C=o In R Patents (Class 514/621)
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Patent number: 5534533Abstract: Novel carboxylate derivatives exhibiting phospholipase A.sub.2 inhibitory activity are disclosed, Specifically, the following compounds of the formula and pharmaceutically acceptable salts thereof are disclosed: ##STR1## wherein A is hydroxy, amino, or lower alkylamino; R.sup.1 to R.sup.12 are independently hydrogen, methyl, methoxy, or hydroxy, provided that all of R.sup.1 to R.sup.12 are not hydrogen; G.sup.1 is a single bond, or a group of --(CH.sub.2).sub.x O(CH.sub.2).sub.y -- wherein x and y are independently 0-5; G.sup.2 is a single bond, oxygen, sulfur, carbonyl, etc.; G.sup.3 is alkyl, aryl, or a group of the formula: ##STR2## wherein R.sup.13 and R.sup.14 are independently hydrogen, alkyl, aryl, etc.; or R.sup.13 and R.sup.14 may be taken together with the adjacent nitrogen atom to form a heterocyclic group or a group of the formula: ##STR3## wherein Z is a carbon atom or a nitrogen atom, J, K, and L are independently hydrogen or aryl, etc.Type: GrantFiled: September 28, 1994Date of Patent: July 9, 1996Assignee: Shionogi & Co., Ltd.Inventors: Mitsuaki Ohtani, Toshiyuki Kato, Yozo Hori
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Patent number: 5514718Abstract: Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein Q.sup.1 is halo substituted phenyl; naphthyl; indolyl; benzthiophenyl; benzofuranyl; benzyl; or fluorenyl;. . is an optional covalent bond;one of X and Y is H and the other is hydroxy or C.sub.1-6 alkoxy, or X and Y are together .dbd.O or .dbd.NOR.sup.5 ;R.sup.1 and R.sup.2 are H; C.sub.1-6 alkyl optionally substituted by hydroxy, cyano, COR.sup.c, CO.sub.2 R.sup.c, CONR.sup.c R.sup.d, or NR.sup.c R.sup.d (where R.sup.c and R.sup.d are H, C.sub.1-6 alkyl or phenyl(C.sub.0-4 alkyl) optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo and trifluoromethyl); phenyl(C.sub.1-4 alkyl) (optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halo or trifluoromethyl); COR.sup.c ; CO.sub.2 R.sup.c ; CONR.sup.c R.sup.d ; COC.sub.1-6 alkylNR.sup.c R.sup.d ; CONR.sup.c COOR.sup.d ; or SO.sub.2 R.sup.c ;R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; andR.sup.4 is phenyl optionally substituted by C.sub.1-6 alkyl, C.sub.Type: GrantFiled: April 15, 1994Date of Patent: May 7, 1996Assignee: Merck, Sharp & Dohme LimitedInventors: Richard T. Lewis, Kevin J. Merchant, Angus M. MacLeod
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Patent number: 5502053Abstract: 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 of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: August 23, 1994Date of Patent: March 26, 1996Assignee: Merck & Co., Inc.Inventors: Bruce D. Dorsey, Joel R. Huff, Susan F. Britcher
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Patent number: 5492917Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: September 29, 1993Date of Patent: February 20, 1996Assignee: Merck & Co., Inc.Inventors: Ralph A. Rivero, Peter D. Williams, Daniel F. Veber
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Patent number: 5478835Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.Type: GrantFiled: May 2, 1994Date of Patent: December 26, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
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Patent number: 5475034Abstract: Novel ester and amide derivatives of 3-benzoylphenylacetic acid are disclosed. The use of these novel derivatives and certain known derivatives in topically administrable compositions for the treatment of ophthalmic inflammatory disorders is also disclosed.Type: GrantFiled: June 6, 1994Date of Patent: December 12, 1995Assignee: Alcon Laboratories, Inc.Inventors: John M. Yanni, Gustav Graff, Mark R. Hellberg
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Patent number: 5461075Abstract: The present invention provides methods of preventing lesions due to herpes simplex infections in humans and lower animals by treatment with natural and synthetic vanilloid compounds.Type: GrantFiled: March 14, 1991Date of Patent: October 24, 1995Assignee: The Procter & Gamble CompanyInventors: Timothy P. O'Neill, Gerald B. Kasting, Thomas L. Cupps
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Patent number: 5446069Abstract: Disclosed are compounds of formula ##STR1## wherein F represents: ##STR2## or a pharmaceutically acceptable salt. The compounds are useful in treating hyperproliferative skin disease, allergic reactions and inflamation.Type: GrantFiled: March 29, 1993Date of Patent: August 29, 1995Assignee: Schering CorporationInventors: Neng-Yang Shih, Pietro Mangiaracina, Michael J. Green, Ashit K. Ganguly
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Patent number: 5434186Abstract: Compounds of the formula ##STR1## wherein X is O or CH.sub.2 ; Y is O, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, or --OCH.sub.2 C.sub.6 H.sub.4 --;Z is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.C--;f, h, k, m and t, independently, are 0 or 1;n is an integer from 1 to 12;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, or aralkyl; and A is B or --O--B, wherein B is a mono-, di- or tricyclic aromatic or heteroaromatic moiety substituted by the group --COR.sup.2, --(O).sub.t --(W).sub.s --COR.sup.2 or --(CH.dbd.CH).sub.p COR.sup.2 and which may also contain up to 4 additional substituents selected, independently, from the group consisting of halogen, cyano, lower alkyl, lower alkoxy, sulfonamido, alkanoyl, aroyl, --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, provided that no more than one of said substituents is --(Q).sub.k --(W).sub.s' --E or --(Q).sub.k --(W).sub.s" --C.sub.6 H.sub.4 --(W).sub.s'" --E, and wherein E is COR.sup.Type: GrantFiled: September 28, 1993Date of Patent: July 18, 1995Assignee: Hoffmann-La Roche Inc.Inventors: Noal Cohen, Ferdinand K. Lee, Keith A. Yagaloff
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Patent number: 5416118Abstract: Novel bicyclic amides of the formula ##STR1## wherein Ar.sup.1 and Ar.sup.2 are phenyl, R.sup.2 -substituted phenyl, heteroaryl or R.sup.2 -substituted heteroaryl, wherein R.sup.2 is 1 to 3 substituents independently selected from the group consisting of halogeno, hydroxy, lower alkyl, lower alkoxy, nitro, amino, lower alkylamino and lower dialkylamino;X, Y and Z are --CH.sub.2 --, --CH(alkyl)--, --C(alkyl).sub.2 --, --NH--, --N(alkyl)--, --O-- or --SO.sub.r, wherein r is 0, 1 or 2, and m, n and p are 0 or 1;R.sup.1 is an alkyl chain of 1 to 25 carbon atoms; an alkyl chain substituted by one or more optionally substituted phenyl or heteroaryl groups; an alkyl chain --O--, --SO.sub.r, phenylene, R.sup.2 -substituted phenylene, heteroarylene or R.sup.Type: GrantFiled: September 28, 1993Date of Patent: May 16, 1995Assignee: Schering CorporationInventors: John W. Clader, Thomas Fevig, Wayne Vaccaro, Joel G. Berger
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Patent number: 5393776Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.Type: GrantFiled: May 13, 1994Date of Patent: February 28, 1995Assignee: Bristol-Myers Squibb CompanyInventor: Bradley C. Pearce
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Patent number: 5380755Abstract: The present invention provides alkyl and alkylbenzyl ethers of substituted hydroquinones and pharmaceutical compositions containing them. The present invention further provides methods of using these compounds and compositions to inhibit monoamine oxidase, particularly monoamine oxidase B. The present invention further provides methods for the treatment of diseases involving monoamine oxidase.Type: GrantFiled: July 24, 1992Date of Patent: January 10, 1995Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Argyrios G. Arvanitis, Everett L. Scholfield
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Patent number: 5378728Abstract: Compound of the formula ##STR1## where R is CH.sub.3 (CH.sub.2).sub.m, A and B are hydrogen, a bond or --(CH.sub.2).sub.n,X is ##STR2## m is 0, 1 , 2 or 3, n is 1 , 2, or 3, R.sub.1 is hydrogen or lower alkyl, andY is --OH, --OR.sub.2 or --NR.sub.3 R.sub.4where R.sub.2, R.sub.3 and R.sub.4 are hydrogen or unsubstituted or substituted alkyl, aryl and aralkyl substituents.Type: GrantFiled: September 20, 1993Date of Patent: January 3, 1995Assignee: Sandoz Ltd.Inventors: Jeffrey Nadelson, William R. J. Simpson, Robert C. Anderson, Joginder S. Bajwa
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Patent number: 5364884Abstract: The invention relates to arginine and arginine-like compounds and to methods employing these compounds as ocular hypotensive agents. These compounds are effective when applied topically, may be used in low concentrations and are nontoxic. Additionally, the invention includes several new arginine derivatives with varying lipophilicities particularly suited for topical administration.Type: GrantFiled: January 21, 1993Date of Patent: November 15, 1994Assignee: Baylor College of MedicineInventors: Rajender S. Varma, George C. Y. Chiou
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Patent number: 5354779Abstract: New oxime ether amides of the formula (I) ##STR1## in which R has the meaning given in the description, and a plurality of processes for their preparation were described.The new oxime ether amides are used as pesticides.Type: GrantFiled: November 30, 1992Date of Patent: October 11, 1994Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Dieter Berg, Heinz-Wilhelm Dehne, Stefan Dutzmann, Christoph Erdelen
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Patent number: 5314914Abstract: A group of known naphthoquinone derivatives have been found to be useful for preventing or relieving herpes viral infections.Type: GrantFiled: February 19, 1992Date of Patent: May 24, 1994Assignee: BioMega/Boehringer Ingelheim Research Inc.Inventor: Yvan Guindon
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Patent number: 5288742Abstract: The invention concerns .alpha.,.alpha.-dialkylbenzyl derivatives of the formula I ##STR1## wherein Ar.sup.1 is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;the phenylene group may optionally bear one or two substituents R.sup.3 ;each of R.sup.1 and R.sup.2, which may be the same or different, is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, fluoro-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, provided that both of R.sup.1 and R.sup.2 are not methyl or fluoromethyl; andQ is cyano, amino, nitro, formyl, (1-4C)alkoxy, thiazolyl or (2-4C)alkanoyl;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.Type: GrantFiled: March 18, 1992Date of Patent: February 22, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Philip N. Edwards, David Waterson
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Patent number: 5280045Abstract: The subject invention involves compositions comprising 4-(3,5-bis(1,1-dimethylethyl-4-hydroxyphenyl)-4-oxobutanamide, or 4-(3,5-bis-(1,1-dimethylethyl)-4-hydroxyphenyl)-4-oxobutanoic acid and pharmaceutically-acceptable salts thereof, and a pharmaceutically-acceptable carrier. The subject invention also involves methods for treating diseases characterized by inflammation and/or pain, such as rheumatoid arthritis and osteoarthritis, in humans or lower animals by administration of a safe and effective amount of this compound to the human or lower animal in need of such treatment.Type: GrantFiled: October 1, 1992Date of Patent: January 18, 1994Assignee: The Procter & Gamble CompanyInventors: Roy L. M. Dobson, Kenneth R. Wehmeyer, Steven P. Sirko, Benjamin F. Floyd
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Patent number: 5250570Abstract: The invention concerns novel phenoxy- and phenylthio-acetyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.Type: GrantFiled: December 31, 1992Date of Patent: October 5, 1993Assignee: Imperial Chemical Industries PLCInventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Slater
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Patent number: 5225436Abstract: Certain aryl substituted naphthalene, benzoxepine, benzazepine and henzocycloheptene derivatives are disclosed. The compounds are useful in treating hyperproliferative skin disease, allergic reactions and inflammation.Type: GrantFiled: October 15, 1991Date of Patent: July 6, 1993Assignee: Schering CorporationInventors: Neng-Yang Shih, Pietro Mangiaracina, Michael J. Green, Ashit K. Ganguly
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Patent number: 5223539Abstract: The present invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Z can be: ##STR2## wherein R.sup.3 is alkyl having 1 to 6 carbon atoms and, when n is greater than 1, each R.sup.3 can be the same or different; and n is an integer from 1 to 3;R.sup.1 and R.sup.2 can each independently be hydrogen, straight or branched chain alkyl, or cycloalkyl having 3 to 8 carbon atoms which can optionally be substituted at one or more positions by alkyl of 1 to 6 carbon atoms; X is oxygen, sulfur, NR.sup.4, wherein R.sup.4 is hydrogen or alkyl having 1 to 4 carbon atoms, C.dbd.O, CHOH, or CH.sub.2 ; Y is hydrogen, alkoxy, halogen, alkyl, or hydroxy; and m is an integer from 0 to 3. The compounds are antagonists of platlet-activating factor (PAF).Type: GrantFiled: November 21, 1991Date of Patent: June 29, 1993Assignee: G. D. Searle & Co.Inventors: Roger A. Nosal, Michael A. Stealey, Richard M. Weiser
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Patent number: 5221691Abstract: Fungicidal compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted aryloxyalkyl, optionally substituted heterocyclyloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heterocyclyl, optionally substituted aryloxy, optionally substituted heterocyclyloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.sup.3).sub.Type: GrantFiled: January 29, 1992Date of Patent: June 22, 1993Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Paul J. de Fraine, Ian R. Matthews
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Patent number: 5218000Abstract: A compound of formula I optionally in the form of an acid addition salt ##STR1## in which formula: A represents a substituent which is: hydroxyl, O-alkyl, O-cycloalkyl, O-alkenyl, O-aryl, O-aralkyl, O-carbamate, O-carbonate, O-acyl or halogena is 0-5;the substituents A are identical or different when a is more than 1;B represents a C.sub.1 -C.sub.6 aliphatic hydrocarbon group optionally carrying one or more of the substituents: hydroxyl, amino, halogen, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, aryloxy or carboalkoxy and optionally comprising one or more sites of unsaturation and/or one or more carbonyl groups or ketal derivatives thereof;b is 0 or 1;c, d, f and h, which may be identical or different, are 2, 3, 4, 5 or 6; andi is 0 or 1D, E and F, which may be identical or different, represent hydrogen or C.sub.1 -C.sub.Type: GrantFiled: April 18, 1990Date of Patent: June 8, 1993Assignee: National Research Development CorporationInventors: Peter N. R. Usherwood, Barrie W. Bycroft, Ian S. Blagbrough, Alan J. Mather
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Patent number: 5204370Abstract: The present invention provides novel substituted anthraquinones having the formula ##STR1## wherein R.sub.1 and R.sub.2 are independently H, C.sub.1 -C.sub.10 alkyl, aryl, arylalkyl, alkylaryl;n and m are independently 1, 2, or 3;A is Halogen, OH, alkoxy, OCO(NR.sub.3 R.sub.4), S--C(NH.sub.2).dbd.NR.sub.5, or when m=1, comprises an oxirane ring with the adjacent oxygen atom;R.sub.3, R.sub.4, and R.sub.5 are independently H, alkyl, or aryl;X is H, OH, NR.sub.6 R.sub.7, Cl, Br, I, F, alkyl, aryl, alkoxy, aryloxy, COOR.sub.8, or CONR.sub.9 R.sub.10 ; andR.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are independently H, lower alkyl, or aryluseful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.Type: GrantFiled: November 5, 1990Date of Patent: April 20, 1993Assignee: Sphinx Pharmaceuticals CorporationInventors: Jack B. Jiang, Mary G. Johnson
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Patent number: 5153226Abstract: The present invention are novel amino acid amide compounds of the following general formula which inhibit the enzyme acylcoenzyme A:cholesterol acyltransferase: ##STR1## wherein R is phenyl or 1- or 2-naphthyl which are unsubstituted or may be substituted; R.sub.1 is hydrogen or a straight or branched alkyl group having from 1 to 6 carbon atoms; R.sub.2 is hydrogen, an aliphatic group, an aromatic group, an aralkyl or diarylalkyl group or R.sub.1 and R.sub.2 form a carbocyclic group; R.sub.3 is hydrogen, an aliphatic group, an aralkyl group wherein the alkyl moiety may contain a carbocyclic entity; R.sub.4 is hydrogen, an aliphatic group, SO.sub.2 R.sub.14, --C(.dbd.S)NHR.sub.15, --CO.sub.2 R.sub.15, --COR.sub.18, or --C(.dbd.O)NHR.sub.15 wherein R.sub.14 is morpholino, phenyl or substituted phenyl; R.sub.15 is an alkyl group, phenyl or phenylalkyl wherein the phenyl group may be substituted; and R.sub.18 is the same is R.sub.15 or is halo-substituted alkyl, 9-fluoroenylmethylene or pyrrolidino.Type: GrantFiled: July 30, 1990Date of Patent: October 6, 1992Assignee: Warner-Lambert CompanyInventors: Alexander W. Chucholowski, Mark W. Creswell, William H. Roark, Ila Sircar
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Patent number: 5145874Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.Type: GrantFiled: February 25, 1991Date of Patent: September 8, 1992Assignee: The Upjohn CompanyInventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased, by Vera M. Wallach, legal representative
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Patent number: 5135940Abstract: Compounds of the Formulae: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reacting substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: March 20, 1991Date of Patent: August 4, 1992Assignee: Merck Frosst Canada, Inc.Inventors: Patrice C. Belanger, Joshua Rokach, Rejean Fortin, Christiane Yoakim, Yvan Guindon
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Patent number: 5126371Abstract: Novel diarylacetylenes of the formula I ##STR1## where A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have the meanings stated in the description, are useful for the treatment of disorders.Type: GrantFiled: August 20, 1990Date of Patent: June 30, 1992Assignee: BASF AkteingesellschaftInventors: Hans-Heiner Wuest, Fritz-Frieder Frickel, Axel Nuerrenbach
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Patent number: 5124354Abstract: A composition suitable for topical application to mammalian skin or hair for inducing, maintaining or increasing hair growth comprises:(i) a special protein tyrosine kinase inhibitor; and(ii) a cosmetically acceptable vehicle for the inhibitor.Type: GrantFiled: June 11, 1990Date of Patent: June 23, 1992Assignee: Chesebrough Pond's USA Co., Division of Conopco, Inc.Inventor: Martin R. Green
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Patent number: 5112868Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.Type: GrantFiled: May 2, 1990Date of Patent: May 12, 1992Assignee: Warner-Lambert CompanyInventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
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Patent number: 5098895Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radial; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.Type: GrantFiled: March 30, 1990Date of Patent: March 24, 1992Assignee: Centre International de Recherches Dermatologiques (C.I.R.D.)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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Patent number: 5066680Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is aryl which may have one or more suitable substituent(s),R.sup.2 is aryl which may have one or more suitable substituent(s), lower alkyl or cyclo(lower)alkyl,R.sup.3 is hydrogen, hydroxy, halogen, lower alkenyl, amino or protected amino,R.sup.4 is a group of the formula: ##STR2## wherein R.sup.5 is lower alkyl which may have one or more suitable substituent(s), cyclo(lower)alkyl, aryl, ar(lower)alkyl which may have one or more suitable substituent(s), andR.sup.6 is hydrogen or lower alkyl; or N-containing heterocyclic group which may have one or more suitable substituent(s), andA is lower alkylene or lower alkynylene, in which R.sup.1 and R.sup.2 may be linked through oxygen atom, their preparation and use in treatment of dysuria, and starting materials for their preparation.Type: GrantFiled: February 5, 1990Date of Patent: November 19, 1991Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Kazuo Okumura, Kazuhiko Take, Kazunori Tsubaki
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Patent number: 5064861Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of Ar-O- and aryl, polyaryl and condensed polyaryl unsubstituted or substituted and heterocycle unsubstituted or substituted, Ar is aryl of 6 to 14 carbon atoms unsubstituted or substituted, heteroaryl unsubstituted or substituted and heterocyclic unsubstituted or substituted, W is selected from the group comsisting of --(CH.sub.2).sub.n.sbsb.1 --or --(CH.sub.2).sub.n.sbsb.2 --NY--(CH.sub.2).sub.n.sbsb.3, n.sub.1, n.sub.2 and n.sub.3 are individually integers from 2 to 6, Y is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms, aryl of 6 to 12 carbon atoms and aralkyl of 7 to 14 carbon atoms unsubstituted or substituted, --COOAlk and --COR.sub.2, Alk is alkyl of 1 to 12 carbon atoms, R.sub.Type: GrantFiled: December 21, 1989Date of Patent: November 12, 1991Assignee: Roussel UclafInventors: Jean-Louis Brayer, Laurent Taliani, Jean Tessier
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Patent number: 5047420Abstract: Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.Type: GrantFiled: August 21, 1989Date of Patent: September 10, 1991Assignee: Merck & Co., Inc.Inventors: Donald W. Graham, Tesfaye Biftu, John C. Chabala, Michael N. Chang, Yuan-Ching P. Chiang, Kathryn L. Thompson, Shu S. Yang
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Patent number: 5047410Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.Type: GrantFiled: July 12, 1989Date of Patent: September 10, 1991Assignee: Istituto de Angeli S.p.A.Inventors: Arturo Donetti, Marco Turconi, Massimo Nicola, Rosamaria Micheletti
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Patent number: 5034418Abstract: A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--N4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.Type: GrantFiled: June 9, 1989Date of Patent: July 23, 1991Assignee: Eisai Co., Ltd.Inventors: Youji Yamagishi, Kozo Akasaka, Takeshi Suzuki, Mitsuaki Miyamoto, Kouji Nakamoto, Kazuo Okano, Shinya Abe, Hironori Ikuta, Kenji Hayashi, Hiroyuki Yoshimura, Tohru Fujimori, Koukichi Harada, Isao Yamatsu
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Patent number: 5032617Abstract: A method for sensitizing hypoxic tumor cells to radiation using derivatives of benzamide are disclosed. Some of the compounds useful in theREFERENCE TO GOVERNMENT GRANT OR CONTRACTThe invention described herein was made in the course of work under grant or contract from the National Institutes of Health.Type: GrantFiled: May 18, 1989Date of Patent: July 16, 1991Assignee: SRI InternationalInventors: William W. Lee, Edward W. Grange, J. Martin Brown
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Patent number: 4992574Abstract: A compound of the formula ##STR1## wherein R.sup.1 is hydroxy, lower-alkoxy, amino, mono- or di-lower-alkylamino;R.sup.2 is hydrogen, alkyl, akoxy or halogen;R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.11 and R.sup.12 independently are hydrogen or lower-alkyl;R.sup.3 and R.sup.5 taken together are methylene or hydroxymethylene;R.sup.7, R.sup.8, R.sup.9 and R.sup.10 independently are hydrogen or lower-alkyl;R.sup.11 and R.sup.12 taken together are oxo or spiro-cyclo-lower alkyl; or R.sup.11 is hydrogen and R.sup.12 is hydroxy or acetoxy; and one of the residues R.sup.13 and R.sup.14 is hydrogen and the other is lower-alkyl or trifluoromethyl, as well as physiologically compatible salts of carboxylic acids of formula I, which can be used as medicaments, especially for the treatment of neoplasms, acne and psoriasis, are described. The compounds of the invention can be prepared by the synthesis of the C(R.sup.13).dbd.C(R.sup.Type: GrantFiled: October 27, 1988Date of Patent: February 12, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr
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Patent number: 4983633Abstract: Amide-compounds represented by the formula (I): ##STR1## wherein R.sub.1 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino which can be substituted by lower alkyl, nitro, cyano, sulfamoyl which can be substituted by lower alkyl, R.sub.2 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino, nitro, wherein R.sub.1 and R.sub.2 can be combined to form methylenedioxy, R.sub.3 means hydrogen, lower alkyl, halogen, or amino, R.sub.4 and R.sub.5 may be the same or different and each represents lower alkyl or wherein R.sub.4 and R.sub.Type: GrantFiled: September 2, 1988Date of Patent: January 8, 1991Assignee: Hokuriku Pharmaceutical Co., Ltd.Inventors: Yasuo Itoh, Hideo Kato, Eiichi Koshinaka, Nobuo Ogawa, Hiroyuki Nishino, Jun Sakaguchi
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Patent number: 4981872Abstract: Prostaglandin derivatives having an oxo group at specified positions in the .alpha. side chain have a variety of physiological effects, notably a strong anti-ulcer activity accompanied by a limited ability to inhibit blood platelet aggregation.Type: GrantFiled: January 15, 1988Date of Patent: January 1, 1991Assignee: Sankyo Company LimitedInventors: Koichi Kojima, Shigeo Amemiya, Kazuo Koyama, Keiichi Tabata, Nobuyoshi Iwata
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Patent number: 4971997Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, or --CH.dbd.CH--;wherein Z is OR.sup.1 or --NR.sup.4 R.sup.5 ;wherein R.sup.1 is hydrogen, lower alkyl, or a pharmaceutically acceptable cation;wherein R.sup.2 is H, --CH.sub.3 or --C.sub.2 H.sub.5 ;wherein R.sup.3 is OH, H or .dbd.O;wherein R.sup.4 and R.sup.5 may independently be hydrogen, or lower alkyl having 1-6 carbon atoms, or R.sup.4 and R.sup.5 may act together with N to form a cyclic amide of the formula: ##STR2## wherein n is an integer from 4-5; and m is an integer from 0-4. More particularly, this invention relates to compounds of the above formula which have utility as LTB.sub.4 antagonists.Type: GrantFiled: August 7, 1989Date of Patent: November 20, 1990Assignee: G. D. Searle & Co.Inventors: Stevan W. Djuric, Richard A. Haack, Stella S. Yu
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Patent number: 4959366Abstract: A series of [N-alkyl-N-(nitro-, alkylsulphonamido, or amino-phenalkyl)amino]-alkyl, alkoxy or alkylthio phenyl derivatives having utility as anti-arrhythmic agents.Type: GrantFiled: April 29, 1987Date of Patent: September 25, 1990Assignee: Pfizer Inc.Inventors: Peter E. Cross, Geoffrey N. Thomas, John E. Arrowsmith
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Patent number: 4950669Abstract: The growth rate of an animal is stimulated by administering to the animal a growth promoting amount of a compound of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, are each selected from the group consisting of hydrogen, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms and halogen; X is selected from carbonyl and a ketal group of the formula ##STR2## wherein R.sub.6 and R.sub.7, which can be the same or different, are each selected from hydrogen and alkyl having 1 to 3 carbon atoms; A is a linear or branched alkylene having from 1 to 8 carbon atoms; and R.sub.8 and R.sub.9, which can be the same or different, are each selected from the group consisting of hydrogen, alkyl having 1 to 4 carbon atoms, or 2-hydroxy-alkyl wherein the alkyl group has 2 to 4 carbon atoms, or R.sub.8 and R.sub.Type: GrantFiled: July 19, 1988Date of Patent: August 21, 1990Assignee: Cometec s.r.l.Inventors: Aldo Garzia, Umberto Bucci
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Patent number: 4948812Abstract: Compounds of formula ##STR1## (the substituents R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are explained in the specification) may be prepared by conventional methods.Owing to their favorable activity profile the compounds may advantageously be used to treat certain heart and circulatory disorders.Type: GrantFiled: November 25, 1987Date of Patent: August 14, 1990Assignee: Boehringer Ingelheim KGInventors: Herbert Koppe, Franz Esser, Walter Kobinge, Christian Lillie
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Patent number: 4940696Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.Type: GrantFiled: November 16, 1987Date of Patent: July 10, 1990Assignee: Centre International de Recherches Dermatologioues (CIRD)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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Patent number: 4939163Abstract: This invention provides certain 4-substituted benzamide derivatives, their pharmaceutical formulations, and their use as anticonvulsant agents.Type: GrantFiled: April 10, 1989Date of Patent: July 3, 1990Assignee: Eli Lilly and CompanyInventors: Edward E. Beedle, David W. Robertson
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Patent number: 4931469Abstract: The specification describes and claims methods of controlling acarine pests by application of a compound of Formula (I), methods of controlling arthropod pests by application of a compound of Formula (IA), compounds of Formula (IA) per se, pesticidal compositions comprising a compound of Formula (IA), and processes for preparing a compound of Formula (IA).Type: GrantFiled: June 8, 1988Date of Patent: June 5, 1990Assignee: Burroughs Wellcome Co.Inventors: Malcolm H. Black, Robert J. Blade
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Patent number: 4918108Abstract: An antibacterial substance which does not have optimum absorbability and is administered parentally into tissue, is administered to a host in conjunction with a benzylamine derivative of the formula ##STR1## wherein R.sub.1 is hydroxyl in the 2- or 4-position or amino in the 2-position;R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms; andR.sub.3 is cyclohexyl optionally substituted by hydroxyl;or a non-toxic, pharmacologically acceptable acid addition salt thereof, to improve the absorption of the parenterally administered antibacterial substance.Type: GrantFiled: June 29, 1987Date of Patent: April 17, 1990Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Otto Kern, Franz Wilhelm, Ernst Salamon
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Patent number: RE34440Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radial; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.Type: GrantFiled: July 16, 1992Date of Patent: November 9, 1993Assignee: Centre International de Recherches Dermatologiques (C.I.R.D.)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
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Patent number: RE34805Abstract: A benzonaphthalene compound has the formula ##STR1## wherein R.sub.1 represents ##STR2## or (ii) --CH.sub.2 OH; R.sub.6 represents ##STR3## or OR.sub.7 wherein R.sub.7 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl or polyhydroxyalkyl, r' or r" represent hydrogen, lower alkyl, mono or polyhydroxyalkyl, aryl or a residue of an amino acid or a sugar, or together form a heterocycle; R.sub.2 represents hydrogen, alkyl having 1-15 carbon atoms, alkoxy having 1-4 carbon atoms or a cycloaliphatic radical; R.sub.3 represents hydrogen, hydroxy, alkyl having 1-4 carbon atoms, alkoxy having 1-10 carbon atoms, a cycloaliphatic radical, a thiocycloaliphatic radical or --O--Si(CH.sub.3).sub.2 --R.sub.8 wherein R.sub.8 represents lower alkyl; and R.sub.4 and R.sub.5 represent hydrogen, lower alkyl, hydroxy or lower acyloxy.This compound is useful in the topical and systemic treatment of dermatologic diseases and in the treatment of the degeneration of conjunctive tissues.Type: GrantFiled: July 10, 1992Date of Patent: December 6, 1994Assignee: Centre International de Recherches Dermatologiques (CIRD)Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon