CA2479256A1 - Phosphate prodrugs of fluorooxindoles - Google Patents

Phosphate prodrugs of fluorooxindoles Download PDF

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Publication number
CA2479256A1
CA2479256A1 CA002479256A CA2479256A CA2479256A1 CA 2479256 A1 CA2479256 A1 CA 2479256A1 CA 002479256 A CA002479256 A CA 002479256A CA 2479256 A CA2479256 A CA 2479256A CA 2479256 A1 CA2479256 A1 CA 2479256A1
Authority
CA
Canada
Prior art keywords
chloro
fluoro
dihydro
methoxy
phenyl
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.)
Abandoned
Application number
CA002479256A
Other languages
English (en)
French (fr)
Inventor
Kevin W. Gillman
Piyasena Hewawasam
William D. Schmitz
Omar D. Lopez
John E. Starrett, Jr.
David P. Provencal
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Original Assignee
Individual
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.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of CA2479256A1 publication Critical patent/CA2479256A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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

Landscapes

  • 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)
CA002479256A 2002-03-20 2003-03-20 Phosphate prodrugs of fluorooxindoles Abandoned CA2479256A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36601002P 2002-03-20 2002-03-20
US60/366,010 2002-03-20
PCT/US2003/008613 WO2003080047A1 (en) 2002-03-20 2003-03-20 Phosphate prodrugs of fluorooxindoles

Publications (1)

Publication Number Publication Date
CA2479256A1 true CA2479256A1 (en) 2003-10-02

Family

ID=28454740

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002479256A Abandoned CA2479256A1 (en) 2002-03-20 2003-03-20 Phosphate prodrugs of fluorooxindoles

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
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
JP4359150B2 (ja) 2009-11-04
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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Legal Events

Date Code Title Description
EEER Examination request
FZDE Discontinued