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    Antitumor compounds
    2.
    发明授权
    Antitumor compounds 失效
    抗菌化合物

    公开(公告)号：US5126351A

    公开(公告)日：1992-06-30

    申请号：US645373

    申请日：1991-01-24

    申请人： Michael J. Luzzio ,  Jeffrey M. Besterman ,  Michael G. Evans ,  M. Ross Johnson

    发明人： Michael J. Luzzio ,  Jeffrey M. Besterman ,  Michael G. Evans ,  M. Ross Johnson

    IPC分类号： C07D491/04 ,  C07D491/056

    CPC分类号： C07D491/04

    摘要： The present invention relates to the compounds of formula (I), ##STR1## wherein: R.sup.1 is hydrogen, hydroxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or methoxymethoxy;R.sup.3 is hydrogen, hydroxy, amino, methoxy, methoxymethyoxy, or taken together with R.sup.2, methylenedioxy (also known as 1,3-dioxolo);R.sup.4 is hydrogen, hydroxy, methoxy, methoxymethoxy, benzyl, di(C.sub.1-4)alkylaminomethyl or, taken together with R.sup.3, methylenedioxy;R.sup.5 is hydrogen or hydroxy; provided that at least one of R.sup.1 through R.sup.5 is other than hydrogen; andi) X.sup.2 is hydroxy or methoxy with X.sup.1, X.sup.3 and X.sup.4 being hydrogen; orii) X.sup.1 taken together with X.sup.2,X.sup.2 taken together with X.sup.3 or X.sup.3 taken together with X.sup.4, is methylenedioxy, provided that each of the remaining respective X.sup.1, X.sup.2, X.sup.3 and X.sup.4 substituents are hydrogen,intermediates in the synthesis of them, pharmaceutical formulation containing them, their use as inhibitors of topoisomerase and their use in the treatment of tumors.

    Water soluble camptothecin derivatives
    4.
    发明授权
    Water soluble camptothecin derivatives 失效
    水溶性喜树碱衍生物

    公开(公告)号：US5559235A

    公开(公告)日：1996-09-24

    申请号：US258136

    申请日：1994-06-10

    申请人： Michael J. Luzzio ,  Jeffrey M. Besterman ,  Michael G. Evans ,  Peter L. Myers

    发明人： Michael J. Luzzio ,  Jeffrey M. Besterman ,  Michael G. Evans ,  Peter L. Myers

    IPC分类号： C07D317/66 ,  C07D319/18 ,  C07D491/22 ,  A61K31/47

    CPC分类号： C07D319/18 ,  C07D317/66

    摘要： The present invention relates to water soluble, camptothecin derivatives of formula (I), ##STR1## wherein: 1) R.sup.1 and R.sup.2 represent independently, hydrogen, lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl;ii) R.sup.1 represents hydrogen, lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl or lower alkoxy lower alkyl, and R.sup.2 represents --COR.sup.3,wherein:R.sup.3 represents hydrogen, lower alkyl, perhalo-lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy or lower alkoxy lower alkyl; oriii) R.sup.1 and R.sup.2 taken together with the linking nitrogen form a saturated 3 to 7 atom heterocyclic group of formula (IA) ##STR2## wherein: Y represents O, S, SO, SO.sub.2, CH.sub.2 or NR.sup.4wherein:R.sup.4 represents hydrogen, lower alkyl, perhalo lower alkyl, aryl, aryl substituted with one or more lower alkyl, lower alkoxy, halogen, nitro, amino, lower alkyl amino, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups or;--COR.sup.5,wherein:R.sup.5 represents hydrogen, lower alkyl, perhalo-lower alkyl, lower alkoxy, aryl, aryl substituted with one or more lower alkyl, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups or;the pharmaceutically acceptable salts thereof; their use in the treatment of tumors and methods of their preparation.

    摘要翻译： 本发明涉及式（I）的水溶性喜树碱衍生物，其中：1）R1和R2独立地表示氢，低级烷基，C3-7）环烷基，C3-7）环烷基低级烷基 低级烯基，羟基低级烷基，低级烷氧基低级烷基; ii）R1表示氢，低级烷基，C3-7）环烷基，C3-7）环烷基低级烷基，低级烯基，羟基低级烷基或低级烷氧基低级烷基，R2表示-COR3，其中：R3表示氢，低级烷基， 全卤代低级烷基，C3-7）环烷基，C3-7）环烷基低级烷基，低级烯基，羟基低级烷基，低级烷氧基或低级烷氧基低级烷基; 或（iii）R 1和R 2与连接氮一起形成式（IA）的饱和3至7个原子的杂环基（IA）其中：Y表示O，S，SO，SO 2，CH 2或NR 4，其中：R 4 代表氢，低级烷基，全卤代低级烷基，芳基，被一个或多个低级烷基，低级烷氧基，卤素，硝基，氨基，低级烷基氨基，全卤代低级烷基，羟基低级烷基，低级烷氧基低级烷基取代的芳基。 -COR 5，其中：R 5表示氢，低级烷基，全卤代低级烷基，低级烷氧基，芳基，被一个或多个低级烷基，全卤代低级烷基，羟基低级烷基，低级烷氧基低级烷基取代的芳基。 其药学上可接受的盐; 其用于治疗肿瘤及其制备方法。

    Substituted oxindole derivatives as tyrosine kinase inhibitors
    5.
    发明授权
    Substituted oxindole derivatives as tyrosine kinase inhibitors 失效
    取代的羟吲哚衍生物作为酪氨酸激酶抑制剂

    公开(公告)号：US07071217B2

    公开(公告)日：2006-07-04

    申请号：US10362743

    申请日：2001-08-23

    申请人： Scott Howard Dickerson ,  Robert N Hunter ,  Lee Frederick Kuyper ,  Karen Elizabeth Lackey ,  Michael J. Luzzio ,  Edgar Raymond Wood, III

    发明人： Scott Howard Dickerson ,  Robert N Hunter ,  Lee Frederick Kuyper ,  Karen Elizabeth Lackey ,  Michael J. Luzzio ,  Edgar Raymond Wood, III

    IPC分类号： A61K31/44 ,  C07D401/02

    CPC分类号： C07D401/12 ,  C07D209/34 ,  C07D209/40 ,  C07D417/12

    摘要： The present invention is related to oxindole derivatives of structure (I), compositions containing the same, and methods of use and manufacture of the same. Such compounds generally are useful pharmacologically as agents in those disease states alleviated by the alteration of mitogen activated signaling pathways in general, and in particular in the inhibition or antagonism of protein kinases, which pathologically involve aberrant cellular proliferation. Such disease states include tumor growth, restenosis, atherosclerosis, pain and thrombosis, In particular, the present invention relates to a series of substituted oxindole compounds, which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in cancer therapy and chronic pain indications.

    摘要翻译： 本发明涉及结构（I）的羟吲哚衍生物，含有它们的组合物及其使用和制造方法。 这些化合物通常在药理学上作为通常通过改变促分裂原活化的信号通路而减轻的疾病状态中的药物有用，特别是在病理学上涉及异常细胞增殖的蛋白激酶的抑制或拮抗作用中。 这种疾病状态包括肿瘤生长，再狭窄，动脉粥样硬化，疼痛和血栓形成。特别地，本发明涉及一系列取代的羟吲哚化合物，其表现出Trk家族蛋白酪氨酸激酶抑制，并且其可用于癌症治疗和慢性疼痛适应症 。

    Cyclic antitumor compounds
    6.
    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.

    Methods for Augmenting Bone
    8.
    发明申请
    Methods for Augmenting Bone 审中-公开
    增强骨的方法

    公开(公告)号：US20090118316A1

    公开(公告)日：2009-05-07

    申请号：US11570815

    申请日：2005-06-10

    申请人： Lisa M. Olson ,  Thomas A. Brown ,  Leonard Buckbinder ,  Angel Guzman-Perez ,  John C. Kath ,  Hua Zhu Ke ,  Michael J. Luzzio

    发明人： Lisa M. Olson ,  Thomas A. Brown ,  Leonard Buckbinder ,  Angel Guzman-Perez ,  John C. Kath ,  Hua Zhu Ke ,  Michael J. Luzzio

    IPC分类号： A61K31/506 ,  A61K31/405 ,  A61K31/40

    CPC分类号： A61K31/506 ,  A61K31/00

    摘要： The present invention relates to methods of stimulating osteoblast function with a PYK2 inhibitor in subjects with osteoporosis, bone fractures, non-unions, pseudoarthroses, periodontal disease or other disorders of bone metabolism. Optionally, the method further comprises administration of a second therapeutic bone agent. The present invention also relates to methods to identify a PYK2 inhibitor effective as a therapeutic bone agent comprising administering a test agent to an osteoblast-like cell and determining if osteoblast function is stimulated. Optionally, the identifying method further comprises contacting the test agent with PYK2 and determining if PYK2 activity is inhibited.

    摘要翻译： 本发明涉及在具有骨质疏松症，骨折，非联合，假性关节炎，牙周病或其他骨代谢紊乱的受试者中用PYK2抑制剂刺激成骨细胞功能的方法。 任选地，所述方法还包括施用第二治疗骨剂。 本发明还涉及鉴定有效作为治疗性骨质的PYK2抑制剂的方法，其包括向成骨细胞样细胞施用测试试剂并确定是否刺激成骨细胞功能。 任选地，识别方法还包括使测试试剂与PYK2接触并确定PYK2活性是否被抑制。

    Benzimidazole derivatives useful as antiproliferative agents
    9.
    发明授权
    Benzimidazole derivatives useful as antiproliferative agents 有权
    可用作抗增殖剂的苯并咪唑衍生物

    公开(公告)号：US07019147B1

    公开(公告)日：2006-03-28

    申请号：US10148335

    申请日：2000-11-10

    申请人： Wayne E. Barth ,  Michael J. Luzzio ,  Joseph P. Lyssikatos

    发明人： Wayne E. Barth ,  Michael J. Luzzio ,  Joseph P. Lyssikatos

    IPC分类号： C07D27/02 ,  C07D401/00 ,  C07D215/20 ,  A61K31/47 ,  A01N43/50

    CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07D491/10

    摘要： The invention relates to compounds of formula (1) and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R7, R8, R9, R10, and R11 are as defined herein. The invention also relates to methods of treating abnormal cell growth, such as cancer, in mammals by administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula (1). The invention also relates to methods of preparing the compounds of formula (1).

    摘要翻译： 本发明涉及式（1）的化合物及其药学上可接受的盐，前药和溶剂化物，其中R 1，R 7，R 8， >，R 9，R 10和R 11如本文所定义。 本发明还涉及通过施用式1化合物和用于治疗含有式（1）化合物的这种病症的药物组合物来治疗哺乳动物中异常细胞生长如癌症的方法。 本发明还涉及制备式（1）化合物的方法。