Chalcogen Or Nitrogen Bonded Directly To The Imidazole Ring By Nonionic Bonding Patents (Class 514/398)
  • Patent number: 12037339
    Abstract: The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of GLP-1 receptor, a pharmaceutical composition comprising a compound of Formula (I), and a method of treating or preventing a disease in which GLP-1 receptor plays a role.
    Type: Grant
    Filed: July 20, 2021
    Date of Patent: July 16, 2024
    Assignee: Eccogene Inc.
    Inventors: Zaifang Ren, Xuefeng Sun, Jingye Zhou
  • Patent number: 11957737
    Abstract: Methods of treating or preventing microbial infection in a subject in need of treatment by administering a therapeutically effective amount of ergothioneine, or functional analog, or prodrug, or salt thereof. Ergothioneine may be advantageously administered in conjunction with lactoferrin.
    Type: Grant
    Filed: June 30, 2022
    Date of Patent: April 16, 2024
    Assignees: COLORADO SEMINARY, OWNER AND OPERATOR OF UNIVERSITY OF DENVER, THE REGENTS OF THE UNIVERSITY OF COLORADO
    Inventors: John Repine, Amani Alhalwani
  • Patent number: 11584751
    Abstract: The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of GLP-1 receptor, a pharmaceutical composition comprising a compound of Formula (I), and a method of treating or preventing a disease in which GLP-1 receptor plays a role.
    Type: Grant
    Filed: November 2, 2021
    Date of Patent: February 21, 2023
    Assignee: Eccogene (Shanghai) Co., Ltd.
    Inventors: Zaifang Ren, Xuefeng Sun, Jingye Zhou, Qing Xu
  • Patent number: 11541035
    Abstract: The present disclosure provides oral pharmaceutical compositions comprising: 1) metronidazole or a pharmaceutically acceptable salt thereof; and magnesium aluminum silicate; or 2) metronidazole or a pharmaceutically acceptable salt thereof; magnesium aluminum silicate; and a flavoring agent. Methods of treating infection utilizing the oral pharmaceutical compositions are also provided.
    Type: Grant
    Filed: January 16, 2019
    Date of Patent: January 3, 2023
    Assignee: Appili Therapeutics Inc.
    Inventors: Bernard J. Guarino, Jr., Jamie L. Doran, Zorana Radovic, Kevin Sullivan
  • Patent number: 11400076
    Abstract: The object of the present invention is to provide a novel pharmaceutical for suppressing cancer stem cells. In the present invention, a mitochondria inhibitor comprising a 2-nitroimidazole derivative is applied to the cancer stem cell as an active ingredient.
    Type: Grant
    Filed: October 2, 2018
    Date of Patent: August 2, 2022
    Assignees: KEIO UNIVERSITY, Sun Pharma Japan Limited
    Inventors: Hideyuki Saya, Oltea Sampetrean, Naoyoshi Koike, Nobuo Kubota
  • Patent number: 11207283
    Abstract: Disclosed are methods, compounds, and compositions for treating infection by an Apicomplexan parasite that include administering a compound that selectively inactivates ornithine aminotransferase of the Apicomplexan parasite. Specifically, the methods, compounds, compounds may be utilized for treating infection by Toxoplasma gondii and toxoplasmosis and for treating infection by Plasmodium falciparum and malaria. The compounds disclosed herein are observed to selectively inactivate Toxoplasma gondii ornithine aminotransferase (TgOAT) relative to human OAT and relative to human ?-aminobutyric aminotransferase (GABA-AT).
    Type: Grant
    Filed: March 31, 2020
    Date of Patent: December 28, 2021
    Assignees: Northwestern University, The University of Chicago
    Inventors: Richard B. Silverman, Hoang V. Le, Rima L. McLeod, Dustin D. Hawker
  • Patent number: 11013710
    Abstract: The present invention discloses herein a synergistic composition(s) of bioactive agents for optimizing cellular health. Particularly, a synergistic bioactive composition for optimizing cellular health, wherein the composition comprising therapeutic blend of betaine of thiol histidine and sirtuin activator(s) or salts thereof present in the ratio of 1:0.5 to 1:90, along with pharmaceutically acceptable excipients. In another embodiment, the invention discloses novel synergistic nutritional composition comprising synergistic combination of bioactives L-ergothioneine and nicotinamide mononucleotide chloride present in the ratio ranges from 1:1 to 1:80. The present invention provides promising and effective nutritional composition for improving cellular health by regulating expression of transcriptional factor, pro-inflammatory cytokines, and reducing cell apoptosis, ROS level and DNA damage in the cell.
    Type: Grant
    Filed: December 5, 2019
    Date of Patent: May 25, 2021
    Assignee: CELAGENEX RESEARCH (INDIA) PVT. LTD.
    Inventors: Dhiraj Dhamane, Rajendra Prasad Tongra
  • Patent number: 10933030
    Abstract: The present invention relates to a composition comprising paeonol of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient for inhibiting angiogenesis, or for enhancing radiosensitization. The present invention also relates to novel use of paeonol of formula (I) or a pharmaceutically acceptable salt thereof for the manufacture of a composition for inhibiting angiogenesis, or for the manufacture of a composition for enhancing radiosensitization. Also, the present invention relates to a method for inhibiting angiogenesis which comprises administrating to a subject in need thereof an effective amount of paeonol of formula (I) or a pharmaceutically acceptable salt thereof, or a method for enhancing radiosensitization which comprises administrating an effective amount of paeonol of formula (I) or pharmaceutically acceptable salts thereof to a subject in need of radiotherapy.
    Type: Grant
    Filed: May 4, 2006
    Date of Patent: March 2, 2021
    Assignee: ANGIOLAB, INC.
    Inventors: Min-Young Kim, Hee-Suk Lee, Ki-Hwan Bae, Yeon-Sook Yun, Jie-Young Song, Young-Soo Han
  • Patent number: 10653672
    Abstract: The invention provides a novel myogenesis promotor, a novel muscle atrophy inhibitor, a novel composition or a novel TAZ activator. The myogenesis promotor, the muscle atrophy inhibitor, the composition and the TAZ activator include a composition represented by the following Formula (I) as an active ingredient. In Formula (I), R1 represents a hydrogen atom or an alkyl group; R2 represents an aryl group, a heterocyclic group, an alkyl group or the like; R3 represents —NR5R6 or —N?C—R7; each of R5 and R6 independently represents a hydrogen atom, an alkyl group or the like; R7 represents —NR10R11, an aryl group or a heterocyclic group; R8 represents a hydrogen atom, an alkyl group or the like; R9 represents a hydrogen atom, an alkyl group or the like; each of R10 and R11 independently represents a hydrogen atom, an alkyl group or the like; R4 represents a cyano group or —C(?O)R12; and R12 represents an aryl group, a heterocyclic group, an alkyl group or the like.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: May 19, 2020
    Assignee: National University Corporation Tokyo Medical and Dental University
    Inventors: Yutaka Hata, Hiroyuki Kagechika, Kentaro Nakagawa, Shigeru Ito
  • Patent number: 10596155
    Abstract: The present disclosure provides mucoadhesive aqueous-based gel formulations of metronidazole useful for a variety of purposes including intravaginal application as a therapeutic approach towards the treatment of individuals suffering from and/or diagnosed with bacterial vaginosis.
    Type: Grant
    Filed: January 14, 2019
    Date of Patent: March 24, 2020
    Assignee: CHEMO RESEARCH, S.L.
    Inventors: Michael T. Nordsiek, Kodumudi S. Balaji
  • Patent number: 10487072
    Abstract: The present invention relates to a novel imidazole compound or a pharmaceutically acceptable salt thereof having a melanocortin receptor agonistic activity, and medical use thereof. The present invention relates to an imidazole compound represented by general formula [I] [wherein: Ring A represents an optionally substituted aryl group or the like; R1 represents a hydrogen atom, an optionally substituted alkyl group, or the like; R2 represents a hydrogen atom, a halogen atom, or the like; and R3 represents an optionally substituted alkyl group] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 25, 2016
    Date of Patent: November 26, 2019
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Atsushi Sato, Ritsuo Imashiro, Hidekazu Tsujishima, Kouichi Tanimoto, Yasuo Yamamoto, Tetsu Nakane, Chihiro Toshikawa
  • Patent number: 10045965
    Abstract: Disclosed are gel compositions suitable for the topical administration of an active compound having poor solubility and skin penetration, for example, of a COX-2 inhibitor compounds, processes of preparation thereof and methods of use thereof for the treatment of indications treatable by the active compound.
    Type: Grant
    Filed: April 9, 2015
    Date of Patent: August 14, 2018
    Assignee: EGIS Pharmaceuticals PLC
    Inventors: Endre Mikulásik, Tamás Spaits, Ágota Szakályné Sinka
  • Patent number: 9830554
    Abstract: Audio sensors collaborate for geo-location and tracking of multiple users. Different users can be independently geo-located and tracked within the AI environment. Location is determined from two or more AI clients of known locations that detect an event such as a human voice command to connect a call with a specific user. Responsive to classification of the event in view of the estimated location, a command for an AI action, such as connecting a call between users, is received for a response to the event at the AI clients that detected the event, or others.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: November 28, 2017
    Assignee: Lumin, LLC
    Inventors: Nima Lahijani Shams, Suhas Maheshaiah
  • Patent number: 9818061
    Abstract: Audio sensors collaborate for geo-location and tracking of multiple users. Different users can be independently geo-located and tracked within the AI environment. Location is determined from two or more AI clients of known locations that detect an event such as a human voice command to connect a call with a specific user. Responsive to classification of the event in view of the estimated location, a command for an AI action, such as connecting a call between users, is received for a response to the event at the AI clients that detected the event, or others.
    Type: Grant
    Filed: September 15, 2016
    Date of Patent: November 14, 2017
    Assignee: Lumin, LLC
    Inventors: Nima Lahijani Shams, Suhas Maheshaiah
  • Patent number: 9710753
    Abstract: An artificial intelligence (AI) system leverages collaboration of multiple audio sensors for geo-location of an event. Location information is stored for each of the plurality of geographically-dispersed AI clients. Each of the AI clients can include an audio sensor, a network controller, and a feedback mechanism (e.g., a speaker or an LED) within a common enclosure. Responsive to detection of an event (e.g., involving a human, machine, or ambient condition) at two or more of the plurality of geographically-dispersed AI clients, audio event data is centrally received from audio sensors of the two or more of the plurality of geographically-dispersed AI sensors. A location is estimated based on the location information and the audio event data. Responsive to classification of the event in view of the estimated location, a command is received for a response to the event at the AI clients that detected the event, or others.
    Type: Grant
    Filed: October 22, 2014
    Date of Patent: July 18, 2017
    Assignee: Lumin, LLC
    Inventors: Nima Lahijani Shams, Vinay Venkatesh Malekal, Narges Banou Nourshahi
  • Patent number: 9649298
    Abstract: The present invention provides a substance comprising a preparation of at least one chemotherapeutic or cytotoxic substance for the use in treatment of a disease of a mammalian patient, especially in the treatment of cancer. The invention suggests a symbiotic or synergistic combination of radiotherapy and chemotherapeutic or cytotoxic drug delivery.
    Type: Grant
    Filed: June 4, 2014
    Date of Patent: May 16, 2017
    Assignees: Fumedica AG, Universität Bern
    Inventors: Valentin Djonov, Beat Steger
  • Patent number: 9511053
    Abstract: Therapeutic compositions capable of removing excess nitric oxide are provided. The therapeutic compositions include nitronyl nitroxide monoradicals, B12 derivatives, flavonoid derivatives, the like and combinations thereof. The therapeutic compositions can be utilized in a number of suitable applications, such as to prevent or treat intradialytic hypotension during dialysis.
    Type: Grant
    Filed: December 30, 2015
    Date of Patent: December 6, 2016
    Assignees: Baxter International Inc., Baxter Healthcare S.A.
    Inventors: Sujatha Karoor, Ton That Hai, Cong Jiang, Paul Sanders, Cliff Holmes
  • Patent number: 9481652
    Abstract: The present invention provides a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, which comprises the solid preparation and an environment-controlling agent packaged together. The packaged product of present invention is useful as a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, with which discoloration of the solid preparation is suppressed, and superior storage stability of the solid preparation is obtained.
    Type: Grant
    Filed: June 24, 2015
    Date of Patent: November 1, 2016
    Assignee: FUJIFILM Corporation
    Inventor: Shumma Nakano
  • Patent number: 9433680
    Abstract: The present invention relates to improved topical gel compositions comprising an active agent, and uses thereof.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: September 6, 2016
    Assignee: MERZ PHARMACEUTICALS, LLC
    Inventors: Bhushan Hardas, Donna Dalton, Petra Scheppler, Anja Hensche, Peter Boderke
  • Patent number: 9388141
    Abstract: The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: July 12, 2016
    Assignees: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: Andreas Haupt, Jürgen Dinges, Liliane Unger, Karsten Wicke, Robert Van Waterschoot, Karla Drescher, Ana Relo
  • Patent number: 9273008
    Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, 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: Grant
    Filed: March 19, 2015
    Date of Patent: March 1, 2016
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell, Brooke Olson
  • Patent number: 9249105
    Abstract: The invention provides crystalline salt forms of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: February 2, 2016
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Paul R. Fatheree, Venkat R. Thalladi
  • Publication number: 20150148393
    Abstract: The invention relates to a cosmetic and/or pharmaceutical composition in combination with suitable carriers for topical use, comprising a mixture consisting of methyl sulfonyl methane and at least one compound belonging to the class of 4-alkyl cyclohexanols, which is useful in the treatment of various inflammatory conditions such as rosacea. The composition can act to simultaneously hinder both the release of chemical mediators which are up-regulated in rosacea and their action of causing the activation of TRPV receptors. The composition can reduce the effect of ultraviolet radiations on a skin already affected by an inflammatory process, and particularly, it can reduce the erythema induced by ultraviolet radiations on a skin already affected by an inflammatory process.
    Type: Application
    Filed: June 4, 2013
    Publication date: May 28, 2015
    Applicant: GENERAL TOPICS S.R.L.
    Inventor: Gianfranco De Paoli Ambrosi
  • Publication number: 20150141476
    Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, rosacea.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 21, 2015
    Inventors: Pedro Cuevas Sànchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Gorman, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
  • Publication number: 20150133366
    Abstract: C. difficile infection (CDI) is the most common cause of antibiotic-associated diarrhea. Unfortunately, antibiotic therapy remains as the standard treatment for this antibiotic-induced disease and relapses are common. Antibiotic treatment typically is given for 10 to 14 days for initial or second episode of CDI. For recurrent episodes, more prolonged courses are recommended. It is disclosed herein that lower dose or shorter course of the antimicrobial treatment is sufficient to treat the disease and prevent recurrent disease by enabling a good immunologic response to infection, and perhaps also by better preserving normal flora, thus protecting against relapses or reinfection.
    Type: Application
    Filed: November 12, 2014
    Publication date: May 14, 2015
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Richard L. Guerrant, Cirle Alcantara Warren, John Hudson Moore, II, Edward van Opstal
  • Publication number: 20150133471
    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: Application
    Filed: September 15, 2014
    Publication date: May 14, 2015
    Inventors: Gabor Csjernyik, Sofia Karlstrom, Annika Kers, Karin Kolmodin, Martin Nylof, Liselotte Ohberg, Laszlo Rakos, Lars Sandberg, Fernando Sehgelmeble, Peter Soderman, Britt-Marie Swahn, Stefan Von Berg
  • Publication number: 20150133518
    Abstract: The invention provides crystalline salt forms of 4?-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3?-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension.
    Type: Application
    Filed: June 27, 2014
    Publication date: May 14, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Venkat R. Thalladi
  • Patent number: 9012485
    Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, 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: Grant
    Filed: January 9, 2014
    Date of Patent: April 21, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell, Brooke Olson
  • Patent number: 9005643
    Abstract: Disclosure is provided for imidazole-phenyl derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: April 14, 2015
    Assignee: North Carolina State University
    Inventors: Christian Melander, Justin J. Richards, Cynthia Bunders
  • Publication number: 20150093435
    Abstract: Compositions, and methods of use thereof, are provided for the treatment of painful neuropathy by local or topical delivery of compounds that interact with ?-adrenergic receptors, especially an alpha2 adrenergic agonist such as clonidine, to the entire painful area such that the need for systemic dosing is minimized. The compounds are delivered to or adjacent to painful areas in patients with painful length dependent neuropathy, and other neuropathies that affect the pain signaling fibers in the skin. A preferred compound for the treatment of patients with length dependent neuropathy is clonidine applied in a transdermal patch, gel, ointment, lotion, liposomal formulation, cream, or emulsion, wherein the concentration is sufficient to provide an effective dose in the painful area or immediately adjacent areas.
    Type: Application
    Filed: December 9, 2014
    Publication date: April 2, 2015
    Inventor: James N. Campbell
  • Publication number: 20150093338
    Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.
    Type: Application
    Filed: October 8, 2014
    Publication date: April 2, 2015
    Inventor: Michael Farber
  • Patent number: 8993584
    Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as procymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: March 31, 2015
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Koji Sugimoto, Hiroyuki Hayashi
  • Publication number: 20150079116
    Abstract: NK cell licensing predisposes patients to chronic inflammatory disease. Methods and kits to diagnose and treat chronic inflammatory disease based on genetic haplotype and cytokine profile are described herein.
    Type: Application
    Filed: April 11, 2013
    Publication date: March 19, 2015
    Inventors: Jonathan Braun, Lin Lin
  • Patent number: 8980920
    Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: March 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Patent number: 8980932
    Abstract: The present invention concerns novel carbonic anhydrase IX inhibitors comprising a nitroimidazole moiety and their use in therapy of hypoxic conditions, in particular cancer treatment, especially chemotherapy and radiotherapy. The compounds of the invention have an increased specificity for the carbonic anhydrase IX enzyme compared to the art. The present invention relates to novel nitroimidazole derivates represented by formula (1).
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: March 17, 2015
    Assignees: Stichting Maastricht Radiation Oncology “Maastro-Clinic”, Université Montpellier 2 Sciences et Techniques
    Inventors: Philippe Lambin, Jean-Yves Winum, Claudiu Supuran
  • Patent number: 8975411
    Abstract: An object of the present invention is to provide a pharmaceutical agent useful for treating and preventing neurological disease, having satisfactory solubility and oxidative stress-mediated cell death suppressive activity as well as capable of exhibiting excellent blood-brain barrier permeability. The present invention is directed to an acylaminoimidazole derivative represented by general formula (I) or a salt thereof, and a pharmaceutical and a therapeutic or preventive agent for neurological disease containing the same, as an active ingredient.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: March 10, 2015
    Assignees: Neugen Pharma Inc., Wakunaga Pharmaceutical Co., Ltd.
    Inventors: Joh-E Ikeda, Noriaki Hirayama, Satoshi Inoue, Kazunori Tanaka, Takuya Kanno
  • Publication number: 20150065543
    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: October 23, 2014
    Publication date: March 5, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
  • Patent number: 8962668
    Abstract: Compositions, and methods of use thereof, are provided for the treatment of painful neuropathy by local or topical delivery of compounds that interact with ?-adrenergic receptors, especially an alpha2 adrenergic agonist such as clonidine, to the entire painful area such that the need for systemic dosing is minimized. The compounds are delivered to or adjacent to painful areas in patients with painful length dependent neuropathy, and other neuropathies that affect the pain signaling fibers in the skin. A preferred compound for the treatment of patients with length dependent neuropathy is clonidine applied in a transdermal patch, gel, ointment, lotion, liposomal formulation, cream, or emulsion, wherein the concentration is sufficient to provide an effective dose in the painful area or immediately adjacent areas.
    Type: Grant
    Filed: February 21, 2011
    Date of Patent: February 24, 2015
    Assignee: Arcion Therapeutics, Inc.
    Inventor: James N. Campbell
  • Patent number: 8946275
    Abstract: Cancer can be treated by administration of a hypoxia-activated prodrug, such as TH-302, alone or in combination with other anticancer agents and/or radiation therapy. In combination therapy, the hypoxia-activated prodrug and another anti-cancer agent or radiation therapy may be administered within the same 24-hour period, and administration of the hypoxia-activated prodrug may be completed prior to beginning administration of the other anticancer agent or radiation therapy.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: February 3, 2015
    Assignee: Threshold Pharmaceuticals, Inc.
    Inventors: Stewart Kroll, Mark Matteucci, Charles P. Hart, Jian-Xin Duan, Karen Curd
  • Patent number: 8946276
    Abstract: The present disclosure provides mucoadhesive aqueous-based gel formulations of metronidazole useful for a variety of purposes, including intravaginal application as a therapeutic approach towards the treatment of individuals suffering from and/or diagnosed with bacterial vaginosis.
    Type: Grant
    Filed: June 28, 2012
    Date of Patent: February 3, 2015
    Assignee: Watson Laboratories, Inc.
    Inventors: Michael T. Nordsiek, Kodumudi S. Balaji
  • Publication number: 20150023955
    Abstract: The present invention discloses novel agents and methods for diagnosis and treatment of melanoma. Also disclosed are related arrays, kits, and screening methods.
    Type: Application
    Filed: September 15, 2014
    Publication date: January 22, 2015
    Applicant: THE ROCKEFELLER UNIVERSITY
    Inventors: Sohail Tavazoie, Nora Pencheva
  • Publication number: 20150025094
    Abstract: The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of —S—, —S—S—, —S—(CH2)n—, —NH—, —NH—(CH2)n—, —O—, —S02-, arylene, heteroarylene; R1 is selected from the group consisting of straight or branched C4-C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5-C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or heteroaromatic ring, each optionally substituted with at least one group selected from —COOH, —NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 carboxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, hal
    Type: Application
    Filed: August 1, 2012
    Publication date: January 22, 2015
    Applicants: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD., DIAB R&d 1, BAR-IIan University
    Inventors: Shlomo Sasson, Erol Cerasi, Arie Lev Gruzman, Ella Meltzer-Mats
  • Patent number: 8933245
    Abstract: Compositions comprising ergothioneine and a trimethylamine absorber are provided. Also provided are methods for preventing, reducing or minimizing the fishy, amine odor, due to trimethylamine, that is associated with the processing and/or storage of a preparation containing ergothioneine, by combining with the ergothioneine, during processing or prior to storage, a trimethylamine absorber in an amount sufficient to prevent the detection of any trimethylamine odor by the human nose. A method is further provided for ameliorating the methylamine odor associated with an aqueous ergothioneine-containing preparation after it has developed a fishy trimethylamine odor.
    Type: Grant
    Filed: November 8, 2012
    Date of Patent: January 13, 2015
    Assignee: ELC Management LLC
    Inventor: Daniel B. Yarosh
  • Patent number: 8921406
    Abstract: The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.
    Type: Grant
    Filed: August 21, 2006
    Date of Patent: December 30, 2014
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Andreas Haupt, Francisco Javier Garcia-Ladona, Alfred Hahn
  • Publication number: 20140378466
    Abstract: This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Applicant: ARDEA BIOSCIENCES
    Inventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoul, Zhi Hong
  • Publication number: 20140378520
    Abstract: The invention provides (among other things) small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer.
    Type: Application
    Filed: September 4, 2014
    Publication date: December 25, 2014
    Inventors: Zhongxu Ren, Jennifer Riggs-Sauthier, Michael D. Bentley
  • Patent number: 8912225
    Abstract: The present invention provides methods for inhibiting VEGF production or secretion in a subject comprising administering to the subject an effective amount of a compound of Formula I. The invention also provides methods for the treatment or prevention of conditions associated with abnormal levels of VEGF production or secretion.
    Type: Grant
    Filed: August 31, 2005
    Date of Patent: December 16, 2014
    Assignee: Pitney Pharmaceuticals Pty Limited
    Inventors: David L. Morris, Mohammad H. Pourgholami
  • Publication number: 20140364474
    Abstract: Disclosure is provided for 1,4,5-substituted amino imidazole compounds useful to control microbial growth, compositions including these compounds, devices including these compounds, and methods of using the same.
    Type: Application
    Filed: August 21, 2014
    Publication date: December 11, 2014
    Inventors: Christian Melander, Zhaoming Su, Lingling Peng
  • Publication number: 20140363479
    Abstract: There is disclosed herein a composition for treating extracellular parasitic infections, the composition comprising one or more of the following combinations: at least one quinolone or fluoroquinolone together with at least one tetracycline, iodoquinol, an azole or imidazole; or at least two agents selected from the group consisting of iodoquinol, thiazolidones, tetracycline, nitroimidazoles, cotrimoxazole and diloxanide furoate.
    Type: Application
    Filed: August 21, 2014
    Publication date: December 11, 2014
    Inventors: Thomas Julius BORODY, Soledad CARSULA
  • Patent number: 8889672
    Abstract: The invention provides a method of inhibiting atypical protein kinase C (aPKC) comprising contacting an aPKC with a compound having a structure selected from the group consisting of structural formulas (I) to (IX). The invention further provides a method of inhibiting or reducing vascular permeability. The method comprising administering to a subject a composition comprising an amount of a compound having a structure selected from the group consisting of structural formulas (I) to (IX) effective to inhibit or reduce vascular permeability. A method of treating or preventing a disease or disorder characterized by abnormal vascular permeability, a method of inhibiting angiogenesis, a method of inhibiting cancer cell proliferation, a formulation, and a method of preparing a formulation also are provided.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: November 18, 2014
    Assignees: The Regents of The University of Michigan, The Penn State Research Foundation
    Inventors: David A. Antonetti, Paul Titchenell