. Author manuscript; available in PMC: 2007 Jan 1.

Published in final edited form as: Recent Pat Cardiovasc Drug Discov. 2006 Jan;1(1):95–108. doi: 10.2174/157489006775244263

Table 3.

Recently Patented Compounds with Potential ET Receptor Antagonist Properties

Compounds	Examples	Receptor Specificity	US Patent
Benzothia(oxa)diazols	3-(2,1,3-benzothiadiazol-5-yl)-4-(3-cyclopentyloxy-4,5-dimethoxybenzyl)-5-hydroxy-5-(4 methoxyphenyl)- 5H-furan-2-one	ET_A, ET_B	6017939 [95] 6197800 [96]
Benzothiazine dioxides	4-(3,5-Dimethoxy-phenyl)-2-(2-trifluoromethyl-phenyl)-1,1-dioxo-1,2-dihydro -1.γ⁶ -benzo[e][1,2]thiazine-3-carboxylic acid	ET_A	6440962 [97]
Cyclopentanes	(1RS,2RS,3SR)-1,3 bis(4-methoxyphenyl) cyclopentane-2-carboxylic acid	ET_A, ET_B	5929106 [98]
Dibenzodiazepines	5,11-Dihydro-8-(1-naphthalenylmethoxy)-11-oxo-10H-dibenzo[b,e][1,4]diazepine-10-acetic acid	ET_A, ET_B	5420123 [99]
Furans	(E)-3-[3-[2-(2-Carboxyphenyl)methoxy-4-methoxy] phenylfuran-2-yl]-2-[(2-meth oxy-4,5-methylene dioxy) phenylmethyl]-prop-2-enoic acid	ET_A, ET_B	6051599 [100]
Indanes, Indenes, Indoles	(1RS,2SR,3RS)-3-(2-Carboxymethoxy-4-methoxy phenyl)-1-(3,4-methylenedioxy-phenyl)-5-(prop-1-yloxy)-indane-2-carboxylic acid	ET_A, ET_B	6448260 [101] 6384070 [102]
Isooxazoles, Oxazoles, Imidazoles	(E)-Ethyl alpha-[[3-[4methoxy-2-[[2-(methoxycarbonyl) phenyl]methoxy]-phenyl]isoxazol -4-yl]methylene]-6-methoxy-1,3-benzodioxole-5-propanoate	ET_A, ET_B	6174906 [103] 6620826 [104]
Ketoacids	Benzo[1,3]dioxol-5-yl-4-(4-methoxy-phenyl)-4-oxo-3-(3,4,5-trimethoxy- benzyl)-but-2-enoic acid	ET_A, ET_B	6043241 [105]
Phenoxyphenylacetic acids	2-[(2,6-Dipropyl-4-hydroxymethyl) phenoxy]-2-(3-methyl phenyl)acetic acid	ET_A, ET_B	5565485 [106]
Phenylalanine derivatives	(R,S)-N-(Diphenylacetyl)-3-methoxy-2-(phenylmethoxy) phenylalanine	ET_A, ET_B	5658943 [107]
Prostaglandins	difluoro-13,14-dihydro-15-keto-PGE₁ Methyl Ester	ET_A, ET_B	6197821 [108]
Pyrazoles, Triazoles	(E)-a-[[5-[2-[(2-carboxyphenyl)methoxy]-4-methoxy phenyl]-1-ethyl-1H-pyrazol-4-yl]methylene]-6-methoxy-1,3-benzodioxole-5-propanoic acid	ET_A, ET_B	6545031 [109]
Pyridizinones	2-(1,3-benzodioxol-5-yl)-2-(2,3-dihydro-4,6-dimethyl pyridazin-3-on-2-yl)N- (4-isopropylphenyl sulfonyl) acetamide	ET_A, ET_B	5883090 [110]
Pyrimidines	3-6-(4-t-butylphenyl-sulfonylamino)-5-(2-methoxyphen oxy)-2-morpholino-4-pyrimidinyl oxypropionic acid	ET_A, ET_B	5883092 [111]
Pyrrolo[2,3-b]pyridines	(Methoxyphenyl)-1-(3,4-methylenedioxy-phenylmethyl) pyrrolo[2,3-b]pyridine-2-carboxylic acid	ET_A, ET_B	6075037 [112]
Sulfanyl derivatives	Methyl 3,3-diphenyl-2-(4,6-dimethoxypyrimidine-2-sulfanyl)propionate	ET_A, ET_B	6235903 [113]
Aryl, hetaryl, isoxazole, N-heterocyclic, phenyl, and thieno-pyridine sulfonamides	5-(Dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulfonamide	ET_A, ET_B	6387915 [114] 6686382 [115] 6107320 [116] 6013655 [117]
Benzene, biphenyl sulfonamides	N-(3,4-Dimethyl-5-isoxazolyl)-4-biphenylsulfonamide	ET_B	6541498 [118]

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