Nova Patents
IL222773A

Biaryl compounds as serine protease inhibitors

Abstract

This record has no abstract on file.

Term

No projected expiry on record.

  1. Priority
  2. Filed
  3. Published
  4. Today

48 claims: 29 independent, 19 dependent

  1. 1
    222773/2 What is claimed is 1. A compound represented by the structure wherein R is selected from the group consisting of -OCH3;and R' is selected from the group consisting of -CHO, -CO2H, and -CO2MEM;and pharmaceutically acceptable salts thereof;wherein MEM designates a methoxyethoxymethyl group.
  2. 2
    A compound represented by the structure 287 222773/2 wherein R is selected from the group consisting of -OBn,-OH,-OSO2CF3, // \\ , // \\ , I , 288 222773/2 and R' is selected from the group consisting of -CHO, -CO2H, and -CO2MEM;and pharmaceutically acceptable salts thereof;wherein MEM designates a methoxy ethoxymethyl group.
  3. 3
    A compound represented by the structure wherein R is selected from the group consisting of 289 222773/1
  4. 4
    A compound represented by the structure wherein R is selected from the group consisting of 290 222773/1 291 222773/1 and R' is selected from the group consisting of and pharmaceutically acceptable salts thereof. 292 222773/1
  5. 5
    A compound represented by the structure wherein R is selected from the group consisting of o / \ · -°-A\ // -OBn, -OCH3, and ;and pharmaceutically acceptable salts thereof. ch2nh2
  6. 6
    A compound represented by the structure wherein R is selected from the group consisting of 293 222773/1 tips -OSO2CF3, NH and R' is -H or θθ ;and pharmaceutically acceptable salts thereof. wherein R is selected from the group consisting of -OBn,-OH,-OSO2CF3, , ,-CH=CH2, and-H;R' is selected from the group consisting of -CHO, -CO2H, and -CO2MEM;and R" is selected from the group consisting of O 294 222773/1 and pharmaceutically acceptable salts thereof;wherein MEM designates a methoxy ethoxymethyl group.
  7. 7
    8. A compound represented by the structure wherein R is selected from the group consisting of -OBn, -OH, -OSO2CF3, ’ and -CH=CH2;C) R' is -H or -Boc;and R" is -CO2MEM or -CO2H;and pharmaceutically acceptable salts thereof;wherein MEM designates a methoxyethoxymethyl group.
  8. 8
    9. A compound of c-tai-m 1 represented by the structure wherein R is -CH3;and 295 222773/1 -Nv NHR’ is ,or , or R’ is selected from the group consisting of and pharmaceutically acceptable salts thereof. 296 222773/1 wherein R is / ;and R’ is selected from the group consisting of 297 222773/1 and pharmaceutically acceptable salts thereof. and pharmaceutically acceptable salts thereof.
  9. 9
    12. A compound represented by the structure 298 222773/1 wherein R is -CH3 and R’ is selected from the group consisting of and pharmaceutically acceptable salts thereof.
  10. 10
    13. A compound represented by the structure wherein R is selected from the group consisting of -OCH3, -OH, -OSO2CF3, -CH=CH2, -OCH2CO2C2H5, -OCH2CONH2, , s 299 222773/1 // V ch3 R1 is selected from the group consisting of 300 222773/1 Ν' Η and R" is selected from the group consisting of-H, -CH3 and -Bn;and pharmaceutically acceptable salts thereof;wherein MEM designates a methoxy ethoxy methyl group.
  11. 11
    14. A compound represented by the structure wherein R is selected from the group consisting of 301 222773/1 -CH=CH2, -OSO2CF3, -och2co2c2h5, -och2conh2, 0 // A , -och3 ,-O-CH2-CH2-OAc, -oh, ch3 -OCH2CO2H, -O-CH2-CH2-OH, -CH(OH)CH2OH, -ch2oh, -co2h, , -OBn, -OH, -0CH3, -OC2H5, -OBuy and -CH(OH)CH3;and R' is selected from the group consisting of -CH3, -OHiO^Hsv -Bn, and -H;and pharmaceutically acceptable salts thereof.
  12. 12
    15. A compound represented by the structure wherein R is selected from the group consisting of -CH=CH2, -CH(OH)CH2OH, -CH=O, -CH2OH, -CO2H, and -OCH3;and pharmaceutically acceptable salts thereof. 302 222773/1
  13. 13
    16. A compound represented by the structure and pharmaceutically acceptable salts thereof.
  14. 14
    17. A compound represented by the structure NHR"' o wherein R is selected from the group consisting of O -CH3, -C2Hs, -CH(CH3)2, and II ;^C(CH3)3 R' is selected from the group consisting of -OBn, -OH, -OSO2CF3, and -CH=CH2;R" is selected from the group consisting of-CO2H, -CO2MEM, or and -CHO;and R'" is selected from the group consisting of 303 222773/1 Cll, , and Cll, ;and pharmaceutically acceptable salts thereof CH, wherein MEM designates a methoxyethoxymethyl group.
  15. 15
    18. A compound represented by the structure wherein R is selected from the group consisting of O -CH3, -C2H5, -CH(CH3)2, 11 , and -H;C(CH3)3 R' is -H or alkyl;and R" is selected from the group consisting of CH CH, 'ch3 , CH3 , -CH, CH, CH CF, CH 3 , and CH, ;and pharmaceutically acceptable salts thereof.
  16. 17
    20. A compound represented by the structure wherein R is selected from the group consisting of 305 222773/1 306 222773/1 R' is -H, or -CH=CH2;and R" is -H or alkyl;and pharmaceutically acceptable salts thereof.
  17. 18
    21. The compound of clam 20 wherein said alkyl is -CH3.
  18. 19
    22. A compound represented by the structure wherein R is selected from the group consisting of -CH=CH2, and -H;R' is -H or alkyl;and R" is selected from the group consisting of CH3
  19. 21
    24. A compound represented by the structure wherein N is located at position 3 or 4 in the phenyl ring;R is selected from the group consisting of -CHO, -CO2H, and and R' is -H or alkyl;and pharmaceutically acceptable salts thereof.
  20. 23
    26. A compound represented by the structure wherein R is selected from the group consisting of -CH3, -C2Hs, -CH2C6H5, -C(CH3)3, -ch2-cci3, \\ // OMe \\ // 308 222773/1 and R' is -H or alkyl;and pharmaceutically acceptable salts thereof.
  21. 25
    28. A compound represented by the structure wherein R is selected from the group consisting of -CH=CH2, -OCH3, -OBn, -OH, and -H;R' is R" is selected from the group consisting of CH, /CF3 ;and /CH3 ;and R'" is-H;and pharmaceutically ch3 ’ acceptable salts thereof.
  22. 26
    29. A compound represented by the structure 309 222773/1 wherein R is selected from the group consisting of -CHO, -CO2H, and -CO2MEM, \ // NH R' is selected from the group consisting of-OBn, -OH, -OSO2CF3, and -CH=CH2;and R" is -H or alkyl;and pharmaceutically acceptable salts thereof;wherein MEM designates a methoxyethoxymethyl group.
  23. 28
    31. A compound represented by the structure R' is selected from the group consisting of -CHO, -CO2H, and and R" is -H or alkyl;and pharmaceutically acceptable salts thereof.
  24. 30
    33. A compound represented by the structure wherein R is selected from the group consisting of -CH(OH)-CH2OH, -CHO, and -CH(OH)-CH=CH2;R' is -Boc or -H;and R" is -H or alkyl;and pharmaceutically acceptable salts thereof.
  25. 32
    35. A compound represented by the structure wherein R is alkyl;and 311 222773/2 and pharmaceutically acceptable salts thereof.
  26. 33
    36. The compound represented by the structure 312 222773/2 wherein X is CH or N;R is -CH3;R' is -H or -CH3;and R" is selected from the group consisting of
  27. 35
    38. A pharmaceutical composition containing at least one compound according to any one of claims 1-37, and a pharmaceutically acceptable carrier.
  28. 46
    49. A method for inhibiting in vitro clotting of blood which comprises contacting said blood with at least one compound according to any one of claims 1-37.
  29. 48
    51. An extracorporeal device having a coating thereon which comprises a compound according to any one of claims 1-37. S. HOROWITZ amp;CO. AGENT FOR THE APPLICANT 315
Independent claims29