Plural Nitrogens In The Hetero Ring Patents (Class 540/460)
  • Patent number: 11072688
    Abstract: A method for preparation of (meth)acrylate esters of polysiloxanes. The method comprises contacting in the presence of zirconium acetylacetonate or hafnium acetylacetonate: (i) a polysiloxane having at least two hydroxyl groups, each of which is attached to a carbon atom, and (ii) a C1-C4 alkyl (meth)acrylate.
    Type: Grant
    Filed: November 9, 2017
    Date of Patent: July 27, 2021
    Assignee: Rohm and Haas Company
    Inventors: Muhunthan Sathiosatham, James H. Pawlow, Lan T. P. Hoang Nguyen
  • Patent number: 10926248
    Abstract: An especially robust compound and its derivative metal complexes that are approximately one hundred-fold superior in catalytic performance to the previously invented TAML analogs is provided having the formula: wherein Y1, Y2, Y3 and Y4 are oxidation resistant groups which are the same or different and which form 5- or 6-membered rings with a metal, M, when bound to D; at least one Y incorporates a group that is significantly more stable towards nucleophilic attack than the organic amides of TAML activators; D is a metal complexing donor atom, preferably N; each X is a position for addition of a labile Lewis acidic substituent such as (i) H, deuterium, (ii) Li, Na, K, alkali metals, (iii) alkaline earth metals, transition metals, rare earth metals, which may be bound to one or more than one D, (iv) or is unoccupied with the resulting negative charge being balanced by a nonbonded countercation; at least one Y may contain a site that is labile to acid dissociation, providing a mechanism for shortening co
    Type: Grant
    Filed: September 22, 2016
    Date of Patent: February 23, 2021
    Assignee: CARNEGIE MELLON UNIVERSITY
    Inventors: Terrence James Collins, Matthew Alan DeNardo, Genoa Rose Warner, Scott Wallace Gordon-Wylie, William Chadwick Ellis, Yogesh Somasundar
  • Patent number: 10399970
    Abstract: The invention relates to pyrridinobenzodiazepines (PDDs) comprising three fused 6-7- 6-membered rings and to benzopyrridodiazecines (BPDs) comprising three fused 6-8- 6-membered rings and, in particular, to PDD or BPD dimers linked together or PDD and BPD monomers linked to aromatic groups, and pharmaceutically acceptable salts thereof, which are useful as medicaments, such as anti-proliferative agents.
    Type: Grant
    Filed: June 9, 2016
    Date of Patent: September 3, 2019
    Assignee: Femtogenix Limited
    Inventors: David Edwin Thurston, Khondaker Mirazur Rahman, Paul Joseph Mark Jackson
  • Patent number: 10084141
    Abstract: Provided are an antiaromatic compound and an organic light-emitting device including the same. The antiaromatic compound is represented by Formula 1, where the substituents of Formula 1 are described herein. The organic light-emitting device light includes a first electrode, a second electrode, and an organic layer between the first electrode and the second electrode. The organic layer includes the antiaromatic compound represented by Formula 1.
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: September 25, 2018
    Assignees: Samsung Display Co., Ltd., Industry-Academic Cooperation Foundation Gyeongsang National University
    Inventors: Mikyung Kim, Yunhi Kim, Soonki Kwon, Boram Kim, Yongjin Yoon
  • Patent number: 9579404
    Abstract: The invention relates to compositions of DOTA derivative compounds, lanthanoid-DOTA derivative molecular complex, and lanthanoid-complex encapsulated solid lipid particles or capsules, and methods of making and using the compositions. The solid lipid particles or capsules contain micelle cores stabilized by a hyperbranched polymer shell based from a crosslinked DOTA derivative compound or crosslinked lanthanoid-DOTA derivative complex. These solid lipid particles or capsules can be used in various applications, such as contrast agents or drug delivery vehicles.
    Type: Grant
    Filed: September 22, 2014
    Date of Patent: February 28, 2017
    Assignee: New York University
    Inventor: Marc Anton Walters
  • Patent number: 9315511
    Abstract: Special C-functionalized cyclic bisaminal compounds having formula (I) or (II), their salts or solvates, methods for their preparation, their uses, and methods for preparing functional tetraazacycloalkane compounds implementing such cyclic bisaminal compounds.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: April 19, 2016
    Assignees: UNIVERSITE DE BRETAGNE OCCIDENTALE, CNRS—CENTRE NATIONAL DE LA RECHERCHE
    Inventors: Raphael Tripier, Nathalie Camus
  • Patent number: 9132163
    Abstract: The present invention relates to a method for the purification of Micafungin. Specifically, a method is provided in which a micafungin starting material containing a first micafungin salt is adsorbed to a solid support, the adsorbed micafungin is washed with an aqueous solution comprising a dissolved second salt, the second micafungin salt is eluted using a water miscible organic solvent.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: September 15, 2015
    Assignee: XELLIA PHARMACEUTICALS APS
    Inventors: Lene Aassveen, Eli Karin Dale, Espen Fridtjof Hansen, Kjersti Meldahl Eide
  • Patent number: 9108981
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts 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: October 30, 2014
    Date of Patent: August 18, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Patrick Y. S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Publication number: 20150147275
    Abstract: A water-soluble compound of the formula (I): (Formula (I)) wherein R9 and R10 are suitably hydrophilic substituents, which may be used to selectively bind to a target saccharide such as glucose and which exhibits a detectable spectroscopic response to such binding, thus enabling its use in the detection and correction of blood glucose concentrations in vivo.
    Type: Application
    Filed: April 26, 2013
    Publication date: May 28, 2015
    Inventors: Chenfeng Ke, Anthony P. Davis
  • Patent number: 9040562
    Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitroge
    Type: Grant
    Filed: May 23, 2014
    Date of Patent: May 26, 2015
    Assignees: Janssen R&D Ireland, Medivir AB
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist
  • Publication number: 20150141392
    Abstract: The disclosure provides for novel compounds which have proteasome inhibitory activity, pharmaceutical compositions made thereof, and methods of use thereof to treat various disorders, including cancer and nonmalignant tumors.
    Type: Application
    Filed: June 14, 2013
    Publication date: May 21, 2015
    Inventor: Michael C. Pirrung
  • Patent number: 9023808
    Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein the dashed line, X, R1, R2, R3, R4, R5, R6, and R7 have defined meanings; the preparation thereof; compositions containing compounds of formula (I), including bioavailable combinations with ritonavir; and the pharmaceutical uses thereof.
    Type: Grant
    Filed: January 16, 2008
    Date of Patent: May 5, 2015
    Assignees: Medivir AB, Janssen R&D Ireland
    Inventors: Kenneth Alan Simmen, Herman Agustinus De Kock, Carl Erik Daniel Jonsson, Karl Magnus Milsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Susana Ayesa Alverez, Bjorn Olaf Classon, Hans Kristian Wallberg
  • Publication number: 20150112058
    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: December 22, 2014
    Publication date: April 23, 2015
    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
  • Patent number: 9012441
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Grant
    Filed: January 9, 2014
    Date of Patent: April 21, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-Hung Chou, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • Patent number: 9006423
    Abstract: The invention provides a process of preparing 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Compound I and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: April 14, 2015
    Assignee: Achillion Pharmaceuticals Inc.
    Inventors: Avinash Phadke, Akihiro Hashimoto
  • Patent number: 8993607
    Abstract: The invention provides compounds of formula I, II, and III as defined herein, as well as salts thereof. The compounds may have activity as anti-proliferative agents.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: March 31, 2015
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Joseph E. Rice
  • Patent number: 8981082
    Abstract: The present invention relates to an improved process for preparing (2R,3aR,10Z,11aS,2aR,14aR)-cyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxylic acid, 2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydro-2-[[7-methoxy-8-methyl-2-[4-10(1-methylethyl)-2-thiazolyl]-4-quinolinyl]oxy]-5-methyl-4,14-dioxo-, ethyl ester. This compound is an intermediate in the overall synthesis route of the macrocyclic compound TMC 435. TMC 435 is an inhibitor of NS3/4A protease which plays an important role in the replication of the hepatitis C virus.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: March 17, 2015
    Assignee: Janssen Pharmaceuticals, Inc.
    Inventors: Andras Horvath, Stijn Wuyts, Dominique Paul Michel Depré, Wouter Louis J. Couck, Jozef Ludo Jan Cuypers, Syuzanna Harutyunyan, Gregory Fabien Sebastian Binot
  • Patent number: 8969373
    Abstract: A compound of general formula (I); A is O, S, CH, NH or NR?, when O links with Z3, Z1 is N or CRZ1, Z2 is CRZ2, when Z1 links with O, Z2 is CH, Z3 is C—Ar; Ra, Rb, Rc and Rd independently is H, OH, halogen or —Y1—Rm; A1 is NH or CH2; R1? is alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl; A2 is N, O or linking bond; R1 is hydrogen, or, R1 linking covalently with R3 forms C5-C9 saturated or unsaturated hydrocarbon chain substituted by O or N; R3 is alkyl, cycloalkyl, heterocycloalkyl, alkyl substituted by cycloalkyl etc; R4 is alkoxy-CO, alkyl-NHCO, (alkyl)2NCO, or formyl substituted by aryl, cycloalkyl, heterocycloalkyl.
    Type: Grant
    Filed: July 23, 2012
    Date of Patent: March 3, 2015
    Assignee: Shanghai Tangrun Pharmaceuticals Co., Ltd.
    Inventor: Suoming Zhang
  • Publication number: 20150057262
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts 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: October 30, 2014
    Publication date: February 26, 2015
    Inventors: Patrick Y.S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Patent number: 8962605
    Abstract: Disclosed is a novel family of macrocyclic compounds, coined calixurenes, which comprises linear and cyclic oligomers composed of alternating moieties of an aromatic unit and a ureatic unit, linked to one another via a bridging moiety. The disclosed calixurenes feature multiple heteroatom-containing groups, and can be designed so as to feature other functionalities, and can thus be used in a variety of applications. Further disclosed are processes of preparing the calixurenes, articles containing same and uses thereof.
    Type: Grant
    Filed: August 12, 2010
    Date of Patent: February 24, 2015
    Assignee: Technion Research & Development Foundation Limited
    Inventors: Ehud Keinan, Galit Parvari, Doron Pappo
  • Patent number: 8957203
    Abstract: Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: February 17, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Sheldon Hiebert, Ramkumar Rajamani, Li-Qiang Sun, Eric Mull, Eric P. Gillis, Michael S. Bowsher, Qian Zhao, Nicholas A. Meanwell, Kishore V. Renduchintala, Kandhasamy Sarkunam, Pulicharla Nagalakshmi, P. V. K. Suresh Babu, Paul Michael Scola
  • Patent number: 8937080
    Abstract: Compounds of the formula I: including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: January 20, 2015
    Assignees: Medivir AB, Janssen R&D Ireland
    Inventors: Pierre Jean-Marie Bernard Raboisson, Anna Karin Gertrud Linnea Belfrage, Björn Olof Classon, Karin Charlotta Lindquist, Karl Magnus Nilsson, Åsa Annica Kristina Rosenquist, Bertil Bengt Samuelsson, Horst Jürgen Wähling
  • Patent number: 8927569
    Abstract: A class of macrocyclic compounds of formula (I), wherein R1, R3, R4, Ra, Rb, A, Z, Y, X, M, W, n and m are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes 5 for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: January 6, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Steven Harper, Vincenzo Summa, Nigel J. Liverton, John A. McCauley, John W. Butcher, Marcello Di Filippo, Maria Emilia Di Francesco, Marco Ferrara, Joseph J. Romano, Michael T. Rudd
  • Publication number: 20150005319
    Abstract: The invention relates generally to macrocyclic compounds of formula I and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of IL-17 and/or are useful in the treatment of medical conditions, such as inflammatory diseases and other IL-17-associated disorders.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 1, 2015
    Inventors: Michael Taylor, Nicholas K. Terrett, William H. Connors, Cheri Snedeker, Kelley C. Shortsleeves, Benjamin A. Seigal, Stephen P. Hale, Timothy F. Briggs, Frank G. Favaloro, Jr., Tyler J. Cipriani, Dingxue Yan, Sethu L. Alexander, Atli Thorarensen, Li Xing
  • Patent number: 8921543
    Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.
    Type: Grant
    Filed: January 9, 2012
    Date of Patent: December 30, 2014
    Assignee: AnaSpec Incorporated
    Inventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang, Xiang Guobing
  • Patent number: 8921319
    Abstract: The invention provides methods of making and using compounds of the formula shown, which are inhibitors of human plasmin and plasma kallikrein. (Formula I) The compounds are useful for the prevention of blood loss, and as components of fibrin adhesives.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: December 30, 2014
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Torsten Steinmetzer, Sebastian Martin Saupe
  • Patent number: 8901115
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts 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: August 6, 2012
    Date of Patent: December 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Patrick Y. S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Publication number: 20140350241
    Abstract: Provided herein are ruthenium complexes of Formula I, and processes of preparation thereof. Also provided are methods of their use as a metathesis catalyst.
    Type: Application
    Filed: June 6, 2014
    Publication date: November 27, 2014
    Inventors: Christophe Claude PARSY, Francois-Rene ALEXANDRE, Florence Marie-Emilie BONNATERRE, Dominique SURLERAUX
  • Publication number: 20140343276
    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: July 31, 2014
    Publication date: November 20, 2014
    Inventors: Mimi L. Quan, Carl P. Decicco, James R. Corte, Cailan Wang
  • Patent number: 8883771
    Abstract: Inhibitors of IAP proteins and compositions containing the same are disclosed. Methods of using the IAP protein inhibitors in the treatment of diseases and conditions wherein inhibition of IAP proteins provides a benefit, like cancers, also are disclosed.
    Type: Grant
    Filed: August 16, 2013
    Date of Patent: November 11, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Rong Sheng, Haiying Sun, Liu Liu, Jianfeng Lu, Donna McEachern
  • Publication number: 20140329823
    Abstract: Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes.
    Type: Application
    Filed: July 21, 2014
    Publication date: November 6, 2014
    Applicant: TETRALOGIC PHARMACEUTICALS CORPORATION
    Inventors: Stephen M. Condon, Matthew G. Laporte, Yijun DENG, Susan R. Rippin
  • Publication number: 20140328796
    Abstract: The invention provides 4-amino-4-oxobutanoyl peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof. The variables R1-R9, R16, R18, R19, n, M, n, M, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain 4-amino-4-oxobutanoyl peptide compounds disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide compounds and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain 4-amino-4-oxobutanoyl peptide compound as the only active agent or may contain a combination of 4-amino-4-oxobutanoyl peptide containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.
    Type: Application
    Filed: July 21, 2014
    Publication date: November 6, 2014
    Inventors: Avinash Phadke, Xiangzhu Wang, Suoming Zhang, Atul Agarwal
  • Publication number: 20140323465
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: July 14, 2014
    Publication date: October 30, 2014
    Inventors: Deqiang Niu, Russell C. Petter, Juswinder Singh, Arthur F. Kluge, Lixin Qiao
  • Publication number: 20140323717
    Abstract: Special C-functionalized cyclic bisaminal compounds having formula (I) or (II), their salts or solvates, methods for their preparation, their uses, and methods for preparing functional tetraazacycloalkane compounds implementing such cyclic bisaminal compounds.
    Type: Application
    Filed: November 16, 2012
    Publication date: October 30, 2014
    Inventors: Raphael Tripier, Nathalie Camus
  • Patent number: 8871753
    Abstract: The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
    Type: Grant
    Filed: April 23, 2009
    Date of Patent: October 28, 2014
    Assignee: Incyte Corporation
    Inventors: Andrew Paul Combs, Richard B. Sparks, Eddy W. Yue, Hao Feng, Michael Jason Bower, Wenyu Zhu
  • Publication number: 20140315790
    Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.
    Type: Application
    Filed: April 17, 2013
    Publication date: October 23, 2014
    Inventors: Simon Bushell, Matthew J, LaMarche, Michael A. Patane, Lewis Whitehead
  • 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
  • Patent number: 8853249
    Abstract: The present invention relates to an improved method for the synthesis of particular macrocycles that are inhibitors of the proteasomic degradation of p27, in particular argyrin and derivatives thereof.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: October 7, 2014
    Assignees: Helmholtz-Zentrum für Infektionsforschungs GmbH, Medizinische Hochschule Hannover, Gottfried Wilhelm Leibniz Universität
    Inventors: Markus Kalesse, Ulrike Eggert
  • Publication number: 20140275520
    Abstract: The invention provides a process of preparing 4-amino-4-oxobutanoyl peptides and cyclic analogues thereof of Compound I and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Applicant: Achillion Pharmaceuticals, Inc.
    Inventors: Avinash Phadke, Akihiro Hashimoto
  • Publication number: 20140255347
    Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitroge
    Type: Application
    Filed: May 23, 2014
    Publication date: September 11, 2014
    Applicants: Janssen R&D Ireland, Medivir AB
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Vladimir Ivanov, Mikael Pelcman, Anna Karin Gertrud Linea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
  • Patent number: 8828983
    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: September 9, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mimi L. Quan, Carl P. Decicco, James R. Corte, Cailan Wang
  • Patent number: 8815927
    Abstract: The invention relates to diazo bicyclic Smac mimetics that are tethered through a covalent linker to give a bivalent species. Bivalent diazo bicyclic Smac mimetics function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs). The invention also relates to the use of bivalent diazo bicyclic Smac mimetics for inducing or sensitizing cells to the induction of apoptotic cell death. Thus, compounds of the invention are useful in the treatment, amelioration, or prevention of hyperproliferative diseases such as cancer.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: August 26, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Haiying Sun
  • Publication number: 20140221417
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: January 9, 2014
    Publication date: August 7, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Steven S. BONDY, Carina E. CANNIZZARO, Chien-Hung CHOU, Yunfeng Eric HU, John O. LINK, Qi LIU, Scott D. SCHROEDER, Winston C. TSE, Jennifer R. ZHANG
  • Publication number: 20140221338
    Abstract: The present invention provides compounds of Formula (Ia): 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: August 6, 2012
    Publication date: August 7, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Donald J. P. Pinto, James R. Corte, Paul J. Gilligan, Tianan Fang, Leon M. Smith, II, Yufeng Wang, Wu Yang, William R. Ewing
  • 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: 20140200226
    Abstract: Novel compositions and methods for the treatment and prevention of malaria are disclosed herein.
    Type: Application
    Filed: December 12, 2013
    Publication date: July 17, 2014
    Applicants: Florida Atlantic University, University of Central Florida Research Foundation, Inc.
    Inventors: Debopam Chakrabarti, Amy Wright
  • Patent number: 8779120
    Abstract: The present invention relates to novel macrocyclic derivatives of glycolurils of general formula I, and methods of their preparation. These novel derivatives can be used for the selective removing of various compounds from solutions in polar and nonpolar solvents, and from water, e.g. for water purification and desalination, also for separation of liquid mixtures and mixtures of gases and organic solvent vapors, preparation of ion-exchange materials and materials which are used as stationary phase in chromatography, construction of sensors, transport and targeting of drugs in organisms, and also preparation of materials bearing aromatic or curative compounds.
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: July 15, 2014
    Assignee: Masarykova Univerzita
    Inventors: Vladimir Sindelar, Jan Svec, Vaclav Havel
  • Patent number: 8765728
    Abstract: The present invention relates to compounds of formula (I) compositions, in particular pharmaceutical compositions, and medicaments comprising at least one compound of formula (I). The invention also relates to the use of such a compound for manufacturing a medicament. In particular the medicament and the pharmaceutical composition are intended to treat diseases linked with insulin regulation problems, such as diabetes. This invention aims also to methods for treating or preventing such diseases.
    Type: Grant
    Filed: November 16, 2010
    Date of Patent: July 1, 2014
    Assignee: MelliTech
    Inventors: Didier Roche, Fabrice Chimienti, Martin Ohsten
  • Patent number: 8754106
    Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrog
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: June 17, 2014
    Assignees: Janssen R&D Ireland, Medivir AB
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Vladimir Ivanov, Mikael Pelcman, Anna Karin Gertrud Linea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
  • Patent number: 8754116
    Abstract: Inhibitors of HCV replication of formula (I) wherein W is a heterocycle of formula and the remaining variables are as defined in the specification.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: June 17, 2014
    Assignee: Janssen R&D Ireland
    Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Dominique Louis Nestor Ghislain Surleraux, Wim Van De Vreken