Abstract: The present invention provides compounds having the of the formula I: ##STR1## and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.

Abstract: Mercapto amino acid derivatives of formula (I), wherein R is hydrogen, a salt-forming cation of a in vivo hydrolysable ester-forming group; R.sub.1 is selected from (a) and (b) in which A is a monocyclic aryl or heteroaryl ring and B is a monocyclic aryl, alicyclic or heterocyclic ring, C and D are independently --Z.sub.p --(CR.sub.8 CR.sub.9).sub.q -- or --(CR.sub.8 CR.sub.9).sub.q --Z.sub.p -- where p is 0 or 1, q is 0 to 3 provided that p+q in C is not 0, R.sub.8 and R.sub.9 are independently hydrogen or (C.sub.1-6)alkyl or together represent oxo and Z is O, NR.sub.10 or S(O).sub.x where R.sub.10 is hydrogen, (C.sub.1-6)alkyl or aryl(C.sub.1-6)alkyl and x is 0-2, and wherein C and D are linked ortho to one another on each of the rings A and B in formula (b); R.sub.2 is hydrogen, (C.sub.1-6)alkyl or aryl(C.sub.1-6)alkyl; R.sub.3 is hydrogen, (C.sub.1-6)alkyl optionally substituted by up to three halogen atoms, (C.sub.3-7)cycloalkyl, fused aryl(C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl(C.sub.2-6)alkyl, (C.

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

Abstract: Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.

Abstract: The present invention relates to novel 3-(substituted)-2-indolinones compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related disorders such as cancer.

Abstract: The present invention relates, in general, to methods of treating disorders of the eye, and, in particular, to methods of preventing or treating elevated eye pressure and glaucoma. The invention further relates to compounds and compositions suitable for use in such methods.

Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.

Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.

Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) ##STR1## in which Het represents one of the groups ##STR2## in which A, B, D, G, X and Z are each as defined in the description, to a plurality of processes and intermediates for their preparation, and to their use as pesticides.

Abstract: This invention provides novel benzothiophene compounds of the formula I: ##STR1## which are useful for the treatment of the various medical conditions associated with postmenopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus, and cervix. The present invention further relates to pharmaceutical formulations of compounds of formula I.

Abstract: The present invention provides a method of treating depression, mood swings, or Alzheimer's disease in a patient in need of such treatment by administering a selective estrogen receptor modulating compound of the formula ##STR1## in which R.sup.1 and R.sup.2 are independently hydroxy and alkoxy of one to four carbon atoms; and R.sup.3 and R.sup.4 are independently methyl or ethyl, or R.sup.3 and R.sup.4, taken together with the nitrogen atom to which they are attached, form a pyrrolidino, methyl-pyrrolidino, dimethylpyrrolidino, piperidino, morpholino, or hexamethyleneimino ring.

Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.

Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease-hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, and Z are as defined. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof.The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.

Abstract: A compound of the formula:Ar.sub.1 --B--Ar.sub.2wherein Ar.sub.1 is unsubstituted or substituted phenyl, thienyl, furanyl, or pyrrolyl, in which each substituent of the substituted phenyl, substituted thienyl, substituted furanyl, and substituted pyrrolyl, independently, is aldehyde, acyl, ester, carboxyl, amido, nitrile, nitro, cyano, acetal, ketal, oxoalkyl, aminoalkyl, hydroxyalkyl, haloalkyl, iminoalkyl, acid halide, aminoalkylaminoalkyl, aminoalkylaminoalkylamino, hydroxyalkylaminoalkyl, or hydroxyalkylaminoalkylaminoalkyl; B is, --CH.dbd.CH--, or --C C--, in which R is H, alkyl, hydroxyl, alkoxy, ester, aldehyde, hydroxyalkyl, aminoalkyl, carboxyl, --CH(OR.sub.1).sub.2, or NR.sub.2 R.sub.3, where each R.sub.1, independently, is H, alkyl, or acyl; and each of R.sub.2 and R.sub.3, independently, is H, alkyl, hydroxyalkyl, or aminoalkyl; and Ar.sub.

Abstract: The objects of the present invention are:novel organoselenium compounds: aromatic diselenides and selenosulphides;the use of said novel compounds as antioxidant agents;pharmaceutical compositions containing them;a method of preparation of said novel compounds.

Abstract: Tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.

Abstract: Disclosed are novel thiophene nitrone compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for preventing and/or treating neurodegenerative, autoimmune and inflammatory conditions in mammals and as analytical reagents for detecting free radicals.

Abstract: The present invention relates to compounds of the formula: ##STR1## and their use in therapeutics, especially as medicaments with anti-inflammatory and analgesic properties.

Abstract: A compound having formula (1) for use as a medicament wherein n is 2 or 3; Y is O, S or NH; X is O, S or NH; and R is C.sub.1 -C.sub.18 alkyl or acyl which may be substituted.

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

Abstract: Compounds of this invention have the formula: ##STR1## and pharmaceutically acceptable salts, e.g.

Abstract: The present invention relates to novel 3-aryl-4-hydroxy-.DELTA..sup.3 -dihydrothiophenone derivatives of the formula (I) ##STR1## in which A, B, G, S, X, Y, Z and n have the meaning given in the description, to processes for their preparation, to novel intermediates and to the use of the compounds of the formula (I) as agents for controlling pests.

Abstract: A compound of the formula: ##STR1## wherein X is arylene, heteroarylene, fused arylene, fused heteroarylene, or deleted; Y is sulfonyl, --O--, or deleted; R.sub.1 is aryl, heteroaryl, fused aryl, or fused heteroaryl; R.sub.2 is H, lower alkyl, lower alkoxy, halo, nitro, cyano, haloalkyl, hydroxyl, carboxyl, amido, amino, or aminoalkyl; or a salt thereof are disclosed. Also disclosed are a pharmaceutical composition which contains an excipient and an effective amount of a compound of the above formula and a method of treating cancer which involves the administration of an effective amount of such a compound to a patient in need thereof.

Abstract: The invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists of formula I and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, and to a method of using such compounds as LBT.sub.4 antagonists. The compounds of the 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, pruitus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma and other conditions where marked neutrophil infiltration occurs.

Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.

Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N,R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.

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 the farnesylation of the oncogene protein Ras.

Abstract: An ester compound represented by the formula ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and each represent a C.sub.1 -C.sub.6 alkyl group, or other specified groups, which may be optionally substituted with one or more halogen atoms; and R.sub.3 represents a pyrethroid acid residue (a group resulting from elimination of the carboxyl group from pyrethroid acid), and a pesticidal composition containing the ester compound as an active ingredient.

Abstract: The present invention relates to new aromatic compounds, to their preparation and to their use in human and veterinary medicine and in cosmetic compositions.

Abstract: Inhibitors for matrix metalloproteases, pharmaueutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each Tis a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 reresents a variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12, and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.

Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate .alpha. configuration, solid triangles are used to indicate .beta. configuration, dashed bonds represent a double bond, or a single bond, R is a substituted heteroaryl radical, R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2, Y is .dbd.O or represents 2 hydrogen radicals. Certain of the compounds represented by Formula I comprise another aspect of the present invention.

Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.

Abstract: This invention relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are defined as in the specification and the pharmaceutically acceptable salts of such compounds. Compounds of the formula I exhibit antibiotic activity against a wide range of gram-positive and gram-negative organisms, including organisms that are resistant to tetracycline antibiotics.

Abstract: This invention relates to 3-(4-acrylamidobenzoyl)benzo?b! thiophenes, to the process for their preparation, to pharmaceutical compositions and to their use for modifying the balance between bone resorption and bone production in a mammal. The compounds useful in this invention are represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl containing 1-8 carbon atoms, or R.sup.1 and R.sup.2 together with the interposed nitrogen forms a 5-7 membered ring optionally containing an additional heteroatom selected from nitrogen, sulfur or oxygen.

Abstract: A compound of formula (I): ##STR1## wherein: R.sup.1 represents a (C.sub.1 -C.sub.6)alkyl, phenyl, substituted phenyl, or heterocyclyl group; R.sup.2 represents a (C.sub.1 -C.sub.6)alkyl group; R.sup.3 represents:(I) the side chain of arginine, lysine, tryptophan, histidine, serine, threonine, or cysteine, in which any polar amino, hydroxy, mercapto, guanidyl, imidazolyl or indolyl group is rendered substantially non-polar by substitution at the polar N-, O- or S-atom; or(ii) the side chain of aspartic or glutamic acid, in which side chain the carboxylic acid group is amidated;R.sup.4 represents hydrogen or a (C.sub.1 -C.sub.6)alkyl or phenyl (C.sub.1 -C.sub.6)alkyl group; R.sup.5 represents hydrogen or and n is 0, 1 or 2; or substituted phenyl groups; or a salt solvate or hydrate thereof. Compositions containing compound (I) and methods for treatment of diseases or conditions mediated by TNF or MMPs in mammals.

Abstract: Substituted thiophenesulfonylureas and -thioureas I ##STR1## wherein R(1) is selected from the group consisting of hydrogen, halogen, alkyl having 1 or 2 carbon atoms, alkoxy having 1 or 2 carbon atoms, mercaptoalkyl having 1 or 2 carbon atoms, fluoroalkoxy having 1 or 2 carbon atoms, and fluoroalkyl having 1 or 2 carbon atoms;R(2) is selected from the group consisting of hydrogen, alkyl having 1 or 2 carbon atoms such as methyl, alkoxy having 1 or 2 carbon atoms, and trifluoromethyl;X is selected from the group consisting of oxygen (compounds Ia) or sulfur (compounds Ib);Y and Z are identical or different and are selected from the group consisting of hydrogen, F, Cl, Br, I, alkyl having 1 or 2 carbon atoms and alkoxy having 1 or 2 carbon atoms.

Abstract: Disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF and/or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: Disclosed is a benzoylethylene derivative represented by the following formula (I) or a salt thereof. ##STR1## R.sup.1 to R.sup.5 : a hydrogen atom, --OR.sup.9 (R.sup.9 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc.), etc.,R.sup.6 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc.,R.sup.7 : a hydrogen atom, a cyano group, a C.sub.1 -C.sub.5 alkyl group, --SO.sub.q R.sup.15 (q: 0, 1, 2, R.sup.15 : a thienyl group, a phenyl group, etc.) etc.,R.sup.8 : a cyano group, --CR.sup.22 R.sup.23 X (R.sup.22, R.sup.23 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc., X: --NR.sup.24 R.sup.25 (R.sup.24, R.sup.25 : a C.sub.1 -C.sub.5 alkyl group, etc., an alkylene group by combining, etc.)), etc.The benzoylethylene derivative of the present invention has potent tyrosine kinase inhibiting activity and cancer cell growth inhibiting activity. The tyrosine kinase inhibitor of the present invention is useful as a carcinostatic agent.

Abstract: Novel pharmaceutically/cosmetically-active adamantyl-substituted biaromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a')-(f'): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: 2,5-Disubstituted thiophene derivatives, and more particularly, to 2-aryloxy-5-alkansulfonamido-thiophenes of the general formula: ##STR1## Wherein, R.sub.2 is CF.sub.3, C.sub.1 -C.sub.10 alkyl, or phenyl;X is O, S, or CH.sub.2 ; andR is aryl, C.sub.1 -C.sub.10 alkyl, or C.sub.3 -C.sub.8 cycloalkyl; which compounds are pharmacologically active in alleviating inflammation, asthma, arthritis, hypersensitivity, myocardial ischemia and dermatological conditions, such as, psoriasis and dermatitis, and gastrointestinal inflammatory conditions, such as, inflammatory bowel syndrome.

Abstract: This invention relates to novel compounds and a novel use of phenyl ureas in the treatment of disease scates mediated by the chemokine, Interleukin-8 (IL-8). In particular, this invention relates to the novel compounds of Formula (Ia) and their use in treating chemokine mediated diseases wherein the chemokine binds to an IL-8 a or b receptor. Compounds of Formula (Ia) are represented by the structure: ##STR1## wherein interalia, X is oxygen or sulfur;Rb is NR.sub.6 R.sub.7, alkcyl, aryl, arylC.sub.1-4 alkyl, aryl C.sub.2-4 alkenyl, heteroaryl, heteroarylC.sub.1-4 alkyl, heteroarylC.sub.2-4 alkenyl, heterocyclic or heterocyclic C.sub.1-4 alkyl, or a heterocyclic C.sub.2-4 alkenyl moiety, camphor, all of which may be optionally substituted;R.sub.1 is independently selected from hydrogen; halogen; nitro; cyano; C.sub.1-10 alkyl; halosubstituted C.sub.1-10 alkyl; C.sub.2-10 alkoxy; halosubstituted C.sub.1-10 alkoxy; azide; (CR.sub.8 R.sub.8)q S(O).sub.t R.sub.4 ; hydroxy; hydroxy substituted C.sub.

Abstract: Disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF and/or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: A compound having formula (1) for use as a medicament wherein n is 2 or 3; Y is O, S or NH; X is O, S or NH; and R is C.sub.1 -C.sub.18 alkyl or acyl which may be substituted.

Abstract: This invention describes the use of aminoindane and amino-tetrahydronaphthalene derivatives of general formula (I) ##STR1## in which Ar, X, R.sub.1, R.sub.2 and n are defined in claim 1, for the manufacture of a medicament for the treatment of disorders in which a calcium channel antagonist is indicated. Novel compounds falling within formula (I) are also claimed.

Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.

Abstract: A compound of formula (I): ##STR1## wherein R.sub.4 is an optionally substituted C.sub.3 -C.sub.8 cycloalkenyl group. The compounds are inhibitors of matrix metalloproteinases.

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