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![PROCESS FOR PREPARING 17&agr;-ACETOXY-11&bgr;-[4-N,N(DIMETHYLAMINO)PHENYL]-21-METHOXY-19-NORPREGNA-4,9-DIENE-3,20-DIONE, INTERMEDIATES USEFUL IN THE PROCESS , AND PROCESSES FOR PREPARING SUCH INTERMEDIATES](/abs-image/US/2004/07/27/US06768014B2/abs.jpg.150x150.jpg)
1.发明授权PROCESS FOR PREPARING 17&agr;-ACETOXY-11&bgr;-[4-N,N(DIMETHYLAMINO)PHENYL]-21-METHOXY-19-NORPREGNA-4,9-DIENE-3,20-DIONE, INTERMEDIATES USEFUL IN THE PROCESS , AND PROCESSES FOR PREPARING SUCH INTERMEDIATES 有权制备17α-乙酰氧基-11β-[4-N，N（二甲基氨基）苯基] -2-甲氧基-19-壬基-4,9-二烯-3,20-二酮的方法，该方法中有用的中间体和方法 准备这样的中间人公开(公告)号：US06768014B2
公开(公告)日：2004-07-27
申请号：US10169139
申请日：2002-06-27
IPC分类号： C07J500
CPC分类号： C07J53/00 , C07J7/0085 , C07J21/006 , C07J41/0083 , C07J71/001
摘要： A compound having general formula (I) 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： 具有通式（I）的化合物，其中R 1是选自-OCH 3，-SCH 3，-N（CH 3）2，-NHCH 3，-CHO，-COCH 3和-CHOHCH 3的成员; 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; 并且X是选自-O和-N-OR 5的成员，其中R 5是选自氢和烷基的成员。 除了提供式（I）化合物外，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：US06900193B1
公开(公告)日：2005-05-31
申请号：US09526855
申请日：2000-03-17
申请人： Hyun K. Kim , Richard P. Blye , Pemmaraju N. Rao , James W. Cessac , Carmie K. Acosta , Anne Marie Simmons
发明人： Hyun K. Kim , Richard P. Blye , Pemmaraju N. Rao , James W. Cessac , Carmie K. Acosta , Anne Marie Simmons
IPC分类号： C07J5/00 , C07J7/00 , C07J9/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J51/00 , C07J71/00 , A61K31/56 , A61K31/58 , C07J43/00
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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3.发明授权公开(公告)号：US08003629B2
公开(公告)日：2011-08-23
申请号：US12641172
申请日：2009-12-17
IPC分类号： A61K31/56
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，-SCH 3，-N（CH 3）2，-NHCH 3，-CHO，-COCH 3和-CHOHCH 3的成员; R2是选自卤素，烷基，酰基，羟基，烷氧基，酰氧基，碳酸烷基酯，环戊氧基，S-烷基和S-酰基的成员; R3是选自烷基，羟基，烷氧基和酰氧基的成员; R4是选自氢和烷基的成员; 并且X是选自由以下组成的组的成员：= O和= NO-OR 5，其中R 5是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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4.发明授权公开(公告)号：US06861415B2
公开(公告)日：2005-03-01
申请号：US09180132
申请日：1997-04-30
IPC分类号： A61K31/57 , A61K31/00 , A61P5/24 , C07J5/00 , C07J7/00 , C07J9/00 , C07J21/00 , C07J41/00 , C07J51/00 , C07J71/00 , A61K31/56
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，-SCH 3，-N（CH 3）2，-NHCH 3，-CHO，-COCH 3和-CHOHCH 3的成员; 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; 并且X是选自= O和= N-OR 5的成员，其中R 5是选自氢和烷基的成员。除了提供式I化合物外， 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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5.发明申请公开(公告)号：US20100113408A1
公开(公告)日：2010-05-06
申请号：US12641172
申请日：2009-12-17
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，-SCH 3，-N（CH 3）2，-NHCH 3，-CHO，-COCH 3和-CHOHCH 3的成员; R2是选自卤素，烷基，酰基，羟基，烷氧基，酰氧基，碳酸烷基酯，环戊氧基，S-烷基和S-酰基的成员; R3是选自烷基，羟基，烷氧基和酰氧基的成员; R4是选自氢和烷基的成员; 并且X是选自由以下组成的组的成员：= O和= NO-OR 5，其中R 5是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.发明授权Structural modification of 19-norprogesterone I: 17-α-substituted-11-β-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents 有权19-去甲孕酮I：17-α-取代-11-β-取代-4-芳基和21-取代的19-去甲孕酮二酮作为新的抗孕剂的结构修饰公开(公告)号：US08569276B2
公开(公告)日：2013-10-29
申请号：US11069817
申请日：2005-02-28
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, R2, R3, R4 and X are as defined by the present specification. 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.
摘要翻译： 本发明特别涉及具有以下通式的化合物：其中R1，R2，R3，R4和X如本说明书所定义。 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; 治疗脑膜瘤; 治疗子宫平滑肌瘤; 治疗子宫肌瘤; 抑制子宫内膜增生; 诱导宫颈成熟; 诱导劳动; 并用于避孕。
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7.发明授权公开(公告)号：US07759330B2
公开(公告)日：2010-07-20
申请号：US11500627
申请日：2006-08-07
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，-SCH 3，-N（CH 3）2，-NHCH 3，-CHO，-COCH 3和-CHOHCH 3的成员; R2是选自卤素，烷基，酰基，羟基，烷氧基，酰氧基，碳酸烷基酯，环戊氧基，S-烷基和S-酰基的成员; R3是选自烷基，羟基，烷氧基和酰氧基的成员; R4是选自氢和烷基的成员; 并且X是选自由以下组成的组的成员：= O和= NO-OR 5，其中R 5是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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8.发明授权公开(公告)号：US07087591B2
公开(公告)日：2006-08-08
申请号：US11065632
申请日：2005-02-23
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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公开(公告)号：US4379779A
公开(公告)日：1983-04-12
申请号：US191805
申请日：1980-09-29
CPC分类号： G01N33/743 , C07J1/0059 , Y10S436/804 , Y10S436/817 , Y10S436/822 , Y10S436/825 , Y10S530/807
摘要： A hapten is obtained by replacing the 3-hydroxy group of equilin with HO--CO--A--O-- wherein A is an alkylene of one to six carbon atoms. The hapten is conjugated with an immunological carrier to provide an immunogen, which in turn produces a specific antiserum to equilin. The antiserum is used in a radioimmunoassay for equilin.
摘要翻译： 通过用HO-CO-A-O-替代3-羟基的平衡而获得半抗原，其中A是1至6个碳原子的亚烷基。 半抗原与免疫载体缀合以提供免疫原，其又产生特异性抗血清以达到平衡。 抗血清用于放射免疫测定以获得平衡。
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公开(公告)号：US4379780A
公开(公告)日：1983-04-12
申请号：US191807
申请日：1980-09-29
申请人： Pemmaraju N. Rao
发明人： Pemmaraju N. Rao
CPC分类号： G01N33/743 , C07J1/007 , Y10S436/804 , Y10S436/817 , Y10S436/822 , Y10S436/823 , Y10S530/807
摘要： A hapten is obtained by replacing the 3-hydroxy group of 17 .alpha.-dihydroequilin with HO--CO--A--O-- wherein A is an alkylene of one to six carbon atoms. The hapten is conjugated with an immunological carrier to provide an immunogen, which in turn produces a specific antiserum to 17 .alpha.-dihydroequilin. The antiserum is used in a radioimmunoassay for 17 .alpha.-dihydroequilin.
摘要翻译： 通过将17α-二氢异构蛋白的3-羟基用HO-CO-A-O-代替，得到半抗原，其中A是1至6个碳原子的亚烷基。 半抗原与免疫载体缀合以提供免疫原，其反过来产生对17α-二氢异构体的特异性抗血清。 抗血清用于17α-二氢同功酶的放射免疫测定。
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