Additional Nitrogen Containing Hetero Ring (e.g., Thiazetidine, Etc.) Patents (Class 544/111)
  • Patent number: 10457654
    Abstract: The invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein the variables X, Y1—Y5, R1, R2, R3, R4, and Het have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: October 31, 2017
    Date of Patent: October 29, 2019
    Assignees: GENENTECH, INC., XENON PHARMACEUTICALS INC.
    Inventors: Daniel Sutherlin, Steven McKerrall, Michael Scott Wilson, Kwong Wah Lai, Philippe Bergeron, Birong Zhang, Ramsay Beveridge, Jean-Philippe Leclerc, Alexandre Lemire, Liang Zhao, Claudio Sturino
  • Patent number: 10329285
    Abstract: Crystals of a quinazoline derivative are provided. The present invention relates to an acid addition salt of a compound represented by Formula (I): a pharmaceutical composition containing it, and the like.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: June 25, 2019
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Yukio Tada, Yuusuke Tamura, Shuji Yonezawa, Kenichi Ishibashi
  • Patent number: 10287291
    Abstract: seco-Cyclopropapyrroloindole compounds of formula (I) where Hal, R1, R2, and R3 are as defined in the application, are potent anti-cancer agents that can be used in antibody-drug conjugates.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: May 14, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Fukang Yang, Qian Zhang, Lawrence B. Snyder, Sanjeev Gangwar, Dale L. Boger
  • Patent number: 9815835
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: August 31, 2016
    Date of Patent: November 14, 2017
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Patent number: 9040528
    Abstract: The present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
    Type: Grant
    Filed: January 13, 2014
    Date of Patent: May 26, 2015
    Assignee: AstraZeneca AB
    Inventors: Kevin Barvian, Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
  • Publication number: 20150141399
    Abstract: Disclosed are compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Application
    Filed: February 5, 2015
    Publication date: May 21, 2015
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Patent number: 9029370
    Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, X, Z, Ar, and n are as described in the claims, Ar is phenyl or heteroaryl, selected from the group consisting of 1H-indazole-3yl, pyridine-2-yl, pyridine-3-yl, pyridine-4-yl, pyrimidine-5-yl, 1H-pyrazole-3-yl, 1H-pyrazole-4-yl and 1H-pyrazole-5-yl; or to a pharmaceutically suitable acid addition salt thereof, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: May 12, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Roger Norcross, Philippe Pflieger
  • Patent number: 8952006
    Abstract: Morpholinoalkyl fumarates, pharmaceutical compositions comprising the morpholinoalkyl fumarates, and methods of using morpholinoalkyl fumarates and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: February 10, 2015
    Assignee: XenoPort, Inc.
    Inventors: Kenneth C. Cundy, Suresh K. Manthati, David J. Wustrow
  • Publication number: 20150038481
    Abstract: Described are compounds of Formula I or Formula II: wherein: ring A is a 5- or 6-membered heteroaryl group; dashed lines are optional double bonds; X is N or O; Y is a carbon atom or an S or N heteroatom in ring A in any suitable location; and substituents are as given herein. Compositions containing the same and methods of using the same in treating cancers such as acute lymphoblastic leukemia are also described.
    Type: Application
    Filed: May 21, 2013
    Publication date: February 5, 2015
    Inventors: Xiaodong Wang, Weihe Zhang, Dmitri Kireev, Dehui Zhang, Andrew Mclver
  • Publication number: 20150031878
    Abstract: The invention provides derivatives of DEA which have increased potency and hydrolysis resistance as compared to DEA, and compositions thereof, as well as methods of using these derivatives to promote neurogenesis, neurite growth and/or length, and/or promote synaptogenesis.
    Type: Application
    Filed: March 15, 2013
    Publication date: January 29, 2015
    Inventors: Hee-Yong Kim, Juan Jose Marugan, Erika E. Englund, Samarjit Patnaik
  • Patent number: 8927710
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: January 6, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Publication number: 20140371198
    Abstract: Compounds are disclosed that have a formula represented by the following: These compounds may be prepared as a pharmaceutical composition, 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, infectious diseases, autoimmune diseases, diseases involving impairment of immune cell functions, cardiometabolic diseases, and/or proliferative diseases.
    Type: Application
    Filed: June 23, 2014
    Publication date: December 18, 2014
    Inventors: Laurent Raymond Maurice Sanière, Mathieu Rafaël Pizzonero, Nicolas Triballeau, Nick Ernest René Vandeghinste, Steve Irma Joel De Vos, Reginald Christophe Xavier Brys, Christelle Dominique Bénédict Pourbaix-L'ebraly
  • Patent number: 8877753
    Abstract: The invention relates to the use of a group of sigma receptor ligands of formula (I) for the potentiation of the analgesic effect of opioids and opiates and at the same time for decreasing the dependency induced by them.
    Type: Grant
    Filed: April 24, 2009
    Date of Patent: November 4, 2014
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Helmut Heinrich Buschmann, Jose Miguel Vela Hernandez, Daniel Zamanillo-Castanedo
  • Patent number: 8859765
    Abstract: The present invention provides efficient and economical methods for synthesis of (?)-2-exo-morpholinoisoborne-10-thiol, its enantiomer, and related chiral catalysts. Novel compounds and methods of asymmetric synthesis are also disclosed.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: October 14, 2014
    Assignee: ScinoPharm Taiwan, Ltd.
    Inventors: Ping-Yu Wu, Julian Paul Henschke
  • Publication number: 20140275527
    Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Application
    Filed: June 27, 2013
    Publication date: September 18, 2014
    Applicant: Exelixis, Inc.
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Patent number: 8815926
    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: Grant
    Filed: January 24, 2013
    Date of Patent: August 26, 2014
    Assignee: Novartis AG
    Inventors: Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Lv Liao, Robert Mah, Liang Mao, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
  • Patent number: 8796267
    Abstract: This invention relates to novel N-[[3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]-acetamide derivatives, their acceptable acid addition salts, solvates and hydrates. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antimicrobial agents.
    Type: Grant
    Filed: June 17, 2008
    Date of Patent: August 5, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Roger Tung, Scott Harbeson
  • Patent number: 8754211
    Abstract: The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein the variables are defined herein.
    Type: Grant
    Filed: September 30, 2013
    Date of Patent: June 17, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Pratik Devasthale, William N. Washburn, Kishore V. Renduchintala, Radhakrishnan Sridhar
  • Patent number: 8754209
    Abstract: Disclosed are novel indazole derivatives represented by the following Chemical Formula 1 or pharmaceutically acceptable salts, hydrates or solvates thereof, and pharmaceutical compositions for the prevention or treatment of proliferative diseases, containing the same as an active ingredient. Having potent inhibitory effect against protein kinase, such as b-raf, KDR, Fms, Tie2, SAPK2a and Ret, inducing diseases caused by abnormal cell proliferation, the novel indazole derivatives can be used for the prevention or treatment of diseases caused by abnormal cell proliferation.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: June 17, 2014
    Assignees: Korea Institute of Science and Technology, Korea Research Institute of Chemical Technology, Korea Research Institute of Bioscience and Biotechnology
    Inventors: Tae Bo Sim, Jung Beom Son, Hwan Kim, Dong Sik Park, Hwan Geun Choi, Young Jin Ham, Jung Mi Hah, Kyung Ho Yoo, Chang Hyun Oh, So Ha Lee, Jae Du Ha, Sung Yun Cho, Byoung Mog Kwon, Dong Cho Han
  • Publication number: 20140107336
    Abstract: The present invention relates to a novel class of tri-aryl compounds, compositions comprising the same and processes for the preparation thereof.
    Type: Application
    Filed: November 1, 2013
    Publication date: April 17, 2014
    Applicant: BEN-GURION UNIVERSITY OF THE NEGEV RESEARCH AND DEVELOPMENT AUTHORITY
    Inventors: Esther PRIEL, Aviv GAZIT, Shimon SLAVIN, Sara YITZCHAK
  • Patent number: 8685975
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: April 1, 2014
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Patent number: 8658641
    Abstract: The present invention relates to compounds of Formula (I); to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: February 25, 2014
    Assignee: AstraZeneca AB
    Inventors: Kevin Barvian, Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
  • Patent number: 8604245
    Abstract: The present invention relates to a novel class of tri-aryl compounds, compositions comprising the same and processes for the preparation thereof.
    Type: Grant
    Filed: June 3, 2008
    Date of Patent: December 10, 2013
    Assignee: Ben-Gurion University of the Negev Research and Development Authority
    Inventors: Esther Priel, Aviv Gazit, Shimon Slavin, Sara Yitzchak
  • Patent number: 8546375
    Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: October 1, 2013
    Assignee: AstraZeneca AB
    Inventors: Susanne Doris Margit Bökman-Winiwarter, Marlene Fredenwall, Carl Anders Hogner, Lars Anders Mikael Johansson, Robert Andrew Judkins, Lanna Li, Björn Christian Ingvar Löfberg, Sverker Von Unge
  • Patent number: 8545984
    Abstract: Described herein are compounds generally comprising an indeno[2?,3?:3,4]naptho[1,2-b]pyran structure. Such compounds may be useful for their photochromic properties, and be used in certain photochromic compositions. Such compositions may further comprise other photochromic compositions and/or materials. Additionally, such compounds and/or compositions may be suitable for preparing certain photochromic articles. Also described herein are methods for preparing certain photochromic compounds, compositions, and articles.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: October 1, 2013
    Assignee: Transitions Optical, Inc.
    Inventors: Meng He, Darrin R. Dabideen, Anil Kumar, Ruisong Xu
  • Publication number: 20130150574
    Abstract: The present invention provides efficient and economical methods for synthesis of (?)-2-exo-morpholinoisoborne-10-thiol, its enantiomer, and related chiral catalysts. Novel compounds and methods of asymmetric synthesis are also disclosed.
    Type: Application
    Filed: November 29, 2012
    Publication date: June 13, 2013
    Applicant: Scinopharm Taiwan, LTD.
    Inventor: Scinopharm Taiwan, LTD.
  • Patent number: 8445478
    Abstract: The invention relates to azetidine derivatives having the formula (I): Wherein R?, R1, R2, R3, R6, R7, R, Y, A and B are as defined herein. The invention also relates to a method for preparing the same and therapeutic use thereof.
    Type: Grant
    Filed: June 18, 2010
    Date of Patent: May 21, 2013
    Assignee: Sanofi
    Inventor: Jean-Francois Sabuco
  • Patent number: 8399497
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: November 23, 2010
    Date of Patent: March 19, 2013
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Patent number: 8367661
    Abstract: Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: February 5, 2013
    Assignee: Cytokinetics, Inc.
    Inventors: Bradley Paul Morgan, Fady Malik, Erica Anne Kraynack, Alexander Ramon Muci, Xiangping Qian, David J. Morgans, Jr.
  • Patent number: 8343970
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: January 1, 2013
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Patent number: 8338595
    Abstract: This invention relates to pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.
    Type: Grant
    Filed: July 20, 2009
    Date of Patent: December 25, 2012
    Assignee: Bayer HealthCare LLC
    Inventors: Julie A. Dixon, Catherine Brennan, Karl Miranda, Brent Chandler, Barton Phillips, Jianmei Fan, Michael Brands, Andrea McClure, Benjamin D. Jones, Wenlang Fu, Donald Bierer, Steven Magnuson, Harold C. E. Kluender
  • Patent number: 8299073
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof, which are inhibitors of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: October 30, 2012
    Assignee: Respivert Ltd.
    Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Simon Christopher Hirst, David Michel Adrien Taddei, Catherine Elisabeth Charron
  • Patent number: 8299074
    Abstract: The present disclosure relates to compounds of formula (I): which are inhibitors of p38 mitogen-activated protein kinase enzymes, particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: October 30, 2012
    Assignee: RespiVert Ltd.
    Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Kevin Joly, Catherine Elisabeth Charron
  • Publication number: 20120252743
    Abstract: The invention provides methods of making and using compounds of the formula: or a pharmaceutically acceptable salt thereof; wherein n is an integer between 1 and 2 inclusively; m is an integer between 0 and 2 inclusively; X is selected from the group consisting of CH or N; R1 is selected from the group consisting of —CH2NH2, and R2 is selected from the group consisting of —H, —OH, —NH2 and acetyl; R3 is selected from the group consisting of —H, benzyloxycarbonyl and benzylsulfonyl; and R4 is selected from the group consisting of —OH, wherein p is an integer between 0 and 2 inclusively, Y is selected from the group consisting of —O—, —S—, —S(?O)—, —SO2—, methylene, —CH(OH)—, —CH(NH2)—, —CH(CH2—OH)—, —CH(CH2—NH2)— or —N(R6)—, R5 is selected from the group consisting of —H or a simple (C1-C3) alkyl and R6 is selected from the group consisting of —H, a simple (C1-C3) alkyl or a simple (C1-C3) acyl.
    Type: Application
    Filed: December 21, 2011
    Publication date: October 4, 2012
    Applicant: The Medicines Company (Leipzig) GmbH
    Inventors: Peter Herold, Stjepan Jelakovic, Mohammed Daghish, Claudia Reichelt, Alexander Schulze, Andrea Schweinitz, Friedrich-Alexander Ludwig, Adel Rafai Far, Ting Kang
  • Patent number: 8273905
    Abstract: Compounds corresponding to formula I, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n have the meanings given in the description, and also a process for the preparation of these compounds and intermediate products of this process. Furthermore, pharmaceutical compositions comprising the compounds of Formula I and related methods of treatment.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: September 25, 2012
    Assignee: Abbott Products GmbH
    Inventors: Brian Moloney, Lester Marrison, Dieter Ziegler, Michael Mlinaric, Christiane Boecker, Reinhard Brueckner, Michael Weske, Klaus Witte, Yvan Fischer
  • Publication number: 20120220580
    Abstract: Compounds having the structure of general formula I or pharmaceutically acceptable salts thereof which are derivatives of fucoxanthin and fucoxanthol are disclosed. A preparation method of the compound and its use in weight reducing are also disclosed.
    Type: Application
    Filed: April 19, 2012
    Publication date: August 30, 2012
    Applicant: BEIJING GINGKO GROUP BIOLOGICAL TECHNOLOGY CO., LTD.
    Inventors: YANMEI LI, QINGHUA LIU
  • Patent number: 8247401
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: October 29, 2008
    Date of Patent: August 21, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Diem Nguyen, Zhengwu Deng, Daniel V. Paone, Craig M. Potteiger, Joseph P. Vacca
  • Patent number: 8232273
    Abstract: In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: July 31, 2012
    Assignees: Genentech, Inc., Abbott Laboratories, The Walter and Eliza Hall Institute of Medical Research
    Inventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Peter Czabotar, Danette A. Dudley, Wayne J. Fairbrother, John A. Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Lisa A. Hasvold, Andrew M. Petros, Andrew J. Souers, Zhi-Fu Tao, Le Wang, Xilu Wang, Kurt Deshayes
  • 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
  • Patent number: 8217037
    Abstract: Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.
    Type: Grant
    Filed: April 5, 2007
    Date of Patent: July 10, 2012
    Assignees: Board of Supervisors of Louisiana State University and Agricultural and Mechanical College, B.V. Patel Pharmaceutical Education & Research Development (PERD)
    Inventors: Anthony Giordano, Kamala K. Vasu, Hardik M. Thakar, Rajan S. Giri, Swapnil G. Yerande, Gajanan S. Inamdar, Vasudevan Sudarsanam
  • Publication number: 20120172345
    Abstract: This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof: wherein Z, HY, R1, R2, R3, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: August 11, 2011
    Publication date: July 5, 2012
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Brian S. Freeze, Masaaki Hirose, Yongbo Hu, Todd B. Sells, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • Patent number: 8188277
    Abstract: The present invention provides a novel compound, which has an excellent effect of suppressing the generation of collagen and less side effects, with being excellent in terms of safety. The compound of the present invention is represented by the following general formula (1): [wherein X1 represents a nitrogen atom or a group —CH?; R1 represents a group —Z—R6, wherein Z represents a group —CO—, a group —CH(OH)—, or the like, and R6 represents a 5- to 15-membered monocyclic, dicyclic, or tricyclic, saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms, or sulfur atoms; R2 represents a hydrogen atom, a halogen atom or a lower alkylene group; Y represents a group —O—, a group —CO—, a group —CH(OH)—, a lower alkylene group, or the like; and A represents a group or the like, wherein R3 represents a hydrogen atom, a lower alkoxy group, or the like, p represents 1 or 2, and R4 represents an imidazolyl lower alkyl group or the like.
    Type: Grant
    Filed: August 3, 2005
    Date of Patent: May 29, 2012
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Tae Fukushima, Shuji Matsumura, Noriaki Takemura, Hideaki Satou, Nobuaki Ito, Takuya Shitsuta, Hironori Tsutsui, Michinori Tanaka, Keizo Kan, Hitoshi Nagao, Kenji Watanabe, Kuninori Tai, Takashi Nakagawa, Hideki Takasu, Makoto Sakamoto, Keisuke Miyajima, Satoshi Yamada, Yutaka Kojima, Koichi Yasumura, Naoto Ohi, Mitsuhiro Okuno, Kazuhisa Sugiyama, Kunihiko Kiyono, Takashi Suzuki, Seiji Akamatsu, Takeshi Kodama, Yasuo Yanagihara, Takumi Sumida
  • Patent number: 8178535
    Abstract: Substituted sulfonamide compounds corresponding to the formula I? wherein m, n, p, X, Y, Z, R1, RA and RB have specified meanings, processes for their preparation, pharmaceutical compositions containing these compounds, and the use of these substituted sulfonamide compounds for the treatment and/or inhibition of pain or other conditions.
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: May 15, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Beatrix Merla, Stefan Oberboersch, Ruth Jostock, Michael Engels, Stefan Schunk, Melanie Reich, Sabine Hees
  • Patent number: 8178527
    Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.
    Type: Grant
    Filed: October 2, 2007
    Date of Patent: May 15, 2012
    Assignee: Erimos Pharmaceuticals LLC
    Inventors: Qingqi Chen, Rocio Alejandra Lopez, Jonathan Daniel Heller, Amanda Jean Morris
  • Patent number: 8173647
    Abstract: Phosphatidylinositol (PI) 3-kinase inhibitor compounds, their pharmaceutically acceptable salts, and prodrugs thereof; compositions of the new compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of diseases characterized by the abnormal activity of growth factors, protein serine/threonine kinases, and phospholipid kinases, including proliferative diseases, inflammatory and obstructive airways diseases, allergic conditions, autoimmune and cardiovascular diseases.
    Type: Grant
    Filed: February 6, 2008
    Date of Patent: May 8, 2012
    Inventors: Gordana Atallah, Sarah Bartulis, Matthew Burger, Hanne Merritt, Simon Ng, Zhi-Jie Ni, Sabina Pecchi, Keith B. Pfister, Aaron Smith, Charles Voliva, Allan Wagman, Yanchen Zhang
  • Publication number: 20120101080
    Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula (1) wherein R1 is optionally substituted phenyl, optionally substituted pyridyl or optionally substituted indolyl; R2 is (CH2)n wherein n is 0, 1, 2, 3 or 4; R3 is (CH2)mR3A wherein m is 0, 1, 2, 3 or 4, and R3A is methyl, isopropyl, tert-butyl, OCH3, OH, optionally substituted phenoxy, C?CH, C?N, optionally substituted phenyl, furanyl or thienyl; A is a ring containing X1 with the meaning O, S, NH, N(CH3) or CH2; and X2 is O, S or NH; and a compound of formula (2) wherein R4 is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted indolyl, —NR7R8; or —NH—N?CH—R9; and substituents R5 to R9 have the meanings indicated in the description, in particular ethionamide. The pharmaceutical composition is useful, e.g., in the treatment of multidrug-resistant tuberculosis.
    Type: Application
    Filed: June 25, 2010
    Publication date: April 26, 2012
    Applicant: BioVersys AG
    Inventors: Ronald Schoenmakers, Wilfried Weber, Marc Gitzinger, Martin Fussenegger, Marcel Tigges, Peter Schneider
  • Patent number: 8158622
    Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: April 17, 2012
    Assignee: Prosidion Limited
    Inventors: Stuart Edward Bradley, Thomas Martin Krulle, Peter John Murray, Martin James Procter, Robert John Rowley, Colin Peter Sambrook Smith, Gerard Hugh Thomas, Karen Lesley Schofield
  • Patent number: 8153631
    Abstract: The present invention provides a triazole compound of the following formula: a prodrug thereof or a pharmaceutically acceptable salt thereof. The above-mentioned triazole compound has superior HSD1 inhibitory activity, and is useful as an HSD1 inhibitor, a therapeutic drug of diabetes or a therapeutic drug of obesity or a therapeutic drug of metabolic syndrome.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: April 10, 2012
    Assignee: Amgen Inc.
    Inventors: Jay P. Powers, Mario G. Cardozo, Hiroyuki Goto, Kazuhito Harada, Katsuaki Imamura, Makoto Kakutani, Isamu Matsuda, Yasuhiro Ohe, Shinji Yata
  • Patent number: 8143393
    Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: December 1, 2006
    Date of Patent: March 27, 2012
    Assignee: Bayer HealthCare LLC
    Inventors: Julie A. Dixon, Barton Phillips, Furahi Achebe, Harold C. E. Kluender, Jason Newcom, Kyle Parcella, Steven Magnuson, Zhenqiu Hong, Zhonghua Zhang, Zheng Liu, Uday Khire, Lei Wang, Martin Michels, Brent Chandler, Stephen O'Connor
  • Patent number: 8129379
    Abstract: This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: September 2, 2009
    Date of Patent: March 6, 2012
    Assignee: Bayer HealthCare LLC
    Inventors: Julie A. Dixon, Barton Phillips, Furahi Achebe, Harold C. E. Kluender, Jason Newcom, Kyle Parcella, Steven Magnuson, Zhenqiu Hong, Zhonghua Zhang, Zheng Liu, Uday Khire, Lei Wang, Martin Michels, Brent Chandler, Stephen O'Connor