Acyclic Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 544/400)
  • Publication number: 20150099886
    Abstract: The present application relates to a preparation method for solid powder of a carbamic acid derivative, which includes reacting an amine derivative with carbon dioxide at a temperature in a range of from about ?30° C. to about 500° C. and at a pressure in a range of from about 0.3 MPa to about 100 MPa. In addition, the present disclosure relates to a reduction method for solid powder of a carbamic acid derivative to an amine derivative and carbon dioxide, which includes dissolving solid powder of the carbamic acid derivative prepared in a solvent; refluxing the carbamic acid derivative at a temperature in a range of from about 30° C. to about 100° C.; and evaporating the solvent.
    Type: Application
    Filed: December 11, 2014
    Publication date: April 9, 2015
    Inventors: Nam Hwi HUR, Byeong No LEE
  • Publication number: 20140377219
    Abstract: Chemical compounds that inhibit retroviruses are presented herein. More particularly, this disclosure provides small molecule compounds that inhibit infection with, or treat infection caused by, human immunodeficiency viruses.
    Type: Application
    Filed: September 6, 2012
    Publication date: December 25, 2014
    Applicant: New York Blood CEnter, Inc.
    Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
  • Patent number: 8916705
    Abstract: The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.
    Type: Grant
    Filed: October 15, 2012
    Date of Patent: December 23, 2014
    Assignee: The Board of Trustees of the University of Illilnois
    Inventor: Paul J. Hergenrother
  • Publication number: 20140371293
    Abstract: The present invention relates to lipid compounds and uses thereof. In particular, the compounds include a class of cationic lipids having an amine moiety, such as an amino-amine or an amino-amide moiety. The lipid compounds are useful for in vivo or in vitro delivery of one or more agents (e.g., a polyanionic payload or an antisense payload, such as an RNAi agent).
    Type: Application
    Filed: April 17, 2014
    Publication date: December 18, 2014
    Applicant: Dicerna Pharmaceuticals, Inc.
    Inventors: Bob Dale Brown, Sujit Kumar Basu, David A. Schwartz, Allister Fraser
  • Publication number: 20140336185
    Abstract: Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP (1-42), PTH (1-34), Glucagon (1-29), GLP-2 (1-33), GLP-1 (7-36), GLP-1 (9-36), oxyntomodulin and exendin variants.
    Type: Application
    Filed: May 31, 2012
    Publication date: November 13, 2014
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Thomas Fowler, Andrew Novak, Premji Meghani, Enugurthi Brahmachary, Adam Richard Yeager
  • Publication number: 20140323487
    Abstract: Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
    Type: Application
    Filed: July 8, 2014
    Publication date: October 30, 2014
    Inventors: David John Cowan, Andrew Lamont Larkin, Cunyu Zhang, David Lee Musso, Gary Martin Green, Rodolfo Cadilla, Paul Kenneth Spearing, Michael Joseph Bishop, Jason Daniel Speake
  • Publication number: 20140221391
    Abstract: To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R1 represents a hydrogen atom or a C1-C3 alkyl group; R2 represents a hydrogen atom or a C1-C3 alkyl group; R3 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C3 alkoxy C1-C3 alkyl group, or a C1-C3 hydroxyalkyl group; R4 represents a hydrogen atom, a C1-C6 alkyl group, or a halogen atom; n represents an integer of 1 to 4; and X represents methylene, —O—, —NH—, —N(C1-C3 alkyl)-, —C(?O)—, —S—, —S(O)—, —S(O2)—, or a single bond.
    Type: Application
    Filed: December 27, 2013
    Publication date: August 7, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Narihiro Toda, Rieko Takano, Takeshi Shida, Takahiro Katagiri, Mitsuhiro Iwamoto, Shinji Ashida, Mami Yamazaki
  • Patent number: 8778945
    Abstract: Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed that have lower neurotoxicity effects than other compounds.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: July 15, 2014
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Paul Joseph Hergenrother, Quinn Patrick Peterson, Danny Chung Hsu, Diana C. West, Timothy M. Fan, Chris J. Novotny
  • Publication number: 20140179532
    Abstract: The invention relates to a method for producing oligourea compounds by chain building and depolymerization, and to oligourea dispersions, as well as to their use as fungicides, biocides and/or herbicides.
    Type: Application
    Filed: January 13, 2012
    Publication date: June 26, 2014
    Inventor: Werner Klockemann
  • Publication number: 20140128335
    Abstract: The present invention relates to the use of polyaminoisoprenyl derivatives in antibiotic or antiseptic treatment of bacteria including those presenting multiple drug resistance (MDR), in particular as efflux pump inhibitors. It also relates to novel polyaminoisoprenyl derivatives, compositions comprising the same, process for preparing the same, and use thereof in antibiotic or antiseptic treatment.
    Type: Application
    Filed: February 23, 2012
    Publication date: May 8, 2014
    Applicants: UNIVERSITE D'AIX-MARSEILLE, UNIVERSITE DE CORSE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Jean-Michel Bolla, Jean Michel Brunel, Joseph Pierre Felix Casanova, Vannina Lorenzi, Liliane Berti
  • Patent number: 8710060
    Abstract: To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R1 represents a hydrogen atom or a C1-C3 alkyl group; R2 represents a hydrogen atom or a C1-C3 alkyl group; R3 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C3 alkoxy C1-C3 alkyl group, or a C1-C3 hydroxyalkyl group; R4 represents a hydrogen atom, a C1-C6 alkyl group, or a halogen atom; n represents an integer of 1 to 4; and X represents methylene, —O—, —NH—, —N(C1-C3 alkyl)-, —C(?O)—, —S—, —S(O)—, —S(O2)—, or a single bond.
    Type: Grant
    Filed: March 26, 2013
    Date of Patent: April 29, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Narihiro Toda, Rieko Takano, Takeshi Shida, Takahiro Katagiri, Mitsuhiro Iwamoto, Shinji Ashida, Mami Yamazaki
  • Publication number: 20140107129
    Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Application
    Filed: December 11, 2013
    Publication date: April 17, 2014
    Applicant: Galderma Research & Development
    Inventors: Laurence CLARY, Sandrine CHAMBON, Laurent CHANTALAT, Carine ROSIGNOLI, Olivier ROYE, Jean-Claude PASCAL, Marlene SCHUPPLI-NOLLET
  • Publication number: 20140106991
    Abstract: A composition comprising the following formula and optionally salts thereof is disclosed and claimed.
    Type: Application
    Filed: October 15, 2012
    Publication date: April 17, 2014
    Inventors: Eric J. Acosta, Peter A. Webber
  • Publication number: 20140081017
    Abstract: The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, the invention relates to compounds, compositions thereof, and methods for selectively enhancing fungal sensitivity to antifungal compounds.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 20, 2014
    Applicant: METHYLGENE INC.
    Inventor: METHYLGENE INC.
  • Publication number: 20140073609
    Abstract: Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.
    Type: Application
    Filed: May 14, 2013
    Publication date: March 13, 2014
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Paul J. HERGENROTHER, Karson S. PUTT, Quinn P. PETERSON, Valerie FAKO
  • Publication number: 20140051858
    Abstract: The present disclosure relates to a preparation method for powder of a carbamic acid derivative, which includes reacting a liquid amine derivative with carbon dioxide at a temperature in a range of from about ?30° C. to about 500° C. at a pressure in a range of from about 0.3 MPa to about 100 MPa. In addition, the present disclosure relates to a reduction method for powder of a carbamic acid derivative to a liquid amine derivative and carbon dioxide, which includes dissolving powder of the carbamic acid derivative prepared in a solvent; refluxing the carbamic acid derivative at a temperature in a range of from about 30° C. to about 100° C.; and evaporating the solvent.
    Type: Application
    Filed: August 14, 2013
    Publication date: February 20, 2014
    Applicant: Sogang University Research Foundation
    Inventors: Nam Hwi HUR, Byeong No LEE
  • Patent number: 8633196
    Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: January 21, 2014
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marlène Schuppli-Nollet
  • Publication number: 20130323777
    Abstract: A ligand design allows compact nanoparticle materials, such as quantum dots (QDs), with excellent colloidal stability over a wide range of pH and under high salt concentrations. Self-assembled biomolecular conjugates with QDs can be obtained which are stable in biological environments. Energy transfer with these ligands is maximized by minimizing distances between QDs/nanoparticles and donors/acceptors directly attached to the ligands or assembled on their surfaces.
    Type: Application
    Filed: July 16, 2013
    Publication date: December 5, 2013
    Applicant: Naval Research Laboratory
    Inventors: Igor L. Medintz, Kimihiro Susumu, Michael H. Stewart
  • Patent number: 8592584
    Abstract: Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.
    Type: Grant
    Filed: April 15, 2011
    Date of Patent: November 26, 2013
    Assignee: The Board of Trustees of the of The University of Illinois
    Inventors: Paul J. Hergenrother, Karson S. Putt, Quinn P. Peterson, Valerie Fako
  • Patent number: 8575170
    Abstract: Flurbiprofen analog compounds having an amino acid derivatized at the flurbiprofen alkanoic acid carboxyl group and terminating at an ester or amide group are effective in inhibiting cancer cells in vitro and inhibiting the growth of cancers in viva. The compounds and pharmaceutical compositions containing them are particularly useful for the treatment of lung, pancreatic and head and neck cancers.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: November 5, 2013
    Assignee: The Regents of the Unversity of Colorado, a body corporate
    Inventors: Lajos Gera, Daniel C. Chan, Robert S. Hodges, Paul A. Bunn
  • Publication number: 20130289048
    Abstract: To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R1 represents a hydrogen atom or a C1-C3 alkyl group; R2 represents a hydrogen atom or a C1-C3 alkyl group; R3 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C3 alkoxy C1-C3 alkyl group, or a C1-C3 hydroxyalkyl group; R4 represents a hydrogen atom, a C1-C6 alkyl group, or a halogen atom; n represents an integer of 1 to 4; and X represents methylene, —O—, —NH—, —N(C1-C3 alkyl)-, —C(?O)—, —S—, —S(O)—, —S(O2)—, or a single bond.
    Type: Application
    Filed: March 26, 2013
    Publication date: October 31, 2013
    Inventors: Narihiro Toda, Rieko Takano, Takeshi Shida, Takahiro Katagiri, Mitsuhiro Iwamoto, Shinji Ashida, Mami Yamazaki
  • Publication number: 20130289049
    Abstract: The present invention relates to the new acid addition salts AB of the following free base of formula A or the enantiomer thereof with a physiologically acceptable acid B which is selected from among hydrochloric acid, fumaric acid and tartaric acid, as well as the polymorphs, hydrates and solvates thereof.
    Type: Application
    Filed: August 4, 2011
    Publication date: October 31, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Thorsten Pachur, Waldemar Pfrengle, Manfred Birk, Juergen Schnaubelt, Ulrike Werthmann
  • Publication number: 20130281353
    Abstract: The present invention relates to the use of selected metal complex compounds and ligands as oxidation catalysts as well as to a process for removing stains and soil on textiles and hard surfaces. The metal complex compounds have hydrazide ligands, preferably with electron withdrawing groups in the phenyl ring adjacent to the acyl group. Further aspects of the invention are formulations comprising such metal complex compounds, novel metal complex compounds and novel ligands.
    Type: Application
    Filed: June 18, 2013
    Publication date: October 24, 2013
    Inventors: Barbara Winkler, Hauke Rohwer, Marie-Josee Dubs, Menno Hazenkamp, Kai Eichin, Albert Schneider
  • Patent number: 8563714
    Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: October 22, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Publication number: 20130231319
    Abstract: The invention relates to a method for preparing linear polymers having an amide end or having a star architecture comprising an amide core, by means of a ring opening using lactide and glycolide monomers or a lactide monomer ring in the presence of a catalyst, wherein the method includes the steps of: (i) reacting the excess monomer(s) with an initiator in a solvent, said initiator being selected from among an amine and an amino alcohol, given that the initiator has at least one primary or secondary amine function; (ii) adding a catalyst, said catalyst being a non-nucleophilic base and including at least one neutral sp2 nitrogen atom; and (iii) neutralizing the reaction mixture. Said novel method is particularly advantageous in that it can be easily monitored and enables better modulation of the polymers, and thus of the properties thereof, than the methods of the prior art. The invention also relates to novel polymers that are obtainable by means of said method.
    Type: Application
    Filed: November 16, 2011
    Publication date: September 5, 2013
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeup, Sylvaine Gren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein, Davide Pozzi
  • Patent number: 8519188
    Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: August 27, 2013
    Assignee: Marc-Henry Pitty
    Inventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
  • Publication number: 20130203764
    Abstract: Substances and methods are disclosed for reducing or preventing metastatic behaviour in VGSC expressing cancer by the effect of at least reducing the persistent part of the voltage gated sodium channel current without eliminating the transient part. Inhibition of metastatic cell behaviours such as detachability, lateral motility, transverse migration and invasiveness is demonstrated using the known drugs ranolazine and riluzole.
    Type: Application
    Filed: October 13, 2010
    Publication date: August 8, 2013
    Inventor: Mustafa Bilgin Ali Djamgoz
  • Publication number: 20130172363
    Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Application
    Filed: February 22, 2013
    Publication date: July 4, 2013
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Galderma Research & Development
  • Publication number: 20130137702
    Abstract: Novel anticoagulant reversal compounds are disclosed, as well as methods of making the compounds, pharmaceutical compositions including the compounds, methods of using the compounds to reverse the anticoagulant effects of coagulation inhibitors, and diagnostic assays comprising the compounds.
    Type: Application
    Filed: November 29, 2012
    Publication date: May 30, 2013
    Applicant: PEROSPHERE INC.
    Inventor: PEROSPHERE INC.
  • Publication number: 20130137690
    Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: January 28, 2013
    Publication date: May 30, 2013
    Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Matthew G. Stanton, Paul Tempest, Kevin J. Wilson, David J. Witter
  • Publication number: 20130137679
    Abstract: The present invention relates to novel functionally selective ligands of dopamine D2 receptors, FIG. 1 including agonists, antagonists, and inverse agonists. The invention further relates to the use of these compounds for treating central nervous system disorders related to D2 receptors.
    Type: Application
    Filed: July 1, 2011
    Publication date: May 30, 2013
    Inventors: Jian Jin, Bryan Roth, Stephen Frye
  • Patent number: 8450306
    Abstract: Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumor pain and headache diseases.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: May 28, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
  • Publication number: 20130116227
    Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.
    Type: Application
    Filed: July 12, 2011
    Publication date: May 9, 2013
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
  • Patent number: 8435992
    Abstract: Methods for treating cancer by using compound PM00104, in particular, for treating multiple myeloma are provided.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: May 7, 2013
    Assignee: Pharma Mar S.A.
    Inventors: Enrique Ocio, Atanasio Pandiella, Jesús San Miguel, Pablo Manuel Avilés Marín
  • Publication number: 20130109701
    Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfon-amide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein X, Ar1, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Application
    Filed: July 4, 2011
    Publication date: May 2, 2013
    Applicant: Pfizer Limited
    Inventors: Alan Daniel Brown, David James Rawson, Robert Ian Storer, Nigel Alan Swain
  • Patent number: 8426422
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: January 18, 2010
    Date of Patent: April 23, 2013
    Assignee: Abbvie Inc.
    Inventors: Laura A. Hexamer, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Michael D. Wendt
  • Publication number: 20130096133
    Abstract: The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.
    Type: Application
    Filed: October 15, 2012
    Publication date: April 18, 2013
    Applicant: The Board of Trustees of the University lllinois
    Inventor: The Board of Trustees of the University of Illinoi
  • Publication number: 20130090475
    Abstract: A process for the preparation of ranolazine comprises the step of condensing N-(2,6-dimethylphenyl)-1-piperazinyl acetamide with a compound of formula (I) to obtain ranolazine, in which X is chlorine or bromine Ranolazine is prepared by condensing ring-opening halide which replaces epoxide in this process.
    Type: Application
    Filed: December 2, 2010
    Publication date: April 11, 2013
    Applicants: ZHEJIANG JIANFENG HAIZHOU PHARMACEUTICAL CO., LTD., SHANGHAI KUOIKEE LABORATORIES CO., LTD.
    Inventors: Mingfeng Shi, Dan Li, Ling Xu
  • Patent number: 8394805
    Abstract: Novel compounds of which the following is exemplary:
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: March 12, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
  • Publication number: 20130058990
    Abstract: The present invention relates to a cosmetic composition containing a combination i) of at least one screening agent of the dibenzoylmethane derivative type and ii) of at least one particular hydrophilic or water-soluble merocyanin UV-screening agent, especially corresponding to one of the formulae (I) or (II) below: in which at least one or two of the radicals contain: either an alkylsulfonate radical in its acid or salified form, or one or two hydroxyl radicals. The invention also relates to a process for the radiation-photostabilization of at least one screening agent of the dibenzoylmethane derivative type with an effective amount of at least one particular hydrophilic or water-soluble merocyanin UV-screening agent, especially corresponding to one of the formulae (I) or (II).
    Type: Application
    Filed: March 7, 2011
    Publication date: March 7, 2013
    Applicant: L'OREAL
    Inventors: Herve Richard, Benoit Muller
  • Publication number: 20130053392
    Abstract: A carbonic anhydrase IX (CA IX) inhibitor which comprises a compound of general formula: R—NH—CX—NH—(CH2)n—Ar-Q-SO2—NH2 or a pharmaceutically-acceptable salt, derivative or prodrug thereof; wherein n=0, 1 or 2; Q is O or NH; X is O or S; and R comprises an organic substituent group.
    Type: Application
    Filed: February 14, 2011
    Publication date: February 28, 2013
    Inventors: Peter Ebbesen, Claudlu T. Supuran, Andrea Scozzafava, Erik Olai Pettersen, Kaye Williams, Ludwig Dubois, Philippe Lambin
  • Publication number: 20130045499
    Abstract: A ligand design allows compact nanoparticle materials, such as quantum dots (QDs), with excellent colloidal stability over a wide range of pH and under high salt concentrations. Self-assembled biomolecular conjugates with QDs can be obtained which are stable in biological environments. Energy transfer with these ligands is maximized by minimizing distances between QDs/nanoparticles and donors/acceptors directly attached to the ligands or assembled on their surfaces.
    Type: Application
    Filed: August 15, 2011
    Publication date: February 21, 2013
    Applicant: The Government of the United States of America, as represented by the Secretary of the Navy
    Inventors: Igor L. Medintz, Kimihiro Susumu, Michael H. Stewart
  • Patent number: 8357679
    Abstract: The present invention relates to hexafluoroisopropanol derivatives having the general formula I to pharmaceutical compositions comprising the same and to the use of these hexafluoroisopropanol derivatives in the treatment of atherosclerosis.
    Type: Grant
    Filed: May 13, 2009
    Date of Patent: January 22, 2013
    Assignee: MSD Oss B.V.
    Inventors: Andrew John Cooke, Andrew Stanley Edwards, Fiona Elizabeth Andrews, David Jonathan Bennett, Olaf Nimz, Emma Louise Carswell
  • Patent number: 8343963
    Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: January 1, 2013
    Assignee: 4SC AG
    Inventor: Stefano Pegoraro
  • Patent number: 8329751
    Abstract: The invention relates to aryl-sulphonamido compounds endowed with inhibitory activity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, R4, R5, n and m have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.
    Type: Grant
    Filed: March 14, 2008
    Date of Patent: December 11, 2012
    Assignee: Bracco Imaging S.p.A.
    Inventors: Aldo Balsamo, Armando Rossello, Elisa Nuti, Elisabetta Orlandini, Tiziano Tuccinardi
  • Publication number: 20120260825
    Abstract: Dispersants for pigments as well as dispersions containing them, and compositions such as inks and coatings containing them are described. The dispersants are the reaction product of at least one dianhydride with at least two different reactants, each of which can be an amine, alcohol, or thiol, and at least one of which is polymeric.
    Type: Application
    Filed: June 20, 2012
    Publication date: October 18, 2012
    Inventors: Tatiana N. ROMANOVA, Russell J. SCHWARTZ
  • Publication number: 20120263670
    Abstract: The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.
    Type: Application
    Filed: June 29, 2011
    Publication date: October 18, 2012
    Applicant: Ardelyx, Inc.
    Inventors: Dominique Charmot, Jeffrey W. Jacobs, Michael Robert Leadbetter, Marc Navre, Christopher Carreras, Noah Bell
  • Publication number: 20120238754
    Abstract: The present invention relates to an improved process for manufacturing dihydropteridinones of general formula (12) as well as intermediates thereof, wherein the groups R1, R2, R3, R4, and R5 have the meanings given in the claims and specification.
    Type: Application
    Filed: September 15, 2011
    Publication date: September 20, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Juergen Schnaubelt, Rolf Herter
  • Publication number: 20120220603
    Abstract: Compounds of formula (I) which are useful in ameliorating conditions characterized by unwanted sodium and/or calcium channel activity, particularly unwanted NaV 1.7, NaV 1.8, or CaV 3.2 channel activity are disclosed. Specifically, a series of compounds containing piperidine or piperazine linked through an amide, isoxazole or similar linker to an aryl ring are described and are shown to be useful for the treatment of pain or epilepsy. A is selected from Formulae (i) or (ii).
    Type: Application
    Filed: September 3, 2010
    Publication date: August 30, 2012
    Applicant: ZALICUS PHARMACEUTICALS LTD.
    Inventors: Hassan Pajouhesh, Mike Grimwood, Yongbao Zhu, Yanbing Ding, Richard Holland
  • Patent number: 8242175
    Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: August 14, 2012
    Assignee: DAC S.R.L.
    Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa