Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/243)
  • Aromatic ring fused triazine derivatives and uses thereof
    Patent number: 8349835
    Abstract: The invention belongs to pharmaceutical field. The invention relates to the compounds according to Formula I, including their optically active forms, pharmaceutically acceptable salts or hydrates, and the pharmaceutical composition comprising thereof as active ingredient; uses in the preparation of vascular endothelial growth factor receptor tyrosine kinase inhibitors, and uses in the preparation of medicament for the treatment and/or prevention of cancer.
    Type: Grant
    Filed: February 10, 2009
    Date of Patent: January 8, 2013
    Assignee: Shenyang Pharmaceutical University
    Inventors: Linxiang Zhao, Jinling Lv, Rui Wang, Dan Liu, Yongkui Jing
  • Dioxolane derivates for the treatment of cancer
    Patent number: 8349834
    Abstract: This invention relates to certain unsaturated fatty acid derivatives of therapeutically active 1,3-dioxolane nucleoside analogues and to pharmaceutical formulations containing them. The said derivatives fall within formula (I). Compounds of formula (I) can be used in the treatment of a cancerous disease, including solid tumors and haematological cancers such as leukaemias, lymphomas and multiple myelomas.
    Type: Grant
    Filed: December 7, 2006
    Date of Patent: January 8, 2013
    Assignee: Clavis Pharma AS
    Inventors: Finn Myhren, Marit Liland Sandvold, Steinar Hagen, Ole Henrik Eriksen
  • COMBINATION ANTI-CANCER THERAPY
    Publication number: 20130005733
    Abstract: Methods and compositions for treating cancer comprising administering to a patient inhibitors of mT0RC1/C2, IGF-1 R, and IR. In some aspects, a combination of an mT0RC1/C2 inhibitor and an IGF-1 R/IR inhibitor is employed. Other aspects are described herein.
    Type: Application
    Filed: March 9, 2011
    Publication date: January 3, 2013
    Inventors: Sharon Barr, Elizabeth A. Buck, David M. Epstein, Prafulla C. Gokhale, Mark R. Miglarese
  • Triazinedione derivatives as GABAreceptor modulators
    Patent number: 8344138
    Abstract: The present invention provides novel compounds of formula I wherein W1, W2, W3, W4, W5, B, X1, X2, X3, X4, X5, E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B (“GABAB”) positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.
    Type: Grant
    Filed: November 9, 2007
    Date of Patent: January 1, 2013
    Assignee: Addex Pharma S.A.
    Inventors: Eric Riguet, Brice Campo, Antoine Gibelin, Karim Mhalla
  • Pyrrolotriazine derivatives useful for treating cancer through inhibition of aurora kinase
    Patent number: 8338594
    Abstract: This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly Cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly Cancer.
    Type: Grant
    Filed: December 1, 2006
    Date of Patent: December 25, 2012
    Assignee: Bayer HealthCare LLC
    Inventors: Steven Magnuson, Julie Dixon, Barton Phillips, Uday Khire, Lei Wang, Zhonghua Zhang, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Philip Wickens, Alan Olague
  • Pyrrolotriazine derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
    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
  • Methods and Compositions for Treating Cancer
    Publication number: 20120316137
    Abstract: The invention features methods, kits, and pharmaceutical compositions for treating cancer using 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)-methyl)-3-(trifluoromethyl)phenyl)benzamide.
    Type: Application
    Filed: November 1, 2010
    Publication date: December 13, 2012
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: Wei-Sheng Huang, Victor M. Rivera, Timothy P. Clackson, William C. Shakespeare, Rachel M. Squillace, Joseph M. Gozgit
  • HETEROCYCLIC OXIME COMPOUNDS
    Publication number: 20120302570
    Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
    Type: Application
    Filed: August 6, 2012
    Publication date: November 29, 2012
    Applicant: NOVARTIS AG
    Inventors: Miao DAI, Xingnian FU, Feng HE, Lei JIANG, Yue LI, Fang LIANG, Lei LIU, Yuan MI, Yao-Chang XU, Guoliang XUN, Xiaoxia YAN, Zhengtian YU, Ji Yue ZHANG
  • CRYSTALLINE FORMS OF (S)-1-(4-(5-CYCLOPROPYL-1H-PYRAZOL-3-YLAMINO)PYRROLO[1,2-f][1,2,4]TRIAZIN-2-YL)-N-(6-FLUOROPYRIDIN-3-YL)-2-METHYLPYRROLIDINE-2-CARBOXAMIDE
    Publication number: 20120302571
    Abstract: Crystalline forms of (S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide of the formula (I) are provided. Also provided is a pharmaceutical composition comprising one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol, as well as a method of using one or more crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol in the treatment of cancer and other proliferative diseases.
    Type: Application
    Filed: February 3, 2011
    Publication date: November 29, 2012
    Inventors: Roxana Schlam, Alicia Tee Fuay Ng, Chenkou Wei
  • Reverse-turn mimetics and method relating thereto
    Patent number: 8318738
    Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: November 27, 2012
    Assignee: Choongwae Pharma Corporation
    Inventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
  • COMBINATION OF KINASE INHIBITORS AND USES THEREOF
    Publication number: 20120294930
    Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.
    Type: Application
    Filed: February 23, 2012
    Publication date: November 22, 2012
    Applicant: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
  • HETEROCYCLIC COMPOUND AS PROTEIN KINASE INHIBITOR
    Publication number: 20120289509
    Abstract: Provided are novel heterocyclic compounds useful as anti-cancer drugs by suppressing protein kinase activities of growth factor receptors such as c-Met, pharmaceutical compositions containing the same, and methods for using the compound.
    Type: Application
    Filed: July 6, 2012
    Publication date: November 15, 2012
    Applicant: NEOPHARM CO., LTD.
    Inventors: Tae-Seong KIM, Eunkyung LEE, Doyoung KIM, Bu-mahn PARK, Jiyeon PARK, JungJe JOO
  • FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS
    Publication number: 20120289493
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: May 8, 2012
    Publication date: November 15, 2012
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Compounds for treating pulmonary hypertension
    Patent number: 8304406
    Abstract: The present invention relates to pharmaceutical compositions and combinations for treating, preventing or managing pulmonary hypertension comprising small molecule heterocyclic pharmaceuticals, and more particularly, substituted pyridines and pyridazines optionally combined with at least one additional therapeutic agent.
    Type: Grant
    Filed: April 3, 2007
    Date of Patent: November 6, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Martina Klein, Peter Sandner, Reiner Frey, Bernd Riedl, Olaf Christensen
  • HYDROXYMETHYL PYRROLIDINES AS BETA 3 ADRENERGIC RECEPTOR AGONISTS
    Publication number: 20120258963
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Application
    Filed: June 20, 2012
    Publication date: October 11, 2012
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
  • USE OF PHOSPHODIESTERASE INHIBITORS FOR TREATING MULTIDRUG RESISTANCE
    Publication number: 20120252816
    Abstract: The present invention relates to methods of treating multidrug resistance in cancerous cells with phosphodiesterase (PDE) inhibitors, e.g., PDE5 inhibitors. More specifically, the invention relates to methods of treating multidrug resistance that arises, e.g., during administration of chemotherapeutic/antineoplastic (anticancer) agents for treatment of cancer, with a PDE5 inhibitor (e.g., sildenafil, vardenafil, and tadalafil). The invention also relates to methods of treating cancer, e.g., multidrug resistant cancer, using a PDE5 inhibitor in combination with an antineoplastic therapeutic agent. Further, the invention relates to pharmaceutical compositions for treating multidrug resistant cancers comprising a PDE5 inhibitor, or a combination of a PDE5 inhibitor and an antineoplastic agent.
    Type: Application
    Filed: March 28, 2012
    Publication date: October 4, 2012
    Inventors: Zhe-Sheng CHEN, Zhi SHI, Charles R. ASHBY, JR.
  • GAMMA SECRETASE MODULATORS
    Publication number: 20120245158
    Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula I: Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula I.
    Type: Application
    Filed: June 15, 2010
    Publication date: September 27, 2012
    Inventors: Xianhai Huang, Zhaoning Zhu, William J. Greenlee, Anandan Palani, Robert G. Aslanian
  • Medicaments containing vardenafil hydrochloride trihydrate
    Patent number: 8273876
    Abstract: The invention relates to a method for producing medicaments that contain vardenafil hydrochloride, essentially as trihydrate in solid form, and to medicaments that can be obtained according to this method.
    Type: Grant
    Filed: July 3, 2003
    Date of Patent: September 25, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Peter Serno, Alfons Grunenberg, Andreas Ohm, Rainer Bellinghausen, Eimer Vollers, Jan-Olav Henck
  • Pyrrolotriazine kinase inhibitors
    Patent number: 8268998
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB, TrkC or Flt-3 thereby making them useful as anticancer agents.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: September 18, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Brian E. Fink, Ping Chen
  • PYRROLOTRIAZINE COMPOUNDS
    Publication number: 20120232054
    Abstract: A compound of formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, has a Btk inhibitory activity, and is useful as a method for preventing and/or treating a rheumatoid arthritis, an autoimmune disease, a B cell lymphoma of cancer, and the like.
    Type: Application
    Filed: April 28, 2010
    Publication date: September 13, 2012
    Applicant: LOCUS PHARMACEUTICALS, INC.
    Inventors: Kevin J. Moriarty, Dora Do-York Wong, Zenon Konteatis, Kristofer Moffett, Younghee Lee, Wenchun Chao
  • Pyrrolotriazine kinase inhibitors
    Patent number: 8263765
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: September 11, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark D. Wittman, Kurt Zimmermann, Xiaopeng Sang
  • Anti-cancer drugs and uses relating thereto for metastatic malignant melanoma and other cancers
    Patent number: 8258119
    Abstract: The present invention discloses triazene analogs of the general formula (I) and formula (II), their tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, and pharmaceutically acceptable salts thereof for the metastatic malignant melanoma and other cancers including but not limited to lymphomas, sarcomas, carcinomas, and gliomas. The invention further discloses a process for the preparation of the above said triazene analogs of formula (I) and formula (II), and their pharmaceutically acceptable compositions.
    Type: Grant
    Filed: September 15, 2009
    Date of Patent: September 4, 2012
    Assignee: Kasina Laila Innova Pharmaceuticals
    Inventors: Ganga Raju Gokaraju, Sudhakar Kasina, Rama Raju Gokaraju, Trimurtulu Golakoti, Venkateswarlu Somepalli, Sengupta Krishanu, Kiran Bhupathiraju
  • METHODS FOR TREATING CANCER IN PATIENTS HAVING IGF-1R INHIBITOR RESISTANCE
    Publication number: 20120220594
    Abstract: A method for treating cancer comprising identifying a mammal that overexpresses breast cancer resistance protein; and administering to said mammal a pharmaceutical composition comprising a therapeutically effective amount of ixabepilone. In one aspect, the mammal is not administered an agent that is susceptible to breast cancer resistance protein overexpression resistance. In another aspect, the cancer is a solid tumor.
    Type: Application
    Filed: October 29, 2010
    Publication date: August 30, 2012
    Inventors: Fei Huang, Joan Carboni
  • HETEROCYCLIC COMPOUNDS AND METHODS OF USE
    Publication number: 20120220584
    Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
    Type: Application
    Filed: September 23, 2011
    Publication date: August 30, 2012
    Applicant: TargeGen, Inc.
    Inventors: Wolfgang WRASIDLO, Elena Dneprovskaia
  • Deuterated Tyrosine Kinase Inhibitors
    Publication number: 20120220595
    Abstract: Compounds of Formula I, as shown below and defined herein: enriched in deuterium, and pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by IGF-1R and/or IR.
    Type: Application
    Filed: November 11, 2010
    Publication date: August 30, 2012
    Inventors: David M. Epstein, Meizhong Jin, Mark J. Mulvihill
  • Imidazo[5,1-f][1,2,4]Triazines for the Treatment of Neurological Disorders
    Publication number: 20120214791
    Abstract: The present invention relates to compounds of the Formula and pharmaceutically acceptable salts thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as a method for the treatment of a disease or condition selected from the group consisting of central nervous system disorders, cognitive disorders, schizophrenia, dementia and other disorders in a mammal.
    Type: Application
    Filed: February 20, 2012
    Publication date: August 23, 2012
    Inventors: Christopher John HELAL, Thomas Allen CHAPPIE, John Michael HUMPHREY, Patrick Robert VERHOEST, Eddie YANG
  • HETEROCYCLIC COMPOUNDS USEFUL AS PDK1 INHIBITORS
    Publication number: 20120208819
    Abstract: The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.
    Type: Application
    Filed: October 5, 2010
    Publication date: August 16, 2012
    Inventors: Joseph Arndt, Timothy Chan, Kevin Guckian, Gnanasambandam Kumaravel, Wen-Cherng Lee, Edward Yin-Shiang Lin, Daniel Scott, Lihong Sun, Jermaine Thomas, Kurt van Vloten, Deping Wang, Lei Zhang, Daniel Erlanson
  • Combined Treatment with an EGFR Kinase Inhibitor and an Agent that Sensitizes Tumor Cells to the Effects of EGFR Kinase Inhibitors
    Publication number: 20120207767
    Abstract: The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein said agent is an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases. The present invention also provides a pharmaceutical composition comprising an EGFR kinase inhibitor and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing the methods of this invention is the compound erlotinib HCl (also known as TARCEVA®).
    Type: Application
    Filed: February 10, 2012
    Publication date: August 16, 2012
    Inventors: Elizabeth A. Buck, Graeme Griffin, Sharon M. Barr
  • VASODILATOR-ENHANCED CARDIOPULMONARY RESUSCITATION
    Publication number: 20120203147
    Abstract: A method for increasing blood flow to vital organs during cardiopulmonary resuscitation of a person experiencing a cardiac arrest may include performing standard or active compression decompression cardiopulmonary resuscitation on a person to create artificial circulation by repetitively compressing the person's chest such that the person's chest is subject to a compression phase and a relaxation or decompression phase. The method may also include administering one or more vasodilator drugs to the person to improve the artificial circulation created by the cardiopulmonary resuscitation. The method may also include binding at least a portion of the person's abdomen, either manually or with an abdominal compression device. Performing cardiopulmonary resuscitation on a person may include ventilating the person with either an impedance threshold device or a intrathoracic pressure regulator.
    Type: Application
    Filed: July 1, 2011
    Publication date: August 9, 2012
    Applicant: ResQSystems, Inc.
    Inventors: Keith Lurie, Demetris Yannopoulos
  • Pellets Formulation
    Publication number: 20120201893
    Abstract: A process for preparing pellets by high shear granulation containing a pharmaceutical active ingredient with a pH dependent water solubility, the pellets obtained with said process and pharmaceutical oral dosage forms comprising said pellets.
    Type: Application
    Filed: July 6, 2010
    Publication date: August 9, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Svenja Gutsche, Heiko Kranz, Michael Krause
  • (R)-1-(4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-5-METHYLPYRROLO[2,1-f][1,2,4]TRIAZIN-6-YLOXY)PROPAN-2-OL METABOLITES
    Publication number: 20120196814
    Abstract: The present invention is directed to metabolites of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol, the compound of formula (I), pharmaceutical compositions thereof, and to methods of using the metabolites and the pharmaceutical compositions in the treatment of cancer.
    Type: Application
    Filed: October 4, 2010
    Publication date: August 2, 2012
    Applicant: Bristol-Myers Squibb Company
    Inventors: Jiachang Gong, Lisa J. Christopher, Vinod Kumar Arora
  • 6,6-Bicyclic Ring Substituted Heterobicyclic Protein Kinase Inhibitors
    Publication number: 20120196847
    Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.
    Type: Application
    Filed: April 13, 2012
    Publication date: August 2, 2012
    Inventors: Lee D. Arnold, Heather Coate, Andrew Philip Crew, Hanqing Dong, Kenneth Foreman, Ayako Honda, Radoslaw Laufer, An-Hu Li, Kristen Michelle Mulvihill, Mark Joseph Mulvihill, Anthony Nigro, Bijoy Panicker, Arno G. Steinig, Qingua Weng, Douglas S. Werner, Michael J. Wyle, Tao Zhang, Cara Cesario, Yingchuan Sun
  • COMPOSITION COMPRISING A PDE4 INHIBITOR AND A PDE5 INHIBITOR
    Publication number: 20120196867
    Abstract: The claimed subject matter relates to pharmaceutical compositions comprising a PDE4 inhibitor and a PDE5 inhibitor and the treatment of a disease in which phosphodiesterase 4 (PDE4) and/or phosphodiesterase 5 (PDE5) is detrimental.
    Type: Application
    Filed: April 12, 2012
    Publication date: August 2, 2012
    Applicant: NYCOMED GMBH
    Inventors: Torsten DUNKERN, Armin HATZELMANN, Christian SCHUDT, Friedrich GRIMMINGER, Hossein Ardeschir GHOFRANI
  • 2-Oxo-1-Pyrrolidine Derivatives, Processes for Preparing Them and Their Uses
    Publication number: 20120196866
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: April 6, 2012
    Publication date: August 2, 2012
    Applicant: UCB PHARMA, S.A.
    Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
  • CO-PRECIPITATE COMPRISING A PHOSPHODIESTERASE-5 INHIBITOR (PDE-5-INHIBITOR) AND A PHARMACEUTICALLY COMPATIBLE CARRIER, PRODUCTION AND USE THEREOF
    Publication number: 20120189694
    Abstract: The invention relates to a co-precipitate comprising a phosphodiesterase-5 inhibitor (PDE-5-inhibitor) and a pharmaceutically compatible copolymer carrier comprising 2 or more different acrylic acid derivatives, a method for production thereof and a medication comprising the co-precipitate according to the invention, a method for producing said medication and the use of said medication for treating an illness wherein the inhibiting of phosphodiesterase-5 is of therapeutic benefit.
    Type: Application
    Filed: July 8, 2010
    Publication date: July 26, 2012
    Applicant: ratiopharm GmbH
    Inventors: Katrin Rimkus, Frank Muskulus
  • SUBSTITUTED ENZOIMIDAZOLESULFONAMIDES AND SUBSTITUTED INDOLESULFONAMIDES AS MGLUR4 POTENTIATORS
    Publication number: 20120184556
    Abstract: Disclosed are substituted benzoimidazolesulfonamides and substituted indolesulfonamides as mGluR4 potentiators.
    Type: Application
    Filed: July 23, 2010
    Publication date: July 19, 2012
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
  • Pyrrolotriazine kinase inhibitors
    Patent number: 8212031
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: July 3, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Upender Velaparthi, Dolatrai M. Vyas
  • SUBSTITUTED 4-AMINO-PYRROLOTRIAZINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
    Publication number: 20120165314
    Abstract: This invention relates to novel 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: Application
    Filed: March 7, 2012
    Publication date: June 28, 2012
    Applicant: Bayer HealthCare LLC
    Inventors: Julie Dixon, Barton Phillips, Yamin Wang, Tindy Li, Kyle Parcella, Jason Newcom, Harold C.E. Kluender, Zhenqiu Hong, Brent Chandler, Zhonghua Zhang, Steven Magnuson, Kristen M. Allegue, Zheng Liu
  • RAF INHIBITOR COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20120157439
    Abstract: Compounds of Formula I are useful for inhibition of Raf kinases. Methods of using compounds of Formula I and stereoisomers, tautomers, prodrugs and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Application
    Filed: August 27, 2010
    Publication date: June 21, 2012
    Applicants: GENENTECH, INC., ARRAY BIOPHARMA INC.
    Inventors: Ignacio Aliagas, Stefan Gradl, Janet Gunzner, Simon Mathieu, Rebecca Pulk, Joachim Rudolph, Zhaoyang Wen, Jonas Grina, Joshua D. Hansen, Ellen Laird, David Moreno, Li Ren, Steven Mark Wenglowsky
  • IMIDAZOTRIAZINONE COMPOUNDS
    Publication number: 20120157458
    Abstract: The present invention provides imidazotriazinone compounds which are inhibitors of phosphodiesterase 9. The present invention further provides processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of PDE9 associated diseases or disorders in mammals, including humans.
    Type: Application
    Filed: September 20, 2011
    Publication date: June 21, 2012
    Inventors: Amy Ripka, Gideon Shapiro, Andrew J. McRiner
  • NEUROPROTECTION FROM BRAIN ANOXIA AND REPERFUSION INJURY DURING STROKE AND COMPOSITIONS OF PKG PATHWAY ACTIVATORS AND METHOD OF USE THEREOF
    Publication number: 20120148560
    Abstract: A pharmaceutical composition for treating or preventing one or both of neural anoxia and reperfusion injury, which includes a pharmacological activator of the PKG pathway, and methods of treating or preventing medical conditions using a pharmacological activator of the PKG pathway.
    Type: Application
    Filed: December 15, 2011
    Publication date: June 14, 2012
    Applicant: Florida Atlantic University
    Inventors: Kenneth DAWSON-SCULLY, Sara Louise Milton
  • Heterocyclic Compounds as Janus Kinase Inhibitors
    Publication number: 20120149662
    Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula (I) and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula (I).
    Type: Application
    Filed: August 27, 2010
    Publication date: June 14, 2012
    Applicant: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pravin L. Kotian, V. Satish Kumar, Minwan Wu, Tsu-Hsing Lin
  • Pyrrolotriazine kinase inhibitors
    Patent number: 8198438
    Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anti-cancer agents and for the treatment of Alzheimer's Disease.
    Type: Grant
    Filed: April 17, 2008
    Date of Patent: June 12, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Anthony J. Sampognaro, Mark D. Wittman
  • HETEROCYCLIC HYDRAZONE COMPOUNDS
    Publication number: 20120142681
    Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
    Type: Application
    Filed: August 10, 2010
    Publication date: June 7, 2012
    Applicant: NOVARTIS AG
    Inventors: Feng He, Miao Dai, Xingnian Fu, Yue Li, Lei Liu, Yuan Mi, Yao-chang Xu, Guoliang Xun, Zhengtian Yu, Ji Yue Zhang
  • Methods of Use of Inhibitors of Phosphodiesterases and Modulators of Nitric Oxide, Reactive Oxygen Species, and Metalloproteinases in the Treatment of Peyronie's Disease, Arteriosclerosis and Other Fibrotic Diseases
    Publication number: 20120141454
    Abstract: The present methods and compositions are of use for treatment of conditions involving fibrosis, such as Peyronie's disease plaque, penile corporal fibrosis, penile veno-occlusive dysfunction, Dupuytren's disease nodules, vaginal fibrosis, clitoral fibrosis, female sexual arousal disorder, abnormal wound healing, keloid formation, general fibrosis of the kidney, bladder, prostate, skin, liver, lung, heart, intestines or any other localized or generalized fibrotic condition, vascular fibrosis, arterial intima hyperplasia, atherosclerosis, arteriosclerosis, restenosis, cardiac hypertrophy, hypertension or any condition characterized by excessive fibroblast or smooth muscle cell proliferation or deposition of collagen and extracellular matrix in the blood vessels and/or heart.
    Type: Application
    Filed: February 13, 2012
    Publication date: June 7, 2012
    Applicant: Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center
    Inventors: Nestor F. Gonzalez-Cadavid, Jacob Rajfer
  • Fused heterocyclic compounds useful as kinase modulators
    Patent number: 8188272
    Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, [PLEASE INSERT CHEMICAL STRUCTURE HERE] (I) are useful as kinase modulators, including Btk modulation, wherein R1, R2, R4, Q, Y, A and D are as defined herein.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: May 29, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Chunjian Liu, Katerina Leftheris, Andrew J. Tebben
  • Polycyclic carbamoylpyridone derivative having HIV integrase inhibitory activity
    Patent number: 8188271
    Abstract: Is to provide a novel compound having an anti-viral activity, particularly a HIV integrase inhibitory activity, and a pharmaceutical composition, particularly an anti-HIV agent. (wherein R1 is hydrogen or lower alkyl; X is lower alkylene etc.; R2 is optionally substituted aryl; R3 is hydrogen, halogen, hydroxy, optionally substituted lower alkyl etc.; R4 is hydrogen, optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkyl lower alkyl, optionally substituted aryl, optionally substituted aryl lower alkyl, optionally substituted heterocyclic group, optionally substituted heterocyclic lower alkyl etc.; A broken line indicates the presence or absence of a bond; B1 and B2 are such that any one of them is CR20R21, and the other is NR22 and, in this case, there is no broken line.
    Type: Grant
    Filed: October 26, 2006
    Date of Patent: May 29, 2012
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroshi Yoshida, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
  • TREATMENT OF LUNG CANCER WITH A NITROBENZAMIDE COMPOUND IN COMBINATION WITH A GROWTH FACTOR INHIBITOR
    Publication number: 20120130144
    Abstract: In one aspect, the present invention provides a method of treating lung cancer, comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor. In another aspect, the present invention provides a method of treating non-small cell lung cancer comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor.
    Type: Application
    Filed: February 4, 2010
    Publication date: May 24, 2012
    Applicant: BiPar Sciences, Inc.
    Inventors: Barry M. Sherman, Charles Bradley, Valeria S. Ossovskaya
  • mTOR INHIBITOR AND ANGIOGENESIS INHIBITOR COMBINATION THERAPY
    Publication number: 20120128670
    Abstract: Cancer therapy comprising treatment with an mTOR inhibitor, such as a dual mTORC1/mTORC2 inhibitor, such as OSI-027, in combination with an angiogenesis inhibitor.
    Type: Application
    Filed: July 30, 2010
    Publication date: May 24, 2012
    Applicant: OSI PHARMACEUTICALS, LLC
    Inventors: Sharon M. Barr, Prafulla C. Gokhale, Robert C. Wild
  • GAMMA SECRETASE MODULATORS
    Publication number: 20120129846
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: November 5, 2009
    Publication date: May 24, 2012
    Inventors: Zhaoning Zhu, William J. Greenlee, Mihir Baran Mandal, Duane A. Burnett, Chad E. Bennett, Troy McCracken