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    Neuroactive 13,24-cyclo-18,21-dinorcholanes and structurally related pentacylic steroids
    1.
    发明授权
    Neuroactive 13,24-cyclo-18,21-dinorcholanes and structurally related pentacylic steroids 有权
    神经活性13,24-环-18,21-二硼胆碱和结构相关的五酰基类固醇

    公开(公告)号：US08759330B2

    公开(公告)日：2014-06-24

    申请号：US12860345

    申请日：2010-08-20

    申请人： Douglas F. Covey ,  Xin Jiang

    发明人： Douglas F. Covey ,  Xin Jiang

    IPC分类号： A61K31/56 ,  A61K31/58

    CPC分类号： C07J53/002 ,  C07J53/00 ,  C07J71/001

    摘要： Novel pentacyclic steroids and pentacyclic D-homosteroids comprising: (i) the tetracyclic steroid ring system or tetracyclic D-homosteroid ring system, respectively; (ii) a C(3) substituent selected from the group consisting of (a) a hydroxyl or carboxyl in the α-configuration and (b) a sulfate or other negatively charged moiety; and (iii) a fused fifth ring, the fused fifth ring comprising a hydrogen bond acceptor, and (a) in the case of the pentacyclic steroid the C(13) and C(17) carbons, or (b) in the case of the pentacyclic D-homosteroid the C(13) and C(17a) carbons, having utility as anesthetics and in the treatment of disorders relating to GABA function and activity.

    摘要翻译： 新型五环类固醇和五环D-类固醇激素分别包括：（i）四环类固醇环系统或四环D-类固醇环系统; （ii）选自（a）α-构型中的羟基或羧基和（b）硫酸盐或其它带负电荷的部分的C（3）取代基; 和（iii）稠合的第五环，所述稠合的第五环包含氢键受体，和（a）在五环类固醇的情况下，C（13）和C（17）的碳，或（b）在 五环D-类固醇，C（13）和C（17a）碳，可作为麻醉剂用于治疗与GABA功能和活性有关的疾病。

    Neuroactive 13, 24-cyclo-18, 21-dinorcholanes and structurally related pentacyclic steriods
    2.
    发明授权
    Neuroactive 13, 24-cyclo-18, 21-dinorcholanes and structurally related pentacyclic steriods 有权
    神经活性13,24-环-18,21-二硼胆碱和结构相关的五环类固醇

    公开(公告)号：US07781421B2

    公开(公告)日：2010-08-24

    申请号：US10856314

    申请日：2004-05-28

    申请人： Douglas F. Covey ,  Xin Jiang

    发明人： Douglas F. Covey ,  Xin Jiang

    IPC分类号： A61K31/56 ,  A61K31/58 ,  C07J53/00 ,  C07J71/00

    CPC分类号： C07J53/002 ,  C07J53/00 ,  C07J71/001

    摘要： Novel pentacyclic steroids and pentacyclic D-homosteroids comprising: (i) the tetracyclic steroid ring system or tetracyclic D-homosteroid ring system, respectively; (ii) a C(3) substituent selected from the group consisting of (a) a hydroxyl or carboxyl in the α-configuration and (b) a sulfate or other negatively charged moiety; and (iii) a fused fifth ring, the fused fifth ring comprising a hydrogen bond acceptor, and (a) in the case of the pentacyclic steroid the C(13) and C(17) carbons, or (b) in the case of the pentacyclic D-homosteroid the C(13) and C(17a) carbons, having utility as anesthetics and in the treatment of disorders relating to GABA function and activity.

    摘要翻译： 新型五环类固醇和五环D-类固醇激素分别包括：（i）四环类固醇环系统或四环D-类固醇环系统; （ii）选自（a）α-构型的羟基或羧基和（b）硫酸盐或其它带负电荷的部分的C（3）取代基; 和（iii）稠合的第五环，所述稠合的第五环包含氢键受体，和（a）在五环类固醇的情况下，C（13）和C（17）的碳，或（b）在 五环D-类固醇，C（13）和C（17a）碳，可作为麻醉剂用于治疗与GABA功能和活性有关的疾病。

    Neuroactive 13,24-Cyclo-18,21-Dinorcholanes and Structurally Related Pentacylic Steroids
    3.
    发明申请
    Neuroactive 13,24-Cyclo-18,21-Dinorcholanes and Structurally Related Pentacylic Steroids 有权
    神经活性13,24-环-18,21-二硼胆碱和结构相关的Pentacylic类固醇

    公开(公告)号：US20100317638A1

    公开(公告)日：2010-12-16

    申请号：US12860345

    申请日：2010-08-20

    申请人： Douglas F. Covey ,  Xin Jiang

    发明人： Douglas F. Covey ,  Xin Jiang

    IPC分类号： A61K31/58 ,  A61P25/08 ,  A61P25/24 ,  A61P25/22 ,  A61P25/30 ,  A61K31/575

    CPC分类号： C07J53/002 ,  C07J53/00 ,  C07J71/001

    摘要： Novel pentacyclic steroids and pentacyclic D-homosteroids comprising: (i) the tetracyclic steroid ring system or tetracyclic D-homosteroid ring system, respectively; (ii) a C(3) substituent selected from the group consisting of (a) a hydroxyl or carboxyl in the α-configuration and (b) a sulfate or other negatively charged moiety; and (iii) a fused fifth ring, the fused fifth ring comprising a hydrogen bond acceptor, and (a) in the case of the pentacyclic steroid the C(13) and C(17) carbons, or (b) in the case of the pentacyclic D-homosteroid the C(13) and C(17a) carbons, having utility as anesthetics and in the treatment of disorders relating to GABA function and activity.

    摘要翻译： 新型五环类固醇和五环D-类固醇激素分别包括：（i）四环类固醇环系统或四环D-类固醇环系统; （ii）选自（a）α-构型中的羟基或羧基和（b）硫酸盐或其它带负电荷的部分的C（3）取代基; 和（iii）稠合的第五环，所述稠合的第五环包含氢键受体，和（a）在五环类固醇的情况下，C（13）和C（17）的碳，或（b）在 五环D-类固醇，C（13）和C（17a）碳，可作为麻醉剂用于治疗与GABA功能和活性有关的疾病。

    "> Open
    5.
    发明授权
    Open "D" ring hormone analogs 失效
    打开“D”环激素类似物

    公开(公告)号：US4874891A

    公开(公告)日：1989-10-17

    申请号：US858393

    申请日：1986-05-01

    申请人： Douglas F. Covey ,  Ricahrd J. Auchus

    发明人： Douglas F. Covey ,  Ricahrd J. Auchus

    IPC分类号： C07C39/17 ,  C07C39/23 ,  C07C62/38

    CPC分类号： C07C62/38 ,  C07C39/17 ,  C07C39/23 ,  C07C2103/26

    摘要： Compounds of the formula: ##STR1## and the pharmaceutically acceptable esters thereof, wherein rings A and B are selected from the group consisting of ##STR2## wherein x represents an aromatic ring, or the presence or absence of 0, 1, or 2 conjugated or unconjugated .pi. bond(s), andwherein x represents the presence or absence of 0, 1, or 2 conjugated or unconjugated .pi. bond(s), andwherein a non-aromatic .pi. bond, if present, may optionally be converted to an epoxide;and wherein the dotted line represents the presence or absence of a .pi. bond,and wherein:R.sup.1 is H, acyl(1-6), or alkyl(1-6);R.sup.2 is H, alkyl(1.varies.6), 2-propynyl, or allenyl;R.sup.3 and R.sup.4 is each independently H or OR.sup.5, wherein R.sup.5 is H, acyl(1-6), or alkyl(1-6); andwherein R.sub.1 and R.sub.2 is each independently H, alkyl(1-6) or is --C.tbd.CR.sub.3, --CH.dbd.CHR.sub.3, or --CH.dbd.C.dbd.CHR.sub.3, wherein R.sub.3 is selected from the group consisting of H, halo, CF.sub.3, alkyl(1-6), acyloxy, carboxylate, carboalkoxylate, alkoxy, or alkylthio;and wherein when at least one of R.sub.1 and R.sub.2 is H, the compound of Formula 1 may also be in the oxidized oxo form and when both R.sub.1 and R.sub.2 are H, the compound of Formula 1 may also be in the oxidized carboxylic acid form or the alkyl(1-6) ester thereof are useful in regulating steroid metabolism.

    摘要翻译： （a）化合物及其药学上可接受的酯，其中环A和B选自由下列组成的组：（a）图像（b）图像（c）图像（d） ）其中x表示芳族环，或0,1或2个共轭或非共轭π键的存在或不存在，其中x表示0,1或2共轭或未偶联的π键的存在或不存在（ s），并且其中非芳族π键（如果存在）可以任选地转化为环氧化物; 并且其中虚线表示π键的存在或不存在，并且其中：R 1是H，酰基（1-6）或烷基（1-6）; R2是H，烷基（1比例6），2-丙炔基或丙二烯基; R 3和R 4各自独立地为H或OR 5，其中R 5为H，酰基（1-6）或烷基（1-6）; 并且其中R 1和R 2各自独立地为H，烷基（1-6）或-C 3 CH 3，-CH = CHR 3或-CH = C = CHR 3，其中R 3选自H，卤素，CF 3 ，（1-6）烷基，酰氧基，羧酸酯，烷氧羰基，烷氧基或烷硫基; 并且其中当R 1和R 2中的至少一个为H时，式1的化合物也可以是氧化的氧代形式，并且当R 1和R 2均为H时，式1的化合物也可以是氧化的羧酸形式或 其烷基（1-6）酯可用于调节类固醇代谢。

    Modified, hydroxy-substituted aromatic structures having cytoprotective activity
    6.
    发明授权
    Modified, hydroxy-substituted aromatic structures having cytoprotective activity 有权
    具有细胞保护活性的改性羟基取代芳族结构

    公开(公告)号：US09156876B2

    公开(公告)日：2015-10-13

    申请号：US12888560

    申请日：2010-09-23

    申请人： Douglas F. Covey

    发明人： Douglas F. Covey

    IPC分类号： A61K31/566 ,  A61K31/565 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P27/06 ,  A61P27/12 ,  A61P9/10 ,  C07J1/00

    CPC分类号： C07J1/00 ,  A61K31/565 ,  C07J1/0059 ,  C07J1/007

    摘要： The present invention is directed to a process for conferring cytoprotection on a population of cells which comprises administering to that population of cells a compound comprising a hydroxy-substituted aromatic ring structure and a non-fused polycyclic, hydrophobic substituent attached thereto. In particular, the present invention is directed to such a process wherein the administered compound is phenolic, such as a steriod (e.g., estrogen), and has a non-fused polycyclic, hydrophobic substituent attached to the hydroxy-substituted A-ring thereof.

    摘要翻译： 本发明涉及对细胞群赋予细胞保护作用的方法，其包括向所述细胞群施用包含羟基取代的芳环结构和与其连接的非稠合多环疏水性取代基的化合物。 特别地，本发明涉及这样的方法，其中所施用的化合物是酚类，例如steriod（例如雌激素），并且具有与其羟基取代的A环连接的非稠合的多环疏水性取代基。

    Lactam and thiolactam derivatives as anesthetic and conscious sedation agents
    7.
    发明授权
    Lactam and thiolactam derivatives as anesthetic and conscious sedation agents 失效
    内酰胺和硫代内酰胺衍生物作为麻醉剂和清醒镇静剂

    公开(公告)号：US06680331B2

    公开(公告)日：2004-01-20

    申请号：US09907547

    申请日：2001-07-16

    申请人： James A. Ferrendelli ,  Douglas F. Covey

    发明人： James A. Ferrendelli ,  Douglas F. Covey

    IPC分类号： A61K3140

    CPC分类号： A61K31/40

    摘要： This invention relates to lactam and thiolactam derivatives having useful anesthetic and conscious sedation activity. Particularly useful compounds include the diethyl lactams such as 3,3-diethyl-2-pyrrolidinone. Methods for using these compounds and pharmaceutical compositions containing these compounds are provided.

    摘要翻译： 本发明涉及具有有用的麻醉和清醒镇静作用的内酰胺和硫代内酰胺衍生物。 特别有用的化合物包括二乙基内酰胺如3,3-二乙基-2-吡咯烷酮。 提供使用这些化合物的方法和含有这些化合物的药物组合物。