Patent application number | Description | Published |
20090054665 | ANALOGS OF SALINOSPORAMIDE A - Disclosed herein are analogs of Salinosporamide A, having the Formula I as follows: | 02-26-2009 |
20090093640 | SYNTHESIS OF ENONE INTERMEDIATE - The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate. | 04-09-2009 |
20090143581 | SYNTHESIS OF AVRAINVILLAMIDE, STREPHACIDIN B, AND ANALOGUES THEREOF - The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The α,β-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores. The compounds of the invention may be used in the treatment of diseases such as cancer, autoimmune diseases, and bacterial infection. | 06-04-2009 |
20100130451 | SYNTHESIS OF TETRACYCLINES AND ANALOGUES THEREOF - The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetra-cycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-pro liferative agents in the treatment of diseases of humans or other animals. | 05-27-2010 |
20110009371 | SYNTHESIS OF TETRACYCLINES AND ANALOGUES THEREOF - The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals. | 01-13-2011 |
20110009639 | SYNTHESIS OF ENONE INTERMEDIATE - The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate. | 01-13-2011 |
20110105515 | TARGETING THE ONCOPROTEIN NUCLEOPHOSMIN - (+)-Avrainvillamide, a naturally occurring alkaloid with antiproliferative activity, is shown to bind to the oncoprotein nucleophosmin. Nucleophosmin is known to regulate the tumor suppressor protein p53 and is overexpressed in many different human tumors. The invention provides methods of modulating nucleophosmin and p53 using (+)-avrainvillamide and analogues thereof. These compounds may provide leads for the development of novel anti-cancer therapies that target nucleophosmin. | 05-05-2011 |
20110166170 | SYNTHESIS OF AVRAINVILLAMIDE, STEPHACIDIN B, AND ANALOGUES THEREOF - The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The α,β-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores. The compounds of the invention may be used in the treatment of diseases such as cancer, autoimmune diseases, and bacterial infection. | 07-07-2011 |
20110190323 | CORTISTATIN ANALOGUES AND SYNTHESES THEREOF - The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: I and salts thereof, wherein R | 08-04-2011 |
20120029199 | SYNTHESIS OF ENONE INTERMEDIATE - The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate. | 02-02-2012 |
20120115818 | SYNTHESIS OF TETRACYCLINES AND INTERMEDIATES THERETO - Efficient method for preparing the enone intermediate (VII) used in the synthesis of tetracyclines derivatives. In particular, the invention provides a synthesis which allows for substituents at positions 4 | 05-10-2012 |
20130150314 | TRIOXACARCINS AND USES THEREOF - The present invention relates to trioxacarcin compounds of the formula: (I) or pharmaceutically acceptable forms thereof; wherein R | 06-13-2013 |
20130217886 | SYNTHESIS OF ENONE INTERMEDIATE - The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate. | 08-22-2013 |
20140163238 | SYNTHESIS OF TETRACYCLINES AND ANALOGUES THEREOF - The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals. | 06-12-2014 |
20140179929 | SYNTHESIS OF ENONE INTERMEDIATE - The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate. | 06-26-2014 |
20150111921 | CORTISTATIN ANALOGUES AND SYNTHESES THEROF - The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: I and salts thereof, wherein R | 04-23-2015 |
20150297747 | TRIOXACARCINS, TRIOXACARCIN-ANTIBODY CONJUGATES, AND USES THEREOF - Provided herein are trioxacarcin-antibody drug conjugates of Formula (A): and pharmaceutically acceptable salts thereof, comprising at least one instance of the group -L | 10-22-2015 |
20150376201 | CORTISTATIN ANALOGUES AND SYNTHESES THEREOF - The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: | 12-31-2015 |
20160002183 | SYNTHESIS OF TETRACYCLINES AND INTERMEDIATES THERETO - The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system. | 01-07-2016 |
20160052951 | MACROLIDES AND METHODS OF THEIR PREPARATION AND USE - Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided. | 02-25-2016 |
Patent application number | Description | Published |
20160055170 | SHARING RESOURCES AMONG REMOTE REPOSITORIES UTILIZING A LOCK FILE IN A SHARED FILE SYSTEM OR A NODE GRAPH IN A PEER-TO-PEER SYSTEM - A method, system and computer program product for sharing resources among remote repositories. In a shared file system, a resource identifier and metadata are created for a resource, where the resource identifier is stored in a lock file in a shared volume accessible by the remote repositories. The lock file is then released in response to distributing the associated resource to the remote repositories. Alternatively, in a peer-to-peer system, a request is received to create, read, update or delete a resource stored in a content repository. A resource name, a resource version and/or a resource fingerprint are received in connection with the request to create, read, update or delete the resource in the content repository. A determination is then made as to whether the received resource name, resource version and/or resource fingerprint matches the respective resource name, resource version and/or resource fingerprint stored in a node graph for the resource. | 02-25-2016 |
20160055241 | SHARING RESOURCES AMONG REMOTE REPOSITORIES UTILIZING A LOCK FILE IN A SHARED FILE SYSTEM OR A NODE GRAPH IN A PEER-TO-PEER SYSTEM - A method, system and computer program product for sharing resources among remote repositories. In a shared file system, a resource identifier and metadata are created for a resource, where the resource identifier is stored in a lock file in a shared volume accessible by the remote repositories. The lock file is then released in response to distributing the associated resource to the remote repositories. Alternatively, in a peer-to-peer system, a request is received to create, read, update or delete a resource stored in a content repository. A resource name, a resource version and/or a resource fingerprint are received in connection with the request to create, read, update or delete the resource in the content repository. A determination is then made as to whether the received resource name, resource version and/or resource fingerprint matches the respective resource name, resource version and/or resource fingerprint stored in a node graph for the resource. | 02-25-2016 |
Patent application number | Description | Published |
20100062487 | Novel genes encoding proteins having prognostic, diagnostic, preventive, therapeutic, and other uses - The invention provides isolated nucleic acids encoding a variety of proteins having diagnostic, preventive, therapeutic, and other uses. These nucleic and proteins are useful for diagnosis, prevention, and therapy of a number of human and other animal disorders. The invention also provides antisense nucleic acid molecules, expression vectors containing the nucleic acid molecules of the invention, host cells into which the expression vectors have been introduced, and non-human transgenic animals in which a nucleic acid molecule of the invention has been introduced or disrupted. The invention still further provides isolated polypeptides, fusion polypeptides, antigenic peptides and antibodies. Diagnostic, screening, and therapeutic methods using compositions of the invention are also provided. The nucleic acids and polypeptides of the present invention are useful as modulating agents in regulating a variety of cellular processes. | 03-11-2010 |
20120045777 | NOVEL GENES ENCODING PROTEINS HAVING PROGNOSTIC, DIAGNOSTIC, PREVENTIVE, THERAPEUTIC, AND OTHER USES - The invention provides isolated nucleic acids encoding a variety of proteins having diagnostic, preventive, therapeutic, and other uses. These nucleic and proteins are useful for diagnosis, prevention, and therapy of a number of human and other animal disorders. The invention also provides antisense nucleic acid molecules, expression vectors containing the nucleic acid molecules of the invention, host cells into which the expression vectors have been introduced, and non-human transgenic animals in which a nucleic acid molecule of the invention has been introduced or disrupted. The invention still further provides isolated polypeptides, fusion polypeptides, antigenic peptides and antibodies. Diagnostic, screening, and therapeutic methods using compositions of the invention are also provided. The nucleic acids and polypeptides of the present invention are useful as modulating agents in regulating a variety of cellular processes. | 02-23-2012 |
Patent application number | Description | Published |
20080213778 | Novel genes encoding proteins having prognostic, diagnostic, preventive, therapeutic, and other uses - The invention provides isolated TANGO 239, TANGO 219, TANGO 232, TANGO 281, A236 (INTERCEPT 236), TANGO 300, TANGO 353, TANGO 393, TANGO 402, TANGO 351 and TANGO 509 nucleic acid molecules and polypeptide molecules. The invention also provides antisense nucleic acid molecules, expression vectors containing the nucleic acid molecules of the invention, host cells into which the expression vectors have been introduced, and non-human transgenic animals in which a nucleic acid molecule of the invention has been introduced or disrupted. The invention still further provides isolated polypeptides, fusion polypeptides, antigenic peptides and antibodies. Diagnostic, screening and therapeutic methods utilizing compositions of the invention are also provided. | 09-04-2008 |
20090136959 | Novel genes encoding proteins having prognostic, diagnostic preventive, therapeutic, and other uses - The invention provides isolated nucleic acids encoding a variety of proteins having diagnostic, preventive, therapeutic, and other uses. These nucleic and proteins are useful for diagnosis, prevention, and therapy of a number of human and other animal disorders. The invention also provides antisense nucleic acid molecules, expression vectors containing the nucleic acid molecules of the invention, host cells into which the expression vectors have been introduced, and non-human transgenic animals in which a nucleic acid molecule of the invention has been introduced or disrupted. The invention still further provides isolated polypeptides, fusion polypeptides, antigenic peptides and antibodies. Diagnostic, screening, and therapeutic methods using compositions of the invention are also provided. The nucleic acids and polypeptides of the present invention are useful as modulating agents in regulating a variety of cellular processes. | 05-28-2009 |
20110065124 | Novel genes encoding proteins having prognostic, diagnostic, preventive, therapeutic, and other uses - The invention provides isolated TANGO 239, TANGO 219, TANGO 232, TANGO 281, A236 (INTERCEPT 236), TANGO 300, TANGO 353, TANGO 393, TANGO 402, TANGO 351 and TANGO 509 nucleic acid molecules and polypeptide molecules. The invention also provides antisense nucleic acid molecules, expression vectors containing the nucleic acid molecules of the invention, host cells into which the expression vectors have been introduced, and non-human transgenic animals in which a nucleic acid molecule of the invention has been introduced or disrupted. The invention still further provides isolated polypeptides, fusion polypeptides, antigenic peptides and antibodies. Diagnostic, screening and therapeutic methods utilizing compositions of the invention are also provided. | 03-17-2011 |
20120270219 | NOVEL GENES ENCODING PROTEINS HAVING PROGNOSTIC, DIAGNOSTIC, PREVENTIVE, THERAPEUTIC, AND OTHER USES - The invention provides isolated TANGO 509 nucleic acid molecules and polypeptide molecules. The invention also provides antisense nucleic acid molecules, expression vectors containing the nucleic acid molecules of the invention, host cells into which the expression vectors have been introduced, and non-human transgenic animals in which a nucleic acid molecule of the invention has been introduced or disrupted. The invention still further provides isolated polypeptides, fusion polypeptides, antigenic peptides and antibodies. Diagnostic, screening and therapeutic methods utilizing compositions of the invention are also provided. | 10-25-2012 |
20140072968 | Novel Genes Encoding Proteins Having Prognostic, Diagnostic, Preventive, Therapeutic, and Other Uses - The invention provides isolated TANGO 509 nucleic acid molecules and polypeptide molecules. The invention also provides antisense nucleic acid molecules, expression vectors containing the nucleic acid molecules of the invention, host cells into which the expression vectors have been introduced, and non-human transgenic animals in which a nucleic acid molecule of the invention has been introduced or disrupted. The invention still further provides isolated polypeptides, fusion polypeptides, antigenic peptides and antibodies. Diagnostic, screening and therapeutic methods utilizing compositions of the invention are also provided. | 03-13-2014 |