Patents Examined by Barbara P. Badio
  • 2-alkyl-or-aryl-substituted tanshinone derivatives, and preparation method and application thereof
    Patent number: 9771343
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-alkyl- or 2-aromatic-substituted tanshinone I derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments. When Z=R, said derivative is 2-alkyl-substituted tanshinone I; when Z=Ar, said derivative is 2-aryl-substituted tanshinone I; when Z=Het, said derivative is 2-heteroaryl- or 2-heterocyclyl-substituted tanshinone I.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: September 26, 2017
    Assignee: HANGZHOU BENSHENG PHARMACEUTICAL CO., LTD.
    Inventors: Frank Rong, Rongzhen Xu, Fuwen Xie, Hongxi Lai
  • Sulfoximine substituted 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives and their use as CDK9 kinase inhibitors
    Patent number: 9770445
    Abstract: The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: July 3, 2014
    Date of Patent: September 26, 2017
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Dirk Kosemund, Ulrich Lücking, Arne Scholz, Gerhard Siemeister, Philip Alexander Lienau
  • Compositions and methods for treating toxoplasmosis, cryptosporidiosis, and other apicomplexan protozoan related diseases
    Patent number: 9765037
    Abstract: Compositions and methods for the treatment of toxoplasmosis, caused by the infectious eukaryotic parasite Toxoplasma gondii (T. gondii) and for the treatment of cryptosporidiosis, caused by the infectious eukaryotic parasites Cryptosporidium parvum (C. parvum) and Cryptosporidium hominus (C. hominus) are described. In particular, the present disclosure is directed to compositions and methods for inhibiting either T. gondii calcium dependent protein kinases (TgCDPKs) or C. parvum and C. hominus calcium dependent protein kinases (CpCDPKs) using pyrazolopyrimidine and/or imidazo[1,5-a]pyrazine inhibitors, of the formula, wherein the variables X, Y, Z, L, R1, and R3 are defined herein.
    Type: Grant
    Filed: July 30, 2012
    Date of Patent: September 19, 2017
    Assignee: University of Washington Through its Center for Commercialization
    Inventors: Wesley C. Van Voorhis, Wilhelmus G. J. Hol, Eric T. Larson, Dustin James Maly, Ethan Merritt, Kayode K. Ojo
  • Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions
    Patent number: 9763964
    Abstract: The present invention relates to compounds of formula (I): wherein R is hydrogen or alpha-hydroxy, the hydroxyl group in position 7 is in the alpha or beta position; and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: September 19, 2017
    Assignee: Intercept Pharmaceuticals, Inc.
    Inventors: Roberto Pellicciari, Stefano Fiorucci, Mark Pruzanski
  • Method for treating hypertension
    Patent number: 9744165
    Abstract: Dextromethorphan is used to lower blood pressure in a subject suffering from hypertension, alone or in combination with another anti-hypertensive agent. In particular, dextromethorphan acts synergistically with a calcium channel blocker, such as amlodipine, to result in a major improvement in the treatment of hypertension, with no or little adverse effects.
    Type: Grant
    Filed: April 28, 2016
    Date of Patent: August 29, 2017
    Assignee: TSH Biopharm Corporation Ltd.
    Inventors: Jaw-Wen Chen, Hsi-Chieh Wang, Shin-Yi Juang
  • Therapeutic use of imidazopyridine derivatives
    Patent number: 9732078
    Abstract: The invention relates to the use of compounds corresponding to formula (I) in which R2 and R3 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of the formulae (A), (B) and (C) in which the wavy lines represent the phenyl nucleus to which R2 and R3 are attached, or of a pharmaceutically acceptable salt thereof, for preparing a medicament for the treatment of bladder cancer.
    Type: Grant
    Filed: January 3, 2013
    Date of Patent: August 15, 2017
    Assignee: SANOFI
    Inventors: Chantal Alcouffe, Corentin Herbert
  • Steroids as agonists for FXR
    Patent number: 9732117
    Abstract: The invention relates to compounds of formula (I): wherein R is ethyl, propyl or allyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
    Type: Grant
    Filed: February 5, 2016
    Date of Patent: August 15, 2017
    Assignee: Intercept Pharmaceuticals, Inc.
    Inventor: Roberto Pellicciari
  • 3-(4?-substituted)-benzyl-ether derivatives of pregnenolone
    Patent number: 9732115
    Abstract: The invention relates to a compound of Formula (I), or a pharmaceutically acceptable salt thereof: wherein R1 is C1-8 alkyl, C1-8 alkoxy, CN, NO2, amino, COOH, COOCH3, OH, N3, or halogen and R2 is H, OH, C1-8 alkyl, C1-8 alkoxy, C2-C6 alkenyl, halogen, Bn-O—, Bn- optionally substituted, or Ph- optionally substituted.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: August 15, 2017
    Assignees: INSERM (Institut National de la Sante et de la Recherche Medicale), SC BELENOS, Universite de Bordeaux
    Inventors: Pier Vincenzo Piazza, Monique Vallee, Francois-Xavier Felpin, Jean-Michel Revest, Sandy Fabre
  • Cleavable lipids
    Patent number: 9717690
    Abstract: Disclosed herein are novel compounds, pharmaceutical compositions comprising such compounds and related methods of their use. The compounds described herein are useful, e.g., as liposomal delivery vehicles to facilitate the delivery of encapsulated polynucleotides to target cells and subsequent transfection of said target cells, and in certain embodiments are characterized as having one or more properties that afford such compounds advantages relative to other similarly classified lipids.
    Type: Grant
    Filed: June 8, 2012
    Date of Patent: August 1, 2017
    Assignee: RaNA Therapeutics, Inc.
    Inventors: Braydon Charles Guild, Michael Heartlein, Frank DeRosa, Jerry Chi Zhang
  • 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives, method of production thereof and use thereof for the treatment of diseases
    Patent number: 9717739
    Abstract: The invention relates to 17-hydroxy-17-pentafluoroethyl-estra-4,9(10)-dien-11-aryl derivatives of Formula I with progesterone antagonizing action and method of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of fibroids of the uterus (myomas, uterine leiomyoma), endometriosis, heavy menstrual bleeds, meningiomas, hormone-dependent breast cancers and complaints associated with the menopause or for fertility control and emergency contraception.
    Type: Grant
    Filed: June 4, 2015
    Date of Patent: August 1, 2017
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Wolfgang Schwede, Ulrich Klar, Carsten Moller, Andrea Rotgeri, Wilhelm Bone
  • Estra-1,3,5(10),16-tetraene-3-carboxamides for inhibition of 17.beta.-hydroxysteroid dehydrogenase (AKR1C3)
    Patent number: 9714266
    Abstract: The invention relates to AKR1C3 inhibitors of formula (I) and to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of bleeding disorders and endometriosis.
    Type: Grant
    Filed: February 18, 2014
    Date of Patent: July 25, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Bothe, Matthias Busemann, Naomi Barak, Andrea Rotgeri, Oliver Martin Fischer, Tobias Marquardt
  • 2,2-difluoropropionamide derivatives of bardoxolone methyl, polymorphic forms and methods of use thereof
    Patent number: 9701709
    Abstract: The present invention relates generally to the compound: N-((4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-octadecahydropicen-4a-yl)-2,2-difluoropropanamide, polymorphic forms thereof, methods for preparation and use thereof, pharmaceutical compositions thereof, and kits and articles of manufacture thereof.
    Type: Grant
    Filed: February 19, 2015
    Date of Patent: July 11, 2017
    Assignee: REATA PHARMACEUTICALS, INC.
    Inventors: Eric Anderson, Xiaofeng Liu, Andrea Decker
  • Synthesis of Tetracyclines and intermediates thereto
    Patent number: 9688644
    Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
    Type: Grant
    Filed: July 6, 2015
    Date of Patent: June 27, 2017
    Assignee: President and Fellows of Harvard College
    Inventors: Andrew G. Myers, David A. Kummer, Derun Li, Evan Hecker, Amelie Dion, Peter M. Wright
  • Synthetic bile acid compositions and methods
    Patent number: 9683008
    Abstract: Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: June 20, 2017
    Assignee: Kythera Biopharmaceuticals, Inc.
    Inventors: Robert M. Moriarty, Nathaniel E. David, Nadir Ahmeduddin Mahmood
  • Methods for the purification of deoxycholic acid
    Patent number: 9683007
    Abstract: Synthetic methods for preparing deoxycholic acid and intermediates thereof, high purity synthetic deoxycholic acid, compositions and methods of use are provided. Also, provided are processes for the synthesis of 12-keto or 12-?-hydroxysteroids from ?-9,11-ene, 11-keto or 11-hydroxy-?-steroids. This inversion is also directed to novel compounds prepared during the synthesis. This invention is also directed to the synthesis of deoxycholic acid starting from hydrocortisone.
    Type: Grant
    Filed: November 4, 2014
    Date of Patent: June 20, 2017
    Assignee: Kythera Biopharmaceuticals, Inc.
    Inventors: Robert M. Moriarty, Achampeta Rathan Prasad, John Gregory Reid, Roy A. Swaringen, Jr.
  • Certain steroids and methods for using the same in the treatment of cancer
    Patent number: 9676813
    Abstract: Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Grant
    Filed: April 29, 2013
    Date of Patent: June 13, 2017
    Assignee: NEUPHARMA, INC.
    Inventor: Xiangping Qian
  • Process for the esterification of a carbothioic acid
    Patent number: 9670246
    Abstract: A process for preparing compounds of formula [II] by esterification of the C-17 hydroxyl group of 6?,9?-difluoro-11?,17?-dihydroxy-16?-methyl-3-oxoandrosta-1,4-diene-17?-carbothioic acid, the compound of formula [I] comprises treating compound [I] with a slight excess of an acyl chloride of general formula R—COCl, where R represents —CH2CH3, —CH2CH2CH3 or —CH(CH3)2, in an inert solvent, in the presence of a tertiary amine. Preferably the process is carried out using pyridine in the presence of acetone at a temperature of from 5° C. to ?20° C.
    Type: Grant
    Filed: December 2, 2004
    Date of Patent: June 6, 2017
    Assignee: Hovione Inter Ltd.
    Inventors: Luis Sobral, Dionisio Martin, William Heggie, Emilia Leitäo
  • Oxysterol compounds and the hedgehog pathway
    Patent number: 9670244
    Abstract: This invention relates, for example, to synthetic oxysterols. Also described are methods for using the compounds, including treating subjects in need thereof, and pharmaceutical compositions and kits for implementing methods of the invention.
    Type: Grant
    Filed: February 27, 2007
    Date of Patent: June 6, 2017
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Farhad Parhami, Michael E. Jung, Jennifer R. Dwyer, Khanhlinh Nguyen
  • Contraceptive agents
    Patent number: 9670247
    Abstract: The invention provides compounds of formula I, II, III, or IV: wherein R1 to R11, X, and Y have any of the values defined in the specification. The compounds inhibit Na, K-ATPase ?4 and are useful as contraceptive agents.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: June 6, 2017
    Assignees: The University of Kansas, Regents of The University of Minnesota
    Inventors: Gustavo Blanco, Gunda I. Georg, Shameem Sultana Syeda
  • 3-(4?-substituted)-benzyl-ether derivatives of pregnenolone
    Patent number: 9657051
    Abstract: The invention relates to a compound of Formula (I), or a pharmaceutically acceptable salt thereof: wherein R1 is C1-8 alkyl, C1-8 alkoxy, CN, NO2, amino, COOH, COOCH3, OH, N3, or halogen and R2 is H, OH, C1-8 alkyl, C1-8 alkoxy, C2-C6 alkenyl, halogen, Bn-O—, Bn- optionally substituted, or Ph- optionally substituted.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: May 23, 2017
    Assignees: INSERM (Institut National de la Sante et de la Recherche Medicale), SC BELENOS, Universite de Bordeaux
    Inventors: Pier Vincenzo Piazza, Monique Vallee, Francois-Xavier Felpin, Jean-Michel Revest, Sandy Fabre