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1.发明授权Bronchospasmolytic 1-(p-amino-phenyl)-2-amino-ethanols-(1) and salts 失效支气管解痉剂1-（对氨基 - 苯基）-2-氨基 - 乙醇 - （1）和盐
公开(公告)号：US4119710A
公开(公告)日：1978-10-10
申请号：US754981
申请日：1976-12-28
IPC分类号： C07D263/04 , C07D317/58 , A61K31/04 , A61K31/135 , A61K31/275 , A61K31/36
CPC分类号： C07D263/04 , C07D317/58
摘要： Racemic and optically active compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, fluorine, chlorine, bromine, iodine or cyano,R.sub.2 is fluorine, trifluoromethyl, nitro or cyano, andR.sub.3 is alkyl of 3 to 5 carbon atoms, hydroxy(alkyl of 3 to 5 carbon atoms), cycloalkyl of 3 to 5 carbon atoms, 1-(3,4-methylenedioxy-phenyl)-2-propyl or 1-(p-hydroxy-phenyl)-2-propyl,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as analgesics, uterospasmolytics, bronchospasmolytics and antispastics for the skeletal musculature, and especially as .beta..sub.2 -receptor mimetics and .beta..sub.1 -receptor blockers.
摘要翻译： 其中R 1为氢，氟，氯，溴，碘或氰基的外消旋和旋光活性化合物，R 2为氟，三氟甲基，硝基或氰基，R 3为3至5个碳原子的烷基，羟基（烷基 3至5个碳原子的环烷基，3至5个碳原子的环烷基，1-（3,4-亚甲二氧基 - 苯基）-2-丙基或1-（对羟基 - 苯基）-2-丙基，和非毒性 其药理学可接受的酸添加剂; 这些化合物作为其作为骨质疏松症，骨质疏松症，骨质疏松症和骨质疏松症的抗生素有用的化合物，特别适用于β2受体的MIME和β受体阻断剂。
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公开(公告)号：US4093734A
公开(公告)日：1978-06-06
申请号：US734818
申请日：1976-10-22
申请人： Gerd Kruger , Johannes Keck , Klaus Reinhold Noll , Helmut Pieper , Harald Ziegler , Helmut Ballhause , Joachim Kahling
发明人： Gerd Kruger , Johannes Keck , Klaus Reinhold Noll , Helmut Pieper , Harald Ziegler , Helmut Ballhause , Joachim Kahling
IPC分类号： C07D295/12 , A61K31/165 , A61K31/40 , A61K31/415 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P1/04 , A61P1/08 , A61P25/24 , A61P25/26 , C07C237/30 , C07D207/09 , C07D211/26 , C07D211/56 , C07D211/58 , C07D213/40 , C07D213/75 , C07D233/30 , C07D295/13 , C07D453/02 , C07D207/44
CPC分类号： C07D213/40 , C07D207/09 , C07D211/26 , C07D211/56 , C07D233/30 , C07D295/13 , C07D453/02
摘要： Compounds of the formula ##STR1## wherein (A) WHEN THE AMINO-SUBSTITUENT IS IN THE P-POSITION WITH RESPECT TO THE CARBONYL GROUP,R.sub.1 is chlorine in the o-position with respect to the carbonyl group,R.sub.2 is hydrogen, andR.sub.3 is ethylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, N-methyl-cyclohexylamino, benzylamino or 1-ethyl-pyrrolidyl-(2)-aminomethyl, or(b) when the amino-substituent is in the o--, m-- or p-position with respect to the carbonyl group,R.sub.1 is hydrogen, chlorine or bromine,R.sub.2 is trifluoromethyl, nitro or, when R.sub.4 is 1-(alkyl of 1 to 3 carbon atoms)-pyrrolidyl or 1-(alkyl of 1 to 3 carbon atoms)-piperidyl, also fluorine, chlorine, bromine or methyl,R.sub.3 is (alkyl of 1 to 5 carbon atoms)-amino, (cycloalkyl of 3 to 7 carbon atoms)-amino, benzylamino, quinuclidinyl-amino or --NH--(CH.sub.2).sub.n --R.sub.4where R.sub.4 is pyridyl, 1-(alkyl of 1 to 3 carbon atoms)-pyrrolidyl, 1-(alkyl of 1 to 3 carbon atoms)-piperidyl or, when n is 2 or 3, also imidazolonyl, pyrrolidino, piperidino or morpholino, andn is 0, 1, 2 or 3,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anxiolytics, anticonvulsives, antiemetics and antiulcerogenics.
摘要翻译： 式（A）的化合物其中（A）当氨基取代基位于与碳组相对位置时，R 1为相对于羰基的o位置的氯，R 2为氢，R 3为 是乙基氨基，环戊基氨基，环己基氨基，环庚基氨基，N-甲基 - 环己基氨基，苄基氨基或1-乙基 - 吡咯烷基 - （2） - 氨基甲基，或（B）当氨基取代基位于O-， 对于羰基，R1是氢，氯或溴，R2是三氟甲基，硝基，或当R4是1-（1至3个碳原子的烷基） - 吡咯烷基或1-（1至3个碳原子的烷基）时， - 哌啶基，氟，氯，溴或甲基，R3是（碳原子数1〜5的烷基） - 氨基，（3〜7个碳原子的环烷基） - 氨基，苄基氨基，奎宁环基 - 氨基或-NH-（CH2） n-R4，其中R4是吡啶基，1-（1至3个碳原子的烷基） - 吡咯烷基，1-（1至3个碳原子的烷基） - 哌啶基，或当n是2或3时，也是咪唑啉基，吡咯烷子基，哌啶子基 或mor pholino和N IS 0,1,2或3，以及非毒性，药理学上可接受的酸添加量; 化合物作为它们的有效的有用的ANXIOLYTICS，ANTICONVULSIVES，抗原和抗生素。
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公开(公告)号：US4073942A
公开(公告)日：1978-02-14
申请号：US635220
申请日：1975-11-25
申请人： Johannes Keck , Sigfrid Puschmann , Gerd Kruger , Klaus-Reinhold Noll , Matyas Leitold , Helmut Pieper
发明人： Johannes Keck , Sigfrid Puschmann , Gerd Kruger , Klaus-Reinhold Noll , Matyas Leitold , Helmut Pieper
IPC分类号： A61K31/135 , C07C87/29
CPC分类号： A61K31/135 , Y10S514/849 , Y10S514/925
摘要： Compounds of the formula ##STR1## wherein X is chlorine or bromine;R.sub.1 is hydrogen, chlorine or bromine;R.sub.2 is isopropyl; tert.butyl; tert.pentyl; mono-, di- or tri-hydroxy-substituted branched alkyl of 3 to 5 carbon atoms; cyclohexyl; or hydroxycyclohexyl; andR.sub.3 is alkyl of 1 to 4 carbon atoms or, when R.sub.2 is other than cyclohexyl, also hydrogen;And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as secretolytics, antitussives, anti-ulcerogenics and stimulants for the production of the surfactant or anti-atelectasis factor of the alveoli.
摘要翻译： 其中X是氯或溴的式“IMAGE”的化合物; R1是氢，氯或溴; R2是异丙基; 叔丁基 叔戊基 3至5个碳原子的单，二或三羟基取代的支链烷基; 环己基 或羟基环己基; 并且R 3是1至4个碳原子的烷基，或者当R 2不是环己基时，也是氢; 和非毒性，药理学上可接受的酸添加量; 该化合物作为其生物利用作为秘密，抗生素，抗生素和抗生素用于生产ALVEOLI的表面活性剂或抗原决定因子。
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公开(公告)号：US4113777A
公开(公告)日：1978-09-12
申请号：US812325
申请日：1977-07-01
申请人： Johannes Keck , Sigfrid Puschmann , Gerd Kruger , Klaus-Reinhold Noll , Matyas Leitold , Helmut Pieper
发明人： Johannes Keck , Sigfrid Puschmann , Gerd Kruger , Klaus-Reinhold Noll , Matyas Leitold , Helmut Pieper
IPC分类号： A61K31/135 , C07C87/28
CPC分类号： A61K31/135 , Y10S514/849 , Y10S514/925
摘要： Compounds of the formula ##STR1## wherein X and R.sub.1 are each chlorine or bromine;R.sub.2 is isopropyl; tert.butyl; tert.pentyl; mono-, di- or tri-hydroxy-substituted branched alkyl of 3 to 5 carbon atoms; cyclohexyl; or hydroxycyclohexyl; andR.sub.3 is alkyl of 1 to 4 carbon atoms or, when R.sub.2 is other than cyclohexyl, also hydrogen;And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as secretolytics, antitussives, anti-ulcerogenics and stimulants for the production of the surfactant or antiatelectasis factor of the alveoli.
摘要翻译： 其中X和R 1各自为氯或溴的式“IMAGE”的化合物; R2是异丙基; 叔丁基 叔戊基 3至5个碳原子的单，二或三羟基取代的支链烷基; 环己基 或羟基环己基; 并且R 3是1至4个碳原子的烷基，或者当R 2不是环己基时，也是氢; 和非毒性，药理学上可接受的酸添加量; 化合物作为其生物利用作为秘密，抗生素，抗生素和抗生素用于生产ALVEOLI的表面活性剂或抗原决定因子。
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5.发明授权
公开(公告)号：US4006246A
公开(公告)日：1977-02-01
申请号：US649481
申请日：1976-01-15
IPC分类号： A61K31/135 , A61K31/19 , A61K31/24
CPC分类号： A61K31/19 , A61K31/135
摘要： Pharmaceutical dosage unit compositions containing as an active ingredient a compound of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkanoyl, benzoyl or halobenzoyl,R.sub.2 is hydrogen, chlorine or bromine,R.sub.3 is carboxyl or lower carbalkoxy, andR.sub.4 and R.sub.5 are each hydrogen, alkyl of 1 to 5 carbon atoms, mono- or di-hydroxy-(alkyl of 1 to 5 carbon atoms), alkenyl or 2 to 4 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, mono- or di-hydroxy-(cycloalkyl of 5 to 7 carbon atoms) or benzyl,Or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as anti-ulcerogenics, secretolytics, antitussives, and stimulants of the production of the surfactant or antiatelectasis factor of the alveoli.
摘要翻译： 含有下式化合物作为活性成分的药物剂量单位组合物，其中R 1是氢，低级烷酰基，苯甲酰基或卤代苯甲酰基，R 2是氢，氯或溴，R 3是羧基或低级烷氧羰基，R 4和R 5各自是 氢，1至5个碳原子的烷基，一或二羟基 - （1至5个碳原子的烷基），烯基或2至4个碳原子，5至7个碳原子的环烷基，一或二羟基 - （5至7个碳原子的环烷基）或苄基，或非毒性，药理学上可接受的酸添加盐; 以及使用它们作为抗生素，秘密，抗生素和生物活性物质的抗生素或抗原决定因子的方法。
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6.发明授权Pharmaceutical compositions containing a 3-(amino-methylene)-5-phenyl-1,4-benzodiazepin-2-one and method of use 失效含有3-（氨基 - 亚甲基）-5-苯基-1,4-苯并二氮杂-2-酮的药物组合物及其使用方法
公开(公告)号：US3956492A
公开(公告)日：1976-05-11
申请号：US532069
申请日：1974-12-12
IPC分类号： A61K31/33 , A61K31/495 , A61K31/535 , A61K31/54
摘要： Pharmaceutical dosage unit compositions containing as an active ingredient a compound of the formula ##SPC1##WhereinR.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen, cycloalkyl, phenyl, --A--YwhereinA is alkyl of 1 to 5 carbon atoms or alkenyl of 1 to 5 carbon atoms, andY is furyl, dialkylamino, hydroxyl, carbalkoxy or carbamido,Or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino, hexamethyleneimino, morpholino, thiomorpholino, thiomorpholino-S-oxide or N'-alkylpiperazino,R.sub.3 is halogen, nitro or trifluoromethyl,R.sub.4 is hydrogen, halogen or trifluoromethyl, andR.sub.5 is hydrogen, alkyl, cycloalkyl-methyl, alkylamino-alkyl, dialkylamino-alkyl or trifluoromethyl-alkyl;And a method of using the same as sedatives, tranquilizers, muscle-relaxants and anticonvulsives.
摘要翻译： 含有作为活性成分的式WHEREIN R1和R2彼此相同或不同的化合物的药物剂量单位组合物各自为氢，环烷基，苯基，其中A为1至5个碳原子的烷基 或1至5个碳原子的链烯基，Y是呋喃基，二烷基氨基，羟基，烷氧羰基或氨基甲酰基，或者与其它任何其它的氮原子一起形成吡啶并吡咯烷酮，哌啶，异丙基苯胺，吗啉，噻唑啉， N-氧化物或N-烷基哌嗪基，R3是卤素，硝基或三氟甲基，R4是氢，卤素或三氟甲基，R5是氢，烷基，环烷基 - 甲基，烷基氨基 - 烷基，二烷基氨基 - 烷基或三氟甲基 - 烷基; 以及将其用作SEDATIVES，TRANQUILIZERS，MUSCLE-RELAXANTS和ANTICONVULSIVES的方法。
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公开(公告)号：US4101671A
公开(公告)日：1978-07-18
申请号：US780903
申请日：1977-03-24
IPC分类号： A61K31/135 , A61K31/19 , C07D221/24 , C07D295/135 , C07C87/28
CPC分类号： C07D295/135 , A61K31/135 , A61K31/19 , C07D221/24
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or aliphatic or aromatic carboxylic acyl,R.sub.2 is hydrogen, chlorine or bromine,R.sub.3 is fluorine, alkyl of 1 to 4 carbon atoms, trifluoromethyl, cyano, carbamoyl, carboxyl, carbalkoxy, alkoxy, acetyl, 1-hydroxyethyl or ##STR2## where R.sub.6 and R.sub.7 are each alkyl, cycloalkyl, hydroxy-cycloalkyl or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino or morpholino, andR.sub.4 and R.sub.5 are each hydrogen, alkyl of 1 to 5 carbon atoms, mono- or di-hydroxy (alkyl of 1 to 5 carbon atoms), alkenyl of 2 to 4 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, mono- or di-hydroxy (cycloalkyl of 5 to 7 carbon atoms), benzyl, morpholinocarbonylmethyl or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino, hexamethyleneimino, morpholino, N-methyl-piperazino or camphidino,Provided, however, that when R.sub.3 is carboxyl or carbalkoxy, R.sub.4 and R.sub.5 are other than hydrogen, alkyl, mono- or di-hydroxyalkyl, alkenyl, cycloalkyl, mono- or di-hydroxy-cycloalkyl or benzyl; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.
摘要翻译： 其中R 1是氢或脂族或芳族羧酰基，R 2是氢，氯或溴，R 3是氟，1-4个碳原子的烷基，三氟甲基，氰基，氨基甲酰基，羧基，烷氧基，烷氧基， 乙酰基，1-羟乙基或者其中R 6和R 7各自为烷基，环烷基，羟基 - 环烷基，或彼此连接的氮原子，与它们相连的氮原子，吡咯烷子基，哌啶子基或吗啉代，R 4和R 5各自为 氢，1至5个碳原子的烷基，一或二羟基（1至5个碳原子的烷基），2至4个碳原子的烯基，5至7个碳原子的环烷基，一或二羟基（环烷基 5至7个碳原子），苄基，吗啉代羰基甲基或彼此连接的氮原子，吡咯烷基，哌啶子基，六亚甲基亚氨基，吗啉代，N-甲基 - 哌嗪子基或樟脑酸，提供，但是当R3 是羧基或烷氧基，R4和R5不同于氢 烷基，单 - 或二 - 羟基烷基，烯基，环烷基，单 - 或二 - 羟基 - 环烷基或苄基; 和无毒的，药学上可接受的酸加成盐。 化合物及其盐可用作抗溃疡发生剂。
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公开(公告)号：USRE29628E
公开(公告)日：1978-05-09
申请号：US746954
申请日：1976-12-02
IPC分类号： A61K31/135 , A61K31/19 , C07D221/24
CPC分类号： A61K31/19 , A61K31/135 , C07D221/24
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or aliphatic or aromatic carboxylic acyl,R.sub.2 is hydrogen, chlorine or bromine,R.sub.3 is fluorine, alkyl of 1 to 4 carbon atoms, trifluoromethyl, cyano, carbamoyl, carboxyl, carbalkoxy, alkoxy, acetyl, 1-hydroxyethyl or ##STR2## where R.sub.6 and R.sub.7 are each alkyl, cycloalkyl, hydroxy-cycloalkyl or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino or morpholino, andR.sub.4 and R.sub.5 are each hydrogen, alkyl of 1 to 5 carbon atoms, mono- or di-hydroxy (alkyl of 1 to 5 carbon atoms), alkenyl of 2 to 4 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, mono- or di-hydroxy(cycloalkyl of 5 to 7 carbon atoms), benzyl, morpholinocarbonylmethyl or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino, hexamethyleneimino, morpholino, N-methyl-piperazino or camphidino, and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anti-ulcerogenics, secretolytics, .[.antitussive,.]. .Iadd.antitussives .Iaddend.and stimulants of the production of the surfactant or antiatelectasis factor of the alveoli.
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公开(公告)号：US3950393A
公开(公告)日：1976-04-13
申请号：US458099
申请日：1974-04-05
IPC分类号： C07C211/52 , A61K31/135 , A61K31/19 , C07C209/10 , C07C209/50 , C07C209/62 , C07C209/74 , C07C211/29 , C07C211/49 , C07C211/53 , C07C221/00 , C07C225/22 , C07C231/12 , C07C233/43 , C07C255/58 , C07D221/24 , C07D295/135 , C07C101/48 , C07C101/68
CPC分类号： C07D295/135 , A61K31/135 , A61K31/19 , C07D221/24 , Y10S514/849
摘要： Compounds of the formula ##SPC1##WhereinR.sub.1 is hydrogen or aliphatic or aromatic carboxylic acyl,R.sub.2 is hydrogen, chlorine or bromine,R.sub.3 is fluorine, alkyl of 1 to 4 carbon atoms, trifluoromethyl, cyano, carbamoyl, carboxyl, carbalkoxy, alkoxy, acetyl, 1-hydroxyethyl or ##EQU1## where R.sub.6 and R.sub.7 are each alkyl, cycloalkyl, hydroxy-cycloalkyl or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino or morpholino, andR.sub.4 and R.sub.5 are each hydrogen, alkyl of 1 to 5 carbon atoms, mono- or di-hydroxy (alkyl of 1 to 5 carbon atoms), alkenyl of 2 to 4 carbon atoms, cycloalkyl of 5 to 7 carbon atoms, mono- or di-hydroxy(cycloalkyl of 5 to 7 carbon atoms), benzyl, morpholinocarbonylmethyl or, together with each other and the nitrogen atom to which they are attached, pyrrolidino, piperidino, hexamethyleneimino, morpholino, N-methyl-piperazino or camphidino,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anti-ulcergenics, secretolytics, antitussive, and stimulants of the production of the surfactant or antiatelectasis factor of the alveoli.
摘要翻译： 式WHEREIN R 1的化合物是氢或脂族或芳族羧酸酰基，R 2是氢，氯或溴，R 3是氟，1至4个碳原子的烷基，三氟甲基，氰基，氨基甲酰基，羧基，烷氧基，烷氧基，乙酰基， 羟乙基或R6 -CH2-N ANGLE R7，其中R6和R7各自为烷基，环烷基，羟基 - 环烷基或彼此连接的氮原子，吡咯烷基，哌啶子基或吗啉代，R4和R5各自为 氢，1至5个碳原子的烷基，一或二羟基（1至5个碳原子的烷基），2至4个碳原子的烯基，5至7个碳原子的环烷基，一或二羟基（环烷基 5至7个碳原子），苄基，吗啉代羰基甲基或彼此连接的氮原子，吡咯烷基，哌啶子基，六亚甲基亚氨基，吗啉代，N-甲基哌嗪基或卡宾多，以及非毒性，药理学上可接受的 其添加量： 化合物作为其生物利用作为抗生素，秘密，抗生素和生物活性成分或抗生素因子的有效途径。
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10.发明授权Antiphlogistic pharmaceutical compositions containing a phenylethanolamine and methods of use 失效含有苯乙醇胺的消炎药物组合物及其使用方法
公开(公告)号：US4244967A
公开(公告)日：1981-01-13
申请号：US72553
申请日：1979-09-04
申请人： Gunther Engelhardt , Johannes Keck , Gerd Kruger , Klaus Noll , Helmut Pieper , Rainer Zimmermann
发明人： Gunther Engelhardt , Johannes Keck , Gerd Kruger , Klaus Noll , Helmut Pieper , Rainer Zimmermann
IPC分类号： A61K31/135 , A61K31/17 , A61K31/275 , A61K31/325 , A61P29/00 , A61P43/00 , A61K31/27
CPC分类号： A61K31/135 , A61K31/17 , A61K31/275 , A61K31/325
摘要： The method of using compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, fluorine, chlorine, bromine, iodine or cyano,R.sub.2 is fluorine, cyano, trifluoromethyl, nitro or alkyl of 1 to 4 carbon atoms,R.sub.3 is cycloalkyl or alkyl, each of 3 to 5 carbon atoms, andR.sub.4 is hydrogen or --CO--R.sub.5, whereR.sub.5 is alkoxy of 1 to 5 carbon atoms, alkenyloxy of 2 to 5 carbon atoms, aryloxy of 6 to 10 carbon atoms, aralkoxy of 7 to 11 carbon atoms, or amino which may be mono- or di-substituted by alkyl of 1 to 5 carbon atoms, alkenyl of 2 to 5 carbon atoms, aryl of 6 to 10 carbon atoms and/or aralkyl of 7 to 11 carbon atoms,and non-toxic, pharmacologically acceptable acid addition salts thereof as antirheumatics and antiphlogistics.
摘要翻译： 使用下式化合物的方法其中R1是氢，氟，氯，溴，碘或氰基，R2是氟，氰基，三氟甲基，硝基或1-4个碳原子的烷基，R3是环烷基或烷基， 3〜5个碳原子，R4为氢或-CO-R5，R5为1〜5个碳原子的烷氧基，2〜5个碳原子的烯氧基，6〜10个碳原子的芳氧基，7〜11个芳氧基 碳原子或可以被1至5个碳原子的烷基，2至5个碳原子的烯基，6至10个碳原子的芳基和/或7至11个碳原子的芳烷基单取代或二取代的氨基，以及 无毒，药理学上可接受的酸加成盐作为抗风湿剂和消炎药。
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