التفاصيل البيبلوغرافية
| العنوان: |
CONJUGATED SMALL MOLECULES |
| Document Number: |
20100048890 |
| تاريخ النشر: |
February 25, 2010 |
| Appl. No: |
12/495526 |
| Application Filed: |
June 30, 2009 |
| مستخلص: |
Provided herein are linker compounds and conjugates that include the linker compounds. In one embodiment, the linker compounds comprise 2 or 3 residues of 6-aminohexanoic acid and optionally 7-10 residues of polyethyleneglycol (PEG). The linker compounds are useful in forming conjugates with one or more components useful in biopharmaceutical or bioanalytical applications. In particular, the biopharmaceutically useful compounds are kinase inhibitors. The conjugates described herein have utility in a variety of diagnostic, separation, and therapeutic applications. |
| Inventors: |
Grotzfeld, Robert M. (Carlsbad, CA, US); Milanov, Zdravko V. (San Diego, CA, US); Patel, Hitesh K. (Encinitas, CA, US); Lai, Andiliy G. (San Diego, CA, US); Mehta, Shamal A. (San Diego, CA, US); Lockhart, David J. (Del Mar, CA, US) |
| Claim: |
1. A compound having a formula: A-(X1—(CR1R2)p—C(═X2))n—X3-T1-(CR3R4X4CR5R6)m-T2-L-B (FORMULA A1) wherein: B is selected from: [chemical expression included] A is biotin, a biotinyl group or a derivative of a biotinyl group; X1, X2, X3, and X4 are independently selected from the group consisting of O, S, and NH; R1, R2, R3, R4, R5, R6, R7, and R8, are each independently selected from a group consisting of hydrogen, halogen, or lower alkyl; T1 and T2 are each independently selected from a group consisting of (CH2)r, a bond or triazole; L is a bond or a moiety comprising a —NH— group; p is 1, 2, 3, 4, 5, or 6; n is 0, 1, 2, 3, 4, 5, or 6; r is 1, 2, 3, 4, 5, or 6; and m is 4 to 20. |
| Claim: |
2. The compound of claim 1, wherein L is a moiety comprising an —NH—C(O)— group. |
| Claim: |
3. The compound of claim 1, wherein L is selected from the group consisting of —NH—, —C(O)NH—, —NHC(O)NH—, and —C(O)CH2CH2C(O)NH—. |
| Claim: |
4. The compound of claim 1, wherein p is 5. |
| Claim: |
5. The compound of claim 1, wherein p is 5; n is 1, 2, or 3; and m is 6, 7, 8, 9, or 10. |
| Claim: |
6. The compound of claim 1, wherein A is: [chemical expression included] |
| Claim: |
7. The compound of claim 1, wherein X2 is O. |
| Claim: |
8. The compound of claim 1, wherein X4 is O. |
| Claim: |
9. The compound of claim 1, wherein T2 is CH2. |
| Claim: |
10. The compound of claim 1, wherein T1 is triazole. |
| Claim: |
11. The compound of claim 1 selected from: [chemical expression included] [chemical expression included] |
| Claim: |
12. A compound having formula: [chemical expression included] |
| Current U.S. Class: |
540/545 |
| Current International Class: |
07; 07; 07 |
| رقم الانضمام: |
edspap.20100048890 |
| قاعدة البيانات: |
USPTO Patent Applications |