135682-53-0Relevant articles and documents
7-oxabicycloheptyl substituted heterocyclic thioamide prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
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, (2008/06/13)
7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasospastic disease have the structural formula STR1 wherein m is 1, 2 or 3; n is 1, 2, 3 or 4; Z is --(CH2)2 --, --CH=CH-- or STR2 wherein Y is O, a single bond or vinyl, with the proviso that when n is O, if Z is STR3 then Y cannot be O, and when Z is --CH=CH--, n is 1, 2, 3 or 4; and when Y=vinyl, n=0; R is CO2 H, CO2 lower alkyl, CH2 OH, CO2 alkali metal, CONHSOR3, CONHR3a or --CH2 -5-tetrazolyl, X is O, S or NH; and where R1, R2, R3 and R3a are as defined herein.
Heterocyclic amido prostaglandin analogs
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, (2008/06/13)
Prostaglandin analogs useful in treating thrombotic and vasospastic disease having the structural formula STR1 wherein: m is 1, 2, or 3; n is 0, 1, 2 or 3; R is CO2 R', CH2 OH, CONHSO2 Rhu 3, CONHR4,
Interphenylene 7-Oxabicycloheptane Oxazoles. Highly Potent, Selective, and Long-Acting Thromboxane A2 Receptor Antagonists
Misra, Raj N.,Brown, Baerbel R.,Sher, Philip M.,Patel, Manorama M.,Hall, Steven E.,et al.
, p. 1401 - 1417 (2007/10/02)
A series of interphenylene 7-oxabicycloheptane oxazoles (2) were prepared and evaluated for their thromboxane (TxA2) antagonistic activity in vitro and duration of action in vivo.Examination of the carboxyl side chain indicated that the
7-oxabicycloheptyl substituted heterocyclic amide or ester prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
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, (2008/06/13)
7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasopastic disease have the structural formula STR1 wherein m is 1, 2 or 3; n is 1, 2, 3 or 4; Z is --(CH2)2 --, --CH=CH-- or STR2 wherein Y is O, a single bond or vinyl, with the proviso that when n is 0, if Z is STR3 then Y cannot be O, and Z is --CH=CH--, n is 1, 2, 3 or 4; and when Y=vinyl, n=0; R is CO2 H, CO2 lower alkyl, CH2 OH, CO2 alkali metal, CONHSOR3, CONHR3a or --CH2 --5-tetrazolyl, X is O, S or NH; and where R1, R2, R3 and R3a are as defined herein.
Anti-thrombotic heterocyclic amido prostaglandin analogs
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, (2008/06/13)
Prostaglandin analogs useful in treating thrombotic and vasospastic disease having the structural formula STR1 wherein: m is 1, 2 or 3: n is 1, 2 or 3, except that n is O when Y is vinylene; p is 1, 2 or 3; R is CO2 R', CH2 OH, CONHS
Heterocyclic ketone prostaglandin analogs
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, (2008/06/13)
Prostaglandin analogs useful in treating thrombotic and vasospastic disease having the structural formula STR1 wherein: m is 1, 2, or 3; n is 0, 1, 2 or 3; R1 is hydrogen, alkyl, alkenyl, alkynyl, aralkyl, aryl cycloalkyl, cycloalkylalkyl, cycl
Interphenylene 7-oxabicyclo[2.2.1]heptane thromboxane A2 antagonists. Semicarbazone ω-chains
Misra,Brown,Han,Harris,Hedberg,Webb,Hall
, p. 2882 - 2891 (2007/10/02)
A series of chiral interphenylene 7-oxabicyclo[2.2.1]heptane semicarbazones 19-26 were prepared and evaluated for their in vitro thromboxane (TxA2) antagonistic activity and in vivo duration of action. The potency of 19-26 was found to be highly dependent on the substitution pattern of the interphenylene ring and decreased in the order ortho > meta >> para. SQ 35,091 (25), [1S-(1α,2α,3α,4α)]-2-[[3-[[[(phenylamino)carbonyl]hydrazono] methyl]-7-oxabicyclo[2.2.1]hept-2-yl]methyl]benzenepropanoic acid, was identified as a potent and long-acting TxA2 antagonist. In human platelet rich plasma SQ 35,091 inhibited arachidonic acid (800 μM) and U-46,619 (10 μM) induced aggregation with I50 values of 3 and 12 nM, respectively. In contrast, no inhibition of ADP (20 μM) induced aggregation was observed at >1000 μM. Receptor binding studies with [3H]-SQ 29,548 showed SQ 35,091 was a competitive antagonist with a K(d) value of 1.0 ± 0.1 nM in human platelet membranes. In vivo SQ 35,091 (0.2 mg/kg po) showed extended protection (T50 = 16 h) from U-46,619 (2 mg/kg iv) induced death in mice. These compounds have for the first time demonstrated that a metabolically stable interphenylene α-sidechain can be introduced into a prostanoid-like series of TxA2 antagonists with the maintenance of potent antagonistic activity.
7-oxabicycloheptane imidazole prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
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, (2008/06/13)
7-Oxabicycloheptane imidazole prostaglandin analogs are provided which are useful in treating thrombotic and vasospastic disease and have the structural formula STR1 wherein m is 0, 1, 2, 3 or 4; n is 1, 2 or 3; and p is 1, 2 or 3; Z is --CH=CH--, --CH2 CH2 -- or STR2 wherein Y is 1 or a single bond; R is CO2 H, CO2 lower alkyl, CO2 alkali metal, CONHSO2 R2 (wherein R2 is lower alkyl or aryl) or --CH2 -5-tetrazolyl; A is CHOH, C=O, STR3 (wherein R3 is H or lower alkyl), or a single bond; R1 is lower alkyl, aryl, cycloalkyl or H, R1 can be H only when A is a single bond.
