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    Antidepressant azaheterocyclylmethyl derivatives of 1,4-dioxino[2,3-b]pyridine
    2.
    发明授权
    Antidepressant azaheterocyclylmethyl derivatives of 1,4-dioxino[2,3-b]pyridine 失效
    1,4-二氧杂环己烯并[2,3-b]吡啶的抗抑郁药氮杂环甲基衍生物

    公开(公告)号：US06656950B2

    公开(公告)日：2003-12-02

    申请号：US10127923

    申请日：2002-04-23

    申请人： Megan Tran ,  Gary P. Stack

    发明人： Megan Tran ,  Gary P. Stack

    IPC分类号： A61K31436

    CPC分类号： C07D491/04

    摘要： Compounds of the formula useful for the treatment of depression, obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction, eating disorders, obesity, addictive disorders caused by ethanol or cocaine abuse, and dysthymia.

    摘要翻译： 治疗抑郁症，强迫症，恐慌发作，广泛性焦虑症，社会焦虑症，性功能障碍，进食障碍，肥胖症，乙醇或可卡因滥用引起的成瘾性疾病以及精神抑制的化合物。

    Heterocyclic derivatives of quinolinone benimidazoles
    4.
    发明授权
    Heterocyclic derivatives of quinolinone benimidazoles 失效
    喹啉酮咪唑的杂环衍生物

    公开(公告)号：US06756383B2

    公开(公告)日：2004-06-29

    申请号：US09943382

    申请日：2001-08-30

    申请人： Paul A. Renhowe ,  Timothy D. Machajewski ,  Cynthia M. Shafer ,  Mary Ellen Wernette Hammond ,  Sabina Pecchi

    发明人： Paul A. Renhowe ,  Timothy D. Machajewski ,  Cynthia M. Shafer ,  Mary Ellen Wernette Hammond ,  Sabina Pecchi

    IPC分类号： A61K31436

    CPC分类号： C07D471/04 ,  C07D495/04

    摘要： Organi c compounds having the structural formulas I, II, and III are provided where the variables have the values described herein and R1 and R2 in structure I join together to form a 5 to 7 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z is an O, S, NH or NR group in structures I and II. Pharmaceutical formulations include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. A method of treating a patient includes administering a pharmaceutical formulation according to the invention to a patient in need thereof.

    摘要翻译： 提供具有结构式I，II和III的有机化合物，其中变量具有本文所述的值，结构I中的R 1和R 2连接在一起形成5至7元取代或未取代的环，包括 至少一个O，N或S原子，Z是结构I和II中的O，S，NH或NR基团。药物制剂包括有机化合物或其药学上可接受的盐和药学上可接受的载体。 治疗患者的方法包括向有需要的患者施用本发明的药物制剂。

    Methods for inhibiting the growth of tumors with 7-substituted camptothecin derivatives
    5.
    发明授权
    Methods for inhibiting the growth of tumors with 7-substituted camptothecin derivatives 失效
    用7-取代的喜树碱衍生物抑制肿瘤生长的方法

    公开(公告)号：US06306868B1

    公开(公告)日：2001-10-23

    申请号：US09643256

    申请日：2000-08-22

    申请人： Lucio Merlini ,  Sergio Penco ,  Franco Zunino

    发明人： Lucio Merlini ,  Sergio Penco ,  Franco Zunino

    IPC分类号： A61K31436

    CPC分类号： C07D491/22

    摘要： Compounds of formula (I), wherein: R1 is —CN, —CH(CN)—R4, —CH═C(CN)—R4, —CH2—CH(CN)—R4, —C(═NOH)—NH2, —C(═NH)—NH2, —CH═C(NO2)—R4, —CH(CN)—R5, —CH(CH2NO2)—R5; 5-tetrazolyl, 2-(4,5-dihydrooxazolyl), 1,2,4-oxadiazolin-3-yl-5-one; R2 is hydrogen; R3 is hydrogen, OR6; R4 is hydrogen, C1-C6 linear or branched alkyl, CN, COOR7; R5 is hydrogen, OR8; R6 is hydrogen, C1-C6 linear or branched alkyl, (C6-C12) aryl (C1-C4) alkyl, (C1-C4) alkoxy (C1-C4) alkyl, (C1-C4) alkyl (C6-C12) aryl, (C6-C12) aryl (C2-C4) acyl, (C2-C4) acyl, amino (C1-C4) alkyl, amino (C2-C4) acyl, glycosyl; R7 is hydrogen, C1-C6 linear or branched alkyl, (C6-C12) aryl (C1-C4) alkyl, (C1-C4) alkoxy (C1-C4) alkyl, (C1-C4) alkyl (C6-C12) aryl; R8 has the same meanings of R6, independently of the latter. These compounds are active as topoisomerase I inhibitors and can be used as antitumor drugs.

    摘要翻译： 式（I）化合物，其中：R1是-CN，-CH（CN）-R4，-CH = C（CN）-R4，-CH2-CH（CN）-R4，-C（= NOH） ，-C（= NH）-NH 2，-CH = C（NO 2）-R 4，-CH（CN）-R 5，-CH（CH 2 NO 2） 5-四唑基，2-（4,5-二氢恶唑基），1,2,4-恶二唑啉-3-基-5-酮; R2是氢; R3是氢，OR6; R4是氢，C1-C6直链或支链烷基，CN，COOR7; R5是氢，OR8; R6是氢，C1-C6直链或支链烷基，（C6-C12）芳基（C1-C4）烷基，（C1-C4）烷氧基（C1-C4）烷基，（C1-C4） ，（C 6 -C 12）芳基（C 2 -C 4）酰基，（C 2 -C 4）酰基，氨基（C 1 -C 4）烷基，氨基（C 2 -C 4）酰基，糖基; R7是氢，C1-C6直链或支链烷基，（C6-C12）芳基（C1-C4）烷基，（C1-C4）烷氧基（C1-C4）烷基，（C1-C4） ; R8与R6具有相同的含义，独立于后者。 这些化合物作为拓扑异构酶I抑制剂是有活性的，可用作抗肿瘤药物。

    Furopyridine antibacterials
    6.
    发明授权
    Furopyridine antibacterials 失效
    呋喃西林抗菌剂

    公开(公告)号：US06277860B1

    公开(公告)日：2001-08-21

    申请号：US09430763

    申请日：1999-10-29

    申请人： Yutaka Sugie ,  Akemi Sugiura ,  Nobuji Yoshikawa ,  Susan J. I Truesdell ,  John W. Wong

    发明人： Yutaka Sugie ,  Akemi Sugiura ,  Nobuji Yoshikawa ,  Susan J. I Truesdell ,  John W. Wong

    IPC分类号： A61K31436

    CPC分类号： C07D491/04 ,  C07D491/14

    摘要： This invention provides a compound of formula (I): or pharmaceutically acceptable salts thereof, wherein X1 and X2 are C or N, respectively; R1 and R2 are independently phenyl optionally substituted with a hydroxy group with proviso that X1 and X2 are not simultaneously C or N, when X1 is N, R1 is absent, and when X2 is N, R2 is absent; R3 is methyl or hydroxymethyl; R4 is formyl, hydroxymethyl or hydroxy C3-6 alkenyl; R5 is hydroxy, C3-6 alkenyl or hydroxy C3-6 alkenyl; or R4 and R5, together with the carbon atoms in the furopyridine ring to which they are attached, may form the following ring (to be fused with the furopyridine ring): with the proviso that when R3 is methyl and R5 is 2-buten-2-yl, X2 is not N. These compounds and pharmaceutical compositions containing such compounds are useful for treating infectious diseases caused by bacteria.

    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X 1和X 2分别是C或N; R1和R2独立地为羟基取代的苯基，条件是X1和X2不同时为C或N，当X1为N时，R1不存在，当X2为N时，R2为不; R3是甲基或羟甲基; R4是甲酰基，羟甲基或羟基C 3-6烯基; R5是羟基，C3-6烯基或羟基C3-6烯基; 或R 4和R 5与它们所连接的呋喃啶环中的碳原子一起形成以下环（与呋喃啶环稠合）：条件是当R 3为甲基且R 5为2-丁烯基时， 2-这些化合物和含有这些化合物的药物组合物可用于治疗由细菌引起的感染性疾病。

    Preparation of a camptothecin derivative by intramolecular cyclisation
    7.
    发明授权
    Preparation of a camptothecin derivative by intramolecular cyclisation 失效
    通过分子内环化制备喜树碱衍生物

    公开(公告)号：US06821982B2

    公开(公告)日：2004-11-23

    申请号：US10395806

    申请日：2003-03-24

    申请人： Francis Gerard Fang ,  Edward McDonald Huie ,  Shiping Xie ,  Daniel L. Comins

    发明人： Francis Gerard Fang ,  Edward McDonald Huie ,  Shiping Xie ,  Daniel L. Comins

    IPC分类号： A61K31436

    CPC分类号： C07D491/22 ,  C07D519/00

    摘要： The present invention relates to a method for the preparation for camptothecin and camptothecin-like compounds and to novel intermediates used in this preparation. In particular, the invention provides a process for the preparation of the camptothecin derivative of formula (I′) known by the chemical name “7-(4-methylpiperazino-methylene)-10,11-ethylenedioxy-20(R,S)-camptothecin”, which comprises cyclising the compound of formula (II′), wherein X is halogen, particularly chloro, bromo, or iodo; and when the compound of formula (I′) is obtained as a mixture of enantiomers optionally resolving the mixture to obtain the desired enantiomer; and/or if desired, converting the resulting compound of formula (I′) or a salt thereof into a physiologically acceptable salt or solvate thereof.

    摘要翻译： 本发明涉及一种制备喜树碱和喜树碱样化合物的方法以及本制剂中使用的新型中间体。 特别地，本发明提供制备式（I'）的喜树碱衍生物的方法，该化合物名称为“7-（4-甲基哌嗪基 - 亚甲基）-10,11-亚乙基二氧基-20（R，S） - 喜树碱“，其包括使式（II'）化合物环化，其中X是卤素，特别是氯，溴或碘; 并且当以对映异构体的混合物获得式（I'）化合物时，任选地拆分混合物以获得所需的对映异构体; 和/或如果需要，将所得的式（I'）化合物或其盐转化为其生理学上可接受的盐或溶剂化物。

    O-alkylated rapamycin derivatives and their use, particularly as immunosuppressants
    9.
    发明授权
    O-alkylated rapamycin derivatives and their use, particularly as immunosuppressants 失效
    O-烷基化雷帕霉素衍生物及其用途，特别是作为免疫抑制剂

    公开(公告)号：US06440990B1

    公开(公告)日：2002-08-27

    申请号：US08862911

    申请日：1997-05-23

    申请人： Sylvain Cottens ,  Richard Sedrani

    发明人： Sylvain Cottens ,  Richard Sedrani

    IPC分类号： A61K31436

    CPC分类号： C07D498/18

    摘要： Novel derivatives of rapamycin, particularly 9-deoxo-rapamycins, 26-dihydro-rapamycins, and 40-O-substituted and 28,40-O,O-disubstituted rapamycins. are found to have pharmaceutical utility, particularly as immunosuppressants.

    摘要翻译： 雷帕霉素的新型衍生物，特别是9-脱氧 - 雷帕霉素，26-二氢 - 雷帕霉素和40-O-取代的和2840- O，O-二取代的雷帕霉素。 被发现具有药物效用，特别是作为免疫抑制剂。