17 Alpha-position Substituted (e.g., 17 Alpha-alkynylandrosta-4, 6-diene 3,17-diols, Etc.) Patents (Class 552/639)
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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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Publication number: 20130012573Abstract: A method for intracellular delivery of isolated naked nucleic acids into a biological tissue or organ, that includes (a) contacting the tissue or organ with an efficient amount of at least one active corticosteroid, and (b) contacting the tissue or organ treated in step b with an efficient amount of isolated naked nucleic acids, wherein step (a) is carried out for a period of time ranging from at least five minutes to at most two hours and being immediately followed by step (b).Type: ApplicationFiled: January 14, 2011Publication date: January 10, 2013Applicant: UNIVERSITE PARIS DESCARTESInventors: Francine Behar-Cohen, Elodie Touchard
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Publication number: 20110301363Abstract: The invention relates to a method for carrying out an oxidation reaction for producing a product by heating a reaction medium containing a reactant and oxygen or an oxygen carrier in a reactor, wherein the reaction medium is brought into contact with a solid heating medium which may be heated by electromagnetic induction, which is surrounded by the reaction medium. The heating medium is heated by electromagnetic induction using an inductor, wherein an oxidation reaction is carried out on the first reactant to give a product and the product is separated from the heating medium. The inductor preferably generates an alternating field with a frequency in the range 1 to 100 kHz, preferably in the range 10 to 80 kHz and in particular up to 50 kHz.Type: ApplicationFiled: August 16, 2011Publication date: December 8, 2011Inventors: Carsten FRIESE, Andreas Kirschning, Sascha-Volkan Ceylan
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Publication number: 20110262540Abstract: A solid pharmaceutical composition of exemestane, in particular for oral use and treatment of cancer, comprises micronized exemestane and anti-oxidant in a film-coated tablet.Type: ApplicationFiled: July 27, 2009Publication date: October 27, 2011Applicant: ARROW INTERNATIONAL LIMITEDInventors: Peter Henry Robert Persicaner, Rahul Sareen
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Patent number: 7196074Abstract: Methods of using 7?,11?-dimethyl-17?-hydroxyestra-4,14-dien-3-one (III) and 17 esters thereof for various hormonal therapies, oral and parenteral dosage forms comprising these actives, and processes for their preparation.Type: GrantFiled: October 28, 2002Date of Patent: March 27, 2007Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Richard P. Blye, Hyun K. Kim, Pemmaraju Narasimha Rao, Carmie Kirk Acosta
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Patent number: 6780854Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C,1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.Type: GrantFiled: October 24, 2002Date of Patent: August 24, 2004Assignee: Akzo Nobel NVInventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
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Patent number: 6756366Abstract: Orally Active androgens are derivative of 7&agr;-methyl-19-nortestosterone. The compounds satisfy formula (I) wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6)alkyl, or (C1-6)acyl; R2 is selected from the group consisting of (C2-3)alkyl, isopropyl, (C2-3)1-alkenyl, isopropenyl, 1,2-proandienyl, or (C2-3)1-alynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2)alkyl, or halogen; R3 is hydrogen, (C1-2)alkyl, or ethenyl; R4 is (C1-2)alkyl; R5 is hydrogen, or (C1-15)acyl; and the dotted lines indicate optional bonds.Type: GrantFiled: September 24, 2001Date of Patent: June 29, 2004Assignee: Akzo Nobel N.V.Inventors: Jaap van der Louw, Dirk Leysen, Roberta Burma Bursi
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Publication number: 20030134831Abstract: A compound is provided for increasing the concentration of a parent androgen in a subject in vivo. The parent androgen has a skeletal structure including a 4 position and a 17 position. It has a 17&bgr;-hydroxy group that includes a 17&bgr;-hydroxy oxygen appended to the 17 position and a 17&bgr;-hydroxy hydrogen appended to the 17&bgr;-hydroxy oxygen. The compound includes a substrate having the skeletal structure of the parent androgen, wherein the substrate includes a 4 position and a 17 position corresponding to the 4 and 17 positions respectively of the parent androgen. The substrate according to one aspect of the invention includes a carbon-carbon double bond at the 4 position. The skeletal structure of the parent androgen embodied in the substrate being selected from the group consisting of androst-4-ene-3&agr;,17&bgr;-diol, androst-4-ene-3&bgr;,17&bgr;-diol, and mixtures thereof, or estr-4-ene-3&agr;,17&bgr;-diol, estr-4-ene-3&bgr;,17&bgr;-diol, and mixtures thereof, or combinations of these.Type: ApplicationFiled: January 16, 2002Publication date: July 17, 2003Inventor: William J. Roberts
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Publication number: 20030134830Abstract: A compound is provided for increasing the concentration of a parent androgen in a subject in vivo. The parent androgen has a skeletal structure including a 1 position and a 17 position, a 17&bgr;-hydroxy group comprising a 17&bgr;-hydroxy oxygen appended to the 17 position, and a 17&bgr;-hydroxy hydrogen appended to the 17&bgr;-hydroxy oxygen. The compound includes a substrate having the skeletal structure of the parent androgen. It includes a 1 position and a 17 position corresponding to the 1 and 17 positions respectively of the parent androgen. The substrate has a carbon-carbon double bond at the 1 position. The compound also has a promoiety appended to the 17&bgr;-hydroxy oxygen of the substrate as a substitute for the 17&bgr;-hydroxy hydrogen of the parent androgen. The promoiety includes, and preferably consists of, an alkylcarbonate ester. A related method also is provided.Type: ApplicationFiled: January 16, 2002Publication date: July 17, 2003Inventor: William J. Roberts
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Patent number: 6541465Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.Type: GrantFiled: July 31, 2001Date of Patent: April 1, 2003Assignee: Akzo Nobel N.V.Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
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Patent number: 6406718Abstract: The invention relates to a new polymorphic crystalline form of S-fluoromethyl 6&agr;,9&agr;-difluoro-11&bgr;-hydroxy-16&agr;-methyl-3-oxo-17&agr;-propionyloxyandrosta-1,4-diene-17&bgr;-carbothiate (fluticasone propionate). The new polymorphic crystalline form is easily handled and easily fluidised and its particle size and shape can be controlled. The invention also relates to the use of this new material in therapy, particularly in the treatment of respiratory disorders, e.g. asthma.Type: GrantFiled: April 15, 1999Date of Patent: June 18, 2002Assignee: SmithKline Beecham CorporationInventor: Simon Murray Cooper
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Patent number: 6313108Abstract: Novel, orally active androgens are 7&agr;-substituted &Dgr;14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1-6) alkyl, or (C1-6) acyl; R2 is selected from the group consisting of (C2-4) alkyl, (C2-4) alkenyl, or (C2-4) alkynyl, each optionally substituted by halogen; or R2 is cyclopropyl, or cyclopropenyl, each optionally substituted by (C1-2) alkyl, or halogen; R3 is hydrogen, (C1-2) alkyl, or ethenyl; R4 is (C1-2) alkyl; R5 is hydrogen, or (C1-15) acyl; and the dotted lines indicate optional bonds.Type: GrantFiled: July 11, 2000Date of Patent: November 6, 2001Assignee: Akzo Nobel N.V.Inventors: Hubert Jan Jozef Loozen, Dirk Leysen, Jaap van der Louw
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Patent number: 5977096Abstract: Novel substituted steroid compounds are disclosed which are more effective than known radical-trapping agents in methods of prophylaxis and therapy of radical-mediated cell damage and of treatment of diseases due to radical-mediated cell damage. The novel substituted steroid compounds can be made from steroids having an estrane, androstane, pregnane or cholestane basic skeleton and have a radical-attracting aromatic substituent of the general formula --(CH.sub.2).sub.n X, or .dbd.CH--(CH.sub.2).sub.m X at the 17 or 6 position of the steroid nucleus, wherein X=Y, OY, SY, SeY or NHY; n=0 to 5; m=n-1 and Y is a phenyl group having five substituents A, B, C, D and E, wherein A to E is independently H, alkyl, Oalkyl, Oacyl, OH, or one of the substituents B, C or D is NR.sub.2 wherein R=alkyl and each of the other substituents is hydrogen. Pharmaceutical compositions containing the novel substituted steroid compounds and methods of making them are also part of the invention.Type: GrantFiled: February 20, 1999Date of Patent: November 2, 1999Assignee: Jenapharm GmbH & Co. KGInventors: Peter Droescher, Bernd Menzenbach, Kurt Ponsold, Bernd Undeutsch, Michael Oettel, Wolfgang Romer, Gunter Kaufmann, Jens Schroder
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Patent number: 5952319Abstract: An androgenic steroid compound of the formula: ##STR1## wherein: X, Y, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are as defined herein.Type: GrantFiled: November 26, 1997Date of Patent: September 14, 1999Assignee: Research Triangle InstituteInventors: C. Edgar Cook, John A. Kepler, Yue-Wei Lee, Mansukh C. Wani
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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: 5438134Abstract: The unsaturated 17.alpha.-cyanomethyl-17.beta.-hydroxy steroids of the formula I, ##STR1## in which R.sub.1 =Me, Eth; R.sub.2 =H, Me; R.sub.3 =H, OH, an acetoxy or alkoxy group; R.sub.4 =H, R.sub.5 =OH, an acetoxy, alkoxy group of R.sub.4 and R.sub.5 together represent a keto- or ketal group and double bonds are contained in the basic structure of the steroid, particularly between the 15 and 16 position in the steroid ring, from unsaturated 17-ketosteroids of the general formula II as described herein with the aforementioned meanings of R.sub.1 to R.sub.5 by reacting the unsaturated 17-ketosteroids with LiCH.sub.2 CN and subsequently hydrolyzing.The compounds of formula I are pharmacologically interesting steroid compounds or also intermediate products for the synthesis of highly-effective steroid products which can be used in human and veterinary medicine for the treatment of endocrine disorders and for reproductive control based on their specific hormonal/anti-hormonal actions.Type: GrantFiled: June 1, 1993Date of Patent: August 1, 1995Assignee: Jenapharm GmbHInventors: Gerhard Teichmuller, Gerd Muller
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Patent number: 5081113Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.6 is selected from the group consisting of halogen, --CH.sub.3, fluorine and chlorine, R.sub.9 and R.sub.11 together form a second bond at 9(11) or R.sub.9 is hydrogen or fluorine and R.sub.11 is selected from the group consisnting of hydrogen, --OH and .dbd.O, the dotted lines in rings A and B indicate a possible additonal bond at 1(2) and 6(7), R.sub.17 is hydrogen or acyl or an organic carboxylic acid of 1 to 18 carbon atoms, R'.sub.17 is ##STR2## Z is selected from the group consisting of a single bond, alkylene of 1 to 5 carbon atoms and alkenylene and alkynylene of 2 to 5 carbon atoms, P is pyrimidinyl or pyridyl optionally substituted with one or two individual members of the group consisting of --NH.sub.Type: GrantFiled: March 21, 1990Date of Patent: January 14, 1992Assignee: Roussel UclafInventors: Andre Claussner, Jacques Leclaire, Lucien Nedelec, Daniel Philibert
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Patent number: 5068368Abstract: A process for the preparation of ethynyl carbinols of the formula: ##STR1## wherein R" is hydrogen, a substituted or unsubstituted aliphatic or aromatic hydrocarbon, R'" is a substituted or unsubstituted aliphatic or aromatic hydrocarbon or R" and R'" together to the carbon atom to which they are joined represent a steroid, which comprises the steps ofA. reacting in a solvent system comprising an aromatic hydrocarbon, at least one lithium alkylamide selected from the group consisting of: ##STR2## wherein R is a hydrogen or lower alkyl, R' is hydrogen, lower alkyl, a substituted or unsubstituted aliphatic, alicyclic or aromatic hydrocarbon, x is an integer of 2 to 8, y and z are each 0 to 1, with acetylene to form a monolithium acetylideB. reacting in a solvent system comprising an aromatic hydrocarbon, the monolithium acetylene from Part A with a ketone of the formula R"R'"C.dbd.O, wherein R" and R'" are as hereinbefore defined, and thenC.Type: GrantFiled: May 10, 1990Date of Patent: November 26, 1991Assignee: Cyprus Foote Mineral CompanyInventors: W. Novis Smith, Christopher Louer
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Patent number: 4945064Abstract: Estrane and androstane derivatives of formula I ##STR1## wherein X is bromine, iodine, triphenyltin or trialkyltin of 1 to 6 carbon atoms per alkyl radical,Y represents two hydrogen atoms or methylene,Z represents two hydrogen atoms, oxo or alkylenedioxy of 2 to 6 carbon atoms andV is ethylene, vinylene, 1,3-propylene or cyclopropylene,R.sub.1 is hydrogen or a hydrocarbon radical of up to 8 hydrocarbon atoms, optionally interrupted by an oxa group or substituted by an oxo group,R.sub.2 is methyl or ethyl,R.sub.3 and R.sub.4 represent a carbon-carbon bond or R.sub.3 is hydrogen and R.sub.4 is hydrogen or methyl,.DELTA.symbolizes a 4(5)-double bond if Z signifies two hydrogen atoms or an oxo group; or a 5(6)-double bond or, for the estrane derivatives of formula I, also a 5(10)-double bond, if Z is alkylenedioxy,are pharmacologically effective substances or intermediates for preparation thereof.Type: GrantFiled: January 19, 1988Date of Patent: July 31, 1990Assignee: Schering AktiengesellschaftInventors: Helmut Hofmeister, Henry Laurent, Paul E. Schulze, Klaus Annen, Rudolf Wiechert, Kunhard Pollow, Bernhard Manz, Hans-Joerg Grill