CN103068828B - 三唑并吡嗪衍生物 - Google Patents

三唑并吡嗪衍生物 Download PDF

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Publication number
CN103068828B
CN103068828B CN201180041643.5A CN201180041643A CN103068828B CN 103068828 B CN103068828 B CN 103068828B CN 201180041643 A CN201180041643 A CN 201180041643A CN 103068828 B CN103068828 B CN 103068828B
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China
Prior art keywords
triazolo
phenyl
pyrazin
amine
hplc purity
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Expired - Fee Related
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CN201180041643.5A
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English (en)
Chinese (zh)
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CN103068828A (zh
Inventor
L.布格多夫
M.舒尔茨
C.多奇
H.科马斯
D.斯温南
V.波梅尔
P.加亚尔
B.霍杜斯
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Merck Patent GmbH
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Merck Patent GmbH
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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
    • A61K31/535—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
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Otolaryngology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CN201180041643.5A 2010-08-27 2011-07-29 三唑并吡嗪衍生物 Expired - Fee Related CN103068828B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10008927.5 2010-08-27
EP10008927 2010-08-27
PCT/EP2011/003830 WO2012025186A1 (en) 2010-08-27 2011-07-29 Triazolopyrazine derivatives

Publications (2)

Publication Number Publication Date
CN103068828A CN103068828A (zh) 2013-04-24
CN103068828B true CN103068828B (zh) 2015-09-09

Family

ID=44629489

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180041643.5A Expired - Fee Related CN103068828B (zh) 2010-08-27 2011-07-29 三唑并吡嗪衍生物

Country Status (15)

Country Link
US (1) US9023851B2 (https=)
EP (1) EP2609098B1 (https=)
JP (1) JP5951610B2 (https=)
KR (1) KR20130110163A (https=)
CN (1) CN103068828B (https=)
AR (1) AR082726A1 (https=)
AU (1) AU2011295440B2 (https=)
BR (1) BR112013004517A2 (https=)
CA (1) CA2809331C (https=)
EA (1) EA201300282A1 (https=)
ES (1) ES2614128T3 (https=)
IL (1) IL224869A (https=)
MX (1) MX2013002198A (https=)
SG (1) SG188296A1 (https=)
WO (1) WO2012025186A1 (https=)

Families Citing this family (19)

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CN104114557B (zh) * 2012-02-21 2017-10-24 默克专利股份公司 作为syk酪氨酸激酶抑制剂和gcn2丝氨酸激酶抑制剂的8‑取代2‑氨基‑[1,2,4]三唑并[1,5‑a]吡嗪
US20150051202A1 (en) * 2012-03-07 2015-02-19 Merck Patent Gmbh Triazolopyrazine derivatives
CN104704129A (zh) 2012-07-24 2015-06-10 药品循环公司 与对布鲁顿酪氨酸激酶(btk)抑制剂的抗性相关的突变
CA2880326A1 (en) * 2012-10-26 2014-05-01 F. Hoffmann-La Roche Ag 3,4-disubstituted 1 h-pyrazole and 4,5-disubstituted thiazole inhibitors of syk cap
EP2964648B1 (en) * 2013-03-05 2016-11-16 Merck Patent GmbH 9-(aryl or heteroaryl)-2-(pyrazolyl, pyrrolidinyl or cyclopentyl)aminopurine derivatives as anticancer agents
AU2014224975B2 (en) * 2013-03-05 2017-09-14 Merck Patent Gmbh Triazolo(4,5-d)pyrimidine derivatives for the treatment of diseases such as cancer
WO2014180524A1 (en) * 2013-05-06 2014-11-13 Merck Patent Gmbh Macrocycles as kinase inhibitors
WO2015017402A1 (en) * 2013-07-29 2015-02-05 Board Of Regents Of The University Of Nebraska Compositions and methods for the treatment of biofilm infections
EP3137454A1 (en) 2014-04-28 2017-03-08 Pfizer Inc. Heteroaromatic compounds and their use as dopamine d1 ligands
KR101756934B1 (ko) 2014-07-08 2017-07-12 연세대학교 산학협력단 피롤로[1,2-a]피라진 유도체, 이의 약학적으로 허용가능한 염, 이들 화합물의 제조방법 및 이를 유효성분으로 함유하는 골다공증 치료 또는 예방용 약학조성물
CN114989205A (zh) 2016-12-22 2022-09-02 卡里塞拉生物科学股份公司 用于抑制精氨酸酶活性的组合物和方法
TWI877770B (zh) 2018-02-27 2025-03-21 美商英塞特公司 作為a2a / a2b抑制劑之咪唑并嘧啶及三唑并嘧啶
EP3810610A1 (en) 2018-05-18 2021-04-28 Incyte Corporation Fused pyrimidine derivatives as a2a / a2b inhibitors
WO2020010197A1 (en) 2018-07-05 2020-01-09 Incyte Corporation Fused pyrazine derivatives as a2a / a2b inhibitors
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
TW202202498A (zh) * 2020-07-01 2022-01-16 大陸商四川海思科製藥有限公司 一種並環雜環衍生物及其在醫藥上的應用

Citations (7)

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WO2006096270A1 (en) * 2005-02-03 2006-09-14 Vertex Pharmaceuticals Incorporated Pyrrolopyrimidines useful as inhibitors of protein kinase
WO2007085188A1 (en) * 2006-01-27 2007-08-02 Shanghai Hengrui Pharmaceutical Co. Ltd. Pyrrolo [3,2-c] pyridine-4-one 2-indolinone protein kinase inhibitors
WO2008057994A2 (en) * 2006-11-03 2008-05-15 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
WO2009155551A1 (en) * 2008-06-20 2009-12-23 Genentech, Inc. Triazolopyridine jak inhibitor compounds and methods
WO2010027500A1 (en) * 2008-09-08 2010-03-11 Signal Pharmaceuticals, Llc Aminotriazolopyridines and their use as kinase inhibitors
WO2011086098A1 (en) * 2010-01-15 2011-07-21 Ortho-Mcneil-Janssen Pharmaceuticals, Inc Novel substituted bicyclic triazole derivatives as gamma secretase modulators
CN102762561A (zh) * 2010-02-01 2012-10-31 霍夫曼-拉罗奇有限公司 γ分泌酶调节物

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JP4652906B2 (ja) * 2005-06-30 2011-03-16 富士夫 宮脇 振動型マイクロインジェクション装置
US7834024B2 (en) 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
GB0719803D0 (en) 2007-10-10 2007-11-21 Cancer Rec Tech Ltd Therapeutic compounds and their use
SG165655A1 (en) 2008-04-16 2010-11-29 Portola Pharm Inc 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors
WO2009155565A1 (en) 2008-06-20 2009-12-23 Genentech, Inc. Triazolopyridine jak inhibitor compounds and methods
WO2010010184A1 (en) 2008-07-25 2010-01-28 Galapagos Nv [1, 2, 4] triazolo [1, 5-a] pyridines as jak inhibitors
WO2010010189A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases
WO2010010188A1 (en) 2008-07-25 2010-01-28 Galapagos Nv Novel compounds useful for the treatment of degenerative and inflammatory diseases.
EP2438066A2 (en) * 2009-06-05 2012-04-11 Cephalon, Inc. PREPARATION AND USES OF 1,2,4-TRIAZOLO [1,5a]PYRIDINE DERIVATIVES

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006096270A1 (en) * 2005-02-03 2006-09-14 Vertex Pharmaceuticals Incorporated Pyrrolopyrimidines useful as inhibitors of protein kinase
WO2007085188A1 (en) * 2006-01-27 2007-08-02 Shanghai Hengrui Pharmaceutical Co. Ltd. Pyrrolo [3,2-c] pyridine-4-one 2-indolinone protein kinase inhibitors
WO2008057994A2 (en) * 2006-11-03 2008-05-15 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
WO2009155551A1 (en) * 2008-06-20 2009-12-23 Genentech, Inc. Triazolopyridine jak inhibitor compounds and methods
WO2010027500A1 (en) * 2008-09-08 2010-03-11 Signal Pharmaceuticals, Llc Aminotriazolopyridines and their use as kinase inhibitors
WO2011086098A1 (en) * 2010-01-15 2011-07-21 Ortho-Mcneil-Janssen Pharmaceuticals, Inc Novel substituted bicyclic triazole derivatives as gamma secretase modulators
CN102762561A (zh) * 2010-02-01 2012-10-31 霍夫曼-拉罗奇有限公司 γ分泌酶调节物

Also Published As

Publication number Publication date
CA2809331A1 (en) 2012-03-01
JP2013538214A (ja) 2013-10-10
EP2609098A1 (en) 2013-07-03
EP2609098B1 (en) 2016-07-13
WO2012025186A1 (en) 2012-03-01
CN103068828A (zh) 2013-04-24
BR112013004517A2 (pt) 2016-06-07
KR20130110163A (ko) 2013-10-08
CA2809331C (en) 2018-09-25
US9023851B2 (en) 2015-05-05
SG188296A1 (en) 2013-04-30
JP5951610B2 (ja) 2016-07-13
AU2011295440B2 (en) 2015-06-11
AR082726A1 (es) 2012-12-26
EA201300282A1 (ru) 2013-08-30
IL224869A (en) 2016-06-30
AU2011295440A1 (en) 2013-04-11
US20130225568A1 (en) 2013-08-29
MX2013002198A (es) 2013-03-18
ES2614128T3 (es) 2017-05-29

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