Abstract: Compounds having the formula: are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions, methods for the preparation of urokinase-inhibitors, and a method of inhibiting urokinase in a mammal.

Abstract: The object of the invention consists of novel unsaturated hydroximic acid derivatives, the process for their preparation and as active substance such as compounds containing pharmaceutical compositions. The novel compounds possess valuable pharmaceutical effects, so they can be used in the treatment of states connected with energy deficiency of the cell caused by PARP inhibition, in diabetes complications, in oxygen deficient status of the heart and brain, in neurodegenerative diseases, in the treatment of autoimmune and/or viral diseases. In formula (I).

Abstract: A method for synthesizing dyes excitable by a helium-neon laser (excitable at 633 nm) from hololepidines, e. G., 7-halolepidine, which dyes are suitable for the detection and enumeration of reticulocytes in human blood samples. In another aspect, this invention provides a method for immunotyping phenocytes. The method is based on the phenomenon that when dyes of certain structure intercalate into DNA or RNA, the intensity of the dyes increases. The general structure of dyes suitable for use in this invention is shown below: wherein: R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, Y, and n are as defined in the specification.

Abstract: NHE-1 inhibitors, methods of using such NHE-1 inhibitors and pharmaceutical compositions containing such NHE-1 inhibitors. The NHE-1 inhibitors are useful for the reduction of tissue damage resulting from tissue ischemia.

Abstract: This invention relates to novel isoxazolines and isoxazoles of formula (I): or a pharmaceutically acceptable salt or prodrug form thereof. The invention relates to novel isoxazolines which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

Abstract: The present invention discloses novel isoquinoline carboxamide derivatives which are HIV protease inhibitors or prodrugs thereof, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds are hydroxyethylamine tripeptide mimetics which act as inhibitors of the HIV aspartyl protease, an essential enzyme in the replicative life cycle of HIV. Consequently, the compounds of this invention may be advantageously used in the treatment of HIV infection, either alone or in combination with other inhibitors of HIV viral replication or with pharmacoenhancers such as cytochrome P450 inhibitors.

Abstract: Bezimidazole derivatives of general formula (I) having tryptase-inhibitory activity. Exemplary are: N-{2-[2-(4-amidinophenyl)-ethyl]-1-methyl-benzimidazol-5-yl}-N-diethylaminoethyl-(4-ethoxycarbonyl-benzenesulphonamide)-hydrochloride, N-{2-[2-(4-amidinophenyl)-ethyl]-1-methyl-benzimidazol-5-yl}-N-diethylaminoethyl-(dansylamide)-dihydrochloride, and N-{2-[2-(4-amidinophenyl)-ethyl]-1-methyl-benzimidazol-5-yl}-N-diethylaminoethyl-(3-bromo-benzenesulphonamide)-hydrochloride.

Abstract: The present invention relates to novel tetrahydroisoquinoline-3-carboxylic acid alkoxyguanidine compounds that are antagonists of alpha V (&agr;v) integrins, for example &agr;v&bgr;3 and &agr;v&bgr;5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment and/or prevention of pathological conditions mediated by &agr;v&bgr;3 and &agr;v&bgr;5 integrins such as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, rheumatoid arthritis, sickle cell anemia, and in treatment and/or prevention of central nervous system (CNS) related disorders such as neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia, surgery, neurodegenerative diseases, such as Alzheimer's disease and Parkinson's disease, adverse consequences of overstimulation of one or more excitatory amino acids, anxiety, convulsions, chronic pain, psychosis, schizophrenia, anesthesia, and opiate tolerance.

Abstract: Arylsulphonamide-substituted benzimidazole derivatives of formula (I) having tryptase-inhibiting activity. Exemplary are: 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethylaminoethyl)-benzenesulphonylamino]-benzimidazole; 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(2-diethlylaminoethyl)-benzylsulfonylamino]-benzimidazole; and, 1-Methyl-2-[2-(4-amidinophenyl)-ethyl]-5-[N-(3-diethylaminopropyl)-benzenesulphonylamino]-benzimidazole.

Abstract: The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: wherein X is O or NH, L is —O— or —SO2—, and R1-R4, R9-R19, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing the compounds of Formula I. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal.

Abstract: A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.

Abstract: This invention provides compounds having the following general structure: This invention also provides pharmaceutical compositions comprising same and methods of using these compositions to treat and prevent disorders characterized by neuronal damage.

Abstract: A process is described for preparing an aromatic compound substituted by a tertiary nitrile of Formula (1.0.0): comprising treating a substituted aromatic compound of Formula (2.0.0): with a secondary nitrile of Formula (3.0.0): in the presence of a base having a pKa numerical value in the range of from about 17 to about 30, provided that the difference in pKa numerical values between said base and the corresponding tertiary nitrile of Formula (3.0.0) is no more than about 6; in an aprotic solvent having a dielectric constant (∈) of less than about 20; and at a reaction temperature in the range of from about 0° C. to about 120° C.; whereby there is formed said tertiary-nitrile-substituted aromatic compound final product of Formula (1.0.0); wherein the constituent parts W1, W2, W3, W4, and W5; and the substituent moieties R1, R2, R3, R4, R5, R6, and R7 in the compounds of Formulas (1.0.0), (2.0.0) and (3.0.

Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.

Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Abstract: Ortho-substituted benzoylguanidines of the formula I in which R(1) to R(4) have the meanings given in the claims, are suitable, as antiarrhythmic pharmaceuticals having a cardioprotective component, for the prophylaxis and treatment of infarction and for the treatment of angina pectoris. They also inhibit, in a preventive manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the triggering of ischemically induced cardiac arrhythmias.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R114 R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and mare set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: The present invention relates to a novel thrombin inhibitor which is effective even when orally administered. More specifically, the present invention relates to an aromatic amidine derivative represented by formula (I) and the salts thereof, which show potent selective inhibitory activity for thrombin in which (a), R, R1, R2, R3, A, W, Y and n are defined as described in the specification.

Abstract: There are provided novel compounds of formula (I) ##STR1## wherein R.sup.1 represents a 2-thienyl or 3-thienyl ring and R.sup.2 represents C 1 to 4 alkyl and optical isomers and racemates thereof and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are selective inhibitors of the neuronal isoform of nitric oxide synthase.

Abstract: This invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, and to a method of using such compounds as LTB.sub.4 antagonists. The compounds of this invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruritus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma, and other conditions where marked neutrophil infiltration occurs.

Abstract: There are provided novel compounds of formula I ##STR1## wherein D represents alkyl C1 to 6;T represents a C.sub.3-5 saturated or unsaturated alkylene chain substituted by --(CH.sub.2).sub.m -- NXY; --O--(CH.sub.2).sub.z --NH-- substituted by --(CH.sub.2).sub.m --NXY; or --U--(CH.sub.2).sub.a --N(X)--(CH.sub.2).sub.b --; and a, b, m, X and Y are as defined in the specification together with processes for their preparation, compositions containing them and their use in therapy. Compounds of formula I are expected to be useful inter alia in the treatment of neurodegenerative disorders.

Abstract: The present invention is directed to compounds that act as analgesics and that have the structure of formula (I): ##STR1## wherein; Z is ##STR2## wherein, n is 1 or 2, and R.sub.0 is C.sub.6-12 aryl or C.sub.7-8 aralkyl; orR.sub.1 is selected from the group consisting of hydrogen; --NH--C.sub.1-6 alkyl; C.sub.1-6 alkyl; C.sub.6-12 aryl; C.sub.7-18 aralkyl; arginyl; and R.sub.30 NHC(.dbd.NH)--, wherein R.sub.30 is hydrogen, C.sub.6-12 aryl, C.sub.7-18 aralkyl, or C.sub.1-6 alkyl;R.sub.2 is hydrogen; C.sub.1-6 alkyl; or OH;R.sub.3 is C.sub.6-12 aryl; C.sub.7-18 aralkyl; --CH.sub.2 --C.sub.6 H.sub.2 R.sub.8 R.sub.9 ;or --CH.sub.2 --OHC.sub.6 HR.sub.8 R.sub.9, wherein each of R.sub.8 and R.sub.9 is independently, or hydrogen;R.sub.4 C.sub.6-12 aryl; C.sub.7-18 aralkyl; C.sub.1-12 alkyl; or a substituted or unsubstituted cyclohexyl;R.sub.5 is C.sub.1-6 alkyl; hydrogen; OH; halogen; SH; NO.sub.2 ; NH.sub.2 ; --NH--C.sub.1-6 alkyl; NH.sub.2 C (.dbd.NH--; NH.sub.2 C (.dbd.NH)--NH--; COOR.sub.31, wherein, R.sub.

Abstract: Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(5) have the meanings given in the claims, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and for infarct treatment and also for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiological processes in the formation of ischemically induced damage, in particular in the illicitation of ischemically induced cardiac arrhythmias.

Abstract: This invention relates to compounds and pharmaceutical compositions, and methods for inhibiting or preventing the amyloid protein deposits in the brain which are associated with Alzheimer's disease and aged Down's syndrome patients. More particularly, it relates to the treatment of Alzheimer's disease.

Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or alkyl; R.sup.2 is alkylene; R.sup.3 is hydrogen, alkyl, alkoxy, alkylthio, halogen, nitro group, amino group, monoalkylamino, dialkylamino, aryl, or aralkyl; X is aryl, or aromatic heterocyclic; Y is oxygen, sulfur or a group of formula >N--R.sup.4, in which R.sup.4 is hydrogen, alkyl or acyl; and Z is a group of formula (Za), (Zb), (Zc) or (Zd): ##STR2## and salts thereof can be used to treat or prevent are included those arising from hyperlipidemia, hyperglycemia, obesity, impaired glucose tolerance (IGT), insulin resistant non-IGT (NGT), non-diagnostic glucose tolerance, insulin resistance, diabetic complications, fatty liver, polycystic ovary syndrome (PCOS) and gestational diabetes mellitus (GDM); in addition the compounds of the present invention have aldose reductase inhibitory activity.

Abstract: This invention provides methods for the treatment or amelioration of the symptoms of the common cold or allergic rhinitis which comprises administering to a mammal in need thereof a serotonin 5-HT.sub.1F agonist.

Abstract: 1,8,8-Trifluoro-5,6,7,8-tetrahydroisoquinoline derivatives, and their use in liquid-crystalline mixtures 1,8,8-Trifluoro-5,6,7,8-tetrahydroisoquinoline derivatives of the formula (I)R.sup.1 (--M.sup.1).sub.a (--A.sup.1 --M.sup.2).sub.b (--A.sup.2 --M.sup.3).sub.c --B(--M.sup.4 --A.sup.3).sub.d (--M.sup.5 --A.sup.4).sub.e (--M.sup.6).sub.f --R.sup.2 (I)in which the symbols and indices have the following meanings:the group B is ##STR1## R.sup.1 and R.sup.2 are, for example, alkyl radicals having 1 to 20 carbon atoms;M.sup.1, M.sup.2, M.sup.3, M.sup.4, M.sup.5 and M.sup.6 are, for example, --O--, --CO--O--, --O--CO-- or a single bond;A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are, for example, 1,4-phenylene, pyrimidine-2,5-diyl or trans-1,4-cyclohexylene, anda, b, c, d, e and f are zero or one, with the proviso that the sum of b, c, d and e is 0, 1 or 2.

Abstract: This invention relates to a compound of the Formula IX--C(O)--Y--G--R I(wherein X, Y, G and R have the values defined in the description), or a pharmaceutically acceptable salt thereof, processes and intermediates for the preparation of such a compound or salt, pharmaceutical compositions comprising such a compound or salt and methods of their use as thrombin inhibitors, coagulation inhibitors and agents for the treatment of thromboembolic disorders.

Abstract: The present invention relates to difluorostatone derivatives useful as antiviral agents.

Abstract: Iminooxymephyleneanilides of the formula I ##STR1## where the index and the substituents have the following meanings: n is 0, 1, 2, 3 or 4;R is nitro, cyano, halogen, unsubst. or subst. alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy or an unsubst. or subst. bridge bonded to two adjacent ring atoms;X is a direct bond or CH.sub.2, O or NR.sup.a ;R.sup.a is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl;R.sup.1 is hydrogen,unsubst. or subst. alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkylcarbonyl or alkoxycarbonyl;R.sup.2 is alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, or in the case where X is NR.sup.a, additionally hydrogen;R.sup.3 is hydrogen, cyano, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio or cycloalkyl;R.sup.4 is a 6- to 10-membered mono- or bicyclic, substituted heteroaromatic ring system,and process and intermediates for their preparation and their use.

Abstract: Tetrahydroisoquinoline compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof, in which: R.sub.1 represents one or more substituents selected from H, halo, hydroxy, alkyl (optionally substituted by hydroxy), alkoxy, alkylthio, alkylsulphinyl, alkyl-sulphonyl, nitro, cyano, polyhaloalkyl, polyhaloalkoxy, phenyl (optionally substituted by one or more of halo, alkyl or alkoxy), or R.sub.1 is optionally alkylated carbamoyl;R.sub.2 represents a saturated or unsaturated aliphatic group optionally substituted by hydroxy or alkoxy;E represents an alkylene chain optionally substituted by one or more alkyl groups;and G represents (a) optionally substituted saturated or unsaturated alicyclic group containing 3 to 8 carbon atoms, or (b) optionally substituted saturated or unsaturated aliphatic chain containing 1 to 12 carbon atoms, or (c) optionally substituted 5 or 6 membered heterocyclic ring containing one or more N or O atoms or SO.sub.

Abstract: Disclosed is a 2-oxoindoline derivative represented by the formula (I): ##STR1## wherein Ring A represents a benzene ring which is substituted in the 5-position or 6-position by a lower alkyl group or lower alkoxy group, R.sup.1 represents a phenyl group which is substituted by a halogen atom, a lower alkyl group or a lower alkoxy group, R.sup.2 represents a naphthyl group, indolyl group, isoquinolyl group, benzimidazolyl group or a group represented by the formula: ##STR2## wherein n represents 1 or 2, R.sup.3 represents a lower alkyl group which is substituted by a carboxyl group, a cyano group or a tetrazolyl group, O represents a single bonding arm, and Y represents a single bonding arm,or a pharmaceutically acceptable salt thereof.

Abstract: This invention is directed to compounds of formula (I), ##STR1## pharmaceutically acceptable salts thereof, and pharmaceutically acceptable solvates of either entity, wherein Y is optionally monounsaturated C.sub.3 -C.sub.5 alkylene optionally substituted with C.sub.1 -C.sub.4 alkyl or methylene; R.sup.1 is H; C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy, OH, NR.sup.5 R.sup.6, CONR.sup.5 R.sup.6, C.sub.3 -C.sub.6 cycloalkyl or aryl; or C.sub.3 -C.sub.6 alkenyl; R.sup.2 is H; C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy, OH, NR.sup.5 R.sup.6, CONR.sup.5 R.sup.6, C.sub.3 -C.sub.6 cycloalkyl or aryl; or CONR.sup.5 R.sup.6 ; R.sup.3 and R.sup.4 are each independently selected from H; C.sub.1 -C.sub.4 alkyl optionally substituted with NR.sup.5 R.sup.6 ; C.sub.1 -C.sub.4 alkoxy; halo; CONR.sup.5 R.sup.6 and aryl; aryl is phenyl optionally substituted with one, two or three substituents independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.

Abstract: There are provided novel compounds of formula I ##STR1## wherein D represents alkyl C1 to 6;T represents a C.sub.3-5 saturated or unsaturated alkylene chain substituted by --(CH.sub.2).sub.m --NXY; --O--(CH.sub.2).sub.2 --NH-- substituted by --(CH.sub.2).sub.m --NXY; or --U--(CH.sub.2).sub.a --N(X)--(CH.sub.2).sub.b --;and a, b, m, X and Y are as defined in the specification together with processes for their preparation, compositions containing them and their use in therapy. Compounds of formula I are expected to be useful inter alia in the treatment of neurodegenerative disorders.

Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.

Abstract: A process for the preparation of nitriles of formula ##STR1## wherein X is CH or N, and R.sub.1 and R.sub.2 are each independently of the other hydrogen, chloro, bromo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylamino, CN, phenyl, phenoxy, dimethylamino, piperidyl, morpholinyl or pyrrolidyl, or R.sub.1 and R.sub.2 together form a fused benzene ring, by reacting an aldehyde of formula ##STR2## with hydroxylaminosulfate in the presence of a tertiary amine base of formula ##STR3## wherein R.sub.3 and R.sub.4 are each independently of the other hydrogen, methyl or ethyl, R.sub.5 is branched C.sub.3 -C.sub.5 alkyl or phenyl, and R.sub.6 and R.sub.7 are methyl or ethyl,in the temperature range from 100.degree. to 160.degree. C., while distilling the released water of reaction off concomittantly at a pressure in the range of 0.02 to 1.5 bar, with subsequent removal of the ammonium salts, and isolating the nitrile so obtained by customary methods.

Abstract: This invention relates to compounds of formula (I), ##STR1## pharmaceutically acceptable salt thereof, and pharmaceutically acceptable solvates of either entity, wherein X is CH or N; Y is optionally monousaturated C.sub.3 -C.sub.5 alkylene optionally substituted with C.sub.1 -C.sub.4 alkyl or methylene; R.sup.1 is H; C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy, OH, NR.sup.5 R.sup.6, CONR.sup.5 R.sup.6, C.sub.3 -C.sub.6 cycloalkyl or aryl; or C.sub.3 -C.sub.6 alkenyl; R.sup.2 is H; C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy, OH, NR.sup.5 R.sup.6, CONR.sup.5 R.sup.6, C.sub.3 -C.sub.6 cycloalkyl or aryl; or CONR.sup.5 R.sup.6 ; R.sup.3 and R.sup.4 are each independently selected from H; C.sub.1 -C.sub.4 alkyl optionally substituted with NR.sup.5 R.sup.6 ; C.sub.1 -C.sub.4 alkoxy; halo; CONR.sup.5 R.sup.6 and aryl; R.sup.5 and R.sup.6 are each independently selected from H and C.sub.1 -C.sub.

Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6 ', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.

Abstract: Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R.sup.1, R.sup.2, R.sup.3, G, G.sub.x, R.sup.6', Ra, Xa, R.sup.6, Rb, R.sub.3, p, Q, A and R.sup.4 are as defined herein.

Abstract: A fungicidal compound of formula (I): ##STR1## wherein A is hydrogen, halogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; and one of R.sup.1 and R.sup.2 is optionally substituted isoquinoline while the other is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, halogen or cyano.

Abstract: There are provided novel compounds of formula I ##STR1## wherein D, R.sup.1, R.sup.2, R.sup.3, X and p are as defined in the specification together with processes for their preparation, compositions containing them and their use in therapy.Compounds of formula I are expected to be useful inter alia in the treatment of neurodegenerative disorders.

Abstract: The subject of the invention is the compounds of formula I ##STR1## in which Ar.sub.1 represents naphtyl, phenyl, quinolyl or isoquinolyl optionally substituted;Ar.sub.2 represents a phenyl or thienyl optionally substituted;R.sub.1, R.sub.2 and R'.sub.2 are independently of each other, H or (C.sub.1 -C.sub.4)alkyl;R.sub.1 represents nothing and N is attached to Ar.sub.2, and optionally R.sub.2 and R'.sub.2 form a double bond;or R.sub.1 or R.sub.2 is attached to Ar.sub.2 and represents a (C.sub.1 -C.sub.3)alkylene;R.sub.3 and R.sub.4, which are identical or different, represent H, (C.sub.1 -C.sub.4)alkyl or form, with the nitrogen atom to which they are attached, a (C.sub.5 -C.sub.7) saturated heterocycle selected from pyrrolidine, piperidine and hexahydroazepine;Z.sub.1 represents a (C.sub.1 -C.sub.12)alkylene, optionally interrupted or extended by a (C.sub.5 -C.sub.7)cycloalkyl or phenyl.

Abstract: Novel phosphinic acid-containing peptidyl compounds of formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophobic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. These inhibitors may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to permanent disability. These compounds may also have utility as a means for birth control by preventing ovulation or implantation.

Abstract: The present invention relates to new compounds of formula ##STR1## wherein A is a bicyclic ring chosen from naphthalene, tetrahydronaphthalene, quinoline, isoquinoline and indole.B is a R.sup.2 substituted benzene ring or an unsubstituted pyridine or thiophene ring;R is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy or a group NR.sup.3 R.sup.4 wherein each of R.sup.3 and R.sup.4 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy or a group NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are as defined above;n is zero or an integer of 1 to 2;x is zero or an integer of 1 to 5;and the pharmaceutically acceptable salts thereof.The compounds of the invention are useful as tyrosine kinase inhibitors.

Abstract: Compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.

Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, -N(alkoxycarbonyl)-,-N(acyl)- or --S--or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.

Abstract: Bleach boosters comprising zwitterionic imines and anionic imine polyions having a net negative charge are disclosed. The bleach boosters increase bleaching effectiveness in lower temperature solutions and demonstrate superior color safety profiles. The bleach boosters are ideally suited for inclusion into bleaching compositions including those with detersive surfactants and enzymes. Also provided is a laundry additive product including zwitterionic imines and anionic imine polyions with a net negative charge as bleach boosters. A method for laundering a fabric employing the bleach boosters of the present invention is also disclosed.

Abstract: The present invention provides novel intermediates which are useful for the preparation of excitatory amino acid receptor antagonists. Further provided is a process to enatioselectively prepare hydroisoquinoline compounds with central nervous system activity.

Abstract: Hydrazone compound useful as an excellent organic nonlinear optical material and a highly sensitive coloring chelation agent, represented by the following formula (1): ##STR1## wherein Ar is a substituted or an non-substituted 2-imidazolyl group, a 4-imidazolyl group, 3-pyrazolyl group, 3-pyridazinyl, 2-pyrimidinyl, 4-pyrimidinyl, 2-quinolyl, 1-isoquinolyl, 3-isoquinolyl, 1-phthalazinyl, 2-quinazolinyl, 2-benzimidazolyl, 2-benzothiazolyl, or 2-thiazolyl group,R.sup.1 is a nitro group, cyano group or trifluoromethyl group,R.sup.2 is a nitro group, cyano group, trifluoromethyl group or a halogen atom, or a substituted or an non-substituted alkyl group,R.sup.3 is a hydrogen atom, andn is an integer from 0 to 3.

Abstract: Compounds characterized generally as tetrahydro-quinolinyl or tetrahydro-isoquinolinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein G is a tetrahydro-quinolinyl or tetrahydro-isoquinolinyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from--(CH.sub.2).sbsb.q--C.tbd.C-Vwherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.