CN1314682C - 抑制由α4整合素调介的白血球粘附的杂环化合物 - Google Patents

抑制由α4整合素调介的白血球粘附的杂环化合物 Download PDF

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Publication number
CN1314682C
CN1314682C CNB038115484A CN03811548A CN1314682C CN 1314682 C CN1314682 C CN 1314682C CN B038115484 A CNB038115484 A CN B038115484A CN 03811548 A CN03811548 A CN 03811548A CN 1314682 C CN1314682 C CN 1314682C
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compound
diethylamino
ylcarbonyloxy
phenylalanine
pyrimidin
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Expired - Fee Related
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CNB038115484A
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Chinese (zh)
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CN1656090A (zh
Inventor
安德烈·W·康拉迪
克里斯托夫·M·塞姆科
许英姿
弗兰克·斯塔潘贝克
布赖恩·P·斯图皮
珍妮弗·史密斯
尤金·D·托尔塞特
迈克尔·A·普莱斯
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Elan Pharmaceuticals LLC
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Elan Pharmaceuticals LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/50—Three nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CNB038115484A 2002-05-24 2003-05-27 抑制由α4整合素调介的白血球粘附的杂环化合物 Expired - Fee Related CN1314682C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38302002P 2002-05-24 2002-05-24
US60/383,020 2002-05-24

Publications (2)

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CN1656090A CN1656090A (zh) 2005-08-17
CN1314682C true CN1314682C (zh) 2007-05-09

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Country Link
US (3) US7135477B2 (enExample)
EP (1) EP1507775B1 (enExample)
JP (1) JP4469715B2 (enExample)
KR (1) KR100978832B1 (enExample)
CN (1) CN1314682C (enExample)
AT (1) ATE419243T1 (enExample)
AU (1) AU2003240823C1 (enExample)
BR (1) BR0308881A (enExample)
CA (1) CA2481926C (enExample)
DE (1) DE60325583D1 (enExample)
DK (1) DK1507775T3 (enExample)
EA (1) EA008256B1 (enExample)
EC (1) ECSP045425A (enExample)
ES (1) ES2320436T3 (enExample)
IL (2) IL164225A0 (enExample)
MX (1) MXPA04010995A (enExample)
NO (1) NO329933B1 (enExample)
NZ (1) NZ535504A (enExample)
TW (1) TWI281470B (enExample)
UA (1) UA76339C2 (enExample)
WO (1) WO2003099809A1 (enExample)
ZA (1) ZA200407590B (enExample)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HK1045157A1 (zh) * 1999-01-22 2002-11-15 依兰制药公司 抑制vla-4介导的白细胞粘着的化合物
TWI281470B (en) * 2002-05-24 2007-05-21 Elan Pharm Inc Heterocyclic compounds which inhibit leukocyte adhesion mediated by alpha4 integrins
US20050074451A1 (en) * 2003-06-25 2005-04-07 Elan Pharmaceuticals, Inc. Methods and compositions for treating rheumatoid arthritis
WO2005111020A2 (en) * 2004-04-30 2005-11-24 Elan Pharmaceuticals, Inc. Pyrimidine hydantoin analogues which inhibit leukocyte adhesion mediated by vla-4
CA2573245C (en) * 2004-07-08 2013-10-01 Elan Pharmaceuticals, Inc. Multivalent vla-4 antagonists comprising polymer moieties
BRPI0611285A2 (pt) * 2005-05-20 2010-08-31 Elan Pharm Inc derivados de imidazolona fenilalanina
ZA200803016B (en) 2005-09-29 2009-10-28 Elan Pharmaceuticals Inc Wyeth Carbamate compounds which inhibit leukocyte adhesion mediated by VLA-4
ATE493405T1 (de) 2005-09-29 2011-01-15 Elan Pharm Inc Pyrimidinylamidverbindungen, die die durch vla-4 vermittelte leukozytenadhäsion inhibieren
EA017110B1 (ru) * 2006-02-27 2012-09-28 Элан Фамэсьютикэлс, Инк. ПИРИМИДИНИЛСУЛЬФОНАМИДНЫЕ СОЕДИНЕНИЯ (ВАРИАНТЫ), СПОСОБ ПОЛУЧЕНИЯ ПИРИМИДИНИЛСУЛЬФОНАМИДНЫХ СОЕДИНЕНИЙ (ВАРИАНТЫ), ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ, ОПОСРЕДОВАННОГО ИНТЕГРИНОМ α4, СПОСОБ СНИЖЕНИЯ И/ИЛИ ПРЕДУПРЕЖДЕНИЯ ВОСПАЛИТЕЛЬНОГО КОМПОНЕНТА ЗАБОЛЕВАНИЯ ИЛИ АУТОИММУННОГО ОТВЕТА
US8410115B2 (en) * 2006-02-28 2013-04-02 Elan Pharmaceuticals, Inc. Methods of treating inflammatory and autoimmune diseases with alpha-4 inhibitory compounds
HUE047230T2 (hu) 2006-02-28 2020-04-28 Biogen Ma Inc Gyulladásos és autoimmun betegségek natalizumabbal való kezelésének módszerei
KR20080104343A (ko) * 2006-03-03 2008-12-02 엘란 파마슈티칼스, 인크. 나탈리주마브로 염증 및 자가면역 질환을 치료하는 방법
CA2708262A1 (en) * 2007-12-07 2009-06-18 Elan Pharmaceuticals, Inc. Methods and compositions for treating liquid tumors
EP2085407A1 (en) 2008-02-04 2009-08-05 Sahltech I Göteborg AB Treatment of idiopathic thrombocytopenic purpura
MX2010011724A (es) * 2008-04-29 2010-11-30 Nsab Af Neurosearch Sweden Ab Moduladores de neurotransmision de dopamina.
SG10201401836RA (en) * 2009-04-27 2014-10-30 Elan Pharm Inc Pyridinone antagonists of alpha-4 integrins
US11287423B2 (en) 2010-01-11 2022-03-29 Biogen Ma Inc. Assay for JC virus antibodies
BR112012017014B1 (pt) 2010-01-11 2021-07-20 Biogen Ma Inc Métodos para detecção de anticorpos de vírus jc
HUE061244T2 (hu) 2011-05-31 2023-06-28 Biogen Ma Inc A PML kockázat értékelésének módszere
JP6080521B2 (ja) * 2012-11-30 2017-02-15 インターナショナル・ビジネス・マシーンズ・コーポレーションＩｎｔｅｒｎａｔｉｏｎａｌ Ｂｕｓｉｎｅｓｓ Ｍａｃｈｉｎｅｓ Ｃｏｒｐｏｒａｔｉｏｎ 広域分散医療情報ネットワークのデータ管理機構
EP3004334A4 (en) 2013-05-28 2016-12-21 Biogen Ma Inc METHOD FOR ASSESSING A PML RISK
HK1244806A1 (zh) * 2015-12-30 2018-08-17 Saint Louis University 作為過氧乙醯硝酸整聯蛋白拮抗劑的間氮雜環氨基苯甲酸衍生物
DK3873884T3 (da) 2018-10-30 2025-02-17 Gilead Sciences Inc 3-(quinolin-8-yl)-1,4-dihydropyrido[3,4-d]pyrimidin-2,4-dion-derivater som alpha4beta7-integrinhæmmere til behandling af inflammatoriske sygdomme
ES2987796T3 (es) 2018-10-30 2024-11-18 Gilead Sciences Inc Derivados de N-benzoil-fenilalanina como inhibidores de la integrina alfa4beta7 para el tratamiento de enfermedades inflamatorias
WO2020092394A1 (en) 2018-10-30 2020-05-07 Gilead Sciences, Inc. Imidazopyridine derivatives as alpha4beta7 integrin inhibitors
WO2020092401A1 (en) 2018-10-30 2020-05-07 Gilead Sciences, Inc. COMPOUNDS FOR INHIBITION OF ALPHA 4β7 INTEGRIN
CN109541237A (zh) * 2018-12-28 2019-03-29 吴江近岸蛋白质科技有限公司 纤维连接蛋白的生物学活性测定方法
AU2020329207B2 (en) 2019-08-14 2024-02-29 Gilead Sciences, Inc. Compounds for inhibition of alpha 4 beta 7 integrin

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0330506A2 (en) * 1988-02-26 1989-08-30 Dana Farber Cancer Institute VLA proteins
CN1182746A (zh) * 1996-11-15 1998-05-27 赫彻斯特股份公司 用作白细胞粘合抑制剂和vla-4拮抗剂的新的杂环化合物
CN1201454A (zh) * 1995-08-30 1998-12-09 G·D·瑟尔公司 间－胍基、脲基、硫脲基或氮杂环氨基苯甲酸衍生物用作整合素拮抗剂

Family Cites Families (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2525656A1 (de) 1974-06-19 1976-01-15 Sandoz Ag Verfahren zur herstellung neuer heterocyclischer verbindungen
US4070457A (en) 1974-11-08 1978-01-24 Mitsubishi Chemical Industries Ltd. N2 -naphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
US4096255A (en) 1974-11-08 1978-06-20 Mitsubishi Chemical Industries Limited N2 -naphthalenesulfonyl-L-argininamides, and pharmaceutical salts, compositions and methods
US4041156A (en) 1974-11-08 1977-08-09 Mitsubishi Chemical Industries Limited N2 -alkoxynaphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
US4055636A (en) 1974-11-08 1977-10-25 Mitsubishi Chemical Industries Ltd. N2 -alkoxynaphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
US4055651A (en) 1974-11-08 1977-10-25 Mitsubishi Chemical Industries Ltd. N2 -alkoxynaphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
US4046876A (en) 1974-11-08 1977-09-06 Mitsubishi Chemical Industries Limited N2 -alkoxynaphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
US4073914A (en) 1974-11-08 1978-02-14 Mitsubishi Chemical Industries Limited N2 -naphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
US4018915A (en) 1976-01-05 1977-04-19 Mitsubishi Chemical Industries Ltd. N2 -alkoxynaphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
US4104392A (en) 1974-11-08 1978-08-01 Mitsubishi Chemical Industries Ltd. N2 -naphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof, and antithrombotic compositions and methods employing them
JPS5727454B2 (enExample) 1975-02-21 1982-06-10
CA1102316A (en) 1975-12-09 1981-06-02 Shosuke Okamoto N su2 xx-arylsulfonyl-l-argininamides and the pharmaceutically acceptable salts thereof
US4018913A (en) 1976-01-14 1977-04-19 Mitsubishi Chemical Industries Ltd. N2 -alkoxynaphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
US4036955A (en) 1976-07-22 1977-07-19 Mitsubishi Chemical Industries Ltd. N2 -naphthalenesulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof
DE2742173A1 (de) 1977-09-20 1979-03-29 Bayer Ag Phenoxy-pyridinyl(pyrimidinyl)-alkanole, verfahren zu ihrer herstellung sowie ihre verwendung als fungizide
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
IT1211096B (it) 1981-08-20 1989-09-29 Lpb Ist Farm Pirimidine e s.triazinici adattivita' ipolipidemizzante.
US4672065A (en) 1982-11-19 1987-06-09 Chevron Research Company N-substituted phenoxyacetamide fungicides
US4501728A (en) 1983-01-06 1985-02-26 Technology Unlimited, Inc. Masking of liposomes from RES recognition
US4565814A (en) 1983-01-28 1986-01-21 Sanofi Pyridazine derivatives having a psychotropic action and compositions
JPS59212480A (ja) 1983-05-17 1984-12-01 Nippon Soda Co Ltd ピリダジン誘導体及び除草剤
DE3322720A1 (de) 1983-06-24 1985-01-03 Chemische Werke Hüls AG, 4370 Marl Verwendung von in 2-stellung mit (substituierten) aminogruppen substituierten 4-dl-alkylester-(alpha)-alaninyl-6-chlor-s-triazinen als herbizide, insbesondere gegen flughafer
US4505910A (en) 1983-06-30 1985-03-19 American Home Products Corporation Amino-pyrimidine derivatives, compositions and use
NZ210669A (en) 1983-12-27 1988-05-30 Syntex Inc Benzoxazin-4-one derivatives and pharmaceutical compositions
US4595364A (en) * 1984-02-15 1986-06-17 Molten Corp. Dental prosthesis and process for preparing the same
PH22520A (en) 1984-11-12 1988-10-17 Yamanouchi Pharma Co Ltd Heterocyclic compounds having 4-lover alkyl-3-hydroxy-2-lower alkyl phenoxy-lower alkylene-y-group, and process of producing them
US4959364A (en) 1985-02-04 1990-09-25 G. D. Searle & Co. Method of treating inflammation, allergy, asthma and proliferative skin disease using heterocyclic amides
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US4837028A (en) 1986-12-24 1989-06-06 Liposome Technology, Inc. Liposomes with enhanced circulation time
JPH0784424B2 (ja) 1987-04-15 1995-09-13 味の素株式会社 チロシン誘導体及びその用途
DE3904931A1 (de) 1989-02-17 1990-08-23 Bayer Ag Pyridyl-substituierte acrylsaeureester
US5030644A (en) 1989-07-31 1991-07-09 Merck & Co., Inc. Imidazole compounds and their use as transglutaminase inhibitors
US5260210A (en) 1989-09-27 1993-11-09 Rubin Lee L Blood-brain barrier model
US4992439A (en) 1990-02-13 1991-02-12 Bristol-Myers Squibb Company Pyridazine carboxylic acids and esters
FR2679903B1 (fr) 1991-08-02 1993-12-03 Elf Sanofi Derives de la n-sulfonyl indoline portant une fonction amidique, leur preparation, les compositions pharmaceutiques en contenant.
NZ239846A (en) 1990-09-27 1994-11-25 Merck & Co Inc Sulphonamide derivatives and pharmaceutical compositions thereof
DE4108029A1 (de) 1991-03-13 1992-09-17 Bayer Ag Triazinyl-substituierte acrylsaeureester
WO1992016549A1 (de) 1991-03-18 1992-10-01 Pentapharm Ag Para-substituierte phenylalanin-derivate
IT1247509B (it) 1991-04-19 1994-12-17 Univ Cagliari Composti di sintesi atti all'impiego nella terapia delle infezioni da rhinovirus
US5296486A (en) 1991-09-24 1994-03-22 Boehringer Ingelheim Pharmaceuticals, Inc. Leukotriene biosynthesis inhibitors
AU3420693A (en) 1991-12-24 1993-07-28 Fred Hutchinson Cancer Research Center Competitive inhibition of high-avidity alpha4-beta1 receptor using tripeptide ldv
BR9306058A (pt) 1992-03-11 1997-11-18 Narhex Ltd Derivados de amina de hidrocarbonetos oxo- e hidroxi- substituidos
DE4227748A1 (de) 1992-08-21 1994-02-24 Bayer Ag Pyridyloxy-acrylsäureester
JP2848232B2 (ja) 1993-02-19 1999-01-20 武田薬品工業株式会社 アルデヒド誘導体
US5770573A (en) 1993-12-06 1998-06-23 Cytel Corporation CS-1 peptidomimetics, compositions and methods of using the same
TW574214B (en) 1994-06-08 2004-02-01 Pfizer Corticotropin releasing factor antagonists
US5510332A (en) 1994-07-07 1996-04-23 Texas Biotechnology Corporation Process to inhibit binding of the integrin α4 62 1 to VCAM-1 or fibronectin and linear peptides therefor
EP0769958B1 (en) 1994-07-11 2003-04-16 Athena Neurosciences, Inc. Inhibitors of leukocyte adhesion
US6306840B1 (en) 1995-01-23 2001-10-23 Biogen, Inc. Cell adhesion inhibitors
IL117659A (en) 1995-04-13 2000-12-06 Dainippon Pharmaceutical Co Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same
PT765879E (pt) 1995-09-29 2001-05-31 Sankyo Co Derivados 13-substituidos de milbemicina-5-oxima sua preparacao e utilizacao contra insectos e outras pragas
DE19536891A1 (de) 1995-10-04 1997-04-10 Basf Ag Neue Aminosäurederivate, ihre Herstellung und Verwendung
DE19548709A1 (de) 1995-12-23 1997-07-03 Merck Patent Gmbh Tyrosinderivate
US6211333B1 (en) 1996-06-21 2001-04-03 Takeda Chemical Industries, Ltd. Method for producing peptides and their salts which have an agonist activity of luteinizing hormone releasing hormones secreted from the hypothalamus
EP0907637A1 (de) 1996-06-28 1999-04-14 MERCK PATENT GmbH Phenylalanin-derivate als integrin-inhibitoren
DE19629817A1 (de) 1996-07-24 1998-01-29 Hoechst Ag Neue Imino-Derivate als Inhibitoren der Knochenresorption und Vitronectinrezeptor-Antagonisten
DE19647317A1 (de) 1996-11-15 1998-05-20 Hoechst Schering Agrevo Gmbh Substituierte Stickstoff-Heterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel
NZ334950A (en) 1996-11-22 2001-03-30 Lilly Co Eli N-(aryl/heteroarylacetyl) amino acid esters and pharmaceutical compositions comprising same; useful for inhibiting beta-amyloid peptide release and/or its synthesis
AU6264898A (en) 1997-02-04 1998-08-25 Versicor Inc Solid phase and combinatorial library syntheses of 3,1-benzoxazine-4-ones
DE19713000A1 (de) 1997-03-27 1998-10-01 Merck Patent Gmbh Adhäsionsrezeptor-Antagonisten
EP1001764A4 (en) 1997-05-29 2005-08-24 Merck & Co Inc HETEROCYCLIC AMIDE COMPOUNDS AS INHIBITORS OF CELL ADHESION
ATE318841T1 (de) 1997-05-29 2006-03-15 Merck & Co Inc Biarylalkansäuren in der verwendung als zelladhäsionsinhibitoren
AR016133A1 (es) 1997-07-31 2001-06-20 Wyeth Corp Compuesto de carbamiloxi que inhiben la adhesion de leucocitos mediada por vla-4, compuestos que son prodrogas de dichos compuestos, composicionfarmaceutica, metodo para fijar vla-4 a una muestra biologica, metodo para el tratamiento de una condicion inflamatoria
PL338373A1 (en) 1997-07-31 2000-10-23 Elan Pharm Inc Dipeptide and its affinite compounds inhibiting adhesion of leucocytes occurring through mediation of vla-4
IL133640A0 (en) 1997-07-31 2001-04-30 Elan Pharm Inc Substituted phenylalanine type compounds which inhibit leukocyte adhesion mediated by vla-4
IL133641A0 (en) 1997-07-31 2001-04-30 Elan Pharm Inc Compounds which inhibit leukocyte adhesion mediated by vla-4
ATE260243T1 (de) 1997-08-22 2004-03-15 Hoffmann La Roche N-aroylphenylalaninderivate
KR100554815B1 (ko) 1997-08-22 2006-02-22 에프. 호프만-라 로슈 아게 엔-아로일페닐알라닌 유도체
CN1294576A (zh) 1998-01-23 2001-05-09 诺瓦提斯公司 Vla－4拮抗剂
US6329372B1 (en) 1998-01-27 2001-12-11 Celltech Therapeutics Limited Phenylalanine derivatives
HUP0101419A3 (en) 1998-04-16 2002-08-28 Texas Biotechnology Corp Houst Compounds that inhibit the binding of integrins to their receptors and pharmaceutical compositions containing them
GB9821061D0 (en) 1998-09-28 1998-11-18 Celltech Therapeutics Ltd Chemical compounds
GB9825652D0 (en) 1998-11-23 1999-01-13 Celltech Therapeutics Ltd Chemical compounds
HK1045157A1 (zh) * 1999-01-22 2002-11-15 依兰制药公司 抑制vla-4介导的白细胞粘着的化合物
WO2000043369A1 (en) * 1999-01-22 2000-07-27 Elan Pharmaceuticals, Inc. Compounds which inhibit leukocyte adhesion mediated by vla-4
PE20020384A1 (es) 2000-07-21 2002-05-28 Schering Corp PEPTIDOS COMO INHIBIDORES DE LA PROTEASA SERINA NS3/NS4a DEL VIRUS DE LA HEPATITIS C
TWI281470B (en) * 2002-05-24 2007-05-21 Elan Pharm Inc Heterocyclic compounds which inhibit leukocyte adhesion mediated by alpha4 integrins

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0330506A2 (en) * 1988-02-26 1989-08-30 Dana Farber Cancer Institute VLA proteins
CN1201454A (zh) * 1995-08-30 1998-12-09 G·D·瑟尔公司 间－胍基、脲基、硫脲基或氮杂环氨基苯甲酸衍生物用作整合素拮抗剂
CN1182746A (zh) * 1996-11-15 1998-05-27 赫彻斯特股份公司 用作白细胞粘合抑制剂和vla-4拮抗剂的新的杂环化合物

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