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US 6,747,042 B2Granted
N-heterocyclic derivatives
AssigneeVertex Pharmaceuticals Incorporated
InventorsDavid Lauffer, Brian Ledford, Michael Mullican
Life of this patent
Estimating the term…
Abstract
The present invention relates N-heterocyclic derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.
Claims12
A compound having formula (I):
- and pharmaceutically acceptable derivatives thereof, wherein:
- X is O;
- A is phenyl
- B is hydrogen;
- wherein 1 to 4 hydrogen atoms in A are optionally and independently replaced with halogen, hydroxyl, hydroxymethyl, nitro, SO3H, trifluoromethyl, trifluoromethoxy, (C1-C6)-straight or branched alkyl, (C2-C6)-straight or branched alkenyl, O—[(C1-C6)-straight or branched alkyl], O—[(C3-C6)-straight or branched alkenyl], (CH2)n—N(R4)(R5), (CH2)n—NH(R4)—(CH2)n—Z, (CH2)n—N(R4—(CH2)n—Z)(R5—(CH2)n—Z), (CH2)n—Z, O—(CH2)n—Z, (CH2)nO—Z, S—(CH2)n—Z, CH═CH—Z, 1,2-methylenedioxy, C(O)OH, C(O)O—[(C1-C6)-straight or branched alkyl], C(O)O—(CH2)n—Z or C(O)—N(R4)(R5);
- wherein each of R4 and R5 are independently hydrogen, (C1-C6)-straight or branched alkyl, (C3-C5)-straight or branched alkenyl, or wherein R4 and R5, when bound to the same nitrogen atom, are taken together with the nitrogen atom to form a 5 or 6 membered ring, wherein said ring optionally contains 1 to 3 additional heteroatoms independently selected from N, O or S;
- wherein said alkyl, alkenyl or alkynyl groups in R4 and R5 are optionally substituted with Z.
- each n is independently 0 to 4;
- each Z is independently selected from a saturated, partially saturated or unsaturated, monocyclic or bicyclic ring system, wherein each ring contains 5 to 7 ring atoms independently selected from C, N, O or S;
- and wherein no more than 4 ring atoms are selected from N, O or S;
- wherein 1 to 4 hydrogen atoms in Z are optionally and independently replaced with halo, hydroxy, nitro, cyano, C(O)OH, (C1-C3)-straight or branched alkyl, O—(C1-C3)-straight or branched alkyl, C(O)O—[(C1-C3)-straight or branched alkyl], amino, NH[C1-C3)-straight or branched alkyl], or N—[(C1-C3)-straight or branched alkyl]2;
- K is hydrogen
- J and D are taken together with the nitrogen atom, form 1,2,3,4-tetrahydroisoquinolin-2-yl ring;
- wherein 1 to 4 hydrogen atoms in said ring are optionally and independently replaced with (C1-C6)-straight or branched alkyl, (C2-C6)-straight or branched alkenyl or alkynyl, oxo, hydroxyl or Z.
11 more elements
A compound having formula:
Dependencies are inferred from the claim text.