Abstract: The present invention relates to a racemic or enantiomerically enriched O-carbamoyl-phenylalaninol compound represented by the following structural formula V and pharmaceutically acceptable salts thereof to treat diseases of the central nervous system: ##STR1## wherein Ph is a phenyl group as described as follows: ##STR2## wherein R is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms, and x is an integer from 1 to 3, with the proviso that R is the same or different when x is 2 or 3, R.sup.1 and R.sup.2 may be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cyclic propyl and 5 to 7-membered aliphatic cyclic compounds, and R.sup.1 and R.sup.

Abstract: The present invention relates to a novel selective thrombin inhibitor having the following formula (I), which is also effective by oral administration: ##STR1## in which R.sup.1 represents acetyl substituted with aryl or aryloxy, or represents sulfonyl substituted with substituted or unsubstituted aryl or N-containing heterocyclic group,X represents a group of formula ##STR2## R.sup.2 and R.sup.3 independently of one another represent hydrogen; cycloalkyl substituted or unsubstituted with carboxyl or alkoxycarbonyl; arylalkyloxy; hydroxy; or lower alkyl substituted or unsubstituted with carboxyl, alkoxycarbonyl or hydroxy, orR.sup.2 and R.sup.3 together with nitrogen atom to which they are attached can form a piperidine group substituted with carboxyl or alkoxycarbonyl,R.sup.4 represents hydrogen, lower alkyl or lower alkoxy,R.sup.

Abstract: N-Acyl-.alpha.-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R' to R"' and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion. They are manufactured by cleaving off protecting groups in corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.

Abstract: A benzene derivative of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NH.sub.2, --NHR.sup.21 ; R.sup.2 is hydroxyl, --OR.sup.22, three- to seven-membered saturated cycloaliphatic amino optionally interrupted by one or more nitrogen, oxygen or sulfur atoms, --NHR.sup.23, --N(R.sup.24).sub.2, --NH.sub.2 ; R.sup.4 is hydrogen, C.sub.1-6 -alkyl, or --C(.dbd.O)R.sup.25 ; R.sup.7 is --CO--, --SO.sub.2 --; R.sup.8 is --CO--, single bond; R.sup.12 is --R.sup.11 --R.sup.5 ; R.sup.11 is --N(R.sup.5)--, --NH--, --O--, --N(R.sup.26)--, --N(C(.dbd.O)R.sup.27)--, --N(C(.dbd.O)NH.sub.2)--, --N(C(.dbd.O)NHR.sup.28)--; R.sup.13 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NHC(.dbd.O)(CH.sub.2).sub.m C.sub.6 H.sub.5, --NHC(.dbd.O)R.sup.29, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --NH.sub.2, --NHR.sup.30, --(CH.sub.2).sub.n C.sub.6 H.sub.5 ; Z is C, CH, N; A is CH, N; R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.

Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.

Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of their use.

Abstract: The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, and for use in multi-drug resistant cancer therapy.

Abstract: The present invention provides an anthranilic acid derivative having a cGMP-PDE inhibitory activity.An anthranilic acid derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## ?wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, a nitro group, a hydroxyalkyl group, a cyano group or the like; R.sup.5 and R.sup.6 represent the same or different from each other, a hydrogen atom, a halogen atom, a hydroxy group, a cyano group, an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group or the like;W represents a group of the formula: --N.dbd. or --CH.dbd.; R.sup.7 and R.sup.

Abstract: The invention relates to a process for the production of UV-stable polycarbonates, to the polycarbonates obtainable in accordance with the invention and to their use for the production of sheets, more particularly plastic panels.

Abstract: The present invention relates to a 2,3-diaminopropionic acid derivative of the formula (1): ##STR1## or a pharmaceutically acceptable salt thereof. The compounds of the present invention are useful as a platelet aggregation inhibitor, a cancer metastasis inhibitor, a wound healing agent or a bone resorption inhibitor.

Abstract: The present invention relates to O-carbamoyl-(D)-phenylalaninol compound represented by the following structural formula V and pharmaceutically acceptable salts thereof to treat diseases of the central nervous system: ##STR1## wherein R.sup.1 and R.sup.2 may be the same with or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl containing 1 to 8 carbon atoms, and 5 to 7-membered aliphatic cyclic compounds which may comprise not more than two nitrogen or oxygen atoms directly unconnected, the total number of carbon atom of R.sup.1 and R.sup.2 ranging from 0 to 16.

Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: A benzene derivative of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NH.sub.2, --NHR.sup.21 ; R.sup.2 is hydroxyl, --OR.sup.22, three- to seven-membered saturated cycloaliphatic amino optionally interrupted by one or more nitrogen, oxygen or sulfur atoms, --NHR.sup.23, --N(R.sup.24).sub.2, --NH.sub.2 ; R.sup.4 is hydrogen, C.sub.1-6 -alkyl, or --C(.dbd.O)R.sup.25 ; R.sup.7 is --CO--, --SO.sub.2 --; R.sup.8 is --CO--, single bond; R.sup.12 is --R.sup.11 --R.sup.5 ; R.sup.11 is --N(R.sup.5)--, --NH--, --O--, --N(R.sup.26)--, --N(C(.dbd.O)R.sup.27)--, --N(C(.dbd.O)NH.sub.2)--, --N(C(.dbd.O)NHR.sup.28)--; R.sup.13 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -haloalkyl, --NHC(.dbd.O)(CH.sub.2).sub.m C.sub.6 H.sub.5, --NHC(.dbd.O)R.sup.29, --NHC(.dbd.O)CH(C.sub.6 H.sub.5).sub.2, --NH.sub.2, --NHR.sup.30, --(CH.sub.2).sub.n C.sub.6 H.sub.5 ; Z is C, CH, N; A is CH, N; R.sup.5 is hydrogen, --CH.sub.2 C.sub.6 H.sub.4 COOH, --CH.sub.2 C.sub.6 H.sub.4 COOR.sup.31, --CH.

Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.

Abstract: This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl;R.sup.1 is alkyl;R.sup.2 represents alkyl from 1 to 5 carbon atoms, aryl or aryl substituted with halogen or alkyl from 1 to 5 carbon atoms;R.sup.6 is alkyl;n is 1 to 5;p is 0 to 6;x is 0 or 2; andR.sup.4 and R.sup.5 are independently hydrogen or alkyl or together with N form a cycloalkylamine. The compounds of Formula I are leukotriene B.sub.4 antagonists and are useful as anti-inflammatory agents and in treating disease conditions mediated by LTB.sub.4.

Abstract: Novel .alpha.-mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein the substituents are as defined in the specification.

Abstract: A cyanoketone derivatives of the following formula (1) ##STR1## which are characterized by excellent herbicidal activity and effectiveness against a variety of broad leafed weeds, including barnyard grass, green foxtail, velvet leaf, livid amaranth and hairy beggar ticks.

Abstract: The present invention is directed to compounds of the formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5, R.sup.6, R.sup.7, R.sup.8, m, n and X are defined herein, and pharmaceutically acceptable salts thereof, which are useful as tachykinin antagonists.

Abstract: A process for preparing a compound of the formula (I): ##STR1## in which, R.sup.1 and R.sup.2 each represents hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocycle; E represents methylene, sulfur, oxygen or imino group optionally substituted with C.sub.1 -C.sub.6 alkyl or aralkyl; ring A is aryl or heteroaryl ring, optionally substituted; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen or R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(.dbd.Y)-- (IV)(wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen, up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygen); provided that when E represents a methylene group, then R.sup.3 is a C.sub.1 -C.sub.6 alkyl group or R.sup.3 and R.sup.

Abstract: 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalized carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.

Abstract: The invention relates to the compounds of formula (I) wherein the C(.dbd.NH)--NHR.sub.3 group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which: R.sub.1 is amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen; R.sub.2 is hydroxy which is etherified by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy; R.sub.3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid; X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); and X.sub.2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical.

Abstract: A novel asymmetric synthesis is provided for preparing optically active amides of formula (A) and their salts. ##STR1## In the formula, X represent --N-- or --CH--, R represents a mono or bicyclic aryl or heteroaryl group, R.sup.1 is an aryl or heteroaryl radical, and R.sup.2 and R.sup.3 have specified meanings. The products are useful as 5-HT.sub.1A antagonists.Novel diesters of formula D useful as intermediates in the process are also disclosed.

Abstract: Disclosed herein are cyanoketone derivatives of the following formula (1) ##STR1## such as 1-cyano-1-piperidinocarbonyl-3-[4-(2-chloro-4-trifluoromethylphenoxy)pheno xy]-2-butanone, 1-cyano-1-piperidinocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-pyridyloxy )phenoxy]-2-butanone, 1-cyano-1-(N-methyl-N-dichlorophenyl)aminocarbonyl-3-[4-(2-quinoxalyloxy)p henoxy]-2-butanone, 1-cyano-1-(N,N-dibutyl)aminocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-py ridyloxy)phenoxy-2-butanone, and the like, which are characterized by excellent herbicidal activity and effectiveness against a variety of gramineous weeds.

Abstract: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.

Abstract: Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.

Abstract: This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.

Abstract: N-Acylpiperidines of general structure ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.

Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV Protease.

Abstract: The present invention provides a process for producing a variety of unsaturated carbamic acid derivatives from corresponding unsaturated carbamates by substitution reaction. The present invention provides a process for producing unsaturated carbamic acid derivatives, comprising reacting an unsaturated carbamate represented by ##STR1## wherein R represents a hydrogen atom or an alkyl group having 1 to 8 carbon atoms, R.sup.1 represents a residue of an alcohol from which an OH group is removed,with an alcohol, a primary or secondary amine or an oxime at a temperature of 80.degree. to 150.degree. C. to substitute the --OR.sup.1 group in the formula (A).

Abstract: The compounds of the formula: ##STR1## in which X is ##STR2## where R.sup.7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.9 is hydrogen, alkyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl; R.sup.10 is hydrogen, alkyl or gemdialkyl; n is one of the integers 0, 1 or 2; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl, alkoxycarbonyl or hydroxycarbonyl; and when X is --NR.sup.9 -- or R.sup.7 is an amino alkyl group, a pharmaceutically acceptable salt thereof; are useful as inhibitors of cholesterol ester hydrolase.

Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.

Abstract: The invention relates to amidinophenylalanine derivatives, to the synthesis of these compounds, to their use and to pharmaceutical compositions which contain these compounds which act as thrombin inhibitors.

Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.

Abstract: Urea-substituted benzoylguanidines, process for their preparation, their use as pharmaceutical or diagnostic, and pharmaceutical containing themThere are described benzoylguanidines of the formula I ##STR1## where R(1), R(3) or R(4) is --NR(6) C.dbd.X NR(7)R(8); X is oxygen, sulfur, R(6), R(7) and R(8) are H, (perfluoro)alk(en)yl, where R(7) and R(8) can also together be 4 or 5 methylene groups,the substituents R(1) to R(5) remaining in each case are H, Hal, (fluoro) alk(en)yl, CN, NO.sub.2, NR(16)R(17).

Abstract: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.

Abstract: The present invention relates to 3,4,5,6-tetrahydrophthalamide derivatives and 3,4,5,6-tetrahydroisophthalimide derivatives having excellent effects as effective active ingredients of herbicides, and processes for preparing the same, and provides the compounds having a more efficient herbicidal activity, and efficient and industrial processes for the preparation thereof.More specifically, the tetrahydrophthalimide derivative obtained by reacting a halogen-substituted 5-cycloalkyloxyaniline derivative with a 3,4,5,6-tetrahydrophthalic anhydride, or the tetrahydroisophthalimide derivative of the present invention is reacted with various types of amines to prepare a tetrahydrophthalamide derivative represented by the general formula (I): ##STR1## These tetrahydrophthalamide derivatives and the tetrahydroisophthalimide derivatives exhibit excellent herbicidal activities in the soil treatment in the paddy field and field and the stem-foliar treatment.

Abstract: The invention relates to novel S-nitroso derivatives of ACE inhibitors and to pharmaceutical compositions comprising the S-nitrosothiol derivatives of the invention together with a pharmaceutically acceptable carrier.The invention also relates to methods for treating various pathophysiological conditions including acute myocardial infarction, left ventricular dysfunction without overt heart failure, hypertension, pulmonary hypertension, congestive heart failure, angina pectoris, vascular thrombosis, Raynauds syndrome, scleroderma, toxemia of pregnancy, acute renal failure, diabetic nephropathy, and renal artery stenosis, and to methods of inhibiting ACE and effecting vasodilation comprising administering the S-nitrosothiol derivatives of the ACE inhibitors of the invention to an animal.

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: Isoxazole-4-carboxamides and hydroxyalkylidenecyanoacetamides, pharmaceuticals containing these compounds and their useIsoxazole-4-carboxamide derivatives and hydroxyalkylidene-cyanoacetamide derivatives are suitable for the treatment of carcinoses. These compounds can be prepared by known processes. Some of the compounds are novel and are additionally suitable for the treatment of rheumatic disorders.

Abstract: Novel 3-alkoxybenzylpiperidines have melatonergic properties. They are believed useful in treating depression, jet-lag, work-shift syndrome, sleep disorders, glaucoma, some disorders associated with reproduction, cancer, immune disorders and neuroendocrine disorders.

Abstract: The compounds of the formula: ##STR1## in which ##STR2## where R.sup.7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.9 is hydrogen, alkyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl; R.sup.10 is hydrogen, alkyl or gemdialkyl; n is one of the integers 0, 1 or 2; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl, alkoxycarbonyl or hydroxycarbonyl; and when X is --NR.sup.9 -- or R.sup.7 is an amino alkyl group, a pharmaceutically acceptable salt thereof; are useful as inhibitors of cholesterol ester hydrolase.

Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: The present invention relates to 3,4,5,6-tetrahydrophthalamide derivatives and 3,4,5,6-tetrahydroisophthalimide derivatives having excellent effects as effective active ingredients of herbicides, and processes for preparing the same, and provides the compounds having a more efficient herbicidal activity, and efficient and industrial processes for the preparation thereof.More specifically, the tetrahydrophthalimide derivative obtained by reacting a halogen-substituted 5-cycloalkyloxyaniline derivative with a 3,4,5,6-tetrahydrophthalic anhydride, or the tetrahydroisophthalimide derivative of the present invention is reacted with various types of amines to prepare a tetrahydrophthalamide derivative represented by the general formula (I): ##STR1## These tetrahydrophthalamide derivatives and the tetrahydroisophthalimide derivatives exhibit excellent herbicidal activities in the soil treatment in the paddy field and field and the stem-foliar treatment.

Abstract: The invention relates to the compounds of the formula ##STR1##

Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p -- or C.sub.6 -C.sub.12 cycloalkenyl-C.sub.p H.sub.2p -- (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.

Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: A thioacryloyl compound of the formula ##STR1## wherein Z is selected from the group consisting of OR, R and NR.sup.1 R.sup.2 ;R is selected from the group consisting of hydrogen; (C.sub.1 -C.sub.18)alkyl; (C.sub.1 -C.sub.8)alkenyl; (C.sub.1 -C.sub.8)haloalkynyl; 2-(5-chlorothienyl)methyl; phenyl optionally substituted with one or more substituents selected from the group consisting of halo-, (C.sub.1 -C.sub.3)alkoxy-, nitro-, and (C.sub.1 -C.sub.3)alkyl; phenacyl optionally substituted with one or more substituents selected from the group consisting of ring halo-, (C.sub.1 -C.sub.3)alkoxy-, nitro-, and (C.sub.1 -C.sub.3)alkyl; arylalkyl optionally substituted with one or more substituents selected from the group consisting of ring halo-, (C.sub.1 -C.sub.3)alkoxy-, nitro-, and (C.sub.1 -C.sub.3)alkyl;R.sup.1 and R.sup.2 are independently selected from (C.sub.1 -C.sub.8)alkyl and phenyl, or R.sup.1 and R.sup.

Abstract: This invention relates to novel PDE-IV inhibitors having the formula: ##STR1## where: R.sup.1 =H, C.sub.1 -C.sub.6 alkyl;R.sup.2 =C.sub.3 -C.sub.7 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.4 -C.sub.8 cycloalkylidene when Y is CH; ##STR2## R.sup.4 =H, OR.sup.5, NHR.sup.5, NHOH, NHNH.sub.2 or ##STR3## R.sup.5 =H, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl or ##STR4## W=N or CH; X=CH.sub.2, O, S, or NH;Y=CH.sub.2, CH, O, S, or NH;Q=a bond or CH.dbd.CH;n=0, 1, 2, 3 or 4;M=O, NOH or H.sub.2 ;Z=H or halogen;or a pharmaceutically acceptable salt thereof, as antiasthmatic agents.

Abstract: Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.