The present invention relates to novel compounds according to Formula I or II, methods, and compositions capable of decreasing HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF). Formula (I) or (II). ##STR00001##

Zhou; Xiaoti

Arend; Michael P.

Wu; Min

Flippin; Lee A.

Fibrogen, Inc.

Isothiazole-pyridine derivatives as modulators of HIF (hypoxia inducible factor) activity

FibroGen, Inc.

The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF).

Pyrrolo- and Thiazolo-pyridine compounds, and methods of use thereof

The present invention relates to compounds represented by the general formula (I): ##STR1## wherein R.sub.1 is H or methoxy, R.sub.2 is H, methoxy, OH or F, R.sub.3 is H or F, R.sub.4 is H or F at 7-, 8- or 9-position, and .circle.Ar is a benzene, thiophene or pyridine ring, provided that (i) at least two of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, (ii) R.sub.2 or R.sub.3 is F when R.sub.4 is F, (iii) R.sub.1, R.sub.3 and R.sub.4 are H when R.sub.2 is methoxy or OH, (iv) R.sub.2 and R.sub.3 are not simultaneously F, and (v) R.sub.2 and R.sub.3 are H or F, and both R.sub.1 and R.sub.4 are H when .circle.Ar is a thiophene or pyridine ring, or a physiologically acceptable acid addition salt thereof. The compounds of the present invention have an excellent protective effect against cerebral anoxia and some of them have also an inhibitory effect on lipid peroxidation of mitochondrial membrane of brain and an anti-convulsant activity and are useful as an agent for prevention or treatment of cerebral diseases caused by hypoxia in mammals including human.

Dainippon Pharmaceutical Co., Ltd.

Dibenz[b,e]oxepin derivatives and pharmaceutical composition containing the same

pyridine

hypoxia

pyridine/hypoxia

Isothiazole-pyridine derivatives as modulators of HIF (hypoxia inducible factor) activity

Isothiazole-pyridine derivatives as modulators of HIF (hypoxia inducible factor) activity

Pyrrolo- and Thiazolo-pyridine compounds, and methods of use thereof

Dibenz[b,e]oxepin derivatives and pharmaceutical composition containing the same

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