Unsaturation Between The 4- And 5-positions (e.g., Adrenosterones, 11 Hydroxytestosterones, Etc.) Patents (Class 552/621)
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Patent number: 7495115Abstract: Conjugates comprising one or more steroids conjugated with one or more mammalian proteins are disclosed. The conjugates are useful for diagnosis or treatment of solid cancer and haematological malignancies. Further the conjugates exhibits a synergistic action together with a cytoskeleton acting drug such as Taxol®, which enable the treatment of cancers that otherwise would be non responsive to Taxol®.Type: GrantFiled: July 14, 2003Date of Patent: February 24, 2009Assignee: Bionature E.A., Ltd.Inventor: Elias Castanas
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Patent number: 7225083Abstract: The first crystal structure of the androgen receptor ligand binding domain has been determined to 2.0 angstrom resolution. Disclosed are the coordinates for the crystal structure, and methods for determining agonists, partial agonists, antagonists, partial antagonists and selective androgen receptors modulators (SARMs) of the androgen receptor.Type: GrantFiled: June 28, 2004Date of Patent: May 29, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Roberto Weinmann, Howard M. Einspahr, Stanley R. Krystek, John S. Sack, Mark E. Salvati, John S. Tokarski, Ricardo M. Attar, Chihuei Wang
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Patent number: 6795776Abstract: The first crystal structure of the androgen receptor ligand binding domain has been determined to 2.0 angstrom resolution. Disclosed are the coordinates for the crystal structure, and methods for determining agonists, partial agonists, antagonists, partial antagonists and selective androgen receptors modulators (SARMs) of the androgen receptor.Type: GrantFiled: October 13, 2000Date of Patent: September 21, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Roberto Weinmann, Howard M. Einspahr, Stanley R. Krystek, John S. Sack, Mark E. Salvati, John S. Tokarski, Ricardo M. Attar, Chihuei Wang
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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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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: 6046023Abstract: The invention relates to a microbial method of in vitro transformation of a steroid into its corresponding 11.alpha.-hydroxy analogue using oxygen and a microorganism selected from the Aspergillus ochraceus, Aspergillus niger, Rhizopus stolonifer, Rhizopus nigricans, Rhizopus arrhizus, and strains of Pestelotia, using as substrate a steroid having a purity of less than 97% and more than 90% at a concentration greater than 10 g/l.Type: GrantFiled: September 30, 1998Date of Patent: April 4, 2000Assignee: Akzo Nobel, N.V.Inventors: Marten Wiersma, Peter van der Meijden
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Patent number: 5837269Abstract: The invention relates to a vaccine which comprises an antigen and an immune response augmenting agent. The immune response augmenting agent is capable of enhancing T cell lymphokine production. Suitable immune response augmenting agents include, but are not limited to, DHEA, DHEA-derivatives and DHEA congeners.The invention also relates to a method for enhancing a vaccine-induced humoral immune response which comprises administering a vaccine which comprises an antigen and an immunomodulator. The immunomodulator may be an immune response augmenting agent, a lymphoid organ modifying agent or a mixture of the immune response augmenting agent and lymphoid organ modifying agent. Suitable lymphoid organ modifying agents include, but are not limited to, 1,25-dihydroxy Vitamin D.sub.3, 25-hydroxy Vitamin D.sub.3, biologically active 1,25-dihydroxy Vitamin D.sub.3, derivatives which are capable of activating the intra-cellular Vitamin D.sub.Type: GrantFiled: June 7, 1995Date of Patent: November 17, 1998Assignee: University of Utah Research FoundationInventors: Raymond A. Daynes, Barbara A. Araneo
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Patent number: 5831104Abstract: The invention is directed to novel steroid intermediate products of general formula I ##STR1## The steroid intermediate products which can be isolated according to the invention are suitable for the synthesis of 13-ethyl-11-methylene-18,19-bisnor-17.alpha.-pregn-4-en-20-in-17-ol (desogestrel).Further, processes for producing the steroid intermediate products of general formula I are described. The olefination of the 11-oxo steroids is carried out under the influence of ultrasound.Type: GrantFiled: September 9, 1994Date of Patent: November 3, 1998Assignee: Jenapharm GmbHInventors: Sven Ring, Gerhard Teichmueller, Gisela Weber, Sigfrid Schwarz, Bernd Erhart, Bernd Undeutsch, Harald Raethe, Peter Moellmann, Carmen Pfeiffer, Hans-Joachim Palme
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Patent number: 5426198Abstract: The present invention involves improved processes for the dehalogenation of 9.alpha.-halosteroids (I) ##STR1## to produce the corresponding 11.beta.-hydroxy steroids (II) ##STR2## which are known to be useful as pharmaceutical, where the improvements comprise (1) adding the 9.alpha.-halo steroid (I) to the chromium and (2) using catalytic amounts of chromium in the presence of a means of converting chromium (II) to chromium (III).Type: GrantFiled: January 31, 1990Date of Patent: June 20, 1995Assignee: The Upjohn CompanyInventors: Joel E. Huber, Jeffrey A. Fleming
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Patent number: 5296481Abstract: A method for controlling weight gain or promoting weight loss which includes the step of treating a subject with an effective weight gain controlling or weight loss promoting amount of a substituted .DELTA.5-Androstene which is biologically effective for controlling weight gain or promoting weight loss and biologically ineffective for promoting the synthesis of sex hormones. Steroids believed to provide the desired weight control/weight loss characteristics include:.DELTA.5-Androstene-3.beta.,7.alpha.-diol-17-one.DELTA.5-Androstene-3.beta.-ol-7,17-dione.DELTA.5-Androstene-3.beta.,7.alpha.,17-triol.DELTA.5-Androstene-3.beta.,17.beta.-diol-7-oneand various derivatives thereof.Type: GrantFiled: April 10, 1992Date of Patent: March 22, 1994Assignee: Humanetics CorporationInventors: Bruce E. Partridge, Henry A. Lardy
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Patent number: 5064822Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of naphthyl, phenylphenyl, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms optionally containing additional unsaturations, phenoxy, furyl, cycloalkyl of 3 to 6 carbon atoms, thienyl optionally substituted with at least one member of the group consisting of halogen and alkyl and haloalkyl of 1 to 6 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of --OH, halogen, --CF.sub.3, alkyl and alkoxy of 1 to 6 carbon atoms, alkenyloxy of 2 to 6 carbon atoms, phenoxy and alkylthio of 1 to 6 carbon atoms optionally oxidized to the sulfoxide or sulfone, R.sub.2 is selected from the group consisting of methyl and ethyl, R.sub.Type: GrantFiled: November 16, 1989Date of Patent: November 12, 1991Assignee: Roussel UclafInventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt