[EN] CARBAZOLE AND CARBOLINE COMPOUNDS FOR USE IN THE DIAGNOSIS, TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH AMYLOID OR AMYOLID-LIKE PROTEINS [FR] COMPOSÉS DE CARBAZOLE ET DE CARBOLINE DESTINÉS À ÊTRE UTILISÉS DANS LE DIAGNOSTIC, LE TRAITEMENT, L'ATTÉNUATION OU LA PRÉVENTION DE TROUBLES ASSOCIÉS AUX PROTÉINES AMYLOÏDES ET DE TYPE AMYLOÏDE
Carbazole and Carboline Compounds for Use in the Diagnosis, Treatment, Alleviation or Prevention of Disorders Associated with Amyloid or Amyloid-Like Proteins
申请人:AC IMMUNE SA
公开号:US20170002005A1
公开(公告)日:2017-01-05
The present invention relates to novel compounds that can be employed in the diagnosis, treatment, alleviation or prevention of a group of disorders and abnormalities associated with amyloid proteins and amyloid-like proteins, such as Alzheimer's disease. Precursors for the preparation of the compounds according to the present invention are also provided.
[EN] ADENOSINE RECEPTOR BINDING COMPOUNDS<br/>[FR] COMPOSÉS SE LIANT AU RÉCEPTEUR DE L'ADÉNOSINE
申请人:NIKANG THERAPEUTICS INC
公开号:WO2020014332A1
公开(公告)日:2020-01-16
The present invention relates to pharmaceutical compounds and compositions of Formula (I) and methods of treatment using the compounds and compositions, especially for the treatment and/or prevention of a proliferation disorder, such as cancer. Compounds of Formula (I) as further described herein are shown modulators of the adenosine A2A receptor and exhibit antiproliferative activity. Accordingly, these compounds are useful to treat proliferative disorders such as cancer, and other adenosine receptor-related conditions including an inflammatory disease, renal disease, diabetes, vascular disease, lung disease, or an autoimmune disease.
[EN] C-ABL TYROSINE KINASE INHIBITORY COMPOUND EMBODIMENTS AND METHODS OF MAKING AND USING THE SAME<br/>[FR] COMPOSÉ INHIBITEUR DE TYROSINE KINASE C-ABL, MODES DE RÉALISATION, PROCÉDÉS DE FABRICATION ET D'UTILISATION ASSOCIÉS
申请人:US HEALTH
公开号:WO2019173761A1
公开(公告)日:2019-09-12
Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as "c-Abl"). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c- Abl inhibitory compound embodiments.
The invention relates to compounds of a general formula (I):
wherein Ar
1
is an optionally-substituted aryl or heteroaromatic group; R
1
is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R
2
is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R
3
is a hydrogen atom or a lower alkyl group; R
4
is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R
1k
)R
1m
; T and U are a nitrogen atom or a methine group, etc.
The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.
The invention relates to compounds of a general formula (I):
wherein Ar
1
is an optionally-substituted aryl or heteroaromatic group; R
1
is an optionally-substituted lower alkyl, lower alkenyl, lower alkynyl or cyclo-lower alkyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R
2
is a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, or is an aryl, aralkyl or heteroaromatic group optionally having a substituent; R
3
is a hydrogen atom or a lower alkyl group; R
4
is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a group of —N(R
1k
)R
1m
; T and U are a nitrogen atom or a methine group, etc.
The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.