Additional Unsaturation In The Cyclopentanohydrophenanthrene Ring System Patents (Class 552/640)
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Patent number: 8586770Abstract: The invention relates to methods to manipulate stem cells in vivo and in vitro to treat, e.g., a condition where cell or tissue repair is needed.Type: GrantFiled: February 18, 2011Date of Patent: November 19, 2013Assignee: Harbor Therapeutics, Inc.Inventor: James M. Frincke
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Patent number: 8541609Abstract: A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R1, R2, R3, R4, independently, is hydrogen, halogen or C1-C6 alkyl. In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherein R1, R2, R3, R4 are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R5SO2X wherein R5 is C1-C5 alkyl and X is halogen so as to obtain a compound of formula (III) wherein R1, R2, R3, R4, R5 are as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).Type: GrantFiled: April 19, 2012Date of Patent: September 24, 2013Assignee: Cedarburg Pharmaceuticals, Inc.Inventors: Kevin Kunnen, Nathan W. Stehle, Scot W. Weis, John M. Pascone, Richard J. Pariza, Scott G. Van Ornum, Paul Zizelman
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Publication number: 20120209016Abstract: A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R1, R2, R3, R4, independently, is hydrogen, halogen or C1-C6 alkyl. In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherein R1, R2, R3, R4 are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R5SO2X wherein R5 is C1-C5 alkyl and X is halogen so as to obtain a compound of formula (III) wherein R1, R2, R3, R4, R5 are as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).Type: ApplicationFiled: April 19, 2012Publication date: August 16, 2012Inventors: Kevin Kunnen, Nathan W. Stehle, Scot W. Weis, John M. Pascone, Richard J. Pariza, Scott G. Van Ornum, Paul Zizelman
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Patent number: 8183401Abstract: A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R1, R2, R3, R4, independently, is hydrogen, halogen or C1-C6 alkyl. In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherein R1, R2, R3, R4 are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R5SO2X wherein R5 is C1-C5 alkyl and X is halogen so as to obtain a compound of formula (III) wherein R1, R2, R3, R4, R5 are as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).Type: GrantFiled: January 14, 2005Date of Patent: May 22, 2012Assignee: Cedarburg Pharmaceuticals, Inc.Inventors: Kevin Kunnen, Nathan W. Stehle, Scot W. Weis, John M. Pascone, Richard J Pariza, Scott G. Van Ornum, Paul Zizelman
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Publication number: 20110009615Abstract: An object of the present invention is to provide a novel method for producing a steroid compound. The present invention provides a method for producing 3,7-dioxo-5?-cholanic acid or ester derivatives thereof, which uses, as raw materials, sterols having double bonds at positions 5 and 24, such as cholesta-5,7,24-trien-3?-ol, ergosta-5,7,24(28)-trien-3?-ol, desmosterol, fucosterol, or ergosta-5,24(28)-dien-3?-ol, and which comprises the following 4 steps: (I) a step of performing oxidation of a hydroxyl group at position 3 and isomerization of a double bond at position 5 to position 4; (II) a step of converting position 24 to a carboxyl group or an ester derivative thereof by the oxidative cleavage of a side chain; (III) a step of introducing an oxygen functional group into position 7; and (IV) a step of constructing a 5?-configuration by reduction of a double bond at position 4.Type: ApplicationFiled: June 30, 2010Publication date: January 13, 2011Applicant: MITSUBISHI CHEMICAL GROUP SCIENCE AND TECHNOLOGY RESEARCH CENTER, INC.Inventors: Jun Takehara, Naoya Fujiwara, Junya Kawai, Kyouko Endou, Kiyoshi Ooyama
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Patent number: 7846918Abstract: 6-Methyloxaalkyl exemestane compounds and related compositions, as can be used, chemotherapeutically, to inhibit growth and proliferation of cancer cells.Type: GrantFiled: October 2, 2006Date of Patent: December 7, 2010Assignee: Endece, LLCInventors: Richard J. Pariza, James G. Yarger
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Patent number: 5969168Abstract: The invention relates to novel, androstane steroids which are the ligand semiochemicals which bind to neuroepithelial receptors. The steroids are useful as ligands to neuroepithelial receptors in the human vomeronasal gland to stimulate autonomic and hypothalamic activity.Type: GrantFiled: September 29, 1994Date of Patent: October 19, 1999Assignee: Pherin CorporationInventors: David L. Berliner, Nathan W. Adams, Clive L. Jennings-White
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Patent number: 5925630Abstract: The invention relates to 3.alpha.-hydroxy, 17-(un)substituted derivatives of the androstane series and 3.alpha.-hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at a recently identified site on the GRC, thereby modulating brain excitability in a manner that will alleviate stress, anxiety, insomnia, mood disorders that are amenable to GRC-active agents (such as depression) and seizure activity. The steroid derivatives of this invention are those having the general structural Formula: ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are further defined herein and the dotted lines are single or double bonds. The structure includes androstanes, pregnanes (R.sub.4 =methyl), 19-norandrostanes, and norpregnanes (R.sub.4 =H).Type: GrantFiled: June 6, 1996Date of Patent: July 20, 1999Assignee: CoCensys, Inc.Inventors: Ravindra B. Upasani, David B. Fick, Derk J. Hogenkamp, Nancy C. Lan
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Patent number: 5866558Abstract: Compounds of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are inhibitors of aromatase, and are useful for treating diseases such as breast cancer, in mammals. Also disclosed are pharmaceutical compositions, processes for preparing compounds of formula (I) and intermediates useful for preparing compounds of formula I.Type: GrantFiled: May 8, 1997Date of Patent: February 2, 1999Assignee: Regents of the University of MinnesotaInventors: Yusuf J. Abul-Hajj, Abraham Akanni
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Patent number: 5723455Abstract: 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: GrantFiled: March 11, 1997Date of Patent: March 3, 1998Assignee: SRI InternationalInventors: Masato Tanabe, Wan-Ru Chao, Wesley K. M. Chong, David F. Crowe
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Patent number: 5597701Abstract: A process and appropriate device are disclosed for determining the androstenone content of adipose tissues in clearly shorter times. The disclosed process has the following steps: (a) liquefying an adipose tissue sample by heating up to a predetermined temperature in the 45.degree. to 60.degree. C.Type: GrantFiled: March 7, 1995Date of Patent: January 28, 1997Assignee: Riedel-De Haen AktiengesellschaftInventors: Rolf P. Claus, Martin Dehnhard
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Patent number: 4946834Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase. Also invented are intermediates used in preparing these compounds.Type: GrantFiled: December 23, 1988Date of Patent: August 7, 1990Assignee: SmithKline Beecham CorporationInventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
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Patent number: 4917827Abstract: 9(11)-dehydroandrostanes and 9(11)-dehydropregnanes are prepared by dehydrating the corresponding 9-alpha-hydroxy steroid in the presence of a Lewis acid. The corresponding 8(9)-dehydro-isomer was not detectable. The resulting products are valuable intermediates in steroid synthesis especially in the preparation of corticosteroids.Type: GrantFiled: June 10, 1988Date of Patent: April 17, 1990Assignee: Gist-Brocades N.V.Inventors: Jacobus N. M. Batist, Nicolaas C. M. E. Barendse, Arthur F. Marx
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Patent number: RE33364Abstract: The present invention discloses a process for the production of androsta-4,9(11)-diene-3,17-dione type compounds from 9.alpha.-hydroxyandrostenedione type compounds by non-aromatic oxygenated strong acid dehydration.Type: GrantFiled: April 14, 1988Date of Patent: October 2, 1990Assignee: The Upjohn CompanyInventors: John M. Beaton, Joel E. Huber, Amphlett G. Padilla, Max E. Breuer