Abstract: We describe a method of identifying a molecule suitable for the treatment, prophylaxis or alleviation of a GPR86 associated disease, in particular inflammatory disease or pain, the method comprising determining whether a candidate molecule is an agonist or antagonist of GPR86 polypeptide, in which the GPR86 polypeptide comprises the amino acid sequence shown in SEQ ID NO: 3 or SEQ ID NO: 5 or SEQ ID NO: 7, a fragment thereof or a sequence which is at least 90% identical thereto.

Abstract: The present invention provides mTOR inhibitors of the formula wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods of making the compounds and intermediates thereof; and methods of using the compounds.

Abstract: It is intended to provide a process for producing unstable amorphous benzimidazole compounds having a proton pump inhibitor function, and stable solid preparations for medicinal use containing these compounds which are produced by blending such an amorphous benzimidazole compound with a nontoxic base such as a basic inorganic salt, forming an intermediate coating layer on the layer containing the active ingredient and further forming an enteric coating layer or a release-controlling coating layer.

Abstract: An orally disintegrable tablet, of the present invention, which comprises (i) fine granules having an average particle diameter of 400 ?m or less, which fine granules comprise a composition coated by an enteric coating layer, said composition having 10 weight % or more of an acid-labile physiologically active substance and (ii) an additive, has superior disintegrability or dissolution in the oral cavity so that it can be used for treatment or prevention of various diseases, as an orally disintegrable tablet capable of being administered to the aged or children and easily administered without water. Also, because the tablet of the present invention contains fine granules having the average particle diameter such that it will not impart roughness in mouth, it can be administered easily without discomfort at the administration.

Abstract: The present invention relates to a compound represented by the formula (I) wherein R1 is a group represented by the formula wherein R2, R3, R4, R5, R6, R7 and R8 are each independently a hydrogen atom or a C1-6 alkyl, or a salt thereof. The compound of the present invention is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and metabolic diseases such as diabetes and the like.

Abstract: Disclosed is a vinamidinium salt represented by the formula (I): [wherein R1 represents a hydrogen atom, a halogen atom, an optionally substituted hydrocarbon group or the like; R2 and R3 are the same or different and each represents a lower alkyl group, or alternatively R2 and R3 may combine together to form a ring; R4 and R5 are the same or different and each represents a lower alkyl group, or alternatively R4 and R5 may combine together to form a ring; X and Y are the same or different and each represents a bromine atom or a chlorine atom; n represents a number of not less than 2; and m represents 0 or n], which can be used as a general purpose reagent useful for synthesis of various nitrogen-containing heteroaromatic rings having a substituent. The vinamidinium salt has excellent storage stability and reaction selectivity. A method for synthesizing a nitrogen-containing heteroaromatic ring compound using the vinamidinium salt is also disclosed.

Abstract: The present invention provides a solid preparation containing compound (I) [compound (I) is as defined in the specification] or a salt thereof, and metformin hydrochloride, which is useful as a therapeutic drug for diabetes and the like, and superior in the preservation stability. A solid preparation having a first part and a second part: a first part: a part containing compound (I) or a salt thereof and substantially free of metformin hydrochloride a second part: a part containing metformin hydrochloride and substantially free of compound (I) and a salt thereof.

Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a member selected from the group consisting of: wherein E is CH or N, Q is selected from the group consisting of CO, CS, SO, SO2, or C?NR4, and L, X, Z, R2 and R3 are as defined herein.

Abstract: An object of the present invention is to provide an agent for preventing or treating schizophrenia or the like, wherein the compound of the present invention has GPRS2 agonist activity.

Abstract: There is provided an imidazole derivative useful as a thrombosis treating agent, which is represented by the formula (I): wherein R represents an optionally substituted cyclic hydrocarbon group or an optionally substituted heterocyclic group, W represents a bond or an optionally substituted divalent linear hydrocarbon group, X represents an optionally substituted divalent hydrocarbon group, Y represents —CO—, —S(O)—, —S(O)2— or a bond, ring A represents an optionally substituted pyrrolidine ring, an optionally substituted piperidine ring or an optionally substituted perhydroazepine ring, Z1 and Z3 independently represent a bond or an optionally substituted divalent linear hydrocarbon group, Z2 represents —N(R1)—, —O—, —S(O)—, —S(O)2—, —CO—, —CH(R1)— or a bond, ring B represents an optionally substituted imidazole ring, wherein a substituent which the optionally substituted imidazole ring represented by ring B may have may be taken together with R1 to form an optionally substituted ring, and a represents 0

Abstract: The present invention relates to a compound represented by the formula (I) or (I?): wherein each symbol is as defined in the specification, or a salt thereof, and a PI3K and(or) mTOR inhibitor containing the compound or a prodrug thereof.

Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

Abstract: Provided is a combination drug. The present invention provides a pharmaceutical agent comprising (1) a HER2 inhibitor having a pyrrolopyrimidine skeleton or pyrazolopyrimidine skeleton, and (2) not less than one pharmaceutical agent selected from an mTOR inhibitor, a PI3 kinase inhibitor and a cMet inhibitor in combination.

Abstract: The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula (I) wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR1 (R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R2 is carbamoyl optionally having substituent(s); and R3 is hydroxy optionally having substituent(s), or a salt thereof.

Abstract: The present invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, a gonadotrophic hormone secretion stimulating activity, sex hormone secretion stimulating activity, etc.). By substituting the constituent amino acids of metastin with specific amino acids in the metastin derivative of the present invention, blood stability, solubility, etc. are more improved, gelation tendency is reduced, pharmacokinetics are also improved, and an excellent cancer metastasis suppressing activity or a cancer growth suppressing activity is exhibited. Furthermore, the metastin derivative of the present invention has the effects of suppressing gonadotropic hormone secretion, suppressing sex hormone secretion, etc.

Abstract: The present invention provides a novel prophylactic or therapeutic agent for attention deficit/hyperactivity disorder. A prophylactic or therapeutic agent for attention deficit/hyperactivity disorder, containing (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide as an active ingredient.

Abstract: The present invention provides a pharmaceutical composition, wherein solubility and stability of a water-insoluble or slightly water-soluble compound represented by formula (I): wherein each symbol is as defined in the specification, are improved, by combination of the above-mentioned compound and a cyclodextrin derivative and a method for improving solubility, stability and the like of the above-mentioned compound.

Abstract: A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.

Abstract: A mechanism for opening and closing an opening portion is disclosed. The mechanism can simply and reliably open and close the opening portion without requiring a spring but using a simple mechanism and can stably maintain the closed state of the opening portion. When the opening portion is closed by a lid, with the head end side of the opening and closing member being protruded from the opening portion, the head end of the opening and closing member makes contact with the surface of the lid which faces the inner side of the opening portion, causing the lid to rotate about one end thereof which is rotatably supported by a rotation supporting shaft. This changes the state of the opening portion from the closed state to the opened state.

Abstract: The present invention provides an orally-disintegrating solid preparation comprising fine granules showing controlled release of a pharmaceutically active ingredient, wherein the outermost layer of the fine granules is coated with a coating layer comprising hydroxypropylmethylcellulose and low-substituted hydroxypropylcellulose and breakage of the fine granules during tableting is suppressed.