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US 2016/0250342 A1Published application
Hydrazinyl-Indole Compounds and Methods for Producing a Conjugate
AssigneeRedwood Bioscience, Inc.
InventorsRomas Alvydas Kudirka, Aaron Edward Albers, Robyn M. Barfield, David Rabuka
Life of this patent
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Abstract
The present disclosure provides conjugate structures (e.g., polypeptide conjugates) and hydrazinyl-indole compounds used to produce these conjugates. The disclosure also provides methods of production of such conjugates, as well as methods of using the same.
Claims27
A conjugate comprising:
- at least one modified amino acid residue of formula (I):
- wherein
- n is 0 or 1;
- R1 is selected from hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl;
- R2 and R3 are each independently selected from hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, amino, substituted amino, carboxyl, carboxyl ester, acyl, acyloxy, acyl amino, amino acyl, alkylamide, substituted alkylamide, sulfonyl, thioalkoxy, substituted thioalkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl;
- X1, X2, X3 and X4 are each independently selected from C, N, O and S;
- X5 is C;
- Y1, Y2, Y3, Y4 and Y5 are each independently selected from hydrogen, halogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, amino, substituted amino, carboxyl, carboxyl ester, acyl, acyloxy, acyl amino, amino acyl, alkylamide, substituted alkylamide, sulfonyl, thioalkoxy, substituted thioalkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl;
- Q1 is a bond to either X4 or X5, wherein if Q1 is a bond to X4, then Y4 is absent, or if Q1 is a bond to X5, then Y5 is absent;
- and
- L is an optional linker,
- wherein one of W1 and W2 is a polypeptide and the other is a drug or a detectable label.
9 more elements
-18. (canceled)
A compound of formula (IV):
- wherein
- one of Q2 and Q3 is —(CH2)nNR3NHR2 and the other is Y4;
- n is 0 or 1;
- R2 and R3 are each independently selected from hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, amino, substituted amino, carboxyl, carboxyl ester, acyl, acyloxy, acyl amino, amino acyl, alkylamide, substituted alkylamide, sulfonyl, thioalkoxy, substituted thioalkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl;
- X1, X2, X3 and X4 are each independently selected from C, N, O and S;
- Y1, Y2, Y3 and Y4 are each independently selected from hydrogen, halogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, amino, substituted amino, carboxyl, carboxyl ester, acyl, acyloxy, acyl amino, amino acyl, alkylamide, substituted alkylamide, sulfonyl, thioalkoxy, substituted thioalkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl;
- L is an optional linker;
- and
- W1 is selected from a drug, a detectable label and a polypeptide.
6 more elements
-43. (canceled)
Dependencies are inferred from the claim text.