Plural Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 514/212.06)
  • Patent number: 11045446
    Abstract: The invention provides compounds, methods, pharmaceutical compositions, and kits for the treatment of proliferative disorders such as cancer. In one aspect, the methods comprise compounds that inhibit the activity of protein kinases, such as cell division cycle (Cdc) kinase. In another aspect, the methods comprise compounds that inhibit Cdc7 and/or Dbf4 activity. In another aspect, the methods comprise compounds that exhibit anti-proliferative properties useful in treating diseases such as cancer. Compounds useful for any of the methods include compounds of the Formula (A) or (B): or pharmaceutically acceptable salts thereof. Exemplary compounds of Formula (A) or (B) include granaticin A, granaticin B, dihydrogranaticin A, dihydrogranaticin B, medermycin, and actinorhodin.
    Type: Grant
    Filed: November 13, 2018
    Date of Patent: June 29, 2021
    Assignee: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Mark G. Frattini, Hakim Djaballah, Thomas J. Kelly
  • Patent number: 11021483
    Abstract: A method of preparing a tricyclic compound of formula (I), comprising the step of converting a compound of formula (II) into a compound of formula (III); and hydrogenating the compound of formula (III) in the presence of hydrogenation catalyst and hydrogen to form the tricyclic compound of formula (I); wherein R1 is H or a C1-3 alkyl group; and R2 is H, a halogen element or a C1-3 alkyl group.
    Type: Grant
    Filed: August 1, 2019
    Date of Patent: June 1, 2021
    Assignee: Formosa Laboratories, Inc.
    Inventors: Wen-Chieh Yang, Mei-Jing Lee, Hsueh-Chen Lee, Lung-Hsiang Li
  • Patent number: 10875870
    Abstract: Disclosed are solid state forms of Rucaparib and of Rucaparib salts, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: January 23, 2018
    Date of Patent: December 29, 2020
    Inventors: Dijana Skalec Samec, Jasna Dogan, Tomislav Biljan, Maja Matanovic Skugor, Moris Mihovilovic, Tina Mundorfer, Nikolina Janton, Mihaela Tuksar, Sara Morasi Pipercic, Nea Baus
  • Patent number: 10561647
    Abstract: Provided in the present invention are a use of quinoline derivatives for treating oesophageal cancer and a treatment method, a pharmaceutical composition and a kit thereof. The 1-[[[4-(4-fluoro-2-methyl-1H-indole-5-yl)oxy-6-methoxyquinoline-7-yl]oxy]methyl]cyclopropylamine provided by the present invention can effectively treat oesophageal cancer, and reduce the sum of the diameters of patient's target lesions.
    Type: Grant
    Filed: January 6, 2017
    Date of Patent: February 18, 2020
    Assignee: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.
    Inventors: Xunqiang Wang, Ling Yang, Zhongnan Xu, Xiangjian Wang, Wenjun Geng
  • Patent number: 10370378
    Abstract: The use of 7-chloro-3-(5-dimethylaminomethyl-[1,2,4]oxadiazol-3-yl)-5methyl-4,5-dihydro-imidazol[1,5,-a][1,4]benzodiazepine-6-one or its pharmaceutically acceptable salt for treating various types of insomnia.
    Type: Grant
    Filed: April 3, 2014
    Date of Patent: August 6, 2019
    Assignee: EVOTEC INTERNATIONAL GMBH
    Inventors: John Alan Kemp, Ian Michael Hunneyball, Timothy Tasker
  • Patent number: 10287337
    Abstract: The present invention provides compositions, and methods for local administration of certain peptides or combination with certain small molecules that produce analgesia and anti-inflammation in a mammal. Exemplary polypeptides provide peripheral analgesia and anti-inflammation when administered via local topical, subcutaneous, intradermal, or intranasal administration, to provide analgesia and anti-inflammation. Through antagonism of peripheral CGRP receptors alone, or in combination with inhibition of sensory sodium channels or anti-inflammation, the compositions of the invention provide local therapeutic pain relief with minimal undesired systemic side effects in a subject. Also provided are improved peptide delivery techniques including microneedle unit dose administering apparatus and methods.
    Type: Grant
    Filed: June 1, 2015
    Date of Patent: May 14, 2019
    Assignee: AFASCI, Inc.
    Inventors: Xinmin Xie, Conrado Pascual, Xi Xie, James Xie
  • Patent number: 10273208
    Abstract: Disclosed are methods for preparing and screening for an inhibitor of the activity of a biological molecule having a catalytic or non-catalytic cysteine residue. The methods including preparing a library of candidate inhibitor molecules by conjugating an electrophile to a plurality of drug molecules where the library of candidate inhibitor molecules thus formed react with cysteine residues. The library of candidate inhibitor molecules then may be reacted with the biological molecule to identify those inhibitor molecule that react with the catalytic or non-catalytic cysteine residue of the biological molecule in order to identify an inhibitor of the biological molecule.
    Type: Grant
    Filed: February 9, 2017
    Date of Patent: April 30, 2019
    Assignee: Northwestern University
    Inventors: Alexander V. Statsyuk, Stefan G. Kathman
  • Patent number: 10273240
    Abstract: New cortistatin compounds and pharmaceutically acceptable salts and pharmaceutically acceptable compositions thereof are provided. These compounds can be used to treat a disorder mediated by CDK8 and/or CDK19 kinase or by the Mediator Complex generally. In particular, the compounds can be used, for example, to treat a disorder such as a tumor, cancer, or a disorder associated with angiogenesis.
    Type: Grant
    Filed: November 8, 2017
    Date of Patent: April 30, 2019
    Assignee: President and Fellows of Harvard College
    Inventors: Matthew D. Shair, Henry Efrem Pelish
  • Patent number: 9827249
    Abstract: The present invention relates to arylthiazine compounds, metabolites, N-oxides, amides, esters, pharmaceutically acceptable salts, hydrates and solvates thereof and their use as cytoprotectants in the treatment or prophylaxis of diseases or states, either acute or chronic, involving aberrant cellular lipid peroxidation in the central nervous system or in the periphery of the body. The present invention also relates to a method for their preparation and to pharmaceutical composition comprising as an active ingredient one or more of the aforementioned compounds.
    Type: Grant
    Filed: May 30, 2014
    Date of Patent: November 28, 2017
    Assignee: ARANDA PHARMA LTD
    Inventors: Jari Ratilainen, Gundars Goldsteins
  • Patent number: 9586890
    Abstract: Disclosed are methods for screening for the binding affinity of chemical entities to other bioactive molecules. The screened chemical entities may be utilized in pharmaceutical composition or therapeutic methods for treating disease or disorders associated with the bioactive molecules including NEDD4-1.
    Type: Grant
    Filed: May 26, 2015
    Date of Patent: March 7, 2017
    Assignee: Northwestern University
    Inventors: Alexander V. Statsyuk, Stefan G. Kathman
  • Patent number: 9045501
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: June 2, 2015
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter R. Guzzo, David D. Manning, William Earley
  • Publication number: 20150148334
    Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: June 27, 2014
    Publication date: May 28, 2015
    Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20150140122
    Abstract: The invention relates to methods for detecting inactivation of the DNA Homologous Recombination pathway in a patient, and in particular for detecting BRCA1 inactivation.
    Type: Application
    Filed: June 6, 2013
    Publication date: May 21, 2015
    Applicant: INSERM (Institut National de la Sante et de la Rec herche)
    Inventors: Marc-Henri Stern, Elodie Manie, Tatiana Popova
  • Publication number: 20150094289
    Abstract: Provided herein are small molecules that have a neuroprotective or modulatory effect in the nervous system. The small molecules provided herein modulate dopaminergic neuronal activity. Also provided herein are methods of for the prophylaxis of or preventing the progression of Parkinson's Disease (PD).
    Type: Application
    Filed: June 3, 2013
    Publication date: April 2, 2015
    Inventors: Rudolfo Gonzalez, Ibon Garitaonandia, Ruslan Semechkin
  • Patent number: 8980837
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: March 17, 2015
    Assignee: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Patent number: 8952003
    Abstract: The present invention provides a sterol derivative or a pharmaceutically acceptable salt thereof having an activity to promote proliferation of neural stem cells. Namely, the present invention provides a sterol derivative represented by the general formula (I) (wherein Y represents optionally substituted lower alkyl or the like; Xa and Xb are the same or different, and represent a bond or the like; R1, R2, R3, R4, R7 and R8 are the same or different, and represent a hydrogen atom or the like; R5 and R6 are the same or different, and represent a hydrogen atom or the like; R9 represents a hydrogen atom or the like; R10 and R11 together represent a bond or the like; and R12 represents a hydrogen atom or the like) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 22, 2010
    Date of Patent: February 10, 2015
    Assignee: Kyowa Hakko Kirin Co., Ltd
    Inventors: Kenji Uchida, Tsutomu Agatsuma, Kazuhiro Hibino, Setsuya Sasho, Kyoichiro Iida, Hideyuki Onodera
  • Publication number: 20140314791
    Abstract: The present invention provides methods of treating cancer, particularly cancers that are null or have decreased expression or activity of the Lkb1 gene. Also included are methods of identifying therapeutic targets for the treatment of cancer.
    Type: Application
    Filed: January 4, 2013
    Publication date: October 23, 2014
    Inventors: Kwok-Kin Wong, Yan Liu
  • Publication number: 20140296201
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Application
    Filed: June 16, 2014
    Publication date: October 2, 2014
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
  • Patent number: 8846951
    Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[c]pyrrole, and octahydrocyclohepta[c]pyrrole derivatives of formula (I) wherein R1, R2, R3, R4, R5, A, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: September 30, 2014
    Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: Irini Akritopoulou-Zanze, Wilfried Braje, Stevan W. Djuric, Noel S. Wilson, Sean C. Turner, Albert W. Kruger, Ana-Lucia Relo, Shashank Shekhar, Dennie S. Welch, Hongyu Zhao, Jorge Gandarilla, Alan F. Gasiecki, Huanqiu Li, Christina M. Thompson, Min Zhang
  • Publication number: 20140275033
    Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Chiang Jia Li, Ji-Feng Liu, Wei Li, Amanda Gibeau, Harry Rogoff
  • Publication number: 20140275019
    Abstract: The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicants: Aurigene Discovery Technologies Limited, UM Pharmauji Sdn.BHD
    Inventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi, Muni Kumar Mahadari, Chandrashekar Reddy Kottam, Noorsaadah Abd Rahman, Rohana Yusof
  • Publication number: 20140256710
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R6, Y1, Y2, A1, A2, A3, and A4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: March 11, 2014
    Publication date: September 11, 2014
    Inventors: Dachun Liu, John Pratt, Le Wang, Lisa A. Hasvold, Andrew Bogdan
  • Publication number: 20140243318
    Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicant: Pfizer Inc.
    Inventors: Patricia Ann Basford, Anthony Michael Campeta, Adam Gillmore, Matthew Cameron Jones, Eleftherios Kougoulos, Suman Luthra, Robert Walton
  • Publication number: 20140234443
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: March 10, 2014
    Publication date: August 21, 2014
    Applicant: Albany Molecular Research, Inc.
    Inventors: Peter R. GUZZO, David D. MANNING, William EARLEY
  • Publication number: 20140228353
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 14, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
  • Publication number: 20140194410
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, and R6 are as described in the specification. The compounds are inhibitors of PLK and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: November 7, 2013
    Publication date: July 10, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Matthew O. Duffey, Amy M. Elder, Jianping Guo, Gang Li, Dominic Reynolds, Francois Soucy, Tricia J. Vos
  • Publication number: 20140179676
    Abstract: The invention provides a compound 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 invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: ABBVIE INC.
    Inventors: Kevin P. Cusack, Thomas D. Gordon, Michael Z. Hoemann, David C. Ihle, Bin Li, Gloria Y. Lo Schiavo, Gagandeep K. Somal, Michael Friedman, Martin E. Hayes, Wouter Iwema Bakker
  • Patent number: 8754072
    Abstract: The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: June 17, 2014
    Assignee: Pfizer Inc.
    Inventors: Patricia Ann Basford, Anthony Michael Campeta, Adam Gillmore, Matthew Cameron Jones, Eleftherios Kougoulos, Suman Luthra, Robert Walton
  • Patent number: 8729048
    Abstract: This document provides methods and materials involved in assessing responsiveness to PARP inhibitors and platinating agents. For example, methods and materials for using levels of non-homologous end-joining pathway members (e.g., artemis mRNA or polypeptide levels, Ku80 mRNA or polypeptide levels, or DNA-PKcs mRNA or polypeptide levels) to determine if cancer cells that are homologous recombination-deficient are likely to be susceptible or resistant to PARP inhibitors and platinating agents are provided.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: May 20, 2014
    Assignee: Mayo Foundation for Medical Education and Research
    Inventors: Scott H. Kaufmann, Anand G. Patel
  • Publication number: 20140128375
    Abstract: Compounds of formula I: (wherein variables A1, m, R1, R2, R3, R4 and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Application
    Filed: January 10, 2014
    Publication date: May 8, 2014
    Inventors: Ian M. Bell, Harold B. Selnick
  • Patent number: 8710047
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: April 29, 2014
    Assignee: Albany Molecular Research, Inc.
    Inventors: David D. Manning, Christopher L. Cioffi
  • Patent number: 8710046
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: June 30, 2010
    Date of Patent: April 29, 2014
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter R. Guzzo, David D. Manning, William Earley
  • Publication number: 20140107123
    Abstract: The invention relates to the treatment and prevention of type I diabetes. More specifically, the invention relates to compounds that treat or prevent the body's immune system from destroying ?-cells (i.e., insulin-producing cells in the pancreatic islets of Langerhans) by inhibition of JNK2, selective inhibition of JNK2, or inhibition of the expression of the MAPK9 gene or gene product. In one embodiment, the present invention contemplates the diagnosis, identification, production, and use of compounds which modulate MAPK9 gene expression or the activity of the MAPK9 gene product including but not limited to, JNK2, the nucleic acid encoding MAPK9 and homologues, analogues, and deletions thereof, as well as antisense, ribozyme, triple helix, antibody, and polypeptide molecules as well as small inorganic molecules. The present invention contemplates a variety of pharmaceutical formulations and routes of administration for such compounds.
    Type: Application
    Filed: August 5, 2013
    Publication date: April 17, 2014
    Applicant: University of Massachusetts
    Inventors: Roger J. Davis, Anja Jaeschke
  • Publication number: 20140045821
    Abstract: Compounds according to Formula (I), are potent inhibitors of protein kinase D (pan-PKD) activity. PKD controls key signaling cascades in cells, affecting cell proliferation, gene transcription, and protein trafficking. Accordingly, pharmaceutically acceptable compositions of the inventive compounds are candidate therapeutics for pathological conditions conditioned by changes in PKD activity.
    Type: Application
    Filed: December 8, 2011
    Publication date: February 13, 2014
    Inventors: Peter Wipf, Qiming Jan Wang
  • Publication number: 20140044802
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase and combination therapies thereof. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Application
    Filed: April 5, 2013
    Publication date: February 13, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20140030224
    Abstract: The present invention relates to methods and pharmaceutical compositions for inhibiting influenza virus replication. More particularly, the present invention relates to a compound selected from the group consisting of Gemcitabine, Obatoclax Mesylate, Docetaxel, HA-14, Alsterpaullone, GSK3B inhibitor VIII, GSK3B inhibitor XV, Indirubin 3?- monoxime, L glutathione reduced, Fluocinolone acetonide, Tirofiban, Topotecan hydrochloride, Clofarabine, Vinblastine, Menadione Crystalline and derivatives or analogues thereof for use in the treatment of an influenza infection in a subject in need thereof.
    Type: Application
    Filed: April 10, 2012
    Publication date: January 30, 2014
    Applicant: UNIVERSITÉ CLAUDE BERNARD - LYON 1
    Inventors: Vincent Lotteau, Benoit De Chassey, Patrice Andre, Laurene Meyniel-Schicklin, Anne Aublin-Gex
  • Patent number: 8637501
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: January 28, 2014
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter R. Guzzo, Matthew David Surman, James Francis Grabowski, Jr., Emily Elizabeth Freeman
  • Patent number: 8598158
    Abstract: The present invention relates to certain lactam ring-containing compounds of the Formula (I) and pharmaceutically acceptable salts thereof, wherein D, E, X1, R1, R2, R3, R4, R9, and R10 are as herein described. In addition, the invention relates to pharmaceutically acceptable compositions comprising at least one such compound, and methods of using the compounds for treating or preventing various inflammatory disorders such as rheumatoid arthritis, inflammatory bowel disease, psoriasis, asthma, and chronic obstructive pulmonary disorder.
    Type: Grant
    Filed: December 9, 2010
    Date of Patent: December 3, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dong Xiao, Anandan Palani, Robert G. Aslanian, Sylvia Degrado, Xianhai Huang, Wei Zhou, Michael Sofolarides, Xiao Chen
  • Publication number: 20130310366
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: July 12, 2013
    Publication date: November 21, 2013
    Applicant: Albany Molecular Research, Inc.
    Inventors: David D. MANNING, Christopher L. CIOFFI
  • Publication number: 20130303518
    Abstract: The invention provides a method of inhibiting the catalytic activity of a protein kinase comprising contacting said protein kinase with a compound of formula (I), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the same, and also provides a method of treating a protein kinase related disorder comprising a step of administering to a patient in need thereof a therapeutically effective amount of the compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the same, wherein each substituent in formula (I) is same as defined in the description.
    Type: Application
    Filed: September 27, 2012
    Publication date: November 14, 2013
    Applicants: Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Hansoh Pharmaceutical Co., Ltd.
    Inventors: Peng Cho Tang, Yidong Su, Yali Li, Lei Zhang, Fuqiang Zhao, Jialiang Yang, Ying Zhou, Pingyan Bie, Guangtao Qian, Minggang Ju
  • Patent number: 8569286
    Abstract: The present invention provides a compound, or a pharmaceutically acceptable salt or hydrate, and a pharmaceutical composition containing said compound, or a pharmaceutically acceptable salt or hydrate, useful as a Notch pathway signaling inhibitor for the treatment of cancer.
    Type: Grant
    Filed: July 18, 2012
    Date of Patent: October 29, 2013
    Assignee: Eli Lilly and Company
    Inventors: Philip Arthur Hipskind, Gregory Alan Stephenson
  • Publication number: 20130267498
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. 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. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: February 13, 2013
    Publication date: October 10, 2013
    Inventors: Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
  • Publication number: 20130252943
    Abstract: In one aspect, the invention relates to substituted bicyclic oxazole lactam analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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: February 27, 2013
    Publication date: September 26, 2013
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, José Manuel Bartolomé-Nebreda, Gregor James Macdonald, Susana Conde-Ceide, María Luz Martín-Martín
  • Publication number: 20130237523
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 12, 2013
    Applicant: AFFINIUM PHARMACEUTICALS, INC.
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Patent number: 8524701
    Abstract: The present invention provides the use in a pharmaceutical composition of a specific cyclic amine derivative, or its pharmaceutically acceptable salts, for the treatment of heart failure of any aetiology.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: September 3, 2013
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Brian Guth, Randolph Seidler, Juergen Daemmgen
  • Publication number: 20130224312
    Abstract: This document provides methods and materials involved in assessing responsiveness to PARP inhibitors and platinating agents. For example, methods and materials for using levels of non-homologous end-joining pathway members (e.g., artemis mRNA or polypeptide levels, Ku80 mRNA or polypeptide levels, or DNA-PKcs mRNA or polypeptide levels) to determine if cancer cells that are homologous recombination-deficient are likely to be susceptible or resistant to PARP inhibitors and platinating agents are provided.
    Type: Application
    Filed: November 16, 2012
    Publication date: August 29, 2013
    Applicant: MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCH
    Inventor: Mayo Foundation for Medical Education and Research
  • Publication number: 20130210779
    Abstract: The present invention provides means for identifying or classifying breast tumors based on the levels of nuclear cathepsin-L (CTSL) and nuclear p53 binding protein (53BP1), and methods of treating thereof.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 15, 2013
    Applicant: The Washington University
    Inventor: The Washington University
  • Patent number: 8501729
    Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: August 6, 2013
    Assignee: Albany Molecular Research, Inc.
    Inventors: David D. Manning, Christopher Lawrence Cioffi
  • Publication number: 20130115312
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Application
    Filed: November 9, 2012
    Publication date: May 9, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20130115311
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.
    Type: Application
    Filed: November 9, 2012
    Publication date: May 9, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: Vertex Pharmaceuticals Incorporated