Patent classifications
C07D487/14
NOVEL MACROCYCLIC SPIROPYRROLIDINE DERIVED ANTIVIRAL AGENTS
The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof:
##STR00001##
which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.
Synthesis of echinocandin antifungal agent
The present invention relates to echinocandin cyclopeptides and to methods for preparing echinocandin cyclopeptides.
BIFUNCTIONAL DEGRADERS AND THEIR METHODS OF USE
Described herein are bifunctional degrader compounds, their various targets, their preparation, pharmaceutical compositions comprising them, and their use in the treatment of conditions, diseases, and disorders mediated by various target proteins.
1,4-DIHYDROBENZO[D]PYRAZOLO[3,4-F][1,3]DIAZEPINE DERIVATIVES AND RELATED COMPOUNDS AS LRRK2, NUAK1 AND/OR TYK2 KINASE MODULATORS FOR THE TREATMENT OF E.G. AUTOIMMUNE DISEASE
The present invention relates to compounds of formula (I) that are capable of modulating, e.g., inhibiting or activating, one or more kinases, especially LRRK2 and/or NUAK1 and/or TYK2 or mutants thereof. The compounds are useful for treating diseases, such as autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, Alzheimer's disease, Parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 40 to 146; examples 1 to 63; compounds 1 to 248; tables 1 to 3). Preferred compounds are e.g. 1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds. An exemplary compound is e.g. 5-(2,6-difluorophenyl)-8-methoxy-1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine (example 49). (Formula (II):
##STR00001##
1,4-DIHYDROBENZO[D]PYRAZOLO[3,4-F][1,3]DIAZEPINE DERIVATIVES AND RELATED COMPOUNDS AS LRRK2, NUAK1 AND/OR TYK2 KINASE MODULATORS FOR THE TREATMENT OF E.G. AUTOIMMUNE DISEASE
The present invention relates to compounds of formula (I) that are capable of modulating, e.g., inhibiting or activating, one or more kinases, especially LRRK2 and/or NUAK1 and/or TYK2 or mutants thereof. The compounds are useful for treating diseases, such as autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, Alzheimer's disease, Parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 40 to 146; examples 1 to 63; compounds 1 to 248; tables 1 to 3). Preferred compounds are e.g. 1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds. An exemplary compound is e.g. 5-(2,6-difluorophenyl)-8-methoxy-1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine (example 49). (Formula (II):
##STR00001##
ORGANIC ELECTROLUMINESCENT ELEMENT AND ELECTRONIC APPLIANCE
An organic electroluminescence device includes an anode, a cathode, and an emitting layer disposed between the anode and the cathode. The emitting layer comprises a delayed fluorescent compound M2 having at least one deuterium atom and a compound M3 having at least one deuterium atom. A singlet energy S.sub.1(M2) of the compound M2 and a singlet energy S.sub.1(M3) of the compound M3 satisfy the relationship S.sub.1(M3)>S.sub.1(M2).
ORGANIC ELECTROLUMINESCENT ELEMENT AND ELECTRONIC APPLIANCE
An organic electroluminescence device includes an anode, a cathode, and an emitting layer disposed between the anode and the cathode. The emitting layer comprises a delayed fluorescent compound M2 having at least one deuterium atom and a compound M3 having at least one deuterium atom. A singlet energy S.sub.1(M2) of the compound M2 and a singlet energy S.sub.1(M3) of the compound M3 satisfy the relationship S.sub.1(M3)>S.sub.1(M2).
CONDENSED HETEROCYCLES AS BCL-2 INHIBITORS
The disclosure includes compounds of Formula (A) wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, and R.sub.11, h, j, m, n, k, v, s, g, V, W, L, Z.sub.1, Q.sub.1, Q.sub.2, Q.sub.3, Q.sub.4, Q.sub.5, Q.sub.6, and Q.sub.7, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.
##STR00001##
CONDENSED HETEROCYCLES AS BCL-2 INHIBITORS
The disclosure includes compounds of Formula (A) wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, and R.sub.11, h, j, m, n, k, v, s, g, V, W, L, Z.sub.1, Q.sub.1, Q.sub.2, Q.sub.3, Q.sub.4, Q.sub.5, Q.sub.6, and Q.sub.7, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.
##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.