Plural Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/234.5)
  • Patent number: 10308631
    Abstract: A compound of formula I, wherein the compound of formula I has the structure: wherein R1 to R5, Y, L, Z and X1 to X7 have meanings given in the description, said compounds having utility in the treatment of hyperproliferative disease.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: June 4, 2019
    Assignee: NATIONAL UNIVERSITY OF SINGAPORE
    Inventors: Sang Hyun Lee, Brian William Dymock, Mayumi Kitagawa, Cheng Shang See
  • Patent number: 10278976
    Abstract: The invention relates to methods for preventing cancer in a KRAS-variant subject which include administering to the KRAS-variant subject an amount of estrogen effective to reduce the risk of developing cancer. In another aspect, the invention further relates to methods for treating cancer in a KRAS-variant subject, which include gradually decreasing estrogen exposure in the KRAS-variant subject to reduce the risk of aggressive tumor growth. In another aspect, the invention relates to a method of predicting an increased risk of developing a second, independent breast cancer in a subject. The method can include detecting a single nucleotide polymorphism (SNP) at position 4 of the let-7 complementary site 6 of KRAS in a patient sample wherein the presence of said SNP indicates an increased risk of developing a second, independent cancer in said subject.
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: May 7, 2019
    Assignee: Mira Dx, Inc.
    Inventor: Joanne Weidhaas
  • Patent number: 10265320
    Abstract: Amino, amido, and heterocyclic compounds are disclosed. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia/reperfusion injury, cardiovascular disease and other diseases related to RAGE activity.
    Type: Grant
    Filed: May 25, 2016
    Date of Patent: April 23, 2019
    Assignees: The Research Foundation for The State University of New York, New York Universirty
    Inventors: Ann Marie Schmidt, Ravichandran Ramasamy, Alexander Shekhtman, Vivek Rai, Michaele B. Manigrasso
  • Patent number: 10266529
    Abstract: The present invention provides crystalline Forms FUM-P3, FUM-P4, MLA-P3 and MLA-P4 of compound formula 1 and related methods of treating and/or preventing a disease, such as a central nervous system disease (e.g., an anxiety disorder), using a crystalline Form FUM-P3, FUM-P4, MLA-P3 and MLA-P4 of compound formula 1 and/or pharmaceutical compositions thereof.
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: April 23, 2019
    Assignees: Bionomics Limited, Ironwood Pharmaceuticals, Inc.
    Inventors: Bernard Luke Flynn, Dharam Paul, Andrew John Harvey, Vasu V. Sethuraman, Raymond E. Forslund, Song Xue, Rob Livingston, Ahmad Hashash
  • Patent number: 10213445
    Abstract: The present disclosure provides methods utilizing the diazeniumdiolate-based prodrugs for the treatment of cancer via various mechanisms and procedures. The disclosure also provides kits comprising the diazeniumdiolate-based prodrugs.
    Type: Grant
    Filed: November 6, 2015
    Date of Patent: February 26, 2019
    Assignees: Arizona Board of Regents on Behalf of the University of Arizona, a body corporate, The United States of America as Represented by the Secretary of the Department of Health and Human Services
    Inventors: Katrina M. Miranda, David A. Wink, Debashree Basudhar
  • Patent number: 10206924
    Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a quinazoline structure or a quinoline structure which function as dual inhibitors of EGFR proteins and PI3K proteins, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Grant
    Filed: December 15, 2015
    Date of Patent: February 19, 2019
    Assignee: The Regents of the University of Michigan
    Inventors: Christopher Emil Whitehead, Judith S. Leopold
  • Patent number: 10202330
    Abstract: The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A?), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A?) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CH2C(=0)NH2, heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from a single bond, —CH2—, —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy.
    Type: Grant
    Filed: September 2, 2015
    Date of Patent: February 12, 2019
    Assignee: ORYZON GENOMICS, SA
    Inventors: Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe
  • Patent number: 10150783
    Abstract: Disclosed herein are heterocyclic compounds and compositions useful in the treatment of ITK mediated diseases, such as inflammation, having the structure of Formula (I): wherein R1, R2, and X are as defined in the detailed description. Methods of inhibition of ITK activity in a human or animal subject are also provided.
    Type: Grant
    Filed: May 31, 2017
    Date of Patent: December 11, 2018
    Assignee: ACLARIS THERAPEUTICS, INC.
    Inventors: Eric Jon Jacobsen, James Robert Blinn, John Robert Springer, Susan L. Hockerman
  • Patent number: 10105324
    Abstract: Disclosed is a method of treating or ameliorating a condition which can be treated or ameliorated by the administration of guaifenesin, which method comprises orally administering to a subject in need thereof an effective amount of an immediate release solution for oral administration of guaifenesin and at least one additional drug. In addition to water the solution comprises as solvents propylene glycol and glycerol in a concentration which significantly increases the bioavailability of guaifenesin in the human body.
    Type: Grant
    Filed: October 30, 2017
    Date of Patent: October 23, 2018
    Assignee: SOVEREIGN PHARMACEUTICALS, LLC
    Inventor: Paul Hafey
  • Patent number: 10100058
    Abstract: The present disclosure relates to compounds that are CaM Kinase inhibitors and to their use in the treatment of various disease states, including atrial fibrillation and myocardial infarction. In particular embodiments, the general structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, R5, R6, R9 and R10 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: November 29, 2017
    Date of Patent: October 16, 2018
    Assignee: Gilead Sciences, Inc.
    Inventors: Elfatih Elzein, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Eric Q. Parkhill, Thao Perry, Scott Preston Simonovich, Jeff Zablocki, Christopher Allen Ziebenhaus
  • Patent number: 10093657
    Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: March 9, 2017
    Date of Patent: October 9, 2018
    Assignees: HOFFMANN-LA ROCHE INC., CHUGAI PHARMACEUTICAL CO.
    Inventors: Francisco Javier Lopez-Tapia, Sung-Sau So, Qi Qiao, Romyr Dominique
  • Patent number: 10071091
    Abstract: The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxymorphone (4,5-?-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxymorphone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxymorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.
    Type: Grant
    Filed: May 8, 2017
    Date of Patent: September 11, 2018
    Assignee: KemPharm, Inc.
    Inventors: Travis Mickle, Sven Guenther, Sanjib Bera, Jaroslaw Kanski, Andrea Martin
  • Patent number: 10064834
    Abstract: The present invention includes a method of inhibiting or reducing mTOR signaling or inhibition of indoleamine dioxygenase-1 (IDO1) in a subject with a proliferative disease, which comprises administering to the subject having or suspected to have the proliferative disease, a therapeutically or prophylactically effective amount of the compound of Formula I: or a pharmaceutically acceptable salt or solvate thereof.
    Type: Grant
    Filed: May 9, 2017
    Date of Patent: September 4, 2018
    Assignee: Texas Tech University System
    Inventors: Vadivel Ganapathy, Yangzom D. Bhutia, Babu Ellappan, Sabarish Ramachandran
  • Patent number: 10053737
    Abstract: The invention is directed to methods, reagents, and kits for the detection of MAPK/ERK pathway mutations in a patient diagnosed for cancer. In one embodiment, the invention comprises a sensitive and selective method to identify mutations to the BRAF, KRAS, and NRAS genes in a single reaction. In another aspect of this embodiment, the invention comprises primers and probes for the detection of the BRAF, KRAS, and NRAS mutations using a single nucleotide primer extension assay. In another embodiment the invention is used to identify and select patients amenable for treatment with an ERK inhibitor.
    Type: Grant
    Filed: April 3, 2014
    Date of Patent: August 21, 2018
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Ken C. N. Chang, Stefan Galuska, Matthew J. Marton
  • Patent number: 10052284
    Abstract: The present invention provides, among other things, methods of delivering mRNA in vivo, including administering to a subject in need of delivery a composition comprising an mRNA encoding a protein, encapsulated within a liposome such that the administering of the composition results in the expression of the protein encoded by the mRNA in vivo, wherein the liposome comprises a cationic lipid of formula I-c: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 2017
    Date of Patent: August 21, 2018
    Assignee: TRANSLATE BIO, INC.
    Inventors: Michael Heartlein, Daniel Anderson, Yizhou Dong, Frank DeRosa
  • Patent number: 10045962
    Abstract: Provided in the present invention are uses of duloxetine hydrochloride in preparing a pharmaceutical composition for treatment of cancer.
    Type: Grant
    Filed: April 20, 2017
    Date of Patent: August 14, 2018
    Assignee: LAUNX BIOMEDICAL CO., LTD.
    Inventors: Chiu-Hung Chen, Show-Mei Chuang, Tzong-Der Way, Nai-Wan Hsiao
  • Patent number: 10035777
    Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
    Type: Grant
    Filed: July 27, 2015
    Date of Patent: July 31, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carolyn Diane Dzierba, Joanne J. Bronson, John E. Macor, Bireshwar Dasgupta, Susheel Jethanand Nara, Vivekananda M. Vrudhula, Senliang Pan, Richard A. Hartz, Ramkumar Rajamani
  • Patent number: 10022387
    Abstract: The present invention provides aza-heteroaryl derivatives of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, Z, A, W, R4, R5, and R6 are defined herein, that inhibit the activity of phosphoinositide 3-kinases-gamma (PI3K?) and are useful in the treatment of diseases related to the activity of PI3K? including, for example, autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.
    Type: Grant
    Filed: January 25, 2017
    Date of Patent: July 17, 2018
    Assignee: Incyte Corporation
    Inventors: Ge Zou, Andrew P. Combs, Andrew W. Buesking
  • Patent number: 10023569
    Abstract: A method of preparing Compound (1) or a pharmaceutically acceptable salt thereof: comprises: (a) reacting Compound (X): or a pharmaceutically acceptable salt thereof with Compound (Y): in the presence of a palladium catalyst and a carbonate or phosphate base to form compound (Z): or a pharmaceutically acceptable salt thereof; and (b) deprotecting the Ts group of Compound (Z) to form Compound (1) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 10, 2016
    Date of Patent: July 17, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Gerald J. Tanoury, William Aloysius Nugent, Vadims Dvornikovs, Peter Jamison Rose
  • Patent number: 10016390
    Abstract: Provided in the present invention are uses of duloxetine hydrochloride in preparing a pharmaceutical composition for treatment of cancer.
    Type: Grant
    Filed: April 20, 2017
    Date of Patent: July 10, 2018
    Assignee: LAUNX BIOMEDICAL CO., LTD.
    Inventors: Chiu-Hung Chen, Show-Mei Chuang, Tzong-Der Way, Nai-Wan Hsiao
  • Patent number: 9994529
    Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, and Z are as defined herein, and methods of making and using the same.
    Type: Grant
    Filed: February 14, 2017
    Date of Patent: June 12, 2018
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Michael Jonathan Bury, Linda N. Casillas, Adam K. Charnley, Michael P. Demartino, Xiaoyang Dong, Patrick M. Eidam, Pamela A. Haile, Robert W. Marquis, Jr., Joshi M. Ramanjulu, Joseph J. Romano, Ami Lakdawala Shah, Robert R. Singhaus, Jr., Gren Wang
  • Patent number: 9962348
    Abstract: The present invention discloses novel agents and methods for diagnosis and treatment of melanoma. Also disclosed are related arrays, kits, and screening methods.
    Type: Grant
    Filed: July 14, 2017
    Date of Patent: May 8, 2018
    Assignee: The Rockefeller University
    Inventors: Sohail F. Tavazoie, Nora Pencheva
  • Patent number: 9949932
    Abstract: Disclosed are pharmaceutical compositions comprising a compound having the formula: or a pharmaceutically acceptable salt thereof, or a hydrate of thereof, and at least one pharmaceutically acceptable polymer. The pharmaceutically acceptable salt of the compound of Formula I, or a hydrate thereof, can be a mesylate salt, including, for example, a mono-mesylate or a bis-mesylate salt, or a hydrate thereof. Also disclosed are methods of use for the pharmaceutical composition.
    Type: Grant
    Filed: June 9, 2016
    Date of Patent: April 24, 2018
    Assignee: Gilead Connecticut, Inc.
    Inventors: Melissa Jean Casteel, Bei Li, Rowchanak Pakdaman, Diana Sperger, Dimitrios Stefanidis
  • Patent number: 9943398
    Abstract: The present invention relates to methods of tissue grafting and microvascular free flap transfer that involve administering a phosphodiesterase type-5 inhibitor to the tissue graft or microvascular free flap to produce a treated graft or flap, and implanting the treated graft or flap into a recipient site of a host subject.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: April 17, 2018
    Assignee: New York University
    Inventor: Daniel J. Ceradini
  • Patent number: 9943519
    Abstract: Compounds of Formulae Ia, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia 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 26, 2014
    Date of Patent: April 17, 2018
    Assignees: Genentech, Inc., F. Hoffmann-La Roche AG
    Inventors: Adrian Folkes, Stephen Shuttleworth, Irina Chuckowree, Sally Oxenford, Nan Chi Wan, Georgette Castanedo, Richard Goldsmith, Janet Gunzer-Toste, Tim Heffron, Simon Mathieu, Alan Olivero, Daniel P. Sutherlin, Bing-Yan Zhu
  • Patent number: 9884855
    Abstract: A fumarate salt and a maleate salt of compound (I) represented by the following structural formula, as well as their corresponding pharmaceutical compositions, are disclosed. Particular single crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are also disclosed. The present invention also provides methods of treating a subject with a cancer.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: February 6, 2018
    Assignee: University Health Network
    Inventors: Peter Brent Sampson, Miklos Feher, Heinz W. Pauls
  • Patent number: 9873690
    Abstract: A compound of Formula I is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates to a process for manufacturing compounds of Formula I.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: January 23, 2018
    Assignees: Pfizer Inc, iTeos Therapeutics
    Inventors: Sacha Ninkovic, Stefano Crosignani, Indrawan James McAlpine, Michael Raymond Collins, Stephanie Anne Scales, Andreas Maderna, Martin Wythes
  • Patent number: 9862704
    Abstract: The present invention relates to novel substituted oxindole derivatives of formula (I) wherein the variables are as defined in the claims and description; to pharmaceutical compositions comprising them, and to their use for the treatment of vasopressin-related disorders.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: January 9, 2018
    Assignees: ABBVIE DEUTSCHLAND GMBH & CO. KG, ABBVIE INC.
    Inventors: Hervé Geneste, Wilfried Hornberger, Charles W. Hutchins, Katja Jantos, Andreas Kling, Loic Laplanche, Marcel Van Gaalen
  • Patent number: 9796703
    Abstract: The present invention is directed to novel synthetic methods for preparing cyclopropyl indolinone compound represented by Structural Formula (A): (A) or its pharmaceutically acceptable salt thereof. Also included are synthetic intermediates described herein.
    Type: Grant
    Filed: February 23, 2017
    Date of Patent: October 24, 2017
    Assignee: University Health Network
    Inventors: Graham Cumming, Narendra Kumar B. Patel, Bryan T. Forrest, Yong Liu, Sze-Wan Li, Peter Brent Sampson, Louise G. Edwards, Heinz W. Pauls
  • Patent number: 9796709
    Abstract: A compound represented by the general formula (I) or a pharmacologically acceptable salt thereof has an excellent LCAT-activating effect and is useful as an active ingredient in a therapeutic or prophylactic agent for arteriosclerosis, arteriosclerotic heart disease, coronary heart disease (including heart failure, myocardial infarction, angina pectoris, cardiac ischemia, cardiovascular disturbance, and restenosis caused by angiogenesis), cerebrovascular disease (including stroke and cerebral infarction), peripheral vascular disease (including diabetic vascular complications), dyslipidemia, hypo-HDL-cholesterolemia, hyper-LDL-cholesterolemia, or renal disease, particularly, an anti-arteriosclerotic agent, wherein R is an optionally substituted aryl group or an optionally substituted heteroaryl group, and R1 is a hydrogen atom or a hydroxy group.
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: October 24, 2017
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Hideki Kobayashi, Masami Arai, Toshio Kaneko, Naoki Terasaka
  • Patent number: 9790198
    Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R5, R6, W, and A are defined herein.
    Type: Grant
    Filed: October 8, 2015
    Date of Patent: October 17, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Hui Huang, Gee-Hong Kuo, Mark R. Player, Shyh-Ming Yang, Yue-Mei Zhang
  • Patent number: 9789117
    Abstract: The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat type-2 diabetes-associated pain and related symptoms.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: October 17, 2017
    Assignee: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Jose Miguel Vela Hernandez, Maria Isabel Martin Fontelles
  • Patent number: 9771327
    Abstract: The invention relates to a compound of Formula I and methods of treating CFTR (cystic fibrosis transmembrane conductance regulator) mediated diseases, in particular cystic fibrosis, comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: September 26, 2017
    Assignee: FLATLEY DISCOVERY LAB, LLC
    Inventors: Michael P. Zawistoski, Yevgen Barsukov, Bridget M. Cole, Richard A. Nugent
  • Patent number: 9763900
    Abstract: This invention relates to chemistry and biochemistry applied to the field of medicine and is referred to a new method of prevention and therapeutic treatment of conformational diseases (CD), in particular to amyloid origin diseases by administrating an effective amount of one or more compounds, salts, prodrugs or solvates, which are considered herein as chemical chaperonins, of Formula I, Where: R1: -alkylenyl-C(O)NH-alkylenyl-R3, -alkylenyl-C(O)O—R4; R3: —COOH, —OH, —SH, —NH2, —NH-alkyl-, —NH-dithiocarbamate-alkyl, —N-alkyl-dithiocarbamate alkaline earth metal salts. R4: succinimidyl group. R2: —H, -alkyl; wherein the term “alkyl” is characterized by a linear or branched aliphatic chain, hydrogen and saturated carbon atoms, comprising a methyl, ethyl, n-propyl, iso-propyl, n-butyl or iso-butyl groups. Wherein, the term “alkylenyl” refers to a divalent analog of a linear or branched alkyl group, preferably ethylenyl (—CH2CH2—) or butylenyl (—CH2CH2CH2CH2—) radicals.
    Type: Grant
    Filed: December 30, 2013
    Date of Patent: September 19, 2017
    Assignee: CENTRO DE NEUROCIENCIAS DE CUBA
    Inventors: Marquiza Sablón Carrazana, Chryslaine Rodriguez-Tanty, Myriam Marlene Altamirano Bustamante, Fernand Vedrenne Gutiérrez, Suchitil Rivera Marrero, Isaac Fernández Gómez, Rosa María López Barroso, Lina Andrea Rivillas Acevedo, Reyna Lara Martinez, Rafaela Perez Perera, Alberto Bencomo Martínez, María Guadalupe Domínguez Macouzet, Luis Felipe Jiménez García, Massiel Díaz Miranda, Julio Morán Andrade, Pedro Valdés Sosa, Alejandro Perera Pintado, Anaís Prats Capote, Sergio Agustín Islas Andrade
  • Patent number: 9725442
    Abstract: The present invention is related to a compound represented by formula (I), wherein X1, X2, X3, X4, X5, R5, R6, R7, R8, n, p, q, ring A and ring B are as described in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: August 8, 2017
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Kayoko Hata, Manami Masuda, Hiromi Nakai, Daisuke Taniyama, Hiroyuki Tobinaga, Yoshio Hato, Motohiro Fujiu
  • Patent number: 9700551
    Abstract: The present invention relates to the new use of 1H-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta (GSK-3?) inhibitors and to their use in the treatment of GSK-3?-related disorders such as, for example, (i) insulin-resistance disorders; (ii) neurodegenerative diseases; (iii) mood disorders; (iv) schizophrenic disorders; (v) cancerous disorders; (vi) inflammation, (vii) substance abuse disorders; and (viii) epilepsies.
    Type: Grant
    Filed: August 13, 2015
    Date of Patent: July 11, 2017
    Assignee: AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.P.A.
    Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Barbara Garofalo, Guido Furlotti, Gabriele Magaro', Rosella Ombrato, Francesca Mancini
  • Patent number: 9694014
    Abstract: Administration of a monoamine oxidase inhibitor is useful in the prevention and treatment of muscle dystrophy. Methods and compositions for inhibiting the production of reactive oxygen species in a muscle cell overproducing reactive oxygen species are provided herein.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: July 4, 2017
    Assignee: Universita Degli Studi di Padova
    Inventors: Paolo Bonaldo, Marcella Canton, Fabio DiLisa, Sara Menazza
  • Patent number: 9676783
    Abstract: Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: June 13, 2017
    Assignee: Array BioPharma, Inc.
    Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
  • Patent number: 9676768
    Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: March 20, 2015
    Date of Patent: June 13, 2017
    Assignee: ASTEX THERAPEUTICS LIMITED
    Inventors: Alison Jo-Anne Woolford, Steven Howard, Ildiko Maria Buck, Gianni Chessari, Christopher Norbert Johnson, Emiliano Tamanini, James Edward Harvey Day, Elisabetta Chiarparin, Thomas Daniel Heightman, Martyn Frederickson, Charlotte Mary Griffiths-Jones
  • Patent number: 9676771
    Abstract: A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is N, C(OH), or CH; Y is H or OH; each of Z1-Z5 is independently H or halogen; R4 is H, OH, NH2, NHR8, NR8R9 or R8; R5, R6, and R7 is each independently H, halogen, OR8, R8, NHR8, NR8R9, CO2R8, CONR8R9, SO2NR8R9, or R5 and R6 together with the carbon atoms to which R5 and R6 are attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; and R8 and R9 is each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or R8 and R9 together with the nitrogen t
    Type: Grant
    Filed: May 13, 2014
    Date of Patent: June 13, 2017
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Xue Zhi Zhao, Steven Smith, Mathieu Metifiot, Barry Johnson, Christophe Marchand, Stephen H. Hughes, Yves Pommier, Terrence R. Burke, Jr.
  • Patent number: 9657023
    Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula I: or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula IA: Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: May 23, 2017
    Assignee: Gilead Connecticut, Inc.
    Inventors: Tim G. Elford, Peter Chee-Chu Fung, Michael Laird Hurrey, Dimitrios Stefanidis, Dragos Vizitiu
  • Patent number: 9624201
    Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: April 18, 2017
    Assignees: HOFFMANN-LA ROCHE INC., CHUGAI PHARMACEUTICAL CO.
    Inventors: Francisco Javier Lopez-Tapia, Sung-Sau So, Qi Qiao, Romyr Dominique
  • Patent number: 9611253
    Abstract: Solid forms comprising pyrazolylaminoquinazoline, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders are disclosed.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: April 4, 2017
    Assignee: Ambit Biosciences Corporation
    Inventor: Timothy David Gross
  • Patent number: 9603820
    Abstract: Therapeutic methods relating to the use of GABA-AT inhibitor compounds for the treatment of hepatocellular carcinoma.
    Type: Grant
    Filed: November 9, 2015
    Date of Patent: March 28, 2017
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Yaron Ilan
  • Patent number: 9579319
    Abstract: This invention relates to novel compounds of formula (I). The compounds of the invention are hedgehog pathway antagonists. Specifically, the compounds of the invention are useful as Smoothened (SMO) inhibitors. The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of the Hedgehog pathway and SMO, for example cancer.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: February 28, 2017
    Assignee: Redx Pharma PLC
    Inventors: Richard Armer, Matilda Bingham, Inder Bhamra, Andrew McCarroll
  • Patent number: 9573946
    Abstract: Provided are compounds, compositions and methods for inhibiting fascin activity or treating a condition or disorder mediated by fascin activity in a subject in need thereof.
    Type: Grant
    Filed: February 19, 2015
    Date of Patent: February 21, 2017
    Assignees: Novita Pharmaceuticals, Inc., Cornell University
    Inventors: Xin-Yun Huang, Christy Young Shue
  • Patent number: 9562013
    Abstract: Provided herein are HDAC3 inhibitors, as well as methods of treatment comprising administering these compounds to a subject in need thereof.
    Type: Grant
    Filed: June 29, 2015
    Date of Patent: February 7, 2017
    Assignee: Acetylon Pharmaceuticals, Inc.
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 9556150
    Abstract: This application discloses compounds according to generic Formula (I) wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: January 31, 2017
    Assignees: Hoffmann-La Roche Inc., Chugai Pharmaceutical Co.
    Inventors: Francisco Javier Lopez-Tapia, Norman Kong, Sung-Sau So, Yan Lou, Romyr Dominique
  • Patent number: 9550770
    Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions containing the same, and methods of use thereof are described. Specifically quinazoline derivatives of Formula Ia: and their uses in modulating kinase activities are disclosed.
    Type: Grant
    Filed: August 22, 2014
    Date of Patent: January 24, 2017
    Assignee: NeuPharma, Inc.
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Patent number: 9539251
    Abstract: The present invention is directed to a combination therapy involving a type II anti-CD20 antibody and a selective Bcl-2 inhibitor for the treatment of a patient suffering from cancer, particularly, a CD20-expressing cancer.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: January 10, 2017
    Assignees: Genentech, Inc., F. Hoffmann-La Roche AG
    Inventors: Deepak Sampath, Christian Klein, Wayne John Fairbrother