Asahi Kasei Pharma Corporation

Raqualia Pharma Inc.

Koki Matsubara

Hitoshi Kida

Yoshimasa Arano

Kazuki Toyoshima

Toshihiko Sone

Shunsuke Kaneko

Kazuo Ando

Hirohide Noguchi

Minoru Seto

Rintaro Yamada

Yoshihito Kanzawa

Atsushi Iesato

Akifumi Oomura

Koh Kawasaki

The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.

Tetrahydroquinoline derivatives as P2X7 receptor antagonists

(S)-1-(4-Chloro-5-isoquinolinesulfonyl)-3-(methylamino)pyrrolidine monohydrochloride and a crystal thereof, and a crystal of the aforementioned monohydrochloride having a major peak or peaks at one or more positions selected from the group consisting of positions where 2&#x3b8;s are about 13.9&#xb0;, 21.5&#xb0;, 21.7&#xb0;, 22.4&#xb0;, 22.8&#xb0;, 24.5&#xb0; and 35.0&#xb0; in a powder X-ray diffraction spectrum, which have excellent properties as active ingredient of a medicament for prophylactic and/or therapeutic treatment of glaucoma and the like.

Sulfonamide compound and crystal thereof

A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; Grepresents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; Grepresents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; Grepresents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkoxycarbonyl group, an acyl group, an acyloxy group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; Y represents a single bond, or &#x2014;C(R)(R)&#x2014; (Rand Rrepresent hydrogen atom, or an alkyl group, or alkylene groups which combine together to form a saturated hydrocarbon ring group); Grepresents hydroxyl group (Y is a single group), or &#x2014;N(R)(R) (Rand Rrepresent hydrogen atom, an alkyl group, an aralkyl group, an alkenyl group, an alkynyl group, a saturated heterocyclic group, an alkylsulfonyl group, an acyl group, or an amidino group); Gis a substituent on a ring-constituting carbon atom of A, and represents hydrogen atom, fluorine atom, or an alkyl group] or a salt thereof, or a derivative thereof that is a prodrug, which potently inhibits Rho kinase. 

Sulfonamide compound

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Tokyo, Japan

Koki Matsubara