Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/393)
  • Patent number: 8426457
    Abstract: Methods of improving skin quality are disclosed. Generally, the methods include topically administering an IRM compound to a treatment area of skin for a period of time and in an amount effective for improving the quality of the skin. Suitable IRM compound compounds include agonists of one or more TLRs.
    Type: Grant
    Filed: March 12, 2004
    Date of Patent: April 23, 2013
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Richard L. Miller, James H. Lee, Mary L. Owens
  • Publication number: 20130096169
    Abstract: This invention relates to compositions and methods utilizing a chemotherapeutic drug and 6-bromoindirubin3?-oxime (BIO) for the treatment of cancer, including glioblastoma multiforme. The present invention demonstrates that BIO works synergistically with chemotherapeutic drugs to increase the cytotoxic effects of these drugs in glioma cells.
    Type: Application
    Filed: December 7, 2012
    Publication date: April 18, 2013
    Applicant: CEDARS-SINAI MEDICAL CENTER
    Inventor: CEDARS-SINAI MEDICAL CENTER
  • Publication number: 20130096162
    Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 3, 2012
    Publication date: April 18, 2013
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Publication number: 20130090364
    Abstract: Compounds represented by formula I or pharmaceutically acceptable salts thereof, wherein A, B, B?, X, Y, R1, R2, R2?, R3, R3?, R4, R4?, R5, R5?m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Application
    Filed: September 24, 2012
    Publication date: April 11, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventor: Vertex Pharmaceuticals Incorporated
  • Patent number: 8415483
    Abstract: The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: April 9, 2013
    Assignee: AstraZeneca AB
    Inventors: Gabor Csjernyik, Sofia Karlström, Annika Kers, Karin Kolmodin, Martin Nylöf, Liselotte Öhberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Söderman, Britt-Marie Swahn, Stefan Von Berg
  • Publication number: 20130084334
    Abstract: The invention relates to novel pharmaceutical compositions highly dosed with biotin, as well as to the use thereof in treating visual impairments which are related, in particular, to optic atrophy.
    Type: Application
    Filed: April 5, 2011
    Publication date: April 4, 2013
    Applicant: Assistance Publique - Hopitaux de Paris
    Inventors: Frédéric Sedel, Agnès Bellanger
  • Patent number: 8409574
    Abstract: Provided herein are compounds and methods for the treatment of brain cancer in a mammal, wherein the method comprises the administration to the mammal a compound that stabilizes tubulin dimers or microtubles at G2-M interface during mitosis but is not a substrate for MDR protein. In particular, the present application relates to the use of an orally effective abeo-taxane, alone or in combination with temozolomide or bevacizumab, for the treatment of brain cancer.
    Type: Grant
    Filed: August 20, 2010
    Date of Patent: April 2, 2013
    Inventors: James D. McChesney, Gilles Tapolsky, David E. Emerson, John Marshall, Tauseef Ahmed, Allen Cohn, Michael Kurman, Manuel Modiano
  • Patent number: 8399444
    Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, processes for their preparation, pharmaceutical compositions containing these compounds, and their use in the treatment of allergic disorders, such as allergic rhinitis and asthma.
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: March 19, 2013
    Assignee: GlaxoSmithKline Intellectual Property Development Ltd.
    Inventors: Ian Baxter Campbell, Simon Peace, John Martin Pritchard, Daniel Tape, Robert Charles Wheeler
  • Publication number: 20130065893
    Abstract: The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, R5, R7 and p are defined herein. The invention also relates to 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: November 29, 2010
    Publication date: March 14, 2013
    Applicant: NOVARTIS AG
    Inventors: Robert Sun, Lauren G. Monovich, Sylvie Chamoin, John Westbrook
  • Patent number: 8394968
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: March 12, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventor: Jeffrey Lee Romine
  • Publication number: 20130059018
    Abstract: This invention relates to the use of phytocannabinoids, either in an isolated form or in the form of a botanical drug substance (BDS) in the treatment of cancer. Preferably the cancer to be treated is cancer of the prostate, cancer of the breast or cancer of the colon.
    Type: Application
    Filed: March 11, 2011
    Publication date: March 7, 2013
    Applicants: OTSUKA PHARMACEUTICAL CO., LIMITED, GW PHARMA LIMITED
    Inventors: Daniela Parolaro, Paola Massi, Angelo Antonio Izzo, Francesca Borelli, Gabriella Aviello, Vincenzo Di Marzo, Luciano De Petrocellis, Aniello Schiano Moriello, Alessia Ligresti, Ruth Alexandra Ross, Lesley Ann Ford, Sharon Anavi-Goffer, Manuel Guzman, Guillermo Velasco, Mar Lorente, Sofia Torres, Tetsuro Kikuchi, Geoffrey Guy, Colin Stott, Stephen Wright, Alan Sutton, David Potter, Etienne De Meijer
  • Patent number: 8389558
    Abstract: The present invention is directed to pharmaceutical compositions comprising bendamustine and one or more amphiphilic anionic compounds and self assembled aggregates, which aggregates exhibit enhanced stability in aqueous solutions, including plasma, are disclosed. The unexpectedly enhanced stability afforded by such aggregates permits patients to be treated with bendamustine in lower and/or with less frequent dosages or to improve its therapeutic effect while using the same as presently used treatment protocol.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: March 5, 2013
    Assignee: Supratek Pharma Inc.
    Inventors: Valery Alakhov, Grzegroz Pietrzynski, Patel Kishore, Thomasz Popek
  • Patent number: 8389554
    Abstract: Novel imidazo[2,1-b][1,3,4]thiadiazole derivatives of formula (I) wherein R1 and R2 have the meaning according to claim 1, are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: March 5, 2013
    Assignee: Merck Patent Gesellschaft mit Beschränkter Haftung
    Inventors: Guenter Hoelzemann, Hartmut Greiner, Emilie Rossignol, Dominique Swinnen
  • Patent number: 8383663
    Abstract: The present invention is directed to pharmaceutical compositions including: (a) bendamustine, (b) a first charged cyclopolysaccharide, and (c) a stabilizing agent which is a second charged cyclopolysaccharide having a charge opposite to that of the first charged cyclopolysaccharide. The composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. The compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.
    Type: Grant
    Filed: February 22, 2011
    Date of Patent: February 26, 2013
    Assignee: Supratek Pharma Inc.
    Inventors: Valery Alakhov, Grzegorz Pietrzynski, Patel Kishore, Thomasz Popek
  • Publication number: 20130045957
    Abstract: Provided herein are methods for preventing and/or reducing the severity of drug induced ototoxicity. Provided herein are methods for recovery from hearing loss due to drug-induced ototoxicity.
    Type: Application
    Filed: February 16, 2012
    Publication date: February 21, 2013
    Applicant: Otonomy, Inc.
    Inventors: Fabrice Piu, Qiang Ye, Luis Dellamary, Carl Lebel
  • Patent number: 8377945
    Abstract: This disclosure concerns compounds which are useful as inhibitors of spleen tyrosine kinase (Syk) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of Syk. This disclosure also relates to pharmaceutical compositions containing these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: February 19, 2013
    Assignee: Rigel Pharmaceuticals Inc.
    Inventors: Jing Zhang, Rajinder Singh, Dane Goff, Taisei Kinoshita
  • Publication number: 20130030237
    Abstract: Provided herein are pharmaceutical compositions and methods of treating cancer wherein the cytotoxic activity of an anticancer agent is potentiated by the combination of base excision repair (BER) pathway inhibitors.
    Type: Application
    Filed: April 15, 2011
    Publication date: January 31, 2013
    Inventor: Charles Theuer
  • Publication number: 20130029964
    Abstract: An object of the present invention is to provide a novel low molecular weight compound exhibiting an osteogenesis-promoting action. This object is achieved by a compound having the general formula (I) or a pharmacologically acceptable salt thereof. In the general formula (I), R1 and R2 represent hydrogen atoms, and the like; R3 represents a hydrogen atom, and the like; X, Y, and Z represent nitrogen atoms, and the like; A represents a phenylene group, and the like; n represents 1 or 2, and the like; and V and W represent oxygen atoms, and the like.
    Type: Application
    Filed: August 27, 2012
    Publication date: January 31, 2013
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Kazumasa Aoki, Satoshi Matsui, Kenji Yoshikawa, Hiroki Shimizu, Junko Sasaki, Katsuyoshi Nakajima, Osamu Kanno, Kiyoshi Oizumi
  • Publication number: 20130028989
    Abstract: Targeting uncontrolled cell proliferation and resistance to DNA damaging chemotherapeutics with at least one reagent has significant potential in cancer treatment. Replication Protein A, the eukaryotic single-strand (ss) DNA binding protein, is essential for genomic maintenance and stability via roles in both DNA replication and repair. Reported herein are small molecules that inhibits the in vitro, in vivo, and cellular ssDNA binding activity of RPA, thereby disrupting the eukaryotic cell cycle, inducing cytotoxicity and increasing the efficacy of chemotherapeutic agents damage DNA, and/or disrupt its replication and/or function. These results provide new insights into the mechanism of RPA-ssDNA interactions in chromosome maintenance and stability. This represents a molecularly targeted eukaryotic DNA binding inhibitor and demonstrates the utility of targeting a protein-DNA interaction as a means of studying the cell cycle and providing a therapeutic strategy for cancer treatment.
    Type: Application
    Filed: February 5, 2011
    Publication date: January 31, 2013
    Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: John J. Turchi, Sarah Shuck
  • Publication number: 20130023574
    Abstract: Provided are a method for generating a data set for integrated proteomics analysis, whereby expression level variations of both of proteins and genes can be integrally united together and, moreover, highly accurate and appropriate analysis results can be obtained compared with the existing cases where the expression variation amount of proteins or genes is singly analyzed, an integrated proteomics analysis method, a method for identifying a protein causative of a disease or the like using these methods, and a method of using the same???.
    Type: Application
    Filed: March 31, 2011
    Publication date: January 24, 2013
    Applicant: National University Corporation Kumamoto University
    Inventors: Norie Araki, Souhei Mizuguchi, Daiki Kobayashi, Nobuyuki Tsubota, Takashi Morikawa, Junichi Kuratsu, Masayo Wilson Morifuji
  • Patent number: 8354434
    Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: January 15, 2007
    Date of Patent: January 15, 2013
    Assignee: Purdue Pharma L.P.
    Inventor: Xiaoming Zhou
  • Publication number: 20130011483
    Abstract: Formulations of mazindol having superior stability and methods of administering same are provided. The formulations may be immediate, enhanced, or otherwise delayed release formulations of mazindol.
    Type: Application
    Filed: March 30, 2011
    Publication date: January 10, 2013
    Inventors: Argaw Kidane, Padmanabh P. Bhatt
  • Publication number: 20130004481
    Abstract: The invention describes anti-cancer therapies comprising using dual Aurora kinase/MEK inhibitors as described herein.
    Type: Application
    Filed: January 5, 2012
    Publication date: January 3, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Flavio Solca, Ulrich Guertler, Michael Sanderson, Ulrike Tontsch-Grunt, Irene Waizenegger
  • Publication number: 20120316150
    Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1, R2, R3, R4, R5 and R6 are as defined herein: and compositions, processes for the preparation, and uses thereof, e.g. in the treatment of endometriosis or uterine fibroids.
    Type: Application
    Filed: June 18, 2012
    Publication date: December 13, 2012
    Inventors: KARL RICHARD GIBSON, Martin Peter Green, Toby James Underwood, Florian Wakenhut
  • Publication number: 20120308668
    Abstract: The present invention relates to the field of human health, and more particularly to the treatment of attention deficit/hyperactivity disorder (ADHD) with mazindol. The latter can be administered as monotherapy or in combination with one or more compounds, including psychostimulants, for the indication of ADHD and associated or co-morbid symptoms.
    Type: Application
    Filed: August 21, 2012
    Publication date: December 6, 2012
    Applicant: ASSISTANCE PUBLIQUE-HOPITAUX DE PARIS
    Inventor: Eric Konofal
  • Publication number: 20120302615
    Abstract: The invention comprises a method of treatment of CNS disorders by a pharmaceutical agent exhibiting combined noradrenergic, serotonergic or dopaminergic reuptake transporter inhibitory and ?-opioid agonistic activity.
    Type: Application
    Filed: December 2, 2010
    Publication date: November 29, 2012
    Inventor: Christopher D. Breder
  • Patent number: 8318728
    Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: November 27, 2012
    Assignee: Hydra Biosciences, Inc.
    Inventor: Jayhong A. Chong
  • Publication number: 20120295888
    Abstract: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4)alkyl, or —(C1-C4)alkyl-(C5-C7)aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4)alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10)aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: January 13, 2011
    Publication date: November 22, 2012
    Inventors: Qi-Ying Hu, Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Christoph Schumacher
  • Patent number: 8314097
    Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.
    Type: Grant
    Filed: August 23, 2006
    Date of Patent: November 20, 2012
    Assignee: Novartis AG
    Inventors: Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
  • Patent number: 8314134
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: November 20, 2012
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Jun Jiang, Hao Li, David James, Dinesh Chimmanamada, Christopher Borella, Lijun Sun, Yu Xie, Mats Holmqvist, Jerome Mahiou, Zhiqiang Xia
  • Publication number: 20120283304
    Abstract: The present invention relates to a parenteral formulation of Temozolomide comprising an excipient selected from the group consisting of bulking agents, buffers, pH adjusting agents, with the proviso that the formulation is free of dissolution enhancing agents.
    Type: Application
    Filed: December 22, 2010
    Publication date: November 8, 2012
    Applicant: SAHAJ LIFE SCIENCES PVT. LTD.
    Inventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty
  • Publication number: 20120282179
    Abstract: Methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments are described, wherein R1 is halo; R2 is halo; and Q is CH or N.
    Type: Application
    Filed: August 6, 2010
    Publication date: November 8, 2012
    Applicant: Exelixis, Inc.
    Inventors: Dana T. Aftab, Thomas Mueller, Aaron Weitzman, Jaymes Holland
  • Patent number: 8304409
    Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.
    Type: Grant
    Filed: December 11, 2009
    Date of Patent: November 6, 2012
    Assignee: Nicox S.A.
    Inventors: Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
  • Publication number: 20120277217
    Abstract: Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
    Type: Application
    Filed: October 27, 2010
    Publication date: November 1, 2012
    Applicant: NewLink Genetics Corporation
    Inventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Xiaoxia Zhang
  • Publication number: 20120277240
    Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Application
    Filed: February 17, 2011
    Publication date: November 1, 2012
    Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
  • Publication number: 20120277215
    Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.
    Type: Application
    Filed: July 2, 2012
    Publication date: November 1, 2012
    Inventors: Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
  • Patent number: 8299079
    Abstract: This application relates to the use of one or more parasympathomimetic drugs in combination with one or more alpha agonists to create optically beneficial miosis to, for example, temporarily treat presbyopia. The invention provides a pharmaceutical preparation comprising a therapeutically effective amount of one or more parasympathomimetic drugs or cholinesterase inhibitors, or a pharmaceutically acceptable salt thereof, in combination with one or more alpha agonists or antagonists, or a pharmaceutically acceptable salt thereof. The invention further provides for a method for treating, ameliorating or reducing presbyopia of a patient having an eye, comprising administering to said eye a pharmaceutically effective amount of the ophthalmic preparation.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: October 30, 2012
    Inventor: Herbert E. Kaufman
  • Patent number: 8299109
    Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available ALDARA 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for ALDARA 5% imiquimod cream to treat actinic keratosis are also disclosed and described.
    Type: Grant
    Filed: July 13, 2011
    Date of Patent: October 30, 2012
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Michael T. Nordsiek, Sharon F. Levy, James H. Lee, James H. Kulp, Kodumudi S. Balaji, Tze-Chiang Meng, Jason J. Wu, Valyn S. Bahm, Robert Babilon
  • Publication number: 20120270899
    Abstract: The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a cardiovascular disease in an individual using such pharmaceutical compositions.
    Type: Application
    Filed: February 3, 2012
    Publication date: October 25, 2012
    Inventors: Robin Mark Bannister, John Brew, Suzanne Jane Dilly, Gregory Alan Stoloff, Wilson Caparros-Wanderley
  • Patent number: 8293779
    Abstract: The present invention relates to the field of human health, and more particularly to the treatment of attention deficit/hyperactivity disorder (ADHD) with mazindol. The latter can be administered as monotherapy or in combination with one or more compounds, including psychostimulants, for the indication of ADHD and associated or co-morbid symptoms.
    Type: Grant
    Filed: April 11, 2007
    Date of Patent: October 23, 2012
    Assignee: Assistance Publique-Hopitaux de Paris
    Inventor: Eric Konofal
  • Publication number: 20120264752
    Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: June 22, 2012
    Publication date: October 18, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Patent number: 8288424
    Abstract: Substituted tetrahydroimidazopyridine compounds corresponding to formula I: in which R1, R2 and R3 have defined meanings, processes for preparing such compounds, pharmaceutical compositions containing such compounds, and the use of such compounds for treating or inhibiting pain, epilepsy, migraine, anxiety or urinary incontinence.
    Type: Grant
    Filed: January 21, 2009
    Date of Patent: October 16, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Beatrix Merla, Stefan Oberboersch, Sven Kuehnert, Gregor Bahrenberg, Achim Kless
  • Publication number: 20120258181
    Abstract: The present invention relates to combinations between artemisinin-based potent anti-malarial agents, selected from the group consisting of ART, DHA and ARM, and a further chemotherapeutic drug selected from the group consisting of a camptothecin derivative, or a PARP-1 inhibitor, or an intercalating DNA agent, or an alkylating agent. Such combinations, showed medium to strong synergism in various models of cancer, in particular in NSCL.
    Type: Application
    Filed: December 6, 2010
    Publication date: October 11, 2012
    Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.
    Inventors: Claudio Pisano, Loredana Vesci
  • Publication number: 20120258992
    Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: June 19, 2012
    Publication date: October 11, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
  • Publication number: 20120252856
    Abstract: The present invention relates to methods of dividing cancer into subgroups based upon Akt pathway gene expression. In one embodiment, the present invention provides a method of diagnosing glioblastoma multiforme (GBM) subtype in an individual by determining the presence of an abnormal expression of an Akt pathway gene cluster and diagnosing the cancer subtype in the individual.
    Type: Application
    Filed: December 10, 2010
    Publication date: October 4, 2012
    Applicant: Dignity Health
    Inventors: Anna Joy, Burt G. Feuerstein, Ivan Smimov
  • Publication number: 20120245126
    Abstract: Nitromethylene analogues of imidacloprid and divalent and oxabridged heterocyclic neonicotinoid compounds constructed by dialdehydes, preparation methods and uses thereof are disclosed. Compounds represented by formula (A) or (B), their optical isomers or agrochemically acceptable salts are provided. Agrochemical compositions comprising the said compounds, their optical isomers or agrochemically acceptable salts, the uses of the said agrochemical compositions and the preparation methods of the said compounds, their optical isomers or agrochemically acceptable salts are also disclosed. The compounds and their derivatives have high insecticidal activities to several farming and forestry pests including homoptera and lepidoptera pests, such as aphis, fulgorid, whitefly, leafhopper, common thrips, cotton bollworm, cabbage caterpillar, cabbage moth, cotton leafworm and armyworm.
    Type: Application
    Filed: December 9, 2010
    Publication date: September 27, 2012
    Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Xuhong Qian, Zhong Li, Xusheng Shao, Xiaoyong Xu, Zhiping Xu, Gonghua Song
  • Publication number: 20120237502
    Abstract: The present invention relates to a method for the prevention or treatment of certain breast cancers or ovarian cancer comprising administering to a patient in need thereof of a therapeutically effective amount of a 17,20-lyase inhibitor, wherein the breast cancer or ovarian cancer is estrogen receptor (ER) negative.
    Type: Application
    Filed: November 18, 2011
    Publication date: September 20, 2012
    Applicant: Takeda Pharmaceutical Company Limited
    Inventor: James W. Darnowski
  • Publication number: 20120230989
    Abstract: This document provides methods and materials related to treating renal cell carcinoma. For example, methods and materials for assessing a cancer patient (e.g., a renal cell carcinoma patient) for tumor or peritumoral tissue containing CD14+ cells and proceeding with a cancer treatment option (e.g., a renal cell carcinoma treatment option) based on the presence, absence, or level of CD14+ cells present within the tumor or peritumoral tissue are provided.
    Type: Application
    Filed: November 8, 2010
    Publication date: September 13, 2012
    Applicant: MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCH
    Inventor: Allan B. Dietz
  • Patent number: 8263615
    Abstract: Heterocyclic compounds of the general formula (I) are provided in which R, R1, R2, R3, R4 and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldostereone synthase inhibitors,
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: September 11, 2012
    Assignee: Novartis AG
    Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Michael Quirmbach, Christiane Marti, Aleksandar Stojanovic, Stefan Stutz
  • Publication number: 20120220640
    Abstract: The present invention relates to computer-implemented methods and system for analysing a biomarker which cycles in a subject. In some other aspects, the present invention relates to analysing a biomarker which at least initially increases or decreases in amount in a subject following a treatment for a disease. In further aspects, the present invention relates to computer-implemented methods and systems for determining a preferred time to administer a therapy to treat a disease in a subject. The present invention also relates to computer program product to implement the methods. Further, the present invention relates to methods of determining the timing of treating a disease in a subject in which the immune system is cycling.
    Type: Application
    Filed: May 27, 2010
    Publication date: August 30, 2012
    Applicant: IMMUNAID PTY LTD
    Inventors: Martin Leonard Ashdown, Andrew Robinson