Chalcogen, Halogen, Or Nitrogen Attached Indirectly To The Cyclopentanohydrophenanthrene Ring System By Acyclic Nonionic Bonding Patents (Class 540/44)
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Patent number: 9562068Abstract: 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: GrantFiled: October 16, 2015Date of Patent: February 7, 2017Assignee: INDUSTRIALE CHIMICA, S.r.l.Inventors: Roberto Lenna, Riccardo Di Brisco, Francesco Barbieri
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Publication number: 20140011785Abstract: 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: ApplicationFiled: September 6, 2013Publication date: January 9, 2014Applicant: Yale UniversityInventor: Richard Hochberg
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Patent number: 8015725Abstract: 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: GrantFiled: September 21, 2004Date of Patent: September 13, 2011Assignee: DOS-I Solutions, S.L.Inventor: Joan Iglesias Vives
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Publication number: 20100184735Abstract: 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: ApplicationFiled: May 2, 2008Publication date: July 22, 2010Inventor: Richard Hochberg
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Patent number: 7129345Abstract: Multiple novel keto-substituted intermediates are provided for the synthesis of epoxymexrenone, useful as an Aldosterone Receptor Antagonist.Type: GrantFiled: June 20, 2005Date of Patent: October 31, 2006Assignee: Pharmacia CorporationInventors: 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
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Patent number: 7112669Abstract: 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: GrantFiled: February 7, 2005Date of Patent: September 26, 2006Assignee: 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
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Patent number: 6586591Abstract: 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: GrantFiled: August 31, 2001Date of Patent: July 1, 2003Assignee: 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
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Patent number: 6541463Abstract: 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: GrantFiled: March 10, 1999Date of Patent: April 1, 2003Assignee: Endorecherche, Inc.Inventors: Fernand Labrie, Alain Belanger, Sylvain Gauthier, Van Luu-The, Yves Merand, Donald Poirier, Louis Provencher, Shankar M. Singh
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Patent number: 6331622Abstract: 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: GrantFiled: February 8, 1999Date of Patent: December 18, 2001Assignee: 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
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Patent number: 6177416Abstract: 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: GrantFiled: October 5, 1999Date of Patent: January 23, 2001Assignee: Schering AktiengesellschaftInventors: Henry Laurent, Ralph Lipp, Peter Esperling, Johannes-Wilhelm Tack
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11.beta.-aryl-4-estrenes, process for their production as well as their use as pharmaceutical agents
Patent number: 5843933Abstract: 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: GrantFiled: May 3, 1995Date of Patent: December 1, 1998Assignee: Schering AktiengesellschaftInventors: Arwed Cleve, Cornelius Scheidges, Gunter Neef, Eckhard Ottow, Walter Elger, Sybille Beier -
Patent number: 5426102Abstract: 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: GrantFiled: June 22, 1993Date of Patent: June 20, 1995Assignee: Schering AktiengesellschaftInventors: Wolfgang Schwede, Eckhard Ottow, Gunter Neef, Arwed Cleve, Krzysztof Chwalisz, Horst Michna
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Patent number: 5244886Abstract: 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: GrantFiled: March 20, 1991Date of Patent: September 14, 1993Assignee: Schering AktiengesellschaftInventors: Stefan Scholz, Gunter Neef, Eckhard Ottow, Walter Elger, Sybille Beier, Krzysztof Chwalisz
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Patent number: 4987128Abstract: 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: GrantFiled: February 24, 1987Date of Patent: January 22, 1991Assignee: Roussel UclafInventors: Lucien Nedelec, Francois Nique, Anne-Marie Moura
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Patent number: 4978657Abstract: 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: GrantFiled: December 17, 1985Date of Patent: December 18, 1990Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Vesperto Torelli, Roger Deraedt, Daniel Philibert, Germain Costerousse
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Patent number: 4912097Abstract: 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: GrantFiled: April 30, 1987Date of Patent: March 27, 1990Assignee: Roussel UclafInventors: Jean-Georges Teutsch, Michel Klich, Daniel Philibert
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Patent number: 4701449Abstract: 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: GrantFiled: August 23, 1985Date of Patent: October 20, 1987Assignee: Roussel UclafInventors: Vesperto Torelli, Lucien Nedelec, Martine Moguilewski, Anne-Marie Moura
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Patent number: 4614616Abstract: 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: GrantFiled: September 26, 1983Date of Patent: September 30, 1986Assignee: Schering AktiengesellschaftInventors: Karl Petzoldt, Rudolf Wiechert, Henry Laurent, Klaus Nickisch, Dieter Bittler
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Patent number: 5236596Abstract: 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: GrantFiled: July 24, 1991Date of Patent: August 17, 1993Inventor: Edward H. Greenwald, Sr.