JP6243918B2 - Ｐｋｍ２調節因子およびそれらの使用方法 - Google Patents

Ｐｋｍ２調節因子およびそれらの使用方法 Download PDF

Info

Publication number
JP6243918B2
JP6243918B2 JP2015537799A JP2015537799A JP6243918B2 JP 6243918 B2 JP6243918 B2 JP 6243918B2 JP 2015537799 A JP2015537799 A JP 2015537799A JP 2015537799 A JP2015537799 A JP 2015537799A JP 6243918 B2 JP6243918 B2 JP 6243918B2
Authority
JP
Japan
Prior art keywords
pharmaceutically acceptable
stereoisomer
tautomer
acceptable salt
compound
Prior art date
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.)
Active
Application number
JP2015537799A
Other languages
English (en)
Japanese (ja)
Other versions
JP2015536325A (ja
JP2015536325A5 (cg-RX-API-DMAC7.html
Inventor
コク−カン ホ，
コク−カン ホ，
ヨン シュー，
ヨン シュー，
マイケル デイビッド サンダース，
マイケル デイビッド サンダース，
シャオフイ リウ，
シャオフイ リウ，
スコット アルバート ピーアス，
スコット アルバート ピーアス，
ケビン ブレット ライト，
ケビン ブレット ライト，
ジェイソン マーク フォークス，
ジェイソン マーク フォークス，
ケネス マーク パーネル，
ケネス マーク パーネル，
スティーブン ブライアン カナー，
スティーブン ブライアン カナー，
デイビッド リー ボルマー，
デイビッド リー ボルマー，
ジーフア リウ，
ジーフア リウ，
Original Assignee
トレロ ファーマシューティカルズ， インコーポレイテッド
トレロ ファーマシューティカルズ， インコーポレイテッド
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.)
Filing date
Publication date
Application filed by トレロ ファーマシューティカルズ， インコーポレイテッド, トレロ ファーマシューティカルズ， インコーポレイテッド filed Critical トレロ ファーマシューティカルズ， インコーポレイテッド
Publication of JP2015536325A publication Critical patent/JP2015536325A/ja
Publication of JP2015536325A5 publication Critical patent/JP2015536325A5/ja
Application granted granted Critical
Publication of JP6243918B2 publication Critical patent/JP6243918B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/16—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero 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
    • C07F9/645—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
    • C07F9/65031—Five-membered rings having the nitrogen atoms in the positions 1 and 2

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
JP2015537799A 2012-10-16 2013-10-16 Ｐｋｍ２調節因子およびそれらの使用方法 Active JP6243918B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261714659P 2012-10-16 2012-10-16
US61/714,659 2012-10-16
US201361875855P 2013-09-10 2013-09-10
US61/875,855 2013-09-10
PCT/US2013/065296 WO2014062838A2 (en) 2012-10-16 2013-10-16 Pkm2 modulators and methods for their use

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2017203963A Division JP6526767B2 (ja) 2012-10-16 2017-10-20 Ｐｋｍ２調節因子およびそれらの使用方法

Publications (3)

Publication Number Publication Date
JP2015536325A JP2015536325A (ja) 2015-12-21
JP2015536325A5 JP2015536325A5 (cg-RX-API-DMAC7.html) 2016-12-01
JP6243918B2 true JP6243918B2 (ja) 2017-12-06

Family

ID=50488890

Family Applications (7)

Application Number Title Priority Date Filing Date
JP2015537799A Active JP6243918B2 (ja) 2012-10-16 2013-10-16 Ｐｋｍ２調節因子およびそれらの使用方法
JP2017203963A Active JP6526767B2 (ja) 2012-10-16 2017-10-20 Ｐｋｍ２調節因子およびそれらの使用方法
JP2018186629A Withdrawn JP2019023209A (ja) 2012-10-16 2018-10-01 Ｐｋｍ２調節因子およびそれらの使用方法
JP2020035656A Withdrawn JP2020105190A (ja) 2012-10-16 2020-03-03 Ｐｋｍ２調節因子およびそれらの使用方法
JP2020035657A Withdrawn JP2020097631A (ja) 2012-10-16 2020-03-03 Ｐｋｍ２調節因子およびそれらの使用方法
JP2021120679A Active JP7128331B2 (ja) 2012-10-16 2021-07-21 Ｐｋｍ２調節因子およびそれらの使用方法
JP2021129580A Pending JP2021181467A (ja) 2012-10-16 2021-08-06 Ｐｋｍ２調節因子およびそれらの使用方法

Family Applications After (6)

Application Number Title Priority Date Filing Date
JP2017203963A Active JP6526767B2 (ja) 2012-10-16 2017-10-20 Ｐｋｍ２調節因子およびそれらの使用方法
JP2018186629A Withdrawn JP2019023209A (ja) 2012-10-16 2018-10-01 Ｐｋｍ２調節因子およびそれらの使用方法
JP2020035656A Withdrawn JP2020105190A (ja) 2012-10-16 2020-03-03 Ｐｋｍ２調節因子およびそれらの使用方法
JP2020035657A Withdrawn JP2020097631A (ja) 2012-10-16 2020-03-03 Ｐｋｍ２調節因子およびそれらの使用方法
JP2021120679A Active JP7128331B2 (ja) 2012-10-16 2021-07-21 Ｐｋｍ２調節因子およびそれらの使用方法
JP2021129580A Pending JP2021181467A (ja) 2012-10-16 2021-08-06 Ｐｋｍ２調節因子およびそれらの使用方法

Country Status (6)

Country Link
US (5) US9394257B2 (cg-RX-API-DMAC7.html)
EP (1) EP2909181B1 (cg-RX-API-DMAC7.html)
JP (7) JP6243918B2 (cg-RX-API-DMAC7.html)
DK (1) DK2909181T3 (cg-RX-API-DMAC7.html)
ES (1) ES2644758T3 (cg-RX-API-DMAC7.html)
WO (1) WO2014062838A2 (cg-RX-API-DMAC7.html)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2909181T3 (da) * 2012-10-16 2017-11-20 Tolero Pharmaceuticals Inc PKM2-modulatorer og fremgangsmåder til anvendelse deraf
ES2788856T3 (es) 2017-03-20 2020-10-23 Forma Therapeutics Inc Composiciones de pirrolopirrol como activadores de quinasa de piruvato (PKR)
WO2019075367A1 (en) * 2017-10-13 2019-04-18 Tolero Pharmaceuticals, Inc. PKM2 ACTIVATORS IN COMBINATION WITH OXYGEN REACTIVE SPECIES FOR THE TREATMENT OF CANCER
WO2020061378A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
ES2989438T3 (es) 2018-09-19 2024-11-26 Novo Nordisk Healthcare Ag Activación de la piruvato cinasa R
CA3133460A1 (en) * 2019-03-22 2020-10-01 Sumitomo Dainippon Pharma Oncology, Inc. Compositions comprising pkm2 modulators and methods of treatment using the same
JP2022527451A (ja) * 2019-03-22 2022-06-02 スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド Ｐｋｍ２モジュレーターおよびその使用方法
WO2021026182A1 (en) 2019-08-06 2021-02-11 Biocryst Pharmaceuticals, Inc. Process-scale synthesis of a plasma kallikrein inhibitor
MA57202B1 (fr) 2019-09-19 2025-09-30 Novo Nordisk Health Care Ag Compositions d'activation de la pyruvate kinase r (pkr)
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R

Family Cites Families (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2779780A (en) 1955-03-01 1957-01-29 Du Pont 1, 4-diamino-2, 3-dicyano-1, 4-bis (substituted mercapto) butadienes and their preparation
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
JP2861087B2 (ja) * 1989-08-08 1999-02-24 三菱化学株式会社 Ｎ―アシル‐５‐ピラゾールカルボキサミド類およびこれを有効成分とする殺虫、殺ダニ剤
FI941572L (fi) 1991-10-07 1994-05-27 Oncologix Inc Anti-erbB-2-monoklonaalisten vasta-aineiden yhdistelmä ja käyttömenetelmä
DE69333807T2 (de) 1992-02-06 2006-02-02 Chiron Corp., Emeryville Marker für krebs und biosynthetisches bindeprotein dafür
IT1255527B (it) * 1992-09-29 1995-11-09 Mini Ricerca Scient Tecnolog Pirazolcarbossammidi ad attivita' insetticida ed acaricida
US6177401B1 (en) 1992-11-13 2001-01-23 Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften Use of organic compounds for the inhibition of Flk-1 mediated vasculogenesis and angiogenesis
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
EP0647450A1 (en) 1993-09-09 1995-04-12 BEHRINGWERKE Aktiengesellschaft Improved prodrugs for enzyme mediated activation
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
JP3053222B2 (ja) 1995-04-20 2000-06-19 ファイザー・インコーポレーテッド Ｍｍｐおよびｔｎｆ抑制剤としてのアリールスルホニルヒドロキサム酸誘導体
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
GB9520822D0 (en) 1995-10-11 1995-12-13 Wellcome Found Therapeutically active compounds
PT780386E (pt) 1995-12-20 2003-02-28 Hoffmann La Roche Inibidores de metaloprotease de matriz
DE19600097C1 (de) 1996-01-03 1997-07-31 Siemens Ag Verfahren und Vorrichtung zur Bestimmung einer Flüssigkeitshöhe mit Hilfe von Ultraschallimpulsen
KR100489174B1 (ko) 1996-03-05 2005-09-30 제네카-파마 소시에떼아노님 4-아닐리노퀴나졸린유도체
EP0818442A3 (en) 1996-07-12 1998-12-30 Pfizer Inc. Cyclic sulphone derivatives as inhibitors of metalloproteinases and of the production of tumour necrosis factor
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
CN1230185A (zh) 1996-07-13 1999-09-29 葛兰素集团有限公司 双环芳杂环化合物用作蛋白质酪氨酸激酶的抑制剂
PT912559E (pt) 1996-07-13 2003-03-31 Glaxo Group Ltd Compostos heterociclicos fundidos como inibidores de proteina tirosina quinase
AU712973B2 (en) 1996-07-18 1999-11-18 Pfizer Inc. Phosphinate based inhibitors of matrix metalloproteases
AU711585B2 (en) 1996-08-23 1999-10-14 Pfizer Inc. Arylsulfonylamino hydroxamic acid derivatives
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
AU5131998A (en) 1997-01-06 1998-08-03 Pfizer Inc. Cyclic sulfone derivatives
PL335027A1 (en) 1997-02-03 2000-03-27 Pfizer Prod Inc Derivatives of arylsulphonylamino hydroxamic acid
BR9807824A (pt) 1997-02-07 2000-03-08 Pfizer Derivados de n-hidróxi-beta-sulfonil-propionamida e seu uso como inibidores de metaloproteinases de matriz
JP3710489B2 (ja) 1997-02-11 2005-10-26 ファイザー・インク アリールスルホニルヒドロキサム酸誘導体
JP2002511852A (ja) 1997-05-07 2002-04-16 スージェン・インコーポレーテッド 蛋白質キナーゼ活性の調節剤としての２−インドリノン誘導体
EP0984692A4 (en) 1997-05-30 2001-02-21 Merck & Co Inc ANGIOGENESIS INHIBITORS
DK1003720T3 (da) 1997-08-08 2004-05-10 Pfizer Prod Inc Aryloxyarylsulfonylaminohydroxamsyrederivater
AU8816298A (en) 1997-08-22 1999-03-16 Zeneca Limited Oxindolylquinazoline derivatives as angiogenesis inhibitors
AU744939B2 (en) 1997-09-26 2002-03-07 Merck & Co., Inc. Novel angiogenesis inhibitors
KR100446363B1 (ko) 1997-11-11 2004-09-01 화이자 프로덕츠 인코포레이티드 항암제로 유용한 티에노피리미딘 및 티에노피리딘 유도체
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
GB9800569D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
GB9800575D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
EP1082305A4 (en) 1998-05-29 2001-09-26 Sugen Inc PYRROL SUBSTITUTED 2-INDOLINONE EFFECTIVE AS A PROTEIN KINASE INHIBITOR
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
DK1004578T3 (da) 1998-11-05 2004-06-28 Pfizer Prod Inc 5-oxo-pyrrolidin-2-carboxylsyrehydroxamidderivater
KR100609800B1 (ko) 1998-12-16 2006-08-09 워너-램버트 캄파니 엘엘씨 Ｍｅｋ 저해제를 사용한 관절염 치료 방법
UA71945C2 (en) 1999-01-27 2005-01-17 Pfizer Prod Inc Substituted bicyclic derivatives being used as anticancer agents
GB9912961D0 (en) 1999-06-03 1999-08-04 Pfizer Ltd Metalloprotease inhibitors
JP2001172261A (ja) * 1999-12-20 2001-06-26 Mitsubishi Chemicals Corp ピラゾールカルボン酸アミド類、およびこれを有効成分とする殺虫、殺ダニ剤
MXPA02008021A (es) 2000-02-15 2004-04-05 Sugen Inc Indolinonas sustituidas con pirroles inhibidoras de proteinquinasas.
YU2503A (sh) 2000-07-19 2006-05-25 Warner-Lambert Company Oksigenovani estri 4-jodo fenilamino benzhidroksamskih kiselina
US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
JP2004509115A (ja) * 2000-09-15 2004-03-25 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 プロテインキナーゼインヒビターとして有用なピラゾール化合物
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US20050085524A1 (en) * 2001-04-06 2005-04-21 Nihon Nohyaku Co,. Ltd. Pyrazolecarboxamides, intermediates therefor and pest control agent comprising the same as active ingredients
JP2002363164A (ja) * 2001-04-06 2002-12-18 Mitsubishi Chemicals Corp ピラゾールカルボキサミド類、その中間体およびこれを有効成分とする有害生物防除剤
IL163711A0 (en) 2002-03-08 2005-12-18 Eisai Co Ltd Macrocyclic compounds useful as pharmaceuticals
TWI350285B (en) 2002-03-13 2011-10-11 Array Biopharma Inc N3 alkylated benzimidazole derivatives as mek inhibitors
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
US20070060589A1 (en) 2004-12-21 2007-03-15 Purandare Ashok V Inhibitors of protein arginine methyl transferases
GEP20105053B (en) 2005-04-08 2010-07-26 Pfizer Prod Inc Bicyclic [3.1.0] heteroaryl amides as type i glycine transport inhibitors
WO2006126695A1 (ja) * 2005-05-23 2006-11-30 Japan Tobacco Inc. ピラゾール化合物及びそれらピラゾール化合物を含んでなる糖尿病治療薬
EP1912636B1 (en) 2005-07-21 2014-06-25 Ardea Biosciences, Inc. N-(arylamino)-sulfonamide inhibitors of mek
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
WO2009025781A1 (en) 2007-08-16 2009-02-26 Beth Israel Deaconess Medical Center Activators of pyruvate kinase m2 and methods of treating disease
WO2009028280A1 (ja) * 2007-08-29 2009-03-05 Mitsui Chemicals, Inc. ピラゾールカルボン酸誘導体及びその製造方法、並びに殺菌剤
PE20090678A1 (es) 2007-09-12 2009-06-27 Genentech Inc Combinaciones de compuestos inhibidores de fosfoinositida 3-quinasa y agentes quimioterapeuticos y los metodos de uso
WO2009055730A1 (en) 2007-10-25 2009-04-30 Genentech, Inc. Process for making thienopyrimidine compounds
WO2010042867A2 (en) * 2008-10-09 2010-04-15 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Activators of human pyruvate kinase
US8637550B2 (en) * 2008-11-17 2014-01-28 Boehringer Ingelheim International Gmbh Heteroaryl diamide compounds useful as MMP-13 inhibitors
WO2010083246A1 (en) 2009-01-15 2010-07-22 Amgen Inc. Fluoroisoquinoline substituted thiazole compounds and methods of use
CN102448951B (zh) * 2009-04-06 2017-05-10 安吉奥斯医药品有限公司 丙酮酸激酶m2调节剂、治疗组合物和相关使用方法
CA2760929C (en) 2009-05-04 2018-01-02 Agios Pharmaceuticals, Inc. Pkm2 activators for use in the treatment of cancer
US8349832B2 (en) 2009-09-02 2013-01-08 Canthera Therapeutics Compounds and compositions for treating cancer
WO2011069298A1 (en) * 2009-12-11 2011-06-16 F. Hoffmann-La Roche Ag Novel cyclopropane indolinone derivatives
JP5902174B2 (ja) 2010-09-30 2016-04-13 ナショナル ヤン−ミン ユニバーシティ 抗癌性抽出物及び化合物
WO2012056319A1 (en) 2010-10-27 2012-05-03 Dynamix Pharmaceuticals Ltd. Sulfonamides for the modulation of pkm2
US9221792B2 (en) * 2010-12-17 2015-12-29 Agios Pharmaceuticals, Inc N-(4-(azetidine-1-carbonyl) phenyl)-(hetero-) arylsulfonamide derivatives as pyruvate kinase M2 (PMK2) modulators
ES2569712T3 (es) 2010-12-21 2016-05-12 Agios Pharmaceuticals, Inc. Activadores de PKM2 bicíclicos
TWI549947B (zh) 2010-12-29 2016-09-21 阿吉歐斯製藥公司 治療化合物及組成物
EP2497775A1 (en) 2011-03-11 2012-09-12 Ruprecht-Karls-Universität Heidelberg Ferrocene-based compounds and their use as ROS regulating prodrugs
WO2012160447A1 (en) * 2011-05-25 2012-11-29 Dynamix Pharmaceuticals Ltd. 3, 5 -diphenyl- substituted pyrazolines for the treatment of cancer, proliferative, inflammatory or autoimmune diseases
WO2013005157A1 (en) 2011-07-05 2013-01-10 Lupin Limited Sulfone derivatives and their use as pkm2 modulators for the treatment of cancer
DK2909181T3 (da) 2012-10-16 2017-11-20 Tolero Pharmaceuticals Inc PKM2-modulatorer og fremgangsmåder til anvendelse deraf
NZ707778A (en) 2012-11-08 2019-03-29 Agios Pharmaceuticals Inc Therapeutic compounds and compositions and their use as pkm2 modulators
US9447054B2 (en) 2014-01-15 2016-09-20 Korea Institute Of Radiological & Medical Sciences Anticancer supplement agent including benzo[D]oxazol derivative as effective ingredient

Also Published As

Publication number Publication date
EP2909181A2 (en) 2015-08-26
EP2909181B1 (en) 2017-08-09
JP6526767B2 (ja) 2019-06-05
JP2015536325A (ja) 2015-12-21
US20210002233A1 (en) 2021-01-07
JP2019023209A (ja) 2019-02-14
DK2909181T3 (da) 2017-11-20
EP2909181A4 (en) 2016-03-23
JP7128331B2 (ja) 2022-08-30
JP2020097631A (ja) 2020-06-25
ES2644758T3 (es) 2017-11-30
JP2021181467A (ja) 2021-11-25
WO2014062838A3 (en) 2014-10-16
US10207996B2 (en) 2019-02-19
US20200109120A1 (en) 2020-04-09
WO2014062838A2 (en) 2014-04-24
JP2020105190A (ja) 2020-07-09
US20170015631A1 (en) 2017-01-19
US10766865B2 (en) 2020-09-08
US20150344436A1 (en) 2015-12-03
US10472328B2 (en) 2019-11-12
JP2021176878A (ja) 2021-11-11
US9394257B2 (en) 2016-07-19
US20190119219A1 (en) 2019-04-25
JP2018009036A (ja) 2018-01-18

Similar Documents

Publication Publication Date Title
JP7128331B2 (ja) Ｐｋｍ２調節因子およびそれらの使用方法
JP6869947B2 (ja) 置換キナゾリン化合物ならびにそのｇ１２ｃ変異ｋｒａｓ、ｈｒａｓおよび／またはｎｒａｓタンパク質の阻害剤としての使用
CA2905993C (en) Substituted 4-amino-pyrimidinyl-2-amino-phenyl derivatives and pharmaceutical compositions thereof for use as jak2 and alk2 inhibitors
KR102744039B1 (ko) 인간 히스톤 메틸트랜스퍼라제 ｅｚｈ２ 억제제의 염 형태
JP6275153B2 (ja) ヘテロ環式グルタミナーゼ阻害剤
TWI398441B (zh) 作為ｅｒｋ抑制劑之新穎化合物
CN111770914B (zh) 作为神经激肽-1受体拮抗剂的化合物及其用途
CN101959404A (zh) 单磷酸腺苷活化蛋白激酶调节剂
KR20180129783A (ko) Ｒｓｋ 억제제로서 유용한 카르복사미드 유도체
US20240409528A1 (en) Binders of cereblon and methods of use thereof
CA2529083A1 (en) Pyrazolo[3,4-b]pyridin-6-ones as gsk-3 inhibitors
NO342001B1 (no) C-kit kinase inhibitor for anvendelse i terapeutisk behandling av gastrointestinal stromaltumor eller mastocytose.
JP7129728B2 (ja) Ｆｇｆｒ４阻害剤として使用される縮環誘導体
JP2022527451A (ja) Ｐｋｍ２モジュレーターおよびその使用方法
WO2023049691A1 (en) Cdk7 inhibitors and methods of treating cancer
JP2023551019A (ja) 重水素化２－芳香族ヘテロ環－３－オキソ－２，３－ジヒドロピリダジン－４－カルボキサミド系阻害剤及びその製造方法並びに応用
EP4488276A1 (en) Novel heterocyclic compound and pharmaceutical composition comprising same
HK40029219B (en) Compounds as neurokinin-1 receptor antagonists and uses thereof
TW200538104A (en) Phenyl derivatives for the treatment of abnormal cell growth
HK1124766B (en) A c-kit kinase inhibitor for use in the treatment of gastrointestinal stromal tumor or mastocytosis

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20161014

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20161014

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20170720

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20170727

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20171020

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20171031

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20171110

R150 Certificate of patent or registration of utility model

Ref document number: 6243918

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

S111 Request for change of ownership or part of ownership

Free format text: JAPANESE INTERMEDIATE CODE: R313111

S531 Written request for registration of change of domicile

Free format text: JAPANESE INTERMEDIATE CODE: R313531

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S533 Written request for registration of change of name

Free format text: JAPANESE INTERMEDIATE CODE: R313533

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

S531 Written request for registration of change of domicile

Free format text: JAPANESE INTERMEDIATE CODE: R313531

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250