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    CCK or gastrin modulating benzo �b!�1,4! diazepines derivatives
    5.
    发明授权
    CCK or gastrin modulating benzo �b!�1,4! diazepines derivatives 失效
    CCK或胃泌素调节苯并[b] [1,4]二氮杂衍生物

    公开(公告)号：US5859007A

    公开(公告)日：1999-01-12

    申请号：US722051

    申请日：1996-11-14

    申请人： Christopher Joseph Aquino ,  Marcus Brackeen ,  Milana Dezube ,  Brad Richard Henke ,  Gavin Charles Hirst ,  Peter Walter Jeffs ,  Tanya Momtahen ,  Elizabeth Ellen Sugg ,  Edward Martin Suh ,  Timothy Mark Willson

    发明人： Christopher Joseph Aquino ,  Marcus Brackeen ,  Milana Dezube ,  Brad Richard Henke ,  Gavin Charles Hirst ,  Peter Walter Jeffs ,  Tanya Momtahen ,  Elizabeth Ellen Sugg ,  Edward Martin Suh ,  Timothy Mark Willson

    IPC分类号： A61K31/55 ,  A61P1/00 ,  A61P1/16 ,  A61P3/04 ,  C07D243/12 ,  C07D401/04 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D471/04 ,  C07D498/04 ,  A01N43/62

    CPC分类号： C07D401/04 ,  C07D243/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D471/04

    摘要： Benzo�b!�1,4!diazepine compounds of formula (I), where R.sup.1 is selected from C.sub.1 C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, phenyl, or substituted phenyl; R.sup.2 is selected from C.sub.3 -C.sub.6 alkyl, C.sub.3 C.sub.6 cycloalkyl, C.sub.3 -C.sub.6 alkenyl, benzyl, phenylC.sub.1 -C.sub.3 alkyl of substituted phenyl; or NR.sup.1 R.sup.2 together form 1,2,3,4-tetrahydroquinoline or benzazepine, mono-, di-, or trisubstituted independently with C.sub.1-6 alkyl C.sub.1-6 alkoxy or halogen substituents; p is an integer 0 or 1; q is an integer 0 or 1; r is an integer 0 or 1; t is an integer 0 or 1, provided that when r is 0 then t is 0; R.sup.3, R.sup.5, and R.sup.6 are independently hydrogen or C.sub.1-6 alkyl; R.sup.4 is C.sub.1-6 alkyl or C.sub.1-6 alkenyl; R.sup.7 is selected from the group consisting of hydrogen, C.sub.1-6 alkyl, C.sub.1-6 cycloalkyl, C.sub.1-6 alkenyl, phenyl, substituted phenyl, napthyl, heteroaryl, substituted heteroaryl, bicycloheteroaryl or substituted bicycloheteroaryl; or NR.sup.6 R.sup.7 together form a saturated 5,6, or 7 membered ring optionally interrupted by 1,2,3 or 4 N, S or O heteroatoms, with the proviso that any two O or S atoms are not bonded to each other, m is an integer selected from the group of 0, 1, 2, 3 or 4; R.sup.8 and R.sup.9 are selected from a variety of substituents; Z is hydrogen or halogen; novel intermediates, a pharmaceutical composition for treating obesity, gall bladder stasis, disorders of pancreatic secretion, methods for such treatment and processes for preparing compounds of formula (I).

    摘要翻译： PCT No.PCT / EP95 / 01336 Sec。 371日期：1996年11月14日 102（e）1996年11月14日PCT PCT 1995年4月13日PCT公布。 公开号WO95 / 28391 日期：1995年10月26日（I）式（I）的苯并[b] [1,4]二氮杂化合物，其中R 1选自C 1 -C 6烷基，C 3 -C 6环烷基，苯基或取代的苯基; R2选自C3-C6烷基，C3C6环烷基，C3-C6链烯基，苄基，取代苯基的苯基C1-3烷基; 或NR1R2一起形成1,2,3,4-四氢喹啉或苯并氮杂，独立地与C 1-6烷基C 1-6烷氧基或卤素取代基单取代，二取代或三取代; p是整数0或1; q是整数0或1; r为整数0或1; t为整数0或1，条件是当r为0时，t为0; R3，R5和R6独立地是氢或C1-6烷基; R4是C1-6烷基或C1-6链烯基; R 7选自氢，C 1-6烷基，C 1-6环烷基，C 1-6烯基，苯基，取代的苯基，萘基，杂芳基，取代的杂芳基，双环杂芳基或取代的双环杂芳基; 或NR6R7一起形成饱和的5,6或7元环，任选地被1,2,3或4个N，S或O杂原子间隔，条件是任何两个O或S原子彼此不结合，m是 选自0,1,2,3或4的整数; R8和R9选自多种取代基; Z是氢或卤素; 新型中间体，用于治疗肥胖的药物组合物，胆囊淤滞，胰腺分泌障碍，这种治疗方法和制备式（I）化合物的方法。

    Method of inducing cholecystokinin agonist activity using 1,4- Benzodiazepine compounds
    6.
    发明授权
    Method of inducing cholecystokinin agonist activity using 1,4- Benzodiazepine compounds 失效
    使用1,4-苯二氮卓类化合物诱导胆囊收缩素激动剂活性的方法

    公开(公告)号：US5795887A

    公开(公告)日：1998-08-18

    申请号：US718552

    申请日：1996-10-11

    申请人： Christopher Joseph Aquino ,  Milana Dezube ,  Ronald George Sherrill ,  Elizabeth Ellen Sugg ,  Jerzy Ryszard Szewczyk ,  Timothy Mark Willson

    发明人： Christopher Joseph Aquino ,  Milana Dezube ,  Ronald George Sherrill ,  Elizabeth Ellen Sugg ,  Jerzy Ryszard Szewczyk ,  Timothy Mark Willson

    IPC分类号： C07D243/14 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  A61P1/00 ,  A61P1/16 ,  A61P3/04 ,  A61P25/00 ,  A61P43/00 ,  C07D243/24 ,  C07D401/04 ,  C07D403/06 ,  C07D403/12 ,  C07D487/04 ,  A01N43/62 ,  C07D243/12

    CPC分类号： C07D401/04 ,  A61K31/55 ,  A61K31/5513 ,  C07D243/24 ,  C07D403/06 ,  C07D403/12 ,  C07D487/04

    摘要： A method of inducing a Cholescystokinin-A receptor agonist response in a mammal by administering a compound of formula (I), ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3-6 cycloalkyl, phenyl, or substituted phenyl; R.sup.2 is C.sub.3-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.3-6 alkenyl, benzyl, phenylC.sub.1-3 alkyl or substituted phenyl; or NR.sup.1 R.sup.2 together form 1,2,3,4-tetrahydroquinoline or benzazepine mono-, di-, or trisubstituted independently with C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen substituents; n is an integer selected from the grouping consisting of 0,1,2 or 3; p is the integer 0 or 1; q is the integer 0 or 1; r is the integer 0 or 1, provided that when q is 0 then r is 0; R.sup.3, R.sup.4, R.sup.5 and R.sup.8 are selected from a variety of substituents; X is nitrogen, nitroso or R.sup.8 ; m is an integer selected from the group consisting of 0, 1, 2 or 3; Y and Z are hydrogen or halogen, novel intermediates, a pharmaceutical composition for treating obesity, gall bladder stasis, disorders of pancreatic secretion, methods for such treatment and processes for preparing compounds of formula (I).

    摘要翻译： PCT No.PCT / EP95 / 01335 Sec。 371日期：1996年10月11日 102（e）日期1996年10月11日PCT提交1995年4月13日PCT公布。 WO95 / 28399 PCT公开号 日期1995年10月26日一种通过给予式（I）化合物，其中R1是C1-C6烷基，C3-6环烷基，苯基或取代的式（I）化合物来诱导哺乳动物中胆囊糖尿病A受体激动剂反应的方法 苯基; R2是C3-6烷基，C3-6环烷基，C3-6烯基，苄基，苯基C 1-3烷基或取代的苯基; 或NR1R2一起形成1,2,3,4-四氢喹啉或苯并氮杂单独，二或三取代为C 1-6烷基，C 1-6烷氧基或卤素取代基; n是从0,1,2或3组成的组中选择的整数; p是整数0或1; q是整数0或1; r为整数0或1，条件是当q为0时，r为0; R3，R4，R5和R8选自多种取代基; X为氮，亚硝基或R8; m是选自0,1,2或3的整数; Y和Z是氢或卤素，新的中间体，用于治疗肥胖的药物组合物，胆囊淤滞，胰腺分泌障碍，这种治疗的方法和制备式（I）化合物的方法。