Abstract: The compounds of formula I ##STR1## wherein R.sup.1 -R.sup.9, R.sup.15, A, X, Y, Z and n have the meaning given in the specification are active as protein kinase inhibitors and can be used as medicaments, particularly for the treatment of inflammatory skin disorders and alopecia.

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: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.

Abstract: Disclosed are compounds of formula I: ##STR1## wherein R.sub.8 and R.sub.9 independently represent hydrogen or organic substituents;W represents optionally substituted thiazolyl or quinoxalinyl;X is hydrogen, hydroxy or lower alkyl; andT is hydrogen, halogen, hydroxy, nitro, amino or alkyl,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptor. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

Abstract: The invention relates to new amino acid derivatives of general formula IR.sup.1 -R.sup.11 --A.sup.1 --B (I)and the pharmaceutically acceptable salts thereof, wherein group B is --A.sup.2 --NR.sup.2 R.sup.3 or R.sup.5, and whereinR.sup.1, A.sup.1, A.sup.2, R.sup.2, R.sup.3, R.sup.5 and R.sup.11 have the meanings described in the specification, as well as the preparation and use thereof. The novel compounds are valuable neurokinin (tachykinin) antagonists.

Abstract: The present invention provides novel hydroxamic acid derivatives represented by the compound of formula I ##STR1## or pharmaceutical acceptable salts thereof, wherein the compounds of the present invention inhibit various enzymes from the matrix metalloproteinase family, including collagenase, stromelysin, and gelatinase, and hence are useful for the treatment of matrix metallo endoproteinase diseases such as osteoarthrits, rheumatoid arthritis, septic arthritis, osteopenias such as osteoporosis, tumor metastasis (invasion and growth), periodontitis, gingivitis, corneal ulceration, dermal ulceration, gastric ulceration, and other diseases related to connective tissue degradation.

Abstract: This invention concerns compounds of formula (I) ##STR1## where A is a C.sub.1 or C.sub.2 alkylene chain optionally substituted by lower alkyl; Z is a bicyclic oxygen-containing aryl radical (e.g. 2,3-dihydro-1,4-benzodioxin-5-yl); R is hydrogen or lower alkyl; R.sup.1 is aryl or aryl(lower)alkyl; R.sup.2 is hydrogen or lower alkyl; and R.sup.3 is hydrogen, an alkyl group of 1 to 10 carbon atoms, cycloalkyl of 3 to 12 carbon atoms; cycloalkyl(lower)alkyl, aryl or aryl(lower)alkyl or R.sup.2 and R.sup.3 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom, and the pharmaceutically acceptable acid addition salts thereof. The compounds are 5-HT.sub.1A -antagonists which may be used, for example, in treating anxiety.

Abstract: Compounds of formula (I) wherein X is (a) or (b), R is Het as defined in the description. These compounds are oxytocin and vasopressin antagonists useful in the treatment of preterm labor, dysmenorrhea, and for the stoppage of labor preparatory to Cesarean delivery.

Abstract: The invention is directed to a series of novel compounds of the formula ##STR1## where Y is carbonyl or sulfonyl; R.sup.7 and R.sup.8 are alkyl, or R.sup.7 and R.sup.8, together with the carbon to which they are attached, form a C.sub.3-6 carbocyclic ring; R.sup.9 and R.sup.10 are each independently selected from hydrogen, hydroxyl, oximido, methyl, carboxyl, carboxyalkyl, unsubstituted or substituted alkoxycarbonyl, alkylcarbonyloxyalkyl, cyanoalkyl, hydroxyalkyl or unsubstituted amino; R.sup.11 is hydrogen, oxo, --N(R.sup.12)--CO--R.sup.13 or --CO--N(R.sup.14)--R.sup.15 ; R.sup.12 is hydrogen or unsubstituted or substituted alkyl; R.sup.13 is alkoxyl, unsubstituted or substituted heterocyclic rings selected from ##STR2## or unsubstituted or substituted alkyl; and R.sup.14 and R.sup.15 are each independently selected from hydrogen or unsubstituted or substituted alkyl. The Y moiety cannot be bonded to the camphor ring at the 3 or 6 positions.

Abstract: A novel compound of the formula: ##STR1## wherein Ar represents an optionally substituted tricyclic condensed benzene ring group which includes at least one heterocyclic ring as a component ring; n represents an integer from 2 to 10; R.sup.1 represents H or an optionally substituted hydrocarbon group, which may be different from one another in the repetition of n; and Y represents an optionally substituted 4-piperidinyl, 1-piperazinyl or 4-benzyl-1-piperidinyl group, or a salt thereof, inhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.

Abstract: A compound represented by formula (I): ##STR1## wherein Q represents an aryl group, a heterocyclic group, a diarylmethyl group, an aralkyl group composed of an aryl group and an alkylene group, an alkyl group or a cycloalkyl group, in which the aryl group, heterocyclic group, and the aryl moiety of the diarylmethyl group and aralkyl group may be substituted with one or more substituents; R represents a bicyclic, substituted, nitrogen-containing heterocyclic group or a substituted phenyl group, in which the nitrogen-containing heterocyclic group is composed of a 5-membered, substituted, aromatic or saturated ring containing one or two nitrogen atoms and a 6-membered ring; and Z represents an alkylene group, an alkenylene group, an alkylene group, a carbonyl group, an alkylene group containing a carbonyl group or an oxalyl group, or a salt thereof.

Abstract: Diarylmethyl piperazine compounds having utility as exogenous receptor combinant species for binding with receptors such as delta, mu, sigma, and/or kappa receptors are disclosed. Compounds of the invention may be employed as conjugates in agonist/antagonist pairs for transductional monitoring and assays of neurotransmitter function, and also variously exhibit therapeutic utility, including mediating analgesia, and possessing utility for the treatment of diarrhea, urinary incontinence, mental illness, drug and alcohol addiction/overdose, lung edema, depression, asthma, emphysema, cough, and apnea, respiratory depression, cognitive disorders, emesis and gastrointestinal disorders.

Abstract: The present invention relates to therapeutic agents for thrombocytopenia which contain an indolocarbazole derivative represented by the formula (I) given below or a pharmaceutically acceptable salt thereof as an active ingredient, and to novel indolocarbazole derivatives.

Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.

Abstract: Aromatic sulfonamide derivatives, particularly benzenesulfonamide, 4-fluorobenzenesulfonamide, 5-chloro-1-naphthalenesulfonamide and 5-isoquinolinesulfonamide derivatives are provided that inhibit Ca.sup.2+ -dependent enzymes and proteins such as Phospholipase A.sub.2, protein kinases such as Protein Kinase C, and inhibit membrane fusion, thereby being a valuable drug for the treatment of inflammation, arthritis, infarction, nephritis and many other types of tissue injury.

Abstract: Diarylmethylpiperazine compounds having utility as receptor-binding species, e.g., for mediating analgesia, and for combatting drug addiction, alcohol addiction, and drug overdose. The compounds may be administered orally, rectally, topically, nasally, ophthalmically, or parenterally (subcutaneously, intramuscularly, and intravenously), for veterinary and human use, and include delta receptor and mu receptor binding species.

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: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds fused on the naphtho-portion of the naphthopyran ring with an indeno group or certain heterocyclic substituents. Certain substituents are also present at the 2 and 5 positions and sometimes at the 6 position of the naphthopyran ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.

Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the 5 and 6-positions of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring, e.g., 2,2-bis(4-methoxy phenyl)-5-methoxycarbonyl-6-morpholino-2H-naphtho[1,2-b]pyran. Certain substituents may also be present at the number 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.

Abstract: The invention is directed to a series of novel piperazinylcamphorsulfonyl compounds where the camphor ring is substituted by amides, amines, alkanes, alkenes, alkylamines, halogens, hydroxy, carboxy, alkoxycarbonyl and heterocyclic tings. Such compounds are oxytocin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery.

Abstract: Compounds having both calcium antagonist and antioxidant activity are disclosed. The compounds are useful in preventing or alleviating damage to tissues at the cellular level. Methods of treatment which employ these properties of the compounds and corresponding pharmaceutical compositions are also disclosed.

Abstract: Compounds, compositions and method of treating hyperalgesia comprising a compound of formula I, II, III and IV as defined in the specification.

Abstract: The invention relates to polycyclic amine compounds of formula (I) ##STR1## and their enantiomers, useful as neurokinin receptor antagonists.

Abstract: A novel compound of the formula ##STR1## wherein Ar represents a tetracyclic fused heterocyclic group which may be substituted; R.sup.1 represents H or a hydrocarbon group which may be substituted; Y represents an amino or nitrogen-containing saturated heterocyclic group which may be substituted, its salt, inhibiting excellent cholinesterase inhibitory activity and monoamine uptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.

Abstract: Urea derivatives of formula (I) ##STR1## wherein the valuable groups are as defined in the specification, which possess both an ACAT inhibitory activity and an antioxidative activity. Those derivatives are useful in the prophylaxis and treatment of hypercholesterolemia and atherosclerosis.

Abstract: A class of substituted piperazine derivatives of formula I ##STR1## are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated conditions, for which a selective agonist of these receptors is indicated.

Abstract: A heterocycle-containing carbonic acid derivative represented by the following general formula (I): ##STR1## or a physiologically acceptable salt thereof which exhibits an excellent preventive and therapeutic effect against various diseases, and an intermediate which is useful for the production of the heterocycle-containing carbonic acid derivative.

Abstract: A process is provided for preparing intermediates of the structure ##STR1## wherein Rpg is preferably .dbd.CHC.sub.6 H.sub.5 ; and P.G. is a protecting group CBZ or BOC, wherein a protected guanylpyrazole is reacted with an azacycloalkyl, azacycloalkenyl or azaheteroalkyl derivative (such as a piperidine derivative) in the presence of a DBU catalyst. The resulting intermediate may be used as a starting material for preparing thrombin inhibitors.

Abstract: Compounds of formula (I): ##STR1## wherein Ra, Rb, B and D have the meanings reported in the disclosure, processes for making the same, and methods of using the same in the treatment of asthma and/or inflammation of the respiratory tract are disclosed.

Abstract: The present invention relates to novel positive inotropic and lusitropic compounds of formula ##STR1## the pharmaceutical acceptable acid addition salts thereof and the stereochemically isomeric forms thereof wherein L is a radical of formula --O-Alk-(NH).sub.p -C(.dbd.O)-R.sup.1, pharmaceutical compositions thereof, methods of preparing said compounds and intermediates in the preparation thereof.

Abstract: The invention relates to new amino acid derivatives of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein group B is --A.sup.2 --NR.sup.2 R.sup.3 or R.sup.5, wherein group R.sup.5 is ##STR2## and R.sup.1, A.sup.1, A.sup.2, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9, X, Y, Z, t and u have the meanings described in the specification, as well as the preparation and use thereof. The novel compounds are valuable neurokinin (tachykinin) antagonists.

Abstract: This invention relates to L-arginine aldehyde derivatives, having the formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.

Abstract: Compounds of general formula (I) are useful for treating mental disorders, wherein R.sub.1 and R.sub.2 are the same or different and selected from hydrogen or lower alkyl; Ar are the same or different and selected from pyridyl and phenyl groups, n is 1 or 2, X is nitrogen or methine. When X is nitrogen, Y is methylene. When X is methine, Y is selected from nitrogen or oxygen. A is selected from carboxylic derivatives. The pharmacologically active salts of formula (I) are also embraced.

Abstract: The invention relates to TS-inhibiting compounds of the formula ##STR1## where W is an alkylene group; D is a structure having two rings that are unsubstituted or substituted, where (i) one ring is a phenyl ring and (ii) the other ring is a phenyl ring or a 6-membered heterocyclic ring; R is a hydrogen atom or an alkyl group; and X and Y together form ##STR2## and to salts of these compounds. The moiety W can be CH.sub.2, and D can be a phenyl ring bridged through a sulfonyl group to another ring.

Abstract: Compounds of the general formula I: ##STR1## are disclosed as novel antipsychotic agents.

Abstract: There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl,with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.

Abstract: An enzymatic process employing pancreatin or choelsterol esterase for resolution of racemates of 4-aryl-2-oxo-pyrrolidine-3-carboxylic acid esters of general formula I ##STR1## in which X represents a carbon-carbon bond or an oxygen atom,R.sub.1 means a hydrocarbon radical optionally substituted by hydroxy groups, oxo groups and/or halogen atoms and/or interrupted by nitrogen atoms with at most 16 carbon atoms,R.sub.2 symbolizes an alkyl group with up to 4 carbon atoms andR.sub.3 represents an alkyl group with at most 6 carbon atoms is described.

Abstract: The present invention relates to therapeutically active heterocyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system related to the metabotropic glutamate receptor system.

Abstract: There are disclosed various compounds of the formula below, ##STR1## where n, X and R.sub.1 through R.sub.4 are as defined in the specification, which are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.Compounds of this invention also inhibit monoamine oxidase and/or act at central .alpha..sub.2 -adrenergic receptors, and hence are useful as antidepressants.

Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.

Abstract: The present invention relates to a compound represented by the general formula (I): ##STR1## [wherein R.sup.1 is a lower alkyl group or the like, R.sup.2 is a lower alkyl group or the like, R.sup.3 and R.sup.4, which may be the same or different, are halogen atoms or the like, R.sup.5, R.sup.6 and R.sup.7, which may be the same or different, are halogen atoms or the like, and X is .dbd.N-- or .dbd.CH--] or a pharmacologically acceptable salt thereof, which has inhibitory effect on acyl-CoA:cholesterol O-acyltransferase (ACAT), a process for producing said compound, and uses of said compound.

Abstract: Compounds of formulae I and II ##STR1## wherein D is H or --OR wherein R is phenyl and R.sub.1 to R.sub.4 are H or a substituent such as phenylthio, and one of the substituents R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a group of formula III--E-CR.sub.5 =C(R.sub.6).sub.2 (III)or R is substituted by a group of formula III, wherein E is a direct bond or --X-C(O)-- wherein X is a linking group, and R.sub.5 and R.sub.6 are each independently of the other H, halogen, C.sub.1 -C.sub.12 alkyl or C.sub.6 -C.sub.10 aryl, can be polymerised to homopolymers or copolymers. The monomers and polymers are reversible photochromic systems which can be used as color indicators, as photochemically modifiable color filters, or for the optical storage of information.

Abstract: Novel piperazinyl- and piperidinyl-cyclohexanols are useful as anxiolytic agents and have other psychotropic properties.

Abstract: The anthracene-spiro-pyrrolidines according to the invention are prepared by reacting either anthracene-spiro-furans or unsubstituted anthracene-spiropyrrolidines with appropriately substituted amines or by reacting unsubstituted anthracene derivatives with appropriately substituted methylenepyrrolidines. The substances can be used as active agents in medicaments, in particular for the production of immunomodulating medicaments.

Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.

Abstract: The invention relates to cyclic imino derivatives of general formulaB--X.sub.5 --X.sub.4 --X.sub.3 --X.sub.2 --X.sub.1 --A--Y--E(I)whereinA, B, E, X.sub.2 to X.sub.5 and Y are defined as in claim 1, the stereoisomers, tautomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting effects, pharmaceutical compositions which contain these compounds and processes for preparing them.

Abstract: Compounds of the formula ##STR1## wherein A, Y, X, B and D are described in the specification are disclosed. The compounds possess activity in treating asthma and other pathologies of the respiratory tract.

Abstract: Compounds of the general formula I ##STR1## are disclosed as novel antipsychotic agents. Pharmaceutical compositions and methods of treating convulsions employing such compounds of formula I are also disclosed.

Abstract: This invention relates to bisulfite adducts of L-Arginine aldehyde derivatives, pharmaceutical formulations containing those adducts and methods of their use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents.

Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.