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1. 发明申请

WO03014089A8 AMINOTETRAHYDROISOQUINOLINE DERIVATIVES AS ANALGESICS 审中-公开
标题翻译：氨基甲酰喹啉衍生物作为分析物
公开(公告)号：WO03014089A8
公开(公告)日：2004-05-27
申请号：PCT/US0223698
申请日：2002-07-25
申请人： UNIV VIRGINIA COMMONWEALTH , GLENNON RICHARD A , MARTIN BILLY R , DUKAT MALGOZATA , DAMAJ IMAD M
发明人： GLENNON RICHARD A , MARTIN BILLY R , DUKAT MALGOZATA , DAMAJ IMAD M
IPC分类号： A61P29/00 , C07D217/02 , A61K31/472
CPC分类号： C07D217/02
摘要： Tetrahydroisoquinolines are provided having a secondary, tertiary or quaternary amino group spaced by three carbon atoms from the ring nitrogen, and pharmaceutically acceptable salts and prodrugs thereof. Preferred compounds are of Formula (I), wherein R , R and R are independently selected from the group consisting of hydrogen, C1-6 alkyl and a moiety wherein any two of R , R and R , together with the nitrogen to which they are attached, form a heterocyclic ring of 2 to 5 carbons, provided that R and R , and R when present, are not each hydrogen, R and R are independently selected from the group of moieties which are effective to alter the solubility of the compound in physiological fluids or pharmaceutical carriers n and m are independently selected from integers of 0 to 3 and 0 to 4 respectively, p is an integer 0 or 1 and pharmaceutically acceptable salts and prodrugs thereof.
摘要翻译：提供四环异喹啉，其具有从环氮中间隔三个碳原子的仲，叔或季氨基，及其药学上可接受的盐和前药。优选的化合物是式（I），其中R 1，R 2和R 5独立地选自氢，C 1-6烷基和其中R 1， R 2和R 5与它们所连接的氮一起形成2至5个碳的杂环，条件是R 1和R 2以及当R 5为R 5时，不是每个氢，R 3和R 4独立地选自有效改变化合物在生理流体或药物载体中的溶解度的部分，n和m独立地选自0至3的整数和0至4，p是整数0或1及其药学上可接受的盐和前药。

2. 发明申请

WO03011828A3 3-PYRIDYLETHER RERIVATIVES AND THEIR USE AS ANALGESICS 审中-公开
标题翻译： 3-吡啶基衍生物及其作为分析物的用途
公开(公告)号：WO03011828A3
公开(公告)日：2003-10-16
申请号：PCT/US0223686
申请日：2002-07-25
申请人： UNIV VIRGINIA COMMONWEALTH , GLENNON RICHARD A , MARTIN BILLY R , DUKAT MALGOZATA , DAMAJ IMAD M
发明人： GLENNON RICHARD A , MARTIN BILLY R , DUKAT MALGOZATA , DAMAJ IMAD M
IPC分类号： A61P25/04 , C07D213/65 , A61K31/44
CPC分类号： C07D213/65
摘要： A salt of general formula (I) wherein R , R and R are independently selected from the group consisting of C1-6 alkyl groups or any two or three of R , R and R may, together with the nitrogen to which they are attached, form a heterocyclic ring. R is a selected from the group of moieties which are effective to alter the solubility of the compound in physiological fluids and pharmaceutical carries, n is an integer of 0 to 5, A is selected from hydrogen or may, with the carbon to which it is attached and with any one of R , R and R and the nitrogen to which they are attached, form a heterocyclic ring X is a negatively charged counterion and p is the number of negative charges thereon, the number of molecules of the positively charged tertiary amino ion being equal to the integer p in any given salt. Preferably the salt is of formula (II) below.
摘要翻译：通式（I）的盐，其中R 1，R 2和R 3独立地选自C 1-6烷基或R 1，R 2中的任何两个或三个 >和R 3可以与它们所连接的氮一起形成杂环。 R 4选自有效改变化合物在生理流体和药物载体中的溶解度的部分组，n是0-5的整数，A选自氢或可以与碳或其与R 1，R 2和R 3中的任何一个和它们所连接的氮形成杂环X是带负电的抗衡离子，p是负电荷的数量在任何给定的盐中，带正电的叔氨基离子的分子数等于整数p。优选的盐是下式（II）。

3. 发明申请

WO2003014089A1 AMINOTETRAHYDROISOQUINOLINE DERIVATIVES AS ANALGESICS 审中-公开
标题翻译：氨基甲酰喹啉衍生物作为分析物
公开(公告)号：WO2003014089A1
公开(公告)日：2003-02-20
申请号：PCT/US2002/023698
申请日：2002-07-25
申请人： VIRGINIA COMMONWEALTH UNIVERSITY , GLENNON, Richard, A. , MARTIN, Billy, r. , DUKAT, Malgozata , DAMAJ, Imad, M.
发明人： GLENNON, Richard, A. , MARTIN, Billy, r. , DUKAT, Malgozata , DAMAJ, Imad, M.
IPC分类号： C07D217/02
CPC分类号： C07D217/02
摘要： Tetrahydroisoquinolines are provided having a secondary, tertiary or quaternary amino group spaced by three carbon atoms from the ring nitrogen, and pharmaceutically acceptable salts and prodrugs thereof. Preferred compounds are of Formula (I), wherein R 1 , R 2 and R 5 are independently selected from the group consisting of hydrogen, C 1-6 alkyl and a moiety wherein any two of R 1 , R 2 and R 5 , together with the nitrogen to which they are attached, form a heterocyclic ring of 2 to 5 carbons, provided that R 1 and R 2 , and R 5 when present, are not each hydrogen, R 3 and R 4 are independently selected from the group of moieties which are effective to alter the solubility of the compound in physiological fluids or pharmaceutical carriers n and m are independently selected from integers of 0 to 3 and 0 to 4 respectively, p is an integer 0 or 1 and pharmaceutically acceptable salts and prodrugs thereof.
摘要翻译：提供四环异喹啉，其具有从环氮中间隔三个碳原子的仲，叔或季氨基，及其药学上可接受的盐和前药。优选的化合物是式（I），其中R 1，R 2和R 5独立地选自氢，C 1-6烷基和其中R 1， R 2和R 5与它们所连接的氮一起形成2至5个碳的杂环，条件是R 1和R 2以及当R 5为R 5时，不是每个氢，R 3和R 4独立地选自有效改变化合物在生理液体或药物载体中的溶解度的部分，n和m独立地选自0至3的整数和0至4，p是整数0或1及其药学上可接受的盐和前药。

4. 发明申请

WO2003011828A2 NOVEL ANALGESICS 审中-公开
标题翻译：新闻学
公开(公告)号：WO2003011828A2
公开(公告)日：2003-02-13
申请号：PCT/US2002/023686
申请日：2002-07-25
申请人： VIRGINIA COMMONWEALTH UNIVERSITY , GLENNON, Richard, A. , MARTIN, Billy, R. , DUKAT, Malgozata , DAMAJ, Imad, M.
发明人： GLENNON, Richard, A. , MARTIN, Billy, R. , DUKAT, Malgozata , DAMAJ, Imad, M.
IPC分类号： C07D213/00
CPC分类号： C07D213/65
摘要： A salt of general formula I wherein R 1 , R 2 and R 3 are independently selected from the group consisting of C 1-6 alkyl groups or any two or three of R 1 , R 2 and R 3 may, together with the nitrogen to which they are attached, form a heterocyclic ring. R 4 is a selected from the group of moieties which are effective to alter the solubility of the compound in physiological fluids and pharmaceutical carries, n is an integer of 0 to 5, A is selected from hydrogen or may, with the carbon to which it is attached and with any one of R 1 , R 2 and R 3 and the nitrogen to which they are attached, form a heterocyclic ring X is a negatively charged counterion and p is the number of negative charges thereon, the number of molecules of the positively charged tertiary amino ion being equal to the integer p in any given salt. Preferably the salt is of formula II below.
摘要翻译：通式I的盐，其中R 1，R 2和R 3独立地选自C 1-6烷基或R 1，R 2和R 2的任何两个或三个， R 3可以与它们所连接的氮一起形成杂环。 R 4选自有效改变化合物在生理流体和药物载体中的溶解度的部分组，n是0-5的整数，A选自氢或可以与碳或其与R 1，R 2和R 3中的任何一个和它们所连接的氮形成杂环X是带负电的反离子，p是负电荷的数量在任何给定的盐中，带正电的叔氨基离子的分子数等于整数p。优选地，盐的下面是式II。

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