Chalcogen Attached Indirectly To The Cyclopentanohydrophenanthrene Ring System By Nonionic Bonding Patents (Class 540/120)
  • Publication number: 20150094288
    Abstract: A method of treating a solid tumor in a mammal by inhibiting angiogenesis, including administering to the mammal which has a solid tumor selected from the group consisting of breast carcinoma, lung carcinoma, prostate carcinoma, colon carcinoma, ovarian carcinoma, neuroblastoma, central nervous system tumor, multiform glioblastoma and melanoma; a composition including brassinosteroids of general formula (I) wherein can be a single or double bond and the configurations of carbon atoms C22 and C23 respectively linked to the substituents HO are S for both carbon atoms and a pharmaceutically acceptable additive.
    Type: Application
    Filed: December 14, 2012
    Publication date: April 2, 2015
    Applicant: CONSEJO NACIONAL DE INVESTIGACIONES CIENTIFICAS Y TECHNICAS (CONICET)
    Inventors: Javier Alberto Ramirez, Flavia Mariana Michelini, Lydia Raquel Galagovsky, Alejandro Berra, Laura Edith Alche
  • Publication number: 20150093708
    Abstract: Acid generators comprising a carbocyclic or heteroaromatic group substituted with at least one diester moiety are provided. These acid generators are particularly useful as a photoresist composition component.
    Type: Application
    Filed: September 27, 2013
    Publication date: April 2, 2015
    Inventor: Paul J. LaBEAUME
  • Publication number: 20150065470
    Abstract: The present invention is related to a dosage regimen of a steroid sulfatase inhibitor, E2MATE, for use in the prevention or treatment of endometriosis. The present invention further relates to a method for preventing or treating endometriosis.
    Type: Application
    Filed: April 4, 2013
    Publication date: March 5, 2015
    Applicant: PregLem SA
    Inventors: Ernest Loumaye, Oliver Pohl, Jean-Pierre Gotteland
  • Publication number: 20140256696
    Abstract: The present invention describes steroid conjugates. These single drug entities are formed by connecting two or more steroids via a linker. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual steroid drugs.
    Type: Application
    Filed: March 6, 2014
    Publication date: September 11, 2014
    Applicant: Allergan, Inc.
    Inventors: Santosh C. Sinha, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
  • Publication number: 20140256660
    Abstract: The present invention describes novel single drug entities, formed by the linkage of an antibiotic with a steroidal drug via a linker. Upon topical application to the eye, the conjugate would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.
    Type: Application
    Filed: March 6, 2014
    Publication date: September 11, 2014
    Applicant: Allergan, Inc.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
  • Publication number: 20120115169
    Abstract: Provided is a derivative of 22-hydroxycholesterol, 24S-hydroxycholesterol, 25-hydroxycholesterol, 26-hydroxycholesterol or 27-hydroxycholesterol. Also provided is a protein conjugated to the above derivative. Further provided is an antibody composition comprising antibodies that specifically bind to 22-hydroxycholesterol, 24S-hydroxycholesterol, 25-hydroxycholesterol, 26-hydroxycholesterol or 27-hydroxycholesterol. Additionally, a method of making antibodies that specifically bind to 22-hydroxycholesterol, 24S-hydroxycholesterol, 25-hydroxycholesterol, 26-hydroxycholesterol or 27-hydroxycholesterol is provided. Also, a method of assaying for 22-hydroxycholesterol, 24S-hydroxycholesterol, 25-hydroxycholesterol, 26-hydroxycholesterol or 27-hydroxycholesterol is provided. Additionally provided is a kit for detecting 22-hydroxycholesterol, 24S-hydroxycholesterol, 25-hydroxycholesterol, 26-hydroxycholesterol or 27-hydroxycholesterol.
    Type: Application
    Filed: November 9, 2010
    Publication date: May 10, 2012
    Applicant: ENZO LIFE SCIENCES, INC. C/O ENZO BIOCHEM, INC.
    Inventors: Michael C. Mullenix, Robert Elliot Zipkin, Jeffrey Kroll Adams, Wayne Forrest Patton, James J. Donegan
  • Publication number: 20120100486
    Abstract: A sulfonium salt of a naphthyltetrahydrothiophenium cation having a fluoroalkoxy chain with a specific anion is provided. The sulfonium salt is used as a photoacid generator to form a resist composition which when processed by immersion lithography, offers advantages of restrained dissolution in the immersion water and less pattern dependence or dark/bright bias.
    Type: Application
    Filed: September 23, 2011
    Publication date: April 26, 2012
    Inventors: Masayoshi Sagehashi, Youichi Ohsawa, Koji Hasegawa, Takeshi Kinsho, Tomohiro Kobayashi
  • Publication number: 20110280847
    Abstract: Certain bile acids, including novel bile acids, and derivatives thereof can be used to inhibit the germination of C. difficile spores and/or the growth of C. difficile cells. The methods and compositions of the invention are useful for preventing and treating C. difficile-associated diseases, including but not limited to C. difficile colitis.
    Type: Application
    Filed: November 2, 2009
    Publication date: November 17, 2011
    Applicant: TUFTS UNIVERSITY
    Inventors: Joseph Sorg, Abraham L. Sonenshein
  • Patent number: 8058045
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain pyrazin-2-yl-pyridin-2-yl-amine and pyrazine-2-yl-pyrimidin-4-yl-amine compounds of formula (I), which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc.
    Type: Grant
    Filed: October 6, 2008
    Date of Patent: November 15, 2011
    Assignee: Cancer Research Technology Limited
    Inventors: Ian Collins, John Charles Reader, Thomas Peter Matthews, Kwai Ming Cheung, Nicolas Proisy, David Hugh Williams, Sukhbinder Singh Klair, Jane Elizabeth Scanlon, Nelly Piton, Glynn Jonathan Addison, Michael Cherry
  • Publication number: 20110082091
    Abstract: The invention teaches a method for testing a prospective or known immunomodulatory drug for T-cell activation, comprising the step of contacting in-vitro a peripheral blood mononuclear cell (PBMC) culture with a predetermined amount of the prospective or known immunomodulatory drug and observing the PBMC culture for T-cell activation using a readout system, upon contact with the prospective or known immunomodulatory drug, wherein the cell density of a PBMC preculture is adjusted such that cell-cell contact of the PBMC is enabled and wherein the PBMC preculture is cultured for at least 12 h.
    Type: Application
    Filed: September 28, 2010
    Publication date: April 7, 2011
    Applicant: TheraMAB GmbH
    Inventor: Thomas Hünig
  • Publication number: 20110071100
    Abstract: The subject of the invention provides a pharmaceutical composition comprising a sulfobetaine, a sulfobetaine for therapy, uses thereof and methods of treating cancer obesity, age related macular degeneration or neurodegenerative diseases comprising administering a composition comprising a sulfobetaine.
    Type: Application
    Filed: May 5, 2009
    Publication date: March 24, 2011
    Applicant: TILTAN PHARMA LTD.
    Inventors: Shmuel A. Ben-Sasson, Arie Dagan
  • Patent number: 7888000
    Abstract: Salt sensitivity is measured as a function of the urinary 25-OHD binding activity, which may be evaluated by measuring 25-hydroxyvitamin D binding activity using radiolabeled 25-hydroxyvitamin D3. High binding activity is indicative of salt sensitivity and is an important predictor for development of salt-sensitivity related hypertension.
    Type: Grant
    Filed: July 11, 2003
    Date of Patent: February 15, 2011
    Assignee: Morehouse School of Medicine
    Inventors: Myrtle Thierry-Palmer, Akins Doherty, Keri J. Griffin, Mohamed A. Bayorh
  • Publication number: 20110008297
    Abstract: Synthetic oxysterols can be made and can be used for the treatment of bone disorders, obesity, cardiovascular disorders, and neurological disorders.
    Type: Application
    Filed: December 3, 2008
    Publication date: January 13, 2011
    Applicant: The Regents of the University of California
    Inventors: Farhad Parhami, Michael E. Jung, Khanhlinh Nguyen, Dongwon Yoo, Woo-Kyun Kim
  • Patent number: 7498321
    Abstract: There are provided according to the invention compounds of formula (I) wherein R1 represents C1-6 alkyl or C1-6 haloalkyl; R2 represents —C(?O)-aryl or —C(?O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the ? or ? configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and——represents a single or a double bond; and salts and solvates thereof. There are also provided processes for preparing compounds of formula (I) and use of the compounds in therapy especially in the treatment of inflammatory and allergic conditions.
    Type: Grant
    Filed: August 3, 2001
    Date of Patent: March 3, 2009
    Assignee: Glaxo Group Limited
    Inventors: Keith Biggadike, Paul Jones, Jeremy John Payne
  • Patent number: 7498334
    Abstract: Pyrrolopyrimidine derivatives of the formula I in which R3, R4, R5, R6 and X are as defined in claim 1, act as phosphodiesterase VII inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS.
    Type: Grant
    Filed: November 8, 2002
    Date of Patent: March 3, 2009
    Assignee: Merck Patent GmbH
    Inventors: Hans-Michael Eggenweiler, Michael Wolf
  • Publication number: 20080146642
    Abstract: The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to, the prevention and treatment of Alzheimer's disease.
    Type: Application
    Filed: October 12, 2007
    Publication date: June 19, 2008
    Inventors: Xianqi Kong, Mohamed Atfani, Benoit Bachand, Abderrahim Bouzide, Stephane Ciblat, Sophie Levesque, David Migneault, Isabelle Valade, Xinfu Wu, Daniel Delorme
  • Publication number: 20070207989
    Abstract: The present invention relates to useful diterpenes and pharmaceutical compositions containing them of the formula: for use in the treatment of cardiovascular and inflammatory diseases and for cancers susceptible to an NF-?B inhibitor and an endothelin receptor inhibitor. The present invention also relates to compounds and methods useful to inhibit cell proliferation and for the induction of apoptosis.
    Type: Application
    Filed: March 1, 2007
    Publication date: September 6, 2007
    Applicant: SaviPu Pharmaceuticals
    Inventors: Inderjit Kumar Dev, Ven Subbiah
  • Patent number: 7049305
    Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.
    Type: Grant
    Filed: February 9, 2005
    Date of Patent: May 23, 2006
    Assignee: XenoPort, Inc.
    Inventors: Kenneth C. Cundy, Mark A. Gallop, Cindy X. Zhou
  • Patent number: 6900192
    Abstract: This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed to pharmaceutical compositions including and methods using such compounds.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: May 31, 2005
    Assignee: XenoPort, Inc.
    Inventors: Kenneth C. Cundy, Mark A. Gallop, Cindy X. Zhou
  • Patent number: 6780855
    Abstract: This invention describes the new 11&bgr;-halogen-7&agr;-substituted estratrienes of general formula I in which R11 is a fluorine or chlorine atom, and the other substituents have the meanings that are explained in more detail in the description. The compounds have antiestrogenic properties or tissue-selective estrogenic properties and are suitable for the production of pharmaceutical agents.
    Type: Grant
    Filed: December 2, 1999
    Date of Patent: August 24, 2004
    Assignee: Schering Aktiengesellschaft
    Inventors: Rolf Bohlmann, Nikolaus Heinrich, Helmut Hofmeister, Jorg Kroll, Hermann Kunzer, Gerhard Sauer, Ludwig Zorn, Karl-Heinrich Fritzemeier, Monika Lessl, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
  • Patent number: 6596885
    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
  • Patent number: 6479063
    Abstract: A method of decreasing atherosclerosis and its complications involving administering to a human or animal various combinations of medications with Finasteride, Bicalutamide, Flutamide and Nilutamide.
    Type: Grant
    Filed: December 26, 2000
    Date of Patent: November 12, 2002
    Inventors: Kenneth Weisman, Michael E. Goldberg
  • Patent number: 6271403
    Abstract: This invention describes new, substituted 7&agr;-(&egr;-aminoalkyl)-estratrienes of general formula I in which side chain SK is a radical of partial formula The new compounds represent compounds with very strong antiestrogenic action. The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
    Type: Grant
    Filed: April 14, 2000
    Date of Patent: August 7, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: Rolf Bohlmann, Dieter Bittler, Josef Heindl, Nikolaus Heinrich, Helmut Hofmeister, Hermann Künzer, Gerhard Sauer, Christa Hegele-Hartung, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
  • Patent number: 5948925
    Abstract: Cationic amphiphiles are provided that facilitate transport of biologically active (therapeutic) molecules into cells. There are provided also therapeutic compositions prepared typically by contacting a dispersion of one or more cationic amphiphiles with the therapeutic molecules. Therapeutic molecules that can be delivered into cells according to the practice of the invention include DNA, RNA, and polypeptides. Representative uses of the therapeutic compositions of the invention include providing gene therapy, and delivery of antisense polynucleotides or biologically active polypeptides to cells. With respect to therapeutic compositions for gene therapy, the DNA is provided typically in the form of a plasmid for complexing with the cationic amphiphile.
    Type: Grant
    Filed: May 6, 1997
    Date of Patent: September 7, 1999
    Assignee: Genzyme Corporation
    Inventors: Mikaela N. Keynes, Craig S. Siegel, Edward R. Lee, David J. Harris
  • Patent number: 5760025
    Abstract: Compounds of formula (I): ##STR1## ?wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.
    Type: Grant
    Filed: March 31, 1995
    Date of Patent: June 2, 1998
    Assignee: Sankyo Company, Limited
    Inventors: Koichi Kojima, Hitoshi Kurata, Koki Ishibashi, Hiroyoshi Horikoshi, Takakazu Hamada
  • Patent number: 5725840
    Abstract: The present invention relates to metabolically labile esters, and to contrast media for X-ray and magnetic resonance imaging comprising these esters. The esters have formula (I): ##STR1## in which R.sup.3 is asteroid residue. The esters contain at least one iodine atom and/or heavy metal atom. The compound are metabolizable to products which are soluble in body fluids and are physiologically acceptable.
    Type: Grant
    Filed: October 4, 1996
    Date of Patent: March 10, 1998
    Assignee: Nycomed Imaging AS
    Inventors: Jo Klaveness, Frode Rise, John Varadarajan, Arne J.o slashed.rgen Aasen
  • Patent number: 5717088
    Abstract: Compounds of formula (I): ##STR1## ?wherein: R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is: aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl!; and pharmaceutically acceptable salts and esters thereof have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydrotestosterone.
    Type: Grant
    Filed: March 20, 1996
    Date of Patent: February 10, 1998
    Assignee: Sankyo Company, Limited
    Inventors: Koichi Kojima, Hitoshi Kurata, Koki Ishibashi, Hiroyoshi Horikoshi, Takakazu Hamada
  • Patent number: 5646272
    Abstract: Bile acid derivatives of the formula IW--X--Gin which G is a bile acid radical, W is an active compound moiety of a medicament and X is a bonding member between a bile acid radical and active compound moiety, are outstandingly suitable for introducing active compounds into the entercepatic circulation. The compounds I are absorbed and pass into the bloodstream. It is possible in this way, using the natural reabsorption of the bile acids, to achieve improved absorption of non-absorbable or poorly absorbable pharmaceuticals.W may be, for example, a peptide, an antibiotic, an antiviral substance, an anticancer agent, a hepatoprotective agent, an antihyperlipidemic, a diuretic, a hypotensive, a renin inhibitor, a substance for the treatment of cirrhosis of the liver or a substance for the treatment of diabetes.G is a bile acid radical in the form of the free natural or chemically modified acids, the esters and amides, the salt forms and forms derivatized on alcohol groups.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 8, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Werner Kramer, Gunther Wess
  • Patent number: 5646316
    Abstract: The present invention relates to a bile acid derivative, which comprises a bile acid derivatized at the carboxyl group with a hydroxamic acid or hydroxamate ester. The carboxyl group in the bile acid compound can also be derivatized with an amino acid or oligopeptide, whose C-terminus is derivatized with a hydroxamic acid or a hydroxamate ester. The present invention also relates to a method of use of a bile acid or a bile acid derivative to inhibit a metalloproteinase enzyme, comprising contacting a metalloproteinase with an effective amount of a bile acid or bile acid derivative. In another embodiment, the present invention further relates to a method of use of a bile acid or bile acid derivative to therapeutically treat a disease, which is ameliorated by inhibiting a metalloproteinase enzyme. In this method, a therapeutically effective amount of a bile acid, a bile acid derivative or physiologically acceptable salts thereof, is administered to a human or other mammal.
    Type: Grant
    Filed: April 25, 1995
    Date of Patent: July 8, 1997
    Assignee: OsteoArthritis Sciences, Inc.
    Inventors: Alan R. Jacobson, Douglas G. Gabler, Jozef Oleksyszyn
  • Patent number: 5616743
    Abstract: A compound having the formulae selected from the group consisting of ##STR1## wherein R.sub.2 and R.sub.3 are hydrogen or R.sub.2 is fluorine and R.sub.3 is formyloxy or acetyloxy, the dotted line in 9(11) position indicates an optional double bond and the dotted line in position 16(17) indicates an optional double bond ##STR2## is a 3-keto-.DELTA..sup.4 -system or 3-keto-.DELTA..sup.1,4 -system or 3-OR.sub.4 -.DELTA..sup.5 -system, R.sub.4 is hydrogen or a protector group of hydroxy, R is --CH.sub.3, --CH.sub.2 OH or --CH.sub.2 --OR', R' is a hydroxy protector group and R'.sub.1 is selected from the group consisting of methyl, a branched alkyl of 5 to 8 carbon atoms not possessing hydrogen in the .beta.-position, aryl of up to 10 carbon atoms and benzyl, hetroaryl of up to 10 carbon atoms and at least one heteroatom selected from the group consisting of nitrogen, sulfur and oxygen, with the exception of the compounds of formula Vc in which R is methyl, R.sub.2 and R.sub.3 are hydrogen or R.sub.2 and R.sub.
    Type: Grant
    Filed: January 13, 1995
    Date of Patent: April 1, 1997
    Assignee: Roussel UCLAF
    Inventors: Jean Boivin, Samir Zard, Christine Chauvet
  • Patent number: 5591733
    Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, insomnia and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-aminobutyric acid receptor-chloride ionophore (GR) complex.
    Type: Grant
    Filed: August 2, 1993
    Date of Patent: January 7, 1997
    Assignee: University of Southern California
    Inventors: Michael B. Bolger, Kelvin W. Gee, Nancy C. Lan, Robert H. Purdy, Seid Mirsadeghi, Syed Hasan Tahir, Delia Belelli
  • Patent number: 5536714
    Abstract: The invention includes compounds of formula (I): ##STR1## in which R.sup.1 is hydrogen, alkyl, aryl-substituted alkyl or aromatic heterocyclic-substituted alkyl; R.sup.2 is aryl-substituted alkyl, aromatic heterocyclic-substituted alkyl or diarylamino; and R.sup.3 is carboxy or a group of formula --CONHSO.sub.2 R.sup.4 wherein R.sup.4 is alkyl; and pharmaceutically acceptable salts and esters of the compounds. The compounds have valuable 5.alpha.-reductase inhibitory activity and can thus be used for the treatment and prophylaxis of, inter alia, prostatic hypertrophy as well as other disorders arising from excess levels of 5.alpha.-dihydro-testosterone.
    Type: Grant
    Filed: January 19, 1995
    Date of Patent: July 16, 1996
    Assignee: Sankyo Company, Limited
    Inventors: Koichi Kojima, Hitoshi Kurata, Koki Ishibashi, Hiroyoshi Horikoshi, Takakazu Hamada
  • Patent number: 5504203
    Abstract: A compound of the formula ##STR1## wherein R is=0 or ##STR2## and the rings A and B are selected from the group consisting of ##STR3## K is oxo or a protector group of oxo of the formula ##STR4## n is 2 or 3 and R.sub.1 is an ether or ester remainder, K' is oxo or a protector oxime, hydrazone or semicarbazone group and the wavy lines symbolize an isomer mixture, a process for their preparation and their use as intermediates.
    Type: Grant
    Filed: March 9, 1995
    Date of Patent: April 2, 1996
    Assignee: Roussel Uclaf
    Inventors: Jean Buendia, Remi Chauvin, Michel Vivat
  • Patent number: 5420120
    Abstract: Topically administrable C-21 thioether glucocorticoid steroid derivatives are disclosed as effective anti-inflammatory agents for the treatment of ophthalmic inflammatory disorders. These C-21 thioether derivatives do not cause a significant increase in intraocular pressure as a side effect.
    Type: Grant
    Filed: December 17, 1993
    Date of Patent: May 30, 1995
    Assignee: Alcon Laboratories, Inc.
    Inventor: John J. Boltralik
  • Patent number: 5412091
    Abstract: A compound of the formula ##STR1## in which ##STR2## is either a 3-keto-.DELTA.4-system or a 3-keto -.DELTA.1,4-system or a 3-OR.sub.4 - .DELTA.5-system in which R.sub.4 is hydrogen or a protector group of hydroxy, R is methyl --CH.sub.2 OH or --CH.sub.2 OR', in which R' is a protector group of hydroxy, R.sub.1 and R'.sub.1 are individually selected from the group consisting of methyl, a branched alkyl not possessing hydrogen in the .beta. position of 5 to 8 carbon atoms, aryl of up to 10 carbon atoms, heteroaryl of up to 10 carbon atoms and at least one heteroatom chosen from nitrogen, sulfur and oxygen and benzyl, n and m, are individually numbers 0 or 1, R.sub.2 and R.sub.3 are hydrogen or R.sub.2 is fluorine and R.sub.3 is formyloxy or acetyloxy and the dotted lines in position 9(11) indicate the optional presence of a second bond which is useful for the preparation of compounds of formula A.
    Type: Grant
    Filed: July 1, 1993
    Date of Patent: May 2, 1995
    Assignee: Roussel Uclaf
    Inventors: Jean Boivin, Christine Chauvet, Samir Zard
  • Patent number: 5397563
    Abstract: Accordingly, the present invention is directed to biological compounds derivatized so as to contain at least one perfluoro-t-butyl moiety for use in fluorine-19 NMR and/or MRI studies. The perfluoro-t-butyl (PFTB) moiety, ##STR1## is an excellent reporter group for fluorine-19 NMR/MRI. It is a source of nine magnetically equivalent fluorine nuclei which generate a single intense resonance for easy detection in spectroscopy or imaging. This signal is a sharp singlet, not split by neighboring nuclei or spread over a wide frequency range and eliminates any chance of ghost images which might arise from multiple resonances. These spectral properties ensure a maximum signal-to-noise ratio (S/N) for readily detecting this moiety. The foregoing allows either reduction in the concentration of the derivatized compound, ability to use MRI instruments with lower field strengths, a reduction in imaging times, or a combination of the foregoing as a result of this moiety producing a single, sharp, intense resonance.
    Type: Grant
    Filed: March 1, 1994
    Date of Patent: March 14, 1995
    Assignees: The Johns Hopkins University, Towson State University
    Inventors: Walter J. Rogers, Jr., Thomas S. Everett
  • Patent number: 5359054
    Abstract: The invention includes compounds of the following formula ##STR1## where A and B either A and B form an additional double bond and D is a hydrogen atom or B and D form an additional double bond and A is a hydrogen atom and the other variables are as defined in the specification. Also disclosed is a process of making the compounds and a process of using the compounds to make compounds of the following formula ##STR2## where the variables are defined in the specification. These compounds are useful as antigestigens.
    Type: Grant
    Filed: November 30, 1992
    Date of Patent: October 25, 1994
    Assignee: Schering Aktiengesellschaft
    Inventors: Eckhard Ottow, Gunter Neef, Arwed Cleve, Rudolf Weichert
  • Patent number: 5319115
    Abstract: This invention provides a simplified method for converting pregnan-3,20-dione compounds to 3.alpha.-hydroxy,3.beta.-substituted-pregnanes. By selective use of reagents the unprotected dione is converted chemoselectively and diastereoselectively into a 3(R)-pregnan-3-spiro-2'oxirane-20-one intermediate. This intermediate can then be converted regioselectively by a second set of reactions to the 3.alpha.-hydroxy,3.beta.-substituted-20-one form, which can be further modified at the 20-keto position.Through this method, each ketone group is independently treated. By modifying the ketones one at a time, one can obtain the desired stereo-specificity at each site.
    Type: Grant
    Filed: March 4, 1992
    Date of Patent: June 7, 1994
    Assignee: Cocensys Inc.
    Inventors: Hasan Tahir, Michael Bolger, Richard Buswell, Richard Gabriel, Jay Stearns
  • Patent number: 5248773
    Abstract: A compound of the formula ##STR1## in which ##STR2## is either a 3-keto-.DELTA.4-system or a 3-keto -.DELTA.1,4-system or a 3-OR.sub.4 -.DELTA.5-system in which R.sub.4 is hydrogen or a protector group of hydroxy, R is methyl, --CH.sub.2 OH or --CH.sub.2 OR', in which R' is a protector group of hydroxy, R.sub.1 and R'.sub.1 are individually selected from the group consisting of methyl, a branched alkyl not possessing hydrogen in the .beta. position of 5 to 8 carbon atoms, aryl of up to 10 carbon atoms, heteroaryl of up to 10 carbon atoms and at least one heteroatom chosen from nitrogen, sulfur and oxygen and benzyl, n and m, are individually numbers 0 or 1, R.sub.2 and R.sub.3 are hydrogen or R.sub.2 is fluorine and R.sub.3 is formyloxy or acetyloxy and the dotted lines in position 9(11) indicate the optional presence of a second bond which are useful for the preparation of compounds of formula A.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: September 28, 1993
    Assignee: Roussel-UCLAF
    Inventors: Jean Boivin, Christine Chauvet, Samir Zard
  • Patent number: 5208227
    Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionophore (GBR) complex.
    Type: Grant
    Filed: February 13, 1991
    Date of Patent: May 4, 1993
    Assignee: University of Southern California
    Inventors: Kelvin W. Gee, Michael B. Bolger, Roberta E. Brinton, Deborah J. Burke, Bruce S. McEwen
  • Patent number: 5120723
    Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.
    Type: Grant
    Filed: May 10, 1990
    Date of Patent: June 9, 1992
    Assignee: University of Southern California
    Inventors: Kelvin W. Gee, Michael B. Bolger
  • Patent number: 5099019
    Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
    Type: Grant
    Filed: August 8, 1988
    Date of Patent: March 24, 1992
    Assignee: Upjohn Company
    Inventors: John M. McCall, Donald E. Ayer, E. Jonathan Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
  • Patent number: 5034548
    Abstract: Lanosterols substituted in the 14 and/or 15 position(s) which are active in inhibiting lanosta-8,24-dien-3.beta.-ol 14.alpha.-methyl-demethylase activity, suppressing 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) activity, decreasing cholesterol synthesis and reducing serum cholesterol levels are disclosed.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: July 23, 1991
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: James L. Gaylor, Paul R. Johnson, Soo S. Ko, Ronald L. Magolda, Simon H. Stam, James M. Trzaskos
  • Patent number: 4948533
    Abstract: The present invention relates to 21-(3-carboxy-1-oxopropoxy) -17.alpha.-hydroxy-11.alpha.-(3,3-dimethyl-1-oxobutoxy)pregna-1,4-diene-3, 20 dione and pharmaceutically acceptable salts thereof which are useful steroid prodrugs.
    Type: Grant
    Filed: February 16, 1989
    Date of Patent: August 14, 1990
    Assignee: The Upjohn Company
    Inventors: John M. Braughler, Edward D. Hall, Wendell Wierenga, John M. McCall
  • Patent number: RE35053
    Abstract: Disclosed are .DELTA..sup.9(11) -steroids (VI) and amino substituted steroids (XI) which contain an amino group attached to the terminal carbon atom of the C.sub.17 -side chain, more particularly amino steroids (Ia and Ib), aromatic steroids (II), .DELTA..sup.16 -steroids (IIIa and IIIb), reduced A-ring steroids (IV), .DELTA..sup.17(20) -steroids (Va and Vb) and .DELTA..sup.9(11) -steroids (VI) which are useful as pharmaceutical agents for treating a number of conditions.
    Type: Grant
    Filed: October 9, 1992
    Date of Patent: October 10, 1995
    Assignee: The Upjohn Company
    Inventors: John M. McCall, E. Jon Jacobsen
  • Patent number: RE35517
    Abstract: Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.
    Type: Grant
    Filed: November 23, 1992
    Date of Patent: May 20, 1997
    Assignee: University of Southern California
    Inventors: Kelvin W. Gee, Michael B. Bolger, Nancy C. Lan