WO2002087587A3 - 4-aminosulfonylquinazolines and -quinolines as tyrosine kinase inhibitors - Google Patents

4-aminosulfonylquinazolines and -quinolines as tyrosine kinase inhibitors Download PDF

Info

Publication number
WO2002087587A3
WO2002087587A3 PCT/GB2002/002011 GB0202011W WO02087587A3 WO 2002087587 A3 WO2002087587 A3 WO 2002087587A3 GB 0202011 W GB0202011 W GB 0202011W WO 02087587 A3 WO02087587 A3 WO 02087587A3
Authority
WO
WIPO (PCT)
Prior art keywords
aminosulfonylquinazolines
quinolines
tyrosine kinase
kinase inhibitors
compounds
Prior art date
Application number
PCT/GB2002/002011
Other languages
French (fr)
Other versions
WO2002087587A2 (en
Inventor
David Festus Charles Moffat
Mark James Batchellor
Daniel Christopher Brookings
Peter David Davis
Original Assignee
Celltech R&D Ltd
David Festus Charles Moffat
Mark James Batchellor
Daniel Christopher Brookings
Peter David Davis
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
Application filed by Celltech R&D Ltd, David Festus Charles Moffat, Mark James Batchellor, Daniel Christopher Brookings, Peter David Davis filed Critical Celltech R&D Ltd
Priority to AU2002253350A priority Critical patent/AU2002253350A1/en
Publication of WO2002087587A2 publication Critical patent/WO2002087587A2/en
Publication of WO2002087587A3 publication Critical patent/WO2002087587A3/en

Links

Classifications

    • 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
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/93—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • 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
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
    • 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

Abstract

Compounds of formula (1) are described wherein Ar is an optionally substituted aryl, heteroaryl, aralkyl, heteroaralkyl or alkyl group, X is a nitrogen atom or a C(R1a) group, n is zero or the integer 1 or 2 and R, R?1, R2, R3 and R4¿ are substituents defined in the specification. The compounds are able to inhibit the activity of Class 1 receptor tyrosine kinases and are of use in the treatment of hyperproliferative disorders such as psoriasis.
PCT/GB2002/002011 2001-05-02 2002-05-02 4-aminosulfonylquinazolines and -quinolines as tyrosine kinase inhibitors WO2002087587A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002253350A AU2002253350A1 (en) 2001-05-02 2002-05-02 4-aminosulfonylquinazolines and -quinolines as tyrosine kinase inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0110797.8 2001-05-02
GBGB0110797.8A GB0110797D0 (en) 2001-05-02 2001-05-02 Chemical compounds

Publications (2)

Publication Number Publication Date
WO2002087587A2 WO2002087587A2 (en) 2002-11-07
WO2002087587A3 true WO2002087587A3 (en) 2003-01-09

Family

ID=9913913

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2002/002011 WO2002087587A2 (en) 2001-05-02 2002-05-02 4-aminosulfonylquinazolines and -quinolines as tyrosine kinase inhibitors

Country Status (3)

Country Link
AU (1) AU2002253350A1 (en)
GB (1) GB0110797D0 (en)
WO (1) WO2002087587A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
USRE43098E1 (en) 2000-11-01 2012-01-10 Millennium Pharmaceuticals, Inc. Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1496907B1 (en) * 2002-04-12 2007-09-19 Merck & Co., Inc. Tyrosine kinase inhibitors
DE102007042154A1 (en) * 2007-09-05 2009-03-12 Boehringer Ingelheim Pharma Gmbh & Co. Kg Arylsulfonylaminomethyphosphonsäure derivatives, their preparation and their use as medicaments
EP2279174A2 (en) * 2008-05-21 2011-02-02 Genentech, Inc. Arylsulfonamide compounds, compositions and methods of use
CN106317037A (en) * 2016-08-09 2017-01-11 浙江医药高等专科学校 Ethoxy benzo quinazoline type tyrosine kinase inhibitor containing thiophenesulfonyl structure, preparation method and application
CN106432215A (en) * 2016-08-09 2017-02-22 浙江医药高等专科学校 Benzo-quinazoline tyrosine kinase inhibitor containing thiophene sulfamide structure and application

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2473931A (en) * 1945-11-09 1949-06-21 Merck & Co Inc 2-and 4-sulfanilamido quinazoline
GB1092737A (en) * 1965-06-02 1967-11-29 Mead Johnson & Co 2-methoxy-4-[n-glutarylsulfanilamido]quinazoline and process for preparing the same
GB1144022A (en) * 1965-03-11 1969-03-05 Biochemie Gmbh Improvements in or relating to organic compounds
WO1996009294A1 (en) * 1994-09-19 1996-03-28 The Wellcome Foundation Limited Substituted heteroaromatic compounds and their use in medicine
WO1997032856A1 (en) * 1996-03-05 1997-09-12 Zeneca Limited 4-anilinoquinazoline derivatives
US5710158A (en) * 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
WO2001072720A1 (en) * 2000-03-29 2001-10-04 Celltech Chiroscience Limited Bicyclic amine derivatives as inhibitors of class 1 receptor tyrosine kinases

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2473931A (en) * 1945-11-09 1949-06-21 Merck & Co Inc 2-and 4-sulfanilamido quinazoline
GB1144022A (en) * 1965-03-11 1969-03-05 Biochemie Gmbh Improvements in or relating to organic compounds
GB1092737A (en) * 1965-06-02 1967-11-29 Mead Johnson & Co 2-methoxy-4-[n-glutarylsulfanilamido]quinazoline and process for preparing the same
US5710158A (en) * 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
WO1996009294A1 (en) * 1994-09-19 1996-03-28 The Wellcome Foundation Limited Substituted heteroaromatic compounds and their use in medicine
WO1997032856A1 (en) * 1996-03-05 1997-09-12 Zeneca Limited 4-anilinoquinazoline derivatives
WO2001072720A1 (en) * 2000-03-29 2001-10-04 Celltech Chiroscience Limited Bicyclic amine derivatives as inhibitors of class 1 receptor tyrosine kinases

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002214204, Database accession no. 312115 (BRN) *
MARTIN, T. A. ET AL: "Sulfanilamidoquinazolines", JOURNAL OF MEDICINAL CHEMISTRY, vol. 7, 1964, pages 812 - 814, XP002214203 *
ZH. OBSHCH. KHIM.;, vol. 14, 1944, pages 848 - 854 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
USRE43098E1 (en) 2000-11-01 2012-01-10 Millennium Pharmaceuticals, Inc. Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof

Also Published As

Publication number Publication date
WO2002087587A2 (en) 2002-11-07
AU2002253350A1 (en) 2002-11-11
GB0110797D0 (en) 2001-06-27

Similar Documents

Publication Publication Date Title
TW200510342A (en) Chemical compounds
EP1288202A4 (en) N-acyltetrahydroisoquinoline derivatives
MY143466A (en) Inhibitors of tyrosine kinases
MXPA02011974A (en) Substituted quinazoline derivatives and their use as inhibitors.
WO2005092858A3 (en) Alpha aryl or heteroaryl methyl beta piperidino propanamide compounds as orl1-receptor antagonist
HK1071510A1 (en) Acetylene derivatives having mglur 5 antagonistic activity
PL1635835T3 (en) 2-aminopyrimidine derivatives as raf kinase inhibitors
ATE321038T1 (en) QUINOLINE AND QUINAZOLINE DERIVATIVES AND THEIR USE AS FARNESYL TRANSFERASE INHIBITORS
EE200200148A (en) Quinazoline derivatives, methods for their preparation and their use
WO2004014913A3 (en) Derivatives of 2-trifluormethyl-6-aminopurine as phosphodiesterase 4 inhibitors
CA2309551A1 (en) Aminothiazole inhibitors of cyclin dependent kinases
WO2004098528A3 (en) Pyrazole-amine compounds useful as kinase inhibitors
GB0217757D0 (en) Novel compounds
WO2001038324A3 (en) Imidazole derivatives and their use as raf kinase inhibitors
GB0124933D0 (en) Chemical compounds
WO2001077107A8 (en) Oxazole derivatives and their uses as tyrosine kinase inhibitors
WO2004031401A3 (en) Novel tyrosine kinases inhibitors
TW200505852A (en) Novel compounds
HUP0400246A2 (en) 1,2,4-trioxolane antimalarial pharmaceutical compositions and process for their preparation and use
MXPA05006920A (en) Quinazoline compounds.
WO2002074726A3 (en) Aniline derivatives useful as phosphodiesterase 4 inhibitors
AU2003246100A1 (en) Amide derivative
AU2001235838A1 (en) Imidazol derivatives as raf kinase inhibitors
WO2004004730A3 (en) 2-aminopyrazine derivatives as inhibitors of cyclin dependent kinases for the treatment of proliferative disorders
WO2002062767A1 (en) Novel quinazoline derivatives

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ OM PH PL PT RO RU SD SE SG SI SK SL TJ TM TN TR TT TZ UA UG US UZ VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
AK Designated states

Kind code of ref document: A3

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ OM PH PL PT RO RU SD SE SG SI SK SL TJ TM TN TR TT TZ UA UG US UZ VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP

WWW Wipo information: withdrawn in national office

Country of ref document: JP