Claims
- 1. A compound of formula I:
- 2. The compound according to claim 1, wherein:
U is selected from a valence bond, —N(R)—, —S—, —O—, —N(R)N(R)—, —N(R)—O—, —O—N(R)—, a C1-4 alkylidene chain, —N(R)CO—, or —N(R)CO2—, or:
U—R1 and Rx are taken together to form an optionally substituted 5-6 membered saturated, partially unsaturated, or fully unsaturated ring having 0-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R1 is selected from R, Ar, —(CH2)yCH(R5)R3, or —(CH2)yCH(R5)CH(R3)2; Q is a C1-4 alkylidene chain wherein one methylene unit of Q is replaced by —C(O)—, —CO2—, —C(O)N(R)—, —SO2—, —SO2N(R)—, —OC(O)N(R)—, —C(O)ON(R)—, or —C(O)N(R)N(R)—; and R2 is —(CH2)yR3, —(CH2)yCH(R3)2, —(CH2)yCH(R5)CH(R3)2, or —(CH2)yN(R6)2.
- 3. The compound according to claim 1, wherein said compound is of formula II or II′:
- 4. The compound according to claim 3, wherein said compound is of formula III or III′:
- 5. The compound according to claim 3, wherein said compound is of formula formula IV or IV′:
- 6. The compound according to either of claims 4 or 5 wherein:
U is selected from a valence bond, —N(R)—, —S—, —O—, —N(R)N(R)—, —N(R)—O—, —O—N(R)—, a C1-4 alkylidene chain, —N(R)CO—, or —N(R)CO2—, or:
U—R1 and Rx are taken together to form an optionally substituted 5-6 membered saturated, partially unsaturated, or fully unsaturated ring having 0-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R1 is selected from R, Ar, —(CH2)yCH(R5)R3, or —(CH2)yCH(R5)CH(R3)2; and each R3 is independently selected from R, OR4, Ar, CO2R4, —(CH2)N(R6)2, or CN.
- 7. A compound according to claim 1, wherein said compound is selected from the group consisting of:
- 8. A composition comprising an effective amount of a compound according to claim 1, and a pharmaceutically acceptable carrier, adjuvant, or vehicle.
- 9. The composition according to claim 8, additionally comprising a therapeutic agent selected from an anti-proliferative agent, an anti-inflammatory agent, an immunomodulatory agent, a neurotrophic factor, an agent for treating cardiovascular disease, an agent for treating liver disease, an anti-viral agent, an agent for treating blood disorders, an agent for treating diabetes, or an agent for treating immunodeficiency disorders.
- 10. A method of inhibiting ERK2, GSK3, PKA, or CDK2 kinase activity in a biological sample comprising the step of contacting said biological sample with:
a) a compound according to claim 1; or b) a composition according to claim 8.
- 11. A method of inhibiting ERK2, GSK3, PKA, or CDK2 kinase activity in a patient comprising the step of administering to said patient:
a) a compound according to claim 1; or b) a composition according to claim 8.
- 12. A method for treating, or lessening the severity of, a disease or condition selected from allergy, asthma, diabetes, Alzheimer's disease, Huntington's disease, Parkinson's disease, AIDS-associated dementia, amyotrophic lateral sclerosis (AML, Lou Gehrig's disease), multiple sclerosis (MS), schizophrenia, cardiomyocyte hypertrophy, reperfusion/ischemia, stroke, or baldness, wherein said method comprises administering to a patient in need thereof an effective amount of the composition according to claim 8.
- 13. The method according to claim 11, wherein said disease or condition is stroke.
- 14. A method for treating or lessening the severity of a neurodegenerative or neurological disorder, wherein said method comprises administering to a patient in need thereof an effective amount of the composition according to claim 8.
- 15. A method for treating or lessening the severity of a proliferative disorder, a cardiac disorder, an inflammatory disorder, an autoimmune disorder, a viral disease, or a bone disorder, wherein said method comprises administering to a patient in need thereof an effective amount of the composition according to claim 8.
- 16. A method for treating or lessening the severity of cancer, wherein said method comprises administering to a patient in need thereof an effective amount of the composition according to claim 8.
- 17. The method according to claim 16, wherein said cancer is selected from brain (gliomas), breast, colon, head and neck, kidney, lung, liver, melanoma, ovarian, pancreatic, prostate, sarcoma, or thyroid.
- 18. The method according to claim 12, comprising the additional step of administering to said patient an additional therapeutic agent selected from an anti-proliferative agent, an anti-inflammatory agent, an immunomodulatory agent, a neurotrophic factor, an agent for treating cardiovascular disease, an agent for treating liver disease, an anti-viral agent, an agent for treating blood disorders, an agent for treating diabetes, or an agent for treating immunodeficiency disorders, wherein:
said additional therapeutic agent is appropriate for the disease being treated; and said additional therapeutic agent is administered together with said composition as a single dosage form or separately from said composition as part of a multiple dosage form.
Priority Claims (1)
Number |
Date |
Country |
Kind |
PCT/US03/40512 |
Dec 2003 |
WO |
|
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application claims priority to U.S. Provisional Patent Application Ser. No. 60/445,962 filed Feb. 7, 2003 and U.S. Provisional Patent Application Ser. No. 60/463,847 filed Apr. 18, 2003, the contents of which are incorporated herein by reference.
Provisional Applications (2)
|
Number |
Date |
Country |
|
60445962 |
Feb 2003 |
US |
|
60463847 |
Apr 2003 |
US |