Msd K.k.

Banyu Pharmaceutical Co. Ltd

Takashi Yoshizumi

Toshihiro Sakamoto

Hidetomo Furuyama

Fuyuki Yamamoto

Keiji Takahashi

Makoto Bamba

Satoshi Sunami

Kenji Niiyama

Yasuhiro Goto

Takeshi Sagara

Hiroshi Hirai

Sachie Otsuki

Toshihide Nishibata

Hirobumi Takahashi

Tetsuya Kato

Masanori Asai

Osamu Okamoto

Hiroshi Kawamoto

Mikako Kawamura

Kensuke Kobayashi

Satoru Itoh

Yuichi Sugimoto

Hiroshi Miyazoe

Hidetomo Fruyama

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 relates to a compound of General Formula (I) below, among others. In the Formula, Aris an optionally substituted aryl or heteroaryl group; Ris a hydrogen atom, an optionally substituted C1-C6 alkyl group, or an optionally substituted aryl, aralkyl, or heteroaryl group; Ris an optionally substituted aryl, aralkyl, or heteroaryl group; and Ris a hydrogen atom or a C1-C6 alkyl group. A compound of the present invention has an excellent Wee1 kinase inhibiting effect, and is therefore useful in the filed of medicine, particularly in various types of cancer therapy. 

Dihydropyrazolopyrimidinone derivative

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 relates to compounds of general formula (I-0): wherein R, R, R, R, R, R, R, R, X, and Y are as defined herein. Compounds of the invention have, based on excellent Wee1 kinase-inhibitory effect, a cell growth-inhibitory effect and an additive/synergistic effect with any other anticancer agent, and are therefore useful in the field of medicine.

Pyridone-substituted-dihydropyrazolopyrimidinone derivative

Provided are cycloalkanopyridine derivatives of formula [I]: [wherein the symbols are the same as those stated in the description]. The compounds act as a nociceptin receptor antagonist, and are useful as medicines for diseases associated with a nociceptin receptor, for example, as a reliever against tolerance to a narcotic analgesic; a reliever against dependence on or addiction to a narcotic analgesic; an analgesic enhancer; an antiobesitic or appetite suppressor; a treating or prophylactic agent for cognitive impairment and dementia/amnesia; an agent for treating developmental cognitive abnormality; a remedy for schizophrenia; an agent for treating neurodegenerative diseases; an anti-depressant or treating agent for affective disorder; a treating or prophylactic agent for diabetes insipidus; a treating or prophylactic agent for polyuria; or a remedy for hypotension.

Cycloalkanopyridine derivative

Substituted pyrazolo[3,4-d]pyrimidinone derivatives

This invention provides compounds which are represented by a general formula [I] [in which X stands for hydrogen or halogen; B stands for halogen, cyano or optionally fluorine-substituted lower alkyl; D stands for a 3&#x2013;10 membered aliphatic nitrogen-containing heterocyclic group; R, Rand Rmay be same or different, and each stands for hydrogen, lower alkyl optionally having substituent group(s) and the like; and a is 0 or 1]. These compounds exhibit high affinity to nociceptin receptors and whereby inhibit actions of nociceptin, and are useful as an analgesic, antiobestic, agent for ameliorating brain function, treating agents for Alzheimer's disease and dementia, and therapeutic agents for schizophrenia, neurodegenerative diseases, depression, diabetes insipidus, polyuria, hypotension and the like.

Benzimidazole derivatives

Growing community of inventors

Ushiku, Japan

Takashi Yoshizumi