Mitsubishi Chemical Corporation

Mitsubishi Kasei Corporation

Norimichi Iwase

Yoshikuni Tamao

Yasuhiro Morinaka

Koichi Sugawara

Toshiji Kanayama

Masahiro Ohshima

Kumi Yamada

Naoto Inakoshi

Misao Okitsu

Masahiro Oshima

Jun Anabuki

Shigeo Sugiyama

Compounds represented by the general formula (I) wherein n represents 1 or 2; R,represents, for example, a C,-C,alkyl group which may be substituted with a C,-C,cycloalkyl group or carboxyl group; R,represents hydrogen atom, a C,-C,alkyl group or other; and R,represents amino group or amidino group, whose example include trans-4-amino-&lsqb;(S)-N-&lsqb;(S)-2-propoxycarbonylamino-3-isopropylthio-3-methyl-butanoyl&rsqb;prolyl&rsqb;aminomethylcyclohexane. The compounds have potent inhibitory activity against thrombin, and are useful as anticoagulants.

Penicillaminamide derivatives

A 1/2 sulfate of a [(S)-1-[(S)-2-[(trans-4-aminocyclohexylmethyl) carbamoyl]pyrrolidine-1-carbonyl]-2-isopropylthio-2-methylpropyl]carbamic acid propyl ester represented by the following formula (I): a hydrate or solvate thereof.

1/2 sulfate of a [(S) -1- [(S) -2- [(trans-4- aminocyclohexylmethyl)

A prolineamide derivative represented by the formula (I): ##STR1## or a salt or hydrate thereof or a pharmaceutically acceptable salt thereof, which has a protease inhibition activity and is useful as an active ingredient of pharmaceutical compositions is provided.

Prolineamide derivatives

A method is provided for treating a disease caused by smooth muscle cell hyperplasia. According to this method, there is administered to a patient suffering from said disease a therapeutically or prophylactically effective amount of an aminopyridazine derivative or a salt thereof represented by the formula: ##STR1##

Medicament for therapeutic and prophylactic treatment of diseases caused

A 3,6-disubstituted pyridazine derivative having excellent platelet agglutination inhibitory effects. It is useful for a preventive medicine or a therapeutic medicine for a cerebrovascular disorder such as cerebral thrombosis and cerebral embolism, an ischemic heart disease such as myocardial infarction, and a circulation disorder such as peripheral circulation disorder. A pharmaceutical composition containing a compound of the present invention as an effective ingredient and a process for preparing the same are also disclosed. The compound has the formula (I) ##STR1## wherein A represents an alkyl group having 3 to 6 carbon atoms; a cycloalkyl group having 5 to 7 carbon atoms; a phenyl group, a thienyl group, a furyl group, a thiazolyl group, a phenoxy group, a phenylalkyl group having 7 to 9 carbon atoms, a phenylthio group, a 5-6 membered saturated heterocyclic group containing one or more nitrogen atoms, a pyridyl group or an imidazolyl group each of which may have at least one substituent selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a halogen atom; B represents (a) --NH--D wherein D represents ##STR2## (4) --CH.sup.3 R.sup.4 ; or (5) an alkyl group having 3 to 8 carbon atoms; or ##STR3## and the ring C represents a benzene ring.

3,6-disubstituted pyradazine derivatives

4-Phenylphthalazine derivatives having platelet aggregation inhibitory activity of the formula: ##STR1## wherein R.sup.1 is an alkyl or hydroxyalkyl group of 1-5 carbon atoms; R.sup.2 is a hydrogen atom or an alkyl group of 1-5 carbon atoms; or R.sup.1 and R.sup.2, when taken together, may represent an alkylene group of 2-6 carbon atoms, said group optionally containing one or more oxygen atoms; R.sup.3 and R.sup.4 are independently a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, or when two of R.sup.3 are adjacently positioned, (R.sup.3)l may represent a --O--(CH.sub.2).sub.p --O-- group and/or when two of R.sup.4 are adjacently positioned, (R.sup.4).sub.m may represent a --O--(CH.sub.2).sub.p --O-- group; R.sup.5 is a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, a trifluoromethyl group or a hydroxy group, or when two of R.sup.5 are adjacently positioned, (R.sup.5).sub.n may represent a --O--(CH.sub.2).sub.p --O-- group; p is an integer of 1-3; l and m are independently an integer of 1-2; and n is an integer of 1-3, and optical isomers and pharmaceutically acceptable acid addition salts thereof.

Growing community of inventors

Yokohama, Japan

Norimichi Iwase