Amidine, Azomethine, Ketimine Or Oxime In Acid Moiety Patents (Class 560/168)
  • Publication number: 20150031854
    Abstract: The invention relates to novel hemin derivatives of general formula (I), preparing and use thereof as antibacterial and/or antiviral agents, including, as a component in a pharmaceutical compositions. Advantages of the novel antibacterial and antiviral agents based on the hemin derivatives are in their biocompatibility, biodegradability, a high efficacy against resistant bacteria and widespread viruses which are dangerous to humans, and the lack of toxicity.
    Type: Application
    Filed: November 15, 2012
    Publication date: January 29, 2015
    Applicant: OBSSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU "PHARMENTERPRISES"
    Inventors: Vladimir Evgenievich Nebolsin, Galina Alexandrovna Zheltukhina, Sergei Alexandrovich Okorochenkov
  • Publication number: 20150023900
    Abstract: A process for preparing amino acid-modified siloxanes that can be carried out under mild conditions is provided as well as organically modified silicones for care formulations for skin, hair and textiles that are toxicologically unobjectionable.
    Type: Application
    Filed: July 15, 2014
    Publication date: January 22, 2015
    Applicant: Evonik Industries AG
    Inventors: Wilfried Knott, Frauke Henning, Sadik Amajjahe, Sarah Krauskopf, Michael Fiedel, Olga Jazkewitsch, Christian Hartung
  • Patent number: 8907120
    Abstract: Compounds containing at least one perfluoropolyether segment and at least two oxalylamino groups as well as methods of making these compounds are described. The compounds can be polymeric materials or can be used in the preparation of various copolymeric materials by reaction with compounds having at least two primary or secondary amino groups.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: December 9, 2014
    Assignee: 3M Innovative Properties Company
    Inventors: Yu Yang, Miguel A. Guerra, Richard G. Hansen, David S. Hays, Suresh S. Iyer, Ramesh C. Kumar, George G. I. Moore
  • Publication number: 20140323756
    Abstract: The present invention is related to synthesis of highly pure cationic surfactant products by eliminating or reducing impurities generation that has beset prior art. This is achieved through the N-acylation of ester of amino acid and its inorganic salts or its organic salts (e.g. amino acid or hydrochloride of amino acid or sulfate of amino acid or acetate of amino acid etc.) in non-hydrolytic or nearly non-hydrolytic reaction conditions involving mono or biphasic reaction system with fatty acid halide (C4 to C20), under moderate uniform basic condition yielding high purity N-acyl substituted amino acid ester, particularly ethyl lauroyl arginate. The present process achieves pH control through process strategy rather than the measurement and control steps. This ambient temperature process is stable through a range of temperature variation eliminating rigid low temperature control.
    Type: Application
    Filed: May 4, 2012
    Publication date: October 30, 2014
    Applicant: EBURON ORGANICS INTERNATIONAL II, LLC
    Inventors: Dilip S. Mehta, Mayank Shastri
  • Publication number: 20130324600
    Abstract: The invention relates to compounds of general formula (I) wherein R is (C1-C7)alkyl, (C2-C7)alkenyl or (C2-C7)alkynyl; wherein R is substituted with R1; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
    Type: Application
    Filed: December 22, 2011
    Publication date: December 5, 2013
    Applicant: LEO LABORATORIES LIMITED
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg
  • Publication number: 20130158021
    Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.
    Type: Application
    Filed: October 26, 2012
    Publication date: June 20, 2013
    Applicant: Massachusetts Institute of Technology
    Inventor: Massachusetts Institute of Technology
  • Publication number: 20120289736
    Abstract: Compounds containing at least one perfluoropolyether segment and at least two oxalylamino groups as well as methods of making these compounds are described. The compounds can be polymeric materials or can be used in the preparation of various copolymeric materials by reaction with compounds having at least two primary or secondary amino groups.
    Type: Application
    Filed: December 22, 2010
    Publication date: November 15, 2012
    Applicant: 3M INNOVATIVE PROPERTIES COMPANY
    Inventors: Yu Yang, Miguel A. Guerra, Richard G. Hansen, David S. Hays, Suresh S. Iyer, Ramesh C. Kumar, George G.I. Moore
  • Publication number: 20120283299
    Abstract: A biguanide derivative compound with N1-N5 substitution, which is represented by Formula 1, or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a pharmaceutical composition containing the same as an active ingredient are provided. The biguanide derivative may exhibit excellent effect on activation of AMPK? and inhibition of cancer cell proliferation in a low dose, compared to conventional drugs, and thus, may be useful to treat diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer, etc.
    Type: Application
    Filed: January 6, 2011
    Publication date: November 8, 2012
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Sung Wuk Kim, Sung Soo Jun, Chang Hee Min, Young Woong Kim, Min Seok Kang, Byung Kyu Oh, Se Hwan Park, Yong Eun Kim, Duck Kim, Ji Sun Lee, Ju Hoon Oh
  • Publication number: 20120277459
    Abstract: The invention relates to the field of pharmaceutical chemistry, specifically to processes for preparing biologically active substances (BAS), in particular creatine amides. What is proposed is a process for preparing creatine amides which comprises treating creatine with para-toluenesulfonic acid in an organic solvent with subsequent reaction of the resultant complex with compounds comprising a primary or secondary amino group in the presence of a condensing agent and a base which are introduced subsequently. The claimed process makes it possible to increase the yield of the end product by 2-5 times in comparison with analogs and also to extend the range of the compounds prepared.
    Type: Application
    Filed: September 28, 2010
    Publication date: November 1, 2012
    Inventors: Sergej Vladimirovich Burov, Olga Sergeevna Veselkina, Maria Victorovna Leko
  • Patent number: 8252952
    Abstract: The present invention discloses an optically active quarternary ammonium salt having axial asymmetry and a method for producing an ?-amino acid and a derivative thereof using the same. The optically active quarternary ammonium salt having axial asymmetry of the present invention is a chiral phase-transfer catalyst that has a simple structure and that can be produced in a smaller number of process steps. The compound of the present invention is very useful as a phase-transfer catalyst in the synthesis of an ?-alkyl-?-amino acid and a derivative thereof as well as an ?,?-dialkyl-?-amino acid and a derivative thereof. Therefore, the compound of the present invention can be used in the development of novel foods and pharmaceuticals.
    Type: Grant
    Filed: December 28, 2011
    Date of Patent: August 28, 2012
    Assignee: Nagase & Co., Ltd.
    Inventors: Keiji Maruoka, Kenichiro Yamamoto, Yukifumi Nishimoto
  • Publication number: 20120123111
    Abstract: The present invention relates to physically-chemically and pharmacokinetically enhanced N?-hydroxy-L-arginine (NOHA) derivatives and a method for producing the NOHA derivatives having enhanced physical-chemical and pharmacokinetic properties according to the invention.
    Type: Application
    Filed: January 4, 2010
    Publication date: May 17, 2012
    Applicant: Christian-Albrechts-Universitaet Zu Kiel
    Inventors: Bernd Clement, Dennis Schade, Jürke Kotthaus
  • Patent number: 8173157
    Abstract: A pharmaceutical composition comprising a phenylamidine derivative or a salt thereof, represented by a general formula, wherein R1 and R2 may be same or different, and represent an optionally substituted C3-4alkyl group; and one or more agents selected from azole antifungal agents, polyene antifungal agents, candin antifungal agents and fluoropyrimidine antifungal agents, and a method for combination use of the phenylamidine derivative or a salt thereof and the agents are useful for treating fungal infections caused by a fungal pathogen.
    Type: Grant
    Filed: October 3, 2007
    Date of Patent: May 8, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventor: Hiroshi Nishikawa
  • Publication number: 20120027680
    Abstract: The present invention relates to biodegradable biocompatible polyketals, methods for their preparation, and methods for treating animals by administration of biodegradable biocompatible polyketals. In one aspect, a method for forming the biodegradable biocompatible polyketals comprises combining a glycol-specific oxidizing agent with a polysaccharide to form an aldehyde intermediate, which is combined with a reducing agent to form the biodegradable biocompatible polyketal. The resultant biodegradable biocompatible polyketals can be chemically modified to incorporate additional hydrophilic moieties. A method for treating animals includes the administration of the biodegradable biocompatible polyketal in which biologically active compounds or diagnostic labels can be disposed. The present invention also relates to chiral polyketals, methods for their preparation, and methods for use in chromatographic applications, specifically in chiral separations.
    Type: Application
    Filed: July 28, 2011
    Publication date: February 2, 2012
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Mikhail I. Papisov, Alexander Yurkovetskiy
  • Publication number: 20110224423
    Abstract: The invented inositol and trehalose derivatives, prepared by introducing multiple units of the guanidine group to the backbone molecules, show excellent blood-brain barrier permeability, and accordingly, it can be easily transported to the brain tissues and utilized for the treatment of neurodegenerative diseases such as Alzheimer's disease and Huntington's disease.
    Type: Application
    Filed: March 23, 2009
    Publication date: September 15, 2011
    Inventors: Sung-Kee Chung, Woo Sirl Lee, Boram Kim, Jungkyun Im, Subhash C. Ghosh
  • Publication number: 20110223105
    Abstract: There is provided a compound of Formula and salts thereof wherein R1 is an imine or an alkylated imine, said imine or alkylated imine comprising a linear or branched alkyl group of length C1 to C5; R2 are each independently (a) an unsubstituted or substituted linear or branched alkyl group of chain length C1-7; (b) an aryl substituted alkyl group, wherein said aryl group is substituted, (c) an alkoxy substituted alkyl group, wherein said alkoxy group is substituted by a methoxy group or an alkoxy group substituted with an alkoxy group; or (d) an H atom; wherein said substituents in (a) and (b) are selected from hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, nitro, oxo and fluoro groups. R3 and R4 are linear or branched alkyl groups of length C1 to C6 constituting a ketal or a cyclic ketal. The compounds claimed may be used for the manufacture of a medicament.
    Type: Application
    Filed: September 1, 2009
    Publication date: September 15, 2011
    Inventors: Leif A. Eriksson, Lennart Löfgren
  • Publication number: 20110172306
    Abstract: The present invention describes a method for providing creatine to an animal, which includes receiving a creatine ester by the animal. The creatine ester is suitable for being modified by the animal to form creatine.
    Type: Application
    Filed: March 23, 2011
    Publication date: July 14, 2011
    Inventors: Jonathan L. Vennerstrom, Donald W. Miller
  • Patent number: 7939505
    Abstract: This disclosure provides a range of amino acid lipid compounds and compositions useful for drug delivery, therapeutics, and the diagnosis and treatment of diseases and conditions. The amino acid lipid compounds and compositions can be used for delivery of various agents such as nucleic acid therapeutics to cells, tissues, organs, and subjects.
    Type: Grant
    Filed: May 2, 2008
    Date of Patent: May 10, 2011
    Assignee: Marina Biotech, Inc.
    Inventors: Steven C. Quay, Michael Houston, Jr., Pierrot Harvie, Roger C. Adami, Renata Fam, Mary Gallagher Prieve, Kathy Lynn Fosnaugh, Shaguna Seth
  • Publication number: 20110092601
    Abstract: Polyamine, polyamine/guanidino, and polyamine/biguanide compounds bearing allene, propargyl, cyclopropyl, and other reactive moieties are disclosed. The compounds are useful as irreversible inhibitors of the enzyme lysine-specific demethylase-1 and for the treatment of cancer.
    Type: Application
    Filed: April 14, 2008
    Publication date: April 21, 2011
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Patrick M. Woster, Robert A. Casero
  • Publication number: 20100330136
    Abstract: This invention relates to a use of a composition for protecting oral cavity and teeth containing ethyl-N?-lauroyl-L-arginate HCl (LAE), a corresponding composition and a corresponding method for protecting teeth. Because of nearly epidemic incidence of dental erosion, there is a continuing need for improved products that provide protection against dental erosion. Hence, it is an object of the present invention to protect teeth against dental erosion. Surprisingly, it has been found that ethyl-N?-lauroyl-L-arginate HCl (LAE) and its salts attach to teeth and provide protection of teeth from erosion especially caused by the action of acid in food products and drinks such as chewing gum and lozenges compositions. Special advantages of this invention are: (a) sustained coating of the teeth by LAE and its homologues; (b) the coating agent provides a source of neutralizing plaque acids by providing sustained base formation.
    Type: Application
    Filed: February 11, 2009
    Publication date: December 30, 2010
    Inventor: Xavier Rocabayera Bonvila
  • Publication number: 20100330608
    Abstract: The inventive molecular transporter compound shows significantly high permeability through a biological membrane such as a plasma membrane, nuclear membrane and blood-brain barrier, and accordingly, can be effectively used in delivering various biologically active molecules.
    Type: Application
    Filed: August 20, 2010
    Publication date: December 30, 2010
    Applicants: Postech Foundation, Postech Academy-Industry Foundation
    Inventors: Sung-Kee Chung, Kaustabh Kumar Maiti, Woo Sirl Lee, Ock-Youm Jeon, Seok-Ho Lee
  • Publication number: 20100274029
    Abstract: Provided is a method of preparing a (6R)-3-hexyl-4-hydroxy-6-undecyl-5,6-dihydropyran-2-one, and a (5R)-2-hexyl-5-hydroxy-3-iminohexadecanoate derivative used in said method as an intermediate.
    Type: Application
    Filed: October 29, 2008
    Publication date: October 28, 2010
    Applicant: HANMI PHARM. CO., LTD.
    Inventors: Sang Min Yun, Young Ho Moon, Young-Kil Chang, Dong Jin Hong, Ji-Yeon Chang, Moon Sub Lee, Jaeho Yoo, Ji Sook Kim, Cheol Kyung Kim
  • Publication number: 20100184709
    Abstract: The present invention is based on the surprising finding of a proteolytic cleavage function of human Malt1. More particularly, the present invention relates to enzyme and screening assays, methods for assessing cleaving activity, methods for screening, isolated polypeptides, antibodies and inhibitors of Malt1. The present invention also relates to the use of Malt1 as a proteolytic enzyme and the use of compounds comprising a peptide comprising an amino acid sequence according to any one of SEQ ID NO: 1-47 as substrates susceptible for specific proteolytic cleavage.
    Type: Application
    Filed: May 30, 2008
    Publication date: July 22, 2010
    Applicant: UNIVERSITY OF LAUSANNE
    Inventors: Margot Thome, Fabien Rebeaud, Stephan Hailfinger
  • Publication number: 20100179106
    Abstract: Compositions and methods for treating mitochondrial disorders are provided. The compositions include compounds having a mitochondrial targeting moiety, for example a lipophilic cation. Certain compounds are effective for increasing the ratio of phosphocreatine/creatine in a host, for example a mammal. Other compounds decrease the ratio of phophocreatine/creating in a host. An exemplary compound is defined by the following structure (Formula Ia): wherein R1 is H or phosphate and the double bond is between N1 and C1 or between N2 and C1; R2 is a mitochondrial targeting moiety; R3 an alkyl, alkylaryl, alkylheteroaryl spacer group, a cleavable linker, or absent; R4 is H or an alkyl, aryl, or heteroaryl group; and R5 is alkyl, aryl, or heteroaryl; or N1 C1, and N together form a heterocyclic ring containing at least 5 atoms, wherein N1, N3, and R1-R5 are as defined above, or N3 and R5 together form a heterocyclic ring containing at least four atoms; or a pharmaceutically acceptable salt or prodrug thereof.
    Type: Application
    Filed: September 8, 2008
    Publication date: July 15, 2010
    Applicant: Gencia Corporation
    Inventor: Shaharyar Khan
  • Publication number: 20100173993
    Abstract: A controlled release biocidal salt of a first component comprises a cation of a N?—(C1-C22)alkanoyl di-basic amino acid alkyl(C1-C22)ester cationic biocidal molecule and a second component comprising an anion of a monomeric anionic molecule having insignificant biocidal activity. The salt is characterized such that when the salt is exposed to an aqueous medium, the salt partially dissolves thereby releasing biocidal ions in an amount sufficient to exceed the MIC or MBC of a target bacteria being controlled, and further characterized as leaving a residual reservoir of undissolved salt capable of releasing more biocidal ions as the salt is consumed or otherwise removed from the environment encompassing the target bacteria. The preferred cationic biocidal molecule comprises N?-lauroyl-L-arginine ethyl ester (“LAE”).
    Type: Application
    Filed: February 4, 2010
    Publication date: July 8, 2010
    Inventors: Anthony J. Sawyer, Richard F. Stockel
  • Patent number: 7732558
    Abstract: A dendritic compound of the following structure: PDn-Z-L is disclosed. In the structure above, P is X—(CH2CH2—O)r—, r is an integer ranging from 1000 to 4000, X is OH, NH2, or OR, R is C1 to C10alkyl, Dn is a residue of branched C3 to C30 polyol compounds, n is the quantity of layers of the residue of branched compounds and is an integer equal to or greater than 1, L is a metal cation, Z is the residue of a C3 to C30 compound with multi functional groups. The functional groups illustrated above can be carboxylic groups, amino groups, amide groups, or chelating groups. The carboxylic groups, ester groups, amino groups, or amide groups bind to Dn, and the chelating groups bind to the metal cations.
    Type: Grant
    Filed: December 27, 2005
    Date of Patent: June 8, 2010
    Assignee: Industrial Technology Research Institute
    Inventors: Abraham Josephk, Hui-Ju Cho, Yu-Hau Shih, Chao-Hung Kao, Huang-Chien Liang
  • Publication number: 20090312419
    Abstract: Disclosed are creatine ?-alaninate, compositions and formulations containing same, and methods of use therefor.
    Type: Application
    Filed: August 21, 2009
    Publication date: December 17, 2009
    Inventor: Bruce W. Kneller
  • Publication number: 20090137669
    Abstract: The present invention provides a creatine ester anti-inflammatory compound which may be received by animals and then metabolized into a biologically active form of creatine. The biologically active creatine inhibits the production of chemical mediators, released during an inflammatory response, which are important components in the inflammatory response and the inflammation and pain resulting from physical or chemical trauma to cells and tissue.
    Type: Application
    Filed: December 13, 2007
    Publication date: May 28, 2009
    Inventors: Donald W. Miller, Samuel C. Augustine, Jon C. Wagner, Thomas L. McDonald, Dennis H. Robinson
  • Patent number: 7527733
    Abstract: The present invention provides for Troika acids attached to a macroporous resin and Methods of preparing the same, including direct attachment of a Troika acid, and attachment of a Troika acid precursor followed by generation of the Troika acid in situ. Methods of functionalizing a resin to facilitate attachment are also described. Multiple Troika acids, comprising a pair of Troika acids joined together are described. Synthetic routes to both microporous and macroporous resins modified by introduction of a suitable Troika-type acid have been designed and validated. In a preferred embodiment, a macroporous Troika resin removes Cu2+ and Ni2+ from aqueous solution with high affinity, and is selective against Mg2+ or Ca2+. The materials of the present invention have advantages for metal removal from power plant waste water.
    Type: Grant
    Filed: September 30, 2004
    Date of Patent: May 5, 2009
    Assignee: The University of Southern California
    Inventors: Charles E. McKenna, Boris A Kashemirov, Isabelle Favier, Thomas D. Wolfe
  • Patent number: 7449446
    Abstract: There is provided a combination product comprising; (A) melagatran or a pharmaceutically acceptable derivative thereof; and (B) dexamethasone or a pharmaceutically acceptable derivative there of, wherein each of components (A) and (B) is formulated in admixture with a pharmaceutically-acceptable adjuvant, diluent or carrier, as well as the use of such a combination product in the treatment of conditions including disseminated intravascular coagulation.
    Type: Grant
    Filed: October 24, 2002
    Date of Patent: November 11, 2008
    Assignee: AstraZeneca AB
    Inventor: Margareta Elg
  • Publication number: 20080103202
    Abstract: This invention discloses the method of preparation of creatine ester-salts. Creatine is an extremely popular ergogenic aid, and is found most often in the form of creatine monohydrate. Creatine monohydrate is poorly soluble in water however and while esters gain solubility, there functionality is greatly decreased. The material can be administered in a variety of ways including capsules, tablets, powdered beverages, bars, gels, liquids, liposomes or drinks.
    Type: Application
    Filed: November 8, 2004
    Publication date: May 1, 2008
    Inventors: Chris Ferguson, Jiang Shengli
  • Patent number: 7354905
    Abstract: There is provided compounds of formula I, R1O(O)C—CH2—(R)Cgl-Aze-Pab-R2I wherein R1 and R2 have meanings given in the description, which are useful as prodrugs of inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (eg thrombosis) or as anticoagulants.
    Type: Grant
    Filed: February 12, 2004
    Date of Patent: April 8, 2008
    Assignee: AstraZeneca AB
    Inventors: Thomas Antonsson, David Gustafsson, Kurt-Jürgen Hoffmann, Jan-Erik Nyström, Henrik Sörensen, Mikael Sellén
  • Patent number: 7223745
    Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.
    Type: Grant
    Filed: August 12, 2004
    Date of Patent: May 29, 2007
    Assignee: Cephalon, Inc.
    Inventors: Sankar Chatterjee, Mohamed Iqbal, Ernesto Menta, Ambrogio Oliva
  • Patent number: 7135587
    Abstract: Novel urea and urethane derivatives of general formula (I) in which R1, R2, R3, R5, R5?, X, Y, B, m, n and o are as defined in Patent Claim 1, and physiologically acceptable salts or solvates thereof are integrin inhibitors and can be employed for combating thromboses, cardiac infarction, coronary heart disease, arteriosclerosis, inflammation, tumors. Osteoporosis, infections and restenosis after angioplasty or in pathological processes maintained or propagated by antiogenesis.
    Type: Grant
    Filed: November 30, 2001
    Date of Patent: November 14, 2006
    Assignee: Merck Patent GmbH
    Inventors: Wolfgang Staehle, Alfred Jonczyk, Oliver Schadt, Simon Goodman
  • Patent number: 7015348
    Abstract: To provide a producing method of an optically active ?-amino acid useful as intermediate for the production of medicines, agricultural chemicals and physiologically active substances, by means of a catalytic and asymmetric synthesis method of high performance and a high enantiomeric excess, without requiring additional procedures such as introduction and removal of protecting group and so on. A producing method of an optically active ?-amino acids which comprises subjecting an enamine to an asymmetric hydrogenation.
    Type: Grant
    Filed: July 29, 2003
    Date of Patent: March 21, 2006
    Assignee: Takasago International Corporation
    Inventors: Kazuhiko Matsumura, Xiaoyong Zhang, Takao Saito
  • Patent number: 6962905
    Abstract: A kit of parts containing (a) a pharmaceutical formulation including a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, and (b) a pharmaceutical formulation including a prodrug of a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative of that prodrug, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier. Components (a) and (b) are each provided in a form that is suitable for administration in conjunction with the other. The kit is useful in the treatment of conditions in which inhibition of thrombin is required or desired.
    Type: Grant
    Filed: April 19, 2000
    Date of Patent: November 8, 2005
    Assignee: AstraZeneca AB
    Inventor: David Gustafsson
  • Patent number: 6960588
    Abstract: Compounds of formula (I) in which M, B1, B2, B3, B4, B5, B6, A1, A2, A3, A4, A5, A6, K1 and K2 have the meanings as indicated in the description, are novel effective tryptase inhibitors.
    Type: Grant
    Filed: September 12, 2000
    Date of Patent: November 1, 2005
    Assignee: Altana Pharma AG
    Inventor: Thomas Martin
  • Patent number: 6919449
    Abstract: The present invention relates to a method for the preparation of cephalosporin antibiotic of the formula (II), which comprises hydrolyzing and halogenating the ester of formula (III) by photochemical irradiation in one pot using a halogenating agent in the absence or presence of a solvent, to produce compound of formula (I), activating the 4-halogeno-2-substitutedimino-3-oxo-butyric acid of formula (I) using conventional activation agents gives compound of formula (IV), condensing the activated compound of the formula (IV) with 7-amino cephem derivative of the formula (V) to produce a compound of formula (VI), and cyclizing the compound of formula (VI) with thiourea to give cephalosporin compounds of the formula (II).
    Type: Grant
    Filed: September 18, 2002
    Date of Patent: July 19, 2005
    Assignee: Orchid Chemicals and Pharmaceuticals Limited
    Inventors: Pandurang Balwant Deshpande, Parven Kumar Luthra, Pratik Ramesh Sathe, Sivakumaran Sundaravadivelan, Praveen Nagesh Ganesh
  • Patent number: 6888022
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: May 3, 2005
    Assignees: Athena Neurosciences, Inc., Eli Lilly & Company
    Inventors: James E. Audia, Thomas C. Britton, James J. Droste, Beverly K. Folmer, George W. Huffman, Varghese John, Lee H. Latimer, Thomas E. Mabry, Jeffrey S. Nissen, Warren J. Porter, Jon K. Reel, Eugene D. Thorsett, Jay S. Tung, Jing Wu, Clark Norman Eid, William Leonard Scott
  • Publication number: 20040186060
    Abstract: The present invention provides matriptase inhibitors and compositions thereof useful for treating cancer. Martripase is a trypsin-like serine protease active in the development of cancerous conditions, such as tumors and metastasis of cancer.
    Type: Application
    Filed: December 18, 2003
    Publication date: September 23, 2004
    Applicant: Dendreon Corporation
    Inventors: David F. Duncan, L. Josue Alfaro-Lopez, Mallareddy Komandla, Odile Esther Levy, Ofir Moreno, Joseph E. Semple, Amir P. Tamiz
  • Patent number: 6784311
    Abstract: Process for the preparation of 3-aminoalkanoic acid esters of the general formula: in which R is C1-6-alkyl and R1 is hydrogen, C1-6-alkyl or phenyl, or their salts, by catalytic hydrogenation of the corresponding 3-amino-2-alkenoic acid esters of the general formula: in which R and R1 have the above mentioned meanings. The hydrogenation is carried out in the presence of a strong acid and the salt of the 3-aminoalkanoic acid ester (I) and the strong acid formed is optionally converted into the free 3-aminoalkanoic acid ester (I) or into another salt in a manner known per se.
    Type: Grant
    Filed: August 21, 2002
    Date of Patent: August 31, 2004
    Assignee: Lonza AG
    Inventor: Rudolf Fuchs
  • Publication number: 20040127426
    Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Application
    Filed: June 24, 2003
    Publication date: July 1, 2004
    Applicant: AXYS PHARMACEUTICALS, INC.
    Inventors: Michael Graupe, John O. Link
  • Publication number: 20040024224
    Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.
    Type: Application
    Filed: May 15, 2003
    Publication date: February 5, 2004
    Applicant: Genzyme Corporation
    Inventors: Mukund S. Chorghade, Mukund K. Gurjar, Debendra K. Mohapatra
  • Patent number: 6660246
    Abstract: Novel compounds of the formula and novel complexes of these compounds with metals are useful in diagnostic and therapeutic methods.
    Type: Grant
    Filed: August 9, 1996
    Date of Patent: December 9, 2003
    Assignee: Bracco International, BV
    Inventors: David P. Nowotnik, Palaniappa Nanjappan
  • Patent number: 6608196
    Abstract: Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: August 19, 2003
    Assignee: Galileo Pharmaceuticals, Inc.
    Inventors: Bing Wang, Satyanarayana Janagani, Wyeth B. Callaway, Jonathan L. Sessler
  • Patent number: 6605688
    Abstract: This invention concerns low viscosity aldimine and ketimine reactive diluents having multi-imine functionality, which are useful in automotive refinish coating compositions, including a process for making them and the coatings that contain them.
    Type: Grant
    Filed: November 9, 2001
    Date of Patent: August 12, 2003
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Marko Strukelj
  • Publication number: 20030060653
    Abstract: The invention relates to N-unsubstituted imidic ester alkyl sulphates, N-unsubstituted amidinium alkyl sulphates and a process for their preparation, which is characterized in that carboxamides are converted with sulphuric diesters into the corresponding imidic ester alkyl sulphates, which are reacted further with ammonia to give the analogous amidinium alkyl sulphates.
    Type: Application
    Filed: August 27, 2002
    Publication date: March 27, 2003
    Inventors: Helmut Kraus, Rosemarie Wodarsch
  • Publication number: 20030050251
    Abstract: The present invention provides compounds which inhibit serine protease activity of matriptase or MTSP1. Also provided are pharmaceutical compositions comprising those compounds and methods of using the compounds and pharmaceutical compositions to treat conditions ameliorated by inhibition of matriptase or MTSP1.
    Type: Application
    Filed: March 5, 2002
    Publication date: March 13, 2003
    Inventors: Joseph E. Semple, Gary S. Coombs, John E. Reiner, Edgar O. Ong, Gian Luca Araldi
  • Publication number: 20030013657
    Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.
    Type: Application
    Filed: May 3, 2002
    Publication date: January 16, 2003
    Inventors: Bing Wang, Guy Miller, Satyanarayana Janagani
  • Publication number: 20020198141
    Abstract: A molecular conjugate is provided having the formula: 1
    Type: Application
    Filed: March 25, 2002
    Publication date: December 26, 2002
    Inventors: James D. McChesney, Madhavi C. Chander, Teruna J. Siahaan, Christine R. Xu
  • Patent number: 6482974
    Abstract: Processes for the preparation of pyrrolidones (7 and 8) and pyrrolidines (9 and 10) from tri-O-acetyl-D-erythro-4-pentulosonic acid esters are described. The compounds are aza sugar analogs of D-ribofuranoside and are intermediates to drugs which regulate nucleoside and nucleic acid synthesis.
    Type: Grant
    Filed: September 4, 2001
    Date of Patent: November 19, 2002
    Assignee: Board of Trustees of Michigan State University
    Inventor: Rawle I. Hollingsworth