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    Fluocinolone acetonide drug substance polymorphic interconversion
    41.
    发明申请
    Fluocinolone acetonide drug substance polymorphic interconversion 审中-公开
    氟轻松药物物质多态互变

    公开(公告)号：US20070122483A1

    公开(公告)日：2007-05-31

    申请号：US11604552

    申请日：2006-11-27

    申请人： Sharon Myers

    发明人： Sharon Myers

    IPC分类号： A61K9/14

    CPC分类号： A61K31/573 ,  C07D317/70 ,  C07J71/0031

    摘要： Disclosed in embodiments herein is a method of providing the same form of FA. Regardless of which form or mixture of forms are present by forming a slurry from samples of fluocinolone acetonide containing mostly Form A and little to no Form A.

    摘要翻译： 在本文的实施方案中公开的是提供相同形式的FA的方法。 通过从主要形式A和很少到没有形式A的氟轻松的样品形成浆液，不管形式是哪种形式或混合物。

    Nitrosated and nitrosylated compounds and compositions and their use for treating respiratory disorders
    44.
    发明授权
    Nitrosated and nitrosylated compounds and compositions and their use for treating respiratory disorders 失效
    亚硝化和亚硝化化合物及其组合物及其用于治疗呼吸系统疾病的用途

    公开(公告)号：US06579863B1

    公开(公告)日：2003-06-17

    申请号：US09689851

    申请日：2000-10-13

    申请人： David S. Garvey ,  L. Gordon Letts ,  H. Burt Renfroe ,  Stewart K. Richardson

    发明人： David S. Garvey ,  L. Gordon Letts ,  H. Burt Renfroe ,  Stewart K. Richardson

    IPC分类号： A61K3156

    CPC分类号： C07D451/06 ,  C07C313/36 ,  C07D311/22 ,  C07D451/10 ,  C07D471/04 ,  C07J5/00 ,  C07J7/00 ,  C07J31/00 ,  C07J71/00 ,  C07J71/0031

    摘要： Disclosed are (i) compounds of a steroid, a &bgr;-agonist, an anticholinergic, a mast cell stabilizer and a phosphodiesterase (PDE) inhibitor directly or indirectly linked to a NO or NO2 group or a group which stimulates endogenous production of NO or EDRF in vivo; (ii) compositions of steroids, &bgr;-agonists, anticholinergics, mast cell stabilizers and PDE inhibitors, which can optionally be substituted with at least one NO or NO2 moiety or a group which stimulates endogenous production of NO or EDRF in vivo, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or that stimulates endogenous production of NO or EDRF in vivo; and (iii) uses for them in preventing and/or treating respiratory disorders.

    摘要翻译： 公开的是（i）直接或间接连接到NO或NO 2基团或刺激NO或EDRF的内源性产生的基团的类固醇，β-激动剂，抗胆碱能药，肥大细胞稳定剂和磷酸二酯酶（PDE）抑制剂的化合物 体内; （ii）类固醇，β-激动剂，抗胆碱能药物，肥大细胞稳定剂和PDE抑制剂的组合物，其可任选地被至少一个NO或NO 2部分或刺激体内NO或EDRF内源性产生的基团取代;以及化合物 捐赠，转移或释放一氧化氮作为带电物质，即亚硝酸盐（NO +）或硝酰基（NO-），或作为中性物质，一氧化氮（NO））或刺激体内NO或EDRF的内源性产生; 和（iii）用于预防和/或治疗呼吸系统疾病。

    Lambda-1,4-pregnadiene-3,20-diones
    46.
    发明授权
    Lambda-1,4-pregnadiene-3,20-diones 失效
    λ-1,4-孕二烯-3,20-二酮

    公开(公告)号：US5451690A

    公开(公告)日：1995-09-19

    申请号：US372647

    申请日：1995-01-13

    申请人： Luc Devocelle ,  Philippe Mackiewicz

    发明人： Luc Devocelle ,  Philippe Mackiewicz

    IPC分类号： A61K31/57 ,  B01J27/10 ,  C07B61/00 ,  C07J5/00 ,  C07J71/00 ,  C07J7/00

    CPC分类号： C07J71/0031 ,  C07J5/0092

    摘要： A compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, acyl of an organic carboxylic acid of 1 to 8 carbon atoms, allyloxycarbonyl, alkoxycarbonyl and aralkoxycarbonyl of up to 8 carbon atoms and alkylsulfonyl and arylsulfonyl of up to 8 carbon atoms and their use to prepare substituted 16,17-methylenedioxy-steroids and novel intermediates.

    摘要翻译： 式Ⅰ化合物，其中R选自氢，碳原子数1〜8的有机羧酸的酰基，高达8个碳原子的烷氧羰基和芳烷氧基羰基，烷基磺酰基和芳基磺酰基 至8个碳原子，并用于制备取代的16,17-亚甲二氧基类固醇和新型中间体。

    16,17-acetalsubstituted androstane-17.beta.-carboxylic acid esters prossessing high binding affinity to the glucocorticosteroid receptor
    48.
    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。

    Androstane carbothioic acids
    50.
    发明授权
    Androstane carbothioic acids 失效
    雄甾烷硫代酸

    公开(公告)号：US4650610A

    公开(公告)日：1987-03-17

    申请号：US753428

    申请日：1985-07-10

    申请人： Gordon H. Phillipps ,  Brian M. Bain ,  Stuart B. Laing

    发明人： Gordon H. Phillipps ,  Brian M. Bain ,  Stuart B. Laing

    IPC分类号： C07J3/00 ,  C07J31/00 ,  C07J41/00 ,  C07J71/00

    CPC分类号： C07J31/006 ,  C07J3/005 ,  C07J41/0038 ,  C07J71/001 ,  C07J71/0015 ,  C07J71/0031

    摘要： Androstane carbothioic acids of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, a hydroxy group in the .alpha.-configuration, a methyl group which may be in either the .alpha.- or .beta.-configuration, or a methylene group;R.sup.2 represents a hydroxy or protected hydroxy group in either the .alpha.- or .beta.-configuration or an oxo group;R.sup.3 represents a hydrogen, bromine, chlorine or fluorine atom; or R.sup.2 and R.sup.3 together represent a carbon-carbon bond or an epoxy group in the .beta.-configuration;R.sup.4 represents a hydrogen or fluorine atom; and the symbol represents a single or double bond and the salts thereof are useful as intermediates in the preparation of anti-inflammatory androstane 17.beta.-carbothioate esters.The compounds of formula I are prepared by reaction of a reactive derivative of a 17.beta.-carboxylic acid corresponding to the compound of formula I with hydrogen sulphide or a sulphide or hydrosulphide salt.

    摘要翻译： 具有下式的雄甾烷硫代酸：其中R 1表示氢原子，α-构型中的羟基，可以是α或β-构型的甲基或亚甲基; R2表示α或β构型或氧代基中的羟基或被保护的羟基; R3表示氢，溴，氯或氟原子; 或R 2和R 3一起表示β-构型中的碳 - 碳键或环氧基; R4表示氢或氟原子; 符号表示单键或双键，其盐可用作制备抗炎雄激素17β-硫代磷酸酯的中间体。 通式Ⅰ的化合物是通过将对应于式I化合物的17β-羧酸的活性衍生物与硫化氢或硫化物或硫化氢盐反应来制备的。