Sumitomo Pharmaceuticals Company Limited

Sumitomo Chemical Company, Limited

Dainippon Sumitomo Pharma Co., Ltd.

Naohito Ohashi

Kikuo Ishizumi

Masahumi Kitano

Masami Muraoka

Shoji Nagata

Junki Katsube

Koji Morishita

Masatoshi Yuri

Hideki Yagi

Kazuki Matsui

Kazuhiro Nakano

Atsuyuki Kojima

Kozo Shimago

Takaharu Ikeda

Akira Miyagishi

Nagisa Aida

Masashi Tanaka

Tsuyoshi Noguchi

Yoshihiro Tanaka

Hitoshi Ban

Isamu Maruyama

Norihiko Tanno

Shunji Aono

Hiromi Sato

Norio Fujiwara

Masaru Fukui

Yoshinori Takashima

Hiroyuki Mizote

Michihisa Muramatsu

Yoshihide Ueno

Yutaka Ueda

Masashi Nakatsuka

Seiji Katayama

Kikuo Ioshizumi

Teruo Sakurama

Naonori Imazaki

Shinya Morisada

Masafumi Kitano

Takaaki Yamamoto

Koji Fujimoto

Katsuhisa Ioriya

An optically active form of the quinazolinone derivatives represented by the general formula (1): [wherein Y represents a phenyl group or C2-C7 alkyl group; E represents &#x2014;CH&#x2550; or nitrogen atom; and R represents a C1-C4 alkyl group and so on], or pharmaceutically acceptable salts thereof, has a selective antagonism for the M3 muscarinic receptor and depressant action on the frequency of rhythmic bladder contractions, and it is useful for the treatment of pollakiuria and urinary incontinence.

Quinazolinone derivative

A compound represented by the formula (1): wherein R&#x2014;X&#x2014; indicates that 1 to 4 R&#x2014;X&#x2014; groups are present which may be the same or different,

Rho kinase inhibitors

Substituted guanidine derivatives

Quinazolinone derivatives

Pyridone derivatives and process for preparing the same

Naphthyridine derivatives

Substituted guanidine derivatives and process for producing the same

A process for preparing a pyridone derivative (4), which comprises reacting the compound (1) with a hypochlorite or a hypobromite or with lead tetraacetate to give the compound (2), and reacting the compound (2) with the compound (3). Said process is preferably especially from the standpoint of safety.

Preparation of pyridone derivatives using phthalimido containing starting material

A substituted guanidine derivative represented by the general formula:

Substituted guanidine derivatives, process for production thereof, and pharmaceutical uses thereof

Novel indoloylguanidine derivatives shown by formula (1), wherein R,represents one or more, the same or different substituent(s) which is selected from the group consisting of a hydrogen atom, an alkyl group, a substituted alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a halogen atom, nitro group, an acyl group, carboxyl group, an alkoxycarbonyl group, an aromatic group, and a group shown by formula: &mdash;OR,, &mdash;NR,R,, &mdash;SO,NR,R,or &mdash;S(O),R,; and R,represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, hydroxy group, an alkoxy group or a group shown by formula: &mdash;CH,R,; and which inhibit the Na,/H,exchanger activity and are useful for the treatment and prevention of a disease caused by increased Na,/H,exchanger activity, such as hypertension, arrhythmia, angina pectoris, cardiac hypertrophy, diabetes, disorders associated with ischemia or ischemic reperfusion, cerebro-ischemic disorders; or diseases caused by excessive cell proliferation.

Indoloylguanidine derivatives

LDL receptor gene expression promoters

A substituted guanidine derivative represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a hydrogen atom, an unsubstituted alkyl group, a substituted alkyl group, a halogen atom or the like; Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4, Y.sub.5, Y.sub.6 and Y.sub.7, which may be the same or different, are independently a single bond, --CH.sub.2 --, --O--, --CO-- or the like, adjacent members of a group consisting of Y.sub.1 through Y.sub.7 being able to be taken together to represent --CH.dbd.CH--, and at least two of Y.sub.1 through Y.sub.7 being independently a group other than a single bond; Z may be absent, or one or more Zs may be present and are, the same or different, independently a substituent for a hydrogen atom bonded to any of the carbon atoms constituting the ring formed by Y.sub.1 through Y.sub.7, for example, an unsubstituted alkyl group or a substituted alkyl group, or a pharmaceutically acceptable acid addition salt thereof, is useful as a therapeutic or prophylactic agent for diseases caused by the acceleration of the sodium/proton (Na.sup.+ /H.sup.+) exchange transport system, for example, hyperpiesia, arrhythmia, angina pectoris, hypercardia, diabetes, organopathies due to ischemia or ischemia re-perfusion, troubles due to cerebral ischemia, diseases caused by cell over-proliferations, and diseases caused by trouble with endothelial cells.

Substituted guanidine derivatives, process for production thereof, and

Naphthyridine derivative of the formula: ##STR1## wherein Ring A is substituted or unsubstituted pyridine, X is --N(R.sup.2)--CO--(R.sup.2 is H, alkyl, substituted alkyl, etc.), Z is a direct bond, --NH--, C.sub.1 -C.sub.2 alkylene, or --CH.dbd.CH--, Y is alkyl, substituted alkyl, aromatic group or substituted aromatic group, etc., B is alkyl, substituted alkyl, aromatic group or substituted aromatic group, or an acid addition salt thereof, these compounds having acyl-CoA: cholesterol acyl transferase inhibitory activity, and being useful as an agent for prophylaxis or treatment of hyperlipidemia, atherosclerosis, and related diseases thereof.

A substituted guanidine derivative represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a hydrogen atom, an unsubstituted alkyl group, a substituted alkyl group, a halogen atom or the like; Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4, Y.sub.5, Y .sub.6 and Y.sub.7, which may be the same or different, are independently a single bond, --CH.sub.2 --, --O--, --CO--or the like, adjacent members of a group consisting of Y.sub.1 through Y.sub.7 being able to be taken together to represent --CH.dbd.CH--, and at least two of Y.sub.1 through Y.sub.7 being independently a group other than a single bond; Z may be absent, or one or more Zs may be present and are, the same or different, independently a substituent for a hydrogen atom bonded to any of the carbon atoms constituting the ring formed by Y.sub.1 through Y.sub.7, for example, an unsubstituted alkyl group or a substituted alkyl group, or a pharmaceutically acceptable acid addition salt thereof, is useful as a therapeutic or prophylactic agent for diseases caused by the acceleration of the sodium/proton (Na.sup.+ /H.sup.+) exchange transport system, for example, hyperpiesia, arrhythmia, angina pectoris, hypercardia, diabetes, organopathies due to ischemia or ischemia re-perfusion, troubles due to cerebral ischemia, diseases caused by cell overproliferations, and diseases caused by trouble with endothelial cells.

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Takatsuki, Japan

Naohito Ohashi