Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/471)
  • Patent number: 10790452
    Abstract: An antiaromatic compound and an organic light-emitting device including the same.
    Type: Grant
    Filed: November 4, 2014
    Date of Patent: September 29, 2020
    Assignees: Samsung Display Co., Ltd., Industry-Academic Cooperation Foundation Gyeongsang National University
    Inventors: Mi-Kyung Kim, Yun-Hi Kim, Soon-Ki Kwon, Chang-Woong Chu
  • Patent number: 10676486
    Abstract: The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of RIP2 and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of RIP2-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent.
    Type: Grant
    Filed: September 17, 2015
    Date of Patent: June 9, 2020
    Assignee: ONCODESIGN S.A.
    Inventors: Jan Hoflack, Petra Blom, Pascal Benderitter
  • Patent number: 10421738
    Abstract: Provided herein are cyclodecynes, including chiral cyclodecynes, and methods of making cyclodecynes. The methods may include providing a 1,1?-biaryl compound substituted independently at the 2-position and the 2?-position with a hydroxyl or an amino group; and contacting the 1,1?-biaryl compound with a protected but-2-yne-1,4-diol to form the cyclodecyne.
    Type: Grant
    Filed: June 25, 2018
    Date of Patent: September 24, 2019
    Assignee: Florida State University Research Foundation, Inc.
    Inventors: Trevor Michael Harris, Igor V. Alabugin
  • Patent number: 8969549
    Abstract: Amine chelates capable of antioxidant capacity and amyloid disaggregation are shown which may be useful in targeting metal-based oxidative stress in neurodegenerative disorders. Pyclen, a backbone commonly investigated for contrast agent imaging, may be repurposed as an anti-oxidant chelator for disaggregating amyloid. The antioxidant capacity of pyclen is enhanced dramatically via conversion of the pyridine backbone to a pyridol with cellular studies showing superior antioxidant capacity while retaining chelation ability to protect amyloid from metal ions aggregation and also disaggregate amyloid aggregates. Another family of molecules based upon hybrid heterocyclic amine ligands is also presented.
    Type: Grant
    Filed: January 16, 2014
    Date of Patent: March 3, 2015
    Assignee: Texas Christian University
    Inventors: Kayla Nalynn Green, Kimberly Marie Lincoln, Paulina Gonzalez
  • Patent number: 8969548
    Abstract: Amine chelates capable of antioxidant capacity and amyloid disaggregation are shown which may be useful in targeting metal-based oxidative stress in neurodegenerative disorders. Pyclen, a backbone commonly investigated for contrast agent imaging, may be repurposed as an anti-oxidant chelator for disaggregating amyloid. The antioxidant capacity of pyclen was enhanced dramatically via conversion of the pyridine backbone to a pyridol with cellular studies showing superior antioxidant capacity while retaining chelation ability to protect amyloid from metal ions aggregation and also disaggregate amyloid aggregates.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: March 3, 2015
    Assignee: Texas Christian University
    Inventors: Kayla Nalynn Green, Kimberly Marie Lincoln, Paulina Gonzalez
  • Patent number: 8951998
    Abstract: The present invention discloses compounds of formula I and II or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: February 10, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yonghua Gai, Yat Sun Or, Zhe Wang
  • Patent number: 8921543
    Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.
    Type: Grant
    Filed: January 9, 2012
    Date of Patent: December 30, 2014
    Assignee: AnaSpec Incorporated
    Inventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang, Xiang Guobing
  • Publication number: 20140350036
    Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides dermatological compositions comprising a compound of formula I or mixtures of one or more compounds of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for protecting skin or DNA from photodamage or repairing photodamaged skin or DNA.
    Type: Application
    Filed: January 11, 2013
    Publication date: November 27, 2014
    Inventors: Robert Vince, Abbas Raza, Christine Dreis
  • Patent number: 8815872
    Abstract: Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.
    Type: Grant
    Filed: September 3, 2009
    Date of Patent: August 26, 2014
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Lizbeth Celeste De Selm, Xuliang Jiang, Benny C. Askew, Jr., Srinivasa R. Karra, Andreas Goutopoulos
  • Publication number: 20140213781
    Abstract: The invention relates to peptide mimetics comprising the residues P4-P3-P2-P1, which were cyclized between the side chains of P3 and P2 amino acid and are, as inhibitors of the serine protease plasmin, suitable to be used to inhibit fibrinolysis and thus to reduce blood loss in hyperfibrinolytic conditions, for example during surgery.
    Type: Application
    Filed: July 9, 2012
    Publication date: July 31, 2014
    Applicant: PHILIPPS-UNIVERSITÄT MARBURG
    Inventors: Torsten Steinmetzer, Sebastian Saupe
  • Patent number: 8778919
    Abstract: The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents 1, n represents 1, Z represents N or C, in particular N; —X1— represents C1-4alkyl, in particular methyl; —X2— represents —C1-4alkyl- or —C1-4alkyl-NR7—, in particular propyl, -ethyl-NR7— or -propyl-NR7—; —Y— represents —NR2—C1-6alkyl-CO—NR4—, -Het1-C1-6alkyl-CO—NR5— or -Het2-CO—NR6— and wherein the —C1-6alkyl-linker of —NR2—C1-6alkyl-CO—NR4— or -Het1-C1-6alkyl-CO—NR5— is optionally substituted with one or where possible two or more substituents selected from hydroxy, halo and phenyl; R1 represents hydrogen, chloro, fluoro or bromo; R2 represents —C1-4alkyl-, in particular ethyl or methyl; R7 represents hydrogen; R8 represents hydrogen; R4, R5 and R6 represent hydrogen; Het1 is selected from piperazinyl or piperidinyl, in particular -piperazinyl; Het2 selected from pyrrolidinyl or piperidinyl, in particular pyrrolid
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: July 15, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frederik Jan Rita Rombouts, Christopher John Love, Kristof Van Emelen, Sven Franciscus Anna Van Brandt, Tongfei Wu
  • Patent number: 8772272
    Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein a1-a2=a3-a4 represents a divalent radical selected from N—CH?CH—CH, N—CH?N—CH or CH—CH?N—CH; Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O— or —NR11—; X2 represents —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen; R4 represents hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R4 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R11 represents hydrogen; R12 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R13 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from m
    Type: Grant
    Filed: March 15, 2010
    Date of Patent: July 8, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Eddy Jean Edgard Freyne, Marc Willems, Pierre Henri Storck, Virginie Sophie Poncelet, Kristof Van Emelen, Peter Jacobus Johnnes Antonius Buijnsters, Werner Constant Johan Embrechts, Timothy Pietro Suren Perera
  • Patent number: 8772301
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: July 8, 2014
    Assignee: Sunovion Pharmaceuticals, Inc.
    Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
  • Patent number: 8765727
    Abstract: The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: July 1, 2014
    Assignee: Incyte Corporation
    Inventors: Andrew Paul Combs, Richard B. Sparks, Eddy Wai Tsun Yue, Hao Feng, Michael Jason Bower, Wenyu Zhu
  • Patent number: 8741884
    Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: June 3, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhiwei Yin, Zhongxing Zhang, Annapurna Pendri, Guo Li, Samuel Gerritz, Weixu Zhai, Paul Michael Scola, Li-Qiang Sun, Eric Mull
  • Patent number: 8697680
    Abstract: The present invention provides pharmaceutical compositions comprising substituted 1,4 naphthoquinones that are effective in preventing oligomerization of beta amyloid and subsequent pathologies associated with amyloid fibrils. These compositions are useful for the treatment of disease involving amyloidogenesis including neurodegenerative diseases such as Alzheimer's Disease or senile dementia. Particularly effective compositions comprise 1,4 naphthoquinones substituted with an amino acid residue selected from a heterocyclic or aromatic amino acid.
    Type: Grant
    Filed: September 6, 2009
    Date of Patent: April 15, 2014
    Assignee: Ramot At Tel Aviv University Ltd.
    Inventors: Roni Scherzer, Ehud Gazit, Daniel Segal
  • Patent number: 8674088
    Abstract: The invention is related to anti-viral phosphinate compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: March 18, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Anthony Casarez, Kleem Chaudhary, Aesop Cho, Michael Clarke, Edward Doerffler, Maria Fardis, Choung U. Kim, Hyungjung Pyun, Xiaoning C. Sheng, Jianying Wang
  • Publication number: 20130289075
    Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPB (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.
    Type: Application
    Filed: June 25, 2013
    Publication date: October 31, 2013
    Inventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
  • Patent number: 8546291
    Abstract: A compound represented by formula (1): wherein Y1 to Y4 each independently represent any one of the following groups: in which R? represents a hydrogen atom or a monovalent hydrocarbon group; P1 to P4 each independently represent a group of atoms necessary for forming a heterocyclic ring together with each of Y1 to Y4 and the two carbon atoms adjacent to each of Y1 to Y4, respectively; P5 and P6 each independently represent a group of atoms necessary for forming a cyclic skeleton together with the carbon atom to which Z1 bonds or Z2 bonds and the two carbon atoms adjacent to the carbon atom to which Z1 bonds or Z2 bonds; P1 and P2, P2 and P6, P6 and P4, P4 and P3, P3 and P5, and P5 and P1 may further combine with each other to form a ring; Q1 and Q2 each independently represent a connecting group or a direct binding; and Z1 and Z2 each independently represent any one of the following groups; —NR?2, —OR?, —SR?, —PR?2 in which R? represents a hydrogen atom or a monovalent hydrocarbon group,
    Type: Grant
    Filed: September 5, 2008
    Date of Patent: October 1, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Tadafumi Matsunaga, Nobuyoshi Koshino, Hideyuki Higashimura, Yusuke Ishii
  • Patent number: 8486928
    Abstract: The present invention relates to compounds which are effective as catalysts for dismutating superoxide and, more particularly, the manganese or iron complexes of substituted, unsaturated heterocyclic 16-membered macrocyclic complexes that catalytically dismutate superoxide. It also relates to methods of using these complexes to reduce the concentration or the effects of superoxide, pharmaceutical compositions comprising these compounds or their metal complexes, and methods of treating conditions associated with excessive superoxide activity.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: July 16, 2013
    Assignee: Galera Therapeutics
    Inventor: Dennis P. Riley
  • Patent number: 8394786
    Abstract: The present invention concerns the compounds of formula wherein Z represents NH; Y represents —C3-9alkyl-, —C2-9alkenyl-, —C3-7alkyl-CO—NH optionally substituted with amino, mono- or di(C1-4alkyl)amino or C1-4alkyloxycarbonylamino-, —C3-7alkenyl-CO—NH— optionally substituted with amino, mono- or di(C1-4alkyl)amino- or C1-4alkyloxycarbonylamino-, C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-5alkyl-CONR15—C1-5alkyl-, —C1-3alkyl-NH—CO-Het20-, —C1-2alkyl-CO-Het21-CO—, —C1-2alkyl-NH—CO—CR16R17—NH—, —C1-2alkyl-CO—NH—CR18R19—CO—, —C1-2alkyl-CO—NR20—C1-3alkyl-CO—, or —NR22—CO—C1-3alkyl-NH—; X1 represents a direct bond, O or —O—C1-2alkyl-; X2 represents a direct bond, —CO—C1-2alkyl-, NR12, —NR12—C1-2alkyl-, —O—N?CH— or —C1-2alkyl-; R1 and R2 are hydrogen or halo; R3 are hydrogen; R4 represents hydrogen or C1-4alkyloxy; R12 and R13 are hydrogen or C1-4alkyl; R14 and R15 are hydrogen; R16 and R17 each independently represent hydrogen or C1-4alkyl; R18 and R19 are hydrogen or C1-4
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: March 12, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Eddy Jean Edgard Freyne, Timothy Pietro Suren Perera, Peter Jacobus Johannes Antonius Buijnsters, Marc Willems, Gaston Stanislas Marcella Diels, Werner Constant Johan Embrechts, Peter ten Holte, Frederik Jan Rita Rombouts, Carsten Schultz-Fademrecht
  • Patent number: 8389560
    Abstract: This invention relates to macrocyclic compounds of formula (I) shown in the specification. These compounds can be used to treat hepatitis C virus infection.
    Type: Grant
    Filed: September 15, 2009
    Date of Patent: March 5, 2013
    Assignee: TaiGen Biotechnology Co., Ltd.
    Inventors: Chen-Fu Liu, Kuang-Yuan Lee, Pei-Chin Cheng, Yo-Chin Liu, Pin Lo, Kuo-Feng Tseng, Chih-Ming Chen, Chi-Hsin Richard King, Chu-Chung Lin
  • Publication number: 20120261650
    Abstract: An organic electroluminescent device comprising: a pair of electrodes comprising an anode and a cathode, and one or more layers arranged between the anode and the cathode; wherein at least one of the one or more layers is a light emitting layer and wherein the one or more layers, comprises an organic compound represented by a substituted 2,2?-biimidazole.
    Type: Application
    Filed: October 21, 2011
    Publication date: October 18, 2012
    Applicant: Commonwealth Scientific and Industrial Research Organisation
    Inventors: James Matthew MacDonald, Mark Bown, Kazunori Ueno, Karl Peter Weber, Jenny Lee O'Connell, Tadahiko Hirai
  • Publication number: 20120238745
    Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.
    Type: Application
    Filed: January 9, 2012
    Publication date: September 20, 2012
    Applicant: AnaSpec Incorporated
    Inventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang, Xiang Guobing
  • Publication number: 20120172350
    Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: September 9, 2010
    Publication date: July 5, 2012
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
  • Patent number: 8193346
    Abstract: The present invention relates to a process for the preparation of macrocyclic compounds that are useful as hepatitis C virus (HCV) protease inhibitor compounds.
    Type: Grant
    Filed: December 4, 2008
    Date of Patent: June 5, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Seble Wagaw, Matthew Ravn, Kenneth Engstrom, Guoyou Xu, Zhe Wang, Ying Sun, Deqiang Niu, Yat Sun Or
  • Patent number: 8182695
    Abstract: This invention is related to the fields of organic chemistry and nanotechnology. In particular, it relates to materials and methods for the preparation of organic synthons and bridged macrocyclic module compounds. The bridged macrocyclic module compounds may be used to prepare macrocyclic compositions such as nanofilms, which may be useful for filtration.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: May 22, 2012
    Inventors: Jeffery A. Whiteford, William Freeman, Joshua W. Kriesel
  • Patent number: 8173803
    Abstract: Tribenzo-1,4,7-triazacyclononane and derivatives thereof having a formula (I) are disclosed. Methods of making tribenzo-1,4,7-triazacyclononane and related compounds also are disclosed.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: May 8, 2012
    Assignee: Loyola University of Chicago
    Inventors: Daniel P. Becker, Andria M. Panagopoulos, Marlon R. Lutz, Jr.
  • Patent number: 8110679
    Abstract: Nanofilms useful for filtration are prepared from oriented amphiphilic molecules and oriented macrocyclic modules. The amphiphilic species may be oriented on an interface or surface. The nanofilm may be prepared by depositing or attaching an oriented layer to a substrate. A nanofilm may also be prepared by coupling the oriented macrocyclic modules to provide a membrane.
    Type: Grant
    Filed: July 31, 2008
    Date of Patent: February 7, 2012
    Assignee: Covalent Partners LLC
    Inventors: Joshua W. Kriesel, Timothy B. Karpishin, Donald B. Bivin, Grant Merrill, Martin S. Edelstein, Thomas H. Smith, Jeffery A. Whiteford, Robert T. Jonas, Mark Micklatcher, Serena Joshi
  • Publication number: 20120015907
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: April 19, 2011
    Publication date: January 19, 2012
    Applicant: NOVARTIS AG
    Inventors: David BARNES, Rajiv CHOPRA, Scott Louis COHEN, Jiping FU, Mitsunori Kato, Peichao LU, Mohindra SEEPERSAUD, Wei ZHANG
  • Publication number: 20110315933
    Abstract: The present invention relates to metal complexes of the general formulae I to V, in particular as emitter molecules in organic electronic devices, to ligands of the general formulae Ia to Va, and to the use thereof for the preparation of metal complexes, to a layer and an electronic device which comprise the compounds according to the invention, and to a process for the preparation of the compounds according to the invention.
    Type: Application
    Filed: February 15, 2010
    Publication date: December 29, 2011
    Applicant: MERCK PATENT GMBH
    Inventors: Philipp Stoessel, Holger Heil, Dominik Joosten, Christof Pflumm, Anja Gerhard
  • Publication number: 20110294772
    Abstract: Use of squaramide-based macrocylic compounds as kinase inhibitor agents and as anti-tumour agents. More specifically, said compounds are used to treat diseases such as cancer, diabetes, neurodegenerative diseases, HIV replication, etc.
    Type: Application
    Filed: December 9, 2009
    Publication date: December 1, 2011
    Inventors: Antonio Costa Torres, Maria del Carmen Rotger Pons, Silvia Fernández De Mattos, Priam De Villalonga Smith
  • Publication number: 20110224184
    Abstract: The present invention provides pharmaceutical compositions comprising substituted 1,4 naphthoquinones that are effective in preventing oligomerization of beta amyloid and subsequent pathologies associated with amyloid fibrils. These compositions are useful for the treatment of disease involving amyloidogenesis including neurodegenerative diseases such as Alzheimer's Disease or senile dementia. Particularly effective compositions comprise 1,4 naphthoquinones substituted with an amino acid residue selected from a heterocyclic or aromatic amino acid.
    Type: Application
    Filed: September 6, 2009
    Publication date: September 15, 2011
    Applicant: RAMOT AT TEL AVIV UNIVERSITY LTD.
    Inventors: Roni Scherzer, Ehud Gazit, Daniel Segal
  • Patent number: 7973026
    Abstract: The present invention relates to tetracyclic thienopyrrole compounds of formula (I), wherein Ar, A, D1, D2, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
    Type: Grant
    Filed: May 3, 2006
    Date of Patent: July 5, 2011
    Assignee: Istituto Di Ricerche Di Biologia Molecolare P. Angeletti SpA
    Inventors: Stefania Colarusso, Joerg Habermann, Frank Narjes, Simona Ponzi, Maria del Rosario Rico Ferreira
  • Publication number: 20110160450
    Abstract: The invention relates to an explosive comprising 2,6,10-trinitro-s-heptazine and/or derivatives thereof as an active chemical compound.
    Type: Application
    Filed: July 24, 2009
    Publication date: June 30, 2011
    Applicant: DURFERRIT GMBH
    Inventor: Ulrich Baudis
  • Patent number: 7960181
    Abstract: The invention relates to methods of determining potassium ions in a sample, wherein the ions are contacted with a compound having chromophoric moiety and an ionophoric moiety, where the ionophoric moiety interacts with the potassium ions present in the sample, resulting in the chromophoric moiety changing its radiation absorption properties in the ultraviolet and visible regions of the spectrum. For example, a change in an intensity of an absorption maximum is measured and the ion concentration is determined accordingly.
    Type: Grant
    Filed: May 2, 2007
    Date of Patent: June 14, 2011
    Assignee: OPTI Medical Systems
    Inventors: Huarui He, Chao Lin, Neeta Raje, Chuseng Liu
  • Patent number: 7955859
    Abstract: A rare-earth fluorescent complex which forms a fluorescent complex with two or more rare-earth metals such as europium and terbium and can effectively be excited at a wavelength of 340 nm or longer; a fluorescent labeling agent comprising the rare-earth fluorescent complex; a method of fluorescent labeling in which the rare-earth fluorescent complex is used as a labeling agent; and a method of fluorometric analysis in which the fluorescent labeling agent is used. The rare-earth fluorescent complex is characterized by having a cyclic ligand comprising a 4-biphenyl-2,2?:6?,2?-terpyridine skeleton and a 2,6-bis(3?-aminomethyl-1?-pyrazolyl)pyrazine skeleton bonded thereto.
    Type: Grant
    Filed: August 31, 2006
    Date of Patent: June 7, 2011
    Assignee: Japan Science and Technology Agency
    Inventors: Kazuko Matsumoto, Nishioka Takuya, Miyabe Masahito
  • Publication number: 20110071179
    Abstract: The present invention relates to the use of novel macrocyclic compounds of Formula I, wherein the variables Q, Q1, Q2, Q3, and Q4 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Application
    Filed: September 17, 2010
    Publication date: March 24, 2011
    Inventors: Alam Jahangir, Stephen M. Lynch, Michael Soth, Hanbiao Yang
  • Publication number: 20110065694
    Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: September 9, 2010
    Publication date: March 17, 2011
    Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang
  • Publication number: 20110053916
    Abstract: The present invention relates to compounds useful as inhibitors of treating tuberculosis.
    Type: Application
    Filed: August 12, 2010
    Publication date: March 3, 2011
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Tiansheng Wang, Brian Hanzelka, Ute Muh, Guy Bemis
  • Publication number: 20110015059
    Abstract: A compound represented by formula (1): wherein Y1 to Y4 each independently represent any one of the following groups: in which R? represents a hydrogen atom or a monovalent hydrocarbon group; P1 to P4 each independently represent a group of atoms necessary for forming a heterocyclic ring together with each of Y1 to Y4 and the two carbon atoms adjacent to each of Y1 to Y4, respectively; P5 and P6 each independently represent a group of atoms necessary for forming a cyclic skeleton together with the carbon atom to which Z1 bonds or Z2 bonds and the two carbon atoms adjacent to the carbon atom to which Z1 bonds or Z2 bonds; P1 and P2, P2 and P6, P6 and P4, P4 and P3, P3 and P5, and P5 and P1 may further combine with each other to form a ring; Q1 and Q2 each independently represent a connecting group or a direct binding; and Z1 and Z2 each independently represent any one of the following groups; —NR?2, —OR?, —SR?, —PR?2 in which R? represents a hydrogen atom or a monovalent hydrocarbon group, and whe
    Type: Application
    Filed: September 5, 2008
    Publication date: January 20, 2011
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Tadafumi Matsunaga, Nobuyoshi Koshino, Hideyuki Higashimura, Yusuke Ishii
  • Publication number: 20100292465
    Abstract: Novel N-heterocyclic carbene ligand precursors, N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are provided. Metal-carbene complexes comprising N-heterocyclic carbene ligands can be chiral, which are useful for catalyzing enantioselective synthesis. Methods for the preparation of the N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are given.
    Type: Application
    Filed: February 15, 2008
    Publication date: November 18, 2010
    Applicant: University of Florida Research Foundation, Inc.
    Inventors: Adam Steven Veige, Mathew S. Jeletic, Roxy J. Lowry, Khalil A. Abboud
  • Patent number: 7767810
    Abstract: Certain macrocyclic modules comprising 3-24 synthons are provided herein. Each synthon is independently selected from cyclic substituents, wherein each synthon selected is bonded to the next through a linker to form a closed ring that defines a pore. One or more lipophilic moieties and one or more hydrophilic moieties are bonded to one or more of the synthons, resulting in the formation of the desired macrocyclic modules. Those modules may be subsequently linked to one another to form selectively-permeable membranes. Membranes comprising macrocyclic modules may be useful in filtering certain molecular species from a solution. Selective passage of particular species is determined, in part, by the size of the module's pore and the nature of the lipophilic/hydrophobic species attached thereto. Also provided are methods of making and using macrocyclic modules and membranes.
    Type: Grant
    Filed: August 8, 2005
    Date of Patent: August 3, 2010
    Assignee: Covalent Partners, LLC
    Inventors: Joshua W. Kriesel, Timothy B. Karpishin, Donald B. Bivin, Grant Merrill, Martin S. Edelstein, Thomas H. Smith, Jeffery A. Whiteford, Robert T. Jonas
  • Patent number: 7750149
    Abstract: Disclosed are carbenes of the general formula: and including salts thereof, and metal complexes thereof. The carbenes are useful in any reaction where carbenes and carbene-metal complexes are used. The carbenes disclosed herein are particularly useful in asymmetric catalysis.
    Type: Grant
    Filed: April 11, 2005
    Date of Patent: July 6, 2010
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Shannon S. Stahl, Christopher C. Scarborough
  • Patent number: 7737272
    Abstract: Transition metal complexes include a diazaphosphacycle of formula III and a transition metal. The phosphorus atom of the diazaphosphacycle is bonded to the transition metal and the diazaphosphacycle of formula III has the following structure where the variables have the values set forth herein.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: June 15, 2010
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Clark R. Landis, Wiechang Jin, Jonathan S. Owen, Thomas P. Clark
  • Patent number: 7723322
    Abstract: The present invention provides a compound of the formula wherein R1 is an ammonium bridge. The compounds of the present invention can be linked to a biological molecule that targets a specific type of cell. The compounds of the present invention can trap isotopic fluorine so that when the biological molecule accumulates in the desired type of cell, the isotopic fluorine is imaged by positron emission tomography (PET).
    Type: Grant
    Filed: March 29, 2007
    Date of Patent: May 25, 2010
    Assignee: The Regents of the University of California
    Inventor: Mark Mascal
  • Patent number: 7687620
    Abstract: Compounds of Formula I or a pharmaceutically acceptable salt thereof are provided: where R1 through R7 are defined herein. The compounds of Formula I are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.
    Type: Grant
    Filed: September 11, 2006
    Date of Patent: March 30, 2010
    Assignee: Wyeth LLC
    Inventor: P. Sivaramakrishnan Ramamoorthy
  • Publication number: 20100076046
    Abstract: Compounds of the formula (I) wherein A, B, D, M, Ar, W, X, Y, Z and R1 are as defined herein, are useful in the prevention and treatment of hepatitis C infections. The compounds, their preparation, pharmaceutical compositions containing them and their use in medicine are disclosed.
    Type: Application
    Filed: December 19, 2007
    Publication date: March 25, 2010
    Applicant: Istituto di Ricerche di Biologia Molecolare P. Angeletti SPA
    Inventors: Ian Stansfield, Uwe Koch, Joerg Habermann, Frank Narjes
  • Patent number: 7674899
    Abstract: This invention relates to novel azacyclic derivatives and their use as pharmaceuticals. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Grant
    Filed: February 1, 2005
    Date of Patent: March 9, 2010
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen, Daniel B Timmermann
  • Publication number: 20100041728
    Abstract: Compounds of the formula 1: including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
    Type: Application
    Filed: February 8, 2008
    Publication date: February 18, 2010
    Inventors: Dmitry Antonov, Susana Ayesa Alvarez, Anna Karin Gertrud Linnea Belfrage, Carl Erik Daniel Jönsson, David Craig Mc Gowan, Karl Magnus Nilsson, Pierre Jean-Marie Bernard Raboisson, Åsa Annica Kristina Rosenquist, Bengt Bertil Samuelsson