ZA200206192B - 2,4,di(hetero-)arylamino(-oxy)-5-substituted pyrimidines as antineoplastic agents. - Google Patents

2,4,di(hetero-)arylamino(-oxy)-5-substituted pyrimidines as antineoplastic agents. Download PDF

Info

Publication number: ZA200206192B
Authority: ZA; South Africa
Prior art keywords: alkyl; amino; optionally substituted; heterocyclic group; substituted
Prior art date: 2000-03-01

Application number

ZA200206192A

Other languages

English (en)

Inventor

Elizabeth Janet Pease

Robert Hugh Bradbury

Emma Jane Williams

Stuart Eric Pearson

Original Assignee

Astrazeneca Ab

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.)

2000-03-01

Filing date

2002-08-02

Publication date

2003-11-26

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=9886703&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ZA200206192(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2002-08-02 Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab

2003-11-26 Publication of ZA200206192B publication Critical patent/ZA200206192B/en

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150000003230 pyrimidines Chemical class 0.000 title claims abstract description 28
239000002246 antineoplastic agent Substances 0.000 title description 2
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150000002148 esters Chemical class 0.000 claims abstract description 30
150000003839 salts Chemical class 0.000 claims abstract description 27
238000001727 in vivo Methods 0.000 claims abstract description 22
238000004519 manufacturing process Methods 0.000 claims abstract description 10
238000000034 method Methods 0.000 claims abstract description 8
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 3
-1 substituted C Chemical group 0.000 claims description 171
125000000217 alkyl group Chemical group 0.000 claims description 134
125000000623 heterocyclic group Chemical group 0.000 claims description 57
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 54
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 32
229910052799 carbon Inorganic materials 0.000 claims description 32
125000001424 substituent group Chemical group 0.000 claims description 32
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 30
IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 29
125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 25
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TURAMGVWNUTQKH-UHFFFAOYSA-N propa-1,2-dien-1-one Chemical group C=C=C=O TURAMGVWNUTQKH-UHFFFAOYSA-N 0.000 description 1
125000006308 propyl amino group Chemical group 0.000 description 1
QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 description 1
125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 description 1
108060006633 protein kinase Proteins 0.000 description 1
102000004169 proteins and genes Human genes 0.000 description 1
125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 description 1
HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 description 1
125000001422 pyrrolinyl group Chemical group 0.000 description 1
210000001210 retinal vessel Anatomy 0.000 description 1
206010039073 rheumatoid arthritis Diseases 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
239000011734 sodium Substances 0.000 description 1
239000001117 sulphuric acid Substances 0.000 description 1
238000003786 synthesis reaction Methods 0.000 description 1
125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
125000005329 tetralinyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
125000001984 thiazolidinyl group Chemical group 0.000 description 1
125000005505 thiomorpholino group Chemical group 0.000 description 1
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
125000004306 triazinyl group Chemical group 0.000 description 1
125000001425 triazolyl group Chemical group 0.000 description 1
210000004881 tumor cell Anatomy 0.000 description 1
230000003827 upregulation Effects 0.000 description 1

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
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C—CHEMISTRY; METALLURGY
- C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
- C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
- C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
- C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
- C04B35/632—Organic additives
- 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
- 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
- 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

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Engineering & Computer Science (AREA)
Ceramic Engineering (AREA)
Manufacturing & Machinery (AREA)
Health & Medical Sciences (AREA)
Inorganic Chemistry (AREA)
Structural Engineering (AREA)
Materials Engineering (AREA)
Medicinal Chemistry (AREA)
Chemical Kinetics & Catalysis (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Bioinformatics & Cheminformatics (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Hydrogenated Pyridines (AREA)
Saccharide Compounds (AREA)

ZA200206192A 2000-03-01 2002-08-02 2,4,di(hetero-)arylamino(-oxy)-5-substituted pyrimidines as antineoplastic agents. ZA200206192B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
GBGB0004887.6A GB0004887D0 (en)	2000-03-01	2000-03-01	Chemical compounds

Publications (1)

Publication Number	Publication Date
ZA200206192B true ZA200206192B (en)	2003-11-26

Family

ID=9886703

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ZA200206192A ZA200206192B (en)	2000-03-01	2002-08-02	2,4,di(hetero-)arylamino(-oxy)-5-substituted pyrimidines as antineoplastic agents.

Country Status (25)

Country	Link
US (2)	US6838464B2 (2)
EP (1)	EP1278735B1 (2)
JP (2)	JP2003525279A (2)
KR (2)	KR100855258B1 (2)
CN (1)	CN1220684C (2)
AT (1)	ATE472537T1 (2)
AU (2)	AU3397901A (2)
BE (1)	BE2021C507I2 (2)
BR (1)	BR0108879A (2)
CA (1)	CA2398887C (2)
CY (2)	CY1111093T1 (2)
DE (1)	DE60142469D1 (2)
DK (1)	DK1278735T3 (2)
ES (1)	ES2346288T3 (2)
FR (1)	FR21C1010I2 (2)
GB (1)	GB0004887D0 (2)
HK (1)	HK1053111B (2)
IL (2)	IL150920A0 (2)
LU (1)	LUC00197I2 (2)
MX (1)	MXPA02007581A (2)
NO (2)	NO325443B1 (2)
NZ (1)	NZ520502A (2)
PT (1)	PT1278735E (2)
WO (1)	WO2001064656A1 (2)
ZA (1)	ZA200206192B (2)

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- 2021-02-23 LU LU00197C patent/LUC00197I2/fr unknown
- 2021-02-24 CY CY2021005C patent/CY2021005I2/el unknown

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Publication number	Publication date
NO2021008I1 (no)	2021-02-22
PT1278735E (pt)	2010-08-12
NZ520502A (en)	2004-05-28
HK1053111A1 (en)	2003-10-10
CA2398887C (en)	2008-12-16
US7067522B2 (en)	2006-06-27
CY2021005I1 (el)	2021-05-05
BR0108879A (pt)	2003-04-29
FR21C1010I2 (fr)	2022-02-11
IL150920A (en)	2009-08-03
CA2398887A1 (en)	2001-09-07
CY2021005I2 (el)	2021-06-25
FR21C1010I1 (2)	2021-05-07
JP2005041878A (ja)	2005-02-17
CN1220684C (zh)	2005-09-28
EP1278735B1 (en)	2010-06-30
CY1111093T1 (el)	2015-06-11
ATE472537T1 (de)	2010-07-15
KR20070106806A (ko)	2007-11-05
CN1416423A (zh)	2003-05-07
NO20024126D0 (no)	2002-08-29
WO2001064656A1 (en)	2001-09-07
KR20020075463A (ko)	2002-10-04
EP1278735A1 (en)	2003-01-29
GB0004887D0 (en)	2000-04-19
ES2346288T3 (es)	2010-10-14
JP4801335B2 (ja)	2011-10-26
IL150920A0 (en)	2003-02-12
MXPA02007581A (es)	2002-12-13
LUC00197I2 (2)	2021-07-05
US20030181474A1 (en)	2003-09-25
US20050090515A1 (en)	2005-04-28
NO20024126L (no)	2002-08-29
DE60142469D1 (de)	2010-08-12
US6838464B2 (en)	2005-01-04
BE2021C507I2 (2)	2021-02-26
LUC00197I1 (2)	2021-02-23
HK1053111B (en)	2011-02-18
AU3397901A (en)	2001-09-12
AU2001233979B2 (en)	2004-11-11
NO325443B1 (no)	2008-05-05
DK1278735T3 (da)	2010-08-30
JP2003525279A (ja)	2003-08-26
KR100855258B1 (ko)	2008-08-29

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