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DK2928474T3 - Diazollactamer - Google Patents

Diazollactamer Download PDF

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Publication number
DK2928474T3
DK2928474T3 DK13859762.0T DK13859762T DK2928474T3 DK 2928474 T3 DK2928474 T3 DK 2928474T3 DK 13859762 T DK13859762 T DK 13859762T DK 2928474 T3 DK2928474 T3 DK 2928474T3
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mmol
alkyl
group
cycloalkyl
compound according
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DK13859762.0T
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Xi Chen
Pingchen Fan
Yandong Li
Jay P Powers
Viengkham Malathong
Sreenivas Punna
Hiroko Tanaka
Penglie Zhang
Dean Dragoli
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Chemocentryx Inc
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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Claims (21)

1. Forbindelse repræsenteret ved strukturen (I): hvor n er et heltal på fra 0 til 3; hver A er uafhængigt valgt fra gruppen bestående af N og CH; X og Z hver uafhængigt er valgt fra gruppen bestående af (i) monocyklisk eller kondenseret-bicyklisk aryl og heteroaryl, hvor heteroarylgruppen har fra 1-4 heteroatomer som ringelementer valgt fra N, O og S; (ii) monocyklisk fire-, fem-, seks- eller syv-leddet ring valgt fra gruppen bestående af cycloalkan og heterocycloalkan, hvor heterocycloalkanringene har fra 1-3 heteroatomer som ringelementer valgt fra N, O og S; hvor hver af ringene i (i) og (ii) eventuelt er substitueret med fra 1 til 5 substituenter valgt fra halogen, CN, Ci-s-alkyl, C3-8-cycloalkyl, C2-8-alkenyl, C2-8-alkynyl, Ci-e-haloalkyl, Ci-8-hydroxyalkyl, -ORa, -CCteR3, -SCteR3, -NRaRb, -CONRaRb, aryl, 5-eller 6-leddet heteroaryl, og 3-, 4-, 5- eller 6-leddet heterocycloalkan, hvor heteroatomerne, der er til stede som ringtoppunkter af heteroaryl- og heterocycloalkanringen, er valgt fra N, O og S, og hvor alkyl-, cycloalkyl-, aryl-, heteroaryl- og heterocycloalkandelene af substituenterne eventuelt endvidere er substitueret med 1-3 Ra; og eventuelt, to substituenter på tilstødende ringtoppunkter er forbundet for at danne en supplerende 5- eller 6-leddet ring, der er mættet, umættet eller aromatisk med ringtoppunkter valgt fra C, O, N og S; R3 er et element valgt fra gruppen bestående af H, halogen, CN, Ci-8-alkyl, C3-8-cycloalkyl, C2-8-alkenyl, C2-8-alkynyl, Ci-8-haloalkyl, Ci-8-hydroxyalkyl, -ORa, -CC>2Ra, -NRaRb, -CONRaRb, aryl, 5- eller 6-leddet heteroaryl og 3-, 4-, 5- eller 6-leddet heterocycloalkan, hvor heteroatomerne, der er til stede som ringtoppunkter af heteroaryl- og heterocycloalkanringene, er valgt fra N, O og S, og hvor alkyl-, cycloalkyl-, aryl-, heteroaryl- og heterocycloalkandelene af R3 eventuelt endvidere er substitueret med 1-3 Ra;
R4 er et element valgt fra gruppen bestående af H, -0Ra og Ci-s-alkyl eventuelt substitueret med -ORa; R9 er et element valgt fra gruppen bestående af H og Ci-8-alkyl eventuelt substitueret med -ORa; hver Ra og Rb er uafhængigt valgt fra gruppen bestående af hydrogen, hydroxyl, halogen, cyano, Ci-8-alkyl, Ci-8-alkoxy, Ci-8-haloalkyl, C3-6-cycloalkyl, C3-6-cycloalkylalkyl, amino, Ci-8-alkylamino, di-Ci-8-alkylamino, carboxamid, carboxy C1-4-alkylester, carboxylsyre og -SO2-Ci-8-alkyl, eller et hvilket som helst salt, solvat, hydrat, N-oxid eller en hvilken som helst rotamer deraf.
2. Forbindelse ifølge krav 1, repræsenteret ved strukturen:
hvor A1 er N eller C(R5); A2 er N eller C(R7); R5, R6, R7 og R8 hver uafhængigt er valgt fra gruppen bestående af H, halogen, CN, Ci-8-alkyl, C3-8-cycloalkyl, C2-8-alkenyl, C2-8-alkynyl, Ci-8-haloalkyl, C1-8-hydroxyalkyl, -ORa, -CCteR3, -NRaRb, -CONRaRb, aryl, 5- eller 6-leddet heteroaryl og 3-, 4-, 5- eller 6-leddet heterocycloalkan, hvor heteroatomerne, der er til stede som ringtoppunkter af heteroaryl- og heterocycloalkanringen er valgt fra N, O og S, og hvor alkyl-, cycloalkyl-, aryl-, heteroaryl- og heterocycloalkandelene af R5, R6, R7 og R8 eventuelt endvidere er substitueret med 1-3 Ra; og eventuelt, tilstødende elementer af R5, R6, R7 og R8 er forbundet for at danne en supplerende 5- eller 6-leddet ring, der er mættet, umættet eller aromatisk med ringtoppunkter valgt fra C, O, N og S; eller et farmaceutisk acceptabelt salt, hydrat, solvat, en rotamer eller et N-oxid deraf.
3. Forbindelse ifølge krav 2, hvor R8 er andet end H.
4. Forbindelse ifølge krav 2, der er repræsenteret ved strukturen:
hvor R1 og R2 hver uafhængigt er valgt fra gruppen bestående af H, halogen, CN, C1-8-alkyl, C3-8-cycloalkyl, C2-8-alkenyl, C2-8-alkynyl, Ci-8-haloalkyl, Ci-8-hydroxyalkyl, -ORa, -CO2Ra, -SO2Ra, -NRaRb, -CONRaRb og 3-, 4-, 5- eller 6-leddet heterocycloalkan, hvor heteroatomerne, der er til stede som ringtoppunkter af heterocycloalkanringen, er valgt fra N, O og S, og hvor alkyl-, cycloalkyl- og heterocycloalkandelene af R1 og R2 eventuelt endvidere er substitueret med 1-3 Ra.
5. Forbindelse ifølge krav 4, hvor hver R1 og R2 er uafhængigt valgt fra gruppen bestående af H, halogen, CN, Ci-s-alkyl, Ci-8-haloalkyl, -CO2Ra og -SO2Ra.
6. Forbindelse ifølge krav 4, hvor R9 er H eller CH3.
7. Forbindelse ifølge krav 4, repræsenteret ved strukturen:
hvor n er 1,2 eller 3, eventuelt hvor n er 1.
8. Forbindelse ifølge krav 4, hvor ringdelen med N, A1 og A2 som ringtoppunkter er valgt fra gruppen bestående af:
hvor bølgelinjen indikerer bindingspunktet til det resterende af forbindelsen.
9. Forbindelse ifølge krav 4, hvor ringdelen med N, A1 og A2 som ringtoppunkter er valgt fra gruppen bestående af:
hvor R1 og R2 hver uafhængigt er valgt fra gruppen bestående af H, halogen, CN, C1-8-alkyl, C3-8-cycloalkyl, C2-8-alkenyl, C2-8-alkynyl, Ci-8-haloalkyl, Ci-8-hydroxyalkyl, -ORa, -CO2Ra, -SO2Ra, -NRaRb, -CONRaRb og 3-, 4-, 5- eller 6-leddet heterocycloalkan, hvor heteroatomerne, der er til stede som ringtoppunkter af heterocycloalkanringen, er valgt fra N, O og S, og hvor alkyl-, cycloalkyl- og heterocycloalkandele af R1 og R2 eventuelt endvidere er substitueret med 1-3 Ra; og R7 er H eller Cl og R8 er Ci-s-alkyl eventuelt substitueret med 1 eller 2 Ra; og hvor bølgelinjen indikerer bindingspunktet til det resterende af forbindelsen.
10. Forbindelse ifølge krav 7, hvor n er 1, der er repræsenteret ved strukturen:
hvor R1 er Cl eller F; og eventuelt hvor R3 er valgt fra gruppen bestående af H, Ci-s-alkyl, C3-8-cycloalkyl og C2-8-alkenyl.
11. Forbindelse ifølge krav 10, der er repræsenteret ved strukturen: (i)
eventuelt hvor R3 er valgt fra gruppen bestående af H, Ci-s-alkyl, C3-8-cycloalkyl og C2-8-alkenyl eller
(ii)
eventuelt hvor R3 er valgt fra gruppen bestående af H, Ci-s-alkyl, C3-8-cycloalkyl og C2-8-alkenyl eller (iii)
12. Forbindelse ifølge krav 7, hvor n er 1, der er repræsenteret ved strukturen: hvor R1 er Cl eller F
13. Forbindelse ifølge krav 7, hvor n er 1, der er repræsenteret ved strukturen: (i)
eventuelt hvor R3 er valgt fra gruppen bestående af H, Ci-s-alkyl, C3-8-cycloalkyl og C2-8-alkenyl eller (ϋ)
eventuelt hvor R3 er valgt fra gruppen bestående af H, Ci-s-alkyl, C3-8-cycloalkyl og C2- -alkenyl eller (iii)
14. Forbindelse ifølge et hvilket som helst af kravene 9, 10, 11 struktur (i) eller (ii), eller 13, hvor R3 er valgt fra gruppen bestående af H, Ci-8-alkyl, C3-8-cycloalkyl og C2-8-alkenyl.
15. Forbindelse ifølge krav 1, der har formlen
eller et farmaceutisk acceptabelt salt, hydrat eller solvat deraf.
16. Forbindelse ifølge krav 1, der har formlen
eller et farmaceutisk acceptabelt salt, hydrat eller solvat deraf.
17. Farmaceutisk sammensætning, der omfatter forbindelsen ifølge et hvilket som helst af de foregående krav og en farmaceutisk acceptabel excipiens eller bærer.
18. Forbindelse ifølge et hvilket som helst af kravene 1-16 til anvendelse i en fremgangsmåde til behandling af en CCR1-medieret sygdom eller tilstand, hvilken fremgangsmåde omfatter administration til et individ med behov derfor af en terapeutisk virksom mængde af forbindelsen; hvor den CCR1-medierede sygdom eller tilstand er en inflammatorisk tilstand, en immunregulatorisk forstyrrelse eller en cancer.
19. Forbindelse ifølge et hvilket som helst af kravene 1-16 til anvendelse i en fremgangsmåde til behandling af en CCR1 -medieret sygdom eller tilstand, hvilken fremgangsmåde omfatter administration til et individ med behov derfor af en terapeutisk virksom mængde af forbindelsen; hvor den CCR1-medierede sygdom eller tilstand er valgt fra gruppen bestående af transplantatafvisning, dermatitis, eksem, urticaria, vasculitis, inflammatorisk tarmsygdom, fødevareallergi, astma, Alzheimers sygdom, Parkinsons sygdom, psoriasis, lupus erythematosus, apopleksi, restenose og encephalomyelitis.
20. Forbindelse ifølge et hvilket som helst af kravene 1-16 til anvendelse i en fremgangsmåde til behandling af en CCR1-medieret sygdom eller tilstand, hvilken fremgangsmåde omfatter administration til et individ med behov derfor af en terapeutisk virksom mængde af forbindelsen; hvor sygdommen er valgt fra gruppen af rheumatoid arthritis, multipel sklerose, osteoarthritis, multipelt myelom og osteoporose.
21. Forbindelse ifølge et hvilket som helst af kravene 1 -16 til anvendelse i en fremgangsmåde til behandling af en CCR1-medieret sygdom eller tilstand ifølge krav 18-20, hvilken fremgangsmåde omfatter administration til et individ med behov derfor af en terapeutisk virksom mængde af forbindelsen i kombination med et antiinflammatorisk middel, analgetikum, et antiproliferativt middel, en metabolisk hæmmer, en leukocytmigrationshæmmer eller en immunmodulator.
DK13859762.0T 2012-12-07 2013-12-06 Diazollactamer DK2928474T3 (da)

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