Daiichi Sankyo Company, Limited

Daiichi Pharmaceutical Co., Ltd.

Other

Pharmacopeia Drug Discovery, Inc.

Nobuo Machinaga

Jun Chiba

Atsushi Nakayama

Yoshiyuki Yoneda

Shin Iimura

John J Baldwin

Edward McDonald

Christopher Ronald Sarko

Kevin Joseph Moriarty

Fumihito Muro

Jun Watanabe

Toshiyuki Watanabe

Ryuji Hashimoto

Mamoru Otoyo

Masaki Setoguchi

Yuichi Sugimoto

Hideko Hoh

Hiroshi Yuita

Ryotaku Inoue

Iimura Shin

To provide a novel compound that has S1P lyase inhibitory ability and induces a reduction in the number of lymphocytes, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the compound or pharmaceutically acceptable salt thereof as an active ingredient. A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof.

Phosphoric acid ester derivatives

To provide a novel compound or an isotope thereof or a pharmaceutically acceptable salt thereof having S1P lyase inhibitory capacity and inducing the decrease in number of lymphocytes, and a pharmaceutical composition containing these as active ingredients. A compound represented by the general formula (I): or the general formula (II): or an isotope thereof or a pharmaceutically acceptable salt thereof.

Imidazole derivative

There is provided a VLA-4 inhibitory drug having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally. A compound represented by the following formula (I): wherein Rrepresents a hydrogen atom or a C1-8 alkyl group; Rrepresents a hydrogen atom, a halogen atom, a C1-8 alkoxy group, or a benzyloxy group which may be substituted; Q represents a monocyclic or bicyclic nitrogen-containing heterocyclic group which may be substituted, and has a nitrogen atom as the bonding site; Y represents an oxygen atom or CH; W represents a bicyclic aromatic hydrocarbon ring group which may be substituted, or a bicyclic aromatic heterocyclic group which may be substituted; R, Rand Reach independently represent a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; and Arepresents a nitrogen atom or C&#x2014;R(wherein Rrepresents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group),

VLA-4 inhibitory drug

This invention provides an industrially useful process for producing 1,4-transcyclohexanecarboxylic acid derivative (1) which has excellent VLA-4 inhibitory action and safety, and an intermediate which is useful in such method. More particularly, this invention relates to a process for converting a compound of formula (I) into a compound of formula (VI) by the reaction scheme: 

Process for producing pyrrolidine derivative

Compounds that selectively inhibit the binding of ligands to &#x3b1;4&#x3b2;1 integrin (VLA-4) and methods for their preparation are disclosed. In one embodiment, compounds of the invention are represented by Formula I: As selective inhibitors of VLA-4 mediated cell adhesion, compounds of the present invention are useful in the treatment of conditions associated with such adhesion, including, but not limited to, such conditions as inflammatory and autoimmune responses, diabetes, asthma, psoriasis, inflammatory bowel disease, transplantation rejection, and tumor metastasis. Also disclosed are methods of inhibiting VLA-4 mediated cell adhesion and methods of treating conditions associated with LA-4 mediated cell adhesion.

VLA-4 inhibitor compounds

The present invention relates to a compound represented by the following formula (I): (wherein, W represents W-A-W- (in which, Wis substituted or unsubstituted aryl, etc., Ais &#x2014;NR&#x2014;, single bond, &#x2014;C(O)&#x2014;, etc., and Wis substituted or unsubstituted arylene, etc.), R is single bond, &#x2014;NH&#x2014;, &#x2014;OCH&#x2014;, alkenylene, etc., X is &#x2014;C(O)&#x2014;, &#x2014;CH&#x2014;, etc., and M is, for example, the following formula: (in which, R, Rand Reach independently represents hydrogen, hydroxyl, amino, halogen, etc., Ris hydrogen or lower alkyl, Y represents &#x2014;CH&#x2014;O&#x2014;, etc., Z is substituted or unsubstituted arylene, etc., Ais single bond, etc, and Ris hydroxyl or lower alkoxy)), or salt thereof; and a medicament containing the same. This compound or salt thereof selectively inhibits binding of cell adhesion molecules to VLA-4 and exhibits high bioavailability so that it is useful as a preventive and/or remedy for inflammatory diseases, autoimmune diseases, metastasis, bronchial asthma, rhinostenosis, diabetes, and the like.

Vla-4 inhibitors

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Tokyo, Japan

Nobuo Machinaga