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    Process for the preparation of 16,17 acetals of pregnane derivatives with control of the epimeric distribution at the C-22 position
    11.
    发明授权
    Process for the preparation of 16,17 acetals of pregnane derivatives with control of the epimeric distribution at the C-22 position 失效
    制备16,17缩醛的孕烷衍生物的方法，控制C-22位置的差向异构体分布

    公开(公告)号：US06169178A

    公开(公告)日：2001-01-02

    申请号：US09067711

    申请日：1998-04-28

    申请人： Filippo La Loggia ,  Paolo Petacchi

    发明人： Filippo La Loggia ,  Paolo Petacchi

    IPC分类号： C07J7100

    CPC分类号： C07J71/0031 ,  C07J71/0015

    摘要： Described herein is a process for the preparation of an acetal of formula (I) in which R1 is an alkyl, R2 is H or an acyl, X is &bgr;-OH and Y is H, comprising the acetalization with control of the epimeric distribution at the C-22 position, for treatment with R1 CHO in aqueous HBr or HI of a compound of formula (II) in which R2 has the meaning specified above, R3 and R4 are both H, or, taken together, are —C(R5)(R6)—, where R5 and R6, which may be the same or different from one another, are alkyl groups, and X and Y are chosen from among the following: A) X and Y, taken together, are an additional bond between C-9 and C-11; B) X is &bgr;-OH, and Y is H or an &agr;-halogen; C) X is &bgr;-OR7 where R7 is an acyl, and Y is H or an &agr;-halogen; and D) X and Y, taken together, are —O—.

    摘要翻译： 本文描述了制备式（I）的缩醛的方法，其中R 1是烷基，R 2是H或酰基，X是β-OH，Y是H，包括缩醛化，其控制在 C-22位，用于在R 2具有上述含义的式（II）化合物的HBr或HI水溶液中用R 1 CHO处理，R 3和R 4均为H或一起为-C（R 5） ）（R 6） - ，其中可以相同或不同的R 5和R 6是烷基，X和Y选自如下：A）X和Y一起是附加键 C-9和C-11之间; B）X是β-OH，Y是H或α-卤素; C）X是β-OR7，其中R7是酰基，Y是H或α-卤素; 和D）X和Y一起为-O-。

    Steroid esters
    12.
    发明授权
    Steroid esters 失效
    类固醇酯

    公开(公告)号：US5888995A

    公开(公告)日：1999-03-30

    申请号：US493733

    申请日：1995-06-22

    申请人： Bengt Ingemar Axelsson ,  Ralph Lennart Brattsand ,  Leif Arne Kallstrom ,  Bror Arne Thalen

    发明人： Bengt Ingemar Axelsson ,  Ralph Lennart Brattsand ,  Leif Arne Kallstrom ,  Bror Arne Thalen

    IPC分类号： C07J71/00 ,  A61K31/58

    CPC分类号： C07J71/0031

    摘要： The invention concerns compounds of formula I ##STR1## in which R.sub.1 is hydrogen or a straight or branched hydrocarbon chain; R.sub.2 is hydrogen or a straight or branched hydrocarbon chain; R.sub.3 is acyl; X.sub.1 is hydrogen, fluorine or chlorine; and X.sub.2 is hydrogen, fluorine or chlorine. Also disclosed are processes for preparation of the compounds, pharmaceutical compositions containing them and methods employing the compounds in the treatment of inflammatory and allergic conditions.

    摘要翻译： 本发明涉及其中R 1为氢或直链或支链烃链的式Ⅰ化合物; R2是氢或直链或支链烃链; R3是酰基; X1是氢，氟或氯; X2是氢，氟或氯。 还公开了制备化合物的方法，含有它们的药物组合物和使用该化合物治疗炎性和过敏性疾病的方法。

    Process for the preparation of steroid derivatives
    14.
    发明授权
    Process for the preparation of steroid derivatives 失效
    类固醇衍生物的制备方法

    公开(公告)号：US5750734A

    公开(公告)日：1998-05-12

    申请号：US849015

    申请日：1997-05-23

    申请人： Nigel Christopher Parkinson ,  Andrew Paul Van Sickle

    发明人： Nigel Christopher Parkinson ,  Andrew Paul Van Sickle

    IPC分类号： C07J71/00

    CPC分类号： C07J71/0031

    摘要： A process is described for the preparation of a compound of formula (I) or a stereoisomeric compound thereof, in which the 1,2-position is saturated or is a double bond; X.sup.1 and X.sup.2 are each independently hydrogen or halogen; R.sup.1 is hydrogen or acyl; R.sup.2 is hydroxyl, acyloxy or oxo; and R.sup.3 is alkyl, by reacting a compound of formula (II) with an aldehyde R.sup.3 CHO in either phosphoric acid or about 60% to about 75% w/w sulphuric acid. Compounds of formula (I) are either pharmacologically active steroids or are intermediates in the synthesis of pharmacologically active steroids. ##STR1##

    摘要翻译： PCT No.PCT / GB95 / 02568 Sec。 371日期1997年5月23日 102（e）日期1997年5月23日PCT提交1995年11月2日PCT公布。 公开号WO96 / 16978 日期1996年6月6日描述了制备式（I）化合物或其立体异构体化合物的方法，其中1,2-位饱和或为双键; X1和X2各自独立地为氢或卤素; R1是氢或酰基; R2是羟基，酰氧基或氧代; 和R 3是烷基，通过式（II）化合物与醛R3CHO在磷酸或约60％至约75％w / w硫酸中反应。 式（I）化合物是药理学活性类固醇，或是合成药理活性类固醇的中间体。 （I）（II）

    Silyl Compounds and their use
    15.
    发明授权
    Silyl Compounds and their use 失效
    硅烷化合物及其用途

    公开(公告)号：US5728826A

    公开(公告)日：1998-03-17

    申请号：US704574

    申请日：1996-11-25

    申请人： Beate Gutterer

    发明人： Beate Gutterer

    IPC分类号： A61K31/58 ,  A61P29/00 ,  C07J71/00

    CPC分类号： C07J71/0031

    摘要： The invention describes a process for the epimer enrichment of compounds of formula (I) by silation, fractionated crystallization and acid hydrolysis. ##STR1##

    摘要翻译： PCT No.PCT / EP95 / 00836 Sec。 371日期：1996年11月25日 102（e）日期1996年11月25日PCT 1995年3月7日PCT PCT。 公开号WO95 / 24416 PCT 日期1995年9月14日本发明描述了通过淤浆，分级结晶和酸水解使式（I）化合物的差向异构体富集的方法。 （一）

    Pregna-1,4-diene3,20-dione-16-17-acetal-21 esters, process for their preparation, composition, and methods for the treatment of inflammatory conditions
    17.
    发明授权
    Pregna-1,4-diene3,20-dione-16-17-acetal-21 esters, process for their preparation, composition, and methods for the treatment of inflammatory conditions 失效
    前草-1,4-二烯-3,20-二酮-16-17-乙缩醛-21酯，其制备方法，组合物和治疗炎性病症的方法

    公开(公告)号：US5482934A

    公开(公告)日：1996-01-09

    申请号：US278112

    申请日：1994-07-20

    申请人： Jose Calatayud ,  Jose R. Conde ,  Manuel Luna

    发明人： Jose Calatayud ,  Jose R. Conde ,  Manuel Luna

    IPC分类号： A61K31/58 ,  A61P29/00 ,  C07J5/00 ,  C07J71/00

    CPC分类号： C07J5/0092 ,  C07J71/0031

    摘要： The present invention relates to compounds of the formula: ##STR1## in which X.sub.1 and X.sub.2 correspond to H or F without distinction; R.sub.1 represents the following radicals: ##STR2## and R.sub.2 represents the radicals ##STR3## in the form of an R epimer, an S epimer, or a stereoisomeric mixture of the R and S epimers in terms of the orientation of the substituents on the carbon atom at position 22, novel intermediates and a method of their preparation by hydrolysis-ketalization, and use of such compounds as drugs and/or therapeutic agents.

    摘要翻译： 本发明涉及下式的化合物：其中X1和X2不区分对应于H或F; R1表示以下基团：R 1和R 2分别代表取代基的R取代基的取代基的R差向异构体，S差向异构体或立体异构体混合物的形式的基团 在22位的碳原子上，新的中间体及其通过水解缩醛化制备的方法，以及使用这些化合物作为药物和/或治疗剂。

    Anti-inflammatory carboxycyclic acetal pregnane derivatives
    18.
    发明授权
    Anti-inflammatory carboxycyclic acetal pregnane derivatives 失效
    抗炎性羧基环缩醛孕烷衍生物

    公开(公告)号：US5200518A

    公开(公告)日：1993-04-06

    申请号：US658542

    申请日：1991-02-21

    申请人： Hyun P. Kim ,  Kwan S. Sin ,  Chang M. Kim ,  Moon Y. Heo ,  Henry J. Lee

    发明人： Hyun P. Kim ,  Kwan S. Sin ,  Chang M. Kim ,  Moon Y. Heo ,  Henry J. Lee

    IPC分类号： C07J5/00 ,  C07J7/00 ,  C07J13/00 ,  C07J21/00 ,  C07J41/00 ,  C07J71/00

    CPC分类号： C07J13/005 ,  C07J21/00 ,  C07J41/005 ,  C07J5/0092 ,  C07J7/0095 ,  C07J71/0031

    摘要： Compounds of the formula: ##STR1## wherein X is H, F, Cl, or CH.sub.3and Y is ##STR2## wherein R.sub.1 is H, alkyl of 1-5 carbon atoms, phenyl, or benzyl;R.sub.2 is COOR.sub.6, R.sub.5 COOR.sub.6, or R.sub.5 CONHR.sub.6 ;R.sub.3 is H, F, OH, or CH.sub.3 ;R.sub.4 is CH.sub.2 OH, CH.sub.2 OCOR.sub.6, COOR.sub.6, or CONHR.sub.6 ;R.sub.5 is alkyl of 1-3 carbon atoms;R.sub.6 is alkyl of 1-5 carbon atoms, or benzyl; represents a single or double bond;.about. represents .alpha.-position, .beta.-position, or a mixture of both .alpha.- and .beta.-positions; and-- represents .alpha.-position;and methods for preparing the same.

    摘要翻译： 其中X是H，F，Cl或CH 3，Y是下式的化合物：其中R 1是H，1-5个碳原子的烷基，苯基或苄基; R2是COOR6，R5 COOR6或R5CONHR6; R3是H，F，OH或CH3; R4是CH2OH，CH2OCOR6，COOR6或CONHR6; R5是1-3个碳原子的烷基; R6是1-5个碳原子的烷基，或苄基; 代表单键或双键; 差异表示α位，β位，或α和β位的混合物; 和 - 表示α位; 及其制备方法。

    Redox carriers for brain-specific drug delivery
    19.
    发明授权
    Redox carriers for brain-specific drug delivery 失效
    用于脑特异性药物递送的氧化还原载体

    公开(公告)号：US5087618A

    公开(公告)日：1992-02-11

    申请号：US295663

    申请日：1989-01-11

    申请人： Nicholas S. Bodor

    发明人： Nicholas S. Bodor

    IPC分类号： A61K38/00 ,  C07D209/32 ,  C07D211/90 ,  C07D213/80 ,  C07D213/82 ,  C07D401/12 ,  C07J43/00 ,  C07J71/00 ,  C07K5/078 ,  C07K5/097 ,  C07K14/70

    CPC分类号： C07D213/80 ,  A61K47/48161 ,  C07D209/32 ,  C07D211/90 ,  C07D213/82 ,  C07D401/12 ,  C07J43/003 ,  C07J71/0031 ,  C07K14/70 ,  C07K5/06139 ,  C07K5/0821 ,  A61K38/00

    摘要： The invention provides compounds of the formulaD--DHC].sub.n (I)and the nontoxic pharmaceutically acceptable salt thereof, wherein D is the residue of a centrally acting drug containing at least one reactive functional group selected from the group consisting of amino, hydroxyl, mercapto, carboxyl, amide and imide, said residue being characterized by the absence of a hydrogen atom from at least one of said reactive functional groups in said drug; n is a positive integer equal to the number of said functional groups from which a hydrogen atom is absent; and [DHC] is the reduced, biooxidizable, bloodbrain barrier penetrating lipoidal form of a dihydropyridine.revreaction.pyridinium salt redox carrier, said carrier comprising a bivalent radical of the formula ##STR1## wherein the alkylene group can be straight or branched and can contain 1 to 3 carbon atoms; R.sub.o is a radical identical to the corresponding portion of a natural amino acid; and p is 1 or 2, provided that, when p is 2, then the alkylene groups can be the same or different and the R.sub.0 radicals can be the same or different; said bivalent radical being so positioned that the terminal carbonyl function of the bivalent radical is linked to the drug residue while the terminal amino function of the bivalent radical is linked to the remaining portion of the carrier moiety. The subject compounds are adapted for the site-specific/sustained delivery of centrally acting drugs to the brain. The corresponding pyridinium salt type drug/carrier entities D--QC.sup.+ ].sub.n qY.sup.-t are also disclosed.

    摘要翻译： 本发明提供式D-DHC] n（I）化合物及其无毒的药学上可接受的盐，其中D是含有至少一个选自氨基，羟基， 巯基，羧基，酰胺和酰亚胺，所述残基的特征在于所述药物中至少一个所述反应性官能团不存在氢原子; n是与不存在氢原子的所述官能团的数目相等的正整数; 和[DHC]是二氢吡啶 - >β-吡啶鎓盐氧化还原载体的还原的，生物可氧化的血脑屏障穿透的脂质形式，所述载体包含式“IMAGE”的二价基团，其中亚烷基可以是直链或支链的，并且可以 含有1至3个碳原子; Ro是与天然氨基酸的相应部分相同的基团; p为1或2，条件是当p为2时，亚烷基可以相同或不同，R 0基团可以相同或不同; 所述二价基团的定位使得二价基团的末端羰基官能团与药物残基连接，而二价基团的末端氨基官能团与载体部分的剩余部分连接。 主题化合物适用于将中枢作用药物的位点特异性/持续递送给脑。 还公开了相应的吡啶鎓盐型药物/载体实体D-QC +] n qY-t。