| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 141 | 17-beta HSD1 and STS Inhibitors | US12892351 | 2010-09-28 | US20110021480A1 | 2011-01-27 | Josef Messinger; Heinrich-Hubert Thole; Bettina Husen; Michael Weske; Pasi Koskimies; Lila Pirkkala |
| Substituted steroid compounds which represent selective inhibitors of 17β-hydroxysteroid dehydrogenase type I (17β-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17β-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17β-estradiol concentration. | ||||||
| 142 | Cyanine dyes and their applications as luminescence quenching compounds | US12807180 | 2010-08-30 | US20100331543A1 | 2010-12-30 | Zhenjun Diwu; Jianheng Zhang; Yi Tang |
| The quenching compounds of the invention are weakly luminescent cyanines that are substituted by one or more heteroaromatic quenching moieties. The quenching compounds of the invention exhibit little or no observable luminescence and efficiently quench a broad spectrum of luminescent compounds. The chemically reactive quenching compounds possess utility for labeling a wide variety of substances, including biomolecules. These labeled substances are highly useful for a variety of energy-transfer assays and applications. | ||||||
| 143 | STEROIDS AS AGONISTS FOR FXR | US12547147 | 2009-08-25 | US20100022498A1 | 2010-01-28 | Roberto Pellicciari |
| The invention relates to compounds of formula (I): wherein R is ethyl and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists. | ||||||
| 144 | Pure rocuronium bromide | US11521197 | 2006-09-13 | US07642246B2 | 2010-01-05 | Juana Araceli Mendez; Marco A. De La Mora; Alejandro Guillen; Hugo Herrera |
| Disclosed herein is rocuronium bromide having a potentiometrical assay of from 99% to 101% in acetic acid and perchloric acid, having less than about 0.2% area by HPLC of 2β-(4-morpholinyl)-16β-(1-pyrrolidinyl)-5α-androstan-3α-ol-17β-acetate, and having at least one of the solvents ethyl ether and dichioromethane in an amount equal to or less than about 850 ppm, and 600 ppm, respectively. | ||||||
| 145 | Nitrooxyderivative steroidal compounds | US11643887 | 2006-12-22 | US07524836B2 | 2009-04-28 | Piero Del Soldato |
| Steroidal compounds or their salts having general formulas (I) and (II) wherein: s is an integer equal to 1 or 2, preferably s=2; b0=0 or 1; A=R—, wherein R is the steroidal drug radical, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological tests reported in the description. A-(B)b0—C—N(O)s (I) | ||||||
| 146 | FREE CHOLESTEROL ANALOGS BEARING A BORON DIPYRROMETHENE DIFLUORO (BODIPY) FLUOROPHORE IN THE SIDE CHAIN AND METHOD OF PREPARATION AND USE THEREOF | US12013120 | 2008-01-11 | US20080177059A1 | 2008-07-24 | Robert Bittman; Zaiguo Li |
| The present invention relates to free cholesterol analogs bearing a boron dipyrromethene difluoro (BODIPY) fluorophore in the side chain and methods of preparation. The compounds of the present invention can be used in fluorescence spectroscopy and fluorescence microscopy to visualize the exchange, distribution, and trafficking of free cholesterol between living cells and to monitor the movement of free cholesterol between ordered and disordered lipid domains in membranes. | ||||||
| 147 | STEROL DERIVATIVES, LIPOSOMES COMPRISING STEROL DERIVATIVES AND METHOD OF LOADING LIPOSOMES WITH ACTIVE SUBSTANCES | US11934147 | 2007-11-02 | US20080113017A1 | 2008-05-15 | STEFFEN PANZNER; Gerold Endert; Stefan Fankhanel; Anja Behrens |
| A sterol derivative with a pKa value of between 3.5 and 8, according to the general formula cation-spacer 2-Y-spacer 1-X-sterol, wherein Y and X represent linking groups, is suggested, as well as liposomes comprising such sterol derivatives. | ||||||
| 148 | Nitrate esters of corticoid compounds and pharmaceutical applications thereof | US11714724 | 2007-03-07 | US20070161612A1 | 2007-07-12 | Piero Soldato |
| Compounds of the formula and use of the compounds as medicaments. | ||||||
| 149 | Pharmaceutical compounds | US11643887 | 2006-12-22 | US20070142342A1 | 2007-06-21 | Piero Soldato |
| Steroidal compounds or their salts having general formulas (I) and (II) wherein: s is an integer equal to 1 or 2, preferably s-2: bO 0 or 1; A═R—, wherein R is the steroidal drug radical, C and C1 are two bivalent radicals. The precursors of the radicals B and B1 are such as to meet the pharmacological tests reported in the description. | ||||||
| 150 | Steroids as agonists for FXR | US11602307 | 2006-11-21 | US20070142340A1 | 2007-06-21 | Roberto Pellicciari |
| The invention relates to compounds of formula (I): wherein R is ethyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists. | ||||||
| 151 | Processes for the synthesis of rocuronium bromide | US11521282 | 2006-09-13 | US20070117975A1 | 2007-05-24 | Juana Mendez; Marco De La Mora; Angel Rodriguez; Efrain Barragan; Hugo Herrera; Alejandro Guillen |
| The invention encompasses processes for synthesizing 1-[17β-acetyloxy-3α-hydroxy-2β-(4-morpholinyl)-5α-androstan-16β-yl]-1-(2-propenyl)pyrrolidinium bromide (rocuronium bromide) and intermediates thereof. | ||||||
| 152 | Nitrate esters of corticoid compounds and pharmaceutical applications thereof | US11445140 | 2006-06-02 | US07205288B2 | 2007-04-17 | Piero Del Soldato |
| Compounds of the formula and use of the compounds as medicaments. | ||||||
| 153 | Steroidal compounds | US11028198 | 2005-01-04 | US07186708B2 | 2007-03-06 | Piero Del Soldato |
| Steroidal compounds or their salts having general formula: A—B—C—NO2 are described, wherein: A=R—, wherein R is a steroidal drug radical; B=—TB—X2—TBI—, wherein TB is (CO), TBI is O, S, NH, and X2 is a bivalent bridging group; and C is a bivalent radical. | ||||||
| 154 | Derivative prodrugs of ethinyl estradiol | US11478582 | 2006-07-03 | US20070015740A1 | 2007-01-18 | James Keown; James McIlroy; John King; Claire Gilligan; William Armstrong |
| The present invention is a prodrug derivative of ethinyl estradiol according to Formula I: | ||||||
| 155 | Steroids as agonists for FXR | US10471549 | 2002-02-21 | US07138390B2 | 2006-11-21 | Roberto Pellicciari |
| The invention relates to compounds of formula (I): wherein R is ethyl and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists. | ||||||
| 156 | Cyanine dyes and their applications as luminescence quenching compounds | US11222049 | 2005-09-07 | US20060223076A1 | 2006-10-05 | Zhenjun Diwu; Jianheng Zhang; Yi Tang |
| The quenching compounds of the invention are weakly luminescent cyanines that are substituted by one or more heteroaromatic quenching moieties. The quenching compounds of the invention exhibit little or no observable luminescence and efficiently quench a broad spectrum of luminescent compounds. The chemically reactive quenching compounds possess utility for labeling a wide variety of substances, including biomolecules. These labeled substances are highly useful for a variety of energy-transfer assays and applications. | ||||||
| 157 | 3-nitrogen-6, 7-dioxygen steroids and uses related thereto | US10624946 | 2003-07-21 | US07112580B2 | 2006-09-26 | Jeffery R Raymond; Claudia E Kasserra; Yaping Shen |
| 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 compounds may be formulated into pharmaceutical compositions, and used in the treatment and/or prevention of various conditions, including inflammation, asthma, an allergic disease, chronic obstructive pulmonary disease, atopic dermatitis, solid tumors, AIDS, ischemia, and cardiac arrhythmias. | ||||||
| 158 | Nitrate esters of corticoid compounds and pharmaceutical applications thereof | US11374315 | 2006-03-14 | US20060160781A1 | 2006-07-20 | Piero Soldato |
| Compounds of the formula and use of the compounds as medicaments. | ||||||
| 159 | Steroid compounds with anti-tumor activity | US10538993 | 2003-12-18 | US20060149045A1 | 2006-07-06 | Jean-Claude Braekman; Eric Quaquebeke; Laurent Ingrassia; Janique Dewelle; Robert Kiss; Francis Darro |
| The present invention relates to novel steroid compounds of Formula (IB) having anti-tumor activity. The present invention also relates to a method for the preparation of said steroid compounds. The invention further relates to a pharmaceutical composition comprising an effective amount of said steroid compounds. Furthermore, the present invention concerns the use of said steroid compounds as a medicament and in the preparation of a medicament for the treatment of cancer. The present invention also relates to the use of a steroid compound or a pharmaceutical composition comprising said steroid compound according to the invention in the treatment of cancer. | ||||||
| 160 | Nitrate esters of corticoid compounds and pharmaceutical applications thereof | US10462637 | 2003-06-17 | US07056905B2 | 2006-06-06 | Piero Del Soldato |
| Compounds of the formula and use of the compounds as medicaments. | ||||||
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