CA2093203A1 - Pyrimidine derivatives and processes for the preparation thereof - Google Patents

Pyrimidine derivatives and processes for the preparation thereof

Info

Publication number
CA2093203A1
CA2093203A1 CA002093203A CA2093203A CA2093203A1 CA 2093203 A1 CA2093203 A1 CA 2093203A1 CA 002093203 A CA002093203 A CA 002093203A CA 2093203 A CA2093203 A CA 2093203A CA 2093203 A1 CA2093203 A1 CA 2093203A1
Authority
CA
Canada
Prior art keywords
lower alkyl
free
amino
substituted
aliphatic
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
CA002093203A
Other languages
French (fr)
Other versions
CA2093203C (en
Inventor
Jurg Zimmermann
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Ciba Geigy 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=4202064&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2093203(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ciba Geigy AG filed Critical Ciba Geigy AG
Publication of CA2093203A1 publication Critical patent/CA2093203A1/en
Application granted granted Critical
Publication of CA2093203C publication Critical patent/CA2093203C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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
    • C07D239/42—One nitrogen atom
    • 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
    • C07D401/04—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 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
    • A61K31/495—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Paints Or Removers (AREA)
  • Macromonomer-Based Addition Polymer (AREA)

Abstract

There are described N-phenyl-2-pyrimidine-amine derivatives of formula I
wherein R1 is pyrazinyl, 1-methyl-1H pyrrolyl, amino- or amino-lower alkyl-substituted phenyl wherein the amino group in each cast is free, alkylated or acylated, 1H-indolyl or 1H-imidazolyl bonded at a five-membered ring carbon atom, or unsubstitut ed or lower alkyl-substituted pyridyl bonded at a ring carbon atom and unsubstituted or substituted at the nitrogen atom by oxygen, R2 and R3 are each independently of the other hydrogen or lower alkyl, one or two of the radicals R4, R5, R6, R7 and R8 are each nitro, fluoro-substituted lower alkoxy or a radical of formula II
-N(R9)-C(=X)-(Y)n-R10 (II), wherein R9 is hydrogen or lower alkyl, -X is oxo, thio, imino, N-lower alkyl-imino, hydroximino or O-lower alkyl-hydrox-imino, Y is oxygen or the group NH, n is a or 1 and R10 is an aliphatic radical having at least 5 carbon atoms, or an aromatic, aromatic-aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, heterocyclic or heterocyclic-aliphatic radical, and the remaining radicals R4, R5, R6, R7 and R8 are each independently of the others hydrogen, lower alkyl that is unsubstituted or substituted by free or alkylated amino, piperazinyl, piperidinyl, pyrrolidinyl or by morpholinyl, or lower alkanoyl, trifluoro-methyl, free, etherified or esterifed hydroxy, free, alkylated or acylated amino or free or esterified carboxy.
These compounds can be used, for example, in the therapy of tumoral diseases.
CA002093203A 1992-04-03 1993-04-01 Pyrimidine derivatives and processes for the preparation thereof Expired - Lifetime CA2093203C (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH108392 1992-04-03
CH1083/92-1 1992-04-03

Publications (2)

Publication Number Publication Date
CA2093203A1 true CA2093203A1 (en) 1993-10-04
CA2093203C CA2093203C (en) 2002-11-26

Family

ID=4202064

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002093203A Expired - Lifetime CA2093203C (en) 1992-04-03 1993-04-01 Pyrimidine derivatives and processes for the preparation thereof

Country Status (29)

Country Link
EP (1) EP0564409B1 (en)
JP (1) JP2706682B2 (en)
KR (1) KR100261366B1 (en)
CN (1) CN1043531C (en)
AT (1) ATE188964T1 (en)
AU (1) AU666709B2 (en)
BR (1) BR1100739A (en)
CA (1) CA2093203C (en)
CY (2) CY2229B1 (en)
CZ (1) CZ283944B6 (en)
DE (2) DE59309931D1 (en)
DK (1) DK0564409T3 (en)
ES (1) ES2142857T3 (en)
FI (1) FI109534B (en)
GR (1) GR3032927T3 (en)
HU (2) HU226488B1 (en)
IL (1) IL105264A (en)
LU (1) LU90908I2 (en)
MX (1) MX9301929A (en)
NL (1) NL300086I2 (en)
NO (2) NO302473B1 (en)
NZ (1) NZ247299A (en)
PT (1) PT564409E (en)
RU (1) RU2125992C1 (en)
SA (1) SA93140441B1 (en)
SG (1) SG43859A1 (en)
SK (1) SK280620B6 (en)
TW (1) TW225528B (en)
ZA (1) ZA932397B (en)

Cited By (7)

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US9018205B2 (en) 2007-09-04 2015-04-28 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
US10000469B2 (en) 2014-03-25 2018-06-19 Duke University Heat shock protein 70 (hsp-70) receptor ligands
US10442806B2 (en) 2012-08-06 2019-10-15 Duke University Substituted heterocycles for targeting HSP90
US11261187B2 (en) 2016-04-22 2022-03-01 Duke University Compounds and methods for targeting HSP90

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