Chalcogen, Halogen, Or Nitrogen Attached Indirectly To The Cyclopentanohydrophenanthrene Ring System By Acyclic Nonionic Bonding Patents (Class 540/44)
  • Patent number: 9562068
    Abstract: An improved process for the preparation of intermediate (V) through the elimination of a molecule of water from intermediate (IV) is described. Intermediate (V) is a key molecule for the synthesis of eplerenone, a synthetic steroid with pharmacological activity used in the treatment of chronic pathological conditions, including hypertension.
    Type: Grant
    Filed: October 16, 2015
    Date of Patent: February 7, 2017
    Assignee: INDUSTRIALE CHIMICA, S.r.l.
    Inventors: Roberto Lenna, Riccardo Di Brisco, Francesco Barbieri
  • Publication number: 20140011785
    Abstract: The present invention relates to antiandrogenic compounds which may be administered for the treatment of androgen excess in the skin and by way of consequence, the treatment of acne, baldness or hirsuitism in subject or patient.
    Type: Application
    Filed: September 6, 2013
    Publication date: January 9, 2014
    Applicant: Yale University
    Inventor: Richard Hochberg
  • Patent number: 8015725
    Abstract: The invention relates to a method and a device, as well as the variants thereof, which operates continuously or discontinuously for the agglomeration and/or drying of powder materials using selective infrared irradiation on a surface which is continually supplied with renewed powder, with or without the spraying of liquids. The process can be performed in sealed conditions or open to the atmosphere, with or without the recovery of volatile components.
    Type: Grant
    Filed: September 21, 2004
    Date of Patent: September 13, 2011
    Assignee: DOS-I Solutions, S.L.
    Inventor: Joan Iglesias Vives
  • Publication number: 20100184735
    Abstract: The present invention relates to antiandrogenic compounds which may be administered for the treatment of androgen excess in the skin and by way of consequence, the treatment of acne, baldness or hirsuitism in subject or patient.
    Type: Application
    Filed: May 2, 2008
    Publication date: July 22, 2010
    Inventor: Richard Hochberg
  • Patent number: 7129345
    Abstract: Multiple novel keto-substituted intermediates are provided for the synthesis of epoxymexrenone, useful as an Aldosterone Receptor Antagonist.
    Type: Grant
    Filed: June 20, 2005
    Date of Patent: October 31, 2006
    Assignee: Pharmacia Corporation
    Inventors: John S. Ng, Ping T. Wang, Julio A. Baez, Chin Liu, Dennis K. Anderson, Jon P. Lawson, Bernhard Erb, Joseph Wieczorek, Gennaro Mucciariello, Fortunato Vanzanella, Sastry A. Kunda, Leo J. Letendre, Mark J. Pozzo, Yuen-Lung L. Sing, Edward E. Yonan
  • Patent number: 7112669
    Abstract: Intermediates in the preparation of 9,11-epoxy steroids are disclosed. Particularly, disclosed are 11,12-epoxy steroid, 4,5-9,11-diepoxy steroid and 12-keto steroid intermediates.
    Type: Grant
    Filed: February 7, 2005
    Date of Patent: September 26, 2006
    Assignee: Pharmacia Corporation (of Pfizer, Inc.)
    Inventors: John S. Ng, Chin Liu, Dennis K. Anderson, Jon P. Lawson, Joseph J. Wieczorek, Sastry A. Kunda, Leo J. Letendre, Mark J. Pozzo, Yuen-Lung L. Sing, Ping T. Wang, Edward E. Yonan, Richard M. Weier, Thomas R. Kowar, Julio A. Baez, Bernhard Erb
  • Patent number: 6586591
    Abstract: A process for the formation of compounds of Formula VI: comprising hydrolyzing a compound corresponding to Formula VII: wherein —A—A—, —B—B—, R3, R8 and R9 are as defined in the specification.
    Type: Grant
    Filed: August 31, 2001
    Date of Patent: July 1, 2003
    Assignee: G.D. Searle & Co.
    Inventors: John S. Ng, Ping T. Wang, Julio A. Baez, Chin Liu, Dennis K. Anderson, Jon P. Lawson, Bernhard Erb, Joseph Wieczorek, Gennaro Mucciariello, Fortunato Vanzanella, Sastry A. Kunda, Leo J. Letendre, Mark J. Pozzo, Yuen-Lung L. Sing, Edward E. Yonan
  • Patent number: 6541463
    Abstract: Novel methods of medical treatment and/or inhibition of development of diseases are disclosed for diseases that are sensitive to androgenic or estrogenic activity. The treatments utilize inhibitors of type 5 and/or type 3 17&bgr;-hydroxysteroid dehydrogenase. Novel inhibitors of type 5 17&bgr;-hydroxysteroid dehydrogenase are also disclosed, as are novel inhibitors of type 3 17&bgr;-hydroxysteroid dehydrogenase.
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: April 1, 2003
    Assignee: Endorecherche, Inc.
    Inventors: Fernand Labrie, Alain Belanger, Sylvain Gauthier, Van Luu-The, Yves Merand, Donald Poirier, Louis Provencher, Shankar M. Singh
  • Patent number: 6331622
    Abstract: A process for the formation of an epoxy compound comprising contacting a substrate compound having an olefinic double bond with a peroxide compound in the presence of a peroxide activator, said peroxide activator corresponding to the formula: where Ro is a substituent having an electron withdrawing strength not less than that of monochloromethyl.
    Type: Grant
    Filed: February 8, 1999
    Date of Patent: December 18, 2001
    Assignee: G.D. Searle & Co.
    Inventors: John S. Ng, Ping T. Wang, Julio A. Baez, Chin Liu, Dennis K. Anderson, Jon P. Lawson, Bernhard Erb, Joseph Wieczorek, Gennaro Mucciariello, Fortunato Vanzanella, Sastry A. Kunda, Leo J. Letendre, Mark J. Pozzo, Yuen-Lung L. Sing, Edward E. Yonan
  • Patent number: 6177416
    Abstract: 3-Oxyiminopregnane-21-carbolactones of formula I, wherein R is as defined by the specification, their production and use as pharmaceutical agents are described.
    Type: Grant
    Filed: October 5, 1999
    Date of Patent: January 23, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: Henry Laurent, Ralph Lipp, Peter Esperling, Johannes-Wilhelm Tack
  • Patent number: 5843933
    Abstract: Compounds of formula I ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings indicated in the description, are described, as well as processes for their production, pharmaceutical preparations containing these compounds as well as their use for treatment of diseases. The compounds have antigestagenic, antiglucocorticoid, antimineralocorticoid and antiandrogenic properties.
    Type: Grant
    Filed: May 3, 1995
    Date of Patent: December 1, 1998
    Assignee: Schering Aktiengesellschaft
    Inventors: Arwed Cleve, Cornelius Scheidges, Gunter Neef, Eckhard Ottow, Walter Elger, Sybille Beier
  • Patent number: 5426102
    Abstract: Novel compounds of the general formula I ##STR1## and the pharmacologically tolerable addition salts thereof with acids are described, in which eitherIa) R.sup.11 represents a hydrogen atom in the .beta.-configuration and each of R.sup.12 and R.sup.13 represents a hydrogen atom, orIb) R.sup.11 represents a hydrogen atom in the .beta.-configuration and R.sup.12 and R.sup.13 together represent a second bond, orIc) R.sup.11 and R.sup.12 together represent a second bond and R.sup.13 represents a hydrogen atom, orId) R.sup.11 represents a hydrogen atom in the .alpha.-configuration and R.sup.12 and R.sup.13 together represent a second bond,and in Ia), Ib), Ic) or Id)X represents an oxygen atom, the hydroxyimino grouping >N.about.OH or two hydrogen atoms,R.sup.1 represents a hydrogen atom or a methyl group,R.sup.2 represents a hydroxy group, a C.sub.1 -C.sub.10 -alkoxy group or a C.sub.1 -C.sub.10 -acyloxy group, andR.sup.3 and R.sup.
    Type: Grant
    Filed: June 22, 1993
    Date of Patent: June 20, 1995
    Assignee: Schering Aktiengesellschaft
    Inventors: Wolfgang Schwede, Eckhard Ottow, Gunter Neef, Arwed Cleve, Krzysztof Chwalisz, Horst Michna
  • Patent number: 5244886
    Abstract: New 11.beta.-phenyl-14.beta.H-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N.about.OH, and M and N are either jointly a second compound or L is a hydrogen atom and M is an .alpha.-permanent hydroxy group and either A and B together are a second compound and D is a hydrogen atom, where R.sup.1 is a five or six-part heteroalkyl residue or a cycloalkyl, cycloalkenyl or aryl residue or A is a hydrogen atom and B and D together are a methylene bridge, where R.sup.1 besides the aforementioned residues may be a possibly substituted hydrocarbon residue with up to 10 C atoms, a possibly substituted amino group, a hydroxy or C.sub.1-8 alkoxy, mercapto or thioalkyl group, R.sup.2 is a methyl or ethyl residue, and R.sup.3 /R.sup.4 represents the usual combination of substituents on the C17 atom in steroid chemistry, having antigestagenic and other properties.
    Type: Grant
    Filed: March 20, 1991
    Date of Patent: September 14, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Stefan Scholz, Gunter Neef, Eckhard Ottow, Walter Elger, Sybille Beier, Krzysztof Chwalisz
  • Patent number: 4987128
    Abstract: Novel 10.beta.-alkynyl-steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl and alkoxy of 1 to 8 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, optionally substituted aryl and aralkyl, optionally esterified carboxy, dialkylamino with alkyl of 1 to 6 carbon atoms, halogen and trialkylsilyl of 1 to 7 alkyl carbon atoms, R.sub.6 and R.sub.7 taken together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms, optionally substituted alkenyl and alkynyl of 2 to 6 carbon atoms and acetylthio, R.sub.
    Type: Grant
    Filed: February 24, 1987
    Date of Patent: January 22, 1991
    Assignee: Roussel Uclaf
    Inventors: Lucien Nedelec, Francois Nique, Anne-Marie Moura
  • Patent number: 4978657
    Abstract: Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at leat one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.
    Type: Grant
    Filed: December 17, 1985
    Date of Patent: December 18, 1990
    Assignee: Roussel Uclaf
    Inventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert, Germain Costerousse
  • Patent number: 4912097
    Abstract: Novel 11.beta.-alkynylphenyl-19-nor-steroids of the formula ##STR1## wherein R.sub.1 is alkynyl of 2 to 8 carbon atoms optionally substituted with at least one member of the group consisting of --OH halogen, trialkylsilyl of 1 to 6 alkyl carbon atoms, alkoxy and alkylthio of 1 to 6 carbon atoms and dialkylamino of 1 to 6 alkyl carbon atoms having remarkably antiprogestomimetic and antiglucocorticoidal activity.
    Type: Grant
    Filed: April 30, 1987
    Date of Patent: March 27, 1990
    Assignee: Roussel Uclaf
    Inventors: Jean-Georges Teutsch, Michel Klich, Daniel Philibert
  • Patent number: 4701449
    Abstract: Novel 10-substituted steroids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 8 carbon atoms, alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 8 carbon atoms, aryl and substituted aryl, aralkyl and substituted aralkyl, protected hydroxy, optionally esterified carboxy, --NH.sub.2, protected amino, mono and di-alkyl amino of 1 to 4 alkyl carbon atoms, halogen and trialkylsilyl, R.sub.2 is methyl or ethyl, R.sub.6 and R.sub.7 together with the carbon atoms to which they are attached form cyclopropyl or R.sub.6 is hydrogen and R.sub.7 is R.sub.1, R.sub.1 is selected from the group consisting of hydrogen, alkyl and substituted alkyl of 1 to 6 carbon atoms, acetylthio and alkenyl, substituted alkenyl, alkynyl and substituted alkynyl of 2 to 6 carbon atoms, X is optionally acylated or etherified hydroxyl and Y is selected from the group consisting of hydrogen, R.sub.4, --CH.sub.2 --CH.sub.2 COOM and --CH.sub.2 --CH.sub.
    Type: Grant
    Filed: August 23, 1985
    Date of Patent: October 20, 1987
    Assignee: Roussel Uclaf
    Inventors: Vesperto Torelli, Lucien Nedelec, Martine Moguilewski, Anne-Marie Moura
  • Patent number: 4614616
    Abstract: A process for preparing a 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 -steroid of the formula ##STR1## wherein Q is ##STR2## and R.sub.1 is hydrogen, trimethylacetyl, tert-butyldimethylsilyl, dimethyl-2-(3-methylbutyl)silyl or tribenzylsilyl, comprises fermenting a 3.beta.-hydroxy-.DELTA..sup.5 -steroid of the formula ##STR3## wherein Q is as defined above, andR.sub.2 is hydrogen or alkanoyl of 2-6 carbon atoms, with a culture of Botryodiplodia malorum to obtain the corresponding 3.beta.,7.beta.-dihydroxy-.DELTA..sup.5 -steroid; and, optionally, reacting the resultant product with trimethylacetic anhydride, tert-butyldimethylsilyl chloride, dimethyl-2-(3-methylbutyl)silyl chloride, or tribenzylsilyl chloride.
    Type: Grant
    Filed: September 26, 1983
    Date of Patent: September 30, 1986
    Assignee: Schering Aktiengesellschaft
    Inventors: Karl Petzoldt, Rudolf Wiechert, Henry Laurent, Klaus Nickisch, Dieter Bittler
  • Patent number: 5236596
    Abstract: A method and apparatus for dewatering an aqueous coal slurry includes imparting high shear forces to the aqueous coal slurry in the presence of a peptizing agent to render coal particles hydrophobic by stripping clay from the coal particles and peptizing the clay in the aqueous medium of the slurry. The slurry is separating to recover coal particles and the aqueous medium is draining medium from the hydrophobic surface of the coal particles.
    Type: Grant
    Filed: July 24, 1991
    Date of Patent: August 17, 1993
    Inventor: Edward H. Greenwald, Sr.