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1. 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.

2. 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.

3. 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。

4. 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.

5. 发明授权

US5428042A 1-(2H-1-oxo-3,4-dihydronaphtyl-6-yl)-acetyl-piperidines as kappa agonists 失效
标题翻译： 1-（2H-1-氧代-3,4-二氢萘基-6-基） - 乙酰基 - 哌啶作为κ激动剂
公开(公告)号：US5428042A
公开(公告)日：1995-06-27
申请号：US940858
申请日：1992-12-23
申请人： Vittorio Vecchietti , Roberto Colle , Giuseppe Giardina
发明人： Vittorio Vecchietti , Roberto Colle , Giuseppe Giardina
IPC分类号： A61K31/445 , A61P9/08 , A61P9/10 , A61P25/04 , A61P25/28 , C07D211/16 , C07D211/26
CPC分类号： A61K31/445 , C07D211/26
摘要： ##STR1## Azacyclic derivatives of formula (I), in which R
1 and R
2 are each linear or branched alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, cycloalkenyl or alkynyl; R
3 and R
4 are identical, and each is a hydrogen or alkyl; and R
5 is hydrogen or alkyl, and their use in medicine are disclosed.
摘要翻译： PCT No.PCT / EP91 / 00717 Sec。 371日期1992年12月23日 102（e）日期1992年12月23日PCT 1991年4月12日提交PCT公布。出版物WO91 / （I）式（I）的二环衍生物，其中R 1和R 2各自是直链或支链烷基，环烷基，环烷基烷基，烯基，环烯基或炔基; R3和R4相同，各自为氢或烷基; R5是氢或烷基，并且它们在药物中的用途被公开。

6. 发明授权

US5322848A N-acyl-substituted azacyclic compounds, processes for their preparation, 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：US5322848A
公开(公告)日：1994-06-21
申请号：US859388
申请日：1992-05-22
申请人： Robert Colle , Giulio Dondio , Giuseppe Giardina , Lorenzo Leurini , Vittorio Vecchietti
发明人： Robert Colle , Giulio Dondio , Giuseppe Giardina , Lorenzo Leurini , Vittorio Vecchietti
IPC分类号： A61K31/445 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61P3/00 , A61P9/00 , A61P25/04 , C07D211/40 , C07D211/42 , C07D211/74 , C07D401/06 , C07D405/14 , C07D409/14 , C07D417/14 , C07D217/06
CPC分类号： C07D401/06 , C07D211/42
摘要： A compound, or solvate or salt thereof, of formula ##STR1## R.sub.1 is hydrogen, halogen, or C.sub.1-6 alkyl; R.sub.2 and R.sub.3 are hydrogen or C.sub.1-6 alkyl;R.sub.5 together with R.sub.4 forms a --(CH).sub.2).sub.2 -- group optionally substituted by one or two C.sub.1-6 alkyl;W is halogen or when A is gem-dimethyl substituted piperidine, is OH;a is 1 or 2,useful in the treatment of pain.
摘要翻译： PCT No.PCT / EP90 / 02011 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20日PCT PCT。出版物WO91 / 08206 日期：1991年6月13日。化学式，或其溶剂合物或其盐，其分子式为：其中R 2和R 3为氢或C 1-6烷基; R5与R4一起形成任选被一个或两个C 1-6烷基取代的 - （CH）2）2-基团; W是卤素或当A是偕二甲基取代的哌啶时，是OH; a是1或2，用于治疗疼痛。

7. 发明授权

US5030649A 2-aminoethylamine derivatives, compositions of the same and use of said compounds in medicine 失效
标题翻译： 2-氨基乙胺衍生物，其组合物和所述化合物在医药中的用途
公开(公告)号：US5030649A
公开(公告)日：1991-07-09
申请号：US598825
申请日：1990-10-16
申请人： Vittorio Vecchietti , Giuseppe Giardina
发明人： Vittorio Vecchietti , Giuseppe Giardina
IPC分类号： C07D295/125
CPC分类号： C07D295/125
摘要： A compound of formula (I): ##STR1## or a salt and/or solvate thereof, wherein R represents an acyl group containing a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic group;R.sup.1 and R.sup.2 each independently represents an alkyl, alkenyl or alkynyl group or R.sup.1 together with R.sup.2 represents a C.sub.3-6 polymethylene or alkenylene group;R.sup.3 represents hydrogen or alkyl;R.sup.4 represents hydrogen, halogen, alkyl, hydroxy, alkoxy, nitrile, nitro, amino or mono or disubstituted amino; andn represents O or an integer 1,is useful in the treatment of pain.

8. 发明授权

US4806547A Isoquinoline derivatives, analgesic compounds thereof and method of treating pain 失效
标题翻译：异喹啉衍生物，其镇痛化合物和治疗疼痛的方法
公开(公告)号：US4806547A
公开(公告)日：1989-02-21
申请号：US6068
申请日：1987-01-22
申请人： Giuseppe Giardina , Vittorio Vecchietti
发明人： Giuseppe Giardina , Vittorio Vecchietti
IPC分类号： C07D401/06 , A61K31/47 , A61K31/472 , A61P25/04 , C07D217/14 , C07D217/16
CPC分类号： C07D217/14
摘要： A compound of formula 1, or a solvate or salt thereof: ##STR1## in which: RCO is an acyl group in which the group R comprises a substituted or unsubstituted carbocyclic or heterocyclic aromatic ring and R.sub.1 and R.sub.2 are independently C.sub.1-6 alkyl groups or together form a C.sub.3-6 polymethylene or alkenylene group, is useful for treating pain.
摘要翻译：式1的化合物或其溶剂合物或盐：其中：RCO是酰基，其中基团R包含取代或未取代的碳环或杂环芳族环，并且R 1和R 2独立地为C 1-6烷基基团或一起形成C3-6聚亚甲基或亚链烯基，可用于治疗疼痛。

9. 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。

10. 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。

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