Phosphorus Attached Directly Or Indirectly To The Cyclopentanohydrophenanthrene Ring System By Nonionic Bonding Patents (Class 540/5)
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Publication number: 20150140088Abstract: 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: ApplicationFiled: December 27, 2012Publication date: May 21, 2015Inventors: Laura Garcia Pupo, Yanier Nuñez Figueredo, Juan Enrique Tacoronte Morales, Yamila Verdecia Reyes, Estael Ochoa Rodriguez, Zaldo Castro Armando
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Publication number: 20150038472Abstract: 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: ApplicationFiled: October 21, 2014Publication date: February 5, 2015Inventor: Wolfgang STREMMEL
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Patent number: 8895723Abstract: Disclosed herein are methods of preparing a phosphorothioate nucleotide analog, which are useful in treating diseases and/or conditions such as viral infections.Type: GrantFiled: March 18, 2013Date of Patent: November 25, 2014Assignees: 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
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Publication number: 20130004425Abstract: Drug carriers, methods of synthesizing, and methods of use thereof are provided.Type: ApplicationFiled: February 7, 2011Publication date: January 3, 2013Inventors: Dong Wang, Xin-Ming Liu
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COMPOSITIONS AND METHODS FOR ENHANCING CELLULAR UPTAKE AND INTRACELLULAR DELIVERY OF LIPID PARTICLES
Publication number: 20120264810Abstract: 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 subjectType: ApplicationFiled: September 22, 2010Publication date: October 18, 2012Applicant: The University of British ColumbiaInventors: Paulo J.C. Lin, Yuen Yi c. Tam, Srinivasulu Masuna, Marco A. Ciufolini, Michel Roberge, Pieter R. Cullis -
Publication number: 20120010173Abstract: 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: ApplicationFiled: March 3, 2010Publication date: January 12, 2012Applicant: SEPS PHARMA N.V.Inventors: Yves Rene Johanna Paul Gonnissen, Jody Firmin Marceline Voorspoels
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Publication number: 20110312916Abstract: 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: ApplicationFiled: February 5, 2010Publication date: December 22, 2011Applicant: TOKAI PHARMACEUTICALS, INC.Inventor: David Casebier
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Publication number: 20100075314Abstract: 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: ApplicationFiled: May 26, 2009Publication date: March 25, 2010Inventors: Viswanadham Garimella, Thomas F. Holzman, Yijia P. Bao
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Publication number: 20090286973Abstract: This invention relates composition and methods for making and using chemically modified oligonucleotides agents for inhibiting gene expression.Type: ApplicationFiled: July 2, 2009Publication date: November 19, 2009Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah MANOHARAN, Venkitasamy KESAVAN, Kallanthottathil G. RAJEEV
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Patent number: 7479486Abstract: 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: GrantFiled: May 6, 2005Date of Patent: January 20, 2009Assignee: Laboratoires Serono SAInventors: Gerardo Burton, Carlos P. Lantos, Adriana Silvia Veleiro
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Patent number: 7071328Abstract: 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: GrantFiled: September 17, 2001Date of Patent: July 4, 2006Assignee: Applied Research System ARS Holding N.V.Inventors: Gerardo Burton, Carlos P. Lantos, Adriana Silvia Veleiro
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Publication number: 20040157810Abstract: 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: ApplicationFiled: August 22, 2003Publication date: August 12, 2004Inventors: Martin H. Teicher, Susan L. Andersen-Navalta
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Publication number: 20040092733Abstract: 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: ApplicationFiled: July 18, 2003Publication date: May 13, 2004Inventors: Gerardo Burton, Carlos P Lantos, Adriana Silvia Veleiro
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Publication number: 20030232981Abstract: The present invention involves intermediates, including a 7&agr;-substituted steroid (II), 1Type: ApplicationFiled: March 21, 2003Publication date: December 18, 2003
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Publication number: 20020156051Abstract: Novel phytosterol and/or phytostanol derivatives, including salts thereof, are represented by the general formulae: 1Type: ApplicationFiled: July 25, 2001Publication date: October 24, 2002Applicant: FORBES MEDI-TECH INC.Inventors: James P. Kutney, Radka K. Milanova, Yangbing Ding, Hongming Chen, Duanjie Hou
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Patent number: 5776922Abstract: 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: GrantFiled: July 29, 1996Date of Patent: July 7, 1998Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Kazumi Ogata, Hideki Tsuruoka, Takahiro Sakaue, Hidetoshi Nakao
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Patent number: 5646272Abstract: 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: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Hoechst AktiengesellschaftInventors: Werner Kramer, Gunther Wess
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Patent number: 5506354Abstract: 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: GrantFiled: December 1, 1992Date of Patent: April 9, 1996Assignee: The Upjohn CompanyInventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer, Harold A. Karnes
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Patent number: 5462933Abstract: 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: GrantFiled: March 10, 1994Date of Patent: October 31, 1995Assignee: Hoechst AktiengesellschaftInventors: Werner Kramer, Gunther Wess
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Patent number: 5428181Abstract: 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: GrantFiled: December 24, 1992Date of Patent: June 27, 1995Assignee: Hoechst Japan LimitedInventors: Tatsuo Sugioka, Mizuho Inazu
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Patent number: 5372996Abstract: 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: GrantFiled: October 19, 1992Date of Patent: December 13, 1994Assignee: Endorecherche, Inc.Inventor: Fernand Labrie
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Patent number: 5215972Abstract: 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: GrantFiled: May 1, 1992Date of Patent: June 1, 1993Assignee: Hoffmann-La Roche Inc.Inventors: Jean-Marie Cassal, Nigel Gains, Eva-Maria Gutknecht, Georges Hirth, Hans Lengsfeld
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Patent number: 5183815Abstract: 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: GrantFiled: February 19, 1992Date of Patent: February 2, 1993Assignee: Merck & Co., Inc.Inventors: Walfred S. Saari, Gideon A. Rodan, Thorsten E. Fisher, Paul S. Anderson
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Patent number: 5116830Abstract: 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: GrantFiled: June 2, 1986Date of Patent: May 26, 1992Assignee: SRI InternationalInventors: Masato Tanabe, David F. Crowe, Richard H. Peters, John G. Johansson
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Patent number: 5026882Abstract: 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: GrantFiled: December 23, 1988Date of Patent: June 25, 1991Assignee: SmithKline Beecham CorporationInventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
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Patent number: 4946834Abstract: 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: GrantFiled: December 23, 1988Date of Patent: August 7, 1990Assignee: SmithKline Beecham CorporationInventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
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Patent number: 4939128Abstract: 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: GrantFiled: April 5, 1989Date of Patent: July 3, 1990Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Norio Shimamoto
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Patent number: 4686309Abstract: 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: GrantFiled: February 15, 1985Date of Patent: August 11, 1987Assignee: Rhone-Poulenc SanteInventors: Jean-Claude Barriere, Jean-Pierre Corbet, Claude Cotrel, Daniel Farge, Jean-Marc Paris
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Patent number: 4634695Abstract: 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: GrantFiled: January 22, 1985Date of Patent: January 6, 1987Assignee: Roussel UclafInventors: Vesperto Torelli, Jean G. Teutsch, Daniel Philibert