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1. 发明专利

SG11201810245WA PREPARATION OF (S)-N-(5-((R)-2-(2,5-DIFLUOROPHENYL)PYRROLIDIN-1-YL)PYRAZOLO[1,5-A]PYRIMIDIN-3-Y L)-3-HYDROXYPYRROLIDINE-1-CARBOXAMIDE 未知
公开(公告)号：SG11201810245WA
公开(公告)日：2018-12-28
申请号：SG11201810245W
申请日：2017-05-18
申请人： REYNOLDS MARK , EARY CHARLES TODD , SPENCER STACEY , JUENGST DERRICK , HACHE BRUNO , JIANG YUTONG , HAAS JULIA , ANDREWS STEVEN W
发明人： REYNOLDS MARK , EARY CHARLES TODD , SPENCER STACEY , JUENGST DERRICK , HACHE BRUNO , JIANG YUTONG , HAAS JULIA , ANDREWS STEVEN W
IPC分类号： A61K31/5025 , C07D487/04 , A61P35/00
摘要： Process for preparing (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a] pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide (formula I) or a salt thereof by reacting phenyl(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-3,3a-dihydropyrazolo[1,5-a]pyrimidin-3-yl)carbamate or a similar derivative (formula 13) with (S)-pyrrolidin-3-ol (formula 14).Process for preparing phenyl(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-3,3a-dihydropyrazolo[1,5-a]pyrimidin-3-yl)carbamate (formula 13) or a similar derivative by reduction of (R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)-3-nitropyrazolo[1,5-a]pyrimidine (formula 11) to (R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-amine (formula 12).Process for preparing (R)-2-(2,5-difluorophenyl)pyrrolidine(R)-2-hydroxysuccinate (formula 10) by treating (R)-N-((R)-1-(2,5-difluorophenyl)-3-(1,3-dioxan-2-yl)propyl)-2-methylpropane-2-sulfinamide (formula 19) with an acid and a reducing agent.(S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-l-yl)-pyrazolo[l,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, is a tyrosin kinase (TRK) inhibitor for trearing e.g. cancer.

2. 发明专利

CA3024603A1 PROCESS FOR THE PREPARATION OF (S)-N-(5-((R)-2-(2,5-DIFLUOROPHENYL)PYRROLIDIN-1-YL)-PYRAZOLO[1,5-A]PYRIMIDIN-3-YL)-3-HYDROXYPYRROLIDINE-1-CARBOXAMIDE AND SALTS THEREOF 未知
公开(公告)号：CA3024603A1
公开(公告)日：2017-11-23
申请号：CA3024603
申请日：2017-05-18
申请人： EARY CHARLES TODD , REYNOLDS MARK , SPENCER STACEY , JUENGST DERRICK , HACHE BRUNO , JIANG YUTONG , HAAS JULIA , ANDREWS STEVEN W
发明人： EARY CHARLES TODD , REYNOLDS MARK , SPENCER STACEY , JUENGST DERRICK , HACHE BRUNO , JIANG YUTONG , HAAS JULIA , ANDREWS STEVEN W , REYNOLDS MARK , SPENCER STACEY , JUENGST DERRICK , HACHE BRUNO , JIANG YUTONG , HAAS JULIA , ANDREWS STEVEN W
IPC分类号： C07D487/04 , A61K31/5025 , A61P35/00
摘要： Process for preparing (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-l- yl)pyrazolo[l,5-a] pyrimidin-3-yl)-3-hydroxypyrrolidine-l-carboxamide (formula I) or a salt thereof by reacting phenyl(5-((R)-2-(2,5- difluorophenyl)pyrrolidin-l-yl)-3,3a-dihydropyrazolo[l,5-a]pyrimidin-3- yl)carbamate or a similar derivative (formula 13) with (S)-pyrrolidin-3- ol (formula 14). Process for preparing phenyl(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-l- yl)-3,3a-dihydropyrazolo[l,5-a]pyrimidin-3-yl)carbamate (formula 13) or a similar derivative by reduction of (R)-5-(2-(2,5-difluorophenyl) pyrrolidin-l-yl)-3-nitropyrazolo[l,5-a]pyrimidine (formula 11) to (R) -5-(2-(2,5-difluorophenyl)pyrrolidin-l-yl)pyrazolo[l,5-a]pyrimidin-3- amine (formula 12). Process for preparing (R)-2-(2,5-difluorophenyl)pyrrolidine(R) -2-hydroxysuccinate (formula 10) by treating (R)-N-((R)-l-(2,5- difluorophenyl)-3-(l,3-dioxan-2-yl)propyl)-2-methylpropane-2- sulfinamide (formula 19) with an acid and a reducing agent. (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-l-yl)-pyrazolo[l,5- a]pyrimidin-3-yl)-3-hydroxypyrrolidine-l-carboxamide, is a tyrosin kinase (TRK) inhibitor for trearing e.g. cancer.

3. 发明申请

WO0250082A3 INHIBITORS OF PAPILLOMA VIRUS 审中-公开
标题翻译： PAPILLOMA病毒的抑制剂
公开(公告)号：WO0250082A3
公开(公告)日：2002-12-19
申请号：PCT/CA0101800
申请日：2001-12-14
申请人： BOEHRINGER INGELHEIM CA LTD , YOAKIM CHRISTIANE , HACHE BRUNO , OGILVIE WILLIAM W , O'MEARA JEFFREY , WHITE PETER , GOUDREAU NATHALIE
发明人： YOAKIM CHRISTIANE , HACHE BRUNO , OGILVIE WILLIAM W , O'MEARA JEFFREY , WHITE PETER , GOUDREAU NATHALIE
IPC分类号： A61K31/34 , A61K31/343 , A61K31/36 , A61K31/381 , A61K31/407 , A61K31/4245 , A61K31/428 , A61K31/4725 , A61K31/5377 , A61P31/12 , A61P31/20 , C07D307/94 , C07D405/12 , C07D407/10 , C07D407/12 , C07D407/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D491/04 , C07D491/107 , C07D493/04 , C07D493/10 , C07D495/10 , C07D495/12 , C07D495/14 , C07D495/20
CPC分类号： C07D405/12 , C07D307/94 , C07D407/12 , C07D407/14 , C07D413/12 , C07D417/12 , C07D491/04 , C07D493/04 , C07D493/10 , C07D495/12
摘要： A compound of formula (I) or its enantiomers or diastereoisomers thereof:wherein: A is a 5- or 6-membered homocyclic ring, or a 5- or 6-membered heterocyclic ring containing 1 or more heteroatoms; X is H and W is OH; or X and W together form a carbonyl group or an epoxide; R1 is H; or one or two substituents; Y is phenyl optionally mono- or di-substituted, said phenyl ring being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; or Y is a heterocycle (Het) containing one or more heteroatoms, said Het optionally mono- or di-substituted, said Het being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; or Y is ethylene-phenyl, said ethylene moiety being optionally mono-substituted, wherein said phenyl ring is optionally mono- or di-substituted, said phenyl ring being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; or Y is ethylene-Het, said ethylene moiety being optionally mono-substituted, wherein Het is optionally mono- or di-substituted; said Het being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; R3 is selected from the group consisting of: lower alkyl, lower cycloalkyl, lower alkylene, aryl or lower aralkyl, all of which optionally mono- or di-substituted, said lower cycloalkyl, aryl, lower aralkyl or Het being optionally fused with a saturated or unsaturated 4 to 6-membered ring optionally containing a heteroatom; and R4 is a carboxylic acid, a salt or an ester thereof.The compounds of the invention may be used as inhibitors of the papilloma virus E1-E2-DNA complex. The invention further provides a method of treating or preventing human papilloma virus infection.
摘要翻译：式（I）化合物或其对映异构体或非对映异构体：其中：A为5-或6-元级环，或含有1个或多个杂原子的5或6元杂环; X是H，W是OH; 或X和W一起形成羰基或环氧化物; R1是H; 或一个或两个取代基; Y是任选被一或二取代的苯基，所述苯环任选地与任选地含有杂原子的饱和或不饱和的4至6元环稠合; 或Y是含有一个或多个杂原子的杂环（Het），所述Het任选地被单取代或二取代，所述Het任选地与任选地含有杂原子的饱和或不饱和的4至6元环稠合; 或Y是乙烯 - 苯基，所述乙烯部分任选被单取代，其中所述苯环任选被一或二取代，所述苯环任选与饱和或不饱和的4至6元环稠合，任选地含有杂原子 ; 或Y是乙烯-Het，所述乙烯部分任选是单取代的，其中Het任选被一或二取代; 所述Het任选地与任选地含有杂原子的饱和或不饱和的4至6元环稠合; R 3选自：低级烷基，低级环烷基，低级亚烷基，芳基或低级芳烷基，所有这些可任选被一或二取代，所述低级环烷基，芳基，低级芳烷基或Het任选地与饱和的或任选含有杂原子的不饱和4至6元环; 并且R 4是羧酸，其盐或酯。本发明的化合物可以用作乳头瘤病毒E1-E2-DNA复合物的抑制剂。本发明还提供了治疗或预防人乳头状瘤病毒感染的方法。

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