The Hetero Ring Is Five-membered And Has Plural Hetero Atoms Patents (Class 540/108)
  • Patent number: 5149696
    Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein the A and B rings have a structure selected from the group consisting of ##STR2## having hormonal properties and their preparation and intermediates.
    Type: Grant
    Filed: February 23, 1990
    Date of Patent: September 22, 1992
    Assignee: Roussel Uclaf
    Inventors: Andre Claussner, Lucien Nedelec, Daniel Philibert, Patrick Van De Velde
  • Patent number: 5120723
    Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.
    Type: Grant
    Filed: May 10, 1990
    Date of Patent: June 9, 1992
    Assignee: University of Southern California
    Inventors: Kelvin W. Gee, Michael B. Bolger
  • Patent number: 5041433
    Abstract: Invented are carboxyl and carboxyl alkyl ester substituted 11-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase.
    Type: Grant
    Filed: November 1, 1989
    Date of Patent: August 20, 1991
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis A. Holt, Brian W. Metcalf, Mark A. Levy
  • Patent number: 5032586
    Abstract: Invented are carboxyl and carboxyl alkyl ester substituted 7-keto and hydroxy analogues of synthetic steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase. Also invented are methods for preparing these compounds.
    Type: Grant
    Filed: August 24, 1989
    Date of Patent: July 16, 1991
    Assignee: SmithKline Beecham Corporation
    Inventors: Brian W. Metcalf, Dennis A. Holt, Mark A. Levy
  • Patent number: 4954446
    Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase including using these compounds to reduce prostate size. Also invented are intermediates used in preparing these compounds.
    Type: Grant
    Filed: July 14, 1989
    Date of Patent: September 4, 1990
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • Patent number: 4927921
    Abstract: A compound of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl, R.sub.2 is methyl or ethyl, and A,B,C and D rings optionally containing at least one double bond and optionally substituted with at least one member of the group consisting of optionally protected --OH, .dbd.O, alkyl and alkoxy of 1 to 4 carbon atoms, halogen and alkenyl and alkynyl of 2 to 4 carbon atoms, R is selected from the group consisting of halogen, --OH, alkylthio and alkoxy of 1 to 6 carbon atoms, aralkoxy, arylthio and aralkylthio of 7 to 15 carbon atoms and ##STR2## R.sub.3 and R.sub.4 are individually hydrogen, or alkyl of 1 to 6 carbon atoms or aralkyl of 7 to 15 carbon atoms or taken together with the nitrogen form a heterocycle optionally containing another nitrogen or oxygen atom, excepting the product in which R is methoxy, R.sub.1 and R.sub.2 each represent methyl, A ring carries a 3.beta.-acetoxy function and B ring contains a double bond in 5(6) useful as intermediates for the preparation of 20-keto-pregnanes.
    Type: Grant
    Filed: December 4, 1987
    Date of Patent: May 22, 1990
    Assignee: Roussel Uclaf
    Inventors: Michel Vivat, Jean Buendia
  • Patent number: 4921845
    Abstract: The invention relates to new 11-arylsteroid compounds, having a strong antiprogestin and a weak or nonexistent antiglucocorticoid activity, to processes for preparing said compounds and also to pharmaceutical preparations which contain these derivatives as active constituent, characterized in that said steroids have the following formula: ##STR1## in which R.sub.1 is an aryl group with a ##STR2## group as substituent, X and Y each being separately H or a (1-4 C) hydrocarbyl group or together a (2-C) hydrocarbyl group which forms a 3- to 7-membered ring together with the nitrogen atom;R.sub.2 is hydrogen, hydroxyl, an acyloxy or an alkoxy group or a saturated or unsaturated hydrocarbyl group containing 1-8 carbon atoms, which hydrocarbyl group is provided with at least one hydroxyl, oxo, azido, cyano and/or halogen group;R.sub.3 is a hydroxyl, an acyloxy or an alkoxy group or an acyl group optionally substituted by a hydroxyl, alkoxy, acyloxy or halogen group; or R.sub.2 and R.sub.
    Type: Grant
    Filed: December 8, 1988
    Date of Patent: May 1, 1990
    Assignee: Akzo N.V.
    Inventors: Hendrick Paul de Jongh, Nicolaas P. van Vliet
  • 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: 4774236
    Abstract: Steroids of the formula: ##STR1## which are characterized by a 17.alpha.-cyanomethyl, azidomethyl, methoxymethyl, phenylmethyl, or ethynylmethyl substituent and a 17.beta.-hydroxy/esterified hydroxy substituent. The steroids of this invention have glucocorticoid, anti-glucocorticoid, progestational, or anti-progestational activity, depending on the particular structure.
    Type: Grant
    Filed: September 17, 1986
    Date of Patent: September 27, 1988
    Assignee: Research Triangle Institute
    Inventors: C. Edgar Cook, C. Ray Tallent, Jerry R. Reel, Mansukh C. Wani
  • Patent number: 4689410
    Abstract: Novel 23-dihydro-oxazolyl steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and methyl, R.sub.2 is selected from the group consisting of methyl and ethyl, R.sub.3 and R.sub.4 are individually selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, the A, B, C and D rings may contain 1 to 3 double bonds and may be optionally substituted with one or more members of the group consisting of --OH, protected hydroxyl, .dbd.0, protected keto, halogen alkyl or alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms and the dotted line indicates the optional presence of a second bond useful for the preparation of 20-keto-pregnanes and novel intermediates.
    Type: Grant
    Filed: October 16, 1985
    Date of Patent: August 25, 1987
    Assignee: Roussel Uclaf
    Inventors: Derek H. R. Barton, Samir Z. Zard, Jocelyne Wozniak
  • Patent number: 4609651
    Abstract: 11.beta.-Arylestradienes of general Formula I are disclosed ##STR1## wherein R.sup.2 is a hydrogen atom, a methyl group, or an ethyl group,R.sup.3 is a hydrogen atom or an acyl group,R.sup.1 and A-B have various meanings,which possess antigestagen and antimineralocorticoid activity.
    Type: Grant
    Filed: December 21, 1984
    Date of Patent: September 2, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Ralph Rohde, Klaus Annen, Gunter Neef, Rudolf Wiechert, Sybille Beier, Walter Elger, David Henderson