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| Number | Title | Issue Date |
| 7037907 | Estradiol conjugates and uses thereof A conjugated prodrug of an estradiol compound conjugated to a biological activity modifying agent. ... | 05/02/2006 |
| 6995278 | 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 the spec... | 02/07/2006 |
| 6930128 | 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 below in a dosa... | 08/16/2005 |
| 6689768 | Pharmaceutical preparations for treating side effects during and/or after GnRHa therapy The pharmaceutical preparations for treating side effects, such as hot flashes, prostate enlargement and gynecomastia, during and/or after treatment with analogs or antagonists of gonadotropin-releasing hormone (GnRHa therapy) contain an effective amount ... | 02/10/2004 |
| 6436917 | Non-estrogenic estradiol derivative compounds with anti-oxidative activity New non-estrogenic derivative compounds of estradiol, which have no estrogenic activity and comparatively high anti-oxidative activity, are disclosed. These new non-estrogenic derivative compounds are potentially useful as non-estrogenic antioxidants, esp... | 08/20/2002 |
| 6271220 | Anti-angiogenic agents The application discloses methods of treating mammalian diseases characterized by undesirable angiogenesis by administering compounds including those having the general formulae ##STR1## wherein A is a fused tropone having a general formula: ##STR2##... | 08/07/2001 |
| 6054598 | Synthesis of 2-alkoxyestradiols Disclosed is a method of preparing a compound represented by the following structural formula: ##STR1## The method comprises reacting bromine (Br2) and an aliphatic organic acid with a compound represented by the following structural formu... | 04/25/2000 |
| 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 |
| 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 |
| 5496813 | Spontaneously dispersible concentrates and aqueous microemulsions with steryl retinates having anti-tumor activity There are described spontaneously dispersible agents containing sterolester and/or sterolphosphor compounds having a pronounced antitumour activity. Novel sterolesters and sterolphosphor compounds, their use for treating tumors, and processes for their pr... | 03/05/1996 |
| 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 |
| 5480878 | Method for treating prostatic hypertrophy with estradiol derivatives Disclosed is a method for treating prostatic hypertrophy with an estradiol derivative-alkylating agent conjugate of the formula (1'): ##STR1## wherein R1 is C1-4 alkyl or C1-4 alkoxy; R2 is acyl or benzyl; ... | 01/02/1996 |
| 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 |
| 4828764 | N-Fluoro-N-Perfluoromethyl sulfonamides N-fluoro-N-perfluoromethyl sulfonamide compounds are provided as fluorinating agents for the fluorination of organic compounds by either the direct electrophilic fluorination of organic compounds or by the fluorination of organic compound carbanions.... | 05/09/1989 |
| 4676932 | Synthesis of 1-haloestradiols Estrogens characterized by an aromatic ring of the formula ##STR1## are halogenated by electrophilic substitution of a halo atom at the 1-position of the aromatic ring after protection of the sensitive 3-hydroxyl substituent and amination at the 4-po... | 06/30/1987 |
| 4584137 | Synthesis of 1-haloestradiols Estrogens characterized by an aromatic ring of the formula ##STR1## are halogenated by electrophilic substitution of a halo atom at the 1-position of the aromatic ring after protection of the sensitive 3-hydroxyl substituent and amination at the 4-po... | 04/22/1986 |
| 4577046 | Deamination of aromatic amines Deamination of aromatic primary amines by diazotization and hydrogen replacement of the diazo group is accelerated in the presence of hydrogen peroxide. Yields of at least about 85% are typical, with reaction times of usually about one hour or less.... | 03/18/1986 |
| 4522758 | Method of preparing 2-fluoro-17ଲ-estradiol 2-Fluoro-17ଲ-estradiol is synthesized by mercurating a 17ଲ-estradiol diacylate or dietherate at C-2, replacing the mercury group with fluorine and then cleaving the acyl or ether protecting groups.... | 06/11/1985 |
| 4379780 | 17 -Dihydroequilin hapten and assay method A hapten is obtained by replacing the 3-hydroxy group of 17 -dihydroequilin with HO--CO--A--O-- wherein A is an alkylene of one to six carbon atoms. The hapten is conjugated with an immunological carrier to provide an immunogen, which in turn produ... | 04/12/1983 |
| 4321208 | Preparation of directly iodinated steroid hormones and related compounds A process for the direct iodination of steroids and steroid hormones in the presence of hydrogen peroxide or chloramine-T is disclosed. The antigenicity and the specific receptor binding of directly iodinated estradiol 17-beta is identical to tritiated es... | 03/23/1982 |
| 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 |
| 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 |
| 4215044 | Synthesis of -fluorocarbonyl compounds Process for preparing an organic compound of the formula R2 R2 CFC(O)R3, which process comprises contacting and reacting in a reaction mixture which includes an inert solvent, at a temperature of -40° C. to -100° C., ROF... | 07/29/1980 |
| 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 |
| 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 |
| 3956348 | Steroid ether splitting Ethers of aromatic steroids are cleaved to regenerate the hydroxy group with aluminum hydride, dialkylaluminum hydride or trialkylaluminum.... | 05/11/1976 |
| 3939186 | Process for producing ethers of steroids A process for producing a steroid ether which comprises admixing an alkali, a reactant steroid having a hydroxyl group attached directly to an aromatic ring in the steroid nucleus, and a dialkyl sulfate in the presence of at least one hydrophilic solvent ... | 02/17/1976 |
