Oxygen Bonded Directly At The 1-, 2- Or 4-position Patents (Class 552/560)
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Publication number: 20090291933Abstract: The invention provides and describes solid state 17?-ethynyl-androst-5-ene-3?,7?,17?-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17?-ethynyl-androst-5-ene-3?,7?,17?-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17?-ethynyl-androst-5-ene-3?,7?,17?-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17?-ethynyl-androst-5-ene-3?,7?,17?-triol and uses of such formulations in treating the described conditions.Type: ApplicationFiled: April 3, 2009Publication date: November 26, 2009Applicant: Hollis-Eden Pharmaceuticals, Inc.Inventors: Steven K. White, Igor Ivanisevic, Kyle Stephens, Mark Andres, Brenton Skylar Wolfe
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Publication number: 20020147355Abstract: The invention provides a process for the isolation of 2-deoxy ecdysterone from Zoanthus sp process comprising the steps (a) preparing crude methanol extract of Zoanthus sp., (b)subjecting the crude methanol extract to fractionation using petroleum ether, ethyl acetate, chloroform, n-butanol and mixtures thereof to yield a fraction, (c) subjecting the active fraction to flash chromatography over silica gel to obtain partially purified active compound, and (d) subjecting the active subfraction obtained from step (c) above to gel permeation chromatography to obtain the active pure compound.Type: ApplicationFiled: January 16, 2002Publication date: October 10, 2002Inventors: Cynthia Olimpia Lydia Gonsalves, Perunninakulath Parameswaran Subrayan, Chandrakant Govind Naik, Chittur Thelakkat Achuthankutty
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Publication number: 20020045774Abstract: This invention describes the new 17a-fluoroalkyl steroids of general formula I 1Type: ApplicationFiled: October 18, 2001Publication date: April 18, 2002Applicant: Schering AktiengesellschaftInventors: Wolfgang Schwede, Arwed Cleve, Ulrich Klar, Gunter Neef, Kristof Chwalisz, Martin Schneider, Ulrike Fuhrmann, Holger Heb-Stumpp
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Patent number: 5824811Abstract: Compounds of the general formula: ##STR1## wherein R.sub.1 represents a C1-10 alkyl group which may be substituted by one or more hydroxyl groups, R.sub.2 represents a hydrogen atom or a hydroxyl group, and R.sub.3 represents a hydrogen atom or a hydroxyl group; their intermediates; as well as synthesis processes of these compounds and intermediates are disclosed. The compounds of this invention, vitamin D derivatives substituted by sulfur atoms at the 22-position have a strong inhibitory effect against proliferation of keratinocytes.Type: GrantFiled: October 1, 1996Date of Patent: October 20, 1998Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Noboru Kubodera, Akira Kawase
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Patent number: 5710293Abstract: The present invention relates to a method of using a perchloric acid catalyzed reaction to make acyl derivatives of norprogesterone compounds and, in particular, 16-methylene-17.alpha.-hydroxy-19-norpregn-4-ene-3,20-dione.Type: GrantFiled: October 13, 1995Date of Patent: January 20, 1998Assignee: The Population Council, Center for Biomedical ResearchInventor: Fang Li
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Patent number: 5703067Abstract: The present invention is directed to steroidal or terpenoidal compounds which inhibit farnesyl-protein transferase (FPTase). The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.Type: GrantFiled: May 8, 1995Date of Patent: December 30, 1997Assignee: Merck & Co., Inc.Inventors: Hiranthi Jayasuriya, Russell B. Lingham, Fernando Pelaez, Manuel Sanchez, Keith C. Silverman, Sheo Bux Singh, Deborah L. Zink
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Patent number: 5352808Abstract: A process for the preparation of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted by halogen or a nitrogen or oxygen function and alkenyl and alkynyl of 2 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and the A, B, C and D rings are optionally substituted by at least one member of the group consisting of optionally protected --OH or .dbd.0, halogen, alkyl and alkoxy of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms comprising reacting a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 and the A, B, C and D rings are defined as above with an oxidizing agent in the presence of water and an at least partially water-miscible solvent to obtain a compound of the formula ##STR3## wherein R.sub.1 and R.sub.Type: GrantFiled: November 5, 1992Date of Patent: October 4, 1994Assignee: Roussel UclafInventors: Jean Buendia, Michel Vivat
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Patent number: 5112998Abstract: There are provided pregnane derivatives represented by formula ##STR1## wherein A.sup.1 represents a hydrogen atom or a hydroxyl group, A.sup.2 represents a substituent such as a hydroxyl group when A.sup.1 represents a hydrogen atom, or A.sup.2 represents a hydrogen atom when A.sup.1 represents a hydroxyl group, or A.sup.1 and A.sup.2 are combined together to form an oxo group; D.sup.1 represents a substitutent such as a hydroxyl group, and D.sup.2 represents a hydrogen atom, or D.sup.1 and D.sup.2 are combined together to form an epoxy group or a single bond; D.sup.3, D.sup.5 and D.sup.7 each represents a hydrogen atom, D.sup.4 represents a hydroxyl group, and D.sup.6 represents a substitutent such as a hydroxyl group, or D.sup.3 and D.sup.4 may be combined together to form an epoxy group or a single bond, or D.sup.4 and D.sup.5 may be combined together to form a single bond, or D.sup.5 and D.sup.6 may be combined together to form an epoxy group or a single bond, or D.sup.6 and D.sup.Type: GrantFiled: June 15, 1990Date of Patent: May 12, 1992Assignee: Kuraray Co., Ltd.Inventors: Jiro Tsuji, Takashi Takahashi, Masao Tsuji, Naoshi Nakagawa, Tetsuo Takigawa
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Patent number: 5093502Abstract: A process for the preparation of novel 14.alpha., 17.alpha.-dihydroxy-17.beta.-substituted steroids by reacting 14.alpha.-hydroxy-17-oxo-steroids with metal organic compounds and the use of the said novel steroids in the production of 14.alpha., 17.alpha.-methylenedioxy-pregnane derivatives.Type: GrantFiled: February 16, 1990Date of Patent: March 3, 1992Assignee: Akzo N.V.Inventors: Peter M. Smid, Willem J. Van Zoest, Pieter G. Weber, Arthur F. Marx