Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/243)
  • Patent number: 10280172
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein B, W, X, Y, R1, R2a, R2b, R3a, R3b, R4a, R4b, G1, G2, m1, m2, L1, L2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: May 7, 2019
    Assignee: Araxes Pharma LLC
    Inventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Pingda Ren, Yi Liu
  • Patent number: 10265314
    Abstract: The present invention relates to soluble guanylate cyclase (sGC) and to phosphodiesterases (PDEs) and the pharmacology of sGC stimulators, sGC activators and PDE inhibitors (PDE5i) in combination with a) treatments, leading to increased cGMP mobilization, and/or b) tretaments correcting and/or potentiatiating CFTR function, and/or c) treatments currently used as standard of care in Cystic Fibrosis, and/or d) antinflammatory treatments for the preparation of medicaments for the treatment of Cystic Fibrosis (CF) with improved efficacy over methods of treatments already known.
    Type: Grant
    Filed: July 21, 2014
    Date of Patent: April 23, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Peter Sandner, Johannes-Peter Stasch, Michael Hahn, Markus Follmann
  • Patent number: 10245265
    Abstract: The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.
    Type: Grant
    Filed: November 18, 2016
    Date of Patent: April 2, 2019
    Assignees: INCYTE INCORPORATION, INCYTE HOLDINGS CORPORATION
    Inventors: Lingkai Weng, Lei Qiao, Jiacheng Zhou, Pingli Liu, Yongchun Pan
  • Patent number: 10221197
    Abstract: The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, or a mixture thereof, wherein n, m, q, A?, W1, W2, W3, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.
    Type: Grant
    Filed: June 10, 2015
    Date of Patent: March 5, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Zhimin Du, Jerry Evarts, Joshua Kaplan, Musong Kim, Devan Naduthambi, Leena Patel, Stephane Perreault, Barton W. Phillips, Gary Phillips, Kirk L. Stevens, Jennifer A. Treiberg, Joshua Van Veldhuizen, William J. Watkins, Suet Chung Yeung
  • Patent number: 10208053
    Abstract: The present invention relates to 1,3-disubstituted-1H-pyrazolo[3,4-d]pyrimidin-4-amine derivatives and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compounds, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjögren's Syndrome, and other CFTR associated disorders.
    Type: Grant
    Filed: September 17, 2018
    Date of Patent: February 19, 2019
    Assignee: CYSTIC FIBROSIS FOUNDATION THERAPEUTICS, INC.
    Inventors: Joseph Walter Strohbach, David Christopher Limburg, John Paul Mathias, Atli Thorarensen, John James Mousseau, Rajiah Aldrin Denny, Christoph Wolfgang Zapf, Ivan Viktorovich Efremov
  • Patent number: 10189843
    Abstract: The present invention provides a compound of formula (1), wherein R1, R2, R3, R4a, R4b, R5a and R5b are as defined in the description, which has an autotaxin inhibitory activity, a pharmaceutical composition comprising the compound as an active ingredient, and a method of prevention or treatment of a disease involving autotaxin, which is characterized by administering the compound.
    Type: Grant
    Filed: February 26, 2015
    Date of Patent: January 29, 2019
    Assignees: THE UNIVERSITY OF TOKYO, TOHOKU UNIVERSITY, SHIONOGI & CO., LTD.
    Inventors: Tetsuo Nagano, Takayoshi Okabe, Hirotatsu Kojima, Mitsuyasu Kawaguchi, Osamu Nureki, Ryuichiro Ishitani, Hiroshi Nishimasu, Junken Aoki, Chiaki Fujikoshi, Manabu Katou, Masahide Odan, Nobuyuki Tanaka, Yusuke Tateno, Junji Yamane
  • Patent number: 10131670
    Abstract: The present invention relates to 1,3-disubstituted-1H-pyrazolo[3,4-d]pyrimidin-4-amine derivatives, 5,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives or 5,7-disubstituted-imidazo[5,1-f][1,2,4]triazine-4-amine derivatives, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compounds, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjögren's Syndrome, and other CFTR associated disorders.
    Type: Grant
    Filed: December 14, 2017
    Date of Patent: November 20, 2018
    Assignee: CYSTIC FIBROSIS FOUNDATION THERAPEUTICS, INC.
    Inventors: Joseph Walter Strohbach, David Christopher Limburg, John Paul Mathias, Atli Thorarensen, John James Mousseau, Rajiah Aldrin Denny, Christoph Wolfgang Zapf, Ivan Viktorovich Efremov
  • Patent number: 10106545
    Abstract: The present teachings provide a compound represented by structural formula (I-0), or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
    Type: Grant
    Filed: February 16, 2017
    Date of Patent: October 23, 2018
    Assignee: University Health Network
    Inventors: Yong Liu, Heinz W. Pauls, Radoslaw Laufer, Sze-Wan Li, Peter Brent Sampson, Miklos Feher, Grace Ng, Narendra Kumar B. Patel, Yunhui Lang
  • Patent number: 10100048
    Abstract: The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
    Type: Grant
    Filed: September 30, 2015
    Date of Patent: October 16, 2018
    Assignee: ABBVIE DEUTSCHLAND GMBH & CO. KG
    Inventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Marcel van Gaalen, Falko Ernst Wolter, Wilfried Hornberger, Marjoleen Nijsen
  • Patent number: 10085993
    Abstract: The present invention is related to tablets comprising of 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, processes for the production thereof, and uses in the treatment of certain cancers.
    Type: Grant
    Filed: July 22, 2015
    Date of Patent: October 2, 2018
    Assignee: Novartis AG
    Inventors: Elisabete Goncalves, Christin Tauchmann, Shau-Fong Yen, Sudha Vippagunta, Zhixin Zong
  • Patent number: 10065965
    Abstract: A compound of Formula (I), or a salt thereof, compositions comprising the compound, processes for its preparation and its use in therapy, for example in the treatment of parasitic diseases such as Chagas disease, Human African Trypanosomiasis (HAT) and leishmaniasis, particularly visceral leishmaniasis (VL).
    Type: Grant
    Filed: May 26, 2016
    Date of Patent: September 4, 2018
    Assignees: GlaxoSmithKline Intellectual Property Development Limited, The University of Dundee
    Inventors: Stephen Brand, Elisabet Viayna Gaza, Ian Gilbert, Eun Jung Ko, Maria Marco Martin, Timothy James Miles, Lars Henrik Sandberg, Michael George Thomas
  • Patent number: 9993475
    Abstract: A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: June 12, 2018
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael J. Gerber, Christopher Dufton
  • Patent number: 9981925
    Abstract: Novel azaquinazoline carboxamide derivatives of formula (I) wherein W1, W2, W3, W4, R1, R2, R3 and m which are defined above, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: May 29, 2018
    Assignee: Merck Patent GmbH
    Inventors: Bayard R. Huck, Ruoxi Lan, Justin Potnick, Lizbeth Celeste Deselm, Mark W. Cronin, Jr., Constantin Neagu, Xiaoling Chen, Roch Boivin, Theresa L. Johnson, Andreas Goutopoulos
  • Patent number: 9969741
    Abstract: The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3 and R4 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
    Type: Grant
    Filed: June 17, 2015
    Date of Patent: May 15, 2018
    Assignee: MASARYKOVA UNIVERZITA
    Inventors: Jiri Damborsky, Fedor Nikulenkov, Alexandra Sisakova, Stepan Havel, Lumir Krejci, Benoit Carbain, Jan Brezovsky, Lukas Daniel, Kamil Paruch
  • Patent number: 9944645
    Abstract: The present invention is directed to imidazo[1,2-b][1,2,4]triazines and imidazo[1,2-a]pyrimidines, and pharmaceutical compositions thereof, which are inhibitors of kinases such as c-Met and are useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: April 17, 2018
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Jincong Zhuo, Meizhong Xu, Chunhong He, Colin Zhang, Ding-Quan Qian, David M. Burns, Yun-Long Li, Brian Metcalf, Wenqing Yao
  • Patent number: 9856263
    Abstract: The present invention provides, in part, compounds of Formula (I): and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), schizotypal personality disorder, cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, Parkinson's disease, anxiety, and depression.
    Type: Grant
    Filed: April 15, 2015
    Date of Patent: January 2, 2018
    Assignee: PFIZER INC.
    Inventors: David Lawrence Firman Gray, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, Scot Richard Mente, Chakrapani Subramanyam
  • Patent number: 9737542
    Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
    Type: Grant
    Filed: October 8, 2014
    Date of Patent: August 22, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carolyn Diane Dzierba, Bireshwar Dasgupta, John E. Macor, Joanne J. Bronson, Ramkumar Rajamani, George N. Karageorge
  • Patent number: 9714251
    Abstract: A series of substituted imidazo[1,2-b][1,2,4]triazine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: July 25, 2017
    Assignee: UCB Biopharma SPRL
    Inventors: Daniel Christopher Brookings, Julien Alistair Brown, Victoria Elizabeth Jackson, John Robert Porter, Joanna Rachel Quincey
  • Patent number: 9714244
    Abstract: The present invention relates to compounds of formula (I) that are useful as inhibitors of the activity of Wee-1 kinase. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.
    Type: Grant
    Filed: April 11, 2014
    Date of Patent: July 25, 2017
    Assignee: ALMAC DISCOVERY LIMITED
    Inventors: Colin Roderick O'Dowd, James Samuel Shane Rountree, Frank Burkamp, Andrew John Wilkinson
  • Patent number: 9688699
    Abstract: The present application relates to novel 3-(pyrimidin-2-yl)imidazo[1,2-a]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for the treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: February 17, 2015
    Date of Patent: June 27, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Alexandros Vakalopoulos, Alexey Gromov, Markus Follmann, Damian Brockschnieder, Johannes-Peter Stasch, Tobias Marquardt, Adrian Tersteegen, Frank Wunder, Gorden Redlich, Dieter Lang, Volkhart Min-Jian Li
  • Patent number: 9688680
    Abstract: Compounds and compositions useful for treating disorders related to Kit are described herein.
    Type: Grant
    Filed: August 4, 2015
    Date of Patent: June 27, 2017
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventor: Brian L. Hodous
  • Patent number: 9663478
    Abstract: Benzotriazine doxides are disclosed as drugs targeting mycobacterium tuberculosis, including novel compounds of formula I:
    Type: Grant
    Filed: December 23, 2012
    Date of Patent: May 30, 2017
    Assignee: SRI INTERNATIONAL
    Inventors: Peter Madrid, Sidharth Chopra, Kenneth Ryan, Gary Koolpe
  • Patent number: 9605008
    Abstract: The present application relates to novel benzyl-1H-pyrazolo[3,4-b]pyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: July 8, 2014
    Date of Patent: March 28, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Alexandros Vakalopoulos, Alexey Gromov, Markus Follmann, Damian Brockschnieder, Johannes-Peter Stasch, Tobias Marquardt, Adrian Tersteegen, Frank Wunder, Gorden Redlich, Dieter Lang, Volkhart Min-Jian Li
  • Patent number: 9562046
    Abstract: In a cytotoxic compound of the general formula (I) R is H or methyl or methylene substituted by C1-C4 straight or branched alkyl, R1 is selected from the group consisting of H, C1-C4 straight or branched alkyl, methoxy, methoxy substituted by from one to three fluorine, halogen; R2 is H or C1-C4 straight or branched alkyl; X is CH or N; Y is CH or N.
    Type: Grant
    Filed: September 17, 2013
    Date of Patent: February 7, 2017
    Assignee: VIVOLUX AB
    Inventor: Stig Linder
  • Patent number: 9549926
    Abstract: Provided are formulations comprising therapeutically effective amounts of ambrisentan or a pharmaceutically acceptable salt thereof and tadalafil or a pharmaceutically acceptable salt thereof and methods of treating and/or preventing pulmonary hypertension by administration of the formulations.
    Type: Grant
    Filed: November 13, 2013
    Date of Patent: January 24, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Luiz Belardinelli, Hunter Campbell Gillies, Faquan Liang, John Shryock, Suya Yang
  • Patent number: 9504685
    Abstract: A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.
    Type: Grant
    Filed: April 24, 2015
    Date of Patent: November 29, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael J. Gerber, Christopher Dufton
  • Patent number: 9353119
    Abstract: Disclosed is a composition comprising a pyrazino-triazine derivative, an isomer thereof or a pharmaceutically acceptable salt thereof. It is very effective for preventing and treating NSCLC.
    Type: Grant
    Filed: August 7, 2012
    Date of Patent: May 31, 2016
    Assignee: JW PHARMACEUTICAL CORPORATION
    Inventors: Joo-Young Cha, Kwan-Hoo Lee, Ji-Eun Jung
  • Patent number: 9255108
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: February 9, 2016
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Katrina Chan, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Liansheng Li, Tao Liu, Yi Liu, Pingda Ren, Daniel A. Snyder, Martin R. Tremblay
  • Patent number: 9221824
    Abstract: The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer.
    Type: Grant
    Filed: June 12, 2013
    Date of Patent: December 29, 2015
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Jincong Zhuo, Chunhong He, Wenqing Yao
  • Patent number: 9200002
    Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.
    Type: Grant
    Filed: October 15, 2014
    Date of Patent: December 1, 2015
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventors: Brian L. Hodous, Joseph L. Kim, Kevin J. Wilson, Douglas Wilson, Yulian Zhang
  • Patent number: 9193734
    Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.
    Type: Grant
    Filed: June 3, 2013
    Date of Patent: November 24, 2015
    Assignee: PRISM Pharma Co., Ltd.
    Inventors: Takenao Odagami, Yuji Kogami, Hiroyuki Kouji
  • Patent number: 9133191
    Abstract: The present application relates to novel substituted fused pyrimidines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: January 8, 2013
    Date of Patent: September 15, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Frank Wunder, Dieter Lang
  • Patent number: 9066951
    Abstract: A method of inhibiting HPV virus infection is disclosed. In one embodiment, the method involves exposing a papillomavirus to an effective amount of a compound selected from the group consisting of Compound 13, Compound 14, and analogs of Compounds 13 and 14. In another embodiment, the method involves administering an inhibitor selected from the group consisting of Compound 13, Compound 14, and analogs of Compounds 13 and 14 to a susceptible tissue or cell.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: June 30, 2015
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Paul F. Lambert, Paul G. Ahlquist, Dohun Pyeon, Hao Shun Huang
  • Publication number: 20150148348
    Abstract: The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)-imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and pharmaceutical compositions thereof, useful in the treatment of cancer and other diseases related to the dysregulation of kinase pathways. The present invention further relates to processes and intermediates for preparing 2-fluoro-N-methyl-4-[7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide, and salts thereof.
    Type: Application
    Filed: October 28, 2014
    Publication date: May 28, 2015
    Inventors: Lingkai Weng, Lei Qiao, Jiacheng Zhou, Pingli Liu, Yongchun Pan
  • Patent number: 9040531
    Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a chemical library relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.
    Type: Grant
    Filed: May 7, 2010
    Date of Patent: May 26, 2015
    Assignee: PRISM BioLab Co., Ltd.
    Inventors: Takenao Odagami, Yuji Kogami, Hiroyuki Kouji
  • Patent number: 9040691
    Abstract: This invention relates to novel 5-[(hydroxymethyl)aryl]-substituted pyrrolo[2,1-f][1,2,4]triazin-4-amines of formula (I), to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating angiogenesis-related disorders, in particular angiogenesis-related ocular disorders.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: May 26, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jürgen Klar, Verena Vöhringer, Joachim Telser, Mario Lobell, Frank Süβmeier, Volkhart Min-Jian Li, Michael Böttger, Stefan Golz, Dieter Lang, Karl-Heinz Schlemmer, Thomas Schlange, Andreas Schall, Wenlang Fu
  • Publication number: 20150141423
    Abstract: Disclosed are pesticidally active pyridyl- and pyrimidyl-substituted thiazole derivatives, processes for their preparation, compositions comprising those compounds, and their use for controlling insects.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 21, 2015
    Applicant: Syngenta Participations AG
    Inventors: Ruifang Chen, Laura Quaranta, Andrew Edmunds, Andre Jeanguenat, Aurelien Bigot, Sebastian Rendler, Roger Graham Hall, Long Lu, Peter Renold
  • Publication number: 20150141429
    Abstract: The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly (ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radiosensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects.
    Type: Application
    Filed: November 11, 2014
    Publication date: May 21, 2015
    Applicant: EISAI INC.
    Inventors: Weizheng XU, Greg Delahanty, Ling Wei, Jie Zhang
  • Patent number: 9034872
    Abstract: Novel heterocyclic compounds having the Formula I: wherein A, B, D, E, G, K, L, M, Q, T, X, Y and Z are as defined herein, which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity, processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction are disclosed.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: May 19, 2015
    Assignee: ATIR Holding S.A.
    Inventors: Dmitry Tworowski, Ron Matsievitch, Vladimir Kogan
  • Publication number: 20150133453
    Abstract: Compounds of the formula I in which X, R1 and Y have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Application
    Filed: April 6, 2013
    Publication date: May 14, 2015
    Applicant: Merck Patent GmbH
    Inventors: Dieter Dorsch, Hans-Peter Buchstaller
  • Publication number: 20150111887
    Abstract: Compounds and compositions useful for treating disorders related to mutant KIT are described herein.
    Type: Application
    Filed: October 15, 2014
    Publication date: April 23, 2015
    Inventors: Brian L. Hodous, Joseph L. Kim, Kevin J. Wilson, Douglas Wilson, Yulian Zhang
  • Publication number: 20150111854
    Abstract: The present invention provides a compound having antiviral effects, particularly having growth inhibitory activity on influenza viruses, a preferred example of the compound being a substituted 3-hydroxy-4-pyridone derivative prodrug having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: December 5, 2014
    Publication date: April 23, 2015
    Inventors: Chika TAKAHASHI, Hindenori MIKAMIYAMA, Toshiyuki AKIYAMA, Kenji TOMITA, Yoshiyuki TAODA, Makoto KAWAI, Kosuke ANAN, Masayoshi MIYAGAWA, Naoyuki SUZUKI
  • Patent number: 9012454
    Abstract: This document provides methods and materials related to treating mammals (e.g., humans) having a sexual dysfunction that is refractory to treatment with a PDE V inhibitor. For example, methods and materials related to the use of an ACE inhibitor and/or an angiotensin II receptor blocker with a PDE V inhibitor to treat mammals having a sexual dysfunction (e.g., erective dysfunction) that is unresponsive to treatment with a PDE V inhibitor are provided.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: April 21, 2015
    Assignee: Mayo Foundation for Medical Education and Research
    Inventor: Frank V. Brozovich
  • Publication number: 20150099752
    Abstract: New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
    Type: Application
    Filed: April 26, 2012
    Publication date: April 9, 2015
    Applicant: ALMIRALL, SA
    Inventors: Francisco Javier Bernal Anchuela, Marta Carrascal Riera, Juan Francisco Caturla Javaloyes, Jordi Gracia Ferrer, Victor Giulio Matassa, Emma Terricabras Belart, Joan Tal Tavul Moll, Montserat Eraa Sola
  • Publication number: 20150099751
    Abstract: The in situ gel loaded with phosphodiesterase Type V (PDE5) inhibitors nanoemulsion was prepared using an innovative approach to reformulate the PDE5 inhibitors in a nanoemulsion, and then loading the nanoemulsion into an in situ gel base. These preparations are administered by intramuscular injection in order to give a depot effect for a period of time that exceeds 15 days. The in situ gel composition gives slow, controlled release of the PDE5 inhibitor. The in situ gel composition is useful for prophylaxis and treatment of some important chronic diseases, such as diabetic complications, benign prostatic hyperplasia, erectile dysfunction, and diseases associated with endothelial dysfunction.
    Type: Application
    Filed: October 7, 2013
    Publication date: April 9, 2015
    Applicant: KING ABDULAZIZ UNIVERSITY
    Inventors: HISHAM AHMED MOHAMMED MOSLI, SALAH ABDELMONEIM GHAREIB ATTEIAH, KHALED MOHAMED HOSNY OMAR, HANY MOHAMED ABD EL-MALIK EL-BASSOSSY, MOHAMED HANY ABDULWAHAB MOSILHY HELAL
  • Publication number: 20150094309
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 2, 2015
    Inventors: James H. Cook, II, Ivar M. McDonald, Dalton King, Richard E. Olson, Nenghui Wang, Christiana I. Iwuagwu, F. Christopher Zusi, John E. Macor
  • Publication number: 20150093391
    Abstract: A method of treating cancer or metastasis is provided involving administering at least one oncostatin M (OSM) antagonist to a subject, wherein the subject has been diagnosed with cancer. Administration of an OSM antagonist such as a small molecule pharmaceutical is provided as well as an anti-OSM antibody, an anti-OSM aptamer, and an OSM mRNA antagonist. The OSM antagonists were found to inhibit or prevent tumor cell detachment, proliferation and metastasis in several cancer types.
    Type: Application
    Filed: September 5, 2014
    Publication date: April 2, 2015
    Applicant: BOISE STATE UNIVERSITY
    Inventors: Cheryl Jorcyk, Dong Xu
  • Publication number: 20150087627
    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. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject.
    Type: Application
    Filed: April 15, 2014
    Publication date: March 26, 2015
    Applicant: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
  • Publication number: 20150080371
    Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-fJ[1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
    Type: Application
    Filed: December 11, 2012
    Publication date: March 19, 2015
    Inventors: Marie-Pierre Collin, Dirk Brohm, Melanie Heroult, Mario Lobell, Walter Hübsch, Klemens Lustig, Sylvia Grünewald, Ulf Bömer, Verena Vöhringer, Niels Lindner
  • Publication number: 20150080401
    Abstract: The present invention is directed to a new class of triazine derivatives as described by formula I below in which A, X, R1, R2, R3, and R4 are as defined herein and to the use of the compounds as PDE10 inhibitors.
    Type: Application
    Filed: November 21, 2014
    Publication date: March 19, 2015
    Inventors: Thomas Allen Chappie, Christopher John Helal, Bethany Lyn Kormos, Jamison Bryce Tuttle, Patrick Robert Verhoest