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1. 发明授权

US4683245A Laevorotatory antipode of moprolol as an antihypertensive 失效
标题翻译：作为抗高血压药的莫维洛的左旋对映体
公开(公告)号：US4683245A
公开(公告)日：1987-07-28
申请号：US434362
申请日：1982-10-14
申请人： Giorgio Ferrari , Vittorio Vecchietti
发明人： Giorgio Ferrari , Vittorio Vecchietti
IPC分类号： A61K31/13 , A61K20060101 , A61K31/05 , A61K31/135 , A61P25/02 , C07B31/00 , C07B57/00 , C07C39/06 , C07C67/00 , C07C213/00 , C07C217/34
CPC分类号： C07C237/34 , C07C213/10 , C07B2200/07
摘要： This invention relates to a process for the separation of moprolol into its two optical antipodes, substantially characterized by the fact of salifying racemic moprolol with L(+)glutamic acid; treating the thus obtained mixture of diastereoisomeric salts with a water/alcohol mixture, in this way separating the L(+)glutamate insoluble salt of (+)moprolol; treating the resultant mother liquors which contain in solution the L(+)glutamate salt of (-)moprolol with a base so as to separate the laevorotatory isomer of crystalline moprolol, which finally undergoes a purification. The invention also relates to a pharmaceutical composition containing said laevorotatoryisomer of moprolol.
摘要翻译：本发明涉及一种将莫莫洛分离成其两个光学对映体的方法，其基本特征在于用L（+）谷氨酸使外消旋莫糖醇成盐; 用水/醇混合物处理由此得到的非对映异构体盐的混合物，以这种方式分离（+）莫维洛尔的L（+）谷氨酸盐不溶性盐; 将含有（ - ）莫昔洛尔的L（+）谷氨酸盐的溶液中的所得母液处理得到的母液，以分离最后进行纯化的结晶莫莫洛的lavoorotative异构体。本发明还涉及含有莫莫洛尔的左旋异构体的药物组合物。

2. 发明授权

US4644004A Pyridynecarboxylic esters of dopamine and of its N-alkyl derivatives 失效
标题翻译：多巴胺及其N-烷基衍生物的吡啶并羧酸酯
公开(公告)号：US4644004A
公开(公告)日：1987-02-17
申请号：US699598
申请日：1985-02-08
申请人： Cesare Casagrande , Emilio Mussini , Vittorio Vecchietti
发明人： Cesare Casagrande , Emilio Mussini , Vittorio Vecchietti
IPC分类号： A61K31/4406 , A61K31/455 , A61P7/10 , A61P9/08 , A61P9/12 , A61P13/02 , A61P15/00 , C07D213/79 , C07D213/80 , C07D401/02 , A61K31/44
CPC分类号： C07D213/79 , C07D213/80
摘要： Pyridinecarboxylic esters of dopamine and of its N-alkyl derivatives, salts thereof with pharmaceutically acceptable organic or inorganic acids, process for preparing them and pharmaceutical compositions containing them which are particularly useful in the treatment of cardiovascular and renal disorders.
摘要翻译：多巴胺及其N-烷基衍生物的吡啶羧酸酯，其盐与药学上可接受的有机酸或无机酸，其制备方法和含有它们的药物组合物，其特别可用于治疗心血管和肾脏疾病。

3. 发明授权

US4362721A Penicillanic and cephalosporanic derivatives, preparation thereof, and pharmaceutical compositions containing same 失效
标题翻译：青霉烷和头孢菌素衍生物，其制备物和含有它们的药物组合物
公开(公告)号：US4362721A
公开(公告)日：1982-12-07
申请号：US327058
申请日：1981-12-03
申请人： Giorgio Ferrari , Vittorio Vecchietti
发明人： Giorgio Ferrari , Vittorio Vecchietti
IPC分类号： A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D499/00 , C07D499/68 , C07D501/22 , C07D519/06 , C07H13/12 , A61K31/70 , C07H15/26
CPC分类号： C07H13/12 , C07D499/00
摘要： There are disclosed penicillanic and cephalosporanic derivatives of the formula: ##STR1## wherein R is H or --OH; R.sub.1 is a carbohydrate hexose radical of 3-O-glucose, 6-O-galactose, 3-O-glucose acetals, 3-O-glucose ketals, 6-O-galactose acetals, and 6-O-galactose ketals, and R.sub.2 is: ##STR2## where R.sub.3 is H or an alkali or alkaline-earth metal. The preparation of the derivatives and pharmaceutical compositions containing same are also disclosed.A process according to the invention comprises reacting a compound of the formula ##STR3## with a hexose carbohydrate, in --OH protected form, in an aqueous medium, in the presence of a water-miscible organic solvent, in the presence of a base, the reaction product being optionally transformed into the derivative wherein R.sub.1 is a carbohydrate in the unprotected form by treatment with Lewis' acid or a hydrogen halide acid.The compounds according to the invention are used in pharmaceutical compositions useful for treatment of infections by gram-positive and gram-negative pathogenous bacteria.
摘要翻译：公开了下式的青霉素和头孢菌素衍生物：其中R是H或-OH;（I）其中R是H或-OH; R1是3-O-葡萄糖，6-O-半乳糖，3-O-葡萄糖缩醛，3-O-葡萄糖缩酮，6-O-半乳糖缩醛和6-O-半乳糖缩酮的碳水化合物己糖基，R2 是： + TR 其中R3是H或碱金属或碱土金属。还公开了含有它们的衍生物和药物组合物的制备。根据本发明的方法包括在水溶性有机溶剂的存在下，在碱的存在下，使式IMA的化合物与-OH保护形式的己糖碳水化合物在水性介质中反应，反应产物任选地转化为衍生物，其中R1是未保护形式的碳水化合物，用路易斯酸或卤化氢酸处理。根据本发明的化合物用于治疗革兰氏阳性和革兰氏阴性病原菌感染的药物组合物中。

4. 发明授权

US5441956A Hydroisoquinoline derivatives 失效
标题翻译：氢异喹啉衍生物
公开(公告)号：US5441956A
公开(公告)日：1995-08-15
申请号：US175371
申请日：1994-01-05
申请人： Vittorio Vecchietti , Giulio Dondio , Silvano Ronzoni , Roberto Colle
发明人： Vittorio Vecchietti , Giulio Dondio , Silvano Ronzoni , Roberto Colle
IPC分类号： A61K31/47 , A61K31/475 , A61P25/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D495/04 , A61K31/495
CPC分类号： C07D471/04 , C07D491/04 , C07D495/04
摘要： ##STR1## Compounds of formula (I) in which, R is linear or branched alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, aryl, aralkyl or furan-2-yl alkyl; R
1 and R
2 , which may be the same or different, are each hydrogen, hydroxy, alkoxy, or halogen; R
3 is hydrogen, hydroxy or alkoxy; "Het" is optionally substituted single or fused heteroxyclic ring, containing from 5 to 10 ring atoms and comprising up to four heteratoms in the or each ring, selected from oxygen, nitrogen and sulphur; R
4 and R
5 , which may be the same or different, are each hydrogen alkyl, halogen, nitro; CF, cyano, alkoxy carbonyl, NH, alkylcarbonylamino, hydroxy, alkoxy, or benzyl, are selective delta receptor agonists and are useful in the treatment of pain.
摘要翻译： PCT No.PCT / EP92 / 01483第 371日期1994年1月5日 102（e）日期1994年1月5日PCT提交1992年7月1日PCT公布。公开号WO93 / 01186 （I）其中R为直链或支链烷基，环烷基，环烷基烷基，烯基，芳基，芳烷基或呋喃-2-基烷基的式（I）化合物; R 1和R 2可以相同或不同，分别为氢，羟基，烷氧基或卤素; R3是氢，羟基或烷氧基; “Het”是任选取代的单或稠环氧环，其含有5至10个环原子，并且在该环或每个环中包含至多四个杂原子，选自氧，氮和硫; R 4和R 5可以相同或不同，分别为氢烷基，卤素，硝基; CF，氰基，烷氧基羰基，NH，烷基羰基氨基，羟基，烷氧基或苄基是选择性δ受体激动剂，可用于治疗疼痛。

5. 发明授权

US5254564A Substituted isoquinoline compounds, pharmaceutical composition and method of use in treating pain in mammals 失效
标题翻译：取代的异喹啉化合物，药物组合物和用于治疗哺乳动物疼痛的方法
公开(公告)号：US5254564A
公开(公告)日：1993-10-19
申请号：US553723
申请日：1990-07-16
申请人： Vittorio Vecchietti , Giuseppe Giardina , Roberto Colle
发明人： Vittorio Vecchietti , Giuseppe Giardina , Roberto Colle
IPC分类号： C07D217/06 , A61K31/47 , A61K31/472 , A61P7/10 , A61P9/00 , A61P9/10 , A61P25/04 , C07D217/14 , C07D221/16 , C07D221/20 , C07D217/26
CPC分类号： C07D221/20 , C07D217/14 , C07D221/16
摘要： A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, preferably methyl or ethyl, .sup.4 or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group;R.sub.4 and R.sub.5 are identical and are hydrogen or C.sub.1-6 alkyl, or together form a C.sub.2-5 linear polymethylene group; R.sub.6 and R.sub.7 are identical and are hydrogen or C.sub.1-6 alkyl, or together form a C.sub.2-5 linear polymethylene group;or R.sub.5 and R.sub.6 are together --CH.sub.2 -- when each of R.sub.4 and R.sub.7 is hydrogen or C.sub.1-6 alkyl;with the proviso that R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are not simultaneously hydrogen;R.sub.8 and R.sub.9, which may be the same or different, are each hydrogen, C.sub.1-6 alkyl, --CH.sub.2 OR.sub.10, halogen, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, thiol, C.sub.1-6 alkylthio, ##STR2## --NHCOR.sub.12, --NHSO.sub.2 R.sub.13, --CH.sub.2 SO.sub.2 NR.sub.14 R.sub.15, in which each of R.sub.10 to R.sub.15 is independently hydrogen, C.sub.1-6 alkyl, aryl or aralkyl, is useful for the treatment of pain, and or hyponatraemic disease states and/or cerebral ischaemia.

6. 发明授权

US4954509A Isoquinoline derivatives and their use as analgesics 失效
标题翻译：异喹啉衍生物及其用作镇痛药
公开(公告)号：US4954509A
公开(公告)日：1990-09-04
申请号：US312648
申请日：1989-02-17
申请人： Vittorio Vecchietti , Giuseppe Giardina
发明人： Vittorio Vecchietti , Giuseppe Giardina
IPC分类号： A61K31/47 , A61K31/472 , A61P25/04 , C07D217/14 , C07D409/06
CPC分类号： C07D409/06 , C07D217/14
摘要： A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring and R.sub.1 R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4 -12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.3 together with R.sub.1 forms a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 --, group; R.sub.4 and R.sub.5, which may be the same or different and may be attached to the same or different carbon atoms of the isoquinoline nucleus, are each hydrogen, halogen, hydroxy, C.sub.1-6 alkyl, aryl, or R.sub.4 together with R.sub.5 form a --(CH.sub.2).sub.p -- group, where p is an integer of from 1 to 5 and one or more of the --(CH.sub.2)-- moieties is optionally substituted by a C.sub.1-6 alkyl group.R.sub.6 and R.sub.6a, which may be the same or different, are each hydrogen, C.sub.1-6 alkyl, --CH.sub.2 OR.sub.6b, halogen, hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, thiol, C.sub.1-6 alkylthio, ##STR2## --NHCOR.sub.6d, --NHSO.sub.2 R.sub.6e, --CH.sub.2 SO.sub.2 NR.sub.6f R.sub.6g, in which each of R.sub.6b to R.sub.6g is independently hydrogen, C.sub.1-6 alkyl, aryl or aralkyl;with the proviso that R.sub.4, R.sub.5, R.sub.6 and R.sub.6a are not simultaneously hydrogen,is useful for the treatment of pain.

7. 发明授权

US4287211A Derivatives of phenylethylamines, processes for their preparation and related pharmaceutical compositions 失效
标题翻译：苯乙胺的衍生物，其制备方法和相关药物组合物
公开(公告)号：US4287211A
公开(公告)日：1981-09-01
申请号：US108157
申请日：1979-12-28
申请人： Giorgio Ferrari , Vittorio Vecchietti
发明人： Giorgio Ferrari , Vittorio Vecchietti
IPC分类号： A61K31/17 , A61P1/04 , C07C67/00 , C07C239/00 , C07C275/40 , C07C127/19
CPC分类号： C07C275/40
摘要： Novel derivatives of phenylethylamine, having general formula: ##STR1## wherein R is hydrogen or a lower alkyl, are disclosed, to be used in the therapy of diseases of the digestive apparatus, particularly gastric and/or duodenal ulcers. The novel derivatives of phenylethylamine are prepared(a) from a compound of formula (II) ##STR2## by reaction with potassium cyanate, in the presence of an organic acid; (b) from the compound of formula (II) which is converted to the corresponding phenylcarbonic derivative by reacting with phenylchloroformiate and then with ammonia(c) from a compound of formula (IV) ##STR3## which is converted to a compound of formula (V), the latter being converted to the desired derivatives (I) by treatment with aqueous alkali.
摘要翻译：公开了用于治疗消化器官疾病，特别是胃和/或十二指肠溃疡的具有以下通式的苯乙胺的新型衍生物：其中R是氢或低级烷基。通过与有机酸的存在下与氰酸钾反应，由式（II）化合物（II）制备苯乙胺的新衍生物（a）（Ⅳ）化合物与式（Ⅳ）化合物反应得到式（Ⅳ）化合物，式（Ⅳ）化合物转化成相应的苯基碳酸衍生物，然后与式（Ⅳ）化合物（V）化合物，后者通过用碱水溶液处理而转化为所需的衍生物（I）。

8. 发明授权

US5366981A N-acyl-substituted azacyclic compounds, processes for their preparaion, and their use as pharmaceuticals 失效
标题翻译： N-酰基取代的氮杂环化合物，其制备方法及其作为药物的用途
公开(公告)号：US5366981A
公开(公告)日：1994-11-22
申请号：US859389
申请日：1992-05-22
申请人： Vittorio Vecchietti , Roberto Colle , Giulio Dondio , Giuseppe Giardina
发明人： Vittorio Vecchietti , Roberto Colle , Giulio Dondio , Giuseppe Giardina
IPC分类号： A61K31/40 , A61K31/4427 , A61K31/445 , A61K31/55 , A61P9/08 , A61P9/10 , A61P25/28 , C07D207/20 , C07D401/06 , C07D403/06 , C07D495/04 , A61K31/47
CPC分类号： C07D401/06 , C07D495/04
摘要： A compound, a solvate or salt thereof, of formula (I): ##STR1## in which: A is ##STR2## p is 2; ROC-- is an acyl group linked to a substituted or unsubstituted carbocyclic aromatic ring system;R.sub.1 and R.sub.2 are substituents on the same or different carbon atoms and are independently hydrogen or C.sub.1-6 alkyl; andR.sub.a is a phenyl or thienyl ring, andis useful for the treatment of pain, hyponatremic disease states or cerebral ischemia.
摘要翻译： PCT No.PCT / EP90 / 01961 Sec。 371日期：1992年5月22日 102（e）日期1992年5月22日PCT 1990年11月14日PCT PCT。出版物WO91 / 08205 日期：1991年6月13日。式（I）的化合物，其溶剂合物或盐：其中：A为或 p为2; ROC-是与取代或未取代的碳环芳环连接的酰基; R1和R2是相同或不同碳原子上的取代基，独立地是氢或C1-6烷基; 并且R a是苯基或噻吩基环，并且可用于治疗疼痛，hyponatremic疾病状态或脑缺血。

9. 发明授权

US4999359A Heterocyclic ethylene diamine compounds and their pharmaceutical compositions and methods 失效
标题翻译：杂环乙二胺化合物及其药物组合物和方法
公开(公告)号：US4999359A
公开(公告)日：1991-03-12
申请号：US323617
申请日：1989-03-14
申请人： Vittorio Vecchietti , Giuseppe Giardina
发明人： Vittorio Vecchietti , Giuseppe Giardina
IPC分类号： A61K31/38 , A61K31/435 , A61K31/44 , A61K31/4406 , A61K31/4418 , A61P25/04 , C07D213/40 , C07D333/20 , C07D471/04 , C07D495/04
CPC分类号： C07D213/40 , C07D333/20 , C07D471/04 , C07D495/04
摘要： A compound, or a solvate or salt thereof, of formula I: ##STR1## in which: R.CO-- is an acyl group containing a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic group;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom;R.sub.3 is hydrogen, C.sub.1-6 alkyl, or phenyl or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;R.sub.4 is C.sub.1-6 alkyl, or phenyl;R.sub.5 is hydrogen or together with R.sub.4 forms a --(CH.sub.2).sub.n -- group in which n=1, 2 or 3; and `Het` is an optionally substituted single or fused ring heterocyclic group, containing from 5 to 12 ring atoms and comprising up to four hetero-atoms in the or each ring selected from oxygen, nitrogen and sulphur, with the proviso that when, simultaneously, R.sub.1 and R.sub.2 together are linear butylene, R.sub.3 is hydrogen, R.sub.4 is methyl, R.sub.5 is hydrogen and R is 3,4-dichlorophenyl, `Het` is not pyridyl, is useful for the treatment of pain.

10. 发明授权

US4994450A Azacyclic compounds and their use as analgesic agents 失效
标题翻译：氮环化合物及其作为止痛剂的用途
公开(公告)号：US4994450A
公开(公告)日：1991-02-19
申请号：US309687
申请日：1989-02-10
申请人： Vittorio Vecchietti , Antonio Giordani
发明人： Vittorio Vecchietti , Antonio Giordani
IPC分类号： C07D223/04 , A61K31/4433 , A61K31/445 , A61K31/451 , A61K31/55 , A61P25/04 , C07D211/26 , C07D225/02 , C07D409/06
CPC分类号： C07D409/06 , C07D211/26
摘要： A compound, or a solvate or salt thereof, of formula (I) ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups, or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom, provided that R.sub.1 and R.sub.2 are not simultaneously hydrogen;R.sub.3 is hydrogen, C.sub.1-6 alkyl, preferably methyl or ethyl, or phenyl, or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;p is 1, 2, 3 or 4, andR is a group of formula (II) ##STR2## in which the group --(CHR.sub.4).sub.n --X-- is in the meta- or para-position with respect to YR.sub.5 or R.sub.6, R.sub.4 is hydrogen or C.sub.1-6 alkyl, preferably hydrogen;n is 0, 1 or 2, preferably 1;X is a direct bond, or O, S or NR.sub.a in which R.sub.a is hydrogen or C.sub.1-6 alkyl, and is preferably a direct bond;Y is >C.dbd.O, >CHOH, --S.dbd.O or --SO.sub.2 ; each of R.sub.5 and R.sub.6 is C.sub.1-6 alkyl, orR.sub.5 and R.sub.6 are linked together and R.sub.5 represents --(Z).sub.m -- where m is 0 or 1 and Z is O, S or NR.sub.7 where R.sub.7 is hydrogen or C.sub.1-6 alkyl, andR.sub.6 represents --(CH.sub.2).sub.9 -- where q is an integer of from 1 to 4, preferably 2 or 3, and in which one or more of the --(CH.sub.2)-- groups is optionally substituted by a C.sub.1-6 alkyl group, is useful for the treatment of pain.

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