Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.

Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): ?wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.

Abstract: The invention relates to N-bisaryl- and N-aryl-cycloalkylidenyl-a-hydroxy- and a-alkoxy acetic acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, C1–C12alkyl; C2–C12alkenyl; C2–C12alkynyl; C1–C12haloalkyl; R2 is hydrogen; optionally substituted alkyl; or optionally substituted alkynyl; R3 is optionally substituted aryl or optionally substituted heteroaryl; A is an optionally substituted saturated or unsaturated C3–C8-cycloalkylidene, optionally substituted phenylidene or optionally substituted saturated or unsaturated heterocyclylidene bridge, R4 and R5 are each independently hydrogen or an organic radical, and R6 is hydrogen; tri-C1–C4alkyl-silyl; di-C1–C4alkyl-phenylsilyl; C1–C4alkyl-diphenylsilyl; triphenylsilyl; optionally substituted alkyl; optionally substituted alkenyl or optionally substituted alkynyl.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Abstract: The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.

Abstract: The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor.

Abstract: 7, 8 and 9-substituted tetracycline compounds, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7, 8 and 9-substituted tetracycline compounds are described.

Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.

Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.

Abstract: Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.

Abstract: Aminobutylic acid derivatives of the formula (I): wherein the symbols are as defined in specification; and non-toxic salts thereof. Because of inhibiting matrix metalloproteinase, the compounds of the formula (I) are useful for prevention and/or treatment of diseases, for example, rheumatoid diseases, arthrosteitis, osteoarthritis, unusual bone resorption, osteoporosis, periodontitis, interstitial nephritis, arteriosclerosis, pulmonary emphysema, cirrhosis, cornea injury, cornea ulcer, metastasis, invasion or growth of tumor cells, autoimmune disease, disease caused by vascular emigration or infiltration of leukocytes, arterialization, multiple sclerosis, arota aneurysm, endometriosis, restenosis after PTCA, unstable angina, acute myocardial infarction, transient ischemic attack.

Abstract: Substituted C-furan-2-yl-methylamine and C-thiophen-2-yl-methylamine compounds, processes for their preparation, medicaments and pharmaceutical compositions containing them, and their use in treatment methods and in the preparation of analgesics, in the preparation of a local anaesthetic, an antiarrhythmic, an antiemetic, a nootropic agent and/or a medicament for the treatment and/or prophylaxis of cardiovascular diseases, urinary incontinence, diarrhea, pruritus and/or inflammations, and/or a medicament for the treatment of depression and/or alcohol and/or drug and/or medicament abuse, and/or a medicament for increasing vigilance.

Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Abstract: New benzenedicarboxylic acid derivative compounds; pharmaceutical compositions, diagnostic methods, and diagnostic kits that include those compounds; and methods of using those compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-? activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers, and glaucoma.

Abstract: Compounds of formula I, or a pharmaceutically acceptable salt thereof, The compounds of the present invention are suitable for the treatment of pain and migraine. Also disclosed are method for preparing the compounds, and pharmaceutical composition comprising the compounds as well as methods for treating pain and migraine using the pharmaceutical compositions.

Abstract: N-substituted dithiocarbamate esters, pharmaceutical compositions containing them, and methods of treating hyperproliferative disorders such as cancer by administering the N-substituted dithiocarbamate esters.

Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.

Abstract: The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl, C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR12R13 wherein R12 and R13 are each independently of the other hydrogen or C1-C6-alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; R4, R5, R6 and R7 are each independently hydrogen or C1-C4al

Abstract: Provided, among other things, is a compound of Formula I: wherein: Ar1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl-substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl-substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl-substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioaryl-alkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRR′, NRR′, CO2R (where R and R′ are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; R1 is selected from the group consisting of H and alkyl; R2 is selec

Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.

Abstract: The invention is directed to acylphenylurea derivatives and their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I in which the radicals have the stated meanings, and their physiologically tolerated salts and a process for their preparation are described. The compounds are suitable, for example, for treating type II diabetes.

Abstract: Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Inhibition of histone deacetylase can lead to the histone deacetylase-mediated transcriptional repression of tumor suppressor genes. For example, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, such as hematopoiesis, and genetic related metabolic disorders, such as, cystic fibrosis and adrenoleukodystrophy.

Abstract: Disclosed herein are polymerizable compounds represented by the following formula (1): wherein one of R1 and R2 represents an alkyl group, which has 1 to 4 carbon atoms and is other than a tert-butyl group, and the other represents a hydrogen atom or an alkyl group which has 1 to 4 carbon atoms and is other than a tert-butyl group, R3 to R9 each independently represent a hydrogen atom, a silyl group, a cyano group, a hydroxyl group, a halogen atom or a monovalent nonpolymerizable organic substituent group, and A represents a polymerizable group having a carbon-carbon double bond; polymers obtained by singly polymerizing the polymerizable compounds or copolymerizing them with copolymerizable compounds; and resist compositions comprising the polymers. These polymers are useful as base polymers for resist materials for an exposure light source of a short wavelength.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl 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. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes 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, to a patient in need of such therapy.

Abstract: Novel 2,5-substituted benzolsulfonyl ureas and thioureas of formula (I) as illustrated in the disclosure. The compounds are useful active ingredients for medicaments. The compounds of formula (I) act as inhibitors on ATP-sensitive potassium canals and are suitable for the treatment of cardiovascular disorders, especially the treatment of arrhythmias, prevention of sudden death from heart disease or affect diminished contractility of the heart. The invention also relates to methods for producing compounds of formula (I), the use thereof and pharmaceutical preparations containing said compounds.

Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: The invention relates to compounds of the formula (I), in which the symbols have the following meaning: R(1) is 1. alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms; 2. alkyl having 1, 2, 3, 4, 5, 6, 7 or 8 carbon atoms, in which one to all hydrogen atoms are replaced by fluorine; 3. alkenyl having 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12 carbon atoms; or 4. —CnH2n−nn—Y, nn is zero or 2; and n is zero, 1, 2, 3 or 4; where n is unequal to zero or 1 if nn is equal to 2; 5. —CnH2n−nn—Y, nn is zero or 2; and n is 1, 2, 3 or 4; where n is unequal to 1 if nn is equal to 2.

Abstract: The invention relates to compounds having usefulness in the control of Take-All disease in plants, particularly cereals, a method for the control of Take-All disease, and fungicidal compositions for carrying out the method. Compounds of the invention are oximes or hydrazones of arylgloxamides or heteroarylglyoxamides or cycloalkenylglyoxamides.

Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved

Abstract: The present invention relates to cinnamoylaminoalkyl-substituted benzenesulfonamide derivatives of formula I in which A(1), A(2), A(3), R(1), R(2), R(3), R(4), X, Y, and Z have the meanings indicated in the claims. Compounds of formula I are valuable pharmaceutical active compounds which exhibit, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency or cardiomyopathies, or for the prevention of sudden cardiac death, or for improving decreased contractility of the heart. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, and pharmaceutical preparations comprising them.

Abstract: Phenoxyacetic acid derivatives of the formula: wherein R1, R2, Xn and A are as defined herein, and a process for preparing the derivatives. The derivatives are used as herbicides.

Abstract: O-Benzyloxime ethers of the formula I where X is substituted or unsubstituted CH2, NOalkyl Y is O, S, NR5 R1, R2, R5 are H, alkyl Z1, Z2 are H, halogen, methyl, methoxy, cyano R3, R4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl, N(R6)2, where R6 is H, alkyl, substituted or unsubstituted phenyl, —CO—N(R7)2, where R7 is H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aryloxy, substituted or unsubstituted arylthio, substituted or unsubstituted hetaryl, substituted or unsubstituted hetaryloxy, substituted or unsubstituted hetarylthio, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocy

Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.

Abstract: Certain cyclopropyl oxime ethers substituted by aryl and heterocyclic moieties possess broad spectrum fungicidal and insecticidal properties. These compounds are disclosed along with compositions containing these compounds and methods for controlling fungi and insects by the use of a fungitoxic or insecticidal amount of these compounds.

Abstract: The invention includes inter alia new methods for preparation of the pharmaceutically active compound 2-(4-fluorophenoxymethyl)-5-(4-N-hydroxyureidyl-1-butynyl)-tetrahydrofuran and precursors thereof.

Abstract: Compounds of formula (I), wherein A, B, X, R1, R2, R3, R4, R5, R6 are as defined in the specification, are matrix metalloproteinase inhibitors.

Abstract: This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract: Substituted tetrahydrofuran analogs of prostaglandins and methods of their use in treating glaucoma and ocular hypertension are disclosed.

Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-&agr; converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.

Abstract: 2-Cyano-3,5-dihydroxyhex-2-enecarboxamide derivatives are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases or disorders whose course involves increased connective tissue or cartilage degradation.

Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The compounds 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; the solid triangle is used to indicate .beta. configuration; dashed bonds represent a double bond, or a single bond; R is a substituted heteroaryl radical having at least two pendant substituents selected from the group consisting of C.sub.1 to C.sub.6 alkyl; halogen; trifluoromethyl; COR.sup.1 ; COCF.sub.3 ; SO.sub.2 NR.sup.1 ; NO.sub.2 and CN or at least one cyano group; 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.

Abstract: Compound of formula (I): ##STR1## wherein: T represents alkylene,A and B together form a naphthalene, dihydronaphthalene, or tetrahydronaphthalene group,R represents hydrogen, hydroxy, R' or OR', R' being as defined in the description,G.sub.1 represents halogen, a radical R.sub.1 or a group --O--CO--R.sub.1, R.sub.1 being as defined in the description,G.sub.2 represents a group selected from: ##STR2## X, R.sub.2 and R.sub.21 being as defined in the description, and medicinal products containing the same which are useful in the treatment of a condition related to the melatoninergic system.

Abstract: A fungicidal compound of formula (I): or a stereoisomer thereof, wherein A is CH or N, B is OCH.sub.3 or NHCH.sub.3, E is --NR.sup.1 --C(CH.sub.3).dbd.N-- or --N.dbd.C(CH.sub.3)--NR.sup.1 --, R.sup.1 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl or optionally substitute benzyl, R.sup.2 is H, C.sub.1-4 alkyl, halo(C.sub.1-4)alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl, and R.sup.3 is optionally substituted aryl or optionally substituted heterocyclyl.

Abstract: This invention relates to matrix metalloproteinase (MMP) inhibiting compounds of the formula: ##STR1## where R.sup.1 is C.sub.1 -C.sub.12 alkyl, straight or branched and optionally substituted by halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, carboxamido, nitrile, mono- or di-(C.sub.1 -C.sub.6)alkylamino, thio, C.sub.1 -C.sub.6 alkylthio, aryl, --Oaryl or --OCH.sub.2 aryl where aryl is optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, carboxy, halogen, cyano, nitro, carboxamido, or hydroxy; and C.sub.1 -C.sub.6 alkanesulfonyloxy. R.sup.2 is .alpha.-OH or .beta.-OH and R.sup.6 is H or R.sup.2 and R.sup.6 together are carbonyl; the chemical intermediates; and processes for the preparation of these compounds and the intermediates thereto.Matrix metalloproteinases (MMP) are a family of zinc-containing calcium dependent proteinases, including stromelysins, collagenases, and gelatinases.

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: Iminoacetamides of the formula (I) ##STR1## in which A represents a single bond or optionally substituted alkylene,Q represents oxygen or sulphur,R.sup.1 represents respectively optionally substituted cycloalkyl, cycloalkenyl, aryl or heterocyclyl,R.sup.2 represents respectively optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aryl or heterocyclyl,R.sup.3 represents hydrogen or respectively optionally substituted alkyl, alkenyl, alkinyl or cycloalkyl,R.sup.4 represents respectively optionally substituted cycloalkyl, cycloalkenyl, aryl or heterocyclcyla process for their preparation, pesticidal compositions containing them, and their use for controlling pests.

Abstract: The present invention relates to a compound represented by general formula (I) or a pharmaceutically acceptable salt or ester thereof: ##STR1## [wherein each of ##STR2## is an aryl group or an aromatic heterocyclic group; A.sup.1 is a C.sub.1-6 chain hydrocarbon group or a group represented by --A.sup.1a --W.sup.1 --A.sup.1b -- (wherein W.sup.1 is an oxygen atom, a sulfur atom, an ethynylene group, a cyclopropylene group or a group represented by --NR.sup.W --); A.sup.2 is a C.sub.1-8 chain hydrocarbon group; R.sup.1 is a lower alkyl group, a lower alkenyl group, a lower alkoxy group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a lower alkylcarbamoyl group, a group represented by R.sup.a COO-- (wherein R.sup.a is a hydrogen atom, an amino group, a lower alkyl group, a lower alkoxy group or a lower alkylamino group) or by R.sup.b CONR.sup.c -- (wherein R.sup.

Abstract: Phenylacetic acid benzylamides having the following general structure wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.