Plural Oxygens In The Spiro Hetero Ring Patents (Class 540/31)
  • Publication number: 20120283450
    Abstract: This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: July 18, 2012
    Publication date: November 8, 2012
    Inventors: Eric Anderson, Gary L. Bolton, Deborah A. Ferguson, Xin Jiang, Robert M. Kral, JR., Patrick M. O'Brien, Melean Visnick
  • Publication number: 20120283217
    Abstract: As described herein, the present invention provides compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.
    Type: Application
    Filed: July 16, 2012
    Publication date: November 8, 2012
    Applicant: SATORI PHARMACEUTICALS, INC.
    Inventors: Mark A. Findeis, Steffen P. Creaser
  • Patent number: 8258329
    Abstract: This invention provides novel compounds comprising the following anti-inflammatory pharmacore: wherein X, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Grant
    Filed: April 20, 2009
    Date of Patent: September 4, 2012
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Gary L. Bolton, Deborah A. Ferguson, Xin Jiang, Robert M. Kral, Jr., Patrick M. O'Brien, Melean Visnick
  • Patent number: 8105504
    Abstract: Organic materials which possess outstanding stability to oxidative, thermal or light-induced degradation comprise as stabilizers at least one compound of the formula (I) wherein the general symbols are as defined in claim 1. The compounds of formula I are especially useful as stabilizers for protecting polymers and lubricants against oxidative, thermal or light-induced degradation and as scavengers for oxidized developer in color photographic material.
    Type: Grant
    Filed: August 22, 2005
    Date of Patent: January 31, 2012
    Assignee: BASF SE
    Inventors: Michèle Gerster, Peter Nesvadba
  • Patent number: 8007938
    Abstract: A non-aqueous electrolyte solution is provided that realizes a large capacity, exhibits high storage characteristics and cycle characteristics, and is capable of inhibiting gas generation.
    Type: Grant
    Filed: April 19, 2005
    Date of Patent: August 30, 2011
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Minoru Kotato, Asao Kominato
  • Publication number: 20110028711
    Abstract: The instant invention provides potent antiandrogen compounds, such as 3?-acetoxyandrost-1,5-diene-17-ethylene ketal and 3?-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.
    Type: Application
    Filed: October 15, 2010
    Publication date: February 3, 2011
    Inventors: Henry A. Lardy, Ashok Marwah, Padma Marwah
  • Patent number: 7842680
    Abstract: The instant invention provides potent antiandrogen compounds, such as 3?-acetoxyandrost-1,5-diene-17-ethylene ketal and 3?-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: November 30, 2010
    Assignee: Harbor BioSciences, Inc.
    Inventors: Henry A. Lardy, Padma Marwah, Ashok Marwah
  • Publication number: 20100056487
    Abstract: As described herein, the present invention provides compounds useful for treating or lessening the severity of a neurodegenerative disorder. The present invention also provides methods of treating or lessening the severity of such disorders wherein said method comprises administering to a patient a compound of the present invention, or composition thereof. Said method is useful for treating or lessening the severity of, for example, Alzheimer's disease.
    Type: Application
    Filed: November 20, 2007
    Publication date: March 4, 2010
    Applicant: Satori Pharmaceuticals, Inc.
    Inventors: Mark A. Findeis, Steffen P. Creaser
  • Patent number: 7638509
    Abstract: The instant invention provides potent antiandrogen compounds, such as 3?-acetoxyandrost-1,5-diene-17-ethylene ketal and 3?-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: December 29, 2009
    Assignee: Hollis-Eden Pharmaceuticals, Inc.
    Inventors: Henry A. Lardy, Padma Marwah, Ashok Marwah
  • Publication number: 20090181936
    Abstract: The instant invention provides potent antiandrogen compounds, such as 3?-acetoxyandrost-1,5-diene-17-ethylene ketal and 3?-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.
    Type: Application
    Filed: March 17, 2009
    Publication date: July 16, 2009
    Applicant: Hollis-Eden Pharmaceuticals, Inc.
    Inventors: Henry A. Lardy, Ashok Marwah, Padma Marwah
  • Publication number: 20090176752
    Abstract: The instant invention provides potent antiandrogen compounds, such as 3?-acetoxyandrost-1,5-diene-17-ethylene ketal and 3?-hydroxyandrost-1,5-diene-17-ethylene ketal, and methods for their use in the prevention and treatment of biological conditions mediated by androgen receptors. Thus, for example, compounds of the invention are useful in the prevention and treatment of prostrate cancer. Furthermore, it has been discovered that compounds of the invention are useful in the prevention and treatment of androgen-independent cancers such as androgen-independent prostrate cancer. Finally, inventive compounds may be used to treat antiandrogen induced withdrawal syndrome.
    Type: Application
    Filed: March 17, 2009
    Publication date: July 9, 2009
    Applicant: Hollis-Eden Pharmaceuticals, Inc.
    Inventors: Henry A. Lardy, Ashok Marwah, Padma Marwah
  • Patent number: 7067682
    Abstract: Steroid compounds having various oxygen substitution on the steroid nucleus are disclosed. A specific functionality present on many of the steroid compounds is oxygen substitution at both of positions 6 and 7. Thus, certain steroids have oxygen substitution at C6 and C7, and some have specific stereochemistries such as 6? and 7? oxygen substitution, and an alpha hydrogen at the 5 position in addition to having 6? and 7? oxygen substitution. Steroids having 3,4-epoxy functionality are also disclosed. In addition, steroids having C17 pyran and ?-lactone functionality, with oxygen substitution at C6 and C7, or at C15, of the steroid nucleus, are disclosed.
    Type: Grant
    Filed: November 6, 2003
    Date of Patent: June 27, 2006
    Assignees: Inflazyme Pharmaceuticals Ltd., The University of British Columbia, The University of Alberta
    Inventors: David L. Burgoyne, Yaping Shen, John M. Langlands, Christine Rogers, Joseph H L Chau, Edward Piers, Hassan Salari
  • Patent number: 6982329
    Abstract: Steroids containing a cyclohexene moiety are efficiently oxidized to the corresponding ?,?-unsaturated ketone using copper iodide and t-butyl hydroperoxide. A steroid compound containing the ?,?-unsaturated ketone structure is efficiently converted to the corresponding vicinal diol using a hydroborating reagent followed by oxidative workup, e.g., borane followed by sodium perborate. Benzoyl and substituted benzoyls are superior protecting groups for hydroxyl groups present in the compounds.
    Type: Grant
    Filed: December 22, 2003
    Date of Patent: January 3, 2006
    Assignee: Inflazyme Pharmaceuticals Ltd.
    Inventors: David L. Burgoyne, Gueijun Ji, Eugene W. Kelleher, Nicholas D. Paschalides, Kishore Ramachandran, Yaping Shen, Yuanlin Zhou
  • Publication number: 20040019200
    Abstract: Disclosed herein are mixed steroidal tetraoxanes having the following structural formula 1 1
    Type: Application
    Filed: February 7, 2003
    Publication date: January 29, 2004
    Inventors: Bogdan Solaja, Dejan M. Opsenica, Gabriella Pocsfalvi, Wilbur K. Milhous, Dennis E. Kyle
  • Publication number: 20030232981
    Abstract: The present invention involves intermediates, including a 7&agr;-substituted steroid (II), 1
    Type: Application
    Filed: March 21, 2003
    Publication date: December 18, 2003
  • Patent number: 6111118
    Abstract: A procedure for oxidizing organic compounds having allylic hydrogen atom(s) involving the steps of reactively contacting the organic compound with a combination of a periodic acid or metal periodate and an alkyl hydroperoxide under conditions of normal as well as elevated pressure of a suitable gas like air. The reaction can conveniently be conducted at temperatures between about 0-65.degree. C. in a cosolvent system of water and organic solvent(s).
    Type: Grant
    Filed: January 11, 1999
    Date of Patent: August 29, 2000
    Assignee: Humanetics Corporation
    Inventors: Padma Marwah, Henry A. Lardy
  • Patent number: 6107036
    Abstract: Compounds of the general formula Ia and Ib are described ##STR1## in which R.sup.1 and R.sup.2 are the same or different and represent hydrogen, straight-chain or branched C.sub.1 to C.sub.6 lower alkyl or an aryl group optionally substituted by electron-withdrawing groups, R.sup.3 denotes a cleavable group, W is hydrogen, halogen or a pseudohalogen and at least one of the groups R.sup.4 or R.sup.5 is a group stabilizing the dioxetane structure and at most one of the groups R.sup.4 or R.sup.5 represents hydrogen and X or Y represents oxygen, N-R or C(R).sub.2 in which R has the meanings stated for R.sup.1 and R.sup.2 or represents a mesomeric double bond or a carbonyl group and n denotes the number 0 or 1 and m denotes the number 1 or 2, as well as a process for their production. These compounds are new and can be used as substrates in immunological assays and in DNA diagnostics using activating agents for colour formation.
    Type: Grant
    Filed: April 20, 1998
    Date of Patent: August 22, 2000
    Assignee: Roche Diagnostics GmbH
    Inventors: Dieter Heindl, Hans-Peter Josel, Herbert Von Der Eltz, Rupert Herrmann, Hans-Joachim Holtke, Rainer Beckert, Dieter Weiss, Waldemar Adam
  • Patent number: 5869709
    Abstract: A procedure for oxidizing organic compounds having allylic hydrogen atom(s) involving the steps of reactively contacting the organic compound with a combination of an alkali metal periodate and an alkyl hydroperoxide. The reaction can conveniently be conducted under ambient temperature and pressure conditions, and is conveniently conducted in a cosolvent system of water and organic solvent(s).
    Type: Grant
    Filed: May 7, 1997
    Date of Patent: February 9, 1999
    Assignee: Humanetics Corporation
    Inventors: Padma Marwah, Henry A. Lardy
  • Patent number: 5831104
    Abstract: The invention is directed to novel steroid intermediate products of general formula I ##STR1## The steroid intermediate products which can be isolated according to the invention are suitable for the synthesis of 13-ethyl-11-methylene-18,19-bisnor-17.alpha.-pregn-4-en-20-in-17-ol (desogestrel).Further, processes for producing the steroid intermediate products of general formula I are described. The olefination of the 11-oxo steroids is carried out under the influence of ultrasound.
    Type: Grant
    Filed: September 9, 1994
    Date of Patent: November 3, 1998
    Assignee: Jenapharm GmbH
    Inventors: Sven Ring, Gerhard Teichmueller, Gisela Weber, Sigfrid Schwarz, Bernd Erhart, Bernd Undeutsch, Harald Raethe, Peter Moellmann, Carmen Pfeiffer, Hans-Joachim Palme
  • Patent number: 5756722
    Abstract: The novel intermediates of the formula ##STR1## wherein L, K and M are as defined in the specification which are useful intermediates for the preparation of .DELTA..sup.4,9(11),16 -pregnatriene-3-ones.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: May 26, 1998
    Assignee: Roussel Uclaf
    Inventors: Francis Brion, Jean Buendia, Christian Diolez, Michel Vivat
  • Patent number: 5723455
    Abstract: Novel antiandrogenic agents are provided. An exemplary group of compounds has the structural formula (I) ##STR1## wherein R.sup.1 through R.sup.10, a and b are as defined herein. Pharmaceutical compositions and methods for using the compounds of formula (I) to treat androgen-related clinical conditions are provided, as are methods and compositions for using the compounds as contraceptive agents.
    Type: Grant
    Filed: March 11, 1997
    Date of Patent: March 3, 1998
    Assignee: SRI International
    Inventors: Masato Tanabe, Wan-Ru Chao, Wesley K. M. Chong, David F. Crowe
  • Patent number: 5708164
    Abstract: Synthetically produced cephalostatin analogues of the formula I described in the disclosure, synthetic methods for preparing the cephalostatin analogues, pharmaceutical compositions containing the analogues and methods for using the analogues as active agent in pharmaceutical uses, particularly due to their cytotoxic activity.
    Type: Grant
    Filed: June 6, 1996
    Date of Patent: January 13, 1998
    Assignee: Schering Aktiengesellschaft
    Inventors: Ekkehard Winterfeldt, Andreas Kramer, Ulrike Ullmann, Henry Laurent
  • Patent number: 5523428
    Abstract: A process for the production of 1-methyl-3-keto-.DELTA..sup.1,4 steroids of general formula I ##STR1## in which St symbolizes the radical of asteroid molecule, where a 3-keto-.DELTA..sup.1,4 steroid of general formula II ##STR2## in which St has the above-mentioned meaning, is reacted in an inert solvent in the presence of a nickel salt soluble therein with an organometallic compound of formula III, IV or V ##STR3## where X, Y.sub.1, Y.sub.2, Y.sub.3, Z.sub.1 and Z.sub.2 are as defined in the specification.
    Type: Grant
    Filed: April 18, 1995
    Date of Patent: June 4, 1996
    Assignee: Schering Aktiengesellschaft
    Inventors: Jurgen Westermann, Klaus Nickisch, Annette Prelle
  • Patent number: 5200518
    Abstract: Compounds of the formula: ##STR1## wherein X is H, F, Cl, or CH.sub.3and Y is ##STR2## wherein R.sub.1 is H, alkyl of 1-5 carbon atoms, phenyl, or benzyl;R.sub.2 is COOR.sub.6, R.sub.5 COOR.sub.6, or R.sub.5 CONHR.sub.6 ;R.sub.3 is H, F, OH, or CH.sub.3 ;R.sub.4 is CH.sub.2 OH, CH.sub.2 OCOR.sub.6, COOR.sub.6, or CONHR.sub.6 ;R.sub.5 is alkyl of 1-3 carbon atoms;R.sub.6 is alkyl of 1-5 carbon atoms, or benzyl;represents a single or double bond;.about. represents .alpha.-position, .beta.-position, or a mixture of both .alpha.- and .beta.-positions; and-- represents .alpha.-position;and methods for preparing the same.
    Type: Grant
    Filed: February 21, 1991
    Date of Patent: April 6, 1993
    Assignee: Kangweon National University
    Inventors: Hyun P. Kim, Kwan S. Sin, Chang M. Kim, Moon Y. Heo, Henry J. Lee
  • Patent number: 5194602
    Abstract: New 9.alpha.-hydroxy-17-methylene steroids are prepared by the introduction of a substituted 17-methylene group in 9.alpha.-hydroxyandrost-4-ene-3, 17-dione.The resulting compounds are useful starting compounds in the synthesis of corticosteroids.
    Type: Grant
    Filed: December 12, 1990
    Date of Patent: March 16, 1993
    Assignee: Gist-Brocades N.V.
    Inventors: Jacobus N. M. Batisi, Arthur F. Marx
  • Patent number: 5093490
    Abstract: The invention relates to a process for the production of (+)-bicyclo[3.3.0]octan-3-one-2 carboxylic acid steroid esters of formula I ##STR1## in which X means oxygen or the radicals --O--(CH.sub.2).sub.n --O-- or --O--CH.sub.2 --C(CH.sub.3).sub.2 --CH.sub.2 --O--,n means 2 or 3R.sub.2 means hydrogen or methyl,Y means the radicals X or X.sub.1,X.sub.1 means the radicals OCH.sub.3 or OCOR.sub.3,R.sub.3 means methyl, ethyl, phenyl, benzyl or pivalyl and the radical ##STR2## the radicals ##STR3## and X and X.sub.1 have the meanings indicated above, characterized in that D,L-bicyclo[3.3.0]octan-3-one-2 carboxylic acid esters of formula II ##STR4## in which X has the meaning indicated above and R is an alkyl group with 1-4 carbon atoms, with optically active steroids with a free 17'beta hydroxy group of formula III ##STR5## in which R.sub.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: March 3, 1992
    Assignee: Schering Aktiengesellschaft
    Inventor: Helmut Vorbrueggen
  • Patent number: 4762919
    Abstract: Compounds of the formula: ##STR1## wherein one X is COOR, CH.sub.2 COOR, CH(COOR).sub.2, CONHR, CH.sub.2 CONHR, or CNremaining X's are H, F, CH.sub.3, OH, COOR, CH.sub.2 COOR, CH(COOR).sub.2, CONHR, CH.sub.2 CONHR, or CN;Y is ##STR2## R is H, alkyl of 1-5 carbon atoms, or benzyl; R.sub.1 is CH.sub.2 OR.sub.3, COOR, or CONHR;R.sub.2 is H, OR.sub.3, or BR;R.sub.3 is H, COR.sub.4, or tetrahydropyranyl;R.sub.4 is alkyl of 1-5 carbon atoms or benzyl;R.sub.5 is H or COR.sub.4 ;represents a single or double bond;represents .alpha.-position, .beta.-position, or a mixture of .alpha.- and .beta.-positions; and--- represents .alpha.-position;and methods for preparing the same.
    Type: Grant
    Filed: February 12, 1986
    Date of Patent: August 9, 1988
    Assignee: Florida Agricultural and Mechanical University
    Inventor: Henry J. Lee
  • Patent number: 4622181
    Abstract: A process of preparing radical anions which comprises reacting sodium and a polycyclic aromatic compound in a reaction solvent to prepare radical anions and supplying androstane-1,4-diene-3,17-dione-17-acetal into the obtained reaction mixture to reduce the same into an estrone acetal, characterized in that a solvent comprising polyethers having three or more ether bonds and maintained at a concentration higher than a predetermined value is used as the reaction solvent and the reaction is carried out at a temperature of from the melting point of sodium to 105.degree. C. The process according to this invention can produce an estrone acetal at a high yield and with economical advantages in the industrial scale and the estrone acetal thus obtained is useful as an estrone precursor which is important as a female hormone.
    Type: Grant
    Filed: September 21, 1984
    Date of Patent: November 11, 1986
    Assignee: Mitsubishi Chemical Industries Ltd.
    Inventors: Kazumasa Kinugasa, Eiichiro Tanaka, Yoshihiro Tanaka, Yoshiharu Morita