Msd K.k.

Banyu Pharmaceutical Co. Ltd

Merck Sharp + Dohme Corp.

Taiho Pharmaceutical Company Limited

Taiho Pahrmaceutical Co., Ltd.

Fuyuki Yamamoto

Toshihiro Sakamoto

Hidetomo Furuyama

Satoshi Sunami

Takashi Yoshizumi

Keiji Takahashi

Makoto Bamba

Kenji Niiyama

Yasuhiro Goto

Takeshi Sagara

Hiroshi Hirai

Sachie Otsuki

Toshihide Nishibata

Tetsuya Sugimoto

Mikako Kawamura

Yu Kobayakawa

Masashi Kawasaki

Koji Ichikawa

Yoshikazu Iwasawa

Shinji Kato

Yoshio Ogino

Morihiro Mitsuya

Taketo Ikeno

Yaling Wang

Takashi Mizutani

Yoshiyuki Sato

Hideya Komatani

Takashi Hashihayata

Shoki Hara

Kaori Kamijo

Sachin Lohani

Hisaki Kojima

Takumitsu Machida

Hidefumi Kasuga

Hirokazu Fuchida

Shuntaro Furukawa

Wataru Minagawa

Naoki Egashira

Naotaka Sawada

Hidetomo Fruyama

The present invention provides a novel compound inhibiting EGFR or a salt of the compound. According to one embodiment of the present invention, provided is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.

Substituted pyrrolo[2,3-d]pyrimidines as EGFR inhibitors

The invention of the present application provides a compound represented by Formula (I) or a salt thereof, which exhibits an inhibitory activity against at least one kinase selected from the group consisting of Akt kinase, Rsk kinase, and S6K kinase and/or a cell proliferation inhibiting effect and is useful as a prophylactic and/or therapeutic agent for diseases associated with the above-mentioned kinases, particularly cancer. [In the formula, Rrepresents a 4- to 6-membered monocyclic unsaturated heterocyclic group which has 1 to 3 hetero atoms independently selected from N, S and O and may have a substituent; Rrepresents a hydrogen atom or the like; R, R, and R, may be the same as or different from one another and independently represent a hydrogen atom or the like; Rrepresents a hydrogen atom or the like; Rand R, may be the same as or different from each other and independently represent a hydrogen atom or the like; Xand Xmay be the same as or different from each other and independently represent N or CR; Rrepresents a hydrogen atom or the like; and Xrepresents N or CH when the broken line () represents a single bond, and represents C when a broken line indicates a double bond, wherein at least one of Xor Xrepresents N.] 

5H-pyrrolo[2,3-D]pyrimidin-6(7H)-one derivative

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 present invention relates to a process for producing a hydrate of 3-(2,6-dichlorophenyl)-4-imino-7-[(2'-methyl-2&#x2032;,3&#x2032;-dihydro-1&#x2032;H-spiro[cyclopropane-1,4&#x2032;-isoquinolin]-7&#x2032;-yl)amino]-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one (Compound A) or of a pharmaceutically acceptable salt of Compound A and a crystalline form of Compound A or of a pharmaceutically acceptable salt of Compound A, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor.

Process for producing bicycloaniline derivatives

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

Substituted pyrazolo[3,4-d]pyrimidinone derivatives

The present invention relates to a compound represented by Formula [I] or a pharmaceutically acceptable salt or ester thereof: wherein:

Substituted imidazole derivative

Growing community of inventors

Tsukuba, Japan

Fuyuki Yamamoto