US2014194423A1PendingUtilityA1
Combination products
Est. expiryJun 30, 2028(~1.9 yrs left)· nominal 20-yr term from priority
A61P 43/00A61K 31/465A61K 31/4709A61K 31/4545A61K 31/198A61K 45/06A61K 31/4427A61K 31/12A61K 31/404A61K 31/4985A61K 31/444A61K 31/428A61K 31/405A61K 31/4725A61K 31/473A61P 25/16A61K 31/165A61K 31/437A61K 31/5377
46
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Claims
Abstract
The invention concerns the combinations of an mGluR modulator, e.g. an mGluR5 modulator and at least one of L-dopa, a dopamine modulator, e.g. a dopamine agonist, a dopa decarboxylase inhibitor or a catechol-O-methyl transferase inhibitor.
Claims
exact text as granted — not AI-modified1 . The use of an mGluR modulator in combination with at least one of
i) L-dopa, or ii) a dopa decarboxylase inhibitor, or iii) a catechol-O-methyl transferase inhibitor iv) a dopamine agonist or in any case a pharmaceutically acceptable salt thereof; for the treatment, prevention or delay of progression of Parkinson's Disease and/or a disorder associated with Parkinson's Disease.
2 . Use according to claim 1 , wherein the modulator is an mGluR5 modulator.
3 . Use according to claim 1 or claim 2 , wherein the modulator is an mGluR antagonist.
4 . Use according to claim 2 or claim 3 , wherein the modulator is an mGluR5 antagonist.
5 . Use according to any preceding claim, wherein the modulator is a compound of the formula (I)
wherein
R 1 represents optionally substituted alkyl or optionally substituted benzyl; and
R 2 represents hydrogen (H), optionally substituted alkyl or optionally substituted benzyl; or
R 1 and R 2 form together with the nitrogen atom to which they are attached an optionally substituted heterocycle with less than 14 ring atoms;
R 3 represents halogen, alkyl, alkoxy, alkylamino or dialkylamino;
R 4 represents hydroxy (OH), halogen, alkyl or alkoxy;
Q represents CH, CR 4 or N;
V represents CH, CR 4 or N;
W represents CH, CR 4 or N;
X represents CH or N;
Y represents CH, CR 3 or N;
Z represents CH 2 , NH or O; and
provided that Q, V and W are not N at the same time;
in free base or acid addition salt form.
6 . Use according to any of claims 1 to 4 , wherein the modulator is a compound of the formula (II), wherein a compound of the formula (II) is a compound of formula (I) in which at least one of Q, V and W is N, in free base or acid addition salt form.
7 . Use according to any of claims 1 to 4 , wherein the modulator is a compound of the formula (IV) or the formula (V):
wherein
m is 0 or 1,
n is 0 or 1 and
A is hydroxy
X is hydrogen and
Y is hydrogen, or
A forms a single bond with X or with Y;
R 0 is hydrogen, (C 1-4 alkyl, (C 1-4 alkoxy, trifluoromethyl, halogen, cyano, nitro, —COOR 1 wherein R 1 is (C 1-4 )alkyl or —COR 2 wherein R 2 is hydrogen or (C 1-4 alkyl, and
R is —COR 3 , —COOR 3 , —CONR 4 R 5 or —SO 2 R 6 , wherein R 3 is (C 1-4 alkyl, (C 3-7 )cycloalkyl or optionally substituted phenyl, 2-pyridyl or 2-thienyl; R 4 and R 5 , independently, are hydrogen or (C 1-4 alkyl; and R 6 is (C 1-4 )alkyl, (C 3-7 )cycloalkyl or optionally substituted phenyl,
R′ is hydrogen or (C 1-4 )alkyl and
R″ is hydrogen or (C 1-4 )alkyl, or
R′ and R″ together form a group —CH 2 —(CH 2 ) m —
wherein m is 0, 1 or 2, in which case one of n and m is different from 0,
with the proviso that R 0 is different from hydrogen, trifluoromethyl and methoxy when n is 0,
A is hydroxy, X and Y are both hydrogen, R is COOEt and R′ and R″ together form a group —(CH 2 ) 2 —,
OR
wherein
R 1 represents hydrogen or alkyl;
R 2 represents an unsubstituted or substituted heterocycle or
R 2 represents an unsubstituted or substituted aryl;
R 3 represents alkyl or halogen;
X represents a single bond or an alkandiyl-group, optionally interrupted by one or more oxygen atoms or carbonyl groups or carbonyloxy groups;
in free base or acid addition salt form.
8 . Use according to any preceding claim, wherein the disorder is Parkinson's associated levodopa (L-dopa) induced dyskinesia.
9 . Use according to any preceding claim, wherein the disorder is Parkinson's Disease non-L-dopa induced dyskinesia.
10 . Use according to any preceding claim, wherein the Dopa decarboxylase inhibitors are, carbidopa or benserazide.
11 . Use according to any preceding claim, wherein the Catechol-O-methyl transferase inhibitors are tolcapone or entacapone.
12 . Use according to any preceding claim, wherein the Dopamine agonists are bromocriptine, pergolide, pramipexole, ropinirole, cabergoline, apomorphine or lisuride.
13 . A method for the treatment, prevention or delay of progression of Parkinson's Disease and/or a disorder associated with Parkinson's Disease in a subject in need of such treatment, which comprises administering to said subject a therapeutically effective amount of an mGluR modulator.
14 . A method according to claim 13 , wherein the mGluR modulator is as defined in any of claims 2 to 7 .
15 . A method according to claim 13 or claim 14 , wherein the mGluR modulator is an mGluR5 modulator.
16 . A method according to claim 14 , wherein the mGluR modulator is an mGluR5 antagonist.
17 . A method according to any of claims 13 to 16 , wherein the disorder is as defined in claim 8 or claim 9 .
18 . A combination comprising an mGluR modulator or a pharmaceutically acceptable salt thereof, and at least one of
v) L-dopa, or vi) a dopa decarboxylase inhibitor, or vii) a catechol-O-methyl transferase inhibitor viii) a dopamine agonist or in any case a pharmaceutically acceptable salt thereof.
19 . The combination of claim 15 , wherein the mGluR modulator is as defined in any one of claims 2 to 7 .
20 . The combination of claim 15 or 16 , wherein the dopa decarboxylase inhibitor, the catechol-O-methyl transferase inhibitor and the dopamine agonist are as defined in claims 10 , 11 and 12 .
21 . A pharmaceutical composition comprising an mGluR modulator and at least one of
ix) L-dopa, or x) a dopa decarboxylase inhibitor, or xi) a catechol-O-methyl transferase inhibitor xii) a dopamine agonist for the treatment, prevention or delay of progression of Parkinson's Disease and/or a disorder associated with Parkinson's Disease.
22 . A composition according to claim 15 , wherein the mGluR modulator is as defined in any of claims 2 to 7 .
23 . A composition according to claim 15 or claim 16 , wherein the mGluR modulator is an mGluR5 modulator.
24 . A composition according to claim 16 or claim 17 , wherein the mGluR modulator is an mGluR5 antagonist.
25 . A composition according to any of claims 16 to 18 , wherein the disorder is as defined in claim 8 or claim 9 .
26 . A composition according to any of claims 16 to 18 , which is for the treatment, prevention or delay of progression of Parkinson's Disease.
27 . A kit comprising
(a) an amount of an mGluR modulator or a pharmaceutically acceptable salt thereof in a first unit dosage form; (b) an amount of at least one active ingredient selected from L-dopa, or a dopa decarboxylase inhibitor, or a catechol-O-methyl transferase inhibitor, or a dopamine agonist or, in each case, where appropriate, a pharmaceutically acceptable salt thereof; and (c) a container for containing said first, second etc. unit forms; and (d) instructions for using the modulator in the treatment, prevention or delay of progression of Parkinson's Disease and/or a disorder associated with Parkinson's Disease.
28 . A kit according to claim 27 , wherein the mGluR modulator is as defined in any of claims 2 to 7 and wherein the disorder is as defined in claim 8 or claim 9 .Join the waitlist — get patent alerts
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