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HRP20230458T1 - Piridazinoni kao inhibitori parp7 - Google Patents

Piridazinoni kao inhibitori parp7 Download PDF

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HRP20230458T1
HRP20230458T1 HRP20230458TT HRP20230458T HRP20230458T1 HR P20230458 T1 HRP20230458 T1 HR P20230458T1 HR P20230458T T HRP20230458T T HR P20230458TT HR P20230458 T HRP20230458 T HR P20230458T HR P20230458 T1 HRP20230458 T1 HR P20230458T1
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nrc3rd3
aryl
ora3
optionally substituted
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Melissa Marie Vasbinder
Laurie B. Schenkel
Kerren Kalai Swinger
Kevin Wayne Kuntz
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Ribon Therapeutics Inc.
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Claims (39)

1. Spoj, naznačen time, da je predstavljen Formulom I: [image] ili njegova farmaceutski prihvatljiva sol, gdje: X je Cl, Br, CH3, CF3, CN, OCH3, etil, ciklopropil, SCH3, ili izopropil; A je skupina koja ima formulu (A-1): [image] svaki od Y1, Y2 i Y3 se neovisno bira od O, S, NRY, C(=O), C(=)O, C(=O)NRY, S(=O), S(=O)2, S(=O)NRY, S(=O)2NRY, ili NRYC(=O)NRY, gdje je svaki RY neovisno H ili C1-4 alkil; L je C1-34 alkilen, O, S, NRY, C(=O), C(=O)O, C(=O)NRY, S(=O), S(=O)NRY, ili NRYC(=O)NRY; Z je H, CyZ, halogen, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, C(=NRe)Rb, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcS(O)Rb,NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, i S(O)2NRcRd; gdje je svaki navedeni C1-6 alkil, C2-6 alkenil, C2-6 alkinil, i C1-6 haloalkil od Z, opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituenata koji su neovisno odabrani od CyZ, halogena, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, C(=NRe)NRcRd, NRcC(=NRe)NRcRd, NRcRd, NRcC(O)Rb, NRcC(O)ORa, NRcC(O)NRcRd, NRcS(O)Rb,NRcS(O)2Rb, NRcS(O)2NRcRd, S(O)Rb, S(O)NRcRd, S(O)2Rb, i S(O)2NRcRd; CyZ se bira od C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, i 4-10-člani heterocikloalkil, od kojih je svaki opcionalno supstituiran s 1, 2, 3 ili 4 supstituenta neovisno odabrana od halogena, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe1)NRc1Rd1, NRc1C(=NRe1)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1,NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, i S(O)2NRc1Rd1; gdje su alkil, C2-6 alkenil, i C2-6 alkinil, opcionalno supstituirani s 1, 2 ili 3 supstituenta koji su neovisno odabrani od halogena, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe1)NRc1Rd1, NRc1C(=NRe1)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1,NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, i S(O)2NRc1Rd1; Prsten D je monociklička ili policiklička 4-10-člana heterocikloalkil skupina koja je opcionalno supstituirana s 1, 2 ili 3 skupine neovisno odabrane od halogena, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(=NRe2)NRc2Rd2, NRc2C(=NRe2)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, NRc2S(O)Rb2,NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, i S(O)2NRc2Rd2; gdje je svaki C1-6 alkil, C2-6 alkenil, i C2-6 alkinil, opcionalno supstituiran s 1, 2 ili 3 skupine koje su neovisno odabrane od halogena, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(=NRe2)NRc2Rd2, NRc2C(=NRe2)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, NRc2S(O)Rb2,NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, i S(O)2NRc2Rd2; svaki od R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 i R12se neovisno bira od H, halogena, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-7 cikloalkil-C1-4 alkil, 5-10-člani heteroaril-C1-4 alkil, 4-10-člani heterocikloalkil-C1-4 alkil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, C(=NRe3)Rb3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3S(O)Rb3,NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, i S(O)2NRc3Rd3; gdje je svaki navedeni C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-7 cikloalkil-C1-4 alkil, 5-10-člani heteroaril-C1-4 alkil, i 4-10-člani heterocikloalkil-C1-4 alkil od navedenih R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 i R12, opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituenata koji su neovisno odabrani od halogena, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, C(=NRe3)Rb3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3S(O)Rb3,NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, i S(O)2NRc3Rd3; ili R1 i R3 zajedno s atomima ugljika s kojima su vezani, tvore C5-10 cikloalkil prsten ili 5-10-člani heterocikloalkil prsten, od kojih je svaki opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od halogena, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, C(=NRe3)Rb3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3S(O)Rb3,NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, i S(O)2NRc3Rd3; ili R3 i R5 zajedno s atomima ugljika s kojima su vezani, tvore C5-10 cikloalkil prsten ili 5-10-člani heterocikloalkil prsten, od kojih je svaki opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od halogena, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, C(=NRe3)Rb3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3S(O)Rb3,NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, i S(O)2NRc3Rd3; ili R7 i R9 zajedno s atomima ugljika s kojima su vezani, tvore C5-10 cikloalkil prsten ili 5-10-člani heterocikloalkil prsten, od kojih je svaki opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od halogena, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, C(=NRe3)Rb3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3S(O)Rb3,NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, i S(O)2NRc3Rd3; ili R9 i R11 zajedno s atomima ugljika s kojima su vezani, tvore C5-10 cikloalkil prsten ili 5-10-člani heterocikloalkil prsten, od kojih je svaki opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od halogena, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, C(=NRe3)Rb3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3S(O)Rb3,NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, i S(O)2NRc3Rd3; ili R5 i R7 zajedno s atomima ugljika s kojima su vezani i zajedno s Y2, tvore 5-10-člani heterocikloalkil prsten koji je opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od halogena, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, C(=NRe3)Rb3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3S(O)Rb3,NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, i S(O)2NRc3Rd3; ili R1 i R3 zajedno tvore dvostruku vezu između atoma ugljika s kojima su vezani; ili R3 i R5 zajedno tvore dvostruku vezu između atoma ugljika s kojima su vezani; ili R7 i R9 zajedno tvore dvostruku vezu između atoma ugljika s kojima su vezani; ili R9 i R11 zajedno tvore dvostruku vezu između atoma ugljika s kojima su vezani; ili R9, R10, R11 i R12 zajedno tvore trostruku vezu između atoma ugljika s kojima su vezani; svaki od Ra, Rb, Rc, Rd, Ra1, Rb1, Rc1, Rd1, Ra2, Rb2, Rc2, Rd2, Ra3, Rb3, Rc3 i Rd3 se neovisno bira od H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-7 cikloalkil-C1-4 alkil, 5-10-člani heteroaril-C1-4 alkil, i 4-10-člani heterocikloalkil-C1-4 alkil, gdje je svaki navedeni C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-7 cikloalkil-C1-4 alkil, 5-10-člani heteroaril-C1-4 alkil, i 4-10-člani heterocikloalkil-C1-4 alkil od navedenih Ra, Rb, Rc, Rd, Ra1, Rb1, Rc1, Rd1, Ra2, Rb2, Rc2, Rd2, Ra3, Rb3, Rc3 i Rd3, opcionalno supstituiran s 1, 2 ili 3 supstituenta koji su neovisno odabrani od halogena, C1-4 alkil, C1-4 haloalkil, C2-6 alkenil, C2-6 alkinil, CN, ORa7, SRa7, C(O)Rb7, C(O)NRc7Rd7, C(O)ORa7, OC(O)Rb7, OC(O)NRc7Rd7, NRc7Rd7, NRc7C(O)Rb7, NRc7C(O)NRc7Rd7, NRc7C(O)ORa7, C(=NRe7)NRc7Rd7, NRc7C(=NRe7)NRc7Rd7, S(O)Rb7, S(O)NRc7Rd7, S(O)2Rb7, NRc7S(O)2Rb7, NRc7S(O)2NRc7Rd7, i S(O)2NRc7Rd7; ili Rc i Rd zajedno s N atomom s kojim su vezani, tvore 4-7-članu heterocikloalkil skupinu opcionalno supstituiranu s 1, 2 ili 3 supstituenta neovisno odabrana od CN, halogena, C1-4 alkil, C1-4 haloalkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, CN, NO2, ORa7, SRa7, C(O)Rb7, C(O)NRc7Rd7, C(O)ORa7, OC(O)Rb7, OC(O)NRc7Rd7, NRc7Rd7, NRc7C(O)Rb7, NRc7C(O)NRc7Rd7, NRc7C(O)ORa7, C(=NRe7)NRc7Rd7, NRc7C(=NRe7)NRc7Rd7, S(O)Rb7, S(O)NRc7Rd7, S(O)2Rb7, NRc7S(O)2Rb7, NRc7S(O)2NRc7Rd7, i S(O)2NRc7Rd7; ili Rc1 i Rd1 zajedno s N atomom s kojim su vezani, tvore 4-7-članu heterocikloalkil skupinu koja je opcionalno supstituirana s 1, 2 ili 3 supstituenta neovisno odabrana od CN, halogena, C1-4 alkil, C1-4 haloalkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, CN, ORa7, SRa7, C(O)Rb7, C(O)NRc7Rd7, C(O)ORa7, OC(O)Rb7, OC(O)NRc7Rd7, NRc7Rd7, NRc7C(O)Rb7, NRc7C(O)NRc7Rd7, NRc7C(O)ORa7, C(=NRe7)NRc7Rd7, NRc7C(=NRe7)NRc7Rd7, S(O)Rb7, S(O)NRc7Rd7, S(O)2Rb7, NRc7S(O)2Rb7, NRc7S(O)2NRc7Rd7, i S(O)2NRc7Rd7; ili Rc2 i Rd2 zajedno s N atomom s kojim su vezani, tvore 4-7-članu heterocikloalkil skupinu koja je opcionalno supstituirana s 1, 2 ili 3 supstituenta neovisno odabrana od CN, halogena, C1-4 alkil, C1-4 haloalkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, CN, ORa7, SRa7, C(O)Rb7, C(O)NRc7Rd7, C(O)ORa7, OC(O)Rb7, OC(O)NRc7Rd7, NRc7Rd7, NRc7C(O)Rb7, NRc7C(O)NRc7Rd7, NRc7C(O)ORa7, C(=NRe7)NRc7Rd7, NRc7C(=NRe7)NRc7Rd7, S(O)Rb7, S(O)NRc7Rd7, S(O)2Rb7, NRc7S(O)2Rb7, NRc7S(O)2NRc7Rd7, i S(O)2NRc7Rd7; ili Rc3 i Rd3 zajedno s N atomom s kojim su vezani, tvore 4-7-članu heterocikloalkil skupinu koja je opcionalno supstituirana s 1, 2 ili 3 supstituenta neovisno odabrana od CN, halogena, C1-4 alkil, C1-4 haloalkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, CN, ORa7, SRa7, C(O)Rb7, C(O)NRc7Rd7, C(O)ORa7, OC(O)Rb7, OC(O)NRc7Rd7, NRc7Rd7, NRc7C(O)Rb7, NRc7C(O)NRc7Rd7, NRc7C(O)ORa7, C(=NRe7)NRc7Rd7, NRc7C(=NRe7)NRc7Rd7, S(O)Rb7, S(O)NRc7Rd7, S(O)2Rb7, NRc7S(O)2Rb7, NRc7S(O)2NRc7Rd7, i S(O)2NRc7Rd7; Ra7, Rb7, Rc7 i Rd7 se neovisno biraju od H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-7 cikloalkil-C1-4 alkil, 5-10-člani heteroaril-C1-4 alkil, i 4-10-člani heterocikloalkil-C1-4 alkil; gdje je svaki navedeni C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-7 cikloalkil, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-7 cikloalkil-C1-4 alkil, 5-10-člani heteroaril-C1-4 alkil, i 4-10-člani heterocikloalkil-C1-4 alkil, opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od OH, CN, amino, halogena, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi; svaki Re, Re1, Re2, Re3 i Re7 se neovisno bira od H, C1-4 alkil, i CN; a je 0 ili 1; m je 0 ili 1; n je 0 ili 1; p je 0 ili 1; q je 0 ili 1; r je 0 ili 1; pri čemu bilo koja gore navedena heteroaril ili heterocikloalkil skupina sadrži 1, 2, 3 ili 4 heteroatoma koji tvore prsten i koji se neovisno biraju od O, N i S; i pri čemu je jedan ili više C i N atoma koji tvore prsten iz bilo koje od gore navedenih heterocikloalkil skupina, opcionalno supstituiran s okso (=O) skupinom.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) A je skupina koja ima formulu (A-1a): [image] ili b) A je skupina koja ima formulu (A-1b): [image] ili c) A je skupina koja ima formulu (A-1c): [image] u kojoj se svaki Z1 i Z2 neovisno bira od N i CH, i pritom R je CN, Cl ili CF3; ili d) A je skupina koja ima formulu (A-1d): [image] u kojoj se svaki Z1 i Z2 neovisno bira od N i CH, i pritom R je CN, Cl ili CF3.
3. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, naznačen time, da L je NRY ili O.
4. Spoj prema bilo kojem od patentnih zahtjeva 1-3, ili njegova farmaceutski prihvatljiva sol, naznačen time, da X je CF3, CH3, CN, Cl ili Br.
5. Spoj prema bilo kojem od patentnih zahtjeva 1-4, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) Y1 je NRY ili O; ili b) Y1 je NRY, O ili S; ili c) Y1 je NRY; ili d) Y1 je O.
6. Spoj prema bilo kojem od patentnih zahtjeva 1-5, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) Y2 je NRY ili O; ili b) Y2 je NRY, O ili S; ili c) Y2 je O.
7. Spoj prema bilo kojem od patentnih zahtjeva 1-6, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) Y3 je C(=O); ili b) Y3 je C(=O) ili S(=O)2.
8. Spoj prema bilo kojem od patentnih zahtjeva 1-7, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) RY je H ili C1-4 alkil; ili b) RY je metil; ili c) RY je H.
9. Spoj prema bilo kojem od patentnih zahtjeva 1-8, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) Z je H, CyZ, halogen, C1-6 alkil, C1-6 haloalkil, CN, NO2, ORa, C(O)Rb, C(O)NRcRd, C(O)ORa, NRcRd, i NRcC(O)Rb; pri čemu je svaki navedeni C1-6 alkil, i C1-6 haloalkil od Z, opcionalno supstituiran s 1, 2, 3, 4 ili 5 supstituenata koji su neovisno odabrani od CyZ, halogena, CN, NO2, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, i NRcC(O)Rb; ili b) Z je CyZ.
10. Spoj prema bilo kojem od patentnih zahtjeva 1-9, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) CyZ se bira od 5-10-članog heteroarila i 4-10-članog heterocikloalkila, od kojih je svaki opcionalno supstituiran s 1, 2, 3 ili 4 supstituenta neovisno odabrana od halogena, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe1)NRc1Rd1, NRc1C(=NRe1)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1,NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, i S(O)2NRc1Rd1; gdje su alkil, C2-6 alkenil, i C2-6 alkinil, opcionalno supstituirani s 1, 2 ili 3 supstituenta neovisno odabrana od halogena, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe1)NRc1Rd1, NRc1C(=NRe1)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1,NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, i S(O)2NRc1Rd1; ili b) CyZ je 5-10-člani heteroaril, opcionalno supstituiran sa CN, CF3 ili Cl; ili c) CyZ je 5-10-člani heteroaril, opcionalno supstituiran sa CN, C1-6 alkil, C1-6 haloalkil, halogen, ili NRc1Rd1, gdje je C1-6 alkil, opcionalno supstituiran sa CN, ili NRc1Rd1; ili d) CyZ je piridinil ili pirimidinil, od kojih je svaki opcionalno supstituiran sa CN, CF3, ili Cl.
11. Spoj prema bilo kojem od patentnih zahtjeva 1-10, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) Prsten D je monociklička ili policiklička 4-10-člana heterocikloalkil skupina koja je opcionalno supstituirana s 1, 2 ili 3 skupine neovisno odabrane od halogena, C1-6 alkil, C1-6 haloalkil, CN, NO2, ORa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, NRc2Rd2, NRc2C(O)Rb2, gdje je C1-6 alkil opcionalno supstituiran s 1, 2 ili 3 skupine neovisno odabrane od halogena, CN, NO2, ORa2, C(O)Rb2, NRc2Rd2, i NRc2C(O)Rb2; ili b) Prsten D je monociklička 4-10-člana heterocikloalkil skupina; ili c) Prsten D je piperazinil; ili d) Prsten D je piperazinil, dihidropiridazinil, diazepail, pirolidinil, ili heksahidropirolo[3,2-b]pirol-1(2H)-il.
12. Spoj prema bilo kojem od patentnih zahtjeva 1-11, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R1 je H, halogen, ORa3, C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, C6-10 aril-C1-4 alkil, gdje je navedeni C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, opcionalno supstituiran s ORa3, ili NRc3Rd3; ili b) R1 je H, halogen, ORa3, C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, 4-10-člani heterocikloalkil, C6-10 aril-C1-4 alkil, 5-10-člani heteroaril-C1-4 alkil, ili 4-10-člani heterocikloalkil-C1-4 alkil, gdje je navedeni C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, C6-10 aril-C1-4 alkil, 5-10-člani heteroaril-C1-4 alkil, ili 4-10-člani heterocikloalkil-C1-4 alkil, opcionalno supstituiran s ORa3, ili NRc3Rd3; ili c) R1 je C1-6 alkil; ili d) R1 je C1-6 alkil, opcionalno supstituiran s ORa3; ili e) R1 je H; ili f) R1 je metil, etil, ili izopropil; ili g) R1 je metoksimetil, ili hidroksimetil; ili h) R1 je fenil, fenilmetil, ili piridinil.
13. Spoj prema bilo kojem od patentnih zahtjeva 1-12, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R2 je H, halogen, ORa3, C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, C6-10 aril-C1-4 alkil, gdje je navedeni C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, opcionalno supstituiran s ORa3 ili NRc3Rd3; ili b) R2 je ORa3; ili c) R2 je H.
14. Spoj prema bilo kojem od patentnih zahtjeva 1-13, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R3 je H, halogen, ORa3, C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, C6-10 aril-C1-4 alkil, gdje je navedeni C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, opcionalno supstituiran s ORa3, ili NRc3Rd3; ili b) R3 je H; ili c) R3 je metil, etil, ili izopropil; ili d) R3 je metoksimetil, ili hidroksimetil; ili e) R3 je fenil, fenilmetil, ili piridinil.
15. Spoj prema bilo kojem od patentnih zahtjeva 1-14, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R4 je H, halogen, ORa3, C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, C6-10 aril-C1-4 alkil, gdje je navedeni C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, opcionalno supstituiran s ORa3, ili NRc3Rd3; ili b) R4 je H.
16. Spoj prema bilo kojem od patentnih zahtjeva 1-15, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R5 je H, halogen, ORa3, C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, C6-10 aril-C1-4 alkil, gdje je navedeni C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, opcionalno supstituiran s ORa3, ili NRc3Rd3; ili b) R5 je H; ili c) R5 je metil, etil, ili izopropil; ili d) R5 je metoksimetil, ili hidroksimetil; ili e) R5 je fenil, fenilmetil, ili piridinil.
17. Spoj prema bilo kojem od patentnih zahtjeva 1-16, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R6 je H, halogen, ORa3, C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, C6-10 aril-C1-4 alkil, gdje je navedeni C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, opcionalno supstituiran s ORa3, ili NRc3Rd3; ili b) R6 je H.
18. Spoj prema bilo kojem od patentnih zahtjeva 1-17, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R7 je H, halogen, ORa3, C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, C6-10 aril-C1-4 alkil, gdje je navedeni C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, opcionalno supstituiran s ORa3, ili NRc3Rd3; ili b) R7 je C1-6 alkil; ili c) R7 je metil.
19. Spoj prema bilo kojem od patentnih zahtjeva 1-18, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R8 je H, halogen, ORa3, C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, gdje je navedeni C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, opcionalno supstituiran s ORa3, ili NRc3Rd3; ili b) R8 je H.
20. Spoj prema bilo kojem od patentnih zahtjeva 1-19, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R9 je H, halogen, ORa3, C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, gdje je navedeni C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, opcionalno supstituiran s ORa3 ili NRc3Rd3; ili b) R9 je H.
21. Spoj prema bilo kojem od patentnih zahtjeva 1-20, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R10 je H, halogen, ORa3, C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, C6-10 aril-C1-4 alkil, gdje je navedeni C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, opcionalno supstituiran s ORa3, ili NRc3Rd3; ili b) R10 je H.
22. Spoj prema bilo kojem od patentnih zahtjeva 1-21, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R11 je H, halogen, ORa3, C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, gdje je navedeni C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, opcionalno supstituiran s ORa3 ili NRc3Rd3; ili b) R11 je H.
23. Spoj prema bilo kojem od patentnih zahtjeva 1-22, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R12 je H, halogen, ORa3, C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, gdje je navedeni C1-6 alkil, C6-10 aril, 5-10-člani heteroaril, ili C6-10 aril-C1-4 alkil, opcionalno supstituiran s ORa3 ili NRc3Rd3; ili b) R12 je H.
24. Spoj prema bilo kojem od patentnih zahtjeva 1-13, 15, i 17-23, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R3 i R5 zajedno s atomima ugljika s kojima su vezani, tvore C5-10 cikloalkil prsten, ili 5-10-člani heterocikloalkil prsten, od kojih je svaki opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od halogena, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, C(=NRe3)Rb3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3S(O)Rb3,NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, i S(O)2NRc3Rd3; ili b) R3 i R5 zajedno s atomima ugljika s kojima su vezani, tvore C5-10 cikloalkil prsten, ili 5-10-člani heterocikloalkil prsten; ili c) R3 i R5 zajedno s atomima ugljika s kojima su vezani, tvore tetrahidrofuranil prsten; ili d) R3 i R5 zajedno s atomima ugljika s kojima su vezani, tvore ciklobutil ili ciklopentil prsten.
25. Spoj prema bilo kojem od patentnih zahtjeva 1-15, 17, i 19-24, ili njegova farmaceutski prihvatljiva sol, naznačen time, da: a) R5 i R7 zajedno s atomima ugljika s kojima su vezani, i zajedno s Y2, tvore 5-10-člani heterocikloalkil prsten koji je opcionalno supstituiran s 1, 2 ili 3 supstituenta neovisno odabrana od halogena, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, C(=NRe3)Rb3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3S(O)Rb3,NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, i S(O)2NRc3Rd3; ili b) R5 i R7 zajedno s atomima ugljika s kojima su vezani, i zajedno s Y2, tvore 5-10-člani heterocikloalkil prsten; ili c) R5 i R7 zajedno s atomima ugljika s kojima su vezani, i zajedno s Y2, tvore tetrahidrofuranil prsten, ili tetrahidropiranil prsten; ili d) R5 i R7 zajedno s atomima ugljika s kojima su vezani, i zajedno s Y2, tvore tetrahidrofuranil prsten, tetrahidropiranil prsten, ili pirolidinil prsten.
26. Spoj prema bilo kojem od patentnih zahtjeva 1 i 3-25, ili njegova farmaceutski prihvatljiva sol, naznačen time, da m je 1.
27. Spoj prema bilo kojem od patentnih zahtjeva 1 i 3-26, ili njegova farmaceutski prihvatljiva sol, naznačen time, da n je 0.
28. Spoj prema bilo kojem od patentnih zahtjeva 1 i 3-27, ili njegova farmaceutski prihvatljiva sol, naznačen time, da p je 1.
29. Spoj prema bilo kojem od patentnih zahtjeva 1 i 3-28, ili njegova farmaceutski prihvatljiva sol, naznačen time, da q je 0.
30. Spoj prema bilo kojem od patentnih zahtjeva 1 i 3-29, ili njegova farmaceutski prihvatljiva sol, naznačen time, da r je 1.
31. Spoj prema bilo kojem od patentnih zahtjeva 1 i 3-30, ili njegova farmaceutski prihvatljiva sol, naznačen time, da a je 0.
32. Spoj prema bilo kojem od patentnih zahtjeva 1-2, i 4-25, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je predstavljen: a) Formulom IIa: [image] ili b) Formulom IIb: [image] ili c) Formulom IIc: [image] u kojoj se svaki Z1 i Z2 neovisno bira od N i CH, i gdje R je CN, Cl, ili CF3; ili d) Formulom IId: [image] u kojoj se svaki Z1 i Z2 neovisno bira od N i CH, i gdje R je CN, Cl, ili CF3.
33. Spoj prema patentnom zahtjevu 1, naznačen time, da spoj je 5-[[(2S)-1-(3-okso-3-[4-[5-(trifluorometil)pirimidin-2-il]piperazin-1-il]propoksi)propan-2-il]amino]-4-(trifluorometil)-2,3-dihidropiridazin-3-on, ili njegova farmaceutski prihvatljiva sol.
34. Spoj prema patentnom zahtjevu 33, naznačen time, da spoj je kristal.
35. Spoj prema patentnom zahtjevu 33 ili 34, naznačen time, da spoj posjeduje: a) najmanje jedan karakteristični maksimum XRPD rendgenske difrakcije na prahu, odabran od oko 5,8, oko 10,8, oko 11,9, i oko 17,2 stupnjeva 2-theta; ili b) najmanje jedan karakteristični maksimum XRPD rendgenske difrakcije na prahu, odabran od oko 5,8, oko 10,8, oko 11,9, oko 13,3, oko 13,5, oko 15,5, i oko 17,2 stupnjeva 2-theta; ili c) uzorak XRPD rendgenske difrakcije na prahu s karakterističnim maksimumima kao što je u bitnom prikazano na Slici 8.
36. Spoj prema bilo kojem od patentnih zahtjeva 33-35, naznačen time, da spoj posjeduje: a) termogram DSC diferencijalne skenirajuće kalorimetrije, naznačen time, da ima endotermički maksimum na temperaturi od oko 174 °C; ili b) termogram DSC diferencijalne skenirajuće kalorimetrije koji je u bitnom opisan na Slici 9.
37. Farmaceutski pripravak, naznačen time, da sadrži spoj prema bilo kojem od patentnih zahtjeva 1-36, ili njegovu farmaceutski prihvatljivu sol, i najmanje jedan farmaceutski prihvatljiv nosač.
38. Spoj prema bilo kojem od patentnih zahtjeva 1-36, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u postupku liječenja raka kod pacijenta kojemu je potrebno liječenje, pri čemu postupak obuhvaća davanje navedenom pacijentu terapijski učinkovite količine spoja, ili njegove farmaceutski prihvatljive soli.
39. Spoj ili njegova farmaceutski prihvatljiva sol, za uporabu prema patentnom zahtjevu 38, naznačen time, da navedeni rak je rak dojke, rak središnjeg živčanog sustava, rak endometrija, rak bubrega, rak velikog crijeva, rak pluća, rak jednjaka, rak jajnika, rak gušterače, rak prostate, rak abdomena, rak glave i vrata (gornjeg aerodigestivnog centra), rak urinarnog trakta, ili rak debelog crijeva.
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