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
Original Assignee
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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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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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Family Applications (1)

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

Country Status (16)

Country Link
US (1) US10370371B2 (OSRAM)
EP (1) EP3039015B1 (OSRAM)
JP (2) JP6524094B2 (OSRAM)
KR (1) KR102232595B1 (OSRAM)
CN (1) CN105683166B (OSRAM)
AR (1) AR093580A1 (OSRAM)
AU (2) AU2013399092A1 (OSRAM)
CA (1) CA2922657C (OSRAM)
CL (1) CL2016000466A1 (OSRAM)
EA (1) EA034866B1 (OSRAM)
IL (1) IL244321B (OSRAM)
MX (1) MX370588B (OSRAM)
NZ (2) NZ748260A (OSRAM)
TW (1) TWI692477B (OSRAM)
WO (1) WO2015030847A1 (OSRAM)
ZA (1) ZA201601697B (OSRAM)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI692477B (zh) * 2013-08-30 2020-05-01 美商Ｐｔｃ治療公司 經取代嘧啶ｂｍｉ-１抑制劑
GB201321736D0 (en) * 2013-12-09 2014-01-22 Ucb Pharma Sa Therapeutic agents
IL291017B2 (en) 2015-10-21 2023-11-01 Otsuka Pharma 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)
CN109311846B (zh) 2016-01-22 2021-03-19 杨森制药有限公司 作为nik抑制剂的新的6元杂芳族取代的氰基吲哚衍生物
WO2017125530A1 (en) 2016-01-22 2017-07-27 Janssen Pharmaceutica Nv New substituted cyanoindoline derivatives as nik inhibitors
EP3464275B1 (en) 2016-05-26 2024-05-08 Recurium IP Holdings, LLC Egfr inhibitor compounds
WO2018002219A1 (en) 2016-06-30 2018-01-04 Janssen Pharmaceutica Nv Cyanoindoline derivatives as nik inhibitors
CN109641882B (zh) 2016-06-30 2022-10-28 杨森制药有限公司 作为nik抑制剂的杂芳族衍生物
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
CN118286225A (zh) 2018-04-26 2024-07-05 辉瑞公司 作为细胞周期蛋白依赖性激酶抑制剂的2-氨基-吡啶或2-氨基-嘧啶衍生物
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)
CA3102777A1 (en) 2018-06-07 2019-12-12 The Regents Of The University Of Michigan Prc1 inhibitors and methods of treatment therewith
US12023335B2 (en) 2018-08-17 2024-07-02 Ptc Therapeutics, Inc. Method for treating pancreatic cancer
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
EA202192117A1 (ru) * 2019-02-28 2021-11-23 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Способ лечения множественной миеломы
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US20220296595A1 (en) 2019-05-05 2022-09-22 Qilu Regor Therapeutics Inc. Cdk inhibitors
AU2020311297A1 (en) * 2019-07-10 2022-02-03 Aucentra Therapeutics Pty Ltd DERIVATIVES OF 4-(IMIDAZO[l,2-a]PYRIDIN-3-YL)-N-(PYRIDINYL)PYRIMIDIN- 2-AMINE AS THERAPEUTIC AGENTS
IL289953B2 (en) * 2019-07-24 2025-03-01 Merck Patent Gmbh 4-(Imidazo[1,2-a]pyridin-3-yl)-pyrimidine derivatives
BR112022002698A2 (pt) 2019-08-14 2022-07-19 Incyte Corp Compostos de imidazolil pirimidinilamina como inibidores de cdk2
MX2022004390A (es) 2019-10-11 2022-08-08 Incyte Corp Aminas biciclicas como inhibidores de la cinasa dependiente de ciclina 2 (cdk2).
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 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 (OSRAM) 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
JP2896532B2 (ja) * 1994-08-13 1999-05-31 ユーハン コーポレーション 新規なピリミジン誘導体およびその製造方法
IN188411B (OSRAM) * 1997-03-27 2002-09-21 Yuhan Corp
KR100272471B1 (ko) * 1998-11-17 2000-11-15 김선진 신규의 피리미딘 유도체 및 그의 제조방법
CA2383546A1 (en) * 1999-06-30 2001-01-04 William H. Parsons Src kinase inhibitor compounds
GB9919778D0 (en) 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
CA2386218A1 (en) 1999-10-07 2001-04-12 Amgen Inc. Triazine kinase inhibitors
DE60024480T2 (de) * 1999-10-27 2006-07-27 Novartis Ag Thiazol und imidazo[4,5-b]pyridin verbindungen und ihre verwendung als pharmazeutika
US20030004174A9 (en) 2000-02-17 2003-01-02 Armistead David M. Kinase inhibitors
AU4262901A (en) * 2000-03-29 2001-10-08 Cyclacel Ltd 2-substituted 4-heteroaryl-pyrimidines and their use in the treatmetn of proliferative disorders
ATE346064T1 (de) 2000-09-15 2006-12-15 Vertex Pharma Pyrazolverbindungen als protein-kinasehemmer
HK1054393B (en) 2000-09-20 2009-08-28 Ortho-Mcneil Pharmaceutical, 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
ES2316546T3 (es) 2001-02-20 2009-04-16 Astrazeneca Ab 2-arilamino-pirimidinas para el tratamiento de trastornos asociados a gsk3.
ATE497603T1 (de) 2001-03-02 2011-02-15 Gpc Biotech Ag Drei-hybrid-assaysystem
US7196095B2 (en) 2001-06-25 2007-03-27 Merck & Co., Inc. (Pyrimidinyl) (phenyl) substituted fused heteroaryl p38 inhibiting and PKG kinase inhibiting compounds
JP4342937B2 (ja) * 2001-07-03 2009-10-14 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 ＳｒｃおよびＬｃｋタンパク質キナーゼの阻害剤としてのイソキサゾールピリミジン
US7109204B2 (en) * 2001-08-01 2006-09-19 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
KR101164541B1 (ko) 2004-01-12 2012-07-10 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 선택적 키나제 저해제
WO2005076854A2 (en) * 2004-02-04 2005-08-25 Smithkline Beecham Corporation Pyrimidinone compounds useful as kinase inhibitors
PT1730146E (pt) 2004-03-30 2011-07-11 Vertex Pharma Azaindoles úteis como inibidores de jak e outras proteínas quinases
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
AU2006219231B2 (en) 2005-02-28 2010-01-14 Japan Tobacco Inc. Novel aminopyridine compound with Syk inhibitory activity
BRPI0713328A2 (pt) 2006-06-22 2012-10-30 Biovitrum Ab derivados de piridina e pirazina como inibidores de cinase mnk
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
CA2665398A1 (en) 2006-10-03 2008-04-10 Neurosearch A/S Indazolyl derivatives useful as potassium channel modulating agents
ZA200902384B (en) 2006-10-19 2010-07-28 Signal Pharm Llc Heteroaryl compounds, compositions thereof, and use thereof as protein kinase inhibitors
AU2007336933A1 (en) * 2006-12-22 2008-07-03 Novartis Ag Heteroaryl-heteroaryl compounds as CDK inhibitors for the treatment of cancer, inflammation and viral infections
AR065015A1 (es) 2007-01-26 2009-05-13 Smithkline Beecham Corp Derivados de antranilamida, composiciones farmaceuticas que los contienen, y usos para el tratamiento del cancer
CA2676715A1 (en) 2007-02-12 2008-08-21 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
WO2009064835A1 (en) 2007-11-16 2009-05-22 Incyte Corporation 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
CA2707989A1 (en) 2007-12-07 2009-06-11 Novartis Ag Pyrazole derivatives and use thereof as inhibitors of cyclin dependent kinases
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
NZ588830A (en) 2008-04-22 2012-11-30 Portola Pharm Inc Inhibitors of protein kinases
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
AU2010214440A1 (en) 2009-02-12 2011-09-01 Astellas Pharma Inc. Hetero ring derivative
NZ595372A (en) 2009-03-27 2013-11-29 Vetdc Inc Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy
ES2453097T3 (es) 2009-05-27 2014-04-04 Abbvie Inc. Inhibidores de pirimidina de actividad quinasa
PH12015501678B1 (en) 2009-06-17 2022-07-06 Vertex Pharma Inhibitors of influenza viruses replication
EP2451802A1 (en) 2009-07-07 2012-05-16 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
EA022188B1 (ru) 2010-01-12 2015-11-30 Аб Сьянс Оксазольные ингибиторы киназы, содержащие их композиции и их применение
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.
MX346042B (es) 2010-08-10 2017-03-03 Astellas Pharma Inc Compuesto heterociclico.
EA026132B1 (ru) 2010-09-13 2017-03-31 Новартис Аг Триазиноксадиазолы, фармацевтические композиции на их основе и их применение
WO2012050884A2 (en) 2010-09-28 2012-04-19 President And Fellows Of Harvard College Cardiac glycosides are potent inhibitors of interferon-beta gene expression
CA2819373A1 (en) 2010-12-09 2012-06-14 Amgen Inc. Bicyclic compounds as pim inhibitors
PL2678332T3 (pl) 2011-02-25 2016-12-30 Pochodne diaminopirymidyny i sposoby ich wytwarzania
US9199962B2 (en) 2011-07-07 2015-12-01 Merck Patent Gmbh Substituted azaheterocycles for the treatment of cancer
EP2922828B1 (en) 2012-11-21 2020-07-08 PTC Therapeutics, Inc. 4,6-diamino-pyrimidine derivatives as bmi-1 inhibitors for treating cancer
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
TWI692477B (zh) * 2013-08-30 2020-05-01 美商Ｐｔｃ治療公司 經取代嘧啶ｂｍｉ-１抑制劑

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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