公开(公告)号：EP0387091A3

公开(公告)日：1992-05-06

申请号：EP90302544.3

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, Anna ,  Csorgei, Janos ,  Szekely, Krisztina ,  Forgacs, Lilla ,  Fekete, Gyorgy ,  Herenyi, Bulcsu ,  Holly, Sandor ,  Szunyog, Jozsef

IPC分类号： C07J5/00 ,  A61K31/57

CPC分类号： C07J5/0092 ,  C07J13/005

摘要： The invention relates to Δ¹⁴-16α,17-dihydroxypregnane derivatives of general formula (I),

wherein
A represents a hydrogen atom, or hydroxyl or trifluoroacetoxy group;
X represents a hydrogen or halogen atom with the proviso that
if A is a hydrogen atom, X is also a hydrogen atom;
R represents a hydrogen atom, a benzoyl or C₁₋₈ alkanoyl group;
and --- represents a single or double bond between the 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 valuable antiinflammatory effects and thus may be used as active ingredients in antiinflammatory pharmaceutical compositions. They may also be useful in the preparation of other therapeutically useful steroid derivatives.

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.

公开(公告)号：EP0387091A2

公开(公告)日：1990-09-12

申请号：EP90302544.3

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, Anna ,  Csorgei, Janos ,  Szekely, Krisztina ,  Forgacs, Lilla ,  Fekete, Gyorgy ,  Herenyi, Bulcsu ,  Holly, Sandor ,  Szunyog, Jozsef

IPC分类号： C07J5/00 ,  A61K31/57

CPC分类号： C07J5/0092 ,  C07J13/005

摘要： The invention relates to Δ¹⁴-16α,17-dihydroxypregnane derivatives of general formula (I),

wherein
A represents a hydrogen atom, or hydroxyl or trifluoroacetoxy group;
X represents a hydrogen or halogen atom with the proviso that
if A is a hydrogen atom, X is also a hydrogen atom;
R represents a hydrogen atom, a benzoyl or C₁₋₈ alkanoyl group;
and
--- represents a single or double bond between the 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 valuable antiinflammatory effects and thus may be used as active ingredients in antiinflammatory pharmaceutical compositions. They may also be useful in the preparation of other therapeutically useful steroid derivatives.

摘要翻译： 本发明涉及DELTA <1> <4> -16α，通式（I）的17-二羟基衍生物，其中，A darstellt氢原子，或羟基或三氟乙酰氧基; X darstellt前提做如果A是一个氢原子，X是氢原子，从而氢原子或卤原子; řdarstellt氢原子，链烷酰基，苯甲酰或C1-8; 和--- darstellt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）的化合物具有有价值的抗炎作用，因此可以用作药物组合物的抗炎活性成分。 因此，它们可能是在其他治疗上有用的甾类衍生物的制备方法是有用的。

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。