公开(公告)号：US07655690B2

公开(公告)日：2010-02-02

申请号：US10566400

申请日：2004-07-29

Applicant: Ramon Merce Vidal ,  Xavier Codony Soler ,  Alberto Dordal Zueras

Inventor： Ramon Merce Vidal ,  Xavier Codony Soler ,  Alberto Dordal Zueras

IPC: A61K31/415 ,  C07D209/04

CPC classification number: C07D401/04 ,  C07D209/40 ,  C07D471/04

Abstract: The present invention refers to new sulfonamide derivatives, of general formula (Ia, Ib, Ic), (I), (Ia, Ib, Ic), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemate, or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or their salts, preferably their corresponding physiologically acceptable salts or corresponding solvates; to the processes for their preparation, to their application as medicaments in human and/or veterinary therapeutics, and to the pharmaceutical compositions containing them. The new compounds of the present invention can be used in the pharmaceutical industry as intermediates and for preparing medicaments.

Abstract translation: 本发明涉及通式（Ia，Ib，Ic），（I），（Ia，Ib，Ic）的新型磺酰胺衍生物，其任选为其立体异构体之一的形式，优选对映异构体或非对映异构体，其外消旋体或 其形式为至少两种其立体异构体，优选对映异构体或非对映异构体，以任何混合比例的混合物，或其盐，优选其相应的生理学上可接受的盐或相应的溶剂合物; 其制备方法，作为人和/或兽医治疗剂中的药物的应用，以及含有它们的药物组合物。 本发明的新化合物可用于制药工业中作为中间体并用于制备药物。

公开(公告)号：US20090163547A1

公开(公告)日：2009-06-25

申请号：US12093100

申请日：2006-11-07

Applicant: Maria De Las Ermitas Alcalde-Pais ,  Jordi Frigola-Constansa ,  Joerg Holenz ,  Ramon Merce-Vidal ,  Maria De Les Neus Mesquida-Estevez ,  Sara Lopez-Perez

Inventor： Maria De Las Ermitas Alcalde-Pais ,  Jordi Frigola-Constansa ,  Joerg Holenz ,  Ramon Merce-Vidal ,  Maria De Les Neus Mesquida-Estevez ,  Sara Lopez-Perez

IPC: A61K31/454 ,  C07C205/56 ,  C07C317/14 ,  C07D333/66 ,  C07C233/11 ,  C07D295/192 ,  C07D513/04 ,  C07D285/14 ,  A61K31/195 ,  A61K31/381 ,  A61K31/165 ,  A61K31/402 ,  A61K31/429 ,  A61K31/433 ,  A61P3/04 ,  A61P7/12 ,  A61P25/28 ,  A61P25/18

CPC classification number: C07C311/21 ,  C07C205/45 ,  C07C205/56 ,  C07C211/30 ,  C07C225/22 ,  C07C233/11 ,  C07C309/86 ,  C07C311/37 ,  C07C311/44 ,  C07C311/46 ,  C07C2602/08 ,  C07D285/01 ,  C07D285/14 ,  C07D295/073 ,  C07D295/135 ,  C07D295/182 ,  C07D295/185 ,  C07D333/62 ,  C07D513/04

Abstract: The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.

Abstract translation: 本发明涉及具有通式（I）的新的茚衍生物及其制备方法，它们作为药物的应用和含有它们的药物组合物。 式（I）的新化合物显示出对5-HT 6受体的亲和力，因此对于治疗由这些受体介导的疾病是有效的。

公开(公告)号：US20090030013A1

公开(公告)日：2009-01-29

申请号：US12175660

申请日：2008-07-18

Applicant: Jose Luis Diaz-Fernandez ,  Ramon Merce-Vidal ,  Lajos Novak

Inventor： Jose Luis Diaz-Fernandez ,  Ramon Merce-Vidal ,  Lajos Novak

IPC: A61K31/496 ,  C07D401/02 ,  A61P3/00 ,  A61P25/00

CPC classification number: A61K31/4709 ,  C07D215/38 ,  C07D215/58

Abstract: The present invention refers to substituted tetrahydro-quinoline-sulfonamide compounds of general formula (I): a method for their preparation, a medicament comprising these compounds and the use of substituted tetrahydro-quinoline-sulfonamide compounds for the preparation of medicaments for 5-HT6 receptor regulation as well as for the treatment of disorders related thereto.

Abstract translation: 本发明涉及通式（I）的取代的四氢 - 喹啉 - 磺酰胺化合物：其制备方法，包含这些化合物的药物以及取代的四氢 - 喹啉 - 磺酰胺化合物用于制备5-HT6的药物 受体调节以及与之相关的疾病的治疗。

公开(公告)号：US20080280942A1

公开(公告)日：2008-11-13

申请号：US11997136

申请日：2006-07-26

Applicant: Jose Luis Diaz-Fernandez ,  Ramon Merce-Vidal ,  Joerg Holenz

Inventor： Jose Luis Diaz-Fernandez ,  Ramon Merce-Vidal ,  Joerg Holenz

IPC: A61K31/437 ,  C07D471/14 ,  A61P3/00 ,  A61P25/22 ,  A61P25/28 ,  A61P25/18

CPC classification number: C07D471/04

Abstract: The present invention relates to new tetrahydro-β-carbolin-sulfonamide derivatives of general formula (I), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemates or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or corresponding physiologically acceptable salts or corresponding solvates. These compounds are suitable as pharmacologically active agents in a medicament for the prophylaxis and/or treatment of disorders or diseases related to 5-HT6 receptors. The invention also relates to two different methods for obtaining the mentioned compounds and to pharmaceutical compositions containing them.

Abstract translation: 本发明涉及通式（I）的新的四氢-β-咔啉 - 磺酰胺衍生物，任选地以其立体异构体之一的形式，优选对映异构体或非对映异构体，其外消旋体或其至少两种立体异构体的混合物的形式 ，优选对映异构体或非对映体，以任何混合比例，或相应的生理上可接受的盐或相应的溶剂化物。 这些化合物在用于预防和/或治疗与5-HT 6受体相关的疾病或疾病的药物中适合作为药理学活性剂。 本发明还涉及获得所述化合物和含有它们的药物组合物的两种不同方法。

公开(公告)号：US20070185158A1

公开(公告)日：2007-08-09

申请号：US10566164

申请日：2004-07-29

Applicant: Ramon Merce Vidal ,  Xavier Codony Soler ,  Alberto Dordal Zueras

Inventor： Ramon Merce Vidal ,  Xavier Codony Soler ,  Alberto Dordal Zueras

IPC: C07D455/02 ,  A61K31/4745 ,  A61K31/454 ,  A61K31/405 ,  C07D403/02

CPC classification number: C07D409/12 ,  C07D209/08 ,  C07D513/04

Abstract: The present invention refers to new sulfonamide derivatives, of general formula (1a, 1b, 1c), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemate, or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or their salt thereof s, preferably the corresponding, physiologically acceptable salt thereofs, or corresponding solvate thereofs; to the processes for their preparation, to their application as medicaments in human and/or veterinary therapeutics, and to the pharmaceutical compositions containing them.

Abstract translation: 本发明涉及通式（1a，1b，1c）的新的磺酰胺衍生物，任选地以其立体异构体之一的形式，优选对映体或非对映异构体，其外消旋体或其至少两种立体异构体的混合物的形式 ，优选对映异构体或非对映体，以任何混合比例，或其盐，优选相应的生理学上可接受的盐或其相应的溶剂合物; 其制备方法，作为人和/或兽医治疗剂中的药物的应用，以及含有它们的药物组合物。

公开(公告)号：US20070009597A1

公开(公告)日：2007-01-11

申请号：US10566402

申请日：2004-07-29

Applicant: Antoni Torrens Jover ,  Josep Mas Prio ,  Albert Dordal Zueras ,  Xavier Codony Soler ,  Ramon Merce Vidal ,  Jose-Aurello Castillo Perez ,  Jordi Frigola Constansa ,  Helmut-Heinrich Buschmann

Inventor： Antoni Torrens Jover ,  Josep Mas Prio ,  Albert Dordal Zueras ,  Xavier Codony Soler ,  Ramon Merce Vidal ,  Jose-Aurello Castillo Perez ,  Jordi Frigola Constansa ,  Helmut-Heinrich Buschmann

IPC: A61K39/395 ,  A61K31/538 ,  A61K31/445 ,  A61K31/405 ,  A61K9/22

CPC classification number: A61K45/06

Abstract: The present invention relates to an active substance combination comprising at least one compound with neuropeptide Y-receptor affinity, preferably neuropeptide Y5-receptor affinity, and at least one compound with 5-HT6 receptor affinity, a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament.

Abstract translation: 本发明涉及包含至少一种具有神经肽Y受体亲和力的化合物，优选神经肽Y5-受体亲和力的活性物质组合物和至少一种具有5-HT 6受体亲和力的化合物，药物 包括所述活性物质组合，以及所述活性物质组合用于制备药物的用途。

公开(公告)号：US07129361B2

公开(公告)日：2006-10-31

申请号：US10779287

申请日：2004-02-13

Applicant: Ramon Merce-Vidal ,  Blas Andaluz-Mataro ,  Jordi Frigola-Constansa

Inventor： Ramon Merce-Vidal ,  Blas Andaluz-Mataro ,  Jordi Frigola-Constansa

IPC: C07D257/06 ,  C07D403/04 ,  C07D249/08 ,  C07D233/02

CPC classification number: A61K31/4155 ,  C07D409/04 ,  C07D409/06

Abstract: 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.

公开(公告)号：US5532234A

公开(公告)日：1996-07-02

申请号：US344377

申请日：1994-11-23

Applicant: Jordi Frigola-Constansa ,  Ramon Merce-Vidal

Inventor： Jordi Frigola-Constansa ,  Ramon Merce-Vidal

IPC: C07D249/08 ,  A61K31/495 ,  A61K31/505 ,  A61P1/04 ,  C07D207/325 ,  C07D231/16 ,  C07D233/68 ,  C07D403/12 ,  C07D417/12 ,  C07D471/04 ,  A61K31/54 ,  A61K31/535

CPC classification number: A61K31/505 ,  A61K31/495 ,  Y10S514/925

Abstract: The present invention relates to the use of 1-{4-[4-aryl(or heteroaryl)-1-piperazinyl]butyl}-1H-azole derivatives and of their physiologically acceptable salts for the manufacture of medicaments intended for the treatment of disorders associated with gastric secretion.

Abstract translation: 本发明涉及1- {4- [4-芳基（或杂芳基）-1-哌嗪基]丁基} -1H-吡唑衍生物及其生理学上可接受的盐在制备用于治疗疾病的药物中的用途 与胃分泌相关。

公开(公告)号：US5444059A

公开(公告)日：1995-08-22

申请号：US192142

申请日：1994-02-04

Applicant: Jordi Frigola-Constansa ,  Ramon Merce-Vidal

Inventor： Jordi Frigola-Constansa ,  Ramon Merce-Vidal

IPC: A61K31/505 ,  A61K31/506 ,  A61P25/00 ,  A61P25/20 ,  A61P25/22 ,  C07D239/28 ,  C07D239/42 ,  C07D403/12 ,  C07D403/14 ,  A61K31/495

CPC classification number: C07D403/12

Abstract: 2-[4-(4-azolylbutyl)-1-piperazinyl]-pyrimidine derivatives characterized in that they correspond to the general formula I ##STR1## in which X.sub.2 represents a nitrogen atom or a C-R.sub.2 group, X.sub.4 represents a nitrogen atom or a C-R.sub.4 group, X.sub.5 represents a nitrogen atom or a C-R.sub.5 group, the process for preparing them, their application as medicinal product, and the pharmaceutical compositions containing them.

Abstract translation: 2- [4-（4-氮杂丁基）-1-哌嗪基] - 嘧啶衍生物，其特征在于它们对应于其中X 2表示氮原子或C-R 2基团的通式I I，其中X 4表示氮 原子或C-R 4基团，X 5表示氮原子或C-R 5基团，其制备方法，其作为药用产品的应用，以及含有它们的药物组合物。

公开(公告)号：US08097643B2

公开(公告)日：2012-01-17

申请号：US10566164

申请日：2004-07-29

Applicant: Ramon Merce Vidal ,  Xavier Codony Soler ,  Alberto Dordal Zueras

Inventor： Ramon Merce Vidal ,  Xavier Codony Soler ,  Alberto Dordal Zueras

IPC: A61K31/404 ,  C07D209/10

CPC classification number: C07D409/12 ,  C07D209/08 ,  C07D513/04

Abstract: The present invention refers to new sulfonamide derivatives, of general formula (1a, 1b, 1c), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemate, or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or their salt thereof s, preferably the corresponding, physiologically acceptable salt thereofs, or corresponding solvate thereofs; to the processes for their preparation, to their application as medicaments in human and/or veterinary therapeutics, and to the pharmaceutical compositions containing them.

Abstract translation: 本发明涉及通式（1a，1b，1c）的新型磺酰胺衍生物，任选呈其立体异构体之一形式，优选对映异构体或非对映异构体，其外消旋物或其至少两种立体异构体的混合物的形式 ，优选对映异构体或非对映体，以任何混合比例，或其盐，优选相应的生理上可接受的盐或其相应的溶剂合物; 其制备方法，作为人和/或兽医治疗剂中的药物的应用，以及含有它们的药物组合物。