Oxygen Bonded Directly At The 7-, 8- Or 9-position Patents (Class 552/562)
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Patent number: 10995112Abstract: Described herein are solid state 17?-ethynylandrost-5-ene-3?,7?,17?-triol including amorphous and crystalline forms and specific polymorphic forms thereof, and use of solid state 17?-ethynylandrost-5-ene-3?,7?,17?-triol in treating numerous diseases and disorders, including hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions, and neurodegenerative conditions in subjects or human patients.Type: GrantFiled: October 10, 2019Date of Patent: May 4, 2021Assignee: NeurMedix, Inc.Inventors: Steven K. White, Igor Ivanisevic, Kyle Stephens, Mark Andres, Brenton Skylar Wolfe
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Patent number: 9850271Abstract: 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: GrantFiled: November 10, 2016Date of Patent: December 26, 2017Assignee: NeurMedix, Inc.Inventors: Steven K White, Igor Ivanisevic, Kyle Stephens, Mark Andres, Brenton Skylar Wolfe
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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: 8252947Abstract: 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?, ?,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: GrantFiled: April 3, 2009Date of Patent: August 28, 2012Assignee: Harbor Therapeutics, Inc.Inventors: Steven K. White, Igor Ivanisevic, Kyle Stephens, Mark Andres, Brenton Skylar Wolfe
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Publication number: 20110098260Abstract: The invention provides methods to treating conditions such as prostate cancer, or for ameliorating one or more symptoms associated with prostate cancer, or for agents that modulate the biological activity of the androgen receptor. The invention also provides methods and compositions suitable for therapeutic applications.Type: ApplicationFiled: December 1, 2010Publication date: April 28, 2011Applicant: Harbor BioSciences, Inc.Inventor: James M. Frincke
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Publication number: 20090061358Abstract: Photoacid generators generate sulfonic acids of formula (1a) or (1c) upon exposure to high-energy radiation. R1—COOCH(CF3)CF2SO3+H+??(1a) R1—O—COOCH(CF3)CF2SO3?H+??(1c) R1 is a C20-C50 hydrocarbon group having a steroid structure. The photoacid generators are compatible with resins and can control acid diffusion and are thus suited for use in chemically amplified resist compositions.Type: ApplicationFiled: September 4, 2008Publication date: March 5, 2009Inventors: Masaki OHASHI, Youichi Ohsawa, Takeru Watanabe, Takeshi Kinsho
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Publication number: 20030181742Abstract: A process for preparing pregnane derivatives represented by the formula (V), 1Type: ApplicationFiled: March 4, 2003Publication date: September 25, 2003Inventors: Makoto Nakazawa, Satoru Kita, Shigeo Ohzono
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Patent number: 6043603Abstract: The invention relates to a low-pressure discharge lamp with at least one porting element (12) placed inside a discharge vessel (10). Said supporting element is provided with a mercurial coating (13) and is coated with a getter material (14). The coated surfaces of the supporting element (12) are inclined at an angle of at least 30 degrees in relation to the longitudinal axis (A--A) of the discharge vessel (10).Type: GrantFiled: May 21, 1998Date of Patent: March 28, 2000Assignee: Patent-Treuhand-Gesellschaft fuer elektrische Gluehlampen mbHInventor: Erolf Weinhardt
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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: 5565588Abstract: New 9-alpha-hydroxy steroids are prepared by the introduction of substituents on the D-ring of 9-alpha-hydroxy-androst-4-ene-3,17-dione.The resulting compounds are useful intermediates in the synthesis of corticosteroids.Type: GrantFiled: October 4, 1994Date of Patent: October 15, 1996Assignee: Roussel UCLAFInventors: Jacobus N. M. Batist, Arthur F. Marx, Willem J. Van Zoest, Jagdish C. Kapur
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Patent number: 5502183Abstract: Novel steroids having a 9.alpha.-hydroxy or a 9.alpha.-carbonate substituent can be prepared from 9.alpha.-hydroxyandrostenedione and can be utilized in the synthesis of commercially valuable corticosteroids such as betamethasone. The 9.alpha.-carbonates are prepared by reaction of the corresponding 9.alpha.-hydroxy steroid with a sequence of excess base, trialkylsilyl chloride, alkyl haloformate and alkanol or by using excess base, alkyl haloformate and alkoxide. 9.alpha.-Carbonate-17-keto compounds can be treated with lithium acetylide and a lithium salt to afford the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-9.alpha.-carbonate. This compound is then esterified with a novel series of reagents to give the 17-ester which can be reduced the corresponding 17-allene. Oxidation of this allene to the bis-epoxide compound, followed by treatment with an alkali metal salt of a carboxylic acid under phase transfer conditions gives the 17.alpha.-hydroxy 21-ester 9.alpha.-carbonate. Elimination of the 9.alpha.Type: GrantFiled: July 25, 1994Date of Patent: March 26, 1996Assignee: Schering CorporationInventors: David R. Andrews, Anantha R. Sudhakar
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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: 5194602Abstract: 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: GrantFiled: December 12, 1990Date of Patent: March 16, 1993Assignee: Gist-Brocades N.V.Inventors: Jacobus N. M. Batisi, Arthur F. Marx
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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
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Patent number: 5028722Abstract: Novel 7.beta.-hydroxy-4-pregnene-3,20-dione derivatives are disclosed.The group of these compounds has possibility of being utilized as an intermediate for the synthesis of progesterone derivatives having ovulation-inhibiting activity. These compounds themselves have also cell differentiation activity for M1 cells.Type: GrantFiled: September 26, 1988Date of Patent: July 2, 1991Assignee: Snow Brand Milk Products Co., Ltd.Inventors: Makoto Yoshihama, Koji Tamura, Nobuo Miyata, Masamichi Nakakoshi