Chalcogen Bonded Directly To The Bicyclo Ring System Patents (Class 544/144)
  • Patent number: 10752586
    Abstract: The present invention provides process for preparation of molindone (I) comprising: a) reacting compound with cyclohexane-1,3-dione to form 2-(2-oxopentan-3-yl)cyclohexane-1,3-dione wherein X is Cl, Br or I, b) cyclizing 2-(2-oxopentan-3-yl)cyclohexane-1,3-dione to 2-methyl-3-ethyl-4-oxo-4,5,6,7-tetrahydroindole, c) reacting 2-methyl-3-ethyl-4-oxo-4,5,6,7-tetrahydroindole with morpholine and formaldehyde to give molindone (I), and d) optionally converting molindone (I) to its salt. The present invention further provides process for preparation of compound comprising: a) reacting compound with ethyl halide and another halide source to form compound wherein R is alkyl and X is Cl, Br or I; b) converting compound to compound.
    Type: Grant
    Filed: February 14, 2020
    Date of Patent: August 25, 2020
    Assignee: LUPIN LIMITED
    Inventors: Amit Madanrao Agarkar, Tejas Vilas Puranik, Rajesh Bharat Gapat, Umesh Babanrao Rananaware, Radhakrishna Bhikaji Shivdavkar, Girij Pal Singh
  • Patent number: 9810962
    Abstract: Comparing to conventional electrochromic material showing a primary drawback of high manufacturing cost due to low synthetic yield, the inventors of the present invention modulate the chemical structure of a traditional viologen compounds so as to develop a novel electrochromic material performing an excellent advantage of low manufacturing cost resulted from high recovery rate. Moreover, differing from conventional electrochromic devices (ECD) installed with the conventional electrochromic material, the inventors of the present invention also propose an anti-dazzle mirror having the novel electrochromic material, wherein the proposed anti-dazzle mirror shows an outstanding reflectivity performance.
    Type: Grant
    Filed: August 24, 2016
    Date of Patent: November 7, 2017
    Assignee: E-CHEM ENTERPRISE CORP.
    Inventor: Tzun-Wu Wang
  • Patent number: 9802893
    Abstract: The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.
    Type: Grant
    Filed: November 30, 2016
    Date of Patent: October 31, 2017
    Assignee: Supernus Pharmaceuticals, Inc.
    Inventors: Martin Hanbauer, Zarghun Nazir, Peter Hildebrand, Attilia Figini, Likan Liang, Tiziano Fumagalli
  • Patent number: 9562011
    Abstract: The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.
    Type: Grant
    Filed: January 29, 2015
    Date of Patent: February 7, 2017
    Assignee: Supernus Pharmaceuticals, Inc.
    Inventors: Martin Hanbauer, Zarghun Nazir, Peter Hildebrand, Attilia Figini, Likan Liang, Tiziano Fumagalli
  • Patent number: 9362508
    Abstract: The present invention relates to oligomers of the formula (I), and their use as organic semiconductor in organic devices, especially in organic photovoltaics (solar cells) and photodiodes, or in a device containing a diode and/or an organic field effect transistor. High efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when the oligomers according to the invention are used in organic field effect transistors, organic photovoltaics (solar cells) and photodiodes.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: June 7, 2016
    Assignee: BASF SE
    Inventors: Pascal Hayoz, Natalia Chebotareva
  • Publication number: 20150141645
    Abstract: The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 21, 2015
    Inventors: Martin HANBAUER, Zarghun NAZIR, Peter HILDEBRAND, Attilia FIGINI, Likan LIANG, Tiziano FUMAGALLI
  • Publication number: 20150119394
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 30, 2015
    Inventors: Abhijit Roychowdhury, Rajiv Sharma, Malcolm Mascarenhas, Chandrika B-Rao, Shashikant M. Patil, Sambhaji Chavan, Nitin Lad, Smriti Khanna, Christopher J. Dinsmore
  • Publication number: 20150111890
    Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof,that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: April 19, 2013
    Publication date: April 23, 2015
    Inventors: Lisa A. Hasvold, Dachun Liu, Chang Hoon Park, John K. Pratt, George S. Sheppard, Le Wang
  • Publication number: 20150099746
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 9, 2015
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
  • Publication number: 20150087617
    Abstract: The invention provides indole and indoline derivatives and slats thereof, compositions comprising them and uses thereof for the treatment of diseases and disorders.
    Type: Application
    Filed: April 2, 2013
    Publication date: March 26, 2015
    Inventors: Abraham Nudelman, Marta Weinstock-Rosin
  • Publication number: 20150057278
    Abstract: Amido compounds are disclosed that have a formula represented by the following: and wherein Cy1, Cy2, n1, n2, R1a, R1b, R2, R3, R4, R5, and R6 are as described herein. 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, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.
    Type: Application
    Filed: September 10, 2012
    Publication date: February 26, 2015
    Inventors: Dan Littman, Jun R. Huh, Ruili Huang, Wenwei Huang, Erika E. Englund
  • Patent number: 8957206
    Abstract: The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: February 17, 2015
    Assignee: Supernus Pharmaceuticals Inc.
    Inventors: Martin Hanbauer, Zarghun Nazir, Peter Hildebrand, Attilia Figini, Likan Liang, Tiziano Fumagalli
  • Publication number: 20150045362
    Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.
    Type: Application
    Filed: August 25, 2014
    Publication date: February 12, 2015
    Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford
  • Patent number: 8940784
    Abstract: This invention relates to novel analogs of the DNA-binding alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and their conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: January 27, 2015
    Assignee: Syntarga B.V.
    Inventors: Patrick Henry Beusker, Franciscus Marinus Hendrikus de Groot, Lutz F. Tietze, Felix Major, Johannes Albertus Frederikus Joosten, Henri Johannes Spijker
  • Publication number: 20150018310
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: September 29, 2014
    Publication date: January 15, 2015
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone, Julie Wurster
  • Publication number: 20150005494
    Abstract: Methods for the synthesis of an indole in provided. Methods comprise oxidizing a N-aryl imine in the presence of a palladium-based catalyst, an oxidant, and a solvent.
    Type: Application
    Filed: December 19, 2012
    Publication date: January 1, 2015
    Inventors: Naohiko Yoshikai, Ye Wei
  • Publication number: 20140343037
    Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Inventors: Kenneth He Huang, Jeron Eaves, Gunnar Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
  • Patent number: 8877923
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: November 4, 2014
    Assignee: Allergan, Inc.
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
  • Publication number: 20140275076
    Abstract: Disclosed is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, R1 is optionally substituted heteroaryl etc.; R2 is hydrogen etc.; R3 and R4 are each independently hydrogen etc., R5 is the following group: (wherein Y is optionally substituted five membered heteroaryl etc., R9a is optionally substituted aryl etc., R9b and R9c are each dependently hydrogen etc., and m is the integral 0 etc.) etc.; R6 is hydrogen etc.; and R7 is hydrogen etc.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Katsunori Tsuboi, Yosuke Takanashi, Shingo Tojo, Tomohiro Kodama, Katsumi Kubota, Toshio Kanai
  • Publication number: 20140275075
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.
    Type: Application
    Filed: March 13, 2013
    Publication date: September 18, 2014
    Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Craig C. BEESON, Christopher C. LINDSEY, Yuri K. PETERSON, Baerbel ROHRER
  • Publication number: 20140275033
    Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Chiang Jia Li, Ji-Feng Liu, Wei Li, Amanda Gibeau, Harry Rogoff
  • Patent number: 8796244
    Abstract: The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: June 12, 2009
    Date of Patent: August 5, 2014
    Assignee: Astex Therapeutics Ltd
    Inventors: Valerio Berdini, Maria Grazia Carr, Miles Stuart Congreve, Martyn Frederickson, Charlotte Mary Griffiths-Jones, Christopher Charles Frederick Hamlett, Andrew Madin, Christopher William Murray, Rajdeep Kaur Benning, Gordon Saxty, Emma Vickerstaffe, Andrew James Woodhead, Steven John Woodhead, Eddy Jean Edgard Freyne, Tom Cornelis Hortense Govaerts, Patrick René Angibaud, Marian Williams
  • Publication number: 20140171363
    Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Gregory Raymond BEBERNITZ, Kevin CLAIRMONT, Scott Louis COHEN, Robert Edson DAMON, II, Robert Francis DAY, Stephanie Kay DODD, Christoph GAUL, Hatice Belgin GULGEZE EFTHYMIOU, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Kai LIN, Justin Yik Ching MAO, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, SU Liansheng
  • Patent number: 8691815
    Abstract: The invention relates to novel oxindol derivative of general formula (I), wherein substituents R1, R2, A, B and Y are such as defined in a claim 1. Drugs containing said derivatives and the use thereof for preventing and/or treating vassopress-and/or oxytocin-dependent-diseases are also disclosed.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: April 8, 2014
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Lubisch, Wilfried Hornberger, Liliane Unger, Andrea Hager-Wernet
  • Publication number: 20140081020
    Abstract: The present invention is directed towards novel methods of synthesis of molindone, synthesis of the intermediates of molindone, and high-purity compositions of molindone. In particular, the invention relates to the methods of synthesis of molindone through the Mannich reaction.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 20, 2014
    Inventors: Martin Hanbauer, Zarghun Nazir, Peter Hildebrand, Attilia Figini, Likan Liang, Tiziano Fumagalli
  • Publication number: 20140045832
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Application
    Filed: April 19, 2012
    Publication date: February 13, 2014
    Applicants: PIRAMAL ENTERPRISES LIMITED, MERCK SHARP & DOHME CORP.
    Inventors: Sarala Balachandran, Christopher J. Dinsmore, Abhijit Roychowdhury, Rajiv Sharma, Ram Asrey Vishwakarma
  • Publication number: 20140039100
    Abstract: The instant invention pertains to novel bi- or tricyclic sterically hindered alkoxyamines, their precursors, a process for their preparation and their use as light stabilizers for polymers or coatings, as flame retardants, as peroxide substitutes (rheology modifiers) or carbon radical scavengers.
    Type: Application
    Filed: October 4, 2013
    Publication date: February 6, 2014
    Applicant: BASF SE
    Inventors: Stefan Hauck, Walter Fischer, Kai-Uwe Schoening
  • Patent number: 8637681
    Abstract: Provided are pyrrolyl substituted dihydroindol-2-one derivatives represented by formula (I), pharmaceutically acceptable salts or solvates of said derivatives, or solvates of said salts, which are effective tyrosine kinase inhibitors. Also provided are the preparation methods of the above compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in manufacturing drugs useful for the treatment or adjunctive treatment of tumors medicated by tyrosine kinases or proliferation or migration of tumor cells driven by tyrosine kinases in mammals (including human).
    Type: Grant
    Filed: March 31, 2011
    Date of Patent: January 28, 2014
    Assignee: Qilu Pharmaceutical Co., Ltd.
    Inventors: Jingyi Wang, Chuanwen Fan, Long Zhang, Boyan Xu, Shousheng Yan, Zongru Guo, Minghui Zhang, Dong Lin, Zhantao Zhang, Haojie Zhou
  • Publication number: 20130317024
    Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
    Type: Application
    Filed: May 22, 2013
    Publication date: November 28, 2013
    Applicant: NOVARTIS AG
    Inventors: Simona Cotesta, Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Publication number: 20130281450
    Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula I.
    Type: Application
    Filed: March 12, 2013
    Publication date: October 24, 2013
    Inventors: John K. Pratt, Dachun Liu, Chang H. Park, George S. Sheppard, Lisa A. Hasvold, Le Wang
  • Publication number: 20130281451
    Abstract: A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.
    Type: Application
    Filed: April 3, 2013
    Publication date: October 24, 2013
    Applicant: ANNJI PHARMACEUTICAL CO., LTD.
    Inventors: Ji-Wang Chern, Ajit Dhananjay Jagtap, Hsiao-Chun Wang, Grace Shiahuy Chen
  • Publication number: 20130263390
    Abstract: The invention relates to 4-aminoindole derivatives of formula (I), and the addition salts thereof, mesomers thereof, isomers thereof and solvates thereof: and to their use for the oxidation dyeing of keratin fibres, and in particular of human keratin fibres such as the hair. The present invention makes it possible to achieve dark shades, natural shades and dark natural shades. The present invention also makes it possible to obtain powerful, chromatic, aesthetic, sparingly selective coloration of keratin fibres in varied shades, which is resistant to the various attacking factors to which the hair may be subjected. In particular, when the 4-aminoindole derivatives are combined with one or more heterocyclic oxidation bases, they make it possible to obtain a wide range of colours and coloration of keratin fibres that shows good chromaticity and good selectivity.
    Type: Application
    Filed: December 14, 2011
    Publication date: October 10, 2013
    Applicant: L'OREAL
    Inventors: Aziz Fadli, Fatima Makhlouf
  • Publication number: 20130259830
    Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.
    Type: Application
    Filed: June 24, 2011
    Publication date: October 3, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Timothy Barden, Colleen Hudson, James Jia, Charles Kim, Regina Graul, Ara Mermerian, Joel Moore, Kevin Sprott, Yueh-tyng Chien
  • Patent number: 8530469
    Abstract: The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I inhibitors; antimetabolites; tubulin targeting agents; DNA binder and topoisomerase II inhibitors; alkylating agents; monoclonal antibodies; anti-hormones; signal transduction inhibitors; proteasome inhibitors; DNA methyl transferases; cytokines; retinoids and HDAC or HAT modulators.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: September 10, 2013
    Assignee: Astex Therapeutics Ltd.
    Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford, Maria Grazia Carr, Robert Downham, Michael Alistair O'Brien, Theresa Rachel Phillips, Andrew James Woodhead
  • Patent number: 8524709
    Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.
    Type: Grant
    Filed: January 12, 2012
    Date of Patent: September 3, 2013
    Assignee: Tyrogenex, Inc.
    Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
  • Publication number: 20130217679
    Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
    Type: Application
    Filed: March 23, 2011
    Publication date: August 22, 2013
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, THE JOHNS HOPKINS UNIVERSITY
    Inventors: Donald J. Zack, Thomas Bannister, Tomas Vojkovsky, Zhiyong Yang, Cynthia Berlinicke
  • Publication number: 20130217650
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: November 15, 2012
    Publication date: August 22, 2013
    Applicant: Allergan, Inc.
    Inventor: Allergan, Inc.
  • Publication number: 20130158030
    Abstract: Provided are pyrrolyl substituted dihydroindol-2-one derivatives represented by formula (I), pharmaceutically acceptable salts or solvates of said derivatives, or solvates of said salts, which are effective tyrosine kinase inhibitors. Also provided are the preparation methods of the above compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in manufacturing drugs useful for the treatment or adjunctive treatment of tumors medicated by tyrosine kinases or proliferation or migration of tumor cells driven by tyrosine kinases in mammals (including human).
    Type: Application
    Filed: March 31, 2011
    Publication date: June 20, 2013
    Applicant: QILU PHARMACEUTICAL CO., LTD
    Inventors: Jingyi Wang, Chuanwen Fan, Long Zhang, Boyan Xu, Shousheng Yan, Zongru Guo, Minghui Zhang, Dong Lin, Zhantao Zhang, Haojie Zhou
  • Publication number: 20130137686
    Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
    Type: Application
    Filed: November 5, 2012
    Publication date: May 30, 2013
    Inventor: Esanex, Inc.
  • Publication number: 20130123259
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Application
    Filed: December 20, 2012
    Publication date: May 16, 2013
    Applicant: Allergan, Inc.
    Inventor: Allergan, Inc.
  • Patent number: 8415486
    Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: April 9, 2013
    Assignee: TetraLogic Pharmaceuticals Corp.
    Inventors: Stephen M. Condon, Yijun Deng, Matthew D. Alexander, Matthew G. Laporte
  • Patent number: 8367664
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: January 23, 2007
    Date of Patent: February 5, 2013
    Assignee: Allergan, Inc.
    Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone
  • Publication number: 20130029970
    Abstract: The present disclosure relates to compounds of formula I useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: July 9, 2010
    Publication date: January 31, 2013
    Applicant: IRONWOOD PHARMACEUTICALS, INC
    Inventors: Kevin Sprott, Jason Rohde, Takashi Nakai, Bo Peng, John Jeffrey Talley
  • Publication number: 20130030173
    Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
    Type: Application
    Filed: September 13, 2012
    Publication date: January 31, 2013
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Ke Ding, Guoping Wang
  • Publication number: 20130012705
    Abstract: Disclosed are new dicycloazaalkane derivates represented by general formula (I), preparation processes and pharmaceutical compositions containing them, and the uses for treatment especially for dipeptidyl peptidase inhibitor (DPP-IV), in which each substitute group of general formula (I) is as defined in specification.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Applicant: Jiangsu Hansoh Pharmaceutical Co., Ltd.
    Inventors: Peng Cho Tang, Zhigang Lin, Hejun Lü, Fuqiang Zhao, Li Li, Fanglong Yang, Jianghong Fu, Lin Wang, Guangyuan Shen, Dongliang Guan
  • Patent number: 8344018
    Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
    Type: Grant
    Filed: July 14, 2009
    Date of Patent: January 1, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Chandrasekar Venkataramani
  • Patent number: 8338590
    Abstract: The present invention relates to novel oxindole derivatives of the general formula (I), wherein the substitutes A, B, R1, R2 and R3 are as defined in Claim 1, and medicaments containing the same for the prophylaxis and/or treatment of vasopressin-dependent or oxytocin-dependent diseases.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: December 25, 2012
    Assignee: Abbott GmbH & Co. KG
    Inventors: Wilfried Lubisch, Thorsten Oost, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Hervé Geneste, Andrea Hager-Wernet, legal representative
  • Publication number: 20120322800
    Abstract: Disclosed herein are small molecule heterocyclic inhibitors of sepiapterin reductase (SPR), and prodrugs and pharmaceutically acceptable salts thereof. The Also featured are pharmaceutical compositions of the compounds and uses of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, and neuropathic pain).
    Type: Application
    Filed: October 14, 2010
    Publication date: December 20, 2012
    Inventor: Julian Blagg
  • Publication number: 20120309759
    Abstract: The present invention embraces methods for identifying compounds that modulate the activity of telomerase. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the TRBD, “thumb,” “finger,” and/or “palm” domain; or FP-pocket, PT-pocket or Th-pocket of telomerase and testing the compound for its ability to modulate the activity of telomerase. Compounds selected for interacting with the T-pocket or Fingers-Palm pocket of telomerase are also provided.
    Type: Application
    Filed: February 8, 2011
    Publication date: December 6, 2012
    Applicant: The Wistar Institute
    Inventor: Emmanuel Skordalakes
  • Patent number: 8309547
    Abstract: Provided are process for the preparation of (R)- and/or (S)-Rivaroxaban, and compounds which are intermediate compounds used in the processes for the preparation of (R)- and/or (S)-Rivaroxaban.
    Type: Grant
    Filed: October 18, 2010
    Date of Patent: November 13, 2012
    Assignee: Apotex Pharmachem Inc.
    Inventors: Prabhudas Bodhuri, Gamini Weeratunga