Benzene Ring Bonded Directly To The Diazole Ring By Nonionic Bonding Patents (Class 514/391)
  • Patent number: 11091444
    Abstract: In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition.
    Type: Grant
    Filed: January 10, 2020
    Date of Patent: August 17, 2021
    Assignee: BUCK INSTITUTE FOR RESEARCH ON AGING
    Inventors: Varghese John, Dale E. Bredesen
  • Patent number: 9895355
    Abstract: Methods for treating androgen receptor-mediated diseases, such as breast cancer, with imidazoline derivatives of formula (I) are provided:
    Type: Grant
    Filed: January 20, 2017
    Date of Patent: February 20, 2018
    Assignees: Shanghai Hengru Pharmaceutical Co., Ltd., Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Hejun Lu, Piaoyang Sun, Hongbo Fei, Hongjian Jiang, Haowei Wang, Qing Dong
  • Publication number: 20150140127
    Abstract: Provided is a method for detecting injury to the brain comprising: a) determining the level of a tight junction (TJ) protein in exosomes isolated from a test sample from a subject, wherein the TJ protein is occludin, claudin-3, claudin-5, claudin-12, ZO-1, ZO-2, ZO-3, JAM-A, JAM-B or JAM-C, or any combination thereof; b) comparing the level of the TJ protein in the test sample to the level of the TJ protein in a control sample, wherein an elevated level of the TJ protein in the test sample relative to the level of the TJ protein in the control sample indicates that the subject has an injury to the brain.
    Type: Application
    Filed: June 25, 2013
    Publication date: May 21, 2015
    Applicant: TEMPLE UNIVERSITY-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
    Inventors: Servio H. Ramirez, Slava Rom, Yuri Persidsky
  • Publication number: 20150125389
    Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R4, R5, X1, X2, X3 and X4 are as defined herein, and wherein the compound comprises at least one F, Cl, Br, I or 123I moiety, are provided. Uses of such compounds for imaging diagnostics in cancer and therapeutics methods for treatment of subjects in need thereof, including prostate cancer as well as methods and intermediates for preparing such compounds are also provided.
    Type: Application
    Filed: September 9, 2014
    Publication date: May 7, 2015
    Applicants: THE UNIVERSITY OF BRITISH COLUMBIA, BRITISH COLUMBIA CANCER AGENCY BRANCH
    Inventors: Raymond John Andersen, Carmen Adriana Banuelos, Javier GARCIA FERNANDEZ, Yusuke IMAMURA, Jian KUNZHONG, Nasrin R. MAWJI, Marianne Dorothy Sadar, Jun Wang, Amy (Hsing Chen) Tien
  • Publication number: 20150119435
    Abstract: The present invention includes compounds that act as degraders of a target protein, wherein degradation is independent of the class of the target protein or its localization. In certain embodiments, the invention comprises a compound comprising a protein degradation moiety covalently bound to a linker, wherein the ClogP of the compound is equal to or higher than 1.5. In other embodiments, the target protein contemplated within the invention comprises a posttranslational modified protein or intracellular protein. In yet other embodiments, compounds of the present invention are used to treat disease states wherein protein degradation is a viable therapeutic approach, such as cancer or any sort of oxidative stress disease state.
    Type: Application
    Filed: May 10, 2013
    Publication date: April 30, 2015
    Inventors: Craig Crews, Jeff Gustafson, Anke Gundula Roth, Hyun Seop Tae, Dennis Buckley, Taavi Neklesa
  • Publication number: 20150111937
    Abstract: The present invention provides methods, compositions, and kits for treating intestinal hyperpermeability in a subject in need thereof, including conditions such as hyperglycemia and underlying diseases such as diabetes, autism, fibromyalgia, inflammatory bowel disease (IBD), graft versus host disease (GVHD), HIV/AIDS, multiple organ dysfunction syndrome, irritable bowel syndrome (IBS), celiac disease, eczema, psoriasis, acute pancreatitis, Parkinson's disease, depression, chronic fatigue syndrome, asthma, multiple sclerosis, arthritis, ankylosing spondylitis, nonalcoholic fatty liver disease, alcoholic cirrhosis, environmental enteropathy, or kwashiorkor.
    Type: Application
    Filed: October 21, 2014
    Publication date: April 23, 2015
    Inventor: Steven Hoffman
  • Publication number: 20150111878
    Abstract: The present invention provides methods, compositions, and kits for treating intestinal hyperpermeability in a subject in need thereof, including underlying diseases such as diabetes, autism, fibromyalgia, inflammatory bowel disease (IBD), graft versus host disease (GVHD), HIV/AIDS, multiple organ dysfunction syndrome, irritable bowel syndrome (IBS), celiac disease, eczema, psoriasis, acute pancreatitis, Parkinson's disease, depression, chronic fatigue syndrome, asthma, multiple sclerosis, arthritis, ankylosing spondylitis, nonalcoholic fatty liver disease, alcoholic cirrhosis, environmental enteropathy, or kwashiorkor.
    Type: Application
    Filed: October 24, 2013
    Publication date: April 23, 2015
    Inventor: STEVEN HOFFMAN
  • Publication number: 20150065546
    Abstract: The present invention relates to diarylhydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Application
    Filed: March 24, 2014
    Publication date: March 5, 2015
    Applicant: The Regents of the University of California
    Inventors: Michael E. Jung, Dongwon Yoo, Charles L. Sawyers, Chris Tran, John Wongvipat
  • Publication number: 20150065475
    Abstract: Oil-in-water fungicidal formulations are prepared having pigment dispersed therein, the pigment being stable within the oil-in-water emulsion as a result of the addition of suitable silicone surfactants and suitable emulsifiers. The formulations can be prepared either as a 2-pack formulation or as a single formulation. In the case of the single formulation polyethylene glycol is also added. In either case, the formulations show a synergistic effect through the addition of the pigment, the resulting formulations having an increased efficacy. Further, the formulations show a synergistic effect when mixed with conventional chemical fungicides, both being added in reduced amounts compared to recommended rates.
    Type: Application
    Filed: September 9, 2014
    Publication date: March 5, 2015
    Inventors: Michael Fefer, Jun Liu, Tomoki Ruo, Sonia Edith Hevia
  • Publication number: 20150065548
    Abstract: A liquid composition comprises an organic diluent and at least one cellulose ether having anhydroglucose units joined by 1-4 linkages and having methyl groups, hydroxyalkyl groups, and optionally alkyl groups being different from methyl as substituents such that hydroxyl groups of anhydroglucose units are substituted with methyl groups such that s23/s26 is 0.29 or less, wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 3-positions of the anhydroglucose unit are substituted with a methyl group and wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 6-positions of the anhydroglucose unit are substituted with a methyl group. The liquid composition can be used for preparing a solid dispersion of an active ingredient in a cellulose ether.
    Type: Application
    Filed: April 8, 2013
    Publication date: March 5, 2015
    Inventors: Roland Adden, Robert L. Sammler, Meinolf Brackhagen, Nicholas S. Grasman, Oliver Petermann, Steven J. Guillaudeu
  • Publication number: 20150065547
    Abstract: An esterified cellulose ether comprises (i) aliphatic monovalent acyl groups or (ii) groups of the formula —C(O)—R—COOA wherein R is a divalent aliphatic or aromatic hydrocarbon group and A is hydrogen or a cation or (iii) a combination of aliphatic monovalent acyl groups and groups of the formula —C(O)—R—COOA, wherein the cellulose ether has anhydroglucose units joined by 1-4 linkages and has methyl groups, hydroxyalkyl groups, and optionally alkyl groups being different from methyl as substituents such that the esterified cellulose ether has an MS (hydroxyalkyl) of 0.05 to 1.00, and hydroxyl groups of anhydroglucose units are substituted with methyl groups such that [s23/s26?0.2*MS(hydroxyalkyl)] is 0.
    Type: Application
    Filed: October 24, 2012
    Publication date: March 5, 2015
    Applicant: Dow Global Technologies LLC
    Inventors: Robert L. Schmitt, Robert L. Sammler, Meinolf Brackhagen, Oliver Petermann, Roland Adden, Nicholas S. Grasman, Steven J. Guillaudeu
  • Publication number: 20150056164
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: April 24, 2014
    Publication date: February 26, 2015
    Applicant: AbbVie Inc.
    Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
  • Patent number: 8957099
    Abstract: A method is described for treating attention deficit hyperactivity disorder (ADHD), by administering to the individual an anti-epileptic mood stabilizer at a dose which is sub-therapeutic for mood stabilization, optionally in combination with a psychostimulant. Also described is a method of improving reading comprehension and/or fluency in an individual suffering from learning difficulties which method comprises administering to the individual an anti-epileptic mood stabilizer.
    Type: Grant
    Filed: February 7, 2008
    Date of Patent: February 17, 2015
    Assignee: Gosforth Centre (Holdings) Pty Ltd.
    Inventor: Philip Bird
  • Publication number: 20150018377
    Abstract: The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy.
    Type: Application
    Filed: March 27, 2014
    Publication date: January 15, 2015
    Applicant: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Giuseppe ALVARO, Anne Decor, Stefano Fontana, Dieter Hamprecht, Charles Large, Agostino Marasco
  • Publication number: 20150018323
    Abstract: Methods and kits for characterizing a subject having a steroid-dependent disease such as prostate cancer are described. A method of treating a steroid-dependent disease in a subject by obtaining a biological sample from the subject, determining if the HSD3B1(1245C) gene or 3?HSD1(367T) protein is expressed in the biological sample, and providing treatment other than or in addition to steroid ablation to the subject if the HSD3B1(1245C) gene or 3?HSD1(367T) protein is expressed is also described.
    Type: Application
    Filed: July 14, 2014
    Publication date: January 15, 2015
    Inventors: Nima Sharifi, Kai-Hsiung Chang
  • Publication number: 20150011516
    Abstract: Pharmaceutical compositions that bind to a predicted FK506 Binding Protein 52 (FKBP52) interaction surface on the androgen receptor hormone binding domain, otherwise known as FKBP52 Targeting Agents (FTAs) are provided. These compositions of the present invention are found to specifically recognize the FKBP52 regulatory surface on the androgen receptor and inhibit FKBP52 from functionally interacting with the androgen receptor. Compositions comprising the pharmaceutical composition, as well as methods of use, treatment and screening are also provided.
    Type: Application
    Filed: July 21, 2014
    Publication date: January 8, 2015
    Inventors: Leonard M. Neckers, Marc B. Cox, Jane B. Neckers, Yeong Sang Kim, Aki Iwai, Yangmin Ning, Johanny Tonos de Leon, Heather A. Balsiger, Robert Fletterick
  • Publication number: 20150010651
    Abstract: The present invention is directed to a wound composition comprising an effective amount of phenyloin and an effective amount of vitamin C. The present invention is further directed to a method of treating a wound in a patient comprising administering an effective amount of phenyloin and an effective amount of vitamin C to the wound.
    Type: Application
    Filed: July 8, 2014
    Publication date: January 8, 2015
    Inventor: Keshav Malshe
  • Publication number: 20140378517
    Abstract: This disclosure provides formulations of enzalutamide and their use for treating hyperproliferative disorders.
    Type: Application
    Filed: September 10, 2014
    Publication date: December 25, 2014
    Inventors: Douglas Alan Lorenz, Sanjay Konagurthu, Randy J. Wald, Jason A. Everett, Sheila Matz, Yuuki Takaishi, Toshiro Sakai, Ryousuke Irie, Shinsuke Oba, Hiroyasu Toyota, Koji Nishimura, Atsushi Kanbayashi
  • Publication number: 20140371284
    Abstract: Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. Said imidazolidinedione compounds posses androgen receptor antagonist activity and can be used for preventing and treating diseases and disorders related to androgen receptor, such as prostate cancer, alopecia, hair regeneration, acne and adolescent acne.
    Type: Application
    Filed: December 13, 2012
    Publication date: December 18, 2014
    Applicant: HC PHARMACEUTICAL CO., LTD.
    Inventor: Yuanwei Chen
  • Publication number: 20140371283
    Abstract: In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition.
    Type: Application
    Filed: February 12, 2014
    Publication date: December 18, 2014
    Applicant: Buck Institute for Research on Aging
    Inventors: VARGHESE JOHN, Dale E. BREDESEN
  • Publication number: 20140343111
    Abstract: The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Application
    Filed: December 20, 2013
    Publication date: November 20, 2014
    Applicant: The Regents of the University of California
    Inventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Chris Tran, John Wongvipat, Dongwon Yoo
  • Publication number: 20140335080
    Abstract: Compounds having a structure of Structure I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein R1, R2, R3, R4, R5, J1, J2, X, Z, n1 and n2 are as defined herein, and wherein at least one of R1, R2 or R3 is an alkyl, alkenyl, aryl or aralkyl ester, are provided. Uses of such compounds for treatment of various indications, including prostate cancer, as well as methods of treatment involving such compounds are also provided.
    Type: Application
    Filed: May 9, 2014
    Publication date: November 13, 2014
    Applicants: The University of British Columbia, British Columbia Cancer Agency Branch
    Inventors: Raymond J. Andersen, Marianne D. Sadar, Javier Garcia Fernandez, Nasrin R. Mawji, Jun Wang, Carmen Adriana Banuelos
  • Publication number: 20140296312
    Abstract: The disclosure describes the use of one or more compounds that fall within the scope of one or more of structural formulae I, II, III, IV, V, or VI for treating triple negative breast Compounds useful for treating breast cancer include those compounds of formulae I, II, III, IV, V, or VI that inhibit proliferation of breast cancer cells and/or lead to the death of breast cancer cells, especially triple negative breast cancer.
    Type: Application
    Filed: July 27, 2012
    Publication date: October 2, 2014
    Applicants: THE REGENTS OF THE UNIVERSITY OF COLORADO, MEDIVATION PROSTATE THERAPEUTICS, INC.
    Inventors: Andrew A. Protter, Jennifer Richer, Dawn Cochrane
  • Patent number: 8829036
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Grant
    Filed: March 14, 2012
    Date of Patent: September 9, 2014
    Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Inc.
    Inventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voight, Corey O. Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, Jr., John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Xiaoiang Liu, Tao Guo, Thuy X. E. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse, Ying Huang, Guoqing Li, Jianping Pan, Jeffrey A. Misiaszek, Gaifa Lai, Jingqi Duo, Chuanxing Qu, Yuefei Shao
  • Patent number: 8816095
    Abstract: Disclosed are molecules and their synthesis, for use in blocking gated ion channels such as voltage-gated sodium channels (VGSCs) and prostate voltage sodium channels (PVSCs). These inhibitors have superior blocking efficacy, for instance in displacing the radioligand [3H]-Batrachotoxin-B ([3H]-BTX-B) that binds to site 2 of a VGSC. The molecules of the invention comprise a moiety which increases the binding affinity of molecules for the protein binding site in prostate cancer cells (PCs), and which is also fluorescent. In one embodiment the invention molecules are an inhibition system that can be used to target over-abundant or hyperactive VGSCs selectively in pain, epilepsy or prostate cancer, inhibiting the proliferation of PCs. The fluorescent moiety also facilitates screening, tracking, and pharmacodynamic studies of the drug in a biological system both in vitro and in vivo.
    Type: Grant
    Filed: August 17, 2009
    Date of Patent: August 26, 2014
    Assignee: Georgetown University
    Inventors: Milton L. Brown, Scott Grindrod, Thomas H. Walls, Todd Hansen, Simeng Suy, Mikell A. Paige
  • Publication number: 20140235681
    Abstract: Disclosed herein is method of treating glaucoma or ocular hypertension comprising administering a prostaglandin agonist and a second therapeutically active agent to a mammal in need thereof, wherein said second therapeutically active agent is selected from: ?-Blockers, Adrenergic Agonists, non-selective adrenergic agonists, ?2-selective adrenergic agonists, Carbonic Anhydrase Inhibitors, Cholinergic Agonists, direct acting cholinergic agonists, chlolinesterase inhibitors, Glutamate Antagonists, Ca2+ channel blockers, Prostamides, Prostaglandins, Cannabinoids, and combinations thereof. Compositions and medicaments containing a combination of these two active agents are also disclosed.
    Type: Application
    Filed: December 6, 2013
    Publication date: August 21, 2014
    Applicant: ALLERGAN, INC.
    Inventors: SCOTT M. WHITCUP, ROBERT M. BURK, DAVID W. OLD, YARIV DONDE, WHA-BIN IM, MARK A. HOLOBOSKI
  • Publication number: 20140221286
    Abstract: It is discovered that sodium-channel blockers inhibit the secretion of glucagon from pancreatic alpha cells. The present disclosure, based on such discoveries, provides compositions and methods for the treatment of hyperglycemia and related diseases and conditions with Na-channel blockers.
    Type: Application
    Filed: September 20, 2012
    Publication date: August 7, 2014
    Inventors: Luiz Belardinelli, Arvinder Dhalla
  • Publication number: 20140200516
    Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II; aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.
    Type: Application
    Filed: March 18, 2014
    Publication date: July 17, 2014
    Applicant: ABBOTT LABORATORIES
    Inventor: Harry A. DUGGER, III
  • Patent number: 8772324
    Abstract: The present invention is directed to a wound composition comprising an effective amount of phenytoin and an effective amount of vitamin C. The present invention is further directed to a method of treating a wound in a patient comprising administering an effective amount of phenytoin and an effective amount of vitamin C to the wound.
    Type: Grant
    Filed: March 18, 2010
    Date of Patent: July 8, 2014
    Inventor: Keshav Malshe
  • Publication number: 20140179749
    Abstract: This disclosure provides formulations of enzalutamide and their use for treating hyperproliferative disorders.
    Type: Application
    Filed: September 11, 2013
    Publication date: June 26, 2014
    Applicants: BEND RESEARCH, ASTELLAS PHARMA INC., MEDIVATION PROSTATE THERAPEUTICS, INC.
    Inventors: Douglas Alan Lorenz, Sanjay Konagurthu, Randy J. Wald, Jason A. Everett, Sheila Matz, Yuuki Takaishi, Toshiro Sakai, Ryousuke Irie, Shinsuke Oba, Hiroyasu Toyota, Koji Nishimura, Atsushi Kanbayashi
  • Publication number: 20140142140
    Abstract: An anti-epileptic agent for use in the treatment of a neurological disorder other than epilepsy characterised in that the anti-epileptic agent is the sole active agent and that the daily dose of the anti-epileptic is less than 20% of the minimum daily dose which is effective for mood stabilisation or treatment of epileptic symptoms.
    Type: Application
    Filed: July 9, 2012
    Publication date: May 22, 2014
    Applicant: GOSFORTH CENTRE (HOLDINGS) PTY LTD
    Inventor: Philip Bird
  • Patent number: 8710086
    Abstract: Substituted di-arylhydantoin and di-arylthiohydantoins are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including CRPC and/or hormone-sensitive prostate cancer.
    Type: Grant
    Filed: April 9, 2010
    Date of Patent: April 29, 2014
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Rajendra Parasmal Jain
  • Publication number: 20140105908
    Abstract: Disclosed herein are methods and compositions for reducing the recurrence of prostate cancer and for treating prostate cancer.
    Type: Application
    Filed: May 3, 2012
    Publication date: April 17, 2014
    Applicant: UNIVERSITY OF ROCHESTER
    Inventor: Chawnshang Chang
  • Publication number: 20140100256
    Abstract: This disclosure provides formulations of enzalutamide and their use for treating hyperproliferative disorders.
    Type: Application
    Filed: September 11, 2013
    Publication date: April 10, 2014
    Applicants: BEND RESEARCH, ASTELLAS PHARMA INC., MEDIVATION PROSTATE THERAPEUTICS, INC.
    Inventors: Douglas Alan Lorenz, Sanjay Konagurthu, Randy J. Wald, Jason A. Everett, Sheila Matz, Yuuki Takaishi, Toshiro Sakai, Ryousuke Irie, Shinsuke Oba, Hiroyasu Toyota, Koji Nishimura, Atsushi Kanbayashi
  • Publication number: 20140088129
    Abstract: Described herein are methods of treating non-metastatic castrate-resistant prostate cancer with anti-androgens.
    Type: Application
    Filed: September 23, 2013
    Publication date: March 27, 2014
    Applicant: Aragon Pharmaceuticals, Inc.
    Inventor: Isan Chen
  • Patent number: 8680291
    Abstract: The present invention relates to diarylhydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Grant
    Filed: October 24, 2008
    Date of Patent: March 25, 2014
    Assignee: The Regents of the University of California
    Inventors: Michael E. Jung, Dongwon Yoo
  • Patent number: 8658681
    Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.
    Type: Grant
    Filed: April 17, 2012
    Date of Patent: February 25, 2014
    Assignee: The Regents of the University of California
    Inventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Chris Tran, John Wongvipat
  • Publication number: 20140039020
    Abstract: The invention relates to (among other things) oligomer-containing hydantoin compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.
    Type: Application
    Filed: December 15, 2011
    Publication date: February 6, 2014
    Applicant: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Stephanie Allums-Donald
  • Patent number: 8624037
    Abstract: The subject matter of the present application is novel imidazolidine-2,4-dione derivatives. These products have an antiproliferative activity. They are particularly advantageous for treating pathological conditions and diseases associated with abnormal cell proliferation, such as cancers. The invention also relates to pharmaceutical compositions containing said products and to the use thereof for preparing a medicament.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: January 7, 2014
    Assignee: Ipsen Pharma S.A.S.
    Inventors: Dennis Bigg, Serge Auvin, Christophe Lanco, Grégoire Prevost
  • Publication number: 20130336962
    Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R, R1, R2, R3, R4, M1, M2, X, L1, L2, J1, J2, a1, a2, b1 and b2 are as defined herein, and wherein at least one of M2 or L2 is a moiety comprising an aziridine, acrylamide or sulfonate functional group, are provided. Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided.
    Type: Application
    Filed: April 16, 2013
    Publication date: December 19, 2013
    Applicants: The University of Biritish Columbia, British Columbia Cancer Agency Branch
    Inventors: British Columbia Cancer Agency Branch, The University of British Columbia
  • Publication number: 20130331421
    Abstract: Compositions, such as pharmaceutical compositions, comprising specific diarylhydantoin and diarylthiohydantoin compounds, or salts or solvates thereof, are provided. Isolated and purified forms of the compounds are also described, as are unit dosage forms, compositions of substantially pure compound and kits comprising the compounds. The compounds and pharmaceutical compositions thereof may find use in the prevention and/or treatment of a variety of conditions, including prostate cancer, Parkinson's disease, Alzheimer's disease, and others.
    Type: Application
    Filed: June 24, 2013
    Publication date: December 12, 2013
    Applicant: MEDIVATION PROSTATE THERAPEUTICS, INC.
    Inventors: Rajendra Parasmal Jain, Jacqueline A. Gibbons
  • Publication number: 20130289085
    Abstract: Compounds of Formula (I), and methods of making and using thereof, are described herein; wherein AR is an aryl group, ZBG is a Zinc Binding Group, and other substituents are as defined herein. The compounds can be administered as a pharmaceutically acceptable salt, prodrug, or solvate. The compounds may be useful to treat and/or prevent hyperproliferative disorders which may include hormone sensitive and hormone refractory prostate cancers. The compounds can be formulated with a pharmaceutically acceptable carrier and, optionally one or more pharmaceutically acceptable excipients, for enteral or parenteral administration.
    Type: Application
    Filed: September 28, 2011
    Publication date: October 31, 2013
    Inventors: Adegboyega Oyelere, Berkley Gryder
  • Publication number: 20130281500
    Abstract: The novel active compound combinations of a carboxamide of the general formula (I) (group 1) in which R, G, R and A have the meanings given in the description and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.
    Type: Application
    Filed: June 12, 2013
    Publication date: October 24, 2013
    Inventors: Ulrike WACHENDORFF-NEUMANN, Peter DAHMEN, Ralf DUNKEL
  • Publication number: 20130267510
    Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Application
    Filed: December 6, 2011
    Publication date: October 10, 2013
    Applicant: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Giuseppe Alvaro, Paolo Dambruoso, Simona Tommasi, Anne Decor, Charles Large
  • Publication number: 20130252992
    Abstract: The present invention relates to novel cyclic N,N?-diarylurea-androgen receptor antagonist, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of breast cancer disease. Cyclic N,N?-diarylthioureas or N,N?-diarylureas of the general formula 1, their optical (R)- and (S)-isomers and pharmaceutically acceptable salts thereof exhibiting properties of androgen receptor antagonists have been proposed, wherein: R1 represents C1-C3 alkyl; R4 and R5 represent hydrogen; or R4 represents hydrogen, R5 represents methyl; or R4 represents methyl, R5 represents CH2R6 group in which R6 is C1-C3 alkoxycarbonyl, carboxyl, hydroxyl group optionally substituted with methyl or benzyl; or R4 and R5 together with the carbon atom they are attached to form 5- or 6-membered saturated heterocycle including at least one oxygen atom or nitrogen atom optionally substituted with methyl.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 26, 2013
    Inventors: Alexandre Vasilievich IVACHTCHENKO, Oleg Dmitrievich MITKIN
  • Publication number: 20130210769
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).
    Type: Application
    Filed: March 15, 2013
    Publication date: August 15, 2013
    Applicant: IRM LLC
    Inventors: Hong Liu, Xiaohui He, Dean Paul Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
  • Publication number: 20130196981
    Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description, and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 1, 2013
    Applicant: Bayer Intellectual Property GmbH
    Inventor: Bayer Intellectual Property GmbH
  • Publication number: 20130184214
    Abstract: Pharmaceutical compositions and kits including a tyrosine hydroxylase inhibitor, a melanin promoter, a p450 3A4 promoter, and a leucine aminopeptidase inhibitor are provided. Also provided are methods of treating cancer in a subject, comprising administering an effective amount of a tyrosine hydroxylase inhibitor, a melanin promoter, a p450 3A4 promoter, and a leucine aminopeptidase inhibitor to the subject in need thereof. Also provided are methods of reducing cell proliferation in a subject comprising administering an effective amount of a tyrosine hydroxylase inhibitor, a melanin promoter, a p450 3A4 promoter, and a leucine aminopeptidase inhibitor to the subject in need thereof.
    Type: Application
    Filed: February 10, 2012
    Publication date: July 18, 2013
    Inventor: Steven Hoffman
  • Publication number: 20130184227
    Abstract: This invention is to provide multiple specific inhibitors of cytochrome P450 isozyme CYP2C9. These inhibitors can be derived from any combinations with the following compounds including: Tamarixetin, Formononetin, isoliquritigenin, Phloretin, luteolin, Quercitrin, quercetin, myricetin, Wongonin, Puerarin, Genistein, Nordihydroguaiaretic acid, Narigenin, Capillarisin, Chrysin, Fisefin, eriodictyol, 6-Gingerol, Isorhamneti, isoquercitrin, Morin, (+)-Taxifolin, isovitexin, 3-Phenylpropyl Acetate, Oleanolic acid, ursolic acid, ?-Myrcene, cinnamic acid, Luteolin-7-Glucoside, Liquiritin, (+) Limonene, Homoorientin, Swertiamarin, Embelin, Daidzein, Poncirin, (?)-Epicatechin, ergosterol. These natural products can be used to enhance the bioavailability of therapeutic agents (drugs).
    Type: Application
    Filed: November 30, 2009
    Publication date: July 18, 2013
    Inventors: Oliver Yoa-Pu HU, Hong-Jaan Wang, Cheng-Huei Hsiong, Li-Heng Pao
  • Patent number: 8470829
    Abstract: An imidazole derivative represented by formula (I): wherein Q is: A is hydrogen, halogen, or a substituted or unsubstituted C1-4 alkyl group; E is independently selected from a C1-6 alkyl group; R2 and R3 are independently selected from C1-6 alkyls; X1 and X2 are independently selected from O and S; Y is selected from a substituted or unsubstituted arylene group and a substituted or unsubstituted divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group; Z is —CON(—Ra)—, —CO—, —OOO—, —NRa—C(?NH)NRb—, —NRa—C(?N—CN)NRb—, —N(—Ra)COO—, —C(?NH)—, —SO2—, —SO2N(—Ra)—, —SO2NR1—, —N(—Ra)CO—, —N(—Ra)CON(—Rb)—, —N(COR1)CO—, —N(—Ra)SO2—, —N(SO2R1)SO2—, —N(—Ra)— or —N(—Ra)SO2N(—Rb)—; R1 is independently a hydrogen atom, a hydroxyl group, or substituted or unsubstituted group selected from C1-6 alkyl group, heterocyclic group, aryl group, C3-8 cycloalkyl group and C3-8 cycloalkenyl group; or salt or prodrug thereof.
    Type: Grant
    Filed: September 9, 2005
    Date of Patent: June 25, 2013
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Kazutaka Tachibana, Haruhiko Sato, Masateru Ohta, Mitsuaki Nakamura, Takuya Shiraishi, Hitoshi Yoshino, Takashi Emura, Akie Honma, Etsuro Onuma, Hiromitsu Kawata, Kenji Taniguchi