LV10435B - Azole derivatives, method for their preparation and use - Google Patents

Azole derivatives, method for their preparation and use Download PDF

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Publication number
LV10435B
LV10435B LVP-93-286A LV930286A LV10435B LV 10435 B LV10435 B LV 10435B LV 930286 A LV930286 A LV 930286A LV 10435 B LV10435 B LV 10435B
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alkyl
hydrogen
aryl
alkenyl
phenyl
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LVP-93-286A
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LV10435A (lv
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Wagner Adalbert
Englert Heinrich
Kleemann Heinz-Werner
Gerhards Hermann
Schilkens Bernward
Becker Reinhard
Linz Wolfgang
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Hoechst Ag
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Priority claimed from SU5010754 external-priority patent/RU2104272C1/ru
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Publication of LV10435A publication Critical patent/LV10435A/lv
Publication of LV10435B publication Critical patent/LV10435B/en

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Claims (21)

  1. LV 10435 Izgudro .imna formula 1. Azola atvasinājumi ar formulu (l):
    (I), L—(0) q—A kurā simboliem ir sekojošas nozīmes: a) X, Y un z ir vienādi vai atšķirīgi un apzīmē N vai CR2; b) R1· ir 1 . (c2-c10)-alkil-, 2. (c3alkenil-, 3. (c3-C1Q)-alkinil-, 4. R30-, 5. (c3-Cs)-oikloalkil-, 6. (c^-c10)-c.ikloalkilalkil-, 7. (c3-c10)-cikloalkilalkenil-, Θ. (cs-c10)-cikloalkilalkinil-, 9. R4- (CH2) n-B- (CH2) m- , 10. benzil-, 11. grupa kā punktā b-1 , 2, 3 vai 9, kas monoaizvietota ar r3o2c-, 12. grupa kā punktā b-1, 2, 3 vai 9, kurā viens līdz visi H-atorni aizvietoti ar fluoru, vai 13. grupa kā punktā b-10, kurā fenilgredzens satur 1-2 vienādus vai dažādus aizvietotājus no halogēniem,(θ±-θ^)-alkoksi- un nitrogrupas; c) R2 ir 1. ūdeņradis, 8. fenil-, 2. halogēns, 3. nitro-, 4. CvF2v+1 —, 5. pentafluorfenil-, 6. oiāno-, 7. RbO-, 9. fenil-(Ci-Cg)alkil-, 10. (Ct-Cgp)-alkil, 11. (c1-c1D)-alkenil-, 12. fenil(c2-cB)-alkenil-, 13. 1 -imidazolil- (CH2)m-, . 1,2,3-triazolil-(CH2)n-, 14 15. tetrazolil- (CH2)m-, 16. Rs0-R7CH-(CH2)o-1-, 17. r3coo- (ch2)o- 18. RbS- (CH2) O-, 19. R13-S (o) r~, • o OJ Rb0-R3CH-(CH2)m-CH=CH-, 21 . RsC0-(CH2)m-CH=CH-, 22. RsC0-, 23. R7C00-(CH2)m-CH=CH—, ΓΟ • RaC0-CH(CH3)- (CH2)m-, 25. RsC0- (CH2)o-, 26. r3nh-c (=w) -0- (CH2) o-, 27. R30-C (=VW) -NR7- (CH2) o- ro 00 • r3nh-co-nr7-(ch2)O- 29. r3so2-nr7- (CH2)o- 30. R3C (=W) -NR7- (CH2) o-, 31 . F(CH2)n-, 32. 02N0- (CH2) n—, 33. n3-ch2-, 34. 02N- (CH2) n—, 35. RsR7N-N=CH-, 42. 36, ftalimīdo-(CH2)n-,
    40.
    N-C0-(CH2)o-1· 0CH- 41. fenil-S02-NH-N=CH-, ,N XS-NH-N=CH—, NH
  2. 43. RBR3N-CS-NR7-S02-(CH2)n-,
  3. 44. RBRsN-C0-NR7-S02-(CH2)n~, 45. R3S02-(CH2)o~, 46. grupa kā punktā c-8 vai 9, kurā fenilg'redzens satur 1 vai 2 vienādus vai dažādus aizvietotājus no halogēniem, hidrok-sil-, metoksi-, trifluorrnetil-, r302c- un ienilgrupas, 47. grupa kā punktā c-10, 11 vai 19, kur 1 līdz visi H-atomi aizvietoti ar fluoru, 48. grupa kā punktā c-14, kura satur 1 vai 2 vienādus vai dažādus aizvietotājus no rnetoksikarbonil- un (c^-c^)-alkil-grupas',
  4. 49. RBC0-NR7-S02-(CH2)n-,
  5. 50. RBCS-NR7-S02-(CH2)n-; R3 ir 1. ūdeņradis, 2. (Ci-C8)-alkil-, 3. (C3-Ca)-cikloalkil-, 4. fenil- LV 10435
    5. benzil- vai 6. grupa kā punktā d-2, kurā 1 līdz visi H-atomi aizvietoti ar fluoru; ir 1. ūdeņradis, 4. -alkenil- vai 2. (Ci-Cg)-alkil-, 5. (C2-Cu)-alkinil-; 3. (c3-C8)-cikloalkil-, ir 1. ūdeņradis, 4. fenil- vai 2. (Cjļ_—Cg) —alkil—, 5. benzil-; 3. (C3-C8)-cikloalkil-, g) Rb, R3 ir vienādi vai dažādi: 1. ūdeņradis, 2. (Cļ-Cg)-alkilgrupa, kas var saturēt 1-3 aizvietotājus no sekojošas rindas: (Ci-Cg)-alkoksi- (kas, savukārt, var būt aizvietots ar 1-3 hidroksil-, (C±-C£)-alkoksi-, amino-, mono(θ±-αΒ) -alkilamino-, di (C^-Og)-alkilamino-, (C2-C10)-alkenilgrupām), hidroksil-, amino-, mono-(Ci-Cg)-alkilamino-, di (c^-Og) -alkilamino-, (Ci-Ce)-alkoksikarbonilamino-, (CE-C12)-aril-(C^-C^)-alkoksi- karbon 1 I.amino —, —aril—, (Cg-C^q) —aril — (cC3) — allcil-, (Ci-Cg) -heteroaril-, karboksi- un (C1-Cu)-alk-oksikarbonil-, (c3-c8)-cikloalkil-, kas var saturēt 1-3 (Ci-C^-alkil-un (Ca-Ct*) -alkenilaizvietotājus, 4. 5. 6. 7. (C3-C8)-cikloalkil-(Ci~C3)-alkil-, (cB-cl2)-aril-, vislabāk fenil-, (Cg-Cio)-aril-(0.,.-0^)-alkil-, (Ci-Cg)-heteroaril-, kas var būt daļēji vai pilnīgi hidrogenēts, Θ. grupa kā punktā g-5, 6, 7, 9, 15, 16, 17, 19, 20 vai 21, kas satur 1 vai 2 vienādus vai dažādus aizvietotājus no sekojošas rindas: halogēns, hidroksil-, (¢3.-0^)-alkil-» metoksi-, nitro-, ciāno-, R302C-, trifluorme-til-, RliRi2N- un 4“(εΗ2)ς-Λ D N- 9. (Ci-Cg)-heteroaril-(Cļ-Cg)-alkil-, kur heteroarildaļa 4 var būt daļēji vai pilnīgi hidrogenēta, 10. (C4-C6)-alkil-, kurā 1 līdz visi H-atomi aizvietoti ar fluoru, * 11. (c2-C1D)-alkenil-, (c2-C10)-alkenoil- vai (C2-C1D)-al-kadienil-, 12. (C3-C8)-cikloalkenil-, 13. (c3-c8) -cikloalkenil- (C^C;,) -alkil-, 14. bi- vai trioikliska (0^-01ο)-cikloalkenil-(04-0^)-al-kilgrupa, kas var saturēt 1-3 (c^G,,) -alkilaizvietotā-jus, 15. (CB—Cj_q) — ari 1 — (c^—Ciļ.) — alkil—, 16. (c6-Ci0) -aril-(c3-cB) -alkenil-, 17. (Ci-Cg) -heteroar.il-(C3-Ce) -alkenil-, 18. (C3-C8)-alkinil-, 19. (CB-C10) -aril-(C3-CB) -alkinil-, 20. (Ojl—Cg) -heteroaril- (C3-CB) -alkinil-,
  6. 21. RB, R3 kopā ar savienoto N-atomu apzīmē heteroarilgru-pu, kas ari var būt daļēji vai pilnīgi hidrogenēta; h) R7 ir 1. ūdeņradis, 2. (Ci-Cg)-alkil-, 3. (C3-C8)-cikloalkil-, 4. (CB-C12)-aril-(Ci-Cg)-alkil-, vislabāk benzil-, 5. fenil- vai 6. (Cj.—C3) -heteroaril; i) R8 ir 1. ūdeņradis, 5. 2. (Ci-Cg)-alkil-, 6. 3. (c3-C8)-cikloalkil-, 5. RB0-, 6. R1:lR12N- vai 4. fenil-(cH2)q-, j) R10 ir ciāno-, nitro- vai R702c-grupa; k) R11 un R12 ir vienādi vai dažādi: 0 (CH2) q—\
    1. ūdeņradis, 2. (Ci-Cj-alkil-, 4. benzil- vai 5. «-metilbenzil-; 3. fenil-, l) D ir R13N<, 0 vai CH2; m) R13 ir ūdeņradis, (Cļ-C^)-alkil- vai fenil-; - 5 LV 10435 η) A apzīmē bifenil,grupu, kura var būt aizvietota ar 1-4, vislabāk līdz 2 vienādiem vai dažādiem aizvietotājiem R14, un R1S, pie kam Δ obligāti ir aizvietots ar grupu no punkta p-44 vai 45; 1 . halogēns, 12. trifluormetānsulfonilami 2. nitrozo-, no-, 3. nitro-, 13. R30-NH-C0-, 4. amino-, 14. RBR7N-S02-, 5. ciāno-, 15. R70-CH2-, 6. hidroksil-, 16. (Ci_C3) -heteroaril- (CH2) q 7. (Ci-Ce)-alkil-, vislabāk 1-tetrazolil-, 8. (Ci-cJ-alkanoil-, 17. (C7-C13)-aroil-, 9. (Ci-Cj-alkanoiloksi-, 10. r3o2c-, 11. metānsulfonilamino-, /—\ 18. Q N—CH2—, \_/ 19. 0 N-(C0CH2)o-, 20. (CB-C12)-aril-; Ρ) R 1S 1. ūdeņradis, 19. Rs-CH2-S02-NR6-C0-NR7-, 2. (Ci-Cg)-alkil-, 20. H0(CF3)2C-, 3. (C3-Cs)-cikloalkil-, 21. fosfonoksi-, 4. (Ce-Ci2)-aril-, 22. H2P03-, 5. (c7-C13)“aroil-, 23. (H0)2P0-NH-, 6. (Cj.-c J-alkoksi-, 24. ReS (O)r-, 7. (Ci-cJ-alkanoiloksi-, 25. Rs-CO-, 8. (Ci-Cg)-heteroaril-, 26. RBR3N-CO-, 9. R302C-, 27 . (HO) 2PO-R2 °C (OH) - , 10. halogēns, 28. grupa kā punktā c-20, 11. ciāno-, RB φ 12. nitro-, 29. ^OS-NH-SOa-, R8 13. R6R7N-, 30. H02C^_^CO-NH-, 14. hidroksil- 15. r3o2c-chrs-nh-co-, /—\ . 31. _N-(CHa)n-0-, 16. sulfo-, 17. R3S03-, 32. 5-tetrazolil-NH-CO-, 18. ReR3N-C0-NR7-S02- vai 33. cf3-so2-nh-nh-co-, 6 34 (LļN-CO-, C02H
    ^RiB 38. ο.-,
    40. r13-so2-nh-co-,
  7. 41. RB-C0-NH-S02- vai 42. grupa kā punktā p-4, kas satur 1 vai 2 vienādus vai dažādus aizvietotājus no sekojošas rindas: halogēni, ciāno-, nitro-, rbr7N- un hidroksilgrupa, 43. R15 kopā ar R11* apzīmē -C0-NH-S02- grupu,
  8. 44. Rb-00C-NH-S02-,
  9. 45. ReR3N-S02-NH-S02-,
  10. 46. Rb-S02-NH-S02-; q) B ir r7n, 0 vai S; r) w apzīmē 0 vai S; s) L apzīmē (Ci-Ca)-alkāndiilgrupu; t) R1B apzīmē R302c- vai R302CCH2-grupu; u) RA7 apzīmē ūdeņradi, halogēnu, {0±-0^) -alkil- vai (Cjl-C^)-alkok-sigrupu; v) Rla apzīmē ūdeņradi, (Cj.-cJ -alkil- vai fenilgrupu; ir 1. (Ci-Ce)-alkil-, 2. (c3-c8)-cikloalkil-, 3. fenil-, ‘ 4. benzil- vai 5. grupa kā punktā w-1, kurā viens līdz visi H-atomi var būt aizvietoti ar fluoru; 1. vienkāršā saite, 5.-S- I O 0 1 OJ 6. -NR21-, 3. -CH2-, 7. -C0-NR21-, • 0 1 <>* 8. -NR21-C0- - 7 -LV 10435 9. -0-CH2-, 18. -CF=CF-, 10. 1 O X M 1 0 1 4« 19. -CH=CF-, 11 . -s-ch2-, 20. * -CF=CH-, 12. -ch2-s-, 21 . -ch2-ch2-, 13. -nh-cr2Dr22-, 22. -cf2-cf2-, 14. -nr21-so2-, 23. -CH (0R3) -, 15. -S02-NR2i—, • OJ -CH (OCORs) -, 16. -cr20r22-nh-, 25. -C- vai II 17. -CH=CH-, NR23 26. yC\ R2*Cr OR2S y) R2Ū un R22 ir vienādi vai dažādi un apzīmē ūdeņradi, (c1-C5)-al-kil-, fenil-, benzil- vai alilgrupu; z) R21 apzīmē ūdeņradi, (Ο^-Οβ)-alkil-, benzil- vai alilgrupu; a*) r23 ir 1. R2°R21N-, 4. toluol-4-sulfonil- vai 2. ureido-, 5. benzolsulfonilamino-; 3. tioureido-, b’) R2* un R25 ir vienādas vai dažādas (cx-Ch)-alkilgrupas vai kopā tie abi apzīmē -(CH2)q- grupu; o’) 0 apzīmē CH2, NH, 0 vai S; d') m apzīmē veselu skaitli no 0 līdz 5; e’) n apzīmē veselu skaitli no 1 līdz 5; fT) o apzīmē veselu skaitli no 1 līdz 10; g’) q apzīmē 0 vai 1 ; h') r apzīmē 0, 1 vai 2 un i*) v apzīmē veselu skaitli no 1 līdz 6; un to fizioloģiski pieņemami sāļi, izņemot savienojumu ar formulu(*) CH. CH-
    - 8 2. Azola atvasinājumi atbilstoši 1.p. ar formulu (i)> kur a) X ir N, V ir CR2 un Z ir CR2; b) X ir CR2, Y ir N un Z ir CR2; c) X apzīmē CR2, Y apzīmē CR2 un Z apzīmē N vai d) X, Y un Z apzīmē N; un to fizioloģiski pieņemami sāļi. 3. Azola atvasinājumi atbilstoši 1.p. ar formulu (i), kurā simboliem ir sekojošas nozīmes: X ir N, Y ir CR2 un z ir cr2, X ir CR2, y ir N un z ir cr2, X ir CR2, y ir cr2 un Z ir N vai X, Y un Z visi ir N; a) R1 ir 1. (c2-c1D)-alkil-, 4. (c3-Ca)-cikloalkil-, 2. (C3-C10)-alkenil-, 5. benzil- vai 3. (c3-C10)-alkinil-, 6. benzil-, kas aizvietots kā 1.p.; b) R2 ir 1. ūdeņradis, 2. halogēns, 3. nitro-, 4. CvF2v+1—, 5. pentafluorfenil-, 6. oiāno-, 7. Rso-, 8. fenil-, 9. fenil-(Ci-Ca)-alkil-, 10. (Ci-c-,,ο)-alkil-, 11. (c3-c1D)-alkenil-, 12. fenil-(c2-cB)-alkenil-, 13. 1-imidazol.il-(CH2)m-, 14. 1 ,2,3-triazolil-(CH2)o- 29. grupa kā 3.p. b-8, 9, 10, 11 tota kā norādīts 1.p. c-46,
  11. 30. RB-C0-NR7-S02- (CH2)n-’, 15. tetrazolil-(CH2)m-,
  12. 16. Rs0-CHR7-(CH2)o-1-, 17. R3C00-(CH2)o-,
  13. 18. RsC0-, 19. R8C0-(CH2)o-,
  14. 20. RlsS (o) r—,
  15. 21. RB0-CHR3-(CH2)m-CH=CH-, 22. R8C0-(CH2)m-CH=CH-,
  16. 23. RSOOONH- (CH2) o~, 24. R8-S02-NH-(CH2)o-, 25. F(CH2)n~, 26. R3-S03- (CH2)o~,
  17. 27. ReR3N-C0-NH-S02-(CH2)n-, -, 28. RBR3N-CS-NH-S02-(CH2)n-, vai 14 apakšpunktā, kas aizvie-47 vai 48 apakšpunktā,
  18. 31. Rb-CS-NR7-S02-(CH2)n~; - 9 - LV 10435 o) R8 ir ūdeņradis, (Ci-Cs)-alkil-, Rb0-, riiri2n- vai morfolino- d) T ir 1. vienkārša saite, 7 . -ch2-o-, 2. -C0-, 8. ♦ -s-ch2-, 3. -C0-NR21-, 9. -ch2-s-, 4. -CH2-CH2-, 10. -NH-CH2“, 5. -NR21-C0-, 11 . -CH2-NH- vai 6. -ū-ch2-, 12. -CH=CH- un pārējās grupas un mainīgie lielumi kā noteikts 1 -p.; kā arī to fizioloģiski pieņemami sāļi • 4. Azola atvasinājumi atbilstoši 1 . p. ar formulu (i) , kur sim- boliem .ir sekojošas nozīmes: X ir N, Y ir cr2 un 2 ir CR2, X ir CR2, Y ir n un z ir CR2, X ir cr2, Y ir cr2 un Z ir N vai X, Y un t visi ir N; a) R1 ir (c2*c7)-alkil-, (c3-C7)-alkenil- vai (c3-c7)-alkinil-; b) R2 ir 1. hlors, 9. r8co-, 2. broms, 10. R8C0-(CH2)o-, 3. CvF2v+1 ar v=1 , 2 vai 3 , 11 · r8co-nh-ch2-, 4. pentafluorfenil-, 12. r3-so2-nh-(ch2)O-, 5. R60-, 13. r8o-chr3-ch=ch-, 6. R13S (o) r*“, 14. tetrazolil-(CH2)m-, 7. Rs0-CHR7-(CH2)o-1-, 15. ReR3N-C0-NH-S02- (CH2)n- 8. R3C00-(CH2)o-, 16. r3so3-(ch2)o- vai vajadzības gadījumā hidroksilaizvietota (Ci-Ce)-alkilgrupa, vislabāk hidroksimetilgrupa; c) R3 ir ūdeņradis, (Cļ-C,,.) -alkil- vai benzilgrupa; d) RB, R3 ir vienādi vai dažādi: 1. ūdeņradis, 2. (Ci-Cg)-alkilgrupa, kas var saturēt 1-3 aizvietotājus no sekojošas rindas: (Ca.-CB)-alkoksi- (kas, savukārt, var būt aizvietots ar 1-3 hidroksil-, (Ci-CB)-alkoksi-amino- , mono ((^-Οε)-alkilamino-, di (Ci-Ce) -alkilamino-^C2——aikenllgriupsin), hidroksil , amino—, mono 10 (ci“cb) -alkilamino-, diCc-L-Cg)-alkilamino-, (cA-ce)-alkoksikarbonilamino-, (Ce_Ci2) -aril- (Ci-C,,.) -alkoksi-karbonilamino-, (cB-C10)-aril-, (Ce-C^-aril-fci-Ca)-alki.1-, (C^-Cg)-heteroaril-, karboksi- un (C^-C^-alk-oksikarbonil-, 3· (c3“cs)-cikloalkil-, 4. (C3-CB)-cikloalkil-(CA-C3)-alkil-, 5. fenil-, 6. fenil-(θΑ-θ3)-alkil-, 7. (Cļ-C-ļ) -heteroaril-, kas var būt daļēji vai pilnīgi hidrogenēts, 8. grupa kā 1 .p. g-5, 6, 7 vai 9, 14-16 un 18-20 apakšpunktā, kas aizvietota ar 1 vai 2 vienādiem vai dažādiem aizvietotājiem no sekojošas rindas: halogēns, hid-roksil-, (c±-c^)-alkil- metoksi-, nitro-, ciāno-, R302c-, trifluormetilgrupa, RAiR12N- un ^ (CH2) v__/ * 9. (Ci-Cg)-heteroaril-(C1-c3)-alkil-, pie kam heteroaril- da.ļa var būt daļēji vai pilnīgi hidrogenēta, 10. (C^-Cg)-alkil-, kuram 1 līdz visi H-atomi aizvietoti ar fluoru, 11. (C2-Ci*) -alkenil vai c3-alkenoil-, 12. (C3-cB)-oikloalkenil-, 13. (C3-c6)-cikloalkenil-(c1-c3)-alkil-, 14. bi- vai trioikliska (c,*-c1D) -cikloalkenil- (C^-C^) -al-kilgrupa, kas var būt aizvietota ar 1-3 (Ci-C*)-alkil-grupām, 15. Cg-aril-(Ci-C^-alkil-, 16. CB-āril-c3-alkenil-, 17. (Ci-Cg)-hetaril-C3-alkenil-, 18. C3-alkinil-,
  19. 19. CB-aril-c3-alkinil-, 20. (Ci-Cg)-hetaril-C3-alkinil-,
  20. 21. RB, r3 kopā ar savienoto N-atomu apzīmē heteroarilgru-pu, kas var būt daļēji vai pilnīgi hidrogenēta; - 11- LV 10435 vai e) R7 ir ūdeņradis, (c^-cj-alkil-, (C^-Og) -heteroaril- (Ce-C12) -aril-^i-Cķ) -alkil-; f) R8 ir ūdeņradis, (C^-Cj-alkil-, Re0- vai morfolino-; g) R11* ir 1. (Ci-Cj-alkil-, * 9. broms, 2. (c1-Cit) -alkoksi-, 10. (C^-Cg)-heteroaril-CH 3, oiāno-, 11. (Cjl-C^) -alkanoiloksi— 4. amino-, 12. (C^-C^)-alkanoil-, 5. nitrozo-, 13. benzoil-, 6. nitro-, 14. R7-C0-NH-, 7. fluors, 15. tetrazolil-; 2 » » 8. hlors, h) R15 ir 1 o ,4, 5, (c^-cj alkil-, (Cs-C12) -aril-, (Ci_C3)-alkanoiloksi-, (C^-C,*) -alkoksi-, (Cji-Cg) -heteroaril-, vislabāk 5-tetrazolil-, oiāno-, 21 .'O RsCH2-S0-NH-C0-NH-, 5-tetrazolil-NH-CO-, R8 + -^:os-nh-so2-, 7. nitro-, 8. hidroksil 9. RBS(0)x—, 10. r3so3-, 11. hlors, 12. broms, bensoil-, r3o2c-, 13. 14. R* 24. 25.
    (L).N-CO-, cū2h 18 27.
    - (CH2)n-S02-NH-C0-, 28. grupa kā punktā h-2, kas 15. RB-NH-C0-, aizvietota kā norādīts 16. Rs-C0-, augstāk, 17. RBR7N-S02~, 29. R1S un R1* kopā apzīmē 18. RbR3N-C0-NH-S02-, grupu -C0-NH-SQ2-, 19. ho3p-, • o ro rb-ooc-nh-so2-, ro O • H02C-CHRs-C0-, 31 . rer3n-so2-nh-so2-, 32. Rb-S02-NH-S02-; i) R1B ir ūdeņradis, metil- vai etilgrupa; 12 - j) T ir vienkāršā saite, -0-, -00-, -NHCO- vai -0CH2-; k) q = o un L = metilēngrupa, bet pārējās grupas un mainīgie lielumi kā 1.p., kā arī uzskaitīto savienojumu fizioloģiski pieņemami sāļi. 5.· Azola atvasinājumi atbilstoši 1.p. ar vispārīgo formulu (i) , kur» Z ir slāpekļa atoms un X un Y neatkarīgi viens no otra ir CR2, bet pārējie simboli noteikti kā 1.p., un to fizioloģiski pieņemami sāļi. e. Savienojumi ar vispārīgo formulu (l) atbilstoši 1.p., kur simboliem ir sekojošas nozīmes: Z ir slāpeklis; X un V neatkarīgi viens no otra apzīmē CR2; R1 ir (C2-C7)-alkil-, (c3-c7)-alkenil- vai (c3-c7)-alkinil-; R2 ir ūdeņradis, halogēns, nitro-, (C1-C3)-perfluoralkil-, eiāno-, (Ci-Cia)-alkil-, (C3-C1D)-alkenil-, Rs0CH2-, Rla-S(o)r-, Rs-C0- vai RB-0-; Rs ir ūdeņradis vai (Ci“cb)-alkil-; RB, Ra ir: 1 . ūdeņradis, 2. (Ci-Cb) -alkilgrupa, kas var saturēt 1-3 aizvietotājus no sekojošas rindas: (Cj.-CB)-alkoksi- (kas, savukārt, var būt aizvietots ar 1-3 hidroksil-, (Cjl-cs)-alkoksi-, amino-, mo.no (Cx-CB) -alkilamino-, di 0^i~cb) -alkilamino-, (C2-C1D)-alkenilgrupām), hidroksil-, amino-, mono-(Ci-Cg)-alkilamino-, di (cx-Cg)-alkilamino-, (Ci“Ce)“ alkoksikarbonilamino-, (Ce-C:t2)-aril-(C1-cu)-alkoksi-karboni.1 amino-, (CB-C10)-aril-, (Ce_cio)-aril-(Ci-C3)-alkil-, 02i“Cs)-heteroaril-, karboksi- un (c1-clt)-alk-oksikarbonil; 3. (c3—Cg)—cikloalkx1—, 4 · 0—3 —CB) — oikloalkil— 0-± —C3) —alkil—, 5. (cB'ci2)-aril-, vislabāk fenil-, 6. (CB-C1Q)-aril-O^i-1^)-alkil-, - 13 - LV 10435 7. (Ci-Cg)-heteroar.il-, kas var būt daļēji vai pilnīgi hidro- 8. (Ci-Cg)-heteroaril- (C^-Ca) -alkil-, pie kam heteroarildaļa var būt daļēji vai pilnīgi hidrogenēta, 9. grupa kā augstāk minētajos punktos 5., 6., 7. un 8., kas sekojošas metoksi-, un satur 1 vai 2 vienādus vai dažādus aizvietotājus no rindas: halogēns, hicLroks.il*-, (θχ-0^)-alkil-, nit.ro-,· ciāno-, R302C-, trifluormetil-, R1AR12N- q \ D N-, \_/ 10. (Ci~C6)-alkil-, kura 1 līdz visi H-atomi aizvietoti ar fluoru, 11. (C2-CB)-alkenil- vai (C3-CB)-alkenoil-, 12. (c3-Cs)-cikloalkenil-, 13. (C3-C8)-cikloalkenil-(CA-C3)-alkil-, 14. (eb-C10) -aril- (Ci-C^) -alkil-, 1 5. (cB-C10) -aril-(C3-CE)-alkenil-, 16. (Ci-Cg)-hetaril-(C3-CE) -alkenil-, 17. (c3-cB)-alkinil-, 18. (cB-C1Q) -aril-(c3-CB) -alkinil-, 19. (Ci-Cg)-hetaril-(C3-CB)-alkinil-,
  21. 20. Rs, R3 kopā ar savienoto N-atomu apzīmē hetarilgrupu, kas var būt daļēji vai pilnīgi hidrogenēta; R7 ir ūdeņradis; Rs ir ūdeņradis vai RB0-; R11, R12 neatkarīgi viens no otra ir ūdeņradis vai (C;l“Cu) -alkil-; D ir -NR13-, -0- vai -CH2-; Ri3 ir ūdeņradis vai (c^-c^.) -alkil-; Δ ir bifenilgrupa, kas aizvietota ar R1S vai Rllf un R1S kopā; RiS ir ReRsN-C0-NR7-S02-, Re-00C-NH-S02-, RsR3N-S02-NH-S02-, Re-C0-NH-S02-, Rs-S02-NH-S02-; vai arī . R11* un R15 kopā apzīmē -C0-NH-S02-grupu; L ir -CH2-; q = 0 un r = 0, 1 vai 2, kā arī to fizioloģiski pieņemami sāļi. 14 - 7. Paņēmiens azola atvasinājumu iegūšanai ar vispārīgo formulu (i) atbilstoši vienam no punktiem 1-6, kā arī fizioloģiski pieņemamu sāļu pagatavošanai, kas atšķiros ar to, ka savienojumu ar formulu (Π), R
    (II) kur R1, X kur L, A šamības g , Y un Z noteikti 1.p., alkilē ar savienojumu (iIi), U-L- (ū) q—A (III) un q noteikti 1.p., bet U apzīmē gaistošu grupu, nepiecie-ādijumā atšķeļ, ievadītās aizsarggrupas, ja vajadzīgs,pārvērš iegūtos sulfonamīdus ar formulu (i) par uretāniem ar formulu (i), vai arī iegūtos sulfonamīdus (i) vai uretānus (l) vajadzības gadījumā pārvērš par suifoniiurīnvielām (i), un iegūtos savienojumus (i), ja nepieciešams, pārveido fizioloģiski pieņemamos sāļos. ι 8. Savienojumu atbilstoši punktiem 1-6 pielietošana par ārstniecības līdzekļiem. -6 pielietošana augsta asins 9. Savienojumi atbilstoši punktiem spiediena ārstēšanai. 10. Farmaceitiska ār tniecības forma uz aktīvās vielas un piedevu bāzes, kas atšķiras ar to, ka par aktīvo vielu izmanto savienojumu a t bi1sto š i punktiem 1 -6. ll. Paņēmiens ārstnieciskās formas iegūšanai atbilstoši 10.p., kas atšķiras ar to, ka savienojumu ar formulu (i) atbilstoši 1.p. kopā ar fizioloģiski nekaitīgu nesēju un, ja nepieciešams, citām piedevām un palīgvielām pārveido piemērotā ievadīšanas formā.
LVP-93-286A 1991-01-04 1993-05-04 Azole derivatives, method for their preparation and use LV10435B (en)

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IE920020A1 (en) 1992-07-15
AU653760B2 (en) 1994-10-13
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DK0503162T3 (da) 1998-12-07
DE59209292D1 (de) 1998-05-28
CS1092A3 (en) 1992-07-15
EP0503162A1 (de) 1992-09-16
NO920048L (no) 1992-07-06
KR920014785A (ko) 1992-08-25
EP0503162B1 (de) 1998-04-22
JPH04308587A (ja) 1992-10-30
PL168887B1 (pl) 1996-04-30
IL100568A (en) 1996-11-14
HU9200021D0 (en) 1992-03-30
HUT60249A (en) 1992-08-28
IL100568A0 (en) 1992-09-06
ATE165351T1 (de) 1998-05-15
HU211985A9 (en) 1996-01-29
ES2114874T3 (es) 1998-06-16
CA2058198A1 (en) 1992-07-05
LV10435A (lv) 1995-02-20
NO301881B1 (no) 1997-12-22
FI920017A (fi) 1992-07-05
AU9011091A (en) 1992-07-09
FI920017A0 (fi) 1992-01-02
US5482957A (en) 1996-01-09
BR9200011A (pt) 1992-09-08
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NZ241169A (en) 1995-01-27

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