JP2011523646A - キナーゼ阻害剤としてのリン誘導体 - Google Patents

キナーゼ阻害剤としてのリン誘導体 Download PDF

Info

Publication number
JP2011523646A
JP2011523646A JP2011510716A JP2011510716A JP2011523646A JP 2011523646 A JP2011523646 A JP 2011523646A JP 2011510716 A JP2011510716 A JP 2011510716A JP 2011510716 A JP2011510716 A JP 2011510716A JP 2011523646 A JP2011523646 A JP 2011523646A
Authority
JP
Japan
Prior art keywords
ring
compound
phenyl
compounds
general formula
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.)
Withdrawn
Application number
JP2011510716A
Other languages
English (en)
Japanese (ja)
Other versions
JP2011523646A5 (https=
Inventor
ワン、イーハン
ホワン、ウェイ−シェン
リゥ、シュアンギン
シェークスピア、ウィリアム・シー
トーマス、アール・マシュー
チー、ジーウェイ
リー、フェン
チュー、シャオチァン
コールマン、アンナ
ダルガーノ、ディビッド・シー
ロメロ、ジャン・アントワネット・シー
ツォウ、ドン
Original Assignee
アリアド・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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41340562&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JP2011523646(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by アリアド・ファーマシューティカルズ・インコーポレイテッド filed Critical アリアド・ファーマシューティカルズ・インコーポレイテッド
Publication of JP2011523646A publication Critical patent/JP2011523646A/ja
Publication of JP2011523646A5 publication Critical patent/JP2011523646A5/ja
Withdrawn legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6527Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07F9/6533Six-membered 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/58Pyridine rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509Six-membered rings
    • C07F9/650905Six-membered rings having the nitrogen atoms in the positions 1 and 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509Six-membered rings
    • C07F9/6512Six-membered rings having the nitrogen atoms in positions 1 and 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6515Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having three nitrogen atoms as the only ring hetero atoms
    • C07F9/6521Six-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6515Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having three nitrogen atoms as the only ring hetero atoms
    • C07F9/6521Six-membered rings
    • C07F9/65218Six-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic 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
    • C07F9/65583Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic 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
    • C07F9/65586Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6568Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms
    • C07F9/65685Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms the ring phosphorus atom being part of a phosphine oxide or thioxide
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/657163Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom
    • C07F9/657172Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom the ring phosphorus atom and one oxygen atom being part of a (thio)phosphinic acid ester: (X = O, S)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • C07F9/65842Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring
    • C07F9/65846Cyclic amide derivatives of acids of phosphorus, in which one nitrogen atom belongs to the ring the phosphorus atom being part of a six-membered ring which may be condensed with another ring system

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Cephalosporin Compounds (AREA)
JP2011510716A 2008-05-21 2009-05-21 キナーゼ阻害剤としてのリン誘導体 Withdrawn JP2011523646A (ja)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US12831708P 2008-05-21 2008-05-21
US61/128,317 2008-05-21
US13749008P 2008-07-31 2008-07-31
US61/137,490 2008-07-31
US18879608P 2008-08-13 2008-08-13
US61/188,796 2008-08-13
US19296408P 2008-09-23 2008-09-23
US19293808P 2008-09-23 2008-09-23
US61/192,964 2008-09-23
US61/192,938 2008-09-23
PCT/US2009/044918 WO2009143389A1 (en) 2008-05-21 2009-05-21 Phosphorous derivatives as kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2015087857A Division JP6190415B2 (ja) 2008-05-21 2015-04-22 キナーゼ阻害剤としてのリン誘導体

Publications (2)

Publication Number Publication Date
JP2011523646A true JP2011523646A (ja) 2011-08-18
JP2011523646A5 JP2011523646A5 (https=) 2012-07-05

Family

ID=41340562

Family Applications (9)

Application Number Title Priority Date Filing Date
JP2011510716A Withdrawn JP2011523646A (ja) 2008-05-21 2009-05-21 キナーゼ阻害剤としてのリン誘導体
JP2015087857A Active JP6190415B2 (ja) 2008-05-21 2015-04-22 キナーゼ阻害剤としてのリン誘導体
JP2017091616A Active JP6271064B2 (ja) 2008-05-21 2017-05-02 キナーゼ阻害剤としてのリン誘導体
JP2017248633A Active JP6483233B2 (ja) 2008-05-21 2017-12-26 キナーゼ阻害剤としてのリン誘導体
JP2019023097A Active JP6690032B2 (ja) 2008-05-21 2019-02-13 キナーゼ阻害剤としてのリン誘導体
JP2020069505A Pending JP2020125308A (ja) 2008-05-21 2020-04-08 キナーゼ阻害剤としてのリン誘導体
JP2022079291A Pending JP2022116057A (ja) 2008-05-21 2022-05-13 キナーゼ阻害剤としてのリン誘導体
JP2024074178A Pending JP2024102203A (ja) 2008-05-21 2024-05-01 キナーゼ阻害剤としてのリン誘導体
JP2025205323A Pending JP2026035717A (ja) 2008-05-21 2025-11-27 キナーゼ阻害剤としてのリン誘導体

Family Applications After (8)

Application Number Title Priority Date Filing Date
JP2015087857A Active JP6190415B2 (ja) 2008-05-21 2015-04-22 キナーゼ阻害剤としてのリン誘導体
JP2017091616A Active JP6271064B2 (ja) 2008-05-21 2017-05-02 キナーゼ阻害剤としてのリン誘導体
JP2017248633A Active JP6483233B2 (ja) 2008-05-21 2017-12-26 キナーゼ阻害剤としてのリン誘導体
JP2019023097A Active JP6690032B2 (ja) 2008-05-21 2019-02-13 キナーゼ阻害剤としてのリン誘導体
JP2020069505A Pending JP2020125308A (ja) 2008-05-21 2020-04-08 キナーゼ阻害剤としてのリン誘導体
JP2022079291A Pending JP2022116057A (ja) 2008-05-21 2022-05-13 キナーゼ阻害剤としてのリン誘導体
JP2024074178A Pending JP2024102203A (ja) 2008-05-21 2024-05-01 キナーゼ阻害剤としてのリン誘導体
JP2025205323A Pending JP2026035717A (ja) 2008-05-21 2025-11-27 キナーゼ阻害剤としてのリン誘導体

Country Status (26)

Country Link
US (5) US9012462B2 (https=)
EP (2) EP2300013B2 (https=)
JP (9) JP2011523646A (https=)
KR (3) KR101781605B1 (https=)
CN (1) CN102105150B (https=)
AU (1) AU2009248923B2 (https=)
BR (1) BRPI0908637B8 (https=)
CA (1) CA2723961C (https=)
CY (2) CY1119534T1 (https=)
DK (1) DK2300013T4 (https=)
EA (1) EA029131B1 (https=)
ES (1) ES2645689T5 (https=)
FI (2) FI2300013T4 (https=)
FR (1) FR19C1033I2 (https=)
HR (1) HRP20171534T4 (https=)
HU (2) HUE035029T2 (https=)
IL (2) IL208716B (https=)
LT (2) LT2300013T (https=)
LU (1) LUC00120I2 (https=)
MX (2) MX353308B (https=)
NL (1) NL300990I2 (https=)
NO (2) NO2300013T3 (https=)
PL (1) PL2300013T5 (https=)
PT (1) PT2300013T (https=)
SI (1) SI2300013T2 (https=)
WO (1) WO2009143389A1 (https=)

Cited By (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012528864A (ja) * 2009-06-01 2012-11-15 オーエスアイ・ファーマシューティカルズ,エルエルシー アミノピリミジン抗癌性化合物
JP2015163621A (ja) * 2008-05-21 2015-09-10 アリアド・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害剤としてのリン誘導体
JP2015535266A (ja) * 2012-11-06 2015-12-10 シャンハイ フォチョン ファーマシューティカル カンパニー リミテッド Alkキナーゼ阻害剤
JP2017516825A (ja) * 2014-05-30 2017-06-22 ベイジン・パール・バイオテクノロジー・リミテッド・ライアビリティ・カンパニー Alkキナーゼ阻害剤並びにその調製方法及び使用
JP2017518336A (ja) * 2014-06-17 2017-07-06 コリア リサーチ インスティチュート オブ ケミカル テクノロジーKorea Research Institute Of Chemical Technology ピリミジン‐2,4‐ジアミン誘導体及びそれを有効成分として含有する抗癌用医薬組成物
JP2017535538A (ja) * 2014-10-21 2017-11-30 アリアド ファーマシューティカルズ,インコーポレーテッド 5−クロロ−n4−[2−(ジメチルホスホリル)フェニル]−n2−{2−メトキシ−4−[4−(4−メチルピペラジン−1−イル)ピペリジン−1−イル]ピリミジン−2,4−ジアミンの結晶形態
JP2018514559A (ja) * 2015-04-29 2018-06-07 シアメン ユニヴァーシティー ピリミドピロール類化合物、その調製方法、医薬用組成物及びその応用
JP2018515514A (ja) * 2015-05-13 2018-06-14 アリアド ファーマシューティカルズ, インコーポレイテッド キナーゼ阻害のためのヘテロアリール化合物
JP2018536667A (ja) * 2015-11-27 2018-12-13 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッドChia Tai Tianqing Pharmaceutical Group Co., Ltd. 重水素化されたBrigatinib誘導体、かかる誘導体を含む薬学的組成物、並びにそれらの使用
JP2019535673A (ja) * 2016-10-21 2019-12-12 ニンバス ラクシュミ, インコーポレイテッド Tyk2阻害剤およびその使用
JP2020503271A (ja) * 2016-11-30 2020-01-30 アリアド ファーマシューティカルズ, インコーポレイテッド 造血前駆体キナーゼ1(hpk1)阻害剤としてのアニリノピリミジンas
JP2021506937A (ja) * 2017-12-21 2021-02-22 深▲チェン▼市塔吉瑞生物医薬有限公司Shenzhen TargetRx, Inc. キナーゼ活性を阻害するためのアリールホスフィンオキシド
JP2021506942A (ja) * 2017-12-21 2021-02-22 深▲チェン▼市塔吉瑞生物医薬有限公司Shenzhen TargetRx, Inc. キナーゼ活性を阻害するためのジアニリノピリミジン系化合物
JP2021506820A (ja) * 2017-12-13 2021-02-22 上海科技大学Shanghai Tech University Alkタンパク質分解剤及びそれらの癌療法における使用
JP2021521163A (ja) * 2018-04-09 2021-08-26 上海科技大学Shanghai Tech University 標的タンパク質分解化合物、その抗腫瘍応用、その中間体および中間体の応用
JP2022508055A (ja) * 2018-11-01 2022-01-19 サイロス ファーマシューティカルズ, インコーポレイテッド サイクリン依存性キナーゼ7(cdk7)の阻害剤
JP2022518723A (ja) * 2019-01-18 2022-03-16 ボロノイ・カンパニー・リミテッド ピロロピリジン誘導体およびタンパク質キナーゼ関連疾患の予防または治療での使用のためのその用途
JP2023507319A (ja) * 2019-12-16 2023-02-22 コリア リサーチ インスティチュート オブ ケミカル テクノロジー 新規なピリミジン誘導体及びその用途
JP2023513333A (ja) * 2020-02-14 2023-03-30 貝達薬業股▲ふん▼有限公司 キノリニル基ホスフィンオキシド化合物、並びにその組成物及び使用
JP2023532151A (ja) * 2020-07-03 2023-07-26 成都地奥九泓製薬廠 アリールリン酸化物化合物およびその使用
JP2024502174A (ja) * 2021-01-07 2024-01-17 オンタリオ・インスティテュート・フォー・キャンサー・リサーチ(オーアイシーアール) Nuakキナーゼの阻害剤としてのチエニル及びシクロアルキルアミノピリミジン化合物、その組成物及び使用
JP2024502175A (ja) * 2021-01-07 2024-01-17 オンタリオ・インスティテュート・フォー・キャンサー・リサーチ(オーアイシーアール) Nuakキナーゼの阻害剤としてのイソインドリノンアミノピリミジン化合物、その組成物及び使用
US12564638B2 (en) 2019-08-05 2026-03-03 Shanghaitech University EGFR protein degradant and anti-tumor application thereof
US12582641B2 (en) 2019-02-25 2026-03-24 Shanghaitech University Sulfur-containing compound based on glutarimide skeleton and application thereof

Families Citing this family (162)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI389893B (zh) 2007-07-06 2013-03-21 Astellas Pharma Inc 二(芳胺基)芳基化合物
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
CA2743449C (en) 2008-11-12 2016-10-18 Ariad Pharmaceuticals, Inc. Pyrazinopyrazines and derivatives as kinase inhibitors
EP2381777A4 (en) 2008-12-12 2012-08-08 Ariad Pharma Inc AZAINDOL DERIVATIVES AS KINASEHEMMER
US9908884B2 (en) 2009-05-05 2018-03-06 Dana-Farber Cancer Institute, Inc. EGFR inhibitors and methods of treating disorders
LT3009428T (lt) 2009-05-08 2018-04-10 Astellas Pharma Inc. Diamino heterociklinis karboksamido junginys
ES2577829T3 (es) 2010-06-04 2016-07-19 F. Hoffmann-La Roche Ag Derivados de aminopirimidina como moduladores de la LRRK2
MX336875B (es) 2010-08-10 2016-02-04 Celgene Avilomics Res Inc Sal de besilato de un inhibidor de tirosina cinasa de bruton (btk).
WO2012051587A1 (en) * 2010-10-14 2012-04-19 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in egfr-driven cancers
WO2012061303A1 (en) 2010-11-01 2012-05-10 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof
EP2635284B1 (en) 2010-11-01 2019-12-18 Celgene CAR LLC Heterocyclic compounds and uses thereof
NO2638031T3 (https=) 2010-11-10 2018-03-10
WO2012064706A1 (en) 2010-11-10 2012-05-18 Avila Therapeutics, Inc. Mutant-selective egfr inhibitors and uses thereof
EP2646448B1 (en) 2010-11-29 2017-08-30 OSI Pharmaceuticals, LLC Macrocyclic kinase inhibitors
BR112013015000A2 (pt) * 2010-12-17 2016-08-09 Novartis Ag formas cristalinas de 5-cloron2-(2-isopropóxi-5-metil-4-piperidin-4-il-fenil)-n4-[2-(propano-2-sulfonil)-fenil]-pirimidina-2,4-diamina
US20130324532A1 (en) 2011-02-17 2013-12-05 Cancer Therapeutics Crc Pty Limited Fak inhibitors
US9174946B2 (en) 2011-02-17 2015-11-03 Cancer Therapeutics Crc Pty Ltd Selective FAK inhibitors
US8951993B2 (en) 2011-02-24 2015-02-10 Jiangsu Hansoh Pharmaceutical Co., Ltd. Phosphorus containing compounds as protein kinase inhibitors
US9139534B2 (en) 2011-04-22 2015-09-22 Signal Pharmaceuticals, Llc Substituted diaminocarboxamide and diaminocarbonitrile pyrimidines, compositions thereof, and methods of treatment therewith
EP2704572B1 (en) * 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
TWI577693B (zh) * 2011-05-31 2017-04-11 江蘇康緣藥業股份有限公司 聚(adp-核糖)聚合酶之三環抑制劑
EP3812387A1 (en) 2011-07-21 2021-04-28 Sumitomo Dainippon Pharma Oncology, Inc. Heterocyclic protein kinase inhibitors
US9364476B2 (en) 2011-10-28 2016-06-14 Celgene Avilomics Research, Inc. Methods of treating a Bruton's Tyrosine Kinase disease or disorder
US9464089B2 (en) 2012-01-13 2016-10-11 Acea Biosciences Inc. Heterocyclic compounds and uses thereof
US9586965B2 (en) 2012-01-13 2017-03-07 Acea Biosciences Inc. Pyrrolo[2,3-d]pyrimidine compounds as inhibitors of protein kinases
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
WO2013106792A1 (en) 2012-01-13 2013-07-18 Acea Biosciences Inc. Heterocyclic compounds and uses as anticancer agents.
BR112014022790B1 (pt) 2012-03-15 2022-04-19 Celgene Car Llc Sais de um inibidor de quinase de receptor de fator do crescimento epidermal, composição farmacêutica e usos do mesmo
CA2866852C (en) 2012-03-15 2020-12-29 Celgene Avilomics Research, Inc. Solid forms of an epidermal growth factor receptor kinase inhibitor
WO2013169401A1 (en) 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
CN103420902A (zh) * 2012-05-18 2013-12-04 苏州爱斯鹏药物研发有限责任公司 一种2-氯-4-碘-5-甲基吡啶的制备方法
JO3300B1 (ar) 2012-06-06 2018-09-16 Novartis Ag مركبات وتركيبات لتعديل نشاط egfr
RU2509770C2 (ru) * 2012-06-22 2014-03-20 Общество с ограниченной ответственностью "Молекулярные Технологии" Новые химические соединения производные 2,4-диамино-1,3,5-триазина для профилактики и лечения заболеваний человека и животных
KR101446742B1 (ko) 2012-08-10 2014-10-01 한국화학연구원 N2,n4-비스(4-(피페라진-1-일)페닐)피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
US9126950B2 (en) 2012-12-21 2015-09-08 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
MX2015009952A (es) 2013-02-08 2015-10-05 Celgene Avilomics Res Inc Inhibidores de cinasas reguladas por señales extracelulares (erk) y sus usos.
TW201522337A (zh) 2013-03-12 2015-06-16 Arqule Inc 經取代之三環吡唑並-嘧啶化合物類
MX394360B (es) * 2013-03-14 2025-03-24 Sumitomo Pharma Oncology Inc Inhibidores de jak2 y alk2 y metodos para su uso.
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
CN103242341B (zh) * 2013-04-19 2015-12-09 中国科学院广州生物医药与健康研究院 噻吩并2,4取代嘧啶类化合物及其药物组合物与应用
WO2014183520A1 (zh) * 2013-05-17 2014-11-20 上海恒瑞医药有限公司 吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用
KR102173433B1 (ko) 2013-07-11 2020-11-04 에이시아 바이오사이언시스 인코포레이티드. 키나아제 억제제로써의 피리미딘 유도체
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
KR101744033B1 (ko) 2013-10-16 2017-06-07 후지필름 가부시키가이샤 함질소 복소환 화합물의 염 또는 그 결정, 의약 조성물 및 flt3 저해제
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
NZ715903A (en) 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
KR101656382B1 (ko) 2014-02-28 2016-09-09 한국화학연구원 피리미딘-2,4-디아민 유도체 및 이를 유효성분으로 함유하는 항암용 약학적 조성물
AU2015283850B2 (en) 2014-07-03 2020-06-04 Board Of Regents, University Of Texas System GLS1 inhibitors for treating disease
WO2016004413A2 (en) * 2014-07-03 2016-01-07 Board Of Regents, University Of Texas System Gls1 inhibitors for treating disease
CN105330698B (zh) * 2014-07-04 2019-05-28 齐鲁制药有限公司 螺环芳基磷氧化物和硫化物
JP6487527B2 (ja) 2014-07-04 2019-03-20 チル ファーマシューティカル カンパニー リミテッド スピロ環アリールリン酸化物及びアリールリン硫化物(spirocyclic aryl phosphorus oxide and aryl phosphorus sulfide)
CN106661064B (zh) * 2014-08-07 2019-10-15 江苏豪森药业集团有限公司 一种抗癌化合物的新晶型及其制备方法和用途
CN105330697B (zh) * 2014-08-07 2019-05-28 江苏豪森药业集团有限公司 一种抗癌化合物的晶型及其制备方法和用途
WO2016019910A1 (zh) * 2014-08-07 2016-02-11 江苏豪森药业股份有限公司 一种抗癌化合物的晶型及其制备方法和用途
EP3179858B1 (en) 2014-08-13 2019-05-15 Celgene Car Llc Forms and compositions of an erk inhibitor
EP3195866B1 (en) 2014-08-22 2020-11-18 FUJIFILM Corporation Pharmaceutical composition for treating flt3 mutation-positive cancer, mutant flt3 inhibitor and uses thereof
KR101633722B1 (ko) 2014-10-08 2016-06-28 한국화학연구원 4-(1-퍼롤-3,4-디카르복시아미드)피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
CN107108524A (zh) 2014-12-16 2017-08-29 西格诺药品有限公司 2‑(叔丁基氨基)‑4‑((1r,3r,4r)‑3‑羟基‑4‑甲基环己基氨基)‑嘧啶‑5‑甲酰胺的配制物
US9513297B2 (en) 2014-12-16 2016-12-06 Signal Pharmaceuticals, Llc Methods for measurement of inhibition of c-Jun N-terminal kinase in skin
EP3250557B1 (en) 2015-01-29 2024-11-20 Signal Pharmaceuticals, LLC Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
CN105985317B (zh) * 2015-02-12 2018-09-18 正大天晴药业集团股份有限公司 一种色瑞替尼的制备方法及其中间体
KR101772134B1 (ko) 2015-04-14 2017-08-29 한국화학연구원 N2-(2-메톡시페닐)피리미딘 유도체, 이의 제조 방법 및 이를 유효 성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
CN106146468B (zh) * 2015-04-17 2020-12-01 杭州雷索药业有限公司 吡啶酮类蛋白激酶抑制剂
KR101653571B1 (ko) 2015-04-22 2016-09-05 한국화학연구원 4-(2-아미노-테트라하이드로나프탈렌닐)피리미딘 유도체, 이의 제조 방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
CN104892526A (zh) * 2015-06-17 2015-09-09 药源药物化学(上海)有限公司 一种2,5-二氯-n-(2-(异丙基磺酰基)苯基)嘧啶-4-胺的制备方法
ES2794868T3 (es) 2015-06-30 2020-11-19 Univ Texas Inhibidores de GLS1 para el tratamiento de enfermedades
CN106336398A (zh) * 2015-07-06 2017-01-18 杭州雷索药业有限公司 2‑饱和环基取代的苯胺类蛋白激酶抑制剂
WO2017009751A1 (en) 2015-07-15 2017-01-19 Pfizer Inc. Pyrimidine derivatives
JP6412471B2 (ja) 2015-07-15 2018-10-24 富士フイルム株式会社 含窒素複素環化合物の製造方法およびその中間体
CN107922287B (zh) 2015-07-24 2021-04-09 细胞基因公司 合成(1r,2r,5r)-5-氨基-2-甲基环己醇盐酸盐的方法和其中可用的中间体
CN105061506B (zh) * 2015-07-27 2017-08-29 苏州明锐医药科技有限公司 抗肿瘤药物ap26113的制备方法
CN106478700B (zh) * 2015-08-26 2020-12-29 杭州雷索药业有限公司 硼基取代的苯胺类蛋白激酶抑制剂
JP6889494B2 (ja) 2015-10-09 2021-06-18 エイシア セラピューティクス, インコーポレイテッド ピロロピリミジンキナーゼ阻害剤の薬学的塩、物理的形態、および組成物、ならびにそれらを作製する方法
CN106699810A (zh) * 2015-11-17 2017-05-24 清华大学 一种含氮杂环化合物及其制备方法与在抑制激酶活性中的应用
RU2606951C1 (ru) * 2015-11-19 2017-01-10 Закрытое акционерное общество "Р-Фарм" (ЗАО "Р-Фарм") Дихлорацетаты замещенных N4-[2-(диметилфосфорил)фенил]-N2-(2-метокси-4-пиперидин-1-илфенил)-5-хлорпиримидин-2,4-диаминов в качестве модуляторов ALK и EGFR, предназначенных для лечения рака
CN105294759B (zh) * 2015-12-02 2018-01-19 苏州东南药业股份有限公司 一种抗肿瘤药物的制备方法
CN113912648A (zh) * 2015-12-02 2022-01-11 深圳市塔吉瑞生物医药有限公司 一种二氨基嘧啶化合物及包含该化合物的组合物
JP6976248B2 (ja) 2015-12-22 2021-12-08 ボード オブ リージェンツ、ザ ユニバーシテイ オブ テキサス システム (r)−1−(4−(6−(2−(4−(3,3−ジフルオロシクロブトキシ)−6−メチルピリジン−2−イル)アセトアミド)ピリダジン−3−イル)−2−フルオロブチル)−n−メチル−1h−1,2,3−トリアゾール−4−カルボキサミドの塩形態および多形体
CN109071512A (zh) * 2016-02-03 2018-12-21 重庆复创医药研究有限公司 作为激酶抑制剂的含磷化合物
US10813933B2 (en) * 2016-05-17 2020-10-27 Japanese Foundation For Cancer Research Therapeutic agent for lung cancer that has acquired EGFR-TKI resistance
CN106220608B (zh) 2016-07-25 2018-11-27 安润医药科技(苏州)有限公司 二苯氨基嘧啶及三嗪化合物、其药用组合物及用途
CN107698603B (zh) 2016-08-09 2022-04-08 南京红云生物科技有限公司 噻吩并嘧啶类化合物、其制备方法、药用组合物及其应用
US10544129B2 (en) 2016-10-25 2020-01-28 Crystal Pharmatech Co., Ltd. Crystalline forms of AP26113, and preparation method thereof
WO2018108064A1 (zh) * 2016-12-13 2018-06-21 南京明德新药研发股份有限公司 作为第四代egfr激酶抑制剂的螺环芳基磷氧化合物
AR110351A1 (es) * 2016-12-13 2019-03-20 Bristol Myers Squibb Co COMPUESTOS DE HETEROARILO SUSTITUIDOS CON FOSFINÓXIDO ALQUILAMIDA COMO MODULADORES DE RESPUESTAS DE IL-12, IL-23 Y/O IFNa
EP3592338A1 (en) * 2017-03-08 2020-01-15 ARIAD Pharmaceuticals, Inc. Pharmaceutical formulations comprising 5-chloro-n4
AU2017408099A1 (en) 2017-04-07 2019-11-07 ACEA Therapeutics, Inc. Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same
JOP20190281A1 (ar) 2017-06-13 2019-12-02 Korea Res Inst Chemical Tech مشتق n2، n4 ثنائي فينيل بيريميدين -2، 4- ثنائي أمين، وطريقة لتحضيره، وتركيبة صيدلانية تحتوي على المشتق بوصفه مكون فعال للوقاية من السرطان أو علاجه
RU2020112558A (ru) 2017-10-18 2021-11-18 Боард Оф Регентс, Зе Юниверсити Оф Тексас Систем Терапия на основе ингибитора глутаминазы
KR101992621B1 (ko) 2017-12-07 2019-09-27 주식회사 온코빅스 암세포 성장 억제 효과를 나타내는 신규한 피리미딘 유도체 및 그를 포함하는 약제학적 조성물
WO2019112344A1 (ko) 2017-12-07 2019-06-13 주식회사 온코빅스 암세포 성장 억제 효과를 나타내는 신규한 피리미딘 유도체 및 그를 포함하는 약제학적 조성물
US11918592B2 (en) 2018-01-16 2024-03-05 Syros Pharmaceuticals, Inc. Inhibitors of cyclin dependent kinase 7 (CDK7)
AU2019209470A1 (en) 2018-01-16 2020-08-13 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
WO2019148789A1 (zh) * 2018-02-02 2019-08-08 苏州科睿思制药有限公司 布格替尼的晶型及其制备方法
WO2019154091A1 (zh) * 2018-02-07 2019-08-15 深圳市塔吉瑞生物医药有限公司 取代的二氨基嘧啶化合物
US20210046096A1 (en) 2018-02-13 2021-02-18 Sandoz Ag Pharmaceutical Composition of Brigatinib
WO2019182936A1 (en) 2018-03-19 2019-09-26 Ariad Pharmaceuticals, Inc. Methods of treating cancer in pediatric patients
CN110305161A (zh) * 2018-03-20 2019-10-08 暨南大学 2-氨基嘧啶类化合物及其应用
JP2021521170A (ja) 2018-04-13 2021-08-26 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 骨髄増殖性新生物およびがんに関連する線維症の処置のためのpimキナーゼ阻害剤
CN110467638A (zh) * 2018-05-09 2019-11-19 北京赛特明强医药科技有限公司 一种含有间氯苯胺类取代基的双氨基氯代嘧啶类化合物、制备方法及其应用
CN110467637B (zh) * 2018-05-09 2022-02-18 北京赛特明强医药科技有限公司 一种含有氧化膦类取代苯胺的双氨基氯代嘧啶类化合物、制备方法及其应用
CN111836819A (zh) * 2018-05-24 2020-10-27 北京赛特明强医药科技有限公司 一种含有芳胺基取代的吡咯并嘧啶类化合物、制备方法及其应用
CN110526941A (zh) * 2018-05-24 2019-12-03 北京赛特明强医药科技有限公司 一种含有间氯苯胺类取代基的吡咯并嘧啶类化合物、制备方法及其应用
AU2019310590A1 (en) 2018-07-26 2021-01-14 Sumitomo Pharma Oncology, Inc. Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same
CN109053693B (zh) * 2018-09-20 2021-02-05 顺毅股份有限公司 哒嗪胺类化合物的制备及其应用
JP2022508751A (ja) * 2018-10-15 2022-01-19 ゲロ ディスカバリー リミテッド ライアビリティ カンパニー Pfkfb3阻害剤とその使用
WO2020088390A1 (zh) * 2018-10-29 2020-05-07 江苏先声药业有限公司 作为第四代egfr抑制剂的嘧啶吡唑类化合物
WO2020099483A1 (en) 2018-11-15 2020-05-22 Sandoz Ag Crystalline forms of brigatinib
US20220040324A1 (en) 2018-12-21 2022-02-10 Daiichi Sankyo Company, Limited Combination of antibody-drug conjugate and kinase inhibitor
KR20260008165A (ko) 2019-02-12 2026-01-15 스미토모 파마 아메리카, 인크. 헤테로시클릭 단백질 키나제 억제제를 포함하는 제제
CN113939518B (zh) * 2019-03-15 2025-02-07 杭州英创医药科技有限公司 作为激酶抑制剂的稠合三环化合物
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
CN111825719A (zh) * 2019-04-15 2020-10-27 北京赛特明强医药科技有限公司 一种含有芳胺基取代的吡咯并嘧啶类化合物、制备方法及其应用
CN111848677B (zh) * 2019-04-29 2023-03-17 浙江同源康医药股份有限公司 一种alk激酶抑制剂化合物的晶型、制备方法及应用
WO2020245208A1 (en) 2019-06-04 2020-12-10 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of cd9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis
CN112047978A (zh) * 2019-06-05 2020-12-08 北京赛思源生物医药技术有限公司 5-氯-n4-[2-(二甲基磷酰基)苯基]-n2-{2-甲氧基-4-[4-(4-甲基哌嗪-1-基)哌啶-1-基]苯基}嘧啶-2,4-二胺新晶型
EP3994132A1 (en) 2019-07-03 2022-05-11 Sumitomo Dainippon Pharma Oncology, Inc. Tyrosine kinase non-receptor 1 (tnk1) inhibitors and uses thereof
US12428395B2 (en) 2019-08-01 2025-09-30 Sperogenix Therapeutics Limited Heterocyclic compounds as kinase inhibitor and uses thereof
US20230133169A1 (en) * 2019-10-17 2023-05-04 Betta Pharmaceuticals Co., Ltd Egfr inhibitor, composition, and method for preparation thereof
CN110713497A (zh) * 2019-10-30 2020-01-21 成都海杰亚医药科技有限公司 一种Brigatinib的中间体2-氨基苯基二甲基氧化膦制备方法
KR102168179B1 (ko) 2019-10-31 2020-10-20 주식회사 온코빅스 암세포 성장 억제 효과를 나타내는 신규한 헤테로 고리 치환 피리미딘 유도체 및 그를 포함하는 약제학적 조성물
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
CN114728932B (zh) * 2019-11-29 2024-11-29 江苏先声药业有限公司 作为egfr激酶抑制剂的多芳基化合物
AU2020406824A1 (en) * 2019-12-16 2022-08-11 Korea Research Institute Of Chemical Technology Novel pyrimidine derivative and use thereof
BR112022011857A2 (pt) 2019-12-16 2022-09-06 Oncobix Co Ltd Derivado de pirimidina substituído por deutério e composição farmacêutica compreendendo o mesmo
CN111138492B (zh) * 2020-01-06 2022-08-02 沈阳药科大学 Alk抑制剂布格替尼的制备方法
CN114787154A (zh) * 2020-01-19 2022-07-22 苏州科睿思制药有限公司 一种Deucravacitinib的晶型及其制备方法和用途
CN111620852B (zh) * 2020-01-19 2023-05-09 镇江植生源农业科技有限公司 一种5-氯-嘧啶-2,4-二胺类化合物及其制备方法和应用
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
TW202204339A (zh) 2020-03-31 2022-02-01 美商施萬生物製藥研發 Ip有限責任公司 經取代的嘧啶及使用方法
CN112225703B (zh) * 2020-09-28 2022-03-11 广州智睿医药科技有限公司 一种治疗或预防与lrrk2激酶或异常lrrk2突变激酶活性相关疾病的药物
KR20220081631A (ko) 2020-12-09 2022-06-16 보로노이 주식회사 염증성 질환의 예방 및/또는 치료를 위한 피롤로-피리딘 유도체 화합물의 신규 용도
EP4294806A1 (en) 2021-02-19 2023-12-27 Sudo Biosciences Limited Tyk2 inhibitors and uses thereof
CA3208361A1 (en) 2021-02-19 2022-08-25 Anjali Pandey Tyk2 inhibitors and uses thereof
AU2022222470A1 (en) 2021-02-19 2023-09-21 Sudo Biosciences Limited Tyk2 inhibitors and uses thereof
WO2022199589A1 (zh) * 2021-03-23 2022-09-29 南京明德新药研发有限公司 嘧啶衍生物
EP4074317A1 (en) 2021-04-14 2022-10-19 Bayer AG Phosphorus derivatives as novel sos1 inhibitors
EP4330251A4 (en) * 2021-04-30 2025-03-05 BeiGene Switzerland GmbH EGFR DEGRADING AGENTS AND METHODS OF USE THEREOF
WO2022253081A1 (zh) * 2021-06-03 2022-12-08 希格生科(深圳)有限公司 氧化膦衍生物及其制备方法和应用
CN117500813A (zh) * 2021-06-17 2024-02-02 微境生物医药科技(上海)有限公司 芳基氧膦类化合物
CN115716850B (zh) * 2021-08-27 2024-12-13 成都地奥九泓制药厂 芳基磷氧化合物的晶型、制备方法及用途
CN117043151A (zh) * 2021-12-13 2023-11-10 希格生科(深圳)有限公司 嘧啶或吡啶类衍生物及其医药用途
WO2023204822A1 (en) * 2022-04-22 2023-10-26 Vivace Therapeutics, Inc. Phenyl phosphine oxide compounds and methods of use thereof
CN115260234A (zh) * 2022-07-01 2022-11-01 江苏医药职业学院 一种2-氨基-4-氨基芳基磷氧基嘧啶化合物及其制备方法与应用
CN117045664A (zh) * 2022-08-04 2023-11-14 中国人民解放军陆军特色医学中心 布格替尼作为st3gal4抑制剂的新应用
CN115448906B (zh) * 2022-09-26 2024-04-02 深圳大学 一种2-苯胺基嘧啶类衍生物及其制备方法与应用
EP4602049A1 (en) 2022-10-13 2025-08-20 Bayer Aktiengesellschaft Sos1 inhibitors
IL320456A (en) * 2022-10-27 2025-06-01 Suzhou Genhouse Bio Co Ltd Phosphorus-containing compound, pharmaceutical composition and use thereof
CN120302975A (zh) 2022-10-31 2025-07-11 住友制药美国公司 治疗骨髓增生性肿瘤的pim1抑制剂
CN116870016B (zh) * 2022-12-01 2024-05-28 希格生科(深圳)有限公司 杂芳环化合物及其医药用途
CN116768885B (zh) * 2023-03-14 2026-03-24 浙江大学 N2-取代双环-2-氨基嘧啶类衍生物、其制备方法及医药用途
CN119019454A (zh) * 2023-05-23 2024-11-26 广州智睿医药科技有限公司 一种杂芳基衍生物的制备及用途
WO2024249831A2 (en) * 2023-06-02 2024-12-05 Unogen Biotech Ltd. Triple kinase inhibitors
EP4719394A2 (en) * 2023-06-02 2026-04-08 Atomwise Inc. Inhibitors of tyk2
AU2024287547A1 (en) 2023-07-07 2026-01-22 Viridian Therapeutics, Inc. Methods of treating chronic thyroid eye disease
WO2025073765A1 (en) 2023-10-03 2025-04-10 Institut National de la Santé et de la Recherche Médicale Methods of prognosis and treatment of patients suffering from melanoma
US20260048051A1 (en) * 2024-06-03 2026-02-19 Atomwise Inc. Treatment of inflammatory bowel disease
CN121319053A (zh) * 2024-07-10 2026-01-13 中国科学院基础医学与肿瘤研究所(筹) 一类带有二乙烯基磷酰基的2-氨基嘧啶类化合物及其应用
CN119143806B (zh) * 2024-11-19 2025-03-11 四川大学华西医院 一种靶向egfr突变的二甲基氧膦取代的苯胺嘧啶衍生物、其制备方法、用途及其制成的药物

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH1160573A (ja) * 1997-08-22 1999-03-02 Nippon Kayaku Co Ltd トリアジン誘導体及びテロメラーゼ阻害剤
US20040242611A1 (en) * 2001-06-21 2004-12-02 Metcalf Chester A. Novel phenylamino-pyrimidines and uses thereof
WO2006078846A1 (en) * 2005-01-19 2006-07-27 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
JP2006524487A (ja) * 2002-04-26 2006-11-02 ギリアード サイエンシーズ, インコーポレイテッド 抗hiv治療化合物を同定するための方法および組成物
WO2007006926A2 (fr) * 2005-07-11 2007-01-18 Sanofi-Aventis Nouveaux derives de 2,4-dianilinopyrimidines, leur preparation, a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk
JP2007502260A (ja) * 2003-08-15 2007-02-08 ノバルティス アクチエンゲゼルシャフト 新生物疾患、炎症および免疫障害の処置に有用な2,4−ピリミジンジアミン
JP2007537234A (ja) * 2004-05-14 2007-12-20 ファイザー・プロダクツ・インク 異常な細胞増殖を処置するためのピリミジン誘導体

Family Cites Families (276)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1129797A (en) 1966-03-31 1968-10-09 Ici Ltd Phosphorus-containing pyrimidine derivatives and biologically active compositions containing them
US4736866B1 (en) 1984-06-22 1988-04-12 Transgenic non-human mammals
EP0387923B1 (en) 1986-04-17 1994-02-16 Zeneca Limited Fungicides
US4966622A (en) 1988-04-12 1990-10-30 Ciba-Geigy Corporation N-phenyl-N-pyrimidin-2-ylureas
GB8828222D0 (en) 1988-12-02 1989-01-05 Ici Plc Reactive dyes
GB8903019D0 (en) 1989-02-10 1989-03-30 Ici Plc Fungicides
US5175383A (en) 1989-02-17 1992-12-29 President And Fellows Of Harvard College Animal model for benign prostatic disease
GB9016584D0 (en) 1990-07-27 1990-09-12 Ici Plc Fungicides
DE69129611T2 (de) 1990-08-20 1998-12-17 Eisai Co., Ltd., Tokio/Tokyo Sulfonamid-Derivate
GB9220964D0 (en) 1991-11-15 1992-11-18 Ici Plc Anionic compounds
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
TW225528B (https=) 1992-04-03 1994-06-21 Ciba Geigy Ag
WO1995009847A1 (en) 1993-10-01 1995-04-13 Ciba-Geigy Ag Pyrimidineamine derivatives and processes for the preparation thereof
BR9407799A (pt) 1993-10-12 1997-05-06 Du Pont Merck Pharma Composição de matéria método de tratamento e composição farmaceutica
DE69630214T2 (de) 1995-03-10 2004-07-15 Berlex Laboratories, Inc., Richmond Benzamidin-derivate, deren herstellung und deren verwendung als anti-koagulantien
US5728201A (en) 1995-09-14 1998-03-17 Canon Kabushiki Kaisha Ink, and ink-jet recording method and instruments using the same
GB9519197D0 (en) 1995-09-20 1995-11-22 Affinity Chromatography Ltd Novel affinity ligands and their use
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
WO1997020822A1 (en) 1995-12-01 1997-06-12 Novartis Ag Quinazolin-2,4-diazirines as npy receptor antagonist
GB9608771D0 (en) 1996-04-27 1996-07-03 Agrevo Uk Ltd Pyrimethanil salts
JP3106966B2 (ja) 1996-07-17 2000-11-06 富士ゼロックス株式会社 インクジェット記録用インク及びインクジェット記録方法
JPH1060338A (ja) 1996-08-21 1998-03-03 Fuji Xerox Co Ltd インクジェット記録用インク及びインクジェット記録方法
EP0929547B1 (en) 1996-09-12 2002-11-27 Schering Aktiengesellschaft Benzamidine derivatives substituted by cyclic amino acid or cycl ic hydroxy acid derivatives and their use as anti-coagulants
US6008234A (en) 1996-09-12 1999-12-28 Berlex Laboratories, Inc. Benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives and their use as anti-coagulants
US6004985A (en) 1996-10-09 1999-12-21 Berlex Laboratories, Inc. Thio acid derived monocylic N-heterocyclics as anticoagulants
CO4940418A1 (es) 1997-07-18 2000-07-24 Novartis Ag Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso
US6573044B1 (en) 1997-08-07 2003-06-03 The Regents Of The University Of California Methods of using chemical libraries to search for new kinase inhibitors
EP1054004B1 (en) 1997-12-15 2008-07-16 Astellas Pharma Inc. Novel pyrimidine-5-carboxamide derivatives
US6562833B1 (en) 1998-06-10 2003-05-13 Basf Aktiengesellschaft Use of 2-(n-phenylamino)pyrimidines as fungicides, and novel 2-(n-phenylamino) pyrimidines
AU5648599A (en) 1998-09-11 2000-04-03 Kyorin Pharmaceutical Co. Ltd. Phosphonic ester derivatives and process for producing the same
SK287270B6 (sk) 1998-11-10 2010-05-07 Janssen Pharmaceutica N. V. Derivát pyrimidínu
US6576631B1 (en) 1998-11-17 2003-06-10 Kumiai Chemical Industry Co., Ltd. Pyrimidinylbenzimidazole and triazinylbenzimidazole derivatives and agricultural/horticultural bactericides
US6262088B1 (en) 1998-11-19 2001-07-17 Berlex Laboratories, Inc. Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants
US6127376A (en) 1998-12-04 2000-10-03 Berlex Laboratories, Inc. Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
AU2871900A (en) 1999-02-04 2000-08-25 Millennium Pharmaceuticals, Inc. G-protein coupled heptahelical receptor binding compounds and methods of use thereof
GB9910807D0 (en) 1999-05-10 1999-07-07 Prometic Biosciences Limited Novel detoxification agents and their use
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
GB9918035D0 (en) 1999-07-30 1999-09-29 Novartis Ag Organic compounds
MXPA02003436A (es) 1999-10-07 2002-08-20 Amgen Inc Inhibidores de triazina cinasa.
ITMI992711A1 (it) 1999-12-27 2001-06-27 Novartis Ag Composti organici
AU3704101A (en) * 2000-02-17 2001-08-27 Amgen Inc Kinase inhibitors
GB0004888D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7087608B2 (en) 2000-03-03 2006-08-08 Robert Charles Atkins Use of PDGF receptor tyrosine kinase inhibitors for the treatment of diabetic nephropathy
US6525051B2 (en) 2000-03-27 2003-02-25 Schering Aktiengesellschaft N-heterocyclic derivatives as NOS inhibitors
AU782948B2 (en) 2000-05-08 2005-09-15 Janssen Pharmaceutica N.V. Prodrugs of HIV replication inhibiting pyrimidines
AU783981C (en) 2000-05-08 2007-05-03 Janssen Pharmaceutica N.V. HIV replication inhibitors
WO2002000024A1 (en) 2000-06-30 2002-01-03 The Regents Of The University Of California New strategy for leukemia therapy
GB0016877D0 (en) 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
GB0022438D0 (en) 2000-09-13 2000-11-01 Novartis Ag Organic Compounds
WO2002022605A1 (en) 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CN1243794C (zh) 2000-12-05 2006-03-01 克莱里安特财务(Bvi)有限公司 三色染色法
BR0116452A (pt) 2000-12-21 2003-09-30 Glaxo Group Ltd Composto, composição farmacêutica, uso de um composto
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
WO2002096933A1 (en) 2001-05-30 2002-12-05 Novartis Ag 2-{[n-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl]-amino}-alkylboronic acid derivatives
CA2450769A1 (en) 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
US7132427B2 (en) 2001-06-21 2006-11-07 Ariad Pharmaceuticals, Inc. Quinazolines and uses thereof
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
WO2003023010A2 (en) 2001-09-07 2003-03-20 Irm Llc Sensory neuron receptors
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
US20060009642A1 (en) 2001-10-12 2006-01-12 Irm Llc, A Delaware Limited Liability Company Methods for the synthesis of substituted purines
EP1578722A4 (en) 2001-10-12 2006-09-06 Irm Llc KINASEINHIBITOR SCAFFOLD AND METHOD FOR THE PRODUCTION THEREOF
US6949644B2 (en) 2001-10-12 2005-09-27 Irm Llc Methods for the synthesis of substituted purines
US6770652B2 (en) * 2001-10-18 2004-08-03 Duquesne University Of The Holy Ghost Multiple acting anti-angiogenic and cytotoxic compounds and methods for using the same
HUP0402106A3 (en) 2001-11-01 2009-07-28 Janssen Pharmaceutica Nv Heteroaryl amines as glycogen synthase kinase 3 beta inhibitors, process for their preparation and pharmaceutical compositions containing them
IL162838A0 (en) 2002-01-04 2005-11-20 Univ Rockefeller Compositions and methods for prevention and treatment peptide-of amyloid- related disorders
PT1478648E (pt) 2002-02-01 2014-07-15 Ariad Pharma Inc Compostos contendo fósforo e suas utilizações
AU2003209077A1 (en) 2002-02-08 2003-09-02 Smithkline Beecham Corporation Pyrimidine compounds
GB0206215D0 (en) 2002-03-15 2002-05-01 Novartis Ag Organic compounds
US20050239054A1 (en) 2002-04-26 2005-10-27 Arimilli Murty N Method and compositions for identifying anti-HIV therapeutic compounds
US7704995B2 (en) 2002-05-03 2010-04-27 Exelixis, Inc. Protein kinase modulators and methods of use
WO2003095448A1 (en) 2002-05-06 2003-11-20 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
AR039540A1 (es) 2002-05-13 2005-02-23 Tibotec Pharm Ltd Compuestos microbicidas con contenido de pirimidina o triazina
BR0311347A (pt) 2002-05-27 2005-02-22 Novartis Ag Alcanóis bis-aromáticos
GB0217431D0 (en) 2002-07-27 2002-09-04 Astrazeneca Ab Novel compounds
HRP20050089B1 (hr) 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
WO2004018435A1 (en) 2002-08-24 2004-03-04 Astrazeneca Ab Pyrimidine derivatives as modulators of chemokine receptor activity
AU2003286876A1 (en) 2002-11-01 2004-06-07 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of jak and other protein kinases
HRP20050690A2 (en) 2003-02-07 2006-08-31 Janssen Pharmaceutica N.V. Hiv inhibiting 1,2,4-triazines
PL378134A1 (pl) 2003-02-11 2006-03-06 Irm Llc Nowe pochodne bicykliczne i kompozycje farmaceutyczne zawierające pochodne bicykliczne
CL2004000306A1 (es) 2003-02-20 2005-04-08 Tibotec Pharm Ltd Compuestos derivados de pirimidina sustituidas con indano; proceso para su preparacion; composicion farmaceutica que lo comprende; combinacion farmaceutica; y su uso para el tratamiento o profilaxis de una enfermedad infecciosa.
ES2325440T3 (es) 2003-02-20 2009-09-04 Smithkline Beecham Corporation Compuestos de pirimidina.
WO2004078682A2 (en) 2003-03-05 2004-09-16 Irm Llc Cyclic compounds and compositions as protein kinase inhibitors
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
TW200505902A (en) 2003-03-20 2005-02-16 Schering Corp Cannabinoid receptor ligands
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
US7253166B2 (en) 2003-04-22 2007-08-07 Irm Llc 6-phenyl-7H-pyrrolo[2,3-d]pyrimidine compounds that induce neuronal differentiation in embryonic stem cells
WO2004098520A2 (en) 2003-05-01 2004-11-18 Irm Llc Compounds and compositions as protein kinase inhibitors
MY150088A (en) 2003-05-19 2013-11-29 Irm Llc Immunosuppressant compounds and compositions
US7317027B2 (en) 2003-05-19 2008-01-08 Sanofi-Aventis Deutschland Gmbh Azaindole-derivatives as factor Xa inhibitors
WO2005011597A2 (en) 2003-07-29 2005-02-10 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2005012294A1 (en) 2003-07-30 2005-02-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
ATE506953T1 (de) 2003-08-07 2011-05-15 Rigel Pharmaceuticals Inc 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel
MXPA06001758A (es) 2003-08-15 2006-08-11 Irm Llc Anilino purinas sustituidas en la posicion 6 utiles como inhibidores de rtk.
US7338957B2 (en) 2003-08-28 2008-03-04 Irm Llc Compounds and compositions as protein kinase inhibitors
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
US20070105839A1 (en) 2003-09-18 2007-05-10 Patricia Imbach 2, 4-Di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
EP1670771A4 (en) 2003-09-30 2010-09-01 Irm Llc COMPOUNDS AND COMPOSITIONS INHIBITING PROTEIN-KINASES
US7569593B2 (en) 2003-10-02 2009-08-04 Irm Llc Compounds and compositions as protein kinase inhibitors
AU2004279427B2 (en) 2003-10-08 2008-07-03 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2005042773A1 (en) 2003-10-24 2005-05-12 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds
DE10349587A1 (de) 2003-10-24 2005-05-25 Merck Patent Gmbh Benzimidazolylderivate
WO2005047279A1 (en) 2003-11-10 2005-05-26 Merck Sharp & Dohme Limited Substituted nitrogen-containing six-membered amino-heterocycles as vanilloid-1 receptor antagonists for treating pain
ATE388430T1 (de) 2003-12-01 2008-03-15 Tuchenhagen Gmbh Verfahren zur zeitnahen überwachung, erfassung und übermittlung von prozessdaten
CA2545422C (en) 2003-12-03 2015-06-02 Cytopia Research Pty Ltd Tubulin inhibitors
MY141255A (en) 2003-12-11 2010-03-31 Memory Pharm Corp Phosphodiesterase 4 inhibitors, including n-substituted diarylamine analogs
WO2005063722A1 (en) 2003-12-19 2005-07-14 Rigel Pharmaceuticals, Inc. Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates
US20080227786A1 (en) 2004-01-16 2008-09-18 Ferlita Russell R Novel Crystalline Salts of a Dipeptidyl Peptidase-IV Inhibitor
GT200500008A (es) 2004-01-16 2005-08-16 Intermediarios de quinolina como inhibidores de receptores de tirosina quinasas y la sintesis de los mismos
CN1918158B (zh) 2004-02-14 2011-03-02 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
US7754714B2 (en) 2004-05-18 2010-07-13 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
EP1598343A1 (de) 2004-05-19 2005-11-23 Boehringer Ingelheim International GmbH 2-Arylaminopyrimidine als PLK Inhibitoren
RU2401265C2 (ru) 2004-06-10 2010-10-10 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназы
AU2005258266A1 (en) 2004-06-23 2006-01-05 Irm Llc Compounds and compositions as protein kinase inhibitors
GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
US7923554B2 (en) 2004-08-10 2011-04-12 Janssen Pharmaceutica N.V. HIV inhibiting 1,2,4-triazin-6-one derivatives
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
GB0419161D0 (en) 2004-08-27 2004-09-29 Novartis Ag Organic compounds
WO2006038594A1 (ja) 2004-10-04 2006-04-13 Ono Pharmaceutical Co., Ltd. N型カルシウムチャネル阻害薬
JP2008515986A (ja) 2004-10-13 2008-05-15 ワイス N−ベンゼンスルホニル置換アニリノ−ピリミジン類似物
GT200500321A (es) 2004-11-09 2006-09-04 Compuestos y composiciones como inhibidores de proteina kinase.
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
ES2325035T3 (es) 2004-12-21 2009-08-24 Smithkline Beecham Corporation Inhibidores de quinasa erbb de 2-pirimidinil pirazolopiridina.
ATE519759T1 (de) 2004-12-30 2011-08-15 Exelixis Inc Pyrimidinderivate als kinasemodulatoren und anwendungsverfahren
WO2006081172A2 (en) 2005-01-26 2006-08-03 Irm Llc Compounds and compositions as protein kinase inhibitors
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
US20080188483A1 (en) 2005-03-15 2008-08-07 Irm Llc Compounds and Compositions as Protein Kinase Inhibitors
JP2008533166A (ja) 2005-03-16 2008-08-21 ターゲジェン インコーポレーティッド ピリミジン化合物および使用法
DE102005016634A1 (de) 2005-04-12 2006-10-19 Merck Patent Gmbh Neuartige Aza-Hetercyclen als Kinase-Inhibitoren
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
US8183248B2 (en) 2005-05-13 2012-05-22 Irm Llc Substituted pyrrolo[2,3-d]pyrimidines and compositions as protein kinase inhibitors
RU2387653C2 (ru) 2005-05-16 2010-04-27 Айрм Ллк Соединения и композиции в качестве ингибиторов протеинкиназ
EP2049497A2 (en) 2005-05-19 2009-04-22 Astex Therapeutics Limited Pyrimidine derivatives as hsp90 inhibitors
WO2006128129A2 (en) 2005-05-26 2006-11-30 Synta Pharmaceuticals Corp. Method for treating cancer
US20070032493A1 (en) 2005-05-26 2007-02-08 Synta Pharmaceuticals Corp. Method for treating B cell regulated autoimmune disorders
WO2006129100A1 (en) 2005-06-03 2006-12-07 Glaxo Group Limited Novel compounds
BRPI0610876B8 (pt) 2005-06-08 2021-05-25 Rigel Pharmaceuticals Inc composto, formulação farmacêutica, e métodos de inibir uma atividade de uma jak cinase, e de inibir uma cascata de transdução de sinal em que jak3 cinase desempenha um papel
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
JP5054004B2 (ja) 2005-07-01 2012-10-24 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としてのピリミジン置換ベンゾイミダゾール誘導体
US20070032514A1 (en) 2005-07-01 2007-02-08 Zahn Stephan K 2,4-diamino-pyrimidines as aurora inhibitors
JP5255438B2 (ja) 2005-07-26 2013-08-07 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阻害薬として有用なベンズイミダゾール
CN101273023A (zh) 2005-08-02 2008-09-24 Irm责任有限公司 作为蛋白激酶抑制剂的5-取代的噻唑-2-基氨基化合物和组合物
WO2007021795A2 (en) 2005-08-09 2007-02-22 Irm Llc Compounds and compositions as protein kinase inhibitors
JP5321061B2 (ja) 2005-08-11 2013-10-23 アリアド・ファーマシューティカルズ・インコーポレイテッド 不飽和複素環誘導体
US7589101B2 (en) 2005-08-16 2009-09-15 Irm Llc Compounds and compositions as protein kinase inhibitors
JP2009511528A (ja) 2005-10-13 2009-03-19 グラクソ グループ リミテッド Syk阻害物質としてのピロロピリミジン誘導体群
US7973060B2 (en) 2005-10-13 2011-07-05 Crystalgenomics, Inc. Fab I inhibitor and process for preparing same
US8372851B2 (en) 2005-10-21 2013-02-12 Exelixis, Inc. Pyrazolo pyrimidines as casein kinase II (CK2) modulators
PT1940844E (pt) 2005-10-28 2010-01-06 Scripps Research Inst Compostos e composições como inibidores de proteína-quinase
JP5191391B2 (ja) 2005-11-01 2013-05-08 ターゲジェン インコーポレーティッド キナーゼのビ−アリールメタ−ピリミジン阻害剤
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
JP2009514876A (ja) 2005-11-03 2009-04-09 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼのための化合物および組成物
JP5103403B2 (ja) 2005-12-05 2012-12-19 スミスクライン ビーチャム コーポレーション 2−ピリミジニルピラゾロピリジンErbBキナーゼ阻害剤
US20080318989A1 (en) 2005-12-19 2008-12-25 Burdick Daniel J Pyrimidine Kinase Inhibitors
DE102005062742A1 (de) 2005-12-22 2007-06-28 Bayer Schering Pharma Ag Sulfoximin substituierte Pyrimidine, Verfahren zu deren Herstellung und ihre Verwendung als Arzneimittel
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
KR20080110998A (ko) 2006-01-30 2008-12-22 엑셀리시스, 인코포레이티드 Jak­2 조절자로서 4­아릴­2­아미노­피리미딘 또는 4­아릴­2­아미노알킬­피리미딘 및 이들을 포함하는 약제학적 조성물
KR20080092412A (ko) 2006-02-06 2008-10-15 아이알엠 엘엘씨 단백질 키나제 억제제로서의 화합물 및 조성물
TW200804364A (en) 2006-02-22 2008-01-16 Boehringer Ingelheim Int New compounds
US20070208164A1 (en) 2006-02-27 2007-09-06 Wyeth Methods of synthesizing radiolabeled 3-cyano[14C]quinolines
ES2353725T3 (es) 2006-03-30 2011-03-04 Tibotec Pharmaceuticals Pirimidinas sustituidas con 5-(hidroximetileno y aminometileno) que inhiben el vih.
CN101405283B (zh) 2006-03-30 2014-06-18 泰博特克药品有限公司 Hiv抑制性5-酰氨基取代的嘧啶类化合物
GB0608386D0 (en) 2006-04-27 2006-06-07 Senexis Ltd Compounds
US7601716B2 (en) 2006-05-01 2009-10-13 Cephalon, Inc. Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors
MX2008014618A (es) 2006-05-15 2008-11-28 Irm Llc Composiciones y metodos para inhibidores de cinasas del receptor fgf.
DE102006027156A1 (de) 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
EP2043651A2 (en) 2006-07-05 2009-04-08 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
WO2008009458A1 (en) 2006-07-21 2008-01-24 Novartis Ag 2, 4 -di (arylaminio) -pyrimidine-5-carboxamide compounds as jak kinases inhibitors
GB0614579D0 (en) 2006-07-21 2006-08-30 Black James Foundation Pyrimidine derivatives
DE102006041382A1 (de) 2006-08-29 2008-03-20 Bayer Schering Pharma Ag Carbamoyl-Sulfoximide als Proteinkinaseinhibitoren
US8314234B2 (en) 2006-09-25 2012-11-20 Janssen Pharmaceutica N.V. Bicyclic pyrimidine kinase inhibitors
WO2008045978A1 (en) 2006-10-10 2008-04-17 Rigel Pharmaceuticals, Inc. Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors
CA2598893C (en) 2006-10-11 2012-04-10 Astellas Pharma Inc. Eml4-alk fusion gene
MX337906B (es) 2006-10-19 2016-03-28 Signal Pharm Llc Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas.
JP5161233B2 (ja) 2006-10-19 2013-03-13 ライジェル ファーマシューティカルズ, インコーポレイテッド 自己免疫疾患の処置のためのjakキナーゼの阻害剤としての2,4−ピリミジンアミン誘導体
ES2555803T3 (es) 2006-10-23 2016-01-08 Cephalon, Inc. Fusión de derivados bicíclicos 2,4-diaminopirimidina como utilizar inhibidores ALK y c-Met
WO2008057280A1 (en) 2006-10-27 2008-05-15 Amgen Inc. Multi-cyclic compounds and methods of use
US7982033B2 (en) 2006-11-03 2011-07-19 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
EA017405B9 (ru) 2006-12-08 2014-05-30 АйАрЭм ЭлЭлСи Соединения и композиции в качестве ингибиторов протеинкиназы
NZ577197A (en) 2006-12-08 2011-02-25 Irm Llc Pyrimidine compounds especially 4-phenylamino-2-arylamino-pyrimidine derivatives and compositions as protein kinase inhibitors
CN101563327A (zh) 2006-12-19 2009-10-21 健泰科生物技术公司 嘧啶类激酶抑制剂
EP1939185A1 (de) 2006-12-20 2008-07-02 Bayer Schering Pharma Aktiengesellschaft Neuartige Hetaryl-Phenylendiamin-Pyrimidine als Proteinkinaseinhibitoren zur Behandlung von Krebs
CA2673965A1 (en) 2006-12-28 2008-07-10 Taisho Pharmaceutical Co., Ltd. Pyrazolopyrimidine compound
AU2007341228B2 (en) 2006-12-29 2013-04-18 Janssen Sciences Ireland Uc HIV inhibiting 5,6-substituted pyrimidines
AU2007341227C1 (en) 2006-12-29 2013-08-29 Janssen Sciences Ireland Uc HIV inhibiting 6-substituted pyrimidines
FR2911138B1 (fr) * 2007-01-05 2009-02-20 Sanofi Aventis Sa Nouveaux derives de n, n'-2,4-dianilinopyrimidines, leur preparation a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk
KR20090112732A (ko) * 2007-01-26 2009-10-28 아이알엠 엘엘씨 플라스모듐 관련 질환의 치료를 위한 키나제 억제제로서의 퓨린 화합물 및 조성물
PE20081636A1 (es) 2007-01-26 2009-01-10 Smithkline Beecham Corp Inhibidores de antranilamida para aurora quinasa
PT2114900T (pt) 2007-01-31 2019-01-17 Ym Biosciences Australia Pty Compostos à base de tiopirimidina e as suas utilizações
TW200834459A (en) 2007-02-05 2008-08-16 Huper Lab Co Ltd Video object segmentation method applied for rainy situations
DE102007010801A1 (de) 2007-03-02 2008-09-04 Bayer Cropscience Ag Diaminopyrimidine als Fungizide
EA200901133A1 (ru) 2007-03-20 2010-04-30 Смитклайн Бичем Корпорейшн Производные дианилинопиримидина как ингибиторы киназы wee1, фармацевтическая композиция и применение
EP2136635A4 (en) 2007-03-20 2011-07-27 Glaxosmithkline Llc CHEMICAL COMPOUNDS
WO2008118822A1 (en) 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
NZ579892A (en) 2007-03-30 2012-03-30 Sanofi Aventis Pyrimidine hydrazide compounds as prostaglandin D synthase inhibitors
TWI433677B (zh) 2007-06-04 2014-04-11 Avila Therapeutics Inc 雜環化合物及其用途
WO2008157575A1 (en) 2007-06-21 2008-12-24 Irm Llc Protein kinase inhibitors and methods for using thereof
TWI389893B (zh) 2007-07-06 2013-03-21 Astellas Pharma Inc 二(芳胺基)芳基化合物
CN101903357A (zh) 2007-07-17 2010-12-01 里格尔药品股份有限公司 作为pkc抑制剂的环状胺取代的嘧啶二胺
ES2424977T3 (es) 2007-08-08 2013-10-10 Glaxosmithkline Intellectual Property Development Limited Derivados de 2-[(2-{fenilamino}-1H-pirrolo[2,3-D]pirimidin-4-il)amino]benzamida como inhibidores de IGF-1R para el tratamiento del cáncer
AU2008296479A1 (en) 2007-08-28 2009-03-12 Dana Farber Cancer Institute Amino substituted pyrimidine, pyrollopyridine and pyrazolopyrimidine derivatives useful as kinase inhibitors and in treating proliferative disorders and diseases associated with angiogenesis
EA017252B1 (ru) 2007-08-28 2012-11-30 Айрм Ллк Производные 2-бифениламино-4-аминопиримидина в качестве ингибиторов киназ
US7989465B2 (en) 2007-10-19 2011-08-02 Avila Therapeutics, Inc. 4,6-disubstituted pyrimidines useful as kinase inhibitors
TWI552752B (zh) 2007-10-19 2016-10-11 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
EA019869B1 (ru) 2007-11-28 2014-06-30 Дана Фарбер Кансер Инститьют, Инк. Низкомолекулярные миристатные ингибиторы тирозинкиназы bcr-abl и способы их применения
US8461147B2 (en) 2007-12-03 2013-06-11 Boehringer Ingelheim International Gmbh Diaminopyridines for the treatment of diseases which are characterised by excessive or anomal cell proliferation
CA2710118A1 (en) 2007-12-20 2009-07-02 Cellzome Limited Sulfamides as zap-70 inhibitors
CA2710144A1 (en) 2007-12-21 2009-07-02 Avila Therapeutics, Inc. Hcv protease inhibitors and uses thereof
MX2010006736A (es) 2007-12-21 2010-10-15 Avila Therapeutics Inc Inhibidores de proteasa del virus de la hepatitis c (hcv) y usos de los mismos.
US8293705B2 (en) 2007-12-21 2012-10-23 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
US8309685B2 (en) 2007-12-21 2012-11-13 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
WO2009091476A1 (en) 2008-01-14 2009-07-23 Irm Llc Compositions and methods for treating cancers
EP2255190A4 (en) 2008-02-12 2011-05-04 Brigham & Womens Hospital FISH TEST FOR EML4-ALK FUSION IN LUNG CANCER
US20110033453A1 (en) 2008-03-05 2011-02-10 Carlos Garcia-Echeverria Use of pyrimidine derivatives for the treatment of egfr dependent diseases or diseases that have acquired resistance to agents that target egfr family members
US20110098288A1 (en) 2008-03-11 2011-04-28 Jeremy Major Sulfonamides as zap-70 inhibitors
CL2009000600A1 (es) 2008-03-20 2010-05-07 Bayer Cropscience Ag Uso de compuestos de diaminopirimidina como agentes fitosanitarios; compuestos de diaminopirimidina; su procedimiento de preparacion; agente que los contiene; procedimiento para la preparacion de dicho agente; y procedimiento para combatir plagas de animales y/u hongos dañinos patogenos de plantas.
AU2009233963B2 (en) 2008-04-07 2011-10-06 Irm Llc Compounds and compositions as kinase inhibitors
MX2010010968A (es) 2008-04-07 2010-10-26 Irm Llc Compuestos y composiciones como inhibidores de cinasa de proteina.
WO2009127642A2 (en) 2008-04-15 2009-10-22 Cellzome Limited Use of lrrk2 inhibitors for neurodegenerative diseases
WO2009127822A2 (en) 2008-04-16 2009-10-22 Biolipox Ab Bis-aryl compounds for use as medicaments
AU2009238590A1 (en) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
US20130225527A1 (en) 2008-05-21 2013-08-29 Ariad Pharmaceuticals, Inc. Phosphorus Derivatives as Kinase Inhibitors
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
MX353308B (es) * 2008-05-21 2018-01-08 Ariad Pharma Inc Derivados fosforosos como inhibidores de cinasa.
US20130225528A1 (en) 2008-05-21 2013-08-29 Ariad Pharmaceuticals, Inc. Phosphorus Derivatives as Kinase Inhibitors
CN102089278A (zh) 2008-06-11 2011-06-08 Irm责任有限公司 用于治疗疟疾的化合物和组合物
CA2727174A1 (en) 2008-06-20 2010-01-21 Jiangao Song Aryl gpr119 agonists and uses thereof
NZ603525A (en) 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
AU2009289378A1 (en) 2008-09-02 2010-03-11 Boehringer Ingelheim International Gmbh Novel benzamides, production thereof, and use thereof as medicaments
KR20110049905A (ko) 2008-09-03 2011-05-12 바이엘 크롭사이언스 아게 4-알킬-치환된 디아미노피리미딘
JP2012501654A (ja) 2008-09-05 2012-01-26 アビラ セラピューティクス, インコーポレイテッド 不可逆的インヒビターの設計のためのアルゴリズム
EP2350053B1 (en) 2008-10-17 2013-12-11 Whitehead Institute For Biomedical Research Modulators of MTOR Complexes
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
US8110578B2 (en) 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
CN101723936B (zh) 2008-10-27 2014-01-15 上海睿星基因技术有限公司 激酶抑制剂及其在药学中的用途
CA2743449C (en) 2008-11-12 2016-10-18 Ariad Pharmaceuticals, Inc. Pyrazinopyrazines and derivatives as kinase inhibitors
EP2381777A4 (en) 2008-12-12 2012-08-08 Ariad Pharma Inc AZAINDOL DERIVATIVES AS KINASEHEMMER
US8809343B2 (en) 2008-12-26 2014-08-19 Fudan University Pyrimidine derivative, preparation method and use thereof
EP3828185B1 (en) 2009-01-06 2024-11-20 Dana-Farber Cancer Institute, Inc. Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders
EP3266795A1 (en) 2009-02-12 2018-01-10 Cell Signaling Technology, Inc. Method for detecting a fig-ros fusion polynucleotide
WO2010098866A1 (en) 2009-02-27 2010-09-02 Supergen, Inc. Cyclopentathiophene/cyclohexathiophene dna methyltransferase inhibitors
US20110071158A1 (en) 2009-03-18 2011-03-24 Boehringer Ingelheim International Gmbh New compounds
WO2010111406A2 (en) 2009-03-24 2010-09-30 Myriad Pharmaceuticals, Inc. Compounds and therapeutic uses thereof
CA2757671A1 (en) 2009-04-03 2010-10-07 Cellzome Ag Methods for the identification of kinase interacting molecules and for the purification of kinase proteins
US9908884B2 (en) 2009-05-05 2018-03-06 Dana-Farber Cancer Institute, Inc. EGFR inhibitors and methods of treating disorders
US8410126B2 (en) 2009-05-29 2013-04-02 Boehringer Ingelheim International Gmbh Pyrimidine inhibitors of PKTK2
CA2763717A1 (en) 2009-06-10 2010-12-16 Cellzome Limited Pyrimidine derivatives as zap-70 inhibitors
CA2763720A1 (en) 2009-06-18 2010-12-23 Cellzome Limited Sulfonamides and sulfamides as zap-70 inhibitors
NZ713361A (en) 2009-08-17 2017-06-30 Memorial Sloan Kettering Cancer Center Heat shock protein binding compounds, compositions, and methods for making and using same
JP2013504325A (ja) 2009-09-09 2013-02-07 アビラ セラピューティクス, インコーポレイテッド Pi3キナーゼインヒビターおよびその使用
US9556426B2 (en) 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
CN102548994A (zh) 2009-09-25 2012-07-04 沃泰克斯药物股份有限公司 用于制备用作蛋白激酶抑制剂的嘧啶衍生物的方法
SG10201500511TA (en) 2009-10-26 2015-03-30 Signal Pharm Llc Methods Of Synthesis And Purification Of Heteroaryl Compounds
WO2011079231A1 (en) 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
JP2013516422A (ja) 2009-12-30 2013-05-13 アビラ セラピューティクス, インコーポレイテッド タンパク質のリガンド−指向性共有的修飾
WO2011103196A1 (en) 2010-02-17 2011-08-25 Amgen Inc. Aryl carboxamide derivatives as sodium channel inhibitors for treatment of pain
US8383793B2 (en) 2010-04-15 2013-02-26 St. Jude Children's Research Hospital Methods and compositions for the diagnosis and treatment of cancer resistant to anaplastic lymphoma kinase (ALK) kinase inhibitors
WO2011140338A1 (en) 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
JP2013526546A (ja) 2010-05-13 2013-06-24 アムジエン・インコーポレーテツド Pde10阻害剤としてのヘテロアリ−ルオキシヘテロシクリル化合物
MX342164B (es) 2010-06-23 2016-09-19 Hanmi Science Co Ltd Derivados de pirimidina fusionados novedosos para la inhibicion de la actividad de tirosina cinasa.
MX336875B (es) 2010-08-10 2016-02-04 Celgene Avilomics Res Inc Sal de besilato de un inhibidor de tirosina cinasa de bruton (btk).
WO2012022045A1 (en) 2010-08-20 2012-02-23 Hutchison Medipharma Limited Pyrrolopyrimidine compounds and uses thereof
WO2012051587A1 (en) 2010-10-14 2012-04-19 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in egfr-driven cancers
EP2635284B1 (en) 2010-11-01 2019-12-18 Celgene CAR LLC Heterocyclic compounds and uses thereof
WO2012061303A1 (en) 2010-11-01 2012-05-10 Avila Therapeutics, Inc. Heteroaryl compounds and uses thereof
WO2012064706A1 (en) 2010-11-10 2012-05-18 Avila Therapeutics, Inc. Mutant-selective egfr inhibitors and uses thereof
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
EP4119551A1 (en) 2011-07-27 2023-01-18 Astrazeneca AB 2-(2,4,5-substituted-anilino)pyrimidine compounds
EP2758402B9 (en) 2011-09-22 2016-09-14 Pfizer Inc Pyrrolopyrimidine and purine derivatives
WO2013169401A1 (en) 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH1160573A (ja) * 1997-08-22 1999-03-02 Nippon Kayaku Co Ltd トリアジン誘導体及びテロメラーゼ阻害剤
US20040242611A1 (en) * 2001-06-21 2004-12-02 Metcalf Chester A. Novel phenylamino-pyrimidines and uses thereof
JP2006524487A (ja) * 2002-04-26 2006-11-02 ギリアード サイエンシーズ, インコーポレイテッド 抗hiv治療化合物を同定するための方法および組成物
JP2007502260A (ja) * 2003-08-15 2007-02-08 ノバルティス アクチエンゲゼルシャフト 新生物疾患、炎症および免疫障害の処置に有用な2,4−ピリミジンジアミン
JP2007537234A (ja) * 2004-05-14 2007-12-20 ファイザー・プロダクツ・インク 異常な細胞増殖を処置するためのピリミジン誘導体
WO2006078846A1 (en) * 2005-01-19 2006-07-27 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
WO2007006926A2 (fr) * 2005-07-11 2007-01-18 Sanofi-Aventis Nouveaux derives de 2,4-dianilinopyrimidines, leur preparation, a titre de medicaments, compositions pharmaceutiques et notamment comme inhibiteurs de ikk

Cited By (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015163621A (ja) * 2008-05-21 2015-09-10 アリアド・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害剤としてのリン誘導体
JP2017186345A (ja) * 2008-05-21 2017-10-12 アリアド・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害剤としてのリン誘導体
JP2018065864A (ja) * 2008-05-21 2018-04-26 アリアド・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害剤としてのリン誘導体
JP2012528864A (ja) * 2009-06-01 2012-11-15 オーエスアイ・ファーマシューティカルズ,エルエルシー アミノピリミジン抗癌性化合物
JP2018119003A (ja) * 2012-11-06 2018-08-02 シャンハイ フォチョン ファーマシューティカル カンパニー リミテッド Alkキナーゼ阻害剤
JP2015535266A (ja) * 2012-11-06 2015-12-10 シャンハイ フォチョン ファーマシューティカル カンパニー リミテッド Alkキナーゼ阻害剤
JP2017516825A (ja) * 2014-05-30 2017-06-22 ベイジン・パール・バイオテクノロジー・リミテッド・ライアビリティ・カンパニー Alkキナーゼ阻害剤並びにその調製方法及び使用
JP2017518336A (ja) * 2014-06-17 2017-07-06 コリア リサーチ インスティチュート オブ ケミカル テクノロジーKorea Research Institute Of Chemical Technology ピリミジン‐2,4‐ジアミン誘導体及びそれを有効成分として含有する抗癌用医薬組成物
JP2017535538A (ja) * 2014-10-21 2017-11-30 アリアド ファーマシューティカルズ,インコーポレーテッド 5−クロロ−n4−[2−(ジメチルホスホリル)フェニル]−n2−{2−メトキシ−4−[4−(4−メチルピペラジン−1−イル)ピペリジン−1−イル]ピリミジン−2,4−ジアミンの結晶形態
JP2020063276A (ja) * 2014-10-21 2020-04-23 アリアド ファーマシューティカルズ,インコーポレーテッド 5−クロロ−n4−[2−(ジメチルホスホリル)フェニル]−n2−{2−メトキシ−4−[4−(4−メチルピペラジン−1−イル)ピペリジン−1−イル]フェニル}ピリミジン−2,4−ジアミンの結晶形態
JP2018514559A (ja) * 2015-04-29 2018-06-07 シアメン ユニヴァーシティー ピリミドピロール類化合物、その調製方法、医薬用組成物及びその応用
JP2018515514A (ja) * 2015-05-13 2018-06-14 アリアド ファーマシューティカルズ, インコーポレイテッド キナーゼ阻害のためのヘテロアリール化合物
JP2018536667A (ja) * 2015-11-27 2018-12-13 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッドChia Tai Tianqing Pharmaceutical Group Co., Ltd. 重水素化されたBrigatinib誘導体、かかる誘導体を含む薬学的組成物、並びにそれらの使用
JP2019535673A (ja) * 2016-10-21 2019-12-12 ニンバス ラクシュミ, インコーポレイテッド Tyk2阻害剤およびその使用
JP7082120B2 (ja) 2016-10-21 2022-06-07 ニンバス ラクシュミ, インコーポレイテッド Tyk2阻害剤およびその使用
JP2020503271A (ja) * 2016-11-30 2020-01-30 アリアド ファーマシューティカルズ, インコーポレイテッド 造血前駆体キナーゼ1(hpk1)阻害剤としてのアニリノピリミジンas
JP7025426B2 (ja) 2016-11-30 2022-02-24 アリアド ファーマシューティカルズ, インコーポレイテッド 造血前駆体キナーゼ1(hpk1)阻害剤としてのアニリノピリミジンas
US11771709B2 (en) 2017-12-13 2023-10-03 Shanghaitech University ALK protein degradation agent and anti-tumor application thereof
JP2021506820A (ja) * 2017-12-13 2021-02-22 上海科技大学Shanghai Tech University Alkタンパク質分解剤及びそれらの癌療法における使用
JP7594757B2 (ja) 2017-12-13 2024-12-05 上海科技大学 Alkタンパク質分解剤及びそれらの癌療法における使用
JP2022174114A (ja) * 2017-12-13 2022-11-22 上海科技大学 Alkタンパク質分解剤及びそれらの癌療法における使用
JP2021506937A (ja) * 2017-12-21 2021-02-22 深▲チェン▼市塔吉瑞生物医薬有限公司Shenzhen TargetRx, Inc. キナーゼ活性を阻害するためのアリールホスフィンオキシド
US11254696B2 (en) 2017-12-21 2022-02-22 Shenzhen Targetrx, Inc. Dianilinopyrimidine compound for inhibiting kinase activity
JP7043098B2 (ja) 2017-12-21 2022-03-29 深▲チェン▼市塔吉瑞生物医薬有限公司 キナーゼ活性を阻害するためのジアニリノピリミジン系化合物
JP2021506942A (ja) * 2017-12-21 2021-02-22 深▲チェン▼市塔吉瑞生物医薬有限公司Shenzhen TargetRx, Inc. キナーゼ活性を阻害するためのジアニリノピリミジン系化合物
JP7085242B2 (ja) 2017-12-21 2022-06-16 深▲チェン▼市塔吉瑞生物医薬有限公司 キナーゼ活性を阻害するためのアリールホスフィンオキシド
JP7367908B2 (ja) 2018-04-09 2023-10-24 上海科技大学 標的タンパク質分解化合物、その抗腫瘍応用、その中間体および中間体の応用
JP2021521163A (ja) * 2018-04-09 2021-08-26 上海科技大学Shanghai Tech University 標的タンパク質分解化合物、その抗腫瘍応用、その中間体および中間体の応用
US12226424B2 (en) 2018-04-09 2025-02-18 Shanghaitech University Target protein degradation compounds, their anti-tumor use, their intermediates and use of intermediates
JP2022508055A (ja) * 2018-11-01 2022-01-19 サイロス ファーマシューティカルズ, インコーポレイテッド サイクリン依存性キナーゼ7(cdk7)の阻害剤
US12240869B2 (en) 2018-11-01 2025-03-04 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
JP2022518723A (ja) * 2019-01-18 2022-03-16 ボロノイ・カンパニー・リミテッド ピロロピリジン誘導体およびタンパク質キナーゼ関連疾患の予防または治療での使用のためのその用途
JP7564983B2 (ja) 2019-01-18 2024-10-10 ボロノイ インコーポレイテッド ピロロピリジン誘導体およびタンパク質キナーゼ関連疾患の予防または治療での使用のためのその用途
US12582641B2 (en) 2019-02-25 2026-03-24 Shanghaitech University Sulfur-containing compound based on glutarimide skeleton and application thereof
US12564638B2 (en) 2019-08-05 2026-03-03 Shanghaitech University EGFR protein degradant and anti-tumor application thereof
JP2023507319A (ja) * 2019-12-16 2023-02-22 コリア リサーチ インスティチュート オブ ケミカル テクノロジー 新規なピリミジン誘導体及びその用途
JP7659560B2 (ja) 2019-12-16 2025-04-09 コリア リサーチ インスティチュート オブ ケミカル テクノロジー 新規なピリミジン誘導体及びその用途
JP2023513333A (ja) * 2020-02-14 2023-03-30 貝達薬業股▲ふん▼有限公司 キノリニル基ホスフィンオキシド化合物、並びにその組成物及び使用
JP7602630B2 (ja) 2020-07-03 2024-12-18 成都地奥九泓製薬廠 アリールリン酸化物化合物およびその使用
JP2023532151A (ja) * 2020-07-03 2023-07-26 成都地奥九泓製薬廠 アリールリン酸化物化合物およびその使用
JP2024502175A (ja) * 2021-01-07 2024-01-17 オンタリオ・インスティテュート・フォー・キャンサー・リサーチ(オーアイシーアール) Nuakキナーゼの阻害剤としてのイソインドリノンアミノピリミジン化合物、その組成物及び使用
JP2024502174A (ja) * 2021-01-07 2024-01-17 オンタリオ・インスティテュート・フォー・キャンサー・リサーチ(オーアイシーアール) Nuakキナーゼの阻害剤としてのチエニル及びシクロアルキルアミノピリミジン化合物、その組成物及び使用

Also Published As

Publication number Publication date
LUC00120I2 (https=) 2019-12-27
LTC2300013I2 (lt) 2022-04-11
DK2300013T3 (en) 2017-12-04
EP2300013A1 (en) 2011-03-30
HRP20171534T8 (hr) 2018-08-24
US20200048288A1 (en) 2020-02-13
BRPI0908637A2 (pt) 2018-10-23
CY1119534T1 (el) 2018-04-04
JP2015163621A (ja) 2015-09-10
AU2009248923B2 (en) 2015-01-29
EP2300013A4 (en) 2012-09-12
KR20160132127A (ko) 2016-11-16
SI2300013T2 (sl) 2025-05-30
JP2017186345A (ja) 2017-10-12
JP2026035717A (ja) 2026-03-04
ES2645689T3 (es) 2017-12-07
CN102105150A (zh) 2011-06-22
KR20110010801A (ko) 2011-02-07
CY2019027I1 (el) 2019-11-27
ES2645689T5 (en) 2025-06-24
IL257083A (en) 2018-03-29
BRPI0908637B1 (pt) 2020-11-17
KR20180014882A (ko) 2018-02-09
DK2300013T4 (da) 2025-02-03
MX2010012703A (es) 2010-12-21
KR101956261B1 (ko) 2019-03-08
US20200317705A1 (en) 2020-10-08
CY2019027I2 (el) 2019-11-27
EA029131B1 (ru) 2018-02-28
JP6690032B2 (ja) 2020-04-28
HK1158497A1 (en) 2012-07-20
FI2300013T4 (fi) 2025-02-04
NL300990I1 (nl) 2019-05-29
IL208716B (en) 2018-02-28
IL257083B (en) 2019-08-29
US20170218000A1 (en) 2017-08-03
CN102105150B (zh) 2014-03-12
CA2723961C (en) 2017-03-21
JP2019094344A (ja) 2019-06-20
US9012462B2 (en) 2015-04-21
JP2018065864A (ja) 2018-04-26
NL300990I2 (nl) 2019-07-11
MX353308B (es) 2018-01-08
US20150225436A1 (en) 2015-08-13
HUS1900029I1 (hu) 2020-04-28
HRP20171534T1 (hr) 2018-01-26
FR19C1033I1 (https=) 2019-06-21
EP2300013B1 (en) 2017-09-06
EP3210609A1 (en) 2017-08-30
JP2020125308A (ja) 2020-08-20
WO2009143389A1 (en) 2009-11-26
NO2019024I1 (no) 2019-05-20
JP2022116057A (ja) 2022-08-09
JP6271064B2 (ja) 2018-01-31
JP6483233B2 (ja) 2019-03-13
SI2300013T1 (en) 2018-03-30
NO2300013T3 (https=) 2018-02-03
LT2300013T (lt) 2017-12-27
PT2300013T (pt) 2017-10-31
JP2024102203A (ja) 2024-07-30
HUE035029T2 (en) 2018-03-28
BRPI0908637B8 (pt) 2021-05-25
EA201071339A1 (ru) 2011-06-30
KR101781605B1 (ko) 2017-09-25
JP6190415B2 (ja) 2017-08-30
IL208716A0 (en) 2010-12-30
PL2300013T3 (pl) 2018-05-30
FIC20190029I1 (fi) 2019-05-17
EP2300013B2 (en) 2024-11-13
FR19C1033I2 (fr) 2020-01-31
AU2009248923A1 (en) 2009-11-26
LUC00120I1 (https=) 2019-05-24
KR101860057B1 (ko) 2018-05-21
CA2723961A1 (en) 2009-11-26
HRP20171534T4 (hr) 2025-02-14
LTPA2019510I1 (lt) 2019-06-10
US20120202776A1 (en) 2012-08-09
PL2300013T5 (pl) 2025-04-28

Similar Documents

Publication Publication Date Title
JP6690032B2 (ja) キナーゼ阻害剤としてのリン誘導体
US9273077B2 (en) Phosphorus derivatives as kinase inhibitors
JP5590040B2 (ja) キナーゼ阻害剤としてのピラジノピラジンおよび誘導体
US20130225528A1 (en) Phosphorus Derivatives as Kinase Inhibitors
JP2012511575A (ja) キナーゼ阻害剤としてのアザインドール誘導体
US20130225527A1 (en) Phosphorus Derivatives as Kinase Inhibitors
AU2016205003B2 (en) Phosphorous derivatives as kinase inhibitors
HK1158497B (en) Phosphorous derivatives as kinase inhibitors

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120518

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20120518

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20131031

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20131112

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140206

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140214

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140310

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140317

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20140407

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20140414

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140509

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20141224

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150422

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20150422

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20150625

A912 Re-examination (zenchi) completed and case transferred to appeal board

Free format text: JAPANESE INTERMEDIATE CODE: A912

Effective date: 20150731

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20160816

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20160908

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20161027

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20161130

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20161201

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20161201

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170316

RD02 Notification of acceptance of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7422

Effective date: 20170426

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20170509

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170511

A761 Written withdrawal of application

Free format text: JAPANESE INTERMEDIATE CODE: A761

Effective date: 20170517

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20170511