PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS, PHARMACEUTICAL COMPOSITION SHOWING ABILITY TO INHIBIT GABA RECEPTORS, AND DRUG FOR TREATING AND PREVENTING DISORDERS ASSOCIATED WITH GABA RECEPTOR INHIBITION Russian patent published in 2012 - IPC C07D487/04 A61K31/519 A61P25/20 A61P25/08 A61P25/22 

Abstract RU 2458063 C2

FIELD: medicine, pharmaceutics.

SUBSTANCE: pyrazolo[1,5-a]-pyrimidine compounds according to the invention are specified in a group consisting of: N-{2-fluor-5-[3-nitro-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-fluor-5-[3-cyano-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-chlor-5-[3-nitro-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-chlor-5-[3-cyano-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-fluor-5-[3-nitro-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-ethylmethanesulphonamide; {2-fluor-5-[3-cyano-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylmethanesulphonamide, N-{2-chlor-5-[3-nitro-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylmethanesulphonamide, N-{2-chlor-5-[3-cyano-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylmethanesulphonamide, N-{2-fluor-5-[3-cyano-2-methyl-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-chlor-5-[3-cyano-2-methyl-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-fluor-5-[3-cyano-2-methyl-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-methanesulphonamide, N-{2-chlor-5-[3-cyano-2-methyl-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-methanesulphonamide, N-{2-methyl-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2-methoxy-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide, N-{2,4-difluor-5-[3-(thiophene_2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide and N-{5-fluor-2-methoxy-3-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methylacetamide.

EFFECT: preparing pyrazolo[1,5-a]pyrimidine compounds, their pharmaceutically acceptable salts and hydrates showing an ability to inhibit GABAA receptors, and applicable for treating and preventing anxiety, epilepsy and sleeping disorders, including insomnia, as well as for inducing a sedative-hypnotic, analgesic and sleeping effects and myorelaxation.

14 cl, 6 tbl, 4 dwg, 22 ex

Similar patents RU2458063C2

Title Year Author Number
HALOGENISED PYRAZOLO[1,5-a]PYRIMIDINES (VERSIONS), METHODS FOR PREPARING THEM, BASED PHARMACEUTICAL COMPOSITION, INTERMEDIATE COMPOUNDS AND METHOD FOR PREPARING THEM (VERSIONS) 2006
  • Anglada Luis
  • Gul'Etta Antonio
  • Palomer Al'Bert
RU2478101C2
TRIAZOLE DERIVATIVES AS GABA RECEPTOR LIGANDS 2011
  • Gebriel Stiven Dims
  • Tomas Endrju
RU2582337C2
NOVEL LIGANDS OF ESTROGEN RECEPTORS 2009
  • Rennstad Patrik
  • Kallin Ehlizabet
  • Apel'Kvist Tereza
  • Vennerstol Mattias
  • Chen Aipin
RU2492164C2
AMINOPYRAZOLOPYRIMIDINE COMPOUND USED AS INHIBITOR OF TYROSINE KINASE RECEPTOR OF NEUROTROPHIC FACTOR 2017
  • Zhu Li
  • Hu Yuandong
  • Wu Wei
  • Dai Liguang
  • Duan Xiaowei
  • Yang Yanqing
  • Sun Yinghui
  • Han Yongxin
  • Peng Yong
  • Kong Fansheng
  • Luo Hong
  • Yang Ling
  • Xu Hongjiang
  • Guo Meng
  • Wang Shanchun
  • Zhong Zhaobai
RU2764523C2
THIAZOLOPYRIMIDINONES AS MODULATORS OF NMDA RECEPTOR ACTIVITY 2014
  • Yuj Tszyan
  • U Goshen
  • Yuen Po-Vaj
  • Villemur Eliziya
  • Shvarts Yakob
  • Li Kuon
  • Sellers Bendzhamin
  • Volgraf Metyu
RU2703273C2
2,6-SUBSTUTED-4-MONOSUBSTITUTED AMINO-PYRIMIDINES AS PROSTAGLANDIN D2 RECEPTOR ANTAGONISTS 2005
  • Lim Sungtaek
  • Kharris Kejt Dzhon
  • Stefani Dehvid
  • Gardner Charl'Z Dzh.
  • Tsao Bin
  • Boffi Rehj
  • Gillespi Timoti A.
  • Agiar Zhuasi K.
  • Khant Khejzel Dzh.
  • Desho Ehl'Za A.
RU2417990C2
NEW PYRIMIDINE DERIVATIVE WITH AN EFFECT OF INHIBITING GROWTH OF CANCER CELLS AND PHARMACEUTICAL COMPOSITION CONTAINING IT 2018
  • Kim, Sung-Eun
  • Lee, Sunho
  • Rajesh, Rengasamy
  • Kang, Dae Ho
  • Ryu, Hyung Chul
  • Kim, Jae-Sun
  • Lee, Sangryul
  • Kim, Kyong Cheol
  • Rho, Jin Kyung
  • Lee, Jae Cheol
RU2744168C1
ARYL- AND HETEROARYL-SUBSTITUTED TETRAHYDROISOQUINOLINES AND USE THEREOF FOR INHIBITING NOREPINEPHRINE, DOPAMINE AND SEROTONIN REUPTAKE 2005
  • Molino Brjus F.
  • Lju Shuan
  • Berkovits Behrri A.
  • Gazzo Piter R.
  • Bek Dzhejms P.
  • Kokhen Marlin
RU2388751C2
NOVEL 1,2-BIS-SULPHONAMIDE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR 2011
  • Yuan Khajtsin
  • Bird Richard L.
  • Lyu Syaosya
  • Donello Dzhon E.
  • Visvanat Veena
  • Garst Majkl E.
RU2654213C9
AMINOPYRIMIDINE DERIVATIVES AND USE THEREOF AS AROMATIC HYDROCARBON RECEPTOR MODULATORS 2021
  • Park, Jung-Sang
  • Cha, Daewon
  • Lee, Wonhyung
  • Joo, Min Sung
  • Yoon, Taeyoung
  • Doh, Hyounmie
  • Sung, Hyun Jung
  • Lee, Bo Ryeong
  • Song, Seunghyun
  • Kim, Yoonjung
  • Choi, Ji Hoon
  • Jung, Hyeon Seok
RU2826628C1

RU 2 458 063 C2

Authors

Anglada Luis

Gul'Etta Antonio

Palomer Al'Bert

Dates

2012-08-10Published

2007-08-02Filed