Japan Tobacco Inc.

Japan Tabacco Inc.

Kimiya Maeda

Hisashi Shinkai

Hiroshi Okamoto

Hiroshi Nakamura

Daisuke Takahashi

Hironobu Nagamori

Toshio Taniguchi

Yasunori Suzuki

The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity. the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.

CETP activity inhibitors

A dibenzylamine compound represented by the formula (1) wherein Rand Rare each a Callyl group optionally substituted by halogen atoms and the like; R, Rand Rare each a hydrogen atom, a halogen atom and the like, or Rand Rmay form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is &#x2014;N(R)(R) and the like; ring B is an aryl group or a heterocyclic residue; Ris a hydrogen atom, a halogen atom, a nitro group, a Callyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.

Dibenzylamine compounds and pharmaceutical use thereof

The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X, X, X, and Xmay be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents &#x2014;CO&#x2014; or &#x2014;SO&#x2014;, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof. The compounds represented by the formula (I) can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity and, therefore, is expected to be useful as a new type of a preventive or therapeutic agent for atherosclerosis or hyperlipidemia.

A dibenzylamine compound represented by the formula (1) wherein Rand Rare each a Calkyl group optionally substituted by halogen atoms and the like; R, Rand Rare each a hydrogen atom, a halogen atom and the like, or Rand Rmay form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is&#x2014;N(R) (R) and the like; ring B is an aryl group or a heterocyclic residue; Ris a hydrogen atom, a halogen atom, a nitro group, a Calkyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.

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Takatsuki, Japan

Kimiya Maeda