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1. 发明申请

WO2003035599A1 QUARTERNARY AMMONIUM COMPOUNDS AND THEIR USE AS ANTIMUSCARINIC AGENTS 审中-公开
标题翻译：季铵化合物及其作为抗菌药物使用
公开(公告)号：WO2003035599A1
公开(公告)日：2003-05-01
申请号：PCT/US2002/034529
申请日：2002-10-25
申请人： PHARMACIA & UPJOHN COMPANY , RICHARDS, Ivan , CAMMARATA, Sue, K. , WEGNER, Craig, D. , HAWLEY, Michael , WARCHOL, Mark, P. , KONTNY, Mark , MOROZOWICH, Walter , KOLBASA, Karen, P. , MOON, Malcolm, W. , BONAFOUX, Dominique , WOLFSON, Sergey, G. , LENNON, Patrick, J.
发明人： RICHARDS, Ivan , CAMMARATA, Sue, K. , WEGNER, Craig, D. , HAWLEY, Michael , WARCHOL, Mark, P. , KONTNY, Mark , MOROZOWICH, Walter , KOLBASA, Karen, P. , MOON, Malcolm, W. , BONAFOUX, Dominique , WOLFSON, Sergey, G. , LENNON, Patrick, J.
IPC分类号： C07C211/27
CPC分类号： C07D295/096 , C07C215/54 , C07C215/66 , C07C217/62 , C07C219/28 , C07C237/30
摘要： Novel quaternary ammonium compounds of the formula (I) and any stereoisomers thereof, wherein, R 1 , R 2 , and R 3 independently represent C 1 -C 6 alkyl, optionally substituted with phenyl or hydroxyl, or both, and wherein any two of R 1 , R 2 and R 3 may form a ring together with the quaternary ammonium nitrogen; R 4 represents -H, -CH 3 , or -CO-R 4 -1, wherein R 4-1 represents -(C 1 -C 4 alkyl), -(C 1 -C 4 alkoxy), or NR 4-2 R 4-3 , wherein R 4-2 and R 4-3 independently represent -H or -(C 1 -C 4 alkyl); R 5 , R 6 and R 7 independently represent -H, -OCH 3 , -OH, -CONH 2 , -SO 2 NH 2 , -F, -Cl, -Br, -I, -CF 3 , or -(C 1 -C 4 alkyl), optionally substituted with one or two -OH, -(C 1 -C 4 alkoxy), -COOH, or -CO-O-(C 1 -C 3 alkyl); and X represents an anion of a pharmaceutically acceptable acid, the compounds for use as medicaments, use of the compounds for the manufacture of specific medicaments, and pharmaceutical compositions comprising the compounds. The present invention also concerns a method of treatment involving administration of the compounds.
摘要翻译：式（I）的新型季铵化合物及其任何立体异构体，其中R 1，R 2，R 2和R 3彼此独立地表示C 任选被苯基或羟基取代的烷基，或两者，并且其中R 1，R 2，R 2中任意两个和R 3可以与季铵氮一起形成环; R 4b表示-H，-CH 3 s或3-s-4，其中R 4 = sb表示 - （C 1 -C 6）烷基）， - （C 1 -C 14烷基），或NR b-4-2，R 4b，其中R 4b和R 4b各自独立地表示表示-H或 - （C 1 -C 6 - 烷基）烷基）。 R 15和R 7独立地表示-H，-OCH 3 S，-OH，-CONH -SO 2，-SO 2，-SH 2，-SF 3，-SF 2，S-3，-SF 2，或任选被一个或两个-OH取代的（C 1 -C 4）烷基， - （C 1 -C 4）烷基）烷基），-COOH或-CO-O-（C 1 -C 6烷基）; X表示药学上可接受的酸的阴离子，用作药物的化合物，用于制备特定药物的化合物的用途，以及包含该化合物的药物组合物。本发明还涉及涉及给药化合物的治疗方法。

2. 发明申请

WO2003053972A1 PYRIDOQUINOXALINE ANTIVIRALS 审中-公开
标题翻译：吡咯烷酮类抗生素
公开(公告)号：WO2003053972A1
公开(公告)日：2003-07-03
申请号：PCT/US2002/037614
申请日：2002-12-19
申请人： PHARMACIA & UPJOHN COMPANY , STROHBACH, Joseph, W. , TANIS, Steven, P. , MOON, Malcolm, W. , PERRAULT, William, R.
发明人： STROHBACH, Joseph, W. , TANIS, Steven, P. , MOON, Malcolm, W. , PERRAULT, William, R.
IPC分类号： C07D471/06
CPC分类号： C07D471/06 , C07D241/44
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein R 1 and R 2 are as defined in the specification. The compounds are useful for the treatment of viral infections.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中R 1和R 2如说明书中所定义。该化合物可用于治疗病毒感染。

3. 发明申请

WO2003053971A1 PYRIDOQUINOXALINE ANTIVIRALS 审中-公开
标题翻译：吡咯烷酮类抗生素
公开(公告)号：WO2003053971A1
公开(公告)日：2003-07-03
申请号：PCT/US2002/037613
申请日：2002-12-19
申请人： PHARMACIA & UPJOHN COMPANY , STROHBACH, Joseph, W. , TANIS, Steven, P. , MOON, Malcolm, W. , NIEMAN, James, A. , BEAUCHAMP, Thomas, J. , NORTHUIS, Jill, M. , MCGHEE, William, D.
发明人： STROHBACH, Joseph, W. , TANIS, Steven, P. , MOON, Malcolm, W. , NIEMAN, James, A. , BEAUCHAMP, Thomas, J. , NORTHUIS, Jill, M. , MCGHEE, William, D.
IPC分类号： C07D471/06
CPC分类号： C07D213/74 , C07D215/12 , C07D215/56 , C07D239/26 , C07D241/12 , C07D277/28 , C07D307/14 , C07D307/81 , C07D333/38 , C07D333/58 , C07D471/06
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein R 1 , R 2 and R 3 are as defined in the specification. The compounds are useful for the treatment of viral infections.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中R 1，R 2和R 3如说明书中所定义。该化合物可用于治疗病毒感染。

4. 发明申请

WO03053971A8 PYRIDOQUINOXALINE ANTIVIRALS 审中-公开
标题翻译：吡咯烷酮类抗生素
公开(公告)号：WO03053971A8
公开(公告)日：2004-01-29
申请号：PCT/US0237613
申请日：2002-12-19
申请人： UPJOHN CO , STROHBACH JOSEPH W , TANIS STEVEN P , MOON MALCOLM W , NIEMAN JAMES A , BEAUCHAMP THOMAS J , NORTHUIS JILL M , MCGHEE WILLIAM D
发明人： STROHBACH JOSEPH W , TANIS STEVEN P , MOON MALCOLM W , NIEMAN JAMES A , BEAUCHAMP THOMAS J , NORTHUIS JILL M , MCGHEE WILLIAM D
IPC分类号： A61K31/4985 , A61K31/522 , A61K45/00 , A61P9/10 , A61P31/22 , A61P43/00 , C07D213/38 , C07D213/74 , C07D215/12 , C07D215/14 , C07D215/56 , C07D239/26 , C07D241/12 , C07D277/28 , C07D307/14 , C07D307/42 , C07D307/81 , C07D333/20 , C07D333/38 , C07D333/58 , C07D471/06 , A61K31/497 , A61P31/12
CPC分类号： C07D213/74 , C07D215/12 , C07D215/56 , C07D239/26 , C07D241/12 , C07D277/28 , C07D307/14 , C07D307/81 , C07D333/38 , C07D333/58 , C07D471/06
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein R , R and R are as defined in the specification. The compounds are useful for the treatment of viral infections.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中R 1，R 2和R 3如说明书中所定义。该化合物可用于治疗病毒感染。

5. 发明申请

WO1990015058A1 HETEROCYCLIC AMINES HAVING CENTRAL NERVOUS SYSTEM ACTIVITY 审中-公开
标题翻译：具有中枢神经系统活性的杂环氨基酸
公开(公告)号：WO1990015058A1
公开(公告)日：1990-12-13
申请号：PCT/US1990002621
申请日：1990-05-15
申请人： THE UPJOHN COMPANY , MOON, Malcolm, W. , HEIER, Richard, F. , MORRIS, Jeanette, K.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D455/04
CPC分类号： C07D471/06 , C07D215/40 , C07D455/04 , C07D513/06
摘要： Tricyclic nitrogen containing compounds, having central nervous system activity of structural formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 are independently hydrogen, C1-6 alkyl, alkenyl, or alkynyl, C3-10 cycloalkyl, or R1 and R2 are joined to form a C3-7 cyclic amine which can contain additional heteroatoms; X is hydrogen, C1-6 alkyl, halogen, hydroxy, alkoxy, cyano, carboxamide, carboxyl, or carboalkoxyl; A is SO2, N, CH, CH2, CHCH3, C=O, C=S, C-SCH3, C=NH, C-NH2, C-NHCH3, C-NHCOOCH3, or C-NHCN; B is CH2, CH, C=O, N, NH or N-CH3; n is 0 or 1; and D is CH, CH2, C=O, O, N, NH or N-CH3. These new compounds are suitable for treating schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure in animal or human hosts.
摘要翻译：具有结构式（I）的中枢神经系统活性的三环氮类化合物及其药学上可接受的盐，其中R1，R2和R3独立地是氢，C1-6烷基，烯基或炔基，C3-10环烷基或R1 和R 2连接形成可含有其它杂原子的C 3-7环胺; X是氢，C 1-6烷基，卤素，羟基，烷氧基，氰基，羧酰胺，羧基或烷氧羰基; A是SO 2，N，CH，CH 2，CHCH 3，C = O，C = S，C-SCH 3，C = NH，C-NH 2，C-NHCH 3，C-NHCOOCH 3或C-NHCN; B是CH 2，CH，C = O，N，NH或N-CH 3; n为0或1; 且D为CH，CH 2，C = O，O，N，NH或N-CH 3。这些新化合物适用于治疗精神分裂症，帕金森病，焦虑症，抑郁症或作为降低动物或人类宿主血压的化合物。

6. 发明申请

WO1990001026A1 ACETYLENIC IMIDAZOLES HAVING CENTRAL NERVOUS SYSTEM ACTIVITY 审中-公开
标题翻译：具有中枢神经系统活性的乙酰咪唑
公开(公告)号：WO1990001026A1
公开(公告)日：1990-02-08
申请号：PCT/US1989002537
申请日：1989-06-14
申请人： THE UPJOHN COMPANY , MOON, Malcolm, W. , HEIER, Richard, F.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D233/61
CPC分类号： C07D231/12 , C07D233/56 , C07D233/68 , C07D249/08 , C07D403/06
摘要： Acetylenic imidazole compounds comprising structural formula (I) or a therapeutically acceptable salt thereof, wherein X is H2 or O; R1 is hydrogen, methyl, ethyl, methylamino, dimethylamino, methoxy or ethoxy; R2 is hydrogen, methyl or ethyl or R1 and R2 are joined to form a cyclic ring which can be methyl or carbonyl substituted; and R3, R4 and R5 are independently chosen from hydrogen, methyl, ethyl, fluorine, chlorine, bromine or iodine, having cholinergic agonist or antagonist activity useful in the treatment of mental disorders, extrapyramidal motor disorders, disorders of the parasympathetic nervous system and glaucoma or as analgesics for the treatment of pain. Typical central nervous system disorders for which the subject compounds can be used include cognitive disorders of all ages, including senile dementia, Alzheimer's disease and other related disorders. The compounds are particularly developed to improve mental performance when a mental deficiency is diagnosed.
摘要翻译：包含结构式（I）或其治疗上可接受的盐的乙炔咪唑化合物，其中X是H 2或O; R 1是氢，甲基，乙基，甲基氨基，二甲基氨基，甲氧基或乙氧基; R 2是氢，甲基或乙基，或者R 1和R 2连接形成可以被甲基或羰基取代的环， R3，R4和R5独立地选自氢，甲基，乙基，氟，氯，溴或碘，具有胆碱能激动剂或拮抗剂活性，可用于治疗精神障碍，锥体外运动障碍，副交感神经系统疾病和青光眼或作为止痛剂治疗疼痛。可以使用主题化合物的典型的中枢神经系统疾病包括所有年龄的认知障碍，包括老年性痴呆，阿尔茨海默病和其他相关疾病。当诊断出精神缺陷时，这些化合物特别开发用于改善心理表现。

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