4-Benzylamino-1-chloro-6-substituted Phthalazines: Synthesis and Inhibitory Activity toward Phosphodiesterase 5
摘要:
We synthesized various 4-benzylamino-1-chloro-6-substituted phthalazines (15) and 4-benzylamino-1-chloro-7-substituted phthalazines (16) and evaluated their inhibitory activity toward phosphodiesterase 5 (PDE5) purified from porcine platelets. The PDE5-inhibitory activities of 15 were greater than those of the isomers (16). The preferred substituent at the 4-position of phthalazine was a (3-chloro-4-methoxybenzyl)amino group, and those at the B-position were cyano, nitro, and trifluoromethyl groups. Compounds 15a (IC50 = 4.8 nM), 15f (3.5 nM), and 15i (5.3 nM) were more potent inhibitors than E4021 (8.6 nM). Compounds 15a and 15f also showed vasorelaxant activity in isolated porcine coronary arteries precontracted with prostaglandin F-2 alpha (10(-5) M). The EC50 values for vasorelaxant action of 15a, 15f, and E4021 were 150, 160, and 980 nM, respectively. These results show that novel PDE5 inhibitors possessing a potent vasorelaxant effect may exist among phthalazine derivatives.
A fused pyridazine compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof which exhibits an inhibitory activity against cyclic GMP phosphodiesterase (hereinafter referred to as "cGMP-PDE"). The compounds are useful as preventive and therapeutic agents for diseases for which a cGMP-PDE inhibiting action is efficacious, for example, ischemic heart diseases such as angina pectoris, myocardial infarct and chronic and acute cardiac failure, pulmonary hypertension, arteriosclerosis and bronchial asthma. ##STR1##
Amide-imide copolymer resin of lowered water absorption and composites made therefrom
申请人:AMOCO CORPORATION
公开号:EP0417897A1
公开(公告)日:1991-03-20
Polyamide-imide matrix resins derived from trimellitic acid compounds and an aromatic diamine are improved in moisture resistance when from 10 to about 90 mole % of the trimellitic acid compounds are replaced by biphenyl tetracarboxylic acid compounds. The matrix resins are particularly useful for fiber-filled composites having improved retention of properties when exposed to moisture.
Improved imide-containing copolymers comprising, in the aromatic diamine component, p-phenylene diamine and at least one additional aromatic diamine have increased rigidity and useful processability. The copolymers of this invention also may exhibit improved resistance to the detrimental effects of humid environments and retain mechanical properties at elevated temperatures after exposure to humid environments
A fused pyridazine compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof which exhibits an inhibitory activity against cyclic GMP phosphodiesterase (hereinafter referred to as "cGMP-PDE").
The compounds are useful as preventive and therapeutic agents for diseases for which a cGMP-PDE inhibiting action is efficacious, for example, ischemic heart diseases such as angina pectoris, myocardial infarct and chronic and acute cardiac failure, pulmonary hypertension, arteriosclerosis and bronchial asthma.
Production method of beta-type copper phthalocyanine pigment
申请人:DAINIPPON INK AND CHEMICALS, INC.
公开号:EP0783029A1
公开(公告)日:1997-07-09
A production method of beta-type copper phthalocyanine pigment comprising steps of: a) producing a reaction mixture containing crude copper phthalocyanine in an organic solvent; b) wet-grounding the reaction mixture by mechanical energy to form a suspension; c) removing the organic solvent from the obtained suspension does not contaminate the work environment and represents an improvement in terms of both productivity and economic savings compared with conventional methods. The beta-type copper phthalocyanine pigment produced by this method demonstrates excellent dispersability, such that it may be dispersed without further modification in a resin, varnish, plastic or other medium as required, to produce a paint, ink, or plastic tinting agent, for example.