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公开(公告)号：US4118396A
公开(公告)日：1978-10-03
申请号：US713901
申请日：1976-08-12
申请人： Giorgio Pifferi , Mario Pinza
发明人： Giorgio Pifferi , Mario Pinza
IPC分类号： C07D207/27 , A61K31/40 , A61K31/4015 , A61P25/00 , C07D207/12 , C07D207/26 , C07D207/273 , C07D207/277 , C07D207/38 , C07D207/28
CPC分类号： C07D207/273 , C07D207/38
摘要： Pyrrolidin-2-one derivatives of the formula: ##STR1## wherein R represents hydrogen, an acyl radical containing from 2 to 7 carbon atoms, a saturated or unsaturated alkyl, containing from 1 to 6 carbon atoms, aralkyl, cycloalkyl or aromatic, R.sub.1 and R.sub.2 may be the same or different and represent hydrogen, a saturated or unsaturated alkyl radical, containing from 1 to 3 carbon atoms, cycloalkyl radical or R.sub.1 and R.sub.2, together with the adjacent nitrogen atom, may form an heterocyclic ring optionally containing an additional heteroatom selected from the group consisting of oxygen and nitrogen, n represents an integer from 0 to 2 inclusive, and the process for their preparation are described.
摘要翻译： 吡咯烷-2-酮衍生物，其结构式如下：其中R表示氢，含有2至7个碳原子的酰基，含1至6个碳原子的饱和或不饱和烷基，芳烷基，环烷基或芳族，R1 并且R 2可以相同或不同，表示氢，含有1至3个碳原子的饱和或不饱和的烷基，环烷基或R 1和R 2与相邻的氮原子一起可以形成任选地含有另外的杂环 选自氧和氮的杂原子，n表示0〜2的整数，其制备方法进行说明。
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公开(公告)号：US3960858A
公开(公告)日：1976-06-01
申请号：US523789
申请日：1974-11-14
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。
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13.发明授权Derivatives of benzoyloxyacetic acid, and preparation and formulations thereof for therapeutic use 失效苯甲酰氧基乙酸的衍生物及其制备及其制剂用于治疗用途
公开(公告)号：US4879311A
公开(公告)日：1989-11-07
申请号：US222552
申请日：1988-07-21
申请人： Raffaello Giorgi , Marisa Conti , Giorgio Pifferi
发明人： Raffaello Giorgi , Marisa Conti , Giorgio Pifferi
IPC分类号： A61K31/245 , A61K31/24 , A61P25/04 , A61P29/00 , C07C67/00 , C07C227/00 , C07C227/18 , C07C229/58
CPC分类号： A61K31/24
摘要： Benzoyoxyacetic acid derivatives of formula (I) ##STR1## wherein M denotes hydrogen or one equivalent of a pharmaceutically acceptable inorganic or organic cation are useful as analgesics and anti-inflammatory agents. A novel process for their preparation is also disclosed along with novel intermediates.
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公开(公告)号：US4329285A
公开(公告)日：1982-05-11
申请号：US221365
申请日：1980-12-29
IPC分类号： C07D333/24 , C07D499/00 , C07D499/44 , C07D499/64 , C07D499/68 , C07D499/70
CPC分类号： C07C243/00 , C07D333/24 , C07D499/00
摘要： Formyl derivatives of hydrazinopenicillins of the formula ##STR1## wherein R is thienyl or phenyl, R' is hydrogen, formyl or alkyl containing from 1 to 3 carbon atoms and R" is hydrogen or formyl, provided that at least one of R' and R" is a formyl group, the carbon atom with the asterisk indicating a center of asymmetry of the molecule, and pharmaceutically acceptable salts and esters thereof, as mixture or as separated epimers. These compounds have antibacterial activity against Gram-negative and Gram-positive bacteria and are prepared by a process wherein the corresponding hydrazinopenicillin is reacted under anhydrous conditions with acetoformic anhydride to give the desired compounds.
摘要翻译： 其中R是噻吩基或苯基，R'是氢，甲酰基或含有1至3个碳原子的烷基，R“是氢或甲酰基，其中R'和R'中至少有一个是式 R“是甲酰基，具有星号的碳原子表示分子的不对称中心，以及其药学上可接受的盐和酯，作为混合物或分离的差向异构体。 这些化合物对革兰氏阴性和革兰氏阳性菌具有抗菌活性，并通过其中相应的肼青霉素在无水条件下与乙酰甲酸酐反应得到所需化合物的方法制备。
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公开(公告)号：US4324788A
公开(公告)日：1982-04-13
申请号：US142457
申请日：1980-04-21
IPC分类号： A61K31/50 , A61P9/08 , A61P9/12 , C07D237/22 , C07D405/12
CPC分类号： C07D237/22
摘要： There are described new alkoxyalkylidenhydrazinopyridazines having antihypertensive activity having the formula: ##STR1## wherein R is alkyl or cycloalkyl having up to 5 carbon atoms, optionally substituted with unsubstituted phenyl, substituted phenyl or cycloalkyl, R.sub.1 is hydrogen or alkyl having 1 to 3 carbon atoms and R.sub.2 is alkyl having 1 to 3 carbon atoms, a carboxylic group or phenyl and the process for their preparation.
摘要翻译： 描述了具有抗高血压活性的新型烷氧基亚乙基肼哒嗪，具有下式：其中R是具有至多5个碳原子的烷基或环烷基，任选被未取代的苯基，取代的苯基或环烷基取代，R 1是氢或具有1至3个碳原子的烷基 并且R 2是具有1至3个碳原子的烷基，羧基或苯基及其制备方法。
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公开(公告)号：US4231927A
公开(公告)日：1980-11-04
申请号：US913325
申请日：1978-06-07
IPC分类号： C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70
CPC分类号： C07D499/00 , C07C251/72
摘要： Hydrazono penicillin derivatives of the formula ##STR1## wherein R represents phenyl optionally substituted, 2- or 3- thienyl optionally substituted, or 2- or 3-furyl optionally substituted, R.sub.1 represents hydrogen, alkyl containing from 1 to 4 carbon atoms, or phenyl, and R.sub.2 represents hydrogen, pivaloyloxymethyl, or 1-(ethoxycarbonyloxy)ethyl radical. The compounds have antibacterial activity against gram-negative and gram-positive microorganisms. Methods of preparation are also disclosed.
摘要翻译： 其中R表示任选取代的苯基，任选取代的2-或3-噻吩基，或任选取代的2-或3-呋喃基，R 1表示氢，含有1至4个碳原子的烷基或苯基 ，R2代表氢，新戊酰氧基甲基或1-（乙氧基羰氧基）乙基。 该化合物对革兰氏阴性和革兰氏阳性微生物具有抗菌活性。 还公开了制备方法。
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公开(公告)号：US4173648A
公开(公告)日：1979-11-06
申请号：US886145
申请日：1978-03-13
IPC分类号： A61K31/19 , A61K20060101 , A61K31/20 , A61K31/215 , A61K31/22 , A61K31/30 , A61K31/56 , A61P1/04 , C07C20060101 , C07C51/00 , C07C62/32 , C07C63/42 , C07C67/00 , C07C69/013 , C07C69/02 , C07C69/145 , C07C69/24 , C07C69/34 , C07C69/74 , C07J63/00 , C07C65/14
CPC分类号： C07C2102/10
摘要： 3.beta.-Hydroxy-18.beta.-olean-9-en-30-oic acids having anti-ulcer activity of the formula ##STR1## compositions containing the same and process for their preparation.
摘要翻译： 具有下式抗溃疡活性的ββ-羟基-18β-烯丙基-9-烯-30-酸：（I）含有该组合物的组合物及其制备方法。
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公开(公告)号：US4041048A
公开(公告)日：1977-08-09
申请号：US523790
申请日：1974-11-14
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。
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公开(公告)号：US4005082A
公开(公告)日：1977-01-25
申请号：US126357
申请日：1971-03-19
申请人： Giorgio Pifferi
发明人： Giorgio Pifferi
IPC分类号： C07D265/02 , C07D265/20
CPC分类号： C07D265/02
摘要： 4-Substituted-1H-2,3-benzoxazines with a chlorine atom linked to the benzene ring, and a process for their preparation, are described. The compounds are administered as sedative, hypnotic and tranquillizing agents.
摘要翻译： 描述了与苯环连接的氯原子的4-取代的1H-2,3-苯并恶嗪及其制备方法。 化合物作为镇静剂，催眠剂和镇静剂施用。
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公开(公告)号：US4002753A
公开(公告)日：1977-01-11
申请号：US613865
申请日：1975-09-16
申请人： Carlo Carpi , Luciano Dorigotti , Giorgio Pifferi
发明人： Carlo Carpi , Luciano Dorigotti , Giorgio Pifferi
IPC分类号： C07D237/20 , A61K31/50
CPC分类号： C07D237/20
摘要： 6-SUBSTITUTED 3-CARBETHOXYHYDRAZINOPYRIDAZINES OF THE GENERAL FORMULA: ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, represent a lower alkyl group containing from 1 to 6 carbon atoms, an allyl group, a 2-hydroxyethyl group or a 2-hydroxypropyl group, as well as the pharmaceutically acceptable salts thereof. Also a method of preparation. These compounds have anti-hypertensive activity.
摘要翻译： 通式（6）的6-取代的3-甲氧基乙酰基吡啶类化合物：其中R 1和R 2可以相同或不同，表示含有1-6个碳原子的低级烷基，烯丙基， 羟乙基或2-羟丙基，以及其药学上可接受的盐。 也是一种制备方法。 这些化合物具有抗高血压活性。
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