公开(公告)号：JPH1059969A

公开(公告)日：1998-03-03

申请号：JP16346797

申请日：1997-06-06

Applicant: HOECHST AG

Inventor： GEBERT ULRICH DR ,  WOLF ERHARD DR ,  DEFOSA ELISABETH DR ,  HEINELT UWE DR ,  ANAGNOSTOPULOS HIRISTO ,  RUDOLPHI KARL DR ,  GROME JOHN J DR

IPC: C07D473/04 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61P7/08 ,  A61P9/00 ,  A61P9/10 ,  A61P31/04 ,  A61P31/12 ,  A61P43/00 ,  C07D473/06

Abstract: PROBLEM TO BE SOLVED: To obtain a therapeutic agent and a preventive for shock disease, by using a theophylline derivative. SOLUTION: A preparation having antishock action is obtained by using a theophyline derivative containing at least one ether function at a structurally modified methyl group at the 1-position. The compound having the substitution type is a new xanthin compound of formula I (R is a 1-5C alkyl, phenyl, etc.; A is a 1-4C alkylene cross-linking; R is a 1-5C alkyl, a 3-6C cycloalkyl, etc.). The compound of formula I is obtained by reacting a 3-substituted xanthin of formula II with a reagent of the formula R -X (R is benzyl, benzhydryl, etc.; X is Cl, Br, sulfonic acid ester, etc.) to give a 1,3,7-trisubstituted xanthin of formula III and removing R . The compound if effective for treating and preventing systemic inflammatory reaction syndrome, septic shock, multiple organ insufficiency, acute dyspnea syndrome, hemorrhagic and traumatic shock.

公开(公告)号：DE3865443D1

公开(公告)日：1991-11-21

申请号：DE3865443

申请日：1988-01-26

Applicant: HOECHST AG

Inventor： WOLF ERHARD DR ,  ROSSMANITH ERHARD ,  BARTLETT ROBERT R DR ,  SCHLEYERBACH RUDOLF DR

IPC: A61K31/55 ,  A61P29/00 ,  A61P37/00 ,  C07D243/08

Abstract: 1-(4-Hydroxy-3,4-di-tert. -butyl-benzoyl) -homopiperazine derivs. of formula (I) and their physiologically tolerable acid addn. salts are new. R1=H, (1-6C alkoxy) carbonyl, or opt. nuclear-substd. benzoyloxycarbonyl.

公开(公告)号：DE3702755A1

公开(公告)日：1988-08-11

申请号：DE3702755

申请日：1987-01-30

Applicant: HOECHST AG

Inventor： WOLF ERHARD DR ,  ROSSMANITH ERHARD ,  BARTLETT ROBERT DR ,  SCHLEYERBACH RUDOLF DR

IPC: A61K31/55 ,  A61P29/00 ,  A61P37/00 ,  C07D243/08 ,  C07D295/18 ,  C07D241/08 ,  C07D317/58 ,  C07D295/20 ,  C07D521/00 ,  C07C103/82 ,  C07C103/78 ,  C07C103/76 ,  A61K31/495 ,  C07C83/10 ,  A61K31/165

Abstract: 1-(4-Hydroxy-3,5-di-tert.-butylbenzoyl)homopiperazine and various derivatives thereof substituted on the nitrogen are prepared starting from 4-hydroxy-3,5-di-tert.-butylbenzoic acid or its derivatives and homopiperazine or appropriate derivatives thereof. The compounds and their physiologically tolerated acid addition salts are suitable for the treatment of inflammatory and painful, in particular inflammatory rheumatic, disorders.

公开(公告)号：HU225040B1

公开(公告)日：2006-05-29

申请号：HU9701016

申请日：1997-06-06

Applicant: HOECHST AG

Inventor： WOLF ERHARD DR ,  DEFOSSA ELISABETH DR ,  RUDOLPHI KARL DR ,  GROME JOHN J DR ,  ANAGNOSTOPULOS HIRISTO ,  GEBERT ULRICH DR ,  HEINELT UWE DR

IPC: C07D473/04 ,  C07D473/06 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61P7/08 ,  A61P9/00 ,  A61P9/10 ,  A61P31/04 ,  A61P31/12 ,  A61P43/00

Abstract: The use of at least one theophylline 1-ether analogue of formula (I) or its diastereoisomer or salt is claimed for the preparation of a medicament for the treatment and/or prophylaxis of shock states. R1 = 1-5C alkyl or (1-2C)alkoxy-(1-3C) alkyl; or phenyl or phenyl-(1-2C)alkyl (both optionally mono- or dihalo-substituted in the ring); A = 1-4C alkylene; R2 = 1-5C alkyl, 3-6C cycloalkyl, 4-8C cycloalkyl, phenyl or phenyl-(1-2C)alkyl. Compounds (I) and their stereoisomers and salts are new, with the exception of compounds in which (a) R2 = n-propyl, R1= Me or Et and A = CH2CH2 or (b) R2 = n-propyl, R1 = Me and A = (CH2)3. Certain intermediates in the preparation of (I) are also new.

公开(公告)号：DE19629815A1

公开(公告)日：1998-01-29

申请号：DE19629815

申请日：1996-07-24

Applicant: HOECHST AG

Inventor： GEBERT ULRICH DR ,  WOLF ERHARD DR ,  DEFOSA ELISABETH DR ,  HEINELT UWE DR ,  ANAGNOSTOPULOS HIRISTO ,  RUDOLPHI KARL DR ,  GROME JOHN J DR

IPC: C07D473/06 ,  A61K31/52 ,  C07D473/04 ,  C07D473/18

Abstract: The use of at least one theophylline 1-ether analogue of formula (I) or its diastereoisomer or salt is claimed for the preparation of a medicament for the treatment and/or prophylaxis of shock states. R1 = 1-5C alkyl or (1-2C)alkoxy-(1-3C) alkyl; or phenyl or phenyl-(1-2C)alkyl (both optionally mono- or dihalo-substituted in the ring); A = 1-4C alkylene; R2 = 1-5C alkyl, 3-6C cycloalkyl, 4-8C cycloalkyl, phenyl or phenyl-(1-2C)alkyl. Compounds (I) and their stereoisomers and salts are new, with the exception of compounds in which (a) R2 = n-propyl, R1= Me or Et and A = CH2CH2 or (b) R2 = n-propyl, R1 = Me and A = (CH2)3. Certain intermediates in the preparation of (I) are also new.

公开(公告)号：DE4433244A1

公开(公告)日：1996-03-28

申请号：DE4433244

申请日：1994-09-19

Applicant: HOECHST AG

Inventor： WOLF ERHARD DR ,  ROSMANITH ERHARD ,  THORWART WERNER DR ,  RAISS RUTH DR ,  WEITHMANN KLAUS ULRICH DR

IPC: A61K31/66 ,  A61K31/665 ,  A61K31/675 ,  A61P29/00 ,  A61P43/00 ,  C07F9/30 ,  C07F9/32 ,  C07F9/38 ,  C07F9/40 ,  C07F9/48 ,  C07F9/58 ,  C07F9/59 ,  C07F9/6509 ,  C07F9/6512 ,  C07F9/6533 ,  C07F9/655 ,  C07F9/547 ,  A61K31/33

Abstract: Medicaments contg. alpha-amino-3,5-di-t-butyl-4-hydroxybenzyl- phosphorus cpds. of formula (I) or their salts or stereoisomers are new: R1, R2 = H, 1-12C alkyl*, 1-12C alkyl (substd. by one or more of (a) phenyl*; (b) phenyl substd. by 1-3 halo, 1-3C alkyl, 1-3C alkoxy, methylenedioxy, NO2, NH2, amidino, guanidino, OH, 2-7C alkoxycarbonyl and/or CN; (c) 5- or 6-membered monocyclic satd. heterocyclyl; (d) amino opt. mono- or disubstd. by 1-3C alkyl; and (e) 2-4C alkoxycarbonyl; tetrahydronaphthyl; phenyl*; phenyl substd. by 1-3 f 1-4C alkyl, 1-4C haloalkyl, halo*, NO2, SO2NH2, amidino, guanidino, 1-3C alkoxy, methylenedioxy, OH, COOH, CN, 2-4C alkoxycarbonyl, CH=CHCOOR (R = H or 1-3C alkyl), NH2 and/or NHQ(Q = a gp. of formula (I) minus NR1R2); naphthyl*; naphthyl substd. by one or more of the above phenyl substits.; heteroaryl opt. substd. by one or more of phenyl, benzyl and the above phenyl substits.; or NR1R2 = a 4-7-membered ring* or a 5- 7-membered ring in which a C atom is replaced by O, N, NPh or NQ; X, Y = H, 1-6C alkyl, 1-6C alkoxy, 3-6C alkenyloxy, OPh or OH. Also claimed are : (A) cpds. (I) where the asterisked definitions are omitted; (B) cpds. (I) where R1 = phenyl or mono-, di- or trihalophenyl, R2 = H and X and Y are as above but not alkoxy.

公开(公告)号：CZ292205B6

公开(公告)日：2003-08-13

申请号：CZ174397

申请日：1997-06-05

Applicant: HOECHST AG

Inventor： GEBERT ULRICH DR ,  WOLF ERHARD DR ,  DEFOSSA ELISABETH DR ,  HEINELT UWE DR ,  ANAGNOSTOPULOS HIRISTO DB ,  RUDOLPHI KARL DR ,  GROME JOHN J DR

IPC: C07D473/04 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61P7/08 ,  A61P9/00 ,  A61P9/10 ,  A61P31/04 ,  A61P31/12 ,  A61P43/00 ,  C07D473/06

Abstract: In the present invention there are disclosed compounds of the general formula I, in which Re1 represents alkyl containing 1 to 5 carbon atoms, alkoxy containing 1 to 2 carbon atoms, alkyl with 1 to 3 carbon atoms or optionally halogen-substituted phenyl or phenylalkyl containing 1 to 2 carbon atoms in the alkyl moiety, A represents alkylene containing 1 to 4 carbon atoms, and Re2 denotes alkyl containing 1 to 5 carbon atoms, cycloalkyl containing 3 to 6 carbon atoms, cycloalkylalkyl containing 4 to 8 carbon atoms in the cycloalkyl moiety, phenyl or phenylalkyl having 1 to 2 carbon atoms in the alkyl moiety. The above-specified compounds are suitable for preparing medicaments intended for the treatment and prophylaxis of shock diseases. Further claimed is also process of their preparation and intermediates in their preparation of the general formula VIII, in which Rea represents benzyl.

公开(公告)号：CZ174397A3

公开(公告)日：1997-12-17

申请号：CZ174397

申请日：1997-06-05

Applicant: HOECHST AG

Inventor： GEBERT ULRICH DR ,  WOLF ERHARD DR ,  DEFOSSA ELISABETH DR ,  HEINELT UWE DR ,  ANAGNOSTOPULOS HIRISTO DB ,  RUDOLPHI KARL DR ,  GROME JOHN J DR

IPC: C07D473/04 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61P7/08 ,  A61P9/00 ,  A61P9/10 ,  A61P31/04 ,  A61P31/12 ,  A61P43/00 ,  C07D473/06 ,  C07D487/04 ,  A61K31/41

Abstract: The use of at least one theophylline 1-ether analogue of formula (I) or its diastereoisomer or salt is claimed for the preparation of a medicament for the treatment and/or prophylaxis of shock states. R1 = 1-5C alkyl or (1-2C)alkoxy-(1-3C) alkyl; or phenyl or phenyl-(1-2C)alkyl (both optionally mono- or dihalo-substituted in the ring); A = 1-4C alkylene; R2 = 1-5C alkyl, 3-6C cycloalkyl, 4-8C cycloalkyl, phenyl or phenyl-(1-2C)alkyl. Compounds (I) and their stereoisomers and salts are new, with the exception of compounds in which (a) R2 = n-propyl, R1= Me or Et and A = CH2CH2 or (b) R2 = n-propyl, R1 = Me and A = (CH2)3. Certain intermediates in the preparation of (I) are also new.

公开(公告)号：AT68488T

公开(公告)日：1991-11-15

申请号：AT88101054

申请日：1988-01-26

Applicant: HOECHST AG

Inventor： WOLF ERHARD DR ,  ROSSMANITH ERHARD ,  BARTLETT ROBERT R DR ,  SCHLEYERBACH RUDOLF DR

IPC: A61K31/55 ,  A61P29/00 ,  A61P37/00 ,  C07D243/08

公开(公告)号：CH627444A5

公开(公告)日：1982-01-15

申请号：CH696376

申请日：1976-06-02

Applicant: HOECHST AG

Inventor： ERTEL HARTMUT DR ,  HEUBACH GUENTHER DR ,  WOLF ERHARD DR

IPC: A61K31/275 ,  A61K31/357 ,  A61K31/36 ,  A61K31/42 ,  A61P25/04 ,  A61P29/00 ,  C07C67/00 ,  C07C233/00 ,  C07C253/00 ,  C07C255/30 ,  C07C255/58 ,  C07C313/00 ,  C07C323/41 ,  C07D261/18 ,  C07D317/58 ,  C07D317/66 ,  G05D16/06 ,  G05D23/12 ,  G09F7/00 ,  H01F7/02 ,  H01J3/02 ,  H01J23/00 ,  H01J23/065 ,  H01J23/087 ,  H01J23/42 ,  H01J25/38 ,  H01J29/38 ,  C07C121/417