C07D211/92

Gut barrier dysfunction treatment and prevention

Methods are disclosed for treating and preventing gut barrier dysfunction or an illness associated with gut barrier dysfunction in a subject comprising administering to the subject bacterium that produce an indole or an indole metabolite and for identifying compounds and bacteria for use in treatment and prevention of gut barrier dysfunction or an illness associated with gut barrier dysfunction.

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.

Metal amides of cyclic amines

Compounds, and oligomers of the compounds, are synthesized with cyclic amine ligands attached to a metal atom. These compounds are useful for the synthesis of materials containing metals. Examples include pure metals, metal alloys, metal oxides, metal nitrides, metal phosphides, metal sulfides, metal selenides, metal tellurides, metal borides, metal carbides, metal silicides and metal germanides. Techniques for materials synthesis include vapor deposition (chemical vapor deposition and atomic layer deposition), liquid solution methods (sol-gel and precipitation) and solid-state pyrolysis. Suitable applications include electrical interconnects in microelectronics and magnetoresistant layers in magnetic information storage devices. The films have very uniform thickness and high step coverage in narrow holes.

Metal amides of cyclic amines

Compounds, and oligomers of the compounds, are synthesized with cyclic amine ligands attached to a metal atom. These compounds are useful for the synthesis of materials containing metals. Examples include pure metals, metal alloys, metal oxides, metal nitrides, metal phosphides, metal sulfides, metal selenides, metal tellurides, metal borides, metal carbides, metal silicides and metal germanides. Techniques for materials synthesis include vapor deposition (chemical vapor deposition and atomic layer deposition), liquid solution methods (sol-gel and precipitation) and solid-state pyrolysis. Suitable applications include electrical interconnects in microelectronics and magnetoresistant layers in magnetic information storage devices. The films have very uniform thickness and high step coverage in narrow holes.

Charge Generation Layer Comprising a Compound of Formula (I), Organic Electronic Device and Display Device Comprising the Charge Generation Layer as Well as Compounds of Formula (I)

The present invention relates to a charge generation layer comprising a compound of formula (I). The invention further relates to organic electronic devices and display devices comprising the charge generation layer as well as compounds of formula (I).

Charge Generation Layer Comprising a Compound of Formula (I), Organic Electronic Device and Display Device Comprising the Charge Generation Layer as Well as Compounds of Formula (I)

The present invention relates to a charge generation layer comprising a compound of formula (I). The invention further relates to organic electronic devices and display devices comprising the charge generation layer as well as compounds of formula (I).

Mono quaternary ammonium salts and methods for modulating neuronal nicotinic acetylcholine receptors

Provided are monoquaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse, and gastrointestinal tract disorders.

PROCESSES FOR PREPARATION OF AVACOPAN AND INTERMEDIATES THEREOF

The present disclosure encompasses a process for chiral resolution of racemic amines, particularly ethyl 2-(4-((tert-butoxycarbonyl)amino)phenyl)piperidine-3-carboxylate, into its desired isomer, ethyl (2R,3S)-2-(4-((tert-butoxycarbonyl)amino)phenyl)-piperidine-3-carboxylate, which is an intermediate useful in the synthesis of Avacopan.

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.