Title:
TETRAHYDROPYRROLE COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/129025
Kind Code:
A1
Abstract:
The present invention discloses a tetrahydropyrrole compound, a preparation method therefor, a pharmaceutical composition containing the same, and a use thereof. The tetrahydropyrrole compound of the present invention is represented by general formula (I). The tetrahydropyrrole compound of the present invention has better inhibitory effects on the positive symptoms of schizophrenia, and the potency thereof is equivalent to or slightly stronger than that of the positive drug olanzapine. In addition, the compound of the present invention has dual inhibitory effects on D2 receptors and DAT receptors, and is effective for treating schizophrenia and improving negative symptoms and cognitive functions, while also reducing vertebral side effects and prolactin secretion.
Inventors:
DANG ZHU (CN)
CAI CHRISTINE JUE (CN)
LUO ZHEN (CN)
WANG LIUGANG (CN)
BAO DAN (CN)
CAI CHRISTINE JUE (CN)
LUO ZHEN (CN)
WANG LIUGANG (CN)
BAO DAN (CN)
Application Number:
PCT/CN2018/123751
Publication Date:
July 04, 2019
Filing Date:
December 26, 2018
Export Citation:
Assignee:
MEDICONNS SHANGHAI BIOPHARMACEUTICAL CO LTD (CN)
International Classes:
A61P25/18; C07D487/04; C07D493/04; C07D495/04; C07D498/04; C07D513/00
Domestic Patent References:
| WO2012074912A1 | 2012-06-07 | |||
| WO2011050245A1 | 2011-04-28 | |||
| WO2008063670A1 | 2008-05-29 |
Foreign References:
| US20120157479A1 | 2012-06-21 | |||
| CN201711435683A | 2017-12-26 |
Other References:
DONALD M. N ET AL.: "Synthesis and evaluation of ligands for D2-like receptors:The role of common pharmacophoric groups", BIOORGANIC & MEDICINAL CHEMISTRY, vol. 17, no. 4, 31 December 2009 (2009-12-31), pages 1716 - 1723, XP025949581
PAUL L. FELDMAN ET AL.: "Phosphodiesterase Type IV Inhibition. Structure - Activity Relationships of 1, 3-Disubstituted Pyrrolidines", JOURNAL OF MEDICINAL CHEMISTRY, vol. 38, no. 9, 31 December 1995 (1995-12-31), pages 1505 - 1510, XP002064439
YANG FEI-PU; HE YANG; WANG ZHEN; WANG YU; JIANG XIANG-RUI; SHEN JING-SHAN: "Research Progress of Antipsychotics", ACTA PHARMACEUTICA SINICA, vol. 12, no. 51, 12 December 2016 (2016-12-12), pages 1809 - 1821, XP009522624, DOI: 10.16438/j.0513-4870.2016-0449
KULAGOWSKI ET AL., J. MED. CHEM., vol. 39, 1996, pages 1941 - 1942
SIKAZWE ET AL., BIOORG. MED. CHEM., vol. 17, 2009, pages 1716 - 1723
See also references of EP 3733670A4
PAUL L. FELDMAN ET AL.: "Phosphodiesterase Type IV Inhibition. Structure - Activity Relationships of 1, 3-Disubstituted Pyrrolidines", JOURNAL OF MEDICINAL CHEMISTRY, vol. 38, no. 9, 31 December 1995 (1995-12-31), pages 1505 - 1510, XP002064439
YANG FEI-PU; HE YANG; WANG ZHEN; WANG YU; JIANG XIANG-RUI; SHEN JING-SHAN: "Research Progress of Antipsychotics", ACTA PHARMACEUTICA SINICA, vol. 12, no. 51, 12 December 2016 (2016-12-12), pages 1809 - 1821, XP009522624, DOI: 10.16438/j.0513-4870.2016-0449
KULAGOWSKI ET AL., J. MED. CHEM., vol. 39, 1996, pages 1941 - 1942
SIKAZWE ET AL., BIOORG. MED. CHEM., vol. 17, 2009, pages 1716 - 1723
See also references of EP 3733670A4
Attorney, Agent or Firm:
SHANGHAI BESHINING LAW OFFICE (CN)
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