N,N-di(aryl) cyclic urea derivatives as anti-coagulants

Details N,N-di(aryl) cyclic urea derivatives as anti-coagulants N,N-di(aryl) cyclic urea derivatives as anti-coagulants

1996-12-12

1998-03-24

Morris, Patricia L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

5142355, 514252, 514255, 514318, 514326, 514333, 514341, 514392, 544124, 544139, 544360, 544370, 546194, 546210, 546256, 5462741, 5483137, 5483144, 5483147, 5483164, 5483175, 5483185, 5483195, 5483201, A61K 31535, A61K 31495, C07D41310, C07D40310

Patent

active

057313113

ABSTRACT:
N,N-di(aryl) cyclic urea derivatives, such as the compounds of the following formula: ##STR1## wherein R.sup.1 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.11, --C(NH)N(H)C(O)R.sup.9, or --C(NH)N(H)C(O)OR.sup.11 ;
R.sup.2 and R.sup.3 are independently hydrogen, halo, lower alkyl, lower haloalkyl, aryl, --OR.sup.11, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, --N(R.sup.11)R.sup.12, --N(H)C(O)R.sup.11, or --N(H)S(O).sub.2 R.sup.11 ;
R.sup.4 is halo, lower haloalkyl, imidazolyl, --C(NH)NH.sub.2, --C(NH)NHOR.sup.11, --C(NH)N(H)C(O)R.sup.9, --C(NH)N(H)C(O)OR.sup.11, --OR.sup.11, --C(O)R.sup.13, --(CH.sub.2).sub.n C(O)OR.sup.11 (where n is 0 to 6), --C(O)N(R.sup.11)R.sup.12, or --N(R.sup.11)R.sup.12 ;
R.sup.7 and R.sup.8 are independently hydrogen, lower alkyl, lower haloalkyl, 4-pyridinyl, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, or aryl (optionally substituted by one or more substituents selected from the group consisting of halo, hydroxy, lower alkyl, lower haloalkyl, lower alkoxy and --N(R.sup.11)R.sup.12);
R.sup.11 and R.sup.12 are independently hydrogen, lower alkyl, aryl or lower aralkyl; or
R.sup.13 is pyrrolidinyl, 4-morpholinyl, piperazinyl, N-methylpiperazinyl, or piperidinyl; or a pharmaceutically acceptable salt thereof, are disclosed herein as being inhibitors of factor Xa and thereby being useful as anticoagulants.

REFERENCES:
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patent: 5332822 (1994-07-01), Misra
patent: 5478942 (1995-12-01), Himmelsbach et al.
Tidwell, R. et al., "Strategies for Anticoagulation with Synthetic Protease Inhibitors, Xa Inhibitors Versus Thrombin Inhibitors," Thrombosis Research, (1980) 19:339-349.
Sturzebecher, J. et al., "Cyclic Amides of N.alpha.-arysulfonylaminoacylated 4-amidinophenylalanine--Tight Binding Inhibitors of Thrombin," Thrombosis Research, (1983) 29:635-642.
Kikumoto, R. et al., "Selective inhibition of Thrombin by dinecarboxylic Acid," Biochemistry, (1984) 23:85-90.
Sturzebecher, J. et al., "Synthetic Inhibitors of Serine Proteinases XXIII, Inhibition of Factor Xa by Diamidines", Thrombosis Research, (1980) 17:545:548.
Wagner, G. et al., "Synthese von N-Amidinobenzylverbindungen von Salicylamid, 2-4-Dioxodihydro-5.6-benzoxazin-(1.3) und-benzothiazin-(1.3) sowie von 2.4-Dioxo-1.2.3.4-tetrahydrochinazolin", Die Pharmazie, (1978) 33:15-19.

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