Kyoto Pharmaceutical Industries, Ltd.

Sankyo Company, Limited

Hiroaki Shirahase

Hiroshi Matsui

Shohei Nakamura

Akihisa Yoshimi

Shoji Kamiya

Katsuo Wada

Masayasu Kasai

Hideo Kobayashi

Satoru Azukizawa

Yoshimichi Shoji

Shigemitsu Takeda

Fumio Fukata

Mamoru Kanda

Hideki Okunishi

Tatsuya Kitao

Yuta Kobayashi

Shouji Kamiya

Miho Ikai

Kenji Takahashi

Kenji Takahash

Tadatsugu Tarumi

The present invention aims to provide a novel cyclin-dependent kinase 8 and/or 19 inhibitor useful as an anti-cancer agent. The present invention relates to a cyclin-dependent kinase 8 and/or 19 inhibitor containing a compound represented by the formula (I): [wherein each symbol is as defined in the DESCRIPTION] or a pharmaceutically acceptable salt thereof as an active ingredient, and use thereof as an agent for preventing and/or treating cancer.

Cyclin-dependent kinase 8 and/or 19 inhibitor

Provided is a compound showing a bone formation promoting action (and/or bone resorption suppressive action). A compound of the formula (I) or a pharmacologically acceptable salt: [wherein each substituent is as defined in the DESCRIPTION], has low toxicity, shows good pharmacokinetics, has an action to promote bone formation, and is useful for the prophylaxis or treatment of metabolic bone diseases (osteoporosis, fibrous osteitis (hyperparathyroidism), osteomalacia, Paget's disease that influences the systemic bone metabolism parameter etc.) associated with a decrease in the bone formation ability as compared to the bone resorption capacity.

Aromatic compound and use thereof

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

A heterocyclic derivative of the formula (I)wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof exhibit superior ACAT inhibitory activity and lipoperoxidation inhibitory activity in mammals, and are useful as ACAT inhibitors and lipoperoxidation inhibitors. Specifically, they are useful for the prophylaxis and treatment of arteriosclerosis, hyperlipemia, arteriosclerosis in diabetes, and cerebrovascular and cardiovascular ischemic diseases.

Indolyl or indolinyl derivatives and medicinal use thereof as ACAT or lipid peroxidation inhibitors

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

Heterocyclic derivatives, method of production thereof and pharmaceutical use thereof

The cromoglycic acid compound of the formula (I)

Medicinal use of cromoglycic acid compounds

A heterocyclic derivative of the formula (I)

Heterocyclic derivatives and pharmaceutical use thereof

A therapeutic agent for allergic dermatitis caused by type IV allergic reaction, which contains diethyl L-lysylcromoglycate of the formula:

Therapeutic agent for allergic dermatitis

Antirheumatic agent

Heterocyclic derivatives of the formula (I) ##STR1## wherein each symbol is as defined in the specification, pharmaceutically acceptable salts thereof and method of producing them. Pharmaceutical compositions containing the heterocyclic derivative or a pharmaceutically acceptable salt thereof, particularly, ACAT inhibitors and lipoperoxidation inhibitors. The heterocyclic derivatives and pharmaceutically acceptable salts thereof of the present invention show superior ACAT inhibitory activity and lipoperoxidation inhibitory activity, and are useful as ACAT inhibitors and hyperlipemia inhibitors. To be specific, they are useful for the prevention and treatment of arteriosclerotic lesions of arteriosclerosis, hyperlipemia and diabetes, as well as ischemic diseases of brain, heart and the like.

Growing community of inventors

Kyoto, Japan

Hiroaki Shirahase