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公开(公告)号:US5559256A
公开(公告)日:1996-09-24
申请号:US79978
申请日:1993-06-25
申请人: Eric M. Gordon , Joel C. Barrish , Gregory S. Bisacchi , Chong-Qing Sun , Joseph A. Tino , Gregory D. Vite , Robert Zahler
发明人: Eric M. Gordon , Joel C. Barrish , Gregory S. Bisacchi , Chong-Qing Sun , Joseph A. Tino , Gregory D. Vite , Robert Zahler
IPC分类号: A61K31/13 , A61K31/16 , A61K31/18 , A61K31/265 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/496 , A61K31/505 , A61P31/12 , A61P31/18 , A61P37/00 , C07C215/28 , C07C233/40 , C07C233/78 , C07C235/40 , C07C237/10 , C07C271/10 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/05 , C07C313/06 , C07C333/04 , C07C333/12 , C07D207/09 , C07D207/16 , C07D207/26 , C07D207/267 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/44 , C07D209/46 , C07D213/30 , C07D213/36 , C07D213/40 , C07D213/55 , C07D213/56 , C07D213/65 , C07D215/14 , C07D215/48 , C07D217/16 , C07D231/56 , C07D233/30 , C07D233/32 , C07D233/54 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/24 , C07D239/34 , C07D239/91 , C07D241/42 , C07D243/04 , C07D263/22 , C07D263/24 , C07D263/26 , C07D263/32 , C07D263/56 , C07D265/32 , C07D277/64 , C07D295/092 , C07D295/185 , C07D303/36 , C07D305/08 , C07D307/20 , C07D307/24 , C07D309/10 , C07D333/64 , C07D413/14 , C07D491/04 , C07D521/00 , C07F7/08 , C07F7/18 , C07D401/12
CPC分类号: C07D207/267 , C07C215/28 , C07C233/40 , C07C233/78 , C07C235/40 , C07C237/10 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C333/04 , C07C333/12 , C07D207/09 , C07D207/16 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/44 , C07D209/46 , C07D213/30 , C07D213/40 , C07D213/56 , C07D213/65 , C07D215/14 , C07D215/48 , C07D217/16 , C07D231/12 , C07D231/56 , C07D233/32 , C07D233/56 , C07D233/64 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/24 , C07D239/91 , C07D241/42 , C07D249/08 , C07D263/22 , C07D263/24 , C07D263/26 , C07D263/32 , C07D263/56 , C07D265/32 , C07D277/64 , C07D295/088 , C07D295/185 , C07D305/08 , C07D307/20 , C07D307/24 , C07D309/10 , C07D333/64 , C07D413/14 , C07D491/04 , C07F7/0812 , C07F7/0818 , C07F7/1852 , C07F7/1856 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2103/18
摘要: Novel aminediol compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds in inhibiting retroviral protease, particularly useful in the treatment and/or prevention of HIV infection (AIDS).
摘要翻译: 新型二胺化合物,含有这些化合物的药物组合物,以及使用这些化合物抑制逆转录病毒蛋白酶的方法,特别可用于治疗和/或预防HIV感染(AIDS)。
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公开(公告)号:US5776933A
公开(公告)日:1998-07-07
申请号:US456125
申请日:1995-05-31
申请人: Eric M. Gordon , Joel C. Barrish , Gregory S. Bisacchi , Chong-Qing Sun , Joseph A. Tino , Gregory D. Vite , Robert Zahler
发明人: Eric M. Gordon , Joel C. Barrish , Gregory S. Bisacchi , Chong-Qing Sun , Joseph A. Tino , Gregory D. Vite , Robert Zahler
IPC分类号: A61K31/13 , A61K31/16 , A61K31/18 , A61K31/265 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/496 , A61K31/505 , A61P31/12 , A61P31/18 , A61P37/00 , C07C215/28 , C07C233/40 , C07C233/78 , C07C235/40 , C07C237/10 , C07C271/10 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/05 , C07C313/06 , C07C333/04 , C07C333/12 , C07D207/09 , C07D207/16 , C07D207/26 , C07D207/267 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/44 , C07D209/46 , C07D213/30 , C07D213/36 , C07D213/40 , C07D213/55 , C07D213/56 , C07D213/65 , C07D215/14 , C07D215/48 , C07D217/16 , C07D231/56 , C07D233/30 , C07D233/32 , C07D233/54 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/24 , C07D239/34 , C07D239/91 , C07D241/42 , C07D243/04 , C07D263/22 , C07D263/24 , C07D263/26 , C07D263/32 , C07D263/56 , C07D265/32 , C07D277/64 , C07D295/092 , C07D295/185 , C07D303/36 , C07D305/08 , C07D307/20 , C07D307/24 , C07D309/10 , C07D333/64 , C07D413/14 , C07D491/04 , C07D521/00 , C07F7/08 , C07F7/18 , A61K31/445 , A61K31/535
CPC分类号: C07D207/267 , C07C215/28 , C07C233/40 , C07C233/78 , C07C235/40 , C07C237/10 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C333/04 , C07C333/12 , C07D207/09 , C07D207/16 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/44 , C07D209/46 , C07D213/30 , C07D213/40 , C07D213/56 , C07D213/65 , C07D215/14 , C07D215/48 , C07D217/16 , C07D231/12 , C07D231/56 , C07D233/32 , C07D233/56 , C07D233/64 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/24 , C07D239/91 , C07D241/42 , C07D249/08 , C07D263/22 , C07D263/24 , C07D263/26 , C07D263/32 , C07D263/56 , C07D265/32 , C07D277/64 , C07D295/088 , C07D295/185 , C07D305/08 , C07D307/20 , C07D307/24 , C07D309/10 , C07D333/64 , C07D413/14 , C07D491/04 , C07F7/0812 , C07F7/0818 , C07F7/1852 , C07F7/1856 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2103/18
摘要: Novel aminediol compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds in inhibiting retroviral protease, particularly useful in the treatment and/or prevention of HIV infection (AIDS).
摘要翻译: 新型二胺化合物,含有这些化合物的药物组合物,以及使用这些化合物抑制逆转录病毒蛋白酶的方法,特别可用于治疗和/或预防HIV感染(AIDS)。
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公开(公告)号:US5760036A
公开(公告)日:1998-06-02
申请号:US455295
申请日:1995-05-31
申请人: Eric M. Gordon , Joel C. Barrish , Gregory S. Bisacchi , Chong-Oing Sun , Joseph A. Tino , Gregory D. Vite , Robert Zahler
发明人: Eric M. Gordon , Joel C. Barrish , Gregory S. Bisacchi , Chong-Oing Sun , Joseph A. Tino , Gregory D. Vite , Robert Zahler
IPC分类号: A61K31/13 , A61K31/16 , A61K31/18 , A61K31/265 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4166 , A61K31/4184 , A61K31/496 , A61K31/505 , A61P31/12 , A61P31/18 , A61P37/00 , C07C215/28 , C07C233/40 , C07C233/78 , C07C235/40 , C07C237/10 , C07C271/10 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C311/05 , C07C313/06 , C07C333/04 , C07C333/12 , C07D207/09 , C07D207/16 , C07D207/26 , C07D207/267 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/44 , C07D209/46 , C07D213/30 , C07D213/36 , C07D213/40 , C07D213/55 , C07D213/56 , C07D213/65 , C07D215/14 , C07D215/48 , C07D217/16 , C07D231/56 , C07D233/30 , C07D233/32 , C07D233/54 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/24 , C07D239/34 , C07D239/91 , C07D241/42 , C07D243/04 , C07D263/22 , C07D263/24 , C07D263/26 , C07D263/32 , C07D263/56 , C07D265/32 , C07D277/64 , C07D295/092 , C07D295/185 , C07D303/36 , C07D305/08 , C07D307/20 , C07D307/24 , C07D309/10 , C07D333/64 , C07D413/14 , C07D491/04 , C07D521/00 , C07F7/08 , C07F7/18 , A61K31/445 , A61K31/535 , C07D295/192
CPC分类号: C07D207/267 , C07C215/28 , C07C233/40 , C07C233/78 , C07C235/40 , C07C237/10 , C07C271/20 , C07C271/22 , C07C271/34 , C07C275/16 , C07C275/24 , C07C311/03 , C07C333/04 , C07C333/12 , C07D207/09 , C07D207/16 , C07D209/12 , C07D209/14 , C07D209/18 , C07D209/44 , C07D209/46 , C07D213/30 , C07D213/40 , C07D213/56 , C07D213/65 , C07D215/14 , C07D215/48 , C07D217/16 , C07D231/12 , C07D231/56 , C07D233/32 , C07D233/56 , C07D233/64 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/24 , C07D239/91 , C07D241/42 , C07D249/08 , C07D263/22 , C07D263/24 , C07D263/26 , C07D263/32 , C07D263/56 , C07D265/32 , C07D277/64 , C07D295/088 , C07D295/185 , C07D305/08 , C07D307/20 , C07D307/24 , C07D309/10 , C07D333/64 , C07D413/14 , C07D491/04 , C07F7/0812 , C07F7/0818 , C07F7/1852 , C07F7/1856 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2103/18
摘要: Novel aminediol compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds in inhibiting retroviral protease, particularly useful in the treatment and/or prevention of HIV infection (AIDS).
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公开(公告)号:US5314893A
公开(公告)日:1994-05-24
申请号:US9485
申请日:1993-01-25
IPC分类号: A61K31/52 , A61K31/522 , A61P31/12 , C07D239/46 , C07D239/54 , C07D239/553 , C07D405/04 , C07D473/00 , C07D473/16 , C07D473/18 , C07D473/34 , C07D473/40 , C07H19/04 , A61K31/505 , C07D239/47 , C07D239/545
CPC分类号: C07D239/47 , C07D239/54 , C07D239/553 , C07D405/04 , C07D473/00 , C07H19/04 , Y02P20/55
摘要: Compounds of the formula ##STR1## wherein R.sub.1 is an amino substituted pyrimidinone or a pyrimidinedione including pharmaceutically acceptable salts are useful as antiviral agents.
摘要翻译: 其中R1是氨基取代的嘧啶酮或包含药学上可接受的盐的嘧啶二酮的式IMA化合物可用作抗病毒剂。
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公开(公告)号:US5414096A
公开(公告)日:1995-05-09
申请号:US200022
申请日:1994-02-22
IPC分类号: A61K31/52 , A61K31/522 , A61P31/12 , C07D239/46 , C07D239/54 , C07D239/553 , C07D405/04 , C07D473/00 , C07D473/16 , C07D473/18 , C07D473/34 , C07D473/40 , C07H19/04 , A61K31/505 , C07D239/47 , C07D239/545
CPC分类号: C07D239/47 , C07D239/54 , C07D239/553 , C07D405/04 , C07D473/00 , C07H19/04 , Y02P20/55
摘要: ##STR1## wherein R
4 is a leaving group and P
1 and P
2 are hydroxy protecting groups are useful in the preparation of purinyl and pyrimidinyl substituted tetrahydropyran antiviral agents.摘要翻译: 其中R4是离去基团,P1和P2是羟基保护基团可用于制备嘌呤基和嘧啶基取代的四氢吡喃抗病毒剂。
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公开(公告)号:US5414000A
公开(公告)日:1995-05-09
申请号:US200024
申请日:1994-02-22
IPC分类号: A61K31/52 , A61K31/522 , A61P31/12 , C07D239/46 , C07D239/54 , C07D239/553 , C07D405/04 , C07D473/00 , C07D473/16 , C07D473/18 , C07D473/34 , C07D473/40 , C07H19/04 , A61K31/505 , C07D239/47 , C07D239/545
CPC分类号: C07D239/47 , C07D239/54 , C07D239/553 , C07D405/04 , C07D473/00 , C07H19/04 , Y02P20/55
摘要: Compounds of the formula ##STR1## wherein R.sub.1 is a substituted purinyl group including pharmaceutically acceptable salts are useful as antiviral agents.
摘要翻译: 其中R 1是包括药学上可接受的盐的取代的嘌呤基的式IMAMA的化合物可用作抗病毒剂。
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公开(公告)号:US5164520A
公开(公告)日:1992-11-17
申请号:US741860
申请日:1991-08-07
申请人: Robert Zahler , Joseph A. Tino
发明人: Robert Zahler , Joseph A. Tino
IPC分类号: C07D307/20 , C07D405/04 , C07D473/00 , C07F9/6558 , C07F9/6561
CPC分类号: C07D473/00 , C07D307/20 , C07D405/04 , C07F9/65586 , C07F9/65616
摘要: Intermediate for the preparation of antiviral compounds having the formula ##STR1## wherein R.sub.1 is a purine or pyrimidine base or an analog thereof.
摘要翻译: 制备具有式“IMAGE”的抗病毒化合物的中间体,其中R1是嘌呤或嘧啶碱基或其类似物。
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公开(公告)号:US5059690A
公开(公告)日:1991-10-22
申请号:US486988
申请日:1990-05-01
申请人: Robert Zahler , Joseph A. Tino
发明人: Robert Zahler , Joseph A. Tino
IPC分类号: C07D405/04 , C07D473/00 , C07F9/6558 , C07F9/6561
CPC分类号: C07D473/00 , C07D405/04 , C07F9/65586 , C07F9/65616
摘要: Antiviral activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1 is a purine or pyrimidine base or an analog thereof and R.sub.2 and R.sub.3 are independently hydrogen, --PO.sub.3 H.sub.2 or ##STR2## wherein X.sub.7 is hydrogen, alkyl, substituted alkyl or aryl.
摘要翻译: 抗肿瘤活性由具有下式的化合物及其药学上可接受的盐显示,其中R1是嘌呤或嘧啶碱基或其类似物,R2和R3独立地是氢,-PO3H2或者其中X7是氢,烷基, 取代的烷基或芳基。
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公开(公告)号:US5145960A
公开(公告)日:1992-09-08
申请号:US741861
申请日:1991-08-07
申请人: Robert Zahler , Joseph A. Tino
发明人: Robert Zahler , Joseph A. Tino
IPC分类号: C07D307/20 , C07D405/04 , C07D473/00
CPC分类号: C07D473/00 , C07D307/20 , C07D405/04
摘要: Antiviral activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1 is a pyrimidine base or an analog thereof and R.sub.2 and R.sub.3 are independently hydrogen, --PO.sub.3 H.sub.2 or ##STR2## wherein X.sub.7 is hydrogen, alkyl, substituted alkyl or aryl.
摘要翻译: 抗病毒活性由具有下式的化合物及其药学上可接受的盐显示,其中R1是嘧啶碱基或其类似物,R2和R3独立地是氢,-PO3H2或者其中X7是氢,烷基,取代的烷基 或芳基。
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公开(公告)号:US07262195B2
公开(公告)日:2007-08-28
申请号:US10940240
申请日:2004-09-14
IPC分类号: A61K31/50 , C07D237/00 , C07D487/00
CPC分类号: C07D471/20 , A61K31/495 , A61K31/50
摘要: Compounds are provided which are useful in treating disorders of gastrointestinal motility and which have the structure or a pharmaceutically acceptable salt thereof, a prodrug ester thereof, and all stereoisomers thereof, wherein R1 and R2 are the same or different and are independently selected from hydrogen, alkyl, aryl, cycloalkyl, alkenyl, alkynyl, arylalkyl, heteroaryl, heteroarylalkyl or heterocycloalkyl; Z is selected from —CON(R4)R4a, —CO2R4, —SO2N(R4)R4a, —SO2R4, CN, and R4 and R4a are the same or different and are independently selected from hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl or R4 and R4a can be joined together to form a heterocycle. R4b is selected from hydrogen, halogen, hydroxyl, CN, OCF3, CF3, CONH2, SONH2, SO2CH3, NHCOCH3 or NHCO2CH3; and Q is a substituted bicyclic heterocycle. A method for using such compounds for treating disorders of gastrointestinal motility is also provided.
摘要翻译: 提供了可用于治疗胃肠蠕动障碍并且具有其结构或其药学上可接受的盐,其前药酯及其所有立体异构体的化合物,其中R 1和R 2 独立地选自氢,烷基,芳基,环烷基,烯基,炔基,芳基烷基,杂芳基,杂芳基烷基或杂环烷基; Z选自-CON(R 4 S)R 4a,-CO 2 R 4,-SO 3, N 2(R 4)R 4a,-SO 2 R 4,CN R 4a和R 4a相同或不同并且独立地选自氢,烷基,环烷基,芳基,芳基烷基,杂芳基或杂芳基烷基或R 1, 4和R 4a可以连接在一起形成杂环。 R 4b选自氢,卤素,羟基,CN,OCF 3,CF 3,CONH 2, SO 2 H 2,CH 2 CH 3,NHCOCH 3或NHCO 2 CH 3, SUB> 3 SUB> Q是取代的双环杂环。 还提供了使用这些化合物治疗胃肠蠕动障碍的方法。
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