Abstract: The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the treatment of diabetic nephropathy.

Abstract: The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the treatment of macular degeneration.

Abstract: Tetrazole derivatives of the formula wherein R is a substituted or unsubstituted phenyl group, heterocyclic group, or benzo-fused heterocyclic group,which exhibit activity as insecticides and acaricides.

Abstract: The present invention is directed spiro-substituted azacycles of formula I: (wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, k, l and m are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.

Abstract: The present invention relates to compounds of the formula IA--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.

Abstract: Carboxylic acid derivatives of the formula I ##STR1## here R.sup.1 is a tetrazole [sic], nitrile [sic], a group COOH or a radical which can be hydrolyzed to COOH, and the other substituents have the meaning explained in the description.

Abstract: Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group; R.sup.1 is hydrogen or an optionally substituted hydrocarbon residue; R.sup.2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R' is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g.

Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein: B and D are each, independently, hydrogen, halogen, --CN, alkyl of 1-6 carbon atoms, aryl, aralkyl of 6-12 carbon atoms;X is H, or halogen;R.sup.1 is hydrogen, alkyl of 1-6 carbon atoms, --CH(R.sup.2)W, --C(CH.sub.3).sub.2 CO.sub.2 R.sup.3, 5-thiazolidine-2,4-dione, --CH(R.sup.4)CH.sub.2 CO.sub.2 R.sup.3, --COR.sup.3, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.2 is hydrogen, alkyl of 1-6 carbon atoms, aralkyl of 6-12 carbon atoms, aryl, --CH.sub.2 (1H-imidazol-4-yl), --CH.sub.2 (3-1H-indolyl), --CH.sub.2 CH.sub.2 (1,3-dioxo-1,3-dihydro-isoindol-2-yl), --CH.sub.2 CH.sub.2 (1-oxo-1,3-dihydro-isoindol-2-yl), or --CH.sub.2 (3-pyridyl);W is --CO.sub.2 R.sup.3, --CONH.sub.2, --CONHOH, --CN, --CONH(CH.sub.2).sub.2 CN, 5-tetrazole, or --PO.sub.3 (R.sup.3).sub.2 ;R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, or aryl;R.sup.

Abstract: Novel methods for the treatment and/or prophylaxis of diseases caused by tissue-adhering bacteria are disclosed. By interacting with periplasmic molecular chaperones it is achieved that the assembly of pili is prevented or inhibited and thereby the infectivity of the bacteria is diminished. Also disclosed are methods for screening for drugs as well as methods for the de novo design of such drugs, methods which rely on novel computer drug modelling methods involving an approximative calculation of binding free energy between macromolecules. Finally, novel pyranosides which are believed to be capable of interacting with periplasmic molecular chaperones are also disclosed.

Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.

Abstract: The invention relates to the use of a histamine antagonist, an interleukin-1-antagonist and/or a TNF antagonist in a cosmetic, pharmaceutical or dermatological composition for treating sensitive skins. It relates especially to the use of a histamine antagonist, an interleukin-1 antagonist and/or a TNF alpha antagonist for preventing and/or combating skin irritations and/or sores and/or erythema and/or dysaesthetic sensations and/or sensations of inflammation and/or pruritus and/or prickling and/or tingling and/or discomfort and/or tightness of the skin and/or mucosae. It also relates to a composition containing a histamine antagonist, an interleukin-1 antagonist and/or a TNF alpha antagonist which limits or eliminates the irritant side-effects of certain products, and in particular of certain cosmetic, dermatological or pharmaceutical active agents.

Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.

Abstract: The present invention relates to novel 4-oxo-4H-1-benzopyran compounds containing benzyloxymethyl, 3-phenylpropyl, or other araliphatic substituents in their 8-position. These compounds show a leukotriene-antagonistic activity. The compounds are characterized by good oral adsorption. The compounds of the present invention may be used as anti-inflammatory and antiallergic medicaments, and in the treatment of cardiovascular diseases.

Abstract: The present invention relates to novel 1-Phenyl-5-anilinotetrazoles of the formula (I): ##STR1## wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4, m and n have the meaning provided in the specification, precesses for their preparation and their use as microbiocides, insecticides and/or herbicides.

Abstract: This invention comprises novel substituted tetronic acid type compounds, 2, 4(3H, 5H)-furandiones, that are useful for the inhibition of the HIV protease enzyme. The compounds may be useful for the treatment of a person with AIDS or AIDS related diseases. The compounds may be used in the attempt to retard the further replication of any retrovirus containing the aspartyl protease enzyme. Compounds are represented by the formula below.

Abstract: A method for the prevention and treatment of stunning of the heart subsequent to ischemia-reperfusion is described. The method comprises administering a therapeutically effective amount of a phospholamban inhibitor to a patient. Phospholamban inhibitors relieve the inhibitory effect of phospholamban on cardiac sarcoplasmic reticulum Ca.sup.2+ -ATPase.

Abstract: Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group; R.sup.1 is hydrogen or an optionally substituted hydrocarbon residue; R.sup.2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R' is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g.

Abstract: This invention relates to novel carboxylic acid indole compounds and compositions for use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## R.sub.1 is C.sub.1 -C.sub.7 alkyl that is unsubstituted or substituted by halogen or by hydroxy, or is C.sub.2 -C.sub.7 -alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkoxy, C.sub.1 -C.sub.7 alkoxy or C.sub.3 -C.sub.7 cycloalkyl-C.sub.1 -C.sub.7 alkoxy;R.sub.2 is 1H-tetrazol-5-yl, carboxy, C.sub.1 -C.sub.7 alkoxycarbonyl, SO.sub.3 H, PO.sub.2 H.sub.2, PO.sub.3 H.sub.2 or halo-C.sub.1 -C.sub.7 alkanesulfonylamino;R.sub.3 is 1H-tetrazol-5-yl, hydroxymethyl, C.sub.1 -C.sub.7 alkoxymethyl, formyl, carboxy, C.sub.1 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.7 alkoxy-C.sub.1 -C.sub.7 alkoxycarbonyl, phenyl-C.sub.1 -C.sub.4 alkoxycarbonyl or carbamoyl, the amino group of which is unsubstituted or mono-substituted by C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 alkenyl or by phenyl-C.sub.1 -C.sub.7 alkyl or di-substituted by C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 alkenyl or by phenyl-C.sub.1 -C.sub.

Abstract: This invention covers certain hydroxy-substituted benzopyrans which are useful for treating asthma and other diseases involving leukotriene-related disease states.

Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.

Abstract: A method of treating ocular hypertension and/or glaucoma in a mammal by locally administering to the eyes of a mammal a composition comprising an effective amount of a compound of the formula wherein R.sup.1 is lower alkyl, lower alkenyl, or R.sup.5 --A--B--, where R.sup.5 is hydrogen, lower alkyl, cycloalkyl or aliphatic acyl; A is oxygen or sulfur; and B is a single bond or a lower alkylene; R.sup.2 is lower alkyl, lower alkenyl, or --C(R.sup.6)(R.sup.7)(R.sup.8), wherein R.sup.6 is hydroxyl or lower alkoxy; and R.sup.7 and R.sup.8 each is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, aryl or aralkyl; R.sup.3 is carboxyl or --CON(R.sup.9)(R.sup.10), wherein R.sup.9 and R.sup.10 each is hydrogen or lower alkyl; R.sup.4 is carboxyl, carboxycarbonyl or tetrazol-5-yl; or a pharmacologically acceptable salt or ester thereof.

Abstract: A method of treatment of a human to inhibit a steroid 5.alpha.-reductase, particularly a testosterone 5.alpha.-reductase, which comprises treating said human with an effective amount of a compound of the formula (I) ##STR1## or a pharmaceutically acceptable base salt thereof, wherein R is --CO.sub.2 H or tetrazol-5-yl;R.sup.1 is C.sub.3 -C.sub.8 alkyl optionally substituted by fluoro; andR.sup.2 is C.sub.2 -C.sub.4 alkylor with a pharmaceutically acceptable base salt or composition thereof. Conditions which are treatable by such inhibition include acne vulgaris, alopecia, seborrhoea, female hirsutism, benign prostatic hypertropy, male pattern baldness and human prostate adenocarcinomas.

Abstract: The present invention provides a compound of formula: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6a and R.sup.6b are defined herein or a pharmaceutically acceptable salt thereof, a process for its preparation, intermediates and its use as a tachykinin antagonist.

Abstract: The present invention relates to the use of angiotensin antagonist or a pharmaceutically acceptable salt thereof for the treatment of normal tension glaucoma, wherein said angiotensin antagonist and salt thereof have pronunced selectivity for the AT1 receptor.

Abstract: Ketoconazole is used for treating cocaine addiction. Mammals, including humans, that are chronically addicted to cocaine are treated with ketoconazole to decrease self-administration of the drug.

Abstract: Tetrazole derivatives of the formula ##STR1## wherein R is a substituted or unsubstituted phenyl group, heterocyclic group, or benzo-fused heterocyclic group,which exhibit activity as insecticides and acaricides.

Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole and triazole peptoids which are useful as inhibitors of human neutrophil elastase (HNE) for the treatment of HNE-mediated processes implicated in conditions such as adult respiratory distress syndrome, septic shock and multiple organ failure. A series of studies also have indicated the involvement HNE in myocardial ischemia-reperfusion injury, emphysema. HNE-mediated processes are implicated in other conditions such as arthritis, periodontal disease, glomerulonephritis, dermatitis, psoriasis, cystic fibrosis, chronic bronchitis, atherosclerosis, Alzheimer's disease, organ transplantation, corneal ulcers, and invasion behavior of malignant tumors.

Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is alkyl, Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)-- where R.sup.8 is hydrogen, alkyl, haloalkyl, aryl, arylalkyl, cycloalkyl or (cycloalkyl)alkyl, and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.

Abstract: The invention is a method of using Angiotensin (AII) Antagonists as inhibitors of the growth of adipose tissue, reducing adipocyte growth and body weight gain.

Abstract: The present invention relates to the use of an angiotensin II receptor antagonist in the manufacture of a medicament for the treatment of chronic inflammatory disease states.

Abstract: Novel compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and X have the meaning indicated in claim 1, and their salts exhibit endothelin receptor-antagonistic properties.

Abstract: Novel compounds of the formula: ##STR1## are disicosed which are endothelin receptor antagonists.

Abstract: Naphthoic derivatives of the Formula (I) ##STR1## wherein the variables are defined herein; and pharmaceutical compositions containing these compounds, and their use as endothelin receptor antagonists are disclosed.

Abstract: The present invention provides compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, together with pharmaceutically compositions containing, uses of, processes for the preparation of and intermediates used in the preparation of, such compounds.

Abstract: A method of promoting drainage of mucous secretions in the congested airways of a bedridden/immobilized patient or an intubated/mechanically-ventilated patient is disclosed. The method comprises administering to the airways of the patient a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5')tetraphosphate, an analog of UTP, or any other analog, in an amount effective to promote drainage of fluid in the congested airways, including sinuses, by hydrating mucous secretions or by stimulating ciliary beat frequency in the airways. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal drops or eye drops or spray), oral form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.

Abstract: Described herein are compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein L is selected from the group consisting of ##STR2## R.sup.2 is selected from (a) ##STR3## R.sup.3 is selected from optionally substituted phenyl, and optionally substituted pyridyl; Y is selected from halogen, alkyl, haloalkyl, alkoxy, pyridylmethoxy, thiazolylmethoxy, benzothiazolylmethoxy, quinolylmethoxy, and optionally substituted quinolylmethoxy; W is selected from hydrogen, alkyl, hydroxyalkyl, and hydroxy; A is absent or is selected from optionally substituted alkylene optionally substituted cycloalkylene, optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, and ##STR4## and X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from (b-1) a pharmaceutically acceptable metabolically cleavable group, (b-2)--OR.sup.10,(b-3)--O(CH.sub.2).sub.w --CH(OR.sup.

Abstract: An angiotensin II antagonist compound is administered to mammals with viral disease. This administration ameliorates virus-associated cell injuries, producing therapeutic effects in viral diseases. This compound is also useful for the prevention of such diseases.

Abstract: Disclosed herein is a method of treating a disease of the central nervous system with a compound of the formula ##STR1## in which m is 0, 1 or 2, n and q are each 0 or 1 to 5, and p is 0 or 1, X is --CO.sub.2 H or tetrazolyl,Y is --CH.dbd.CH--, andZ is(i) phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted,(ii) --CHR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted,(iii) .dbd.CR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted, or(iv) ##STR2## where r is 0 or 1 to 3 and the phenyl rings are optionally substituted; provided that when Z is phenyl and m is 1, p is 1; and salts and esters thereof.

Abstract: Certain novel aminoacyl adenylate mimics are described. An exemplary compound of this invention is ?S-(R*,R*)!-3,6-anhydro-1,2-dideoxy-1-?5-?4-?(5-nitro-2-thienyl)ethynyl!ph enyl!-2H-tetrazol-2-yl!-D-allo-heptitol 7-(2-amino-3-methyl-1-oxopentyl)sulfamate. These compounds inhibit isoleucyl-tRNA synthetases and are useful as antimicrobial and antiparasitic agents.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: A tetrazole derivatives of formula (I) ##STR1## a non-toxic salt thereof, an acid addition salt thereof or a hydrate thereof which has an inhibitory effect on interleukin-1.beta. converting enzyme (ICE).

Abstract: Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group; R' is hydrogen or an optionally substituted hydrocarbon residue; R.sup.2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R' is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g.

Abstract: Methods for the treatment of bone disorders utilizing certain prostaglandin agonists/antagonists.

Abstract: Compounds of formula (I) ##STR1## and the pharmaceutically acceptable base salts thereof, wherein R is --CO.sub.2 H or tetrazol-5 yl; R.sup.1 is C.sub.3 -C.sub.8 alkyl optionally substituted by fluoro; and R.sup.2 is C.sub.2 -C.sub.4 alkyl, together with compositions containing, uses of, process for the preparation of, and intermediates used in the preparation of, such compounds. The compounds have steroid 5.alpha.-reductase inhibitory activity and are useful for treating a disease such as benign prostatic hypertrophy.

Abstract: Disclosed herein is a method of using compounds of the formula:A-N(R.sup.1)C(O)CH.sub.2 CHR.sup.2 C(O)-Bwherein A is R.sup.3 R.sup.4 NC(O)CH.sub.2 when, for example, R.sup.3 is hydrogen or alkyl and R.sup.4 is hydrogen, alkyl or a substituted alkyl such as 2-(2-pyridinyl)ethyl, or R.sup.3 and R.sup.4 together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino or thiomorpholino; R.sup.1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R.sup.2 is, for example, alkyl, cycloalkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolyl-methyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state analog, for example, ?1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl!amino for the treatment of congestive heart failure.

Abstract: Novel derivatives of the general structural Formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, complications of diabetes, migraine, bone resorption, and inflammatory diseases, including Raynaud's disease and asthma.

Abstract: The present invention relates to compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein the dashed line represents an optional covalent bond; X is O, NH, S or a direct link; R.sup.3 is hydroxy when the dashed line does not represent a covalent bond and R.sup.3 is absent when the dashed line represents a covalent bond; R.sup.4 is (a), when X is O, a group of formula (i), (b), when X is O, NH or S, optionally substituted hydroxyphenyl, (c) an optionally substituted 4- to 7-membered heterocyclic ring, or (d), when X is NH, a group of formula (ii). The compounds are useful for the treatment of disease associated with the altered tone or motility of smooth muscle.