Bayer Aktiengesellschaft

Masaomi Umeda

Toshiki Murata

Tsutomu Masuda

Karl Ziegelbauer

Takuya Shintani

Kinji Fuchikami

Hiroshi Komura

Yuji Koriyama

Hiroki Sato

Sachiko Sakakibara

Hiroshi Kadono

Timothy B Lowinger

Takashi Yoshino

Mitsuyuki Shimada

Timothy Lowinger

Takashi Yoshiro

Mitsuiyuki Shimada

Nagahiro Yoshida

Sachiko Sasaki

Yuka Ikegami

Makoto Shimazaki

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

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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Nara-ken, Japan

Masaomi Umeda