US2018235974A1PendingUtilityA1
Compounds comprising tricyclic heterocyclic compounds
Est. expiryAug 19, 2035(~9.1 yrs left)· nominal 20-yr term from priority
Inventors:Stephen Joseph ShuttleworthElizabeth Ann BoneFranck Alexandre SilvaAlexander Richard Liam Cecil
A61P 35/00A61P 37/02A61P 37/06A61P 35/02A61P 29/00A61P 19/02A61K 9/2054A61K 9/2018A61K 31/5386A61K 9/2027A61K 31/519A61K 31/5377A61K 9/2095
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Claims
Abstract
The invention relates to a pharmaceutical composition comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and at least one pharmaceutical excipient selected from the group consisting of fillers, binders, disintegrants, glidants and lubricants, wherein the compound according to formula I is represented by:
Claims
exact text as granted — not AI-modified1 . A pharmaceutical composition comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and at least one pharmaceutical excipient selected from the group consisting of fillers, binders, disintegrants, glidants and lubricants, wherein the compound according to formula I is represented by:
wherein:
W is O, N—H, N—(C 1 -C 10 alkyl) or S;
each X is independently CH or N;
R 1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O;
R 2 is LY;
each L is a direct bond, C 1 -C 10 alkylene, C 2 -C 10 alkenylene or C 2 -C 10 alkynylene;
Y is an optionally substituted fused, bridged or spirocyclic non-aromatic 5-12 membered heterocycle containing up to 4 heteroatoms selected from N or O; and
each R 3 is independently H, C 1 -C 10 alkyl, halogen, fluoro C 1 -C 10 alkyl, O— C 1 -C 10 alkyl, NH—C 1 -C 10 alkyl, S—C 1 -C 10 alkyl, O-fluoro C 1 -C 10 alkyl, NH-acyl, NH—C(O)—NH—C 1 -C 10 alkyl, C(O)—NH—C 1 -C 10 alkyl, aryl or heteroaryl.
2 . The composition according to claim 1 , wherein the compound according to formula I is in its succinate salt form.
3 . The composition according to claim 1 , further comprising a surfactant in an amount of from 0.1 to 5 wt % based on the total weight of the composition.
4 . The composition according to claim 1 , wherein the composition is in the form of a tablet or capsule.
5 . The composition according to claim 1 , wherein the composition comprises at least two or at least three pharmaceutical excipients.
6 . The composition according to claim 1 , wherein the compound according to formula I is present in an amount of from 5 to 30 wt % based on the total weight of the composition.
7 . The composition according to claim 1 , wherein a filler is present in an amount of from 10 to 90 wt % based on the total weight of the composition.
8 . The composition according to claim 1 , wherein a binder is present in an amount of from 0.1 to 20 wt % based on the total weight of the composition.
9 . The composition according to claim 1 , wherein a disintegrant is present in an amount of from 1 to 20 wt % based on the total weight of the composition.
10 . The composition according to claim 1 , wherein a lubricant is present in an amount of from 0.5 to 5 wt % based on the total weight of the composition.
11 . The composition according to claim 1 , wherein the composition comprises:
1 to 50 wt % of a compound according to claim 1 ; 10 to 90 wt % of at least one filler; 0.1 to 20 wt % of at least one binder; 1 to 20 wt % of at least one disintegrant; and 0.1 to 10 wt % of at least one lubricant or glidant.
12 . The composition according to claim 1 , wherein R 1 is represented by any of the following structures:
13 . The composition according to claim 1 , wherein R 1 is morpholine.
14 . The composition according to claim 1 , wherein W is O or S.
15 . The composition according to claim 1 , wherein W is O.
16 . The composition according to claim 1 , wherein X is CH.
17 . The composition according to claim 1 , wherein R 3 is H.
18 . The composition according to claim 1 , wherein L is methylene.
19 . The composition according to claim 1 , wherein Y contains two heteroatoms.
20 . The composition according to claim 1 , wherein Y is selected from:
wherein:
A is selected from O, S, NR 4 or optionally substituted C 1 -C 3 alkylene, C 2 -C 3 alkenylene or C 2 -C 3 alkynylene;
B is NR 4 , O or CH 2 ;
wherein R 4 is H or optionally substituted C 1 -C 10 alkyl, C 2 -C 10 alkenyl or C 2 -C 10 alkynyl;
p is selected from 0 or 1;
each m is independently selected from 0, 1 or 2; and
each n is independently selected from 1, 2 or 3.
21 . The composition according to claim 20 , wherein A is methylene.
22 . The composition according to claim 20 , wherein B is O.
23 . A composition according to claim 1 , wherein the compound according to formula I is illustrated by any one of the following structures:
24 .- 28 . (canceled)
29 . A method for the manufacture of a pharmaceutical composition, according to claim 1 , comprising:
a) mixing a compound according to formula I with at least one pharmaceutical excipient selected from the group consisting of fillers, binders, disintegrants, glidants and lubricants to form a blend; b) processing the blend into a pharmaceutical composition; and c) compressing the composition of step (b) in to a tablet.
30 . The method of claim 29 , wherein step (b) further comprises screening to ensure a particle size of less than 500 μm.Cited by (0)
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