C07F9/6541

NOVEL PYRIMIDINE DERIVATIVE AND USE THEREOF

The present invention relates to a novel pyrimidine derivative and a use thereof. The pyrimidine derivative has excellent MLK3 inhibitory activity and LRRK2 inhibitory activity and thus can be utilized in a pharmaceutical composition for preventing or treating cancers, virus infectious diseases, Parkinson's disease, nonalcoholic fatty liver disease, and tuberculosis.

NOVEL PYRIMIDINE DERIVATIVE AND USE THEREOF

The present invention relates to a novel pyrimidine derivative and a use thereof. The pyrimidine derivative has excellent MLK3 inhibitory activity and LRRK2 inhibitory activity and thus can be utilized in a pharmaceutical composition for preventing or treating cancers, virus infectious diseases, Parkinson's disease, nonalcoholic fatty liver disease, and tuberculosis.

Amine prodrugs of pharmaceutical compounds
11083711 · 2021-08-10 · ·

Disclose are amine prodrugs and methods of synthesis thereof. In particular, the amine prodrug comprises a drug molecule and at least one or more prodrug appendage moieties and the method for synthesis the amine prodrug comprises a step of coupling the drug molecule and at least one or more prodrug appendage moieties. Also disclosed are exemplary riluzole prodrugs and methods of synthesis thereof.

Amine prodrugs of pharmaceutical compounds
11083711 · 2021-08-10 · ·

Disclose are amine prodrugs and methods of synthesis thereof. In particular, the amine prodrug comprises a drug molecule and at least one or more prodrug appendage moieties and the method for synthesis the amine prodrug comprises a step of coupling the drug molecule and at least one or more prodrug appendage moieties. Also disclosed are exemplary riluzole prodrugs and methods of synthesis thereof.

Organic Electronic Device Comprising an Organic Semiconductor Layer

The present invention relates to a compound of formula 1 and an organic electronic device comprising an organic semiconductor layer, wherein at least one organic semiconductor layer comprises a compound of formula (1), wherein L.sup.1 has the formula (2) and L.sup.2 has the formula (3), wherein L.sup.1 and L.sup.2 are bonded at * via a single bond independently to the same or different arylene groups or heteroarylenes group of Ar.sup.1; and wherein X.sup.1, X.sup.2 are independently selected from O, S and Se; Ar.sup.1 is selected from substituted or unsubstituted C.sub.20 to C.sub.52 arylene or C.sub.14 to C.sub.64 heteroarylene, wherein the substituent of the substituted C.sub.20 to C.sub.52 arylene or C.sub.14 to C.sub.64 heteroarylene are independently selected from C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 alkoxy, CN, halogen, OH, C.sub.6 to C.sub.25 aryl and C.sub.2 to C.sub.21 heteroaryl; R.sup.1, R.sup.2 are independently selected from substituted or unsubstituted C.sub.1 to C.sub.16 alkyl, wherein the substituent of substituted C.sub.1 to C.sub.16 alkyl is selected from C.sub.6 to C.sub.18 arylene or C.sub.2 to C.sub.12 heteroarylene; R.sup.3, R.sup.4 are independently selected from substituted or unsubstituted C.sub.1 to C.sub.16 alkyl, substituted or unsubstituted C.sub.6 to C.sub.18 arylene, C.sub.2 to C.sub.20 heteroarylene, wherein the substituent of substituted C.sub.1 to C.sub.16 alkyl, the substituent of the substituted C.sub.6 to C.sub.18 arylene, C.sub.2 to C.sub.20 heteroarylene are independently selected from C.sub.6 to C.sub.18 arylene or C.sub.2 to C.sub.12 heteroarylene; n is selected from 1 to 5, wherein n is an integer number.

Substituted tricyclic heterocyclic compounds

Disclosed are compounds of Formula (I), Formula (II), Formula (III), and Formula (IV) or salts thereof, wherein R.sub.2 is OH or OP(O)(OH).sub.2; and R.sub.1 is defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease. ##STR00001##

Substituted tricyclic heterocyclic compounds

Disclosed are compounds of Formula (I), Formula (II), Formula (III), and Formula (IV) or salts thereof, wherein R.sub.2 is OH or OP(O)(OH).sub.2; and R.sub.1 is defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease. ##STR00001##

AMINE PRODRUGS OF PHARMACEUTICAL COMPOUNDS
20190365721 · 2019-12-05 ·

Disclose are amine prodrugs and methods of synthesis thereof. In particular, the amine prodrug comprises a drug molecule and at least one or more prodrug appendage moieties and the method for synthesis the amine prodrug comprises a step of coupling the drug molecule and at least one or more prodrug appendage moieties. Also disclosed are exemplary riluzole prodrugs and methods of synthesis thereof.

SUBSTITUTED TRICYCLIC HETEROCYCLIC COMPOUNDS

Disclosed are compounds of Formula (I), Formula (II), Formula (III), and Formula (IV) or salts thereof, wherein R.sub.2 is OH or OP(O)(OH).sub.2; and R.sub.1 is defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

##STR00001##

Protein biosensors, cross reactive sensor arrays and methods of use thereof

The present invention is directed to fluorescent protein biosensors based on oligonucleotide cross reactive sensor arrays including a selective and a non-selective protein surface binding domain for protein detection. Interaction of different protein isoforms with the sensors of this invention yields a unique optical signature for each protein. The unique optical signature allows differentiating between closely related protein isoforms and diagnosing diseases and disorders associated with the proteins also in biofluids.