公开(公告)号：EP0387090A2

公开(公告)日：1990-09-12

申请号：EP90302543.5

申请日：1990-03-09

申请人： RICHTER GEDEON VEGYESZETI GYAR R.T.

发明人： Molnar, Csaba ,  Hajos, Gyorgy ,  Szporny, Laszlo ,  Toth, Jozsef ,  Kiraly, Arpad ,  Boor nee Mezei, Arma ,  Csorgei, Janos ,  Szekely, Krisztina ,  Forgacs, Lilla ,  Fekete, Gyorgy ,  Herenyi, of Bulcsu ,  Holly, Sandor ,  Szunyog, Jozef

IPC分类号： C07J71/00 ,  C07J7/00 ,  A61K31/58

CPC分类号： C07J71/0031 ,  C07J7/008

摘要： The invention relates to novel Δ¹⁴-16α,17-dihydroxy-pregnane-16,17-cyclic aldehyde acetal and -cyclic ketone ketal derivatives of general formula (I),

wherein
A stands for hydrogen or hydroxyl group;
X stands for hydrogen or halogen with the proviso that if A is hydrogen, then X also means hydrogen;
R stands for hydrogen,benzoyl or C₁ ⁻ ₈alkanoyl group;
R¹ and R², which are the same or different, stand for hydrogen or a C₁ ⁻ ₄alkyl group; or one of R¹ and R² is hydrogen and the other is phenyl group; or R¹ and R² together form a C₄ ⁻ ₅alkylene group;
--- means a single or double bond between two adjacent carbon atoms,
as well as pharmaceutical compositions containing these compounds and a process for their preparation.
The compounds of general formula (I) possess a very strong antiinflammatory effect and only week harmful side effect. Thus, they can be used as active ingredients of antiinflammatory pharmaceutical compositions being useful in the therapy.

摘要翻译： 本发明涉及新颖的DELTA通式（I）<1> <4> -16α，17二羟基孕甾-16,17-环缩醛和 - 环状缩酮衍生物 worin A表示氢 或羟基; X代表氢或卤素与做如果A是氢，则X因此指的是氢，条件; R代表氢，苯甲酰基或C1 < - > 8alkanoyl基; [R <1>和R <2>哪些是相同的或不同的，独立地为氢或C1 < - > 1-4烷基; 或R之一<1>和R <2>是氢，另一个是苯基; 或R <1>和R <2>一起形成C4 < - > 5alkylene基; ---装置和两个相邻的碳原子之间的单键或双键，以及含有合成的化合物的药物组合物的方法对于它们的制备方法。 通式（I）的化合物具有非常强的抗炎效果和只周有害的副作用。 因此，它们可以被用来作为抗炎药物组合物是在治疗有用的活性成分。

公开(公告)号：EP0387090A3

公开(公告)日：1992-05-06

申请号：EP90302543.5

申请日：1990-03-09

申请人： RICHTER GEDEON VEGYESZETI GYAR R.T.

发明人： Molnar, Csaba ,  Hajos, Gyorgy ,  Szporny, Laszlo ,  Toth, Jozsef ,  Kiraly, Arpad ,  Boor nee Mezei, Arma ,  Csorgei, Janos ,  Szekely, Krisztina ,  Forgacs, Lilla ,  Fekete, Gyorgy ,  Herenyi, of Bulcsu ,  Holly, Sandor ,  Szunyog, Jozef

IPC分类号： C07J71/00 ,  C07J7/00 ,  A61K31/58

CPC分类号： C07J71/0031 ,  C07J7/008

摘要： The invention relates to novel Δ¹⁴-16α,17-dihydroxy-pregnane-16,17-cyclic aldehyde acetal and -cyclic ketone ketal derivatives of general formula (I),

wherein
A stands for hydrogen or hydroxyl group;
X stands for hydrogen or halogen with the proviso that if A is hydrogen, then X also means hydrogen;
R stands for hydrogen,benzoyl or C₁ ⁻ ₈alkanoyl group;
R¹ and R², which are the same or different, stand for hydrogen or a C₁ ⁻ ₄alkyl group; or one of R¹ and R² is hydrogen and the other is phenyl group; or R¹ and R² together form a C₄ ⁻ ₅alkylene group; --- means a single or double bond between two adjacent carbon atoms,
as well as pharmaceutical compositions containing these compounds and a process for their preparation. The compounds of general formula (I) possess a very strong antiinflammatory effect and only week harmful side effect. Thus, they can be used as active ingredients of antiinflammatory pharmaceutical compositions being useful in the therapy.