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EA201171030A1 - 2-МОРФОЛИНОПИРИДО[3,2-d]ПИРИМИДИНЫ - Google Patents

2-МОРФОЛИНОПИРИДО[3,2-d]ПИРИМИДИНЫ

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Publication number
EA201171030A1
EA201171030A1 EA201171030A EA201171030A EA201171030A1 EA 201171030 A1 EA201171030 A1 EA 201171030A1 EA 201171030 A EA201171030 A EA 201171030A EA 201171030 A EA201171030 A EA 201171030A EA 201171030 A1 EA201171030 A1 EA 201171030A1
Authority
EA
Eurasian Patent Office
Prior art keywords
morfolinopirido
pyrimidines
diseases
cancer
compounds
Prior art date
Application number
EA201171030A
Other languages
English (en)
Inventor
Сирил Монтань
Аньес Бомбрэн
Гвенаэлль Дефорж
Анна Кваттропани
Паскаль Гайяр
Original Assignee
Мерк Сероно С.А.
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 Мерк Сероно С.А. filed Critical Мерк Сероно С.А.
Publication of EA201171030A1 publication Critical patent/EA201171030A1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • 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
    • 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
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • 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
    • A61P7/06—Antianaemics
    • 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
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Virology (AREA)
  • Vascular Medicine (AREA)
  • Psychology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Transplantation (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)

Abstract

Настоящее изобретение относится к соединениям формулы (I) в качестве ингибиторов Pi3K для лечения аутоиммунных заболеваний, воспалительных расстройств, рассеянного склероза и других заболеваний, таких как рак.
EA201171030A 2009-02-12 2010-02-04 2-МОРФОЛИНОПИРИДО[3,2-d]ПИРИМИДИНЫ EA201171030A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09152709 2009-02-12
US20774409P 2009-02-17 2009-02-17
PCT/EP2010/051373 WO2010091996A1 (en) 2009-02-12 2010-02-04 2-morpholino-pyrido[3,2-d]pyrimidines

Publications (1)

Publication Number Publication Date
EA201171030A1 true EA201171030A1 (ru) 2012-03-30

Family

ID=40521722

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201171030A EA201171030A1 (ru) 2009-02-12 2010-02-04 2-МОРФОЛИНОПИРИДО[3,2-d]ПИРИМИДИНЫ

Country Status (15)

Country Link
US (1) US8609666B2 (ru)
EP (1) EP2396322B9 (ru)
JP (1) JP5667086B2 (ru)
KR (1) KR20110115160A (ru)
CN (1) CN102388041B (ru)
AR (1) AR075393A1 (ru)
AU (1) AU2010213014B2 (ru)
CA (1) CA2751501C (ru)
EA (1) EA201171030A1 (ru)
ES (1) ES2570456T3 (ru)
IL (1) IL214450A0 (ru)
MX (1) MX2011008505A (ru)
SG (1) SG173155A1 (ru)
WO (1) WO2010091996A1 (ru)
ZA (1) ZA201105528B (ru)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102911172A (zh) * 2011-08-04 2013-02-06 上海恒瑞医药有限公司 杂芳基并嘧啶类衍生物、其制备方法和用途

Family Cites Families (24)

* Cited by examiner, † Cited by third party
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DE2117657B2 (de) * 1971-04-10 1976-04-08 Dr. Karl Thomae Gmbh, 7950 Biberach Pyrido eckige klammer auf 3,2- d eckige klammer zu pyrimidine
DE2208534A1 (de) * 1972-02-23 1973-08-30 Thomae Gmbh Dr K Neue pyrido eckige klammer auf 3,2-d eckige klammer zu pyrimidin
DE2208535A1 (de) * 1972-02-23 1973-08-30 Thomae Gmbh Dr K Neue pyrido eckige klammer auf 3,2-d eckige klammer zu pyrimidine
DE2202367A1 (de) * 1972-01-19 1973-08-02 Thomae Gmbh Dr K Neues verfahren zur herstellung von pyrido eckige klammer auf 3,2-d eckige klammer zu pyrimidinen
JPH075594B2 (ja) * 1986-03-25 1995-01-25 三井石油化学工業株式会社 新規ピリドピリミジン誘導体
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
JP3649395B2 (ja) 2000-04-27 2005-05-18 山之内製薬株式会社 縮合ヘテロアリール誘導体
BR0312650A (pt) 2002-07-10 2005-05-03 Applied Research Systems Derivados de benzeno fundido azolidinona-vinila
CA2510851A1 (en) 2002-12-20 2004-07-08 Warner-Lambert Company Llc Benzoxazines and derivatives thereof as inhibitors of pi3ks
CA2517802A1 (en) * 2003-03-03 2004-09-16 Arizona Board Of Regents On Behalf Of The University Of Arizona Protein tyrosine phosphatase-prl-1 a a marker and therapeutic target for pancreatic cancer
GB0305152D0 (en) 2003-03-06 2003-04-09 Novartis Ag Organic compounds
GB0320197D0 (en) 2003-08-28 2003-10-01 Novartis Ag Organic compounds
CN101052640B (zh) * 2004-09-03 2011-05-11 默克雪兰诺有限公司 吡啶亚甲基唑烷酮类及其作为磷酸肌醇抑制剂的用途
GB0428475D0 (en) 2004-12-30 2005-02-02 4 Aza Bioscience Nv Pyrido(3,2-D)pyrimidine derivatives and pharmaceutical compositions useful as medicines for the treatment of autoimmune disorders
JP2008526704A (ja) * 2004-12-30 2008-07-24 ４・アー・ゼット・アー・アイ・ピー・ナムローゼ・フエンノートシャップ ピリド（３，２−ｄ）ピリミジンおよび医療処置に有用な医薬組成物
US20090264415A2 (en) 2004-12-30 2009-10-22 Steven De Jonghe Pyrido(3,2-d)pyrimidines and pharmaceutical compositions useful for medical treatment
GB0503506D0 (en) 2005-02-21 2005-03-30 4 Aza Bioscience Nv Substituted pyrido(2,3-d) pyrimidine derivatives and pharmaceutical compositions useful as medicines for the treatment of autoimmune disorders
GB0503961D0 (en) * 2005-02-25 2005-04-06 Kudos Pharm Ltd Compounds
EP1871377A1 (en) * 2005-02-25 2008-01-02 Kudos Pharmaceuticals Ltd 2,4-diamino-pyridopyrimidine derivatives and their use as mtor inhibitors
US8338435B2 (en) 2006-07-20 2012-12-25 Gilead Sciences, Inc. Substituted pyrido(3,2-D) pyrimidines and pharmaceutical compositions for treating viral infections
BRPI0714614A2 (pt) * 2006-07-28 2013-05-14 Novartis Ag quinazolina 2,4-substituÍdas como inibidores de lipÍdeos cinase
MY148688A (en) * 2006-08-23 2013-05-31 Kudos Pharm Ltd 2-methylmorpholine pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mtor inhibitors
TW200840584A (en) 2006-12-26 2008-10-16 Gilead Sciences Inc Pyrido(3,2-d)pyrimidines useful for treating viral infections
UY31137A1 (es) * 2007-06-14 2009-01-05 Smithkline Beecham Corp Derivados de quinazolina como inhibidores de la pi3 quinasa

Also Published As

Publication number Publication date
CA2751501C (en) 2018-01-16
ES2570456T3 (es) 2016-05-18
KR20110115160A (ko) 2011-10-20
JP2012517453A (ja) 2012-08-02
AU2010213014A1 (en) 2011-08-18
EP2396322B9 (en) 2016-09-14
CN102388041B (zh) 2014-12-24
MX2011008505A (es) 2012-10-15
JP5667086B2 (ja) 2015-02-12
AU2010213014B2 (en) 2016-02-25
EP2396322B1 (en) 2016-02-03
EP2396322A1 (en) 2011-12-21
IL214450A0 (en) 2011-09-27
US20110293564A1 (en) 2011-12-01
CN102388041A (zh) 2012-03-21
SG173155A1 (en) 2011-08-29
AR075393A1 (es) 2011-03-30
WO2010091996A1 (en) 2010-08-19
CA2751501A1 (en) 2010-08-19
ZA201105528B (en) 2012-09-26
US8609666B2 (en) 2013-12-17

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