公开(公告)号：AU1628397A

公开(公告)日：1997-09-25

申请号：AU1628397

申请日：1997-03-17

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT ,  HEITSCH HOLGER ,  NOLKEN GERHARD ,  WIRTH KLAUS ,  SCHOLKENS BERNWARD

IPC: C07D237/28 ,  A61K31/345 ,  A61K31/47 ,  A61K31/495 ,  A61K31/53 ,  A61P43/00 ,  C07D215/04 ,  C07D215/26 ,  C07D239/72 ,  C07D239/74 ,  C07D241/36 ,  C07D241/44 ,  C07D253/04 ,  C07D253/065 ,  C07D257/10

Abstract: Fluoroalkyl- and fluoroalkoxy-substituted benzyloxy-azaheterocyclic compounds of formula (I) and their salts are new: X1-X3 = N or CR ; R , R = H or halo; R , R = H, halo, 1-5C alkyl or 2-5C alkenyl; R = 2-5C alkenediyl, halo, OR , SR , NHR , -COOR or COOH; 1-6C alkyl, 6-12C aryl or 6-12C aryl-1-3C alkyl (all optionally substituted by e.g. OR , SR , NO2, CN, NHR or halo); R , R = H, 1-5C alkyl, 3-5C alkenyl or 6-12C aryl-1-3C alkyl; R = 1-5C alkyl or 1-5C alkoxy (both substituted by 1 or more F or Cl); B = amino acid; D = 2-5C alkanediyl, 1-5C alkanediyl or -(CH2)n-Yp-(CH2)m-; E = O or S; Y = O, S or NR ; n, m = 0-3; o = 1-3; and p = 0 or 1.

公开(公告)号：SK32097A3

公开(公告)日：1998-01-14

申请号：SK32097

申请日：1997-03-11

Applicant: HOECHST AG

Inventor： HEITSCH HOLGER ,  WAGNER ADALBERT ,  WIRTH KLAUS ,  SCHOLKENS BERNWARD ,  NOLKEN GERHARD

IPC: A61K31/47 ,  A61P43/00 ,  C07D215/26 ,  C07D215/48 ,  A61K31/09

Abstract: 8-(3-(Aminoalkoxy)-benzyloxy)-quinoline compounds of formula (I) and their salts are new. R1-R3 = H, halo, CHO, COOH, 1-5C alkyl, 6-10C aryl, 1-3C alkyl-(6-10C) aryl, 3-8C cycloalkyl or 1-3C alkoxycarbonyl; R4, R5 = H, halo, NO2, CN, 1-3C alkoxy or 1-3C alkylthio; R6 = H, 1-3C alkyl, 3-5C alkylalkenyl (sic) or 1-3C alkyl-6-10C aryl; R7 = H, 1-6C alkanoyl, alkanoyl (substituted by 1-3C alkoxy, alkylcarbamoyl or aryl), 3-7C alkenoyl, 3-8C cycloalkylcarbonyl, 5-7C cycloalkenylcarbonyl, 1-3C alkoxycarbonyl, aryloxycarbonyl, 6-12C aroyl (optionally substituted by 1-3C alkoxy or halo), alkenoyl (substituted by aryl (optionally substituted by 1-3C alkoxy, 1-3C alkylenedioxy, NO2, CN, halo, 1-3C haloalkyl, hetero-3-8C cycloalkyl (sic), NH2, 1-4C alkylamino, 6-12C heteroaryl-alkanoylamino, aroylamino, 6-12C heteroarylcarbonylamino, 1-5C alkylsulphonylamino, 1-5C alkylureido, alkanoyl, 1-5C alkoxycarbonyl, 1-5C alkylcarbamoyl or arylcarbamoyl), 2-5C acylamino-arylcinnamoyl, 1-3C alkoxycarbonylamino-arylcinnamoyl, 1-4C alkylaminocarbonylaminocinnamoyl, aryl-1-5C alkoxycarbonyl, 1-5C alkylcarbamoyl, arylcarbamoyl, aroylcarbamoyl, alkylsulphonyl, arylsulphonyl, aryl-alkylsulphonyl or phthaloyl (for R6=R7(sic)); n = 1-8; alkyl has 1-6C, aryl has 6-12C, alkanoyl has 2-6C, and alkenoyl has 3-6C unless specified other wise.

公开(公告)号：MX9702028A

公开(公告)日：1997-09-30

申请号：MX9702028

申请日：1997-03-18

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT ,  HEITSCH HOLGER ,  NOLKEN GERHARD ,  WIRTH KLAUS ,  SCHOLKENS BERNWARD

IPC: C07D237/28 ,  A61K31/345 ,  A61K31/47 ,  A61K31/495 ,  A61K31/53 ,  A61P43/00 ,  C07D215/04 ,  C07D215/26 ,  C07D239/72 ,  C07D239/74 ,  C07D241/36 ,  C07D241/44 ,  C07D253/04 ,  C07D253/065 ,  C07D257/10 ,  C07D215/20

Abstract: Se describen derivados heterocíclicos de fluoroalquilo y fluoroalcoxi de la formula (I) con un efecto antagonista de bradiquinina (Ver Formula) en la que X1-X3 significan N o CR5, R1 y R2 significan H o halogeno, R3 y R4 significan H, halogeno, alquilo o alquenilo, R5 significa H, halogeno, alquilo (sustituido), O-R6, S-R6, NHR6, arilo (sustituido), aril (sustituido)-alquilo, -C(O)-OR6 o -C(O)-H, R6 Y R8 significan H, alquilo, alquenilo o aril-alquilo, R7 significa alquilo (sustituido) o alcoxi (sustituido), B significa un ácido aminocarboxílico, D significa alquenodiílo, alcanodiílo o (CH2)n-Yp-(CH2)m-; E significa oxígeno o azufre, Y significa oxígeno, azufre o NR8, n y m significan un numero de 0 - 3, o significa un numero de 1 - 3 y p significa 0 o 1, así como sus sales fisiologicamente compatibles y un procedimiento para su preparacion.

公开(公告)号：SK34897A3

公开(公告)日：1998-01-14

申请号：SK34897

申请日：1997-03-17

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT ,  HEITSCH HOLGER ,  NOLKEN GERHARD ,  WIRTH KLAUS ,  SCHOLKENS BERNWARD

IPC: C07D237/28 ,  A61K31/345 ,  A61K31/47 ,  A61K31/495 ,  A61K31/53 ,  A61P43/00 ,  C07D215/04 ,  C07D215/26 ,  C07D239/72 ,  C07D239/74 ,  C07D241/36 ,  C07D241/44 ,  C07D253/04 ,  C07D253/065 ,  C07D257/10 ,  C07D237/32 ,  C07D239/70 ,  C07D241/38 ,  A61K31/395

Abstract: Fluoroalkyl- and fluoroalkoxy-substituted benzyloxy-azaheterocyclic compounds of formula (I) and their salts are new: X1-X3 = N or CR ; R , R = H or halo; R , R = H, halo, 1-5C alkyl or 2-5C alkenyl; R = 2-5C alkenediyl, halo, OR , SR , NHR , -COOR or COOH; 1-6C alkyl, 6-12C aryl or 6-12C aryl-1-3C alkyl (all optionally substituted by e.g. OR , SR , NO2, CN, NHR or halo); R , R = H, 1-5C alkyl, 3-5C alkenyl or 6-12C aryl-1-3C alkyl; R = 1-5C alkyl or 1-5C alkoxy (both substituted by 1 or more F or Cl); B = amino acid; D = 2-5C alkanediyl, 1-5C alkanediyl or -(CH2)n-Yp-(CH2)m-; E = O or S; Y = O, S or NR ; n, m = 0-3; o = 1-3; and p = 0 or 1.

公开(公告)号：AU2351097A

公开(公告)日：1997-11-27

申请号：AU2351097

申请日：1997-05-20

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT ,  HEITSCH HOLGER ,  NOLKEN GERHARD ,  WIRTH KLAUS ,  SCHOLKENS BERNWARD

IPC: C07D277/60 ,  A61K31/38 ,  A61K31/395 ,  A61K31/41 ,  A61K31/425 ,  A61K31/428 ,  A61K31/53 ,  A61P43/00 ,  C07D253/10 ,  C07D277/62 ,  C07D277/64 ,  C07D277/66 ,  C07D277/68 ,  C07D277/70 ,  C07D277/74 ,  C07D277/82 ,  C07D417/12

Abstract: Sulphur-containing bradykinin antagonist compounds of formula (I) and their salts are claimed: one of X1-X3 = COR , and the other X1-X4 = N, CR ; R ,R = H, halo, 1-6C alkyl, OR , SR , NHR , 6-12C aryl, (6-12C aryl)(1-3C alkyl), C(O)OR , C(O)H, 2-5C alkenyl, NO2, SO3R , CN, C(O)NHR , where alkyl, aryl, alkenyl may be substituted by C(O)(O)o(1-5C alkyl), OR , SR , NO2, CN, NHR , halo; R = (II); R ,R = e.g. H; R -R = H, 1-5C alkyl, 3-5C alkenyl, etc.; A = amino acid e.g. methionine, alanine, phenylalanine, etc.; R = H, C(O)(O)o(1-5C alkyl), C(O)(O)o(11-3C alkyl)(6-10C aryl); R = e.g. C(O)DE; D = 2-5C alkendiyl, 1-8C alkandiyl, (CH2)nYo(CH2)m, etc., where any of the groups are optionally substituted by e.g. OR ; E = H, 6-10C aryl, 1-9C heteroaryl, etc.;Y = O, S, NR ; n,m = 0-6; o = 0 or 1.

公开(公告)号：MX9701857A

公开(公告)日：1997-09-30

申请号：MX9701857

申请日：1997-03-12

Applicant: HOECHST AG

Inventor： HEITSCH HOLGER ,  WAGNER ADALBERT ,  WIRTH KLAUS ,  SCHOLKENS BERNWARD ,  NOLKEN GERHARD

IPC: A61K31/47 ,  A61P43/00 ,  C07D215/26 ,  C07D215/48 ,  C07D215/24 ,  C07C217/90

Abstract: Se describen aminoalquil-éteres y acilaminoalquil-éteres, que se distinguen por una alta afinidad para el receptor B2 de bradiquinina y por una solubilidad mejorada en agua. Estos aminoalquil-éteres y acilaminoalquil-éteres se pueden representar por la formula general (I): (Ver Formula) en la que R1, R2, R3 significan alquilo, arilo, alquilarilo, halogeno, hidrogeno, cicloalquilo, CHO, CO-O-alquilo, COOH; R4, R5 significan hidrogeno, halogeno, alcoxi, nitro, ciano, S-alquilo; n significa un numero de 1 a 8; R6 significa hidrogeno, alquilo, alquilalquenilo, alquilarilo; R7 significa hidrogeno y un radical acilo sustituido o sin sustituir. También se describe un procedimiento para la preparacion de los componentes de la formula (I).

公开(公告)号：PT795547E

公开(公告)日：2000-10-31

申请号：PT97103163

申请日：1997-02-27

Applicant: HOECHST AG

Inventor： HEITSCH HOLGER ,  WIRTH KLAUS ,  SCHOLKENS BERNWARD ,  WAGNER ADALBERT ,  NOLKEN GERHARD

IPC: A61K31/47 ,  A61P43/00 ,  C07D215/48 ,  C07D215/26

Abstract: 8-(3-(Aminoalkoxy)-benzyloxy)-quinoline compounds of formula (I) and their salts are new. R1-R3 = H, halo, CHO, COOH, 1-5C alkyl, 6-10C aryl, 1-3C alkyl-(6-10C) aryl, 3-8C cycloalkyl or 1-3C alkoxycarbonyl; R4, R5 = H, halo, NO2, CN, 1-3C alkoxy or 1-3C alkylthio; R6 = H, 1-3C alkyl, 3-5C alkylalkenyl (sic) or 1-3C alkyl-6-10C aryl; R7 = H, 1-6C alkanoyl, alkanoyl (substituted by 1-3C alkoxy, alkylcarbamoyl or aryl), 3-7C alkenoyl, 3-8C cycloalkylcarbonyl, 5-7C cycloalkenylcarbonyl, 1-3C alkoxycarbonyl, aryloxycarbonyl, 6-12C aroyl (optionally substituted by 1-3C alkoxy or halo), alkenoyl (substituted by aryl (optionally substituted by 1-3C alkoxy, 1-3C alkylenedioxy, NO2, CN, halo, 1-3C haloalkyl, hetero-3-8C cycloalkyl (sic), NH2, 1-4C alkylamino, 6-12C heteroaryl-alkanoylamino, aroylamino, 6-12C heteroarylcarbonylamino, 1-5C alkylsulphonylamino, 1-5C alkylureido, alkanoyl, 1-5C alkoxycarbonyl, 1-5C alkylcarbamoyl or arylcarbamoyl), 2-5C acylamino-arylcinnamoyl, 1-3C alkoxycarbonylamino-arylcinnamoyl, 1-4C alkylaminocarbonylaminocinnamoyl, aryl-1-5C alkoxycarbonyl, 1-5C alkylcarbamoyl, arylcarbamoyl, aroylcarbamoyl, alkylsulphonyl, arylsulphonyl, aryl-alkylsulphonyl or phthaloyl (for R6=R7(sic)); n = 1-8; alkyl has 1-6C, aryl has 6-12C, alkanoyl has 2-6C, and alkenoyl has 3-6C unless specified other wise.

公开(公告)号：MX9703724A

公开(公告)日：1998-06-28

申请号：MX9703724

申请日：1997-05-21

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT ,  HEITSCH HOLGER ,  NOLKEN GERHARD ,  WIRTH KLAUS ,  SCHOLKENS BERNWARD

IPC: C07D277/60 ,  A61K31/38 ,  A61K31/395 ,  A61K31/41 ,  A61K31/425 ,  A61K31/428 ,  A61K31/53 ,  A61P43/00 ,  C07D253/10 ,  C07D277/62 ,  C07D277/64 ,  C07D277/66 ,  C07D277/68 ,  C07D277/70 ,  C07D277/74 ,  C07D277/82 ,  C07D417/12

Abstract: Se describen compuestos de la formula I: en donde uno de los radicales X1, X2 o X3, representan C-O-R2 los respectivos otros X1, X2, X3 y X4 son entonces, iguales o diferentes, N o CR1; R1 y R3, iguales o diferentes, son H, halogeno, alquilo (C1-C6), O-R6, S-R6, NHR6, arilo (C6-C12), aril (C6-C12)-alquilo (C2-C3), C(O)-OR6, C(O)-H, alquenilo (C2-C5), NO2, SO3R7, CN o C(O)-NHR8, pudiendo estar alquilo, arilo y el alquenilo eventualmente sustituidos; R2 es un compuesto de la formula (II) R4 y R5, iguales o diferentes, son H, halogeno, OR6, SR6, CN o alquilo (C1-C5); R6, R7 y R8, iguales o diferentes, son H, alquilo (C1-C5), alquenilo (C3-C5), aril (C6-C12)-alquilo (C1-C3), cicloalquilo (C3-C10), cicloalquil (C3-C10)-alquilo (C1-C3), C(O)-(O)0-1-alquilo (C1-C5) o C(O)- (NH) 0-1-alquilo (C1-C5) o C(O)-(O)0-1-alquil (C1-C3)-arilo (C6-C10); R10 es -C(O)-D-E, -C(S)-D-E, -SO2-D-E o hidrogeno; D es alquendiilo (C2-C5), alcandiilo (C1-C8), -(CH2)n-Yo-(CH2)m-, cicloalcandiilo (C3-C10), cicloalquil (C3-C10)-alcandiilo (C1-C3), cicloalquendiilo (C3-C10) o cicloalquenil (C3-C10)-alcandiilo (c1-C3), que eventualmente pueden estar sustituidos; E es H, arilo (C6-C10) o heteroarilo (C1-C9), que eventualmente pueden estar sustituidos; Y es O, S o NR8; así como sus sales fisiologicamente compatibles, un procedimiento para su preparacion y su empleo como agentes curativos y terapéuticos.

公开(公告)号：SK63197A3

公开(公告)日：1997-12-10

申请号：SK63197

申请日：1997-05-20

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT ,  HEITSCH HOLGER ,  NOLKEN GERHARD ,  WIRTH KLAUS ,  SCHOLKENS BERNWARD

IPC: C07D277/60 ,  A61K31/38 ,  A61K31/395 ,  A61K31/41 ,  A61K31/425 ,  A61K31/428 ,  A61K31/53 ,  A61P43/00 ,  C07D253/10 ,  C07D277/62 ,  C07D277/64 ,  C07D277/66 ,  C07D277/68 ,  C07D277/70 ,  C07D277/74 ,  C07D277/82 ,  C07D417/12 ,  C07D417/04

Abstract: Sulphur-containing bradykinin antagonist compounds of formula (I) and their salts are claimed: one of X1-X3 = COR , and the other X1-X4 = N, CR ; R ,R = H, halo, 1-6C alkyl, OR , SR , NHR , 6-12C aryl, (6-12C aryl)(1-3C alkyl), C(O)OR , C(O)H, 2-5C alkenyl, NO2, SO3R , CN, C(O)NHR , where alkyl, aryl, alkenyl may be substituted by C(O)(O)o(1-5C alkyl), OR , SR , NO2, CN, NHR , halo; R = (II); R ,R = e.g. H; R -R = H, 1-5C alkyl, 3-5C alkenyl, etc.; A = amino acid e.g. methionine, alanine, phenylalanine, etc.; R = H, C(O)(O)o(1-5C alkyl), C(O)(O)o(11-3C alkyl)(6-10C aryl); R = e.g. C(O)DE; D = 2-5C alkendiyl, 1-8C alkandiyl, (CH2)nYo(CH2)m, etc., where any of the groups are optionally substituted by e.g. OR ; E = H, 6-10C aryl, 1-9C heteroaryl, etc.;Y = O, S, NR ; n,m = 0-6; o = 0 or 1.

公开(公告)号：AU1621797A

公开(公告)日：1997-09-18

申请号：AU1621797

申请日：1997-03-11

Applicant: HOECHST AG

Inventor： HEITSCH HOLGER ,  WAGNER ADALBERT ,  WIRTH KLAUS ,  SCHOLKENS BERNWARD ,  NOLKEN GERHARD

IPC: C07D215/48 ,  A61K31/47 ,  A61P43/00 ,  C07D215/26

Abstract: 8-(3-(Aminoalkoxy)-benzyloxy)-quinoline compounds of formula (I) and their salts are new. R1-R3 = H, halo, CHO, COOH, 1-5C alkyl, 6-10C aryl, 1-3C alkyl-(6-10C) aryl, 3-8C cycloalkyl or 1-3C alkoxycarbonyl; R4, R5 = H, halo, NO2, CN, 1-3C alkoxy or 1-3C alkylthio; R6 = H, 1-3C alkyl, 3-5C alkylalkenyl (sic) or 1-3C alkyl-6-10C aryl; R7 = H, 1-6C alkanoyl, alkanoyl (substituted by 1-3C alkoxy, alkylcarbamoyl or aryl), 3-7C alkenoyl, 3-8C cycloalkylcarbonyl, 5-7C cycloalkenylcarbonyl, 1-3C alkoxycarbonyl, aryloxycarbonyl, 6-12C aroyl (optionally substituted by 1-3C alkoxy or halo), alkenoyl (substituted by aryl (optionally substituted by 1-3C alkoxy, 1-3C alkylenedioxy, NO2, CN, halo, 1-3C haloalkyl, hetero-3-8C cycloalkyl (sic), NH2, 1-4C alkylamino, 6-12C heteroaryl-alkanoylamino, aroylamino, 6-12C heteroarylcarbonylamino, 1-5C alkylsulphonylamino, 1-5C alkylureido, alkanoyl, 1-5C alkoxycarbonyl, 1-5C alkylcarbamoyl or arylcarbamoyl), 2-5C acylamino-arylcinnamoyl, 1-3C alkoxycarbonylamino-arylcinnamoyl, 1-4C alkylaminocarbonylaminocinnamoyl, aryl-1-5C alkoxycarbonyl, 1-5C alkylcarbamoyl, arylcarbamoyl, aroylcarbamoyl, alkylsulphonyl, arylsulphonyl, aryl-alkylsulphonyl or phthaloyl (for R6=R7(sic)); n = 1-8; alkyl has 1-6C, aryl has 6-12C, alkanoyl has 2-6C, and alkenoyl has 3-6C unless specified other wise.