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5320839 |
Topical ophthalmic compositions comprising 4-(3-substituted amino-2-hydroxypropoxy)-1,2,5-thiadiazoles and methods for their use
Topical ophthalmic compositions comprising certain thiadiazoles are useful in the treatment of glaucoma and ocular hypertension. The thiadiazoles are slightly less potent than timolol; however,...
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5296499 |
Indole derivatives, their production and use
An agent for inhibiting bone resorption comprising an indole derivative of the formula (I): ##STR1## wherein each ring of A and B is optionally substituted, R is a hydrogen atom, a lower alkyl...
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5290798 |
(hetero-arylmethoxy)indoles 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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5281614 |
Substituted 1,2,4-triazoles bearing acidic functional groups as angiotensin II antagonists
Novel substituted triazolinone, triazolinethione, and triazolinimine compounds of the formula I are useful as angiotensin II antagonists. ##STR1##
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5273993 |
Compounds having one or more aminosulfonyloxy radicals useful as pharmaceuticals
Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula: (HO)p--A--[--OS(O) 2 NR 1 R 2 ] z wherein A...
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5234946 |
Substituted alkylamine derivatives
The substituted alkylamine derivatives represented by formula (I) ##STR1## wherein R 1 represents (a) substituted or unsubstituted C 2 -6 alkenyl group, (b) substituted or unsubstituted C 3 -6...
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5206252 |
Thiadiazolyl-amino derivatives of benzopyrans and indanes
The compounds of the formula: ##STR1## wherein R 1 and R 2 , independent from each other, are selected from the following: C 1 -6 perfluoroalkoxy, C 1 -6 perfluoroalkyl, C 1 -6 alkyl, C 1 -6...
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5194440 |
Substituted cyclic sulphamide derivatives
A class of substituted cyclic sulphamide derivatives are selective agonists of 5-HT 1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and...
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5051420 |
4-substituted-3-1H-imidazol-1-,2,5-thiadiazoles as antiarrhythmic agents
Invention compounds of the formula: ##STR1## wherein Z is ##STR2## are novel. Compounds of the above formula have shown antiarrhythmic activity in an electrophysiological assay.
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5051421 |
Benzo-[b]thiophene derivatives
Benzo[b]thiophene derivatives of formula ##STR1## their tautomers and salts, in which the index n is 0, 1 or 2, alk is lower alkylene, Ar is phenyl, naphthyl or a monocyclic, five- or six-membered...
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5032591 |
Pharmaceutical preparations
A pharmaceutical product comprising a potassium channel activator antihypertensive agent and a β-blocker antihypertensive agent as a combined preparation for simultaneous, separate or sequential...
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5023257 |
Intramuscular injection forms of gyrase inhibitors
Ciprofloxacin and related gyrase inhibitors are tolerated well if administered intramuscularly in the form of an aqueous suspension of the betaine form having an approximate neutral pH value or in...
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4987146 |
N-hetaryl imidazole derivatives
N-hetaryl imidazole derivatives of general Formula I ##STR1## are disclosed in which Het represents an optionally substituted monocyclic or bicyclic heteroaromate, R 3 represents hydrogen, a...
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4981864 |
Method for inhibition of erythrocyte aggregation using anellated tricyclic compounds
The present invention is concerned with the use of compounds of the general formula: ##STR1## wherein R 1 is a phenyl radical of the general formula: ##STR2## or R 1 is a 5 or 6 membered...
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4968691 |
Heterocyclo-substituted azabicyclo muscannic agonists
A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which X represents a group ##STR2## in which p represents an integer of 2 to 4; r represents an integer of 1 or...
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4960798 |
Methods for the treatment of angina
Acetylene compounds of the formula (I): ##STR1## wherein Y, R 1 , R 2 R 3 , and R 4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The...
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4956356 |
Pesticidal 3-substituted 1-nitro-2-imino-1,3-diazacycloalkanes
Pesticidal 3-substituted 1-nitro-2-imino-1,3-diazacycloalkanes of the formula ##STR1## in which n stands for the numbers 0 or 1, R 1 stands for a five- or six-membered heterocyclic group which...
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4943678 |
Pesticidal composition
The invention relates to pesticidal composition against bacterial plant diseases comprising as active ingredient a nitrofurane derivative of the general Formula I ##STR1## wherein X represents a...
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4943307 |
Plant-protective pesticidal composition
The invention relates to a plant-protective solution containing 2.5 to 40 % by weight of one or more water-insoluble plant-protective ingredient(s) 20 to 71.5 % by weight of dimethylformamide...
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4904660 |
Histidine derivatives as superior renin inhibitors
Novel compounds of the following formula (I) and their salts: A compound of the formula (I) ##STR1## These compounds are expected to be useful for renin inhibitors. Thus, the compounds are useful...
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4898889 |
Methods for the treatment of hypertension
Acetylene compounds of the formula (I): ##STR1## wherein Y, R 1 , R 2 , R 3 , and R 4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The...
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4882342 |
5-alkylbenzimidazoles, method of use and pharmaceutical compositions
The present invention concerns new 5-alkylbenzimidazoles of the formula: ##STR1## wherein R 1 is a phenyl ring of the formula: ##STR2## or R 1 is naphthyl, heterocycle or a bicyclic heterocycle...
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4874792 |
Thiophenyl Alkanoic acids useful as leukotriene antagonists
This invention relates to alkanoic acid compounds having phenyl and thio substituents which are useful as leukotriene antagonists and pharmaceutical compositions containing such compounds. This...
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4863945 |
Pyrrolobenzimidazoles and pharmaceutical compositions containing them
Pyrrolobenzimidazoles of the formula: ##STR1## are useful for treatment of heart and circulatory diseases. R 1 is substituted phenyl; or optionally substituted naphthyl or a five- or six-membered...
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4861788 |
Antibacterial 1-normon-2-yl-heterocyclic compounds
Compounds of formula (I): ##STR1## wherein ##STR2## is a 5-membered heterocyclic group having a 6-πelectron system, the five ring atoms being either (a) one carbon atom and four atoms selected...
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4855310 |
Thiadiazole compounds as antagonists of SRS-A
Novel heterocyclic compounds shown by the general formula ##STR1## or the pharmaceutically acceptable salts thereof useful as medicament in particular as antagonist of slow reacting substance of...
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4851406 |
Heterocyclic-substituted indoles and pharmaceutical compositions containing them
The present invention provides indole derivatives of the general formula: ##STR1## wherein R 1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl,...
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4851410 |
1,4-disubstituted pyrazole derivatives, compositions and use
1,4-disubstituted pyrazole derivatives of the formula I ##STR1## where R 1 and R 2 independently of one another are each hydrogen, lower alkyl or benzyl, or R 1 and R 2 , together with the...
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4833152 |
Anti-hypertensive agents
Novel inhibitors of angiotensin coverting enzyme having the general formula R - A - S - Z are disclosed as potent inhibitors of angiotensin converting enzyme and are useful anti-hypertensive agents.
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4831032 |
Cardiotonic benzimidazoles
The present invention provides benzimidazoles of the general formula: ##STR1## wherein R 1 , X, A, and R 2 are as defined in the specification. The present invention also provides processes for...
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4818754 |
Certain anti-inflammatory pyrazolo [4,3-b] pyridine 7-amines
A compound of the formula (1) or a salt or solvate thereof: ##STR1## in which: R 0 is hydrogen or C 1 -6 alkyl; R 1 and R 2 are both hydrogen; or R 1 is hydrogen, C 1 -6 alkyl; and R 2 ...
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4803211 |
Thiadizazole compounds as antagonists of SRS-A
This invention relates to novel heterocyclic compounds structurally characterized by containing a specific heterocyclic group and by the presence of --CH 2 --S-- directly bound to the specific...
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4786639 |
Method for the treatment of reversible airways obstruction and asthma
A method for the treatment and/or prophylaxis of reversible airways obstruction and asthma in mammals, which method comprises administering to the mammal in need of said treatment an effective...
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4774240 |
N-indolylethyl-sulphonic acid amides and their use
The invention relates to N-indolylethyl-sulphonic acid amides of the formula ##STR1## wherein R 1 , R 2 , R 3 , R 4 and R 5 are defined in the specification and X is carboxyl, alkoxycarbonyl,...
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4772622 |
3,5-diamino-1,2,4-oxidiazoles as gastric secretion inhibitors
Novel diamino oxadiazoles, wherein one of the amine functions is connected to a basicly-substituted heterocyclic group through a linear or cyclic connecting group, which are useful for the...
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4772603 |
Method for treating congestive heart failure, angina, occlusive peripheral vascular disease or cerebral vascular disease in mammals
A method for the treatment and/or prophylaxis of congestive heart failure, angina, occlusive peripheral vascular disease or cerebral vascular disease in mammals, such as humans, which method...
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4746669 |
Substituted thiazoles as immunoregulants
Thiazole derivatives have been made, for example, by reacting a 2-aryl-2,2-dialkoxyethylamine with an appropriately substituted aryl acetyl halide followed by treating the resulting amide with...
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4746672 |
Oxides of 1,2,5-thiadiazoles, their use in pharmaceutical compositions
Sulphur derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion of the formula I: ##STR1## in which R 1 and R 2 independently are hydrogen or 1-10C alkyl, 3-8C...
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4745124 |
Orally effective anti-hypertensive agents
Novel thiolester compounds are disclosed which are orally effective angiotensin converting enzyme inhibitors useful in the treatment of mammalian hypertension. They have the formula, R 1 -A 1 ...
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4738963 |
Method for the treatment of incontinence in mammals
A method for the treatment and/or prophylaxis of incontinence in mammals, which method comprises administering to the mammal in need of said treatment an effective amount of a compound of formula...
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4721712 |
1,3-disubstituted 2-oxindoles as analgesic and anti-inflammatory agents
Certain 2-oxindole-1-carboxamide compounds having an acyl substituent at the 3-position, and also on the carboxamide nitrogen atom, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO)...
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4713393 |
Phenylpropyl-2,3-dihydrobenzofurans useful as anti-inflammatory agents
Phenylalkyl-2,3-dihydrobenzofurans and analogs were prepared by (1) nucleophilic substitution involving an appropriately substituted 2,3-dihydrobenzofuranol (or 2,3-dihydrobenzopyranol) and a...
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4695567 |
Pyrrolobenzimidazoles, pharmaceutical compositions containing them and method of using them to treat certain heart and circulatory diseases
The present invention provided pyrrolobenzimidazoles or tautomer thereof, of the general formula: ##STR1## wherein R 1 is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl or C 3 -C 7 cycloalkyl; ...
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4684664 |
Derivatives of β-(4-isocyano-1,2,3,4-diepoxycyclopentyl) acrylic acid
Disclosed herein are derivatives of β-(4-isocyano-1,2,3,4-diepoxycyclopentyl)acrylic acid, the derivatives showing an antibacterial activity, an antifungal activity and an antimycoplasmal activity.
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4683228 |
Guanidinopyrazolylamides, guanidimoimidazolylamides, compositions containing them, and method of using them to inhibit gastric acid secretion
A guanidine derivative of the formula I: ##STR1## in which R 1 , R 2 , R 3 , R 4 , ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is...
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4668673 |
Bicycle benzo-oxy heterocyclic ethers and thioethers, pharmaceutical compositions and use
A class of bicyclic benzo-oxy heterocyclic ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions...
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4663331 |
1,2,5-thiadiazol-3,4-diamines
This invention relates to Mannich-alkynyl aminothiadiazole oxides having histamine H 2 -antagonist activity. A particular compound of this invention is...
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4659721 |
Alkanol derivatives, and pharmaceutical preparation containing these compounds
Alkanol derivatives corresponding to the general formula I R 1 R 2 N--(CH 2 ) m --Q--CH 2 X--CH 2 --Y--(CH 2 ) n --NHR 3 (I) which have a highly selective action on...
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4656180 |
Diamine derivatives and pharmaceutical preparations containing these compounds
Diamine derivatives corresponding to the general formula I R 1 R 2 N--(CH 2 ) m --Q--A--NH--R--NH--B--Q'--(CH 2 ) n NR 3 R 4 (I) which have a highly selective action on histamine-H 2 ...
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4656176 |
2-thiazolyl, oxazolyl, triazolyl and thiadiazolyl alkylamino-3-nitro-heterocyclic compounds
2,3-Unsaturated nitrogen-containing heterocyclic compounds with a 3-nitro group and a 2-heterocyclyl alkylamino group. The alkyl group of 2-position substituents is preferably interrupted by sulfur...
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