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81. 发明申请

US20100317638A1 Neuroactive 13,24-Cyclo-18,21-Dinorcholanes and Structurally Related Pentacylic Steroids 有权
标题翻译：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。

82. 发明申请

US20070060746A1 PROCESSES FOR PREPARATION OF 9,11 EPOXY STEROIDS AND INTERMEDIATES USEFUL THEREIN 审中-公开
标题翻译：制备9,11环氧甾体的方法及其有用的中间体
公开(公告)号：US20070060746A1
公开(公告)日：2007-03-15
申请号：US11459040
申请日：2006-07-21
申请人： John Ng , Ping Wang , Julio Baez , Chin Liu , Dennis Anderson , Jon Lawson , Bernhard Erb , Joseph Wieczorek , Gennaro Mucciariello , Fortunato Vanzanella , Sastry Kunda , Leo Letendre , Mark Pozzo , Yuen-Lung Sing , Edward Yonan
发明人： John Ng , Ping Wang , Julio Baez , Chin Liu , Dennis Anderson , Jon Lawson , Bernhard Erb , Joseph Wieczorek , Gennaro Mucciariello , Fortunato Vanzanella , Sastry Kunda , Leo Letendre , Mark Pozzo , Yuen-Lung Sing , Edward Yonan
IPC分类号： C07J71/00 , C07J53/00
CPC分类号： C07J71/00 , C07J21/00 , C07J21/003 , C07J31/006 , C07J53/00 , C07J53/002 , C07J71/0015 , C12P33/005 , C12P33/10 , C12Q1/02
摘要： Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I wherein: -A-A- represents the group —CHR4—CHR5— or —CR4═CR5— —R3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, aryloxy, R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical, —B—B— represents the group —CHR6—CHR7— or an alpha- or beta-oriented group: where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, and R8 and R9 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, or R8 and R9 together comprise a carbocyclic or heterocyclic ring structure, or R8 or R9 together with R6 or R7 comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring.
摘要翻译：提供了多种新的反应方案，新的方法步骤和新的中间体，用于合成环氧麦克风和其它式I化合物，其中：-AA-代表基团-CHR 4 -CHR 5， SUP→ - 或-CR 4 -CR 5 - -R 3，R 4和R 4 - 5个独立地选自氢，卤素，羟基，低级烷基，低级烷氧基，羟基烷基，烷氧基烷基，羟基羰基，氰基，芳氧基，R 1表示α取向的低级烷氧基羰基或羟烷基，-BB-代表基团-CHR 6 -CHR 7 - 或α或β取代基团：其中R 6， SO 2和R 7独立地选自氢，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基，芳氧基和R 8和R 9独立地选自氢，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基，芳氧基或R 8和R 9共同构成碳环或杂环结构或R 9或R 9与R 6或R 7连同包含碳环或杂环结构稠合到五环D环。

83. 发明申请

US20040102426A1 16,17-carbocyclic condensed steroid compounds having selective estrogenic activity 有权
标题翻译：具有选择性雌激素活性的16,17-碳环缩合类固醇化合物
公开(公告)号：US20040102426A1
公开(公告)日：2004-05-27
申请号：US10297706
申请日：2002-12-06
发明人： Hubert Jan Jozef Loozen
IPC分类号： A61K031/58 , A61K031/56 , C07J053/00
CPC分类号： C07J53/002
摘要： The invention discloses a steroid compound having the formula (1), wherein dotted bonds represent optional double bonds; R6 is H, nullCH2, or nullCH3, or nullCH2nullCH3; R7 is H C1-4-alkyl, C2-5 alkenyl or C2-5-alkynyl, wherein the alkyl, alkenyl or alkynyl group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; R11 is H, C1-4-alkyl, C2-4-alkenyl, C2-4-alkynyl or C1-4-alkylidene, wherein the alkyl, alkenyl, alkynyl or alkylidene group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; E represents together with carbon atoms 16 and 17 of the steroid skeleton a four to seven-membered ring, said ring being null and in cis-configuration with respect to the steroid skeleton, optionally comprising one or two endocyclic bonds; or a prodrug thereof. Such compounds can be used in therapy and for methods for selective modification of the activity of estrogen receptors. 1
摘要翻译：本发明公开了具有式（1）的类固醇化合物，其中虚线键代表任选的双键; R 6是H，= CH 2或-CH 3或-CH 2 -CH 3; R 7是C 1-4 - 烷基，C 2-5烯基或C 2-5炔基，其中烷基，烯基或炔基可以被独立地选自氟或氯原子的1至3个卤素原子取代; R 11是H，C 1-4 - 烷基，C 2-4 - 烯基，C 2-4 - 炔基或C 1-4 - 亚烷基，其中烷基，烯基，炔基或亚烷基可以被1至3个独立地选自该组氟或氯原子; E与类固醇骨架的碳原子16和17一起形成4至7元环，所述环为α并且相对于类固醇骨架为顺式构型，任选包含一个或两个内环键; 或其前药。这些化合物可用于治疗和选择性修饰雌激素受体活性的方法。

84. 发明申请

US20040067917A1 Processes for preparation of 9, 11-epoxy steroids and intermediates useful therein 失效
标题翻译：用于制备9,11-环氧类固醇及其中有用的中间体的方法
公开(公告)号：US20040067917A1
公开(公告)日：2004-04-08
申请号：US10672680
申请日：2003-09-26
申请人： G. D. Searle & Company
发明人： John S. Ng , Ping T. Wang , Julio A. Baez , Chin Liu , Dennis K. Anderson , Jon P. Lawson , Bernhard Erb , Joseph Wieczorek , Gennaro Mucciariello , Fortunato Vanzanella , Sastry A. Kunda , Leo J. Letendre , Mark J. Pozzo , Yuen-Lung L. Sing , Edward E. Yonan
IPC分类号： A61K031/56 , C07J053/00
CPC分类号： C07J71/00 , C07J21/00 , C07J21/003 , C07J31/006 , C07J53/00 , C07J53/002 , C07J71/0015 , C12P33/005 , C12P33/10 , C12Q1/02
摘要： Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I 1 wherein: -A-A- represents the group nullCHR4nullCHR5null or nullCR4nullCR5nullR3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, aryloxy, R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical, -B-B- represents the group nullCHR6nullCHR7 or an alpha- or beta-oriented group: 2 where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, and R1 and R9 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano, aryloxy, or R8 and R9 together comprise a carbocyclic or heterocyclic ring structure, or R8 or R9 together with R6 or R7 comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring.
摘要翻译：提供了多种新的反应方案，新的方法步骤和新的中间体用于合成环氧麦克风和其它式I化合物，其中：-AA-表示-CHR 4 -CHR 5 - 或-CR 4 = CR 5 -R 3，R 4和R 5独立地选自氢，卤素，羟基，低级烷基，低级烷氧基，羟基烷基，烷氧基烷基，羟基羰基，氰基，芳氧基，R 表示α-取代的低级烷氧基羰基或羟烷基，-BB-表示-CHR 6 -CHR 7基团或α或β-取代基团：其中R 6和R 7为卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基，芳氧基，R 1和R 9独立地选自由以下组成的组：氢，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基，芳氧基或R 8 nd R 9一起包含碳环或杂环结构，或R 8或R 9与R 6或R 7一起包含与五环D环稠合的碳环或杂环结构。

85. 发明申请

US20030130246A1 Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs 失效
标题翻译：用于增强口服吸收和药物全身生物利用度的胆汁酸衍生化合物
公开(公告)号：US20030130246A1
公开(公告)日：2003-07-10
申请号：US10229565
申请日：2002-08-28
发明人： Laxminarayan Bhat , Mark A. Gallop , Bernd Jandeleit
IPC分类号： A61K031/58 , C07J043/00 , C07J017/00 , A61K031/56
CPC分类号： C07J31/006 , C07J9/005 , C07J41/0055 , C07J53/002 , C07J71/0005 , C07J71/0047 , C07J71/0063
摘要： Disclosed are compounds that exhibit high transport across the intestinal wall of an animal. The compounds may optionally be linked to drugs that are poorly absorbed or poorly transported across the intestinal wall after oral administration to provide for enhanced therapeutic, and optionally prolonged therapeutic, systemic blood concentrations of the drugs upon oral administration of the drug-compound conjugate. Also disclosed are pharmaceutical compositions containing and methods of using such compounds.
摘要翻译：公开了表现出高度运输通过动物肠壁的化合物。所述化合物可任选地与口服给药后通过肠壁不良吸收或运输不良的药物连接，以提供药物 - 化合物缀合物口服后药物的增强的治疗和任选地延长的治疗性全身血液浓度。还公开了含有药物组合物和使用这些化合物的方法。

86. 发明申请

US20020038021A1 Eplerenone crystalline form exhibiting enhanced dissolution rate 审中-公开
标题翻译：依普利酮结晶形式具有增强的溶解速率
公开(公告)号：US20020038021A1
公开(公告)日：2002-03-28
申请号：US09732208
申请日：2000-12-07
发明人： Kathleen P. Barton , Thomas B. Borchardt , Marlon V. Carlos , Subhash Desai , Leonard J. Ferro , Henry T. Gaud , Scott S. Ganser , Clay R. Little , Partha S. Mudipalli , Mark A. Pietz , Daniel R. Pilipauskas , Yuen-Lung L. Sing , Glenn L. Stahl , Joseph J. Wieczorek , Chris Y. Yan
IPC分类号： C07J017/00 , C07J001/00 , C07J021/00
CPC分类号： C12P33/005 , C07D301/12 , C07J1/0059 , C07J21/00 , C07J21/003 , C07J31/006 , C07J41/0094 , C07J53/002 , C07J71/0005 , C07J71/0015 , C12P33/10 , C12Q1/02
摘要： A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.
摘要翻译：提供醛固酮受体拮抗剂药物依普利酮的新型结晶形式（形式H），其在水性介质中具有相对快速的溶解速率。还提供了eplerenone的新型溶剂化结晶形式，当脱溶时，可以产生H形式。还提供了非依依普利酮。提供了药物组合物，其包含H形式H eplerenone，任选地伴随有一种或多种其他固体形式的依普利酮，总单位剂量为约10至约1000mg的依普利酮，并且还包含一种或多种药学上可接受的赋形剂。提供了制备H形式H eplerenone和制备包含H型肝素的组合物的方法。还提供了用于预防和/或治疗醛固酮介导的病症或病症的方法，其包括向受试者施用治疗有效量的依普利酮，其中至少一部分所述的依普利酮是H型肾上腺素。

87. 发明授权

US06335441B1 5&bgr;-cyano-substituted steroid compounds 失效
标题翻译： 5β-氰基取代的类固醇化合物
公开(公告)号：US06335441B1
公开(公告)日：2002-01-01
申请号：US09583158
申请日：2000-05-30
申请人： John S. Ng , Chin Liu , Dennis K. Anderson , Jon P. Lawson , Bernhard Erb , Joseph Wieczorek , Sastry A. Kunda , Leo J. Letendre , Mark J. Pozzo , Yuen-Lung L. Sing , Edward E. Yonan
发明人： John S. Ng , Chin Liu , Dennis K. Anderson , Jon P. Lawson , Bernhard Erb , Joseph Wieczorek , Sastry A. Kunda , Leo J. Letendre , Mark J. Pozzo , Yuen-Lung L. Sing , Edward E. Yonan
IPC分类号： C07J5300
CPC分类号： C07J71/00 , C07J21/00 , C07J21/003 , C07J31/006 , C07J53/00 , C07J53/002 , C07J71/0015 , C12P33/005 , C12P33/10 , C12Q1/02
摘要： Novel 5&bgr;-cyano steroid compounds including compounds of Formula VII: wherein A—A, B—B, R3, R8 and R9 are as defined in the specification.
摘要翻译：包括式VII化合物的新型5β-氰基类固醇化合物：其中A-A，B-B，R 3，R 8和R 9如说明书中所定义。

88. 发明授权

US06313180B1 Steroid compounds having contraceptive and anti-osteoporosis activity 有权
标题翻译：具有避孕和抗骨质疏松活性的类固醇化合物
公开(公告)号：US06313180B1
公开(公告)日：2001-11-06
申请号：US09538783
申请日：2000-03-30
申请人： Hubert Jan Jozef Loozen
发明人： Hubert Jan Jozef Loozen
IPC分类号： A61K3156
CPC分类号： C07J53/002
摘要： The invention relates to a steroid compound having the formula (I) comprising a ring E, said ring sharing carbon atoms at position 16 and 17 with the five-membered ring D and being &agr; with respect to said D-ring. In addition, the carbon atom at position 17 is substituted with an oxygen atom-comprising group through a CO bond. The invention also relates to a pharmaceutical composition comprising said steroid compound. The steroid compounds of the present invention are very suitable for use in the prevention or treatment of peri-menopausal or menopausal complaints, more preferably the prevention or treatment of osteoporosis. Furthermore, the steroid compounds of the present invention can be used for contraceptive purposes.
摘要翻译：本发明涉及具有式（I）的类固醇化合物，其包含环E，所述环与16位和17位的碳原子具有五元环D并且相对于所述D环为α。此外，通过CO键将17位的碳原子被含氧原子的基团取代。本发明还涉及包含所述类固醇化合物的药物组合物。本发明的类固醇化合物非常适用于预防或治疗围绝经期或绝经期的投诉，更优选预防或治疗骨质疏松症。此外，本发明的类固醇化合物可用于避孕目的。

89. 发明授权

US5712264A 17-spiromethylene steroids 失效
公开(公告)号：US5712264A
公开(公告)日：1998-01-27
申请号：US98665
申请日：1993-07-28
申请人： Johannes Antonius Maria Hamersma , Everardus Otto Maria Orlemans , Johannes Bernardus Maria Rewinkel
发明人： Johannes Antonius Maria Hamersma , Everardus Otto Maria Orlemans , Johannes Bernardus Maria Rewinkel
IPC分类号： A61K31/58 , A01N43/80 , A61P5/24 , C07J5/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J43/00 , C07J51/00 , C07J53/00 , C07J63/00 , C07J71/00
CPC分类号： C07J51/00 , C07J21/00 , C07J21/006 , C07J31/006 , C07J41/0016 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J53/002 , C07J71/001 , C07J71/0015
摘要： The invention relates to a steroid derivative which steroidal skeleton is bound at carbon atom 17 to a spiromethylene ring of the formula: ##STR1## wherein R.sub.a and R.sub.b are independently selected from the group consisting of hydrogen, methyl, and halogen; m is 1 or 2; and the asterisk denotes carbon atom 2 of the spiromethylene ring which is carbon atom 17 (or carbon atom 17.alpha. of a homosteroid skeleton) of the steroid. The steroids have progestational or antiprogestational activity.

90. 发明授权

US5523298A Progestationally active 19,11-bridged 4-estrenes 失效
标题翻译：推荐活跃的19,11桥接4-雌激素
公开(公告)号：US5523298A
公开(公告)日：1996-06-04
申请号：US135486
申请日：1993-10-13
申请人： Eckhard Ottow , Wolfgang Schwede , Wolfgang Halfbrodt , Karl-Heinrich Fritzemeier , Rolf Krattenmacher
发明人： Eckhard Ottow , Wolfgang Schwede , Wolfgang Halfbrodt , Karl-Heinrich Fritzemeier , Rolf Krattenmacher
IPC分类号： A61K31/56 , A61K31/569 , A61K31/57 , A61K31/58 , A61K31/585 , A61P5/34 , A61P13/02 , A61P15/00 , A61P15/18 , C07J53/00
CPC分类号： C07J53/002
摘要： In this invention, the new etheno- and ethano-19,11-bridged 4-estrenes of general formula I ##STR1## are described, in which W, R.sup.1, R.sup.2, R.sup.6a, R.sup.6b, R.sup.7, R.sup.14, R.sup.15, R.sup.16, R.sup.11, R.sup.11' and R.sup.19 have the meaning indicated in the description, as well as a process for their production.The new compounds have strong progestational activity and are suitable for the production of pharmaceutical agents.
摘要翻译：在本发明中，描述了通式I（I）的新的乙烯 - 和乙酰基-19,11-桥接的4-雌酮，其中W，R 1，R 2，R 6a，R 6b，R 7，R 14，R 15， R16，R11，R11'和R19具有说明书中指出的含义，以及其制备方法。新化合物具有强烈的促孕活性，适用于制药。

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