Patent classifications
C07D221/20
HEPATITIS B ANTIVIRAL AGENTS
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:
X-A-Y-Z-R (I)
which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
HEPATITIS B ANTIVIRAL AGENTS
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:
X-A-Y-Z-R (I)
which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Compounds and methods for the targeted degradation of androgen receptor
The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.
Compounds and methods for the targeted degradation of androgen receptor
The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.
POLYCYCLIC COMPOUND AND ORGANIC ELETROLUMINESCENCE DEVICE INCLUDING THE SAME
A polycyclic compound according to an embodiment of the inventive concept is represented by the following Formula 1:
##STR00001##
In Formula 1, Ar.sub.1 and Ar.sub.2 are each independently substituted or unsubstituted aryl group having 6 to 30 carbon atoms for forming a ring, or substituted or unsubstituted heteroaryl group having 2 to 30 carbon atoms for forming a ring, where Ar.sub.1 and Ar.sub.2 may combine with each other to form a ring, and A is represented by the following Formula 2-1 or 2-2:
##STR00002##
POLYCYCLIC COMPOUND AND ORGANIC ELETROLUMINESCENCE DEVICE INCLUDING THE SAME
A polycyclic compound according to an embodiment of the inventive concept is represented by the following Formula 1:
##STR00001##
In Formula 1, Ar.sub.1 and Ar.sub.2 are each independently substituted or unsubstituted aryl group having 6 to 30 carbon atoms for forming a ring, or substituted or unsubstituted heteroaryl group having 2 to 30 carbon atoms for forming a ring, where Ar.sub.1 and Ar.sub.2 may combine with each other to form a ring, and A is represented by the following Formula 2-1 or 2-2:
##STR00002##
ORGANIC ELECTROLUMINESCENT MATERIAL AND ORGANIC OPTOELECTRONIC DEVICE
A compound and an organic optoelectronic device are provided. The compound has the chemical formula (I):
##STR00001##
In the chemical formula (I): Ar is selected from N-substituted or unsubstituted C.sub.6 to C.sub.30 aryl; m denotes a positive integer and 1≦m≦8, n denotes a positive integer and 1≦n≦8, and A.sub.1 is selected from chemical groups of the following chemical formula (II):
##STR00002##
In the chemical formula (II): R1 to R.sub.S are independently selected from hydrogen, deuterium, C.sub.1 to C.sub.30 alkyl, C.sub.1 to C.sub.30 heteroatom-substituted alkyl, C.sub.6 to C.sub.30 aryl, and C.sub.2 to C.sub.30 heteroaryl. X is selected from O, S, substituted or unsubstituted imino, substituted or unsubstituted methylene, and substituted or unsubstituted silylene, and a substituent is selected from hydrogen, deuterium, C.sub.1 to C.sub.30 alkyl, C.sub.1 to C.sub.50 heteroatom-substituted alkyl, C.sub.6 to C30 aryl, and C.sub.2 to C.sub.30 heteroaryl.
ORGANIC ELECTROLUMINESCENT MATERIAL AND ORGANIC OPTOELECTRONIC DEVICE
A compound and an organic optoelectronic device are provided. The compound has the chemical formula (I):
##STR00001##
In the chemical formula (I): Ar is selected from N-substituted or unsubstituted C.sub.6 to C.sub.30 aryl; m denotes a positive integer and 1≦m≦8, n denotes a positive integer and 1≦n≦8, and A.sub.1 is selected from chemical groups of the following chemical formula (II):
##STR00002##
In the chemical formula (II): R1 to R.sub.S are independently selected from hydrogen, deuterium, C.sub.1 to C.sub.30 alkyl, C.sub.1 to C.sub.30 heteroatom-substituted alkyl, C.sub.6 to C.sub.30 aryl, and C.sub.2 to C.sub.30 heteroaryl. X is selected from O, S, substituted or unsubstituted imino, substituted or unsubstituted methylene, and substituted or unsubstituted silylene, and a substituent is selected from hydrogen, deuterium, C.sub.1 to C.sub.30 alkyl, C.sub.1 to C.sub.50 heteroatom-substituted alkyl, C.sub.6 to C30 aryl, and C.sub.2 to C.sub.30 heteroaryl.
Piperidinone Derivatives as MDM2 Inhibitors for the Treatment of Cancer
- Michael D. Bartberger ,
- Ana Gonzalez Buenrostro ,
- Hilary Plake Beck ,
- Xiaoqi Chen ,
- Richard Victor Connors ,
- Jeffrey Deignan ,
- Jason A. Dequette, I ,
- John Eksterowicz ,
- Benjamin Fisher ,
- Brian M. Fox ,
- Jiasheng Fu ,
- Zice Fu ,
- Felix Gonzalez Lopez De Turiso ,
- Michael W. Gribble ,
- Darin J. Gustin ,
- Julie A. Heath ,
- Xin Huang ,
- XianYun Jiao ,
- Michael G. Johnson ,
- Frank Kayser ,
- David John Kopecky ,
- SuJen Lai ,
- Yihong Li ,
- Zhihong Li ,
- Jiwen Liu ,
- Jonathan D. Low ,
- Brian S. Lucas ,
- Zhihua Ma ,
- Lawrence R. McGee ,
- Josel McIntosh ,
- Dustin L. McMinn ,
- Julio C. Medina ,
- Jeffrey Thomas Mihalic ,
- Steven H. Olson ,
- Yossup Rew ,
- Philip M. Roveto ,
- Daqing Sun ,
- Xiaodong Wang ,
- Yingcai Wang ,
- Xuelei Yan ,
- Ming Yu ,
- Jiang Zhu
The present invention provides MDM2 inhibitor compounds of Formula I,
##STR00001##
wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
Piperidinone Derivatives as MDM2 Inhibitors for the Treatment of Cancer
- Michael D. Bartberger ,
- Ana Gonzalez Buenrostro ,
- Hilary Plake Beck ,
- Xiaoqi Chen ,
- Richard Victor Connors ,
- Jeffrey Deignan ,
- Jason A. Dequette, I ,
- John Eksterowicz ,
- Benjamin Fisher ,
- Brian M. Fox ,
- Jiasheng Fu ,
- Zice Fu ,
- Felix Gonzalez Lopez De Turiso ,
- Michael W. Gribble ,
- Darin J. Gustin ,
- Julie A. Heath ,
- Xin Huang ,
- XianYun Jiao ,
- Michael G. Johnson ,
- Frank Kayser ,
- David John Kopecky ,
- SuJen Lai ,
- Yihong Li ,
- Zhihong Li ,
- Jiwen Liu ,
- Jonathan D. Low ,
- Brian S. Lucas ,
- Zhihua Ma ,
- Lawrence R. McGee ,
- Josel McIntosh ,
- Dustin L. McMinn ,
- Julio C. Medina ,
- Jeffrey Thomas Mihalic ,
- Steven H. Olson ,
- Yossup Rew ,
- Philip M. Roveto ,
- Daqing Sun ,
- Xiaodong Wang ,
- Yingcai Wang ,
- Xuelei Yan ,
- Ming Yu ,
- Jiang Zhu
The present invention provides MDM2 inhibitor compounds of Formula I,
##STR00001##
wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.