Bayer Aktiengesellschaft

Bayer Pharma Aktiengesellschaft

Bayer Healthcare Aktiengesellschaft

Bayer Pharmaceuticals Corporation

Kinji Fuchikami

Toshiki Murata

Yuji Koriyama

Mitsuyuki Shimada

Tsutomu Masuda

Karl Ziegelbauer

Takuya Shintani

Hiroki Sato

Hiroshi Komura

Masaomi Umeda

Sachiko Sakakibara

Timothy B Lowinger

Takashi Yoshino

Hiroshi Kadono

Kevin Bacon

Klaus Urbahns

Timothy Lowinger

Naoki Omori

Issei Kato

Mami Miura

Florian Gantner

Takashi Yoshiro

Mitsuiyuki Shimada

Rolf Grosser

Nagahiro Yoshida

Noriko Nunami

Keiko Fukushima

Megumi Yamauchi

Makoto Shimazaki

Hideki Tsujishita

Sachiko Sasaki

Hideki Jishita

Yuka Ikegami

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

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.

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

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

An optically active (&#x2212;)-7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-5-[(3S)-3-piperidinyl]-1,4-dihydro-2H-pyrido[2,3-d][1,3]oxazin-2-one of the formula (I) or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity 

Optically active pyridine derivative and a medicament containing the same

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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Kyoto-fu, Japan

Kinji Fuchikami