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Tobishi Yakuhin Kogyo Kabushiki Kaisha

Osamu Sakuma

Tadashi Morita

Tsutomu Inoue

Takashi Inaba

Tomohiko Ishikawa

Masayuki Yuasa

Masatoshi Hagiwara

Hiroyoshi Hidaka

Isao Umezawa

Tadashi Toshioka

Kenji Naitoh

Masayasu Kimura

Kenji Naito

Horoyoshi Hidaka

Shinpei Kidokoro

Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.

Compound having vessel smooth muscle relaxation activity

Derivatives of isoquinoline (and naphthalene) sulfonamides

A quaternary ammonium having a muscle relaxation activity compound represented by the formula (I): ##STR1## wherein R.sub.1 represents a methylene, a lower alkylenoxy, a lower alkenylene, a lower alkynylene, --CO--, --COO--, a lower alkylene carbonyloxy, --CH(OR.sub.5)--, a lower alkylenecarbonyl, a hydroxy lower alkylene, --O--, --S--, --SO--, or --SO.sub.2 --; R.sub.2 represents a hydrogen atom, a hydroxy lower alkyl, an aldehyde, a lower alkyl carbonyl, --NO.sub.2, or --NHR.sub.6 ; R.sub.3 represents a hydrogen atom of a group --R.sub.1 --(CH.sub.2).sub.a --[CH(CH.sub.2 A)--CH.sub.2 ].sub.b --A; R.sub.4 represents an anion; R.sub.5 and R.sub.6 represent a hydrogen atom or a acetyl; A represents a quaternary ammonium group; a represents an integer of 1 to 8; b represents 0 or 1; m represents an integer of 1 to 4; and (Z) represents a trivalent benzene ring, a trivalent naphthalene ring, a trivalent diphenyl or a trivalent ethane radical.

Quaternary ammonium compounds having muscle relaxation activity

Novel compounds represented by the formula: ##STR1## wherein R.sub.1 represents an alkyl group having 1 to 3 carbon atoms, R.sub.2 represents an amino group or a group of formula ##STR2## in which R.sub.4 represents an alkyl group having 1 to 3 carbon atoms, R.sub.5 represents an alkyl group having 1 to 3 carbon atoms or may combine with R.sub.6 to form a five or six membered ring containing 4 to 5 carbon atoms, R.sub.6 represents a hydrogen atom or may combine with R.sub.5 to form a five or six membered ring containing 4 to 5 carbon atoms, R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms or a halogen atom, X represents a carbonyl group or a methylene group, Y represents a sulfur atom or a vinylene group and pharmaceutically acceptable salts thereof which exhibit a vasodilating activity and inhibitory activity for platelet aggregation. Thus, they are useful as therapeutic agents for treatment of angina pectoris, hypertension, throbosis and the like.

Novel compounds exhibiting a vasodilating activity and inhibitory

Growing community of inventors

Tama, Japan

Osamu Sakuma