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DK2986610T3 - Bicykliske heterocykler som fgfr-inhibitorer - Google Patents

Bicykliske heterocykler som fgfr-inhibitorer Download PDF

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DK2986610T3
DK2986610T3 DK14732662.3T DK14732662T DK2986610T3 DK 2986610 T3 DK2986610 T3 DK 2986610T3 DK 14732662 T DK14732662 T DK 14732662T DK 2986610 T3 DK2986610 T3 DK 2986610T3
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nrc6rd6
alkyl
nrc6c
independently selected
cycloalkyl
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DK2986610T5 (da
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Liang Lu
Wenqing Yao
Jincong Zhuo
Meizhong Xu
Ding Quan Qian
Fenglei Zhang
Chunhong He
Yaping Sun
Liangxing Wu
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Incyte Holdings Corp
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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Claims (23)

1. Forbindelse med formel Illa:
Illa eller et farmaceutisk acceptabelt salt deraf, hvor: R2 og R5 er hver uafhængigt valgt fra H, halo, Ci-e alkyl, C2-6 alkenyl, C2-6 alkynyl, Ci-e haloalkyl, cyclopropyl, CN, eller3, SRa, C(0)Rb, C(0)NRcRd, C(0)0Ra, 0C(0)Rb, 0C(0)NRcRd, NRcRd, NRcC(0)Rb, NRcC(0)0Ra, NRcC(0)NRcRd, C( = NRe)Rb, C( = NRe)NRcRd, NRcC( = NRe)NRcRd, NRcS(0)Rb, NRcS(0)2Rb, NRcS(0)2NRcRd, S(0)Rb, S(0)NRcRd, S(0)2Rb, og S(0)2NRcRd; R6 er H, halo, Ci-e alkyl, C2-6 alkenyl, C2-6 alkynyl, Ci-e haloalkyl, Ce-io aryl, C3-10 cycloalkyl, 5-10-leddet heteroaryl, 4-10-leddet heterocycloalkyl, CN, NO2, eller32, SR32, C(0)Rb2, C(0)NRc2Rd2, C(0)0Ra2, 0C(0)Rb2, 0C(0)NRc2Rd2, NRc2Rd2, NRc2C(0)Rb2, NRc2C(0)0Ra2, NRc2C(0)NRc2Rd2, C( = NRe2)Rb2, C(=NRe2)NRc2Rd2, NRc2C(=NRe2)NRc2Rd2, NRc2S(0)Rb2, NRc2S(0)2Rb2, NRc2S(0)2NRc2Rd2, S(0)Rb2, S(0)NRc2Rd2, S(0)2Rb2, eller S(0)2NRc2Rd2; hvor C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, Ce-io aryl, C3-10 cycloalkyl, 5-10-leddet heteroaryl, og 4-10-leddet heterocycloalkyl er hver eventuelt substitueret med 1, 2, 3, 4, eller 5 substituenter uafhængigt valgt fra R6a; hver R6a er uafhængigt valgt fra Cy1, halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, Ci-e haloalkyl, CN, NO2, eller32, SRa2, C(0)Rb2, C(0)NRc2Rd2, C(0)0Ra2, 0C(0)Rb2, 0C(0)NRc2Rd2, C( = NRe2)NRc2Rd2, NRc2C( = NRe2)NRc2Rd2, NRc2Rd2, NRc2C(0)Rb2, NRc2C(0)0Ra2, NRc2C(0)NRc2Rd2, NRc2S(0)Rb2, NRc2S(0)2Rb2, NRc2S(0)2NRc2Rd2, S(0)Rb2, S(0)NRc2Rd2, S(0)2Rb2, og S(0)2NRc2Rd2, hvor Ci-β alkyl, C2-6 alkenyl, og C2-6 alkynyl er hver eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra Cy1, halo, CN, N02, eller32, SRa2, C(0)Rb2, C(0)NRc2Rd2, C(0)0Ra2, 0C(0)Rb2, 0C(0)NRc2Rd2, C( = NRe2)NRc2Rd2, NRc2C( = NRe2)NRc2Rd2, NRc2Rd2, NRc2C(0)Rb2, NRc2C(0)0Ra2, NRc2C(0)NRc2Rd2, NRc2S(0)Rb2, NRc2S(0)2Rb2, NRc2S(0)2NRc2Rd2, S(0)Rb2, S(0)NRc2Rd2, S(0)2Rb2, og S(0)2NRc2Rd2; R7 og R8 er hver uafhængigt valgt fra H, Ci-e alkyl, C2-e alkenyl, C2-e alkynyl, -C(0)RA, S(0)RA, S(0)2RA, Ce-io aryl, C3-10 cycloalkyl, 5-10-leddet heteroaryl, 4-10-leddet heterocycloalkyl, Ce-io aryl-Ci-4 alkyl, C3-10 cycloalkyl-Ci-4 alkyl, (5-10-leddet heteroaryl)-Ci-4 alkyl, og (4-10-leddet heterocycloalkyl)-Ci-4 alkyl, hvor Ci-e alkyl, C2-6 alkenyl, C2-6 alkynyl, Ce-io aryl, C3-10 cycloalkyl, 5-10-leddet heteroaryl, 4-10-leddet heterocycloalkyl, Ce-io aryl-Ci-4 alkyl, C3-10 cycloalkyl-Ci-4 alkyl, (5-10-leddet heteroaryl)-Ci-4 alkyl, og (4-10-leddet heterocycloalkyl)-Ci-4 alkyl er hver eventuelt substitueret med 1, 2, 3, 4, eller 5 substituenter uafhængigt valgt fra R7a; hver R7a er uafhængigt valgt fra Cy2, halo, Ci-e alkyl, C2-e alkenyl, C2-6 alkynyl, Ci-e haloalkyl, CN, N02, eller33, SRa3, C(0)Rb3, C(0)NRc3Rd3, C(0)0Ra3, 0C(0)Rb3, 0C(0)NRc3Rd3, C( = NRe3)NRc3Rd3, NRc3C( = NRe3)NRc3Rd3, NRc3Rd3 , NRc3C(0)Rb3, NRc3C(0)0Ra3, NRc3C(0)NRc3Rd3, NRc3S(0)Rb3, NRc3S(0)2Rb3, NRc3S(0)2NRc3Rd3, S(0)Rb3, S(0)NRc3Rd3, S(0)2Rb3, og S(0)2NRc3Rd3, hvor Ci-e alkyl, C2-6 alkenyl, og C2-6 alkynyl er hver eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra Cy2, halo, CN, N02, eller33, SRa3, C(0)Rb3, C(0)NRc3Rd3, C(0)0Ra3, 0C(0)Rb3, 0C(0)NRc3Rd3, C( = NRe3)NRc3Rd3, NRc3C( = NRe3)NRc3Rd3, NRc3Rd3, NRc3C(0)Rb3, NRc3C(0)0Ra3, NRc3C(0)NRc3Rd3, NRc3S(0)Rb3, NRc3S(0)2Rb3, NRc3S(0)2NRc3Rd3, S(0)Rb3, S(0)NRc3Rd3, S(0)2Rb3, og S(0)2NRc3Rd3; R10 og R11 sammen med det carbonatom til hvilket de er bundet danner en 3-, 4-, 5-, 6-, eller 7-leddet cycloalkylgruppe eller en 4-, 5-, 6-, eller 7-leddet heterocycloalkylgruppe, hver eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra Cy3, C1-6 alkyl, Ci-e haloalkyl, halo, CN, eller34, SRa4, C(0)Rb4, C(0)NRc4Rd4, C(0)0Ra4, 0C(0)Rb4, 0C(0)NRc4Rd4, NRc4Rd4, NRc4C(0)Rb4, NRc4C(0)NRc4Rd4, NRc4C(0)0Ra4, C( = NRe4)NRc4Rd4, NRc4C(=NRe4)NRc4Rd4, S(0)Rb4, S(0)NRc4Rd4, S(0)2Rb4, NRc4S(0)2Rb4, NRc4S(0)2NRc4Rd4, og S(0)2NRc4Rd4, hvor Ci-e alkyl eventuelt er substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra Cy3, halo, CN, eller34, SRa4, C(0)Rb4, C(0)NRc4Rd4, C(0)0Ra4, 0C(0)Rb4, 0C(0)NRc4Rd4, NRc4Rd4, NRc4C(0)Rb4, NRc4C(0)NRc4Rd4, NRc4C(0)0Ra4, C(=NRe4)NRc4Rd4, NRc4C( = NRe4)NRc4Rd4, S(0)Rb4, S(0)NRc4Rd4, S(0)2Rb4, NRc4S(0)2Rb4, NRc4S(0)2NRc4Rd4, og S(0)2NRc4Rd4; hver RA er uafhængigt valgt fra H, Ci-e alkyl, Ci-e alkoxy, Ce-ιο aryl, C3-10 cycloalkyl, 5-10-leddet heteroaryl, 4-10-leddet heterocycloalkyl, Ce-io aryl-C1-4 alkyl, C3-10 cycloalkyl-Ci-4 alkyl, (5-10-leddet heteroaryl)-Ci-4 alkyl, og (4-10-leddet heterocycloalkyl)-Ci-4 alkyl, hvor C1-6 alkyl, C1-6 alkoxy, Ce-ιο aryl, C3-10 cycloalkyl, 5-10-leddet heteroaryl, 4-10-leddet heterocycloalkyl, Ce-io aryl-Ci-4 alkyl, C3-10 cycloalkyl-Ci-4 alkyl, (5-10-leddet heteroaryl)-Ci-4 alkyl, og (4-10-leddet heterocycloalkyl)-Ci-4 alkyl er hver eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra R7a; Cy1, Cy2, og Cy3 er hver uafhængigt valgt fra Ce-io aryl, C3-10 cycloalkyl, 5-10-leddet heteroaryl, og 4-10-leddet heterocycloalkyl, der hver eventuelt er substitueret med 1, 2, 3, 4, eller 5 substituenter uafhængigt valgt fra halo, Ci-6 alkyl, C2-e alkenyl, C2-6 alkynyl, C1-6 haloalkyl, Ce-ιο aryl, C3-10 cycloalkyl, 5-10-leddet heteroaryl, 3-10-leddet heterocycloalkyl, CN, N02, eller35, SRa5, C(0)Rb5, C(0)NRc5Rd5, C(0)0Ra5, 0C(0)Rb5, 0C(0)NRc5Rd5, NRc5Rd5, NRc5C(0)Rb5, NRc5C(0)0Ra5, NRc5C(0)NRc5Rd5, C(=NRe5)Rb5, C( = NRe5)NRc5Rd5, NRc5C( = NRe5)NRc5Rd5, NRc5S(0)Rb5, NRcSS(0)2Rb5, NRc5S(0)2NRc5Rd5, S(0)Rb5, S(0)NRc5Rd5, S(0)2Rb5, og S(0)2NRc5Rd5; hvor Ci-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, Ce-ιο aryl, C3-10 cycloalkyl, 5-10-leddet heteroaryl, og 4-10-leddet heterocycloalkyl er hver eventuelt substitueret med 1, 2, 3, 4, eller 5 substituenter uafhængigt valgt fra halo, Ci-6 alkyl, C2-6 alkenyl, C2-e alkynyl, Ci-e haloalkyl, CN, N02, eller35, SRa5, C(0)Rb5, C(0)NRc5Rd5, C(0)0R35, 0C(0)Rb5, 0C(0)NRc5Rd5, C( = NRe5)NRc5Rd5, NRc5C( = NRe5)NRc5Rd5, NRc5Rd5, NRc5C(0)Rb5, NRc5C(0)0Ra5, NRc5C(0)NRc5Rd5, NRc5S(0)Rb5, NRc5S(0)2Rb5, NRc5S(0)2NRc5Rd5, S(0)Rb5, S(0)NRc5Rd5, S(0)2Rb5, og S(0)2NRc5Rd5; hver Ra, Rb, Rc, og Rd er uafhængigt valgt fra H, Ci-e alkyl, Ci-4 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, og cyclopropyl, hvor C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, og cyclopropyl er eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra C1-4 alkyl, C1-4 haloalkyl, halo, CN, eller36, SRa6, C(0)Rb6, C(0)NRc6Rd6, C(0)0Ra6, 0C(0)Rb6, 0C(0)NRc6Rd6, NRc6Rd6, NRc6C(0)Rb6, NRc6C(0)NRc6Rd6, NRc6C(0)0Ra6, C( = NRe6)NRc6Rd6, NRc6C( = NRe6)NRc6Rd6, S(0)Rb6, S(0)NRc6Rd6, S(0)2Rb6, NRc6S(0)2Rb6, NRc6S(0)2NRc6Rd6, og S(0)2NRc6Rd6; hver Ra2, Rb2, Rc2, Rd2, Ra3, Rb3, Rc3, Rd3, Ra4, Rb4, Rc4, Rd4, Ra5, Rb5, Rc5, og Rd5 er uafhængigt valgt fra H, Ci-e alkyl, C1-4 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, Ce-ιο aryl, C3-10 cycloalkyl, 5-10-leddet heteroaryl, 4-10-leddet heterocycloalkyl, Ce-ιο aryl-Ci-4 alkyl, C3-10 cycloalkyl-Ci-4 alkyl, (5-10-leddet heteroaryl)-Ci-4 alkyl, og (4-10-leddet heterocycloalkyl)-Ci-4 alkyl, hvor Ci-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, Ce-io aryl, C3-10 cycloalkyl, 5-10-leddet heteroaryl, 4-10-leddet heterocycloalkyl, Ce-ιο aryl-Ci-4 alkyl, C3-10 cycloalkyl-Ci-4 alkyl, (5-10-leddet heteroaryl)-Ci-4 alkyl, og (4-10-leddet heterocycloalkyl)-Ci-4 alkyl er eventuelt substitueret med 1, 2, 3, 4, eller 5 substituenter uafhængigt valgt fra C1-4 alkyl, C1-4 haloalkyl, halo, CN, eller36, SRa6, C(0)Rb6, C(0)NRc6Rd6, C(0)0Ra6, 0C(0)Rb6, 0C(0)NRc6Rd6, NRc6Rd6, NRc6C(0)Rb6, NRc6C(0)NRc6Rd6, NRc6C(0)0Ra6, C(=NRe6)NRc6Rd6, NRc6C( = NRe6)NRc6Rd6, S(0)Rb6, S(0)NRc6Rd6, S(0)2Rb6, NRc6S(0)2Rb6, NRc6S(0)2NRc6Rd6, og S(0)2NRc6Rd6; eller hvilken som helst af Rc og Rd sammen med det N-atom til hvilket de er bundet danner en 4-, 5-, 6-, eller 7-leddet heterocycloalkylgruppe eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra Ci-6 alkyl, C3-7 cycloalkyl, 4-7-leddet heterocycloalkyl, Ce-ιο aryl, 5-6-leddet heteroaryl, Ci-6 haloalkyl, halo, CN, eller36, SRa6, C(0)Rb6, C(0)NRc6Rd6, C(0)0Ra6, 0C(0)Rb6, 0C(0)NRc6Rd6, NRc6Rd6, NRc6C(0)Rb6, NRc6C(0)NRc6Rd6, NRc6C(0)0Ra6, C(=NRe6)NRc6Rd6, NRc6C( = NRe6)NRc6Rd6, S(0)Rb6, S(0)NRc6Rd6, S(0)2Rb6, NRc6S(0)2Rb6, NRc6S(0)2NRc6Rd6, og S(0)2NRc6Rd6, hvor Ci-6 alkyl, C3-7 cycloalkyl, 4-7-leddet heterocycloalkyl, Ce-io aryl, og 5-6-leddet heteroaryl er eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra halo, CN, eller36, SRa6, C(0)Rb6, C(0)NRc6Rd6, C(0)0Ra6, 0C(0)Rb6, 0C(0)NRc6Rd6, NRc6Rd6, NRc6C(0)Rb6, NRc6C(0)NRc6Rd6, NRc6C(0)0Ra6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(0)Rb6, S(0)NRc6Rd6, S(0)2Rb6, NRc6S(0)2Rb6, NRc6S(0)2NRc6Rd6, og S(0)2NRc6Rd6; eller hvilken som helst af Rc2 og Rd2 sammen med det N-atom til hvilket de er bundet danner en 4-, 5-, 6-, eller 7-leddet heterocycloalkylgruppe eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra Ci-6 alkyl, C3-7 cycloalkyl, 4-7-leddet heterocycloalkyl, Ce-io aryl, og 5-6-leddet heteroaryl, C1-6 haloalkyl, halo, CN, eller36, SRa6, C(0)Rb6, C(0)NRc6Rd6, C(0)0Ra6, 0C(0)Rb6, 0C(0)NRc6Rd6, NRc6Rd6, NRc6C(0)Rb6, NRc6C(0)NRc6Rd6, NRc6C(0)0Ra6, C( = NRe6)NRc6Rd6, NRc6C( = NRe6)NRc6Rd6, S(0)Rb6, S(0)NRc6Rd6, S(0)2Rb6, NRc6S(0)2Rb6, NRc6S(0)2NRc6Rd6, og S(0)2NRc6Rd6, hvor Ci-e alkyl, C3-7 cycloalkyl, 4-7-leddet heterocycloalkyl, Ce-io aryl, og 5-6-leddet heteroaryl er eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra halo, CN, eller36, SRa6, C(0)Rb6, C(0)NRc6Rd6, C(0)0Ra6, 0C(0)Rb6, 0C(0)NRc6Rd6, NRc6Rd6, NRc6C(0)Rb6, NRc6C(0)NRc6Rd6, NRc6C(0)0Ra6, C( = NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(0)Rb6, S(0)NRc6Rd6, S(0)2Rb6, NRc6S(0)2Rb6, NRc6S(0)2NRc6Rd6, og S(0)2NRc6Rd6; eller hvilken som helst af Rc3 og Rd3 sammen med det N-atom til hvilket de er bundet danner en 4-, 5-, 6-, eller 7-leddet heterocycloalkylgruppe eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra Ci-6 alkyl, C3-7 cycloalkyl, 4-7-leddet heterocycloalkyl, Ce-io aryl, 5-6-leddet heteroaryl, Ci-6 haloalkyl, halo, CN, eller36, SRa6, C(0)Rb6, C(0)NRc6Rd6, C(0)0R36, 0C(0)Rb6, 0C(0)NRc6Rd6, NRc6Rd6, NRc6C(0)Rb6, NRc6C(0)NRc6Rd6, NRc6C(0)0Ra6, C( = NRe6)NRc6Rd6, NRc6C( = NRe6)NRc6Rd6, S(0)Rb6, S(0)NRC6Rd6, S(0)2Rb6, NRc6S(0)2Rb6, NRc6S(0)2NRc6Rd6, og S(0)2NRc6Rd6, hvor Ci-e alkyl, C3-7 cycloalkyl, 4-7-leddet heterocycloalkyl, Ce-io aryl, og 5-6-leddet heteroaryl er eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra halo, CN, eller36, SR36, C(0)Rb6, C(0)NRc6Rd6, C(0)0R36, 0C(0)Rb6, 0C(0)NRc6Rd6, NRc6Rd6, NRc6C(0)Rb6, NRc6C(0)NRc6Rd6, NRc6C(0)0R36, C( = NRe6)NRc6Rd6, NRc6C( = NRe6)NRc6Rd6, S(0)Rb6, S(0)NRc6Rd6, S(0)2Rb6, NRc6S(0)2Rb6, NRc6S(0)2NRc6Rd6, og S(0)2NRc6Rd6; eller hvilken som helst af Rc4 og Rd4 sammen med det N-atom til hvilket de er bundet danner en 4-, 5-, 6-, eller 7-leddet heterocycloalkylgruppe eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra Ci-6 alkyl, C3-7 cycloalkyl, 4-7-leddet heterocycloalkyl, Ce-io aryl, 5-6-leddet heteroaryl, C1-6 haloalkyl, halo, CN, eller36, SRa6, C(0)Rb6, C(0)NRc6Rd6, C(0)0Ra6, 0C(0)Rb6, 0C(0)NRc6Rd6, NRc6Rd6, NRc6C(0)Rb6, NRc6C(0)NRc6Rd6, NRc6C(0)0Ra6, C( = NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(0)Rb6, S(0)NRc6Rd6, S(0)2Rb6, NRc6S(0)2Rb6, NRc6S(0)2NRc6Rd6, og S(0)2NRc6Rd6, hvor C1-6 alkyl, C1-4 cycloalkyl, 4-7-leddet heterocycloalkyl, C6-10 aryl, og 5-6-leddet heteroaryl er eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra halo, CN, eller36, SRa6, C(0)Rb6, C(0)NRc6Rd6, C(0)0Ra6, 0C(0)Rb6, 0C(0)NRc6Rd6, NRc6Rd6, NRc6C(0)Rb6, NRc6C(0)NRc6Rd6, NRc6C(0)0Ra6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(0)Rb6, S(0)NRc6Rd6, S(0)2Rb6, NRc6S(0)2Rb6, NRc6S(0)2NRc6Rd6, og S(0)2NRc6Rd6; eller hvilken som helst af Rc5 og Rd5 sammen med det N-atom til hvilket de er bundet danner en 4-, 5-, 6-, eller 7-leddet heterocycloalkylgruppe eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra Ci-6 alkyl, C3-7 cycloalkyl, 4-7-leddet heterocycloalkyl, C6-10 aryl, 5-6-leddet heteroaryl, Ci-e haloalkyl, halo, CN, eller36, SRa6, C(0)Rb6, C(0)NRc6Rd6, C(0)0R36, 0C(0)Rb6, 0C(0)NRc6Rd6, NRc6Rd6, NRc6C(0)Rb6, NRc6C(0)NRc6Rd6, NRc6C(0)0Ra6, C(=NRe6)NRc6Rd6, NRc6C( = NRe6)NRc6Rd6, S(0)Rb6, S(0)NRc6Rd6, S(0)2Rb6, NRc6S(0)2Rb6, NRc6S(0)2NRc6Rd6, og S(0)2NRc6Rd6, hvor Ci-e alkyl, C3-7 cycloalkyl, 4-7-leddet heterocycloalkyl, Ce-io aryl, og 5-6-leddet heteroaryl er eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra halo, CN, eller36, SRa6, C(0)Rb6, C(0)NRc6Rd6, C(0)0R36, 0C(0)Rb6, 0C(0)NRc6Rd6, NRc6Rd6, NRc6C(0)Rb6, NRc6C(0)NRc6Rd6, NRc6C(0)0Ra6, C( = NRe6)NRc6Rd6, NRc6C( = NRe6)NRc6Rd6, S(0)Rb6, S(0)NRc6Rd6, S(0)2Rb6, NRc6S(0)2Rb6, NRc6S(0)2NRc6Rd6, og S(0)2NRc6Rd6; hver Re, Re2, Re3, Re4, og Re5 er uafhængigt valgt fra H, Ci-4 alkyl, CN, eller36, SRb6, S(0)2Rb6, C(0)Rb6, S(0)2NRc6Rd6, og C(0)NRc6Rd6; hver Ra6, Rb6, Rc6, og Rd6 er uafhængigt valgt fra H, Ci-4 alkyl, Ci-4 haloalkyl, C2-4 alkenyl, og C2-4 alkynyl, hvor Ci-4 alkyl, C2-4 alkenyl, og C2-4 alkynyl er eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra OH, CN, amino, halo, Ci-4 alkyl, Ci-4 alkoxy, Ci-4 alkylthio, Ci-4 alkylamino, di(Ci-4 alkyl)amino, Ci-4 haloalkyl, og Ci-4 haloalkoxy; eller hvilken som helst af Rc6 og Rd6 sammen med det N-atom til hvilket de er bundet danner en 4-, 5-, 6-, eller 7-leddet heterocycloalkylgruppe eventuelt substitueret med 1, 2, eller 3 substituenter uafhængigt valgt fra OH, CN, amino, halo, Ci-e alkyl, Ci-4 alkoxy, Ci-4 alkylthio, Ci-4 alkylamino, di(Ci-4 alkyl)amino, Ci-4 haloalkyl, og Ci-4 haloalkoxy; og hver Re6 er uafhængigt valgt fra H, Ci-4 alkyl, og CN.
2. Forbindelsen ifølge krav 1, eller et farmaceutisk acceptabelt salt deraf, hvor R2 er halo.
3. Forbindelsen ifølge krav 1, eller et farmaceutisk acceptabelt salt deraf, hvor R2 er fluor.
4. Forbindelsen ifølge et hvilket som helst af kravene 1-3, eller et farmaceutisk acceptabelt salt deraf, hvor R5 er halo.
5. Forbindelsen ifølge et hvilket som helst af kravene 1-3, eller et farmaceutisk acceptabelt salt deraf, hvor R5 er fluor.
6. Forbindelsen ifølge et hvilket som helst af kravene 1-5, eller et farmaceutisk acceptabelt salt deraf, hvor R6 er H.
7. Forbindelsen ifølge et hvilket som helst af kravene 1-6, eller et farmaceutisk acceptabelt salt deraf, hvor R10 og R11 sammen med det carbonatom til hvilket de er bundet danner en 3-, 4-, 5-, 6-, eller 7-leddet cycloalkylgruppe.
8. Forbindelsen ifølge et hvilket som helst af kravene 1-6, eller et farmaceutisk acceptabelt salt deraf, hvor R10 og R11 sammen med det carbonatom til hvilket de er bundet danner en cyclopropylgruppe.
9. Forbindelsen ifølge et hvilket som helst af kravene 1-8, eller et farmaceutisk acceptabelt salt deraf, hvor R7 og R8 er hver uafhængigt valgt fra H, Ci-e alkyl, -C(0)RA, Ce-io aryl, C3-10 cycloalkyl, 5-10-leddet heteroaryl, 4-10-leddet heterocycloalkyl, Ce-io aryl-Ci-4 alkyl, (5-10-leddet heteroaryl)-Ci-4 alkyl, og (4-10-leddet heterocycloalkyl)-Ci-4 alkyl, hvor Ci-e alkyl, Ce-io aryl, C3-10 cycloalkyl, 5-10-leddet heteroaryl, 4-10-leddet heterocycloalkyl, (5-10-leddet heteroaryl)-Ci-4 alkyl, og (4-10-leddet heterocycloalkyl)-Ci-4 alkyl er hver eventuelt substitueret med 1, 2, 3, 4, eller 5 substituenter uafhængigt valgt fra R7a.
10. Forbindelsen ifølge et hvilket som helst af kravene 1-8, eller et farmaceutisk acceptabelt salt deraf, hvor R7 og R8 er hver uafhængigt valgt fra H, 2-hydroxypropyl, -C(0)0CH3, 3-fluorphenyl, cyclopropyl, cyclobutyl, 3,3-difluorcyclobutyl, cyclopentyl, cyclohexyl, 4-hydroxycyclohexyl, methyl, l-methyl-lH-pyrazol-4-yl, pyridin-3-yl, N-methylpiperidin-4-yl, tetrahydro-2H-pyran-4-yl, tetrahydrofuran-3-yl, 1-phenylethyl, (l-methyl-lH-pyrazol-4-yl)methyl, 2-morpholino-4-ylethyl, pyridin-2-ylmethyl, N-methylpiperazin-1-ylethyl, og tetrahydrofuran-2-ylmethyl.
11. Forbindelsen ifølge et hvilket som helst af kravene 1-8, eller et farmaceutisk acceptabelt salt deraf, hvor én af R7 og R8 er H.
12. Forbindelsen ifølge et hvilket som helst af kravene 1-8, eller et farmaceutisk acceptabelt salt deraf, hvor R7 og R8 hver er H.
13. Forbindelsen ifølge krav 1 valgt fra: 2'-(2,6-difluor-3,5-dimethoxyphenyl)-6'-[(2-morpholin-4-ylethyl)amino]- l',2'-dihydro-3'H-spiro[cyclopropan-l,4,-[2,7]naphthyridin]-3'-on; 6,-amino-2,-(2,6-difluor-3,5-dimethoxyphenyl)-l,H-spiro[cyclopropan-l,4'- [2,7]naphthyridin]-3'(2'H)-on; 2,-(2,6-difluor-3,5-dimethoxyphenyl)-6,-(methylamino)-l',2'-dihydro-3,H- spiro[cyclopropan-l,4'-[2,7]naphthyridin]-3'-on; 2'-(2,6-difluor-3,5-dimethoxyphenyl)-6'-(tetrahydro-2H-pyran-4-ylamino)- l',2,-dihydro-3'H-spiro[cyclopropan-l,4,-[2,7]naphthyridin]-3'-on; (S)-2'-(2,6-difluor-3,5-dimethoxyphenyl)-6'-(2-hydroxypropylamino)-l'H- spiro[cyclopropan-l,4'-[2,7]naphthyridin]-3'(2'H)-on; 2'-(2,6-difluor-3,5-dimethoxyphenyl)-6'-(pyridin-2-ylmethylamino)-l'H- spiro[cyclopropan-l,4'-[2,7]naphthyridin]-3'(2'H)-on; (S)-2'-(2,6-difluor-3,5-dimethoxyphenyl)-6'-(tetrahydrofuran-3-ylamino)- l'H-spiro[cyclopropan-l,4'-[2,7]naphthyndin]-3'(2'f/)-on; 2'-(2,6-difluor-3,5-dimethoxyphenyl)-6,-(2-(4-methylpiperazin-l- yl)ethylamino)-l,H-spiro[cyclopropan-l,4,-[2,7]naphthyridin]-3'(2,H)-on; methyl 2'-(2,6-difluor-3,5-dimethoxyphenyl)-3'-oxo-2,,3,-dihydro-l,H-spiro[cyclopropan- l,4'-[2,7]naphthyridin]-6'-ylcarbamat; 2'-(2,6-difluor-3,5-dimethoxyphenyl)-6,-(pyridin-3-ylamino)-l'H- spiro[cyclopropan-l,4'-[2,7]naphthyridin]-3'(2,H)-on; 2'-(2,6-difluor-3,5-dimethoxyphenyl)-6,-(3-fluorphenylamino)-l'H- spiro[cyclopropan-l,4,-[2,7]naphthyridin]-3'(2'H)-on; 6,-(cyclopentylamino)-2,-(2,6-difluor-3,5-dimethoxyphenyl)-l'H- spiro[cyclopropan-l,4,-[2,7]naphthyridin]-3'(2'H)-on; (S)-2'-(2,6-difluor-3,5-dimethoxyphenyl)-6'-((tetrahydrofuran-2- yl)methylamino)-l,H-spiro[cyclopropan-l,4,-[2,7]naphthyridin]-3'(2,H)-on; 2'-(2,6-difluor-3,5-dimethoxyphenyl)-6'-(l-methyl-lH-pyrazol-4-ylamino)- l'H-spiro[cyclopropan-l,4,-[2,7]naphthyridin]-3,(2'H)-on; 2'-(2,6-difluor-3,5-dimethoxyphenyl)-6,-((l-methyl-lH-pyrazol-4- yl)methylamino)-l'H-spiro[cyclopropan-l,4,-[2,7]naphthyridin]-3'(2,H)-on; (R)-2'-(2,6-difluor-3,5-dimethoxyphenyl)-6,-(l-phenylethylamino)-l'H- spiro[cyclopropan-l,4'-[2,7]naphthyndin]-3'(2'H)-on; 6'-(cyclohexylamino)-2'-(2,6-difluor-3,5-dimethoxyphenyl)-l'H- spiro[cyclopropan-l,4,-[2,7]naphthyridin]-3'(2'H)-on; 2'-(2,6-difluor-3,5-dimethoxyphenyl)-6'-(trans-4- hydroxycyclohexylamino)-l,H-spiro[cyclopropan-l,4,-[2,7]naphthyridin]- 3'(2'H)-on; 6'-(cyclopropylamino)-2'-(2,6-difluor-3,5-dimethoxyphenyl)-l,H- spiro[cyclopropan-l,4'-[2,7]naphthyridin]-3'(2,H)-on; 6'-(cyclobutylamino)-2'-(2,6-difluor-3,5-dimethoxyphenyl)-l,H- spiro[cyclopropan-l,4,-[2,7]naphthyridin]-3,(2,H)-on; 2'-(2,6-difluor-3,5-dimethoxyphenyl)-6'-(3,3-difluorcyclobutylamino)-l,H-spiro[cyclopropan-l,4'-[2,7]naphthyridin]-3,(2'H)-on; og 2,-(2,6-difluor-3,5-dimethoxyphenyl)-6,-(l-methylpiperidin-4-ylamino)- l'H-spiro[cyclopropan-l,4,-[2,7]naphthyridin]-3,(2,H)-on; eller et farmaceutisk acceptabelt salt af en hvilken som helst af de ovenfor nævnte.
14. Forbindelsen ifølge krav 1, hvor forbindelsen er 2'-(2,6-difluor-3,5-dimethoxyphenyl)-6'-[(2-morpholin-4-ylethyl)amino]-l',2,-dihydro-3,H-spiro[cyclopropan-l,4'-[2,7]naphthyridin]-3'-on, elleret farmaceutisk acceptabelt salt deraf.
15. Forbindelsen ifølge krav 1, hvor forbindelsen er 2'-(2,6-difluor-3,5-dimeth-oxyphenyl)-6'-(2-(4-methylpiperazin-l-yl)ethylamino)-l'H-spiro[cyclo-propan-l,4'-[2,7]naphthyridin]-3'(2'H)-on, eller et farmaceutisk acceptabelt salt deraf.
16. Forbindelsen ifølge krav 1, hvor forbindelsen er (S)-2'-(2,6-difluor-3,5-dimethoxyphenyl)-6'-((tetrahydrofuran-2-yl)methylamino)-l'H-spiro[cyclopropan-l,4'-[2,7]naphthyridin]-3'(2'H)-on, eller et farmaceutisk acceptabelt salt deraf.
17. Farmaceutisk sammensætning omfattende en forbindelse ifølge et hvilket som helst af kravene 14-16, eller et farmaceutisk acceptabelt salt deraf, og mindst en farmaceutisk acceptabel bærer.
18. Farmaceutisk sammensætning omfattende en forbindelse ifølge et hvilket som helst af kravene 1 til 13, eller et farmaceutisk acceptabelt salt deraf, og mindst en farmaceutisk acceptabel bærer.
19. Fremgangsmåde til inhibering af et FGFR-enzym omfattende at bringe enzymet in vitro i kontakt med en forbindelse ifølge et hvilket som helst af kravene 1 til 16, eller et farmaceutisk acceptabelt salt deraf.
20. Forbindelse ifølge et hvilket som helst af kravene 1 til 16, eller et farmaceutisk acceptabelt salt deraf, til anvendelse i:- a) fremgangsmåde til behandling af cancer hos en patient; eller b) fremgangsmåde til behandling af cancer hos en patient, hvor canceren er valgt blandt blærecancer, brystcancer, livmoderhalscancer, kolorektalcancer, endometriecancer, mavecancer, hoved- og halscancer, nyrecancer, levercancer, lungecancer, ovariecancer, prostatacancer, øsofagealcancer, galdeblærecancer, bugspytkirtelcancer, skjoldbrusk-kirtelcancer, hudcancer, leukæmi, multipel myelom, kronisk lymfocytisk lymfom, voksen T-celle-leukæmi, B-celle lymfom, akut myelogenøs leukæmi, Hodgkin's eller non-Hodgkin's lymfom, Waldenstrom's makroglobulinæmi, hårcellelymfom, Burkett's lymfom, glioblastom, melanom, og Rhabdosarcom.
21. Forbindelse ifølge et hvilket som helst af kravene 1 til 16, eller et farmaceutisk acceptabelt salt deraf, til anvendelse i:- a) fremgangsmåde til behandling af en myeloproliferativ forstyrrelse hos en patient; eller b) fremgangsmåde til behandling af en myeloproliferativ forstyrrelse hos en patient hvor den myeloproliferativ forstyrrelse er valgt fra polycytæmi vera, essentiel thrombocytæmi, og primær myelofibrose.
22. Forbindelse ifølge et hvilket som helst af kravene 1 til 16, eller et farmaceutisk acceptabelt salt deraf, til anvendelse i:- a) fremgangsmåde til behandling af en skeletal- eller chondrocyt-forstyrrelse hos en patient; eller b) fremgangsmåde til behandling afen skeletal- eller chondrocyt-forstyrrelse hos en patient hvor skeletal- eller chondrocyt-forstyrrelsen er valgt fra achrondroplasi, hypochondroplasi, dværgvækst, thanatophorisk dysplasi (TD), Apert syndrom, Crouzon syndrom, Jackson-Weiss syndrom, Beare-Stevenson cutis gyrat syndrom, Pfeiffer syndrom, og craniosynostosis syndrom.
23. Forbindelse ifølge et hvilket som helst af kravene 1 til 16, eller et farmaceutisk acceptabelt salt deraf, til anvendelse i:- a) fremgangsmåde til behandling afen hypophosphatæmi-forstyrrelse hos en patient; eller b) fremgangsmåde til behandling afen hypophosphatæmi-forstyrrelse hos en patient hvor hypophosphatæmi-forstyrrelsen er X-bundet hypophosphatæmisk lidelse, autosomal recessiv hypophosphatæmisk lidelse, autosomal dominant hypophosphatæmisk lidelse, eller tumorinduceret osteromalaci.
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