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5665744 |
6-heterocyclic-4-amino-1,2,2A,3,4,5-hexahydrobenzn [cd] indoles
6-Thiadiazole-4-1-amino-1,2,2a,3,4,5-hexahydrobenz[c-d]indol
es are provided which are useful in modifying the function of serotonin in mammals.
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5654322 |
Biphenylmethane derivatives and pharmaceuticals containing the same
This invention relates to a biphenylmethane derivative represented by the formula (1): ##STR1## wherein A represents a group ##STR2## in which R 1 , X, Y, Z and B are as defined in the...
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5646172 |
Method of inducing antiandrogenic activity using imidazolidines substituted with a heterocycle
Novel imidazoles of the formula ##STR1## wherein the substituents are as defined in the disclosure and their non-toxic, pharmaceutically acceptable addition salts with acids and bases having...
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5633268 |
Substituted ortho-ethenylphenylacetic acid derivatives
Compounds of the formula I ##STR1## where the index and the substituents have the following meanings as defined in the specification.
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5631253 |
Fungicidal propenoic acid derivatives
Compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C 1 -4 alkyl, C 1 -4 alkoxy, C 1 -4 haloalkyl, C 1 -4 haloalkoxy, C 1 -4 alkylcarbonyl, C...
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5631207 |
Use of 5-alkyl-1,3,4-oxadiazol (and thiadiazol)-2-thiomethylthiocyanates as marine antifouling agents
Disclosed is the use of compositions employing 5-alkyl-1,3,4-oxadiazol(or thiadiazol)-2-thiomethylthiocyanates as the active marine antifouling agent.
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5627198 |
Heterocyclic amides
The invention relates to heterocyclic amides of the formula ##STR1## in which the radicals A, Z, A 1 , R 1 , R 2 and R 3 are as defined in the description, to a process for the preparation of...
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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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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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5604224 |
Substituted heterocyclylisoquinolinium salts and compositions and methods of use thereof
Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries...
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5583128 |
Contraception in female primates without affecting the menstrual cycle
The invention relates to the use of aromatase inhibitors for contraception in female primates and to a method for contraception in female primates using such substances and to the use of those...
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5578595 |
Cyclopropylacetic acid derivatives
Novel 2-(2,2-difluorocyclopropyl)-acetic acid derivatives of formula I ##STR1## wherein A is oxygen or --NR 1 --, B is C 2 -C 6 alkylene, D is oxygen, sulfur or --O--CH 2 --, E is...
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5571821 |
Sulfonamides and derivatives thereof that modulate the activity of endothelin
Sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods...
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5569655 |
Substituted heterocyclylisoquinolinium salts and compositions and method of use thereof
Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries...
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5563159 |
Dithiocarbonimide derivatives useful as acaricidal, fungicidal, and insecticidal agents
There is disclosed a dithiocarbonimide derivative of the formula: ##STR1## wherein B is a C 1 -C 6 alkyl group; X is an NH group or an oxygen atom and Y is a nitrogen atom or a CH group, A is a...
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5559128 |
3-substituted piperidines promote release of growth hormone
The present invention is directed to certain novel compounds identified as 3-substituted piperidines of the general structural formula: ##STR1## wherein R 1 , R 1a , R 2a , R 4 , R 5 , A, X, and Y...
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5556855 |
N-heterocyclic substituted salicylic acids
A compound of the formula Het--NR--SO 2 --Ph 2 --A--Ph 1 (COOH)(OH) and tautomic form, salts, solvates, C 1 -6 alkyl esters and pharmaceutical compositions of the compound. Ph 1 and Ph 2 are...
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5554633 |
Substituted amines as tachykinin receptor antagonists
Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR 9 , where R 9 is...
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5552422 |
Aryl substituted 5,5 fused aromatic nitrogen compounds as anti-inflammatory agents
The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a...
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5550141 |
Method for inhibiting the formation of acid mine drainage
A method is described for inhibiting the production of acid mine drainage from the disposal of sulphide tailings and waste rock deposition during mining and milling of sulphide containing ores,...
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5550140 |
Oxa(thia)diazol- and triazol-ones(thiones) having a miticide and insecticide activity
A description follows of oxa(thia)diazol- and triazol-ones(thiones), with a iticide and insecticide activity, having the general formula ##STR1## wherein: Y=0, S; Z=0, S, NCH 3 , one of the two...
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5547968 |
Treatment of ocular hypertension with a synergistic combination
A method for treatment of ocular hypertension which comprises ocularly administering, to a subject in need of such treatment, an oculo-hypotensively synergistic combination of (a) a...
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5545656 |
2-Oxidole-1-carboxamide pharmaceutical agents for the treatment of alzheimer's disease
This invention relates to the use of certain 3-substituted 2-oxindole-1-carboxamides and their pharmaceutically acceptable base salts for the treatment or prevention of Alzheimer's disease in...
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5543433 |
Azine-substituted phenylacetic acid derivatives and fungicides containing these
Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro, Y is an amino, methylamino or dimethylamino group, Z is a group CHCH 3 ,...
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5538991 |
Endothelin antagonists bearing 5-membered heterocyclic amides
Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension,...
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5523312 |
Antipicornaviral agents
Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1##...
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5514691 |
N-(4-halo-isoxazolyl)-sulfonamides and derivatives thereof that modulate the activity of endothelin
N-(4-halo-isoxazolyl)sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(4-halo-3-isoxazolyl)sulfonamides and...
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5510359 |
Heteroaromatic 5-hydroxytryptamine receptor agonists
A class of substituted five-membered heteroaromatic compounds possessing an imino spacer group are selective agonists of 5-HT 1 -like receptors and are therefore useful in the treatment of...
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5494901 |
Topical compositions for the eye comprising a β-cyclodextrin derivative and a therapeutic agent
A topical composition comprising an amount of a carbonic anhydrase inhibitor and an amount of β-cyclodextrin derivative effective in increasing the bioavailability of the carbonic anhydrase...
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5494919 |
2-substituted piperidines, pyrrolidines and hexahydro-1H-azepines promote release of growth hormone
The present invention is directed to certain piperidine, pyrrolidine, and hexahydro-1H-azepine compounds of the general structural formula: ##STR1## wherein R 1 , R 3 , R 4 , R 5 , A, W, X, Y, and...
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5494926 |
2/3-(heterocyclic alkyl amino)-1-(subst.-phenyl-methoxy)-ethanes/propanes as tachykinin-receptor antagonists
Compounds of formula (I), and salts and prodrugs thereof, wherein Q represents phenyl or benzhydryl; X and Y each represent H or X and Y together form a group =0; Z is O, S or NR 8 (R 8 is H or C...
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5494925 |
2-heterocyclyloxymethyl and 2-heterocyclylthiomethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxides and compositions and method of use thereof
2-Heterocyclyloxymethyl and 2-heterocyclylthiomethyL-1,2,5-thiadiazolidin-3-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases...
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5484804 |
Perhydroisoindole derivatives as antagonists of substance P
This invention relates to novel perhydroisoindole derivatives of general formula (I), ##STR1## wherein radicals R are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl...
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5453433 |
Thiadiazoles and antipicornaviral compositions
Compounds of the formula; ##STR1## wherein: Thi is thiadiazolyl or substituted thiadiazolyl; Y is alkylene bridge of 3-9 carbon atoms; R 1 and R 2 are each independently chosen from...
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5438066 |
Oxa- and thiadiazole derivatives
Fungicidal and insecticidal compounds having the general formula (I): ##STR1## or a stereoisomer thereof, wherein A is CH or N; B is OCH 3 or NHCH 3 ; one of L and M is N and the other is S or O;...
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5418225 |
***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST***
Topical compositions for the eye comprising a β-cyclodextrin derivative and a therapeutic agent
A topical composition comprising an amount of a carbonic anhydrase inhibitor and an amount of β-cyclodextrin derivative effective in increasing the bioavailability of the carbonic anhydrase...
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5414006 |
Arylalkoxythiocoumarins, the preparation thereof and therapeutic compositions containing these
Arylalkoxythiocoumarins of the formula ##STR1## where R 1 and R 2 are each, independently of one another, hydrogen, C 1 -C 5 -alkyl, trifluoromethyl, phenyl or halogen, or together are a C 3 ...
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5409944 |
Alkanesulfonamido-1-indanone derivatives as inhibitors of cyclooxygenase
Disclosed are compounds of Formula I useful in the treatment of cyclooxygenase mediated diseases such as pain, fever and inflammation of a variety of conditions including rheumatic fever, symptoms...
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5401853 |
Thiadiazole derivatives for the treatment of depressive states
Thiadiazole derivatives of general formula (I) ##STR1## wherein R 1 is selected from the class consisting of: C 1 -C 10 linear or branched alkyl, benzyl, optionally substituted at the aromatic...
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5401743 |
Aminoalkyl-substituted 2-amino-5-mercaptothiadiazoles the preparation and use thereof
Aminoalkyl-substituted 2-amino-5-mercapto-1,3,4-thiadiazole derivatives of the formula ##STR1## where A and n have the meanings stated in the description, and the preparation thereof are described....
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5391560 |
Substituted carbamoylpyrazolines
The invention relates to new substituted carbamoylpyrazolines ##STR1## to processes in their preparation, and to their use as pesticides.
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5389663 |
1-(1h-1,2,4-triazole-yl)-2-propanol compounds
An azole compound represented by the formula (I): ##STR1## wherein X is a nitrogen atom; Ar is a phenyl group substituted by halogen or a halogenated C 1 -4 alkyl group; R 1 and R 2 independently...
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5374642 |
Hydroquinone diethers, their preparation and their use
Hydroquinone diethers of the general formula I ##STR1## where R 1 is hydrogen, halogen or C 1 -C 6 -alkyl, A and B are each unsubstituted or substituted methylene, ethylene or propylene and X...
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5369107 |
Thiazole derivatives, processes for production thereof and pharmaceutical compositions comprising the same
Compounds of the formula: ##STR1## wherein A is S, SO, or SO 2 , R 1 is H or acyl, R 2 is H, alkyl, hydroxyalkyl, halogen or carboxy, and R 3 is pyridyl are claimed. The compounds are useful as...
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5366984 |
Methyl α-arylacrylates substituted by a heterocyclic radical and their use
Methyl α-arylacrylates substituted by a heterocyclic radical and having the general formula ##STR1## where R is alkyl, alkenyl, haloalkyl, cycloalkyl, alkoxy, alkylcarbonyl, alkoxycarbonyl,...
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5344482 |
Use of thiadiazoles as biocides for material protection
The present invention relates to the use of thiadiazoles of the type ##STR1## in which R 1 , R 2 and R 3 = hydrogen, alkyl groups having 1-4 carbon atoms substituted alkyl groups having...
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5342849 |
Phenoxyalkyl-substituted heteroaromatics and a method for controlling pests
Phenoxyalkyl-substituted heteroaromatics of the formulae Ia and Ib ##STR1## where the substituents have the following meanings: R 1 C 1 -C 12 -alkyl, C 2 -C 12 -alkenyl, C 2 -C 12 -alkynyl,...
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5338737 |
Biphenyl oxadiazoles and thiadiazoles as angiotensin II antagonists
Novel heterocyclic methyl derivatives of biphenyl oxadiazoles and thiadiazoles are described, as well as methods for the preparation of said derivatives and pharmaceutical compositions of the same,...
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5336686 |
17 Methylene lactones of steroids
A compound selected from the group consisting of a compound of the formula ##STR1## wherein the substituents are defined as in the application having antiglucocorticoid and antiprogestomimetic...
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5334603 |
Composition and use of 3-phenyl-5-thiocyano-methylthio-1,3,4-thiadiazole-2(3h)thione
A compound is prepared which corresponds to the formula: ##STR1## This compound has been found to exhibit antimicrobial activity in industrial and commercial applications and compositions...
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