Cyclic Alcohol Moiety Patents (Class 560/173)
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Patent number: 4675341Abstract: The invention relates to novel [(5,6-dichloro-3-oxo-9a-propyl-2,3,9,9a-tetrahydrofluoren-7-yl)oxy]ethanol , its 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 including that due to AIDS virus, various brain concussions and elevated intracranial pressure.Type: GrantFiled: August 13, 1986Date of Patent: June 23, 1987Assignee: Merck & Co., Inc.Inventor: Edward J. Cragoe, Jr.
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Patent number: 4654433Abstract: A simple single step process for preparing alkyl and substituted alkyl esters of amino acids is described. The products are bioactive compounds including compounds useful as antihypertensive agents.Type: GrantFiled: January 14, 1985Date of Patent: March 31, 1987Assignee: Merck & Co., Inc.Inventor: David L. Hughes
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Patent number: 4622413Abstract: Amino acid ester hydrohalide is produced by reacting amino acid, alcohol, and halocarbonyl compound represented by the formula: ##STR1## in the presence of an excess of the alcohol and under substantially anhydrous conditions, wherein X.sub.1 and X.sub.2 are each independently fluoro, chloro, bromo, trichloromethoxy or tribromomethoxy.Type: GrantFiled: August 31, 1984Date of Patent: November 11, 1986Assignee: PPG Industries, Inc.Inventor: James A. Krogh
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Patent number: 4588833Abstract: Substituted succinic acid amides, in particular substituted succinic acid amides containing differing derivative groups, are prepared by reacting unsaturated carboxamides with carbon monoxide and with a nucleophilic component containing at least one mobile hydrogen atom, in the presence of cobalt compounds and, if appropriate, in the presence of one or more tertiary nitrogen bases, under an elevated pressure and at an elevated temperature.Type: GrantFiled: October 26, 1984Date of Patent: May 13, 1986Assignee: Bayer AktiengesellschaftInventors: Jurgen Kadelka, Hans-Helmut Schwarz
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Patent number: 4585887Abstract: Process for the production of an optically active 3-aminocarboxylic acid ester from a .beta.-keto acid ester. The .beta.-keto acid ester is converted with a chiral amine into the corresponding enamine. The enamine is converted by hydrogenation in the presence of a platinum catalyst into the corresponding N-substituted amino acid esters. Such ester mix is converted by means of HCl gas into the hydrochlorides. The latter are neutralized. Then by liberation and isolation from the neutralized products by hydrogenolysis in the presence of a palladium catalyst, the desired optically-active 3-aminocarboxylic acid ester is obtained.Type: GrantFiled: December 4, 1984Date of Patent: April 29, 1986Assignee: Lonza Ltd.Inventors: Synese Jolidon, Thomas Meul
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Patent number: 4511731Abstract: Preparation of monoethers of dihydroxybenzenes from an isopropenylphenol and an alkylating agent and thereafter oxidizing in the presence of an acid catalyst.Type: GrantFiled: June 24, 1983Date of Patent: April 16, 1985Assignee: The Dow Chemical CompanyInventors: Abel Mendoza, Eric W. Otterbacher
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Patent number: 4474806Abstract: Sulfonyl or carbonyl derivatives of inositols are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These inositol derivatives are prepared by condensation of a protected inositol with a substituted sulfonic or carboxylic acid derivative followed by removal of protecting groups.Type: GrantFiled: May 10, 1982Date of Patent: October 2, 1984Assignee: Merck & Co., Inc.Inventors: Thomas R. Beattie, Shu S. Yang
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Patent number: 4468352Abstract: The distyrylbiphenyls of the formula ##STR1## in which X and X' independently of one another are a direct bond, oxygen, sulfur, --O--C.sub.1-3 -alkylene-CON(R.sub.4)----CON(R.sub.4)--, --O--C.sub.1-3 -alkylene-COO--, OCO or --COO--, with the proviso that if n+n'=O, X and Y' may not be --CON(R.sub.4)-- or O--C.sub.1-3 -alkylene-CON(R.sub.4)--, and if n+n'=2 and X and X' are --CON(R.sub.4)-- or --COO--, A.sup..crclbar. may not be a phosphite or phosphonate anion, and Y and Y' independently of one another are C.sub.1-20 -alkylene, R.sub.1 and R.sub.1 ' independently of one another are unsubstituted or substituted C.sub.1-8 -alkyl or C.sub.3-4 -alkenyl, or R.sub.1 together with R.sub.2, or R.sub.1 ' together with R.sub.2 ', is a heterocyclic ring, R.sub.2 and R.sub.2 ' independently of one another are unsubstituted or substituted C.sub.1-8 -alkyl or C.sub.3-4 -alkenyl, or R.sub.2 together with R.sub.1, or R.sub.2 ' together with R.sub.1 ', is a heterocyclic ring, or R.sub.1 and R.sub.2, or R.sub.1 ' and R.sub.Type: GrantFiled: April 28, 1982Date of Patent: August 28, 1984Assignee: Ciba-Geigy CorporationInventors: Christian Luthi, Hans R. Meyer, Kurt Weber
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Patent number: 4442302Abstract: It has been found that excellent quality photopolymer printing plates having resistance to alcohol-based inks can be prepared from photopolymer compositions comprising a chain extended, liquid, terminally olefinically unsaturated polymer; from about 1% to about 50% by weight based on the weight of the polymer of at least one ethylenically unsaturated monomer; from about 0.1% to about 10% by weight based on the weight of the polymer of photoinitiator; and from about 0.01% to about 2% by weight based on the weight of the polymer of a stabilizer.Type: GrantFiled: July 2, 1982Date of Patent: April 10, 1984Assignee: Hercules IncorporatedInventor: Rudolph L. Pohl
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Patent number: 4422870Abstract: 2-Aryl-1, 3-cyclohexanedione enol ester compounds exhibit outstanding miticidal,mite ovicidal and herbicidal activity.Type: GrantFiled: March 28, 1977Date of Patent: December 27, 1983Assignee: Union Carbide CorporationInventor: Thomas N. Wheeler
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Patent number: 4313889Abstract: Soft quaternary surface active agents having the formula: ##STR1## wherein ##STR2## represents a tertiary open chain or cyclic aliphatic amine; wherein ##STR3## represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.20 open chain or cyclo alkyl group, a C.sub.1 -C.sub.20 alkoxyalkyl group, a C.sub.1 -C.sub.20 acyloxyalkyl group, a C.sub.1 -C.sub.20 haloalkyl group, a C.sub.1 -C.sub.20 carboxyalkyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O--C.sub.1 -C.sub.4 alkyl group, an O--C.sub.1 -C.sub.8 acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 represents a C.sub.9 -C.sub.22 straight or branched alkyl group, a --(CH.sub.2).sub.n -- ##STR4## wherein R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each selected from the group consisting of a hydrogen atom, a methyl group or an ethyl group, a C.sub.0 -C.sub.Type: GrantFiled: June 10, 1980Date of Patent: February 2, 1982Assignee: Merck & Co., Inc.Inventor: Nicolae S. Bodor
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Patent number: 4311706Abstract: Novel, transient prodrug forms of dopa and dopamine have (i) the structural formula (I): ##STR1## wherein each R is independently selected from the group consisting of hydrogen, R.sup.3 -CO- and ##STR2## wherein X is O, S or NR.sup.6 ; R.sup.1 is hydrogen or --COOR.sup.8 ; R.sup.2 is hydrogen or OR; R.sup.Type: GrantFiled: January 22, 1980Date of Patent: January 19, 1982Assignee: INTERx Research CorporationInventors: Nicholas S. Bodor, Kenneth B. Sloan, Stefano A. Pogany
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Patent number: 4299844Abstract: Anti-inflammatory naphthyl compounds, their preparation and pharmaceutical compositions containing the same. The anti-inflammatory activity has a wide spectrum coupled with low side effects such as gastrointestinal irritancy or oestrongenicity. The compounds possess a chiral center at C-2 and can exist as mixtures of optical isomers or as substantially pure optical isomers.Type: GrantFiled: July 9, 1979Date of Patent: November 10, 1981Assignee: Beecham Group LimitedInventor: Alexander C. Goudie
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Patent number: 4284829Abstract: Compounds useful for pharmacological and medicinal purposes having the formulae ##STR1## wherein R is H, C.sub.1 -C.sub.5 alkanoyl; R.sub.1 is H, benzyl, C.sub.1 14 C.sub.5 alkanoyl, P(O)(OH).sub.2, --CO(CH.sub.2).sub.2 COOH or a basic acyl group; each of R.sub.2 and R.sub.4 is H, C.sub.1 -C.sub.6 alkyl, phenyl, pyridyl or (CH.sub.2).sub.y C.sub.6 H.sub.5 ; y is 1-4; R.sub.3 is H or CH.sub.3 ; Z is C.sub.1 -C.sub.13 alkylene or --(alk.sub.1).sub.m --O--(alk.sub.2).sub.n --; each of (alk.sub.1) and (alk.sub.2) is C.sub.1 -C.sub.13 alkylene with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 13; each of m and n is 0 or 1; and W is H, pyridyl, phenyl, fluorophenyl or chlorophenyl; intermediates therefor and methods for their preparation and use.Type: GrantFiled: December 22, 1978Date of Patent: August 18, 1981Assignee: Pfizer Inc.Inventors: Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4256745Abstract: Prostan-1-ol esters and intermediates for their preparation are described; the former compounds exhibit improved organ specificity and a longer duration of activity at lower dosages than the corresponding non-esterified prostaglandins and are useful, inter alia, in triggering abortion, inducing labor and regulating the menstrual cycle.Type: GrantFiled: March 2, 1978Date of Patent: March 17, 1981Assignee: Schering AktiengesellschaftInventors: Werner Skuballa, Bernd Raduchel, Helmut Vorbruggen, Walter Elger, Olaf Loge, Eckehard Schillinger
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Patent number: 4237311Abstract: A compound of the general formula ##STR1## and pharmaceutically acceptable salts thereof, in which formula the groups R.sup.o are the same or different and are selected from the group consisting of hydrogen, halogen, alkyl having 1, 2 or 3 carbon atoms, and alkoxy having 1, 2 or 3 carbon atoms; R.sup.1 is hydrogen, methyl or ethyl; R.sup.2 is methyl or ethyl; R.sup.3 and R.sup.4 are the same or different and are hydrogen or an alkyl group having 1, 2 or 3 carbon atoms; and n is 0, 1 or 2. Pharmaceutical preparations containing these compounds are useful for treatment of depressive disorders.Type: GrantFiled: August 10, 1978Date of Patent: December 2, 1980Assignee: Astra Lakemedel AktiebolagInventors: Ulf M. A. Lindberg, Svante B. Ross, Seth-Olov Thorberg, Sven O. / gren
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Patent number: 4201787Abstract: Isovaleric acid ester derivatives, process for producing thereof, and insecticides containing said derivatives of the general formula I: ##STR1## wherein A represents O, NH, or CH.sub.2,R.sub.1 represents, if A is O or NH, an alkyl, an alkenyl, a haloalkyl and a haloalkenyl radical with 2-6 carbon atoms, and a radical selected from those of the general formulae II, III, IV and V: ##STR2## in which n is an integer of 1-3, R.sub.3 represents hydrogen, methyl group or chlorine atom; andif A is CH.sub.2, R.sub.1 represents an alkyl, an alkenyl, a haloalkyl and a haloalkenyl radical with 1-5 carbon atoms, whileR.sub.1 --A represents a naphthyl group bonding to the main chain at the .beta.-position, andR.sub.2 represents hydrogen or a cyano group.Type: GrantFiled: November 30, 1977Date of Patent: May 6, 1980Assignee: Dainippon Jochugiku Kabushiki KaishaInventors: Yoshio Katsuda, Yoshihiro Minamite
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Patent number: 4182761Abstract: Acyloxy-substituted aryloxyalkyl diketones, useful as anti-viral agents, are prepared either by esterification of the corresponding hydroxy-substituted compounds or by reacting a haloalkyl diketone with an alkali metal salt of an acyloxy-substituted phenol.Type: GrantFiled: June 7, 1978Date of Patent: January 8, 1980Assignee: Sterling Drug Inc.Inventors: Joseph C. Collins, Guy D. Diana
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Patent number: 4123614Abstract: The present invention relates to novel assay reagents, their composition, methods of preparation, and use in the detection and measurement of various biological systems and/or components, e.g. enzymes, antibodies, antigens, and periodate concentration. This invention in its basic form utilizes a class of compounds having, inter alia., a backbone chain, an indicator group, and vicinal oxidizable groups.Type: GrantFiled: October 18, 1976Date of Patent: October 31, 1978Assignee: Syntex (U.S.A.) Inc.Inventor: David H. Rammler
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Patent number: 4115589Abstract: 4-Amino-4-cyclohexan-1-ols are formulated into pharmaceutical compositions for the relief of pain in mammals in need of said treatment.Type: GrantFiled: May 17, 1977Date of Patent: September 19, 1978Assignee: The Upjohn CompanyInventor: Daniel Lednicer
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Patent number: 4113972Abstract: 1,1-Diphenyl-2-hydroxy-3-aminopropane derivatives are useful for their psychotropic activity and, in particular are useful as antidepressants.Type: GrantFiled: June 21, 1976Date of Patent: September 12, 1978Assignee: Beecham Group LimitedInventor: Judith Ann Clark
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Patent number: 4105792Abstract: Prostan-1-ol esters and intermediates for their preparation are described; the former compounds exhibit improved organ specificity and a longer duration of activity at lower dosages than the corresponding non-esterified prostaglandins and are useful, inter alia, in triggering abortion, inducing labor and regulating the menstrual cycle.Type: GrantFiled: May 25, 1976Date of Patent: August 8, 1978Assignee: Schering AktiengesellschaftInventors: Werner Skuballa, Bernd Raduchel, Helmut Vorbruggen, Walter Elger, Olaf Loge, Eckehard Schillinger
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Patent number: 4104043Abstract: A new series of substituted esters of 3-hydroxyindone compounds have been found to have exceptional miticidal and herbicidal activity.Type: GrantFiled: December 12, 1972Date of Patent: August 1, 1978Assignee: Union Carbide CorporationInventors: John A. Durden, Jr., Anthony A. Sousa, John F. Stephen
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Patent number: 4103025Abstract: Pharmaceutically active compounds of the formula ##STR1## wherein --OR.sub.1, --OR.sub.2, --OR.sub.3 and --OR.sub.4, which may be the same or different, each represents a free or esterified hydroxyl group and --COOR.sub.5 represents a free or esterified carboxyl group, are provided together with processes for their production and pharmaceutical compositions containing them. Compounds of formula II and III possess valuable cicatrizing and anti-inflammatory properties.Type: GrantFiled: March 17, 1977Date of Patent: July 25, 1978Assignee: Inverni Della Beffa S.p.A.Inventor: Giuseppe Mustich
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Patent number: 4098901Abstract: A compound of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof, in which formula the group R.sup.o is trifluoromethyl.Pharmaceutical compositions containing these compounds are useful for treatment of depressive disorders.Type: GrantFiled: August 30, 1976Date of Patent: July 4, 1978Assignee: Astra Lakemedel AktiebolagInventors: Ulf Henrik Anders Lindberg, Svante Bertil Ross, Seth Olov Thorberg, Sven Ove Ogren
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Patent number: 4078066Abstract: The compounds of the invention have the formula ##STR1## wherein Y is a radical of the formula ##STR2## or of the formula ##STR3## WHEREIN (CH.sub.2) is a straight or branched chain alkyl radical, n is 1-6, m is 0 or 1 and R.sup.5 and R.sup.6 may be the same or different and may be hydrogen, alkyl, arylalkyl, and R.sup.5', R.sup.5 and R.sup.6 may be the same or different and may be the nitrogen to which they are attached may be pyrrolidino, piperidino or N'-alkyl piperazino;R.sup.1, r.sup.2, r.sup.3 or R.sup.4 may be the same or different and may be hydrogen; alkyl, trifluoromethyl; alkanoyl; haloalkanoyl; alkoxycarbonyl of the formula ##STR4## wherein R is an alkyl radical; alkoxyalkyl; aminoalkanoyl of the formula ##STR5## wherein R.sup.5 and R.sup.6 are as previously defined and p is 0-3; 2-, 3-, or 4-pyridylcarbonyl; phenyl; monosubstituted phenyl wherein the substituent is alkyl, alkoxy, hydroxy, nitro, amino, or dialkylamino; alkenoyl; or aroyl; radical of 1-6 carbon atoms;R.sup.7 and R.sup.Type: GrantFiled: December 17, 1976Date of Patent: March 7, 1978Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic Peter Hauck, Joseph E. Sundeen