Abstract: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.

Abstract: This invention relates to a process for producing optically active alcohols using asymmetric reduction of aromatic ketones. This process gives optically active alcohols in high enantioselectivity at large scale production. Aromatic ketones represented by formula (I) [wherein, R1 are selected from hydrogen atom, halogen atom, lower alkyl group etc. R2 is —(CH2)n-R3 [wherein, n is 1 to 5 integer. R3 are selected from hydrogen atom, halogen atom, lower alkoxycarbonyl group etc. and formula (II) and (III). {wherein, R4 is selected from lower alkyl group (1 to 5 carbon atom) etc. R5 and R6 are the same or different and are selected from hydrogen atom, halogen atom, lower alkyl group etc.}]] are reduced by sodium borohydride, chlorotrimethylsilane and optically active 2-[bis(4-methoxyphenyl)hydroxymethyl]pyrrolidine represented by formula (IV) to give optically active alcohol represented by formula (V) stereoselectively. (wherein, R1 and R2 are as defined above.

Abstract: The invention is directed to a drug for treating hypertension combined with serum hyperuricemia and/or hypercholesterolemia, with the active ingredients being 2-propyl-3-{[21-(1H-tetrazole-5-yl)biphenyl-4-yl]methyl}-5,6,7, 8-tetrahydrocyclohepta imidazole-4-(3H)-one and a prodrug or salt thereof. Pratosartan can be used in combination with one or more diuretics chosen from sulfonamide-, phenoxyacetic acid- and thiazide-type diuretics, triamterene, amiloride, spironolactone, potassium canrenoate and traxanox sodium. Also, pratosartan can be used in combination with one or more hypolipidemic drugs chosen from statins, fibrates, cholesterol absorption inhibitors, cholesterol sequestrants and cholesterol excretion enhancers.

Abstract: This invention related to a series of new phosphonic acid derivatives having anti-hyperphosphatemia activity. (I) [wherein: A is selected from —(CH2)n—, —CO—, —(CH2)n—CO—(CH2)m—, —(CH2)n—CS—(CH2)m— or branched alkylene group. B ring and C ring are selected from benzene ring, naphthalene ring, azulene ring or, heterocycle or fused heterocycle. D is —(CH2)(n+1)—, —(CH2)-O—(CH2)m—, —(CH2)—S(O)o—(CH2)m—, —CF3 or —(CH2)n—NR10—(CH2)m— (wherein: D ring is connected with the carbon atom composing C ring.) E is selected from oxygen atom or sulfur atom. P is phosphine atom. R1˜R7 (wherein R1 and R2, R4 and R5 are joined together with neighbored carbon atom to form 5˜7 membered saturated or unsaturated hydrocarbon ring, or 5˜6 membered fused heterocycle. R1, R2 and R3 are not hydrogen atom if B ring is benzene ring.) may be the same or different and are substituents. R8 and R9 are may be the same or different and are substituents. R10 is alkyl group. n and m are 0-10. o is 0-2.

Abstract: The piperidine derivative of the present invention in which the 4-position of the piperidine ring is bonded, via vinylene, to a mono-substituted (—R1) or unsubstituted benzene ring and the 1-position of the piperidine ring has an acyl group [—C(?O)—R4], or a pharmaceutically acceptable salt thereof has an excellent sodium channel inhibition action and an excellent analgesic action and shows a high analgesic effect particularly to neurogenic pain.

Abstract: A process for producing an azulene derivative useful as a Na+-glucose cotransporter inhibitor, which is high in yield, is simple in operation, is low in cost, is suited for environmental protection, and is advantageous industrially, the process being characterized by reducing and deprotecting at least one compound selected from penta-acyl compounds and tetra-acyl compounds or salts thereof to obtain a C-glycoside compound; and a useful intermediate for synthesis of such an azulene derivative, obtained in the course of the above process.

Abstract: The purpose in this invention is to providing drugs for treating or preventing duplication of hypertension with serum hyperuricemia and/or hypercholesterolemia that is much frequency among the duplication onset in geriatric diseases. This invention is related to drugs for treating or preventing duplication of hypertension with serum hyperuricemia and/or hypercholesterolemia of which active principles are 2-propyl-3-{[2?-(1H-tetrazole-5-yl) biphenyl 4-yl]methyl}-5,6,7,8-tetrahydrocyclohepta imidazole-4-(3H)-one and that prodrug or that salt. Pratosartan is able to use in combination with one or more than two diuretics chosen from sulfonamide-, phenoxyacetic acid- and thiazide-type diuretics, triamterene, amiloride, spironolactone, potassium canrenoate and traxanox sodium. Also, pratosartan is able to use in combination with one or more than two hypolipidemic drugs chosen from statins, fibrates, cholesterol absorption inhibitors, cholesterol sequestrants and cholesterol excretion enhancers.

Abstract: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.

Abstract: The invention provides a novel nitrogen-containing heterocyclic derivative having 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the nitrogen-containing heterocyclic derivative and a pharmaceutically acceptable salt thereof, in particular, a pharmaceutical composition effective as a sodium channel inhibitor, having an excellent analgesic action especially on neuropathic pain with minimized side effects.

Abstract: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.

Abstract: The present invention provides an azulene derivative and a salt thereof, wherein an azulene ring is bonded to a benzene ring directly or via a lower alkylene which may be substituted with a halogen atom and the benzene ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes-related diseases such as insulin-resistant diseases and obesity.

Abstract: A serum cholesterol lowing agent or a preventive or therapeutile agent for atherosclerosis, which each comprises a combination of a compound represented by the following general formula (I) or pharmaceutical acceptable salts thereof with a cholesterol biosynthesis inhibitor and/or a fibrate type cholesterol lowing agent. (I) (b) (a) [In the formula, A1, A2, A3 and A4 each is hydrogen, a group represented by the formula (b), or a group represented by the formula (a), provided that at least one of these is a group represented by the formula (a); A2 is C1-5 alkyl etc; and n. p, q and r each is an integer of 0, 1 or 2.

Abstract: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.

Abstract: Novel ?-lactam compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof which are useful as serum cholesterol-lowering agents: (I) wherein A1, A3 and A4 represent each hydrogen, halogen C1-5 alkyl, C1-5 alkoxy, —COOR1, a group represented by the following general formula (b): (b) wherein R1 represents hydrogen or C1-5 alkyl, or a group represented by the following general formula (a): (a) wherein R2 represents —CH2OH, —CH2OC(O)—R1 or —CO2—R1; R3 represents —OH or —OC(O)—R1; R4 represents —(CH2)kR5(CH2)1- wherein K and 1 are each 0 or an integer of 1 or above provided k+1 is an integer of not more than 10; and R5 represents a single bond, —CH?CH—, —OCH2—, carbonyl or —CH(OH)—; provided that at least one of A1, A3 and A4 is a group represented by the above formula (a); A2 represents C1-5 alkyl, C1-5 alkoxy, C1-5 alkenyl, C1-5 hydroxyalkyl or C1-5 carbonylalkyl; and n, p, q and r are each an integer of 0, 1 or 2.

Abstract: The present invention provides an azulene derivative and a salt thereof, wherein an azulene ring is bonded to a benzene ring directly or via a lower alkylene which may be substituted with a halogen atom and the benzene ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes-related diseases such as insulin-resistant diseases and obesity.

Abstract: An isoquinuclidine derivative represented by the following general formula (I): (I) [wherein A1 is methylene or carbonyl]: R1 is hydrogen or methyl: R2 is —(CH2)n-A2-Ph (n is an integer of 0 to 3 and A2 is a single bond or —O—): and R3 is —COOH, —COOR4, —COSR4 (R4 is lower alkyl, unsubstituted phenyl, or phenyl substituted by a lower alkyl, lower alkoxy, hydroxyl, methoxycarbonyl, ethoxycarbonyl, or trifluoromethanesulfonamide group or by a halogen atom), etc.] or a pharmaceutically acceptable salt of the compound. Also provided is an oral remedy for diabetes, which contains the compound and has hypoglycemic activity.

Abstract: The purposes of this invention are preparation of the non-mucin type synthetic compounds-carrier conjugated compounds which are stable against enzymes, and which have the ability of specific reactivity to induce immune response for cancer and HIV. A compound of the general formula (1), wherein A represents OH or sialic acid and/or it's derivatives, and B represents OH or galactose and/or it's derivatives; T represents H or protecting groups of amine; M represents H or OH; X represents oxygen atom, —NH— or S(O)z (where z is 0, 1 or 2); Q is H or oxygen atom; V represents lower alkyl or H; W is straight or branched alkylene groups from 0 to 5; Z is straight or branched alkylene groups from 1 to 5; i, m, and t is 0 or 1; non-mucin type synthetic compounds or it's carrier conjugated compounds, which have above mentioned compounds as a core structure of antigen.

Abstract: An isoquinuclidine derivative represented by the following general formula (I): (I) [wherein A1 is methylene or carbonyl]: R1 is hydrogen or methyl: R2 is —(CH2)n-A2-Ph (n is an integer of 0 to 3 and A2 is a single bond or —O—): and R3 is —COOH, —COOR4, —COSR4 (R4 is lower alkyl, unsubstituted phenyl, or phenyl substituted by a lower alkyl, lower alkoxy, hydroxyl, methoxycarbonyl, ethoxycarbonyl, or trifluoromethanesulfonamide group or by a halogen atom), etc.] or a pharmaceutically acceptable salt of the compound. Also provided is an oral remedy for diabetes, which contains the compound and has hypoglycemic activity.

Abstract: The present invention is a compound of general formula (I) or a pharmaceutically acceptable salt of, wherein W represents carbon chain from 9 to 17 which containing double bond or hydroxy group occasionally; X represents carbon chain from 11 to 25 which containing double bond or hydroxy group occasionally; Y represents —(CH2)a—CH═CH—(CH2)a′—, —(CH2)a— (a, a′ denotes an integer of 0-5 and a+a′ is 5 and under.), —S(O)0-2CH2—, —NHCH2—; Z represents —CO—, —SO2—; R represents —CH2OH, CO2H, CH2OCH2CO2SO3H; R0 represents —OH, —NH2, —NHAc.

Abstract: C-glycoside derivatives are disclosed, which are represented by the following formula (I) and its pharmaceutical acceptable salt, and which are useful for the treatment and/or prevention of diabetes and hypoglycemia. wherein: with the provisos that R1 is H, OH, lower alkyl, O-lower alkyl or R2 is H, —COO-lower alkyl, R5 is —CH2OH, —CH2OCO2-lower alkyl, —CH2OSO3H, —COOH or —COONa; wherein: A is (with the provisos that X is oxygen atom, nitrogen atom or sulfur atom R3 is lower alkyl when m=0, and is lower alkyl, —OH or —O-lower alkyl when m=1, . . . means saturated or unsaturated carbon bond; m is 0 or 1; n is 0, 1 or 2; above mentioned-lower alkyl means C1-C5.) or a pharmaceutical acceptable salt.