Alkyl, Hydroxyalkyl, Alkoxyalkyl, Or Alkanoyloxyakyl Bonded Directly To 3-position Patents (Class 514/209)
  • Patent number: 9828622
    Abstract: The present invention provides photosensitizer compounds for use in detecting beta-lactamase activity. Methods and kits that utilize the photosensitizer compounds of the invention for the detection of, quantitation of, and classification or typing of microbial beta-lactamases.
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: November 28, 2017
    Assignee: The General Hospital Corporation
    Inventors: Tayyaba Hasan, Ulysses W. Sallum, Sarika Verma, Gerard Nau
  • Patent number: 9303021
    Abstract: Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas 1 and 2 wherein the variables have the meaning disclosed in the specification.
    Type: Grant
    Filed: March 18, 2014
    Date of Patent: April 5, 2016
    Assignee: Allergan, Inc.
    Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
  • Patent number: 8933016
    Abstract: It is an object of the present invention to provide antimicrobial metallodrugs comprising an antimicrobial peptide (“AMP”) and/or an antibiotic covalently bound to a metal binding moiety. These metallodrugs combine a metal binding domain which typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, with a member of a diverse class of antimicrobial agents currently validated in preclinical and clinical settings for the treatment of a broad spectrum of pathogenic organisms.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: January 13, 2015
    Assignee: MetalloPharm, LLC
    Inventors: James A. Cowan, Ada S. Cowan
  • Publication number: 20150011524
    Abstract: Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.
    Type: Application
    Filed: September 19, 2014
    Publication date: January 8, 2015
    Inventors: Larry SUTTON, Sophia YU
  • Publication number: 20140378415
    Abstract: The present invention provides compounds of formula (I) wherein P is P0, heterocyclyl or heterocyclyl substituted by one to five Z formula (II); Y1, Y2, Y3 and Y4 are independently of each other C—H, C—R5, or nitrogen; G1 is oxygen or sulfur; X4 is C1-C8 haloalkyl; R4 is aryl or aryl substituted by one to five R9, or heteroaryl or heteroaryl substituted by one to five R9; and R1, R2, R4, R5, R9 and Z are as defined in the claims. The invention also provides compositions comprising the compounds of formula (I), intermediates useful in the preparation of compounds of formula (I) and methods of using the compounds of formula (I) to control insects, acarines, nematodes or molluscs.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi
  • Patent number: 8901293
    Abstract: New monobactam antibiotics compounds which contain an 3-amino-azetidin-2-one ring and are active against gram-negative bacteria, wherein the compounds include the compound 2-(2-amino-thiazol-4-yl)-2-[(Z)-(1H,4H-1,5-dihydroxy-4-oxo-pyridin-2-yl)methoxyimino]-N-[3(S)-1-oxysulfonyl-2,2-dimethyl-4-oxo-azetidin-3-yl]acetamide.
    Type: Grant
    Filed: December 7, 2006
    Date of Patent: December 2, 2014
    Assignee: Basilea Pharmaceutica AG
    Inventors: Eric Desarbre, Bérangére Gaucher, Malcolm G. P. Page, Patrick Roussel
  • Publication number: 20140286876
    Abstract: The present invention, as described above and as further defined by the claims, provides methods of administering an active agent via adhesion of a film to a mucous membrane in the oral cavity of a mammal, as well as and ODF formed therefore. An active agent may be ingested as the ODF dissolves resulting in systemic treatment of the mammal. In additional embodiments, an ODF may provide topical administration of an active agent.
    Type: Application
    Filed: March 28, 2014
    Publication date: September 25, 2014
    Inventor: Andrew L. Skigen
  • Patent number: 8796458
    Abstract: The invention relates to 6-cyclohexylamine-substituted isoquinolone derivatives of the formula (I) or isoquinoline derivatives of the formula (I?) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: August 5, 2014
    Assignee: Sanofi
    Inventors: Oliver Plettenburg, Armin Hofmeister, Dieter Kadereit, Joachim Brendel, Matthias Loehn, Jean-Michel Altenburger
  • Publication number: 20140206606
    Abstract: The present invention provides compounds of formula (I), wherein G1 is oxygen; R1 is hydrogen; R2 is group P (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y1 is C—R6, CH or nitrogen; Y2 and Y3 are independently CH or nitrogen; wherein no more than two of Y1, Y2 and Y3 are nitrogen and wherein Y2 and Y3 are not both nitrogen; R5 is hydrogen, halogen, cyano, nitro, NH2, C1-C2alkyl, C1-C2haloalkyl, C3-C5cycloalkyl, C3-C5halocycloalkyl, C1-C2alkoxy, C1-C2haloalkoxy; R6 together with R5 forms a —CH?CH—CH?CH— bridge; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl.
    Type: Application
    Filed: August 24, 2012
    Publication date: July 24, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Publication number: 20140206633
    Abstract: The present invention relates to processes for the preparation of compounds of formula IB wherein A1, A2, A3, A4, L, Y1, Y2, R1, R2, R3, R4 and R5 are as defined in the claims, comprising reacting a compound of formula (II) wherein Y1, Y2, L, A1, A2, R1, R2, R3, R4 and R5 are as defined for the compound of formula (I); with hydroxylamine in the presence of water, a base and a chiral phase transfer catalyst, which chiral phase transfer catalyst is a quinine derivative. The invention also relates to compounds of formula IB and enantiomerically enriched mixtures comprising compounds of formula IB.
    Type: Application
    Filed: February 3, 2011
    Publication date: July 24, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Nicholas Phillip Mulholland, Edouard Godineau, Jérôme Yves Cassayre, Peter Renold, Myriem El Qacemi, Guillaume Revol
  • Publication number: 20140194376
    Abstract: The present invention provides compounds of formula (I) wherein G1 is oxygen; R1 is hydrogen; R2 is group (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—; R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y2 and Y3 are independently CH or nitrogen, wherein Y2 and Y3 are not both nitrogen; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl. The invention also provides intermediates useful for the preparation of compounds of formula (I), as well as methods of controlling insects, acarines, nematodes or molluscs using the compounds of formula (I).
    Type: Application
    Filed: August 24, 2012
    Publication date: July 10, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Publication number: 20140105884
    Abstract: Disclosed herein are materials, means and methods for sustained release of therapeutic agents for topical treatments. In particular, disclosed are means and methods for topical treatment of diseases of internal body cavities by embedding therapeutic agents in a slowly degrading biocompatible mixture applied to affected tissue.
    Type: Application
    Filed: October 15, 2013
    Publication date: April 17, 2014
    Applicant: THERACOAT LTD.
    Inventors: Marina Konorty, Gil Hakim
  • Publication number: 20140107056
    Abstract: The present invention provides compounds of formula (I): wherein A1, A2, A3 and A4 are independently of one another C—H, C—R5, or nitrogen; B1—B2—B3—B4 is —CH2—C?N—CH2—, —CH2—N—CH2—CH2—, —CH2—C?CH-0- or —CH?C—CH2-0-; G1 is oxygen or sulfur; L is a single bond or C1-C8alkylene; R1 is hydrogen, C1-C8alkyl, C1-C8alkylcarbonyl-, C1-C8alkoxy, C2-C8alkenyl, C2-C8alkynyl, C1-C8alkoxy-C1-C8alkyl, aryl or aryl substituted by one to three R6, or R1 is heterocyclyl or heterocyclyl substituted by one to three R6 or C1-C8alkoxycarbonyl-; R2 is hydrogen, C1-C8haloalkyl or C1-C8alkyl; R3 is C1-C8haloalkyl; R4 is aryl or aryl substituted by one to three R6, or R4 is heterocyclyl or heterocyclyl substituted by one to three R6; Y1 is CR7R8, C?O or C?S; Y2, Y3 and Y4 are independently CR7R8, C=0, C?S, N—R9, O, S, SO or SO2; wherein at least two adjacent ring atoms in the ring formed by Y1, Y2, Y3 and Y4 are heteroatoms; each R7 and R8 is independently hydrogen, halogen, C1-C8alkyl, or C1-C8haloalkyl; and R5, R6, R7, R8 and R9 a
    Type: Application
    Filed: May 30, 2012
    Publication date: April 17, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Publication number: 20140047569
    Abstract: The present invention relates to methods of treatment of clinical disorders associated with protein aggregation comprising administering, to a subject, an effective amount of an anti-protein aggregate (“APA”) compound selected from the group consisting of pimozide, fluphenazine (e.g., fluphenazine hydrochloride), tamoxifen (e.g., tamoxifen citrate), taxol, cantharidin, cantharidic acid, salts thereof and their structurally related compounds. It is based, at least in part, on the discovery that each of the aforelisted compounds were able to promote degradation of aggregated ATZ protein in a Caenorhabditis elegans model system. According to the invention, treatment with one or more of these APA compounds may be used to ameliorate the symptoms and signs of AT deficiency as well as other disorders marked by protein aggregation, including, but not limited to, Alzheimer's Disease, Parkinson's Disease, and Huntington's Disease.
    Type: Application
    Filed: May 3, 2012
    Publication date: February 13, 2014
    Applicant: University of Pittsburgh - of the Commonwealth System of Higher Education
    Inventors: Stephen C. Pak, David Hirsch Perlmutter, Gary A. Silverman
  • Publication number: 20130251790
    Abstract: The present invention provides a pharmaceutical composition comprising a low dose of zanamivir and a process for preparing the pharmaceutical composition comprising a low dose of zanamivir. The pharmaceutical composition comprising a low dose zanamivir may be used in the treatment and/or prophylaxis of influenza. The present invention also provides a method of treatment and/or prophylaxis of influenza which comprises administering a dry powder inhaler composition comprising a low dose zanamivir. The pharmaceutical composition of the present invention comprises zanamivir and one or more pharmaceutically acceptable excipients, wherein the total daily dose of the zanamivir is less than 10 mg, preferably for administration at least once a day, and preferably wherein the composition delivers from 3 mg to 8 mg of zanamivir per administered dose.
    Type: Application
    Filed: September 26, 2011
    Publication date: September 26, 2013
    Applicant: CIPLA LIMITED
    Inventors: Geena Malhotra, Shrinivas Madhukar Purandare
  • Publication number: 20130217659
    Abstract: Cefodroxil monohydrate is formed by a processing which includes a) bringing an aqueous solution of cefadroxil monohydrate to a pH of between 7 to 9 with a suitable titrant; b) lowering the pH to a value of between 5 and 6.5 to obtain a suspension of cefadroxil monohydrate in crystal form; and c) isolating the cefadroxil monohydrate in crystal form from the suspension obtained in step b). The cefadroxil monohydrate thereby obtained exhibits a CIE b value of below 6, and advantageously a CIE b value of below 12 when stored at a temperature of 25° C. for at least 1 month.
    Type: Application
    Filed: March 18, 2013
    Publication date: August 22, 2013
    Applicant: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.
    Inventors: Carlos Enrique LENHARD, Harold Monro MOODY, Theodorus Johannes Godfried Maria VAN DOOREN
  • Publication number: 20130210705
    Abstract: It is an object of the present invention to provide antimicrobial metallodrugs comprising an antimicrobial peptide (“AMP”) and/or an antibiotic covalently bound to a metal binding moiety. These metallodrugs combine a metal binding domain which typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, with a member of a diverse class of antimicrobial agents currently validated in preclinical and clinical settings for the treatment of a broad spectrum of pathogenic organisms.
    Type: Application
    Filed: January 18, 2013
    Publication date: August 15, 2013
    Applicant: METALLOPHARM LLC
    Inventor: Metallopharm LLC
  • Publication number: 20130203726
    Abstract: The present invention relates to the use of inhibitors of FtsZ, an ancestral tubulin of prokaryotes, to restore susceptibility to ?-lactam antibiotics, including carbapenems and cephalosporins, particularly in methicillin-resistant Staphylococcus aureus (MRSA), methicillin-resistant Staphyloccus epidermis (MRSE), and other coagulase negative staphylococci (MRCNS).
    Type: Application
    Filed: March 4, 2011
    Publication date: August 8, 2013
    Inventors: Terry Roemer, Sang Ho Lee, Lisa Wang Jarantow
  • Patent number: 8497260
    Abstract: 2-arylbenzothiophene derivatives or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition for the diagnosis or treatment of degenerative brain disease containing the same as an active ingredient. Since the 2-arylbenzothiophene derivatives of Formula 1 have a relatively high binding affinity for ?-amyloid, they can be used as diagnostic reagents for diagnosing Alzheimer's disease at an early stage by non-invasive techniques when they are labeled with radioisotopes: wherein R1-R4, V, W, X, Y and Z are as defined in the Detailed Descript of the specification. Further, when the pharmaceutical composition containing the 2-arylbenzothiophene derivative binds with a low-molecular weight ?-amyloid peptide binding compound, generation of malignant high-molecular weight ?-amyloid deposits is minimized. Accordingly, the pharmaceutical composition can be used as a therapeutic agent of degenerative brain disease such as Alzheimer's disease.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: July 30, 2013
    Assignee: Industry-University Cooperation Foundation Sogang University
    Inventors: Dae Yoon Chi, Byoung Se Lee, Youjung Jung, Uthaiwan Sirion, Yoo Jin Lim, Yu Jin Bae, Heejun Kim, So Young Chu, Dae Hyuk Moon, Jin-Sook Ryu, Jae Seung Kim, Seung Jun Oh
  • Publication number: 20130131032
    Abstract: A method for improving sexual function is described. A mammal suffering from sexual dysfunction or otherwise in need of enhanced sexual function is administered a compound selected from those that are capable of inhibiting the activity of ?-lactams, penicillin-binding protein, carboxypeptidase. Such compounds, including particularly ?-lactam ring-containing compounds, can be used to formulate pharmaceutical formulations useful for improving sexual function.
    Type: Application
    Filed: January 25, 2013
    Publication date: May 23, 2013
    Applicant: Revaax Pharmaceuticals, LLC
    Inventor: Revaax Pharmaceuticals, LLC
  • Publication number: 20130053336
    Abstract: The invention relates to a method for treating infections of bacteria of the Chlamydiaceae family using a ?-lactam. The invention also relates to a method for treating diseases caused by an infection of bacteria of the Chlamydiaceae family using a ?-lactam.
    Type: Application
    Filed: January 13, 2011
    Publication date: February 28, 2013
    Inventors: Philippe Verbeke, Maud Dumoux, Colette Kanellopoulos
  • Publication number: 20130024953
    Abstract: The present invention relates to methods of treatment of clinical disorders associated with protein aggregation comprising administering, to a subject, an effective amount of an anti-protein aggregate (“APA”) compound selected from the group consisting of pimozide, fluphenazine (e.g., fluphenazine hydrochloride), tamoxifen (e.g., tamoxifen citrate), taxol, cantharidin, cantharidic acid, salts thereof and their structurally related compounds. It is based, at least in part, on the discovery that each of the aforelisted compounds were able to promote degradation of aggregated ATZ protein in a Caenorhabditis elegans model system. According to the invention, treatment with one or more of these APA compounds may be used to ameliorate the symptoms and signs of AT deficiency as well as other disorders marked by protein aggregation, including, but not limited to, Alzheimer's Disease, Parkinson's Disease, and Huntington's Disease.
    Type: Application
    Filed: May 3, 2012
    Publication date: January 24, 2013
    Applicant: University of Pittsburgh - of the Commonwealth System of Higher Education
    Inventors: Stephen C. Pak, David Hirsch Perlmutter, Gary A. Silverman
  • Publication number: 20120329770
    Abstract: The present invention relates to cephalosporin derivatives having ?-lactamase inhibitory activity. The compounds are useful in preventing or treating bacterial resistance to an antibiotic, e.g. a ?-lactam antibiotic. Disclosed herein are compounds that are inhibitors of class B metallo-?-lactamases, as well as class A, C, and D serine ?-lactamases. In some preferred embodiments, the compounds are 3?-thiobenzoate derivatives of a cephalosporin. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the compounds are also disclosed.
    Type: Application
    Filed: February 25, 2011
    Publication date: December 27, 2012
    Inventors: Gary Igor Dmitrienko, Ahmad Ghavami, Valerie Joy Goodfellow, Jarrod W. Johnson, Anthony Paul Krismanich, Laura Marrone, Thammaiah Viswanatha, Sundaramma Viswanatha
  • Publication number: 20120316124
    Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: February 17, 2011
    Publication date: December 13, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
  • Publication number: 20120172292
    Abstract: This invention discloses a method for enhancing the efficacy of antimicrobial, anti-protozoa and anti-cancer treatments by co-administering an inhibitor of endogenous NO production and/or NO scavenger.
    Type: Application
    Filed: September 10, 2010
    Publication date: July 5, 2012
    Applicant: NEW YORK UNIVERSITY
    Inventors: Evgeny A. Nudler, Ivan Gusarov
  • Publication number: 20120107400
    Abstract: A pH dependent drug delivery system comprising a pH sensitive graft copolymer, a therapeutically active agent and other pharmaceutically acceptable ingredients. More specifically, a composition which is capable of suppressing the drug release in the acidic pH prevalent in the stomach and releasing the drug over an extended period of time at pH prevalent in the intestinal region.
    Type: Application
    Filed: March 5, 2010
    Publication date: May 3, 2012
    Inventors: Ramesh Muthusamy, Mohan Gopalkrishna Kulkarni
  • Publication number: 20110311628
    Abstract: A pulsatile release composition which releases the content rapidly after a predetermined lag time comprising a drug containing a core, coated with a pH sensitive graft copolymer. The coating suppresses the drug release at acidic pH prevalent in the stomach and releases it either immediately or after a lag time in the intestinal region. Combinations of multiple numbers of coated and uncoated units provide a sequential pulsatile release of same or different therapeutic agents.
    Type: Application
    Filed: March 8, 2010
    Publication date: December 22, 2011
    Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
    Inventors: Ramesh Muthusamy, Mohan Gopalkrishna Kulkarni
  • Publication number: 20110294774
    Abstract: The present invention provides a pharmaceutical composition useful for treating bacterial infections in humans and animals which comprises administering to a human or animal in need thereof, an antibacterially effective combination of a ?-lactam antibiotic and an inhibitor of any bacterial peptidoglycan biosynthesis enzyme, especially GlmU, GlmU, MurA, MurB, MurC, MurD, MurE, MurF, MurG, MraY, and UppS.
    Type: Application
    Filed: May 6, 2011
    Publication date: December 1, 2011
    Applicant: TRIUS THERAPEUTICS
    Inventors: Vickie Brown-Driver, Kedar GC, John M. Finn, Robert Haselbeck, Mark Hilgers, Karen Shaw, Mark Stidham
  • Publication number: 20110275558
    Abstract: The present invention relates to the field of medical treatments for diseases and disorders. More specifically, the present invention relates to the use of the lanthionine synthetase component C-like (LANCL) proteins as therapeutic targets for novel classes of anti-inflammatory, immune regulatory and antidiabetic drugs.
    Type: Application
    Filed: May 4, 2011
    Publication date: November 10, 2011
    Applicant: Virginia Tech Intellectual Properties, Inc.
    Inventors: Josep BASSAGANYA-RIERA, Pinyi LU, Raquel HONTECILLAS
  • Publication number: 20110171232
    Abstract: Disclosed is a method of diagnosing autoimmune diseases, such as multiple sclerosis and systemic lupus erythematosus, which involves detecting the presence of small intestinal bacterial overgrowth (SIBO) in a human subject having at least one symptom associated with a suspected diagnosis an autoimmune disease. Also disclosed is a method of treating these autoimmune diseases, which involves at least partially eradicating a SIBO condition in the human subject. The method includes administration of antimicrobial or probiotic agents, or normalizing intestinal motility by employing a prokinetic agent. Also disclosed is a kit for the diagnosis or treatment of autoimmune diseases.
    Type: Application
    Filed: March 28, 2011
    Publication date: July 14, 2011
    Applicant: CEDARS-SINAI MEDICAL CENTER
    Inventors: Henry C. Lin, Mark Pimentel
  • Publication number: 20110112059
    Abstract: The present invention provides photosensitizer compounds for use in detecting beta-lactamase activity. Methods and kits that utilize the photosensitizer compounds of the invention for the detection of, quantitation of, and classification or typing of microbial beta-lactamases.
    Type: Application
    Filed: May 5, 2009
    Publication date: May 12, 2011
    Applicant: The General Hospital Corporation
    Inventors: Tayyaba Hasan, Ulysses W. Sallum, Sarika Verma
  • Patent number: 7723389
    Abstract: The invention provides pharmaceutical compositions for the treatment or prevention of the toxic effects of therapeutic agents and methods of treating or preventing such toxicity using a toxicity reducing amount of N-acetylcysteine either alone or in combination with a therapeutically effective amount or, to achieve its therapeutic advantages, an amount larger than what is customarily given as a therapeutically effective amount, of a therapeutic agent.
    Type: Grant
    Filed: November 4, 2002
    Date of Patent: May 25, 2010
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Leonard A. Herzenberg, Leonore A. Herzenberg, Stephen C. De Rosa, James Andrus
  • Publication number: 20100056478
    Abstract: A pharmaceutically composition, comprising a combination of an antibiotically active compound of the formula (I): with a ?-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another ?-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI).
    Type: Application
    Filed: December 7, 2006
    Publication date: March 4, 2010
    Inventors: Eric Desarbre, Bérangère Gaucher, Malcolm G.P. Page, Patrick Roussel
  • Publication number: 20090306036
    Abstract: The invention provides methods of screening agents, conjugates or conjugate moieties, linked or linkable to agents, for capacity to be transported as substrates through the PEPT2 transporter. The invention also provides methods of treatment involving delivery of agents that either alone, or as a result of linkage to a conjugate moiety, are substrates of the PEPT2 transporter. The invention also provides conjugates comprising a pharmaceutical agent which is linked to a conjugate moiety that is a substrate for a PEPT2 transporter.
    Type: Application
    Filed: February 20, 2009
    Publication date: December 10, 2009
    Applicant: XenoPort, Inc.
    Inventors: Noa Zerangue, Tracy Dias, William J. Dower
  • Publication number: 20090143335
    Abstract: The present invention relates to a pharmaceutical composition comprising gaboxadol or a pharmaceutically acceptable salt thereof and one or more inhibitors of PAT1 and/or one or more inhibitors of OAT. The present invention further relates to a pharmaceutical composition comprising from about 0.5 mg to about 50 mg gaboxadol or a pharmaceutically acceptable salt thereof, wherein the composition provides an in vivo plasma profile comprising a mean Tmax which is longer than about 20 minutes.
    Type: Application
    Filed: October 17, 2008
    Publication date: June 4, 2009
    Applicant: H. LUNDBECK A/S
    Inventors: Mie Larsen, Carsten Uhd Nielsen, Birger Brodin Larsen, Rene Holm
  • Patent number: 7476650
    Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include an electron withdrawing group adjacent to the ring functionality, and the peptide include at least three peptide units. Among other therapeutic utilities, the peptide-based compounds exhibit anti-inflammatory and inhibition of cell proliferation, involving therapeutic applications for these compounds.
    Type: Grant
    Filed: June 17, 2004
    Date of Patent: January 13, 2009
    Assignee: Yale University
    Inventors: Craig M. Crews, Mikael Elofsson, Ute Splittgerber, Kyung Bo Kim
  • Publication number: 20080312203
    Abstract: The present invention provides a compound of formula I wherein one of A and B is hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X is O, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
    Type: Application
    Filed: August 21, 2008
    Publication date: December 18, 2008
    Applicant: Wyeth
    Inventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo Dos Santos, Fuk-Wah Sum, Yang-I Lin
  • Patent number: 7185647
    Abstract: Disclosed are methods for determining the smoothness index of the interior of a metered dose container.
    Type: Grant
    Filed: July 31, 2003
    Date of Patent: March 6, 2007
    Assignee: Schering Corporation
    Inventors: Stefan A. Sharpe, Slavka Libovicova-Tarzian, Joel A. Sequeira
  • Patent number: 7094431
    Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.
    Type: Grant
    Filed: September 30, 2003
    Date of Patent: August 22, 2006
    Inventor: Mickey L. Peshoff
  • Patent number: 6906054
    Abstract: The invention provides pharmaceutical compositions comprising compounds of formula I and IV: wherein R1-R11 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts. The pharmaceutical compositions are useful for inhibiting ?-lactamase enzymes, for enhancing the activity of ?-lactam antibiotics, and for treating ?-lactam resistant bacterial infections in a mammal.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: June 14, 2005
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, A. Srinivasa Rao, Greg C. Adam, Sirishkumar D. Nidamarthy, Venkata Ramana Doppalapudi
  • Patent number: 6831099
    Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like and PGPH activities of the 20S proteasome can be selectively inhibited with the inventive compounds. The peptide-based compounds include an electron withdrawing group adjacent to the ring functionality, and the peptide include at least three peptide units. Among other therapeutic utilities, the peptide-based compounds exhibit anti-inflammatory and inhibition of cell proliferation, involving therapeutic applications for these compounds.
    Type: Grant
    Filed: May 11, 2000
    Date of Patent: December 14, 2004
    Assignee: Yale University
    Inventors: Craig M. Crews, Mikael Elofsson, Ute Splittgerber, Ny Sin, Kyung Bo Kim
  • Patent number: 6815426
    Abstract: This invention pertains to methods and compositions for inhibiting endothelial cell tube formation, the initial step of tumor angiogenesis. More specifically, the present invention relates to tripeptides that show inhibition of angiogenesis-mediated processes.
    Type: Grant
    Filed: February 12, 2002
    Date of Patent: November 9, 2004
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Mark A. Scialdone, Shaker Ahmed Mousa, Steven W. Shuey
  • Patent number: 6599892
    Abstract: Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of &bgr;-lactamase enzymes.
    Type: Grant
    Filed: July 30, 2001
    Date of Patent: July 29, 2003
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Brian Bachmann
  • Publication number: 20030004137
    Abstract: N-Heterocyclic derivatives of the formula (I): 1
    Type: Application
    Filed: April 12, 2002
    Publication date: January 2, 2003
    Applicant: Berlex Laboratories, Inc.
    Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H.J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
  • Patent number: 6489319
    Abstract: Administration of inhibitors of carboxypeptidase E provides significant neurotropic effects in warm-blooded vertebrates evidenced inter alia by anxiolytic and anti-aggressive behavior and enhanced cognition. Certain &bgr;-Lactam antibiotics, most significantly, certain 1-oxa-1-dethia cephems with blood brain barrier transport, exhibit potent therapeutic neurologic activity.
    Type: Grant
    Filed: February 14, 2001
    Date of Patent: December 3, 2002
    Assignee: Revaax Pharmaceuticals, LLC
    Inventors: Gary A. Koppel, Michael O. Chaney
  • Patent number: 6475522
    Abstract: Synthetic polymer compositions contain antibiotics as antidegradants. Antibiotics from classes of glycopeptides and &bgr;-lactams have been found to prevent or inhibit synthetic polymer degradation.
    Type: Grant
    Filed: August 30, 2000
    Date of Patent: November 5, 2002
    Assignee: Hammond Group, Inc.
    Inventor: Richard F. Grossman
  • Patent number: 6458779
    Abstract: Compounds of Formula (1) wherein: R is methyl substituted by one to three groups from alkyl, aryl, alkenyl, and alkynyl; n is ) or 1; R1 is arylmethyl or heterocyclylmethyl; R2 is alkyl, alkenyl, cycloalkyl or cycloalkenyl; and R3 is hydrogen, alkyl, alkenyl, alkynyl or aryl; are useful in the treatment of disorders mediated y s-CD23.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: October 1, 2002
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Andrew Faller, David Timothy MacPherson, Peter Henry Milner, Jayshree Mistry, John Gerald Ward
  • Patent number: 6407091
    Abstract: The invention provides compounds of formula I and IV: wherein R1-R11 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting &bgr;-lactamase enzymes, for enhancing the activity of &bgr;-lactam antibiotics, and for treating &bgr;-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I and IV, and novel intermediates useful for the synthesis of compounds of formula I and IV. The A can be, for example, thio, sulfinyl, or sulfonyl.
    Type: Grant
    Filed: April 13, 2000
    Date of Patent: June 18, 2002
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, A. Srinivasa Rao, Greg C. Adam, Sirishkumar D. Nidamarthy, Venkata Ramana Doppalapudi
  • Patent number: 6337339
    Abstract: Methods and compositions are disclosed utilizing the optically pure (S)-isomer of lomefloxacin to treat bacterial infection. In particular, this compound is a potent drug for the treatment of Mycobacteria infection.
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: January 8, 2002
    Assignee: Sepracor Inc.
    Inventors: James W. Young, A. K. Gunnar Aberg
  • Patent number: 6303592
    Abstract: Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of &bgr;-lactamase enzymes.
    Type: Grant
    Filed: March 14, 1997
    Date of Patent: October 16, 2001
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Brian Bachmann