Xention Limited

Bayer Aktiengesellschaft

Axikin Pharmaceuticals, Inc.

Bayer Healthcare Aktiengesellschaft

Nagahiro Yoshida

Toshiya Moriwaki

Klaus Urbahns

Muneto Mogi

Tsutomu Masuda

Noriyuki Yamamoto

Takeshi Yura

Masaomi Tajimi

Hiroshi Fujishima

Yasuhiro Tsukimi

Toshio Kokubo

Masahiro Shiroo

Yingfu Li

Makiko Marumo

Naoki Tsuno

Kevin Bacon

Hiromi Sugimoto

Hiroshi Komura

Keiko Fukushima

Timothy Lowinger

Noriko Nunami

Kentaro Hashimoto

Karl-Heinz Schlemmer

William Johnston Scott

Bernd Riedl

Martha E Rodriguez

Margaret Ann Popp

Bernard Schmidt

Toshiki Murata

Takashi Yoshino

Mitsuyuki Shimada

Ming Wang

Karl Ziegelbauer

Franz-Josef Van Der Staay

Takuya Shintani

Kinji Fuchikami

Chantal F&uuml;rstner

Masaomi Umeda

Scott Miller

Arnel B Concepcion

Werner Schr&ouml;der

Norihiro Kawamura

Hiroko Yoshino

Frank B&ouml;ss

Yuka Ikegami

Jens-Kerim Erg&uuml;den

Sachiko Sasaki

Aniko M Redmann

Gyoonhee Han

Makoto Shimazaki

Provided herein are 2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity. These compounds are useful for the treatment of diseases associated with CCR3 activity, including but not limited to, atopic dermatitis, allergic rhinitis, rheumatoid arthritis, Grave's disease, HIV infection, Alzheimer's disease, atherosclerosis and other inflammatory and/or immunological disorders.

2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity for the treatment of inflammatory or immunological disorders

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.

The present invention relates to a benzenesulfonamide derivative of formula (I), which is useful as an active ingredient of pharmaceutical preparations. The benzenesulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders. In said formula, X represents O or S; Rrepresents formulae (a), (b), (c), (d), (e), (f), (g), (h), (i) or (j), the other substituents are as defined in claim

2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity for the treatment of asthma and other inflammatory or immunological disorders

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 hydroxy-tetrahydro-naphthalenylurea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The hydroxy-tetrahydro-naphthalenylurea derivatives of the present invention have an excellent activity as VR1 antagonist 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.

Hydroxy-tetrahydro-naphthalenylurea derivatives

4-aryl pyrimidine compounds of general formula and salts thereof: wherein X is CH or N; R1 is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, etc.; R2 is hydrogen or hydroxy; R3 is hydrogen, C1-6 alkyl, etc.; R4 is hydrogen, hydroxy, halogen, amino, etc.; R5 is hydroxy, amino, carboxy, etc.; R6 is hydrogen, carbamoyl, cyano, carboxy, C1-6 alkoxycarbonyl, etc. and R7 is amino or C1-6 alkanoylamino. The compounds (I) or the salts thereof have an excellent anti-inflammatory activity and the like.

4-6-diphenyl pyridine derivatives as antiinflammatory agents

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

The invention relates to novel 3-oxo-2,1-benzisomazol-1(3H)-carboxamides (I), where R , R are the same or different and independently&equals;H, halogen, C C alkyl C C alkoxy, C C perfluoroalkyl, or a group NR R ; R , R are the same or different and independently&equals;C C alkyl, whose carbon chain is optionally interrupted by an O, S or NR and is optionally singly or severally substituted by C C cycloalkyl, C C alkoxy, OH, halogen or NR R ; C C cycloalkyl whose carbon chain is optionally interrupted by an O, S or NR and is optionally singly or severally substituted by C C alkoxy, OH, halogen or NR R , or R and R together with a nitrogen atom form a saturated or partially unsaturated - to -membered mono- or bi-cyclic heteocycle, which, optionally, contains up to two further heteroatoms, from N, O or S and is, optionally, substituted by C C alkyl, C C alkoxy, OH, halogen, COOR or NR R and X&equals;O or S. The invention further relates to methods for production thereof and use thereof in the production of medicaments for the prophylaxis and/or treatment of diseases of the central nervous system, in particular, cognitive disorders, such as Alzheimer's disease and other forms of dementia, cerebral infarct, skull and brain trauma and pain.

3-oxo-2,1-benzisoxazol-1(3H)-carboxamides for treatment of CNS diseases

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Kyoto-fu, Japan

Nagahiro Yoshida