PE20121527A1 - 5-alquinil-pirimidinas - Google Patents

5-alquinil-pirimidinas

Info

Publication number
PE20121527A1
PE20121527A1 PE2012001051A PE2012001051A PE20121527A1 PE 20121527 A1 PE20121527 A1 PE 20121527A1 PE 2012001051 A PE2012001051 A PE 2012001051A PE 2012001051 A PE2012001051 A PE 2012001051A PE 20121527 A1 PE20121527 A1 PE 20121527A1
Authority
PE
Peru
Prior art keywords
cycloalkyl
alkinyl
pyrimidines
compounds
don
Prior art date
Application number
PE2012001051A
Other languages
English (en)
Inventor
Siegfried Schneider
Dirk Kessler
Der Veen Lars Van
Tobias Wunberg
Original Assignee
Boehringer Ingelheim Int
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42140100&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20121527(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of PE20121527A1 publication Critical patent/PE20121527A1/es

Links

Classifications

    • 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
    • C07D413/14—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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • 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
    • C07D471/10—Spiro-condensed systems
    • 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
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
    • 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
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE 5-ALQUINIL-PIRIMIDINAS DE FORMULA (1) DONDE R1 ES CICLOALQUILO(C3-C8), HETEROCICLOALQUILO DE 3 A 13 MIEMBROS O HETEROALQUILO DE 2 A 6 MIEMBROS OPCIONALMENTE SUSTITUIDO CON R5, DONDE R5 ES Ra5 O Rb5, EN DONDE Ra5 ES H, ALQUILO(C1-C6), HALOALQUILO(C1-C6), ARILO(C6-C10), ENTRE OTROS; Rb5 ES =O, HALOALQUILOXI(C1-C3), OCF3, CF3, ENTRE OTROS; R2 ES H, ALQUILO(C1-C4), HALOALQUILO(C1-C4), CICLOALQUILO(C3-C8), ENTRE OTROS; R3 ES CICLOALQUILO(C3-C8), HETEROCICLOALQUILO DE 3 A 8 MIEMBROS, ARILO(C6-C10), ENTRE OTROS. SON COMPUESTOS PREFERIDOS LOS DE FORMULA: (a), (b), ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA FOSFATIDILINOSITOL-3-QUINASA (PI3K?) Y mTOR SIENDO UTILES EN EL TRATAMIENTO DE CANCER
PE2012001051A 2010-01-26 2011-01-26 5-alquinil-pirimidinas PE20121527A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10151722 2010-01-26

Publications (1)

Publication Number Publication Date
PE20121527A1 true PE20121527A1 (es) 2012-11-21

Family

ID=42140100

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012001051A PE20121527A1 (es) 2010-01-26 2011-01-26 5-alquinil-pirimidinas

Country Status (23)

Country Link
US (1) US8618111B2 (es)
EP (1) EP2528910B1 (es)
JP (1) JP5670479B2 (es)
KR (1) KR20130030742A (es)
CN (1) CN102781931A (es)
AP (1) AP2012006361A0 (es)
AR (1) AR080019A1 (es)
AU (1) AU2011209343A1 (es)
BR (1) BR112012018454A2 (es)
CA (1) CA2787396A1 (es)
CL (1) CL2012001926A1 (es)
CO (1) CO6592046A2 (es)
EA (1) EA201201049A1 (es)
EC (1) ECSP12012110A (es)
IN (1) IN2012DN06600A (es)
MA (1) MA33938B1 (es)
MX (1) MX2012008359A (es)
PE (1) PE20121527A1 (es)
SG (1) SG182676A1 (es)
TN (1) TN2012000370A1 (es)
TW (1) TW201139412A (es)
UY (1) UY33198A (es)
WO (1) WO2011092197A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY33199A (es) * 2010-01-26 2011-08-31 Boehringer Ingelheim Int 5-alquinil-pirimidinas.
US8466162B2 (en) * 2011-01-26 2013-06-18 Boehringer Ingelheim International Gmbh 5-alkynyl-pyridines

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3832570A1 (de) 1988-09-24 1990-03-29 Hoechst Ag 7-substituierte derivate der 3,5-dihydroxyhept-6-insaeure, verfahren zur ihrer herstellung, ihre verwendung als arzneimittel, sowie zwischenprodukte
JPH08504798A (ja) 1992-12-18 1996-05-21 ザ ウエルカム ファウンデーション リミテッド 酵素阻害薬としての，ピリミジン，ピリジン，プテリジノンおよびインダゾール誘導体
US5622954A (en) 1994-05-11 1997-04-22 Fmc Corporation 5[W(substituted aryl)alkenylene and alkynylene]-2,4-diaminopyrimidines as pesticides
DK1303495T3 (da) * 2000-07-24 2010-09-20 Krenitsky Pharmaceuticals Inc Substituerede 5-alkylnylpyrimidiner med neurotrofisk aktivitet
AU2004221812B2 (en) * 2003-03-19 2010-02-18 Exelixis Inc. Tie-2 modulators and methods of use
WO2005016914A1 (en) * 2003-08-14 2005-02-24 Smithkline Beecham Corporation Chemical compounds
EP1737462B1 (en) * 2003-12-24 2008-07-30 AstraZeneca AB Pyrimidines with tie2 (tek) activity
US7776869B2 (en) 2004-10-18 2010-08-17 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
WO2006082373A1 (en) 2005-02-01 2006-08-10 Astrazeneca Ab Pyrimidine compounds having ties (tek) inhibitory activity
EP1846399A1 (en) 2005-02-01 2007-10-24 AstraZeneca AB Pyrimidine compounds having tie2 (tek) inhibitory activity
GB0502418D0 (en) * 2005-02-05 2005-03-16 Astrazeneca Ab Compounds
US20070135437A1 (en) 2005-03-04 2007-06-14 Alsgen, Inc. Modulation of neurodegenerative diseases
WO2006106721A1 (ja) * 2005-03-30 2006-10-12 Shionogi & Co., Ltd. チロシンキナーゼ阻害作用を有するピリミジン誘導体
WO2006103449A2 (en) 2005-03-31 2006-10-05 Astrazeneca Ab Saminopyrimidine derivates with tie2 inhibiting activity
AU2007204208A1 (en) * 2006-01-11 2007-07-19 Astrazeneca Ab Morpholino pyrimidine derivatives and their use in therapy
GB0616747D0 (en) * 2006-08-24 2006-10-04 Astrazeneca Ab Novel compounds
US20090325957A1 (en) 2006-08-24 2009-12-31 Astrazeneca Ab Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders
AU2007341228B2 (en) 2006-12-29 2013-04-18 Janssen Sciences Ireland Uc HIV inhibiting 5,6-substituted pyrimidines
EP2022785A1 (en) 2007-06-20 2009-02-11 Bayer Schering Pharma Aktiengesellschaft Alkynylpyrimidines as Tie2 kinase inhibitors
UY32009A (es) * 2008-07-29 2010-02-26 Boehringer Ingelheim Int 5-alquinil-pirimidinas
JP2010018601A (ja) * 2009-02-16 2010-01-28 Tetsuya Nishio 複素環化合物、その製造法および用途
UY33199A (es) * 2010-01-26 2011-08-31 Boehringer Ingelheim Int 5-alquinil-pirimidinas.

Also Published As

Publication number Publication date
EP2528910A1 (en) 2012-12-05
CL2012001926A1 (es) 2012-11-30
CA2787396A1 (en) 2011-08-04
MA33938B1 (fr) 2013-01-02
EA201201049A1 (ru) 2013-02-28
KR20130030742A (ko) 2013-03-27
AP2012006361A0 (en) 2012-08-31
SG182676A1 (en) 2012-08-30
AU2011209343A1 (en) 2012-08-02
JP5670479B2 (ja) 2015-02-18
EP2528910B1 (en) 2015-03-18
CO6592046A2 (es) 2013-01-02
US8618111B2 (en) 2013-12-31
BR112012018454A2 (pt) 2016-04-19
MX2012008359A (es) 2012-08-08
TN2012000370A1 (en) 2014-01-30
ECSP12012110A (es) 2012-09-28
TW201139412A (en) 2011-11-16
AR080019A1 (es) 2012-03-07
IN2012DN06600A (es) 2015-10-23
US20120028958A1 (en) 2012-02-02
WO2011092197A1 (en) 2011-08-04
UY33198A (es) 2011-08-31
CN102781931A (zh) 2012-11-14
JP2013518078A (ja) 2013-05-20

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