CN102548984B - Pi3激酶和/或mtor的抑制剂 - Google Patents

Pi3激酶和/或mtor的抑制剂 Download PDF

Info

Publication number
CN102548984B
CN102548984B CN201080030184.6A CN201080030184A CN102548984B CN 102548984 B CN102548984 B CN 102548984B CN 201080030184 A CN201080030184 A CN 201080030184A CN 102548984 B CN102548984 B CN 102548984B
Authority
CN
China
Prior art keywords
methyl
amine
triazin
amino
pyridyl
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.)
Expired - Fee Related
Application number
CN201080030184.6A
Other languages
English (en)
Chinese (zh)
Other versions
CN102548984A (zh
Inventor
K·安德鲁斯
Y·Y·伯
S·布克
V·J·西
N·德安格罗
B·J·赫贝里奇
F-T·洪
C·L·M·杰克逊
B·A·兰曼
H·廖
L·刘
N·尼施穆拉
M·H·诺尔曼
L·H·佩图斯
A·B·里德
A·L·史密斯
S·泰德斯
N·A·塔马约
B·吴
R·乌尔茨
K·杨
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Amgen Inc
Original Assignee
Amgen Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Amgen Inc filed Critical Amgen Inc
Publication of CN102548984A publication Critical patent/CN102548984A/zh
Application granted granted Critical
Publication of CN102548984B publication Critical patent/CN102548984B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • 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
    • 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
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201080030184.6A 2009-04-28 2010-04-27 Pi3激酶和/或mtor的抑制剂 Expired - Fee Related CN102548984B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US17352009P 2009-04-28 2009-04-28
US61/173520 2009-04-28
US61/173,520 2009-04-28
US25853209P 2009-11-05 2009-11-05
US61/258532 2009-11-05
US61/258,532 2009-11-05
PCT/US2010/032593 WO2010126895A1 (en) 2009-04-28 2010-04-27 Inhibitors of pi3 kinase and / or mtor

Publications (2)

Publication Number Publication Date
CN102548984A CN102548984A (zh) 2012-07-04
CN102548984B true CN102548984B (zh) 2015-11-25

Family

ID=42315845

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201080030184.6A Expired - Fee Related CN102548984B (zh) 2009-04-28 2010-04-27 Pi3激酶和/或mtor的抑制剂

Country Status (23)

Country Link
US (2) US8362241B2 (enExample)
EP (1) EP2424859B1 (enExample)
JP (1) JP5697662B2 (enExample)
KR (1) KR20120007540A (enExample)
CN (1) CN102548984B (enExample)
AR (1) AR076486A1 (enExample)
AU (1) AU2010241723B2 (enExample)
BR (1) BRPI1015262A2 (enExample)
CA (1) CA2758986C (enExample)
CL (1) CL2011002691A1 (enExample)
CO (1) CO6440596A2 (enExample)
CR (1) CR20110634A (enExample)
EA (1) EA019700B1 (enExample)
IL (1) IL215731A0 (enExample)
MA (1) MA34207B1 (enExample)
MX (1) MX2011011335A (enExample)
NZ (1) NZ595572A (enExample)
PE (1) PE20121159A1 (enExample)
SG (1) SG175364A1 (enExample)
TW (1) TW201103902A (enExample)
UY (1) UY32582A (enExample)
WO (1) WO2010126895A1 (enExample)
ZA (1) ZA201108101B (enExample)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2725014C (en) * 2008-05-30 2014-06-17 Amgen Inc. Inhibitors of pi3 kinase
AU2010226490A1 (en) 2009-03-20 2011-10-06 Amgen Inc. Inhibitors of PI3 kinase
UY32582A (es) * 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
FR2958290B1 (fr) 2010-03-30 2012-10-19 Sanofi Aventis Procede de preparation de derives de sulfonamido-benzofurane
JO2998B1 (ar) 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
HUP1000330A2 (en) 2010-06-18 2011-12-28 Sanofi Sa Process for the preparation of dronedarone and the novel intermediates
AU2011337461B2 (en) * 2010-12-02 2015-04-02 Bisichem Co., Ltd. Novel purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition with inhibitory activity against Raf kinase, containing same as active ingredient
US9284270B2 (en) 2011-02-14 2016-03-15 The Governers Of The University Of Alberta Boronic acid catalysts and methods of use thereof for activation and transformation of carboxylic acids
US20120258967A1 (en) * 2011-03-09 2012-10-11 Avila Therapeutics, Inc. Pi3 kinase inhibitors and uses thereof
HUP1100167A2 (en) 2011-03-29 2012-11-28 Sanofi Sa Process for preparation of dronedarone by mesylation
HUP1100165A2 (en) 2011-03-29 2012-12-28 Sanofi Sa Process for preparation of dronedarone by n-butylation
SG10201604682VA (en) 2011-06-10 2016-07-28 Merck Patent Gmbh Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity
MX352672B (es) 2011-09-27 2017-12-04 Amgen Inc Compuestos heterocíclicos como inhibidores de mdm2 para el tratamiento del cáncer.
EP2780341B1 (en) * 2011-11-14 2019-02-13 Chia Tai Tianqing Pharmaceutical Group Co.,Ltd Kinase modulating compounds, compositions containing the same and use thereof
CN103102349B (zh) * 2011-11-14 2017-03-15 北京赛林泰医药技术有限公司 蛋白激酶抑制剂及其组合物和用途
FR2983198B1 (fr) 2011-11-29 2013-11-15 Sanofi Sa Procede de preparation de derives de 5-amino-benzoyl-benzofurane
EP2617718A1 (en) 2012-01-20 2013-07-24 Sanofi Process for preparation of dronedarone by the use of dibutylaminopropanol reagent
US9221778B2 (en) 2012-02-13 2015-12-29 Sanofi Process for preparation of dronedarone by removal of hydroxyl group
WO2013121234A1 (en) * 2012-02-14 2013-08-22 Sanofi Process for the preparation of dronedarone by oxidation of a sulphenyl group
WO2013124745A1 (en) 2012-02-22 2013-08-29 Sanofi Process for preparation of dronedarone by oxidation of a hydroxyl group
WO2013178337A1 (en) 2012-05-31 2013-12-05 Sanofi Process for preparation of dronedarone by grignard reaction
CA2881472A1 (en) * 2012-08-09 2014-02-13 Neuropore Therapies, Inc. Aryl-and heteroaryl-substituted benzene derivatives as modulators of pi3-kinase signalling pathways
FR2994572B1 (fr) * 2012-08-17 2015-04-17 Centre Nat Rech Scient Pyrido[3,2-d]pyrimidines trisubstituees, leurs procedes de preparation et leurs utilisation en therapeutique
JP6417338B2 (ja) 2013-02-19 2018-11-07 アムジエン・インコーポレーテツド 癌の治療のためのmdm2阻害剤としてのシス−モルホリノン及び他の化合物
EP2970237B1 (en) 2013-03-14 2017-09-27 Amgen Inc. Heteroaryl acid morpholinone compounds as mdm2 inhibitors for the treatment of cancer
WO2014177915A1 (en) 2013-05-01 2014-11-06 Piramal Enterprises Limited Cancer combination therapy using imidazo[4,5-c]quinoline derivatives
JOP20200296A1 (ar) 2013-06-10 2017-06-16 Amgen Inc عمليات صنع وأشكال بلورية من mdm2 مثبط
KR20160099081A (ko) 2013-07-26 2016-08-19 업데이트 파마 인코포레이트 비산트렌의 치료 효과 개선용 조합 방법
CN104447727B (zh) * 2013-09-02 2018-04-27 广东东阳光药业有限公司 取代的氨基嘧啶类化合物及其使用方法和用途
CA2925601C (en) * 2013-09-25 2022-11-01 Vertex Pharmaceuticals Incorporated A selective inhibitor of phosphatidylinositol 3-kinase-gamma
SI3068393T1 (sl) 2013-11-11 2022-11-30 Amgen Inc. Kombinirana terapija, ki vključuje zaviralec MDM2 in eno ali več dodatnih farmacevtskih učinkovin za zdravljenje različnih vrst raka
CN104744446B (zh) * 2013-12-30 2019-06-25 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用
BR112016029662B1 (pt) 2014-06-19 2023-10-24 Takeda Pharmaceutical Company Limited COMPOSTO DE FÓRMULA Bf OU UMA FORMA FARMACEUTICAMENTE ACEITÁVEL DO MESMO, COMPOSIÇÃO FARMACÊUTICA COMPREENDENDO O MESMO E SEU USO
WO2017047602A1 (ja) * 2015-09-18 2017-03-23 科研製薬株式会社 ビアリール誘導体及びそれを含有する医薬
CA3013569A1 (en) * 2016-02-03 2017-08-10 Samjin Pharmaceutical Co., Ltd. Pyridine derivative inhibiting raf kinase and vascular endothelial growth factor receptor, method for preparing same, pharmaceutical composition containing same, and use thereof
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
CN109952303B (zh) * 2016-10-14 2022-10-21 林伯士拉克许米公司 Tyk2抑制剂及其用途
EP3538091A4 (en) 2016-11-08 2020-06-10 Navitor Pharmaceuticals, Inc. PHENYL AMINO PIPERIDINE MTORC INHIBITORS AND USES THEREOF
JP6469272B2 (ja) * 2017-03-01 2019-02-13 科研製薬株式会社 ビアリール誘導体又はその塩からなる医薬
EA201992166A1 (ru) 2017-03-14 2020-02-04 Басф Се Гербицидные азины
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
EP4403175A3 (en) 2017-09-08 2024-10-02 Amgen Inc. Inhibitors of kras g12c and methods of using the same
SG11202003879RA (en) 2017-10-30 2020-05-28 Neuropore Therapies Inc Substituted phenyl sulfonyl phenyl triazole thiones and uses thereof
CN112074505B (zh) * 2018-03-08 2024-04-05 因赛特公司 作为PI3K-γ抑制剂的氨基吡嗪二醇化合物
CA3098574A1 (en) 2018-05-04 2019-11-07 Amgen Inc. Kras g12c inhibitors and methods of using the same
WO2019222093A1 (en) 2018-05-14 2019-11-21 Ariad Pharmaceuticals, Inc. Pharmaceutical salts of pyrimidine derivatives and method of treating disorders
AU2019336588B2 (en) 2018-06-12 2022-07-28 Amgen Inc. KRAS G12C inhibitors encompassing a piperazine ring and use thereof in the treatment of cancer
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法
US12168644B2 (en) * 2018-12-21 2024-12-17 Saltigo Gmbh Process for preparing 2-alkoxy-4-amino-5-methyl-pyridines and/or 2-alkoxy-4-alkylamino-5-methyl-pyridines
WO2020146779A1 (en) * 2019-01-11 2020-07-16 The Regents Of The University Of California mTORC1 INHIBITORS FOR ACTIVATING AUTOPHAGY
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
NZ782284A (en) 2019-05-21 2024-11-29 Amgen Inc Solid state forms
US20240139193A1 (en) 2019-10-15 2024-05-02 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
US20230028414A1 (en) 2019-12-16 2023-01-26 Amgen Inc. Dosing regimen of kras g12c inhibitor
KR102852061B1 (ko) * 2020-03-09 2025-08-27 삼성중공업 주식회사 선박용 볼라드
CN116075504B (zh) * 2020-06-23 2025-08-12 深圳福沃药业有限公司 化合物的结晶形式
CN116283467B (zh) * 2023-01-18 2024-06-11 四川大学 一种合成二芳基烷基甲烷的方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005113494A2 (en) * 2004-05-07 2005-12-01 Amgen Inc. Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer
WO2007042806A1 (en) * 2005-10-11 2007-04-19 Ludwig Institute For Cancer Research Pyrimidine derivatives for the treatment of cancer

Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU6526896A (en) 1995-07-22 1997-02-18 Rhone-Poulenc Rorer Limited Substituted aromatic compounds and their pharmaceutical use
AU2108601A (en) 1999-12-15 2001-06-25 Axys Pharmaceuticals, Inc. Salicylamides as serine protease inhibitors
AU2001250850A1 (en) 2000-03-17 2001-10-03 Dupont Pharmaceuticals Company Beta-amino acid derivatives as inhibitors of matrix metalloproteases and tnf-alpha
WO2001083456A1 (en) 2000-04-27 2001-11-08 Yamanouchi Pharmaceutical Co., Ltd. Condensed heteroaryl derivatives
US6864255B2 (en) 2001-04-11 2005-03-08 Amgen Inc. Substituted triazinyl amide derivatives and methods of use
US20030187026A1 (en) * 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
CA2484209C (en) 2002-05-03 2013-06-11 Exelixis, Inc. Protein kinase modulators and methods of use
WO2004000820A2 (en) 2002-06-21 2003-12-31 Cellular Genomics, Inc. Certain aromatic monocycles as kinase modulators
AU2003249369A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain amino-substituted monocycles as kinase modulators
WO2004099127A1 (en) 2003-05-07 2004-11-18 Novo Nordisk A/S Novel compounds as kinase inhibitors
US7781591B2 (en) * 2006-06-13 2010-08-24 Wyeth Llc Substituted 3-cyanopyridines as protein kinase inhibitors
UA86614C2 (ru) 2004-01-23 2009-05-12 Амген Инк Соединение, которое имеет активность ингибитора киназ, фармацевтическая композиция, которая включает указанное соединение, и их применение для приготовления лекарственного препарата
GB0415364D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
ES2395196T3 (es) * 2005-03-11 2013-02-11 Zenyaku Kogyo Kabushikikaisha Agente inmunosupresor que comprende un compuesto heterocíclico como ingrediente activo
WO2006123165A2 (en) 2005-05-19 2006-11-23 Astex Therapeutics Limited Pyrimidine derivatives as hsp90 inhibitors
WO2007011721A1 (en) 2005-07-15 2007-01-25 Kalypsys, Inc. Inhibitors of mitotic kinesin
US7989461B2 (en) 2005-12-23 2011-08-02 Amgen Inc. Substituted quinazolinamine compounds for the treatment of cancer
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
CA2637658C (en) 2006-01-23 2012-07-17 Amgen Inc. Aurora kinase modulators and method of use
BRPI0707666A2 (pt) * 2006-02-06 2011-05-10 Irm Llc compostos e composiÇÕes como inibidores de proteÍna cinase
WO2008001076A1 (en) * 2006-06-26 2008-01-03 Ucb Pharma S.A. Fused thiazole derivatives as kinase inhibitors
WO2008032089A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-2-m0rph0lin0-6-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032036A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 6-benzimidaz0lyl-2-m0rph0lin0-4- (azetidine, pyrrolidine, piperidine or azepine) pyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032077A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
WO2008032041A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives having inhibitory activity against pi3k enzymes
CN101563340A (zh) 2006-09-14 2009-10-21 阿斯利康(瑞典)有限公司 用作pi3k和mtor抑制剂用于治疗增殖性疾病的2-苯并咪唑基-6-吗啉代-4-哌啶-4-基嘧啶衍生物
US20090325954A1 (en) 2006-09-14 2009-12-31 Sam Butterworth 2-benzimidazolyl-6-morpholino-4-phenylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032033A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032064A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives
WO2008032091A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-6-m0rph0lin0-2-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
WO2008032060A1 (en) 2006-09-14 2008-03-20 Astrazeneca Ab 4-benzimidaz0lyl-6-m0rph0lin0-2-piperazinylpyrimidine derivatives as p13k and mtor inhibitors for the treatment of proliferative disorders
EP2069330A1 (en) 2006-09-14 2009-06-17 AstraZeneca AB 2 -benzimidazolyl- 6 -morpholino-4- (azetidine, pyrrolidine, piperidine or azepine) pyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders
KR20090108124A (ko) 2007-02-06 2009-10-14 노파르티스 아게 Pi 3-키나제 억제제 및 그의 사용 방법
AU2008273892A1 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
EP2074118A2 (en) 2007-07-09 2009-07-01 AstraZeneca AB Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
ATE554075T1 (de) 2007-07-09 2012-05-15 Astrazeneca Ab Bei mit mtor-kinase und/oder pi3k in zusammenhang stehenden krankheiten angewendete morpholinopyrimidinderivate
MX2010001020A (es) 2007-07-26 2010-03-01 Novartis Ag Derivados de pirimidina utiles para el tratamiento de condiciones inflamatorias o alergicas.
JP2011500823A (ja) 2007-10-22 2011-01-06 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Pi3キナーゼ阻害物質としてのピリドスルホンアミド誘導体
WO2009093981A1 (en) 2008-01-23 2009-07-30 S Bio Pte Ltd Triazine compounds as kinase inhibitors
US8268834B2 (en) 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
US20110053907A1 (en) 2008-03-27 2011-03-03 Auckland Uniservices Limited Substituted pyrimidines and triazines and their use in cancer therapy
RS55960B1 (sr) 2008-05-23 2017-09-29 Wyeth Llc Triazinska jedinjenja kao inhibitori pi3 kinaze i mtor
EP2318377B1 (en) 2008-07-31 2013-08-21 Genentech, Inc. Pyrimidine compounds, compositions and methods of use
US20100113523A1 (en) * 2008-10-30 2010-05-06 Alberte Randall S Tryptase Enzyme Inhibiting Aminopyridines
MX2011004570A (es) 2008-10-31 2011-06-17 Merck Sharp & Dohme Antagonistas del receptor p2x3 para el tratamiento del dolor.
GB2465405A (en) 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
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
SG172353A1 (en) 2008-12-23 2011-07-28 Abbott Lab Anti-viral compounds
CN102388037B (zh) 2009-02-10 2014-12-03 詹森药业有限公司 作为脯氨酰羟化酶抑制剂的喹唑啉酮
WO2010096314A1 (en) 2009-02-18 2010-08-26 Amgen Inc. INDOLE/BENZIMIDAZOLE COMPOUNDS AS mTOR KINASE INHIBITORS
EP2403847B1 (en) 2009-03-06 2016-03-02 UCB Biopharma SPRL Triazine derivatives as kinase inhibitors
WO2010110686A1 (en) 2009-03-27 2010-09-30 Pathway Therapeutics Limited Pyrimidinyl and 1,3,5 triazinyl benzimidazoles and their use in cancer therapy
NZ595372A (en) 2009-03-27 2013-11-29 Vetdc Inc Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy
UY32582A (es) * 2009-04-28 2010-11-30 Amgen Inc Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero
AU2010259009A1 (en) 2009-06-08 2012-01-12 Nantbioscience, Inc. Triazine derivatives and their therapeutical applications

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005113494A2 (en) * 2004-05-07 2005-12-01 Amgen Inc. Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer
WO2007042806A1 (en) * 2005-10-11 2007-04-19 Ludwig Institute For Cancer Research Pyrimidine derivatives for the treatment of cancer

Also Published As

Publication number Publication date
AU2010241723A1 (en) 2011-11-17
US20100273764A1 (en) 2010-10-28
EA019700B1 (ru) 2014-05-30
PE20121159A1 (es) 2012-09-19
CN102548984A (zh) 2012-07-04
ZA201108101B (en) 2012-07-25
CR20110634A (es) 2012-01-06
US8772480B2 (en) 2014-07-08
BRPI1015262A2 (pt) 2016-05-03
US8362241B2 (en) 2013-01-29
EP2424859A1 (en) 2012-03-07
MA34207B1 (fr) 2013-05-02
SG175364A1 (en) 2011-11-28
MX2011011335A (es) 2011-11-18
US20130079303A1 (en) 2013-03-28
UY32582A (es) 2010-11-30
KR20120007540A (ko) 2012-01-20
TW201103902A (en) 2011-02-01
AU2010241723B2 (en) 2012-12-13
JP2012525395A (ja) 2012-10-22
HK1167862A1 (en) 2012-12-14
CA2758986C (en) 2014-05-27
EP2424859B1 (en) 2015-04-08
CL2011002691A1 (es) 2012-03-16
NZ595572A (en) 2013-07-26
CA2758986A1 (en) 2010-11-04
IL215731A0 (en) 2012-01-31
AR076486A1 (es) 2011-06-15
JP5697662B2 (ja) 2015-04-08
WO2010126895A1 (en) 2010-11-04
CO6440596A2 (es) 2012-05-15
EA201101583A1 (ru) 2012-05-30

Similar Documents

Publication Publication Date Title
CN102548984B (zh) Pi3激酶和/或mtor的抑制剂
JP7005582B2 (ja) ブルトン型チロシンキナーゼ(btk)インヒビターとしての多フルオロ置換化合物
EP3152210B1 (en) Tank-binding kinase inhibitor compounds
EP2430013B1 (en) Heteroaryl compounds as pikk inhibitors
CN104837829B (zh) 抑制剂化合物
CN103596952B (zh) 作为Syk抑制剂的新型取代的吡啶并吡嗪类化合物
US12109198B2 (en) Macrocyclic azolopyridine derivatives as EED and PRC2 modulators
CN112055709A (zh) 吡嗪化合物和其用途
AU2014368725A1 (en) Isochromene derivatives as phosphoinositide 3-kinases inhibitors
CN112279837B (zh) 吡嗪化合物和其用途
CN111747954B (zh) 吡嗪化合物和其用途
HK1172024A (en) Inhibitors of pi3 kinase and/or mtor
HK40074500A (en) Pyrazine compounds and uses thereof
HK40045062B (en) Pyrazine compounds and uses thereof
TWI673268B (zh) 作為fgfr4抑制劑之稠環雙環吡啶基衍生物
HK40045062A (en) Pyrazine compounds and uses thereof
HK40074500B (zh) 吡嗪化合物和其用途
HK40037929B (en) Pyrazine compounds and uses thereof
HK40037929A (en) Pyrazine compounds and uses thereof
HK40038625A (en) Pyrazine compounds and uses thereof
HK1167862B (en) Inhibitors of pi3 kinase and / or mtor
HK1236197B (en) Tank-binding kinase inhibitor compounds
HK1236197A1 (en) Tank-binding kinase inhibitor compounds

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1172024

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20151125

Termination date: 20170427

CF01 Termination of patent right due to non-payment of annual fee
REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1172024

Country of ref document: HK