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7507725 |
Compounds with sulphonamide group and pharmaceutical compositions containing these compounds
The invention relates to compounds which, acting as a prodrug and/or support, enable an active agent to be taken up by the erythrocytes and/or an active agent to bind to the erythrocytes. The...
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7495115 |
Steroid conjugates, preparation thereof and the use thereof
Conjugates comprising one or more steroids conjugated with one or more mammalian proteins are disclosed. The conjugates are useful for diagnosis or treatment of solid cancer and haematological...
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7435757 |
2-substituted D-homo-estra-1,3,5(10)-trienes as inhibitors of 17β-hydroxy steroid dehydrogenase type 1
The invention relates to new 2-substituted D-homo-estra-1,3,5(10)-trienes of general formula I
in which
R 2 means a C 1 -C 8 -alkyl group, a C 1 -C 8 -alkyloxy group or a halogen atom,...
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7378404 |
8β-hydrocarbyl-substituted estratrienes for use as selective estrogens
This invention describes the new 8β-substituted estratrienes of general formula I in which R 2 , R 3 , R 6 , R 6′ , R 7 , R 7′ , R 9 , R 11 , R 11′ , R 12 , R 14 , R 15 , R 15′ , R 16 , R...
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7371741 |
Estradiol derivatives and pharmaceutical compositions using same
Compositions and methods for treating mammalian disease characterized by undesirable angiogenesis by administering compounds of the general formula:
wherein the variables are defined in the...
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RE39592 |
Extended release growth promoting two component composition
An extended release composition comprising a first composition comprising growth promoters and a second composition comprising growth promoters and a biodegradable polymer is described. A method of...
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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...
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6958327 |
18 Norsteroids as selectively active estrogens
The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R 1 , R 2 , R 3 , R 6 , R 7 , R 8 , R 9 , R 11 , R 11′ , R 14 , R 15 , R 15′ , R 16 , R 17 and R...
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6831073 |
Hormonal composition consisting of an oestrogen compound and of a progestational compound
A method of treating estrogenic deficiencies in women while further avoiding the appearance of osteoporosis, withdrawal bleeding and cardiovascular diseases in post-menopausal women without any...
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6767903 |
New7α, 17α-bis-alkylated testosterone derivatives and their use in long-term therapy of androgen-dependent diseases
The invention relates to new 7α, 17α, 17β-substituted testosterone derivatives of general formula (I) and their use as pure antiandrogens for the long-term therapy of androgen-dependent...
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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...
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6670348 |
Methods and compositions for destruction of selected proteins
Compounds having an ansamycin anitibiotic, or other moiety which binds to hsp90, coupled to a targeting moiety which binds specifically to a protein, receptor or marker can provide effective...
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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 wherein the substituents are defined as in the specification which are intermediates for the production of vinyl compounds...
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6579995 |
Process for phosphorylation and compounds produced by this process
The present invention is directed to improved processes for phosphorylation and compounds produced by the improved processes. The improved process for phosphorylating complex alcohols comprises the...
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6544971 |
Method of increasing alertness by administration of a vomeropherin, and vomeropherin-emitting alarm devices
A method of increasing alertness in an individual by administering an effective amount of an alertness-increasing vomeropherin to the individual; and an alarm device that, when activated, emits an...
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6476012 |
Estradiol-16α-carboxylic acid esters as locally active estrogens
The present invention relates to analogs of estradiol, which, in their most preferred embodiment, act as locally active estrogens without significant systemic action. A series of 16α-carboxylic...
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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...
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6417365 |
Method for recovering medicaments from preparations, and from the precursors or wastes thereof
In a process for recovering medicinal substances or active substances from preparations, their initial products or waste, a flat-shaped starting material in the form of a film with adhesive and an...
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6333317 |
Regulation of amyloid precursor protein (APP) expression by administration of an estrogenic compound
It has been discovered that lipophilic hormones that interact with cytosolic or nuclear receptors regulate APP expression and synthesis, through modification of APP mRNA stability and/or regulation...
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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...
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6201141 |
Determination of steroids by competitive immunoassay
A method and kit for measurement of a steroid by means of a competitive immunoassay, preferably a competitive enzyme immunoassay. The method and kit involve the use of a steroid analogue conjugated...
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6169082 |
Salts of 8,9-dehydroestrone sulfate ester
This invention presents alkali metal salts of 8,9-dehydroestrone, salts of its sulfate ester, and stable compositions thereof, as well as processes for their production and use in estrogen...
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5998639 |
Sulfatation of estrogen mixtures
The invention relates to a method for the preparation of a mixture of sulfated estrogens containing delta(8,9)-dehydro estrone [delta(8,9)DHE] or derivatives thereof.
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5994568 |
Estrenes for inducing hypothalamic effects
The invention relates to estrene steroids, which bind to neuroepithelial receptors. The steroid is preferably administered in the form of a pharmaceutical composition containing one or more...
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5986115 |
7α-(ξ-aminoalkyl)-estratrienes, process for their production, pharmaceutical preparations which contain these 7α-(ξ-aminoalkyl)-estratrienes as well as their use for the production of pharmaceutical agents
This invention describes new, substituted 7α-(ξ-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their...
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5977096 |
Steroids with radical-attracting aromatic substituents, process for the production thereof and pharmaceutical compounds containing the said substances
Novel substituted steroid compounds are disclosed which are more effective than known radical-trapping agents in methods of prophylaxis and therapy of radical-mediated cell damage and of treatment...
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5928666 |
Crystalline form of estradiol and pharmaceutical formulations comprising same
The present invention is directed to a stable crystalline form of estradiol suitable for incorporation into pharmaceutical formulations. The invention further provides methods of preparing said...
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5798348 |
Fatty-acid monoesters of estrogens for the treatment of obesity and/or overweight
The pharmaceutical and/or cosmetic compositions for treatment of obesity and/or overweight contain an effective amount of a fatty-acid monoester of an estrogen and a fatty acid wherein the estrogen...
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5739363 |
Isomerisation of equilin
The invention relates to a method of isomerisation of equilin or a derivative thereof to delta(8,9)-dehydro estrone delta(8,9)DHE!, characterized in that equilin or a derivative thereof is treated...
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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...
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5597701 |
Process for determining androstenone contents in adipose tissues
A process and appropriate device are disclosed for determining the androstenone content of adipose tissues in clearly shorter times. The disclosed process has the following steps: (a) liquefying an...
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5552395 |
Δ9(11)-dehydro-8-isoestrone used to treat alzheimer's disease
This invention relates to treating Alzheimer's disease with 8α-3-hydroxyestra-1,3,5(10),9(11)tetraen-17-one (Δ9(11)-dehydro-8-isoestrone) (VI), ##STR1## or a pharmaceutically acceptable salt...
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5514673 |
Pharmaceutical composition containing lipophilic drugs
A pharmaceutical composition having a form suitable for transmucosal administration containing progesterone and/or 17-β-estradiol as an active ingredient.
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5510342 |
Method of lowering cholesterol
This invention provides a method of lowering cholesterol and blood lipid levels, preventing hypercholesterolemia, hyperlipidemia, cardiovascular disease, atherosclerosis, and peripheral vascular...
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5496814 |
Method of modifying bone resorption with Δ9(11)-dehydro-8-isoestrone
This invention relates to 8α-3-hydroxyestra-1,3,5(10),9(11)tetraen-17-one (Δ9(11)-dehydro-8-isoestrone) (VI), ##STR1## to the process for its preparation, to pharmaceutical compositions...
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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,...
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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...
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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 R 1 is C 1 -4 alkyl or C 1 -4 alkoxy; R 2 is...
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5395831 |
Treating cardiac disorders with Δ9(11)-dehydro-8-isoestrone
This invention relates to 8α-3-hydroxyestra- 1,3,5( 10),9( 11 )tetraen-17-one (Δ9( 11 )-dehydro-8-isoestrone) (VI), ##STR1## to the process for its preparation, to pharmaceutical compositions...
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5391778 |
2-iodo-3-keto-Δ.sup.4 steroids, process for their production, as well as their further processing
The new intermediate products of general formula I ##STR1## in which R 1 stands for a hydrogen atom or a straight-chain or branched alkyl group with 1 to 4 carbon atoms, R 2 stands for a...
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5288717 |
Alkali metal 8,9-dehydroestrone sulfate esters
This invention presents alkali metal salts of 8,9-dehydroestrone, its sulfate ester, and stable compositions thereof, as well as processes for their production. The sulfate ester salts are useful...
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5266712 |
Process for crystallizing the organic substances from steroidal origin and the thus obtained compounds
A process for crystallizing a pharmaceutically active steroidal product, without mechanical procedure, to obtain a homogeneous granulometric class which may be prepared beforehand, wherein the...
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5182381 |
Intermediates for 3-keto-19-nor-Δ.sup.4,9 -steroids
Novel 3-keto-19-nor-Δ 4 ,9 -steroids of the formula ##STR1## and their non-toxic, pharmaceutically acceptable acid addition salts possessing a remarkable antiglucocorticoidal activity.
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5151533 |
Process for the production of 3-hydroxy-1,3,5(10)-estratrien-17-one
A process for the production of 3-hydroxy-1,3,5(10)-estratrien-17-one by pyrolysis of 1,4-androstadiene-3,17-dione in the presence of 1,2,3,4-tetrahydronaphthalene as hydrogen donor is described,...
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5116994 |
Deacylating agent and deacylating method
Deacylating agent represented by the formula (I): ##STR1## wherein R represents an insoluble polymer substituent, and R' and R" each represents an alkyl group, and a deacylation method using the...
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5093490 |
Process for optical resolution of bicyclo[3.3.0]octane-3,7-dione-2 carboxylic acid esters and their 7-monoketals
The invention relates to a process for the production of (+)-bicyclo[3.3.0]octan-3-one-2 carboxylic acid steroid esters of formula I ##STR1## in which X means oxygen or the radicals --O--(CH 2 ) n ...
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4983646 |
Organometallic complexes of estrogens and their application to the determination of hormone receptors
The present invention relates to an estrogen complex which consists of an estrogen or an estrogen derivative complexed with an organometallic compound containing at least one free carbonyl ligand,...
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4938897 |
Chlorambucil derivatives and cell-discriminating agent containing the same
Disclosed herein are (1) a fluorescent substance represented by the formula (I), (2) a process for producing the fluorescent substance, and (3) a cell-discriminating agent containing the...
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4923640 |
Process for the production of 17α-ethinyl-17β-hydroxy-18-methyl-4,15-estradien-3-one and new intermediate products for this process
A process for the production of 17α-ethinyl-17β-hydroxy-18-methyl-4,15-estradien-3-one is described comprising reacting a 17-enolester of formula II ##STR1## wherein R 1 represents an alkyl...
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4855125 |
Iodinated estradiols, intermediate products and methods of production
A method of preparation of estradiol derivatives labeled by iodine, especially 123 I, substitution at C-16 are synthesized according to the present invention. A triflate intermediate is prepared...
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