Mochida Pharmaceutical Co., Ltd.

Merck Sharp + Dohme Corp.

Fumihiko Saitoh

Hiroshi Nagasue

Hidemitsu Nishida

William J Greenlee

Samuel Chackalamannil

Michael P Dwyer

Tsutomu Satoh

Yan Xia

Tin-Yau Chan

Mariappan Chelliah

Martin C Clasby

Tomokazu Hirabayashi

Yuji Kawada

Takafumi Mukaihira

Kousuke Harada

Ikuya Shiromizu

Santhosh Francis Neelamkavil

Unmesh G Shah

Akihiro Okano

Muneyoshi Makabe

Kouki Ogawa

Tomoyuki Kamino

Motoi Nakahara

Mariappan V Chelliah

Provided are type I, III, V and VI crystals of 1-((1R,2R)-2-hydroxy-4,4-dimethyl-1,2,3,4-tetrahydronaphthalen-1-yl)-3-(5-methyl-6-(2-methylpyrimidin-5-yl)-2-phenylpyridin-3-yl)urea which are useful as bulk pharmaceutical crystals. Also provided are type I, III, V and VI crystals of 1-((1R,2R)-2-hydroxy-4,4-dimethyl-1,2,3,4-tetrahydronaphthalen-1-yl)-3-(5-methyl-6-(2-methylpyrimidin-5-yl)-2-phenylpyridin-3-yl)urea having excellent TrkA inhibitory effect, medicines and medicinal composition containing these crystals, and a method for producing these crystals.

Crystals of tetrahydronaphthyl urea derivative

The present invention aims to provide a compound having a TrkA inhibitory action, a pharmaceutically acceptable salt thereof, or a solvate thereof, a pharmaceutical composition containing the same as an active ingredient, and a preventive and/or therapeutic agent for medicinal use, in particular for a disease in which TrkA in involved (pain, cancers, inflammation/inflammatory diseases, allergic diseases, skin diseases, neurodegenerative diseases, infectious diseases, Sjogren's syndrome, endometriosis, renal diseases, osteoporosis, and the like). Specifically, the present invention provides a compound or an optical isomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, or the like, the compound 

Tetrahydronaphthyl urea derivative

The present invention aims to provide a compound having a TrkA inhibitory action, a pharmaceutically acceptable salt thereof, or a solvate thereof, a pharmaceutical composition containing the same as an active ingredient, and a preventive and/or therapeutic agent for medicinal use, in particular for a disease in which TrkA in involved (pain, cancers, inflammation/inflammatory diseases, allergic diseases, skin diseases, neurodegenerative diseases, infectious diseases, Sjogren's syndrome, endometriosis, renal diseases, osteoporosis, and the like). Specifically, the present invention provides a compound or an optical isomer thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, or the like, the compound represented by formula (I): 

The present invention provides a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof or a solvate of these. A compound having Nrf2 activation ability is provided by the present invention. 

Indazolyl-oxo-isothiazole compounds

It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates. 

Pyrazole derivative

The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.

Morpholinone compounds as factor IXA inhibitors

Morpholinone compounds as factor IXa inhibitors

This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action.  The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.

Tricyclic compound having spiro union

This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which exhibits strong anticoagulation action. The invention also relates to a pharmacophore which was derived from the compound and is useful in molecular designing of the FXa inhibitor.

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Tokyo, Japan

Fumihiko Saitoh