公开(公告)号：US20070203121A1

公开(公告)日：2007-08-30

申请号：US11673328

申请日：2007-02-09

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

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

IPC: A61K31/55 ,  A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  A61K31/405 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

CPC classification number: C07D209/18 ,  C07D209/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D513/04

Abstract: The present invention relates to substituted indole compounds of general formula (I), a process for their preparation, medicaments comprising substituted indole compounds as well as the use of substituted indole compounds for the preparation medicaments, which are suitable e.g., for the prophylaxis and/or treatment of disorders or diseases that are at least partially mediated via 5-HT6 receptors.

Abstract translation: 本发明涉及通式（I）的取代的吲哚化合物，其制备方法，包含取代的吲哚化合物的药物以及用于制备药物的取代的吲哚化合物的用途，其适用于预防和/ 或治疗至少部分通过5-HT 6受体介导的病症或疾病。

公开(公告)号：US20070185207A1

公开(公告)日：2007-08-09

申请号：US10566403

申请日：2004-07-29

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

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

IPC: A61K31/18

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

Abstract: The present invention refers to new sulfonamide derivatives, of general formula (1a, 1b, 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 the 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.

Abstract translation: 本发明涉及通式（1a，1b，ic）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，或其盐，优选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。

公开(公告)号：US20070059364A1

公开(公告)日：2007-03-15

申请号：US10566100

申请日：2004-07-29

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

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

IPC: A61K31/538 ,  A61K31/404 ,  A61K9/22

CPC classification number: A61K31/404 ,  A61K31/4045 ,  A61K31/536 ,  A61K2300/00

Abstract: The present invention relates to an active substance combination comprising at least one compound with neuropeptide Y-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和至少一种具有5-HT 6受体亲和力的化合物的活性物质组合物，包含所述活性物质组合的药物，以及所述活性物质组合物用于 制造药物。

公开(公告)号：US20070043041A1

公开(公告)日：2007-02-22

申请号：US10566101

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: A61K31/5377 ,  A61K31/498 ,  A61K31/454 ,  A61K31/405 ,  C07D413/02 ,  C07D403/02

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

Abstract: The present invention refers to new sulfonamide derivatives, of general formula (la, lb, lc) 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, at any mixing ratio or their salts, preferably the corresponding, physiologically acceptable salts, or corresponding solvates; to the process 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（Ia，1b，1c）的新型磺酰胺衍生物，其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，优选相应的生理上可接受的盐或相应的溶剂合物; 其制备方法，其作为人和/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：US20070032520A1

公开(公告)日：2007-02-08

申请号：US10566094

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

CPC classification number: C04B35/632 ,  C07D209/08 ,  C07D401/12 ,  C07D409/12 ,  C07D417/12 ,  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 salts, preferably the 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.

Abstract translation: 本发明涉及通式（1a，1b，1c）的新磺酰胺衍生物，其任选为其立体异构体之一，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形式， 优选对映体或非对映体，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：US20060258653A1

公开(公告)日：2006-11-16

申请号：US11487745

申请日：2006-07-17

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

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

IPC: A61K31/5377 ,  A61K31/496 ,  A61K31/498 ,  A61K31/454 ,  A61K31/405 ,  C07D413/02 ,  C07D403/02

CPC classification number: C04B35/632 ,  C07D209/14 ,  C07D209/16 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.

公开(公告)号：US20050131049A1

公开(公告)日：2005-06-16

申请号：US11045708

申请日：2005-01-28

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

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

IPC: C07D231/12 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/4196 ,  A61P7/12 ,  A61P13/10 ,  C07D409/06 ,  A61K31/416 ,  C07D49/02

CPC classification number: A61K31/4196 ,  A61K31/40 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164

Abstract: Derivatives of aryl(or heteroaryl)azolylcarbinoles of general formula (I), in which Ar represents a phenyl radical or a thienyl radical, optionally substituted, R1 represents a hydrogen atom or a lower alkyl group, R2 represents a dialkylaminoalkyl or azaheterocylclylalkyl and Het represents an azole unsubstituted or optionally substituted by one or two substituents, and their physiologically acceptable salts; are useful as drugs in human and/or veterinary therapeutics to treat urinary incontinence in mammals, including man.

Abstract translation: 其中Ar表示苯基或噻吩基，任意取代的R 1表示氢原子或低级烷基，R（R 1）表示通式（I）的芳基（或杂芳基）唑基偶氮的衍生物， 代表二烷基氨基烷基或氮杂环己基烯基烷基，Het表示未取代或任选被一个或两个取代基取代的唑类及其生理上可接受的盐; 可用作人类和/或兽医治疗药物以治疗哺乳动物（包括人）中的尿失禁。

公开(公告)号：US06355659B1

公开(公告)日：2002-03-12

申请号：US09492640

申请日：2000-01-27

Applicant: Ramon Merce-Vidal ,  Jordi Frigola-Constansa ,  Blas Andaluz-Mataró ,  Josep Mas-Prió

Inventor： Ramon Merce-Vidal ,  Jordi Frigola-Constansa ,  Blas Andaluz-Mataró ,  Josep Mas-Prió

IPC: A61K314439

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06

Abstract: Antipsychotic compound 4-(4-chlorophenyl)-1,2,3,6-tetrahydro-1-[4-(1H-1,2,4-triazol-1-yl) butyl]pyridine, or one of its physiologically acceptable salts, pharmaceutical compositions containing those compounds and a method of treating a disease selected from psychosis and dementias in which a deficit of cognition predominates comprising administering to a patient in need of such treatment a therapeutically effective amount of the antipsychotic compound.

Abstract translation: 抗精神病药化合物4-（4-氯苯基）-1,2,3,6-四氢-1- [4-（1H-1,2,4-三唑-1-基）丁基]吡啶或其生理上可接受的 盐，含有这些化合物的药物组合物和治疗选自认知缺陷占主导地位的精神病和痴呆症的疾病的方法，包括向需要这种治疗的患者施用治疗有效量的抗精神病化合物。

公开(公告)号：US06232329B1

公开(公告)日：2001-05-15

申请号：US09031024

申请日：1998-02-26

Applicant: Ramon Merce-Vidal ,  Jordi Frigola-Constansa

Inventor： Ramon Merce-Vidal ,  Jordi Frigola-Constansa

IPC: C07D40106

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06

Abstract: The present invention relates to the compounds of general formula used as medicaments possessing therapeutic activity for the treatment of anxiety, psychosis, epilepsy, convulsion, motoricity problems, amnesia, cerebrovascular diseases or senile dementia.

Abstract translation: 本发明涉及具有治疗焦虑，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症的治疗活性的药物的通式的化合物。

公开(公告)号：US5536836A

公开(公告)日：1996-07-16

申请号：US240111

申请日：1994-05-09

Applicant: Ramon Merce-Vidal ,  Jordi Frigola-Constansa

Inventor： Ramon Merce-Vidal ,  Jordi Frigola-Constansa

IPC: A61K31/505 ,  A61P25/00 ,  A61P25/20 ,  A61P25/22 ,  C07D403/12 ,  C07D403/14 ,  C07D401/14

CPC classification number: C07D403/12

Abstract: The present invention relates to a process for the preparation of 2-{4-[4-(4-chloro-1-pyrazolyl)buty1]-1-piperazinyl}pyrimidine (Lesopitron) of formula I: ##STR1## characterized in that the reaction between 2-(1-piperazinyl)pyrimidine, 4-chloropyrazole and the carbon chain of formula (III) ##STR2## in which X and Y, which may be identical or different, represent a suitable leaving group, is carried out in a single step in a suitable solvent.

Abstract translation: 本发明涉及制备式I的2- {4- [4-（4-氯-1-吡唑基）丁基] -1-哌嗪基}嘧啶（Lesopitron）的方法：其特征在于 2-（1-哌嗪基）嘧啶，4-氯吡唑和式（III）的碳链之间的反应（III）其中可以相同或不同的X和Y表示合适的离去基团是 在一个合适的溶剂中进行一步。