Abstract: A quinoxalinone derivative of the formula (I): or a pharmaceutically acceptable salt or ester thereof, wherein; X is NH, S or the like; Y is O or the like; the partial structure is, for example, the formula: B1, B2, . . . , Bn?1 and Bn, (in which n is 4, 5 or 6) are each independently CH, N or the like; B?1, B?2, . . . , B?n?1 and B?n (in which n is 4, 5 or 6) are each independently hydrogen or the like; and R is hydrogen, lower alkyl or the like.

Abstract: A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided. The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.

Abstract: A full-length cDNA encoding a human-derived G protein-coupled receptor protein is isolated by screening a human hippocampus library. Also, a rat-derived cDNA corresponding to the human-derived cDNA is isolated. Proteins encoded by these cDNAs have an activity of lowering intracellular cAMP concentration under stimulation with histamine. These proteins are usable as tools in screening ligands thereof or in screening candidate compounds for drugs capable of regulating signal transduction from the above proteins.

Abstract: This invention relates to a process for making spirolactone compounds analogous to formula I

Abstract: The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V and W are independently methine or nitrogen, said methine being optionally substituted by a substituent, and at least two of T, U, V and W are said methine groups; and X is nitrogen or methine. The compounds of the present invention are useful as agents for the treatment of various kinds of diseases related to NPY, for example, cardiovascular disorders, nervous system disorders, genitative diseases, metabolic diseases, genital or reproductive disorders, gastrointestinal disorders, respiratory disorders, inflammatory diseases or glaucoma, and the like.

Abstract: The present invention relates to a compound of Formula (I) and the manufacturing method(s) thereof and the use thereof: Formula (I) wherein: Ar is a nitrogen-containing heteroaromatic ring group; X and Z are each a carbon atom, and so on; Y is CO, and so on; R1 is a hydrogen atom, and so on; R2 and R3 are each a hydrogen atom, and so on; R4 and R5 are each a hydrogen atom, and so on; and the formula is a single bond or a double bond. According to the present invention, the compound of the present invention can provide Cdk4 and/or Cdk6 inhibitors for treating malignant tumors, because the compounds of the present invention exhibit a prominent growth inhibitory activity against tumor cells.

Abstract: The present invention relates to a compound represented by Formula [I]: wherein X is O, S, NH or CH2; Y1, Y2, Y3, Y4 and Y5, which may be identical or different, are each CH or N; however, at least one of Y1, Y2, Y3, Y4 and Y5 is N; Z1 and Z2, which may be identical or different, are each CH or N; n is an integer from 1 to 3; R1 is a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aliphatic heterocyclic ring or an aromatic heterocyclic ring, or a bicyclic aliphatic saturated hydrocarbon group; R2 and R3, which may be identical or different, are each a hydrogen atom, a lower alkyl group, a lower alkenyl group, a C3-C8 cycloalkyl group, a C6-C10 aryl group, an aromatic heterocyclic ring, or the like; and R4 is a hydrogen atom, a lower alkyl group, a C3-C6 cycloalkyl group or the like, or a pharmaceutically acceptable salt or ester thereof, and a selective inhibitor against Cdk4 and/or Cdk6 or an anticancer agent containing the compound or a pharmaceutically acceptable salt or ester thereof.

Abstract: Compounds represented by the general formula (I) wherein Ar1 represents an aryl or heteroaryl which may be substituted; n represents 0 or 1; T, U, V and W each independently represent a nitrogen atom or a methine group which may have a substituent selected from the group consisting of halogen, lower alkyl, hydroxy and lower alkoxy, wherein at least two of which represent said methine group; X represents methine, hydroxy substituted methine or nitrogen atom; Y represents an imino which may be substituted with lower alkyl, or oxygen; and a salt, ester or N-oxide derivative thereof. The compounds exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metabolic diseases, sexual and reproductive dysfunctions, gastro-intestinal disorders, respiratory disorders, inflammation or glaucoma, and the like.

Abstract: The invention provides the compounds represented by the formula (I) in which, R stands for a dihydroxy-substituted C1-C6 alkyl group, and Cy stands for an optionally substituted C6-C10 bi- or tri-cyclic aliphatic carbocyclic group. These compounds act as nociceptin receptor antagonist, and are useful, for example, as relievers against tolerance to narcotic analgesic, dependence on narcotic analgesic or addiction; analgesic enhancers; antiobestic or appetite suppressors; treating or prophylactic agents for cognitive impairment and dementia/amnesia; agents for treating developmental cognitive abnormality; remedy for schizophrenia; agents for treating neurodegenerative diseases; anti-depressant or treating agents for affective disorder; treating or prophylactic agents for diabetes insipidus; treating or prophylactic agents for polyuria; and remedy for hypotension and the like.

Abstract: A sampling method sampling a lower-layer liquid from a liquid body comprised of two layers of liquids, an upper-layer liquid (octanol) and the lower-layer liquid (buffer solution), without mixing the layers. An extracting device is provided with a tubular apical end and is adapted to bring the apical end from above into a liquid to extract the liquid through the apical end. The method includes a plug injection step of injecting a plug liquid without mixing with the upper-layer liquid 50a, into the apical end 11a of the extracting device, and an extraction step of extracting the lower-layer liquid with the plug liquid by means of the extracting device.

Abstract: Internal domain 3 of seven transmembrane G protein-coupled receptors is important for G protein binding or receptor activity, and is well conserved. In H3 receptors, which are a type of G protein-coupled receptor, this region is also conserved in the same way. Therefore, as a result of using PCR to introduce point mutations into sequences encoding the region in H3 receptor cDNA, H3 receptor mutants comprising extremely strong constitutive activity could be successfully produced. The present inventors further found that by using constitutively active H3 receptor mutants, drug candidate compounds such as H3 receptor inverse agonists can be screened more easily and efficiently.

Abstract: The present invention relates to an industrially preferable process for producing an indolopyrrolocarbazole derivative represented by the formula (I): or a pharmaceutically acceptable salt thereof, which is useful as an anti-cancer agent. The above process comprises treating a compound represented by the formula (V): or a pharmaceutically acceptable salt thereof, a solvate thereof or a salt thereof, with a base in an inert solvent, followed by treatment with an acid, and further treating the resulting reaction solution with a base in an inert solvent and subsequently with an acid, and then reacting the resulting compound with an acid addition salt of hydrazine diol in the presence of an acid scavenger, followed by removal of protecting group(s) from the resulting compound.

Abstract: The present invention relates to a compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 is a linear or branched alkoxy group, a cycloalkoxy group, a linear or branched lower alkyl group, etc.; R2 is halogen atom, a lower alkyl group, etc.; Q1 is carbon atom or nitrogen atom; Q2 is carbon atom which may be substituted with oxo group; the formula (III): ??(II) is a single bond or a double bond; A is a group selected from the group consisting of the substitutent group ?; and R5 is hydrogen atom, a lower alkyl group, cyano group, an alkoxy group or a trialkylsilyl group; having an mGluR1 inhibiting action and being useful as treatment and/or prevention of convulsion, acute pain, cerebral disturbance such as cerebral infarction or transient cerebral ischemia onset, anxiety, chemical dependency or Parkinson's disease.

Abstract: This invention relates to a novel compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is —S(O)p-A, —S—(O)q-B or —O-D, wherein p and q, which are the same or different, each represent an integer from 0 to 2, A is a straight chain C1-C10 alkyl group which may be substituted by R10, and B and D each independently represent R12 which may be substituted by R10; R2 is a hydrogen atom, a halogen atom, or a straight chain or branched C1-C6 alkyl group which may be substituted by R10; X1 and X2 each independently represent N or CH, but cannot both be N; the formula (II): shows a monocyclic or bicyclic heteroaryl group which has a nitrogen atom adjacent to the carbon atom bonded to the amide group, and the heteroaryl group may be substituted by R10; R10 is R11, or a hydrocarbon group which may be substituted by R11; R11 is, for example, a hydrogen atom or amino; and R12 is, for example, phenyl, thiazolyl, pyridyl or methylene dioxyphenyl.

Abstract: The present inventors conducted a similarity search of the amino acid sequence of known G protein-coupled receptor proteins in GenBank, and obtained a novel human GPCR gene “BG37”. cDNA containing the ORF of the gene was cloned and its nucleotide sequence was determined. Moreover, novel GPCR “BG37” genes from mouse and rat were isolated. Use of the novel GPCR of the present invention enables screening of ligands, compounds inhibiting the binding to a ligand, and candidate compounds of pharmaceuticals which can regulate signal transduction from the “BG37” receptor.

Abstract: The present invention relates to a protein which excretes cancer chemotherapeutic drugs from a cell and which confers drug-resistance on the cell, a DNA encoding the protein, a method for detecting a cell type resistant to cancer chemotherapeutic drugs, a method for screening an inhibitor to overcome the resistance to cancer chemotherapeutic drugs as well as utilizing this knowledge to improve the therapeutic treatment of cancer patients.

Abstract: The present invention identifies the presence of MCH-2R in the dog, ferret and rhesus monkey. MCH-2R is a G-protein coupled receptor that responds to MCH and is distinct from MCH-1R. MCH-2R polypeptide and nucleic acid sequences related to the dog, ferret, and rhesus monkey MCH-2R are described herein along with uses of such polypeptides and nucleic acids.

Abstract: Compounds of the formula (I): (wherein A is an optionally substituted straight-chain hydrocarbon having 1 to 6 carbon atoms, which is optionally intervened by oxygen or nitrogen atom; Ar1 is aryl or heteroaryl, any of which is optionally substituted; n is 0 or 1; R0 is hydrogen, or lower alkylene attached to an arbitrary, bondable position of A; T, U, V and W are independently nitrogen atom or optionally substituted methine, and at least two of T, U, V and W are said methine group; X is —N(SO2R1)—, —N(COR2)— or —CO—; Y is —C(R3)(R4)—, —O— or —N(R5)—; Z is methine or nitrogen atom) exhibit NPY antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders such as hypertension, nephropathy, heart disease, vasospasm, arteriosclerosis, etc., central nervous system disorders such as bulimia, depression, anxiety, seizure, epilepsy, dementia, pain, alcoholism, drug withdrawal, circadian rhythm disorders, schizophrenia, etc.

Abstract: The present inventors conducted a similarity search of the amino acid sequence of known G protein-coupled receptor proteins in GenBank, and obtained a novel human GPCR gene “BG37”. cDNA containing the ORF of the gene was cloned and its nucleotide sequence was determined. Moreover, novel GPCR “BG37” genes from mouse and rat were isolated. Use of the novel GPCR of the present invention enables screening of ligands, compounds inhibiting the binding to a ligand, and candidate compounds of pharmaceuticals which can regulate signal transduction from the “BG37” receptor.

Abstract: This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I); [in which A signifies a group expressed by a formula (a0) or (b0); Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X? signifies an anion].