Phosphorus Attached Directly Or Indirectly To The Cyclopentanohydrophenanthrene Ring System By Nonionic Bonding Patents (Class 540/5)
  • Publication number: 20150140088
    Abstract: The present invention relates to the fields of chemistry and pharmacy and, in particular, to the production of novel molecular entities: esterane derivatives fused with spirostanes rings, acting upon the Central Nervous Systems (CNS). From diosgenin, a naturally occurring sapogenin, with some subsequent transformations thereof, spirosteroid derivatives of the I-IV general formula can be obtained, with a cyclopentaneperhydrophenantrene nucleus fused to a 25R-spirostanes nucleus. Such molecular entities have an anti-inflammatory and anti-glutamatergic actions that can be used to treat inflammatory, cerebrovascular, neurodegenerative, neuropsychiatric, and neurologic diseases.
    Type: Application
    Filed: December 27, 2012
    Publication date: May 21, 2015
    Inventors: Laura Garcia Pupo, Yanier Nuñez Figueredo, Juan Enrique Tacoronte Morales, Yamila Verdecia Reyes, Estael Ochoa Rodriguez, Zaldo Castro Armando
  • Publication number: 20150038472
    Abstract: The use of therapeutically active lipids for organ/tissue-specific enrichment for the treatment of inflammatory, ischemic or degenerative disorders and/or for stimulating a regeneration is arranged and developed such that the lipids are bound on application to carrier molecules for which cell-specific uptake systems in the cells of the organs and/or tissue exist. In addition, a method of producing organ/tissue-specific therapeutically active lipids for treatment of inflammatory, ischemic or degenerative disorders and/or stimulation of a regeneration, in particular for treating inflammatory liver disorders, is claimed, which is arranged and developed such that lysophosphatidylethanolamine (LysoPE) is coupled to the carboxyl group of ursodeoxycholate (UrsoDOCA) converted to an ester to give a LysoPE-DOCA compound.
    Type: Application
    Filed: October 21, 2014
    Publication date: February 5, 2015
    Inventor: Wolfgang STREMMEL
  • Patent number: 8895723
    Abstract: Disclosed herein are methods of preparing a phosphorothioate nucleotide analog, which are useful in treating diseases and/or conditions such as viral infections.
    Type: Grant
    Filed: March 18, 2013
    Date of Patent: November 25, 2014
    Assignees: Alios BioPharma, Inc., Vertex Pharmaceuticals Inc.
    Inventors: Vladimir Serebryany, Jyanwei Liu, Leonid Beigelman, Young Chun Jung, Peter Jamison Rose, Shereen Ibrahim, Cavan McKeon Bligh, Luigi Anzalone
  • Publication number: 20130004425
    Abstract: Drug carriers, methods of synthesizing, and methods of use thereof are provided.
    Type: Application
    Filed: February 7, 2011
    Publication date: January 3, 2013
    Inventors: Dong Wang, Xin-Ming Liu
  • Publication number: 20120264810
    Abstract: Compositions, methods and compounds useful for enhancing the uptake of a lipid particle b\ a cell are described In particular embodiments, the methods of the invention include contacting a cell with a lipid particle and a compound that binds a Na+/K+ ATPase to enhance uptake of the lipid particle b\ the cell Related compositions useful in practicing methods include lipid particles comprising a conjugated compound that enhances uptake of the lipid particles b\ the cell The methods and compositions are useful in delivering a therapeutic agent to a cell, e g for the treatment of a disease or disorder in a subject
    Type: Application
    Filed: September 22, 2010
    Publication date: October 18, 2012
    Applicant: The University of British Columbia
    Inventors: Paulo J.C. Lin, Yuen Yi c. Tam, Srinivasulu Masuna, Marco A. Ciufolini, Michel Roberge, Pieter R. Cullis
  • Publication number: 20120010173
    Abstract: The invention relates to a compound of formula (I) and the salts, N-oxides, quaternary amines, and stereoisomers thereof, wherein R1 to R8 are as defined in the claims. The invention further relates to intermediates and methods for the preparation of the compounds of formula (I). The invention also relates to the compounds of formula (I) for use as a medicament, particularly for the prevention or treatment of fungal infections.
    Type: Application
    Filed: March 3, 2010
    Publication date: January 12, 2012
    Applicant: SEPS PHARMA N.V.
    Inventors: Yves Rene Johanna Paul Gonnissen, Jody Firmin Marceline Voorspoels
  • Publication number: 20110312916
    Abstract: Prodrugs of C-17-heterocyclic-steroidal drugs providing improved oral bioavailability and pharmacokinetics are described. The drugs are inhibitors of human CYP 17 enzyme, as well as potent antagonists of both wild type and mutant androgen receptors (AR), and are useful for the treatment of urogenital and/or androgen-related cancers, diseases and/or conditions, such as human prostate cancer, breast cancer, and prostate hyperplasia. The disclosure describes methods of synthesizing and using the prodrugs in cancer therapy.
    Type: Application
    Filed: February 5, 2010
    Publication date: December 22, 2011
    Applicant: TOKAI PHARMACEUTICALS, INC.
    Inventor: David Casebier
  • Publication number: 20100075314
    Abstract: The invention provides stable bioconjugate-nanoparticle probes which are useful for detecting nucleic acids and other target analytes, e.g., proteins, and methods of preparing those probes.
    Type: Application
    Filed: May 26, 2009
    Publication date: March 25, 2010
    Inventors: Viswanadham Garimella, Thomas F. Holzman, Yijia P. Bao
  • Publication number: 20090286973
    Abstract: This invention relates composition and methods for making and using chemically modified oligonucleotides agents for inhibiting gene expression.
    Type: Application
    Filed: July 2, 2009
    Publication date: November 19, 2009
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah MANOHARAN, Venkitasamy KESAVAN, Kallanthottathil G. RAJEEV
  • Patent number: 7479486
    Abstract: The present invention is related to novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues, their use as antiglucocorticoids for the treatment and/or prophylaxis of disease associated to an excess of glucocorticoids. In particular, the invention relates to the use of novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues for treating Cushing's syndrome, iatrogenic hypercortisolism or depression. Also the present invention is related to methods of preparing the novel 21-hydroxy-6,19-oxidoprogesterone (21OH-6OP) analogues.
    Type: Grant
    Filed: May 6, 2005
    Date of Patent: January 20, 2009
    Assignee: Laboratoires Serono SA
    Inventors: Gerardo Burton, Carlos P. Lantos, Adriana Silvia Veleiro
  • Patent number: 7071328
    Abstract: The present invention relates to a novel method for preparing 21-hydroxy-6,19-oxidopro-gesterone (21OH-6OP) and/or its 21-acetate, 21-propionate, 21-hemisuccinate, 21-phosphate, 21-oleate derivatives. 21OH-6OP and its ester derivatives are antiglucocorticoids for the treatment or prophyl axis of diseases associated to an excess of glucocorticoids, in particular for treating Cushing's syndrome, iatrogenic hypercortisolism or depression.
    Type: Grant
    Filed: September 17, 2001
    Date of Patent: July 4, 2006
    Assignee: Applied Research System ARS Holding N.V.
    Inventors: Gerardo Burton, Carlos P. Lantos, Adriana Silvia Veleiro
  • Publication number: 20040157810
    Abstract: The invention features corticosteroids conjugated to either a charged group or a bulky group in a manner that resists in vivo cleavage, the resulting conjugate is a peripherally acting steroid with reduced activity in the central nervous system. The invention provides a method for treating a patient having an inflammatory disease by administering to the patient a corticosteroid conjugate.
    Type: Application
    Filed: August 22, 2003
    Publication date: August 12, 2004
    Inventors: Martin H. Teicher, Susan L. Andersen-Navalta
  • Publication number: 20040092733
    Abstract: The present invention relates to a novel method for preparing 21-hydroxy-6,19-oxidopro-gesterone (21OH-6OP) and/or its 21-acetate, 21-propionate, 21-hemisuccinate, 21-phosphate, 21-oleate derivatives. 21OH-6OP and its ester derivatives are antiglucocorticoids for the treatment or prophylaxis of diseases associated to an excess of glucocorticoids, in particular for treating Cushing's syndrome, iatrogenic hypercortisolism or depression.
    Type: Application
    Filed: July 18, 2003
    Publication date: May 13, 2004
    Inventors: Gerardo Burton, Carlos P Lantos, Adriana Silvia Veleiro
  • Publication number: 20030232981
    Abstract: The present invention involves intermediates, including a 7&agr;-substituted steroid (II), 1
    Type: Application
    Filed: March 21, 2003
    Publication date: December 18, 2003
    Inventors: Bruce Allen Pearlman, Amphlett Greg Padilla, Jeffrey L. Havens, Sonja S. Mackey, Haifeng Wu
  • Publication number: 20020156051
    Abstract: Novel phytosterol and/or phytostanol derivatives, including salts thereof, are represented by the general formulae: 1
    Type: Application
    Filed: July 25, 2001
    Publication date: October 24, 2002
    Applicant: FORBES MEDI-TECH INC.
    Inventors: James P. Kutney, Radka K. Milanova, Yangbing Ding, Hongming Chen, Duanjie Hou
  • Patent number: 5776922
    Abstract: 1. A corticoid derivative of the general formula ##STR1## wherein R represents hydrogen, hydroxy, methyl or methylene; inclusive of the acylation product thereof where the 17-position of the steroid skeleton is hydroxy and the ketone form thereof where R is hydroxy, or a physiologically acceptable salt thereof.Since the corticosteroid derivative of this invention is readily soluble in water and has antiallergic, antiinflammatory and antioxidant activities, it can be used with advantage in the prevention and therapy of various allergic diseases, inflammatory diseases, cataract and various ischemic organ diseases.
    Type: Grant
    Filed: July 29, 1996
    Date of Patent: July 7, 1998
    Assignee: Senju Pharmaceutical Co., Ltd.
    Inventors: Kazumi Ogata, Hideki Tsuruoka, Takahiro Sakaue, Hidetoshi Nakao
  • 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: 5506354
    Abstract: Disclosed are amino substituted steroids (XI) which contain an imidazolylpiperazinyl group attached to the terminal carbon atom of the C.sub.17 -side chain which are useful as pharmaceutical agents for treating a number of conditions.
    Type: Grant
    Filed: December 1, 1992
    Date of Patent: April 9, 1996
    Assignee: The Upjohn Company
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
  • Patent number: 5462933
    Abstract: Bile acid derivatives, processes for their preparation and use as pharmaceuticals 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 enterohepatic 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.
    Type: Grant
    Filed: March 10, 1994
    Date of Patent: October 31, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Werner Kramer, Gunther Wess
  • Patent number: 5428181
    Abstract: A compound represented by the general formula: ##STR1## wherein A-O-denotes a residue of a compound having an estrogenic activity; R.sub.1 denotes H or a C.sub.1 -C.sub.6 alkyl group; X denotes a single bond, a C.sub.1 -C.sub.10 alkylene group or a group of the formula ##STR2## wherein R.sub.2 denotes H or a C.sub.1 -C.sub.5 alkyl group; Z denotes a nitro group or a halogen; n is an integer of 3 to 12; k is an integer of 1 to 5; L is an integer of 0 to 5; and q is an integer of 1 to 3,and physiologically acceptable salts thereof are disclosed.The compounds have a high affinity to bone tissues, and the compounds per se and metabolites thereof show significant therapeutic effect on bone diseases such as osteoporosis, rheumatoid arthritis and osteoarthritis.
    Type: Grant
    Filed: December 24, 1992
    Date of Patent: June 27, 1995
    Assignee: Hoechst Japan Limited
    Inventors: Tatsuo Sugioka, Mizuho Inazu
  • Patent number: 5372996
    Abstract: A method of treatment of androgen-related diseases such as prostate cancer in susceptible male animals, including humans, comprises administering novel antiandrogens and/or novel sex steroid biosynthesis inhibitors as part of a combination therapy. Sex steroid biosynthesis inhibitors, especially those capable of inhibiting conversion of dehydroepiandrosterone (DHEA) or 4-androstenedione (.DELTA..sup.4 -dione) to natural sex steroida (and testosterone into dihydrotestosterone) in peripheral tissues, are used in combination with antiandrogens usually after blockade of testicular hormonal secretions. Antiestrogens can also be part of the combination therapy. Pharmaceutical compositions and two, three, four and five component kits are useful for such combination treatment.
    Type: Grant
    Filed: October 19, 1992
    Date of Patent: December 13, 1994
    Assignee: Endorecherche, Inc.
    Inventor: Fernand Labrie
  • Patent number: 5215972
    Abstract: Steroids of the formula ##STR1## wherein R.sup.1 to R.sup.4, X and n have the significance given in the description, which lower the intestinal resorption of cholesterol and plasma cholesterol and a process of making same from corresponding steroids having an alcohol residue of the formula --O--X--OH in the 3-position.
    Type: Grant
    Filed: May 1, 1992
    Date of Patent: June 1, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Marie Cassal, Nigel Gains, Eva-Maria Gutknecht, Georges Hirth, Hans Lengsfeld
  • Patent number: 5183815
    Abstract: Described are new agents for treating bone disorders associated with a reduction in bone mass and abnormalities in bone resportion or bone formation including osteoporosis. Paget's disease, bone metastases and malignant hypercalcemia. The agents are hydroxyl containing steroidal hormones, having bone resportion antagonist or bone formation stimulatory activity, covalently linked through the hydroxyl group via a bond hydrolyzable in the human body, e.g. carbamate or carbonate, which is further covalently linked to an amino, or hydroxy substituted alkylidene-1,1-bisphosphonate, through the respective amino or hydroxy group. The alkyl bisphosphonate moiety confers bone affinity. The agent acts by delivering the steroidal hormone directly to the bone target site where it is released for bone resorption antagonist or bone formation stimulatory action by hydrolysis of the hydrolyzable covalent bond.
    Type: Grant
    Filed: February 19, 1992
    Date of Patent: February 2, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Walfred S. Saari, Gideon A. Rodan, Thorsten E. Fisher, Paul S. Anderson
  • Patent number: 5116830
    Abstract: This invention relates to a stereoisomerically pure .DELTA..sup.2 compound of the formula (I): ##STR1## wherein: R.sup.1 is hydrogen or --(C.dbd.O)--R.sup.2, wherein:R.sup.2 is an organic substituent selected from the group consisting of alkyls, alkenyls, alkynyls, cycloalkyls, cycloalkylalkylenes, haloalkyls, aryls, haloaryls and arylalkylenes, and their product by the process of:(a) reacting the 17.beta.-hydroxy group of 17.beta.-hydroxy-5.alpha.-estr-1-en-3-one with dihydropyran to produce the 3-keto-17.beta.-ether;(b) reducing the 3-keto-17.beta.-ether product of step (a) with lithium in ammonia;(c) reacting the product of step (b) with dialkyl chlorophosphate to produce the 3-substituted phosphate;(d) reducing the product of step (c) with lithium and ammonia to produce the .DELTA..sup.2 -protected-17.beta.-ether product;(e) hydrolysis of the produce of step (d) to product the .DELTA..sup.2 -17.beta.-hydroxy compound;(f) oxidizing the 17.beta.
    Type: Grant
    Filed: June 2, 1986
    Date of Patent: May 26, 1992
    Assignee: SRI International
    Inventors: Masato Tanabe, David F. Crowe, Richard H. Peters, John G. Johansson
  • Patent number: 5026882
    Abstract: The invention relates to 3-phosphinic acid steroidal compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: June 25, 1991
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • Patent number: 4946834
    Abstract: Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5.alpha.-reductase. Also invented are intermediates used in preparing these compounds.
    Type: Grant
    Filed: December 23, 1988
    Date of Patent: August 7, 1990
    Assignee: SmithKline Beecham Corporation
    Inventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
  • Patent number: 4939128
    Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, carboxylic acid acyl or carbamoyl which may be substituted; R is an aliphatic hydrocarbon group which may be substituted or alicylic hydrocarbon group which may be substituted, or a salt thereof.The compound of the present invention has the effects to prevent and improve dysfunctions caused by oxygen free radicals, and can be used as preventive and therapeutic drugs against dysfunctions in the circulatory system.
    Type: Grant
    Filed: April 5, 1989
    Date of Patent: July 3, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kaneyoshi Kato, Norio Shimamoto
  • Patent number: 4686309
    Abstract: The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl, either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl, or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and (i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.
    Type: Grant
    Filed: February 15, 1985
    Date of Patent: August 11, 1987
    Assignee: Rhone-Poulenc Sante
    Inventors: Jean-Claude Barriere, Jean-Pierre Corbet, Claude Cotrel, Daniel Farge, Jean-Marc Paris
  • Patent number: 4634695
    Abstract: Novel 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR1## wherein R.sub.1 is an organic radical of 1 to 18 carbon atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the atom immediately adjacent to the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of a pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, B and C together form a double bond or an epoxy group, the C.dbd.A group at position 3 is selected from the group consisting of C.dbd.O, ketal, which may be open or closed ##STR2## are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anti-glucocorticoid activity and a process for their preparation.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: January 6, 1987
    Assignee: Roussel Uclaf
    Inventors: Vesperto Torelli, Jean G. Teutsch, Daniel Philibert