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Title:
m-SUBSTITUTED BENZOIC ACID DERIVATIVES EXHIBITING INTEGRIN$g(a)¿v?$g(b)¿3? ANTAGONISM
Document Type and Number:
WIPO Patent Application WO/2001/027090
Kind Code:
A1
Abstract:
m-Substituted benzoic acid derivatives represented by general formula (I) and exhibiting integrin alpha v beta 3 antagonism; and intermediates for preparing the same [wherein A is an optionally substituted mono- or bi-cyclic heterocycle group containing two nitrogen atoms, or the like; D is a bond, >NR<4>, >CR<5>R<6>, -NR<4>-CR<5>R<6>-, or the like; X is CH or N; R<7> to R<9> are each hydroxyl, alkyl, or the like; Q is >C=O or the like; J is a bond or alkylene; and R<10> is optionally substituted hydroxyl, amino, or the like]. These derivatives are useful in the treatment or prevention of cardiovascular diseases, vascularization-related diseases, cerebrovascular diseases, cancers and metastases thereof, immunologic diseases, bone diseases, and so on.

Inventors:
AJITO KEIICHI (JP)
ISHIKAWA MINORU (JP)
KUBOTA DAI (JP)
MURAKAMI SHOICHI (JP)
YAMAMOTO MIKIO (JP)
YAHATA NAOKAZU (JP)
FUJISHIMA KAZUYUKI (JP)
OYAMA MAKOTO (JP)
Application Number:
PCT/JP2000/007031
Publication Date:
April 19, 2001
Filing Date:
October 10, 2000
Export Citation:
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Assignee:
MEIJI SEIKA KAISHA (JP)
AJITO KEIICHI (JP)
ISHIKAWA MINORU (JP)
KUBOTA DAI (JP)
MURAKAMI SHOICHI (JP)
YAMAMOTO MIKIO (JP)
YAHATA NAOKAZU (JP)
FUJISHIMA KAZUYUKI (JP)
OYAMA MAKOTO (JP)
International Classes:
A61P7/02; A61P9/00; A61P9/02; A61P19/00; A61P35/00; C07C229/54; C07C229/60; C07D239/14; C07D239/42; C07D401/12; (IPC1-7): C07D239/42; C07D239/14; C07D401/04; C07D403/04; C07D211/52; C07C229/54; A61K31/606; A61P7/02; A61P9/00; A61P19/00; A61P35/00
Domestic Patent References:
WO1999052872A11999-10-21
WO1999038849A11999-08-05
Foreign References:
US4032676A1977-06-28
Other References:
K.C. NICOLAOU ET AL.: "Design, synthesis and biological evaluation of nonpeptide integrin antagonists", BIOORG. MED. CHEM., vol. 6, no. 8, 1998, pages 1185 - 1208, XP002935433
TAYLOR E.C. ET AL.: "A convenient synthesis of 1-aryl-4-piperidones", SYNTHESIS, no. 8, 1981, pages 606 - 608, XP002935434
SU TSANN LONG ET AL.: "Synthesis of 4-((1,3-diamonipyrrolo(3',4':4,5)pyrido(2,3-d)pyrimidin-8-yl)benzoyl)-L-glutamic acid as a potential antifolate", J. HETEROCYCL. CHEM., vol. 30, no. 5, 1993, pages 1437 - 1443, XP002935435
Attorney, Agent or Firm:
Sato, Kazuo (Fuji Bldg. 2-3 Marunouchi 3-chome Chiyoda-ku, Tokyo, JP)
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