Polycyclo Ring System (e.g., Naphthols, Etc.) Patents (Class 514/732)
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Patent number: 5869067Abstract: The present invention relates to new aromatic compounds, to their preparation and to their use in human and veterinary medicine and in cosmetic compositions.Type: GrantFiled: September 26, 1994Date of Patent: February 9, 1999Assignee: Centre International De Recherches Dermatologiques Galderma (CIRD Galderma)Inventors: Jean-Phillippe Rocher, Jean-Michel Bernardon
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Patent number: 5859067Abstract: Use of a compound of formula (I), wherein Ar is an aromatic ring system comprising one or more optionally substituted phenyl rings optionally linked to or fused with one or more other optionally substituted phenyl rings or one or more 5 or 6-membered, optionally substituted heterocyclic rings wherein the heteroatom is oxygen; and wherein the ring system comprises 1-4 phenyl rings and wherein Ar can be linked to another Ar via a group X wherein the Ar is independently selected; where X is optionally substituted C.sub.1-20 alkylene, C.sub.2-20 alkenylene or C.sub.2-20 alkynylene; R is hydrogen; C.sub.1-20 alkenyl, C.sub.2-20 alkynyl, C.sub.2-20 alkanoyl, C.sub.2-20 alkynoyl, each of which can be optionally substituted; R.sub.1 is independently selected and is hydrogen; optionally substituted C.sub.1-12 alkyl, C.sub.2-12 alkenyl, C.sub.2-12 alkynyl; --COOR'--NR'R', halogen, --OR', --COR', --CONR'R', .dbd.O, --SR', --SO.sub.3 R', --SO.sub.2 NR'R', --SOR', --SO.sub.2 R', --NO.sub.Type: GrantFiled: November 12, 1997Date of Patent: January 12, 1999Inventors: Basil Don Roufogalis, Colin Charles Duke, Qian Li
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Patent number: 5739118Abstract: Methods of introducing genetic material into cells of an individual and compositions and kits for practicing the same are disclosed. The methods comprise the steps of contacting cells of an individual with a genetic vaccine facilitator and administering to the cells, a nucleic acid molecule that is free of retroviral particles. The nucleic acid molecule comprises a nucleotide sequence that encodes a protein that comprises at least one epitope that is identical or substantially similar to an epitope of a pathogen antigen or an antigen associated with a hyperproliferative or autoimmune disease, a protein otherwise missing from the individual due to a missing, non-functional or partially functioning gene, or a protein that produce a therapeutic effect on an individual. Methods of prophylactically and therapeutically immunizing an individual against HIV are disclosed. Pharmaceutical compositions and kits for practicing methods of the present invention are disclosed.Type: GrantFiled: April 1, 1994Date of Patent: April 14, 1998Assignees: Apollon, Inc., The Trustees of the University of PennsylvaniaInventors: Richard A. Carrano, Bin Wang, David B. Weiner
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Patent number: 5733929Abstract: There is disclosed a pharmaceutical composition for treating or preventing allergic rhinitis which comprises a quinone or hydroquinone derivative having thromboxane A.sub.2 receptor antagonism. This compound is hardly inactivated by in vivo metabolism and can maintain its effective blood level for a long term and exhibit excellent pharmacological activity in a low dose.Type: GrantFiled: January 30, 1996Date of Patent: March 31, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Yasuko Ashida, Tatsumi Matsumoto
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Patent number: 5716624Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): ##STR1## in which X is one of the radicals: ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: December 15, 1994Date of Patent: February 10, 1998Assignee: C.I.R.D. GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5550145Abstract: An antimicrobial composition comprising an antimicrobially effective amount of a combination of: A) a monoglyceride of lauric acid, a monoglyceride of monomyristic acid or a mixture of these monoglycerides, and B) at least one chemical substance selected from the following groups: i) local anesthetics of the amide type; ii) carbamide, iii) antibacterial substances in the form of steroid antibiotics, imidazole derivatives or nitroimidazole derivatives, and iv) diols with 3-6 carbon atoms, and C) optionally, a conventional physiologically acceptable carrier and/or physiologically acceptable additives. A process for the preparation of this composition by heating (A) to the transition temperature of the lipid, adding (B), and optionally (C), and cooling the mixture to form a solid lipid crystal composition. Use of the composition for the preparation of a dermatological preparation for combatting bacteria and fungi or as a preservative additive in a cosmetic product, a food product, or a medical product.Type: GrantFiled: September 27, 1994Date of Patent: August 27, 1996Assignee: Bioglan ABInventors: Karin Olund, Lena-Karin L utz, Rickard Bryland, .ANG.ke Lindahl
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Patent number: 5506271Abstract: A method for treating a papilloma virus infection comprising topically administering hypericin which is effective to inhibit the replication, growth and/or the infectivity of the virus. The papilloma viruses include those capable of causing benign warts or a malignancy such as human papilloma virus-1 (HPV-1), HPV-2, HPV-6, HPV-11, HPV-16 and HPV-18.Type: GrantFiled: August 10, 1993Date of Patent: April 9, 1996Assignee: New York UniversityInventors: Daniel Meruelo, Gad Lavie
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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: 5480913Abstract: Disclosed are novel classes of anti-androgens including dihydrophenanthrene derivatives, their method of synthesis and their use in treating disorders associated with excessive androgenic activities.Type: GrantFiled: May 3, 1993Date of Patent: January 2, 1996Assignee: Arch Development CorporationInventors: Shutsung Liao, John Pataki, Ronald G. Harvey
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Patent number: 5476860Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.Type: GrantFiled: December 8, 1993Date of Patent: December 19, 1995Assignee: Centre International de Recherches Dermatologiques (CIRD Galderma)Inventor: Jean-Michel Bernardon
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Patent number: 5447960Abstract: A plant fungicide method comprises applying to the locus of a plant pathogen a fungicidally effective amount of a compound of formula (I) ##STR1## or a salt or a complex thereof, wherein: R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.8 are independently H, halo, NO.sub.2, (C.sub.1 -C.sub.4) alkyl, or halo(C.sub.1 -C.sub.4) alkyl;R.sup.3', R.sup.4', R.sup.5', R.sup.3", R.sup.4", and R.sup.5" are independently H, halo, OH, or CH.sub.3, provided that at least one is OH;R.sup.6 ' and R.sup.6 " are independently H or OH.Type: GrantFiled: October 4, 1993Date of Patent: September 5, 1995Assignee: DowElancoInventors: Deirdre M. Sinnott, Hak-Fun Chow, Robert J. Ehr, Steven D. Lubetkin, Stephen E. Bales, Muthiah N. Inbasekaran
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Patent number: 5441983Abstract: A method for inhibiting cell infection by an enveloped virus, by administering to an infection site, a therapeutically effective amount of a calix(n)arene compound derivatized, at its ring positions meta to the bridge attachements to the ring, with polar substitutent having a terminal carboxylate, phosphate, or sulfonate groups, including esters and amides which are cleavable in vivo. The compound may be administered orally, or topically, e.g., for treatment of herpes virus.Type: GrantFiled: August 6, 1992Date of Patent: August 15, 1995Assignee: Genelabs IncorporatedInventors: Kou M. Hwang, You M. Qi, Su-Ying Liu, William Choy, Jen Chen
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Patent number: 5409959Abstract: A method of inhibiting thrombus formation in a mammalian subject. The method involves administering to the subject a therapeutically effective dose of a calix(n)arene compound derivatized, at its ring positions meta to the bridge attachments to the ring, with polar substituents having terminal sulfonate groups, including esters and amides which are cleavable in vivo.Type: GrantFiled: August 6, 1992Date of Patent: April 25, 1995Assignee: Genelabs IncorporatedInventors: Kou M. Hwang, You M. Qi, Su-Ying Liu, Thomas C. Lee, William Choy, Jen Chen
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Patent number: 5326788Abstract: The present invention provides compositions, articles and methods for inactivating viruses present in whole blood and other body fluids. The method comprises contacting the body fluids with an effective amount of an antiviral compound. Blood bags, vacuum blood tubes, condoms, spermicidal jellies and vaginal lubricants containing effective amounts of the antiviral compounds are also provided.Type: GrantFiled: July 1, 1992Date of Patent: July 5, 1994Assignee: New York UniversityInventors: Daniel Meruelo, Gad Lavie
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Patent number: 5256700Abstract: Carnosic acid is obtained by extracting sage and rosemary with an apolar solvent, contacting the extract with an adsorbent material to separate carnosic acid from apolar compounds of the extract, desorbing the adsorbent with a polar solvent and then evaporating the solvent to obtain a residue containing carnosic acid. The carnosic acid contained in the residue may be purified by crystallizing it from the residue.Type: GrantFiled: September 18, 1991Date of Patent: October 26, 1993Assignee: Nestec S.A.Inventors: Robert Aeschbach, Georges Philippossian
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Patent number: 5248494Abstract: A lenitive composition is provided for application to the skin of an anthralin patient for reducing anthralin-induced inflammation and the staining associated with anthralin use. The lenitive composition is a single phase aqueous treating solution comprising an organic amine and a film-forming agent dissolved within a nontoxic dermatologically acceptable carrier. The organic amine is selected from the group consisting of lower alkyl and lower alkanol primary, secondary and tertiary amines and comprises about 1 to 25 percent by weight of the single phase aqueous treating solution. The solution is topically applied to the anthralin-treated areas so as to completely cover the treated areas. The solution is applied before or after anthralin wash off, preferably in the form of a fine spray or mist.Type: GrantFiled: June 10, 1992Date of Patent: September 28, 1993Assignee: Young Pharmaceuticals Inc.Inventors: John E. Kuleza, Lawrence Clifford M., Sam Shuster
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Patent number: 5215924Abstract: The invention relates to a method for determining an ion in an aqueous sample. The method involves contacting the sample with a water immiscible material including an ionophore, a pH indicator and a compound which stabilizes sensitivity of the assay. The ion reacts with the ionophore in the water immiscible material, releasing a proton which reacts with the pH indicator generating a color change which is representative of the ion to be measured. The stabilizing compound stabilizes this change. Also described are compositions including the three recited elements, and various new compounds useful as the stabilizer.Type: GrantFiled: May 10, 1991Date of Patent: June 1, 1993Assignee: Boehringer Mannheim GmbHInventors: Walter Rittersdorf, Werner Guethlein, Detlef Thym, Peter Vogel
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Patent number: 5208263Abstract: Disclosed are novel classes of anti-androgen including dihydrophenanthrene derivatives, their method of synthesis and their use in treating disorders associated with excessive androgenic activities.Type: GrantFiled: September 27, 1989Date of Patent: May 4, 1993Assignee: Arch Development CorporationInventors: Shutsung Liao, John Pataki, Ronald G. Harvey
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Patent number: 5204373Abstract: The invention relates to novel farnesylated tetrahydro-naphthalenols, that inhibit HMGR activity which results in a decrease in serum total cholesterol, a decrease in LDL cholesterol levels, and inhibition of LDL oxidation. The farnesylated tetrahydro-naphthalenols of the present invention are thus useful for cholesterol/lipid lowering in cases of hypercholesterolemia, hyperlipidemia, and atherosclerosis.Type: GrantFiled: August 26, 1991Date of Patent: April 20, 1993Assignee: Bristol-Myers Squibb CompanyInventor: Bradley C. Pearce
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Patent number: 5177108Abstract: Aryloxyalkanol derivatives having the formulaAr--O(CH.sub.2).sub.n OHwherein n is an integer from 3 to 8 and Ar is (1) 1- or 2-naphthylenyl, (2) phenyl optionally substituted by from 1 to 3 C.sub.1-4 lower alkyl groups, or (3) a diphenyl moiety of structure ##STR1## wherein Y is a bond, CH.sub.2 or CH.sub.2 O, and esters thereof have antiretrovirus activity and are effective in a method for treatment of a retrovirus infection.Type: GrantFiled: November 8, 1991Date of Patent: January 5, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Roger A. Parker, Sai P. Sunkara
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Patent number: 5158977Abstract: A 5,6,7,8-tetrahydro-1-naphthalenol derivative of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 represent lower alkyl,R.sub.5 and R.sub.6 represent hydrogen or lower alkyl,R represents hydrogen, C.sub.1 -C.sub.18 alkyl, C.sub.2 -C.sub.18 alkyl substituted by one or more hydroxyl groups, C.sub.3 -C.sub.18 alkenyl, C.sub.2 -C.sub.18 acyl, benzyl, benzoyl, carboxyl and carboxylic salts of an alkali or alkaline earth metal or of an organic amine.The derivative is useful as an antioxidant in cosmetic compositions and in pharmaceutical compositions for the preventive treatment of cutaneous inflammations and allergies or certain forms of cancer.Type: GrantFiled: June 7, 1991Date of Patent: October 27, 1992Assignee: L'OrealInventors: Jean Maignan, Gerard Malle, Andre Deflandre, Gerard Lang
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Patent number: 5149718Abstract: The present invention provides compositions, articles and methods for inactivating viruses present in whole blood and other body fluids. The method comprises contacting the body fluids with an effective amount of an antiviral compound. Blood bags, vacuum blood tubes, condoms, spermicidal jellies and vaginal lubricants containing effective amounts of the antiviral compounds are also provided.Type: GrantFiled: January 19, 1989Date of Patent: September 22, 1992Assignee: New York UniversityInventors: Daniel Meruelo, Gad Lavie
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Patent number: 5112869Abstract: This invention concerns compounds having the structure: ##STR1## wherein each of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.2', R.sup.3', R.sup.4', and R.sup.5', is independently hydrogen (--H), or a hydroxyl (--OH), methoxy (--OMe), methyl (--Me), carboxaldehyde (--CHO) or phenylformazen (Ph--N.dbd.CH--) group.This invention also provides a novel process of synthesizing the compounds of the subject invention, including intermediate compounds useful in the process.The present invention also provides pharmaceutical compositions comprising a pharmaceutically effective amount of a compound according to the subject invention and a pharmaceutically acceptable carrier. Finally, the invention provides spermicidal methods and methods of killing or of retarding the proliferation of, cancer cells.Type: GrantFiled: April 4, 1989Date of Patent: May 12, 1992Assignee: Sloan-Kettering Institute For Cancer ResearchInventors: Kyoichi A. Watanabe, Tsann-Long Su, Jai-Tung Huang
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Patent number: 5108733Abstract: Spontaneous aspecific coloration in so-called Trinder reagents which can alter subsequent colorimetric determinations is inhibited by adding compounds of the chelating agent class to the solution. The resultant compositions contain a peroxidase enzyme, a phenylpyrazone derivative, a compound of phenolic or aromatic amine structure and a stabilizer. Preferred stabilizers are ethylenediaminetetraacetic acid (EDTA) and diethylenetriaminepentaacetic acid (DTPA).Type: GrantFiled: August 30, 1990Date of Patent: April 28, 1992Assignees: Instrumentation Laboratory S.p.A., 501 Instrumentation Laboratory S.p.A.Inventors: Dario Frontini, Maurizio D'Alterio
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Patent number: 5061486Abstract: The invention provides novel compositions for topical application, e.g. for the treatment of psoriasis, comprising finely divided dithranol dispersed in a thickened aqueous medium.Type: GrantFiled: April 25, 1990Date of Patent: October 29, 1991Assignee: Drythanol Ltd.Inventor: Martin Whitefield
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Patent number: 5049589Abstract: The invention relates to antiviral compositions of matter containing as active ingredient hypericin or pseudohypericin. The novel compositions are of special use in the treatment of, and alleviation of symptons of various diseases caused by viruses such as vesicular stomatitis, influenza, herpes simplex, HSV-1 and HSV-2. The mode of activity seems to be by inhibition of RNA synthesis and interfering with virus replication. The pharmaceutical compositions can be applied by a variety of routes. Topical applications have proved to be effective against a variety of viral afflictions.Type: GrantFiled: December 19, 1989Date of Patent: September 17, 1991Assignee: Yeda Research and Development Company, Ltd.Inventors: David Lavie, Michel Revel, Dalia Rotman, Vincent Vande Velde
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Patent number: 5047435Abstract: Pharmaceutical formulations comprising aromatic polycyclic dione compounds useful for treating mammals suffering from diseases caused by retroviruses are disclosed herein. A method for treating mammals suffering from retrovirus infections is also disclosed.Type: GrantFiled: March 27, 1989Date of Patent: September 10, 1991Assignees: New York University, Yeda Research and Development Company, Ltd.Inventors: David Lavie, Daniel Meruelo, Gad Lavie, Michel Revel, Vincent Vande Velde, Dalia Rotman
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Patent number: 5034420Abstract: This invention relates to an anthralin composition having improved stability. The invention further relates to a method for increasing the stability of anthralin in dermatological compositions by incorporating therein a stability enhancing amount of an acid stable anionic surfactant and a water soluble antioxidant.Type: GrantFiled: May 17, 1989Date of Patent: July 23, 1991Assignee: Bristol-Myers Squibb Co.Inventor: Jonas C. T. Wang
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Patent number: 5019569Abstract: The present invention is directed to the topical administration of a retinoid-containing pharmaceutical composition for reversing the effects of glucocorticoid-induced skin atrophy.Type: GrantFiled: August 31, 1989Date of Patent: May 28, 1991Assignee: Ortho Pharmaceutical CorporationInventors: Albert M. Kligman, James A. Mezick, Robert J. Capetola
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Patent number: 4985435Abstract: 2-Substituted-1-naphthols are 5-lipoxygenase inhibitors which make them useful in the treatment of inflammation, obstructive lung diseases and/or psoriasis. Useful 2-substituent groups are alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkenyls, the groups CH.sub.2 --C.tbd.C--(CH.sub.2).sub.m R.sup.5 and CH.dbd.CH--(CH.sub.2).sub.n R.sup.5 (where m is 1-4, n is 0-3 and R.sup.5 includes phenyl, COOR.sup.9, where R.sup.9 is H or alkyl of 1-4 carbons, AR.sup.6 l (where A is a methylene chain and R.sup.6 is a variety of groups including Cl, Br, I, CHO, CN, COOR.sup.9, NH.sub.2, SC(NH)NH.sub.2, phenyl, P(O)(OR.sup.9).sub.2, etc.), and CHR.sup.7 R.sup.21 (where R.sup.7 is a variety of aromatic and heterocyclic groups and R.sup.21 is H, optionally substituted phenyl and a variety of heterocyclic groups).Type: GrantFiled: March 16, 1989Date of Patent: January 15, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventor: Douglas G. Batt
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Patent number: 4985442Abstract: 2-Substituted-1-naphthols are 5-lipoxygenase inhibitors which make them useful in the treatment of inflammation, obstructive lung diseases and/or psoriasis. Useful 2-substituent groups are alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkenyls, the groups CH.sub.2 --C.tbd.C--(CH.sub.2).sub.m R.sup.5 and CH.dbd.CH--(CH.sub.2).sub.n R.sup.5 (where m is 1-4, n is 0-3 and R.sup.5 includes phenyl, COOR.sup.9, where R.sup.9 is H or alkyl of 1-4 carbons, AR.sup.6 (where A is a methylene chain and R.sup.6 is a variety of groups including Cl, Br, I, CHO, CN, COOR.sup.9, NH.sub.2, SC(NH)NH.sub.2, phenyl, P(O)(OR.sup.9).sub.2, etc.), and CHR.sup.7 R.sup.21 (where R.sup.7 is a variety of aromatic and heterocyclic groups and R.sup.21 is H, optionally substituted phenyl and a variety of heterocyclic groups).Type: GrantFiled: March 23, 1989Date of Patent: January 15, 1991Assignee: E. I. du Pont de Nemours and CompanyInventor: Douglas G. Batt
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Patent number: 4961922Abstract: A complex based on anthralin and a sterol, characterized in that its melting point is 10 to 25 degrees Celsius lower than that of the constituent of the complex melting at the lowest temperature and that the proportion of anthralin varies between 10 and 90 mol %.Type: GrantFiled: April 13, 1989Date of Patent: October 9, 1990Assignee: Centre International De Recherches DermatolociquesInventors: Braham Shroot, Daniele Caron, Jean-Claude Caron, Alain Brzokewicz
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Patent number: 4952401Abstract: A composition and a method of using the same wherein said composition comprises a rodenticide and an additive selected from the group consisting of1. polyoxyalkylated alkyl phenols;2. sorbitan fatty acids and polyoxyalkylated derivatives thereof;3. polyoxyalkylated fatty amines;4. polyoxyalkylated branched or linear alcohols, diols or polyols;5. polyoxyalkylated branched or linear mercaptans;6. polyoxyalkylated esters; and7. polyoxyalkylated amines.The composition may optionally include an organic solvent and/or a dye. The rodenticide may be selected from a wide host of compounds, including brodifacoum, bromadiolone, diphacinone, chlorodiphacinone, monofluoroacetatic acid, bromethalin, calciferol, flocoumafen, and salts of such compounds.Type: GrantFiled: June 12, 1990Date of Patent: August 28, 1990Assignee: ICI Americas Inc.Inventor: David G. Hobbs
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Patent number: 4898891Abstract: The invention relates to antiviral compositions of matter containing as active ingredient hypericin or pseudohypericin. The novel compositions are of special use in the treatment of, and alleviation of symptoms of various diseases caused by viruses such as vesicular stomatitis, influenza, herpes simplex, HSV-1 and HSV-2. The mode of activity seems to be by inhibition of RNA synthesis and interfering with virus replication. The pharmaceutical compositions can be applied by a variety of routes. Topical applications have proved to be effective against a variety of viral afflictions.Type: GrantFiled: August 7, 1987Date of Patent: February 6, 1990Assignee: Yeda Research and Development Company Ltd.Inventors: David Lavie, Michel Revel, Dalia Rotman, Vincent V. Velde
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Patent number: 4889847Abstract: The present invention is directed to the topical administration of a retinoid-containing pharmaceutical composition for the prevention of glucocorticoid-induced skin atrophy.Type: GrantFiled: November 3, 1986Date of Patent: December 26, 1989Assignee: Ortho Pharmaceutical CorporationInventors: Albert M. Kligman, James A. Mezick, Robert J. Capetola
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Patent number: 4833164Abstract: 2-Substituted-1-naphthols are 5-lipoxygenase inhibitors which make them useful in the treatment of inflammation, obstructive lung diseases and/or psoriasis. Useful 2-substituent groups are alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkenyls, the groups CH.sub.2 --C.tbd.C--(CH.sub.2).sub.m R.sup.5 and CH.dbd.CH--(CH.sub.2).sub.n R.sup.5 (where m is 1-4, n is 0-3 and R.sup.5 includes phenyl, COOR.sup.9, where R.sup.9 is H or alkyl of 1-4 carbons, AR.sup.6 (where A is a methylene chain and R.sup.6 is a variety of groups including Cl, Br, I, CHO, CN, COOR.sup.9, NH.sub.2, SC(NH)NH.sub.2, phenyl, P(O)(OR.sup.9).sub.2, etc.), and CHR.sup.7 R.sup.21 (where R.sup.7 is a variety of aromatic and heterocyclic groups and R.sup.21 is H, optionally substituted phenyl and a variety of heterocyclic groups).Type: GrantFiled: March 19, 1986Date of Patent: May 23, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Douglas G. Batt
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Patent number: 4788061Abstract: The healing of a number of skin disorders is effectively enhanced by prolonged continuous occlusion and/or hydration. Treating these disorders, e.g. psoriasis, is significantly facilitated by occluding affected skin areas with a suitable barrier for a prolonged and continuous period of time. Such occlusion is effective by itself, but is materially improved by concurrent topical administration of medicament useful for treating the disorder. In such cases the prolonged, continuous occlusion markedly increases hydration which has the further therapeutic benefit of tremendously facilitating penetration of medicament. The provided barrier is advantageously one with low vapor transmission or one which is water impermeable.Type: GrantFiled: July 5, 1985Date of Patent: November 29, 1988Inventor: Ronald N. Shore
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Patent number: 4777166Abstract: This invention relates to various compositions, comprising a 2-acetylprid thiosemicarbazone and a diol, which are useful in the treatment of viral infections.Type: GrantFiled: March 31, 1986Date of Patent: October 11, 1988Assignees: The United States of America as represented by the Secretary of the Army, The Regents of The University of MichiganInventors: Sandra H. Smith, John C. Drach, Gordon L. Flynn
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Patent number: 4769390Abstract: A pharmaceutical preparation for topical treatment of skin disorders, particularly psoriasis, comprising active ingredients consisting essentially of combinations of 1,8,9-anthracenetriol, and/or derivatives thereof, and urea. The subject preparation is applied in an essentially water-free excipient. The preparation includes surfactants, which are ordinarily incompatible with the active ingredients. By the use of surfactant-urea combinations, surfactants can be incorporated into a stable, lipophilic pharmaceutical preparation, whereby after use the surfactants are liberated by the action of water, to form a readily washable emulsion system. The inventive preparation is advantageously used in the "short time" method of therapy of psoriasis.Type: GrantFiled: January 21, 1987Date of Patent: September 6, 1988Assignee: Rohm GmbH Chemische FabrikInventors: Wolfgang Roelz, Josef Mueller
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Patent number: 4707473Abstract: 4-Monosubstitued and 4,6-disubstituted phenoxazines, methods of preparing them and pharmaceutical compositions containing them. These compounds are useful as anti-inflammatories.Type: GrantFiled: May 30, 1986Date of Patent: November 17, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Joseph M. Muchowski, Robert J. Greenhouse, Angel Guzman
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Patent number: 4699929Abstract: Pharmaceutical compositions for the treatment of skin have been prepared in a carrier which contains 40 to 60% of liquid paraffin, 40 to 60% of solid paraffin, and 0.5 to 5% of microcrystalline wax. The new carrier is especially suitable for readily oxidizable drugs such as dithranol and its derivatives. From the compositions of the invention it is possible to prepare sufficiently thin and hard, yet non-brittle sticks by means of which the drug can be applied at precisely the desired point of the skin.Type: GrantFiled: September 25, 1986Date of Patent: October 13, 1987Assignee: Orion-yhtyma OyInventors: Kimmo K. Mustakallio, Gunnar A. Sothmann, Hanna-Maija Heikinheimo
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Patent number: 4680310Abstract: Tetrahydronaphthalene derivatives of the formula ##STR1## wherein Y, m, n, R and R.sup.1 to R.sup.9 are as set forth herein, are described.These compounds have a pronounced calcium-antagonistic and anti-arrhythmic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischaemia, arrhythmias and high blood pressure. The compounds of formula I can be prepared by the amination of a compound of the formula ##STR2## with a corresponding N-methyl-phenylalkylamine and optional subsequent O-acylation. Compounds of formula II and IV are also described and are within the scope of the invention.Type: GrantFiled: October 10, 1985Date of Patent: July 14, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Urs Hengartner, Henri Ramuz
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Patent number: 4626529Abstract: The present invention discloses a homogeneous oily composition essentially consisting of a dermatological active principle, an oily compound and an oil-soluble surface-active component, the oil-soluble surface-active component comprising an anionic surface-active agent, the acid group of which has been neutralized by an amine, generally comprising 0.01 to 15% by weight of active principle, 5 to 85% by weight of oily compound and 15 to 95% by weight of oil-soluble surface-active agent.Type: GrantFiled: November 20, 1984Date of Patent: December 2, 1986Assignee: L'orealInventor: Jean F. Grollier
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Patent number: 4596798Abstract: This invention relates to the use of various 2-acetylpyridine thiosemicarbazones which are substituted on the 4-nitrogen atom in the treatment of viral infections. Also disclosed are several synthetic procedures used to prepare the thiosemicarbazones.Type: GrantFiled: March 30, 1982Date of Patent: June 24, 1986Assignee: The United States of America as represented by the Secretary of the ArmyInventors: Charles Shipman, Jr., Daniel L. Klayman, Sandra H. Smith, John C. Drach
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Patent number: 4576964Abstract: Tricyclic benzo fused compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, wherein n is zero, 1 or 2, and t is 1 or 2; M is CH or N, R.sub.1 is H or certain acyl groups; Q is CO.sub.2 R.sub.4, COR.sub.5, C(OR.sub.7)R.sub.5 R.sub.6, CN, CONR.sub.9 R.sub.10, CH.sub.2 NR.sub.9 R.sub.10, CH.sub.2 NHCOR.sub.11, CH.sub.2 NHSO.sub.2 R.sub.12, 5-tetrazolyl or when n is 1, Q and OR.sub.1 together form a lactone or certain reduced derivatives thereof; and Z is certain alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl groups, are valuable central nervous system active agents, methods for their use, pharmaceutical compositions containing them and certain intermediates therefor.Type: GrantFiled: June 7, 1984Date of Patent: March 18, 1986Assignee: Pfizer Inc.Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4551480Abstract: A topical anthralin cream composition in which the anthralin demonstrates improved stability, comprises from about 0.05% to about 5% by weight of anthralin in a water: fluid hydrocarbon emulsion having a weight ratio of at least about 5:1, at least one anionic emulsifying agent, at least one oil soluble anti-oxidant, at least one water soluble acidic material, and at least one bifunctional sequestering agent.Type: GrantFiled: March 2, 1984Date of Patent: November 5, 1985Assignee: Stiefel Laboratories, Inc.Inventors: Werner K. Stiefel, Daniel W. Nicolai
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Patent number: 4495203Abstract: Anhydrous composition, stable to oxidation, of anthralin or a derivative thereof.This composition contains anthralin or a derivative thereof in a carrier composed of (i) at least one fatty acid alkyl ester, the fatty acid having 12 to 18 carbon atoms and the alkyl radical having 2 or 3 carbon atoms, and (ii) at least one thickener taken from the group made up of silicas having particle sizes less than 30 m.mu. and polyethylene powders having densities between 0.9 and 0.96 (g/cm.sup.3).This composition is used in the treatment of skin diseases, particularly psoriasis.Type: GrantFiled: October 22, 1982Date of Patent: January 22, 1985Assignee: Societe Anonyme dite: L'OREALInventors: Jean-Francois Grollier, Georges Rosenbaum, Josiane Allec, Braham Shroot
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Patent number: RE32161Abstract: Pharmaceutical compositions for application topically or by suppository comprise:(a) a medicament, preferably protected from degradation by moisture by being presented in small particles of a waxy material,(b) from 5% to 40% of an inclusion compound of urea with a straight-chain aliphatic compound, preferably a fatty acid or alcohol,(c) up to 50% of an inert insoluble powder such as starch,(d) from 25% to 90% of an inert carrier, components (a), (b) and (c) being dispersed in (d).The compositions have good storage stability and a smooth texture.Type: GrantFiled: September 21, 1983Date of Patent: May 27, 1986Assignee: Phares Pharmecutical Research N.V.Inventors: Steven Leigh, Peter J. Ayres
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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