Patent classifications
C07D271/08
NOVEL SUBSTITUTED N'-HYDROXYCARBAMIMIDOYL-1,2,5-OXADIAZOLE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE IDO INHIBITORS
Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof. Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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Acylated N-(1 ,2,5-oxadiazol-3-yl)-, N-(1,3,4-oxadiazol-2-yl)-, N-(tetrazol-5-yl)- and N-(triazol-5-yl)-aryl carboxamides, and use thereof as herbicides
Acylated N-(1,2,5-oxadiazol-3-yl)-, N-(1,3,4-oxadiazol-2-yl)-, N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of the formula (I) and the use thereof as herbicides are described. ##STR00001## In this formula (I), R, V, X, Y and Z are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is an oxadiazole, triazole or tetrazole radical. W is CY or N.
Acylated N-(1 ,2,5-oxadiazol-3-yl)-, N-(1,3,4-oxadiazol-2-yl)-, N-(tetrazol-5-yl)- and N-(triazol-5-yl)-aryl carboxamides, and use thereof as herbicides
Acylated N-(1,2,5-oxadiazol-3-yl)-, N-(1,3,4-oxadiazol-2-yl)-, N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of the formula (I) and the use thereof as herbicides are described. ##STR00001## In this formula (I), R, V, X, Y and Z are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is an oxadiazole, triazole or tetrazole radical. W is CY or N.
NOVEL SUBSTITUTED SULFOXIMINE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS
Compounds of Formula I, or a pharmaceutically acceptable salt, solvate or hydrate thereof: (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
##STR00001##
NOVEL SUBSTITUTED SULFOXIMINE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS
Compounds of Formula I, or a pharmaceutically acceptable salt, solvate or hydrate thereof: (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
##STR00001##
Compounds as indoleamine 2,3-dioxygenase inhibitors
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. ##STR00001##
Compounds as indoleamine 2,3-dioxygenase inhibitors
Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. ##STR00001##
HETEROCYCLIC UREA COMPOUND, AND DRUG COMPOSITION AND APPLICATION THEREOF
A heterocyclic urea compound, and specifically discloses an indoleamine-2,3-dioxygenase inhibitor of a heterocyclic urea compound, which solves the problems of weak curative effect and larger toxic and side effects of existing immunological therapy drugs. The invention further provides a preparation method for an indoleamine-2,3-dioxygenase inhibitor of a heterocyclic urea compound, and an application of the indoleamine-2,3-dioxygenase inhibitor of a heterocyclic urea compound or a pharmaceutically acceptable salt thereof in preparing drugs for treating or preventing tumors.
OXADIAZOLE INHIBITORS OF HIPK2 FOR TREATING KIDNEY FIBROSIS
Compounds that are selective inhibitors of Smad3 activation are disclosed. The compounds have the following structure:
##STR00001##
in which Z is an oxadiazole. The compounds disclosed are useful in treatment of fibrotic disease, particularly renal fibrosis, and similar diseases associated with the dysregulation of the HIPK2/Smad3 signaling pathway.
14-CHLORO-BETA-ELEMENE NITRIC OXIDE DONOR TYPE DERIVATIVE, PREPARATION AND APPLICATION THEREOF
The disclosure relates to the field of medicinal chemistry. Disclosed are a 14-chloro-?-elemene nitric oxide donor derivative and a preparation method and use thereof in the preparation of anti-tumor drugs. The 14-chloro-?-elemene nitric oxide donor derivative has a general formula shown in formula (I): in formula (I): R.sup.1 represents a linear or cyclic alcohol amine structure containing nitrogen and oxygen atoms; and each of R.sup.2 and R.sup.3 is independently selected from the group consisting of C.sub.1-10 alkyl, C.sub.3-12 cycloalkyl, C.sub.6-12 aryl, 5- to 10-membered cyclic heteroaryl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, and C.sub.2-10 alkoxy. In the disclosure, the derivative is superior to the previous ?-elemene nitric oxide donor derivatives in terms of the design strategy, an alcohol amine structure that can enhance in vivo anti-tumor activity is introduced as a linker, which improves in vivo stability, and provides good therapeutic activity against malignant brain glioma against which effective therapeutic drugs is short in clinical practice.
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