Patents Examined by Mark L. Berch
  • Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith
    Patent number: 7723340
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and 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: January 12, 2006
    Date of Patent: May 25, 2010
    Assignees: Signal Pharmaceuticals, LLC, Pharmacopeia Drug Discovery, Inc.
    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, Ian Henderson, Andrew G. Cole
  • Preparation of 9-hydroxy-3-(2-hydroxyethyl)-2-methyl-4-pyrido[1,2-A]pyrimidin-4-one
    Patent number: 7723518
    Abstract: The present invention concerns a process for preparing crystalline 3-(2-chloro-ethyl)-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one substantially free of 2-acetylbutyrolactone.
    Type: Grant
    Filed: September 7, 2005
    Date of Patent: May 25, 2010
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Eduard Jozef Contantia Vreysen, Joannes Petrus Van Dun, Wim Albert Alex Aelterman
  • Xanthines with HM74A receptor activity
    Patent number: 7713982
    Abstract: The present invention relates to a therapeutically active xanthine derivative compound of formula (I): corresponding pharmaceutical formulations containing, manufacture processes for, methods or uses of such compounds in therapy, in particular for treatment of diseases where under-activation of the HM74A receptor contributes to such diseases or where activation of the HM74A receptor will be beneficial.
    Type: Grant
    Filed: February 10, 2005
    Date of Patent: May 11, 2010
    Assignee: Smithkline Beecham Corporation
    Inventor: Ivan Leo Pinto
  • Process for producing penam compound useful for preparing tazobactam
    Patent number: 7714125
    Abstract: An object of the invention is to provide an industrially advantageous process capable of remarkably suppressing the generation of an undesirable by-product cepham compound to thereby efficiently produce a desired 2?-methyl-2?-[(1,2,3-triazol-1-yl)methyl]penam-3?-carboxylic acid ester. In the present invention, a diphenylmethyl 2?-bromomethyl-2?-methylpenam-3?-carboxylate (BMPB) is reacted with 1,2,3-triazole in a halogenated hydrocarbon solvent at ?5° C. or lower. The reaction in a halogenated hydrocarbon solvent at ?5° C. or less can remarkably suppress the generation of an undesirable by-product cepham compound, so that the desired diphenylmethyl 2?-methyl-2?-[(1,2,3-triazol-1-yl)methyl]penam-3?-carboxylate (TMPB) can be efficiently produced.
    Type: Grant
    Filed: October 25, 2005
    Date of Patent: May 11, 2010
    Assignee: Otsuka Chemical Co., Ltd.
    Inventors: Isao Wada, Yoshihisa Tokumaru, Akihiro Shimabayashi
  • Process for the preparation of cefixime
    Patent number: 7705142
    Abstract: There is provided an improved process for preparing cefixime. Thus, for example, 7-amino-3-vinyl-3-cephem-4-carboxylic acid is reacted with 2-mercapto-1,3-benzothiazolyl-(Z)-2-(2-aminothiazol-4-yl)-2-(methoxycarbonyl)-methoxyimino acetate in tetrahydrofuran and water at 4° C. in the presence of triethylamine. The reaction mass is extracted with ethyl acetate. 7-[2-(2-Amino-4-thiazolyl)-2-(methoxycarbonylmethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid triethylamine salt present in the aqueous layer is hydrolyzed with sodium hydroxide in less than 30 minutes and aqueous hydrochloric acid is added immediately to adjust the pH to 4.8 to 5.2. Then, aqueous hydrochloric acid is added at 35° C. to adjust the pH 2.5 and cooled to crystallize cefixime trihydrate in high purity.
    Type: Grant
    Filed: March 29, 2005
    Date of Patent: April 27, 2010
    Assignee: Hetero Drugs Limited
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Nagabelli Murali
  • Protein kinase modulators and methods of use
    Patent number: 7704995
    Abstract: This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.
    Type: Grant
    Filed: May 2, 2003
    Date of Patent: April 27, 2010
    Assignee: Exelixis, Inc.
    Inventors: Chris A. Buhr, Tae-Gon Baik, Sunghoon Ma, Zerom Tesfai, Longcheng Wang, Erick Wang Co, Sergey Epshteyn, Abigail R Kennedy, Baili Chen, Larisa Dubenko, Neel Kumar Anand, Tsze H. Tsang, John M. Nuss, Csaba J Peto, Kenneth D. Rice, Mohamed Abdulkader Ibrahim, Kevin Luke Schnepp, Xian Shi, James William Leahy, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Grace Mann, Larry Wayne Mann, Craig Stacy Takeuchi, Peter Lamb, David J. Matthews, Nicole Miller
  • Anti-hypercholesterolemic compounds
    Patent number: 7704988
    Abstract: This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.
    Type: Grant
    Filed: October 4, 2006
    Date of Patent: April 27, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Robert J. DeVita, Gregori J. Morriello, Peter Lin
  • Cephalosporin compounds comprising a C3 thio-methyl moiety substituted with N-containing heterocyclic group, and a C7 thiourea acetamido group, their preparations and uses thereof
    Patent number: 7700581
    Abstract: Disclosed herein are a cephalosporin compound of formula I, wherein R1 is selected from the following groups: wherein R2 is selected from the following groups: the preparation and uses thereof. A method of preparing the cephalosporin compound as disclosed herein comprises reacting a starting cephalosporin comprising a C7 amino group and a C3 thio-methyl moiety substituted with an N-containing heterocyclic group with bromoacetyl bromide and then with a N,N?-bissubstituted thiourea. Methods of treating an infectious disease are also disclosed, comprising administering to a patient in need thereof the pharmaceutical composition disclosed herein.
    Type: Grant
    Filed: January 31, 2007
    Date of Patent: April 20, 2010
    Assignee: Guangzhou Baiyunshan Pharmaceutical Co., Ltd.
    Inventors: Mao Chen, Shaoxuan Zhu, Xuebin Liu, Chun Luo, Shuwen Xu, Lizhen Zheng, Fang Ye, Chenglong Yi, Xiaona Zhang
  • Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
    Patent number: 7696212
    Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: April 13, 2010
    Assignee: Boehringer Ingelheim Pharma GmbH and Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Ralf Lotz, Michael Mark, Mohammad Tadayyon
  • Penicillin crystals and process for producing the same
    Patent number: 7692003
    Abstract: The present invention provides 2?-chloromethyl-2?-methylpenam-3?-carboxylic acid benzhydryl ester (CMPB) crystals of excellent stability, and a process for producing the CMPB crystals comprising the steps of (A) concentrating a solution containing CMPB; (b) subjecting the thus-obtained concentrate to column chromatography; (C) concentrating a CMPB-containing fraction; and (D) dissolving the thus-obtained CMPB-containing concentrate in an ether solvent and adding a hydrocarbon solvent to the resulting solution to precipitate CMPB crystals.
    Type: Grant
    Filed: October 8, 2004
    Date of Patent: April 6, 2010
    Assignees: Otsuka Chemical Co., Ltd., Taiho Pharmaceutical Co., Ltd.
    Inventors: Isao Wada, Yutaka Kameyama
  • Kinase inhibitors and methods of use thereof
    Patent number: 7691858
    Abstract: Compositions and methods and are provided for treating disorders associated with compromised vasculostasis. Invention methods and compositions are useful for treating a variety of disorders including for example, stroke, myocardial infarction, cancer, ischemia/reperfusion injury, autoimmune diseases such as rheumatoid arthritis, eye diseases such as uveitis, retinopathies or macular degeneration, macular edema or other vitreoretinal diseases, inflammatory diseases such as autoimmune diseases, vascular leakage syndrome, edema, or diseases involving leukocyte activation, transplant rejection, respiratory diseases such as asthma, adult or acute respiratory distress syndrome (ARDS), chronic obstructive pulmonary disease, and the like.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: April 6, 2010
    Assignee: TargeGen, Inc.
    Inventors: John Doukas, Chi Ching Mak, Elena Dneprovskaia, Glenn Noronha
  • Phthalazinone derivatives
    Patent number: 7692006
    Abstract: 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form A.
    Type: Grant
    Filed: October 17, 2007
    Date of Patent: April 6, 2010
    Assignee: Kudos Pharmaceuticals Limited
    Inventors: Keith Allan Menear, Anthony Peter Ottridge, Derek John Londesbrough, Michael Raymond Hallett, Keith Raymond Mulholland, John David Pittam, David Dermot Patrick Laffan, Ian Woodward Ashworth, Martin Francis Jones, Janette Helen Cherryman
  • Tricyclic 6-alkylidene-penems as ?-lactamase inhibitors
    Patent number: 7691842
    Abstract: The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof, wherein one of A and B denotes hydrogen and the other an optionally substituted fused tricyclic heteroaryl group; and X is O.
    Type: Grant
    Filed: August 7, 2008
    Date of Patent: April 6, 2010
    Assignee: Wyeth LLC
    Inventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Ado Mihira, Atul Agarwal, Hideki Ushirogochi, Yansong Gu, Satoshi Tamai, Fuk-Wah Sum
  • Cyclic derivatives as modulators of chemokine receptor activity
    Patent number: 7687508
    Abstract: This invention relates generally to modulators of chemokine receptor activity having unexpected combination of desirable pharmacological properties. Pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and prevention of inflammatory, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases, particularly diabetes, Crohn's disease, atherosclerosis, and multiple sclerosis, along with methods of preparing compounds and intermediates therefor. Metabolites of active compounds are also provided herein, pharmaceutical compositions and use thereof are also provided.
    Type: Grant
    Filed: July 25, 2007
    Date of Patent: March 30, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Percy H. Carter, Robert J. Cherney, John Hynes, Soo S. Ko, Anurag S. Srivastava, Zili Xiao, Michael G. Yang
  • 2-thioethenyl substituted carbapenem derivatives
    Patent number: 7687490
    Abstract: An objective of the present invention is to provide compounds that are effective against various resistant bacteria which cause current clinical problems, for example, pneumococci including penicillin resistant Streptococcus pneumoneae (PRSP), Haemophilus influenzae including bata-lactamase-nonproducing ampicillin-resistant Haemophilus influenzae (BLNAR), and Moraxella (Branhamella) catarrhalis.
    Type: Grant
    Filed: April 12, 2006
    Date of Patent: March 30, 2010
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Takahisa Maruyama, Yuko Kano, Takashi Ando, Takehiko Sawabe, Nobuyoshi Baba, Hiromi Takata, Hisashi Suzuki, Kazuhiro Aihara, Toshiki Fujita
  • Substituted quinazoline or pyridopyrimidine derivative
    Patent number: 7687502
    Abstract: The present invention provides a compound having a glucokinase activating action being useful for prevention or treatment of diabetes mellitus, etc. being represented by the formula (I): X is nitrogen atom, etc.; Y is oxygen atom, etc.; R1 is an optionally substituted five to six-membered heteroaryl group, etc.; R2 is hydrogen atom or fluorine atom; and ring A is a monocyclic or bicyclic heteroaryl group which may have a substituent represented by the formula (II)] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 23, 2005
    Date of Patent: March 30, 2010
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Morihiro Mitsuya, Makoto Bamba, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki, Keisuke Arakawa
  • Carbapenem antibacterials with gram-negative activity and processes for their preparation
    Patent number: 7683049
    Abstract: The present invention provides ?-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions, wherein the compounds are generally of the Formulae The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
    Type: Grant
    Filed: June 10, 2005
    Date of Patent: March 23, 2010
    Assignee: FOB Synthesis, Inc.
    Inventors: Woo-Baeg Choi, Ewa Kowalik
  • Compounds
    Patent number: 7678801
    Abstract: Novel substituted 2,4,8-trisubstituted 8H-pyrido[2,3-d]pyrimidin-7-one containing compounds and compositions, and their use use in therapy as CSBP/RK/p38 kinase inhibitors.
    Type: Grant
    Filed: March 24, 2006
    Date of Patent: March 16, 2010
    Assignee: Glaxo Group Limited
    Inventors: James F. Callahan, Jeffrey C. Boehm, Anthony William James Cooper, Stefano Livia, Neysa Nevins, Zehong Wan, Beth A. Norton, Paul Bamborough, Xichen Lin
  • MGluR5 modulators I
    Patent number: 7678796
    Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: March 16, 2010
    Assignee: AstraZeneca AB
    Inventors: Andreas Wallberg, Karolina Nilsson, Björn Holm, Mats Nagard, Kenneth Granberg, Abdelmalik Slassi, Louise Edwards, Methvin Isaac, Tao Xin, Tomislav Stefanac
  • Piperazinylpiperidine derivatives as chemokine receptor antagonists
    Patent number: 7678798
    Abstract: The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.
    Type: Grant
    Filed: April 12, 2005
    Date of Patent: March 16, 2010
    Assignee: Incyte Corporation
    Inventors: Chu-Biao Xue, Ganfeng Cao, Taisheng Huang, Lihua Chen, Ke Zhang, Anlai Wang, David Meloni, Rajan Anand, Joseph Glenn, Brian W. Metcalf