Teikoku Hormone Mfg. Co., Ltd.

Teikoju Hormone Mfg. Co., Ltd.

Arihiro Kanada

Nobuyoshi Minami

Katsuyuki Keino

Jun Sato

Michitaka Sato

Shuichiro Sato

Satoshi Doi

Akira Asagarasu

Takahisa Saito

Norio Yamamoto

Teruaki Matsui

Koichi Hasumi

Motohiro Kobayashi

Shuji Ohta

Hajime Asano

Koichi Miyazaki

The invention provides crystals of N-(N,N-dimethyl-L-valyl)-N-[(1S,2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[(2-phenylethyl)amino]propyl]-1-pyrrolidinyl]-1-[(S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide or salts thereof which possess potent antitumor activity and methods for their preparation.

Method of making tetrapeptide derivative TZT-1027 crystal

Substituted pyrazole compounds represented by formula (I), or salts thereof are disclosed, wherein Ris &#x2014;CH(OH)&#x2014;CH(R)-(A)-Y, &#x2014;CH&#x2014;CH(R)-(A)-Y, &#x2014;CO-B-A-Y or the like (wherein A is a lower alkylene; Y is an aryl group which may be substituted, for example, by halogen, or the like; Ris a hydrogen atom or a lower alkyl group; Bis &#x2014;CH(R)&#x2014; or &#x2014;N(R)&#x2014;; and n is 0 or 1); Ris a hydrogen atom, a lower alkyl group which may be substituted by hydroxyl or the like, or an aralkyl group; Ris a phenyl group which may be substituted by halogen or the like, or a pyridyl group; and Q is a pyridyl or quinolyl group. These substituted pyrazole compounds or their salts have an excellent p38MAP kinase inhibiting effect and are hence useful in the prevention or treatment of tumor necrosis factor &#x3b1;-related diseases, interleukin 1-related diseases, interleukin 6-related diseases or cyclooxygenase II-related diseases 

Substituted pyrazole compounds

Tetrapeptide derivative TZT-1027 crystal

Substituted pyrazole compounds represented by formula (I), or salts thereof are disclosed, wherein R is &mdash;CH(OH)&mdash;CH(R )&mdash;(A) &mdash;Y, &mdash;CH &mdash;CH(R )&mdash;(A) &mdash;Y, &mdash;CO&mdash;B &mdash;A&mdash;Y or the like (wherein A is a lower alkylene; Y is an aryl group which may be substituted, for example, by halogen, or the like; R is a hydrogen atom or a lower alkyl group; B is &mdash;CH(R )&mdash; or &mdash;N(R )&mdash;; and n is 0 or 1); R is a hydrogen atom, a lower alkyl group which may be substituted by hydroxyl or the like, or an aralkyl group; R is a phenyl group which may be substituted by halogen or the like, or a pyridyl group; and Q is a pyridyl or quinolyl group. These substituted pyrazole compounds or their salts have an excellent p38MAP kinase inhibiting effect and are hence useful in the prevention or treatment of tumor necrosis factor &agr;-related diseases, interleukin 1-related diseases, interleukin 6-related diseases or cyclooxygenase II-related diseases.

Aminopyrazole derivatives

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Kawasaki, Japan

Arihiro Kanada