CN101010317A - 作为磷脂酰肌醇（pi）3－激酶抑制剂的2,4,6－三取代的嘧啶及其在癌症治疗中的用途 - Google Patents

作为磷脂酰肌醇（pi）3－激酶抑制剂的2,4,6－三取代的嘧啶及其在癌症治疗中的用途 Download PDF

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CN101010317A
CN101010317A CNA2005800297623A CN200580029762A CN101010317A CN 101010317 A CN101010317 A CN 101010317A CN A2005800297623 A CNA2005800297623 A CN A2005800297623A CN 200580029762 A CN200580029762 A CN 200580029762A CN 101010317 A CN101010317 A CN 101010317A
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alkyl
group
methyl
amino
base
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Chinese (zh)
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M·帕斯
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AstraZeneca AB
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    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • 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
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/00—Drugs for dermatological disorders
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
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    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
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    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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 chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
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  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
CNA2005800297623A 2004-07-09 2005-07-07 作为磷脂酰肌醇（pi）3－激酶抑制剂的2,4,6－三取代的嘧啶及其在癌症治疗中的用途 Pending CN101010317A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0415367.2A GB0415367D0 (en) 2004-07-09 2004-07-09 Pyrimidine derivatives
GB0415367.2 2004-07-09

Publications (1)

Publication Number Publication Date
CN101010317A true CN101010317A (zh) 2007-08-01

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ID=32865684

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CNA2005800297623A Pending CN101010317A (zh) 2004-07-09 2005-07-07 作为磷脂酰肌醇（pi）3－激酶抑制剂的2,4,6－三取代的嘧啶及其在癌症治疗中的用途

Country Status (18)

Country Link
US (1) US20080051401A1 (https=)
EP (1) EP1778681A1 (https=)
JP (1) JP2008505877A (https=)
KR (1) KR20070032810A (https=)
CN (1) CN101010317A (https=)
AR (1) AR049712A1 (https=)
AU (1) AU2005261555A1 (https=)
BR (1) BRPI0513056A (https=)
CA (1) CA2571756A1 (https=)
GB (1) GB0415367D0 (https=)
IL (1) IL180138A0 (https=)
MX (1) MX2007000118A (https=)
NO (1) NO20070681L (https=)
RU (1) RU2007104838A (https=)
TW (1) TW200618801A (https=)
UY (1) UY29009A1 (https=)
WO (1) WO2006005918A1 (https=)
ZA (1) ZA200700060B (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104718203A (zh) * 2012-08-17 2015-06-17 国家科学研究中心 三取代吡啶并[3,2-d]嘧啶及其制备方法和治疗用途
CN105143209A (zh) * 2013-03-14 2015-12-09 诺华股份有限公司 作为激酶抑制剂的联芳基酰胺化合物

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0415364D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0520657D0 (en) 2005-10-11 2005-11-16 Ludwig Inst Cancer Res Pharmaceutical compounds
GB0525081D0 (en) * 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
GB0525080D0 (en) * 2005-12-09 2006-01-18 Astrazeneca Ab Pyrimidine derivatives
JP2009523161A (ja) * 2006-01-11 2009-06-18 アストラゼネカ アクチボラグ モルホリノピリミジン誘導体と療法におけるその使用
GB0616747D0 (en) * 2006-08-24 2006-10-04 Astrazeneca Ab Novel compounds
JP2010501537A (ja) * 2006-08-24 2010-01-21 アストラゼネカ アクチボラグ 増殖性障害の治療に有用なモルホリノピリミジン誘導体
MX2009002046A (es) * 2006-08-24 2009-03-06 Astrazeneca Ab Derivados de morfolino pirimidina utiles en el tratamiento de trastornos proliferativos.
WO2008032041A1 (en) * 2006-09-14 2008-03-20 Astrazeneca Ab Pyrimidine derivatives having inhibitory activity against pi3k enzymes
CN101809002B (zh) * 2007-07-09 2013-03-27 阿斯利康(瑞典)有限公司 用于与mtor激酶和/或pi3k相关的疾病中的吗啉代嘧啶衍生物
EP2519102B1 (en) * 2009-12-28 2016-10-19 Development Center For Biotechnology NOVEL PYRIMIDINE COMPOUNDS AS mTOR AND PI3K INHIBITORS
SA111320519B1 (ar) 2010-06-11 2014-07-02 Astrazeneca Ab مركبات بيريميدينيل للاستخدام كمثبطات atr
EP2970240B1 (en) 2013-03-14 2018-01-10 Novartis AG 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
AU2017329090B9 (en) 2016-09-19 2019-09-05 Novartis Ag Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor
ES2952265T3 (es) 2017-05-02 2023-10-30 Novartis Ag Terapia combinada que comprende un inhibidor de Raf y trametinib
EP3736266A4 (en) * 2018-01-04 2021-01-06 Peking University Shenzhen Graduate School COMPOUND SIMULTANEOUSLY INHIBITING THE LSD1 AND HDAC TARGETS AND ITS APPLICATION
ES3025633T3 (en) 2019-05-13 2025-06-09 Novartis Ag New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
WO2025255134A1 (en) * 2024-06-04 2025-12-11 Soley Therapeutics, Inc. Piperazinone based modulators for the treatment of disease

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19836697A1 (de) * 1998-08-13 2000-02-17 Hoechst Marion Roussel De Gmbh Substituierte 4-Amino-2-aryl-pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate
CN1186324C (zh) * 2000-04-27 2005-01-26 山之内制药株式会社 稠合杂芳基衍生物

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104718203A (zh) * 2012-08-17 2015-06-17 国家科学研究中心 三取代吡啶并[3,2-d]嘧啶及其制备方法和治疗用途
CN105143209A (zh) * 2013-03-14 2015-12-09 诺华股份有限公司 作为激酶抑制剂的联芳基酰胺化合物
CN105143209B (zh) * 2013-03-14 2018-03-13 诺华股份有限公司 作为激酶抑制剂的联芳基酰胺化合物
CN108467369A (zh) * 2013-03-14 2018-08-31 诺华股份有限公司 作为激酶抑制剂的联芳基酰胺化合物
TWI662025B (zh) * 2013-03-14 2019-06-11 瑞士商諾華公司 用作激酶抑制劑的二芳基醯胺化合物
CN108467369B (zh) * 2013-03-14 2021-08-20 诺华股份有限公司 作为激酶抑制剂的联芳基酰胺化合物

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Publication number Publication date
IL180138A0 (en) 2007-06-03
WO2006005918A1 (en) 2006-01-19
GB0415367D0 (en) 2004-08-11
CA2571756A1 (en) 2006-01-19
TW200618801A (en) 2006-06-16
JP2008505877A (ja) 2008-02-28
BRPI0513056A (pt) 2008-04-22
ZA200700060B (en) 2008-06-25
AR049712A1 (es) 2006-08-30
AU2005261555A1 (en) 2006-01-19
UY29009A1 (es) 2006-02-24
EP1778681A1 (en) 2007-05-02
RU2007104838A (ru) 2008-08-27
US20080051401A1 (en) 2008-02-28
KR20070032810A (ko) 2007-03-22
NO20070681L (no) 2007-03-21
MX2007000118A (es) 2007-03-09

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