157023-34-2Relevant articles and documents
N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
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, (2008/06/13)
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
Discovery of diaminobutane derivatives as Ca(2+)-permeable AMPA receptor antagonists.
Yoneda, Yoshiyuki,Mimura, Tetuya,Kawagoe, Keiichi,Yasukouchi, Takanori,Tatematu, Toshiaki,Ito, Masayuki,Saito, Masaki,Sugimura, Masunobu,Kito, Fusako,Kawajiri, Shinichi
, p. 1347 - 1359 (2007/10/03)
We designed and synthesized a series of the polyamine derivatives as potent Ca(2+)-permeable AMPA receptor antagonists. In the course of this study, we found that the polyamine derivatives exhibited strong hypotensive activity which was undesirable activity for neuroprotective agents. Therefore, we tried to find non-hypotensive antagonists by structural modification of such compounds. Through this derivatization, we obtained the diamine compounds having desired profiles. Especially, compound 8f, which was non-hypotensive and potent Ca(2+)-permeable AMPA receptor antagonist, showed neuroprotective effects in transient global ischemia models in gerbils.
N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists
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, (2019/08/08)
Compounds represented by Formula (I): 1or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
N-SUBSTITUTED-N'-SUBSTITUTED UREA DERIVATIVE AND USE THEREOF AS TNF-γ(a) PRODUCTION INHIBITOR
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Page 10, (2008/06/13)
N-Substituted-N'-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF- α production inhibitory activity.
Synthesis of polyamine derivatives having non-hypotensive Ca2+-permeable AMPA receptor antagonist activity
Yoneda, Yoshiyuki,Kawajiri, Shinichi,Hasegawa, Atushi,Kito, Fusako,Katano, Sumie,Takano, Emi,Mimura, Tetuya
, p. 1261 - 1264 (2007/10/03)
In order to obtain non-hypotensive and Ca2+-permeable AMPA receptor antagonists, we have synthesized a series of 1,4-bis(4-piperidinylmethyl)diaminobutanes. Compounds 13b, c, f had desirable properties.
Dibasic inhibitors of human mast cell tryptase. Part 3: Identification of a series of potent and selective inhibitors containing the benzamidine functionality
Dener, Jeffrey M.,Rice, Kenneth D.,Newcomb, William S.,Wang, Vivian R.,Young, Wendy B.,Gangloff, Anthony R.,Kuo, Elaine Y.-L.,Cregar, Lynne,Putnam, Daun,Wong, Martin
, p. 1629 - 1633 (2007/10/03)
A survey of charged groups and linkers for a series of symmetrical and unsymmetrical dibasic inhibitors is described, leading to several classes of potent and selective inhibitors. In particular, the benzamidine functionality was identified as the most potent charged group investigated.
SRC kinase inhibitor compounds
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, (2008/06/13)
Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of proteins tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.
Fibrinogen receptor antagonists
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, (2008/06/13)
Novel fibrinogen receptor antagonists of the formula: are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.