JP2000505814A - Nos阻害剤として有用な6−フェニルピリジル−2−アミン誘導体 - Google Patents
Nos阻害剤として有用な6−フェニルピリジル−2−アミン誘導体Info
- Publication number
- JP2000505814A JP2000505814A JP10525397A JP52539798A JP2000505814A JP 2000505814 A JP2000505814 A JP 2000505814A JP 10525397 A JP10525397 A JP 10525397A JP 52539798 A JP52539798 A JP 52539798A JP 2000505814 A JP2000505814 A JP 2000505814A
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- JP
- Japan
- Prior art keywords
- disease
- phenyl
- compound
- alkyl
- ylamine
- Prior art date
- Legal status (The legal status 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 status listed.)
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- 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
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
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- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- 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
- C07D401/10—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 aromatic rings
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- 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
- C07D401/14—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 three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Ophthalmology & Optometry (AREA)
- Psychiatry (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Psychology (AREA)
- Physical Education & Sports Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Addiction (AREA)
- Cardiology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1. 下記式の化合物及びそのような化合物の薬学的に許容し得る塩。 (ここで、nはゼロ又は1であり、xはN又はCHであり、qはゼロ、1又は2で あり、かつR3及びR4は水素、ヒドロキシ、メチル及びメトキシから独立に選択 され;及びGは下記式の基であり、 ここでnはゼロ又は1であり; YはNR3R4、(C1−C6)アルキル又はアラルキルであって、該アラルキルの アリール部分はフェニルもしくはナフチルであり、かつアルキル部分は直鎖もし くは分岐鎖であって1ないし6個の炭素原子を含み、並びに該(C1−C6)アルキ ル及び該アラルキルのアリール部分はハロ(例えば、クロロ、フルオロ、ブロモ もしくはヨード)、ニトロ、ヒドロキシ、シアノ、アミノ、(C1−C4)アルコキ シ及び(C1−C4)アルキルアミノから独立に選択される1つないし3つ(thours -ee)の置換基、好ましくはゼロないし2つの置換基で置換されていてもよく; Xは、Yが(C1−C6)アルキル、アラルキル、又は置換(C1−C6)アルキ ルである場合にはN、YがNR3R4である場合にはCHであり; qはゼロ、1又は2であり; mはゼロ、1又は2であり:並びに R3及びR4は(C1−C6)アルキル、テトラヒドロナフタレン及びアラルキル から独立に選択され、ここで、該アラルキルのアリール部分はフェニルもしくは ナフチルであり、かつアルキル部分は直鎖もしくは分岐鎖であって1ないし6個の 炭素原子を含み、並びに該(C1−C6)アルキル及び該テトラヒドロナフタレン 及び該アラルキルのアリール部分はハロ(例えば、クロロ、フルオロ、ブロモも しくはヨード)、ニトロ、ヒドロキシ、シアノ、アミノ、(C1−C4)アルコキシ 及び(C1−C4)アルキルアミノから独立に選択される1つないし3つ(thoursee)の 置換基、好ましくはゼロないし2つの置換基で置換されていてもよく; 又は、R3及びR4はそれらが結合する窒素と共にピペラジン、ピペリジンもし くはピロリジン環又は6ないし14個の環構成要素を有するアザニ環式環を形成し 、該環構成要素のうちの1ないし3個は窒素であって残りは炭素である。) 2. qがゼロ又は1である請求項1に記載の化合物。 3. NR3R4がピペリジン、ピペラジンもしくはピロリジン環又は3−アザ− ビシクロ[3.1.0]ヘキス−6−イルアミン環であり、 及び該ピペラジン、ピペリジン及びピロリジン環はアミノ、(C1−C6)アルキ ルアミノ、[ジ−(C1−C6)アルキル]アミノ、1ないし4個の環窒素原子を有 するフェニル置換5ないし6員複素環、ベンゾイル、ベンゾイルメチル、、ベンジ ルカルボニル、フェニルアミノカルボニル、フェニルエチル及びフェノキシカル ボニルから独立に選択される1つ以上の置換基、好ましくはゼロないし2つの置換 基で置換されていてもよく、かつ前記置換基のいずれのフェニル部分もハロ、( C1−C3)アルキル、(C1−C3)アルコキシ、ニトロ、アミノ、シアノ、CF3及 びOCF3から独立に選択される1つ以上の置換基、好ましくはゼロないし2つの 置換基で置換されていてもよい、請求項1に記載の化合物。 4. NR3R4が4−フェニルエチルピペラジン−1−イル、4−メチルピペラジ ン−1−イル、フェネチルアミノ、又は3−アザ−ビシクロ[3.1.0]ヘキス−6− イルアミンである、請求項1に記載の化合物。 5. NR3R4が下記式の基である請求項1に記載の化合物。(ここで、NR5R6はNH2である。) 6. 哺乳動物における、片頭痛炎症性疾患、発作、急性及び慢性(choursonic )の痛み、血液量減少性のショック、外傷性ショック、再潅流傷害、クローン病 、潰瘍性大腸炎、敗血症性ショック、多発性硬化症、AIDS関連痴呆、神経変 性疾患、ニューロン毒性、アルツハイマー病、薬物依存及び中毒、嘔吐、癲癇、 不安、精神病、頭部外傷、成人呼吸促進症候群(ARDS)、モルヒネ誘発寛容及 び禁断症状、炎症性腸疾患、骨関節炎、関節リウマチ、排卵、拡張型心筋症、急 性脊髄損傷、ハンチントン病、パーキンソン病、緑内障、黄斑変性症、糖尿病性 神経障害、糖尿病性腎障害及び癌からなる群より選択される状態を治療又は予防 するための医薬組成物であって、そのような状態の治療又は予防に有効である量 の請求項1に記載の化合物及び薬学的に許容し得る担体を含む医薬組成物。 7. 哺乳動物における、片頭痛炎症性疾患、発作、急性及び慢性(choursonic )の痛み、血液量減少性のショック、外傷性ショック、再潅流傷害、クローン病 、潰瘍性大腸炎、敗血症性ショック、多発性硬化症、AIDS関連痴呆、神経変 性疾患、ニューロン毒性、アルツハイマー病、薬物依存及び中毒、嘔吐、癲癇、 不安、精神病、頭部外傷、成人呼吸促進症候群(ARDS)、モルヒネ誘発寛容及 び禁断症状、炎症性腸疾患、骨関節炎、関節リウマチ、排卵、拡張型心筋症、急 性脊髄損傷、ハンチントン病、パーキンソン病、緑内障、黄斑変性症、糖尿病性 神経障害、糖尿病性腎障害及び癌からなる群より選択される状態の治療又は予防 方法であって、該哺乳動物にそのような状態の治療又は予防に有効である量の請 求項1に記載の化合物を投与することを包含する方法。 8. 請求項1による、哺乳動物において酸化窒素合成酵素(NOS)を阻害す るための医薬組成物であって、NOS阻害有効量の請求項1に記載の化合物及び 薬学的に許容し得る担体を含む医薬組成物。 9. 哺乳動物においてNOSを阻害する方法であって、該哺乳動物にNOS阻 害有効量の請求項1に記載の化合物を投与することを包含する方法。 10. 哺乳動物における、片頭痛、炎症性疾患、発作、急性及び慢性(chours onic)の痛み、血液量減少性のショック、外傷性ショック、再潅流傷害、クロー ン病、潰瘍性大腸炎、敗血症性ショック、多発性硬化症、AIDS関連痴呆、神 経変性疾患、ニューロン毒性、アルツハイマー病、薬物依存及び中毒、嘔吐、癲 癇、不安、精神病、頭部外傷、成人呼吸促進症候群(ARDS)、モルヒネ誘発寛 容及び禁断症状、炎症性腸疾患、骨関節炎、関節リウマチ、排卵、拡張型心筋症 、急性脊髄損傷、ハンチントン病、パーキンソン病、緑内障、黄斑変性症、糖尿 病性神経障害、糖尿病性腎障害及び癌からなる群より選択される状態を治療又は 予防するための医薬組成物であって、NOS阻害有効量の請求項1に記載の化合 物及び薬学的に許容し得る担体を含む医薬組成物。 11. 哺乳動物における、片頭痛、炎症性疾患、発作、急性及び慢性(chours onic)の痛み、血液量減少性のショック、外傷性ショック、再潅流傷害、クロー ン病、潰瘍性大腸炎、敗血症性ショック、多発性硬化症、AIDS関連痴呆、神 経変性疾患、ニューロン毒性、アルツハイマー病、薬物依存及び中毒、嘔吐、癲 癇、不安、精神病、頭部外傷、成人呼吸促進症候群(ARDS)、モルヒネ誘発寛 容及び禁断症状、炎症性腸疾患、骨関節炎、肌節リウマチ、排卵、拡張型心筋症 、急性脊髄損傷、ハンチントン病、パーキンソン病、緑内障、黄斑変性症、糖尿 病性神経障害、糖尿病性腎障害及び癌からなる群より選択される状態を治療又は 予防する方法であって、該哺乳動物にNOS阻害有効量の請求項1に記載の化合 物を投与することを包含する方法。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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US3279396P | 1996-12-06 | 1996-12-06 | |
US60/032,793 | 1996-12-06 | ||
PCT/IB1997/001446 WO1998024766A1 (en) | 1996-12-06 | 1997-11-17 | 6-phenylpyridyl-2-amine derivatives useful as nos inhibitors |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
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JP2004186311A Division JP2005170924A (ja) | 1996-12-06 | 2004-06-24 | Nos阻害剤として有用な6−フェニルピリジル−2−アミン誘導体 |
Publications (2)
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JP2000505814A true JP2000505814A (ja) | 2000-05-16 |
JP3604399B2 JP3604399B2 (ja) | 2004-12-22 |
Family
ID=21866837
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
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JP52539798A Expired - Fee Related JP3604399B2 (ja) | 1996-12-06 | 1997-11-17 | Nos阻害剤として有用な6−フェニルピリジル−2−アミン誘導体 |
JP2004186311A Pending JP2005170924A (ja) | 1996-12-06 | 2004-06-24 | Nos阻害剤として有用な6−フェニルピリジル−2−アミン誘導体 |
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Application Number | Title | Priority Date | Filing Date |
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JP2004186311A Pending JP2005170924A (ja) | 1996-12-06 | 2004-06-24 | Nos阻害剤として有用な6−フェニルピリジル−2−アミン誘導体 |
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EP (1) | EP0946512B1 (ja) |
JP (2) | JP3604399B2 (ja) |
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1997
- 1997-02-18 HN HN1997000027A patent/HN1997000027A/es unknown
- 1997-11-17 PT PT97910587T patent/PT946512E/pt unknown
- 1997-11-17 AU AU47917/97A patent/AU4791797A/en not_active Abandoned
- 1997-11-17 EP EP97910587A patent/EP0946512B1/en not_active Expired - Lifetime
- 1997-11-17 CZ CZ19992017A patent/CZ293863B6/cs not_active IP Right Cessation
- 1997-11-17 PL PL97333918A patent/PL333918A1/xx unknown
- 1997-11-17 ES ES97910587T patent/ES2206691T3/es not_active Expired - Lifetime
- 1997-11-17 EA EA199900448A patent/EA002907B1/ru not_active IP Right Cessation
- 1997-11-17 JP JP52539798A patent/JP3604399B2/ja not_active Expired - Fee Related
- 1997-11-17 CN CN97180350A patent/CN1117077C/zh not_active Expired - Fee Related
- 1997-11-17 AT AT97910587T patent/ATE251612T1/de not_active IP Right Cessation
- 1997-11-17 DE DE69725465T patent/DE69725465T2/de not_active Expired - Fee Related
- 1997-11-17 IL IL13011197A patent/IL130111A0/xx unknown
- 1997-11-17 NZ NZ335733A patent/NZ335733A/xx unknown
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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JP2010500977A (ja) * | 2006-08-09 | 2010-01-14 | スミスクライン ビーチャム コーポレーション | オピオイド受容体のアンタゴニストまたはインバースアゴニストである新規化合物 |
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