EA034866B1 - Замещенные пиримидиновые ингибиторы bmi-1 - Google Patents

Замещенные пиримидиновые ингибиторы bmi-1 Download PDF

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Publication number
EA034866B1
EA034866B1 EA201690502A EA201690502A EA034866B1 EA 034866 B1 EA034866 B1 EA 034866B1 EA 201690502 A EA201690502 A EA 201690502A EA 201690502 A EA201690502 A EA 201690502A EA 034866 B1 EA034866 B1 EA 034866B1
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EA
Eurasian Patent Office
Prior art keywords
diamine
benzimidazol
phenyl
pyrimidin
methyl
Prior art date
Application number
EA201690502A
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English (en)
Russian (ru)
Other versions
EA201690502A1 (ru
Inventor
У Ду
Рамиль Байазитов
Чан-Сун Ли
Йоунг-Чоон Моон
Стивен Д. Пэджет
Хунюй Жэнь
Надя Сидоренко
Ричард Джеральд Уайлде
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ПиТиСи ТЕРАПЬЮТИКС, ИНК.
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Publication of EA201690502A1 publication Critical patent/EA201690502A1/ru
Publication of EA034866B1 publication Critical patent/EA034866B1/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EA201690502A 2013-08-30 2013-11-21 Замещенные пиримидиновые ингибиторы bmi-1 EA034866B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361872091P 2013-08-30 2013-08-30
PCT/US2013/071216 WO2015030847A1 (en) 2013-08-30 2013-11-21 Substituted pyrimidine bmi-1 inhibitors

Publications (2)

Publication Number Publication Date
EA201690502A1 EA201690502A1 (ru) 2016-08-31
EA034866B1 true EA034866B1 (ru) 2020-03-31

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EA201690502A EA034866B1 (ru) 2013-08-30 2013-11-21 Замещенные пиримидиновые ингибиторы bmi-1

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US (1) US10370371B2 (enExample)
EP (1) EP3039015B1 (enExample)
JP (2) JP6524094B2 (enExample)
KR (1) KR102232595B1 (enExample)
CN (1) CN105683166B (enExample)
AR (1) AR093580A1 (enExample)
AU (2) AU2013399092A1 (enExample)
CA (1) CA2922657C (enExample)
CL (1) CL2016000466A1 (enExample)
EA (1) EA034866B1 (enExample)
IL (1) IL244321B (enExample)
MX (1) MX370588B (enExample)
NZ (2) NZ718055A (enExample)
TW (1) TWI692477B (enExample)
WO (1) WO2015030847A1 (enExample)
ZA (1) ZA201601697B (enExample)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102232595B1 (ko) * 2013-08-30 2021-03-26 피티씨 테라퓨틱스, 인크. 치환된 피리미딘 bmi-1 저해제
GB201321736D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
US10457669B2 (en) 2015-10-21 2019-10-29 Otsuka Pharmaceutical Co., Ltd. Benzolactam compounds as protein kinase inhibitors
US10851082B2 (en) 2015-10-28 2020-12-01 Northwestern University Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (MNK1) and 2 (MNK2)
US11001569B2 (en) 2016-01-22 2021-05-11 Janssen Pharmaceutica Nv 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors
HUE047684T2 (hu) 2016-01-22 2020-05-28 Janssen Pharmaceutica Nv Új szubsztituált cianoindolin származékok mint NIK inhibitorok
AU2017269335B2 (en) 2016-05-26 2021-07-01 Recurium Ip Holdings, Llc EGFR inhibitor compounds
WO2018002219A1 (en) 2016-06-30 2018-01-04 Janssen Pharmaceutica Nv Cyanoindoline derivatives as nik inhibitors
KR102517352B1 (ko) 2016-06-30 2023-03-31 잔센파마슈티카엔.브이. Nik 억제제로서의 헤테로방향족 유도체
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
EP3697777A1 (en) 2017-10-19 2020-08-26 eFFECTOR Therapeutics, Inc. Benzimidazole-indole inhibitors of mnk1 and mnk2
MD3784664T2 (ro) 2018-04-26 2025-06-30 Pfizer Derivați de 2-amino-piridină sau de 2-amino-pirimidină utilizați ca inhibitori de kinaze dependente de cicline
EP3564235A1 (en) * 2018-05-03 2019-11-06 Northwestern University Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (mnk1) and 2 (mnk2)
EP4155293B1 (en) * 2018-06-07 2025-07-30 The Regents of The University of Michigan Prc1 inhibitors and methods of treatment therewith
JP2021535198A (ja) 2018-08-17 2021-12-16 ピーティーシー セラピューティクス, インコーポレイテッド 膵臓癌を治療する方法
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
MX2021010398A (es) * 2019-02-28 2022-01-18 Ptc Therapeutics Inc Metodo para tratar un mieloma multiple.
TW202100520A (zh) 2019-03-05 2021-01-01 美商英塞特公司 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
BR112021022105A2 (pt) 2019-05-05 2021-12-28 Qilu Regor Therapeutics Inc Inibidores de cdk
CA3146375A1 (en) * 2019-07-10 2021-01-14 Aucentra Therapeutics Pty Ltd Derivatives of 4-(imidazo[l,2-a]pyridin-3-yl)-n-(pyridinyl)pyrimidin-2-amine as therapeutic agents
KR102894509B1 (ko) * 2019-07-24 2025-12-02 메르크 파텐트 게엠베하 4-(이미다조[1,2-a]피리딘-3-일)-피리미딘 유도체
CN116348458A (zh) 2019-08-14 2023-06-27 因赛特公司 作为cdk2抑制剂的咪唑基嘧啶基胺化合物
CN119930611A (zh) 2019-10-11 2025-05-06 因赛特公司 作为cdk2抑制剂的双环胺
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
WO2023250439A1 (en) * 2022-06-22 2023-12-28 Tempest Therapeutics, Inc. Trex1 inhibitors and uses thereof
WO2025024388A1 (en) 2023-07-21 2025-01-30 Accutar Biotechnology Inc. Aminopyrimidine derivatives as cyclin-dependent kinase inhibitors

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7582630B2 (en) * 2002-10-15 2009-09-01 Smithkline Beecham Corporation Pyradazine compounds as GSK-3 inhibitors
US7855205B2 (en) * 2004-10-29 2010-12-21 Janssen Pharmaceutica Nv Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
US20110039873A1 (en) * 2009-06-08 2011-02-17 Gaeta Federico C A SUBSTITUTED PYRAZOLO[1,5-a] PYRIDINE COMPOUNDS HAVING MULTI-TARGET ACTIVITY
US20110098301A1 (en) * 2005-03-10 2011-04-28 Bayer Healthcare Llc Pyrimidine Derivatives for Treatment of Hyperproliferative Disorders
US20110190239A1 (en) * 2008-07-01 2011-08-04 Ptc Therapeutics, Inc. Bmi-1 protein expression modulators

Family Cites Families (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH593266A5 (enExample) 1973-09-20 1977-11-30 Delalande Sa
AU677772B2 (en) 1991-10-07 1997-05-08 Biogen Idec Ma Inc. Method of prophylaxis or treatment of antigen presenting cell driven skin conditions using inhibitors of the CD2/LFA -3 interaction
US6162432A (en) 1991-10-07 2000-12-19 Biogen, Inc. Method of prophylaxis or treatment of antigen presenting cell driven skin conditions using inhibitors of the CD2/LFA-3 interaction
AU688087B2 (en) 1994-08-13 1998-03-05 Yuhan Corporation Novel pyrimidine derivatives and processes for the preparation thereof
IN188411B (enExample) * 1997-03-27 2002-09-21 Yuhan Corp
KR100272471B1 (ko) 1998-11-17 2000-11-15 김선진 신규의 피리미딘 유도체 및 그의 제조방법
AU5636900A (en) * 1999-06-30 2001-01-31 Merck & Co., Inc. Src kinase inhibitor compounds
GB9919778D0 (en) * 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
JP2003511378A (ja) 1999-10-07 2003-03-25 アムジエン・インコーポレーテツド トリアジン系キナーゼ阻害薬
AU7922900A (en) 1999-10-27 2001-05-08 Novartis Ag Thiazole and imidazo (4,5-b) pyridine compounds and their pharmaceutical use
HUP0301117A3 (en) 2000-02-17 2004-01-28 Amgen Inc Thousand Oaks Imidazole derivatives kinase inhibitors, their use, process for their preparation and pharmaceutical compositions containing them
AU2001242629B2 (en) 2000-03-29 2005-08-11 Cyclacel Limited 2-substituted 4-heteroaryl-pyrimidines and their use in the treatment of proliferative disorders
ES2266258T3 (es) 2000-09-15 2007-03-01 Vertex Pharmaceuticals Incorporated Compuestos de pirazol utiles como inhibidores de proteina cinasas.
AU9458401A (en) 2000-09-20 2002-04-02 Ortho Mcneil Pharm Inc Pyrazine derivatives as modulators of tyrosine kinases
US6716851B2 (en) 2000-12-12 2004-04-06 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
BR0207096A (pt) 2001-02-20 2004-01-20 Astrazeneca Ab Uso de um composto, compostos, formulação farmacêutica, e, método de tratamento e/ou profilaxia de condições associadas com a inibição de glicogênio sintase quinase-3
US20030165873A1 (en) 2001-03-02 2003-09-04 Come Jon H. Three hybrid assay system
CA2450555A1 (en) 2001-06-25 2003-01-03 Merck & Co., Inc. (pyrimidyl)(phenyl)substituted fused heteroaryl p38 inhibiting and pkg kinase inhibiting compounds
US6689778B2 (en) 2001-07-03 2004-02-10 Vertex Pharmaceuticals Incorporated Inhibitors of Src and Lck protein kinases
WO2003011837A1 (en) * 2001-08-01 2003-02-13 Merck & Co., Inc. Tyrosine kinase inhibitors
US7494997B2 (en) 2002-06-28 2009-02-24 Nippon Shinyaku Co., Ltd. Amide derivative
GB0215844D0 (en) 2002-07-09 2002-08-14 Novartis Ag Organic compounds
WO2004007407A2 (en) 2002-07-11 2004-01-22 Fluorous Technologies Incorporated Fluorous tagging and scavenging reactants and methods of synthesis and use thereof
US20040110821A1 (en) 2002-08-07 2004-06-10 Konkel Michael J. GAL3 receptor antagonists for the treatment of affective disorders
UA80296C2 (en) * 2002-09-06 2007-09-10 Biogen Inc Imidazolopyridines and methods of making and using the same
US7169781B2 (en) 2003-10-17 2007-01-30 Hoffmann-La Roche Inc. Imidazole derivatives and their use as pharmaceutical agents
US20080207613A1 (en) 2004-01-12 2008-08-28 Cytopia Research Pty Ltd Selective Kinase Inhibitors
JP2007520558A (ja) * 2004-02-04 2007-07-26 スミスクライン・ビーチャム・コーポレイション キナーゼ阻害剤として有用なピリミジノン化合物
US7507826B2 (en) 2004-03-30 2009-03-24 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of JAK and other protein kinases
JP2006045119A (ja) 2004-08-04 2006-02-16 Toray Ind Inc ピラジン誘導体及びそれを有効成分とする腎炎治療薬
EP1854793A4 (en) 2005-02-28 2011-01-26 Japan Tobacco Inc NEW AMINOPYRIDEIN COMPOUND WITH SYK-HEMDERING EFFECT
US20080039450A1 (en) 2006-06-22 2008-02-14 Jensen Annika J Compounds
CN101516873A (zh) 2006-10-03 2009-08-26 神经研究公司 用作钾通道调节剂的吲唑基衍生物
AU2007304195A1 (en) 2006-10-03 2008-04-10 Neurosearch A/S Indazolyl derivatives useful as potassium channel modulating agents
ES2383370T3 (es) 2006-10-19 2012-06-20 Signal Pharmaceuticals Llc Compuestos de heteroarilo, sus composiciones y uso de los mismos como inhibidores de proteína quinasa
WO2008079933A2 (en) 2006-12-22 2008-07-03 Novartis Ag Heteroaryl-heteroaryl compounds as cdk inhibitors for the treatment of cancer, inflammation and viral infections
TW200902010A (en) 2007-01-26 2009-01-16 Smithkline Beecham Corp Anthranilamide inhibitors of aurora kinase
EP2121633A2 (en) 2007-02-12 2009-11-25 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
WO2008132502A1 (en) 2007-04-25 2008-11-06 Astrazeneca Ab Pyrazolyl-amino-substituted pyrimidines and their use for the treatment of cancer
GB0714573D0 (en) 2007-07-26 2007-09-05 Imp Innovations Ltd Marker gene
WO2009037247A1 (en) 2007-09-17 2009-03-26 Neurosearch A/S Pyrazine derivatives and their use as potassium channel modulators
MX2010005300A (es) * 2007-11-16 2010-06-25 Incyte Corp 4-pirazolil-n-arilpirimidin-2-aminas y 4-pirazolil-n-heteroarilpir imidin-2-aminas como inhibidores de cinasas janus.
JP2011506303A (ja) * 2007-12-07 2011-03-03 ノバルティス アーゲー ピラゾール誘導体およびサイクリン依存性キナーゼの阻害剤としてのその使用
DE102008005493A1 (de) 2008-01-22 2009-07-23 Merck Patent Gmbh 4-(Pyrrolo[2,3-c] pyridine-3-yl)-pyrimidin-2-yl-amin-derivate
GB0801416D0 (en) 2008-01-25 2008-03-05 Piramed Ltd Pharmaceutical compounds
JP2011518219A (ja) 2008-04-22 2011-06-23 ポートラ ファーマシューティカルズ, インコーポレイテッド タンパク質キナーゼの阻害剤
CN102177154A (zh) 2008-09-02 2011-09-07 神经研究公司 吡唑基-嘧啶衍生物及其作为钾通道调节剂的应用
WO2010061903A1 (ja) 2008-11-27 2010-06-03 塩野義製薬株式会社 Pi3k阻害活性を有するピリミジン誘導体およびピリジン誘導体
WO2010092962A1 (ja) 2009-02-12 2010-08-19 アステラス製薬株式会社 へテロ環誘導体
AU2010229468A1 (en) 2009-03-27 2011-10-13 Vetdc, Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy
EP2435435B1 (en) 2009-05-27 2014-01-29 AbbVie Inc. Pyrimidine inhibitors of kinase activity
DK2442809T3 (en) 2009-06-17 2016-12-19 Vertex Pharma Inhibitors of the replication of influenza virus
US8486939B2 (en) 2009-07-07 2013-07-16 Pathway Therapeutics Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
JP2012533553A (ja) * 2009-07-15 2012-12-27 アボット・ラボラトリーズ ピロロピリジン系キナーゼ阻害薬
JP5415176B2 (ja) 2009-08-06 2014-02-12 株式会社マキタ スイッチ
TWI523852B (zh) 2010-01-12 2016-03-01 Ab科學公司 經取代之唑衍生物、含彼之組合物及其用途
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
ES2365960B1 (es) 2010-03-31 2012-06-04 Palobiofarma, S.L Nuevos antagonistas de los receptores de adenosina.
EP2604601B1 (en) 2010-08-10 2016-02-24 Astellas Pharma Inc. Hetero ring compound
CA2812081A1 (en) 2010-09-13 2012-03-22 Novartis Ag Triazine-oxadiazoles
WO2012050884A2 (en) 2010-09-28 2012-04-19 President And Fellows Of Harvard College Cardiac glycosides are potent inhibitors of interferon-beta gene expression
US9090593B2 (en) 2010-12-09 2015-07-28 Amgen Inc. Bicyclic compounds as Pim inhibitors
CN103402997B (zh) 2011-02-25 2015-08-26 柳韩洋行 二氨基嘧啶衍生物及其制备方法
ES2698847T3 (es) 2011-07-07 2019-02-06 Merck Patent Gmbh Azaheterociclos sustituidos para el tratamiento del cáncer
JP6412503B2 (ja) 2012-11-21 2018-10-24 ピーティーシー セラピューティクス, インコーポレイテッド 置換逆ピリミジンBmi−1阻害剤
UY35148A (es) 2012-11-21 2014-05-30 Amgen Inc Immunoglobulinas heterodiméricas
US9695228B2 (en) 2012-11-21 2017-07-04 Janssen Biotech, Inc. EGFR and c-Met fibronectin type III domain binding molecules
KR102232595B1 (ko) * 2013-08-30 2021-03-26 피티씨 테라퓨틱스, 인크. 치환된 피리미딘 bmi-1 저해제

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7582630B2 (en) * 2002-10-15 2009-09-01 Smithkline Beecham Corporation Pyradazine compounds as GSK-3 inhibitors
US7855205B2 (en) * 2004-10-29 2010-12-21 Janssen Pharmaceutica Nv Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
US20110098301A1 (en) * 2005-03-10 2011-04-28 Bayer Healthcare Llc Pyrimidine Derivatives for Treatment of Hyperproliferative Disorders
US20110190239A1 (en) * 2008-07-01 2011-08-04 Ptc Therapeutics, Inc. Bmi-1 protein expression modulators
US20110039873A1 (en) * 2009-06-08 2011-02-17 Gaeta Federico C A SUBSTITUTED PYRAZOLO[1,5-a] PYRIDINE COMPOUNDS HAVING MULTI-TARGET ACTIVITY

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