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7605151 |
Nitrate esters of corticoid compounds and pharmaceutical applications thereof
Compounds of the formula
and use of the compounds as medicaments.
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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...
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7157450 |
Nitrate esters of corticoid compounds and pharmaceutical applications thereof
Compounds of the formula
and use of the compounds as medicaments.
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6780854 |
Orally active androgens
Novel, orally active androgens are 7α-substituted Δ 14 -nandrolone derivatives. The compounds satisfy the general formula: wherein R 1 is O, (H,H), (H,OR), NOR, with R being hydrogen, (C 1-6...
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6713465 |
Pregnanes
This invention provides a pharmaceutically acceptable salt of 5α-pregn-16-en-3β-ol-20-one 3-sulfate ester, which is useful as a progestational agent.
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5910478 |
Peptidomimetics inhibiting the oncogenic action of p21 ras
The present invention provides peptides, cyclized peptides and peptidomimetics which inhibit the oncogenic and/or transforming activity of the p21 ras protein, pharmaceutical compositions...
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5710293 |
Method of preparation of ester derivatives of steroids
The present invention relates to a method of using a perchloric acid catalyzed reaction to make acyl derivatives of norprogesterone compounds and, in particular,...
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5567830 |
Process for synthesis of acetylenic carbinols
A method for the preparation of an acetylenic alcohol by reaction of 1,2-dibromoethylene with an alkyl, aryl an heteroaryl lithium in an inert solvent, followed by reaction with a...
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5352808 |
Process for steroid preparation
A process for the preparation of a compound of the formula ##STR1## wherein R 1 is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms optionally substituted by halogen or...
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5250711 |
Amine salts of alkane-1,n-dicarboxylic acid mono-(2-sulfato-ethyl) amides
Amine salts of alkane-1,n-dicarboxylic acid mono-(2-sulfatoethyl)amides of the Formula I HOC(O)--(CH 2 ) n --C(O)--N(R 1 )--CH 2 CH 2 SO 3 - -+ HN(R 2 ) 3 I wherein R 1...
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4948533 |
11a-hydroxy steroid diester
The present invention relates to 21-(3-carboxy-1-oxopropoxy) -17α-hydroxy-11α-(3,3-dimethyl-1-oxobutoxy)pregna-1,4-dien
e-3, 20 dione and pharmaceutically acceptable salts thereof which are...
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4933331 |
Hydrocortisone 17-oxo-21-thioesters and their uses as medicaments
3,20-dione-11β-hydroxypregn-4-ene-21-thioacetate-17-butyrat
e and 3,20-dione-11β-hydroxypregn-4-ene-21-thiopropionate-17-buty
rate, are anti-inflammatory agents.
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4913852 |
Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with pregnane derivatives
Compounds obtained from the associative synthesis of sulfur-containing or sulfur-free amino acids with derivatives of Δ-4-pregnene-3,20-dione or with derivatives of Δ-1,4-pregnadiene-3,20-dione...
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4762919 |
Anti-inflammatory carboxy pregnane derivatives
Compounds of the formula: ##STR1## wherein one X is COOR, CH 2 COOR, CH(COOR) 2 , CONHR, CH 2 CONHR, or CN remaining X's are H, F, CH 3 , OH, COOR, CH 2 COOR, CH(COOR) 2 , CONHR, CH 2 CONHR,...
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4609496 |
Steroid esters of N-(2-halogenoethyl)-N-nitroso-carbamoyl-amino acids and peptides thereof, as well as methods for preparing them
Steroid-N-(2-halogen ethyl)-N-nitroso-carbamoyl-amino acid or peptide esters of the general formula: ##STR1## where R 1 and R 2 , which may be identical or different, mean the radical of an amino...
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4602009 |
Corticoid derivatives and process for production thereof
Novel corticoid 17α-alkoxycarbonyl carboxylate derivatives are disclosed. These derivatives have strong topical anti-inflammatory activity and extremely weak systemic adverse reactions and are...
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4588718 |
Carboxy containing ester prodrugs of corticosteroids
A compound of the formula ##STR1## wherein St represents a corticosteroid moiety bonded to the carbonyl via the 21-hydroxy group of said corticosteroid; wherein Z is a bond or --O--; wherein ...
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4588530 |
Anti-inflammatory prednisolone steroids
Derivatives of prednisolone of the formula ##STR1## wherein CR 1 is CO, α-HCOH, β-HCOH, or a mixture of α-HCOH and β-HCOH CR 2 is HC(OH) OR 6 or HCO when CR 1 is CO; CR 2 is COOR...
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4537722 |
Steroid esters preparation
This invention relates to an improved steroid ester synthesis in which carbodiimides and catalytic amounts of 4-(tertiary amino)-pyridines, in combination with acid catalysts, are used as...
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4525303 |
Process for preparation of steroids
A novel process for preparing a steroid of the following formula (to be referred to as compound .circle.13 ) is provided. ##STR1## This compound is known to have marked anti-inflammatory and...
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4511511 |
Prednisolone derivatives
Novel prednisolone derivatives modified at C-17,C-20 and/or C-21 positions. Many of the compounds are anti-inflammatory agents which do not significantly suppress the pituitary-adrenal axis.
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4472392 |
Sulfonate containing ester prodrugs of corticosteroids
Novel solution stable ester prodrugs of corticosteroids of the formula ##STR1## and their salts.
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4456602 |
Amine containing ester prodrugs of corticosteroids
Novel solution stable ester prodrugs of corticosteroids of the formula ##STR1##
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4444689 |
17α-Acyloxy-5β-corticoids and 17α-acyloxy-5α-corticoids
17α-Acyloxy-5β-pregnanes (I) and 17α-acyloxy-5α-pregnanes (IV) have an excellent activity split providing high topical anti-inflammatory activity with very low systemic side effects.
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4404141 |
Δ.sup.9(11) - And Δ.sup.16 -21-chloro-20-keto steroids of the pregnane and D-homopregnane series, their preparation and use as intermediates for the synthesis of highly effective corticoids
Δ 16 - and Δ 17 -21-chloro-20-keto steroids of the formula ##STR1## wherein n is 1 or 2, C 1 C 2 and C 9 C 11 represent a CC-single or CC-double bond, R 1 is H or OH, R 2 is H...
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4381307 |
Soft tertiary amine esters of bio-affecting carboxylic acids
Novel derivatives of known bio-affecting carboxylic acids R-COOH are disclosed, said derivatives having the structural formula ##STR1## wherein Y and Y' are each H or C 1 -C 4 alkyl; n is 0 or 1;...
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4377575 |
Corticoid-17-(alkyl carbonates) and process for their manufacture
What is disclosed are steroid-21-halogeno-17-(alkyl carbonates), useful as medicaments for the treatment of inflammatory dermatoses, and a method for making them.
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4336200 |
17α-Acyloxy-5β-corticoids
17α-Acyloxy-5β-pregnanes (I) and 17α-acyloxy-5α-pregnanes (IV) have an excellent activity split providing high topical antiinflammatory activity with very low systemic side effects.
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4330541 |
Novel corticoid 17-thioacetals, their preparation and use
Novel corticoid 17-thioacetals of the formula: ##STR1## wherein X is hydrogen, fluorine or methyl, R 1 is hydrogen or C 1 -C 6 alkyl, and R 2 is hydrogen or the acyl group of a C 1 -16 -...
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4318853 |
9β,11β-Epoxy-5β-corticoids
17α-Acyloxy-5α-pregnanes (I) and 17α-acyloxy-5α-pregnanes (IV) have an excellent activity split providing high topical anti-inflammatory activity with very low systemic side effects.
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4296109 |
Corticoid 21-sulfopropionates and the salts thereof, a process for the production thereof and pharmaceutical preparations thereof
Corticoid 21-sulfopropionates of the formula ##STR1## wherein St is a steroid nucleus of a corticoid having anti-inflammatory activity, and the salts thereof with physiologically acceptable bases,...
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4264585 |
Hydrocortisone esters, pharmaceutical formulations containing these and processes for their preparation
Hydrocortisone esters of the formula ##STR1## wherein R 1 is H, formyl or acetyl and R 2 is H or CH 3 are antiphlogistically active.
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4260605 |
Novel alkylated pregnanes, processes for their preparation and pharmaceutical compositions containing same
The present invention relates to novel 21-alkylated steroids of the pregnane series having the formula: ##STR1## wherein R 1 =alkyl (1-4 C); R 2 =carboxyacyl (1-18 C); X=H, F or Cl; Y=O, H(OH),...
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4242334 |
Corticoid 17-(alkyl carbonates) and processes for their preparation
What is disclosed is corticoid 17-(alkyl carbonates) of the formula ##STR1## as defined in the specification, which compounds can be used in veterinary therapy and human therapy, in the form of...
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4216159 |
Synthesis of 16-unsaturated pregnanes from 17-keto steroids
17-Keto steroids (I) in their protected form (IIa or IIb) are reacted with a metalated olefin (VI) to give a 21-aldehyde (IV) which is readily transformed to a 16-unsaturated pregnane (V) which is...
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4207316 |
Novel 17-substituted 11 β-hydroxy steroids of the pregnane series, their manufacture, preparation and use
Corticoids of the formula ##STR1## wherein represents a single bond or a double bond; X is hydrogen, fluorine, chlorine or methyl; Y is hydrogen and Z is hydrogen, fluorine or chlorine, or ...
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4181669 |
Steroid esters preparation
This invention relates to an improved steroid ester synthesis in which a carbodiimide, in combination with an acid catalyst, is used as condensing agent.
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4180504 |
Method for the preparation of esters
This invention relates to an improved ester synthesis in which a carbodiimide, in combination with an acid catalyst, is used as condensing agent.
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4150126 |
Novel enol esters of steroids, compositions containing such compounds, processes for their preparation and methods of treatment therewith
This invention relates to novel enol esters of steroids having an antitumor activity and to the preparation thereof. The invention is also concerned with pharmaceutical compositions containing the...
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4086254 |
Photocleavable steroids
This invention relates to novel compounds of the formula: ##STR1## wherein X is H, methoxy, bromine or chloro; R 1 is hydrogen or hydroxy, acyloxy wherein acyl is 2 to 8 carbon atoms, R 2 is...
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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,...
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3984544 |
Retinoic acid esters of steroids of the pregnane series, their use in the treatment of acne and pharmaceutical formulations useful therefor
Novel retinoic acid esters of anti-inflammatory steroids of the pregnane series are described and their use in the treatment and control of acne vulgaris via the topical or intralesional route. A...
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3963707 |
Novel N-nitroso compounds, compositions containing such compounds, processes for their preparation and methods of treatment therewith, and novel intermediates
This invention relates to novel N-halogenoalkyl-N-nitroso carbamates and N 4 halogenalkyl-N 4 -nitroso allophanates of steroid compounds, having an anti-tumor activity, and to the preparation...
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3894004 |
Novel 11-oxygenated pregneno (17,16α-D)-1,3-oxathiolanes and process for the preparation thereof
Topical anti-inflamatory 11-oxygenated pregneno[17,16α-d]-1', 3'-oxathiolanes of the formula I ##SPC1## wherein R 1 and R 2 , can be the same or different and are a hydrogen atom, an alkyl, a...
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3673179 |
C-21 LOWER ALKYLSULFINYL ESTERS OF CERTAIN 21-HYDROXYCORTICOSTEROIDS
C-21 Lower alkylsulfinyl esters of certain 21-hydroxycorticosteroids are good antiinflammatory agents which have both topical and systemic activities. These compounds are best prepared by a 2-step...
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3609172 |
NEW STEROID DERIVATIVES
New 21-esters of steroids of formula St--OCO (CH 2 ) 5 --NH--COCH 3 wherein St represents a steroid residue from pregnadiene series, the ester group being attached to the carbon at 21- position...
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3531503 |
TETRACYCLIC COMPOUNDS AND PROCESSES
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3484436 |
BICYCLO(2.2.2)OCTANE - 1 - -CARBOXYLATE ESTERS OF DELTA**4 - PREGNENE CORTICOID STEROIDS
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3463793 |
PROCESS FOR THE PREPARATION OF 9ALPHA-HALOGENO-11BETA-SUBSTITUTED STEROIDS
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3445571 |
HYDROCORTISONE CYCLOHEXYLSULFAMATE,PHARMACEUTICAL COMPOSITIONS THEREOF,AND METHOD OF USE
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