13-08-2020 дата публикации
Номер: US20200255478A1
Автор:
Albericio Palomera Fernando,
BRUN CUBERO Omar,
Davis Andrew,
FIACCO Stephen,
GESCHWINDNER Stefan,
Gongora Benitez Miriam,
HERAS PANIAGUA Carlos,
MIRET CASALS Laia,
PARADIS BAS Marta,
Puig Duran Carlos,
RAMOS TOMILLERO Ivan,
TRALLERO CANELA Nuria
Принадлежит:
The invention relates to peptidic compounds, which peptidic compounds are compounds of formula (I)′, or a pharmaceutically acceptable salt, or solvate, or N-oxide, or stereoisomer thereof: 3. The peptidic compound according to claim 1 , wherein Aais chosen from a direct bond claim 1 , a leucine claim 1 , a valine claim 1 , a lysine claim 1 , a proline claim 1 , a 4-aminoproline claim 1 , and a 4-acetaminoproline residue claim 1 , wherein (a) when Aais other than a direct bond it is optionally linked to Aa; and/or (b) when Aais leucine claim 1 , the leucine residue is optionally alkylated with a methyl group on the N at the peptidic bond.4. The peptidic compound according to claim 1 , wherein Aais chosen from a direct bond claim 1 , a glutamine claim 1 , a leucine claim 1 , a lysine claim 1 , and a valine residue.5. The peptidic compound according to claim 1 , wherein claim 1 , when m is 1 and n is 1 claim 1 , Lis a —C(O)—(CH)-NH— group.6. The peptidic compound according to claim 1 , wherein Tag claim 1 , is chosen from a —C(O)—(CH)—CHgroup claim 1 , a —C(O)—(CH)-((E-CH═CH)—CH)—(CH)—CHgroup claim 1 , a —C(O)—(CH)—((Z—CH═CH)—CH)—(CH)—CHgroup claim 1 , and a —C(O)—(CH)—((Z—CH═CH)—CH)—CHgroup claim 1 , wherein when Aais a 4-aminoproline residue and m is 0 claim 1 , the Taggroup is linked to Aathrough the 4-amino substituent of the 4-aminoproline residue; and r is 6 to 20.7. The peptidic compound according to claim 6 , wherein Tagis a —C(O)—(CH)—CHgroup claim 6 , wherein when Aais a 4-aminoproline residue and m is 0 claim 6 , the Taggroup is linked to Aathrough the 4-amino substituent of the 4-aminoproline residue; and r is 6 to 20.8. The peptidic compound according to claim 1 , wherein in -Aa-Aa-[L]-[Tag]:{'sub': 74', '74', '85', '74, 'Aais chosen from a direct bond, a leucine, a valine, a lysine, a proline, a 4-aminoproline, and a 4-acetaminoproline residue, wherein (a) when Aais other than a direct bond it is optionally linked to Aa; and/or (b) when Aais leucine, the ...
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