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Class 514/176 - Nitrogen containing hetero ring


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the hetero ring contains at least
No. of patents: 275
Last issue date: 04/24/2012


1              
NumberTitleIssue Date
8163724Glucocorticosteroids, processes for their preparation, pharmaceutical compositions containing them and their use in therapy
The present invention provides compounds of formula (I) wherein n, p, R1, R2, X1, X2, X3, X4, X5, R3a, R3b, R4, R...
04/24/2012
808875817β-hydroxysteroid dehydrogenase type I inhibitors
3,15-substituted estrone compounds which act as inhibitors of 17β-hydroxysteroid dehydrogenase type I (17β-HSD1), salts thereof, pharmaceutical preparations containing such compounds, processes for preparing such compounds, and therapeutic uses of such compounds, ...
01/03/2012
8080540Therapeutically active triazoles and their use
Estratrien-triazoles corresponding to formula (I) (shown below) which are useful in therapy, especially for the treatment and/or prevention or inhibition of a steroid hormone dependent disorder, preferably a steroid hormone dependent disease or disorder requiring th...
12/20/2011
8067401Compounds and compositions for treating infection
Compounds from 14 Kenyan plants, including from the root of Dovyalis abyssinica and Clutia robusta have been characterized and isolated, and their uses are disclosed. ...
11/29/2011
7947668Aminoalkyl sterol compounds having an anti-tumoral and neuroprotective activity
Sterol derivatives of formula (I) and a method for the production of the compounds, a medicament using one of the compounds and a pharmaceutical composition comprising the medicament. ...
05/24/2011
7875599C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity
Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3β-acetoxy-17-c...
01/25/2011
7838515Formulations of quaternary ammonium neuromuscular blocking agents
Muscle relaxant formulations which include one or more quaternary ammonium neuromuscular blocking agents have a reduced tendency for hydrolytic degradation, and therefore a longer shelf life stability, when combined with one or more organic anions having at least si...
11/23/2010
7727976Bile-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 the intestinal wall after oral administration to provide for enhanced t...
06/01/2010
7691836Progesterone receptor modulators
The subject invention provides a compound according to Formula I, wherein each of the substituents is given the definition as set forth in the specification and claims, or a pharmaceutically acceptable salt and/or hydrate f...
04/06/2010
7687486Selective estrogen receptor modulators
Compositions and methods for treating a cancer in mammals by administering selective estrogen receptor modulators particularly compounds represented by: or any other of the structures contained herein, or of a stereoisomer,...
03/30/2010
767104517-phosphorous steroid derivatives useful as progesterone receptor modulators
The present invention is directed to novel 17-phosphorous steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor. ...
03/02/2010
7557097Structural, behavioral characterization, and synthesis of attractants for migratory lamprey
Compounds that function as lamprey attractants and methods. ...
07/07/2009
7517870Use 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 diseases related with ocular neovascularization. Particularly, the above-me...
04/14/2009
7407947Amphoteric 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, together with liposomes containing such compounds and their uses....
08/05/2008
7396827Pharmaceutical 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 comprises less than about 3% water. The compositions are useful to make imp...
07/08/2008
7381718Method for preparing oestrogen derivatives
A process for the preparation of compounds of formula (I) in which R1, R2, R3 and n are defined as indicated in the description, use of said compoun...
06/03/2008
73750988β-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 products, pharmaceutical preparat...
05/20/2008
7345034Azacyclosteroid 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. ...
03/18/2008
7312206Sterol 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 relates to liposomes containing said sterol derivatives. ...
12/25/2007
7265099Use 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 reversal, and to cyclophane derivatives having general formula (A) whe...
09/04/2007
7244762Antitumoral d-homoestra-1,3,5 (10)-trien-3-yl 2-substituted sulfamates
This invention relates to 2-substituted D-homo-estra-1,3,5(10)-trien-3-yl sulfamates of general formula I (I), in which R3 means a C1-C5-alkyl or C1-C5-alkyloxy group as well as their use for the production of a pharmaceutical agent for treating tumor diseases, whic...
07/17/2007
7229835Amine detection method and materials
A compound linked to a solid support (R) through a divalent linker moiety (X) and which is represented by the following formula: is disclosed. In particular, the 1-hydroxybenzotriazole-6-carboxylic acid is direct...
06/12/2007
7205415Process for the preparation of simvastatin
A process for manufacturing simvastatin is provided using novel intermediates. Thus, for example, lovastatin is reacted with methoxyethylamine, alpha methylated 2-methylbutyryl side chain of the amide formed, hydrolyzed and lactonized to produce finally simvastatin ...
04/17/2007
7182942Vaccine 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 (CY), or an effective amount of indomethacin (INDO), wherein the NCM, C...
02/27/2007
7176221Low dose pharmaceutical composition having uniform drug distribution and potency
A method for manufacturing a pharmaceutical composition having uniform drug distribution and potency is described which utilizes silicon dioxide to reduce the loss of active ingredient during the manufacturing process. The method is particularly useful for the manuf...
02/13/2007
7161008Optically active β-aminoketones, optically active 1,3-amino alcohols and processes for preparing them
The invention relates to chiral Mannich bases of formula (I), chiral 1,3-amino alcohols of formula (II) derived therefrom, wherein R1, R2, R3, R4 and R5 are as defined herein, and to processes for preparing Mann...
01/09/2007
7153930Peptide transport
The present invention relates to improving and/or increasing the bioavailability of a biologically active substance, such as a peptide. In particular, the present invention relates to the conjugation of the biologically active substance to a bile acid. The conjugate...
12/26/2006
7153844Estrogen-linked platinum (II) complexes as anticancer agents
wherein X may be —CH2—O—CH2— or —CH2—, wherein n may be 1, 2, 3, 4 or 5 when X is —CH2—O—CH2—, wherein n may be 2, 3, 4, 5, 6, 7, 8, 9 or 10 when X is ...
12/26/2006
7135581Antiangiogenic 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 th...
11/14/2006
7078396Method of treating disorder related to high cholesterol concentration
A method of treating a disorder related to a high cholesterol concentration, comprising administering to a subject in need thereof a compound of formula (I): Also disclosed are methods, kits, combinations, and co...
07/18/2006
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
7074779Estrieno[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 by an estrogen receptor. ...
07/11/2006
706750317-aryl linker derivatised estrogen 3-sulphamates as inhibitors of steroid sulphatase
There is provided a compound comprising a steroidal ring system and a group R1 selected from any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring of the steroidal ring ...
06/27/2006
7056906Combinations of hormone replacement therapy composition(s) and sterol absorption inhibitor(s) and treatments for vascular conditions in post-menopausal women
The present invention provides compositions, therapeutic combinations and methods including: (a) at least one hormone replacement therapy composition; and (b) at least one sterol absorption inhibitor which can be useful for treating vascular conditions in post-menop...
06/06/2006
7053076Bile-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 the intestinal wall after oral administration to provide for enhanced t...
05/30/2006
7053074Prevention of ovarian cancer by administration of a Vitamin D compound
The present invention relates to methods for preventing the development of epithelial ovarian cancer by administering a Vitamin D compound in an amount capable of increasing apoptosis in non-neoplastic ovarian epithelial cells of the female subject. ...
05/30/2006
7049305Bile-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 to pharmaceutical compositions including and methods using such comp...
05/23/2006
7045513DHEA composition and method
Disclosed are improved pharmaceutical formulations comprising dehydroepiandrosterone (DHEA), enriched in selected polymorphic forms, for therapeutic applications. In one embodiment, the formulation comprises, in solid form, DHEA, at least 85% of which is present as ...
05/16/2006
7040756Process for surface modifying substrates and modified substrates resulting therefrom
The present invention generally relates to a method of modifying the surface of substrates such as contact lenses and other biomedical articles by at least partially coating the surfaces of such substrates with a polymeric tie layer having reactive sites. Various ot...
05/09/2006
7037907Estradiol conjugates and uses thereof
A conjugated prodrug of an estradiol compound conjugated to a biological activity modifying agent. ...
05/02/2006
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