Abstract: This invention relates to compounds (I) or pharmaceutically acceptable salts thereof, having a function to inhibit type IV phosphodiesterase (PDE) ##STR1## [X: an oxygen atom or a sulfur atom, R.sup.1 : a lower alkyl group, a cycloalkyl-lower alkyl group or a cycloalkyl group,R.sup.2 : a hydrogen atom, a halogen atom, a lower alkyl group, a halogeno-lower alkyl group, a hydroxy-lower alkyl group, a mercapto-lower alkyl group, a lower alkoxy-lower alkyl group, a lower alkylthio-lower alkyl group, a lower alkanoyloxy-lower alkyl group, a lower alkanoylthio-lower alkyl group, a lower alkanoyl-lower alkyl group, a hydroxyimino-lower alkyl group, a lower alkoxyimino-lower alkyl group, a cycloalkyl group, an aryl group or a lower alkanoyl group,R.sup.3 : a hydrogen atom, a halogen atom or a lower alkyl group,R.sup.4 : a hydrogen atom or a lower alkyl group,R.sup.

Abstract: Neuroprotective agents based on inhibition of kainic acid neurotoxicity and compounds useful as neuroprotective agents based on inhibition of kainic acid neurotoxicity. An inhibitors of kainic acid neurotoxicity, comprising as an active ingredient a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof, and a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein symbols in the formula have the following respective meanings: the ring A: a pyridine ring; ##STR2## R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 may be the same or different and each represent a hydrogen atom or a lower alkyl, cycloalkyl, alkenyl, aryl, carboxyl or lower alkoxycarbonyl group which may have substituent(s), or are not present, with the proviso that R.sup.2 and R.sup.

Abstract: Imidazole-substituted quinoxalinedione derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof and pharmaceutical compositions useful as glutamate receptor antagonists and the like, which comprise said compounds or salts thereof and pharmaceutically acceptable carriers. ##STR1## (Each symbol in the formula has the following meaning: A: a group represented by a formula (CH.sub.2).sub.m or a group represented by a formula Ph--(CH.sub.2).sub.p (Ph: a phenyl group),X: an oxygen atom or a group represented by a formula NR.sup.4,R.sup.1 : a hydrogen atom, a hydroxyl group or a triazolyl group, with the proviso that X may be a bond when R.sup.1 is a triazolyl group,R.sup.2 : a hydrogen atom, a nitro group, a halogeno-lower alkyl group, a cyano group, an amino group, a mono- or di-lower alkylamino group or a halogen atom,R.sup.3 and R.sup.

Abstract: A 1,2,3,4-tetrahydroquinoxalinedione derivative represented by the following formula (I) or salt thereof, an NMDA-glycine receptor and/or AMPA receptor antagonist or kainic acid neurotoxicity inhibitor containing the derivative or salt. In addition, a pharmaceutical composition comprising said compound and a pharmaceutically acceptable carrier: ##STR1## wherein the substituents are as described in the specification.

Abstract: Thiophene derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof. Said compounds act as an anti-PCP agonist and therefore are useful as psychotropic or antischizophrenic agents and so on. ##STR1## (In the above formula, R.sub.1 is a formula --A.sub.1 --X.sub.1 --R.sub.3 ; R.sub.2 is a formula --A.sub.2 --X.sub.2 --R.sub.4 or does not exist; B ring is a 7- to 10-membered nitrogen-containing cycloalkyl ring; Ar ring is an aryl or heteroaryl ring; A.sub.1, A.sub.2 and A.sub.3 may be the same or different from one another and each represents a bond or a lower alkylene group; X.sub.1 and X.sub.2 may be the same or different from each other and each represents a bond or a formula --O--, --S--or the like; R.sub.3 and R.sub.

Abstract: Novel arylethenesulfonamide derivative having a high affinity for drugs, especially endoserine receptors, and represented by general formula (I); pharmaceutically acceptable salts thereof; and drugs comprising the same as the active ingredient, especially endoserine receptor antagonist, whereinAr: optionally substituted aryl group or optionally substituted five- to six-membered heteroaryl group;X: oxygen atom, sulfur atom or a group represented by a formula --NH--;Y: oxygen atom or sulfur atom;R.sub.1 : hydrogen atom, optionally halogen-substituted lower alkyl group, cycloalkyl group, optionally substituted aryl group or optionally substituted five- to six-membered heteroaryl group.R.sub.2 : lower alkyl group, lower alkenyl group or lower alkynyl group where each of which may be substituted with one to three substituent(s) selected from a group consisting of hydroxyl group, lower alkoxy group, cycloalkyl group, halogen atom, carboxyl group and lower alkoxycarbonyl group;R.sub.

Abstract: A substituted-amidinobenzene derivative of the following general formula (I) or a salt thereof, and a pharmaceutical composition comprising said derivative or a salt thereof and a pharmaceutically acceptable carrier. ##STR1## (the symbols in the above formula have the following meanings: R.sup.1 : a group which can be converted into an amidino group in vivo;R.sup.2 and R.sup.3 : the same or different and each represents a carboxyl group or a group which can be converted into a carboxyl group in vivo;X.sup.1 and X.sup.2 : the same or different and each represents a lower alkylene group;m: 0, 1 or 2;n: 0 or 1, provided that n=1 when m=0.They have GPIIb/IIIa receptor antagonizing activity and are useful as medicines for ameliorating ischemic cardiac disorders, adminicula in cardiosurgery operations or in vascular surgery operations, medicines for ameliorating cerebrovascular disorders, And medicines for ameliorating peripheral artery disorders.

Abstract: An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle. ##STR1## (The symbols in the formula have the following meanings. (whereinA: heteroarylene;X: bond, O, S, --NR.sup.5 --, --NR.sup.5 CO--, --NR.sup.5 CONH--, --NR.sup.5 SO.sub.2 -- or --NR.sup.5 C(.dbd.NH)NH--;R.sup.1 : --H, -optionally substituted lower alkyl, -optionally substituted aryl, -optionally substituted heteroaryl or -optionally substituted cycloalkyl;R.sup.2a, R.sup.2b : --H or -lower alkyl, which may be the same or different;R.sup.3 : --H or -lower alkyl;R.sup.4a, R.sup.4b : --H or --OH, which may be the same different, or R.sup.4a and R.sup.4b are taken together to form .dbd.O or .dbd.N.about.O-lower alkyl; andR.sup.5 : --H or -lower alkyl.

Abstract: Quinuclidine derivatives represented by general following general formula (I), salts, N-oxides or quaternary ammonium salts thereof, and medicinal compositions containing the same. ##STR1## The compound has an antagonistic effect on muscarinic M.sub.3 receptors and is useful as a preventive or remedy for urologic diseases, respiratory diseases or digestive diseases.

Abstract: An azole derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof, having both of a leukotriene antagonistic effect and a thromboxane A2 antagonistic effect and being useful in preventing or treating allergic diseases, ischemic heart diseases or ischemic brain diseases, and a medicinal composition containing the same as the active ingredient, wherein R.sup.1 and R.sup.2 may be the same or different and represent each hydrogen, cycloalkyl, etc., or R.sup.1 and R.sup.2 together with (a) may form a fused ring (b) or (c) which may be substituted by optionally substituted lower alkyl, amino, etc.; R.sup.3, R.sup.6, R.sup.7, R.sup.8 may be the same or different and represent each hydrogen, amino, etc.; R.sup.4 represents cyano, tetrazolyl, --COOR.sup.9, etc.; R.sup.5 represents hydrogen or lower alkyl; D represents optionally substituted lower alkylene; X and Z may be the same or different and represent each oxygen or sulfur; Y represents --N.dbd. or --CH.dbd.

Abstract: A benzodiazepine derivative of formula (I), or a pharmaceutically acceptable salt thereof, wherein (a) R.sup.1 is --CH.sub.2 CHOH(CH.sub.2).sub.a R.sup.4 or a ketone group --CH.sub.2 CO(CH.sub.2).sub.a R.sup.5 in which a is 0 or 1 and R.sup.4 and R.sup.5 are selected from alkyl and cycloalkyl groups and saturated heterocyclic groups optionally substituted at a hetero-atom; (b) R.sup.2 and R.sup.3 are independently selected from aromatic carbocyclic and heterocylic residues; and (c) W and X are selected independently from halogen and hydrogen atoms and alkyl and alkoxy groups. These compounds are gastrin and/or CCK-B receptor antagonists.

Abstract: A mixed feed or a feed additive, which comprises Cucurbita Seed, Plantago and Lornicera.Other crude drugs such as Safflower, Licorice, Mabiacao, Pugongying, Houttuynia and Juhua may be compounded in addition to the above crude drugs.For breeding cattle, swine, fowl, Hamachi, and the like, the above-described mixed feed, or the feed additive compounded with the marketed feed may be used.The resistance to diseases of the fed animals is improved, healthy candicidin can be maintained during the breeding, and the meat quality, egg quality, or the like is improved.

Abstract: An amidinonaphthyl derivative represented by the following general formula (I) which has coagulation factor X inhibiting action and is useful as an anti-thrombus agent and the like, a salt thereof, an intermediate thereof and a pharmaceutical composition which comprises the amidinonaphthyl derivative. An amidinonaphthyl derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof. ##STR1## (symbols in the formula have the following meanings; R.sup.1 : a hydrogen atom or a group represented by the formula --A--W--R.sup.4,A: a group represented by the formula ##STR2## a group represented by the formula ##STR3## or a group represented by the formula --SO.sub.2 --, X: an oxygen atom or a sulfur atom, W: a single bond or a group represented by the formula --NR.sup.5 --, R.sup.4 : a hydroxyl group, a lower alkoxy group, etc., R.sup.5 : a hydrogen atom, a carbamoyl group, a lower alkoxycarbonyl group, etc., R.sup.2 : a lower alkyl group, R.sup.

Abstract: This invention relates to nitrogen-containing aromatic 5-membered ring-condensed benzazepine derivatives represented by the general formula (I) ##STR1## (symbols in the formula have the following meanings; ring B: a nitrogen-containing aromatic 5-membered ring having at least 1 nitrogen atom and optionally one oxygen or sulfur atom, which may optionally have substituent(s), R.sup.1 and R.sup.2 : these may be the same or different from each other and each represents a hydrogen atom, a halogen atom, a lower alkyl group, an amino group which may optionally be substituted by lower alkyl group(s), or a lower alkoxy group,A: a single bond; a group represented by the formula --NHCO--(CR.sup.3 R.sup.4).sub.n --,n: 0 or an integer of from 1 to 3,R.sup.3 and R.sup.4 : these may be the same or different from each other and each represents a hydrogen atom, a lower alkyl group (provided that R.sup.3 and R.sup.

Abstract: A 5-HT.sub.3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): ##STR1## wherein the A ring is substituted or unsubstituted and represents a benzene or a heterocyclic ring with one or two heteroatoms;one of L.sub.1 or L.sub.

Abstract: A serine derivative represented by the general formula (I) ##STR1## (symbols in the formula represent the following meanings; X: a sulfur atom or an oxygen atom,Y: a nitrogen atom or CH,R.sup.1 and R.sup.2 : the same or different from each other and each represents a hydrogen atom, a lower alkyl group or a protecting group for the amino group, or R.sup.1 and R.sup.2 may be combined together to form a four- to nine-membered nitrogen-containing cycloalkyl group,R.sup.3 : a hydrogen atom, a carboxyl group, a protected carboxyl group, an aralkyl group, or a lower alkyl group unsubstituted or substituted with a hydroxyl group,R.sup.4 : a hydrogen atom or a hydroxyl group,R.sup.

Abstract: A quinuclidine derivative represented by the following general formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, which has strong squalene synthase inhibiting activity and is useful as a cholesterol lowering agent without causing side effects. ##STR1## (Symbols in the formula represent the following meanings; R.sub.1 : a hydrogen atom, a halogen atom or a lower alkyl group,R.sub.2 : a hydrogen atom, a hydroxyl group or a lower alkoxy group,. . : a single bond or a double bond, with the proviso thatR.sub.2 does not exist when . . . is a double bond,X and Y: the same or different from each other and each represents a bond, an oxygen atom (--O--), a carbonyl group (--CO--), a group represented by the formula --S(O).sub.p -- or a group represented by the formula --NR.sub.3 --,p: 0, 1 or 2,R.sub.3 : a hydrogen atom or a lower alkyl group which may have a substituent,A: a saturated or unsaturated lower alkylene group, a group of the formula --(CH.sub.2).sub.m Z(CH.sub.

Abstract: A bone-forming graft that includes a bone morphogenetic protein (BMP) carried on a composite porous body. The composite porous body has a porous frame of a bioabsorbable hydrophilic material and a surface layer of a bioabsorbable polymer material. In particular, the present invention relates to a bone-forming graft in which the bioabsorbable hydrophilic material is one or more compounds selected from a group consisting of gelatin, hyaluronic acid, a hyaluronic acid derivative, collagen, a collagen derivative, chitosan, a chitosan derivative, and triethanolamine alginate. The bioabsorbable polymeric material is one or more compounds selected from a group consisting of a polylactic acid, a copolymer of a polylactic acid and a polyglycolic acid, and a copolymer of poly?bis(p-carboxyphenoxy)propane!anhydride and sebacic acid. The graft has excellent formability and workability and has an internal structure suitable for in vivo bone formation.

Abstract: 1,8-Naphthyridine derivatives represented by the following general formula (I), salts thereof, hydrates thereof and solvates thereof. ##STR1## They have an activity to inhibit type IV phosphodiesterase and are useful as agents for the prevention and treatment of respiratory diseases, inflammatory diseases accompanying organ transplantation, systemic or local arthropathy, proliferative diseases, micturition-related diseases and diseases in which tumor necrosis factor (TNF) and other cytokine (IL-1, IL-6 or the like) are concerned.

Abstract: An azole derivative represented by the following general formula (I) ##STR1## (symbols in the formula have the following meanings; R.sup.1 and R.sup.2 : the same or different from each other and each represents a hydrogen atom, a lower alkyl group or a phenyl group which may be substituted with a halogen atom,A, B and D: the same or different from one another and each represents a group represented by the formula ##STR2## or a nitrogen atom,X and Y: the same or different from each other and each represents a single bond, a methylene group, an oxygen atom,a group represented by a formula S(O).sub.n, or a group represented by the formula ##STR3## R.sup.3 and R.sup.4 : the same or different from each other and each represents a hydrogen atom or a lower alkyl group, andn: 0, 1 or 2),a salt thereof, a hydrate thereof or a solvate thereof.