Patents Examined by Brian McDowell
  • Inhibitors of human immunodeficiency virus replication
    Patent number: 8377960
    Abstract: Compounds of formula I: wherein c, R2, R3, R4, R5, R6, R7 and R8 are defined herein, are useful as inhibitors of HIV replication.
    Type: Grant
    Filed: November 3, 2008
    Date of Patent: February 19, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Youla S. Tsantrizos, Murray D. Bailey, François Bilodeau, Rebekah J. Carson, Lee Fader, Teddy Halmos, Stephen Kawai, Serge R. Landry, Steven Laplantea, Bruno Simoneau
  • Process of making ?-aminooxyketone/?-aminooxyaldehyde and ?-hydroxyketone/?-hydroxyaldehyde compounds and a process of making reaction products from cyclic ?, ?-unsaturated ketone substrates and nitroso substrates
    Patent number: 8372985
    Abstract: The present invention is directed to a process of making ?-aminooxyketone and ?-hydroxyketone compounds. The synthetic pathway generally involves reacting an aldehyde or ketone substrate and a nitroso substrate in the presence of a catalyst of the formula (IV): wherein Xa-Xc represent independently nitrogen, carbon, oxygen or sulfur and Z represents a 4 to 10-membered ring with or without a substituent and optionally a further step to convert the ?-aminooxyketone compound formed to the ?-hydroxyketone compound. The present invention results in ?-aminooxyketone and ?-hydroxyketone compounds with high enantioselectivity and high purity. The present invention is also directed to a catalytic asymmetric O-nitroso Aldol/Michael reaction. The substrates of this reaction are generally cyclic ?,?-unsaturated ketone substrate and a nitroso substrate.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: February 12, 2013
    Assignee: Japan Science and Technology Agency
    Inventors: Norie Momiyama, Hiromi Torii, Susumu Saito, Hisashi Yamamoto, Yuhei Yamamoto
  • Methods of treatment comprising the administration of heteroaryl compounds
    Patent number: 8372976
    Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1, R2, L, X, Y, Z, Q, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: February 12, 2013
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Deborah Sue Mortensen, Maria Mercedes Delgado Mederos, John Joseph Sapienza, Ronald J. Albers, Branden G. Lee, Roy Leonard Harris, III, Graziella Isabel Shevlin, Dehua Huang, Kimberly Lyn Schwarz, Garrick K. Packard, Jason Simon Parnes, Patrick William Papa, Lida Radnia Tehrani, Sophie Perrin-Ninkovic, Jennifer R. Riggs
  • Pyrazine derivatives as enac blockers
    Patent number: 8372845
    Abstract: Compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 have the meanings as indicated in the specification, are useful for treating diseases mediated by blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: February 12, 2013
    Assignee: Novartis AG
    Inventors: Gurdip Bhalay, Lee Edwards, Catherine Howsham, Peter Hunt, Nichola Smith
  • Co-crystals and pharmaceutical compositions comprising the same
    Patent number: 8372846
    Abstract: The invention relates to compositions and co-crystals each comprising (1S,3aR,6aS)-2-[(2S)-2-[[(2S)-2-Cyclohexyl-2-(pyrazine-2-carbonylamino)acetyl]amino]-3,3-dimethylbutanoyl]-N-[(3S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl]-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrole-1-carboxamide having the structure: and the co-crystal former 4-amino salicylic acid. Also within the scope of this invention are methods of making and using the same.
    Type: Grant
    Filed: October 10, 2011
    Date of Patent: February 12, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Patrick R. Connelly, Sherry Collier, Michael Tauber
  • Process for the preparation of dihydroquinazolines
    Patent number: 8372972
    Abstract: The present invention relates to a process for the preparation of dihydroquinazolines, for example, methyl (S)-{8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoro -methyl)-phenyl]-3,4-dihydroquinazolin-4-yl}acetate (2S,3S)-2,3-bis[(4-methylbenzoyl) -oxy]succinic acid salt, which are used for the production of antiviral medicaments.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: February 12, 2013
    Assignee: AiCuris GmbH & Co. KG
    Inventors: Käthe Gooβen, Oliver Kuhn, Mathias Berwe, Joachim Kruger, Hans-Christian Militzer
  • Heterocyclic sulfonamides
    Patent number: 8367661
    Abstract: Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: February 5, 2013
    Assignee: Cytokinetics, Inc.
    Inventors: Bradley Paul Morgan, Fady Malik, Erica Anne Kraynack, Alexander Ramon Muci, Xiangping Qian, David J. Morgans, Jr.
  • Selective subtype alpha 2 adrenergic agents and methods for use thereof
    Patent number: 8362022
    Abstract: The invention provides well-defined heterocyclic compounds that are useful as subtype selective alpha 2 adrenergic agonists. As such, the compounds described herein, having the structure: are useful in treating a wide variety of disorders associated with selective subtype modulation of alpha 2 adrenergic receptors.
    Type: Grant
    Filed: January 14, 2009
    Date of Patent: January 29, 2013
    Assignee: Allergan, Inc.
    Inventors: Todd M. Heidelbaugh, Ken Chow, Santosh C. Sinha, Phong X. Nguyen, Wenkui K. Fang, Ling Li, Janet A. Takeuchi, Smita S. Bhat
  • Heterocyclic sulfonamides as inhibitors of ion channels
    Patent number: 8357711
    Abstract: The invention is directed to compounds of the formula in which R5, R6 B and Z are defined supra.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: January 22, 2013
    Assignees: Pfizer Limited, Icagen, Inc.
    Inventors: Brian Edward Marron, Paul Christopher Fritch, Christopher John Markworth, Andrew Thomas Maynard, Nigel Alan Swain
  • Selective androgen receptor modulators (SARMs) and uses thereof
    Patent number: 8354446
    Abstract: Provided herein are compounds of formulae I to II that bind to androgen receptors and/or modulate activity of androgen receptors; and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.
    Type: Grant
    Filed: December 12, 2008
    Date of Patent: January 15, 2013
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventor: Lin Zhi
  • Process for the preparation of gefitinib
    Patent number: 8350029
    Abstract: There is provided a compound of formula III, and a process for preparing a compound of formula V comprising converting a compound of formula III to the compound V, wherein X is fluoro, chloro, bromo or iodo. There is also provided a process for preparing a compound of formula XI comprising converting a compound of formula X to the compound XI. The compounds V and XI so prepared may be used in a process for preparing gefitinib.
    Type: Grant
    Filed: April 16, 2008
    Date of Patent: January 8, 2013
    Assignee: CIPLA Limited
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Srinivas Laxminarayan Pathi
  • Salts of 4-aniline quinazoline derivative
    Patent number: 8349854
    Abstract: The present invention relates to salt forms of N-{4-[3-chloro-4-(3-fluoro-benzyloxy)phenylamino]-quinazolin-6-yl}-acrylamide as exemplified by formula (I), methods of preparation thereof, pharmaceutical compositions comprising the same and their use thereof. The salt forms of the present invention, which possess excellent tumor inhibitory activity, good bioavailability and low toxicity in an animal body, are suitable for use of preparation of anti-tumor medicaments.
    Type: Grant
    Filed: February 4, 2008
    Date of Patent: January 8, 2013
    Assignee: Shanghai Allist Pharmaceuticals, Inc.
    Inventors: Jianhui Guo, Yong Jiang
  • Polymorphs of erlotinib hydrochloride and method of preparation
    Patent number: 8349855
    Abstract: The present invention relates to three novel crystalline forms of Erlotinib hydrochloride and method of preparation thereof. Erlotinib hydrochloride is N-(3-ethynylphenyl)-6,7-bis(2-methoxy ethoxy)-4-quinazolinamine hydrochloride of formula-(I). The present invention provides stable novel crystalline forms of Erlotinib hydrochloride designated as Form-M, Form-N and Form-P, and processes for the preparation of the same. Erlotinib hydrochloride can be used as medicament for the treatment of hyperproliferative disorders, such as cancers, in humans.
    Type: Grant
    Filed: September 11, 2007
    Date of Patent: January 8, 2013
    Assignee: Natco Pharma Limited
    Inventors: Ramanadham Jyothi Prasad, Bhujanga rao Adibhatla Kali Satya, Nannapaneni Venkaiah Chowdary
  • Fused pyrimidine derivatives as TRPV3 modulators
    Patent number: 8349846
    Abstract: The present invention related to fused pyrimidine derivatives, which are useful as Transient Receptor Potential Vanilloid 3 (TRPV3) receptors, methods of treating diseases, disorders, conditions modulated by TRPV3. The present invention having the formula (I) and its pharmaceutically acceptable salts thereof, and its processes thereof, wherein all variables are as described herein.
    Type: Grant
    Filed: January 7, 2009
    Date of Patent: January 8, 2013
    Assignee: Glenmark Pharmaceuticals, S.A.
    Inventors: V S. Prasadarao Lingam, Abraham Thomas, Dattaguru Anandrao More, Javed Yusuf Khatik, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Process for preparing 6-phenoxypyrimidin-4-OL derivatives in the presence of a quinuclidine or a -methyl pyrrolidine derivatives
    Patent number: 8350025
    Abstract: The present invention relates, inter alia, to a process for preparing a compound of formula (I): using a quinuclidine-based catalyst or an optionally 3-substituted N-methyl pryrrolidine-based catalyst.
    Type: Grant
    Filed: October 2, 2007
    Date of Patent: January 8, 2013
    Assignee: Syngenta Limited
    Inventors: Gillan Beveridge, Ewan Campbell Boyd, Jack Hugh Vass, Alan John Whitton
  • Heterobicyclic sphingosine 1-phosphate analogs
    Patent number: 8349849
    Abstract: Compounds of formula (I): that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Grant
    Filed: October 30, 2009
    Date of Patent: January 8, 2013
    Assignee: Biogen Idec MA Inc.
    Inventors: Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Wen-Cherng Lee, Edward Yin-Shiang Lin, Xiaogao Liu, Bin Ma, Daniel M. Scott, Zhan Shi, Jermaine Thomas, Arthur G. Taveras, Guo Zhu Zheng
  • Therapeutic agents useful for treating pain
    Patent number: 8349842
    Abstract: Piperidine Compounds; compositions comprising a Piperidine Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Piperidine Compound are disclosed. In one embodiment, the Piperidine Compound has the formula: and pharmaceutically acceptable salts thereof, wherein Ar1, Ar2, X, R3, R4, and m are as disclosed herein.
    Type: Grant
    Filed: July 20, 2009
    Date of Patent: January 8, 2013
    Assignee: Purdue Pharma, L.P.
    Inventors: Qun Sun, Kate Xin Wen, Xiaoming Zhou
  • Quinazolinone derivatives useful as vanilloid antagonists
    Patent number: 8349852
    Abstract: There is described a new polymorphic form of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile and a method of preparing it.
    Type: Grant
    Filed: January 6, 2010
    Date of Patent: January 8, 2013
    Assignee: Novartis AG
    Inventors: Weichun Chen, Hong-Yong Kim, Jessica Liang, Michael Mutz, Mahavir Prashad, Christopher Towler, Ruoqiu Wu
  • Vinyl-aryl derivatives for inflammation and immune-related uses
    Patent number: 8349841
    Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders. In some embodiments, compounds of structural formula (I): or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, are provided.
    Type: Grant
    Filed: July 31, 2008
    Date of Patent: January 8, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventor: Shoujun Chen
  • Heterocyclic compounds and uses thereof in the treatment of sexual disorders
    Patent number: 8349850
    Abstract: Novel heterocyclic compounds having the formula: or a pharmaceutically acceptable salt thereof, wherein A, B, D, E, G, K, L, M, Q, T, X, Y and Z are as described in the specification, which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity, are disclosed, as well as processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction.
    Type: Grant
    Filed: March 28, 2007
    Date of Patent: January 8, 2013
    Assignee: ATIR Holding S.A.
    Inventors: Dmitry Tworowski, Ron Matsievitch, Vladimir Kogan