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    Compounds, which are potent inhibitors of na+ / ca2+ exchange mechanism and are useful in the treatment of arrhythmias
    1.
    发明申请
    Compounds, which are potent inhibitors of na+ / ca2+ exchange mechanism and are useful in the treatment of arrhythmias 失效
    化合物，其是na + / ca2 +交换机制的有效抑制剂，并且可用于治疗心律失常

    公开(公告)号：US20040235905A1

    公开(公告)日：2004-11-25

    申请号：US10482396

    申请日：2004-06-08

    发明人： Tuula Koskelainen ,  Leena Otsomaa ,  Arto Karjalainen ,  Pekka Kotovuori ,  Jukka Tenhunen ,  Sirpa Rasku ,  Pentti Nore ,  Eija Tiainen ,  Olli Tormakangas

    IPC分类号： A61K031/443 ,  A61K031/4178 ,  A61K031/4025 ,  A61K031/382 ,  A61K031/353

    CPC分类号： C07D405/12 ,  C07C217/14 ,  C07C217/54 ,  C07C217/90 ,  C07C2602/08 ,  C07D213/64 ,  C07D311/28 ,  C07D311/58 ,  C07D311/60 ,  C07D411/12

    摘要： Therapeutically active compounds of formula (I): wherein X is nullOnull, nullCH2null or nullC(O)null; Z is nullCHR9null or valence bond; Y is nullCH2null, nullC(O)null, CH(OR10)null, nullCH(NR11R12)null, nullOnull, nullSnull, nullS(O)null or nullS(O2)null, provided that in case Z is a valence bond, Y is not C(O); the dashed line represents an optional double bond in which case Z is nullCR9null and Y is nullCHnull, C(OR10)null or nullC(NR11R12)null; R1 is null(CH2)nNR4R7 or one of the following groups: n is 1-4; R2 and R3 are independently H, lower alkyl, lower alkoxy, nullNO2, halogen, nullCF3, nullOH, nullNHR8 or nullCOOH, R4 and R7 are independently H, lower alkyl or lower hydroxyalkyl; R5 is H, lower alkoxy, nullCF3, nullNH2 or nullCN; R6 is nullNO2, nullNR14R19, nullCF3 or R8 and R16 are independently H or acyl; R9 is H or lower alkyl; R10 is H, alkylsulfonyl or acyl; R11 and R12 are independently H, lower alkyl or acyl; R13 and R18 are independently H or nullOR20; R14 and R19 are independently H, acyl, alkylsulfonyl, C(S)NHR17 or C(O)NHR17; R15 is H or NH2; R17 is H or lower alkyl; R20 is H or acyl; and pharmaceutically acceptable salts and esters thereof are disclosed. The compounds are potent inhibitors of Nanull/Ca2null exchange mechanism. 1

    摘要翻译： 式（I）的治疗活性化合物：其中X是-O-，-CH 2 - 或-C（O） - ; Z是-CHR9-或价键; Y是-CH 2 - ， - C（O） - ，CH（OR 10） - ， - CH（NR 11 R 12） - ， - O - ， - S - ， - S（O） - 或-S（O 2） 在Z是价键的情况下，Y不是C（O）; 虚线表示任选的双键，其中Z为-CR9-，Y为-CH-，C（OR10） - 或-C（NR11R12） - ; R1为 - （CH2）nNR4R7或以下基团之一：n为1-4; R2和R3独立地是H，低级烷基，低级烷氧基，-NO2，卤素，-CF3，-OH，-NHR8或-COOH，R4和R7独立地是H，低级烷基或低级羟烷基; R5是H，低级烷氧基，-CF3，-NH2或-CN; R 6是-NO 2，-NR 14 R 19，-CF 3或R 8，R 16独立地是H或酰基; R9为H或低级烷基; R 10为H，烷基磺酰基或酰基; R 11和R 12独立地为H，低级烷基或酰基; R 13和R 18独立地为H或-OR 20; R 14和R 19独立地为H，酰基，烷基磺酰基，C（S）NHR 17或C（O）NHR 17; R15是H或NH2; R 17为H或低级烷基; R 20是H或酰基; 及其药学上可接受的盐和酯。 这些化合物是Na + / Ca 2+交换机制的有效抑制剂。

    Benzofuran inhibitors of factor VIIa
    2.
    发明申请
    Benzofuran inhibitors of factor VIIa 有权
    因子VIIa的苯并呋喃抑制剂

    公开(公告)号：US20040235852A1

    公开(公告)日：2004-11-25

    申请号：US10850231

    申请日：2004-05-19

    发明人： Alan G. Olivero ,  Daniel P. Sutherlin

    IPC分类号： A61K031/501 ,  A61K031/443 ,  A61K031/343

    CPC分类号： C07D405/12 ,  C07D307/81

    摘要： Compounds of Formula I are useful for inhibiting serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein and have improved pharmacokinetic properties. These compounds may be used in methods of preventing and/or treating clotting disorders. 1

    摘要翻译： 式I的化合物可用于抑制丝氨酸蛋白酶，例如TF /因子VIIa，因子Xa，凝血酶和激肽释放酶，并具有改善的药代动力学性质。 这些化合物可用于预防和/或治疗凝血障碍的方法。

    Novel enantiomeric compounds for treatment of cardiac arrhythmias and methods of use
    4.
    发明申请
    Novel enantiomeric compounds for treatment of cardiac arrhythmias and methods of use 有权
    用于治疗心律失常的新型对映异构体化合物和使用方法

    公开(公告)号：US20020193428A1

    公开(公告)日：2002-12-19

    申请号：US10123573

    申请日：2002-04-15

    发明人： Pascal Druzgala ,  Peter G. Milner

    IPC分类号： A61K031/443 ,  A61K031/4025 ,  A61K031/343 ,  C07D45/02

    CPC分类号： C07D307/54 ,  C07D307/80

    摘要： The subject invention pertains to novel enantiomerically pure compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making and purifying the compounds. The enantiomerically purified compounds, and compositions of these compounds, exhibit unexpectedly distinct and advantageous characteristics, such as a markedly superior ability to reduce or inhibit ventricular premature beats, as compared to racemic mixtures of the compounds.

    摘要翻译： 本发明涉及新颖的对映异构体纯的化合物和包含该化合物的组合物，用于治疗心律失常。 本发明还涉及制备和纯化化合物的方法。 与化合物的外消旋混合物相比，对映异构体纯化的化合物和这些化合物的组合物显示出意想不到的和有利的特征，例如显着优异的降低或抑制心室过早搏动的能力。

    Iodobenzopyran-4-one derivatives having fungicidal activity
    6.
    发明申请
    Iodobenzopyran-4-one derivatives having fungicidal activity 审中-公开
    具有杀真菌活性的碘苯并吡喃-4-酮衍生物

    公开(公告)号：US20040192672A1

    公开(公告)日：2004-09-30

    申请号：US10485337

    申请日：2004-01-30

    发明人： Thomas Wegmann ,  Nathalie Huser ,  Rainer Karl Preuss ,  Joseph Perez

    IPC分类号： A61K031/55 ,  A61K031/443 ,  A61K031/4025 ,  C07D45/02

    CPC分类号： C07D311/22 ,  C07D311/56

    摘要： The present invention relates to iodobenzopyran-4-one derivativespossessing fungicidal properties against phytopathogenic organisms, amethod for preparing some of these derivatives. their use for protecting plants, and fungicidal compositions comprising such derivatives incombination with one or more other lungicidal compounds.

    摘要翻译： 本发明涉及具有抗植物病原生物的杀真菌性的碘代苯并吡喃-4-酮衍生物，制备这些衍生物的一些方法。 其用于保护植物的用途，以及包含这样的衍生物的杀真菌组合物与一种或多种其它杀辣化合物的混合。

    Cyclopropyl and cyclobutyl epothilone analogs
    7.
    发明申请
    Cyclopropyl and cyclobutyl epothilone analogs 失效
    环丙基和环丁基埃博霉素类似物

    公开(公告)号：US20040039026A1

    公开(公告)日：2004-02-26

    申请号：US10227073

    申请日：2002-08-23

    申请人： The Scripps Research Institute

    发明人： Kyriacos C. Nicoloou ,  Kenji Namoto ,  Andreas Ritzen ,  Mitsuru Shoji ,  Trond Ulven ,  Karl-Heinz Altmann

    IPC分类号： A61K031/443 ,  C07D45/02

    CPC分类号： C07D495/08 ,  C07D313/00 ,  C07D405/06 ,  C07D405/12 ,  C07D417/06 ,  C07D417/12

    摘要： The invention relates to cis- and trans-12, 13-cyclopropyl and 12,13-cyclobutyl epothilones of formula I to IV 1 wherein Ar is a radical represented by the following structure: 2 and the other radicals and symbols have the meanings as defined herein; to their chemical synthesis and biological evaluation; their use in the treatment of neoplastic diseases and to pharmaceutical preparations containing such compounds. The compounds described herein are potent tubulin polymerization promoters and cytotoxic agents.

    摘要翻译： 本发明涉及式I至IV的顺式 - 和反式12,13-环丙基和12,13-环丁基埃坡霉素，其中Ar是由以下结构表示的基团：其它基团和符号具有如本文所定义的含义; 对其化学合成和生物学评价; 它们在治疗肿瘤疾病中的用途以及含有这些化合物的药物制剂。 本文所述的化合物是有效的微管蛋白聚合启动子和细胞毒性剂。

    Oxy-and amino-substituted tetrahydrofuryl derivatives with antitumour activity
    8.
    发明申请
    Oxy-and amino-substituted tetrahydrofuryl derivatives with antitumour activity 失效
    具有抗肿瘤活性的羟基和氨基取代的四氢呋喃衍生物

    公开(公告)号：US20030092738A1

    公开(公告)日：2003-05-15

    申请号：US10203918

    申请日：2002-10-10

    发明人： Tatsuo Higa ,  Junichi Tanaka ,  Dolores Garcia Gravalos

    IPC分类号： A61K031/665 ,  A61K031/443 ,  A61K031/35 ,  A61K031/34 ,  C07D45/02

    CPC分类号： C07D307/22

    摘要： Compounds of formula (I) wherein the substituent groups defined by R1, R2, R3 and R4 are each independently selected of H, C(nullO)R, P(nullO)RnullRnull, S(nullO)RnullRnull, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl; wherein each of the Rnull, Rnull groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, nullO, C(nullO)H, C(nullO)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstitued aryl; wherein R1, R2, R3 could form part of a heterocyclic ring; R2 can be independently an internal salt; wherein X1, X2 and X3 on formula (I) are independently placed in any particular position of the chain and independently selected of H, OH, ORnull, SH, SRnull, SORnull, SO2Rnull, NO2, NH2, NHRnull, N(Rnull)2, NHC(O)Rnull, CN, halogen, nullO, C(nullO)H, C(nullO)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18, alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic; wherein substituent groups defined by Rnull are each independently selected from the group consisting of H, OH, ORnull, SH, SRnull, SORnull, SO2Rnull, NO2, NH2, NHRnull, N(Rnull)2, NHC(O)Rnull, CN, halogen, nullO, C(nullO)H, C(nullO)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic; wherein x can be between 6 and 20; and wherein the dotted line is one or several double bonds placed in any particular position of the side chain; are useful as antitumor compounds and include compound IK-8-73-4 of structure (a) which was isolated from a sponge Pachastrissa sp.

    摘要翻译： 式（I）化合物，其中由R 1，R 2，R 3和R 4定义的取代基各自独立地选自H，C（= O）R，P（= O）R'R“，S（= O）R 取代或未取代的C 1 -C 18烷基，取代或未取代的C 2 -C 18烯基，取代或未取代的C 2 -C 18炔基，取代或未取代的芳基; 其中R'，R“各自独立地选自H，OH，NO 2，NH 2，SH，CN，卤素，= O，C（= O）H，C（= O） 取代或未取代的C 2 -C 18烯基，取代或未取代的C 2 -C 18炔基，取代或未取代的芳基; 其中R1，R2，R3可以形成杂环的一部分; R2可以独立地是内盐; 其中式（I）中的X 1，X 2和X 3独立地位于链的任何特定位置，独立地选自H，OH，OR'，SH，SR'，SOR'，SO 2 R'，NO 2，NH 2，NHR' N（R'）2，NHC（O）R'，CN，卤素，= O，C（= O）H，C（= O）CH 3，CO 2 H，CO 2 CH 3，取代或未取代的C 1 -C 18烷基，取代或未取代的 C2-C18烯基，取代或未取代的C2-C18炔基，取代或未取代的芳基，取代或未取代的杂芳族; 其中由R'定义的取代基各自独立地选自H，OH，OR'，SH，SR'，SOR'，SO 2 R'，NO 2，NH 2，NHR'，N（R'）2，NHC O）R'，CN，卤素，= O，C（= O）H，C（= O）CH 3，CO 2 H，CO 2 CH 3，取代或未取代的C 1 -C 18

    Modulators of dopamine neurotransmission
    9.
    发明申请
    Modulators of dopamine neurotransmission 有权
    多巴胺神经传递调节剂

    公开(公告)号：US20030004169A1

    公开(公告)日：2003-01-02

    申请号：US10168019

    申请日：2002-06-18

    发明人： Clas Sonesson ,  Bengt Andersson ,  Susanna Waters ,  Nicholas Waters ,  Joakim Tedroff

    IPC分类号： C07D47/02 ,  C07D49/02 ,  A61K031/496 ,  A61K031/443 ,  A61K031/4436 ,  A61K031/4525 ,  A61K031/4535

    CPC分类号： C07D295/073 ,  C07D211/18 ,  C07D241/04 ,  C07D295/096

    摘要： New substituted 4-phenyl N-alkyl)-piperazine and 4-phenyl-N-alkyl)-piperidine compounds of Formula (1) wherein X is N, CH, or C, however X may only be C when the compound comprises a double bind at the dotted line; R1 is CF3, OSO2CF3, OSO2CH3, SOR7, SO2R7, COR7, CN, OR3, NO2, CONHR3, 3-thiophene, 2-thiophene, 3-furane, 2-furane, F, Cl, Br, or I; R2 is F, Cl, Br, I, CN, CF3, CH3, OCH3, OH, and NH2; R3 and R4 are independently H or a C1-C4 alkyl; R5 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, or null(CH2)nullR6; R6 is a C3-C6 cycloalkyl, 2-tetrahydrofurane, or 3-tetrahydrofurane; R7 is a C1-C3 alkyl, CF3, or N(R4)2, and pharmaceutically acceptable salts thereof are disclosed. Also pharmaceutical compositions comprising the above compounds and methods wherein the above compounds are used for treatment of disorders in the central nervous system are disclosed.

    摘要翻译： 新的取代的4-苯基N-烷基） - 哌嗪和4-苯基-N-烷基） - 哌啶化合物，其中X是N，CH或C，但是当化合物包含双 以虚线绑定; R1是CF3，OSO2CF3，OSO2CH3，SOR7，SO2R7，COR7，CN，OR3，NO2，CONHR3,3噻吩，2-噻吩，3-呋喃，2-呋喃，F，Cl，Br或I; R2是F，Cl，Br，I，CN，CF3，CH3，OCH3，OH和NH2; R 3和R 4独立地为H或C 1 -C 4烷基; R5是C1-C4烷基，烯丙基，CH2SCH3，CH2CH2OCH3，CH2CH2CH2F，CH2CF3,3,3,3-三氟丙基，4,4,4-三氟丁基或 - （CH2）-R6; R6是C3-C6环烷基，2-四氢呋喃或3-四氢呋喃; R7是C1-C3烷基，CF3或N（R4）2，并且其药学上可接受的盐被公开。 还公开了包含上述化合物的药物组合物和其中上述化合物用于治疗中枢神经系统疾病的方法。