Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/357)
  • Patent number: 10806794
    Abstract: Provided herein (among other things) are protease inhibitor compounds having enhanced features, along with methods for administering such compounds. For example, the subject compounds can be administered without concomitant administration of a CYP3A4 inhibitor, have increased therapeutic index and/or increased potency, and are low-resistance inducing in nature.
    Type: Grant
    Filed: August 21, 2018
    Date of Patent: October 20, 2020
    Assignee: Nektar Therapeutics
    Inventors: C. Simone Jude-Fishburn, Laurie A. VanderVeen, Timothy A. Riley
  • Patent number: 10793552
    Abstract: The present invention provides compounds of the Formula (I), or a pharmaceutically acceptable salt thereof, where n and R1 are defined herein, methods of treating patients for liver disease, and processes for preparing the compounds.
    Type: Grant
    Filed: September 26, 2019
    Date of Patent: October 6, 2020
    Assignee: ELI LILLY AND COMPANY
    Inventors: David Andrew Coates, Luo Heng Qin, Yi Wei, Jingye Zhou
  • Patent number: 10791738
    Abstract: The present invention can provide a composition and a method excellent in plant protection effect against diseases and pests. The composition comprises fluopyram and fluxapyroxad, and the method comprises a step of applying fluopyram and fluxapyroxad to a plant or soil for cultivating the plant.
    Type: Grant
    Filed: March 12, 2020
    Date of Patent: October 6, 2020
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Masato Soma
  • Patent number: 10759761
    Abstract: The present invention relates to a process for the preparation of compounds endowed with phosphodiesterase (PDE4) inhibitory activity having formula (I). The invention also relates to the process for the isolation by crystallization of the compound (I) and to its use for the preparation of pharmaceutical compositions for inhalation in combination with suitable carriers or vehicles. The present invention also relates to solvates and crystal forms of a compound of formula (I). The synthesized product is suitable for use in pharmaceutical applications for instance in the treatment of respiratory diseases.
    Type: Grant
    Filed: April 23, 2019
    Date of Patent: September 1, 2020
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Alessandro Falchi, Emilio Lutero, Emanuele Ferrari, Fausto Pivetti, Rocco Bussolati, Edoardo Mariani, Orsola Vecchi, Erhard Bappert, Caterina Ventrici
  • Patent number: 10689354
    Abstract: A compound, represented by the following formula or a medically acceptable salt thereof, having an effect of regulating the activity of an androgen receptor. In the formula, X represents S, O; Z represents (Ra)n-A-(CR13R14)0-1—(CR11R12)0-1; A represents aryl, heteroaryl; R1 represents alkyl, cycloalkyl, alkenyl, alkynyl, alkoxyalkyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl; R2 represents hydrogen, halogen, alkyl, cycloalkyl, phenyl; R3 represents hydrogen, halogen, alkyl, cycloalkyl, alkoxyalkyl, alkenyl, alkynyl, cycloalkenyl, aryl, arylalkyl, heterocycle, heterocyclic alkyl, acyl, cycloalkylcarbonyl, benzoyl, spiroalkyl, adamantyl, silyl, R31R32NCO—; R4 and R5 represent hydrogen, halogen, alkyl, phenyl, and cycloalkyl.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: June 23, 2020
    Assignee: Teijin Pharma Limited
    Inventors: Shinnosuke Hosoda, Gen Unoki, Hidekazu Watanabe, Kosuke Sasaki, Jun Shibata, Emi Yokoyama, Kyohei Horie, Kenichiro Takagi
  • Patent number: 10675257
    Abstract: The present invention relates to a composition for use in treating a glioma or ameliorating the effects of a glioma, particularly glioblastoma, wherein said composition comprises a first active agent selected from the group consisting of a compound of formula (I), or a pharmaceutically acceptable salt thereof, (I) and a second active agent, which is temozolomide, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: July 26, 2016
    Date of Patent: June 9, 2020
    Assignee: INFLECTIS BIOSCIENCE
    Inventors: Philippe Guedat, Pierre Miniou
  • Patent number: 10639300
    Abstract: Methods of treating and preventing conditions of a nasal or paranasal mucous membrane are described. The methods include administering a pharmaceutical composition including a nicotinic acetylcholine receptor (nAChR) agonist, such as (S)-(1-methyl-2-pyrrolidinyl)-pyridine, or a pharmaceutically acceptable salt, analog, precursor or derivative thereof. The methods can be used to treat a wide variety of conditions of the nasal or paranasal mucous membrane, such as nasal congestion and nose bleeds.
    Type: Grant
    Filed: April 12, 2017
    Date of Patent: May 5, 2020
    Inventor: Arturo Solis Herrera
  • Patent number: 10624344
    Abstract: The present invention can provide a composition and a method excellent in plant protection effect against diseases and pests. The composition comprises fluopyram and fluxapyroxad, and the method comprises a step of applying fluopyram and fluxapyroxad to a plant or soil for cultivating the plant.
    Type: Grant
    Filed: June 14, 2019
    Date of Patent: April 21, 2020
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Masato Soma
  • Patent number: 10626100
    Abstract: The present invention provides a compound having the structure: wherein R1 is halogen, —NR5R6, —NR5—C(?O)—R6, —NH—C(?O)—OR7, —OR7, —NO2, —CN, —SR7, —SO2R7, —CO2R7, CF3, —SOR7, —POR7, —C(?S)R7, —C(?O)—NR5R6, —CH2—C(?O)—NR5R6, —C(?NR5)R6, —P(?O)(OR5)(OR6), —P(OR5)(OR6), —C(?S)R7, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, aryl, heteroaryl, or heterocyclyl, wherein R5, R6, and R7 and are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, hydroxyalkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, C1-5 alkyl-aryl, or C1-5 alkyl-NH-aryl; Ar1 is phenyl or thiophene; wherein when Ar1 is phenyl, then R1 is other than —C(?O)—NR5R6, where one of R5 or R6 is phenyl or quinoline and the other of R5 or R6 is hydroxyalkyl, or where one of R5 or R6 is quinoline and the other of R5 or R6 is H; and wherein when Ar1 is phenyl, then R1 is other than —NR5—C(?O)—R6, where one of R5 is H and R6 is quinoline, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: April 21, 2020
    Assignees: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK, MEMORIAL SLOAN-KETTERING CANCER CENTER
    Inventors: Ronald Breslow, Paul Marks, Adaickapillai Mahendran, Yuanshan Yao
  • Patent number: 10548315
    Abstract: The present invention relates to the use of succinate dehydrogenase Inhibitors for extending shelf life and storage stability of fruits and vegetables, to a method for extending shelf life of fruits and vegetables by applying a succinate dehydrogenase inhibitor to the crops prior to the harvest of the fruits or vegetables and to a fruit or vegetable treated with a succinate dehydrogenase Inhibitor.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: February 4, 2020
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Heiko Rieck, Hélène Lachaise, Gilbert Labourdette, Pete Howard Davies, Dominique Steiger, Luk De Maeyer, George Hauley Musson, IV, Lorianne Fought, Sylvain Tafforeau
  • Patent number: 10517857
    Abstract: Methods of treating and preventing conditions of a nasal or paranasal mucous membrane are described. The methods include administering a pharmaceutical composition including a nicotinic acetylcholine receptor (nAChR) agonist, such as (S)-(1-methyl-2-pyrrolidinyl)-pyridine, or a pharmaceutically acceptable salt, analog, precursor or derivative thereof. The methods can be used to treat a wide variety of conditions of the nasal or paranasal mucous membrane, such as nasal congestion and nose bleeds.
    Type: Grant
    Filed: April 12, 2017
    Date of Patent: December 31, 2019
    Inventor: Arturo Solis Herrera
  • Patent number: 10500190
    Abstract: A pharmaceutical composition for sublingual or buccal administration of melatonin and valerian is complexed with a beta cyclodextrin or another complexation agent. It is then encased in a liposome. The molecules encased in the liposome are then dehydrated and compounded into any of a number of dosage forms such as a dissolvable strip of material, a gum, lozenge, mint, tablet, or powder.
    Type: Grant
    Filed: April 19, 2019
    Date of Patent: December 10, 2019
    Inventor: Michael Farber
  • Patent number: 10390476
    Abstract: Provided are methods for reducing the occurrence of sudden death syndrome in plants, such as soybeans, using compounds of the general formula (I).
    Type: Grant
    Filed: November 23, 2011
    Date of Patent: August 27, 2019
    Assignee: Bayer CropScience LP
    Inventors: Jennifer Riggs, David Doran
  • Patent number: 10357507
    Abstract: The present invention provides a method of inhibiting renal fibrosis in a subject in need thereof.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: July 23, 2019
    Inventor: Sheau-Long Lee
  • Patent number: 10350200
    Abstract: The present invention is directed at aqueous suspensions of oxime compounds, such as 2-pyridine aldoxime methyl chloride (2-PAM Cl) for autoinjectors. The suspensions are able to provide 600 mg of 2-PAM Cl in one relatively small dose of less than or equal to 1.0 mL, and are particularly useful for placement in relatively small size autoinjectors.
    Type: Grant
    Filed: January 23, 2017
    Date of Patent: July 16, 2019
    Assignee: SOUTHWEST RESEARCH INSTITUTE
    Inventors: Hong Dixon, Joseph A. McDonough, Larry A. Cabell
  • Patent number: 10266499
    Abstract: The present invention relates to a compound of formula (I): wherein R1 is R3—IPU and R2 is the acyloxy residue of diclofenac, and specified by the following structures: wherein OH—R3—IPU is selected from and R4 and R5 may be the same or different selected from H and CH3 and salts, solvates and hydrates thereof.
    Type: Grant
    Filed: October 27, 2015
    Date of Patent: April 23, 2019
    Inventor: Claus Selch Larsen
  • Patent number: 10253372
    Abstract: The present invention relates to the methods and products for detection of colorectal cancer. Additionally, the present invention relates to methods and products for determining the probability, risk or incidence of colorectal cancer and of colorectal cancer metastasis. The products and methods of the present invention include detecting the level of expression of COL10A1 or MMP11, in combination, from samples, including tissue samples, from humans who currently have been diagnosed with cancer or who were previously diagnosed with cancer and those who are thought to have cancer and are undergoing diagnosis.
    Type: Grant
    Filed: August 29, 2016
    Date of Patent: April 9, 2019
    Assignee: Siemens Healthcare Diagnostics Inc.
    Inventors: Michael Stürzl, Roland S. Croner, Andreas Konrad
  • Patent number: 10253027
    Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
    Type: Grant
    Filed: July 1, 2014
    Date of Patent: April 9, 2019
    Assignees: Bristol-Myers Squibb Company, Syngene International Limited, Bristol-Myers Squibb Company
    Inventors: Richard A. Hartz, Vijay T. Ahuja, Joanne J. Bronson, Carolyn Diane Dzierba, John E. Macor, Susheel Jethanand Nara, Ramkumar Rajamani
  • Patent number: 10246448
    Abstract: The invention relates to compounds acting as antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula (I): Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold-induced and/or exacerbated-respiratory disorders, urological disorders, corneal disorders associated to disturbances in the production of the tears and/or altered blinking such as epiphora and dry eye disease.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: April 2, 2019
    Assignee: DOMPÉ FARMACEUTICI S.P.A.
    Inventors: Andrea Aramini, Gianluca Bianchini, Samuele Lillini
  • Patent number: 10238609
    Abstract: Cyanide antidote compositions and methods of use are described herein. A cyanide antidote composition may include a sulfur analog, sulfur analog derivative, or a pharmaceutically acceptable derivative of a sulfur analog.
    Type: Grant
    Filed: November 8, 2016
    Date of Patent: March 26, 2019
    Assignee: Sam Houston State University
    Inventors: Ilona Petrikovics, Csaba Jaszberenyi
  • Patent number: 10149860
    Abstract: Compounds, pharmaceutical compositions, and methods of using such compounds and compositions to treat or prevent Alzheimer's disease and related tauopathies through the inhibition of USP-9X and/or enhancement of SCF(?-TrCP).
    Type: Grant
    Filed: February 3, 2016
    Date of Patent: December 11, 2018
    Assignee: Board of Trustees of the Leland Stanford Junior University, Stanford University Office of Technology Licensing
    Inventors: Bingwei Lu, Seongsoo Lee
  • Patent number: 10130907
    Abstract: A class of water lean, organic solvents that can bind with various acid gasses to form acid gas bound molecules having a high degree of intramolecular hydrogen bonding which enables their use as regenerable solvents for acid gas capture. Unlike the other devices described in the prior art, the present invention takes advantage of shortened distances between the portions of the molecule that form hydrogen bonds within the structures when loaded with an acid gas so as to create a molecule with a higher internal bonding affinity and a reduced proclivity for agglomeration with other molecules.
    Type: Grant
    Filed: January 19, 2017
    Date of Patent: November 20, 2018
    Assignee: BATTELLE MEMORIAL INSTITUTE
    Inventors: Phillip K. Koech, Deepika Malhotra, David J. Heldebrant, Vassiliki-Alexandra Glezakou, Roger J. Rousseau, David C. Cantu
  • Patent number: 10092656
    Abstract: Provided herein (among other things) are protease inhibitor compounds having enhanced features, along with methods for administering such compounds. For example, the subject compounds can be administered without concomitant administration of a CYP3A4 inhibitor, have increased therapeutic index and/or increased potency, and are low-resistance inducing in nature.
    Type: Grant
    Filed: August 4, 2016
    Date of Patent: October 9, 2018
    Assignee: Nektar Therapeutics
    Inventors: C. Simone Jude-Fishburn, Laurie A. VanderVeen, Timothy A. Riley
  • Patent number: 10077245
    Abstract: The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window.
    Type: Grant
    Filed: April 22, 2015
    Date of Patent: September 18, 2018
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Fajun Nan, Min Li, Zhaobing Gao, Yangming Zhang, Haining Hu, Haiyan Xu, Huanan Liu, Xiaoping Pi
  • Patent number: 10064817
    Abstract: The present invention provides pharmaceutical compositions comprising azelastine, or a pharmaceutically acceptable salt or ester thereof including azelastine hydrochloride, and optionally one or more additional active agents. Preferred such compositions further comprise one or more pharmaceutically acceptable carriers or excipients that reduce the amount of post-nasal drip, and/or that minimize or mask the unpleasant bitter taste associated with post-nasal drip, of the compositions into the oral cavity, upon intranasal or ocular administration of the compositions. Especially effective excipients used in the compositions of the present invention are hypromellose as a viscosity modifier and sucralose as a taste-masking agent. The invention also provides methods of treating or preventing certain disorders, or symptomatic relief therefrom, by administering the compositions of the invention to a patient, e.g.
    Type: Grant
    Filed: October 28, 2011
    Date of Patent: September 4, 2018
    Assignee: Meda Pharmaceuticals Inc.
    Inventors: Phuong Grace Dang, Brian D. Lawrence, Gul Balwani, Alexander D. D'Addio
  • Patent number: 10059698
    Abstract: A hesperetin aza-cinnamic acid derivative has the following formula (I): R1 is H or alkyl, and R2 and R2 are independently H, alkyl, hydroxy, halogen, nitro, or alkoxy.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: August 28, 2018
    Assignee: Shaanxi University of Science and Technology
    Inventors: Chengyuan Liang, Minyi Jia, Yuecheng Lyu, Xingke Ju, Lei Tian
  • Patent number: 9993464
    Abstract: The invention relates to a pharmaceutical composition comprising methyl (2R.3R)-2-{3-[amino(imino)methyl]benzyl}-3-{[4-(1-oxidopyridin-4-yl)benzoyl]amino}butanoate or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable acidic reacting compound or to an aqueous solution or dispersion of the composition as well as a process for the preparation of the same, methods of using such compositions to treat subjects suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.
    Type: Grant
    Filed: September 14, 2016
    Date of Patent: June 12, 2018
    Assignee: SANOFI
    Inventors: Walter Kamm, Till Bussemer, Doris Andert, Bernd Kuehn, Ernst-Josef Todt
  • Patent number: 9988353
    Abstract: The present invention relates to a novel catalytic hydrogenation of substituted 2-methyl cyanopyridyl derivatives, in particular 3-chloro-5-(trifluoromethyl)pyridin-2-yl]acetonitrile [=Py-CN] to substituted 2-ethylaminopyridine derivatives, in particular 2-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]ethanamine [=Py-ethanamine] or salts thereof in the presence of metal catalysts, in particular palladium catalysts.
    Type: Grant
    Filed: November 11, 2014
    Date of Patent: June 5, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Wahed Ahmed Moradi, Thomas Himmler, Thomas Norbert Mueller, Albert Schnatterer, Guenter Schlegel
  • Patent number: 9937262
    Abstract: The present invention relates to a compound of formula (I): wherein R1 is R3-IPU and R2 is the acyloxy residue of diclofenac or naproxen, and specified by the following structures (A) wherein OH—R3-IPU is selected from (B) and R4 and R5 may be the same or different selected from (C) and salts, solvates and hydrates thereof.
    Type: Grant
    Filed: April 28, 2014
    Date of Patent: April 10, 2018
    Inventor: Claus Selch Larsen
  • Patent number: 9914717
    Abstract: The present invention provides compounds of formula (I) or a pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein W, X, n, s, t, and Ra are as described herein. The present invention relates generally to selective inhibitors of histone deacetylase and to methods of making and using them.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: March 13, 2018
    Assignee: The Broad Institute, Inc.
    Inventors: Edward Holson, Fanny Lazzaro, David Olson, Florence Fevrier Wagner, Michel Weiwer
  • Patent number: 9844560
    Abstract: The present invention provides a method of treating a subject afflicted with lupus nephritis comprising administering to the subject an amount of ginsenoside M1 effective to treat the subject.
    Type: Grant
    Filed: May 4, 2015
    Date of Patent: December 19, 2017
    Inventor: Sheau-Long Lee
  • Patent number: 9839645
    Abstract: The present invention relates to an agent for killing HIV-1-infected cells, comprising a compound represented by formula (I): wherein Ar1 and Ar2 are the same or different and represent a substituted or unsubstituted aromatic group, and X represents —CH2O— or —CH?CH—, its salt, or their solvate, and a combined preparation for simultaneous, separate, or sequential administration in treating or preventing HIV-1 infection, comprising two separate preparations: (a) a preparation comprising a compound represented by the formula (I), its salt, or their solvate, and (b) a preparation comprising an anti-HIV-1 drug.
    Type: Grant
    Filed: July 17, 2017
    Date of Patent: December 12, 2017
    Assignee: KAGOSHIMA UNIVERSITY
    Inventor: Mika Okamoto
  • Patent number: 9809557
    Abstract: The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.
    Type: Grant
    Filed: October 31, 2012
    Date of Patent: November 7, 2017
    Inventor: Claus Selch Larsen
  • Patent number: 9776963
    Abstract: The invention provides for compounds of formula I: wherein Z is absent or (CRARB)nW; each RA and RB is independently (i) H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, heteroaralkyl, haloalkyl, each of which may be optionally substituted; (ii) OH, ORc, NH2, NHRc, NRcRc, SH, S(O)mRc; or (iii) RA and RB together form C(O); W is absent, C(O), C(O)O, C(O)NRcRc, O, S(O)m, or NRcRc; Y is an optionally substituted heterocyclic, optionally substituted heteroaryl, optionally substituted cycloalkyl, optionally substituted aryl, or NRXRY; wherein Rx and Ry are each independently H, alkyl or aryl; X1 is selected from the group consisting of halogen, methyl, and hydroxyl; X2 is a halogen; each Rc is independently alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl, each of which may be optionally substituted; m is O, 1, or 2; and n is 1, 2, 3, 4, 5, or 6; and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: October 3, 2017
    Assignees: The Trustees of the University of Pennsylvania, Dana-Farber Cancer Institute, Inc., The Johns Hopkins University, Bryn Mawr College, The Trustees of Columbia University in the City of New York
    Inventors: Joseph G. Sodroski, Navid Madani, Arne Schön, Judith M. LaLonde, Joel R. Courter, Takahiro Soeta, Danny Ng, Ernesto Freire, Amos B. Smith, III, Amy M. Princiotto, Matthew Le-Khac, Wayne A. Hendrickson
  • Patent number: 9763958
    Abstract: The present invention is directed to preservative-free solutions of bimatoprost and timolol for lowering intra-ocular pressure and treatment of glaucoma.
    Type: Grant
    Filed: April 21, 2015
    Date of Patent: September 19, 2017
    Assignee: ALLERGAN, INC.
    Inventors: Sukhon Likitlersuang, Ajay Parashar, Chetan P. Pujara, William F. Kelly, Jie Shen, Marina Bejanian, Rhett Schiffman
  • Patent number: 9725467
    Abstract: Novel fluorinated benzenesulfonamides compounds of general formula (I) can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression.
    Type: Grant
    Filed: October 30, 2012
    Date of Patent: August 8, 2017
    Assignee: VILNIUS UNIVERSITY
    Inventors: Daumantas Matulis, Virginija Dudutiene, Asta Zubriene
  • Patent number: 9708302
    Abstract: The present invention relates to compounds of formula wherein R1 is C4-6-cycloalkyl or C4-6-heterocycloalkyl, which are optionally substituted by one or two substituents, selected from hydroxy or lower alkyl; A is phenyl, pyridinyl or piperidinyl; R2 is hydrogen, halogen, lower alkyl, cyano, C4-6-cycloalkyl, lower alkoxy, lower alkoxy substituted by halogen, or is a five- or six-membered heteroaryl, optionally substituted by lower alkyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment or prophylaxis of Alzheimer's disease, cognitive impairment, schizophrenia, pain or sleep disorders.
    Type: Grant
    Filed: July 21, 2016
    Date of Patent: July 18, 2017
    Assignee: HOFFMANN-LA-ROCHE INC.
    Inventors: Katrin Groebke Zbinden, Emmanuel Pinard, Thomas Ryckmans
  • Patent number: 9624167
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain substituted N-(4-hydroxy-4-methyl-cyclohexyl)-4-phenyl-benzenesulfonamide and N-(4-hydroxy-4-methyl -cyclohexyl)-4-(2-pyridyl)benzenesulfonamide compounds (collectively referred to herein as HMC compounds) that are useful, for example, in the treatment of disorders (e.g.
    Type: Grant
    Filed: June 24, 2014
    Date of Patent: April 18, 2017
    Assignee: PIMCO 2664 Limited
    Inventors: Lisa Patel, Stephen Allan Smith, Iain Robert Greig, Samuel Cameron Williams
  • Patent number: 9539249
    Abstract: Methods of treatment of multiple sclerosis (MS) with PPAR? agonists, and in particular with the compound of formula (I) known as INT131:
    Type: Grant
    Filed: May 8, 2015
    Date of Patent: January 10, 2017
    Assignee: Intekrin Therapeutics, Inc.
    Inventor: David Weinstein
  • Patent number: 9533963
    Abstract: Alkylamidothiazoles of general formula (I), wherein R 1=—C1-C24 alkyl (linear and branched), —C1-C24 alkenyl (linear and branched), —C1-C8 cycloalkyl, —C1-C8 cycloalkyl-alkylhydroxy, —C1-C24 alkylhydroxy (linear and branched), —C1-C24 alkylamine (linear and branched), —C1-C24 alkylaryl (linear and branched), —C1-C24 alkylaryl-alkyl-hydroxy (linear and branched), —C1-C24 alkyl-heteroaryl (linear and branched), —C1-C24-alkyl-O—C1-C24-alkyl (linear and branched), —C1-C24 alkyl morpholino, —C1-C24 alkyl piperidino, —C1-C24 alkyl piperazino, —C1-C24 alkyl-piperazino-N-alkyl, as well as cosmetic or dermatological preparations having an effective content of one or more alkylamidothiazoles, as well as the use thereof for the cosmetic or dermatological treatment and/or prophylaxis of undesired skin pigmentation.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: January 3, 2017
    Assignee: BEIERSDORF AG
    Inventors: Ludger Kolbe, Cathrin Scherner, Sabrina Breitkreutz, Michael Woehrmann, Tobias Mann, Wolfram Gerwat, Torsten Schlaeger
  • Patent number: 9464042
    Abstract: A biguanide derivative compound with N4-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPK and inhibition of cancer cell proliferation in a low dose, compared with conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.
    Type: Grant
    Filed: September 8, 2015
    Date of Patent: October 11, 2016
    Assignee: IMMUNOMET THERAPEUTICS INC.
    Inventors: Sung Wuk Kim, Sung Soo Jun, Chang Hee Min, Se Hwan Park, Yong Eun Kim, Duck Kim, Ji Sun Lee, Ju Hoon Oh
  • Patent number: 9452980
    Abstract: The invention relates to compounds of formula wherein R, R1, R2, X, and Y are as defined herein and to a pharmaceutically suitable acid addition salt thereof. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: September 27, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Katrin Groebke Zbinden, Roger Norcross, Philippe Pflieger
  • Patent number: 9428490
    Abstract: The invention generally relates to nuclear transport modulators, e.g CRM1 inhibitors, and more particularly to a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula (I), or a pharmaceutically acceptable salt or composition thereof, e.g, in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Grant
    Filed: July 26, 2012
    Date of Patent: August 30, 2016
    Assignee: Karyopharm Therapeutics Inc.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Michael Kauffman, Sharon Shechter, Dilara McCauley, Yosef Landesman, William Senapedis, Jean-Richard Saint-Martin
  • Patent number: 9422276
    Abstract: The present application relates to known and novel aryl- and hetarylcarboxamides of the formula (I) and to their use as medicaments for controlling endoparasites in animals or humans, and also to parasiticidal compositions, in particular endoparasites, comprising aryl- and hetarylcyclylcarboxamides.
    Type: Grant
    Filed: November 23, 2012
    Date of Patent: August 23, 2016
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Hans-Georg Schwarz, Axel Trautwein, Lothar Willms, Maike Hink, Peter Lümmen, Ulrich Görgens, Pierre-Yves Coqueron, Achim Harder, Claudia Welz, Joerg Nico Greul
  • Patent number: 9346796
    Abstract: Methods and intermediates useful for preparing a compound of formula I: and salts thereof.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: May 24, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Aaron J. Cullen, Richard Hung Chiu Yu
  • Patent number: 9289400
    Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: March 22, 2016
    Assignees: Drexel University, Rutgers, The State University of New Jersey
    Inventors: Sandhya Kortagere, Eldo V. Kuzhikandahil
  • Patent number: 9289448
    Abstract: Compounds, pharmaceutical compositions, and methods of using such compounds and compositions to treat or prevent Alzheimer's disease and related tauopathies through the inhibition of USP-9X and/or enhancement of SCF(?-TrCP).
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: March 22, 2016
    Assignee: Board of Trustees of the Leland Stanford Junior University
    Inventors: Bingwei Lu, Seongsoo Lee
  • Patent number: 9232794
    Abstract: The invention relates to the use of succinate dehydrogenase inhibitors, especially of fluopyram, for controlling Sclerotinia ssp., to a method for treating plants or plant parts for controlling Sclerotinia ssp. and to a method for treating seed for controlling Sclerotinia ssp. in the seed and in the plants which grow from the seed, by treating the seed with a succinate dehydrogenase inhibitor.
    Type: Grant
    Filed: June 2, 2010
    Date of Patent: January 12, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ingo Wetcholowsky, Heiko Rieck, Gilbert Labourdette, Jose Augusto Geraldes
  • Patent number: 9198419
    Abstract: The present disclosure is related to the field of agrochemicals, including profungicides of UK-2A and their use to control Black Sigatoka.
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: December 1, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: W. John Owen, Leonardo Paniagua, David G. Oimette
  • Patent number: 9179674
    Abstract: The invention relates to compounds of macrocyclic picolinamides of Formula I suitable to control or prevent growth of fungi.
    Type: Grant
    Filed: September 29, 2014
    Date of Patent: November 10, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Timothy P. Martin, Kevin G. Meyer, Benjamin Nugent, Chenglin Yao, W. John Owen, Anne M. Wilson, Ian O'Callaghan, Jeremy Wilmot, Johnathan E. DeLorbe, William Dent, III