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1. 发明授权

US06255326B1 Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic-or heteroatom-containing linking group 失效
标题翻译：含有通过含脂肪族或含杂原子的连接基与芳基或杂芳基连接的苯基的化合物
公开(公告)号：US06255326B1
公开(公告)日：2001-07-03
申请号：US09239075
申请日：1999-01-27
申请人： Michael John Ashton , David Charles Cook , Garry Fenton , Susan Jacqueline Hills , Ian Michael McFarlane , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher , Nigel Vicker
发明人： Michael John Ashton , David Charles Cook , Garry Fenton , Susan Jacqueline Hills , Ian Michael McFarlane , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher , Nigel Vicker
IPC分类号： C07D21172
CPC分类号： C07C43/225 , C07C45/004 , C07C45/292 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/58 , C07C59/60 , C07C59/62 , C07C65/21 , C07C65/24 , C07C65/26 , C07C65/42 , C07C69/76 , C07C69/92 , C07C205/59 , C07C217/88 , C07C235/56 , C07C255/57 , C07C255/60 , C07C275/34 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/42 , C07C327/48 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07D213/50 , C07D213/75 , C07D213/89 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/03 , C07D409/12
摘要： This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
摘要翻译：本发明涉及通过各种连接与芳基部分连接的用于抑制肿瘤坏死因子的苯基化合物的药物用途。本发明还涉及含有这些化合物的化合物及其制备方法和药物组合物。此外，本发明涉及化合物抑制环AMP磷酸二酯酶的药物用途。

2. 发明授权

US6096768A Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic- or heteroatom-containing linking group 有权
标题翻译：含有通过含脂肪族或含杂原子的连接基与芳基或杂芳基连接的苯基的化合物
公开(公告)号：US6096768A
公开(公告)日：2000-08-01
申请号：US301877
申请日：1999-04-29
申请人： Michael John Ashton , David Charles Cook , Garry Fenton , Susan Jacqueline Hills , Ian Michael McFarlane , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher , Nigel Vicker
发明人： Michael John Ashton , David Charles Cook , Garry Fenton , Susan Jacqueline Hills , Ian Michael McFarlane , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher , Nigel Vicker
IPC分类号： C07C65/21 , C07C65/24 , C07C65/26 , C07C65/42 , C07C69/76 , C07C69/92 , C07C235/56 , C07C255/60 , C07C311/46 , C07C323/42 , C07D213/75 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/02 , C07D275/03 , A61K31/435 , A61K31/165 , A61K31/44 , A61K31/4523 , C07D211/72
CPC分类号： C07D213/75 , C07C235/56 , C07C255/60 , C07C311/46 , C07C323/42 , C07C65/21 , C07C65/24 , C07C65/26 , C07C65/42 , C07C69/76 , C07C69/92 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/03 , C07C2101/08 , C07C2101/14 , C07C2102/42
摘要： This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
摘要翻译：本发明涉及通过各种连接与芳基部分连接的用于抑制肿瘤坏死因子的苯基化合物的药物用途。本发明还涉及含有这些化合物的化合物及其制备方法和药物组合物。此外，本发明涉及化合物抑制环AMP磷酸二酯酶的药物用途。

3. 发明授权

US5935978A Compounds containing phenyl linked to aryl or heteroaryl by an aliphatic- or heteroatom-containing linking group 失效
公开(公告)号：US5935978A
公开(公告)日：1999-08-10
申请号：US98178
申请日：1993-07-28
申请人： Garry Fenton , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher , Michael John Ashton , David Charles Cook , Susan Jacqueline Hills , Ian Michael McFarlane , Nigel Vicker
发明人： Garry Fenton , Andrew David Morley , Malcolm Norman Palfreyman , Andrew James Ratcliffe , Brian William Sharp , Sukanthini Thurairatnam , Bernard Yvon Jack Vacher , Michael John Ashton , David Charles Cook , Susan Jacqueline Hills , Ian Michael McFarlane , Nigel Vicker
IPC分类号： C07C43/225 , C07C45/00 , C07C45/29 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/58 , C07C59/60 , C07C59/62 , C07C65/21 , C07C65/24 , C07C65/42 , C07C69/76 , C07C69/92 , C07C205/59 , C07C217/88 , C07C235/56 , C07C255/57 , C07C255/60 , C07C275/34 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/42 , C07C327/48 , C07D213/50 , C07D213/75 , C07D213/89 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/02 , C07D275/03 , C07D409/12 , A61K31/44
CPC分类号： C07D213/75 , C07C205/59 , C07C217/88 , C07C235/56 , C07C255/57 , C07C255/60 , C07C275/34 , C07C311/29 , C07C311/46 , C07C317/40 , C07C323/42 , C07C327/48 , C07C43/225 , C07C45/004 , C07C45/292 , C07C45/71 , C07C47/575 , C07C49/84 , C07C59/58 , C07C59/60 , C07C59/62 , C07C65/21 , C07C65/24 , C07C65/42 , C07C69/76 , C07C69/92 , C07D213/50 , C07D213/89 , C07D239/42 , C07D241/20 , C07D261/14 , C07D275/03 , C07D409/12 , C07C2101/08 , C07C2101/14 , C07C2102/42
摘要： This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.

4. 发明授权

US07132419B2 Pharmaceutical compounds 失效
公开(公告)号：US07132419B2
公开(公告)日：2006-11-07
申请号：US11024759
申请日：2004-12-30
申请人： John Milton , Nigel Vicker , Adrian Folkes , Shouming Wang , William Alexander Denny
发明人： John Milton , Nigel Vicker , Adrian Folkes , Shouming Wang , William Alexander Denny
IPC分类号： C07D241/46 , A61K31/498
CPC分类号： C07D403/12 , C07D241/46
摘要： A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R1 to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1–C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1–C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2R11, SO2N(R12)2, N(R12)2, NR10SO2R11, N(SO2R11)2 NR10(CH2)nCN, NR10COR11, OCOR11 or COR10; each of R5 to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1–C6 alkoxy, C1–C6 alkyl, SR10 and N(R12)2; Q is C1–C6 alkylene which is unsubstituted or substituted by (i) C1–C6 alkyl which is unsubstituted or substituted, (ii) hydroxy, provided that the hydroxy group is not α to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12); R8 and R9, which are the same or different, are each hydrogen or C1–C6 alkyl, or R8 and R9 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered N-containing heterocyclic ring which may include one additional heteroatom selected from O, N and S, or one of R8 and R9 is an alkylene chain optionally interrupted by O, N or S, which is attached to a carbon atom on the alkylene chain represented by Q to complete a saturated 5- or 6-membered N-containing heterocyclic ring as defined above; R10 is hydrogen, C1–C6 alkyl, C3–C6 cycloalkyl, benzyl or phenyl; R11 is C1–C6 alkyl, C3–C6 cycloalkyl, benzyl or phenyl; each R12, which are the same or different, is hydrogen, C1–C6 alkyl cycloalkyl, benzyl or phenyl, or the two R12 groups form, together with the nitrogen atom to which they are attached a 5- or 6-membered saturated N-containing heterocyclic ring which may include 1 or 2 additional heteroatoms selected from O, N and S; and n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; with the proviso that at least one of R1 to R4 is other than hydrogen. These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR.

5. 发明申请

US20050143383A1 Pharmaceutical compounds 失效
公开(公告)号：US20050143383A1
公开(公告)日：2005-06-30
申请号：US11024759
申请日：2004-12-30
申请人： John Milton , Nigel Vicker , Adrian Folkes , Shouming Wang , William Denny
发明人： John Milton , Nigel Vicker , Adrian Folkes , Shouming Wang , William Denny
IPC分类号： C07D241/46 , C07D403/12 , A61K31/498 , C07D241/36
CPC分类号： C07D403/12 , C07D241/46
摘要： A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R1 to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1-C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1-C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2R11, SO2N(R12)2, N(R2)2, NR10SO2R11, N(SO2R11)2 NR10(CH2)nCN, NR10COR11, OCOR11 or COR10; each of R5 to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1-C6 alkoxy, C1-C6 alkyl, SR10 and N(R12)2; Q is C1-C6 alkylene which is unsubstituted or substituted by (i) C1-C6 alkyl which is unsubstituted or substituted, (II) hydroxy, provided that the hydroxy group is not α to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12); R8 and R9, which are the same or different, are each hydrogen or C1-C6 alkyl, or R8 and R9 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered N-containing heterocyclic ring which may include one additional heteroatom selected from O, N and S, or one of R8 and R9 is an alkylene chain optionally interrupted by O, N or S, which is attached to a carbon atom on the alkylene chain represented by Q to complete a saturated 5- or 6-membered N-containing heterocyclic ring as defined above; R10 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, benzyl or phenyl; R11 is C1-C6 alkyl, C3-C6 cycloalkyl, benzyl or phenyl; each R12, which are the same or different, is hydrogen, C1-C6 alkyl cycloalkyl, benzyl or phenyl, or the two R12 groups form, together with the nitrogen atom to which they are attached a 5- or 6-membered saturated N-containing heterocyclic ring which may include 1 or 2 additional heteroatoms selected from O, N and S; and n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; with the proviso that at least one of R1 to R4 is other than hydrogen. These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR.

6. 发明申请

US20110112151A1 COMPOUND CAPABLE OF INHIBITING 11-BETA HYDROXYSTERIOD DEHYDROGENASE 审中-公开
标题翻译：抑制11-β羟化酶脱氢酶的化合物
公开(公告)号：US20110112151A1
公开(公告)日：2011-05-12
申请号：US12919707
申请日：2009-02-25
申请人： Nigel Vicker , Xiangdong Su , Fabienne Pradaux-Caggiano , Barry Victor Lioyd Potter
发明人： Nigel Vicker , Xiangdong Su , Fabienne Pradaux-Caggiano , Barry Victor Lioyd Potter
IPC分类号： A61K31/44 , A61K31/4406 , A61K31/4402 , A61K31/4196 , A61K31/4184 , A61K31/4164 , C07D213/82 , C07D213/71 , C07D213/70 , C07D213/50 , C07D249/12 , C07D235/28 , C07D233/42 , A61P19/02 , A61P3/10 , A61P35/00 , A61P3/04 , A61P19/10 , A61P9/12 , A61P37/00 , A61P11/06
CPC分类号： C07D233/84 , C07D213/30 , C07D213/32 , C07D213/34 , C07D213/50 , C07D213/61 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/80 , C07D213/82 , C07D213/89 , C07D235/28 , C07D249/12 , C07D257/04 , C07D285/125 , C07D285/135 , C07D405/04 , C07D409/04
摘要： There is provided a compound of formula R1—CO—X—Y—Z—R2 wherein X and Z are each optional groups that are, independently, saturated or unsaturated carbon chains having a length of 1 to 3 carbons; Y is SO, S, SO2, CH═CH, CH2CH2 or O; R1 is wherein denotes the point of attachment; R2 is a heteroaryl group comprising an optionally substituted 5 or 6 membered ring, which ring contains only carbon and at least one nitrogen, or contains only carbon, and at least two nitrogens and at least one sulfur; and wherein (i) when R1 is and —CO—X—Y—Z— is CO—CH2—SO, CO—CH2—S, or CO—CH2—SO2, R2 is other than and; (ii) when R1 is and —CO—X—Y—Z— is —CO—CH2—O—, R2 is other than
摘要翻译：提供式R1-CO-X-Y-Z-R2的化合物，其中X和Z各自是任选的基团，独立地是具有1至3个碳原子的长度的饱和或不饱和碳链; Y是SO，S，SO 2，CH = CH，CH 2 CH 2或O; R1是其中表示连接点; R2是包含任选取代的5或6元环的杂芳基，该环仅含有碳和至少一个氮，或仅含有碳，以及至少两个氮和至少一个硫; 并且其中（i）当R 1为和-CO-X-Y-Z-为CO-CH 2 -SO，CO-CH 2 -S或CO-CH 2 -SO 2时，（ii）当R 1为-CO-X-Y-Z-为-CO-CH 2 -O-时，R 2为

7. 发明申请

US20100286204A1 COMPOUND CAPABLE OF INHIBITING 17-BETA HYDROXYSTERIOD DEHYDROGENASE 失效
标题翻译：抑制17-β羟化酶脱氢酶的化合物
公开(公告)号：US20100286204A1
公开(公告)日：2010-11-11
申请号：US12744044
申请日：2008-11-19
申请人： Nigel Vicker , Helen Victoria Bailey , Wesley Heaton , Joanna Mary Day , Atul Purohit , Barry Victor Lloyd Potter
发明人： Nigel Vicker , Helen Victoria Bailey , Wesley Heaton , Joanna Mary Day , Atul Purohit , Barry Victor Lloyd Potter
IPC分类号： A61K31/4468 , C07C233/43 , A61K31/167 , C07D317/66 , A61K31/357 , C07D211/58 , C07D211/62 , A61K31/445 , C07C233/81 , C07D209/14 , A61K31/404 , C07D207/27 , A61K31/402 , A61P35/00
CPC分类号： C07D207/26 , C07C217/90 , C07C233/43 , C07C237/42 , C07D211/58 , C07D211/62 , C07D317/66
摘要： There is provided a compound having Formula I wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, —OC(R13)3, —OCH(R13)2, —OCH2R13, C(R13)3, —CH(R13)2, or —CH2R13 wherein R13 is a halogen; (c) —CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) —SO2-alkyl; and (n) —N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=0, S(═O)2, C═O, S(═O)2NR16, C═ONR17, NR18, in which R16, R17, and R18 are independently selected from H and hydrocarbyl, R10 is selected from H and hydrocarbyl, R11 is selected from CR19R20 and C═O, in which R19 and R20 are independently selected from H and hydrocarbyl, R12 is selected from a substituted five or six membered carbon rings optionally containing one or more hetero atoms selected from N, S, and O and optionally having fused thereto a further ring, and wherein the one or more substituents are selected from hydrocarbyl groups.
摘要翻译：提供具有式I的化合物，其中R1，R2，R3，R4，R5，R6，R7，R8和R9各自独立地选自（a）H，（b）R13，-OC（R13）3， - OCH（R 13）2，-OCH 2 R 13，C（R 13）3，-CH（R 13）2或-CH 2 R 13，其中R 13是卤素; （c）-CN; （d）任选取代的烷基，（e）任选取代的杂烷基; （f）任选取代的芳基; （g）任选取代的杂芳基; （h）任选取代的芳基烷基; （i）任选取代的杂芳基烷基; （j）羟基; （k）烷氧基; （I）芳氧基; （m）-SO 2 - 烷基; 和（n）-N（R 14）C（O）R 15，其中R 14和R 15独立地选自H和烃基，其中选择（d）（e）（f）（h）和（i）羟基，C 1-6烷氧基，羧基，羧基烷基，羧酰胺，巯基，氨基，烷基氨基，二烷基氨基，磺酰基，亚磺酰氨基，芳基和杂芳基; 其中n和p独立地选自0和1; X是选自O，S，S = 0，S（= O）2，C = O，S（= O）2 NR 16，C = CONR 17，NR 18的任选基团，其中R 16，R 17和R 18独立地选自由H和烃基组成，R 10选自H和烃基，R 11选自CR 19 R 20和C = O，其中R 19和R 20独立地选自H和烃基，R 12选自取代的五或六元碳环，任选含有一个或多个选自N，S和O的杂原子，并且任选地与另一个环稠合，并且其中一个或多个取代基选自烃基。

8. 发明申请

US20090042929A1 11-Beta-Hydroxysteroid Dehydrogenase Inhibitors 审中-公开
标题翻译： 11-β-羟基类固醇脱氢酶抑制剂
公开(公告)号：US20090042929A1
公开(公告)日：2009-02-12
申请号：US11886884
申请日：2006-03-23
申请人： Nigel Vicker , Xiangdong Su , Fabienne Pradaux , Michael John Reed , Barry Victor Lloyd Potter
发明人： Nigel Vicker , Xiangdong Su , Fabienne Pradaux , Michael John Reed , Barry Victor Lloyd Potter
IPC分类号： A61K31/437 , A61P3/00 , A61P29/00 , A61P37/00 , A61P19/00 , A61P35/00 , C07C311/20 , A61K31/428 , A61K31/18 , C12Q1/32 , A61K31/381 , A61K31/4439 , C07C311/16 , C07D277/64 , C07D333/24 , C07D213/56 , C07D495/04
CPC分类号： C07C233/25 , C07C233/58 , C07C233/59 , C07C311/13 , C07C311/16 , C07C311/20 , C07C317/24 , C07C323/22 , C07C2603/74 , C07D207/09 , C07D207/335 , C07D209/14 , C07D213/40 , C07D213/75 , C07D213/82 , C07D233/24 , C07D233/54 , C07D233/64 , C07D239/26 , C07D271/06 , C07D277/20 , C07D277/64 , C07D295/13 , C07D307/52 , C07D333/20 , C07D333/34 , C07D333/58
摘要： There is provided a compound having Formula (I) R1-Z-R2 wherein R1 is a group selected from optionally substituted fused polycyclic groups, substituted alkyl groups, branched alkyl groups, and optionally substituted cycloalkyl groups Z is a linker which is or comprises a carbonyl group or a isostere of a carbonyl group R2 is selected from optionally substituted aromatic rings and optionally substituted heterocyclic rings wherein (a) R2 is a 2-substituted thiophene group, and/or (b) Z is a group of the formula —C(═O)—CR3R4—X—(CR5R6)n-, wherein X is selected from NR7, S, O, S═O, and S(═O)2, wherein n is 0 or 1 and/or (c) R1 is an adamantyl group and Z is or comprises an amide group, and/or (d) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR8R9)p-NR10—S(═O)2—(CR11R12)q-, wherein p is 0 or 1 and q is 0 or 1 and/or (e) R1 is an adamantyl group and Z is or comprises a group of the formula —(CR13R14)V—Y—(CR15R16)W— where Y is a heteroaryl group in which a bond in the heteroaryl ring is a isostere of a carbonyl group, wherein v is o or 1 and w is 0 or 1; wherein each of R3, R4, R5, R6, R8, R9, R11, R12, R13, R14, R15 and R16, are independently selected from H, hydrocarbyl and halogen, wherein each of R7 and R10 are independently selected from H and hydrocarbyl.
摘要翻译：提供了具有式（I）的化合物，其中R 1是选自任选取代的稠合多环基团，取代的烷基基团，支链烷基基团和任选取代的环烷基基团。Z是一个或多个羰基或羰基的等排基团选自任选取代的芳环和任选取代的杂环，其中（a）R 2是2-取代的噻吩基团，和/或（b）Z是式-C （-O）-CR 3 R 4 -X-（CR 5 R 6）n - ，其中X选自NR 7，S，O，SO和S（-O）2，其中n为0或1和/或（c）金刚烷基，Z是或包含酰胺基，和/或（d）R 1是金刚烷基，Z是或包含式 - （CR 8 R 9）p -NR 10 -S（-O）2 - （CR 11 R 12））q-，其中p为0或1，q为0或1，和/或（e）R1为金刚烷基，Z为或包含式 - （CR13R14）VY-（CR15R16）W-的基团，其中Y 是其中的键 e杂芳基环是羰基的等排物，其中v是o或1，w是0或1; 其中R 3，R 4，R 5，R 6，R 8，R 9，R 11，R 12，R 13，R 14，R 15和R 16各自独立地选自H，烃基和卤素，其中R 7和R 10各自独立地选自H和烃基。

9. 发明申请

US20120041207A1 Compound 审中-公开
标题翻译：复合
公开(公告)号：US20120041207A1
公开(公告)日：2012-02-16
申请号：US13137395
申请日：2011-08-10
申请人： Nigel Vicker , Su Xiangdong , Dharshini Ganeshapillai , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
发明人： Nigel Vicker , Su Xiangdong , Dharshini Ganeshapillai , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
IPC分类号： C07D277/64 , C07D235/08 , C07D209/12 , C07D417/12
CPC分类号： C07D277/64 , C07D209/08 , C07D235/08 , C07D263/56 , C07D277/14 , C07D417/12
摘要： A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl, R5 is a hydrocarbyl group and L is an optional linker group, or R1 and R2 together form a ring substituted with the group wherein R3 is H or a substituent, and wherein X is selected from S, O, NR6 and C(R7)(R8), wherein R6 is selected from H and hydrocarbyl groups, wherein each of R7 and R8 are independently selected from H and hydrocarbyl groups.
摘要翻译：具有式I的化合物，其中R 1和R 2中的一个是下式的基团其中R 4选自H和烃基，R 5是烃基，L是任选的连接基团，或者R 1和R 2一起形成被其中R 3是H或取代基，其中X选自S，O，NR 6和C（R 7）（R 8），其中R 6选自H和烃基，其中R 7和R 8各自独立地选自H 和烃基。

10. 发明授权

US08003783B2 17B-hydroxysteroid dehydrogenase inhibitors 失效
标题翻译： 17B-羟类固醇脱氢酶抑制剂
公开(公告)号：US08003783B2
公开(公告)日：2011-08-23
申请号：US11234868
申请日：2005-09-23
申请人： Nigel Vicker , Harshani Rithma Ruchiranani Lawrence , Gillian Margaret Allan , Christian Bubert , Delphine Sophie Marion Fischer , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
发明人： Nigel Vicker , Harshani Rithma Ruchiranani Lawrence , Gillian Margaret Allan , Christian Bubert , Delphine Sophie Marion Fischer , Atul Purohit , Michael John Reed , Barry Victor Lloyd Potter
IPC分类号： A61K31/58 , C07J71/00
CPC分类号： C07J71/00 , C07J41/00
摘要： There is provided a compound of Formula (III) wherein R1 is a selected from an alkyloxyalkyl group, a nitrile group, alkylaryl group, alkenylaryl group, alkylheteroaryl group, alkenylheteroaryl group, ═N—O—alkyl or ═N—O—H group, branched alkenyl, alkyl-alcohol group, amide or alkylamide or —CHO so that R1 together with R3 provide the enol tautomer or R1 together with R3 form a pyrazole, wherein (a) R4 is ═N—O-alkyl or ═N—O—H group, (b) the pyrazole is substituted with one of alkyl-OH group, alkyl ester group, alkyloxyalkyl group, branched alkyl group, and an amide and/or (c) the 2-position is substituted with a group selected from —OH and —O-hydrocarbyl or a heteroaryl ring; R2 is selected from —OH and a sulphamate group; and R3 is selected from —OH or ═O; wherein the ring system may be further substituted with one or more hydroxyl, alkyl, alkoxy, alkinyl or halo substituents.
摘要翻译：提供式（III）的化合物，其中R 1选自烷氧基烷基，腈基，烷基芳基，链烯基芳基，烷基杂芳基，烯基杂芳基，N-O-烷基或= N-O-H基，支链烯基，烷基醇基，酰胺或烷基酰胺或-CHO，使得R 1与R 3一起提供烯醇互变异构体或R 1与R 3一起形成吡唑，其中（a）R 4是= N-O-烷基或= O-H基，（b）吡唑被烷基-OH基，烷基酯基，烷氧基烷基，支链烷基和酰胺中的一个取代，和/或（c）2-位被选定的基团取代从-OH和-O-烃基或杂芳基环; R2选自-OH和氨基磺酸酯基; 并且R 3选自-OH或= O; 其中所述环系可以进一步被一个或多个羟基，烷基，烷氧基，炔基或卤素取代基取代。

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