JP2018501315A - TGFβ受容体アンタゴニスト - Google Patents

TGFβ受容体アンタゴニスト Download PDF

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Publication number
JP2018501315A
JP2018501315A JP2017552007A JP2017552007A JP2018501315A JP 2018501315 A JP2018501315 A JP 2018501315A JP 2017552007 A JP2017552007 A JP 2017552007A JP 2017552007 A JP2017552007 A JP 2017552007A JP 2018501315 A JP2018501315 A JP 2018501315A
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JP
Japan
Prior art keywords
alkyl
hydrogen
pyridin
halogen
independently
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Pending
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JP2017552007A
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Japanese (ja)
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JP2018501315A5 (https=
Inventor
ブライアン・イー・フィンク
ユーフェン・ジャオ
ロバート・エム・ボルジレリ
ジャン・リーピン
キョン・エス・キム
ムソニ・ジー・カマウ
アンドリュー・ジェイ・テベン
ジャン・ヨン
アンドリュー・エフ・ドネル
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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Publication of JP2018501315A publication Critical patent/JP2018501315A/ja
Publication of JP2018501315A5 publication Critical patent/JP2018501315A5/ja
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/582Recycling of unreacted starting or intermediate materials

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2017552007A 2014-12-22 2015-12-22 TGFβ受容体アンタゴニスト Pending JP2018501315A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462095328P 2014-12-22 2014-12-22
US62/095,328 2014-12-22
PCT/US2015/067252 WO2016106266A1 (en) 2014-12-22 2015-12-22 TGFβ RECEPTOR ANTAGONISTS

Publications (2)

Publication Number Publication Date
JP2018501315A true JP2018501315A (ja) 2018-01-18
JP2018501315A5 JP2018501315A5 (https=) 2019-01-24

Family

ID=55135542

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2017552007A Pending JP2018501315A (ja) 2014-12-22 2015-12-22 TGFβ受容体アンタゴニスト

Country Status (7)

Country Link
US (1) US9708316B2 (https=)
EP (1) EP3237415A1 (https=)
JP (1) JP2018501315A (https=)
CN (1) CN107257798A (https=)
AR (1) AR103232A1 (https=)
TW (1) TW201630907A (https=)
WO (1) WO2016106266A1 (https=)

Cited By (1)

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JP2021528451A (ja) * 2018-06-28 2021-10-21 フェネックス−エフイクスエル ゲゼルシャフト ミット ベシュレンクテル ハフツング 二環式コア部分を有する新規lxrモジュレーター

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AU2017357333A1 (en) 2016-11-14 2019-05-02 Jiangsu Hengrui Medicine Co., Ltd. 3,4-bipyridyl pyrazole derivative, and preparation method therefor and medical application thereof
WO2018171611A1 (zh) * 2017-03-22 2018-09-27 江苏恒瑞医药股份有限公司 6-吡唑-[1,2,4]三唑并[4,3-a]吡啶-3-酰胺类衍生物、其制备方法及其在医药上的应用
WO2018226846A1 (en) * 2017-06-07 2018-12-13 Plexxikon Inc. Compounds and methods for kinase modulation
FI3728252T3 (fi) * 2017-12-18 2023-10-18 Bristol Myers Squibb Co 4-atsaindoliyhdisteitä
LT3796975T (lt) 2018-05-22 2023-12-11 Orsobio, Inc. Sulfonilaminobenzamido dariniai
EP3921317B1 (en) 2019-02-07 2023-08-02 Bayer Aktiengesellschaft 3-amino-2-[2-(acylamino)pyridin-4-yl]-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one as csnk1 inhibitors
CN112694477B (zh) * 2019-10-22 2024-02-06 四川科伦博泰生物医药股份有限公司 吡唑并环类化合物,包含其的药物组合物,其制备方法及其用途
CN110885329B (zh) * 2019-12-16 2020-12-15 诚达药业股份有限公司 一种1,7-萘啶衍生物的合成方法
EP4188928B1 (en) 2020-07-29 2024-07-24 Bayer Aktiengesellschaft Substituted 1 h-pyrrolo[3,2-b]pyridin compounds and methods of use thereof
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Publication number Priority date Publication date Assignee Title
US20050014942A1 (en) * 2001-10-30 2005-01-20 Yasufumi Maruyama Amide derivatives and drugs
JP2006519249A (ja) * 2003-03-04 2006-08-24 ファイザー・プロダクツ・インク 形質転換成長因子(tgf)阻害薬としての新規縮合複素芳香族化合物
WO2010017541A2 (en) * 2008-08-08 2010-02-11 The Johns Hopkins University Compositions and methods for treatment of neurodegenerative disease
JP2012506389A (ja) * 2008-10-23 2012-03-15 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング アザインドール誘導体

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021528451A (ja) * 2018-06-28 2021-10-21 フェネックス−エフイクスエル ゲゼルシャフト ミット ベシュレンクテル ハフツング 二環式コア部分を有する新規lxrモジュレーター
JP7214086B2 (ja) 2018-06-28 2023-01-30 オルソバイオ,インコーポレイティド 二環式コア部分を有する新規lxrモジュレーター

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WO2016106266A1 (en) 2016-06-30
TW201630907A (zh) 2016-09-01
EP3237415A1 (en) 2017-11-01
US9708316B2 (en) 2017-07-18
CN107257798A (zh) 2017-10-17
AR103232A1 (es) 2017-04-26
US20160176871A1 (en) 2016-06-23

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