Santen Pharmaceutical Co., Ltd.

Ayumi Pharmaceutical Corporation

Yusuke Yamazaki

Minoru Yamamoto

Hisashi Tajima

Shinji Yoneda

Junko Fujikawa

Katsuhiko Watanabe

Noriko Mishina

Hiroyuki Mogi

Kenji Kawashima

Tomoko Oda

Takahiro Matsuyama

Daisuke Shii

Shinji Takaoka

Hiroyuki Aono

Satoshi Shirae

Tomomi Tanaka

Miwa Imamura

Iwao Seki

The 6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,2,4]triazepine derivatives or salts thereof of the present invention have BRD4 inhibitory activity, and thus, they are useful as medicaments, in particular, as prophylaxis and/or therapeutic agents for diseases associated with BRD4.

6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,2,4]triazepine derivative

The present invention relates to defined quinoxalin-2-one compounds or a pharmaceutically acceptable salt or a hydrate or a solvate thereof. The compounds, salts or hydrates have a glucocorticoid receptor agonist activity, and are useful as a medicine, in particular as a prophylactic or therapeutic agent for a glucocorticoid receptor related disease.

[4-(1,3,3-trimethyl-2-OXO-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or salt thereof

The present invention relates to a novel [4-(1,3,3-trimethyl-2-oxo-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or a salt thereof. The compound or a salt thereof of the present invention has a glucocorticoid receptor agonist activity, and is useful as a medicine, in particular as a prophylactic or therapeutic agent for the glucocorticoid receptor related disease.

[4-(1,3,3-trimethyl-2-oxo-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or salt thereof

A compound of formula (1): wherein Rand Rrepresent hydrogen, lower alkyl, lower alkenyl, lower alkynyl or Rrepresents hydroxyl, lower alkoxy, lower cycloalkyloxy, aryloxy, carboxy, lower alkoxycarbonyl, or NRRof the formula Rand Rrepresent halogen, lower alkyl, hydroxyl, or lower alkoxy; Rrepresents halogen, lower alkyl, aryl, heterocyclic, hydroxy, lower alkoxy, mercapto, lower alkylthio, lower alkylcarbonyl, amino, nitro or cyano; Rrepresents lower alkyl, hydroxyl or lower alkoxy; Rand Rrepresent hydrogen or lower alkyl; ring A represents a cyclic hydrocarbon or a heterocyclic ring; ring B represents a heterocyclic ring; X represents lower alkylene; Z represents a single bond or lower alkylene; Y represents lower alkylene and W&#x2014;Wrepresents CH&#x2014;CH, or Y represents a single bond and W&#x2014;Wrepresents N&#x2014;CH, CH&#x2014;N or CH&#x2014;CH; and 1, m, n and o represent 0, 1, 2, or 3.

Thiophenediamine derivative having urea structure

A compound having the following formula (1) or a salt thereof: wherein Rand Rrepresent hydrogen, a lower alkyl, a lower alkenyl, a lower alkynyl or a group having the following formula (2):(R)&#x2014;{circle around (A)}&#x2014;Z&#x2014;&#x2003;&#x2003;(2),Rrepresents hydroxy, a lower alkoxy, a lower cycloalkyloxy, an aryloxy, carboxy, a lower alkoxycarbonyl, or &#x2014;NRRhaving the following formula (3):(R)&#x2014;{circle around (B)}&#x2014;&#x2003;&#x2003;(3),Rand Rrepresent halogen, a lower alkyl, hydroxy, or a lower alkoxy; Rrepresents halogen, a lower alkyl, an aryl group, a heterocyclic, a hydroxy, a lower alkoxy, mercapto, a lower alkylthio, a lower alkylcarbonyl, amino, nitro or cyano; Rrepresents a lower alkyl, hydroxy or a lower alkoxy; Rand Rrepresent hydrogen or a lower alkyl; the ring A represents a cyclic hydrocarbon or a heterocyclic ring; the ring B represents a heterocyclic ring having one or more heteroatoms selected from the group consisting of nitrogen and oxygen; X represents a lower alkylene; Y represents a lower alkylene; Z represents a single bond or a lower alkylene; W-Wrepresents N&#x2014;CH or C&#x2014;N and l, m, n and o represent 0, 1, 2, or 3.

The present invention relates to a study on the synthesis of a novel N-(2-aminophenyl)benzamide derivative having an urea structure and represented by the general formula (1); and the utilization of a pharmacological effect of the derivative. A compound represented by the general formula (1) or a salt thereof has an effect of cellular morphological change on trabecular meshwork cells and is effective in the prevention and/or treatment of a disease considered to be related to intraocular pressure. In the formula, Rand Rrepresent a hydrogen atom, a lower alkyl group, or the like; Rrepresents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, or the like; Rand Rrepresent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, or the like; X represents a lower alkylene group or the like; Y represents a single bond, a lower alkylene group, or the like; l and m represent 0, 1, 2, or the like. 

N- (2-aminophenyl) benzamide derivative having urea structure

Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof. In the formula, Rand Rrepresent a hydrogen atom, a lower alkyl group or the like; Rrepresents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, a carboxy group, a lower alkoxycarbonyl group, &#x2014;OCONRR, &#x2014;NRRor the like; Rand Rrepresent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or the like; Rand Rrepresent a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group, a heterocyclic group or the like; Rand Rrepresent a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group or the like; X represents a lower alkylene group; Y represents a single bond, a lower alkylene group; W-Wrepresents N&#x2014;C or C&#x2014;N; and l and m represent 0, 1, 2 or 3. 

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Ikoma, Japan

Yusuke Yamazaki