【WO2019209908A1】达沙替尼的晶型【专利】

) (

(51)International Patent Classification:MG,MK,MN,MW,MX,MY,MZ,NA,NG,NI,NO,NZ,

C07D417/12(2006.01)A61K31/506(2006.01)OM,PA,PE,PG,PH,PL,PT,QA,RO,RS,RU,RW,SA, A61P35/02(2006.01)SC,SD,SE,SG,SK,SL,SM,ST,SV,SY,TH,TJ,TM,TN,

TR,TT,TZ,UA,UG,US,UZ,VC,VN,ZA,ZM,ZW. (21)International Application Number:

PCT/US2019/028853(84)Designated States(unless otherwise indicated,for every

kind o f regional protection available).ARIPO(BW,GH, (22)International Filing Date:

GM,KE,LR,LS,MW,MZ,NA,RW,SD,SL,ST,SZ,TZ,

24April2019(24.04.2019)

UG,ZM,ZW),Eurasian(AM,AZ,BY,KG,KZ,RU,TJ,

(25)Filing Language:English TM),European(AL,AT,BE,BG,CH,CY,CZ,DE,DK,

EE,ES,FI,FR,GB,GR,HR,HU,IE,IS,IT,LT,LU,LV, (26)Publication Language:English MC,MK,MT,NL,NO,PL,PT,RO,RS,

SE,SI,SK,SM, (30)Priority Data:TR),OAPI(BF,BJ,CF,CG,Cl,CM,GA,GN,GQ,GW,

62/662,37925April2018(25.04.2018)US KM,ML,MR,NE,SN,TD,TG).

(71)Applicant:JOHNSON MATTHEY PUBLIC LIMITED Declarations under Rule4.17:

COMPANY[GB/GB];5th Floor,25Farringdon Street,

—o f inventorship(Rule4.17(iv))

London EC4A4AB(GB).

Published:

(72)Inventor;and—with international search report

(Art.21(3))

(71)Applicant:KAVURU,Padmini[US/US];124Turner—before the expiration o f the time limit for amending the

Road,Townsend,MA01469(US).claims and to be republished in the event o f receipt o f (74)Agent:PARKER,Raymond,S.;c/o Johnson Matthey amendments(Rule48.2(h))

Inc.,435Devon Park Drive;Suite600,Wayne,PA19087

(US).

(81)Designated States(unless otherwise indicated,for every

kind o f national protection available):AE,AG,AL,AM,

AO,AT,AU,AZ,BA,BB,BG,BH,BN,BR,BW,BY,BZ,

CA,CH,CL,CN,CO,CR,CU,CZ,DE,DJ,DK,DM,DO,

DZ,EC,EE,EG,ES,FI,GB,GD,GE,GH,GM,GT,HN,

HR,HU,ID,IL,IN,IR,IS,JO,JP,KE,KG,KH,KN,KP,

KR,KW,KZ,LA,LC,LK,LR,LS,LU,LY,MA,MD,ME,

(54)Title:CRYSTALLINE FORMS OF DASATINIB

(57)Abstract:The present disclosure relates to a dasatinib co-crystal form comprising dasatimb and a second compound,also referred

to as a co-crystal former,wherein the second compound is selected from buty1paraben.propyl paraben and ethyl vanillin.The present disclosure is also related to an ethyl formate solvate form of dasatinib.The present disclosure is also related to processes for the preparation of the dasatinib co-crystal and solvate form of dasatinib.Further,the present disclosure also relates to pharmaceutical compositions comprising the dasatinib co-crystal and solvate form of dasatinib and methods for treating disease using the dasatinib co-crvstal and solvate form of dasatinib.