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    16,17-acetalsubstituted androstane-17.beta.-carboxylic acid esters prossessing high binding affinity to the glucocorticosteroid receptor
    2.
    发明授权
    16,17-acetalsubstituted androstane-17.beta.-carboxylic acid esters prossessing high binding affinity to the glucocorticosteroid receptor 失效
    16,17-乙缩醛取代的雄甾烷-17β-羧酸酯，其对糖皮质激素受体具有高结合亲和力

    公开(公告)号：US4950659A

    公开(公告)日：1990-08-21

    申请号：US843771

    申请日：1986-03-25

    申请人： Paul H. Andersson ,  Per T. Andersson ,  Bengt I. Axelsson ,  Bror A. Thalen ,  Jan W. Trofast

    发明人： Paul H. Andersson ,  Per T. Andersson ,  Bengt I. Axelsson ,  Bror A. Thalen ,  Jan W. Trofast

    IPC分类号： A61K31/58 ,  A61P5/38 ,  A61P29/00 ,  C07F3/00 ,  C07J1/00 ,  C07J5/00 ,  C07J71/00

    CPC分类号： C07J71/0031

    摘要： The invention refers to compounds having anti-inflamatory activity characterized by the formula ##STR1## or a stereoisomeric component thereof, in which formula the 1,2-position is saturated or is a double bondX.sub.1 is selected from hydrogen, fluorine, chlorine and bromineX.sub.2 is selected from hydrogen, fluorine, chlorine and bromineR.sub.1 is selected from hydrogen or a straight or branched hydrocarbon chain having 1-4 carbon atomsR.sub.2 is selected from hydrogen or straight and branched hydrocarbon chains having 1-10 carbon atoms andR.sub.3 is selected from ##STR2## is O or S R.sub.4 is selected from hydrogen, straight or branched hydrocarbon chains having 1-10 carbon atoms or from phenylR.sub.5 is selected from hydrogen or methyl andR.sub.6 is selected from hydrogen, straight or branched, saturated or unsaturated hydrocarbon chains having 1-10 carbon atoms, an alkyl group substituted by at least one halogen atom, a heterocyclic ring system containing 3-10 atoms in the ring system, ##STR3## (m=0,1,2; n=2,3,4,5,6), phenyl or benzyl groups which are unsubstituted or substituted by one or more alkyl, nitro, carboxy, alkoxy, halogen, cyano, carbalkoxy or trifluoromethyl group(s),provided that when R.sub.2 is hydrogen R.sub.1 is methyl.The invention also refers to a process and intermediates for the prearation of these compunds, a pharmaceutical preparation containing one of the compunds and a method for the treatment of inflammatory conditions.

    摘要翻译： 本发明涉及具有以式I表示的抗炎活性或其立体异构体组分的化合物，其中1,2-位饱和或双键X1选自氢，氟，氯和 溴X 2选自氢，氟，氯和溴R1选自氢或具有1-4个碳原子的直链或支链烃链R2选自氢或具有1-10个碳原子的直链和支链烃链，并且R 3是 选自是O或S R4选自具有1-10个碳原子的氢，直链或支链烃链或者从苯基R5选自氢或甲基，R6选自氢，直链或支链，饱和或不饱和的 具有1-10个碳原子的烃链，被至少一个卤素原子取代的烷基，在环状体系中含有3-10个原子的杂环体系，＆lt; IMAGE＆gt;（m = 0,1,2; n = 3,4,5， 6），未被取代或被一个或多个烷基，硝基，羧基，烷氧基，卤素，氰基，烷氧基或三氟甲基取代的苯基或苄基，条件是当R 2为氢时，R 1为甲基。 本发明还涉及这些化合物的制备方法和中间体，含有一种化合物的药物制剂和治疗炎性病症的方法。

    Novel androstane-17.beta.-carboxylic acid esters
    4.
    发明授权
    Novel androstane-17.beta.-carboxylic acid esters 失效
    新型雄甾烷-17β-羧酸酯

    公开(公告)号：US4804656A

    公开(公告)日：1989-02-14

    申请号：US847933

    申请日：1986-04-03

    申请人： Paul H. Andersson ,  Per T. Andersson ,  Bengt I. Axelsson ,  Bror A. Thalen ,  Jan W. Trofast

    发明人： Paul H. Andersson ,  Per T. Andersson ,  Bengt I. Axelsson ,  Bror A. Thalen ,  Jan W. Trofast

    IPC分类号： A61K31/56 ,  A61P29/00 ,  C07J3/00 ,  C07J31/00 ,  C07J41/00 ,  C07J1/00

    CPC分类号： C07J41/0038 ,  C07J3/005 ,  C07J31/006

    摘要： The invention refers to compounds having anti-inflammatory activity characterized by the formula ##STR1## or a stereoisomeric component thereof, in which formula X.sub.1 represents a hydrogen, chlorine, bromine or fluorine atom;X.sub.2 represents a hydrogen, chlorine, bromine or fluorine atom;R.sub.1 represents a .beta.-hydroxy group, a .beta.-chlorine atom or an oxo group;R.sub.2 represents a hydrogen atom, a methylene group or an .alpha.- or .beta.-methyl group;R.sub.3 represents a hydrogen atom or an acyl group of 1 through 8 carbon atoms;R.sub.4 represents a hydrogen atom, a (C.sub.1 -C.sub.5) alkyl group or a phenyl group;R.sub.5 represents a hydrogen atom, a (C.sub.1 -C.sub.5) alkyl group or a phenyl group;Y represents either CR.sub.7 R.sub.8, O, S or NR.sub.9, where R.sub.7, R.sub.8 and R.sub.9 are selected from hydrogen or from straight or branched hydrocarbon chains having 1-8 carbon atoms or from a phenyl group.R.sub.6 represents a hydrogen; a methyl group; a phenyl or an alkenyl or cycloalkylene group optionally substituted by alkyl, nitro, carboxy, alkoxy, halogen, cyano, carbalkoxy and trifluoromethyl group(s); a (C.sub.1 -C.sub.5) alkyl group substituted by at least one halogen atom; a saturated or unsaturated carbocyclic or heterocyclic (O, S, N) ring system containing 3-10 atoms in the ring system; a C.sub.1 alkyl group substituted by either one or two alicyclic or aromatic 3,4,5 or 6-numbered ring system(s) or one, two or three straight or branched alkyl or alkenyl group(s) of 1 through 18 carbon atoms; and represents a single or double bond.The invention also refers to a process and intermediates for the preparation of these compounds, a pharmaceutical preparation containing one of the compounds and a method for the treatment of inflammatory conditions.

    摘要翻译： 本发明涉及具有以下式表示的抗炎活性的化合物或其立体异构体组分，其中式X1表示氢，氯，溴或氟原子; X2表示氢，氯，溴或氟原子; R1表示β-羟基，β-氯原子或氧代基; R2表示氢原子，亚甲基或α-或β-甲基; R3表示氢原子或1〜8个碳原子的酰基; R4表示氢原子，（C1-C5）烷基或苯基; R5表示氢原子，（C1-C5）烷基或苯基; Y表示CR7R8，O，S或NR9，其中R7，R8和R9选自氢或具有1-8个碳原子的直链或支链烃链或苯基。 R6表示氢; 甲基; 任选被烷基，硝基，羧基，烷氧基，卤素，氰基，烷氧基和三氟甲基取代的苯基或烯基或亚环烷基; 被至少一个卤素原子取代的（C1-C5）烷基; 在环系中含有3-10个原子的饱和或不饱和碳环或杂环（O，S，N）环体系; 被1或2个脂环族或芳族3,4,5或6号环系或1至2个碳原子数1或2个或3个直链或支链烷基或烯基取代的C1烷基; 并且表示单键或双键。 本发明还涉及制备这些化合物的方法和中间体，含有一种化合物的药物制剂和治疗炎性病症的方法。