公开(公告)号：JPH1067662A

公开(公告)日：1998-03-10

申请号：JP20434597

申请日：1997-07-30

Applicant: HOECHST AG

Inventor： MUELLNER STEFAN DR ,  DAX CLAUDIA DCH

IPC: C07D473/04 ,  A01N37/34 ,  A61K31/445 ,  A61K31/52 ,  A61K31/522 ,  A61K48/00 ,  A61K49/04 ,  A61P1/00 ,  A61P9/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P21/00 ,  A61P25/00 ,  A61P29/00 ,  A61P31/12 ,  A61P35/00 ,  A61P37/00 ,  A61P37/04 ,  A61P43/00 ,  B32B27/34 ,  C07C29/149 ,  F24F6/08 ,  G03G5/047

Abstract: PROBLEM TO BE SOLVED: To enable the production of a medicine for the modulation of apoptosis, capable of suppressing the dephosphorylation of a cofilin and manifesting excellent modulation effects on the apoptosis by using a specific xanthine derivative. SOLUTION: A compound represented by formula I R is a 1-4C alkyl; either one of R and R is represented by the formula (CH2 )n -R-CH3 [R is a covalent single bond and (n) is 0-7; R is a group represented by CO and (n) is 1-6; R is a group represented by the formula C(R )(OH) (R ) is H or a 1-3C alkyl) and (n) is 1-6] and the other is H, a 1-7C alkyl, a 4-8C cycloalkyl, etc.}, e.g. 1-(5-hydroxy-5-methylcyclohexyl)-3-methyl-7-propylxanthine is used. Concretely. the medicine is prepared by using, e.g. (A) the compound represented by formula I, (B) a compound (salt) represented by formula II (R is a 1-4C alkyl, etc.; R is a halogen, etc.; X is N, etc.) or formula III (R is CF3 , etc.) and (C) a pharmaceutical excipient.

公开(公告)号：JPH10231279A

公开(公告)日：1998-09-02

申请号：JP1392298

申请日：1998-01-27

Applicant: HOECHST AG

Inventor： MUELLNER STEFAN DR ,  KIRSCHBAUM BERND DR ,  SCHWAB WILFRIED DR

IPC: B01J20/281 ,  A61K31/167 ,  A61K31/275 ,  A61K31/42 ,  A61K39/385 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  A61P43/00 ,  C07C233/58 ,  C07C235/28 ,  C07C235/74 ,  C07C237/04 ,  C07C255/23 ,  C07C255/30 ,  C07D261/08 ,  C07D261/18 ,  G01N30/88 ,  G01N33/53 ,  G01N33/543 ,  G01N33/558 ,  G01N33/68 ,  G01N33/94 ,  G01N30/48

Abstract: PROBLEM TO BE SOLVED: To obtain a new isoxazole and a crotonamide derivative suitable for preventing and treating cancerous diseases, inflammations and autoimmune diseases. SOLUTION: This compound is shown by formula I [R is a group of formula II or formula III; R is O-(CH2 )n -CH=CH2 ((n) is 1-3, etc.)] or a compound of formula IV (L is O, etc.; X is a polymer, etc.) such as 2-cyano-3-hydroxybut-2- enecarboxylic acid(4-allyloxyphenyl)amide. The compound of formula I is obtained, for example, by treating isoxazole-4-carboxylic acid with thionyl chloride or phosphorus oxychloride in an aprotic solvent to convert into an acid chloride and reacting the acid chloride with an organic base such as a tertiary amine in a bipolar aprotic solvent such as a chlorinated hydrocarbon by a proper method.

公开(公告)号：JP2003176237A

公开(公告)日：2003-06-24

申请号：JP2002289401

申请日：2002-10-02

Applicant: HOECHST AG

Inventor： MUELLNER STEFAN DR ,  KOENIG WOLFGANG ,  MUELLER GUENTER DR

IPC: A61K38/00 ,  A61K38/06 ,  A61K38/08 ,  A61K38/28 ,  A61P3/08 ,  A61P3/10 ,  A61P43/00 ,  C07K1/113 ,  C07K5/08 ,  C07K5/087 ,  C07K5/10 ,  C07K7/00 ,  C07K7/06 ,  C07K14/62

Abstract: PROBLEM TO BE SOLVED: To provide a therapeutic medicine for diabetes mellitus having insulin activity. SOLUTION: This therapeutic medicine for diabetes mellitus comprises at least one kind of peptide selected from a group consisting of Leu-Glu-Asn-Tyr- Cys-Asn, acetyl-Leu-Glu-Asn-Tyr-Cys-Asn and Tyr-Gln-Leu-Glu-Asn-Tyr-Cys-Asn as an active ingredient. COPYRIGHT: (C)2003,JPO

公开(公告)号：JPH1087484A

公开(公告)日：1998-04-07

申请号：JP20434497

申请日：1997-07-30

Applicant: HOECHST AG

Inventor： MUELLNER STEFAN DR ,  DAX CLAUDIA DCH

IPC: C07D213/40 ,  A61K31/165 ,  A61K31/275 ,  A61K31/41 ,  A61K31/42 ,  A61K31/421 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/445 ,  A61K38/13 ,  A61K45/00 ,  A61K45/06 ,  A61P1/00 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P13/02 ,  A61P13/12 ,  A61P15/00 ,  A61P17/00 ,  A61P25/00 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P37/00 ,  A61P43/00 ,  C07D213/75 ,  C07D263/34 ,  C07D413/12

Abstract: PROBLEM TO BE SOLVED: To obtain a pharmaceutical agent capable of exhibiting modulation effect even on apoptosis by using a compound having an action to inhibit the dephosphorylation of cophylline as an active component. SOLUTION: This agent contains at least one kind of substance selected from a compound of the formula I and/or the formula II (R is a 1-4C alkyl, a 3-5C cycloalkyl, etc.; R is CF3 , O-CF3 , S-CF3 , OH, etc.; R is a 1-4C alkyl, a halogen or H; X is CH or N atom) and/or its optical steric isomer and/or its physiologically permissible salt. The compound of the formula I or II is e.g. N-(4-trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide. The administration rate of the compound of the formula I and/or the formula II is preferably 2-250mg, especially 10-50mg. The agent is expected to be useful for the treatment of infarction, fit, transplantation, autoimmune diseases, etc.

公开(公告)号：EP0778347A3

公开(公告)日：1998-06-03

申请号：EP96118816

申请日：1996-11-25

Applicant: HOECHST AG

Inventor： KIRSCHBAUM BERND DR ,  MUELLNER STEFAN DR ,  BARTLETT ROBERT DR

IPC: C12N15/09 ,  A61K38/00 ,  C07K14/00 ,  C07K14/47 ,  C12N5/10 ,  C12N9/90 ,  C12N15/55 ,  C12Q1/68 ,  C12N9/14 ,  C12N15/61 ,  C12P21/02 ,  C12Q1/42 ,  C12Q1/533 ,  G01N33/50

CPC classification number: C12Q1/6886 ,  A61K38/00 ,  C07K14/47 ,  C12N9/90 ,  C12Q1/68 ,  C12Q1/6823 ,  C12Q2600/156 ,  C12Q2521/301

Abstract: Die vorliegende Erfindung hat die Identifizierung und molekularbiologische und biochemische Charakterisierung eines ATP- und Nukleinsäure-bindenden Proteins mit putativen Helikase- und ATPase-Eigenschaften, sowie Verfahren zu dessen Herstellung und Anwendung in pharmakologisch relevanten Test- und Assay-Systemen zum Gegenstand.

Abstract translation: 核酸结合蛋白（I）具有解旋酶活性，其mRNA（或其翻译产物）在来氟米特（II，即4-（N-（4-三氟甲基苯基）-5-甲基 - 异恶唑）存在下强烈表达） 或具有相似活性的化合物是新的。 还有新的：（1）编码（I）的DNA（III）或其部分，以及在严格条件下与（III）杂交的序列; （2）包含（III）或（III）和（3）含有（III）或载体的宿主细胞的载体的载体。

公开(公告)号：DK0545198T3

公开(公告)日：2000-03-20

申请号：DK92119913

申请日：1992-11-23

Applicant: HOECHST AG

Inventor： MUELLNER STEFAN DR ,  FRICK WENDELIN DR ,  MUELLER GUENTER DR ,  BREIPOHL GERHARD DR

IPC: A61K38/28 ,  A61K38/00 ,  A61P3/08 ,  A61P3/10 ,  C07K5/06 ,  C07K5/065 ,  C07K5/08 ,  C07K5/087 ,  C07K5/093 ,  C07K5/097 ,  C07K7/06 ,  C07K7/08 ,  C07K9/00 ,  A61K37/02

Abstract: Peptides with insulin-like activity and the formula I where C is a hydrogen atom, amino-acid residue, substituted amino-acid residue or sugar residue, D is an amino-acid residue, phosphoamino-acid residue, sugar residue, covalent bond or hydroxyl radical, E is a hydrogen atom, hydroxyl radical, substituted sugar residues, substituted alkyldiamine or glycerol residue, R is (C1-C4)-alkyl, =O or -O-(C1-C4)-alkyl, R is a sulphur protective group, SO2, SO3, (C1-C3)-alkyl, O2 radical, O3 radical, or hydrogen atom, R or R is, independently of one another, hydrogen or methyl, and W is an integer 1 or 2, the preparation and use thereof for the treatment of diabetes mellitus or non-insulin-dependent diabetes are described.

公开(公告)号：DK0580078T3

公开(公告)日：1998-05-25

申请号：DK93111375

申请日：1993-07-15

Applicant: HOECHST AG

Inventor： AHLERS MICHAEL DR ,  GLOMBIK HEINER DR ,  GRABLEY SUSANNE DR ,  GRANZER ERNOLD DR DR ,  MUELLNER STEFAN DR ,  WALCH AXEL DR ,  XU GUAN-YU PROF

IPC: A23L33/00 ,  A61K31/785 ,  A61K47/30 ,  A61P3/06 ,  A61P3/12 ,  C08F8/12 ,  C08F26/00 ,  C08F226/02

Abstract: The invention relates to polyvinylamine derivatives containing hydrophilic centres, of the formula I in which R , R , R , X, w, x, y and z are as defined, and to a process for their preparation, and to the use of these compounds as medicaments (drugs, pharmaceuticals), active compound (active ingredient) carriers and as foodstuff auxiliaries. The preparation starts, in particular, from highly pure polyvinylamines containing the recurring unit of the formula Ia whose preparation is likewise described.a

公开(公告)号：AT159262T

公开(公告)日：1997-11-15

申请号：AT93111375

申请日：1993-07-15

Applicant: HOECHST AG

Inventor： AHLERS MICHAEL DR ,  GLOMBIK HEINER DR ,  GRABLEY SUSANNE DR ,  GRANZER ERNOLD DR DR ,  MUELLNER STEFAN DR ,  WALCH AXEL DR ,  XU GUAN-YU PROF

IPC: A23L33/00 ,  A61K31/785 ,  A61K47/30 ,  A61P3/06 ,  A61P3/12 ,  C08F8/12 ,  C08F26/00 ,  C08F226/02

Abstract: The invention relates to polyvinylamine derivatives containing hydrophilic centres, of the formula I in which R , R , R , X, w, x, y and z are as defined, and to a process for their preparation, and to the use of these compounds as medicaments (drugs, pharmaceuticals), active compound (active ingredient) carriers and as foodstuff auxiliaries. The preparation starts, in particular, from highly pure polyvinylamines containing the recurring unit of the formula Ia whose preparation is likewise described.a

公开(公告)号：DE19608592A1

公开(公告)日：1997-09-11

申请号：DE19608592

申请日：1996-03-06

Applicant: HOECHST AG

Inventor： MUELLNER STEFAN DR ,  HOFFMANN AXEL DR

IPC: C07K16/00 ,  C07K16/18 ,  G01N33/92 ,  G01N33/53

公开(公告)号：DE19545126A1

公开(公告)日：1997-06-05

申请号：DE19545126

申请日：1995-12-04

Applicant: HOECHST AG

Inventor： KIRSCHBAUM BERND DR ,  MUELLNER STEFAN DR ,  BARTLETT ROBERT DR

IPC: A61K38/00 ,  C07K14/00 ,  C07K14/47 ,  C12N5/10 ,  C12N9/90 ,  C12N15/55 ,  C12Q1/68 ,  C12Q1/6823 ,  C12N15/09 ,  C12Q1/6886 ,  C12N15/63 ,  C12N15/79 ,  C12N9/14 ,  C12Q1/34 ,  C12P19/34

Abstract: Nucleic acid binding protein (I) with helicase activity, the mRNA of which (or its translation products) are strongly expressed in presence of leflunomide (II, i.e. 4-(N-(4-trifluoromethylphenyl)-5-methyl-isoxazole)) or compounds with similar activity is new. Also new are: (1) DNA (III) encoding (I), or parts of it, and sequences that hybridise under stringent conditions with (III); (2) vectors containing (III) or sequences antisense to (III) and (3) host cells containing (III) or the vectors.