Xention Limited

Bayer Aktiengesellschaft

Toshio Kokubo

Muneto Mogi

Nagahiro Yoshida

Noriyuki Yamamoto

Takeshi Yura

Klaus Urbahns

Toshiya Moriwaki

Tsutomu Masuda

Masaomi Tajimi

Hiroshi Fujishima

Yasuhiro Tsukimi

Masahiro Shiroo

William Johnston Scott

Martha E Rodriguez

Margaret Ann Popp

Ming Wang

Hiroshi Komura

Yingfu Li

Scott Miller

Timothy Lowinger

Arnel B Concepcion

Makiko Marumo

Norihiro Kawamura

Hiroko Yoshino

Gyoonhee Han

Aniko M Redmann

This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

Tetrahydro-naphthalene derivatives

This invention relates to tetrahydro-Naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tethrahydro&#x2014;Naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontienence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

This invention relates to tetrahydro-naphthalene derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence, inflammatory disorders such as asthma and COPD.

Hydroxy tetrahydro-naphthalenylurea derivatives

This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.

Tetrahydro-naphthalene derivatives as vanilloid receptor antagonists

This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. They have the general formula (I) in which Rrepresents hydrogen or Calkyl, and X represents &#x2014;N(H)Y, &#x2014;(H)&#x2014;CalkyleneY, biphenyl or Calkyl substituted by biphenyl, and the group Yis an optionally substituted biphenyl. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

A compound of the formula (I)in which Ris &#x2014;OR, &#x2014;SR, &#x2014;SOR, &#x2014;SOR, &#x2014;NHR, or &#x2014;NRR, and R, R, and Rare as defined broadly in the text. Ris H, C-Calkyl, carbamoyl, or an ester group. Ris thienyl, pyridyl optionally substituted by halogen or C-Calkoxy; naphthyl optionally substituted by C-Calkoxy; dioxane fused phenyl; dioxacyclopentane fused phenyl; or optionally substituted phenyl. Y is CH or N. A process for preparing such compounds, pharmaceutical compositions containing such compounds, and a method of treating asthma using them are also disclosed and claimed.

Imidazopyrimidine derivatives and triazolopyrimidine derivatives

Growing community of inventors

Nara-ken, Japan

Toshio Kokubo