公开(公告)号：US4207316A

公开(公告)日：1980-06-10

申请号：US6693

申请日：1979-01-25

申请人： Ernst Schottle ,  Alfred Weber ,  Mario Kennecke ,  Helmut Dahl ,  Joachim-Friedrich Kapp ,  Hans Wendt ,  Klaus Annen ,  Henry Laurent ,  Rudolf Wiechert

发明人： Ernst Schottle ,  Alfred Weber ,  Mario Kennecke ,  Helmut Dahl ,  Joachim-Friedrich Kapp ,  Hans Wendt ,  Klaus Annen ,  Henry Laurent ,  Rudolf Wiechert

IPC分类号： A61K31/57 ,  A61K31/573 ,  C07J5/00 ,  C07J7/00 ,  C07J17/00 ,  C07J31/00 ,  C07J71/00 ,  A61K31/56

CPC分类号： C07J5/0053 ,  C07J17/00 ,  C07J31/006 ,  C07J5/0076 ,  C07J5/0084 ,  C07J7/0045 ,  C07J7/0085 ,  C07J71/0015 ,  Y10S435/911

摘要： Corticoids of the formula ##STR1## wherein represents a single bond or a double bond;X is hydrogen, fluorine, chlorine or methyl;Y is hydrogen and Z is hydrogen, fluorine or chlorine, orY and Z together are a carbon-to-carbon bond;V is .beta.-hydroxymethylene, .beta.-chloromethylene or carbonyl;W is methylene, ethylidene or vinylidene;Q is oxygen or sulfur;R.sub.1 is alkyl of 1-8 carbon atoms, alkyl of 2-8 carbon atoms with an oxygen atom between two of the carbon atoms or benzyl, and R.sub.2 is hydrogen or alkyl of 1-4 carbon atoms, orR.sub.1 and R.sub.2 collectively are trimethylene or tetramethylene; andR.sub.3 is hydrogen, fluorine, chlorine, hydroxy, or hydroxy esterified by a C.sub.1-16 hydrocarbon carboxylic acid have valuable pharmacological properties, e.g., anti-inflammatory activity.

摘要翻译： 其中代表单键或双键的式“IMAGE”的皮质激素; X是氢，氟，氯或甲基; Y是氢，Z是氢，氟或氯，或Y和Z一起是碳 - 碳键; V是β-羟基亚甲基，β-氯亚甲基或羰基; W是亚甲基，亚乙基或亚乙烯基; Q是氧或硫; R1是1-8个碳原子的烷基，2-8个碳原子的烷基，其中两个碳原子之间的氧原子或苄基，R2是氢或1-4个碳原子的烷基，或者R1和R2一起是三亚甲基 或四亚甲基; 并且R 3是氢，氟，氯，羟基或被C 1-6烃基羧酸羟基酯化，具有有价值的药理学性质，例如抗炎活性。

公开(公告)号：US4224320A

公开(公告)日：1980-09-23

申请号：US6692

申请日：1979-01-25

申请人： Helmut Dahl ,  Ernst Schottle ,  Reinhold Wieske ,  Alfred Weber ,  Mario Kennecke

发明人： Helmut Dahl ,  Ernst Schottle ,  Reinhold Wieske ,  Alfred Weber ,  Mario Kennecke

IPC分类号： A61K31/57 ,  A61P29/00 ,  C07J5/00 ,  C07J7/00 ,  C07J17/00 ,  A61K31/56 ,  C07J9/00

CPC分类号： C07J5/0053 ,  C07J17/00 ,  C07J5/0076 ,  C07J7/0045

摘要： Steroids of the formula ##STR1## wherein represents a single or double bond,X is hydrogen, fluorine or methyl;Y is hydrogen, hydroxy or alkanoyloxy of 1-6 carbon atoms;Z is hydrogen or methyl;V is methylene, ethylidene, hydroxymethylene or vinylidene; andR.sub.1 is alkyl of 1-6 carbon atoms or alkyl of 2-6 carbon atoms with an oxygen atom between two of the carbon atoms;R.sub.2 is hydrogen or alkyl of 1-6 carbon atoms, orR.sub.1 and R.sub.2 together form a tri- or tetramethylene group provided that Y is hydroxy or alkanoyloxy;have pharmacological activity and are useful as intermediates for preparing other pharmacologically active steroids.

摘要翻译： 式“IMAGE”的类固醇，其中表示单键或双键，X为氢，氟或甲基; Y是氢，1-6个碳原子的羟基或烷酰氧基; Z是氢或甲基; V是亚甲基，亚乙基，羟基亚甲基或亚乙烯基; R1为1-6个碳原子的烷基或2-6个碳原子的烷基，氧原子在两个碳原子之间; R2是氢或1-6个碳原子的烷基，或者R1和R2一起形成三或四亚甲基，条件是Y是羟基或烷酰氧基; 具有药理活性，可用作制备其他药理活性类固醇的中间体。