U.S. patents available from 1976 to present.
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Heterocyclic ketones

Patent 5164371 Issued on November 17, 1992. Estimated Expiration Date: Icon_subject November 17, 2009. 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

Proline derivatives
Patent #: 4596789
Issued on: 06/24/1986
Inventor: Dutta ,   et al.

Peptide elastase inhibitors and methods
Patent #: 4643991
Issued on: 02/17/1987
Inventor: Digenis ,   et al.

Proline derivatives
Patent #: 4691007
Issued on: 09/01/1987
Inventor: Dutta ,   et al.

Selected difluoro derivatives
Patent #: 4880780
Issued on: 11/14/1989
Inventor: Trainor, et al.

Peptide derivatives Patent #: 4910190
Issued on: 03/20/1990
Inventor: Bergeson, et al.

Inventors

Assignee

Application

No. 193317 filed on 05/11/1988

US Classes:

514/18, 3 or 4 peptide repeating units in known peptide chain514/19, 2 peptide repeating units in known peptide chain530/331, Tripeptides, e.g., tripeptide thyroliberin (TRH), melanostatin (MIF), etc.544/297, Nitrogen attached directly at 2-position by nonionic bonding and sulfur bonded directly to the nitrogen544/322, Nitrogen attached directly to diazine ring by nonionic bonding544/333, Additional hetero ring which is unsaturated546/293, Sulfur bonded directly to acyclic nitrogen546/306, Plural acyclic nitrogens bonded directly to the same carbon or single bonded directly to each other546/332, Plural acyclic nitrogens bonded directly to the same carbon or single bonded directly to each other548/110, Boron or silicon containing548/159, Additional polycyclo heterocyclic ring system containing548/179, Chalcogen attached indirectly to the bicyclo ring system by nonionic bonding548/188, The -C(=X)- group is bonded directly to the thiazole ring548/205, Nitrogen attached indirectly to the thiazole ring by nonionic bonding548/217, Polycyclo ring system having the oxazole ring as one of the cyclos548/228, Chalcogen bonded directly at 5-position of the oxazole ring548/233, Nitrogen bonded directly to ring carbon of the oxazole ring548/235, Plural double bonds between the ring members of the oxazole ring548/237One double bond between the ring members of the oxazole ring

Examiners

Primary: Bond, Robert T.
Assistant: Ward, Edward C.

Attorney, Agent or Firm

International Classes

C07D 237/08
C07D 239/06
C07K 005/08
A61K 037/02

Foreign Application Priority Data

1987-05-11 GB

Abstract

The invention provides a series of novel heterocyclic ketones of formula I ##STR1## and pharmaceutically acceptable base-addition salts thereof, in which the values of R4, L, A, X and Q have the meanings defined in the following specification. The compounds of formula I are inhibitors of human leukocytic elastase. The invention also provides pharmaceutical compositions containing a compound of formula I, or a pharmaceutically acceptable base-addition salt thereof, and processes and intermediates for the manufacture of compounds of formula I.

Other References

  • R. Graf, "Reactions with N-Carbonylsulfamoyl Chloride", Angew. Chem. Internat. Edit. (1968), 7, 172-182
  • Chemical Abstracts, vol. 95, No. 25, 21st Dec. 1981, p. 223, abstract No. 216963a, Columbus, Ohio, U.S.; B. M. Ashe et al.: "Selective inhibition of human leukocyte elastase and bovine alpha-chymotrypsin by novel heterocycles", J. Biol. Chem. 1981, 256(22), 11603-6 *Abstract*
  • Chemical Abstracts, vol. 97, No. 7, 16th Aug. 1982, p. 268, abstract No. 51652z, Columbus, Ohio, U.S.; T. Teshima et al.: "A new class of heterocyclic serine protease inhibitors. Inhibition of human leukocyte elastase, porcine pancreatic elastase, cathepsin G, and bovine chymotrypsin A, with substituted benzoxazinones, quinazolines, and anthranilates", J. Bio. Chem. 1982, 257(9), 5085-5091 *Abstract
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