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(12) Patent Application Publication (10) Pub. No.: US 2009/0012057 A1 Garvey (43) Pub US 20090012057A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2009/0012057 A1 Garvey (43) Pub. Date: Jan. 8, 2009 (54) CARDOVASCULAR COMPOUNDS Publication Classification COMPRISING NITRC OXDE ENHANCNG (51) Int. Cl. GROUPS, COMPOSITIONS AND METHODS A6II 3/554 (2006.01) OF USE A 6LX 3/5.377 (2006.01) C07D 417/04 (2006.01) C07D 409/06 (2006.01) (75) Inventor: David S. Garvey, Dover, MA (US) A6IP 9/10 (2006.01) A6IP 9/00 (2006.01) A6II 3/478 (2006.01) Correspondence Address: C07D 22.3/22 (2006.01) WILMERHALEADC A6II 3/55 (2006.01) 1875 PENNSYLVANIAAVE, NW (52) U.S. Cl. ................. 514/211.07: 54.4/138: 514/236.2: WASHINGTON, DC 20004 (US) 514/397: 548/315.1: 540/588: 514/217 (57) ABSTRACT Assignee: NitroMed, Inc., Lexington, MA (73) The invention describes compositions and kits comprising at (US) least one cardiovascular compound comprising at least one nitric oxide enhancing group, orpharmaceutically acceptable Appl. No.: 11/815,270 salts thereof, and, optionally, at least one nitric oxide enhanc (21) ing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascu (22) PCT Fled: Feb. 28, 2006 lar diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases (86) PCT NO.: PCT/USO6/O6843 caused by endothelial dysfunctions; (g) treating cirrhosis: (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating S371 (c)(1), nephropathy: (1) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disor (2), (4) Date: Mar. 24, 2008 ders; (o) treating metabolic syndrome; and (p) treating hyper lipidemia. The cardiovascular compounds are angiotensin II Related U.S. Application Data antagonists, aldosterone antagonists, endothelin antagonists, hydralazine compounds, neutral endopeptidase inhibitors (60) Provisional application No. 60/656,544, filed on Feb. and renin inhibitors. The nitric oxide enhancing groups are 28, 2005. nitroxides and/or heterocyclic nitric oxide donors. US 2009/0012057 A1 Jan. 8, 2009 CARDOVASCULAR COMPOUNDS more sites such as oxygen (hydroxyl condensation), Sulfur COMPRISING NITRC OXDE ENHANCNG (sulfhydryl condensation) and/or nitrogen via a bond or moi GROUPS, COMPOSITIONS AND METHODS ety that can be hydrolyzed. The heterocyclic nitric oxide OF USE donor groups are furoxans, Sydnonimines, oXatriazole-5- ones and/or oXatriazole-5-imines. The invention also pro RELATED APPLICATIONS vides compositions comprising the novel compounds 0001. This application claims priority under 35 USC S 119 described herein in a pharmaceutically acceptable carrier. to U.S. Application No. 60/656,544 filed Feb. 28, 2005. 0006. The invention is also based on the discovery that administering at least one cardiovascular compound compris FIELD OF THE INVENTION ing at least one nitric oxide enhancing group or a pharmaceu tically acceptable salt thereof, and, optionally, at least one 0002 The invention describes compositions and kits com nitric oxide enhancing compound improves the properties of prising at least one cardiovascular compound comprising at the cardiovascular compound. Nitric oxide enhancing com least one nitric oxide enhancing group, or pharmaceutically pounds include, for example, S-nitrosothiols, nitrites, acceptable salts thereof, and, optionally, at least one nitric nitrates, N-oxo-N-nitrosamines, furoxans, Sydnonimines, oxide enhancing compound and/or at least one therapeutic SPM3672, SPM 4757, SPM5185, SPM5186 and analogues agent. The invention also provides methods for (a) treating thereof, substrates of the various isozymes of nitric oxide cardiovascular diseases; (b) treating renovascular diseases; synthase, and nitroxides. Thus, another embodiment of the (c) treating diabetes; (d) treating diseases resulting from oxi invention provides compositions comprising at least one car dative stress; (e) treating endothelial dysfunctions; (f) treating diovascular compound comprising at least one nitric oxide diseases caused by endothelial dysfunctions; (g) treating cir enhancing group and at least one nitric oxide enhancing com rhosis: (h) treating pre-eclampsia; () treating osteoporosis: pound. The invention also provides for Such compositions in (k) treating nephropathy: (1) treating peripheral vascular dis a pharmaceutically acceptable carrier. eases; (m) treating portal hypertension, (n) treating oph 0007. The invention provides compositions comprising at thalmic disorders; (o) treating metabolic syndrome; and (p) least one cardiovascular compound comprising at least one treating hyperlipidemia. The cardiovascular compounds are nitric oxide enhancing group, and, optionally, at least one angiotensin II antagonists, aldosterone antagonists, endothe nitric oxide enhancing compound and/or at least one thera lin antagonists, hydralazine compounds, neutral endopepti peutic agent, including, but not limited to, aldosterone dase inhibitors and renin inhibitors. The nitric oxide enhanc antagonists, C-adrenergic receptor agonists, C.-adrenergic ing groups are nitroxides and/or heterocyclic nitric oxide receptor antagonists, angiotensin II antagonists, angiotensin donors. converting enzyme (ACE) inhibitors, antidiabetic com BACKGROUND OF THE INVENTION pounds, anti-hyperlipidemic compounds, antimicrobial com pounds, antioxidants, antithrombotic and vasodilator 0003. The decline in cardiovascular morbidity and mor compounds, B-adrenergic antagonists, calcium channel tality in the United States over the past three decades has been blockers, carbonic anhydrase inhibitors, digitalis, diuretics, the result of significant advances in research on cardiovascu endothelin antagonists, hydralazine compounds, H2 receptor lar disease mechanisms and therapeutic strategies. The inci antagonists, neutral endopeptidase inhibitors, nonsteroidal dence and prevalence of myocardial infarction and death antiinflammatory compounds (NSAIDs), phosphodiesterase from myocardial infarction, as well as that from cerebrovas inhibitors, potassium channel blockers, platelet reducing cular accident, have decreased significantly over this period agents, prostaglandins, proton pump inhibitors, renin inhibi largely owing to advances in prevention, early diagnosis, and tors, selective cyclooxygenase-2 (COX-2) inhibitors, ste treatment of these very common diseases. roids, and combinations of two or more thereof. In one 0004. The compounds administered for the treatment of embodiment the at least one therapeutic agent is selected diuresis, cardiovascular diseases, and diseases resulting from from the group consisting of an aldosterone antagonist, an oxidative and/or endothelial dysfunctions often result in angiotensin II antagonist, an angiotensin-converting enzyme toxic, chronic and/or debilitating side effects. Cardiovascular (ACE) inhibitor, a 3-adrenergic antagonist, a calcium channel compounds such as ACE inhibitors, beta-adrenergic blockers, blocker, a diuretic, a hydralazine compound and a renin antithrombotic and vasodilator compounds or anti-hyperlipi inhibitor. The invention also provides for such compositions demic compounds, show, for example, respiratory toxicity in a pharmaceutically acceptable carrier. resulting in asthma and/or bronchitis. Hence there is a need in 0008 Another embodiment of the invention provides the art for compounds that have improved efficacy, lower compositions comprising at least one cardiovascular com toxicity and that can be used at low dosages. The invention is pound of the invention comprising at least one nitric oxide directed to these, as well as other, important ends. enhancing group, and at least one therapeutic agentis selected from the group consisting of an aldosterone antagonist, an SUMMARY OF THE INVENTION angiotensin II antagonist, an angiotensin-converting enzyme 0005. The invention provides novel cardiovascular com (ACE) inhibitor, a 3-adrenergic antagonist, a calcium channel pounds comprising at least one nitric oxide enhancing group, blocker, a diuretic, a hydralazine compound and a renin and pharmaceutically acceptable salts thereof. The cardiovas inhibitor. The invention also provides for such compositions cular compounds can be, for example, aldosterone antago in a pharmaceutically acceptable carrier. nists, angiotensin II antagonists, endothelin antagonists, 0009. The invention provides methods for (a) treating car hydralazine compounds, neutral endopeptidase inhibitors diovascular diseases; (b) treating renovascular diseases; (c) and renin inhibitors. The nitric oxide enhancing groups are treating diabetes; (d) treating diseases resulting from oxida nitroxides and/or heterocyclic nitric oxide donor groups that tive stress; (e) treating endothelial dysfunctions, (f) treating are linked to the cardiovascular compounds through one or diseases caused by endothelial dysfunctions; (g) treating cir US 2009/0012057 A1 Jan. 8, 2009 rhosis: (h) treating pre-eclampsia; () treating osteoporosis: more thereof. The cardiovascular compound comprising at (k) treating nephropathy: (1) treating peripheral vascular dis least one nitric oxide enhancing group, the nitric oxide eases; (m) treating portal hypertension, (n) treating oph enhancing compound and/or therapeutic agent, can be sepa thalmic disorders; (o) treating metabolic syndrome; and (p) rate components in the kit or can be in the form of a compo treating hyperlipidemia in a patient in need thereof compris sition in
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