Chalcogen Or Additional Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 548/196)
  • Patent number: 10647680
    Abstract: Provided are a urea compound represented by general formula (I), a pharmaceutically acceptable salt thereof, a preparation method therefor, and use thereof as an FLT3 tyrosine protein kinase inhibitor, particularly in the prevention and/or treating of cancer.
    Type: Grant
    Filed: March 10, 2017
    Date of Patent: May 12, 2020
    Assignee: Ancureall Pharmaceutical (Shanghai) Co., Ltd.
    Inventors: Jutong Si, Meifeng Jiang
  • Publication number: 20150111868
    Abstract: The present invention is concerned with novel 1,3-dihydro-2H-benzimidazol-2-one derivatives substituted with heterocycles having formula (I) stereoisomeric forms thereof, and the pharmaceutically acceptable addition salts, and the solvates thereof, wherein R4, R5, Z and Het have the meaning defined in the claims. The compounds according to the present invention are useful as inhibitors on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.
    Type: Application
    Filed: June 14, 2013
    Publication date: April 23, 2015
    Applicant: Jansen R&D Ireland
    Inventors: Abdellah Tahri, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Sandrine Marie Helene Vendeville, Lili Hu, Samuel Dominique Demin, Ludwig Paul Cooymans
  • Patent number: 8993567
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: March 31, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
  • Publication number: 20150038523
    Abstract: The invention relates to compounds of formula (I): wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-integrin antagonists to target cells expressing alpha-V-beta-3.
    Type: Application
    Filed: January 22, 2013
    Publication date: February 5, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Robert Alan Goodnow, Jr., Matthew Michael Hamilton, Agnieszka Kowalczyk, Achyutharao Sidduri
  • Patent number: 8940771
    Abstract: The present invention relates to compounds of formula I and its salts, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: January 27, 2015
    Assignee: Novartis AG
    Inventors: Giorgio Caravatti, Robin Alec Fairhurst, Pascal Furet, Vito Guagnano, Patricia Imbach
  • Publication number: 20140348947
    Abstract: This document discloses molecules having the following formula (“Formula I”):
    Type: Application
    Filed: August 8, 2014
    Publication date: November 27, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. H. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl DeAmicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra Lee McLeod, Ronald Ross, JR., Yuanming Zhu, Peter Lee Johnson, Joseph D. Eckelbarger, Marshall H. Parker
  • Publication number: 20140274688
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Lindsey G. Fischer, Erich W. Baum, Gary D. Crouse, Carl DeAmicis, Beth Lorsbach, Jeff Petkus, Thomas C. Sparks, Gregory T. Whiteker
  • Publication number: 20140275047
    Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Lindsey G. Fischer, Erich W. Baum, Gary D. Crouse, Jeff Petkus, Andrew L. Ward, Thomas C. Sparks
  • Publication number: 20140275189
    Abstract: The present invention relates to compounds and methods for the treatment of bacterial infections. The compounds and methods involve the disruption of the QseC signaling pathway which modulates the virulence of some bacteria. This methodology for treatment of bacterial infections reduces evolutionary pressure to develop resistance because the bacteria are not killed in the process.
    Type: Application
    Filed: March 10, 2014
    Publication date: September 18, 2014
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Vanessa Sperandio, John R. Falck
  • Publication number: 20140206691
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 24, 2014
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M.P. Doweyko, Joel C. Barrish, John Wityak
  • Patent number: 8716320
    Abstract: The present invention provides novel heterocyclic urea compounds having useful antibacterial activity, pharmaceutical compositions comprising one or more of these compounds, methods of making the same, and methods of using the same.
    Type: Grant
    Filed: July 23, 2007
    Date of Patent: May 6, 2014
    Assignee: Replidyne, Inc.
    Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun
  • Patent number: 8703961
    Abstract: Compounds of the formula Ia and Ib, in which R1, R1?, R2, R3, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: April 22, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Hannes Koolman
  • Patent number: 8674111
    Abstract: The invention relates to oxazole and thiazole derivatives of formula (I), wherein A, E, X, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Grant
    Filed: June 11, 2010
    Date of Patent: March 18, 2014
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Patent number: 8642576
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: February 4, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Publication number: 20130338162
    Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: July 29, 2013
    Publication date: December 19, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Lijun Sun, Keizo Koya, Shoujun Chen, Zachary Demko, Zhi-Qiang Xia
  • Patent number: 8586614
    Abstract: The invention provides a compound of general formula (I) wherein the substituents are defined further in the application, as well as further embodiments hereof described in the attached embodiments. The present invention also provides use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes.
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: November 19, 2013
    Assignee: Novo Nordisk A/S
    Inventors: Jesper Lau, Anthony Murray, Per Vedso, Marit Kristiansen, Lone Jeppesen
  • Publication number: 20130281708
    Abstract: A process for the production of fluorinated compound represented by the formula (I): or salts thereof wherein R1 and R2 are the same or different and each is selected from the group consisting of a hydrogen atom, a carbonyl group, a sulfonyl group and a phosphoryl group.
    Type: Application
    Filed: March 4, 2011
    Publication date: October 24, 2013
    Applicant: TAKEDA CALIFORNIA, INC.
    Inventor: Matthew Neil Mattson
  • Publication number: 20130252984
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: March 12, 2013
    Publication date: September 26, 2013
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing YUAN, Richard L. BEARD, Xiaoxia LIU, John E. DONELLO, Veena VISWANATH, Michael E. GARST
  • Publication number: 20130217706
    Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pulmonary arterial hypertension (PAH); idiopathic PAH; familial PAH; PAH associated with a collagen vascular disease; and other diseases.
    Type: Application
    Filed: September 13, 2012
    Publication date: August 22, 2013
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Yoúng-Jun Shin, Pureza Vallar, Ning Zou
  • Publication number: 20130165460
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: February 20, 2013
    Publication date: June 27, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130143910
    Abstract: A method and composition for treating cancer cells that targets fructose-1,6-biphosphataseenzymes (FBPs, type 1 and type 2) and/or their respective pathways. In one embodiment, inhibitors of FBPs or FBPs pathways are administered to a patient to treat brain cancer metastasis. In another embodiment, the present invention is particularly well suited for treating cancer cells that generally survive under glucose-independent conditions, or any other condition where cancer cells produce glucose via FBPs mediated pathways.
    Type: Application
    Filed: November 14, 2012
    Publication date: June 6, 2013
    Inventor: Zhang Weihua
  • Publication number: 20130102462
    Abstract: The present invention relates to a process for producing aromatic carbonyl compounds of formula I and aromatic imine compounds of formula III comprising the step of reacting a (hetero)aromatic halogen or sulfonate compound II wherein the variables are as defined in the claims and description, with a mixture of carbon monoxide and hydrogen in the presence of a transition metal complex catalyst. The invention also relates to specific compounds III, to compositions comprising them and to their use for combating invertebrate pests.
    Type: Application
    Filed: June 22, 2011
    Publication date: April 25, 2013
    Applicant: BASF SE
    Inventors: Karsten Koerber, Florian Kaiser, Christian Rein, Joachim Schmidt-Leithoff, Wolfgang Von Deyn, Prashant Deshmukh, Arun Narine, Joachim Dickhaut, Nina Gertrud Bandur, Juergen Langewald
  • Publication number: 20130089622
    Abstract: This document discloses molecules having the following formula (“Formula I”):
    Type: Application
    Filed: November 14, 2012
    Publication date: April 11, 2013
    Applicant: Dow AgroSciences LLC
    Inventor: Dow AgroSciences LLC
  • Patent number: 8362267
    Abstract: Disclosed are a novel thiazole-containing benzophenone derivative represented by formula 1, and an isomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof and a solvate thereof, a pharmaceutical composition comprising the derivative, a use of the derivative as therapeutic agent and a method for preparing the derivative. The benzophenone thiazole derivatives inhibit formation of microtubules and eliminate actively proliferating cells of malignant tumors to control general cell proliferation. In formula 1, R, R1 and R2 are defined as above.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: January 29, 2013
    Assignee: Chong Kun Dang Pharmaceutical Corp.
    Inventors: Nam-Song Choi, Young-Hoon Kim, Jae-Kwang Lee, Hee-Ryong Kang, Ho-Jin Choi, Seung-Kee Moon, Soo-Jin Kim, Gyu-Tae Park, Byeong-Hoon Han, Dal-Hyun Kim, Jae-Hoon Choi, Sung-Sook Lee, Soon-Kil Ahn, Kyung-Joo Lee, Su-Yeal Bae
  • Publication number: 20130023463
    Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Application
    Filed: April 19, 2012
    Publication date: January 24, 2013
    Applicant: ABBOTT LABORATORIES
    Inventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
  • Publication number: 20130019348
    Abstract: This document discloses molecules having the following formula (“Formula One”) The molecules disclosed in this document are related to the field of processes to produce molecules that are useful as pesticides (e.g., acaricides, insecticides, molluscicides, and nematicides), such molecules, and processes of using such molecules to control pests.
    Type: Application
    Filed: July 11, 2012
    Publication date: January 17, 2013
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Gary D. Crouse, David A. Demeter, Thomas C. Sparks, Nick X. Wang, William H. Dent, III, Carl Deamicis, Noormohamed M. Niyaz, Erich W. Baum, Lindsey G. Fischer, Natalie C. Giampietro
  • Publication number: 20120322761
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Application
    Filed: August 29, 2012
    Publication date: December 20, 2012
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Patent number: 8304403
    Abstract: Compounds of formula Ia and Ib and wherein A, B, C and R1 are described herein.
    Type: Grant
    Filed: June 10, 2010
    Date of Patent: November 6, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Patent number: 8299102
    Abstract: The present invention relates to heteroarylcyclopropanecarboxamides of the formula I, in which Het, X, Ra, Rb, Rc, Rd, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.
    Type: Grant
    Filed: June 17, 2009
    Date of Patent: October 30, 2012
    Assignee: Sanofi
    Inventors: Hartmut Strobel, Paulus Wohlfart, Gerhard Zoller, David William Will
  • Patent number: 8293919
    Abstract: The present invention provides novel sulfone and sulfoxide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and methods of production are provided.
    Type: Grant
    Filed: July 23, 2008
    Date of Patent: October 23, 2012
    Assignee: Crestone, Inc.
    Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
  • Patent number: 8293753
    Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameliorated by inhibition of phosphatidylinositol 3-kinase.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: October 23, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Pascal Furet, Marc Gerspacher, Robert Mah
  • Publication number: 20120252759
    Abstract: Compounds of the formula Ia and Ib, in which R1, R1?, R2, R3, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: November 9, 2010
    Publication date: October 4, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKER HAFTING
    Inventors: Timo Heinrich, Hannes Koolman
  • Patent number: 8252782
    Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of formula (I).
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: August 28, 2012
    Assignee: Pfizer Inc.
    Inventors: Steven Joseph Brickner, Mark Edward Flanagan, Manjinder Singh Lall
  • Publication number: 20120214808
    Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 23, 2012
    Applicant: Prosidion Limited
    Inventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Simon Andrew Swain, Philippe Wong-Kai-In
  • Patent number: 8227605
    Abstract: The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: July 24, 2012
    Assignee: Schering Corporation
    Inventors: Gerald W. Shipps, Jr., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards
  • Publication number: 20120178780
    Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
    Type: Application
    Filed: March 19, 2012
    Publication date: July 12, 2012
    Inventors: Jill E. WOOD, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
  • Patent number: 8211926
    Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
    Type: Grant
    Filed: June 16, 2010
    Date of Patent: July 3, 2012
    Assignee: Cara Therapeutics, Inc.
    Inventor: Robert Zhiyong Luo
  • Publication number: 20120157487
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: December 9, 2011
    Publication date: June 21, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 8148380
    Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.
    Type: Grant
    Filed: July 23, 2008
    Date of Patent: April 3, 2012
    Assignee: Crestone, Inc.
    Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
  • Patent number: 8129541
    Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: March 6, 2012
    Assignee: Novartis AG
    Inventors: Ian Bruce, Peter Finan, Catherine LeBlanc, Clive McCarthy, Lewis Whitehead, Nicola Press, Graham Charles Bloomfield, Judy Hayler, Louise Kirman, Mrinalini Sachin Oza, Lena Shukla
  • Publication number: 20120015941
    Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.
    Type: Application
    Filed: July 23, 2008
    Publication date: January 19, 2012
    Applicant: CRESTONE, INC.
    Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
  • Publication number: 20120014906
    Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Application
    Filed: September 21, 2011
    Publication date: January 19, 2012
    Applicants: XENON PHARMACEUTICALS INC., NOVARTIS AG
    Inventors: Sultan Chowdhury, Natalie Dales, Julia Fonarev, Jianmin Fu, Duanjie Hou, Qi Jia, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Shaoyi Sun, Zaihui Zhang
  • Publication number: 20120015990
    Abstract: Provided herein are small molecule inhibitors of Taspase1 and methods of using the small molecule inhibitors of Taspase1 to treat neoplasm in subjects in need thereof.
    Type: Application
    Filed: June 17, 2011
    Publication date: January 19, 2012
    Applicant: THE WASHINGTON UNIVERSITY
    Inventors: James Hsieh, Emily Cheng
  • Patent number: 8063081
    Abstract: This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: November 22, 2011
    Assignee: Novo Nordisk A/S
    Inventors: Dharma Rao Polisetti, Janos Tibor Kodra, Jesper Lau, Paw Bloch, Maria Carmen Valcarce Lopez, Niels Blume, Mustafa Guzel, Kalpathy Chidambareswaran Santhosh, Adnan M. M. Mjalli, Robert Carl Andrews, Govindan Subramanian, Michael Ankersen, Per Vedso, Anthony Murray, Lone Jeppesen
  • Patent number: 8049016
    Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: November 1, 2011
    Assignees: Novartis AG, Xenon Pharmaceuticals Inc
    Inventors: Sultan Chowdhury, Natalie Dales, Julia Fonarev, Jianmin Fu, Duanjie Hou, Qi Jia, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Shaoyi Sun, Zaihui Zhang
  • Patent number: 7998990
    Abstract: The present invention concerns a compound of formula Ia wherein: Ra* is hydrogen or C1-C4-alkyl; Rb* is —(C1-C4-alkylene)-Y—C1-C4-haloalkyl or —(C1-C4-alkylene)-Y—C1-C4-hydroxyalkyl; Y represents —CONH— or a five membered heteroaryl group.
    Type: Grant
    Filed: May 21, 2007
    Date of Patent: August 16, 2011
    Assignee: Novartis AG
    Inventors: Emma Budd, Judy Fox Hayler, Ian Bruce, Darren Mark Legrand, Brian Cox
  • Patent number: 7999114
    Abstract: This invention relates to dicycloalkylcarbamoyl ureas of formula (I), which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
    Type: Grant
    Filed: July 7, 2006
    Date of Patent: August 16, 2011
    Assignee: Novo Nordisk A/S
    Inventors: Anthony Murray, Jesper Lau, Per Vedso, Lone Jeppesen, Marit Kristiansen
  • Patent number: 7973051
    Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: November 10, 2008
    Date of Patent: July 5, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Paul Hebeisen, Eric A. Kitas, Rudolf E. Minder, Peter Mohr, Hans Peter Wessel
  • Publication number: 20110124624
    Abstract: Compounds of Formula I: in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Application
    Filed: February 3, 2011
    Publication date: May 26, 2011
    Inventors: Graham Charles Bloomfield, Ian Bruce, Judy Fox Hayler, Catherine LeBlanc, Darren Mark Le Grand, Clive McCarthy
  • Publication number: 20110077251
    Abstract: The invention relates to 17? lupane derivatives of formula (I): wherein R1 and X are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infection by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.
    Type: Application
    Filed: August 16, 2010
    Publication date: March 31, 2011
    Inventors: Christophe Moinet, Bingcan Liu, Liliane Halab, Nathalie Turcotte, Real Denis, Carl Poisson, Paul Nguyen-Ba, Monica Bubenik, Laval Chan Chun Kong