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7622578 |
Scalable process for the preparation of a rapamycin 42-ester from a rapamycin 42-ester boronate
A scalable process for the preparation of a rapamycin 42-ester by reacting a rapamycin 42-ester boronate with a diol and purifying crude rapamycin 42-ester by recrystallization and treatment with a...
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7622477 |
Isomers and 42-epimers of rapamycin alkyl ether analogs, methods of making and using the same
Isomers and 42-epimers of rapamycin alkyl ether analogs and pharmaceutically acceptable salts or prodrugs thereof, are immunomodulatory agents and are useful in the treatment of restenosis and...
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7612199 |
Polymorphic forms α, β, and γ of rifaximin
Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal...
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7608613 |
Analogs of benzoquinone-containing ansamycins and methods of use thereof
The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present...
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7605258 |
Processes for the synthesis of individual isomers of mono-peg CCI-779
Processes for preparing individual diastereomers of mono-pegylated rapamycin 42 ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) are provided.
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7605257 |
Processes for preparing water-soluble polyethylene glycol conjugates of macrolide immunosuppressants
Processes are described for preparing 42-pegylated rapamycins including reacting a rapamycin with an acylating agent in the presence of a lipase to form an acylated rapamycin and reacting the...
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7598375 |
Method of acylating maytansinol with chiral amino acids
This invention provides a method for making maytansinoids having a chiral amino acid side chain, such as DM1 and DM4 that are used to treat cancer. According to this method, the side chain may be...
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7592331 |
Macrocyclic factor VIIa inhibitors useful as anticoagulants
The present invention relates generally to novel macrocycles of Formula (I):
or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables...
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7589100 |
Non-hygroscopic and powdery amorphous pimecrolimus
An amorphous pimecrolimus and processes for providing an amorphous pimecrolimus are provided.
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7579337 |
Analogs of benzoquinone-containing ansamycins and methods of use thereof
The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present...
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7572804 |
Macrolides
A mixture comprising a poly-ene macrolide and an antioxidant. Preferably, the poly-ene macrolide is rapamycin and the antioxidant is 2,6-di-tert.-butyl-4-methylphenol. The presence of the...
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7560457 |
Rapamycin analogues and the uses thereof in the treatment of neurological, proliferative, and inflammatory disorders
The present invention provides compounds of the following structure, wherein R 1 , R 2 , R 4 , R 4′ , R 6 , R 7 , and R 15 are defined above:
These compounds are useful in treating...
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7553843 |
Process for the preparation of purified crystalline CCI-779
The present invention provides purified crystalline CCI-779 and processes for preparing the same.
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7553842 |
Macrocyclic analogs for the treatment of immunoregulatory disorders and respiratory diseases
Disclosed are compounds of the Formula I
and diastereomers, tautomers, solvates, metabolites, and pharmaceutically acceptable salts thereof, wherein X, A, L and Y are as defined herein. Such...
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7538119 |
41-Methoxy isotope labeled rapamycin 42-ester
41-methoxy-labeled rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) compounds are provided, along with methods for the synthesis and use thereof.
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7521458 |
Spiropiperidylrifamycins for the treatment of mycobacterial infections
The compounds of formula (1), their pharmaceutically acceptable salts and their solvates, wherein R 1 is a radical selected between hydrogen and alkyl; R 2 is selected from hydroxyalkyl, phenyl,...
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7514554 |
Heteroatoms-containing tricyclic compounds
A process for the production of 33-Epi-33-chloro-FR 520 in one step from FR520 wherein protecting groups are avoided.
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7485706 |
Neurodegenerative protein aggregation inhibition methods and compounds
Methods and compositions are provided for reducing aggregation of neurodegenerative proteins associated with neurotoxicity or other proteins. The compounds comprise a first domain or targeting...
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7473796 |
Cytotoxic agents comprising new maytansinoids
New thiol and disulfide-containing maytansinoids bearing a mono or di-alkyl substitution on the α-carbon atom bearing the sulfur atom are disclosed. Also disclosed are methods for the synthesis of...
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7473366 |
Process for the purification of macrolides
The invention relates to a process for the recovery of a macrolide in substantial pure form including:
a) treating an impure or crude macrolide with water immiscible solvent to form a mixture, b)...
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7465718 |
Ansamycins having improved pharmacological and biological properties
Ansamycins and methods of preparing and using the same are described. At least some of these ansamycins exhibit one or more of improved aqueous formulation ability, chemical stability, and...
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7446111 |
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...
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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...
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7439252 |
Ascomycin crystalline forms and preparation thereof
The present invention provides novel crystalline forms of ascomycin as well as processes for the preparation thereof and pharmaceutical compositions comprising such crystalline forms of ascomycin.
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7432277 |
Phosphorus-containing macrocycles
This invention concerns a new family of phosphorus-containing macrocycles containing various phosphonate- and phosphonate-containing moieties.
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7411063 |
Process for preparation of maytansinol
The present invention describes the preparation of maytansinol by methods that minimize processing steps, and reduce solvent volumes, making the process more efficient, and scaleable. This process...
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7393952 |
Solvent free amorphous rapamycin
An improved process for coating implantable medical devices utilizes a number of techniques for improving the stability of therapeutic agents contained within the coating. The stability of the...
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7390895 |
Production of polyketides and other natural products
The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. One important area is the isolation and potential...
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7384953 |
Purification of rapamycin
Purified rapamycin and a chemical process for obtaining the purified rapamycin are described.
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7375218 |
Process for preparing macrocyclic HCV protease inhibitors
Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection:
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7371853 |
Macrocyclic β-secretase inhibitors for the treatment of Alzheimer's disease
The present invention is directed to compounds of formula (I)
which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the...
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7345069 |
Oxidative activation and episulfonium ion-mediated DNA alkylation-based anticancer
The present invention relates to TG-25 and/or analogs thereof and their use of TG-25 in the treatment of cancer. TG-25 inhibits the growth of prostate cells by inhibiting DNA synthesis, more...
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7345053 |
Nitrosated and nitrosylated rapamycin compounds, compositions and methods of use
The invention describes novel nitrosated and/or nitrosylated rapamycin compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated rapamycin compound, and, optionally,...
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7338974 |
Macrocyclic diaminopropanes as beta-secretase inhibitors
There is provided a series of novel macrocyclic diaminopropanes of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof,
wherein R 1 , R 2 , R 4 , R 5 , n, L, Z, and as...
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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...
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7320974 |
Cytoskeletal active compounds, compositions and use
The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical...
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7301019 |
Method for the preparation of maytansinoid esters
Improved processes for the preparation and purification of maytansinoid esters, especially thiol and disulfide-containing maytansinoids are described. In one aspect the process comprises a process...
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7288647 |
Recovery of CCI-779 from mother liquors
The invention provides a process for recovering CCI-779 from mother liquors.
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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...
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7279571 |
Methods of preparing pimecrolimus
The present invention provides a process for the preparation of pimecrolimus from ascomycin in which ascomycin is reacted with a conversion reagent that converts ascomycin to its activated...
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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...
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7265107 |
Rifamycin C-11 oxime cyclo derivatives effective against drug-resistant microbes
The current invention relates to a series of rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms, specifically, the 3,4-cyclo-rifamycin...
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7256286 |
Bryostatin analogues, synthetic methods and uses
Biologically active compounds related to the bryostatin family of compounds, having simplified spacer domains and/or improved recognition domains are disclosed, including methods of preparing and...
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7256187 |
Rifamycin C-11 oxime derivatives effective against drug-resistant microbes
The invention relates to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms, specifically, the rifamycin derivatives having an oxime...
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7253160 |
Depeptidized inhibitors of hepatitis C virus NS3 protease
The present invention discloses novel depeptidized compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them...
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7250413 |
C-25 carbamate rifamycin derivatives with activity against drug-resistant microbes
Compounds of the current invention relate to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. More specifically, compounds of the...
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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.
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7247634 |
Rifamycin derivatives effective against drug-resistant microbes
Rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms are claimed in this invention. The inventive rifamycin derivatives are uniquely...
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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...
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7238694 |
Rifamycin imino derivatives effective against drug-resistant microbes
The present invention relates to rifamycin 3-iminomethylenyl (—CH═N—) derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. The claimed...
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