Nitrogen, Other Than As Nitro Or Nitroso, Attached Directly To The Carbocyclic Ring Of The Quinoline Ring System By Nonionic Bonding Patents (Class 546/171)
  • Patent number: 11427544
    Abstract: Disclosed is hydroxamic acid compounds of Formula (I) set forth herein. Also disclosed are a pharmaceutical composition containing such a compound and a method of using the compound for treating a condition associated with histone deacetylase 6.
    Type: Grant
    Filed: May 16, 2017
    Date of Patent: August 30, 2022
    Assignees: TAIPEI MEDICAL UNIVERSITY, NATIONAL TAIWAN UNIVERSITY
    Inventors: Che-Ming Teng, Jing-Ping Liou, Shiow-Lin Pan, Chia-Ron Yang
  • Patent number: 9737525
    Abstract: This disclosure relates to compounds that act as activators of the NRF2/KEAP1/ARE pathway. Specifically, the compounds provided herein can act as high affinity reversible bindings for the NRF2 inhibitor, KEAP1. In some cases, NRF2/KEAP1/ARE pathway activation compounds are capable of repressing expression of inflammatory markers and/or reducing levels of TNFa to provide neuroprotective anti-inflammatory effects in the CNS. Such compounds are useful in the treatment of a variety of diseases including Huntington's disease, Parkinson's disease, Alzheimer's disease, inflammation, and cancer.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: August 22, 2017
    Assignees: The General Hospital Corporation, The Regents of the University of California
    Inventors: Aleksey G. Kazantsev, Leslie M. Thompson, Ruben Abagyan, Malcolm Casale
  • Patent number: 9269907
    Abstract: A compound is shown by the following formula (1). wherein l, m, and n are independently an integer from 1 to 3, Ar1 to Ar4 are independently a substituted or unsubstituted aryl group having 6 to 30 ring carbon atoms, or a substituted or unsubstituted heteroaryl group having 5 to 30 ring atoms, Ar5, Ar6, and Ar7 are independently a substituted or unsubstituted arylene group having 6 to 30 ring carbon atoms, or a substituted or unsubstituted heteroarylene group having 5 to 30 ring atoms, and p is an integer from 0 to 2, and Ar6 and N are bonded via a single bond when p is 0, provided that at least one of Ar1 to Ar4 is substituted with a substituted silyl group, a substituted or unsubstituted alkyl group having 1 to 20 carbon atoms, or a substituted or unsubstituted cycloalkyl group having 3 to 10 carbon atoms, and at least one of Ar1 to Ar4 is substituted with a cyano group.
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: February 23, 2016
    Assignee: IDEMITSU KOSAN CO., LTD.
    Inventors: Yumiko Mizuki, Hiroyuki Saito, Yuichiro Kawamura, Hirokatsu Ito, Masahiro Kawamura
  • Patent number: 9073821
    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: Grant
    Filed: April 20, 2011
    Date of Patent: July 7, 2015
    Assignees: TAISHO PHARMACEUTICAL CO., LTD, TOYAMA CHEMICAL 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
  • Patent number: 9062206
    Abstract: The present disclosure relates to a bis-quinophthalone pigment of Formula I, and a process for the same. wherein X1, X2, X3 and X4 are independently H or halogen, preferably Cl or Br; R2 is substituent selected from the group consisting of H, C1-C20 straight or branched chain alkyl substituents, aromatic substituents, aliphatic substituents, and combinations thereof.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: June 23, 2015
    Inventor: Keki Hormusji Gharda
  • Patent number: 9040532
    Abstract: Compounds are described herein useful for treating diseases and conditions by modulation of one or more alpha adrenergic receptor. The compounds can include a naphthalene, a quinoline, a benzoimidazole or an isoquinoline as a core structure. Methods of making, using and formulating these compounds are described.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: May 26, 2015
    Assignee: Allergan, Inc.
    Inventors: Ken Chow, Liming Wang, Wenkui K. Fang, Evelyn G. Corpuz, Santosh C. Sinha, Daniel W. Gil, Mohammad I. Dibas, John E. Donello
  • Publication number: 20150110809
    Abstract: Embodiments of the invention are directed to compounds that inhibit an activity of EP AC proteins and methods of using the same. The inventors have developed a sensitive and robust high throughput screening (HTS) assay for the purpose of identifying EPAC specific inhibitors (Tsalkova et al. (2012) PLOS ONE 7 (1):e30441).
    Type: Application
    Filed: February 8, 2013
    Publication date: April 23, 2015
    Applicant: The Board of Regents of the University of Texas System
    Inventors: Xiaodong Cheng, Jia Zhou, Tamara Tsalkova, Fang Mei, Haijun Chen
  • Patent number: 8980892
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 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 the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: March 17, 2015
    Assignees: Syngenta Crop Protection LLC, Syngenta Limited
    Inventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
  • Publication number: 20150065554
    Abstract: Disclosed herein are methods of treating a patient at risk of developing or having a neurofibromatosis or a sporadic schwannoma. In exemplary embodiments, the method involves administering to a subject in need an effective amount of a modulator of a target related to neurofibromatosis. Also disclosed are screening assays involving the implementation of Merlin-null Schwann cells, and to compounds identified using same.
    Type: Application
    Filed: March 13, 2013
    Publication date: March 5, 2015
    Applicant: University of Central Florida Research Foundation, Inc.
    Inventor: Cristina Fernandez-Valle
  • Patent number: 8969577
    Abstract: The present invention relates to curable compositions comprising a thermolatent amidine base and an organic material which is polymerizable or crosslinkable with a basic or nucleophilic catalyst. In particular, the invention relates to curable coating compositions, especially powder coating compositions, and curable adhesive compositions, as well as to the use a thermolatent amidine base as a curing catalyst for thermally induced base-catalyzed polymerization or crosslinking reactions.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: March 3, 2015
    Assignee: BASF SE
    Inventors: Peter Nesvadba, Lucienne Bugnon Folger, Ralf Knischka
  • Publication number: 20150045368
    Abstract: Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: March 1, 2013
    Publication date: February 12, 2015
    Inventors: Howard Bregman, John L. Buchanan, Nagasree Chakka, Erin F. Dimauro, Hakan Gunaydin, Angel Guzman-Perez, Zihao Hua, Hongbing Huang, Xin Huang, Matthew W. Martin, Vinod F. Patel
  • Patent number: 8946429
    Abstract: While methodologies for the Kinetic Resolution of alcohols are well established, no analogous direct methods exist for the highly selective, direct catalytic Kinetic Resolution of thiols (i.e., R—SH). The present invention relates to a method for resolving stereoisomeric mixtures of thiols. In particular, the present invention relates to purely organocatalytic mediated resolution of enantiomeric mixtures of thiols without the need for enzymes. Also disclosed are some novel catalysts. Such catalysts may comprise a cinchona alkaloid-derived moiety.
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: February 3, 2015
    Assignee: The Provost, Fellows, Foundation Scholars, and the other Members of the Board, of the College of the Holy and Undivided Trinity of Queen Elizabeth, Near Dublin
    Inventors: Stephen Joseph Connon, Aldo Peschiulli, Barbara Procuranti
  • Publication number: 20150031663
    Abstract: The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo.
    Type: Application
    Filed: October 13, 2014
    Publication date: January 29, 2015
    Applicant: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Shahriar Mobashery, Dusan Hesek, Mayland Chang
  • Patent number: 8937184
    Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CB2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB2 receptors are involved. The compounds have the general formula (I) wherein R1-R4 have the meanings given in the specification.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: January 20, 2015
    Assignee: Abbvie B.V.
    Inventors: Josephus H. M. Lange, Herman H. Van Stuivenberg, Bernard J. Van Vliet
  • Publication number: 20150005345
    Abstract: The present invention features benzhydrol-pyrazole derivatives and related compounds having kinase inhibitory activity. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions, such as cancers, inflammatory disorders, or autoimmune disorders.
    Type: Application
    Filed: January 9, 2013
    Publication date: January 1, 2015
    Inventors: Anthony D. Keefe, Richard W. Wagner, Matthew Clark, Ying Zhang, Diana Gikunju, John Cuozzo, Heather Thomson
  • Publication number: 20140371222
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Kowalczyk-Prezewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Paul Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
  • Publication number: 20140352713
    Abstract: The invention relates to the use of specific heterocyclic couplers which are cationic 7-amino-1,2,3,4-tetrahydroquinoline derivatives of formula (I) for dyeing keratin fibres such as the hair: in which formula (I): R1 to R6, CAT+, An?, and Ra to Rb are as defined in the description.
    Type: Application
    Filed: December 17, 2012
    Publication date: December 4, 2014
    Inventor: Aziz Fadli
  • Patent number: 8895535
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumors.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: November 25, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Frank Zenke, Michel Calderini, Djordje Musil
  • Publication number: 20140336193
    Abstract: The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 13, 2014
    Inventors: Donald W. Landry, Shi-Xian Deng, Stevan Pecic, Kirsten Alison Rinderspacher
  • Publication number: 20140335019
    Abstract: Provided herein are compositions and methods for the treatment and analysis of neurological disorders. In particular, provided herein are small molecules targeted to amyloid-? (A?) or metal-A? species for the treatment, diagnosis, or study of neurological conditions such as Alzheimer's disease (AD) and other diseases and conditions.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 13, 2014
    Inventors: Mi Hee Lim, Katayoun Saatchi, Urs Hafeli, Joo-Yong Lee
  • Publication number: 20140336378
    Abstract: Disclosed are a novel benzamide derivative and pharmaceutical use thereof, and more particularly, a novel benzamide derivative having a structure of Formula 1 or pharmaceutically acceptable salts thereof, and a composition for prevention or treatment of pain or itching including the above material. The novel benzamide derivative and pharmaceutically acceptable salt thereof according to the present invention exhibit excellent pain-suppressive effect and, in particular, pain-suppressive effect in not only a neuropathic animal model but also other models such as a formalin model, and therefore, may be used in suppression of different pains such as nociceptive pain, chronic pain, etc.
    Type: Application
    Filed: November 29, 2012
    Publication date: November 13, 2014
    Inventor: Doo Hyun Lee
  • Publication number: 20140329675
    Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
    Type: Application
    Filed: May 3, 2014
    Publication date: November 6, 2014
    Applicant: INSCENT, INC.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Publication number: 20140315947
    Abstract: The present invention relates to a pharmaceutical composition for inhibiting angiogenesis and a novel sulfonyl amide derivative compound which can be useful for the prevention or treatment of angiogenesis-related diseases or disorders. Since the compound used as an active ingredient in the pharmaceutical composition of the invention is specifically bound to UQCRB and inhibits biological functions thereof, apoptosis is not induced and angiogenic responses are inhibited. Therefore, the compound used as an active ingredient in the pharmaceutical composition of the invention can be useful as an effective and safe angiogenesis inhibitory agent.
    Type: Application
    Filed: May 23, 2011
    Publication date: October 23, 2014
    Applicant: INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
    Inventors: Ho Jeong Kwon, Gyoon Hee Han, Hye Jin Jung, Jeong Jea Seo
  • Publication number: 20140309225
    Abstract: The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, wherein R1 is a substituent represented by the following formula (II-1), (III-1), or (IV-1) (wherein R3, R4, R5, n, and X1 have the same definitions as those described in the specification), and R2 is a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 16, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Hideyasu FUJIWARA, Shinsuke MIZUMOTO, Yohei KUBO, Hiyoku NAKATA, Shinji HAGIWARA, Yasutaka BABA, Takashi TAMURA, Hidenobu KUNIYOSHI, Tomoyuki MASHIKO, Mari YAMAMOTO
  • Publication number: 20140309257
    Abstract: The invention provides methods of inhibiting the growth or metastasis of cancer in a mammal by inhibiting TopoIIa in the mammal. The invention also provides small molecule inhibitors of TopoIIa useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds and methods of using the same.
    Type: Application
    Filed: November 13, 2012
    Publication date: October 16, 2014
    Inventor: Daniel V. Labarbera
  • Publication number: 20140296236
    Abstract: The invention relates to new quinoline derivative compounds of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Valerio Berdini, Patrick Rene Angibaud, Steven John Woodhead, Gordon Saxty
  • Publication number: 20140296529
    Abstract: The present disclosure relates to a bis-quinaldine compound of formula I and a process for the same. wherein R2 is a substituent selected from the group consisting of H, C1-C20 straight or branched chain alkyl substituents, aromatic substituents, aliphatic substituents, combinations thereof and the like.
    Type: Application
    Filed: October 22, 2012
    Publication date: October 2, 2014
    Inventor: Keki Hormusji GHARDA
  • Publication number: 20140288065
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Application
    Filed: June 10, 2014
    Publication date: September 25, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
  • Publication number: 20140288119
    Abstract: This invention provides a compound having the structure: wherein R1 is H, halogen, —NR5R6, —NR5—C(?O)—R6, —NH—C(?O)—OR7, —OR7, —NO2, —CN, —SR7, —SO2R7, —CO2R7, CF3, —SOR7, —POR7, —C(?S)R7, —C(?O)—NR5R6, —CH2—C(?O)—NR5R6, —C(?NR5)R6, —P(?O)(OR5)(OR6), —P(OR5)(OR6), —C(?S)R7, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, aryl, heteroaryl, or heterocyclyl, wherein R5, R6, and R7 and are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; m is an integer from 0 to 2; R2 and R3 are each, independently, H, halogen, —NH2, —CX3, —C(?O)OR8, C(?O)R8, —C(?O)NR9R10, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, heteroalkyl, aryl, heteroaryl, or heterocyclyl; wherein X is Cl, Br, or F; R8, R9 and R10 are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; Q is —Ar1—Z— or —Z—Ar1—Z—, wherein Ar1 is aryl or heteroaryl; and each occurrence of Z is independently present or
    Type: Application
    Filed: October 3, 2012
    Publication date: September 25, 2014
    Applicants: The Trustees of Columbia University in the City of New York, SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Ronald Breslow, Paul A. Marks
  • Publication number: 20140275165
    Abstract: The present invention relates to compounds with activity as BACE1 and NF?B modulators, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease. The present invention is also directed to the treatment of diseases related to dysfunction of cell proliferation, the immune system and/or inflammation using such compounds or pharmaceutical compositions containing such candidate compounds.
    Type: Application
    Filed: March 24, 2014
    Publication date: September 18, 2014
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Donald W. Landry, Tae-Wan Kim, Shi-Xian Deng, Gangli Gong, Jeremy C. Hwang, Yuli Xie, Yidong Liu, Kirsten Alison Rinderspacher
  • Publication number: 20140242135
    Abstract: In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Method of employing such agents, and articles incorporating the same, are also provided. 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: Application
    Filed: April 25, 2012
    Publication date: August 28, 2014
    Applicant: Vanderbilt University
    Inventors: Laurence Zwiebel, Gregory M. Pask, David C. Rinker, Ian M. Romaine, Gary A. Sulikowski, Paul R. Reid, Alex G. Waterson, Kwangho Kim, Patrick L. Jones, Robert W. Taylor
  • Patent number: 8809368
    Abstract: This invention relates to novel quinoline compounds which affect gap junction activity. Also provided are methods of using such compounds and compositions containing the compounds to treat gap junction disorders.
    Type: Grant
    Filed: October 28, 2008
    Date of Patent: August 19, 2014
    Assignee: Kansas State University Research Foundation
    Inventors: Duy H. Hua, Dolores J. Takemoto, Thu Nguyen
  • Publication number: 20140225070
    Abstract: Provided is an organic light-emitting diode including a compound of Formula 1 below: A detailed description of a substituent in Formula 1 above is defined as described in the detailed description.
    Type: Application
    Filed: June 21, 2013
    Publication date: August 14, 2014
    Applicant: Samsung Display Co., Ltd.
    Inventors: Jun-Ha Park, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee
  • Patent number: 8802701
    Abstract: The present invention refers to new compounds represented by the general formula (I) where X is represented by the general formula (II) and Y is represented by the general formula (III). The relation X to Y may vary from 1:1 to 1:7. The radicals R1, R2, R3, R4, R5, and R6 in formula (II) are represented by: R1=H, CF3, CH3, OCH3, NH2, halogen; R2=H, CH3, NH2, halogen, NH—CHCH3(CH2)3N(C2H5)(CH2CH2OH), CH(OH)-2(C5H11N), NH—R7—N—(C2H5)2; R3=H, m-OC6H4CF3, NH2; R4=H, CH3, OCH3, NH2, halogen; R5=H, CH3, CF3, NH2, halogen; R6=H, CF3, CH3, NH2, halogen, NH—R8—N—(C2H5)2, NHCH(CH3)(CH2)3NH2; R7=(CH2)2, (CH2)3, CHCH3CH2, (CH2)4, (CH2)5, CHCH3(CH2)3, (CH2)6, (CH2)8, (CH2)10, (CH2)12; R8=CHCH3(CH2)3, CHCH3(CH2)CHCH3, (CH2)2, (CH2)3, (CH2)6, (CH2)3O(CH2)3. This invention also refers to a process of preparation of these compounds (formula I), and antiparasitic pharmaceutical compositions thereof.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: August 12, 2014
    Assignee: Fundação Oswaldo Cruz
    Inventors: Nubia Boechat, Marcus Vinicius Nora de Souza, Alessandra Leda Valverde, Antoniana Ursine Krettli
  • Publication number: 20140219960
    Abstract: The present invention relates a novel composition for preventing or treating hepatitis C virus, regulating the phosphorylation of a replicase. More specifically, it is possible to prevent or treat hepatitis C using a novel PRK2 inhibitor discovered through structure modeling, and to prevent or treat hepatitis C, particularly, interferon-insensitive hepatitis C through coadministration of an Hsp90 inhibitor.
    Type: Application
    Filed: April 23, 2012
    Publication date: August 7, 2014
    Applicant: Industry-Academic Cooperation Foundation, Yonsei University
    Inventor: Jong-Won Oh
  • Publication number: 20140209872
    Abstract: A compound having an electron injection capability and/or electron transport capability represented by Formula 1, an organic light emitting device including the compound; and a flat display device including the organic light emitting device. The descriptions of substituents are referred to in the detailed description.
    Type: Application
    Filed: July 26, 2013
    Publication date: July 31, 2014
    Inventors: Jun-Ha Park, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee
  • Patent number: 8778967
    Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).
    Type: Grant
    Filed: January 25, 2012
    Date of Patent: July 15, 2014
    Assignee: Genzyme Corporation
    Inventors: Gary Bridger, Renato T Skelj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R Wilson, Jason B Crawford, Ernest J McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria R Di Fluri
  • Patent number: 8759348
    Abstract: There is provided the use of compounds of formula wherein R1, R2, R3 and E have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula (I) per se.
    Type: Grant
    Filed: May 16, 2008
    Date of Patent: June 24, 2014
    Assignee: Helperby Therapeutics Limited
    Inventors: Mandy Christine Beswick, Susan Mary Cramp, Yanmin Hu, Thomas David Pallin, Hazel Joan Dyke, Anthony Coates
  • Publication number: 20140162980
    Abstract: The present invention provides compounds of formula (I) wherein G1, G2, G3, G4, G5, G6, Y1, Y2, Y3, Y4, Y5 and Y6 and p and q are as defined in the claims. The invention further relates to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
    Type: Application
    Filed: July 28, 2011
    Publication date: June 12, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Daniel Stierli, Kurt Nebel, Werner Zambach, Andrea Bortolato
  • Publication number: 20140138632
    Abstract: An amine-based compound and an organic light-emitting diode including the amine-based compound are provided. The amine-based compound may be used between a pair of electrodes of an organic light-emitting diode. For example, the amine-based compound may be used in an emission layer and/or between the emission layer and an anode (for example, in a hole injection layer, a hole transport layer, a functional layer having a hole injection ability and a hole transport ability). Accordingly, an organic light-emitting diode including a first electrode, a second electrode facing the first electrode, and an organic layer that is interposed between the first electrode and the second electrode, and includes the amine-based compound is provided.
    Type: Application
    Filed: March 13, 2013
    Publication date: May 22, 2014
    Inventors: Young-Kook Kim, Seok-Hwan Hwang, Hye-Jin Jung, Jun-Ha Park, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee
  • Publication number: 20140135325
    Abstract: The invention encompasses compound and pharmaceutical composition comprising the compound of the following Formula (I): or pharmaceutically acceptable salts or prodrugs thereof, that are useful for inhibiting ezrin protein in a cell or for inhibiting the growth of a cancer cell.
    Type: Application
    Filed: October 7, 2013
    Publication date: May 15, 2014
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Milton L. Brown, Mikell Paige, Jeffrey A. Torestsky, Aykut Uren, George Kosturko, Gullay Bulut
  • Patent number: 8722930
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: May 13, 2014
    Assignee: Orion Corporation
    Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
  • Publication number: 20140113931
    Abstract: Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Application
    Filed: March 15, 2013
    Publication date: April 24, 2014
    Applicant: Portola Pharmaceuticals, Inc.
    Inventor: Portola Pharmaceuticals, Inc.
  • Publication number: 20140073668
    Abstract: The present invention relates to the NQBS class of molecules. It is based, at least in part, on the discovery that a representative group of compounds have been observed to inhibit nuclear translocation of NF-?B subunits. Without being bound by any particular theory, this inhibition of nuclear translocation may be mediated by either (i) binding of the NQBS or related compound to the C-terminus of the RHD, which specifically mediates the nuclear internalization; or (ii) NQBS-mediated stabilization of the dimer/I?B complex, disallowing dissociation of the active NF-?B monomers, and thus, inhibiting the generation of the subunits necessary to enter the nucleus. The NQBS class of molecules, and related molecules, may be used in therapeutic applications where inhibition of NF-?B translocation is beneficial, including but not limited to the treatment of cancer, autoimmune disorders, and inflammatory states.
    Type: Application
    Filed: September 6, 2013
    Publication date: March 13, 2014
    Applicant: The Trustees of Columbia Unversity in the City of New York
    Inventors: Donald W. Landry, Owen O'Connor, Shi-Xian Deng, Matko Kalac, Kristen Alison Rinderspacher
  • Publication number: 20140073500
    Abstract: Organic compounds containing heteroatoms and their use in preparing Ziegler-Natta(Ziegler-Natta) catalyst with single activation center. The Ziegler-Natta olefin polymerization catalyst is preparing by adding organic or inorganic solid carrier or compound of them which is pre-activated by heating or pre-treated chemically, organic compound containing heteroatoms and metallic compound into magnesium compound/tetrahydrofuran solution. The Ziegler-Natta olefin polymerization catalyst prepared in the present invention is fluidizable powder and can prepare ethene homopolymer and copolymer of controllable construction with high catalytic activity, during homo-polymerization and combined polymerization with alpha-olefin of C3˜C18 under action of catalyst promoter such as alkyl aluminum, alkyl aluminoxane, and so on.
    Type: Application
    Filed: September 16, 2013
    Publication date: March 13, 2014
    Applicant: Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences
    Inventors: Yong Tang, Xiaohong Yang, Bo Liu, Xiuli Sun, Zhi Ma, Yuan Gao, Cong Wang
  • Publication number: 20140051688
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Q, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: February 20, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Michael WINTERS, Zhihua Sui
  • Publication number: 20140045855
    Abstract: Chroman compounds and derivatives of Formula I are useful inhibitors of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: August 2, 2013
    Publication date: February 13, 2014
    Applicant: AMGEN INC.
    Inventors: Kaustav BISWAS, Jian J. CHEN, Vijay Keshav GORE, Scott HARRIED, Daniel B. HORNE, Matthew R. KALLER, Vu Van MA, Kelvin SHAM, Wenge ZHONG
  • Publication number: 20140031368
    Abstract: This disclosure is related to compounds having the structure wherein Ar1, Ar2, R1-R6, Z, m, n, o, and p are defined herein. This disclosure also relates to pharmaceutical compositions comprising the above compounds and methods for their use.
    Type: Application
    Filed: July 8, 2013
    Publication date: January 30, 2014
    Applicants: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK, SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Ronald Breslow, Paul A. Marks, K. G. Abhilash, Jianing Wang
  • Patent number: 8623860
    Abstract: The invention relates to new azetidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: January 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Bernd Nosse, Gerald Juergen Roth
  • Publication number: 20130345249
    Abstract: The invention encompasses pharmaceutical formulations for the prevention and treatment of Wolbachia-related disease wherein the formulations comprise a compound previously unknown and unused for such a purpose, the compound being one or more of: Pararosaniline Pamoate, Pyrvinium Pamoate, Clofoctol, and Isoreserpine, derivatives, metabolites, precursors, pro-drugs and variants thereof.
    Type: Application
    Filed: January 13, 2012
    Publication date: December 26, 2013
    Applicant: The Regents of the University of California
    Inventors: Alain Debec, Laura Serbus, Frederic Landmann, William Sullivan