1,3-diazoles Patents (Class 514/385)
  • Patent number: 10131636
    Abstract: The present invention relates to an improved process for the preparation of enzalutamide by conventional synthesis, which avoids utilization of microwave irradiation and noxious reagents. The present invention also relates to an improved process for preparation of 4-isothiocyanato-2-(trifluoromethyl) benzonitrile, which is an intermediate in the synthesis of Enzalutamide.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: November 20, 2018
    Assignee: Laurus Labs Limited
    Inventors: Kameswar R. Chivukula, Veera Venkateswara Rao Karuturi, Srinivas Benda, Ramachandra Anke, Dharmapuri Gajula, Venkata Rama Krishna Murthy Moturu, Venkata S. Indukuri, Seeta Ram Anjaneyulu Gorantla, Satyanarayana Chava
  • Patent number: 10125387
    Abstract: The invention relates to methods for the identification of compounds, peptides and proteins that can act as substrates for histone deacetylases. The invention further relates to compounds of Formula I: F1—X1-L1-X2—P1—X3-G1??(Formula I) The invention relates to the treatment of diseases or disorders mediated by ARID1A (BAF250A).
    Type: Grant
    Filed: August 3, 2017
    Date of Patent: November 13, 2018
    Assignee: The Broad Institute, Inc.
    Inventors: Edward Holson, David Olson
  • Patent number: 10098837
    Abstract: Aerosol formulations comprising glycopyrronium bromide, formoterol or a salt thereof, and beclometasone dipropionate are useful for the prevention or treatment of moderate/severe chronic obstructive pulmonary disease.
    Type: Grant
    Filed: July 28, 2017
    Date of Patent: October 16, 2018
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Mario Scuri, Pierfrancesco Coli, Giuseppe Delmonte
  • Patent number: 10028992
    Abstract: Disclosed herein are ?7?1 integrin modulatory agents and methods of using such to treat conditions associated with decreased ?7?1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an ?7?1 integrin modulatory agent to the subject with muscular dystrophy, wherein the ?7?1 integrin modulatory agent increases ?7?1 integrin expression or activity as compared to ?7?1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing ?7?1 integrin expression by use of the disclosed ?7?1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.
    Type: Grant
    Filed: September 10, 2013
    Date of Patent: July 24, 2018
    Assignee: BOARD OF REGENTS OF THE NEVADA SYSTEM OF HIGHER EDUCATION ON BEHALF OF THE UNIVERSITY OF NEVADA, RENO
    Inventors: Dean Burkin, Ryan Wuebbles
  • Patent number: 9937169
    Abstract: Provided herein are methods for treating or preventing a cancer, comprising administering an effective amount of a Dihydropyrazino-Pyrazine Compound and an effective amount of an androgen receptor antagonist to a patient having a cancer.
    Type: Grant
    Filed: April 16, 2014
    Date of Patent: April 10, 2018
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Heather Raymon, Toshiya Tsuji, Rama K. Narla, Kristen Mae Hege
  • Patent number: 9682093
    Abstract: The invention provides methods, compositions, uses of compositions, assays and kits for modulating brown adipose tissue (BAT) in animals and patients with obesity, insulin resistance and perturbed glucose homeostasis are disclosed. Accordingly, methods, compositions, uses of compositions, and kits are useful for the amelioration of pathological conditions characterized by storage of excess energy, insulin resistance and related metabolic syndromes often associated with obesity.
    Type: Grant
    Filed: April 1, 2013
    Date of Patent: June 20, 2017
    Assignee: Charles R. Drew University of Medicine and Science
    Inventor: Rajan Singh
  • Patent number: 9586947
    Abstract: New imidazoline derivatives represented by formula (I): preparation methods thereof, pharmaceutical compositions comprising such derivatives, and applications of such derivatives in preparing androgen receptor antagonists and medicaments for treating diseases such as prostate cancer are described.
    Type: Grant
    Filed: August 26, 2013
    Date of Patent: March 7, 2017
    Assignees: Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Hejun Lu, Piaoyang Sun, Hongbo Fei, Hongjian Jiang, Haowei Wang, Qing Dong
  • Patent number: 9481653
    Abstract: Optionally substituted benzoimidazol-1,2-yl amides, such as compounds of Formula 1 or Formula 2, can be used to treat disorders associated with a Kv7 potassium channel activator. Compositions, medicaments, and dosage forms related to the treatment are also disclosed herein.
    Type: Grant
    Filed: September 14, 2015
    Date of Patent: November 1, 2016
    Assignee: KNOPP BIOSCIENCES LLC
    Inventors: Lynn Resnick, George T. Topalov, Steven A. Boyd, Justin K. Belardi, Charles A. Flentge, James S. Hale, Scott S. Harried, David A. Mareska, Kai Zhang
  • Patent number: 9439891
    Abstract: Disclosed herein are pharmaceutical compositions, methods and kits for lowering the serum uric acid level of a subject and for the treatment of a condition associated with elevated serum uric acid levels comprising administering a composition comprising a first urate-lowering agent and a second urate-lowering agent. In some aspects the first urate-lowering agent is (?)-halofenate, (?)-halofenic acid, or a pharmaceutically acceptable salts thereof. In some aspects the second urate-lowering agent is an inhibitor of uric acid production, a uricosuric agent, a uricase, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 24, 2015
    Date of Patent: September 13, 2016
    Assignees: CymaBay Therapeutics, Inc., DiaTex, Inc.
    Inventors: Brian K. Roberts, Gopal Chandra Saha, Brian Edward Lavan, Charles A. McWherter
  • Patent number: 9340531
    Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: May 17, 2016
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Tsutomu Nagata, Masahiro Inoue, Yuka Ashida, Kengo Noguchi, Makoto Ono
  • Patent number: 9296719
    Abstract: Compositions and methods for the treatment of norovirus infection are disclosed.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: March 29, 2016
    Assignees: Indiana University Research and Technology Corporation, Alios Biopharma, Inc.
    Inventors: Ch. V. Subba-Reddy, C. Cheng Kao, Dave Smith, Leo Beigelman
  • Patent number: 9247732
    Abstract: Agrochemical compositions are described which contain a carboxylic acid salt of dodecylguanidine and a compatibility agent for slowing down the dissociation reaction of the carboxylic acid salt of dodecylguanidine in an aqueous medium. Also, the formation of anionic dodecylguanidine is suppressed or prevented. The ratio of the dodecylguanidine acetate to that of the compatibility agent in the agricultural compositions is below 5.0, preferably between 3.0 and 0.5, more preferably equals 1.4.
    Type: Grant
    Filed: May 10, 2011
    Date of Patent: February 2, 2016
    Inventor: Alan Pirotte
  • Patent number: 9108948
    Abstract: Compounds of formula (I) wherein R1, R2, R3, R3a, R3b, R4, and R5 are defined in the description, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: August 18, 2015
    Assignee: AbbVie Inc.
    Inventors: Huaqing Liu, Lawrence A. Black, Youssef L. Bennani, Marlon D. Cowart, Zhenping Tian, Paul J. Brackemeyer
  • Patent number: 9078883
    Abstract: The present invention relates to a method for the prevention and treatment of hypotension and shock due to low peripheral resistance, comprising administering to a mammal in need thereof an effective amount of a certain imidazole derivative or pharmaceutically acceptable ester or salt thereof. In addition, the present invention relates to a method for the treatment of cardiopulmonary resuscitation, comprising administering to a mammal in need thereof an effective amount of a certain imidazole derivative or pharmaceutically acceptable ester or salt thereof.
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: July 14, 2015
    Assignee: Recro Pharma, Inc.
    Inventors: Riitta Heino, Tiina Leino, Tarja Lehtimaki
  • Patent number: 9023841
    Abstract: This disclosure provides methods for treating asthma or an associated disorder in a patient in need thereof, by administering to the patient an effective amount of an autophagy inducing agent, thereby treating the asthma or the associated disorder. Disorders that can be treated include, allergic asthma, chronic obstructive pulmonary disease, lung inflammation, respiratory tolerance and a lung infection or disorder.
    Type: Grant
    Filed: August 2, 2012
    Date of Patent: May 5, 2015
    Assignee: University of Southern California
    Inventor: Omid Akbari
  • Patent number: 8969397
    Abstract: Disclosed herein are systems and methods for contributing to the local treatment of pain. More specifically, the disclosed systems and methods contribute to the local treatment pain by inhibiting the NF?B family of transcription factors.
    Type: Grant
    Filed: February 5, 2010
    Date of Patent: March 3, 2015
    Assignee: Warsaw Orthopedic, Inc.
    Inventors: Eric N. Burright, Lisa L. Shafer, Bill McKay, John Zanella
  • Patent number: 8937056
    Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: January 20, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Sergei Agoulnik, Bruce Decosta, Hong Du, Yimin Jiang, Xiang-Yi Li, Kenichi Nomoto, John (Yuan) Wang, Huiming Zhang
  • Patent number: 8927587
    Abstract: The invention relates to benzimidazole and imidazopyridine derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new Nav1.8 modulators of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7. X and Y are as defined in the description. Nav1.8 modulators are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Grant
    Filed: January 29, 2013
    Date of Patent: January 6, 2015
    Assignee: Pfizer LImited
    Inventors: Sharanjeet Kaur Bagal, Alan Daniel Brown, Mark Ian Kemp, Wolfgang Klute, Laia Malet Sanz, Brian Edward Marron, Duncan Charles Miller, Sarah Elizabeth Skerratt, Mark J. Suto, Christopher William West
  • Patent number: 8916562
    Abstract: Improved methods and compositions for safe and effective treatment of telangiectasia or a symptom associated with telangiectasia in a subject are described. The methods involve topically applying to an affected skin area a topical composition comprising about 0.3% to about 10% by weight of brimonidine and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 25, 2011
    Date of Patent: December 23, 2014
    Assignee: Galderma Research & Development SNC
    Inventors: Michael Graeber, Christian Loesche, Philip Freidenreich, Yin Liu, Matthew James Leoni
  • Publication number: 20140343077
    Abstract: A compound of formula (I) useful for the treatment or prevention of hepatitis C viral infection, (Formula (I)) wherein: X1 and X2 are each independently CRB or N; RB is H, (C1-6)alkyl, (C1-6)haloalkyl, halo.
    Type: Application
    Filed: August 22, 2012
    Publication date: November 20, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Christian Brochu, Chantal Grand-Maitre, Lee Fader, Cyrille Kuhn, Megan Bertrand-Laperle, Marc Pesant
  • Patent number: 8853251
    Abstract: The present invention relates to method of treating retinal diseases in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: November 4, 2013
    Date of Patent: October 7, 2014
    Assignee: Allergan, Inc.
    Inventors: Mohammed I. Dibas, Daniel W. Gil, Ken Chow, Liming Wang, Michael E. Garst, John E. Donello
  • Patent number: 8846739
    Abstract: TGR5 agonists of structural formula VIII(Q), wherein X, R1, R2, and R5 are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Exelixis Patent Company LLC
    Inventors: Venkataiah Bollu, Brant Clayton Boren, Jackaline Dalgard Julien, Brenton T. Flatt, Nadia Haq, Sarah Hudson, Raju Mohan, Michael Morrissey, Benjamin Pratt
  • Patent number: 8835471
    Abstract: There is provided a compound of formula I, wherein Y1, Y2, Y3, Y4, Z1, Z2, R1, R2, R3, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, for use in the treatment of spinal cord injury.
    Type: Grant
    Filed: June 9, 2011
    Date of Patent: September 16, 2014
    Inventors: Ulrike Steckelings, Thomas Unger
  • Publication number: 20140249195
    Abstract: Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided
    Type: Application
    Filed: April 14, 2014
    Publication date: September 4, 2014
    Applicant: THERON PHARMACEUTICALS, INC
    Inventors: Jürg R. PFISTER, Gwenaella RESCOURIO, Meenakshi S. VENKATRAMAN, Xiaoming ZHANG
  • Publication number: 20140221383
    Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
    Type: Application
    Filed: April 14, 2014
    Publication date: August 7, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Hallet, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
  • Patent number: 8795729
    Abstract: The present invention provides methods for feeding older sows that beneficially reduce feed intake in older sows, yet improve pig survival and weaning weight of pigs from older sows.
    Type: Grant
    Filed: December 30, 2013
    Date of Patent: August 5, 2014
    Assignee: APC, Inc.
    Inventors: Joe David Crenshaw, Joy Campbell, Louis E. Russell
  • Patent number: 8785488
    Abstract: The present invention comprises TGR5 agonists of structural formula I, wherein X, R1, R2, and R5 are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: July 22, 2014
    Assignee: Exelixis Patent Company LLC
    Inventors: Venkataiah Bollu, Brant Clayton Boren, Jackaline Dalgard Julien, Brenton T. Flatt, Nadia Haq, Sarah Hudson, Raju Mohan, Michael Morrissey, Benjamin Pratt, Tie-Lin Wang, Richard Martin, Xiao-Hui Gu
  • Patent number: 8741928
    Abstract: Provided are protected antimicrobial compounds which are useful for controlling microorganisms in aqueous or water-containing systems, such as oil or gas field fluids, at elevated temperature. The antimicrobial compounds are of the formula I: wherein R, R1, R2, X and Y are as defined herein.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: June 3, 2014
    Assignees: Dow Global Technologies LLC, ANGUS Chemical Company
    Inventors: Charles E. Coburn, Michael V. Enzien, Heather R. Mcginley, David W. Moore
  • Patent number: 8735437
    Abstract: The present invention relates to imidazolidinecarboxamide derivatives of the general formula I, wherein R, R1, R2, X and Y are as defined herein, or pharmaceutically usable salts thereof and the use thereof as medicinal substances.
    Type: Grant
    Filed: October 2, 2009
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventors: Gerhard Zoller, Stefan Petry, Gunter Müller, Norbert Tennagels
  • Patent number: 8735438
    Abstract: A compound having selective modulating activity at the alpha 2B and/or alpha 2C adrenergic receptor subtypes is represented by the general Formula 1: wherein n=1-4; X is C or N; R1-R6 can be the same or different and are independently selected from the group consisting of H, C1-6 alkyl, OCH3, OH, F, Cl, Br, CH2OH, CH2N(R7)2, C(O)R8, CH2CN, CF3, wherein R7 is H or C1-6 alkyl; and R8 is C1-6 alkyl or aryl. The compounds of Formula 1 can be incorporated in pharmaceutical compositions and used in methods of treatment of alpha 2 receptor mediated diseases and conditions.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: May 27, 2014
    Assignee: Allergan, Inc.
    Inventors: Santosh C. Sinha, Todd M. Heidelbaugh, Smita Bhat, Ken Chow, Michael Garst
  • Patent number: 8729056
    Abstract: The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be provided. The agent for the prevention and/or treatment of Hand-Foot Syndrome comprising a compound with anticholinergic activity can be safely administered to the patients with Hand-Foot Syndrome, and has shown the superior preventive and/or treatment effect against Hand-Foot Syndrome.
    Type: Grant
    Filed: March 30, 2011
    Date of Patent: May 20, 2014
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kazuhiro Ishizaka, Tadashi Nomizu, Aya Kitao
  • Patent number: 8729271
    Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: May 20, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Minoru Moriya, Akito Yasuhara, Kazunari Sakagami, Hiroshi Ohta, Kumi Abe, Shuji Yamamoto, Yuko Araki, Hiroki Urabe, Xiang-Min Sun
  • Patent number: 8729117
    Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
    Type: Grant
    Filed: September 20, 2012
    Date of Patent: May 20, 2014
    Assignee: Pharmacyclics, Inc.
    Inventors: Daniel A. Dickman, Dange Vijay Kumar, Colin O'Bryan, Roopa Rai, William Dvorak Shrader
  • Patent number: 8703964
    Abstract: The present invention is directed to pharmaceutical compositions comprising: (a) bendamustine, (b) a charged cyclopolysaccharide, and (c) a stabilizing agent having a charge opposite to that of the cyclopolysaccharide. Such composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. Such compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: April 22, 2014
    Assignee: Supratek Pharma Inc.
    Inventors: Tomasz Popek, Kishore Patel, Valery Alakhov, Grzegorz Pietrzynski
  • Patent number: 8673953
    Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: March 18, 2014
    Assignee: Allergan, Inc.
    Inventors: Stuart D. Shanler, Andrew Ondo
  • Publication number: 20140066425
    Abstract: Disclosed are substituted thioimidazolidinone compounds and pharmaceutical compositions comprising such compounds. The compounds and compositions can be used for treatment of androgen receptor-associated diseases or disorders, such as prostate cancer, benign prostatic hypertrophy, male hair loss and hypertrichosis.
    Type: Application
    Filed: March 8, 2012
    Publication date: March 6, 2014
    Applicants: SUZHOU KINTOR PHARMACEUTICALS, INC.
    Inventor: Youzhi Tong
  • Patent number: 8663695
    Abstract: The invention involves methods and formulations for treating or preventing rhinosinusitis, including fungus-induced rhinosinusitis in mammals. In one embodiment, the formulation of the present invention comprises a steroidal anti-inflammatory agent having a specific particle size distribution profile. The formulation may also comprise an antifungal agent, antibiotic or antiviral agent.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: March 4, 2014
    Assignee: Mylan Specialty L.P.
    Inventor: Imtiaz Chaudry
  • Patent number: 8653123
    Abstract: The present invention relates to method of treating retinal diseases in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl) -2-methylphenyl]methanol, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: September 15, 2011
    Date of Patent: February 18, 2014
    Assignee: Allergan, Inc.
    Inventors: Mohammad I. Dibas, Daniel W. Gil, Ken Chow, Liming Wang, Michael E. Garst, John E. Donello
  • Patent number: 8642634
    Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: July 27, 2007
    Date of Patent: February 4, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Robert James Pasteris, Mary Ann Hanagan
  • Patent number: 8642585
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Sara Frattini, Dieter Hamprecht, Frank Himmelsbach, Elke Langkopf, Iain Lingard, Stefan Peters, Holger Wagner
  • Patent number: 8642278
    Abstract: The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non-small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.
    Type: Grant
    Filed: November 22, 2006
    Date of Patent: February 4, 2014
    Assignee: University of South Florida
    Inventors: Said M. Sebti, Srikumar Chellappan, Nicholas James Lawrence
  • Patent number: 8632812
    Abstract: The present invention provides methods for feeding older sows that beneficially reduce feed intake in older sows, yet improve pig survival and weaning weight of pigs from older sows.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: January 21, 2014
    Assignee: APC, Inc.
    Inventors: Joe David Crenshaw, Joy Campbell, Louis E. Russell
  • Patent number: 8633233
    Abstract: Methods of treating a TRPC5 mediated disorder in a subject by administering an effective amount of a TRPC5 antagonist, such as a compound disclosed herein, are described.
    Type: Grant
    Filed: August 6, 2009
    Date of Patent: January 21, 2014
    Assignee: Hydra Biosciences, Inc.
    Inventors: Jayhong Chong, Christopher Fanger, Magdalene M. Moran, Elisha Singer, Timothy Strassmaier, Howard Ng
  • Patent number: 8633182
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: January 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dieter Hamprecht, Sara Frattini, Iain Lingard, Stefan Peters
  • Patent number: 8633235
    Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
    Type: Grant
    Filed: September 24, 2004
    Date of Patent: January 21, 2014
    Assignee: Neomed Institute
    Inventors: Ziping Liu, Daniel Pagé, Christopher Walpole, Hua Yang
  • Patent number: 8623898
    Abstract: The present invention aims to provide novel compounds of formula [I] or pharmaceutically acceptable salts thereof that are based on a glycine uptake inhibiting action and which are useful in the prevention or treatment of such diseases as schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsory disorder, social anxiety disorder, posttraumatic stress disorder, specific phobia, acute stress disorder, etc.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: January 7, 2014
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Akito Yasuhara, Shuji Yamamoto, Hiroshi Ohta, Yoshihisa Shirasaki, Kazunari Sakagami, Masato Hayashi, Tsuyoshi Shibata, Youichi Shimazaki, Yuko Araki, Kumi Abe, Xiang-Min Sun
  • Patent number: 8623899
    Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
    Type: Grant
    Filed: August 6, 2010
    Date of Patent: January 7, 2014
    Assignee: Janssen Research & Development Ireland
    Inventors: David McGowan, Samuel Dominique Demin, Stefaan Julien Last, Koen Vandyck, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 8618148
    Abstract: The present invention relates to a method for the prophylaxis of vascular headaches which do not originate from hypertension, especially migraine, the method comprising administration of telmisartan to a subject in need of such a treatment. The present invention relates also to a method for the prophylaxis of vascular headaches, comprising the co-administration of telmisartan in combination with other drugs suitable for migraine prophylaxis and/or acute treatment of migraine.
    Type: Grant
    Filed: June 16, 2006
    Date of Patent: December 31, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Giora Davidai
  • Patent number: 8618149
    Abstract: Disclosure is provided for methods of preventing, removing or inhibiting microbial biofilm formation or microbial infection in a plant or plant part thereof, including applying thereto a treatment effective amount of an active compound as described herein, or an agriculturally acceptable salt thereof. Methods of enhancing a microbicide (e.g., including a copper, antibiotic, bacteriophage, etc.) and/or plant defense activator are also provided, including applying an active compound as described herein. Compositions comprising an active compound as described herein in an agriculturally acceptable carrier are also provided, and in some embodiments the compositions further include a microbicide (e.g., including copper, antibiotic, bacteriophage, etc.) and/or plant defense activator.
    Type: Grant
    Filed: August 31, 2012
    Date of Patent: December 31, 2013
    Assignee: North Carolina State University
    Inventors: Christian Melander, John Cavanagh, David Ritchie, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards, Thomas W. Lindsey, Jonathan S. Lindsey
  • Patent number: 8609640
    Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: December 17, 2013
    Assignee: Eisai, Inc.
    Inventors: Sergei Agoulnik, Bruce Decosta, Hong Du, Yimin Jiang, Xiang-Yi Li, Kenichi Nomoto, John (Yuan) Wang, Huiming Zhang, Jiayi Wu