Patent classifications
C07C229/18
Prodrugs of fumarates and their use in treating various diseases
The present invention provides compounds of formula (I), wherein: ##STR00001## R.sub.1 is unsubstituted C.sub.1-C.sub.6 alkyl; L.sub.a is substituted or unsubstituted C.sub.1-C.sub.6 alkyl linker, substituted or unsubstituted C.sub.3-C.sub.10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R.sub.2 and R.sub.3 are each, independently, H, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or substituted or unsubstituted C.sub.6-C.sub.10aryl; or alternatively, R.sub.2 and R.sub.3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S. The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.
Prodrugs of fumarates and their use in treating various diseases
The present invention provides compounds of formula (I), wherein: ##STR00001## R.sub.1 is unsubstituted C.sub.1-C.sub.6 alkyl; L.sub.a is substituted or unsubstituted C.sub.1-C.sub.6 alkyl linker, substituted or unsubstituted C.sub.3-C.sub.10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R.sub.2 and R.sub.3 are each, independently, H, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or substituted or unsubstituted C.sub.6-C.sub.10aryl; or alternatively, R.sub.2 and R.sub.3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S. The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.
Aminated lignin-derived compounds and uses thereof
The present invention relates to novel lignin-derived compounds and compositions comprising the same and their use as redox flow battery electrolytes. The invention further provides a method for preparing said compounds and compositions as well as a redox flow battery comprising said compounds and compositions. Additionally, an assembly for carrying out the inventive method is provided.
COMPOSITION AND METHODS FOR MEASURING ION CHANNEL ACTIVITY IN A CELL
Compositions and methods for detecting the activity of an ion channel in a cell are described. The methods include providing a loading buffer solution to the cell, where the loading buffer includes a thallium ion indicator and optionally chloride ions, and providing a stimulus buffer that includes thallium ions to the cell. Providing the stimulus buffer can cause thallium ion influx into or efflux out of the cell through the ion channel. After providing the stimulus buffer, a change in at least one optical property of the thallium ion indicator is detected in response to thallium influx or efflux, thereby detecting the activity of the ion channel.
MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same.
MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF
The present invention provides compounds, compositions thereof, and methods of using the same.
Prodrugs of fumarates and their use in treating various diseases
The present invention provides compounds of formula (I), ##STR00001##
wherein: R.sub.1 is unsubstituted C.sub.1-C.sub.6 alkyl; L.sub.a is substituted or unsubstituted C.sub.1-C.sub.6 alkyl linker, substituted or unsubstituted C.sub.3-C.sub.10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R.sub.2 and R.sub.3 are each, independently, H, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or substituted or unsubstituted C.sub.6-C.sub.10 aryl; or alternatively, R.sub.2 and R.sub.3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S. The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.
Prodrugs of fumarates and their use in treating various diseases
The present invention provides compounds of formula (I), ##STR00001##
wherein: R.sub.1 is unsubstituted C.sub.1-C.sub.6 alkyl; L.sub.a is substituted or unsubstituted C.sub.1-C.sub.6 alkyl linker, substituted or unsubstituted C.sub.3-C.sub.10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R.sub.2 and R.sub.3 are each, independently, H, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or substituted or unsubstituted C.sub.6-C.sub.10 aryl; or alternatively, R.sub.2 and R.sub.3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S. The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.
Chiral N-substituted allylic amine compounds
The method relates to the field of asymmetric allylic amination and comprises preparing a chiral N-substituted allylic amine compound from the corresponding allylic substrates and substituted hydroxylamines, in the presence of a catalyst, said catalyst comprising copper compounds and a chiral ligand. Examples of chiral amine compounds which can be made using the method include Vigabatrin, Ezetimibe Terbinafine, Naftifine 3-methylmorphine, Sertraline, Cinacalcet, Mefloquine hydrochloride, and Rivastigmine. There are over 20,000 known bioactive molecules with chiral N-substituted allylic amine substructure. The method may also be used to produce non-natural chiral -aminoacid esters, a sub-class of chiral N-substituted allylic amine compounds. Examples of -aminoacid ester which can be produced by the disclosed method, include, but are not limited to, N-(2-methylpent-1-en-3-yl)benzenamine and Ethyl 2-methylene-3-(phenylamino)butanoate. Further, the products of the method described herein can be used to produce chiral heterocycles and bioactive molecules or materials. A novel chiral copper-ligand nitrosoarene complex is also set forth.
Chiral N-substituted allylic amine compounds
The method relates to the field of asymmetric allylic amination and comprises preparing a chiral N-substituted allylic amine compound from the corresponding allylic substrates and substituted hydroxylamines, in the presence of a catalyst, said catalyst comprising copper compounds and a chiral ligand. Examples of chiral amine compounds which can be made using the method include Vigabatrin, Ezetimibe Terbinafine, Naftifine 3-methylmorphine, Sertraline, Cinacalcet, Mefloquine hydrochloride, and Rivastigmine. There are over 20,000 known bioactive molecules with chiral N-substituted allylic amine substructure. The method may also be used to produce non-natural chiral -aminoacid esters, a sub-class of chiral N-substituted allylic amine compounds. Examples of -aminoacid ester which can be produced by the disclosed method, include, but are not limited to, N-(2-methylpent-1-en-3-yl)benzenamine and Ethyl 2-methylene-3-(phenylamino)butanoate. Further, the products of the method described herein can be used to produce chiral heterocycles and bioactive molecules or materials. A novel chiral copper-ligand nitrosoarene complex is also set forth.