[EN] AMINOPYRAZINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES<br/>[FR] COMPOSÉS AMINOPYRAZINES AYANT DES PROPRIÉTÉS ANTAGONISTES DE L'A2A
申请人:MERCK SHARP & DOHME
公开号:WO2016081290A1
公开(公告)日:2016-05-26
Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein "R1", "RA-1", "R2", "R3", and "Het" are defined herein above, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.
Pyrimidine derivatives useful as inhibitors of PKC-theta
申请人:Barbosa J.M. Antonio
公开号:US20060025433A1
公开(公告)日:2006-02-02
Disclosed are novel compounds of formula (I):
wherein X, Y, R
1
, R
2
and R
3
are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
The subject matter described herein is directed to Ferroportin inhibitor compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis.
PYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF PKC-THETA
申请人:BARBOSA Antonio J.M.
公开号:US20080287410A1
公开(公告)日:2008-11-20
Disclosed are novel compounds of formula (I):
wherein X, Y, R
1
, R
2
and R
3
are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
BIPHENYL DERIVATIVE INHIBITOR, PREPARATION METHOD THEREFOR AND USE THEREOF
申请人:Shanghai Hansoh Biomedical Co., Ltd.
公开号:EP4086253A1
公开(公告)日:2022-11-09
A biphenyl derivative inhibitor represented by general formula (Ib) and use in the preparation of medicaments for treating cancer, infectious diseases, and autoimmune diseases.