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US 2025/0101013 A1Published application
Functionalized aminothiazoles
AssigneeLeadxpro AG
InventorsWerner NEIDHART, Denis BUCHER
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AssigneeLeadxpro AG
InventorsWerner NEIDHART, Denis BUCHER
Estimating the term…
The present invention relates to novel antagonists of the A2B adenosine receptor and pharmaceutical compositions comprising said antagonists as well as their uses for the treatment and prevention of disorders known to be susceptible to improvement by antagonism of the A2B receptor such as asthma, chronic obstructive pulmonary disorder (COPD), pulmonary fibrosis, vascular diseases, allergic diseases, hypertension, retinopathy, diabetes mellitus, inflammatory gastrointestinal tract disorders, inflammatory diseases, autoimmune diseases, renal diseases, neurological disorders and, in particular, cancers. In particular, the present invention relates to compounds of Formula (I) wherein: R1 is H, halogen, —C1-C8 alkyl, —C3-C8 cycloalkyl, —O—C1-C8 alkyl, or —CN, wherein each alkyl, cycloalkyl, or —O-alkyl is optionally substituted with one or more R2; R2 is independently, at each occurrence, selected from halogen, —OH, and —OC1-C8 alkyl; RA is a 5- to 6-membered heteroaryl, wherein said heteroaryl is optionally substituted with one or more RA1; RA1 is independently, at each occurrence, selected from halogen, —OH, oxo, cyano, —C1-C8 alkyl, —C3-C8 cycloalkyl, and —O—C1-C8 alkyl, wherein each alkyl, cycloalkyl, or —O-alkyl is optionally substituted with one or more RA2; RA2 is independently, at each occurrence, halogen, —OC1-C8 alkyl, or —OH; RB is phenyl or a 5- to 6-membered heteroaryl, wherein each phenyl or heteroaryl is optionally substituted with one or more RB1; and RB1 is independently, at each occurrence, selected from halogen, —OH, cyano, —C1-C8alkyl, and —O—C1-C8 alkyl, wherein each alkyl and —O-alkyl is optionally substituted with one or more RB2; and RB2 is independently, at each occurrence, halogen, —OH, or —OC1-C8 alkyl; or a pharmaceutically acceptable salt, solvate, or hydrate thereof.
A compound of Formula I:
The compound of any of the preceding claims, wherein RA is imidazolyl, triazolyl, isoxazolyl, oxazolyl, pyrazolyl, pyridinyl, pyridazinyl, pyrimidinyl, or pyrazinyl;
The compound of any of the preceding claims, wherein RA1 is independently halogen, —OH, —C1-C4 alkyl, or —C3-C6 cycloalkyl, wherein each alkyl or cycloalkyl is optionally substituted with one or more halogen or —OH.
The compound of any of the preceding claims, wherein RA is selected from:
The compound of any of the preceding claims, wherein RB is selected from phenyl, oxazolyl, pyridinyl, pyrimidinyl, pyridazinyl, and pyrazinyl, wherein each phenyl, oxazolyl, pyridinyl, pyrimidinyl, pyridazinyl, and pyrazinyl is optionally substituted by one or more RB1.
The compound of any of the preceding claims, wherein RB1 is selected from halogen, —OH, cyano, —C1-C4 alkyl, and —C1-C4 alkoxy, wherein each alkyl and alkoxy is independently substituted with one or more halogen, —OH, or —OC1-C4 alkoxy.
The compound of any of the preceding claims, wherein RB is selected from:
The compound of any of the preceding claims, wherein RB is phenyl substituted with one or two RB1, wherein RB1 is independently, at each occurrence, cyano or fluoro.
The compound of any of the preceding claims, wherein the compound is of the Formula Ia3b or Ia2b:
The compound of any of the preceding claims, wherein the compound is of the Formula Ia1b1, Ia1b2, Ia1b3, Ia2b1, Ia2b2, Ia2b3, Ia3b1, Ia3b2, or Ia3b3:
A pharmaceutical composition comprising a compound according to any of the preceding claims and a pharmaceutically acceptable diluent or carrier.
Dependencies are inferred from the claim text.