Ring Nitrogen In The Polycyclo Ring System Patents (Class 514/339)
  • Patent number: 10703717
    Abstract: A novel type of water-soluble isatin derivatives, and manufacturing method and application thereof. An isatin derivative comprising a phenolic hydroxy group is used as the substrates. A dimethylaminomethylene group is introduced to an ortho position of the phenolic hydroxy group to significantly improve the water solubility of a class of compounds provided by the invention. An antitumor activity study showed that the activity of the class of compounds was not reduced, and even improved. The class of compounds has great prospects for applications in developing an antitumor pharmaceutical product.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: July 7, 2020
    Assignee: Tianjin University of Science & Technology
    Inventors: Peng Yu, Dong Wang, Yuou Teng, Longfei Miao, Jing Wang, Qian Zhang, Yuan Yuan
  • Patent number: 10669296
    Abstract: This invention features compounds that modulate the activity of liver X receptors, pharmaceutical compositions including the compounds of the invention, and methods of utilizing those compositions for modulating the activity of liver X receptors in the treatment of cancer.
    Type: Grant
    Filed: January 9, 2015
    Date of Patent: June 2, 2020
    Assignee: Rgenix, Inc.
    Inventors: Eduardo J. Martinez, Bernd Kaiser, Sohail F. Tavazoie, Isabel Kurth, Foster Casimir Gonsalves, David M. Darst, Jr., Masoud Fakhr Tavazoie
  • Patent number: 10654827
    Abstract: The present disclosure relates to a compound of formula (Ia), (Ib), (IIa), and (IIb): which are useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Grant
    Filed: June 25, 2018
    Date of Patent: May 19, 2020
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Steven J. Henry, John O. Link, Roland D. Saito, Scott D. Schroeder, Dimitrios Stefanidis, Winston C. Tse, Jennifer R. Zhang
  • Patent number: 10383850
    Abstract: The present invention provides compounds of formula (I), wherein A1, A2, Z1, Z2, Z3, R1, R2, R3, R4, R5, R6, n, p and q are as defined herein. In certain embodiments, the compounds of the invention are ROR?t antagonists. In other embodiments, the compounds of the invention are useful in the treatment and/or prevention of inflammatory and autoimmune conditions.
    Type: Grant
    Filed: October 23, 2015
    Date of Patent: August 20, 2019
    Assignee: ORCA PHARMACEUTICALS LIMITED
    Inventors: Clive McCarthy, Naomi Went, Roine Inge Olsson
  • Patent number: 10385041
    Abstract: A novel terpene derivative-based PAR1 inhibitor, a preparation method thereof and a pharmaceutical composition including the same or a salt thereof, as well as a use of the PAR1 inhibitor and the salt thereof in preparation of medicaments for preventing and/or treating thrombotic diseases. The structural formula of the compound is as follows: The compound has the advantages of clear target, novel structure, low bleeding risk, high safety, outstanding active effect, low preparation cost and the like, and has a great application prospect in the preparation of the medicaments for treating the thrombotic diseases.
    Type: Grant
    Filed: January 14, 2016
    Date of Patent: August 20, 2019
    Assignee: SHANDONG UNIVERSITY
    Inventors: Hongxiang Lou, Bin Sun, Jun Liu
  • Patent number: 10308642
    Abstract: An anti-hepatitis B virus agent comprising a compound represented by general formula [1], wherein R1 represents an aryl group, which may be substituted, or the like; R2 represents an aryl group, which may be substituted, or the like; and R3 represents a hydrogen atom or the like; or a salt thereof.
    Type: Grant
    Filed: October 5, 2016
    Date of Patent: June 4, 2019
    Assignees: FUJIFILM Toyama Chemical Co., Ltd., PUBLIC UNIVERSITY CORPORATION NAGOYA CITY UNIVERSITY
    Inventors: Kazuki Shimane, Yasuhito Tanaka
  • Patent number: 10251864
    Abstract: The present invention is directed to indole derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.
    Type: Grant
    Filed: September 5, 2017
    Date of Patent: April 9, 2019
    Assignee: JANSSEN PHARMACEUTICA NV
    Inventors: Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
  • Patent number: 10239833
    Abstract: The present invention provides novel process for the preparation of the ?1-adrenoceptor antagonists, Silodosin and its pharmaceutically acceptable salts indoline compounds, utilizing derivatives of Formula 1 and salts thereof.
    Type: Grant
    Filed: December 5, 2017
    Date of Patent: March 26, 2019
    Assignee: MANKIND PHARMA LTD.
    Inventors: Gurpreet Singh, Kuldeep Singh Gangwar, Bhuwan Bhashkar, Anil Kumar
  • Patent number: 9872854
    Abstract: Methods of treating, managing or preventing psoriatic arthritis are disclosed. Specific methods encompass the administration of apremilast, alone or in combination with a second active agent.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: January 23, 2018
    Assignee: Celgene Corporation
    Inventor: Robert Day
  • Patent number: 9796694
    Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.
    Type: Grant
    Filed: July 10, 2014
    Date of Patent: October 24, 2017
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Helen E. Blackwell, Grant D. Geske, Jennifer C. Campbell Butler
  • Patent number: 9718775
    Abstract: Compounds that are derivatives of oxindole conform to the general structure of Formula (I) These compounds are believed to exhibit antioxidant properties. A composition comprises an organic material and a compound conforming to the structure of Formula (I).
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: August 1, 2017
    Assignee: Milliken & Company
    Inventors: Sanjeev K. Dey, Eduardo Torres, Suchitra Datta, Mary E. Mason, Philip G. Harris
  • Patent number: 9604975
    Abstract: Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1-C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, —N(R11)—R12, -Alk-N(R11)—R12, —O-Alk-N(R11)—R12, —C(?O)OH, carboxy-(C1-C3)-alkyl, or —C(?O)—NH—R13; Alk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(?O)—N(—R16)— or —N(—R17)—C(?O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substitu
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: March 28, 2017
    Assignee: Vernalis (R&D) Ltd
    Inventors: Stephen Stokes, Nicolas Foloppe, Andrea Fiumana, Martin Drysdale, Simon Bedford, Paul Webb
  • Patent number: 9593096
    Abstract: The present invention relates to chemical compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7 nAChR).
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: March 14, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Andrew Harvey, Belinda Huff, Rajinder Singh, Nathan Kuchel
  • Patent number: 9284322
    Abstract: Provided herein are compounds and methods of preparation of compounds that are capable of functioning as agonists or antagonists of a nicotinic receptor. Also provided are pharmaceutical compositions comprising one or more of these compounds, which may further comprise one or more additional therapeutic agents. Further provided are methods of treatment of various conditions that may be responsive to such activity at the nicotinic receptors, such as nicotine dependence.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: March 15, 2016
    Assignee: Research Triangle Institute
    Inventors: Frank Ivy Carroll, Pauline Wanjiku Ondachi
  • Patent number: 9120776
    Abstract: The present invention provides a fused heterocyclic compound having an ROR?t inhibitory action. The present invention relates to a compound represented by the formula (I?): wherein each symbol is as defined in the specification, provided that 2-(2-((4-cyanophenyl)amino)-2-oxoethoxy)-N-(9-ethyl-9H-carbazol-3-yl)acetamide and N-(4-cyanophenyl)-N?-(9-ethyl-9H-carbazol-3-yl)-3-methylpentanediamide are excluded, or a thereof.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: September 1, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Satoshi Yamamoto, Junya Shirai, Yoshiyuki Fukase, Yoshihide Tomata, Ayumu Sato, Atsuko Ochida, Kazuko Yonemori, Hideyuki Nakagawa
  • Patent number: 9040565
    Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: May 26, 2015
    Assignee: Orexo AB
    Inventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer, Juergen Mack, Dirk Stenkamp
  • Publication number: 20150141456
    Abstract: The present invention relates to tertiary amines of formula (I) for use in therapy, particularly for use in treating cardiovascular disorders. The compounds have been found to regulate phospholamban phosphorylation by interfering with the A-kinase anchor protein 18delta (AKAP18?) binding to the PKA substrate phospholamban. The compounds share a tri(alkylaryl/alkylheteroaryl) amine structure.
    Type: Application
    Filed: November 20, 2014
    Publication date: May 21, 2015
    Inventors: Jo Klaveness, Kjetil Tasken
  • Publication number: 20150133505
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein R1 is phenyl, which is optionally substituted by 1-2 halogen atoms; selected from fluorine or chlorine; or to a pharmaceutically acceptable acid addition salt in enantiomerically pure form. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: January 15, 2015
    Publication date: May 14, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Patent number: 9028796
    Abstract: The present invention provides materials and methods to induce cell death by methuosis, a non-apoptotic cell death mechanism. Small molecules herein are useful for treating cell proliferation disorders or anomalies, particularly, but not exclusively, cancer. Methods related to the research and pharmaceutical use of the small molecules are also provided herein.
    Type: Grant
    Filed: February 24, 2012
    Date of Patent: May 12, 2015
    Assignee: The University of Toledo
    Inventors: William A. Maltese, Paul W. Erhardt, Michael W. Robinson, Jean H. Overmeyer
  • Patent number: 9029399
    Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: May 12, 2015
    Assignee: Novartis AG
    Inventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Saumitra Sengupta
  • Publication number: 20150126485
    Abstract: The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Patent number: 9023871
    Abstract: The present invention provides materials and methods to induce cell death by methuosis, a non-apoptotic cell death mechanism, to induce vacuolization without cell death, or to induce cell death without vacuolization. Small molecules herein are useful for treating cell proliferation disorders or anomalies, particularly, but not exclusively, cancer. Methods related to the research and pharmaceutical use of the small molecules are also provided herein.
    Type: Grant
    Filed: April 7, 2014
    Date of Patent: May 5, 2015
    Assignee: The University of Toledo
    Inventors: William A. Maltese, Paul W. Erhardt, Christopher Trabbic, Jean H. Overmeyer
  • Publication number: 20150119402
    Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 30, 2015
    Inventor: Derk Hogenkamp
  • Publication number: 20150111890
    Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof,that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: April 19, 2013
    Publication date: April 23, 2015
    Inventors: Lisa A. Hasvold, Dachun Liu, Chang Hoon Park, John K. Pratt, George S. Sheppard, Le Wang
  • Patent number: 9012445
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20150105393
    Abstract: The present invention relates to amide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 16, 2015
    Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Mikio Morita
  • Publication number: 20150105386
    Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).
    Type: Application
    Filed: October 24, 2014
    Publication date: April 16, 2015
    Inventors: Helmut Mack, Nicole Teusch, Bernhard K. Muller, Wilfried Hornberger, Michael F. Jarvis, Daryl Sauer, Steven L. Swann, Jr., Dominique Bonafoux, Ryan Keddy, Adrian Donald Hobson, Anil Vasudevan
  • Patent number: 9006276
    Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: April 14, 2015
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
  • Publication number: 20150099782
    Abstract: Provided herein are antagonists of prostaglandin EP3 receptor, processes to make said antagonists, and methods comprising administering said antagonists to a mammal in need thereof.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Applicant: PFIZER INC.
    Inventors: Kevin Barry Bahnck, David James Edmonds, Kentaro Futatsugi, Esther Cheng Yin Lee, Alan Martin Mathiowetz, Elnaz Menhaji-Klotz, Robert Vernon Stanton
  • Publication number: 20150099747
    Abstract: The invention comprises reagents and methods for detecting cancer-associated mutations in the human EZH2 gene. Further, a method of detecting the mutations and a method of treatment are disclosed.
    Type: Application
    Filed: October 7, 2014
    Publication date: April 9, 2015
    Inventors: Xiaoju Max Ma, Chitra Manohar, Alison Tsan
  • Publication number: 20150099736
    Abstract: Compounds of formula (I) have checkpoint kinase 1 (CHK1) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, trifluoromethoxy, methylamino and dimethylamino; R3, and R4 are independently selected from hydrogen, hydroxy, C1-C3 alkyl, fluoro-(C1-C3)-alkyl, hydroxy-(C1-C3)-alkyl, C1-C3 alkoxy, fluoro-(C1-C3)-alkoxy, hydroxy-(C1-C3)-alkoxy, —N(R11)—R12, -Alk-N(R11)—R12, —O-Alk-N(R11)—R12, —C(?O)OH, carboxy-(C1-C3)-alkyl, or —C(?O)—NH—R13; Alk is a straight or branched chain divalent C1-C6 alkylene radical; R7 and R8 are independently selected from hydrogen, hydroxy, or C1-C3 alkoxy; X is a straight chain divalent C1-C3 alkylene radical, optionally substituted on one or more carbons by R9 and/or R10; W is selected from —C(?O)—N(—R16)— or —N(—R17)—C(?O)—; Y is hydrogen, C1-C3 alkyl, C1-C3 alkoxy, or halo; and Q is selected from optionally substituted phenyl, optionally substituted cyclohexyl, or an optionally substitu
    Type: Application
    Filed: November 10, 2014
    Publication date: April 9, 2015
    Inventors: Stephen Stokes, Nicolas Foloppe, Andrea Fiumana, Martin Drysdale, Simon Bedford, Paul Webb
  • Publication number: 20150099758
    Abstract: The present application is related to compounds represented by Formula I, which are novel positive allosteric modulators of al nAChRs. The application also discloses the treatment of disorders that are responsive to enhancement of acetylcholine action on al nAChRs in a mammal by administering an effective amount of a compound of Formula I.
    Type: Application
    Filed: May 8, 2013
    Publication date: April 9, 2015
    Applicant: Anvyl LLC
    Inventors: David Putnam, Olivier Dasse
  • Patent number: 8987307
    Abstract: This invention relates to novel 3-aminopyridines of the formula wherein B1, B2 and R1 to R6 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.
    Type: Grant
    Filed: February 28, 2012
    Date of Patent: March 24, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Prabha Saba Karnachi, Kyungjin Kim, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ullmer
  • Patent number: 8987308
    Abstract: Disclosed are compounds of formula (I): or a pharmaceutically acceptable N-oxide, salt, hydrate, solvate, complex, bioisostere, metabolite or prodrug thereof, which are of use in the treatment of infection with, and diseases caused by, Clostridium difficile.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: March 24, 2015
    Assignee: Summit Corporation Plc
    Inventors: Peter David Johnson, Richard John Vickers, Francis Xavier Wilson, Colin Richard Dorgan, Lauren Jayne Sudlow, Stephen Paul Wren, Renate van Well
  • Patent number: 8987305
    Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: March 24, 2015
    Assignee: Aptose Biosciences Inc.
    Inventors: Raed H. Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon S. Lee
  • Publication number: 20150079154
    Abstract: The invention provides a pharmaceutical composition comprising Sorafenib in combination with an inhibitor of a specific kinase inhibitor as a medicament for the treatment or prevention of liver cancer.
    Type: Application
    Filed: July 9, 2012
    Publication date: March 19, 2015
    Applicant: HELMHOLTZ-ZENTRUM FUER INFEKTIONSFORSCHUNG GMBH
    Inventors: Lars Zender, Ramona Rudalska, Daniel Dauch
  • Patent number: 8980926
    Abstract: The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)—The values and preferred values of the variables in Structural Formula I are defined herein.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: March 17, 2015
    Assignees: Genzyme Corporation, President and Fellows of Harvard College, Massachusetts Institute of Technology
    Inventors: Ralph Mazitschek, Jon C. Clardy, Dyann Wirth, Roger Wiegand, Sameer Urgaonkar, Mary Lynn Baniecki, Joseph Cortese, Cassandra Celatka, Yibin Xiang, Renato Skerlj, Elyse M. J. Bourque
  • Patent number: 8980927
    Abstract: Compounds of general formula (II) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(?O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C?O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: March 17, 2015
    Assignee: Atopix Therapeutics Limited
    Inventors: Richard Edward Armer, Eric Roy Pettipher, Mark Whittaker, Graham Michael Wynne, Julia Vile, Frank Schroer
  • Publication number: 20150072859
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.
    Type: Application
    Filed: November 19, 2014
    Publication date: March 12, 2015
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Noormohamed M. Niyaz, Negar Garizi, Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse, Asako Kubota, Paul R. LePlae, Jr., Daniel Knueppel, Christian T. Lowe, Dan Pernich, David A. Demeter, Timothy C. Johnson
  • Publication number: 20150065477
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 5, 2015
    Inventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Möller, Wilfried Hornberger, Gisela Backfisch, Yanbin Lao, Marjoleen Nijsen
  • Patent number: 8969383
    Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Grant
    Filed: June 12, 2014
    Date of Patent: March 3, 2015
    Assignee: RaQualia Pharma Inc.
    Inventors: Hirohide Noguchi, Tadashi Inoue, Mikio Morita, Yoshimasa Arano
  • Publication number: 20150057301
    Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protectiong from neuron cell death.
    Type: Application
    Filed: July 24, 2014
    Publication date: February 26, 2015
    Inventors: Steven L. McKnight, Joseph M. Ready, Andew A. Pieper, Jef K. De Brabander
  • Publication number: 20150051177
    Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Inventor: Darren Orton
  • Patent number: 8957070
    Abstract: The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof. According to the present invention, a glucokinase activator useful as a pharmaceutical agent such as agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like can be provided.
    Type: Grant
    Filed: April 20, 2006
    Date of Patent: February 17, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuneo Yasuma, Osamu Ujikawa
  • Patent number: 8957093
    Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit kinase-mediated, e.g., cdk5-mediated, phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. In methods of treatment of these conditions using a compound of the invention, the compound can avoid producing side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, in the patient receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
    Type: Grant
    Filed: June 6, 2012
    Date of Patent: February 17, 2015
    Assignee: The Scripps Research Institute
    Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Marcel Koenig, Alice Asteian, Anne-Laure Blayo, Yuanjun He, Youseung Shin
  • Publication number: 20150045395
    Abstract: This invention relates to methods of reversing and inhibiting liver fibrosis and hepatitis using a small indolinone molecule Hesperadin and related compounds. Methods of identifying such agents and using them to inhibit the expression of collagens and ECM proteins including MMPs and TIMPs in purified hepatic stellate cells are provided. In vivo data of Hesperadin in inhibiting induced collagen production are presented. This method of specifically targeting drugs to hepatic stellate cells in vivo, provides a novel therapy for liver diseases.
    Type: Application
    Filed: August 9, 2013
    Publication date: February 12, 2015
    Applicant: Acclaim BioMed USA LLC
    Inventors: Kenneth Ka-Ho Lee, Stanton Hon-Lung Kok, Tsz-Wai Kok, Sing-Wan Wong, John Yeuk-Hon Chan
  • Publication number: 20150045362
    Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.
    Type: Application
    Filed: August 25, 2014
    Publication date: February 12, 2015
    Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford
  • Publication number: 20150038517
    Abstract: This invention relates to modulation of the ?7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a salt thereof: wherein R1 is imidazolyl, pyridinyl or pyrimidinyl, any of which is optionally substituted by one group independently selected from C1-3alkyl and C1-3alkoxy.
    Type: Application
    Filed: August 7, 2014
    Publication date: February 5, 2015
    Inventor: Kevin Dinnell
  • Patent number: RE47333
    Abstract: The present invention relates to stable and bioavailable immediate release formulations comprising dopamine receptor ligands. Methods of treating various disorders by administering the formulations are also described.
    Type: Grant
    Filed: May 18, 2017
    Date of Patent: April 2, 2019
    Assignee: Richter Gedeon Nyrt.
    Inventors: Ranajoy Sarkar, Mahendra G. Dedhiya, Anil Chhettry
  • Patent number: RE47350
    Abstract: The present invention relates to stable and bioavailable immediate release formulations comprising dopamine receptor ligands. Methods of treating various disorders by administering the formulations are also described.
    Type: Grant
    Filed: May 18, 2017
    Date of Patent: April 16, 2019
    Assignee: Richter Gedeon Nyrt.
    Inventors: Ranajoy Sarkar, Mahendra G. Dedhiya, Anil Chhettry