Ono Pharmaceutical Co., Ltd.

Hisao Tajima

Yoshisuke Nakayama

Daikichi Fukushima

Hiroyuki Ohno

Koichiro Kitagawa

Hiroshi Hagiya

Tadashi Tatsumi

Masashi Minami

Shinya Kusuda

Takahiko Sakamoto

(1) A novel polypeptide prostaglandin E receptor, (2) a cDNA encoding the polypeptide and a fragment selectively hybridized to the sequence of the cDNA, (3) a replication or expression vector carrying the DNA, (4) a host cell transformed with the replication or the expression vector, (5) a method for producing the polypeptide which comprises culturing the host cells, (6) a monoclonal or polyclonal antibody against the polypeptide, (7) a pharmaceutical composition containing the polypeptide or the antibody, in association with pharmaceutically acceptable excipient and/or antibody, (8) a screening method for a compound having agonistic or antagonistic activity against EP1, comprising using the polypeptide or the host cell. The polypeptide of the present invention can be used for treating diseases, which is caused by over production of PGE, such as pain, fever and pollakiuria.

Prostaglandin receptor EP1

The present invention relates to the compound represented by formula (I) (wherein Rand Ris hydrogen atom, C1-8 alkyl etc.; Ris C1-8 alkyl which may be substituted with 1 to 3 halogen atom(s), phenyl; Ris hydrogen atom etc.; Rand Ris hydrogen atom, C1-8 alkyl etc.; X is sulfur atom or oxygen atom etc.; ringA is cyclic group which may have a substituent(s).), or a salt thereof. Toxicity of the compound represented by formula (I) is very low, and it is safe enough to use as a pharmaceutical agent and since it has PPAR &#x3b4; agonistic activity, it is useful as preventive and/or therapeutic agent for glucose&#x2022;lipid metabolic disorder, hypertension, circulatory diseases etc.

Phenylacetic acid derivative, process for producing the same, and use

A compound of formula (I) (wherein all symbols are as defined in the specification) and a salt thereof, and peroxisome proliferator activated receptor regulator comprising thereof as active ingredient. Because a compound of formula (I) have an activity of regulating peroxisome proliferator activated receptor regulator, the compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or treatment agent for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, ischemic heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or syndrome X.

Carboxylic acid derivatives compounds and agents comprising the compounds as active ingredient

A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from, risk factors of diabetes or syndrome X.

Carboxylic acid derivative and a pharmaceutical composition containing the derivative as active ingredient

The compound 3-(5-(2-(2-(4-methylphenyl)-5-methyloxazol-4-yl)ethoxy)-3,4-dihydronaphthalene-1-yl)propanoic acid or a nontoxic salt thereof. Because this compound has activity of regulating peroxisome proliferators activated receptor regulator, it is useful as a hyperglycemic agent, a hypolipidemic agent, a preventative and/or treatment agent for diseases associated with metabolic disorders etc.

Dihydronaphthalene derivative compounds and agent comprising the derivative as active ingredient

A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.

A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I)(wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.

A compound of formula (I)(wherein all symbols are as defined in the specification) and salt thereof, and peroxisome proliferator activated receptor regulator comprising thereof as active ingredient. Because a compound of formula (I) have an activity of regulating peroxisome proliferator activated receptor regulator, the compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or treatment agent for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diabetes or syndrome X.

Tetrahydroquinoline derivative compound and drug containing the compound as active ingredient

A plasmid DNA comprising a novel reporter gene DNA; a transformant transformed with the above plasmid DNA and a DNA encoding a known effector protein; a therapeutic agent for a cancer or an autoimmune disease, comprising both of the above DNAs as active ingredients; and a method for detecting a ligand of an intracellular receptor, comprising using the above transformant.

Plasmid DNA containing reporter gene DNA and use of the same

Carboxylic acid derivatives and drugs containing the same as the active ingredient

Polypeptide of protein p140 and DNAs encoding it

The present invention is related to a novel protein p140 polypeptide which is a key protein involved in the signal transmission system of insulin; method for preparation of it; DNA encoding the polypeptide; vector derived with the DNA; host cells transformed with the vector; antibody of the polypeptide; pharmaceutical composition containing the peptide or antibody; method for the prevention and/or treatment of diabetes, which is characterized by tyrosine phosphorylation of the protein p140; agent for the prevention and/or treatment of diabetes, which is characterized by containing a compound which can tyrosine phosphorylate protein p140, as active ingredient and the screening methods of the prevention and/or treatment agent. Tyrosine phosphorylation of protein p140 is an essential step in the induction of hypoglycemia by glucose uptake. Method and agent of prevention and/or treatment based on tyrosine phosphorylation of protein p140 in the present invention not only improve the diabetes-derived hyperglycemic conditions but are also useful for the treatment and/or prevention of diabetes, especially non-insulin dependent diabetes mellitus (NIDDM).

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Osaka, Japan

Hisao Tajima