利索-全球专利检索

  1. Login
  2. Sign Up

Search Results

41 records (took 0.026 seconds)

    THERAPEUTIC COMPOUND FOR PAIN AND SYNTHESIS THEREOF
    1.
    发明申请
    THERAPEUTIC COMPOUND FOR PAIN AND SYNTHESIS THEREOF 审中-公开
    用于疼痛和合成的治疗化合物

    公开(公告)号：WO2017040778A1

    公开(公告)日：2017-03-09

    申请号：PCT/US2016/049893

    申请日：2016-09-01

    Applicant: JANSSEN PHARMACEUTICA NV ,  DECORTE, Bart Lieven Daniel

    Inventor： DECORTE, Bart Lieven Daniel ,  RUSSCHER, Jacob Cornelis ,  MONNEE, Menno Cornelis Franciscus

    IPC: C07D471/12 ,  C07D471/18 ,  C07D317/46 ,  C07D491/147 ,  A61K31/437 ,  A61K31/36 ,  A61K31/336

    CPC classification number: C07D471/18 ,  C07D451/00

    Abstract: The invention provides compounds of Formula XXIII: (Formula XXIII) wherein R 1 is hydrogen, alkyl, acyl, or silyl, R 2 is hydrogen, alkyl, benzyl, acyl, or ester, and R 3 is hydrogen, alkyl, an aromatic group, azacyclic, carbocycle, aryl, cycloalkyl, heterocycloalkyl, heterocycle, heteroaryl, heteroalkyl, acyl, or ester, as well as derivatives and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

    Abstract translation: 本发明提供式XXIII化合物：其中R 1是氢，烷基，酰基或甲硅烷基，（R 2是氢，烷基，苄基，酰基或酯）的式（ⅩⅩⅢ）化合物，R 3是氢，烷基，芳族基团，氮杂环， 杂环烷基，杂芳基，杂芳基，杂烷基，酰基或酯，以及衍生物和立体异构体，其药学上可接受的盐和衍生物; 以及制备和使用这些化合物的方法。 本发明包括含有这些化合物的药物组合物，以及这些化合物在治疗疾病或病症的方法中的用途。

    BICYCLIC AMINE DERIVATIVES
    5.
    发明申请
    BICYCLIC AMINE DERIVATIVES 审中-公开
    双相胺衍生物

    公开(公告)号：WO98046600A1

    公开(公告)日：1998-10-22

    申请号：PCT/GB1998/000693

    申请日：1998-03-04

    IPC: A01N43/90 ,  C07D451/00 ,  C07D451/02 ,  A01N43/34 ,  A61K31/46

    CPC classification number: C07D451/02 ,  C07D451/00

    Abstract: The invention concerns a method of combating and controlling insect, acarine or nematode pests which comprises treating said pests, or the locus of said pests, with an effective amount of a compound of formula (I), wherein A is WXC-CYZ or XC=CY; R is hydrogen, formyl 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 X'R (where X' represents oxygen or a group NR ), provided that when R is alkenyl, aralkenyl or alkynyl said group does not have an unsaturated carbon atom bonding directly to the ring nitrogen of formula (I); Ar is optionally substituted phenyl or an optionally substituted 5- or 6-membered heterocyclic ring system containing from 1 to 3 heteroatoms individually selected from nitrogen, oxygen and sulfur atoms, and at least one unsaturation (double bond) between adjacent atoms in the ring, said heterocyclic ring being optionally fused to a benzene ring, wherein the substituents, if present, are selected from halogen atoms, cyano, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkenyl, alkylthio and alkyl amino groups, any of which groups contain up to six carbon atoms; W, X, Y and Z are, independently, hydrogen, hydroxy, acyloxy, alkoxy, alkylsilyloxy, cyano or halogen; alkyl moieties of R, R and R comprise from 1 to 15 carbon atoms, and are optionally substituted with one or more substituents selected from halogen, cyano, carboxyl, carboxylic acyl, carbamyl, alkoxycarbonyl, alkoxy, alkylenedioxy, hydroxy, nitro, amino, acylamino, imidate and phosphonato groups; aryl, heteroaryl, aralkyl, heteroarylalkyl, alkenyl, aralkenyl, alkynyl, alkoxycarbonyl, alkanesulfonyl, arenesulfonyl, alkanyloxycarbonyl, aralkyloxycarbonyl, aryloxycarbonyl, heterocyclylalkyl, carbamyl, dithiocarboxyl moieties of R, R and R comprise from 1 to 15 carbon atoms, and are optionally substituted with one or more substituents selected from halogen, cyano, carboxyl, carboxylic acyl, carbamyl, alkoxycarbonyl, alkoxy, alkylenedioxy, hydroxy, nitro, haloalkyl, alkyl, amino, acylamino, imidate and phosphonato groups; or an acid addition salt, quaternary ammonium salt or N -oxide derived therefrom; or an effective amount of a composition comprising a compound of formula (I), as hereinbefore defined, and an insecticidally, acaricidally or nematocidally acceptable carrier or diluent therefor. In other aspects the invention concerns compositions comprising a compound of formula (I), certain compounds of formula (I) and processes for making said compounds.

    Abstract translation: 本发明涉及一种防治昆虫，螨虫或线虫害虫的方法，其包括用有效量的式（I）化合物处理所述害虫或所述害虫的场所，其中A是WXC-CYZ或XC = CY; R是氢，甲酰基或氰基或选自烷基，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X'R （其中X'表示氧或基团NR 4），条件是当R是烯基时，所述基团不具有与式（I）的环氮直接键合的不饱和碳原子。 Ar是任选取代的苯基或任选取代的含有1至3个选自氮，氧和硫原子的杂原子的5或6元杂环系统，以及环中相邻原子之间的至少一个不饱和键（双键） 所述杂环任选地与苯环稠合，其中取代基（如果存在的话）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， 至6个碳原子; W，X，Y和Z独立地为氢，羟基，酰氧基，烷氧基，烷基甲硅烷氧基，氰基或卤素; R 3，R 3和R 4的烷基部分含有1至15个碳原子，并且任选地被一个或多个选自卤素，氰基，羧基，羧基酰基，氨基甲酰基，烷氧基羰基，烷氧基，亚烷基二氧基， 羟基，硝基，氨基，酰氨基，亚胺基和膦酸基; 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，烷磺酰基，芳烃磺酰基，烷氧基羰基，芳烷氧基羰基，芳氧基羰基，杂环基烷基，氨基甲酰基，R 3，R 3和R 4的二硫代羧基部分包含1至15个碳 氰基，羧基，羧基酰基，氨基甲酰基，烷氧基羰基，烷氧基，亚烷基二氧基，羟基，硝基，卤代烷基，烷基，氨基，酰氨基，亚氨酸酯和膦酸酯基中的一个或多个取代基任选取代。 或由其衍生的酸加成盐，季铵盐或N，N-氧化物; 或有效量的包含如上文所定义的式（I）化合物的组合物和杀虫，杀螨剂或杀线虫可接受的载体或稀释剂。 在其它方面，本发明涉及包含式（I）化合物，某些式（I）化合物和制备所述化合物的方法的组合物。

    A METHOD OF PREPARING THE SCOPINE ESTER OF DI-(2-THIENYL)GLYCOLIC ACID, AN INTERMEDIATE IN THE SYNTHESIS OF TIOTROPIUM BROMIDE, AND ITS NEW FORM
    8.
    发明申请
    A METHOD OF PREPARING THE SCOPINE ESTER OF DI-(2-THIENYL)GLYCOLIC ACID, AN INTERMEDIATE IN THE SYNTHESIS OF TIOTROPIUM BROMIDE, AND ITS NEW FORM 审中-公开
    制备DI-（2-乙烯基）甘油酸的四水合物的方法，中间体在溴化钍的合成中的应用及其新形式

    公开(公告)号：WO2013135219A1

    公开(公告)日：2013-09-19

    申请号：PCT/CZ2013/000041

    申请日：2013-03-14

    Applicant: ZENTIVA, K.S.

    Inventor： CERNA, Igor ,  HAJICEK Josef

    IPC: C07D451/10

    CPC classification number: C07D451/10 ,  C07D451/00

    Abstract: The invention relates to a preparation method of the scopine ester of di-(2- thienyl)glycolic acid of formula I. The scopine ester of formula I is an important intermediate in the synthesis of tiotropium bromide, the substance with the chemical name (1R,2R,4S,5S,7S)-7-(2-hydroxy-2,2-di(thiophen-2-yl)acetoxy)-9,9-dimethyl-3- oxa-9-azatricyclo[3.3.1.02'4]nonan-9-ium bromide of formula II. The method consists of the following steps, reaction of scopine of formula III with derivatives of oxalic acid of formula XIII, wherein X means F, CI, Br, I, and R is X or O-terf-butyl, O-methyl, A/-pyrrolidinyl, N-morpholinyl and /V-imidazolyl, in the presence of a weak base and a catalyst in an inert organic solvent, producing the derivative of formula XIV; reaction of the derivative of formula XIV with at least 2 equivalents of 2- thienylmagnesium bromide of formula XV; and isolating the resulting scopine ester of formula I is then and crystallization from a crystallization solvent.

    Abstract translation: 本发明涉及式I的二（2-噻吩基）乙醇酸的秋水仙碱的制备方法。式I的西酞菁酯是合成噻托溴铵的重要中间体，化学名称为（1R ，2R，4S，5S，7S）-7-（2-羟基-2,2-二（噻吩-2-基）乙酰氧基）-9,9-二甲基-3-氧杂-9-氮杂三环[3.3.1.02“ 4]式Ⅱ的壬-9-溴化物。 该方法由以下步骤组成：式Ⅲ化合物与式XIII的草酸衍生物的反应，其中X表示F，Cl，Br，I和R为X或O-叔丁基，O-甲基，A N-吡咯烷基，N-吗啉基和/或N-咪唑基，在弱碱和催化剂存在下，在惰性有机溶剂中反应生成式XIV的衍生物; 式XIV的衍生物与至少2当量的式XV的2-噻吩基溴化镁的反应; 然后分离出所得到的式I的扇贝酯，然后从结晶溶剂中结晶。

Patent Agency Ranking