WO2008126899A1 - ５員環へテロ環誘導体及びその医薬用途 - Google Patents

５員環へテロ環誘導体及びその医薬用途 Download PDF

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Publication number
WO2008126899A1
WO2008126899A1 PCT/JP2008/057093 JP2008057093W WO2008126899A1 WO 2008126899 A1 WO2008126899 A1 WO 2008126899A1 JP 2008057093 W JP2008057093 W JP 2008057093W WO 2008126899 A1 WO2008126899 A1 WO 2008126899A1
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WIPO (PCT)
Prior art keywords
independently represent
membered heterocyclic
heterocyclic derivative
haloalkyl
prophylactic
Prior art date
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PCT/JP2008/057093
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English (en)
French (fr)
Inventor
Kazuo Shimizu
Yasushi Takigawa
Hideki Fujikura
Masato Iizuka
Masahiro Hiratochi
Norihiko Kikuchi
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Kissei 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.)
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Publication date
Priority to CA2682393A priority Critical patent/CA2682393C/en
Priority to BRPI0810523-5A2A priority patent/BRPI0810523A2/pt
Priority to EP08740194A priority patent/EP2133331A4/en
Priority to MX2009010491A priority patent/MX2009010491A/es
Priority to RU2009141613/04A priority patent/RU2515968C2/ru
Priority to CN200880018819.3A priority patent/CN101679244B/zh
Application filed by Kissei Pharmaceutical Co., Ltd. filed Critical Kissei Pharmaceutical Co., Ltd.
Priority to US12/595,437 priority patent/US8227500B2/en
Priority to AU2008239018A priority patent/AU2008239018B2/en
Priority to KR1020097021439A priority patent/KR101502959B1/ko
Priority to JP2009509372A priority patent/JP5378988B2/ja
Publication of WO2008126899A1 publication Critical patent/WO2008126899A1/ja
Priority to US13/494,380 priority patent/US9023882B2/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/402—1-aryl substituted, e.g. piretanide
    • A—HUMAN NECESSITIES
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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    • 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
    • C07D207/30—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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—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 two double bonds between ring members or between ring members and non-ring members 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
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    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
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  • Plural Heterocyclic Compounds (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

本発明は、血漿尿酸値異常に起因する疾患等の予防又は治療薬として有用な化合物を提供する。すなわち、本発明は、キサンチンオキシダーゼ阻害活性を有し、血漿尿酸値異常に起因する疾患の予防又は治療薬として有用な、下記一般式（Ｉ）で表される５員環へテロ環誘導体、そのプロドラッグ、その塩等に関する。式（Ｉ）中、Ｔはニトロ、シアノ等；環Ｊはアリール又はヘテロアリール；Ｑはカルボキシ、５－テトラゾリル等；ＹはＨ、ＯＨ、ＮＨ２、ハロゲン、ハロアルキル等；Ｘ１、Ｘ２は独立してＣＲ２又はＮ；Ｒ２はＨ、アルキル等；Ｒ１はハロゲン、シアノ、ハロアルキル、Ａ－Ｄ－Ｅ－Ｇ－Ｌ－Ｍ、－Ｎ（－Ｄ－Ｌ－Ｍ）２等（式中、Ａは単結合、Ｏ、Ｓ等；Ｄ、Ｇ及びＭは独立して置換可アルキレン、シクロアルキレン、ヘテロシクロアルキレン、アリーレン、ヘテロアリーレン等；Ｅ及びＬは独立して単結合、Ｏ、Ｓ、ＣＯＯ、ＳＯ２等；である。
PCT/JP2008/057093 2007-04-11 2008-04-10 ５員環へテロ環誘導体及びその医薬用途 WO2008126899A1 (ja)

Priority Applications (11)

Application Number Priority Date Filing Date Title
BRPI0810523-5A2A BRPI0810523A2 (pt) 2007-04-11 2008-04-10 Derivado heterocíclico de 5 membros e uso do mesmo para propósitos médicos.
EP08740194A EP2133331A4 (en) 2007-04-11 2008-04-10 FIVE-GLASS HETEROCYCLIC DERIVATIVE AND ITS USE IN MEDICAL PURPOSES
MX2009010491A MX2009010491A (es) 2007-04-11 2008-04-10 Derivado heterociclico de 5 miembros y su uso para propositos medicos.
RU2009141613/04A RU2515968C2 (ru) 2007-04-11 2008-04-10 5-членное гетероциклическое соединение и его применение для лекарственных целей
CN200880018819.3A CN101679244B (zh) 2007-04-11 2008-04-10 5元杂环衍生物及其医药用途
CA2682393A CA2682393C (en) 2007-04-11 2008-04-10 5-membered heterocyclic derivative and use thereof for medical purposes
US12/595,437 US8227500B2 (en) 2007-04-11 2008-04-10 5-membered nitrogen containing heterocyclic derivatives and pharmaceutical compositions comprising the same
AU2008239018A AU2008239018B2 (en) 2007-04-11 2008-04-10 5-membered heterocyclic derivative and use thereof for medical purposes
KR1020097021439A KR101502959B1 (ko) 2007-04-11 2008-04-10 5원환 헤테로환 유도체 및 그 의약 용도
JP2009509372A JP5378988B2 (ja) 2007-04-11 2008-04-10 ５員環へテロ環誘導体及びその医薬用途
US13/494,380 US9023882B2 (en) 2007-04-11 2012-06-12 5-membered nitrogen containing heterocyclic derivatives and pharmaceutical compositions comprising the same

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US20100227864A1 (en) 2010-09-09
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EP2133331A4 (en) 2011-06-22
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