Patents Examined by Sabiha Qazi
  • Patent number: 8802830
    Abstract: A method of preparing an anthracyclin such as epirubicin from a starting material comprising 13-dihydrodaunorubicine (13-daunorubicinol). The method comprises producing N-Trifluoroacetyl-13-daunorubicinol from 13-daunorubicinol by acylation. The N-Trifluoroacetyl-13-daunorubicinol is reacted with an aprotic solvent and an acylating agent to produce an intermediate sulfoxy salt which is treated with a strong base to produce 4?-keto-N-Trifluoroacetyldaunorubicin. The 4?-keto-N-Trifluoroacetyldaunorubicin is reacted with a reducing agent, such as borohydride of an alkaline metal, to produce N-Trifluoroacetyl-4?-epi-daunorubicin. The N-Trifluoroacetyl-4?-epi-daunorubicin is hydrolyzed in a basic solution to produce an intermediate compound. The intermediate compound is reacted with a halogenizing agent to produce a 14-Hal-derivative. The 14-Hal derivative is hydrolized in the presence of a formate of an alkaline metal to produce the desired final compound.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: August 12, 2014
    Assignee: Solux Corporation
    Inventors: Alexander F. Zabudkin, Victor Matvienko, Aleksandr M. Itkin, Alexey Matveev
  • Patent number: 8604008
    Abstract: Compounds of formula I are provided where X1 and X2 are independently selected from H or hydroxy protecting groups. Such compounds may be used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: December 10, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame
  • Patent number: 8575136
    Abstract: Compounds of formula I are provided where X1 and X2 are independently selected from H or hydroxy protecting groups. Such compounds are used in preparing pharmaceutical compositions and are useful in treating a variety of biological conditions.
    Type: Grant
    Filed: April 6, 2007
    Date of Patent: November 5, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Lori A. Plum, Margaret Clagett-Dame, Rafal Barycki
  • Patent number: 8481515
    Abstract: The object of the invention is the use as a drug of a compound fitting formula I wherein X represents an oxygen atom or a ?N—OH group and R represents a group selected from or one of its esters and/or of its addition salts with pharmaceutically acceptable acids, particularly as a cytoprotective drug, preferentially a cardioprotective and/or neuroprotective drug, the compounds of formula I wherein R is R2, R3, R4, R5 or R6 as novel compounds as well as their preparation method and use.
    Type: Grant
    Filed: December 15, 2006
    Date of Patent: July 9, 2013
    Assignee: Trophos
    Inventors: Cyrille Drouot, Delphine Maux
  • Patent number: 8377913
    Abstract: The invention relates to compounds that are vitamin D receptor activators, compositions comprising such compounds, methods of using such compounds and compositions, processes for preparing such compounds, and intermediates obtained during such processes.
    Type: Grant
    Filed: September 8, 2008
    Date of Patent: February 19, 2013
    Assignee: AbbVie Inc.
    Inventors: Thomas W. Von Geldern, Jufang H. Barkalow, David M. Barnes, Anthony R. Haight, John E. Hengeveld, Xiaofeng Li, Maureen A. McLaughlin, William T. Noonan, Zhonghua Pei, Jinshyun Ruth Wu-Wong
  • Patent number: 8362286
    Abstract: Applicants have discovered a method for the stereoselective and regioselective synthesis of 3?-hydroxy, 3?-methyl-5?-pregnan-20-one (ganaxolone) comprising reacting 5?-pregnane-3,20-dione; with an organometallic methylating agent in an inert solvent to provide a compound of the formula
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: January 29, 2013
    Assignee: Marinus Pharmaceuticals, Inc.
    Inventors: Kenneth Shaw, Alan Hutchison
  • Patent number: 8362074
    Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: January 29, 2013
    Assignee: BASF Aktiengesellschaft
    Inventors: Michael Frank Treacy, Raymond Frank Borysewicz, Kurt Allen Schwinghammer, Paul E. Rensner, Hassan Oloumi-Sadeghi
  • Patent number: 8362287
    Abstract: The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.
    Type: Grant
    Filed: March 10, 2005
    Date of Patent: January 29, 2013
    Assignee: Leo Pharma A/S
    Inventors: Thomas Peter Sabroe, Martin John Calverley
  • Patent number: 8357685
    Abstract: Compounds of formula (1) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is 2-methyl-1,3-oxazol-4-yl and R4 and R5 together with the nitrogen atom to which they are attached represents morpholino, process for their preparation, pharmaceutical compositions containing them and their use in medicine.
    Type: Grant
    Filed: September 13, 2011
    Date of Patent: January 22, 2013
    Assignee: Glaxo Group Limited
    Inventor: John Liddle
  • Patent number: 8357816
    Abstract: A fungicidal compound of formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by groups R7, R8 and R9; R1 is hydrogen, optionally substituted (C1-4alkyl, optionally substituted (C1-4alkylC(?O), optionally substituted (C1-4alkylC(?O)O, optionally substituted (C1-4)alkoxy(C1-4)alkyl, optionally substituted allyl, optionally substituted propargyl or optionally substituted allenyl; R2, R3, R4 and R5 are each, independently, hydrogen, halogen, optionally substituted (C1-4)alkyl, optionally substituted (C1-4)alkoxy or optionally substituted (C1-4)alkoxy(C1-4alkyl; R6 is an organic group containing three to thirteen carbon atoms and at least one silicon atom and, optionally, one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, and is optionally substituted by one to four independently selected halogen atoms; R7, R8 and R9 are each, independen
    Type: Grant
    Filed: July 22, 2010
    Date of Patent: January 22, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Josef Ehrenfreund, Pierre Joseph Marcel Jung, Hans Tobler, Harald Walter
  • Patent number: 8338628
    Abstract: A novel, improved method of synthesizing alkylated bile acid derivatives is provided. Such derivatives include, but are not limited to the active, potent, and selective FXR receptor agonist such as 6-ECDCA and other CA, DCA and CDCA derivatives. The first step of the synthesis selectively oxidates CDCA, CD, or DCA related starting material. An efficient combined deprotonation, trapping, ethylation, deprotection and reduction system is used to produce the desired alkylated bile acid derivatives. This practical synthesis offers a simple and economical pathway suitable for a large-scale manufacturing of alkylated bile acid derivatives including, but not limited to, 6-ECDCA.
    Type: Grant
    Filed: May 22, 2008
    Date of Patent: December 25, 2012
    Assignee: City of Hope
    Inventors: Donna D. Yu, Barry M. Forman
  • Patent number: 8338460
    Abstract: Compounds of a formula (I) and their pharmaceutically-acceptable salts are disclosed. The compounds have glucokinase-activating effect and are therefore useful for treatment of diabetes and obesity. R1 and R2 each independently represent a lower alkyl group; X1 represent a group of a formula (II-1): wherein: R11 and R12 each independently represent a hydrogen atom or a lower alkyl group, or taken together with the nitrogen atom to which they bond, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring (one carbon atom constituting the 4- to 7-membered nitrogen-containing aliphatic ring may be replaced by an oxygen atom), or taken together with a carbon atom in (CH2)m, R11 and R12 may form a 4- to 7-membered nitrogen-containing aliphatic ring; m indicates an integer of from 1 to 3.
    Type: Grant
    Filed: October 5, 2007
    Date of Patent: December 25, 2012
    Assignee: MSD K. K.
    Inventors: Noriaki Hashimoto, Yufu Sagara, Masanori Asai, Teruyuki Nishimura
  • Patent number: 8318706
    Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: November 27, 2012
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Oak Kim, Haregewein Assefa, Laura Honeyman
  • Patent number: 8318757
    Abstract: There is provided a novel pest control agent, particularly an insecticide or miticide. A substituted isoxazoline compound of General Formula (1): where A1, A2 and A3 independently are CH or N, etc., X1, X2 and X3 are independently are H, a halogen atom, etc., Y1 is H, etc., R1 is —C(O)R1a, —C(S)R1a, R1a is —C(R9)(R9a)—S(O)rR10, —C(R9)(R9a)—S(O)t(R10)?NR11, etc., R2 is H, etc., R3 is CF3, CClF2, etc., R4 is H, etc., R9 is H, etc., R9a is H, etc., R10 is C1-2 alkyl, etc., R11 is H, etc., r is an integer of 0-2, t is an integer of 0 or 1; and a pest control agent comprising the compound or the salt thereof.
    Type: Grant
    Filed: September 10, 2008
    Date of Patent: November 27, 2012
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Takeshi Mita, Kazushige Maeda, Youko Yamada, Eitatsu Ikeda, Ken-ichi Toyama, Mitsuaki Komoda
  • Patent number: 8314254
    Abstract: The present invention relates to novel intermediates used in the preparation of substituted spirocyclic ketoenols of the formula (I) in which W, X, Y, Z, A, B, D and G are as defined in the disclosure.
    Type: Grant
    Filed: May 25, 2010
    Date of Patent: November 20, 2012
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Angelika Lubos-Erdelen, legal representative, Jorg Konze, Peter Losel, Mark Wilhelm Drewes, Dieter Feucht, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann
  • Patent number: 8314145
    Abstract: The invention relates to a new process for the synthesis of high purity 17?-cyanomethyl-17?-hydroxy-estra-4,9-diene-3-one (further on dienogest) of formula (I) from 3-methoxy-17-hydroxy-estra-2,5(10)-diene of formula (V). The invention relates also to the high purity 17?-cyanomethyl-17?-hydroxy-estra-4,9-diene-3-one and pharmaceutical compositions containing that as active ingredient. The pharmaceutical compositions according to this invention contain high purity dienogest of formula (I) in which the total amount of impurities is less than 0.1%, while the amount of 4-bromo-dienogest is under the detection limit (0.02%) as active ingredient or at least one of the active ingredients and auxiliary materials, which are commonly used in practice, such as carriers, excipients or diluents.
    Type: Grant
    Filed: October 11, 2006
    Date of Patent: November 20, 2012
    Assignee: Richter Gedeon Vegyeszeti Gyar RT
    Inventors: Lajosné Dancsi, Sándor Mahó, Antal Aranyi, János Horváth
  • Patent number: 8268306
    Abstract: This invention relates to pesticide and antiparasitic compositions for the control of pests, diseases and parasites attacking plants and animals. The compositions include, at least one chitinolytic agent or a chitinolytic activity-inducing agent, and sulfide or a sulfide-producing agent from microorganisms or chemical compounds, wherein the chitinolytic agent or the chitinolytic activity-inducing agent and sulfur or a sulfur-producing agent obtaining from microorganisms or chemical compounds are concurrently applied at a range significantly lower than any of the above-mentioned compounds, when they are individually to attain effective control.
    Type: Grant
    Filed: August 16, 2010
    Date of Patent: September 18, 2012
    Assignee: Centro de Ingenieria Genetica y Biotecnologia
    Inventors: Jesus Mena Campos, Eulogio Pimentel Vazquez, Armando Tomas Hernadez Garcia, Liuven Veloz Gonzalez, Marieta Marin Bruzos, Oscar Compte Alberto, Marilin Domingo Puente, Licette Leon Barreras, Merardo Pujol Ferrero, Juan Diego Mencho Ponce, Carlos Borroto Nordelo
  • Patent number: 8268873
    Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH-mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
    Type: Grant
    Filed: August 7, 2008
    Date of Patent: September 18, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Dean Stamos, Martin Trudeau, Randy S. Bethiel, Steven M. Ronkin, Michael C. Badia, Jeffrey O. Saunders
  • Patent number: 8258120
    Abstract: The present invention pertains, at least in part, to novel 9-substituted minocycline compounds. These minocycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
    Type: Grant
    Filed: January 9, 2009
    Date of Patent: September 4, 2012
    Assignees: Paratek Pharmaceuticals, Inc., Trustees of Tufts College
    Inventors: Mark L. Nelson, Mohamed Y. Ismail, Laura Honeyman
  • Patent number: 8232263
    Abstract: This invention discloses 17,20(Z)-dehydro vitamin D analogs, and specifically 17(Z)-1?,25-dihydroxy-17(20)-dehydro-2-methylene-19-nor-vitamin D3 and pharmaceutical uses therefor. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also may be used to treat autoimmune disorders and inflammatory diseases in humans as well as renal osteodystrophy and obesity. This compound also has significant calcemic activity making it a therapeutic agent for the treatment or prophylaxis of osteoporosis, osteomalacia, renal osteodystrophy and hypoparathyroidism.
    Type: Grant
    Filed: July 9, 2007
    Date of Patent: July 31, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Bulli Padmaja Tadi, Lori A. Plum, Margaret Clagett-Dame