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5512568 |
Method of using 4-amino derivatives of 5-substituted mycophenolic acid
The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other...
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5506242 |
Arylsufonamido-substituted hydroxamic acids
The invention relates to a method of inhibiting metalloellastase activity, of inhibiting the degradation of elastin, or of treating macrophage metalloelastase dependent conditions in mammals which...
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5506257 |
Aminocyclohexylamides for antiarrhythmic and anaesthetic uses
The present invention provides methods for blocking sodium channels in cardiac or neuronal tissue using aminocyclohexylamides. This invention also provides kits including aminocyclohexylamides and...
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5502053 |
HIV protease inhibitor compounds
Compounds of formula ##STR1## are HIV protease inhibitors, and are synthesized via a novel route. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment...
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5502061 |
Peptidyl substituted benzamides and naphthamies
The present invention provides HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.
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5491152 |
Derivatives of cyclic ethers and sulfides for the treatment of atherosclerosis
The present invention provides compounds of Formula I, ##STR1## or a pharmaceutically acceptable salt forms thereof, which are inhibitors of acyl-Coenzyme A: cholesterol O-acyltransferase (ACAT),...
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5484810 |
Tissue protective tocopherol analogs
This invention relates to alkylated sulfonium alkylene derivatives of certain 2H-1-benzopyrans, to the intermediates and processes useful for their preparation, to their free-radical scavenger and...
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5484805 |
Heterocyclene derivatives
The invention concerns a heterocyclene derivative of the formula I ##STR1## wherein Ar 1 is optionally substituted phenyl, naphthyl or a 9- or 10-membered bicyclic heterocyclic moiety; A 1 is...
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5482966 |
Oxime derivatives
The invention concerns oxime derivatives of the formula I ##STR1## wherein R 4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di-(1-4C)alkylamino and...
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5462965 |
Use of heterocyclic amino-alcohol compounds for treatment of CNS diseases
A class of heterocyclic amino-alcohol compounds is described for treatment of CNS-related diseases, namely, for use as a neuroprotective agent, to reduce neurotoxic injury associated with...
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5441722 |
Short synthesis of 5,6-dihydro-(S)-4-(ethylamino)-(S)-6-[C.sup.3 H.sub.3 ]-4[2,3-b]thiopyran-2-sulfonamide 7,7-dioxide and related non radioactive compounds
This invention concerns the short synthesis of 5,6-dihydro-(S)-4-(ethylamino)-(S)-6-[C 3 H 3 ]-4H-thieno [2,3-b]thiopyran-2-sulfonamide 7,7-dioxide and related non-radioactive and radioactive...
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5428027 |
Substituted semicarbazone arthropodicieds
Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.
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5428061 |
Organic nitrates and method for their preparation
New organic nitrate compounds, formed by condensing a nitrato alkanoic acid with a sulfur-containing amino acid or peptide, which prevent nitrate tolerance or overcome existing tolerance and which...
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5426109 |
Phenylnaphthalene hydroxy acids
Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They...
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5403857 |
Benzenesulphonamide derivatives having 5-lipoxygenase inhibitory activity
The invention concerns benzenesulphonamide derivatives of the formula I ##STR1## wherein R 1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; R 2 and R 3 together form -A 2 -X 2 -A 3 - which...
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5399584 |
Use of flavone derivatives for gastroprotection
The subject invention relates to methods for preventing or treating damage to the mucosal lining of the gastrointestinal tract of a human or lower animal by administering a safe and effective...
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5399561 |
Acetylenes disubstituted with a phenyl or heteroaryl group and a 2-oxochromanyl, 2-oxothiochromanyl or 2-oxo-1,2,3,4-tetrahydro-quinolinyl group having retinoid-like biological activity
Compounds of the formula ##STR1## where R 1 and R 2 are hydrogen, lower alkyl of 1-6 carbons, or halogen; R 3 is hydrogen, lower alkyl of 1-6 carbons, halogen, OR 11 , SR 11 , OCOR 11 , SCOR 11...
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5399589 |
Oxalyl hydrazide-hydroxamic acid derivatives, their preparation and their use as fungicides
Oxalyl hydrazide-hydroxamic acid derivatives of the formula I ##STR1## where the substituents have the following meanings: R, R 1 , R 2 and R 3 independently of one another are hydrogen,...
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5382572 |
Alkyl and acyl substituted quinolines
Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically...
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5378694 |
Acyl and alkoxy substituted quinolines
Compounds useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are are represented by compounds of Formula 1.0: ##STR1## and their...
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5360815 |
Heteroaryl cinnamic acids as inhibitors of leukotriene biosynthesis
Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They...
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5348976 |
Condensed heterocyclic derivatives and agricultural or horticultural fungicides containing the same
The present invention provides a condensed heterocyclic derivative represented by a formula: ##STR1## wherein R 1 represents a lower alkyl group, an alkenyl group, or the like, R 2 , R 3 , R 4 , R...
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5346915 |
Chromans and thiochromans with phenylethynyl substituents at the 7-position having retinold-like biological activity
Novel compounds of the formula ##STR1## where X is S, O; R 1 -R 5 are hydrogen or lower alkyl; R 6 is lower alkyl, lower alkenyl, lower cycloalkyl having 1 to 6 carbons, or halogen; A is lower...
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5346895 |
Chromans and thiochromans with heteroarylethynyl substituents at the 7-position having retinoid-like biological activity
Novel compounds of the formula ##STR1## where X is S, O; R 1 -R 5 are hydrogen or lower alkyl; R 6 is lower alkyl, lower alkenyl, lower cycloalkyl having 1 to 6 carbons, or halogen; A is lower...
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5314891 |
Benzenesulphonamide derivatives
The invention concerns benzenesulphonamide derivatives of the formula I ##STR1## wherein R 1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; R 2 and R 3 together form --A 2 --X 2 --A 3 --...
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5308863 |
Substituted aromatic sulfonamides as antiglaucoma agents
Thieno[2,3-b]thiopyran-2-sulfonamides and ring homologs with a hydrophilic substituted-alkyl group adjacent to the thiopyran sulfur are carbonic anhydrase inhibitors topically effective in lowering...
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5292768 |
Compound effective as cerebral insufficiency improver
A compound having the formula (I): ##STR1## wherein A is --CH 2 --, --O--, or --S--; R 1 is CH 3 or OCH 3 ; R 2 is hydroxy or carboxy which may be optionally esterized or amidated; R 3 is H...
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5278174 |
Sigma binding site agents
Sigma binding site agents having the formula ##STR1## which are useful to inhibit sigma binding site-induced activity, pharmaceutical compositions including these agents, and methods of using these...
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5276053 |
Polycyclic amines useful as cerebrovascular agents
A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of...
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5252608 |
Inhibitors of lysyl oxidase
This invention relates to certain inhibitors of lysyl oxidase and their use in the treatment of diseases and conditions associated with the abnormal deposition of collagen.
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5246961 |
β-d-phenylthioxylosides, and their use as therapeutic agents
The present invention relates, by way of novel industrial products, to the β-D-phenylthioxyloside compounds of the formula ##STR1## in which: X represents a sulfur atom or an oxygen atom; R 1 ,...
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5227399 |
Pyranylphenyl naphthalene lactones as inhibitors of leukotriene biosynthesis
Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They...
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5208222 |
4"-and 4'-alkylthio avermectin derivatives
Avermectin derivatives are disclosed wherein the 4"-hydroxy group is replaced by a substituted alkylthio or acylthio group or an iodo group. These avermectin derivatives can be further derivatized...
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5200410 |
Medicaments for the treatment of cerebral apoplexy
A method of treating cerebral apoplexy in a patient in need thereof which comprises administering to said patient an amount effective therefor of a serotonin agonist which has a binding strength of...
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5190956 |
Certain N-substituted 3-oximino-2,4-dioxoquinolin-2,4-(1H)diones useful for treating viral infections
Compounds useful as antiviral agents against DNA containing viruses, such as herpes group viruses, are disclosed. The compounds are selected from the group consisting of: ##STR1## and their...
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5180735 |
Cyclohexanol derivatives, production and use thereof
The present invention relates to a compound of the formula: ##STR1## wherein A is halogen, N(O)mR 1 R 2 , N ♁ R 1 R 2 R 3 X .crclbar ., S(O)nR 1 or S ♁ (O)mR 1 R 2 X .crclbar . ...
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5166161 |
1,3-dicarbonyl compounds and their use
3-Oxo-4-acyl or carbamyl-bicyclic aromatic and heterocyclic compounds as inhibitors of cyclooxygenase and lipoxygenase and useful as antiallergy and antiinflammatory agents.
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5145855 |
6- and 7-deoxyforskolin and derivatives thereof
Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are...
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5128348 |
Bicyclo(3.1.0)hexane amines and bicyclo(4.1.0)-heptane amines as agricultural fungicides
Certain hexane and heptane amines including geometric and stereoisomers, agricultural compositions containing them and their use as fungicides.
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5116874 |
Anti-tumor method and compounds
This invention provides certain N-[(phenyl)amino]carbonyl-bicyclicsulfonamide sulfonamide derivatives, their pharmaceutical formulations, and their use in the treatment of susceptible neoplasms in...
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5100913 |
Novel sulfonylphenyl-β-D-thioxylosides, their method of preparation and their use in therapeutics
The present invention relates, by way of novel industrial products, to the sulfonylphenyl-β-D-thioxyloside compounds of the formula ##STR1## in which: X is a sulfur atom or an oxygen atom; R is...
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5093356 |
Indenyl hydroxamic acids and hydroxy ureas as inhibitors of 5-lipoxygenase
Compounds having the formula I: ##STR1## are inhibitors of the 5-lipoxygenase enzyme. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They...
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5091409 |
4-alkylamino-6-(C.sub.3-5 -hydrocarbyl)thieno[2,3-B]thiopyran-2-sulfonamide-7,7-dioxides
4-Alkylamino-6-(C 3 -5 -hydrocarbyl)thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxid
es wherein the 4-alkylamino group is an ethylamino or propylamino are powerful carbonic anhydrase inhibitors...
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5071841 |
Sulfur-containing heterocyclic compounds useful for the treatment of osteoporosis, and their production
The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon...
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5071853 |
Polycyclic amines useful as cerebrovascular agents
A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of...
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5071871 |
Pharmaceutically useful benzo(β)pyranes and pyranopyridines
New benz[b]pyranes and pyranopyridines of formula I, ##STR1## wherein the significances of substituents V, T, W, R 3 to R 5 , R 9 , R 10 , m, X, Y and Z are given in claim 1 and their N-oxides and...
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5059621 |
Aromatic heterocyclic derivatives and their thereapeutic and cosmetic use
An aromatic heterocyclic compound has the formula ##STR1## wherein R 1 represents (i) --CH 3 , (ii) --CH 2 OH or (iii) ##STR2## wherein R 3 represents hydrogen, --OR 4 wherein R 4 represents...
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5047419 |
Photodynamic therapy of glioma or mammary carcinoma using seleno- or telluropyrylium salts
There are disclosed pyrylium salts and a method of using them medicinally in photodynamic therapy for increasing the survival time of animals affected with glioma or mammary carcinoma. The salts...
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5045561 |
Substituted furan sulfonamides as antiglaucoma agents
Furan sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
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5021458 |
Amine derivatives and fungicides containing the same
Amine derivatives having the general formula (I): ##STR1## wherein X is selected from the group consisting of ##STR2## wherein Q is oxygen, sulfur or nitrogen atom, and ##STR3## wherein Q is as...
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