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：NO301878B1

公开(公告)日：1997-12-22

申请号：NO940023

申请日：1994-01-04

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT ,  BHATNAGAR NEERJA ,  BUENDIA JEAN ,  GRIFFOUL CHRISTINE

IPC: B01J23/44 ,  A61K31/235 ,  A61K31/41 ,  C07B37/04 ,  C07B61/00 ,  C07C41/48 ,  C07C45/61 ,  C07C45/71 ,  C07C47/546 ,  C07C67/30 ,  C07C67/343 ,  C07C69/76 ,  C07C69/767 ,  C07C253/30 ,  C07C255/37 ,  C07C255/40 ,  C07C255/56 ,  C07C303/40 ,  C07C311/09 ,  C07C311/48 ,  C07C311/51 ,  C07C311/52 ,  C07C311/53 ,  C07C311/54 ,  C07C311/57 ,  C07C311/58 ,  C07D257/04

Abstract: The invention relates to a method for the preparation of a compound of the general formula (I) in which X represents an optionally protected formyl group and R denotes a group which is itself inert to the reaction conditions of the synthesis, for example -CN, characterised in that a compound of the general formula (II) where X is as defined above, is reacted with a substituted phenyl halogen compound of the formula (III) where Hal denotes e.g. bromine. The compounds are useful intermediates for pharmaceutical synthesis.

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：ZA9702129B

公开(公告)日：1997-09-15

申请号：ZA9702129

申请日：1997-03-12

Applicant: HOECHST AG

Inventor： HEITSCH HOLGER ,  WAGNER ADALBERT ,  WIRTH KLAUS ,  SCHOELKENS BERNWARD ,  NOELKEN GERHARD

IPC: C07D215/48 ,  A61K31/47 ,  A61P43/00 ,  C07D215/26 ,  C07D ,  A61K

CPC classification number: C07D215/26

公开(公告)号：CA2199771A1

公开(公告)日：1997-09-13

申请号：CA2199771

申请日：1997-03-12

Applicant: HOECHST AG

Inventor： HEITSCH HOLGER ,  WAGNER ADALBERT ,  WIRTH KLAUS ,  SCHOELKENS BERNWARD ,  NOELKEN GERHARD

IPC: C07D215/48 ,  A61K31/47 ,  A61P43/00 ,  C07D215/26 ,  C07D471/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/505

Abstract: Aminoalkyl and acylaminoalkyl ethers, process for their preparation, and their use as bradykinin receptor antagonists Aminoalkyl and acylaminoalkyl ethers which are distinguished by high affinity for the bradykinin B2 receptor and improved solubility in water are described. These aminoalkyl and acylaminoalkyl ethers can be represented by the formula (I) (See Fig. I) in which R1,R2,R3 are alkyl, aryl, alkylaryl, halogen, hydrogen, cycloalkyl, CHO, COO-alkyl, COOH; R4,R5 are hydrogen, halogen, alkoxy, nitro, cyano, S-alkyl; n is a number from 1 to 8; R6 is hydrogen, alkyl, alkylalkenyl, alkylaryl; R7 is hydrogen and a substituted or unsubstituted acyl radical. A process for preparing the compounds of the formula (I) is likewise described.

公开(公告)号：HU9700914D0

公开(公告)日：1997-07-28

申请号：HU9700914

申请日：1997-05-20

Applicant: HOECHST AG

Inventor： HEITSCH HOLGER ,  NOELKEN GERHARD ,  SCHOELKENS BERNWARD ,  WAGNER ADALBERT ,  WIRTH KLAUS

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：AU677247B2

公开(公告)日：1997-04-17

申请号：AU5302994

申请日：1994-01-04

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT ,  BHATNAGAR NEERJA ,  BUENDIA JEAN ,  GRIFFOUL CHRISTINE

IPC: B01J23/44 ,  A61K31/235 ,  A61K31/41 ,  C07B37/04 ,  C07B61/00 ,  C07C41/48 ,  C07C45/61 ,  C07C45/71 ,  C07C47/546 ,  C07C67/30 ,  C07C67/343 ,  C07C69/76 ,  C07C69/767 ,  C07C253/30 ,  C07C255/37 ,  C07C255/40 ,  C07C255/56 ,  C07C303/40 ,  C07C311/09 ,  C07C311/48 ,  C07C311/51 ,  C07C311/52 ,  C07C311/53 ,  C07C311/54 ,  C07C311/57 ,  C07C311/58 ,  C07D257/04

Abstract: The invention relates to a method for the preparation of a compound of the general formula (I) in which X represents an optionally protected formyl group and R denotes a group which is itself inert to the reaction conditions of the synthesis, for example -CN, characterised in that a compound of the general formula (II) where X is as defined above, is reacted with a substituted phenyl halogen compound of the formula (III) where Hal denotes e.g. bromine. The compounds are useful intermediates for pharmaceutical synthesis.

公开(公告)号：NO971238D0

公开(公告)日：1997-03-18

申请号：NO971238

申请日：1997-03-18

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT ,  HEITSCH HOLGER ,  NOELKEN GERHARD ,  WIRTH KLAUS ,  SCHOELKENS 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：NO179705B

公开(公告)日：1996-08-26

申请号：NO950118

申请日：1995-01-12

Applicant: HOECHST AG

Inventor： WAGNER ADALBERT ,  HENNING RAINER ,  GERHARDS HERMANN ,  SCHOLKENS BERNWARD

IPC: C07D20060101 ,  C07D233/84 ,  C07D233/90