Mediators of hedgehog signaling pathways, compositions and uses related thereto
First Claim
Patent Images
1. A pharmaceutical preparation comprising a sterile pharmaceutical excipient and a compound represented by the general formula (V):
-
wherein, as valence permits,Y is O or S;
Z′
is SO2, —
(C═
S)—
, —
(C═
O)—
, —
(C═
NH)—
, or SO;
q and r represent, independently for each occurrence, an integer from 0 to 2;
V is absent or represents O, S, or NR8;
G is absent or represents —
C(═
O)—
or —
SO2—
;
J, independently for each occurrence, represents H or substituted or unsubstituted lower alkyl or alkylene attached to NC(═
Y), such that both occurrences of N adjacent to J are linked through at least one occurrence of J, and R9, independently for each occurrence, is absent or represents H or lower alkyl, or two occurrences of J or one occurrence of J taken together with one occurrence of R9, forms a ring of from 5 to 8 members, which ring includes one or both occurrences of N;
R5 represents substituted or unsubstituted alkyl (branched or unbranched), alkenyl (branched or unbranched), alkynyl (branched or unbranched), cycloalkyl, or cycloalkylalkyl;
R6 represents substituted or unsubstituted aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, heterocyclylalkyl, cycloalkyl, or cycloalkylalkyl; and
R7 represents substituted or unsubstituted aryl, aralkyl, heteroaryl, or heteroaralkyl.
3 Assignments
0 Petitions
Accused Products
Abstract
The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.
72 Citations
43 Claims
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1. A pharmaceutical preparation comprising a sterile pharmaceutical excipient and a compound represented by the general formula (V):
-
wherein, as valence permits, Y is O or S;
Z′
is SO2, —
(C═
S)—
, —
(C═
O)—
, —
(C═
NH)—
, or SO;
q and r represent, independently for each occurrence, an integer from 0 to 2;
V is absent or represents O, S, or NR8;
G is absent or represents —
C(═
O)—
or —
SO2—
;
J, independently for each occurrence, represents H or substituted or unsubstituted lower alkyl or alkylene attached to NC(═
Y), such that both occurrences of N adjacent to J are linked through at least one occurrence of J, andR9, independently for each occurrence, is absent or represents H or lower alkyl, or two occurrences of J or one occurrence of J taken together with one occurrence of R9, forms a ring of from 5 to 8 members, which ring includes one or both occurrences of N;
R5 represents substituted or unsubstituted alkyl (branched or unbranched), alkenyl (branched or unbranched), alkynyl (branched or unbranched), cycloalkyl, or cycloalkylalkyl;
R6 represents substituted or unsubstituted aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, heterocyclylalkyl, cycloalkyl, or cycloalkylalkyl; and
R7 represents substituted or unsubstituted aryl, aralkyl, heteroaryl, or heteroaralkyl. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 23, 32, 36, 37, 38, 39, 40, 41, 42, 43)
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-
19. A pharmaceutical preparation comprising a sterile pharmaceutical excipient and a compound represented by the general formula (VI):
-
wherein, as valence permits, Y is O or S;
Z′
is SO2, —
(C═
S)—
, —
(C═
O)—
, —
(C═
NH)—
, or SO;
V is absent or represents O, S, or NR8;
G is absent or represents —
C(═
O)—
or —
SO2—
;
J, independently for each occurrence, represents H or substituted or unsubstituted lower alkyl or alkylene attached to NC(═
Y), such that both occurrences of N adjacent to J are linked through at least one occurrence of J, andR9, independently for each occurrence, is absent or represents H or lower alkyl, or two occurrences of J or one occurrence of J taken together with one occurrence of R9, forms a ring of from 5 to 8 members, which ring includes one or both occurrences of N;
R5 represents substituted or unsubstituted alkyl (branched or unbranched), alkenyl (branched or unbranched), alkynyl (branched or unbranched), cycloalkyl, or cycloalkylalkyl;
R6 represents substituted or unsubstituted aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, heterocyclylalkyl, cycloalkyl, or cycloalkylalkyl; and
R7 represents substituted or unsubstituted aryl, aralkyl, heteroaryl, or heteroaralkyl. - View Dependent Claims (20, 21, 22, 24, 25, 26, 27, 28, 29, 30, 31, 33, 34, 35)
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Specification