HRP20110465T1 - Modulatori aktivnosti receptora kemokina, kristalni oblici i postupak - Google Patents

Modulatori aktivnosti receptora kemokina, kristalni oblici i postupak Download PDF

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HRP20110465T1
HRP20110465T1 HR20110465T HRP20110465T HRP20110465T1 HR P20110465 T1 HRP20110465 T1 HR P20110465T1 HR 20110465 T HR20110465 T HR 20110465T HR P20110465 T HRP20110465 T HR P20110465T HR P20110465 T1 HRP20110465 T1 HR P20110465T1
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disease
crystalline form
compound according
form according
pharmaceutically acceptable
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H. Carter Percy
V. Duncia John
M. Mudryk Boguslaw
E. Randazzo Michael
Xiao Zili
G. Yang Michael
Zhao Rulin
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Bristol-Myers Squibb Company
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Abstract

Spoj N-((1R,2S,5R)-5-(tert-butilamino)-2-((S)-2-okso-3-(6-(trifluorometil)kinazolin-4-ilamino)pirolidin-1-il)cikloheksil)acetamid, ili njegova farmaceutski prihvatljiva sol. Patent sadrži još 11 patentnih zahtjeva.

Claims (12)

1. Spoj N-((1R,2S,5R)-5-(tert-butilamino)-2-((S)-2-okso-3-(6-(trifluorometil)kinazolin-4-ilamino)pirolidin-1-il)cikloheksil)acetamid, ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema zahtjevu 1 koji je kristalni oblik N-((1R,2S,5R)-5-(tert-butilamino)-2-((S)-2-okso-3-(6-(trifluorometil)kinazolin-4-ilamino)pirolidin-1-il)cikloheksil)acetamida, ili njegove farmaceutski prihvatljive soli.
3. Kristalni oblik prema zahtjevima 1-2, naznačen time što su parametri jedinične ćelije u biti jednaki sljedećima: Dimenzije ćelije: a = 18.7240(4) b= 8.0171(2) c = 19.6568(5) α = 90 β = 114.935(2) γ = 90 V(Å3) = 2675.7(1) Prostorna grupa P212121 Molekula/jedinična ćelija 2 pri čemu je taj kristal pri temperaturi od oko +22 ̊C (RT).
4. Kristalni oblik prema zahtjevima 1-3, naznačen time što obrazac difrakcije rendgenskog zračenja na prašku obuhvaća tri ili više 2θ vrijednosti (CuKα λ=1.5418 Å) izabrane između 5.5, 9.1, 12.1, 14.0 i 19.2, pri temperaturi od oko 22 ̊C.
5. Kristalni oblik prema zahtjevima 1-4, dalje naznačen time što obrazac difrakcije rendgenskog zračenja na prašku obuhvaća četiri ili više 2θ values (CuKα λ=1.5418 Å) izabrane između 5.5, 9.1, 12.1, 14.0 i 19.2 pri temperaturi od oko 22 ̊C.
6. Kristalni oblik prema zahtjevima 1-5, naznačen time što su frakcijske atomske koordinate u biti onakve kako su navedene u Tablici 3.
7. Kristalni oblik prema zahtjevima 1-6 čiji je obrazac difrakcije rendgenskog zračenja na prašku u biti onakav kao što je prikazano na Slici 2.
8. Farmaceutska smjesa koja sadrži spoj prema zahtjevima 1-7, i farmaceutski prihvatljiv nosač ili punilo.
9. Spoj prema zahtjevima 1-8 za uporabu u liječenju bolesti kod sisavaca, pri čemu se ta bolest izabire između dijabetesa, pretilosti, metaboličkog sindroma, moždanog udara, neuropatske boli, ishemijske kardiomiopatije, psorijaze, hipertenzije, skleroderme, osteoartritisa, aneurizme, povišene temperature, kardiovaskularne bolesti, Crohnove bolesti, kongestivnog zatajenja srca, autoimunih bolesti, HIV-zaraze, demencije povezane s HIV-om, psorijaze, idiopatske plućne fibroze, arterioskleroze transplantata, fizički ili kemijski inducirane traume mozga, inflamatorne bolesti crijeva, alveolitisa, kolitisa, sistemskog lupusa eritematosusa, nefrotoksičnog serumskog nefritisa, glomerulonefritisa, astme, multiple skleroze, ateroskleroze, vaskulitisa, vulnerabilnog plaka, reumatoidnog artritisa, restenoze, venske neointimalne hiperplazije, dijaliza-graft neointimalne hiperplazije, arterio-venske shunt intimalne hiperplazije, transplantacije organa, kronične nefropatije alografta i raka.
10. Spoj prema zahtjevu 9 pri čemu se bolest izabire između dijabetesa, pretilosti, Crohnove bolesti, sistemskog lupusa eritematosusa, glomerulonefritisa, multiple skleroze, ateroskleroze, restenoze i transplantacije organa.
11. Spoj prema zahtjevima 9-10 pri čemu se bolest izabire između multiple skleroze, ateroskleroze, Crohnove bolesti i dijabetesa.
12. Farmaceutska smjesa prema zahtjevu 8 koja dalje sadrži jednu ili više drugih djelatnih tvari.
HR20110465T 2006-07-28 2011-06-20 Modulatori aktivnosti receptora kemokina, kristalni oblici i postupak HRP20110465T1 (hr)

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US83423506P 2006-07-28 2006-07-28
US89602607P 2007-03-21 2007-03-21
US11/782,742 US7629351B2 (en) 2006-07-28 2007-07-25 N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino) pyrrolidin-1-yl)cyclohexyl)acetamide and other modulators of chemokine receptor activity, crystalline forms and process
PCT/US2007/074377 WO2008014360A2 (en) 2006-07-28 2007-07-26 Modulators of chemokine receptor activity, crystalline forms and process

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US (2) US7629351B2 (hr)
EP (2) EP2046779B1 (hr)
JP (1) JP5236643B2 (hr)
KR (1) KR20090033915A (hr)
CN (1) CN101535301B (hr)
AR (1) AR062124A1 (hr)
AT (2) ATE522522T1 (hr)
AU (1) AU2007279333B2 (hr)
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EA (1) EA016563B1 (hr)
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HR (1) HRP20110465T1 (hr)
IL (2) IL196427A (hr)
MX (1) MX2009000808A (hr)
NO (1) NO20090190L (hr)
NZ (1) NZ574425A (hr)
PE (1) PE20080732A1 (hr)
PL (1) PL2046779T3 (hr)
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CA2831219A1 (en) 2008-01-31
US7629351B2 (en) 2009-12-08
US20100113489A1 (en) 2010-05-06
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WO2008014360A2 (en) 2008-01-31
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CN101535301A (zh) 2009-09-16
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