Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/228.2)
  • Patent number: 10335380
    Abstract: The present findings point to mutant HSCs as the cause of BM neuroglial damage that compromises MSC survival and function, critically contributing to MPN pathogenesis. In this sense, the present invention shows that the niche damage triggered by the mutant HSC is essential for the development of a haematopoietic malignancy previously considered to be caused by the HSC alone. Targeting HSC niche-forming MSCs and their neural regulation paves the way to more efficient therapeutic strategies in MPN. For this purpose, the present invention shows that an efficient therapeutic strategy for the treatment of MPN lies on the administration of neuroprotective compounds, such as 4-methylcatechol, capable of protecting BM sympathetic nerve fibers. Additionally, another efficient therapeutic strategy is shown herein as the administration of selective ?3-adrenergic agonists such as BRL37344 or Mirabegron, since this strategy will compensate for deficient sympathetic stimulation of nestin+ MSCs.
    Type: Grant
    Filed: May 12, 2014
    Date of Patent: July 2, 2019
    Assignee: CNIC Fundacion Centro Nacional De Investigaciones Cardiovasculares Carlos III
    Inventors: Simon Mendez Ferrer, Lorena Arranz Salas, Joan Isern Marin
  • Patent number: 10294205
    Abstract: There is provided a compound of formula I, having the structure: wherein R1 to R5 have the meanings given in the description.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: May 21, 2019
    Assignee: Nanyang Technological University
    Inventors: Ata Abbas, Teck Peng Loh, Bengang Xing
  • Patent number: 10292974
    Abstract: The present invention provides a prophylactic or therapeutic agent for giant cell tumors occurring in a bone and soft tissue or for chondrosarcoma, which comprises a non-steroidal anti-inflammatory agent or thiazolidine derivative as an active ingredient, and the like.
    Type: Grant
    Filed: March 18, 2013
    Date of Patent: May 21, 2019
    Assignee: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Akihiko Takeuchi, Hiroyuki Tsuchiya
  • Patent number: 10154990
    Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R5 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.
    Type: Grant
    Filed: December 29, 2015
    Date of Patent: December 18, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John Edward Park, Gerald Juergen Roth, Armin Heckel, Nveed Chaudhary, Trixi Brandl, Georg Dahmann, Matthias Grauert
  • Patent number: 10111884
    Abstract: The present invention provides compositions and methods for treating, preventing, and inhibiting viral replication, viral infections and viral diseases and disorders, comprising the use of artemisinin derivatives having anti-viral activity.
    Type: Grant
    Filed: November 25, 2016
    Date of Patent: October 30, 2018
    Assignees: Hadasit Medical Research Services and Development Ltd., The Hong Kong University of Science and Technology
    Inventors: Richard K. Haynes, Dana G. Wolf
  • Patent number: 10112954
    Abstract: The present invention relates to a novel bicyclic heteroaryl derivative, a pharmaceutically acceptable salt thereof, a hydrate thereof, and a solvate thereof having an improved inhibitory activity for protein kinases, and a pharmaceutical composition for preventing or treating an abnormal cell growth disorder comprising same as an active ingredient.
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: October 30, 2018
    Assignees: HANMI PHARM. CO., LTD., HANMI SCIENCE CO., LTD.
    Inventors: Seung Hyun Jung, Young Hee Jung, Wha Il Choi, Jung Beom Son, Eun Ju Jeon, In Ho Yang, Tae Hun Song, Mi Kyoung Lee, Myoung Sil Ko, Young Gil Ahn, Maeng Sup Kim, Young Jin Ham, Tae Bo Sim, Hwan Geun Choi, Jung Mi Hah, Dong-sik Park, Hwan Kim
  • Patent number: 10000451
    Abstract: The invention provides mitogen-activated protein kinase kinase kinase kinase 4 (MAP4K4) inhibitors, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant diminution of tumor cell growth, cancer or metastasis.
    Type: Grant
    Filed: July 15, 2017
    Date of Patent: June 19, 2018
    Assignee: SRI International
    Inventors: Ling Jong, Chih-Tsung Chang, Jaehyeon Park
  • Patent number: 9879016
    Abstract: The disclosure provides compounds of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the disclosure are useful for treating immunological and oncological conditions.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: January 30, 2018
    Assignee: AbbVie Inc.
    Inventors: Eric Breinlinger, Andrew Burchat, Justin Dietrich, Michael Friedman, David Ihle, David Kinsman, Kelly Mullen, Augustine Osuma, Anil Vasudevan, Noel Wilson
  • Patent number: 9802915
    Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR4 or N; R1, R2, R3, R4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Grant
    Filed: November 17, 2016
    Date of Patent: October 31, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Qingjie Liu, Scott Hunter Watterson, Saleem Ahmad, Andrew J. Tebben
  • Patent number: 9682930
    Abstract: A compound of formula (I) R-L-CO—X??(I) (wherein R is a C10-24 unsaturated hydrocarbon group optionally interrupted by one or more heteroatoms or groups of heteroatoms selected from S, O, N, SO, SO2, said hydrocarbon group comprising at least 4 non-conjugated double bonds; L is a linking group forming a bridge of 1 to 5 atoms between the R group and the carbonyl CO; and X is an electron withdrawing group) for use in the treatment of rheumatoid arthritis.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: June 20, 2017
    Assignee: Avexxin AS
    Inventors: Astrid Jullumstro Feuerherm, Berit Johansen
  • Patent number: 9662325
    Abstract: The invention provides methods of attenuating, e.g., inhibiting or reducing, cellular proliferation and migration, particularly endothelial cell proliferation and migration, including that associated with angiogenesis, using opioid antagonists, including, but not limited to, those that are peripherally restricted antagonists.
    Type: Grant
    Filed: May 30, 2014
    Date of Patent: May 30, 2017
    Assignee: THE UNIVERSITY OF CHICAGO
    Inventors: Jonathan Moss, Mark Lingen, Patrick A. Singleton, Joe G. N. Garcia, Chun-Su Yuan
  • Patent number: 9566281
    Abstract: The present invention relates to MEK inhibitors that are capable of displaying one or more beneficial therapeutic effects. The MEK inhibitors can be used in the prevention and/or treatment of viral infection. MEK inhibitors in combination with neuraminidase inhibitor compounds are capable of displaying one or more beneficial therapeutic effects in the treatment of viral diseases.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: February 14, 2017
    Assignee: ATRIVA THERAPEUTICS GmbH
    Inventors: Stephan Pleschka, Oliver Planz, Stephan Ludwig
  • Patent number: 9532493
    Abstract: A surface treating composition for copper or a copper alloy comprising an imidazole compound and means for using the composition in the soldering of electronic parts to printed wiring boards are disclosed.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: December 27, 2016
    Assignee: SHIKOKU CHEMICALS CORPORATION
    Inventors: Hirohiko Hirao, Noriaki Yamaji, Masato Nakanishi, Takayuki Murai
  • Patent number: 9512086
    Abstract: The present invention provides a compound of Formula (I) and a salt thereof, wherein, m is an integer of 2 to 7, and R is independently at least one selected from the group consisting of hydrogen and C1-C20 alkyl. The compound promotes apoptosis in cancer cell and inhibits its growth. The present invention also provides a pharmaceutical composition which comprises the compound of Formula (I), a salt thereof and a pharmaceutically acceptable carrier. The present invention further provides a method for production of the pharmaceutical composition used for treating cancer.
    Type: Grant
    Filed: January 14, 2015
    Date of Patent: December 6, 2016
    Assignee: National Chiao Tung University
    Inventors: Jui-I Chao, Su-Pei Wang, Chinpiao Chen, Kai-Hao Yin, Jinn-Moon Yang, Ya-Hui Wu
  • Patent number: 9493478
    Abstract: The present invention provides a fused ring compound containing furan or a pharmaceutically acceptable salt thereof, a method for preparing same, a pharmaceutical composition comprising same, and a use thereof. The fused ring compound containing furan or a pharmaceutically acceptable salt thereof inhibits the activity of phosphatidylinositol 3-kinase (PI3K) and can therefore be used in a pharmaceutical composition for treating and preventing respiratory diseases, inflammatory diseases, proliferative diseases, cardiovascular diseases, or central nervous system diseases which occur due to the over-activation of PI3K.
    Type: Grant
    Filed: July 23, 2013
    Date of Patent: November 15, 2016
    Assignee: YUHAN CORPORATION
    Inventors: Hyoung Sig Seo, Tae Kyun Kim, Hyun Joo Lee, Dong Hoon Kim, Gyu Jin Lee, Jun Chul Park, Ji Yeong Gal, Tae-hoon Kim, Kwan Hoon Hyun, Kyoung Kyu Ahn, Kaapjoo Park, Su Youn Nam, Ge Hyeong Lee, Hee Jong Lim
  • Patent number: 9434711
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: September 6, 2016
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Shawn T Branum, Raymond W Colburn, Scott L Dax, Christopher M Flores, Michele C Jetter, Yi Liu, Donald Ludovici, Mark J Macielag, Jay M Matthews, James J McNally, Laura M Andraka, Ronald K Russell, Ning Qin, Christopher Teleha, Kenneth M Wells, Scott C Youells, Mark A Youngman
  • Patent number: 9359373
    Abstract: Novel N-substituted norcantharimide derivatives are disclosed herein. The novel N-substituted norcantharimide derivatives are useful as lead compounds for manufacturing a medicament or a pharmaceutical composition for treating cancer, particularly for treating leukemia.
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: June 7, 2016
    Assignees: TAIPEI VETERANS GENERAL HOSPITAL, NATIONAL CHIAYI UNIVERSITY, MACKAY MEMORIAL HOSPITAL
    Inventors: Cheng-Deng Kuo, Yu-Jen Chen, Jin-Yi Wu, Hui-Fen Liao
  • Patent number: 9353122
    Abstract: Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.
    Type: Grant
    Filed: February 14, 2014
    Date of Patent: May 31, 2016
    Assignee: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, Ben C. Askew, Jinsoo Kim
  • Patent number: 9340528
    Abstract: The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: May 17, 2016
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Benjamin Bader, Ulf Bömer, Stuart Ince, Marcus Koppitz, Philip Lienau, Tobias Marquardt, Duy Nguyen, Stefan Prechtl, Gerhard Siemeister, Christof Wegscheid-Gerlach
  • Patent number: 9187458
    Abstract: Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2, R3 and R4 are each as defined in the present application.
    Type: Grant
    Filed: June 8, 2011
    Date of Patent: November 17, 2015
    Assignee: Tianjin Hemay Bio-Tech Co., LTD.
    Inventors: Hesheng Zhang, Yingwei Chen, Qingchao He
  • Patent number: 9115059
    Abstract: The invention relates to novel chemical compounds, in particular oxime derivatives of 3,5-seco-4-nor-cholestane, to the application thereof as drugs, in particular cytoprotective drugs, and more particularly as neuroprotective, cardioprotective and/or hepatoprotective drugs.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: August 25, 2015
    Assignee: TROPHOS
    Inventors: Cyrille Drouot, Abdesslame Nazih, Corinne Chaimbault
  • Patent number: 9051315
    Abstract: Compounds that inhibit protein kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.
    Type: Grant
    Filed: October 18, 2010
    Date of Patent: June 9, 2015
    Assignee: AbbVie Inc.
    Inventors: Nwe Y. Ba-maung, Richard F. Clark, Scott A. Erickson, Steve D. Fidanze, Megumi Kawai, Robert A. Mantei, George S. Sheppard, Bryan K. Sorensen, Gary T. Wang
  • Publication number: 20150148331
    Abstract: A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease.
    Type: Application
    Filed: July 24, 2014
    Publication date: May 28, 2015
    Inventors: Esther Birtalan, Peter Hoelig, David J. Lindley, Yeshwant D. Sanzgiri, Ping Tong
  • Publication number: 20150148311
    Abstract: Compounds having the following structure (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or prodrug thereof, wherein R1, R2, R3, R4, R8, R9, R10, R11, R12, A1, A2, X, Y and Z are as defined herein. Uses of such compounds as TGR5 antagonists and for treatment of various indications, including Type II diabetes meletus are also provided.
    Type: Application
    Filed: June 20, 2014
    Publication date: May 28, 2015
    Inventors: Jason G. Lewis, Nicholas Reich, Tao Chen, Jeffrey W. Jacobs, Dominique Charmot, Marc Navre, Patricia Finn, Christopher Carreras, Andrew Spencer
  • Publication number: 20150148329
    Abstract: Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1A2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.
    Type: Application
    Filed: June 24, 2013
    Publication date: May 28, 2015
    Inventors: Allen B. Reitz, Garry Robert Smith
  • Patent number: 9040050
    Abstract: The invention relates to novel method for the treatment of cancer using a combination therapy comprising an antibody that binds CD38, a corticosteroid and a non-corticosteroid chemotherapeutic agent.
    Type: Grant
    Filed: September 26, 2007
    Date of Patent: May 26, 2015
    Assignee: GENMAB A/S
    Inventors: Jan Van De Winkel, Paul Parren, Yvo Graus, Judith Oprins, Michel De Weers, Martine Van Vugt, Ole Baadsgaard, Steen Lisby
  • Publication number: 20150141406
    Abstract: The present invention provides a compound having a superior JAK inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: May 31, 2013
    Publication date: May 21, 2015
    Inventors: Hiroshi Nara, Masaki Daini, Akira Kaieda, Taku Kamei, Toshihiro Imaeda, Fumiaki Kikuchi
  • Patent number: 9034869
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: May 19, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Publication number: 20150133427
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: October 15, 2014
    Publication date: May 14, 2015
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Michael John Munchhof, Lei Jin
  • Publication number: 20150133439
    Abstract: The Present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.
    Type: Application
    Filed: July 9, 2014
    Publication date: May 14, 2015
    Inventors: Anjali Pandey, Robert M. Scarborough, Kenji Matsuno, Michio Ichimura, Yuji Nomoto, Shinichi Ide, Eiji Tsukuda, Junko Sasaki, Shoji Oda
  • Publication number: 20150119387
    Abstract: The present invention relates to a compound having the structure of Formula I as inhibitor of WNT signal transduction pathways, as well as a composition comprising the compound. Further, the present invention relates to the use of the compound and the method of inhibiting the WNT signal transduction pathways.
    Type: Application
    Filed: June 15, 2012
    Publication date: April 30, 2015
    Applicant: Curegenix Inc.
    Inventor: Songzhou An
  • Publication number: 20150119385
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.
    Type: Application
    Filed: October 24, 2014
    Publication date: April 30, 2015
    Applicant: Novartis AG
    Inventors: Nicole Buschmann, Robin Alec Fairhurst, Pascal Furet, Thomas Knöpfel, Catherine Leblanc, Lv Liao, Robert Mah, Pierre Nimsgern, Sebastien Ripoche, Jing Xiong, Bo Han, Can Wang, Xianglin Zhao
  • Publication number: 20150105380
    Abstract: The present invention provides methods for treating polycystic kidney disease by administering a compound or pharmaceutical composition thereof having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein.
    Type: Application
    Filed: September 23, 2014
    Publication date: April 16, 2015
    Applicant: ANGION BIOMEDICA CORP.
    Inventors: Prakash NARAYAN, Brian HUANG, Prani PAKA, Latha PAKA, Itzhak D. GOLDBERG
  • Patent number: 9006442
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: April 14, 2015
    Assignee: Lupin Limited
    Inventors: Sanjeev Anant Kulkarni, Sachin Madan, Nirmal Kumar Jana, Prashant Vitthalrao Tale, Narasimha Murthy Cheemala, Sachin Jaysing Mahangare, Prashant Popatrao Vidhate, Chaitanya Prabhakar Kulkarni, Sapana Suresh Patel, Amolsing Dattu Patil, Seema Prabhakar Zade, Rohan Mahadev Shinde, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150099731
    Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 me
    Type: Application
    Filed: May 5, 2014
    Publication date: April 9, 2015
    Applicant: University of Kentucky
    Inventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
  • Patent number: 8999977
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic [4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: April 7, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Patent number: 8999978
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: April 7, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sundeep Dugar, Sarvajit Chakravarty
  • Patent number: 8993561
    Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.
    Type: Grant
    Filed: November 18, 2011
    Date of Patent: March 31, 2015
    Assignee: Sanofi
    Inventor: Alain Pellet
  • 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
  • Patent number: 8981131
    Abstract: The present invention provides compounds represented by formula I: wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: March 17, 2015
    Assignee: Piramal Enterprises Limited
    Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Roda Dalal, Sapna Parikh, Aditi Amol Tannu
  • Publication number: 20150072978
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.
    Type: Application
    Filed: November 17, 2014
    Publication date: March 12, 2015
    Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew J. Souers
  • Publication number: 20150065492
    Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
    Type: Application
    Filed: June 10, 2014
    Publication date: March 5, 2015
    Inventors: Peter Dragovich, Douglas E. Murphy
  • Publication number: 20150065494
    Abstract: The present invention provides an aminostyrylbenzofuran compound of Formula (I), and a pharmaceutical composition comprising same. The pharmaceutical composition of the present invention comprising the compound of Formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof as an active ingredient can be useful for the prevention and treatment of degenerative brain diseases caused by accumulation of beta-amyloid.
    Type: Application
    Filed: April 1, 2013
    Publication date: March 5, 2015
    Inventors: Dong Jin Kim, Kyung Ho Yoo, Young Soo Kim, Woong Seo Park, Yong Koo Kang, Hye Yun Kim, Yun Kyung Kim, Ki Duk Park, Maeng Sup Kim, Kwee Hyun Suh, Young Gil Ahn
  • Publication number: 20150065495
    Abstract: The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (“LSD1”). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions.
    Type: Application
    Filed: August 28, 2014
    Publication date: March 5, 2015
    Applicant: UNIVERSITY OF UTAH
    Inventors: Hariprasad Vankayalapati, Sunil Sharma, Venkataswamy Sorna
  • Publication number: 20150051189
    Abstract: Compounds of formula (I): wherein Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Application
    Filed: January 23, 2013
    Publication date: February 19, 2015
    Inventors: Thierry Le Diguarher, Patrick Casara, Jérôme-Benoît Starck, Jean-Michel Henlin, James Edward Paul Davidson, James Brooke Murray, Christopher John Graham, I-Jen Chen, Olivier Geneste, John Hickman, Stéphane Depil, Arnaud Le Tiran, Miklos Nyerges, Guillaume De Nanteuil
  • Patent number: 8957069
    Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R3 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, wherein R2 and R3 do not exist when carbon atoms respectively adjacent to R2: and R3 form a double bond, and there is n
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: February 17, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
  • Publication number: 20150045354
    Abstract: The present invention relates to a novel class of quinolone-4-carboxamide Pf3D7 inhibitors of general formula (I) (Formula (I)) wherein R1, R2, R3, R4, R5, R6, R7, R8 and X are as defined herein, to their use in medicine, and in the treatment of malaria in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.
    Type: Application
    Filed: March 14, 2013
    Publication date: February 12, 2015
    Inventors: Ian Hugh Gilbert, Neil Norcross, Beatriz Baragana Ruibal, Achim Porzelle
  • Publication number: 20150038486
    Abstract: Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae IA, IB, and IC, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.
    Type: Application
    Filed: July 7, 2014
    Publication date: February 5, 2015
    Inventors: Gordon William Rewcastle, Swarnalatha Akuratiya Gamage, Jack Urquhart Flanagan, Anna Claire Giddens, Kit Yee Tsang
  • Publication number: 20150038501
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Inventors: Leping LI, Min ZHONG
  • Publication number: 20150038500
    Abstract: The invention relates to a pharmaceutical composition for preventing or treating an ophthalmologic disease comprising a compound of formula (1) as defined in the specification, or a pharmaceutically acceptable salt or isomer thereof as an active ingredient. Also, the invention relates to a composition for cleansing or preserving a contact lens comprising the above active ingredient.
    Type: Application
    Filed: November 9, 2012
    Publication date: February 5, 2015
    Inventors: In-Beom Kim, Muyan Kim, Sung Won Jung, Eojin Jeong, Sooyeon Sim