Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/351)
  • Publication number: 20130281469
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: June 7, 2013
    Publication date: October 24, 2013
    Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier
  • Patent number: 8558001
    Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: October 15, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G. Strickley, Chandrasekar Venkataramani, Jeff Zablocki
  • Publication number: 20130245019
    Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.
    Type: Application
    Filed: April 30, 2013
    Publication date: September 19, 2013
    Applicant: CONGENIA SRL
    Inventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
  • Publication number: 20130237571
    Abstract: The present invention relates to compounds that have the ability to modulate the activity of GPR40 and are therefore useful in the treatment of GPR40 related disorders. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders related to GPR40 activity.
    Type: Application
    Filed: July 20, 2011
    Publication date: September 12, 2013
    Applicant: Conexios Life Sciences PVT. LTD.
    Inventors: Jagannath Madanahalli Ranganath Rao, Nagarajan Arumugam, Mohd Mudabbir Ansari, Chandrasekhas Gudla, Shanmugam Pachiyappan, Manivannan Ramalingam, Jenson George, George Fernanda Arul, Kenchegowda Bommegowda, Y, Sathesh Kumar Angupillai, Ramamoorthy Kottamalai, Pradeep Jidugu, Shivanageshwara Rao, D
  • Publication number: 20130236434
    Abstract: A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of ?4?1, ?5?1, ?4?7, ?v?3 and ?L?2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.
    Type: Application
    Filed: November 16, 2011
    Publication date: September 12, 2013
    Applicant: TEXAS HEART INSTITUTE
    Inventors: Ronald J. Biediger, William C. Gundlach, IV, Robert V. Market, Michael M. Savage, Peter Vanderslice
  • Publication number: 20130237539
    Abstract: The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed.
    Type: Application
    Filed: April 15, 2013
    Publication date: September 12, 2013
    Applicant: The General Hospital Corporation
    Inventors: Michael Andrew Foley, Robert Gould, Peter Elliott, Anna Mandinova, Sam W. Lee
  • Patent number: 8530502
    Abstract: The present invention discloses methods of application employing B51B6 vitamins in molecular transport creams or gels to deliver B6 in a high dose to bring about therapeutic ways in human or mammal tissues to reverse a disease process or injury to bring about normal function of the affected tissues. Examples of disease changes to normal include, but are not limited to strokes, cellulitis, facial acne, precancerous lesions, nerve injury like paresthesia, periorbital hematoma, pentathol general anesthesia recovery, headaches, improved sight, hypothyroidism, dental pain, dental gingivitis, insect bites, delayed hypersensitivity states, phlebitis of veins and synergism of steroid activity.
    Type: Grant
    Filed: May 8, 2009
    Date of Patent: September 10, 2013
    Assignee: Dr. N's Health Care Products, LLC
    Inventor: Alfred A. Nickel
  • Publication number: 20130225619
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: January 18, 2013
    Publication date: August 29, 2013
    Applicant: Acucela Inc.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • Publication number: 20130202573
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: June 15, 2011
    Publication date: August 8, 2013
    Applicant: Ardea Biosciences, Inc.
    Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier, Chixu Chen
  • Publication number: 20130203704
    Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
    Type: Application
    Filed: March 8, 2013
    Publication date: August 8, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • Publication number: 20130203779
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: April 4, 2013
    Publication date: August 8, 2013
    Applicant: Ardea Biosciences, Inc.
    Inventor: Ardea Biosciences, Inc.
  • Publication number: 20130197039
    Abstract: The present invention provides compounds of Formula below: and analogues thereof where the various substituent groups, R1, R2, R3, R4, R5 A, and X are described herein; or a pharmaceutical salt thereof; a method of treating a condition such as hypertriglyceridemia and a process for preparing the compounds.
    Type: Application
    Filed: January 24, 2013
    Publication date: August 1, 2013
    Applicant: Eli Lilly and Company
    Inventor: Eli Lilly and Company
  • Patent number: 8476257
    Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Grant
    Filed: December 3, 2008
    Date of Patent: July 2, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
  • Patent number: 8470854
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Grant
    Filed: April 12, 2012
    Date of Patent: June 25, 2013
    Assignee: Bristol-Meyers Squibb Company
    Inventor: Donald J. P. Pinto
  • Publication number: 20130158036
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: November 1, 2012
    Publication date: June 20, 2013
    Applicant: PANMIRA PHARMACEUTICALS, LLC
    Inventor: PANMIRA PHARMACEUTICALS, LLC
  • Patent number: 8461344
    Abstract: Polymorph forms of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine p-hydroxybenzoate, and methods for their preparation, pharmaceutical composition containing said polymorph(s) and use, are disclosed. The polymorphs can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.
    Type: Grant
    Filed: May 8, 2007
    Date of Patent: June 11, 2013
    Assignee: Targacept, Inc.
    Inventors: Gary M. Dull, Julio A. Munoz
  • Patent number: 8461183
    Abstract: The present invention relates to novel PPAR agonist compounds as well as pharmaceutical compositions containing them. The compounds according to the invention are of quite particular therapeutic interest, notably for treating diabetes and/or dyslipidemias, as well as for preventing cardiovascular pathologies.
    Type: Grant
    Filed: May 26, 2009
    Date of Patent: June 11, 2013
    Assignee: Genfit
    Inventors: Christophe Masson, Karine Caumont-Bertrand
  • Patent number: 8450347
    Abstract: The invention relates to a method of controlling feelings of pain in infants or diseased or elderly persons using a complete nutrition or a nutritional supplement. The method comprises administering increased levels of folic acid, vitamin B6 and vitamin B12 or their functional equivalents.
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: May 28, 2013
    Assignee: N.V. Nutricia
    Inventors: Robert Johan Joseph Hageman, Jacob Geert Bindels
  • Publication number: 20130123234
    Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: December 20, 2012
    Publication date: May 16, 2013
    Applicants: EISAI R&D MANAGEMENT CO., LTD., EPIZYME, INC.
    Inventors: EPIZYME, INC., EISAI R&D MANAGEMENT CO., LTD.
  • Publication number: 20130116285
    Abstract: The invention relates to sulfonamide 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 a new sulfonamide Nav1.7 inhibitors of formula 10 (I):(I) or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Application
    Filed: July 6, 2011
    Publication date: May 9, 2013
    Applicant: Pfizer Limited
    Inventors: Andrew Simon Bell, Alan Daniel Brown, Russell Andrew Lewthwaite, Manuel Perez-Pacheco, David James Rawson, Robert Ian Storer, Nigel Alan Swain
  • Publication number: 20130109655
    Abstract: This invention relates to a method of mitigating side effects of non-steroidal anti-inflammatory drugs, specifically to administration of a pyridine derivative to mitigate and/or prevent prostaglandin e2 reducing side effects of non-steroidal anti-inflammatory drugs. Also provided is the use of a pyridine derivative in the preparation of a medicament for the reduction of said side effects of non-steroidal anti-inflammatory drugs, and a pharmaceutical composition comprising a non-steroidal anti-inflammatory drug and a pyridine derivative.
    Type: Application
    Filed: October 31, 2011
    Publication date: May 2, 2013
    Inventors: Serghei Gargaun, Ana Gargaun
  • Publication number: 20130109708
    Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to 5 compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I):10 X NH O S O O R1 R2 R5 R4 R3 Het1 (I) or a pharmaceutically acceptable salt thereof, wherein X, Het1, R1, R2, R3, R4 and R5 are as defined in the description. 15 Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Application
    Filed: July 4, 2011
    Publication date: May 2, 2013
    Applicant: Pfizer Limited
    Inventors: Alan Daniel Brown, David James Rawson, Robert Ian Storer, Nigel Alan Swain
  • Publication number: 20130102597
    Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: October 15, 2012
    Publication date: April 25, 2013
    Applicant: INTERMUNE, INC.
    Inventor: INTERMUNE, INC.
  • Patent number: 8426449
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Grant
    Filed: March 25, 2009
    Date of Patent: April 23, 2013
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Brian Andrew Stearns, Yen Pham Truong, Thomas Jon Seiders
  • Publication number: 20130096162
    Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 3, 2012
    Publication date: April 18, 2013
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Publication number: 20130096161
    Abstract: The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: July 8, 2011
    Publication date: April 18, 2013
    Applicant: N30 PHARMACEUTICALS, INC.
    Inventors: Xicheng Sun, Jian Qiu
  • Patent number: 8410115
    Abstract: Alpha 4 inhibitors are used in treatment of inflammatory and autoimmune diseases, such as multiple sclerosis, Crohn's Disease, rheumatoid arthritis and asthma. Rare occurrences of progressive multifocal leucoencephalopathy during treatment with an alpha-4 agent suggest the possibility that it may be related to such treatment. Monitoring for the JC virus and educating caregivers and patients about the manifestations of progressive multifocal leucoencephalopathy can improve the safety of alpha 4 inhibitor therapy.
    Type: Grant
    Filed: February 28, 2007
    Date of Patent: April 2, 2013
    Assignee: Elan Pharmaceuticals, Inc.
    Inventor: Ivan Lieberburg
  • Patent number: 8410088
    Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: April 2, 2013
    Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.
    Inventors: Kevin W. Kuntz, Richard Chesworth, Kenneth W. Duncan, Masashi Seki, Syuji Shirotori
  • Publication number: 20130065929
    Abstract: Methods for treating and/or preventing at least one symptom of a disorder associated with oxidative stress, carbonyl stress, or combinations thereof in a subject. In some embodiments, the methods include administering to the subject an effective amount of pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing. Also provided are methods for treating or preventing a nephropathy, acute renal injury, acute renal failure, or combinations thereof in a subject, and formulations adapted for intravenous administration comprising pyridoxamine, an analog or derivative thereof, or a pharmaceutically acceptable salt of any of the foregoing.
    Type: Application
    Filed: October 24, 2012
    Publication date: March 14, 2013
    Applicant: VANDERBILT UNIVERSITY
    Inventor: VANDERBILT UNIVERSITY
  • Publication number: 20130052190
    Abstract: The present invention provides a method for the treatment of allergic and inflammatory diseases or conditions by administering a compound of Formula (I). The invention provides a method of treatment that is particularly suited for patients with a high degree of airway eosinophilia in contrast to those with a lower degree of airway eosinophilia. The invention also provides a method of treatment that is particularly suited for patients with a high atopic status in contrast to those patients with a lower atopic status.
    Type: Application
    Filed: February 22, 2012
    Publication date: February 28, 2013
    Applicant: Oxagen Limited
    Inventors: Lisa Pearce Collins, Colin Michael Perkins, Michael Hunter, Eric Roy Pettipher
  • Publication number: 20130039944
    Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
    Type: Application
    Filed: April 20, 2011
    Publication date: February 14, 2013
    Applicant: Kineta, Inc.
    Inventors: Shawn P. Iadonato, Kristin Bedard
  • Publication number: 20130035351
    Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.
    Type: Application
    Filed: August 3, 2011
    Publication date: February 7, 2013
    Applicant: SOUTHWEST RESEARCH INSTITUTE
    Inventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
  • Patent number: 8362044
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: January 29, 2013
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong, Jeffrey Roger Roppe, Nicholas Simon Stock, Jeannie M. Arruda, Thomas Jon Seiders, Bowei Wang, Deborah Volkots
  • Publication number: 20130017616
    Abstract: The present invention provides methods for treating or limiting development of inflammatory disorders.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 17, 2013
    Applicant: Vanderbilt University - Center for Technology Transfer and Commercialization
    Inventor: Billy G. Hudson
  • Publication number: 20130011379
    Abstract: The present invention provides pharmaceutical compositions comprising dosage units of pyridoxamine, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier, and methods for their use in limiting the progression of renal disease and/or diabetic complications in human diabetic patient.
    Type: Application
    Filed: April 13, 2012
    Publication date: January 10, 2013
    Applicant: NEPHROGENEX, INC.
    Inventors: Thorsten Degenhardt, Robert Schotzinger, Wesley J. Fox
  • Publication number: 20130012530
    Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 10, 2013
    Applicant: H. Lundbeck A/S
    Inventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
  • Publication number: 20130005712
    Abstract: The present invention relates to a composition for noxious organisms-controlling agent having a synergistic effect and a method for using said composition, which comprises, as active ingredients thereof, one or more compounds selected from the phthalamide derivatives represented by general formula (I) being useful as an insecticide or acaricide and one or more compounds selected from the compounds having insecticidal, acaricidal or nematocidal activity: wherein R1, R2 and R3 may be the same or different and each represent hydrogen atom, C3-C6 cycloalkyl, -A1--Qp, etc., each of X and Y may be the same or different and represents hydrogen atom, halogen atom, etc., n is an integer of 1 to 4, m is an integer of 1 to 5, and each of Z1 and Z2 represents O or S.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Inventors: Kazuyuki Sakata, Masayuki Morimoto, Hiroshi Kodama, Tetsuyosi Nishimatsu
  • Publication number: 20130005689
    Abstract: Disclosed are novel compounds having the structure of Formula (I): which are useful for treating mammals for dependence upon substances of addiction, for example addiction to a dopamine-producing agent such as cocaine, morphine, amphetamines, nicotine, and/or alcohol. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of a compound of Formula (I) and methods of using the compounds of Formula (I) in the treatment of addiction to a dopamine-producing agent.
    Type: Application
    Filed: June 29, 2012
    Publication date: January 3, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Carina E. Cannizzaro, Michael Graupe, Juan A. Guerrero, Yafan Lu, Robert G. Strickley, Chandrasekar Venkataramani, Jeff Zablocki
  • Patent number: 8334307
    Abstract: Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: December 18, 2012
    Assignee: Biotheryx Inc.
    Inventors: Frank Mercurio, Kyle W. H. Chan
  • Patent number: 8334308
    Abstract: The present invention relates to biphenyl-based renin inhibitor compounds having amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: December 18, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helene Juteau, Michel Gallant, Daniel Dube, Patrick Roy, Renee Aspiotis, Rejean Fortin, Patrick Lacombe, Daniel McKay, Tom Yao-Hsiang Wu
  • Publication number: 20120316138
    Abstract: The present invention relates to thiazolidinedione analogues and pharmaceutical compositions that are useful for treating and/or preventing obesity or diabetes, optionally in combination with a second treatment therapy such a diet restriction or an increase in duration or exertion in physical activity.
    Type: Application
    Filed: December 15, 2010
    Publication date: December 13, 2012
    Applicant: METABOLIC SOLUTIONS DEVELOPMENT COMPANY, LLC
    Inventors: Gerard R. Colca, Rolf F. Kletzien, Steven P. Tanis, Scott D. Larsen
  • Patent number: 8288420
    Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.
    Type: Grant
    Filed: May 10, 2010
    Date of Patent: October 16, 2012
    Assignee: Targacept, Inc.
    Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishakumar Basawannappa Hadimani, Haeil Park, Jared Miller Wagner, Peter A. Crooks
  • Publication number: 20120251632
    Abstract: The invention provides a method of improving one or more clinical outcomes of an individual experiencing an acute respiratory attack. The acute respiratory attack may include acute reversible bronchospasm, severe acute bronchospasm, or acute exacerbation of asthma. The method includes administering to an individual suffering from an acute respiratory attack an effective amount of bedoradrine or a pharmaceutically acceptable salt thereof in combination with a standard of care (SOC) treatment regimen.
    Type: Application
    Filed: June 15, 2012
    Publication date: October 4, 2012
    Inventors: Kazuko MATSUDA, Yuichi Iwaki, Kirk W. Johnson
  • Patent number: 8273773
    Abstract: Compounds having the formula I wherein R1, R2, R3, R4a, R4b, R4c, R5, R6, R9 and n are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: September 25, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Kenneth Albert Brameld, David Scott Carter, Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Eric Brian Sjogren, Francisco Xavier Talamas
  • Patent number: 8269008
    Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF) by inhibiting the activity of at least one HIF hydroxylase enzyme.
    Type: Grant
    Filed: December 2, 2008
    Date of Patent: September 18, 2012
    Assignee: FibroGen, Inc.
    Inventors: Michael P. Arend, Heng Cheng, Lee A. Flippin, Danny Ng, Eric D. Turtle, Min Wu
  • Publication number: 20120232111
    Abstract: The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin—inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and further provides an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent comprises one or more compounds selected from the group consisting of ?-alanine derivatives and salts thereof. The external composition for skin comprises the one or more compounds selected from the group consisting of ?-alanine derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent.
    Type: Application
    Filed: April 28, 2006
    Publication date: September 13, 2012
    Applicant: Shiseido Company, Ltd.
    Inventors: Mikiko Kaminuma, Masaru Suetsugu, Toshii Iida, Shinji Inomata
  • Patent number: 8263627
    Abstract: The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
    Type: Grant
    Filed: January 18, 2011
    Date of Patent: September 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Thomas S. Reger, Zhi-Qiang Yang
  • Publication number: 20120220592
    Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.
    Type: Application
    Filed: January 26, 2012
    Publication date: August 30, 2012
    Applicant: Newron Pharmaceuticals S.p.A.
    Inventors: Florian THALER, Mauro NAPOLETANO, Cibele SABIDO-DAVID, Ermanno MORIGGI, Carla CACCIA, Laura FARAVELLI, Alessandra RESTIVO, Patricia SALVATI
  • Patent number: 8242145
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: August 14, 2012
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Thomas Jonathan Seiders, Brian Andrew Stearns, Bowei Wang, Yen Pham Truong, Jeannie M. Arruda
  • Patent number: 8242118
    Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: August 14, 2012
    Assignee: Axikin Pharmaceuticals Inc.
    Inventors: Yingfu Li, Akihiko Watanabe, Timothy B. Lowinger, Kevin Bacon, Norihiro Kawamura, Takuya Shintani, Tetsuo Kikuchi, Toshiya Moriwaki, Klaus Urbahns, Keiko Fukushima, Noriko Nunami, Takashi Yoshino, Toshiki Murata, Megumi Yamauchi, Hiroko Yoshino