公开(公告)号：US20040242549A1

公开(公告)日：2004-12-02

申请号：US10856314

申请日：2004-05-28

Applicant: Washington University

Inventor： Douglas F. Covey ,  Xin Jiang

IPC: A61K031/56 ,  C07J053/00

CPC classification number: C07J53/002 ,  C07J53/00 ,  C07J71/001

Abstract: 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 null-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.

Abstract translation: 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。

公开(公告)号：US20040198670A1

公开(公告)日：2004-10-07

申请号：US10407509

申请日：2003-04-04

Inventor： Edward N. Hill ,  Thomas W. Leonard ,  Robert R. Whittle

IPC: A61K031/66 ,  A61K031/56 ,  C07J001/00 ,  C07J053/00

CPC classification number: C07J31/006

Abstract: The present invention relates to novel estrogenic compounds. The present invention also relates to methods of treating estrogen deprivation in a subject comprising administering novel estrogenic compounds. Additionally, the present invention relates to methods of synthesizing novel estrogenic compounds.

Abstract translation: 本发明涉及新型雌激素化合物。 本发明还涉及治疗受试者中雌激素剥夺的方法，包括施用新的雌激素化合物。 另外，本发明涉及新型雌激素化合物的合成方法。

公开(公告)号：US20040072807A1

公开(公告)日：2004-04-15

申请号：US10431351

申请日：2003-05-07

Inventor： David J. Gibson ,  Robert M. Carlson

IPC: A61K031/56 ,  C07J053/00

CPC classification number: A61K31/56 ,  C07J63/008 ,  Y10S514/844

Abstract: The invention is directed to methods of treating fungal and yeast infections using lupeol or solvates, hydrates, or clathrates thereof. The method also encompasses methods of treating fungal and yeast infections by administering to a mammal in need of such treatment a therapeutically effective amount of lupeol. Among the methods used include topical formulations for the improvement of skin appearance.

Abstract translation: 本发明涉及使用lupeol或溶剂化物，水合物或笼形物治疗真菌和酵母菌感染的方法。 该方法还包括通过向需要这种治疗的哺乳动物施用治疗有效量的lupeol来治疗真菌和酵母菌感染的方法。 所使用的方法包括用于改善皮肤外观的局部制剂。

公开(公告)号：US20040030165A1

公开(公告)日：2004-02-12

申请号：US10450278

申请日：2003-06-11

Inventor： Jaap Van Der Louw ,  Dirk Leysen ,  Marcel Evert De Gooijer

IPC: C07J053/00

CPC classification number: C07J53/004

Abstract: Disclosed are androgenic steroids of the (14null,17null)-17-(hydroxymethyl) type. The invention relates to an improvement hereof, which is based on the presence of a &x3B2;-oriented, annellated cyclopropyl group which includes carbon atoms 16 and 17 of the steroid skeleton, i.e. a 16,17null-methylene moiety. These steroids show an unexpectedly high androgenic potency.

Abstract translation: 公开了（14beta，17α）-17-（羟甲基）型的雄激素类固醇。 本发明涉及其改进，其基于存在具有类固醇骨架的碳原子16和17（即16,17β-亚甲基部分）的＆x3B2;取向的环状基团。 这些类固醇表现出意想不到的高雄激素效力。

公开(公告)号：US20030153776A1

公开(公告)日：2003-08-14

申请号：US10356295

申请日：2003-01-31

Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG

Inventor： Markus Sauter ,  Carsten Bender

IPC: C07J053/00

CPC classification number: C07J63/008

Abstract: The invention relates to an improved process for obtaining pure crystalline betulin which is substantially free from betulinic acid, from an extract of birch bark.

Abstract translation: 本发明涉及从桦树皮提取物获得基本上不含桦木酸的纯结晶桦木酸的改进方法。

公开(公告)号：US20030149286A1

公开(公告)日：2003-08-07

申请号：US10355806

申请日：2003-01-31

Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG

Inventor： Markus Sauter

IPC: C07J053/00

CPC classification number: C07J53/00

Abstract: The invention relates to an improved process for obtaining highly pure, crystalline betulinic acid from a methanolic extract of ground plane tree cortex and/or plane tree bark, as well as highly pure crystalline betulinic acid which is solvated with one equivalent of ethanol.

Abstract translation: 本发明涉及从地平面树皮质和/或平面树皮的甲醇提取物以及用一当量乙醇溶剂化的高纯度结晶桦木酸获得高纯度的结晶桦木酸的改进方法。

公开(公告)号：US20030013900A1

公开(公告)日：2003-01-16

申请号：US10172267

申请日：2002-06-14

Inventor： Bruce Allen Pearlman

IPC: C07J053/00 ,  C07J005/00

CPC classification number: C07J5/0053 ,  C07J7/0045 ,  C07J7/0085

Abstract: The present invention is a novel process for the transformation of 11null, 17null dihydroxy-6null-methylpregna-1,4-diene-3,20-dione 17-acetate (III) 1 to 11null,17null,21-trihydroxy-6null-methylpregna-1,4-diene-3,20-dione 21-acetate (VI) 2

Abstract translation: 本发明是一种将11beta，17α二羟基-6α-甲基孕甾-1,4-二烯-3,20-二酮17-乙酸酯（III）转化为11beta，17α，21-三羟基-6α-甲基孕酮 - 1,4-二烯-3,20-二酮21-乙酸酯（VI）

公开(公告)号：US20020016482A1

公开(公告)日：2002-02-07

申请号：US09840627

申请日：2001-04-23

Inventor： Pavel A. Krasutsky

IPC: C07J053/00

CPC classification number: C07C51/367 ,  C07C51/16 ,  C07C62/32 ,  C07C67/08 ,  C07C67/14 ,  C07C67/29 ,  C07C2603/52 ,  C07C69/013 ,  C07C69/16 ,  C07C69/78 ,  C07C69/14

Abstract: The present invention provides a method for preparing betulin-3-acetate including alcoholyzing betulin 3,28-dibenzoate; a process for preparing betulin-3-acetate including: (1) acylating betulin to provide betulin 3,28-dibenzoate and (2) alcoholyzing betulin 3,28-dibenzoate to provide betulin-3-acetate; and a process for preparing betulinic acid including: (1) acylating betulin to provide betulin 3,28-dibenzoate; (2) alcoholyzing betulin 3,28-dibenzoate to provide betulin-3-acetate; (3) oxidizing betulin-3-acetate to provide betulinic aldehyde-3-acetate; (4) oxidizing betulinic aldehyde-3-acetate to provide betulinic acid-3-acetate; and (5) deprotecting betulinic acid-3-acetate to provide betulinic acid.

Abstract translation: 本发明提供了一种制备桦木酸-3-乙酸酯的方法，包括：乙酸bet ulin 3,28-二苯甲酸酯; 制备桦木酸-3-乙酸酯的方法，包括：（1）酰化桦木醇以提供桦木328-二苯甲酸酯和（2）醇zing ulin ulin ulin 3,28-二苯甲酸酯以提供桦木醇-3-乙酸酯; 和一种制备桦木酸的方法，包括：（1）酰化桦木醇以提供桦木328-二苯甲酸酯; （2）将桦木醇3,28-二苯甲酸乙醇溶解，得到桦木醇-3-乙酸酯; （3）氧化桦木醇-3-乙酸酯以提供桦木醛-3-乙酸酯; （4）氧化桦木醛-3-乙酸酯，得到桦木酸-3-乙酸酯; 和（5）将桦木酸-3-乙酸酯脱保护得到桦木酸。

公开(公告)号：US20040266744A1

公开(公告)日：2004-12-30

申请号：US10478581

申请日：2004-07-15

Inventor： David L Burgoyne ,  Yaping Shen ,  Gueijun Ji ,  Yuanlin Zhou ,  Kishore D. Ramachandran ,  Nicholas D. Paschalides ,  Eugene W. Kelleher

IPC: A61K031/56 ,  C07J053/00

CPC classification number: C07J53/00 ,  C07J1/0011 ,  C07J21/008 ,  C07J41/0038 ,  Y02P20/55

Abstract: Steroids containing a cyclohexene moiety are efficiently oxidized to the corresponding null, null-unsaturated ketone using copper iodide and t-butyl hydroperoxide. A steroid compound containing the null, null-unsaturated ketone structure is efficiently converted to the corresponding vicinal diol using a hydroborating reagent followed by oxidative workup, e.g., borane followed by sodium perborate. Benzoyl and substituted benzoyls are superior protecting groups for hydroxyl groups present in the compounds.

公开(公告)号：US20040225139A1

公开(公告)日：2004-11-11

申请号：US10862591

申请日：2004-06-07

Inventor： Keith Biggadike ,  Steven John Coote ,  Rosalyn Kay Nice

IPC: C07J053/00

CPC classification number: A61K31/58 ,  A61K9/0043 ,  A61K31/56

Abstract: The present invention relates to, for example, a compound of formula (VIII) 1 useful in the manufacture of anti-inflammatory androstane derivatives.

Abstract translation: 本发明涉及例如可用于制造消炎雄甾烷衍生物的式（Ⅷ）化合物。