公开(公告)号：US20020188017A1

公开(公告)日：2002-12-12

申请号：US10139674

申请日：2002-05-06

Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.

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

IPC: C07D49/02

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.

Abstract translation: 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。

公开(公告)号：US20030022925A1

公开(公告)日：2003-01-30

申请号：US10189915

申请日：2002-07-03

Applicant: Laboratorios del Dr. Esteve, S.A.

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

IPC: A61K031/4196 ,  A61K031/4164 ,  A61K031/415 ,  A61K031/40

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. 1

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 2表示二烷基氨基烷基或氮杂环己基烯基烷基，Het表示芳基（或杂芳基）唑基偶氮衍生物， 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：US20040162324A1

公开(公告)日：2004-08-19

申请号：US10779287

申请日：2004-02-13

Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.

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

IPC: A61K031/4196 ,  A61K031/4178 ,  C07D49/02

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.

Abstract translation: 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。