Banyu Pharmaceutical Co. Ltd

Msd K.k.

Merck Sharp + Dohme Corp.

Sumitomo Osaka Cement Co., Ltd.

Taiho Pharmaceutical Company Limited

Sumitomo Cement Co., Ltd.

Taiho Pahrmaceutical Co., Ltd.

Toshihiro Sakamoto

Akio Kanatani

Takehiro Fukami

Yuji Haga

Toshiyuki Takahashi

Yasuyuki Ishii

Hidetomo Furuyama

Akane Ishihara

Takahiro Itoh

Fuyuki Yamamoto

Takashi Yoshizumi

Yasuhiro Goto

Keiji Takahashi

Makoto Bamba

Satoshi Sunami

Yoshio Ogino

Kenji Niiyama

Nobuhiko Kawanishi

Hirotoshi Nagata

Takeshi Sagara

Hiroshi Hirai

Takashi Mita

Sachie Otsuki

Mark E Layton

Philip E Sanderson

Jiabing Wang

Takashi Shinriki

Minoru Moriya

Akira Naya

Hideki Kazuno

Manabu Yamada

Norikazu Miyazaki

Junichiro Ichikawa

Makoto Ishikawa

Toru Sugamata

Masashi Kawasaki

Koji Ichikawa

Norikazu Otake

Tony Siu

Tetsuya Sugimoto

Toshihide Nishibata

Yu Onozaki

Yasuyuki Miyama

Tomohiro Yamamoto

Weiming Fan

Tetsuya Fujino

Michael Robert Peel

Kevin J Rodzinak

Michael A Rossi

Hidekazu Takahashi

Michael James Malaska

Bharathi Pandi

Masanao Kurihara

Hideya Komatani

Hitomi Kondo

Matthew G Jenks

Mikako Kawamura

Shunji Sakuraba

Hiroyuki Kishino

Takao Suzuki

Junichiro Minowa

Shinichi Shimotsu

Hao Liu

Kazuaki Shibata

Arlene E McKeown

Yu Kobayakawa

Hiroo Mizuno

Kazumasa Kiuchi

Masanobu Kobayashi

Hideki Honda

Jamshid Nayyer

Junichi Ogiwara

Naoki Egashira

Takumitsu Machida

Masato Chiba

Thomas F N Haxell

Shuliang Lee

Joseph A Moore, Iii

Kimimasa Suzuki

Joseph A Iii Moore

Hidetomo Fruyama

The present invention provides a phenol compound represented by the following Formula (I) or a salt thereof: wherein R, R, R, L, L, L, A, X, and m are as described in the specification.

Phenol compound or salt thereof

An indazole compound represented by the following Formula (I) or a salt thereof: wherein X, R, R, ring A, L, L, L, and Rare as defined in this specification.

Indazole compound or salt thereof

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 present invention provides a compound represented by the following general formula (I) or a salt thereof which has a Syk inhibitory effect (in the formula Rrepresents a hydrogen atom or an optionally substituted C-Calkyl group; A represents a hydrogen atom, an optionally substituted C-Calkyl group, an optionally substituted C-Calkenyl group, an optionally substituted C-Calkynyl group, an optionally substituted C-Ccycloalkyl group, an optionally substituted C-Caromatic hydrocarbon group, an optionally substituted 4- to 10-membered unsaturated heterocyclic group, or an optionally substituted 4- to 10-membered saturated heterocyclic group, or optionally forms a 4- to 10-membered unsaturated heterocyclic ring or a 4- to 10-membered saturated heterocyclic ring together with Rand the nitrogen atom bonded thereto; Rrepresents a hydrogen atom or an optionally substituted C-Calkyl group; and B represents an optionally substituted unsaturated heterocyclic group).

1,2,4-triazine-6-carboxamide 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 instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

Inhibitors of Akt activity

The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer.

Inhibitors of AKT activity

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

The compounds of Formula D are of the class of triazolo-pyrido-pyrazines which are inhibitors of AKT useful for the treatment of cancer 

Substituted [1,2,4]triazolo[4',3&#x2032;:1,6]pyrido[2,3-b]pyrazines of the formula D

The present invention relates to the crystalline forms of 2-allyl-1-[6-(I-hydroxy-1 methylethyl)pyridin-2-yl]-6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one or a salt thereof, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor. 

Crystalline forms of dihydropyrazolopyrimidinone

A compound represented by the formula (I) is contained as an active ingredient: wherein Rand Rindependently represent a hydrogen atom, a lower alkyl group or the like, or Rtogether with a nitrogen atom to which L, Zand Rare attached may form an aliphatic nitrogenated heterocyclic group and Rand Rtogether with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents &#x2014;CH&#x2014;O&#x2014;, &#x2014;CH&#x2550;CH&#x2014; or the like; Zrepresents a single bond, a Calkylene group or the like; Zrepresents a single bond or a Calkylene group; L represents a methylene group, a Ccycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.

Phenylpyridone derivative

Substituted pyrazolo[3,4-d]pyrimidinone derivatives

Growing community of inventors

Moriya, Japan

Toshihiro Sakamoto