Daiichi Sankyo Company, Limited

Daiichi Asubio Pharma Co., Ltd.

Norihito Murayama

Naohiro Takemoto

Kenji Murata

Chikaomi Yamada

Hirokazu Annoura

Tsuyoshi Matsuo

Mayumi Furuya

Compounds of Formula (I) promote axonal outgrowth angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases, peripheral arterial occlusive diseases, or after-effects of these diseases. in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R, Rand Rare each independently a hydrogen atom, an alkyl group, or an amino group; E is an oxygen atom or an &#x2014;NRgroup (wherein Ris an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, or &#x2014;CO&#x2014;; and Q is a hydrogen atom or a phenyl group.

Nitrogen-containing six-membered aromatic ring derivatives and pharmaceutical products containing the same

Compounds of Formula (I) promote axonal outgrowth angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases, peripheral arterial occlusive diseases, or after-effects of these diseases. in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R, Rand Rare each independently a hydrogen atom, an alkyl group, or an amino group; E is an oxygen atom or an &#x2014;NRgroup (wherein Ris an alkyl group or the like); n is an integer of of 0 to 5; X and Y are each a connected bond, a cycloalkyl group, or &#x2014;CO&#x2014;; and Q is a hydrogen atom or a phenyl group.

Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R, Rand Rare each independently a hydrogen atom, an alkyl group, an amino group or the like; E is an oxygen atom or an &#x2014;NRgroup (wherein Ris an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, &#x2014;CO&#x2014; or the like; and Q is a hydrogen atom or a phenyl group.

The present invention relates to an aminophenoxyacetamide derivative of the formula (I): wherein Rto Rare, independent from each other, a hydrogen atom or an optionally substituted alkyl group; Eis &#x2014;NR&#x2014;; and Eis an oxygen atom or &#x2014;NR&#x2014;; Q is the group &#x2014;X&#x2014;Y-Q', wherein X and Y are connecting bonds or X is an alkylene or alkenylene group and Y is selected from a group comprising C&#x2550;O, NHC(&#x2550;), and C(&#x2550;O)NH, and Q&#x2032; is a hydrogen atom or a phenyl or pyridyl group which may be substituted; and pharmaceutically acceptable salts thereof. The present invention further relates to compositions comprising compounds of the formula (I) and methods of using said compounds for treating cerebral functional disorders and cerebral organic disorders.

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Tokyo, Japan

Norihito Murayama