Toa Eiyo Ltd.

Yamasa Shoyu Kabushiki Kaisha

Sagami Chemical Research Center

Sagami Chemical Research Center Toa Eiyo Ltd.

Kentaro Kogi

Shin-ichi Yamada

Toichi Abiru

Atsuo Takahashi

Toyofumi Yamaguchi

Masakatsu Shibasaki

Akira Matsuda

Tohru Ueda

Sen-ichi Narita

Takao Goto

Senichi Narita

Hiroyasu Sato

Tuyoshi Aoki

Takaji Yamaguchi

Shinji Sakata

Takanori Miyashita

Fumiya Yoneyama

Takahiro Yamaguchi

Eizi Shimanuki

Yukiko Oguchi

Takashi Yamaguchi

Jun Sasamori

Takeshi Nara

Yozo Nishimiya

Kazuyuki Aihara

Takahashi Atsuo

Tetsuo Kimura

Michiko Kudo

Yoichi Manome

Kaoru Genkyou

Eiji Shimanuki

Isamu Sato

Takashi Satoh

Toshihisa Mashiko

Rie Yorita

Tsuyoshi Aoki

Kaoru Gengyou

Sachiko Yoneyama

Sachiko Ishigami

Toyoki Nishimata

This invention relates to a cycloalka&lsqb;b&rsqb;pyridine-3-carbonylguanidine derivative represented by the following general formula (1):

Cycloalka&lsqb;b&rsqb;pyridine-3-carbonylguanidine derivatives, process for producing the same, and drugs containing the same

A substituted cyclic amine compound represented by the following general formula (1) ##STR1## wherein each of R.sup.1 to R.sup.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or the like, A represents a carbonyl group or a sulfonyl group, B represents a methine moiety or a nitrogen atom, D represents a methine moiety, a nitrogen atom or .dbd.N(.fwdarw.O)-- and n is an integer of 2 to 3; and synthetic methods thereof. The inventive compound is useful in preventing and treating circulatory organ-related diseases such as hypertension, ischemic heart disease, cerebrovascular disease, peripheral circulatory disease and the like.

Substituted cyclic amine compound, production process thereof and

The present invention relates to a novel compound represented by the following formula [I] which is useful as a synthetic intermediate of a 2-alkynyladenosine. The present invention also relates to a process for producing the compound and a process for producing a 2-alkynyladenosine [IV] by way of the compound. Further, the present invention relates to a 2-alkynyladenosine derivative represented by the following formula [V] having excellent storage stability and, to a method of storing the 2-alkynyladenosine in the form of that derivative. ##STR1## [I] A=a leaving group, [II] A=NH.sub.2, [V] A=NHR.sup.4, wherein R.sup.1 through R.sup.4 represent a hydrogen atom or a protective group, and n denotes an integer of 1 to 15, provided that R.sup.1 through R.sup.4 do not represent a hydrogen atom simultaneously.

Process for preparing synthetic intermediates of 2-alkynyladenosines and

Tri-O-acetyl-2-alkynyladenosines

Therapeutic 2-alkynyl adenosine agent for ischemic diseases of the heart

Provided are cycloheptenopyridine derivatives represented by the general formula ##STR1## [wherein R represents a hydrogen atom or lower alkyl group; R.sup.1 represents a hydrogen atom, halogen atom, lower cycloalkoxy group, amido group, substituted phenoxy group, substituted benzyloxy group, lower alkoxy group optionally containing halogen atoms(s), nitro group, hydroxyl group, lower alkenyloxy group, lower alkylthio group, or a group--NR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 may be the same or different and each represent a hydrogen atom or lower alkyl group, or R.sup.4 and R.sup.5 mutually combine together with the nitrogen atom adjacent thereto to form a 5- or 6-membered heterocyclic group); R.sup.2 represents a hydrogen atom, halogen atom, lower alkyl group optionally containing a halogen atom, lower alkoxy group optionally containing a halogen atom, hydroxyl group, acyl group, lower alkoxycarbonyl group, nitro group or amino group; R.sup.3 represents a hydrogen atom, a lower alkyl group, lower alkoxymethyl group, lower alkylcarbonyl group, lower alkoxycarbonyl group, carbamoyl group, lower alkylcarbamoyl group, lower alkylcarbonylmethyl group, lower alkoxycarbonyl group, lower acyloxymethyl group, lower alkylsulfonyl group, or physiologically acceptable protective group eliminatable in an acid medium or under a physiological condition; n represents 0 or 1; and A represents a methine carbon or nitrogen atom] or their salts. These derivatives and their salts are useful as antiulcer agents.

Cycloheptenopyridine derivatives, process for preparation thereof and

A cis-bicyclo[4.3.0]non-2-ene derivative of the formula: ##STR1## wherein R is a hydrogen atom, or a protecting group for a hydroxyl group, R.sup.1 is a hydrogen atom, A C.sub.1 -C.sub.12 straight or branched chain alkyl group, a substituted or unsubstituted phenyl group, a C.sub.6 -C.sub.12 aralkyl group containing a condensed aromatic ring or an aromatic hetero ring, or 1 equivalent of a cation, A is --CH.dbd.CH--CH.sub.2 --, or --CH.sub.2 --CH.sub.2 --O--, R.sup.2 is a C.sub.3 -C.sub.10 straight or branched chain alkyl group, a C.sub.1 -C.sub.3 alkyl group substituted by an aryloxy group which may be substituted, a C.sub.3 -C.sub.12 straight or branched chain alkenyl group, a C.sub.3 -C.sub.8 straight or branched chain alkynyl group, a C.sub.1 -C.sub.3 alkyl group substituted by a phenyl or phenoxy group which may be substituted, by a C.sub.1 -C.sub.6 alkoxy group or by a C.sub.5 -C.sub.8 cycloalkyl group, R.sup.3 is a hydrogen atom, a methyl group, or a vinyl group, and X is a halogen atom.

Cis-bicyclo[4,3.0]non-2-end derivatives

A 4,7-dihydroisothiazole[5,4-b]pyridine derivative represented by the general formula ##STR1## wherein R.sup.1 represents an alkyl group which may be substituted,

4,7-dihydroisothiazolo(5,4-b)pyridine derivatives and cardiovascular

A prostacyclin analogue having the formula: ##STR1## wherein R.sup.1 is --CO.sub.2 R.sup.5 (wherein R.sup.5 is a hydrogen atom, a straight chain or branched alkyl group having from 1 to 12 carbon atoms, an aralkyl group having from 7 to 12 carbon atoms, a cycloalkyl group having from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group having from 1 to 4 carbon atoms, a substituted or unsubstituted phenyl group, or one equivalent of a cation), or --CONR.sup.6 R.sup.7 (wherein each of R.sup.6 and R.sup.7 is a hydrogen atom or an alkyl group having from 1 to 10 carbon atoms, or R.sup.6 and R.sup.7 together with the adjacent nitrogen atom, form a 5- or 6-membered substituted or unsubstituted hetero ring which may contain a hetero atom other than said nitrogen atom); A is --CH.sub.2 CH.sub.2 CH.sub.2 --, CH.sub.2 --O--CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 --O--CH.sub.2 -- or --CH.dbd.CHCH.sub.2 CH.sub. 2 --; B is trans --CH.dbd.CH-- or --C.tbd.C--; R.sup.2 is a straight chain or branched alkyl group having from 3 to 10 carbon atoms, a cycloalkyl group having from 4 to 7 carbon atoms and unsubstituted or substituted by at least one alkyl group having from 1 to 4 carbon atoms, a straight chain or branched alkenyl group having from 3 to 12 carbon atoms, a straight chain or branched alkynyl group having from 3 to 8 carbon atoms, or an alkyl group having from 1 to 3 carbon atoms substituted by a substituted or unsubstituted phenyl or phenoxy group, by an alkoxy group having from 1 to 6 carbon atoms or by a cycloalkyl group having from 5 to 8 carbon atoms; R.sup.3 is a hydrogen atom, a methyl group or a vinyl group; and R.sup.4 is a hydrogen atom, an acyl group having from 1 to 7 carbon atoms, a tri-C.sub.1 -C.sub.7 hydrocarbon-silyl group or a group capable of forming an acetal bond together with the oxygen atom of a hydroxyl group; provided that the double bond in a substituent for A is E or Z, or a mixture thereof; the asymmetric center in a substituent for R.sup.2 assumes a R-conformation or a S-conformation, or a mixture thereof; and the bonds shown by dotted lines at the 2-3 and 3-4 positions mean that either one of them is a double bond.

Prostacyclin analogue, and blood circulation improving agent and

Growing community of inventors

Fukushima, Japan

Kentaro Kogi