JP4359150B2 - フルオロオキシインドールのホスフェートプロドラッグ - Google Patents

フルオロオキシインドールのホスフェートプロドラッグ Download PDF

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Publication number
JP4359150B2
JP4359150B2 JP2003577875A JP2003577875A JP4359150B2 JP 4359150 B2 JP4359150 B2 JP 4359150B2 JP 2003577875 A JP2003577875 A JP 2003577875A JP 2003577875 A JP2003577875 A JP 2003577875A JP 4359150 B2 JP4359150 B2 JP 4359150B2
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JP
Japan
Prior art keywords
oxo
chloro
dihydro
fluoro
trifluoromethyl
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Expired - Fee Related
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JP2003577875A
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English (en)
Japanese (ja)
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JP2005526097A (ja
JP2005526097A5 (OSRAM
Inventor
ケビン・ダブリュー・ギルマン
ピヤセナ・ヘワワサム
ウィリアム・ディ・シュミッツ
オマー・ディ・ロペス
ジョン・イー・スターレット
デイビッド・ピー・プローベンカル
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572Five-membered rings
    • C07F9/5728Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/54Quaternary phosphonium compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/02Antidotes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Toxicology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2003577875A 2002-03-20 2003-03-20 フルオロオキシインドールのホスフェートプロドラッグ Expired - Fee Related JP4359150B2 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36601002P 2002-03-20 2002-03-20
PCT/US2003/008613 WO2003080047A1 (en) 2002-03-20 2003-03-20 Phosphate prodrugs of fluorooxindoles

Publications (3)

Publication Number Publication Date
JP2005526097A JP2005526097A (ja) 2005-09-02
JP2005526097A5 JP2005526097A5 (OSRAM) 2006-04-27
JP4359150B2 true JP4359150B2 (ja) 2009-11-04

Family

ID=28454740

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2003577875A Expired - Fee Related JP4359150B2 (ja) 2002-03-20 2003-03-20 フルオロオキシインドールのホスフェートプロドラッグ

Country Status (21)

Country Link
US (1) US6930100B2 (OSRAM)
EP (1) EP1485085A4 (OSRAM)
JP (1) JP4359150B2 (OSRAM)
KR (1) KR100951499B1 (OSRAM)
CN (1) CN100384820C (OSRAM)
BR (1) BR0308737A (OSRAM)
CA (1) CA2479256A1 (OSRAM)
CO (1) CO5611143A2 (OSRAM)
GE (1) GEP20074230B (OSRAM)
HR (1) HRP20040853A2 (OSRAM)
IL (2) IL164022A0 (OSRAM)
IS (1) IS7456A (OSRAM)
MX (1) MXPA04008999A (OSRAM)
NO (1) NO20044442L (OSRAM)
NZ (1) NZ535365A (OSRAM)
PL (1) PL372413A1 (OSRAM)
RS (1) RS81904A (OSRAM)
RU (1) RU2312857C2 (OSRAM)
UA (1) UA77296C2 (OSRAM)
WO (1) WO2003080047A1 (OSRAM)
ZA (1) ZA200407337B (OSRAM)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
IL166241A0 (en) 2002-07-29 2006-01-15 Rigel Pharmaceuticals Inc Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds
US6916937B2 (en) * 2003-02-03 2005-07-12 Bristol-Myers Squibb Company Carbohydrate prodrugs of fluorooxindoles
RS53109B (sr) 2003-07-30 2014-06-30 Rigel Pharmaceuticals Inc. Jedinjenja 2,4 pirimidindiamina za upotrebu u tretmanu ili prevenciji autoimunih bolesti
US7169803B2 (en) * 2004-03-15 2007-01-30 Bristol-Myers Squibb Company N-substituted prodrugs of fluorooxindoles
US7253167B2 (en) 2004-06-30 2007-08-07 Bristol-Myers Squibb Company Tricyclic-heteroaryl compounds useful as kinase inhibitors
NZ555947A (en) 2005-01-19 2010-11-26 Rigel Pharmaceuticals Inc Prodrugs of 2,4-pyrimidinediamine compounds and their uses
US8227455B2 (en) * 2005-04-18 2012-07-24 Rigel Pharmaceuticals, Inc. Methods of treating cell proliferative disorders
US20090114877A1 (en) * 2005-09-13 2009-05-07 Eisai R&D Management Co., Ltd. Composition Containing Stability-Improved Chloromethyl Phosphate Derivatve and Process for Producing Same
TWI385169B (zh) 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd 經雜環取代之吡啶衍生物及含有彼之抗真菌劑
TW200841879A (en) * 2007-04-27 2008-11-01 Eisai R&D Man Co Ltd Pyridine derivatives substituted by heterocyclic ring and phosphonoamino group, and anti-fungal agent containing same
US8513287B2 (en) * 2007-12-27 2013-08-20 Eisai R&D Management Co., Ltd. Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same
EP2249833B1 (en) * 2008-02-05 2012-10-17 Merck Sharp & Dohme Corp. Prodrugs of cgrp receptor antagonist
US8188119B2 (en) * 2008-10-24 2012-05-29 Eisai R&D Management Co., Ltd Pyridine derivatives substituted with heterocyclic ring and γ-glutamylamino group, and antifungal agents containing same
HUE033442T2 (en) * 2009-06-25 2017-11-28 Alkermes Pharma Ireland Ltd Heterocyclic compounds for the treatment of neurological and psychological disorders
EP2445343B1 (en) * 2009-06-25 2021-08-04 Alkermes Pharma Ireland Limited Prodrugs of nh-acidic compounds
JP5848761B2 (ja) * 2010-06-24 2016-01-27 アルカーメス ファーマ アイルランド リミテッド Nh酸性化合物のプロドラッグ:エステル、カルボネート、カルバメートおよびホスホネートの誘導体
IL293770B2 (en) 2015-07-06 2023-07-01 Gilead Sciences Inc Modulators of cot and methods of using them
KR20200121800A (ko) 2018-01-05 2020-10-26 싸이브렉사 1, 인크. 산성 또는 저산소성 질환에 걸린 조직에 관련된 질환의 치료를 위한 화합물, 조성물 및 방법
CA3093234A1 (en) * 2018-03-05 2019-09-12 Teon Therapeutics, Inc. Adenosine receptor antagonists and uses thereof
CA3092335A1 (en) 2018-03-05 2019-09-12 Alkermes Pharma Ireland Limited Aripiprazole dosing strategy
TWI770527B (zh) 2019-06-14 2022-07-11 美商基利科學股份有限公司 Cot 調節劑及其使用方法
US11555019B2 (en) 2019-07-10 2023-01-17 Cybrexa 3, Inc. Peptide conjugates of microtubule-targeting agents as therapeutics
CN114341162B (zh) 2019-07-10 2025-10-17 赛博克萨2公司 作为治疗剂的细胞毒素的肽缀合物
JP2023520650A (ja) 2020-03-30 2023-05-18 ギリアード サイエンシーズ, インコーポレイテッド (S)-6-(((1-(ビシクロ[1.1.1]ペンタン-1-イル)-1H-1,2,3-トリアゾール-4-イル)2-メチル-1-オキソ-1,2-ジヒドロイソキノリン-5-イル)メチル)))アミノ)8-クロロ-(ネオペンチルアミノ)キノリン-3-カルボニトリルCot阻害剤化合物の固体形態
CN119390681A (zh) 2020-04-02 2025-02-07 吉利德科学公司 用于制备cot抑制剂化合物的方法
EP3912625A1 (en) 2020-05-20 2021-11-24 Kaerus Bioscience Limited Novel maxi-k potassium channel openers for the treatment of fragile x associated disorders
WO2025233532A1 (en) 2024-05-10 2025-11-13 Les Laboratoires Servier Maxi-k potassium channel openers and therapeutic applications thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU749063A1 (ru) * 1979-01-29 1996-09-10 Военно-медицинская академия им.С.М.Кирова 3-(4-карбэтокси)-фенилимино-2-оксоиндолин, повышающий устойчивость организма к повторной черепно-мозговой травме
US5234947A (en) 1991-11-07 1993-08-10 New York University Potassium channel activating compounds and methods of use thereof
US5187173A (en) 1991-12-27 1993-02-16 Sterling Winthrop Inc. 2-saccharinylmethyl and 4,5,6,7-tetrahydro-2-saccharinylmethyl phosphates, phosphonates and phosphinates useful as proteolytic enzyme inhibitors and compositions and method of use thereof
US5565483A (en) * 1995-06-07 1996-10-15 Bristol-Myers Squibb Company 3-substituted oxindole derivatives as potassium channel modulators
DE69822514T2 (de) 1997-12-31 2005-03-24 The University Of Kansas, Lawrence Wasserlösliche pro-pharmaka von arzneistoffen, die ein tertiäres amin enthalten, und verfahren zu ihrer herstellung
CA2318817A1 (en) * 1998-01-29 1999-08-05 Bristol-Myers Squibb Company Phosphate derivatives of diaryl 1,3,4-oxadiazolone

Also Published As

Publication number Publication date
RU2004131201A (ru) 2005-05-10
US6930100B2 (en) 2005-08-16
JP2005526097A (ja) 2005-09-02
US20030195169A1 (en) 2003-10-16
KR100951499B1 (ko) 2010-04-07
IL164022A (en) 2008-04-13
CA2479256A1 (en) 2003-10-02
UA77296C2 (en) 2006-11-15
IS7456A (is) 2004-09-17
ZA200407337B (en) 2006-02-22
EP1485085A1 (en) 2004-12-15
PL372413A1 (en) 2005-07-25
RU2312857C2 (ru) 2007-12-20
IL164022A0 (en) 2005-12-18
HRP20040853A2 (en) 2004-12-31
CN1652769A (zh) 2005-08-10
AU2003215017A1 (en) 2003-10-08
CN100384820C (zh) 2008-04-30
NO20044442L (no) 2004-10-19
RS81904A (sr) 2007-02-05
EP1485085A4 (en) 2007-03-14
KR20040106293A (ko) 2004-12-17
GEP20074230B (en) 2007-11-12
MXPA04008999A (es) 2004-12-07
NZ535365A (en) 2006-07-28
BR0308737A (pt) 2005-01-11
WO2003080047A1 (en) 2003-10-02
CO5611143A2 (es) 2006-02-28

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