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    Compounds of the pregnane series with an oxygen function in the 19-position, processes for their manufacture and pharmaceutical preparations containing these compounds
    2.
    发明授权
    Compounds of the pregnane series with an oxygen function in the 19-position, processes for their manufacture and pharmaceutical preparations containing these compounds 失效
    在19位具有氧功能的孕烷系列化合物，其制备方法和含有这些化合物的药物制剂

    公开(公告)号：US4309423A

    公开(公告)日：1982-01-05

    申请号：US119702

    申请日：1980-02-08

    申请人： Michel Biollaz

    发明人： Michel Biollaz

    IPC分类号： A61K31/57 ,  A61P5/38 ,  C07J5/00 ,  C07J31/00 ,  C07J33/00 ,  C07J41/00 ,  A61K31/56

    CPC分类号： C07J31/003 ,  C07J31/006 ,  C07J33/007 ,  C07J41/0094 ,  C07J5/0015

    摘要： 19-Oxygenated steroid compounds of the pregnane series of the formula I ##STR1## in which R.sup.1 represents a hydrogen atom, andR.sup.2 represents an .alpha.-oriented lower alkanoylthio group, orR.sup.1 and R.sup.2 together represent a carbon-carbon bond or an .alpha.-or .beta.-oriented methylene radical,R.sup.3 represents a free hydroxymethyl group or a hydroxymethyl group etherified by a lower alkyl or esterified by a lower alkanoyl; or represents a formyl group, a carboxyl group or a lower alkoxycarbonyl group, andR.sup.4 represents a hydrogen atom or the acyl radical Ac of a carboxylic acid,and corresponding 1,2-dehydro derivatives have valuable aldosterone-antagonizing properties with a minimum effect on sexual functions. As the compounds reduce the excessive sodium retention and potassium excretion induced by aldosterone, they are especially useful as the active ingredient in pharmaceutical preparations for alleviating diseases involving hyperaldosteronismus in man and other warm-blooded animals.

    摘要翻译： 19-式I的孕烷系列的氧合类固醇化合物，其中R1代表氢原子，R2代表α-取代的低级烷酰硫基，或者R1和R2一起代表碳 - 碳键或 α或β取向的亚甲基，R 3表示游离羟甲基或被低级烷基醚化或被低级烷酰基酯化的羟甲基; 或表示甲酰基，羧基或低级烷氧基羰基，R4表示氢原子或羧酸的酰基Ac，相应的1,2-脱氢衍生物具有有价值的醛固酮拮抗特性，对 性功能。 由于化合物减少醛固酮诱导的过量的钠滞留和钾排泄，所以它们特别可用作用于缓解人类和其他温血动物中醛固酮增多症的疾病的药物制剂中的活性成分。

    2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives
    4.
    发明授权
    2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives 失效

    公开(公告)号：US6080743A

    公开(公告)日：2000-06-27

    申请号：US29525

    申请日：1998-02-27

    申请人： Pierre Acklin ,  Hans Allgeier ,  Yves Auberson ,  Michel Biollaz ,  Robert Moretti ,  Silvio Ofner ,  Siem Jacob Veenstra

    发明人： Pierre Acklin ,  Hans Allgeier ,  Yves Auberson ,  Michel Biollaz ,  Robert Moretti ,  Silvio Ofner ,  Siem Jacob Veenstra

    IPC分类号： A61K31/00 ,  A61K31/495 ,  A61K31/498 ,  A61K31/502 ,  A61K31/505 ,  A61K31/506 ,  A61K31/535 ,  A61K31/5355 ,  A61K31/5375 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/662 ,  A61P25/28 ,  A61P43/00 ,  C07D241/44 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12 ,  C07D491/113 ,  C07F9/6509

    CPC分类号： C07D401/06 ,  C07D241/44 ,  C07D401/12 ,  C07D417/12 ,  C07F9/650994

    摘要： 2,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), ##STR1## wherein one of the radicals R.sub.1, and R.sub.2 is a group R.sub.5 and the other is a group of formula --CH(R.sub.6)--alk--R.sub.7 (Ia), --alk--CH(R.sub.6 -R.sub.7 (Ib), --alk--N(R.sub.8)--X--R.sub.7 (Ic), --alk--N.sup.+ (R.sub.8)(R.sup.9)--X--R.sub.7 A.sup.- (Id), --alk--O--X--R.sub.7 (Ie) or --alk--S--X--R.sub.7 (If), R.sub.3, R.sub.4 and R.sub.5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R.sub.6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R.sub.7 is hydrogen; an aliphatic, cycloaliphatic or heterocycloaliphatic radical; cyano; acyl derived from carbonic acid or from a semiester or semiamide of carbonic acid, from sulfuric acid or from an aliphatic or aromatic sulfonic acid or from phosphoric acid or from a phosphonic acid ester; amino that is unsubtituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, R.sub.8 is hydrogen; an aliphatic or araliphatic radical; or acyl derived from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or R.sub.7 and R.sub.8, together with X and the nitrogen atom bonding R.sub.8 and X, form an unsubstitued or substituted mono- or di-azaxycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidised thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hxdrogenated aryl or heteroaryl radical, R.sub.9 is an aliphatic or araliphatic radical, or R.sub.7, R.sub.8 and R.sub.9 together with X and the nitrogen atom bonding R.sub.8, R.sub.9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A.sup.- being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R.sub.7 and R.sub.8 and the nitrogen atom bonding R.sub.8 and X or together with the nitrogen atom bonding R.sub.8, R.sub.9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, and the pharmaceutically acceptable salts thereof can be used in the preparation of a medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.

    Novel diuretics
    5.
    发明授权
    Novel diuretics 失效
    小说利尿剂

    公开(公告)号：US4261985A

    公开(公告)日：1981-04-14

    申请号：US94266

    申请日：1979-11-14

    申请人： Michel Biollaz

    发明人： Michel Biollaz

    IPC分类号： A61K31/57 ,  A61K31/63 ,  A61K31/635 ,  A61P5/38 ,  A61K31/56

    CPC分类号： A61K31/57 ,  A61K31/63 ,  A61K31/635 ,  Y10S514/869

    摘要： An advantageous diuretic action by excretion of water, sodium and chloride ions, with reduced excretion of potassium ions, is effected by combined administration of a 19-oxygenated steroid compound of the pregnane series of the formula ##STR1## wherein R.sub.a represents a hydrogen atom, andR.sub.b represents an .alpha.-oriented lower alkanoylthio group, orR.sub.a and R.sub.b together represent a carbon-carbon bond or an .alpha.- or .beta.-oriented methylene radical,R represents a free hydroxymethyl group or a hydroxymethyl group etherified by a lower alkyl or esterified by a lower alkanoyl; or represents a carboxyl group or a lower alkoxycarbonyl group, andR.sup.2 represents a hydrogen atom or the acyl radical Ac of a carboxylic acid,as the aldosterone-antagonising component A on the one hand, and, on the other hand, of a conventional diuretic which is unspecific in respect of electrolyte excretion, e.g. a diuretically effective derivative of benzothiadiazine, benzenesulfonamide, phenoxyacetic acid, benzofuran-2-carboxylic acid or 2,3-dihydrobenzofuran-2-carboxylic acid, as component B. The two components A and B can be administered separately or together as an appropriate composition or pharmaceutical preparation.

    摘要翻译： 通过排出水分，钠和氯离子以及钾离子排泄减少的有利的利尿作用通过组合施用式（I）的孕烷系列的19-氧化类固醇化合物来实现，其中Ra表示 氢原子，Rb表示α-取代的低级烷酰硫基，或者Ra和Rb一起代表碳 - 碳键或α或β-取向的亚甲基，R表示游离羟甲基或羟基甲基被低级 烷基或被低级烷酰基酯化; 或表示羧基或低级烷氧基羰基，R2表示氢原子或羧酸的酰基Ac，一方面作为醛固酮拮抗成分A，另一方面为常规利尿剂 其在电解质排泄方面是非特异性的，例如 作为组分B的苯并噻二嗪，苯磺酰胺，苯氧基乙酸，苯并呋喃-2-羧酸或2,3-二氢苯并呋喃-2-羧酸的利尿作用有效的衍生物。两种组分A和B可以作为适当组合物单独或一起施用 或药物制剂。

    Fluoro-steroids and processes for their manufacture
    6.
    发明授权
    Fluoro-steroids and processes for their manufacture 失效
    氟类固醇及其制造方法

    公开(公告)号：US4172075A

    公开(公告)日：1979-10-23

    申请号：US879413

    申请日：1978-02-21

    申请人： Michel Biollaz ,  Jaroslav Kalvoda

    发明人： Michel Biollaz ,  Jaroslav Kalvoda

    IPC分类号： C07J1/00 ,  C07J5/00 ,  C07J7/00 ,  C07J21/00 ,  C07J71/00

    CPC分类号： C07J21/00 ,  C07J1/0037 ,  C07J5/0076 ,  C07J7/009 ,  C07J71/0031

    摘要： 11,12-Unsaturated 9.alpha.-fluorosteroids comprising a new class of steroid compounds are obtained by a novel process, wherein a corresponding 9.alpha.-fluoro-11.beta.-hydroxysteroid is dehydrated with a reagent of the formula F.sub.3 SX in which X denotes an amino group derived from a secondary amine. Of a particular interest among the products of the invention are compounds of the general formula IB ##STR1## in which the symbols R.sub.5 -R.sub.10 have the meanings given hereinafter; such compounds are especially useful as analogues of cortical hormones possessing antiinflammatory activity.

    摘要翻译： 11,12-不饱和的包含新类固醇化合物的9种α-氟甾醇通过新方法获得，其中相应的9α-氟-11β-羟基类固醇用式F3SX的试剂脱水，其中X表示氨基 基团衍生自仲胺。 在本发明的产品中特别感兴趣的是通式IB（IB）的化合物，其中符号R5-R10具有下文给出的含义; 这样的化合物特别可用作具有抗炎活性的皮质激素的类似物。

    Difluorosteroids and processes for their manufacture
    7.
    发明授权
    Difluorosteroids and processes for their manufacture 失效
    二氟类固醇及其制造方法

    公开(公告)号：US4092310A

    公开(公告)日：1978-05-30

    申请号：US598300

    申请日：1975-07-23

    申请人： Michel Biollaz ,  Jaroslav Kalvoda

    发明人： Michel Biollaz ,  Jaroslav Kalvoda

    IPC分类号： C07J75/00 ,  C07J1/00 ,  C07J5/00 ,  C07J7/00 ,  C07J17/00

    CPC分类号： C07J5/0053 ,  C07J1/0003 ,  C07J1/0051 ,  C07J7/0005

    摘要： A novel group of 18,18-difluorosteroids of the general formula ##STR1## wherein St, R.sub.1 and R.sub.2 have the meanings given hereinafter is produced by a chemically novel process characterized in that a corresponding 18-oxo compound is treated with a compound of the formula F.sub.3 SX, wherein X denotes a fluorine atom or an amino group derived from a secondary amine. The compounds of the invention are useful as pharmaceutical intermediates. A number of them are physiologically active and possess hormone-like properties, e.g. those of sexual and/or adrenocortical hormones, such as the gonadotropin-blocking, ovulation-blocking, androgenic, oestrogenic, progestagenic, anabolic, antioestrogenic, antiandrogenic, mineralocorticoid, glucocorticoid and antiinflammatory activity, and can be used in lieu of known hormones or agents possessing corresponding hormone-like properties.

    摘要翻译： 通式（Ⅰ）的新颖的18,18-二氟甾族化合物，其中St，R 1和R 2具有下文给出的含义，是通过化学方法制备的，其特征在于相应的18-氧代化合物用 式F3SX的化合物，其中X表示氟原子或衍生自仲胺的氨基。 本发明的化合物可用作药物中间体。 其中许多具有生理活性并且具有激素样特性，例如， 那些性和/或肾上腺皮质激素，例如促性腺激素阻断，排卵阻断，雄激素，雌激素，孕激素，合成代谢，抗雌激素，抗雄激素，盐皮质激素，糖皮质激素和抗炎活性，并且可以用于代替已知的激素或药剂 具有相应的激素样特性。

    Process for the manufacture of 11.beta.,18-oxido-18,21-dihydroxy-20-oxo-pregnane compounds
    8.
    发明授权
    Process for the manufacture of 11.beta.,18-oxido-18,21-dihydroxy-20-oxo-pregnane compounds 失效
    用于制备11 {62,18-氧化-18,21-二羟基-20-氧代 - 孕烷化合物的方法

    公开(公告)号：US3993644A

    公开(公告)日：1976-11-23

    申请号：US542148

    申请日：1975-01-20

    申请人： Julius Schmidlin ,  Michel Biollaz

    发明人： Julius Schmidlin ,  Michel Biollaz

    IPC分类号： C07J71/00 ,  C07J17/00

    CPC分类号： C07J71/0005

    摘要： A new method for converting 11.beta.,18; 18,20-bis-epoxy-pregn-20-enes to 11.beta.,18-epoxy-18,21-dihydroxy-20-oxo-pregnane compounds or functional derivatives thereof is described and claimed. It consists in treating said bis-epoxy compounds with a heavy metal acylate having an acyloxylating action, such as lead - (IV), cerium - (IV), mercury - (II) and thallium - (III) - acylates. Preferred agent is lead tetraacetate. The reaction is conducted in a solvent or suspending agent like benzene or its homologs or chlorinated paraffins, like methylene chloride, preferably at room temperature and optionally in the presence of an acid.In the 21- acylates of 11.beta.,18-epoxy-18,21-dihydroxy-20-oxo-pregnane compounds thus obtained the 21-hydroxy group and any other protected functional groups can be set free in manner known.The process is especially important for the manufacture of aldosterone or its derivatives.

    摘要翻译： 一种用于转换11 beta，18; 描述和要求保护18,20-双环氧 - 孕-220-烯与11β，18-环氧-18,21-二羟基-20-氧代 - 孕烷化合物或其官能衍生物。 它包括用具有酰氧化作用的重金属酰化物如铅 - （IV），铈 - （IV），汞 - （II）和铊 - （III） - 酰化物）处理所述双环氧化合物。 优选的试剂是四乙酸铅。 反应在溶剂或悬浮剂如苯或其同系物或氯化石蜡如二氯甲烷中进行，优选在室温下，任选地在酸的存在下进行。

    17.beta.-substituted aza-androstane derivatives
    9.
    发明授权
    17.beta.-substituted aza-androstane derivatives 失效
    17β-取代的氮杂 - 雄甾烷衍生物

    公开(公告)号：US5378710A

    公开(公告)日：1995-01-03

    申请号：US132399

    申请日：1993-10-06

    申请人： Michel Biollaz

    发明人： Michel Biollaz

    IPC分类号： A61K31/557 ,  A61P3/00 ,  A61P35/02 ,  A61P43/00 ,  C07J73/00 ,  C07D221/02

    CPC分类号： C07J73/005

    摘要： Compounds of the formula ##STR1## wherein carbon atoms 1 and 2 are linked by a single bond or a double bond, R.sub.1 is hydrogen, methyl or ethyl, and A is a group of the formula --N(--R.sub.2)--X-- wherein R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl and X is C.sub.1 -C.sub.12 alkylene or C.sub.3 -C.sub.6 cycloalkylidene; a group of the formula --N(--R.sub.2)--Y--Phe-- wherein R.sub.2 is as defined above, Y is a direct bond or C.sub.1 -C.sub.6 -alkylene and Phe is an unsubstituted or substituted phenylene radical; a group of the formula --O--X-- wherein X is as defined above, or a group --O--Y--Phe-- wherein Y and Phe are as defined above, are inhibitors of 5.alpha.-reductase and can be used for the therapeutic treatment of the human and animal body.

    摘要翻译： 通过单键或双键连接碳原子1和2的式（I）的化合物，R 1是氢，甲基或乙基，A是式-N（-R 2） - X-其中R 2是氢或C 1 -C 4烷基，X是C 1 -C 12亚烷基或C 3 -C 6亚烷基; 式-N（-R 2）-Y-Phe-的基团，其中R 2如上定义，Y是直接键或C 1 -C 6亚烷基，Phe是未取代或取代的亚苯基; 或式-O-X-的基团，其中X如上定义，或基团-OY-Phe-，其中Y和Phe如上定义，是5α-还原酶的抑制剂，可用于治疗人 和动物体。

    17.beta.-substituted Aza-androstane derivatives
    10.
    发明授权
    17.beta.-substituted Aza-androstane derivatives 失效
    17β-取代的氮杂 - 雄甾烷衍生物

    公开(公告)号：US5304562A

    公开(公告)日：1994-04-19

    申请号：US954081

    申请日：1992-09-30

    申请人： Michel Biollaz

    发明人： Michel Biollaz

    IPC分类号： A61K31/557 ,  A61P3/00 ,  A61P35/02 ,  A61P43/00 ,  C07J73/00 ,  C07D221/02

    CPC分类号： C07J73/005

    摘要： Compounds of the formula ##STR1## wherein carbon atoms 1 and 2 are linked by a single bond or a double bond, R.sub.1 is hydrogen, methyl or ethyl, and A is a group of the formula --N(--R.sub.2)--X-- wherein R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl and X is C.sub.1 -C.sub.12 alkylene or C.sub.3 -C.sub.6 cycloalkylidene; a group of the formula --N(--R.sub.2)--Y--Phe-- wherein R.sub.2 is as defined above, Y is a direct bond or C.sub.1 -C.sub.6 -alkylene and Phe is an unsubstituted or substituted phenylene radical; a group of the formula --O--X-- wherein X is as defined above, or a group --O--Y--Phe-- wherein Y and Phe are as defined above, are inhibitors of 5.alpha.-reductase and can be used for the therapeutic treatment of the human and animal body.

    摘要翻译： 通过单键或双键连接碳原子1和2的式（I）的化合物，R 1是氢，甲基或乙基，A是式-N（-R 2） - X-其中R 2是氢或C 1 -C 4烷基，X是C 1 -C 12亚烷基或C 3 -C 6亚烷基; 式-N（-R 2）-Y-Phe-的基团，其中R 2如上定义，Y是直接键或C 1 -C 6亚烷基，Phe是未取代或取代的亚苯基; 或式-O-X-的基团，其中X如上定义，或基团-OY-Phe-，其中Y和Phe如上定义，是5α-还原酶的抑制剂，可用于治疗人 和动物体。