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Home Vasodialators Nitrosated-and-nitrosylated-alpha-adrenergic-receptor-antagonist-compounds-compositions-and-their-uses

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 Nitrosated and nitrosylated .alpha.-adrenergic receptor antagonist compounds, compositions and their uses

Details
Inventors: Garvey, David S.; Schroeder, Joseph D.; Saenz de Tejada, Inigo;
Assignee: NitroMed, Inc. (Bedford, MA)
Primary Examiner: Tsang; Cecilia J.
Assistant Examiner: Celsa; Bennett
Attorney, Agent or Firm: Hale and Dorr LLP

Disclosed are nitrosated and nitrosylated .alpha.-adrenergic receptor antagonists, compositions of an .alpha.-adrenergic receptor antagonist (.alpha.-antagonist), which can optionally be substituted with at least one NO or NO.sub.2 moiety, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO.sup.+) or nitroxyl (NO.sup.-), or as the neutral species, nitric oxide (NO.circle-solid.); and uses for each of them in treating human male impotence or erectile dysfunction.

DETAILED DESCRIPTION OF THE INVENTION The term "lower alkyl" as used herein refers to branched or straight chain alkyl groups comprising one to ten carbon atoms, including methyl, ethyl, propyl, isopropyl, n-butyl, t-butyl, neopentyl and the like.
The term "alkoxy" as used herein refers to R.
sub.
50 O-wherein R.
sub.
50 is lower alkyl as defined above.
Representative examples of alkoxy groups include methoxy, ethoxy, t-butoxy and the like.
The term "alkoxyalkyl" as used herein refers to an alkoxy group as previously defined appended to an alkyl group as previously defined.
Examples of alkoxyalkyl include, but are not limited to, methoxymethyl, methoxyethyl, isopropoxymethyl and the like.
The term "hydroxy" as used herein refers to --OH.
The term "hydroxyalkyl" as used herein refers to a hydroxy group as previously defined appended to an alkyl group as previously defined.
The term "alkenyl" as used herein refers to a branched or straight chain C.
sub.
2 -C.
sub.
10 hydrocarbon which also comprises one or more carbon-carbon double bonds.
The term "amino" as used herein refers to --NH.
sub.
2.
The term "nitrate" as used herein refers to --O--NO.
sub.
2.
The term "alkylamino" as used herein refers to R.
sub.
11 NH-- wherein R.
sub.
11 is a lower alkyl group, for example, methylamino, ethylamino, butylamino, and the like.
The term "dialkylamino" as used herein refers to R.
sub.
12 R.
sub.
13 N-- wherein R.
sub.
2 and R.
sub.
13 are independently selected from lower alkyl, for example dimethylamino, diethylamino, methyl propylamino and the like.
The term "nitro" as used herein refers to the group --NO.
sub.
2 and "nitrosated" refers to compounds that have been substituted therewith.
The term "nitroso" as used herein refers to the group --NO and "nitrosylated" refers to compounds that have been substituted therewith.
The term "aryl" as used herein refers to a mono- or bicyclic carbocyclic ring system having one or two aromatic rings including, but not limited to, phenyl, naphthyl, tetrahydronaphthyl, indanyl, indenyl, and the like



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