Santen Pharmaceutical Co., Ltd.

Ayumi Pharmaceutical Corporation

Minoru Yamamoto

Kenji Kawashima

Hisashi Tajima

Kazuyoshi Okamoto

Takahiro Honda

Yusuke Yamazaki

Toshiyuki Mori

Masatomo Kato

Mamoru Matsuda

Miwa Takai

Masato Nagatsuka

Sachiko Kobayashi

Hiroshi Enomoto

Masaaki Murai

Shinji Yoneda

Hiroyuki Mogi

Noriko Mishina

Katsuhiko Watanabe

Junko Fujikawa

Masakazu Ban

Takaaki Inaba

Yoshimasa Sasabuchi

Tomoko Oda

Kazuhiro Kudou

Noriko Ishizaka

Hiroyuki Aono

Noriko Kawashima

Yuriko Takeno

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

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 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 [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

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.

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

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

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 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. 

Growing community of inventors

Ikoma, Japan

Minoru Yamamoto