WO2008117861A1 - Intraocular pressure lowering agents containing phenylenediamine derivatives as the active ingredient - Google Patents

Intraocular pressure lowering agents containing phenylenediamine derivatives as the active ingredient Download PDF

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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
French (fr)
Japanese (ja)
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/en

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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

Abstract

The invention aims at finding new pharmacological effects of phenylenediamine derivatives and at synthesizing novel phenylenediamine derivatives and finding pharmacological effects of the derivatives. The invention provides intraocular pressure lowering agents which each contain as the active ingredient at least one member selected from the group consisting of compounds represented by the general formula (1) and salts thereof: [Chemical formula 1] (1) wherein A is thiophene, pyridine, or the like; R1 and R2 are each hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, hydroxy, lower alkoxy, or the like, or R1 and R2 may be united to form a nitrogenous heterocycle which may be substituted; R3 is halogeno, lower alkyl, hydroxy, or the like; and m is 0, 1 or 2.
PCT/JP2008/056010 2007-03-28 2008-03-28 Intraocular pressure lowering agents containing phenylenediamine derivatives as the active ingredient WO2008117861A1 (en)

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 (en) 2008-10-02

Family

ID=39788592

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2008/056010 WO2008117861A1 (en) 2007-03-28 2008-03-28 Intraocular pressure lowering agents containing phenylenediamine derivatives as the active ingredient

Country Status (2)

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

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2332528A1 (en) * 2009-12-14 2011-06-15 Grünenthal GmbH Substituted aromatic dicarbonic acid amides as medicaments
CN102477001A (en) * 2010-11-29 2012-05-30 江苏先声药物研究有限公司 Benzamide histone deacetylase inhibitor
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 (en) * 2002-08-02 2005-12-22 アージェンタ・ディスカバリー・リミテッド Substituted thienyl hydroxamic acids as histone deacetylase inhibitors
JP2006508120A (en) * 2002-11-12 2006-03-09 アルコン，インコーポレイテッド Histone deacetylase inhibitors for treating degenerative diseases of the eye
JP2006512318A (en) * 2002-11-12 2006-04-13 アルコン，インコーポレイテッド Histone deacetylase inhibitors for treating ocular neovascularization or edema-like diseases and disorders
JP2006516553A (en) * 2003-02-06 2006-07-06 エフ．ホフマン−ラ　ロシュ　アーゲー Novel mono-acylated o-phenylenediamine derivatives

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005539001A (en) * 2002-08-02 2005-12-22 アージェンタ・ディスカバリー・リミテッド Substituted thienyl hydroxamic acids as histone deacetylase inhibitors
JP2006508120A (en) * 2002-11-12 2006-03-09 アルコン，インコーポレイテッド Histone deacetylase inhibitors for treating degenerative diseases of the eye
JP2006512318A (en) * 2002-11-12 2006-04-13 アルコン，インコーポレイテッド Histone deacetylase inhibitors for treating ocular neovascularization or edema-like diseases and disorders
JP2006516553A (en) * 2003-02-06 2006-07-06 エフ．ホフマン−ラ　ロシュ　アーゲー Novel mono-acylated o-phenylenediamine derivatives

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2332528A1 (en) * 2009-12-14 2011-06-15 Grünenthal GmbH Substituted aromatic dicarbonic acid amides as medicaments
CN102477001A (en) * 2010-11-29 2012-05-30 江苏先声药物研究有限公司 Benzamide histone deacetylase inhibitor
CN102477001B (en) * 2010-11-29 2015-07-15 江苏先声药物研究有限公司 Benzamide histone deacetylase inhibitor
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 (en) 2008-11-06

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