专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 再颁专利

USRE39113E1 Utilization of derivatives of tetrahydropyridines(or 4-hydroxypiperidines)-butylazols in the preparation of a medicament for the treatment of pain 失效
标题翻译：四氢吡啶衍生物（或4-羟基哌啶） - 丁基二醇在制备用于治疗疼痛的药物中的应用
公开(公告)号：USRE39113E1
公开(公告)日：2006-05-30
申请号：US10355216
申请日：1999-07-09
申请人： Ramon Merce-Vidal , Jordi Frigola-Constansa
发明人： Ramon Merce-Vidal , Jordi Frigola-Constansa
IPC分类号： A61K31/445 , A61K31/44 , C07D211/06 , C07D401/00
CPC分类号： A61K31/454 , A61K31/4439
摘要： Derivatives of tetrahydropyridines (or 4-hydroxypiperidines)-butylazols of formula (I), wherein R1, R2 and R3, which are similar or different, represent each of them hydrogen, halogen, alkyl C1-C4, trifluoromethyl, hydroxyl, alkoxyl, or two adjacent radicals can form a ring; A is a C atom and the dotted line represents an additional bond, or A is a C atom joined to a hydroxyl group and the dotted line represents absence of additional bond; Z1 is N or CR4; Z2 is N or CR5; Z4 is N or CR7; and R4, R5, R6 and R7, which different, represent hydrogen, halogen, alkyl C3-C4, aryl or substituted aryl, or two adjacent radicals can form part of another ring. These derivatives are useful for the treatment of acute pain, neuropathic pain or nociceptive pain in mammals, including human beings.
摘要翻译：式（I）的四氢吡啶（或4-羟基哌啶） - 丁基二醇的衍生物，其中R 1，R 2，R 3，类似或不同的，代表氢，卤素，烷基C 1 -C 4，三氟甲基，羟基，烷氧基或两个相邻的基团可以形成环; A是C原子，虚线表示附加键，或A是连接到羟基的C原子，虚线表示不存在附加键; Z 1是N或CR 4; Z 2是N或CR 5; Z 4是N或CR 7; 和R 4，R 5，R 6和R 7，其不同表示氢，卤素，烷基 C 3 -C 4，芳基或取代的芳基或两个相邻的基团可以形成另一个环的一部分。这些衍生物可用于治疗哺乳动物（包括人类）的急性疼痛，神经性疼痛或伤害性疼痛。

42. 发明申请

US20050096474A1 Procedure for the preparation of racemic derivatives of 1,5-diaryl-3-trifluoromethyl-delta2-pyrazolines 审中-公开
公开(公告)号：US20050096474A1
公开(公告)日：2005-05-05
申请号：US11006931
申请日：2004-12-08
申请人： Monserrat Alcon-Marrugat , Miguel Pericas-Brondo , Maria Cuberes-Altisen , Jordi Frigola-Constansa
发明人： Monserrat Alcon-Marrugat , Miguel Pericas-Brondo , Maria Cuberes-Altisen , Jordi Frigola-Constansa
IPC分类号： C07D231/06 , C07D231/12
CPC分类号： C07D231/06
摘要： Procedure for preparation of compounds with the general formula 1, which include the racemic mixtures (±)-1, and the enantiomerically pure compounds (−)-1 and (+)-1, wherein R1 and R3, like or different, represent an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl or methoxy group; R2 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group; R4 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group, with the condition that one of the substituents R2 or R4 is a methylsulphonyl or aminosulphonyl group; which involves obtaining the racemic mixture with the general formula (±)-1 by reacting an (E)-1,1,1-trifluoro-4-aryl-3-buten-2-one with a phenylhydrazine, followed by a treatment with chlorosulphonic acid, or by reacting with chlorosulphonic acid followed by a reaction with sodium hydroxide and, finally, with thionyl chloride. The product obtained by either of these methods is made to react with ammonium carbonate or ammonia, or with sodium sulphite and methyl iodide or methyl sulphate. In addition, to obtain the enantiomerically pure compounds with the general formula 1 by resolving the racemic mixture with the general formula (±)-1, a reaction is effected with optically active ephedrine, followed by formation of the sodium salt of each enantiomer, reaction with thionyl chloride and ammonium carbonate or ammonia, or instead with thionyl chloride followed by sodium sulphite and methyl iodide or methyl sulphate to thereby obtain separately the enantiomerically pure compounds with the general formulae (−)-1 and (+)-1.

43. 发明授权

US06846935B2 Procedure for the preparation of racemic and enantionmerically pure derivatives of 1,5-diaryl-3-trifluoromethyl-Δ2-pyrazolines 失效
标题翻译：制备1,5-二芳基-3-三氟甲基-3a-吡唑啉的外消旋和对映纯的衍生物的方法
公开(公告)号：US06846935B2
公开(公告)日：2005-01-25
申请号：US10312194
申请日：2002-06-06
申请人： Montserrat Alcon-Marruga , Miguel Angel Pericas-Brondo , Maria Rosa Cuberes-Altisen , Jordi Frigola-Constansa
发明人： Montserrat Alcon-Marruga , Miguel Angel Pericas-Brondo , Maria Rosa Cuberes-Altisen , Jordi Frigola-Constansa
IPC分类号： C07D231/06 , C07D231/12
CPC分类号： C07D231/06
摘要： Procedure for preparation of compounds with the general formula 1, which include the racemic mixtures (±)-1, and the enantiomeric ally pure compounds (−)-1 and (+)-1, wherein R1 and R3, like or different, represent an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl or methoxy group; R2 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group; R4 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group, with the condition that one of the substituents R2 or R4 is a methylsulphonyl or aminosulphonyl group; which involves obtaining the racemic mixture with the general formula (±)-1 by reacting an (E)-1,1,1-trifluoro-4-aryl-3-buten-2-one with a phenylhydrazine, followed by a treatment with chlorosulphonic acid, or by reacting with chlorosulphonic acid followed by a reaction with sodium hydroxide and, finally, with thionyl chloride. The product obtained by either of these methods is made to react with ammonium carbonate or ammonia, or with sodium sulphite and methyl iodide or methyl sulphate. In addition, to obtain the enantiomerically pure compounds with the general formula 1 by resolving the racemic mixture with the general formula (±)-1, a reaction is effected with optically active ephedrine, followed by formation of the sodium salt of each enantiomer, reaction with thionyl chloride and ammonium carbonate or ammonia, or instead with thionyl chloride followed by sodium sulphite and methyl iodide or methyl sulphate to thereby obtain separately the enantiomerically pure compounds with the general formulae (−)-1 and (+)-1.
摘要翻译：制备具有通式1的化合物的方法，其包括外消旋混合物（±）-1和对映异构体烯丙基化合物（ - ）-1和（+） - 1，其中R1和R3等同或不同表示氢，氯，氟，甲基，三氟甲基或甲氧基的原子; R2代表氢，氯，氟，甲基，三氟甲基，甲氧基，三氟甲氧基，甲基磺酰基或氨基磺酰基的原子; R4表示氢，氯，氟，甲基，三氟甲基，甲氧基，三氟甲氧基，甲基磺酰基或氨基磺酰基的原子，条件是取代基R2或R4中的一个为甲基磺酰基或氨基磺酰基; 其包括通过（E）-1,1,1-三氟-4-芳基-3-丁烯-2-酮与苯肼反应获得具有通式（±）-1的外消旋混合物，然后用或通过与氯磺酸反应，然后与氢氧化钠反应，最后与亚硫酰氯反应。通过这些方法得到的产物与碳酸铵或氨，或与亚硫酸钠和甲基碘或甲基硫酸盐反应。另外，为了通过拆分通式（±）-1的外消旋混合物来获得具有通式1的对映异构体纯的化合物，用光学活性麻黄碱进行反应，随后形成各对映异构体的钠盐，反应与亚硫酰氯和碳酸铵或氨反应，或代之以亚硫酰氯，然后加入亚硫酸钠和甲基碘或甲基硫酸盐，从而分别得到具有通式（ - ） - 1和（+） - 1的对映体纯的化合物。

44. 发明授权

US06518295B1 Utilization of aryl(or heteroaryl)azolylcarbinol derivatives in the preparation of a medicament for the treatment of troubles mediated by an excess of substance P 失效
标题翻译：芳基（或杂芳基）唑基甲醇衍生物在制备用于治疗过量物质P介导的麻烦的药物中的应用
公开(公告)号：US06518295B1
公开(公告)日：2003-02-11
申请号：US09762079
申请日：2001-02-01
申请人： Ramón Merce-Vidal , Jordi Frigola-Constansa
发明人： Ramón Merce-Vidal , Jordi Frigola-Constansa
IPC分类号： A61K31415
CPC分类号： A61K31/415 , A61K31/00 , A61K31/4164 , A61K31/5517
摘要： The present invention relates to the use of derivatives of aryl (or heteroaryl) azolylcarbinols of general formula (1) of the specification, as well as their physiologically acceptable salts, in the manufacture of medicaments, useful in human and/or veterinary therapy, for the treatment of disorders that are mediated by an excess of substance P, and especially disorders of the central nervous system such as anxiety, depression, schizophrenia, manic depressive psychosis, sexual dysfunction, drug addiction, cognitive disorders, and locomotive disorders.
摘要翻译：本发明涉及本说明书通式（1）的芳基（或杂芳基）唑基甲醇衍生物及其生理上可接受的盐在制备用于人和/或兽医疗法的药物中的用途，其用于治疗由过量的物质P介导的疾病，特别是中枢神经系统的障碍如焦虑，抑郁，精神分裂症，躁狂抑郁精神病，性功能障碍，药物成瘾，认知障碍和机车病症。

45. 发明授权

US06410582B1 Thienylazolylalcoxyethanamines, their preparation and their application as medicaments 失效
标题翻译：噻吩并噻唑基羟乙胺，它们的制备及其作为药物的应用
公开(公告)号：US06410582B1
公开(公告)日：2002-06-25
申请号：US09673186
申请日：2000-10-12
申请人： Ramon Merce-Vidal , Blas Andaluz-Mataro , Jordi Frigola-Constansa
发明人： Ramon Merce-Vidal , Blas Andaluz-Mataro , Jordi Frigola-Constansa
IPC分类号： A61K3141
CPC分类号： A61K31/4155 , C07D409/04 , C07D409/06
摘要： The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromatic group, N-methyl-substituted, that contains from one to three nitrogen atoms. They have analgesic activity in mammals, including humans. The compounds (I) can be obtained, for example, by reaction of a derivative of hydroxy-thienylazol (IV) with a derivative of a suitable N-(ethyl)amine. The compounds (IV) are useful intermediates in the synthesis of the compounds (I). The compounds (I) have an application in human and/or veterinary medicine.
摘要翻译：其中R 1是氢原子，卤素原子或低级烷基的噻吩基唑烷基乙胺（I） R2，R3和R4独立地表示氢原子或低级烷基; 并且Az表示含有一至三个氮原子的五元氮杂环芳族基团N-甲基取代基。它们在哺乳动物，包括人类中具有止痛活性。化合物（I）可以通过例如羟基噻吩唑（IV）的衍生物与合适的N-（乙基）胺衍生物的反应来获得。化合物（IV）是化合物（I）的合成中的有用的中间体。化合物（I）在人和/或兽医学中有应用。

46. 发明授权

US06372746B1 Derivatives of acyl-piperazinyl-pyrimidines, preparation thereof and application as medicaments 失效
标题翻译：酰基 - 哌嗪基 - 嘧啶的衍生物，其制备和作为药物的应用
公开(公告)号：US06372746B1
公开(公告)日：2002-04-16
申请号：US09462880
申请日：2000-02-24
申请人： Jordi Corbera-Arjona , David Vaño-Domenech , Jordi Frigola-Constansa
发明人： Jordi Corbera-Arjona , David Vaño-Domenech , Jordi Frigola-Constansa
IPC分类号： C07D40304
CPC分类号： C07D405/12 , C07D239/42 , C07D401/12 , C07D403/12 , C07D409/12 , C07D417/12
摘要： The derivatives of acyl-piperazinyl-pyrimidines of general formula (I), where X is O or S; R1 is alkoxy or trifluoromethyl; R2 is alkyl, cycloalkyl, heterocycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl, show activity in the central nervous system. Compounds of general formula (I) in which X is O can be obtained by reacting a derivative of pyrimidine with a derivative of piperazine or by reacting a derivative of piperazinyl-pyrimidine with a carboxylic acid or a salt or derivative thereof. Compounds of general formula (I) in which X is S can be obtained by reacting (I) in which X is O with Lawesson's reagent or with phosphorous pentasulphide. The compounds (I) show sedative activity, anticonvulsant, sleep-inducing or general anaesthetic activity and can be applied in human or veterinary medicine
摘要翻译：通式（I）的酰基哌嗪基 - 嘧啶衍生物，其中X为O或S; R1是烷氧基或三氟甲基; R2是烷基，环烷基，杂环烷基，芳基，芳基烷基，杂芳基或杂芳基烷基，在中枢神经系统中显示活性。其中X为O的通式（I）化合物可以通过使嘧啶衍生物与哌嗪的衍生物反应或通过使哌嗪基 - 嘧啶的衍生物与羧酸或其盐或衍生物反应来获得。其中X为S的通式（I）的化合物可以通过（I）其中X为O与Lawesson's试剂或五硫化磷反应而获得。化合物（I）显示镇静活性，抗惊厥，睡眠诱导或全身麻醉活性，可应用于人或兽药

47. 发明授权

US06303608B1 2-{4-[4-(4,5-dichloro-2-methylimidazol-1-yl)butyl]-1-piperazinyl}-5-fluoropyrimidine, its preparation and its therapeutic use 失效
标题翻译： 2- {4- [4-（4,5-二氯-2-甲基咪唑-1-基）丁基] -1-哌嗪基} -5-氟嘧啶，其制备及其治疗用途
公开(公告)号：US06303608B1
公开(公告)日：2001-10-16
申请号：US09445081
申请日：2000-02-29
申请人： Ramon Merce-Vidal , Jordi Frigola-Constansa
发明人： Ramon Merce-Vidal , Jordi Frigola-Constansa
IPC分类号： C07D40314
CPC分类号： C07D403/12
摘要： 2-{4-[4-(4,5-dichloro-2-methylimidazol-1-yl)butyl]-1-piperazinyl}-5-fluoropyrimidine, and its physiologically acceptable salts; pharmaceutical compositions containing these compounds, and a method of treating vertigo, travel sickness, nausea, depression, anxiety, gastric acid secretion, obsessive/compulsive disorders, panic attacks or sleep apnea using these compounds are disclosed.
摘要翻译： 2- {4- [4-（4,5-二氯-2-甲基咪唑-1-基）丁基] -1-哌嗪基} -5-氟嘧啶及其生理上可接受的盐; 公开了含有这些化合物的药物组合物和使用这些化合物治疗眩晕，旅行病，恶心，抑郁，焦虑，胃酸分泌，强迫症/强迫症，恐慌发作或睡眠呼吸暂停的方法

48. 发明授权

US5849931A Process for separating carbinols 失效
标题翻译：分离甲醇的方法
公开(公告)号：US5849931A
公开(公告)日：1998-12-15
申请号：US875806
申请日：1997-08-05
申请人： Jordi Frigola-Constansa , Juana Maria Berrocal Romero , Maria Rosa Cuberes Altisent , Vicente Gotor Santamaria
发明人： Jordi Frigola-Constansa , Juana Maria Berrocal Romero , Maria Rosa Cuberes Altisent , Vicente Gotor Santamaria
IPC分类号： C07D231/12
CPC分类号： C07D231/12
摘要： A method for predominantly preparing the enantiomer (R)-(+)-5-(phenyl)hydroxymethyl-1-methyl-1H-pyrazole, (R)-(+)-1, by separating the racemate (+)-5-(phenyl)hydroxymethyl-1-methyl-1H-pyrazole of formula (1), comprising the series of steps of using a lipase or material derived therefrom having enzymatic activity in a transesterification reaction, as well as hydrolysing the resulting ester, (S)-(-)-5-(phenyl)alkylcarbonyloxymethyl-1-methyl-1H-pyrazole, of formula (S)-(-)-4, wherein R.sub.1 is a methyl or ethyl radical.
摘要翻译： PCT No.PCT / EP96 / 05596 Sec。 371日期：1997年8月5日 102（e）日期1997年8月5日PCT 1997年12月4日PCT PCT。出版物WO97 / 20817 日期：1997年6月12日主要通过将外消旋体（R） - （+） - （ - ） - （+） - +） - 5-（苯基）羟甲基-1-甲基-1H-吡唑，其包括使用脂肪酶或其衍生的物质在酯交换反应中具有酶活性的一系列步骤，以及水解所得酯，（S） - （ - ） - （ - ） - （ - ） - 5-（苯基）烷基羰基氧基甲基-1-甲基-1H-吡唑，其中R1是甲基或乙基。

49. 发明授权

US5731331A Tetrahydropyridine-(or 4-hydroxypiperidine) alkylazoles 失效
标题翻译：四氢吡啶 - （或4-羟基哌啶）烷基唑
公开(公告)号：US5731331A
公开(公告)日：1998-03-24
申请号：US473066
申请日：1995-06-07
申请人： Ramon Merce-Vidal , Jordi Frigola-Constansa
发明人： Ramon Merce-Vidal , Jordi Frigola-Constansa
IPC分类号： A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/454 , A61P9/00 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/26 , A61P25/28 , A61P43/00 , C07D207/325 , C07D211/14 , C07D211/70 , C07D401/06 , C07D521/00 , A01N43/40
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06
摘要： The present invention relates to the compounds of general formula ##STR1## used as medicaments possessing therapeutic activity for the treatment of anxiety, psychosis, epilepsy, convulsion, motoricity problems, amnesia, cerebrovascular diseases or senile dementia.
摘要翻译：本发明涉及用作治疗焦虑，精神病，癫痫，惊厥，运动性问题，遗忘症，脑血管疾病或老年痴呆的治疗活性的药物的通式（IMAGE）（1）的化合物。

50. 发明授权

US5182281A (Omega-(4-(2-pyrimidinyl)-1-piperazinyl)alkyl)-1H-azole derivatives for the treatment of disorders of cognitive functions 失效
标题翻译：（OMEGA-（4-（2-吡啶基）-1-哌嗪基）亚基）-1H-氨基衍生物用于治疗认知功能障碍
公开(公告)号：US5182281A
公开(公告)日：1993-01-26
申请号：US824995
申请日：1992-01-24
申请人： Jordi Frigola-Constansa , Juan Pares-Corominas
发明人： Jordi Frigola-Constansa , Juan Pares-Corominas
IPC分类号： A61K31/505 , A61K9/20 , A61K9/48 , A61K31/496 , A61K31/506 , A61P25/28 , C07D403/12 , C07D403/14 , C07D513/04 , C07D521/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D403/12 , C07D403/14
摘要： The present invention relates to the use of the derivatives of general formula I ##STR1## in which: n can have values 1 to 6, andR represents a hydrogen atom, a halogen, a C.sub.1 to C.sub.4 lower alkyl radical, a heteroaryl radical, a sulpho radical, an N-substituted or N,N-disubstituted sulphamoyl radical, a nitro radical, a hydroxyl radical, an oxo radical, a C.sub.1 to C.sub.4 lower alkoxy radical, a cyano radical, a C.sub.1 to C.sub.4 lower alkylcarboxylate radical, an aryl or substituted aryl radical, or an amino or substituted amino radical of formula ##STR2## in which R.sub.1 and R.sub.2, which may be identical or different, represent a hydrogen atom, an alkyl radical, an aryl radical, an alkylcarbonyl radical, an arylcarbonyl radical, an alkylsulphonyl radical or an arylsulphonyl radical, the alkyl fragments of these radicals containing from 1 to 4 carbon atoms,and their therapeutically acceptable salts, for the manufacture of medicinal products intended for the treatment of disorders of cognitive funciton, such as presenile dementia, senile dementia, memory dysfunctions, deterioration of awareness and Alzheimer's disease.
摘要翻译：本发明涉及通式I（I）的衍生物的用途，其中：n可以具有1-6的数值，R代表氢原子，卤素，C1-C4低级烷基，杂芳基，磺酰基，N-取代或N，N-二取代的氨磺酰基，硝基，羟基，氧代基，C 1至C 4低级烷氧基，氰基，C 1至C 4低级烷基羧酸酯基团，芳基或取代的芳基，或式“IMAGE”的氨基或取代的氨基，其中可以相同或不同的R 1和R 2表示氢原子，烷基，芳基，烷基羰基，芳基羰基，烷基磺酰基或芳基磺酰基，这些含有1至4个碳原子的基团的烷基片段及其治疗上可接受的盐，用于制造旨在治疗认知功能障碍的药物，例如作为老年痴呆症，老年痴呆，记忆功能障碍，意识恶化和阿尔茨海默病。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式