Daewoong Pharmaceutical Co., Ltd.

Hong-Chul Yoon

Ji Duck Kim

In Woo Kim

Hyae Jung Hyun

In Young Lee

Min Jae Cho

Sang Ho Lee

Inwoo Kim

Seong Hee Cho

Sang Hyun Nam

Eunkyung Park

Kwon Jo Lim

Eun Kyung Park

Disclosed are biaryl benzoimidazole derivatives. They have an inhibitory effect on calcium influx in HEK cells, thereby showing a powerful antagonistic effect on a vanilloid receptor, and further have an analgesic effect, thereby being useful for preventing or treating pain, acute pain, chronic pain, neuropathic pain, postoperative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurological illness, neurodermatitis, stroke, bladder hypersensitivity, irritable bowel syndrome, a respiratory disorder such as cough, asthma, and chronic obstructive pulmonary disease, burning, psoriasis, itching, vomiting, irritation of the skin, eyes, and mucous membranes, gastric-duodenal ulcers, inflammatory intestinal diseases, and inflammatory diseases.

Biaryl benzoimidazole derivatives and pharmaceutical composition comprising the same

Disclosed are biaryl benzoimidazo derivatives. They have an inhibitory effect on calcium influx in HEK cells, thereby showing a powerful antagonistic effect on a vanilloid receptor, and further have an analgesic effect, thereby being useful for preventing or treating pain, acute pain, chronic pain, neuropathic pain, postoperative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurological illness, neurodermatitis, stroke, bladder hypersensitivity, irritable bowel syndrome, a respiratory disorder such as cough, asthma, and chronic obstructive pulmonary disease, burning, psoriasis, itching, vomiting, irritation of the skin, eyes, and mucous membranes, gastric-duodenal ulcers, inflammatory intestinal diseases, and inflammatory diseases.

Biaryl benzolmidazole derivatives and pharmaceutical composition comprising the same

The present invention relates to a novel benzoxazine benzimidazole derivative of formula (1) as an antagonist against a vanilloid receptor-1, a pharmaceutical composition comprising the same as an active ingredient, and a use thereof. The benzoxazine benzimidazole derivative of the present invention may be useful for preventing or treating a disease associated with antagonistic activity of vanilloid receptor-1: 

Benzoxazine benzimidazole derivative, a pharmaceutical composition comprising the same, and a use thereof

Discloses is a benzoxazine benzimidazole derivative, represented by Chemical Formula 1, functioning as an antagonist to the vanilloid receptor-1, a pharmaceutical composition comprising the same, and the use thereof. The benzoxazine benzimidazole derivative can be useful for preventing or treating a disease associated with antagonistic activity of vanilloid receptor-1, without hyperthermia: wherein, R, R, R, Rand Rare as defined in the specification.

Pyridyl benzoxazine derivatives, pharmaceutical composition comprising the same, and use thereof

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Paju-si, South Korea

Hong-Chul Yoon