138227-69-7Relevant articles and documents
Cinnamyl derivatives: Synthesis and factor Xa (FXa) inhibitory activities
Noguchi, Tetsuji,Tanaka, Naoki,Nishimata, Toyoki,Goto, Riki,Hayakawa, Miho,Sugidachi, Atsuhiro,Ogawa, Taketoshi,Asai, Fumitoshi,Fujimoto, Koichi
experimental part, p. 758 - 770 (2009/05/31)
To develop a potent and oral anticoagulant, a series of compounds with cinnamyl moiety was synthesized and their factor Xa (FXa) inhibitory activities were examined. As a result, some cinnamyl derivatives showed potent FXa inhibitory activities in vitro. Among them, compounds with substituent at the 3-position on the central benzene ring represented by (N-{4-[1-(acetimidoyl) piperidin-4-yloxy]-3-chlorophenyl}-N-[(E)-3-(3-amidinophenyl)-2-propenyl] sulfamoyl)acetic acid dihydrochloride (45b) and (N-{4-[1-(acetimidoyl)piperidin- 4-yloxy]-3-carbamoylphenyl}-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl) acetic acid dihydrochloride (45j) exhibited potent FXa inhibitory activities with IC50 values of less than 10 nM in vitro. These compounds also showed potent anticoagulant activities both in vitro and ex vivo. Furthermore, these compounds exhibited no lethal toxicity (30 mg/kg, i.v.).
The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer
Lippa, Blaise,Kauffman, Goss S.,Arcari, Joel,Kwan, Tricia,Chen, Jinshan,Hungerford, William,Bhattacharya, Samit,Zhao, Xumiao,Williams, Courtney,Xiao, Jun,Pustilnik, Leslie,Su, Chunyan,Moyer, James D.,Ma, Ling,Campbell, Mary,Steyn, Stefanus
, p. 3081 - 3086 (2008/02/03)
The synthesis and biological evaluation of potent and selective inhibitors of the erbB2 kinase is presented. Based on the 4-anilinoquinazoline chemotype, the syntheses of several new series of erbB2 inhibitors are described with quinazoline and pyrido[4,3
BENZAMIDINE DERIVATIVE
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Page 160, (2010/02/05)
Compounds of general formula (1) and pharmacologically acceptable salts thereof: ???[wherein ??????R1 represents a hydrogen atom, a halogen atom, an alkyl group or a hydroxyl group; ??????R2 represents a hydrogen atom or a halogen atom; ??????R3 represents a hydrogen atom, an alkyl group which may be substituted, an aralkyl group, an alkylcarbonyl group which may be substituted, an alkylsulfonyl group which may be substituted or the like; ??????each of R4 and R5 represents a hydrogen atom, a halogen atom, an alkyl group which may be substituted, a carbamoyl group or the like; ??????R6 represents a heterocycle or the like; ??????each of R7 and R8 represents a hydrogen atom, an alkyl group or the like; ??????n represents 0, 1 or 2] ???exhibit excellent activated blood coagulation factor X inhibitory activity and are useful for the prevention or treatment of blood coagulation-related diseases.
BENZAMIDINE DERIVATIVES
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, (2008/06/13)
Benzamidine derivatives of formula (I) or pharmaceutically acceptable salts thereof exhibit excellent inhibitory activity against factor Xa and are useful for treating or preventing blood coagulation disorders: wherein R 1represents a hydrogen atom, a halogen atom, an alkyl group or a hydroxyl group; R 2represents a hydrogen atom, a halogen atom or an alkyl group, R 3represents a hydrogen atom, an optionally substituted alkyl group, an aralkyl group, an optionally substituted alkanoyl group or an optionally substituted alkylsulfonyl group, R 4and R 5 are the same as or different from each other and each represent a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an alkoxy group, a carboxyl group, an alkoxycarbonyl group or an optionally substituted carbamoyl group, and R 6represents a substituted pyrrolidine group or substituted piperidine group.
Aminobenzene compounds to prevent nerve cell degradation
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, (2008/06/13)
A compound useful for central antioxidant having inhibitory activity of degeneration and necrocytosis of cerebral cells of the formula (I): STR1 wherein A and B are independently (1) a group of the formula: STR2 wherein R1 and R2 are independently hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted heterocyclic group, or R1 together with R2 and the nitrogen atom to which they are bound may form a cyclic amino group, provided that both R1 and R2 are not hydrogen atom at the same time, or (2) a group of the formula: STR3 wherein D is O or S, R3 is hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group, m is 1, 2, or 3 and n is 0, 1, 2, 3 or 4; p is 1 or 2, provided that both A may be the same or different when p is 2; and R4, R5 and R6 are independently hydrogen atom, a lower alkyl or a lower alkoxy, or R5 and R6 may bond together to form --CH=CH--CH=CH--, or a salt thereof.