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Tittel PYRAZOLOTHIAZOLE COMPOUND AND MEDICINE COMPRISING SAME
Status
Hovedstatus
Detaljstatus 		I kraft info EP patent gjort gjeldende i Norge EP patent besluttet gjeldende i Norge
Patentnummer NO/EP3190116
Europeisk (EP) publiserings nummer EP3190116
EP levert
EP søknadsnummer 15838466.9
EP meddelt
Prioritet 2014.09.02, JP 2014177969
Sakstype Europeisk
Løpedag
Utløpsdato
Allment tilgjengelig
Validert i Norge
Innehaver Nippon Shinyaku Co., Ltd. (JP)
Oppfinner SHIBA, Yoshinobu (JP) .... se mer/flere nedenfor
Fullmektig BRYN AARFLOT AS (NO)
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Patentkrav1. Pyrazolotiazolforbindelse representert ved formel [I]:hvor,R1 er hydrogen, alkyl eller alkoksy;Z er -OR3 eller -NR4R5;hvoriR3 er alkyl, alkyl substituert med sykloalkyl, sykloalkyl, aryl eller heteroaryl;R4 er hydrogen eller alkyl;R5 er alkyl, sykloalkyl eller mettet heterosyklisk gruppe, nevnte alkyl og sykloalkyl i R5 er eventuelt substituert med én eller to grupper valgt fra gruppen bestående av de følgende (1) til (6):(1) hydroksy,(2) alkoksy, og difluoralkoksy,(3) sykloalkyl, sykloalkyl substituert med (difluoralkoksy)alkyl, og sykloalkyl substituert med alkoksyalkyl,(4) mettet heterosyklisk gruppe eventuelt substituert med (difluoralkoksy)alkyl, (5) aryl, aryl substituert med halogen, og aryl substituert med alkoksy, og(6) nitril, ognevnte mettede heterosykliske gruppe i R5 er eventuelt substituert med én eller to grupper valgt fra gruppen bestående av de følgende (1) til (3):(1) alkyl,(2) alkylkarbonyl, og(3) alkoksykarbonyl;R2 er hydroksy eller -NHR8,hvoriR8 er heteroaryl, heteroaryl substituert med halogen, heteroaryl substituert med alkyl, -COL1, -COOL2 eller -SO2L3, nevnte L1 er en gruppe valgt fra gruppen bestående av de følgende (1) til (5):(1) alkyl, monohaloalkyl, dihaloalkyl, trihaloalkyl, og alkyl substituert med alkoksy, (2) sykloalkyl,(3) aryl,(4) heteroaryl, og(5) dialkylamino, og sykloalkylamino,nevnte L2 er en gruppe valgt fra gruppen bestående av de følgende (1) til (3):(1) alkyl, monohaloalkyl, dihaloalkyl, trihaloalkyl, og alkyl substituert med alkoksy, (2) sykloalkyl, og(3) dialkylaminoalkyl, ognevnte L3 er alkyl eller sykloalkyl,eller farmasøytisk akseptabelt salt derav, eller solvat derav.2. Pyrazolotiazolforbindelse ifølge krav 1 eller farmasøytisk akseptabelt salt derav, eller solvat derav, hvor R1 er hydrogen.3. Pyrazolotiazolforbindelse ifølge krav 2 eller farmasøytisk akseptabelt salt derav, eller solvat derav, hvorZ er -NR4R5;hvoriR4 er hydrogen,R5 er alkyl eller sykloalkyl,nevnte alkyl og sykloalkyl i R5 er eventuelt substituert med en gruppe valgt fra gruppen bestående av de følgende (1) til (3):(1) hydroksy,(2) alkoksy, og(3) sykloalkyl,R2 er hydroksy eller -NHR8,R8 er heteroaryl, heteroaryl substituert med halogen, heteroaryl substituert med alkyl, -COL1 eller -COOL2,nevnte L1 er en gruppe valgt fra gruppen bestående av de følgende (1) til (4):(1) alkyl, monohaloalkyl, dihaloalkyl, trihaloalkyl, og alkyl substituert med alkoksy, (2) sykloalkyl,(3) aryl, og(4) heteroaryl, ognevnte L2 er alkyl, monohaloalkyl, dihaloalkyl, trihaloalkyl, alkyl substituert med alkoksy eller sykloalkyl. 4. Pyrazolotiazolforbindelse ifølge krav 3 eller farmasøytisk akseptabelt salt derav, eller solvat derav, hvorR5 er alkyl, alkyl substituert med hydroksy, alkyl substituert med syklopropyl eller alkyl substituert med alkoksy, ogR2 er -NHR8.5. Pyrazolotiazolforbindelse ifølge krav 3 eller farmasøytisk akseptabelt salt derav, eller solvat derav, hvorR5 er alkyl som har 2 til 6 karbon atoms eller alkyl substituert med syklopropyl, R2 er -NHR8,R8 er -COL1 eller -COOL2,nevnte L1 er alkyl som har 2 til 6 karbon atoms eller syklopropyl,ognevnte L2 er alkyl eller syklopropyl.6. Pyrazolotiazolforbindelse ifølge krav 1, som er hvilken som helst av de følgende (1) til (135):(1) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(2) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)acetamid,(3) N-(1-{[6-{[(2S)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(4) N-(1-{[6-{[(2S)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)acetamid,(5) N-(1-{[6-{[(1S,2S)-2-(difluormetoksy)syklopentyl](metyl)amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(6) N-(1-{[6-{[(2S)-3,3-dimetylbutan-2-yl]amino}-5-metyl-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)acetamid,(7) N-(1-{[6-{[(2S)-3,3-dimetylbutan-2-yl]amino}-5-metyl-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid, (8) N-[1-({6-[({1-[(difluormetoksy)metyl]syklopropyl}metyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid, (9) N-[1-({6-[({1-[(difluormetoksy)metyl]syklobutyl}metyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid, (10) N-[1-({6-[({1-[(difluormetoksy)metyl]syklopentyl}metyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid,(11) N-[1-({6-[({4-[(difluormetoksy)metyl]tetrahydro-2H-pyran-4-yl}metyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid,(12) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-5-metyl-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid, (13) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-5-metyl-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)acetamid,(14) N-(1-{[6-{[(1S,2S)-2-(difluormetoksy)syklopentyl]amino}-2-(pyrazolo[5,1-b] [1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid, (15) N-[1-({6-[(2,2-dimetylpropyl)amino]-2-(pyrazolo[5,1-b] [1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid,(16) N-(1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(17) N-(1-{[6-{[(2S)-1-(difluormetoksy)propan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid, (18) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-5-metyl-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)-2,2-difluoracetamid, (19) N-(1-{[6-{[(1S,2S)-2-metoksysyklopentyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(20) [6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl](4-hydroksypiperidin-1-yl)metanon,(21) 1-fluoro-2-metylpropan-2-yl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat, (22) metyl (1-{[6-{[(2S)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(23) [6-{[(2S)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl](4-hydroksypiperidin-1-yl)metanon,(24) metyl (1-{[6-{[(2R)-3-metylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(25) metyl (1-{[6-{[(2S)-3-metylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(26) metyl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat, (27) etyl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(28) propan-2-yl (1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(29) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)benzamid,(30) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)pyridin-3-karboksamid,(31) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)tiofen-2-karboksamid,(32) N-(1-{[6-{[(1S)-1-syklopropyletyl](metyl)amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(33) 1-syklopropyl-3-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)urea,(34) [6-{[(1S)-1-syklopropyletyl](metyl)amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl][4-(pyrimidin-2-ylamino)piperidin-1-yl]metanon,(35) N-(1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(36) N-[1-({6-[(1-metylsyklopropyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid,(37) N-[1-({6-[(1-metoksy-2-metylpropan-2-yl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid,(38) metyl (1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(39) etyl (1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(40) propan-2-yl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(41) N-(1-{[6-{[(1S)-1-syklopropyletyl](metyl)amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)benzamid,(42) N-(1-{[6-(syklopropylmetoksy)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(43) N-[1-({6-[(3,3-dimetylbutan-2-yl)oksy]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid,(44) N-(1-{[6-(syklobutyloksy)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid, (45) N-(1-{[6-(syklopentyloksy)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(46) N-(1-{[6-{[(1R)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(47) N-[1-({6-[(1-hydroksy-2-metylpropan-2-yl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid,(48) [6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl][4-(1,2-oksazol-3-ylamino)piperidin-1-yl]metanon,(49) [6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl][4-(1,3-tiazol-2-ylamino)piperidin-1-yl]metanon,(50) [6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]{4-[(3-metyl-1,2-oksazol-5-yl)amino]piperidin-1-yl}metanon,(51) N-(1-{[6-{[(2S)-1-hydroksy-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid, (52) [6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl](4-hydroksypiperidin-1-yl)metanon,(53) metyl (1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(54) propan-2-yl (1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(55) metyl [1-({6-[(1-hydroksy-2-metylpropan-2-yl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(56) [6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl](4-hydroksypiperidin-1-yl)metanon,(57) metyl (1-{[6-{[(2S)-1-hydroksy-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(58) metyl [1-({6-[(3,3-dimetylbutan-2-yl)oksy]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(59) metyl (1-{[6-(syklobutyloksy)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(60) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)metansulfonamid,(61) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropanesulfonamid,(62) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)etansulfonamid, (63) N-(1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b] [1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)-2-metylpropanamid,(64) N-(1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b] [1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)-2,2-difluoracetamid,(65) etyl (1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b] [1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(66) [6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl][4-(pyridin-2-ylamino)piperidin-1-yl]metanon,(67) etyl (1-{[6-{[(1R)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(68) [6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl][4-(1,3-tiazol-2-ylamino)piperidin-1-yl]metanon,(69) [6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl][4-(pyrimidin-2-ylamino)piperidin-1-yl]metanon,(70) metyl [1-({6-[(2-metylbutan-2-yl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(71) (4-hydroksypiperidin-1-yl)[6-(pentan-3-ylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]metanon,(72) propyl (1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(73) propyl (1-{[6-{[(1R)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(74) propyl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(75) propyl (1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(76) propyl (1-{[6-{[(2S)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(77) metyl [1-({6-[(2,2-dimetylpropyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(78) 2-metoksyetyl (1-{[6-{[(1R)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(79) 2-metoksyetyl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(80) 2-metoksyetyl (1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat, (81) 2-metoksyetyl (1-{[6-{[(2S)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(82) N-(1-{[6-{[(1R)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)-2-metoksyacetamid,(83) N-(1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)-2-metoksyacetamid,(84) metyl [1-({6-[{[1-(metoksymetyl)syklopropyl]metyl}(metyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat, (85) 2,2-difluoroetyl (1-{[6-{[(1R)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(86) 2,2-difluoroetyl (1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(87) 2,2-difluoroetyl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(88) 2,2-difluoroetyl (1-{[6-{[(2S)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(89) tert-butyl (1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(90) 2-metoksyetyl (1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(91) 2-(dimetylamino)etyl (1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat, (92) 2,2,2-trifluoroetyl (1-{[6-{[(1R)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(93) 2,2,2-trifluoroetyl (1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(94) 2-metoksy-N-(1-{[6-(pentan-3-ylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)acetamid,(95) N-(1-{[6-(2-etylbutoksy)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(96) metyl (1-{[6-(pentan-3-yloksy)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(97) metyl (1-{[6-(pentan-3-ylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(98) N-[1-({6-[(2-etylbutyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid, (99) N-(1-{[6-(pentan-3-yloksy)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(100) metyl [1-({6-[metyl(pentan-3-yl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(101) metyl (1-{[6-{[(2R)-3,3-dimetylbutan-2-yl](metyl)amino}-2-(pyrazolo[5,1-b] [1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(102) N-(1-{[6-(2-etylbutoksy)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)propanamid,(103) N-(1-{[6-{[(2R)-3,3-dimetylbutan-2-yl](metyl)amino}-2-(pyrazolo[5,1-b] [1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)propanamid,(104) N-[1-({6-[metyl(pentan-3-yl)amino]-2-(pyrazolo[5,1-b] [1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]propanamid,(105) [6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]{4-[(3-fluoropyridin-2-yl)amino]piperidin-1-yl}metanon, (106) N-[1-({6-[(2-metoksy-2-metylpropyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]propanamid,(107) (4-hydroksypiperidin-1-yl){6-[metyl(pentan-3-yl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}metanon,(108) N-(1-{[6-{[(2R)-3-metylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)propanamid,(109) N-(1-{[6-{[(2R)-3-metylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(110) N-(1-{[6-{[(2S)-3-metylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(111) N-(1-{[6-(pentan-3-ylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(112) metyl [1-({6-[(2S)-butan-2-ylamino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(113) metyl [1-({6-[(2R)-butan-2-ylamino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(114) N-[1-({6-[(1-metylsyklopropyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]propanamid,(115) [6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]{4-[(5-fluoropyridin-2-yl)amino]piperidin-1-yl}metanon, (116) 2-metyl-N-[1-({6-[(2-metylbutan-2-yl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]propanamid, (117) N-[1-({6-[(2S)-butan-2-ylamino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]propanamid,(118) metyl [1-({6-[tert-butyl(metyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(119) syklopropyl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(120) syklopropyl (1-{ [6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(121) 2,2-difluoro-N-(1-{[6-{[(2R)-3-metylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)acetamid,(122) 3-[1-({6-[(2,2-dimetylpropyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]-1,1-dimetylurea,(123) 3-(1-{[6-{[(1R)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)-1,1-dimetylurea,(124)propan-2-yl [1-({6-[(3-metyloksetan-3-yl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(125) metyl [1-({6-[(disyklopropylmetyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(126) metyl (1-{[6-phenoksy-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(127) tert-butyl 4-{[6-({4-[(metoksykarbonyl)amino]piperidin-1-yl}karbonyl)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]amino}piperidine-1-carboksylate, (128) metyl (1-{[6-(piperidin-4-ylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(129) metyl [1-({6-[(1-cyanosyklopropyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(130) metyl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-5-metoksy-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(131) metyl (1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-5-metoksy-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(132) metyl [1-({6-[(2S)-butan-2-ylamino]-5-metoksy-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(133) metyl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-5-etoksy-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(134) metyl (1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-5-etoksy-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat, og (135) metyl (1-{[2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)-6-(pyridin-3-yloksy)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,eller farmasøytisk akseptabelt salt derav, eller solvat derav.7. Pyrazolotiazolforbindelse ifølge krav 1 som er hvilken som helst av de følgende (1) til (58):(1) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(2) N-(1-{[6-{[(2S)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(3) N-(1-{[6-{[(1S,2S)-2-(difluormetoksy)syklopentyl](metyl)amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(4) N-(1-{[6-{[(2S)-3,3-dimetylbutan-2-yl]amino}-5-metyl-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid, (5) N-[1-({6-[({1-[(difluormetoksy)metyl]syklopropyl}metyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid, (6) N-[1-({6-[({1-[(difluormetoksy)metyl]syklobutyl}metyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid, (7) N-[1-({6-[({1-[(difluormetoksy)metyl]syklopentyl}metyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid, (8) N-[1-({6-[({4-[(difluormetoksy)metyl]tetrahydro-2H-pyran-4-yl}metyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid,(9) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-5-metyl-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(10) N-(1-{[6-{[(1S,2S)-2-(difluormetoksy)syklopentyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid, (11) N-[1-({6-[(2,2-dimetylpropyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid,(12) N-(1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(13) N-(1-{[6-{[(2S)-1-(difluormetoksy)propan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid, (14) metyl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat, (15) etyl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(16) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)benzamid,(17) N-(1-{[6-{[(1S)-1-syklopropyletyl](metyl)amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(18) propan-2-yl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(19) N-(1-{[6-(syklopropylmetoksy)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(20) N-[1-({6-[(3,3-dimetylbutan-2-yl)oksy]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid,(21) N-(1-{[6-(syklobutyloksy)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(22) N-[1-({6-[(1-hydroksy-2-metylpropan-2-yl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid,(23) [6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl][4-(1,3-tiazol-2-ylamino)piperidin-1-yl]metanon,(24) N-(1-{[6-{[(2S)-1-hydroksy-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid, (25) metyl (1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(26) propan-2-yl (1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(27) metyl [1-({6-[(1-hydroksy-2-metylpropan-2-yl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(28) [6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl](4-hydroksypiperidin-1-yl)metanon,(29) metyl (1-{[6-{[(2S)-1-hydroksy-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(30) metyl [1-({6-[(3,3-dimetylbutan-2-yl)oksy]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(31) metyl (1-{[6-(syklobutyloksy)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(32) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropanesulfonamid, (33) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)etansulfonamid,(34) etyl (1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(35) [6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl][4-(pyridin-2-ylamino)piperidin-1-yl]metanon,(36) propyl (1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(37) N-(1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)-2-metoksyacetamid,(38) 2,2-difluoroetyl (1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(39) 2,2-difluoroetyl (1-{[6-{[(2S)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(40) tert-butyl (1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(41) 2-metoksyetyl(1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(42) 2-(dimetylamino)etyl(1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat, (43) 2,2,2-trifluoroetyl(1-{[6-{[(1R)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(44) 2,2,2-trifluoroetyl(1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(45) metyl(1-{[6-(pentan-3-yloksy)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(46) N-[1-({6-[(2-etylbutyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]syklopropankarboksamid,(47) N-(1-{[6-(pentan-3-yloksy)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(48) metyl[1-({6-[(2S)-butan-2-ylamino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(49) metyl[1-({6-[(2R)-butan-2-ylamino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(50) N-[1-({6-[(1-metylsyklopropyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]propanamid, (51) metyl[1-({6-[tert-butyl(metyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(52) syklopropyl(1-{[6-(tert-butylamino)-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(53) propan-2-yl[1-({6-[(3-metyloksetan-3-yl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(54) metyl[1-({6-[(1-cyanosyklopropyl)amino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(55) metyl[1-({6-[(2S)-butan-2-ylamino]-5-metoksy-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat,(56) metyl(1-{[6-{[(1S)-1-syklopropyletyl]amino}-5-etoksy-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(57) metyl(1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-5-etoksy-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat, og(58) metyl(1-{[2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)-6-(pyridin-3-yloksy)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,eller farmasøytisk akseptabelt salt derav, eller solvat derav.8. Pyrazolotiazolforbindelse ifølge krav 1 som er hvilken som helst av de følgende (1) til (8):(1) N-(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(2) N-(1-{[6-{[(2R)-3,3-dimetylbutan-2-yl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(3) metyl(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(4) etyl(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(5) N-(1-{[6-{[(1S)-1-syklopropyletyl](metyl)amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)syklopropankarboksamid,(6) propan-2-yl(1-{[6-{[(1S)-1-syklopropyletyl]amino}-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl]karbonyl}piperidin-4-yl)karbamat,(7) metyl[1-({6-[(2S)-butan-2-ylamino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat, og(8) metyl[1-({6-[(2R)-butan-2-ylamino]-2-(pyrazolo[5,1-b][1,3]tiazol-7-yl)pyrimidin-4-yl}karbonyl)piperidin-4-yl]karbamat, eller farmasøytisk akseptabelt salt derav, eller solvat derav.9. Farmasøytisk sammensetning som omfatter en pyrazolotiazolforbindelse eller farmasøytisk akseptabelt salt derav eller solvat derav ifølge hvilket som helst av kravene 1 til 8 som et virkestoff.10. Pyrazolotiazolforbindelse eller farmasøytisk akseptabelt salt derav eller solvat derav ifølge hvilket som helst av kravene 1 til 8 for anvendelse som en JAK1-hemmer.11. Pyrazolotiazolforbindelse eller farmasøytisk akseptabelt salt derav eller solvat derav ifølge hvilket som helst av kravene 1 til 8 for anvendelse som et terapeutisk middel for en inflammatorisk sykdom.12. Pyrazolotiazolforbindelse for anvendelse ifølge krav 11, hvor den inflammatoriske sykdommen er atopisk dermatitt, eksem, bronkial astma, eosinofil lungebetennelse, kronisk obstruktiv lungesykdom, allergisk rhinitt, eosinofil sinusitt, nesepolypp, ankyloserende spondylitt eller eosinofil øsofagitt.13. Pyrazolotiazolforbindelse eller farmasøytisk akseptabelt salt derav eller solvat derav ifølge hvilket som helst av kravene 1 til 8 for anvendelse i behandling av en autoimmun sykdom.14. Pyrazolotiazolforbindelse for anvendelse ifølge krav 13, hvor den autoimmune sykdommen er revmatoid artritt, psoriasisartritt, juvenil artritt, Castlemans sykdom, systemisk lupus erythematosus, Sjögrens syndrom, inflammatorisk tarmsykdom, psoriasis, sklerodermi, tørt øye, Takayasus arteritt, mikroskopisk polyangiitt, granulomatose med polyangiitt, eosinofil granulomatose med polyangiitt eller neuromyelitis optica.15. Pyrazolotiazolforbindelse eller farmasøytisk akseptabelt salt derav eller solvat derav ifølge hvilket som helst av kravene 1 til 8 for anvendelse som et terapeutisk middel for en proliferativ sykdom.16. Pyrazolotiazolforbindelse for anvendelse ifølge krav 15, hvor den proliferative sykdommen er solide kreftformer, blodkreft, ondartet lymfekreft, myeloproliferative sykdommer, multippelt myelom, pulmonal fibrose eller eosinofili. 17. Pyrazolotiazolforbindelse eller farmasøytisk akseptabelt salt derav eller solvat derav ifølge hvilket som helst av kravene 1 til 8 for anvendelse i behandling av diabetisk nefropati, alopecia areata, avvisning av benmargstransplantasjon eller avvisning av organtransplantasjon.
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SHIBA, Yoshinobu
c/o NIPPON SHINYAKU CO. LTD.14 Kisshoin Nishinosho MonguchichoMinami-ku Kyoto-shiKyoto 601-8550 JP
AKIYAMA, Satoshi
c/o NIPPON SHINYAKU CO. LTD.14 Kisshoin Nishinosho MonguchichoMinami-ku Kyoto-shiKyoto 601-8550 JP

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2014.09.02, JP 2014177969

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