Invention Grant
US09181259B2 Substituted pyrrolo[1,2-a]piperazines and pyrrolo[1,2-a][1,4]diazepines as neurokinin 1 receptor antagonists
有权
取代的吡咯并[1,2-a]哌嗪和吡咯并[1,2-a] [1,4]二氮杂卓作为神经激肽1受体拮抗剂
- Patent Title: Substituted pyrrolo[1,2-a]piperazines and pyrrolo[1,2-a][1,4]diazepines as neurokinin 1 receptor antagonists
- Patent Title (中): 取代的吡咯并[1,2-a]哌嗪和吡咯并[1,2-a] [1,4]二氮杂卓作为神经激肽1受体拮抗剂
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Application No.: US14380078Application Date: 2013-02-20
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Publication No.: US09181259B2Publication Date: 2015-11-10
- Inventor: Morten Dahl Sørensen , Romano Di Fabio , Alfonso Pozzan , Maria Pia Catalani , Haakon Bladh , Jakob Felding
- Applicant: LEO PHARMA A/S
- Applicant Address: DK Ballerup
- Assignee: LEO PHARMA A/S
- Current Assignee: LEO PHARMA A/S
- Current Assignee Address: DK Ballerup
- Agency: Birch Stewart Kolasch & Birch, LLP
- International Application: PCT/EP2013/053319 WO 20130220
- International Announcement: WO2013/124286 WO 20130829
- Main IPC: A61K31/4985
- IPC: A61K31/4985 ; A61K31/551 ; C07D241/38 ; C07D243/10 ; C07D487/04 ; A61K31/5377 ; C07D471/20 ; C07D491/20
![Substituted pyrrolo[1,2-a]piperazines and pyrrolo[1,2-a][1,4]diazepines as neurokinin 1 receptor antagonists](/abs-image/US/2015/11/10/US09181259B2/abs.jpg.150x150.jpg)
Abstract:
The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(═O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(═O)R7, C(═O)OR7, C(═O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(═O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ═CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically acceptable salt or solvate thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating or ameliorating pruritic dermal diseases or conditions with said compounds, and to the use of said compounds in the manufacture of medicaments.
Public/Granted literature
- US20150018345A1 NOVEL NEUROKININ 1 RECEPTOR ANTAGONIST COMPOUNDS Public/Granted day:2015-01-15
Information query
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