Polycyclo Ring System Is Tricyclo-carbocyclic Patents (Class 514/325)
  • Patent number: 9238014
    Abstract: Pharmaceutical composition for treating alcohol dependence in humans comprising two active ingredients: a compound having an antagonistic action on the 5-HT2 serotoninergic receptors selected as being cyproheptadine; and a compound having an antagonistic action on the alpha1-noradrenergic receptors selected from prazosin, alfuzosin, terazosin and tamsulosin.
    Type: Grant
    Filed: December 29, 2010
    Date of Patent: January 19, 2016
    Inventors: Philippe Bernard, Fabrice Trovero
  • Publication number: 20150139987
    Abstract: Treatment of homozygous familial hypercholesterolemia by administration of (R)-2-(4-((2-ethoxy-3-(4-(trifluoromethyl)phenoxy)propyl)thio)-2-methylphenoxy)acetic acid or a salt thereof, optionally in combination with an MTP inhibitor, an apoB-100 synthesis inhibitor, or a PCSK9 inhibitor.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 21, 2015
    Applicant: CymaBay Therapeutics, Inc.
    Inventors: Robert L. Martin, Charles A. McWherter, Patrick J. O'Mara
  • Publication number: 20150056274
    Abstract: Compositions, methods, and kits useful for treating hyperlipidemic conditions are provided herein. Such compositions can contain synergizing amounts of nicotinic acid, nicotinamide riboside and/or nicotinic acid metabolites in combination with leucine and/or a leucine metabolite, with or without resveratrol.
    Type: Application
    Filed: August 28, 2014
    Publication date: February 26, 2015
    Inventors: Michael Zemel, Antje Bruckbauer
  • Patent number: 8937087
    Abstract: [Problem] A compound which is useful as a dopamine D1 receptor positive allosteric modulator (D1 PAM) is provided. [Means for Solution] The present inventors have studied a compound which has a dopamine D1 receptor positive allosteric modulating activity and is useful as an active ingredient of a pharmaceutical composition for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like, and they have thus found that a heterocyclic acetamide compound has a dopamine D1 receptor positive allosteric modulating activity, thereby completing the present invention. The heterocyclic acetamide compound of the present invention has a dopamine D1 receptor positive allosteric modulating activity and can be used as an agent for preventing and/or treating cognitive impairment, negative symptoms of schizophrenia, Parkinson's disease, Alzheimer's disease, Huntington's disease, drug addictions, or the like.
    Type: Grant
    Filed: April 18, 2014
    Date of Patent: January 20, 2015
    Assignee: Astellas Pharma Inc.
    Inventors: Ryota Shiraki, Takahiko Tobe, Shimpei Kawakami, Hiroyuki Moritomo, Makoto Ohmiya
  • Publication number: 20140371207
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
    Type: Application
    Filed: December 13, 2013
    Publication date: December 18, 2014
    Applicants: Kyowa Hakko Kirin Co., Ltd., Millennium Pharmaceuticals, Inc.
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C.B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
  • Patent number: 8907096
    Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: December 9, 2014
    Assignee: High Point Pharmaceuticals, LLC
    Inventor: Soren Ebdrup
  • Patent number: 8889716
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: November 18, 2014
    Assignee: CHDI Foundation, Inc.
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas MacDonald, John Wityak
  • Publication number: 20140315905
    Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventor: Soren Ebdrup
  • Publication number: 20140303209
    Abstract: The present invention provides methods and compositions for treating hyperlipidemia and/or hypercholesterolemia comprising administering to the subject an effective amount of an MTP inhibitor to inhibit hyperlipidemia and/or hypercholesterolemia in said subject, wherein said administration comprises an escalating series of doses of the MTP inhibitor. In some embodiments the method comprises administering at least three step-wise, increasing dosages of the MTP inhibitor to the subject. In some embodiments, the method further comprises the administration of one or more other lipid modifying compounds.
    Type: Application
    Filed: November 8, 2013
    Publication date: October 9, 2014
    Applicant: The Trustees of the University of Pennsylvania
    Inventor: Daniel J. Rader
  • Publication number: 20140256730
    Abstract: Compounds represented by formulae I, II, III, and IV including pro-drugs for treprostinil and prostacyclin analogs. Uses include treatment of pulmonary hypertension (PH) or pulmonary arterial hypertension (PAH). The structures of the compounds can be adapted to the particular application for a suitable treatment dosage. Transdermal applications can be used.
    Type: Application
    Filed: January 13, 2014
    Publication date: September 11, 2014
    Applicant: Corsair Pharma, Inc.
    Inventors: Cyrus K. BECKER, Jürg R. PFISTER, Gwenaella RESCOURIO, Meenakshi S. VENKATRAMAN, Xiaoming ZHANG
  • Publication number: 20140255517
    Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing posttraumatic stress disorder comprising administering a pharmaceutical composition comprising effective amount of an angiotensin-converting enzyme inhibitor to a subject in need thereof. In certain embodiments, the angiotensin-converting enzyme inhibitor is administered in combination with an angiotensin receptor blocker.
    Type: Application
    Filed: March 5, 2014
    Publication date: September 11, 2014
    Applicant: EMORY UNIVERSITY
    Inventors: Kerry J. Ressler, Paul J. Marvar
  • Patent number: 8822692
    Abstract: The present invention relates to new diterpenoid derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, urinary incontinence, asthma, or Alzheimer's disease and/or to prevent obstructive vascular lesions consequently to arteriotomy and/or angioplasty, and to prevent organ damage in hypertensive patients.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: September 2, 2014
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite, S.p.A.
    Inventors: Alberto Cerri, Mauro Gobbini, Marco Torri, Patrizia Ferrari, Mara Ferrandi, Giuseppe Bianchi
  • Publication number: 20140213578
    Abstract: Tricyclic chemical modulators of FOXO transcription factor proteins are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 31, 2014
    Applicant: MT. SINAI SCHOOL OF MEDICINE
    Inventors: Michael Ohlmeyer, Goutham Narla, Neil Dhawan, David Kastrinsky
  • Patent number: 8772013
    Abstract: A composition comprising intact minicells that contain a drug molecule is useful for targeted drug delivery. One targeted drug delivery method employs bispecific ligands, comprising a first arm that carries specificity for a bacterially derived minicell surface structure and a second arm that carries specificity for a mammalian cell surface receptor, to target drug-loaded minicells to specific mammalian cells and to cause endocytosis of the minicells by the mammalian cells. Another drug delivery method exploits the natural ability of phagocytic mammalian cells to engulf minicells without the use of bispecific ligands.
    Type: Grant
    Filed: January 27, 2005
    Date of Patent: July 8, 2014
    Assignee: Engeneic Molecular Delivery Pty Ltd
    Inventors: Himanshu Brahmbhatt, Jennifer MacDiarmid
  • Publication number: 20140178374
    Abstract: The disclosure relates to BAX activators and therapeutic uses relates thereto. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.
    Type: Application
    Filed: August 17, 2012
    Publication date: June 26, 2014
    Applicants: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, EMORY UNIVERSITY
    Inventors: Xingming Deng, Jia Zhou, Chunyong Ding
  • Publication number: 20140148476
    Abstract: The disclosure relates to methods for treating hyperlipidemia in a mammal. The present disclosure also relates to methods for treating and/or controlling obesity in a mammal. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, AEGR-733 and implitapide) and a DGAT inhibitor (for example, JTT-553 or PF-04415060). Co-administration of the MTP inhibitor with the DGAT inhibitor produces a therapeutic benefit, for example, a reduction in the concentration of cholesterol and/or triglycerides in the blood stream, but with fewer or reduced side effects than when higher dosages of the MTP inhibitor are used during monotherapy to provide the same or similar therapeutic benefit.
    Type: Application
    Filed: June 6, 2013
    Publication date: May 29, 2014
    Inventor: William J. Sasiela
  • Publication number: 20140100249
    Abstract: This invention discloses a treatment for a patient receiving medication to treat an attention deficit disorder such as ADHD wherein the treatment results in a loss of appetite and impairment of the patient's attentiveness. The treatment combines a treatment for an attention deficit disorder with an appetite stimulant, wherein the appetite stimulant increases the caloric intake of a patient, which can increase the patient's attentiveness. The combination treatment can be given for an indefinite, including, without limitation, life-long, to allow a patient to maintain normal caloric intake during treatment for an attention deficit disorder.
    Type: Application
    Filed: October 4, 2013
    Publication date: April 10, 2014
    Inventors: Douglas Sears, Michael Reilly
  • Publication number: 20140100227
    Abstract: Disclosed herein are novel C17-alkanediyl and alkenediyl derivatives of oleanolic acid, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.
    Type: Application
    Filed: September 10, 2013
    Publication date: April 10, 2014
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventors: Christopher F. BENDER, Xin JIANG, Eric ANDERSON, Melean VISNICK
  • Patent number: 8618135
    Abstract: The present invention provides methods and compositions for treating hyperlipidemia and/or hypercholesterolemia comprising administering to the subject an effective amount of an MTP inhibitor to inhibit hyperlipidemia and/or hypercholesterolemia in said subject, wherein said administration comprises an escalating series of doses of the MTP inhibitor. In some embodiments the method comprises administering at least three step-wise, increasing dosages of the MTP inhibitor to the subject. In some embodiments, the method further comprises the administration of one or more other lipid modifying compounds.
    Type: Grant
    Filed: March 11, 2011
    Date of Patent: December 31, 2013
    Assignee: The Trustees of the University of Pennsylvania
    Inventor: Daniel J. Rader
  • Publication number: 20130310423
    Abstract: The present invention relates to new diterpenoid derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, urinary incontinence, asthma, or Alzheimer's disease and/or to prevent obstructive vascular lesions consequently to arteriotomy and/or angioplasty, and to prevent organ damage in hypertensive patients.
    Type: Application
    Filed: July 26, 2013
    Publication date: November 21, 2013
    Applicant: SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Mauro Gobbini, Marco Torri, Patrizia Ferrari, Mara Ferrandi, Giuseppe Bianchi
  • Patent number: 8586611
    Abstract: This invention is directed to compounds of Formula (1) including all geometric and stereoisomers, N oxides, and agriculturally suitable salts thereof, agricultural compositions containing them and their use as fungicides, (1) provided that the compound of Formula 1 is other than 2-[1-[(2-chlorophenyl)acetyl]-4-piperidinyl]-N-methyl-N-[(1R)-1-phenylethyl]-4-thiazolecarboxamide and R1 is other than 4-fluorophenyl; wherein R1, R2, A, G, Q, W1, W2, X and n are otherwise as defined in the disclosure, Also disclosed are compositions containing the a compound having a formula corresponding to Formula (1) where the provisos are both omitted; and methods for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound having a formula corresponding to Formula (1) where the provisos are both omitted.
    Type: Grant
    Filed: July 26, 2006
    Date of Patent: November 19, 2013
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: John Joseph Bisaha, Patrick Ryan Kovacs, Renee Marie Lett, Jeffrey Keith Long, Robert James Pasteris, Boris Abramovich Klyashchitsky, Bruce Lawrence Finkelstein, Brenton Todd Smith
  • Publication number: 20130274240
    Abstract: The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.
    Type: Application
    Filed: November 5, 2012
    Publication date: October 17, 2013
    Inventor: JAPAN TOBACCO INC.
  • Publication number: 20130244994
    Abstract: This invention relates to novel compounds of the Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Application
    Filed: February 15, 2013
    Publication date: September 19, 2013
    Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice
  • Patent number: 8530465
    Abstract: The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.
    Type: Grant
    Filed: August 1, 2012
    Date of Patent: September 10, 2013
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Chia-Chung Lee
  • Publication number: 20130231341
    Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Application
    Filed: January 11, 2013
    Publication date: September 5, 2013
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventor: Soren Ebdrup
  • Publication number: 20130203709
    Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.
    Type: Application
    Filed: August 9, 2011
    Publication date: August 8, 2013
    Applicants: THE PENN STATE RESEARCH FOUNDATION, UNIVERSITY OF SOUTH FLORIDA
    Inventors: Roman Manetsch, Sameer Kulkarni, Iredia D. Iyamu, Hong-Gang Wang, Kenichiro Doi, Wayne Guida, Daniel Santiago, Courtney du Boulay
  • Patent number: 8466200
    Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Grant
    Filed: February 7, 2012
    Date of Patent: June 18, 2013
    Assignee: Merck Patent GmbH
    Inventors: Denis Carniato, Christine Charon, Johannes Gleitz, Didier Roche, Bjoern Hock
  • Publication number: 20130137726
    Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
    Type: Application
    Filed: April 25, 2012
    Publication date: May 30, 2013
    Applicant: The Regents of the University of California
    Inventors: Bruce D. Hammock, Paul D. Jones, Christophe Morisseau, Huazhang Huang, Hsing-Ju Tsai, Richard Gless, JR.
  • Publication number: 20130102635
    Abstract: The invention is directed to methods for treating hyperlipidemia in a mammal. The methods involve combination therapies using a microsomal triglyceride transfer protein (MTP) inhibitor (for example, BMS-201038 and implitapide) and a HMG-CoA reductase inhibitor (for example simvastatin or atorvastatin). Co-administration of the MTP inhibitor with the HMG-CoA reductase inhibitor produces a therapeutic benefit, for example, a reduction in the concentration of cholesterol and/or triglycerides in the blood stream, but with fewer or reduced side effects than when higher dosages of the MTP inhibitor are used during monotherapy to provide the same or similar therapeutic benefit.
    Type: Application
    Filed: April 11, 2012
    Publication date: April 25, 2013
    Inventor: Gerald L. Wisler
  • Patent number: 8383820
    Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: February 26, 2013
    Assignee: High Point Pharmaceuticals, LLC
    Inventor: Soren Ebdrup
  • Publication number: 20130040953
    Abstract: The present invention provides compositions and methods that promote wound healing in a subject with a cutaneous injury. In particular, the present invention provides systemic and/or local administration of one or more compositions that cause ganglioside depletion (e.g., glucosylceramide synthase (GCS) inhibitors) for the treatment of cutaneous wounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: February 14, 2013
    Inventor: Amy S. Paller
  • Patent number: 8334305
    Abstract: Novel substituted amide inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: December 18, 2012
    Assignee: High Point Pharmaceuticals, LLC
    Inventor: Soren Ebdrup
  • Publication number: 20120302539
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Application
    Filed: May 7, 2012
    Publication date: November 29, 2012
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas Macdonald, John Wityak
  • Publication number: 20120289514
    Abstract: Pharmaceutical composition for treating alcohol dependence in humans comprising two active ingredients: a compound having an antagonistic action on the 5-HT2 serotoninergic receptors selected as being cyproheptadine; and a compound having an antagonistic action on the alpha1-noradrenergic receptors selected from prazosin, alfuzosin, terazosin and tamsulosin.
    Type: Application
    Filed: December 29, 2010
    Publication date: November 15, 2012
    Inventors: Philippe Bernard, Fabrice Trovero
  • Publication number: 20120289512
    Abstract: The present invention relates to inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
    Type: Application
    Filed: May 10, 2012
    Publication date: November 15, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Steven Fung, Peer B. Jacobson, Lynne E. Rueter, Marina I. Strakhova, Jiahong Wang, Jeffrey J. Rohde, Qi Shuai, James T. Link, Jyoti R. Patel, Jurgen Dinges, Bryan K. Sorensen, Hong Yong, Vince S. Yeh, Ravi Kurukulasuriya
  • Publication number: 20120282255
    Abstract: The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated.
    Type: Application
    Filed: April 6, 2012
    Publication date: November 8, 2012
    Inventor: Greg Plucinski
  • Patent number: 8278329
    Abstract: The invention relates to a compound represented by the following general formula (1) or its analogue, which selectively inhibit N-type calcium channels or its analogue, and to a method for treating pain etc. comprising the compound represented by the following general formula (1) or its analogue to a patient in need of such treatment: wherein, A represents CH?CH, etc., a, b, c and d represents CH etc., R1, R2, R3, R4, R5 and R6 represents H etc., V—W represents C?C, etc., n represents 0 to 3, Y1 represents O etc., B represents —(CH2)vCHR21 wherein v is 0 to 3, R21 represents H, a lower alkyl group or the like, etc., G represents —CO—, a covalent bond, etc., m is 0 to 6, R7 and R8 represents H, a lower alkyl group, —COR18a, —COOR20 wherein R18a and R20 each represents a lower alkyl group or the like, etc.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: October 2, 2012
    Assignee: Ajinomoto Co., Inc.
    Inventors: Takashi Yamamoto, Seiji Niwa, Kayo Otani, Seiji Ohno, Hajime Koganei, Satoshi Iwayama, Akira Takahara, Yukitsugu Ono, Tomoko Takeda, Shinichi Fujita, Keiko Moki
  • Patent number: 8278321
    Abstract: The present disclosure characterizes the activity of Golgicide A (GCA), as a potent, specific and reversible small molecule inhibitor of Golgi BFA resistance factor 1 (GBF1) function. A mutant GBF1 gene that is resistant to GCA is also described. Methods of using GCA and the GCA-resistant GBF1 gene are described including methods for modulating GBF1 activity for research and therapeutic purposes. Also described are compositions incorporating a GCA-resistant GBF1.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: October 2, 2012
    Assignee: Washington University
    Inventor: David B. Haslam
  • Publication number: 20120214796
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: April 27, 2012
    Publication date: August 23, 2012
    Inventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
  • Patent number: 8242103
    Abstract: Bridged bicyclic sulphamides of formula (I) are disclosed for treatment of cancer.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: August 14, 2012
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Huw David Lewis, Timothy Harrison, Mark Steven Shearman
  • Publication number: 20120172396
    Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Application
    Filed: February 7, 2012
    Publication date: July 5, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Denis CARNIATO, Christine CHARON, Johannes GLEITZ, Didier ROCHE, Bjoern HOCK
  • Patent number: 8188288
    Abstract: The present invention relates to 2-adamantylurea derivatives of formula I as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11?-HSD1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Grant
    Filed: November 22, 2006
    Date of Patent: May 29, 2012
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Denis Carniato, Christine Charon, Johannes Gleitz, Didier Roche, Bjoern Hock
  • Publication number: 20120129834
    Abstract: Methods are provided for the treatment and/or prophylaxis of Huntington's disease. In various embodiments the methods involve administration of one or more serotonin receptor antagonists. In certain embodiments the serotonin receptor antagonists include, but are not limited to loxapine, and/or a loxapine analogue, and/or cyproheptadine, and/or a cyproheptadine analogue (e.g., pizotifen).
    Type: Application
    Filed: September 16, 2011
    Publication date: May 24, 2012
    Applicant: BUCK INSTITUTE FOR RESEARCH ON AGING
    Inventors: ROBERT HUGHES, LISA ELLERBY
  • Publication number: 20120129889
    Abstract: Disclosed herein are non-competitive NMDA receptor antagonists having chemical structures similar to that of phencyclidine (PCP). These antagonists contain a polycyclic ring structure in place of the cycloalkyl ring of PCP. The antagonists also differ from PCP in that they include an electron withdrawing group, a hydroxyl group, or an amine group at the para position of the phenyl ring. The antagonists disclosed herein are useful for treating or ameliorating a symptom of ailments associated with over excitation of cells (e.g., neurons) that express NMDA receptors. Examples of ailments that can be treated and for which symptoms can be ameliorated include epilepsy, neurodegenerative disease (e.g., Alzheimer's and Parkinson's diseases), drug addiction, neuropathic pain, and neuronal and glutamate-dependent tumors.
    Type: Application
    Filed: January 31, 2012
    Publication date: May 24, 2012
    Inventor: Adeboye Adejare
  • Publication number: 20120122870
    Abstract: Ischemia-reperfusion injury remains a primary cause of morbidity and mortality in individuals who experience disruption of normal blood flow to one or more major organs. For example, there are no clinically proven strategies that prevent acute renal failure following cardiac surgery. The present invention provides a variety of methods for the treatment or prevention of ischemia-reperfusion injury. In one aspect of the invention, a method for treating or preventing ischemia-reperfusion injury includes administering to a subject an effective amount of a sphingosine kinase inhibitor. Sphingosine kinase inhibitors are very effective in the protection against IR-induced acute renal failure and liver failure. Moreover, the effects occur very early after administration, requiring only a very short time of treatment. Toxicology studies with sphingosine kinase inhibitors demonstrate that they have low toxicity, even in long-term treatment.
    Type: Application
    Filed: May 10, 2010
    Publication date: May 17, 2012
    Applicants: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT, APOGEE BIOTECHNOLOGY CORPORATION
    Inventors: Charles D. Smith, Zhi Zhong, Lynn W. Maines
  • Publication number: 20120108570
    Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.
    Type: Application
    Filed: January 6, 2012
    Publication date: May 3, 2012
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Miodrag Radulovacki, David W. Carley
  • Publication number: 20120095004
    Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.
    Type: Application
    Filed: October 19, 2011
    Publication date: April 19, 2012
    Applicant: APOGEE BIOTECHNOLOGY CORPORATION
    Inventors: Charles D. Smith, Kevin J. French, Yan Zhuang
  • Publication number: 20120065194
    Abstract: A method of treating exposure to an organophosphate compound by administering a cyproheptadine compound to a subject in need thereof.
    Type: Application
    Filed: September 14, 2011
    Publication date: March 15, 2012
    Inventors: David HELTON, David FICK
  • Publication number: 20120052118
    Abstract: The present invention provides an apparatus and process for making softgel capsules having incorporated therein other solid dosage forms selected from the group consisting of pellets, smaller capsules, smaller tablets, sustained release solid dosage forms, immediate release solid dosage forms, extended release solid dosage forms and zero order release solid dosage forms, said apparatus comprising: (a) two spreader boxes; (b) two casting drums; (c) a pair of rotary dies having means for suction; (d) a liquid fill system; (e) a wedge for heating gelatine ribbons and feeding said fill; and (f) two lateral dispensing devices said lateral dispensing devices including hoppers having said solid dosage forms, channelguides for transporting said solid dosage forms and a grasping claw for dispensing said solid dosage form into the softgel pocket formed in the rotary dies.
    Type: Application
    Filed: July 18, 2011
    Publication date: March 1, 2012
    Inventors: Carlos Salazar Altamar, Gustavo Anaya, Braulio Teran, Newman Aguas Navarro, Willmer Herrera
  • Patent number: RE43390
    Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.
    Type: Grant
    Filed: October 27, 1998
    Date of Patent: May 15, 2012
    Assignees: GlaxoSmithKline LLC, SmithKline Beecham Limited
    Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt