Ring Nitrogen In The Bicyclo Ring System Patents (Class 514/235.2)
  • Patent number: 11420963
    Abstract: Disclosed are a novel rebamipide prodrug, a method for preparing the same, and use thereof. Also, a pharmaceutical composition comprising the novel rebamipide prodrug as an active ingredient is provided. The rebamipide prodrug is increased 25-fold in absorption rate compared to rebamipide itself, and can be applied to the prophylaxis or therapy of gastric ulcer, acute gastritis, chronic gastritis, xerophthalmia, cancer, osteoarthritis, rheumatoid arthritis, or obesity.
    Type: Grant
    Filed: June 26, 2013
    Date of Patent: August 23, 2022
    Assignees: SAMJIN PHARMACEUTICAL CO., LTD., ASTECH. CO., LTD.
    Inventors: Eui Hwan Cho, Sung Ju Choi, Sung Woo Lee, Hee Jong Shin, Ho Seok Kwon, Jae Woong Lee, Jeong Ho Joo, Hyun Tae Kim, Woo Heon Song, Jong Bae Yoon, Ki Seok Park, Ho Joon Park, Ho Tae Nam
  • Patent number: 11420961
    Abstract: The invention provides new heterocyclic compounds having the general formula (IA) wherein A, L, X, Y, m, n, R1 and R2 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
    Type: Grant
    Filed: May 27, 2020
    Date of Patent: August 23, 2022
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Joerg Benz, Uwe Grether, Benoit Hornsperger, Buelent Kocer, Bernd Kuhn, Hans Richter, Satoshi Tsuchiya, Charles Bell, Xiang Wu, Xiaofei Yan, Luca Gobbi
  • Patent number: 11414384
    Abstract: Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).
    Type: Grant
    Filed: February 15, 2019
    Date of Patent: August 16, 2022
    Assignee: Constellation Pharmaceuticals, Inc.
    Inventors: Jonathan E. Wilson, Julian R. Levell
  • Patent number: 11369595
    Abstract: The present invention concerns a tryptophan metabolite chosen from kynurenic acid, anthranilic acid, quinolinic acid, picolinic acid, quinaldic acid and the mixtures of same or an enantiomer, diastereoisomer, hydrate, solvate, tautomer, racemic mixture or pharmaceutically acceptable salt of same, for use as a drug intended for increasing and/or maintaining muscle mass and/or strength in a mammal, and in particular intended for treating and/or preventing muscle atrophy in mammals and/or for promoting muscle growth in mammals doing exercise and aiming to increase muscle mass and/or quality and/or strength, for preventing the appearance of symptoms of sarcopenia or for rehabilitation following muscle loss and/or for improving recovery time after an intense physical effort.
    Type: Grant
    Filed: September 5, 2017
    Date of Patent: June 28, 2022
    Assignee: METABRAIN RESEARCH
    Inventors: Sophie N. Raynal, Annick Audet, Valérie Autier, Christine Charon, Jean-Denis Durand, Micheline Kergoat
  • Patent number: 11352344
    Abstract: Disclosed herein are substituted hexahydro-1H-cyclopenta[c]pyrrole compounds of formula (Ia), which may be useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: June 7, 2022
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Darren W. Engers, Kayla J. Temple
  • Patent number: 11299496
    Abstract: Compounds are provided which bind to an allosteric site on the mammalian alpha-7 nicotinic acetylcholine receptor (alpha-7 nAChR) and act as positive allosteric modulators with or without allosteric agonist activity. The compounds are useful in diagnosing, preventing, or treating a variety of disorders involving cognition, learning, memory, neurodegeneration, drug addiction, inflammation, chronic pain, and neuropathic pain. The compounds also can be used to enhance memory and learning in normal individuals.
    Type: Grant
    Filed: July 23, 2015
    Date of Patent: April 12, 2022
    Assignees: Northeastern University, University of Florida Research Foundation, Inc.
    Inventors: Ganeshsingh A. Thakur, Abhijit R. Kulkarni, Roger Lee Papke
  • Patent number: 11241439
    Abstract: Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed.
    Type: Grant
    Filed: February 25, 2020
    Date of Patent: February 8, 2022
    Assignee: Celgene Corporation
    Inventors: Benjamin M. Cohen, John F. Traverse, Jean Xu, Ying Li
  • Patent number: 11241428
    Abstract: The present invention relates to novel heteroaryl amide derivatives of formula (1) as selective inhibitors of histone deacetylase 1 and 2 (hdac1-2) to processes for their preparation, to pharmaceutical compositions comprising said compounds and to the use of said compounds for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by inhibition the activity of histone deacetylase class I, particularly HDAC1 and HDAC2, such as cancer, neurodegenerative diseases, Infectious diseases, inflammatory diseases, heart failure and cardiac hypertrophy, diabetes, polycystic kidney disease, sickle cell disease and ?-thalassemia disease and to methods for the treatment of the diseases mentioned above.
    Type: Grant
    Filed: July 9, 2018
    Date of Patent: February 8, 2022
    Assignee: Medibiofarma, S.L.
    Inventors: Julio Castro Palomino Laria, Juan Camacho Gómez, Rodolfo Rodríguez Iglesias
  • Patent number: 11213701
    Abstract: Disclosed herein are methods and compositions comprising compounds capable of activating and increasing protein SUMOylation. Disclosed herein are methods and compositions comprising compounds capable of showing neuroprotective and cytoprotective effects when administered to injured cells. Also disclosed are methods comprising these compounds for treating neuronal or neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, fronto-temporal dementia, chronic traumatic encepholopathy, traumatic brain injury, or stroke.
    Type: Grant
    Filed: December 1, 2019
    Date of Patent: January 4, 2022
    Inventor: Russell Dahl
  • Patent number: 11117909
    Abstract: Provided are crystals of 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate, compositions comprising the same, and methods of making and using such crystals.
    Type: Grant
    Filed: May 12, 2017
    Date of Patent: September 14, 2021
    Assignee: AEROMICS, INC.
    Inventors: Paul Robert Mcguirk, Robert Zamboni, Melanie Bevill, Stephan Parent
  • Patent number: 11117882
    Abstract: This disclosure relates to pyrazoline dihydroquinolone derivatives, pharmaceutical compositions, and uses. In certain embodiments, the compounds are selective NMDA receptor inhibitors and are useful in therapeutic methods related thereto. In certain embodiments, this disclosure relates to pharmaceutical compositions comprising a compound of the following formula: or salts, esters, or prodrugs thereof, as provided herein.
    Type: Grant
    Filed: August 2, 2018
    Date of Patent: September 14, 2021
    Assignee: Emory University
    Inventors: Timothy M. Acker, Dennis C. Liotta, Stephen F. Traynelis, Yao Jing
  • Patent number: 11078201
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.
    Type: Grant
    Filed: September 14, 2020
    Date of Patent: August 3, 2021
    Assignee: Nimbus Saturn, Inc.
    Inventors: Neelu Kaila, Ian Linney, Stuart Ward, Grant Wishart, Ben Whittaker, Alexandre Cote, Jeremy Robert Greenwood, Abba Leffler, Steven K. Albanese, Daniel L. Severance
  • Patent number: 11077114
    Abstract: Formulations of molindone having superior stability and methods of administering same are provided. The formulations may be immediate, modified, or otherwise delayed release formulations of molindone.
    Type: Grant
    Filed: October 30, 2018
    Date of Patent: August 3, 2021
    Assignee: Supernus Pharmaceuticals, Inc.
    Inventors: Rong-Kun Chang, Michael L. Vieira, Likan Liang, Padmanabh P. Bhatt, Austin B. Huang, Sachin V. Patel
  • Patent number: 11053224
    Abstract: The invention discloses polymorphic forms of a compound of formula I, pharmaceutical compositions containing same, preparation method therefor and use thereof. The compound of formula I of the present invention is as shown in formula I, of which the crystalline form can be crystalline form 1, crystalline form 2, crystalline form 3, crystalline form 5, crystalline form 6 or crystalline form 7. All the crystalline forms of the compound of formula I in the present invention have good crystalline stability and chemical stability and a decrease in purity of their main ingredient less than 2%. The preparation method of the present invention may be used to produce the various crystalline forms of the compound of formula I with high purity, and suitable for large scale production.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: July 6, 2021
    Assignee: EQUINOX SCIENCES, LLC
    Inventors: Congxin Liang, Lihua Xie
  • Patent number: 11020380
    Abstract: The present embodiments relate to substituted heterocyclic derivative therapeutic compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of diseases mediated by aberrant cell signalling, such as inflammatory disorders, cancer and neoplastic disease. Particular compounds described herein exhibit selective inhibitory activity against CBP compared with BRD4.
    Type: Grant
    Filed: January 27, 2020
    Date of Patent: June 1, 2021
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Lynnie Trzoss, Juan Manuel Betancort, Toufike Kanouni, Michael Brennan Wallace, Amogh Boloor
  • Patent number: 10988437
    Abstract: The invention relates to bis(aniline) compounds containing multiple arylethynyl, alkylethynyl, ethynyl groups or their combinations, processes of making such compounds and materials comprising such compounds. Such, bis(aniline) compounds preferably comprise multiple phenylethynyl (PE) groups, i.e. 2-4 PE moieties. Such compounds are useful monomers for the preparation of polyimides, polyamides and poly(amide-imides) whose post-fabrication crosslinking chemistry (i.e. reaction temperature) can be controlled by the number of PE per repeat unit as well as finding utility in thermosetting matrix resins, 3D printable resins, and as high-carbon-content precursors to carbon-carbon composites.
    Type: Grant
    Filed: January 27, 2020
    Date of Patent: April 27, 2021
    Assignee: United States of America as represented by the Secretary of the Air Force
    Inventors: Loon-Seng Tan, Zhenning Yu
  • Patent number: 10980792
    Abstract: This document relates to compositions comprising a non-covalently bound complex comprising cabozantinib and human serum albumin, wherein the cabozantinib and the human serum albumin in the composition have a ratio by weight from about 1:5 to about 1:2000. This document also relates to compositions comprising cabozantinib and human serum albumin, wherein the cabozantinib and the human serum albumin in the composition have a ratio by weight from about 1:5 to about 1:2000. This document also relates to compositions consisting essentially of cabozantinib and human serum albumin, wherein the cabozantinib and the human serum albumin in the composition have a ratio by weight from about 1:5 to about 1:2000.
    Type: Grant
    Filed: September 11, 2017
    Date of Patent: April 20, 2021
    Inventor: Qun Sun
  • Patent number: 10953071
    Abstract: Pre-implantation factor (PIF) may be used to treat intracellular damage. Aspects of the invention are directed to a method of treating intracellular damage comprising administering PIF to a subject in need thereof. Some aspects may be directed to methods of increasing cytokine secretion in response to intracellular damage comprising administering PIF to a subject in need thereof. The intracellular damage may be a result of a disease such as Listeria monocytogenes infection, malaria, Lyme disease, cardiovascular disease, duodenal peptic ulcer, atherosclerosis, peritonitis or tuberculosis. In some aspects, a method of treating tuberculosis is disclosed, comprising administering PIF to a subject in need thereof. In some aspects, a method of treating atherosclerosis is disclosed, comprising administering PIF to a subject in need thereof. In some aspects, a method of treating peritonitis is disclosed, comprising administering PIF to a subject in need thereof.
    Type: Grant
    Filed: August 9, 2017
    Date of Patent: March 23, 2021
    Assignee: BIOINCEPT, LLC
    Inventor: Eytan R. Barnea
  • Patent number: 10934274
    Abstract: The present invention relates to novel compounds which are inhibitors of TAM (Axl, Mer and Tyro 3) and/or Met family receptor tyrosine kinases (RTKs). These compounds are suitable for the treatment of disorders associated with, accompanied by, caused by or induced by a receptor of the TAM family, in particular a hyperfunction thereof. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly immune-suppressive cancer, refractory cancer and cancer metastases.
    Type: Grant
    Filed: April 14, 2016
    Date of Patent: March 2, 2021
    Assignees: QURIENT CO., LTD., LEAD DISCOVERY CENTER GMBH
    Inventors: Kiyean Nam, Jaeseung Kim, Seohyun Ahn, Yeejin Jeon, Doohyung Lee, Dongsik Park, Young-In Yang, SaeYeon Lee, Jeongjun Kim, Jiye Ahn, Hana Kim, Chun-won Jung, Carsten Schultz-Fademrecht
  • Patent number: 10934278
    Abstract: The present invention provides compounds of the formula (I) and their use as Kv3 modulators.
    Type: Grant
    Filed: July 28, 2017
    Date of Patent: March 2, 2021
    Assignee: Autifony Therapeutics Limited
    Inventors: Giuseppe Alvaro, Agostino Marasco, Guido Marconi
  • Patent number: 10894055
    Abstract: Provided are novel formulations of 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate as described below and uses thereof.
    Type: Grant
    Filed: December 31, 2018
    Date of Patent: January 19, 2021
    Assignee: AEROMICS, INC.
    Inventors: Marc F. Pelletier, Paul Robert McGuirk, George William Farr
  • Patent number: 10851093
    Abstract: Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, X, Y1, Y2, Y3 and Z are as described herein. In certain embodiments, a compound disclosed herein inhibits a cellular TAM receptor, and can be used to treat disease mediated by or involving the TAM receptor family.
    Type: Grant
    Filed: May 29, 2019
    Date of Patent: December 1, 2020
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Ihab Darwish, Jiaxin Yu, Rao Kolluri, Sacha Holland
  • Patent number: 10745357
    Abstract: The present invention relates (i) to a process for the preparation of quinolin-2-yl-phenylamine derivatives of formula (I) without a metal catalyst, and (ii) to soluble mineral acid or sulfonic acid salts of (8-chloro-quinolin-2-yl)-(4-trifluoromethoxyphenyl)-amine.
    Type: Grant
    Filed: November 1, 2019
    Date of Patent: August 18, 2020
    Inventors: Sebastian Rabe, Wolfgang Albrecht
  • Patent number: 10729677
    Abstract: The present invention relates to a method of preventing and/or treating chronic traumatic encephalopathy.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: August 4, 2020
    Assignee: EUSTRALIS PHARMACEUTICAL LIMITED (TRADING AS PRESSURA NEURO)
    Inventor: Robert Vink
  • Patent number: 10688100
    Abstract: Methods for inhibiting a ROS1 kinase with compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein. The compounds and methods provided herein are useful in the treatment of cancer (e.g., ROS1-associated cancers as defined herein).
    Type: Grant
    Filed: November 26, 2018
    Date of Patent: June 23, 2020
    Assignee: Array BioPharma Inc.
    Inventors: Steven W. Andrews, James F. Blake, Julia Haas, Gabrielle R. Kolakowski
  • Patent number: 10647683
    Abstract: The present invention, among other things, provides compounds and compositions thereof for use in the modulation of Hsp70. In some embodiments, the present invention provides a method for inhibiting Hsp70 activity. In some embodiments, the present invention provides a method of treating a subject suffering from or susceptible to a disease, disorder, or condition responsive to Hsp70 inhibition comprising administering to the subject a therapeutically effective amount of a provided compound. In some embodiments, the present invention provides a method for treating or preventing cancer in a subject suffering therefrom, comprising administering to a patient in need thereof a therapeutically effective amount of a provided compound.
    Type: Grant
    Filed: November 2, 2018
    Date of Patent: May 12, 2020
    Assignee: Memorial Sloan Kettering Cancer Center
    Inventors: Gabriela Chiosis, Yanlong Kang, Hardik J. Patel, Maulik Patel, Stefan Ochiana, Anna Rodina, Tony Taldone, Liza Shrestha
  • Patent number: 10633338
    Abstract: This invention provides compound having a structure of Formulas: Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provide.
    Type: Grant
    Filed: May 30, 2019
    Date of Patent: April 28, 2020
    Assignees: THE UNIVERSITY OF BRITISH COLUMBIA, SIMON FRASER UNIVERSITY
    Inventors: Paul Rennie, Artem Tcherkassov, Robert N. Young, Christophe M. Andre
  • Patent number: 10596179
    Abstract: Provided herein are methods of using compounds and compositions for treating, managing, and/or preventing systemic lupus erythematosus (SLE). Pharmaceutical compositions and dosing regimens for use in the methods are also provided herein.
    Type: Grant
    Filed: March 1, 2019
    Date of Patent: March 24, 2020
    Assignee: Celgene Corporation
    Inventors: Peter H. Schafer, Lei Wu, Ying Ye
  • Patent number: 10519141
    Abstract: Provided are a pyrimidine compound represented by Formula 1, a method of preparing the same, and a pharmaceutical use of the pyrimidine compound for the prevention or treatment of cancer.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: December 31, 2019
    Assignee: HANMI PHARM. CO., LTD.
    Inventors: Young Jin Ham, Seok Jong Kang, Jae Yul Choi, Seo Hee Kim, Tae Woo Kim, In Hwan Bae, Young Gil Ahn, Kwee Hyun Suh
  • Patent number: 10485769
    Abstract: In one embodiment, the invention provides methods of treatment which use therapeutically effective amounts of Cholesteryl Ester Transfer Protein (CETP) inhibitors to treat a variety of cancers. In certain embodiments, the inhibitor is a CETP-inhibiting small molecule, CETP-inhibiting antisense oligonucleotide, CETP-inhibiting siRNA or a CETP-inhibiting antibody. Related pharmaceutical compositions, kits, diagnostics and screens are also provided.
    Type: Grant
    Filed: February 23, 2016
    Date of Patent: November 26, 2019
    Assignee: King Abdullah University of Science and Technology
    Inventors: Mandeep Kaur, Luke E. Esau, Sunil Sagar
  • Patent number: 10464903
    Abstract: The present invention relates (i) to a process for the preparation of quinolin-2-yl-phenylamine derivatives of formula (I) without a metal catalyst, and (ii) to soluble mineral acid or sulfonic acid salts of (8-chloro-quinolin-2-yl)-(4-trifluoromethoxyphenyl)-amine.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: November 5, 2019
    Assignee: RATIOPHARM GMBH
    Inventors: Sebastian Rabe, Wolfgang Albrecht
  • Patent number: 10463672
    Abstract: Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed.
    Type: Grant
    Filed: December 28, 2017
    Date of Patent: November 5, 2019
    Assignee: Celgene Corporation
    Inventors: Benjamin M. Cohen, John F. Traverse, Jean Xu, Ying Li
  • Patent number: 10448637
    Abstract: Identification and evaluation of a set of first-in-class potent inhibitors targeting a new cancer target, Grb2-associated binder˜1 (GAB1), which integrates signals from different signaling pathways and is frequently over-expressed in cancer ceils. Intensive computational modeling is utilized to understand the structure of the GAB1 pleckstrin homology (PH) domain and screened five million compounds. Upon biological evaluation, several inhibitors were found that induced large conformational changes of the target structure exhibited strong selective binding to GAB1 PH domain. Particularly, these inhibitors demonstrated potent and tumor-specific cytotoxicity in breast cancer cells. This targeting GAB1 signaling may be used for cancer therapy, especially for triple negative breast cancer patients.
    Type: Grant
    Filed: October 5, 2015
    Date of Patent: October 22, 2019
    Assignees: Arizona Board of Regents on Behalf of the University of Arizona, The University of Texas System
    Inventors: Emmanuelle J. Meuillet, Shuxing Zhang, Lu Chen
  • Patent number: 10435367
    Abstract: Indirubin is the major active anti-tumor component of a traditional Chinese herbal medicine used for treatment of chronic myelogenous leukemia (CML). Indirubin derivatives (IRDs) potently reduce the viabilities of various cancer cells and affect kinase activities. IRDs disclosed herein provide new therapeutics for cancer and conditions regulated by the kinase activities.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: October 8, 2019
    Assignees: City of Hope, The National and Kapodistrian University of Athens
    Inventors: Sangkil Nam, Richard Jove, Leandros Skaltsounis
  • Patent number: 10383868
    Abstract: Provided herein are quinoline, pharmaceutical compositions thereof, and methods of their use for treating, preventing, or ameliorating one or more symptoms of an endoplasmic reticulum stress-caused disease. Also provided herein are methods of their use for reducing endoplasmic reticulum stress and modulating the activity of a sarcoplasmic/endoplasmic reticulum Ca2+ ATPase.
    Type: Grant
    Filed: November 27, 2016
    Date of Patent: August 20, 2019
    Inventor: Russell Dahl
  • Patent number: 10370333
    Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.
    Type: Grant
    Filed: February 5, 2018
    Date of Patent: August 6, 2019
    Assignee: SANFORD-BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
    Inventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D. P. Cosford, Jose Luis Millan
  • Patent number: 10358443
    Abstract: The present invention relates to certain heteroaryl amide compounds, pharmaceutical compositions containing them, and methods of using them, including methods for preventing, reversing, slowing, or inhibiting protein aggregation, and methods of treating diseases that are associated with protein aggregation, including neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, Lewy body disease, Parkinson's disease with dementia, fronto-temporal dementia, Huntington's Disease, amyotrophic lateral sclerosis, and multiple system atrophy, and cancer and melanoma.
    Type: Grant
    Filed: August 1, 2017
    Date of Patent: July 23, 2019
    Assignee: UCB Biopharma SPRL
    Inventors: Wolfgang Wrasidlo, Emily M. Stocking
  • Patent number: 10344026
    Abstract: Compounds and compositions are presented that inhibit K-Ras, and especially mutant K-Ras. Certain compounds preferentially or even selectively inhibit specific forms of mutant K-Ras, and particularly the G12D mutant form.
    Type: Grant
    Filed: January 18, 2018
    Date of Patent: July 9, 2019
    Assignee: NantBio, Inc.
    Inventors: Chunlin Tao, Laxman Nallan, David G. Ho, Qinwei Wang, Paul Weingarten, Anna B. Juncker-Jensen
  • Patent number: 10343991
    Abstract: The present invention describes the C5,C6 Substituted and/or fused oxindole compounds useful as anti-cancer agents and process for preparation thereof. Particularly the present invention relates to C5,C6 Substituted and/or fused oxindole compounds of formula I.
    Type: Grant
    Filed: November 2, 2017
    Date of Patent: July 9, 2019
    Assignee: Council of Scientific & Industrial Research
    Inventors: Raji Reddy Chada, Srigiridhar Kotamraju, Santosh Karnewar, Nagendra Babu Bathini, Nagarsenkar Atulya, Anuradha Singampalli
  • Patent number: 10300073
    Abstract: Provided are methods for the combined use of cyclin-dependent kinase 9 (CDK9) inhibitors and bromodomain containing 4 (BRD4) inhibitors to reduce, inhibit and/or prevent cartilage degradation and systemic traumatic inflammation. A combination of CDK9 inhibitors and BRD4 inhibitors can be used to reduce, inhibit and/or prevent cartilage degradation and loss of cartilage viability during allograft storage. A combination of CDK9 inhibitors and BRD4 inhibitors can be used as a post-injury intervention treatment to reduce, inhibit and/or prevent the acute cellular responses that lead to future cartilage degradation and osteoarthritis.
    Type: Grant
    Filed: October 13, 2015
    Date of Patent: May 28, 2019
    Assignee: The Regents of the University of California
    Inventors: Dominik Haudenschild, Jasper Yik
  • Patent number: 10246457
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R7, R8 and R9 are as herein described. The present invention also provides pharmaceutical compositions comprising these compounds and methods for their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the treatment of Btk mediated disorders.
    Type: Grant
    Filed: April 4, 2016
    Date of Patent: April 2, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tony Siu, Michael D. Altman, Brian M. Andresen, Jian Liu, Joseph Kozlowski, Sobhana Babu Boga, Younong Yu, Rajan Anand, Jiaqiang Cai, Dahai Wang, Shilan Liu
  • Patent number: 10245266
    Abstract: Provided herein are methods of using compounds and compositions for treating, managing, and/or preventing systemic lupus erythematosus (SLE). Pharmaceutical compositions and dosing regimens for use in the methods are also provided herein.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: April 2, 2019
    Assignee: Celgene Corporation
    Inventors: Peter H. Schafer, Lei Wu, Ying Ye
  • Patent number: 10245270
    Abstract: 3-[(3-{[4-(4-morpholinylmethyl)-1H-pyrrol-2-yl]methylene}-2-oxo-2,3-dihydro-1H-indol-5-yl)methyl]-1,3-thiazolidine-2,4-dione methanesulphonate of formula (II): Medicinal products containing the same which are useful in treating cancer.
    Type: Grant
    Filed: September 4, 2018
    Date of Patent: April 2, 2019
    Assignee: LES LABORATOIRES SERVIER
    Inventors: Alexandre Le Flohic, Jérôme Guidotti, Philippe Letellier
  • Patent number: 10220041
    Abstract: The present invention relates to methods of inducing the self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair cells. Specifically, the invention relates to methods of using compounds comprising a 3-(pyridin-2-yl)-1H-indol-2-ol containing moiety having a Formula I: and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 10, 2018
    Date of Patent: March 5, 2019
    Assignee: Frequency Therapeutics, Inc.
    Inventors: Christopher Loose, Will McLean, Melissa Hill-Drzewi
  • Patent number: 10214502
    Abstract: This invention offers an effective method of decreasing expression of apolipoprotein E and increasing expression of at least one of either LDL-receptor protein or AbcA1 protein including selecting mammalian cells expressing apoE and at least one of either LDL-receptor protein or AbcA1 protein, contacting the mammalian cell with an effective amount of a compound having general formula (I) or general formula (II) in an amount sufficient to decrease expression of the apoE and increase expression of at least one of the LDL-receptor protein or the AbcA1 protein in the mammalian cell.
    Type: Grant
    Filed: October 4, 2016
    Date of Patent: February 26, 2019
    Assignees: Mayo Foundation for Medical Education and Research, California State University, Fresno
    Inventors: Santanu Maitra, Jungsu Kim
  • Patent number: 10201547
    Abstract: The invention comprises a method of treatment of aggression and similar behavioral syndromes, such as impulsivity and irritability, by a pharmaceutical agent exhibiting combined D2 and D5 antagonistic activity.
    Type: Grant
    Filed: July 26, 2018
    Date of Patent: February 12, 2019
    Assignee: Supernus Pharmaceuticals, Inc.
    Inventor: Christopher D. Breder
  • Patent number: 10155001
    Abstract: The invention relates to a Rac1 inhibitor for use as bronchodilator in a patient in need thereof. The invention provides a Rac1 inhibitor for use in a method for inducing bronchodilation in a patient in need thereof. The invention also relates to a Rac1 inhibitor for use in a method for reducing AHR in a patient in need thereof.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: December 18, 2018
    Assignees: INSERM (Institut National de la Sante et de la Recherche Medicale), Centre National de la Recherche Scientifique (CNRS), Universite de Nantes, Centre Hospitalier Universitaire de Nantes
    Inventors: Vincent Sauzeau, Gwennan Andre, Gervaise Loirand, Antoine Magnan, David Lair
  • Patent number: 10092567
    Abstract: The invention provides combinations comprising a) compound of formula I: or a pharmaceutically acceptable salt thereof wherein R1, R2, R5, R10, and A have any of the values defined in the specification; and b) one or more agents selected from 5-FU, a platinum agent, leucovorin, irinotecan, docetaxel, doxorubicin, gemcitabine, SN-38, capecitabine, temozolomide, paclitaxel, bevacizumab, pertuzumab, tamoxifen, rapamycin and lapatinib. The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.
    Type: Grant
    Filed: February 21, 2017
    Date of Patent: October 9, 2018
    Assignee: GENENTECH, INC.
    Inventors: Kui Lin, Michelle Nannini, Elizabeth Punnoose, Deepak Sampath, Jeffrey Wallin, Premal Patel
  • Patent number: 10071089
    Abstract: The present invention is concerned with an oral pharmaceutical dosage form comprising oxycodone or a pharmaceutically acceptable salt thereof and naloxone or a pharmaceutically acceptable salt thereof for use in the treatment of pain in patients suffering from i) pain and at least one further disease ii), wherein said at least one further disease ii) results in intestinal dysbiosis, or for use in the treatment of pain in patients suffering from i) pain and at least one further disease iii), wherein said at least one further disease iii) increases the risk for intestinal bacterial translocation and thus for peritonitis, SIRS and/or sepsis.
    Type: Grant
    Filed: July 23, 2014
    Date of Patent: September 11, 2018
    Assignee: Euro-Celtique S.A.
    Inventors: Yvonne Von Coburg, Karen Reimer, Alexander Oksche, Peter Holzer
  • Patent number: 10058556
    Abstract: The invention comprises a method of treatment of aggression and similar behavioral syndromes, such as impulsivity and irritability, by a pharmaceutical agent exhibiting combined D2 and D5 antagonistic activity.
    Type: Grant
    Filed: October 12, 2017
    Date of Patent: August 28, 2018
    Assignee: SUPERNUS PHARMACEUTICALS, INC.
    Inventor: Christopher D. Breder