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1. 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。

2. 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。

3. 发明授权

US4409388A 1,2,4-Triazole derivatives, and their use as antifertility agents 失效
标题翻译： 1,2,4-三唑衍生物及其作为抗生育剂的用途
公开(公告)号：US4409388A
公开(公告)日：1983-10-11
申请号：US87376
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 , C07D249/08
CPC分类号： C07D249/08
摘要： Novel 1,2,4-triazole derivatives are described having the following formula ##STR1## wherein R represents hydrogen or methyl, R.sub.1 stands for hydrogen or (C.sub.1 -C.sub.4)alkyl, or R and R.sub.1 taken together may represent a further bond between the carbon atom and the oxygen atom, R.sub.2 and R.sub.4, each independently, represent hydrogen, chloro, fluoro, bromo, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, R.sub.3 stands for (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, chloro, fluoro, bromo or dimethylamino or R.sub.3 and R.sub.4 taken together may represent a methylenedioxy group.Also described is a process for their manufacture.Use of the novel compounds as antireproductive agents and pharmaceutical compositions containing them as active ingredients are also claimed.
摘要翻译：描述了具有下列结构式的新的1,2,4-三唑衍生物：其中R代表氢或甲基，R1代表氢或（C1-C4）烷基，或者R和R1一起代表在碳原子和氧原子，R2和R4各自独立地代表氢，氯，氟，溴，（C1-C4）烷基或（C1-C4）烷氧基，R3代表（C1-C4）烷基，（C1- C4）烷氧基，烯丙氧基，炔丙氧基，三氟甲基，苯基，氯，氟，溴或二甲基氨基或R3和R4一起表示亚甲二氧基。还描述了其制造方法。还要求保护使用新化合物作为抗生素剂和含有它们作为活性成分的药物组合物。

4. 发明授权

US4370337A 1,2,4-Triazole derivatives as antifertility agents and pharmaceutical compositions containing them 失效
标题翻译： 1,2,4-三唑衍生物作为抗生育剂和含有它们的药物组合物
公开(公告)号：US4370337A
公开(公告)日：1983-01-25
申请号：US283715
申请日：1980-07-16
申请人： Amedeo Omodei-Sale' , Pietro Consonni , Giulio Galliani
发明人： Amedeo Omodei-Sale' , Pietro Consonni , Giulio Galliani
IPC分类号： C07D249/08 , A61K31/41
CPC分类号： C07D249/08
摘要： Novel 1,2,4-triazole derivatives are described having the following formula ##STR1## wherein R represents hydrogen or methyl, R.sub.1 stands for hydrogen or (C.sub.1 -C.sub.4)alkyl, or R and R.sub.1 taken together may represent a further bond between the carbon atom and the oxygen atom, R.sub.2 and R.sub.4, each independently, represent hydrogen, chloro, fluoro, bromo, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy, R.sub.3 stands for (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, chloro, fluoro, bromo or dimethylamino or R.sub.3 and R.sub.4 taken together may represent a methylenedioxy group.Also described is a process for their manufacture. Use of the novel compounds as antireproductive agents and pharmaceutical compositions containing them as active ingredient are also claimed.
摘要翻译：描述了具有下列结构式的新的1,2,4-三唑衍生物：其中R代表氢或甲基，R1代表氢或（C1-C4）烷基，或者R和R1一起代表在碳原子和氧原子，R2和R4各自独立地代表氢，氯，氟，溴，（C1-C4）烷基或（C1-C4）烷氧基，R3代表（C1-C4）烷基，（C1- C4）烷氧基，烯丙氧基，炔丙氧基，三氟甲基，苯基，氯，氟，溴或二甲基氨基或R3和R4一起表示亚甲二氧基。还描述了其制造方法。还要求保护使用新化合物作为抗再生剂和含有它们作为活性成分的药物组合物。

5. 发明授权

US4041048A 3,2-Benzoxazepine derivatives 失效
标题翻译： 3,2 - 苯并氧氮杂衍生物
公开(公告)号：US4041048A
公开(公告)日：1977-08-09
申请号：US523790
申请日：1974-11-14
申请人： Giorgio Pifferi , Amedeo Omodei-Sale' , Pietro Consonni
发明人： Giorgio Pifferi , Amedeo Omodei-Sale' , Pietro Consonni
IPC分类号： C07D267/04 , C07D267/14 , C07D267/02
CPC分类号： C07D267/14 , C07D267/04
摘要： 3,2-Benzoxazepines of the formula ##STR1## and their preparation. In formula (I), R respesents hydrogen or lower alkyl; R.sup.1 represents hydrogen, lower alkyl, lower alkenyl, hydroxy-lower alkyl, carbamyloxy-lower alkyl, acyl, amidino, carbamyl, mono- or di-substituted carbamyl; R.sup.2 may be in position 7 or 8 of the benzoxazepine ring and represents hydrogen, nitro, amino, acetamino or halo. The compounds are prepared by reacting 1,2,4,5-tetrahydro-3,2-benzoxazepine with a reactant which reacts with a secondary amino group to give substitution in the 2-position. The compounds have anti-inflammatory and central nervous system activity.
摘要翻译：式（I）的“3-苯并氧氮杂”＆lt; IMAGE＆gt;及其制备。在式（I）中，R表示氢或低级烷基; R 1表示氢，低级烷基，低级烯基，羟基 - 低级烷基，氨基甲酰氧基 - 低级烷基，酰基，脒基，氨基甲酰基，单或二取代的氨基甲酰基; R2可以位于苯并氧氮杂环的7或8位，代表氢，硝基，氨基，乙酰氨基或卤素。该化合物通过使1,2,4,5-四氢-3,3-苯并氧氮杂与与仲氨基反应以在2-位取代的反应物进行制备。该化合物具有抗炎和中枢神经系统活性。

6. 发明授权

US3960858A 3-Hetero acyl-2,3-benzoxazepines 失效
标题翻译： 3-杂酰基-2,3-苯并氧氮杂
公开(公告)号：US3960858A
公开(公告)日：1976-06-01
申请号：US523789
申请日：1974-11-14
申请人： Giorgio Pifferi , Amedeo Omodei-Sale' , Pietro Consonni
发明人： Giorgio Pifferi , Amedeo Omodei-Sale' , Pietro Consonni
IPC分类号： C07D267/04 , C07D413/06
CPC分类号： C07D267/04
摘要： A new class of 2,3-benzoxazepine compounds of the formula ##SPC1##In the formula, R is heterocyclic acyl or heterocyclic acetyl. The compounds have central nervous system and anti-inflammatory activity.
摘要翻译：一类新的2,3-苯并氧氮杂鏻化合物，式中R是杂环酰基或杂环乙酰基。该化合物具有中枢神经系统和抗炎活性。

7. 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。

8. 发明授权

US4435417A Antiinflammatory 3H-naphtho[1,2-d]imidazoles 失效
标题翻译：抗炎3H-萘并[1,2-d]咪唑
公开(公告)号：US4435417A
公开(公告)日：1984-03-06
申请号：US391653
申请日：1982-06-24
申请人： Emilio Toja , Amedeo Omodei-Sale' , Domenica Selva
发明人： Emilio Toja , Amedeo Omodei-Sale' , Domenica Selva
IPC分类号： C07D235/02 , A61K31/415 , C07D235/18
CPC分类号： C07D235/02 , Y10S514/825
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 stands for hydrogen, hydroxy, methoxy, ethoxy, or mono- or di-methylamino, and R.sub.4 represents hydrogen or (C.sub.1-4)alkyl.Also described and claimed are their use as antiinflammatory agents and the pharmaceutical compositions containing them.
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代表氢，羟基，甲氧基，乙氧基，或单 - 或二 - 甲基氨基，R 4表示氢或（C 1-4）烷基。还描述和要求保护它们用作抗炎剂和含有它们的药物组合物。

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