Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 546/82)
  • Patent number: 10874670
    Abstract: The disclosure relates to substituted fused heteroaromatic compounds and the use thereof. Specifically, the disclosure provides compounds of the following Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A1-A4, B1-B3, D1-D4 and R1-R3 are defined herein. Compounds having Formula I are kinalse inhibitors. Therefore, compounds of the disclosure may be used to treat clinical conditions caused by DDR functional defects, such as cancer.
    Type: Grant
    Filed: January 9, 2018
    Date of Patent: December 29, 2020
    Assignee: IMPACT THERAPEUTICS, INC.
    Inventors: Suixiong Cai, Ye Edward Tian
  • Patent number: 10870648
    Abstract: The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.
    Type: Grant
    Filed: June 28, 2019
    Date of Patent: December 22, 2020
    Assignee: Forma Therapeutics, Inc.
    Inventors: Shawn E. R. Schiller, Torsten Herbertz, Hongbin Li, Bradford Graves, Steven Mischke, Angela West, Jennifer R. Downing, Anna Ericsson
  • Patent number: 10745399
    Abstract: A compound of formula (IV) or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer thereof These imidazolonylquinoline compounds are useful in the inhibition, regulation and/or modulation of signal transduction by kinases, in particular ATM kinase, furthermore in pharmaceutical compositions, and in their use for the treatment of diseases which relate to ATM kinase, in particular cancer.
    Type: Grant
    Filed: March 14, 2019
    Date of Patent: August 18, 2020
    Assignee: Merck Patent GmbH
    Inventors: Thomas Fuchss, Kai Schiemann
  • Patent number: 10662193
    Abstract: The present invention relates to novel compounds that can be employed in the diagnosis, treatment, alleviation or prevention of a group of disorders and abnormalities associated with amyloid proteins and amyloid-like proteins, such as Alzheimer's disease. Precursors for the preparation of the compounds according to the present invention are also provided.
    Type: Grant
    Filed: January 21, 2015
    Date of Patent: May 26, 2020
    Assignees: AC IMMUNE SA, LIFE MOLECULAR IMAGING SA
    Inventors: Heiko Kroth, Sreenivasachary Nampally, Jér{hacek over (o)}me Molette, Emanuele Gabellieri, Pascal André René Benderitter, Wolfgang Froestl, Hanno Schieferstein, Andre Mueller, Heribert Schmitt-Willich, Mathias Berndt
  • Patent number: 10556903
    Abstract: This disclosure features compounds of Formula I, or a pharmaceutically acceptable salt thereof: in which R1, R2, R3, and R4 are as defined herein. These compounds are modulators of NLRP3, which are useful, e.g., for treating a condition, disease or disorder in which a decrease in NLRP3 activity (e.g., a condition, disease or disorder associated with repressed or impaired NLRP3 signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Grant
    Filed: April 19, 2017
    Date of Patent: February 11, 2020
    Assignee: Innate Tumor Immunity, Inc.
    Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James Olhava
  • Patent number: 10487083
    Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
    Type: Grant
    Filed: February 13, 2019
    Date of Patent: November 26, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Kevin D. Kreutter, Kristi Leonard, Michele C. Rizzolio, Russell C. Smith, Mark S. Tichenor, Aihua Wang
  • Patent number: 10364246
    Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
    Type: Grant
    Filed: January 9, 2019
    Date of Patent: July 30, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Tatiana Koudriakova, Kevin D. Kreutter, Kristi Leonard, Michele C. Rizzolio, Russell C. Smith, Mark S. Tichenor, Aihua Wang
  • Patent number: 10294226
    Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: May 21, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Tatiana Koudriakova, Kevin D. Kreutter, Kristi Leonard, Michele C. Rizzolio, Russell C. Smith, Mark S. Tichenor, Aihua Wang
  • Patent number: 10130622
    Abstract: A corrector agent capable of stabilizing a newly synthesized cystic fibrosis transmembrane conductance regulator (CFTR) protein, useful in the treatment of cystic fibrosis.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: November 20, 2018
    Assignees: AbbVie S.á.r.l., Galapagos NV
    Inventors: Rhalid Akkari, Luke Jonathan Alvey, Xavier Marie Bock, Brian S. Brown, Pieter Isabelle Roger Claes, Marlon D. Cowart, Katja E. Conrath, Douglas Cyr, Elsa De Lemos, Gert Jules Hector De Wilde, Nicolas Desroy, Béranger Duthion, Gregory A. Gfesser, Romain Luc Marie Gosmini, Christopher Gaëtan Housseman, Koen Karel Jansen, Jianguo Ji, Philip R. Kym, Jean-Michel Lefrancois, Oscar Mammoliti, Christel Jeanne Marie Menet, Nuria Merayo Merayo, Gregory John Robert Newsome, Adeline Marie Elise Palisse, Sachin V. Patel, Mathieu Rafaël Pizzonero, Anurupa Shrestha, Elizabeth C. Swift, Chris Tse, Steven Emiel Van der Plas, Xueqing Wang
  • Patent number: 10118925
    Abstract: Imidazo[4,5-c] ring compounds, (particularly imidzao[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridine compounds) having a substituted guanidine substituent at the 1-position, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are also disclosed.
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: November 6, 2018
    Assignee: 3M Innovative Properties Company
    Inventor: George W. Griesgraber
  • Patent number: 10105349
    Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.
    Type: Grant
    Filed: December 7, 2015
    Date of Patent: October 23, 2018
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Hailin Zheng, Gretchen Snyder, Lawrence P. Wennogle, Joseph Hendrick
  • Patent number: 9938275
    Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: January 23, 2017
    Date of Patent: April 10, 2018
    Assignee: 3M Innovative Properties Company
    Inventors: Doris Stoermer, Joseph F. Dellaria, Jr., David T. Amos, Bernhard M. Zimmermann, Luke T. Dressel, Jason D. Bonk, Matthew R. Radmer
  • Patent number: 9913844
    Abstract: Reversing resistance to a B-Raf inhibitor for the treatment of a proliferative disease by obtaining a tumor sample from the patient and testing it for genetic alterations in a panel of genes comprising BRAF, CRAF, CCND1, CDK4, HER2, IGF-1R, cMET, FGFR1, FGFR2, FGFR3 EGFR, MAP2K1, MAP2K2, NRAS, KRAS HRAS, PTEN, PIK3CA, and P16 and administering a drug combination therapy comprising the B-Raf inhibitor and a second inhibitor which overcomes resistance to the B-Raf inhibitor, which second inhibitor is selected based on genetic alterations discovered in the tumor sample.
    Type: Grant
    Filed: March 19, 2014
    Date of Patent: March 13, 2018
    Assignee: NOVARTIS AG
    Inventors: Giordano Caponigro, Darrin Stuart, Laure De Parseval
  • Patent number: 9873694
    Abstract: The present invention relates to a compound of Formula I: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
    Type: Grant
    Filed: October 3, 2012
    Date of Patent: January 23, 2018
    Assignee: JANUS BIOTHERAPEUTICS, INC.
    Inventors: Grayson B. Lipford, Charles M. Zepp
  • Patent number: 9598413
    Abstract: Crystalline form, Form T2H1.5-4, of N,Ndicyclopropyl-4-(1,5-dimethyl-1 Hpyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide, (Compound (I)) is provided. Also provided is a pharmaceutical composition and an oral dosage form comprising Form T2H1.5-4 of Compound (I) as well as a method of using the Form T2H1.5-4 of Compound (I) in the treatment of myeloproliferative disorders, which include polycythaemia vera, thrombocythaemia and primary myelofibrosis.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: March 21, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventor: Shella Tameze
  • Patent number: 9593117
    Abstract: Crystalline form, Form HI.5-4, of N,N-di-cyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide, (Compound I) is provided. Also provided are a pharmaceutical composition and an oral dosage form comprising Form HI.5-4 of Compound I as well as a method of using the Form HI.5-4 of Compound I in the treatment of myeloproliferative disorders, which include polycythaemia vera, thrombocythaemia and primary myelofibrosis.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: March 14, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventor: Shella Tameze
  • Patent number: 9593116
    Abstract: Crystalline form, Form T1H1.5-4, of N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl -1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide (Compound (I)) is provided. Also provided is a pharmaceutical composition and an oral dosage form comprising Form T1H1.5-4 of Compound (I) as well as a method of using the Form T1H1.5-4 of Compound for the treatment of myeloproliferative disorders, which include polycythaemia vera, thrombocythaemia and primary myelofibrosis.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: March 14, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashok Vinayak Purandare, Honghe Wan
  • Patent number: 9533997
    Abstract: The present invention relates to tricyclic heterocycles of Formula (I), which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: February 10, 2016
    Date of Patent: January 3, 2017
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Andrew P. Combs, Thomas P. Maduskuie, Jr.
  • Patent number: 9518058
    Abstract: The invention relates to an improved process for synthesizing N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide of the formula: (I) Compound (I) is currently in clinical trials for the treatment of myeloproliferative disorders, such as polycythaemia vera, thrombocythaemia and primary myelofibrosis.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: December 13, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Martin D. Eastgate, Gregory L. Beutner, Benjamin Cohen, Nicolas Cuniere, Lopa V. Desai, Monica Fitzgerald, Qi Gao, Michael Bryan Hay, Michael Joseph Lawler, Paul C. Lobben, Christopher S. Regens, Thorsten Rosner, Neil Strotman, Carolyn S. Wei, Yi Xiao, Bin Zheng, Keming Zhu
  • Patent number: 9475812
    Abstract: The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.
    Type: Grant
    Filed: June 4, 2012
    Date of Patent: October 25, 2016
    Assignee: Xuanzhu Pharma Co., Ltd.
    Inventors: Frank Wu, Yan Zhang
  • Patent number: 9376392
    Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.
    Type: Grant
    Filed: January 3, 2013
    Date of Patent: June 28, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Kerim Babaoglu, Kyla L. Bjornson, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu
  • Patent number: 9353113
    Abstract: An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. The present invention provides a compound represented by the general formula (I): (wherein definition of each group is as defined in the description) having the ENPP2 inhibitory activity, a salt thereof or a solvate thereof or a prodrug thereof, and an agent for preventing or treating urinary excretion disorder and/or improving symptoms thereof, containing them as an active ingredient.
    Type: Grant
    Filed: January 5, 2012
    Date of Patent: May 31, 2016
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Akira Ohata, Shingo Nakatani, Tetsuya Sugiyama, Takashi Morimoto
  • Patent number: 9328110
    Abstract: Imidazo ring systems substituted at the 1-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: May 3, 2016
    Assignee: 3M INNOVATIVE PROPERTIES COMPANY
    Inventors: Larry R. Krepski, Joseph F. Dellaria, Jr., Daniel E. Duffy, Matthew R. Radmer, David T. Amos
  • Patent number: 9326978
    Abstract: The claimed subject matter relates to allosteric modulation of A3 adenosine receptor (A3AR) and provides for the use of an A3 adenosine receptor modulator (A3RM), for the preparation of pharmaceutical compositions for modulating the A3AR in a subject, as well as pharmaceutical compositions including the same and therapeutic methods including administering to a subject an amount of an A3RM, the amount being effective to modulate A3AR activity. The A3RM according to claimed subject matter are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives. Also provided are 1H-Imidazo-[4,5-c]quinolin-4-amine derivatives.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: May 3, 2016
    Assignees: The United States of America, Represented by the Secretary, Dept. of Health and Human Services, Universiteit Leiden
    Inventors: Anikó Göblyös, Johannes Brussee, Adriaan P. Ijzerman, Zhan-Guo Gao, Kenneth Jacobson
  • Patent number: 9324955
    Abstract: Provided herein are organic compounds useful in a variety of OLED applications.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: April 26, 2016
    Assignee: The Trustees of Dartmouth College
    Inventors: Ivan Abrahamian, Xin Su
  • Patent number: 9284330
    Abstract: Disclosed are 1,4-dihydro-naphthyridine derivatives and pharmaceutical composition and uses thereof. The 1,4-dihydro-naphthyridine derivatives are a compound capable of inhibiting acetylcholinesterase activity and preventing extracellular calcium from flowing into a cell via a calcium channel, i.e., having a dual-activity, which are of potential importance as a pharmaceutical and can be used to prepare the drugs for treating cardiovascular diseases, cerebrovascular diseases and dementia.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: March 15, 2016
    Assignee: Jiangsu Simovay Pharmaceutical Co., Ltd.
    Inventors: Rong Chen, Lin Feng, Zhengping Zhang, Fang Fang, Qingli Dong, Fulong Li, Lei Wang, Yao Hua, Shibao Yang, Peng Wang
  • Patent number: 9273047
    Abstract: The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Grant
    Filed: September 16, 2014
    Date of Patent: March 1, 2016
    Assignee: Corcept Therapeutics, Inc.
    Inventors: Hazel Hunt, Tony Johnson, Nicholas Ray, Iain Walters
  • Patent number: 9127007
    Abstract: The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: September 8, 2015
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Bernard Matthijs Poulie, Cornelis Marius Timmers, Saskia Verkaik
  • Patent number: 9096594
    Abstract: The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3? or GSK3?) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychiatric disorders, metabolic disorders, and cancer.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: August 4, 2015
    Assignees: The Broad Institute, Inc., The General Hospital Corporation, Dana-Farber Cancer Institute, Inc.
    Inventors: Florence Fevrier Wagner, Jennifer Q. Pan, Sivaraman Dandapani, Andrew Germain, Edward Holson, Benito Munoz, Partha P. Nag, Michel Weiwer, Michael C. Lewis, Stephen J. Haggarty, Joshua A. Bishop, Kimberly Stegmaier, Versha Banerji
  • Patent number: 9045472
    Abstract: Disclosed herein are a compound of formula (I) and pharmaceutically acceptable salts thereof, processes for preparing the same, pharmaceutical compositions containing the same, and methods of using the same.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: June 2, 2015
    Assignees: ASTRAZENECA AB, SUMITOMO DAINIPPON PHARMA CO., LTD.
    Inventors: Thomas McInally, Austen Pimm
  • Publication number: 20150148341
    Abstract: The present invention provides octahydro fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Hazel Hunt, Iain Walters, Benoit Gourdet
  • Patent number: 9040706
    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 A, Q, X1, X2, Y, R1, R2, R3, R4, R4?, R5, R6 and R6? are as described herein.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: May 26, 2015
    Assignee: GENENTECH, INC.
    Inventors: Frederick Cohen, Vickie Hsiao-Wei Tsui, Cuong Ly, John A. Flygare
  • Publication number: 20150141625
    Abstract: The present invention provides IRM conjugates that includes an IRM moiety and a second active moiety covalently linked to the IRM moiety in which the covalent link does not depend on UV irradiation.
    Type: Application
    Filed: January 20, 2015
    Publication date: May 21, 2015
    Inventors: Doris Stoermer, George W. Griesgraber, James D. Mendoza, Jason D. Bonk
  • Patent number: 9034336
    Abstract: The invention provides compounds of formula I: wherein R1-R3, Ra, and Rb have any of the values defined herein, and salts thereof. The compounds have immunomodulatory properties.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: May 19, 2015
    Assignee: Regents of the University of Minnesota
    Inventors: David M. Ferguson, John Ohlfest, Courtney Aldrich
  • Patent number: 9029388
    Abstract: The present invention provides a compound having a superior PDE10A inhibitory action and use thereof. The compound is a compound represented by the following formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: May 12, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiko Taniguchi, Jun Kunitomo, Masato Yoshikawa, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Haruhi Kamisaki, Shinkichi Suzuki, Kasei Miura
  • Patent number: 9012470
    Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I in the manufacture of a medicament for the treatment of GABAA receptor associated disorders. The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: April 21, 2015
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Varsha Gupta, Joel Renick, Graeme Freestone, Alan P. Kaplan
  • Publication number: 20150105415
    Abstract: The present invention relates to the compound represented by formula (I): (wherein, all the symbols have the same meaning as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuyuki OHMOTO, Masashi KATO, Yoshifumi KAGAMIISHI, Junichiro MANAKO
  • Patent number: 9006264
    Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
    Type: Grant
    Filed: September 9, 2013
    Date of Patent: April 14, 2015
    Assignee: 3M Innovative Properties Company
    Inventors: Doris Stoermer, Joseph F. Dellaria, Jr., David T. Amos, Bernhard M. Zimmermann, Luke T. Dressel, Jason D. Bonk
  • Patent number: 9006246
    Abstract: An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. The present invention provides a compound represented by the general formula (I): (wherein definition of each group is as defined in the description) having the ENPP2 inhibitory activity, a salt thereof or a solvate thereof or a prodrug thereof, and an agent for preventing or treating urinary excretion disorder and/or improving symptoms thereof, containing them as an active ingredient.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: April 14, 2015
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Akira Ohata, Shingo Nakatani, Tetsuya Sugiyama, Takashi Morimoto
  • Patent number: 9000153
    Abstract: The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).
    Type: Grant
    Filed: July 26, 2011
    Date of Patent: April 7, 2015
    Assignee: Merck Patent GmbH
    Inventors: Thomas Fuchss, Werner Mederski, Frank Zenke
  • Patent number: 8993765
    Abstract: The present invention relates to tetrahydro-azacarboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: March 31, 2015
    Assignee: Albany Molecular Research, Inc.
    Inventors: Matthew D. Surman, Peter R. Guzzo, Emily Freeman
  • Publication number: 20150080366
    Abstract: Compounds of Formula (I) wherein n, A, R1, R2, R3 and R5 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
    Type: Application
    Filed: April 3, 2013
    Publication date: March 19, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Lee Fader, Pierre Louis Beaulieu, Murray Bailey, Francois Bilodeau, Rebekah J. Carson, André Giroux, Cédrickx Godbout, Oliver Hucke, Marc-André Joly, Mélissa Leblanc, Olivier Lepage, Benoit Moreau, Julie Naud, Martin Poirier, Elisia Villemure
  • Patent number: 8962649
    Abstract: A multidose package containing an imiquimod formulation suitable for treating topical conditions includes: a) a dispensing aperture for dispensing the formulation from the package; b) a reservoir containing sufficient formulation to provide two or more doses; c) a metered dosage element for measuring a predetermined dose of the formulation, the element including an inlet from the reservoir and an outlet to the dispensing aperture; and d) an actuating element operating the dosage element so the predetermined dose is delivered to the dispensing aperture; wherein the dose is dispensed without microbial or other contamination or degradation of the formulation in reservoir. A corresponding course of treatment for various maladies includes providing a multidose package containing an imiquimod formulation suitable for the treatment. A corresponding method of treatment of diseases with multiple doses of an imiquimod formulation includes multiple doses provided by a multidose package.
    Type: Grant
    Filed: April 1, 2010
    Date of Patent: February 24, 2015
    Assignee: iNova Pharmaceuticals (Australia) Pty Limited
    Inventors: Mark J. Hutchings, Christiaan M. Van Niekerk
  • Publication number: 20150051209
    Abstract: The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 19, 2015
    Applicant: NOVARTIS AG
    Inventors: Mark Gary BOCK, Henrik MOEBITZ, Sunil Kumar PANIGRAHI, Ramulu PODDUTOORI, Susanta SAMAJDAR
  • Publication number: 20150045374
    Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.
    Type: Application
    Filed: January 3, 2013
    Publication date: February 12, 2015
    Inventors: Kerim Babaoglu, Kyla L. Bjornson, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu
  • Patent number: 8946421
    Abstract: The compounds of the subject invention are adjuvant molecules that comprise an imidazoquinoline molecule covalently linked to a phospho- or phosphonolipid group. The compounds of the invention have been shown to be inducers of interferon-a, IL-12 and other immunostimulatory cytokines and possess an improved activity profile in comparison to known cytokine inducers when used as adjuvants for vaccine antigens.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: February 3, 2015
    Assignee: GlaxoSmithKline Biologicals S.A.
    Inventor: David A. Johnson
  • Patent number: 8946279
    Abstract: The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description.
    Type: Grant
    Filed: August 18, 2011
    Date of Patent: February 3, 2015
    Assignee: KBP Biosciences Co., Ltd.
    Inventors: Zhenhua Huang, Jinyuan Wang, Dedong Zhang
  • Publication number: 20150030540
    Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled carbazoles and derivatives thereof and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.
    Type: Application
    Filed: October 14, 2014
    Publication date: January 29, 2015
    Inventors: Anna Katrin Szardenings, Hartmuth C Kolb, Joseph C Walsh, Gang Chen, Umesh B Gangadharmath, Dhanalakshmi Kasi, Changhui Liu, Anjana Sinha, Eric Wang, Chul Yu, Wei Zhang, Kai Chen, Vani P Mocharla, Peter J. H. Scott
  • Publication number: 20150023990
    Abstract: Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
    Type: Application
    Filed: September 30, 2014
    Publication date: January 22, 2015
    Inventors: Kyle J. Lindstrom, Bryon A. Merrill, Chad A. Haraldson, Michael J. Rice, Tushar A. Kshirsagar, Philip D. Heppner, Joshua R. Wurst, Shri Niwas, Sarah J. Slania
  • Patent number: 8932557
    Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled carbazoles and derivatives thereof and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: January 13, 2015
    Assignee: Eli Lilly and Company
    Inventors: Gang Chen, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Anjana Sinha, Wei Zhang, Kai Chen, Vani P. Mocharla