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1. 发明授权

US4119635A Substituted 1,2,4-triazole derivatives 失效
标题翻译：取代的1,2,4-三唑衍生物
公开(公告)号：US4119635A
公开(公告)日：1978-10-10
申请号：US720479
申请日：1976-09-03
申请人： Amedeo Omodei-Sale , Giorgio Pifferi , Pietro Consonni , Alberto Diena , Bonaccorso Rosselli del Turco
发明人： Amedeo Omodei-Sale , Giorgio Pifferi , Pietro Consonni , Alberto Diena , Bonaccorso Rosselli del Turco
IPC分类号： C07C243/38 , C07D249/08
CPC分类号： C07D249/08 , C07C243/38
摘要： New 1-alkyl-3,5-disubstituted-1,2,4-triazole derivatives of following formula I ##STR1## wherein R may represent phenyl; phenyl substituted by a radical selected from (C.sub.1-4)alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec.-butyl, isobutyl or tert.-butyl, (C.sub.1-4)alkoxy, e.g. methoxy, ethoxy, propoxy, butoxy, isobutyloxy or tert.-butoxy, fluoro, chloro, bromo, nitro, amino, cyano, carbamoyl, carboxy, hydroxymethyl, methylenedioxy and trifluoromethyl; dichlorophenyl; dimethoxyphenyl; 3,4,5-trimethoxyphenyl;R.sub.1 may represent phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl as above defined, (C.sub.1-4)alkoxy as above defined; fluoro, chloro, bromo, hydroxymethyl, (C.sub.2-4)aliphatic acyloxymethyl, e.g. acetoxymethyl, propionyloxymethyl or butyryloxymethyl, carbamoyloxymethyl, bromomethyl and dimethylaminomethyl; dimethylphenyl; dimethoxyphenyl; phenyl contemporaneously substituted by o-hydroxymethyl and chloro;R.sub.2 represents a (C.sub.1-4)alkyl group as above defined;With the proviso that R and R.sub.1 cannot simultaneously represent phenyl;With the further proviso that, when R is phenyl, R.sub.1 cannot be p-chlorophenyl;And processes for their preparation.The compounds of the invention have CNS depressant utility. They are especially useful as sedatives and hypnotics. Some of the compounds of the invention are also useful as anxiety relieving means.
摘要翻译：新的下式I的1-烷基-3,5-二取代-1,2,4-三唑衍生物其中R可以表示苯基; 被选自（C 1-4）烷基的基团取代的苯基，例如甲基，乙基，丙基，异丙基，丁基，仲丁基，异丁基或叔丁基，（C 1-4）烷氧基。甲氧基，乙氧基，丙氧基，丁氧基，异丁氧基或叔丁氧基，氟，氯，溴，硝基，氨基，氰基，氨基甲酰基，羧基，羟甲基，亚甲二氧基和三氟甲基; 二氯苯; 二甲氧基苯基; 3,4,5-三甲氧基苯基; R 1可以表示苯基，被选自上述定义的（C 1-4）烷基的基团取代的苯基，如上定义的（C 1-4）烷氧基; 氟，氯，溴，羟甲基，（C 2-4）脂族酰氧基甲基，乙酰氧基甲基，丙酰氧基甲基或丁酰氧基甲基，氨基甲酰氧基甲基，溴甲基和二甲基氨基甲基; 二甲基苯基; 二甲氧基苯基; 同时由邻羟甲基和氯取代的苯基; R2表示如上定义的（C 1-4）烷基; R和R1不能同时表示苯基; 另外，当R是苯基时，R 1不能是对氯苯基; 及其制备方法。

2. 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。

3. 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。

4. 发明授权

US4151169A Process for preparing substituted 1,2,4-triazole derivatives 失效
标题翻译：制备取代的1,2,4-三唑衍生物的方法
公开(公告)号：US4151169A
公开(公告)日：1979-04-24
申请号：US921911
申请日：1978-07-03
申请人： Amedeo O. Sale , Giorgio Pifferi , Pietro Consonni , Alberto Diena , Bonaccorso R. Del Turco
发明人： Amedeo O. Sale , Giorgio Pifferi , Pietro Consonni , Alberto Diena , Bonaccorso R. Del Turco
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： New 1-alkyl-3,5-disubstituted-1,2,4-triazole derivatives of following formula I ##STR1## wherein R may represent phenyl; phenyl substituted by a radical selected from (C.sub.1-4)alkyl, e.g. methyl, ethyl, propyl, isopropyl, butyl, sec.-butyl, isobutyl or tert.-butyl, (C.sub.1-4)alkoxy, e.g. methoxy, ethoxy, propoxy, butoxy, isobutyloxy or tert.-butoxy, fluoro, chloro, bromo, nitro, amino, cyano, carbamoyl, carboxy, hydroxymethyl, methylenedioxy and trifluoromethyl; dichlorophenyl; dimethoxyphenyl; 3,4,5-trimethoxyphenyl;R.sub.1 may represent phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl as above defined, (C.sub.1-4)alkoxy as above defined, fluoro, chloro, bromo, hydroxymethyl, (C.sub.2-4)aliphatic acyloxymethyl, e.g. acetoxymethyl, propionyloxymethyl or butyryloxymethyl, carbamoyloxymethyl, bromomethyl and dimethylaminomethyl; dimethylphenyl; dimethoxyphenyl; phenyl contemporaneously substituted by o-hydroxymethyl and chloro;R.sub.2 represents a (C.sub.1-4)alkyl group as above defined; with the proviso that R and R.sub.1 cannot simultaneously represent phenyl;With the further proviso that, when R is phenyl, R.sub.1 cannot be p-chlorophenyl; and processes for their preparation.The compound of the invention have CNS depressant utility. They are especially useful as sedatives and hypnotics. Some of the compounds of the invention are also useful as anxiety relieving means.
摘要翻译：新的下式I的1-烷基-3,5-二取代-1,2,4-三唑衍生物其中R可以表示苯基; 被选自（C 1-4）烷基的基团取代的苯基，例如甲基，乙基，丙基，异丙基，丁基，仲丁基，异丁基或叔丁基，（C 1-4）烷氧基。甲氧基，乙氧基，丙氧基，丁氧基，异丁氧基或叔丁氧基，氟，氯，溴，硝基，氨基，氰基，氨基甲酰基，羧基，羟甲基，亚甲二氧基和三氟甲基; 二氯苯; 二甲氧基苯基; 3,4,5-三甲氧基苯基; R 1可以表示苯基，被选自上述定义的（C 1-4）烷基的基团取代的苯基，如上所定义的（C 1-4）烷氧基，氟，氯，溴，羟甲基，（C 2-4）脂族酰氧基甲基，乙酰氧基甲基，丙酰氧基甲基或丁酰氧基甲基，氨基甲酰氧基甲基，溴甲基和二甲基氨基甲基; 二甲基苯基; 二甲氧基苯基; 同时由邻羟甲基和氯取代的苯基; R2表示如上定义的（C 1-4）烷基; 条件是R和R1不能同时表示苯基; 另外，当R是苯基时，R 1不能是对氯苯基; 及其制备方法。

5. 发明授权

US5549913A Multilayer matrix systems for the controlled release of active principles 失效
标题翻译：用于控制释放有源原理的多层矩阵系统
公开(公告)号：US5549913A
公开(公告)日：1996-08-27
申请号：US153437
申请日：1993-11-16
申请人： Paolo Colombo , Antonio C. Cardona , Giorgio Pifferi
发明人： Paolo Colombo , Antonio C. Cardona , Giorgio Pifferi
IPC分类号： A61J3/10 , A61K9/20 , A61K9/24 , A61K9/48 , A61K47/04 , A61K47/10 , A61K47/12 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/38 , A61K47/42
CPC分类号： A61K9/2086 , A61K9/209
摘要： This invention concerns systems for the release of active principles which are capable of releasing active principle(s) into an aqueous medium at a controlled rate.More precisely, the invention concerns a monolithic system for the controlled release of active principles, consisting of:a) at least one swelling layer containing one or more active principles, in a matrix of swellable, hydrophilic polymers;b) at least one erodible and/or soluble layer comprising excipients and/or water soluble polymers, possibly containing one or more active principles, either the same or different from those present in the layer a), the said erodible and/or soluble layer being in contact with the swelling layer(s) a).
摘要翻译：本发明涉及释放能够以受控速率将有效原理释放到水性介质中的活性原理的系统。更准确地说，本发明涉及用于控制释放活性成分的整体系统，其包括：a）在可溶胀亲水性聚合物基质中含有一种或多种活性成分的至少一种溶胀层; b）至少一个包含赋形剂和/或水溶性聚合物的可侵蚀和/或可溶性层，其可能含有一个或多个与层a）中存在的活性成分相同或不同的活性成分，所述可侵蚀和/或可溶层与膨胀层a）接触。

6. 发明授权

US5196449A Methods and pharmaceutical compositions for the treatment of ophthalmic diseases 失效
标题翻译：用于治疗眼底疾病的方法和药物组合物
公开(公告)号：US5196449A
公开(公告)日：1993-03-23
申请号：US557558
申请日：1990-06-24
申请人： Maria J. Magistretti , Marisa Conti , Giorgio Pifferi
发明人： Maria J. Magistretti , Marisa Conti , Giorgio Pifferi
IPC分类号： C07D311/62 , A61K31/00 , A61K31/35 , A61K31/352 , A61K31/353 , A61P9/00 , A61P9/14 , A61P27/00 , A61P27/02
CPC分类号： A61K31/35 , Y10S514/912
摘要： The anthocyanidins pelargonidin and delphidin, have been found to possess novel and unexpected activity in the ophthalmic field, specifically that they are active in reducing the permeability of ciliary body vessels. According to one aspect of the present invention there is provided a method of reducing the hyperpermeability of the ciliary body ocular vessels in a subject which comprises administering to the subject an effective dose of pelargonidin or delphidin. The invention further provides the use of pelargonidin or delphidin in the manufacture of pharmaceutical compositions for carrying out the method of treatment referred to above.

7. 发明授权

US3976673A 4-Cyclopropylmethyleneoxy-3-chlorophenylacetic acid and salts thereof 失效
标题翻译： 4-环丙基亚甲基氧基-3-氯苯基乙酸及其盐
公开(公告)号：US3976673A
公开(公告)日：1976-08-24
申请号：US539912
申请日：1975-01-09
申请人： Giorgio Pifferi
发明人： Giorgio Pifferi
IPC分类号： A61K31/19 , A61P25/04 , A61P29/00 , C07C51/00 , C07C59/64 , C07C59/72 , C07C65/00 , C07C67/00 , C07C63/52 , C07C87/14 , C07F1/08
CPC分类号： C07C59/72
摘要： The compound 4-cyclopropylmethyleneoxy-3-chlorophenylacetic acid and its non-toxic pharmaceutically acceptable salts have activity as anti-inflammatory, antipiretic and analgesic agents. It is prepared by reacting a lower alkyl ester of 3-chloro-4-hydroxyphenyl acetic acid with a cyclopropylmethylene halide and subsequently saponifying the ester obtained. The acid obtained is optionally salified to give corresponding non-toxic, inorganic or organic pharmaceutically acceptable salts.
摘要翻译：化合物4-环丙基亚甲基氧基-3-氯苯基乙酸及其无毒的药学上可接受的盐具有作为抗炎，止痒和止痛剂的活性。其通过使3-氯-4-羟基苯基乙酸的低级烷基酯与环丙基亚甲基卤反应并随后皂化所得的酯来制备。获得的酸任选盐化以产生相应的无毒，无机或有机的药学上可接受的盐。

8. 发明授权

US4886791A Soluble derivatives of silybin, a method of preparing them, and pharmaceutical compositions containing them 失效
标题翻译：水飞蓟宾的可溶性衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US4886791A
公开(公告)日：1989-12-12
申请号：US219058
申请日：1988-07-13
申请人： Raffaello Giorgi , Marisa Conti , Giorgio Pifferi
发明人： Raffaello Giorgi , Marisa Conti , Giorgio Pifferi
IPC分类号： A61K31/665 , A61P1/16 , A61P9/00 , A61P9/10 , A61P25/28 , A61P39/02 , C07F9/09 , C07F9/655 , C07F9/6558
CPC分类号： C07F9/65586
摘要： Novel water-soluble derivatives of silybin of enhanced activity are provided as well as methods of preparing the derivatives and pharmaceutical compositions containing them. The novel derivatives according to the invention have the following general formula (I); ##STR1## where: R=H or PO(OH).sub.2 and R'=PO(OH).sub.2 The compounds of the invention are useful inter alia in therapy of liver disorders and other applications where an anti-radical effect is required. They have the advantages of high hydrophilicity and are soluble at approximately pH 4, compared to prior art compounds which are water-soluble only at higher pH and enhanced stability.

9. 发明授权

US4173569A Preparation of pyrrolidine and pyrrolidin-2-one derivatives 失效
标题翻译：吡咯烷和吡咯烷-2-酮衍生物的制备
公开(公告)号：US4173569A
公开(公告)日：1979-11-06
申请号：US876169
申请日：1978-02-08
申请人： Silvano Banfi , Renato Pellegata , Giorgio Pifferi , Mario Pinza
发明人： Silvano Banfi , Renato Pellegata , Giorgio Pifferi , Mario Pinza
IPC分类号： A61K31/40 , A61K31/4015 , A61P25/00 , B43K24/08 , C07D207/26 , C07D207/273 , C09J115/00
CPC分类号： C07D207/273 , B43K24/084 , C09J115/00 , Y10S514/87
摘要： Preparation of compounds of the formula: ##STR1## wherein n is 1, 2 or 3, R.sub.1 and R.sub.2, which may be the same or different, are hydrogen or alkyl containing 1 to 3 carbon atoms and the asterisk indicates the center of asymmetry of the molecule, and compounds of the formula ##STR2## wherein R" is a saturated or unsaturated aliphatic hydrocarbon containing 1 to 6 carbon atoms, R.sub.3 is hydrogen or acyl containing 1 to 7 carbon atoms and the asterisk indicates the center of asymmetry of the molecule. The compounds produced by the present invention improve learning memory and display a protecting effect against the E.E.G. consequence of an overdose of barbiturates and against the reduced performance following brain damage (e.g. cerebral edema).
摘要翻译：下式化合物的制备：其中n为1,2或3，可以相同或不同的R 1和R 2为氢或含有1至3个碳原子的烷基，并且星号表示中心的化合物的分子的不对称性和式（Ia）的化合物，其中R“是含有1至6个碳原子的饱和或不饱和脂族烃，R 3是氢或含有1至7个碳原子的酰基，而星号表示分子的不对称中心。本发明生产的化合物改善了学习记忆并显示出对E.E.G.的保护作用。过量巴比妥类药物和脑损伤（例如脑水肿）后降低性能的后果。

10. 发明授权

US3998950A 7-.alpha.Hydrazinoacetamido derivatives of cephalosporanic 失效
标题翻译： 7- {60头孢菌素的肼基-N-乙酰氨基衍生物
公开(公告)号：US3998950A
公开(公告)日：1976-12-21
申请号：US563135
申请日：1975-03-28
申请人： Renato Broggi , Giuseppe Libassi , Giorgio Pifferi
发明人： Renato Broggi , Giuseppe Libassi , Giorgio Pifferi
IPC分类号： A61K20060101 , A61K31/545 , C07D20060101 , C07D205/08 , C07D213/04 , C07D279/06 , C07D333/04 , C07D501/06 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/26 , C07D501/32 , C07D501/34 , C07D501/38 , C07D501/42 , C07D501/60
CPC分类号： C07D501/20 , Y02P20/55
摘要： Derivatives of 7-aminocephalosporanic acid of the formula: ##STR1## wherein the carbon atom marked with an asterisk represents an asymmetry center of the molecule, A represents an aromatic nucleus, preferably phenyl which may be substituted by alkyl having 1-4 carbon atoms, halogen, hydroxy or alkoxy having 1-4 carbon atoms, or a heterocyclic nucleus, preferably 2- or 3-thiophene which may be, for example, substituted by halogen, R represents a hydrogen atom or a straight or branched chain lower alkyl radical, R.sub.1 represents a hydrogen atom, a hydroxy group, an acetoxy or pyridinium group. The invention includes the compounds as such or in the form of separated epimers as well as the corresponding pharmaceutically acceptable salts with alkali or alkaline-earth metals, with suitable organic bases or corresponding suitable organic or inorganic acid addition salts. Also method of preparing same. The compounds have powerful antibacterial action against gram-positive and gram-negative bacteria.
摘要翻译： 7-氨基头孢烷酸的衍生物，具有下式：其中标有星号的碳原子代表分子的不对称中心，A代表芳香核，优选苯基，其可被具有1-4个碳原子的烷基取代碳原子，卤素，羟基或具有1-4个碳原子的烷氧基，或杂环核，优选可以被卤素取代的2-或3-噻吩，R表示氢原子或直链或支链低级烷基，R 1表示氢原子，羟基，乙酰氧基或吡啶鎓基。本发明包括这样的化合物或分离的差向异构体的形式，以及与碱金属或碱土金属的相应的药学上可接受的盐，以及合适的有机碱或相应的合适的有机或无机酸加成盐。还有制备方法。这些化合物对革兰氏阳性和革兰氏阴性细菌具有强大的抗菌作用。

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