S Of S-x-c Attached Directly To A Benzene Ring Patents (Class 514/518)
  • Patent number: 10813904
    Abstract: 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: Grant
    Filed: February 21, 2018
    Date of Patent: October 27, 2020
    Assignee: University of Florida Research Foundation, Incorporated
    Inventors: Brian Keith Law, Ronald K. Castellano, Renan B. Ferreira
  • Patent number: 10188111
    Abstract: 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: Grant
    Filed: October 5, 2016
    Date of Patent: January 29, 2019
    Assignee: Hypo-Stream Limited
    Inventor: Myles H. E. Dakin
  • Publication number: 20150119426
    Abstract: 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: Application
    Filed: March 15, 2013
    Publication date: April 30, 2015
    Inventors: Juan Jose Marugan, Jingbo Xiao, Marc Ferrer-Alegre, Catherine Chen, Noel Southall, Wei Zheng, Alexander Agoulnik, Irina Agoulnik
  • Patent number: 8980869
    Abstract: 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: Grant
    Filed: July 9, 2013
    Date of Patent: March 17, 2015
    Assignee: AmDerma Pharmaceuticals, LLC
    Inventor: Pedro Cuevas Sànchez
  • Patent number: 8912171
    Abstract: 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: Grant
    Filed: July 9, 2013
    Date of Patent: December 16, 2014
    Assignee: AmDerma Pharmaceuticals, LLC
    Inventor: Pedro Cuevas Sànchez
  • Publication number: 20140329900
    Abstract: 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: Application
    Filed: April 7, 2014
    Publication date: November 6, 2014
    Applicants: H. Lee Moffitt Cancer Center And Research Institute, Inc., University of Central Florida, University of South Florida
    Inventors: JAMES TURKSON, SAID M. SEBTI, WAYNE GUIDA, MAN LUN YIP, NICHOLAS LAWRENCE, HARSHANI RITHMA LAWRENCE, BENJAMIN GREEDY
  • Patent number: 8865736
    Abstract: 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: Grant
    Filed: November 28, 2011
    Date of Patent: October 21, 2014
    Assignee: Biota Scientific Pty Ltd
    Inventors: David Ryall Brown, Ian Collins, Lloyd George Czaplewski, David John Haydon
  • Patent number: 8815836
    Abstract: 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: Grant
    Filed: August 15, 2011
    Date of Patent: August 26, 2014
    Assignee: AmDerma Pharmaceuticals, LLC
    Inventors: Pedro Cueva Sànchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Gorman, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
  • Publication number: 20140221477
    Abstract: 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: Application
    Filed: April 10, 2014
    Publication date: August 7, 2014
    Applicant: BRACCO IMAGING S.P.A.
    Inventors: Pier Lucio ANELLI, Maria ARGESE, Valeria BOI, Livio CAVALIERI, Laura GALIMBERTI, Sonia GAZZETTO, Luciano LATTUADA, Fulvia VELLA
  • Publication number: 20140206654
    Abstract: 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: Application
    Filed: August 12, 2013
    Publication date: July 24, 2014
    Applicant: 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
  • Patent number: 8765808
    Abstract: 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: Grant
    Filed: October 26, 2007
    Date of Patent: July 1, 2014
    Assignee: CHS Pharma, Inc.
    Inventors: Herbert Weissbach, Lionel Resnick, David Binninger
  • Publication number: 20140155420
    Abstract: 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: Application
    Filed: January 10, 2012
    Publication date: June 5, 2014
    Applicants: The Regents of the University of Colorado, a body corporate, Department of Health and Human Services
    Inventors: Rui Zhao, Heide L. Ford, Noel Southall, Erika Englund, Samarjit Patnaik, Marc Ferrer, Wei Zheng, Seameen Dehdashti, Juan Marugan
  • Publication number: 20140088191
    Abstract: The invention provides compositions and methods for inhibiting renal fibrosis.
    Type: Application
    Filed: May 21, 2012
    Publication date: March 27, 2014
    Applicant: RHODE ISLAND HOSPITAL
    Inventor: Shougang Zhuang
  • Publication number: 20140018330
    Abstract: 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: Application
    Filed: July 9, 2013
    Publication date: January 16, 2014
    Inventors: Pedro Cuevas Sànchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Gorman, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
  • Patent number: 8613909
    Abstract: 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: Grant
    Filed: June 25, 2013
    Date of Patent: December 24, 2013
    Assignee: Virginia Commonwealth University
    Inventors: Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
  • Patent number: 8603985
    Abstract: 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: Grant
    Filed: April 14, 2010
    Date of Patent: December 10, 2013
    Assignee: CHS Pharma, Inc
    Inventors: Herbert Weissbach, Lionel Resnick, David Binninger
  • Patent number: 8586607
    Abstract: 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: Grant
    Filed: July 23, 2009
    Date of Patent: November 19, 2013
    Assignee: Syddansk Universitet
    Inventors: Trond Ulven, Elisabeth Christiansen
  • Patent number: 8497257
    Abstract: 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: Grant
    Filed: October 24, 2008
    Date of Patent: July 30, 2013
    Assignee: Amderma Pharmaceuticals, LLC
    Inventor: Pedro Cuevas Sanchez
  • Patent number: 8491872
    Abstract: 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: Grant
    Filed: August 4, 2009
    Date of Patent: July 23, 2013
    Assignee: Virginia Commonwealth University
    Inventors: Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
  • Patent number: 8492367
    Abstract: 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: Grant
    Filed: June 6, 2011
    Date of Patent: July 23, 2013
    Assignee: AmDerma Pharmaceuticals, LLC
    Inventors: Pedro Cuevas Sánchez, Guillermo Gimenez Gallego, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
  • Patent number: 8436045
    Abstract: 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: Grant
    Filed: November 15, 2010
    Date of Patent: May 7, 2013
    Assignee: AmDerma Pharmaceuticals, LLC
    Inventor: Pedro Cuevas Sánchez
  • Publication number: 20130072520
    Abstract: 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, nit
    Type: Application
    Filed: November 28, 2011
    Publication date: March 21, 2013
    Applicant: Biota Scientific Management Pty Ltd
    Inventors: David BROWN, Ian COLLINS, Lloyd CZAPLEWSKI, David HAYDON
  • Patent number: 8357720
    Abstract: 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: Grant
    Filed: September 10, 2009
    Date of Patent: January 22, 2013
    Assignee: Florida Atlantic University
    Inventors: Herbert Weissbach, Lionel Resnick, David Binninger
  • Patent number: 8258181
    Abstract: 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: Grant
    Filed: March 23, 2006
    Date of Patent: September 4, 2012
    Assignee: Florida Atlantic University
    Inventors: Herbert Weissbach, Lionel Resnick, David Binninger
  • Publication number: 20120149678
    Abstract: 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: Application
    Filed: December 9, 2011
    Publication date: June 14, 2012
    Inventors: Bryan T. Oronsky, Susan Knox, Jan Scicinski, Shoucheng Ning
  • Publication number: 20120122918
    Abstract: 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: Application
    Filed: November 28, 2011
    Publication date: May 17, 2012
    Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTD
    Inventors: David Ryall BROWN, Ian COLLINS, Lloyd George CZAPLEWSKI, David John HAYDON
  • Publication number: 20120027691
    Abstract: 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: Application
    Filed: August 4, 2009
    Publication date: February 2, 2012
    Inventors: Umesh R. Desai, Brian L. Henry, Aiye Liang, Jay Thakkar, John B. Mangrum, Ivo Torres Filho, Bruce D. Spiess, Masahiro Sakagami, Bhawana Saluja
  • Publication number: 20120015912
    Abstract: 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: Application
    Filed: January 7, 2011
    Publication date: January 19, 2012
    Applicant: Action Medicines
    Inventors: 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
  • Publication number: 20110311528
    Abstract: 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: Application
    Filed: June 22, 2011
    Publication date: December 22, 2011
    Applicant: Action Medicines
    Inventors: Pedro Cuevas Sánchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Gorman, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
  • Publication number: 20110275603
    Abstract: 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: Application
    Filed: May 5, 2011
    Publication date: November 10, 2011
    Applicants: Rhizen Pharmaceuticals SA, Incozen Therapeutics Pvt. Ltd.
    Inventors: Meyyappan MUTHUPPALANIAPPAN, Prashant K. BHAVAR, Srikant VISWANADHA, Swaroop Kumar V.S. VAKKALANKA, Gayatri S. MERIKAPUDI
  • Publication number: 20110257264
    Abstract: 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: Application
    Filed: November 15, 2010
    Publication date: October 20, 2011
    Applicant: Action Medicines
    Inventors: 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
  • Publication number: 20110237555
    Abstract: 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: Application
    Filed: June 6, 2011
    Publication date: September 29, 2011
    Applicant: Action Medicines
    Inventors: Pedro Cuevas Sánchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Morgan, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
  • Publication number: 20110201576
    Abstract: 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: Application
    Filed: February 4, 2011
    Publication date: August 18, 2011
    Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South Florida, University of Central Florida
    Inventors: James Turkson, Said M. Sebti, Wayne Guida, Man Lun Yip, Nicholas J. Lawrence, Harshani Lawrence, Benjamin Greedy
  • Publication number: 20110166157
    Abstract: 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: Application
    Filed: March 11, 2011
    Publication date: July 7, 2011
    Applicant: ALBIREO AB
    Inventors: Anders Broo, Johan Gottfries, Michael Kossenjans, Li Lanna, Eva-Lotte Lindstedt-Alstermark, Kristina A. Nilsson, Bengt Ohlsson, Maria Thorstensson, Maria Boije, Per Olof Sjögren
  • Publication number: 20110166223
    Abstract: 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: Application
    Filed: August 19, 2009
    Publication date: July 7, 2011
    Applicant: CEDARS-SINAI MEDICAL CENTER
    Inventors: Pavel Krejci, William Wilcox
  • Publication number: 20110152315
    Abstract: 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: Application
    Filed: July 23, 2009
    Publication date: June 23, 2011
    Inventors: Trond Ulven, Elisabeth Christiansen
  • Publication number: 20110152222
    Abstract: 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: Application
    Filed: August 15, 2007
    Publication date: June 23, 2011
    Inventors: Pedro Cuevas Sànchez, Guillermo Gimenez Gallego
  • Patent number: 7960434
    Abstract: 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: Grant
    Filed: May 21, 2007
    Date of Patent: June 14, 2011
    Assignees: University of South Florida, University of Central Florida Research Foundation, Inc., H. Lee Moffitt Cancer Center & Research Institute
    Inventors: James Turkson, Said M. Sebti, Wayne Guida, Man Lun Yip, Nicholas J. Lawrence, Harshani Lawrence, Benjamin Greedy
  • Patent number: 7951972
    Abstract: 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: Grant
    Filed: February 2, 2009
    Date of Patent: May 31, 2011
    Assignee: 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
  • Publication number: 20100324058
    Abstract: 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: Application
    Filed: June 27, 2008
    Publication date: December 23, 2010
    Applicant: 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
  • Publication number: 20100273739
    Abstract: 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: Application
    Filed: February 16, 2010
    Publication date: October 28, 2010
    Inventors: Wilhelm Amberg, Micheal Ochse, Udo Lange, Andreas King, Berthold Behl, Wilfried Hamberger, Maric Mezier, Charles W. Hutchins
  • Publication number: 20100234456
    Abstract: 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: Application
    Filed: May 25, 2010
    Publication date: September 16, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Michael D. Wendt, Hong Ding, Sheela A. Thomas, Steven W. Elmore, Wang Shen, Daniel A. Dickman, David Augeri
  • Publication number: 20100233086
    Abstract: 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: Application
    Filed: October 14, 2008
    Publication date: September 16, 2010
    Inventors: Lutz Lehmann, Andrea Thiele, Tobias Heinrich, Thomas Brumby, Christer Halldin, Balazs Gulyas, Sangram Nag
  • Publication number: 20100227791
    Abstract: 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: Application
    Filed: January 7, 2010
    Publication date: September 9, 2010
    Inventors: Gianfranco Peluso, Menotti Calvani
  • Publication number: 20100216835
    Abstract: 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: Application
    Filed: February 25, 2010
    Publication date: August 26, 2010
    Inventors: Jo E. Handelsman, Bradley R. Borlee
  • Patent number: 7605166
    Abstract: 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: Grant
    Filed: June 25, 2004
    Date of Patent: October 20, 2009
    Assignee: Elan Pharmaceuticals Inc.
    Inventors: Theodore A. Yednock, Stephen B. Freedman, Ivan Lieberburg, Michael A. Pleiss, Andrei W. Konradi, George Shopp, Elizabeth Messersmith
  • Publication number: 20090069420
    Abstract: 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: Application
    Filed: May 21, 2007
    Publication date: March 12, 2009
    Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South Florida
    Inventors: James Turkson, Said M. Sebti, Wayne Guida, Man Lun Yip, Nicholas J. Lawrence, Harshani Lawrence, Benjamin Greedy
  • Patent number: 7498358
    Abstract: 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: Grant
    Filed: December 13, 2002
    Date of Patent: March 3, 2009
    Assignee: 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
  • Patent number: 7485667
    Abstract: 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: Grant
    Filed: February 21, 2007
    Date of Patent: February 3, 2009
    Assignee: Wyeth Holdings Corporation
    Inventors: Jeremy Ian Levin, Mila Ti Du
  • Patent number: 7449599
    Abstract: 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: Grant
    Filed: May 9, 2005
    Date of Patent: November 11, 2008
    Assignee: 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