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17 条记录 (耗时 0.047 秒)

    Antitumor compounds
    1.
    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.

    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.

    Water soluble camptothecin derivatives
    3.
    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。

    Acyl phosphonate inhibitors of β-lactamases
    5.
    发明授权
    Acyl phosphonate inhibitors of β-lactamases 失效
    β-内酰胺酶的酰基膦酸酯抑制剂

    公开(公告)号：US07205285B2

    公开(公告)日：2007-04-17

    申请号：US10628649

    申请日：2003-07-28

    申请人： Jeffrey M. Besterman ,  Jubrail Rahil ,  Rex Pratt

    发明人： Jeffrey M. Besterman ,  Jubrail Rahil ,  Rex Pratt

    IPC分类号： A61K31/66 ,  C07F9/02

    CPC分类号： C07F9/65744 ,  C07F9/096 ,  C07F9/098 ,  C07F9/4093 ,  C07F9/657181 ,  C07F9/65742

    摘要： The invention provides novel β-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic β-lactamase inhibitors presently available, and which do not possess a β-lactam pharmacophore. These new inhibitors are fully synthetic, allowing ready access to a wide variety of structurally related analogs. Certain embodiments of these new inhibitors also bind bacterial DD-peptidases, thus potentially acting both as β-lactamase inhibitors and as antibiotics.

    摘要翻译： 本发明提供了新型β-内酰胺酶抑制剂，其在结构上与目前可获得的天然产物和半合成β-内酰胺酶抑制剂无关，并且不具有β-内酰胺药效团。 这些新的抑制剂是完全合成的，可以方便地访问各种结构相关的类似物。 这些新抑制剂的某些实施方案也结合细菌DD-肽酶，因此潜在地作为β-内酰胺酶抑制剂和抗生素起作用。

    Antifungal Agents and Uses Thereof
    9.
    发明申请
    Antifungal Agents and Uses Thereof 审中-公开
    抗真菌剂及其用途

    公开(公告)号：US20120046331A1

    公开(公告)日：2012-02-23

    申请号：US13213372

    申请日：2011-08-19

    申请人： Jeffrey M. Besterman

    发明人： Jeffrey M. Besterman

    IPC分类号： A61K31/185 ,  A61K31/351 ,  A61P31/10 ,  C07D209/08 ,  C07D309/12 ,  A61K31/404 ,  C07C259/10

    CPC分类号： A61K31/165 ,  A61K31/137 ,  A61K31/351 ,  A61K31/404 ,  A61K31/4196 ,  A61K31/496 ,  A61K45/06 ,  C07D209/04 ,  C07D309/10 ,  A61K2300/00

    摘要： This invention relates to new antifungal agents, compositions thereof, and methods for inhibiting the growth of fungi involved in infection and disease of keratinized tissue, such as onychomycosis. The invention also relates to new antifungal agents, compositions thereof, and methods for treating and/or preventing fungal infection and/or disease of keratinized tissue, such as onychomycosis. The invention further relates to a kit comprising said antifungal agent and use of said kit in treatment of fungal infection and/or disease of keratinized tissue, such as onychomycosis.

    摘要翻译： 本发明涉及新的抗真菌剂，其组合物，以及用于抑制角质化组织感染和疾病如真菌感染的真菌生长的方法。 本发明还涉及新的抗真菌剂，其组合物，以及用于治疗和/或预防角质化组织的真菌感染和/或疾病的方法，例如甲真菌病。 本发明还涉及包含所述抗真菌剂的试剂盒和所述试剂盒在治疗真菌感染和/或角质化组织疾病如甲癣的用途。