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1.发明授权Process for preparing (±)trans-4-p-fluorophenyl-3-hydroxymethyl-1-methylpiperidine 失效制备（±）反式-4-对氟苯基-3-羟甲基-1-甲基哌啶的方法公开(公告)号：US06881845B2
公开(公告)日：2005-04-19
申请号：US10250519
申请日：2001-01-04
申请人： Rafael Foguet , Jorge Ramentol , Diego Fernandez-Cano , Miguel P. Armengol , Inés Petschen , Juan Sallares , Francesc X. Camps , Manuel M. Raga , Josep M. Castello
发明人： Rafael Foguet , Jorge Ramentol , Diego Fernandez-Cano , Miguel P. Armengol , Inés Petschen , Juan Sallares , Francesc X. Camps , Manuel M. Raga , Josep M. Castello
IPC分类号： C07C221/00 , C07C223/02 , C07C225/08 , C07C225/10 , C07C231/02 , C07C233/31 , C07C235/80 , C07D211/22 , C07D211/78 , C07D211/90 , C07D211/20 , C07D211/40
CPC分类号： C07D211/22 , C07C221/00 , C07C231/02 , C07D211/90 , C07C225/08 , C07C235/80
摘要： The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hyroxymethyl-1-methylpiperdine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX′) methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.
摘要翻译： 本发明涉及式（I）的（±） - 反式-4-对氟苯基-3-羟甲基-1-甲基哌啶的制备方法。 本发明还涉及用于制备所述中间体的式（IX）和（IX'）方法的新中间体和所述化合物用于制备帕罗西汀和奥莫西汀的用途。
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公开(公告)号：US06930096B2
公开(公告)日：2005-08-16
申请号：US10221581
申请日：2001-03-13
申请人： Rafael Foguet , Jorge Ramentol , Isidro J. Ferrer , Rafael Lozano , Julio J. Secades , Manuel M. Raga , Josep M. Castello , José A. Ortiz
发明人： Rafael Foguet , Jorge Ramentol , Isidro J. Ferrer , Rafael Lozano , Julio J. Secades , Manuel M. Raga , Josep M. Castello , José A. Ortiz
IPC分类号： C07H19/10 , A61K31/7068 , A61P9/10 , A61P43/00 , A61K31/70
CPC分类号： A61K31/7068
摘要： The invention describes the prophylactic treatment of cerebral ischemia with CDP-Choline in patients who have undergone major surgery or are at risk of suffering an acute ischemic event.
摘要翻译： 本发明描述了在经历大手术或患有急性缺血事件的风险的患者中用CDP-Choline预防性治疗脑缺血。
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公开(公告)号：US4883797A
公开(公告)日：1989-11-28
申请号：US143214
申请日：1988-01-07
IPC分类号： A61K31/42 , A61K31/421 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P9/00 , A61P9/06 , C07D207/27 , C07D263/18 , C07D263/20 , C07D263/22 , C07D263/28 , C07D295/02 , C07D295/03 , C07D295/06 , C07D295/067 , C07D295/10 , C07D295/108 , C07D295/12 , C07D295/13 , C07D295/14 , C07D295/145 , C07D295/18 , C07D295/192 , C07D317/28 , C07D333/22
CPC分类号： C07D263/20 , C07D263/28 , C07D295/02 , C07D295/03 , C07D295/067 , C07D295/108 , C07D295/13 , C07D295/145 , C07D295/192 , C07D317/28 , C07D333/22
摘要： Derivatives of piperazine having the general formula ##STR1## wherein R.sub.1 is benzhydryl or cinnamyl and R.sub.2 is selected from the group consisting of ##STR2## --(CH.sub.2).sub.3 --R.sub.8, --CH.sub.2 NHR.sub.9, --CH.sub.2 NH.sub.2 and --COR.sub.10 ; wherein R.sub.3 is hydrogen, chloromethyl, (4-benzhydryl-1-piperazinyl) methyl, 4-morpholinylmethyl or 1-piperidinylmethyl, R.sub.4 is hydrogen, chloromethyl or carbethoxy, R.sub.5 and R.sub.6 taken together are an oxygen atom or the radical --O--(CH.sub.2).sub.2 --O--, R.sub.7 is methyl, phenyl or 2-thienyl, R.sub.8 is 4-morpholinyl, 1-piperidinyl or 4-benzhydryl-1-piperazinyl, R.sub.9 is 2-oxo-1- (pyrrolidinyl) acetyl, 2-hydroxybenzoyl or 4-sulfamoylbenzoyl, R.sub.10 is 2-oxo-1-(pyrrolidinyl)methyl or 4-sulfamoylphenyl and X is oxygen or NH; as well as methods for making the same and their use in a pharmaceutical composition is proposed. The compounds have cardiovascular properties and increasing effects on cerebral flow.
摘要翻译： 其中R 1是二苯甲基或肉桂基，R 2选自CH 2 CR 3 CHR 4， - （CH 2）3 -R 8，-CH 2 NHR 9，-CH 2 NH 2和-COR 10; 其中R 3是氢，氯甲基，（4-二苯甲基-1-哌嗪基）甲基，4-吗啉基甲基或1-哌啶基甲基，R 4是氢，氯甲基或乙氧羰基，R 5和R 6一起是氧原子或-O- CH2）2-O-，R7是甲基，苯基或2-噻吩基，R8是4-吗啉基，1-哌啶基或4-二苯甲基-1-哌嗪基，R9是2-氧代-1-（吡咯烷基）乙酰基， 羟基苯甲酰基或4-氨磺酰基苯甲酰基，R 10是2-氧代-1-（吡咯烷基）甲基或4-氨磺酰基苯基，X是氧或NH; 以及其制备方法及其在药物组合物中的应用。 该化合物具有心脑血管性质和对脑流量的增加作用。
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公开(公告)号：US07635691B2
公开(公告)日：2009-12-22
申请号：US11133251
申请日：2005-05-20
申请人： Rafael Foguet , Jorge Ramentol , Isidro J. Ferrer , Rafael Lozano , Julio J. Secades , Manuel M. Raga , Josep M. Castello , José A. Ortiz
发明人： Rafael Foguet , Jorge Ramentol , Isidro J. Ferrer , Rafael Lozano , Julio J. Secades , Manuel M. Raga , Josep M. Castello , José A. Ortiz
IPC分类号： A61K31/70
CPC分类号： A61K31/7068
摘要： The invention describes a prophylactic treatment of cerebral ischemia with CDP-Choline in patients who have undergone major surgery or are at risk of suffering an acute ischemic event.
摘要翻译： 本发明描述了在经历大手术或患有急性缺血事件的风险的患者中用CDP-Choline预防性治疗脑缺血。
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5.发明申请公开(公告)号：US20080206158A1
公开(公告)日：2008-08-28
申请号：US11886792
申请日：2006-03-20
IPC分类号： A61K9/12 , A61K31/235 , A61K31/185 , A61Q17/04 , A61K8/37 , A61K31/40
CPC分类号： C07C69/76 , A61K8/046 , A61K8/37 , A61K8/585 , A61K31/216 , A61Q1/06 , A61Q3/02 , A61Q17/04 , C07C67/14 , C07C69/92 , C07C219/34 , C07C309/42
摘要： Benzoic acid ester compounds of formula (I): wherein R and R1-R5 have the meanings explained in the description, methods for producing them and use thereof in cosmetic, pharmaceutical, personal care and industrial preparations as sunscreens based on photochemical precursor properties of ultraviolet absorbers.
摘要翻译： 式（I）的苯甲酸酯化合物：其中R和R 1〜R 5具有说明书中所述的含义，其制备方法及其在化妆品中的用途， 制药，个人护理和工业制剂，作为基于紫外线吸收剂的光化学前体性质的防晒剂。
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公开(公告)号：US06894032B2
公开(公告)日：2005-05-17
申请号：US10240159
申请日：2001-03-28
申请人： Rafael Foguet , Jorge Ramentol , Rafael Lozano , Julián Agut , Jesús Torres , Manuel M. Raga , Josep M. Castello , José A. Ortiz
发明人： Rafael Foguet , Jorge Ramentol , Rafael Lozano , Julián Agut , Jesús Torres , Manuel M. Raga , Josep M. Castello , José A. Ortiz
IPC分类号： C07H19/10 , A61K20060101 , A61K31/00 , A61K31/133 , A61K31/205 , A61K31/505 , A61K31/685 , A61K31/70 , A61K31/7068 , A61P25/32 , A61P43/00 , C07H20060101
CPC分类号： A61K31/685
摘要： The invention relates to the use of CDP-Choline or its pharmaceutically acceptable salts for the preparation of a medicinal product for the treatment of alcohol withdrawal syndrome at daily doses equivalent to 0.5-2 g of free CDP-Choline.
摘要翻译： 本发明涉及CDP-胆碱或其药学上可接受的盐在制备用于治疗酒精戒断综合征的药物产品中的用途，其剂量相当于0.5-2g游离CDP-胆碱。
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公开(公告)号：US4600780A
公开(公告)日：1986-07-15
申请号：US595662
申请日：1984-03-20
申请人： Rafael Foguet , Luis Anglada , Manuel M. Raga , Jose A. Ortiz , Aurelio Sacristan , Jose M. Castello
发明人： Rafael Foguet , Luis Anglada , Manuel M. Raga , Jose A. Ortiz , Aurelio Sacristan , Jose M. Castello
IPC分类号： C07D295/08 , A61K31/34 , A61K31/341 , A61K31/415 , A61P1/04 , A61P43/00 , C07D233/54 , C07D233/64 , C07D277/20 , C07D277/48 , C07D295/096 , C07D307/52 , C07D211/18
CPC分类号： C07D233/64 , C07D277/48 , C07D295/096 , C07D307/52 , Y10S514/927
摘要： New N-cyano-formamidine are disclosed of the formula I: ##STR1## wherein R is 2-[[(5-methyl-1H-Imidazol-4-yl)methyl]thio]ethyl, 2-[[[5-[dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl, 2-[[[2-[(aminoiminomethyl)amino]-4-thiazolyl]methyl]thio]ethyl or 3-[3-(1-piperidinylmethyl)phenoxy]propyl, as well as a process for its production, and pharmaceutical preparations containing the same. The compounds possess histamine--induced gastric acid secretion--inhibiting activity, and are indicated for use in the treatment of peptic ulcer and other pathologies caused or stimulated by gastric acidity.
摘要翻译： 公开了式I的新型N-氰基甲脒：其中R是2 - [[（5-甲基-1H-咪唑-4-基）甲基]硫基]乙基，2 - [[[5- [二甲基氨基]甲基] -2-呋喃基]甲基]硫基]乙基，2 - [[[2 - [（氨基亚氨基甲基）氨基] -4-噻唑基]甲基]硫基]乙基或3- [3-（1-哌啶基甲基） 苯氧基]丙基，以及其制备方法，以及含有它们的药物制剂。 该化合物具有组胺诱导的胃酸分泌抑制活性，并被用于治疗由胃酸引起或刺激的消化性溃疡和其他病态。
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8.发明授权公开(公告)号：US08545816B2
公开(公告)日：2013-10-01
申请号：US11886792
申请日：2006-03-20
CPC分类号： C07C69/76 , A61K8/046 , A61K8/37 , A61K8/585 , A61K31/216 , A61Q1/06 , A61Q3/02 , A61Q17/04 , C07C67/14 , C07C69/92 , C07C219/34 , C07C309/42
摘要： Benzoic acid ester compounds of formula (I): wherein R and R1-R5 have the meanings explained in the description, methods for producing them and use thereof in cosmetic, pharmaceutical, personal care and industrial preparations as sunscreens based on photochemical precursor properties of ultraviolet absorbers.
摘要翻译： 式（I）的苯甲酸酯化合物：其中R和R 1 -R 5具有说明书中所述的含义，其制备方法及其在化妆品，药物，个人护理和工业制剂中的用途，作为基于紫外线的光化学前体性质的防晒剂 吸收体。
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9.发明申请Hypocholesterolemic Compositions Comprising a Statin and an Antiflatulent Agent 审中-公开包含他汀类药物和抗凝剂的低胆固醇血症组合物公开(公告)号：US20080206328A1
公开(公告)日：2008-08-28
申请号：US10588377
申请日：2005-02-02
IPC分类号： A61K9/28 , A61K31/40 , A61K31/351 , A61K33/00
CPC分类号： A61K31/40 , A61K9/2009 , A61K9/2013 , A61K9/2054 , A61K31/22 , A61K31/366 , A61K31/695 , A61K2300/00
摘要： The present invention relates to hypocholesterolemic compositions comprising statins plus antiflatulent agents. In particular the compositions of the present invention comprise a statin selected from the group consisting of atorvastatin, cerivastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin and simvastatin, whether in free form or as pharmaceutically acceptable salts and hydrates thereof, plus an antiflatulent agent. selected from the group consisting of simethicone and dimethicone. The combination of statins plus antiflatulent agents is useful in the prevention and management of flatulence caused by statins.
摘要翻译： 本发明涉及包含他汀类加抗消化剂的降血胆固醇组合物。 特别地，本发明的组合物包含选自阿伐他汀，西立伐他汀，氟伐他汀，洛伐他汀，匹伐他汀，普伐他汀，罗苏伐他汀和辛伐他汀的他汀类，无论是游离形式还是药学上可接受的盐和水合物，以及抗消化剂 。 选自二甲硅油和聚二甲基硅氧烷。 他汀类药物联合消炎药可有效预防和治疗他汀类药物引起的肠胃气胀。
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公开(公告)号：US20080166398A1
公开(公告)日：2008-07-10
申请号：US11885554
申请日：2006-02-22
CPC分类号： A61K45/06 , A61K9/0014 , A61K9/1075 , A61K31/4178 , A61K31/4725 , A61K31/57 , A61K2300/00
摘要： Pharmaceutical compositions useful for treating dermal diseases caused by fungi and yeasts with inflammation and/or associated with a bacterial infection. Such compositions contain a therapeutically effective amount of sertaconazole, or a pharmaceutically acceptable salt, solvate, isomer thereof or mixtures thereof; and a therapeutically effective amount of at least one compound selected from the group consisting of hydrocortisone, a pharmaceutically acceptable ester of hydrocortisone, an antibacterial quinolone compound, and mixtures thereof.
摘要翻译： 用于治疗由真菌和酵母引起的具有炎症和/或与细菌感染相关的真皮疾病的药物组合物。 这样的组合物含有治疗有效量的丝光康唑或其药学上可接受的盐，溶剂合物，异构体或其混合物; 和治疗有效量的至少一种选自氢化可的松，氢化可的松的药学上可接受的酯，抗菌喹诺酮化合物及其混合物的化合物。
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