Plural Nitrogens In The Hetero Ring Patents (Class 540/469)
  • Patent number: 9328122
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel 7-substituted fangchinoline derivatives of formula (I) and a pharmaceutically acceptable adduct, complex and salt thereof, to a process for the preparation of these compounds, pharmaceutical compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Grant
    Filed: January 21, 2013
    Date of Patent: May 3, 2016
    Assignee: HANGZHOU BENSHENG PHARMACEUTICALS CO., LTD.
    Inventors: Frank Rong, Rongzhen Xu, Hongxi Lai, Fuwen Xie
  • Patent number: 9133207
    Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel 5-substituted tetrandrine derivatives of formula (I) and a pharmaceutically acceptable adduct, complex and salt thereof, to a process for the preparation of these compounds, pharmaceutical compositions containing such compounds and their use in preparing antineoplastic medicaments.
    Type: Grant
    Filed: August 20, 2012
    Date of Patent: September 15, 2015
    Assignee: Hangzhou Bensheng Pharmaceutical Co., Ltd.
    Inventors: Rongzhen Xu, Frank Rong, Fuwen Xie, Hongxi Lai
  • Patent number: 9085548
    Abstract: A pseudorotaxane, a rotaxane and a catenane are provided. The pseudorotaxane includes at least a macrocyclic host molecule, a guest molecule, and a metal ion. The host molecule contains at least a binding unit and an aromatic linking spacer. The guest molecule has at least a recognition unit. The metal ion is used to template the threading of the guest molecule through the macrocycle host molecule by coordinating to a binding pocket formed from the binding unit of the macrocycle and the recognition moiety of the guest molecule. Rotaxanes or catenanes can be synthesized from the pseudorotaxane complexes, with or without the metal template ion in their molecular structures.
    Type: Grant
    Filed: October 28, 2014
    Date of Patent: July 21, 2015
    Assignee: NATIONAL TAIWAN UNIVERSITY
    Inventors: Sheng-Hsien Chiu, You-Han Lin
  • Patent number: 9034861
    Abstract: The invention pertains to compound of Formula (I) wherein X, Y, Z, R1, R2, R3, R4, A and A? are as described hereinabove. Formula (I) and (II) compounds can be used in pharmaceutical compositions, useful for the treatment of diseases.
    Type: Grant
    Filed: October 13, 2010
    Date of Patent: May 19, 2015
    Assignee: Allomek Therapeutics LLC
    Inventors: Uday R. Khire, Mahendra Devichand Chordia
  • Publication number: 20150114261
    Abstract: An adhesive material produced by contacting a catechol with an amine may be stable under heated conditions and produce minimal outgassing under vacuum. The catechol may be an un-substituted catechol or a substituted catechol, such as hydroxychavicol. In some examples, the catechol may be derived from botanical sources. The amine may be a diamine, such as phenylene diamine. The adhesive polymer may form dendritic structures or macrocyclic structures. A joined article may be fabricated from two materials by applying the adhesive to a prepared surface of at least one of the materials, and the two materials may be placed together with the adhesive between them. The adhesive in the joined article may be cured at ambient temperature or under heating conditions.
    Type: Application
    Filed: October 31, 2014
    Publication date: April 30, 2015
    Inventor: Arockiadoss THEVASAHAYAM
  • Publication number: 20150111962
    Abstract: Macrocycle containing carbamate compounds that inhibit HIV proteolytic enzymes and processes for preparing them are described. Compositions and methods for treating a patient infected with HIV are described.
    Type: Application
    Filed: October 21, 2014
    Publication date: April 23, 2015
    Inventor: Arun K. Ghosh
  • Patent number: 8987243
    Abstract: The present invention relates to certain salts of a 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26triaza-tetra-cyclo[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 maleate salt of this compound. The invention also relates to pharmaceutical compositions containing this salt and methods of use of the salt in the treatment of certain medical conditions.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: March 24, 2015
    Assignee: CTI Biopharma Corp.
    Inventors: Brian Dymock, Cheng H. Lee, Anthony D. William
  • Patent number: 8987440
    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: Grant
    Filed: December 15, 2009
    Date of Patent: March 24, 2015
    Assignee: Teijin Limited
    Inventors: Shinichiro Shoji, Hirotaka Suzuki
  • Patent number: 8980873
    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: Grant
    Filed: December 9, 2009
    Date of Patent: March 17, 2015
    Assignee: CTI Biopharma Corp.
    Inventors: Brian Dymock, Cheng H. Lee, Anthony D. William
  • Publication number: 20150068602
    Abstract: A polyester film including a cyclic carbodiimide compound represented by the following Formula (O-1) has good film thickness uniformity without increase in viscosity. R1 and R5 represent an alkyl group, an aryl group, or an alkoxy group; R2 to R4 and R6 to R8 represent a hydrogen atom, an alkyl group, an aryl group, or an alkoxy group; X1 and X2 represent a single bond, —O—, —CO—, —S—, —SO2—, —NH—, or —CH2—; and L1 represents a divalent linking group.
    Type: Application
    Filed: November 12, 2014
    Publication date: March 12, 2015
    Applicant: FUJIFILM CORPORATION
    Inventors: Seiya SAKURAI, Makoto FUKUDA
  • Publication number: 20150051393
    Abstract: A pseudorotaxane, a rotaxane and a catenane are provided. The pseudorotaxane includes at least a macrocyclic host molecule, a guest molecule, and a metal ion. The host molecule contains at least a binding unit and an aromatic linking spacer. The guest molecule has at least a recognition unit. The metal ion is used to template the threading of the guest molecule through the macrocycle host molecule by coordinating to a binding pocket formed from the binding unit of the macrocycle and the recognition moiety of the guest molecule. Rotaxanes or catenanes can be synthesized from the pseudorotaxane complexes, with or without the metal template ion in their molecular structures.
    Type: Application
    Filed: October 28, 2014
    Publication date: February 19, 2015
    Inventors: Sheng-Hsien CHIU, You-Han LIN
  • Patent number: 8940720
    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: Grant
    Filed: February 10, 2011
    Date of Patent: January 27, 2015
    Assignee: Bristol-Myers Squibb Company
    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: 20150025066
    Abstract: Compounds of the formula I in which A, L1, L2, X and Y have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis.
    Type: Application
    Filed: December 18, 2012
    Publication date: January 22, 2015
    Applicant: Merck Patent GmbH
    Inventors: Henry Yu, Lizbeth Celeste Deselm
  • Patent number: 8906929
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Grant
    Filed: August 5, 2013
    Date of Patent: December 9, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: B. Narasimhulu Naidu, Manoj Patel, Stanley D'Andrea, Zhizhen Barbara Zheng, Timothy P. Connolly, David R. Langley, Kevin Peese, Zhongyu Wang, Michael A. Walker, John F. Kadow
  • Publication number: 20140350242
    Abstract: A pseudorotaxane, a rotaxane and a catenane are provided. The pseudorotaxane includes at least a macrocyclic host molecule, a guest molecule, and a metal ion. The host molecule contains at least a binding unit and an aromatic linking spacer. The guest molecule has at least a recognition unit. The metal ion is used to template the threading of the guest molecule through the macrocycle host molecule by coordinating to a binding pocket formed from the binding unit of the macrocycle and the recognition moiety of the guest molecule. Rotaxanes or catenanes can be synthesized from the pseudorotaxane complexes, with or without the metal template ion in their molecular structures.
    Type: Application
    Filed: May 24, 2013
    Publication date: November 27, 2014
    Inventors: Sheng-Hsien CHIU, You-Han LIN
  • Publication number: 20140309265
    Abstract: The invention relates generally to macrocyclic compounds and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of inhibitors of apoptosis (IAPs) and/or are useful in the treatment of medical conditions, such as cancer.
    Type: Application
    Filed: November 9, 2012
    Publication date: October 16, 2014
    Inventors: Benjamin Adam Seigal, Nicholas Terrett, Percy H. Carter, Robert M. Borzilleri, Yong Zhang, Michael M. Miller
  • Publication number: 20140303159
    Abstract: The present invention relates to macrocylic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of FLT3 (FMS-Related Tyrosine kinase 3). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine, in particular for the treatment of cell proliferative disorders, such as cancer.
    Type: Application
    Filed: September 28, 2012
    Publication date: October 9, 2014
    Inventors: Petra Marcella Francoise Blom, Jan Marie Cyriel Jozef Hoflack
  • Publication number: 20140286927
    Abstract: A engineered composition and method of delivery of said composition providing effective therapy for the treatment of ulcerative colitis, and Crohn's disease.
    Type: Application
    Filed: June 19, 2012
    Publication date: September 25, 2014
    Inventor: Peter Edward Smith
  • Publication number: 20140256714
    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-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: May 22, 2014
    Publication date: September 11, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Eddy Jean Edgard FREYNE, Marc Willems, Peter Ten Holte, Alexandra Papanikos, Werner Constant Johan Embrechts, Pierre Henri Storck, Virginie Sophie Poncelet
  • 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: 20140234758
    Abstract: Disclosed are a photosensitive resin composition for a color filter and a color filter using the same. The photosensitive resin composition for a color filter includes (A) a dye represented by the following Chemical Formula 1, (B) an alkali soluble resin, (C) a photopolymerizable monomer, (D) a photopolymerization initiator, and (E) a solvent.
    Type: Application
    Filed: May 15, 2012
    Publication date: August 21, 2014
    Applicant: Cheil Industries Inc.
    Inventors: Jae-Hyun Kim, Kyung-Soo Moon, Myoung-Youp Shin, Dong-Hoon Won, Seung-Hyun Kim, Atsushi Endo, Hwan-Sung Cheon, Gyu-Seok Han
  • Publication number: 20140206683
    Abstract: The present invention relates to novel macrocylic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 (Leucine-Rich Repeat Kinase 2). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine or diagnostic agent, in particular for the treatment and/or diagnosis of diseases characterized by LRRK2 kinase activity such as neurological disorders including Parkinson's disease and Alzheimer's disease.
    Type: Application
    Filed: September 28, 2012
    Publication date: July 24, 2014
    Inventors: Jan Hoflack, Petra Blom
  • Publication number: 20140200319
    Abstract: This disclosure relates generally to potassium ion sensors and monomers derived from such sensors. The disclosure also provides for polymers (e.g., random copolymers, nanoparticles, polymer thin films, and sensors) having polymerized monomeric potassium ion sensors as described herein. These compounds and polymers are useful for measuring intracellular and extracellular potassium ion concentrations.
    Type: Application
    Filed: February 13, 2012
    Publication date: July 17, 2014
    Applicant: Arizona Board of Regents, a body corporate of the State of Arizona acting for and on behalf of Arizo
    Inventors: Yanqing Tian, Deirdre Meldrum, Xianfeng Zhou, Fengyu Su, Roger H. Johnson, Cody Youngbull
  • Publication number: 20140091264
    Abstract: The present invention relates to organic electronic devices, in particular organic electroluminescent devices, which comprise organic cyclophanes, in particular as matrix materials for fluorescent or phosphorescent emitter compounds or as charge-transport materials, in particular electron-transport materials, and to diverse organic cyclophanes themselves.
    Type: Application
    Filed: May 16, 2012
    Publication date: April 3, 2014
    Applicant: Merck Patent GmbH
    Inventors: Junyou Pan, Niels Schulte
  • Publication number: 20140051692
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Application
    Filed: August 5, 2013
    Publication date: February 20, 2014
    Inventors: B. Narasimhulu Naidu, Manoj Patel, Stanley D'Andrea, Zhizhen Barbara Zheng, Timothy P. Connolly, David R. Langley, Kevin Peese, Zhongyu Wang, Michael A. Walker, John F. Kadow
  • Publication number: 20140051851
    Abstract: The present invention claims complexing [18F] fluoride anion with disubstituted-cryptand to form novel [18F] fluoride disubstituted-cryptate complexes suitable for performing radio-labeling reactions to generate [18F] fluorinated species.
    Type: Application
    Filed: August 19, 2012
    Publication date: February 20, 2014
    Inventors: YOUSRY M.A. NAGUIB, Ashraf Naguib, Ahmed Naguib
  • Publication number: 20140046053
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: October 10, 2013
    Publication date: February 13, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
  • Patent number: 8637523
    Abstract: Compounds of the formula (I) are provided, including pharmaceutically acceptable salts thereof: which modulate ?-amyloid peptide (?-AP) production, and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Grant
    Filed: July 12, 2011
    Date of Patent: January 28, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Lorin A. Thompson, III, Yong-Jin Wu, Yunhui Zhang
  • Publication number: 20130344607
    Abstract: The present invention relates to ?-conjugated fluoroionophores, methods for their preparation, and their use and a method for determining an alkali ion. Fluoroionophoric compounds of the general formula I are described Ionophore-?-Linker-Fluorophore??(I) wherein the Ionophore is an anilino containing crown ether or cryptand with one or more anilino donor moieties as electron donors, forming a stable complex with an alkali metal ion the ?-Linker is an aromatic or heteroaromatic conjugative linking moiety, and the Fluorophore is an electron acceptor moiety. Variation of the ionophoric unit offers a broad spectrum of detectable K+ and Na+-concentrations, ranging from high concentration around 800 mM down to very low concentrations around 3 mM.
    Type: Application
    Filed: March 9, 2012
    Publication date: December 26, 2013
    Applicant: UNIVERSITAET POTSDAM
    Inventors: Sandra Ast, Hans-Juergen Holdt
  • Publication number: 20130324715
    Abstract: The present invention provides a novel method for the preparation of 18F-fluoride (18F) for use in radiofluorination reactions. The method of the invention finds use especially in the preparation of 18F-labelled positron emission tomography (PET) tracers. The method of the invention is particularly advantageous where bulk solutions are prepared and stored in prefilled vials rather than being freshly prepared on the day of synthesis. Also provided by the present invention is a radiofluorination reaction which comprises the method of the invention, as well as a cassette for use in carrying out the method of the invention and/or the radiofluorination method of the invention on an automated radiosynthesis apparatus.
    Type: Application
    Filed: December 21, 2011
    Publication date: December 5, 2013
    Applicant: GE HEALTHCARE LIMITED
    Inventors: Torild Wickstrom, Anders Svadberg, Ole Kristian Hjelstuen, Dag M. Evje, Liane Ochsenfeld
  • Patent number: 8586536
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: November 19, 2013
    Assignee: Theravance, Inc.
    Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
  • Patent number: 8518715
    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, 111In 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: Grant
    Filed: May 21, 2012
    Date of Patent: August 27, 2013
    Assignee: Nordion (Canada) Inc.
    Inventors: Zoltan Kovacs, Garry E. Kiefer, Corinne Bensimon, A. Dean Sherry, Gyula Tircso, Cara Ferreira
  • Publication number: 20130203776
    Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.
    Type: Application
    Filed: May 13, 2011
    Publication date: August 8, 2013
    Inventors: Steven Wade Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, HongWoon Yang, Qian Zhao
  • Publication number: 20130150378
    Abstract: Provided herein are salt forms of macrocyclic protein kinase inhibitors, pharmaceutical compositions containing the same, methods of making and using these compounds and compositions to treat proliferative disease mediated by kinase activity.
    Type: Application
    Filed: February 4, 2011
    Publication date: June 13, 2013
    Inventors: Robert K. Mansfield, Tracy Lawhon, Brian Dymock
  • Publication number: 20130096300
    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: September 12, 2012
    Publication date: April 18, 2013
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Kyle GEE, Vladimir MARTIN
  • Publication number: 20130095066
    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 5, 2012
    Publication date: April 18, 2013
    Inventors: Tao Wang, Li-Qiang Sun, Paul Michael Scola
  • Patent number: 8415338
    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 tumors and cancers as well as other disorders or conditions related to or associated with kinases.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: April 9, 2013
    Assignee: Cell Therapeutics, Inc.
    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: 20130079510
    Abstract: Disclosed is a cyclic carbodiimide compound useful as an end-capping agent for polymer compounds. The cyclic carbodiimide compound is represented by the following formula (i): wherein X is a specific divalent group or tetravalent group, q is 0 when X is a divalent group, while q is 1 when X is a tetravalent group, and Ar1 to Ar4 are selected from aromatic groups each independently optionally substituted with a group that serves as X.
    Type: Application
    Filed: June 6, 2011
    Publication date: March 28, 2013
    Applicant: TEIJIN LIMITED
    Inventor: Shinichiro Shoji
  • Publication number: 20130035341
    Abstract: Compound having formula I and pharmaceutically acceptable salts or solvates thereof, their pharmaceutical formulations and use as HIV inhibitors.
    Type: Application
    Filed: April 1, 2011
    Publication date: February 7, 2013
    Applicant: Janssen R&D Ireland
    Inventors: Johannes Wilhelmus J. Thuring, Jean-Francois Bonfanti
  • Publication number: 20130028872
    Abstract: Described are methods for inducing differentiation of a human embryonic stem cell or a population of human embryonic stem cells toward a cell or population of cells characteristic of the definitive endoderm, the method comprising incubating the cell or population of cells with a GSK-3 inhibitor. Also described are methods for inducing differentiation of a cell or population of cells, characteristic of the definitive endoderm, towards a hepatocyte-like cell or a population of hepatocyte-like cells, and methods for inducing differentiation of a human embryonic stem cell or a population of human embryonic stem cells toward a hepatocyte-like cell or a population of hepatocyte-like cells. Further described are cells obtained by the methods and uses thereof in therapy and toxicity screening.
    Type: Application
    Filed: November 26, 2010
    Publication date: January 31, 2013
    Inventors: Heather K. Bone, David Tosh, Melanie J. Welham
  • Patent number: 8263586
    Abstract: The present invention is directed to oxo bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: May 14, 2008
    Date of Patent: September 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, David B. Whitman
  • Publication number: 20120196876
    Abstract: The present invention relates to certain salts of a 9E-15-(2-pyrrolidin-1-yl-ethoxy)-7,12,25-trioxa-19,21,24-triaza-tetracyclo[18.3.1.1(2,5). 1(14,18)]hexacosa-1(24),2,4,9, 14,16,18(26),20,22-nonaene (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: July 14, 2010
    Publication date: August 2, 2012
    Applicant: S*Bio Pte Ltd.
    Inventors: Brian Dymock, Cheng Hsia Angeline Lee, Anthony Deodaunia William
  • Publication number: 20120196855
    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: April 4, 2012
    Publication date: August 2, 2012
    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: 20120184565
    Abstract: Compounds of the formula (I) are provided, including pharmaceutically acceptable salts thereof: which modulate ?-amyloid peptide (?-AP) production, and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Application
    Filed: July 12, 2011
    Publication date: July 19, 2012
    Inventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Lorin A. Thompson, III, Yong-Jin Wu, Yunhui Zhang
  • Publication number: 20120178774
    Abstract: The present invention provides a compound selected from the group consisting of: where n, m, X1, X2, X3, X4, R1, R2, R3, R11, R12, Y1, Y2, Y3, Y4, and Y5 are those defined herein. Some aspects of the invention also provides methods for using these compounds and compositions comprising the same.
    Type: Application
    Filed: September 23, 2010
    Publication date: July 12, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATE
    Inventors: Hang Yin, Linda R. Watkins
  • Publication number: 20120172367
    Abstract: Compound having formula (I), wherein —W is NH—, —N(CH3)— or piperazine, —X is a bond, —C(?O)— or S(?O)2—, —Y is C3-7alkylene, and —Z is NH—C(?O)— or —O—, and pharmaceutically acceptable salts thereof, their pharmaceutical formulations and use as HIV inhibitors.
    Type: Application
    Filed: October 13, 2010
    Publication date: July 5, 2012
    Applicant: ELANCO ANIMAL HEALTH IRELAND LIMITED
    Inventors: Johannes Wilhelmus J Thuring, Jean-Francois Bonfanti, Jerome Michel Claude Fortin
  • Publication number: 20120157383
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: December 14, 2011
    Publication date: June 21, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Roland GENDRON, Melissa FLEURY, Adam D. HUGHES
  • Publication number: 20120157658
    Abstract: This invention relates to methods, compositions, and apparatuses for producing macrocyclic compounds. First, one or more reactants are provided in a reaction medium, which are capable of forming the macrocyclic compound through a desired reaction pathway that includes at least cyclization, and which are further capable of forming undesired oligomers through a undesired reaction pathway that includes undesirable oligomerization. Oligomerization of such reactions in the reaction medium is modulated to reduce formation of undesired oligomers and/or to reduce separation of the undesired oligomers from the reaction medium, relative to a corresponding unmodulated oligomerization reaction, thereby maximizing yields of the macrocyclic compound. The macrocyclic compound so formed is then recovered from the reaction medium. Preferably, the macrocyclic compound spontaneously separates from the reaction medium via phase separation.
    Type: Application
    Filed: November 8, 2011
    Publication date: June 21, 2012
    Inventors: Thomas E. Johnson, Billy T. Fowler
  • Patent number: 8198101
    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: Grant
    Filed: March 6, 2007
    Date of Patent: June 12, 2012
    Assignee: Nordion (Canada) Inc.
    Inventors: Zoltan Kovacs, Garry E. Kiefer, Corinne Bensimon, A. Dean Sherry, Gyula Tircso
  • Publication number: 20120142647
    Abstract: The present invention includes compositions that are useful in the treatment of breathing control diseases or disorders in a subject in need thereof. The present invention also includes a method of treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention. The present invention further includes a method of preventing destabilization or stabilizing breathing rhythm in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention.
    Type: Application
    Filed: November 29, 2011
    Publication date: June 7, 2012
    Inventors: Scott L. Dax, Richard Woodward, Sean Peng