Invention Grant
US07750049B2 O-substituted-dibenzyl urea-derivatives as TRPV1 receptor antagonists
有权
O-取代二苄基脲衍生物作为TRPV1受体拮抗剂
- Patent Title: O-substituted-dibenzyl urea-derivatives as TRPV1 receptor antagonists
- Patent Title (中): O-取代二苄基脲衍生物作为TRPV1受体拮抗剂
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Application No.: US12519753Application Date: 2007-12-06
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Publication No.: US07750049B2Publication Date: 2010-07-06
- Inventor: Pier Giovanni Baraldi , Pier Andrea Borea , Pierangelo Geppetti , Francesca Fruttarolo , Maria Giovanna Pavani , Marcello Trevisani
- Applicant: Pier Giovanni Baraldi , Pier Andrea Borea , Pierangelo Geppetti , Francesca Fruttarolo , Maria Giovanna Pavani , Marcello Trevisani
- Applicant Address: IT Ferrara
- Assignee: Pharmeste S.R.L.
- Current Assignee: Pharmeste S.R.L.
- Current Assignee Address: IT Ferrara
- Agency: Steinfl & Bruno
- Priority: EP06026533 20061221
- International Application: PCT/IB2007/003784 WO 20071206
- International Announcement: WO2008/075150 WO 20080626
- Main IPC: A61K31/535
- IPC: A61K31/535 ; A61K31/497 ; A61K31/44 ; A61K31/335 ; A61K31/195 ; A61K31/17

Abstract:
The invention relates to compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-carboxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl. R2 is te/t-butyl or trifluoromethyl; R3 is independently selected from hydrogen, carboxy, cyano, alkyl or hydroxyalkyl, The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, hemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.
Public/Granted literature
- US20100105740A1 O-SUBSTITUTED-DIBENZYL UREA-DERIVATIVES AS TRPV1 RECEPTOR ANTAGONISTS Public/Granted day:2010-04-29
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