Amino Nitrogen, Not Bonded Directly To Carbonyl, Containing Patents (Class 564/157)
  • Patent number: 9090658
    Abstract: The invention relates to the novel base-substituted benzylamine analogs of general formula (I), wherein A represents P2-P1 with P1?(A) and P2?(B), for use as coagulation factor Xa inhibitors. The invention also relates to the production and use of said analogs in the therapy and prophylaxis of cardiovascular diseases and thromboembolic events.
    Type: Grant
    Filed: September 13, 2004
    Date of Patent: July 28, 2015
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz, Anne Stürzebecher, Daniel Dönnecke
  • Publication number: 20150148517
    Abstract: A compound represented by Chemical Formula 1: wherein in Chemical Formula 1, R1 and R2 are the same or different, and are each independently an electron-withdrawing group, R3 to R6 are the same or different, and are each independently selected from a hydrogen, a substituted or unsubstituted C1 to C20 alkyl group, and a substituted or unsubstituted C6 to C20 aryl group, and n11 and n12 are the same or different, and are each independently an integer from 1 to 4.
    Type: Application
    Filed: July 28, 2014
    Publication date: May 28, 2015
    Inventors: DMITRY Androsov, MIKHAIL Kovalev, EVGENY Kiryushchenkov, FEDOSYA Kalinina
  • Patent number: 9012687
    Abstract: The present invention provides a process for isolating kukoamine by solid phase extraction using a polyamide or a derivative thereof as an adsorbent. Said process is convenient, economical and environmental-friendly, and obtains highly purified kukoamines with a high yield.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: April 21, 2015
    Assignee: City University of Hong Kong
    Inventors: Hon-Yeung Cheung, Yuan-Yuan Li, Rui Di
  • Publication number: 20150080472
    Abstract: The invention provides methods of treating Friedreich's ataxia using histone deacetylase inhibitors.
    Type: Application
    Filed: September 9, 2014
    Publication date: March 19, 2015
    Inventors: JOEL M. GOTTESFELD, ANN-KRISTIN JENSSEN, DAVID M. HERMAN, RYAN BURNETT, C. JAMES CHOU
  • Publication number: 20150065721
    Abstract: Provided is a method for producing an aromatic amide derivative represented by Formula (4), the method including a process in which an aromatic amide derivative represented by Formula (1) and a haloalkyl compound represented by Formula (3) are reacted with each other in the presence of a base and a metal or metal salt. In the formulae, each of X and Y represents a hydrogen atom, a halogen atom, or the like. A represents a hydrogen atom, an alkyl group, a group represented by Formula (2), or the like. Each of G1 and G2 represents an oxygen atom or the like. Q1 represents a phenyl group or the like. R1 represents a hydrogen atom, an alkyl group, or the like. Z1 represents a haloalkyl group or the like. Xa represents an iodine atom or the like. m represents a number of from 1 to 4, n1 represents a number from 1 to 5, and n2 represents a number of from 1 to 4.
    Type: Application
    Filed: March 29, 2013
    Publication date: March 5, 2015
    Applicant: Mitsui Chemicals Agro, Inc.
    Inventor: Hironari Okura
  • Publication number: 20150065752
    Abstract: The present invention provides a process for isolating kukoamine by solid phase extraction using a polyamide or a derivative thereof as an adsorbent. Said process is convenient, economical and environmental-friendly, and obtains highly purified kukoamines with a high yield.
    Type: Application
    Filed: April 24, 2014
    Publication date: March 5, 2015
    Applicant: City University of Hong Kong
    Inventors: Hon-Yeung Cheung, Yuan-Yuan Li, Rui Di
  • Publication number: 20150025274
    Abstract: This invention relates to processes for the preparation of (R)-2-acetamido-N-benzyl-3-methoxypropionamide (I) and intermediates thereof. Formula (I).
    Type: Application
    Filed: August 29, 2012
    Publication date: January 22, 2015
    Applicant: SIGNA S.A. DE C.V.
    Inventors: Pablo Miguel Bernal-Vazquez, José Miguel Lazcano-Seres, Yaneth Mariá-Antonieta Contreras-Martinez, Jorge Alberto Juárez-Lagunas, Donato Sánchez-Mereles, Juan Rolando Vázquez-Miranda, Armando Zambrano-Huerta
  • Publication number: 20150018566
    Abstract: The invention provides combretastatin A-4 like compounds that are modified to have enhanced tubulin binding activity and in some embodiments the ability to promote accumulation in the vasculature undergoing angiogenesis (homing activity). The compounds are based on the combretastatin A-4 skeletal structure having a tubulin-binding pharmacophore comprising two fused rings (A and B rings) in which the B ring is substituted with (a) an aromatic ring structure (C ring) and (b) a second substituent/functional group that comes off the B ring. The aromatic ring structure is typically a six membered ring phenolic or aniline structure, or may also be a fused ring structure such as a substituted or unsubstituted naphthalene.
    Type: Application
    Filed: August 27, 2012
    Publication date: January 15, 2015
    Inventors: John Jarlath Walsh, Richard Shah, Emmet Martin McCormack, Gillian Joy Hudson, Martina White, Gary Daniel Stack, Brian William Moran, Adrian Coogan, Elaine Carmel Breen
  • Patent number: 8933065
    Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula I or Ia: or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: January 13, 2015
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Harold L. Kohn, Christophe Salomé, Ki Duk Park, Elise Salomé-Grosjean
  • Publication number: 20150011730
    Abstract: Structural and functional analysis of peptide inhibitor binding to the cyclin D and cyclin A groove has been investigated and used to design peptides that provide the basis for structure-activity relationships, have improved binding and have potential for development as chemical biology probes, as potential diagnostics and as therapeutics in the treatment of proliferative diseases including cancer and inflammation.
    Type: Application
    Filed: September 22, 2014
    Publication date: January 8, 2015
    Inventors: Campbell McInnes, Shu Liu
  • Publication number: 20150011793
    Abstract: The present invention relates to an improved process for the preparation of pure compound of Formula-II, which is an intermediate in the preparation of Aliskiren and further conversion of compound of Formula-II into Aliskiren or its pharmaceutically acceptable salts.
    Type: Application
    Filed: February 15, 2013
    Publication date: January 8, 2015
    Applicant: MYLAN LABORATORIES LTD
    Inventors: Shankar Rama, Seshadri Rao Manukonda, Srinivasa Rao Dasari
  • Publication number: 20150011726
    Abstract: Provided are (i) a polyimide which is transparent and has an excellent solution processability, a high heat resistance, and a low linear thermal expansion coefficient, and (ii) a polyimide film of the polyimide. According to the present invention, it is possible to produce, by use of a novel diamine characterized in having an amide group and a trifluoromethyl group, the polyimide which is transparent and has the excellent solution processability, the high heat resistance, and the low linear thermal expansion coefficient. The polyimide can be applied to various electronic devices such as an electronic display device.
    Type: Application
    Filed: February 4, 2013
    Publication date: January 8, 2015
    Inventors: Masatoshi Hasegawa, Junichi Ishii
  • Publication number: 20150004698
    Abstract: Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.
    Type: Application
    Filed: August 29, 2014
    Publication date: January 1, 2015
    Applicants: YALE UNIVERSITY, UNIVERSITY OF SOUTH FLORIDA
    Inventors: Said M. Sebti, Jin Q. Cheng, Andrew D. Hamilton, Katherine Kayser-Bricker
  • Patent number: 8912359
    Abstract: A method of combating infectious agents, such as Pneumocystis pneumonia, and a method of treating a subject in need of such treatment is disclosed. The method comprises administering to the subject a bis-benzamidoxime of formula I wherein the linker is a di-substituted cyclic moiety of any ring size and may contain at least one heteroatom; the aromatic group is 1,2-; 1,3-; or 1,4-disubstituted; R is selected from the group consisting of a hydrogen, a linear or branched alkyl group, containing from 1 to 20 carbon atoms; R? is selected from the group consisting of a hydrogen, a linear or branched alkyl group containing from one to twenty carbon atoms, an aromatic ring, a cycloalkyl group containing three to eight carbon atoms, or a hydroxyl group; alternatively, R and R? may form a cyclic structure that can be fused to another cyclic system; or a pharmaceutically acceptable salt thereof. Pharmaceutical formulations and active compounds useful in the practice of the present invention are also disclosed.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: December 16, 2014
    Assignees: University of Cincinnati, Xavier University
    Inventors: Peter D. Walzer, Melanie T. Cushion, Annie Mayence, Tien Liang Huang, Jean Jacques Vanden Eynde
  • Publication number: 20140350284
    Abstract: Provided herein are compositions including diastereomers in substantially diastereomerically pure form and enantiomers in substantially enantiomerically pure form, and processes for preparing them and converting them to metyrosine.
    Type: Application
    Filed: August 8, 2014
    Publication date: November 27, 2014
    Inventors: Kevin John HALLORAN, Alex COMELY, Zhengming CHEN, Shyam KRISHNAN
  • Publication number: 20140350300
    Abstract: Aliskiren hemi fumarate has novel distinctive physico-chemical properties. An amorphous solid is also made of the same Aliskiren hemi fumarate. process for the prepares the forms of Aliskiren hemifumarate.
    Type: Application
    Filed: July 10, 2012
    Publication date: November 27, 2014
    Applicant: DJADA PHARMACEUTICAL SA
    Inventors: Domenico Badone, Lau C.K., Yuan Jiandong
  • Publication number: 20140350113
    Abstract: Described herein are small-molecule mimics of CD4, which both enter the Phe43 cavity and target Asp368 of gp120, the HIV-1 envelope protein. Also described herein are methods of using these compounds to inhibit the transmission or progression of HIV infection. These compounds exhibit antiviral potency greater than that of a known antiviral, NBD-556, with 100% breadth against clade B and C viruses. Importantly, the compounds do not activate HIV infection of CD4-negative, CCR5-positive cells, in contrast to NBD-556.
    Type: Application
    Filed: December 14, 2012
    Publication date: November 27, 2014
    Inventors: Joseph Sodroski, Judith M. LaLonde, Amos B. Smith, III, Peter D. Kwong, Young Do Kwon, David M. Jones, Alexander W. Sun, Joel R. Courter, Takahiro Soeta, Toyoharu Kobayashi, Amy M. Princiotto, Xueling Wu, John R. Mascola, Ame Schon, Emesto Freire, Navid Madani, Matthew Le-Khac, Wayne A. Hendrickson
  • Patent number: 8889163
    Abstract: Facially amphiphilic polyphenylene and heteroarylene polymers and articles made therform having biocidal surfaces are disclosed. The polymers can inhibit the growth of microorganisms in contact with the surface or in areas adjacent to said biocidal surface. There is also disclosed a methods to attach facially amphiphilic polmers to a solid support. Utility as a contact disinfectant is disclosed.
    Type: Grant
    Filed: March 7, 2002
    Date of Patent: November 18, 2014
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Gregory N. Tew, Michael L. Klein
  • Patent number: 8889678
    Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: November 18, 2014
    Assignees: Centre National de la Recherche Scientifique, Universite de Strasbourg
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
  • Publication number: 20140329746
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
  • Publication number: 20140323738
    Abstract: The invention is a novel process for the preparation of lacosamide by employing novel intermediates of formula III and IV:
    Type: Application
    Filed: November 8, 2012
    Publication date: October 30, 2014
    Inventor: RAMAMOHAN RAO DAVULURI
  • Publication number: 20140309174
    Abstract: The present invention provides compounds having formula (I): and additionally provides methods for the synthesis thereof and methods for the use thereof in the treatment of cancer, wherein R1-R7, X1, X2, R, Q, and n are as defined herein.
    Type: Application
    Filed: November 12, 2013
    Publication date: October 16, 2014
    Applicant: Eisai Co., Ltd
    Inventors: James J. Kowalczyk, Galina Kuznetsov, Shawn Schiller, Boris M. Seletsky, Mark Spyvee, Hu Yang
  • Publication number: 20140303395
    Abstract: The present invention relates to the use of oligohydroxybenzoic acid derivatives in washing and cleaning agents in order to improve washing or cleaning performance with respect to bleachable stains.
    Type: Application
    Filed: June 18, 2014
    Publication date: October 9, 2014
    Inventors: Christian Kropf, Mareile Job, Christian Umbreit, Siglinde Erpenbach
  • Publication number: 20140296343
    Abstract: Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule.
    Type: Application
    Filed: March 31, 2014
    Publication date: October 2, 2014
    Inventors: Frank M. LONGO, Stephen M. MASSA, Sandeep GUPTA
  • Patent number: 8846932
    Abstract: Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3. Also disclosed are small molecule modulators of MEF2 and its associated factors that include but not limited to histone deacetylases (HDACs), p300/CBP and Cabin1 and the therapeutic applications thereof.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: September 30, 2014
    Assignee: University of Southern California
    Inventors: Lin Chen, Nimanthi Jayathilaka, Aidong Han, Nicos A. Petasis
  • Publication number: 20140275268
    Abstract: Novel solid forms of tacedinaline (4-(acetylamino)-N-(2-aminophenyl)benzamide), including crystalline tacedinaline Form B, a novel crystalline tacedinaline TFA salt, and amorphous tacedinaline, are disclosed. Pharmaceutical compositions comprising crystalline tacedinaline Form B, the novel crystalline tacedinaline TFA salt, and/or amorphous tacedinaline, and methods of treating various conditions by administering those novel solid forms, are also disclosed.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: THE BROAD INSTITUTE, INC.
    Inventors: Edward Holson, Florence F. Wagner, G. Patrick Stahly
  • Publication number: 20140256963
    Abstract: The present invention provides a novel process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren, or a salt thereof, preferably Aliskiren hemifumarate.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 11, 2014
    Inventors: Sujay Biswas, Sankareswaran Srimurugan, Anjul Kumar, Atulya Kumar Panda, Danish Jamshad, Mukesh Masand, Bidyut Biswas, Vikas Bansal, Ashish Kumar Gupta, Dharam Vir
  • Publication number: 20140256775
    Abstract: The present disclosure provides novel compounds capable of functioning as transcription factor modulators, as well as compositions, pharmaceutical formulations, and kits. Also provided are methods of treating a condition regulatable by a transcription factor and/or cofactor using the compounds, compositions, pharmaceutical formulations, and kits provided herein.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 11, 2014
    Inventors: Lin CHEN, Xiaojiang CHEN, Yongqing WU, Dahai GAI
  • Publication number: 20140256698
    Abstract: The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 11, 2014
    Inventors: Robert Booth, Jeff Dener, Michael Green
  • Publication number: 20140248236
    Abstract: The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.
    Type: Application
    Filed: November 7, 2012
    Publication date: September 4, 2014
    Inventors: Michael G. Natchus, Richard Arrendale
  • Publication number: 20140249201
    Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 4, 2014
    Applicant: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
  • Patent number: 8822524
    Abstract: Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: September 2, 2014
    Assignees: University of South Florida, Yale University
    Inventors: Said M. Sebti, Jin Q. Cheng, Andrew D. Hamilton, Katherine Kayser-Bricker
  • Publication number: 20140221431
    Abstract: Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 7, 2014
    Applicants: Shanghai Institute of Pharmaceutical Industry, Sinopharm A-think Pharmaceutical Co., Ltd
    Inventors: Jianqi Li, Qingwei Zhang, Zhidan Jia, Jiajing Wang
  • Publication number: 20140213821
    Abstract: It is described a process for the opening of lactone or lactam rings useful in the synthesis of pharmaceutically active compounds and the intermediates thereof, particularly Aliskiren. It has found that by selecting a type of solvent it is possible to obtain excellent yields and high optical and chemical purity of the isolated products.
    Type: Application
    Filed: July 25, 2012
    Publication date: July 31, 2014
    Applicant: CHEMO IBERICA, S. A.
    Inventors: Luca Carcone, Domenico Magrone, Giuseppe Barreca, Marcello Rasparini, Huang Liming
  • Publication number: 20140213611
    Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R9 are as defined herein.
    Type: Application
    Filed: July 6, 2012
    Publication date: July 31, 2014
    Applicant: KalVista Pharmaceuticals Limited
    Inventors: David Michael Evans, Rebecca Louise Davie, Hannah Joy Edwards, David Philip Rooker
  • Patent number: 8791246
    Abstract: An inventive substrate is provided which includes a substrate compound of formula A-B1-B2-B3-B4: wherein A is a sugar moiety; B1 is a linker moiety allowing the conjugation of moiety A and the remaining structure of the substrate; B2 is a linker moiety with a free reactive amino group so as to be available for reaction with carboxylic acids or detectable tags; B3 contains a permanently charged element such as a quaternary ammonium group so as to increase sensitivity for mass spectrometry analysis; and B4 of various carbon length conferring specificity amongst individual substrates in detection methods. Also provided is a molecule of the formula B1-B2-B3-B4, with similar structural characteristics to an enzymatic product produced by the action of a target enzyme on an inventive substrate. Further provided are methods for using inventive substrates for detecting enzymatic activity.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: July 29, 2014
    Assignee: PerkinElmer Health Sciences, Inc.
    Inventors: Blas Cerda, Mark Norman Bobrow
  • Patent number: 8791076
    Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 29, 2014
    Inventors: Pablo Villoslada, Angel Messeguer
  • Patent number: 8779198
    Abstract: The present invention provides a novel process for opening a lactone and/or a lactam ring. More particularly, the present invention provides a process that employs a novel catalyst in the opening of a lactone ring and/or a lactam ring. Additionally, the present invention also provides a novel deprotection process of any protecting group present in either the lactone ring-containing and/or lactam ring-containing compound and/or in the ring-opened product thereof.
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: July 15, 2014
    Assignees: Novartis AG, Massachusetts Institute of Technology
    Inventors: Megan Alene Foley, Timothy F. Jamison, Oljan Repic
  • Patent number: 8759388
    Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
    Type: Grant
    Filed: April 9, 2012
    Date of Patent: June 24, 2014
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
  • Publication number: 20140155436
    Abstract: The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.
    Type: Application
    Filed: November 4, 2013
    Publication date: June 5, 2014
    Applicants: CENTRE NATIONAL DE RECHERCHE SCIENTIFIQUE, UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUES, INSTITUT CURIE
    Inventors: Jamal TAZI, David GRIERSON, Florence MAHUTEAU-BETZER, Pierre ROUX
  • Publication number: 20140142117
    Abstract: The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
    Type: Application
    Filed: November 11, 2013
    Publication date: May 22, 2014
    Inventors: John H. van Duzer, Ralph Mazitschek, Walter Ogier, James E. Bradner, Guoxiang Huang, Dejian Xie, Nan Yu
  • Publication number: 20140141510
    Abstract: The present invention relates to the use of a compound which inhibits the activity of MKK4 as a medicament for the treatment of a patient suffering from an impaired liver function, to the use of a compound as a medicament for the treatment of liver failure, including acute/fulminant or chronic liver failure and/or for increasing the regeneration of liver tissue in a patient.
    Type: Application
    Filed: April 10, 2012
    Publication date: May 22, 2014
    Applicants: MEDIZINISCHE HOCHSCHULE HANNOVER, HELMHOLTZ ZENTRUM FUER INFEKTIONSFORSCHUNG GMBH
    Inventors: Lars Zender, Torsten Wuestefeld
  • Publication number: 20140142114
    Abstract: The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X2, X3, X4, X5, X6, X7 and X8 are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.
    Type: Application
    Filed: November 19, 2013
    Publication date: May 22, 2014
    Applicant: Merial Limited
    Inventors: Charles Q. Meng, Alan Long, Scot Huber, Srinivas Reddy Gurrala, Douglas Edward Wilkinson, Gregory Pacofsky
  • Patent number: 8729130
    Abstract: Novel solid forms of tacedinaline (4-(acetylamino)-N-(2-aminophenyl)benzamide), including crystalline tacedinaline Forms A, B, and D, a novel crystalline tacedinaline TFA salt, and amorphous tacedinaline, are disclosed. Pharmaceutical compositions comprising crystalline tacedinaline Forms A, B, and D, the novel crystalline tacedinaline TFA salt, and/or amorphous tacedinaline, and methods of treating various conditions by administering those novel solid forms, are also disclosed.
    Type: Grant
    Filed: September 15, 2012
    Date of Patent: May 20, 2014
    Assignee: The Broad Institute, Inc.
    Inventors: Edward Holson, Florence F. Wagner, G. Patrick Stahly
  • Patent number: 8716530
    Abstract: The present invention discloses methods of use of facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, including, but not limited to, pharmaceutical uses of the polymers and oligomers as antimicrobial agents and as antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, compositions of the novel polymers and oligomers, including pharmaceutical compositions, and methods of designing and synthesizing the facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers.
    Type: Grant
    Filed: February 3, 2012
    Date of Patent: May 6, 2014
    Assignee: The Trustess of the University of Pennsylvania
    Inventors: William F. DeGrado, Dahui Liu, Gregory N. Tew, Michael L. Klein
  • Publication number: 20140121279
    Abstract: The present invention relates to dipeptide enkephalin analogues of Formula (I) and their tautomers, ionic forms and pharmaceutically acceptable salts, and their use in medicine, in particular as opioid agonists.
    Type: Application
    Filed: June 29, 2012
    Publication date: May 1, 2014
    Applicant: Pfizer Limited
    Inventor: Dafydd Rhys Owen
  • Patent number: 8697729
    Abstract: Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3. Also disclosed are small molecule modulators of MEF2 and its associated factors that include but not limited to histone deacetylases (HDACs), p300/CBP and Cabin1 and the therapeutic applications thereof.
    Type: Grant
    Filed: November 5, 2009
    Date of Patent: April 15, 2014
    Assignee: University of Southern California
    Inventors: Lin Chen, Nimanthi Jayathilaka, Aidong Han, Nicos Petasis
  • Patent number: 8691875
    Abstract: Novel solid forms of tacedinaline (4-(acetylamino)-N-(2-aminophenyl)benzamide), including crystalline tacedinaline Forms A, B, and D, a novel crystalline tacedinaline TFA salt, and amorphous tacedinaline, are disclosed. Pharmaceutical compositions comprising crystalline tacedinaline Forms A, B, and D, the novel crystalline tacedinaline TFA salt, and/or amorphous tacedinaline, and methods of treating various conditions by administering those novel solid forms, are also disclosed.
    Type: Grant
    Filed: September 15, 2012
    Date of Patent: April 8, 2014
    Assignee: Broad Institute, Inc.
    Inventors: Edward Holson, Florence F. Wagner, G. Patrick Stahly
  • Publication number: 20140094613
    Abstract: A process for producing a 3-alkoxy-2-amino-6-fluoro bicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivative represented by the formula (I) or a salt thereof, which includes converting a compound represented by the formula (VI) or a salt thereof to the compound represented by the formula (I) or a salt thereof.
    Type: Application
    Filed: December 5, 2013
    Publication date: April 3, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Noriaki MURASE, Toshihito KUMAGAI, Hisaya WADA, Hisahide TANIMOTO, Koumei OHTA, Yoshihiro KIMURA
  • Patent number: 8664440
    Abstract: A method for preparing Aliskiren and intermediate thereof, which comprises the following steps: reacting 4-bromo-1-methoxy-2-(3-methoxypropoxy)benzene with magnesium isopropyl chloride and n-BuLi to obtain the compound of formula XXII; reacting the product of methylsulfonylation of the compound of formula XIX with anhydrous LiBr to obtain the compound of formula XXI; obtaining the intermediate of Aliskiren shown as formula XV by reacting the compound of formula XXII with the compound of formula XXI in an ether as the solvent and in the presence of a catalyst containing iron; then reacting the compound of formula XV with the compound of formula VII to obtain the compound of formula XXIII, following removing R1 from the amino group and obtaining Aliskiren shown as formula I.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: March 4, 2014
    Assignee: Zhejiang Tianyu Pharmaceutical Co., Ltd
    Inventors: Yongjun Tu, Yi Zhang, Rongde Cheng, Lingchao Peng