摘要:
The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.
摘要翻译:本发明提供式I化合物:其中R 1是烷基,苯基,杂环基,环烷基,烷氧基,酯,氨基或酰胺基; R 2是苯基,杂环基,烷基,环烷基或环烷基烷基; R 3是烷基,环烷基,环烷基烷基,氨基或杂环基; R 4和R 5是氢或烷基或形成环烷基环; A是O或N; m为零或一; 作为GlyT1的抑制剂,因此可用于治疗或预防精神分裂症等疾病; 提供药物组合物,第一和第二医疗用途和治疗方法。
摘要:
The present invention is directed to pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
摘要:
The present invention provides compounds of formula (I), wherein both p's are one or two, R1 is generally heteroaryl or cycloalkyl, R2 is C3-6cycloalkyl or phenyl and R3 is heteroaryl, and pharmaceutically acceptable salts thereof, as GlyT1 inhibitors for treating schizophrenia, pharmaceutical compositions comprising the same and methods for their preparation.
摘要:
A class of 4-phenylpyridazine derivatives of Formula (I), being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译:一类式(I)的4-苯基哒嗪衍生物,作为GABA A A受体的选择性配体,特别是对α2和/或α3和α5亚基具有高亲和力,因此具有益处 在治疗和/或预防中枢神经系统的不利条件,包括焦虑,抽搐和认知障碍。
摘要:
A class of 8-fluoroimidazo[1,2-α]pyridine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译:一类由任选取代的五元或六元杂芳环在3-位被取代的8-氟咪唑并[1,2-α]吡啶衍生物,是GABA A A受体的选择性配体 特别是对α2和/或α3和/或α5亚基具有高亲和力,因此有益于治疗和/或预防中枢神经系统的不利条件,包括焦虑,抽搐和认知障碍。
摘要:
The present invention is directed to pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
摘要:
The present invention relates to novel thienopyhmidine compounds of general formula (I), pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
摘要:
The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
摘要:
The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
摘要:
Compounds of formula (I) act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for treating and/or preventing broncho-obstructive and inflammatory diseases.