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11. 发明授权

US4891367A 17.beta.-(cyclopropyloxy)androst-5-en-3.beta.-ol and related compounds useful as C.sub.17-20 lyase inhibitors 失效
标题翻译： 17β-（环丙氧基）雄甾-5-烯-3β-醇和可用作C17-20裂解酶抑制剂的相关化合物
公开(公告)号：US4891367A
公开(公告)日：1990-01-02
申请号：US41170
申请日：1987-04-22
申请人： Michael R. Angelastro , Thomas R. Blohm
发明人： Michael R. Angelastro , Thomas R. Blohm
IPC分类号： C12N9/88 , A61K31/565 , A61P13/02 , A61P15/00 , C07J1/00 , C07J31/00 , C07J51/00
CPC分类号： C07J1/0029 , C07J31/003 , C07J51/00
摘要： This invention is directed to 17.beta.-(cyclopropyloxy)androst-5-en-3.beta.-ol and related compounds and also to a method for using such compounds in the treatment of androgen-dependent disorders. The ethers are prepared by using the Simmons-Smith reaction and an appropriate vinyl ether.

12. 发明授权

US4126612A Substituted cycloalkyl lactamimides 失效
标题翻译：取代的环丙基乳糖
公开(公告)号：US4126612A
公开(公告)日：1978-11-21
申请号：US877664
申请日：1978-02-14
申请人： Johann M. Grisar , Thomas R. Blohm , Edward M. Roberts
发明人： Johann M. Grisar , Thomas R. Blohm , Edward M. Roberts
IPC分类号： C07D207/22 , C07D211/72 , C07D223/10 , C07D223/12 , C07D225/02
CPC分类号： C07D207/22 , C07D211/72 , C07D223/10 , C07D223/12 , C07D225/02 , Y10S514/822 , Y10S514/866 , Y10S514/869 , Y10S514/884
摘要： Compounds possessing hypoglycemic, hypotensive, anti-inflammatory, anticoagulant and diuretic activity are represented by compounds of the following formula ##STR1## wherein Y is thienyl, cycloalkyl of from 5 to 7 carbon atoms, phenyl or substituted phenyl in which case the substituents on the substituted phenyl are selected from halogen, such as fluorine, chlorine, bromine or iodine, lower alkyl of from 1 to 4 carbon atoms and lower alkoxy of from 1 to 4 carbon atoms; Z is hydrogen or hydroxy; R is hydrogen, lower alkyl of from 1 to 4 carbon atoms, phenyl or benzyl; R.sup.1 is hydrogen, lower alkyl of from 1 to 4 carbon atoms or halogen, such as chlorine, fluorine, bromine or iodine; m is from 3 to 6; and n is from 3 to 11. Pharmaceutical compositions of these compounds and their use are also disclosed.

13. 发明授权

US4966898A 4-substituted 17.beta.-(cyclopropylamino)androst-5-en-3.beta.-ol and related compounds useful as C.sub.17-20 lyase inhibitors 失效
标题翻译： 4-取代的17β-（环丙基氨基）雄甾-5-烯-3β-醇和可用作C17-20裂解酶抑制剂的相关化合物
公开(公告)号：US4966898A
公开(公告)日：1990-10-30
申请号：US394025
申请日：1989-08-15
申请人： Michael R. Angelastro , Thomas R. Blohm
发明人： Michael R. Angelastro , Thomas R. Blohm
IPC分类号： A61K31/13 , C07J41/00
CPC分类号： C07J41/0005
摘要： This invention is directed to 4-substituted 17.beta.-(cyclopropylamino)androst-5-en-3.beta.-ol and related compounds and also to a method for using such compounds in the treatment of androgen-dependent disorders. The compounds are prepared by the hydride reduction of an appropriate steroidal imine or enamine.

14. 发明授权

US4317817A Novel steroid 5.alpha.-reductase inhibitors 失效
标题翻译：新型类固醇5α-还原酶抑制剂
公开(公告)号：US4317817A
公开(公告)日：1982-03-02
申请号：US216112
申请日：1980-12-15
申请人： Thomas R. Blohm , Brian W. Metcalf
发明人： Thomas R. Blohm , Brian W. Metcalf
IPC分类号： C07J1/00 , C07J3/00 , C07J9/00 , C07J17/00 , C07J21/00 , C07J31/00 , C07J41/00 , C07J51/00 , A01N47/08 , A61K31/655
CPC分类号： C07J9/005 , C07J1/0011 , C07J17/00 , C07J21/00 , C07J3/00 , C07J3/005 , C07J31/006 , C07J41/0005 , C07J51/00 , C07J9/00
摘要： Compounds of the following general formula are testosterone 5.alpha.-reductase inhibitors rendering the compounds useful in the treatment of acne and oily skin and benign prostatic hypertrophy: ##STR1## wherein R is: .dbd.O, --OH, --OCO--alkyl C.sub.1-5, --COOH, --CH.sub.2 OH, --COO--alkyl C.sub.1-6, --COCH.sub.3, ##STR2##
摘要翻译：以下通式的化合物是睾酮5α-还原酶抑制剂，其使得化合物可用于治疗痤疮和油性皮肤和良性前列腺肥大：其中R为：= O，-OH，-OCO-烷基C1-5 ，-COOH，-CH 2 OH，-COO-烷基C 1-6，-COCH 3，＆lt; IMAGE＆gt; + TR＆lt; IMAGE＆gt;

15. 发明授权

US4187319A Substituted benzaldehyde hypolipidemic agents 失效
标题翻译：取代苯甲醛降血脂药
公开(公告)号：US4187319A
公开(公告)日：1980-02-05
申请号：US802853
申请日：1977-06-02
申请人： Thomas R. Blohm , J. Martin Grisar , Roger A. Parker
发明人： Thomas R. Blohm , J. Martin Grisar , Roger A. Parker
IPC分类号： A61K31/11 , C07C47/575 , C07C47/48
CPC分类号： C07C323/00 , A61K31/11 , C07C45/41
摘要： Substituted benzaldehydes of the following general structure are useful as hypolipidemic agents: ##STR1## wherein Y is selected from oxygen and divalent sulfur; R is selected from a straight or branched saturated hydrocarbon chain having from 10 to 20 carbon atoms and a straight or branched unsaturated hydrocarbon chain having from 10 to 20 carbon atoms and from 1 to 4 double bonds.
摘要翻译：具有以下通用结构的取代的苯甲醛可用作降血脂剂：其中Y选自氧和二价硫; R选自具有10至20个碳原子的直链或支链饱和烃链和具有10至20个碳原子和1至4个双键的直链或支链不饱和烃链。

16. 发明授权

US4126621A Substituted cycloalkyl lactamimides 失效
公开(公告)号：US4126621A
公开(公告)日：1978-11-21
申请号：US877652
申请日：1978-02-14
申请人： Johann M. Grisar , Thomas R. Blohm , Edward M. Roberts
发明人： Johann M. Grisar , Thomas R. Blohm , Edward M. Roberts
IPC分类号： C07D207/22 , C07D211/72 , C07D223/10 , C07D223/12 , C07D225/02 , A61K31/40 , A61K31/445 , A61K31/55 , C07D409/08
CPC分类号： C07D207/22 , C07D211/72 , C07D223/10 , C07D223/12 , C07D225/02 , Y10S514/822 , Y10S514/866 , Y10S514/869 , Y10S514/884
摘要： Compounds possessing hypoglycemic, hypotensive, antiinflammatory, anticoagulant and diuretic activity are represented by compounds of the following formula ##STR1## wherein Y is thienyl, cycloalkyl of from 5 to 7 carbon atoms, phenyl or substituted phenyl in which case the substituents on the substituted phenyl are selected from halogen, such as fluorine, chlorine, bromine or iodine, lower alkyl of from 1 to 4 carbon atoms and lower alkoxy of from 1 to 4 carbon atoms; Z is hydrogen or hydroxy; R is hydrogen, lower alkyl of from 1 to 4 carbon atoms, phenyl or benzyl; R.sup.1 is hydrogen, lower alkyl of from 1 to 4 carbon atoms or halogen, such as chlorine, fluorine, bromine or iodine; m is from 3 to 6; and n is from 3 to 11. Pharmaceutical compositions of these compounds and their use are also disclosed.

17. 发明授权

US4126613A Substituted cycloalkyl lactamimides 失效
公开(公告)号：US4126613A
公开(公告)日：1978-11-21
申请号：US386995
申请日：1973-08-09
申请人： Johann M. Grisar , Thomas R. Blohm , Edward M. Roberts
发明人： Johann M. Grisar , Thomas R. Blohm , Edward M. Roberts
IPC分类号： C07C17/26 , C07C45/28 , C07C45/68 , C07D211/72 , C07D211/76 , C07D333/20 , C07D207/22 , C07D223/00 , C07D225/00
CPC分类号： C07C17/263 , C07C17/2632 , C07C45/28 , C07C45/68 , C07D211/72 , C07D211/76 , C07D333/20 , Y10S514/822 , Y10S514/866 , Y10S514/869
摘要： Compounds possessing hypoglycemic, hypotensive, anti-inflammatory, anticoagulant and diuretic activity are represented by compounds of the following formula ##STR1## where Y is thienyl, cycloalkyl of from 5 to 7 carbon atoms, phenyl or substituted phenyl in which case the substituents on the substituted phenyl are selected from halogen, such as fluorine, chlorine, bromine or iodine, lower alkyl of from 1 to 4 carbon atoms and lower alkoxy of from 1 to 4 carbon atoms; Z is hydrogen or hydroxy; R is hydrogen, lower alkyl of from 1 to 4 carbon atoms, phenyl or benzyl; R.sup.1 is hydrogen, lower alkyl of from 1 to 4 carbon atoms or halogen, such as chlorine, fluorine, bromine or iodine; m is from 3 to 6; and n is from 3 to 11. Pharmaceutical compositions of these compounds and their use are also disclosed.

18. 发明授权

US4088760A Testosterone 5.alpha.-reductase inhibitors 失效
标题翻译：睾酮5 {60-还原酶抑制剂
公开(公告)号：US4088760A
公开(公告)日：1978-05-09
申请号：US698824
申请日：1976-06-23
申请人： Harvey D. Benson , Thomas R. Blohm
发明人： Harvey D. Benson , Thomas R. Blohm
IPC分类号： C07J9/00 , C07J21/00 , C07J31/00 , C07J41/00 , A61K31/56
CPC分类号： C07J9/00 , C07J21/006 , C07J31/006 , C07J41/0061 , C07J9/005
摘要： Compounds of the following general formula are testosterone 5.alpha.-reductase inhibitors rendering said compounds useful in the treatment of acne and oily skin: ##STR1## wherein n is an integer of from 0 to 4; R.sub.1 is --COOR.sub.2, --CONR.sub.3 R.sub.4, --CHO or --CH.sub.2 OR.sub.5 ; R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, or benzyl; each of R.sub.3 and R.sub.4 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms; and R.sub.5 is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 20 carbon atoms and is straight or branched, benzoyl, phenylalkylcarbonyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched, or cycloalkylcarbonyl wherein the cycloalkyl moiety has from 5 to 10 carbon atoms.
摘要翻译：以下通式的化合物是使所述化合物用于治疗痤疮和油性皮肤的睾酮5α-还原酶抑制剂：其中n为0至4的整数; R1是-COOR2，-CONR3R4，-CHO或-CH2OR5; R2是氢，1至4个碳原子的直链或支链低级烷基，或苄基; R 3和R 4各自为氢或具有1至4个碳原子的直链或支链低级烷基; 并且R 5是氢，烷基羰基，其中烷基部分具有1至20个碳原子，并且是直链或支链的苯甲酰基苯基烷基羰基，其中烷基部分具有1至6个碳原子并且是直链或支链或环烷基羰基，其中环烷基部分具有 5至10个碳原子。

19. 发明授权

US4066788A Substituted benzaldehyde hypolipidemic agents 失效
标题翻译：取代苯甲醛降血脂药
公开(公告)号：US4066788A
公开(公告)日：1978-01-03
申请号：US619304
申请日：1975-10-03
申请人： Thomas R. Blohm , J. Martin Grisar , Roger Alan Parker
发明人： Thomas R. Blohm , J. Martin Grisar , Roger Alan Parker
IPC分类号： A61K31/11 , C07C45/41 , C07C45/71 , C07C47/575
CPC分类号： C07C45/41 , A61K31/11 , C07C323/00 , C07C45/71 , C07C47/575
摘要： Substituted benzaldehydes of the following general structure are useful as hypolipidemic agents: ##STR1## wherein Y is selected from oxygen and divalent sulfur; R is selected from a straight or branched saturated hydrocarbon chain having from 10 to 20 carbon atoms and a straight or branched unsaturated hydrocarbon chain having from 10 to 20 carbon atoms and from 1 to 4 double bonds.
摘要翻译：具有以下通用结构的取代的苯甲醛可用作降血脂剂：其中Y选自氧和二价硫; R选自具有10至20个碳原子的直链或支链饱和烃链和具有10至20个碳原子和1至4个双键的直链或支链不饱和烃链。

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