Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/443)
  • Patent number: 10160752
    Abstract: Disclosed is a compound of formula (I). or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions including the compound of formula (I) and methods of using the compound of formula (I).
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: December 25, 2018
    Assignee: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Gregory R. Thatcher, Marton Siklos, Rui Xiong
  • Patent number: 9955689
    Abstract: The present invention provides a method for promoting plant growth, which comprises treating a plant with at least one compound selected from a group consisting of a compound represented by the following Formula (1): and an agriculturally acceptable salt thereof, provided that a method for promoting plant growth which comprises treating plants with a compound corresponding to any one of the following (1) to (5) and an agriculturally acceptable salt thereof is excluded: (1) 4-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, (2) 5-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, (3) 6-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, (4) 7-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, and (5) Benzo[b]thiophene-2-carboxylic acid.
    Type: Grant
    Filed: October 31, 2013
    Date of Patent: May 1, 2018
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Fujio Mukumoto, Hiroaki Tamaki, Shintaro Kusaka, Mitsuhiko Iwakoshi
  • Patent number: 9894901
    Abstract: The present invention provides a method for promoting plant growth, which comprises treating a plant with a compound represented by the following Formula (1): provided that a method for promoting plant growth which comprises treating plants with a compound corresponding to any one of the following (1) to (8) is excluded: (1) Methyl 4-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, (2) Methyl 5-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, (3) Methyl 6-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, (4) Methyl 7-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, (5) Ethyl 4-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, (6) Ethyl 5-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, (7) Ethyl 6-(trifluoromethyl)benzo[b]thiophene-2-carboxylate, and (8) Ethyl 7-(trifluoromethyl)benzo[b]thiophene-2-carboxylate.
    Type: Grant
    Filed: October 31, 2013
    Date of Patent: February 20, 2018
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Fujio Mukumoto, Hiroaki Tamaki, Shintaro Kusaka, Mitsuhiko Iwakoshi
  • Patent number: 9717725
    Abstract: Embodiments of the invention provide methods of attenuating, e.g., inhibiting or reducing, cellular proliferation and migration, particularly endothelial cell proliferation and migration, including that associated with angiogenesis, as well as attenuating cancerous tumor growth and metastasis, using opioid antagonists, including, but not limited to, those that are peripherally restricted antagonists.
    Type: Grant
    Filed: August 21, 2013
    Date of Patent: August 1, 2017
    Assignee: THE UNIVERSITY OF CHICAGO
    Inventors: Jonathan Moss, Mark Lingen, Patrick A. Singleton, Joe G. N. Garcia
  • Patent number: 9700563
    Abstract: The invention is directed to a method of treatment for chronic pain, the method comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 21, 2016
    Date of Patent: July 11, 2017
    Assignee: MediSynergies, LLC
    Inventors: Dennis Michael Godek, Harry Ralph Howard
  • Patent number: 9394288
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of asthma and allergy may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of respiratory diseases, respiratory disorders, COPD, bronchitis, brain injury, inflammation, inflammatory skin diseases, asthma, allergic reactions, infections due to acute allergy, bronchospasm, respiratory distress, acute asthma, leukotrienes over activity, 5-LO enzyme activity and cancer.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: July 19, 2016
    Assignee: CELLIX BIO PRIVATE LIMITED
    Inventor: Mahesh Kandula
  • Patent number: 9214637
    Abstract: Provided are a novel chalcogen-containing aromatic compound and an organic electronic device using the compound. This compound is a chalcogen-containing aromatic compound represented by the formula (1). Among the organic electronic devices each using this chalcogen-containing aromatic compound are an organic EL device, an organic TFT device, a photovoltaic device, and the like. In the formula (1): X represents oxygen, sulfur, or selenium; A represents an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon group, an aromatic heterocyclic group, or an amino group; and n's each independently represent an integer of 0 to 2, provided that a sum of two n's is 1 to 4.
    Type: Grant
    Filed: October 3, 2011
    Date of Patent: December 15, 2015
    Assignee: NIPPON STEEL & SUMIKIN CHEMICAL CO., LTD.
    Inventors: Mitsuru Suda, Takahiro Kai, Megumi Matsumoto
  • Patent number: 9150537
    Abstract: Provided is a compound which has strong intraocular pressure lowering action and has no side effect on eyes such as ocular stimulating property, humor protein rise etc. Since a compound represented by the formula (I): (wherein definition of each group is as described in the specification), or a salt thereof, a solvate thereof, or a prodrug thereof has strong intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
    Type: Grant
    Filed: January 26, 2012
    Date of Patent: October 6, 2015
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Toru Maruyama, Tohru Kambe, Shinsaku Yamane, Satoshi Nakayama
  • Publication number: 20150148314
    Abstract: There are provided, inter alia, derivatives of seriniquinone and methods useful for the treatment of cancer, and in particular treatment of melanoma and prostate cancer.
    Type: Application
    Filed: January 27, 2015
    Publication date: May 28, 2015
    Inventors: William Fenical, Paul R. Jensen, James J. La Clair, Lynnie Trzoss, Takashi Fukuda
  • Publication number: 20150148389
    Abstract: The invention is directed to methods of treating organ specific infections in a host organism by administering compounds that target host receptors and/or host cellular signaling molecules to prevent a pathogen from infecting the organ. For example, the administration of a compound to prevent a pathogen from crossing the blood-brain barrier to prevent a brain infection.
    Type: Application
    Filed: February 3, 2015
    Publication date: May 28, 2015
    Inventor: Kwang S. Kim
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Publication number: 20150126593
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of asthma and allergy may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of respiratory diseases, respiratory disorders, COPD, bronchitis, brain injury, inflammation, inflammatory skin diseases, asthma, allergic reactions, infections due to acute allergy, bronchospasm, respiratory distress, acute asthma, leukotrienes over activity, 5-LO enzyme activity and cancer.
    Type: Application
    Filed: February 27, 2013
    Publication date: May 7, 2015
    Inventor: Mahesh Kandula
  • Patent number: 9023885
    Abstract: The invention relates to pharmaceutical compositions and methods of treating inflammatory-related diseases associated with pro-inflammatory cytokine expression and/or reduced expression of anti-inflammatory cytokines. The method typically comprises administration of one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, such as, Meisoindigo and NATURA. Preferably the pharmaceutical composition comprises one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, an anti-inflammatory agent, and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: May 5, 2015
    Assignee: Natrogen Therapeutics International, Inc.
    Inventors: Longgui Wang, Xiao Mei Liu, Lian Mo, Simon K. Mencher, James P. McCarron, Jr.
  • Patent number: 9023874
    Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: May 5, 2015
    Assignee: Merial, Inc.
    Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
  • Patent number: 9006283
    Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: April 14, 2015
    Assignee: Acumen Pharmaceuticals, Inc.
    Inventors: Grant A. Krafft, Todd Pray, William F. Goure
  • Patent number: 8980938
    Abstract: The invention relates to compounds of the formula I in which R1, R2, A, B, X and Y have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: March 17, 2015
    Assignee: Sanofi
    Inventors: Stephanie Hachtel, Juergen Dedio, Josef Pernerstorfer, Stephen Shimshock, Carolina Lanter
  • Publication number: 20150072961
    Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) for treatment of pulmonary conditions (e.g. asthma). The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: November 14, 2014
    Publication date: March 12, 2015
    Inventors: Chongxi YU, Lina XU
  • Publication number: 20150056141
    Abstract: It has been found that efficient screening for a compound having anticancer activity can be achieved by selecting a compound having activity to induce alternative autophagy using, as an index, formation of fluorescent bright spots due to aggregation of a lysosomal protein to which a fluorescent protein is attached in cells expressing the lysosomal protein.
    Type: Application
    Filed: February 7, 2013
    Publication date: February 26, 2015
    Applicant: National University Corporation Tokyo Medical and Dental University
    Inventors: Shigeomi Shimizu, Takamitsu Hosoya, Michiko Murohashi, Suguru Yoshida
  • Patent number: 8962648
    Abstract: Tricyclic compounds are provided. These compounds are PBK inhibitors, and are useful for the treatment of PBK related diseases, including cancer.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: February 24, 2015
    Assignee: OncoTherapy Science, Inc.
    Inventors: Yusuke Nakamura, Yo Matsuo, Shoji Hisada, Feryan Ahmed, Raymond Huntley, Zohreh Sajjadi-Hashemi, David M. Jenkins, Robert B. Kargbo, Wenge Cui, Polivina Jolicia F. Gauuan, Joel R. Walker, Helene Decornez, Mahender Gurram
  • Publication number: 20150051220
    Abstract: A compound of formula (I) for use in the treatment of a condition or disorder associated with nicotinamide adenine dinucleotide phosphate oxidase.
    Type: Application
    Filed: March 14, 2013
    Publication date: February 19, 2015
    Applicant: GLUCOX BIOTECH AB
    Inventors: Mona Wilcke, Erik Walum, Per Wikstrom
  • Publication number: 20150045327
    Abstract: The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 12, 2015
    Inventors: Steven Emiel VAN DER PLAS, Hans KELGTERMANS, Sébastien Jean Jacques Cédric DROPSIT MONTOVER, Sébastien Laurent Xavier MARTINA, Martin James Inglis ANDREWS
  • Patent number: 8946219
    Abstract: The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing [4-(6-fluoro-7-methylamino-2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)-phenyl]-5-chloro-thiophen-2-yl-sulfonylurea, or a pharmaceutically acceptable salt thereof, for the treatment of thrombosis diseases.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 3, 2015
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Pamela B. Conley, Patrick Andre, Uma Sinha
  • Publication number: 20150031727
    Abstract: [Problem] To provide a compound that has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. [Means for Solution] The present inventors conducted their studies on a compound that has an NPT-IIb inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. As a result, they created an aminoalkyl-substituted N-thienylbenzamide derivative which has NPT-IIb inhibitory action, thereby completing the present invention. The aminoalkyl-substituted N-thienylbenzamide derivative of the present invention has an NPT-IIb inhibitory action and can be used as an agent for preventing and/or treating hyperphosphatemia.
    Type: Application
    Filed: October 25, 2012
    Publication date: January 29, 2015
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Masanori Miura, Daisuke Kaga, Susumu Watanuki, Shunichiro Hachiya, Takao Okuda, Ippei Sato, Mai Isomura, Kazuhiro Terai, Yoh Terada
  • Publication number: 20150025068
    Abstract: A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 22, 2015
    Inventors: Jessica Martinsson, Katarina Faernegardh, Mattias Joensson, Rune Ringom
  • Publication number: 20150018410
    Abstract: The present invention relates to a novel naphtho class of compounds as Stat3 pathway inhibitors and as cancer stem cell inhibitors; to methods of using such compounds to treat cancer; to methods of using such compounds to treat disorders in a mammal related to aberrent Stat3 pathway activity; to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: September 29, 2014
    Publication date: January 15, 2015
    Inventors: Zhiwei Jiang, Chiang Jia Li, Wei Li, David Leggett
  • Publication number: 20150018399
    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: August 5, 2014
    Publication date: January 15, 2015
    Inventors: SONGNIAN LIN, Fengqi Zhang, Emma R. Parmee, Sunita V. Dewnani
  • Publication number: 20150018400
    Abstract: Disclosed herein is a method comprising administering a compound to a mammal suffering from an inflammatory bowel disease for the treatment of said disease, said compound having a structure according to Formula I wherein X, Y, B, R2, R3, R4, R5, R6 and n have the meanings found herein.
    Type: Application
    Filed: May 2, 2014
    Publication date: January 15, 2015
    Inventors: YARIV DONDE, JEREMIAH H. NGUYEN, KAREN M. KEDZIE, DANIEL W. GIL, JOHN E. DONELLO, WHA-BIN IM
  • Publication number: 20140371274
    Abstract: The present invention relates to novel compounds, their use in the prevention or treatment of symptoms and disorders associated with the bradykinin B1 pathway and pharmaceutical compositions containing them.
    Type: Application
    Filed: June 13, 2014
    Publication date: December 18, 2014
    Inventors: Andrea Rosario BECCARI, Gianluca BIANCHINI, Chiara LIBERATI, Michela FANI', Mara ZIPPOLI
  • Patent number: 8911765
    Abstract: A biodegradable, flexible covering for a breast implant is provided which comprises one or more biodegradable polymer layers dimensioned and shaped to cover at least a portion of the breast implant. The implant can be inserted into an opening of the covering immediately prior to surgery, but alternate configurations and times of insertion are contemplated as well as open or sheet type devices. The coverings can optionally contain one or more drugs for delivery at the surgical site, particularly for treating or preventing infection, pain, inflammation, capsular contracture, scarring or other complications associated with breast augmentation or breast reconstruction.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: December 16, 2014
    Assignee: Tyrx, Inc.
    Inventors: Arikha Moses, Satish Pulapura, Qing Ge, Sarita Nethula, Irene Shatova, Archana Rajaram
  • Patent number: 8901176
    Abstract: New uses of safinamide, safinamide derivatives and MAO-B inhibitors in novel types of treatment for Parkinson's Disease are described. More specifically, the invention relates to methods for treating Parkinson's Disease through the administration of safinamide, a safinamide derivative, or a MAO-B inhibitor, in combination with other Parkinson's Disease agents or treatments, such as levodopa/PDI or dopamine agonists.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: December 2, 2014
    Assignee: Newron Pharmaceuticals, S.P.A.
    Inventors: Ruggero Fariello, Carlo Cattaneo, Patricia Salvati, Luca Benatti
  • Publication number: 20140336111
    Abstract: The present invention relates to the therapeutic use of activators of the zinc finger protein GLI3 in diseases that are associated with reduced Hedgehog signaling in hepatocytes, in particular Polycystic ovary syndrome, Steatosis hepatis, Steatohepatit is and/or Adipositas. The invention further relates to methods of treating an individual with said activator, a pharmaceutical composition comprising said activator and the use of said activator as food supplement.
    Type: Application
    Filed: January 25, 2013
    Publication date: November 13, 2014
    Applicant: Universtität Leipzig
    Inventor: Rolf Gebhardt
  • Publication number: 20140336154
    Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: July 29, 2014
    Publication date: November 13, 2014
    Inventors: Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg
  • Patent number: 8883846
    Abstract: Disclosed embodiments concern the synthesis and use of therapeutic compounds that for treating emerging flu strains and minimizing resistance to such strains. Methods for making the disclosed compounds concern using a base-mediated addition/cyclization sequence followed by functional group manipulation to develop functionalized compounds that can target neuraminidase, which makes them ideal candidates for treating influenza. Pharmaceutical compositions comprising the therapeutic compounds and biologically-acceptable materials are also described. Methods of inhibiting neuraminidase in subjects that are suspected of containing neuraminidase are also described. The use of metabolites of the disclosed compounds can also be used in diagnostic assays for therapeutic dosing of the disclosed compounds.
    Type: Grant
    Filed: August 15, 2012
    Date of Patent: November 11, 2014
    Assignee: UVic Industry Partnerships Inc.
    Inventors: Jeremy E. Wulff, Michael G. Brant, Jeremy W. Mason, Caleb M. Bromba, Martin J. Boulanger
  • Publication number: 20140329675
    Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
    Type: Application
    Filed: May 3, 2014
    Publication date: November 6, 2014
    Applicant: INSCENT, INC.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Publication number: 20140329802
    Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.
    Type: Application
    Filed: March 28, 2014
    Publication date: November 6, 2014
    Applicant: Astellas Pharma Inc.
    Inventors: Shunichiro HACHIYA, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
  • Patent number: 8877801
    Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: November 4, 2014
    Assignee: Novartis AG
    Inventors: Heather Elizabeth Burks, Michael A. Dechantsreiter, Guo He, Jill Nunez, Stefan Peukert, Clayton Springer, Yingchuan Sun, Noel Marie-France Thomsen, George Scott Tria, Bing Yu
  • Publication number: 20140323446
    Abstract: The present invention provides methods of treating nasal polyps in cystic fibrosis patients using zileuton. The present invention also provides methods of treating nasal polyps in cystic fibrosis patients using zileuton in combination with surgical debridement and/or steroid treatment.
    Type: Application
    Filed: August 23, 2012
    Publication date: October 30, 2014
    Applicant: CORNERSTONE THERAPEUTICS INC.
    Inventors: Joseph K. Han, Carmen Dell'Anna
  • Publication number: 20140315899
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Andraka, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
  • Publication number: 20140309264
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 16, 2014
    Inventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK
  • Patent number: 8859616
    Abstract: The present invention provides a method for stimulating hair growth in a mammalian species or converting vellus hair or intermediate hair to terminal hair or stimulating hair follicles to increase hair growth and one or more properties selected from the group consisting of luster, sheen, brilliance, gloss, glow, shine or patina of hair associated with the follicles or increasing one or more of: length, thickness, number, and density, of eyelash hair or eyebrow hair comprising applying to the skin of a patient a composition comprising an effective amount of an EP3 agonist or an EP4 agonist prodrug or a mixture thereof. Such compositions which are used in treating the skin or scalp of a human or non-human animal may comprise an effective amount of 3, 7 or 3 and 7 thia prostanoic acid. A mixture of 3,7-dithia PGE1 and 3,7-dithia PGE1-isopropyl ester is preferred for this treatment.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: October 14, 2014
    Assignee: Allergan, Inc.
    Inventors: Jenny W. Wang, David F. Woodward
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Patent number: 8852937
    Abstract: The present invention makes available methods and reagents for modulating proliferation or differentiation in a cell or tissue comprising contacting the cell with a hedgehog agonist, such as the compounds depicted in FIGS. 32 and 33. In certain embodiments, the methods and reagents may be employed to correct or inhibit an aberrant or unwanted growth state, e.g., by antagonizing a normal ptc pathway or agonizing smoothened or hedgehog activity.
    Type: Grant
    Filed: August 20, 2007
    Date of Patent: October 7, 2014
    Assignee: Curis, Inc.
    Inventors: Anthony David Baxter, Edward Andrew Boyd, Maria Frank-Kamenetsky, Oivin Guicherit, Jeffery Porter, Stephen Price, Lee Rubin, John Harry Alexander Stibbard
  • Publication number: 20140275162
    Abstract: Treating Sonic Hedgehog-Associated Medulloblastoma comprises inhibiting the synthesis or biologic activity of leukotrienes that drive Nestin expression in cancerous or precancerous granule neuron precursors and that further drive growth and proliferation of medulloblastoma cells through Nestin-mediated aberrant Sonic Hedgehog signaling.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Applicant: Institute for Cancer Research d/b/a The Research Institute of Fox Chase Cancer Center
    Inventor: Institute for Cancer Research d/b/a The Research Institute of Fox Chase Cancer Center
  • Publication number: 20140275172
    Abstract: The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Nalin Subasinghe
  • Publication number: 20140275093
    Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: October 16, 2013
    Publication date: September 18, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, Sean J. Harrison, He Xu
  • Patent number: 8835654
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: September 16, 2014
    Assignee: BHI Limited Partnership
    Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
  • Patent number: 8835487
    Abstract: The invention provides methods for treating multiple sclerosis by administering biotin. The invention also provides methods for treating sequalae after multiple sclerosis attacks by administering biotin.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: September 16, 2014
    Assignee: Assistance Publique Hopitaux De Paris
    Inventor: Frédéric Sedel
  • Publication number: 20140256712
    Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 11, 2014
    Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.
    Inventors: Liming SHAO, John Emmerson CAMPBELL, Michael Charles HEWITT, Una CAMPBELL, Taleen G. HANANIA
  • Publication number: 20140256784
    Abstract: Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.
    Type: Application
    Filed: May 21, 2014
    Publication date: September 11, 2014
    Inventors: Joseph BARBOSA, Kenneth Gordon CARSON, Michael Walter GARDYAN, Jason Patrick HEALY, Qiang HAN, Ross MABON, Praveen PABBA, James TARVER, JR., Kristen M. TERRANOVA, Ashok TUNOORI, Xiaolian XU
  • Publication number: 20140248268
    Abstract: This invention relates to compounds and their use as inhibitors or activators of Rab7 GTPase to treat or prevent the onset of Rab 7 GTPase-associated disorders such as neuropathies, cancer, metabolic diseases of bone and lipid storage. The invention is also applicable to infectious diseases where Rab7 is inactivated or its protein-protein interactions are modulated to facilitate intracellular survival of pathogens. The compound described acts as a competitive inhibitor of nucleotide binding and as such also has utility as a scaffold for targeting other small GTPases. In one aspect, methods of treatment of the invention are used to treat or prevent the onset of hereditary sensory neuropathies such as Charcot-Marie-Tooth type 2B disease. Related pharmaceutical compositions, assays, and drug screens are also provided.
    Type: Application
    Filed: May 15, 2014
    Publication date: September 4, 2014
    Inventors: Angela Wandinger-Ness, Larry Sklar, Jacob Agola, Zurab Surviladze, Jeffrey Aube, Jennifer Golden, Chad E. Schroeder, Denise S. Simpson