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    SUBSTITUTED 2(5H)FURANONE, 2(5H)THIOPHENONE AND 2(5H)PYRROLONE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS ENDOTHELIN ANTAGONISTS
    7.
    发明申请
    SUBSTITUTED 2(5H)FURANONE, 2(5H)THIOPHENONE AND 2(5H)PYRROLONE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS ENDOTHELIN ANTAGONISTS 审中-公开
    取代2（5H）呋喃酮，2（5H）噻吩酮和2（5H）吡咯烷酮衍生物，其制备及其用作内皮素拮抗剂

    公开(公告)号：WO1995005376A1

    公开(公告)日：1995-02-23

    申请号：PCT/US1994009091

    申请日：1994-08-09

    申请人： WARNER-LAMBERT COMPANY

    发明人： WARNER-LAMBERT COMPANY ,  BERRYMAN, Kent, Alan ,  DOHERTY, Annette, Marian ,  EDMUNDS, Jeremy, John ,  PATT, William, Chester ,  PLUMMER, Mark, Stephen ,  REPINE, Joseph, Thomas

    IPC分类号： C07D407/04

    CPC分类号： C07D405/04 ,  C07C45/41 ,  C07C45/71 ,  C07C45/74 ,  C07C47/11 ,  C07C47/235 ,  C07C47/575 ,  C07C49/813 ,  C07C49/84 ,  C07C59/90 ,  C07D307/60 ,  C07D405/06 ,  C07D405/14 ,  C07D407/04 ,  C07D407/06 ,  C07D407/14 ,  C07D409/04 ,  C07D409/14

    摘要： Compounds of formula (I), or a tautomeric open chain keto-acid form thereof or a pharmaceutically acceptable salt thereof wherein: R1 is alkyl substituted or unsubstituted, straight, or branched, of from 1 to 12 carbon atoms, cycloalkyl substituted or unsubstituted of from 3 to 12 carbon atoms, phenyl substituted with from 1 to 5 substituents, naphthyl unsubstituted or substituted with from 1 to 5 substituents, or heteroaryl unsubstituted or substituted with from 1 to 5 substituents; R2 is alkyl substituted or unsubstituted, straight, or branched of from 1 to 12 carbon atoms, cycloalkyl substituted or unsubstituted of from 3 to 12 carbon atoms, aryl which is unsubstituted or substituted with from 1 to 5 substituents, heteroaryl wich is unsubstituted or substituted with from 1 to 3 substituents; R3 is alkyl substituted or unsubstituted, straight, or branched, of from 1 to 12 carbon atoms, cycloalkyl substituted or unsubstituted of from 3 to 12 carbon atoms, aryl which is unsubstituted or substituted with from 1 to 5 substituents, heteroaryl which is unsubstituted or substituted with from 1 to 3 substituents; R4 is hydrogen, hydroxy, halogen, SR5, OR5 wherein R5 is alkyl or substituted alkyl of from 1 to 7 carbon atoms, NR6R7 wherein R6 and R7 are each independently hydrogen, alkyl, substituted alkyl, substituted or unsubstituted phenyl, and (CH2)nOR5 wherein n is an integer of from 1 to 3; X is oxygen, S or NR8 wherein R8 is hydrogen, alkyl or substituted alkyl with the proviso that when R1 is monosubstituted phenyl and the substituent is p-methoxy, R3 is not unsubstituted phenyl, monosubstituted phenyl, or mesityl and with the further proviso when R2 is alkyl substituted, the substituent is not oxygen at the alpha -position to the furanone ring and with the further proviso that R1 and R3 are not both alkyl or alkyl substituted in the same molecule, their use as nonpeptide antagonists of endothelin I, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, and diabetes.

    摘要翻译： 式（I）化合物或其互变异构开环酮酸形式或其药学上可接受的盐，其中：R 1为烷基取代或未取代的，直链或支链的1至12个碳原子，取代或未取代的 3至12个碳原子，被1至5个取代基取代的苯基，未取代或被1至5个取代基取代的萘基，或未取代或被1至5个取代基取代的杂芳基; R 2是具有1至12个碳原子的烷基取代或未取代的，直链或支链的，取代或未取代的3至12个碳原子的环烷基，未被取代或被1至5个取代基取代的芳基，未取代或取代的杂芳基 具有1至3个取代基; R3是具有1至12个碳原子的烷基取代或未取代的，直链或支链的，取代或未取代的3-12个碳原子的环烷基，未被取代或被1至5个取代基取代的芳基，未取代的或未被取代的杂芳基 被1至3个取代基取代; R4是氢，羟基，卤素，SR5，OR5，其中R5是1或7个碳原子的烷基或取代的烷基，NR6R7，其中R6和R7各自独立地是氢，烷基，取代的烷基，取代或未取代的苯基和（CH2） nOR5其中n是1至3的整数; X是氧，S或NR8，其中R8是氢，烷基或取代的烷基，条件是当R 1是单取代的苯基且取代基是对甲氧基时，R 3不是未取代的苯基，单取代的苯基或者均三甲基，进一步的条件是 R2是烷基取代的，取代基不是位于呋喃酮环的α-位上的氧，另外条件是R 1和R 3不在同一分子中被烷基或烷基取代，它们作为内皮素I的非肽拮抗剂用作 以及其制备方法及其药物组合物，其可用于治疗升高的内皮素水平，急性和慢性肾衰竭，高血压，心肌梗死，心肌缺血，脑血管痉挛，脑缺血，脑梗塞，肝硬化，败血性休克 ，充血性心力衰竭，内毒素性休克，蛛网膜下腔出血，心律失常，哮喘，先兆子痫，动脉粥样硬化疾病包括雷诺氏病 再狭窄，心绞痛，癌症，肺动脉高压，缺血性疾病，胃粘膜损伤，出血性休克，缺血性肠病，中风和糖尿病。

    IMPROVEMENTS IN OR RELATING TO ORGANIC COMPOUNDS
    8.
    发明申请
    IMPROVEMENTS IN OR RELATING TO ORGANIC COMPOUNDS 审中-公开
    有机化合物的改善或有关

    公开(公告)号：WO2016074698A1

    公开(公告)日：2016-05-19

    申请号：PCT/EP2014/074185

    申请日：2014-11-10

    申请人： GIVAUDAN SA

    发明人： FLACHSMANN, Felix

    IPC分类号： C07C47/238 ,  C07C47/548 ,  C11B9/00

    CPC分类号： C07C47/238 ,  C07C47/235

    摘要： A compound represented by the formula (I), R 1 is -(CHR 4 ) m -(CHR 5 ) n -(CHR 6 ) o -CHO, with F 4 , R 5 , R 6 being independently selected from H or Me, and with m, n, o being independently selected from 0 and 1; R2 is H or Me; and R 3 is a C3-C6 branched, linear or cyclic alkenyl residue. Said compounds are useful as perfume ingredients in personal care and household care products.

    摘要翻译： 由式（I）表示的化合物，R1是 - （CHR4）m-（CHR5）n-（CHR6）o-CHO，其中F4，R5，R6独立地选自H或Me，m，n， o独立地选自0和1; R2是H或Me; 并且R 3是C 3 -C 6支链，直链或环状烯基残基。 所述化合物可用作个人护理和家庭护理产品中的香料成分。