KR100748299B1 - 아졸 화합물의 수용성 프로드럭 - Google Patents

아졸 화합물의 수용성 프로드럭 Download PDF

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Publication number
KR100748299B1
KR100748299B1 KR1020027009320A KR20027009320A KR100748299B1 KR 100748299 B1 KR100748299 B1 KR 100748299B1 KR 1020027009320 A KR1020027009320 A KR 1020027009320A KR 20027009320 A KR20027009320 A KR 20027009320A KR 100748299 B1 KR100748299 B1 KR 100748299B1
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South Korea
Prior art keywords
formula
compound
hydrogen
pharmaceutically acceptable
halogen
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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.)
Expired - Lifetime
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KR1020027009320A
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English (en)
Korean (ko)
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KR20020070492A (ko
Inventor
야스쯔꾸 우에다
존 디. 마티스켈라
저지 고릭
토마스 더블유. 휴다이마
충-핀 첸
Original Assignee
에자이 알앤드디 매니지먼트 가부시키가이샤
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Publication of KR20020070492A publication Critical patent/KR20020070492A/ko
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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
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6503—Five-membered rings
    • C07F9/6506—Five-membered rings having the nitrogen atoms in positions 1 and 3
    • 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
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
    • C07F9/6515—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having three nitrogen atoms as the only ring hetero atoms
    • C07F9/6518—Five-membered rings
    • 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
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Oncology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Communicable Diseases (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Polymerization Catalysts (AREA)
KR1020027009320A 2000-01-20 2001-01-16 아졸 화합물의 수용성 프로드럭 Expired - Lifetime KR100748299B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US17716900P 2000-01-20 2000-01-20
US60/177,169 2000-01-20
US24996900P 2000-11-20 2000-11-20
US60/249,969 2000-11-20

Publications (2)

Publication Number Publication Date
KR20020070492A KR20020070492A (ko) 2002-09-09
KR100748299B1 true KR100748299B1 (ko) 2007-08-09

Family

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Family Applications (1)

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KR1020027009320A Expired - Lifetime KR100748299B1 (ko) 2000-01-20 2001-01-16 아졸 화합물의 수용성 프로드럭

Country Status (22)

Country Link
US (1) US6362172B2 (enExample)
EP (1) EP1284737B1 (enExample)
JP (1) JP3766804B2 (enExample)
KR (1) KR100748299B1 (enExample)
CN (1) CN1178665C (enExample)
AT (1) ATE300946T1 (enExample)
AU (1) AU782177C (enExample)
BR (1) BR0107618A (enExample)
CA (1) CA2397734C (enExample)
CZ (1) CZ20022822A3 (enExample)
DE (1) DE60112433T2 (enExample)
DK (1) DK1284737T5 (enExample)
ES (1) ES2247131T3 (enExample)
HU (1) HU229226B1 (enExample)
IL (2) IL150798A0 (enExample)
MX (1) MXPA02007120A (enExample)
NO (1) NO330352B1 (enExample)
NZ (1) NZ519354A (enExample)
PL (1) PL206024B1 (enExample)
PT (1) PT1284737E (enExample)
RU (1) RU2266909C2 (enExample)
WO (1) WO2001052852A1 (enExample)

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IL166241A0 (en) 2002-07-29 2006-01-15 Rigel Pharmaceuticals Inc Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
ES2421139T3 (es) 2003-07-30 2013-08-29 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias
US7501426B2 (en) 2004-02-18 2009-03-10 Boehringer Ingelheim International Gmbh 8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
DE102004054054A1 (de) 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
US7449458B2 (en) 2005-01-19 2008-11-11 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
JO2691B1 (en) * 2005-05-03 2013-03-03 ايساي آر آند دي مانجمنت كو.، ليمتد Monolysine salts for azole compounds
DE102005035891A1 (de) 2005-07-30 2007-02-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg 8-(3-Amino-piperidin-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
EP1964843B1 (en) * 2005-12-20 2013-08-28 Eisai R&D Management Co., Ltd. Process for production of water-soluble azole prodrug
WO2007092580A2 (en) * 2006-02-08 2007-08-16 Phibro-Tech Inc. Biocidal azole emulsion concentrates having high active ingredient content
KR101250632B1 (ko) 2006-02-22 2013-04-03 에자이 알앤드디 매니지먼트 가부시키가이샤 안정화 의약 조성물
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
BRPI0711558A2 (pt) 2006-05-04 2011-11-08 Boeringer Ingelheim Internat Gmbh polimorfos
PE20080251A1 (es) 2006-05-04 2008-04-25 Boehringer Ingelheim Int Usos de inhibidores de dpp iv
PE20140960A1 (es) 2008-04-03 2014-08-15 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
JP5757864B2 (ja) * 2008-05-20 2015-08-05 ニューロジェシックス, インコーポレイテッド 水溶性アセトアミノフェン類似体
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UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
BRPI0916997A2 (pt) 2008-08-06 2020-12-15 Boehringer Ingelheim International Gmbh Inibidor de dpp-4 e seu uso
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US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
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AR074990A1 (es) 2009-01-07 2011-03-02 Boehringer Ingelheim Int Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
EA034869B1 (ru) 2009-11-27 2020-03-31 Бёрингер Ингельхайм Интернациональ Гмбх Лечение генотипированных пациентов с диабетом ингибиторами дпп-4, такими как линаглиптин
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WO2012060448A1 (ja) 2010-11-05 2012-05-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 抗真菌剤としての併用医薬組成物
US9034883B2 (en) 2010-11-15 2015-05-19 Boehringer Ingelheim International Gmbh Vasoprotective and cardioprotective antidiabetic therapy
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EP2723452A2 (en) 2011-06-22 2014-04-30 Vyome Biosciences Pvt Ltd Conjugate-based antifungal and antibacterial prodrugs
EP3517539B1 (en) 2011-07-15 2022-12-14 Boehringer Ingelheim International GmbH Substituted dimeric quinazoline derivative, its preparation and its use in pharmaceutical compositions for the treatment of type i and ii diabetes
US8426450B1 (en) * 2011-11-29 2013-04-23 Helsinn Healthcare Sa Substituted 4-phenyl pyridines having anti-emetic effect
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US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
US9981040B2 (en) * 2012-04-20 2018-05-29 Eisai R&D Management Co., Ltd. Capsule formulation
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JP6224084B2 (ja) 2012-05-14 2017-11-01 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 糸球体上皮細胞関連障害及び/又はネフローゼ症候群の治療に用いるdpp−4阻害薬としてのキサンチン誘導体
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WO1997028169A1 (en) * 1996-02-02 1997-08-07 Pfizer Research And Development Company, N.V./S.A. Triazole derivatives useful in therapy

Also Published As

Publication number Publication date
PL206024B1 (pl) 2010-06-30
AU782177B2 (en) 2005-07-07
EP1284737A4 (en) 2003-03-19
NO20023468D0 (no) 2002-07-19
CA2397734A1 (en) 2001-07-26
AU2948501A (en) 2001-07-31
ES2247131T3 (es) 2006-03-01
CA2397734C (en) 2010-08-17
AU782177C (en) 2007-10-18
RU2266909C2 (ru) 2005-12-27
HUP0204405A2 (en) 2003-05-28
CZ20022822A3 (cs) 2003-02-12
CN1395485A (zh) 2003-02-05
PT1284737E (pt) 2005-11-30
NZ519354A (en) 2004-05-28
EP1284737B1 (en) 2005-08-03
US6362172B2 (en) 2002-03-26
EP1284737A1 (en) 2003-02-26
IL150798A (en) 2006-08-01
HU229226B1 (en) 2013-09-30
KR20020070492A (ko) 2002-09-09
PL356164A1 (en) 2004-06-14
CN1178665C (zh) 2004-12-08
DK1284737T3 (da) 2005-11-28
JP3766804B2 (ja) 2006-04-19
WO2001052852A1 (en) 2001-07-26
DE60112433D1 (de) 2005-09-08
DK1284737T5 (da) 2007-09-24
ATE300946T1 (de) 2005-08-15
DE60112433T2 (de) 2006-05-18
JP2003520235A (ja) 2003-07-02
US20010041691A1 (en) 2001-11-15
NO20023468L (no) 2002-07-29
BR0107618A (pt) 2002-11-12
IL150798A0 (en) 2003-02-12
HUP0204405A3 (en) 2005-02-28
NO330352B1 (no) 2011-04-04
MXPA02007120A (es) 2003-01-28

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