Chalcogen Attached Directly To Ring Sulfur Of The Hetero Ring By Nonionic Bonding Patents (Class 549/53)
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Patent number: 9884863Abstract: Provided are STAT3 inhibitors and methods of treating inflammation or a hyperproliferative disease such as, e.g., cancer. In some aspects, compounds may be used to treat breast cancer, a head/neck cancer, a lung cancer, a prostate cancer, or pancreatic cancer.Type: GrantFiled: December 15, 2016Date of Patent: February 6, 2018Assignee: Board of Regents, The University of Texas SystemInventors: Jia Zhou, Haijun Chen, Qiang Shen
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Patent number: 8759555Abstract: The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.Type: GrantFiled: June 26, 2012Date of Patent: June 24, 2014Assignee: Leo Pharma A/SInventors: Thomas Peter Sabroe, Martin John Calverley
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Publication number: 20130210904Abstract: Disclosed embodiments concern the synthesis and use of therapeutic compounds that for treating emerging flu strains and minimizing resistance to such strains. Methods for making the disclosed compounds concern using a base-mediated addition/cyclization sequence followed by functional group manipulation to develop functionalized compounds that can target neuraminidase, which makes them ideal candidates for treating influenza. Pharmaceutical compositions comprising the therapeutic compounds and biologically-acceptable materials are also described. Methods of inhibiting neuraminidase in subjects that are suspected of containing neuraminidase are also described. The use of metabolites of the disclosed compounds can also be used in diagnostic assays for therapeutic dosing of the disclosed compounds.Type: ApplicationFiled: August 15, 2012Publication date: August 15, 2013Inventors: Jeremy E. Wulff, Michael G. Brant, Jeremy W. Mason, Caleb M. Bromba, Martin J. Boulanger
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Patent number: 8362287Abstract: The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.Type: GrantFiled: March 10, 2005Date of Patent: January 29, 2013Assignee: Leo Pharma A/SInventors: Thomas Peter Sabroe, Martin John Calverley
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Publication number: 20120329775Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: June 4, 2012Publication date: December 27, 2012Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
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Publication number: 20120271058Abstract: The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.Type: ApplicationFiled: June 26, 2012Publication date: October 25, 2012Inventors: Thomas Peter SABROE, Martin John Calverley
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Patent number: 8158655Abstract: The invention is concerned with the novel sulfonamide derivatives of formula (I) wherein A, R1 to R2?, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.Type: GrantFiled: January 8, 2008Date of Patent: April 17, 2012Assignee: Hoffmann-La Roche Inc.Inventors: David Banner, Harald Mauser, Rudolf E. Minder, Hans P. Wessel
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Publication number: 20110288066Abstract: The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.Type: ApplicationFiled: February 9, 2010Publication date: November 24, 2011Applicant: MERCK SERONO S.A.Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Christophe Cleva, Adeline Pretre
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Patent number: 7973180Abstract: The present invention provides a method for the production of an aqueous dispersion containing an electroconductive polymer component which enables electroconductive thin films which are outstanding in their transparency and electroconductivity to be formed, together with the aqueous dispersion obtained by said method. This method includes a stage in which a 3,4-dialkoxythiophene is polymerized in an aqueous solvent using an oxidizing agent in the presence of a polyanion and, in this stage, said oxidizing agent is added by the dropwise addition of a solution or dispersion containing said oxidizing agent to the reaction solution or, alternatively, in the polymerization stage, the alkali metal ion concentration in the reaction liquid is maintained at no more than 400 ppm.Type: GrantFiled: October 6, 2006Date of Patent: July 5, 2011Assignee: H.C. Starck GmbHInventors: Yoshiyuki Morita, Yasuo Chikusa, Kyoko Miyanishi, Stephan Kirchmeyer, Wilfried Loevenich
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Publication number: 20110144170Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.Type: ApplicationFiled: February 18, 2011Publication date: June 16, 2011Inventors: Mark Phillip Hogarth, Geoffrey Allan Pietersz, Gerard Peter Moloney
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Patent number: 7931696Abstract: Disclosed are dyes of formula wherein D is the radical of anthraquinone, acridine, azo, azomethine, hydrazomethine, benzodifuranone, coumarine, diketopyrrolopyrrol, dioxaxine, diphenylmethane, formazane, indigoid, indophenol, naphtalimide, naphthaquinone, nitroaryl, merocyanine, methine, oxazine, perinone, perylene, pyrenequinone, phtalocyanine, phenazine, quinoneimine, quinacridone, quinophtalone, stilbene, styryl, triphenylmethane, xanthene, thiazine dye and thioxanthene dye; and Q is defined herein.Type: GrantFiled: January 22, 2008Date of Patent: April 26, 2011Assignee: BASF SE LudwigshafenInventors: Victor Paul Eliu, Beate Fröhling, Dominique Kauffmann
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Publication number: 20100311741Abstract: This invention pertains generally to the field of therapeutic compounds, and more particularly, to certain bicyclosulfonyl acid (BCSA) compounds which act as inhibitors of Tumour Necrosis Factor-? Converting Enzyme (TACE). The compounds are useful in the treatment of conditions mediated by TNF-?, such as rheumatoid arthritis; inflammation; psoriasis; septic shock; graft rejection; cachexia; anorexia; congestive heart failure; post ischaemic reperfusion injury; inflammatory disease of the central nervous system; inflammatory bowel disease; insulin resistance; HIV infection; cancer; chronic obstructive pulmonary disease (COPD); and asthma. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in the inhibition of TACE, and in the treatment of conditions that are ameliorated by the inhibition of TACE.Type: ApplicationFiled: May 16, 2008Publication date: December 9, 2010Applicant: INHIBOX LTD.Inventors: Aigars Jirgensons, Gundars Leitis, Ivars Kalvinsh, Daniel Robinson, Paul Finn, Nagma Khan
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Publication number: 20100286118Abstract: The present invention provides compounds of formula (I) in which y, m, n, R1, R2 and Q are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: May 6, 2010Publication date: November 11, 2010Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Ian Millichip
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Publication number: 20100168217Abstract: The invention relates to novel compound of the general formula (I), in which R has the meanings indicated in claim 1, to the preparation thereof and to the use thereof as medicaments. The compounds (I) are inhibitors of steroid sulfatase and are used for the treatment of cancer.Type: ApplicationFiled: November 13, 2007Publication date: July 1, 2010Applicant: MERCK PATENT GMBHInventors: Wolfgang Staehle, David Bruge, Gerald Scholz, Benoit Rondot, Jean Lafay
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Patent number: 7696246Abstract: The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.Type: GrantFiled: June 23, 2005Date of Patent: April 13, 2010Assignee: Ligand Pharmaceuticals IncorporatedInventors: Lin Zhi, Cornelis Arjan Van Oeveren, Esther Martinborough
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Publication number: 20090286863Abstract: The invention relates to novel compound of the general formula (I), in which R has the meanings indicated in Claim 1, to the preparation thereof and to the use thereof as medicaments. The compounds (I) are inhibitors of steroid sulfatase and are used for the treatment of cancer.Type: ApplicationFiled: June 5, 2007Publication date: November 19, 2009Inventors: David Bruge, Wolfgang Staehle, Gerald Scholz, Benoit Rondot, Jean Lafay
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Patent number: 7601851Abstract: Dye reagents useful in labeling biological materials are provided along with methods for their use.Type: GrantFiled: May 10, 2005Date of Patent: October 13, 2009Assignee: Epoch Biosciences, Inc.Inventors: Eugeny A. Lukhtanov, Alexei V. Vorobiev, Michael W. Reed, Nicolaas M. J. Vermeulen
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Publication number: 20090176865Abstract: The present invention is directed to novel sulfamide derivatives, pharmaceutical compositions comprising said compounds and methods for the treatment of epilepsy and related disorders comprising administering to a subject in need thereof, said compounds, either alone or as co-therapy with one or more anticonvulsant and/or anti-epileptic agents.Type: ApplicationFiled: August 7, 2008Publication date: July 9, 2009Inventors: Michael Breslav, Brian Klein, John A. Moyer, Frank J. Villani
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Patent number: 7541454Abstract: Compounds useful in the fluorescent labeling of biological materials are provided along with methods for their use and preparation.Type: GrantFiled: October 25, 2004Date of Patent: June 2, 2009Assignee: Epoch Biosciences, Inc.Inventor: Eugeny A. Lukhtanov
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Publication number: 20090099147Abstract: The present invention relates to non-steroidal progesterone receptor modulators of the general formula I the use of the progesterone receptor modulators for producing medicaments, and pharmaceutical compositions which comprise these compounds. The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.Type: ApplicationFiled: July 9, 2008Publication date: April 16, 2009Inventors: Wolfgnag SCHWEDE, Carsten Moeller, Anja Schmidt, Ulrike Fuhrmann, Andrea Rotgeri, Thomas Kirkland
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Patent number: 7476691Abstract: The present invention relates to sulfamate benzothiophene compounds of the formula: (I) wherein R1, R2, R3, m and n are as defined in the specification. The invention also relates to pharmaceutical compositions containing these compounds and to methods of using them.Type: GrantFiled: May 16, 2003Date of Patent: January 13, 2009Assignee: Laboratoire TheramexInventors: Jean Lafay, Benoît Rondot, Denis Carniato, Paule Bonnet, Thierry Clerc, Jacqueline Shields, Igor Duc, Eric Duranti
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Publication number: 20080300243Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: February 24, 2006Publication date: December 4, 2008Inventors: Michael G. Kelly, John Kincaid, Matthew Duncton, Kiran Sahasrabudhe, Satyanarayana Janagani, Ravindra B. Upasani, Guoxian Wu, YunFeng Fang, Zhi-Liang Wei, Carl Kaub, Jianhua He
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Patent number: 7449483Abstract: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.Type: GrantFiled: December 6, 2006Date of Patent: November 11, 2008Assignee: Hoffman-La Roche Inc.Inventors: Johannes Aebi, Jean Ackermann, Henrietta Dehmlow, Hans-Peter Maerki, Olivier Morand
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Publication number: 20080182889Abstract: This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.Type: ApplicationFiled: March 31, 2008Publication date: July 31, 2008Inventors: Eric David Moher, James Allen Monn, Concepcion Pedregal-Tercero, Jaime Gonzalo Blanco-Urgoiti, Ivan Collado Cano
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Publication number: 20080167348Abstract: The invention is concerned with the novel sulfonamide derivatives of formula (I) wherein A, R1 to R2?, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.Type: ApplicationFiled: January 8, 2008Publication date: July 10, 2008Inventors: David Banner, Harald Mauser, Rudolf E. Minder, Hans P. Wessel
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Publication number: 20080146632Abstract: The present invention provides compounds capable of binding to an Fc receptor and modulating Fc receptor activity comprising a core lipophilic group in the form of an Aryl zing substituted with a group rich in p-electrons. The invention further provides for a method of treating an autoimmune disease involving Fc receptor activity using such compounds. A method for obtaining a compound which modulates Fc receptor activity is also provided, the method comprising: (a) providing or designing compounds having structural characteristics to fit in the groove of the Fc?RIIa structure; and (b) screening the compounds for modulating activity on the Fc receptor.Type: ApplicationFiled: February 1, 2008Publication date: June 19, 2008Applicant: TRILLIUM THERAPEUTICS, INC.Inventors: Mark Phillip Hogarth, Geoffrey Allan Pietersz, Gerard Peter Moloney
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Patent number: 7371872Abstract: This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.Type: GrantFiled: June 6, 2003Date of Patent: May 13, 2008Assignee: Eli Lilly and CompanyInventors: Eric David Moher, James Allen Monn
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Patent number: 7173043Abstract: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.Type: GrantFiled: July 8, 2005Date of Patent: February 6, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Johannes Aebi, Jean Ackermann, Henrietta Dehmlow, Hans-Peter Maerki, Olivier Morand
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Patent number: 6927298Abstract: A 3,4-alkylenedioxythiophenedioxide compound represented by formula (I): in which: A represents a C1-5-alkylene bridge; R represents an optionally substituted C1-24-alkyl, C3-18-cycloalkyl, C1-18-alkoxy or polyethylene oxide group (optionally with at least one substituent selected from the group consisting of an alcohol, amide, ether, ester or sulphonate group) or an optionally substituted aryl group; a polymer comprising monomeric units represented by formula (I); an aqueous dispersion of a polymer comprising monomeric units corresponding to at least one compound according to formula (I) and a polyanion; a chemical polymerization process for preparing the aqueous dispersion comprising the steps of: (i) providing a solution of a polyanion; (ii) adding a compound according to formula (I) and a thiophene or pyrrole compound to the solution provided in step (i); and (iii) adding an oxidizing or reducing system to the mixture provided in step (ii); a printable paste containing the aqueous dispersion; an electType: GrantFiled: August 27, 2003Date of Patent: August 9, 2005Assignee: Agfa-GevaertInventors: Bert Groenendaal, Frank Louwet, Hieronymus Andriessen
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Patent number: 6875787Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein the dashed line indicates the presence or absence of a bond, the hatched wedge indicates the ? (down) configuration, and the solid triangle indicates the ? (up) configuration; B is a single, double, or triple covalent bond; n is 0-6; X is CH2, S or O; Y is any pharmaceutically acceptable salt of CO2H, or CO2R, CONR2, NHCH2CH2OH, N(CH2CH2OH)2, CH2OR, P(O)(OR)2, CONRSO2R, SONR2, or R is H, C1-6 alkyl or C2-6 alkenyl; R2 and R3 are C1-6 linear alkyl which may be the same or different, and may be bonded to each other such that they form a ring incorporating the carbon to which they are commonly attached; R4 is hydrogen, R, C(?O)R, or any group that is easily removed under physiological conditions such that R4 is effectively hydrogen; R5 is hydrogenType: GrantFiled: February 11, 2003Date of Patent: April 5, 2005Assignee: Allergan, Inc.Inventor: Yariv Donde
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Publication number: 20040043326Abstract: An optical information recording medium has a recording layer composed essentially of an oxonol compound of the following formula: 1Type: ApplicationFiled: June 6, 2003Publication date: March 4, 2004Applicant: FUJI PHOTO FILM CO. , LTD.Inventors: Naoki Saito, Koji Wariishi, Michihiro Shibata
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Patent number: 6686390Abstract: The present invention relates to novel heterocyclic compounds of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their regioisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.Type: GrantFiled: May 21, 2001Date of Patent: February 3, 2004Assignee: Dr. Reddy's Laboratories LimitedInventors: Manojit Pal, Koteswar Rao Yeleswarapu, Rajagopalan Ramanujam, Parimal Misra, Prem Kumar Mamnoor, Seshagiri Rao Casturi
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Publication number: 20040002425Abstract: The present invention relates to a novel triketone derivative having a specific structure and a herbicide containing the triketone derivative as an active ingredient. The herbicide is effective for controlling weeds which inhibit growth of crop plants, inter alia, for paddy weeds such as Sanwa millet and Scirups juncoides.Type: ApplicationFiled: April 1, 2003Publication date: January 1, 2004Applicant: Idemitsu Kosan Co., Ltd.Inventors: Masatoshi Saitou, Hiroki Sekiguchi, Shinichiro Ogawa
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Patent number: 6465508Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.Type: GrantFiled: February 23, 2001Date of Patent: October 15, 2002Assignee: WyethInventors: Frances Christy Nelson, Arie Zask, James Ming Chen, Dominick Mobilio, Ramaswamy Nilakantan
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Patent number: 6420391Abstract: The present invention relates to a fused thiophene derivative of the formula (I) (wherein all the symbols are defined as described in the specification) and an inhibitor of producing interleukin-6 and/or interleukin-12 comprising the said derivative as an active ingredient. A fused thiophene derivative of the formula (I) is useful as an agent for the prevention and/or treatment of various inflammatory diseases, sepsis, multiple myeloma, plasma cell leukemia, osteoporosis, cachexia, psoriasis, nephritis, renal cell carcinoma, Kaposi's sarcoma, rheumatoid arthritis, gammopathy, Castleman's disease, atrial myxoma, diabetes mellitus, autoimmune diseases, hepatitis, multiple sclerosis, colitis, graft versus host immune diseases, infectious diseases.Type: GrantFiled: October 2, 2000Date of Patent: July 16, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mikio Konishi, Nobuo Katsube, Mitoshi Konno, Tadamitsu Kishimoto
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Patent number: 6355386Abstract: This invention is a dispersion comprising a solvent having dispersed therein a liquid-crystal forming dye of structural Formula I: [D—(X)m]—(Y)n I wherein: D is a merocyanine dye; each Y contains an ionic or a nonionic solubilizing substituent or a group with a pKa value of less than 4 in water; each X is a nonionic substituent; n is 1 to 10; m is 0-10; and the resulting dye forms a liquid-crystalline phase in solvent. The dispersion is particularly useful in imaging and photographic elements.Type: GrantFiled: October 16, 2000Date of Patent: March 12, 2002Assignee: Eastman Kodak CompanyInventors: Margaret J. Helber, William J. Harrison, Richard L. Parton
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Patent number: 6281240Abstract: This invention provides methods of treating secretory diarrhea or cystic fibrosis in a mammal which comprises administering to a mammal in need thereof an effective amount of diarylsulfonylurea. This invention also describes specific diarylsulfonylureas for use in treating secretory diarrhea or cystic fibrosis.Type: GrantFiled: January 31, 2000Date of Patent: August 28, 2001Assignee: Eli Lilly and CompanyInventor: Bruce D Schultz
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Patent number: 6245255Abstract: A dispersion comprises a solvent having dispersed therein a liquid-crystal forming dye of structural Formula I, II or III: wherein the substituent are as defined in the specification. The dispersion is particularly useful in imaging and photographic elements.Type: GrantFiled: May 23, 2000Date of Patent: June 12, 2001Assignee: Eastman Kodak CompanyInventors: Margaret J. Helber, William J. Harrison, Kevin W. Williams, Steven W. Kortum
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Patent number: 6217642Abstract: A method and composition for protection against fouling of objects which come into contact with sea water or brackish water comprising a benzothiophene-2-carbomide S,S-dioxide as the essential component are described.Type: GrantFiled: March 11, 1998Date of Patent: April 17, 2001Assignee: Bayer AktiengesellschaftInventors: Franz Kunisch, Martin Kugler, Heinrich Schrage, Hans-Ludwig Elbe
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Patent number: 6207686Abstract: A compound of formula (I), in which: R1 is lower alkyl, cyclo(lower)alkyl, optionally substituted aryl, optionally substituted heterocyclic group, cyclo(lower)alkyl(lower)alkyl, or ar(lower)alkyl; R2 is hydrogen, hydroxy or protected hydroxy; R3 is lower alkyl, aryl, ar(lower)alkyl or optionally substituted heterocyclic(lower)alkyl; R4 is carboxy, protected carboxy or lower alkylsufonylcarbamoyl; R5 is hydrogen or lower alkyl; R6 is hydrogen or heterocyclic group; A is a single bond or lower alkylene, and Ar is optionally substituted aryl, or pharmaceutically acceptable salts thereof, having endothelin antagonistic activity.Type: GrantFiled: June 20, 1997Date of Patent: March 27, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masahiro Neya, Tatsuya Zenkoh, Hitoshi Sawada, Chiyoshi Kasahara, Masayoshi Murata, Keiji Hemmi
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Patent number: 6194450Abstract: Novel pharmaceutically/cosmetically-active polyaromatic heterocyclic compounds have the structural formula (I): in which Z is a divalent radical selected from among —O—, —S— or —Nr′— and Ar is either a radical having the following structural formula (II): or a radical having the following structural formula (III): 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: July 23, 1998Date of Patent: February 27, 2001Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Bruno Charpentier, Philippe Diaz, Philippe Nedoncelle
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Patent number: 6169087Abstract: The present invention provides novel compounds of Formula 1 or Formula 2 and compositions thereof, methods of their use, and methods of their manufacture, wherein X, Y, Z, W, R1, R2 and R3 are defined more fully in the description. These compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, and a number of other diseases.Type: GrantFiled: September 21, 1998Date of Patent: January 2, 2001Assignees: Novo Nordisk A/S, OntogenInventors: Henrik Sune Andersen, Sven Branner, Claus Bekker Jeppesen, Niels Peter Hundahl Moeller, Adnan M. M. Mjalli, Sepehr Sarshar
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Patent number: 6103912Abstract: A novel class of bridged indicator dyes is disclosed which possess absorption in the infrared region of the electromagnetic spectrum. These bridged indicator dyes are useful as light-absorbing, pH-sensitive optical filter agents in diffusion transfer photographic processes adapted to be performed in the presence of ambient light and to diffusion transfer products useful in such processes. These indicator dyes will also find utility in titrations and other analytical techniques and products where pH-sensitive indicator dyes are employed and absorption of infrared is useful.Type: GrantFiled: March 31, 1993Date of Patent: August 15, 2000Assignee: Polaroid CorporationInventors: Charles E. Jandrue, Sr., Marcis M. Kampe, Myron S. Simon, David P. Waller, David C. Whritenour
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Patent number: 6063936Abstract: An aromatic carboxylic acid bicyclic sulfur compound of the following formula: ##STR1## wherein X.sup.1 is selected from the group consisting of C.sub.1 to C.sub.4 alkyl, halogen, C.sub.1 to C.sub.4 haloalkyl, C.sub.2 to C.sub.4 alkoxyalkyl, C.sub.1 to C.sub.4 alkoxy and C.sub.1 to C.sub.4 haloalkoxy; each of X.sup.2 and X.sup.3 is independently selected from the group consisting of hydrogen, C.sub.1 to C.sub.4 alkyl and C.sub.1 to C.sub.4 haloalkyl; X.sup.4 is selected from the group consisting of hydrogen, halogen, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 haloalkyl and C.sub.1 to C.sub.4 alkoxy; each of X.sup.5, X.sup.6, X.sup.7 and X.sup.8 is independently hydrogen or C.sub.1 to C.sub.4 alkyl; the bond between X.sup.2 and X.sup.5 is saturated or unsaturated; the bond between X.sup.5 and X.sup.7 is saturated or unsaturated; p is an integer of 0 or 1; and n is an integer of 0, 1 or 2; or a salt thereof.Type: GrantFiled: December 15, 1997Date of Patent: May 16, 2000Assignee: Idemitsu Kosan Co., Ltd.Inventors: Kazufumi Nakamura, Masashi Sakamoto, Ichiro Nasuno
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Patent number: 6028069Abstract: Cyclic sulphones of formula (I) are disclosed, in which: R.sup.1 and R.sup.2 each independently of one another stand for H, A, CF.sub.3, CH.sub.2 F, CHF.sub.2, C.sub.2 F.sub.5, Hal, OH, OA, NH.sub.2, NHA, NA.sub.2, NO.sub.2 or CN; X stands for CR.sup.4 R.sup.5, C.dbd.Z, O, S, NH, NA or NR.sup.3 ; Y stands for CR.sup.6 R.sup.7, C.dbd.Z, O, NH, NA, or NR.sup.3 ; Z stands for O, S, NH, NA, NOH, NOA, CH.sub.2, CHA or CA.sub.2 ; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each independently of one another stand for H, A, R.sup.3, Hal, OH, OA, SH, SA, NH.sub.2, NHA or NA.sub.2, or alternatively, R.sup.5 and R.sup.6 or R.sup.7 and R.sup.8 can together represent a bond, only one such bond being present in each molecule; R.sup.4 and R.sup.5 together can also stand for O--(CH.sub.2).sub.2 --O or O--(CH.sub.2).sub.3 --O; R.sup.8 and R.sup.9 each independently of one another stand for H or A; A stands for alkyl with 1-6 C atoms; Hal stands for F, Cl, Br or I; and R.sup.Type: GrantFiled: March 30, 1999Date of Patent: February 22, 2000Assignee: Merck Patent Gesellschaft mit berschranker HaftungInventors: Manfred Baumgarth, Rolf Gericke, Klaus-Otto Minck, Norbert Beier
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Patent number: 5989451Abstract: This invention provides chiral thioindigo compounds for doping smectic liquid crystal hosts, wherein the compounds modulate a chiral bulk property of an induced chiral smectic liquid crystal phase upon irradiation at a wavelength in the visible range. Modulation of the chiral bulk property is effected by reversible trans-cis photoisomerization of the compound upon irradiation. The compounds maintain their rod-like shape in both isomeric forms, and hence do not destabilize the chiral smectic liquid crystal phase. Compounds according to the invention are useful in optical devices such as optical switches, displays, and memory.Type: GrantFiled: February 6, 1998Date of Patent: November 23, 1999Assignee: Queen's University at KingstonInventors: Robert P. Lemieux, Liviu Dinescu
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Patent number: 5986109Abstract: A compound of fomula XIV: ##STR1## wherein: R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is a hydoxy protecting group;R.sup.2a is --H, halo, or OR.sup.8a in which R.sup.8a is a hydroxy protecting group; andR.sup.Type: GrantFiled: June 18, 1998Date of Patent: November 16, 1999Assignee: Eli Lilly and CompanyInventors: Alan David Palkowitz, Kenneth Jeff Thrasher
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Patent number: 5981765Abstract: The present invention provides a compound of formula ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is a hydroxy protecting group;R.sup.6 is --H or a hydroxy protecting group which can be selectively removed;R.sup.11 is non-existent or .dbd.O; andZ is --O-- or --S--;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 18, 1998Date of Patent: November 9, 1999Assignee: Eli Lilly and CompanyInventors: Alan David Palkowitz, Kenneth Jeff Thrasher
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Patent number: 5977382Abstract: The instant invention provides novel benzo[b]thiophene compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.Type: GrantFiled: June 30, 1998Date of Patent: November 2, 1999Assignee: Eli Lilly and CompanyInventor: Alan David Palkowitz
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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