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公开(公告)号:DE60011940T2
公开(公告)日:2005-07-21
申请号:DE60011940
申请日:2000-12-22
Applicant: CELLTECH R&D LTD
Inventor: LANGHAM JOHN , ALEXANDER PETER , HEAD CLIFFORD , LINSLEY MARSHA , PORTER ROBERT , ARCHIBALD CATHERINE , WARRELLOW JOHN
IPC: C07C229/34 , C07C229/36 , C07D471/04 , C07C225/20 , C07C229/46 , C07D295/12 , A61K31/13 , A61K31/435 , A61P29/00
Abstract: Squaric acid derivatives of formula (1) are described:whereinR1 is a group Ar1Ar2Alk- in whichAr1 is an optionally substituted aromatic or heteroaromatic group;Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; and Alk is a chain-CH2-CH(R)-, -CH=C(R)-,in which R is a carboxylic acid (-CO2H) or a derivative or biostere thereof;R2 is a hydrogen atom or a C1-6 alkyl group;L1 is a covalent bond or a linker atom or group;n is zero or the integer 1;Alk1 is an optionally substituted aliphatic chain;R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group: and the salts, solvates, hydrates and N-oxides thereof.The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.
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公开(公告)号:DE69434041T2
公开(公告)日:2005-10-06
申请号:DE69434041
申请日:1994-12-21
Applicant: CELLTECH R&D LTD
Inventor: WARRELLOW JOHN , BOYD CAMPBELL , ALEXANDER PETER , EATON ANTHONY
IPC: A61K31/41 , A61K31/415 , A61K31/42 , A61K31/44 , A61K31/4418 , A61P11/08 , A61P29/00 , A61P43/00 , C07D213/64 , C07D231/20 , C07D261/12
Abstract: Compounds of general formula (1): (1) wherein Y is a halogen atom or a group -OR1 where R1 is an optionally substituted alkyl group; X is -O-, -S- or -N(R8)-, where R8 is a hydrogen atom or an alkyl group; R2 is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R3 is a hydrogen or halogen atom or an -OR9 group, where R9 is a hydrogen atom or an optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl group, or a formyl, carboxamido or thiocarboxamido group; R4 is a group -(CH2)nAr, where Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms and n is zero or an integer 1,2 or 3; R5 is a C3-9 carbocyclic ketone optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; R6 is a hydrogen atom or an optionally substituted alkyl group; R7 is a hydrogen atom or an optionally substituted alkyl group; and the salts, solvates, hydrates and N-oxides thereof. Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.
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公开(公告)号:DE69526080D1
公开(公告)日:2002-05-02
申请号:DE69526080
申请日:1995-06-22
Applicant: CELLTECH R&D LTD
Inventor: HEAD CLIFFORD , WARRELLOW JOHN , ALEXANDER PETER
IPC: A61K31/44 , A61P11/08 , A61P29/00 , A61P43/00 , C07C43/20 , C07C57/30 , C07C69/76 , C07C205/06 , C07C227/02 , C07C229/44 , C07C233/65 , C07C327/48 , C07D213/30 , C07D213/32 , C07D213/38 , C07D213/61 , C07D213/89
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公开(公告)号:DE69532808T2
公开(公告)日:2005-01-13
申请号:DE69532808
申请日:1995-06-21
Applicant: CELLTECH R&D LTD
Inventor: WARRELLOW JOHN , ALEXANDER PETER
IPC: A61K31/44 , A61P11/06 , A61P43/00 , C07C1/26 , C07C1/32 , C07C15/02 , C07C15/12 , C07C17/263 , C07C25/02 , C07C25/18 , C07C43/20 , C07C57/30 , C07C59/64 , C07C237/04 , C07C307/04 , C07C311/00 , C07C323/00 , C07C327/00 , C07C327/48 , C07C335/04 , C07D213/30 , C07D521/00
Abstract: Tri-substituted phenyl derivatives and processes for their preparation. In a preferred embodiment, the compounds have the general formula (1) wherein L may be -OR; Z may be -C(R3)(R4)-C(R5)(R6)(R7); R may be an optionally substituted cycloalkyl group; R3, R6 and R7 may be hydrogen; R4 may be -(CH2)t-Ar-(L1)n-Ar'; R5 may be -(CH2)tAr; Ar may be a monocyclic or bicyclic aryl or heteroaryl group; L1 may be a divalent linking group; and Ar' is Ar or an Ar containing group. Compounds of the invention may be potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.
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公开(公告)号:DE69533589D1
公开(公告)日:2004-11-04
申请号:DE69533589
申请日:1995-06-22
Applicant: CELLTECH R&D LTD
Inventor: ALEXANDER PETER , WARRELLOW JOHN
IPC: C07D213/30 , A61K31/44
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公开(公告)号:DE69434041D1
公开(公告)日:2004-11-04
申请号:DE69434041
申请日:1994-12-21
Applicant: CELLTECH R&D LTD
Inventor: WARRELLOW JOHN , BOYD CAMPBELL , ALEXANDER PETER , EATON ANTHONY
IPC: A61K31/41 , A61K31/415 , A61K31/42 , A61K31/44 , A61K31/4418 , A61P11/08 , A61P29/00 , A61P43/00 , C07D213/64 , C07D231/20 , C07D261/12
Abstract: Compounds of general formula (1): (1) wherein Y is a halogen atom or a group -OR1 where R1 is an optionally substituted alkyl group; X is -O-, -S- or -N(R8)-, where R8 is a hydrogen atom or an alkyl group; R2 is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R3 is a hydrogen or halogen atom or an -OR9 group, where R9 is a hydrogen atom or an optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl group, or a formyl, carboxamido or thiocarboxamido group; R4 is a group -(CH2)nAr, where Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms and n is zero or an integer 1,2 or 3; R5 is a C3-9 carbocyclic ketone optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; R6 is a hydrogen atom or an optionally substituted alkyl group; R7 is a hydrogen atom or an optionally substituted alkyl group; and the salts, solvates, hydrates and N-oxides thereof. Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.
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公开(公告)号:DE69533589T2
公开(公告)日:2005-02-10
申请号:DE69533589
申请日:1995-06-22
Applicant: CELLTECH R&D LTD
Inventor: ALEXANDER PETER , WARRELLOW JOHN
IPC: C07D213/30 , A61K31/44
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公开(公告)号:DE69433594T2
公开(公告)日:2004-08-05
申请号:DE69433594
申请日:1994-12-21
Applicant: CELLTECH R&D LTD
Inventor: WARRELLOW JOHN , BOYD CAMPBELL , ALEXANDER PETER
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公开(公告)号:DE60011940D1
公开(公告)日:2004-08-05
申请号:DE60011940
申请日:2000-12-22
Applicant: CELLTECH R&D LTD
Inventor: LANGHAM JOHN , ALEXANDER PETER , HEAD CLIFFORD , LINSLEY MARSHA , PORTER ROBERT , ARCHIBALD CATHERINE , WARRELLOW JOHN
IPC: C07C229/34 , C07C229/36 , C07D471/04 , C07C225/20 , C07C229/46 , C07D295/12 , A61K31/13 , A61K31/435 , A61P29/00
Abstract: Squaric acid derivatives of formula (1) are described:whereinR1 is a group Ar1Ar2Alk- in whichAr1 is an optionally substituted aromatic or heteroaromatic group;Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; and Alk is a chain-CH2-CH(R)-, -CH=C(R)-,in which R is a carboxylic acid (-CO2H) or a derivative or biostere thereof;R2 is a hydrogen atom or a C1-6 alkyl group;L1 is a covalent bond or a linker atom or group;n is zero or the integer 1;Alk1 is an optionally substituted aliphatic chain;R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group: and the salts, solvates, hydrates and N-oxides thereof.The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.
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公开(公告)号:DE69532808D1
公开(公告)日:2004-05-06
申请号:DE69532808
申请日:1995-06-21
Applicant: CELLTECH R&D LTD
Inventor: WARRELLOW JOHN , ALEXANDER PETER
IPC: A61K31/44 , A61P11/06 , A61P43/00 , C07C1/26 , C07C1/32 , C07C15/02 , C07C15/12 , C07C17/263 , C07C25/02 , C07C25/18 , C07C43/20 , C07C57/30 , C07C59/64 , C07C237/04 , C07C307/04 , C07C311/00 , C07C323/00 , C07C327/00 , C07C327/48 , C07C335/04 , C07D213/30 , C07D521/00
Abstract: Tri-substituted phenyl derivatives and processes for their preparation. In a preferred embodiment, the compounds have the general formula (1) wherein L may be -OR; Z may be -C(R3)(R4)-C(R5)(R6)(R7); R may be an optionally substituted cycloalkyl group; R3, R6 and R7 may be hydrogen; R4 may be -(CH2)t-Ar-(L1)n-Ar'; R5 may be -(CH2)tAr; Ar may be a monocyclic or bicyclic aryl or heteroaryl group; L1 may be a divalent linking group; and Ar' is Ar or an Ar containing group. Compounds of the invention may be potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.
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