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1.
公开(公告)号:US6133449A
公开(公告)日:2000-10-17
申请号:US12066
申请日:1998-01-22
IPC分类号: C07D213/74 , C07D401/12 , C07D419/04 , C07D213/42
CPC分类号: C07D213/74 , C07D401/12 , C07D419/04
摘要: Compounds having the formulaR.sup.5 O--A--NR.sup.4 --R.sup.2 (V)where R.sup.2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R.sup.4 and R.sup.5 are both hydrogen atoms or together represent --SO-- or --SO.sub.2 -- and A is C.sub.2 -C.sub.4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R.sup.4 and R.sup.5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI).R.sup.2 O--A--NH.sub.2 (VI)
摘要翻译: 具有式R 5 O-A-NR 4 -R 2(V)的化合物,其中R 2是通过与氮原子相邻的碳原子连接到分子的其余部分的杂芳基,R 4和R 5都是氢原子或一起表示-SO-或 - SO 2 - 和A是任选被一个或多个低级烷基取代的C 2 -C 4亚烷基,作为制备作为末端化合物的药学上可用的哌嗪衍生物的新中间体。 具有式V的化合物,其中R 4和R 5是氢可以通过具有式(VI)的化合物的重排来制备:R 2 O-A-NH 2(VI)
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公开(公告)号:US06395902B1
公开(公告)日:2002-05-28
申请号:US09614792
申请日:2000-07-12
IPC分类号: C07D41904
CPC分类号: C07D213/74 , C07D401/12 , C07D419/04
摘要: Compounds having the formula R5O—A—NR4—R2 (V) where R2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R4 and R5 are both hydrogen atoms or together represent —SO— or —SO2— and A is C2-C4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R4 and R5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI). R2O—A—NH2 (VI)
摘要翻译: 具有通式R 2的化合物是通过与氮原子相邻的碳原子与分子的其余部分连接的杂芳基,并且R 4和R 5均为氢原子或一起代表-SO-或-SO 2 - 并且A为任选的C 2 -C 4亚烷基 被一个或多个低级烷基取代是制备药学上可用的哌嗪衍生物作为末端化合物的新中间体。 具有式V的化合物,其中R 4和R 5是氢可以通过具有式(VI)的化合物的重排来制备。
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3.
公开(公告)号:US06175012B1
公开(公告)日:2001-01-16
申请号:US09010741
申请日:1998-01-22
IPC分类号: C07D40112
CPC分类号: C07D213/74 , C07D401/12 , C07D419/04
摘要: Compounds having the formula R5O—A—NR4—R2 (V) where R2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R4 and R5 are both hydrogen atoms or together represent —SO— or —SO2— and A is C2-C4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R4 and R5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI). R2O—A—NH2 (VI)
摘要翻译: 具有通式R 2的化合物是通过与氮原子相邻的碳原子与分子的其余部分连接的杂芳基,并且R 4和R 5均为氢原子或一起代表-SO-或-SO 2 - 并且A为任选的C 2 -C 4亚烷基 被一个或多个低级烷基取代是制备药学上可用的哌嗪衍生物作为末端化合物的新中间体。 具有式V的化合物,其中R 4和R 5是氢可以通过具有式(VI)的化合物的重排来制备。
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公开(公告)号:US06403574B1
公开(公告)日:2002-06-11
申请号:US09600628
申请日:2001-09-17
申请人: David Reginald Adams , Corinna Dagmar Bodkin , Ian Anthony Cliffe , Howard Langham Mansell , Nathaniel Julius Monck , Robin Gerald Shepherd
发明人: David Reginald Adams , Corinna Dagmar Bodkin , Ian Anthony Cliffe , Howard Langham Mansell , Nathaniel Julius Monck , Robin Gerald Shepherd
IPC分类号: A61K31397
CPC分类号: C07D205/04
摘要: A compound of formula (1), wherein: R1 is aryl; R2 is H, alkyl or aryl; and R3 is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and the use of the compounds in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epilepsy.
摘要翻译: 式(1)的化合物,其中:R1是芳基; R2是H,烷基或芳基; 并且R 3是氢或烷基; 其药学上可接受的加成化合物; 以及化合物在治疗中的用途,特别是用于治疗和预防CNS疾病如焦虑和癫痫。
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公开(公告)号:US4000142A
公开(公告)日:1976-12-28
申请号:US526565
申请日:1974-11-25
IPC分类号: C07D215/04 , A61K31/47 , A61K31/473 , A61P1/04 , C07D215/48 , C07D219/02 , C07D219/06 , C07D221/04 , C07D221/06 , C07D221/16 , C07D215/14
CPC分类号: C07D215/48 , C07D221/16
摘要: The invention relates to a process for preparing pyridine compounds which have a fused cycloalkane ring containing an amide, thioamide or nitrile group. The process involves treating a metal derivative of the pyridine compound with a silyl isocyanate or isothiocyanate and then subjecting the product to hydrolysis or alcoholysis.
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公开(公告)号:US06831078B1
公开(公告)日:2004-12-14
申请号:US09600631
申请日:2001-02-12
申请人: David Reginald Adams , Jon Bentley , Corinna Dagmar Bodkin , Ian Anthony Cliffe , James Edward Paul Davidson , Howard Langham Mansell , Nathaniel Julius Monck , Robin Gerald Shepherd , by Joy Miriam Shepherd
发明人: David Reginald Adams , Jon Bentley , Corinna Dagmar Bodkin , Ian Anthony Cliffe , James Edward Paul Davidson , Howard Langham Mansell , Nathaniel Julius Monck , Robin Gerald Shepherd , by Joy Miriam Shepherd
IPC分类号: C07D20504
CPC分类号: C07D205/04
摘要: A compound of formula (1) wherein R1 is aryl; and R2 is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and their use in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epilepsy.
摘要翻译: 式(1)的化合物,其中R 1是芳基; 和R 2是氢或烷基; 其药学上可接受的加成化合物; 以及它们在治疗中的用途,特别是用于治疗和预防CNS疾病如焦虑和癫痫。
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公开(公告)号:US4085108A
公开(公告)日:1978-04-18
申请号:US721263
申请日:1976-09-08
IPC分类号: C07D215/48 , C07D221/16 , C07D215/12
CPC分类号: C07D215/48 , C07D221/16
摘要: The invention relates to novel silicon derivatives of tetrahydroquinolines, which are intermediates in a process for preparing 5,6,7,8-tetrahydroquinoline-8-carboxamides and thiocarboxamides.
摘要翻译: 本发明涉及四氢喹啉的新型硅衍生物,其是制备5,6,7,8-四氢喹啉-8-甲酰胺和硫代羧酰胺的方法中的中间体。
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公开(公告)号:US4046895A
公开(公告)日:1977-09-06
申请号:US651748
申请日:1976-01-23
IPC分类号: C07D221/12 , C07D221/16 , C07D215/48 , A61K31/47
CPC分类号: C07D221/16 , C07D221/12
摘要: The invention provides a compound of formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent hydrogen or alkyl of 1-6 carbon atoms, R.sup.3 represents hydrogen, alkyl of 1-6 carbon atoms, or phenyl, X is Na, K, Li, or CSNHR.sup.4 wherein R.sup.4 is hydrogen or alkyl of 1-6 carbon atoms and n is 3, 4 or 5 or a pharmaceutically acceptacle acid addition salt of a compound where X is CSNHR.sup.4.The compounds of formula I wherein X is CSNHR.sup.4 are anti-ulcer agents. Those in which X is Na, K or Li are intermediates.
摘要翻译: 本发明提供式I化合物(I)其中R 1和R 2相同或不同,表示氢或1-6个碳原子的烷基,R 3表示氢,1-6个碳原子的烷基或苯基, X是Na,K,Li或CSNHR 4,其中R 4是氢或1-6个碳原子的烷基,n是3,4或5,或其中X是CSNHR 4的化合物的药学上接受酸加成盐。
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