Three Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 514/211.1)
  • Patent number: 11912693
    Abstract: The present embodiments are directed, in part, to compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof for modulating the activity of S1P1 receptor and methods of using the same.
    Type: Grant
    Filed: June 12, 2018
    Date of Patent: February 27, 2024
    Assignee: TREVENA, INC.
    Inventors: Philip Michael Pitis, Robert Eugene Boyd, Tamara Ann Miskowski Daubert, Michael John Hawkins, Guodong Liu, Aimee Crombie Speerschneider
  • Patent number: 11884682
    Abstract: The present invention provides compounds of Formula I which can be used as macrophage migration inhibitory factor (MIF) inhibitors; methods for the production of the compounds of the invention; pharmaceutical compositions comprising the compounds of the invention; as well as uses and methods for treating a disease mediated by MIF by administering the compounds of the invention.
    Type: Grant
    Filed: June 23, 2020
    Date of Patent: January 30, 2024
    Assignee: NANJING IMMUNOPHAGE BIOTECH CO., LTD.
    Inventors: Guohuang Fan, Kin Chiu Fong, Hongyu Yang, Jianfei Wang
  • Patent number: 11732006
    Abstract: The present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.
    Type: Grant
    Filed: March 19, 2021
    Date of Patent: August 22, 2023
    Assignee: Albireo AB
    Inventors: Per-Göran Gillberg, Hans Graffner, Ingemar Starke
  • Patent number: 11554103
    Abstract: Provided herein are compositions and methods to reduce toxicity resulting from pharmaceutical treatment, that can lead to increased risk of developing Parkinson's disease (PD) and/or acceleration of PD-associated deterioration.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: January 17, 2023
    Assignee: Northwestern University
    Inventors: Dalton James Surmeier, Jr., Steven M. Graves
  • Patent number: 11427580
    Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein A, G, R1, R5, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: December 18, 2018
    Date of Patent: August 30, 2022
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, Dharmpal S. Dodd, Sreekantha Ratna Kumar, Durga Buchi Raju Barre, Srinivasan Kunchithapatham Duraisamy
  • Patent number: 11357748
    Abstract: A method is provided for treating a Mendelian disorder of the epigenetic machinery in a subject in need thereof. In particular, the method comprises administering a therapeutically effective amount of an agent that restores balance between open and closed chromatin states at one or more target genes, wherein the agent that restores balance between open and closed chromatin states at one or more target genes is an agent that ameliorates the effect of a defective gene encoding a component of the epigenetic machinery.
    Type: Grant
    Filed: May 29, 2015
    Date of Patent: June 14, 2022
    Assignee: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Hans Tomas Bjornsson, Harry Dietz
  • Patent number: 11267794
    Abstract: The invention relates to certain 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives as defined herein. These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.
    Type: Grant
    Filed: January 8, 2021
    Date of Patent: March 8, 2022
    Assignee: Albireo AB
    Inventors: Per-Göran Gillberg, Ingemar Starke, Santosh S. Kulkarni
  • Patent number: 11225483
    Abstract: Disclosed are compounds, pharmaceutical compositions, and methods of treatment. The disclosed compounds are based on fused 1,4-diazepine and pyrrolidinedione scaffolds.
    Type: Grant
    Filed: March 7, 2019
    Date of Patent: January 18, 2022
    Assignee: Northwestern University
    Inventors: Gary E. Schiltz, Karl A. Scheidt
  • Patent number: 11186589
    Abstract: The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-?B-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
    Type: Grant
    Filed: February 6, 2020
    Date of Patent: November 30, 2021
    Assignee: Janssen Pharmaceutica NV
    Inventors: Ian Stansfield, Olivier Alexis Georges Querolle, Yannick Aime Eddy Ligny, Gerhard Max Gross, Edgar Jacoby, Lieven Meerpoel, Simon Richard Green, George Hynd, Janusz Jozef Kulagowski, Calum Macleod, Samuel Edward Mann
  • Patent number: 11180465
    Abstract: The invention relates to 1,5-benzothiazepine and 1,2,5-benzothiadiazepine derivatives of formula (I). These compounds are bile acid modulators having apical sodium-dependent bile acid transporter (ASBT) and/or liver bile acid transport (LBAT) inhibitory activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment of cardiovascular diseases, fatty acid metabolism and glucose utilization disorders, gastrointestinal diseases and liver diseases.
    Type: Grant
    Filed: January 8, 2021
    Date of Patent: November 23, 2021
    Assignee: Albireo AB
    Inventors: Per-Göran Gillberg, Ingemar Starke, Santosh S. Kulkarni
  • Patent number: 10851091
    Abstract: Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
    Type: Grant
    Filed: September 24, 2018
    Date of Patent: December 1, 2020
    Assignee: Genentech, Inc.
    Inventors: Marie-Gabrielle Braun, Emily Hanan, Steven T. Staben, Robert Andrew Heald, Calum Macleod, Richard Elliott
  • Patent number: 10799500
    Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the ?-opioid receptor.
    Type: Grant
    Filed: February 14, 2019
    Date of Patent: October 13, 2020
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Wei Yao, Peng Li, Robert Davis, Sharon Mates, Kimberly Vanover, Gretchen Snyder
  • Patent number: 10576166
    Abstract: Disclosed herein are compositions and methods of modulating the expression of gene or the production of a protein by transfecting target cells with nucleic acids. The compositions disclosed herein demonstrate a high transfection efficacy and are capable of ameliorating diseases associated with protein or enzyme deficiencies.
    Type: Grant
    Filed: April 6, 2016
    Date of Patent: March 3, 2020
    Assignee: Translate Bio, Inc.
    Inventors: Frank DeRosa, Michael Heartlein
  • Patent number: 10508108
    Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is —C(R1)? or —N?; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: December 17, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christian Fischer, Stephane L. Bogen, Matthew L. Childers, Francesc Xavier Fradera Llinas, J. Michael Ellis, Sara Esposite, Dawn M. Hoffman, Chunhui Huang, Solomon D. Kattar, Alexander J. Kim, John W. Lampe, Michelle R. Machacek, Daniel R. McMasters, Dann L. Parker, Jr., Michael H. Reutershan, Nunzio Sciammetta, Pengcheng P. Shao, David L. Sloman, Wanying Sun, Feroze Ujjainwalla, Zhicai Wu, Yang Yu, Craig R. Gibeau
  • Patent number: 10494351
    Abstract: The present invention relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: September 18, 2018
    Date of Patent: December 3, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin
  • Patent number: 10479772
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: December 14, 2018
    Date of Patent: November 19, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin
  • Patent number: 10464909
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: December 13, 2018
    Date of Patent: November 5, 2019
    Assignee: Forma Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Heather Davis, Aleksandra Rudnitskaya, David R. Lancia, Jr., Kenneth W. Bair, David S. Millan, Matthew W. Martin
  • Patent number: 10414738
    Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: December 12, 2018
    Date of Patent: September 17, 2019
    Assignee: Forma Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., David S. Millan, Matthew W. Martin, Kenneth W. Bair
  • Patent number: 10138255
    Abstract: The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
    Type: Grant
    Filed: March 6, 2015
    Date of Patent: November 27, 2018
    Assignees: Merck Sharp & Dohme Corp., MSD R&D (China) Co., Ltd.
    Inventors: Peter D. Williams, John A. McCauley, Christopher J. Bungard, David Jonathan Bennett, Sherman T. Waddell, Gregori J. Morriello, Lehua Chang, Michael P. Dwyer, M. Katharine Holloway, Alejandro Crespo, Xin-Jie Chu, Catherine Wiscount, H. Marie Loughran, Jesse J. Manikowski, Jurgen Schulz, Kartik M. Keertikar, Bin Hu, Bin Zhong, Tao Ji
  • Patent number: 10112932
    Abstract: Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation. Also described are methods of making the benzoxazepin oxazolidinone compounds having the Formula I structure.
    Type: Grant
    Filed: October 10, 2017
    Date of Patent: October 30, 2018
    Assignee: Genentech, Inc.
    Inventors: Marie-Gabrielle Braun, Emily Hanan, Steven T. Staben, Robert Andrew Heald, Calum MacLeod, Richard Elliott
  • Patent number: 9938269
    Abstract: The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: April 10, 2018
    Assignees: ABBVIE INC., ABBVIE DEUTSCHLAND GMBH & CO KG
    Inventors: Hervé Geneste, Michael Ochse, Karla Drescher, Berthold Behl, Loic Laplanche, Jürgen Dinges, Clarissa Jakob, Katja Jantos
  • Patent number: 9867833
    Abstract: Compounds having the formula I wherein R1, X1, X2, X3 and X4 as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
    Type: Grant
    Filed: December 3, 2014
    Date of Patent: January 16, 2018
    Assignee: GENENTECH, INC.
    Inventors: Aleksandr Kolesnikov, Steven Do
  • Patent number: 9598435
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: March 21, 2017
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Michael Graupe, Juan Guerrero, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Chandrasekar Venkataramani, Jeff Zablocki
  • Patent number: 9512140
    Abstract: A dual H1 inverse agonist/5-HT2A receptor antagonist of the formula: its uses, and methods for its preparation are described.
    Type: Grant
    Filed: August 22, 2012
    Date of Patent: December 6, 2016
    Assignee: Eli Lilly and Company
    Inventor: Andrew James Ledgard
  • Patent number: 9481688
    Abstract: A dual H1/5-HT2A receptor antagonist of the formula: its uses, and methods for its preparation are described.
    Type: Grant
    Filed: July 2, 2012
    Date of Patent: November 1, 2016
    Assignee: Eli Lilly and Company
    Inventor: Andrew James Ledgard
  • Patent number: 9481690
    Abstract: The present invention relates to crystalline polymorphs of (2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide (GDC-0032, taselisib), methods of use, and processes of preparing thereof.
    Type: Grant
    Filed: January 8, 2016
    Date of Patent: November 1, 2016
    Assignee: Genentech, Inc.
    Inventors: Jeffrey Stults, Travis Remarchuk, Frederic St-Jean
  • Patent number: 9458176
    Abstract: A compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof works as an mGluR2 antagonist, and is applicable as a therapeutic agent for neurological disorders related to glutamate dysfunction and diseases involving the mGluR2, such as Alzheimer's disease: wherein R is a hydrogen atom, a C1-6 alkyl group or the like, R1 is a C1-6 alkyl group, a C1-6 alkoxy group or the like, R2 is a halogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or the like, R3 is a hydrogen atom, a C1-6 alkyl group or the like, and R4 is a C1-6 alkyl group or the like.
    Type: Grant
    Filed: February 26, 2014
    Date of Patent: October 4, 2016
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Mamoru Takaishi, Nobuhiro Sato, Tomoyuki Shibuguchi, Takafumi Motoki, Yoshinori Takahashi, Takeo Sasaki, Alan Braunton
  • Patent number: 9434747
    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: Grant
    Filed: February 17, 2012
    Date of Patent: September 6, 2016
    Assignee: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty
  • Patent number: 9346824
    Abstract: The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
    Type: Grant
    Filed: April 4, 2014
    Date of Patent: May 24, 2016
    Assignee: Hoffman-La Roche, Inc.
    Inventors: Cosimo Dolente, Patrick Schnider
  • Patent number: 9321718
    Abstract: The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
    Type: Grant
    Filed: June 10, 2011
    Date of Patent: April 26, 2016
    Assignee: CHROMA THERAPEUTICS LTD.
    Inventors: Alastair David Graham Donald, Joanne McDermott, Sanjay Ratilal Patel, David Festus Charles Moffat
  • Patent number: 9309260
    Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: April 12, 2016
    Assignee: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Patent number: 9278103
    Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Grant
    Filed: March 31, 2014
    Date of Patent: March 8, 2016
    Assignee: GRÜNENTHAL GMBH
    Inventors: Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
  • Patent number: 9198918
    Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, 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: June 5, 2014
    Date of Patent: December 1, 2015
    Assignee: GENENTECH, INC.
    Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
  • Patent number: 9133206
    Abstract: The present application relates to benzodiazepine and pyridodiazepine derivatives of formula (I) wherein R1, R2, R3, R4, X1, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: September 15, 2015
    Assignee: AbbVie Inc.
    Inventors: William H. Bunnelle, Marc Scanio, Jason T. Brewer, Ying Wang, Irini Akritopoulou-Zanze
  • Patent number: 9090628
    Abstract: Benzoxazepin Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. 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: March 20, 2012
    Date of Patent: July 28, 2015
    Assignee: GENENTECH, INC.
    Inventors: Timothy Heffron, Brian Safina, Steven Staben, Daniel P. Sutherlin, BinQing Wei, Richard Elliott, Robert Heald, Eileen M. Seward, Emanuela Gancia, Bohdan Waszkowycz
  • Patent number: 9085587
    Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: July 21, 2015
    Assignee: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Patent number: 9079869
    Abstract: Chiral disulfonimides having the formula I to III, wherein at least one of the groups A and B in the compound of formula I, C and D of the compound in formula II, and E and F of the compound in formula III is a chiral group, or E and F together form a chiral backbone, X is C, Si, O, N or S, and n is 0, 1, 2, 3, 4, 5 or 6, where n is >1 only if X is C, and G is as defined herein, and to the organic salts, metal salts and metal complexes thereof, are suited as NMR shift reagents and as reagents for racemate splitting, and also as chiral Brønsted acid catalysts or chiral Lewis acid catalysts for activating ketones, aldehydes and alkenes, and also as catalysts in the organic synthesis.
    Type: Grant
    Filed: March 2, 2010
    Date of Patent: July 14, 2015
    Assignee: STUDIENGESELLSCHAFT KOHLE MBH
    Inventors: Benjamin List, Frank Lay, Pilar Garcia Garcia
  • Patent number: 9067924
    Abstract: The present invention relates to 1,4 Thiazepines/Sulfones of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: February 27, 2012
    Date of Patent: June 30, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Hans Hilpert, Mark Rogers-Evans, Didier Rombach
  • Publication number: 20150111877
    Abstract: The invention provides tetrahydronaphthyridine and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydronaphthyridine and related compounds.
    Type: Application
    Filed: May 7, 2013
    Publication date: April 23, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Blair T. Lapointe, Valdimir Simov, Karin A. Stein, William D. Thomas, Peter L. Toogood, Chad A. Van Huis, Catherine M. White
  • Publication number: 20150080325
    Abstract: This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein (I), Q, J, L and Z are as defined in the specification.
    Type: Application
    Filed: April 1, 2014
    Publication date: March 19, 2015
    Applicant: EnVivo Pharmaceuticals, Inc.
    Inventors: Kathryn Rogers, Holger Patzke
  • Patent number: 8980879
    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: Grant
    Filed: March 11, 2014
    Date of Patent: March 17, 2015
    Assignee: AbbVie Inc.
    Inventors: Dachun Liu, John Pratt, Le Wang, Lisa A. Hasvold, Andrew Bogdan
  • Patent number: 8962610
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: February 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Publication number: 20150018298
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, Y1, Y2, or L are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: July 11, 2014
    Publication date: January 15, 2015
    Inventors: Mingzhe Ji, Scott E. Lazerwith, Hyung-Jung Pyun
  • Patent number: 8927536
    Abstract: The present invention relates to a compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof having an excellent effect of inhibiting 11?-hydroxysteroid dehydrogenase type 1: General formula (I) wherein R1 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from substituent group A or a heterocyclic group that may be substituted with 1 to 4 group(s) independently selected from substituent group A; R2 independently represents a halogen atom or a C1-C6 alkyl group; n represents an integer of 0 to 2; and substituent group A represents the group consisting of halogen atoms, C1-C6 alkyl groups, and so forth.
    Type: Grant
    Filed: October 18, 2013
    Date of Patent: January 6, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Makoto Mori, Kunihiko Fujii, Masaharu Inui, Takayuki Baba, Yukari Onishi, Atsushi Aoyagi
  • Patent number: 8916549
    Abstract: Provision of a compound having a serotonin 5-HT2C receptor activating action. A compound represented by the formula (I): wherein each symbol is as described in the description, or a salt thereof.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: December 23, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiro Matsumoto, Izumi Nomura
  • Publication number: 20140356292
    Abstract: A method of evaluating memory/learning functions with the use of a model with glutamic acid N-methyl-D-aspartate (NMDA) type receptor hypofunction as an animal model for schizophrenia and with the use of reference memory task, wherein there has been found concrete means for detecting any differences in activity between typical anti-psychosis drugs and atypical anti-psychosis drugs is found. An in vivo animal model for screening of a therapeutic agent for improving cognitive dysfunction by schizophrenia is provided.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Applicant: Sumitomo Dainippon Pharma Co., Ltd.
    Inventor: Takeo ISHIYAMA
  • Patent number: 8895545
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: November 25, 2014
    Assignee: Debiopharm International SA
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Publication number: 20140336177
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Application
    Filed: December 11, 2012
    Publication date: November 13, 2014
    Inventors: Barbara Pio, Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Shawn Walsh
  • Publication number: 20140323468
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2. R3, R4, R5, R6, R7, W, Y, m and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: April 28, 2014
    Publication date: October 30, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Michael BALESTRA, Jennifer BURKE, Zhidong CHEN, Derek COGAN, Lee FADER, Xin GUO, Bryan MCKIBBEN, Daniel Richard MARSHALL, Peter Allen NEMOTO, Hui YU
  • Publication number: 20140323424
    Abstract: Described herein are assays, kits and methods for treating mood disorders by testing for one or more polymorphisms in a specific group of genes and for analyzing the results of polymorphism testing; the genes included may converge in one or more signaling pathways, and may be epigenetic. The genes are included based on the relationships of the proteins encoded by the genes in the context of particular signaling pathways and provide a diagnostically relevant nexus. Also described herein are methods of presenting the data collected by the screen, including methods of delivering interpretive comments and/or treatment guidance based on the results of the genetic screening either individually or based on the genetic composition of particular clusters of genes which may be related to each other. Importantly, drugs which modulate these genetic disturbances are described for targeted therapeutic use based upon companion diagnostic method.
    Type: Application
    Filed: July 7, 2014
    Publication date: October 30, 2014
    Inventor: Jay L. LOMBARD