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1. 发明授权

US4888350A New acyl-1H-1,2,4-triazole derivatives 失效
标题翻译：新的酰基-1H-1,2,4-三唑衍生物
公开(公告)号：US4888350A
公开(公告)日：1989-12-19
申请号：US915119
申请日：1986-10-03
申请人： Amedeo Omodei-Sale' , Pietro Consonni , Giulio Galliani
发明人： Amedeo Omodei-Sale' , Pietro Consonni , Giulio Galliani
IPC分类号： C07D233/54 , C07D249/08
CPC分类号： C07D233/64 , C07D233/54 , C07D249/08
摘要： New acyl -1H-1,2,4-triazole derivatives of the formula ##STR1## wherein R may be located on one of the two adjacent nitrogen atoms and may represent hydrogen; a group R.sub.5 -CO wherein R.sub.5 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkenyl, (C.sub.2-4)alkynyl, phenyl, phenyl substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, benzyl, cinnamyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1 -C.sub.4)alkylamino, phenylamino, phenylamino wherein the phenyl ring may be substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylendioxy, halo(C.sub.1-4)alkyl, (C.sub.1-4)alkoxy and benzyloxy; a group R.sub.6 -SO.sub.2 wherein R.sub.6 may represent (C.sub.1-4)alkyl, phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy, or phenactyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluormethyl, phenyl, halo and dimethylamino;R.sub.2 may represent the group ##STR2## wherein R.sub.7 is hydrogen or methyl and R.sub.8 is a (C.sub.1-4)alkyl radical, the group R.sub.5.sup.--CO or the group R.sub.6.sup.-- SO.sub.2 in which R.sub.5 and R.sub.6 are defined as above, or R.sub.7 and R.sub.8 taken together may represent a further bond between the carbon and oxygen atom;R.sub.3 and R.sub.4 are independently selected from hydrogen, halo, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R.sub.1 and R.sub.4 taken together may also repesent a methylenedioxy group; with the provison that, when R represents hydrogen, R.sub.2 must be the group ##STR3## in which R.sub.8 must be the group R.sub.6.sup.--SO.sub.2 wherein R.sub.6 is as above defined; and salts therewith of pharmaceutically acceptable acids. The compounds possess antireproductive utility.
摘要翻译：式Ⅰ的新的酰基-1H-1,2,4-三唑衍生物，其中R可以位于两个相邻的氮原子之一上并且可以代表氢; 其中R 5选自（C 1-4）烷基，（C 2-4）烯基，（C 2-4）炔基，苯基，被一至三个独立地选自卤素，（C 1-4）烷基，（C 1-4）烷氧基，三氟甲基，氰基，硝基，氨基，二 - （C 1-4）烷基氨基，（C 2-4）酰氨基和亚甲二氧基，苄基，肉桂基，氨基，（C 1-4）烷基氨基，（C 1 -C 4）烷基氨基，苯基氨基，苯基氨基，其中苯环可以被一至三个独立地选自卤素，（C 1-4）烷基，（C 1-4）烷氧基，三氟甲基，氰基，硝基，氨基，二 - （C 1-4）烷基氨基，（C 2-4）酰氨基和甲基二氧基，卤代（C 1-4）烷基，（C 1-4）烷氧基和苄氧基; 基团R6-SO2，其中R6可以表示（C1-4）烷基，苯基，被选自（C1-4）烷基和（C1-4）烷氧基的基团取代的苯基或苯甲酰基; R 1选自氢，（C 1-4）烷基，（C 1-4）烷氧基，烯丙氧基，炔丙氧基，三氟甲基，苯基，卤素和二甲基氨基; R 2可以表示基团，其中R 7是氢或甲基，R 8是（C 1-4）烷基，R 5 -CO或其中R 5和R 6如上所定义的基团R 6 -SO 2，或R 7和一起可以代表碳和氧原子之间的另一个键; R 3和R 4独立地选自氢，卤素，（C 1-4）烷基和（C 1-4）烷氧基; R 1和R 4一起也可以代替亚甲二氧基; 当R表示氢时，R2必须是其中R8必须是R6-SO2的基团，其中R6如上所定义; 以及其与药学上可接受的酸的盐。该化合物具有抗生素效用。

2. 发明授权

US4774325A New 8-substituted nucleoside and purine derivatives, the process for the preparation thereof and the pharmaceutical compositions containing them 失效
标题翻译：新的8-取代的核苷和嘌呤衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4774325A
公开(公告)日：1988-09-27
申请号：US776472
申请日：1985-09-16
申请人： Silvano Casadio , Duccio Favara , Amedeo Omodei-Sale , Ezio Panto
发明人： Silvano Casadio , Duccio Favara , Amedeo Omodei-Sale , Ezio Panto
IPC分类号： C07D473/34 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61K31/708 , A61P3/06 , C07D303/22 , C07D309/12 , C07D473/16 , C07D473/18 , C07F9/6561 , C07H19/16 , C07H19/167 , C07H19/20
CPC分类号： C07D303/22 , C07D309/12 , C07D473/18 , C07H19/16 , C07H19/20
摘要： New 8-substituted nucleoside and purine derivatives of the general formula: ##STR1## wherein R represents an amino group or an hydroxy group possibly in the corresponding keto tautomeric form, R.sub.1 is hydrogen or an amino group, R.sub.2 is hydrogen or a .beta.-D-ribofuranosyl radical wherein the primary hydroxy group and/or the two secondary hydroxy groups may be derivatized, R.sub.3 is an optionally substituted aryl or monocyclic heteroaryl radical and, X is --O-- or --S--. The new compounds have antihyperlipaemic activity.
摘要翻译：新的8-取代的核苷和嘌呤衍生物，其通式如下：其中R表示氨基或可能具有相应的酮互变异构形式的羟基，R 1是氢或氨基，R 2是氢或β-D - 呋喃核糖基，其中伯羟基和/或两个仲羟基可以被衍生化，R 3是任选取代的芳基或单环杂芳基，并且X是-O-或-S-。新化合物具有抗高血脂活性。

3. 发明授权

US4576746A Novel .beta.-lactam acetic acid derivatives 失效
标题翻译：新型β-内酰胺乙酸衍生物
公开(公告)号：US4576746A
公开(公告)日：1986-03-18
申请号：US354572
申请日：1982-03-04
申请人： Duccio Favara , Amedeo Omodei-Sale' , Pietro Consonni
发明人： Duccio Favara , Amedeo Omodei-Sale' , Pietro Consonni
IPC分类号： C07D205/08 , C07D477/00 , C07D477/04 , C07D487/04
CPC分类号： C07D477/04 , C07C67/343 , C07D205/08
摘要： New .beta.-lactam acetic acid derivatives I ##STR1## wherein R represents alkyl, alkyl substituted with amino, protected amino, mono- or di-alkylamino, hydroxy, protected hydroxy or alkoxy, and alkenyl, and their salts are useful as intermediates for preparing 1-azabicyclo [3.2.0]hept-2-ene antibiotics II ##STR2## The process for preparing the .beta.-lactam acetic acid derivatives I as well as the overall process which starting from the acids I leads to the antibiotics II are also claimed.
摘要翻译：新的β-内酰胺乙酸衍生物I其中R代表烷基，被氨基，被保护的氨基，一或二 - 烷基氨基，羟基，被保护的羟基或烷氧基和烯基取代的烷基及其盐可用作制备1-氮杂双环[3.2.0]庚-2-烯抗生素II制备β-内酰胺乙酸衍生物I的方法以及从酸I引入抗生素II开始的总体方法是也声称。

4. 发明授权

US4459302A Acyl-1H-1,2,4-triazole derivatives 失效
公开(公告)号：US4459302A
公开(公告)日：1984-07-10
申请号：US87375
申请日：1979-10-23
申请人： Amedeo Omodei-Sale , Pietro Consonni , Giulio Galliani
发明人： Amedeo Omodei-Sale , Pietro Consonni , Giulio Galliani
IPC分类号： A61K31/41 , C07D233/54 , C07D249/08 , C07D249/12 , C07D405/04
CPC分类号： C07D233/64 , C07D233/54 , C07D249/08 , Y10S514/841
摘要： New acyl-1H-1,2,4-triazole derivatives of the formula ##STR1## wherein R may be located on one of the two adjacent nitrogen atoms and may represent hydrogen; a group R.sub.5 -CO wherein R.sub.5 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkenyl, (C.sub.2-4)alkynyl, phenyl, phenyl substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, benzyl, cinnamyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1 -C.sub.4)alkylamino, phenylamino, phenylamino wherein the phenyl ring may be substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, halo(C.sub.1-4)alkyl, (C.sub.1-4)alkoxy and benzyloxy;a group R.sub.6 -SO.sub.2 wherein R.sub.6 may represent (C.sub.1-4)alkyl, phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy, or phenacyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, halo and dimethylamino;R.sub.2 may represent a (C.sub.1-4)alkyl radical or the group ##STR2## wherein R.sub.7 is hydrogen or methyl and R.sub.8 is a (C.sub.1-4)alkyl radical, the group R.sub.5 -CO or the group R.sub.6 -SO.sub.2 in which R.sub.5 and R.sub.6 are defined as above, or R.sub.7 and R.sub.8 taken together may represent a further bond between the carbon and oxygen atom;R.sub.3 and R.sub.4 are independently selected from hydrogen, halo, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R.sub.1 and R.sub.4 taken together may also represent a methylenedioxy group; with the proviso that, when R represents hydrogen, R.sub.2 must be the group ##STR3## in which R.sub.8 must be the group R.sub.5 -CO or the group R.sub.6 -SO.sub.2 wherein R.sub.5 and R.sub.6 are as above defined;and salts therewith of pharmaceutically acceptable acids. The compounds possess antireproductive utility.

5. 发明授权

US4075341A 2-Substituted phenyl-5-triazols [5,1-a] isoquinoline compounds 失效
标题翻译： 2-取代的苯基-5-三唑类{8 5,1-a {9 {0异喹啉化合物
公开(公告)号：US4075341A
公开(公告)日：1978-02-21
申请号：US636330
申请日：1975-11-28
申请人： Amedeo Omodei-Sale , Pietro Consonni , Leonard Lerner
发明人： Amedeo Omodei-Sale , Pietro Consonni , Leonard Lerner
IPC分类号： C07D217/24 , C07D471/04 , A61K31/53
CPC分类号： C07D471/04 , C07D217/24
摘要： A new process for preparing s-triazolo[5,1-a]-isoquinoline derivatives of the formula ##STR1## wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--; R is selected from hydrogen, amino, lower alkylamino, di-lower alkylamino, acylamino, diacylamino, ureido, thioureido, carbethoxythioureido, benzoylthioureido, sulfhydryl, lower alkyl, trifluoromethyl, phenyl, substituted phenyl, pyridyl, methylpyridyl and dimethylpyridyl; and R.sub.1 and R.sub.2 each independently represents hydrogen or lower alkoxy; by condensation of a 2-amino-3,4-dihydro-1(2H)-isoquinolinone with an imidolyl, cyanamide, cyanic or thiocyanic derivative.New compounds of the formula I wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, R has the same meaning as above with the exclusion of hydrogen, methyl, phenyl, and trifluoromethyl, R.sub.1 and R.sub.2 have the same meaning as above, with the proviso that when A represents the group --CH.dbd.CH--, R cannot be tolyl or pyridyl.The new compounds and some of the intermediates of the process are active as antiinflammatories, CNS depressants and anti-fertility agents.
摘要翻译：一种制备式（I）的三唑并[5,1-a] - 异喹啉衍生物的新方法，其中A代表基团-CH 2 -CH 2 - 或-CH = CH-; R选自氢，氨基，低级烷基氨基，二低级烷基氨基，酰氨基，二酰基氨基，脲基，硫脲基，乙氧基硫代脲基，苯甲酰硫基脲基，巯基，低级烷基，三氟甲基，苯基，取代的苯基，吡啶基，甲基吡啶基和二甲基吡啶基。并且R 1和R 2各自独立地表示氢或低级烷氧基; 通过2-氨基-3,4-二氢-1（2H） - 异喹啉酮与亚氨基，氨基氰，氰基或硫氰酸衍生物的缩合。

6. 发明授权

US4340607A Antimicrobial 3H-naphtho[1,2-d]imidazoles 失效
标题翻译：抗微生物3H-萘并[1,2-d]咪唑
公开(公告)号：US4340607A
公开(公告)日：1982-07-20
申请号：US236468
申请日：1981-02-20
申请人： Emilio Toja , Amedeo Omodei-Sale , Domenica Selva
发明人： Emilio Toja , Amedeo Omodei-Sale , Domenica Selva
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61P25/04 , A61P29/00 , A61P31/04 , C07D235/02 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D405/02
CPC分类号： C07D235/02
摘要： 3H-naphtho[1,2-d]imidazole derivatives of formula ##STR1## wherein R stands for (C.sub.1-6)alkyl, (C.sub.3-6)alkenyl, (C.sub.3-6)alkynyl or (C.sub.3-7)cycloalkyl, R.sub.1 and R.sub.2, each independently may represent hydrogen, halogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkylthio, (C.sub.1-4)alkoxy or halo(C.sub.1-4)alkoxy, R.sub.3 and R.sub.4, each independently, represent hydrogen or (C.sub.1-4)alkoxy, R.sub.5 stands for hydrogen, (C.sub.1-4)alkyl, (C.sub.3-4)alkoxy, mono- and di-(C.sub.2-4)alkylamino, (C.sub.2-4)alkanoylamino, carboxymethoxy and [carbo(C.sub.1-4)alkoxy]methoxy and R.sub.6 is hydrogen or R.sub.4 and R.sub.6 taken together may represent a methylenedioxy radical with the proviso that when R.sub.5 is hydrogen at least one of R.sub.3 and R.sub.4 must be different from hydrogen, useful as antimicrobial agents.
摘要翻译：其中R代表（C 1-6）烷基，（C 3-6）烯基，（C 3-6）炔基或（C 3-7）环烷基，R 1 并且R 2各自独立地表示氢，卤素，（C 1-4）烷基，（C 1-4）烷硫基，（C 1-4）烷氧基或卤代（C 1-4）烷氧基，R 3和R 4各自独立地表示氢或（C 1-4）烷氧基，R5代表氢，（C1-4）烷基，（C3-4）烷氧基，单 - 和二 - （C2-4）烷基氨基，（C2-4）烷酰基氨基，羧甲氧基和[ C 1-4）烷氧基]甲氧基并且R 6是氢或R 4和R 6一起可以代表亚甲二氧基，条件是当R 5是氢时，R 3和R 4中的至少一个必须不同于氢，可用作抗微生物剂。

7. 发明授权

US4313950A Antireproductive tricyclic ortho-fused nitrogen containing compounds 失效
标题翻译：抗生素三环邻位稠合含氮化合物
公开(公告)号：US4313950A
公开(公告)日：1982-02-02
申请号：US230138
申请日：1981-01-30
申请人： Umberto Guzzi , Amedeo Omodei-Sale , Giulio Galliani
发明人： Umberto Guzzi , Amedeo Omodei-Sale , Giulio Galliani
IPC分类号： C07D217/24 , C07D223/16 , C07D471/04 , C07D487/04 , A61K31/47
CPC分类号： C07D223/16 , C07D217/24 , C07D471/04 , C07D487/04 , Y10S514/96
摘要： New tricyclic ortho-fused nitrogen containing compounds of the following formula: ##STR1## wherein R and R.sub.1 are independently selected from hydrogen, fluoro, chloro, bromo and (C.sub.1 -C.sub.4)alkoxy; A may be --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --(CH.sub.2).sub.3 --; X represents a nitrogen atom or the group CH; and salts therewith of pharmaceutically acceptable acids.The compounds possess an outstanding antireproductive utility.
摘要翻译：新的具有下式的三环邻 - 稠合氮化合物：其中R和R 1独立地选自氢，氟，氯，溴和（C 1 -C 4）烷氧基; A可以是-CH 2 - ， - CH 2 -CH 2 - ， - CH = CH - 或 - （CH 2）3 - ; X表示氮原子或基团CH; 以及其与药学上可接受的酸的盐。该化合物具有突出的抗生素效用。

8. 发明授权

US4275066A Antireproductive tricyclic ortho-fused nitrogen containing compounds 失效
标题翻译：抗生素三环邻位稠合含氮化合物
公开(公告)号：US4275066A
公开(公告)日：1981-06-23
申请号：US87371
申请日：1979-10-23
申请人： Umberto Guzzi , Amedeo Omodei-Sale' , Giulio Galliani
发明人： Umberto Guzzi , Amedeo Omodei-Sale' , Giulio Galliani
IPC分类号： A61K31/41 , A61K31/415 , A61K31/47 , A61K31/55 , A61P33/02 , C07D217/24 , C07D223/16 , C07D471/04 , C07D487/04
CPC分类号： C07D223/16 , C07D217/24 , C07D471/04 , C07D487/04 , Y10S514/96
摘要： New tricyclic ortho-fused nitrogen containing compounds of the following formula: ##STR1## wherein R and R.sub.1 are independently selected from hydrogen, fluoro, chloro, bromo and (C.sub.1 -C.sub.4)alkoxy; A may be --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- or --(CH.sub.2).sub.3 --; X represents a nitrogen atom or the group CH; and salts therewith of pharmaceutically acceptable acids.The compounds possess an outstanding antireproductive utility.
摘要翻译：新的具有下式的三环邻 - 稠合氮化合物：其中R和R 1独立地选自氢，氟，氯，溴和（C 1 -C 4）烷氧基; A可以是-CH 2 - ， - CH 2 -CH 2 - ， - CH = CH - 或 - （CH 2）3 - ; X表示氮原子或基团CH; 以及其与药学上可接受的酸的盐。该化合物具有突出的抗生素效用。

9. 再颁专利

USRE30456E 2-Substituted phenyl-s-triazolo[5,1-a] isoquinoline compounds 失效
标题翻译： 2-取代的苯基 - 三唑并[5,1-a]异喹啉化合物
公开(公告)号：USRE30456E
公开(公告)日：1980-12-23
申请号：US32205
申请日：1979-04-23
申请人： Amedeo Omodei-Sale , Pietro Consonni , Leonard Lerner
发明人： Amedeo Omodei-Sale , Pietro Consonni , Leonard Lerner
IPC分类号： A61K31/41 , A61K31/435 , A61K31/47 , A61P25/04 , A61P25/20 , A61P29/00 , C07D209/00 , C07D209/46 , C07D217/24 , C07D221/00 , C07D249/00 , C07D249/16 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D209/46 , C07D217/24
摘要： A new process for preparing s-triazolo[5,1-a]-isoquinoline derivatives of the formula ##STR1## wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--; R is selected from hydrogen, amino, lower alkylamino, di-lower alkylamino, acylamino, diacylamino, ureido, thioureido, carbethoxythioureido, benzoylthioureido, sulfhydryl, lower alkyl, trifluoromethyl, phenyl, substituted phenyl, pyridyl, methylpyridyl and dimethylpyridyl; and R.sub.1 and R.sub.2 each independently represents hydrogen or lower alkoxy, by condensation of a 2-amino-3,4-dihydro-1(2H)-isoquinolinone with an imidolyl, cyanamide, cyanic or thiocyanic derivative.New compounds of the formula I wherein A represents the group --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--, R has the same meaning as above with the exclusion of hydrogen, methyl, phenyl, and trifluoromethyl, R.sub.1 and R.sub.2 have the same meaning as above, with the proviso that when A represents the group --CH.dbd.CH--, R cannot be tolyl or pyridyl.The new compounds and some of the intermediates of the process are active as antiinflammatories, CNS depressants and anti-fertility agents.

10. 发明授权

US4535090A 3,5-Diphenyl-1H-1,2,4-triazoles pharmaceutical compositions and uses 失效
标题翻译： 3,5-二苯基-1H-1,2,4-三唑类药物组合物及用途
公开(公告)号：US4535090A
公开(公告)日：1985-08-13
申请号：US434451
申请日：1982-10-15
申请人： Giulio Galliani , Amedeo Omodei-Sale , Pietro Consonni , Alessandro Assandri
发明人： Giulio Galliani , Amedeo Omodei-Sale , Pietro Consonni , Alessandro Assandri
IPC分类号： A61K9/08 , A61K9/107 , A61K31/41 , A61P11/00 , C07C243/38 , C07D249/08 , C07D249/10 , C07D405/04 , C07D405/10
CPC分类号： C07D249/08 , C07C243/38 , C07D405/04 , Y10S514/843
摘要： 3,5-diphenyl-1H-1,2,4-triazoles with contragestational activity of the following formula ##STR1## wherein R may be located on one or the other of the two adjacent nitrogen atoms and may represent hydrogen or a group R.sub.5 CO-- wherein R.sub.5 is an aliphatic saturated or unsaturated hydrocarbyl containing from 1 to 20 carbon atoms, R.sub.1, R.sub.2 and R.sub.3, each independently are selected from hydrogen, lower alkyl and lower alkoxy or R.sub.2 and R.sub.3 together may represent a methylenedioxy group, and R.sub.4 is an aliphatic saturated or unsaturated hydrocarbyl group of from 1 to 20 carbons, with the proviso that when R is hydrogen or an R.sub.5 CO-- group wherein R.sub.5 contains 4 or less carbon atoms, R.sub.4 must contain 5 or more carbons.These compounds have proven to be highly effective in terminating pregnancy in several animal species after a single parenteral injection.
摘要翻译：具有下式的映射活性的3,5-二苯基-1H-1,2,4-三唑：其中R可以位于两个相邻氮原子的一个或另一个上，并且可以表示氢或基团R 5 CO- 其中R 5是含有1至20个碳原子的脂族饱和或不饱和烃基，R 1，R 2和R 3各自独立地选自氢，低级烷基和低级烷氧基，或者R 2和R 3一起可表示亚甲二氧基，并且R 4是具有1至20个碳原子的脂肪族饱和或不饱和烃基，条件是当R是氢或R5含有4个或更少碳原子的R5CO-基时，R4必须含有5个或更多个碳。已经证明这些化合物在单次肠胃外注射后在几种动物物种中终止妊娠是非常有效的。

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