1,2,5-thiadiazoles (including Hydrogenated) Patents (Class 514/362)
  • Patent number: 10987322
    Abstract: Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: April 27, 2021
    Assignee: Flexus Biosciences, Inc.
    Inventors: Juan Carlos Jaen, Maksim Osipov, Jay Patrick Powers, Hunter Paul Shunatona, James Ross Walker, Mikhail Zibinsky
  • Patent number: 10639374
    Abstract: An object of the present invention is to provide a patch preparation having an excellent skin permeability of medicament using an acid additional salt of basic medicament. Provided is a patch preparation comprising a support and an adhesive layer on one surface of the support, wherein the adhesive layer contains a basic medicament, a fatty acid-based ionic liquid, and potassium salts and/or potassium ions. Said potassium salts and/or potassium ions are generated as a result of reaction of an acid addition salt of the basic medicament with a compound capable of generating potassium ion in the adhesive layer.
    Type: Grant
    Filed: June 7, 2018
    Date of Patent: May 5, 2020
    Assignee: MEDRx CO., LTD
    Inventors: Hidetoshi Hamamoto, Takahiro Tanimoto
  • Patent number: 10561619
    Abstract: The present invention relates to a pharmaceutical composition comprising dutasteride and propylene glycol monolaurate, which improves the stability of dutasteride, which is a poorly soluble drug as a 5-alpha reductase inhibitor, and a process for its preparation. More particularly, the present invention also relates to a capsule formulation which is smaller in size than a commercial dutasteride capsule formulation (AVODART®), but has the equivalent dissolution rate by preparing a pharmaceutical composition comprising propylene glycol monolaurate and dutasteride, which can improve the stability of the dutasteride. A dutasteride formulation having enhanced patient's compliance and improved stability and a method for producing the same are provided.
    Type: Grant
    Filed: December 29, 2016
    Date of Patent: February 18, 2020
    Assignee: Yuyu Pharma, Inc.
    Inventors: Tae Gon Baik, Seyeon Kim, Kyeongjin Ahn, Ju-Hee Kim, Young-Joon Park
  • Patent number: 10280157
    Abstract: The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N?-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.
    Type: Grant
    Filed: December 22, 2017
    Date of Patent: May 7, 2019
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Ming Tao, William Frietze, David J. Meloni, Lingkai Weng, Jiacheng Zhou, Yongchun Pan
  • Patent number: 9994518
    Abstract: Disclosed are compounds of Formula (IVA), or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof: Formula (IVA), wherein “RIa”, “RIb”, “RIc”, “RId”, “RIe”, are defined herein above, which compounds are believed suitable for use in positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7 nAChR) receptors, for example, those found in the cerebral cortex and the hippocampus. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Alzheimer's disease (AD), schizophrenia, and Parkinson's disease (PD), or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.
    Type: Grant
    Filed: June 11, 2015
    Date of Patent: June 12, 2018
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Kenneth Leavitt, Brendan Crowley, Ian M. Bell, Andrew Harvey, Thomas Avery, Dharam Paul, Justin Ripper, Belinda Huff, Rajinder Singh, Laurent Schaeffer, Christophe Joseph, Christophe Morice, Bruno Giethlen, Patrick Bazzini, Aurelie Fromeyer
  • Patent number: 9949961
    Abstract: The invention relates to a novel agent in the form of rhodanine derivatives, which has prophylactic, antiproliferative and antimetastatic activity. Said agent can find use in medicine and pharmacology for the prophylaxis and/or treatment of neoplastic diseases of variable localization.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: April 24, 2018
    Inventors: Rahimdzhan Roziev, Anna Ya. Goncharova, Kenes T. Erimbetov, Vladimir Podgorodnichenko, Victor Khomichenok, Natal'ja Novozhilova
  • Patent number: 9776994
    Abstract: The present invention relates to compounds of formula (I) wherein P is selected from P1 and P2, or P and R5 together are P3 or P is a heterocycle H, selected from H1 to H9 wherein Y1, Y2 and Y3 are independently of each other C—H, C—R5, or nitrogen; and G1, G2, G3, Z, R1, R2, R3, R4, R5, R6a, R6b, R7, R8, R9, R10, R11, p, n and k are as defined in the claims. The invention also relates to methods of controlling insects, acarines, nematodes or molluscs which comprises applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I).
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: October 3, 2017
    Assignee: Syngenta Participations AG
    Inventors: Long Lu, Jerome Yves Cassayre, Guillaume Berthon, Myriem El Qacemi, Yaming Wu
  • Patent number: 9649300
    Abstract: Compounds, or pharmaceutically acceptable salts or esters thereof, having a structure of: wherein each of R1-R5 is individually selected from H, halogen, optionally substituted alkyl, optionally substituted alkoxy, nitro, sulfonamide, hydroxy, or amino; and R6 is selected from H, optionally substituted alkyl, or optionally substituted aryl.
    Type: Grant
    Filed: August 19, 2014
    Date of Patent: May 16, 2017
    Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education, Chatham University
    Inventors: Abdelhadi Rebbaa, Robert B. Lettan, II
  • Patent number: 9422318
    Abstract: Compounds and compositions comprising epoxyeicosatrienoic acid (EET) analogs that act as EET agonists and are useful as medications in the treatment of drug-induced nephrotoxicity, hypertension and other related conditions. Methods of making and using the compounds and compositions are further described.
    Type: Grant
    Filed: July 30, 2015
    Date of Patent: August 23, 2016
    Assignees: The Medical College of Wisconsin, Inc., The Board of Regents of the University of Texas System
    Inventors: John David Imig, William B. Campbell, John Russell Falck
  • Patent number: 9339490
    Abstract: Embodiments of the invention generally relate to methods and supplements for increasing sex steroids and human growth hormone in a human being.
    Type: Grant
    Filed: June 10, 2014
    Date of Patent: May 17, 2016
    Inventors: Amy L. Heaton, Mitchell K. Friedlander, Dennis Gay
  • Patent number: 9181553
    Abstract: A method for treating breast cancer in a subject having a breast cancer over-expressing the “SHP2 signature” genes, as compared to normal breast tissue samples, which method comprises the step of administering to said subject a therapeutically effective amount of a modulator of the protein tyrosine phosphatase, non-receptor type 11 (PTPN11) gene or of its gene product (Shp2).
    Type: Grant
    Filed: June 5, 2012
    Date of Patent: November 10, 2015
    Assignee: NOVARTIS FORSCHUNGSSTIFTUNG ZWEIGNIEDERLASSUNG FRIEDRICH MIESCHER INSTITUTE FOR BIOMEDICAL RESEARCH
    Inventors: Mohamed Bentires-Alj, Nicola Aceto, Michael Stadler
  • Publication number: 20150141473
    Abstract: A pharmaceutical composition in liquid dosage form which contains a tizanidine hydrocloride aqueous solution suitable for parenteral, intranasal and oral administration.
    Type: Application
    Filed: June 5, 2014
    Publication date: May 21, 2015
    Applicant: MDM SpA
    Inventor: Massimiliano BORSA
  • Publication number: 20150119390
    Abstract: The present invention provides imidazothiadiazole compounds of Formula (I); Wherein W, Y, R0, R2, R4, Ra, Rb, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Application
    Filed: April 24, 2013
    Publication date: April 30, 2015
    Inventors: Alain Martel, François Tremblay, Anne Marinier, Eldon Scott Priestley, Shoshana L. Posy, R. Michael Lawrence, Michael M. Miller
  • Patent number: 9011910
    Abstract: A method of treating the symptoms of spasticity comprises implanting a reservoir-based drug delivery composition into a subject to systemically deliver a therapeutically effective amount of tizanidine to the subject for a long period of time (e.g., one month or one year). The drug delivery composition may include a rate-controlling excipient (e.g., an elastomeric polymer) defining a reservoir containing at least one discrete solid dosage form (e.g., one or more pellets), which includes tizanidine free base and optionally, a sorption enhancer.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: April 21, 2015
    Assignee: Braeburn Pharmaceuticals BVBA SPRL
    Inventor: Alexander Schwarz
  • Patent number: 8980837
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: March 17, 2015
    Assignee: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Patent number: 8980298
    Abstract: A method of treating the symptoms of spasticity comprises implanting a reservoir-based drug delivery composition into a subject to systemically deliver a therapeutically effective amount of tizanidine to the subject for a long period of time (e.g., one month or one year). The drug delivery composition may include a rate-controlling excipient (e.g., an elastomeric polymer) defining a reservoir containing at least one discrete solid dosage form (e.g., one or more pellets), which includes tizanidine free base and optionally, a sorption enhancer.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: March 17, 2015
    Assignee: Braeburn Pharmaceuticals BVBA SPRL
    Inventor: Alexander Schwarz
  • Publication number: 20150038539
    Abstract: An article and method for increasing the extent of tizanidine absorption in a patient receiving tizanidine therapy. Tizanidine may be administered in the form of an immediate release tablet composition at or around the time food is consumed. The composition may be packaged in a container for distribution.
    Type: Application
    Filed: March 5, 2014
    Publication date: February 5, 2015
    Applicant: Acorda Therapeutics, Inc.
    Inventors: Cara A. Pellegrini, Paul Stark
  • Publication number: 20150031719
    Abstract: The invention is directed to topical formulations and methods of treating a migraines and/or cluster headaches, muscle sprains, muscle spasms, spasticity, tension headaches, tension related migraines and related conditions associated with muscle tension and pain with a therapeutically effective amount of an ergot alkaloid, skeletal muscle relaxant, serotonin agonist, combinations thereof, pharmaceutically acceptable salt thereof, prodrugs thereof or derivative thereof.
    Type: Application
    Filed: October 10, 2014
    Publication date: January 29, 2015
    Inventor: Ronald AUNG-DIN
  • Patent number: 8933107
    Abstract: The present invention relates to aryloxy substituted phenylamidine derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions (I).
    Type: Grant
    Filed: September 12, 2006
    Date of Patent: January 13, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Klaus Kunz, Jörg Greul, Oliver Guth, Benoît Hartmann, Kerstin Ilg, Wahed Ahmed Moradi, Thomas Seitz, Peter Dahmen, Arnd Voerste, Ulrike Wachendorff-Neumann, Ralf Dunkel, Ronald Ebbert, Eva-Maria Franken, Olga Malsam
  • Publication number: 20140341985
    Abstract: An article and method for reducing somnolence in a patient receiving tizanidine therapy. Tizanidine may be administered in the form of an immediate release multiparticulate composition at or around the time food is consumed. The composition may be packaged in a container for distribution.
    Type: Application
    Filed: December 18, 2013
    Publication date: November 20, 2014
    Applicant: Acorda Therapeutics, Inc.
    Inventors: Cara A. PELLEGRINI, Paul Stark
  • Publication number: 20140341776
    Abstract: Thiophene containing water-soluble oligomers were synthesized and characterized. The photophysical properties of these compounds were studied; transient absorption spectroscopy was used to probe the triplet excited state and their ability to sensitize singlet oxygen was spectroscopically monitored in deuterated methanol. The above compounds were tested for their light activated biocidal properties against S. aureus both under UV and visible radiation. Among the oligomers studied, the terthiophene derivative was found to kill the bacteria efficiently.
    Type: Application
    Filed: July 5, 2012
    Publication date: November 20, 2014
    Applicants: STC.UNM, University of Florida Reearch Foundation, Inc.
    Inventors: Kirk S. Schanze, Anand Parthasarathy, Subhadip Goswami, David G. Witten, Eunkyung Ji, Thomas S. Corbitt, Dimitri Dascier
  • Patent number: 8883830
    Abstract: The invention is directed to topical formulations and methods of treating a migraines and/or cluster headaches, muscle sprains, muscle spasms, spasticity, tension headaches, tension related migraines and related conditions associated with muscle tension and pain with a therapeutically effective amount of an ergot alkaloid, skeletal muscle relaxant, serotonin agonist, combinations thereof, pharmaceutically acceptable salt thereof, prodrugs thereof or derivative thereof.
    Type: Grant
    Filed: January 13, 2012
    Date of Patent: November 11, 2014
    Assignee: Afgin Pharma LLC.
    Inventor: Ronald Aung-Din
  • Patent number: 8877748
    Abstract: A heterocyclic fused anthraquinone derivative, which is represented by a formula (I): wherein R1 is a substituent being one selected from a group consisting of hydrogen, halogens, aminoalkyl group, sulfoalkyl group, haloalkyl group, piperazino group, sulfonyl group, morpholino group, alkali group or one substituent represented by a formula (II): wherein R2 is amino group, oxyl group or a thiol group. In the meantime, a method for manufacturing the above-mentioned heterocyclic fused anthraquinone derivatives and a pharmaceutical composition using thereof are also disclosed here.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: November 4, 2014
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Yu-Ru Lee, Tsung-Chih Chen
  • Publication number: 20140315961
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
  • Patent number: 8859592
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, A5, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: October 14, 2014
    Assignee: Syngenta Corp Protection LLC
    Inventors: Peter Renold, Jerome Yves Cassayre, Jagadish Pabba, Myriem El Qacemi, Thomas Pitterna
  • Patent number: 8846727
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Patent number: 8841335
    Abstract: Provided is a pharmaceutical composition for inhibiting apoptosis of neurons or neurodegeneration. The pharmaceutical composition effectively prevents or treats diseases related to apoptosis of neurons or neurodegeneration.
    Type: Grant
    Filed: May 3, 2011
    Date of Patent: September 23, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Cheol Hyoung Park, Hye Kyung Min, In Suk Park, Mi Jung Lim, Ji Won Lee, Jin Yong Chung, Yeo Jin Yoon, Joo Young Park
  • Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • Publication number: 20140221383
    Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
    Type: Application
    Filed: April 14, 2014
    Publication date: August 7, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Hallet, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
  • Patent number: 8716320
    Abstract: The present invention provides novel heterocyclic urea compounds having useful antibacterial activity, pharmaceutical compositions comprising one or more of these compounds, methods of making the same, and methods of using the same.
    Type: Grant
    Filed: July 23, 2007
    Date of Patent: May 6, 2014
    Assignee: Replidyne, Inc.
    Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun
  • Publication number: 20140113891
    Abstract: Methods for treating cancer using compounds that inhibit human DNA ligases. Methods for using compounds that inhibit human DNA ligases to provide insights into the reaction mechanisms of human DNA ligases, for example to identify the human DNA ligase involved in different DNA repair pathways. Screening methods for compounds that inhibit human DNA ligases.
    Type: Application
    Filed: April 17, 2013
    Publication date: April 24, 2014
    Inventors: Alan E. Tomkinson, Xi Chen, Barbara Dziegielewska, Alexander D. Mackerell, Shijun Zhong, Gerald M. Wilson
  • Publication number: 20140100242
    Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
    Type: Application
    Filed: September 17, 2013
    Publication date: April 10, 2014
    Applicant: THE TRUSTEES OF PRINCETON UNIVERSITY
    Inventors: Bonnie Bassler, Lee Swem
  • Publication number: 20140079667
    Abstract: Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, RB and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.
    Type: Application
    Filed: August 23, 2013
    Publication date: March 20, 2014
    Applicant: Infinity Pharmaceuticals, Inc.
    Inventors: Adilah BAHADOOR, Alfredo C. Castro, Lawrence K. Chan, Gregg F. Keaney, Marta Nevalainen, Vesa Nevalainen, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Publication number: 20140080872
    Abstract: Use of phospho-Akt as a biomarker for predicting the response, such as resistance, to a compound, wherein phospho-Akt is Akt that has been phosphorylated on one or more residues, with the proviso that for Akt1, Akt2, and Akt3 the designation phospho-Akt is used to indicate phosphorylation at a site other than T308, T309 or T305 respectively, wherein the compound is a compound of general formula (I) wherein R represents phenyl, thienyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, cyano, halo
    Type: Application
    Filed: March 28, 2012
    Publication date: March 20, 2014
    Inventors: Heidi Alexandra Lane, Felix Bachmann
  • Patent number: 8664249
    Abstract: Tetrasubstituted benzenes that act as modulators of gamma secretase and their use in the treatment of one or more symptoms of treating neurodegenerative disorders, e.g., Alzheimer's disease, are described.
    Type: Grant
    Filed: February 1, 2013
    Date of Patent: March 4, 2014
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Gideon Shapiro, Richard Chesworth
  • Publication number: 20140057871
    Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or the like. [Means of solving the problem] A compound of Formula (III): (where f is 0 to 2; g is 1 to 4; j is 0 to 3; k is 0 to 2; n is 0 to 2; p is 0 to 4; h is 0 to 3; q1 id 0 to 3; q2 is 0 or 1; r1 is 0 to 2 (with the proviso that q1+q2+r1 is 0 to 5); J1a is —CR11a—, N; J2 is —CR12aR12b—, —CR12c—; T is —CH2—, O, —S(O)i— (i is an integer of 0 to 2) or —NR7—; X is O, S, or —NR7—; ring A?? is a benzene ring, a pyridine ring; ring B? is a benzene ring, a pyridine ring, a pyrimidine ring; and R1 to R14 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
    Type: Application
    Filed: April 11, 2012
    Publication date: February 27, 2014
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
  • Publication number: 20140024636
    Abstract: Provided is a sulfamide derivative having an adamantyl group represented by the following Formula 1, or a pharmaceutically acceptable salt thereof. The sulfamide derivative suppresses the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1), and is useful in the treatment of various diseases that are mediated by 11?-HSD1.
    Type: Application
    Filed: March 30, 2012
    Publication date: January 23, 2014
    Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Ki Young Kim, Jin Hee Ahn, Seung Kyu Kang, Sang Dal Rhee, Myung Ae Bae, Sung Hoon Ahn, Hee Youn Kim, Won Hoon Jung, Nam Sook Kang
  • Publication number: 20130338200
    Abstract: A pharmaceutical composition in liquid dosage form which contains a tizanidine hydrocloride aqueous solution suitable for parenteral, intranasal and oral administration.
    Type: Application
    Filed: June 13, 2012
    Publication date: December 19, 2013
    Applicant: MDM SpA
    Inventor: Massimiliano BORSA
  • Patent number: 8592486
    Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: May 14, 2012
    Date of Patent: November 26, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Shoujun Chen, Zhi-Qiang Xia, Jun Jiang, Yu Xie, Junyi Zhang
  • Patent number: 8580799
    Abstract: The present invention relates to hydroximoyl-heterocycle derivatives of formula (I) wherein T represents a substituted or non-substituted heterocyclyl group, Q represents a carbo or heterocyclic group, A represent a carbo or heterocyclic group or a carbo or hetero-polycylic group, and L1 represents various linking groups, their process of preparation, intermediate compounds for their preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: November 12, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
  • Publication number: 20130289028
    Abstract: A heterocyclic fused anthraquinone derivatives, which is represented by a formula (I): wherein R1 is a substituent being one selected from a group consisting of hydrogen, halogens, aminoalkyl group, sulfoalkyl group, haloalkyl group, piperazino group, sulfonyl group, morpholino group, alkali group or one substituent represented by a formula (II): wherein R2 is amino group, oxyl group or a thiol group. In the meantime, a method for manufacturing the above-mentioned heterocyclic fused anthraquinone derivatives and a pharmaceutical composition using thereof are also disclosed here.
    Type: Application
    Filed: March 1, 2013
    Publication date: October 31, 2013
    Applicant: NATIONAL DEFENSE MEDICAL CENTER
    Inventors: Hsu-Shan HUANG, Yu-Ru LEE, Tsung-Chih CHEN
  • Publication number: 20130259934
    Abstract: A method of treating the symptoms of spasticity comprises implanting a reservoir-based drug delivery composition into a subject to systemically deliver a therapeutically effective amount of tizanidine to the subject for a long period of time (e.g., one month or one year). The drug delivery composition may include a rate-controlling excipient (e.g., an elastomeric polymer) defining a reservoir containing at least one discrete solid dosage form (e.g., one or more pellets), which includes tizanidine free base and optionally, a sorption enhancer.
    Type: Application
    Filed: May 22, 2013
    Publication date: October 3, 2013
    Applicant: Endo Pharmaceuticals Solutions Inc.
    Inventor: Alexander SCHWARZ
  • Patent number: 8541596
    Abstract: Novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: September 24, 2013
    Assignee: Probiodrug AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Torsten Hoffmann, Livia Boehme
  • Publication number: 20130245072
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, A5, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: May 10, 2013
    Publication date: September 19, 2013
    Applicant: SYNGENTA CORP PROTECTION LLC
    Inventors: Peter Renold, Jerome Yves Cassayre, Jagadish Pabba, Myriem El Qacemi, Thomas Pitterna
  • Publication number: 20130236539
    Abstract: An article and method for reducing somnolence in a patient receiving tizanidine therapy. Tizanidine may be administered in the form of an immediate release multiparticulate composition at or around the time food is consumed. The composition may be packaged in a container for distribution.
    Type: Application
    Filed: August 28, 2012
    Publication date: September 12, 2013
    Inventors: Cara A. Pellegrini, Paul Stark
  • Patent number: 8524749
    Abstract: The present invention relates to a novel controlled release formulations of tizanidine. The invention also provides methods of using novel controlled release formulations of tizanidine to treat a patient.
    Type: Grant
    Filed: January 16, 2008
    Date of Patent: September 3, 2013
    Assignee: ALZA Corporation
    Inventors: Scott Bull, Suneel Gupta, Rhea Donley, Nishit Modi, Noymi Yam
  • Publication number: 20130210869
    Abstract: An article and method for increasing the extent of tizanidine absorption in a patient receiving tizanidine therapy. Tizanidine may be administered in the form of an immediate release tablet composition at or around the time food is consumed. The composition may be packaged in a container for distribution.
    Type: Application
    Filed: September 13, 2012
    Publication date: August 15, 2013
    Inventors: Cara A. PELLEGRINI, Paul Stark
  • Publication number: 20130203592
    Abstract: This document discloses molecules having the following formulas (“Formula One” &“Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.
    Type: Application
    Filed: January 22, 2013
    Publication date: August 8, 2013
    Applicant: Dow AgroSciences LLC
    Inventor: Dow AgroSciences LLC
  • Publication number: 20130203593
    Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.
    Type: Application
    Filed: January 23, 2013
    Publication date: August 8, 2013
    Applicant: Dow AgroSciences LLC
    Inventor: Dow AgroSciences LLC
  • Publication number: 20130203739
    Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (1): (where n is 0 to 2; p is 0 to 4; h is 0 to 3; j is 0 to 3; k is 0 to 2; a ring B is an aryl group or a heteroaryl group; X is O, S, or —NR7—; J1 is —CR11aR11b— or —NR11c—; J2 is —CR12aR12b— or —NR12c—; and R1 to R12c are specific groups), a salt of the compound, or a solvate of the salt or the compound.
    Type: Application
    Filed: October 11, 2011
    Publication date: August 8, 2013
    Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe