1,3-thiazoles (including Hydrogenated) Patents (Class 514/365)
  • Patent number: 10315998
    Abstract: The present invention belongs to the field of fungicides, and relates to an amide compound and the preparation method and use thereof. The amide compound is as shown in general formula I: Each substituent in Formula I is defined in the description. The compound of general formula I of the present invention has an outstanding fungicidal activity, and can be used for controlling fungal diseases.
    Type: Grant
    Filed: May 4, 2016
    Date of Patent: June 11, 2019
    Assignee: SHENYANG SINOCHEM AGROCHEMICALS R&D CO., LTD.
    Inventors: Liang Lv, Gang Wang, Zhonggang Shan, Jiyong Liu, Qin Sun, Junfeng Wang, Bin Li
  • Patent number: 10272055
    Abstract: Biguanide compounds and salts thereof are disclosed. Also disclosed are pharmaceutical compositions and therapeutic methods for treating certain diseases including cancer such as breast cancer.
    Type: Grant
    Filed: March 6, 2015
    Date of Patent: April 30, 2019
    Assignees: Regents of the University of Minnesota, The Regents of the University of California
    Inventors: David A. Potter, Zhijun Guo, Elizabeth Amin, Gunda Georg, Tom Poulos, Irina Sevrioukova
  • Patent number: 10245251
    Abstract: The present invention relates to a pharmaceutical combination for use in the treatment of squamous cell carcinoma, comprising a CDK inhibitor selected from the compounds of formula (I); or a pharmaceutically acceptable salt thereof and one or more antineoplastic agents selected from sorafenib, lapatinib, erlotinib, cisplatin, 5-fluorouracil, docetaxel or cetuximab or a pharmaceutically acceptable salt thereof. The said pharmaceutical combination exhibits synergy when used in the treatment of squamous cell carcinoma of head and neck (SCCHN). The invention also relates to a pharmaceutical composition comprising the said combination and a method for the treatment of squamous cell carcinoma of head and neck (SCCHN), using a therapeutically effective amount of said combination.
    Type: Grant
    Filed: July 8, 2016
    Date of Patent: April 2, 2019
    Assignee: PIRAMAL ENTERPRISES LIMITED
    Inventors: Veena Agarwal, Arun Balakrishnan, Giridharan Periyasamy
  • Patent number: 10221169
    Abstract: Disclosed ore substituted aminothiazoles, which can be used for, among other things, the treatment of tuberculosis, pharmaceutical compositions containing the same, and methods of using the same.
    Type: Grant
    Filed: March 23, 2017
    Date of Patent: March 5, 2019
    Assignees: The Broad Institute, Inc., The General Hospital Corporation, The Brigham and Women's Hospital, Inc.
    Inventors: Deborah Hung, Michael Serrano-Wu, Sarah Grant, Tomohiko Kawate
  • Patent number: 10195182
    Abstract: A method of cancer intervention or eradication by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its analogs (the active ingredient) to a subject with cancer is disclosed. An effective dose and dosing frequency of the active ingredient are determined by measuring its blood levels of the subject after dosing. The active ingredient formulated with a carrier system is applied topically, enterally, or parenterally to the subject. The formulated drug can also be administered together with one or more of other cancer therapeutic agents. A maintenance dosing is provided after the subject is free of cancer to insure the cancer eradication. Subjects with cancers of prostate, liver, lung, ovarian, and breast are preferably accepted for treatment.
    Type: Grant
    Filed: June 5, 2017
    Date of Patent: February 5, 2019
    Assignee: Ariagen, Inc.
    Inventor: Jiasheng Song
  • Patent number: 10188639
    Abstract: The invention provides enantiopure deuterium-enriched pioglitazone, pharmaceutical compositions, and methods of treating neurological disorders, cancer, respiratory disorders, metabolic disorders, and other disorders using enantiopure deuterium-enriched pioglitazone. A preferred aspect of the invention provides methods of treating Alzheimer's disease, non-small cell lung cancer, hepatocellular carcinoma, and chronic obstructive pulmonary disease using enantiopure deuterium-enriched pioglitazone.
    Type: Grant
    Filed: January 15, 2015
    Date of Patent: January 29, 2019
    Assignee: DeuteRx, LLC
    Inventors: Sheila DeWitt, Vincent Jacques, Leonardus H. T. van der Ploeg
  • Patent number: 10179780
    Abstract: There are provided: 4-methyl-2-[4-(2-methylpropoxy)-3-(1H-1,2,3,4-tetrazol-1-yl)phenyl]-1,3-thiazole-5-carboxylic acid, a sodium salt thereof and crystals of these, useful as a therapeutic agent and a prophylactic agent for gout, hyperuricemia and the like, and a method for producing the same.
    Type: Grant
    Filed: July 29, 2015
    Date of Patent: January 15, 2019
    Assignee: Teijin Pharma Limited
    Inventors: Asahi Kawana, Hisae Nozato, Chikashi Kanazawa
  • Patent number: 10138216
    Abstract: Described herein are analogues of 2-methyl-3-(2-ethynylthiazol-4-yl)cyclopent-2-enol and the corresponding ketone 3-(2-ethynylthiazol-4-yl)-2-methylcyclopent-2-enone, the analogues having terminal alkyne groups at the 2-position of the thiazole ring. These drug-like molecules, referred to as CETZOLE compounds, are useful to treat non-small cell lung cancer and other forms of cancer. Methods of making and using the compounds, methods of treating various diseases, pharmaceutical compositions, and kits are also disclosed.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: November 27, 2018
    Assignee: The University of Toledo
    Inventors: Viranga Tillekeratne, William Taylor, Sara Fedorka
  • Patent number: 10117877
    Abstract: Disclosed herein are methods, compounds, and compositions for fat reduction, and in particular fat reduction without significant hair growth and/or additional hair growth.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: November 6, 2018
    Assignee: ALLERGAN, INC.
    Inventors: Neil J. Poloso, Jenny Wang, David F. Woodward, Robert M. Burk
  • Patent number: 10092617
    Abstract: The present invention relates to the field of nanotechnology, in particular, to the production of biodegradable polymeric nanoparticles. The present invention provides a biodegradable polymeric nanoparticle made up of a block copolymer and a process for producing the same. The nanoparticles are produced without the use of any emulsifiers and have a size ranging from 30-120 nm. The methods of controlling the drug loading capacity are disclosed along with the process of producing entity-loaded nanoparticles. Compositions comprising the nanoparticles and their use in therapeutics, diagnostics and theranostics are also disclosed.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: October 9, 2018
    Assignee: NANOPROTEAGEN
    Inventor: Harpal Singh
  • Patent number: 10073072
    Abstract: This disclosure describes the results of the studies conducted to develop a dissolution method to monitor release profiles of hydrophobic active pharmaceutical ingredients such as ivermectin with or without pyrantel pamoate from a drug product made of complex matrix that includes, but is not limited to beef, tallow, corn cob and soy protein.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: September 11, 2018
    Assignee: MERIAL INC.
    Inventors: Abu M. Rustum, Satish Kumar, Andrew L. McAdoo
  • Patent number: 10065950
    Abstract: [Problem] Provided is a novel 1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, or a solvate thereof, which is useful as an anti-HIV agent. [Solving Means] The present invention provides a compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: September 4, 2018
    Assignee: Japan Tobacco Inc.
    Inventors: Susumu Miyazaki, Yuki Bessho, Kaoru Adachi, Seiji Kawashita, Hirotaka Isoshima, Kengo Oshita, Shunichi Fukuda
  • Patent number: 10043292
    Abstract: A computer-controlled system determines attributes of a frexel, which is an area of human skin, and applies a reflectance modifying agent (RMA) at the pixel level to automatically change the appearance of human features based on one or more digital images. The change may be based on a digital image of the same frexel, for as seen in a prior digital photograph captured previously by the computer-controlled system. The system scans the frexel and uses feature recognition software to compare the person's current features in the frexel with that person's features in the digital image. It then calculates enhancements to the make the current features appear more like the features in the digital image, and it applies the RMA to the frexel to accomplish the enhancements. Or the change may be based on a digital image of another person, through the application of RMAs.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: August 7, 2018
    Assignee: TCMS Transparent Beauty LLC
    Inventors: Albert D. Edgar, David C. Iglehart, Rick B. Yeager
  • Patent number: 10028508
    Abstract: The invention is in the technical field of vector control as well as insecticide-resistant mosquito and bed bug control. The active compound compositions of this invention are used against mosquitos and bed bugs which transmit disease pathogens or which annoy the well-being of humans and animals. The active compound compositions of this invention are in particular useful to overcome target-specific and/or metabolic-specific resistance of mosquitos and bed bugs and are biologically efficient on a variety of surfaces over an extended period of time.
    Type: Grant
    Filed: June 19, 2015
    Date of Patent: July 24, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Karin Horn, Rainer Sonneck, Arnoldus Vermeer, Sebastian Horstmann, Guenther Nentwig, Frederic Schmitt
  • Patent number: 10010535
    Abstract: Iron overload is associated with pathological conditions such as oxidative stress, transfusional iron overload, thalassemia, primary hemochromatosis, secondary hemochromatosis, diabetes, liver disease, heart disease, cancer, radiation injury, neurological or neurodegenerative disorder, Friedreich's ataxia (FRDA), macular degeneration, closed head injury, irritable bowel disease, and reperfusion injury. The present invention provides methods and pharmaceutical compositions using desferrithiocin analogs of Formulae (A) and (J) for treating and/or preventing these pathological conditions, metal (e.g., iron, aluminum, a lanthanide, or an actinide (e.g., uranium)) overload conditions, and infectious diseases (e.g., malaria).
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: July 3, 2018
    Assignee: University of Florida Research Foundation, Incorporated
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 10000474
    Abstract: Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of cancer. Additionally, provided is a method for treating cancer, comprising the step of administering a therapeutically effective amount of a compound according to formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier to a patient in need thereof.
    Type: Grant
    Filed: November 6, 2015
    Date of Patent: June 19, 2018
    Assignee: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Patrick M. Woster, Youxuan Li
  • Patent number: 9918958
    Abstract: The invention provides a method for treating hypoxia in a normal subject, comprising administering 5-HMF to the subject.
    Type: Grant
    Filed: July 12, 2012
    Date of Patent: March 20, 2018
    Inventor: Warren Stern
  • Patent number: 9914712
    Abstract: Compounds of general formula (I): wherein R1, R11, Y, R2, n and A are as defined herein are useful as inhibitors or metallo-?-lactamase (MBL) enzymes and can be used for reducing or removing antibiotic resistance in bacteria.
    Type: Grant
    Filed: June 12, 2014
    Date of Patent: March 13, 2018
    Assignee: ANTABIO SAS
    Inventors: Marc Lemonnier, David Davies, Thomas David Pallin
  • Patent number: 9878970
    Abstract: The present invention relates to a novel a process for the preparation of 9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-ylamine which process comprises a) reacting cyclopentadiene in the presence of a radical initiator and CXCl3, wherein X is chloro or bromo, to a compound of formula I1, or aa) reacting cyclopentadiene with CXCl3, wherein X is chloro, in the presence of a metal catalyst to a compound of formula I1, wherein X is chloro, b) reacting the compound of formula I1 with a base in the presence of an appropriate solvent to the compound of formula III, c) and converting the compound of formula III in the presence of 1,2-dehydro-6-nitrobenzene to the compound of formula IV, and d) hydrogenating the compound of formula IV in the presence of a metal catalyst.
    Type: Grant
    Filed: September 27, 2017
    Date of Patent: January 30, 2018
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Denis Gribkov, Bjorn Antelmann, Fanny Bois, Harald Walter, Alain De Mesmaeker
  • Patent number: 9849147
    Abstract: The present invention relates to a fast dissolving tablet comprising a therapeutically effective amount of a phosphate binding polymer, such as sevelamer or pharmaceutically acceptable salt or derivative thereof, that exhibit limited swelling in the oral cavity, has pleasant taste and mouth feel, high phosphate binding capacity with fast binding kinetics and require limited amount of water intake. A process for the preparation thereof is disclosed.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: December 26, 2017
    Assignee: PHARMATHEN S.A.
    Inventors: Evangelos Karavas, Efthimios Koutris, Vasiliki Samara, Analia Diakidou, Georgia Papanikolaou, Panagiotis Mparmpalexis
  • Patent number: 9815826
    Abstract: There are provided crystals of 2-[4-(2,2-dimethylpropoxy)-3-(1H-1,2,3,4-tetrazol-1-yl)phenyl]-4-methyl-1,3-thiazole-5-carboxylic acid which is useful as a therapeutic agent or prophylactic agent for gout, hyperuricemia and the like.
    Type: Grant
    Filed: July 29, 2015
    Date of Patent: November 14, 2017
    Assignee: Teijin Pharma Limited
    Inventors: Asahi Kawana, Yuki Miyazawa
  • Patent number: 9795615
    Abstract: Disclosed herein are methods, compounds, and compositions for fat reduction, and in particular fat reduction without significant hair growth and/or additional hair growth.
    Type: Grant
    Filed: April 29, 2016
    Date of Patent: October 24, 2017
    Assignee: ALLERGAN, INC.
    Inventors: Neil J. Poloso, Jenny Wang, David F. Woodward, Robert M. Burk
  • Patent number: 9694000
    Abstract: A method of cancer intervention or eradication by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its analogs (the active ingredient) to a subject with cancer is disclosed. An effective dose and dosing frequency of the active ingredient are determined by measuring its blood levels of the subject after dosing. The active ingredient formulated with a carrier system is applied topically, enterally, or parenterally to the subject. The formulated drug can also be administered together with one or more of other cancer therapeutic agents. A maintenance dosing is provided after the subject is free of cancer to insure the cancer eradication. Subjects with cancers of prostate, liver, lung, ovarian, and breast are preferably accepted for treatment.
    Type: Grant
    Filed: December 7, 2015
    Date of Patent: July 4, 2017
    Assignee: AHR PHARMACEUTICALS, INC.
    Inventor: Jiasheng Song
  • Patent number: 9682037
    Abstract: Orally disintegrating film dosage forms for delivering active pharmaceutical agents, methods of formulating the dosage forms to retard absorption through the oral mucosa, and methods of using the dosage forms for the treatment of various medical conditions are provided.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: June 20, 2017
    Assignee: APR APPLIED PHARMA RESEARCH SA
    Inventors: Christian Leichs, Armin Breitenbach, Ingo Lehrke, Paolo Galfetti
  • Patent number: 9567309
    Abstract: Compounds represented by structural formulas described herein, such as Structural Formula (I): or a pharmaceutically acceptable salt thereof are useful in treating conditions such as metal overload, oxidative stress, and neoplastic and preneoplastic conditions.
    Type: Grant
    Filed: July 28, 2015
    Date of Patent: February 14, 2017
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 9556169
    Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: January 31, 2017
    Assignee: Novartis AG
    Inventors: Arnab Kumar Chatterjee, Advait Suresh Nagle, Prasuna Paraselli, Ravinder Reddy Kondreddi, Seh Yong Leong, Pranab Kumar Mishra, Robert Joseph Moreau, Jason Thomas Roland, Wei Lin Sandra Sim, Oliver Simon, Jocelyn Liying Tan, Bryan K S Yeung, Bin Zou, Venkatataiah Bollu
  • Patent number: 9518048
    Abstract: A process for the preparation of teneligliptin.
    Type: Grant
    Filed: August 28, 2013
    Date of Patent: December 13, 2016
    Assignee: Glenmark Pharmaceuticals Limited
    Inventors: Suresh Mahadev Kadam, Bipin Parsottam Kansagra, Ramchandran Vishnue Kale, Jayant Prakashrao Patil, Venkataramana Reddy Yemireddy, Shailendra Nilkanth Bhadane, Uddhav Popat Chaudhar, Ulhas Digambar Patil, Shekhar Bhaskar Bhirud
  • Patent number: 9498537
    Abstract: A method of improving the efficacy of a blood transfusion into a subject is provided comprising administering a composition comprising an EAF PEGylated-blood protein into the subject, prior to, during, or subsequent to the blood transfusion.
    Type: Grant
    Filed: August 7, 2014
    Date of Patent: November 22, 2016
    Assignees: Albert Einstein College of Medicine, Inc., The Regents of the University of California
    Inventors: Seetharama A. Acharya, Marcos Intaglietta
  • Patent number: 9479586
    Abstract: A distributed system for storing digital data is disclosed. The distributed system includes a portable storage device suitable for being connected to a terminal, at least one storage server and a dispatching server. The dispatching server is suitable for retrieving accessibility information indicating that the at least one storage server is accessible by the portable storage device. The portable storage device is suitable for, when connected to the terminal, sending identification information to the dispatching server. The dispatching server is suitable for, upon reception of the identification information, using the identification information for retrieving the accessibility information and for sending the accessibility information to the portable storage device.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: October 25, 2016
    Assignee: Telecom Italia S.p.A.
    Inventors: Pino Castrogiovanni, Giovanni Malnati, Giovanni Martini
  • Patent number: 9447049
    Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: September 20, 2016
    Assignee: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION
    Inventors: Wei Li, Min Xiao, James Dalton, Sunjoo Ahn, Duane D. Miller, Jianjuan Chen, Jin Wang
  • Patent number: 9388235
    Abstract: The use of a therapeutic capable of inhibiting complement, e.g., an anti-C5 antibody, to treat antibody mediated neuropathies is disclosed.
    Type: Grant
    Filed: September 5, 2007
    Date of Patent: July 12, 2016
    Assignee: Alexion Pharmaceuticals, Inc.
    Inventors: Susan Halstead, Hugh Willison, Russell P. Rother
  • Patent number: 9326955
    Abstract: Methods and combination pharmaceuticals for treating bronchospastic medical conditions by utilizing the electrophysiology of proteinacious channels in lipid membranes of mammalian cells. The combination pharmaceuticals include at least one ?-adrenergic receptor agonist, and at least one composition adapted to effect the electrophysiology of Kv7 potassium channels of a lipid membrane of an airway smooth muscle cell. The pharmaceutical may be administered to a living body in a therapeutic amount sufficient to activate the Kv7 potassium channels of an airway smooth muscle cell.
    Type: Grant
    Filed: February 7, 2014
    Date of Patent: May 3, 2016
    Assignee: Loyola University Chicago
    Inventor: Kenneth L. Byron
  • Patent number: 9309237
    Abstract: Chemical compounds that inhibit retroviruses are presented herein. More particularly, this disclosure provides small molecule compounds that inhibit infection with, or treat infection caused by, human immunodeficiency viruses.
    Type: Grant
    Filed: September 6, 2012
    Date of Patent: April 12, 2016
    Assignees: NEW YORK BLOOD CENTER, INC., THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
    Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
  • Patent number: 9295708
    Abstract: This disclosure features modified release pharmaceutical formulations (e.g., extended release pharmaceutical formulations; e.g., solid dosage forms, e.g., tablets) that are useful for the oral administration of oprozomib, or a pharmaceutically acceptable salt thereof, to a human or animal subject as well as methods of making and using the formulations.
    Type: Grant
    Filed: October 24, 2013
    Date of Patent: March 29, 2016
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Mouhannad Jumaa, Tony Muchamuel, Naveen Bejugam, Hansen Wong, Christopher J. Kirk, Rahul Vishram Manek, Sanjeev Sharma
  • Patent number: 9290484
    Abstract: Nitric oxide biosynthesis-inhibiting anti-inflammatory and anti-microbial compounds of Formula (3) and Formula (4) wherein R1 and R2 are independently selected from optionally substituted thienyl, optionally substituted furyl, optionally substituted —CH?CH-thienyl and optionally substituted —CH?CH-furyl, provided that R2 is substituted with as nitro group Treatment methods utilizing the compounds, and methods of synthesis of the compounds are also disclosed.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: March 22, 2016
    Assignees: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY, LEHIGH UNIVERSITY
    Inventors: Jeffrey D. Laskin, Diane E. Heck, Geraldine Guillon, Thomas Finetti, Angela Hunter, Christophe Guillon, Robert D. Rapp, Anna M. Vetrano, Ned D. Heindel
  • Patent number: 9238645
    Abstract: A method of cancer intervention or eradication by administering an effective amount of an endogenous ligand for the aryl hydrocarbon (Ah) receptor (AhR) named ITE or one of its analogs (the active ingredient) to a subject with cancer is disclosed. An effective dose and dosing frequency of the active ingredient are determined by measuring its blood levels of the subject after dosing. The active ingredient formulated with a carrier system is applied topically, enterally, or parenterally to the subject. The formulated drug can also be administered together with one or more of other cancer therapeutic agents. A maintenance dosing is provided after the subject is free of cancer to insure the cancer eradication. Subjects with cancers of prostate, liver, lung, ovarian, and breast are preferably accepted for treatment.
    Type: Grant
    Filed: July 26, 2013
    Date of Patent: January 19, 2016
    Assignee: AHR Pharmaceuticals, Inc.
    Inventor: Jiasheng Song
  • Patent number: 9205125
    Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.
    Type: Grant
    Filed: September 26, 2013
    Date of Patent: December 8, 2015
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Han-jie Zhou, Congcong M. Sun, Kevin D. Shenk, Guy J. Laidig
  • Patent number: 9205124
    Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.
    Type: Grant
    Filed: September 26, 2013
    Date of Patent: December 8, 2015
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Han-jie Zhou, Congcong M. Sun, Kevin D. Shenk, Guy J. Laidig
  • Patent number: 9204646
    Abstract: The present invention relates to novel pyrazole(thio)tetrahydronaphthyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: December 8, 2015
    Assignee: BAYER CROPSCIENCE AG
    Inventors: Simon Maechling, Mazen Es-Sayed, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Jean-Pierre Vors, Stephane Brunet, Helene Lachaise
  • Patent number: 9205126
    Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.
    Type: Grant
    Filed: September 26, 2013
    Date of Patent: December 8, 2015
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Han-jie Zhou, Congcong M. Sun, Kevin D. Shenk, Guy J. Laidig
  • Patent number: 9199941
    Abstract: The present invention relates to novel 1-methyl-pyrazole(thio)indanyl carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: December 1, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Pierre-Yves Coqueron, Mazen Es-Sayed, Simon Maechling, Pierre Wasnaire, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Lionel Carles, Christophe Dubost, Stephane Brunet, Helene Lachaise, Jean-Pierre Vors
  • Patent number: 9174948
    Abstract: A relatively non-toxic desazadesferrithiocin analog having the formula: wherein: R1, R2, R4 and R5 may be the same or different and may be H, straight or branched chain alkyl having up to 14 carbon atoms, e.g., methyl, ethyl, propyl and butyl, or arylalkyl wherein the aryl portion is hydrocarbyl and the alkyl portion is straight or branched chain, the arylalkyl group having up to 14 carbon atoms, R2 optionally being alkoxy having up to 14 carbon atoms; R3 is [(CH2)n—O]x—[(CH2)n—O]y-alkyl; n is, independently, an integer from 1 to 8; x is an integer from 1 to 8; y is an integer from 0 to 8, and R3O may occupy any position on the phenyl ring except the 4-position, or a salt, hydrate or solvate thereof; and methods and compositions for treating the effects of trivalent metal, i.e., iron, overload.
    Type: Grant
    Filed: November 21, 2012
    Date of Patent: November 3, 2015
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron, Jr.
  • Patent number: 9167821
    Abstract: Bis(difluoromethyl)pyrazole derivatives of the formula (I) in which the symbols R1, X and G are each as defined in the description, and agrochemically active salts, metal complexes and N-oxides thereof, and use thereof for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: August 20, 2013
    Date of Patent: October 27, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Tomoki Tsuchiya, Pierre Wasnaire, Jurgen Benting, Daniela Portz, Ulrike Wachendorff-Neumann
  • Patent number: 9156775
    Abstract: The present invention relates to 1,3-thiazole compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof.
    Type: Grant
    Filed: November 8, 2011
    Date of Patent: October 13, 2015
    Assignees: DUKE UNIVERSITY, CHAPERONE THERAPEUTICS, INC.
    Inventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
  • Patent number: 9150563
    Abstract: The present invention provides a compound having excellent regulating action on blood lipid level. The present invention provides a compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, etc., wherein A represents a 5-membered nitrogen-containing aromatic heterocyclyl group; R1 represents COOH or the like; each R2 represents an alkyl or the like; each R3 represents an optionally substituted phenyl, an optionally substituted phenylalkyl, or the like; m represents 0, 1, 2, or 3; n represents 0 or 1; each of R4, R5, R6, and R7 represents H, an alkyl, or the like; and B represents an optionally substituted naphthyl, an optionally substituted aromatic heterocyclyl, or a group represented by the following formula (II) wherein each of B1 and B2 represents an optionally substituted phenyl or an optionally substituted aromatic heterocyclyl.
    Type: Grant
    Filed: February 10, 2014
    Date of Patent: October 6, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Keiko Suzuki, Takahiro Yamaguchi, Akihiro Tamura, Tomohiro Nishizawa, Mitsuhiro Yamaguchi
  • Patent number: 9150527
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: October 6, 2015
    Assignee: Innocrin Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger
  • Patent number: 9139541
    Abstract: The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.
    Type: Grant
    Filed: January 20, 2015
    Date of Patent: September 22, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Manoj C. Desai, Allen Yu Hong, Hongtao Liu, Randall W. Vivian, Lianhong Xu
  • Patent number: 9107912
    Abstract: The present disclosure relates to a method of treating hyperuricemia in a patient that also suffers from a second disease state requiring treatment with theophylline, wherein the patient receives concomitant treatment with a xanthine oxidoreductase inhibitor and theophylline without resulting in theophylline toxicity to the patient and without substantial adjustments to the manufacturer's recommended dosage of theophylline.
    Type: Grant
    Filed: September 8, 2011
    Date of Patent: August 18, 2015
    Assignee: Takeda Pharmaceuticals U.S.A., Inc.
    Inventors: Lhanoo Gunawardhana, Max Tsai, Himanshu Naik
  • Patent number: 9102615
    Abstract: The invention relates to the R-enantiomer of N-carbamoylmethyl-4-phenyl-2-pyrrolidinone (R-Carphedon) of pharmacological value. The method of its preparation includes the N-alkylation of 4(R)-phenyl-2-pyrrolidinone with ethyl bromoacetate in the presence of a strong base and the treatment of intermediate N-ethoxycarbonylmethyl-4(R)-phenyl-2-pyrrolidinone with ammonia.
    Type: Grant
    Filed: March 15, 2007
    Date of Patent: August 11, 2015
    Assignee: Joint Stock Company (JSC) “OLAINFARM”
    Inventors: Grigory Veinberg, Maksim Vorona, Liga Zvejniece, Aleksandrs Chernobrovijs, Ivars Kalvinsh, Ligita Karina, Maija Dambrova
  • Patent number: RE46792
    Abstract: The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: wherein R1 is an aryl group which may have one or more substituents; R2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y1-A1- or or —Y2—C(?O)— wherein Y1 is a group such as —C(?O)—, A1 is a group such as a lower alkylene group, and Y2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.
    Type: Grant
    Filed: June 14, 2017
    Date of Patent: April 17, 2018
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Minoru Okada, Masaya Kato, Norifumi Sato, Tetsuyuki Uno, Hideki Kitagaki, Junpei Haruta, Hidetaka Hiyama, Tomonori Shibata