IP Library › Granted Patent US 9,006,263
Granted Patent B2
US 9,006,263 · App. 13/789,361 · Granted Apr 14, 2015

Compounds and methods for treatment of hypertension

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Quick Facts
Patent No.
US 9,006,263
App. No.
13/789,361
Granted
Apr 14, 2015
Kind
B2
Abstract

Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor α 2B antagonists. The compounds may also bind to and antagonize adrenergic receptor α 1B . The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.

Claims (37)

1. A method of lowering blood pressure in an individual in need thereof comprising administering to the individual an effective amount of a compound selected from the group consisting of Compound Nos. 6, 9 to 12, 14, 16 to 21, 23 to 28, 39 to 40, 42, 44 to 59, 63 to 72, 77 to 82, 104, 108 to 116, 118 to 131, 133 to 142, 144 to 171, 173 to 179, 187 to 192, 195 to 198, 220, 269 to 271, 273 to 287, 290 to 306, 308 to 319, 321 to 338, 340 to 342, II-1 to II-4, II-6 to II-16, II-18 to II-19, II-39 to II-40, II-58 to II-65, II-67 to II-68, II-70 to II-71, II-75 to II-77, II-80 to II-84, II-88 to II-94, II-96 to II-106, II-108 to II-118, II-120 to II-121, II-123 to II-125, II-127 to II-128, II-130 to II-136, II-138 to II-154, II-188 to II-206, II-212 to II-213, II-215, II-220 to II-227, II-229 to II-232, II-240, II-243 to II-253, II-255 to II-269, II-271 to II-272, II-274, II-276 to II-285, II-287 to II-291, II-293 to II-298, IV1, IV-8 to IV-9, IV-11 to IV-18, IV-49 to IV-58, IV-91, IV-93 to IV-98, IV129 to IV-138, IV-169 to IV-178, IV-209 to IV-211, IV-213 to IV-218, and V-1 to V-23; or a salt, solvate or N-oxide thereof.

2. A method of (i) increasing renal blood flow, and/or (ii) decreasing sodium reabsorption, in an individual in need thereof comprising administering to the individual an effective amount of a compound selected from the group consisting of Compound Nos. 6, 9 to 12, 14, 16 to 21, 23 to 28, 39 to 40, 42, 44 to 59, 63 to 72, 77 to 82, 104, 108 to 116, 118 to 131, 133 to 142, 144 to 171, 173 to 179, 187 to 192, 195 to 198, 220, 269 to 271, 273 to 287, 290 to 306, 308 to 319, 321 to 338, 340 to 342, II-1 to II-4, II-6 to II-16, II-18 to II-19, II-39 to II-40, II-58 to II-65, II-67 to 11-68, II-70 to II-71, II-75 to II-77, II-80 to II-84, II-88 to II-94, II-96 to II-106, II-108 to II-118, II-120 to II-121, II-123 to II-125, II-127 to II-128, II-130 to II-136, II-138 to II-154, II-188 to II-206, II-212 to II-213, II-215, II-220 to II-227, II-229 to II-232, II-240, II-243 to II-253, II-255 to II-269, II-271 to II-272, II-274, II-276 to II-285, II-287 to II-291, II-293 to II-298, IV1, IV-8 to IV-9, IV-11 to IV-18, IV-49 to 1V-58, IV-91, IV-93 to IV-98, IV129 to IV-138, IV-169 to IV-178, IV-209 to IV-211, IV-213 to IV-218, and V-1 to V-23; or a salt, solvate or N-oxide thereof.

3. A method of treating a disease or condition that is responsive to any one or more of: (i) a decrease in blood pressure; (ii) an increase in renal blood flow; and (iii) a decrease of sodium reabsorption, comprising administering to an individual in need thereof an effective amount of a compound selected from the group consisting of Compound Nos. 6, 9 to 12, 14, 16 to 21, 23 to 28, 39 to 40, 42, 44 to 59, 63 to 72, 77 to 82, 104, 108 to 116, 118 to 131, 133 to 142, 144 to 171, 173 to 179, 187 to 192, 195 to 198, 220, 269 to 271, 273 to 287, 290 to 306, 308 to 319, 321 to 338, 340 to 342, II-1 to II-4, II-6 to II-16, II-18 to II-19, II-39 to II-40, II-58 to II-65, II-67 to 11-68, II-70 to II-71, II-75 to II-77, II-80 to II-84, II-88 to II-94, II-96 to II-106, II-108 to II-118, II-120 to II-121, II-123 to II-125, II-127 to II-128, II-130 to II-136, II-138 to II-154, II-188 to II-206, II-212 to II-213, II-215, II-220 to II-227, II-229 to II-232, II-240, II-243 to II-253, II-255 to II-269, II-271 to II-272, II-274, II-276 to II-285, II-287 to II-291, II-293 to II-298, IV1, IV-8 to 1V-9, 1V-11 to IV-18, IV-49 to IV-58, IV-91, IV-93 to IV-98, IV129 to IV-138, IV-169 to IV-178, IV-209 to IV-211, IV-213 to IV-218, and V-1 to V-23; or a salt, solvate or N-oxide thereof.

4. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

5. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

6. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

7. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

8. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

9. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

10. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

11. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

12. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

13. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

14. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

15. The method of any one of claims 1 , 3 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

16. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

17. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

18. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

19. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

20. The method of any one of claims 1 , 2 , and 3 , wherein the compound is selected from the group consisting of:

or a salt thereof.

Assignments (3)
RELEASE OF SECURITY INTEREST Recorded Sep 28, 2016
From: JPMORGAN CHASE BANK, N.A., AS ADMINISTRATIVE AGENT
To: MEDIVATION PROSTATE THERAPEUTICS, INC.; MEDIVATION TECHNOLOGIES, INC.
Reel/Frame 040181/0177 →
CONFIRMATORY GRANT OF SECURITY INTEREST IN UNITED STATES PATENTS Recorded Sep 4, 2015
From: MEDIVATION TECHNOLOGIES, INC.
To: JPMORGAN CHASE BANK, N.A., AS ADMINISTRATIVE AGENT
Reel/Frame 036553/0925 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 19, 2014
From: PROTTER, ANDREW ASHER; CHAKRAVARTY, SARVAJIT; JAIN, RAJENDRA PARASMAL; GREEN, MICHAEL JOHN
To: MEDIVATION TECHNOLOGIES, INC.
Reel/Frame 034210/0427 →