Tanabe Seiyaku Company, Limited

Tanabe Seiyaky Co., Ltd.

Koichiro Yamada

Kohei Kikkawa

Kenji Omori

Kenji Matsuki

Masataka Hikota

Rikako Kohno

Sumihiro Nomura

Hiroshi Iwata

Kosuke Yasuda

Mamoru Matsumoto

Hideo Nakai

Masaaki Nagasaki

Toshiro Shikano

Ryuichi Ishida

Michio Yamamura

Kunio Nosaka

Yasuhiko Sato

K Osuke Yasuda

Shumihiro Nomura

Yuichi Koga

Takeshi Yura

1. A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof, 

Pyrazine derivatives

A cyclic compound of the formula (I) or a pharmacologically acceptable salt thereof,  The compound of the present invention has excellent selective PDE V inhibitory activity and therefore, is useful as a therapeutic or prophylactic drug for treating various diseases due to functional disorders on cGMP-signaling.

Pyrimidine compounds

A pyridopyrimidine or a naphthyridine derivative of the formula (I): wherein Ris an optionally substituted nitrogen-containing heterocyclic group, etc.; Ris H or a lower alkyl group; Ris H or an optionally substituted lower alkyl group, etc.; Ris H, a lower alkyl group, COOH, etc.; Ris a lower alkyl group which may optionally be substituted by an optionally substituted aryl etc.; one of X and Y is CH and the other is nitrogen, or both of X and Y are nitrogen; or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent PDE V inhibitory activities, and being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.

Pyridopyrimidine or naphthyridine derivative

Aromatic nitrogen-containing 6-membered cyclic compounds

Agent for prophylaxis or treatment of dysuria

2-oxoindoline derivative

Novel sulfonamide derivatives of the formula �I!: ##STR1## wherein Ring A and Ring B are substituted or unsubstituted monocyclic, bicyclic or tricyclic hydrocarbon, or substituted or unsubstituted heterocyclic group, Q is single bond, --O--, --S--, --SO--, --SO.sub.2 -- or --CH.sub.2 --, Y is --0--, --S-- or --NH--, Alk is lower alkylene or alkenylene, Z is --O-- or --NH --, R is substituted or unsubstituted aromatic heterocyclic or aryl, R.sup.1 is H, substituted or unsubstituted amino, substituted or unsubstituted lower alkyl, alkenyl, alkynyl, substituted or unsubstituted lower alkylthio, or alkoxy, or substituted or unsubstituted heterocyclic or aryl, or pharmaceutically acceptable salts thereof, which are useful in the prophylaxis or treatment of disorders associated with endothelin activities such as hypertension, pulmonary hypertension, renal hypertension, Raynaud disease, bronchial asthma, gastric ulcer, chronic heart failure, etc.

Sulfonamide derivative and process for preparing the same

A benzenesulfonamide derivative of the formula �I!: ##STR1## wherein Ring A and Ring B are the same or different and each substituted or unsubstituted benzene ring, Q is a single bond or a group of the formula: --O--, --S--, --SO--, --SO.sub.2 -- or --CH.sub.2 --, Y is a group of the formula: --O--, --S-- or --NH--, Alk is lower alkylene group or lower alkenylene group, Z is a single bond or a group of the formula: --O-- or --NH--, R is a substituted or unsubstituted aromatic heterocyclic or aryl group, R.sup.1 is hydrogen atom, trifluoromethyl group, substituted or unsubstituted lower alkyl group, substituted or unsubstituted lower alkenyl group, mono- or di-lower alkylamino group, substituted or unsubstituted lower alkylthio group, substituted or unsubstituted lower alkoxy group, substituted or unsubstituted lower alkynyl group, aromatic heterocyclic group, substituted or unsubstituted aliphatic heterocyclic group or aryl group, provided that when Z is a single bond, R is a substituted or unsubstituted aromatic heterocyclic group, or a pharmaceutically acceptable salt thereof, and processes for preparing the same, these compounds having endothelin antagonistic activity and being useful in the prophylaxis or treatment of various diseases caused by endothelin.

Benzenesulfonamide derivative and process for preparing thereof

A benzenesulfonamide derivative of the formula [I]: ##STR1## wherein Ring A and Ring B are the same or different and each substituted or unsubstituted benzene ring, Q is a single bond or a group of the formula: --O--, --S--, --SO--, --SO.sub.2 -- or --CH2--, Y is a group of the formula: --O--, --S-- or --NH--, Alk is lower alkylene group or lower alkenylene group, Z is a single bond or a group of the formula: --O-- or --NH--, R is a substituted or unsubstituted aromatic heterocyclic or aryl group, R.sup.1 is hydrogen atom, trifluoromethyl group, substituted or unsubstituted lower alkyl group, substituted or unsubstituted lower alkenyl group, mono-- or di-lower alkylamino group, substituted or unsubstituted lower alkylthio group, substituted or unsubstituted lower alkoxy group, substituted or unsubstituted lower alkynyl group, aromatic heterocyclic group, substituted or unsubstituted aliphatic heterocyclic group or aryl group, provided that when Z is a single bond, R is a substituted or unsubstituted aromatic heterocyclic group, or a pharmaceutically acceptable salt thereof, and processes for preparing the same, these compounds having endothelin antagonistic activity and being useful in the prophylaxis or treatment of various diseases caused by endothelin.

Disclosed are .beta.-carboline derivatives represented by the formula: ##STR1## wherein R.sup.1 represents hydrogen atom, a lower alkyl group, a lower alkoxy group or hydroxy group; R.sup.5 represents hydrogen atom, or R.sup.1 and R.sup.5 are bonded to represent a lower alkylenedioxy group; R.sup.2 represents hydrogen atom, a halogen atom, a lower alkoxy group or hydroxy group; R.sup.3 represents hydrogen atom, a carbamoyl lower alkyl group, a lower alkyl group, a carboxy lower alkyl group or a lower alkoxycarbonyl lower alkyl group; R.sup.4 represents hydrogen atom, a lower alkyl group, a carboxy lower alkyl group, a lower alkoxycarbonyl lower alkyl group, a lower alkanoyl group, an arylcarbonyl group, a lower alkanesulfonyl group, a lower alkoxycarbonyl group, an aralkyl group, formyl group or a di(lower alkyl)sulfamoyl group; n represents 0, 1 or 2; and the symbol * represents an asymmetric carbon atom, or a pharmaceutically acceptable salt thereof, and a process for preparing the same.

.beta.-carboline derivative

A naphthyloxazolidone derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, hydroxy group, nitro group, amino group, sulfo group, aminosulfonyl group, a lower alkenyloxy group, a lower alkynyloxy group, a mono or di(lower alkyl)aminocarbonyloxy group, a lower alkanoyloxy group or a lower alkoxy group which may have a substituent selected from an aryl group, a cycloalkyl group, an oxygen-containing heteromonocyclic group, hydroxy group, a lower alkoxy group, cyano group, a di(lower alkyl)amino group, aminocarbonyl group, a lower alkoxycarbonyl group, a lower alkanoyloxy group, a lower alkylthio group, a lower alkylsulfinyl group and a lower alkylsulfonyl group; R.sup.2 is hydroxy group, a lower alkoxy group, a lower alkylsulfonyloxy group, triazo group or an amino group which may have a substituent selected from a lower alkyl group and a lower alkanoyl group, and a pharmaceutically acceptable salt thereof are disclosed. Said derivative and a pharmaceutically acceptable salt thereof are useful as an antidepressant.

Naphthyloxazolidone derivatives

A naphthyloxazolidone derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, hydroxy group, nitro group, amino group, sulfo group, aminosulfoyul group, a lower alkenyloxy group, a lower alkynyloxy group, a mono or di(lower alkyl)aminocarbonyloxy group, a lower alkanoyloxy group or a lower alkoxy group which may have a substituent selected from an aryl group, a cycloalkyl group, an oxygen-containing heteromonocyclic group, hydroxy group, a lower alkoxy group, cyano group, a di(lower alkyl)amino group, aminocarbonyl group, a lower alkoxycarbonyl group, a lower alkanoyloxy group, a lower alkylthio group, a lower alkylsulfinyl group and a lower alkylsulfonyl group; R.sup.2 is hydroxy group, a lower alkoxy group, a lower alkylsulfonyloxy group, triazo group or an amino group which may have a substituent selected from a lower alkyl group and a lower alkanoyl group, and a pharmaceuticaly acceptable salt thereof are disclosed. Said derivative and a pharmaceutically acceptable salt thereof are useful as an antidepressant.

There is disclosed a lactam derivative of the formula: ##STR1## wherein R.sup.1 is a substituted or unsubstituted phenyl group; R.sup.2 is a substituted or unsubstituted phenyl group, a cycloalkyl group or a nitrogen-containing 6-membered heterocyclic group; Z is oxygen atom or sulfur atom; and n is an integer of 2 or 3, and a salt thereof. The above lactam derivative is novel and useful as a pharmaceutical compound.

Growing community of inventors

Saitama-ken, Japan

Koichiro Yamada