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US 2018/0002378 A1Published application
CGRP Antagonist Peptides
AssigneeFerring B.V.
InventorsKazimierz WISNIEWSKI, Guangcheng JIANG, Aleksandr K. RABINOVICH, Javier J. SUEIRAS-DIAZ
Life of this patent
Estimating the term…
Abstract
This disclosure relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof: in which m, p, A, Ar1, Ar2, Ar3, R1, R2, and R3 are defined in the specification. The compounds of formula (I) can be used as CGRP antagonists and can be used to treat
Claims18
A compound of formula (I) or a pharmaceutically acceptable salt thereof:
- wherein
- m is 0, 1, 2, 3, 4, or 5;
- p is 0, 1, 2, or 3;
- A is single or double carbon-carbon bond;
- Ar1 is aryl or 5- or 6-membered heteroaryl, each of which is optionally substituted with one or more substituents, each substituent independently being halogen, nitro, C1-C4 alkyl, C1-C4 hydroxyalkyl, ORa, or N(RaRa′), in which each Ra, independently, is H or C1-C4 alkyl and each Ra′, independently, is H or C1-C4 alkyl;
- Ar2 is aryl or 5- or 6-membered heteroaryl, each of which is optionally substituted with one or more substituents, each substituent independently being halogen, cyano, nitro, C1-C4 alkyl, C1-C4 aminoalkyl, C1-C4 hydroxyalkyl, ORb, N(RbRb′), C(O)—N(RbRb′), or NH—C(O)—N(RbRb′), in which each Rb, independently, is H or C1-C4 alkyl and each Rb′, independently, is H or C1-C4 alkyl;
- Ar3 is aryl or 5- or 6-membered heteroaryl, each of which is optionally substituted with one or more substituents, each substituent independently being halogen, C1-C4 alkyl, C1-C4 hydroxyalkyl, ORc, or N(RcRc′), in which each Rc, independently, is H or C1-C4 alkyl and each Rc′, independently, is H or C1-C4 alkyl;
- each R1, independently, is C1-C4 alkyl, C1-C4 aminoalkyl, C1-C4 hydroxyalkyl, ORd, or C(O)—N(RdRd′), in which each Rd, independently, is H or C1-C4 alkyl and each Rd′, independently, is H or C1-C4 alkyl;
- R2 is —(CH2)n—R, in which n is 0, 1, 2, or 3 and R is substituted or unsubstituted guanidino, aminoacyl, C1-C4 alkylaminoacyl, ORe, N(ReRe′), NH—C(O)—CH(NH2)—(CH2)4—N(ReRe′), NH—C(O)—CH2—(OCH2CH2)2—N(ReRe′), or 5-membered heterocycloalkyl optionally substituted with C1-C4 alkyl or N(ReRe′), in which each Re, independently, is H or C1-C4 alkyl and each Re′, independently, is H or C1-C4 alkyl;
- and
- each R3, independently, is halogen, C1-C4 alkyl, or ORf, in which each Rf, independently, is H or C1-C4 alkyl;
- with the provisos that, when n is 0, R is not amino or guanidino and that, when the amino acid residue bonded to Ar1C(O) is L-Val, Ar1 is not unsubstituted phenyl.
9 more elements
18-19. (canceled)
Dependencies are inferred from the claim text.