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    Ethanolamine derivatives
    1.
    发明授权
    Ethanolamine derivatives 失效
    乙醇胺衍生物

    公开(公告)号：US4908386A

    公开(公告)日：1990-03-13

    申请号：US287441

    申请日：1988-12-20

    申请人： Harry Finch ,  Lawrence H. C. Lunts ,  Alan Naylor ,  Ian F. Skidmore ,  Ian B. Campbell ,  David Middlemiss ,  Charles Willbe

    发明人： Harry Finch ,  Lawrence H. C. Lunts ,  Alan Naylor ,  Ian F. Skidmore ,  Ian B. Campbell ,  David Middlemiss ,  Charles Willbe

    IPC分类号： C07D213/65 ,  C07D295/096 ,  C07C143/74 ,  A61K31/18

    CPC分类号： C07D295/096 ,  C07D213/65 ,  Y10S514/826

    摘要： The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain;Y represents a bond or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.

    摘要翻译： 本发明提供通式（I）的化合物，其中Ar表示未取代或取代的苯基; R1和R2各自表示氢原子或C1-3烷基; X表示键或C 1-7亚烷基，C 2-7亚烯基或C 2-7亚炔基链; Y表示键或C 1-6亚烷基，C 2-6亚烯基或C 2-6亚炔基链; Q表示取代的苯基或吡啶环; 以及其可用作2-肾上腺素受体的兴奋剂的生理上可接受的盐和溶剂合物，特别是用于治疗与可逆气道阻塞如哮喘和慢性支气管炎相关的疾病。

    Amine derivatives
    5.
    发明授权
    Amine derivatives 失效
    胺衍生物

    公开(公告)号：US5023378A

    公开(公告)日：1991-06-11

    申请号：US418208

    申请日：1989-10-06

    申请人： Michael D. Dowle ,  David Middlemiss ,  Harry Finch ,  Alan Naylor ,  Lawrence H. C. Lunts

    发明人： Michael D. Dowle ,  David Middlemiss ,  Harry Finch ,  Alan Naylor ,  Lawrence H. C. Lunts

    IPC分类号： C07C323/25

    CPC分类号： C07C323/25

    摘要： The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable acid addition salts, metabolically labile esters and solvates thereof in whichR.sup.1 represents a halogen atom or a methyl, ethyl, n-propyl or n-butyl group;R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each represent hydrogen atoms or one or two of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent a methy or ethyl group;X represents a C.sub.4-7 alkylene chain optionally substituted by one or more C.sub.1-4 alkyl or hydroxyl groups; or optionally containing one or two double or triple bonds; or optionally interrupted by an oxygen or sulphur atom, or by a sulphone (--SO.sub.2 --) or urea (--NHCONH--) group; andY represents a phenyl ring optionally carrying one to three substituents selected from hydroxyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, amino, carboxamido, C.sub.1-4 alkylsulphonylamino and nitro groups and halogen atoms with the proviso that when X is a C.sub.4-7 alkylene chain optionally containing one double bond then Y cannot represent phenyl or phenyl carrying one substituent which is halogen.The compounds according to the invention decrease total peripheral vascular resistance, increase cardiac output and produce a fall in blood pressure. They may be used in the treatment or prophylaxis of renal insuficiency and cardiovascular disorders such as hypertension, ischaemic heart disease or heart failure, for example acute or congestive heart failure.

    摘要翻译： 本发明提供通式（I）的化合物及其生理学上可接受的酸加成盐，其代谢不稳定的酯及其溶剂合物，其中R 1表示卤素原子或甲基，乙基，正丙基或正丁基 组; R2，R3，R4和R5各自表示氢原子，R2，R3，R4和R5中的一个或两个表示甲基或乙基; X表示任选被一个或多个C 1-4烷基或羟基取代的C 4-7亚烷基链; 或任选地含有一个或两个双键或三键; 或任选被氧或硫原子中断，或由砜（-SO 2 - ）或脲（-NHCONH-）基团中断; 并且Y表示任选地携带一至三个选自羟基，C 1-4烷基，C 1-4烷氧基，氨基，甲酰氨基，C 1-4烷基磺酰基氨基和硝基和卤素原子的取代基的苯环，条件是当X为C 4- 7亚烷基链任选地含有一个双键，则Y不能代表携带一个是卤素取代基的苯基或苯基。 根据本发明的化合物降低总周围血管阻力，增加心输出量并产生血压下降。 它们可用于治疗或预防肾功能不全和心血管疾病如高血压，缺血性心脏病或心力衰竭，例如急性或充血性心力衰竭。

    Indolizine Derivatives
    8.
    发明申请
    Indolizine Derivatives 审中-公开
    中氮衍生物

    公开(公告)号：US20090163534A1

    公开(公告)日：2009-06-25

    申请号：US11993412

    申请日：2006-06-26

    申请人： George Hynd ,  Nicholas Charles Ray ,  Harry Finch ,  David Middlemiss ,  Michael Colin Cramp ,  Paul Matthew Blaney ,  Karen Williams ,  Yan Griffon ,  Trevor Keith Harrison ,  Peter Crackett

    发明人： George Hynd ,  Nicholas Charles Ray ,  Harry Finch ,  David Middlemiss ,  Michael Colin Cramp ,  Paul Matthew Blaney ,  Karen Williams ,  Yan Griffon ,  Trevor Keith Harrison ,  Peter Crackett

    IPC分类号： A61K31/437 ,  C07D221/04 ,  A61P29/00

    CPC分类号： C07D471/04

    摘要： Compounds of formula (I) are ligands of the CRTH2 receptor and are useful in the treatment of respiratory disease: Formula (I) wherein R1, R2, R3 and R4 each independently are hydrogen, C1C6alkyl, fully or partially fluorinated C1C6alkyl, halo, —S(O)nR10, —SO2N(R10)2, —N(R10)2, —C(O)N(R10)2, —NR10C(O)R9, —CO2R10, —C(O)R9, —NO2, —CN or —OR11; wherein each R9 is independently C1C6alkyl, aryl, heteroaryl; R10 is independently hydrogen, C1C6alkyl, aryl, or heteroaryl; R11 is hydrogen, C1C6alkyl, fully or partially fluorinated C1C6alkyl or a group —SO2R9; n is 0, 1 or 2; R5 is C1C6alkyl, fully or partially fluorinated C1C6alkyl. C1C6alkenyl, C1C6alkynyl, optionally substituted aryl, or optionally substituted heteroaryl; R6 is hydrogen, C1C6alkyl or fully or partially fluorinated C1C6alkyl; R7 and R5 are independently hydrogen or C1C6alkyl, or R7 and R5 together with the atom to which they are attached form a cycloalkyl group; and X is —CHR6—, —S(O)n—, —NR6SO2— or —SO2NR6— wherein n is 0, 1 or 2.

    摘要翻译： 式（I）化合物是CRTH2受体的配体，可用于治疗呼吸系统疾病：其中R 1，R 2，R 3和R 4各自独立地为氢，C 1 -C 6烷基，完全或部分氟化的C 1 -C 6烷基，卤素， S（O）nR10，-SO2N（R10）2，-N（R10）2，-C（O）N（R10）2，-NR10C（O）R9，-CO2R10，-C（O） ，-CN或-OR11; 其中每个R 9独立地为C 1 -C 6烷基，芳基，杂芳基; R 10独立地是氢，C 1 -C 6烷基，芳基或杂芳基; R 11是氢，C 1 -C 6烷基，完全或部分氟化的C 1 -C 6烷基或基团-SO 2 R 9; n为0,1或2; R5是C1C6烷基，完全或部分氟化的C1C6烷基。 C 1 -C 6烯基，C 1 -C 6炔基，任选取代的芳基或任选取代的杂芳基; R6是氢，C1C6烷基或完全或部分氟化的C 1 -C 6烷基; R 7和R 5独立地为氢或C 1 -C 6烷基，或者R 7和R 5与它们所连接的原子一起形成环烷基; 且X为-CHR 6 - ， - S（O）n - ， - NR 6 SO 2 - 或-SO 2 NR 6 - ，其中n为0,1或2。

    CRTH2 ANTAGONISTS
    10.
    发明申请
    CRTH2 ANTAGONISTS 审中-公开

    公开(公告)号：US20100010034A1

    公开(公告)日：2010-01-14

    申请号：US12519979

    申请日：2006-12-21

    申请人： George Hynd ,  Nicholas Charles Ray ,  Harry Finch ,  David Middlemiss ,  Michael Colin Cramp ,  Paul Matthew Blaney ,  Karen Williams ,  Yann Griffon ,  Trevor Keith Harrison ,  Peter Crackett

    发明人： George Hynd ,  Nicholas Charles Ray ,  Harry Finch ,  David Middlemiss ,  Michael Colin Cramp ,  Paul Matthew Blaney ,  Karen Williams ,  Yann Griffon ,  Trevor Keith Harrison ,  Peter Crackett

    IPC分类号： A61K31/44 ,  C07D471/04 ,  A61P11/00 ,  A61P1/00

    CPC分类号： C07D471/04

    摘要： The following compounds are CRTH2 antagonists, useful in treatment of respiratory disease: [3-(2,4-dichlorophenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(2-fluoro-4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(4-methanesulfonyl-2-trifluoromethylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, (R)-2-[6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]propionic acid, [3-(4-ethanesulfonylphenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, (S)-2-[6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]propionic acid, ethanesulfonylaminobenzenesulfonyl)-6-fluoro-2-methyiindolizin-1-yl]acetic acid, [7-chloro-6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [3-(2-chloro-4-methanesulfonylphenylsulfanyl)-7-cyano-2-methylindolizin-1-yl]acetic acid, [6-cyano-3-(4-methanesulfonylbenzyl)-2-methylindolizin-1-yl]acetic acid, [3-(4-chlorobenzyl)-7-cyano-2-methylindolizin-1-yl]acetic acid, [6-cyano-3-(6-fluoroquinolin-2-yl-methyl)-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(4-methoxyphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [7-chloro-6-fluoro-3-(4-methoxyphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [3-(4-bromophenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, and [3-(4-cyclopropylsulfamoylphenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid.

    摘要翻译： 以下化合物是可用于治疗呼吸系统疾病的CRTH2拮抗剂：[3-（2,4-二氯苯基硫烷基）-6-氟-2-甲基吲哚啉-1-基]乙酸[6-氟-3-（2- （4-甲基磺酰基-2-三氟甲基苯基硫烷基）-2-甲基吲哚哩啶-1-基]乙酸，（R） - （4-氟-4-甲磺酰基苯基硫烷基）-2-甲基吲哚啉-1-基] 2- [6-氟-3-（4-甲磺酰基苯基硫基）-2-甲基吲哚啉-1-基]丙酸，[3-（4-乙磺酰基苯基硫烷基）-6-氟-2-甲基吲哚啉-1-基]乙酸， （S）-2- [6-氟-3-（4-甲磺酰基苯基硫烷基）-2-甲基吲哚啉-1-基]丙酸，乙磺酰氨基苯磺酰基）-6-氟-2-甲基吲哚啉-1-基]乙酸[7 （4-甲磺酰基苯基硫烷基）-2-甲基吲哚哩啶-1-基]乙酸[3-（2-氯-4-甲磺酰基苯基硫烷基）-7-氰基-2-甲基吲哚啉-1-基] ]乙酸[6-氰基-3-（4-甲磺酰基苄基）-2-甲基吲哚啉-1-基]乙酸[3-（4-氯苄基）-7-氰基-2-甲基吲哚 吡啶-1-基]乙酸[6-氰基-3-（6-氟喹啉-2-基 - 甲基）-2-甲基吲哚啉-1-基]乙酸[6-氟-3-（4-甲氧基苯基硫烷基 ）-2-甲基吲哚啉-1-基]乙酸[7-氯-6-氟-3-（4-甲氧基苯基硫烷基）-2-甲基吲哚啉-1-基]乙酸[3-（4-溴苯基硫基） - 6-氟-2-甲基吲哚啉-1-基]乙酸和[3-（4-环丙基氨磺酰基苯基硫烷基）-6-氟-2-甲基吲哚啉-1-基]乙酸。