Aska Pharmaceutical Co., Ltd.

Teikoku Hormone Mfg. Co., Ltd.

Teikoju Hormone Mfg. Co., Ltd.

Akira Asagarasu

Teruaki Matsui

Michitaka Sato

Shuichiro Sato

Norio Yamamoto

Jun Sato

Makoto Okada

Nobuyoshi Minami

Satoshi Doi

Takahisa Saito

Motohiro Kobayashi

Koichi Hasumi

Katsuyuki Keino

Shuji Ohta

Hajime Asano

Arihiro Kanada

Hiroshi Uchida

Hideo Kobayashi

Kotaro Gotanda

Youichi Nakano

Atsushi Shinbo

Hiroyuki Hayashi

Satoru Tamaoki

Yoshiko Yamamoto

Chisato Ogawa

Yukinao Yamauchi

Nobuyuki Takahashi

Sei-ichi Araki

Norihito Isomura

Yosuke Takenaka

Sei-Ichi Araki

Provided is a process for producing a compound, which has an oxo group specifically introduced on the 15-position of a steroid skeleton and which is useful as an intermediate, with a high yield without complicated steps. A compound represented by the formula (2) is allowed to react with an oxidant (e.g., a hypervalent iodine compound) and a co-oxidant (e.g., a peroxide) to produce a 15-oxosteroid compound represented by the formula (1), which is useful as an intermediate: wherein Rto Rare the same or different and each represent a halogen atom, an alkyl group, a haloalkyl group, an alkoxy group, or a haloalkoxy group, Rrepresents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, an acyl group, or an alkoxycarbonyl group, Rrepresents a hydrogen atom, an alkyl group, or an acyl group, Rrepresents a hydrogen atom, an alkyl group, an acyl group, or a sulfonyl group, X represents an oxygen atom (O) or a methylene group (CH).

15-oxosteroid compound and process for producing the same

A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27is provided. The compound or the salt thereof is represented by the following formula (1): 

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This invention provides thienopyrimidine derivatives of the formula, 

Thienopyrimidine derivatives

The invention discloses quinazoline derivatives or salts thereof, which possess PDE9-inhibiting activity and are useful as treating agents of dysuria and the like, the derivatives being represented by the formula (I) 

Quinazoline derivatives

This invention provides pyrimidine derivatives represented by a formula,  or a salt thereof, which concurrently exhibit 5-HTagonistic activity and 5-HTantagonistic activity and are useful for therapy and treatments of diseases such as IBS. The invention furthermore provides a therapeutic method of IBS, characterized by having 5-HTagonistic activity and 5-HTantagonistic activity work simultaneously and cooperatively in vivo, which comprises either administering 5-HTantagonistic agent which concurrently exhibits 5-HTagonistic activity, or administering 5-HTagonistic agent and 5-HTantagonistic agent simultaneously, in sequence or at an interval.

Pyrimidine derivatives

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

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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Machida, Japan

Akira Asagarasu