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Primary Examiner: Coughlan, Jr., Paul M.
Assistant Examiner:
Attorney: Blitzer; Charles N.

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Title: Treating psoriasis with transient pro-drug forms of xanthine derivatives



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Claims: What we claim is:

1. A method for topically treating psoriasis on a warm-blooded animal afflicted with the same which comprises topically administering thereto an anti-psoriatic effective amount of a compound having the formula: ##STR247## wherein R, which may be the same or different, represents a member selected from the group consisting of --CH.sub.3, --C.sub.2 H.sub.5, iso--C.sub.3 H.sub.7, --C.sub.4 H.sub.9, iso--C.sub.4 H.sub.9, pentyl, benzyl, allyl, 2-hydroxyethyl, cyclohexyl, 2-isobutenyl, hydroxymethyl, 2-phenylethyl and --CH.sub.2 O.sub.13R.sub.2, wherein R.sub.2 is defined infra; wherein R.sub.1 represents a member selected from the group consisting of H, C.sub.1 -C.sub.7 straight or branched alky, CCl.sub.3, CBr.sub.3, CI.sub.3, ##STR248## CH.sub.3 O--CH.sub.2 --, (CH.sub.3).sub.2 NCH.sub.2 --, --CHO, ##STR249## wherein R.sub.3 represents a member selected from the group consisting of --OH, halogen, --OCH.sub.3, --COOCH.sub.3, --NO.sub.2 and --OCOCH.sub.3 ; wherein X is ##STR250## and wherein R.sub.2 represents a member selected from the group consisting of ##STR251## wherein R.sub.4 is a member selected from the group consisting of C.sub.2 -C.sub.20 straight or branched alkyl, ##STR252## wherein R.sub.3 is defined as above, ##STR253## the residue of any naturally occurring amino acid, the residue of any N-- substituted amino acid, wherein said substituent is any amino acid protective group cleavable via hydrogenolysis or hydrolysis the residue of an N,N--C.sub.1 --C.sub.5 --dialkyl or cycloalkylamino acid, ##STR254## wherein n represents an integer of from 1-5 and R.sub.5 and R.sub.6 which may be the same or different represent C.sub.1 -C.sub.5 alkyl or together form a heterocyclic ring with the N atom to which they are attached, imidazolyl, O--C.sub.1 --C.sub.8 alkyl, O-benzyl, O-phenyl and ##STR255## wherein n, R.sub.5 and R.sub.6 are defined as above; and wherein R.sub.2 further represents a member selected from the group consisting of straight or branched C.sub.1 -C.sub.20 alkyl, ##STR256## wherein n, R.sub.5 and R.sub.6 are defined as above, phenyl, tolyl, xylyl, and --SO.sub.2 --R.sub.7, wherein R.sub.7 is a straight or branched C.sub.1 -C.sub.20 alkyl.

2. The method of claim 1 wherein said compound is: 7-Pivaloxymethyl theophylline.

3. The method of claim 1, wherein said compound is: 7-(Pyridinium chloride)methyl theophylline.

4. The method of claim 1, wherein said compound is: 7-Hexanoyloxymethyl theophylline.

5. The method of claim 1, wherein said compound is: 7-Octanoyloxymethyl theophylline.

6. The method of claim 1, wherein said compound is: 7-Butanoyloxymethyl theophylline.

7. The method of claim 1, wherein said compound is: 7-Ethoxycarbonoloxymethyl theophylline.

8. The method of claim 1, wherein said compound is: 7-(N,N-diethylamidosuccinyloxymethyl)theophylline.

9. The method of claim 1, wherein said compound is: 7-(N,N-dimethylglycyloxymethyl)theophylline.

10. The method of claim 1, wherein said compound is: 7-Ethoxymethyl-theophylline.

11. The method of claim 1, wherein said compound is: 7-Butyloxymethyl-theophylline.

12. The method of claim 1, wherein said compound is: 7-Benzyloxymethyl-theophylline.

13. The method of claim 1, wherein said compound is: 7-(1-Pyridyl)methyl-theophylline chloride.

14. The method of claim 1, wherein said compound is: 7-(N,N-dimethylaminoethyoxyl)methyl-theophylline.

15. The method of claim 1, wherein said compound is: 7-Acetyloxymethyl-theophylline.

16. The method of claim 1, wherein said compound is: 7-Butanoyloxymethyl-theophylline.

17. The method of claim 1, wherein said compound is: 7-Ethoxycarbonyloxymethyl-theophylline.

18. The method of claim 1, wherein said compound is: 7-Benzyloxycarbonyloxymethyl-theophylline.

19. The method of claim 1, wherein said compound is: 7-(2', 2', 2',-Trichloroethyloxycarbonyloxymethyl)-theophylline.

20. The method of claim 1, wherein said compound is: 7-(N,N-Dimethylglycyloxymethyl)-theophylline.

21. The method of claim 1, wherein said compound is: 7-(1-Piperidylacetyloxymethyl)-theophylline.

22. The method of claim 1, wherein said compound is: 7-p-Toluyloxymethyl-theophylline.

23. The method of claim 1, wherein said compound is: 7-Phenylacetyloxymethyl-theophylline.

24. The method of claim 1, wherein said compound is: 7-Picolinoyloxymethyl-theophylline.

25. The method of claim 1, wherein said compound is: 7-N-Formylglycyloxymethyl-theophylline.

26. The method of claim 1, wherein said compound is: 7-Glycyloxymethyl-theophylline.

27. The method of claim 1, wherein said compound is: 7-Cinnamoyloxymethyl-theophylline.

28. The method of claim 1, wherein said compound is: 7-Methylsuccinyloxymethyl-theophylline.

29. The method of claim 1, wherein said compound is: 7-(N,N-Dimethylsuccinamyloxymethyl)-theophylline.

30. The method of claim 1, wherein said compound is: 7-(N,N,N-Trimethylglycyloxymethyl)-theophylline chloride.

31. The method of claim 1, wherein said compound is: 7-(.alpha.-Ethoxyethyl)-theophylline.

32. The method of claim 1, wherein said compound is: 7-(.alpha.-Benzyloxyethyl)-theophylline.

33. The method of claim 1, wherein said compound is: 7-(.alpha.-Acetyloxyethyl)-theophylline.

34. The method of claim 1, wherein said compound is: 7-(.alpha.-Butanoyloxyethyl)-theophylline.

35. The method of claim 1, wherein said compound is: 7-(.alpha.-Pivalyloxyethyl)-theophylline.

36. The method of claim 1, wherein said compound is: 7-(.alpha.-Ethoxycarbonyloxyethyl)-theophylline.

37. The method of claim 1, wherein said compound is: 7-[.alpha.-(N,N-Dimethylglycyloxy)ethyl]-theophylline.

38. The method of claim 1, wherein said compound is: 7-(.alpha.-Benzoyloxyethyl)-theophylline.

39. The method of claim 1, wherein said compound is: 7-[.alpha.-(N,N-Dimethylsuccinamyloxy)ethyl]-theophylline.

40. The method of claim 1, wherein said compound is: 7-[.alpha.-(N,N,N-Trimethylglycyloxy)ethyl]-theophylline chloride.

41. The method of claim 1, wherein said compound is: 7-(.alpha.-Benzyloxybenzyl)-theophylline.

42. The method of claim 1, wherein said compound is: 7-(.alpha.-Acetyloxybenzyl)-theophylline.

43. The method of claim 1, wherein said compound is: 7-(.alpha.-Butanoyloxybenzyl)-theophylline.

44. The method of claim 1, wherein said compound is: 7-(.alpha.-Ethoxycarbonyloxybenzyl)-theophylline.

45. The method of claim 1, wherein said compound is: 7-[.alpha.-(N,N-Dimethylglycyloxy)benzyl]-theophylline.

46. The method of claim 1, wherein said compound is: 7-[.alpha.-(N-Formylglycyloxy)benzyl]-theophylline.

47. The method of claim 1, wherein said compound is: 7-(.alpha.-Methylsuccinyloxybenzyl)-theophylline.

48. The method of claim 1, wherein said compound is: 7-[.alpha.-(N,N,-Dimethylsuccinamyloxy)benzyl]-theophylline.

49. The method of claim 1, wherein said compound is: 7-[.alpha.-(N,N,N-Trimethylglycyloxy)benzyl]-theophylline chloride.

50. The method of claim 1, wherein said compound is: 7-Ethoxymethyl-1-methyl-3-isobutylxanthine.

51. The method of claim 1, wherein said compound is: 7-Butyloxymethyl-1-methyl-3-isobutylxanthine.

52. The method of claim 1, wherein said compound is: 7-Benzyloxymethyl-1-methyl-3-isobutylxanthine.

53. The method of claim 1, wherein said compound is: 7-(1-Pyridyl)methyl-1-methyl-3-isobutylxanthine chloride.

54. The method of claim 1, wherein said compound is: 7-(N,N-dimethylaminoethyloxy)methyl-1-methyl-3-isobutylxanthine.

55. The method of claim 1, wherein said compound is: 7-Acetyloxymethyl-1-methyl-3-isobutylxanthine.

56. The method of claim 1, wherein said compound is: 7-Butanoyloxymethyl-1-methyl-3-isobutylxanthine.

57. The method of claim 1, wherein said compound is: 7-Pivalyloxymethyl-1-methyl-3-isobutylxanthine.

58. The method of claim 1, wherein said compound is: 7-Hexanoyloxymethyl-1-methyl-3-isobutylxanthine.

59. The method of claim 1, wherein said compound is: 7-Ethoxycarbonyloxymethyl-1-methyl--3-isobutylxanthine.

60. The method of claim 1, wherein said compound is: 7-Benzyloxycarbonyloxymethyl-1-methyl-3-isobutylxanthine.

61. The method of claim 1, wherein said compound is: 7-(2', 2', 2'-Trichloroethyloxycarbonyloxymethyl)-1-methyl-3-isobutylxanthine.

62. The method of claim 1, wherein said compound is: 7-(N,N,-Dimethylglycyloxymethyl)-1-methyl-3-isobutylxanthine.

63. The method of claim 1, wherein said compound is: 7-(1-Piperidylacetyloxymethyl)-1-methyl-3-isobutylxanthine.

64. The method of claim 1, wherein said compound is: 7-p-Toluyloxymethyl-1-methyl-3-isobutylxanthine.

65. The method of claim 1, wherein said compound is: 7-Phenylacetyloxymethyl-1-methyl-3-isobutylxanthine.

66. The method of claim 1, wherein said compound is: 7-Picolinoyloxymethyl-1-methyl-3-isobutylxanthine.

67. The method of claim 1, wherein said compound is: 7-N-Formylglycyloxymethyl-1-methyl-3-isobutylxanthine.

68. The method of claim 1, wherein said compound is: 7-Glycyloxymethyl-1-methyl-3-isobutylxanthine.

69. The method of claim 1, wherein said compound is: 7-Cinnamoyloxymethyl-1-methyl-3-isobutylxanthine.

70. The method of claim 1, wherein said compound is: 7-Methylsuccinyloxymethyl-1-methyl-3-isobutylxanthine.

71. The method of claim 1, wherein said compound is: 7-(N,N-Dimethylsuccinamyloxymethyl)-1-methyl-3-isobutylxanthine.

72. The method of claim 1, wherein said compound is: 7-(N,N,N-Trimethylglycyloxymethyl)-1-methyl-3-isobutylxanthine chloride.

73. The method of claim 1, wherein said compound is: 7-(.alpha.-Ethoxyethyl)-1-methyl-3-isobutylxanthine.

74. The method of claim 1, wherein said compound is: 7-(.alpha.-Benzyloxyethyl)-1-methyl-3-isobutylxanthine.

75. The method of claim 1, wherein said compound is: 7-(.alpha.-Acetyloxyethyl)-1-methyl-3-isobutylxanthine.

76. The method of claim 1, wherein said compound is: 7-(.alpha.-Butanoyloxyethyl)-1-methyl-3-isobutylxanthine.

77. The method of claim 1, wherein said compound is: 7-(.alpha.-Pivalyloxyethyl)-1-methyl-3-isobutylxanthine.

78. The method of claim 1, wherein said compound is: 7-(.alpha.-Ethoxycarbonyloxyethyl)-1-methyl-3-isobutylxanthine.

79. The method of claim 1, wherein said compound is: 7-[.alpha.-(N,N-Dimethylglycyloxy)ethyl]-1-methyl-3-isobutylxanthine.

80. The method of claim 1, wherein said compound is: 7-(.alpha.-Benzoyloxyethyl)-1-methyl-3-isobutylxanthine.

81. The method of claim 1, wherein said compound is: 7-[.alpha.-(N,N-Dimethylsuccinamyloxy)ethyl-1-methyl-3-isobutylxanthine.

82. The method of claim 1, wherein said compound is: 7-[.alpha.-(N,N,N-Trimethylglycyloxy)ethyl]-1-methyl-3-isobutylxanthine chloride.

83. The method of claim 1, wherein said compound is: 7-(.alpha.-Benzyloxybenzyl)-1-methyl-3-isobutylxanthine.

84. The method of claim 1, wherein said compound is: 7-(.alpha.-Acetyloxybenzyl)-1-methyl-3-isobutylxanthine.

85. The method of claim 1, wherein said compound is: 7-(.alpha.-Butanoyloxybenzyl)-1-methyl-3-isobutylxanthine.

86. The method of claim 1, wherein said compound is: 7-(.alpha.-Ethoxycarbonyloxybenzyl)-1-methyl-3-isobutylxanthine.

87. The method of claim 1, wherein said compound is: 7-[.alpha.-(N,N-Dimethylglycyloxy)benzyl]-1-methyl-3-isobutylxanthine.

88. The method of claim 1, wherein said compound is: 7-[.alpha.-(N-Formylglycyloxy)benzyl]-1-methyl-3-isobutylxanthine.

89. The method of claim 1, wherein said compound is: 7-(.alpha.-Methylsuccinyloxybenzyl)-1-methyl-3-isobutylxanthine.

90. The method of claim 1, wherein said compound is: 7-[.alpha.-(N,N-Dimethylsuccinamyloxy)benzyl]-1-methyl-3-isobutylxanthine.

91. The method of claim 1, wherein said compound is: 7-[.alpha.-(N,N,N-Trimethylglycyloxy)benzyl]-1-methyl-3-isobutylxanthine chloride.

92. The method of claim 1, wherein said compound is: 7-Acetylthiomethyl-theophylline.

93. The method of claim 1, wherein said compound is: 7-Propionylthiomethyl-theophylline.

94. The method of claim 1, wherein said compound is: 7-(N,N-Dimethylglycylthiomethyl)-theophylline.

95. The method of claim 1, wherein said compound is: 7-p-Toluylthiomethyl-theophylline.

96. The method of claim 1, wherein said compound is: 7-Cinnamoylthiomethyl-theophylline.

97. The method of claim 1, wherein said compound is: 7-(N,N-Diethylsuccinamylthiomethyl)-theophylline.

98. The method of claim 1, wherein said compound is combined with a pharmaceutically acceptable topical carrier material.

99. The method of claim 98, wherein said pharmaceutically acceptable topical carrier material is triacetin.
Other info:


Inventors: Bodor, Nicolae S. (Lawrence, KS, US)
Sloan, Kenneth B. (Eudora, KS, US)

Application Number: 655786
Filing Date: 1976-02-06
Publication_date: 1977-12-06
Assignee: INTERx Research Corporation (Lawrence, KS)
Primary Class(es): 514/263.22 514/263.23, 514/263.36, 514/863, 544/267, 544/269, 544/270, 544/271, 544/272
Other Classes:
US Patent Ref:
Other Refs: 1,265,8791,226,587
May, 1961FR
Oct, 1966DT
Other References: Roth et al., Chemical Abstracts, 64:5093g.
Burckhalter et al., J. Org. Chem., 24, pp. 562-564 (1959).