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Treating cytokine-mediated diseases, e.g. asthma, allergy, eczema, rheumatoid arthritis or transplant rejection, using new or known maduraphthalazine derivatives

机译：治疗细胞因子介导的疾病，例如使用新的或已知的maduraphthalazine衍生物治疗哮喘，过敏，湿疹，类风湿性关节炎或移植排斥

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The use of maduraphthalazine derivatives (I) for treating diseases mediated by the cytokines interleukin-2 (IL-2), IL-4 and IL-5 is new. The salts of (I) and some (I) themselves are new compounds. The use of maduraphthalazine derivatives of formula (I) or their salts is claimed as drugs for the production of medicaments for treating diseases mediated by the cytokines interleukin-2 (IL-2), IL-4 and IL-5. R1 = H; 1-12 C alkyl or 2-12C mono- or polyunsaturated alkenyl (both optionally substituted (os) by one or more of OH, SH, NH2, NHT, N(T)2, NHAr, N(Ar)2, NTAr, NHCOR7, NO2, CN, COR8, CSR7, halo, OT, OAr, OCOR7, ST, SAr, SOR8, SO2R8, OSO2T, OSO2Ar, CSR7, COR9, Carb (os by one or more R10) or Het (os by one or more R10)); or Carb, Het or Spi (all os by one or more of OH, SH, NH2, NHT, N(T)2, NHAr, N(Ar)2, NTAr, NHCOR7, NO2, CN, COR8, CSR7, halo, OT, OAr, OCOR7, ST, SAr, SOR8, SO2R8, OSO2T, OSO2Ar, CSR7 or COR9); R2-R6 = H; or T, COT or COOT (all os by one or more R10); R7 = T, OT, OAr', NH2, NHT, N(T)2, NHAr', N(Ar')2, NTAr', ST, SAr', Carb or Het; R8 = H, T, NH2, NHT, N(T)2, NHAr', N(Ar')2, NTAr', NHCOR7, OH, OT, OAr', ST, SAr', Carb or Het; R9 = H, T, Carb or Het; Carb = mono-, bi- or tricyclic, saturated or mono- or polyunsaturated 3-14 membered carbocycle; Het = mono-, bi- or tricyclic, saturated or mono- or polyunsaturated 5-15 membered heterocycle, containing 1-6 heteroatoms (preferably N, O or S); Spi = carbocyclic or heterocyclic, saturated or mono- or polyunsaturated 3-10 membered spirocyclic group (where heterocyclic Spi contains 1-6 heteroatoms, preferably N, O or S); Ar = 6-14C aryl (os by one or more R10); R10 = OH, SH, NH2, NHT, N(T)2, NHAr', N(Ar')2, NTAr', NHCOR7, NO2, CN, COR8, CSR7, halo, OT, OAr', OCOR7, ST, SAr, SOR8 or SO2R8, Ar' = 6-14C aryl; T = 1-6C alkyl. Independent claims are included for: (1) new salts of (I), obtained by neutralizing bases (I) with (in)organic acids, neutralizing acids (I) with (in)organic bases or quaternizing tertiary amines (I) to give quaternary ammonium salts; and (2) (I) as new compounds, with the exception of (I; R2-R5 = H; R6 - Me; A = B' = CH2; R1 = H, Me, n-propyl, CH2CH2OH, CH2CHO or Ph) and (I; R1 = Ph; R6 = Me; A = B = CH2; and (a) R2-R5 = Me, (b) R2-R5 = COMe, (c) R2 = R3 = H and R4 = R5 = Me, (d) R2 = R3 = COMe and R4 = R5 = Me, (e) R2 = R4 = R5 = Me and R3 = H or COMe or (f) R2 = R4 = R5 = H and R3 = COMe, COOMe or CH2COOH).

机译：maduraphthalazine衍生物（I）在治疗由细胞因子白介素2（IL-2），IL-4和IL-5介导的疾病中的应用是新的。（I）和一些（I）本身的盐是新化合物。要求保护式（I）的马杜拉酞嗪衍生物或其盐的用途作为生产用于治疗由细胞因子白介素2（IL-2），IL-4和IL-5介导的疾病的药物的药物。 R1 = H; 1-12 C烷基或2-12C单或多不饱和烯基（均被OH，SH，NH2，NHT，N（T）2，NHAr，N（Ar）2，NTAr， NHCOR7，NO2，CN，COR8，CSR7，卤素，OT，OAr，OCOR7，ST，SAr，SOR8，SO2R8，OSO2T，OSO2Ar，CSR7，COR9，Carb（os含一个或多个R10）或Het（os含一个或多个更多R10））;或Carb，Het或Spi（所有os均为以下一种或多种：OH，SH，NH2，NHT，N（T）2，NHAr，N（Ar）2，NTAr，NHCOR7，NO2，CN，COR8，CSR7， OT，OAr，OCOR7，ST，SAr，SOR8，SO2R8，OSO2T，OSO2Ar，CSR7或COR9）; R2-R6 ＝ H;或T，COT或COOT（所有os由一个或多个R10表示）; R7 = T，OT，OAr'，NH2，NHT，N（T）2，NHAr'，N（Ar'）2，NTAr'，ST，SAr'，Carb或Het; R8 ＝ H，T，NH 2，NHT，N（T）2，NHAr′，N（Ar′）2，NTAr′，NHCOR 7，OH，OT，OAr′，ST，SAr′，Carb或Het; R9 = H，T，Carb或Het;碳＝单，双或三环，饱和或单或多不饱和的3-14元碳环; Het =单环，双环或三环，饱和或单不饱和或单不饱和或多不饱和的5-15元杂环，含有1-6个杂原子（最好是N，O或S）; Spi ＝碳环或杂环，饱和或单或多不饱和的3-10元螺环基团（其中杂环Spi含有1-6个杂原子，优选N，O或S）; Ar = 6-14C芳基（os等于一个或多个R10）; R10 = OH，SH，NH2，NHT，N（T）2，NHAr'，N（Ar'）2，NTAr'，NHCOR7，NO2，CN，COR8，CSR7，卤素，OT，OAr'，OCOR7，ST SAr，SOR8或SO2R8，Ar′＝ 6-14C芳基; T ＝ 1-6C烷基。包括以下方面的独立权利要求：（1）（I）的新盐，该盐是通过用（有机）酸中和碱（I），用（有机）碱中和酸（I）或使叔胺（I）季铵化获得的季铵盐; （2）（I）作为新化合物，但以下化合物除外：（I; R2-R5 = H; R6-Me; A = B'= CH2; R1 = H，Me，正丙基，CH2CH2OH，CH2CHO或Ph ）和（I; R1 = Ph; R6 = Me; A = B = CH2;和（a）R2-R5 = Me，（b）R2-R5 = COMe，（c）R2 = R3 = H和R4 = R5 = Me，（d）R2 = R3 = COMe且R4 = R5 = Me，（e）R2 = R4 = R5 = Me且R3 = H或COMe或（f）R2 = R4 = R5 = H且R3 = COMe， COOMe或CH2COOH）。

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公开/公告号DE19917505A1

专利类型
公开/公告日2000-10-19

原文格式PDF
申请/专利权人 ARZNEIMITTELWERK DRESDEN GMBH;
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申请/专利号DE1999117505
发明设计人 DRAHEIM REGINA;KRONBACH THOMAS;HEINISCH LOTHAR;ROEMER ERNST;HOEFGEN NORBERT;POPPE HILDEGARD;JUETTEN PETER;HAAS WOLFGANG;WERNER WALTER;GRAEFE UDO;
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申请日1999-04-17
分类号C07D237/30;C07D401/04;A61K31/495;C07D403/04;
国家 DE
入库时间 2022-08-22 01:42:14

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