.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 6,440,990

« Back to Dashboard

Claims for Patent: 6,440,990

Title: O-alkylated rapamycin derivatives and their use, particularly as immunosuppressants
Abstract:Novel derivatives of rapamycin, particularly 9-deoxo-rapamycins, 26-dihydro-rapamycins, and 40-O-substituted and 28,40-O,O-disubstituted rapamycins. are found to have pharmaceutical utility, particularly as immunosuppressants.
Inventor(s): Cottens; Sylvain (Witterswil, CH), Sedrani; Richard (Basel, CH)
Assignee: Novartis AG (Basel, CH)
Application Number:08/862,911
Patent Claims: 1. A method for treating or preventing graft versus host disease or for treating an autoimmune disease selected from the group consisting of arthritis, rheumatic diseases, autoimmune hematological disorders, systemic lupus erythematosus, polychondritis, sclerodoma, Wegener granulamatosis, dermatomyositis, chronic active hepatitis, myasthenia gravis, psoriasis, Steven-Johnson syndrome, idiopathic sprue, autoimmune inflammatory bowel disease, endocrine ophthalmopathy, Grave's disease, sarcoidosis, multiple sclerosis, primary billiary cirrhosis, juvenile diabetes, anterior uveitis, posterior uveitis, keratoconjunctivitis sicca, vernal keratoconjunctivitis, interstitial lung fibrosis, psoriatic arthritis, glomerulonephritis (with and without nephrotic syndrome), and juvenile dermatomyostis comprising administering to a person in need thereof an effective amount of a compound of the formula ##STR3##

wherein R.sup.1 is hydroxy(C.sub.1-6)alkyl or hydroxy(C.sub.1-3)alkoxy(C.sub.1-3)alkyl.

2. A method of claim 1 wherein R.sup.1 is hydroxy(C.sub.1-3)alkyl or hydroxy(C.sub.1-3)alkoxy(C.sub.1-3)alkyl.

3. A method of claim 1 wherein R.sup.1 is hydroxy(C.sub.1-3)alkyl.

4. A method of claim 1 wherein R.sup.1 is hydroxy(C.sub.1-3)alkoxy(C.sub.1-3)alkyl.

5. A method of claim 1 wherein the compound is 40-O-(3-hydroxypropyl)-rapamycin.

6. A method of claim 1 wherein the compound is 40-O-[2-(2-hydroxyethoxy)ethyl]-rapamycin.

7. A method of claim 1 wherein the autoimmune disease is selected from the group consisting of rheumatoid arthritis, arthritis chronica progrediente, arthritis deformans, hemolytic anaemia, aplastic anaemia, pure red cell anaemia, idiopathic thrombocytopenia, ulcerative colitis, Crohn's disease, idiopathic nephrotic syndrome, and minimal change nephropathy.

8. A method for treating or preventing graft versus host disease or for treating an autoimmune disease selected from the group consisting of arthritis, rheumatic diseases, autoimmune hematological disorders, systemic lupus erythematosus, polychondritis, sclerodoma, Wegener granulamatosis, dermatomyositis, chronic active hepatitis, myasthenia gravis, psoriasis, Steven-Johnson syndrome, idiopathic sprue, autoimmune inflammatory bowel disease, endocrine ophthalmopathy, Grave's disease, sarcoidosis, multiple sclerosis, primary billiary cirrhosis, juvenile diabetes, anterior uveitis, posterior uveitis, keratoconjunctivitis sicca, vernal keratoconjunctivitis, interstitial lung fibrosis, psoriatic arthritis, glomerulonephritis (with and without nephrotic syndrome), and juvenile dermatomyostis comprising administering to a person in need thereof an effective amount of 40-O-(2-hydroxyethyl)-rapamycin.

9. A method of claim 8 wherein the autoimmune disease is selected from the group consisting of rheumatoid arthritis, arthritis chronica progrediente, arthritis deformans, hemolytic anaemia, aplastic anaemia, pure red cell anaemia, idiopathic thrombocytopenia, ulcerative colitis, Crohn's disease, idiopathic nephrotic syndrome, and minimal change nephropathy.

10. A method for treating or preventing the rejection of a transplanted organ or graft versus host disease or for treating an autoimmune disease selected from the group consisting of arthritis, rheumatic diseases, autoimmune hematological disorders, systemic lupus erythematosus, polychondritis, sclerodoma, Wegener granulamatosis, dermatomyositis, chronic active hepatitis, myasthenia gravis, psoriasis, Steven-Johnson syndrome, idiopathic sprue, autoimmune inflammatory bowel disease, endocrine ophthalmopathy, Grave's disease, sarcoidosis, multiple sclerosis, primary billiary cirrhosis, juvenile diabetes, anterior uveitis, posterior uveitis, keratoconjunctivitis sicca, vernal keratoconjunctivitis, interstitial lung fibrosis, psoriatic arthritis, glomerulonephritis (with and without nephrotic syndrome), and juvenile dermatomyostis comprising administering to a host in need thereof an effective amount of a first compound of the formula ##STR4##

wherein R.sup.1 is hydroxy(C.sub.1-6)alkyl or hydroxy(C.sub.1-3)alkoxy(C.sub.1-3)alkyl

and a second compound which is Ciclosporin, FK-506, an immunosuppressive derivative of Ciclosporin or FK-506, a corticosteroid, azathioprene, an immunosuppressive monoclonal antibody, an antiviral, or an antibiotic.

11. A method of claim 10 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is Ciclosporin.

12. A method of claim 10 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is FK-506.

13. A method of claim 10 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is an immunosuppressive derivative of Ciclosporin or FK-506.

14. A method of claim 10 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is a corticosteroid.

15. A method of claim 10 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is azathioprene.

16. A method of claim 10 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is an immunosuppressive monoclonal antibody.

17. A method of claim 16 wherein the second compound is an antibody to CD25.

18. A method of claim 16 wherein the second compound is an antibody to CD3.

19. A method of claim 16 wherein the second compound is an antibody to CD45.

20. A method of claim 10 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is an antiviral.

21. A method of claim 10 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is an antibiotic.

22. A method of claim 10 wherein the autoimmune disease is selected from the group consisting of rheumatoid arthritis, arthritis chronica progrediente, arthritis deformans, hemolytic anaemia, aplastic anaemia, pure red cell anaemia, idiopathic thrombocytopenia, ulcerative colitis, Crohn's disease, idiopathic nephrotic syndrome, and minimal change nephropathy.

23. A pharmaceutical composition comprising a therapeutically effective amount of a compound of the formula ##STR5##

wherein R.sup.1 is hydroxy(C.sub.1-3)alkyl

and a pharmaceutically acceptable carrier therefor.

24. A composition of claim 23 wherein the compound is 40-O-(3-hydroxypropyl)-rapamycin.

25. A pharmaceutical composition comprising a therapeutically effective amount of 40-O-(2-hydroxyethyl)-rapamycin and a pharmaceutically acceptable carrier therefor.

26. A pharmaceutical composition comprising a therapeutically effective amount of a first compound which is of the formula ##STR6##

wherein R.sup.1 is hydroxy(C.sub.1-6)alkyl or hydroxy(C.sub.1-3)alkoxy(C.sub.1-3)alkyl

and a second compound which is Ciclosporin, FK-506, an immunosuppressive derivative of Ciclosporin or FK-506, a corticosteroid, azathioprene, an immunosuppressive monoclonal antibody, an antiviral, or an antibiotic, and a pharmaceutically acceptable carrier therefor.

27. A composition of claim 26 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is Ciclosporin.

28. A composition of claim 26 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is FK-506.

29. A composition of claim 26 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is an immunosuppressive derivative of Ciclosporin or FK-506.

30. A composition of claim 26 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is a corticosteroid.

31. A composition of claim 26 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is azathioprene.

32. A composition of claim 26 wherein the first compound is 40-O-(2-hydroxyethyl)-rapamycin and the second compound is an immunosuppressive monoclonal antibody.

33. A composition of claim 32 wherein the second compound is an antibody to CD25.

34. A composition of claim 32 wherein the second compound is an antibody to CD3.

35. A composition of claim 32 wherein the second compound is an antibody to CD45.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc