AU749351B2 - Alpha V integrin receptor antagonists - Google Patents

Alpha V integrin receptor antagonists Download PDF

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Publication number
AU749351B2
AU749351B2 AU57246/00A AU5724600A AU749351B2 AU 749351 B2 AU749351 B2 AU 749351B2 AU 57246/00 A AU57246/00 A AU 57246/00A AU 5724600 A AU5724600 A AU 5724600A AU 749351 B2 AU749351 B2 AU 749351B2
Authority
AU
Australia
Prior art keywords
oxo
tetrahydro
nonanoic acid
naphthyridin
alkyl
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU57246/00A
Other languages
English (en)
Other versions
AU5724600A (en
Inventor
Michael J Breslin
Paul J. Coleman
Mark E. Duggan
Wasyl Halczenko
George D. Hartman
John H. Hutchinson
Robert S. Meissner
Michael A. Patane
James J. Perkins
Jiabing Wang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and Co 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 Merck and Co Inc filed Critical Merck and Co Inc
Publication of AU5724600A publication Critical patent/AU5724600A/en
Application granted granted Critical
Publication of AU749351B2 publication Critical patent/AU749351B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU57246/00A 1999-06-02 2000-05-30 Alpha V integrin receptor antagonists Ceased AU749351B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US13710199P 1999-06-02 1999-06-02
US60/137101 1999-06-02
US17921600P 2000-01-31 2000-01-31
US60/179216 2000-01-31
PCT/US2000/014901 WO2000072801A2 (en) 1999-06-02 2000-05-30 Alpha v integrin receptor antagonists

Publications (2)

Publication Number Publication Date
AU5724600A AU5724600A (en) 2000-12-18
AU749351B2 true AU749351B2 (en) 2002-06-27

Family

ID=26834930

Family Applications (1)

Application Number Title Priority Date Filing Date
AU57246/00A Ceased AU749351B2 (en) 1999-06-02 2000-05-30 Alpha V integrin receptor antagonists

Country Status (28)

Country Link
US (1) US6410526B1 (enExample)
EP (1) EP1187592B1 (enExample)
JP (3) JP3808707B2 (enExample)
KR (1) KR20020021380A (enExample)
CN (1) CN1589145A (enExample)
AT (1) ATE368462T1 (enExample)
AU (1) AU749351B2 (enExample)
BG (1) BG106232A (enExample)
BR (1) BR0011108A (enExample)
CA (1) CA2373937A1 (enExample)
CY (1) CY1107746T1 (enExample)
CZ (1) CZ20014308A3 (enExample)
DE (1) DE60035779T2 (enExample)
DK (1) DK1187592T3 (enExample)
DZ (1) DZ3263A1 (enExample)
EA (1) EA200101272A1 (enExample)
EE (1) EE200100642A (enExample)
ES (1) ES2288861T3 (enExample)
HR (1) HRP20010895A2 (enExample)
HU (1) HUP0302468A2 (enExample)
IL (1) IL146378A0 (enExample)
IS (1) IS6157A (enExample)
NO (1) NO323906B1 (enExample)
PL (1) PL353364A1 (enExample)
PT (1) PT1187592E (enExample)
SK (1) SK17442001A3 (enExample)
TR (1) TR200103431T2 (enExample)
WO (1) WO2000072801A2 (enExample)

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US6048861A (en) * 1997-12-17 2000-04-11 Merck & Co., Inc. Integrin receptor antagonists
CA2397665A1 (en) 2000-01-24 2001-07-26 Merck & Co., Inc. Alpha v integrin receptor antagonists
WO2001096334A2 (en) 2000-06-15 2001-12-20 Pharmacia Corporation Heteroarylalkanoic acids as integrin receptor antagonists
DE60126496T2 (de) * 2000-07-26 2007-11-15 Merck & Co., Inc. Alpha v integrin-rezeptor-antagonisten
AU2001290772A1 (en) * 2000-09-14 2002-03-26 Merck And Co., Inc. Alpha v integrin receptor antagonists
WO2002028395A1 (en) * 2000-10-04 2002-04-11 Merck & Co., Inc. Phosphoric acid salt of an integrin receptor antagonist
CA2432504A1 (en) * 2001-01-03 2002-07-11 Merck & Co., Inc. Methods and compositions for treating periodontal disease
AU2002316855B2 (en) 2001-04-24 2008-03-13 Merck Patent Gmbh Combination therapy using anti-angiogenic agents and TNFalpha
CA2478317A1 (en) * 2002-03-04 2003-09-18 Medimmune, Inc. Methods of preventing or treating disorders by administering an integrin .alpha.v.beta.3 antagonist in combination with an hmg-coa reductase inhibitor or a bisphosphonate
CA2478239A1 (en) * 2002-03-04 2003-09-18 Medimmune, Inc. The prevention or treatment of cancer using integrin alphavbeta3 antagonists in combination with other agents
US20040224986A1 (en) 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
US7115596B2 (en) 2002-12-20 2006-10-03 Pharmacia Corporation Thiazole compounds as integrin receptor antagonists derivatives
WO2004078109A2 (en) * 2003-03-07 2004-09-16 Merck Sharp & Dohme Limited PROCESS FOR SYNTHESISING USEFUL INTERMEDIATES FOR THE PREPARATION OF ανβ3 RECEPTOR ANTAGONISTS
US8604185B2 (en) 2004-07-20 2013-12-10 Genentech, Inc. Inhibitors of angiopoietin-like 4 protein, combinations, and their use
KR20080089489A (ko) 2006-01-18 2008-10-06 메르크 파텐트 게엠베하 인테그린 리간드를 사용하는 암치료용 특이적 요법
CL2008000467A1 (es) * 2007-02-14 2008-08-22 Janssen Pharmaceutica Nv Compuestos derivados de 2-aminopirimidina, moduladores del receptor histamina h4; su procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar un trastorno inflamatorio seleccionado de alegia, asma
US20100069302A1 (en) 2007-07-18 2010-03-18 Stefan Krueger Specific therapy and medicament using integrin ligands for treating cancer
EP2217238B1 (en) 2007-11-08 2014-03-12 The General Hospital Corporation Methods and compositions for the treatment of proteinuric diseases
SG176103A1 (en) 2009-05-25 2011-12-29 Merck Patent Gmbh Continuous administration of cilengitide in cancer treatments
US8901144B2 (en) 2013-02-07 2014-12-02 Scifluor Life Sciences, Llc Fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives
PT2953948T (pt) 2013-02-07 2017-12-12 Scifluor Life Sciences Inc Antagonistas de integrina fluorada
GB201305668D0 (en) 2013-03-28 2013-05-15 Glaxosmithkline Ip Dev Ltd Avs6 Integrin Antagonists
FI3929196T3 (fi) 2013-09-24 2023-10-02 Fujifilm Corp Typpeä sisältävän yhdisteen tai sen suolan tai niiden metallikompleksin farmaseuttinen koostumus
GB201417011D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201417094D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201417018D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201417002D0 (en) 2014-09-26 2014-11-12 Glaxosmithkline Ip Dev Ltd Novel compound
CA2976634C (en) * 2015-02-19 2023-10-17 Scifluor Life Sciences, Inc Fluorinated tetrahydronaphthyridinyl nonanoic acid derivatives and uses thereof
GB201604680D0 (en) 2016-03-21 2016-05-04 Glaxosmithkline Ip Dev Ltd Chemical Compounds
US10118929B2 (en) 2016-04-27 2018-11-06 Scifluor Life Sciences, Inc. Nonanoic and decanoic acid derivatives and uses thereof
AU2017292754B2 (en) * 2016-07-05 2021-06-17 Icahn School Of Medicine At Mount Sinai Tetrahydronaphthyridinepentanamide integrin antagonists
TW201823208A (zh) 2016-09-07 2018-07-01 美商普萊恩醫療公司 N-醯基胺基酸化合物及其使用方法
BR112019009245A2 (pt) * 2016-11-08 2019-07-16 Bristol-Myers Squibb Company azol amidas e aminas como inibidores de alfav integrina
BR112019009129A2 (pt) * 2016-11-08 2019-07-16 Bristol-Myers Squibb Company compostos mono e espirocíclicos contendo ciclobutano e azetidina como inibidores de alfa v integrina
EP3589285A4 (en) 2017-02-28 2020-08-12 Morphic Therapeutic, Inc. INHIBITORS OF INTEGRIN (ALPHA-V) (BETA-6)
CN116283977A (zh) 2017-02-28 2023-06-23 莫菲克医疗股份有限公司 αvβ6整合蛋白的抑制剂
SG11202101913PA (en) 2018-08-29 2021-03-30 Morphic Therapeutic Inc INHIBITING aV ß6 INTEGRIN

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US5025025A (en) 1989-06-28 1991-06-18 Ciba-Geigy Corporation (Arylsulfonamido- and pyridyl-)-substituted carboxylic acids and derivatives thereof and use for suppressing thromboxane activity
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DK0796855T3 (da) 1996-03-20 2002-05-27 Hoechst Ag Hæmmere af knogleresorption og vitronectin-receptorantagonister
WO1997037655A1 (en) 1996-04-10 1997-10-16 Merck & Co., Inc. αvβ3 ANTAGONISTS
US5668159A (en) 1996-05-08 1997-09-16 The Dupont Merck Pharmaceutical Company 1,3,4-thiadiazoles and 1,3,4-oxadiazoles as IIb/IIIa antagonists
CA2263999A1 (en) 1996-08-29 1998-03-05 Merck & Co., Inc. Integrin antagonists
DE69720771T2 (de) * 1996-10-30 2004-01-29 Merck & Co Inc Integrin antagonist
JP2001504456A (ja) 1996-10-30 2001-04-03 メルク エンド カンパニー インコーポレーテッド インテグリン拮抗薬
AU729869B2 (en) 1997-01-17 2001-02-15 Merck & Co., Inc. Integrin antagonists
US6017926A (en) 1997-12-17 2000-01-25 Merck & Co., Inc. Integrin receptor antagonists
JP2002508323A (ja) 1997-12-17 2002-03-19 メルク エンド カムパニー インコーポレーテッド インテグリン受容体拮抗薬
HUP0100397A3 (en) * 1997-12-17 2002-10-28 Merck & Co Inc Tetrahydro- or octahydrobenzonaphtyridin and quinolin derivatives, pharmaceutical compositions thereof and process for their preparation
US6048861A (en) * 1997-12-17 2000-04-11 Merck & Co., Inc. Integrin receptor antagonists
DE69830806T2 (de) 1997-12-17 2006-04-27 Merck & Co., Inc. Integrinrezeptor antagonisten
EA003095B1 (ru) 1997-12-17 2002-12-26 Мерк Энд Ко., Инк. Антагонисты рецепторов интегринов

Also Published As

Publication number Publication date
EP1187592B1 (en) 2007-08-01
TR200103431T2 (tr) 2002-06-21
WO2000072801A3 (en) 2007-10-11
EP1187592A2 (en) 2002-03-20
WO2000072801A2 (en) 2000-12-07
AU5724600A (en) 2000-12-18
EP1187592A4 (en) 2002-11-06
EA200101272A1 (ru) 2002-06-27
BG106232A (en) 2002-06-28
SK17442001A3 (sk) 2002-03-05
HRP20010895A2 (en) 2003-08-31
CZ20014308A3 (cs) 2002-03-13
NO323906B1 (no) 2007-07-16
DE60035779D1 (de) 2007-09-13
DZ3263A1 (fr) 2000-12-07
IS6157A (is) 2001-11-13
DK1187592T3 (da) 2007-11-05
ES2288861T3 (es) 2008-02-01
CN1589145A (zh) 2005-03-02
CA2373937A1 (en) 2000-12-07
DE60035779T2 (de) 2008-04-30
PL353364A1 (en) 2003-11-17
IL146378A0 (en) 2002-07-25
US6410526B1 (en) 2002-06-25
HUP0302468A2 (hu) 2003-11-28
PT1187592E (pt) 2007-10-19
NO20015858D0 (no) 2001-11-30
JP2004500326A (ja) 2004-01-08
NO20015858L (no) 2002-02-04
CY1107746T1 (el) 2013-04-18
ATE368462T1 (de) 2007-08-15
JP2006206604A (ja) 2006-08-10
EE200100642A (et) 2003-02-17
KR20020021380A (ko) 2002-03-20
BR0011108A (pt) 2002-03-19
JP2006232844A (ja) 2006-09-07
JP3808707B2 (ja) 2006-08-16

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