Patents Examined by Mark Berch
  • Patent number: 8143264
    Abstract: The present invention relates to a xanthine compound derivative which is 3-butyl-8-chloro-1-(3-{5-[(4-fluorophenyl)methyl]-2H-tetrazol-2-yl}propyl)-3,7-dihydro-1H-purine-2,6-dione: a pharmaceutically acceptable salt thereof, corresponding pharmaceutical formulations, combinations, preparation methods and methods or uses in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.
    Type: Grant
    Filed: August 8, 2006
    Date of Patent: March 27, 2012
    Assignee: GlaxoSmithKline LLC
    Inventors: Richard Jonathan Daniel Hatley, Andrew McMurtrie Mason, Ivan Leo Pinto
  • Patent number: 8138172
    Abstract: The present invention provides 8-oxoadenine derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The 8-oxoadenine derivatives act as modulators of Toll-like Receptor (TLR) 7 and thus may be used in the treatment of asthma, hepatitis, allergic diseases, viral and bacterial infection as well as cancer.
    Type: Grant
    Filed: July 3, 2007
    Date of Patent: March 20, 2012
    Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co Ltd.
    Inventors: Anthony Cook, Tom McInally, Stephen Thom, Hiroki Wada
  • Patent number: 8119648
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: February 21, 2012
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf Lotz
  • Patent number: 8114877
    Abstract: Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: February 14, 2012
    Assignee: Novartis AG
    Inventors: Robin A Fairhurst, Roger J Taylor
  • Patent number: 8110678
    Abstract: This invention is the design and synthesis of a caprolactone monomer which bears a pendant protected carboxyl group. This monomer has been copolymerized with caprolactone in varying ratios. After polymerization, the protecting group can be removed and an antibiotic can be attached as a new pendant group. The bioactivity of the antibiotic-bound poly(caprolactone) polymer is described.
    Type: Grant
    Filed: May 10, 2007
    Date of Patent: February 7, 2012
    Assignee: University of South Florida
    Inventors: Edward Turos, Michelle Leslie
  • Patent number: 8106060
    Abstract: The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof.
    Type: Grant
    Filed: July 30, 2006
    Date of Patent: January 31, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Peter Sieger
  • Patent number: 8101588
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: January 24, 2012
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Ronald J. Albers, Leticia Ayala, Steven S. Clareen, Maria Mercedes Delgado Mederos, Robert Hilgraf, Sayee G. Hegde, Kevin Hughes, Adam Kois, Veronique Plantevin-Krenitsky, Meg McCarrick, Lisa Nadolny, Moorthy S. S. Palanki, Kiran Sahasrabudhe, John Sapienza, Yoshitaka Satoh, Marianne K. Sloss, Elise Sudbeck, Jonathan Wright
  • Patent number: 8097723
    Abstract: Process for the preparation of abacavir, or its salts or its solvates comprising the step of reacting a compound (IV) where R1 is a (C1-C4)-alkyl radical with anhydrous hydrochloric acid/(C1-C6)-alcohol, and then with tri(C1-C4)-alkyl orthoformate, in the absence of water. The preparation process may include further steps of reacting the compound obtained with cyclopropylamine and subsequently hydrolysis to yield abacavir.
    Type: Grant
    Filed: December 20, 2007
    Date of Patent: January 17, 2012
    Assignee: Esteve Quimica, S.A.
    Inventors: Jorge Medrano Rupérez, Julio Campon Pardo, Laia Elías Rius, Ramón Berenguer Maimó
  • Patent number: 8097719
    Abstract: The present invention relates to novel crystalline form of (4-Nitrobenzyl (4R,5S,6S)-(3-{(3S,5S)-5-[(dimethylamino)carbonyl]-1-[(4-nitrophenoxy)carbonxyl]pyrrolidin-3-yl}thio-6-[(1R)-1-hydorxyehtyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0].hept-2-ene-2-carboxylate) of compound Formula I as well as an improved process for the preparation of meropenem trihydrate of compound Formula II wherein, PNB represent P-nitro benzyl group and PNZ represent P-nitrobenzyloxycarbonyl group.
    Type: Grant
    Filed: October 22, 2008
    Date of Patent: January 17, 2012
    Assignee: Genesen Labs
    Inventors: Ashwin A. Khemka, Pravin B. Shejul, Amol V. Vyavahare, Dhirendra Kumar Pandey, Sachin N. Shete, Hanumant K. Jadhav, Nitn H. Kadam
  • Patent number: 8093378
    Abstract: An improved crystallization method for an azetidinone compound represented by the formula 1: , which is extremely useful as a common intermediate for the synthesis of 1?-methylcarbapenem compounds. The present method provides crystals having higher quality and stability than conventional crystals and excellent filterability at the time of recovery; and an azetidinone compound having a low content of impurity, and which has a controlled particle size distribution of crystals and improved handleability and stability. The crystallization is carried out by adding a hydrocarbon solvent to a solution in which an azetidinone compound extremely useful as a common intermediate for the synthesis of 1?-methylcarbapenem compounds is dissolved in the presence of a seed crystal in an amount of 200% by weight or less based on the weight of the azetidinone compound.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: January 10, 2012
    Assignee: Kaneka Corporation
    Inventors: Keita Nishino, Teruyoshi Koga, Masafumi Fukae, Yasuyoshi Ueda
  • Patent number: 8093377
    Abstract: The present invention relates to cephalosporin of formula (I) in crystalline form. The compound of formula (I) in crystalline form is useful as antibiotics having potent and broad antibacterial activity; especially against methicillin resistant Staphylococci (MRSA) and Pseudomonas aeruginosa.
    Type: Grant
    Filed: April 1, 2009
    Date of Patent: January 10, 2012
    Assignee: Basilea Pharmaceutica AG
    Inventor: Joerg Berghausen
  • Patent number: 8088754
    Abstract: Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y1A and Y1B are independently Y1; RX1 and RX2 are independently RX; Y1 is ?O, —O(RX), ?S, —N(RX), —N(O)(RX), —N(ORX), —N(O)(ORX), or —N(N(RX)(RX)); and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: February 18, 2009
    Date of Patent: January 3, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Xiaoqin Cheng, Gary P. Cook, Gong-Xin He, Choung U. Kim, John C. Rohloff, Jianying Wang, Zheng-Yu Yang
  • Patent number: 8080555
    Abstract: Compounds useful in the treatment of autoimmune disease are described by the following general formula: n=0-2 m=0-2 m is not necessarily equal to n; where R1, R3?NH2, F, Cl, C1-C4 alkoxy or phenoxy group, but R1 is not necessarily equal to R3; and R2?H, F, Cl, NH2, or NH—R—XH;
    Type: Grant
    Filed: May 15, 2006
    Date of Patent: December 20, 2011
    Assignee: Prometic Biosciences Inc.
    Inventors: Boulos Zacharie, Daniel Fortin, Nicole Wilb, Christopher Penney
  • Patent number: 8071609
    Abstract: This invention relates to compounds of the general formula: in which Q is an ethynyl or ethenyl moiety; Ring A is an aryl, heteroaryl or heterocyclic ring or ring system; and the remaining variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: August 11, 2006
    Date of Patent: December 6, 2011
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Wei-Sheng Huang, Rajeswari Sundaramoorthi, Xiaotian Zhu, R. Mathew Thomas, William C. Shakespeare, David C. Dalgarno, Tomi K. Sawyer
  • Patent number: 8071565
    Abstract: Compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein W, R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Grant
    Filed: July 11, 2007
    Date of Patent: December 6, 2011
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor
  • Patent number: 8067426
    Abstract: Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
    Type: Grant
    Filed: August 7, 2009
    Date of Patent: November 29, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
  • Patent number: 8067411
    Abstract: The present invention provides compounds of formula wherein R1, Y1, X1, Z1, X2, Y2, A, n and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: November 29, 2011
    Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Roger Victor Bonnert, Thomas McInally, Tobias Mochel, Stephen Thom
  • Patent number: 8067413
    Abstract: The present invention provides compounds of formula (I) wherein R1, Y1, X1, L and R2 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: November 29, 2011
    Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Roger Victor Bonnert, Thomas McInally, Stephen Thom
  • Patent number: 8063051
    Abstract: The present invention provides compounds of formula where n, R1, R2, A, X1, Y1, Z1, X2 and Y2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: November 22, 2011
    Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Roger Victor Bonnert, Thomas McInally, Stephen Thom
  • Patent number: 8063033
    Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y is A is —(CH2)6—, cis —CH2CH?CH—(CH2)3—, or —CH2C?C—(CH2)3—, wherein 1 or 2 carbon atoms may be substituted with S or O; or A is —(CH2)m—Ar—(CH2)o— wherein Ar is substituted or unsubstituted phenyl or monocyclic heteroaryl, the sum of m and o is from 1 to 4, and wherein one CH2 may be replaced with S or O; X is S or O; R is a hydrocarbyl or a hydroxyhydrocarbyl moiety having from 1 to 12 carbon atoms; D is independently a moiety comprising from 1 to 6 non-hydrogen atoms; and n is an integer from 0 to 4. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: January 13, 2009
    Date of Patent: November 22, 2011
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh, Robert M. Burk