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1. 发明申请

WO2013055645A1 5,7-SUBSTITUTED-IMIDAZO[1,2-C]PYRIMIDINES 审中-公开
标题翻译： 5,7-取代的咪唑并[1,2-C]嘧啶类
公开(公告)号：WO2013055645A1
公开(公告)日：2013-04-18
申请号：PCT/US2012/059282
申请日：2012-10-09
申请人： ARRAY BIOPHARMA INC. , BOYS, Mark Laurence , BURGESS, Laurence E. , EARY, C. Todd , GRONEBERG, Robert , HACHE, Bruno P. , HARVEY, Darren , HICKEN, Erik James , KRASER, Christopher F. , LAIRD, Ellen , MORENO, David A. , MUNSON, Mark C. , REN, Li , ROBINSON, John E. , SCHLACHTER, Stephen T.
发明人： BOYS, Mark Laurence , BURGESS, Laurence E. , EARY, C. Todd , GRONEBERG, Robert , HACHE, Bruno P. , HARVEY, Darren , HICKEN, Erik James , KRASER, Christopher F. , LAIRD, Ellen , MORENO, David A. , MUNSON, Mark C. , REN, Li , ROBINSON, John E. , SCHLACHTER, Stephen T.
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00 , A61P37/00
CPC分类号： C07D487/04
摘要： Compounds of Formula I: and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X 1 and X 2 have the meanings given in the specification, are inhibitors of one or more JAK kinases and are useful in the treatment of autoimmune diseases, inflammatory diseases, rejection of transplanted organs, tissues and cells, as well as hematologic disorders and malignancies and their co-morbidities.
摘要翻译： R 1，R 2，R 3，R 4，R 5，R 6，X 1和X 2具有本说明书中给出的含义的式I化合物及其立体异构体及其药学上可接受的盐和溶剂合物是一种或多种JAK激酶的抑制剂，并且是有用的治疗自身免疫性疾病，炎症性疾病，移植器官，组织和细胞排斥，以及血液系统疾病和恶性肿瘤及其并发症。

2. 发明申请

WO2007002157A3 PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS 审中-公开
公开(公告)号：WO2007002157A3
公开(公告)日：2007-01-04
申请号：PCT/US2006/024084
申请日：2006-06-21
申请人： ARRAY BIOPHARMA INC. , ASTRAZENECA AB , DEMATTEI, John , SHAKYA, Sagar , PISCOPIO, Anthony, D. , HACHE, Bruno, P. , EVANS, Matthew, Charles , FORD, James, Gair , POINTON, Simon, Mark , PEETERS, Koen , LILLEY, Timothy, John , LEONARD, John
发明人： DEMATTEI, John , SHAKYA, Sagar , PISCOPIO, Anthony, D. , HACHE, Bruno, P. , EVANS, Matthew, Charles , FORD, James, Gair , POINTON, Simon, Mark , PEETERS, Koen , LILLEY, Timothy, John , LEONARD, John
IPC分类号： C07D403/02
摘要： Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X 1 , X 2 , X 5 , R 2 and R 10 are as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

3. 发明申请

WO2007002092A1 SNAr PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS 审中-公开
标题翻译：用于制备苯并咪唑化合物的SNAr方法
公开(公告)号：WO2007002092A1
公开(公告)日：2007-01-04
申请号：PCT/US2006/023986
申请日：2006-06-21
申请人： ARRAY BIOPHARMA INC. , ASTRAZENECA AB , DEMATTEI, John , SHAKYA, Sagar , NICHOLS, Paul, J. , BARNETT, Bradley, R. , HACHE, Bruno, P. , EVANS, Matthew, Charles , FORD, James, Gair , LEONARD, John
发明人： DEMATTEI, John , SHAKYA, Sagar , NICHOLS, Paul, J. , BARNETT, Bradley, R. , HACHE, Bruno, P. , EVANS, Matthew, Charles , FORD, James, Gair , LEONARD, John
IPC分类号： A61K31/4164 , C07D235/04
CPC分类号： C07D235/08 , C07D235/06
摘要： Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-2 and their synthetic intermediates: wherein X 1 , X 2 , X 5 , R 1 , R 2 and R 4 are as defined herein. Compounds of Formula Ia-2 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
摘要翻译：提供了合成杂环化合物的方法，例如具有式Ia-2的苯并咪唑羧酸核心结构及其合成中间体：其中X 1，X 2，X 2 R 5，R 1，R 2和R 4如本文所定义。式Ia-2及其合成中间体的化合物可用于制备杂环衍生物如苯并咪唑衍生物。

4. 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。

5. 发明申请

WO2017201241A1 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 审中-公开
标题翻译：（S）-N-（5 - （（R）-2-（2,5-二氟苯基）吡咯烷-1-基）吡唑并[1,5-a]嘧啶-3-基）-3-羟基吡咯烷 - -1-甲酰胺
公开(公告)号：WO2017201241A1
公开(公告)日：2017-11-23
申请号：PCT/US2017/033257
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： 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.
摘要翻译：制备（S）-N-（5 - （（R）-2-（2,5-二氟苯基）吡咯烷-1-基）吡唑并[1,5-a]嘧啶-4 （5 - （（R）-2-（2,5-二氟苯基）吡咯烷-1-基）-3,3a（三唑-3-基）-3-羟基吡咯烷-1-甲酰胺（式I）或其盐 - 二氢吡唑并[1,5-a]嘧啶-3-基）氨基甲酸叔丁酯或类似衍生物（式13）与（S） - 吡咯烷-3-醇（式14）（5 - （（R）-2-（2,5-二氟苯基）吡咯烷-1-基）-3,3a-二氢吡唑并[1,5-a]嘧啶-3-基）氨基甲酸酯（式13 ）或（R）-5-（2-（2,5-二氟苯基）吡咯烷-1-基）-3-硝基吡唑并[1,5-a]嘧啶（式11）还原成（R） -5-（2-（2,5-二氟苯基）吡咯烷-1-基）吡唑并[1,5-a]嘧啶-3-胺（式12）。通过处理（R）-N - （（R）-1-（2,5-二氟苯基）吡咯烷（R）-2-羟基琥珀酸盐（式10） -3-（1,3-二恶烷-2-基）丙基）-2-甲基丙烷-2-亚磺酰胺（式19）与酸和还原剂反应。（S）-N-（5 - （（R）-2-（2,5-二氟苯基） - 吡咯烷-1-基） - 吡唑并[1,5-a]嘧啶-3-基）-3-羟基吡咯烷-3-甲酸 1-甲酰胺是酪氨酸激酶（TRK）抑制剂，用于处理例如，癌症

6. 发明申请

WO2007002157A2 PROCESS FOR PREPARING BENZIMIDAZOLE COMPOUNDS 审中-公开
标题翻译：制备苯并咪唑化合物的方法
公开(公告)号：WO2007002157A2
公开(公告)日：2007-01-04
申请号：PCT/US2006024084
申请日：2006-06-21
申请人： ARRAY BIOPHARMA INC , ASTRAZENECA AB , DEMATTEI JOHN , SHAKYA SAGAR , PISCOPIO ANTHONY D , HACHE BRUNO P , EVANS MATTHEW CHARLES , FORD JAMES GAIR , POINTON SIMON MARK , PEETERS KOEN , LILLEY TIMOTHY JOHN , LEONARD JOHN
发明人： DEMATTEI JOHN , SHAKYA SAGAR , PISCOPIO ANTHONY D , HACHE BRUNO P , EVANS MATTHEW CHARLES , FORD JAMES GAIR , POINTON SIMON MARK , PEETERS KOEN , LILLEY TIMOTHY JOHN , LEONARD JOHN
IPC分类号： A61K31/4184
CPC分类号： C07D235/06 , C07C201/08 , C07C205/58 , C07C227/04 , C07C227/08 , C07C227/18 , C07C229/60
摘要： Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X 1 , X 2 , X 5 , R 2 and R 10 are as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
摘要翻译：提供了用于合成杂环化合物的方法，例如具有式Ia-1的苯并咪唑羧酸核心结构及其合成中间体：其中Z，X 1，X 2，X，X 如本文所定义，R 2和R 10分别如本文所定义。式Ia-1化合物及其合成中间体可用于制备杂环衍生物如苯并咪唑衍生物。

7. 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.

8. 发明专利

IL223313A Benzimidazoles 未知
公开(公告)号：IL223313A
公开(公告)日：2015-07-30
申请号：IL22331312
申请日：2012-11-28
申请人： ASTRAZENECA AB , ARRAY BIOPHARMA INC , LEONARD JOHN , DEMATEI JOHN , SHAKYA SAGAR , EVANS MATTHEW CHARLES , FORD JAMES GAIR , PISCOPIO ANTHONY D , HACHE BRUNO P , POINTON SIMON MARK , PEETERS KOEN , LILLEY TIMOTHY JOHN
发明人： LEONARD JOHN , DEMATEI JOHN , SHAKYA SAGAR , EVANS MATTHEW CHARLES , FORD JAMES GAIR , PISCOPIO ANTHONY D , HACHE BRUNO P , POINTON SIMON MARK , PEETERS KOEN , LILLEY TIMOTHY JOHN
IPC分类号： C07D20060101
摘要： Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X5, R2b, R2c and R10 are as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.

9. 发明专利

IL188273A Process for preparing benzimidazole compounds comprising single step cyclisation 未知
公开(公告)号：IL188273A
公开(公告)日：2015-03-31
申请号：IL18827307
申请日：2007-12-19
申请人： ASTRAZENECA AB , ARRAY BIOPHARMA INC , LEONARD JOHN , DEMATEI JOHN , SHAKYA SAGAR , EVANS MATTHEW CHARLES , FORD JAMES GAIR , PISCOPIO ANTHONY D , HACHE BRUNO P , POINTON SIMON MARK , PEETERS KOEN , LILLEY TIMOTHY JOHN
发明人： LEONARD JOHN , DEMATEI JOHN , SHAKYA SAGAR , EVANS MATTHEW CHARLES , FORD JAMES GAIR , PISCOPIO ANTHONY D , HACHE BRUNO P , POINTON SIMON MARK , PEETERS KOEN , LILLEY TIMOTHY JOHN
IPC分类号： C07D20060101
摘要： Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X5, R2b, R2c and R10 are as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.

10. 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.

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