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US 5,919,779 AGranted
5,6-Heteroaryl-dipyrido(2,3-B:3', 2'-F) azepines and their use in the prevention or treatment of HIV infection
AssigneeBoehringer Ingelheim Pharmaceuticals, Inc.
InventorsJohn R. Proudfoot, Karl D. Hargrave, Suresh Kapadia
Life of this patent
Estimating the term…
Abstract
"There are disclosed compounds of the formula I, II or III ##STR1## wherein A and D are carbon or nitrogen and B is oxygen, sulfur or nitrogen which are useful in the prevention or treatment of HIV infection."
Claims7
A compound of formula I, formula II or formula III ##STR24## wherein:
- in formula I, formula II and in formula III, A and D are carbon (unsubstituted or optionally substituted with methyl, ethyl, isopropyl, vinyl, isopropenyl, ethynyl, halogen, nitro, cyano, amino, methylamino, dimethylamino, hydroxy, methoxy, mercapto or methylthio) or nitrogen, and B is oxygen, sulfur or nitrogen (unsubstituted or optionally substituted with methyl, ethyl, isopropyl, hydroxy or methoxy);
- and,
- R.sub.1 is a hydrogen atom, alkyl of 1 to 4 carbon atoms, fluoroalkyl of 1 to 4 carbon atoms and 1 to 3 fluorine atoms, cycloalkyl of 3 to 6 carbon atoms, oxetanyl, thietanyl, tetrahydrofuranyl, tetrahydrothienyl, tetrahydropyranyl, tetrahydrothiopyranyl, alkenylmethyl or alkynylmethyl of 3 to 4 carbon atoms, alkyloxyalkyl or alkylthioalkyl of 2 to 3 carbon atoms, alkanoyl or alkyl(thiocarbonyl) of 2 to 5 carbon atoms, or cyanoalkyl of 2 to 3 carbon atoms;
- R.sub.2 is a hydrogen atom, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, alkenyl or alkynyl of 2 to 6 carbon atoms, trihalomethyl, hydroxyalkyl of 1 to 6 carbon atoms, alkyloxy or alkylthio of 2 to 6 carbon atoms, alkyloxyalkyl or alkylthioalkyl of 2 to 6 carbon atoms, pyrrolidinyl, pyrrolinyl, piperidinyl, mono- or di-alkylamino wherein each alkyl moiety contains 1 to 3 carbon atoms, halogen, cyano, nitro, or carboxyl, aryl (wherein aryl is phenyl, pyridinyl, thienyl, furanyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl or isothiazolyl) which is either unsubstituted or substituted by hydroxyl, amino, halogen, alkyl or alkyloxy of 1 to 3 carbon atoms;
- R.sub.3 is a hydrogen atom, methyl or halogen;
- R.sub.4 is a hydrogen atom, methyl, ethyl or halogen;
- R.sub.5 is a hydrogen atom, hydroxy, amino, hydroxymethyl or aminomethyl;
- or a pharmaceutically acceptable salt thereof.
5 more elements
A compound selected from the group consisting of:
- 11-Ethyl-thienyl2',3':6,5!dipyrido2,3-b:3',2'-f!azepine;
- 11-Ethyl-thienyl3',4':6,5!dipyrido2,3-b:3',2'-f!azepine;
- and
- 2-chloro-11-Ethyl-thienyl2',3':6,5!dipyrido2,3-b:3',2'-f!azepine;
- 2-(4-pyrazolyl)-11-Ethyl-thienyl2',3':6,5!dipyrido2,3-b:3',2'-f!azepine;
- 11-Ethyl-thiazolyl4',5':6,5!dipyrido3,2-b:2',3'f!azepine;
- 11-Ethyl-oxazolyl 4',5":6,5!dipyrido3,2-b:2',3'-e!azepine;
- and,
- 11-Ethyl-thiadiazolyl4',5':6,5!dipyrido3,2-b:2',3'-e!azepine;
- or pharmaceutically acceptable salts thereof.
7 more elements
2-(4-Pyrazolyl)-11-ethyl-thienyl2',3':6,5 !dipyrido2,3-b:3',2'-f!azepine.
Dependencies are inferred from the claim text.