Abstract: An N-phenylarylsulfonylamide compound of formula (I) (R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted with methyl; n is zero or 1), a synthetic intermediate for the compound and a process for its preparation. The compound of formula (I) binds to a prostaglandin E2 receptor, especially an EP1 subtype receptor, and antagonizes it. It is less affected by protein binding, so it has a satisfactory in vivo activity. Therefore, it is considered to be useful as an analgesic, an antipyretic agent, an agent for the treatment of pollakiuria (frequent urination) and/or lower urinary tract disease syndrome or an antineoplastic agent.

Abstract: Compositions for cancer or infection treatment via immunopotentiation caused by inhibition of immunosuppressive signal induced by PD-1, PD-L1, or PD-L2 and therapies using them, immunopotentiative substrates included as the active ingredient, screening methods of the substrates for cancer or infection treatment, cell lines used for the screening methods, evaluation methods that select the substrates for cancer treatment, and carcinoma cell transplanted mammals used for the evaluation methods. The compositions of the present invention that inhibits the function of PD-1, PD-L1, or PD-L2 are useful for treatment of cancer or infection.

Abstract: The present invention relates to a preventive and/or therapeutic agent for psychoneurotic diseases, comprising an EP3 antagonist represented by the general formula (I): (wherein the meanings of characters are defined in the description). This compound has an antagonistic potency against EP3 and exhibits efficacy through unusual action mechanism as a preventive and/or therapeutic agent for psychoneurotic disorder, psychosomatic disorder, anxiety disorder, depression and disorder caused by stress.

Abstract: A compound represented by the formula (I), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof: wherein X, Y, and W each independently represent a carbon atom or a nitrogen atom; Z represents CH or a nitrogen atom; R1 represents (1) C3-10 branched alkyl which may be substituted or (2) —(CH2)m—NR4R5; R2 and R3 each independently represent (1) a hydrogen atom, (2) C1-4 alkyl which may be substituted with a halogen atom, hydroxy which may be protected, amino which may be protected, or carboxyl which may be protected, (3) C2-4 alkenyl, (4) C2-4 alkynyl, (5) nitrile, (6) COOR6, (7) CONR7R8, (8) COR101, (9) S(O)nR102, or (10) a halogen atom, in which R6 represents a hydrogen atom or C1-4 alkyl, R7 and R8 each independently represent a hydrogen atom or C1-4 alkyl, R101 represents a hydrogen atom or C1-4 alkyl, R102 represents C1-4 alkyl, n represents 1 or 2; and Ar represents an aromatic ring which may be substituted, is useful as a pharmacologically active ingredient having a CRF antagon

Abstract: The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.

Abstract: A pharmaceutical composition for topical administration for prevention and/or treatment of diseases associated with decrease in bone mass comprising an EP4 agonist as an active ingredient. An EP4 agonist, in which includes a compound possessing prostaglandin skeleton as a representative, possesses promoting action on bone formation, so it is useful for prevention and/or treatment of diseases associated with decrease in bone mass (bone diseases such as primary osteoporosis, secondary osteoporosis, bone metastasis of cancer, hypercalcemia, Paget's disease, bone loss and bone necrosis, postoperative osteogenesis, alternative therapy for bone grafting).

Abstract: (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 PGE2, such as pain, fever and pollakiuria.

Abstract: The present invention relates to a substance specific to human PD-1 comprising a part that recognizes human PD-1, a part that recognizes a membrane protein in cell membrane of human PD-1-expressing cells, and linkers. Since the substance specific to human PD-1 selectively can recognize human PD-1 and a membrane protein on cell membrane of human PD-1-expressing cells and can transmit inhibitory signal of human PD-1, it is useful for therapy and/or prevention of diseases caused by immunopathy.

Abstract: A compound represented by formula (I) wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g.

Abstract: Compositions for cancer or infection treatment via immunopotentiation caused by inhibition of the immunosuppressive signal induced by PD-1, PD-L1, or PD-L2 and therapies using them, immunopotentiative substrates included as the active ingredient, screening methods of the substrates for cancer or infection treatment, cell lines used for the screening methods, evaluation methods that select the substrates for cancer treatment, and carcinoma cell transplanted mammals used for the evaluation methods. The compositions of the present invention that inhibit the function of PD-1, PD-L1, or PD-L2 are useful for treatment of cancer or infection.

Abstract: A compound represented by formula (I): (wherein the symbols are the same as defined in the description), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medicinal use thereof. The compound represented by formula (I) has CXCR4 antagonistic activity. It is hence useful as, e.g., a preventive and/or therapeutic agent for CXCR4-mediated diseases such as inflammatory/immunologic diseases (e.g., rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, and rejection reactions of transplanted organs), allergic diseases, infections diseases (e.g., human immunodeficiency virus infection and acquired immunologic deficiency syndrome), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease, metabolic diseases, cancer diseases (e.g., cancer, cancer metastasis) or as an agent for regeneration therapy.

Abstract: The present invention relates to a process for producing (2R)-2-propyloctanoic acid, which comprises subjecting (2R)-2-hexyloxirane to a two-carbon adding reaction with ring-opening reaction, followed by a protecting reaction of a hydroxyl group to convert it to a compound represented by formula (I): (wherein X represents an optionally protected hydroxyl group) and then subjecting the compound to a one-carbon adding reaction to convert it to (2R)-2-propyloctanamide, followed by recrystallization and hydrolysis. According to the process of the present invention, (2R)-2-propyloctanoic acid can be produced by less steps as compared with the conventional method without a dangerous reaction.

Abstract: An EP2 agonist which may have an EP3 agonistic effect has an effect of regenerating and/or protecting nerves, and is therefore useful as a therapeutic agent for a disease of the peripheral nervous system, such as a lower or upper motor neuron disease, a nerve root disease, plexopathy, thoracic outlet compression syndrome, peripheral neuropathy, neurofibromatosis and neuromuscular transmission disease. An EP2 agonist which has an EP3 agonistic effect is a safe and effective agent for the regeneration and/or protection of nerves which has little influence on the circulatory system.

Abstract: The present invention relates to a hemorrhage reducing agent in cerebrovascular disorder containing a poly (ADP-ribose) polymerase inhibitor (PARP inhibitor). The PARP inhibitor provides an inhibitory effect of vascular endothelial cell disorder so that it may reduce hemorrhage in cerebrovascular disorder. In addition, the PARP inhibitor inhibits the hemorrhage that is concerned about in thrombolytic agent use by using together with a thrombolytic agent, and an effect of extending therapeutic time window of a thrombolytic agent may be further expected. Furthermore, the PARP inhibitor can be a safe hemorrhage reducing agent with fewer side effects because it does not affect the blood coagulation system and the fibrinolytic system.

Abstract: The present invention relates to a DNA having a promoter region containing regulatory sequences of human adiponectin gene, transformants transformed with the DNA, a screening method of a compound which can enhance the human adiponectin promoter activity, which the transformants are used, and the screening kit, and a screening method of a preventive/therapeutic medicine for syndromes such as Syndrome X, metabolic syndrome, multiple risk factor syndrome, insulin resistant syndrome, deadly quartet, and visceral fat syndrome, metabolic disorders such as diabetes, obesity, hypercholesterolemia, and hyperlipoproteinemias, hyperlipidemia, arteriosclerosis, hypertonia, circulatory system disease, and hyperphagia and a pharmaceutical composition obtained by using them.

Abstract: The present invention relates to a compound represented by formula (I) wherein R1 represents optionally protected hydroxy or oxo, indicates ?-configuration, ?-configuration or a mixture of these in an arbitrary proportion, n represents an integer of 1 to 3, and m represents 0 or an integer of 1 to 10; and wherein two or more R1's are not bound to the same carbon atom other than the terminal carbon atom, a salt thereof or a prodrug thereof. The compounds represented by formula (I) have an ability to improve astrocyte function, and they are useful as a preventive and/or therapeutic agent for a brain infarction, neuronal dysfunction by brain infarction, Parkinson's disease, Parkinson's syndrome, amyotrophic lateral sclerosis or Alzheimer's disease.

Abstract: The present invention relates to a carboxylic acid compound of formula (I): wherein R1 is H, alkyl; m is 2, 3; n is 0-2; R2 is phenyl, naphthyl, benzofuran, benzothiophene; Q is —CH2—O-Cyc1, —CH2-Cyc2, -L-Cyc3; R3a and R3b each independently is hydrogen, alkyl or taken together form tetrahydro-2H-pyran; a pharmaceutically acceptable salt thereof, a method for producing a process of the preparation thereof and a pharmaceutical agent comprising the same as an active ingredient. The compound of formula (I) have an antagonizing activity against PGE2 receptor, specifically EP3 receptor which is subtype thereof, and are useful for the prevention and/or treatment of itching, pain, urinary disturbance or stress disease.

Abstract: An agent for treating acute cerebral infarction, comprising (2R)-2-propyloctanoic acid or a salt thereof, which is used for administration after a lapse of time of from about 5 hours to about 72 hours from the onset of the disease is useful for treating acute cerebral infarction, since it safely improves acute cerebral infarction or accompanying symptoms in the patient of acute cerebral infarction, specifically in the patient of acute cerebral infarction defined as a score of 7 to 22 on NIH Stroke Scale.

Abstract: Formula (I) compounds: wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl subsituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together is a saturated heterocyclic ring or amino acid residue; and non-toxic salts and acid addition salts thereof.

Abstract: Formula (I) compounds: wherein R1 is alkyl substituted by fluorine(s); R2 is hydroxy, alkoxy, alkoxy substituted by phenyl, NR3R4, in which R3, R4 is (i) hydrogen, (ii) alkyl, (iii) phenyl, (iv) phenyl substituted by alkoxy or carboxyl, (v) heterocyclic ring containing nitrogen atom, (vi) alkyl substituted by phenyl, phenyl substituted by alkoxy or carboxyl, heterocyclic ring containing nitrogen atom, (vii) the nitrogen bonded to R3 and R4, taken together is a saturated heterocyclic ring or amino acid residue; and non-toxic salts and acid addition salts thereof.