公开(公告)号：US5912238A

公开(公告)日：1999-06-15

申请号：US276276

申请日：1994-07-18

申请人： Karl Baumann ,  Gerhard Emmer

发明人： Karl Baumann ,  Gerhard Emmer

IPC分类号： C07D498/18 ,  C07H19/01 ,  A61K31/395 ,  A61K31/695 ,  C07D489/18 ,  C07F7/18

CPC分类号： C07D498/18 ,  C07H19/01

摘要： The invention concerns the compounds of formula I ##STR1## wherein the substituents have various significances. They are prepared by several processes including epimerizing replacement, treatment with cyanogen bromide or thiophosgene, treatment with an acid having a non-nucleophilic anion, treatment with dimethylsulfoxide and acetic anhydride, acylation, treatment with an oxalyl derivative and ammonia, methylation, oxidation, deprotection and protection. They possess interesting pharmacological activity as antiinflammatory, immunosuppressant, antiproliferative and chemotherapeutic drug resistance reversing agents.

摘要翻译： 本发明涉及式I化合物，其中取代基具有各种含义。 它们通过几种方法制备，包括差向异构取代，用溴化氰或硫光气处理，用具有非亲核阴离子的酸处理，用二甲基亚砜和乙酸酐处理，酰化，用草酰基衍生物和氨处理，甲基化，氧化，脱保护 和保护。 它们具有有趣的药理活性，作为抗炎，免疫抑制剂，抗增殖药和化疗药物耐药逆转剂。

公开(公告)号：US5352671A

公开(公告)日：1994-10-04

申请号：US697864

申请日：1991-05-09

申请人： Karl Baumann ,  Gerhart Emmer

发明人： Karl Baumann ,  Gerhart Emmer

IPC分类号： C07D498/18 ,  C07H19/01 ,  A61K31/695 ,  A61K31/395 ,  C07D498/16

CPC分类号： C07D498/18 ,  C07H19/01

摘要： The invention concerns the compounds of formula I ##STR1## wherein the substituents have various significances. They are prepared by several processes including epimerizing replacement, treatment with cyanogen bromide or thiophosgene, treatment with an acid having a non-nucleophilic anion, treatment with dimethylsulfoxide and acetic anhydride, acylation, treatment with an oxalyl derivative and ammonia, methylation, oxidation, deprotection and protection.They possess interesting pharmacological activity as antiinflammatory, immunosuppressant, antiproliferative and chemotherapeutic drug resistance reversing agents.

摘要翻译： 本发明涉及式Ⅰ化合物，其中取代基具有各种含义。 它们通过几种方法制备，包括差向异构取代，用溴化氰或硫光气处理，用具有非亲核阴离子的酸处理，用二甲基亚砜和乙酸酐处理，酰化，用草酰基衍生物和氨处理，甲基化，氧化，脱保护 和保护。 它们具有有趣的药理活性，作为抗炎，免疫抑制剂，抗增殖药和化疗药物耐药逆转剂。