Plural Nitrogens In The Hetero Ring Patents (Class 540/469)
  • Publication number: 20120136037
    Abstract: The present application describes deuterium-enriched ruboxistaurin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: September 3, 2008
    Publication date: May 31, 2012
    Applicant: Protia, LLC
    Inventor: Anthony W. Czarnik
  • 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
  • Publication number: 20120093767
    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: Application
    Filed: April 14, 2011
    Publication date: April 19, 2012
    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: 8129365
    Abstract: The invention provides chromoionophore compounds comprising a triazacryptand (TAC) K+ ionophore conjugated to at least a first chromophoric moiety (e.g., xanthylium dyes and derivatives thereof). In related embodiments, the chromoionophore compounds further comprise a second chromophoric moiety which is insensitive to potassium binding by the TAC ionophore, thus providing for dual wavelength detection and absolute determination of K+ concentration. The invention further provides methods and kits for the determination of K+ concentrations in biological systems, either in vitro or in vivo, using embodiments of inventive chromoionophores.
    Type: Grant
    Filed: October 11, 2006
    Date of Patent: March 6, 2012
    Assignee: The Regents of the University of California
    Inventors: Alan Verkman, Prashant A. Padmawar
  • Publication number: 20120041190
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: February 10, 2011
    Publication date: February 16, 2012
    Inventors: James R. Corte, Tianan Fang, Carl P. Decicco, Donald J.P. Pinto, Karen A. Rossi, Zilun Hu, Yoon Jeon, Mimi L. Quan, Joanne M. Smallheer, Yufeng Wang, Wu Yang
  • Publication number: 20120021897
    Abstract: A compound represented by the following formula (1): wherein, Y1, Y2, Y3 and Y4 represent a group represented by any of the above formulae; P1, P2, P3 and P4 are an atomic group required for forming an aromatic heterocyclic ring; P5 and P6 are an atomic group required for forming an aromatic ring; Z1 and Z2 represent OR?, —SR? or —NR?2, wherein R? represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; Q1 and Q2 represent a direct bond or a linking group; a P1-containing ring and a P2-containing ring are bonded to form Q1-containing fused structure; a P3-containing ring and a P4-containing ring are bonded to form Q2-containing fused structure; can be used as a ligand of a metal complex, and the metal complex is useful for a catalyst.
    Type: Application
    Filed: February 19, 2010
    Publication date: January 26, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Masatoshi Iwata, Tadafumi Matsunaga, Nobuyoshi Koshino, Hideyuki Higashimura
  • Publication number: 20110294831
    Abstract: The present invention relates to certain salts of a 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (Compound I) which have been found to have improved properties. In particular the present invention relates to the citrate salt of this compound. The invention also relates to pharmaceutical compositions containing the citrate salt and methods of use of the citrate salt in the treatment of certain medical conditions.
    Type: Application
    Filed: December 9, 2009
    Publication date: December 1, 2011
    Applicant: S*BIO Pte Ltd.
    Inventors: Brian Dymock, Cheng H. Lee, Anthony D. William
  • Publication number: 20110294801
    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: Application
    Filed: September 3, 2009
    Publication date: December 1, 2011
    Applicant: MERCK PATENT GMBH
    Inventors: Henry Yu, Lizbeth Celeste De Selm, Xuliang Jiang, Benny C. Askew, Jr., Srinivasa R. Karra, Andreas Goutopoulos
  • Patent number: 8058266
    Abstract: The present invention describes linking a therapeutic agent to a compound which is known to be naturally concentrated in a tissue affected by, or that is causing, a disease, to create a prodrug for treatment of the disease. Embodiments of the present invention include a new class of carotenoid-linked drugs to treat such blinding retinal disease such as age-related macular degeneration, retinoblastoma, and diabetic macular edema. For example, the present invention comprises a method for the treatment of a disorder of the eye comprising linking a therapeutic agent to a xanthophyll carotenoid to create a prodrug, and administering a therapeutically effective amount of the prodrug to an individual in need of treatment. Provided are prodrugs for treatment of retinoblastoma, cystoid macular edema (CME), exudative age-related macular degeneration (AMD), diabetic retinopathy, diabetic macular edema, or inflammatory disorders.
    Type: Grant
    Filed: July 13, 2007
    Date of Patent: November 15, 2011
    Assignee: The University of Georgia Research Foundation, Inc
    Inventors: Dennis Michael Marcus, Chung Kwang Chu
  • Publication number: 20110251384
    Abstract: A cyclic carbodiimide compound which is useful as an end-sealing agent for polymer compounds. The cyclic carbodiimide compound is represented by the following formula (i): In the above formula, X is a divalent group or a tetravalent group represented by the following formula (i-4). When X is divalent, q is 0 and when X is tetravalent, q is 1. Ar1 to Ar4 are each independently an aromatic group. They may be substituted by an alkyl group having 1 to 6 carbon atoms or phenyl group.
    Type: Application
    Filed: December 15, 2009
    Publication date: October 13, 2011
    Applicant: TEIJIN LIMITED
    Inventors: Shinichiro Shoji, Hirotaka Suzuki
  • Publication number: 20110251215
    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: Application
    Filed: January 22, 2010
    Publication date: October 13, 2011
    Applicant: INCYTE CORPORATION
    Inventors: Andrew Paul Combs, Richard B. Sparks, Eddy Wai Tsun Yue, Hao Feng, Michael Jason Bower, Wenyu Zhu
  • Patent number: 7947671
    Abstract: Ecteinascidin compounds with a quinone ring for ring E are active as anti-cancer agents. Related processes and compounds are provided.
    Type: Grant
    Filed: April 12, 2010
    Date of Patent: May 24, 2011
    Assignee: Pharma Mar, S.A.
    Inventors: Valentin Martinez Barrasa, Pilar Gallego, Carmen Cuevas, Simon Munt, Ignacio Manzanares, Roberto Menchaca, Natividad Rodriguez, Alberto Rodriguez
  • 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: 20110065914
    Abstract: The invention relates to a synthetic strategy of using perfluoro crown ethers and other macrocycles to bind to [18F]-labelled fluorination reactions. The optional use of implementing perfluoro kryptofix 2.2.2 in this process is also disclosed. The present invention also claims perfluoro kryptofix structures that are suitable for use in 18F-labelling of fluorous based structures.
    Type: Application
    Filed: August 28, 2008
    Publication date: March 17, 2011
    Inventors: BENGT Langstrom, Johan Ulin, Farhad Karimi
  • Patent number: 7897787
    Abstract: A compound represented by the following general formula (I): [wherein R1 and R2 independently represent hydrogen atom, or a group represented by the following formula (A): (wherein X1 and X2 represent hydrogen atom, an alkyl group, an alkoxy group, or a halogen atom), provided that R1 and R2 do not simultaneously represent hydrogen atom; R3 and R6 represent an alkyl group; R4 and R7 represent hydrogen atom, an alkyl group, carboxy group, an alkoxycarbonyl group, or sulfo group; and R5 and R8 represents an alkyl group, an aryl group, an alkoxycarbonyl group, a vinyl group, a thienyl group, or a pyrrolyl group], or a salt thereof, which is usable for efficient screening for a chemical substance having applicability as a catalyst of the reaction of Michael addition.
    Type: Grant
    Filed: September 13, 2006
    Date of Patent: March 1, 2011
    Assignee: The University of Tokyo
    Inventors: Takuya Matsumoto, Takuji Shoda, Yasuteru Urano, Tetsuo Nagano
  • Publication number: 20110015238
    Abstract: It is intended to provide highly safe and efficacious blood flow promoters for cauda equina tissues. Among prostaglandin-like compounds having a weak hypotensive effect, compounds having an effect of promoting the blood flow in cauda equina tissues (excluding limaprost) are useful as highly safe blood flow promoters for cauda equina tissues and, therefore, are efficacious in preventing and/or treating lumbar pain, lower limb pain, lower limb palsy, intermittent claudication, vesicorectal failure, hypogonadism, etc. caused by cauda equina injuries.
    Type: Application
    Filed: September 24, 2010
    Publication date: January 20, 2011
    Applicant: Ono Pharmaceutical Co., Ltd.
    Inventors: Kazuyuki Ohmoto, Akihiro Kinoshita, Yoshihisa Kamanaka, Hidekazu Matsuya
  • Publication number: 20100330584
    Abstract: Cell permeable metal ion indicator compounds and methods of their use and synthesis are described. The compound comprises a metal chelating moiety (Mc), a reporter molecule and two or more lipophilic groups (GL) covalently bonded through a linker to the reporter molecule, wherein the lipophilic groups, when present in a live cell, are cleaved resulting in two or more negatively charged groups.
    Type: Application
    Filed: June 5, 2008
    Publication date: December 30, 2010
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Kyle Gee, Vladimir Martin
  • Patent number: 7767659
    Abstract: Ecteinascidin compounds with a quinone ring for ring E are active as anti-cancer agents. Related processes and compounds are provided.
    Type: Grant
    Filed: February 4, 2003
    Date of Patent: August 3, 2010
    Assignee: Pharma Mar, S.A.
    Inventors: Valentin Martinez Barrasa, Pilar Gallego, Carmen Cuevas, Simon Munt, Ignacio Manzanares, Roberto Menchaca, Natividad Rodriguez, Alberto Rodriguez
  • Publication number: 20100190804
    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: Application
    Filed: January 22, 2010
    Publication date: July 29, 2010
    Applicant: INCYTE CORPORATION
    Inventors: Andrew Paul Combs, Richard B. Sparks, Eddy Wai Tsun Yue, Hao Feng, Michael Jason Bower, Wenyu Zhu
  • Publication number: 20100173913
    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 mor
    Type: Application
    Filed: March 15, 2010
    Publication date: July 8, 2010
    Applicant: Janssen Pharmaceutica N.V.
    Inventors: Eddy Jean Edgard Freyne, Marc Willems, Pierre Henri Storck, Virginie Sophie Poncelet, Kristof Van Emelen, Peter Jacobus Johannes Antonius Buijnsters, Werner Constant Johan Embrechts, Timothy Pietro Suren Perera
  • Publication number: 20100160310
    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 Z1 and Z2 represent NH; Y represents —C3-9alkyl-, —C3-9alkenyl-, —C1-5alkyl-NR6—C1-5alkyl-, —C1-5alkyl-NR7—CO—C1-5alkyl-, —C1-6alkyl-CO—NH—, —C1-6alkyl-NH—CO—, —C1-2alkyl-CO-Het10-CO—, —C1-3alkyl-NH—CO-Het3-, -Het4-C1-3alkyl-CO—NH—C1-3alkyl-, —C1-2alkyl-NH—CO-L1-NH—, —NH—CO-L2-NH—, —C1-2alkyl-CO—NH-L3-CO—, —C1-2alkyl-NH—CO-L1-NH—CO—C1-3alkyl-, —C1-2alkyl-CO—NH-L3-CO—NH—C1-3alkyl-, —C1-2alkyl-NR11—CH2—CO—NH—C1-3alkyl-, Het5-CO—C1-2alkyl-, (C1-5alkyl-CO—NH—C1-3alkyl-CO—NH, —C1-5alkyl-NR13—CO—C1-3alkyl-NH—, —C1-3alkyl-NH—CO-Het27-CO—, or —C1-3alkyl-CO-Het28-CO—NH—; X1 represents a direct bond, O, —O—C1-2alkyl-, —CO—C1-2alkyl-, —NR16—C1-2alkyl-, —CO—NR17—, Het23-C1-2alkyl- or C1-2alkyl; X2 represents a direct bond, O, —O—C1-2alkyl-, —CO—C1-2alkyl-, —NR18—C1-2alkyl-, —CO—NR19—, Het24—C1-2alkyl- or C1-2alkyl; R1 and R5 each independen
    Type: Application
    Filed: December 8, 2005
    Publication date: June 24, 2010
    Inventors: Eddy Jean Edgard Freyne, Marc Willems, Werner Constant Johan Embrechts, Kristof Van Emelen, Sven Franciscus Anna Van Brandt, Frederik Jan Rita Rombouts
  • Publication number: 20100152174
    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 Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-2alkyl-NR21—H2—CO—NH—C1-3alkyl- or —C1-2alkyl-NR23—CO—CR16R17—NH—; X1 represents O or —O—C1-2alkyl-; X2 represents a direct bond, C1-2alkyl, —CO—C1-2alkyl or NR12—C1-2alkyl; R1 represents hydrogen or halo; R2 represents halo, acetylene or Het1; R3 represents hydrogen or cyano; R4 represents Ar4—C1-4alkyloxy-, C1-4alkyloxy- or C1-4alkyloxy substituted with one or where possible two or more substituents selected from Het2, NR7R8, hydroxy and C1-4alkyloxy-C1-4alkyloxy-; R7 represents hydrogen or C1-4alkyl; R8 represents C1-4alkyl substituted with NR25R26 or C1-4alkylsulfonyl; R12 represents hydrogen or C1-4alkyl-; R13 represents Ar6-sulfonyl or C1-6alkyloxycarbonyl optionally substituted with phenyl; R16 and R17 represents hydr
    Type: Application
    Filed: December 8, 2005
    Publication date: June 17, 2010
    Inventors: Eddy Jean Edgard Freyne, Marc Willems, Peter Ten Holte, Alexandra Papanikos, Werner Constant John Embrechts, Pierre Henri Storck, Virginie Sophie Poncelet, Werner Constant Johan Embrechts, Pierre Henri Storck, Virginie Sophie Poncelet
  • Publication number: 20100086482
    Abstract: The present invention describes a process for preparing new looped dendrimer and dendron compounds by controlling the molar amount of branch cell reagent monomer that is combined with various cores bearing core-XR functionalities (e.g., primary, or secondary amines, thiol, or epoxy functionalities). These looped, macrocyclic structures are more robust to various conditions, with greater resistance to acid/base hydrolysis. Alternatively, the looped, macrocyclic structure may offer new orientations that would qualify it as a better chelation ligand for metals, and other similar uses.
    Type: Application
    Filed: December 28, 2007
    Publication date: April 8, 2010
    Applicant: Dendritic Nanotechnologies, Inc.
    Inventors: Donald A. Tomalia, Douglas R. Swanson, Baohua Huang, Veera Reddy Pulgam
  • Publication number: 20100069424
    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 Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —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, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferab
    Type: Application
    Filed: November 24, 2009
    Publication date: March 18, 2010
    Inventors: Eddy Jean Edgard FREYNE, Peter Jacobus Johannes Antonius Buijnsters, Kristof Van Emelen, Werner Constant Johan Embrechts, Timothy Pietro Suren Perera
  • Publication number: 20100029627
    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 Y represents —C3-9alkyl-, —C1-5alkyl-NR6—C1-5alkyl- or —C1-5alkyl-NR7—CO—C1-5alkyl-; X1 represents —O—; X2 represents NR5—C1-2alkyl-; R1 represents hydrogen, halo or Het3-O—; R2 represents hydrogen; R3 represents hydroxy, C1-4alkyloxy- or C1-4alkyloxy substituted with one or two substituents each independently selected from Het4, hydroxy, C1-4alkyloxy-, C1-4alkyloxy-C1-4alkyloxy and NR9R10; R5 represents hydrogen or C1-4alkyl; R6 represents hydrogen or C1-4alkyl; R7 represents hydrogen; R9 and R10 each independently represent hydrogen; C1-4alkyl-S(?O)2—C1-4alkyl-C(?O)—; C1-4alkyl or C1-4alkyl substituted with hydroxy; Het3 represents pyridinyl optionally substituted with C1-4alkyl; Het4 represents morpholinyl, piperidinyl or piperazinyl wherein said Het4 is optionally substituted with hydroxy-C1-4alkyl or C1-4alkyl-S(?O)2—C1-4al
    Type: Application
    Filed: July 12, 2007
    Publication date: February 4, 2010
    Inventors: Alexandra Papanikos, Freyne Eddy Jean Edgard, Peter Ten Holte, Marc Willems, Werner Constant Johan Embrechts, Laurence Anne Mevellec, Fierre-Henri Storck
  • Patent number: 7625887
    Abstract: It is intended to provide a TGR5 receptor agonist containing a fused ring compound represented by the following general formula, its salt or a prodrug thereof: (1) wherein ring A represents an optionally substituted aromatic ring; and the ring B? represents a 5- to 8-membered ring having one or more substituents; which is useful in treating various diseases.
    Type: Grant
    Filed: January 27, 2004
    Date of Patent: December 1, 2009
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Fumio Itoh, Shuji Hinuma, Naoyuki Kanzaki, Yuji Kawamata, Taisuke Tawaraishi, Yuji Ishichi, Mariko Hirohashi
  • Publication number: 20090286770
    Abstract: The present invention relates to the use of staurosporines derivatives for the preparation of a drug for the treatment of diseases involving ras or FGFR3 signalling pathways and l or c-fos transcription, especially for the curative and/or prophylactic treatment of myeloma or multiple Myeloma, and to a method of treating diseases involving ras or FGFR3 signalling pathways and/or c-fos transcription.
    Type: Application
    Filed: December 7, 2005
    Publication date: November 19, 2009
    Inventors: D. Gary Gilliland, James Douglas Griffin, Jing Chen, Kenneth C. Anderson
  • Publication number: 20090258886
    Abstract: The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to heteroalkyl linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other conditions or disorders associated with kinases.
    Type: Application
    Filed: November 15, 2006
    Publication date: October 15, 2009
    Applicant: S*BIO Pte Ltd.
    Inventors: Stephanie Blanchard, Kantharaj Ethirajulu, Cheng Hsia Angeline Lee, Harish Kumar Mysore Nagaraj, Anders Poulsen, Eric T. Sun, Yee Ling Evelyn Tan, Ee Ling Teo, Anthony Deodaunia William
  • Patent number: 7582280
    Abstract: The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.
    Type: Grant
    Filed: July 8, 2008
    Date of Patent: September 1, 2009
    Assignee: Bracco International B.V.
    Inventors: Ramachandran S. Ranganathan, Helen Fan, Michael F. Tweedle, Rolf E. Swenson
  • Publication number: 20090202521
    Abstract: A bifunctional polyazamacrocyclic chelating agent of the formula (I): wherein: and the variables A, L, Q, Q1, X, Y, Z, Z1, m, n and r are as defined in the description of the present application. Also described is a complex of the above chelating agent to an ion of a metal ion, such as an ion of 90Y, 111Li or 177Lu; a conjugate of the complex covalently attached to a biological carrier; and a pharmaceutical composition containing the conjugate. A method of therapeutic treatment of a mammal involving administration of the pharmaceutical composition is also described.
    Type: Application
    Filed: March 6, 2007
    Publication date: August 13, 2009
    Applicant: MDS (Canada) Inc.
    Inventors: Zoltan Kovaks, Garry E. Kiefer, Corinne Bensimon, A. Dean Sherry, Gyula Tircso
  • Publication number: 20090186830
    Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.
    Type: Application
    Filed: June 3, 2008
    Publication date: July 23, 2009
    Inventors: Roger Aki Fujimoto, Philipp Krastel, Matthew J. LaMarche
  • Publication number: 20090180985
    Abstract: The present invention discloses compounds of formula I, 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. More specifically, the invention relates to oxime compounds containing a carbocyclic P2 unit, and the oxime is tethered to one of the carboxylic acid on P2. 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: Application
    Filed: December 18, 2008
    Publication date: July 16, 2009
    Inventors: DONG LIU, Yat Sun Or, Zhe Wang
  • Publication number: 20090075999
    Abstract: The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.
    Type: Application
    Filed: November 15, 2006
    Publication date: March 19, 2009
    Applicant: S*BIO Pte Ltd.
    Inventors: Stephanie Blanchard, Cheng Hsia Angeline Lee, Harish Kumar Mysore Nagaraj, Anders Poulsen, Eric T. Sun, Yee Ling Evelyn Tan, Anthony Deodaunia William
  • Publication number: 20090075869
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Application
    Filed: April 28, 2006
    Publication date: March 19, 2009
    Inventors: M. Katharine Holloway, Nigel J. Liverton, Steven W. Ludmerer, John A. McCauley, David Olsen, Michael T. Rudd, Joseph P. Vacca
  • Publication number: 20090005373
    Abstract: The invention relates to substituted sulfonamido-macrocycles according to the general formula (I): in which R1, R2, R4, R5, A, B, C, L, X, Y, Z, n, and m are as defined in the claims, and salts, N-oxides, or solvates thereof, to pharmaceutical compositions comprising said substituted sulfonamido-macrocycles, to methods of preparing said substituted sulfonamido-macrocycles as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.
    Type: Application
    Filed: June 20, 2007
    Publication date: January 1, 2009
    Inventors: Ingo Hartung, Hans Briem, Georg Kettschau, Karl-Heinz Thierauch, Ulrich Lucking, Ulf Bomer, Martina Schafer, Stuart Ince
  • Patent number: 7470469
    Abstract: A medical device comprising a substrate having a plasma polymerized functionality bonded to at least a portion of the substrate. A superoxide dismutase mimic agent having a complimentary functional group to the plasma polymerized functionality is bonded to the portion of the substrate by bonding to the plasma polymerized functionality. The functionalities can be carboxylate, amine, or sulfate groups and/or polyethylene glycol and can optionally include crosslinking groups.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: December 30, 2008
    Assignee: Advanced Cardiovascular Systems Inc.
    Inventors: Eugene T. Michal, Murthy Simhambhatla, Charles D. Claude
  • Patent number: 7468434
    Abstract: This invention provides a method for treating an eye disease in a patient comprising: providing a photosensitive prodrug that releases upon exposure to light an active ingredient to treat the eye disease; administering the prodrug in a pharmaceutically accepted vehicle to the subject, and exposing the eye of the subject to an external light source to cause the prodrug to release the active ingredient. This invention also provides a composition for the treatment of glaucoma, comprising a compound containing a lithium ion-chelated in a crown ether- or aza-crown ether-containing chromene or diazene derivative and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 21, 2005
    Date of Patent: December 23, 2008
    Assignee: The University of Hong Kong
    Inventors: Paul Michel Georges Vanhoutte, Chi-Ming Che, Kwok-Fai So, Iona Hiu Tung Sham
  • Publication number: 20080311041
    Abstract: The invention provides chromoionophore compounds comprising a triazacryptand (TAC) K+ ionophore conjugated to at least a first chromophoric moiety (e.g., xanthylium dyes and derivatives thereof). In related embodiments, the chromoionophore compounds further comprise a second chromophoric moiety which is insensitive to potassium binding by the TAC ionophore, thus providing for dual wavelength detection and absolute determination of K+ concentration. The invention further provides methods and kits for the determination of K+ concentrations in biological systems, either in vitro or in vivo, using embodiments of inventive chromoionophores.
    Type: Application
    Filed: October 11, 2006
    Publication date: December 18, 2008
    Inventors: Alan Verkman, Prashant A. Padmawar
  • Publication number: 20080290034
    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: Application
    Filed: March 19, 2008
    Publication date: November 27, 2008
    Inventors: Jeffery A. Whiteford, William Freeman, Joshua W. Kriesel
  • Publication number: 20080262055
    Abstract: There is provided a series of heterocyclic-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, n and X as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Application
    Filed: April 8, 2008
    Publication date: October 23, 2008
    Inventors: Shuhao Shi, Samuel Gerritz, Shirong Zhu
  • Patent number: 7332149
    Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.
    Type: Grant
    Filed: June 21, 2000
    Date of Patent: February 19, 2008
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Milind Rajopadhye, John A. Barrett, Alan P. Carpenter, Jr., Edward H. Cheesman, Thomas D. Harris
  • Patent number: 7321045
    Abstract: The present invention describes novel compounds of the formula: (Q)d-Ln-Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention also provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention also provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.
    Type: Grant
    Filed: February 2, 2004
    Date of Patent: January 22, 2008
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Milind Rajopadhye, Thomas D. Harris, Edward H. Cheesman
  • Patent number: 7312225
    Abstract: Macrocyclic pyrimidine derivatives of general formula I in which R1 to R5, X, Y, A, B, m and n have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinase, their processes for production as well as their use as medications for treating various diseases are described.
    Type: Grant
    Filed: August 20, 2003
    Date of Patent: December 25, 2007
    Assignee: Bayer Schering Pharma AG
    Inventors: Ulrich Luecking, Gerhard Siemeister, Martina Schaefer, Hans Briem
  • Patent number: 7311970
    Abstract: A medical device comprising a substrate having a plasma polymerized functionality bonded to at least a portion of the substrate. A superoxide dismutase mimic agent having a complimentary functional group to the plasma polymerized functionality is bonded to the portion of the substrate by bonding to the plasma polymerized functionality.
    Type: Grant
    Filed: September 17, 2004
    Date of Patent: December 25, 2007
    Assignee: Abbott Cardiovascular Systems Inc.
    Inventors: Eugene T. Michal, Murthy Simhambhatla, Charles D. Claude
  • Patent number: 7309567
    Abstract: The invention relates to a process for reducing the fluorescence quenching caused by the measuring medium, in a fluorescence assay for an analyte using at least one fluorescent label, characterized in that a fluorescent conjugate comprising an oligonucleotide bonded to a rare-earth metal cryptate is introduced into the measuring medium.
    Type: Grant
    Filed: March 14, 2000
    Date of Patent: December 18, 2007
    Assignee: CIS Bio International
    Inventors: Gerard Mathis, Herve Bazin, Eric Trinquet
  • Patent number: 7301020
    Abstract: Macrolide analogs and methods for identifying macrolide analogs capable of unregulated inhibition of actin filament dynamics are provided. A method according to the invention includes the steps of: (a) contacting F-actin with a candidate compound; and (b) assaying the candidate compound's ability to sever the F-actin and cap resulting F-actin (+)-ends. The candidate compound is identified as a macrolide analog where said candidate compound displays an ability to sever F-actin and, following severing, the resulting F-actin (+)-end is capped by the candidate compound thusly preventing subsequent G-actin incorporation. Severing and capping activities are unregulated; i.e., independent of at least physiologically-meaningful concentrations of phosphatidyl inositol and calcium.
    Type: Grant
    Filed: June 16, 2004
    Date of Patent: November 27, 2007
    Assignee: Wisconsin Alumni Research Foundation
    Inventor: Gerard Marriott
  • Patent number: 7214538
    Abstract: The present invention relates to a novel device and method for the detection of lithium ions in a biological fluid. In a preferred embodiment, the present invention provides a novel compound and a optical sensor which incorporates said compound for the detection of lithium ions. Additionally, the present invention provides a method of detecting lithium ions which comprises placing the novel optical sensor into communication with a biological fluid. Once the novel compound of the present invention encounters a lithium ion(s), a fluorescence is generated, the intensity of which is measured and allows for the determination of lithium ion concentration. The present invention provides a medical professional with the ability to selectively determine lithium ion concentration in a biological fluid thereby facilitating the treatment of various diseases, such as manic-depressive illness.
    Type: Grant
    Filed: February 11, 2004
    Date of Patent: May 8, 2007
    Assignees: Worcester Polytechnic Institute, Bayer Health Care, LLC.
    Inventors: John S. Benco, Hubert A. Nienaber, W. Grant McGimpsey
  • Patent number: 7091338
    Abstract: A purification method is disclosed for a predetermined water-insoluble extractant present in a liquid phase composition that additionally contains one or more additional extractants, synthesis reaction starting materials, and reaction byproducts dissolved as solutes in an organic diluent. An ion-containing compound is admixed with the composition to form an extractant/ion complex in the organic diluent phase that has an affinity for a new phase that is greater than the affinity for the first-named phase. The predetermined extractant/ion complex is separated from the diluent by using the new phase affinity, and the extractant/ion complex is preferably although not necessarily recovered. The extractant/ion complex is separated into extractant and ion. The extractant is recovered. Exemplary extractants include polyethers, crown ethers, crown thioethers, calixarenes, polyamines, cryptands, porphyrins and the like.
    Type: Grant
    Filed: October 31, 2002
    Date of Patent: August 15, 2006
    Assignee: PG Research Foundation
    Inventors: Andrew H. Bond, Richard E. Barrans, Jr., E. Philip Horwitz
  • Patent number: 7087384
    Abstract: The invention relates to a process for reducing the fluorescence quenching caused by the measuring medium in a fluorescence assay, by introducing into said medium of rare earth metal cryptates which are not very sensitive to this fluorescence quenching, said rare earth metal cryptates comprising at least one pyridine radical which is substituted one or more times or unsubstituted. The invention also relates to novel rare earth metal cryptates which are not very sensitive to the fluorescence quenching caused by the measuring medium.
    Type: Grant
    Filed: June 12, 2001
    Date of Patent: August 8, 2006
    Assignee: CIS bio international
    Inventors: Herve Autiero, Herve Bazin, Gerard Mathis
  • Patent number: 7014981
    Abstract: The invention discloses new benzoindole styryl compounds and its use for a high-density optical recording medium. The invention uses the dyes of the new benzoindole styryl compounds to form the recording layer of high-density recording media. The new benzoindole styryl compounds are easy to prepare and purify, so they are cheaper when comparing to the compounds generally used in high-density optical recording media. The benzoindole styryl compounds has a maximum absorption for the light wavelength in the range of 500 nanometers to 700 nanometers. The benzoindole styryl compounds also have high sensitivity and chemical stability for light and heat. Using the new benzoindole styryl compounds to form a high-density optical recording medium can match up with the short-wavelength laser beam for high-density optical recording media and have the advantage of a stable quality.
    Type: Grant
    Filed: September 13, 2002
    Date of Patent: March 21, 2006
    Assignee: Industrial Technology Research Institute
    Inventors: Shin-Shin Wang, Wen-Yih Liao, Chii-Chang Lai, Chien-Liang Huang, Hui-Ping Tsai, Chuen-Fuw Yan, Jong-Lieh Yang, Tzuan-Ren Jeng, Ming-Chia Lee