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1.发明授权Progestational 3-(6,6-ethylene-17B-hydroxy-3-oxo-17A-pregna-4-ene-17A-yl)propionic acid G-lactones 有权孕育3-（6,6-亚乙基-17β-羟基-3-氧代-17a-去甲-4-烯-177-基）丙酸G-内酯公开(公告)号：US08222237B2
公开(公告)日：2012-07-17
申请号：US12626398
申请日：2009-11-25
IPC分类号： A61K31/585 , C07J19/00
CPC分类号： C07J21/00 , A61K31/567 , A61K31/585 , A61K45/06 , C07D307/94 , A61K2300/00
摘要： Described herein are 3-(6,6-ethylene-17β-hydroxy-3-oxo-17α-pregna-4-ene-17α-yl)propionic acid γ-lactone derivatives having progestational and aldosterone antagonistic activity. Also described herein are methods of preparing and using these novel compounds.
摘要翻译： 本文描述了具有孕激素和醛固酮拮抗活性的3-（6,6-亚乙基-17β-二羟基-3-氧代-17α-前 - 4-烯-17α-基）丙酸γ-内酯衍生物。 本文还描述了制备和使用这些新化合物的方法。
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2.发明申请PROGESTATIONAL 3-(6,6-ETHYLENE-17B-HYDROXY-3-OXO-17A-PREGNA-4-ENE-17A-YL)PROPIONIC ACID G-LACTONES 有权丙酸3-（6,6-乙烯-17B-羟基-3-氧代-177-孕酮-4-烯-17A-YL）丙酸G-乳糖公开(公告)号：US20100137264A1
公开(公告)日：2010-06-03
申请号：US12626398
申请日：2009-11-25
IPC分类号： A61K31/585 , A61P15/18 , C07J21/00
CPC分类号： C07J21/00 , A61K31/567 , A61K31/585 , A61K45/06 , C07D307/94 , A61K2300/00
摘要： Described herein are 3-(6,6-ethylene-17β-hydroxy-3-oxo-17α-pregna-4-ene-17α-yl)propionic acid γ-lactone derivatives having progestational and aldosterone antagonistic activity. Also described herein are methods of preparing and using these novel compounds.
摘要翻译： 本文描述了具有孕激素和醛固酮拮抗活性的3-（6,6-亚乙基-17β-二羟基-3-氧代-17α-前 - 4-烯-17α-基）丙酸γ-内酯衍生物。 本文还描述了制备和使用这些新化合物的方法。
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3.发明申请公开(公告)号：US20060276443A1
公开(公告)日：2006-12-07
申请号：US11500627
申请日：2006-08-07
申请人： Hyun Kim , Richard Blye , Pemmaraju Rao , James Cessac , Carmie Acosta
发明人： Hyun Kim , Richard Blye , Pemmaraju Rao , James Cessac , Carmie Acosta
CPC分类号： C07J5/00 , C07J5/0053 , C07J7/00 , C07J7/0085 , C07J9/00 , C07J21/006 , C07J41/00 , C07J41/0016 , C07J41/0083 , C07J41/0094 , C07J51/00 , C07J71/001 , Y10S514/841
摘要： A compound having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —CHO, —COCH3 and —CHOHCH3; R2 is a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl; R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; IV is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ═O and ═N—OR5 , wherein R5 is a member selected from the group consisting of hydrogen and alkyl. In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce labor; and for contraception.
摘要翻译： 具有以下通式的化合物：其中：R 1是选自-OCH 3 3，-SCH 3 N， -N（CH 3）2，-NHCH 3，-CHO，-COCH 3，-CHOHCH 3， SUB> 3 R 2是选自卤素，烷基，酰基，羟基，烷氧基，酰氧基，碳酸烷基酯，Cypion氧基，S-烷基和S-酰基的成员; R 3是选自烷基，羟基，烷氧基和酰氧基的成员; IV是选自氢和烷基的成员; 且X为选自-O和-N-OR 5的基团，其中R 5为选自氢和烷基的成员。 除了提供式I化合物之外，本发明提供了其中式I化合物有利地用于拮抗内源性孕酮的方法; 诱发月经; 治疗子宫内膜异位症; 治疗痛经; 治疗内分泌激素依赖性肿瘤; 治疗子宫肌瘤; 抑制子宫内膜增生; 诱导劳动; 和避孕。
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公开(公告)号：US20050143365A1
公开(公告)日：2005-06-30
申请号：US11069817
申请日：2005-02-28
申请人： Hyun Kim , Richard Blye , Pemmaraju Rao , James Cessac , Carmie Acosta , Anne Simmons
发明人： Hyun Kim , Richard Blye , Pemmaraju Rao , James Cessac , Carmie Acosta , Anne Simmons
IPC分类号： C07J5/00 , C07J7/00 , C07J9/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J51/00 , C07J71/00 , A61K31/58
CPC分类号： C07J41/0083 , C07J5/00 , C07J5/0053 , C07J7/00 , C07J7/0045 , C07J7/0085 , C07J9/00 , C07J21/006 , C07J31/006 , C07J41/00 , C07J41/0016 , C07J41/0094 , C07J43/003 , C07J51/00 , C07J71/001 , Y10S514/841
摘要： The present invention relates, inter alia, to compounds having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —NC4H8, —NC5H10, —NC4H8O, —CHO, —CH(OH)CH3, —C(O)CH3, —O(CH2)2N(CH3)2, and —O(CH2)2NC5H10; R2 is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, —SCN, S-acyl and —OC(O)R6, wherein R6 is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., —CH2OCH3) and alkoxy (—OCH3); R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ═O and ═N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl. In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat meningiomas; to treat uterine leiomyomas; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce cervical ripening; to induce labor; and for contraception.
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5.发明申请公开(公告)号：US20050143364A1
公开(公告)日：2005-06-30
申请号：US11065632
申请日：2005-02-23
申请人： Hyun Kim , Richard Blye , Pemmaraju Rao , James Cessac , Carmie Acosta
发明人： Hyun Kim , Richard Blye , Pemmaraju Rao , James Cessac , Carmie Acosta
IPC分类号： A61K31/57 , A61K31/00 , A61P5/24 , C07J5/00 , C07J7/00 , C07J9/00 , C07J21/00 , C07J41/00 , C07J51/00 , C07J71/00 , A61K31/573 , C07J31/00
CPC分类号： C07J5/00 , C07J5/0053 , C07J7/00 , C07J7/0085 , C07J9/00 , C07J21/006 , C07J41/00 , C07J41/0016 , C07J41/0083 , C07J41/0094 , C07J51/00 , C07J71/001 , Y10S514/841
摘要： A compound having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —CHO, —COCH3 and —CHOHCH3; R2 is a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl; R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ═O and ═N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl. In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce labor; and for contraception.
摘要翻译： 具有以下通式的化合物：其中：R 1是选自-OCH 3 3，-SCH 3 N， -N（CH 3）2，-NHCH 3，-CHO，-COCH 3，-CHOHCH 3， SUB> 3 R 2是选自卤素，烷基，酰基，羟基，烷氧基，酰氧基，碳酸烷基酯，Cypion氧基，S-烷基和S-酰基的成员; R 3是选自烷基，羟基，烷氧基和酰氧基的成员; R 4是选自氢和烷基的成员; 且X为选自-O和-N-OR 5的基团，其中R 5为选自氢和烷基的成员。 除了提供式I化合物之外，本发明提供了其中式I化合物有利地用于拮抗内源性孕酮的方法; 诱发月经; 治疗子宫内膜异位症; 治疗痛经; 治疗内分泌激素依赖性肿瘤; 治疗子宫肌瘤; 抑制子宫内膜增生; 诱导劳动; 和避孕。
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6.发明申请Method for preparing 17 alpha-acetoxy-11beta-(4-n,n-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-dione, intermediates thereof, and methods for the preparation of such intermediates 审中-公开制备17α-乙酰氧基-11β-（4-n，n-二甲基氨基苯基）-19-去甲基-4,9-二烯-3,20-二酮的方法，其中间体及其制备方法公开(公告)号：US20060111577A1
公开(公告)日：2006-05-25
申请号：US10542580
申请日：2004-02-13
申请人： Hyun Kim , Pemmaraju Rao , Anne Simmons
发明人： Hyun Kim , Pemmaraju Rao , Anne Simmons
摘要： Methods for the preparation of the 19-norprogesterone of formula I and its intermediates, in crystalline and amorphous forms.
摘要翻译： 用于制备结晶和无定形形式的式I及其中间体的19-去甲孕酮的方法。
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