Abstract: 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.
Inventors:
Alberto Cerri, Giorgio Fedrizzi, Alessandra Benicchio, Giuseppe Bianchi, Patrizia Ferrari, Mauro Gobbini, Rosamaria Micheletti, Marco Pozzi, Piero Enrico Scotti
Abstract: 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.
Abstract: An object of the present invention is to provide a novel method for producing a steroid compound. The present invention provides a method for producing 3,7-dioxo-5?-cholanic acid or ester derivatives thereof, which uses, as raw materials, sterols having double bonds at positions 5 and 24, such as cholesta-5,7,24-trien-3?-ol, ergosta-5,7,24(28)-trien-3?-ol, desmosterol, fucosterol, or ergosta-5,24(28)-dien-3?-ol, and which comprises the following 4 steps: (I) a step of performing oxidation of a hydroxyl group at position 3 and isomerization of a double bond at position 5 to position 4; (II) a step of converting position 24 to a carboxyl group or an ester derivative thereof by the oxidative cleavage of a side chain; (III) a step of introducing an oxygen functional group into position 7; and (IV) a step of constructing a 5?-configuration by reduction of a double bond at position 4.
Type:
Application
Filed:
June 30, 2010
Publication date:
January 13, 2011
Applicant:
MITSUBISHI CHEMICAL GROUP SCIENCE AND TECHNOLOGY RESEARCH CENTER, INC.
Abstract: The present invention relates to steroid hormone products, such as oral contraceptive products, including at least one steroid active ingredient mixed with an excipient and having improved dissolution and release rate properties. The invention further relates to methods for making such steroid hormone products, wherein a mixture of the hormone and the excipient is subjected to sufficient mechanical energy to form a powder blend wherein the hormone is stabilized by the excipient in substantially non-crystalline form.
Type:
Grant
Filed:
December 13, 2001
Date of Patent:
January 11, 2011
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Thomas Schultz, Bradley A. Clark, Angela Falzone
Abstract: 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.
Abstract: The invention relates to a method for the production of 4-(17&agr; substituted 3-oxoestra-4,9-dien-11&bgr;-yl)benzaldehyd-(1E or 1Z)-oximes of general formula (I), where R1═H, C1-6 alkyl or a CnF2n+1 group; R2═C1-4 alkyl, X=E- or Z-OH; and Y═O—C1-6 alkyl, S—C1-6 alkyl or O—CH2CnF2n+1, where n=1, 2 or 3, which produces the target compounds of formula (I) with high yield and selectivity.
Abstract: 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.
Abstract: Certain compounds, structurally related to natural compounds which can be extracted i.a. from bull testes and from human follicular fluid, can be used for regulating the meiosis in oocytes and in male germ cells. Some of these compounds are useful in the treatment of infertility, whereas other compounds are useful as contraceptives.
Type:
Application
Filed:
September 11, 2002
Publication date:
February 13, 2003
Inventors:
Christian Grondahl, Frederik Christian Gronvald, Peter Faarup, Anthony Murray, Jan Lund Ottesen
Abstract: 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:
Grant
Filed:
August 22, 2001
Date of Patent:
February 11, 2003
Assignee:
Akzo Nobel N.V.
Inventors:
D. Leysen, J. van der Louw, R. G. J. M. Hanssen, Anja Wiersma
Abstract: The invention concerns compounds of formula (I) wherein: X, Y, R1, R2, Z, G are as defined in the description, the methods for preparing them and the intermediates in said method, their use as medicine and the pharmaceutical compositions containing them.
Type:
Grant
Filed:
December 17, 2001
Date of Patent:
December 31, 2002
Assignees:
Aventis Pharma S.A., Genentech
Inventors:
Denis Carniato, Thomas R. Gadek, Jochen Knolle, Jean-Francois Gourvest, Anurschirwan Peyman, Sarah C. Bodary
Abstract: The present invention relates to steroid hormone products, such as oral contraceptive products, including at least one steroid active ingredient mixed with an excipient and having improved dissolution and release rate properties. The invention further relates to methods for making such steroid hormone products, wherein a mixture of the hormone and the excipient is subjected to sufficient mechanical energy to form a powder blend wherein the hormone is stabilized by the excipient in substantially non-crystalline form.
Type:
Application
Filed:
December 13, 2001
Publication date:
November 21, 2002
Inventors:
Thomas Schultz, Bradley A. Clark, Angela Falzone
Abstract: 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:
Grant
Filed:
December 3, 1999
Date of Patent:
July 17, 2001
Assignee:
Akzo Nobel N.V.
Inventors:
Johannes Antonius Joseph Leemhuis, Jaap van der Louw, Marinus Bernard Groen
Abstract: The invention relates to 17&bgr;-aryl(arylmethyl)oxy(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)alyl; n is 0, 1, or 2; X is O, S, S(O) or S(O)2; m is 0 or 1; each of R4, R5 and R6 is independently hydrogen, hydroxy, (C1-4)alkoxy, halogen, NR7R8 or (C1-4)alkyl, optionally substituted by hydroxy, alkoxy, halogen or oxo; each of R7 and R8 is independently hydrogen or (C1-4)alkyl, 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 regulating activity and can be used for the control of fertility.
Abstract: 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:
Grant
Filed:
November 5, 1998
Date of Patent:
January 30, 2001
Assignee:
Laboratoire Theramex
Inventors:
Alain Piasco, Jean Lafay, R{acute over (e)}mi Delansorne, Jacques Paris, Jean-Claude Pascal
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