JP2012504631A - 選択的プロトン共役葉酸トランスポーターおよび葉酸受容体、ならびにgarftアーゼインヒビター化合物、ならびにそれらの使用方法 - Google Patents

選択的プロトン共役葉酸トランスポーターおよび葉酸受容体、ならびにgarftアーゼインヒビター化合物、ならびにそれらの使用方法 Download PDF

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JP2012504631A
JP2012504631A JP2011530162A JP2011530162A JP2012504631A JP 2012504631 A JP2012504631 A JP 2012504631A JP 2011530162 A JP2011530162 A JP 2011530162A JP 2011530162 A JP2011530162 A JP 2011530162A JP 2012504631 A JP2012504631 A JP 2012504631A
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アレーム ガンジー,
ラリー エイチ. マザーリー,
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デュケイン ユニバーシティー オブ ザ ホリー スピリット
ウェイン ステート ユニバーシティー
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00Antineoplastic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

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  • Life Sciences & Earth Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Epidemiology (AREA)
  • Rheumatology (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2011530162A 2008-10-01 2009-09-30 選択的プロトン共役葉酸トランスポーターおよび葉酸受容体、ならびにgarftアーゼインヒビター化合物、ならびにそれらの使用方法 Withdrawn JP2012504631A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US12/242,988 2008-10-01
US12/242,988 US8252804B2 (en) 2008-10-01 2008-10-01 Selective proton coupled folate transporter and folate receptor, and GARFTase inhibitor compounds and methods of using the same
PCT/US2009/058968 WO2010039792A1 (en) 2008-10-01 2009-09-30 Selective proton coupled folate transporter and folate receptor, and garftase inhibitor compounds and methods of using the same

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JP2014182217A Division JP2014224159A (ja) 2008-10-01 2014-09-08 選択的プロトン共役葉酸トランスポーターおよび葉酸受容体、ならびにgarftアーゼインヒビター化合物、ならびにそれらの使用方法

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JP2012504631A true JP2012504631A (ja) 2012-02-23
JP2012504631A5 JP2012504631A5 (enExample) 2012-11-15

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JP2011530162A Withdrawn JP2012504631A (ja) 2008-10-01 2009-09-30 選択的プロトン共役葉酸トランスポーターおよび葉酸受容体、ならびにgarftアーゼインヒビター化合物、ならびにそれらの使用方法
JP2014182217A Pending JP2014224159A (ja) 2008-10-01 2014-09-08 選択的プロトン共役葉酸トランスポーターおよび葉酸受容体、ならびにgarftアーゼインヒビター化合物、ならびにそれらの使用方法

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US (5) US8252804B2 (enExample)
EP (2) EP2348843B1 (enExample)
JP (2) JP2012504631A (enExample)
CA (2) CA2993404C (enExample)
WO (1) WO2010039792A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014224159A (ja) * 2008-10-01 2014-12-04 デュケイン ユニバーシティー オブ ザ ホリー スピリット 選択的プロトン共役葉酸トランスポーターおよび葉酸受容体、ならびにgarftアーゼインヒビター化合物、ならびにそれらの使用方法
JP2017537107A (ja) * 2014-12-02 2017-12-14 イーライ リリー アンド カンパニー 1−オキソ−1,2−ジヒドロイソキノリン−7−イル−(5−置換−チオフェン−2−イル)−スルホンアミド化合物、それらの化合物を含む製剤、がん治療におけるaicarft阻害剤としてのそれらの使用

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20110082158A1 (en) * 2008-10-01 2011-04-07 Aleem Gangjee Selective proton coupled folate transporter and folate receptor, and garftase and/or other folate metabolizing enzymes inhibitor compounds and methods of using the same
US9481678B2 (en) * 2015-02-09 2016-11-01 Duquesne University Of The Holy Ghost Substituted pyrrolo[2,3-D]dipyrimidines for selectively targeting tumor cells with FR-alpha and FR-beta type receptors
CN105111197B (zh) * 2015-08-26 2021-05-04 上海鼎雅药物化学科技有限公司 雷替曲塞的合成方法
WO2023086821A1 (en) * 2021-11-11 2023-05-19 Duquesne University Of The Holy Spirit Targeted therapy of pyrrolo[2,3-d]pyrimidine antifolates in a syngeneic mouse model of high grade serous ovarian cancer

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US5028608A (en) * 1989-12-11 1991-07-02 The Trustees Of Princeton University N-(6-Amino-(pyrrolo(2,3-d)pyrimidin-3-ylacyl) )-glutamic acid derivatives
JPH03173890A (ja) * 1989-09-21 1991-07-29 Takeda Chem Ind Ltd ピロロ[2,3―d]ピリミジン誘導体,その製造法,用途及び中間体
US5248775A (en) * 1989-12-11 1993-09-28 The Trustees Of Princeton University Pyrrolo(2,3-d)pyrimidines
JPH06172358A (ja) * 1991-12-27 1994-06-21 Takeda Chem Ind Ltd 縮合ピリミジン誘導体、その製造法および用途
JPH10503762A (ja) * 1994-07-28 1998-04-07 アグーロン ファーマシューティカルズ,インコーポレーテッド 抗増殖剤およびgarft阻害剤として有用な化合物
JP2000516961A (ja) * 1996-08-30 2000-12-19 イーライ・リリー・アンド・カンパニー 非古典的ピロロ[2,3―d]ピリミジン抗葉酸物質
US20080045552A1 (en) * 2006-06-28 2008-02-21 Duquesne University Of The Holy Ghost Methods of using selective chemotherapeutic agents for targeting tumor cells
WO2008027949A2 (en) * 2006-09-01 2008-03-06 Duquesne University Of The Holy Spirit Thieno pyrimidine compounds
CN101195625A (zh) * 2007-12-06 2008-06-11 上海交通大学 用于抗肿瘤药物抗叶酸剂及其盐和中间体

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US4496639A (en) 1983-07-05 1985-01-29 Ceramatec, Inc. Hydrogen selenide treatment of electrolytes
WO1991000092A1 (en) * 1989-06-13 1991-01-10 Smithkline Beecham Corporation Inhibition of interleukin-1 and tumor necrosis factor production by monocytes and/or macrophages
JPH04117381A (ja) 1989-12-20 1992-04-17 Takeda Chem Ind Ltd 縮合複素環化合物,その製造法,用途及び中間体
EP0438261A3 (en) 1990-01-16 1992-02-26 Takeda Chemical Industries, Ltd. Condensed heterocyclic glutamic acid derivatives, their production and use
JPH0578362A (ja) 1990-01-16 1993-03-30 Takeda Chem Ind Ltd 縮合複素環化合物,その製造法,用途及び中間体
US5939420A (en) * 1991-04-08 1999-08-17 Duquesne University Of The Holy Ghost Pyrrolo 2,3d!derivatives
JP3144903B2 (ja) 1991-08-21 2001-03-12 エーザイ株式会社 縮合ピリミジン誘導体
ATE173251T1 (de) * 1991-08-21 1998-11-15 Eisai Co Ltd Kondensierte pyrimidinderivate als antitumorverbindungen
EP0549291A1 (en) 1991-12-27 1993-06-30 Takeda Chemical Industries, Ltd. Thymidylate synthase inhibitors
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EP1424336A4 (en) * 2001-09-03 2004-11-10 Takeda Chemical Industries Ltd 1,3-BENZOTHIAZINE DERIVATIVES AND THEIR USE
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US7981902B2 (en) * 2006-06-28 2011-07-19 Duquesne University Of The Holy Ghost Substituted pyrrolo[2,3-d]pyrimidines for selectively targeting tumor cells with FR type receptors
US8252804B2 (en) 2008-10-01 2012-08-28 Duquesne University Of The Holy Spirit Selective proton coupled folate transporter and folate receptor, and GARFTase inhibitor compounds and methods of using the same

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JPH03173890A (ja) * 1989-09-21 1991-07-29 Takeda Chem Ind Ltd ピロロ[2,3―d]ピリミジン誘導体,その製造法,用途及び中間体
US5028608A (en) * 1989-12-11 1991-07-02 The Trustees Of Princeton University N-(6-Amino-(pyrrolo(2,3-d)pyrimidin-3-ylacyl) )-glutamic acid derivatives
US5248775A (en) * 1989-12-11 1993-09-28 The Trustees Of Princeton University Pyrrolo(2,3-d)pyrimidines
JPH06172358A (ja) * 1991-12-27 1994-06-21 Takeda Chem Ind Ltd 縮合ピリミジン誘導体、その製造法および用途
JPH10503762A (ja) * 1994-07-28 1998-04-07 アグーロン ファーマシューティカルズ,インコーポレーテッド 抗増殖剤およびgarft阻害剤として有用な化合物
JP2000516961A (ja) * 1996-08-30 2000-12-19 イーライ・リリー・アンド・カンパニー 非古典的ピロロ[2,3―d]ピリミジン抗葉酸物質
US20080045552A1 (en) * 2006-06-28 2008-02-21 Duquesne University Of The Holy Ghost Methods of using selective chemotherapeutic agents for targeting tumor cells
WO2008027949A2 (en) * 2006-09-01 2008-03-06 Duquesne University Of The Holy Spirit Thieno pyrimidine compounds
CN101195625A (zh) * 2007-12-06 2008-06-11 上海交通大学 用于抗肿瘤药物抗叶酸剂及其盐和中间体

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2014224159A (ja) * 2008-10-01 2014-12-04 デュケイン ユニバーシティー オブ ザ ホリー スピリット 選択的プロトン共役葉酸トランスポーターおよび葉酸受容体、ならびにgarftアーゼインヒビター化合物、ならびにそれらの使用方法
JP2017537107A (ja) * 2014-12-02 2017-12-14 イーライ リリー アンド カンパニー 1−オキソ−1,2−ジヒドロイソキノリン−7−イル−(5−置換−チオフェン−2−イル)−スルホンアミド化合物、それらの化合物を含む製剤、がん治療におけるaicarft阻害剤としてのそれらの使用

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WO2010039792A1 (en) 2010-04-08
US10000498B2 (en) 2018-06-19
CA2993404C (en) 2020-07-07
EP2348843A4 (en) 2012-08-08
US20180346474A1 (en) 2018-12-06
CA2993404A1 (en) 2010-04-08
CA2739250C (en) 2018-03-20
US10611767B2 (en) 2020-04-07
US20200190097A1 (en) 2020-06-18
US20100081676A1 (en) 2010-04-01
US20120295926A1 (en) 2012-11-22
EP2348843A1 (en) 2011-08-03
CA2739250A1 (en) 2010-04-08
EP2995199A1 (en) 2016-03-16
EP2348843B1 (en) 2015-11-11
US20170114066A1 (en) 2017-04-27
JP2014224159A (ja) 2014-12-04
US8252804B2 (en) 2012-08-28
US11053252B2 (en) 2021-07-06
US9511069B2 (en) 2016-12-06
EP2995199B1 (en) 2018-03-14

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