Additional Ring Containing Patents (Class 546/192)
  • Patent number: 10632111
    Abstract: The present invention relates to a donepezil derivative of general formula (I) or a pharmaceutically acceptable salt thereof, wherein R in the formula is as disclosed herein; and a method for preparation thereof; and a composition comprising an effective amount of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to use of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof in preparing a medicament for treating a disease resulted from an abnormality in acetylcholinesterase activity.
    Type: Grant
    Filed: May 7, 2018
    Date of Patent: April 28, 2020
    Assignee: NANJING NORATECH PHARMACEUTICALS CO., LTD.
    Inventors: Fei Liu, Cuixia Zhang, Chenggang Lin, Chunyan Zhou, Pan Chen, Wei Wang, Lulu Wang
  • Patent number: 10080746
    Abstract: The present invention relates to a donepezil derivative of general formula (I) or a pharmaceutically acceptable salt thereof, wherein R in the formula is as disclosed herein; and a method for preparation thereof; and a composition comprising an effective amount of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to use of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof in preparing a medicament for treating a disease resulted from an abnormality in acetylcholinesterase activity.
    Type: Grant
    Filed: November 26, 2015
    Date of Patent: September 25, 2018
    Assignee: NORATECH PHARMACEUTICALS, INC.
    Inventors: Fei Liu, Cuixia Zhang, Chenggang Lin, Chunyan Zhou, Pan Chen, Wei Wang, Lulu Wang
  • Patent number: 10035768
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Grant
    Filed: October 2, 2017
    Date of Patent: July 31, 2018
    Assignee: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Patent number: 10017472
    Abstract: The present invention relates to 2-isopropoxy-5-methyl-4-(piperidin-4-yl) aniline dihydrochloride monohydrate and a preparation method of the same. The 2-isopropoxy-5-methyl-4-(piperidin-4-yl) aniline dihydrochloride monohydrate has a very good crystal form and is well suitable for recrystallization purification; further, the effect of impurity removal effect is very good, and any single impurity can be controlled less than 0.1%.
    Type: Grant
    Filed: March 2, 2016
    Date of Patent: July 10, 2018
    Assignee: 2Y-CHEM, LTD.
    Inventors: Jinfeng Song, Xungui He, Wensheng Tang, Yuan Wang
  • Patent number: 10000468
    Abstract: The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: June 19, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Mark E. Adams, Jason W. Brown, Stephen Hitchcock, Maria Hopkins, Shota Kikuchi, Betty Lam, Holger Monenschein, Holly Reichard, Huikai Sun
  • Patent number: 9808006
    Abstract: A compound of formula (I) wherein A, p, R1, R3, R4, R5, R6, m, R7, n and R8 are as defined in claim 1. Furthermore, the present invention relates to intermediates used to prepare compounds of formula (I), to methods of using them to combat and control insect, acarine, nematode and mollusc pests and to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them.
    Type: Grant
    Filed: July 23, 2013
    Date of Patent: November 7, 2017
    Assignee: Syngenta Participations AG
    Inventors: Thomas Pitterna, Jerome Yves Cassayre, Camilla Corsi, Peter Maienfisch
  • Publication number: 20150126511
    Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
    Type: Application
    Filed: September 30, 2014
    Publication date: May 7, 2015
    Inventors: Liming SHAO, Fengjiang WANG, Scott Christopher MALCOLM, Michael Charles HEWITT, Larry R. BUSH, Jianguo MA, Mark A. VARNEY, Una CAMPBELL, Sharon Rae ENGEL, Larry Wendell HARDY, Patrick KOCH, John E. CAMPBELL
  • Patent number: 9000005
    Abstract: The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: April 7, 2015
    Assignee: ArQule, Inc.
    Inventors: Yoshitaka Nakamura, Jo Ooyama
  • Patent number: 8969571
    Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: March 3, 2015
    Assignee: Theravance Respiratory Company, LLC
    Inventors: Mathai Mammen, Adam Hughes, Yan Chen
  • Publication number: 20150057443
    Abstract: Cycloalkyl amine compounds of Formula (I), wherein ring A is C3-C6 cycloalkyl, optionally substituted with one or more C1-C3 alkyl, and R5 is ORS2, in which RS2 is H or C1-C6 alkyl, or R5 and R6, together with the carbon atom to which they are attached, form C?O, for use in treating CNS disorders, including movement disorders, depressive disorders, sleep disorders, cognitive dysfunctions, obesity, sexual dysfunction and substance abuse.
    Type: Application
    Filed: August 21, 2014
    Publication date: February 26, 2015
    Inventors: Philip Huxley, Jonathan R. Heal, Richard S. Todd
  • Patent number: 8921559
    Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: December 30, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui, Xuqing Zhang
  • Publication number: 20140370441
    Abstract: An aqueous solution containing 0.1-20 wt % of a cyclic ammonium hydroxide is a useful developer for photosensitive resist materials. A resist pattern is formed by applying a chemically amplified positive resist composition onto a substrate to form a resist film, exposing the resist film to high-energy radiation, and developing the exposed resist film in a cyclic ammonium hydroxide-containing aqueous solution.
    Type: Application
    Filed: May 27, 2014
    Publication date: December 18, 2014
    Applicant: SHIN-ETSU CHEMICAL CO., LTD.
    Inventors: Jun Hatakeyama, Masaki Ohashi
  • Patent number: 8912219
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, X5, X6, Y, Z, G, R1a, R2a, R1b, R2b, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: December 16, 2014
    Assignee: Genentech, Inc.
    Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
  • Publication number: 20140363389
    Abstract: Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor is represented by general formula (1) (excluding clotrimazole) and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent.
    Type: Application
    Filed: August 19, 2014
    Publication date: December 11, 2014
    Inventors: Kouji Yokoyama, Makoto Kimura, Masashi Tamai, Yuko Saitoh, Tomomi Kato, Yu Ikeda
  • Patent number: 8901313
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: December 2, 2014
    Assignee: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
  • Patent number: 8877769
    Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).
    Type: Grant
    Filed: May 3, 2013
    Date of Patent: November 4, 2014
    Assignee: Janseen Pharmaceutica NV
    Inventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Sierestad
  • Patent number: 8859777
    Abstract: 4-Fluoro-4-phenylpiperidin-1-yl ? antagonists of general structure as well as pharmaceutical compositions comprising compounds of formula I, are disclosed. These compounds and compositions are useful as treatments of conditions or diseases associated with binding opioid receptors including pain, obesity, hyperalgesia, inflammation, osteoarthritis, drug addiction, and cancer. These compounds and compositions are also useful as treatments for tardive dyskinesia.
    Type: Grant
    Filed: April 29, 2011
    Date of Patent: October 14, 2014
    Assignee: Kinentia Biosciences LLC
    Inventor: David J. Fairfax
  • Patent number: 8853390
    Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: October 7, 2014
    Assignee: AbbVie Inc.
    Inventors: Yi-Yin Ku, Timothy A. Grieme, Jeffrey M. Kallemeyn, Mathew M. Mulhern
  • Patent number: 8841325
    Abstract: Provided herein are methods of restoring vitamin D sensitivity in tumor cells that are vitamin D resistant. Also provided are methods of treating, preventing or managing cancer using an immunomodulatory compound in combination with a vitamin D agent. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods provided herein are also disclosed.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: September 23, 2014
    Assignee: Celgene Corporation
    Inventors: Carole Brosseau, Justin Blake Bartlett, Angus George Dalgleish, Kay Winifred Colston, Christine Galustian
  • Patent number: 8815775
    Abstract: Bis(difluoromethyl)pyrazole derivatives of the formula (I) in which the symbols R1, X, Y and Q are each as defined in the description, and agrochemically active salts thereof, and use thereof for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).
    Type: Grant
    Filed: May 16, 2011
    Date of Patent: August 26, 2014
    Assignee: Bayer CropScience AG
    Inventors: Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Thomas Seitz, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Ulrike Wachendorff-Neumann
  • Publication number: 20140213785
    Abstract: A process is described for preparing aromatic and heteroaromatic amines of the general formula (I) Ar—NR1R2, in which an aromatic compound with the general formula (II) Ar—X is reacted in the presence of a catalyst with an amine of the general formula (III) H—NR1R2 and a base, wherein the catalyst is selected from transition metal complexes having one or more ligands with the general formula (IV).
    Type: Application
    Filed: April 3, 2012
    Publication date: July 31, 2014
    Inventors: Manfred Reetz, Gerlinde Mehler
  • Patent number: 8772318
    Abstract: This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: July 8, 2014
    Assignee: The Scripps Research Institute
    Inventors: Benjamin F. Cravatt, Jonathan Z. Long, Weiwei Li, Daniel K. Nomura
  • Patent number: 8772493
    Abstract: The present invention relates to a compound represented by formula 1 in the present specification or a pharmaceutically acceptable thereof, which inhibits an apoptosis mechanism of auditory hair cells for various ototoxicities leading to deafness, and protects the auditory organ and hearing, a method for preparation thereof, and a composition containing the same.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: July 8, 2014
    Assignees: Ajou University Industry-Academic Cooperation Foundation, Korea Research Institute of Chemical Technology
    Inventors: Chul Ho Kim, Young Sik Jung
  • Patent number: 8748613
    Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: June 10, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Cristina Pesenti, Stefano Bossolo
  • Publication number: 20140142304
    Abstract: There is provided a process for producing an aminopropyne or an enaminone comprising the step of reacting a metal acetylide, an amine and a carbonyl-containing compound in the presence of a transition metal catalyst. There is also provided a process for producing an aminopropyne comprising the step of reacting a metal acetylide, an amine and a halide-containing compound in the presence of a transition metal catalyst at a reaction temperature of 50° C. to 150° C. There are also provided processes to further synthesize the aminopropyne produced to obtain a butyneamine, another aminopropyne or a triazol.
    Type: Application
    Filed: July 6, 2012
    Publication date: May 22, 2014
    Applicant: Agency for Science, Technology and Research
    Inventors: Yugen Zhang, Dingyi Yu, Zhewang Lin
  • Patent number: 8697728
    Abstract: The invention relates to perhexiline, or a pharmaceutically acceptable salt thereof, for use in the treatment of hypertrophic cardiomyopathy, as well as to a method of treating HCM, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said HCM. The invention further relates to a treatment programme for treating HCM, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating HCM or the symptoms thereof.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: April 15, 2014
    Assignee: The University of Birmingham
    Inventors: Houman Ashrafian, Michael Paul Frenneaux
  • Publication number: 20140081019
    Abstract: The present invention relates to a process for deuteration of amines in the alpha and/or beta position of the N-atom by using a deuterium source and a Ruthenium(II) based catalyst.
    Type: Application
    Filed: May 21, 2012
    Publication date: March 20, 2014
    Applicant: SANOFI
    Inventors: Jens Atzrodt, Volker Derdau, Wolfgang Holla, Matthias Beller, Lorenz Neubert, Dirk Michalik
  • Publication number: 20140039181
    Abstract: The invention relates to a method for producing a N-substituted amine compound by catalyzed alkylation. The method uses amine and alcohol or two kinds of amines as the reaction materials, employs composite metal oxides catalyst at a reaction temperature of 80-180° C. to catalyze the reaction for 6-36 hours, so as to produce the N-substituted amine compound. The reaction condition of the method of the invention is relatively moderate, using a catalyst made of cheap non-noble metals, which is non-caustic and easy to be separated and reused. The reaction does not need any medium and has relatively high conversion rate and selectivity.
    Type: Application
    Filed: December 28, 2012
    Publication date: February 6, 2014
    Applicant: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
    Inventor: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
  • Patent number: 8642774
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: February 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
  • Patent number: 8623859
    Abstract: The invention relates to compounds of formula (I) wherein R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: January 7, 2014
    Assignee: Evotec AG
    Inventors: James Madden, David James Hallett, Alastair Parkes, Ali Raoof, Xiaolu Wang
  • Patent number: 8609731
    Abstract: The invention relates to substituted tetrahydronaphthalenes and derivatives thereof, and also to the physiologically compatible salts and physiologically functional derivatives thereof, to preparation thereof, to medicaments comprising at least one inventive substituted tetrahydronaphthalene or derivative thereof, and to the use of the inventive substituted tetrahydronaphthalenes and derivatives thereof as medicaments.
    Type: Grant
    Filed: February 12, 2010
    Date of Patent: December 17, 2013
    Assignee: SANOFI
    Inventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Torsten Haack, Petra Lennig
  • Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Patent number: 8592454
    Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: November 26, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Junya Shirai, Hideyuki Sugiyama, Taku Kamei, Hironobu Maezaki
  • Publication number: 20130289270
    Abstract: Embodiments of the invention provide methods and materials for chemical cross-coupling reactions that utilize aryl alcohol derivatives as cross-coupling partners. Embodiments of the invention include methods for the amination of aryl sulfamates and carbamates, which are attractive cross-coupling partners, particularly for use in multistep synthesis. Illustrative embodiments include versatile means to use simple derivatives of phenol as precursors to polysubstituted aryl amines, as exemplified by a concise synthesis of the antibacterial drug linezolid.
    Type: Application
    Filed: January 6, 2012
    Publication date: October 31, 2013
    Applicant: The Regents of the University of California
    Inventors: Neil K. Garg, Stephen D. Ramgren, Amanda L. Silberstein, Kyle W. Quasdorf
  • Publication number: 20130281700
    Abstract: The invention relates to palladium(0)-tris{tri-[3,5-bis(trifluoromethyl)-phenyl]-phosphine} complex of formula (I), as well as to its preparation and use. This compound is outstandingly stable, and can be used as catalyst with excellent results.
    Type: Application
    Filed: June 14, 2013
    Publication date: October 24, 2013
    Applicants: CHINOIN GYOGYSZER-ES VEGYESZETI TER-MEKEK GYARA ZRT, H4SEP KFT
    Inventors: Zoltán DALICZEK, Tibor SOÓS, Zoltán FINTA, Géza Timári, Gábor Vlád
  • Patent number: 8563779
    Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 19, 2011
    Date of Patent: October 22, 2013
    Assignee: Bayer CropScience AG
    Inventors: Hartmut Ahrens, Andreas Van Almsick, Elmar Gatzweiler, Dieter Feucht, Isolde Haeuser-Hahn, Stefan Lehr, Christopher Hugh Rosinger
  • Patent number: 8501773
    Abstract: The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
    Type: Grant
    Filed: June 28, 2006
    Date of Patent: August 6, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Craig W. Lindsley, William D. Shipe, Zhiqiang Yang, David Wisnoski
  • Patent number: 8501777
    Abstract: The present invention relates to compounds having therapeutic effects against disorders in the central nervous system, and in particular substituted phenylpiperidines of the formula 1: wherein R is as defined herein.
    Type: Grant
    Filed: October 12, 2006
    Date of Patent: August 6, 2013
    Assignee: NSAB, Filial AF Neurosearch Sweden AB, Sverige
    Inventor: Clas Sonesson
  • Patent number: 8470816
    Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B is an aromatic ring optionally having substituent(s), ring C is a cyclic group optionally having substituent(s), R1 is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group, a heterocyclic group optionally having substituent(s) or an amino group optionally having substituent(s), R2 is an optionally halogenated C1-6 alkyl group, m and n are each an integer of 0 to 5, m+n is an integer of 2 to 5, and is a single bond or a double bond, or a salt thereof and the like. Since the compound has a superior tachykinin receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of various diseases such as lower urinary tract diseases, gastrointestinal diseases, central nervous system diseases and the like.
    Type: Grant
    Filed: December 2, 2008
    Date of Patent: June 25, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yoshinori Ikeura, Junya Shirai, Hideyuki Sugiyama, Yuji Nishikimi, Taku Kamei, Nobuki Sakauchi
  • Patent number: 8461184
    Abstract: The present invention relates to sulphur containing pyrazole derivatives, and their S-oxidized active metabolites, as selective cannabinoid CB1 receptor antagonists having a high CB1/CB2 receptor subtype selectivity, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of these pyrazole derivatives, to pharmaceutical compositions comprising one or more of these pyrazole derivatives as active ingredients, as well as to the use of these pharmaceutical compositions for the treatment of psychiatric and neurological disorders. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: June 11, 2013
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Josephus H. M. Lange, Cornelis G. Kruse, Bernard J. Vliet Van
  • Publication number: 20130131079
    Abstract: The present invention is directed to a compound of formula (I) for use in a method to treat or ameliorate amyloid or tau pathologies, such as Alzheimer's disease, or symptoms thereof. The invention is also directed to new compounds of formula (I), of subformula (II), (III), (IV), or (V).
    Type: Application
    Filed: May 23, 2011
    Publication date: May 23, 2013
    Applicant: FAES FARMA, S.A.
    Inventors: Francisco Ledo Gómez, Ana Muñoz Muñoz, Carmen Pumar Durán
  • Patent number: 8440697
    Abstract: The invention relates to perhexiline, or a pharmaceutically acceptable salt thereof, for use in the treatment of HfnEF, as well as to a method of treating HfnEF, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said HFnEF. The invention further relates to a treatment program for treating HFnEF, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating HFnEF or the symptoms thereof.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: May 14, 2013
    Assignee: Heart Metabolics Limited
    Inventors: Houman Ashrafian, Michael P. Frenneaux
  • Patent number: 8420637
    Abstract: The present invention provides a method of treating glaucoma or ocular hypertension which comprises applying to the eye of a person in need thereof an amount sufficient to treat glaucoma or ocular hypertension of a compound of formula I wherein Y, Q, Z, R, R1 and R2 are as defined in the specification. The present invention further comprises pharmaceutical compositions, e.g. ophthalmic compositions, including said compound of formula I.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: April 16, 2013
    Assignee: Allergan, Inc.
    Inventors: June Chen, Simon Pettit, Hans Fliri
  • Patent number: 8410137
    Abstract: The subject matter of the invention is compounds corresponding to formula (I), in which: R1 and R2, together with the nitrogen atom to which they are attached, constitute a saturated heterocyclic radical containing from 4 to 7 atoms, which is preferably substituted; one of the two substituents R3 and R6 is a group Y-A-R9; Y is an oxygen atom or an —S(O)n?—, or —OSO2 group; A is an unsubstituted (C1-C4) alkylene group; R9 is an —OR19, —CH3, —NR19R20, —CONR19R20, —NR15COR19, —S(O)nR21, or —NR13SO2R21 group; —R10 is a hydrogen atom or a (C1-C4) alkyl group. The present invention also relates to the methods of preparation and the therapeutic uses of the compounds of formula (I).
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: April 2, 2013
    Assignee: Sanofi
    Inventors: Francis Barth, Jean-Philippe Ducoux, Patrick Gueule, Murielle Rinaldi-Carmona, Arnaud Rouquette
  • Patent number: 8399497
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: November 23, 2010
    Date of Patent: March 19, 2013
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Publication number: 20130045165
    Abstract: 4-Fluoro-4-phenylpiperidin-1-yl ? antagonists of general structure as well as pharmaceutical compositions comprising compounds of formula I, are disclosed. These compounds and compositions are useful as treatments of conditions or diseases associated with binding opioid receptors including pain, obesity, hyperalgesia, inflammation, osteoarthritis, drug addiction, and cancer. These compounds and compositions are also useful as treatments for tardive dyskinesia.
    Type: Application
    Filed: April 29, 2011
    Publication date: February 21, 2013
    Applicant: KINENTIA BIOSCIENCES, LLC
    Inventor: David J. Fairfax
  • Patent number: 8377935
    Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: November 22, 2011
    Date of Patent: February 19, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Patrick René Angibaud, Laurence Françoise Bernadette Marconnet-Decrane, Sven Franciscus Anna Van Brandt, Isabelle Noëlle Constance Pilatte
  • Patent number: 8343967
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: January 1, 2013
    Assignee: Abbott Laboratories
    Inventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
  • Patent number: 8324250
    Abstract: The present application relates to compounds of formula wherein the definitions are as described herein. The present compounds are high potential NK-3 receptor antagonists that are useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: December 4, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Walter Vifian
  • Patent number: RE44768
    Abstract: A compound of the structure wherein R1 and R2 are each, independently, hydrogen or —CO(CR3R4)b(CR5R6)dCR7R8R9; R3 and R4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or —F; R5 and R6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, —(CR3R4)fOR10, —CF3, —F, or —CO2R11, or R5 and R6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with —(CR3R4)fOR10; R7 is hydrogen, alkyl, alkenyl, alkynyl, —(CR3R4-)fOR10, —CF3, —F, or CO2R11; R8 and R9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, —(CR3R4)fOR10, —CF3, —F, or —CO2R11, or R8 and R9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with —(CR3R4-)fOR10; R10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl; R11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl; X is
    Type: Grant
    Filed: June 28, 2013
    Date of Patent: February 18, 2014
    Assignee: Wyeth LLC
    Inventors: Jerauld S. Skotnicki, Christina L. Leone, Guy A. Schiehser