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| Number | Title | Issue Date |
| 7135581 | Antiangiogenic agents 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 th... | 11/14/2006 |
| 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 |
| 7041839 | Steroidal antiestrogens and antiandrogens and uses thereof The present invention comprises the design, synthesis and development of a new class of chemotherapeutic agents for prophylactic and therapeutic treatments in a mammal, particularly a human, believed to be at risk of suffering from a hormone-responsive disorde. In a... | 05/09/2006 |
| 6992075 | C(14) estrogenic compounds The present invention relates to novel estrogenic compounds. The present invention also relates to methods of treating estrogen deprivation in a subject comprising administering novel estrogenic compounds. Additionally, the present invention relates to methods of sy... | 01/31/2006 |
| 6566542 | 17-Halogenated 19-nor steroids, preparation process and intermediates, use as medicaments and the pharmaceutical compositions containing them A process for the preparation of a compound of the formula ##STR1## wherein the substituents are defined as in the specification.... | 05/20/2003 |
| 6423700 | 17-halogenated 19-nor steroids, method and intermediates for preparing same, use as medicines and pharmaceutical compositions containing same A compound of the formula ##STR1## wherein the substituents are as defined in the application and its non-toxic, pharmaceutically acceptable acid and base salts useful for hormone replacement for treating menopause or perimenopause without activity a... | 07/23/2002 |
| 6080735 | Estra-1,3,5(10)-trien derivatives, processes for their preparation and pharmaceutical compositions containing these compounds This invention is relating to new estra-1,3,5(10)-trien-sulfamates carrying at the 3-position an R--SO2 --O--group, with R being an R1 R2 N--group in which R1 and R2, independently of each other, repr... | 06/27/2000 |
| 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 |
| 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 |
| 5866560 | 7-(.xi.-aminoalkyl)-estratrienes, process for their production, pharmaceutical preparations which contain these 7-(.xi.-aminoalkyl)-estratrienes as well as their use for the production of pharmaceutical agents This invention describes new, substituted 7-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organ... | 02/02/1999 |
| 5705495 | Sulfamate derivatives of 1,3,5(10)-estratriene derivatives, methods for their production and pharmaceuticals containing these compounds The invention relates to new sulfamate derivatives of 1,3,5(10)-estratriene derivatives of the general formula I ##STR1## wherein the 3-sulfamate moiety is acylated, sulfonated or amidosulfonated. Furthermore, methods for the production of the compou... | 01/06/1998 |
| 5633393 | Estradiol derivative-alkylating agent conjugate with reduced hormonal activity, process for preparing the same, compounds useful for the preparation thereof, and growth inhibiting compositon containing the conjugate or estradiol derivative. Conjugates of the formula ##STR1## are prepared by reacting an estradiol derivative with a compound of the formula: ##STR2## in the presence of thionyl chloride or a metal hydride at -30° to 150° C. for 3 minutes to 48 hours and then reco... | 05/27/1997 |
| 5621124 | Process for the alkylation of estrone derivatives The invention relates to a process for the alkylation of estrone derivatives, which is characterized in that a suspension of the estrone derivatives in dimethylformamide is produced and carbonic acid diester and guanidine and/or alkyl guanidines are disso... | 04/15/1997 |
| 5565588 | 9-alpha-hydroxy steroids, process for their preparation, process for the preparation of the corresponding 9(11)-dehydro derivatives and pharmaceutical preparations containing said steroids New 9-alpha-hydroxy steroids are prepared by the introduction of substituents on the D-ring of 9-alpha-hydroxy-androst-4-ene-3,17-dione. The resulting compounds are useful intermediates in the synthesis of corticosteroids.... | 10/15/1996 |
| 5561125 | Estradiol derivative and growth inhibiting composition thereof Estradiol derivatives of the formula: ##STR1## wherein R1 is C1-4 alky or C1-4 alkoxy; R2 is acyl or benzyl; m is an integer of 1 to 3; n is an integer of 1 to 3; and X is hydroxy or halogen are useful as t... | 10/01/1996 |
| 5554602 | Labelling of hormones with rhenium and tecnetium The disclosed invention is drawn to the organometallic oestrogen complex of formula (I): ##STR1## in which A is a C1-7 alkylene radical or C2-7 alkenylene or alkynylene radical; Mx is one or more identical or differen... | 09/10/1996 |
| 5554603 | Orally active derivatives of 1,3,5(10)-estratriene The invention presents 17ଲ-nitro and 11ଲ, 17ଲ-dinitro esters of estradiol which are made from 3-acyloxy-17-keto- or 3,17-dihydroxy-1,3,5-estratrienes by processes known in the art. The compounds exhibit estrogenic activity.... | 09/10/1996 |
| 5491138 | Estradiol derivative alkylating agent conjugate with reduced hormonal activity, process for preparing the same, compounds useful for the preparation thereof, and growth inhibiting composition containing the conjugate or estradiol derivative Disclosed is a method of inhibiting the growth of tumors by administering an estradiol derivative-alkylating agent conjugate of the formula (I'): ##STR1## wherein R1 is C1-4 alkyl or C1-4 alkoxy; R2 is acyl or ... | 02/13/1996 |
| 5478818 | Estradiol derivative-alkylating agent conjugate with reduced hormonal activity, process for preparing the same, compounds useful for the preparation thereof, and growth inhibiting composition containing the conjugate or estradiol derivative Disclosed is an estradiol derivative-alkylating agent conjugate of the formula (I'): ##STR1## wherein R1 is C1-4 alkyl or C1-4 alkoxy; R2 is acyl or benzyl; m is an integer of 1 to 3; and n is an integer of... | 12/26/1995 |
| 5438134 | Process for the production of unsaturated 17 -cyanomethyl-17 ଲ- h The unsaturated 17-cyanomethyl-17ଲ-hydroxy steroids of the formula I, ##STR1## in which R1 =Me, Eth; R2 =H, Me; R3 =H, OH, an acetoxy or alkoxy group; R4 =H, R5 =OH, an acetoxy, alko... | 08/01/1995 |
| 5354745 | Estradiol derivative-chlorambucil conjugate process for preparing the same, and pharmaceutical composition An estradiol derivative-chlorambucil conjugate of the formula (I): ##STR1## wherein R1 is alkyl or alkoxyl of 1 to 4 carbon atoms; R2 is acyl, dansyl, or alkyl; R3, R4, and R5 independently are H, ... | 10/11/1994 |
| 5252729 | Extraction of compounds from plant materials using supercritical fluids The present invention is directed toward a process for extracting compounds from plant material, comprising a) contacting hydrolyzed plant material with a supercritical fluid and optionally with a co-solvent and p1 b) recovering the compound from the supe... | 10/12/1993 |
| 4885117 | Process for the preparation of (Z)-17-halovinyl steroids (Z)-17-halovinyl steroids of general Formula I ##STR1## wherein . . . . is a single bond or a double bond, V is a carbon-to-carbon bond or a methylene group, R1 is a hydrogen atom or a methyl group, X is a chlorine atom, a bromine atom or an ... | 12/05/1989 |
| 4859370 | 9 alpha, 11 beta-substituted and 11 beta-substituted estranes 9 alpha, 11 beta and 11 beta-substituted estranes are disclosed which exhibit elevated estrogenic and postcoital contraceptive activities. A process for their manufacture and their use in pharmaceuticals is also disclosed.... | 08/22/1989 |
| 4725426 | Estrogenic 17-halogen-vinylestranes 17-bromo- and 17-iodo-vinyl-estrane derivatives of general formula I ##STR1## wherein X is a bromine or iodine atom in Z or E position, R1 is hydrogen, hydroxy or acyloxy with up to 3 C atoms, R2 is hydrogen, alk... | 02/16/1988 |
| 4705783 | 9, 11ଲ-substituted and 11ଲ-substituted estranes 9 alpha, 11 beta and 11 beta-substituted estranes are disclosed which exhibit elevated estrogenic and postcoital contraceptive activities. A process for their manufacture and their use in pharmaceuticals is also disclosed.... | 11/10/1987 |
| 4622181 | Process for producing an estrone acetal A process of preparing radical anions which comprises reacting sodium and a polycyclic aromatic compound in a reaction solvent to prepare radical anions and supplying androstane-1,4-diene-3,17-dione-17-acetal into the obtained reaction mixture to reduce t... | 11/11/1986 |
| 4416821 | Process for preparing 16-methylene steroids A process is disclosed for the production of 17-keto-16-methylene steroids (III) from the corresponding readily available 17-keto steroid (I) via a novel intermediate (II).... | 11/22/1983 |
| 4357278 | Process for synthesizing estrone or estrone derivatives What are disclosed are a multi-step synthesis for the preparation of 9(11)-dehydroestrone 3-methyl ether from 2-methyl,4-methoxy benzaldehyde; 1-(4-methoxy-2-methyl-(phenyl)-3-(1-methyl-2-oxo-5-t-vinyl-cyclopent-r-yl) -propane-1-one, an intermediate in sai... | 11/02/1982 |
| 4307086 | Branched chain and cycloaliphatic esters of the androstane and destrane series and pharmaceutical compositions containing same There are disclosed branched chain and cycloaliphatic esters of steroids having the formula: ##STR1## where R is H or CH3 ; R1 is H or CH3 ; R2 is H or CH3 ; R3 is H, OH, CH3 or ... | 12/22/1981 |
| 4272530 | Ɗ1,3,5(10) -Estratrienes Novel 11ଲ -substituted-Ɗ 1,3,5(10) -estratrienes of the formula ##STR1## wherein R1 is selected from the group consisting of optionally substituted unsaturated alkyl of 2 to 8 carbon atoms, optionally substituted ary... | 06/09/1981 |
| 4259325 | 1,3-Dibenzoic acid esters of 17-ethynyl-7-methyl-1,3,5(10)-estratriene-1,3,17ଲ-tri ol 1,3-Dibenzoic acid esters of 17-ethynyl-7-methyl-1,3,5(10)-estratriene-1,3,17ଲ-triol possess strong estrogenic and ovulation-inhibiting activities. As compared to the corresponding diacetic acid ester, these dibenzoic acid esters ... | 03/31/1981 |
| 4222940 | Cyclization substrates, cyclization process and related 11ଲ-axially-substituted steroids There are disclosed substrates of the formula: ##STR1## wherein: (a) R1 is H or C1 -C4 alkyl; (b) R2 is H or C1 -C4 alkyl with the proviso that R1 is H when R2 is alky... | 09/16/1980 |
| 4212864 | Branched chain and cycloaliphatic esters of the androstane and oestrane series and pharmaceutical compositions containing same There are disclosed branched chain and cycloaliphatic esters of steroids having the formula: ##STR1## or the 5H analog thereof, where R is H or CH3 ; R1 is H or CH3 ; R2 is H or CH3 ; R3 | 07/15/1980 |
| 4191697 | Novel steroids Novel Ɗ1,3,5(10),6 -estratetraenes of the formula ##STR1## R is selected from the group consisting of hydrogen, acyl of an alkanoic acid of 1 to 5 carbon atoms, optionally substituted benzoyl, tetrahydropyranyl, trityl and trimethylsilyl ... | 03/04/1980 |
| 4064173 | 9,10-Seco-steroids A process for the preparation of 9,10-seco-steroids of the formula ##STR1## WHEREIN R1 and R2 independently are hydrogen, amino, OR5, OCOR6 or NHCOR5 wherein R5 is hydrogen or lower alkyl a... | 12/20/1977 |
| 4052421 | 13-Ethinyl-steroids and processes for their manufacture A new class of 13-ethinyl-steroids is prepared by a novel process comprising Wittig reaction of a 13-formyl steroid with a chloro- or bromomethylenephosphorane and dehydrohalogenation of the intermediate 13-(2-halogenovinyl)steroid with an extremely stron... | 10/04/1977 |
| 4029648 | Process of making gona-1,3,5(10),9(11)-tetraenes Gona-1,3,5(10),9(11)-tetraenes having the formula ##STR1## IN WHICH FORMULA N IS 1 OR 2, R1 is a hydrogen, hydroxy, alkoxy, or alkanoyl substituent, R2 is a hydrogen, alkoxy, acetoxy, alkyl, akenyl, or alkynyl substituent, or a subst... | 06/14/1977 |
| 4013688 | Radioimmunoassay agents Novel steroid derivatives containing a tyrosine ester amide group linked to an 11-hydroxysteroid alkylene dicarboxylic hemi-ester are described, suitable for iodination with radioactive iodine, useful in radioimmunoassay.... | 03/22/1977 |
| 3980681 | Process for the preparation of 11-ଲ-nitro-oxysteroids Process for preparing 9 -hydroxy-11 ଲ-nitro-oxysteroids having a aromatic ring A wherein an aromatic A-ring-containing 9, 11-unsubstituted steroid or corresponding 9,11-dehydrosteroid is oxidized with ceric ions in the presence of nitrate ion... | 09/14/1976 |
