JP4789621B2 - ジフェニルUraIMPDHインヒビターおよびアポトーシス誘導性抗癌剤を含む組成物 - Google Patents

ジフェニルUraIMPDHインヒビターおよびアポトーシス誘導性抗癌剤を含む組成物 Download PDF

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Publication number
JP4789621B2
JP4789621B2 JP2005508461A JP2005508461A JP4789621B2 JP 4789621 B2 JP4789621 B2 JP 4789621B2 JP 2005508461 A JP2005508461 A JP 2005508461A JP 2005508461 A JP2005508461 A JP 2005508461A JP 4789621 B2 JP4789621 B2 JP 4789621B2
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composition
compound
apoptosis
alkynyl
cancer
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JP2006524186A (ja
JP2006524186A5 (enExample
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ジュグヌ ジェーン−パンデー,
ロバート ジェイ. フラム,
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/17Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/275Nitriles; Isonitriles
    • A61K31/277Nitriles; Isonitriles having a ring, e.g. verapamil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/4211,3-Oxazoles, e.g. pemoline, trimethadione
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
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    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61P35/00Antineoplastic agents
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
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  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2005508461A 2002-12-06 2003-12-04 ジフェニルUraIMPDHインヒビターおよびアポトーシス誘導性抗癌剤を含む組成物 Expired - Fee Related JP4789621B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US43155502P 2002-12-06 2002-12-06
US60/431,555 2002-12-06
US49626103P 2003-08-19 2003-08-19
US60/496,261 2003-08-19
PCT/US2003/038523 WO2004052349A2 (en) 2002-12-06 2003-12-04 Compositions comprising a combination of diphenyl ura impdh inhibitors and apoptosis-inducing anti-cancer agents

Publications (3)

Publication Number Publication Date
JP2006524186A JP2006524186A (ja) 2006-10-26
JP2006524186A5 JP2006524186A5 (enExample) 2007-01-25
JP4789621B2 true JP4789621B2 (ja) 2011-10-12

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JP2005508461A Expired - Fee Related JP4789621B2 (ja) 2002-12-06 2003-12-04 ジフェニルUraIMPDHインヒビターおよびアポトーシス誘導性抗癌剤を含む組成物

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US (1) US7943593B2 (enExample)
EP (1) EP1575579B1 (enExample)
JP (1) JP4789621B2 (enExample)
AT (1) ATE424198T1 (enExample)
AU (1) AU2003298868B2 (enExample)
CA (1) CA2510006C (enExample)
DE (1) DE60326488D1 (enExample)
WO (1) WO2004052349A2 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009505945A (ja) * 2005-05-26 2009-02-12 バーテックス ファーマシューティカルズ インコーポレイテッド (s)−1−シアノブタン−2−イル(s)−1−(3−(3−(3−メトキシ−4−(オキサゾール−5−イル)フェニル)ウレイド)フェニル)エチルカルバメートの多形形態
AU2020253560A1 (en) * 2019-04-05 2021-11-25 Prolynx Llc Improved conjugation linkers
JP2022136035A (ja) * 2021-03-04 2022-09-15 国立大学法人東京農工大学 化合物、該化合物を用いた金属ナノ粒子複合体、及び標的分子の検出方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2001509132A (ja) * 1996-04-23 2001-07-10 バーテックス ファーマシューティカルズ インコーポレイテッド Impdh酵素のインヒビターとしての尿素誘導体
JP2002539258A (ja) * 1999-03-19 2002-11-19 バーテックス ファーマシューティカルズ インコーポレイテッド Impdh酵素のインヒビター

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4210745A (en) * 1978-01-04 1980-07-01 The United States Of America As Represented By The Department Of Health, Education And Welfare Procedure for the preparation of 9-β-D-arabinofuranosyl-2-fluoroadenine
US4357324A (en) * 1981-02-24 1982-11-02 The United States Of America As Represented By The Department Of Health And Human Services Prodrug derivatives of 9β-D-arabinofuranosyl-2-fluoroadenine
TW409125B (en) * 1996-04-22 2000-10-21 Novartis Ag Antivirally active heterocyclic azahexane derivatives
AU723730B2 (en) 1996-04-23 2000-09-07 Vertex Pharmaceuticals Incorporated Urea derivatives as inhibitors of IMPDH enzyme

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2001509132A (ja) * 1996-04-23 2001-07-10 バーテックス ファーマシューティカルズ インコーポレイテッド Impdh酵素のインヒビターとしての尿素誘導体
JP2002539258A (ja) * 1999-03-19 2002-11-19 バーテックス ファーマシューティカルズ インコーポレイテッド Impdh酵素のインヒビター

Also Published As

Publication number Publication date
AU2003298868B2 (en) 2009-09-17
WO2004052349A3 (en) 2004-07-29
JP2006524186A (ja) 2006-10-26
AU2003298868A1 (en) 2004-06-30
US7943593B2 (en) 2011-05-17
ATE424198T1 (de) 2009-03-15
DE60326488D1 (de) 2009-04-16
EP1575579B1 (en) 2009-03-04
WO2004052349A2 (en) 2004-06-24
EP1575579A2 (en) 2005-09-21
US20050059734A1 (en) 2005-03-17
CA2510006C (en) 2012-02-07
CA2510006A1 (en) 2004-06-24

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