Four Or More Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/118)
  • Patent number: 10039283
    Abstract: The present invention relates to novel substituted pyrazolyl-nicotin(thio)amide derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms, in crop protection and in the protection of materials.
    Type: Grant
    Filed: March 31, 2015
    Date of Patent: August 7, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Christophe Dubost, Cyril Montagne, Ulrike Wachendorff-Neumann, Phillipp Winter, Strphane Brunet, Jean-Pierre Vors, Pierre-Yves Coqueron, Joerg Greul
  • Patent number: 9969738
    Abstract: Novel compounds of Formula I and their use in therapeutic treatments.
    Type: Grant
    Filed: March 28, 2014
    Date of Patent: May 15, 2018
    Assignee: OGEDA SA
    Inventors: Hamid Hoveyda, Guillaume Dutheuil, Graeme Fraser
  • Patent number: 9695166
    Abstract: In one aspect this invention relates generally to compounds of Formula: and sub-formulas thereof, or a tautomer of each thereof, a pharmaceutically acceptable salt of each thereof, or a pharmaceutically acceptable solvate of each of the foregoing, where X1, L1, L3, and R3 are described herein.
    Type: Grant
    Filed: May 4, 2015
    Date of Patent: July 4, 2017
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Zhe Li, Qing Xu, Chul Yu, Calvin Yee, Stephen L. Gwaltney, II, Brian W. Metcalf, Steven Richards, Matthew A. Lardy, Lina Setti, Hing Sham
  • Patent number: 9469664
    Abstract: Oligonucleotide analogs comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: October 18, 2016
    Assignee: Sarepta Therapeutics, Inc.
    Inventors: Gunnar J. Hanson, Alexander Charles Rudolph, Bao Zhong Cai, Ming Zhou, Dwight D. Weller
  • Publication number: 20150133447
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R3, X3 to X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Application
    Filed: November 4, 2014
    Publication date: May 14, 2015
    Inventor: Harald ENGELHARDT
  • Publication number: 20150126508
    Abstract: Provided are a pteridine ketone derivative used as an EGFR, BLK, and FLT3 inhibitor and applications thereof. Specifically, provided are a compound of the following formula I, a pharmaceutical composition containing the compound of the formula I, and use of compound in preparing medicine for treating diseases mediated by EGFR, BLK, or FLT3 or inhibiting EGFR, BLK, and FLT3.
    Type: Application
    Filed: April 2, 2013
    Publication date: May 7, 2015
    Inventors: Honglin Li, Yufang Xu, Zhenjiang Zhao, Xiaofeng Liu, Wei Zhou, Fang Bai, Mengzhu Xue, Lei Zhang, Youli Zhang
  • Publication number: 20150126502
    Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 7, 2015
    Inventors: Robert A. GALEMMO, Dean R. ARTIS, Xiaocong Michael YE, Danielle Aubele, Anh TRUONG, Simeon BOWERS, Roy K. Hom, Yong-Liang ZHU, R. Jeffrey NEITZ, Jennifer SEALY, Marc ADLER, Paul BEROZA, John P. ANDERSON
  • Patent number: 9023385
    Abstract: A method of treating a patient to improve liver functioning includes providing a drug composed of at least one of pharmaceutical 2-(4-morpholinoaniline)-6-cyclohexyl aminopurine and a pharmaceutically acceptable salt thereof; and administering the drug to the patient in a manner and dosage effective to improve liver functioning. The 2-(4-morpholinoaniline)-6-cyclohexyl aminopurine can inhibit the activated hepatic stellate cells from synthesizing and expressing collagens and other extracellular matrix proteins including MMPs and TIMPs, and so it can inhibit liver fibrosis. In the liver, it can inhibit collagen synthesis and expression, and therefore reverse and treat hepatitis and liver cirrhosis effectively.
    Type: Grant
    Filed: December 2, 2013
    Date of Patent: May 5, 2015
    Assignee: Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd.
    Inventors: Ka Ho Kenneth Lee, Ruohan Chen, Zhibo Hou, Quanwei Pan
  • Publication number: 20150105382
    Abstract: The present invention relates to a purine compound useful as a kinase inhibitor.
    Type: Application
    Filed: May 7, 2014
    Publication date: April 16, 2015
    Applicant: VERASTEM, INC.
    Inventors: DiZhong Chen, Meredith Williams
  • Publication number: 20150094295
    Abstract: The present disclosure provides compounds of Formula (IA) and or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: September 6, 2013
    Publication date: April 2, 2015
    Inventors: Tim Owens, Erik Verner
  • Publication number: 20150094305
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: September 25, 2014
    Publication date: April 2, 2015
    Inventors: Donna ROMERO, Craig E. MASSE, Shaughnessy ROBINSON, Jeremy Robert GREENWOOD, Geraldine C. HARRIMAN
  • Patent number: 8993580
    Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating lipid kinases such PI3 kinases, tyrosine kinases and protein kinases such as mTOR. For example, the invention provides compounds of Formula: Also provided in the present invention are methods of using these compositions to modulate these kinases especially for therapeutic applications.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: March 31, 2015
    Assignee: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan
  • Publication number: 20150087643
    Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity; the compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
    Type: Application
    Filed: October 10, 2014
    Publication date: March 26, 2015
    Applicant: Advinus Therapeutics Private Limited
    Inventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
  • Publication number: 20150087644
    Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 26, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
  • Patent number: 8987280
    Abstract: Compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I 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: Grant
    Filed: January 29, 2009
    Date of Patent: March 24, 2015
    Assignees: Genentech, Inc., F. Hoffmann-La Roche AG
    Inventors: Jennafer Dotson, Tim Heffron, Alan Olivero, Daniel P. Sutherlin, Shumei Wang, Bing-Yan Zhu, Irina Chuckowree, Adrian Folkes, Nan Chi Wan
  • Patent number: 8987257
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.
    Type: Grant
    Filed: January 30, 2012
    Date of Patent: March 24, 2015
    Assignee: Novartis AG
    Inventors: Branko Radetich, Bing Yu, Yanyi Zhu
  • Publication number: 20150073140
    Abstract: Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.
    Type: Application
    Filed: June 6, 2014
    Publication date: March 12, 2015
    Applicant: Sarepta Therapeutics, Inc.
    Inventors: Gunnar J. Hanson, Alexander Charles Rudolph, Bao Zhong Cai, Ming Zhou, Dwight D. Weller
  • Patent number: 8969551
    Abstract: The present invention provides a useful morpholino nucleic acid derivative for synthesizing a morpholino nucleic acid oligomer. The present invention provides a compound represented by the following general formula (1) or a salt thereof. Here, R1 represents hydrogen, trityl and so on. R2 represents an amide or an imine. R3 represents a hydroxy group which may be protected by trialkylsilyl and so on, or a group represented by the following general formula (5): (wherein X represents O or S, Y represents dialkylamino or alkoxy, and Z represents chlorine).
    Type: Grant
    Filed: September 29, 2011
    Date of Patent: March 3, 2015
    Assignee: Nippon Shinyaku Co., Ltd.
    Inventor: Toshihiro Ueda
  • Publication number: 20150051202
    Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.
    Type: Application
    Filed: February 14, 2013
    Publication date: February 19, 2015
    Applicant: Merck Patent GmbH
    Inventors: Kai Schiemann, Carl Deutsch, Guenter Hoelzemann, Daniel Kuhn, Ansgar Wegener, Dominique Swinnen, Horacio Comas
  • Publication number: 20150038503
    Abstract: The present invention provides novel 6-substituted [1,2,4]triazolo[4,3-b]pyridazines that are agonists of Rev-Erb. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the activation of Rev-Erb has therapeutic effects, for instance in inflammatory and circadian rhythm-related disorders or cardiometabolic diseases.
    Type: Application
    Filed: September 27, 2012
    Publication date: February 5, 2015
    Applicant: GENFIT
    Inventors: Maryline Bourotte, Jean-Francois Delhomel, Mathieu Dubernet, Marie-Helene Gouy
  • Publication number: 20150031672
    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: Application
    Filed: October 10, 2014
    Publication date: January 29, 2015
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • Publication number: 20150025058
    Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupus
    Type: Application
    Filed: January 22, 2013
    Publication date: January 22, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Carl Deutsch, Daniel Kuhn, Tatjana Ross, Lars Burgdorf
  • Publication number: 20150018349
    Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: March 27, 2014
    Publication date: January 15, 2015
    Applicant: University of Utah Research Foundation
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
  • Publication number: 20150018336
    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Application
    Filed: December 28, 2012
    Publication date: January 15, 2015
    Inventors: Wei Chen, David J. Loury
  • Publication number: 20150011545
    Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.
    Type: Application
    Filed: July 15, 2014
    Publication date: January 8, 2015
    Applicant: AstraZeneca AB
    Inventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle Laurae LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
  • Publication number: 20140378431
    Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.
    Type: Application
    Filed: December 21, 2012
    Publication date: December 25, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Dieter Dorsch, Guenter Hoelzemann, Kai Schiemann, Ansgar Wegener
  • Patent number: 8912178
    Abstract: The 4-urea-phenyl substituted 6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine derivatives are potent and selective inhibitors of mTOR kinase and are useful in treating disorders related to abnormal mTOR activities such as cancer, immune disorders, cardiovascular disease, ocular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.
    Type: Grant
    Filed: May 18, 2011
    Date of Patent: December 16, 2014
    Assignee: Xcovery Holdings Company, LLC
    Inventor: Congxin Liang
  • Publication number: 20140364423
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: August 26, 2014
    Publication date: December 11, 2014
    Inventors: Wei-Sheng Huang, Ranny M. Thomas
  • Publication number: 20140364410
    Abstract: The present disclosure provides compounds of Formula (IA) and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: August 20, 2014
    Publication date: December 11, 2014
    Inventors: Tim OWENS, Erik VERNER
  • Publication number: 20140316132
    Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
    Type: Application
    Filed: July 1, 2014
    Publication date: October 23, 2014
    Inventors: Manoj C. Desai, Randal L. Halcomb, Paul Hrvatin, Hon Chung Hui, Ryan McFadden, Paul A. Roethle, Hong Yang
  • Patent number: 8865896
    Abstract: A method for producing adenine compound (1): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are the same or different, and hydrogen atom, or C1-6 alkyl group, or R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, piperidine, piperazine, etc., and R4 is C1-3 alkyl group, which comprises a step of reacting compound (2): and compound (3): in the presence of a boron-containing reducing agent.
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: October 21, 2014
    Assignees: Astrazeneca Aktiebolag, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Kazuki Hashimoto, Wataru Katoda, Kazuhiko Takahashi, Ayumu Kurimoto
  • Publication number: 20140303366
    Abstract: Provided is a method of treating myasthenia gravis in a patient by administering to the patient an effective amount of a skeletal muscle troponin activator, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 7, 2014
    Publication date: October 9, 2014
    Inventors: Aaron Hinken, Fady Malik, Malar Pannirselvam, Alan Russell
  • Publication number: 20140303161
    Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 9, 2013
    Publication date: October 9, 2014
    Inventor: Principia Biopharma, Inc.
  • Publication number: 20140296216
    Abstract: A compound of formula (I) or (II) and use of the compound in the preparation of drugs for treating cancer are disclosed. The study shows that the compounds can inhibit the growth of many kinds of tumor cells, can be used for targeting epidermal growth factor receptor (EGFR), and particularly can inhibit tumor cells with single or multiple mutations of EGFR (T790M). Therefore, the compound can be used as EGFR inhibitor to treat cancer and has a relatively large application value.
    Type: Application
    Filed: December 21, 2011
    Publication date: October 2, 2014
    Applicant: GUANGZHOU INSTITUTE OF BIOMEDICINE AND HEALTH, CHINESE ACADEMY OF SCIENCES
    Inventors: Ke Ding, Shaohua Chang, Shilin Xu, Lianwen Zhang, Zhengchao Tu, Jian Ding, Meiyu Geng, Yi Chen
  • Publication number: 20140296207
    Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.
    Type: Application
    Filed: June 11, 2014
    Publication date: October 2, 2014
    Inventors: Pingda REN, Yi LIU, Liansheng LI, Troy Edward WILSON
  • Publication number: 20140296233
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 2, 2014
    Applicants: Sanofi, Celgene Avilomics Research, Inc.
    Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson
  • Patent number: 8846673
    Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, (I) are useful as kinase modulators, including Btk modulation, wherein A1, A2, A3, R4 are as defined herein.
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jingwu Duan, Bin Jiang, Zhonghui Lu
  • Patent number: 8846909
    Abstract: Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: September 30, 2014
    Assignee: University of Rochester
    Inventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Torsten Wiemann, Satheesh Babu Ravula, Colin J. Loweth
  • Publication number: 20140287031
    Abstract: The present invention provides for methods and pharmaceutical compositions comprising inhibitors of mTorC1 and/or mTorC2. In some aspects, the invention provides for treatment regimens resulting in enhanced treatment efficacy and better tolerability.
    Type: Application
    Filed: November 21, 2012
    Publication date: September 25, 2014
    Applicant: INTELLIKINE, LLC
    Inventors: Yi Liu, Lynne Bui, Michael Martin, Troy Edward Wilson, Christian Rommel
  • Publication number: 20140288046
    Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: April 11, 2014
    Publication date: September 25, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Jean-Michel Adam, Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
  • Publication number: 20140275528
    Abstract: Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventors: Bertrand L. Chenard, Randall J. Gallaschun, Spencer David Kimball
  • Publication number: 20140275071
    Abstract: Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventors: Bertrand L. Chenard, Randall J. Gallaschun
  • Publication number: 20140275024
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
  • Patent number: 8835420
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3K?.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: September 16, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Edcon Chang, Wolfgang Reinhard Ludwig Notz, Michael B. Wallace
  • Patent number: 8828990
    Abstract: The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4, Y1 and Y2 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.
    Type: Grant
    Filed: November 10, 2010
    Date of Patent: September 9, 2014
    Assignee: Genentech, Inc.
    Inventors: Zhonghua Pei, Joseph P. Lyssikatos, Wendy Lee, Kirk D. Robarge
  • Publication number: 20140249147
    Abstract: Provided herein are novel substituted bicyclic aza-heterocycle sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided, are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 4, 2014
    Applicant: GlaxoSmithKline, LLC
    Inventors: Charles A. Blum, Stephanie K. Springer, Chi B. Vu
  • Publication number: 20140243523
    Abstract: A cellular model is described that targets dysregulation or inappropriate activation of the Sonic Hedgehog/Patched (SHH/PTCH) pathway. Also described, is a screening method using this cellular model to screen for pharmacological compounds that can treat or prevent skin cancer, in particular, Basal Cell Carcinoma (BCC) lesions.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 28, 2014
    Applicants: GALDERMA RESEARCH & DEVELOPMENT, CNRS
    Inventors: Elodie Burty, Thierry Magnaldo, Yannick Gache, Jérôme Aubert
  • Publication number: 20140235856
    Abstract: A cellular model is described that targets dysregulation or inappropriate activation of the Sonic Hedgehog/Patched (SHH/PTCH) pathway. Also described, is a screening method using this cellular model to screen for pharmacological compounds that can treat or prevent skin cancer, in particular, Basal Cell Carcinoma, (BCC) lesions.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 21, 2014
    Inventors: Elodie Burty, Thierry Magnaldo, Yannick Gache
  • Publication number: 20140234852
    Abstract: A cellular model is described for targeting dysregulation or inappropriate activation of the Sonic Hedgehog/Patched (SHH/PTCH) pathway. Also described, is a screening method using this cellular mod& to screen for pharmacological compounds that can treat or prevent skin cancer and, in particular, Basal Cell Carinoma (BCC) lesions.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 21, 2014
    Applicants: GALDERMA RESEARCH & DEVELOPMENT, CNRS
    Inventors: Elodie Burty, Thierry Magnaldo, Yannick Gache
  • Publication number: 20140235632
    Abstract: The present invention concerns a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, where R1-R3 and Y are defined in the description, and its use in the treatment of disorders in which pi3 kinase is implicated.
    Type: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Applicant: NOVARTIS AG
    Inventors: Graham Charles Bloomfield, Ian Bruce, Brian Cox, Lee Edwards, Judy Fox Hayler, Catherine Howsham