Banyu Pharmaceutical Co. Ltd

Msd K.k.

Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Taiho Pharmaceutical Company Limited

Kenji Niiyama

Takehiro Fukami

Toshio Nagase

Masaki Ihara

Toshiaki Mase

Kiyofumi Ishikawa

Mitsuo Yano

Kagari Fujita

Keiji Takahashi

Takashi Hayama

Satoshi Sunami

Fumihiko Ikemoto

Yasuhiro Goto

Toshihiro Sakamoto

Hidetomo Furuyama

Makoto Bamba

Fuyuki Yamamoto

Takashi Yoshizumi

Lihu Yang

Jun Shibata

Mitsuru Ohkubo

Masaru Nishikibe

Tomoharu Iino

Takeshi Sagara

Takeru Yamakawa

Hiroshi Hirai

Hideki Jona

Sachie Otsuki

Toshihide Nishibata

Masayuki Nakamura

Masaaki Hosoi

Jun Kusunoki

Hideaki Imamura

Koji Yamada

Hiroshi Takeshita

Susumu Nakagawa

Kenji Matsuyama

Tadashi Shimamura

Fumio Nakano

Yusuke Hidaka

Hideki Kurihara

Yoshiaki Iida

Hitomi Watanabe

Toshiyasu Shimomura

Kaori Kamijo

Takeshi Hayama

Yoshio Hioki

Ryo Nishioka

The invention relates to compounds of a general formula (I): wherein Aris an optionally-substituted aryl or heteroaromatic group; Ris an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; Ris a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; Ris a hydrogen atom or a lower alkyl group; Ris a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of &#x2014;N(R)R; T and U are a nitrogen atom or a methine group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.

Dihydropyrazolopyrimidinone derivatives

The present invention provides an imidazooxazine compound represented by Formula (I) or a salt thereof, wherein A, B, C, and D are as defined in the specification.

Imidazo-oxazine compound or salt thereof

The invention relates to a compound of a general formula (I): wherein Aand Aeach mean a nitrogen atom or an optionally-substituted methine group; Ring B means a 5-membered to 7-membered aliphatic ring, or a spiro or bicyclo ring formed from the aliphatic ring and any other 3-membered to 7-membered aliphatic ring; Rmeans a hydrogen atom, or an optionally-substituted C1-C6 alkyl group, or an optionally-substituted aryl, aralkyl or heteroaryl group; Rmeans an optionally-substituted aryl, aralkyl or heteroaryl group; and X means a group of &#x2550;NH or &#x2550;O, etc. Based on its excellent Wee1 kinase-inhibitory effect, the compound of the invention has cell growth-inhibitory effect and has an additive/synergistic effect with any other anticancer agent, and is therefore useful in the field of medicine.

Bicycloaniline derivative

The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a): Rmeans a &#x2014;(C&#x2550;O)O(C1-C6)alkyl group, a &#x2014;(C&#x2550;O)O(C2-C6)alkenyl group, a &#x2014;(C&#x2550;O)O(C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; Rand Reach mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a &#x2014;(C&#x2550;O)O(C1-C6)alkyl group or a group of &#x2014;(C&#x2550;O)N(R)R; Rmeans a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments. 

Pyrimidopyrimidoindazole derivative

The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-a]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases. 

Spirochromanon derivatives

The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders. 

Spirochromanone derivatives as acetyl coenzyme A carboxylase (ACC) inhibitors

Substituted pyrazolo[3,4-d]pyrimidinone derivatives

The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.

Spirochromanone derivatives

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

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

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.

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.

Endothelin antagonistic cyclic pentapeptides

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Tsuchiura, Japan

Kenji Niiyama