Santen Pharmaceutical Co., Ltd.

Ayumi Pharmaceutical Corporation

Kenji Kawashima

Shin-Ichiro Hirai

Minoru Yamamoto

Takahiro Honda

Kazuyoshi Okamoto

Hisashi Tajima

Mamoru Matsuda

Hiroshi Enomoto

Toshiyuki Mori

Masatomo Kato

Miwa Takai

Masato Nagatsuka

Sachiko Kobayashi

Tomoko Oda

Masaaki Murai

Masakazu Ban

Yusuke Yamazaki

Takaaki Inaba

Shinji Takaoka

Yoshimasa Sasabuchi

Kazuhiro Kudou

Daisuke Shii

Takahiro Matsuyama

Noriko Ishizaka

Hiroyuki Aono

Shin-ichiro Hirai

Noriko Kawashima

Yuriko Takeno

Yasutaka Fujioka

Tomomi Tanaka

Koji Ohashi

Yukie Fujita

Iwao Seki

Satoshi Shirae

Hiroaki Kurashima

Miwa Imamura

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 represented by the following general formula (1) or a salt thereof. Rrepresents a halogen atom and so on; Rand Reach represent a hydrogen atom and so on; Rand Reach represent a hydrogen atom and so on, or Rand Rmay form an oxo group; Rand Reach represent a lower alkyl group optionally having a substituent and so on, or they may bind to each other to form a nitrogen-containing heterocyclic ring which may be substituted by one or plural R; Rrepresents an aryl group optionally having a substituent and so on; ring A represents a benzene ring and so on; and m represents 0, 1 or 2. 

Compound having PARP inhibitory activity

A 1,2,3,4-tetrahydroquinoxaline compound represented by the following formula: In the formula (1), Rrepresents substituents such as a halogen, an alkyl, a cycloalkyl, an aryl or a heterocyclic group; p represents 0 to 5; Rrepresents substituents such as a halogen, an alkyl, a hydroxyl or an alkoxy group; q represents 0 to 2; Rrepresents substituents such as hydrogen, an alkyl, an alkenyl, an alkylcarbonyl or an arylcarbonyl group; Rand Rindependently represent substituents such as hydrogen, a halogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; Rrepresents substituents such as hydrogen, an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl or a heterocyclic group; A represents an alkylene; Rrepresents OR, NRR, SR, S(O)R, S(O)R; Rand Rindependently represent substituents such as hydrogen, an alkyl or an alkenyl; and X represents O or S.

1,2,3,4-tetrahydroquinoxaline compounds having glucocorticoid receptor binding activity

An object of the present invention is to synthesize a novel 1,2,3,4-tetrahydroquinoxaline derivative represented by formula (1) and to find a pharmacological action of the derivative. In the formula, the Rrepresents a halogen, an alkyl, cycloalkyl, aryl or heterocyclic group, or the like; p represents 0 to 5; Rrepresents a halogen, an alkyl, hydroxyl or alkoxy group, or the like; q represents 0 to 2; Rrepresents hydrogen, an alkyl, alkenyl, alkylcarbonyl or arylcarbonyl group, or the like; Rand Rindependently represent hydrogen, a halogen, an alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heterocyclic group, or the like; Rrepresents hydrogen, an alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heterocyclic group, or the like; A represents an alkylene; Rrepresents OR, NRR, SR, S(O)R, S(O)R; and X represents O or S. 

1,2,3,4-tetrahydroquinoxaline derivative having glucocorticoid receptor binding activity

A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; Rand Rare hydrogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or Rand Rjoin together to form a heterocycle; X and Y are hydrogen, halogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.

Compounds having 4-pyridylalkylthio group as a substituent

A method of treating a disease associated with angiogenesis by administering a therapeutically effective amount of a compound represented by the formula (1) or a salt thereof wherein the ring X represents Rand Rindependently represent a hydrogen atom, an alkyl, an aryl or an aromatic heterocyclic; Rrepresents a hydrogen atom, a halogen atom, a hydroxy, an alkoxy, an aryloxy, an alkyl, an aryl, an amino, an alkylamino, a cycloalkylamino, an arylamino, an alkylcarbonylamino, an arylcarbonylamino, a mercapto, an alkylthio, an arylthio, an alkylsulfinyl or a nonaromatic heterocyclic; Arepresents a sulfur atom, a sulfinyl or a sulfonyl; and Arepresents an alkylene.

Cyclic compound having pyrimidinylalkylthio group

An indole compound having a carbamoyl group, a ureido group and a substituted oxy group having the following formula (1) or a salt thereof: In the formula (1), Rrepresents a hydrogen atom, an alkyl group, a hydroxy group, or an alkoxy group; Rrepresents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; Rrepresents a halogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group, a heterocyclic group an alkoxy group, an alkenyloxy group, an alkynyloxy group, a cycloalkyloxy group, an aryloxy group or a heterocyclic oxy group; m represents 0, 1, 2, or 3.

Indole derivative having, carbamoyl group, ureido group and substituted oxy group

A method of preventing or treating a glucocorticoid receptor-related disease involving administering a therapeutically effective amount of a 1,2-dihydroquinoline compound or a pharmaceutically acceptable salt thereof.

Method for preventing or treating a glucocorticoid receptor-related disease

A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is benzene or an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; Rand Rare hydrogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or Rand Rjoin together to form a heterocycle; X and Y are hydrogen, halogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.

Compounds having a 4-pyridylalkylthio group as a substituent

Disclosed is a compound represented by the general formula (1) or a salt thereof. The compound or a salt thereof has an inhibitory activity on IKK&#x3b2; and is therefore useful as preventive and/or therapeutic agent for a disease associated with IKK&#x3b2;. In the formula, Rrepresents a hydrogen atom, a lower alkyl group, an aryl group, a hydroxy group, or the like; Rrepresents a halogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, or the like; and m represents 0, 1, 2, or the like. 

Indole derivative having I&#x3ba;B kinase &#x3b2; inhibitory activity

A compound represented by the following formula (1) or a salt thereof: The compound has an inhibitory activity on the production of interleukin-6, and is therefore useful as a therapeutic agent for a disease associated with interleukin-6, ocular inflammatory diseases and the like. In the formula, Rrepresents a halogen atom, a hydrogen atom, a lower alkyl group which may have a substituent, a formyl group, or a lower alkylcarbonyl group which may have a substituent, Rrepresents a bicyclic hydrocarbon group which may have a substituent or a bicyclic heterocyclic group which may have a substituent, Rrepresents a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, or an acyl group.

Pyrrole derivative having, as substituents, ureido group, aminocarbonly group and bicyclic group which may have substituent

An object of the present invention is to study synthesis of a novel 1,2-dihydroquinoline derivative and to find a pharmacological action of the derivative. A compound represented by the general formula (1) or a salt thereof is effective in the treatment of a glucocorticoid receptor-related disease. In the formula, the ring X represents a benzene ring or a pyridine ring; Rrepresents a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, an amino group or the like; p represents an integer of 0 to 5; Rrepresents a halogen atom, an alkyl group, a hydroxy group or the like; q represents an integer of 0 to 2; Rrepresents a hydrogen atom, an alkyl group, an alkenyl group or the like; Rand Rrepresent a hydrogen atom or the like; Rrepresents a hydrogen atom or the like; A represents an alkylene group or the like; and Rrepresents OR, NRR, SR, S(O)Ror S(O)R, wherein Rrepresents an aryl group, a heterocyclic group or the like and Rrepresents a hydrogen atom or the like. 

1-2-dihydroquinoline derivative having glucocorticoid receptor binding activity

Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease. In the formula, the ring A represents a benzene ring or the like; Rrepresents a halogen atom, a hydrogen atom, a lower alkyl group or the like; Rrepresents a halogen atom, a lower alkyl group which may have a substituent, a lower alkenyl group, a lower alkynyl group which may have a substituent, a lower cycloalkyl group, an aryl group, a hydroxy group, a lower alkoxy group which may have a substituent or the like; and n represents 0, 1, 2, 3 or the like. 

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Ikoma, Japan

Kenji Kawashima