1. Floor panel, comprising a decor, as well as a top layer or laminate layer on the basis of synthetic material, and wherein the decorative side of the floor panel imitates a wood pattern, wherein the floor panel, at its upper surface, has zones of different gloss degrees, which extend over the upper surface as a function of the imitated global wood pattern.
2. Floor panel according to claim 1, wherein for the aforementioned zones, at least two respective gloss grades are applied, which can be distinguished by the naked eye.
3. Floor panel according to claim 1, wherein the upper side, at the location of the wood structure, substantially shows zones of only two gloss degrees.
4. Floor panel according to claim 1, wherein the decor is made in one colour or substantially in one colour, which preferably is a dark colour and more particularly is black or an almost black-looking colour.
5. Floor panel according to claim 1, wherein the decor comprises at least two different colours, in other words, has two kinds of zones which differ from each other by their colour, and wherein the colours are realized as zones representing a wood structure.
6. Floor panel according to claim 5, wherein the decor is realized in only two colours.
7. Floor panel according to claim 5, wherein the two colours differ at least from each other in that one colour is darker than the other.
8. Floor panel according to claim 7, wherein the darkest colour is a dark colour, more particularly black or a colour approaching black.
9. Floor panel according to claim 7, wherein the lighter colour is brown, brownish or grayish.
10. Floor panel according to claim 5, wherein the zones of different gloss degree and the zones of different colour substantially correspond to each other.
11. Floor panel according to claim 10, wherein the zones of a well-defined gloss degree, and preferably the matte zones, are realized larger than the corresponding colour zone, such that there is or may be an overlap at the edges.
12. Floor panel according to claim 10, wherein the two colours at least differ from each other in that the one colour is lighter than the other and that the zones with the gloss degree giving the most matte effect correspond to the zones exhibiting the lighter colour.
13. Floor panel according to claim 12, wherein the zones having the lowest gloss degree are larger than the zones in the aforementioned lighter colour, such that there is or may be an overlap at the edges, whereby the matte zones extend up into the edge region of the dark zones.
14. Floor panel according to claim 1, wherein said zones of different gloss degree each in their turn are flat, with the exception of a possible fine matting structure at the location of the more matte zones and with the exception of possible local embossments, such as, for example, embossments for imitating wood pores.
15. Floor panel according to claim 1, wherein said zones of different gloss degree are situated substantially in the same plane, thus, at the same level.
16. Floor panel according to claim 1, wherein among the zones of different gloss degree, there is a level difference that is smaller than 10 micrometers.
17. Floor panel according to claim 1, wherein the upper surface of the floor panel, embossments are realized, which imitate wood pores, which are in correspondence with the wood structure.
18. Floor panel according to claim 1, wherein the floor panel imitates the wood species Wenge.
19. Floor panel according to claim 1, wherein at the upper edge, a coloration is provided, with a colour, the tint of which corresponds to the general tint of the decor, either in that, at least at the height of the lateral edge of the laminate layer, a colorant has been applied, or in that a material portion at the height of the upper edge is removed, whereby the formed upper surface is provided with a colour layer.
20. Floor panel according to claim 1, wherein on top of the printed decor, a coloured overlay is present, which, in the case of a dark decor, also is coloured in a dark colour.
21. Floor panel according to claim 1, wherein the panel has a dark decor and that the floor panel has a substrate that is coloured with a dark colour as well, whereby optionally, also the bottom side of the floor panel is dark-tinted.
22. Floor panel according to claim 1, wherein both zones of different gloss degree, the glossy as well as the matte, as such have a surface roughness, which generally is smaller than 1 \u03bcm Ra, with the exception of possible unevennesses due to the imitation of wood pores.
23. Floor panel according to claim 1, wherein the floor panel imitates a wood pattern with a so-called flower structure and that the zones of different gloss degree are attuned to this.
24. Floor panel according to claim 1, wherein the floor panel, at its upper surface, has an imitation of one or more wood silver grains, which are realized by the inclusion of one or more of the following technical characteristics:
a region in which a colour alteration has been performed;
a region with a gloss degree altered in respect to the surrounding region thereof, preferably an increased gloss degree;
a region in which a general pattern of embossments imitating wood pores is locally interrupted;
a combination of two or more of the characteristics listed in the above paragraphs.
25. Floor panel, comprising a decor, as well as a top layer on the basis of synthetic material, and wherein the decorative side of the floor panel imitates a wood pattern, wherein the floor panel, at its upper surface, has an imitation of one or more wood silver grains, which is realized by the inclusion application of one or both of the following technical characteristics:
a region with a gloss degree altered in respect to the surrounding region thereof, preferably an increased gloss degree;
a region in which a general pattern of embossments imitating wood pores is locally interrupted.
26. Floor panel according to claim 25, wherein the imitation of the wood silver grains further is also realized by the application of a region in which a colour alteration has been performed.
27. Floor panel, whereby this floor panel comprises a decor, as well as a top layer or laminate layer on the basis of synthetic material, wherein the floor panel, at least at two opposite sides or edges is provided with coupling parts allowing two of such floor panels to cooperate with each other at these sides, and wherein the floor panel, at the aforementioned sides, at the location of the aforementioned top layer or laminate layer, shows upper edges intended to adjoin against each other when two of such floor panels cooperate with each other, wherein the aforementioned upper edges, at least at the height of the lateral edge of the laminate layer, are coloured.
28. Floor panel according to claim 27, wherein the decorative side of the floor panel imitates a wood pattern and the floor panel, at its upper surface, has zones of different gloss degrees extending over the upper surface as a function of the imitated global wood pattern.
29. Floor panel according to claim 27, wherein the decorative side of the floor panel imitates slate or another flaky kind of stone and that the floor panel has terrace-shaped embossments on the upper side.
30. Floor panel according to claim 27, wherein the floor panel differs from a floor panel with the characteristics of claim 28.
31. Floor panel according to claim 27, wherein the panel is provided with a dark decor layer.
32. Floor panel according to claim 27, wherein the floor panel is provided with a dark decor layer and that it imitates the wood species Wenge.
33. Floor panel according to claim 27, including a light-coloured decor layer.
34. Floor panel according to claim 27, wherein the floor panel is provided with a decor layer imitating the wood species Merbau.
35. Floor panel according to claim 27, wherein the tint of the coloration corresponds to the general tint of the decor.
36. Floor panel according to claim 27, wherein the tint of the coloration is darker than the general tint of the decor.
37. Floor panel according to claim 27, wherein the lateral edge of the laminate layer is coloured with a colorant that is provided in liquid form and subsequently is hardened.
38. Floor panel according to claim 37, wherein the colorant is ink.
39. Floor panel according to claim 37, wherein the coloration is the result of spraying or jetting the colorant onto the upper edge.
40. Floor panel according to claim 38, wherein the coloration comprises a print that has been made by means of an inkjet printer supply system.
41. Floor panel according to claim 27, wherein the top layer or laminate layer, at the location of the aforementioned upper edges, is cut substantially vertical in respect to the plane of the floor panel.
42. Floor panel according to claim 27, wherein the top layer or laminate layer is of the DPL or HPL type, whereby undesired visual effects at the location of the seams, where two floor panels adjoin each other, as a result of masking by means of the aforementioned coloration.
43. Method for manufacturing a floor panel, wherein the floor panel comprises a decor, as well as a top layer or laminate layer on the basis of synthetic material, wherein the floor panel, at least at two opposite sides or edges, is provided with coupling parts enabling two of such floor panels to cooperate with each other at these sides, comprising providing a coloration for the floor panels, at one or more upper edges, at least at the location of the top layer or laminate layer, by spraying a hardening substance onto the these upper edges, by means of an inkjet printer supply system.
44. Method according to claim 43, wherein an ink is used for the hardening substance.
45. Method according to claim 43, wherein the floor panels, of which the top layer or laminate layer, at the location of the aforementioned upper edges, is cut substantially vertical in respect to the plane of the floor panel.
46. Method according to claim 43, wherein the floor panels are provided with a chamfer or the like at their upper edges, and wherein the surface of this chamfer is coloured substantially by means of said substance, such as by means of the aforementioned inkjet printer supply system.
47. Method according to claim 43, wherein the floor panels have a top layer or laminate layer of the DPL or HPL type, and undesired visual effects of the seams, where two floor panels adjoin against each other, are masked by said coloration.
48. Method according to claim 43, wherein, when providing the coloration, use is made of a moving inkjet, or a jet of another substance, wherein the direction is controlled such that the jet covers a well-defined operating area, and while the floor panels are moved with the upper edge to be coloured along this operating area.
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
What is claimed is:
1. A compound of the formula (I) or a pharmaceutically acceptable salt thereof:
wherein
16
and when R6 is OH, then Y can also be:
17
R5 is H or deuterium;
R6 is OR8 or NHOH
where R8 is independently H, alkyl, or aralkyl;
R3 and R4independently H, alkyl or aralkyl;
R2H, alkyl, -(CH2)0-4-cycloalkyl,
18
aryl, aralkyl, or -(CH2)2-4-R10;
where n1-3;
R10alkoxy, CH2F, CHF2, CF3, CF2CF3, OH, COOR11, CONR9R11, or NR9R11;
R9 is independently H, alkyl, aryl, aralkyl, -CH2CH2O-alkyl or C(O)R12;
R11 is independently H, alkyl, aryl, or aralkyl;
and when R9 and R11 are taken together, they can equal a five, six or seven membered ring of the type:
19
where n1-3 and m0-1;
and R12 is alkyl, aryl, or aralkyl;
R7H, CH2F, CHR13O(CO)0-1-aryl, CHR13OP(O)(R14)R15,
20
wherein:
R13H or alkyl
R14H, alkyl or aryl
R15H, alkyl or aryl
R16H, alkyl, aryl or aralkyl;
R17H, alkyl, CF3, CF2CF3, aryl, aralkyl, COOR11, or CONR9R11
R18H, alkyl, CF3, CF2CF3, aryl, or aralkyl;
R1 is defined as:
R19-R2, R19-R20, R19-R21, or R19-NR9R11
where R19(CR3R4)-0-4;
21
R22O-
where R22 is alkyl, aryl, aralkyl, R19-cycloalkyl, R19-R21, R23-R10 or R23-R20;
wherein R23(CR3R4)-2-4,
R9 R11N- or R24R11N-
where R24R19-cycloalkyl, R19-R21, R23-R10, R23-R20, CR3R4COOR11 or CR3CR4CONR9R11.
2. A pharmaceutical composition for inhibiting interleukin-1protease comprising a compound of the formula (I) or a pharmaceutically acceptable salt thereof:
22
wherein
23
and when R6 is OH, then Y can also be:
24
R5 is H or deuterium;
R6 is OR8 or NHOH
where R8 is independently H, alkyl, or aralkyl;
R3 and R4independently H, alkyl or aralkyl;
R2H, alkyl, -(CH2)0-4-cycloalkyl,
25
aryl, aralkyl, or-(CH2)2-4-R10;
where n1-3;
R10alkoxy, CH2F, CHF2, CF3, CF2CF3, OH, COOR11, CONR9R11, or NR9R11;
R9 is independently H, alkyl, aryl, aralkyl, -CH2CH2O-alkyl or C(O)-R12;
R11 is independently H, alkyl, aryl, or aralkyl;
and when R9 and R11 are taken together, they can equal a five, six or seven membered ring of the type:
26
where n1-3 and m0-1;
and R12 is alkyl, aryl or aralkyl;
R7H, CH2F, CHR13O(CO)0-1-aryl, CHR13OP(O)(R14)R15,
27
wherein:
R13H or alkyl;
R14H, alkyl or aryl;
R15H, alkyl or aryl;
R16H, alkyl, aryl or aralkyl;
R17H, alkyl, CF3, CF2CF3, aryl, aralkyl, COOR11, or CONR9R11;
R18H, alkyl, CF3, CF2CF3, aryl, or aralkyl;
R1 is defined as:
R19-R2, R19-R20, R19-R21, or R19-NR9R11
where R19(CR3R4)-0-4;
28
R22O-
where R22 is alkyl, aryl, aralkyl, R19-cycloalkyl, R19-R21, R23-R20, or R23-R20;
wherein R23(CR3R4)-2-4;
R9 R11N- or R24R11N-
where R24R19-cycloalkyl, R19-R21, R23-R10, R23-R20, CR3R4COOR11 or CR3CR4CONR9R11 in combination with a pharmaceutically acceptable carrier.
3. A method of inhibiting interleukin-1protease activity in a mammal in need of such treatment comprising administering to said mammal an effective inhibitory amount of a pharmaceutical composition comprising a compound of the formula (I) or a pharmaceutically acceptable salt thereof:
29
wherein
30
and when R6 is OH, then Y can also be:
31
R5 is H or deuterium;
R6 is OR8 or NHOH
where R8 is independently H, alkyl, or aralkyl;
R3 and R4independently H, alkyl or aralkyl;
R2H, alkyl, -(CH2)2-4-cycloalkyl, -(CH2),
32
aryl, aralkyl, or -(CH2)2-4-R10;
where n1-3;
R10alkoxy, CH2F, CHF2, CF3, CF2CF3, OH, COOR11, CONR9R11, or NR9R11;
R9 is independently H, alkyl, aryl, aralkyl, -CH2CH2O-alkyl or C(O)-R12;
R11 is independently H, alkyl, aryl or aralkyl;
and when R9 and R11 are taken together, they can equal a five, six or seven membered ring of the type:
33
where n0-3 and m0-1;
and R12 is alkyl, aryl or aralkyl;
R7H, CH2F, CHR13O(CO)0-1-aryl, CHR13OP(O)(R14)R15,
34
wherein:
R13H or alkyl;
R14H, alkyl or aryl;
R15 H, alkyl or aryl;
R16H, alkyl, aryl or aralkyl;
R17H, alkyl, CF3, CF2CF3, aryl, aralkyl, COOR11, or CONR9R11;
R18H, alkyl, CF3, CF2CF3, aryl or aralkyl;
R1 is defined as:
R19-R2, R19-R20, R19-R21, or R19-NR9R11;
where R19(CR3R4)-0-4;
35
R22O-
where R22 is alkyl, aryl or aralkyl;
wherein R23(CR3R4)-2-4;
R9R11N- or R24R11N-;
where R24R19-cycloalkyl, R19-R21, R23-R10, R23-R20, CR3R4COOR11 or CR3CR4CONR9R11.
4. The compound according to claim 1 selected from the group consisting of: N-2-(5-benzyloxycarbonylamino-6-oxo-2-(4-fluorophenyl)-1, 6-dihydro- 1- pyrimidinyl)acetoyl-L-aspartic acid 2, 6dichlorobenzoyloxymethyl ketone; N-2-(5- thiomethylbenzoylamino-6-oxo-2-(4-fluorophenyl)-1, 6-dihyro-1 -pyrimidinyl)acetoyl-L- aspartic acid 2, 6-dichlorobenzoyloxymethyl ketone; N-2-(5-benzyloxycarbonylamino- 6-oxo-2-(4-fluorophenyl)-1, 6-dihydro-1 -pyrimidinyl)acetoyl-L-aspartic acid -diphenylphosphinoxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(4- fluorophenyl-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-(4-chlorophenyl)- 3-trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2- (4-fluorophenyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(3- pheny)coumarinyloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(4- fluorophenyl)-1, 6-dihydro-1 -pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)pyrazoloxymethyl ketone, N-2-(5-isopropyloxycarbonylamino-6-oxo-2- phenyl-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)pyrazoloxymethyl ketone, N-2-(5-benzyloxycarbonylamino-6-oxo-2-(3- pyridinyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(2- thienyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)-pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2- methyl-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(2- thienyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-(2-pyridinyl)-3- trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(2- thienyl)-L-aspartic acid 5-(1-(4-chlorophenyl)-3-trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(2-thienyl)-L-aspartic acid 2, 6- dichlorobenzoyloxymethyl ketone; and N-2-(5-benzyloxycarbonyl-amino-6-oxo-2-(2- thienyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid aldehyde.
5. The pharmaceutical composition of claim 3 wherein said compound is selected from the group consisting of: N-2-(5-benzyloxycarbonylamino-6-oxo-2-(4- fluorophenyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 2, 6- dichlorobenzoyloxymethyl ketone; N-2-(5-thiomethylbenzoylamino-6-oxo-2-(4- fluorophenyl)-1, 6-dihyro-1-pyrimidinyl)acetoyl-L-aspartic acid 2, 6- dichlorobenzoyloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(4- fluorophenyl)- 1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid diphenylphosphinoxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(4- fluorophenyl-1, 6-dihydro-1-pyrimidinyl)acetoyi-L-aspartic acid 5-(1-(4-chlorophenyl)- 3-trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2- (4-fluorophenyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(3- pheny)coumarinyloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(4- fluorophenyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)pyrazoloxymethyl ketone, N-2-(5-isopropyloxycarbonylamino-6-oxo-2- phenyl-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)pyrazoloxymethyl ketone, N-2-(5-benzyloxycarbonylamino-6-oxo-2-(3- pyridinyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(2- thienyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)-pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2- methyl-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(2- thienyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-(2-pyridinyl)-3- trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(2- thienyl)-L-aspartic acid 5-(1-(4-chlorophenyl)-3-trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(2-thienyl)-L-aspartic acid 2, 6- dichlorobenzoyloxymethyl ketone; and N-2-(5-benzyloxycarbonyl-amino-6-oxo-2-(2- thienyi)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid aidehyde.
6. The method of claim 5 wherein said compound is selected from the group consisting of: N-2-(5-benzyloxycarbonylamino-6-oxo-2-(4-fluorophenyl)- 1, 6-dihydro- 1-pyrimidinyl)acetoyl-L-aspartic acid 2, 6-dichlorobenzoyloxymethyl ketone; N-2-(5- thiomethylbenzoylamino-6-oxo-2-(4-fluorophenyl)-1, 6-dihyro-1-pyrimidinyl)acetoyl-L- aspartic acid 2, 6-dichlorobenzoyloxymethyl ketone; N-2-(5-benzyloxycarbonylamino- 6-oxo-2-(4-fluorophenyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid diphenylphosphinoxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(4- fluorophenyl-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-(4-chlorophenyl)- 3-trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2- (4-fluorophenyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(3- pheny)coumarinyloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(4- fluorophenyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-isopropyloxycarbony-lamino-6-oxo-2- phenyl-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(3- pyridinyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)-pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2- (2-thienyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2- methyl-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-phenyl-3- trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonyl-amino-6-oxo-2- (2-thienyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid 5-(1-(2-pyridinyl)-3- trifluoromethyl)pyrazoloxymethyl ketone; N-2-(5-benzyloxycarbonylamino-6-oxo-2-(2- thienyl)-L-aspartic acid 5-(1-(4-chlorophenyl)-3-trifluoromethyl)pyrazoloxymethyl ketone;N-2-(5-benzyloxycarbonylamino-6-oxo-2-(2-thienyl)-L-aspartic acid 2, 6- dichlorobenzoyloxymethyl ketone; and N-2-(5-benzyloxycarbonylamino-6-oxo-2-(2- thienyl)-1, 6-dihydro-1-pyrimidinyl)acetoyl-L-aspartic acid aldehyde.