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| Number | Title | Issue Date |
| 7449455 | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in contraception and in treating melanoma, osteoporosis, acne, dysfunctional ... | 11/11/2008 |
| 7442707 | CCI-779 polymorph and use thereof The present invention provides CCI-779 polymorph Form II. This invention also provides processes for preparing CCI-779 polymorph Form II and pharmaceutical compositions including CCI-779 polymorph Form II. ... | 10/28/2008 |
| 7414142 | 5-aryl-indan-1-one oximes and analogs useful as progesterone receptor modulators Compounds of formula I, wherein R1-R9 and n are defined herein, and pharmaceutical compositions and kits containing these compounds are provided. Also provided are methods of inducing contraception, prov... | 08/19/2008 |
| RE40418 | Treatment of neoplasms with CCI-779/EKB-569 combination This invention provides the use of a combination of CCI-779 and EKB-569 in the treatment of neoplasms. ... | 07/01/2008 |
| 7384953 | Purification of rapamycin Purified rapamycin and a chemical process for obtaining the purified rapamycin are described. ... | 06/10/2008 |
| 7381856 | Carbon-carbon cross coupling catalyzed by transition metals on solid supports The present invention provides methods of coupling carbon-containing compounds using a transition metal or transition metal complex on a solid support. The solid support can include alkaline earth metal salts, including carbonate and sulfate salts. The transition me... | 06/03/2008 |
| 7358246 | Thioamide derivatives as progesterone receptor modulators Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies. ... | 04/15/2008 |
| 7354927 | 6H-[1]benzopyrano[4,3-b]quinolines and their use as estrogenic agents This invention provides 6H-[1]benzopyrano[4,3-b]quinoline compounds having the formula I: The invention further provides compositions including the compounds, methods for the use of the compounds, and methods of preparation o... | 04/08/2008 |
| 7332601 | CCI-779 derivatives and methods of making same A method of generating synthetic metabolites of CCI-779 is provided. Five novel CCI-779 derivatives are described, as are methods of using these derivatives for detecting CCI-779 metabolites in samples. ... | 02/19/2008 |
| 7319152 | 5-Aryl-indan-1-one and analogs useful as progesterone receptor modulators Compounds of formula I or II are provided, wherein R1-R8 are defined herein, and pharmaceutical compositions and kits containing these compounds. Also provided are methods of inducing contraception, providing hormone replacement therapy, treati... | 01/15/2008 |
| 7317037 | Progesterone receptor modulators comprising pyrrole-oxindole derivatives and uses thereof Pyrrole-oxindole derivatives useful as progesterone receptor antagonists, and methods for preparing the same, are provided. Pharmaceutical compositions containing these derivatives are described, as is the use thereof in contraception and hormone-related conditions.... | 01/08/2008 |
| 7314932 | Methods for minimizing thioamide impurities Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrite groups, are provided. ... | 01/01/2008 |
| 7297713 | Cyanopyrrole-phenyl amide progesterone receptor modulators and uses thereof Progesterone receptor modulators of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 are as define... | 11/20/2007 |
| 7297688 | Starter kit for low dose oral contraceptives The present invention provides a contraceptive kit which helps to overcome or ameliorate the problem of breakthrough bleeding and spotting associated with lowest dose (15-20 ug EE) estrogen contraceptives. ... | 11/20/2007 |
| 7291643 | Cyanopyrrole-sulfonamide progesterone receptor modulators and uses thereof Progesterone receptor modulators of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are... | 11/06/2007 |
| 7288647 | Recovery of CCI-779 from mother liquors The invention provides a process for recovering CCI-779 from mother liquors. ... | 10/30/2007 |
| 7282505 | Rapamycin polymorphs and uses thereof The present invention provides rapamycin polymorph Form II. This invention also provides processes for preparing rapamycin polymorph Form II and pharmaceutical compositions including rapamycin polymorph Form II. ... | 10/16/2007 |
| 7276498 | Rapamycin analogues and uses thereof in the treatment of neurological disorders The present invention provides compounds of the following structure, wherein R1, R2, R4, R4′, R6, R7, and R15 are defined above: These ... | 10/02/2007 |
| 7273874 | Rapamycin derivatives and the uses thereof in the treatment of neurological disorders The present invention provides compounds of the following structure, wherein R1-R9, R15, and n are defined herein. These compounds are useful in treating neurological disorders or c... | 09/25/2007 |
| 7271177 | Amorphous rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid and its pharmaceutical compositions The present invention provides an amorphous form of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid. This invention also provides processes for preparing the amorphous form and pharmaceutical compositions including the amorphous form. ... | 09/18/2007 |
| 7268144 | Regiospecific synthesis of rapamycin 42-ester derivatives A method for the regiospecific synthesis of rapamycin 42-ester derivatives is described. The method involves lipase-catalyzed acetylation of 42-hydroxy of rapamycin with an acyl donor such as a vinyl ester, an isopropenyl ester or an anhydride in a suitable organic ... | 09/11/2007 |
| 7268149 | Cyclothiocarbamate derivatives as progesterone receptor modulators and methods of treating skin disorders The present invention provides methods of treating skin disorders includes delivering to a mammal a composition containing a compound of formula I, or tautomers thereof, in a regimen, wherein formula I is: and wh... | 09/11/2007 |
| 7253203 | Indoline derivatives This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, havin... | 08/07/2007 |
| 7247624 | 2-Phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in treating colon cancer. ... | 07/24/2007 |
| 7247650 | Macrolides and methods for producing same This invention relates, in part, to macrolide compounds, actinomycete strains for producing them, and pharmaceutical compositions containing them. ... | 07/24/2007 |
| 7247625 | 6-amino-1,4-dihydro-benzo[d][1,3] oxazin-2-ones and analogs useful as progesterone receptor modulators Compounds having the structure of formula I are provided. In formula I, R1 is H, OH, substituted or unsubstituted C1 to C3 alkyl, C1 to C3 perfluoroalkyl, or COR6; R6 is H, substituted or u... | 07/24/2007 |
| 7241771 | Oxepane isomer of 42-O-(2-hydroxy)ethyl-rapamycin The invention provides a purified oxepane isomer of 42-O-(2-hydroxy)ethyl-rapamycin (SDZ-RAD Isomer C), a chemical process for its preparation, as well as pharmaceutical compositions and packs containing SDZ-RAD Isomer C and methods for its use as an immunosuppressi... | 07/10/2007 |
| 7235539 | 6-Hydroxyequilenins as estrogenic agents This invention provides estrogen receptor modulators of formula I, having the structure wherein, R1 is hydrogen, alkyl of 1–6 carbon atoms, benzyl, alkylcarbonyl of... | 06/26/2007 |
| 7202256 | Proline CCI-779, production of and uses therefor, and two-step enzymatic synthesis of proline CCI-779 and CCI-779 Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of 2,2-bis(hydroxymethyl) propionic acid in an organic solvent followed by deprotection. A... | 04/10/2007 |
| 7192956 | Methods of treating hormone-related conditions using cyclothiocarbamate derivatives The present invention provides methods of inducing contraception which includes delivering to a female a composition containing a compound of formula I or formula II, or tautomers thereof, in a regimen which involves delivering one or more of a selective estrogen re... | 03/20/2007 |
| 7153957 | Regioselective synthesis of CCI-779 A method for regioselective synthesis of CCl-779 based on boronate chemistry is provided. Also provided are novel intermediates useful in this method. ... | 12/26/2006 |
| 7148247 | Substituted benzoxazoles as estrogenic agents This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R2a, R3, R3a, and R4, and X as def... | 12/12/2006 |
| 7138392 | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: or which are useful in treat... | 11/21/2006 |
| 7132417 | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in treating uterine leiomyoma. ... | 11/07/2006 |
| 7129258 | Substituted benzoxazoles as estrogenic agents This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R2a, R3, R3a, and R4, and X a... | 10/31/2006 |
| 7122705 | Method for preparing 3-cyclopentyloxy-4-methoxybenzaldehyde Processes for coupling phenol and cycloalkyls including combining an optionally substituted phenol, a cycloalkyl substituted with a leaving group, carbonate salt, tetrahydrofuran, and an optional phase transfer agent are provided. Also provided are processes for pre... | 10/17/2006 |
| 7074804 | CCI-779 Isomer C Purified CCI-779 Isomer C is provided, as are pharmaceutical compositions and kits containing same. ... | 07/11/2006 |
| 7060709 | Method of treating hepatic fibrosis This invention provides the use of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) in the treatment or inhibition of hepatic fibrosis and hepatic cirrhosis. ... | 06/13/2006 |
| 7022733 | Substituted 2-phenyl benzofurans as estrogenic agents This invention provides estrogen receptor modulators of formula I, having the structure wherein R, R′, A, A′, X, Y, and Y are as defined in the specification, or a pharmaceutically acceptable salt there... | 04/04/2006 |
| 6960607 | Naphthyl benzoxazoles and benzisoxazoles as estrogenic agents This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R3, and R4, and X as defined in the specification, or a p... | 11/01/2005 |
