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Attorney: Winslow; Anastasia P.


Number of patents: 55
Last date: December 06, 2011

1    
NumberTitleIssue Date
RE43003Epothilone derivatives
The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1–R7 are as defined herein, methods fo...
12/06/2011
RE42191Methods for the preparation, isolation and purification of epothilone B, and X-ray crystal structures of epothilone B
The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent pur...
03/01/2011
7858639Bicyclic heterocycles as cannabinoid-1 receptor modulators
The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to...
12/28/2010
7816357Azabicyclic heterocycles as cannabinoid receptor modulators
The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to...
10/19/2010
7776859Hexahydroimidazopyrazin-3-one compounds useful as modulators of androgen receptor function
The present invention is directed to compounds having the formula (I), and/or pharmaceutically-acceptable salts thereof, useful in the treatment of androgen-receptor associated conditions, wherein Ar is aryl, substituted ar...
08/17/2010
7767432Methods for the preparation, isolation and purification of epothilone B, and x-ray crystal structures of epothilone B
The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent pur...
08/03/2010
RE41393Treatment of refractory tumors using epothilone derivatives
Methods of treating tumors in a mammal, especially a human that has demonstrated resistance to other chemotherapeutic agents, is disclosed. Specifically, methods of the present invention are effective in tumors that have initially been unresponsive to taxane therapy...
06/22/2010
7655689Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds. ...
02/02/2010
75953007-quinolyl ketolide antibacterial agents
15-fluoroketolides of the formula having improved activity and safety, compositions comprising them, and methods for their preparation and use in the treatment of bacterial infections. ...
09/29/2009
7517904Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds. ...
04/14/2009
7501416Quinoxaline compounds and methods of using them
The present invention generally relates to quinoxaline compounds having Formula 1 or Formula 2 wherein the variables are as defined herein, and methods of using them. ...
03/10/2009
7470797Fused heterocyclic imido and amido compounds
Disclosed are fused cyclic compounds, method of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds of formula
12/30/2008
7459294Method of producing a compound by fermentation
During the production of a product compound by fermentation, the concentration of a precursor compound is maintained within a pre-selected concentration range by having an adsorbent resin in contact with the culture medium. The adsorbent resin reversibly adsorbs pre...
12/02/2008
7432267Fused cyclic modulators of nuclear hormone receptor function
Disclosed are compounds having the formula (I): including compounds of formulae (Ia) and (Ib): wherein G is an optionally substituted aryl or heterocyclo, L is an optional linker,...
10/07/2008
7414056Pyrazole-amide compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where G, X, R1, R2, R3, R4, R5, R6
08/19/2008
7390810Pyrazole-amine compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where G, X, R1, R2, R3, R4, R5, R6
06/24/2008
RE40387Pharmaceutical compositions, dosage forms and methods for oral administration of epothilones
The invention relates to methods of increasing the bioavailability of orally administered epothilones. Epothilones administered by the methods of the invention are sufficiently bioavailable to have a pharmacological effect. The invention further relates to pharmaceu...
06/17/2008
7388009Heteroaryl-substituted pyrrolo-triazine compounds useful as kinase inhibitors
Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R
06/17/2008
7342034Fused heterocyclic compounds and analogs thereof, modulators of nuclear hormone receptor function
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds. ...
03/11/2008
7314876Aryl ketone pyrrolo-triazine compounds useful as kinase inhibitors
Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are surprisingly advantageous as p38 kinase inhibitors, wherein R3 is hydrogen, methyl, perfluor...
01/01/2008
7312237Combination of epothilone analogs and chemotherapeutic agents for the treatment of prolilferative diseases
Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders. ...
12/25/2007
7291637Fused heterocyclic compounds and analogs thereof, modulators of nuclear hormone receptor function
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds. ...
11/06/2007
7244594Microbial transformation method for the preparation of an epothilone
A microbial method for the preparation of an epothilone containing a terminal hydroxyalkyl group, comprising contacting at least one epothilone having a terminal alkyl group with an enzyme or microorganism capable of catalyzing the selective hydroxylation of said al...
07/17/2007
7241755Epothilone derivatives
The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1–R7 are as defined herein,...
07/10/2007
7235669Epothilone side components
The invention concerns compounds which can be obtained by fermenting DSM 6773, especially epothilones A1, A2, A8, A9, B10, C1, C2, C3, C4, C5, C6, C7, C8, C9, D1, D2, D5, G1, G2, H1, H2, I1, I2, I3, I4, I5, I6 and K and trans-epothilones C1 and C2. ...
06/26/2007
7235563Spirocyclic compounds useful as modulators of nuclear hormone receptor function
Spirocyclic compounds, methods of using such spirocyclic compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds are disclosed. ...
06/26/2007
7211593C12-cyano epothilone derivatives
The present invention relates to compounds useful in the treatment of cancer or other proliferative diseases represented by the formula wherein: R1, R2
05/01/2007
7172884Methods for the preparation, isolation and purification of epothilone B, and x-ray crystal structures of epothilone B
The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent pur...
02/06/2007
7169771Thiazolyl-based compounds useful as kinase inhibitors
The present invention provides thiazolyl-based compounds of formula (I), useful for treating p38 kinase-associated conditions, wherein ring A is phenyl or pyridyl, and X, Y, B, R2, R3, Z
01/30/2007
7160883Pyrrolo-triazine aniline compounds useful as kinase inhibitors
Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R...
01/09/2007
7157595Degradation of epothilones
According to one embodiment the invention concerns a process for a degradation of an epothilone C or a epothilone D, wherein an epothilone C or epothilone D is subjected to an olefin metathesis in the presence of ethylene and subsequently an optional ester hydrolysi...
01/02/2007
7151113Pyrazole-amine compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where W, X, R1, R2, R3, R4, R5...
12/19/2006
7141578Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds. ...
11/28/2006
7125899Epothilone derivatives
The present invention relates to epothilone derivatives, having the following formula: in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1–R7...
10/24/2006
RE39356Process for the preparation of epothilone analogs
The present invention relates to a process for the preparation of epothilone analogs by initially forming novel ring-opened epothilones and carrying out a macrolactamization reaction thereon. The subject process is amenable to being carried out in a single reaction ...
10/17/2006
RE39251Polymorphs of an epothilone analog
There are provided in accordance with the present invention two crystalline polymorphs, designated Form A and Form B, respectively, as well as mixtures thereof, of an epothilone analog represented by the formula Also provided are...
08/29/2006
7053069Pharmaceutical compositions and methods of using C-21 modified epothilone derivatives
Pharmaceutical compositions containing C-21 modified epothilone derivatives, methods for their preparation and dosing regimen for administration of these epothilone compounds are provided. The compositions are stable and readily prepared for administration by dissol...
05/30/2006
7041692Methods of treating factor VIIa-associated conditions with compounds having an amine nucleus
Methods of treating Factor VIIa-associated conditions in a mammal are described, comprising administering to the mammal in need of treatment thereof an effective amount of at least one compound having the formula (I), ...
05/09/2006
7022330Parenteral formulation for epothilone analogs
A process for formulating certain epothilone analogs for parenteral administration is disclosed wherein the analog is dissolved in a mixture of at least 50% by volume tertiary-butanol in water, the mixture is lyophilized, the resulting lyophilized product is package...
04/04/2006
7008936Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases
Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative diseases. ...
03/07/2006
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