公开(公告)号：US3915980A

公开(公告)日：1975-10-28

申请号：US42160373

申请日：1973-12-04

Applicant: HOECHST AG

Inventor： GEBERT ULRICH ,  GRANZER ERNOLD

IPC: C07D233/84 ,  C07D233/64

CPC classification number: C07D233/84

Abstract: Imidazolyl-(2)-thioalkanoic acid ester of the formula I

in which R stands for phenyl, phen-(C1-C3)alkyl, R1 stands for hydrogen or (C1-C3)-alkyl and R2 and R3 each stands for (C1-C3)-alkyl, AND THE PHYSIOLOGICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, PROCESS FOR PREPARING THEM AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM AS ACTIVE SUBSTANCE.

Abstract translation: 式I的咪唑基 - （2） - 硫代链烷酸酯，其中R代表苯基，苯 - （C1-C3）烷基，R1代表氢或（C1-C3） - 烷基，R2和R3各自代表（C1 -C 3） - 烷基，以及生理学上可接受的酸添加剂，其制备方法及其作为活性物质的药物制剂。

公开(公告)号：US3915984A

公开(公告)日：1975-10-28

申请号：US42286173

申请日：1973-12-07

Applicant: HOECHST AG

Inventor： GEBERT ULRICH ,  BABEJ MILOS ,  GRANZER ERNOLD

IPC: C07D233/60 ,  C07D235/06 ,  C07D521/00

CPC classification number: C07D235/06 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

Abstract: Compounds of the formula

IN WHICH R1 and R2 each stands for a hydrogen atom or together they stand for the group -CH CH-CH CH- which may carry one or more lower alkyl, halogeno-alkyl or alkoxy groups, halogen atoms or NO2-groups, and R3 and R4, independently of one another, each stands for a hydrogen atom, a lower alkyl, halogeno-alkyl, alkoxy or halogeno-alkoxy group, a halogen atom or NO2 or together they stand as a -CH CH-CH CH- group with the benzene nucleus for the naphthyl group, AND PHYSIOLOGICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, PROCESS FOR PREPARING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AS ACTIVE SUBSTANCE.

Abstract translation: 式Ⅰ的化合物，其中R 1和R 2各自代表氢原子，或一起代表基团-CH = CH-CH = CH-，其可以携带一个或多个低级烷基，卤代烷基或烷氧基，卤素原子或 NO 2 - 基，R 3和R 4彼此独立地表示氢原子，低级烷基，卤代 - 烷基，烷氧基或卤代 - 烷氧基，卤素原子或NO 2，或者一起表示-CH = CH-CH = CH-基团与萘基的萘基，以及生理学上可接受的酸加法盐，其制备它们和作为活性物质的药物组合物的方法。

公开(公告)号：WO8700523A3

公开(公告)日：1987-02-26

申请号：PCT/EP8600401

申请日：1986-07-08

Applicant: HOECHST AG ,  GEBERT ULRICH ,  OKYAYUZ BAKLOUTI ISMAHAN ,  THORWART WERNER

Inventor： GEBERT ULRICH ,  OKYAYUZ-BAKLOUTI ISMAHAN ,  THORWART WERNER

IPC: C07D473/00 ,  A61K31/52 ,  A61K31/522 ,  A61P3/00 ,  A61P9/00 ,  A61P9/08 ,  A61P25/28 ,  C07D473/04 ,  C07D473/06 ,  C07D473/08

CPC classification number: C07D473/06 ,  C07D473/08

Abstract: Tertiary hydroxyalkylxanthines having the general formula (I), characterized by the fact that at least one of the residues R1 and R3 represents a tertiary hydroxyalkyl group of formula (Ia) in which R4 represents an alkyl group having up to 3 carbon atoms and n a whole number from 2 to 5; the other residue which may remain R1 or R3 is a hydrogen atom or an aliphatic hydrocarbon residue R5 having up to 6 carbon atoms, in which the carbon chain may be separated by a maximum of two oxygen atoms or be substituted by an oxo group or two hydroxy groups at the most, and R2 represents an alkyl group with 1 to 4 carbon atoms. Also described is a process for manufacturing these compounds, which are suitable for the manufacture of medicines, in particular for use in the prevention and/or treatment of peripheral and/or cerebral irrigation disorders.

公开(公告)号：WO9605854A3

公开(公告)日：1996-04-11

申请号：PCT/EP9503126

申请日：1995-08-07

Applicant: HOECHST AG ,  UNIV LEUVEN KATH ,  SCHOENHARTING MARTIN ,  GEBERT ULRICH ,  WAER MARK

Inventor： SCHOENHARTING MARTIN ,  GEBERT ULRICH ,  WAER MARK

IPC: A61K31/453 ,  A61K38/12 ,  A61K38/13 ,  A61K31/445 ,  A61K31/52

CPC classification number: A61K31/453 ,  A61K38/12 ,  A61K38/13 ,  A61K31/52 ,  A61K31/445 ,  A61K31/522 ,  A61K2300/00

Abstract: Combination preparations which contain cyclosporin A and a xanthine derivative or FK506 and a xanthine derivative or rapamycin and a xanthine derivative are suitable for use in organ transplantation, cancer, viral diseases or in autoimmune disorders such as systemic lupus erythematosus, rheumatoid arthritis, psoriasis, pemphigus, atopic dermatitis, myositis, multiple sclerosis, nephrotic syndrome (in particular glomerulonephritis), ulcerative colitis or juvenile diabetes.

公开(公告)号：PL186576B1

公开(公告)日：2004-01-30

申请号：PL32041397

申请日：1997-06-06

Applicant: HOECHST AG

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

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

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：AT233095T

公开(公告)日：2003-03-15

申请号：AT95929805

申请日：1995-08-07

Applicant: HOECHST AG ,  UNIV LEUVEN KATH

Inventor： SCHOENHARTING MARTIN ,  GEBERT ULRICH ,  WAER MARK

IPC: A61K31/445 ,  A61K31/453 ,  A61K31/52 ,  A61K38/12 ,  A61K38/13 ,  C04B35/26 ,  A61P37/06

Abstract: Xanthines of the formula Iare useful in producing a superadditive increase in immunosuppressive action when combined with immunosuppressive compounds such as CysA or FK506.

公开(公告)号：AU712277B2

公开(公告)日：1999-11-04

申请号：AU2469897

申请日：1997-06-05

Applicant: HOECHST AG

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

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

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：HU9701018A2

公开(公告)日：1998-12-28

申请号：HU9701018

申请日：1997-06-06

Applicant: HOECHST AG

Inventor： DEFOSSA ELISABETH ,  GEBERT ULRICH ,  GROME JOHN J ,  HEINELT UWE ,  RUDOLPHI KARL

IPC: C07D473/06 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61P9/00 ,  A61P9/02 ,  A61P9/08 ,  A61P9/10 ,  A61P25/28 ,  C07D473/02 ,  C07D473/04 ,  C07D487/04

Abstract: omega -Amino-hydroxyalkynyl substituted xanthine derivatives of formula (I) are new: R and/or R = group of formula (a) or (b); and when only one of R and R is group (a) or (b) the other is H or R ; R = 1-6C alkyl, 3-6C cycloalkyl or 4-8C cycloalkyl-alkyl; R = 1-5C alkyl, 3-6C cycloalkyl or 4-8C cycloalkyl-alkyl; R = H or 1-3C alkyl; R -R = H, 1-6C alkyl, 3-6C cycloalkyl, 4-8C cycloalkyl-alkyl, Ar-1-2C alkyl or tri(1-4C alkyl)silyl; or NR R = 4-7 membered saturated ring optionally substituted by 1-4 1-4C alkyl and/or containing O, S, SO, SO2 or NR in place of 1 CH2; R = H, 1-3C alkylcarbonyl or 1-4C alkyl; A = 1-6C alkylene; Z = inorganic or organic acid anion.

公开(公告)号：PL320413A1

公开(公告)日：1997-12-08

申请号：PL32041397

申请日：1997-06-06

Applicant: HOECHST AG

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

IPC: C07D473/04 ,  A61K31/505 ,  A61K31/52 ,  A61K31/522 ,  A61P7/08 ,  A61P9/00 ,  A61P9/10 ,  A61P31/04 ,  A61P31/12 ,  A61P43/00 ,  C07D473/06 ,  C07D473/28

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：HU9602712D0

公开(公告)日：1996-11-28

申请号：HU9602712

申请日：1995-03-21

Applicant: HOECHST AG

Inventor： ANAGNOSTOPULOS HIRISTO ,  GEBERT ULRICH ,  KAPP ALEXANDER ,  KROEGEL CLAUS

IPC: C07D473/06 ,  A61K31/52 ,  A61K31/522 ,  A61P11/06 ,  A61P17/00 ,  A61P37/08 ,  C07D473/04

Abstract: Tertiary 1-(hydroxy alkyl)-4-alkyl xanthines are suitable for the preparation of medicaments for the treatment of diseases connected with a pathologically raised reactivity of eosinophilic granulocytes. The description relates to novel xanthine derivatives and to a process for producing them.