Abstract: The object of the present invention is to provide an industrial and economical process for preparing (E2)-cis-6,7-epoxy-2-nonenal of the following formula (3): The present invention provides a process for preparing (E2)-cis-6,7-epoxy-2-nonenal (3), comprising at least steps of: subjecting (Z3,Z6)-3,6-nonadien-1-ol of the following formula (1) to oxidation: to form (E2,Z6)-2,6-nonadienal of the following formula (2); and epoxidizing the resulting (E2,Z6)-2,6-nonadienal to form the aforesaid (E2)-cis-6,7-epoxy-2-nonenal (3).
Abstract: The invention relates to nitrooxy derivatives of fluocinolone acetonide, triamcinolone acetonide, betamethasone and beclomethasone, methods for their preparation, pharmaceutical compositions containing these compounds, and methods of using these compounds and compositions for treating diabetic macular edema, diabetic retinopathy, macular degeneration, age-related macular degeneration and other diseases of retina and macula lutea.
Abstract: Methods, devices and compositions for treatment of severe and uncontrolled asthma are provided by which high amounts of an inhaled corticosteroid are directed to the small airways of the lower lungs. The invention provides for a substantial decrease in the dose of concurrently administered oral corticosteroids. A particular advantage of the invention is the significant reduction in corticosteroid-related adverse effects.
Type:
Application
Filed:
February 3, 2010
Publication date:
February 16, 2012
Applicant:
ACTIVAERO GMBH RESEARCH & DEVELOPMENT
Inventors:
Bernard Muellinger, Thomas Hofmann, Gerhard Scheuch, Philipp Kroneberg
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
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
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
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
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
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
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.
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
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