The Five-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/143)
  • Patent number: 10364221
    Abstract: A monomer, an organic layer composition, an organic layer, and a method of forming a pattern, the monomer being represented by the following Chemical Formula 1:
    Type: Grant
    Filed: June 8, 2016
    Date of Patent: July 30, 2019
    Assignee: SAMSUNG SDI CO., LTD.
    Inventors: Hyo Young Kwon, Sunhae Kang, Ran Namgung, Younhee Nam, Yumi Heo, Young Min Kim, Soohyoun Mun
  • Patent number: 9572794
    Abstract: Embodiments of the invention include substituted indole compounds and compositions thereof to inhibit protease activated receptor-4. Also described are methods of preparation of compositions and methods for treating diseases related to thrombotic disorders by administration of the composition.
    Type: Grant
    Filed: August 6, 2015
    Date of Patent: February 21, 2017
    Assignee: Vanderbilt University
    Inventors: Heidi E. Hamm, Shaun R. Stauffer, Craig W. Lindsley, Wandong Wen, Summer E. Young, Matthew T. Duvernay, Kayla J. Temple
  • Patent number: 9556166
    Abstract: The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: January 31, 2017
    Assignee: Proteostasis Therapeutics, Inc.
    Inventors: Megan Foley, Bradley Tait, Matthew Cullen
  • Patent number: 9079895
    Abstract: The invention relates to morpholino-derivatives according to Formula (I) or stereoisomers or pharmaceutically acceptable salts or solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, m and n are as defined in the specification. The compounds are antagonists, reverse agonists or agonists of G-protein coupled receptors, such as dopamine D4 and 5HT1a. The inventions also relates to pharmaceutical compositions comprising the compounds and methods involving the compounds and compositions. The compounds and compositions of the invention may in particular be used in the treatment of diseases and disorders, such as neurological and neurodegenerative diseases; or as lead compounds for the design and selection of further therapeutic compounds.
    Type: Grant
    Filed: November 20, 2013
    Date of Patent: July 14, 2015
    Assignee: University of Dundee
    Inventors: Jeremy Besnard, Andrew Lee Hopkins, Ian Gilbert, Gian Filippo Ruda, Keren Abecassis
  • Publication number: 20150111886
    Abstract: The invention relates to a compound of formula (I) wherein A1, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Atsushi Kimbara, Uwe Grether, Matthias Nettekoven, Bernd Puellmann, Mark Rogers-Evans, Tanja Schulz-Gasch
  • Publication number: 20150105384
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1, HDAC2, and/or HDAC6. Also provided herein are methods for inhibiting migration of a neuroblastoma cell, inducing maturation of a neuroblastoma cell, and altering cell cycle progression of a neuroblastoma cell comprising administering to the cell a therapeutically effective amount of a HDAC1, HDAC2, and/or HDAC6 selective inhibitor or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 9, 2014
    Publication date: April 16, 2015
    Applicant: Acetylon Pharmaceuticals, Inc.
    Inventors: Simon Stewart Jones, Min Yang, David Lee Tamang
  • Publication number: 20150094304
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 2, 2015
    Inventors: SARA SABINA HADIDA RUAH, PETER DIEDERIK JAN GROOTENHUIS, FREDRICK F. VAN GOOR, JINGLAN ZHOU, BRIAN RICHARD BEAR, MARK THOMAS MILLER, JASON MC CARTNEY, MEHDI MICHEL DJAMEL NUMA
  • Publication number: 20150011550
    Abstract: Use of a synthetic compound selected from the group consisting of JKF-006, JKF-011 and JKF-027 in the preparation of a medicament for treating Alzheimer's disease.
    Type: Application
    Filed: January 25, 2013
    Publication date: January 8, 2015
    Applicant: BEIJING JOEKAI BIOTECHNOLOGY LLC
    Inventor: Weiwei Ma
  • Patent number: 8916071
    Abstract: A chromene compound which has a sulfur-containing substituent represented by the following formula (2) at the 6-position and/or 7-position carbon atom of an indeno(2,1-f)naphtho(1,2-b)pyran structure and is excellent in photochromic properties and stability at a high temperature. In the formula (2), ring X is an aromatic hydrocarbon ring or aromatic heterocyclic ring, R3 and R4 are each independently an alkyl group, haloalkyl group, cycloalkyl group, alkoxy group, amino group, heterocyclic group containing a ring member nitrogen atom and bonded to the ring X bonded thereto via the nitrogen atom, halogen atom, aryloxy group or aryl group, and “a” is an integer of 0 to 4.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: December 23, 2014
    Assignee: Tokuyama Corporation
    Inventors: Yasutomo Shimizu, Shinobu Izumi, Junji Takenaka, Junji Momoda
  • Patent number: 8906913
    Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: December 9, 2014
    Assignee: Panacea Biotec Limited
    Inventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Gurmeet Kaur, Sandeep Kanwar, Nishan Singh, Gurmeet Kaur Nanda, Sitaram Kumar Magadi, Sudhir Kumar Sharma
  • Patent number: 8906911
    Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: December 9, 2014
    Assignee: AbbVie Inc.
    Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Guo Ping Wei, Lijuan Jane Wang
  • Publication number: 20140357634
    Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Applicant: GRÜNENTHAL GMBH
    Inventors: BERT NOLTE, WOLFGANG SCHRÖDER, KLAUS LINZ, WERNER ENGLBERGER, HANS SCHICK, HEINZ GRAUBAUM, BIRGIT ROLOFF, SIGRID OZEGOWSKI, JÓZSEF BÁLINT, HELMUT SONNENSCHEIN
  • Publication number: 20140343050
    Abstract: Provided are carboxylic ester derivatives of formula (I), methods of preparing them, and methods for using them. These compounds are prodrugs of D-isoglutamyl-[D/L]-tryptophan. The in vitro bioconversion of some of the prodrugs to the parent drug D-isoglutamyl-D-tryptophan (or thymodepressin) was tested in human hepatocytes and in human blood. In vivo pharmacokinetic studies following oral administration of some of the prodrugs to rats are also reported.
    Type: Application
    Filed: March 30, 2012
    Publication date: November 20, 2014
    Applicant: APTOEX TECHNOLOGIES, INC.
    Inventors: Tim Fat Tam, Regis Leung-Toung, Yingsheng Wang, Yanqing Zhao, Tao Xin, Wanren Li, Jolanta Maria Wodzinska, Vrajlal S. Rabadia, Christopher John Feeney
  • Patent number: 8853209
    Abstract: Compounds of Formula I wherein A1, B1, C1, D1, E1, F1 and L1 are as defined herein, which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mdl-1 protein, such as leukemia and lymphoma, are disclosed.
    Type: Grant
    Filed: April 15, 2011
    Date of Patent: October 7, 2014
    Assignee: AbbVie Inc.
    Inventors: Xiaohong Song, Hong Ding, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Cheol-Min Park, Zhi-Fu Tao, Xilu Wang, Aaron R. Kunzer
  • Publication number: 20140256725
    Abstract: The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.
    Type: Application
    Filed: September 14, 2012
    Publication date: September 11, 2014
    Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Matthijs Poulie, Cornelis Marius Timmers, Saskia Vertaik
  • Publication number: 20140235629
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I or II, or the pharmaceutically acceptable salts thereof, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: September 26, 2012
    Publication date: August 21, 2014
    Inventors: Michael D. Bartberger, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason A. Duquette, John Eksterowicz, Brian M. Fox, Jiasheng Fu, Ana Gonzalez Buenrostro, Felix Gonzalez Lopez De Turiso, Darin J. Gustin, Julie A. Heath, Michael G. Johnson, Frank Kayser, David John Kopecky, Yihong Li, Zhihong Li, Zhihua Ma, Joel Micintosh, Julio C. Medina, Jeffrey Thomas Mihalic, Steven H. Olson, Yosup Rew, Philip M. Roveto, Michael J. Schmitt, Daqing Sun, Xiaodong Wang, Malgorzata Wanska, Christine Weathers, Xuelei Yan
  • Publication number: 20140228359
    Abstract: The present invention relates to novel bis-indolic derivatives, processes for their preparation, and their potential use as new antibacterial drugs.
    Type: Application
    Filed: July 20, 2012
    Publication date: August 14, 2014
    Applicant: UNIVERSITE JOSEPH FOURIER
    Inventors: Jean-Noël Denis, Marcelle Claude Jolivalt, Louis Max Maurin, Nikolaevna Olga Burchak
  • Patent number: 8796268
    Abstract: This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof: wherein Z, HY, R1, R2, R3, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: August 5, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Brian S. Freeze, Masaaki Hirose, Yongbo Hu, Todd B. Sells, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • Patent number: 8778236
    Abstract: A novel photochromic compound which develops a color of a neutral tint and has high color optical density, high fading speed and excellent durability. The present invention is a chromene compound having an indeno(2,1-f)naphtho(1,2-b)pyran structure as the basic skeleton in which a hetero ring having two hetero atoms including at least one sulfur atom is directly bonded to the 6-position and the 7-position of the indeno(2,1-f)naphtho(1,2-b)pyran structure via the hetero atom like the compound represented by the following formula (18).
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: July 15, 2014
    Assignee: Tokuyama Corporation
    Inventors: Junji Takenaka, Junji Momoda, Kazuhiro Teranishi, Toshiaki Takahashi, Mitsuyoshi Sando, Shinobu Izumi
  • Patent number: 8742100
    Abstract: The present invention generally relates to inhibitors of isoprenylcysteine carboxyl methyltransferase (Icmt), in particularly to compounds that inhibit Icmt activity and pharmaceutical compositions thereof. The invention also relates to methods of disease treatment using the same.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: June 3, 2014
    Assignee: National University of Singapore
    Inventors: Jo Lene Leow, Mei-Wang Casey, Patrick J. Casey, Mei Lin Go, Kumar Gorla Suresh
  • Publication number: 20140148452
    Abstract: The invention relates to morpholino-derivatives according to Formula (I) or stereoisomers or pharmaceutically acceptable salts or solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, m and n are as defined in the specification. The compounds are antagonists, reverse agonists or agonists of G-protein coupled receptors, such as dopamine D4 and 5HT1a. The inventions also relates to pharmaceutical compositions comprising the compounds and methods involving the compounds and compositions. The compounds and compositions of the invention may in particular be used in the treatment of diseases and disorders, such as neurological and neurodegenerative diseases; or as lead compounds for the design and selection of further therapeutic compounds.
    Type: Application
    Filed: November 20, 2013
    Publication date: May 29, 2014
    Applicant: University of Dundee
    Inventors: Jeremy Besnard, Andrew Lee Hopkins, Ian Gilbert, Gian Filippo Ruda, Keren Abecassis
  • Publication number: 20140128391
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.
    Type: Application
    Filed: November 1, 2013
    Publication date: May 8, 2014
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 8709308
    Abstract: The chromene compound is represented by the following formula (I), wherein R3 at the 11-position is a sulfur-containing substituent selected from the group consisting of thiol group, alkylthio group, alkoxyalkylthio group, haloalkylthio group, cycloalkylthio group, arylthio group, heteroarylthio group, sulfonyl group and sulfinyl group, R1 and R2 at the 6-position and the 7-position are a combination of an aryl group or a heteroaryl group and an electron donating group having a Hammett constant ?p of ?0.1 or less, or R1 and/or R2 is sulfur-containing substituent selected from thiol group, alkylthio group, alkoxyalkylthio group, haloalkylthio group, cycloalkylthio group, arylthio group and heteroarylthio group.
    Type: Grant
    Filed: January 26, 2012
    Date of Patent: April 29, 2014
    Assignee: Tokuyama Corporation
    Inventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Kazuhiro Teranishi, Mitsuyoshi Sando, Shinobu Izumi
  • Patent number: 8691120
    Abstract: A photochromic chromene compound having an indeno(2,1-f)naphtho(1,2-b)pyran structure as its basic skeleton, an aryl group or a heteroaryl group at the 6-position carbon atom of the structure and an electron donor group having a Hammett constant ?p of not more than ?0.1 at the 7-position carbon atom.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: April 8, 2014
    Assignee: Tokuyama Corporation
    Inventors: Toshiaki Takahashi, Junji Takenaka, Junji Momoda, Mitsuyoshi Sando, Kazuhiro Teranishi
  • Publication number: 20140073584
    Abstract: The invention relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as PI-3 kinase.
    Type: Application
    Filed: September 30, 2013
    Publication date: March 13, 2014
    Applicant: SIGNALRX PHARMACEUTICALS, INC.
    Inventors: Guillermo A. Morales, Kevin Weber, Jessica Newblom, Joseph R. Garlich
  • Publication number: 20140057906
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: October 21, 2013
    Publication date: February 27, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara S. Hadida Ruah, Peter D.J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
  • Publication number: 20140057909
    Abstract: The present invention relates to an indole derivative, The indole derivative according to the present invention effectively inhibits the activity of diacylglycerol acyltransferase (DGAT) which induces metabolic diseases, such as obesity, diabetes, hyperlipidemia, or fatty liver and the like in lipid metabolism, thereby effectively regulating lipid metabolism and energy metabolism, and thus can be useful in pharmaceutical compositions for preventing or treating metabolic disease.
    Type: Application
    Filed: November 4, 2013
    Publication date: February 27, 2014
    Applicant: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY
    Inventors: Hyun Sun LEE, Mun-Ock KIM, Yongseok CHOI, Kyeong Lee, Jeong-Jun PARK, Jee-Hee SEO, Hwayoung JUNG, Sungchan CHO
  • Publication number: 20140051751
    Abstract: Environmentally-friendly alternatives to organometallic antifoulants that are efficacious at preventing biofouling by organisms such as the zebra mussel. Preferred antifoulant compositions utilize compounds having a Lipophilic-Amide-Spacer-ElectroNegative (“LASEN”) structural motif, such as capsaicin, and compounds having a TetraHydroCannibinoid (“THC”) structural motif. The antifoulant compositions are non-toxic, and effective.
    Type: Application
    Filed: October 25, 2013
    Publication date: February 20, 2014
    Applicants: The Board of Regents of the University of Texas System, University of North Texas Health Science Center at Fort Worth
    Inventors: John A. Schetz, Robert F. McMahon
  • Publication number: 20140051683
    Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.
    Type: Application
    Filed: April 23, 2013
    Publication date: February 20, 2014
    Applicant: AbbVie Inc.
    Inventors: Xilu WANG, Xiaohong Song, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Lisa A. Hasvold, Le Wang, Zhi-Fu Tao, Aaron R. Kunzer
  • Publication number: 20140011807
    Abstract: The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.
    Type: Application
    Filed: March 15, 2012
    Publication date: January 9, 2014
    Applicants: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD., MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Toru Iijima, Hiroshi Sugama, Takayuki Kawaguchi, Jingkang Shen, Guangxin Xia, Jianshu Xie
  • Publication number: 20140005386
    Abstract: Novel p53-Mdm2 antogonists that conform to Formula I or to Formula II: where the prescribed substituent groups are defined, are useful in treating or preventing cancer. In particular, the compounds and their pharmaceutical compositions are useful for treating relapsed/refractory acute myeloid and lymphoid leukemia and refractory chronic lymphocytic leukemia/small cell lymphocytic lymphomas.
    Type: Application
    Filed: September 8, 2011
    Publication date: January 2, 2014
    Inventor: Alexander Doemling
  • Publication number: 20140004174
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Application
    Filed: May 20, 2013
    Publication date: January 2, 2014
    Applicant: Pharmacyclics, Inc.
    Inventors: Erik VERNER, Sriram BALASUBRAMANIAN, Joseph J. BUGGY
  • Publication number: 20130336919
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 19, 2013
    Applicant: ARDELYX, INC.
    Inventor: Ardelyx, Inc.
  • Publication number: 20130303539
    Abstract: Compounds, compositions and methods useful for treating ocular diseases are provided. In particular, antagonists of TRPV4, their synthesis, pharmaceutical compositions thereof and methods of treating ocular diseases such as glaucoma, are disclosed.
    Type: Application
    Filed: March 15, 2013
    Publication date: November 14, 2013
    Inventors: David Krizaj, Glenn D. Prestwich, Peter Barabas, Yong Xu, Daniel Ryskamp
  • Publication number: 20130303538
    Abstract: The invention relates to compounds of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them.
    Type: Application
    Filed: January 20, 2012
    Publication date: November 14, 2013
    Inventors: Joachim Nozulak, Dieter Oser
  • Patent number: 8575230
    Abstract: Environmentally-friendly alternatives to organometallic antifoulants that are efficacious at preventing biofouling by organisms such as the zebra mussel. Preferred antifoulant compositions utilize compounds having a Lipophilic-Amide-Spacer-ElectroNegative (“LASEN”) structural motif, such as capsaicin, and compounds having a TetraHydroCannibinoid (“THC”) structural motif. The antifoulant compositions are non-toxic, and effective.
    Type: Grant
    Filed: April 16, 2008
    Date of Patent: November 5, 2013
    Assignees: University of North Texas Health Science Center at Fort Worth, The Board of Regents of the University of Texas System
    Inventors: John A. Schetz, Robert F. McMahon
  • 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: 20130274260
    Abstract: This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic ?-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds. The compounds have the formula (A1) wherein R1, R2, R4, R6, E, n, Y1, Y2, Y3, Y4, Y5, L, B, R8, and m are as defined in the claims.
    Type: Application
    Filed: December 13, 2011
    Publication date: October 17, 2013
    Inventors: Gerard Griffioen, Tom Van Dooren, Verónica Rojas De La Parra, Sara Allasia, Arnaud Marchand, Amuri Kilonda, Patrick Chaltin
  • Patent number: 8557807
    Abstract: The invention, relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as P1-3 kinase.
    Type: Grant
    Filed: January 23, 2009
    Date of Patent: October 15, 2013
    Assignee: Signal Rx Pharmaceuticals, Inc.
    Inventors: Guillermo A. Morales, Kevin T. Weber, Jessica M. Newblom, Xiaodong Peng, Jingdong Su, Joseph R. Garlich
  • Publication number: 20130252955
    Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.
    Type: Application
    Filed: May 16, 2013
    Publication date: September 26, 2013
    Applicant: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
  • Publication number: 20130196960
    Abstract: The present disclosure relates to compounds useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders either alone or in combination therapy.
    Type: Application
    Filed: February 9, 2011
    Publication date: August 1, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Jason Rohde, Charles Kim, Takashi Nakai, Galen John Carey
  • Publication number: 20130178453
    Abstract: The present disclosure relates to compounds useful as agonists of the cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders, either alone or in combination therapy. The compounds of the invention have Formula (I).
    Type: Application
    Filed: February 9, 2011
    Publication date: July 11, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Jason Rohde, Bo Peng, Takashi Nakai, Kevin Sprott, Ara Mermerían, Wayne C. Schairer, Galen John Carey
  • Publication number: 20130178471
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: February 28, 2013
    Publication date: July 11, 2013
    Applicant: Vextex Pharmaceuticals Incorporated
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20130158021
    Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.
    Type: Application
    Filed: October 26, 2012
    Publication date: June 20, 2013
    Applicant: Massachusetts Institute of Technology
    Inventor: Massachusetts Institute of Technology
  • Publication number: 20130131060
    Abstract: The present invention relates to a compound of formula (I) wherein R1, R2 and R3 are as defined in the description and the physiologically acceptable salts thereof as well as the physiologically acceptable solvates of the compounds of formula I and of the salts thereof. The compounds of formula I are suitable for treating tumors.
    Type: Application
    Filed: December 10, 2010
    Publication date: May 23, 2013
    Applicant: Johannes Gutenberg-Universität Mainz
    Inventors: Gerd Dannhardt, Jan-Peter Kramb, Stanislav Plutizki
  • Publication number: 20130102776
    Abstract: An anticancer agent comprising a compound represented by the formula (I) [R1 represents hydrogen atom, hydroxyl group, a C1-6 alkoxy group and the like; R2 and R3 represents hydrogen atom, a halogen atom, a C1-6 alkyl group and the like; R4 represents hydrogen atom, a C1-6 alkyl group, a C1-6 alkylsulfonyl group and the like; R5 represents hydrogen atom or a substituent; represents a single bond or a double bond; R6 and R7 represents hydrogen atom, a C1-6 alkyl group and the like; R8 represents hydrogen atom, a C1-6 alkyl group and the like; A represents —O—, —S—, or —CH2—; D represents —C? or —N?; X represents methylene group, —O—, or —CO—; Q represents —N? or —C(R8)?; and Y represents a heterocyclic group or amino group], which shows a superior inhibitory activity against pim-1 kinase.
    Type: Application
    Filed: April 28, 2011
    Publication date: April 25, 2013
    Applicants: RIKEN, THE UNIVERSITY OF TOKYO
    Inventors: Tetsuo Nagano, Takayoshi Okabe, Hirotatsu Kojima, Nae Saito, Hirofumi Nakano, Masanao Abe, Akiko Tanaka, Teruki Honma, Shigeyuki Yokoyama, Keiko Tsuganezawa, Hitomi Yuki
  • Patent number: 8415349
    Abstract: The invention provides derivatives of azabicyclo alkane having formula (ID), and the method for making them, wherein each substitute in formula (ID) is same as defined in the description.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: April 9, 2013
    Assignee: Jiangsu Hansoh Pharmaceuticals Co., Ltd.
    Inventors: Peng Cho Tang, Zhigang Lin, Hejun Lü, Fuqiang Zhao, Li Li, Fanglong Yang, Jianghong Fu, Lin Wang, Guangyuan Shen, Dongliang Guan
  • Publication number: 20130081213
    Abstract: The present invention relates to a cationic 6-aminoindoline of general formula (I), the addition salts thereof with an acid and the solvates thereof: the present invention is also directed towards a method for synthesizing this cationic 6-aminoindoline, the compositions, the uses, the hair dyeing methods and the devices using this cationic 6-aminoindoline.
    Type: Application
    Filed: March 2, 2011
    Publication date: April 4, 2013
    Inventor: Aziz Fadli
  • Publication number: 20130072677
    Abstract: Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria.
    Type: Application
    Filed: April 20, 2011
    Publication date: March 21, 2013
    Applicants: TOYAMA CHEMICAL CO., LTD., TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Hajime Takashima, Risa Tsuruta, Tetsuya Yabuuchi, Yusuke Oka, Hiroki Urabe, Yoichiro Suga, Masato Takahashi, Fumito Uneuchi, Hironori Kotsubo, Muneo Shoji, Yasuko Kawaguchi
  • Publication number: 20130065882
    Abstract: This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A1 represents a nitrogen atom or C—R3d wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R1 represents H or a C1-8 alkyl group; R2 represents H, a halogen, a C1-8 alkoxy
    Type: Application
    Filed: October 3, 2012
    Publication date: March 14, 2013
    Inventors: Nobuo Machinaga, Shin Iimura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama