Patent classifications
C07D249/18
Heterocyclic compounds for the treatment of arenavirus
The invention relates to compounds of structural formula I ##STR00001## wherein A, D, and E are independently N or C—R.sup.3, G, H, and J are independently N or C, K is N or C—H, L is N, N—R.sup.3 or C—R.sup.3, and A, D, E, G, H, J, K, and L together cannot have more than 4 N, R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl, (C.sub.2 to C.sub.9) heteroaryl, and 5-indolyl, wherein each of the said (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl is substituted with at least one R.sup.4a group, and wherein said (C.sub.2 to C.sub.9) heteroaryl is C-attached, and R.sup.2 is selected from the group consisting of ##STR00002##
Heterocyclic compounds for the treatment of arenavirus
The invention relates to compounds of structural formula I ##STR00001## wherein A, D, and E are independently N or C—R.sup.3, G, H, and J are independently N or C, K is N or C—H, L is N, N—R.sup.3 or C—R.sup.3, and A, D, E, G, H, J, K, and L together cannot have more than 4 N, R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl, (C.sub.2 to C.sub.9) heteroaryl, and 5-indolyl, wherein each of the said (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl is substituted with at least one R.sup.4a group, and wherein said (C.sub.2 to C.sub.9) heteroaryl is C-attached, and R.sup.2 is selected from the group consisting of ##STR00002##
PGDH inhibitors and methods of making and using
Disclosed herein are compounds that can inhibit 15-hydroxyprostaglandin dehydrogenase. Such compounds may be administered to subjects that may benefit from modulation of prostaglandin levels.
INDAZOLES AS LRRK2 INHIBITORS
The present invention is directed to indazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.
SMALL TUNABLE FLUOROPHORES FOR THE DETECTION AND IMAGING OF BIOMOLECULES
The invention relates to small, conjugatable, orthogonal and tunable fluorophores for imaging of small bioactive molecules. The invention further relates to processes for the preparation of the compounds, and uses of the compounds in therapeutic, diagnostic, surgery and analytical applications. The invention provides a compound of formula (I), a derivative or a salt thereof. Wherein X is selected from the group consisting of NH, O, S, SeR5R6, CR7R8; R1 is selected from the group consisting of amines, alcohols, thiols, thiophenols, selenols, selenophenols and aryl groups; R2 and R3 are independently H or a halogen; R4 tis either H, nitro or cyano; R5 is either absent or methyl or oxygen; R6 is either absent or methyl or oxygen; and R7 and R8 are independently selected from the group consisting of linear or cyclic alkyl groups containing halogen, amino, cyano or carboxylic ester substituents, and alkyl aryl groups.
##STR00001##
SMALL TUNABLE FLUOROPHORES FOR THE DETECTION AND IMAGING OF BIOMOLECULES
The invention relates to small, conjugatable, orthogonal and tunable fluorophores for imaging of small bioactive molecules. The invention further relates to processes for the preparation of the compounds, and uses of the compounds in therapeutic, diagnostic, surgery and analytical applications. The invention provides a compound of formula (I), a derivative or a salt thereof. Wherein X is selected from the group consisting of NH, O, S, SeR5R6, CR7R8; R1 is selected from the group consisting of amines, alcohols, thiols, thiophenols, selenols, selenophenols and aryl groups; R2 and R3 are independently H or a halogen; R4 tis either H, nitro or cyano; R5 is either absent or methyl or oxygen; R6 is either absent or methyl or oxygen; and R7 and R8 are independently selected from the group consisting of linear or cyclic alkyl groups containing halogen, amino, cyano or carboxylic ester substituents, and alkyl aryl groups.
##STR00001##
Compounds and their methods of use
The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
Compounds and their methods of use
The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
STRUCTURE OF ADJUSTABLE STERIC HINDRANCE WEAK BASIC LIGHT STABILIZER AND PREPARATION METHOD AND APPLICATION THEREOF
The field of new compounds and synthesis methods thereof are related, and particularly to a structure of a steric hindrance adjustable weak base light stabilizer and a preparation method and application thereof. According to the innovative light stabilizer, a steric hindrance thereof is adjusted by establishing substituent generating the steric hindrance around nitrogen atoms; moreover, an electronegativity of the nitrogen atom can be influenced by adjusting a distance of a polar group, so that an alkalinity or a nucleophilicity of the nitrogen atom is adjusted. A desired effect is obtained by adjusting a steric hindrance and a nucleophilic property or an alkalinity where the nitrogen atom is located, so that an application range of the innovative light stabilizer is widened, and the innovative light stabilizer is suitable for PC, polyester, PVC and other slightly acidic or certain electrophilic polymer materials to serve as a light stability protecting aid.
STRUCTURE OF ADJUSTABLE STERIC HINDRANCE WEAK BASIC LIGHT STABILIZER AND PREPARATION METHOD AND APPLICATION THEREOF
The field of new compounds and synthesis methods thereof are related, and particularly to a structure of a steric hindrance adjustable weak base light stabilizer and a preparation method and application thereof. According to the innovative light stabilizer, a steric hindrance thereof is adjusted by establishing substituent generating the steric hindrance around nitrogen atoms; moreover, an electronegativity of the nitrogen atom can be influenced by adjusting a distance of a polar group, so that an alkalinity or a nucleophilicity of the nitrogen atom is adjusted. A desired effect is obtained by adjusting a steric hindrance and a nucleophilic property or an alkalinity where the nitrogen atom is located, so that an application range of the innovative light stabilizer is widened, and the innovative light stabilizer is suitable for PC, polyester, PVC and other slightly acidic or certain electrophilic polymer materials to serve as a light stability protecting aid.