Patent classifications
C07D475/00
Polycyclic amines as sigma receptor modulators
The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.
Polycyclic amines as sigma receptor modulators
The present invention provides a genus of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.
PYRIDAZINOL COMPOUND, DERIVATIVE THEREOF, PREPARATION METHOD THEREFOR, HERBICIDAL COMPOSITION AND USE THEREOF
The present invention belongs to the technical field of pesticides, and in particular relates to a pyridazinol compound, a derivative thereof, a preparation method therefor, a herbicidal composition and the use thereof. The pyridazinol compound is as represented by general formula I,
##STR00001##
wherein X represents
##STR00002##
and the ring is an unsubstituted or substituted aryl or unsubstituted or substituted heterocyclyl containing a carbon atom at the 1-position; Y represents haloalkyl; and Z represents halogen, cyano, hydroxy, etc. The derivative refers to an agriculturally acceptable derivative of the hydroxyl group at the 4-position of the pyridazine ring in the general formula I, including a salt, an ester, an oxime, a hydroxylamine and an ether derivative, etc. The compound, the derivative thereof and the composition thereof have good herbicidal activity and crop safety.
FGFR4 INHIBITOR, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
Provided are an FGFR4 inhibitor having the structure of formula (1), and a preparation method therefor and the use thereof. The compound has a very strong inhibitory effect on FGFR4 kinase activity and has a very high selectivity, and can be widely used in the preparation of a drug for treating cancers, especially prostate cancer, liver cancer, pancreatic cancer, esophageal carcinomas, gastric cancer, lung cancer, breast cancer, ovarian carcinomas, colon cancer, skin cancer, glioblastomas or rhabdomyosarcomas, and is expected to be developed into a new generation of FGFR4 inhibitor drugs.
##STR00001##
FGFR4 INHIBITOR, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
Provided are an FGFR4 inhibitor having the structure of formula (1), and a preparation method therefor and the use thereof. The compound has a very strong inhibitory effect on FGFR4 kinase activity and has a very high selectivity, and can be widely used in the preparation of a drug for treating cancers, especially prostate cancer, liver cancer, pancreatic cancer, esophageal carcinomas, gastric cancer, lung cancer, breast cancer, ovarian carcinomas, colon cancer, skin cancer, glioblastomas or rhabdomyosarcomas, and is expected to be developed into a new generation of FGFR4 inhibitor drugs.
##STR00001##
4-PYRIDINYL FORMAMIDE COMPOUND OR DERIVATIVE THEREOF, PREPARATION METHOD THEREFOR, HERBICIDAL COMPOSITION AND USE THEREOF
The invention belongs to the technical field of pesticides, and specifically relates to a 4-pyridinyl formamide compound or a derivative thereof, a preparation method therefor, a herbicidal composition and the use thereof. The 4-pyridinyl formamide compound is as represented by formula (I), wherein, X and Y each independently represent nitro, halogen, cyano, formyl, thiocyano, mercapto, etc.; and M represents an unsubstituted or substituted structure (II). The compound, and the derivative and the composition thereof have excellent herbicidal activity and a higher crop safety, and establish good selectivity, especially for key crops such as wheat and rice.
##STR00001##
Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2”). ##STR00001## This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
PYRIDAZINOL COMPOUNDS AND DERIVATIVES, PREPARATION METHODS, HERBICIDAL COMPOSITIONS AND APPLICATIONS THEREOF
The invention belongs to the technical field of agricultural chemicals, and in particular relates to a pyridazinol compound represented by the Formula I, a derivative, preparation method, herbicidal composition and use thereof. The compound, derivative and herbicidal composition thereof have very high herbicidal activity and selectivity, and are safe for crops,
##STR00001##
PIKFYVE KINASE INHIBITORS
The present invention relates to compounds useful as inhibitors of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) as well as their use for treating diseases and disorders associated with PIKfyve.
COMPOUNDS AS CDK2/4/6 INHIBITORS
Provided are certain CDK2/4/6 inhibitors, pharmaceutical compositions thereof, and methods of use thereof.