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7605152 |
17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators
Compounds of structural formula I as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as...
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7576055 |
Artificial low-density lipoprotein carriers for transport of substances across the blood-brain barrier
This invention relates to a highly efficient artificial low-density lipoprotein (LDL) carrier system for the targeted delivery therapeutic agents across the blood-brain barrier (BBB). In...
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7557097 |
Structural, behavioral characterization, and synthesis of attractants for migratory lamprey
Compounds that function as lamprey attractants and methods.
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7547687 |
Therapeutic treatment methods
The invention relates to the use of compounds to ameliorate or treat a condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include...
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7517870 |
Use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/or reversing ocular diseases related with ocular neovascularization
The present invention concerns the use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/or reversing ocular...
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7407947 |
Amphoteric sterols and the use thereof
An amphoteric compound based on a sterol skeleton, the 3-position of the sterol ring system being substituted by one or more amphoteric groups having an isoelectric point of between about 4 and 9,...
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7396827 |
Pharmaceutical compositions and treatment methods
The invention provides compositions comprising formula 1 steroids, e.g., 16α-bromo-3β-hydroxy-5α-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition...
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7381718 |
Method for preparing oestrogen derivatives
A process for the preparation of compounds of formula (I)
in which R 1 , R 2 , R 3 and n are defined as indicated in the description, use of said compounds as intermediates for the...
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7375098 |
8β-vinyl-11β-(ω-substituted)alkyl-estra-1,3,5(10)-trienes
This invention relates to 8β-vinyl-11β-(ω-substituted)alkyl-estra-1,3,5(10)-trienes
of general formula I
with ERβ-antagonistic activity, process for their production, their intermediate...
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7345034 |
Azacyclosteroid histamine-3 receptor ligands
Azacyclosteroid histamine-3 receptor ligands, pharmaceutical compositions comprising such compounds, and methods for using such compounds and compositions are described herein.
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7312206 |
Sterol derivatives, liposomes comprising sterol derivatives and method for loading liposomes with active substances
Disclosed is a sterol derivative having a pKa value of 3.5-8 according to the general formula cation-spacer 2-Y-spacer 1-X-sterol, wherein Y and X represent bonding groups. The invention also...
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7265099 |
Use of chemical chelators as reversal agents for drug-induced neuromuscular block
The invention relates to the use of chemical chelators for the preparation of a medicament for the reversal of drug-induced neuromuscular block, to a kit for providing neuromuscular block and its...
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7182942 |
Vaccine immunotherapy for immune suppressed patients
A method of immunotherapy to treat cancer or a synergistic anti-cancer treatment by administering an effective amount of a natural cytokine mixture (NCM), an effective amount of cyclophosphamide...
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7153844 |
Estrogen-linked platinum (II) complexes as anticancer agents
wherein X may be —CH 2 —O—CH 2 — or —CH 2 —, wherein n may be 1, 2, 3, 4 or 5 when X is —CH 2 —O—CH 2 —, wherein n may be 2, 3, 4, 5, 6, 7, 8, 9 or 10 when X is —CH 2 —,...
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7074779 |
Estrieno[3,2-b]/[3,4-c]pyrrole derivatives useful as modulators of the estrogen receptors
The present invention is directed to novel estrieno[3,2-b]/[3,4-c]pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and diseases mediated...
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7074778 |
Asthma associated factors as targets for treating atopic allergies including asthma and related disorders
This invention relates to methods for treating asthma or allergy in a mammal by administering a 3-aminosteroid compound to a mammal in need thereof. The 3-aminosteroid compound being capable of...
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7067503 |
17-aryl linker derivatised estrogen 3-sulphamates as inhibitors of steroid sulphatase
There is provided a compound comprising a steroidal ring system and a group R 1 selected from any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a...
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7053076 |
Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs
Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across...
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7049305 |
Bile-acid conjugates providing for sustained systemic concentration of drugs
This invention is directed to compounds that provide for sustained systemic concentrations of therapeutic or prophylactic agents following administration to animals. This invention is also directed...
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7018991 |
17β-amino and hydroxylamino-11 β-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.
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6956030 |
Use of mometasone furoate for treating upper airway diseases
The administration of aerosolize particles of mometasone furoate in the form of dry powders, solutions, or aqueous suspension for treating corticosteroid-responsive diseases of the surfaces of...
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6953785 |
Estra-1,3,5(10)-triene derivatives
Provided is steroid sulfatase inhibitors comprising, as the active ingredient, an estra-1,3,5(10)-triene derivative which is represented by formula (I):
{wherein R 1 and R 2 are the same or...
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6949532 |
Use of mometasone furoate for treating airway passage and lung diseases
The administration of aerosolize particles of mometasone furoate in the form of dry powders, solutions, or aqueous suspension for treating corticosteroid-responsive diseases of the surfaces of...
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6921757 |
Organic compounds
Compounds of formula (I), where R is a monovalent cyclic organic group having from 3 to 15 atoms in the ring system, useful as pharmaceuticals
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6900193 |
Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
The present invention relates, inter alia, to compounds having the general formula:
in which: R 1 is a member selected from the group consisting of —OCH 3 , —SCH 3 , —N(CH 3 ) 2 ,...
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6790842 |
11β LONG-CHAIN SUBSTITUTED ESTRATRIENES, METHOD FOR THEIR PRODUCTION, PHARMACEUTICAL PREPARATIONS CONTAINING SAID 11β LONG-CHAIN SUBSTITUTED ESTATRIENES, AND THEIR USE FOR PRODUCING MEDICAMENTS
This invention describes a 11β-long-chain-substituted estratriene of general formula (I), in which R 11 is a long-chain radical that has a nitrogen atom and optionally a sulfur atom, which in...
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6784170 |
Synthesis of anti-estrogenic and other therapeutic steroids from 21-hydroxy-19-norpregna-4-en-3-one
Syntheses of steroids such as 3-hydroxy-7α-methyl-21-[2′-methoxy-4′-(diethylaminometh
yl)-phenoxy]-19-norpregna-1,3,5(10)triene citrate (“SR 16234”) and analogs thereof are provided,...
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6780855 |
11β-HALOGEN-7α-SUBSTITUTED ESTRATRIENES, PROCESS FOR THE PRODUCTION OF PHARMACEUTICAL PREPARATIONS THAT CONTAIN THESE 11β-HALOGEN-7α-SUBSTITUTED ESTRATRIENES AS WELL AS THEIR USE FOR THE PRODUCTION OF PHARMACEUTICAL AGENTS
This invention describes the new 11β-halogen-7α-substituted estratrienes of general formula I in which R 11 is a fluorine or chlorine atom, and the other substituents have the meanings that...
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6780853 |
Neuroactive steroids of the androstane and pregnane series
The invention relates to 3α-hydroxy, 17-(un)substituted derivatives of the androstane series and 3α-hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of...
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6759399 |
Use of antimineralocorticoid compounds against narcotic withdrawal syndrome
The method of treating narcotic withdrawal symptoms in warm-blooded animals comprising administering to warm-blooded animals in need thereof an amount of a compound having anti-mineralocorticoid...
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6740645 |
17β-acyl-17α-propynyl-11β-(cyclic amino) aryl steroids and their derivatives having antagonist hormonal properties
The invention is directed to a novel class of 17β-acyl-17α-propynyl steroids which exhibit potent antiprogestational activity.
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6693090 |
19-norsteroids substituted in position 11β, preparation process and intermediates, application as medicines and pharmaceutical compositions containing them
A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as set forth in the specification which compounds are useful for the treatment of...
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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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6624156 |
Methods of making and method of using hybrid cholinergic agents and compositions
The present invention provides hybrid molecules and methods of synthesizing such hybrid molecules from a cholinergic agent and a bile acid. The hybrid molecules function as cholinergic agents and...
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6624155 |
Hybrid cholinergic agents and compositions
The present invention provides hybrid molecules and methods of synthesizing such hybrid molecules from a cholinergic agent and a bile acid. The hybrid molecules function as cholinergic agents and...
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6613757 |
COMBINATION OF PROSTACYCLIN WITH AN ESTROGEN OR PROGESTIN FOR THE PREVENTION AND TREATMENT OF ATHEROSCLEROTIC VASCULAR DISEASE INCLUDING PREECLAMPSIA AND FOR THE TREATMENT OF HYPERTENSION, AND FOR HORMONE REPLACEMENT THERAPY
Cardiovascular disease, including preeclampsia in pregnant women and hypertension in both women and men, are prevented or treated by administering thereto prostacyclin or a prostacyclin analog in...
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6596713 |
Steroid esters and amides, process for their production and their pharmaceutical use
New steroids and amides of formula I are described, in which the variables are defined by the description. Relative to the basic hydroxy compounds (“initial compounds”), the new compounds...
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6583130 |
C13-substituted estra-1,3,5,(10)-trien-3-yl sulfamates, methods of preparing same, and pharmaceutical compositions containing these compounds
The invention relates to new C 13 -substituted estra-1,3,5(10)-trien-3-yl sulfamates of general formula I, wherein R 1 represents an acyl residue, oxycarbonyl residue, aminocarbonyl residue,...
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6541464 |
Steroids substituted at the 11-position, process for their preparation, their use as medicament and the pharmaceutical compositions containing them
Compounds of the formula Where the substituents are defined in the application.
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6500815 |
Substituted 11.beta steroid derivatives, method for preparing same and intermediates of said method, use as medicine and compositions containing them
The invention concerns compounds of formula (I) wherein: X, Y, R 1 , R 2 , Z, G are as defined in the description, the methods for preparing them and the intermediates in said method, their use as...
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6482813 |
Steroids substituted at the 11-position, process for their preparation, their use as medicament and the pharmaceutical compositions containing them
Compounds of formula for treating osteoporosis with minimal estrogenic activity are disclosed.
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6479476 |
19-nor steroids substituted in position 11β, preparation method and intermediates, application as medicines and pharmaceutical compositions containing them
A compound selected from the group consisting of the compounds of the formula wherein the substituents are defined as in the specification and their addition salts with non-toxic,...
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6472382 |
4-halogenated steroids, their preparation process and intermediates, their use as medicaments and the pharmaceutical compositions containing them
A subject of the invention is the compounds of formula (I): in which X is a halogen atom, D represents the remainder of an optionally substituted pentagonal or hexagonal ring and optionally...
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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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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 wherein the substituents are as defined in the application and its non-toxic, pharmaceutically acceptable acid and base salts useful for hormone replacement for...
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6407083 |
Uses of novel organoselenium compounds with pro-oxidant activity
Compounds represented by the following formula I: in which: R 1 to R 5 can have various meanings of which alkyl, substituted or non-substituted aryl, and m is equal to 0 or 1, X is selected...
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6380179 |
Method for treatment of alopecia
A method of using a specified active ingredient for treating alopecia, female hirsutism and seborrhea and for preventing bone metastasis caused by prostatic cancer. The specified active ingredient...
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6355630 |
Estra-1,3,5(10)-triene-7α-thioethers
This invention provides estrogens and antiestrogens of formula I having the structure wherein X, Y, Z, and R are as defined hereinbefore in the specification, or a pharmaceutically acceptable...
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6339077 |
Substituted 4-benzylaminoquinolines and their hetero analogs, process for their preparation, pharmaceuticals containing these compounds and use thereof
The invention relates to substituted 4-benzylaminoquinolines and their hetero analogs, and to the pharmaceutically acceptable salts and physiologically functional derivatives thereof. Compounds of...
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