CN101678020B - 作为Janus激酶的酪氨酸激酶活性抑制剂的喹喔啉衍生物 - Google Patents

作为Janus激酶的酪氨酸激酶活性抑制剂的喹喔啉衍生物 Download PDF

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Publication number
CN101678020B
CN101678020B CN2008800193524A CN200880019352A CN101678020B CN 101678020 B CN101678020 B CN 101678020B CN 2008800193524 A CN2008800193524 A CN 2008800193524A CN 200880019352 A CN200880019352 A CN 200880019352A CN 101678020 B CN101678020 B CN 101678020B
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phenyl
quinoxaline
methyl
ylmethyl
morpholine
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CN101678020A (zh
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M·格施帕赫
P·菲雷
E·范格莱维灵格
C·皮索特索德曼
C·高尔
P·霍尔策
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Novartis AG
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Novartis AG
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    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
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  • Animal Behavior & Ethology (AREA)
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  • Diabetes (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN2008800193524A 2007-06-08 2008-06-06 作为Janus激酶的酪氨酸激酶活性抑制剂的喹喔啉衍生物 Expired - Fee Related CN101678020B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP07109880 2007-06-08
EP07109880.0 2007-06-08
EP07150266 2007-12-20
EP07150266.0 2007-12-20
PCT/EP2008/057058 WO2008148867A2 (en) 2007-06-08 2008-06-06 Quinoxaline derivatives as inhibitors of the tyrosine kinase activity of janus kinases

Publications (2)

Publication Number Publication Date
CN101678020A CN101678020A (zh) 2010-03-24
CN101678020B true CN101678020B (zh) 2012-08-15

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CN2008800193524A Expired - Fee Related CN101678020B (zh) 2007-06-08 2008-06-06 作为Janus激酶的酪氨酸激酶活性抑制剂的喹喔啉衍生物

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US (1) US8193189B2 (enExample)
EP (1) EP2155201B1 (enExample)
JP (1) JP5574957B2 (enExample)
KR (1) KR20100020465A (enExample)
CN (1) CN101678020B (enExample)
AR (1) AR066879A1 (enExample)
AU (1) AU2008258486B2 (enExample)
BR (1) BRPI0812893A2 (enExample)
CA (1) CA2690288A1 (enExample)
CL (1) CL2008001659A1 (enExample)
EA (1) EA200901608A1 (enExample)
ES (1) ES2392570T3 (enExample)
MX (1) MX2009013218A (enExample)
PA (1) PA8783501A1 (enExample)
TW (1) TW200904814A (enExample)
UY (1) UY31126A1 (enExample)
WO (1) WO2008148867A2 (enExample)

Families Citing this family (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2411930T3 (es) 2008-02-20 2013-07-09 Actelion Pharmaceuticals Ltd. Compuestos antibióticos azatricíclicos
ES2554513T3 (es) 2008-05-23 2015-12-21 Novartis Ag Derivados de quinolinas y quinoxalinas como inhibidores de la proteína tirosina quinasa
US20110130384A1 (en) * 2008-06-25 2011-06-02 Takeda Pharmaceutical Company Limited Amide compound
MY158520A (en) 2008-10-07 2016-10-14 Actelion Pharmaceuticals Ltd Tricyclic oxazolidinone antibiotic compounds
CA2752150A1 (en) * 2009-02-11 2010-08-19 Reaction Biology Corp. Selective kinase inhibitors
US20140128392A1 (en) 2009-03-19 2014-05-08 Bioenergenix Heterocyclic compounds for the inhibition of pask
KR101650981B1 (ko) * 2009-09-03 2016-08-24 바이오에너제닉스 Ｐａｓｋ의 억제를 위한 복소환 화합물
CN102821759A (zh) 2010-03-30 2012-12-12 诺华有限公司 用于治疗具有慢性活性b细胞受体信号传导的b细胞淋巴瘤的pkc抑制剂
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
JP5980812B2 (ja) * 2011-01-05 2016-08-31 バイオエナジェニックス Ｐａｓｋの阻害のための複素環化合物
US8263298B1 (en) 2011-02-24 2012-09-11 Xerox Corporation Electrically tunable and stable imaging members
EP2727920B1 (en) 2011-07-29 2016-11-02 FUJIFILM Corporation 1,5-naphthyridine derivative or salt thereof
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
MX2014005927A (es) 2011-11-15 2014-06-05 Novartis Ag Combinacion de un inhibidor de la fosfoinositida-3-cinasa y un modulador de la senda del transductor y activador de la señal de transcripcion 5 de la cinasa janus 2.
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
ES2625744T3 (es) 2013-06-04 2017-07-20 Bayer Pharma Aktiengesellschaft Imidazo[1,2-a]piridinas sustituidas con 3-arilo y su uso
EP3060557A1 (de) 2013-10-23 2016-08-31 Bayer CropScience Aktiengesellschaft Substituierte chinoxalin-derivate als schädlingsbekämpfungsmittel
CA2939793A1 (en) 2014-02-19 2015-08-27 Bayer Pharma Aktiengesellschaft 3-(pyrimidine-2-yl)imidazo[1,2-a]pyridines
MX370099B (es) 2014-03-26 2019-12-02 Astex Therapeutics Ltd Combinación que comprende un inhibidor de fgfr y un inhibidor de cmet para el tratamiento del cáncer.
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
KR102479696B1 (ko) 2014-03-26 2022-12-22 아스텍스 테라퓨틱스 리미티드 Fgfr 억제제 및 igf1r 억제제의 조합물
EP3227287B1 (de) 2014-12-02 2019-08-07 Bayer Pharma Aktiengesellschaft Heteroaryl-substituierte imidazo[1,2-a]pyridine und ihre verwendung
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
JP2018525371A (ja) * 2015-07-30 2018-09-06 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ アリール置換された二環式ヘテロアリール化合物
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CA2996857C (en) 2015-09-23 2024-05-21 Janssen Pharmaceutica Nv Quinoxaline, quinoline and quinazolinone derivative compounds for the treatment of cancer
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RU2718902C2 (ru) * 2016-02-24 2020-04-15 Пфайзер Инк. Производные пиразоло[1,5-а]пиразин-4-ила в качестве jak-ингибиторов
WO2018041989A1 (en) 2016-09-02 2018-03-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosing and treating refractory celiac disease type 2
CA3115297A1 (en) 2018-10-10 2020-04-16 Albert Einstein College Of Medicine Benzoxazole and related compounds useful as chaperone-mediated autophagy modulators
CN113710661B (zh) * 2019-04-02 2022-11-22 上海睿跃生物科技有限公司 治疗癌症的化合物和方法
US20220177978A1 (en) 2019-04-02 2022-06-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
EP3955920A1 (en) 2019-04-16 2022-02-23 Institut National de la Santé et de la Recherche Médicale (INSERM) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
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KR20220088699A (ko) 2019-09-27 2022-06-28 디스크 메디슨, 인크. 골수섬유증 및 관련 상태의 치료 방법
CN110981819B (zh) * 2019-12-24 2022-07-01 广西师范大学 一种喹喔啉类信号通路抑制剂及其制备方法和应用
KR20230012539A (ko) 2020-05-13 2023-01-26 디스크 메디슨, 인크. 골수섬유증을 치료하기 위한 항-헤모주벨린 (hjv) 항체
EP4526469A1 (en) 2022-05-16 2025-03-26 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stems cells induced by chronic inflammation
CN115385863A (zh) * 2022-08-17 2022-11-25 河南师范大学 一种3-(二乙氧基甲基)-1-烷基-2(1h)-喹喔啉酮衍生物的合成方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5721248A (en) * 1993-06-24 1998-02-24 Bayer Aktiengesellschaft 4-bicyclically substituted dihydropyridines, and their use in medicaments

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9800836D0 (sv) * 1998-03-13 1998-03-13 Astra Ab New Compounds
ATE400274T1 (de) * 2001-04-10 2008-07-15 Merck & Co Inc Hemmstoffe der akt aktivität
CA2548172A1 (en) * 2003-12-04 2005-06-23 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
WO2007044729A2 (en) * 2005-10-07 2007-04-19 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5721248A (en) * 1993-06-24 1998-02-24 Bayer Aktiengesellschaft 4-bicyclically substituted dihydropyridines, and their use in medicaments

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
DENNY, WILLIAM A. ET AL.Structure-activity relationships for the mutagenic activity of tricyclic intercalating agents in Salmonella typhimurium.《MUTATION RESEARCH, FUMDAMENTAL AND MOLECULAR MECHANISMS OF MUTAGENESIS》.1990,第232卷(第2期), *
Dmitry Aldakov. et al.Dipyrrolyl quinoxalines with extended chromophores are efficient flurimetric sensors for pyrophosphate.《Chemical Communication》.2003, *
ITO Y. et al.New Synthesis of Quinoxaline Derivatives Based on Palladium Catalyzed Oligomerization of 1,2-Diisocyanoarenes.《HETEROCYCLES》.1996,第42卷(第2期),597-615. *
ITOY.etal.NewSynthesisofQuinoxalineDerivativesBasedonPalladiumCatalyzedOligomerizationof1 2-Diisocyanoarenes.《HETEROCYCLES》.1996

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