WO2008117861A1 - フェニレンジアミン誘導体を有効成分とする眼圧下降剤 - Google Patents

フェニレンジアミン誘導体を有効成分とする眼圧下降剤 Download PDF

Info

Publication number
WO2008117861A1
WO2008117861A1 PCT/JP2008/056010 JP2008056010W WO2008117861A1 WO 2008117861 A1 WO2008117861 A1 WO 2008117861A1 JP 2008056010 W JP2008056010 W JP 2008056010W WO 2008117861 A1 WO2008117861 A1 WO 2008117861A1
Authority
WO
WIPO (PCT)
Prior art keywords
phenylenediamine derivatives
active ingredient
intraocular pressure
pressure lowering
lowering agents
Prior art date
Application number
PCT/JP2008/056010
Other languages
English (en)
French (fr)
Inventor
Hisashi Tajima
Hiroyuki Mogi
Noriko Mishina
Yusuke Yamazaki
Shinji Yoneda
Katsuhiko Watanabe
Junko Fujikawa
Minoru Yamamoto
Original Assignee
Santen Pharmaceutical Co., Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Santen Pharmaceutical Co., Ltd. filed Critical Santen Pharmaceutical Co., Ltd.
Publication of WO2008117861A1 publication Critical patent/WO2008117861A1/ja

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/04—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

　本発明はフェニレンジアミン誘導体の新たな薬理作用を見出す。さらに、新規フェニレンジアミン誘導体を合成して、その薬理作用を見出すことを目的とする。本発明は式（１）で表される化合物又はその塩からなる群より選択される少なくとも１つを有効成分として含有する眼圧下降剤を提供する。式中、環Ａはチオフェン、ピリジン等、Ｒ1及びＲ2は、水素原子、低級アルキル基、低級アルケニル基、低級アルキニル基、低級シクロアルキル基、アリール基 、ヒドロキシ基、低級アルコキシ基等、Ｒ1及びＲ2が一緒になって、置換基を有してもよい含窒素複素環を形成してもよく、Ｒ3はハロゲン原子、低級アルキル基、ヒドロキシ基等、ｍは０、１又は２を示す。 　【化１】
PCT/JP2008/056010 2007-03-28 2008-03-28 フェニレンジアミン誘導体を有効成分とする眼圧下降剤 WO2008117861A1 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2007-084311 2007-03-28
JP2007084311 2007-03-28

Publications (1)

Publication Number Publication Date
WO2008117861A1 true WO2008117861A1 (ja) 2008-10-02

Family

ID=39788592

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/056010 WO2008117861A1 (ja) 2007-03-28 2008-03-28 フェニレンジアミン誘導体を有効成分とする眼圧下降剤

Country Status (2)

Country Link
JP (1) JP2008266321A (ja)
WO (1) WO2008117861A1 (ja)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2332528A1 (de) * 2009-12-14 2011-06-15 Grünenthal GmbH Substituierte aromatische Dicarbonsäureamide als Arzneimittel
CN102477001A (zh) * 2010-11-29 2012-05-30 江苏先声药物研究有限公司 一种苯甲酰胺类组蛋白去乙酰化酶抑制剂
AU2018203354B2 (en) * 2011-12-21 2019-12-05 Novira Therapeutics, Inc. Hepatitis B antiviral agents
EP3997209A4 (en) * 2019-07-08 2023-06-07 Mayo Foundation for Medical Education and Research WNT ACTIVATORS AND METHODS OF USE

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005539001A (ja) * 2002-08-02 2005-12-22 アージェンタ・ディスカバリー・リミテッド ヒストンデアセチラーゼインヒビターとしての置換チエニルヒドロキサム酸
JP2006508120A (ja) * 2002-11-12 2006-03-09 アルコン，インコーポレイテッド 眼の変性疾患を処置するためのヒストンデアセチラーゼインヒビター
JP2006512318A (ja) * 2002-11-12 2006-04-13 アルコン，インコーポレイテッド 眼の血管新生もしくは水腫状の疾患および障害を処置するためのヒストンデアセチラーゼインヒビター
JP2006516553A (ja) * 2003-02-06 2006-07-06 エフ．ホフマン−ラ　ロシュ　アーゲー 新規なモノ−アシル化ｏ−フェニレンジアミン誘導体

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005539001A (ja) * 2002-08-02 2005-12-22 アージェンタ・ディスカバリー・リミテッド ヒストンデアセチラーゼインヒビターとしての置換チエニルヒドロキサム酸
JP2006508120A (ja) * 2002-11-12 2006-03-09 アルコン，インコーポレイテッド 眼の変性疾患を処置するためのヒストンデアセチラーゼインヒビター
JP2006512318A (ja) * 2002-11-12 2006-04-13 アルコン，インコーポレイテッド 眼の血管新生もしくは水腫状の疾患および障害を処置するためのヒストンデアセチラーゼインヒビター
JP2006516553A (ja) * 2003-02-06 2006-07-06 エフ．ホフマン−ラ　ロシュ　アーゲー 新規なモノ−アシル化ｏ−フェニレンジアミン誘導体

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2332528A1 (de) * 2009-12-14 2011-06-15 Grünenthal GmbH Substituierte aromatische Dicarbonsäureamide als Arzneimittel
CN102477001A (zh) * 2010-11-29 2012-05-30 江苏先声药物研究有限公司 一种苯甲酰胺类组蛋白去乙酰化酶抑制剂
CN102477001B (zh) * 2010-11-29 2015-07-15 江苏先声药物研究有限公司 一种苯甲酰胺类组蛋白去乙酰化酶抑制剂
AU2018203354B2 (en) * 2011-12-21 2019-12-05 Novira Therapeutics, Inc. Hepatitis B antiviral agents
EP3997209A4 (en) * 2019-07-08 2023-06-07 Mayo Foundation for Medical Education and Research WNT ACTIVATORS AND METHODS OF USE

Also Published As

Publication number Publication date
JP2008266321A (ja) 2008-11-06

Similar Documents

Publication Publication Date Title
WO2008114817A1 (ja) 新規なアデニン化合物
WO2008114819A1 (ja) 新規アデニン化合物
MY168201A (en) Agricultural And Horticultural Fungicidal Composition
EP1700856A4 (en) thiazole
EP1982982A4 (en) NEW COUMARINE DERIVATIVE WITH ANTITUM EFFECT
ZA200810739B (en) Pesticide containing novel pyridyl-methanamine derivative or its salt
WO2008146871A1 (ja) グルココルチコイド受容体結合活性を有する、スルホン酸エステル又はスルホン酸アミド構造を導入したフェニル基を置換基として有する新規１，２，３，４－テトラヒドロキノキサリン誘導体
WO2008111441A1 (ja) 医薬組成物
TW200732333A (en) An oxime derivative and preparations thereof
NO20092415L (no) Heteromonocyklisk forbindelse og anvendelse derav
HK1133008A1 (en) Imidazole derivative
WO2009107850A3 (en) Fused heterocyclic derivative and use thereof
WO2009016841A1 (ja) オキソピラジン誘導体及び除草剤
WO2008108378A3 (en) Bicyclic oxomorpholine derivative
WO2008108380A3 (en) Pyrrole compounds
WO2008057775A3 (en) Heterocyclic amide compounds useful as kinase inhibitors
WO2008105058A1 (ja) スルホンアミド化合物
WO2008114812A1 (ja) Jak阻害剤
WO2008146914A1 (ja) 複素環化合物
WO2008140099A1 (ja) テトラゾイルオキシム誘導体および植物病害防除剤
WO2008052379A3 (en) Organic compounds
MX2009008772A (es) Derivado piridil-triazolopirimidina o su sal, pesticida que lo contiene y proceso para su produccion.
WO2008153042A1 (ja) 抗腫瘍剤
WO2008117861A1 (ja) フェニレンジアミン誘導体を有効成分とする眼圧下降剤
MY161992A (en) Novel tetrahydroisoquinoline derivative

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 08739134

Country of ref document: EP

Kind code of ref document: A1

NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 08739134

Country of ref document: EP

Kind code of ref document: A1

NENP Non-entry into the national phase

Ref country code: JP