Claims
- 1. A compound according to formula I
- 2. A compound according to claim 1 wherein
n is 0; R1 is
(i) C1-10 branched or unbranched alkyl; or, (ii) optionally substituted heteroaryl-C1-6alkyl, said heteroaryl optionally substituted with a substituent selected from the group consisting of C1-3 alkyl, C1-3 alkoxy and halogen, (iii) optionally substituted phenyl or heteroaryl said phenyl or heteroaryl optionally substituted with a substituent selected from the group consisting of C1-3 alkyl, C1-3 alkoxy and halogen; (iv) C1-3 alkyl substituted with a phenyl said phenyl optionally substituted with a substituent selected from the group consisting of C1-3 alkyl, C1-3 alkoxy and halogen; R3 is
(i) hydrogen, (ii) C1-6 alkyl, (iii) C3-7 cycloalkyl-C1-3 alkyl, or, (iv) benzyl optionally substituted with C1-3 alkyl, C1-3 alkoxy or halogen; R4 is optionally substituted phenyl.
- 3. A compound according to claim 2 wherein R1 is
(i) C1-10 branched or unbranched alkyl, (ii) C1-10 alkyl substituted with a phenyl said phenyl optionally substituted, or (iii) heteroaryl-C1-6 alkyl wherein said heteroaryl is2-thienyl, 2-furanyl or 3-indolinyl each of said heteroaryl optionally substituted.
- 4. A compound according to claim 3 wherein R4 is 2,4-disubstituted- or 2,4,6-trisubstituted-phenyl.
- 5. A compound according to claim 1 wherein
n is 1; R1 is
(i) C1-10 branched or unbranched alkyl; or, (ii) optionally substituted heteroaryl-C1-6alkyl, said heteroaryl optionally substituted with a substituent selected from the group consisting of C1-3 alkyl, C1-3 alkoxy and halogen, (iii) optionally substituted phenyl or heteroaryl said phenyl or heteroaryl optionally substituted with a substituent selected from the group consisting of C1-3 alkyl, C1-3 alkoxy and halogen; (iv) C1-3 alkyl substituted with a phenyl said phenyl optionally substituted with a substituent selected from the group consisting of C1-3 alkyl, C1-3 alkoxy and halogen; R3 is
(i) hydrogen, (ii) C1-6 alkyl, (iii) C3-7 cycloalkyl-C1-3 alkyl, or, (iv) benzyl optionally substituted with C1-3 alkyl, C1-3 alkoxy or halogen; R4 is optionally substituted phenyl.
- 6. A compound according to claim 5 wherein R4 is 2,4-disubstituted- or 2,4,6-trisubstituted-phenyl.
- 7. A compound according to claim 1 wherein
n is 2; R1 is
(i) C1-10 branched or unbranched alkyl; or, (ii) optionally substituted heteroaryl-C1-6alkyl, said heteroaryl optionally substituted with a substituent selected from the group consisting of C1-3 alkyl, C1-3 alkoxy and halogen, (iii) optionally substituted phenyl or heteroaryl said phenyl or heteroaryl optionally substituted with a substituent selected from the group consisting of C1-3 alkyl, C1-3 alkoxy and halogen; (iv) C1-3 alkyl substituted with a phenyl said phenyl optionally substituted with a substituent selected from the group consisting of C1-3 alkyl, C1-3 alkoxy and halogen; R3 is
(i) hydrogen, (ii) C1-6 alkyl, (iii) C3-7 cycloalkyl-C1-3 alkyl, or, (iv) benzyl optionally substituted with C1-3 alkyl, C1-3 alkoxy or halogen; R4 is optionally substituted phenyl.
- 8. A compound according to claim 7 wherein R4 is 2,4-disubstituted- or 2,4,6-trisubstituted-phenyl.
- 9. A method for treating a subject having a disease state that is alleviated by treatment with a CRF receptor antagonist, which comprises administering to such a subject a therapeutically effective amount of a compound of formula I:
- 10. The method of claim 9, wherein the disease state is selected from the group consisting of phobias, stress-related illnesses, mood disorders, eating disorders, generalized anxiety disorders, stress-induced gastrointestinal dysfunctions, neurodegenerative diseases, and neuropsychiatric disorders.
- 11. A pharmaceutical composition for treating a subject having a disease state that is alleviated by treatment with a CRF receptor antagonist comprising a therapeutically effective amount of at least one compound of formula I
- 12. A process for the preparation of a compound according to formula I
- 13. A process according to claim 12 further comprising contacting pyrimidine XXVII with base and an alkylating agent to afford the tertiary amine XXVIII:
- 14. A process according to claim 12 further comprising contacting a lactam according to formula XXVIII wherein X1 is C═O with a reducing agent to afford the amine wherein X1 is CH2.
CROSS REFERENCE TO PRIOR APPLICATION
[0001] This application claims benefit under Title 35 U.S.C. 119(e) of U.S. Provisional Application No. 60/468,878, filed May 5, 2003, which is hereby incorporated by reference in its entirety
Provisional Applications (1)
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Number |
Date |
Country |
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60468878 |
May 2003 |
US |