Taiho Pharmaceutical Company Limited

Msd K.k.

Merck Sharp + Dohme Corp.

Otsuka Pharmaceutical Company, Limited

Banyu Pharmaceutical Co. Ltd

Tadashi Shimamura

Hiroyuki Takahashi

Hidenori Fujita

Isao Miyazaki

Masanori Kato

Jun Shibata

Satoru Iguchi

Takao Uno

Lihu Yang

Steven Howard

Katsumasa Nonoshita

Tomoharu Iino

Takeru Yamakawa

Takashi Mita

Hideki Kurihara

Hideki Jona

John Walter Liebeschuetz

Christopher Norbert Johnson

Yoshikazu Iwasawa

Takahiro Ogawa

Kenji Niiyama

Teruyuki Nishimura

James Edward Harvey Day

Nobuhiko Kawanishi

Ryo Kato

Takeshi Sagara

Hiroshi Hirai

Jeffrey David St Denis

Sachie Arai

Masayuki Nakamura

Hiromi Oshiumi

Hitomi Watanabe

Keisuke Arakawa

Mikako Kawamura

Takashi Hashihayata

Yuichi Sugimoto

Risako Miura

Yufu Sagara

James Edward Day

The invention provides new pyrazine derivatives of formula (I): or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein. The invention also provides pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Pyrazolo[3,4-b]pyrazine SHP2 phosphatase inhibitors

An object of the invention is to provide a crystal of (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide which is excellent in stability and preferable from the viewpoint of manufacturing and formulation. The present invention provides a crystal having an X-ray powder diffraction spectrum having characteristic peaks at diffraction angles (2θ±0.2°) of 6.0°, 7.7°, 8.9°, 10.6°, 12.1°, 13.1°, 14.0°, 14.7°, 15.5°, 15.8°, 16.8°, 17.7°, 18.1°, 18.4°, 19.4°, 23.4°, 24.1°, 24.7°, 25.1° and 25.7°.

Crystal of pyrazolo[3,4-d]pyrimidine

The invention provides a compound of formula (I):

Heterobicyclic compounds for inhibiting the activity of SHP2

The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malignant tumors) that can be prevented or treated by RET inhibitory activity. The RET inhibitor comprises, as an active ingredient, a compound represented by Formula (I) below or a salts thereof: wherein A, Rto R, X, and n are as defined in the specification.

Fused pyrimidine compound or salt thereof

The problem to be solved by the present invention is to provide a novel compound having RET inhibitory activity. The present invention also provides a pharmaceutical preparation that is useful for the prevention and/or treatment of RET-related diseases, particularly cancer, based on RET inhibitory activity. The present invention provides a compound represented by Formula (I): wherein A, R, and X are as defined in the specification; or a salt thereof.

The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malignant tumors) that can be prevented or treated by RET inhibitory activity. The RET inhibitor comprises, as an active ingredient, a compound represented by Formula (I) below or a salts thereof:  wherein A, Rto R, X, and n are as defined in the specification.

A method for producing a pyrrolopyrimidine ring-containing tricyclic compound represented by Formula (1) or a salt thereof. The method comprising the steps of: (I) reacting an organoborane reagent with a compound represented by Formula (2) or a salt thereof, and (II) performing an intramolecular cyclization reaction of the reaction product of step (I) in the presence of a zerovalent palladium catalyst and an alkali metal hydroxide.

Method for producing a substituted 6,7,8,9-tetrahydropyrimido[5,4-b]indolizine, substituted 7,8,9,10-tetrahydro-6H-pyrimido[5',4&#x2032;:4,5]pyrrolo[1,2-a]azepine and substituted 6,7,8,9,10,11-hexahydropyrimido[5&#x2032;,4&#x2032;:4,5]pyrrolo[1,2-a]azocine

An object to be achieved by the present invention is to provide a novel compound having EGFR inhibitory effects and cell growth inhibitory effects, as well as a medication useful for the prevention and/or treatment of cancer based on the EGFR inhibitory effects. The present invention provides a compound represented by Formula (I) below, or a salt thereof. 

Quinoline-substituted compound

The present invention relates to a compound represented by formula (I): (wherein R, R, Rand Reach independently represent a hydrogen or halogen atom; Rand Reach independently represent a hydrogen atom or lower alkyl or together represent oxo; X represents C(O) or the like; Y represents an oxygen atom or the like; Z represents a hydrogen atom or the like; R represents 5- or 6-membered heteroaryl having 1-3 hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms, contained within a ring, or the like) or to a pharmaceutically acceptable salt thereof. 

Isoindolin-1-one 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

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Tsukuba, Japan

Tadashi Shimamura