公开(公告)号：KR850001269B1

公开(公告)日：1985-09-04

申请号：KR810003193

申请日：1981-08-28

Applicant: HOECHST AG

Inventor： GEIGER ROLF ,  TEETZ VOLKER ,  URBACH HANSJORG ,  SCHOLKENS BERNWARD ,  HENNIG RAINER

IPC: C07D209/42 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/47 ,  A61K31/472 ,  A61K38/00 ,  A61P9/12 ,  C07D217/26 ,  C07D233/64 ,  C07D241/20 ,  C07D307/54 ,  C07D309/10 ,  C07D317/66 ,  C07D333/24 ,  C07D335/02 ,  C07D339/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065 ,  C07K5/078 ,  C07K14/81

公开(公告)号：KR850001288B1

公开(公告)日：1985-09-09

申请号：KR840006028

申请日：1984-09-27

Applicant: HOECHST AG

Inventor： GEIGER ROLF ,  TEETA VOLKER ,  URBACH HANSJORG ,  SCHOLKENS BERNWARD ,  HENNIG RAINER

IPC: C07D209/42 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/47 ,  A61K31/472 ,  A61K38/00 ,  A61P9/12 ,  C07D217/26 ,  C07D233/64 ,  C07D241/20 ,  C07D307/54 ,  C07D309/10 ,  C07D317/66 ,  C07D333/24 ,  C07D335/02 ,  C07D339/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065 ,  C07K5/078 ,  C07K14/81

公开(公告)号：KR850001270B1

公开(公告)日：1985-09-04

申请号：KR840005957

申请日：1984-09-27

Applicant: HOECHST AG

Inventor： GEIGER ROLF ,  TEETZ VOLKER ,  URBACH HANSJORG ,  SCHOLKENS BERNWARD ,  HENNIG RAINER

IPC: C07D209/42 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/47 ,  A61K31/472 ,  A61K38/00 ,  A61P9/12 ,  C07D217/26 ,  C07D233/64 ,  C07D241/20 ,  C07D307/54 ,  C07D309/10 ,  C07D317/66 ,  C07D333/24 ,  C07D335/02 ,  C07D339/08 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065 ,  C07K5/078 ,  C07K14/81

公开(公告)号：US3920627A

公开(公告)日：1975-11-18

申请号：US46783274

申请日：1974-05-07

Applicant: HOECHST AG

Inventor： WISSMANN HANS ,  GEIGER ROLF ,  LINDNER ERNST ,  SCHOLKENS BERNWARD

IPC: C07K7/06 ,  A61K38/00 ,  A61P5/00 ,  C07C231/00 ,  C07K1/113 ,  C07K7/14 ,  C07C103/52 ,  A61K37/26

CPC classification number: C07K7/14 ,  A61K38/00 ,  Y02P20/55

Abstract: Peptides of the formula I X-Arg-Val-Tyr-Ile-His-Pro-Phegly-OH (I) in which X represents the radical of an aliphatic carboxylic acid of up to 5 carbon atoms or the phthalic acid radical, and Phegly-OH represents L-C-phenylglycine, and a process of preparing them by condensing the O-tert. butyl ester of compound I, in which tyrosine is protected by tert. butyl, and X represents hydrogen, with carboxylic acids of the formula X-OH, in which X has the first mentioned meaning, according to the condensation methods usually employed in peptide chemistry.

Abstract translation: 式I X-Arg-Val-Tyr-Ile-His-Pro-Phegly-OH（I）的肽，其中X表示至多5个碳原子的脂肪族羧酸基团或邻苯二甲酸基团，Phegly -OH表示LC-苯基甘氨酸，以及通过将O-叔丁基缩合制备它们的方法。 化合物I的丁酯，其中酪氨酸被叔保护。 丁基，X表示氢，根据肽化学中通常使用的缩合方法，具有式X-OH的羧酸，其中X具有第一个提及的含义。

公开(公告)号：JPH10279563A

公开(公告)日：1998-10-20

申请号：JP7942398

申请日：1998-03-26

Applicant: HOECHST AG

Inventor： HEITSCH HOLGER DR ,  WAGNER ADALBERT DR ,  WIRTH KLAUS DR ,  SCHOLKENS BERNWARD

IPC: C07D215/24 ,  A61K31/395 ,  A61K31/47 ,  A61K31/495 ,  A61P1/16 ,  A61P43/00 ,  C07D215/26 ,  C07D241/36 ,  C07D401/12 ,  C07D405/12

Abstract: PROBLEM TO BE SOLVED: To obtain a novel compound that has high affinity to bradykinin receptor and improved pharmacodynamic effect and is useful for treatment and prevention of hepatocirrhosis and Alzheimer's disease. SOLUTION: This novel compound is represented by formula I D is formula II [X is N, C-R (R is H, a halogen, a lower alkyl; X is N), C-R (R is H, a lower alkyl, an alkenyl; X is N), C-R (R is same as R )]; B is formula III (R and R are each H, a halogen, cyano; R is nitro, amino); R and R are each H, a halogen, a 1-3C alkyl}, typically 8-[6-chloro-2-cyano-3-(N- ethylaminocarbonylglycyloxy)-2-methylquinoline. The objective compound is prepared by reaction of a compound of formula IV with a compound of formula V in an inert solvent in the presence of a metal hydride or an alkali metal carbonate at 0-60 deg.C.

公开(公告)号：SK280787B6

公开(公告)日：2000-07-11

申请号：SK397990

申请日：1990-08-13

Applicant: HOECHST AG

Inventor： HENKE STEPHAN ,  BREIPOHL GERHARD ,  KNOLLE JOCHEN ,  SCHOLKENS BERNWARD ,  GERHARDS HERMANN

IPC: A61K38/00 ,  A61K38/08 ,  A61P43/00 ,  C07K1/06 ,  C07K7/06 ,  C07K7/08 ,  C07K7/18

Abstract: Peptides of the formula (I) A-B-C-E-F-K-(D)-Phe-G-M-F'-I (1) in which A is hydrogen, alkyl, alkanoyl, alkoxycarbonyl, alkylsulphonyl, cycloalkyl, aryl, aryloyl, arylsulphonyl, heteroaryl or an amino acid, each of which can optionally be substituted, B is a basic amino acid, C is a di- or tripeptide, E is the residue of an aromatic amino acid, F is, independently of one another, an amino acid which is optionally substituted in the side chain or is a direct bond, G is an amino acid, F' is defined as F o r can be -NH-(CH2)2-8 or optionally a direct bond, I is -OH, -NH2 or -NHC2H5, and K is a radical -NH-(CH2)1-4-CO- or is a direct bond, act as bradykinin antagonists. Their therapeutic uses comprise all pathological states promoted, induced or assisted by bradykinin and bradykinin-related peptides. The peptides of the formula (I) are prepared by known methods of peptide synthesis.

公开(公告)号：SK381192A3

公开(公告)日：1998-06-03

申请号：SK381192

申请日：1992-12-21

Applicant: HOECHST AG

Inventor： HEITSCH HOLGER ,  HENNING RAINER ,  WAGNER ADALBERT ,  GERHARDS HERMANN ,  BECKER REINHARD ,  SCHOLKENS BERNWARD

IPC: A61K31/4164 ,  A61K31/64 ,  A61P9/10 ,  A61P9/12 ,  A61K31/415 ,  C07D233/84 ,  C07D233/86 ,  C07D233/90

Abstract: Compounds of the formula (I) in which R is, for example, ethyl, R is, for example, methyl, n is, for example, zero, R is, for example, COOH and R is, for example, SO2NHCONHCH3 are highly active antagonists of angiotensin II receptors.

公开(公告)号：MX9604657A

公开(公告)日：1998-04-30

申请号：MX9604657

申请日：1996-10-08

Applicant: HOECHST AG

Inventor： TOEPFER ALEXANDER ,  KRETZSCHMAR GERHARD ,  SCHOLKENS BERNWARD ,  KLEMM PETER ,  HULS CHRISTOPH ,  SEIFFGE DIRK

IPC: A61K31/215 ,  C07D295/20 ,  A61K31/33 ,  A61K31/40 ,  A61K31/435 ,  A61K31/445 ,  A61K31/495 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61P3/08 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D207/08 ,  C07D207/16 ,  C07D211/34 ,  C07D211/62 ,  C07D405/00 ,  C07H15/203 ,  C07H15/207 ,  C07H17/00 ,  C07H19/04 ,  C07D405/10

Abstract: La invencion se refiere a conjugados que consisten en derivados de piperidina o pirrolidina una o varias veces carboxilados y en piranosas, furanosas o polialcoholes enlazados a través de una cadena o un ciclo. Los grupos carboxilo de los derivados de piperidina pueden asentarse directamente en el anillo o estar enlazados con el anillo a través de una cadena corta. La invencion se refiere, además, a la preparacion de estos compuestos, así como a su empleo para la preparacion de medicamentos y agentes de diagnostico.

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.