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
Application number
JP2017552007A
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English (en)
Japanese (ja)
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JP2018501315A5 (enExample
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
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.)
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Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
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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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/54—Heterocyclic 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
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (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 (enExample) 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 (enExample)
EP (1) EP3237415A1 (enExample)
JP (1) JP2018501315A (enExample)
CN (1) CN107257798A (enExample)
AR (1) AR103232A1 (enExample)
TW (1) TW201630907A (enExample)
WO (1) WO2016106266A1 (enExample)

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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CA3043383A1 (en) 2016-11-14 2018-05-17 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
US10428067B2 (en) 2017-06-07 2019-10-01 Plexxikon Inc. Compounds and methods for kinase modulation
BR112020011771A2 (pt) 2017-12-18 2020-11-17 Bristol-Myers Squibb Company compostos 4-azaindol
FI3796975T3 (fi) 2018-05-22 2023-11-20 Orsobio Inc Sulfonyyliaminobentsamidijohdannaisia
CA3128946A1 (en) 2019-02-07 2020-08-13 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
AR123284A1 (es) * 2020-08-19 2022-11-16 Bristol Myers Squibb Co Compuestos heteroarílicos sustituidos útiles como inhibidores de tlr9
EP4469457A1 (en) * 2022-01-27 2024-12-04 The Broad Institute Inc. Substituted heterocyclic csnk1 inhibitors
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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

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Patent Citations (4)

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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

Also Published As

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

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