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21 条记录 (耗时 0.029 秒)

    Tyrosine-derived compounds as calcium channel antagonists
    12.
    发明授权
    Tyrosine-derived compounds as calcium channel antagonists 失效
    酪氨酸衍生化合物作为钙通道拮抗剂

    公开(公告)号：US06323243B1

    公开(公告)日：2001-11-27

    申请号：US09694921

    申请日：2000-10-24

    申请人： Michael Francis Rafferty ,  Yuntao Song

    发明人： Michael Francis Rafferty ,  Yuntao Song

    IPC分类号： A61K31132

    CPC分类号： C07D295/13 ,  C07C237/20 ,  C07C237/22 ,  C07C2601/08

    摘要： The present invention provides compounds that block calcium channels and have the Formula I: and pharmaceutically acceptable salts, esters, and pro-drugs thereof, wherein R1 and R2 are independently H, phenylcyclopentylcarbonyl, C1-C7 alkyl, cyclohexylmethyl, benzyl, C1-C5 alkylbenzyl, or C1-C5 alkoxybenzyl, A is —C(O)— or —CH2—; R3 is H or —CH3; R4 is C1-C4 alkyl or piperidin-1-ylethyl; R5 is phenyl-(CH2)n—, C1-C4 alkylphenyl-(CH2)n—, or halophenyl-(CH2)n—; and n is 1 or 2. The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.

    摘要翻译： 本发明提供了阻断钙通道并具有式I的化合物及其药学上可接受的盐，酯和前药，其中R 1和R 2独立地为H，苯基环戊基羰基，C 1 -C 7烷基，环己基甲基，苄基，C 1 -C 5烷基苄基 或C 1 -C 5烷氧基苄基，A是-C（O） - 或-CH 2 - ; R 3是H或-CH 3; R 4是C 1 -C 4烷基或哌啶-1-基乙基; R 5是苯基 - （CH 2） C 1 -C 4烷基苯基 - （CH 2）n - 或卤代苯基 - （CH 2）n - andn为1或2.本发明还提供含有式I化合物的药物组合物及其用于治疗中风，脑缺血，头部创伤和癫痫的方法。

    Reduced dipeptide analogues as calcium channel antagonitsts
    18.
    发明授权
    Reduced dipeptide analogues as calcium channel antagonitsts 失效
    还原二肽类似物作为钙通道拮抗剂

    公开(公告)号：US06362174B1

    公开(公告)日：2002-03-26

    申请号：US09925947

    申请日：2001-08-09

    申请人： Michael Francis Rafferty ,  Yuntao Song

    发明人： Michael Francis Rafferty ,  Yuntao Song

    IPC分类号： A61K31195

    CPC分类号： C07D295/215 ,  C07C237/20 ,  C07D295/13

    摘要： The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma. The novel compounds provided by this invention have the Formula I: wherein R1 is H or methyl, R2 is H, azepanylcarbonyl, C1-C7 alkyl, —(CH2)n-phenyl, wherein the phenyl is unsubstituted or substituted with C1-C4 alkyl, C1-C4 alkoxy, or halo, R3 is C1-C5 alkyl, X is —NR4R5 or —OR7, R4 and R5 are independently H, C1-C5 alkyl, or R4 and R5 together with the nitrogen to which they are both bound form: R6 is —(CH2)n-phenyl, wherein the phenyl is unsubstituted or substituted with C1-C4 alkyl, C1-C4 alkoxy, or halo, A and B are independently —CO— or —CH2—, provided that A and B are not both —CO—, R7 is C1-C5 alkyl, Z is —CH2—, —O—, —S—, or —N(R8)—, R8 is H or C1-C6 alkyl, and n is 1 or 2.

    摘要翻译： 本发明提供新型的N型钙通道阻滞剂，包含它们的组合物及其使用方法。 本发明的化合物可用于治疗中风，脑缺血，疼痛，癫痫和头部创伤。 本发明提供的新化合物具有式I：其中R 1是H或甲基，R 2是H，氮杂环庚烷基羰基，C 1 -C 7烷基， - （CH 2）n - 苯基，其中苯基是未取代的或被C 1 -C 4烷基， C 1 -C 4烷氧基或卤素，R 3是C 1 -C 5烷基，X是-NR 4 R 5或-OR 7，R 4和R 5独立地是H，C 1 -C 5烷基或R 4和R 5与它们所连接的氮一起形成： R 6是 - （CH 2）n - 苯基，其中苯基是未取代的或被C 1 -C 4烷基，C 1 -C 4烷氧基或卤素取代，A和B独立地是-CO-或-CH 2 - ，条件是A和B是 不是-CO-，R7是C1-C5烷基，Z是-CH2-，-O - ， - S-或-N（R8） - ，R8是H或C1-C6烷基，并且n是1或2。

    Reduced dipeptide analogues as calcium channel antagonists
    19.
    发明授权
    Reduced dipeptide analogues as calcium channel antagonists 失效
    减少二肽类似物作为钙通道拮抗剂

    公开(公告)号：US06316440B1

    公开(公告)日：2001-11-13

    申请号：US09381983

    申请日：1999-12-27

    申请人： Michael Francis Rafferty ,  Yuntao Song

    发明人： Michael Francis Rafferty ,  Yuntao Song

    IPC分类号： C07D29520

    CPC分类号： C07D295/215 ,  C07C237/20 ,  C07D295/13

    摘要： The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma. The novel compounds provided by this invention have Formula (1), wherein R1 is H or methyl; R2 is H, azepanylcarbonyl, C1-C7 alkyl, —(CH2)n-phenyl, wherein the phenyl is unsubstituted or substituted with C1-C4 alkyl, C1-C4 alkoxy, or halo; R3 is C1-C5 alkyl; X is —NR4R5 or —OR7; R4 and R5 are independently H, C1-C5 alkyl; or R4 and R5 together with the nitrogen to which they are both bound form formulae (a); (b); (c); (d) or (e); R6 is —(CH2)n-phenyl, wherein the phenyl is unsubstituted or substituted with C1-C4 alkyl, C1-C4 alkoxy, or halo; A and B are independently —CO— or —CH2—, provided that A and B are not both —CO—; R7 is C1-C5 alkyl; Z is —CH2—, —O—, —S—, or —N(R8)—; R8 is H or C1-C6 alkyl; and n is 1 or 2.

    摘要翻译： 本发明提供新型的N型钙通道阻滞剂，包含它们的组合物及其使用方法。 本发明的化合物可用于治疗中风，脑缺血，疼痛，癫痫和头部创伤。 本发明提供的新化合物具有式（1），其中R 1是H或甲基; R 2是H，氮杂环庚基羰基，C 1 -C 7烷基， - （CH 2）n - 苯基，其中苯基是未取代的或被C 1 -C 4烷基，C 1 -C 4烷氧基或卤素取代; R3是C1-C5烷基; X是-NR 4 R 5或-OR 7; R4和R5独立地是H，C1-C5烷基; 或R 4和R 5与它们所连接的氮一起形成式（a）; （b）; （C）; （d）或（e）; R 6是 - （CH 2）n - 苯基，其中苯基是未取代的或被C 1 -C 4烷基，C 1 -C 4烷氧基或卤素取代; A和B独立地为-CO-或-CH2-，条件是A和B不同时为-CO-; R7是C1-C5烷基; Z是-CH 2 - ， - O - ， - S-或-N（R 8） - 。 R8是H或C1-C6烷基; n为1或2。