CN100384820C - 氟羟吲哚的磷酸酯前体药物 - Google Patents

氟羟吲哚的磷酸酯前体药物 Download PDF

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Publication number
CN100384820C
CN100384820C CNB038109778A CN03810977A CN100384820C CN 100384820 C CN100384820 C CN 100384820C CN B038109778 A CNB038109778 A CN B038109778A CN 03810977 A CN03810977 A CN 03810977A CN 100384820 C CN100384820 C CN 100384820C
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CN
China
Prior art keywords
fluoro
phenyl
chloro
dihydro
trifluoromethyl
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Expired - Fee Related
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CNB038109778A
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English (en)
Chinese (zh)
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CN1652769A (zh
Inventor
K·W·吉尔曼
P·赫瓦瓦萨姆
W·D·施密茨
O·D·罗佩兹
J·E·斯塔雷特
D·P·普罗文卡尔
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings
    • C07F9/5728—Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/54—Quaternary phosphonium compounds
    • 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
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (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)
CNB038109778A 2002-03-20 2003-03-20 氟羟吲哚的磷酸酯前体药物 Expired - Fee Related CN100384820C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36601002P 2002-03-20 2002-03-20
US60/366,010 2002-03-20

Publications (2)

Publication Number Publication Date
CN1652769A CN1652769A (zh) 2005-08-10
CN100384820C true CN100384820C (zh) 2008-04-30

Family

ID=28454740

Family Applications (1)

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CNB038109778A Expired - Fee Related CN100384820C (zh) 2002-03-20 2003-03-20 氟羟吲哚的磷酸酯前体药物

Country Status (21)

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

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TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
ES2445208T3 (es) 2002-07-29 2014-02-28 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para uso en métodos para tratar o prevenir enfermedades autoinmunitarias
US6916937B2 (en) * 2003-02-03 2005-07-12 Bristol-Myers Squibb Company Carbohydrate prodrugs of fluorooxindoles
BRPI0413018B8 (pt) 2003-07-30 2021-05-25 Rigel Pharmaceuticals Inc composto, e, uso de um composto
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
DE602006010979D1 (de) 2005-01-19 2010-01-21 Rigel Pharmaceuticals Inc Prodrugs aus 2,4-pyrimidindiamin-verbindungen und ihre verwendungen
US8227455B2 (en) 2005-04-18 2012-07-24 Rigel Pharmaceuticals, Inc. Methods of treating cell proliferative disorders
JP4981673B2 (ja) * 2005-09-13 2012-07-25 エーザイ・アール・アンド・ディー・マネジメント株式会社 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物およびその製造方法
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
AU2009212514A1 (en) * 2008-02-05 2009-08-13 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
CA2937222C (en) * 2009-06-25 2019-06-04 Alkermes Pharma Ireland Limited Prodrugs of nh-acidic compounds
LT2445502T (lt) 2009-06-25 2017-09-25 Alkermes Pharma Ireland Limited Heterocikliniai junginiai, skirti neurologinių ir fiziologinių susirgimų gydymui
AU2011270701B2 (en) 2010-06-24 2015-05-14 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives
KR101974793B1 (ko) 2015-07-06 2019-05-02 길리애드 사이언시즈, 인코포레이티드 Cot 조정제 및 그의 사용 방법
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
EP3761983A1 (en) 2018-03-05 2021-01-13 Alkermes Pharma Ireland Limited Aripiprazole dosing strategy
ES2975753T3 (es) * 2018-03-05 2024-07-12 Teon Therapeutics Inc Antagonistas del receptor de adenosina y usos de los mismos
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
TW202116356A (zh) 2019-07-10 2021-05-01 美商斯布雷克薩三號公司 作為治療劑之微管靶向藥劑之肽結合物
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
AU2021249010B2 (en) 2020-03-30 2024-09-26 Gilead Sciences, Inc. Solid forms of (S)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1H-1,2,3-triazol-4-yl)2-methyl-1-oxo-1,2- dihydroisoquinolin-5-yl)methyl)))amino)8-chloro-(neopentylamino)quinoline-3-carb onitrile a cot inhibitor compound
JP7446475B2 (ja) 2020-04-02 2024-03-08 ギリアード サイエンシーズ， インコーポレイテッド Ｃｏｔ阻害剤化合物を調製するためのプロセス
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

Citations (1)

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Publication number Priority date Publication date Assignee Title
US5602169A (en) * 1995-06-07 1997-02-11 Bristol-Myers Squibb Company 3-substituted oxindole derivatives as potassium channel modulators

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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
KR20010033811A (ko) 1997-12-31 2001-04-25 토마스 안 빅토리아 2차 및 3차 아민을 함유하는 약제의 물에 용해가능한프로드럭 및 그것의 제조방법
PT1056754E (pt) * 1998-01-29 2004-03-31 Bristol Myers Squibb Co Derivados fosfatados de 1,3,4-oxadiazolona de diarilo

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5602169A (en) * 1995-06-07 1997-02-11 Bristol-Myers Squibb Company 3-substituted oxindole derivatives as potassium channel modulators

Also Published As

Publication number Publication date
EP1485085A4 (en) 2007-03-14
PL372413A1 (en) 2005-07-25
RU2004131201A (ru) 2005-05-10
BR0308737A (pt) 2005-01-11
NO20044442L (no) 2004-10-19
US6930100B2 (en) 2005-08-16
IL164022A (en) 2008-04-13
HRP20040853A2 (en) 2004-12-31
CO5611143A2 (es) 2006-02-28
IS7456A (is) 2004-09-17
UA77296C2 (en) 2006-11-15
CN1652769A (zh) 2005-08-10
AU2003215017A1 (en) 2003-10-08
JP2005526097A (ja) 2005-09-02
JP4359150B2 (ja) 2009-11-04
GEP20074230B (en) 2007-11-12
CA2479256A1 (en) 2003-10-02
KR100951499B1 (ko) 2010-04-07
RS81904A (sr) 2007-02-05
MXPA04008999A (es) 2004-12-07
EP1485085A1 (en) 2004-12-15
US20030195169A1 (en) 2003-10-16
RU2312857C2 (ru) 2007-12-20
NZ535365A (en) 2006-07-28
KR20040106293A (ko) 2004-12-17
IL164022A0 (en) 2005-12-18
ZA200407337B (en) 2006-02-22
WO2003080047A1 (en) 2003-10-02

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