CN106946796B - 用作激酶活性调节剂的氨基嘧啶衍生物 - Google Patents

用作激酶活性调节剂的氨基嘧啶衍生物 Download PDF

Info

Publication number
CN106946796B
CN106946796B CN201710022892.9A CN201710022892A CN106946796B CN 106946796 B CN106946796 B CN 106946796B CN 201710022892 A CN201710022892 A CN 201710022892A CN 106946796 B CN106946796 B CN 106946796B
Authority
CN
China
Prior art keywords
phenyl
amino
pyrimidin
ethyl
piperazin
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
CN201710022892.9A
Other languages
English (en)
Chinese (zh)
Other versions
CN106946796A (zh
Inventor
R·蓝
B·R·胡克
X·陈
L·C·德赛尔姆
Y·肖
H·裘
C·尼古
I·莫恰金
T·L·约翰逊
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.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of CN106946796A publication Critical patent/CN106946796A/zh
Application granted granted Critical
Publication of CN106946796B publication Critical patent/CN106946796B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • 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
    • C07D239/49Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • 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
    • 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
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon 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
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201710022892.9A 2011-09-12 2012-09-12 用作激酶活性调节剂的氨基嘧啶衍生物 Expired - Fee Related CN106946796B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161533606P 2011-09-12 2011-09-12
US61/533,606 2011-09-12
CN201280054959.2A CN103930407B (zh) 2011-09-12 2012-09-12 用作激酶活性调节剂的氨基嘧啶衍生物

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201280054959.2A Division CN103930407B (zh) 2011-09-12 2012-09-12 用作激酶活性调节剂的氨基嘧啶衍生物

Publications (2)

Publication Number Publication Date
CN106946796A CN106946796A (zh) 2017-07-14
CN106946796B true CN106946796B (zh) 2020-05-08

Family

ID=46964039

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201280054959.2A Expired - Fee Related CN103930407B (zh) 2011-09-12 2012-09-12 用作激酶活性调节剂的氨基嘧啶衍生物
CN201710022892.9A Expired - Fee Related CN106946796B (zh) 2011-09-12 2012-09-12 用作激酶活性调节剂的氨基嘧啶衍生物

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CN201280054959.2A Expired - Fee Related CN103930407B (zh) 2011-09-12 2012-09-12 用作激酶活性调节剂的氨基嘧啶衍生物

Country Status (24)

Country Link
US (3) US9321760B2 (OSRAM)
EP (1) EP2755958B9 (OSRAM)
JP (1) JP6082011B2 (OSRAM)
KR (1) KR101992505B1 (OSRAM)
CN (2) CN103930407B (OSRAM)
AU (2) AU2012308681B2 (OSRAM)
BR (1) BR112014005468A2 (OSRAM)
CA (1) CA2844704C (OSRAM)
DK (1) DK2755958T3 (OSRAM)
EA (1) EA028057B1 (OSRAM)
ES (1) ES2646759T3 (OSRAM)
HR (1) HRP20171655T1 (OSRAM)
HU (1) HUE034979T2 (OSRAM)
IL (2) IL231381B (OSRAM)
LT (1) LT2755958T (OSRAM)
MX (1) MX347241B (OSRAM)
NO (1) NO2639780T3 (OSRAM)
PL (1) PL2755958T3 (OSRAM)
PT (1) PT2755958T (OSRAM)
RS (1) RS56486B1 (OSRAM)
SG (1) SG2014009260A (OSRAM)
SI (1) SI2755958T1 (OSRAM)
WO (1) WO2013040044A1 (OSRAM)
ZA (1) ZA201401007B (OSRAM)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LT2718270T (lt) 2011-06-10 2022-08-10 Merck Patent Gmbh Pirimidino ir piridino junginių, turinčių btk inhibitorinį aktyvumą, kompozicijos ir gamybos būdai
SI2755958T1 (sl) * 2011-09-12 2017-12-29 Merck Patent Gmbh Aminopirimidinski derivati za uporabo kot modulatorji kinazne aktivnosti
US9580443B2 (en) 2012-11-16 2017-02-28 Merck Patent Gmbh Heterocyclic derivatives as modulators of kinase activity
US9458134B2 (en) 2013-03-11 2016-10-04 Merck Patent Gmbh Heterocycles as modulators of kinase activity
EP3094629B1 (en) 2014-01-17 2018-08-22 Novartis AG 1-(triazin-3-yl/pyridazin-3-yl)-piper(-azine)idine derivatives and compositions thereof for inhibiting the activity of shp2
JO3517B1 (ar) 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
EP3094627B1 (en) 2014-01-17 2018-08-22 Novartis AG 1-pyridazin-/triazin-3-yl-piper(-azine)/idine/pyrolidine derivatives and and compositions thereof for inhibiting the activity of shp2
AU2015217397B2 (en) * 2014-02-11 2019-01-17 Merck Patent Gmbh Pyrimidine imidazole amines as modulators of kinase activity
EP3420792B1 (en) 2014-04-30 2021-09-22 LG Electronics Inc. Lawn mower robot and control method thereof
CA2948444C (en) 2014-05-28 2022-07-26 Astrazeneca Ab Processes for the preparation of azd5363 and intermediate used therein
US10308660B2 (en) 2015-06-19 2019-06-04 Novartis Ag Compounds and compositions for inhibiting the activity of SHP2
WO2016203404A1 (en) 2015-06-19 2016-12-22 Novartis Ag Compounds and compositions for inhibiting the activity of shp2
EP3310774B1 (en) 2015-06-19 2020-04-29 Novartis AG Compounds and compositions for inhibiting the activity of shp2
WO2017019804A2 (en) 2015-07-28 2017-02-02 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
AU2017232610B2 (en) * 2016-03-16 2021-07-22 Plexxikon Inc. Compounds and methods for kinase modulation and indications therefore
RU2744988C2 (ru) 2016-06-14 2021-03-17 Новартис Аг Соединения и композиции для подавления активности shp2
ES2964956T3 (es) 2017-01-10 2024-04-10 Novartis Ag Combinación farmacéutica que comprende un inhibidor de ALK y un inhibidor de SHP2
CN109467538A (zh) 2017-09-07 2019-03-15 和记黄埔医药(上海)有限公司 环烯烃取代的杂芳环类化合物及其用途
US11369608B2 (en) 2017-10-27 2022-06-28 University Of Virginia Patent Foundation Compounds and methods for regulating, limiting, or inhibiting AVIL expression
US20220213055A1 (en) * 2019-05-02 2022-07-07 University Of Virginia Patent Foundation Substituted (piperidin-1-yl)aryl analogues for modulating avil activity
US11866421B2 (en) 2021-05-31 2024-01-09 Epigen Biosciences, Inc. Pyrimidine and pyridine amine compounds and usage thereof in disease treatment

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006071819A1 (en) * 2004-12-28 2006-07-06 Exelixis, Inc. [1h-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases
CN102786482A (zh) * 2003-11-21 2012-11-21 阿雷生物药品公司 Akt蛋白激酶抑制剂

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020137755A1 (en) * 2000-12-04 2002-09-26 Bilodeau Mark T. Tyrosine kinase inhibitors
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
JP2006522124A (ja) 2003-04-03 2006-09-28 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のインヒビターとして有用な組成物
CN100412066C (zh) 2003-09-30 2008-08-20 Irm责任有限公司 用作蛋白激酶抑制剂的化合物和组合物
EP1678168B1 (en) 2003-10-24 2012-07-11 Exelixis, Inc. P70s6 kinase modulators and method of use
WO2005054237A1 (en) 2003-11-21 2005-06-16 Novartis Ag 1h-imidazoquinoline derivatives as protein kinase inhibitors
ATE447957T1 (de) 2003-12-09 2009-11-15 Us Gov Health & Human Serv Verfahren zur unterdrückung einer immunantwort oder zur behandlung von proliferativen erkrankungen
US8076338B2 (en) 2004-04-23 2011-12-13 Exelixis, Inc. Kinase modulators and methods of use
AU2006206246A1 (en) 2005-01-19 2006-07-27 Neurogen Corporation Heteroaryl substituted piperazinyl-pyridine analogues
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
JP2008546751A (ja) 2005-06-22 2008-12-25 アステックス・セラピューティクス・リミテッド 医薬組成物
DK3421471T3 (da) * 2006-04-25 2021-06-14 Astex Therapeutics Ltd Purin- og deazapurinderivater som farmaceutiske forbindelser
WO2008012635A2 (en) * 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
US8044041B2 (en) * 2006-11-15 2011-10-25 Forest Laboratories Holdings Limited Phthalazine derivatives as inhibitors of protein kinase
WO2008075172A2 (en) * 2006-12-19 2008-06-26 Pfizer Products Inc. Nicotinamide derivatives as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ
AR074072A1 (es) 2008-11-11 2010-12-22 Lilly Co Eli Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme
WO2010093419A1 (en) 2009-02-11 2010-08-19 Merck Patent Gmbh Novel amino azaheterocyclic carboxamides
WO2011029043A1 (en) * 2009-09-04 2011-03-10 Biogen Idec Ma Inc. Heteroaryl btk inhibitors
UA110113C2 (xx) 2010-07-29 2015-11-25 Біциклічні азагетероциклічні карбоксаміди
ES2729754T3 (es) 2010-07-29 2019-11-06 Merck Patent Gmbh Carboxamidas azaheterocíclicas de aminas cíclicas
PL2643313T3 (pl) 2010-11-24 2017-03-31 Merck Patent Gmbh Azetydyny chinazolino-karboksyamidowe
SG10201606301YA (en) * 2011-09-12 2016-09-29 Merck Patent Gmbh Novel imidazole amines as modulators of kinase activity
SI2755958T1 (sl) * 2011-09-12 2017-12-29 Merck Patent Gmbh Aminopirimidinski derivati za uporabo kot modulatorji kinazne aktivnosti
ES2807539T3 (es) * 2012-11-16 2021-02-23 Merck Patent Gmbh Derivados de imidazol-piperidinilo como moduladores de la actividad de quinasa
AU2015217397B2 (en) * 2014-02-11 2019-01-17 Merck Patent Gmbh Pyrimidine imidazole amines as modulators of kinase activity

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102786482A (zh) * 2003-11-21 2012-11-21 阿雷生物药品公司 Akt蛋白激酶抑制剂
WO2006071819A1 (en) * 2004-12-28 2006-07-06 Exelixis, Inc. [1h-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Solid Phase Synthesis of Diamino-Substituted Pyrimidines;Caterina Barillari 等;《 European Journal of Organic Chemistry》;20011126;第24卷;4737–4741 *

Also Published As

Publication number Publication date
EP2755958B9 (en) 2018-02-28
IL266510A (en) 2019-07-31
KR101992505B1 (ko) 2019-06-24
JP6082011B2 (ja) 2017-02-15
HUE034979T2 (en) 2018-05-02
JP2014527082A (ja) 2014-10-09
DK2755958T3 (en) 2017-09-25
MX2014002836A (es) 2014-05-28
EP2755958A1 (en) 2014-07-23
CN103930407B (zh) 2019-02-26
ZA201401007B (en) 2018-07-25
SG2014009260A (en) 2014-09-26
SI2755958T1 (sl) 2017-12-29
US20170217905A1 (en) 2017-08-03
AU2012308681A1 (en) 2014-02-27
BR112014005468A2 (pt) 2017-03-21
RS56486B1 (sr) 2018-01-31
HRP20171655T1 (hr) 2017-12-15
IL266510B (en) 2021-01-31
KR20140062494A (ko) 2014-05-23
MX347241B (es) 2017-04-20
HK1198168A1 (en) 2015-03-13
CA2844704A1 (en) 2013-03-21
ES2646759T3 (es) 2017-12-15
NO2639780T3 (OSRAM) 2018-06-23
IL231381A0 (en) 2014-04-30
PL2755958T3 (pl) 2017-12-29
WO2013040044A1 (en) 2013-03-21
US9321760B2 (en) 2016-04-26
AU2017245469A1 (en) 2017-11-02
PT2755958T (pt) 2017-11-14
AU2012308681B2 (en) 2017-07-13
US10080750B2 (en) 2018-09-25
CN106946796A (zh) 2017-07-14
LT2755958T (lt) 2017-11-10
IL231381B (en) 2019-05-30
CN103930407A (zh) 2014-07-16
EA028057B1 (ru) 2017-10-31
US20160184308A1 (en) 2016-06-30
US20150126484A1 (en) 2015-05-07
CA2844704C (en) 2020-04-28
EP2755958B1 (en) 2017-08-09
US9662330B2 (en) 2017-05-30
AU2017245469B2 (en) 2019-05-23
EA201400338A1 (ru) 2014-12-30

Similar Documents

Publication Publication Date Title
CN106946796B (zh) 用作激酶活性调节剂的氨基嘧啶衍生物
AU2011334173B2 (en) Quinazoline carboxamide azetidines
EP2598497B1 (en) Cyclic amine azaheterocyclic carboxamides
CN113993866A (zh) 杂芳基衍生物、其制备方法、及含其作为有效成分的药物组合物
CN104080782A (zh) 用作激酶活性调节剂的新颖的咪唑胺
CA2902755C (en) 6-[4-(1h-imidazol-2-yl)piperidin-1-yl]pyrimidin-4-amine derivatives as modulators of kinase activity
HK1240220A1 (en) Aminopyrimidine derivatives for use as modulators of kinase activity
HK1198168B (zh) 用作激酶活性调节剂的氨基嘧啶衍生物
HK1201829B (en) Novel heterocyclic carboxamides as modulators of kinase activity
HK1188444B (en) Quinazoline carboxamide azetidines
HK1201829A1 (en) Novel heterocyclic carboxamides as modulators of kinase activity
HK1201825B (en) Imidazole amines as modulators of kinase activity
HK1185077B (en) Cyclic amine azaheterocyclic carboxamides

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for 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: 1240220

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1240220

Country of ref document: HK

CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20200508