Plural Nitrogens In The Hetero Ring Patents (Class 540/469)
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Publication number: 20120136037Abstract: The present application describes deuterium-enriched ruboxistaurin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 3, 2008Publication date: May 31, 2012Applicant: Protia, LLCInventor: Anthony W. Czarnik
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Patent number: 8182695Abstract: 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: GrantFiled: March 19, 2008Date of Patent: May 22, 2012Inventors: Jeffery A. Whiteford, William Freeman, Joshua W. Kriesel
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Publication number: 20120093767Abstract: 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: ApplicationFiled: April 14, 2011Publication date: April 19, 2012Inventors: Tao Wang, Zhiwei Yin, Zhongxing Zhang, Annapurna Pendri, Guo Li, Samuel Gerritz, Weixu Zhai, Paul Michael Scola, Li-Qiang Sun, Eric Mull
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Patent number: 8129365Abstract: 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: GrantFiled: October 11, 2006Date of Patent: March 6, 2012Assignee: The Regents of the University of CaliforniaInventors: Alan Verkman, Prashant A. Padmawar
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Publication number: 20120041190Abstract: 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: ApplicationFiled: February 10, 2011Publication date: February 16, 2012Inventors: 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
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Publication number: 20120021897Abstract: 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: ApplicationFiled: February 19, 2010Publication date: January 26, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Masatoshi Iwata, Tadafumi Matsunaga, Nobuyoshi Koshino, Hideyuki Higashimura
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Publication number: 20110294831Abstract: 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: ApplicationFiled: December 9, 2009Publication date: December 1, 2011Applicant: S*BIO Pte Ltd.Inventors: Brian Dymock, Cheng H. Lee, Anthony D. William
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Publication number: 20110294801Abstract: 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: ApplicationFiled: September 3, 2009Publication date: December 1, 2011Applicant: MERCK PATENT GMBHInventors: Henry Yu, Lizbeth Celeste De Selm, Xuliang Jiang, Benny C. Askew, Jr., Srinivasa R. Karra, Andreas Goutopoulos
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Patent number: 8058266Abstract: 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: GrantFiled: July 13, 2007Date of Patent: November 15, 2011Assignee: The University of Georgia Research Foundation, IncInventors: Dennis Michael Marcus, Chung Kwang Chu
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Publication number: 20110251384Abstract: 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: ApplicationFiled: December 15, 2009Publication date: October 13, 2011Applicant: TEIJIN LIMITEDInventors: Shinichiro Shoji, Hirotaka Suzuki
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Publication number: 20110251215Abstract: 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: ApplicationFiled: January 22, 2010Publication date: October 13, 2011Applicant: INCYTE CORPORATIONInventors: Andrew Paul Combs, Richard B. Sparks, Eddy Wai Tsun Yue, Hao Feng, Michael Jason Bower, Wenyu Zhu
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Patent number: 7947671Abstract: Ecteinascidin compounds with a quinone ring for ring E are active as anti-cancer agents. Related processes and compounds are provided.Type: GrantFiled: April 12, 2010Date of Patent: May 24, 2011Assignee: Pharma Mar, S.A.Inventors: Valentin Martinez Barrasa, Pilar Gallego, Carmen Cuevas, Simon Munt, Ignacio Manzanares, Roberto Menchaca, Natividad Rodriguez, Alberto Rodriguez
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Publication number: 20110071179Abstract: 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: ApplicationFiled: September 17, 2010Publication date: March 24, 2011Inventors: Alam Jahangir, Stephen M. Lynch, Michael Soth, Hanbiao Yang
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Publication number: 20110065914Abstract: 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: ApplicationFiled: August 28, 2008Publication date: March 17, 2011Inventors: BENGT Langstrom, Johan Ulin, Farhad Karimi
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Patent number: 7897787Abstract: 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: GrantFiled: September 13, 2006Date of Patent: March 1, 2011Assignee: The University of TokyoInventors: Takuya Matsumoto, Takuji Shoda, Yasuteru Urano, Tetsuo Nagano
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Publication number: 20110015238Abstract: 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: ApplicationFiled: September 24, 2010Publication date: January 20, 2011Applicant: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Akihiro Kinoshita, Yoshihisa Kamanaka, Hidekazu Matsuya
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Publication number: 20100330584Abstract: 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: ApplicationFiled: June 5, 2008Publication date: December 30, 2010Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Kyle Gee, Vladimir Martin
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Patent number: 7767659Abstract: Ecteinascidin compounds with a quinone ring for ring E are active as anti-cancer agents. Related processes and compounds are provided.Type: GrantFiled: February 4, 2003Date of Patent: August 3, 2010Assignee: Pharma Mar, S.A.Inventors: Valentin Martinez Barrasa, Pilar Gallego, Carmen Cuevas, Simon Munt, Ignacio Manzanares, Roberto Menchaca, Natividad Rodriguez, Alberto Rodriguez
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Publication number: 20100190804Abstract: 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: ApplicationFiled: January 22, 2010Publication date: July 29, 2010Applicant: INCYTE CORPORATIONInventors: Andrew Paul Combs, Richard B. Sparks, Eddy Wai Tsun Yue, Hao Feng, Michael Jason Bower, Wenyu Zhu
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Publication number: 20100173913Abstract: 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 morType: ApplicationFiled: March 15, 2010Publication date: July 8, 2010Applicant: 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
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Publication number: 20100160310Abstract: 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 independenType: ApplicationFiled: December 8, 2005Publication date: June 24, 2010Inventors: Eddy Jean Edgard Freyne, Marc Willems, Werner Constant Johan Embrechts, Kristof Van Emelen, Sven Franciscus Anna Van Brandt, Frederik Jan Rita Rombouts
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Publication number: 20100152174Abstract: 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 hydrType: ApplicationFiled: December 8, 2005Publication date: June 17, 2010Inventors: 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
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Publication number: 20100086482Abstract: 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: ApplicationFiled: December 28, 2007Publication date: April 8, 2010Applicant: Dendritic Nanotechnologies, Inc.Inventors: Donald A. Tomalia, Douglas R. Swanson, Baohua Huang, Veera Reddy Pulgam
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Publication number: 20100069424Abstract: 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-, preferabType: ApplicationFiled: November 24, 2009Publication date: March 18, 2010Inventors: Eddy Jean Edgard FREYNE, Peter Jacobus Johannes Antonius Buijnsters, Kristof Van Emelen, Werner Constant Johan Embrechts, Timothy Pietro Suren Perera
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Publication number: 20100029627Abstract: 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—C1-4alType: ApplicationFiled: July 12, 2007Publication date: February 4, 2010Inventors: Alexandra Papanikos, Freyne Eddy Jean Edgard, Peter Ten Holte, Marc Willems, Werner Constant Johan Embrechts, Laurence Anne Mevellec, Fierre-Henri Storck
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Patent number: 7625887Abstract: 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: GrantFiled: January 27, 2004Date of Patent: December 1, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Fumio Itoh, Shuji Hinuma, Naoyuki Kanzaki, Yuji Kawamata, Taisuke Tawaraishi, Yuji Ishichi, Mariko Hirohashi
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Publication number: 20090286770Abstract: 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: ApplicationFiled: December 7, 2005Publication date: November 19, 2009Inventors: D. Gary Gilliland, James Douglas Griffin, Jing Chen, Kenneth C. Anderson
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Publication number: 20090258886Abstract: 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: ApplicationFiled: November 15, 2006Publication date: October 15, 2009Applicant: 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
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Patent number: 7582280Abstract: 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: GrantFiled: July 8, 2008Date of Patent: September 1, 2009Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Helen Fan, Michael F. Tweedle, Rolf E. Swenson
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Publication number: 20090202521Abstract: 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: ApplicationFiled: March 6, 2007Publication date: August 13, 2009Applicant: MDS (Canada) Inc.Inventors: Zoltan Kovaks, Garry E. Kiefer, Corinne Bensimon, A. Dean Sherry, Gyula Tircso
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Publication number: 20090186830Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.Type: ApplicationFiled: June 3, 2008Publication date: July 23, 2009Inventors: Roger Aki Fujimoto, Philipp Krastel, Matthew J. LaMarche
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Publication number: 20090180985Abstract: 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: ApplicationFiled: December 18, 2008Publication date: July 16, 2009Inventors: DONG LIU, Yat Sun Or, Zhe Wang
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Publication number: 20090075999Abstract: 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: ApplicationFiled: November 15, 2006Publication date: March 19, 2009Applicant: 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
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Publication number: 20090075869Abstract: 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: ApplicationFiled: April 28, 2006Publication date: March 19, 2009Inventors: M. Katharine Holloway, Nigel J. Liverton, Steven W. Ludmerer, John A. McCauley, David Olsen, Michael T. Rudd, Joseph P. Vacca
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Publication number: 20090005373Abstract: 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: ApplicationFiled: June 20, 2007Publication date: January 1, 2009Inventors: Ingo Hartung, Hans Briem, Georg Kettschau, Karl-Heinz Thierauch, Ulrich Lucking, Ulf Bomer, Martina Schafer, Stuart Ince
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Patent number: 7470469Abstract: 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: GrantFiled: July 5, 2007Date of Patent: December 30, 2008Assignee: Advanced Cardiovascular Systems Inc.Inventors: Eugene T. Michal, Murthy Simhambhatla, Charles D. Claude
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Patent number: 7468434Abstract: 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: GrantFiled: December 21, 2005Date of Patent: December 23, 2008Assignee: The University of Hong KongInventors: Paul Michel Georges Vanhoutte, Chi-Ming Che, Kwok-Fai So, Iona Hiu Tung Sham
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Publication number: 20080311041Abstract: 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: ApplicationFiled: October 11, 2006Publication date: December 18, 2008Inventors: Alan Verkman, Prashant A. Padmawar
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Publication number: 20080290034Abstract: 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: ApplicationFiled: March 19, 2008Publication date: November 27, 2008Inventors: Jeffery A. Whiteford, William Freeman, Joshua W. Kriesel
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Publication number: 20080262055Abstract: 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: ApplicationFiled: April 8, 2008Publication date: October 23, 2008Inventors: Shuhao Shi, Samuel Gerritz, Shirong Zhu
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Patent number: 7332149Abstract: 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: GrantFiled: June 21, 2000Date of Patent: February 19, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Milind Rajopadhye, John A. Barrett, Alan P. Carpenter, Jr., Edward H. Cheesman, Thomas D. Harris
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Patent number: 7321045Abstract: 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: GrantFiled: February 2, 2004Date of Patent: January 22, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Milind Rajopadhye, Thomas D. Harris, Edward H. Cheesman
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Patent number: 7312225Abstract: 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: GrantFiled: August 20, 2003Date of Patent: December 25, 2007Assignee: Bayer Schering Pharma AGInventors: Ulrich Luecking, Gerhard Siemeister, Martina Schaefer, Hans Briem
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Patent number: 7311970Abstract: 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: GrantFiled: September 17, 2004Date of Patent: December 25, 2007Assignee: Abbott Cardiovascular Systems Inc.Inventors: Eugene T. Michal, Murthy Simhambhatla, Charles D. Claude
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Patent number: 7309567Abstract: 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: GrantFiled: March 14, 2000Date of Patent: December 18, 2007Assignee: CIS Bio InternationalInventors: Gerard Mathis, Herve Bazin, Eric Trinquet
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Patent number: 7301020Abstract: 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: GrantFiled: June 16, 2004Date of Patent: November 27, 2007Assignee: Wisconsin Alumni Research FoundationInventor: Gerard Marriott
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Patent number: 7214538Abstract: 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: GrantFiled: February 11, 2004Date of Patent: May 8, 2007Assignees: Worcester Polytechnic Institute, Bayer Health Care, LLC.Inventors: John S. Benco, Hubert A. Nienaber, W. Grant McGimpsey
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Patent number: 7091338Abstract: 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: GrantFiled: October 31, 2002Date of Patent: August 15, 2006Assignee: PG Research FoundationInventors: Andrew H. Bond, Richard E. Barrans, Jr., E. Philip Horwitz
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Patent number: 7087384Abstract: 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: GrantFiled: June 12, 2001Date of Patent: August 8, 2006Assignee: CIS bio internationalInventors: Herve Autiero, Herve Bazin, Gerard Mathis
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Patent number: 7014981Abstract: 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: GrantFiled: September 13, 2002Date of Patent: March 21, 2006Assignee: Industrial Technology Research InstituteInventors: 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