S Of S-x-c Attached Directly To A Benzene Ring Patents (Class 514/518)
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Patent number: 10813904Abstract: The invention relates to methods of treating cell proliferative disorders. The invention further relates to pharmaceutical compositions for treating cell proliferative disorders, especially cancer.Type: GrantFiled: February 21, 2018Date of Patent: October 27, 2020Assignee: University of Florida Research Foundation, IncorporatedInventors: Brian Keith Law, Ronald K. Castellano, Renan B. Ferreira
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Patent number: 10188111Abstract: A pharmaceutically acceptable composition comprising dilute stabilized sodium hypochlorite solution and an indicator to show that the dilute stabilized sodium hypochlorite solution is fresh and active.Type: GrantFiled: October 5, 2016Date of Patent: January 29, 2019Assignee: Hypo-Stream LimitedInventor: Myles H. E. Dakin
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Publication number: 20150119426Abstract: Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R1, and R2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.Type: ApplicationFiled: March 15, 2013Publication date: April 30, 2015Inventors: Juan Jose Marugan, Jingbo Xiao, Marc Ferrer-Alegre, Catherine Chen, Noel Southall, Wei Zheng, Alexander Agoulnik, Irina Agoulnik
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Patent number: 8980869Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, rosacea.Type: GrantFiled: July 9, 2013Date of Patent: March 17, 2015Assignee: AmDerma Pharmaceuticals, LLCInventor: Pedro Cuevas Sànchez
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Patent number: 8912171Abstract: The invention describes compositions and methods of use for 2,5-dihydroxybenzene sulfonic acid compounds and pharmaceutically acceptable salts thereof. The invention provides methods for (a) treating skin cancer; (b) treating cancer of the organs; (c) treating leukemia; (d) improving the efficacy of chemotherapy, radiation therapy and/or cancer immunotherapy; (e) treating rosacea; and (f) treating psoriasis by administration of a composition comprising at least one 2,5-dihydroxybenzene sulfonic acid compound or a pharmaceutically acceptable salt thereof, and, optionally at least one therapeutic agent. Also disclosed are compositions comprising administration of at least one 2,5-dihydroxybenzene sulfonic acid compound, or a pharmaceutically acceptable salt thereof, and, at least one therapeutic agent.Type: GrantFiled: July 9, 2013Date of Patent: December 16, 2014Assignee: AmDerma Pharmaceuticals, LLCInventor: Pedro Cuevas Sànchez
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Publication number: 20140329900Abstract: The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S31-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis.Type: ApplicationFiled: April 7, 2014Publication date: November 6, 2014Applicants: H. Lee Moffitt Cancer Center And Research Institute, Inc., University of Central Florida, University of South FloridaInventors: JAMES TURKSON, SAID M. SEBTI, WAYNE GUIDA, MAN LUN YIP, NICHOLAS LAWRENCE, HARSHANI RITHMA LAWRENCE, BENJAMIN GREEDY
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Patent number: 8865736Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q.Type: GrantFiled: November 28, 2011Date of Patent: October 21, 2014Assignee: Biota Scientific Pty LtdInventors: David Ryall Brown, Ian Collins, Lloyd George Czaplewski, David John Haydon
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Patent number: 8815836Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative represented by Formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the therapeutic and/or prophylactic treatment of, inter alia, dermatitis.Type: GrantFiled: August 15, 2011Date of Patent: August 26, 2014Assignee: AmDerma Pharmaceuticals, LLCInventors: Pedro Cueva Sànchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Gorman, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
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Publication number: 20140221477Abstract: The present invention relates to a process for the preparation of the mono sodium salt of the derivative 3,5-diiodo-O-[3-iodo-4-(sulphooxy)phenyl]-L-tyrosine (T3S) by starting from the corresponding phenolic compound, in the presence of chlorosulfonic acid and dimethylacetamide as a solvent. The so obtained T3S compound may conveniently be isolated in a pure form as a solid in good yields. The present invention further relates to the process for T3S preparation, wherein the starting reagent is T2 and further comprising the formulation of such compound in tablets. Furthermore, the invention discloses non-radioactive immunoassays based on T3S derivatives.Type: ApplicationFiled: April 10, 2014Publication date: August 7, 2014Applicant: BRACCO IMAGING S.P.A.Inventors: Pier Lucio ANELLI, Maria ARGESE, Valeria BOI, Livio CAVALIERI, Laura GALIMBERTI, Sonia GAZZETTO, Luciano LATTUADA, Fulvia VELLA
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Publication number: 20140206654Abstract: The present invention refers to the use of a compound of Formula (I?) or pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of hematological dyscrasias, including myelodysplastic syndromes (MDSs) and for improving the efficacy of chemotherapy, radiation therapy and/or cancer immunotherapy. In addition, it relates to the use of a compound of formula (I?) for the treatment and/or prophylaxis of cancer of an organ.Type: ApplicationFiled: August 12, 2013Publication date: July 24, 2014Applicant: Action Medicines, S.L.Inventors: Pedro Cuevas Sanchez, Guillermo Gimenez Gallego, Inigo Saenz De Tejada Morgan, Javier Angulo Frutos, Rosa Maria Lozano Puerto, Antonio Romero Garrido, Serafin Valverde Lopez
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Patent number: 8765808Abstract: The NSAID, sulindac and/or its metabolites and derivatives, in combination with hydrogen peroxide or another oxidizing agent, such as arsenic trioxide that generates reactive oxygen species (ROS), significantly enhances the killing of cancer cells. This effect occurs at concentrations of each compound that individually have little or no activity directed against cancer cells. A skin cream has been developed and used to treat skin cancer and precancerous skin growths that effectively removes the lesions with no effect on surrounding normal skin.Type: GrantFiled: October 26, 2007Date of Patent: July 1, 2014Assignee: CHS Pharma, Inc.Inventors: Herbert Weissbach, Lionel Resnick, David Binninger
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Publication number: 20140155420Abstract: The invention provides small molecule inhibitors of EYA2 phosphatase activity and EYA2 binding to Six1. These inhibitors are proposed for use in methods of treating cancer in a subject, such as those involving Six1 and/or EYA2 disregulation. In some embodiments, the invention further provides for the administration of a second cancer therapy to the subject.Type: ApplicationFiled: January 10, 2012Publication date: June 5, 2014Applicants: The Regents of the University of Colorado, a body corporate, Department of Health and Human ServicesInventors: Rui Zhao, Heide L. Ford, Noel Southall, Erika Englund, Samarjit Patnaik, Marc Ferrer, Wei Zheng, Seameen Dehdashti, Juan Marugan
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Publication number: 20140088191Abstract: The invention provides compositions and methods for inhibiting renal fibrosis.Type: ApplicationFiled: May 21, 2012Publication date: March 27, 2014Applicant: RHODE ISLAND HOSPITALInventor: Shougang Zhuang
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Publication number: 20140018330Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, rosacea.Type: ApplicationFiled: July 9, 2013Publication date: January 16, 2014Inventors: Pedro Cuevas Sànchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Gorman, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
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Patent number: 8613909Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.Type: GrantFiled: June 25, 2013Date of Patent: December 24, 2013Assignee: Virginia Commonwealth UniversityInventors: Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
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Patent number: 8603985Abstract: The NSAID, sulindac and/or its metabolites and derivatives, in combination with hydrogen peroxide or another oxidizing agent, such as arsenic trioxide that generates reactive oxygen species (ROS), significantly enhances the killing of cancer cells. This effect occurs at concentrations of each compound that individually have little or no activity directed against cancer cells. A skin cream has been developed and used to treat skin cancer and precancerous skin growths that effectively removes the lesions with no effect on surrounding normal skin.Type: GrantFiled: April 14, 2010Date of Patent: December 10, 2013Assignee: CHS Pharma, IncInventors: Herbert Weissbach, Lionel Resnick, David Binninger
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Patent number: 8586607Abstract: There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.Type: GrantFiled: July 23, 2009Date of Patent: November 19, 2013Assignee: Syddansk UniversitetInventors: Trond Ulven, Elisabeth Christiansen
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Patent number: 8497257Abstract: The invention describes compositions and methods of use for 2,5-dihydroxybenzene sulfonic acid compounds and pharmaceutically acceptable salts thereof. The invention provides methods for (a) treating skin cancer; (b) treating cancer of the organs; (c) treating leukemia; (d) improving the efficacy of chemotherapy, radiation therapy and/or cancer immunotherapy; (e) treating rosacea; and (f) treating psoriasis by administration of a composition comprising at least one 2,5-dihydroxybenzene sulfonic acid compound or a pharmaceutically acceptable salt thereof, and, optionally at least one therapeutic agent. Also disclosed are compositions comprising administration of at least one 2,5-dihydroxybenzene sulfonic acid compound, or a pharmaceutically acceptable salt thereof, and, at least one therapeutic agent.Type: GrantFiled: October 24, 2008Date of Patent: July 30, 2013Assignee: Amderma Pharmaceuticals, LLCInventor: Pedro Cuevas Sanchez
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Patent number: 8491872Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.Type: GrantFiled: August 4, 2009Date of Patent: July 23, 2013Assignee: Virginia Commonwealth UniversityInventors: Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
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Patent number: 8492367Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, rosacea.Type: GrantFiled: June 6, 2011Date of Patent: July 23, 2013Assignee: AmDerma Pharmaceuticals, LLCInventors: Pedro Cuevas Sánchez, Guillermo Gimenez Gallego, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
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Patent number: 8436045Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative represented by Formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the therapeutic and/or prophylactic treatment of, inter alia, actinic keratosis.Type: GrantFiled: November 15, 2010Date of Patent: May 7, 2013Assignee: AmDerma Pharmaceuticals, LLCInventor: Pedro Cuevas Sánchez
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Publication number: 20130072520Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)— or ?N—; R1 is hydrogen or an optional substituent and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2—, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(?O)—, —O—(C?O)—, —C(?O)—O—, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, or —N(CH2CH3)—; and Q is hydrogen, halogen, nitType: ApplicationFiled: November 28, 2011Publication date: March 21, 2013Applicant: Biota Scientific Management Pty LtdInventors: David BROWN, Ian COLLINS, Lloyd CZAPLEWSKI, David HAYDON
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Patent number: 8357720Abstract: The NSAID, sulindac and/or its metabolites and derivatives, in combination with an agent that generates or induces reactive oxygen species (ROS), significantly enhances the killing of abnormal cells but does not affect normal cells. This effect occurs at concentrations of each compound that individually have little or no activity directed against the abnormal cells.Type: GrantFiled: September 10, 2009Date of Patent: January 22, 2013Assignee: Florida Atlantic UniversityInventors: Herbert Weissbach, Lionel Resnick, David Binninger
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Patent number: 8258181Abstract: The NSAID, sulindac and/or its metabolites and derivatives, in combination with hydrogen peroxide or another oxidizing agent, such as arsenic trioxide that generates reactive oxygen species (ROS), significantly enhances the killing of cancer cells. This effect occurs at concentrations of each compound that individually have little or no activity directed against cancer cells. A skin cream has been developed and used to treat skin cancer and precancerous skin growths that effectively removes the lesions with no effect on surrounding normal skin.Type: GrantFiled: March 23, 2006Date of Patent: September 4, 2012Assignee: Florida Atlantic UniversityInventors: Herbert Weissbach, Lionel Resnick, David Binninger
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Publication number: 20120149678Abstract: The invention provides organonitro compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat non-Hodgkin's lymphoma and certain leukemias in a patient. The compounds, compositions, kits, and methods are contemplated to provide a therapeutic benefit in treating non-Hodgkin's lymphoma, chronic lymphocytic leukemia, acute myelogenous leukemia, chronic myelogenous leukemia, and acute lymphoblastic leukemia. Exemplary organonitro compounds described herein include alkyl-substituted and acyl-substituted di-nitroheterocycles.Type: ApplicationFiled: December 9, 2011Publication date: June 14, 2012Inventors: Bryan T. Oronsky, Susan Knox, Jan Scicinski, Shoucheng Ning
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Publication number: 20120122918Abstract: Compounds of formula (1) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)-Q.Type: ApplicationFiled: November 28, 2011Publication date: May 17, 2012Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTDInventors: David Ryall BROWN, Ian COLLINS, Lloyd George CZAPLEWSKI, David John HAYDON
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Publication number: 20120027691Abstract: Cinnamic acid-based oligomers and therapeutic uses thereof are provided. The oligomers are used as anti-inflammation agents, inhibitors of elastase and anti-oxidants, and in some cases (e.g. the treatment of lung disorders such as lung cancer) all three activities are simultaneously beneficial. Subsets of the oligomers (e.g. ?-O4 and ?-5 trimers and tetramers) are used as anticoagulants.Type: ApplicationFiled: August 4, 2009Publication date: February 2, 2012Inventors: Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
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Publication number: 20120015912Abstract: The present invention relates to the use of a compound of Formula (IIV) or pharmaceutically acceptable salt or solvate, isomer or prodrug thereof in the manufacturing of a medicament for the treatment and/or prophylaxis of any of the diseases selected from the group consisting of macular degeneration, corneal neovascularization or angiogenesis, iris neovascularization or angiogenesis, retinal neovascularization or angiogenesis, diabetic proliferative retinopathy and non-diabetic proliferative retinopathy.Type: ApplicationFiled: January 7, 2011Publication date: January 19, 2012Applicant: Action MedicinesInventors: Pedro Cuevas Sánchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Morgan, Maria Luisa Krauel, Javier Angulo Frutos, Rosa Maria Lozano Puerto, Antonio Romero Garrido, Serafin Valverde Lopez
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Publication number: 20110311528Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, psoriasis.Type: ApplicationFiled: June 22, 2011Publication date: December 22, 2011Applicant: Action MedicinesInventors: Pedro Cuevas Sánchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Gorman, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
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Publication number: 20110275603Abstract: The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.Type: ApplicationFiled: May 5, 2011Publication date: November 10, 2011Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.Inventors: Meyyappan MUTHUPPALANIAPPAN, Prashant K. BHAVAR, Srikant VISWANADHA, Swaroop Kumar V.S. VAKKALANKA, Gayatri S. MERIKAPUDI
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Publication number: 20110257264Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative represented by Formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the therapeutic and/or prophylactic treatment of, inter alia, actinic keratosis.Type: ApplicationFiled: November 15, 2010Publication date: October 20, 2011Applicant: Action MedicinesInventors: Pedro Cuevas S?nchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Morgan, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
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Publication number: 20110237555Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, rosacea.Type: ApplicationFiled: June 6, 2011Publication date: September 29, 2011Applicant: Action MedicinesInventors: Pedro Cuevas Sánchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Morgan, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
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Publication number: 20110201576Abstract: The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S3I-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis.Type: ApplicationFiled: February 4, 2011Publication date: August 18, 2011Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South Florida, University of Central FloridaInventors: James Turkson, Said M. Sebti, Wayne Guida, Man Lun Yip, Nicholas J. Lawrence, Harshani Lawrence, Benjamin Greedy
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Publication number: 20110166157Abstract: The present invention relates to 2-(substituted sulphur, sulphone or sulphoxide)-3-(substituted phenyl)propionic acid derivatives, 2-(substituted oxygen)-3-(substituted phenyl)propionic acid derivatives, benzoic acid derivatives, and derivatives of 2-methyl-2-(phenoxy or phenylthio)propanoic acid and 2-(methyl or ethyl)-2-(phenoxy or phenylthio)butanoic acid, to processes for preparing such compounds, to their use in the treatment of inflammatory conditions, and to pharmaceutical compositions containing them.Type: ApplicationFiled: March 11, 2011Publication date: July 7, 2011Applicant: ALBIREO ABInventors: Anders Broo, Johan Gottfries, Michael Kossenjans, Li Lanna, Eva-Lotte Lindstedt-Alstermark, Kristina A. Nilsson, Bengt Ohlsson, Maria Thorstensson, Maria Boije, Per Olof Sjögren
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Publication number: 20110166223Abstract: Novel inhibitors of FGFR3 signaling having a structure shown as Formula 1 and a method of inhibiting FGFR3 signaling by administering a quantity of the inhibitor, or pharmaceutical equivalent, analog and/or salt thereof, to a mammal are disclosed.Type: ApplicationFiled: August 19, 2009Publication date: July 7, 2011Applicant: CEDARS-SINAI MEDICAL CENTERInventors: Pavel Krejci, William Wilcox
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Publication number: 20110152315Abstract: There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type I1 diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.Type: ApplicationFiled: July 23, 2009Publication date: June 23, 2011Inventors: Trond Ulven, Elisabeth Christiansen
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Publication number: 20110152222Abstract: The present invention relates to the use of a compound of Formula (I??) or pharmaceutically acceptable salt or solvate, isomer or prodrug thereof in the manufacturing of a medicament for the treatment and/or prophylaxis of arthritis and pain.Type: ApplicationFiled: August 15, 2007Publication date: June 23, 2011Inventors: Pedro Cuevas Sànchez, Guillermo Gimenez Gallego
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Patent number: 7960434Abstract: The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S3I-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis.Type: GrantFiled: May 21, 2007Date of Patent: June 14, 2011Assignees: University of South Florida, University of Central Florida Research Foundation, Inc., H. Lee Moffitt Cancer Center & Research InstituteInventors: James Turkson, Said M. Sebti, Wayne Guida, Man Lun Yip, Nicholas J. Lawrence, Harshani Lawrence, Benjamin Greedy
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Patent number: 7951972Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chlorides and ADAM-10 modulators therefrom.Type: GrantFiled: February 2, 2009Date of Patent: May 31, 2011Assignee: Exelixis, Inc.Inventors: S. David Brown, Lynne Canne-Bannen, Erick Wang Co, Vasu Jammalamadaka, Rickard George Khoury, Moon Hwan Kim, Donna T. Le, Amy Lew Tsuhako, Morrison B. Mac, Shumeye Mamo, John M. Nuss, Michael P. Prisbylla, Wei Xu
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Publication number: 20100324058Abstract: This invention relates to new chemical compounds, application of these compound as thrombin inhibitors, and pharmaceutical compositions based on them, and can be used to treat and prevent thrombin-dependent thromboembolic events, and in research.Type: ApplicationFiled: June 27, 2008Publication date: December 23, 2010Applicant: Obschestvo S Organichennoi Otvetsttvennoctiyou "Bionika"Inventors: Elena Ivanovna Sinauridze, Fazoil Inoyatovich Ataullakhanov, Andrey Alexandrovich Butylin, Vladimir Borisovich Sulimov, Alexey Nickolayevich Romanov, Alexey Alexeevich Bogolyubov, Yury Vladimirovich Kuznetsov, Irina Vladimirovna Gribkova, Alexander Sergeevich Gorbatenko, Olga Anatolievna Kondakova
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Publication number: 20100273739Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: February 16, 2010Publication date: October 28, 2010Inventors: Wilhelm Amberg, Micheal Ochse, Udo Lange, Andreas King, Berthold Behl, Wilfried Hamberger, Maric Mezier, Charles W. Hutchins
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Publication number: 20100234456Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds and methods of treating diseases during which are expressed the Mcl-1 protein are disclosed.Type: ApplicationFiled: May 25, 2010Publication date: September 16, 2010Applicant: ABBOTT LABORATORIESInventors: Michael D. Wendt, Hong Ding, Sheela A. Thomas, Steven W. Elmore, Wang Shen, Daniel A. Dickman, David Augeri
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Publication number: 20100233086Abstract: This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).Type: ApplicationFiled: October 14, 2008Publication date: September 16, 2010Inventors: Lutz Lehmann, Andrea Thiele, Tobias Heinrich, Thomas Brumby, Christer Halldin, Balazs Gulyas, Sangram Nag
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Publication number: 20100227791Abstract: Disclosed is the use of compounds of formula (I) wherein X, Y and Z are as defined in the description of the invention, for the preparation of an antitumor medicament, optionally in combination with different biologically active substances.Type: ApplicationFiled: January 7, 2010Publication date: September 9, 2010Inventors: Gianfranco Peluso, Menotti Calvani
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Publication number: 20100216835Abstract: The present invention provides compositions and methods for modulating bacterial quorum sensing using antagonist or agonist compounds. Further, the present invention provides methods of treating or preventing microbial damages and diseases, in particular for diseases where there is an advantage in inhibiting quorum sensing regulated phenotypes of pathogens.Type: ApplicationFiled: February 25, 2010Publication date: August 26, 2010Inventors: Jo E. Handelsman, Bradley R. Borlee
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Patent number: 7605166Abstract: This application relates to methods and compositions for treating rheumatoid arthritis by administering a combination therapy comprising methotrexate and an antibody to alpha-4 integrin or an immunologically active antigen binding fragment in therapeutically effective amounts. The application also relates generally to methods and compositions for treating rheumatoid arthritis by administering a combination therapy comprising methotrexate and small molecule alpha-4 integrin antagonist that inhibits the alpha-4 integrin (?4 integrin) interaction with VCAM-1. The invention further relates to methods of preparing the compounds and methods of using the compounds and compositions.Type: GrantFiled: June 25, 2004Date of Patent: October 20, 2009Assignee: Elan Pharmaceuticals Inc.Inventors: Theodore A. Yednock, Stephen B. Freedman, Ivan Lieberburg, Michael A. Pleiss, Andrei W. Konradi, George Shopp, Elizabeth Messersmith
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Publication number: 20090069420Abstract: The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S3I-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis.Type: ApplicationFiled: May 21, 2007Publication date: March 12, 2009Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South FloridaInventors: James Turkson, Said M. Sebti, Wayne Guida, Man Lun Yip, Nicholas J. Lawrence, Harshani Lawrence, Benjamin Greedy
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Patent number: 7498358Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chlorides and ADAM-10 modulators therefrom.Type: GrantFiled: December 13, 2002Date of Patent: March 3, 2009Assignee: Exelixis, Inc.Inventors: S. David Brown, Lynne Canne-Bannen, Erick Wang Co, Vasu Jammalamadaka, Rickard George Khoury, Moon Hwan Kim, Donna T. Le, Amy Lew Tsuhako, Morrison B. Mac, Shumeye Mamo, John M. Nuss, Michael P. Prisbylla, Wei Xu
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Patent number: 7485667Abstract: Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-?, such as rheumatoid arthritis, graft rejection, cachexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease or HIV infection.Type: GrantFiled: February 21, 2007Date of Patent: February 3, 2009Assignee: Wyeth Holdings CorporationInventors: Jeremy Ian Levin, Mila Ti Du
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Patent number: 7449599Abstract: The present invention is directed to phenyl carboxamide compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: May 9, 2005Date of Patent: November 11, 2008Assignee: Merck + Co Inc.Inventors: Craig A. Coburn, Thomas G. Steele, Joseph P. Vacca, David Allen Annis, Jr., Gergely M. Makara, Huw M. Nash, Praveen K. Tadikonda, Tong Wang