Kowa Company Limited

Hiroyuki Ishiwata

Mototsugu Kabeya

Seiichi Sato

Soichi Oda

Manabu Shibasaki

Makoto Suda

Masami Shiratsuchi

Hiroshi Nakao

Takao Nagoya

Yukio Hattori

Takeshi Doi

Toru Kanke

Masanori Ashikawa

Takahiro Kitamura

Junya Tagashira

Toshiharu Morimoto

Tatsuaki Nishiyama

Hajime Yamada

Hiromichi Shigyo

Takeo Deushi

Shunji Takemura

Yoshio Takahashi

Yoshiharu Miyake

Gen Watanabe

Yukihiro Okuno

Akiyasu Koketsu

Masaki Yamabi

Satoshi Goda

Syunji Takemura

Masahiro Tamura

Tetsuya Ishikawa

Takashi Nakagawa

Toshiaki Takizawa

Toshiaki Oda

Yukiyoshi Yamazaki

Yasushi Wada

Ayumu Okuda

Yasumi Uchida

Shinsuke Itoh

Masahito Nakayama

Tomio Ohta

Hiroshi Ishihama

Kyoko Yasuoka

Noboru Shimizu

Junichi Kawagoe

Takahisa Ogamino

Hisakatsu Itoh

Yuichiro Tabunoki

Takatoshi Ozawa

Shin Tanikawa

Ryota Shigemi

Katsuhiro Yamamoto

Tomoaki Fukuda

Okihisa Tokuda

Akiyasu Kouketsu

Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin. Specifically disclosed is and EPO production enhancer and/or a hemoglobin production enhancer comprising a 1-acyl-4-(substituted oxy, substituted amino, or substituted thio)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by general formula (1) [wherein R, R, R, Rand Rindependently represent a hydrogen atom, a Calkyl group, or the like; R, R, R, R, R, Rand Rindependently represent a hydrogen atom, a halogen atom, a Calkyl group, or the like; A represents N&#x2014;R, a sulfur atom, or an oxygen atom; Rrepresents a hydrogen atom, a Calkyl group, or the like; B represents a Caryl group, or a 5- to 10-membered heterocyclic group; and n represents an integer of 0 or 1], a salt of the tetrahydroquinoline compound, or a solvate of the tetrahydroquinoline compound or the salt.

Prophylactic and/or therapeutic agent for anemia comprising tetrahydroquinoline compound as active ingredient

The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic &#x3b2;-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group;Rand R, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo Calkyl group, a Caryl group, a cyano group, a Calkyl group optionally having a substituent, a Calkenyl group optionally having a substituent, etc.; Rrepresents a hydrogen atom, a Calkyl group optionally having a substituent, etc.; and Rrepresents a hydrogen atom, a halogen atom, a Calkyl group optionally having a substituent, etc.]

Spiroindoline compound, and medicinal agent comprising same

Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin. Specifically disclosed is and EPO production enhancer and/or a hemoglobin production enhancer comprising a 1-acyl-4-(substituted oxy, substituted amino, or substituted thio)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by general formula (1) [wherein R, R, R, Rand R' independently represent a hydrogen atom, a Calkyl group, or the like; R, R, R, R, R, Rand Rindependently represent a hydrogen atom, a halogen atom, a Calkyl group, or the like; A represents N&#x2014;R, a sulfur atom, or an oxygen atom; Rrepresents a hydrogen atom, a Calkyl group, or the like; B represents a Caryl group, or a 5- to 10-membered heterocyclic group; and n represents an integer of 0 or 1], a salt of the tetrahydroquinoline compound, or a solvate of the tetrahydroquinoline compound or the salt.

The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a Caryl group or 5- to 10-membered heterocyclic group, X represents N&#x2014;R, a sulfur atom or an oxygen atom, R, R, R, Rand Rindependently represent a hydrogen atom, Calkyl group or Ccycloalkyl group, and R, Rand Rindependently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.

Fused piperidine compound and pharmaceutical containing same

To provide a novel JAK3 inhibitor that is useful as a preventive and/or therapeutic agent for rejection and graft versus host disease (GvHD) in organ transplantation, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, Sj&#xf6;gren syndrome, Behcet's disease, type I diabetes mellitus, autoimmune thyroiditis, idiopathic thrombocytopenic purpura, ulcerative colitis, Crohn's disease, asthma, allergic rhinitis, atopic dermatitis, contact dermatitis, urticaria, eczema, psoriasis, allergic conjunctivitis, uveitis, cancer, leukemia and the like. The pyridine-3-carboxyamide derivative represented by the general formula (1): or its salt or a solvate thereof.

Pyridine-3-carboxyamide derivative

Compounds represented by the general formula (1) or salts thereof or solvates of both; PAR-2 antagonists containing the compounds; and preventive or therapeutic agents for PAR-2 related diseases containing the antagonists as the active ingredient: (1) wherein Ris hydrogen, halogeno, or a group represented by the general formula (2): (wherein Ris straight-chain or branched Calkylene or the like; and Rand Rtogether with the nitrogen atom adjacent to them form a 5- to 7-membered ring); Ris straight-chain or branched Calkyl or the like; Rand Rare each independently hydrogen, one to three halogen atoms, or the like; and A-A-Ais a tripeptide residue composed of &#x3b1;-amino acids each independently selected from the group consisting of glycine, alanine, cyclohexylalanine, and so on.

PAR-2 antagonists

The present invention relates to a pharmaceutical composition for preventing/treating conditions associated with PAR-2. The present invention also relates to a method for preventing/treating the condition using the pharmaceutical composition and use for manufacturing the pharmaceutical composition. The pharmaceutical composition comprises a compound represented by the following general formula (1), salt or solvate thereof and a pharmaceutically acceptable carrier: Ar&#x2014;CO&#x2014;AA&#x2014;AA&#x2014;AA&#x2014;AA&#x2014;NH&#x2014;X&#x2014;Y (1) wherein, Ar represents a phenyl group or an aromatic heterocyclic group optionally having substituent(s): AArepresents a hydrophobic amino acid: AArepresents an amino acid absent of substituent(s) having more than two carbon atoms: AArepresents an amino acid absent of substituent(s) having more than two carbon atoms: AArepresents a basic amino acid: X represents a straight chain or branched bivalent saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms: Y represents basic substituent(s); straight chain, branched, or cyclic bivalent saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms; or an aromatic hydrocarbon group having 6 to 10 carbon atoms. The compound represented by the general formula (1) has dramatically improved PAR-2 activation potency compared to peptide comprised of 6 amino acids (Tethered receptor agonist peptide: TRAP) in spite of reduction of the number of amino acid.

PAR-2 agonist

A compound, or a salt or solvate thereof having a structure of Ar&#x2014;CO-AA-AA-AA-AA-NH&#x2014;X&#x2014;NRRis disclosed. Ar represents an optionally substituted phenyl group or an aromatic heterocyclic group; AArepresents a hydrophobic amino acid; AArepresents an unsubstituted amino acid containing 2 or more carbon atoms; AArepresents an unsubstituted amino acid containing 2 or more carbon atoms; AArepresents a hydrophobic amino acid; X represents a divalent saturated aliphatic hydrocarbon group having 2-6 carbon atoms; and Rand Rrepresent a saturated or unsubstituted aliphatic hydrocarbon group having 1-8 carbon atoms, or alternatively Rand Rmay form a ring together with an adjacent nitrogen atom. A pharmaceutical composition for prevention/treatment of diseases associated with PAR-2 is also disclosed. The pharmaceutical composition includes the above compound, a salt or a solvate thereof and a pharmaceutically acceptable carrier.

The present invention relates to a composition for prevention and treatment of kidney diseases comprising one or more effective component(s) of a PAR-2 activating agent which is able to activate PAR-2 and a pharmaceutically acceptable carrier. The present invention further relates to a method for prevention and treatment of kidney diseases comprising administration of a composition for prevention and treatment of kidney diseases containing a PAR-2 activating agent which is able to activate PAR-2 to patients suffering from kidney diseases, and also relates to the use of a PAR-2 activating agent which is able to activate PAR-2 for the manufacture of a composition for prevention and treatment of kidney diseases. The present invention furthermore relates to a method for screening an effective ingredient for prevention and treatment of kidney diseases comprising screening of the activating action of the test substance to PAR-2.

Method for treatment of kidney diseases

A bis(5-aryl-2-pyridyl) compound represented by formula (1) or a salt thereof: wherein A is a substituted or unsubstituted aromatic hydrocarbyl group or a substituted or unsubstituted aromatic heterocyclic group, and X is a group selected from the group consisting of moieties having formulas (2) to (5): wherein, in formula (2), m is an integer of 1 or 2; in formula (3), n is an integer of 1 to 6; and in formula (4), R is hydrogen or a lower alkyl group and p is an integer of 1 to 6.

Bis(5-aryl-2-pyridyl) derivatives

A bis(2-aryl-5-pyridyl) compound having formula (1) or a salt thereof:wherein A is a substituted or unsubstituted aromatic hydrocarbon group, and X is a substituent having one of the following formulas (2) to (4):wherein, in formula (2), Ris a hydrogen atom or a di(lower alkyl)amino(lower alkyl) group, and m is an integer of 1 or 2; in formula (3), Yand Yeach is a nitrogen atom or a CH group, and n is 0 or an integer of 1 to 6; in formula (4), Rand Reach is a hydrogen atom or a lower alkyl group, Z represents a single bond, a substituted methylene group, a substituted imino group, an oxygen atom or a cycloalkylene group, and p and q each is 0 or an integer of 1 to 6.

Bis(2-aryl-5-pyridyl) derivatives

Diamide compound and medicine containing the same

Preparation process of biphenylcarboxylic acid amide derivatives

Cyclic amide compound

Growing community of inventors

Chiba, Japan

Hiroyuki Ishiwata