Q Is Acyclic And Benzene Ring In A Substituent E Patents (Class 514/605)
  • Publication number: 20130274297
    Abstract: The invention provides a composite of drug, polymeric carrier and at least one not cross linked polymer useful to improve the solubility of poorly water soluble drugs. The present invention comprises manufacturing process of this composite material. The manufacturing process is carried out by the solvent induced activation process, wherein the not cross-linked polymer is loaded into the composite from organic solution, possibly together with the drug. Pharmaceutical compositions comprising said composite in combination with pharmaceutical acceptable excipients are also described herein.
    Type: Application
    Filed: December 22, 2011
    Publication date: October 17, 2013
    Applicant: APTALIS PHARMA LIMITED
    Inventors: Paolo Gatti, Italo Colombo, Dario Gervasoni, Vincenza Pironti, Lia Alborghetti, Flavio Fabiani, Luigi Boltri
  • Patent number: 8557872
    Abstract: This present disclosure relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present disclosure provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.
    Type: Grant
    Filed: January 28, 2009
    Date of Patent: October 15, 2013
    Assignee: Amorepacific Corporation
    Inventors: Song Seok Shin, Jin Kwan Kim, Sun-Young Kim, Ki-Wha Lee, Byoung Young Woo, Joo-Hyun Moh, Yeon Su Jeong, Kyung Min Lim, Jin Kyu Choi, Hyun-Ju Koh, Young-Ho Park
  • Publication number: 20130252890
    Abstract: The invention relates to selective oestrogen receptor modulators (SERM) and methods of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of bleeding disorders, osteoporosis, endometriosis, myomata, hormone-dependent tumours, for hormone replacement therapy and for contraception.
    Type: Application
    Filed: June 21, 2011
    Publication date: September 26, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Tim Wintermantel, Carsten Möller, Ulrich Bothe, Reinhard Nubbemeyer, Ludwig Zorn, Dirk Kosemund, Antonius Ter Laak, Rolf Bohlmann, Lars Wortmann, Donald Bierer
  • Publication number: 20130244995
    Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
    Type: Application
    Filed: November 21, 2011
    Publication date: September 19, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Per Vedsø, Lars Kristian Albert Blæhr
  • 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: 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
  • Publication number: 20130197074
    Abstract: A method for treating an aging-related disease is disclosed comprising administering to a subject a pharmaceutical composition comprising an adrenergic beta-3-receptor agonist.
    Type: Application
    Filed: January 30, 2013
    Publication date: August 1, 2013
    Inventors: Shuguang LIN, Meng ZHENG
  • Publication number: 20130184279
    Abstract: Compounds of formula Ia and Ib wherein A, B, C, R1 and R14 are described herein.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 18, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130184342
    Abstract: The technology described herein relates to methods of inducing cell death. The technology described herein further relates to treating conditions including cancers and autoimmune diseases comprising administering inhibitors of double strand break repair. Also described herein are inhibitors of double strand break repair and methods of screening for such inhibitors.
    Type: Application
    Filed: March 13, 2013
    Publication date: July 18, 2013
    Applicant: THE JACKSON LABORATORY
    Inventor: THE JACKSON LABORATORY
  • Publication number: 20130172388
    Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 4, 2013
    Applicant: University of Pittsburgh -- Of the Commonwealth System of Higher Education
    Inventor: University of Pittsburgh -- Of the Commonwealth System of Higher Education
  • Patent number: 8461209
    Abstract: The invention provides a sulfonyl malonamide derivative, or a pharmacologically acceptable salt thereof or a solvate thereof, that has therapeutic and/or preventive effects(s) on various diseases due to its agonist action at AT2 receptor, and is useful as a pharmaceutical agent for the treatment and/or prevention of diseases involving the renin-angiotensin-aldosterone system (RAAS).
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: June 11, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Tomohiro Yoshida, Hiroshi Sakashita, Atsushi Numata, Saori Tahara, Hisashi Kawasumi
  • Publication number: 20130131180
    Abstract: A compound represented by the following general formula (I) which has ADAM17 inhibitory activity, or a salt thereof, or a solvate thereof: wherein X represents a phenylene group; Y represents a hydrogen atom, —(CH2)mR1 or the like; R1 represents —NR5COR2, —NR5SO2R2 or —NR3R4; R2 represents a C1-C6 alkyl group, an aryl group, or a C1-C6 alkoxy group; R3 and R4 represent a C1-C6 alkyl group and the like; R5 represents a hydrogen atom or a C1-C6 alkyl group or the like; m indicates an integer of from 0 to 4; and Z represents a hydrogen atom or a C1-C6 alkyl group.
    Type: Application
    Filed: July 5, 2011
    Publication date: May 23, 2013
    Applicant: KAKEN PHARMACEUTICAL CO., LTD.
    Inventors: Kentaro Kawai, Shigeru Miyamoto, Masanao Shimano, Makoto Haino
  • 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: 20130109701
    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 sulfon-amide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar1, 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 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: 20130059908
    Abstract: The use of sulfonamides of formula (I) wherein R and R1 are as defined in the description, for the preparation of medicaments for the prevention of diabetes, in particular of type-1 diabetes is herein disclosed.
    Type: Application
    Filed: October 6, 2010
    Publication date: March 7, 2013
    Applicant: DOMPE' S.P.A.
    Inventors: Lorenzo Piemonti, Luisa Daffonchio, Marcello Allegretti
  • Publication number: 20130059851
    Abstract: A method of identifying a subject having cancer who is likely to benefit from treatment with a combination therapy with a RAF inhibitor and a second inhibitor is provided. A method of treating cancer in a subject in need thereof is also provided and includes administering to the subject an effective amount of a RAF inhibitor and an effective amount of a second inhibitor, wherein the second inhibitor is a MEK inhibitor, a CRAF inhibitor, a CrkL inhibitor or a TPL2/COT inhibitor. A method of identifying a kinase target that confers resistance to a first inhibitor is also provided.
    Type: Application
    Filed: March 9, 2011
    Publication date: March 7, 2013
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Levi A. Garraway, Cory M. Johannessen
  • Patent number: 8389500
    Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (IA) or (IB): as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: March 5, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Xiaofen Li, Thao Perry, Jeff Zablocki
  • Patent number: 8377947
    Abstract: Use of a composition for treating Alzheimer's disease, osteoporosis, sleep apnea, erectile dysfunction, McArdle disease, or a carbohydrate metabolism disorder, or for reducing aging or fatigue. The composition includes a first agent selected from the group consisting of an oxidative phosphorylation inhibitor, an ionophore, and an adenosine 5?-monophosphate-activated protein kinase activator; a second agent that possesses anti-inflammatory activity; and a third agent that possesses serotonin activity.
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: February 19, 2013
    Inventor: Chien-Hung Chen
  • Publication number: 20130022611
    Abstract: The invention provides methods and compositions for modulating hepsin activity and the uPA/plasmin pathway, in particular by regulating pro-uPA activation by hepsin.
    Type: Application
    Filed: May 25, 2012
    Publication date: January 24, 2013
    Applicant: Genentech, Inc.
    Inventors: Daniel K. Kirchhofer, Paul M. Moran
  • Publication number: 20120322823
    Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.
    Type: Application
    Filed: August 28, 2012
    Publication date: December 20, 2012
    Inventors: Anton F. J. Fliri, Randall James Gallaschun, Christopher John O'Donnell, Jacob Bradley Schwarz, Barbara E. Segelstein
  • Patent number: 8334328
    Abstract: The main goal of the present invention is the development of a polymerizable material for isolation and protection of the gums and generally the soft tissues of the oral cavity. For better protection during various procedures of the dental surfaces. The composition of the material can contain many other substances that strengthen its qualities and protective action. Such substances can be various substances that have antioxidative, sedative, anti-inflammatory, analgesic, anti-irritant action etc.
    Type: Grant
    Filed: February 9, 2007
    Date of Patent: December 18, 2012
    Assignee: KLOX Technologies Inc.
    Inventors: Vassilios Marmarinos, Paschalis Paschalakis
  • Patent number: 8324178
    Abstract: Methods for treating or preventing cardiomyopathy in a subject by administering an ?1 adrenergic receptor agonist, wherein the treatment does not result in increased blood pressure are provided.
    Type: Grant
    Filed: November 2, 2009
    Date of Patent: December 4, 2012
    Assignee: The Regents of the University of California
    Inventor: Paul C. Simpson, Jr.
  • Publication number: 20120270876
    Abstract: Methods are provided for treating a subject for a condition caused by an abnormality in the subject's autonomic nervous system. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is pharmacologically modulated with at least one beta-blocker in a manner that is effective to treat the subject for the condition. The subject methods find use in the treatment of a variety of different conditions, where such conditions include various disease conditions. Also provided are systems and kits for use in practicing the subject methods.
    Type: Application
    Filed: April 24, 2012
    Publication date: October 25, 2012
    Inventors: Anthony Joonkyoo Yun, Patrick Yuarn-Bor Lee
  • Publication number: 20120269804
    Abstract: The present invention relates to substituted benzosulphonamide compounds of general formula (I): in which R1, R2, R3, R4, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: October 7, 2010
    Publication date: October 25, 2012
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Marion Hitchcock, Ingo Hartung, Florian Pühler
  • Publication number: 20120269803
    Abstract: The present invention relates to substituted benzosulphonamide compounds of general formula (I): in which R1, R2, R3, R4, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: October 12, 2010
    Publication date: October 25, 2012
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Marion Hitchcock, Ingo Hartung, Florian Pühler
  • Publication number: 20120202884
    Abstract: The invention relates to CXCR1 and/or CXCR2 inhibitors for the preparation of a medicament for use as an adjuvant in the transplant of pancreatic islets in Type 1 diabetes patients. In particular, the compounds that can be used according to the invention have the following formula (I) in which R and R? are as defined in the description.
    Type: Application
    Filed: October 6, 2010
    Publication date: August 9, 2012
    Applicant: DOMPE' S.P.A.
    Inventors: Lorenzo Piemonti, Luisa Daffonchio, Marcello Allegretti
  • Publication number: 20120202781
    Abstract: The present invention relates to anindane derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising one or more of said indane derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.
    Type: Application
    Filed: April 8, 2010
    Publication date: August 9, 2012
    Inventors: Kevin James Gillen, Jonathan Gillespie, Craig Jamieson, John Kinnaird Ferguson MacLean, Elizabeth Margaret Moir, Zoran Rankovic
  • Publication number: 20120178757
    Abstract: A method is provided for the prevention of cancer metastasis in a patient comprising administering an adrenergic receptor antagonist to a patient in need thereof. The invention also includes an adrenergic receptor antagonist for use in the prevention of tumour recurrence in a patient. Also provided is a kit of parts for use in such methods comprising an adrenergic receptor antagonist, and an administration vehicle. A method is further included for identifying a patient at risk of developing cancer comprising the step of assaying for levels of expression of adrenergic receptor genes and proteins in said patient.
    Type: Application
    Filed: December 8, 2011
    Publication date: July 12, 2012
    Applicant: NOTTINGHAM UNIVERSITY HOSPITALS NHS TRUST
    Inventor: Desmond George Powe
  • Publication number: 20120178724
    Abstract: In accordance with the present invention, novel methods and formulations are provided for treating and preventing the incidence of drug-induced pro-arrhythmia, including torsades de pointes. The methods and formulations comprise a combination of a drug that induces torsade de pointes, such as Class III antiarrhythmics, certain antimicrobials, antihistamines, antidepressants, antipsychotics, diuretics, with an aspirin and/or a statin. In certain embodiments, the compositions and methods for treatment comprise azimilide and aspirin and/or a statin. These compositions may be administered by different routes, including orally. In certain embodiments where the antiarrhythmic is azimilide it may be administered orally in a dose of about 25 mg to about 300 mg.
    Type: Application
    Filed: March 22, 2012
    Publication date: July 12, 2012
    Applicant: WARNER CHILCOTT COMPANY, LLC
    Inventors: Joseph Michael Sprafka, II, Jose Mauro Goulart-Brum
  • Publication number: 20120165360
    Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: March 5, 2012
    Publication date: June 28, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
  • Patent number: 8198330
    Abstract: A method of treatment or prophylaxis of diabetes, obesity, dyslipidemia or metabolic syndrome includes administering an effective amount of a benzylamine derivative represented by Formula (I): wherein, R1 represents an alkyl group having 1 to 6 carbon atoms; R2 represents an alkyl group having 1 to 6 carbon atoms; R3 and R5 each independently represent a halogen atom, an alkyl group having 1 to 6 carbon atoms, a haloalkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms; and R4 represents a hydrogen atom or an alkoxy group having 1 to 6 carbon atoms, or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: July 31, 2009
    Date of Patent: June 12, 2012
    Assignee: Toray Industries, Inc.
    Inventors: Ko Hasebe, Satoru Yoshikawa, Hideki Kozono, Seiji Okazaki
  • Patent number: 8183293
    Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: May 22, 2012
    Assignee: Amgen Inc.
    Inventors: Mark Grillo, An-Rong Li, Jiwen Liu, Julio C. Medina, Yongli Su, Yingcai Wang, Janan Jona, Alan Allgeier, Jacqueline Milne, Jerry Murry, Joseph F. Payack, Thomas Storz
  • Publication number: 20120115816
    Abstract: The invention includes aqueous compatibilized pesticidal formulations and methods of making them. In typical embodiments, formulations comprise a first electrolytic pesticide and a second electrolytic pesticide, and about 30 to about 300 g/L of at least one alkyl polyglycoside. The invention also includes methods of preparing pesticidal formulations to increase the concentration of the electrolytic pesticides. The invention also includes storage and transport systems containing formulation embodiments. The invention also includes methods inhibiting pests.
    Type: Application
    Filed: March 4, 2010
    Publication date: May 10, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Julia Lynne Ramsay, David Stock, Gordon Alstair Bell, Claudio Screpanti, Colin Douglas Miln, Henry Ebun Agbaje, Charles A. Jones, III, Ravi Ramachandran
  • Publication number: 20120095092
    Abstract: The invention provides a compound of formula (I), a pharmaceutical composition thereof, a method of preparing a medicament for the treatment of a cancer, and a method of treating cancers. The invention exhibits merits against cancers such as significantly higher potency and effectiveness over a broader range of cancers. In formula (I), Ra is a benzyl group with alkyl and/or alkoxy; Rb is selected from H and alkyl groups; Rf is an alkyl; and R3 is selected from a substituted phenyl, a heterocyclic group, and wherein Rc is selected from a fused ring, fused rings, and any bivalent cyclic group.
    Type: Application
    Filed: October 18, 2010
    Publication date: April 19, 2012
    Inventors: Bin Su, Aimin Zhou, Yan Xu
  • Publication number: 20120088839
    Abstract: The present invention relates to a composition for inhibiting cellular senescence, comprising N-[2-(cyclohexyloxyl)-4-nitrophenyl]-methanesulfonamide.
    Type: Application
    Filed: November 29, 2011
    Publication date: April 12, 2012
    Inventors: Sang Chul PARK, Jeong A. HAN
  • Publication number: 20120088746
    Abstract: Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
    Type: Application
    Filed: May 10, 2007
    Publication date: April 12, 2012
    Applicants: PFIZER INC., RENOVIS, INC.
    Inventors: Yuji Shishido, Kazunari Nakao, Satoshi Nagayama, Hirotaka Tanaka, Matthew Alexander James Duncton, Matthew Cox, John Kincaid, Kiran Sahasrabudhe, Maria de Los Angeles Estiarte-Martinez
  • Publication number: 20120082646
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: March 25, 2010
    Publication date: April 5, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
  • Patent number: 8148427
    Abstract: The benzylamine derivative represented by the formula below and a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutical containing the derivative or the pharmaceutically acceptable acid addition salt thereof, and a therapeutic or prophylactic agent for pollakiuria or urinary incontinence containing the derivative or the pharmaceutically acceptable acid addition salt thereof are provided. The benzylamine derivative of the present invention and the pharmaceutically acceptable acid addition salt thereof have less possibility of occurrence of side effects than known compounds, and show a better therapeutic effect against pollakiuria or urinary incontinence, so that they can be used as excellent therapeutic or prophylactic agents for pollakiuria or urinary incontinence.
    Type: Grant
    Filed: January 31, 2008
    Date of Patent: April 3, 2012
    Assignee: Toray Industries, Inc.
    Inventors: Ryoji Hayashi, Tsukasa Kikuchi, Masaki Arai, Satoshi Kurosawa, Ko Hasebe, Sayoko Kanie, Seiichiro Ozono, Atsushi Otsuka
  • Patent number: 8148422
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: April 3, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Mark J. Macielag, James J. McNally
  • Publication number: 20120063996
    Abstract: The present invention provides nanoparticulate nimesulide compositions. The compositions preferably comprise nimesulide and at least one surface stabilizer adsorbed on or associated with the surface of the nimesulide particles. The nanoparticulate nimesulide particles preferably have an effective average particle size of less than about 2000 nm. The invention also provides methods of making and using nanoparticulate nimesulide compositions.
    Type: Application
    Filed: July 28, 2011
    Publication date: March 15, 2012
    Inventors: H. William Bosch, Christian F. Wertz
  • Patent number: 8097652
    Abstract: The present invention relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: January 17, 2012
    Assignee: Eli Lilly and Company
    Inventor: Esteban Dominguez-Manzanares
  • Publication number: 20120010207
    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 (I): or a pharmaceutically acceptable salt thereof, wherein Ar1, X, 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 11, 2011
    Publication date: January 12, 2012
    Applicant: PFIZER LIMITED
    Inventors: Andrew Simon Bell, Alan Daniel Brown, Russell Andrew Lewthwaite, Ian Roger Marsh, David Simon Millan, Manuel Perez Pacheco, David James Rawson, Nunzio Sciammetta, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Marcel John De Groot
  • Publication number: 20120004264
    Abstract: 4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.
    Type: Application
    Filed: September 15, 2011
    Publication date: January 5, 2012
    Applicant: Dompé pha.r.ma S.p.A.
    Inventors: Marcello Allegretti, Marla Candida Cesta, Riccardo Bertini, Marco Mosca, Francesco Colotta
  • Publication number: 20120003318
    Abstract: Methods of treating atrial arrhythmia include administering an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof, such that the at least one antiarrhythmic pharmaceutical agent first enters the heart through the pulmonary vein to the left atrium. Other methods of treating atrial arrhythmia include administering by inhalation an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof. An amount of the at least one antiarrhythmic pharmaceutical agent may peak in the coronary sinus of the heart at a time ranging from 10 seconds to 30 minutes from initiation of the administering. Unit doses, aerosols, and kits are also contemplated.
    Type: Application
    Filed: March 18, 2010
    Publication date: January 5, 2012
    Inventors: Carlos A. Schuler, Rangachari Narasimhan
  • Publication number: 20110281853
    Abstract: The present invention provides compositions and methods for treating or preventing atrial fibrillation (AF). In particular, the present invention provides administration of muscarinic receptor antagonists (e.g., M2-selective muscarinic receptor blockers), administered alone or in combination with other therapeutic agents (e.g., beta-adrenergic receptor blockers) to treat and/or prevent atrial fibrillation.
    Type: Application
    Filed: May 12, 2011
    Publication date: November 17, 2011
    Inventors: Rishi Arora, David E. Zembower
  • Publication number: 20110275619
    Abstract: Inhibitors of BACE1 and compositions containing them are described. Use of the inhibitors and compositions containing them to treat Alzheimer's disease are described.
    Type: Application
    Filed: December 4, 2009
    Publication date: November 10, 2011
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventor: Arun K. Ghosh
  • Publication number: 20110275719
    Abstract: The present invention is directed to a novel trifluoromethylsulfonamide derivative which inhibits the processing of APP by the putative ?-secretase and thus is useful in the treatment or prevention of Alzheimer's disease. This compound possesses favorable pharmacokinetic properties in higher species (rhesus) and thus can be dosed on an intermittent dosing regiment (e.g., once weekly). When dosed on such a regiment the compound exhibits significant and continuous A? lowering without the manifestation of Notch associated gastrointestinal toxicity for extended periods, e.g., 7 days. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: January 29, 2010
    Publication date: November 10, 2011
    Inventors: Matthew Daniels, Jed Hubbs, Thomas Miller
  • Patent number: RE42889
    Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: November 1, 2011
    Assignee: G.D. Searle LLC
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
  • Patent number: RE43327
    Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: April 24, 2012
    Assignee: Aminex Therapeutics, Inc.
    Inventors: Mark R. Burns, Gerard F. Graminski, Nand Baindur
  • Patent number: RE43802
    Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: September 21, 2011
    Date of Patent: November 13, 2012
    Assignee: G.D. Searle LLC
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz