Japan Tobacco Inc.

Amgen Inc.

Japan Tabacco Inc.

Other

Hisashi Shinkai

Kimiya Maeda

Hiroshi Kawakami

Hiroshi Okamoto

Yuji Matsuzaki

Motohide Satoh

Hisateru Aramaki

Hiroshi Nakamura

Hironobu Nagamori

Takahisa Motomura

Shuichi Wamaki

Lawrence R McGee

Steven Marc Rubenstein

Wataru Watanabe

Atsushi Hagiwara

Noboru Furukawa

Jonathan B Houze

Daisuke Takahashi

Masafumi Inoue

Koichi Suzawa

Toshio Taniguchi

Takao Ito

Hirotsugu Ito

Kazunobu Yamataka

Satoru Kobayashi

Hideki Yamada

Yoshiharu Itoh

Toru Morita

Yasunori Suzuki

Takashi Matsuda

Mitsuru Takahashi

Satoshi Okuda

Masaki Yamashita

Shinichi Kiyonari

Akemi Nagao

Satoshi Ohrui

Tsutomu Shibata

Naohito Yamada

Lawrence R Mcgee

Steven M Rubenstein

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

The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.

Fluorene compound and pharmaceutical use thereof

An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.

4-oxoquinoline compound and use thereof as HIV integrase inhibitor

Compounds, compositions and methods are provided that are useful in the treatment or prevention of a condition or disorder mediated by PPAR&#x3b3;. In particular, the compounds of the invention modulate the function of PPAR&#x3b3;. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis.

Quinolinyl and benzothiazolyl modulators

The present invention relates to a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical composition, an anti-HIV agent and an HIV integrase inhibitor containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an anti-HIV agent, or as an agent for the prophylaxis or treatment of AIDS. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.

6-(heterocyclyl-substituted benzyl)-4-oxoquinoline compound and use thereof as HIV integrase inhibitor

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

A pharmaceutical agent having an anti-HIV action, particularly, a pharmaceutical agent having an integrase inhibitory action, is provided. The present invention relates to a quinolizinone compound represented by the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing same as an active ingredient. The compound of the present invention has an HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compounds can become a more effective anti-HIV agent. Since the compound has a high inhibitory activity specific for integrases, the compound can provide a safe pharmaceutical agent for human with a fewer side effects.

Quinolizinone compound and use thereof as HIV integrase inhibitor

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.

Provision of a compound having an anti-HIV activity, particularly an integrase inhibitory activity. A 4-oxoquinoline compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof: wherein each symbol is as defined in the specification. The present invention also relates to a pharmaceutical composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier; an integrase inhibitor, an antiviral agent, anti-HIV agent, and the like, which contains the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient; an anti-HIV composition containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof, and one or more other kinds of anti-HIV activity substances as active ingredients; an anti-HIV agent containing the 4-oxoquinoline compound or a pharmaceutically acceptable salt thereof as an active ingredient, which is used for a multiple drug therapy with other anti-HIV agent(s), and the like.

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.

Dibenzylamine compound and medicinal use thereof

4-oxoquinoline compound and use thereof as pharmaceutical agent

The present invention relates to a compound of the formula [1']&#x2003;wherein Ris lower alkyl optionally substituted by hydroxy, amino and the like, ring B is phenyl, thienyl and the like, E is a single bond, &#x2014;O&#x2014;, &#x2014;S&#x2014; and the like, ring G is aryl, heterocyclic group and the like, Ris halogen atom, hydroxy, lower alkyl optionally substituted by halogen atom etc., and the like, t is 0 or an integer of 1 to 5, when t is an integer of 2 to 5, each Rmay be the same or different, m is 0 or an integer of 1 to 8, and n is 0 or an integer of 1 to 4, and a nociceptin antagonist containing compound [1&#x2032;] as an active ingredient. The compound [1&#x2032;] shows, due to nociceptin antagonistic action, analgesic effect against sharp pain such as postoperative pain and the like. The present invention also relates to the use of certain amide derivative inclusive of compound [1&#x2032;] as a nociceptin antagonist or analgesic.

Amide derivatives and nociceptin antagonists

Growing community of inventors

Takatsuki, Japan

Hisashi Shinkai