Bayer Aktiengesellschaft

Xention Limited

Axikin Pharmaceuticals, Inc.

Actimis Pharmaceuticals, Inc.

Bayer Corporation

Beiersdorf Ag

Bayer Pharma Aktiengesellschaft

Bayer Healthcare Aktiengesellschaft

Bayer Pharmaceuticals Corporation

Klaus Urbahns

Toshiya Moriwaki

Kevin Bacon

Nagahiro Yoshida

Muneto Mogi

Masaomi Tajimi

Noriyuki Yamamoto

Takeshi Yura

Hiroshi Fujishima

Yasuhiro Tsukimi

Klemens Lustig

Tsutomu Masuda

Delf Schmidt

Christoph Gerdes

Elke Stahl

Beatrix Stelte-Ludwig

Takashi Yoshino

Takuya Shintani

Hiromi Sugimoto

Toshio Kokubo

Masahiro Shiroo

Toshiki Murata

J&ouml;rg Keldenich

Yingfu Li

Ulf Brueggemeier

Keiko Fukushima

Noriko Nunami

Josef Pernerstorfer

Andrea Vaupel

Markus Albers

Tai-wei Ly

Hilmar Bischoff

Timothy B Lowinger

Naoki Tsuno

Claudia Hirth-Dietrich

Yuji Koriyama

Mitsuyuki Shimada

Kinji Fuchikami

Hiroki Sato

Michael Woltering

Elke Dittrich-Wengenroth

Michael H&auml;rter

Megumi Yamauchi

Hiroko Yoshino

Berthold Hinzen

Makiko Marumo

Norihiro Kawamura

Susanne Nikolic

Kentaro Hashimoto

Naoki Omori

Issei Kato

Mami Miura

Florian Gantner

Akihiko Watanabe

Kazuho Tanaka

Yoshihisa Manabe

Masanori Seki

Tetsuo Kikuchi

William Johnston Scott

Jörg Keldenich

Heinrich Meier

Donald J Wolanin

David R Brittelli

Brian R Dixon

Peiying Liu

Jean De Vry

William H Bullock

Michael Härter

Nicole Diedrichs

Robert B Dally

Harold C E Kluender

Cedo Martin Bagi

Catherine R Brennan

Jeffrey Johnson

Jinshan Chen

Axel Bouchon

Anik&oacute; M Redman

Achim Hermann

Elke Reissmuller

Hiroaki Yuasa

Jang Gupta

Fumihiko Hayashi

Hideki Tsujishita

Ulf Br&uuml;ggemeier

William F Lathrop

William L Collibee

Carol Ann Mase

Hideki Jishita

Yuki Takekawa

Elke Reissmüller

Yoshino Hiroko

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

The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide 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.

Arylsulfonamide derivatives for use as CCR3 antagonists in the treatment of inflammatory and 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

The present invention relates to novel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-&#x3b3; inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-&#x3b3; activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoimmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.

Fused azole-pyrimidine 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 pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis. 

Pyrimidine derivatives useful for the treatment of diseases mediated by CRTH2

The present invention relates to an imidazo[1,2-c]pyrimidinylacetic acid derivative and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The imidazo[1,2-c]pyrimidinylacetic acid derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.

Imidazo[1,2-C]pyrimidinylacetic acid derivatives

Arylsulfonamide derivatives for use as ccr3 antagonists in the treatment of inflammatory and immunological disorders

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 a hydroxy-tetrahydro-naphthalene or an urea derivative formula (I) and salts thereof which are useful as active ingredients of pharmaceutical preparations, wherein A represents formula (II) or (III) wherein # represents the connection position to the molecule and Q, Q, Qand Qare defined, and E represents formula (IV) or (V) wherein # represents the connection position to the molecule and Q, Q, Q, Q, Q, R, na, ma, Xand Rare defined.

Tetrahydro-naphthalene and urea derivatives

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

The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-&#x3b3; inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-&#x3b3; activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoixnmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.

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

Growing community of inventors

Lund, Sweden

Klaus Urbahns