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Last Updated: November 28, 2020

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Claims for Patent: 7,176,211

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Summary for Patent: 7,176,211
Title:Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ##STR00001## wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.2a, R.sub.2b, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
Inventor(s): Guo; Zhiqiang (San Diego, CA), Chen; Yongsheng (San Diego, CA), Wu; Dongpei (San Diego, CA), Chen; Chen (San Diego, CA), Wade; Warren (San Diego, CA), Dwight; Wesley J. (San Diego, CA), Huang; Charles Q. (San Diego, CA), Tucci; Fabio C. (San Diego, CA)
Assignee: Neurocrine Biosciences, Inc. (San Diego, CA)
Application Number:11/251,085
Patent Claims: 1. A method for treating a condition selected from the group of prostate cancer, benign prostatic hypertrophy, breast cancer and endometriosis in a subject in need thereof comprising administering to the subject a pharmaceutically effective amount of a compound represented by the following structure: ##STR00047## or a stereoisomer or pharmaceutically acceptable salt thereof, wherein: R.sub.1a, R.sub.1b and R.sub.1c are the same or different and independently hydrogen, halogen, C.sub.1-4alkyl, hydroxy or alkoxy, or R.sub.1a and R.sub.1b taken together form --OCH.sub.2O-- or --OCH.sub.2CH.sub.2--; R.sub.2a and R.sub.2b are the same or different and independently hydrogen, halogen, trifluoromethyl, cyano or --SO.sub.2CH.sub.3; R.sub.3 is hydrogen or methyl; R.sub.4 is phenyl or C.sub.3-7alkyl; R.sub.5 is hydrogen or C.sub.1-4alkyl; R.sub.6 is -COOH or an acid isostere; and X is C.sub.1-6alkanediyl optionally substituted with from 1 to 3 C.sub.1-6alkyl groups.

2. A method according to claim 1, wherein X is a straight chain C.sub.1-6alkanediyl.

3. A method according to claim 2, wherein R.sub.6 is --COOH.

4. A method according to claim 3, wherein R.sub.4 is phenyl.

5. A method according to claim 4, wherein R.sub.1a is halogen and R.sub.1b is alkoxy.

6. A method according to claim 4, wherein R.sub.3 is methyl.

7. A method according to claim 4, wherein the condition is endometriosis.

8. A method according to claim 4, wherein the condition is benign prostatic hypertrophy.

9. A method according to claim 4, wherein the condition is prostate cancer.

10. A method according to claim 4, wherein the condition is breast cancer.

11. A method according to claim 1, wherein the compound is 3-[2(R)-{hydroxycarbonylpropyl-amino}-2-phenylethyl]-5-(2-fluoro-3-methox- yphenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methyl-pyrimidine-2,4(1H- ,3H)-dione, 3-[2(R)-{hydroxycarbonylpropyl-amino}-2-phenylethyl]-5-(3-isopropylphenyl- )-1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methyl-pyrimidine-2,4(1H,3H)-di- one, 3-[2(R)-{hydroxycarbonylpropyl-amino}-2-(cyclohexyl)ethyl]-5-(2-fluor- o-3-methoxyphenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methyl-pyrimid- ine-2,4(1H,3H)-dione, or 3-[2(R)-{2-[1-(5-tetrazoyl)propyl]-amino}-2-phenylethyl]-5-(2-fluoro-3-me- thoxyphenyl)-1-[2-fluoro-6-methylsulfonylbenzyl]-6-methylpyrimidine-2,4(1H- ,3H)-dione.

12. A method according to claim 11, wherein the condition is endometriosis.

13. A method according to claim 11, wherein the condition is benign prostatic hypertrophy.

14. A method according to claim 11, wherein the condition is prostate cancer.

15. A method according to claim 11, wherein the condition is breast cancer.

16. A method according to claim 1, wherein the compound is 3-[2(R)-{hydroxycarbonylpropyl-amino}-2-phenylethyl]-5-(2-chlorophenyl)-1- -[2-fluoro-6-(trifluoromethyl)benzyl]-pyrimidine-2,4(1H,3H)-dione, 3-[2(R)-{hydroxycarbonylpropyl-amino}-2-phenylethyl]-5-(2-fluoro-3-methox- yphenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]-pyrimidine-2,4(1H,3H)-dion- e, 3-[2(R)-{hydroxycarbonylpropyl-amino}-2-phenylethyl]-5-(2-chloro-3-meth- ylphenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]-pyrimidine-2,4(1H,3H)-dio- ne, 3-[2(R)-{hydroxycarbonylpropyl-amino}-2-phenylethyl]-5-(2-chlorophenyl- )-1-[2-fluoro-6-(methylsulfonyl)benzyl]-pyrimidine-2,4(1H,3H)-dione, 3-[2(R)-{hydroxycarbonylpropyl-amino}-2-phenylethyl]-5-(2-chloro-3-methox- yphenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]-pyrimidine-2,4(1H,3H)-dion- e, or 3-[2(R)-{hydroxycarbonylpropyl-amino}-2-(isobutyl)ethyl]-5-(2-chloro- -3-methoxyphenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]-pyrimidine-2,4(1H- ,3H)-dione.

17. A method according to claim 16, wherein the condition is endometriosis.

18. A method according to claim 16, wherein the condition is benign prostatic hypertrophy.

19. A method according to claim 16, wherein the condition is prostate cancer.

20. A method according to claim 16, wherein the condition is breast cancer.

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