Abstract: Indene-1-acetamide compounds of the general formula (I) below; inhibit sPLA2 mediated release of fatty acids and are useful for treatment of conditions such as septic shock.

Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.

Abstract: A compound of the formula (I): wherein for example, a compound below: wherein R1 is CH3, H or Na; and X1-X2-X3 is or its salt or a hydrate thereof is useful as PGD2 antagonist and can be used as a drug for treating diseases in which mast cell dysfunction is involved, for example, systemic mastocytosis and disorder of systemic mast cell activation, and also tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, injury due to ischemic reperfusion, and as an anti-inflammatory agent. It is particularly useful in the treatment of nasal occlusion.

Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.

Abstract: A compound represented by the formula (I): ##STR1## wherein, for example, R.sup.1 is optionally substituted aralkyl, Z is nitrogen atom which optionally substituted with alkyl, X.sup.1 is --CH.sub.2 NHCO--, X.sup.2 is phenylene, X.sup.3 is a bond, Y.sup.2 is optionally substituted aryl, B is oxygen atom, its pharmaceutically acceptable salt, or hydrate thereof and a pharmaceutical composition which contains them as an active ingredient.

Abstract: A method of producing an ether-type thio-phospholipid of the formula (I): ##STR1## wherein: n is an integer of 13 to 17;A is C.sub.14 -C.sub.20 acyl group;G is a group selected from the group consisting of: ##STR2## which is useful as synthetic substrate of cytosolic phospholipase A.sub.2 inhibitors, said method being applicable to mass production of the compound (I), intermediates therefor and the preparation of the same are provided.

Abstract: A compound of the formula I: ##STR1## or a pharmaceutically acceptable salt or a hydrate thereof, which has the activity of inhibiting the production of prostaglandin E.sub.2 by inhibiting cytosolic phospholipase.sub.2.

Abstract: The present invention relates to a compound represented by the formula: ##STR1## wherein a and b are each a carbon atom; a bond:- - - - -between a and b indicates that it is a single bond or a double bond;X is a hydrogen atom, an optionally substituted aryl group, an optionally substitued heteroaryl group, or an optionally substituted aralkyl group;Y is a hydrogen atom, an optionally substituted aryl group, an optionally substituted aralkyl group, or a carboxyl group or related functional groups thereof; andZ is a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted aralkyl, an optionally substituted arylalkenyl group, an optionally substituted heteroarylalkyl group, an optionally substituted heteroarylalkenyl group, an optionally substituted aryloxyalkyl group, an optionally substituted aralkyloxyalkyl group, an optionally substituted arylcarbonylalkyl group, an optionally substituted arylsulfonylalky

Abstract: A process for preparing an optically active 1,4-bridged-cyclohexane carboxylic acid derivatives which are clinically important thromboxane A.sub.2 thromboxane of formula (IV): ##STR1## wherein, R is phenyl or phenyl substituted with hydroxy, lower alkoxy, halogen, or lower alkyl; Y is oxygen, methylene, substituted methylene; m is 0 or 1; n is 0, 1 or 2; q is 3 or 4 with the proviso that when m is 1, n is 0 or 1 from an optically active norbornyl amine derivative.

Abstract: A method of producing an ether-type thio-phospholipid of the formula (I): ##STR1## wherein: n is an integer of 13 to 17;A is C.sub.14 -C.sub.20 acyl group;G is a group selected from the group consisting of: ##STR2## which is useful as synthetic substrate of cytosolic phospholipase A.sub.2 inhibitors, said method being applicable to mass production of the compound (I), intermediates therefor and the preparation of the same are provided.

Abstract: A method of producing an ether-type thio-phospholipid of the formula (I): ##STR1## wherein: n is an integer of 13 to 17;A is C.sub.14 -C.sub.20 acyl group;G is a group selected from the group consisting of: ##STR2## which is useful as synthetic substrate of cytosolic phospholipase A.sub.2 inhibitors, said method being applicable to mass production of the compound (I), intermediates therefor and the preparation of the same are provided.

Abstract: The present invention relates to the new thielocin derivatives, which exhibit phospholipase A.sub.2 inhibitory activity of the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are independently hydrogen, lower alkyl, lower alkoxy, hydroxy, or halogen;E.sub.1 and E.sub.2 are independently hydrogen, or an ester residue;m and n are independently an integer of 0 to 4;--Y-- is a bivalent group which is selected from the group consisiting of the following radicals: ##STR2## or the salts thereof.

Abstract: A method for reduction of an allyl alcohol-type compound, specific to its allylic hydroxyl group, being carried out without any side reactions such as reduction of other portions of the compound or allylic rearrangement, which comprises treating the compound with trialkylsilane in the presence of AlX.sub.3, wherein X refers to a halogen atom.

Abstract: A novel hydroxamic acid compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof having cell growth inhibition, vascularization inhibition activities and the like.The compounds of the present invention possess inhibitory activities against the growth of vascular endothelial cells and the expression of lymphocyte adhesive factors and the detransforming activity of cells transformed by ras gene, and inhibit the cell growth and are effective on inflammation and tumor.

Abstract: Novel carboxylate derivatives exhibiting phospholipase A.sub.2 inhibitory activity are disclosed, Specifically, the following compounds of the formula and pharmaceutically acceptable salts thereof are disclosed: ##STR1## wherein A is hydroxy, amino, or lower alkylamino; R.sup.1 to R.sup.12 are independently hydrogen, methyl, methoxy, or hydroxy, provided that all of R.sup.1 to R.sup.12 are not hydrogen; G.sup.1 is a single bond, or a group of --(CH.sub.2).sub.x O(CH.sub.2).sub.y -- wherein x and y are independently 0-5; G.sup.2 is a single bond, oxygen, sulfur, carbonyl, etc.; G.sup.3 is alkyl, aryl, or a group of the formula: ##STR2## wherein R.sup.13 and R.sup.14 are independently hydrogen, alkyl, aryl, etc.; or R.sup.13 and R.sup.14 may be taken together with the adjacent nitrogen atom to form a heterocyclic group or a group of the formula: ##STR3## wherein Z is a carbon atom or a nitrogen atom, J, K, and L are independently hydrogen or aryl, etc.

Abstract: Optically active mono-esters of dicarboxylic acid of the formula III: ##STR1## being useful as intermediates for preparing optically active natural products or medicines; asymmetric synthesis process for preparing thereof being characterized by the reaction of an acid anhydride with an (R)- or (S)-arylacetic acid derivative; and the key substances therefor are also claimed.

Abstract: A process suitable for industrially preparing 2,3-trans-1,4-bridged cyclohexane sulfonamide derivatives, especially useful as an intermediate for the synthesis of a trans bicyclo[2,2,1] heptane carboxylic acid derivative, a clinically important thromboxane A.sub.2 antagonist, comprising: allowing to react corresponding a cis/trans mixture of sulfonamide derivatives with an anionoid or water-soluble carbonyl reagent at pH 3-7 so that the trans isomer may form a water-soluble adduct with the anionoid or carbonyl reagent, separating the resulting adduct dissolved in an aqueous layer, and recovering the trans isomer by treating the adduct with a base or an acid. Also provided is an alkali metal hydrogen sulfite adduct of 2,3-trans 1,4-bridged cyclohexane sulfonamide derivative.

Abstract: Optically active mono-esters of dicarboxylic acid of the formula III: ##STR1## being useful as intermediates for preparing optically active natural products or medicines; asymmetric synthesis process for preparing thereof being characterized by the reaction of an acid anhydride with an (R)- or (S)-arylacetic acid derivative; and the key substances therefor are also claimed.

Abstract: Optically active mono-esters of dicarboxylic acid of the formula III: ##STR1## being useful as intermediates for preparing optically active natural products or medicines; asymmetric synthesis process for preparing thereof being characterized by the reaction of an acid anhydride with an (R)- or (S)-arylacetic acid derivative; and the key substances therefor are also claimed.

Abstract: Sulfonylamino substituted bicyclyl hydroxamic acid derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is hydrogen or lower alkyl; R.sup.3 is hydrogen, lower alkyl, lower alkoxy, hydroxy or halogen; X is alkylene or alkenylene: Y is methylene or oxygen; and n is 0, 1, or 2, or the pharmaceutically acceptable salt thereof. These compounds have an advanced antagonistic activity to thromboxane A.sub.2 (TXA.sub.2)-receptor and are useful for the treatment of thrombosis, vasoconstriction, or bronchoconstriction, and the like disease which are induced by TXA.sub.2.