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SI9300375B - Imidazole,triazole and tetrazoles derivates - Google Patents

Imidazole,triazole and tetrazoles derivates Download PDF

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Publication number
SI9300375B
SI9300375B SI9300375A SI9300375A SI9300375B SI 9300375 B SI9300375 B SI 9300375B SI 9300375 A SI9300375 A SI 9300375A SI 9300375 A SI9300375 A SI 9300375A SI 9300375 B SI9300375 B SI 9300375B
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Slovenia
Prior art keywords
indol
ylmethyl
methyl
ethylamine
dimethyl
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SI9300375A
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Slovenian (sl)
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SI9300375A (en
Inventor
Raymond Baker
Victor G. Matassa
Leslie J. Street
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Merck Sharp & Dohme Limited
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Application filed by Merck Sharp & Dohme Limited filed Critical Merck Sharp & Dohme Limited
Priority to SI9300375A priority Critical patent/SI9300375B/en
Publication of SI9300375A publication Critical patent/SI9300375A/en
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Claims (9)

-1- PATENTNI ZAHTEVKI 1. Spojina s formulo I ali sol ali predzdravilo od teh: A A 2A compound of formula I or a salt or prodrug thereof: A A 2 (I) v čemer prekinjeni krog predstavlja dve nesosednji dvojni vezi v kateremkoli položaju v petčlenskem obroču; dva, trije ali štirje od V, W, X, Y in Z predstavljajo dušik in preostanek predstavlja ogljik, pod pogojem da sq, kadar dva od V, W, X, Y in Z predstavljata dušik in preostanek predstavlja ogljik, potem omenjeni atomi dušika v nesosednjih položajih v petčlenskem obroču; A1 predstavlja vodik, metil, etil, benzil ali amino; A2 predstavlja nevezan elektronski par, kadar štirje od V, W, X, Y in Z predstavljajo dušik in drugo predstavlja ogljik; ali kadar dva ali trije od V, W, X, Y in Z predstavljajo dušik in preostanek predstavlja ogljik, predstavlja A2 vodik, metil, etil, benzil ali amino; E predstavlja vez ali ravno ali razvejano alkilensko verigo, ki vsebuje od 1 do 4 atome ogljika; F predstavlja skupino s formulo R(I) wherein the broken circle represents two non-adjacent double bonds in any position in the five-membered ring; two, three or four of V, W, X, Y and Z represent nitrogen and the remainder represent carbon, provided that sq, when two of V, W, X, Y and Z represent nitrogen and the remainder represent carbon, then said nitrogen atoms in non-adjacent positions in the five-membered ring; A1 represents hydrogen, methyl, ethyl, benzyl or amino; A2 represents an unbound electron pair when four of V, W, X, Y and Z represent nitrogen and the other represents carbon; or when two or three of V, W, X, Y and Z represent nitrogen and the remainder represents carbon, A2 represents hydrogen, methyl, ethyl, benzyl or amino; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; F represents a group of formula R -9- U predstavlja dušik ali C-R2; B predstavlja kisik, žveplo ali N-R3; R1 predstavlja -CH2. CHR4.NR6R7 ali skupino s formulo-9- U represents nitrogen or C-R2; B represents oxygen, sulfur or N-R3; R1 represents -CH2. CHR4.NR6R7 or a group of formula v kateri prekinjena črta predstavlja fakultativno kemijsko vez; in R2, R3, R4, R5, R6 in R7 neodvisno predstavljajo vodik ali 01-6 alkil.in which the dashed line represents an optional chemical bond; and R 2, R 3, R 4, R 5, R 6 and R 7 independently represent hydrogen or C 1-6 alkyl. 2. Spojina po zahtevku 1, predstavljena s formulo IIA in soli in predzdravila od teh: ,A compound according to claim 1, represented by formula IIA and salts and prodrugs of these:, (HA) v čemer X1 predstavlja dušik ali A12-C; n je nič, 1, 2 ali 3; B* predstavlja kisik, žveplo ali N-R13; A11 in A12 neodvisno predstavljata vodik, metil, etil, benzil ali amino; in R12, R13, R14, R16 in R17 neodvisno predstavljajo vodik ali C^.g alkil.(HA) wherein X1 represents nitrogen or A12-C; n is zero, 1, 2 or 3; B * represents oxygen, sulfur or N-R13; A11 and A12 independently represent hydrogen, methyl, ethyl, benzyl or amino; and R 12, R 13, R 14, R 16 and R 17 independently represent hydrogen or C 1-6 alkyl. 3. Spojina po zahtevku 1, predstavljena s formulo IIB in soli -3- in predzdravila od teh:A compound according to claim 1, represented by formula IIB and salts of -3- and prodrugs of these: (IIB) v čemer Υ1 predstavlja dušik ali A22-C; n je nič, 1, 2 ali 3; B2 predstavlja kisik, žveplo ali N-R23; A21 in A22 neodvisno predstavljata vodik, metil, e>til ali benzil; in R22, R23, R24, R26 in R27 neodvisno predstavljajo vodik ali alkil.(IIB) wherein Υ1 represents nitrogen or A22-C; n is zero, 1, 2 or 3; B2 represents oxygen, sulfur or N-R23; A21 and A22 independently represent hydrogen, methyl, ethyl or benzyl; and R22, R23, R24, R26 and R27 independently represent hydrogen or alkyl. 4. Spojina po zahtevku 1, predstavljena s formulo IIC in soli in predzdravila od teh:A compound according to claim 1, represented by formula IIC and salts and prodrugs of these: (IIC) v čemer -4- Υ2 predstavlja dušik ali A32-C; Z1 predstavlja dušik ali CH; n je nič, 1, 2 ali 3; B3 predstavlja kisik, žveplo ali N-R33; A31 in A32 neodvisno predstavljata vodik, metil ali amino; R31 predstavlja -CH2 . CHR34 . NR36R37 ali skupino s formulo λ N-R 3 5 J ali(IIC) wherein -4- Υ2 represents nitrogen or A32-C; Z1 represents nitrogen or CH; n is zero, 1, 2 or 3; B3 represents oxygen, sulfur or N-R33; A31 and A32 independently represent hydrogen, methyl or amino; R31 represents -CH2. CHR34. NR36R37 or a group of formula λ N-R 3 5 J or m R32, R33, R34, R35, R36 in R37 neodvisno predstavljajo vodik ali alkil.m R32, R33, R34, R35, R36 and R37 independently represent hydrogen or alkyl. 5. Spojina po zahtevku 1, predstavljena s formulo IID in soli in predzdravila od teh:A compound according to claim 1, represented by formula IID and salts and prodrugs of these: (UD) v čemer Vi1 predstavlja dušik ali C-A42; n je nič, 1, 2 ali 3; B4 predstavlja kisik, žveplo ali N-R43; A41 in A42 neodvisno predstavljata vodik ali metil; -5- R41 predstavlja -CH2 .CHR44 .NR46R47 ali skupino s formulo -5- λ I J N-R 4S ali N-R 45 m R42, R43, R44, R45, R46 in R47 neodvisno predstavljajo vodik ali 01-6 alkil.(UD) wherein Vi1 represents nitrogen or C-A42; n is zero, 1, 2 or 3; B4 represents oxygen, sulfur or N-R43; A41 and A42 independently represent hydrogen or methyl; -5- R41 represents -CH2 .CHR44 .NR46R47 or a group of formula -5- λ I J N-R 4S or N-R 45 m R42, R43, R44, R45, R46 and R47 independently represent hydrogen or C1-6 alkyl. 6. Spojina po zahtevku 1, izbrana iz naslednjih, kot so: 2-[5-(2-benziltetrazol-5-ilmetil)-lH-indol-3-il]etilamin; 2- [5-(l-benziltetrazol-5-ilmetil)-lH-indol-3-il]etilamin; N,N-dimetil-2-[5-(l-metiltetrazol-5-ilmetil)-lH-indol-3-il]etilamin; N,N-dimetil-2-[5-(2-metiltetrazol-5-ilmetil)-lE-indol-3-il]etilamin; N,N-dimetil-2-[5-(1,2,4-triazol-l-ilmetil)-lH-indol-3-il] etilcimin; N,N-dimetil-2-[5-(tetrazol-2-ilmetil) -lH-indol-3-il]etilamin; N,N-dimetil-2-[5-(tetrazol-l-ilmetil)-lH-indol-3-il]etilamin; N,N-dimetil-2-[5- (1-metil-l,2,4-triazol-5-ilmetil)-lH-indol-3-il]etilamin; N,N-dimetil-2-[5-(1-metil-l,2,4-triazol-3-ilmetil)-lH-indol-3-il]etilamin; N,N-d±metil-2-[5-(1,2,3-triazol-l-ilmetil)-lH-indol-3-il]etilamin; 3- (2-aminoetil)-5-(l-metiltetrazol-5-il)benzo[b]tiofen; 3- (2-čuninoetil) -5- (2-metiltetrazol-5-il)benzo[b] tiofen; 3- (2- (Ν,Ν-dimetilami.no) etil] -5- (2-metiltetrazol-5- il)benzo[b]tiofen; N,N-dimetil-2-[5- (2-metilimidazol-l-ilmetil)-lH-indol-3- -6- ±1]etilamin; N,N-dimetil-2-[5-(imidazol-l-ilmetil)-lH-indol-3-il]etilamin; N,N-dimetil-2-[5-(2-metilimidazol-l-il)-lH-indol-3-il]etilamin; N,N-dimetil-2-[5-(2-etiltetrazol-5-ilmetil)-lH-indol-3-11] etilamin; N,N-dimetil-2-[5-(l-etiltetrazol-5-ilmetil)-lH-indol-3-il]etilamin; N,N-dimetil-2- [5-(1,2,4-triazol-l-il) -lH-indol-3-il]etilamin; l-metil-4-[5-(2-metilimidazol-l-il)-lH-indol-3-il]piperidin; l-metil-4-[5-(1,2,4-triazol-l-ilmetil)-lH-indol-3-il]piperidin; 4-[5-(2-metilimidazol-l-il)-lH-indol-3-il]piperidin; 4-[5-(1,2,4-triazol-l-ilmetil)-lH-indol-3-il]piperidin; 3- [5-(2-metilimidazol-l-il)-lH-indol-3-il]pirolidin; l-metil-3-[5-(2-metilimidazol-l-il)-lH-indol-3-il]pirolidin; 4- [5-(imidazol-l-il)-lH-indol-3-il)piperidin; 4-[5-(l,2,3-triazol-l-il)-lH-indol-3-il]piperidin; l-metil-4-[5-(imidazol-l-il)-lH-indol-3-il]piperidin; l-metil-4-[5-(1,2,3-triazol-l-il)-lH-indol-3-il]piperidin; l-metil-3-[5-(1,2,3-triazol-l-il)-lH-indol-3-il]pirolidin; l-metil-3- [5- (2-metil.imidazol-l-ilmetil) -lH-indol-3-il]pirolidin; l-metil-3-[5-(imidazol-l-il)-lH-indol-3-il]pirolidin; l-metil-3-[5-(1,2,4-triazol-l-ilmetil)-lH-indol-3-il]pirolidin; l-metil-3-[5-(imidazol-l-ilmetil)-lH-indol-3-il)pirolidin; N,N-dimetil-2-[5-(2-aminoimidazol-l-il)-lH-indol-3-il]etilamin; N,N-dimetil-2-[5-(2-aminoimidazol-l-ilmetil)-lH-indol-3-il]etilamin; N-metil-2-[5-(1,2,4-triazol-l-ilmetil)-lH-indol-3-il]etilamin; in soli in predzdravila od teh.A compound according to claim 1 selected from the following: 2- [5- (2-benzyltetrazol-5-ylmethyl) -1H-indol-3-yl] ethylamine; 2- [5- (1-Benzyltetrazol-5-ylmethyl) -1H-indol-3-yl] ethylamine; N, N-dimethyl-2- [5- (1-methyltetrazol-5-ylmethyl) -1H-indol-3-yl] ethylamine; N, N-dimethyl-2- [5- (2-methyltetrazol-5-ylmethyl) -1E-indol-3-yl] ethylamine; N, N-dimethyl-2- [5- (1,2,4-triazol-1-ylmethyl) -1H-indol-3-yl] ethylcimine; N, N-dimethyl-2- [5- (tetrazol-2-ylmethyl) -1H-indol-3-yl] ethylamine; N, N-dimethyl-2- [5- (tetrazol-1-ylmethyl) -1H-indol-3-yl] ethylamine; N, N-dimethyl-2- [5- (1-methyl-1,2,4-triazol-5-ylmethyl) -1H-indol-3-yl] ethylamine; N, N-dimethyl-2- [5- (1-methyl-1,2,4-triazol-3-ylmethyl) -1H-indol-3-yl] ethylamine; N, N-d ± methyl-2- [5- (1,2,3-triazol-1-ylmethyl) -1H-indol-3-yl] ethylamine; 3- (2-aminoethyl) -5- (1-methyltetrazol-5-yl) benzo [b] thiophene; 3- (2-Chuninoethyl) -5- (2-methyltetrazol-5-yl) benzo [b] thiophene; 3- (2- (N, N-dimethylamino) ethyl] -5- (2-methyltetrazol-5-yl) benzo [b] thiophene; N, N-dimethyl-2- [5- (2-methylimidazole- 1, ylmethyl) -1H-indol-3- -6- ± 1] ethylamine, N, N-dimethyl-2- [5- (imidazol-1-ylmethyl) -1H-indol-3-yl] ethylamine; N-dimethyl-2- [5- (2-methylimidazol-1-yl) -1H-indol-3-yl] ethylamine, N, N-dimethyl-2- [5- (2-ethyltetrazol-5-ylmethyl) - 1H-indol-3-11] ethylamine, N, N-dimethyl-2- [5- (1-ethyltetrazol-5-ylmethyl) -1H-indol-3-yl] ethylamine, N, N-dimethyl-2- [ 5- (1,2,4-triazol-1-yl) -1H-indol-3-yl] ethylamine, 1-methyl-4- [5- (2-methylimidazol-1-yl) -1H-indol-3 1-methyl-4- [5- (1,2,4-triazol-1-ylmethyl) -1H-indol-3-yl] piperidine 4- [5- (2-methylimidazol-1-) yl) -1H-indol-3-yl] piperidine 4- [5- (1,2,4-triazol-1-ylmethyl) -1H-indol-3-yl] piperidine 3- [5- (2- methylimidazol-1-yl) -1H-indol-3-yl] pyrrolidine, 1-methyl-3- [5- (2-methylimidazol-1-yl) -1H-indol-3-yl] pyrrolidine, 4- [5 - (imidazol-1-yl) -1H-indol-3-yl) piperidine; 4- [5- (1,2,3-triazol-1-yl) -1H-indol-3-yl] piperidine; 1-methyl-4- [5- (imidazol-1-yl) -1H-indol-3-yl] piperidine; 1-methyl-4- [5- (1,2,3-triazol-1-yl) -1H-indol-3-yl] piperidine; 1-methyl-3- [5- (1,2,3-triazol-1-yl) -1H-indol-3-yl] pyrrolidine; 1-methyl-3- [5- (2-methylimidazol-1-ylmethyl) -1H-indol-3-yl] pyrrolidine; 1-methyl-3- [5- (imidazol-1-yl) -1H-indol-3-yl] pyrrolidine; 1-methyl-3- [5- (1,2,4-triazol-1-ylmethyl) -1H-indol-3-yl] pyrrolidine; 1-methyl-3- [5- (imidazol-1-ylmethyl) -1H-indol-3-yl) pyrrolidine; N, N-dimethyl-2- [5- (2-aminoimidazol-1-yl) -1H-indol-3-yl] ethylamine; N, N-dimethyl-2- [5- (2-aminoimidazol-1-ylmethyl) -1H-indol-3-yl] ethylamine; N-methyl-2- [5- (1,2,4-triazol-1-ylmethyl) -1H-indol-3-yl] ethylamine; and salts and prodrugs thereof. 7. Farmacevtski sestavek, ki vsebuje spojino po kateremkoli od predhodnih zahtevkov v povezavi s farmacevtsko sprejemljivim nosilcem ali ekscipientom. -7-A pharmaceutical composition comprising a compound according to any one of the preceding claims in association with a pharmaceutically acceptable carrier or excipient. -7- 8. Spojina po kateremkoli od zahtevkov 1 do 6 za uporabo pri terapiji.A compound according to any one of claims 1 to 6 for use in therapy. 9. Uporaba spojine po kateremkoli od zahtevkov 1 do 6 za izdelovanje zdravila za zdravljenje in/ali preprečitev kliničnih stanj, za katere je indiciran selektivni agonist receptorjev, podobnih 5-HTj. Za MERCK SHARP & DOHME LTD. Hoddesdon Hertfordshire EN11 9BU Velika Britanija : OB.VFTN I<C A Mus Ljubljana, Resljeva c!24 tel.. 300 76 60, fex: 433 70 98Use of a compound according to any one of claims 1 to 6 for the manufacture of a medicament for the treatment and / or prevention of clinical conditions for which a selective 5-HT1-like receptor agonist is indicated. For MERCK SHARP & DOHME LTD. Hoddesdon Hertfordshire EN11 9BU Great Britain: OB.VFTN I < C A Mus Ljubljana, Resljeva c! 24 tel. 300 76 60, fex: 433 70 98
SI9300375A 1993-07-12 1993-07-12 Imidazole,triazole and tetrazoles derivates SI9300375B (en)

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SI9300375B true SI9300375B (en) 2002-02-28

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