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    Method of controlling fertility in males with 20-substitute of steroids
    2.
    发明授权
    Method of controlling fertility in males with 20-substitute of steroids 失效
    用20替代类固醇控制男性生育能力的方法

    公开(公告)号：US5679668A

    公开(公告)日：1997-10-21

    申请号：US691667

    申请日：1996-08-02

    申请人： Armelle Bonfils ,  Daniel Philibert

    发明人： Armelle Bonfils ,  Daniel Philibert

    IPC分类号： A61K31/57 ,  A61K31/575 ,  A61P43/00 ,  C07J5/00 ,  C07J15/00 ,  C07J41/00 ,  A61K31/58 ,  A61K31/585

    CPC分类号： C07J41/0094 ,  C07J15/00 ,  C07J41/0072

    摘要： The invention is a method of controlling fertility in male warm-blooded animals by administering a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 12 carbon atoms and aralkyl of 7 to 15 carbon atoms or taken together form a saturated heterocycle of 5 to 6 ring members optionally having a second ring heteroatom selected from the group consisting of sulfur, oxygen and nitrogen, R.sub.3 is an .alpha.-alkyl of 1 to 8 carbon atoms, n is an integer from 2 to 15, R.sub.4 is alkyl of 1 to 12 carbon atoms, R.sub.5 is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and acyl of an organic carboxylic acid of up to 12 carbon atoms and the wavy lines indicate that the 17- and 20- asymmetrical centers are independent of the absolute R and S configurations and their non-toxic, pharmaceutically acceptable acid addition salts.

    摘要翻译： 本发明是通过给予式Ⅰ化合物来控制雄性温血动物的生殖力的方法，其中R1和R2分别选自1至12个碳原子的烷基和7至15个的芳烷基 碳原子或一起形成5至6个环成员的饱和杂环，任选具有选自硫，氧和氮的第二个环杂原子，R 3是1至8个碳原子的α-烷基，n是整数 2至15，R 4为1至12个碳原子的烷基，R 5选自氢，1至12个碳原子的烷基和至多12个碳原子的有机羧酸的酰基，波浪线表示 17和20-不对称中心独立于绝对的R和S构型及其无毒的药学上可接受的酸加成盐。

    Method of controlling male fertility
    3.
    发明授权
    Method of controlling male fertility 失效
    控制男性生殖力的方法

    公开(公告)号：US5672595A

    公开(公告)日：1997-09-30

    申请号：US570134

    申请日：1995-12-11

    申请人： Armelle Bonfils ,  Daniel Philibert

    发明人： Armelle Bonfils ,  Daniel Philibert

    IPC分类号： A61K31/38 ,  A61K31/56 ,  A61K31/565 ,  A61K31/57 ,  A61K31/58 ,  A61P13/02 ,  A61P15/00 ,  A61P15/16 ,  C07J41/00 ,  C07J43/00

    CPC分类号： A61K31/566 ,  A61K31/565 ,  A61K31/567 ,  A61K31/57 ,  A61K31/58

    摘要： A method of controlling male fertility in warm-blooded male animals comprising administering to male warm-blooded animals an amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are taken together with the nitrogen to form a saturated 5 to 6 ring heterocycle, optionally containing a second nitrogen or oxygen in the ring, R.sub.3 is .alpha.- or .beta.-methyl, n is an integer from 2 to 10, R.sub.4 and R.sub.5 together are .dbd.0 or R.sub.4 is selected from the group consisting of hydrogen, --OH and acyloxy of an organic carboxylic acid of up to 12 carbon atoms and R.sub.5 is selected from the group consisting of hydrogen, --OH, acyloxy of an organic carboxylic acid of up to 12 carbon atoms and alkyl, alkenyl and alkynyl of up to 8 carbon atoms, R.sub.6 and R.sub.7 together are .dbd.0 or are individually selected from the group consisting of hydrogen, --OH and acyloxy of an organic carboxylic acid of up to 12 carbon atoms or R.sub.5 and R.sub.6 form a double bond and R.sub.4 and R.sub.7 are hydrogen and their non-toxic, pharmaceutically, acceptable acid addition salts in an amount sufficient to control male fertility.

    摘要翻译： 一种在温血雄性动物中控制雄性生育力的方法，包括向雄性温血动物施用一定量的选自下组的化合物，其中R1和R2与氮一起 形成饱和的5至6环杂环，任选地在该环中含有第二个氮或氧，R3是α-或β-甲基，n是2至10的整数，R4和R5一起为0或选择R4 由最高达12个碳原子的有机羧酸的氢，-OH和酰氧基组成的组中选择，R5选自氢，-OH，至多12个碳原子的有机羧酸的酰氧基和烷基 至多8个碳原子的链烯基和炔基，R 6和R 7一起为0或者分别选自具有至多12个碳原子的有机羧酸的氢，-OH和酰氧基，或者R5和R6形成 双键，R4和R7是氢 基因及其无毒的，药学上可接受的酸加成盐，其量足以控制雄性生育力。

    20-substituted steroids
    4.
    发明授权
    20-substituted steroids 失效
    20-取代的类固醇

    公开(公告)号：US06437157B1

    公开(公告)日：2002-08-20

    申请号：US08403276

    申请日：1995-03-13

    申请人： Armelle Bonfils ,  Daniel Philibert

    发明人： Armelle Bonfils ,  Daniel Philibert

    IPC分类号： C07J300

    CPC分类号： C07J41/0094 ,  C07J15/00 ,  C07J41/0072

    摘要： A compound selected from the group consisting of a compound of the formula wherein R1 and R2 are individually selected from the group consisting of alkyl of 1 to 12 carbon atoms and aralkyl of 7 to 15 carbon atoms or taken together form a saturated heterocycle of 5 to 6 ring members optionally having a second ring heteroatom selected from the group consisting of sulfur, oxygen and nitrogen, R3 is an &agr;-alkyl of 1 to 8 carbon atoms, n is an integer from 2 to 15, R4 is alkyl of 1 to 12 carbon atoms, R5 is selected from the group consisting of hydrogen, alkyl of 1 to 12 carbon atoms and acyl of an organic carboxylic acid of up to 12 carbon atoms and the wavy lines indicate that the 17- and 20-asymmetrical centers are independent of the absolute R and S configurations and their non-toxic, pharmaceutically acceptable acid addition salts useful for controlling fertility in male warm-blooded animals.

    摘要翻译： 选自由下列化合物组成的组的化合物，其中R 1和R 2的化合物分别选自1至12个碳原子的烷基和7至15个碳原子的芳烷基，或者一起形成5至6个饱和杂环 任选具有选自硫，氧和氮的第二环杂原子的环成员，R 3是1至8个碳原子的α-烷基，n是2至15的整数，R 4是1至12个碳的烷基 原子，R5选自氢，1至12个碳原子的烷基和至多12个碳原子的有机羧酸的酰基，波浪线表示17和20不对称中心独立于 绝对R和S构型及其无毒的药学上可接受的酸加成盐，用于控制雄性温血动物的生育力。

    Method of controlling male fertility
    5.
    发明授权
    Method of controlling male fertility 失效
    控制男性生殖力的方法

    公开(公告)号：US5635498A

    公开(公告)日：1997-06-03

    申请号：US570135

    申请日：1995-12-11

    申请人： Armelle Bonfils ,  Daniel Philibert

    发明人： Armelle Bonfils ,  Daniel Philibert

    IPC分类号： A61K31/38 ,  A61K31/56 ,  A61K31/565 ,  A61K31/57 ,  A61K31/58 ,  A61P13/02 ,  A61P15/00 ,  A61P15/16 ,  C07J41/00 ,  C07J43/00

    CPC分类号： A61K31/566 ,  A61K31/565 ,  A61K31/567 ,  A61K31/57 ,  A61K31/58

    摘要： A method of controlling male fertility in warm-blooded animals comprising administering to male warm-blooded animals an amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 8 carbon atoms and benzyl, R.sub.3 is .alpha.- or .beta.- methyl, n is an integer from 2 to 10, either R.sub.4 and R.sub.5 together are .dbd.O and R.sub.6 and R.sub.7 are hydrogen, or R.sub.6 and R.sub.7 together are .dbd.O and R.sub.4 and R.sub.3 are hydrogen or R.sub.4 and R.sub.7 are .dbd.O and R.sub.6 and R.sub.5 are .dbd.O and their non-toxic, pharmaceutically acceptable acid addition salts in an amount sufficient to control male fertility.

    摘要翻译： 一种在温血动物中控制雄性生育力的方法，包括向雄性温血动物施用一定量的选自下列化合物的化合物：其中R1和R2分别选自下组： 1至8个碳原子的烷基和苄基，R3是α-或β-甲基，n是2到10的整数，R4和R5一起是= O，R6和R7是氢，或R6和R7一起是 = O且R 4和R 3为氢或R 4和R 7为= O且R 6和R 5为= O，且其无毒的药学上可接受的酸加成盐的量足以控制雄性生育力。

    Method of controlling male fertility
    7.
    发明授权
    Method of controlling male fertility 失效
    控制男性生殖力的方法

    公开(公告)号：US5739124A

    公开(公告)日：1998-04-14

    申请号：US785203

    申请日：1997-01-17

    申请人： Armelle Bonfils ,  Daniel Philibert

    发明人： Armelle Bonfils ,  Daniel Philibert

    IPC分类号： A61K31/38 ,  A61K31/56 ,  A61K31/565 ,  A61K31/57 ,  A61K31/58 ,  A61P13/02 ,  A61P15/00 ,  A61P15/16 ,  C07J41/00 ,  C07J43/00 ,  A61K31/575

    CPC分类号： A61K31/566 ,  A61K31/565 ,  A61K31/567 ,  A61K31/57 ,  A61K31/58

    摘要： A method of controlling male fertility in warm-blooded animals comprising vaginally administering to female warm-blooded animals an amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 8 carbon atoms and benzyl or taken together with the nitrogen form a saturated 5 to 6 ring heterocycle optionally containing a second nitrogen or oxygen in the ring, R.sub.3 is .alpha.- or .beta.-methyl, n is an integer from 2 to 10; R.sub.4 and R.sub.5 together are =0 or R.sub.4 is selected from the group consisting of hydrogen, --OH and acyloxy of an organic carboxylic acid of up to 12 carbon atoms and R.sub.5 is selected from hydrogen, --OH, acyloxy of an organic acid of up to 12 carbon atoms and alkyl, alkenyl and, alkynyl of up to 8 carbon atoms, R.sub.6 and R.sub.7 together are =0 or are individually selected from the group consisting of hydrogen, --OH and acyloxy of an organic carboxylic acid of up to 12 carbon atoms or R.sub.5 and R.sub.6 form a double bond and R.sub.4 and R.sub.7 are hydrogen and their non-toxic, pharmaceutically acceptable acid addition salts in an amount sufficient to bind to the sigma receptor sites and inhibit the influx of calcium into the spermatozoid.

    摘要翻译： 一种在温血动物中控制雄性生育力的方法，其包括向女性温血动物施用一定量的选自下组的化合物的化合物，其中R1和R2分别选自下组 由1至8个碳原子的烷基和苄基或与氮一起形成饱和的5至6个环杂环，任选地在该环中含有第二个氮或氧，R3是α-或β-甲基，n是从 2至10; R4和R5一起为= 0或R4选自氢，-OH和至多12个碳原子的有机羧酸的酰氧基，R5选自氢，-OH，有机酸的上游的酰氧基 至12个碳原子，最多8个碳原子的烷基，烯基和炔基，R 6和R 7一起为0或者分别选自氢，-OH和最高达12碳的有机羧酸的酰氧基 原子或R 5和R 6形成双键，并且R 4和R 7是氢及其无毒的药学上可接受的酸加成盐，其量足以结合到σ受体位点并抑制钙向精子中的流入。

    Method of controlling male fertility
    8.
    发明授权
    Method of controlling male fertility 失效
    控制男性生殖力的方法

    公开(公告)号：US5580864A

    公开(公告)日：1996-12-03

    申请号：US616162

    申请日：1996-03-14

    申请人： Armelle Bonfils ,  Daniel Philibert

    发明人： Armelle Bonfils ,  Daniel Philibert

    IPC分类号： A61K31/38 ,  A61K31/56 ,  A61K31/565 ,  A61K31/57 ,  A61K31/58 ,  A61P13/02 ,  A61P15/00 ,  A61P15/16 ,  C07J41/00 ,  C07J43/00

    CPC分类号： A61K31/566 ,  A61K31/565 ,  A61K31/567 ,  A61K31/57 ,  A61K31/58

    摘要： A method of controlling male fertility in warm-blooded male animals comprising administering to male warm-blooded animals an amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 8 carbon atoms and benzyl, R.sub.3 is a .alpha.- or .beta.-methyl, n is an integer from 2 to 10, R.sub.4 is hydrogen, R.sub.5 is hydrogen, R.sub.6 and R.sub.7 are hydrogen, and their non-toxic, pharmaceutically acceptable acid addition salts in an amount sufficient to control male fertility.

    摘要翻译： 一种在温血雄性动物中控制雄性生育力的方法，包括向雄性温血动物施用一定量的选自下列化合物的化合物：其中R1和R2分别选自下组 由1-8个碳原子的烷基和苄基组成，R3是α-或β-甲基，n是2到10的整数，R4是氢，R5是氢，R6和R7是氢，它们是无毒的 ，足以控制雄性生育力的药学上可接受的酸加成盐。

    Method of controlling male fertility
    9.
    发明授权
    Method of controlling male fertility 失效
    控制男性生殖力的方法

    公开(公告)号：US5554604A

    公开(公告)日：1996-09-10

    申请号：US401078

    申请日：1995-03-08

    申请人： Armelle Bonfils ,  Daniel Philibert

    发明人： Armelle Bonfils ,  Daniel Philibert

    IPC分类号： A61K31/38 ,  A61K31/56 ,  A61K31/565 ,  A61K31/57 ,  A61K31/58 ,  A61P13/02 ,  A61P15/00 ,  A61P15/16 ,  C07J41/00 ,  C07J43/00 ,  A61K31/575

    CPC分类号： A61K31/566 ,  A61K31/565 ,  A61K31/567 ,  A61K31/57 ,  A61K31/58

    摘要： A method of controlling male fertility in warm-blooded male animals comprising administering to male warm-blooded animals an amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of alkyl of 1 to 8 carbon atoms and benzyl or taken together with the nitrogen form a saturated 5 to 6 ring heterocycle optionally containing a second nitrogen or oxygen in the ring, R.sub.3 is .alpha.- or .beta.- methyl, n is an integer from 2 to 10, R.sub.4 and R.sub.5 together are .dbd.0 or R.sub.4 is selected from the group consisting of hydrogen, --OH and acyloxy of an organic carboxylic acid of up to 12 carbon atoms and R.sub.5 is selected from the group consisting of hydrogen, --OH, acyloxy of an organic carboxylic acid of up to 12 carbon atoms and alkyl, alkenyl and alkynyl of up to 8 carbon atoms, R.sub.6 and R.sub.7 together are .dbd.0 or are individually selected from the group consisting of hydrogen, --OH and acyloxy of an organic carboxylic acid of up to 12 carbon atoms or R.sub.5 and R.sub.6 form a double bond and R.sub.4 and R.sub.7 are hydrogen and their non-toxic, pharmaceutically acceptable acid addition salts in an amount sufficient to control male fertility.

    摘要翻译： 一种在温血雄性动物中控制雄性生育力的方法，包括向雄性温血动物施用一定量的选自下列化合物的化合物：其中R1和R2分别选自下组 由1至8个碳原子的烷基和苄基或与氮一起形成饱和的5至6个环杂环，任选地在该环中含有第二个氮或氧，R3是α-或β-甲基，n是从 2至10，R 4和R 5一起为= 0或R 4选自具有至多12个碳原子的有机羧酸的氢，-OH和酰氧基，R 5选自氢，-OH 至多12个碳原子的有机羧酸的酰氧基和至多8个碳原子的烷基，烯基和炔基，R6和R7一起为0或者分别选自氢，-OH和酰氧基 有机碳 高达12个碳原子的二甲苯酸或R5和R6形成双键，R4和R7是氢，它们的无毒的药学上可接受的酸加成盐的量足以控制男性的生育力。