Abstract: Compounds having the formula (I) wherein R.sub.1 and R.sub.2 are a hydrogen atom, an alkyl group or a hydroxy group, or else R.sub.1 and R.sub.2 form together a bivalent ethylene or trimethylene radical; R.sub.3 is a halogen atom, an alkyl group, an alkoxy group, a mono- or polyhydroxylated alkyl group, an amino group, a mono- or di-alkyl amino group, an acetamido or sulfonamido group; R.sub.1 is a hydroxy group, a mono- or polyhydroxylated alkyl group, an amino group, a mono- or dialkyl amino group, an acetamido or sulfonamido group; R.sub.4 being in the position 3, 4 or 5 and A is a bridge having from 1 to 3 links selected among the groups having the formula (II), --NH--,--N.dbd.--O-- and --S--. R.sub.5 represents an hydrogen atom, an alkyl group, a hydroxy group or an alkoxy group as well as the addition salts thereof with pharmaceutically acceptable acids. Said compound may be used in therapeutical treatment as antihypertensive agents, particularly in the ocular field.
Type:
Grant
Filed:
March 12, 1985
Date of Patent:
May 12, 1987
Assignee:
Laboratoires Chauvin-Blache
Inventors:
Claude Coquelet, Elisabeth Battais, Claude Bonne, Daniel Sincholle
Abstract: The present invention is dealing with cycloalkane-indene-carboximidamide derivatives having the general formula: ##STR1## wherein Rx together with either Ry.sub.1 or Ry.sub.2 represent the moiety ##STR2## (the other Ry being hydrogen), n represents the number 1, 2 or 3,R represents hydrogen or a (1-4 C)-alkyl group,R.sub.1 represents hydrogen, (1-4 C)-alkyl, hydroxyl, (1-4 C)-alkoxy or an amino group which is unsubstituted or substituted by (1-4 C)-alkyl andR.sub.2 is hydrogen, hydroxyl or (1-4 C)-alkyl,as well as the pharmaceutically acceptable salts thereof, with powerful blood platelet aggregation-inhibiting activity.
Abstract: The absorption of a scavenger of oxygen free radicals generated at the time of reperfusion or the absorption of an agent preventing the cytotoxic effects on healthy cells in a mammal. e.g. superoxide dismutase or S-aminotrimethyleneaminoethyl thiophosphate is enhanced by substantially simultaneously administering an absorption enhancing agent therefore, e.g. hydroxylamine or a non-toxic salt thereof. It is also part of the invention to inject WR-2721 intravenously or intramuscularly as a scavenger of oxygen free radicals even in the absence of an absorption enhancing agent.
Abstract: The invention is insecticidal diaminoguanidine hydrazone compounds which are also effective antifeeding agents for insects and methods for their preparation.
Type:
Grant
Filed:
October 17, 1985
Date of Patent:
March 10, 1987
Assignee:
American Cyanamid Company
Inventors:
Roger W. Addor, Donald P. Wright, Jr., Jack K. Siddens, John J. Hand
Abstract: The invention relates to novel [(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-1H-fluoren-yl)oxy]ethanimidamid es and [(2,3,9,9a-tetrahydro-3-oxo-9a-substituted-1H-fluoren-7-yl)oxy]ethanimidic acid hydrazides, their derivatives and their salts. The compounds are useful for the treatment and prevention of injury to the brain and of edema due to head trauma, stroke (particularly ischemic), arrested breathing, cardiac arrest, Reye's syndrome, cerebral thrombosis, cerebral embolism, cerebral hemorrhage, cerebral tumors, encephalomyelitis, spinal cord injury, hydrocephalus, post-operative brain injury trauma, edema due to cerebral infections, various brain concussions and elevated intracranial pressure.
Type:
Grant
Filed:
September 26, 1985
Date of Patent:
August 5, 1986
Assignee:
Merck & Co., Inc.
Inventors:
Edward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
Abstract: An antiviral drug contains as its effective component an isothiosemicarbazone represented by the following general formula (I) or an acidic salt thereof: ##STR1## wherein R.sub.1 represents a halogen atom, a lower (C.sub.1 -C.sub.6) alkyl group, a hydroxy group, a phenyl group which may be or may not be substituted with an alkoxy group containing 1 to 12 carbon atoms, or an unsubstituted or substituted phenylethynyl group represented by the following general formula (II): ##STR2## (wherein R.sub.5 and R.sub.6 may be the same or different, and they each represent a hydrogen atom, a halogen atom, a lower (C.sub.1 -C.sub.6) alkyl group, a hydroxy group or an alkoxy group containing 1 to 12 carbon atoms); R.sub.2 represents a hydrogen atom or a lower (C.sub.1 -C.sub.6) alkyl group; R.sub.3 represents a lower (C.sub.1 -C.sub.6) alkyl group or a benzyl group; R.sub.4 represents a hydrogen atom or a lower (C.sub.1 -C.sub.6) alkyl group.
Abstract: The invention is insecticidal diaminoguanidine hydrazone compounds which are also effective antifeeding agents for insects and methods for their preparation.
Type:
Grant
Filed:
February 25, 1985
Date of Patent:
March 11, 1986
Assignee:
American Cyanamid Company
Inventors:
Roger W. Addor, Donald P. Wright, Jr., Jack K. Siddens, John J. Hand
Abstract: A method of treating cancers or advanced malignant disease involving the weekly administration of methyl-glyoxal bis-guanylhydrazone in amounts of 250-1,000 mg/m.sup.2 per week. In particular the administration involves a weekly dosing regimen and dose escalation over the series of treatments from an initial dosage which may be 250 mg/m.sup.2.
Type:
Grant
Filed:
August 24, 1982
Date of Patent:
May 28, 1985
Assignee:
The United States of America as represented by the Secretary of Department of Health and Human Services
Abstract: The present invention is dealing with compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, in which n and m represent the number 1 or 2, X and Y hydrogen, alkyl (1-4 C), alkoxy (1-4 C), hydroxy, halogen, hydroxymethyl, trifluoromethyl, acyl (1-4 C), acyloxy (1-4 C) or the group NR.sub.x R.sub.y, in which R.sub.x and R.sub.y represent hydrogen, alkyl (1-4 C) or a sulphonyl group and R represents the group ##STR2## in which R.sub.1 and R.sub.2 represent hydrogen, alkyl (1-4 C), hydroxy, alkoxy (1-4 C), phenylalkoxy (7-10 C), acyloxy, amino or mono or dialkyl (1-4 C) amino, having potent platelet aggregation inhibiting properties.
Abstract: (+)-6-methoxy-.alpha.-methyl-2-naphthalene acetate of N,N"-bis (4-chlorophenyl)-3,12-diimino-2,4,11,13-tetraazatetradecan-diimidoamide, possessing the formula (I) ##STR1## has high bioavailability by the cutaneous route which enables it to be used topically for the treatment of dermatoses, infected wounds, scalds, bedsores, inflammations of the oral cavity, vulvovaginitis, etc.