU2008310846C1 (en) * 2007-10-12 2022-10-06 Novartis Ag Compositions comprising sphingosine 1 phosphate (S1P) receptor modulators
GB0725101D0 (en) * 2007-12-21 2008-01-30 Glaxo Group Ltd Compounds
WO2009099174A1 (ja) 2008-02-07 2009-08-13 Kyorin Pharmaceutical Co., Ltd. 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
HUE033168T2 (en) 2008-03-17 2017-11-28 Actelion Pharmaceuticals Ltd Dosage regimen for selective SIP1 receptor agonist
GB0807910D0 (en) * 2008-04-30 2008-06-04 Glaxo Group Ltd Compounds
CN102089305A (zh) 2008-05-08 2011-06-08 阿勒根公司 治疗用取代的1,7-联苯-1,2,3,5,6,7-六氢吡啶并[3,2,1-ij]喹啉化合物
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
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
PT2300013T (pt) 2008-05-21 2017-10-31 Ariad Pharma Inc Derivados de fósforo como inibidores de cinases
US9149459B2 (en) * 2008-07-23 2015-10-06 Novartis Ag Sphingosine 1 phosphate receptor modulators and their use to treat muscle inflammation
EA019252B1 (ru) 2008-07-23 2014-02-28 Арена Фармасьютикалз, Инк. ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ (1,2,3,4-ТЕТРАГИДРОЦИКЛОПЕНТА[b]ИНДОЛ-3-ИЛ)УКСУСНОЙ КИСЛОТЫ, ПРИМЕНИМЫЕ В ЛЕЧЕНИИ АУТОИММУННЫХ И ВОСПАЛИТЕЛЬНЫХ РАССТРОЙСТВ
AU2013209344B2 (en) * 2008-07-23 2015-12-24 Novartis Ag Sphingosine 1 phosphate receptor modulators and their use to treat muscle inflammation
ES2526119T3 (es) * 2008-08-18 2015-01-07 Novartis Ag Derivado de azetidina para el tratamiento de neuropatías periféricas
SI2342205T1 (sl) 2008-08-27 2016-09-30 Arena Pharmaceuticals, Inc. Substituirani triciklični kislinski derivati kot agonisti S1P1 receptorja, uporabni v zdravljenju avtoimunskih in vnetnih obolenj
PT2676953T (pt) * 2008-12-18 2017-06-29 Novartis Ag Sal hemifumarato de ácido 1-[4-[1-(4-ciclo-hexil-3-trifluorometil-benziloxi-imino)-etil]-2-etil-benzil]-azetidino-3-carboxílico para utilização no tratamento de doenças mediadas por linfócitos
CA2747558A1 (en) 2008-12-18 2010-07-15 Novartis Ag New salts
CN102256942B (zh) * 2008-12-18 2013-07-24 诺瓦提斯公司 1-(4-{1-[(e)-4-环己基-3-三氟甲基-苄氧基亚氨基]-乙基}-2-乙基-苄基)-氮杂环丁烷-3-甲酸的多晶型物
CN105213372A (zh) 2008-12-22 2016-01-06 诺华股份有限公司 S1p受体激动剂的给药方案
US8399451B2 (en) 2009-08-07 2013-03-19 Bristol-Myers Squibb Company Heterocyclic compounds
SG10201906876PA (en) 2010-01-27 2019-09-27 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
SG183416A1 (en) 2010-03-03 2012-09-27 Arena Pharm Inc Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof
WO2011116091A1 (en) 2010-03-17 2011-09-22 Novartis Ag Dispenser
WO2011133734A1 (en) 2010-04-23 2011-10-27 Bristol-Myers Squibb Company 4 - (5 - isoxazolyl or 5 - pyrrazolyl -1,2,4- oxadiazol - 3 - yl) -mandelic acid amides as sphingosin- 1 - phosphate 1 rreceptor agonists
EP2619190B1 (en) 2010-09-24 2015-08-12 Bristol-Myers Squibb Company Substituted oxadiazole compounds and their use as s1p1 agonists
AU2011336970A1 (en) * 2010-12-03 2013-07-11 Allergan, Inc. Novel oxime derivatives as sphingosine 1-phosphate (S1P) receptor modulators
JP2013544837A (ja) * 2010-12-03 2013-12-19 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）受容体モジュレーターとしての新規オキシムアゼチジン誘導体
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
BR112013017302B1 (pt) 2011-01-07 2021-12-07 Novartis Ag Composição farmacêutica em fase sólida
WO2012095853A1 (en) 2011-01-10 2012-07-19 Novartis Pharma Ag Modified release formulations comprising sip receptor modulators
US9834518B2 (en) 2011-05-04 2017-12-05 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in EGFR-driven cancers
PH12014500854A1 (en) 2011-10-21 2021-08-09 Novartis Ag Dosage regimen for an s1p receptor modulator or agonist
EP2809645A1 (en) * 2012-02-03 2014-12-10 Novartis AG Process for preparing n-(4-cyclohexyl-3-trifluoromethyl-benzyloxy)-acetimidic acid ethyl ester
US20150166591A1 (en) 2012-05-05 2015-06-18 Ariad Pharmaceuticals, Inc. Methods and compositions for raf kinase mediated diseases
HK1213636A1 (zh) * 2013-04-04 2016-07-08 Novartis Ag 识别病患对投予s1p受体调节剂之反应
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
JP6294872B2 (ja) * 2013-04-26 2018-03-14 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
EP3102576B8 (en) 2014-02-03 2019-06-19 Vitae Pharmaceuticals, LLC Dihydropyrrolopyridine inhibitors of ror-gamma
PT3207043T (pt) 2014-10-14 2019-03-25 Vitae Pharmaceuticals Llc Inibidores de di-hidropirrolopiridina de ror-gama
US9845308B2 (en) 2014-11-05 2017-12-19 Vitae Pharmaceuticals, Inc. Isoindoline inhibitors of ROR-gamma
US9663515B2 (en) 2014-11-05 2017-05-30 Vitae Pharmaceuticals, Inc. Dihydropyrrolopyridine inhibitors of ROR-gamma
MX386419B (es) 2015-01-06 2025-03-18 Arena Pharm Inc Metodos de condiciones de tratamiento relacionadas con el receptor s1p1.
WO2016135644A1 (en) 2015-02-26 2016-09-01 Novartis Ag Treatment of autoimmune disease in a patient receiving additionally a beta-blocker
EP3939965A1 (en) 2015-06-22 2022-01-19 Arena Pharmaceuticals, Inc. Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid for use in sipi receptor-associated disorders
WO2017024018A1 (en) 2015-08-05 2017-02-09 Vitae Pharmaceuticals, Inc. Modulators of ror-gamma
US11008340B2 (en) 2015-11-20 2021-05-18 Vitae Pharmaceuticals, Llc Modulators of ROR-gamma
WO2017120124A1 (en) 2016-01-04 2017-07-13 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
WO2018151834A1 (en) 2017-02-16 2018-08-23 Arena Pharmaceuticals, Inc. Compounds and methods for treatment of inflammatory bowel disease with extra-intestinal manifestations
MA47504A (fr) 2017-02-16 2019-12-25 Arena Pharm Inc Composés et méthodes de traitement de l'angiocholite biliaire primitive
US11958805B2 (en) 2017-03-09 2024-04-16 Novartis Ag Solid forms comprising an oxime ether compound, compositions and methods of use thereof
US11629124B2 (en) 2017-03-09 2023-04-18 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
WO2019018975A1 (en) 2017-07-24 2019-01-31 Vitae Pharmaceuticals, Inc. INHIBITORS OF ROR GAMMA
JP2020528904A (ja) 2017-07-24 2020-10-01 ヴァイティー ファーマシューティカルズ，エルエルシー ＲＯＲγの阻害剤
US11628137B2 (en) * 2017-09-27 2023-04-18 Novartis Ag Parenteral formulation comprising siponimod
CN111405897A (zh) 2017-09-27 2020-07-10 雷迪博士实验室有限公司 辛波莫德、其盐及其固态形式的制备方法
AU2018343239A1 (en) 2017-09-29 2020-03-12 Novartis Ag Dosing regimen of siponimod
MX2020007268A (es) 2017-09-29 2020-08-17 Novartis Ag Regimen de dosificacion de siponimod.
EP3743405B1 (en) 2018-01-22 2023-11-15 Teva Pharmaceuticals International GmbH Crystalline siponimod fumaric acid and polymorphs thereof
ES2987794T3 (es) 2018-06-06 2024-11-18 Arena Pharm Inc Procedimientos de tratamiento de afecciones relacionadas con el receptor S1P1
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
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
WO2020201172A1 (en) 2019-03-29 2020-10-08 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
AU2020372647B2 (en) 2019-10-31 2026-02-05 Idorsia Pharmaceuticals Ltd Combination of a CXCR7 antagonist with an S1P1 receptor modulator
US12569455B2 (en) 2020-02-06 2026-03-10 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
WO2022064007A1 (en) 2020-09-25 2022-03-31 Synthon B.V. Siponimod salts and cocrystals
WO2022199865A1 (en) 2021-03-26 2022-09-29 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
CN119776509A (zh) * 2023-10-08 2025-04-08 华东师范大学 Ndufa10基因和S1pr4基因突变在肌病诊断、预测和治疗中的用途
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
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

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
ATE152718T1 (de) * 1991-08-15 1997-05-15 Ciba Geigy Ag N-acyl-n-heterocyclyl- oder naphthylalkyl- aminosäuren als angiotensin ii antagonisten
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
TW225528B (https=) 1992-04-03 1994-06-21 Ciba Geigy Ag
BR9207175A (pt) 1992-10-28 1995-12-12 Genentech Inc Composição contendo antagonista de fator de crescimento de célula endotelial vascular sequência aminoácida de anticorpo monoclonal polipeptídeo e método de tratamento de tumor em mamífero
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
WO1996005828A1 (en) 1994-08-24 1996-02-29 Eli Lilly And Company Pyrrolidinyl di-carboxylic acid derivatives as metabotropic glutamate receptor antagonists
MX9707453A (es) 1995-03-30 1997-12-31 Pfizer Derivados de quinazolina.
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
MX9800215A (es) 1995-07-06 1998-03-31 Novartis Ag Pirrolopirimidas y procesos para su preparacion.
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
PL327694A1 (en) 1995-12-29 1998-12-21 Smithkline Beecham Corp Antagonists of vitronectin receptor
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
HU228446B1 (en) 1996-04-12 2013-03-28 Warner Lambert Co Kinazoline derivatives as irreversible inhibitors of protein-kinase, pharmaceutical compositions containing these compounds and use thereof
EP0907642B1 (en) 1996-06-24 2005-11-02 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)
CA2265630A1 (en) 1996-09-13 1998-03-19 Gerald Mcmahon Use of quinazoline derivatives for the manufacture of a medicament in the treatment 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
ATE298740T1 (de) 1997-04-04 2005-07-15 Mitsubishi Pharma Corp 2-aminopropan-1,3-diol-verbindungen, ihre medizinische anwendung und zwischenprodukte zu ihrer synthese
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
NZ505757A (en) * 1998-01-16 2002-09-27 Centaur Pharmaceuticals Inc Thioether furan nitrone compounds and pharmaceuticals thereof; useful for the treatment or prophylaxis of neurodegenerative, autoimmune and inflammatory conditions
WO1999046277A1 (en) * 1998-03-09 1999-09-16 Smithkline Beecham Corporation HUMAN EDG-1c POLYNUCLEOTIDES AND POLYPEPTIDES AND METHODS OF USE
ATE459616T1 (de) 1998-08-11 2010-03-15 Novartis Ag Isochinoline derivate mit angiogenesis-hemmender wirkung
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
JP2002531539A (ja) * 1998-12-04 2002-09-24 ニューロサーチ、アクティーゼルスカブ イオンチャネル調節剤
WO2000037502A2 (en) 1998-12-22 2000-06-29 Genentech, Inc. Vascular endothelial cell growth factor antagonists and uses thereof
WO2000059509A1 (en) 1999-03-30 2000-10-12 Novartis Ag Phthalazine derivatives for treating inflammatory diseases
AP2005003199A0 (en) 1999-04-01 2005-03-31 Pfizer Prod Inc Aminopyrimidines as sorbitol dehydrogenase inhibitors
UA73307C2 (uk) * 1999-08-05 2005-07-15 Куміаі Кемікал Індастрі Ко., Лтд. Похідна карбамату і фунгіцид сільськогосподарського/садівницького призначення
AU783158B2 (en) 1999-08-24 2005-09-29 Ariad Pharmaceuticals, 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
WO2002018395A1 (en) 2000-08-31 2002-03-07 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
WO2002092068A1 (en) 2001-05-10 2002-11-21 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
CN1551766A (zh) 2001-09-05 2004-12-01 ������������ʽ���� 淋巴细胞活化抑制剂和自身免疫性疾病治疗剂
AU2002363236A1 (en) 2001-10-30 2003-05-12 Millennium Pharmaceuticals, Inc. Compounds, pharmaceutical compositions and methods of use therefor
US20050070506A1 (en) 2002-01-18 2005-03-31 Doherty George A. Selective s1p1/edg1 receptor agonists
US7479504B2 (en) * 2002-01-18 2009-01-20 Merck & Co., Inc. Edg receptor agonists
US20030207924A1 (en) 2002-03-07 2003-11-06 Xue-Min Cheng Compounds that modulate PPAR activity and methods of preparation
ES2329354T3 (es) 2002-04-26 2009-11-25 F. Hoffmann-La Roche Ag Derivados de isoquinolina.
MXPA04011691A (es) * 2002-05-24 2005-09-12 Pharmacia Corp Moduladores del receptor x anilino hepaticos.
EP1511473B8 (en) * 2002-05-27 2013-07-24 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
MXPA05008531A (es) * 2003-02-11 2005-11-17 Irm Llc Compuestos biciclicos novedosos y composiciones.
BRPI0410439A (pt) 2003-05-19 2006-06-06 Irm Llc compostos e composições imunossupressoras
MY150088A (en) * 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
EP1661881B1 (en) 2003-08-29 2014-12-17 Ono Pharmaceutical Co., Ltd. Compound capable of binding s1p receptor and pharmaceutical use thereof
ES2346665T3 (es) 2004-05-07 2010-10-19 Warner-Lambert Company Llc Derivados de fenol y tiofenol 3- o 4-monosustituidos utiles como ligandos de h3.
BR122020017756B1 (pt) 2004-08-26 2022-02-15 Pfizer Inc Uso de compostos de aminoeteroarila enantiomericamente puros na preparação de um medicamento para o tratamento de crescimento celular anormal em um mamífero
KR101520507B1 (ko) 2006-12-14 2015-05-29 다우 아그로사이언시즈 엘엘씨 최적화된 비-정규 아연 손가락 단백질

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