ES2592219T3 - Derivados de {(4-(4-morfolino-dihidrotieno[3,4-d]pirimidin-2-il)aril}urea o carbamato como inhibidores de mTOR - Google Patents

Derivados de {(4-(4-morfolino-dihidrotieno[3,4-d]pirimidin-2-il)aril}urea o carbamato como inhibidores de mTOR Download PDF

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Publication number
ES2592219T3
ES2592219T3 ES12769098.0T ES12769098T ES2592219T3 ES 2592219 T3 ES2592219 T3 ES 2592219T3 ES 12769098 T ES12769098 T ES 12769098T ES 2592219 T3 ES2592219 T3 ES 2592219T3
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Spain
Prior art keywords
pyrimidin
dioxide
dihydrothiene
phenyl
alkyl
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English (en)
Spanish (es)
Inventor
Rosemary Lynch
Andrew David Cansfield
Daniel Paul HARDY
John Thomas Feutrill
Rita Adrego
Katie Ellard
Tammy LADDUWAHETTY
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Cellzome Ltd
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Cellzome Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—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
    • 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
    • A61K31/535—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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P31/12—Antivirals
    • 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
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychology (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
ES12769098.0T 2011-10-07 2012-10-05 Derivados de {(4-(4-morfolino-dihidrotieno[3,4-d]pirimidin-2-il)aril}urea o carbamato como inhibidores de mTOR Active ES2592219T3 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP11184358 2011-10-07
EP11184358 2011-10-07
US201261649995P 2012-05-22 2012-05-22
US201261649995P 2012-05-22
PCT/EP2012/069676 WO2013050508A1 (en) 2011-10-07 2012-10-05 Morpholino substituted bicyclic pyrimidine urea or carbamate derivatives as mtor inhibitors

Publications (1)

Publication Number Publication Date
ES2592219T3 true ES2592219T3 (es) 2016-11-28

Family

ID=48043187

Family Applications (1)

Application Number Title Priority Date Filing Date
ES12769098.0T Active ES2592219T3 (es) 2011-10-07 2012-10-05 Derivados de {(4-(4-morfolino-dihidrotieno[3,4-d]pirimidin-2-il)aril}urea o carbamato como inhibidores de mTOR

Country Status (12)

Country Link
US (1) US9242993B2 (enExample)
EP (1) EP2763985B1 (enExample)
JP (1) JP5995977B2 (enExample)
KR (1) KR20140084130A (enExample)
CN (1) CN103946222B (enExample)
AU (1) AU2012320465B2 (enExample)
BR (1) BR112014008241A2 (enExample)
CA (1) CA2850852A1 (enExample)
ES (1) ES2592219T3 (enExample)
MX (1) MX341577B (enExample)
RU (1) RU2609208C2 (enExample)
WO (1) WO2013050508A1 (enExample)

Families Citing this family (10)

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EP2542536B1 (en) 2010-03-04 2015-01-21 Cellzome Limited Morpholino substituted urea derivatives as mtor inhibitors
BR112014006743A8 (pt) 2011-09-21 2018-01-09 Cellzome Ltd composto, uso de um composto, e, método para tratar, controlar, retardar ou impedir uma ou mais condições
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
CN106117242B (zh) * 2016-06-27 2018-08-03 山东大学 四氢噻喃并嘧啶类衍生物及其制备方法与应用
FR3075795A1 (fr) * 2017-12-21 2019-06-28 Galderma Research & Development Nouveaux composes inhibiteurs de mtor
AU2019338207B2 (en) 2018-09-10 2025-01-02 Mirati Therapeutics, Inc. Combination therapies
CN111205310B (zh) * 2018-11-22 2023-12-19 上海迪诺医药科技有限公司 杂环稠合嘧啶衍生物、其药物组合物及应用
WO2021143821A1 (zh) * 2020-01-17 2021-07-22 江苏恒瑞医药股份有限公司 稠合杂芳基类衍生物、其制备方法及其在医药上的应用
TWI926033B (zh) 2021-05-11 2026-05-21 美商歐瑞克製藥公司 類polo激酶4抑制劑
GB202415232D0 (en) 2024-10-16 2024-11-27 Nacamed As Composition

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GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
ATE401312T1 (de) 1997-12-15 2008-08-15 Astellas Pharma Inc Pyrimidin-5-carboxamid-derivate
EE05345B1 (et) 1999-02-10 2010-10-15 Astrazeneca Ab Kinasoliini derivaadid angiogeneesi inhibiitoritena
PT1244647E (pt) 1999-11-05 2006-10-31 Astrazeneca Ab Derivados de quinazolina como inibidores de vegf
HRP20020751B1 (hr) 2000-02-15 2011-01-31 Sugen Pirolom supstituirani 2-indolinoni kao inhibitori protein kinaze
IL163771A0 (en) * 2002-02-28 2005-12-18 Novartis Ag N-ä5-Ä4-(4-methyl-piperazino-methyl benzoylamidoÜ--2-methylphenylü-4-(3-pyridyl)-2-pyrimidine-amine coated stents
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JP2010533159A (ja) 2007-07-09 2010-10-21 アストラゼネカ アクチボラグ 化合物947
JP2010533158A (ja) 2007-07-09 2010-10-21 アストラゼネカ アクチボラグ 化合物類−945
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US20140163023A1 (en) 2011-04-04 2014-06-12 Cellzome Limited Dihydropyrrolo pyrimidine derivatives as mtor inhibitors
BR112014006743A8 (pt) 2011-09-21 2018-01-09 Cellzome Ltd composto, uso de um composto, e, método para tratar, controlar, retardar ou impedir uma ou mais condições

Also Published As

Publication number Publication date
EP2763985B1 (en) 2016-06-22
EP2763985A1 (en) 2014-08-13
JP2014528436A (ja) 2014-10-27
CN103946222B (zh) 2016-12-28
AU2012320465B2 (en) 2016-03-03
CN103946222A (zh) 2014-07-23
MX341577B (es) 2016-08-25
WO2013050508A1 (en) 2013-04-11
RU2014109748A (ru) 2015-11-20
KR20140084130A (ko) 2014-07-04
JP5995977B2 (ja) 2016-09-21
CA2850852A1 (en) 2013-04-11
RU2609208C2 (ru) 2017-01-31
MX2014004161A (es) 2014-11-26
AU2012320465A1 (en) 2014-05-08
US9242993B2 (en) 2016-01-26
BR112014008241A2 (pt) 2017-04-18
US20140288066A1 (en) 2014-09-25

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