Carbon Bonded Directly At The 16-position Patents (Class 552/573)
  • Patent number: 7998540
    Abstract: The invention relates to novel 9- and/or 10-substituted anthracenes, to their use in liquid crystal, light-emitting or semiconducting materials and devices, in anisotropic polymers, optical, electrooptical, decorative, security, cosmetic, diagnostic, electric, electronic, charge transport, semiconductor, optical recording, electroluminescent, photoconductor or electrophotographic applications, and to liquid crystal, light-emitting and semiconducting materials, polymers and devices comprising them.
    Type: Grant
    Filed: June 30, 2004
    Date of Patent: August 16, 2011
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Mark John Goulding, Marcus Thompson, Warren Duffy, Martin Heeney, Iain McCulloch
  • 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: 7718793
    Abstract: A method for producing a 6?-fluorinated corticosteroid or derivative thereof by reacting a 17-hydroxy-21-ester epoxide of Formula II with a stereoselective fluorinating agent to stereoselectively form a 21-ester-17-hydroxy 6?-fluorinated compound of Formula VII R1 can be OC(O)—Rd; R4 can be C(O)—Rd; R3 can be H or Rd. Each Rd may be the same or different and is independently selected from (C1-4)alkyl, aryl and heteroaryl. The dashed line can be a single or a double bond. R4 may be, for example, acetyl; R3 may be, for example, alpha or beta methyl; R1 may be, for example, acetate or propionate, The stereoselective fluorinating agent used in the reaction may be, for example, a fluoropyridinium or fluoroquinuclidium compound, for example, Selectfluor®.
    Type: Grant
    Filed: July 13, 2006
    Date of Patent: May 18, 2010
    Assignee: Taro Pharmaceuticals U.S.A., Inc.
    Inventors: Shimon Chernyak, Martin Zarbov, Daniella Gutman
  • Patent number: 7098328
    Abstract: A method for producing a 6?-fluorinated corticosteroid or derivative thereof by reacting a 17-hydroxy-21-ester epoxide of Formula II with a stereoselective fluorinating agent to stereoselectively form a 21-ester-17-hydroxy 6?-fluorinated compound of Formula VII R1 can be OC(O)—Rd; R4 can be C(O)—Rd; R3 can be H or Rd. Each Rd may be the same or different and is independently selected from (C1-4)alkyl, aryl and heteroaryl. The dashed line can be a single or a double bond. R4 may be, for example, acetyl; R3 may be, for example, alpha or beta methyl; R1 may be, for example, acetate or propionate. The stereoselective fluorinating agent used in the reaction may be, for example, a fluoropyridinium or fluoroquinuclidium compound, for example, Selectfluor®.
    Type: Grant
    Filed: November 27, 2002
    Date of Patent: August 29, 2006
    Assignee: Taro Pharmaceutical Industries Limited
    Inventors: Shimon Chernyak, Martin Zarbov, Daniella Gutman
  • Publication number: 20020103392
    Abstract: Corticoid 17,21-dicarboxylic esters and corticosteroid 17-carboxylic ester 21-carbonic esters, processes for their preparation and pharmaceuticals containing these compounds
    Type: Application
    Filed: July 22, 1997
    Publication date: August 1, 2002
    Inventors: ULRICH STACHE, HANS-GEORG ALPERMANN, WALTER DURCKHEIMER, MANFRED BOHN
  • 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: 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: 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: 5362721
    Abstract: The disclosed invention includes corticoid-17-alkylcarbonates substituted in the 17-position, a process for their preparation and pharmaceuticals containing them. These corticoid-17-alkylcarbonates have the following formula I ##STR1## where A is CHOH in any desired steric arrangement, C.dbd.O or CH.sub.2 ; Y is H, F, or Cl; Z is H, F or CH.sub.3 ; R(1) is O-acyl, carbonylalkyl, alkylsulfonate or arylsulfonate;R(2) is branched alkyl or (CH.sub.2).sub.2-4 --OCH.sub.3 andR(3) is H or methyl. They have excellent local and topical antiinflammatory action. They are distinguished by a particularly good ratio of local to systemic antiinflammatory activity and in some cases also show stronger local antiinflammatory activities than their isomeric corticoid-17-alkylcarbonates having a linear alkyl group in the 17-alkylcarbonate moiety.
    Type: Grant
    Filed: February 8, 1993
    Date of Patent: November 8, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ulrich Stache, Walter Durckheimer, Hans G. Alpermann, Walter Petri
  • 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: 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