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Class 540/462 - Oxirane ring is one of the cyclos in the polycyclo ring system (e.g., maytansinol, etc.)


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein one of the cyclos of the polycyclo ring
No. of patents: 56
Last issue date: 10/07/2008


1    
NumberTitleIssue Date
7432088Methods for the production of ansamitocins
A process of the large-scale fermentation of a highly productive ansamitocin-producing strains. A method for isolating crude ansamitocins. A method for purifying ansamitocins. ...
10/07/2008
7375217Analogs 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 invention provides analogs of benzoquinone-containing ansamycins where...
05/20/2008
7361647Analogs 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 invention provides analogs of benzoquinone-containing ansamycins where...
04/22/2008
7317100Epothilone derivatives
The present invention relates to C4-demethyl-epothilones or C4-bisnor-epothilones of Formula (I), their pharmaceutical use, pharmaceutical composition containing the same and methods for their preparation. ...
01/08/2008
7282493Analogs 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 invention provides analogs of benzoquinone-containing ansamycins where...
10/16/2007
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
7192750Mutant strain with increased maytansinoid production
A microorganism that is a mutant bacterial strain of the species Actinosynnema pretiosum, designated PF4-4, (ATCC PTA-3921), being capable of producing maytansinoid ansamitocins such as ansamitocin P-3 in improved yield compared to previous known strains, and...
03/20/2007
7176235Epothilone derivatives and methods for making and using the same
This invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, W, X, Y, and Ar...
02/13/2007
7153879Polymorphs 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 ...
12/26/2006
71258936-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations
This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula I in which R1a, R1b, R2a, R3a, R3b, R4, R...
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
6982276Polymorphs 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 p...
01/03/2006
6965034Synthesis of epothilones, intermediates thereto and analogues thereof
The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates ...
11/15/2005
693010216-halogen-epothilone derivatives, process for their production, and their pharmaceutical use
A compund of formula I, an epothilone derivative, its method of preparation, and use as a pharmaceutical agent in treating malignant tumors ...
08/16/2005
6921769Synthesis of epothilones, intermediates thereto and analogues thereof
The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions com...
07/26/2005
6913748Cross-linkers with high reactivity and solubility and their use in the preparation of conjugates for targeted delivery of small molecule drugs
Disclosed is a method of making conjugates of cell binding agents and small molecule drugs comprising reacting a cell binding agent with a bifunctional cross-linking moiety to thereby provide the cell binding agent with a reactive disulfide group and then reacting t...
07/05/2005
6790954Mutant Actinosynnema pretiosum strain with increased maytansinoid production
A microorganism that is a mutant bacterial strain of the species Actinosynnema pretiosum, designated PF4-4, (ATCC PTA-3921), being capable of producing maytansinoid ansamitocins such as ansamitocin P-3 in improved yield compared to previous known strains, and...
09/14/2004
6716821Cytotoxic agents bearing a reactive polyethylene glycol moiety, cytotoxic conjugates comprising polyethylene glycol linking groups, and methods of making and using the same
Cytotoxic agents bearing a polyethylene glycol (PEG) linking group having a terminal active ester, cytotoxic conjugates comprising one or more cytotoxic agents linked to a cell-binding agent via PEG linking groups, and methods for producing both are disclosed. A the...
04/06/2004
6689802Polymorphs 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 ##STR1## Also provided are methods of formi...
02/10/2004
6656711Fermentative preparation process for and crystal forms of cytostatics
The invention relates to a new process for concentrating epothilones in culture media, a new process for the production of epothilones, a new process for separating epothilones A and B and a new strain obtained by mutagenesis for the production of epothil...
12/02/2003
6605599Epothilone derivatives
The present invention relates to epothilone derivatives, having the following formula ##STR1## in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1 -R7 are as defined herein, method...
08/12/2003
6518421Process 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 singl...
02/11/2003
6489314Epothilone derivatives and methods for making and using the same
The present invention relates to 16-membered macrocyclic compounds. In one aspect of the present invention, compounds of the formula ##STR1## are provided wherein: R1, R2, R3, and R5 are each independently hydrogen, ...
12/03/2002
6441163Methods for preparation of cytotoxic conjugates of maytansinoids and cell binding agents
The present invention discloses a one-step process for the production of cytotoxic conjugates of maytansinoids and cell binding agents. Maytansinoids having a disulfide linker that bears a reactive moiety are linked to cell binding agents, such as antibod...
08/27/2002
5416064Cytotoxic agents comprising maytansinoids and their therapeutic use
A cytotoxic agent comprising one or more maytansinoids linked to a cell binding agent. A therapeutic agent for killing selected cell populations comprising: (a) a cytotoxic amount of one or more maytansinoids linked to a cell binding agent, and (b) a phar...
05/16/1995
5300495Indole antiinsectan metabolites
Sulpinine C, secopenitrem B and 10-oxo-11,33-dihydropenitrem B indole compounds have been isolated from the sclerotia of the fungi Aspergillus sulphureus. Aflatrem B has been isolated from the sclerotia of the fungi Aspergillus flavus, and 14-hydroxypaspa...
04/05/1994
5227396Indole antiinsectan metabolites
Sulpinine C, secopenitrem B and 10-oxo-11,33-dihydropenitrem B indole compounds have been isolated from the sclerotia of the fungi Aspergillus sulphureus. Aflatrem B has been isolated from the sclerotia of the fungi Aspergillus flavus, and 14-hydroxypaspa...
07/13/1993
5208020Cytotoxic agents comprising maytansinoids and their therapeutic use
A cytotoxic agent comprising one or more maytansinoids linked to a cell binding agent. A therapeutic agent for killing selected cell populations comprising: (a) a cytotoxic amount of one or more maytansinoids linked to a cell binding agent, and (b) a phar...
05/04/1993
5130326Sulpinine, secopenitrem B and aflatrem B antiinsectan metabolites
Indole compounds named "sulphinine" and "secopenitrem" have been isolated from the sclerotia of from fungi Aspergillus sulphureus. An indole compound named "aflatrem B" has been isolated from the sclerotia of the fungi Aspergillus flavus. The compounds ar...
07/14/1992
5059618Novel bioactive discodermides and methods of use
A novel lactam discodermide has been isolated from a marine sponge. This compound, and its derivatives, are useful as antifungal and antitumor agents....
10/22/1991
44242199-Thiomaytansinoids and their pharmaceutical compositions and use
This invention relates to 9-thiomaytansinoid compounds represented by the formula ##STR1## wherein R is hydrogen or acyl derived from a carboxylic acid, X is chlorine or hydrogen, Y is hydrogen, lower alkylsulfonyl, or alkyl or aralkyl which are...
01/03/1984
4418064Chemotherapeutically active maytansinoids: treflorine, trenudine, and N-methyltrenudone
A novel group of maytansinoid compounds has been discovered in the seed tissue of Trewia nudiflora. They are represented by the general formula ##STR1## and are uniquely characterized by a 12-membered ring joining C-3 and the amide nitrogen at C-18, ...
11/29/1983
4364866Maytansinoids
Antibiotic C-15003 PHO of the formula: ##STR1## wherein R1 is H, hydroxyl, alkanoyloxy, alkenylcarbonyloxy or arylcarbonyloxy; R2 is H, hydroxyl or alkanoyloxy; R3 is H or alkanoyloxy is produced by introducing a hydr...
12/21/1982
4362663Maytansinoid compound
Antibiotic C-15003 PND of the formula: ##STR1## wherein R is H or alkanoyl containing not more than 5 carbon atoms is produced by contacting a maytansinoid compound with a culture broth, inclusive of a processed matter derived therefrom, of a microor...
12/07/1982
4360462Process for preparing maytansinol
A novel Antibiotic C-15003 is produced by cultivating a microorganism of the genus Nocardia. The Antibiotic C-15003 is useful as an antifungal agent or an antiprotozoan agent....
11/23/1982
4331598Maytansinoids
Novel antibiotic C-15003 PHM, which is produced by cultivating a microorganism belonging to the genus Nocardia and being capable of producing antibiotic C-15003 PHM, and novel C-15003 PHM acylate, which is produced by subjecting C-15003 PHM thus obtained ...
05/25/1982
4322348Maytansinoids
Novel Antibiotic C-15003PND, which has the formula: ##STR1## wherein R represents hydrogen, --CO--CH3, --CO--CH2 --CH3, ##STR2## is produced by cultivating a microorganism of the genus Nocardia. The Antibiotic C-...
03/30/1982
4317821Maytansinoids, their use and pharmaceutical compositions thereof
Novel maytansinoids of the formula: ##STR1## wherein Y is H or Cl, and R is C2-15 alkyl, phenyl-C1-4 alkyl, pyridyl-C1-4 alkyl, imidazolyl-C1-4 alkyl, indolyl-C1-4 alkyl, furyl-C1-4 al...
03/02/1982
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