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    Tropane derivatives useful in therapy
    83.
    发明申请
    Tropane derivatives useful in therapy 有权
    托烷衍生物可用于治疗

    公开(公告)号：US20040067977A1

    公开(公告)日：2004-04-08

    申请号：US10678836

    申请日：2003-10-03

    申请人： Pfizer, Inc.

    发明人： Manoussos Perros ,  David Anthony Price ,  Blanda Luzia Christa Stammen ,  Anthony Wood

    IPC分类号： A61K031/46 ,  C07D43/02

    CPC分类号： C07D451/04 ,  A61K9/2018 ,  A61K31/4196 ,  A61K31/46 ,  A61K2300/00

    摘要： The present invention provides compounds of the formula: 1 wherein R1 is C3-6 cycloalkyl optionally substituted by one or more fluorine atoms, or C1-6 alkyl optionally substituted by one or more fluorine atoms, or C3-6 cycloalkylmethyl optionally ring-substituted by one or more fluorine atoms; and R2 is phenyl optionally substituted by one or more fluorine atoms, to pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such compounds.

    摘要翻译： 本发明提供下式的化合物：其中R 1为任选被一个或多个氟原子取代的C 3-6环烷基，或任选被一个或多个氟原子取代的C 1-6烷基，或任选被C 3-6环烷基甲基任选的环 - 被一个或多个氟原子取代; 和R 2是任选被一个或多个氟原子取代的苯基，其药学上可接受的盐和溶剂合物，以及制备用于制备含这些化合物的组合物和用途的中间体的方法。

    Benzothiazole derivatives
    84.
    发明申请
    Benzothiazole derivatives 有权
    苯并噻唑衍生物

    公开(公告)号：US20030153568A1

    公开(公告)日：2003-08-14

    申请号：US09777554

    申请日：2001-02-06

    申请人： BASF Aktiengesellschaft Ludwigshafen, Germany

    发明人： Kevin P. Cusack ,  Barbara Scott ,  Lee D. Arnold ,  Anna M. Ericsson

    IPC分类号： A61K031/53 ,  A61K031/428 ,  C07D417/02

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D277/82 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D451/04 ,  C07D451/14 ,  C07D453/02 ,  C07D487/08 ,  C07D513/04

    摘要： The present invention is directed to a compound of formula (I), 1 racemic-diastereomeric mixtures thereof, optical isomers thereof, prodrugs thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, prodrugs and isotopes, wherein the variables are defined herein. The compounds of this invention are useful as inhibitors of serine/threonine and tyrosine kinases. In particular, compounds of this invention are useful as inhibitors of tyrosine kinases that are important in hyperproliferative diseases, especially in cancer and in the process of angiogenesis.

    摘要翻译： 本发明涉及式（I）的化合物，其外消旋 - 非对映体混合物，其旋光异构体，其前体药物，其同位素或所述化合物，异构体，前药和同位素的药学上可接受的盐，其中变量在本文中定义 。 本发明的化合物可用作丝氨酸/苏氨酸和酪氨酸激酶的抑制剂。 特别地，本发明的化合物可用作酪氨酸激酶的抑制剂，其在过度增殖性疾病中尤为重要，特别是在癌症和血管发生过程中

    Cocaethylene immunogens and antibodies
    86.
    发明申请
    Cocaethylene immunogens and antibodies 审中-公开
    可可亚乙基免疫原和抗体

    公开(公告)号：US20020102659A1

    公开(公告)日：2002-08-01

    申请号：US10045971

    申请日：2002-01-09

    发明人： Jean-Michel Scherrmann ,  Philippe Pouletty ,  Herve Galons

    IPC分类号： G01N033/53 ,  C12P021/04 ,  C07D451/06 ,  C07K014/765

    CPC分类号： C07D451/04 ,  C07D451/06 ,  C07K16/16 ,  G01N33/5308 ,  G01N33/946

    摘要： The ethyl ester of derivatives of benzoyl ecgonine are provided having a linking group at the para position of the benzoyl group. The derivatives are used to bond to immunogenic polypeptides for production of antisera and monoclonal antibodies. The antisera and antibodies find use in assays, for treatment of cocaine overdose and detoxification.

    摘要翻译： 在苯甲酰基的对位提供具有苯甲酰基十氢化萘衍生物的乙酯，其具有连接基团。 衍生物用于结合免疫原性多肽以产生抗血清和单克隆抗体。 抗血清和抗体可用于测定，用于治疗可卡因过量和解毒。

    Basic derivatives of benz[e] isoindol-1-ones and pyrrolo[3,4-c] quinolin-1-ones with 5-HT3-antagonistic activity, their preparation and their therapeutic use
    87.
    发明授权
    Basic derivatives of benz[e] isoindol-1-ones and pyrrolo[3,4-c] quinolin-1-ones with 5-HT3-antagonistic activity, their preparation and their therapeutic use 失效
    苯并[e]异吲哚-1-酮和具有5-HT3拮抗活性的吡咯并[3,4-c]喹啉-1-酮的基本衍生物及其制备及其治疗用途

    公开(公告)号：US06413978B1

    公开(公告)日：2002-07-02

    申请号：US09967972

    申请日：2001-10-02

    申请人： Francesco Makovec ,  Andrea Cappelli ,  Maurizio Anzini ,  Salvatore Vomero ,  Lucio Claudio Rovati

    发明人： Francesco Makovec ,  Andrea Cappelli ,  Maurizio Anzini ,  Salvatore Vomero ,  Lucio Claudio Rovati

    IPC分类号： A61K31437

    CPC分类号： C07D451/04 ,  C07D453/02

    摘要： Novel basic derivatives of benz[e]isoindol-1-ones and pyrrolo[3,4-c]quinolin-1-ones which can be represented by the general formula (I) indicated below are described: in which X is CH or N, R is H, Cl or OR1 in which R1 is H or an alkyl group having from 1 to 3 carbon atoms, Het is the 3-endotropyl group (that is, the 8-methyl-8-azadicyclo[3.2.l]oct-3-yl group) or the 3-quinuclidyl group (that is, the 1-azadicyclo[2.2.2]oct-3-yl group); these compounds have been found to be potent and selective antagonists of the 5-HT3 serotonin-like receptor and can therefore be used, for example, as anti-emetics as well as in various pathological conditions of the central nervous system, and as antitussives.

    摘要翻译： 可以由下列通式（I）表示的苯并[e]异吲哚-1-酮和吡咯并[3,4-c]喹啉-1-酮的新型碱性衍生物被描述为：其中X是CH或N， R是H，Cl或OR1，其中R 1是H或具有1至3个碳原子的烷基，Het是3-内丙基（即8-甲基-8-氮杂双环[3.2.1] （即，1-氮杂双环[2.2.2]辛-3-基））或3-奎宁环基（即，1-氮杂双环[2.2.2]辛-3-基）。 已经发现这些化合物是5-HT3血清素样受体的有效和选择性拮抗剂，因此可以用作例如抗遗传学以及中枢神经系统的各种病理状况，以及作为镇咳药。

    Novel basic derivatives of benz[e] isoindol-1-ones and pyrrolo[3,4-c] quinolin-1ones with 5-HT3-antagonistic activity, their preparation and their therapeutic use
    89.
    发明申请
    Novel basic derivatives of benz[e] isoindol-1-ones and pyrrolo[3,4-c] quinolin-1ones with 5-HT3-antagonistic activity, their preparation and their therapeutic use 失效
    苯并[e]异吲哚-1-酮和具有5-HT3拮抗活性的吡咯并[3,4-c]喹啉酮的新型碱性衍生物及其制备及其治疗用途

    公开(公告)号：US20020042426A1

    公开(公告)日：2002-04-11

    申请号：US09967972

    申请日：2001-10-02

    申请人： ROTTA RESEARCH LABORATORIUM S.p.A.

    发明人： Francesco Makovec ,  Andrea Cappelli ,  Maurizio Anzini ,  Salvatore Vomero ,  Lucio Claudio Rovati

    IPC分类号： A61K031/4745 ,  A61K031/46 ,  C07D451/02 ,  C07D453/02

    CPC分类号： C07D451/04 ,  C07D453/02

    摘要： Novel basic derivatives of benznullenullisoindol-1-ones and pyrrolonull3,4-cnullquinolin-1-ones which can be represented by the general formula (I) indicated below are described: 1 in which X is CH or N, R is H, Cl or OR1 in which R1 is H or an alkyl group having from 1 to 3 carbon atoms, Het is the 3-endotropyl group (that is, the 8-methyl-8-azadicyclonull3.2.1nulloct-3-yl group) or the 3-quinuclidyl group (that is, the 1-azadicyclonull2.2.2nulloct-3-yl group); these compounds have been found to be potent and selective antagonists of the 5-HT3 serotonin-like receptor and can therefore be used, for example, as anti-emetics as well as in various pathological conditions of the central nervous system, and as antitussives.

    摘要翻译： 可以由下列通式（I）表示的苯并[e]异吲哚-1-酮和吡咯并[3,4-c]喹啉-1-酮的新型碱性衍生物被描述为：其中X是CH或N R是H，Cl或OR1，其中R 1是H或具有1至3个碳原子的烷基，Het是3-内丙基（即8-甲基-8-氮杂双环[3.2.1] -3-基）或3-奎宁环基（即，1-氮杂双环[2.2.2]辛-3-基））。 已经发现这些化合物是5-HT3血清素样受体的有效和选择性拮抗剂，因此可以用作例如抗遗传学以及中枢神经系统的各种病理状况，以及作为镇咳药。

    Bicyclic amine derivatives
    90.
    发明授权
    Bicyclic amine derivatives 失效
    双环胺衍生物

    公开(公告)号：US06174894B1

    公开(公告)日：2001-01-16

    申请号：US09357749

    申请日：1999-07-21

    申请人： Christopher John Urch ,  Terence Lewis ,  Raymond Leo Sunley ,  Roger Salmon ,  Christopher Richard Ayles Godfrey ,  Christopher Ian Brightwell

    发明人： Christopher John Urch ,  Terence Lewis ,  Raymond Leo Sunley ,  Roger Salmon ,  Christopher Richard Ayles Godfrey ,  Christopher Ian Brightwell

    IPC分类号： A61K31435

    CPC分类号： C07D451/02 ,  A01N43/90 ,  A01N47/16 ,  A01N47/18 ,  C07D451/04 ,  C07D451/06 ,  C07D451/14

    摘要： The present invention provides a compound of Formula (I): wherein Ar is optionally substituted phenyl wherein the substutuents, if present, are selected from halogen atoms, cyano, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkenyl, alkylthio and alkyl amino groups; R represents hydrogen or cyano or a group selected from alkyl, aryl, heteroaryl, aralkyl, heteroarylalkyl, alkenyl, aralkenyl, alkynyl, alkoxycarbonyl, alkanesulfonyl, arenesulfonyl, alkenyloxycarbonyl, aralkyloxycarbonyl, aryloxycarbonyl, heterocyclylalkyl, carbamyl, dithiocarboxyl or XR3 (where X represents oxygen or a group NR4); R3 and R4 are, independently, hydrogen, alkyl, aryl, heteroaryl, aralkyl, heteroarylalkyl, alkenyl, aralkenyl, alkynyl, heterocyclylalkyl, alkoxycarbonyl or carboxylic acyl each of which may be optionally substituted; R1 represents hydrogen, hydroxy, alkyl, alkoxy, amino, nitro, isocyanato, acylamino, hydroxyalkyl, optionally substituted heteroaryl, alkoxyalkyl, haloalkyl, halohydroxyalkyl, aralkyloxyalkyl, acyloxyalkyl, amidoximido, sulfonyloxyalkyl, aminoalkyl, alkoxycarbonylamino, acylaminoalkyl, cyanoalkyl, imino, formyl, acyl or carboxylic acid or an ester or amide thereof, or alkenyl or alkynyl either of which is optionally substituted; or an acid addition salt, quaternary ammonium salt or N-oxide derived therefrom; an insecticidal, acaricidal or nematicidal composition comprising a compound of formula (I) and a suitable carrier or diluent therefor; and a method of combating and controlling insect, acarine or nematode pests at a locus which comprises treating the pests or the locus of the pests with an effective amount of a compound of formula (I) or a composition as hereinbefore described.

    摘要翻译： 本发明提供式（I）的化合物：其中Ar是任选取代的苯基，其中如果存在这些取代基，则选自卤素原子，氰基，烷基，烯基，炔基，烷氧基，卤代烷基，卤代烯基，烷硫基和烷基氨基 ; R表示氢或氰基或选自烷基，芳基，杂芳基，芳烷基，杂芳基烷基，烯基，芳烯基，炔基，烷氧基羰基，链烷磺酰基，芳烃磺酰基，烯氧基羰基，芳烷氧基羰基，芳氧基羰基，杂环基烷基，氨基甲酰基，二硫代羧基或XR3（其中X表示氧 或NR4组）; R 3和R 4独立地是氢，烷基，芳基，杂芳基，芳烷基，杂芳基烷基，烯基，芳烯基，炔基，杂环基烷基，烷氧基羰基或羧酰基，各自可以任选被取代; R 1表示氢，羟基，烷基，烷氧基，氨基，硝基，异氰酸酯基，酰氨基，羟基烷基，任选取代的杂芳基，烷氧基烷基，卤代烷基，卤代羟烷基，芳烷氧基烷基，酰氧基烷基，酰氨基亚氨基，磺酰氧基烷基，氨基烷基，烷氧基羰基氨基，酰氨基烷基，氰基烷基，亚氨基，甲酰基， 酰基或羧酸或其酯或酰胺，或任选被取代的链烯基或炔基; 或由其衍生的酸加成盐，季铵盐或N-氧化物; 杀虫杀螨或杀线虫组合物，其包含式（I）化合物及其合适的载体或稀释剂; 以及一种防治昆虫，螨虫或线虫害虫的场所的方法，包括用有效量的式（I）化合物或上述组合物处理害虫或害虫的场所。