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Class 552/521 - The nitrogen is bonded directly at the 3-position


Subclass of Class 552 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the nitrogen is bonded directly at the
No. of patents: 52
Last issue date: 06/01/2010


1    
NumberTitleIssue Date
7728157Regioselective and stereoselective oxidation of fused ring systems useful for the preparation of aminosterols
An efficient method for the synthesis of aminosterol compounds such as squalamine and compound 1436 is described. A method of the invention provides for regioselective sulfonation of a fused ring system. The fused ring system base can be, for example, a steroid ring...
06/01/2010
7410959Therapeutic uses for aminosterol compounds
A pharmaceutical composition includes, as an active ingredient, a compound according to formula 1436 as shown in FIG. 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. Various pharmaceutical products may...
08/12/2008
7371741Estradiol 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 specification. ...
05/13/2008
71384275-β-sapogenin and pseudosapogenin derivatives and their use in the treatment of dementia
The invention discloses the use of sapogenin derivatives in the treatment of cognitive disfunction and similar conditions. Methods of treatment and pharmaceutical compositions are also disclosed ...
11/21/2006
71125803-nitrogen-6, 7-dioxygen steroids and uses related thereto
A compound of the formula: and pharmaceutically acceptable salts, solvates, stereoisomers and prodrugs thereof, in isolation or in mixture, wherein R groups are as defined by the present specification. The compou...
09/26/2006
7074778Asthma 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 down regulating the IL-9 pathway and alleviating asthmatic responses to ...
07/11/2006
6962909Treatment of neovascularization disorders with squalimine
Aminosterol compounds are described that are useful as inhibitors of the sodium/proton exchanger (NHE). Methods of using such aminosterols compounds are also enclosed, including those employing compounds that are inhibitors of a spectrum of NHEs as well as those usi...
11/08/2005
66356293-nitrogen-6,7-dioxygen steroids and uses related thereto
A compound of the formula ##STR1## or pharmaceutically acceptable salts, solvates, and stereoisomers thereof, in isolation or in mixture, wherein the R groups are as defined by the present specification. The compounds may be formulated into pharmaceutical...
10/21/2003
6610866Stereoselective synthesis of 24-hydroxylated compounds useful for the preparation of aminosterols, vitamin D analogs, and other compounds
A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereoselectively reduces ...
08/26/2003
6479681Bile acid salts
A process for the preparation of the compounds of general formula (I) ##STR1## in which R1 is H or OH; R2 is H, ଱-OH, or ଲ-OH; and R3 is a straight or branched C1 -C4 alkyl group or a benzyl gr...
11/12/2002
6388108Aminosterol compounds and uses thereof
Newly isolated aminosterol compounds and pharmaceutical compositions based on the aminosterol compounds are described. Methods for the treatment of various disorders, for example, a microbial infection, are also described....
05/14/2002
6307074Process for the preparation of bile acid derivatives
A process for the preparation of the compounds of general formula (I) ##STR1## in which R1 is H or OH; R2 is H, ଱-OH, or ଲ-OH; and R3 is a straight or branched C1 -C4 alkyl group or a benzyl gr...
10/23/2001
6262283Stereoselective synthesis of 24-hydroxylated compounds useful for the preparation of aminosterols, vitamin D analogs, and other compounds
A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereoselectively reduces ...
07/17/2001
5892116Gelators
Gelators gel a variety of nonpolar and polar liquids. Moreover, gelation of various monomers with subsequent polymerization of the gelled monomers forms organic zeolites and membrane materials. An ionic gelator includes salts of compounds of the formula (...
04/06/1999
5874597Certain aminosterol compounds and pharmaceutical compositions including these compounds
Aminosterol compounds are described that are useful as inhibitors of the sodium/proton exchanger (NHE). Methods of using such aminosterols compounds are also enclosed, including those employing compounds that are inhibitors of a spectrum of NHEs as well a...
02/23/1999
5866603Derivatives of estra 1,3,5(10)triene-17-one, 3-amino compounds and their use
This invention discloses compounds useful as steroid sulfatase inhibitors. The compounds comprise the formula (1) ##STR1## wherein (a) R is selected from the group consisting of hydrogen, a lower alkyl group, an alkoxy group, halogen, NH2,...
02/02/1999
5856535Aminosterol ester compounds
An aminosterol compound according to the following formula: ##STR1## wherein: R1 is a member selected from the group of: ##STR2## R2 is H or OH; R3 is H or OH; R4 is H or OH; and R5 is a C1
01/05/1999
5847172Certain aminosterol compounds and pharmaceutical compositions including these compounds
Aminosterol compounds are described that are useful as inhibitors of the sodium/proton exchanger (NHE). Methods of using such aminosterols compounds are also enclosed, including those employing compounds that are inhibitors of a spectrum of NHEs as well a...
12/08/1998
5840936Aminosterol compounds useful as inhibitors of the sodium/proton exchanger (NHE)
Aminosterol compounds are described that are useful as inhibitors of the sodium/proton exchanger (NHE). Methods of using such aminosterols compounds are also enclosed, including those employing compounds that are inhibitors of a spectrum of NHEs as well a...
11/24/1998
5840740Aminosterol compounds and a method of treating infection using the aminosterol compounds
Disclosed are aminosterol compounds 1360 and 1361: ##STR1## which can be obtained in isolated or purified form from the liver of the dogfish shark....
11/24/1998
5792635Method of inhibiting the sodium/proton exchanger NHE3 and method of inhibiting growth by administering squalamine
Aminosterol compounds are described that are useful as inhibitors of the sodium/proton exchanger (NHE). Methods of using such aminosterols compounds are also disclosed, including those employing compounds that are inhibitors of a spectrum of NHEs as well ...
08/11/1998
5646316Bile acid inhibitors of metalloproteinase enzymes
The present invention relates to a bile acid derivative, which comprises a bile acid derivatized at the carboxyl group with a hydroxamic acid or hydroxamate ester. The carboxyl group in the bile acid compound can also be derivatized with an amino acid or ...
07/08/1997
5637691Steroid derivatives, pharmaceutical compositions containing them, and their use as antibiotics or disinfectants
Compounds having a broad range of antimicrobial activity generally have a structure including asteroid nucleus with a cationic, preferably polyamine, side chain (X) and an anionic side chain (Y). The invention is also directed to compounds of the Formula ...
06/10/1997
5610149Steroidal polyamines
New steroidal polyamines have the structure of formula I or formula II: ##STR1## wherein R1 and R2 are independently N(R')3+ or H in the ଱- or ଲ- position except both R1 and R2...
03/11/1997
5571933Derivatives of estra 1,3,5(10)triene-17-one, 3-amino compounds and their use
This invention discloses compounds useful as steroid inhibitors. The compounds comprise the formula (5) ##STR1## wherein (a) R1 is hydrogen and R2 is selected from the group consisting of SO2 CF3, SO2
11/05/1996
556112417-଱-acyl steroids which inhibit 5-଱-reductase
The invention relates to substituted 17଱-acyl steroidal 5଱-reductase inhibiting compounds. The invention also relates to pharmaceutical compositions containing these compounds and their use for reducing prostate size and treating prostate aden...
10/01/1996
5559258Ethylenically unsaturated bile acid derivatives, processes for their preparation and precursors
Ethylenically unsaturated bile acid derivatives of the formula I G--X--A I in which G, X and A have the meanings indicated, are described. They are suitable for the preparation of polymeric bile acid derivatives. B...
09/24/1996
5486626Process for the preparation of 3ଲ-aminocholanic acid derivatives
Process for the preparation of 3ଲ-aminocholanic acid derivatives A process for the preparation of 3ଲ-aminocholanic acid derivatives of the formula II ##STR1## wherein R(1), R(2) and R(3) have the meanings given, starting from the correspo...
01/23/1996
5192756Aminosterol antibiotic
An aminosterol antibiotic, (3ଲ(N-[3-aminopropyl]-1,4-butanediamine)-7଱,24.zeta.-dihydroxy- 5଱-cholestane 24-sulfate), which can be isolated from the stomach of the common dogfish shark, Squalus acanthias, is disclosed....
03/09/1993
509350214଱,17଱-dihydroxy-17ଲ-substituted steroids
A process for the preparation of novel 14଱, 17଱-dihydroxy-17ଲ-substituted steroids by reacting 14଱-hydroxy-17-oxo-steroids with metal organic compounds and the use of the said novel steroids in the production of 14଱, 17&...
03/03/1992
5086190Method of fluorinating by using N-fluoropyridinium pyridine heptafluorodiborate
The present invention provides a novel compound represented as ##STR1## The present novel compound is prepared by reacting fluorine with pyridine-boron trifluoride and is useful as a fluorinating agent in the fluorination of organic compounds....
02/04/1992
5003063Conversion of steroidal 17-cyanohydrins to corticoids
The invention involves a two step chemical transformation of a steroidal 17-cyanohydrin (II) ##STR1## to a 17଱-hydroxy-21-halo-20-keto steroid (IV) ##STR2## intermediate which can readily be converted to pharmaceutically useful cortic...
03/26/1991
5001234Cyclic hydrocarbons with an aminoalkyl sidechain
This invention provides novel cyclic hydrocarbons of the formula: ##STR1## wherein R is selected from the group consisting of CH2 .dbd.CH--CH2 --, HO--CH2 CH2 CH2 --, and CH3 ; wherein R
03/19/1991
4977255Steroidal 17଱-silyl ethers and process to corticoids and progesterones
17ଲ-Cyano-17଱-hydroxy steroids (I) are transformed to 17଱-halo silyl ethers (II) which are intermediates useful in the production of progesterones (V), 17-hydroxyprogesterones (VI), corticoids (VII) and 21-halo corticoids (III) which can...
12/11/1990
49702043-substituted nitro-steroid derivatives as 5-଱-reductase inhibitors
Invented are 3-nitro- substituted steroidal synthetic compounds, pharmaceutical compositions containing the compounds, and methods of using these compounds to inhibit steroid 5-଱-reductase including using these compounds to reduce prostate size. Als...
11/13/1990
483113111ଲ,17଱-Dihydroxy-17ଲ-cyano-androstanes
Using cyanohydrin intermediates, 17-keto steroids are transformed to corticoids and 17଱-acyl progesterones....
05/16/1989
4780455Lipophilic complexes of pharmacologically active organic compounds
The present invention provides a composition with the structure wherein m and n are each integers, and m and n are different or the same; L is an ampholytic lipid or polymer, or a nonampholytic lipid with hydrophobic properties; E is a nonlipophilic ionic inor...
10/25/1988
4600538Corticosteroids from 17-keto steroids via 20-cyano-Ɗ17 (20)-pregnanes
The process of the present invention transforms 17-keto steroids (I) to the corresponding corticoids (IV) in three steps....
07/15/1986
4585590Cyanohydrin process
Using cyanohydrin intermediates, 17-keto steroids are transformed to corticoids and 17଱-acyl progesterones....
04/29/1986
456700116-Methylene-17଱-hydroxy-progesterones
16-Methylene-17-keto steroids (III) are transformed to the corresponding 16-methylene-17଱-hydroxyprogesterones (VII) which are intermediates useful in the production of betamethasone, diflorasone diacetate and melengesterol acetate....
01/28/1986
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