Chugai Seiyaku Kabushiki Kaisha

Kousuke Aso

Kihito Hada

Masami Hasegawa

Hiroshi Koyano

Atsushi Suda

Miyuki Asai

Yasuko Sato

Compounds having high angiogenesis inhibiting activity useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, e.g. cancer and cancer metastasis, are of formula (II), where Ais C&#x2014;Xor N; Qis -A=A-, or a heteroatom selected from &#x2014;O&#x2014;, &#x2014;S&#x2014;, and &#x2014;N(R)&#x2014;; Qis -A=A-, or a heteroatom selected from &#x2014;O&#x2014;, &#x2014;S&#x2014;, and &#x2014;N(R)&#x2014;; provided that Qand Qare not heteroatoms at the same time; Ais C&#x2014;Xor N, Ais C&#x2014;Xor N, Ais C&#x2014;Xor N, and Ais C&#x2014;Xor N; Y is Calkyl, Ccycloalkyl, Calkenyl, Calkynyl, Calkoxy, Calkenyloxy, Calkynyloxy, or Calkylthio; Z is a hydrogen atom, hydroxy, Calkyl, Ccycloalkyl, or &#x2014;NRR; and L is selected from the formula: 

Benzamide derivative

To provide compounds which have high angiogenesis inhibiting activity, and are useful as agents for effective treatment and prevention of diseases involving pathologic angiogenesis, for example, cancer and cancer metastasis, methods for producing the compounds, intermediate compounds useful for their production, and pharmaceutical compositions containing these compounds. The present invention provides compounds of formula (II), or prodrugs thereof, or pharmaceutically acceptable salts of the compounds or the prodrugs, and pharmaceuticals, and pharmaceutical compositions containing these compounds: where Ais C&#x2014;Xor N; Qis &#x2014;A&#x2550;A&#x2014;, or a heteroatom selected from &#x2014;O&#x2014;, &#x2014;S&#x2014;, and &#x2014;N(R)&#x2014;; Qis &#x2014;A&#x2550;A&#x2014;, or a heteroatom selected from &#x2014;O&#x2014;, &#x2014;S&#x2014;, and &#x2014;N(R)&#x2014;; provided that Qand Qare not heteroatoms at the same time; Ais C&#x2014;Xor N, Ais C&#x2014;Xor N, Ais C&#x2014;Xor N, and Ais C&#x2014;Xor N; Y is Calkyl, Ccycloalkyl, Calkenyl, Calkynyl, Calkoxy, Calkenyloxy, Calkynyloxy, or Calkylthio; Z is a hydrogen atom, hydroxy, Calkyl, Ccycloalkyl, or &#x2014;NRR; and L is selected from the formula: 

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Kamakura, Japan

Kousuke Aso