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    Cyclic antitumor compounds
    1.
    发明授权
    Cyclic antitumor compounds 失效
    环状抗肿瘤化合物

    公开(公告)号：US5318976A

    公开(公告)日：1994-06-07

    申请号：US931611

    申请日：1992-08-18

    申请人： Michael J. Luzzi ,  Jeffrey Besterman ,  Michael G. Evans ,  M. Ross Johnson ,  Milana Dezube ,  Salvatore Profeta, Jr.

    发明人： Michael J. Luzzi ,  Jeffrey Besterman ,  Michael G. Evans ,  M. Ross Johnson ,  Milana Dezube ,  Salvatore Profeta, Jr.

    IPC分类号： C07D221/18 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/056 ,  C07D491/14 ,  C07D491/147 ,  C07D491/153 ,  A61K31/435 ,  C07D471/14

    CPC分类号： C07D221/18 ,  C07D471/04 ,  C07D491/04 ,  C07D491/14

    摘要： The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or amino;R.sup.3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, --OCONH.sub.2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R.sup.2 or R.sup.4, methylenedioxy or ethylenedioxy;R.sup.4 is hydrogen, hydroxy or amino;Z is --CH.sub.2 --, --O-- or --NH--; anda) X.sup.1 is hydrogen;X.sup.2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; andX.sup.3 is hydrogen or hydroxy; orb) X.sup.2 taken together with X.sup.3 is methylenedioxy or ethylenedioxy, and X.sup.1 is hydrogenor a pharmaceutically acceptable salt thereof provided that:i) at least one of R.sup.1 through R.sup.4 is other than hydrogen.

    摘要翻译： 本发明涉及式（I）的某些取代的四环稠合喹啉衍生物：其中：R 1是氢，羟基，氟，氯，溴，碘，甲氧基或氨基; R2是氢，羟基，甲氧基或氨基; R3是氢，羟基，甲氧基，甲氧基甲氧基，氨基，-OCONH2，[2（5H）-3,4-二氢-3-呋喃酮]，2-羟基乙氧基，2-氨基乙氧基，3-羟基丙氧基或3-氨基丙氧基; 或与R2或R4一起亚甲二氧基或亚乙二氧基取代; R4是氢，羟基或氨基; Z是-CH 2 - ， - O-或-NH-; 和a）X1是氢; X2是氢，羟基，氟，氯，溴，碘或甲氧基; X3为氢或羟基; 或b）X 2与X 3一起为亚甲二氧基或亚乙二氧基，并且X 1为氢或其药学上可接受的盐，条件是：i）R 1至R 4中的至少一个不是氢。

    Cyclic antitumor compounds
    2.
    发明授权
    Cyclic antitumor compounds 失效
    循环抗体化合物

    公开(公告)号：US5223506A

    公开(公告)日：1993-06-29

    申请号：US710230

    申请日：1991-06-04

    申请人： Michael J. Luzzio ,  Jeffrey M. Besterman ,  Michael G. Evans ,  M. Ross Johnson ,  Milana Dezube ,  Salvatore Profeta, Jr.

    发明人： Michael J. Luzzio ,  Jeffrey M. Besterman ,  Michael G. Evans ,  M. Ross Johnson ,  Milana Dezube ,  Salvatore Profeta, Jr.

    IPC分类号： C07D221/18 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D491/056 ,  C07D491/14 ,  C07D491/147 ,  C07D491/153

    CPC分类号： C07D221/18 ,  C07D471/04 ,  C07D491/04 ,  C07D491/14

    摘要： The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or amino;R.sup.3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, --OCONH.sub.2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R.sup.2 or R.sup.4, methylenedioxy or ethylenedioxy;R.sup.4 is hydrogen, hydroxy or amino;Z is --CH.sub.2 --, --O-- or --NH--; anda) X.sup.1 is hydrogen; X.sup.2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; and X.sup.3 is hydrogen or hydroxy; orb) X.sup.2 taken together with X.sup.3 is methylenedioxy or ethylenedioxy, and X.sup.1 is hydrogenor a pharmaceutically acceptable salt thereof provided that:i) at least one of R.sup.1 through R.sup.4 is other than hydrogen;ii) when R.sup.1 is methoxy, R.sup.2 is hydroxy or methoxy, R.sup.3 is hydrogen or methoxy and R.sup.4 is hydrogen;iii) when R.sup.2 is hydroxy, methoxy or amino, R.sup.3 is hydrogen, hydroxy or methoxy, and R.sup.4 is hydrogen;iv) when R.sup.4 is hydroxy or amino, R.sup.1 and R.sup.3 are hydrogen and R.sup.2 is hydroxy or amino; and.v) when R.sup.1 is fluoro, chloro, iodo or amino, R.sup.2 is hydrogen, hydroxy or methoxy, R.sup.3 is hydrogen, hydroxy or methoxy and R.sup.4 is hydrogenand the use of these compounds as topoisomerase inhibitors and antitumor agents.

    CCK or gastrin modulating benzo �b!�1,4! diazepines derivatives
    6.
    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
    7.
    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。