Patents Examined by Karen Cheng
  • Solid state forms of spiro-oxindole compounds
    Patent number: 10118932
    Abstract: The present invention provides solid state forms of certain spiro-oxindole compounds, such as funapide and the racemic mixture of funapide and its corresponding (R) enantiomer, pharmaceutical compositions comprising the solid state forms and processes for preparing the solid state forms and the pharmaceutical compositions.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: November 6, 2018
    Assignee: Xenon Pharmaceuticals Inc.
    Inventors: Ronen Ben-David, Stephen Bierlmaier, Ralph Curtis Haltiwanger, Alexandr Jegorov, Raeann Ruiyun Wu, Mehran Yazdanian
  • Nonanoic and decanoic acid derivatives and uses thereof
    Patent number: 10118929
    Abstract: The present disclosure relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present disclosure also relates to pharmaceutical compositions containing the fluorinated compounds of the disclosure, and methods of treating fibrosis, macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: November 6, 2018
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Takeru Furuya, Ben C. Askew
  • Methods for producing optically active valeric acid derivatives
    Patent number: 10112908
    Abstract: A method for producing a compound (4), which comprises allowing a compound (1) to react with hydrogen gas in an inert solvent, in the presence of a specific chiral ligand and a ruthenium catalyst, or in the presence of an asymmetric transition metal complex catalyst previously generated from the chiral ligand and the ruthenium catalyst.
    Type: Grant
    Filed: September 17, 2015
    Date of Patent: October 30, 2018
    Assignee: DAICHI SANKYO COMPANY, LIMITED
    Inventors: Masaki Hayashi, Kazutoshi Ukai
  • Indazolyl thiadiazolamines and related compounds for inhibition of Rho-associated protein kinase and the treatment of disease
    Patent number: 10112935
    Abstract: The invention provides indazolyl thiadiazolamines and related compounds, pharmaceutical compositions, methods of inhibiting Rho-associated protein kinase, and methods of treating inflammatory disorders, immune disorders, fibrotic disorders, and other medical disorders using such compounds. An exemplary indazolyl thiadiazolamine compound is an N-(5-[5-[(1H4ndazol-5-yl)amino]-1,3,4-thiadiazol-2-yl]pyridin-3-yl)acetamide compound.
    Type: Grant
    Filed: February 26, 2016
    Date of Patent: October 30, 2018
    Assignee: Lycera Corporation
    Inventors: Thomas Daniel Aicher, Fernando Padilla, Peter L. Toogood, Shoujun Chen
  • Coumarinyl-thiazole-sulfonyl conjugate and preparation thereof
    Patent number: 10093667
    Abstract: The present application relates to a compound of formula (I) The present application also relates to synthesizing the compound of formula I and treating a patient with the compound of formula I having a neuropsychiatric illnesses such as a depressive disorder, schizophrenia; alcohol, nicotine, and morphine withdrawal induced depression and hyperalgesia; neuropathic pain caused by anticancerous drugs; diabetic neuropathic pain; obsessive compulsive disorder; alcohol withdrawal syndrome; static and dynamic allodynia in diabetic and cancer patients on anticancer therapy and chronic pain therapy.
    Type: Grant
    Filed: October 13, 2017
    Date of Patent: October 9, 2018
    Assignees: COMSATS Institute of Information Technology, Quaid-I-Azam University
    Inventors: Aamer Saeed, Khalid Rauf, Yasser M S A Alkahraman
  • Beta-lactamase inhibitors and uses thereof
    Patent number: 10085999
    Abstract: ?-Lactamase inhibiting compounds, therapeutic methods of using the ?-lactamase inhibiting compounds, particularly in combination with ?-lactam antibiotics and pharmaceutical compositions thereof are disclosed. The ?-lactamase inhibiting compounds are suitable for oral administration.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: October 2, 2018
    Assignee: ARIXA PHARMACEUTICALS, INC.
    Inventors: Eric M. Gordon, John Freund, Mark A. Gallop, Matthew Alexander James Duncton
  • Process for the preparation of aclidinium bromide
    Patent number: 10087177
    Abstract: A process for preparing (3R)-3-[2-Hydroxy(di-2-thienyl)acetoxy]-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide) comprises reacting 2-hydroxy-2,2-dithien-2-ylacetic acid 1-azabicyclo[2.2.2]oct-3(R) yl methyl ester and 3-phenoxypropyl bromide, wherein the reaction takes place in a solvent or mixture of solvents selected from the group of amides and/or the group of solvents with a sulfoxide group. Also provided is a crystalline aclidinium bromide characterized by a powder XRPD pattern having peaks at 7.7±0.2° 2?, 10.4±0.2° 2?, 13.2±0.2° 2?, 13.8±0.2° 2?, 19.9±0.2° 2?, 20.3±0.2° 2?, 20.8±0.2° 2?, 24.2±0.2° 2?, 25.7±0.2° 2?, 26.1±0.2° 2?, 29.2±0.2° 2?, 30.8±0.2° 2?. A pharmaceutical composition comprises aclidinium bromide according to the invention and a pharmaceutically acceptable excipient.
    Type: Grant
    Filed: March 30, 2016
    Date of Patent: October 2, 2018
    Assignee: Hovione Scientia Limited
    Inventors: Zita Mendes, Constança Cacela, Ana Carina Constantino, Bruno Santos
  • Compounds and their methods of use
    Patent number: 10087172
    Abstract: Provided are compounds of formula (I), which can inhibit glutaminase. Pharmaceutical compositions comprising these compounds and uses as glutaminase inhibitors for treating cancers thereof are also provided.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: October 2, 2018
    Assignee: AGIOS PHARMACEUTICALS, INC.
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Yongsheng Chen
  • Trisubstituted benzotriazole derivatives as dihydroorotate oxygenase inhibitors
    Patent number: 10080740
    Abstract: The present invention provides methods for treating a cancer in a subject and for inhibiting tumor growth, metastasis or a dihydrorotate oxygenase enzyme activity of a tumor or cancer cell. At least one trisubstituted benzotriazole derivative with the formula (I) is administered to the subject or is contacted with the cancer cell. Compounds of formula (I) have substituents R1, R2 and R3 which have the meanings given in the specification, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: September 25, 2018
    Assignee: Aurigene Discovery Technologies Limited
    Inventors: Siva Sanjeeva Rao Thunuguntla, Subramanya Hosahalli, Satish Reddy Kunnam
  • N-cycloalkyl-N-{[2-(1-substitutedcycloalkyl)phenyl]methylene}-(thio)carboxamide derivatives
    Patent number: 10071967
    Abstract: The present invention relates to fungicidal N-cycloalkyl-N-{[2-(1-substitutedcycloalkyl)phenyl]methylene} carboxamide derivatives and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: September 11, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Pierre Cristau, Philippe Desbordes, Julie Geist, Lionel Nicolas, Philippe Rinolfi, Jan-Peter Schmidt, Tomoki Tsuchiya, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
  • Beta-lactamase inhibitors
    Patent number: 10065957
    Abstract: This invention pertains generally to compounds of Formula (A), as further described herein, which act as beta-lactamase inhibitors, and salts, crystalline forms and formulations thereof. In certain aspects, the invention pertains to methods of using such compounds in combination with a beta-lactam antibiotic to treat infections caused by Gram-negative bacteria, including drug-resistant strains.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: September 4, 2018
    Assignee: Novartis AG
    Inventors: Anthony Casarez, Markus Furegati, Guido Koch, Xiaodong Lin, Flavio Ossola, Folkert Reck, Robert Lowell Simmons, Qingming Zhu
  • NK-3 receptor selective antagonist compounds, pharmaceutical composition and methods for use in NK-3 receptors mediated disorders
    Patent number: 10065960
    Abstract: The present invention is directed to novel compounds of formula I and their use as therapeutic compounds.
    Type: Grant
    Filed: July 14, 2015
    Date of Patent: September 4, 2018
    Assignee: Ogeda SA
    Inventors: Hamid R. Hoveyda, Marie-Odile Roy, Graeme L. Fraser, Guillaume Dutheuil
  • Chiral N-acyl-5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof
    Patent number: 10065961
    Abstract: The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.
    Type: Grant
    Filed: September 8, 2016
    Date of Patent: September 4, 2018
    Assignee: Ogeda SA.
    Inventors: Hamid R. Hoveyda, Guillaume Dutheuil, Graeme L. Fraser, Marie-Odile Roy, Mohamed E. Bousmaqui, Frederic Batt
  • N-pyridinyl acetamide derivatives as inhibitors of the Wnt signaling pathway
    Patent number: 10047079
    Abstract: Disclosed are compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition, the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example, in treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment.
    Type: Grant
    Filed: October 8, 2015
    Date of Patent: August 14, 2018
    Assignee: Redx Pharma PLC
    Inventors: Inder Bhamra, Matilda Bingham, Richard Testar, Louise Sargent, Craig Donoghue
  • Bone targeted therapeutics and methods of making and using the same
    Patent number: 10046055
    Abstract: The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: August 14, 2018
    Assignee: MBC PHARMA, INC.
    Inventors: Alexander Karpeisky, Shawn Patrick Zinnen
  • Benzimidazole derivatives
    Patent number: 10017499
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: October 31, 2016
    Date of Patent: July 10, 2018
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Process to make non nucleosidal reverse transcriptase inhibitors (NNRTI) for the treatment of HIV
    Patent number: 10017479
    Abstract: A chemical process that can form pharmaceutically acceptable medicaments NNRTI's for the treatment of HIV starting from thiotriazole compounds. The chemical process can form thiotetrazoles such as 2-((1-(naphthalen-1-yl)-1H-tetrazol-5-yl)thio)-N-(2-nitrophenyl)actetamide that is. a potent NNRTI with nanomolar activity.
    Type: Grant
    Filed: August 2, 2013
    Date of Patent: July 10, 2018
    Inventor: Gregory Rosocha
  • Benzimidazole derivatives as ERBB tyrosine kinase inhibitors for the treatment of cancer
    Patent number: 10005765
    Abstract: Provided herein are benzimidazole derivatives, for example, of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.
    Type: Grant
    Filed: March 19, 2015
    Date of Patent: June 26, 2018
    Assignee: Capella Therapeutics, Inc.
    Inventor: Yun Long
  • Agent for preventing and/or treating ophthalmologic diseases
    Patent number: 10004720
    Abstract: It is an object of the present invention to provide a novel medicament for preventing and/or treating ophthalmologic diseases caused by ocular angiogenesis. According to the present invention, provided is a medicament for preventing and/or treating ophthalmologic diseases caused by ocular angiogenesis, which comprises, as an active ingredient, a pyrazolone derivative such as 3-methyl-1-phenyl-2-pyrazolin-5-one, or a physiologically acceptable salt thereof, or a hydrate thereof or a solvate thereof.
    Type: Grant
    Filed: March 19, 2015
    Date of Patent: June 26, 2018
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Hideaki Hara, Masamitsu Shimazawa, Tomomi Masuda
  • Compounds and their methods of use
    Patent number: 10000479
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Grant
    Filed: March 20, 2015
    Date of Patent: June 19, 2018
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Giovanni Cianchetta, Rene M. Lemieux, Sheldon Cao, Yue Ding, Zhixiong Ye