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US 12,006,316 B2Granted
9H-pyrrolo-dipyridine derivatives
AssigneeUcb Biopharma Srl
InventorsJoel Mercier, Laurent Provins, Celine Vermeiren, Yogesh Anil Sabnis
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Abstract
The invention relates to 9H-pyrrolo-dipyridine derivatives of formula I, processes for preparing them, pharmaceutical compositions containing them and their use as radiopharmaceuticals in particular as imaging agents for the detection of Tau aggregates.
Claims4
A compound of general formula I-A, or a pharmaceutically acceptable acid addition salt, a racemic mixture or its corresponding enantiomer and/or optical isomers thereof,
- wherein
- R1 is pyrazole, thiazole, pyridine, or pyrimidine each of which is optionally substituted by one or two substituents independently selected from (1) fluorine;
- (2) methyl, ethyl or propyl, each of which is optionally substituted by fluorine or methoxy;
- (3) cyano;
- (4) amino optionally substituted by methyl or fluoro-ethyl;
- (5) —C(O)NHR1A where R1A is methyl, ethyl, or propyl, each of which is optionally substituted by fluorine or methoxy;
- (6) methoxy, ethoxy or propoxy, each of which is optionally substituted by fluorine or methoxy;
- or (7) morpholine, piperazine or piperidine, each of which is optionally substituted by fluorine or fluoromethyl;
- M is C—R3, and Q is CH;
- or M is CH, and Q is CR3;
- R3 is (1) H;
- (2) fluorine;
- (3) methyl, ethyl or propyl, each of which is optionally substituted by fluorine, hydroxy or methoxy;
- (4) methoxy, ethoxy or propoxy, each of which is optionally substituted by fluorine, hydroxyl or methoxy;
- (4) di-methyl-amino;
- or (5) —NHR3A where R3A is methyl, ethyl or propyl, each of which is optionally substituted by fluorine, hydroxy or methoxy;
- and
- wherein
- any hydrogen of formula I-A is H, 2H or 3H;
- any carbon of formula I-A is C, 14C or 11C;
- and
- any fluorine of formula I-A is F or 18F;
- provided that the compound of formula I is not a compound of general formula Ro I
- wherein
- R is hydrogen or tritium;
- F is fluoro or 18fluoro;
- or a pharmaceutically acceptable acid addition salt thereof.
24 more elements
Dependencies are inferred from the claim text.