The Cyano Is Bonded Directly To A Benzene Ring Patents (Class 514/522)
  • Publication number: 20120029034
    Abstract: The present invention relates to calcium salts of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1, and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.
    Type: Application
    Filed: July 1, 2011
    Publication date: February 2, 2012
    Applicant: 4SC AG
    Inventors: Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT
  • 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
  • Patent number: 8080682
    Abstract: This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.
    Type: Grant
    Filed: August 24, 2007
    Date of Patent: December 20, 2011
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller
  • Publication number: 20110306621
    Abstract: An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on a serotonin 5-HT5A receptor modulating action. It was confirmed that acylguanidine derivatives, which has the characteristic structure in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent 5-HT5A receptor modulating action and excellent pharmacological action based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.
    Type: Application
    Filed: February 8, 2010
    Publication date: December 15, 2011
    Inventors: Isao Kinoyama, Takehiro Miyazaki, Yohei Koganemaru, Nobuyuki Shiraishi, Yuichiro Kawamoto, Takuya Washio
  • Publication number: 20110306539
    Abstract: A process for making particles for delivery of drug nanoparticles is disclosed herein. The process comprises the steps of (a) forming a suspension of drug nanoparticles by mixing a precipitant solution with an anti-solvent solution under micro-mixing environment, where the formed nanoparticles have a narrow particle size distribution; (b) providing an excipient to at least one of the precipitant solution, the anti-solvent solution and the suspension of drug nanoparticles, the excipient being selected to maintain said drug nanoparticles in a dispersed state when in liquid form; and (c) drying the suspension of drug nanoparticles containing the excipient therein to remove solvent therefrom, wherein removal of the solvent causes the excipient to solidify and thereby form micro-sized matrix particles, each micro-sized particle being comprised of drug nanoparticles dispersed in a solid matrix of the excipient.
    Type: Application
    Filed: September 24, 2009
    Publication date: December 15, 2011
    Inventors: Zhigang Shen, Jimmy Sung Lai Yun, Jun Hu, Arvind Jugade, Jiyao Zhang, Wenhao Chen, Zhe Wang, Lingyan Gao, Jian Feng Chen
  • Patent number: 8063103
    Abstract: The application discloses novel polymorphic crystalline forms of 2-[4-Bromo-3-(3-chloro-5-cyano-phenoxy)-2-fluoro-phenyl]-N-(2-chloro-4-propionylsulfamoyl-phenyl)-acetamide, sodium salt (Ib) with improved stability and physical properties which facilitate manufacturing, handling and formulating for treatment or prophylaxis of HIV mediated diseases, AIDS or ARC, in monotherapy or in combination therapy.
    Type: Grant
    Filed: September 9, 2009
    Date of Patent: November 22, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: James Prentice Davidson, Fei Pang, Margaret Wong, Michael Martin
  • Patent number: 8062666
    Abstract: The present invention relates to an extended release composition comprising as active compound Venlafaxine Hydrochloride, in which Venlafaxine Hydrochloride is coated on a non pareil inert core, which coated core is then coated with polymeric layer which enables the controlled release of the Venlafaxine Hydrochloride.
    Type: Grant
    Filed: November 7, 2002
    Date of Patent: November 22, 2011
    Assignee: Lycored Bio Ltd.
    Inventor: Yoram Sela
  • Publication number: 20110281898
    Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: July 26, 2011
    Publication date: November 17, 2011
    Inventors: Roger Victor Bonnert, Anil Patel, Stephen Thom
  • Publication number: 20110275635
    Abstract: Small molecule inhibitors of bacterial nicotinamide adenine dinucleotide synthetase (NADs), bacterial nicotinic acid mononucleotide adenylyltransferase (NaMNAT), and human nicotinamide mononucleotide adenylyltransferase (NMNAT) are provided, as well as methods of making and using the inhibitors.
    Type: Application
    Filed: January 8, 2010
    Publication date: November 10, 2011
    Applicant: THE UAB RESEARCH FOUNDATION
    Inventors: Wayne J. Brouillette, Christie G. Brouillette, Whitney B. Moro
  • Publication number: 20110275599
    Abstract: The invention describes the use of a methylated vegetable oil having less than 10 percent by weight of saturated fatty acid methyl esters and less than 10 percent by weight of fatty acid methyl esters of carbon chain length less than C10 as a low-cloud point coformulant in pesticidal compositions.
    Type: Application
    Filed: May 3, 2011
    Publication date: November 10, 2011
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Christopher J. Voglewede, Karen M. Swayze, Holger Tank
  • Publication number: 20110269761
    Abstract: The invention relates to substituted aryl-sulphonylglycine derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as in the specification and claims, which are suitable for preparing a pharmaceutical composition for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.
    Type: Application
    Filed: April 17, 2009
    Publication date: November 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Elke Langkopf, Frank Himmelsbach, Juergen Mack, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
  • Publication number: 20110263703
    Abstract: The present invention relates to solid forms of (S)-N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide and process for producing the same.
    Type: Application
    Filed: June 5, 2011
    Publication date: October 27, 2011
    Inventors: James T. Dalton, David A. Dickason, Seoung-Soo Hong, Thomas G. Bird, Tai Ahn
  • Publication number: 20110257265
    Abstract: The present invention provides the use of a UV absorber for reducing the E/Z isomerization of pesticides comprising a double bond. It furthermore relates to a composition comprising an E and/or a Z isomer of a pesticide comprising a double bond and a UV absorber.
    Type: Application
    Filed: April 13, 2011
    Publication date: October 20, 2011
    Inventors: Michael ISHAQUE, Vijay Narayanan Swaminathan, Sylke Haremza, Claude Taranta, William Baxter
  • Publication number: 20110251248
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: December 9, 2009
    Publication date: October 13, 2011
    Inventors: Songnian Lin, Xibin Liao, Roman Kats-Kagan, John E. Stelmach, Emma R. Parmee
  • Publication number: 20110237664
    Abstract: This invention provides use of a SARM compound or a composition comprising the same in treating and preventing muscle wasting in patients with non-small cell lung cancer (NSCLC); treating pre-cachexia or early cachexia (preventing muscle wasting in a cancer patient); treating and preventing loss of physical function due to cancer or cancer therapy; increase of physical function; and increasing survival in a patient with NSCLC.
    Type: Application
    Filed: April 8, 2011
    Publication date: September 29, 2011
    Inventors: James T. Dalton, Shontelle Dodson, Mitchell S. Steiner
  • Publication number: 20110236451
    Abstract: Subject of the present invention is a solid ant bait comprising an insecticide and a bait composition. Another subject is a process for the preparation of said ant bait, comprising extruding a mixture, which contains the insecticide and the bait composition. Yet another subject is a method for controlling ants, comprising offering to said ants the ant bait according to the invention. Finally, a subject is a use of the ant bait according to the invention for controlling ants.
    Type: Application
    Filed: November 16, 2009
    Publication date: September 29, 2011
    Applicant: BASF SE
    Inventors: Claude Taranta, Thomas Bork, Gerhard Schnabel, Helmut Müller, Sarah Thompson, Clark D. Klein, Nigel Armes, Tiffany Hennessey
  • Publication number: 20110237665
    Abstract: The present invention relates to an agrochemical composition comprising pesticide and UV absorber, and the abovementioned UV absorbers. The invention furthermore relates to the use of the UV absorbers in agrochemical compositions. It moreover relates to a method of controlling phytopathogenic fungi and/or undesirable plant growth and/or undesirable insect or mite infestation and/or of regulating plant growth.
    Type: Application
    Filed: November 30, 2009
    Publication date: September 29, 2011
    Applicant: BASF SE
    Inventors: Andrea Misske, Christian Bittner, Michael Ishaque, Markus Hoffmann, Richard Riggs, Sens Ruediger, Andre Kabat, Sylke Haremza, Douglas D. Anspaugh, David M. Terry
  • Publication number: 20110223214
    Abstract: Carboxymethylcellulose, notably sodium carboxymethylcellulose or other alkali metal or alkaline earth metal salts of carboxymethylcellulose, are employed to control solidification time of compositions comprising one or more bioresorbable ceramics, notably a hydratable calcium sulphate, in order to facilitate preparation of a ready-to-use composition for inserting into the body by injection.
    Type: Application
    Filed: November 27, 2009
    Publication date: September 15, 2011
    Applicant: LIDDS AB
    Inventors: Lars Åke Malmsten, Niklas Axén, Hans Lennernäs, Anders Carlsson
  • Patent number: 8008348
    Abstract: This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or an analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, impurity or crystal of said SARM compound, or any combination thereof.
    Type: Grant
    Filed: June 7, 2004
    Date of Patent: August 30, 2011
    Assignee: University of Tennessee Research Foundation
    Inventors: Mitchell S. Steiner, Karen A. Veverka, James T. Dalton, Duane D. Miller
  • Publication number: 20110207749
    Abstract: The present disclosure is generally directed to compounds that can inhibit DAGL? and/or ? activity, compositions comprising such compounds, and methods for inhibiting DAGL? and/or ? activity.
    Type: Application
    Filed: February 11, 2011
    Publication date: August 25, 2011
    Inventors: Louis S. Chupak, Xiaofan Zheng, Min Ding, Shuanghua Hu, Yazhong Huang, Robert G. Gentles
  • Publication number: 20110196007
    Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.
    Type: Application
    Filed: July 22, 2009
    Publication date: August 11, 2011
    Inventors: Tadashi Honda, Emilie David, Dale Mierke
  • Publication number: 20110190285
    Abstract: The present invention provides methods of treating a botulinum toxin related condition in a subject. In certain embodiments, the methods involve administering a compound of the following formulas: (I), (II), (III), (IV), (V).
    Type: Application
    Filed: August 26, 2009
    Publication date: August 4, 2011
    Applicant: ABSOLUTE SCIENCE, INC.
    Inventors: Alan Jacobson, Scott Moe
  • Publication number: 20110190231
    Abstract: The present invention relates to novel thioamide derivatives of formula (I) and formula (Ia): wherein, R3, R4, R5, R6, R7, P, Q, T, V, W, X, Y, Z, a, m and n are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.
    Type: Application
    Filed: April 13, 2011
    Publication date: August 4, 2011
    Inventors: Loic Patrick Le Hir de Fallois, Hyoung Ik Lee, Philip Reid Timmons
  • Patent number: 7989498
    Abstract: The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.
    Type: Grant
    Filed: September 25, 2003
    Date of Patent: August 2, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jeffrey O Saunders, Daniel Elbaum, Perry M Novak, Douglas Naegele, Randy S Bethiel, Steven M Ronkin, Michael C Badia, Catharine Frank, Dean P Stamos, William Walters, David Pearlman
  • Publication number: 20110184040
    Abstract: The present invention relates to a method for controlling arthropods comprising the application of an aqueous gel which contains an insecticide, an attractant and a thickener, wherein the aqueous gel is applied in the form of spots on fruit trees. The invention further relates to an aqueous gel comprising an insecticide, an attractant, a thickener, a humectant and a feeding stimulant. The invention also relates to a concentrated gel for preparing the aqueous gel.
    Type: Application
    Filed: January 21, 2011
    Publication date: July 28, 2011
    Applicant: BASF SE
    Inventors: Claude Taranta, Tatjana Levy, Ouidad Benlahmar, Marc Nolte, Thomas Kröhl, Christoph Randt, Thomas Bork, Wolfgang Meier, Clark D. Klein, Tiffany Hennessey
  • Publication number: 20110172302
    Abstract: The present invention includes methods for treating Meibomian gland dysfunctions. The invention also includes methods for improving tear lipid composition, for treating abnormal Meibomian gland secretion and for normalizing Meibomian gland secretions.
    Type: Application
    Filed: January 11, 2011
    Publication date: July 14, 2011
    Inventors: James T. Dalton, Jeetendra Eswaraka
  • Publication number: 20110166117
    Abstract: The invention relates to substituted phenoxyacetic acids (I) as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
    Type: Application
    Filed: December 30, 2010
    Publication date: July 7, 2011
    Inventors: Roger Bonnert, Stephen Brough, Andrew Davies, Timothy Luker, Thomas McInally, Ian Millichip, Garry Pairaudeau, Anil Patel, Rukhsana Rasul, Stephen Thom
  • Publication number: 20110105532
    Abstract: The present invention relates to halogen-substituted amide derivatives of the general formula (I) in which R1 to R6, Q1 to Q8, A, V, W, X, Y, n and m are each defined as described in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.
    Type: Application
    Filed: October 27, 2010
    Publication date: May 5, 2011
    Applicant: Bayer CropScience AG
    Inventors: Markus HEIL, Eike Kevin Heilmann, Alexander Sudau, Tobias Kapferer, Friedrich August Mühlthau, Peter Jeschke, Arnd Voerste, Ulrich Görgens, Klaus Raming, Ulrich Ebbinghaus-Kintscher, Mark Drewes, Martin Adamczewski, Angela Becker
  • Publication number: 20110105485
    Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
    Type: Application
    Filed: July 21, 2010
    Publication date: May 5, 2011
    Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
  • Publication number: 20110082109
    Abstract: The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+/H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.
    Type: Application
    Filed: October 1, 2010
    Publication date: April 7, 2011
    Applicant: AJINOMOTO CO., INC.
    Inventors: Wataru MIYANAGA, Yoichiro Shima, Misato Noguchi, Akiko Oonuki, Yayoi Kawato, Hiroshi Iwata, Eri Harada, Ryuta Takashita, Hirokazu Ueno, Tadakiyo Nakagawa
  • Publication number: 20110046124
    Abstract: The subject invention provides spray formulations, and methods of use, for controlling ant populations.
    Type: Application
    Filed: August 31, 2009
    Publication date: February 24, 2011
    Inventors: Rudolf H. Scheffran, Jack Richard Warner
  • Publication number: 20110046128
    Abstract: A series of novel compounds showing anticonvulsant, chemical countermeasure(s), and analgesic activities is described. Such pharmaceutically active compounds may also show utility in the treatment of other central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, Parkinson's disease, spasticity, Alzheimer's disease, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), chronic neurodegenerative diseases (such as Alzheimer's disease and Huntington's disease), and/or traumatic brain and/or spinal cord injuries. Moreover, these/such compounds may also be useful in the treatment of status epilepticus and/or as chemical countermeasures.
    Type: Application
    Filed: September 13, 2010
    Publication date: February 24, 2011
    Applicant: AURIMMED PHARMA, INC.
    Inventors: Amir Pesyan, Manuel F. Balandrin
  • Publication number: 20110039851
    Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.
    Type: Application
    Filed: October 14, 2008
    Publication date: February 17, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Kaka Dey, Donghong Amy Gao, Daniel R. Goldberg, Alexander Heim-Riether, John Edward Mangette, Ingo Andreas Mugge, Roger John Snow, Alan David Swinamer, Jiang-Ping Wu, Zhaoming Xiong, Yu Yang
  • Publication number: 20110014127
    Abstract: Described herein are methods for effectively and accurately measuring a patient response upon administration of one or more drugs to the patient. The methods are more sensitive than current methodologies. Also described herein are compositions comprising an analgesic and a sufficient amount of an antihistamine to enhance the analgesic properties of the analgesic. With respect to these compositions, the methods described herein are useful for evaluating qualities of pain, definite improvement, and one or more bodily functions of a subject afflicted with pain. The compositions described herein are useful in improving the quality of pain in a subject or a bodily function of a subject afflicted with pain or definite improvement of a subject afflicted with pain.
    Type: Application
    Filed: January 5, 2009
    Publication date: January 20, 2011
    Inventor: Bernard P. Schachtel
  • Publication number: 20110009457
    Abstract: The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases transmitted through parasites, its use for the preparation of a veterinary pharmaceutical for controlling animal parasites, and a method for preventing infection with diseases transmitted through parasites.
    Type: Application
    Filed: December 9, 2008
    Publication date: January 13, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Ulrich Görgens, Katsuaki Wada, Yukiyoshi Watanabe, Jun Mihara, Koichi Araki
  • Patent number: 7863327
    Abstract: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.
    Type: Grant
    Filed: May 3, 2005
    Date of Patent: January 4, 2011
    Assignee: Trustees of Dartmouth College
    Inventors: Gordon W. Gribble, Tadashi Honda, Michael B. Sporn, Nanjoo Suh
  • Patent number: 7855229
    Abstract: This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or an analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, impurity or crystal of said SARM compound, or any combination thereof.
    Type: Grant
    Filed: September 7, 2005
    Date of Patent: December 21, 2010
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka
  • Publication number: 20100305131
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: May 27, 2010
    Publication date: December 2, 2010
    Inventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
  • Publication number: 20100286106
    Abstract: Treating and/or preventing prostate problems and/or metastases, by selectively occluding various groin vessels and tools for selective occluding of various groin veins, including, for example, the deferential vein. Optionally providing anti-androgen treatment after such occluding.
    Type: Application
    Filed: July 13, 2008
    Publication date: November 11, 2010
    Inventors: Yigal Gat, Menachem Goren
  • Publication number: 20100280107
    Abstract: This invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of benign prostate hyperplasia in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of treating a subject suffering from hair loss, comprising the step of administering to the subject a therapeutically effective amount of a 5-? reductase enzyme type 1 and/or type 2 inhibitor, wherein said inhibitor is a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein.
    Type: Application
    Filed: June 30, 2010
    Publication date: November 4, 2010
    Inventors: James T. DALTON, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka, Wenqing Gao
  • Publication number: 20100267702
    Abstract: Disclosed are bisbenzamidine and bisbenzamidoxime compounds useful for treatment of trypanosomiasis. The compounds disclosed are useful for treating mammals infected with parasitic hemoflagellates, in particular Trypanosoma brucei gambiense and Trypanosoma brucei rhodesiense.
    Type: Application
    Filed: July 2, 2010
    Publication date: October 21, 2010
    Inventors: Tien L. HUANG, Jean Jacques VANDEN EYNDE, Annie MAYENCE, Cyrus BACCHI, Isaac O. DONKOR, Nageswara R. KODE
  • Publication number: 20100267676
    Abstract: Gamma-amino-butyric acid derivatives that are GABAB receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed.
    Type: Application
    Filed: April 16, 2010
    Publication date: October 21, 2010
    Inventors: Feng Xu, Mark A. Gallop, Ge Peng, Thu Phan, Usha Dilip, David J. Wustrow
  • Patent number: 7807713
    Abstract: Disclosed herein are novel antagonists of the androgen receptor and androgen receptor mutations associated with clinical failure of currently prescribed anti-androgens and use of said antagonists in the treatment of conditions associated with inappropriate activation of the androgen receptor.
    Type: Grant
    Filed: May 15, 2009
    Date of Patent: October 5, 2010
    Assignee: University of Delaware
    Inventors: John Tze-tzun Koh, Paula Lynn McGinley, Hongmu Pan
  • Publication number: 20100249124
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1c, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Application
    Filed: March 19, 2010
    Publication date: September 30, 2010
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Publication number: 20100249228
    Abstract: This invention is directed to a feed composition and method of affecting the carcass composition by increasing the lean mass, reducing the fat mass, and/or reducing the percent fat mass comprising SARM compounds.
    Type: Application
    Filed: March 23, 2010
    Publication date: September 30, 2010
    Inventors: James T. Dalton, Duane D. Miller, Jeffrey D. Kearbey
  • Patent number: 7803970
    Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.
    Type: Grant
    Filed: June 7, 2004
    Date of Patent: September 28, 2010
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka, Dong Jin Hwang, Jiyun Chen
  • Patent number: 7772433
    Abstract: This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, muscle wasting diseases and/or disorders, bone-related diseases and/or disorders, diabetes, cardiovascular disease, renal disease and others.
    Type: Grant
    Filed: April 16, 2007
    Date of Patent: August 10, 2010
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller
  • Patent number: 7763267
    Abstract: High load concentrate compositions comprising metaflumizone, an optional bridging agent, a surfactant, and a suitable carrier solvent. These compositions may be topically administered to animals, and are useful for preventing or treating ectoparasitic infestations in warm-blooded animals for prolonged periods of time. Additionally, they may be further diluted to provide other types of formulations useable for both topical and oral administration.
    Type: Grant
    Filed: May 17, 2006
    Date of Patent: July 27, 2010
    Assignee: Wyeth LLC
    Inventors: Robert B. Albright, Shobhan Sabnis
  • Patent number: 7754919
    Abstract: The present invention provides for compounds useful for treating an HIV-1 infection, or preventing an HIV-1 infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5 and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
    Type: Grant
    Filed: October 18, 2006
    Date of Patent: July 13, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Tania Silva, Zachary Kevin Sweeney
  • Publication number: 20100173955
    Abstract: Compounds of Formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.
    Type: Application
    Filed: August 21, 2007
    Publication date: July 8, 2010
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: George Doherty, Adam Cook