Oxygen Bonded Directly To The Nitrogen (e.g., Oximes, Isonitrosos, Etc.) Patents (Class 552/519)
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Patent number: 9200028Abstract: Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders.Type: GrantFiled: March 22, 2013Date of Patent: December 1, 2015Assignee: Umecrine Cognition ABInventors: Torbjörn Bäckström, Gianna Ragagnin
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NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, PRODRUGS THEREOF, AND METHODS OF TREATMENT USING SAME
Publication number: 20140235600Abstract: The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: December 18, 2013Publication date: August 21, 2014Applicant: Washington UniversityInventors: Douglas Covey, Albert Jean Robichaud -
Publication number: 20130281421Abstract: Steroid compounds having increased resistance against metabolism and increased water solubility are disclosed, together with methods for their production. These substances are suitable for the manufacture of pharmaceuticals for the treatment of steroid related or steroid induced CNS disorders and for use in methods of prevention, alleviation or treatment of such disorders.Type: ApplicationFiled: March 22, 2013Publication date: October 24, 2013Inventors: Törbjorn Bäckström, Gianna Ragagnin
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Patent number: 8536160Abstract: Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. They are useful for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.Type: GrantFiled: April 11, 2007Date of Patent: September 17, 2013Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Alberto Cerri, Giorgio Fedrizzi, Alessandra Benicchio, Giuseppe Bianchi, Patrizia Ferrari, Mauro Gobbini, Rosamaria Micheletti, Marco Pozzi, Piero Enrico Scotti
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Patent number: 8435975Abstract: The present invention relates to steroidal esters of 17-oximino-5-androsten-3-ol, of compound of general formula (A) wherein R is selected from a group consisting of arylalkyl, aryl, substituted aryl. The ester derivatives are synthesized starting from Dehydroandrosterone acetate. The compounds were tested for their antiproliferative activity and 5?-reductase inhibitory activity in comparison to Finasteride. Decreased androgen level have been found in serum of animal treated with newly synthesized compounds. These compounds have also shown better cytotoxicity in comparison to reference drug Finasteride. Thus such compounds can be useful in treatment of androgen dependent disorder of prostate alone or by synergistic effect they can decrease the size of prostate due to their antiproliferative activity.Type: GrantFiled: August 14, 2008Date of Patent: May 7, 2013Assignee: Council of Scientific & Industrial ResearchInventors: Tilak Raj Bhardwaj, Manoj Kumar, Neelima Dhingra, Neraj Mehta
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Patent number: 7910571Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.Type: GrantFiled: October 13, 2006Date of Patent: March 22, 2011Assignee: Harbor BioSciences, Inc.Inventor: James M. Frincke
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Publication number: 20100292201Abstract: The present invention relates to steroidal esters of 17-oximino-5-androsten-3-ol, of compound of general formula (A) wherein R is selected from a group consisting of arylalkyl, aryl, substituted aryl. The ester derivatives are synthesized starting from Dehydroandrosterone acetate. The compounds were tested for their antiproliferative activity and 5?-reductase inhibitory activity in comparison to Finasteride. Decreased androgen level have been found in serum of animal treated with newly synthesized compounds. These compounds have also shown better cytotoxicity in comparison to reference drug Finasteride. Thus such compounds can be useful in treatment of androgen dependent disorder of prostate alone or by synergistic effect they can decrease the size of prostate due to their antiproliferative activity.Type: ApplicationFiled: August 14, 2008Publication date: November 18, 2010Inventors: Tilak Raj Bhardwaj, Manoj Kumar, Neelima Dhingra, Neeraj Mehta
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Patent number: 7304171Abstract: 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.Type: GrantFiled: May 26, 2005Date of Patent: December 4, 2007Assignee: Migenix Corp.Inventor: Yazhong Pei
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Patent number: 7135581Abstract: 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: GrantFiled: August 24, 2001Date of Patent: November 14, 2006Assignee: 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
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Patent number: 6995278Abstract: 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: GrantFiled: February 8, 2001Date of Patent: February 7, 2006Assignee: Entre Med, Inc.Inventors: Gregory E. Agoston, Victor Pribluda, Anthony M. Treston, Shawn J. Green
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Patent number: 6852710Abstract: 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: GrantFiled: April 11, 2003Date of Patent: February 8, 2005Assignee: Southwest Foundation for Biomedical ResearchInventors: Pemmaraju Narasimha Rao, Susan L. Mooberry, James W. Cessac, Tina L. Tinley
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Publication number: 20040059140Abstract: Disclosed are androgen-related steroids having a &Dgr;14 double bond and carrying a substituent at either or both of the carbon atoms nos. 15 and 16. The present steroids are characterized by possessing a mixed profile of androgenic and progestagenic activities. This makes these compounds suitable for male or female hormone replacement therapy, as well as male contraception.Type: ApplicationFiled: October 1, 2003Publication date: March 25, 2004Inventors: Japp Van Der Louw, Dirk Leysen, Marcel Evert De Gooyer
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Patent number: 6670353Abstract: A sulphamate compound suitable for use as an inhibitor of oestrone sulphatase (E.C.3.1.6.2) is described. The compound is a polycyclic compound comprising at least two ring components, wherein the polycyclic compound comprises at least one sulphamate group attached to at least one of the ring components, and wherein at least one oxime group is attached to or is part of at least one of the ring components.Type: GrantFiled: May 17, 2000Date of Patent: December 30, 2003Assignee: Sterix LimitedInventors: Michael John Reed, Barry Victor Lloyd Potter
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Publication number: 20030229061Abstract: 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: ApplicationFiled: April 11, 2003Publication date: December 11, 2003Applicant: SOUTHWEST FOUNDATION FOR BIOMEDICAL RESEARCHInventors: Pemmaraju Narasimha Rao, Susan L. Mooberry, James W. Cessac, Tina L. Tinley
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Patent number: 6596885Abstract: 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: GrantFiled: June 26, 2001Date of Patent: July 22, 2003Assignee: Aventis Pharma S.A.Inventors: Andre Claussner, Francois Nique, Jean-Georges Teutsch, Patrick Van de Velde
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Patent number: 6579864Abstract: The invention concerns a 3-methylene steroid derivative having general formula (1) wherein R1 is H or together with R3 forms a &bgr;-epoxide or R1 is absent if there is a 5-10 or 4-5 double bond; R2 is (C1-C5) alkyl or CF3; R3 is &bgr;H, &bgr;CH3 or together with R1 forms a &bgr;-epoxide or R3 is absent if there is a 5-10 double bond; R4 is H, lower alkyl; Y is [H, H], [OH, H], ═O, [OH, lower alkyl], [OH, (C2-C5)alkenyl], [OH, (C2-C5)alkynyl] or (C1-C6) alkylidene, whereby said alkyl, alkenyl, alkynyl and alkylidene is optionally halogenated; ═NOR5, whereby R5 is H, lower alkyl; dotted lines represent an optional double bond, or prodrugs thereof for the treatment of arthritic diseases and/or autoimmune diseases.Type: GrantFiled: May 29, 2002Date of Patent: June 17, 2003Assignee: Akzo Nobel NVInventors: Ralf Plate, Wilhelmina Maria Bagchus
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Patent number: 6518262Abstract: The invention relates to 22R-hydroxycholesta-8,14-diene derivatives having general formula (I) wherein R1 is OR, OS03H or ═NOR; with R being H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is independently hydrogen or (C1-6)alkyl; R4 is hydrogen, (C1-6)alkyl or (C1-6)acyl; R5 is hydrogen; or R5 designates, together with R6, an additional bond between the carbon atoms at which R5 and R6 are placed; R6 is hydrogen, hydroxy or halogen; or R6 designates, together with R5, an additional bond between the carbon atoms at which R6 and R5 are placed; each of R7 and R8 is independently hydrogen or (C1-4)alkyl, optionally substituted with OH, (C1-4)alkoxy, or halogen; or a pharmaceutically acceptable salt thereof. The compounds of the invention have meiosis inhibiting activity and can be used for the control of fertility.Type: GrantFiled: August 22, 2001Date of Patent: February 11, 2003Assignee: Akzo Nobel N.V.Inventors: D. Leysen, J. van der Louw, R. G. J. M. Hanssen, Anja Wiersma
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Publication number: 20020183283Abstract: Certain novel sterol derivatives can be used for regulating the meiosis in oocytes and in male germ cells.Type: ApplicationFiled: June 4, 2002Publication date: December 5, 2002Inventors: Peter Faarup, Frederick Christian Gronvald, Thorsten Blume, Anthony Murray, Jens Breinholt
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Patent number: 6303589Abstract: The present invention relates to fungicidally effective compositions containing at least one pentacyclic triterpene compound.Type: GrantFiled: December 8, 1998Date of Patent: October 16, 2001Assignee: Micro Flo CompanyInventors: Jan Glinski, Keith L. Branly
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Patent number: 6262282Abstract: The invention relates to 17&bgr;-allyloxy(thio)alkyl-androstane derivatives having general formula (I) wherein R1 is (H, OR), (H, OSO3H) or NOR; with R being H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is independently hydrogen or (C1-6)alkyl; n is 0, 1 or 2; X is O, S, S(O) or S(O)2; each of R4 and R5 is independently hydrogen or (C1-4)alkyl; each of R6, R7 and R8 is independently hydrogen, phenyl, halogen or (C1-4)alkyl, optionally substituted by hydroxy, (C1-4) alkoxy or halogen; or R7 and R8 together with the carbon atom to which they are bound form a (C3-6)cycloalkane ring; or R6 and R7 together with the carbon atoms to which they are bound form a (C5-6) cycloalkene ring; and wherein the dotted lines indicate a &Dgr;7 or a &Dgr;8 double bond, or a pair of conjugated double bonds selected from &Dgr;7,14, &Dgr;8,14 and &Dgr;6,8(14); or a pharmaceutically acceptable salt thereof. The compounds of the invention have meiosis activating activity and can be used for the control of fertility.Type: GrantFiled: December 3, 1999Date of Patent: July 17, 2001Assignee: Akzo Nobel N.V.Inventors: Johannes Antonius Joseph Leemhuis, Jaap van der Louw, Marinus Bernard Groen
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Patent number: 6180803Abstract: The invention relates to compounds of the formula: in which R1, R2, R3, R4, R5, R6, n and X are as defined in the specification, and to pharmaceutical compositions containing them. These compounds are excellent progestogens which are devoid of residual androgenic activity.Type: GrantFiled: November 5, 1998Date of Patent: January 30, 2001Assignee: Laboratoire TheramexInventors: Alain Piasco, Jean Lafay, R{acute over (e)}mi Delansorne, Jacques Paris, Jean-Claude Pascal
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Patent number: 6177420Abstract: The invention relates to 20-aralkyl-5&agr;-pregnane derivative having general formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 is (H,OR), (H,OSO3H) or NOR; R is H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 is independently hydrogen or (C1-6)alkyl; X is a straight chain divalent C1-8 hydrocarbon radical, optionally comprising a double or a triple bond; or X is —(CH2)m—CR7R8—; m=0-4; at least one of R7 and R8 is (C1-4)alkyl, hydroxy, (C1-4)alkoxy or halogen; the other, if present, being hydrogen; or R7 and R8 together represent O or NOR′; R′ is H, (C1-6)alkyl or (C1-6)acyl; each of R4, R5 and R6 is independently hydrogen, hydroxy, (C1-4)alkoxy, halogen, NR9, R10 or (C1-4)alkyl, optionally substituted by hydroxy, alkoxy, halogen or oxo; each of R9 and R10 is independently hydrogen or (C1-4)alkyl; and the dotted lines indicate a &Dgr;7 or a &Dgr;8 double bond, or a pair of conjugated double bonds selected from &Dgr;7,14, &Dgr;8,14 andType: GrantFiled: November 12, 1999Date of Patent: January 23, 2001Assignee: Akzo Nobel N.V.Inventors: Johannes Antonius Joseph Leemhuis, Jaap van der Louw, Marinus Bernard Groen
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Patent number: 6136992Abstract: 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: GrantFiled: March 12, 1998Date of Patent: October 24, 2000Assignees: The United States of America as represented by the Department of Health and Human Services, Pharm-Eco Laboratories, IncorporatedInventors: Siya Ram, Ravi Varma, Yesh Sachdeva
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Patent number: 5194602Abstract: New 9.alpha.-hydroxy-17-methylene steroids are prepared by the introduction of a substituted 17-methylene group in 9.alpha.-hydroxyandrost-4-ene-3, 17-dione.The resulting compounds are useful starting compounds in the synthesis of corticosteroids.Type: GrantFiled: December 12, 1990Date of Patent: March 16, 1993Assignee: Gist-Brocades N.V.Inventors: Jacobus N. M. Batisi, Arthur F. Marx
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Patent number: 5182381Abstract: Novel 3-keto-19-nor-.DELTA..sup.4,9 -steroids of the formula ##STR1## and their non-toxic, pharmaceutically acceptable acid addition salts possessing a remarkable antiglucocorticoidal activity.Type: GrantFiled: September 10, 1991Date of Patent: January 26, 1993Assignee: Roussel UlcafInventors: Daniel Philibert, Jean G. Teutsch, Germain Costerousse, Roger Deraedt
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Patent number: 5162312Abstract: 11.beta.-substituted-16.alpha., 17.alpha.-methylene-estra-4,9-dien-3-ones of formula I ##STR1## wherein R.sup.1 is a methyl or ethyl group;R.sup.2 is H; a C.sub.1-6 -alkyl, -alkoxymethyl, -alkanoyl or -alkoxcarbonyl group ; 2-methoxyethyl; 2-hydroxyethyl; 2-C.sub.1-4 -alkanoyloxyethyl; or a tri-C.sub.1-4 -alkylsilyl group;R.sup.3 is vinyl; a C.sub.1-6 -alkyl; or a phenyl radical para-substituted by --OCH.sub.3, --SCH.sub.3, --N(CH.sub.3), --CN, --CHO, CH.sub.3 CO--, CH.sub.3 CHOH-- or --CH.sub.2 OH;R.sup.6 is H or a C.sub.1-4 -alkyl group;X is O, a hydroxy- or methoxyimino group (.dbd.N.about.OH or --N.about.OCH.sub.3), or a cyclic thioketal with 2 or 3 carbon ring atomsare provided, as well as pharmaceutical compositions containing said compounds, methods of use of said compounds, and processes for their production.Type: GrantFiled: August 15, 1990Date of Patent: November 10, 1992Assignee: Schering AktiengesellschaftInventors: Helmut Kasch, Reimar Krieg, Anatoil Kurischko, Kurt Ponsold
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Patent number: 5132299Abstract: New 11.beta. phenyl-4,9,15-estratrienes of formula I ##STR1## are described, where X implies an oxygen atom or a hydroxyimino grouping N.about.OH,R.sup.1 stands for a hydrogen atom or a methyl group,R.sup.2 implies a hydrogen atom, an alkyl radical or an acyl radical with in each case 1 to 10 carbon atoms,R.sup.3 stands for a hydrogen atom, a cyanomethyl group, --(CH.sub.2).sub.n CH.sub.2 Z where n implies the numbers 0, 1, 2, 3, 4 or 5, Z=--H or --OR.sup.5 with R.sup.5 having the significance of a hydrogen atom or an alkyl or acyl group with in each case 1 to 10 carbon atoms, or for --(CH.sub.2).sub.m --C.tbd.C--Y where m=0-2 and Y implies a hydrogen, chlorine, fluorine, iodine or bromine atom, an alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl group with in each case 1 to 10 carbon atoms,R.sup.4 represents a straight-chain or branched-chain, saturated or unsaturated hydrocarbon radical with up to 8 carbon atoms which contains the grouping ##STR2## with X having the above significance.Type: GrantFiled: January 16, 1990Date of Patent: July 21, 1992Assignee: Schering AktiengesellschaftInventors: Eckhard Ottow, Helmut Hofmeister, Stefan Scholz, Guenter Neef, Walter Elger, Sybille Beier, Krzysztof Chwalisz
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Patent number: 5086047Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl, alkylthio and haloalkyl of 1 to 6 carbon atoms, alkenyl and alkynyl of 2 to 6 carbon atoms, optionally substituted arylthio of 6 to 10 carbon atoms, aryl of 6 to 12 carbon atoms, acyl of an organic carboxylic acid of 1 to 12 carbon atoms, --CN, cycloalkyl of 3 to 6 carbon atoms and --(CH.sub.2).sub.m --Re, m is an integer from 1 to 3, Re is --OH or --SH or --Salk, Alk is alkyl of 1 to 6 carbon atoms, X is selected from the group consisting of oxygen, N--O--R.sub.1, ##STR2## or =X is H.sub.2 or ##STR3## R.sub.A and R.sub.B are individually selected from the group consisting of hydrogen, halogen and alkyl of 1 to 6 carbon atoms, R.sub.1 is hydrogen or alkyl of 1 to 6 carbon, R' is hydrogen or acyl, the wavy lines indicate --or -position, Y is selected from the group consisting of oxygen, NOR, ##STR4## or =Y is ##STR5## H.sub.Type: GrantFiled: December 24, 1990Date of Patent: February 4, 1992Assignee: Roussel Uclaf, Department des BrevetsInventors: Jean-Francois Gourvest, Dominique Lesuisse
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Patent number: 5034548Abstract: 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: GrantFiled: October 16, 1990Date of Patent: July 23, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventors: James L. Gaylor, Paul R. Johnson, Soo S. Ko, Ronald L. Magolda, Simon H. Stam, James M. Trzaskos