Exactly Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/303)
  • Patent number: 10369222
    Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment and prevention of stroke and the sequelae of stroke. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent to yield more effective treatment tools to treat or prevent stroke and the long term effects of stroke in mammalian subjects.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: August 6, 2019
    Assignee: BIOSUCCESS BIOTECH CO., LTD.
    Inventors: Zheng Tao Han, Hung-Fong Chen
  • Patent number: 10316034
    Abstract: The mesylate and sulphate salts of (3S)-Tetrahydrofuran-3-yl (4S)-4-isopropyl-,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridine-5-carboxylate mesylate, and hydrates thereof, and their use in medicine.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: June 11, 2019
    Assignee: BENEVOLENTAI CAMBRIDGE LIMITED
    Inventors: Edward Savory, Michael Higginbottom
  • Patent number: 10301305
    Abstract: The invention relates to the compounds (I) and their acids and bases salts: wherein: Formula (I) the dotted line indicates a double bond; X is N or C—R1 and Y is N or C—R2, X and Y not being simultaneously N; A is selected from the group consisting of phenyl, naphthyl and (5-11) membered monocyclic or bicyclic unsaturated cycle or heterocycle possibly substituted as defined in the application, and A can also comprise either a further (4-7) membered heterocycle, said heterocycle being a monocycle, fused, saturated or unsaturated, the polycyclic system then comprising up to 14 members and up to 5 heteroatoms selected from N, O and S; B is selected from the group of substituents as defined in the application, or B is a 4 or (6-10) membered mono or bicyclic saturated or unsaturated heterocycle containing 1-3 heteroatoms selected from N, O and S, linked by a carbon atom, and possibly substituted as defined in the application; R1 is Hydrogen or a substituent as defined in the application; R2 is Hydrogen or Halogen;
    Type: Grant
    Filed: February 24, 2015
    Date of Patent: May 28, 2019
    Assignee: MUTABILIS
    Inventors: Dmytro Atamanyuk, Francis Chevreuil, Fabien Faivre, Nicolas Lecointe, Benoît Ledoussal, Chrystelle Oliveira, Christophe Simon, Vincent Gerusz
  • Patent number: 10287286
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, Y1, Y2, R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: March 17, 2016
    Date of Patent: May 14, 2019
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Saleh Ahmed, Gregory Barker, Hannah Canning, Richard Davenport, David Harrison, Kerry Jenkins, David Livermore, Susanne Wright, Natasha Kinsella
  • Patent number: 10272035
    Abstract: A method to provide a therapeutic agent to an eye of a patient by implanting or inject a device that stably fits a particular location or position in the eye. The method thus provides agent inside the eye for a longer duration of agent release over a space-occupying area inside the eye.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: April 30, 2019
    Inventor: Gholam A. Peyman
  • Patent number: 10266522
    Abstract: The present disclosure discusses salt forms of 4-cyano-N-[2-(4,4-dimethylcyclohex-1-en-1-yl)-6-(2,2,6,6-tetramethyltetrahydro-2H-pyran-4-yl)pyridin-3-yl]-1H-imidazole-2-carboxamide.
    Type: Grant
    Filed: July 17, 2017
    Date of Patent: April 23, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Nagy E. Fawzy, David Breslin
  • Patent number: 10251874
    Abstract: The present invention provides crystalline hydrates of the oxalate and succinate salts of 5-ethyl-2-fluoro-4-(3-(5-(1-methylpiperidin-4-yl)-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-2-yl)-1H-indazol-6-yl)phenol. The invention also provides pharmaceutical compositions comprising such crystalline hydrates, methods of using such crystalline hydrates to treat respiratory and other diseases, and processes useful for preparing such crystalline oxalate and succinate hydrates.
    Type: Grant
    Filed: April 30, 2018
    Date of Patent: April 9, 2019
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Marta Dabros, Venkat R. Thalladi, Jerry Nzerem, Melanie A. Kleinschek, Glenn D. Crater
  • Patent number: 10246418
    Abstract: The present disclosure relates to a novel crystalline form of lenvatinib mesylate and the preparation method thereof. The novel crystalline form of mesylate of the present disclosure can be used for treating invasive and differentiated thyroid cancer. The novel crystalline form of mesylate of the present disclosure has good solubility, stability, and remarkable purification effect in process. The preparation method of this novel crystalline form is simple, low cost, and has an important value for future optimization and development of the drug.
    Type: Grant
    Filed: June 8, 2016
    Date of Patent: April 2, 2019
    Assignee: Crystal Pharmatech Co., Ltd.
    Inventors: Minhua Chen, Yanfeng Zhang, Xiaojuan Diao, Xiaoyu Zhang
  • Patent number: 10226448
    Abstract: 7-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a 7-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: March 12, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10214527
    Abstract: The present invention provides compounds of Formula (I): wherein A is as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.
    Type: Grant
    Filed: August 30, 2016
    Date of Patent: February 26, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Scott A. Shaw, Joanne M. Smallheer
  • Patent number: 10206929
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: February 19, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar Kc, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10196436
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Grant
    Filed: January 10, 2018
    Date of Patent: February 5, 2019
    Assignee: BLUEPRINT MEDICINES CORPORATION
    Inventor: Chandrasekhar V. Miduturu
  • Patent number: 10188645
    Abstract: The disclosure is directed to a method of easing a patient's symptoms related to termination of opioid pain therapy, and compositions for achieving said method. The method and compositions comprise a series of self tapering dosages of a pharmaceutical composition that is configured to alleviate or prevent symptoms of the patient's termination of opioid pain therapy. The series of self tapering dosages may be supplied in a dosage package.
    Type: Grant
    Filed: August 26, 2016
    Date of Patent: January 29, 2019
    Inventors: Ian Cain Smith, Robert W. Mooney
  • Patent number: 10189870
    Abstract: The present invention relates to a novel crystalline form of oxazolidinone antibiotics, which has advantages in the aspects of solubility, hygroscopicity, crystallinity and stability; the present invention also relates to a method for preparing the novel crystalline form, a pharmaceutical composition containing thereof and the use thereof in the preparation of drugs for treating and/or preventing diseases caused by microbial infection.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: January 29, 2019
    Assignee: HANGZHOU PUSHAI PHARMAEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Xiaoxia Sheng, Xiaohong Sheng, Tao Zhu, Qiang Jia
  • Patent number: 10189808
    Abstract: Solid forms comprising 2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed.
    Type: Grant
    Filed: January 6, 2017
    Date of Patent: January 29, 2019
    Assignee: Celgene Corporation
    Inventors: Paul F. Fernandez, Antonio C. Ferretti, Mohit A. Kothare, Ying Li, Hon-Wah Man, Weihong Zhang
  • Patent number: 10155751
    Abstract: The invention relates to new substituted heteroaryls of formula 1 or of formula 1? wherein A is either N or CH, wherein R2 is selected from the group consisting of —C1-3-alkyl, —C1-3-haloalkyl, F, Br, Cl, wherein Y is selected from —O— or —CH2—, and wherein R3 is defined as in claim 1, and the pharmaceutically acceptable salts thereof, and the use of these aforementioned compounds for the treatment of diseases such as asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: December 18, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Hoffmann, Georg Dahmann, Christian Gnamm, Daniel Robert Fandrick, John Scott, Clive McCarthy
  • Patent number: 10138242
    Abstract: The present invention relates to pyrazolopyridine derivatives, which are useful as medicaments, pharmaceutical compositions comprising one or more of the pyrazolopyridine derivatives, and the use of one or more of the pyrazolopyridine derivatives in methods for treating and/or preventing a disease caused or mediated by a parasite of the family Trypanosomatidae.
    Type: Grant
    Filed: November 20, 2017
    Date of Patent: November 27, 2018
    Inventors: Michael Sattler, Grzegorz Popowicz, Maciej Dawidowski, Leonidas Emmanouilidis, Ralf Erdmann, Wolfgang Schliebs, Vishal Kalel
  • Patent number: 10105370
    Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:
    Type: Grant
    Filed: November 14, 2017
    Date of Patent: October 23, 2018
    Assignee: Samumed, LLC
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Patent number: 10100045
    Abstract: Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, Also provided herein are pharmaceutical compositions comprising compounds of Formula (I) and methods of using compounds of Formula (I).
    Type: Grant
    Filed: October 23, 2017
    Date of Patent: October 16, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Brian Ngo Laforteza, Brad M. Savall, Warren Stanfield Wade, Stephen Todd Meyer, Márió Gyuris
  • Patent number: 10093649
    Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione monohydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione monohydrate are also disclosed.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: October 9, 2018
    Assignee: Celgene Corporation
    Inventor: Jerry Lee Atwood
  • Patent number: 10093647
    Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate are also disclosed.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: October 9, 2018
    Assignee: Celgene Corporation
    Inventor: Jerry Lee Atwood
  • Patent number: 10093648
    Abstract: Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione hemihydrate are also disclosed.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: October 9, 2018
    Assignee: Celgene Corporation
    Inventor: Jerry Lee Atwood
  • Patent number: 10071086
    Abstract: Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.
    Type: Grant
    Filed: January 31, 2017
    Date of Patent: September 11, 2018
    Assignee: Samumed, LLC
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Patent number: 10065954
    Abstract: Specific compounds of formula (Ia): and pharmaceutically acceptable salts thereof. Pharmaceutical compositions of the specific compounds of formula (Ia) and pharmaceutically acceptable salts thereof. A method for inhibiting tumor growth in a subject that includes administering to the subject an effective amount of a compound selected from the specific compounds of formula (Ia) and pharmaceutically acceptable salts thereof. A method for modulating semicarbazide-sensitive amine oxidase activity in a subject that includes administering to the subject an effective amount of a compound selected from the specific compounds of formula (Ia) and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 17, 2015
    Date of Patent: September 4, 2018
    Assignee: PROXIMAGEN LIMITED
    Inventors: Max Espensen, Lee Patient, Edward Savory
  • Patent number: 10034861
    Abstract: The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: July 31, 2018
    Assignee: H. Lundbeck A/S
    Inventors: Jan Kehler, Karsten Juhl, Mauro Marigo, Paulo Jorge Vieira Vital, Mikkel Jessing, Morten Langgård, Lars Kyhn Rasmussen, Carl Martin Sebastian Clementson
  • Patent number: 10016406
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: August 18, 2017
    Date of Patent: July 10, 2018
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Patent number: 10016362
    Abstract: Apixaban liquid formulation is provided. Also provided is a method of administering an apixaban liquid formulation.
    Type: Grant
    Filed: May 24, 2016
    Date of Patent: July 10, 2018
    Assignees: BRISTOL-MYERS SQUIBB COMPANY, PFIZER INC.
    Inventors: Sherif Ibrahim Farag Badawy, Susan Lum
  • Patent number: 10011586
    Abstract: The present invention relates to a heterocyclic compound having a novel structure that can be used in the prevention or treatment of diseases caused by abnormality in a PRS (prolyl-tRNA synthetase) activity, a method for preparing the same, and a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: June 7, 2016
    Date of Patent: July 3, 2018
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: Joon Seok Park, Youn Jung Yoon, Min Jae Cho, Ho Bin Lee, Ja Kyung Yoo, Bong Yong Lee
  • Patent number: 10000771
    Abstract: Isolated peptides comprising nuclear targeting activity or being capable of preventing endogenous nuclear targeting activity are disclosed. Polynucleotides encoding same, pharmaceutical compositions comprising same, as well as uses thereof are also disclosed.
    Type: Grant
    Filed: April 13, 2016
    Date of Patent: June 19, 2018
    Assignee: Yeda Research and Development Co. Ltd.
    Inventors: Rony Seger, Dana Chuderland
  • Patent number: 10000466
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Grant
    Filed: July 7, 2017
    Date of Patent: June 19, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael J. Orwat, Donald J. P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
  • Patent number: 9994563
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: November 12, 2015
    Date of Patent: June 12, 2018
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Patent number: 9981994
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.
    Type: Grant
    Filed: January 17, 2017
    Date of Patent: May 29, 2018
    Assignee: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Craig C. Beeson, Christopher C. Lindsey, Yuri K. Peterson, Baerbel Rohrer
  • Patent number: 9975893
    Abstract: Disclosed are a compound of formula (I), a tautomer, an optical isomer or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the above-mentioned compounds. The above-mentioned compounds have the activity of inhibiting Xa factor positive effect, and can be used for the preparation of a medicament for preventing and/or treating diseases inhibiting Xa factor positive effect in case of low bleeding risk.
    Type: Grant
    Filed: September 2, 2015
    Date of Patent: May 22, 2018
    Assignee: CSPC ZHONGQI PHARMACEUTICAL TECHNOLOGY (SHIJIAZHUANG) CO., LTD.
    Inventors: Ying Shi, Qingzhi Gao, Yi Mi, Xuliang Wang
  • Patent number: 9944638
    Abstract: Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: April 17, 2018
    Assignee: JANSSEN SCIENCES IRELAND US
    Inventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Patent number: 9925226
    Abstract: A method for manufacturing water-soluble medical amber causes that original great molecular groups of medical amber crystals are decomposed into hydrophilic extracted liquid plentiful of water and having small molecular groups, which can be directly coated on skin without mixing with water and added with grease or oil. The method original performs disinfecting and sterilizing treatment for natural medical amber crystals; after a polishing and cleaning step, they are placed in a bottle with treatment liquid therein for a predetermined time period so that the mixture in the bottle ferments and decomposes into small pieces which presents as cream-like liquid. Then paddies are added into the bottle. The bottle is retained through several months so that the medical amber crystals ferment quickly to form as a liquid composite. Then the bottle is evaporated several hours so that the liquid composite is distilled out of the bottle.
    Type: Grant
    Filed: July 11, 2014
    Date of Patent: March 27, 2018
    Inventor: Huei Chen Yang
  • Patent number: 9914910
    Abstract: Methods of preserving and/or protecting pancreatic beta cells by inhibiting NOX-1. In a further aspect, NOX-1 inhibitors are administered to a subject in order to preserve and/or protect beta cells in the prevention or treatment of diabetes. NOX-1 inhibitors are also disclosed.
    Type: Grant
    Filed: March 31, 2017
    Date of Patent: March 13, 2018
    Assignee: Eastern Virginia Medical School
    Inventor: David Taylor-Fishwick
  • Patent number: 9890178
    Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: February 13, 2018
    Assignee: Janssen Sciences Ireland UC
    Inventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
  • Patent number: 9889140
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: September 16, 2016
    Date of Patent: February 13, 2018
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 9873695
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt or solvate thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example as modulators of the growth hormone secretagogue receptor (also referred to as the ghrelin receptor or GHSR1a receptor) and/or for the treatment and/or prophylaxis of a disorder mediated by the ghrelin receptor.
    Type: Grant
    Filed: August 5, 2015
    Date of Patent: January 23, 2018
    Assignee: RaQualia Pharma Inc.
    Inventors: Yasuhiro Iwata, Kiyoshi Kawamura, Masaki Sudo, Kaoru Shimada, Shinichi Koizumi, Nobuyuki Takahashi, Keiko Obata, Makiko Kuroda
  • Patent number: 9855272
    Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:
    Type: Grant
    Filed: August 23, 2016
    Date of Patent: January 2, 2018
    Assignee: Samumed, LLC
    Inventors: John Hood, Sunil Kumar Kc, David Mark Wallace
  • Patent number: 9844536
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: November 29, 2016
    Date of Patent: December 19, 2017
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 9820976
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (for convenience, collectively referred to herein as “IP compounds”), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterized by (e.g., driven by) mutant RAS (“mutant RAS cancer”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.
    Type: Grant
    Filed: September 1, 2016
    Date of Patent: November 21, 2017
    Assignees: CANCER RESEARCH TECHNOLOGY LIMITED, INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
    Inventors: Caroline Joy Springer, Ion Niculescu-Duvaz, Richard Marais, Dan Niculescu-Duvaz, Alfonso Zambon, Delphine Menard
  • Patent number: 9815854
    Abstract: Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: November 21, 2016
    Date of Patent: November 14, 2017
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar K C, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 9809592
    Abstract: The present invention provides a compound of the Formula (I) below: Wherein R1 is selected from the group consisting of H, CH3, CN, CH2CN, C(CH3)2CN, and F; R2 is selected from the group consisting of H, O(C1-C3alkyl)R5, CH2CN, and CN; R3 is selected from the group consisting of H, OCH3, CN, C(CH3)2CN, and CH2CN; R4 is selected from the group consisting of H and CH3; R5 is selected from the group consisting of H, CN, C(CH3)2CN, OCH3, S(O)2CH3, and C(CH3)2OH; provided that at least one selected from the group consisting of R1, R2, R3 and R4 is H; or a pharmaceutically acceptable salt thereof, methods of treating diabetes using the compound and a process for preparing the compound.
    Type: Grant
    Filed: January 6, 2015
    Date of Patent: November 7, 2017
    Assignee: Eli Lilly and Company
    Inventors: Chafiq Hamdouchi, Pranab Maiti, Anne Reifel Miller
  • Patent number: 9771362
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain triazolo compounds (referred to herein as TAZ compounds), and especially certain [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine compounds, which, inter alia, inhibit AXL receptor tyrosine kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit AXL receptor tyrosine kinase function, and in the treatment of diseases and conditions that are mediated by AXL receptor tyrosine kinase, that are ameliorated by the inhibition of AXL receptor tyrosine kinase function, etc., including proliferative conditions such as cancer, etc.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: September 26, 2017
    Assignee: CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Grégoire Alexandre Pavé, James Donald Firth, Lorna Stewart, Laurent Jean Martin Rigoreau, Emma Louise Stanway
  • Patent number: 9763927
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: June 16, 2016
    Date of Patent: September 19, 2017
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar Kc
  • Patent number: 9725435
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
    Type: Grant
    Filed: June 15, 2016
    Date of Patent: August 8, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael J. Orwat, Donald J. P. Pinto, Leon M. Smith, II, James R. Corte, Shefali Srivastava
  • Patent number: 9725446
    Abstract: Compounds of the formula (I) in which R, R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumors.
    Type: Grant
    Filed: January 5, 2016
    Date of Patent: August 8, 2017
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Christian Sirrenberg, Thomas J. J. Mueller, Eugen Merkul, Gnuni Amatunu Karapetyan
  • Patent number: 9675593
    Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
    Type: Grant
    Filed: May 23, 2016
    Date of Patent: June 13, 2017
    Assignee: INTERMUNE, Inc.
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
  • Patent number: 9624243
    Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: April 18, 2017
    Assignee: NOVARTIS AG
    Inventors: Thomas David McCarthy, Alan Naylor