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| Number | Title | Issue Date |
| 7196074 | Methods of making, using and pharmaceutical formulations comprising 7α, 11β-dimethyl-17β-hydroxyestra-4, 14-dien-3-one and 17 esters thereof Methods of using 7α,11β-dimethyl-17β-hydroxyestra-4,14-dien-3-one (III) and 17 esters thereof for various hormonal therapies, oral and parenteral dosage forms comprising these actives, and processes for their ... | 03/27/2007 |
| 7109360 | 16-hydroxyestratrienes as selectively active estrogens The invention describes new compounds as pharmaceutical active ingredients, which have in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo a preferential action on bone rat... | 09/19/2006 |
| 7037907 | Estradiol conjugates and uses thereof A conjugated prodrug of an estradiol compound conjugated to a biological activity modifying agent. ... | 05/02/2006 |
| 6780854 | Orally active androgens Novel, orally active androgens are 7α-substituted Δ14-nandrolone derivatives. The compounds satisfy the general formula: wherein R1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C1... | 08/24/2004 |
| 6596885 | 19-Nor steroids having a thiocarbonated chain in position 11beta, their preparation process and the intermediates of this process, their use as medicaments and compositions Novel compounds having a formula selected from the group consisting of ##STR1## 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-prolife... | 07/22/2003 |
| 6579864 | 3-methylene steroid derivatives The invention concerns a 3-methylene steroid derivative having general formula (1) wherein R1 is H or together with R3 forms a ଲ-epoxide or R1 is absent if there is a 5-10 or 4-5 double bond; R2 is (C... | 06/17/2003 |
| 6518262 | 22R-hydroxycholesta-8, 14-diene derivatives for the inhibition of meiosis The invention relates to 22R-hydroxycholesta-8,14-diene derivatives having general formula (I) wherein R1 is OR, OS03 H or .dbd.NOR; with R being H, (C1-6)alkyl or (C1-6)acyl; each of R2 and R3 ... | 02/11/2003 |
| 6413951 | 20-fluoro-17(20)-vinyl steroids The invention relates to 20.xi.-fluoropregna-4,17(20)-dien-3-on-21-oic acid ethyl ester, 20.xi.-fluoro-3ଲ-hydroxypregna-5,17(20)-dien-21-oic acid ethyl ester, 20.xi.-fluoro-21-hydroxypregna-4,17 (20)-dien-3-one, 20.xi.-fluoropregna-5,17(20)-dien-3&#... | 07/02/2002 |
| 6262042 | 17ଲ-amino and hydroxylamino-11ଲ-arylsteroids and their derivatives having agonist or antagonist hormonal properties The invention is directed to a novel class of steroids which exhibit potent antiprogestational activity.... | 07/17/2001 |
| 6262282 | 17ଲ-allyloxy(thio)alkyl-androstane derivatives for the modulation of meiosis The invention relates to 17ଲ-allyloxy(thio)alkyl-androstane derivatives having general formula (I) wherein R1 is (H, OR), (H, OSO3 H) or NOR; with R being H, (C1-6)alkyl or (C1-6)acyl; each of R2 | 07/17/2001 |
| 6251887 | 17ଲ-aryl(arylmethyl)oxy(thio)alkyl-androstane derivatives The invention relates to 17ଲ-aryl(arylmethyl)oxy(thio)alkyl-androstane derivatives having general formula (I), wherein R1 is (H,OR), (H,OSO3 H) or NOR; with R being H, (C1-6)alkyl or (C1-6)acyl; each of R | 06/26/2001 |
| 6180803 | 19-nor-pregnene derivatives and pharmaceuticals containing such derivatives The invention relates to compounds of the formula: ##STR1## in which R1, R2, R3, R4, R5, R6, n and X are as defined in the specification, and to pharmaceutical compositions containing them.... | 01/30/2001 |
| 6046186 | Estrone sulfamate inhibitors of estrone sulfatase, and associated pharmaceutical compositions and methods of use Novel compounds useful as inhibitors of estrone sulfatase are provided. The compounds have the structural formula (I) wherein r1 is an optional double bond, R1 and R2 are selected from the group consisting of hydrogen and lower alky,... | 04/04/2000 |
| 5990328 | Process for the preparation of 4-amino-Ɗ4-3-ketosteroids via 4-nitro-Ɗ4-3-ketosteroids The present invention provides 4-nitro-Ɗ4 -3-ketosteroids, their use as steroid C17-20 lyase and 5-reductase inhibitors and to a novel process for preparing a compound of the formula: ##STR1## comprising sequentially: a)... | 11/23/1999 |
| 5965550 | Process for the preparation of 4-amino-Ɗ4 -3-ketosteroids via 4-nitro-Ɗ4 -3-ketosteroids The invention discloses 3-ketosteroids of the following formula used to inhibit steroid C17-20 lyase: ##STR1## wherein R is OH, C1 -C6 alkanoyl, C1 -C6 alkanoyloxy, C1 -C4 a... | 10/12/1999 |
| 5952319 | Androgenic steroid compounds and a method of making and using the same An androgenic steroid compound of the formula: ##STR1## wherein: X, Y, Z, R1, R2, R3, R5 and R6 are as defined herein.... | 09/14/1999 |
| 5922703 | Urethane-containing aminosteroid compounds Urethane-containing amino steroids having the general chemical formula: ##STR1## wherein a, b, R1, R2, R3, R4, R14 and Z are as defined in the specification. Also disclosed are pharmaceutical com... | 07/13/1999 |
| 5902888 | Synthesis of 6-functionalized estriol haptens and protein conjugates thereof Disclosed are 6-derivatized estriol compounds which, when conjugated to a protein, are useful in the in vivo preparation of antibodies specific to estriol. When labeled with a detectable label, the estriol derivatives are useful as haptens in a com... | 05/11/1999 |
| 5892069 | Estrogenic compounds as anti-mitotic agents The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found belo... | 04/06/1999 |
| 5750744 | Process for the preparation of 4-amino- 4-3-ketosteroids via 4-nitro- 4-3-ketosteroids The present invention provides 4-nitro-Ɗ4 -3-ketosteroids, their use as steroid C17-20 lyase and 5-reductase inhibitors and to a novel process for preparing a compound of the formula: ##STR1## comprising sequentially: a)... | 05/12/1998 |
| 5646316 | Bile acid inhibitors of metalloproteinase enzymes 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 ... | 07/08/1997 |
| 5502044 | Fluorinated 4-aminoandrostadienone derivatives and process for their preparation The present invention relates to a compound of formula (I) ##STR1## wherein (x) and (y) are single or double bonds; A is a ##STR2## R and R3 are hydrogen or acyl; R1 is hydrogen or fluorine; and wherein: when (y) is a single bon... | 03/26/1996 |
| 5486511 | 4-amino-17ଲ-(cyclopropyloxy)androst-4-en-3-one, 4-amino-17ଲ-(cyclopropylamino)androst-4-en-3-one and related compounds as C17-20 lyase and 5-reductase This invention is directed to 4-amino-17ଲ-(cyclopropyloxy)androst-4-en-3-one, 4-amino-17ଲ-(cyclopropylylamino)androst-4-en-3-one and related compounds, a process for their synthesis, a pharmaceutical composition having C17-20 l... | 01/23/1996 |
| 5486603 | Oligonucleotide having enhanced binding affinity The present invention relates to an oligonucleotide or analog thereof conjugated to a molecule comprising a structure, which structure (a) is of substantially fixed conformation; (b) contains, is directly attached to, or is attached to a carbon atom that ... | 01/23/1996 |
| 5372996 | Method of treatment of androgen-related diseases 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 st... | 12/13/1994 |
| 5241090 | Process for the preparation of 4-amino-unsaturated androstanedione derivatives 4-amino-unsaturated androstanedione derivatives provided with aromatase inhibitory activity are obtained by hydrolyzation of a corresponding compound of formula II ##STR1##... | 08/31/1993 |
| 5218110 | 4-amino-Ɗ4 -steroids and their use as 5-reductase inhibitors The present invention relates to 4-azido-Ɗ4 -steroids which are useful as inhibitors of 5-reductase. The compounds are prepared by the reaction of an appropriate 4-azido steroid with triphenylphosphine in an aqueous inert solvent with h... | 06/08/1993 |
| 5194602 | 9-hydroxy-17-methylene steroids, process for their preparation and their use in the preparation of corticosteroids New 9-hydroxy-17-methylene steroids are prepared by the introduction of a substituted 17-methylene group in 9-hydroxyandrost-4-ene-3, 17-dione. The resulting compounds are useful starting compounds in the synthesis of corticosteroids.... | 03/16/1993 |
| 5189032 | 4-amino-Ɗ4,6 -steroids and their use as 5-reductase inhibitors The present invention relates to 4-amino-Ɗ4,6 -steroids which are useful as inhibitors of 5-reductase. The compounds are prepared by the reaction of an appropriate 4,5-epoxy steroid with sodium azide in an inert solvent in the presence ... | 02/23/1993 |
| 5143909 | Aminosteroids in a method for inhibiting C17-20 lyase The present invention relates to a method for the inhibition of C17-20 lyase enzyme which comprises administering to a patient in need of such inhibition, an effective amount of certain 4-amino-17-(hydroxyalkyl or dihydroxyalkyl)steroids or the... | 09/01/1992 |
| 5130424 | 4-amino-delta-4,6-steroids and their use as 5 alpha-reductase inhibitors The present invention relates to 4-amino-Ɗ4,6 -steroids which are useful as inhibitors of 5-reductase. The compounds are prepared by the reaction of an appropriate 4,5-epoxy steroid with sodium azide in an inert solvent in the presence ... | 07/14/1992 |
| 5120840 | 4-amino-4-ene-steroids and their use as 5-reductase inhibitors The present invention relates to 4-amino-Ɗ4 -steroids which are useful as inhibitors of 5-reductase. The compounds are prepared by the reaction of an appropriate 4-azido steroid with triphenylphosphine in an aqueous inert solvent with h... | 06/09/1992 |
| 5093502 | 14,17-dihydroxy-17ଲ-substituted steroids A process for the preparation of novel 14, 17-dihydroxy-17ଲ-substituted steroids by reacting 14-hydroxy-17-oxo-steroids with metal organic compounds and the use of the said novel steroids in the production of 14, 17&... | 03/03/1992 |
| 5087700 | Method of producing primary amines in high yields A novel process for producing hindered and unhindered primary amines represented by the formula RNH2 and R*NH2 in high yields from novel intermediates RBMe2 or R*BMe2 wherein R is an organo group, R* is a chiral... | 02/11/1992 |
| 5043332 | Novel 11ଲ-substituted -19-nor-steriods Novel 19-nor-steroids of the formula ##STR1## wherein R1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R2 is a hydro... | 08/27/1991 |
| 5034548 | Steroid derivatives useful as hypocholesterolemics Lanosterols substituted in the 14 and/or 15 position(s) which are active in inhibiting lanosta-8,24-dien-3ଲ-ol 14-methyl-demethylase activity, suppressing 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGR) activity, decreasing cholesterol... | 07/23/1991 |
| 4988684 | Novel 4-alkylthio-steroids A compound of the formula ##STR1## wherein R is selected from the group consisting of alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, R1 is alkyl of 1 to 6 carbon atoms unsubstituted or substituted with at leas... | 01/29/1991 |
| 4954446 | Aromatic steroid 5--reductase inhibitors Invented are substituted acrylate analogues of steroidal synthetic compounds, pharmaceutial compositions containing the compounds, and methods of using these compounds to inhibit steroid 5--reductase including using these compounds to reduce prosta... | 09/04/1990 |
| 4937237 | Phosphinic acid substituted aromatic steroids as inhibitors of steroid 5-60 -reductase Invented are phosphinic acid substituted analogues of steroidal synthetic compounds, pharamaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5--reductase, including using these compounds to r... | 06/26/1990 |
| 4920114 | 19-fluoro- or cyano-21-hydroxyprogesterone derivatives useful as 19-hydroxylase inhibitors 19-Fluoro- and cyano- substituted 21-hydroxyprogesterone derivatives and related compounds which are active as 19-hydroxylase inhibitors and useful as antihypertensive agents are described herein. The compounds are prepared using appropriate synthetic pat... | 04/24/1990 |
