Reverse-turn mimetics and methods relating thereto

Title: Reverse-turn mimetics and methods relating thereto

Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms Doai, Hetero Ring Is Six-membered And Includes At Least Nitrogen And Sulfur As Ring Members, Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos (e.g., 1,3- And 1,4- Benzothiazines, Etc.)

Brief Patent Description - Full Patent Description - Patent Claims

The Patent Description & Claims data below is from USPTO Patent Application 20060079517, Reverse-turn mimetics and methods relating thereto.

1. A method for treating a central nervous system disorder comprising administering to an animal in need thereof an effective amount of a compound having the structure: or pharmaceutically acceptable salt or stereoisomer thereof, wherein A is --(CR.sub.2R.sub.2a).sub.m-- where m is 1, 2 or 3; B is --(CR.sub.3R.sub.3a).sub.n-- where n is 1, 2, 3 or 4; X is --N(R.sub.4)--, --O--, or --S--; R.sub.2 and R.sub.3 are, at each occurrence, the same or different and independently an amino acid side chain moiety or amino acid side chain derivative, a peptide or peptide derivative, a linker or a solid support; R.sub.5 is an amino acid side chain moiety or amino acid side chain derivative; R.sub.2a and R.sub.3a are, at each occurrence, the same or different and independently hydrogen, hydroxy, --COOH, --CONH.sub.2, --R.sub.6, --OR.sub.6, --COOR.sub.6, --COR.sub.6 or --CONHR.sub.6, where R.sub.6 is lower alkyl optionally substituted with halogen or hydroxy; R.sub.1 and R.sub.4 are the same or different and represent the remainder of the molecule; and wherein R.sub.1 and R.sub.2 taken together optionally form a fused heterocycle or substituted heterocycle.

2. The method of claim 1 wherein the compound has the structure:

3. The method of claim 2 wherein the compound has the structure:

4. The method of claim 2 wherein the compound has the structure:

5. The method of claim 2 wherein the compound has the structure:

6. The method of claim 2 wherein the compound has the structure:

7. The method of claim 2 wherein the compound has the structure:

8. The method of claim 1 wherein the compound has the structure:

9. The method of claim 8 wherein the compound has the structure:

10. The method of claim 8 wherein the compound has the structure:

11. The method of claim 8 wherein the compound has the structure:

12. The method of claim 8 wherein the compound has the structure:

13. The method of claim 8 wherein the compound has the structure:

14. The method of claim 1 wherein the compound has the structure:

15. The method of claim 1 wherein the compound has the structure: wherein R' is one or more optional heterocycle substituents.

16. The method of claim 15 wherein the compound has the structure: wherein R' is --OR or --OC(O)R where R is an amino acid side chain moiety or an amino acid side chain derivative.

17. The method of claim 1 wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are independently an amino acid side chain moiety or an amino acid side chain derivative.

18. The method of claim 1 wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are independently: (i) --H, --CH.sub.3, --CH(CH.sub.3).sub.2, --CH.sub.2CH(CH.sub.3).sub.2, --CH(CH.sub.3)CH.sub.2CH.sub.3, --(CH.sub.2).sub.4NH.sub.2, --CH.sub.2).sub.3NHC(NH.sub.2)NH.sub.2, --CH.sub.2COOH, --CH.sub.2CH.sub.2COOH, CH.sub.2CONH.sub.2, --CH.sub.2CH.sub.2CONH.sub.2, --CH.sub.2SH, --CH.sub.2CH.sub.2SCH.sub.3, --CH.sub.2OH, --CH(OH)CH.sub.3, or (ii) a side chain moiety of 3,5-dibromotyrosine, 3,5-diiodotyrosine, hydroxylysine, .gamma.-carboxyglutamate, phosphotyrosine, phosphothreonine or phosphoserine; or (iii) a moiety selected from alkyl, aryl, arylalkyl, heterocyclic or heterocyclicalkyl moieties, each moiety of (iii) being optionally substituted with a substituent selected from halogen, oxo, hydroxy, haloalkyl, --R, --OR, --C(.dbd.O)R, --C(.dbd.O)OR, --C(.dbd.O)NRR, --NRR, --NRC(.dbd.O)R, --NRC(.dbd.O)OR, --NRC(.dbd.O)NRR, --OC(.dbd.O)R, --OC(.dbd.O)OR, --OC(.dbd.O)NRR, --SH, --SR, --SOR, --SO.sub.2R, --NRSO.sub.2R, --Si(R).sub.3, and --OP(OR).sub.3, wherein each occurrence of R is the same or different and independently an amino acid side chain moiety, hydrogen, alkyl, aryl, arylalkyl, heterocycle or heterocyclealkyl, or wherein any two R groups attached to the same nitrogen atom, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring or a substituted heterocyclic ring.

19. The method of claim 1 wherein the central nervous system disorder is anxiety, depression, psychosis, schizophrenia, epilepsy, or a neurodegenerative disorder.

20. The method of claim 1 wherein the central nervous system disorder is dementia, Alzheimer's disease, Down's syndrome, or AIDS dementia.

Brief Patent Description - Full Patent Description - Patent Claims

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