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PE20040156A1 - 2-HETEROARYL-PYRIMIDINES AS INHIBITORS OF CYCLINE-DEPENDENT KINASE - Google Patents

2-HETEROARYL-PYRIMIDINES AS INHIBITORS OF CYCLINE-DEPENDENT KINASE

Info

Publication number
PE20040156A1
PE20040156A1 PE2003000240A PE2003000240A PE20040156A1 PE 20040156 A1 PE20040156 A1 PE 20040156A1 PE 2003000240 A PE2003000240 A PE 2003000240A PE 2003000240 A PE2003000240 A PE 2003000240A PE 20040156 A1 PE20040156 A1 PE 20040156A1
Authority
PE
Peru
Prior art keywords
ilamino
alkyl
group
butan
triazol
Prior art date
Application number
PE2003000240A
Other languages
Spanish (es)
Inventor
Rolf Jautelat
Olaf Prien
Alexander Ernst
Gerhard Siemeister
Martin Kruger
Ulrich Lucking
Original Assignee
Schering Ag
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
Priority claimed from DE2002112100 external-priority patent/DE10212100A1/en
Priority claimed from DE10255984A external-priority patent/DE10255984A1/en
Application filed by Schering Ag filed Critical Schering Ag
Publication of PE20040156A1 publication Critical patent/PE20040156A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • 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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D401/12—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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/12—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 linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE 2-HETEROARIL-PIRIMIDINAS DE FORMULA I DONDE Q ES EL GRUPO (a) Y EL GRUPO (b) DONDE D, E, G, L, M Y T SON CARBONO, OXIGENO, NITROGENO O AZUFRE, DONDE AL MENOS DEBE ESTAR CONTENIDO EN EL ANILLO UN HETEROATOMO; R1 ES HIDROGENO, HALOGENO, ALQUILO C1-C6, ALQIUINILO C1-C6, ENTRE OTROS; R2 ES HIDROGENO, ALQUILO C1-C10, ALQUENILO C2-C10, ARILO ENTRE OTROS; X ES HALOGENO, OXIGENO, AZUFRE O EL GRUPO NH O N (ALQUILO C1-C3); X Y R2 FORMAN JUNTOS UN ANILLO DE CICLOALQUILO C3-C10, QUE OPCIONALMENTE PUEDE CONTENER UNO O VARIOS HETEROATOMOS; A Y B SON HIDROGENO, HIDROXI, HALOGENO O EL GRUPO -SR7, -S(O)R7 ENTRE OTROS; R7 ES ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, BENCILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (R)-2-[5-BROMO-2-(5-METILSULFANIL-4H-[1,2,4]TRIAZOL-3 ILAMINO)-PIRIMIDIN-4-ILAMINO]-3-METIL-BUTAN-1-OL, (R)-2-[5-BROMO-2-(5-METANSULFINIL-4H-[1,2,4]TRIAZOL-3 ILAMINO)-PIRIMIDIN-4-ILAMINO]-3-METIL-BUTAN-1-OL, (R)-2-[5-BROMO-2-(5-METANSULFONIL-4H-[1,2,4]TRIAZOL-3 ILAMINO)-PIRIMIDIN-4-ILAMINO]-3-METIL-BUTAN-1-OL, ENTRE OTROS. LOS COMPUESTOS MENCIONADOS SON INHIBIDORES SELECTIVOS DE LAS QUINASAS DEPENDIENTES DE LAS CICLINAS Y SON UTILES PARA EL TRATAMIENTO DEL CANCER2-HETEROARYL-PYRIMIDINES OF FORMULA I REFERRED TO WHERE Q IS GROUP (a) AND GROUP (b) WHERE D, E, G, L, MYT ARE CARBON, OXYGEN, NITROGEN OR SULFUR, WHERE AT LEAST IT MUST BE CONTAINED IN THE RING A HETEROATOM; R1 IS HYDROGEN, HALOGEN, C1-C6 ALKYL, C1-C6 ALKYUINYL, AMONG OTHERS; R2 IS HYDROGEN, C1-C10 ALKYL, C2-C10 ALKENYL, ARYL, AMONG OTHERS; X IS HALOGEN, OXYGEN, SULFUR OR THE NH O N GROUP (C1-C3 ALKYL); X AND R2 TOGETHER FORM A C3-C10 CYCLOALKYL RING, WHICH OPTIONALLY MAY CONTAIN ONE OR SEVERAL HETEROATOMS; A AND B ARE HYDROGEN, HYDROXY, HALOGEN OR THE GROUP -SR7, -S (O) R7 AMONG OTHERS; R7 IS C1-C6 ALKYL, C2-C6 ALKYL, C2-C6 ALKYL, BENZYL, AMONG OTHERS. PREFERRED COMPOUNDS ARE: (R) -2- [5-BROMO-2- (5-METHYLSULFANIL-4H- [1,2,4] TRIAZOL-3 ILAMINO) -PYRIMIDIN-4-ILAMINO] -3-METTIL-BUTAN- 1-OL, (R) -2- [5-BROMO-2- (5-METANSULFINYL-4H- [1,2,4] TRIAZOL-3 ILAMINO) -PYRIMIDIN-4-ILAMINO] -3-METIL-BUTAN- 1-OL, (R) -2- [5-BROMO-2- (5-METANSULFONYL-4H- [1,2,4] TRIAZOL-3 ILAMINO) -PYRIMIDIN-4-ILAMINO] -3-METIL-BUTAN- 1-OL, AMONG OTHERS. THE MENTIONED COMPOUNDS ARE SELECTIVE INHIBITORS OF CYCLINE-DEPENDENT KINASES AND ARE USEFUL FOR THE TREATMENT OF CANCER

PE2003000240A 2002-03-11 2003-03-10 2-HETEROARYL-PYRIMIDINES AS INHIBITORS OF CYCLINE-DEPENDENT KINASE PE20040156A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE2002112100 DE10212100A1 (en) 2002-03-11 2002-03-11 New 2-aminopyrimidine derivatives are cyclin-dependent kinase inhibitors useful for treating e.g. cancer, autoimmune diseases, cardiovascular diseases, infectious diseases or viral infections
DE10255984A DE10255984A1 (en) 2002-11-26 2002-11-26 New 2-aminopyrimidine derivatives are cyclin-dependent kinase inhibitors useful for treating e.g. cancer, autoimmune diseases, cardiovascular diseases, infectious diseases or viral infections

Publications (1)

Publication Number Publication Date
PE20040156A1 true PE20040156A1 (en) 2004-06-07

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ID=27806091

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003000240A PE20040156A1 (en) 2002-03-11 2003-03-10 2-HETEROARYL-PYRIMIDINES AS INHIBITORS OF CYCLINE-DEPENDENT KINASE

Country Status (8)

Country Link
EP (1) EP1483260A1 (en)
JP (1) JP2005526765A (en)
AR (1) AR038922A1 (en)
AU (1) AU2003212282A1 (en)
PE (1) PE20040156A1 (en)
TW (1) TW200406406A (en)
UY (1) UY27714A1 (en)
WO (1) WO2003076437A1 (en)

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