Spiro Ring System Patents (Class 514/278)
  • Patent number: 11512044
    Abstract: Disclosed is a method for preparing salicylamine acetate. The method comprises the steps of: (1) carrying out amino protection on salicylaldehyde having a structure represented by formula 1 to obtain a compound having a structure represented by formula 2; and (2) carrying out acid hydrolysis to the compound having a structure represented by formula 2 and then reacting the acid-hydrolyzed compound with acetic acid to obtain salicylamine acetate.
    Type: Grant
    Filed: November 26, 2018
    Date of Patent: November 29, 2022
    Assignee: TSI GROUP CO., LTD.
    Inventor: Ling Long
  • Patent number: 11464734
    Abstract: The present application provides methods of treating overactive bladder and methods of training or retraining bladder, prolonging symptom relief, improving the quality of life and/or neuronal remodeling in an individual having overactive bladder, by administering an effective amount of trospium locally to the bladder of the individual for at least about 24 hours.
    Type: Grant
    Filed: July 31, 2019
    Date of Patent: October 11, 2022
    Assignee: TARIS BIOMEDICAL LLC
    Inventor: Dennis Giesing
  • Patent number: 11447466
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: Y is Formula (II), or Formula (III); R1, R2, R2a, R2b, R2c, R3, R4, R5, m, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
    Type: Grant
    Filed: August 3, 2018
    Date of Patent: September 20, 2022
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alaric J. Dyckman, Dharmpal S. Dodd, Tasir Shamsul Haque, Brian K. Whiteley, John L. Gilmore
  • Patent number: 11377396
    Abstract: This invention provides enantioenriched Mannich adducts with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): comprising treating a compound of formula (II): with a transition metal catalyst under alkylation conditions.
    Type: Grant
    Filed: September 23, 2019
    Date of Patent: July 5, 2022
    Assignee: California Institute of Technology
    Inventors: Brian M. Stoltz, Yoshitaka Numajiri, Beau P. Pritchett, Koji Chiyoda
  • Patent number: 11358965
    Abstract: Provided herein are compounds that modulate EGFR and methods of using the same, for example to treat cancer.
    Type: Grant
    Filed: February 25, 2019
    Date of Patent: June 14, 2022
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Mukesh K. Nyati, Theodore S. Lawrence, Christopher Whitehead, Jason Christopher Rech, Brennan Taylor Watch
  • Patent number: 11325909
    Abstract: The invention provides the tris salt of 4-(4-(1-isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4?-piperidine]-1?-carbonyl)-6-methoxypyridin-2-yl)benzoic acid as a crystalline anhydrous or tri-hydrate; as well as polymorphs, pharmaceutical compositions, dosage forms, and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase (ACC) enzyme(s) in an animal.
    Type: Grant
    Filed: November 14, 2018
    Date of Patent: May 10, 2022
    Assignee: Pfizer Inc.
    Inventors: Dilinie Fernando, Shawn Marie LaCasse, Kristin Elizabeth Price Wiglesworth
  • Patent number: 11312701
    Abstract: Formylpyridine derivatives having FGFR4 inhibitory activities, a preparation method therefor and use thereof are described. In particular, the formylpyridine derivatives have a structure of formula (I), and the definition of each substituent in the formula are described in the description and claims. The series of compounds of the formula (I) have very strong inhibitory effects on FGFR4 kinases and very high selectivity, and can be widely used in the preparation of medicaments for treating cancers, particularly prostate cancer, liver cancer, pancreatic cancer, esophageal cancer, stomach cancer, lung cancer, breast cancer, ovarian cancer, colon cancer, skin cancer, neuroglioblastoma or rhabdomyosarcoma, and prospectively will be further developed to become a new generation of FGFR4 inhibitors.
    Type: Grant
    Filed: August 1, 2018
    Date of Patent: April 26, 2022
    Assignee: ABBISKO THERAPEUTICS CO., LTD
    Inventors: Haibing Deng, Fei Yang, Hongping Yu, Zhui Chen, Yaochang Xu
  • Patent number: 11254689
    Abstract: The invention relates to compounds of Formula (I) and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by mycobacterium, such as tuberculosis.
    Type: Grant
    Filed: August 15, 2018
    Date of Patent: February 22, 2022
    Assignees: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED, BIOVERSYS AG
    Inventors: Esther Porras De Francisco, Modesto Jesús Remuiñan-Blanco, Marilyne Bourotte, Benoit Deprez, Nicolas Willand
  • Patent number: 11234943
    Abstract: Micronized trans-resveratrol is provided in 50-200 mg unit dosage form for use as a single unit dose daily for administration to human patients the treatment or prevention of non-alcoholic fatty liver disease and/or for the treatment, prevention or reversal of non-alcoholic hepatic steatosis, e.g. for administration to patients exhibiting evidence of fatty liver on ultrasonography. A reported study shows the effects of resveratrol micronized formulation in reducing the liver fat, decreasing hepatic enzymes, serum glutamate pyruvic transaminase (SGPT) and gamma-glutamyl transpeptidase (g-GT) and decreasing insulin resistance. At the end of the study, statistical analysis showed a strongly statistically significant reduction in the liver fat, which in some patients continued for an extended period after treatment was discontinued.
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: February 1, 2022
    Inventor: Marios Andreou Theodotou
  • Patent number: 11230549
    Abstract: Disclosed are a series of quinolino-pyrrolidin-2-one compounds, and application thereof in preparation of drugs for ATM inhibitor-related diseases. The present disclosure specifically relates to a derivative compound represented by formula (I), tautomers thereof or pharmaceutically acceptable compositions thereof.
    Type: Grant
    Filed: September 27, 2019
    Date of Patent: January 25, 2022
    Assignee: MEDSHINE DISCOVERY INC.
    Inventors: Wenyuan Qian, Chundao Yang, Guoqiang Dai, Jian Li, Shuhui Chen
  • Patent number: 11202776
    Abstract: Provided herein is a method of treating or alleviating one or more symptoms of a disorder, disease, or condition mediated by a dopamine D2 or D3 receptor with 3-((1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoic acid or a pharmaceutically acceptable salt thereof. Also provided herein is a method of increasing the serum prolactin level with 3-((1-cyclohexyl-4-oxo-8-(4-oxo-4-phenylbutyl)-1,3,8-triazaspiro[4.5]decan-3-yl)methyl)benzoic acid or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 11, 2018
    Date of Patent: December 21, 2021
    Inventor: Emil Chuang
  • Patent number: 11124505
    Abstract: The disclosure provides a process of making the compound of Formula I, and pharmaceutically acceptable salts thereof: and the process of making the intermediate of Formula III: wherein PG is as defined as set forth in the specification.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: September 21, 2021
    Assignee: Minoryx Therapeutics S.L.
    Inventors: Ana Maria García Collazo, Wolter Ten Hoeve, Johannes Nicolaas Koek, Johannes B. M. Rewinkel, Sander De Wilde
  • Patent number: 11103506
    Abstract: The present invention relates to combinations comprising a positive allosteric modulator (“PAM”) of metabotropic glutamatergic receptor subtype 2 (“mGluR2”) or a pharmaceutically acceptable salt or a solvate thereof, or an orthosteric agonist of metabotropic glutamatergic receptor subtype 2 compound or a pharmaceutically acceptable salt or a solvate thereof, and a synaptic vesicle protein 2A (“SV2A”) ligand.
    Type: Grant
    Filed: December 19, 2019
    Date of Patent: August 31, 2021
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Brian D. Klein, Hilde Lavreysen, Stefan Maria Christiaan Pype, Roy E. Twyman, Nancy Eulalie Sylvain Van Osselaer, H. Steven White, Marc André Ceusters, José Maria Cid-Núñez, Andrés Avelino Trabanco-Suárez
  • Patent number: 11059766
    Abstract: The present invention relates to ethynyl derivatives of formula I with variables as defined herein, or to a pharmaceutically acceptable acid addition salt thereof. Compounds of formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Grant
    Filed: December 1, 2017
    Date of Patent: July 13, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Eric Vieira
  • Patent number: 11052080
    Abstract: The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3? or GSK3?) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychiatric disorders, metabolic disorders, and cancer.
    Type: Grant
    Filed: November 21, 2018
    Date of Patent: July 6, 2021
    Assignees: The Broad Institute, Inc., Dana-Farber Cancer Institute, Inc., The General Hospital Corporation
    Inventors: Florence Fevrier Wagner, Jennifer Q. Pan, Sivaraman Dandapani, Andrew Germain, Edward Holson, Benito Munoz, Partha P. Nag, Michael C. Lewis, Stephen J. Haggarty, Joshua A. Bishop, Kimberly Stegmaier, Michel Weiwer, Versha Banerji
  • Patent number: 10981910
    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: June 26, 2020
    Date of Patent: April 20, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guanglin Luo, Carolyn Diane Dzierba, John E. Macor
  • Patent number: 10968178
    Abstract: The present invention aims to provide a heterocyclic compound having an IP6K inhibitory action and expected to be useful as a prophylactic or therapeutic agent for—diseases such as cardiac failure, diabetes and the like. A compound represented by the formula (I): wherein each symbol is as defined in the SPECIFICATION, or a salt thereof has an IP6K inhibitory action and is expected to be useful as a prophylactic or therapeutic agent for diseases such as cardiac failure, diabetes and the like.
    Type: Grant
    Filed: March 29, 2018
    Date of Patent: April 6, 2021
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Yoshito Terao, Masashi Takahashi, Ryoma Hara, Kousuke Hidaka, Hideki Furukawa, Takeshi Yamasaki, Shizuo Kasai
  • Patent number: 10960005
    Abstract: Methods are provided for the treatment of relapsed and/or refractory solid tumors (including neuroendocrine carcinomas (NEC)) and non-Hodgkin's lymphomas (NHLs) and the like, using substituted heterocyclic derivative compounds and pharmaceutical compositions comprising compounds useful for the inhibition of lysine specific demethylase-1 (LSD-1).
    Type: Grant
    Filed: June 10, 2020
    Date of Patent: March 30, 2021
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Jiangchun Xu, Robert Cho, Aaron Nguyen
  • Patent number: 10961244
    Abstract: The present invention provides a compound having the structure: or a pharmaceutically acceptable salt or ester thereof, and a method of treating a subject afflicted with pain, a depressive disorder, a mood disorder or an anxiety disorder by administering the compound to the subject.
    Type: Grant
    Filed: March 24, 2017
    Date of Patent: March 30, 2021
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Andrew Kruegel, Dalibor Sames, Madalee G. Wulf, Jonathan A. Javitch
  • Patent number: 10934269
    Abstract: The present invention relates to a process for the preparation of apalutamide. In particular, the present invention relates to a process for the preparation of apalutamide and its intermediates. The present invention also relates to pharmaceutical compositions comprising apalutamide.
    Type: Grant
    Filed: September 27, 2019
    Date of Patent: March 2, 2021
    Assignee: CADILA HEALTHCARE LIMITED
    Inventors: Kumar Kamlesh Singh, Nikhil Amar Singh, Ganpatdan Shimbhu Charan, Nimeshkumar Mukeshkumar Shah
  • Patent number: 10906874
    Abstract: Binding of the transcriptional co-activator, YAP1, to the transcription factor Oct4, induces Sox2, which is a transcription actor necessary for the self-renewal of stem-like cells from non-small cell lung cancer. The WW domain of YAP1 binds to the PPxY motif of Oct4 to induce Sox2. Delivering a peptide corresponding to the WAV domain could prevent the induction of Sox2 and stemness. Similarly, peptides and mimetics of the PPxY motif would be able to inhibit stemness. Disclosed are compounds that affect the Yap1:Oct4 interaction.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: February 2, 2021
    Assignee: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
    Inventors: Srikumar Chellappan, Nicholas J. Lawrence, Sujeewa Ranatunga Mahanthe Mudiyanselage
  • Patent number: 10874649
    Abstract: The present invention is directed to inhibitors of histone deacetylases (HDACs) such as HDAC6, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.
    Type: Grant
    Filed: December 18, 2019
    Date of Patent: December 29, 2020
    Assignee: Valo Early Discovery, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Mary-Margaret Zablocki
  • Patent number: 10875848
    Abstract: The present disclosure is directed to inhibitors of FASN. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of FASN. For instance, the disclosure is concerned with compounds and compositions for inhibition of FASN, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of FASN, and methods of synthesis of these compounds.
    Type: Grant
    Filed: October 10, 2019
    Date of Patent: December 29, 2020
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Matthew W. Martin, Mary-Margaret Zablocki, Scot Mente, Christopher Dinsmore, Zhongguo Wang, Xiaozhang Zheng
  • Patent number: 10858373
    Abstract: The present invention provides, in part, heterocyclic spiro compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.
    Type: Grant
    Filed: June 3, 2019
    Date of Patent: December 8, 2020
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Laura Ann McAllister, Christopher John Helal, Steven Victor O'Neil, Patrick Robert Verhoest
  • Patent number: 10822335
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Grant
    Filed: April 1, 2019
    Date of Patent: November 3, 2020
    Assignee: Pfizer Inc.
    Inventors: Mary Theresa Didiuk, Robert Lee Dow, David Andrew Griffith
  • Patent number: 10779537
    Abstract: In crop production in the fields of agriculture, horticulture and the like, the damage caused by insect pests etc. is still immense, and insect pests resistant to existing insecticides have emerged. Under such circumstances, the development of novel agricultural and horticultural insecticides is desired. The present invention provides an agricultural and horticultural insecticide comprising a 1H-pyrrolo-condensed heterocyclic compound represented by the general formula (1): {wherein A and A1 each represent a nitrogen atom, R3 and R4 each represent a haloalkyl group, R2 represents a hydrogen atom or an acetyl group, R1 represents a halogen atom, and m represents 0 or 2}, an N-oxide thereof or a salt thereof as an active ingredient, and a method for using the insecticide.
    Type: Grant
    Filed: October 12, 2017
    Date of Patent: September 22, 2020
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Yusuke Sano, Ikki Yonemura, Akiyuki Suwa, Shunpei Fujie
  • Patent number: 10759788
    Abstract: Pharmaceutical uses of pyridinecarboxamide derivatives are provided. In particular, pharmaceutical uses of pyridinecarboxamide derivatives represented by general formula (I), wherein the substituents of the formula (I) are defined in the specification, are provided. The pyridinecarboxamide derivatives can be used as therapeutic agents, especially as inhibitors of the Renal Outer Medullary Potassium channel (ROMK) and in the preparation of medicaments for treating and/or preventing ROMK mediated disorders, such as hypertension and heart failure.
    Type: Grant
    Filed: January 25, 2019
    Date of Patent: September 1, 2020
    Assignees: JIANGSU HENGRUI MEDICINE CO., LTD., SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD.
    Inventors: Xin Li, Qing Dong, Piaoyang Sun
  • Patent number: 10702508
    Abstract: Described herein are methods of treating non-metastatic castrate-resistant prostate cancer using an approved drug product comprising apalutamide, enzalutamide or darolutamide. Also described here are drug products containing apalutamide enzalutamide or darolutamide, and methods of selling or offering for sale an anti-androgen drug product.
    Type: Grant
    Filed: April 30, 2018
    Date of Patent: July 7, 2020
    Assignee: Aragon Pharmaceuticals, Inc.
    Inventor: Arturo Molina
  • Patent number: 10689368
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof, wherein Q, R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: July 1, 2019
    Date of Patent: June 23, 2020
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Julie Elaine Cansfield, Miles Stuart Congreve, Michael Alistair O'Brien, Mark Pickworth, Mark David Rackham, Benjamin Gerald Tehan, Barry John Teobald
  • Patent number: 10633384
    Abstract: Compounds having the general formula (I) wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.
    Type: Grant
    Filed: October 13, 2016
    Date of Patent: April 28, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Patrizio Mattei, Harald Mauser, Marco Prunotto, Christoph Ullmer
  • Patent number: 10626125
    Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.
    Type: Grant
    Filed: May 23, 2019
    Date of Patent: April 21, 2020
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Laura Ann McAllister, Christopher John Helal, Steven Victor O'Neil, Patrick Robert Verhoest
  • Patent number: 10538530
    Abstract: Compounds are provided that antagonize vasopressin receptors, particularly the V1a receptor products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof: wherein Q1, Q2, Q3, R2a, R2b, R3 and X are as defined herein.
    Type: Grant
    Filed: September 5, 2018
    Date of Patent: January 21, 2020
    Assignee: BlackThorn Therapeutics, Inc.
    Inventors: Robert M. Jones, Mariangela Urbano, Gary Brandt, Mark Chambers, David Hardick, Chris Knight, Jason Tierney, Chris Lock
  • Patent number: 10479796
    Abstract: The present invention provides spiro-oxazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.
    Type: Grant
    Filed: June 6, 2016
    Date of Patent: November 19, 2019
    Assignee: Hoffman-La Roche Inc.
    Inventors: Valerie Runtz-Schmitt, Patrick Schnider, Cosimo Dolente, Bernhard Fasching
  • Patent number: 10428088
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where m, p, q, W, Z, Y, X1, X2, R1, R2, R3 and R4 are as defined herein.
    Type: Grant
    Filed: May 23, 2018
    Date of Patent: October 1, 2019
    Assignee: Heptares Therapeutics Limited
    Inventors: Miles Stuart Congreve, Giles Albert Brown, Benjamin Gerald Tehan, Mark Pickworth, Julie Elaine Cansfield
  • Patent number: 10407428
    Abstract: The present invention relates to spiro-isoquinoline-1,4?-piperidine compounds having dual pharmacological activity towards both the sigma (?) receptor and the ?-opiod receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
    Type: Grant
    Filed: November 20, 2015
    Date of Patent: September 10, 2019
    Assignee: ESTEVE PHARMACEUTICALS, S.A.
    Inventors: Carmen Almansa-Rosales, Monica Garcia Lopez, Ana-Maria Caamano-Moure
  • Patent number: 10329308
    Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating MAGL-mediated diseases and disorders including, e.g., pain, an inflammatory disorder, depression, anxiety, Alzheimer's disease, a metabolic disorder, stroke, or cancer.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: June 25, 2019
    Assignee: Pfizer Inc.
    Inventors: Michael Aaron Brodney, Christopher Ryan Butler, Laura Ann McAllister, Christopher John Helal, Steven Victor O'Neil, Patrick Robert Verhoest
  • Patent number: 10294225
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3, Z, A1, L and A2 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Grant
    Filed: January 30, 2018
    Date of Patent: May 21, 2019
    Assignee: Pfizer Inc.
    Inventors: Mary Didiuk, Robert Lee Dow, David Andrew Griffith
  • Patent number: 10246459
    Abstract: Use of a tetramic acid compound according to formula (I) or (I?) with a second nematicide as a treatment for crop plants to combat and control nematodes in the soil of said crop plants.
    Type: Grant
    Filed: October 11, 2017
    Date of Patent: April 2, 2019
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Fabienne Hatt, Anke Buchholz
  • Patent number: 10233158
    Abstract: The present invention relates to the compound of the formula: or pharmaceutically acceptable salts thereof, as well as compositions containing the same, processes for the preparation of the same, and therapeutic methods of use therefore in promoting hydration of mucosal surfaces and the treatment of diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchiectasis, acute and chronic bronchitis, cystic fibrosis, emphysema, and pneumonia.
    Type: Grant
    Filed: April 4, 2018
    Date of Patent: March 19, 2019
    Assignee: Parion Sciences, Inc.
    Inventor: Michael R. Johnson
  • Patent number: 10226459
    Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: March 12, 2019
    Assignees: Incyte Holdings Corporation, Incyte Corporation
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian W. Metcalf
  • Patent number: 10220025
    Abstract: A solid self-micro/nano emulsifying formulation comprising CARP-1 functional mimetics (CFM; e.g., CFM-4.16 or CFM-4.17) for oral administration, and methods of fabrication and use thereof to treat cancer (e.g., breast cancer, triple negative breast cancer, resistant lung cancer, and non-resistant lung cancer) and reduce tumor volume. Solid self-micro/nano emulsifying formulation of CFM compounds was found to have significantly enhanced drug loading, aqueous solubility, and oral bioavailability of the formulation.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: March 5, 2019
    Assignee: Florida A&M University
    Inventors: Mandip Sachdeva, Ketankumar Patel, Arun Rishi
  • Patent number: 10220091
    Abstract: Methods for treating cancer using a combination of an inhibitor of the sonic hedgehog signaling pathway (e.g., LDE225) with radiation and a tumor antigen-specific monoclonal antibody (e.g., heat shock protein (HSP) glucose regulated protein of 94000 daltons (Grp94)-specific mAb W9, or chondroitin sulfate proteoglycan 4 (CSPG4)-targeted mAbs), or with a BRAF inhibitor, e.g., in BRAF inhibitor resistant cancers.
    Type: Grant
    Filed: April 3, 2014
    Date of Patent: March 5, 2019
    Assignee: The General Hospital Corporation
    Inventors: Francesco Sabbatino, Yangyang Wang, Xinhui Wang, Steven Isakoff, Cristina Ferrone, Joe Schwab, Soldano Ferrone
  • Patent number: 10196369
    Abstract: Provided herein are small molecule Epstein-Barr virus-induced G-protein coupled receptor 2 (EBI2) modulator compounds, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds. In some embodiments, EBI2 is a therapeutic target for the treatment of diseases or conditions such as, but not limited to, autoimmune diseases or conditions, cancer, and cardiovascular disease.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: February 5, 2019
    Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
    Inventors: Anthony B. Pinkerton, Robert Ardecky, Eduard A. Sergienko, Marcos Gonzalez-Lopez, Santhi Reddy Ganji, Jiwen Zou
  • Patent number: 10183963
    Abstract: The present invention relates to methods of treating immune disorders and/or inflammation using certain modulator compounds. In one embodiment, the present invention provides a method of treating an immune and inflammatory disorders disorder by administering a composition comprising a therapeutically effective dosage of an ascaroside compound, or a mixture of ascaroside compounds, or a mixture containing at least one ascaroside.
    Type: Grant
    Filed: December 6, 2017
    Date of Patent: January 22, 2019
    Assignees: California Institute of Technology, Boyce Thompson Institute for Plant Research
    Inventors: Andrea Choe, Paul W. Sternberg, Frank C. Schroeder, Stephan H. Von Reuss
  • Patent number: 10174052
    Abstract: There are disclosed a series of quinuclidines having the Formula (I), which bind to the nicotinic ?7 receptor and may be useful for the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: November 3, 2015
    Date of Patent: January 8, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: James H. Cook, II, F. Christopher Zusi, Matthew D. Hill
  • Patent number: 10174050
    Abstract: The present invention concerns a spiroisoxazoline compound of general formula (I): in which m and n are 0 or 1, R1 represents, inter alia, an optionally substituted alkyl chain, in particular substituted with fluorine or with a cyclic group, and R2 is chosen from phenyl and optionally substituted benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and the heterocycles having 5 or 6 vertices comprising at least one atom chosen from S, N and O. The present invention also concerns the use of this compound as a drug, in particular in the treatment of bacterial and mycobacterial infections such as tuberculosis in combination with an antibiotic that is active against bacteria and/or mycobacteria, said compound potentiating the activity of said antibiotic.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: January 8, 2019
    Assignee: Universite de Droit et de la Sante de Lille 2
    Inventors: Nicolas Willand, Benoit Deprez, Alain Baulard, Priscille Brodin, Matthieu Frederik Desroses, Laurence Agouridas-Dutot
  • Patent number: 10172838
    Abstract: A solid self-micro/nano emulsifying formulation comprising CARP-1 functional mimetics (CFM; e.g., CFM-4.16 or CFM-4.17) for oral administration, and methods of fabrication and use thereof to treat cancer (e.g., breast cancer, triple negative breast cancer, resistant lung cancer, and non-resistant lung cancer) and reduce tumor volume. Solid self-micro/nano emulsifying formulation of CFM compounds was found to have significantly enhanced drug loading, aqueous solubility, and oral bioavailability of the formulation.
    Type: Grant
    Filed: March 15, 2017
    Date of Patent: January 8, 2019
    Assignee: Florida A&M University
    Inventors: Mandip Sachdeva, Ketankumar Patel, Arun Rishi
  • Patent number: 10150769
    Abstract: Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: June 12, 2018
    Date of Patent: December 11, 2018
    Assignee: Aptinyx Inc.
    Inventor: M. Amin Khan
  • Patent number: 10072017
    Abstract: The invention relates to a compound of Formula I or IA compositions comprising compounds of Formula I or IA, and methods of treating 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: December 28, 2016
    Date of Patent: September 11, 2018
    Assignee: Flatley Discovery Lab, LLC
    Inventors: Michael P. Zawistoski, Asmita Deshpande, Bridget M. Cole
  • Patent number: 10035816
    Abstract: The present invention declares a kind of compound to treat respiratory syncytial virus infection and its preparation method and application. The compound stated is cyclopamine's chemical analogs, has the property of inhibiting respiratory syncytial virus replication, and does not have the property of inhibiting Hedgehog signaling pathways. The preparation method stated is to get the cyclopamine's chemical analogs through drug chemical synthesis, then to screen the analogs with two parallel in vitro experiment. The compound described can be used to treat respiratory virus infection, paramyxovirus, respiratory syncytial virus infection, capillary bronchitis/pneumonia/tympanitis caused by respiratory syncytial virus. Furthermore, the compound described never cause the side effects of fetal malformation, and it overcame the teratogenicity of cyclopamine, and filled the gap of anti-human respiratory syncytial virus drug, especially of the field of pediatric drug.
    Type: Grant
    Filed: December 7, 2017
    Date of Patent: July 31, 2018
    Assignee: SHANDONG UNIVERSITY
    Inventors: Ralf Altmeyer, Jingjing Cao