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Phenylalanine derivative

Info

Publication number
WO2003089410A1
WO2003089410A1 PCT/JP2003/004970 JP0304970W WO2003089410A1 WO 2003089410 A1 WO2003089410 A1 WO 2003089410A1 JP 0304970 W JP0304970 W JP 0304970W WO 2003089410 A1 WO2003089410 A1 WO 2003089410A1
Authority
WO
Grant status
Application
Patent type
Prior art keywords
un
derivative
etc
alkyl
lower
Prior art date
Application number
PCT/JP2003/004970
Other languages
French (fr)
Inventor
Yoshisuke Nakasato
Kiminori Ohta
Eri Arai
Osamu Saku
Hiroko Kusaka
Satoshi Nakanishi
Haruhiko Manabe
Akira Ogawa
Original Assignee
Kyowa Hakko Kogyo Co., Ltd.
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

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with heteroatoms or with carbon atoms having three bonds to hetero atoms, with at the most one to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Abstract

A phenylalanine derivative represented by the formula (I): (I) (wherein m and n are the same or different and each is 1 or 2; R2 represents (un)substituted lower alkyl, etc.; R1 represents (un)substituted lower alkyl, etc.; and R3, R4, R5, and R6 are the same or different and each is hydrogen, (un)substituted lower alkyl, oxo, etc.) or a pharmacologically acceptable salt of the derivative. They are useful as an α4 integrin inhibitor.
PCT/JP2003/004970 2002-04-19 2003-04-18 Phenylalanine derivative WO2003089410A1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2002-117841 2002-04-19
JP2002117841 2002-04-19

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP2003586131A JPWO2003089410A1 (en) 2002-04-19 2003-04-18 Phenylalanine derivatives

Publications (1)

Publication Number Publication Date
WO2003089410A1 true true WO2003089410A1 (en) 2003-10-30

Family

ID=29243507

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2003/004970 WO2003089410A1 (en) 2002-04-19 2003-04-18 Phenylalanine derivative

Country Status (2)

Country Link
JP (1) JPWO2003089410A1 (en)
WO (1) WO2003089410A1 (en)

Cited By (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006068058A1 (en) 2004-12-20 2006-06-29 Eisai R & D Management Co., Ltd. Crystal and salt of 1-cyclopropylmethyl-4-[2-(3,3,5,5)-tetramethylcyclohexyl)phenyl]piperazine
WO2007060408A2 (en) * 2005-11-23 2007-05-31 Astrazeneca Ab L-phenylalanine derivatives and their use as integrin antagonists
WO2007088041A1 (en) * 2006-01-31 2007-08-09 Jerini Ag Compounds for the inhibition of integrins and use thereof
WO2007141473A1 (en) * 2006-06-09 2007-12-13 Astrazeneca Ab N-(benzoyl)-o- [2- (pyridin- 2 -ylamino) ethyl] -l-tyrosine derivatives and related compounds as a5b1 antagonists for the treatment of solid tumors
JP2007537163A (en) * 2004-05-06 2007-12-20 サイトキネティクス・インコーポレーテッドCytokinetics Incorporated Compounds, compositions, and methods
WO2008064823A1 (en) * 2006-11-27 2008-06-05 Ucb Pharma, S.A. Bicyclic and heterobicyclic derivatives, processes for preparing them and their uses
WO2008093065A1 (en) * 2007-01-29 2008-08-07 Astrazeneca Ab L-ALANINE DERIVATIVES AS α5βL ANTAGONISTS
WO2008093064A1 (en) * 2007-01-29 2008-08-07 Astrazeneca Ab L-ALANINE DERIVATIVES AS α5 BETA 1 ANTAGONISTS
US7410971B2 (en) 2004-12-24 2008-08-12 Eisai R&D Management Co., Ltd. 1,2-di(cyclic)substituted benzene compounds
US7563795B2 (en) 2003-09-26 2009-07-21 Vertex Pharmaceuticals Incorporated Phenyl-piperazine derivatives as modulators of muscarinic receptors
US7723345B2 (en) 2005-12-29 2010-05-25 Lexicon Pharmaceuticals, Inc. Multicyclic amino acid derivatives and methods of their use
WO2010075249A2 (en) 2008-12-22 2010-07-01 Genentech, Inc. A method for treating rheumatoid arthritis with b-cell antagonists
WO2011162409A1 (en) * 2010-06-22 2011-12-29 Shionogi & Co., Ltd. Compounds having trpv1 antagonistic activity and uses thereof
US8309735B2 (en) 2006-05-12 2012-11-13 Shire Orphan Therapies Gmbh Heterocyclic compounds for the inhibition of integrins and use thereof
JP2013520497A (en) * 2010-02-24 2013-06-06 リサーチ・トライアングル・インスティチュート Aryl piperazine opioid receptor antagonists
WO2013101771A2 (en) 2011-12-30 2013-07-04 Genentech, Inc. Compositions and method for treating autoimmune diseases
WO2013116287A1 (en) 2012-01-31 2013-08-08 Genentech, Inc. Anti-ig-e m1' antibodies and methods using same
WO2013161904A1 (en) * 2012-04-24 2013-10-31 味の素株式会社 Sulfonamide derivative and medicinal use thereof
JP2015505842A (en) * 2011-12-12 2015-02-26 レセプトス インコーポレイテッドReceptos, Inc. Carboxylic acid derivatives containing four rings which act as glp-1 receptor modulators for the treatment of diseases such as diabetes
WO2015064580A1 (en) * 2013-10-29 2015-05-07 味の素株式会社 Sulfonamide derivative and medicinal use thereof
EP3095463A2 (en) 2008-09-16 2016-11-23 F. Hoffmann-La Roche AG Methods for treating progressive multiple sclerosis
EP3130349A1 (en) 2004-06-04 2017-02-15 Genentech, Inc. Method for treating multiple sclerosis
EP3052515A4 (en) * 2013-09-30 2017-03-15 Univ California Anti-alphavbeta1 integrin compounds and methods
WO2017062682A2 (en) 2015-10-06 2017-04-13 Genentech, Inc. Method for treating multiple sclerosis

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001036376A1 (en) * 1999-11-18 2001-05-25 Ajinomoto Co., Inc. Novel phenylalanine derivatives

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001036376A1 (en) * 1999-11-18 2001-05-25 Ajinomoto Co., Inc. Novel phenylalanine derivatives

Cited By (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7563795B2 (en) 2003-09-26 2009-07-21 Vertex Pharmaceuticals Incorporated Phenyl-piperazine derivatives as modulators of muscarinic receptors
JP4805916B2 (en) * 2004-05-06 2011-11-02 サイトキネティクス・インコーポレーテッドCytokinetics Incorporated Compounds, compositions, and methods
JP2007537163A (en) * 2004-05-06 2007-12-20 サイトキネティクス・インコーポレーテッドCytokinetics Incorporated Compounds, compositions, and methods
EP3130349A1 (en) 2004-06-04 2017-02-15 Genentech, Inc. Method for treating multiple sclerosis
JPWO2006068058A1 (en) * 2004-12-20 2008-06-12 エーザイ・アール・アンド・ディー・マネジメント株式会社 1-cyclopropylmethyl-4- [2- (3,3,5,5-tetramethyl-cyclohexyl) phenyl] piperazine salts and crystalline
US7910734B2 (en) 2004-12-20 2011-03-22 Eisai R&D Management Co., Ltd. Crystal and salt of 1-cyclopropylmethyl-4-[2-(3,3,5,5-tetramethylcyclohexyl)phenyl]piperazine
WO2006068058A1 (en) 2004-12-20 2006-06-29 Eisai R & D Management Co., Ltd. Crystal and salt of 1-cyclopropylmethyl-4-[2-(3,3,5,5)-tetramethylcyclohexyl)phenyl]piperazine
US7410971B2 (en) 2004-12-24 2008-08-12 Eisai R&D Management Co., Ltd. 1,2-di(cyclic)substituted benzene compounds
WO2007060408A2 (en) * 2005-11-23 2007-05-31 Astrazeneca Ab L-phenylalanine derivatives and their use as integrin antagonists
WO2007060408A3 (en) * 2005-11-23 2007-08-02 Astrazeneca Ab L-phenylalanine derivatives and their use as integrin antagonists
US8063057B2 (en) 2005-12-29 2011-11-22 Lexicon Pharmaceuticals, Inc. Multicyclic amino acid derivatives and methods of their use
EP2386547A1 (en) 2005-12-29 2011-11-16 Lexicon Pharmaceuticals, Inc. Multicyclic amino acid derivatives and methods of their use
US7723345B2 (en) 2005-12-29 2010-05-25 Lexicon Pharmaceuticals, Inc. Multicyclic amino acid derivatives and methods of their use
US8629156B2 (en) 2005-12-29 2014-01-14 Lexicon Pharmaceuticals, Inc. Tryptophan hydroxylase inhibitors
US8927534B2 (en) 2006-01-31 2015-01-06 Shire Orphan Therapies Gmbh Compounds for the inhibition of integrins and use thereof
JP2009525296A (en) * 2006-01-31 2009-07-09 イエリニ・アクチェンゲゼルシャフトJerini Ag Integrin inhibitory compounds and their use
WO2007088041A1 (en) * 2006-01-31 2007-08-09 Jerini Ag Compounds for the inhibition of integrins and use thereof
US8309735B2 (en) 2006-05-12 2012-11-13 Shire Orphan Therapies Gmbh Heterocyclic compounds for the inhibition of integrins and use thereof
WO2007141473A1 (en) * 2006-06-09 2007-12-13 Astrazeneca Ab N-(benzoyl)-o- [2- (pyridin- 2 -ylamino) ethyl] -l-tyrosine derivatives and related compounds as a5b1 antagonists for the treatment of solid tumors
WO2008064823A1 (en) * 2006-11-27 2008-06-05 Ucb Pharma, S.A. Bicyclic and heterobicyclic derivatives, processes for preparing them and their uses
WO2008093065A1 (en) * 2007-01-29 2008-08-07 Astrazeneca Ab L-ALANINE DERIVATIVES AS α5βL ANTAGONISTS
WO2008093064A1 (en) * 2007-01-29 2008-08-07 Astrazeneca Ab L-ALANINE DERIVATIVES AS α5 BETA 1 ANTAGONISTS
US9683047B2 (en) 2008-09-16 2017-06-20 Genentech, Inc. Methods for treating progressive multiple sclerosis
EP3095463A2 (en) 2008-09-16 2016-11-23 F. Hoffmann-La Roche AG Methods for treating progressive multiple sclerosis
WO2010075249A2 (en) 2008-12-22 2010-07-01 Genentech, Inc. A method for treating rheumatoid arthritis with b-cell antagonists
US9750738B2 (en) 2010-02-24 2017-09-05 Research Triangle Institute Arylpiperazine opioid receptor antagonists
JP2013520497A (en) * 2010-02-24 2013-06-06 リサーチ・トライアングル・インスティチュート Aryl piperazine opioid receptor antagonists
US9273027B2 (en) 2010-02-24 2016-03-01 Research Triangle Institute Arylpiperazine opioid receptor antagonists
JP2013529593A (en) * 2010-06-22 2013-07-22 塩野義製薬株式会社 Compound and its use with Trpv1 inhibitory activity
WO2011162409A1 (en) * 2010-06-22 2011-12-29 Shionogi & Co., Ltd. Compounds having trpv1 antagonistic activity and uses thereof
US8921373B2 (en) 2010-06-22 2014-12-30 Shionogi & Co., Ltd. Compounds having TRPV1 antagonistic activity and uses thereof
JP2015505842A (en) * 2011-12-12 2015-02-26 レセプトス インコーポレイテッドReceptos, Inc. Carboxylic acid derivatives containing four rings which act as glp-1 receptor modulators for the treatment of diseases such as diabetes
WO2013101771A2 (en) 2011-12-30 2013-07-04 Genentech, Inc. Compositions and method for treating autoimmune diseases
WO2013116287A1 (en) 2012-01-31 2013-08-08 Genentech, Inc. Anti-ig-e m1' antibodies and methods using same
CN104395297A (en) * 2012-04-24 2015-03-04 味之素株式会社 Sulfonamide derivative and medicinal use thereof
US9533985B2 (en) 2012-04-24 2017-01-03 Ea Pharma Co., Ltd. Sulfonamide derivative and medicinal use thereof
RU2607081C2 (en) * 2012-04-24 2017-01-10 ЕА Фарма Ко., Лтд. Sulfonamide derivative and medicinal use thereof
WO2013161904A1 (en) * 2012-04-24 2013-10-31 味の素株式会社 Sulfonamide derivative and medicinal use thereof
JPWO2013161904A1 (en) * 2012-04-24 2015-12-24 味の素株式会社 Sulfonamide derivatives and their pharmaceutical use
EP3052515A4 (en) * 2013-09-30 2017-03-15 Univ California Anti-alphavbeta1 integrin compounds and methods
US9822110B2 (en) 2013-10-29 2017-11-21 Ea Pharma Co., Ltd. Sulfonamide derivative and pharmaceutical use thereof
WO2015064580A1 (en) * 2013-10-29 2015-05-07 味の素株式会社 Sulfonamide derivative and medicinal use thereof
WO2017062682A2 (en) 2015-10-06 2017-04-13 Genentech, Inc. Method for treating multiple sclerosis

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