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Intermediates for the preparation of antihypercholesterolemic tetrazole compounds

Patent 4898949 Issued on February 6, 1990. Estimated Expiration Date: Icon_subject February 18, 2008. 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

Mevalonolactone derivatives
Patent #: 4198425
Issued on: 04/15/1980
Inventor: Mitsui ,   et al.

Substituted pyranone inhibitors of cholesterol synthesis
Patent #: 4375475
Issued on: 03/01/1983
Inventor: Willard ,   et al.

Cholesterol biosynthesis inhibiting pyrazole analogs of mevalonolactone and its derivatives
Patent #: 4613610
Issued on: 09/23/1986
Inventor: Wareing

Prodrugs of antihypercholesterolemic compounds
Patent #: 4678806
Issued on: 07/07/1987
Inventor: Baldwin ,   et al.

Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis
Patent #: 4681893
Issued on: 07/21/1987
Inventor: Roth

Intermediates in the synthesis of indole analogs of mevalonolactone and derivatives thereof Patent #: 4739073
Issued on: 04/19/1988
Inventor: Kathawala

Inventors

Assignee

Application

No. 151512 filed on 02/18/1988

US Classes:

548/253, The chalcogen, X, is in a -C(=X)- group548/118The five-membered hetero ring contains at least three ring nitrogens

Examiners

Primary: Springer, David B.

Attorney, Agent or Firm

Foreign Patent References

  • EP24348 EP. 03/24/1981
  • EP68038 EP. 01/24/1983
  • EP142146 EP. 05/24/1985
  • WO02131 WO. 06/24/1984
  • WO02903 WO. 08/24/1984
  • WO07054 WO. 12/24/1986

International Class

C07D 257/04

Abstract

This invention provides novel tetrazole intermediates of the formula ##STR1## wherein R1 and R4 each are independently hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy or trifluoromethyl;R2,R3,R5 and R6 each are independently hydrogen, halogen, C1-4 alkyl or C1-4 alkoxy;B is hydrogen, C1-4 alkoxycarbonyl, CH2 Y or CH2 Z;Y is hydrogen, hydroxyl or X;Z is ##STR2## X is bromo, chloro or iodo; R10 is C1-4 alkyl; andR11 is phenyl which is unsubstituted or substituted by one or two C1-4 alkyl or chloro substituents.and processes thereof which are useful for the preparation of antihypercholesterolemic agents.

Other References

  • Buchanan et al., "J. Med. Chem.", 12, Nov. 1969, pp. 1001 & 1002
  • A. Endo, et al., Journal of Antibiotics, 29, 1346-1348 (1979)
  • A. W. Alberts, et al., J. Proc. Natl. Acad. Sci. U.S.A., 77, 3957 (1980)
  • G. E. Stokker, et al., J. Med. Chem., 28, 347-358 (1985)
  • W. F. Hoffman, et al., J. Med. Chem., 29, 159-169 (1986)
  • G. E. Stokker, et al., J. Med. Chem., 29, 170-181 (1986
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