DK2081931T3 - [1,2,4]Triazolo[4,3-a]pyridinderivater der er nyttige som inhibitorer for hepatocytvækstfaktorreceptoren - Google Patents
[1,2,4]Triazolo[4,3-a]pyridinderivater der er nyttige som inhibitorer for hepatocytvækstfaktorreceptoren Download PDFInfo
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- DK2081931T3 DK2081931T3 DK07810473.4T DK07810473T DK2081931T3 DK 2081931 T3 DK2081931 T3 DK 2081931T3 DK 07810473 T DK07810473 T DK 07810473T DK 2081931 T3 DK2081931 T3 DK 2081931T3
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Claims (19)
1. ΕΞη forbindelse med formlen I
i et enantiomer, et diastereomer, eller et passende farmaceutisk salt deraf hvori JerN; Wer GR2b; Z er -O-, eller -NR®-; Z* er -O-, -S(Q)v-, eller-NR5-; R2a er -H, R2b er-H eller halo; Ra, Rb Rc og Rd hver uafhængigt er H, halo, alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyi, cploalkenyl, heterocyclo, aryl, heteroaryl, -NO2, -CN, -NR5R5a, -OR4, -C(=0)R4, -C(=0)0R4; -C(=0)NR5R5a, -N(R5)C(=0)NR5R5a, -0C(=0)NR5R5a, -S(0)vR4, -S(0)2NR5R5a, -N(R5)S02R4 som hver især eventuelt uafhængigt kan substitueres med en R10-gruppe som tilladt af valens; eller R8 og Rb,sammen med det carbonatom som de er bundet til, køn kombineres til at døhhé ét 3-10 -ringet cycloalkyi, en 3-1 O-ringet cycloalkenylring, eller en heterocycloring, som hver især eventuelt kan substitueres med en R1Q-gruppe som tilladt af valens; eller Rc og Rd, sammen med det carbonatom som de er bundet til, kan kombineres ti! at danne et 3-1Q -ringet cycloalkyi, en 3-10-ringet cycloalkenylring, eller en heterocycloring, som hver især eventuelt kan substitueres med en R1Q-gruppe som tilladt af valens; eller R8 øg/eiler Rb kan kombineres med en hvilken som helst af Rc eller Rd til at danne en delvis eller fuldt mættet 3-8-ringet cycloalkylring eller heterocycloring, som begge eventuelt kan substitueres med en R10-gruppe som tilladt af valen?; eller Rc og Rd, som er bundettil det samme carbonatom, kan kombineres til at danne en carbonyl gruppe; R1 er phenyl, naphthyl, isoquinolinyi, quinolinyl, naphthyridinyl, furopyridlnyl, quinazoline, quinoxaline som hver Især eventuelt uafhængigt kan substitueres med en R10-gruppe som tilladt øf vaiens, R2 er phenyl, naphthyl; pyrrolyl, imidazolyl, pyrazolyl, triazolyf, tetrazolyl, furanyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, isothiåzoiyi, pyridinyl, tetrahydropyridinyl, ppdinenyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, isoindolyl, indolinyl, indolinonyl, isoindolinyl, isoindolinonyi, dihydrobenzofuranyl, dihydroisobenzofuranyl, benzofuranyl, isobenzofuranyl, quinolinyl, isoquinolinyi, quinazolinyl, quinazolinonyi, ietrahydfdquinohnyi, tetrahydroisoquinolinyl, dihydroquinolinonyl, dihydroisoquinoiinonyi, quihoxalinyl, tetrahydroquinoxalinyl, benzomorphoiinyi, dihydrobenzodioxinyf, irnldåzopyridinyl, naphthyridinyf, benzotriazinyi, triazolopyridinyl, triazplppyrimidinyt, iriazolopyridazinyl, imidazopyrimidinyl, imidazopyridazinyl, pyrrolopyridinyl, pyrrolopyrimidinyl, pyrrpiopyridazinyi, pyrazofopyridinyl, pyrazoiopyrimidinyl, pyrazplopyridazinyl, cinnoSinyi, thienopyrrolyl, tetrahydrothienopyrrolyl, dihydroihienopyrroionyl, thienopyridihyi, thienopyrimidinyl, thienopyridazinyl, furopyridinyl, furopyrimidinyl, furopyrazidinyl, benzoimidazoiyl, benzoisoxazolyl, benzothiazoiyl, eller benzoisothiazolyi som hver især eventuelt uafhængigt kan substitueres med en Ri°-gruppe som tilladt af valens, RS er uafhængigt valgt ved enhver forekomst fra H, alkyl, haloalkyl, cyeloalkyi, alkenyl, aikynyl, ary!, heteroaryl, heterocyclo, arylalkyl, heteroarylalkyl, heterocycloalkyi, og cyeløalkylaikyf, som hver især eventuelt uafhængigt kan substitueres med en R10-gruppe søm tilladt af valens, R5 dg R5a véd enhver forekomst er uafhængigt valgt fra H, alkyl, haloalkyl, cyeloalkyi, alkenyl, aikynyl, aryl, heteroaryl, heterocyclo, arylalkyl, heteroarylalkyl, heterocycloalkyi, pg cycioalkylalkyl, som hver især eventuelt kan substitueres som tilladt af valens, med en R110; eller R5 og R5a kan kombineres til at danne en heterocyclonng eventuelt substitueret med én eller fleré RTO; R10 ved enhver forekomst uafhængigt er halo, cyano, oxo, alkyl, haloalkyl, eller m er 0 eller 1;; n er 0,1 eller 2; q dg t begge uafhængigt er 0 eller 1; v er 0,1 eller 2,
2. En forbindelse Ifølge krav 1 hvori R2 er valgt ffa
hvoim* er 0 éilér 1, som tilladt af valens.
3. En forbindelse ifølge krav 1 hvori R1 grupper enten ikke er substituerede eller er uafhængigt substituerede som tilladt af valens med eri eller flefé halo, cyano, oxo, alkyl, haloatkyi, eller -(aikylene)m-QR4. 4. ih forbindelse ifølge krav 1 med følgende IF-forme!
enantiomerer, diastereomerer og sale deraf hvori q er 0, 1,2 eller 3; n* er 0, 1 eller 2, t* er 0 eller i U1, U\ U3 og U4 hver uafhængigt er C eiier N; Z* er-O-, -S(0)v, eller -MH; Ra Rb rc 0g Rd hver uafhængigt er H, halo, alkyl, alkenyl, afkynyi, haloalkyl, cycloalkyl, eycioalkenyl, heterocyclo, aryl, heteroaryl, -N02, -CN, -NR5R5a, -OR4, -C(=0)R4, -C(=0)OR4; -C(=0)NR5R5a, -N(R5)C(=0)NR5R5a, -00i=0)NR5R^ -SfOJyR4, -S(0)2NR5RSa, -N(RS)S02R4 som hver især eventuelt uafhængigt kan substitueres meden R,0-gruppe som tiiiadt af valens,; eller Ra og Rb, sammen med det carbonatom som de er bundet til, kan kombineres ti! at danne et 3-10 -ringet cycloalkyl, en 3-1 O-ringet cycloalkenylring, eller én heterocycloring, som hver især evéhtueit kan substitueres med en R10-gruppe som tilladt af valens; eller RSeg Ra, sammen med det carbonatom som de er bundet til, kan kombineres fif at danne et 3-10 -ringet cycloalkyl, en 3-1 O-ringet cycloalkenylring, eller en heterocycloring, som hver især eventuelt kan substitueres med en Rt0-gruppe som tilladt af valens; eiier Ra og/e!ler Rb kan kombineres med enhver af Rc eller Rd til at danne en delvis eiier fuldt mættet 3-8-ringet cycioalkylring eller heterocycloring, som begge eventuelt kan substitueres med en R10-gruppe som tiiiadt af valens; eller Rc og Rd, som er bundet ti! det samme cårboriatom, kan kombineret ti! at danne en eårbonylgruppe; Fp er som defineret i krav 1; R2a er H eg R2b er H eller halo; Ri veil enhver forekomst uafhængigt er valgt fra H, alkyl, haloalkyi, cycioalkyl, alkenyl, alkynyl, aryi, heteroaryt, heterocyclo, aryialkyi, heteroarylalkyl, heterocycloalkyl, og cycloalkylalkyl, som hver især eventuelt uafhængigt kan substitueres som tilladt af valéhSSfen R10-gruppe; R5 og R5a ved enhver forekomst, uafhængigt er valgt fra Hi, alkyl, haloalkyi, cycioalkyl, alkenyl, alkynyl, aryl, heteroaryi, heterocyclo, aryialkyi, heteroarylalkyl, heterocycloalkyl, og cycloalkylalkyl, som hver især eventuelt kan substitueres som tilladt af valens af éh R10; eller R5 og R5a kan kombineres til at danne en heteroeycloring eventuelt substitueret af en R10; Ri° pg R10r- ved enhver forekomst uafhængigt er halo, cyano, oxo, alkyl, haloalkyi, eller -{aikylene)m-OR4. verO, 1 eller 2.
5. Err forbindelse ifølge krav 4 med formlen IFi, IFii, IFiii eller IFiv
enantiomerer, diastereomerer og salte deraf.
6, En forbindelse ifølge krav 5 hvori R10c ved enhver forekomst uafhængigt er fraværende, halo, eyano, oxo, alkyl, haloalkyi, eller -(alkylene)m-OR4.
7, En forbindelse ifølge krav 8 hvori n* er 0 eller 1, og t* er 1;
8, En forbindelse ifølge krav 6 hvori n‘ er 1 og t* er 0.
9, En forbindelse som defineret i krav 1 valgt fra
elier salte deraf.
10. En forbindelse valgt fra
enaniiomerer, diastereomerer og saite deraf, hvori q er 0, 1, 2 eller 3; n* er 0,1 eller 2; ί* er Ο eller 1 U1, U2 eg U3 hver uafhængigt er G, eller N; Z* er -Q-i -S(0)v, eller-NN; Ra, Rb, Rc og Rd hver uafhængigt er H, halo, alkyl......alkenyl, alkynyl, haloalkyl, eycloalkyl, cyeloalkenyl, héteroeplo, aryl, heteroaryl, -N02, -CN, -NR5R5a, -OR4, -C(=0)R4, -C(=0)0R4; -C(=0)NR5R5a, N(R»)G{=OpRsR5a, 0C(=;0)NR5R®* -S(Q)vR* -S(0)jNR5R5a, -N(R5)S02R4 som hver især eventuelt «afhængigt kan substitueres med en R10-gruppe som tilladt af valens; eller Ra og Rb, sammen med det carbonatom som de er bundet til, kan kombineres til at danne et 3-10 -ringet cycloalkyl, en 3-10-ringet cycloalkenylring, eller en heterocycioring, som hver især eventuelt kan substitueres med en R1 “-gruppe som tilladt af valens; eller Rc og Rd, sammen med det carbonatom som de er bundet til, kan kombineres til at danne et 3-10 -ringet cycloaiky!, en 3-10-ringet cycloalkenylring, eller en heterocycioring, som hver især eventuelt kan substitueres med en R10-gruppe som tilladt af valens; eller Ra og/eller Rb kan kombineres med enhver af R° eller Rd til at danne en delvis eller fuldt mættet 3-8-ringet cycioalkylring eller heterocycioring, som begge eventuelt kan substitueres med en Rm-gruppe som tilladt af valens, eller Rc and Rri som: er bundet til det samme carbonatom, kan kombineres til at danne en carbonyigruppe; R2 er som defineret I krav 1, R2a er H and R2b er H, eller halo; R4 ved enhver forekomst uafhængigt er valgt fra H, aikyl, haloaikyi, cycloaiky!, alkenyl, alkynyl, aryl, heteroaryl, heterocyclo, arylalkyl, heteroarylaikyl, heteroeycloalkyl, and cydoalkylalkyl, som hver især eventuelt uafhængigt kan substitueres med eh R10-gruppe som tilladt af valens; R5 and R5a ved enhver forekomst uafhængigt er valgt fra H, alkyl, haloalkyl, eycloalkyl, flkenyl, alkynyl, aryl, |eteroaryl, heterocyclo, aryjalkyi, heteroarylaikyl, heteroeycloalkyl, and cydoalkylalkyl, , som hver især eventuelt kan substitueres med en R^-gruppe som tilladt af valens; eller R5 and R5a kan kombineres til åt dahné én heterocycioring eventuelt substitueret méd én éllér flére R10; rio and Rioc ved enhver forekomst uafhængigt er halo, cyano, oxo, alkyl, haloalkyl, eller -(alkylene)m-OR4. v er 0,1 eller 2. 1:2, En forbmdelse ifølge krav 11 rned formel IFAi, IFAii eller iFAii* ^
enantiomerer, diastereomerer eller salte deraf.
13, En forbindelse ifølge krav 12, hvori R10c ved enhver forekomst uafhængigt ér hald, cyano, oxo, alkyi, Dalkyl, eller -(alkyiene)m-OR4.
14, En forbindelse ifølge krav 12 hvori n* er 0 eller 1, and t* er 1;
15, Én forbindelse Ifølge krav 11 hvori n* er 1 and t* er 0 1S. En forbindelse ifølge krav 1 Valgt fra
og salte deraf,
17, Én farmaceutisk sammensætning indeholdende en forbindelse ifølge krav 1 sammen med en passende farmaceutisk vehikel eller bærer.
18, Anvendelse af en forbindelse ifølge krav 1 til fremstilling af et lægemiddel til behandling af cancer.
19, Anvendelsen ifølge krav 18, hvori forbindelsen skal indgives i kombination med mindst en forbindelse valgt fra antibiotikaiignende midler, alkylerende midler, antimetabolitter, hormonmidler; immunologiske midler, interferonlignende midler og diverse midler.
20, Anvendelse af en forbindelse ifølge krav 1 til fremstilling af et lægemiddel til at redueeré én tumors størrelse i et emne.
21. Anvendeise sf en forbindelse ifølge krav 1 ti! fremstilling af et lægemiddel til behandling af HGF-relaferede lidelser.
22. Anvendelse af en forbindelse ifølge krav 1 til fremstilling af et lægemiddel til reducering af metastaser i en tumor.
23. En forbindelse ifølge krav 1 til anvendelse i behandling af cancer, reducering sf en tumors størrelse, behandling af HGF-reiaterede lidelser eller reducering af metastaser i en tumor.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US83088206P | 2006-07-14 | 2006-07-14 | |
PCT/US2007/016068 WO2008008539A2 (en) | 2006-07-14 | 2007-07-13 | Fused heterocyclic derivatives useful as inhibitors of the hepatocyte growth factor receptor |
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Publication Number | Publication Date |
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DK2081931T3 true DK2081931T3 (da) | 2016-12-19 |
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Application Number | Title | Priority Date | Filing Date |
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DK07810473.4T DK2081931T3 (da) | 2006-07-14 | 2007-07-13 | [1,2,4]Triazolo[4,3-a]pyridinderivater der er nyttige som inhibitorer for hepatocytvækstfaktorreceptoren |
Country Status (24)
Country | Link |
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US (1) | US8212041B2 (da) |
EP (3) | EP2578583A1 (da) |
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- 2007-07-13 EP EP12000581.4A patent/EP2578583A1/en not_active Withdrawn
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