Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.

Abstract: The present invention provides a compound of the formula: wherein Ar represents an aromatic group which may be substituted; X represents methylene, S, SO, SO2 or CO; Y represents a spacer having a main chain of 2 to 5 atoms; n represents an integer of 1 to 5; i) R1 and R2 each represents a hydrogen atom or a lower alkyl which may be substituted, ii) R1 and R2 form, taken together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic ring which may be substituted, or iii) R1 or R2 together with —(CH2)n—N═ form, bonded to a component atom of Ring B, a spiro-ring which may be substituted; Ring A represents an aromatic ring which may be substituted; Ring B represents a 4- to 7-membered nitrogen-containing non-aromatic ring which may be further substituted by alkyl or acyl, with a proviso that X represents S, SO, SO2 or CO when Ring A has as a substituent a group represented by the formula: —NHCOR11 where R11 represents alkyl, alkoxyalkyl, alkylthio

Abstract: A pharmaceutical composition which comprises an insulin sensitizer in combination with an anorectic, which is useful as an agent for preventing or treating diabetes.

Abstract: An orally disintegrable tablet, of the present invention, which comprises (i) fine granules having an average particle diameter of 400 &mgr;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: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.

Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.

Abstract: A compound of the formula: wherein ring A is an optionally substituted benzene ring; ring B′ is an optionally substituted non-aromatic heterocyclic ring having, the same or different, two or more hetero atoms; R1 is a hydrogen atom or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; Y is an optionally substituted amino group or an optionally substituted N-containing saturated heterocyclic group; n denotes an integer of 1 to 10, provided that when the ring B′ is a 5- to 7-membered ring, the ring B′ contains at least one nitrogen atom as hetero atom and n denotes an integer of 2 to 10, or a salt thereof. The compounds and salts thereof have an excellent cholinesterase inhibitory activity and antidepressant activity, and are useful as therapeutic and/or prophylactic medicaments of senile dementia.

Abstract: The present invention includes a formulation which comprises an antibacterial substance and an antiulcer substance, wherein at least either of them is formulated into a gastrointestinal mucosa-adherent solid preparation. The formulation of the present invention shows long retention time in the gastrointestinal tract because of adhesion to the gastrointestinal tract mucosa, synergetically enhances the pharmaceutical effects of an antibacterial substance, specially antibiotic against Helicobacter pylori (HP) and an antiulcer substance, with very low doses of active ingredients, particularly the anti-HP antibiotic with low prevalence of side effects. The present agent is useful as an antiulcer agent, showing potent anti-HP activity.

Abstract: Prophylactic or therapeutic drugs for diabetic nephropathy or glomerulonephritis, comprising, as an active ingredient, a compound or salt thereof represented by formula (I) wherein R1 stands for H or an optionally substituted hydrocarbon residue; R2 stands for an optionally esterified carboxyl group; R3 stands for a group actually or potentially capable of forming an anion; X shows that the phenylene and phenyl groups bind to each other directly or through a spacer having an atomic chain length of two or less; n stands for 1 or 2; ring A stands for a benzene ring having an optional substituent in addition to R2; Y stands for a bond, —O—, —S(O)m—, wherein m stands for 0, 1 or 2, or —N(R4)— wherein R4 stands for H or an optionally substituted alkyl group are disclosed.

Abstract: A compound of the formula: wherein Ar is an optionally substituted aromatic hydrocarbon or aromatic heterocyclic group, R is H, halogen or a group bonded through C, N, O, S or P, W is halogen or a group bonded through C, N, O, S or P, X is H or a group bonded through C, N, O or S, Y is H or a group bonded through C, N, O, S or P, or X and Y together with the adjacent nitrogen atom to Y may form an optionally substituted nitrogen-containing heterocyclic group which may further have N, O, S and/or P, or a salt thereof, a method of production thereof and agrochemicals containing the above compound [I]. The compound [I] and their salts are effective in preventing sanitary or horticultural insect pests and animal and plant parasites and can exert potent insecticidal activities when they are applied to harmed living animals or plants.

Abstract: The transgenic animal of this invention can be used as an animal model for renal disease, bone disease, joint disease, pulmonary disease, hyperlipidemia, arteriosclerosis, cardiac disease, diabetes, obesity, digestive organ disease, infectious disease, allergic disease, endocrine disease, dementia or cancer, or complications thereof; and provides a nonhuman transgenic mammal for the unraveling of the mechanisms of said diseases, explorations for the development of therapeutic modalities for the diseases, and the screening of candidate therapeutic drugs.

Abstract: The present invention provides an intermediate for producing a thienopyridine derivative useful as a GnRH antagonist as well as an efficient and safe method for producing the same in an industrial scale at a high yield.

Abstract: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc.

Abstract: The present invention provides a method for chemically removing a N-terminal methionine residue selectively, specifically and efficiently from a peptide or a salt thereof having an optionally oxidized methinine residue at its N-terminal. The method reacts a peptide or a salt thereof having an optionally oxidized methinine residue at its N-terminal with an &agr;-diketone derivative, followed by hydrolysis.

Abstract: The present invention provides a wettable or water-soluble granular agrochemical composition which comprises a guanidine derivative of the formula: wherein R1 represents a homocyclic or heterocyclic group which may optionally be substituted; n is 0 or 1; R2 represents hydrogen or a hydrocarbon group which may optionally be substituted; R3 represents a primary, secondary, or tertiary amino group; X represents an electron attractive group; or a salt thereof, an alkenylsulfonate and a carrier. The agrochemical composition has excellent disintegrability and dispersibility in water.

Abstract: The present invention relates to an aqueous suspension comprising (i) a compound of the formula: or a salt thereof, (ii) a condensate of formaldehyde with an aromatic sulfonic acid or a salt thereof or a polyoxyalkylene allyl phenyl ether sulfate, and (iii) an absorptive water-soluble polymer. The aqueous suspension of the invention can be used with advantage as a stable aqueous suspension of low viscosity providing for excellent delivery from a container, with excellent dispersibility in diluent water and excellent long-term fluidity free from caking due to precipitation of the suspended particles.

Abstract: Pharmaceutical composition which comprises an insulin sensitivity enhancer in combination with other antidiabetics differing from the enhancer in the mechanism of action, which shows a potent depressive effect on diabetic hyperglycemia and is useful for prophylaxis and treatment of diabetes.

Abstract: A solid preparation which comprises (i) a pharmaceutically active ingredient, (ii) one or more water-soluble sugar alcohols selected from the group consisting of sorbitol, maltitol, reduced starch saccharide, xylitol, reduced palatinose and erythritol, and (iii) low-substituted hydroxypropylcellulose having hydroxypropoxyl group contents of 7.0 to 9.9 percent by weight; which exhibits excellent buccal disintegration and dissolution and also appropriate strength.

Abstract: A compound of formula (I) wherein R1 and R2 each is hydrogen, hydroxy, C1-4 alkoxy, C1-4 alkoxy-carbonyl or C1-4 alkyl which may be substituted; R3 is hydrogen, halogen, hydroxy or C1-4 alkoxy which may be substituted; or adjacent two R3 may form C1-4 alkylenedioxy; R4 is hydrogen or C1-4 alkyl; R6 is C1-4 alkyl which may be substituted or a group of the formula (A) wherein R5 is hydrogen of R4 and R5 may form heterocycle; and n is 0-5, or a salt thereof, has an excellent GnRH-antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases.

Abstract: The compound of the present invention possesses excellent gonadotropin-releasing hormone antagonizing activity, and is useful for preventing or treating sex hormone-dependent diseases, e.g., sex hormone-dependent cancers (e.g., prostatic cancer, uterine cancer, breast cancer, pituitary tumor), prostatic hypertrophy, hysteromyoma, endometriosis, precocious puberty, amenorrhea syndrome, multilocular ovary syndrome, pimples etc. or as a pregnancy regulator (e.g., contraceptive), infertility remedy or menstruation regulator.