Patent classifications
C07C225/06
PROCESS OF PRODUCING CYCLOALKYLCARBOXAMIDO-INDOLE COMPOUNDS
The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)N(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), useful for treating CFTR mediated diseases such as cystic fibrosis.
PROCESS OF PRODUCING CYCLOALKYLCARBOXAMIDO-INDOLE COMPOUNDS
The present invention features processes for preparing compounds, such as (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)N(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), useful for treating CFTR mediated diseases such as cystic fibrosis.
Versatile non-destructive surface modification of carbonaceous materials and process for grafting into polymer matrices
Disclosed is a non-destructive universal method of functionalization of graphitic carbonaceous materials that enables their alignment, cross-linking, and effective integration into composite materials.
Versatile non-destructive surface modification of carbonaceous materials and process for grafting into polymer matrices
Disclosed is a non-destructive universal method of functionalization of graphitic carbonaceous materials that enables their alignment, cross-linking, and effective integration into composite materials.
METHOD FOR PRODUCING KAKEROMYCIN AND DERIVATIVES THEREOF
Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1):
##STR00001##
wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2):
##STR00002##
wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.
METHOD FOR PRODUCING KAKEROMYCIN AND DERIVATIVES THEREOF
Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1):
##STR00001##
wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2):
##STR00002##
wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.
PEPTIDE NUCLEIC ACID (PNA) MONOMERS WITH AN ORTHOGONALLY PROTECTED ESTER MOIETY AND NOVEL INTERMEDIATES AND METHODS RELATED THERETO
The present disclosure pertains to peptide nucleic acid (PNA) monomers and oligomers, as well as methods and compositions useful for the preparation of PNA monomer precursors (e.g. PNA Monomer Esters, Backbone Esters and Backbone Ester Acid Salts, as described below) that can be used to prepare PNA monomers wherein said PNA monomers can be used to prepare said PNA oligomers. In some embodiments, the disclosure features sulfonic acid salts of Backbone Ester compounds, which sulfonic acid salts generally tend to be crystalline and can be obtained in reasonably good yield, often without requiring any chromatographic purification of the reaction product of the Backbone Ester synthesis reaction. This disclosure also pertains to novel methods for the synthesis of said Backbone Ester compounds and novel methods for the formation of the related sulfonic acid salts. Exemplary ester groups include, but are not limited to, 2,2,2-trichloroethy-(TCE), 2,2,2-tribromoethyl-(TBE), 2-iodoethyl-groups (2-IE) and 2-bromoethyl-(2-BrE) as the ester group. These particular ester groups can be removed under conditions where both Boc and Fmoc protected amine groups are stable.
PEPTIDE NUCLEIC ACID (PNA) MONOMERS WITH AN ORTHOGONALLY PROTECTED ESTER MOIETY AND NOVEL INTERMEDIATES AND METHODS RELATED THERETO
The present disclosure pertains to peptide nucleic acid (PNA) monomers and oligomers, as well as methods and compositions useful for the preparation of PNA monomer precursors (e.g. PNA Monomer Esters, Backbone Esters and Backbone Ester Acid Salts, as described below) that can be used to prepare PNA monomers wherein said PNA monomers can be used to prepare said PNA oligomers. In some embodiments, the disclosure features sulfonic acid salts of Backbone Ester compounds, which sulfonic acid salts generally tend to be crystalline and can be obtained in reasonably good yield, often without requiring any chromatographic purification of the reaction product of the Backbone Ester synthesis reaction. This disclosure also pertains to novel methods for the synthesis of said Backbone Ester compounds and novel methods for the formation of the related sulfonic acid salts. Exemplary ester groups include, but are not limited to, 2,2,2-trichloroethy-(TCE), 2,2,2-tribromoethyl-(TBE), 2-iodoethyl-groups (2-IE) and 2-bromoethyl-(2-BrE) as the ester group. These particular ester groups can be removed under conditions where both Boc and Fmoc protected amine groups are stable.
Styrenyl derivative compounds for treating ophthalmic diseases and disorders
The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
Styrenyl derivative compounds for treating ophthalmic diseases and disorders
The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.