Kyoto Pharmaceutical Industries, Ltd.

Sumitomo Dainippon Pharma Co., Ltd.

Kyoto Pharmaceuticals Industries, Ltd.

Masayasu Kasai

Hiroaki Shirahase

Hiroshi Matsui

Akihisa Yoshimi

Yoshimichi Shoji

Shigemitsu Takeda

Yoshinobu Yoshimura

Hideo Kobayashi

Satoru Azukizawa

Nobuharu Kakeya

Susumu Nishizawa

Hiroyuki Muro

Satoru Hatano

Kazuhiko Kitao

Ken-ichi Nishimura

Syouzi Kamiya

Shouji Kamiya

Miho Ikai

Kenji Takahash

Tadatsugu Tarumi

The problem of the present invention is to provide a useful prodrug compound of a naphthofuran compound. The present invention relates to a compound represented by the formula (IA): [wherein each symbol is as described in the DESCRIPTION] or a pharmaceutically acceptable salt thereof.

Anticancer agent

The novel heterocyclic compound of the present invention is a novel heterocyclic compound having the formula (I) Y: R&#x2014;C(R)&#x2550;N&#x2014;O&#x2014;wherein Ris H or Calkyl, Ris H, &#x2014;CO&#x2014;C(R)&#x2550;C(R)&#x2014;Rwherein Ris H or Calkyl, and Ris Calkyl, Calkenyl and the like, and the like, Y is the following group wherein X is O or S, Ris the same as R, Ris R&#x2014;C(R)&#x2550;C(R)&#x2014; wherein Ris the same as R, Ris Calkyl and the like, and the like, Ris the same as R, and Ris aryl and the like, Y&#x2014;(CH)n-O&#x2014; is bonded to the 6- or 7-position of the tetrahydroisoquinoline skeleton, and n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof. The compound (I) of the present invention is useful as a hypoglycemic agent, a hypolipidemic agent, an insulin resistance improver, a therapeutic agent of diabetes, a therapeutic agent of diabetic complications, a glucose tolerance improver, an anti-arteriosclerosis agent, an anti-obesity agent, an antiinflammatory agent, an agent for the prophylaxis or treatment of PPAR-mediated diseases or an agent for the prophylaxis or treatment of syndrome X.

Heterocyclic compound and medicinal use thereof

The present invention provides an indoline compound represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing this indoline compound or a pharmaceutically acceptable salt thereof. The compound of the present invention shows superior ACAT inhibitory effect and superior lipoperoxidation inhibitory effect and is useful as an ACAT inhibitor or a lipoperoxidation inhibitor.

Indoline compound and medicinal use thereof

The novel heterocyclic derivative of the present invention is a novel heterocyclic derivative having the formula (I')wherein Ris a hydrogen atom or Calkyl, Ris &#x2014;CO&#x2014;C(R)&#x2550;C(R)&#x2014;Rwherein Ris a hydrogen atom or Calkyl, and Ris Calkyl, Calkenyl, aryl or aromatic heterocycle, &#x2014;CO&#x2014;C&#x2261;C&#x2014;Rwherein Ris Calkyl and the like, Ris a hydrogen atom or Calkyl, X is an oxygen atom or a sulfur atom, Ris optionally substituted phenyl, and n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof. The compound (I&#x2032;) of the present invention is useful as a hypoglycemic agent, a hypolipidemic agent, an insulin resistance improver, a therapeutic agent of diabetes, a therapeutic agent of diabetic complications, a glucose tolerance improver, an anti-arteriosclerosis agent, an anti-obesity agent, an antiinflammatory agent, an agent for the prophylaxis or treatment of PPAR-mediated diseases and an agent for the prophylaxis or treatment of syndrome X.

Heterocyclic derivatives and medicinal use thereof

Heterocyclic compounds and salts thereof and medicinal use of the same

Carbapenem compounds, use thereof, and intermediate compounds of the same

Cephalosporin compounds

Cephalosporin compounds represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.5 independently represent a hydrogen atom or a protective group for an amino group; R.sup.2 represents an alkyl group or a cycloalkyl group; R.sup.3 represents a hydrogen atom, a lower alkenyl group, an alkanoyloxymethyl group, a carbamoyloxymethyl group, a heterocyclic thiomethyl group or a heterocyclic methyl group; R.sup.4 represents a hydrogen atom or an ester residue; and X represents CH or a nitrogen atom and pharmacologically acceptable addition salts thereof, intermediate compounds used in the synthesis process of these compounds, production methods of these compounds and pharmaceutical compositions containing these compounds. Said compounds or addition salts thereof exhibit noticeable antibacterial activities even on Pseudomonas aeruginosa, on which known cephalosporin compounds do not exhibit antibacterial activities, and moreover, work well against ordinary Gram-positive bacteria and Gram-negative bacteria.

Cephalosporin compound and pharmaceutical composition thereof

Growing community of inventors

Kyoto, Japan

Masayasu Kasai