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5866601 |
Carbocyclic compounds
Novel carbocyclic compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane...
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5859034 |
Tri-substituted phenyl compounds which have useful pharmaceutical activity
Tri-substituted phenyl derivatives having the general formula (I): ##STR1## In a preferred embodiment, Y is preferably an --XR a group, X is preferably --O--, Z is preferably an --XR 5 group, R a...
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5855654 |
Pyridazinones as marine antifouling agents
Disclosed is a method of inhibiting the growth of marine organisms on a marine structure, by applying dihydropyridazinone and pyridazinone compounds onto or into the marine structure. These...
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5854268 |
Azetidine, pyrrolidine and piperidine derivatives
A class of substituted azetidine, pyrrolidine and piperidine derivatives are selective agonists of 5-HT 1 -like receptors, being potent agonists of the human 5-HT 1D α receptor subtype whilst...
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5852045 |
Fibrinogen receptor antagonists
Fibrinogen receptor antagonists having the structure, for example, of ##STR1## for example ##STR2##
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5849775 |
Substituted benzoylguanidines process for their preparation, their use as a medicament or diagnostic, and pharmaceutical containing them
Benzoylguaridines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4), R(5) are as defined in the specification, and pharmaceutically tolerated salts thereof.
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5849740 |
Methods for using ketoconazole and related substances in medicaments for treatment of type II diabetes
The present invention is a method of using ketoconazole or molecules resembling ketoconazole with comparable biological activity for the manufacture of drugs and for medical treatment of diabetes...
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5834409 |
Scalp care products containing anti itching/anti irritant agents
Mild aqueous detergent, e.g., shampoo, compositions are disclosed based on a mixture comprising anionic surfactant and amphoteric surfactant, such as betaines, present in the composition at a level...
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5830915 |
Phosphinic acid amides as matrix metalloprotease inhibitors
The invention provides compounds which are useful as inhibitors of matrix metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In...
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5830854 |
Method of treating cystic fibrosis using a tachykinin receptor antagonist
Tachykinin receptor antagonists are useful for the treatment of cystic fibrosis.
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5821259 |
H.sub.3 -receptor agonists as therapeutic agents
The invention provides a method for preventing and alleviating the harmful biological effects of secretion of chemicals from mast cells in the organism of mammals which leads to clinical conditions...
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5817690 |
4-aminoethoxy indolone derivatives
A compound of the formula I: ##STR1## in which Y is hydrogen, halogen or lower alkoxy; R 1 is hydrogen, lower alkyl or aryl(lower)alkyl; R 2 is hydrogen, lower alkyl or --(CH 2 ) n X p Ar,...
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5811444 |
Compositions for reducing abnormal stimulation of endothelin receptors and novel compounds
The invention relates to the new use and the new products of formula (I): ##STR1## in which: R 1 =represents hydroxyl, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, formyl, cycloalkyl, optionally...
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5807878 |
Tetrasubstituted imidazoles
A compound of the formula ##STR1## wherein the substituents are defined in the specification useful for the treatment of cardiovascular disorders.
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5795907 |
Gastin and CCK receptor ligands
Compounds of formula (Ia), (Ib), or (Ic), wherein A represents a group having two fused rings, or a group of formula (Id), R 1 (m) represents up to 6 substituents, K represents --O--, --S--, --CH 2...
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5789432 |
Aromatase-inhibiting composition containing azole derivative
The disclosure describes a pharmaceutical composition comprising an aromatase-inhibiting effective amount of a compound selected from the group consisting of compounds of the formula (I): ##STR1##...
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5767151 |
3,3-(disubstituted) cyclohexan-1-ylidine acetate dimers and related compounds
The present invention relates to novel 3,3-(disubstituted)-cyclohexan-1-ylidene acetate dimers of Formula (I): ##STR1## and related compounds, pharmaceutical compositions containing these...
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5760029 |
Spirocycle integrin inhibitors
This invention relates to novel heterocycles, including (S)-2-phenylsulfonylamino-3- 8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspi ro- 4,5!-dec-2-en-3-yl!carbonylamino! propionic acid, which are...
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5753687 |
Modulators of proteins with phosphotryrosine recognition units
The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions...
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5747542 |
Oxo-substituted tetrahydronaphthalene derivatives having retinold and/or retinoid antagonist-like biological activity
Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
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5739148 |
6-(2-Imidazolinylamino) quinoline compounds useful as alpha-2 adrenoceptor agonists
The subject invention relates to compounds having the structure: ##STR1## wherein: (a) R is unsubstituted C 1 -C 3 alkanyl or alkenyl; (b) R' is selected from unsubstituted C 1 14 C 3 ...
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5731335 |
(1-Heteroazolyl-1-heterocycane derivatives and their use as neuroprotective agents
This invention provides heterocyclic compounds of formula (I) that are potentially useful in the treatment of neuropsychiatric disorders associated with progressive processes leading to neuronal...
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5721265 |
Fluorinated 2-nitroimidazole analogs for detecting hypoxic tumor cells
Agents useful for detecting hypoxic tumor cells are provided. The compounds have the structural formula (I) ##STR1## Methods of using the compounds to detect hypoxic tumor cells are also provided,...
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5712301 |
Use of dexmedetomidine for treating ethanol-induced neurodegeneration
The present invention involves the prevention of ethanol-induced neurodegeneration through the administration to a subject before, during and/or after ethanol consumption an effective amount of...
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5710171 |
Bisphenyl inhibitors of farnesyl-protein transferase
The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzene and analine analogs, further substituted with a second phenyl ring attached via a...
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5710160 |
Diphenyl pyridyl ethane derivatives as PDE IV inhibitors
The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the...
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5705514 |
Signal transduction inhibitor compounds
A method of inhibiting the invasion and metastasis of malignant solid tumors in mammals, said method comprising administering to said mammal an anti-proliferative, anti-invasive and anti-metastasis...
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5693633 |
Angiotensin II antagonists
This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
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5693619 |
Method of using renin inhibiting N-(2-amino-2-oxoethyl) butanediamide derivatives
Disclosed herein is a method of using compounds of the formula: A-N(R 1 )C(O)CH 2 CHR 2 C(O)-B wherein A is R 3 R 4 NC(O)CH 2 when, for example, R 3 is hydrogen or alkyl and R 4 is...
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5677326 |
Indoline compound and 5-HT.sub.3 receptor antagonist containing the same as active ingredient
Indoline compounds represented by the general formula: ##STR1## wherein R 1 represents the group ##STR2## R 2 represents a phenyl group which may be substituted or an aromatic heterocyclic group,...
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5672615 |
Arylsulfonamido-substituted hydrodxamic acids
Disclosed are the compounds of formula I ##STR1## wherein R and R 1 together with the chain to which they are attached or R 1 and R 2 together with the carbon atom to which they are attached...
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5665753 |
Cytokine inhibiting imidazole substituted hydroxamic acid derivatives
The present invention relates to a series of novel imidazole substituted hydroxamic acid derivatives, and compositions useful thereof as inhibitors of matrix degrading metalloproteinases, in...
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5665756 |
Aminoalkyloximes useful in the treatment of depression and obsessive compulsive disorders
Novel aminoalkyloximes of the formula ##STR1## wherein: a. X is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, or a group of the formula ##STR2## wherein Y is hydrogen or loweralkyl,...
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5658938 |
Substituted 1H-imidazoles
Substituted 4-(1,2,3,4-tetrahydro-1-naphthalenyl)-1H-imidazoles and 4-(2,3-dihydro-1H-inden-1-yl)-1H-imidazoles, their optical isomers and their racemic mixtures, their salts, methods for preparing...
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5656650 |
Angiotensin II receptor blocking compositions
This invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier, an angiotensin II receptor antagonist and a second agent selected from a diuretic, a calcium...
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5656651 |
Androgenic directed compositions
Substituted phenylthiohydantoins are provided for use in detecting the presence of tumor cells having androgenic receptors and providing for cytostatic and cytotoxic activity toward such cells. The...
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5643936 |
Treatments for diseases characterized by neovascularization
The applicant has identified a particular class of imidazoles that inhibit angiogenesis. These imidazoles can be used to beneficially treat a variety of angiogenic conditions.
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5641755 |
Regulation of x-ray mediated gene expression
Treatment of cells with ionizing radiation is associated with the production of arachidonic acid. Inhibition of phospholipase A2 abolishes radiation-mediated arachidonate production, protein kinase...
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5633274 |
Cancer treatments
The Applicant has identified a particular class of imidazoles that inhibit nonprostate cancer cell proliferation. These imidazoles can be used to beneficially treat a variety of cancers. The...
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5633237 |
Imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds for treatment of neurotoxic injury
A class of imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac...
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5622973 |
Treatment of osteoporosis with substituted piperidines, pyrrolidines and hexahydro-1H-azepines in combination with bisphosphonates
The present invention is directed to certain novel compounds identified as di- and tri-substituted piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1##...
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5620999 |
Benzenesulfonamide subtituted imidazolyl compounds for the treatment of inflammation
A class of imidazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R 1 is...
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5616599 |
Angiotensin II antagosist 1-biphenylmethylimidazole compounds and their therapeutic use
Compounds of the following formula (I) or the formula (I) p : ##STR1## wherein R 1 is alkyl or alkenyl; R 2 and R 3 are hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl, or aryl fused to...
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5616601 |
1,2-aryl and heteroaryl substituted imidazolyl compounds for the treatment of inflammation
A class of imidazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R 1 -R...
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5610174 |
Use of α.sub.1A -selective adrenoceptor agonists for the treatment of urinary incontinence
The present invention provides a method of treating urinary incontinence in a subject which comprises administering to the subject a therapeutically effective amount of a compound having the...
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5607956 |
1-heteroazolyl-1-heterocyclyl alkane derivatives and their use and their use as neuroprotective agents
The present invention relates to novel heterocyclic compounds having the general formula (1) ##STR1## geometric and optical isomers and racemates thereof where such isomers exist, as well as...
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5604251 |
Imidazole derivatives with a biphenylsulfonylurea or biphenylsulfonylurethane side chain and their use as angitensin II receptors
Imidazole derivatives with a biphenylsulfonylurea or biphenylsulfonylurethane side chain, process for their preparation and their use Compounds of the formula (I) ##STR1## in which R 1 is, for...
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5602122 |
Method for lowering total serum cholesterol and treating hypercholesterolemia with aminoacetylmercapto derivatives
The present invention relates to the use of certain aminoacetylmercapto derivatives in treating patients suffering from hypercholesterolemia.
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5602156 |
Method for inhibiting metalloproteinase expression
Calcium homeostasis is an important regulator of MMP-2 transcription, activation and activity. Disclosed herein are compounds which inhibit the expression of matrix metalloproteinases in cells....
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5587390 |
Imidazole derivatives having a II antagonist activity
Imidazole derivatives having A II antagonist activity, of Formula I, the processes for the preparation thereof, pharmaceutical compositions containing them and the use thereof as therapeutic...
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