Oxygen Bonded Directly At The 21-position (e.g., Triamcinolone, Etc.) Patents (Class 552/566)
  • Patent number: 8258124
    Abstract: The subject matter of this application relates to the combination of ciclesonide or an epimer thereof with R,R-formoterol or a salt, or a hydrate of a salt thereof.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: September 4, 2012
    Assignee: Nycomed GmbH
    Inventors: Christian Weimar, Klaus Dietzel, Helgert Müller, Degenhard Marx
  • Patent number: 7879833
    Abstract: The invention relates to the combination of ciclesonide with formoterol.
    Type: Grant
    Filed: December 11, 2003
    Date of Patent: February 1, 2011
    Assignee: NYCOMED GmbH
    Inventors: Christian Weimar, Klaus Dietzel, Helgert Müller, Degenhard Marx
  • Publication number: 20100278896
    Abstract: A solid, implantable dosage form comprising a therapeutically active agent in solid form, optionally with one or more pharmaceutically acceptable excipients, wherein the one or more excipients, when present, do not lead to a significant delay or prolongation of the release of active agent, as compared to an equivalent dosage form containing no excipients when tested in vitro.
    Type: Application
    Filed: November 17, 2008
    Publication date: November 4, 2010
    Applicant: UCL BUSINESS PLC
    Inventors: Peng T. Khaw, Stephen Brocchini
  • Publication number: 20100234334
    Abstract: The invention relates to nitrooxyderivative of corticosteriods of general formula (I) and pharmaceutical acceptable salts or stereoisomers thereof wherein R is the corticosteriod residue of formulas (II): The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological disease and ocular diseases.
    Type: Application
    Filed: January 28, 2008
    Publication date: September 16, 2010
    Applicant: NICOX S.A.
    Inventors: Francesca Benedini, Stefano Biondi, Ennio Ongini
  • Patent number: 7390796
    Abstract: Compounds are disclosed of the formula in which R3 is C8 to C24 hydrocarbon or the residue of misoprostol. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.
    Type: Grant
    Filed: November 14, 2006
    Date of Patent: June 24, 2008
    Assignee: Sepracor Inc.
    Inventors: Mark G. Currie, Steven Jones, Charles M. Zepp
  • Publication number: 20080107736
    Abstract: The present disclosure is directed at a pharmaceutically active nanoparticle suspension that may be optically clear. Such suspensions may be formed by selective dissolution of a pharmaceutically active compound in a first solvent followed by introduction into a second solvent, such as an aqueous medium, without substantial use of surfactants and/or mechanical shear.
    Type: Application
    Filed: November 2, 2006
    Publication date: May 8, 2008
    Inventors: Joseph A. McDonough, Hong Dixon
  • Patent number: 7018995
    Abstract: Carbonates and carbamates of the formula and related steroid carbonates and carbamates are disclosed. The compounds are useful for treating rhinitis and asthma, particularly by inhalation, and for treating inflammation, particularly by local or topical administration.
    Type: Grant
    Filed: February 20, 2003
    Date of Patent: March 28, 2006
    Assignee: Sepracor Inc.
    Inventors: Mark G. Currie, Steve Jones, Paul Grover, Chris H. Senanayake, Q. Kevin Fang
  • Publication number: 20040236126
    Abstract: 7&agr;-Hydroxy-pregn-4-en-3-one-20-carbaldehyde, a production method thereof and a method for producing 7&agr;,21-dihydroxy-20-methyl-pregn-4-en-3-one, which is useful as a synthetic intermediate for pharmaceuticals such as squalamine and the like, efficiently at high purity from the carbaldehyde.
    Type: Application
    Filed: March 4, 2004
    Publication date: November 25, 2004
    Inventors: Masao Tsuji, Yoko Nakano, Shigeo Ohzono, Makoto Nakazawa
  • Patent number: 6197762
    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•) 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: September 18, 1998
    Date of Patent: March 6, 2001
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Stewart K. Richardson
  • Patent number: 6043603
    Abstract: The invention relates to a low-pressure discharge lamp with at least one porting element (12) placed inside a discharge vessel (10). Said supporting element is provided with a mercurial coating (13) and is coated with a getter material (14). The coated surfaces of the supporting element (12) are inclined at an angle of at least 30 degrees in relation to the longitudinal axis (A--A) of the discharge vessel (10).
    Type: Grant
    Filed: May 21, 1998
    Date of Patent: March 28, 2000
    Assignee: Patent-Treuhand-Gesellschaft fuer elektrische Gluehlampen mbH
    Inventor: Erolf Weinhardt
  • 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: 5670676
    Abstract: Disclosed is a process for producing a compound of the formula: ##STR1## by reacting a compound of the formula: ##STR2## with: (1) a chlorinating reagent selected from an N-chloroimide or an N-chloroamide; (2) an anhydrous strong acid selected from orthophosphoric acid, alkylsulfonic acids, fluoroalkylsulfonic acids or arylsulfonic acids; and (3) anhydrous dimethylformamide; at a temperature within the range of about -78.degree. to about 0.degree. C.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: September 23, 1997
    Assignee: Schering Corporation
    Inventors: Richard W. Draper, Eugene J. Vater
  • Patent number: 5616573
    Abstract: Glucocorticoids of general formula IR--Val--O--GC (II),are described,in whichO-GC is the radical of a 21-hydroxycorticoid that has an antiinflammatory action,Val represents a valine radical in the 21-position of the corticoid andR means a hydrogen atom or a hydrocarbon radical with up to 32 carbon atoms that is optionally substituted by hydroxy groups, amino groups, oxo groups and/or halogen atoms and/or interrupted by oxygen atoms, SO.sub.2 groups and/or NH groups and their salts.
    Type: Grant
    Filed: October 6, 1995
    Date of Patent: April 1, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Hans J. Zentel, Michael Topert, Henry Laurent, Thomas Brumby, Peter Esperling
  • Patent number: 5502183
    Abstract: Novel steroids having a 9.alpha.-hydroxy or a 9.alpha.-carbonate substituent can be prepared from 9.alpha.-hydroxyandrostenedione and can be utilized in the synthesis of commercially valuable corticosteroids such as betamethasone. The 9.alpha.-carbonates are prepared by reaction of the corresponding 9.alpha.-hydroxy steroid with a sequence of excess base, trialkylsilyl chloride, alkyl haloformate and alkanol or by using excess base, alkyl haloformate and alkoxide. 9.alpha.-Carbonate-17-keto compounds can be treated with lithium acetylide and a lithium salt to afford the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-9.alpha.-carbonate. This compound is then esterified with a novel series of reagents to give the 17-ester which can be reduced the corresponding 17-allene. Oxidation of this allene to the bis-epoxide compound, followed by treatment with an alkali metal salt of a carboxylic acid under phase transfer conditions gives the 17.alpha.-hydroxy 21-ester 9.alpha.-carbonate. Elimination of the 9.alpha.
    Type: Grant
    Filed: July 25, 1994
    Date of Patent: March 26, 1996
    Assignee: Schering Corporation
    Inventors: David R. Andrews, Anantha R. Sudhakar
  • Patent number: 5482934
    Abstract: The present invention relates to compounds of the formula: ##STR1## in which X.sub.1 and X.sub.2 correspond to H or F without distinction; R.sub.1 represents the following radicals: ##STR2## and R.sub.2 represents the radicals ##STR3## in the form of an R epimer, an S epimer, or a stereoisomeric mixture of the R and S epimers in terms of the orientation of the substituents on the carbon atom at position 22, novel intermediates and a method of their preparation by hydrolysis-ketalization, and use of such compounds as drugs and/or therapeutic agents.
    Type: Grant
    Filed: July 20, 1994
    Date of Patent: January 9, 1996
    Assignee: Especialidades Latinas Medicamentos Universales, S.A. (Elmu, S.A.)
    Inventors: Jose Calatayud, Jose R. Conde, Manuel Luna
  • Patent number: 5451690
    Abstract: A compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, acyl of an organic carboxylic acid of 1 to 8 carbon atoms, allyloxycarbonyl, alkoxycarbonyl and aralkoxycarbonyl of up to 8 carbon atoms and alkylsulfonyl and arylsulfonyl of up to 8 carbon atoms and their use to prepare substituted 16,17-methylenedioxy-steroids and novel intermediates.
    Type: Grant
    Filed: January 13, 1995
    Date of Patent: September 19, 1995
    Assignee: Roussel Uclaf
    Inventors: Luc Devocelle, Philippe Mackiewicz
  • Patent number: 5434258
    Abstract: A compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, acyl of an organic carboxylic acid of 1 to 8 carbon atoms, allyloxycarbonyl, alkoxycarbonyl and aralkoxycarbonyl of up to 8 carbon atoms and alkylsulfonyl and arylsulfonyl of up to 8 carbon atoms and their use to prepare substituted 16,17-methylenedioxy-steroids and novel intermediates.
    Type: Grant
    Filed: February 2, 1994
    Date of Patent: July 18, 1995
    Assignee: Roussel Uclaf
    Inventors: Luc Devocelle, Philippe Mackiewicz
  • 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: 5082835
    Abstract: The invention relates to antiinflammatory compounds of the formula (I), ##STR1## wherein A stands for hydrogen, hydroxyl or trifluoroacetoxy group;X stands for hydrogen or halogen with the proviso that if A is hydrogen, then X also means hydrogen;R stands for hydrogen, benzoyl or C.sub.1-8 alkanoyl group; andrepresents a single or double bond between two adjacent carbon atoms,as well as pharmaceutical compositions containing these compounds and a process for their preparation.
    Type: Grant
    Filed: March 9, 1990
    Date of Patent: January 21, 1992
    Assignee: Richter Gedeon Vegyeszeti Gyar R.T.
    Inventors: Csaba Molnar, Gyorgy Hajos, Laszlo Szporny, Jozsef Toth, Arpad Kiraly, Anna Boor nee Mezei, Janos Csorgei, Kristina Szekely, Lilla Forgacs, Gyorgy Fekete, Bulcsu Herenyi, Sandor Holly, Jozsef Szunyog
  • 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: 4920216
    Abstract: This invention concerns a method of substituting a chlorine atom for a predetermined hydrogen atom located within an organic compound which comprises contacting the organic compound containing the predetermined hydrogen atom with an esterifying agent comprising a pyridine ring or a substituted or fused ring derivative of a pyridine ring so as to produce an ester and treating the ester with a chlorinating agent so as to substitute the chlorine atom for the predetermined hydrogen atom. The ester comprises the pyridine ring or the substituted or fused ring derivative of the pyridine ring so positioned within the ester with respect to the predetermined hydrogen atom that a chlorine atom attached to the nitrogen atom of the pyridine ring or substituted or fused ring derivative of the pyridine ring reacts with the predetermined hydrogen atom.
    Type: Grant
    Filed: May 28, 1987
    Date of Patent: April 24, 1990
    Assignee: The Trustees of Columbia in the City of New York
    Inventors: Ronald Breslow, Michael Brandl, Alan D. Adams, Jurgen Hunger
  • 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