Title:
置換されたプロピオール酸アミド及び医薬の製造へのその使用
Document Type and Number:
Japanese Patent JP2009522219
Kind Code:
A
Abstract:
Propiolic acid amides (I), optionally as pure stereoisomers, particularly enantiomers or diastereomers, including racemates and mixtures in any proportion, also salts and solvates, are new. Propiolic acid amides of formula (I), optionally as pure stereoisomers, particularly enantiomers or diastereomers, including racemates and mixtures in any proportion, also salts and solvates, are new. R 1>optionally substituted aryl or heteroaryl; a-f : 0 or 1, totaling 1-6; R 2>-R 13>various substituents; M and W : N or C; P : CR 1>4, N, NR 15>, O or S; Q : CR 16>, N, NR 17>, O or S; T : CR 18>, N, NR 19>, O or S; V : CR 20>, N, NR 21>, O or S; g : 0 or 1; R 14>-R 21>various substituents. The full definitions are given in the DEFINITIONS -Full Definitions field. An independent claim is included for several methods for preparing (I). [Image] ACTIVITY : Analgesic; Antimigraine; Antidepressant; Nootropic; Neuroprotective; Antiparkinsonian; Anticonvulsant; Tranquilizer; Antitussive; Uropathic; Antidiarrheal; Antipruritic; Antiasthma; Cerebroprotective; Ophthalmological; Antialcoholic; Antismoking. MECHANISM OF ACTION : Regulation, particularly inhibition, of the mGluR5 receptor. The compound 1-(3-phenylpropiolyl)-2,3-dihydroindole has IC50 against the porcine mGluR5 receptor of 7.94mu M.
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Inventors:
Howland Michael
Sine Claus
Kunert sven
Reich Melanie
Czemolka Zaskia
Sine Claus
Kunert sven
Reich Melanie
Czemolka Zaskia
Application Number:
JP2008547888A
Publication Date:
June 11, 2009
Filing Date:
December 22, 2006
Export Citation:
Assignee:
Grunenthal Gesellschaft Mito Beschlenktel Haftung
International Classes:
C07D209/08; A61K31/4035; A61K31/404; A61K31/437; A61K31/4375; A61K31/47; A61K31/472; A61K31/4725; A61K31/4985; A61K31/55; A61P1/04; A61P1/08; A61P1/12; A61P3/00; A61P3/04; A61P9/10; A61P11/00; A61P11/06; A61P13/02; A61P17/04; A61P21/00; A61P23/00; A61P25/00; A61P25/06; A61P25/08; A61P25/14; A61P25/16; A61P25/22; A61P25/28; A61P25/30; A61P25/32; A61P25/34; A61P25/36; A61P27/02; A61P29/00; A61P35/00; A61P43/00; C07D209/44; C07D215/08; C07D217/06; C07D223/16; C07D401/06; C07D471/04; C07D487/04; C07D498/04; C07B61/00
Foreign References:
| WO2005056524A2 | 2005-06-23 | |||
| WO2000063208A1 | 2000-10-26 | |||
| WO2005115990A1 | 2005-12-08 | |||
| WO1996040640A1 | 1996-12-19 | |||
| WO2000063208A1 | 2000-10-26 |
Attorney, Agent or Firm:
Mitsufumi Esaki
Okumura Yoshimichi
Blacksmith
Okumura Yoshimichi
Blacksmith