C07D513/18

Macrocyclic compounds as IRAK4 inhibitors for the treatment of inflammatory diseases
09617282 · 2017-04-11 · ·

Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein i.a. Ring A is phenylene or 5- to 6-membered heteroarylene; Ring B is phenylene, 5- to 6-membered heterocycloalkylene or 5- to 6-membered heteroarylen; R.sup.4 is absent, heteroarylene, arylene, C1-3 alkylene, or R.sup.4 and R.sup.3 taken together with the nitrogen to which they are bound form a 3- to 7-membered heterocycloalkyl ring; R.sup.5 is absent, C(O)NR.sup.51, NR.sup.52 or O; R.sup.6 is C2-10 alkylene or alkenylene, wherein one or two of the carbon atoms in the alkylene chain is optionally replaced by an O, S, SO, SO.sub.2 or NR.sup.61, and wherein two of the carbon atoms in the alkylene chain are optionally connected by a two or three carbon atom alkylene chain to form a 5- to 7-membered ring; R.sup.7 is absent, NR.sup.71 or O. The compounds are IRAK4 inhibitors useful for the treatment of inflammatory diseases. ##STR00001##

Macrocyclic salt-inducible kinase inhibitors

The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of SIK kinase, more in particular SIK1, SIK2 and/or SIK3 and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of SIK-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent.

Macrocyclic salt-inducible kinase inhibitors

The present invention relates to macrocyclic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of SIK kinase, more in particular SIK1, SIK2 and/or SIK3 and/or mutants thereof, for use in the diagnosis, prevention and/or treatment of SIK-kinase associated diseases. Moreover, the present invention provides methods of using said compounds, for instance as a medicine or diagnostic agent.

ETP DERIVATIVES

Provided herein, inter alia, is the synthesis of ETP derivatives. The uses of the ETP derivatives described herein include treatment of cancer.

ETP DERIVATIVES

Provided herein, inter alia, is the synthesis of ETP derivatives. The uses of the ETP derivatives described herein include treatment of cancer.

MCL1 INHIBITORS

The present disclosure generally relates to compounds of Formula (I) and pharmaceutical compositions that may be used in methods of treating cancer.

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MCL1 INHIBITORS

The present disclosure generally relates to compounds of Formula (I) and pharmaceutical compositions that may be used in methods of treating cancer.

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Antiviral pyrazolopiridinone compounds

The invention provides compounds of Formula (I) ##STR00001##
as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.

COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR MEDICAL USE FOR THE TREATMENT OR PREVENTION OF VASCULAR DISEASES

The present disclosure provides compounds capable of exhibiting effects similar to those of 2-Cys-peroxyredoxin (2-Cys-Prx) in the body with excellent pharmacological effects and reduced side effects such as reduced cytotoxicity, and pharmaceutical uses thereof. The compounds of the present disclosure and their pharmaceutically acceptable salts are useful for the treatment or prevention of vascular diseases, particularly ischemic coronary artery disease, arteriosclerosis, vascular restenosis, or pulmonary arterial hypertension. The compounds of the present invention and their pharmaceutically acceptable salts are particularly useful for the treatment or prevention of pulmonary arterial hypertension. The invention also provides methods of preparing the compounds of the present disclosure.

COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR MEDICAL USE FOR THE TREATMENT OR PREVENTION OF VASCULAR DISEASES

The present disclosure provides compounds capable of exhibiting effects similar to those of 2-Cys-peroxyredoxin (2-Cys-Prx) in the body with excellent pharmacological effects and reduced side effects such as reduced cytotoxicity, and pharmaceutical uses thereof. The compounds of the present disclosure and their pharmaceutically acceptable salts are useful for the treatment or prevention of vascular diseases, particularly ischemic coronary artery disease, arteriosclerosis, vascular restenosis, or pulmonary arterial hypertension. The compounds of the present invention and their pharmaceutically acceptable salts are particularly useful for the treatment or prevention of pulmonary arterial hypertension. The invention also provides methods of preparing the compounds of the present disclosure.