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公开(公告)号：US5773450A
公开(公告)日：1998-06-30
申请号：US167881
申请日：1993-12-14
IPC分类号： A61K31/445 , A61K31/435 , A61K31/439 , A61K31/451 , A61K31/47 , A61K31/473 , A61K31/55 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P29/00 , A61P37/08 , C07C45/44 , C07C45/51 , C07C45/67 , C07C45/71 , C07C47/55 , C07C47/575 , C07D207/14 , C07D209/52 , C07D211/56 , C07D211/76 , C07D215/42 , C07D221/04 , C07D453/00 , C07D453/02 , C07D471/08 , C07D471/18 , C07D487/08 , C07D498/18 , C07D513/18
CPC分类号： C07D453/02 , C07C45/44 , C07C45/513 , C07C45/673 , C07C45/71 , C07C47/575 , C07D211/56
摘要： The present invention relates to novel fluoroalkoxybenzylamino derivatives of nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula ##STR1## wherein Q, X.sup.1, x.sup.2 and X.sup.3 are as defined below. These novel compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.
摘要翻译： PCT No.PCT / US92 / 03571 Sec。 371日期1993年12月14日第 102（e）日期1993年12月14日PCT提交1992年5月5日PCT公布。 出版物WO92 / 06079 日期：1992年04月16日本发明涉及含氮杂环化合物的新的氟代烷氧基苄基氨基衍生物，具体地说，涉及下式的化合物，其中Q，X1，X2和X3定义如下。 这些新型化合物可用于治疗炎性和中枢神经系统疾病以及其它疾病。
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2.发明授权Diphenylheteroalkyl derivatives, the preparation thereof and drugs and cosmetics prepared therefrom 失效二苯基杂烷基衍生物，其制备方法和由其制备的药物和化妆品
公开(公告)号：US5656619A
公开(公告)日：1997-08-12
申请号：US466131
申请日：1995-06-06
申请人： Bernd Janssen , Hans-Heiner Wuest
发明人： Bernd Janssen , Hans-Heiner Wuest
IPC分类号： A61K8/33 , A61K8/34 , A61K8/36 , A61K8/37 , A61K8/40 , A61K8/41 , A61K8/42 , A61K8/44 , A61K8/46 , A61K8/67 , A61K31/195 , A61Q19/00 , C07C37/11 , C07C39/17 , C07C43/20 , C07C43/205 , C07C43/21 , C07C43/23 , C07C45/44 , C07C47/575 , C07C51/367 , C07C59/70 , C07C65/21 , C07C65/24 , C07C65/26 , C07C69/76 , C07C69/92 , C07C205/06 , C07C205/34 , C07C205/35 , C07C205/37 , C07C211/60 , C07C217/48 , C07C217/58 , C07C217/76 , C07C217/86 , C07C223/06 , C07C229/38 , C07C229/60 , C07C233/18 , C07C233/25 , C07C233/43 , C07C233/47 , C07C233/48 , C07C233/75 , C07C235/42 , C07C255/51 , C07C255/54 , C07C259/10 , C07C309/42 , C07C317/22 , C07C317/32 , C07C317/44 , C07C323/16 , C07C323/19 , C07C323/20 , C07C323/32 , C07C323/34 , C07C323/36 , C07C323/41 , C07C323/56 , C07C323/62 , C07C327/30 , C07D263/58 , C07D311/72 , C07F9/38 , C07F9/40 , C07C257/04
CPC分类号： A61K8/46 , A61K8/33 , A61K8/34 , A61K8/36 , A61K8/37 , A61K8/40 , A61K8/41 , A61K8/411 , A61K8/42 , A61K8/445 , A61K8/671 , A61Q19/00 , C07C205/06 , C07C205/34 , C07C205/35 , C07C205/37 , C07C211/60 , C07C217/48 , C07C217/58 , C07C217/76 , C07C217/86 , C07C223/06 , C07C229/38 , C07C229/60 , C07C233/18 , C07C233/25 , C07C233/43 , C07C233/47 , C07C233/48 , C07C233/75 , C07C235/42 , C07C255/54 , C07C259/10 , C07C309/42 , C07C317/22 , C07C317/32 , C07C317/44 , C07C323/16 , C07C323/19 , C07C323/20 , C07C323/32 , C07C323/34 , C07C323/36 , C07C323/41 , C07C323/56 , C07C323/62 , C07C327/30 , C07C37/18 , C07C39/17 , C07C41/26 , C07C43/202 , C07C43/2055 , C07C43/21 , C07C43/23 , C07C45/44 , C07C47/575 , C07C51/367 , C07C65/24 , C07C65/26 , C07C69/76 , C07C69/92 , C07D263/58 , C07D311/58 , C07D311/70 , C07D311/72 , C07D317/22 , C07F9/3834 , C07F9/4021 , C07C2102/10
摘要： Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
摘要翻译： 本发明摘要：描述了其中A和R 1 -R 6具有本说明书中规定的含义的式I的（I）的二苯基杂烷基衍生物及其制备。 该物质适用于控制疾病和化妆品。
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公开(公告)号：US5245085A
公开(公告)日：1993-09-14
申请号：US962016
申请日：1992-10-15
IPC分类号： C07C33/02 , C07C43/178 , C07C43/315 , C07C45/44 , C07C45/51 , C07C45/63 , C07C45/67 , C07C47/21 , C07C47/24 , C07C47/263 , C07C47/277 , C07C49/203 , C07C49/227 , C07C49/24 , C07C49/255 , C07C49/587 , C07C69/007 , C07C69/738 , C07C255/07 , C07C255/10 , C07C255/15 , C07C255/46 , C07C309/65 , C07D309/06 , C07D309/12 , C07F7/18
CPC分类号： C07F7/1856 , C07C255/07 , C07C255/10 , C07C255/15 , C07C255/46 , C07C309/65 , C07C33/02 , C07C43/178 , C07C43/315 , C07C45/44 , C07C45/512 , C07C45/516 , C07C45/63 , C07C45/673 , C07C45/676 , C07C47/21 , C07C47/24 , C07C47/263 , C07C47/277 , C07C49/203 , C07C49/227 , C07C49/24 , C07C49/255 , C07C49/587 , C07C69/007 , C07C69/738 , C07D309/06 , C07D309/12 , C07F7/1852 , C07C2101/18
摘要： Acyclic terpene compounds useful as intermediates for producing sarcophytol A which have an anti-carcinogenic promoter activity and anti-tumor activity, which compounds are shown by the general formula (I): ##STR1##
摘要翻译： 可用作产生具有抗致癌启动子活性和抗肿瘤活性的唾液酸A的中间体的无环萜烯化合物，该化合物由通式（I）表示：
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4.发明授权Diphenylheteroalkyl derivatives, the preparation thereof and drugs and cosmetics prepared therefrom 失效二苯基杂烷基衍生物，其制备方法和由其制备的药物和化妆品
公开(公告)号：US5225601A
公开(公告)日：1993-07-06
申请号：US785829
申请日：1991-10-31
申请人： Bernd Janssen , Hans-Heiner Wuest
发明人： Bernd Janssen , Hans-Heiner Wuest
IPC分类号： A61K8/33 , A61K8/36 , A61K8/37 , A61K8/40 , A61K8/41 , A61K8/42 , A61K8/44 , A61K8/46 , A61K8/67 , A61Q19/00 , C07C39/17 , C07C43/20 , C07C43/205 , C07C43/21 , C07C43/23 , C07C45/44 , C07C47/575 , C07C59/70 , C07C65/24 , C07C65/26 , C07C69/76 , C07C69/92 , C07C205/34 , C07C205/37 , C07C211/60 , C07C217/48 , C07C217/58 , C07C217/76 , C07C217/86 , C07C223/06 , C07C229/38 , C07C229/60 , C07C233/18 , C07C233/25 , C07C233/43 , C07C233/47 , C07C233/75 , C07C255/54 , C07C259/10 , C07C309/42 , C07C317/14 , C07C317/22 , C07C317/32 , C07C317/44 , C07C323/16 , C07C323/19 , C07C323/20 , C07C323/32 , C07C323/34 , C07C323/36 , C07C323/41 , C07C323/56 , C07C323/62 , C07C327/30 , C07F9/38 , C07F9/40
CPC分类号： C07F9/3834 , A61K8/33 , A61K8/36 , A61K8/37 , A61K8/40 , A61K8/411 , A61K8/42 , A61K8/445 , A61K8/46 , A61K8/671 , A61Q19/00 , C07C205/34 , C07C205/37 , C07C211/60 , C07C217/48 , C07C217/58 , C07C217/76 , C07C217/86 , C07C223/06 , C07C229/38 , C07C229/60 , C07C233/18 , C07C233/25 , C07C233/43 , C07C233/47 , C07C233/75 , C07C255/54 , C07C259/10 , C07C309/42 , C07C317/22 , C07C317/32 , C07C317/44 , C07C323/16 , C07C323/19 , C07C323/20 , C07C323/32 , C07C323/34 , C07C323/36 , C07C323/41 , C07C323/56 , C07C323/62 , C07C327/30 , C07C39/17 , C07C43/202 , C07C43/2055 , C07C43/21 , C07C43/23 , C07C45/44 , C07C47/575 , C07C59/70 , C07C65/24 , C07C65/26 , C07C69/76 , C07C69/92 , C07F9/4021 , C07C2102/10
摘要： Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
摘要翻译： 本发明摘要：描述了其中A和R 1 -R 6具有本说明书中规定的含义的式I的（I）的二苯基杂烷基衍生物及其制备。 该物质适用于控制疾病和化妆品。
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公开(公告)号：US4950796A
公开(公告)日：1990-08-21
申请号：US365794
申请日：1989-06-14
申请人： Bernd Wolf , Hans Theobald , Norbert Goetz
发明人： Bernd Wolf , Hans Theobald , Norbert Goetz
IPC分类号： C07C29/136 , C07C25/02 , C07C25/18 , C07C25/22 , C07C25/24 , C07C27/00 , C07C29/16 , C07C33/20 , C07C33/22 , C07C33/30 , C07C33/34 , C07C33/46 , C07C33/50 , C07C35/21 , C07C35/50 , C07C45/00 , C07C45/44 , C07C47/542 , C07C47/546 , C07C47/548 , C07C47/55 , C07C67/00 , C07C255/50
CPC分类号： C07C33/34 , C07C25/02 , C07C25/18 , C07C25/22 , C07C25/24 , C07C255/50 , C07C33/20 , C07C33/30 , C07C33/46 , C07C33/50 , C07C45/44 , C07C47/542 , C07C47/546 , C07C47/548 , C07C47/55 , C07C2101/02 , C07C2101/08 , C07C2101/10 , C07C2101/14 , C07C2101/16 , C07C2101/18 , C07C2102/42
摘要： Novel benzonitriles, benzaldehydes and benzyl alcohols of the formula I ##STR1## where R.sup.1 is methyl or ethyl, R.sup.2 is alkyl, alkenyl, cycloalkyl, cycloalkenyl, bicycloalkyl, bicycloalkenyl, or C.sub.1 -C.sub.5 -alkyl-substituted cycloalkyl, cycloalkenyl, bicycloalkyl or bicycloalkenyl, X is hydrogen, chlorine or fluorine and Z is --CN, CHO or ##STR2## where R.sup.3 is hydrogen, cyano, C.sub.2 -C.sub.4 -alkynyl, C.sub.2 -C.sub.4 -alkenyl or C.sub.1 -C.sub.4 -alkyl, with the proviso that R.sup.2 is not --CH.sub.2 --CH.dbd.CH--B when B is hydrogen, alkyl or alkenyl and at the same time R.sup.1 is methyl and Z is ##STR3## and with the proviso that R.sup.2 is not methyl or ethyl when R.sup.1 is methyl and at the same time Z is ##STR4## and furthermore with the proviso that R.sup.2 is not methyl when R.sup.1 is methyl or ethyl and at the same time Z is --CN or --CHO.
摘要翻译： 式I的新型苯甲腈，苯甲醛和苄醇其中R1是甲基或乙基，R2是烷基，烯基，环烷基，环烯基，双环烷基，双环烯基或C1-C5-烷基取代的环烷基，环烯基，双环烷基或 双链烯基，X是氢，氯或氟，Z是-CN，CHO或者其中R3是氢，氰基，C2-C4-炔基，C2-C4-烯基或C1-C4-烷基，其中R2是 当B是氢，烷基或链烯基并且同时R1是甲基且Z是<！ - SIPO
- >而且当R 1是甲基时，R 2不是甲基或乙基，并且在 同时Z是 ，另外条件是当R 1是甲基或乙基且同时Z是-CN或-CHO时，R 2不是甲基。 -
6.发明授权Producing analgesia with pharmacologically active 2-hydroxy-4-(substituted) phenyl cycloalkanes derivatives 失效用药理活性的2-羟基-4-（取代的）苯基环烷烃衍生物制备镇痛药
公开(公告)号：US4831059A
公开(公告)日：1989-05-16
申请号：US159013
申请日：1988-02-23
IPC分类号： A61K31/045 , A61K31/12 , C07C37/00 , C07C37/055 , C07C39/17 , C07C39/23 , C07C39/42 , C07C45/30 , C07C45/44 , C07C45/51 , C07C45/59 , C07C45/60 , C07C45/64 , C07C45/67 , C07C45/69 , C07C47/27 , C07C47/277 , C07C47/46 , C07C47/47 , C07C49/245 , C07C49/255 , C07C49/747 , C07C49/753 , C07C49/757 , C07D209/48 , C07D303/32
CPC分类号： C07D209/48 , C07C37/002 , C07C37/003 , C07C37/055 , C07C37/0555 , C07C403/02 , C07C45/30 , C07C45/44 , C07C45/51 , C07C45/515 , C07C45/59 , C07C45/60 , C07C45/64 , C07C45/67 , C07C45/673 , C07C45/69 , C07C47/27 , C07C47/277 , C07C47/46 , C07C47/47 , C07C49/245 , C07C49/255 , C07C49/747 , C07C49/753 , C07C49/757 , C07D303/32 , C07C2101/14
摘要： Compounds having the formula ##STR1## R.sub.1 is hydrogen, benzyl or an ester moiety; Y is --CH(R.sub.2 ")CH(R.sub.2)-- or --CH(R.sub.3)CH hd 2--;R.sub.2 " is hydrogen or methyl;R.sub.2 is OH or X-substituted (C.sub.1-6)alkyl;R.sub.3 is OH, cyano or X-substituted (C.sub.1-3)alkyl;X is --OR.sub.6, --SR.sub.6, --S(O)R.sub.6, --S(O).sub.2 R.sub.6, --NR.sub.6 R.sub.7, --COOR.sub.7, --CONR.sub.7 R.sub.8 or oxo;with the proviso that when X is --NR.sub.6 R.sub.7, --COOR.sub.7 or --CONR.sub.7 R.sub.8, said group is located on the terminal carbon atom of R.sub.2 or R.sub.3 ;R.sub.6 is hydrogen, (C.sub.1-6)alkyl or acetyl;each of R.sub.7 and R.sub.8 is hydrogen or (C.sub.1-6)alkyl;s is an integer of 1 or 2;with the proviso that when R.sub.6 is acetyl, R.sub.7 is hydrogen and X is other than S(O)R.sub.6 or S(O).sub.2 R.sub.6 ;Z-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain, and their use as CNS agents, antidiarrheals and anti-emetics. Processes for their preparation and intermediates therefor are described.
摘要翻译： 具有式
的化合物，其中R1是氢，苄基或酯部分; Y是-CH（R 2“）CH（R 2） - 或-CH（R 3）CH hd 2-; R2“是氢或甲基; R2是OH或X取代的（C1-6）烷基; R3是OH，氰基或X取代（C1-3）烷基; X是-OR 6，-SR 6，-S（O）R 6，-S（O）2 R 6，-NR 6 R 7，-COOR 7，-CONR 7 R 8或氧代; 条件是当X是-NR 6 R 7，-COOR 7或-CONR 7 R 8时，所述基团位于R 2或R 3的末端碳原子上; R6是氢，（C1-6）烷基或乙酰基; R 7和R 8各自为氢或（C 1-6）烷基; s是1或2的整数; 条件是当R6为乙酰基时，R7为氢，X为S（O）R6或S（O）2R6; Z-W是可以具有作为烷基链的一部分的氧原子的烷基，苯基烷基或吡啶基烷基，它们用作CNS剂，抗腹泻剂和抗排毒剂。 描述了其制备方法及其中间体。 -
公开(公告)号：US4820719A
公开(公告)日：1989-04-11
申请号：US195355
申请日：1988-05-16
IPC分类号： A61K31/19 , A61K31/415 , C07C45/29 , C07C45/44 , C07C45/56 , C07C45/62 , C07C45/67 , C07C45/68 , C07C45/71 , C07C47/542 , C07C47/546 , C07C47/548 , C07C47/55 , C07C47/575 , C07D233/84 , C07D233/90 , C07D257/04 , C07D307/38 , A61K31/41 , C07D233/64
CPC分类号： C07D257/04 , A61K31/19 , C07C317/46 , C07C323/56 , C07C323/60 , C07C323/66 , C07C323/67 , C07C45/298 , C07C45/44 , C07C45/56 , C07C45/62 , C07C45/673 , C07C45/68 , C07C45/71 , C07C47/542 , C07C47/546 , C07C47/548 , C07C47/55 , C07C47/575 , C07D233/84 , C07D233/90 , C07D307/38 , C07B2200/07 , C07C2101/14
摘要： This invention relates to alkanoic acid compounds having phenyl and thio substituents which are useful as leukotriene antagonists and pharmaceutical compositions containing such compounds. This invention also relates to methods of treating diseases in which leukotrienes are a factor by administration of an effective amount of the above compounds or compositions.
摘要翻译： 本发明涉及具有苯基和硫取代基的链烷酸化合物，其可用作白三烯拮抗剂和含有这些化合物的药物组合物。 本发明还涉及通过施用有效量的上述化合物或组合物治疗白三烯是一个因素的疾病的方法。
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公开(公告)号：US4814352A
公开(公告)日：1989-03-21
申请号：US44604
申请日：1987-05-01
IPC分类号： C07D295/06 , A01N33/02 , A61K31/135 , A61K31/16 , A61K31/165 , A61K31/40 , A61K31/435 , A61K31/495 , A61P25/24 , A61P25/26 , C07C29/147 , C07C33/50 , C07C45/00 , C07C45/42 , C07C45/44 , C07C49/237 , C07C49/567 , C07C57/46 , C07C61/40 , C07C67/00 , C07C209/00 , C07C209/28 , C07C209/40 , C07C209/48 , C07C209/52 , C07C209/56 , C07C209/58 , C07C211/25 , C07C211/26 , C07C213/00 , C07C217/74 , C07C231/00 , C07C231/02 , C07C231/08 , C07C231/10 , C07C231/12 , C07C233/03 , C07C233/05 , C07C233/13 , C07C233/18 , C07C313/00 , C07C323/32 , C07D207/06 , C07D211/70 , C07D295/073 , C07D295/185
CPC分类号： C07D295/185 , C07C255/00 , C07C29/147 , C07C33/50 , C07C45/004 , C07C45/42 , C07C45/44 , C07C49/237 , C07C49/567 , C07C57/46 , C07C61/40 , C07D207/06 , C07D211/70 , C07D295/073 , C07C2101/04
摘要： Compounds of formula I ##STR1## in which R.sub.1 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, cycloalkylalkyl or optionally substituted phenyl; R.sub.2 is H or C.sub.1-3 alkyl; R.sub.3 and/or R.sub.4 are H, formyl, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, C.sub.3-7 cycloalkyl or R.sub.3 and R.sub.4 together with the nitrogen atom form a heterocyclic ring system; R.sub.5 and/or R.sub.6 are H, halo, CF.sub.3, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, C.sub.1-3 alkylthio or R.sub.5 and R.sub.6 together with the carbon atoms to which they are attached form a second benzene ring show therapeutic activity in the treatment of depression. Pharmaceutical compositions and processes for preparing compounds of formula I are disclosed.
摘要翻译： 式I的化合物其中R 1为C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-7环烷基，环烷基烷基或任选取代的苯基; R2是H或C1-3烷基; R 3和/或R 4是H，甲酰基，C 1-3烷基，C 3-6烯基，C 3-6炔基，C 3-7环烷基或R 3和R 4与氮原子一起形成杂环体系; R 5和/或R 6是H，卤素，CF 3，C 1-3烷基，C 1-3烷氧基，C 1-3烷硫基或R 5和R 6与它们所连接的碳原子一起形成第二苯环， 治疗抑郁症。 公开了制备式I化合物的药物组合物和方法。
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公开(公告)号：US4767790A
公开(公告)日：1988-08-30
申请号：US725129
申请日：1985-04-19
IPC分类号： C07D295/06 , A01N33/02 , A61K31/135 , A61K31/16 , A61K31/165 , A61K31/40 , A61K31/435 , A61K31/495 , A61P25/24 , A61P25/26 , C07C29/147 , C07C33/50 , C07C45/00 , C07C45/42 , C07C45/44 , C07C49/237 , C07C49/567 , C07C57/46 , C07C61/40 , C07C67/00 , C07C209/00 , C07C209/28 , C07C209/40 , C07C209/48 , C07C209/52 , C07C209/56 , C07C209/58 , C07C211/25 , C07C211/26 , C07C213/00 , C07C217/74 , C07C231/00 , C07C231/02 , C07C231/08 , C07C231/10 , C07C231/12 , C07C233/03 , C07C233/05 , C07C233/13 , C07C233/18 , C07C313/00 , C07C323/32 , C07D207/06 , C07D211/70 , C07D295/073 , C07D295/185 , C07C87/50
CPC分类号： C07D295/185 , C07C255/00 , C07C29/147 , C07C33/50 , C07C45/004 , C07C45/42 , C07C45/44 , C07C49/237 , C07C49/567 , C07C57/46 , C07C61/40 , C07D207/06 , C07D211/70 , C07D295/073 , C07C2101/04
摘要： Compounds of formula I ##STR1## in which R.sub.1 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl, cycloalkylalkyl or optionally substituted phenyl; R.sub.2 is H or C.sub.1-3 alkyl; R.sub.3 and/or R.sub.4 are H, formyl, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, C.sub.3-7 cycloalkyl or R.sub.3 and R.sub.4 together with the nitrogen atom form a heterocyclic ring system; R.sub.5 and/or R.sub.6 are H, halo, CF.sub.3, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, C.sub.1-3 alkylthio or R.sub.5 and R.sub.6 together with the carbon atoms to which they are attached form a second benzene ring show therapeutic acitivity in the treatment of depression. Pharmaceutical compositions and processes for preparing compounds of formula I are disclosed.
摘要翻译： 式I的化合物其中R 1为C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-7环烷基，环烷基烷基或任选取代的苯基; R2是H或C1-3烷基; R 3和/或R 4是H，甲酰基，C 1-3烷基，C 3-6烯基，C 3-6炔基，C 3-7环烷基或R 3和R 4与氮原子一起形成杂环体系; R 5和/或R 6是H，卤素，CF 3，C 1-3烷基，C 1-3烷氧基，C 1-3烷硫基或R 5和R 6与它们所连接的碳原子一起形成第二苯环，表明在 治疗抑郁症。 公开了用于制备式I化合物的药物组合物和方法。
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公开(公告)号：US4730005A
公开(公告)日：1988-03-08
申请号：US864562
申请日：1986-05-16
IPC分类号： A61K31/19 , A61K31/38 , C07C45/29 , C07C45/44 , C07C45/56 , C07C45/62 , C07C45/67 , C07C45/68 , C07C45/71 , C07C45/72 , C07C47/542 , C07C47/546 , C07C47/548 , C07C47/55 , C07C47/575 , C07C49/86 , C07D333/18 , C07D333/36 , C07D333/32 , C07D333/24
CPC分类号： C07D333/18 , A61K31/19 , C07C317/00 , C07C321/00 , C07C45/298 , C07C45/44 , C07C45/56 , C07C45/62 , C07C45/673 , C07C45/68 , C07C45/71 , C07C45/72 , C07C47/542 , C07C47/546 , C07C47/548 , C07C47/55 , C07C47/575 , C07C49/86
摘要： The compounds represented by the following structural formula (I) ##STR1## wherein m is 1 or 2; n is 1, 2 or 3; R' is hydrogen or methyl; R is a radical selected from the group consisting of: ##STR2## wherein R.sub.1 is C.sub.8 to C.sub.13 alkyl, C.sub.7 to C.sub.12 alkoxy, C.sub.7 to C.sub.12 thioalkyl, C.sub.10 to C.sub.12 1-alkynyl, 11-dodecynyl, 1-trans-dodecenyl, 5-(4-acetyl-3-hydroxy-2-propylphenoxypentoxy, 2(Z), 5(Z)-undecadienyloxy, phenyl-C.sub.4 to C.sub.10 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenylthio-C.sub.3 to C.sub.9 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenyl-CH.dbd.CH--(CH.sub.2).sub.2-8, phenyl-C.sub.3 to C.sub.9 alkoxy, trifluoromethyl-C.sub.7 to C.sub.12 alkyl, cyclohexyl- C.sub.4 to C.sub.10 alkyl or ##STR3## wherein each q is 0, 1, 2 or 3 but the sum of both q's does not exceed 3, and R.sub.2 is hydrogen, bromo, chloro, methyl, trifluoromethyl, hydroxy, methoxy or nitro; or R.sub.1 is hydrogen and R.sub.2 is C.sub.8 to C.sub.13 alkyl, C.sub.7 to C.sub.12 alkoxy, C.sub.7 to C.sub.12 thioalkyl, C.sub.10 to C.sub.12 1-alkynyl, 11-dodecynyl, 1-trans-dodecenyl, 5-(4-acetyl-3-hydroxy-2-propylphenoxy(pentoxy, 2(Z), 5(Z)-undecadienyloxy, phenyl-C.sub.4 to C.sub.10 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenylthio-C.sub.3 to C.sub.9 alkyl with the phenyl optionally mono substituted with bromo, chloro, trifluoromethyl, methoxy, methylthio or trifluoromethylthio, phenyl-CH.dbd.CH--(CH.sub.2).sub.2-8, phenyl-C.sub.3 to C.sub.9 alkoxy, trifluoromethyl-C.sub.7 to C.sub.12 alkyl, cyclohexyl-C.sub.4 to C.sub.10 alkyl or ##STR4## wherein each q is 0, 1, 2 or 3 but the sum of both q's does not exceed 3, and p is 0 or 1, with the proviso that R is not a thiophene radical and any of R.sub.1 and R.sub.2 above are not thioalkyl or phenylthioalkyl when p is 1; and pharmaceutically acceptable salts thereof have been found to be leukotriene antagonists and useful in the treatment of diseases in which leukotrienes are a factor, such as asthma.
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