Patent classifications
C07D473/00
Substituted pyrrolo[2,3-d]pyrimidines as inhibitors of protein arginine methyl transferase 5 (PRMT5)
The disclosure is directed to compounds of Formula (I) and Formula (II). Formula (I) and Formula (II) and pharmaceutically acceptable salts or solvates thereof. Pharmaceutical compositions comprising compounds of Formula (I) or Formula (II), as well as methods of their use and preparation, are also described. ##STR00001##
CD73 inhibitors and uses thereof
The present disclosure provides compounds of Formula (II) ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, W.sup.1, W.sup.2, W.sup.3, X, Y, and A are as described herein. The disclosed compounds modulate CD73 activity. The present disclosure also provides, pharmaceutical compositions containing these compounds, and methods of using these compounds for treating diseases associated with CD73 activity.
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.
2-(1,1′-biphenyl)-1H-benzodimidazole derivatives and related compounds as apelin and APJ agonists for treating cardiovascular diseases
The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification. The compounds are apelin and APJ agonists for treating cardiovascular diseases. Preferred compounds are 2-(1,1′-biphe-1H-benzo[d]imidazole derivatives. The invention further provides compositions comprising the compounds and the compounds for use in methods of medical treatment. ##STR00001##
2-(1,1′-biphenyl)-1H-benzodimidazole derivatives and related compounds as apelin and APJ agonists for treating cardiovascular diseases
The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification. The compounds are apelin and APJ agonists for treating cardiovascular diseases. Preferred compounds are 2-(1,1′-biphe-1H-benzo[d]imidazole derivatives. The invention further provides compositions comprising the compounds and the compounds for use in methods of medical treatment. ##STR00001##
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.
SUBSTITUTED INDOLE COMPOUNDS
- Alaric J. Dyckman ,
- Dharmpal S. Dodd ,
- Christopher P. Mussari ,
- Trevor C. Sherwood ,
- John L. Gilmore ,
- Tsair Shamsul Haque ,
- Brian K. Whiteley ,
- David R. Tortolani ,
- Shoshana L. Posy ,
- John E. Macor ,
- Louis J. Lombardo ,
- Ramesh Kumar Sistla ,
- Anupama Kandhi Ramachandra Reddy ,
- Subramanya Hegde ,
- Laxman Pasunoori ,
- Sreekantha Ratna Kumar
Disclosed are compounds of Formula (I)
##STR00001##
or salts thereof, wherein Ring Het, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, m, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
Substituted pyrazolopyrimidines and substituted purines and their use as ubiquitin-specific-processing protease 1 (USP1) inhibitors
The present disclosure provides compounds having Formula I: ##STR00001##
and the pharmaceutically acceptable salts and solvates thereof, wherein X.sup.1, X.sup.2, X.sup.11, X.sup.12, R.sup.1, R.sup.3, R.sup.5, R.sup.5′, R.sup.6, and R.sup.7 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to inhibit a USP1 protein and/or to treat a disorder responsive to the inhibition of USP1 proteins and USP1 activity. Compounds of the present disclosure are especially useful for treating cancer.
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##