86208-18-6Relevant academic research and scientific papers
Integrin antagonists
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, (2008/06/13)
This invention relates to novel heterocycles which are useful as antagonists of the αvβ3 integrin, the α2bβ3 integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.
Amidinophenol derivatives
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, (2008/06/13)
Amidinophenol derivatives of the formula (I): STR1 wherein R1 and R2 are (i) H, (ii) C1-4 alkyl, (iii) C1-4 alkoxy, (iv) C2-5 acyl, (v) halogen, (vi) NO2, (vii) benzoyl, (viii) COOR4 (in which R4 is C1-3 alkyl); A is bond, C1-4 alkylene, --C(R5)=C(R6)-- (in which R5 and R6 are H or C1-4 alkyl; R3 is (i) CON(R7)(R8), (ii) CON(R9)--CH(R7)(R8) or (iii) STR2 in which STR3 is 4-7 membered, mono-cyclic hetero ring containing 1 or 2 N atom; R10 is H, C7-10 phenylalkyl or COOR13 (in which R13 is H, C1-4 alkyl or C7-10 phenylalkyl)); with the proviso that (i) both R7 and R8 do not represent hydrogen at the same time, and (ii) when at least one group in R7, R8 and R9 represents the group containing t-butyl ester, the other groups do not represent tile group containing carboxy; or an acid-addition salt thereof, have inhibitory activities on PLA2 and on various proteases such as trypsin, plasmin, thrombin, kallikrein, especially trypsin, and are useful for the prevention and/or the treatment of various inflammatory diseases, allergic diseases, disseminated intravascular coagulation, pancreatitis, severity in pancreatitis and multiple organ failure.
Synthesis and antitumor activities of novel 6-5 fused ring heterocycle antifolates: N-[4-[ω-(2-amino-4-substituted-6,7- dihydrocyclopenta[d]pyrimidin-5-yl)alkyl]benzoyl]-L-glutamic acids
Kotake,Iijima,Yoshimatsu,Tamai,Ozawa,Koyanagi,Kitoh,Nomura
, p. 1616 - 1624 (2007/10/02)
Novel antifolates with a 6-5 fused ring system, 6,7- dihydrocyclopenta[d]pyrimidine, (3a,b and 4a,b) were synthesized on the basis of combined modification of the heterocycle and bridge regions of the folate molecule. The synthetic method involves (1) syn
