Two Benzene Rings Bonded Directly To The Same Nitrogen Patents (Class 514/658)
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Patent number: 6458852Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N- bis-phenyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: October 1, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6458849Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkyamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted mercapto amines.Type: GrantFiled: November 14, 2001Date of Patent: October 1, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6403627Abstract: Spin trapping compositions in general have now been discovered to be effective in treating a variety of disorders, including disorders such as those arising from ischemia, infection, inflammation, exposure to radiation or cytotoxic compounds, not just of the central and peripheral nervous systems but of peripheral organ disease having a wide variety of etiologies. In the preferred embodiment, the compositions for treating tissue damage from ischemia contain PBN, or active derivatives thereof, in a suitable pharmaceutical carrier for intravenous, oral, topical, or nasal/pulmonary administration. Other preferred spin-trapping agents include 5,5-dimethyl pyrroline N-oxide (DMPO), &agr;-(4-pyridyl-1-oxide)-N-tert-butylnitrone (POBN), and (TEMPO) and spin-trapping derivatives thereof. Examples of derivatives of PBN include halogenated derivatives, bifunctional derivatives, conjugates with drugs or targeting molecules, dimers and cyclodextran polymers of PBN.Type: GrantFiled: July 20, 1999Date of Patent: June 11, 2002Assignees: Oklahoma Medical Research Foundation, University of Kentucky FoundationInventors: John M. Carney, Robert A. Floyd
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Publication number: 20020068750Abstract: The present invention relates generally to mitochondria protecting agents for treating diseases in which mitochondrial dysfunction leads to tissue degeneration and, more specifically, to compounds, compositions and methods related to the same. The methods of this invention involve administration of a pharmaceutically effective amount of a mitochondria protecting agent to a warm-blooded animal in need thereof, and composition of this invention contain a mitochondrial protecting agent in combination with a pharmaceutically acceptable carrier or diluent. Mitochondrial associated diseases which may be treated by the present invention include (but are not limited to) Alzheimer's Disease, diabetes mellitus, Parkinson's Disease, neuronal and cardiac ischemia, Huntington's disease and stroke.Type: ApplicationFiled: July 31, 2001Publication date: June 6, 2002Inventors: Soumitra S. Ghosh, Scott W. Miller, Robert E. Davis, Walter H. Moos
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Publication number: 20020065298Abstract: The present invention relates generally to mitochondria protecting agents for treating diseases in which mitochondrial dysfunction leads to tissue degeneration and, more specifically, to compounds, compositions and methods related to the same. The methods of this invention involve administration of a pharmaceutically effective amount of a mitochondria protecting agent to a warm-blooded animal in need thereof, and composition of this invention contain a mitochondria protecting agent in combination with a pharmaceutically acceptable carrier or diluent. Mitochondrial associated diseases which may be treated by the present invention include (but are not limited to) Alzheimer's Disease, diabetes mellitus, Parkinson's Disease, neuronal and cardiac ischemia, Huntington's disease and stroke.Type: ApplicationFiled: August 20, 2001Publication date: May 30, 2002Inventors: Soumitra S. Ghosh, Scott W. Miller, Robert E. Davis, Walter H. Moos
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Publication number: 20020028846Abstract: The invention provides a composition suitable for topical application comprising: an effective amount of a prostaglandin, a polymer thickener, a lipophilic component, and a buffer system. In another embodiment, the invention provides a composition suitable for topical application comprising: an effective amount of a vasoactive agent, a polymer thickener, a lipophilic component, and a buffer system. The invention also provides methods of ameliorating female sexual dysfunction. Also provided are methods of increasing female sexual arousal and methods of enhancing female sexual response.Type: ApplicationFiled: December 10, 1998Publication date: March 7, 2002Inventors: JAMES L. YEAGER, NADIR BUYUKTIMKIN, SERVET BUYUKTIMKIN
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Patent number: 6331553Abstract: Compounds represented by the general formula (1): (where R1 and R2 are typically a hydrogen atom; R3 and R4 are typically a hydrogen atom or a lower alkyl group; R5 is typically a hydrogen atom; X1, X2, X3 and X4 are typically a hydrogen atom or a lower alkoxy group; A is typically an optionally substituted pyridine ring; m and n are each 0 or 1) have an NOS inhibiting activity and are useful as therapeutics of cerebrovascular diseases and other pharmaceuticals.Type: GrantFiled: June 24, 1999Date of Patent: December 18, 2001Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Toru Esaki, Toshihiko Makino, Yoshikazu Nishimura, Toshiaki Nagafuji
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Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
Patent number: 6297260Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.Type: GrantFiled: October 29, 1999Date of Patent: October 2, 2001Assignee: NitroMed, Inc.Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang -
Patent number: 6277829Abstract: The present invention describes a process for the preparation of aqueous formulations containing azithromycin for ophthalmic use, as well any formulations obtained by this process and their topical use in the ocular bacterial infections, more preferably in the treatment of conjunctivitis, keratitis and blepharitis.Type: GrantFiled: December 27, 1999Date of Patent: August 21, 2001Assignee: S.I.F.I. Societa Industria Farmaceutica Italiana S.p.A.Inventors: Antonino Asero, Maria Grazia Mazzone, Valeria Moschetti, Anna Rita Blanco
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Patent number: 6274570Abstract: A liquid pesticidal composition, which is substantially free of water, comprising a hydrophobic pesticide or mixture of pesticides dissolved in an organic solvent and comprising as surfactants (a) a castor oil ethoxylate having 30-50 mol ethoxylate, (b) a branched C8-C18 alcohol ethoxylate having 5-10 mol ethoxylate, and (c) a tristyrenephenol-ethoxylate having 8-30 mol ethoxylate, or its phosphate or salt thereof. The compositions also include gels having a viscosity of 500 to 20,000 mPas and comprising additionally a gelling agent.Type: GrantFiled: December 22, 1998Date of Patent: August 14, 2001Assignee: Syngenta Crop Protection, Inc.Inventors: Manfred Vogt, William Baettig
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Patent number: 6267946Abstract: A method of reducing the percentage of Epstein-Barr virus genome-carrying cells which exhibit Epstein-Barr virus early antigen induction, wherein the Epstein-Barr virus genome-carrying cells have been cultivated in the presence of a tumor-promoting chemical and/or a tumor-inducing chemical. The method is performed by: a) cultivating Epstein-Barr virus genome-carrying cells in the presence of a tumor-promoting chemical and/or a tumor-inducing chemical; and b) treating the Epstein-Barr virus genome-carrying cells with a synthetic anthraquinone colorant containing a sulfonated phenylamino group. The colorant is effective to reduce the incidence of Epstein-Barr virus early antigen induction in the cultivated Epstein-Barr virus genome-carrying cells.Type: GrantFiled: February 24, 1999Date of Patent: July 31, 2001Inventor: Govind Kapadia
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Patent number: 6251943Abstract: The present invention provides a method for treating or preventing septic shock. Specifically, the present invention provides a method of treating or preventing septic shock by administering to a patient a MEK inhibitor.Type: GrantFiled: August 2, 1999Date of Patent: June 26, 2001Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
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Patent number: 6235736Abstract: A 3-anilino-2-cycloalkenone derivative of the formula (I): wherein, R1 represents a C1 to C8 alkyl group, which may have a substituent, except for a methyl group, a C3 to C7 cycloalkyl group, a 3-tetrahydrofuryl group, an 2-indanyl group, etc., R2 represents a C1 to C4 alkyl group, R3 represents a hydrogen atom, a C3 to C7 alkyl group, which may have a substituent, a C3 to C7 cycloalkyl group, etc., R4 represents a hydrogen atom, a C1 to C5 alkyl group, which may have a substituent, a halogen atom, etc., R5, R6, R7, and R8 independently represent a hydrogen atom, a C1 to C5 alkyl group, which may have a substituent, etc., X represents —(CR11R12)n—, wherein n is 0 to 2, R11 and R12 independently represent a hydrogen atom, a C1 to C5 alkyl group, which may have a substituent, etc.Type: GrantFiled: March 20, 2000Date of Patent: May 22, 2001Assignee: Nikken Chemicals Co., Ltd.Inventors: Shinji Ina, Kenjirou Yamana, Kyoji Noda, Akane Takahama, Toshihiko Akiyama
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Patent number: 5985880Abstract: A method of reducing, treating or preventing drug-mediated respiratory depression in an animal, incident to the administration to said animal of a respiratory depression-mediating drug, comprising administering to the animal receiving said drug an effective amount of a .delta. receptor agonist compound.Type: GrantFiled: July 3, 1997Date of Patent: November 16, 1999Assignee: Delta PharmaceuticalsInventors: Kwen-Jen Chang, Robert W. McNutt, Jr., Hugh O. Pettit, Michael J. Bishop
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Patent number: 5780510Abstract: 2,4-disulfonyl .alpha.-phenyl-tert-butyl nitrone and its pharmaceutically acceptable salts are disclosed. These materials are useful as pharmaceutical agents for oral or parenteral, e.g. intravenous administration to patients suffering from acute central nervous system oxidation as occurs in a stroke or from gradual central nervous system oxidation which can exhibit itself as progressive central nervous system function loss. The materials are also used to ameliorate the side effects of oxidative-damage causing antineoplastic disease treatments.Type: GrantFiled: June 19, 1997Date of Patent: July 14, 1998Assignees: Oklahoma Medical Research Foundation, University of Kentucky Research FoundationInventor: John M. Carney
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Patent number: 5739169Abstract: Novel compounds ##STR1## wherein R.sup.1 to R.sup.13 are independently selected from C.sub.2 -C.sub.4 linear and branched alkyls, H, NH.sub.2, CH.sub.3, OR.sup.14, fluorine, chlorine, iodine, NO.sub.2, CF.sub.3, NHCOCH.sub.3, NHCOOtBu, NHR.sup.15, NR.sup.16 R.sup.17 and phenyl, for use as immunosuppressive agents to prevent or significantly reduce graft rejection in organ and bone marrow transplantation are described. The novel compounds can also be used as an immunosuppressant drug for T-lymphocyte mediated autoimmune diseases, such as diabetes, and may be useful in alleviating psoriasis and contact dermatitis. Additionally, the novel compounds can be used for antiproliferation and gene therapy.Type: GrantFiled: May 31, 1996Date of Patent: April 14, 1998Assignee: Procept, IncorporatedInventors: Timothy D. Ocain, Huai Gao, Jeffrey I. Krieger, Theresa M. Sampo
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Patent number: 5679660Abstract: A method of preparing an injectable pharmaceutical or veterinary composition which comprises either diclofenac or a salt thereof and 2-hydroxypropyl beta-cyclodextrin, or an inclusion complex of diclofenac or a salt thereof and 2-hydroxypropyl beta-cyclodextrin, includes the step of dissolving either the diclofenac or salt thereof and the 2-hydroxypropyl beta-cyclodextrin, or the inclusion complex, in water to form a solution, the water having been acidified to a pH such that the pH of the solution is from 6.0 to 8.5 inclusive, in the absence of a phosphate buffer. The composition so produced has good stability on storage.Type: GrantFiled: December 2, 1994Date of Patent: October 21, 1997Assignee: Farmarc Nederland BVInventors: Mark David Bodley, Lueta Ann Glintenkamp, Lawrence John Penkler, Michiel Coenraad Bosch van Oudtshoorn
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Patent number: 5633283Abstract: Provided is a method of treating multiple sclerosis employing certain phenol and benzamide compounds.Type: GrantFiled: January 23, 1995Date of Patent: May 27, 1997Assignee: Eli Lilly and CompanyInventors: Ann E. Kingston, Jill A. Panetta
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Patent number: 5475032Abstract: 2,4-disulfonyl .alpha.-phenyl-tert-butyl nitrone and its pharmaceutically acceptable salts are disclosed. These materials are useful as pharmaceutical agents for oral or parenteral, e.g. intravenous administration to patients suffering from acute central nervous system oxidation as occurs in a stroke or from gradual central nervous system oxidation which can exhibit itself as progressive central nervous system function loss. The materials are also used to ameliorate the side effects of oxidative-damage causing antineoplastic disease treatments.Type: GrantFiled: April 24, 1995Date of Patent: December 12, 1995Assignees: Oklahoma Medical Research Foundation, University of Kentucky Research FoundationInventor: John M. Carney
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Patent number: 5438056Abstract: The compounds of the present invention have the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently phenyl, pyridyl, thienyl, naphthyl, substituted phenyl wherein the substituent is selected from the group consisting of halogen, methoxy, and dialkylamino wherein alkyl contains 1 to 3 carbon atoms; or R.sup.1 and R.sup.2 are independently substituted furanone of the structure ##STR2## wherein R.sup.5 and R.sup.6 are independently alkyl containing 1 to 3 carbon atoms, cycloalkyl containing 5 to 7 carbon atoms, phenyl or substituted phenyl wherein the substituent is alkyl containing 1 to 5 carbon atoms or halogen; R.sup.7 is hydrogen or halogen; or R.sup.1 and R.sup.2 are joined to form ##STR3## R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 4 to 20 branched, straight chain, cyclic, saturated or unsaturated carbon atoms; or R.sup.3 and R.sup.4 are joined to form ##STR4## wherein R.sup.Type: GrantFiled: October 5, 1993Date of Patent: August 1, 1995Assignee: American Home Products CorporationInventors: Steven W. Felman, Kevin A. Memoli, Ivo Jirkovsky
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Patent number: 5256699Abstract: The invention provides a dispersible solid drug formulation comprising finely divided diclofenac as the free acid, from 5 to 25% by weight of a disintegrant and a pharmaceutically acceptable diluent.Type: GrantFiled: April 12, 1992Date of Patent: October 26, 1993Assignee: Ciba-Geify CorporationInventors: Lorraine M. Murphy, Graham P. Matthews
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Patent number: 5068250Abstract: Compounds such as 1-(4-bromoacetamidobenzyl)-5-methoxy-2-methylindole-3-acetic acid, N-(4-bromoacetamidophenyl) anthranilic acid and N-(3-bromoacetamidophenyl) anthranilic acid function as irreversible ligands for nonsteroidal antiinflammatory drug (NSAID) and prostaglandin binding sites. It is therefore expected that these compounds, and analogs thereof, will have utility as anti-inflammatory drugs, as affinity labeling agents and as ligands for use in affinity chromatography.Type: GrantFiled: September 29, 1988Date of Patent: November 26, 1991Assignee: Trustees of University of PennsylvaniaInventors: Trevor M. Penning, Leslie J. Askonas
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Patent number: 5059626Abstract: A one phase, liquid composition for oral administration comprises a NSAID such as an anthranilic acid derivative plus a di- or triglyceride of a medium chain fatty acid edible oil which has the characteristics of a pharmaceutical solvent carrier as known to those skilled in the art. Other pharmaceutical additives may be optionally added. An additional stipulation is that ethanol or other monohydric alcohol solvents should not be present.Type: GrantFiled: January 30, 1991Date of Patent: October 22, 1991Assignee: Applied Analytical Industries, Inc.Inventors: Moo W. Park, Henry C. Caldwell
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Patent number: 4906662Abstract: Disclosed are phenol derivatives of the formula ##STR1## wherein R.sup.1 is a substituted phenyl group, R.sup.2 and R.sup.3 are C.sub.1 -C.sub.6 alkyl group and of the formula ##STR2## wherein R.sup.8, R.sup.9 and R.sup.10 are C.sub.1 -C.sub.6 alkyl and the like and A is H, C.sub.1 -C.sub.6 alkylsulfonyl and the like substituents. These compounds and some related compounds have anti-inflammatory activity and lipoxygenase inhibitory activity.Type: GrantFiled: January 27, 1987Date of Patent: March 6, 1990Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Kinji Hashimoto, Kiyoto Goto, Ken-ichi Kanai, Yoshiaki Tsuda
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Patent number: 4840971Abstract: An ether compound represented by the following general formula (I), its produciton method and an insecticidal and/or acaricidal composition containing it as an active ingredient: ##STR1## wherein R.sub.1 and R.sub.2, which may be identical or different, represent a hydrogen or halogen atom or a lower alkyl, lower haloalkyl, lower alkoxyl, lower haloalkoxyl, lower alkenyl or lower alkenyloxyl group, or represent, taken together, methylenedioxy, lower alkylene, ethyleneoxy or lower alkylethyleneoxy group; R.sub.3 represents a hydrogen or fluorine atom; R.sub.4 represents a hydrogen or halogen atom or a lower alkyl, lower haloalkyl, lower alkoxyl or lower haloalkoxyl group; m represents an integer of 1 or 2; Y represents an oxygen or sulfur atom or a group represented by the formula --CH.sub.2 -- or --NH--; and Z represents a nitrogen atom or a group represented by the formula --CH.dbd., and its starting materials.Type: GrantFiled: April 2, 1987Date of Patent: June 20, 1989Assignee: Sumitomo Chemical Company, LimitedInventors: Kazunori Tsushima, Noritada Matsuo, Yoo Tanabe, Toshihiko Yano, Masachika Hirano
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Patent number: 4791123Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: January 22, 1987Date of Patent: December 13, 1988Assignee: Schering Akt.Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
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Patent number: 4772633Abstract: This invention relates to a novel compound represented by the following general formula (I), its production, and an insecticidal and acaricidal composition containing it as an active ingredient: ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, are a hydrogen atom, a halogen atom, a lower alkyl group, a trifluoromethyl group, a lower alkoxyl group, a lower alkenyloxy group or a halogenated lower alkoxyl group or are, taken together, a methylenedioxy group; R.sub.3 is a vinyl group or a ethynyl group; R.sub.4 is a hydrogen atom or a lower alkyl group; R.sub.5 is a hydrogen atom or a fluorine atom; R.sub.6 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group or a trifluoromethyl group; Z is a nitrogen atom or a group represented by the formula --CH.dbd.; when Z is a nitrogen atom, Y is an oxygen atom; and when Z is a group of the formula --CH.dbd., Y is an oxygen atom, a sulfur atom, a methylene group or a group represented by the formula --NH--.Type: GrantFiled: February 20, 1986Date of Patent: September 20, 1988Assignee: Sumitomo Chemical Company, LimitedInventors: Noritada Matsuo, Kazunori Tsushima, Sumio Nishida, Toshihiko Yano, Masachika Hirano
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Patent number: 4764534Abstract: 4-Substituted-N-[2,4-dinitro-6-(trifluoromethyl)phenyl]-1-naphthalenamine derivatives, useful as anticoccidial agents both alone and in combination with polyether antibiotics.Type: GrantFiled: July 17, 1984Date of Patent: August 16, 1988Assignee: Eli Lilly and CompanyInventors: Albert J. Clinton, deceased, George O. P. O'Doherty
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Patent number: 4731384Abstract: The invention relates to topical antiinflammatory medicament formulations which also have analgesic activity and contain 2-(2-hydroxyethoxy)-ethyl N-(.alpha.,.alpha.,.alpha.,-trifluoro-m-tolyl) anthranilate as the active ingredient and an adjuvant which is preferably a triglyceride.Type: GrantFiled: March 20, 1986Date of Patent: March 15, 1988Assignee: Troponwerke GmbH & Co, KGInventors: Hans-Dieter Dell, Reinhold Kraus, Detlef Schierstedt
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Patent number: 4539429Abstract: Novel lower-alkyl 2-(hydroxyphenylamino)phenyl ketones, useful as inhibitors of lipoxygenase activity, are of the formula ##STR1## wherein R is hydrogen, lower-alkyl, lower-alkoxy or halo; R' is hydrogen or lower-alkyl; R" is hydrogen, lower-alkyl or halo; and Alk is lower-alkyl. The compounds are prepared by de-etherification of the corresponding alkyl or benzyl ethers which are in turn prepared by reacting a 2-(alkoxy- or benzyloxyphenylamino)benzoic acid with an alkyllithium.Type: GrantFiled: July 11, 1983Date of Patent: September 3, 1985Assignee: Sterling Drug Inc.Inventor: Denis M. Bailey
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Patent number: 4514383Abstract: Novel sunscreen compositions comprising at least one vinylogous amide compound are described as well as methods of protecting the human skin from damaging radiation.Type: GrantFiled: May 5, 1982Date of Patent: April 30, 1985Assignee: Johnson & Johnson Baby Products CompanyInventors: William V. Murray, Charles E. Clum, Elvin R. Lukenbach
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Patent number: RE37087Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.Type: GrantFiled: June 20, 1991Date of Patent: March 6, 2001Assignee: Schering AktiengesellschaftInventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles