Banyu Pharmaceutical Co. Ltd

Takashi Hayama

Kiyofumi Ishikawa

Mitsuo Yano

Toshio Nagase

Masaki Ihara

Toshiaki Mase

Takehiro Fukami

Masaru Nishikibe

Kenji Niiyama

Kagari Fujita

Fumihiko Ikemoto

Nobuhiko Kawanishi

Kyoko Hayashi

Teruki Honma

Ikuko Takahashi

Tooru Takaki

Norikazu Otake

Kenji Matsuyama

Kazuhito Noguchi

The present invention relates to a compound of Formula (I) and the manufacturing method(s) thereof and the use thereof: Formula (I) wherein: Ar is a nitrogen-containing heteroaromatic ring group; X and Z are each a carbon atom, and so on; Y is CO, and so on; Ris a hydrogen atom, and so on; Rand Rare each a hydrogen atom, and so on; Rand Rare each a hydrogen atom, and so on; and the formulais a single bond or a double bond. According to the present invention, the compound of the present invention can provide Cdk4 and/or Cdk6 inhibitors for treating malignant tumors, because the compounds of the present invention exhibit a prominent growth inhibitory activity against tumor cells.

Biarylurea derivatives

The present invention relates to a compound of the general formula (I): [Aris aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc., V is CH, etc., Wis &#x2014;(CH)&#x2014; (n is zero to four), R, is H or optionally substituted lower alkyl, etc., Ris H, etc., Rand Rare the same or different and are each H, etc., Rand Rare the same or different and are each H, hydroxy, etc.] or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition, an inhibitor of Cdk4 and/or Cdk6 or an anti-cancer agent, containing the same as an active ingredient; and a process for preparing them.

Pyrazinone derivatives

The present invention relates to a compound of Formula (I) and the manufacturing method(s) thereof and the use thereof:&#x2003;wherein: Ar is a nitrogen-containing heteroaromatic ring group; X and Z are each a carbon atom, and so on; Y is CO, and so on; Ris a hydrogen atom, and so on; Rand Rare each a hydrogen atom, and so on; Rand Rare each a hydrogen atom, and so on; and the formulais a single bond or a double bond.According to the present invention, the compound of the present invention can provide Cdk4 and/or Cdk6 inhibitors for treating malignant tumors, because the compounds of the present invention exhibit a prominent growth inhibitory activity against tumor cells.

The present invention relates to a compound of the general formula (I):[Aris aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc., V is CH, etc., Wis &#x2014;(CH)&#x2014; (n is zero to four), Ris H or optionally substituted lower alkyl, etc., Ris H, etc., Rand Rare the same or different and are each H, etc., Rand Rare the same or different and are each H, hydroxy, etc.] or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition, an inhibitor of Cdk4 and/or Cdk6 or an anti-cancer agent, containing the same as an active ingredient; and a process for preparing them.

The present invention relates to a cyclopentenopyridine derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, wherein Ar is a phenyl group or the like. R is a mono- or di-C -C alkylamino group or the like, and R is a hydroxyl group or the like, a process for its production and its use.

Substituted 5-(2,2-difluoro-1,3-benzodioxol-5-yl) cyclopentenopyridine derivative

Endothelin antagonistic heteroaromatic ring-fused cyclopentene

The invention relates to compounds which are antagonists of endothelin, to processes for their preparation, and to their use as pharmaceuticals. The compounds of the invention are Useful in the treatment of hypertension, pulmonary hypertension, Reynaud's disease, myocardial infarction, angina pectoris, acute renal failure, cerebral infarction, cerebral vasospasm, arteriosclerosis, asthma, endotoxin shock, endotoxin-induced multiple organ failure or disseminated intravascular coagulation, and/or cyclosporin-induced renal failure or hypertension.

Endothelin antagonistic peptide derivatives

This invention relates to novel 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols, a process for preparing the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols reioselectively and in a high yield utilizing the Bischler-Napieralski reaction, a process for synthesizing 6,7-dialkoxy-1,2,3,4-tetrahydroisoquinolin-8-ols via the compounds, and use of the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols for preparation of the 6,7-dialkoxy-1, 2,3,4-tetrahydroisoquinolin-8-ols. It is possible according to this invention, to obtain the 6,7 -dialkoxy-1,2,3,4-tetrahydroisoquinolin-8-ols, which have hitherto been difficult to synthesize, via the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols in a high yield.

6,7-dialkoxy-3,4-diydroisoquinolin-8-yl compounds

Peptides having the formula: ##STR1## inhibit the binding of endothelin and are useful in treating diseases associated with excess production or secretion of endothelin.

Endothelin antagonistic substance

Peptides having the formula: ##STR1## inhibit the binding of endothelin to its receptor and are useful in treating diseases associated with excess production or secretion of endothelin.

This invention relates to novel 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols, a process for preparing the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols reioselectively and in a high yield utilizing the Bischler-Napieralski reaction, a process for synthesizing 6,7-dialkoxy-1,2,3,4-tetrahydroisoquinolin-8-ols via the compounds, and use of the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols for preparation of the 6,7-dialkoxy-1,2,3,4-tetrahydroisoquinolin-8-ols. It is possible, according to this invention, to obtain the 6,7-dialkoxy-1,2,3,4-tetrahydroisoquinolin-8-ols, which have hitherto been difficult to synthesize, via the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols in a high yield.

Process for preparing 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ol

Peptides having the formula ##STR1## inhibit the binding of endothelin to its receptor and are useful in treating diseases associated with excess production or secretion of endothelin.

A heteroaromatic ring-fused cyclopentene derivative of the formula: ##STR1## wherein the variables are as defined in the specification; or a pharmaceutically acceptable salt thereof.

There are provided novel aminophosphonic acid derivatives of the general formula [I]: ##STR1## wherein n is an integer of 2 or 3; R.sup.1 is a phenyl, naphthyl, indolyl, benzothienyl, benzofuryl or benzoxazolyl group which may have 1 to 3 substituents selected from the group consisting of hydroxyl and lower alkyloxy groups, or a hydrogen atom; R.sup.2 is a lower alkyl group, a benzyl group, a 4-hydroxybenzyl group, a 3-indolylmethyl group or a .beta.-phenethyl group; and A is an optional residue of an amino acid selected from the group consisting of tryptophane, tyrosine, phenylalanine, homophenylalanine, naphthylalanine or N.sup..omega. -nitroarginine, and their pharmaceutically acceptable salts. The compounds according to the present invention and their pharmaceutically acceptable salts exhibit an inhibitory activity against endothelin-converting enzyme, and are expected to be useful as a drug treating various diseases with which endothelin is concerned.

Aminophosponic acid derivative

Novel isoquinoline derivatives represented by formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X.sup.1 and X.sup.2 are as defined in the specification, have an anti-arrhythmic activity and bradycardiac activity and are effective for the treatment of arrhythmia, myocardiac infarction or angina pectoris.

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Tsukuba, Japan

Takashi Hayama