Unsaturation Between The 5- And 10-positions Patents (Class 552/644)
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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: 7696190Abstract: The invention makes a 16?-substituted steroidal compound available having formula 1, wherein the dotted ring is a fully saturated, a fully aromatic or a saturated ring with a ?5-10 double bond; R1 is (C1-C3)alkyl or (C2-C3)alkenyl, and each of these groups can be substituted with one or more halogens; R2 is (C1-C4;)alkyl, (C2-C4)alkenyl or methylene, and each of these groups can be substituted with one or more halogens; R3 is methyl or ethyl; or a prodrug thereof, which compound can be used for an estrogen receptor ? selective treatmentType: GrantFiled: July 23, 2001Date of Patent: April 13, 2010Assignee: N.V. OrganonInventors: Jordi Mestres, Hubert Jan Jozef Loozen, Gerrit Herman Veeneman
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Patent number: 7361645Abstract: The invention relates to 11?-halogen steroids with general formula (I), whereby R11 is halogen, X—Y-Z represents a group with one of the two structures CH?C—C or CH2—C?C and the other radicals have the meaning that is indicated in the claims, also the production and use of these compounds for the production of pharmaceutical agents as well as pharmaceutical preparations that contain 11?-halogen steroids.Type: GrantFiled: January 24, 2002Date of Patent: April 22, 2008Assignee: Bayer Schering Pharma AGInventors: Rolf Bohlmann, Hermann Kuenzer, Reinhard Nubbemeyer, Dieter Zopf
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Patent number: 6989378Abstract: The invention is the novel androgen (7?,17?)-7-methyl-17-[(1-oxoundecyl)oxy]estr-4en-3one (MENT undecanoate). This compound distinguishes favourably from other testosterone derivatives in that it has a good solubility in oily media. It particularly exhibits a good dissolved potency relative to testosterone. The compound is particularly suitable for administration by means of injection.Type: GrantFiled: October 13, 2004Date of Patent: January 24, 2006Assignee: Akzo Nobel N.V.Inventors: Dirk Leysen, Hendrikus Adrianus Antonius Van Der Voort
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Patent number: 6677329Abstract: Disclosed are novel, selective estrogens type having a steroid skeleton with a non-aromatic A-ring and a free or capped hydroxyl group at carbon atom No. 3. The estrogens satisfy general formula (I), in which R1 is H, (C1-C3)alkyl or (C2-C3)acyl; R2 is H, &agr;-(C1-C4)alkyl, &agr;-(C2-C4)alkenyl or &agr;-(C2-C4)alkynyl; R3 is H or (C1-C4)alkyl, (C2-C4)alkenyl or (C2-C4)alkynyl, each at location 15 or 16 of the steroid skeleton; R4 is H or (C1-C5)alkyl, (C2-C5)alkenyl or (C2-C5)alkynyl, each optionally substituted with halogen; preferred is ethynyl; R5 is H, (C1-C3)alkyl or (C2-C3)acyl; R6 is (C1-C5)alkyl, (C2-C5)alkenyl, (C2-C5)alkynyl or (C1-C5)alkylidene, each optionally substituted.Type: GrantFiled: May 29, 2002Date of Patent: January 13, 2004Assignee: Akzo Nobel N V.Inventors: Hubert Jan Jozef Loozen, Gerrit Herman Veeneman, Wilhelmus Gerardus Eduardus Joseph Schoonen
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Patent number: 6649779Abstract: This invention provides a pharmaceutically acceptable salt of 3&bgr;-hydroxy-5(10)-estrene-17-one 3-sulfate ester and a pharmaceutically acceptable salt of 3&agr;-hydroxy-5(10)-estrene-17-one 3-sulfate ester, which are useful as an estrogens.Type: GrantFiled: June 5, 2002Date of Patent: November 18, 2003Assignee: WyethInventors: Michael Z. Kagan, Fangming Kong, Leonard A. McDonald, Panolil Raveendranath, Syed M. Shah, Joseph Zeldis
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Patent number: 6458778Abstract: This invention provides estra-5(10),7-dien-3&bgr;-ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3&bgr;-ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-dien-3&agr;-ol-17-one or a pharmaceutically acceptable salt of its 3-sulfate ester, estra-5(10),7-dien-3&bgr;-ol-17-one 3-glucuronide or a pharmaceutically acceptable salt thereof, estra-5(10),7-dien-3&bgr;-ol-17-one 3-alkali metal salt, and estra-5(10),7-dien-3&agr;-ol-17-one 3-alkali metal salt which are useful as estrogenic agents.Type: GrantFiled: March 27, 1998Date of Patent: October 1, 2002Assignee: WyethInventors: Fangming Kong, Leonard A. McDonald, Michael Z. Kagan, Syed M. Shah, Panolil Raveendranath, Mark A. Collins
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Patent number: 5994568Abstract: The invention relates to estrene steroids, which bind to neuroepithelial receptors. The steroid is preferably administered in the form of a pharmaceutical composition containing one or more pharmaceutically acceptable carriers.Type: GrantFiled: June 6, 1995Date of Patent: November 30, 1999Assignee: Pherin CorporationInventors: David L. Berliner, Nathan W. Adams, Clive L. Jennings-White
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Patent number: 4923640Abstract: A process for the production of 17.alpha.-ethinyl-17.beta.-hydroxy-18-methyl-4,15-estradien-3-one is described comprising reacting a 17-enolester of formula II ##STR1## wherein R.sub.1 represents an alkyl radical with 1-3 carbon atoms andR.sub.2 represents an acyl or a trialkylsilyl group with 1-10 carbon atomsunder palladium catalysis, with compounds of formula II ##STR2## wherein R.sub.1 represents an alkyl radical with 1-3 carbon atoms, reducing the 17-keto group to the 17-hydroxy group in a manner known in the art, reducing the aromatic A-ring according to Birch, with liquid ammonia, to 3-methoxy-2,5(10),15-estratrien-17.beta.-ol, reoxidizing the 17-hydroxy group to the 17-keto group, ethinylating the 17-keto group and splitting off the 3-enolether to form 17.alpha.-ethinyl-17.beta.-hydroxy-18-methyl-4,15-estradiene-3-one.Type: GrantFiled: March 31, 1988Date of Patent: May 8, 1990Assignee: Schering AktiengesellschaftInventors: Rolf Bohlmann, Henry Laurent, Helmut Hofmeister, Rudolf Wiechert
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Patent number: 4921845Abstract: 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: GrantFiled: December 8, 1988Date of Patent: May 1, 1990Assignee: Akzo N.V.Inventors: Hendrick Paul de Jongh, Nicolaas P. van Vliet