Abstract: The invention provides corticosteroids that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits different properties compared to the properties of the corticosteroid not attached to the water-soluble oligomer.
Type:
Application
Filed:
June 26, 2014
Publication date:
October 16, 2014
Inventors:
Wen Zhang, Jennifer Riggs-Sauthier, J. Milton Harris, Michael D. Bentley
Abstract: The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.
Type:
Grant
Filed:
October 3, 2008
Date of Patent:
August 5, 2014
Assignee:
Nektar Therapeutics
Inventors:
Wen Zhang, Jennifer Riggs-Sauthier, J. Milton Harris, Michael D. Bentley
Abstract: The present invention relates to processes for obtaining abiraterone and derivatives thereof, such as abiraterone acetate, by means of a Suzuki coupling through a steroid borate of general formula (IV) or a C—C coupling through a steroid hydrazone of general formula (II), as well as to intermediates useful in said processes.
Type:
Application
Filed:
December 20, 2012
Publication date:
January 9, 2014
Applicant:
CRYSTAL PHARMA, S.A.U.
Inventors:
Alfonso Perez Encabo, Jose Angel Turiel Hernandez, Francisco Javier Gallo Nieto, Antonio Lorente Bonde-Larsen, Celso Miguel Sandoval Rodriguez
Abstract: Novel benzoic acid hydrazones of 5?-androstan-3,17-dione have been prepared on the basis of steroidal tigogenin of the plant Yucca gloriosa. The hydrazones of the General Formula (I), General Formula (II) and General Formula (III) as shown in the accompanying FIGURE of the drawing are synthesized. The hydrazones have shown promising anti-T.B., anti-cancer and anti-HIV activity revealing immense potential as more efficacious, less toxic drugs with fewer undesirable side effects. They could also prove valuable in correcting hormonal abnormalities that cause severe health problems.
Abstract: Provided are steroid analogues functionalized with polar substituents at the C3 and/or C20 positions of the steroid ring system that exhibit improved water solubility. Also provided are pharmaceutical compositions comprising the steroid analogues and methods using the novel steroid analogues for the treatment and prevention of neurodegeneration in a patient following injury to the central nervous system.
Type:
Application
Filed:
February 26, 2009
Publication date:
October 27, 2011
Inventors:
Christopher Macnevin, Donald G. Stein, Dennis C. Liotta, Iqbal Sayeed, David B. Guthrie, Mark A. Lockwood, Michael G. Natchus
Abstract: The present invention relates to 2-alkoxy and 2-aryloxyestrogen compounds, and the intermediate compounds prepared during the preparation thereof, which intermediate compounds are useful intermediates in the preparation of certain physiologically active compounds.
Abstract: The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer.
Type:
Application
Filed:
October 3, 2008
Publication date:
November 11, 2010
Applicant:
Nektar Therapeutics
Inventors:
Wen Zhang, Jennifer Riggs-Sauthier, J. Milton Harris, Michael D. Bentley
Abstract: Compounds, compositions and methods for treating degenerative diseases and disorders are disclosed, the compounds having the following structure (I): including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein.
Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: wherein the variables are defined in the specification.
Type:
Grant
Filed:
August 24, 2001
Date of Patent:
November 14, 2006
Assignee:
Entremed, Inc.
Inventors:
Gregory E. Agoston, Jamshed H. Shah, Kimberly A. Hunsucker, Victor S. Pribluda, Theresa M. LaVallee, Shawn J. Green, Christopher J. Herbstritt, Xiaoguo H. Zhan, Anthony M. Treston
Abstract: Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering derivatives of 2-methoxyestradiol of the general formula: wherein the variables are defined in the specification.
Type:
Grant
Filed:
February 8, 2001
Date of Patent:
February 7, 2006
Assignee:
Entre Med, Inc.
Inventors:
Gregory E. Agoston, Victor Pribluda, Anthony M. Treston, Shawn J. Green
Abstract: The application discloses novel 2-alkoxyestradiol analogs which exhibit anti-proliferative properties, and methods of making and using such compounds to inhibit undesired cell proliferation and tumor growth. Additionally, methods are disclosed of treating diseases associated with undesired angiogenesis and undesired proliferation, and methods of treating infectious disease wherein the infectious agent is particularly susceptible to inhibition by agents that disrupt microtubule organization and function.
Type:
Grant
Filed:
April 11, 2003
Date of Patent:
February 8, 2005
Assignee:
Southwest Foundation for Biomedical Research
Inventors:
Pemmaraju Narasimha Rao, Susan L. Mooberry, James W. Cessac, Tina L. Tinley
Abstract: Novel compounds having a formula selected from the group consisting of
wherein the substituents are defined as in the specification which are intermediates for the production of vinyl compounds having a remarkable anti-estrogenic and anti-proliferative activity.
Type:
Grant
Filed:
June 26, 2001
Date of Patent:
July 22, 2003
Assignee:
Aventis Pharma S.A.
Inventors:
Andre Claussner, Francois Nique, Jean-Georges Teutsch, Patrick Van de Velde
Abstract: The invention concerns compounds of formula (I) wherein: X, Y, R1, R2, Z, G are as defined in the description, the methods for preparing them and the intermediates in said method, their use as medicine and the pharmaceutical compositions containing them.
Type:
Grant
Filed:
December 17, 2001
Date of Patent:
December 31, 2002
Assignees:
Aventis Pharma S.A., Genentech
Inventors:
Denis Carniato, Thomas R. Gadek, Jochen Knolle, Jean-Francois Gourvest, Anurschirwan Peyman, Sarah C. Bodary
Abstract: Compounds represented by the following structural formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification. The compounds are disclosed as useful in the treatment of various forms of cancer.
Type:
Grant
Filed:
March 12, 1998
Date of Patent:
October 24, 2000
Assignees:
The United States of America as represented by the Department of Health and Human Services, Pharm-Eco Laboratories, Incorporated
Abstract: The invention is drawn to a process for the preparation of a steroid of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms, R.sub.2 is alkyl of 1 to 4 carbon atoms and theo A, B, C, and D ring system has at least one double bond and is optionally substituted by at least one optionally protected hydroxy, optionally protected keto, halogen, alkyl and alkoxy of 1 to 4 carbon atoms, and alkenyl and alkynyl of 2 to 4 carbon atoms by reacting the corresponding 17-ketosteroid with a compound of the formula ##STR2## and then by reacting the resulting compound with an aryl sulfenyl halide. The intermediate produced then undergoes rearrangement followed by epimerization with a strong base to obtain a mixture of the corresponding sulfoxide diastereoisomers which is reacted with a thiophilic compound. The intermediate produced undergoes acid hydrolysis to provide the compound of formula I.