Nitrogen Or Sulfur Containing Patents (Class 552/575)
  • Patent number: 8790691
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Grant
    Filed: May 26, 2009
    Date of Patent: July 29, 2014
    Assignee: The University of British Columbia
    Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Publication number: 20110165225
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Application
    Filed: May 26, 2009
    Publication date: July 7, 2011
    Inventors: Peter Cullis, Marcel Bally
  • Publication number: 20110130376
    Abstract: The invention relates to compounds of general formula (I) and pharmaceutically acceptable salts or stereoisomers thereof The compounds are useful in the treatment of illnesses wherein the known steroid, parent or precursor steroid, is generally applied, with increased benefit in terms of pharmacological profile and fewer or milder side effects than those of the known steroids.
    Type: Application
    Filed: July 24, 2009
    Publication date: June 2, 2011
    Applicant: NICOX S.A.
    Inventors: Francesca Benedini, Laura Carzaniga, Ennio Ongini, Stefamo Biondi
  • Patent number: 7605151
    Abstract: Compounds of the formula and use of the compounds as medicaments.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: October 20, 2009
    Assignee: Nicox S.A.
    Inventor: Piero Del Soldato
  • Patent number: 7368442
    Abstract: Compounds of the formula and use of the compounds as medicaments.
    Type: Grant
    Filed: March 7, 2007
    Date of Patent: May 6, 2008
    Assignee: Nicox S.A.
    Inventor: Piero Del Soldato
  • Patent number: 7205288
    Abstract: Compounds of the formula and use of the compounds as medicaments.
    Type: Grant
    Filed: June 2, 2006
    Date of Patent: April 17, 2007
    Assignee: Nicox S.A.
    Inventor: Piero Del Soldato
  • Patent number: 7196074
    Abstract: Methods of using 7?,11?-dimethyl-17?-hydroxyestra-4,14-dien-3-one (III) and 17 esters thereof for various hormonal therapies, oral and parenteral dosage forms comprising these actives, and processes for their preparation.
    Type: Grant
    Filed: October 28, 2002
    Date of Patent: March 27, 2007
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Richard P. Blye, Hyun K. Kim, Pemmaraju Narasimha Rao, Carmie Kirk Acosta
  • Patent number: 7196075
    Abstract: Compounds of the formula and use of the compounds as medicaments.
    Type: Grant
    Filed: March 14, 2006
    Date of Patent: March 27, 2007
    Assignee: Nicox S.A.
    Inventor: Piero Del Soldato
  • Patent number: 7160871
    Abstract: Compounds of the formula and use of the compounds as medicaments.
    Type: Grant
    Filed: March 14, 2006
    Date of Patent: January 9, 2007
    Assignee: Nicox S.A.
    Inventor: Piero Del Soldato
  • Patent number: 7157450
    Abstract: Compounds of the formula and use of the compounds as medicaments.
    Type: Grant
    Filed: March 14, 2006
    Date of Patent: January 2, 2007
    Assignee: Nicox S.A.
    Inventor: Piero Del Soldato
  • Patent number: 7056905
    Abstract: Compounds of the formula and use of the compounds as medicaments.
    Type: Grant
    Filed: June 17, 2003
    Date of Patent: June 6, 2006
    Assignee: Nicox S.A.
    Inventor: Piero Del Soldato
  • Patent number: 6780854
    Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C,1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.
    Type: Grant
    Filed: October 24, 2002
    Date of Patent: August 24, 2004
    Assignee: Akzo Nobel NV
    Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
  • Patent number: 6713465
    Abstract: This invention provides a pharmaceutically acceptable salt of 5&agr;-pregn-16-en-3&bgr;-ol-20-one 3-sulfate ester, which is useful as a progestational agent.
    Type: Grant
    Filed: November 1, 1999
    Date of Patent: March 30, 2004
    Assignee: Wyeth
    Inventors: Reinhold H. W. Bender, Mahdi B. Fawzi, Horace Fletcher, III, George O. Morton, Syed M. Shah, Xuejun Tang
  • Patent number: 6313108
    Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.
    Type: Grant
    Filed: July 11, 2000
    Date of Patent: November 6, 2001
    Assignee: Akzo Nobel N.V.
    Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
  • Patent number: 5910478
    Abstract: The present invention provides peptides, cyclized peptides and peptidomimetics which inhibit the oncogenic and/or transforming activity of the p21 ras protein, pharmaceutical compositions containing at least one of the ras-inhibiting peptides, cyclized peptides and peptidomimetics, and methods for inhibiting the ras-mediated oncogenic and/or transformation process in mammalian cells or tissues.
    Type: Grant
    Filed: September 20, 1996
    Date of Patent: June 8, 1999
    Assignee: Innapharma, Inc.
    Inventors: Joseph J. Hlavka, John Fowler Noble, Henry Baxter Abajian, Andrew S. Kende, Matthew R. Pincus
  • Patent number: 5824669
    Abstract: Disclosed are (i) compounds of a steroid, a .beta.-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO.sub.2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, .beta.-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO.sub.2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO.sup.+) or nitroxyl (NO.sup.-), or as the neutral species, nitric oxide (NO.circle-solid.) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.
    Type: Grant
    Filed: March 22, 1996
    Date of Patent: October 20, 1998
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Stewart K. Richardson
  • Patent number: 5710293
    Abstract: The present invention relates to a method of using a perchloric acid catalyzed reaction to make acyl derivatives of norprogesterone compounds and, in particular, 16-methylene-17.alpha.-hydroxy-19-norpregn-4-ene-3,20-dione.
    Type: Grant
    Filed: October 13, 1995
    Date of Patent: January 20, 1998
    Assignee: The Population Council, Center for Biomedical Research
    Inventor: Fang Li
  • Patent number: 5567830
    Abstract: A method for the preparation of an acetylenic alcohol by reaction of 1,2-dibromoethylene with an alkyl, aryl an heteroaryl lithium in an inert solvent, followed by reaction with a carbonyl-containing compound to give an acetylenic alcohol is disclosed.
    Type: Grant
    Filed: February 14, 1994
    Date of Patent: October 22, 1996
    Assignee: Cocensys, Inc.
    Inventor: Ravindra B. Upasani
  • Patent number: 5352808
    Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted by halogen or a nitrogen or oxygen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A, B, C and D rings are optionally substituted by at least one member of the group consisting of optionally protected --OH or .dbd.0, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 and the A, B, C and D rings are defined as above with an oxidizing agent in the presence of water and an at least partially water-miscible solvent to obtain a compound of the formula ##STR3## wherein R.sub.1 and R.sub.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: October 4, 1994
    Assignee: Roussel Uclaf
    Inventors: Jean Buendia, Michel Vivat
  • Patent number: 5250711
    Abstract: Amine salts of alkane-1,n-dicarboxylic acid mono-(2-sulfatoethyl)amides of the Formula IHOC(O)--(CH.sub.2).sub.n --C(O)--N(R.sub.1)--CH.sub.2 CH.sub.2 SO.sub.3.sup.--+ HN(R.sub.2).sub.3 Iwherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.8 alkyl and phenyl, R.sub.2 is C.sub.1 -C.sub.8 alkyl or (R.sub.2).sub.3 when taken together with the nitrogen atom is pyridinyl; and n is an integer from 4 to 20, their preparation and use to prepare water-soluble esters of corticosteroids.
    Type: Grant
    Filed: January 12, 1990
    Date of Patent: October 5, 1993
    Assignee: The Upjohn Company
    Inventor: Bruce A. Pearlman
  • Patent number: 4948533
    Abstract: The present invention relates to 21-(3-carboxy-1-oxopropoxy) -17.alpha.-hydroxy-11.alpha.-(3,3-dimethyl-1-oxobutoxy)pregna-1,4-diene-3, 20 dione and pharmaceutically acceptable salts thereof which are useful steroid prodrugs.
    Type: Grant
    Filed: February 16, 1989
    Date of Patent: August 14, 1990
    Assignee: The Upjohn Company
    Inventors: John M. Braughler, Edward D. Hall, Wendell Wierenga, John M. McCall
  • Patent number: 4933331
    Abstract: 3,20-dione-11.beta.-hydroxypregn-4-ene-21-thioacetate-17-butyrate and 3,20-dione-11.beta.-hydroxypregn-4-ene-21-thiopropionate-17-butyrate, are anti-inflammatory agents.
    Type: Grant
    Filed: November 4, 1985
    Date of Patent: June 12, 1990
    Assignee: Jouveinal, S.A.
    Inventors: Gilbert G. Aubard, Agnes G. Grouhel, Jean-Louis Junien, Claude P. Roux, Dieran R. Torossian
  • Patent number: 4913852
    Abstract: Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with derivatives of .DELTA.-4-pregnene-3,20-dione or with derivatives of .DELTA.-1,4-pregnadiene-3,20-dione of the general formulas (I), (II) and (III), having glucocorticoidal and anti-inflammatory properties have been prepared and tested. Pharmaceutical compositions, medicaments containing them as well as their applications are claimed, particularly in the cutaneous and ophthalmic fields.
    Type: Grant
    Filed: February 24, 1988
    Date of Patent: April 3, 1990
    Inventors: Catherine Milioni, Constantin Efthyimiopoulos, Bernard Koch, Louis Jung, Jean Jung
  • Patent number: RE37116
    Abstract: Disclosed are (i) compounds of a steroid, a &bgr;-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, &bgr;-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO&Circlesolid;) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.
    Type: Grant
    Filed: December 23, 1998
    Date of Patent: March 27, 2001
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Stewart K. Richardson