TWI359140B - - Google Patents

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TWI359140B
TWI359140B TW095105236A TW95105236A TWI359140B TW I359140 B TWI359140 B TW I359140B TW 095105236 A TW095105236 A TW 095105236A TW 95105236 A TW95105236 A TW 95105236A TW I359140 B TWI359140 B TW I359140B
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Taiwan
Prior art keywords
oxy
pharmaceutically acceptable
compound
carbonyl
acceptable salt
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TW095105236A
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English (en)
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TW200640864A (en
Inventor
Takahiro Ishii
Takashi Sugane
Jun Maeda
Fumie Narazaki
Akio Kakefuda
Kentaro Sato
Tatsuhisa Takahashi
Takatoshi Kanayama
Chikashi Saitoh
Jotarou Suzuki
Chisato Kanai
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Astellas Pharma Inc
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Publication of TW200640864A publication Critical patent/TW200640864A/zh
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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
    • A61K31/435—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
    • 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
    • A61K31/435—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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • 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
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—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
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • 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
    • C07D401/12—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
    • 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
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Nutrition Science (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Anesthesiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)

Description

更正日期：101.5.22 分別表示：Η或低級烷基； 第95105236號專利申請案申請專利範圍替換本 其中R17及R18係相同或相異，分 或者R17、以可與所結合之Ν原子共同形成5或6員含氮 雜環；且 R20表示-C(=〇)-〇-(低級烷基）或_c〇2h。 5. —種吡啶基非芳香族含氮雜環_丨_綾酸酯化合物或其製 藥學上可接受之鹽，該化合物係以通式(v)表示者；
其中式(V)中之代號係表示下述意義： L2表示低級伸烷基、低級伸烯基或_(低級伸烯 基)-C(=〇)_ ; R21表示Η、鹵基、-CN、-CF3、低級烷基或_〇_低級 烷基；且 R22表示-c(=o)-o-(低級烷基）或-co2h。 6·如申請專利範圍第1項之吼啶基非芳香族含氮雜環-1-羧 酸西旨化合物或其製藥學上可接受之鹽，該化合物係如下 述所述群組中的任一者： 5·{[(4-{4-[(3-敗节基)氧基]苯氧基}旅咬_i-基)羰基]氧基}菸酸、 5'({[4_(2-笨基乙基)°底咬-1-基]羰基}氧基)菸酸、 5·[({4-[4-(2-環己基乙氧基)苯氧基]哌咬小基丨羰基)氧基]菸酸、 5_[(《4·[⑸_2_苯基乙烯基]哌咬-l-基}羰基)氧基]菸酸、 5-{[(4-{3-[1-(6-甲基吡啶-2-基)哌啶_4-基]丙基}哌啶-1-基)羰基] 氧基}菸酸、及 第95105236號專利申請案申請專利範圍替換本 t正日期：101.5.22 5_(甲氧基幾基)π比咬·3-基4-(2-苯基乙基)°瓜°井-1-叛酸自旨。 7. —種藥學組成物，係包含如申請專利範圍第1項之。比啶 基非芳香族含氮雜環-1-羧酸酯化合物或其製藥學上可 接受之鹽以作為有效成分者。 8. 如申請專利範圍第7項之藥學組成物，其係一種FAAH 阻礙劑。 9. 如申請專利範圍第7項之藥學組成物，其係一種頻尿、 尿失禁及/或膀胱過動症之治療藥。 10. 如申請專利範圍第7項之藥學組成物，其係一種疼痛之 治療藥。 11. 一種如申請專利範圍第1項中任一項之化合物或其製藥 學上可接受之鹽的用途，係將如申請專利範圍第1至9 項中任一項之化合物或其製藥學上可接受之鹽用於製 造FAAH阻礙劑、頻尿、尿失禁及/或膀胱過動症之治療 藥者。 12. —種如申請專利範圍第1項中任一項之化合物或其製藥 學上可接受之鹽的用途，係將如申請專利範圍第1至9 項中任一項之化合物或其製藥學上可接受之鹽用於製 造FAAH阻礙劑以及疼痛之治療藥者。
TW095105236A 2005-02-17 2006-02-16 Pyridyl non-aromatic nitrogenated heterocyclic-1-carboxylate ester derivative TW200640864A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2005040197 2005-02-17
JP2005303065 2005-10-18

Publications (2)

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TW200640864A TW200640864A (en) 2006-12-01
TWI359140B true TWI359140B (zh) 2012-03-01

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Application Number Title Priority Date Filing Date
TW095105236A TW200640864A (en) 2005-02-17 2006-02-16 Pyridyl non-aromatic nitrogenated heterocyclic-1-carboxylate ester derivative
TW098121395A TWI385164B (zh) 2005-02-17 2006-02-16 Pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivatives (II)
TW098121399A TWI385152B (zh) 2005-02-17 2006-02-16 Pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivatives (I)

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TW098121395A TWI385164B (zh) 2005-02-17 2006-02-16 Pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivatives (II)
TW098121399A TWI385152B (zh) 2005-02-17 2006-02-16 Pyridyl non-aromatic nitrogen-containing heterocyclic-1-carboxylate derivatives (I)

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US (3) US7919495B2 (zh)
EP (2) EP2607362B1 (zh)
JP (1) JP4702361B2 (zh)
KR (3) KR101065979B1 (zh)
CN (1) CN101160287B (zh)
AU (3) AU2006215080B2 (zh)
BR (1) BRPI0608205B8 (zh)
CA (1) CA2598294C (zh)
CY (2) CY1114709T1 (zh)
DK (2) DK2607362T3 (zh)
ES (2) ES2528674T3 (zh)
IL (1) IL184998A (zh)
MX (1) MX2007010076A (zh)
NO (1) NO20074697L (zh)
PL (2) PL1849773T3 (zh)
PT (2) PT2607362E (zh)
RU (3) RU2408580C2 (zh)
SI (2) SI2607362T1 (zh)
TW (3) TW200640864A (zh)
WO (1) WO2006088075A1 (zh)

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JP2009527479A (ja) * 2006-02-17 2009-07-30 アバロン ファーマシューティカルズ，インコーポレイテッド ヒドロキシピペリジン誘導体とその使用
WO2008023720A1 (fr) 2006-08-23 2008-02-28 Astellas Pharma Inc. COMPOSÉ D'URÉE OU SEL DUDIT COMPOSé
KR101181194B1 (ko) 2006-10-18 2012-09-18 화이자 프로덕츠 인코포레이티드 바이아릴 에터 우레아 화합물
JP5603770B2 (ja) 2007-05-31 2014-10-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃｃｒ２受容体拮抗薬およびその使用
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