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Benzimidazoles useful as angiotensin-11 antagonists

Patent 5591762 Issued on January 7, 1997. Estimated Expiration Date: Icon_subject June 1, 2015. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

Benzimidazole compounds
Patent #: 5338756
Issued on: 08/16/1994
Inventor: Fortin, et al.

Benzimidazoles, pharmaceutical compositions containing these compounds and processes for preparing them Patent #: 5385925
Issued on: 01/31/1995
Inventor: Narr, et al.

Inventors

Assignee

Application

No. 457204 filed on 06/01/1995

US Classes:

514/381, Tetrazoles (including hydrogenated)514/222.2, Hetero ring is six-membered and includes at least nitrogen and sulfur as ring members514/234.5, Plural ring nitrogens in the bicyclo ring system514/248, Polycyclo ring system having a 1,2- or 1,4-diazine as one of the cyclos514/266.23, The additional hetero ring is five-membered consisting of carbon and plural nitrogens as the only ring members514/307, Isoquinolines (including hydrogenated)514/314, Additional hetero ring attached directly or indirectly to the quinoline ring system by nonionic bonding514/322, Plural ring nitrogens in the polycyclo ring system514/338, Plural hetero atoms in the polycyclo ring system514/365, 1,3-thiazoles (including hydrogenated)514/367, Bicyclo ring system having the thiazole ring as one of the cyclos514/375, Polycyclo ring system having the oxazole ring as one of the cyclos514/394, Benzo fused at 4,5-positions of the diazole ring514/398, Chalcogen or nitrogen bonded directly to the imidazole ring by nonionic bonding544/3, Six-membered hetero ring consists of sulfur, nitrogen, and carbon544/132, Five-membered hetero ring having two or more ring hetero atoms of which at least one is nitrogen544/139, 1,3-Diazole ring (including hydrogenated)544/236, At least three ring nitrogens in the bicyclo ring system544/262, The other cyclo in the bicyclo ring system is five-membered544/264, Purines (including hydrogenated)546/118, Three ring nitrogens in the bicyclo ring system546/139, Isoquinolines (including hydrogenated)546/152, Quinolines (including hydrogenated)546/199, Plural ring nitrogens in the polycyclo ring system548/153, At least three ring hetero atoms in the bicyclo ring system548/181, Polycyclo heterocyclic ring system containing ring nitrogen548/250, Tetrazoles (including hydrogenated)548/254, Nitrogen attached indirectly to the tetrazole ring by nonionic bonding548/305.4, The additional polycyclo ring system contains a 1,3-diazole [e.g., bis (benzimidazol-2-yl) stilene, etc.]548/305.7The polycyclo ring systems are bonded to the same acyclic carbon atom or to the same acyclic carbon chain (e.g., di-[2-benzimidazolyl)-methane; di-[benzimidazyl-(2)]-monohydroxyethylene, etc.)

Examiners

Primary: Richter, Johann
Assistant: Stockton, Laura L.

Attorney, Agent or Firm

Foreign Patent References

  • 0468470 EP. 01/11/1992

International Classes

A61K 031/42
A61K 031/415
C07D 403/10
C07D 403/04

Foreign Application Priority Data

1991-02-06 DE

Abstract

Disclosed herein are angiotensin-II antagonists of the formula ##STR1## wherein R1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R3 is, inter alia, lower alkyl; and, R4 is an acidic group, such as carboxyl or tetrazolyl.An exemplary compound is:(a) 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazole-2-yl)-benzimidazol-1-yl] methyl]-biphenyl-2-carboxylic acid.

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