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1. 发明申请

US20060040923A1 Benzodiazepine derivatives and pharmaceutical compositions containing them 失效
公开(公告)号：US20060040923A1
公开(公告)日：2006-02-23
申请号：US10528250
申请日：2003-09-22
申请人： Malcolm Carter , Elisa Henderson , Richard Kelsey , Lara Wilson , Phil Chambers , Debra Taylor , Stan Tyms
发明人： Malcolm Carter , Elisa Henderson , Richard Kelsey , Lara Wilson , Phil Chambers , Debra Taylor , Stan Tyms
IPC分类号： A61K31/5513 , C07D243/12
CPC分类号： C07D401/12 , C07D243/24 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV. Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; —each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, —CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; —n is from 0 to 3; R4 represents hydrogen or C1-6 alkyl; —R6 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— or, —XR6; —X represents —CO—, —S(O)— or —S(O)2—; and —R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6 hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6 hydroxyalkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.

2. 发明授权

US08853204B2 Pharmaceutical composition comprising a benzodiazepine derivative and an inhibitor of the RSV fusion protein 有权
标题翻译：药物组合物，其包含苯并二氮杂衍生物和RSV融合蛋白的抑制剂
公开(公告)号：US08853204B2
公开(公告)日：2014-10-07
申请号：US10593666
申请日：2005-03-18
申请人： Kenneth Powell , Richard Kelsey , Malcolm Carter , Dagmar Alber , Lara Wilson , Elisa Henderson , Phil Chambers , Debra Taylor , Stan Tyms , Verity Dowdell
发明人： Kenneth Powell , Richard Kelsey , Malcolm Carter , Dagmar Alber , Lara Wilson , Elisa Henderson , Phil Chambers , Debra Taylor , Stan Tyms , Verity Dowdell
IPC分类号： A01N43/62 , A61K31/55 , A01N43/52 , A61K31/415 , C07D243/24 , C07D235/04 , A61K45/06 , A61K31/5513
CPC分类号： A61K45/06 , A61K31/5513 , A61K2300/00
摘要： A pharmaceutical composition which comprises a pharmaceutically acceptable carrier or diluent and: (a) an inhibitor of the RSV fusion protein; and (b) a benzodiazepine derivative capable of inhibiting RSV replication is found to be highly active against RSV.
摘要翻译：一种药物组合物，其包含药学上可接受的载体或稀释剂，和：（a）RSV融合蛋白的抑制剂; 发现能够抑制RSV复制的苯并二氮杂衍生物对RSV具有高度活性。

3. 发明申请

US20100015063A1 Benzodiazepine Derivatives and Pharmaceutical Compositions Containing Them 失效
公开(公告)号：US20100015063A1
公开(公告)日：2010-01-21
申请号：US12476797
申请日：2009-06-02
申请人： Malcolm Carter , Elisa Henderson , Richard Kelsey , Lara Wilson , Phil Chambers , Debra Taylor , Stan Tyms
发明人： Malcolm Carter , Elisa Henderson , Richard Kelsey , Lara Wilson , Phil Chambers , Debra Taylor , Stan Tyms
IPC分类号： A61K9/12 , A61K38/20 , A61K31/56 , A61K31/5513 , C07D243/24
CPC分类号： C07D401/12 , C07D243/24 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; -each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; -n is from 0 to 3; R4 represents hydrogen or C1-6 alkyl; —R6 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— or, —XR6; —X represents —CO—, —S(O)— or —S(0)2—; and —R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6 hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6 hydroxyalkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.

4. 发明申请

US20070142403A1 Pharmaceutical composition comprising a benzodiazepine derivative and an inhibitor of the rsv fusion protein 有权
公开(公告)号：US20070142403A1
公开(公告)日：2007-06-21
申请号：US10593666
申请日：2005-03-18
申请人： Kenneth Powell , Richard Kelsey , Malcolm Carter , Dagmar Alber , Lara Wilson , Elisa Henderson , Phil Chambers , Debra Taylor , Stan Tyms , Verity Dowdell
发明人： Kenneth Powell , Richard Kelsey , Malcolm Carter , Dagmar Alber , Lara Wilson , Elisa Henderson , Phil Chambers , Debra Taylor , Stan Tyms , Verity Dowdell
IPC分类号： A01N43/90
CPC分类号： A61K45/06 , A61K31/5513 , A61K2300/00
摘要： A pharmaceutical composition which comprises a pharmaceutically acceptable carrier or diluent and: (a) an inhibitor of the RSV fusion protein; and (b) a benzodiazepine derivative capable of inhibiting RSV replication is found to be highly active against RSV.

5. 发明授权

US08119630B2 Benzodiazepine derivatives and pharmaceutical compositions containing them 失效
公开(公告)号：US08119630B2
公开(公告)日：2012-02-21
申请号：US12476797
申请日：2009-06-02
申请人： Malcolm Carter , Elisa Henderson , Richard Kelsey , Lara Wilson , Phil Chambers , Debra Taylor , Stan Tyms
发明人： Malcolm Carter , Elisa Henderson , Richard Kelsey , Lara Wilson , Phil Chambers , Debra Taylor , Stan Tyms
IPC分类号： A61P31/12
CPC分类号： C07D401/12 , C07D243/24 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; -each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; -n is from 0 to 3; R4 represents hydrogen or C1-6 alkyl; —R6 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— or, —XR6; —X represents —CO—, —S(O)— or —S(0)2—; and —R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6 hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6 hydroxyalkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.

6. 发明授权

US07582624B2 Benzodiazepine derivatives and pharmaceutical compositions containing them 失效
公开(公告)号：US07582624B2
公开(公告)日：2009-09-01
申请号：US10528250
申请日：2003-09-22
申请人： Malcolm Carter , Philip Chambers , Verity Dowdell , Elisa Ann Henderson , Richard David Kelsey , Debra Taylor , Stanley Tyms , Lara Wilson
发明人： Malcolm Carter , Philip Chambers , Verity Dowdell , Elisa Ann Henderson , Richard David Kelsey , Debra Taylor , Stanley Tyms , Lara Wilson
IPC分类号： C07D243/24 , C07D409/12 , C07D405/12 , C07D403/12 , A61K31/5513
CPC分类号： C07D401/12 , C07D243/24 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV. Formula (I) Wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; —each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, —CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; —n is from 0 to 3; R4 represents hydrogen or C1-6 alkyl; —R6 represents C1-6 alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— or, —XR6; —X represents —CO—, —S(O)— or —S(O)2—; and —R6 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6 hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6 hydroxyalkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-.

7. 发明申请

US20080139536A1 Benzodiazepines for Treating or Preventing Rsv Infection 审中-公开
公开(公告)号：US20080139536A1
公开(公告)日：2008-06-12
申请号：US10593667
申请日：2005-03-18
申请人： Verity Dowdell , Richard Kelsey , Malcolm Carter , Dagmar Alber , Elisa Henderson
发明人： Verity Dowdell , Richard Kelsey , Malcolm Carter , Dagmar Alber , Elisa Henderson
IPC分类号： A61K31/5513 , C07D243/24 , A61P31/12
CPC分类号： C07D403/12 , A61K31/5513 , C07D243/24 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/14 , C07D413/12 , C07D417/14 , Y02A50/385 , Y02A50/387 , Y02A50/393
摘要： Use of a compound which is (a) a benzodiazepine derivative of the formula (I) or an N-oxide thereof or (b) a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing an RSV infection wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6alkyl)amino, vitro, cyano, —CO2R′, —CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″, wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; n is from O to 3; R4 represents hydrogen or C1-6 alkyl; X represents —CO—, —CO—NR′—, —S(O)— or —S(O)2—, wherein R′ is hydrogen or a C1-C6 alkyl group; and R5 represents a heteroaryl or heterocyclyl group which is substituted by a C1C6 hydroxyalkyl group or a —(C1-C4 alkyl)-X1—(C1-C4 alkyl)-X2—(C1-C4 alkyl} group, wherein X1 represents -0-, —S— or —NR′—, wherein R′ represents H or a C1-C4 alkyl group and X2 represents —CO—, —SO— or —SO2—, or R5 represents -A1-Y-A2, wherein: -A1 is an aryl, heteroaryl, carbocyclyl or heterocyclyl group; 25 —Y represents a direct bond or a C1-C4 alkylene, —SO2—, —CO—, -0-, —S— or —NR′-moiety, wherein R′ is a C1-C6 alkyl group; and -A2 is an aryl, heteroaryl, carbocyclyl or heterocyclyl group.

8. 发明申请

US20070185096A1 Pharmaceutical composition comprising a benzodiazepine derivative and an inhibitor of the rsv fusion protein 审中-公开
标题翻译：药物组合物，其包含苯并二氮杂衍生物和rsv融合蛋白的抑制剂
公开(公告)号：US20070185096A1
公开(公告)日：2007-08-09
申请号：US10593382
申请日：2005-03-18
申请人： Kenneth Powell , Richard Kelsey , Malcolm Carter , Verity Dowdell , Dagmar Alber , Elisa Henderson
发明人： Kenneth Powell , Richard Kelsey , Malcolm Carter , Verity Dowdell , Dagmar Alber , Elisa Henderson
IPC分类号： A61K31/55
CPC分类号： A61K45/06 , A61K31/5513 , A61K2300/00
摘要： A pharmaceutical composition which comprises a pharmaceutically acceptable carrier or diluent and: (a) an inhibitor of the RSV fusion protein; and (b) a benzodiazepine derivative capable of inhibiting RSV replication is found to be highly active against RSV.
摘要翻译：一种药物组合物，其包含药学上可接受的载体或稀释剂，和：（a）RSV融合蛋白的抑制剂; 发现能够抑制RSV复制的苯并二氮杂衍生物对RSV具有高度活性。

9. 发明申请

US20070293482A1 Process for Preparing Benzodiazepines 审中-公开
公开(公告)号：US20070293482A1
公开(公告)日：2007-12-20
申请号：US10593665
申请日：2005-03-21
申请人： Verity Dowdell , Richard Kelsey , Malcolm Carter , Elisa Henderson
发明人： Verity Dowdell , Richard Kelsey , Malcolm Carter , Elisa Henderson
IPC分类号： A61K31/5513 , A61P31/12 , C07D243/24 , C07D243/26
CPC分类号： C07D243/24 , Y02P20/55
摘要： A process for producing a compound which is a benzodiazepine derivative of formula: (I) wherein: represents or R1 represents C1-6 alkyl, aryl or heteroaryl; each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R′, —CONR′R″, —NH—CO—R′, —S(O)R′, —S(O)2R′, —NH—S(O)2R′, —S(O)NR′R″ or —S(O)2NR′R″, wherein each R′ and R″ is the same or different and represents hydrogen or C1-6 alkyl; n is from 0 to 3; X represents —NH—, —N(C1-C6alkyl)-, —CO—, —CO—NR′—, —S(O)— or —S(O)2—, wherein R′ is hydrogen or a C1-C6 alkyl group; and R4 represents hydrogen; or —CO—R4′ or —CO—NH—R4 ′, wherein R4 ′ is a C1-C6 alkyl, C1-C6 hydroxyalkyl, aryl, heteroaryl, carbocyclyl or heterocyclyl group, which group is substituted by a C1-C6 hydroxyalkyl, aryl, heteroaryl, carbocyclyl or heterocyclyl group or a —(C1-C4 alkyl)-X1—(C1-C4 alkyl)-X2—(C1-C4 alkyl) group, wherein X1 represents —O—, —S— or —NR′—, wherein R′ represents H or a C1-C4 alkyl group and X2 represents —CO—, —SO— or —SO2—; or R4 ′represents -A1-Y-A2, wherein: A1 is an aryl, heteroaryl, carbocyclyl or heterocyclyl group; Y represents a direct bond or a C1-C4 alkylene, —SO2—, —CO—, —O—, —S or —NR′—, wherein R′ is a C1-C6 alkyl group; and A2 is an aryl, heteroaryl, carbocyclyl or heterocyclyl group; or R4 is a group selected from aryl-C(O)—C(O)—, heteroaryl-C(O)—C(O)—, carbocyclyl-C(O)—C(O)—, heterocyclyl-C(O)—C(O)— and -ZR5, wherein: Z represents —CO—, —S(O)— or —S(O)2′; and R5 represents C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkylthio, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 alkyl)-O—, heteroaryl-(C1-6 alkyl)-O—, carbocyclyl-(C1-6 alkyl)-O—, heterocyclyl-(C1-6 alkyl)-O— or —NR′R″ wherein each R′ and R″ is the same or different and represents hydrogen, C1-6 alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)- or heterocyclyl-(C1-6 alkyl)-; or a pharmaceutically acceptable salt thereof; which process comprises: (a) subjecting a racemic benzodiazepine derivative of formula: (IIa): wherein R1, R3, R4, n and X are as defined above, and R2 represents an amino protecting group, to crystallisation induced dynamic resolution to yield a benzodiazepine derivative of formula (II): wherein, R1, R2, R3, R4, n and X are as defined above; and (b) deprotecting the benzodiazepine derivative of formula (II) as defined above to yield a benzodiazepine derivative of formula (I) or a pharmaceutically acceptable form thereof as defined above.

10. 发明申请

US20050130996A1 Heterocyclic compounds 有权
标题翻译：杂环化合物
公开(公告)号：US20050130996A1
公开(公告)日：2005-06-16
申请号：US11050033
申请日：2005-02-03
申请人： Malcolm Carter , George Cockerill , Stephen Guntrip , Karen Lackey , Kathryn Smith
发明人： Malcolm Carter , George Cockerill , Stephen Guntrip , Karen Lackey , Kathryn Smith
IPC分类号： A61K31/47 , A61K31/4709 , A61K31/505 , A61K31/517 , A61K31/519 , A61P9/10 , A61P17/06 , A61P29/00 , A61P35/00 , A61P43/00 , C07D221/00 , C07D239/00 , C07D239/94 , C07D405/04 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D45/02
CPC分类号： A61K31/517 , C07D239/94 , C07D405/04 , C07D405/14 , C07D411/04 , C07D417/04 , C07D417/14 , C07D471/04
摘要： A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) wherein L and L′ are suitable leaving groups, with a compound of formula (III) UNH2 (III) to prepare a compound of formula (IV) and subsequently (b) substituting the group R1 by replacement of the leaving group L′.
摘要翻译：一种制备式（I）化合物的方法，包括步骤：（a）使其中L和L'是合适的离去基团的式（II）化合物与式（III）化合物反应， line-formula description =“In-line Formulas”end =“lead”？> UNH （III）<？in-line-formula description =“In-line Formulas”end =“tail” 制备式（IV）的化合物，随后（b）用R'取代基取代离去基团L'。

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