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1. 发明授权

US4634696A Novel 11 beta-substituted-19-nor-steroids 失效
标题翻译：新型11型β-取代-19-去甲甾类
公开(公告)号：US4634696A
公开(公告)日：1987-01-06
申请号：US760703
申请日：1985-07-30
申请人： Jean-Georges Teutsch , Vesperto Torelli , Roger Deraedt , Daniel Philibert
发明人： Jean-Georges Teutsch , Vesperto Torelli , Roger Deraedt , Daniel Philibert
IPC分类号： A61K31/565 , A61P5/38 , C07J1/00 , C07J21/00 , C07J41/00 , C07J43/00 , C07J71/00 , A61K31/56
CPC分类号： C07J1/0088 , C07J1/0059 , C07J1/007 , C07J21/006 , C07J41/0077 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J71/0063
摘要： Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated--bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms with at least one being other than hydrogen, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.a " are alkyl of 1 to 4 carbon atoms or taken together with the nitrogen atom form a heterocycle of 5 to 6 chain members optionally containing another heteroatom with the proviso that when A and B are ##STR4## R.sub.1 contains at least one nitrogen, phosphorus or silicium atom and when A and B are ##STR5## R.sub.1 is not a linear alkyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antigluococorticoid activity, their preparation and novel intermediates.
摘要翻译：式（I）的新型19-去甲甾类化合物，其中R 1是任选地含有至少一个杂原子的碳原子数为1至18的有机基团，紧邻11个碳原子的原子是碳，R2是1的烃至少8个碳原子，X是任选地被取代且任选地含有一个不饱和键的五边形或六边形环的剩余部分，A和B环选自由下列组成的组：（a）（c）＆lt; IMAGE＆gt;（d）和＆lt; IMAGE＆gt;（e）R'和R“分别选自氢，-CN和1至4个碳原子的烷基，其中至少一个是其它 R x选自氢和ORe，Re选自氢，任选取代的1至6个碳原子的烷基和酰基，R a可以在E或Z位置，如波浪线，并且选自和酰氧基，Ra'和Ra“是烷基 1至4个碳原子或与氮原子一起形成任选含有另一个杂原子的5至6个链成员的杂环，条件是当A和B为至少一个氮，磷或硅原子时， A和B是，R1不是直链烷基及其无毒的药学上可接受的酸加成盐，具有显着的抗皮质激素活性，其制备和新型中间体。

2. 发明授权

US5043332A Novel 11.beta.-substituted -19-nor-steriods 失效
标题翻译：新型11β-取代-19-去甲基异亮氨酸
公开(公告)号：US5043332A
公开(公告)日：1991-08-27
申请号：US421526
申请日：1989-10-13
申请人： Jean-Georges Teutsch , Vesperto Torelli , Roger Deraedt , Daniel Philibert , Germain Costerousse
发明人： Jean-Georges Teutsch , Vesperto Torelli , Roger Deraedt , Daniel Philibert , Germain Costerousse
IPC分类号： C07J1/00 , C07J7/00 , C07J21/00 , C07J41/00 , C07J43/00 , C07J51/00 , C07J63/00 , C07J71/00
CPC分类号： C07J41/0094 , C07J1/0059 , C07J1/007 , C07J1/0088 , C07J21/006 , C07J41/0016 , C07J41/0077 , C07J41/0083 , C07J43/003 , C07J51/00 , C07J63/008 , C07J7/0005 , C07J71/001 , C07J71/0063
摘要： Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated--bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R'.sub.a and R".sub.a are alkyl of 1 to 4 carbon atoms or taken together with the nitrogen atom form a heterocycle of 5 to 6 chain members optionally containing another heteroatom--with the proviso that when A and B are ##STR4## wherein R' and R" are both hydrogen, R.sub.1 contains at least one nitrogen, phosphorus or silicium atom and when A and B are ##STR5## R.sub.1 is not a linear alkyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antiglucocorticoid activity, their preparation and novel intermediates.
摘要翻译：式（I）的新型19-去甲甾类化合物，其中R 1是任选地含有至少一个杂原子的碳原子数为1至18的有机基团，紧邻11个碳原子的原子是碳，R2是1的烃至少8个碳原子，X是任选地被取代且任选地含有一个不饱和键的五边形或六边形环的剩余部分，A和B环选自由下列组成的组：（a）（c）图像（d）图像（e）R'和R“分别选自氢，-CN和1至4个碳原子的烷基，R x选自由氢和ORe组成，Re选自氢，任选取代的1至6个碳原子的烷基和酰基，Ra可以在如波形线所示的E或Z位置，并且选自的＆lt; IMAGE＆gt;和酰氧基，R'a和R'a是1〜4个碳原子的烷基或与n 氢原子形成任选含有另一个杂原子的5至6个链成员的杂环，条件是当A和B为其中R'和R“均为氢时，R 1包含至少一个氮，磷或硅原子当A和B是时，R1不是具有显着的抗糖皮质激素活性的直链烷基及其无毒的药学上可接受的酸加成盐，其制备和新的中间体。

3. 发明授权

US4978657A Novel 11.beta.-substituted-19-nor-steroids 失效
标题翻译：新型11β-取代-19-去甲类固醇
公开(公告)号：US4978657A
公开(公告)日：1990-12-18
申请号：US810316
申请日：1985-12-17
申请人： Jean-Georges Teutsch , Vesperto Torelli , Roger Deraedt , Daniel Philibert , Germain Costerousse
发明人： Jean-Georges Teutsch , Vesperto Torelli , Roger Deraedt , Daniel Philibert , Germain Costerousse
IPC分类号： C07J1/00 , C07J7/00 , C07J21/00 , C07J41/00 , C07J43/00 , C07J51/00 , C07J63/00 , C07J71/00
CPC分类号： C07J41/0094 , C07J1/0059 , C07J1/007 , C07J1/0088 , C07J21/006 , C07J41/0016 , C07J41/0077 , C07J41/0083 , C07J43/003 , C07J51/00 , C07J63/008 , C07J7/0005 , C07J71/001 , C07J71/0063
摘要： Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at leat one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e, R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.a " are alkyl of 1 to 4 carbon atoms or taken together with the nitrogen atom form a heterocycle of 5 to 6 chain members optionally containing another heteroatom with the proviso that when A and B are ##STR4## wherein R' and R" are both hydrogen, R.sub.1 contain at least one nitrogen, phosphorus or silicium atom and when A and B are ##STR5## R.sub.1 is not a linear alkyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antiglucocorticoid activity, their preparation and novel intermediates.
摘要翻译：式（Ⅰ）的新型19-去甲甾类化合物，其中R 1是1至18个碳原子的有机基团，其任选地含有一个杂原子与紧邻11个碳原子的原子是碳，R 2是1的烃至8个碳原子，X是任选地被取代且任选地含有一个不饱和键的五边形或六边形环的剩余部分，A和B环选自由下列组成的组： + TR R'和R“分别选自氢，-CN和1至4个碳原子的烷基，Rx选自氢和ORe，Re选自由以下组成的组：氢，任选取代的1至6个碳原子的烷基和酰基，Ra可以在如波形线所示的E或Z位置，并且选自由下列组成的组：酰氧基，Ra'和Ra“是具有1至4个碳原子的烷基或与氮原子一起形成任选地含有另一个杂原子的5至6个链成员的杂环，条件是当A和B是R 1和B均为氢时，R 1包含至少一个氮，磷或硅原子，当A和 B是不具有显着的抗糖皮质激素活性的线性烷基及其无毒的药学上可接受的酸加成盐，其制备方法和新的中间体。

4. 发明授权

US4547493A Novel 11.beta.-substituted-19-nor-steroids 失效
标题翻译：新型11β-取代-19-去甲类固醇
公开(公告)号：US4547493A
公开(公告)日：1985-10-15
申请号：US501373
申请日：1983-06-06
申请人： Jean-Georges Teutsch , Vesperto Torelli , Roger Deraedt , Daniel Philibert
发明人： Jean-Georges Teutsch , Vesperto Torelli , Roger Deraedt , Daniel Philibert
IPC分类号： A61K31/565 , A61P5/38 , C07J1/00 , C07J21/00 , C07J41/00 , C07J43/00 , C07J71/00 , A61K31/56
CPC分类号： C07J1/0088 , C07J1/0059 , C07J1/007 , C07J21/006 , C07J41/0077 , C07J41/0083 , C07J41/0094 , C07J43/003 , C07J71/0063
摘要： Novel 19-nor-steroids of the formula ##STR1## wherein R.sub.1 is an organic group of 1 to 18 carbon atoms optionally containing at least one heteroatom with the atom immediately adjacent the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is the remainder of a pentagonal or hexagonal ring optionally substituted and optionally containing one unsaturated bond, the A and B rings are selected from the group consisting of ##STR2## R' and R" are individually selected from the group consisting of hydrogen, --CN and alkyl of 1 to 4 carbon atoms with at least one being other than hydrogen, R.sub.x is selected from the group consisting of hydrogen and OR.sub.e R.sub.e is selected from the group consisting of hydrogen, optionally substituted alkyl of 1 to 6 carbon atoms and acyl, R.sub.a may be in the E or Z positions as indicated by the wavy line and is selected from the group consisting of ##STR3## and acyloxy, R.sub.a ' and R.sub.a " are alkyl of 1 to 4 carbon atoms or taken together with the nitrogen atom form a heterocycle of 5 to 6 chain members optionally containing another heteroatom with the proviso that when A and B are ##STR4## R.sub.1 contains at least one nitrogen, phosphorus or silicium atom and when A and B are ##STR5## R.sub.1 is not a linear alkyl and their non-toxic, pharmaceutically acceptable acid addition salts having a remarkable antigluococorticoid activity, their preparation and novel intermediates.
摘要翻译：式（I）的新型19-去甲甾类化合物，其中R 1是任选地含有至少一个杂原子的碳原子数为1至18的有机基团，紧邻11个碳原子的原子是碳，R2是1的烃至8个碳原子，X是任选地被取代且任选地含有一个不饱和键的五边形或六边形环的剩余部分，A和B环选自由下列组成的组：＆lt; IMAGE＆gt; + TR＆lt; IMAGE＆gt; R'和 R“分别选自氢，-CN和具有1至4个碳原子的烷基，其中至少一个不同于氢，Rx选自氢和ORe + L，Re选自由氢，任选取代的1至6个碳原子的烷基和酰基组成的组Ra可以在如波形线所示的E或Z位置，并且选自由下列组成的组：酰基氧基，R a'和 R a“为1至4个碳原子的烷基或被取代与氮原子一起形成任选含有另外杂原子的5至6个链成员的杂环，条件是当A和B为至少一个氮，磷或硅原子时，当A和B为 R1不是直链烷基及其无毒的药学上可接受的酸加成盐，具有显着的抗皮质激素活性，其制备和新型中间体。

5. 发明授权

US4753932A Novel 10-substituted steroids 失效
标题翻译：新型10-取代的类固醇
公开(公告)号：US4753932A
公开(公告)日：1988-06-28
申请号：US818884
申请日：1986-01-14
申请人： Jean-Georges Teutsch , Germain Costerousse , Vesperto Torelli , Daniel Philibert
发明人： Jean-Georges Teutsch , Germain Costerousse , Vesperto Torelli , Daniel Philibert
IPC分类号： A61K31/565 , A61K31/57 , A61K31/575 , A61K31/58 , A61P3/04 , A61P3/08 , A61P3/10 , A61P5/38 , A61P9/10 , A61P9/12 , A61P25/20 , A61P27/02 , A61P27/06 , A61P29/00 , A61P37/04 , A61P43/00 , C07J1/00 , C07J3/00 , C07J5/00 , C07J7/00 , C07J9/00 , C07J17/00 , C07J21/00 , C07J31/00 , C07J33/00 , C07J41/00 , C07J43/00 , C07J51/00 , H02J3/18 , A61K31/56
CPC分类号： C07J51/00 , C07J1/0081 , C07J1/0096 , C07J21/006 , C07J31/003 , C07J41/0083 , C07J41/0094 , C07J43/003
摘要： A novel steroid of the formula ##STR1## wherein X is methylene and R is an optionally substituted carbocyclic aryl or heterocyclic aryl or optionally substituted vinyl or ethynyl or X is a simple bond or --S-- and R is optionally substituted carbocyclic aryl or heterocyclic aryl, R.sub.2 is methyl or ethyl, R.sub.3 is selected from the group consisting of optionally substituted alkyl of 1 to 8 carbon atoms and optionally substituted alkenyl and alkynyl of 2 to 8 carbon atoms, R.sub.4 is selected from the group consisting of hydrogen and acyl, ##STR2## is selected from the group consisting of ##STR3## R.sub.6 is selected from the group consisting of hydrogen and methyl, the wavy line indicates .alpha. or .beta.- and the dotted line in 1(2) indicates the optional presence of a second carbon-carbon bond and novel process and intermediates therefore having anti-glucocorticoid activity.
摘要翻译：一种新颖的式I的类固醇，其中X是亚甲基，R是任选取代的碳环芳基或杂环芳基或任选取代的乙烯基或乙炔基或X是简单键或-S-，R是任选取代的碳环芳基或杂环芳基，R 2是甲基或乙基，R 3选自任选取代的1至8个碳原子的烷基和任选取代的2至8个碳原子的烯基和炔基，R 4选自氢和酰基，选自 R6选自氢和甲基，波浪线表示α或β - 而1（2）中的虚线表示任选存在第二碳碳键和新工艺和中间体因此具有抗糖皮质激素活性。

6. 发明授权

US4395408A Steroids 失效
标题翻译：新型类固醇
公开(公告)号：US4395408A
公开(公告)日：1983-07-26
申请号：US292794
申请日：1981-08-14
申请人： Vesperto Torelli , Roger Deraedt , Lucien Nedelec
发明人： Vesperto Torelli , Roger Deraedt , Lucien Nedelec
IPC分类号： A61K31/56 , A61K31/57 , A61P35/00 , A61P37/00 , A61P37/04 , C07J13/00 , C07J41/00 , C07J5/00 , A01N45/00 , C07C117/00
CPC分类号： C07J41/0027 , C07J13/007 , C07J41/0005 , Y10S514/885
摘要： Novel 3-amino-steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and methyl, W is selected from the group consisting of hydrogen and --OH and taken together with x forms ethylidene, X is selected from the group consisting of ethyl, ##STR2## and taken together with W forms ethylidene and the wavy lines signify that the substituents are in the .alpha. or .beta.-position with the proviso that when R.sub.1 is methyl and X is ethyl, ##STR3## W is --OH and their non-toxic, pharmaceutically acceptable acid addition salts and their preparation and intermediates therefore capable of stimulating immunitary activity.
摘要翻译：式（Ⅰ）的新型3-氨基类固醇，其中R 1选自氢和甲基，W选自氢和-OH，并与x一起形成亚乙基，X选自由乙基组成的基团与W一起形成亚乙基，波浪线表示取代基在α或β-位，条件是当R 1是甲基且X是乙基时，W是 -OH及其无毒的药学上可接受的酸加成盐及其制备和中间体因此能够刺激免疫活性。

7. 发明授权

US4424218A Novel 3 .alpha.-amino steroids 失效
标题翻译：新型3α-氨基类固醇
公开(公告)号：US4424218A
公开(公告)日：1984-01-03
申请号：US292791
申请日：1981-08-14
申请人： Roger Deraedt , Vesperto Torelli , Jean Vacher , Josette Benzoni
发明人： Roger Deraedt , Vesperto Torelli , Jean Vacher , Josette Benzoni
IPC分类号： C07J13/00 , C07J41/00 , C07J43/00 , A01N45/00
CPC分类号： C07J13/007 , C07J41/0005 , C07J41/0027 , C07J43/003 , Y10S514/885
摘要： A 3-amino-steroid of the formula ##STR1## wherein W is selected from the group consisting of hydrogen and --OH and taken together with X is ethylidene, X is selected from the group consisting of ethyl, ##STR2## the wavy line indicates the substituent has the .alpha.- and .beta.-position, R.sub.1 is selected from the group consisting of hydrogen and --CH.sub.3, R.sub.2 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and hydroxyalkyl of 2 to 5 carbon atoms, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, hydroxyalkyl of 2 to 5 carbon atoms, acyl of organic acid of 2 to 8 carbon atoms, alkoxycarbonyl of 2 to 8 carbon atoms, acyl of an .alpha.-amino-carboxylic acid and a peptide of 2 to 3 .alpha.-amino-carboxylic acids and their non-toxic, pharmaceutically acceptable acid addition acids with the proviso that R.sub.2 and R.sub.3 are not both hydrogen and (i) when R.sub.1 is methyl, W and R.sub.2 are hydrogen and X is ##STR3## in the case R.sub.3 is not methyl, acetyl or derived from an anminocarboxylic acid, (ii) when R.sub.1 is --CH.sub.3, W is hydrogen, R.sub.2 is --CH.sub.3 and X is ##STR4## in the case R.sub.3 is not methyl or acetyl, (iii) when R.sub.1 is methyl, R.sub.2 and W are hydrogen, X is ##STR5## with the --OH having the (S) configuration and the amino group is in the .alpha.-position in the case R.sub.3 is not methyl (iiii) R.sub.2 and W are hydrogen, X is ##STR6## and the 3-amino is in the .alpha.-position in the case at least one of R.sub.1, R.sub.2 and R.sub.3 is not methyl and (iiiii) R.sub.2 and W are hydrogen, R.sub.1 is methyl, X is ##STR7## with the --OH having the (R) configuration and the 3-amino is in the .alpha.-position in the case R.sub.3 is not ethoxycarbonyl capable of stimulating the defenses of an organism, especially by potentializing the production of IgE (immunoglobulins E) and their preparation.
摘要翻译：其中W选自氢和-OH并与X一起并与X一起形成的式（I）的3-氨基类固醇是亚乙基，X选自乙烯基，波浪线表示取代基具有α-和β-位，R 1选自氢和-CH 3，R 2选自氢，1至5个碳原子的烷基和2至5个碳原子的羟烷基 R 3选自氢，1至5个碳原子的烷基，2至5个碳原子的羟基烷基，2至8个碳原子的有机酸酰基，2至8个碳原子的烷氧基羰基， - 氨基 - 羧酸和2至3个α-氨基 - 羧酸的肽及其无毒的药学上可接受的酸加成酸，条件是R2和R3不同时为氢和（i）当R1为甲基时，W 在R 3不是甲基的情况下，R 2是氢并且X是，乙酰基或（ii）当R 1为-CH 3时，W为氢，R 2为-CH 3，X为不是甲基或乙酰基的情况下为X，（ⅲ）当R 1为甲基时，R 2和W为是氢，X是具有（S）构型的-OH，而在R3不是甲基的情况下氨基位于α位置（iiii），R2和W是氢，X是＆lt; IMAGE＆gt;和在R1，R2和R3中的至少一个不是甲基的情况下，3-氨基是α-位，并且（iiiii）R 2和W是氢，R 1是甲基，X是OH，其中-OH具有（R）构型，并且在R3不是能够刺激生物体的防御性的乙氧基羰基的情况下，特别是通过潜在地产生IgE（免疫球蛋白E）及其制备，3-氨基是α-位。

8. 发明授权

US4203981A Novel 17 .alpha.-aryl-steroids 失效
标题翻译：新型17α-芳基类固醇
公开(公告)号：US4203981A
公开(公告)日：1980-05-20
申请号：US692
申请日：1979-01-03
申请人： Andre Pierdet , Vesperto Torelli , Roger Deraedt
发明人： Andre Pierdet , Vesperto Torelli , Roger Deraedt
IPC分类号： A61K31/565 , A61K31/58 , A61P29/00 , C07J1/00 , C07J17/00 , C07J33/00 , C07J43/00 , C07J71/00 , A61K31/56
CPC分类号： C07J43/003 , C07J1/0011 , C07J1/0033 , C07J17/00 , C07J33/002 , C07J71/0015
摘要： Novel steroids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and acyl of an organic carboxylic acid of 1 to 18 carbon atoms, R.sub.2 is selected from the group consisting of optionally substituted aryl of 6 to 12 carbon atoms and optionally substituted heterocyclic selected from the group consisting of furyl, thienyl, pyridyl and pyrimidyl, the optional substituents being selected from the group consisting of hydroxy, alkyl and alkoxy of 1 to 4 carbon atoms, halogens and --CF.sub.3, the dotted line in the A ring indicates an optional .DELTA..sup.1(2) - double bond and A may be oxo and B is hydrogen or A is .DELTA.--OH and B is hydrogen or halogen or A and B form a .DELTA..sup.9(10) - double bond having very good anti-inflammatory activity and their preparation and novel intermediates.
摘要翻译：式（Ⅰ）的新型类固醇，其中R 1选自氢和1至18个碳原子的有机羧酸的酰基，R 2选自任选取代的6至12个碳原子的芳基和任选取代的杂环基，其选自呋喃基，噻吩基，吡啶基和嘧啶基，任选的取代基选自羟基，1至4个碳原子的烷基和烷氧基，卤素和-CF 3，环表示可选的DELTA 1（2） - 双键，A可以是氧代，B是氢或A是DELTA -OH，B是氢或卤素，或A和B形成具有非常特异的DELTA 9（10） - 双键良好的抗炎活性及其制备及新型中间体。

9. 发明授权

US4154730A Novel 17-spirosultines 失效
标题翻译：小说17-spirosultines
公开(公告)号：US4154730A
公开(公告)日：1979-05-15
申请号：US843962
申请日：1977-10-20
申请人： Vesperto Torelli , Daniel Philibert
发明人： Vesperto Torelli , Daniel Philibert
IPC分类号： A61K31/565 , A61K31/58 , A61P5/38 , C07J21/00 , C07J31/00 , C07J33/00 , C07J17/00
CPC分类号： C07J31/006 , C07J21/006 , C07J33/005 , Y10S514/899
摘要： Novel 17-spirosultines of steroids and the corresponding .gamma.-hydroxy acids of the formula ##STR1## wherein R.sub.1 is alkyl of 1 to 4 carbon atoms, A is hydrogen and B is hydrogen or hydroxyl of .beta.configuration or A and B together form a double bond, X and Y together form the group ##STR2## or X is --OH and Y is ##STR3## and M is selected from the group consisting of hydrogen, --NH.sub.4 and an alkali metal having a remarkable progestomimetic and antialdosteronic activity and a novel process for their preparation and novel intermediates.
摘要翻译：类固醇的新型17-螺旋体和相应的式（I）的γ-羟基酸，其中R 1是1至4个碳原子的烷基，A是氢，B是氢或β构型的羟基或A和B一起形成双键，X和Y一起形成基团，或X是-OH，Y是，M选自氢，-NH 4和具有显着的假动物模拟和反向递质活性的碱金属，和新型制备方法及新型中间体。

10. 发明授权

US4444767A Derivatives of 3-amino-pregn-5-ene 失效
标题翻译： 3-氨基妊娠-5-烯的衍生物
公开(公告)号：US4444767A
公开(公告)日：1984-04-24
申请号：US436524
申请日：1982-10-25
申请人： Vesperto Torelli , Josette Benzoni , Roger Deraedt
发明人： Vesperto Torelli , Josette Benzoni , Roger Deraedt
IPC分类号： A61K31/57 , A61P29/00 , A61P37/00 , C07J41/00 , A61K31/56
CPC分类号： C07J41/00
摘要： A compound selected from the group consisting of: 3-amino-.DELTA..sup.5 -pregnenes of the formula I: ##STR1## wherein X is selected from the group of ##STR2## the wavy lines indicate that the group may be in the .alpha.-or .beta.-position, R.sub.1 is selected from the group consisting of hydrogen and hydroxyalkyl or 2 to 5 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, hydroxyalkyl of 2 to 5 carbon atoms, acyl of an aliphatic carboxylic acid of 3 to 8 carbon atoms, alkoxycarbonyl of 2 to 8 carbon atoms, acyl of an .alpha.-amino-carboxylic acid or from a peptide of 2 to 3 amino acids of which amines may be either unsubstituted or mono-or disubstituted with alkyl of 1 to 5 carbon atoms with the proviso that R.sub.1 and R.sub.2 are not both hydrogen and that if the 3-amino group is in the .beta.-position, (i) when X is ##STR3## R.sub.1 and R.sub.2 are not both hydroxyethyl or (ii) when X is ##STR4## and R.sub.1 is hydrogen, R.sub.2 is not ethoxycarbonyl, the compound of the formula I wherein X is ##STR5## R.sub.1 is hydrogen and R.sub.2 is methyl, the 3-amino group is in the .alpha.-positionand their non-toxic, pharmaceutically acceptable acid addition salts which are useful as stimulants of the mammalian immune system.
摘要翻译：选自以下的化合物：式I的3-氨基-TATA 5-孕烯：其中X选自，波浪线表示该基团可以在 α-或β-位，R 1选自氢和羟基烷基或2至5个碳原子，R 2选自氢，2至5个碳原子的羟烷基，酰基的脂族羧酸的 2至8个碳原子的烷氧基羰基，2至8个碳原子的烷氧基羰基，α-氨基 - 羧酸的酰基或2至3个氨基酸的肽，其中胺可以是未取代的或被1至 5个碳原子，条件是R1和R2不同时为氢，如果3-氨基为β-位，则（i）当X为R 1和R 2不是羟乙基或（ii）当 X是，R 1是氢，R 2不是乙氧基羰基，其中X是R 1的式I化合物是h ydrogen和R2是甲基，3-氨基是α-位及其无毒的药学上可接受的酸加成盐，其可用作哺乳动物免疫系统的兴奋剂。

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