Bayer Aktiengesellschaft

Xention Limited

Pfizer Corporation

Bayer Healthcare Aktiengesellschaft

Tsutomu Masuda

Nagahiro Yoshida

Muneto Mogi

Klaus Urbahns

Toshiya Moriwaki

Masaomi Tajimi

Noriyuki Yamamoto

Takeshi Yura

Hiroshi Fujishima

Yasuhiro Tsukimi

Toshiki Murata

Karl Ziegelbauer

Takuya Shintani

Kinji Fuchikami

Toshio Kokubo

Hiroshi Komura

Masahiro Shiroo

Masaomi Umeda

Yuji Koriyama

Hiroki Sato

Hiroshi Kadono

Sachiko Sakakibara

Timothy B Lowinger

Takashi Yoshino

Mitsuyuki Shimada

Timothy Lowinger

Takashi Yoshiro

Mitsuiyuki Shimada

Kazuo Ando

Makoto Kawai

Hirofumi Omura

Sachiko Sasaki

Yuka Ikegami

Makoto Shimazaki

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 compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R, Rand Rare each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthma, dermatitis, seasonal allergic rhinitis, gastroesophageal reflux disease (GERD), constipation, diarrhea, functional gastrointestinal disorder, cutaneous T cell lymphoma, multiple sclerosis, osteoarthritis, psoriasis, systemic lupus erythematosus, diabetes, glaucoma, osteoporosis, glomerulonephritis, renal ischemia, nephritis, hepatitis, cerebral stroke, vasculitis, myocardial infarction, cerebral ischemia, reversible airway obstruction, adult respiratory disease syndrome, chronic obstructive pulmonary disease (COPD), cryptogenic fibrosing alveolitis or bronchitis. 

Benzimidazolone derivatives as CB2 receptor ligands

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

Pyrimidine compounds of general formula: wherein &#x2014;Rrepresents in which Ris hydrogen, Calkyl, halogen, hydroxy, Calkoxy, nitro, amino, Calkylsulfonylamino, Calkoxycarbonyl, Calkylamino, di (Calkyl)amino, Calkanoylamino, phenyl Calkylamino, phenylsulfonylamino, or &#x2014;O&#x2014;(CH)&#x2014;R; Rrepresents hydrogen or halogen; Rrepresents hydrogen, &#x2014;CRRR; Ris hydrogen, carbamoyl, CN, carboxyl, etc.; Ris amino, Calkylamino, di Calkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.

Pyridine derivatives

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.

This invention is to provide a process for producing 2-amino-4,6-disubstituted nicotinic acid ester analogs and salts thereof, comprising the reaction shown by the following scheme. The ester analogs can be prepared in one pot, and in good yield by using tertiary alkyl cyanoacetate. Furthermore, the method is useful for preparing derivatives of various analogs of the ester, e.g. alkyl substituted and aryl substituted analogs. 

Pyridine compounds of general formula:wherein &#x2014;Rrepresentsin which Ris hydrogen, Calkyl, halogen, hydroxy, Calkoxy, nitro, amino, Calkylsulfonylamino, Calkoxycarbonyl, Calkylamino, di (Calkyl)amino, Calkanoylamino, phenyl Calkylamino, phenylsulfonylamino, or &#x2014;O&#x2014;(CH)&#x2014;R; Rrepresents hydrogen or halogen; Rrepresents 1.2.3.6-tetrahydro-pyridine, or &#x2014;CRRRwherein Rrepresents H or Calkyl and Rand Rare joined to form a 5-8 membered saturated ring optionally containing up to three heteroatoms; Ris carbamoyl, CN, carboxyl, etc.; Ris amino, Calkylamino, di Calkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.

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Aichi-ken, Japan

Tsutomu Masuda