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Details for Patent: 6,602,888

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Details for Patent: 6,602,888

Title: Use of .alpha.1C specific compounds to treat benign prostatic hyperplasia
Abstract:A method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than ten-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, and a human histamine H.sub.1 receptor, and, binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to such .alpha..sub.1C adrenergic receptor. Compounds meeting these criteria are provided.
Inventor(s): Gluchowski; Charles (Danville, CA), Forray; Carlos C. (Paramus, NJ), Chiu; George (Bridgewater, NJ), Branchek; Theresa A. (Teaneck, NJ), Wetzel; John M. (Elmwood Park, NJ), Hartig; Paul R. (Pennington, NJ)
Assignee: Synaptic Pharmaceutical Corporation (Paramus, NJ)
Filing Date:Nov 22, 1999
Application Number:09/444,783
Claims:1. A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and an amount of a compound effective to treat benign prostatic hyperplasia, which compound: a. binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity greater than ten-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor, a human .alpha..sub.1B adrenergic receptor, and a human histamine H.sub.1 receptor; b. binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to such .alpha..sub.1C adrenergic receptor; and c. binds to a calcium channel with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to a human .alpha..sub.1C adrenergic receptor.

2. The pharmaceutical composition of claim 1, wherein the binding affinity of the compound is at least 10-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human dopamine D.sub.2 receptor.

3. The pharmaceutical composition of claim 1, wherein the binding affinity of the compound is at least 10-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for any human serotonin receptor.

4. The pharmaceutical composition of claim 1, wherein the binding affinity of the compound is at least 10-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human dopamine D.sub.3, D,.sub.4, or D.sub.5 receptor.

5. A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and an amount of a compound effective to treat benign prostatic hyperplasia, which compound: a. binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity at least 26-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1B adrenergic receptor; and b. binds to a human .alpha..sub.2 adrenergic receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to a human .alpha..sub.1C adrenergic receptor; and c. binds to a calcium channel with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to a human .alpha..sub.1C adrenergic receptor.

6. The pharmaceutical composition of claim 5, wherein the binding affinity of the compound is at least 91-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human .alpha..sub.1A adrenergic receptor.

7. The pharmaceutical composition of claim 5, wherein the binding affinity of the compound for the human .alpha..sub.1C adrenergic receptor is at least 41-fold higher than it is for the calcium channel.

8. The pharmaceutical composition of claim 5, wherein the binding affinity of the compound for the human .alpha..sub.1C adrenergic receptor is at least 234-fold higher than it is for a human histamine H.sub.2 to receptor.

9. The pharmaceutical composition of claim 5, wherein the binding affinity of the compound for the human .alpha..sub.1C adrenergic receptor is at least 30-fold higher than it is for a human serotonin receptor.

10. The pharmaceutical composition of claim 5, wherein the binding affinity of the compound is at least 65- fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human histamine H.sub.1 receptor.

11. The pharmaceutical composition of claim 5, wherein the binding affinity of the compound for the human .alpha..sub.1C adrenergic receptor is (i) at least 91-fold higher than it is for the human .alpha..sub.1A adrenergic receptor, (ii) at least 65-fold higher than it is for the human histamine H.sub.1 receptor, and (iii) at least 229-fold higher than it is for the human .alpha..sub.2 adrenergic receptor.

12. A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and an amount of a compound effective to treat benign prostatic hyperplasia, which compound: a. binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity at least 35-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1A adrenergic receptor; and b. binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity at least 417-fold higher than the binding affinity with which the compound binds to a human histamine H.sub.1 receptor.

13. The pharmaceutical composition of claim 12, wherein the binding affinity of the compound is at least 28-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human .alpha..sub.2 adrenergic receptor.

14. A pharmaceutical composition which comprises a pharmaceutically acceptable carrier and an amount of a compound effective to treat benign prostatic hyperplasia, which compound: a. binds to a human .alpha..sub.1C adrenergic receptor with a binding affinity at least 48-fold higher than the binding affinity with which the compound binds to a human .alpha..sub.1B adrenergic receptor; and b. binds to a calcium channel with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to a human .alpha..sub.1C adrenergic receptor.

15. The pharmaceutical composition of claim 14, wherein the binding affinity of the compound is at least 10-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human .alpha..sub.1A adrenergic receptor or a human .alpha..sub.2 adrenergic receptor.

16. The pharmaceutical composition of claim 14, wherein the binding affinity of the compound is at least 10-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human histamine H.sub.1 receptor.

17. The pharmaceutical composition of claim 14, wherein the binding affinity of the compound is at least 10-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human dopamine D.sub.2 receptor.

18. The pharmaceutical composition of claim 14, wherein the binding affinity of the compound is at least 10-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human serotonin receptor.

19. The pharmaceutical composition of claim 14, wherein the binding affinity of the compound is at least 10-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human dopamine D.sub.3, D.sub.4, or D.sub.5 receptor.

20. The pharmaceutical composition of claim 14, wherein the binding affinity of the compound is at least 200-told higher for the human .alpha..sub.1C adrenergic receptor than it is for a human .alpha..sub.1B adrenergic receptor.

21. The pharmaceutical composition of claim 20, wherein the binding affinity of the compound is at least 51-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human histamine H.sub.1 receptor.

22. The pharmaceutical composition of claim 15, wherein the binding affinity of the compound is at least 107-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human .alpha..sub.1A adrenergic receptor.

23. The pharmaceutical composition of claim 20, wherein the binding affinity of the compound is at least 776-fold higher for the human .alpha..sub.1C adrenergic receptor than it is for a human .alpha..sub.1A adrenergic receptor.

24. The pharmaceutical composition of claim 14, wherein the binding affinity of the compound for the human .alpha..sub.1C adrenergic receptor is (i) at least 107-fold higher than it is for the human .alpha..sub.1A adrenergic receptor, (ii) at least 93-fold higher than it is for the human histamine H.sub.1 receptor, and (iii) at least 209-fold higher than it is for the human .alpha..sub.2 adrenergic receptor.

25. The pharmaceutical composition of claim 14, wherein the binding affinity of the compound for the human .alpha..sub.1C adrenergic receptor is (i) at least 776-fold higher than it is for the human .alpha..sub.1A adrenergic receptor, (ii) at least, 200-fold higher than it is for the human .alpha..sub.1B adrenergic receptor, (iii) at least 51-fold higher than it is for the human histamine H.sub.1 receptor, and (iv) at least 871-fold higher than it is for the human .alpha..sub.2 adrenergic receptor.

26. The pharmaceutical, composition of claim 20, wherein the binding affinity of the compound for the human .alpha..sub.1C adrenergic receptor is at least 550-fold higher than it is for the calcium channel.

27. The pharmaceutical composition of claim 20, wherein the binding affinity of the compound for the human .alpha..sub.1C adrenergic receptor is at least 25-fold higher than it is for a human histamine H.sub.2 receptor.

28. The pharmaceutical composition of claim 18, wherein the binding affinity of the compound for the human .alpha..sub.1C adrenergic receptor is at least 56-fold higher than it is for a human serotonin receptor.

29. The pharmaceutical composition of claim 28, wherein the binding affinity of the compound for the human .alpha..sub.1C adrenergic receptor is at least 74-fold higher than it is for a human serotonin receptor.

30. The pharmaceutical composition of claim 1, 5, 12 or 14 , wherein the compound additionally does not cause an orthostatic fall in blood pressure at dosages effective to alleviate benign prostatic hyperplasia.

31. A pharmaceutical composition of claim 1, 5, 12 or 14, wherein the compound additionally does not cause an orthostatic fall in blood pressure in rats at a dosage of 10 micrograms of antagonist per kilogram of rat.
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