WO2005016883A3 - Acrylamide derivatives as vla-1 integrin antagonists and uses thereof - Google Patents

Acrylamide derivatives as vla-1 integrin antagonists and uses thereof Download PDF

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Publication number
WO2005016883A3
WO2005016883A3 PCT/US2004/026653 US2004026653W WO2005016883A3 WO 2005016883 A3 WO2005016883 A3 WO 2005016883A3 US 2004026653 W US2004026653 W US 2004026653W WO 2005016883 A3 WO2005016883 A3 WO 2005016883A3
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WO
WIPO (PCT)
Prior art keywords
vla
integrin antagonists
acrylamide derivatives
compounds
integrin
Prior art date
Application number
PCT/US2004/026653
Other languages
French (fr)
Other versions
WO2005016883A2 (en
Inventor
Steven A Boyd
Scott Miller
Allen Thomas
Rui Xu
Yvan Lehuerou
Indrani Gunawardana
Gan Zhang
Jason Demeese
Martin Mclaughlin
Matthew Yanik
Mark L Lupher Jr
Irina C Jacobson
Eugene D Thorsett
Francine S Farouz
Ramesh A Kasar
Original Assignee
Icos Corp
Steven A Boyd
Scott Miller
Allen Thomas
Rui Xu
Yvan Lehuerou
Indrani Gunawardana
Gan Zhang
Jason Demeese
Martin Mclaughlin
Matthew Yanik
Mark L Lupher Jr
Irina C Jacobson
Eugene D Thorsett
Francine S Farouz
Ramesh A Kasar
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 Icos Corp, Steven A Boyd, Scott Miller, Allen Thomas, Rui Xu, Yvan Lehuerou, Indrani Gunawardana, Gan Zhang, Jason Demeese, Martin Mclaughlin, Matthew Yanik, Mark L Lupher Jr, Irina C Jacobson, Eugene D Thorsett, Francine S Farouz, Ramesh A Kasar filed Critical Icos Corp
Publication of WO2005016883A2 publication Critical patent/WO2005016883A2/en
Publication of WO2005016883A3 publication Critical patent/WO2005016883A3/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • CCHEMISTRY; METALLURGY
    • C04CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04BLIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632Organic additives
    • 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Manufacturing & Machinery (AREA)
  • Ceramic Engineering (AREA)
  • Inorganic Chemistry (AREA)
  • Materials Engineering (AREA)
  • Structural Engineering (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Compounds that are VLA-1 integrin antagonists are disclosed. Also disclosed are compositions containing such compounds, and methods of using such compounds in treating diseases mediated, at least in part, by the VLA-1 integrin.
PCT/US2004/026653 2003-08-14 2004-08-12 Acrylamide derivatives as vla-1 integrin antagonists and uses thereof WO2005016883A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US49560703P 2003-08-14 2003-08-14
US60/495,607 2003-08-14

Publications (2)

Publication Number Publication Date
WO2005016883A2 WO2005016883A2 (en) 2005-02-24
WO2005016883A3 true WO2005016883A3 (en) 2005-04-14

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/US2004/026653 WO2005016883A2 (en) 2003-08-14 2004-08-12 Acrylamide derivatives as vla-1 integrin antagonists and uses thereof
PCT/US2004/026207 WO2005019177A1 (en) 2003-08-14 2004-08-12 Aminopiperidine amide derivatives as vla-1 integrin antagonists and uses thereof

Family Applications After (1)

Application Number Title Priority Date Filing Date
PCT/US2004/026207 WO2005019177A1 (en) 2003-08-14 2004-08-12 Aminopiperidine amide derivatives as vla-1 integrin antagonists and uses thereof

Country Status (1)

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WO (2) WO2005016883A2 (en)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR0011250A (en) 1999-06-01 2002-03-05 Biogen Inc Monoclonal vla-1 blocking antibody and its use for the treatment of inflammatory disorders
AU2002258778C1 (en) 2001-04-13 2008-12-04 Biogen Ma Inc. Antibodies to VLA-1
CA2626103C (en) * 2006-01-13 2013-07-30 Dow Agrosciences Llc 6-(poly-substituted aryl)-4-aminopicolinates and their use as herbicides
US7714025B2 (en) * 2006-05-10 2010-05-11 Arizona Biomedical Research Commission Modified chalcone compounds as antimitotic agents
PT2034830E (en) * 2006-05-25 2014-10-14 Biogen Idec Inc Anti-vla-1 antibody for treating stroke
ES2304220B1 (en) * 2007-03-02 2009-09-11 Universidad De Zaragoza COMPOSITION FOR THE TREATMENT OF INFECTIOUS DISEASES.
US8088793B2 (en) 2007-08-15 2012-01-03 Cytokinetics, Inc. Certain chemical entities, compositions, and methods
WO2009104147A2 (en) 2008-02-20 2009-08-27 Actelion Pharmaceuticals Ltd Azatricyclic antibiotic compounds
PT2344495E (en) 2008-10-07 2015-04-01 Actelion Pharmaceuticals Ltd Tricyclic oxazolidinone antibiotic compounds
US7994357B2 (en) * 2009-04-03 2011-08-09 Naturewise Biotech & Medicals Corporation Cinamic compounds and derivatives therefrom for the inhibition of histone deacetylase
CN102850317B (en) 2011-06-27 2017-02-08 天士力制药集团股份有限公司 Substituted cinnamide derivative, its preparation method and application
AU2013221635B2 (en) 2012-02-16 2017-12-07 Santarus, Inc. Anti-VLA1 (CD49a) antibody pharmaceutical compositions
US9364535B2 (en) 2012-08-15 2016-06-14 The Regents Of The University Of California Methods and compositions for modulating lymphangiogenesis, e.g., to treat transplant rejection, in a subject
AU2013365742B2 (en) 2012-12-19 2016-11-24 Novartis Ag Autotaxin inhibitors
US9409895B2 (en) 2012-12-19 2016-08-09 Novartis Ag Autotaxin inhibitors
KR101498218B1 (en) * 2014-09-23 2015-03-12 연세대학교 산학협력단 Novel Pentadienoyl Piperidine Derivatives and Use Thereof
US11370761B2 (en) 2017-01-23 2022-06-28 Nippon Chemiphar Co., Ltd. Voltage-dependent T-type calcium channel inhibitor
EP4051678A1 (en) 2019-10-28 2022-09-07 Merck Sharp & Dohme Corp. Small molecule inhibitors of kras g12c mutant
EP4067343A4 (en) * 2019-11-29 2024-01-03 Taiho Pharmaceutical Co Ltd Novel phenol compound or salt thereof
GB202010626D0 (en) * 2020-07-10 2020-08-26 Univ Nottingham Compound

Citations (7)

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JPH04334357A (en) * 1991-05-02 1992-11-20 Fujirebio Inc Acyl derivative having enzyme-inhibiting action
WO1996029309A1 (en) * 1995-03-17 1996-09-26 Fujisawa Pharmaceutical Co., Ltd. N-ACYLPIPERIDINYLCARBONYLAMINOCARBOXYLIC ACIDS AND THEIR USE AS GLYCOPROTEIN IIB/IIa ANTAGONISTS AND FIBRINOGEN-BLOOD PLATELETS BINDING INHIBITORS
JPH08277285A (en) * 1995-04-06 1996-10-22 Fujisawa Pharmaceut Co Ltd Piperdine compound, its production and use
WO1998016512A1 (en) * 1996-10-15 1998-04-23 Basf Aktiengesellschaft New derivates from piperidine-keto acid, their preparation and use
WO1999025685A1 (en) * 1997-11-18 1999-05-27 Merck & Co., Inc. 4-substituted-4-piperidine carboxamide derivatives
WO2000059880A1 (en) * 1999-04-02 2000-10-12 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds
WO2001060813A1 (en) * 2000-02-17 2001-08-23 Fujisawa Pharmaceutical Co., Ltd. Beta-alanine derivatives and their use as receptor antagonists

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AU2001294552A1 (en) * 2000-09-11 2002-03-26 Temple University-Of The Commonwealth System Of Higher Education Compounds and methods for inhibiting alpha-1 beta-1 integrins

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH04334357A (en) * 1991-05-02 1992-11-20 Fujirebio Inc Acyl derivative having enzyme-inhibiting action
WO1996029309A1 (en) * 1995-03-17 1996-09-26 Fujisawa Pharmaceutical Co., Ltd. N-ACYLPIPERIDINYLCARBONYLAMINOCARBOXYLIC ACIDS AND THEIR USE AS GLYCOPROTEIN IIB/IIa ANTAGONISTS AND FIBRINOGEN-BLOOD PLATELETS BINDING INHIBITORS
JPH08277285A (en) * 1995-04-06 1996-10-22 Fujisawa Pharmaceut Co Ltd Piperdine compound, its production and use
WO1998016512A1 (en) * 1996-10-15 1998-04-23 Basf Aktiengesellschaft New derivates from piperidine-keto acid, their preparation and use
WO1999025685A1 (en) * 1997-11-18 1999-05-27 Merck & Co., Inc. 4-substituted-4-piperidine carboxamide derivatives
WO2000059880A1 (en) * 1999-04-02 2000-10-12 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds
WO2001060813A1 (en) * 2000-02-17 2001-08-23 Fujisawa Pharmaceutical Co., Ltd. Beta-alanine derivatives and their use as receptor antagonists

Non-Patent Citations (3)

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Title
HOEKSTRA ET AL: "Potent, Orally Active GPIIb/IIIa Antagonists Containing a Nipecotic Acid Subunit. Structure-Activity Studies Leading to the Discovery of RWJ-53308", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 42, no. 25, 1999, pages 5254 - 5265, XP002142349, ISSN: 0022-2623 *
PATENT ABSTRACTS OF JAPAN vol. 0171, no. 80 (C - 1046) 8 April 1993 (1993-04-08) *
PATENT ABSTRACTS OF JAPAN vol. 1997, no. 02 28 February 1997 (1997-02-28) *

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WO2005016883A2 (en) 2005-02-24
WO2005019177A1 (en) 2005-03-03

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