HRP20192336T1 - Derivati imidazotiadiazola i imidazopirazina kao inhibitori proteazom aktiviranog receptora 4 (par4) za liječenje agregacije trombocita - Google Patents

Derivati imidazotiadiazola i imidazopirazina kao inhibitori proteazom aktiviranog receptora 4 (par4) za liječenje agregacije trombocita Download PDF

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HRP20192336T1
HRP20192336T1 HRP20192336TT HRP20192336T HRP20192336T1 HR P20192336 T1 HRP20192336 T1 HR P20192336T1 HR P20192336T T HRP20192336T T HR P20192336TT HR P20192336 T HRP20192336 T HR P20192336T HR P20192336 T1 HRP20192336 T1 HR P20192336T1
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Croatia
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alkyl
halo
group
alkoxy
independently selected
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HRP20192336TT
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Jacques Banville
Roger RÉMILLARD
Edward H. Ruediger
Daniel H. Deon
Marc Gagnon
Laurence DUBÉ
Julia GUY
Eldon Scott Priestley
Shoshana L. POSY
Brad D. MAXWELL
Pancras C. Wong
Michael R. Lawrence
Michael M. Miller
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Bristol-Myers Squibb Company
Université de Montréal
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Claims (15)

1. Spoj sa formulom I: ili stereoizomer, tautomer, farmaceutski prihvatljiva sol ili solvat istog, gdje: WjeO; R0 je R1; Y je S ili -CR8=CR9-; R1 je nezavisno odabran od grupe koja se sastoji od: H, halo, C1-C2 alkila, ciklopropila, C1-C2 alkoksi, C1-C2 alkiltio, halo-C1-C2-alkila, koji sadrži 1 do 5 halogena, gdje je halo F ili Cl, i halo-C3-C4 cikloalkila; R8 i R9 su nezavisno odabrani od grupe koja se sastoji od: H, fluoro, kloro, C1-C3 alkila, C1-C2 alkoksi, i halo-C1-C2 alkila; pod uvjetom da najmanje jedan od R1, R8 i R9 je drugačije od H; R2 je H, X1 je odabran od grupe koja se sastoji od CH ili N; X2, X3 i X4 su nezavisno odabrani od CR3; R3 je odabran od grupe koja se sastoji od H, C1-C3 alkila, C1-C3 alkoksi, fluoro, kloro, OCF3, i halo-C1-C2-alkila, koji sadrži 1 do 5 halogena; R4 i R5 su nezavisno odabrani od H i metila; je heteroaril prsten sa 5 članova odabran od tiazola, tiadiazola, oksazola, oksadiazola, i triazola; R6 je odabran od grupe koja se sastoji od H, halo, OCF3, OCHF2, OH, CN, NO2, NR11R12, C1-C4 alkoksikarbonila, (C=O)NR11R12 i C1-C5 alkila koji je supstituiran sa 0 do 7 grupa koje su nezavisno odabrane od halo, CF3, OCF3, OH, hidroksi-C1-C4-alkila, C1-C4 alkoksi, C1-C4 alkoksi-C1-C4 alkoksi, di-C1-C4-alkilaminofenil-C1-C4-alkila, (di-C1-C4-alkoksi-C1-C4-alkil)-C1-C4-alkila, di-C1-C4-alkilamino, C3-C6-cikloalkila, i C1-C4 alkiltio, ili R6 je B-D-, gdje D je veznik, koji je odabran od: jednostruke veze, -O-, -S-,
C1-C4 alkilena koji je supstituiran sa 0 do 4 grupe koje su nezavisno odabrane od halo ili OH, C1-C4 alkilenoksi, C2-C6 alkenilena, i B je odabran iz grupe koja se sastoji od: C6-C10 arila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, halo-C1-C4 alkoksi, C1-C4 alkila, halo-C1-C4 alkila, C3-C6 cikloalkila, cijano, nitro, NR11R12, OH, C1-C4-alkilkarboniloksi-C1-C4-alkila, hidroksi-C1-C4-alkila, COOR14, SO2R14, (C=O)NR11R12, SO2NR11R12, N(R13)(C=O)NR11R12, N(R13)(C=O)OR14, N(R13)(C=O)R14, NR13S(O)R14, NR13SO2R14, O(C=O)NR11R12, O(C=O)OR14, O(C=O)R14, (C=O)OR14, i 5-6-očlanog heteroarila, 5- do 10-očlanog heteroarila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, halo-C1-C4 alkoksi, C1-C4 alkila, halo-C1-C4 alkila, C3-C6 cikloalkila, cijano, nitro, NR11R12, OH, C1-C4-alkilkarboniloksi-C1-C4-alkila, hidroksi-C1-C4-alkila, COOR14, SO2R14, (C=O)NR11R12, SO2NR11R12, N(R13)(C=O)NR11R12, N(R13)(C=O)OR14, N(R13)(C=O)R14, NR13S(O)R14, NR13SO2R14, O(C=O)NR11R12, O(C=O)OR14, O(C=O)R14, (C=O)OR14, 5-6-očlanog heteroarila, i (CH2)fenila, 4- do 10-očlanog heterociklila koji sadrži atome ugljika i 1 do 2 dodatna heteroatoma odabrana od N, O, i S, i supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, okso, -(CHR13)n1-5- ili 6-očlanog heteroarila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, C1-C4 alkila, ciklopropila, CF3, OCF3, i CF2CH3; NR13S(O)R14, NR13SO2R14, -(CHR13)n1-4- do 10-očlanog-heterociklila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, C1-C4 alkila, ciklopropila, CF3, OCF3, i CF2CH3; OH, hidroksi-C1-C4-alkila, C1-C4 alkoksi, halo-C1-C4 alkoksi, di-C1-C4-alkilamino-C1-C4-alkila, NR11R12, cijano, C1-C4 alkila, halo-C1-C4 alkila, C3-C6 cikloalkila, C1-C4-alkoksi-C1-C4-alkila, C3-C6 cikloalkil-C1-C4-alkilkarbonila, C6-C10 arilkarbonila, C1-C4-alkilkarboniloksi-C1-C4-alkila, COOR14, SO2R14, (C=O)NR11R12, SO2NR11R12, N(R13)(C=O)NR11R12, N(R13)(C=O)OR14, N(R13)(C=O)R14, O(C=O)NR11R12, O(C=O)OR14, O(C=O)R14, (C=O)OR14, i C6-C10 arila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, C1-C4 alkila, ciklopropila, C1-C4-alkoksikarbonila, (C=O)NR11R12, CF3, OCF3, i CF2CH3; C3-C6 cikloalkila koji može sadržati nezasićenje, supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, CF3, OCF3, 5- ili 6-očlanog heteroarila, OH, okso, hidroksi-C1-C4-alkila, C6-C10 arila, COOH, okso, C1-C4-alkoksikarbonila, (C=O)NR11R12, i C1-C4 alkila; i C5-C11 spirocikloalkila koji može da sadrži nezasićenje i koji po izboru sadrži 1 do 3 heteroatoma odabrana od O, N ili S i supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, CF3, OCF3, 5- ili 6-očlanog heteroarila, OH, hidroksi-C1-C4-alkila, C6-C10 arila, i C1-C4 alkila; R11 i R12 su nezavisno, pri svakom pojavljivanju, odabrani iz grupe koja se sastoji od: H, C1-C4 alkila, halo-C1-C4-alkila, C2-C4 alkenila, -(CR14R14)n1-fenila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, C1-C4 alkila, ciklopropila, CF3, OCF3, 5- ili 6-očlanog heteroarila, OH, OCHF2, di-C1-C4-alkilamino, i cijano, -(CHR13)n1-C3-C6-cikloalkila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, CF3, OCF3, 5- ili 6-očlanog heteroarila, OH, hidroksi-C1-C4-alkila, i C1-C4 alkila, -(CHR13)n1-4- do 10-očlanog-heterociklila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, CF3, OCF3, 5- ili 6-očlanog heteroarila, OH, okso, hidroksi-C1-C4-alkila, i C1-C4 alkila, -(CHR13 )n1-5- do 10-očlanog-heteroarila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, CF3, OCF3, 5- ili 6-očlanog heteroarila, OH, hidroksi-C1-C4-alkila, i C1-C4 alkila, di-C1-C4-alkilamino-C1-C4-alkila, di-C1-C4-alkoksi-C1-C4-alkila, hidroksi-C1-C4-alkila, cijano-C1-C4-alkila, C1-C4-alkoksi-C1-C4-alkila, C1-C4-alkoksikarbonil-C1-C4-alkila, C1-C4-alkoksikarbonila, C1-C4-alkilkarbonila, fenilkarbonila; C1-C4-alkoksikarbonilamino-C1-C4-alkilkarbonila, i di-C1-C4-alkilamino-C1-C4-alkilkarbonila, alternativno, R11 i R12, kada su vezani za isti dušik, kombiniraju se da formiraju 4- do 8-očlani heterociklični prsten koji sadrži atome ugljika supstituirane sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, CF3, CHF2, OCF3, OCHF2, OCH2F, 5- ili 6-očlanog heteroarila, OH, okso, hidroksi-C1-C4-alkila, C1-C4 alkila i C1-C4 alkoksi, i 0 do 2 dodatna heteroatoma odabrana od N, NR13, O i S(O)p; R13 je nezavisno, pri svakom pojavljivanju, odabran iz grupe koja se sastoji od H, C1-C6 alkila i -(CH2)fenila; R14 je nezavisno, pri svakom pojavljivanju, odabran iz grupe koja se sastoji od H, C1-C6 alkila, halo-C1-C4-alkila, C1-C4-alkoksikarbonilamino i -(CH2)n1fenila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, C1-C4 alkila, ciklopropila, CF3, OCF3, 5- ili 6-očlanog heteroarila, OH, OCHF2, di-C1-C4-alkilamino, i cijano, R7 je odabran iz grupe koja se sastoji od H, halo, hidroksila, okso, C1-C3 alkila, hidroksi-C1-C3-alkila, i halo-C1-C2-alkila, koji sadrži 1 do 5 halogena; n1, pri svakom pojavljivanju, je odabrano od 0, 1, 2 ili 3; i p, pri svakom pojavljivanju, je odabrano od 0, 1 i 2.
2. Spoj iz patentnog zahtjeva 1, ili stereoizomer, tautomer, farmaceutski prihvatljiva sol ili solvat istog, gdje: WjeO; R0 je R1; Y je S ili -CR8=CR9-; R1 je nezavisno odabran iz grupe koja se sastoji od: H, fluoro, kloro, C1-C2 alkila, C1-C2 alkoksi, C1-C2 alkiltio, i halo-C1-C2-alkila, koji sadrži 1 do 5 halogena, gdje halo je F ili Cl; R8 i R9 su nezavisno odabrani iz grupe koja se sastoji od: H, fluoro, kloro, CH3, OCH3, CF3, i CHF2; pod uvjetom da najmanje jedan od R1, R8 i R9 je drugačiji od H; R2 je H; X1 je odabran iz grupe koja se sastoji od CH ili N; X2 i X4 su CH; X3 je CR3; R3 je odabran iz grupe koja se sastoji od H, C1-C3 alkila, C1-C3 alkoksi, fluoro, kloro, OCF3, i halo-C1-C2-alkila, koji sadrži 1 do 5 halogena; R4 i R5 su nezavisno odabrani od H i metila; je 5-očlani heteroaril prsten odabran od tiazola, tiadiazola, oksazola, oksadiazola, i triazola; R6 je odabran iz grupe koja se sastoji od H, halo, OCF3, OCHF2, OH, NR11R12, C1-C4 alkoksikarbonila, (C=O)NR11R12 i C1-C5 alkila supstituiranog sa 0 do 7 grupa nezavisno odabranih od halo, CF3, OCF3, OH, hidroksi-C1-C4-alkila, C1-C4 alkoksi, C1-C4 alkoksi-C1-C4 alkoksi, di-C1-C4-alkilaminofenil-C1-C4-alkila, (di-C1-C4-alkoksi-C1-C4-alkil)-C1-C4-alkila, di-C1-C4-alkilamino, C3-C6-cikloalkila, i C1-C4 alkiltio, ili R6 je B-D-, gdje D je veznik, koji je odabran od: jednostruke veze, -O-, -S-,
C1-C4 alkilena supstituiranog sa 0 do 4 grupe nezavisno odabrane od halo ili OH, i C2-C6 alkenilena, i B je odabran iz grupe koja se sastoji od: C6-C10 arila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, halo-C1-C4 alkoksi, C1-C4 alkila, halo-C1-C4 alkila, C3-C6 cikloalkila, cijano, nitro, NR11R12, OH, C1-C4-alkilkarboniloksi-C1-C4-alkila, hidroksi-C1-C4-alkila, COOR14, SO2R14, (C=O)NR11R12, SO2NR11R12, N(R13)(C=O)NR11R12, N(R13)(C=O)OR14, N(R13)(C=O)R14, NR13S(O)R14, NR13SO2R14, O(C=O)NR11R12, O(C=O)OR14, O(C=O)R14, (C=O)OR14, i 5-6-očlanog heteroarila, 5- do 10-očlanog heteroarila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, halo-C1-C4 alkoksi, C1-C4 alkila, halo-C1-C4 alkila, C3-C6 cikloalkila, cijano, nitro, NR11R12, OH, C1-C4-alkilkarboniloksi-C1-C4-alkila, hidroksi-C1-C4-alkila, COOR14, SO2R14, (C=O)NR11R12, SO2NR11R12, N(R13)(C=O)NR11R12, N(R13)(C=O)OR14, N(R13)(C=O)R14, NR13S(O)R14, NR13SO2R14, O(C=O)NR11R12, O(C=O)OR14, O(C=O)R14, (C=O)OR14, 5-6-očlanog heteroarila, i (CH2)fenila, 4- do 10-očlanog heterociklila koji sadrži atome ugljika i 1 do 2 dodatna heteroatoma odabrana od N, O, i S, i supstituiranog sa 0 do 3 grupe nezavisno odabrane od grupe koja se sastoji od halo, okso, -(CHR13)n1-5- ili 6-očlanog heteroarila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, C1-C4 alkila, ciklopropila, CF3, OCF3, i CF2CH3; NR13S(O)R14, NR13SO2R14, -(CHR13)n1-4- do 10-očlanog-heterociklila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, C1-C4 alkila, ciklopropila, CF3, OCF3, i CF2CH3; OH, hidroksi-C1-C4-alkila, C1-C4 alkoksi, halo-C1-C4 alkoksi, di-C1-C4-alkilamino-C1-C4-alkila, NR11R12, cijano, C1-C4 alkila, halo-C1-C4 alkila, C3-C6 cikloalkila, C1-C4-alkoksi-C1-C4-alkila, C3-C6 cikloalkil-C1-C4-alkilkarbonila, C6-C10 arilkarbonila, C1-C4-alkilkarboniloksi-C1-C4-alkila, COOR14, SO2R14, (C=O)NR11R12, SO2NR11R12, N(R13)(C=O)NR11R12, N(R13)(C=O)OR14, N(R13)(C=O)R14, O(C=O)NR11R12, O(C=O)OR14, O(C=O)R14, (C=O)OR14, i C6-C10 arila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, C1-C4 alkila, ciklopropila, C1-C4-alkoksikarbonila, (C=O)NR11R12, CF3, OCF3, i CF2CH3; i C3-C6 cikloalkila koji može da sadrži nezasićenje, supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, CF3, OCF3, 5- ili 6-očlanog heteroarila, OH, okso, hidroksi-C1-C4-alkila, C6-C10 arila, COOH, okso, C1-C4-alkoksikarbonila, (C=O)NR11R12, i C1-C4 alkila; R11 i R12 su nezavisno, pri svakom pojavljivanju, odabrani iz grupe koja se sastoji od: H, C1-C4 alkila, halo-C1-C4-alkila, C2-C4 alkenila, -(CR14R14)n1-fenila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, C1-C4 alkila, ciklopropila, CF3, OCF3, 5- ili 6-očlanog heteroarila, OH, OCHF2, di-C1-C4-alkilamino, i cijano, -(CHR13)n1-C3-C6-cikloalkila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, CF3, OCF3, 5- ili 6-očlanog heteroarila, OH, hidroksi-C1-C4-alkila, i C1-C4 alkila, -(CHR13)n1-4- do 10-očlanog-heterociklila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, CF3, OCF3, 5- ili 6-očlanog heteroarila, OH, okso, hidroksi-C1-C4-alkila, i C1-C4 alkila, -(CHR13)n1-5- do 10-očlanog-heteroarila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, CF3, OCF3, 5- ili 6-očlanog heteroarila, OH, hidroksi-C1-C4-alkila, i C1-C4 alkila, di-C1-C4-alkilamino-C1-C4-alkila, di-C1-C4-alkoksi-C1-C4-alkila, hidroksi-C1-C4-alkila, cijano-C1-C4-alkila, C1-C4-alkoksi-C1-C4-alkila, C1-C4-alkoksikarbonil-C1-C4-alkila, C1-C4-alkoksikarbonila, C1-C4-alkilkarbonila, i fenilkarbonila; alternativno, R11 i R12, kada su vezani za isti dušik, kombiniraju se da formiraju 4- do 8-očlani heterociklični prsten koji sadrži atome ugljika supstituirane sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, CF3, CHF2, OCF3, OCHF2, OCH2F, 5- ili 6-očlanog heteroarila, OH, okso, hidroksi-C1-C4-alkila, C1-C4 alkila i C1-C4 alkoksi, i 0 do 2 dodatna heteroatoma odabrana od N, NR13, O i S(O)p; R13 je nezavisno, pri svakom pojavljivanju, odabran iz grupe koja se sastoji od H, i C1-C3 alkila; R14 je nezavisno, pri svakom pojavljivanju, odabran iz grupe koja se sastoji od H, C1-C3 alkila, i halo-C1-C2-alkila; R7 je odabran iz grupe koja se sastoji od H, fluoro, kloro, okso, C1-C3 alkila, hidroksi-C1-C3-alkila, i halo-C1-C2-alkila, koji sadrži 1 do 5 halogena; n1, pri svakom pojavljivanju, je odabrano od 0, 1, 2 ili 3; i p, pri svakom pojavljivanju, je odabrano od 0, 1 i 2.
3. Spoj iz patentnog zahtjeva 1, ili stereoizomer, tautomer, farmaceutski prihvatljiva sol ili solvat istog, gdje: WjeO; R0 je R1; Y je S ili -CH=CH-; R1 je nezavisno odabran iz grupe koja se sastoji od: kloro, CH3, OCH3, SCH3, CHFCH3, i CF2CH3; R2 je H; X1 je CH; X2 i X4 su CH; X3 je CR3; R3 je odabran iz grupe koja se sastoji od OCH3, fluoro, i kloro; R4 i R5 su nezavisno odabrani od H i CH3; je 5-očlani heteroaril prsten odabran od tiazola i oksazola; R6 je odabran iz grupe koja se sastoji od, NR11R12, i C1-C5 alkila supstituiranog sa 0 do 3 grupe nezavisno odabrane od halo, CF3, OCF3, OH, hidroksi-C1-C4-alkila, C1-C4 alkoksi, C1-C4 alkoksi-C1-C4 alkoksi, di-C1-C4-alkilaminofenil-C1-C4-alkila, (di-C1-C4-alkoksi-C1-C4-alkil)-C1-C4-alkila, di-C1-C4-alkilamino, C3-C6-cikloalkila, i C1-C4 alkiltio, ili R6 je B-D-, gdje D je jednostruka veza; B je odabran iz grupe koja se sastoji od: C6-C10 arila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, halo-C1-C4 alkoksi, C1-C4 alkila, halo-C1-C4 alkila, C3-C6 cikloalkila, cijano, nitro, NR11R12, OH, C1-C4-alkilkarboniloksi-C1-C4-alkila, hidroksi-C1-C4-alkila, COOR14, SO2R14, (C=O)NR11R12, SO2NR11R12, N(R13)(C=O)NR11R12, N(R13)(C=O)OR14, N(R13)(C=O)R14, NR13S(O)R14, NR13SO2R14, O(C=O)NR11R12, O(C=O)OR14, O(C=O)R14, (C=O)OR14, i 5-6-očlanog heteroarila, 5- do 10-očlanog heteroarila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, halo-C1-C4 alkoksi, C1-C4 alkila, halo-C1-C4 alkila, C3-C6 cikloalkila, cijano, nitro, NR11R12, OH, C1-C4-alkilkarboniloksi-C1-C4-alkila, hidroksi-C1-C4-alkila, COOR14, SO2R14, (C=O)NR11R12, SO2NR11R12, N(R13)(C=O)NR11R12, N(R13)(C=O)OR14, N(R13)(C=O)R14, NR13S(O)R14, NR13SO2R14, O(C=O)NR11R12, O(C=O)OR14, O(C=O)R14, (C=O)OR14, 5-6-očlanog heteroarila, i (CH2)fenila, 4- do 10-očlanog heterociklila koji sadrži atome ugljika i 1 do 2 dodatna heteroatoma odabrana od N, O, i S, i supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, okso, -(CHR13)n1-5- ili 6-očlanog heteroarila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, C1-C4 alkila, ciklopropila, CF3, OCF3, i CF2CH3; NR13S(O)R14, NR13SO2R14, -(CHR13)n1-4- do 10-očlanog-heterociklila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, C1-C4 alkila, ciklopropila, CF3, OCF3, i CF2CH3; OH, hidroksi-C1-C4-alkila, C1-C4 alkoksi, halo-C1-C4 alkoksi, di-C1-C4-alkilamino-C1-C4-alkila, NR11R12, cijano, C1-C4 alkila, halo-C1-C4 alkila, C3-C6 cikloalkila, C1-C4-alkoksi-C1-C4-alkila, C3-C6 cikloalkil-C1-C4-alkilkarbonila, C6-C10 arilkarbonila, C1-C4-alkilkarboniloksi-C1-C4-alkila, COOR14, SO2R14, (C=O)NR11R12, SO2NR11R12, N(R13)(C=O)NR11R12, N(R13)(C=O)OR14, N(R13)(C=O)R14, O(C=O)NR11R12, O(C=O)OR14, O(C=O)R14, (C=O)OR14, i C6-C10 arila supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, C1-C4 alkoksi, C1-C4 alkila, ciklopropila, C1-C4-alkoksikarbonila, (C=O)NR11R12, CF3, OCF3, i CF2CH3; i C3-C6 cikloalkila koji može da sadrži nezasićenje, supstituiranog sa 0 do 3 grupe nezavisno odabrane iz grupe koja se sastoji od halo, CF3, OCF3, 5- ili 6-očlanog heteroarila, OH, okso, hidroksi-C1-C4-alkila, C6-C10 arila, COOH, okso, C1-C4-alkoksikarbonila, (C=O)NR11R12, i C1-C4 alkila; R11 i R12 su nezavisno, pri svakom pojavljivanju, odabrani iz grupe koja se sastoji od: H, C1-C4 alkila, halo-C1-C4-alkila, di-C1-C4-alkilamino-C1-C4-alkila, di-C1-C4-alkoksi-C1-C4-alkila, hidroksi-C1-C4-alkila, cijano-C1-C4-alkila, C1-C4-alkoksi-C1-C4-alkila, C1-C4-alkoksikarbonil-C1-C4-alkila, i C1-C4-alkoksikarbonila; alternativno, R11 i R12, kada su vezani za isti dušik, kombiniraju se da formiraju 4- do 7-očlani heterociklični prsten koji sadrži atome ugljika supstituirane sa 0 do 2 grupe nezavisno odabrane iz grupe koja se sastoji od halo, CF3, CHF2, OCF3, OCHF2, OCH2F, OH, okso, hidroksi-C1-C2-alkila, C1-C3 alkila i C1-C3 alkoksi, i 0 do 2 dodatna heteroatoma odabrana od N, NR13, O i S(O)p; R13 je nezavisno, pri svakom pojavljivanju, odabran iz grupe koja se sastoji od H, i C1-C3 alkila; R14 je nezavisno, pri svakom pojavljivanju, odabran iz grupe koja se sastoji od H, i C1-C3 alkila R7 je odabran iz grupe koja se sastoji od H, fluoro, kloro, C1-C3 alkila, hidroksi-C1-C3-alkila, i halo-C1-C2-alkila, koji sadrži 1 do 5 halogena; n1, pri svakom pojavljivanju, je odabrano od 0, 1, 2 ili 3; i p, pri svakom pojavljivanju, je odabrano od 0, 1 i 2.
4. Spoj iz patentnog zahtjeva 1 koje ima Formulu:
5. Spoj iz patentnog zahtjeva 1 koje ima Formulu:
6. Spoj iz patentnog zahtjeva 1 koje ima Formulu:
7. Spoj iz patentnog zahtjeva 1 koje ima Formulu:
8. Farmaceutska kompozicija, koja sadrži farmaceutski prihvatljiv nosač i spoj kao što je definirano u bilo kojem od patentnih zahtjeva 1 do 3, ili stereoizomere, tautomere, farmaceutski prihvatljive soli, ili solvate istog, zasebno ili u kombinaciji sa drugim terapijskim agensom.
9. Farmaceutska kompozicija, koja sadrži farmaceutski prihvatljiv nosač i spoj kao što je definirano u bilo kojem od patentnih zahtjeva 4 do 7, zasebno ili u kombinaciji sa drugim terapijskim agensom.
10. Spoj kao što je definirano u bilo kojem od patentnih zahtjeva 1 do 3, ili stereoizomeri, tautomeri, farmaceutski prihvatljive soli, ili solvati istog, za primjenu u terapiji.
11. Spoj kao što je definirano u bilo kojem od patentnih zahtjeva 1 do 3, ili stereoizomeri, tautomeri, farmaceutski prihvatljive soli, ili solvati istog, za primjenu u liječenju tromboembolijskog poremećaja ili primarnoj ili sekundarnoj profilaksi tromboembolijskog poremećaja.
12. Spoj za primjenu kao što je definirano u patentnom zahtjevu 11, gdje je tromboembolijski poremećaj odabran iz grupe koja se sastoji od arterijskih kardiovaskularnih tromboembolijskih poremećaja, venskih kardiovaskularnih tromboembolijskih poremećaja, cerebrovaskularnih tromboembolijskih poremećaja, i tromboembolijskih poremećaja u komorama srca ili u perifernoj cirkulaciji.
13. Spoj kao što je definirano u bilo kojem od patentnih zahtjeva 4 do 7 za primjenu u terapiji.
14. Spoj kao što je definirano u bilo kojem od patentnih zahtjeva 4 do 7 za primjenu u liječenju tromboembolijskog poremećaja ili primarnoj ili sekundarnoj profilaksi tromboembolijskog poremećaja.
15. Spoj za primjenu kao što je definirano u patentnom zahtjevu 14, gdje tromboembolijski poremećaj je odabran iz grupe koja se sastoji od arterijskih kardiovaskularnih tromboembolijskih poremećaja, venskih kardiovaskularnih tromboembolijskih poremećaja, cerebrovaskularnih tromboembolijskih poremećaja, i tromboembolijskih poremećaja u komorama srca ili u perifernoj cirkulaciji.
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