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1. 发明申请

WO9604266A3 INDOL, INDAZOL, PYRIDOPYRROL AND PYRIDOPYRAZOL DERIVATIVES WITH ANTI-ASTHMATIC, ANTI-ALLERGIC, ANTI-INFLAMMATORY AND IMMUNOMODULATING EFFECTS 审中-公开
标题翻译： INDOL，INDAZOL，吡咯并吡咯和吡哆醛衍生物具有抗哮喘，抗过敏，抗炎和免疫调节作用
公开(公告)号：WO9604266A3
公开(公告)日：1996-05-17
申请号：PCT/EP9502867
申请日：1995-07-20
申请人： ASTA MEDICA AG , LEBAUT GUILLAUME , FOUCHARD FABIENNE , KUTSCHER BERNHARD , EMIG PETER , FLEISCHHAUER ILONA , SCHMIDT JUERGEN , SZELENYI STEFAN
发明人： LEBAUT GUILLAUME , FOUCHARD FABIENNE , KUTSCHER BERNHARD , EMIG PETER , FLEISCHHAUER ILONA , SCHMIDT JUERGEN , SZELENYI STEFAN
IPC分类号： C07D231/56 , A61K31/415 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/475 , A61K31/495 , A61K31/505 , A61K31/55 , A61P11/00 , A61P29/00 , A61P37/04 , A61P37/08 , A61P43/00 , C07D209/18 , C07D209/22 , C07D401/12 , C07D401/14 , C07D403/12 , C07D471/04 , C07D401/02 , A61K31/40 , A61K31/405 , A61K31/47 , C07D209/20 , C07D401/56 , C07D471/14
CPC分类号： C07D403/12 , C07D401/12 , C07D471/04
摘要： N-benzylindol and benzopyrazol derivatives having the general formula (1) have anti-asthmatic, anti-allergic, anti-inflammatory and immunomodulating effects and are suitable for preparing medicaments.

2. 发明申请

WO0122954A3 INDOLYL-3-GLYOXYLIC ACID DERIVATIVES SERVING AS ANTITUMOR AGENTS 审中-公开
标题翻译：吲哚-3-GLYOXYLSÄUREDERIVATE抗肿瘤剂
公开(公告)号：WO0122954A3
公开(公告)日：2002-03-28
申请号：PCT/EP0009390
申请日：2000-09-26
申请人： BAXTER HEALTHCARE SA , NICKEL BERND , KLENNER THOMAS , BACHER GERALD , BECKERS THOMAS , EMIG PETER , ENGEL JUERGEN , BRUYNEEL ERIK , KAMP GUENTER , PETERS KIRSTEN
发明人： NICKEL BERND , KLENNER THOMAS , BACHER GERALD , BECKERS THOMAS , EMIG PETER , ENGEL JUERGEN , BRUYNEEL ERIK , KAMP GUENTER , PETERS KIRSTEN
IPC分类号： C07D401/12 , A61K31/404 , A61K31/4439 , A61P35/00 , A61P9/00 , A61P35/02 , A61P35/04
CPC分类号： A61K31/404
摘要： The invention relates to the use of N-substituted indol-3- glyoxylamides of general formula (I) for treating tumors, in particular, in cases of drug resistance and metastatic carcinoma, and as angiogenesis inhibitors having distinctly fewer side effects, in particular, distinctly lower neurotoxicity. The invention also relates to medicaments containing the inventive compounds.
摘要翻译：本发明涉及使用N-取代的吲哚-3- gloxylamiden用于特别是在耐药性和转移性癌肿瘤治疗的通式（1），并作为血管生成抑制剂，具有显着较低的副作用特别是显着降低的神经毒性，以及药物组合物含有它们。

3. 发明专利

CA2326833C INDOLYL-3-GLYOXYLIC ACID DERIVATIVES WITH ANTITUMORAL ACTIVITY 未知
公开(公告)号：CA2326833C
公开(公告)日：2009-06-23
申请号：CA2326833
申请日：1999-03-22
申请人： ASTA MEDICA AG
发明人： REICHERT DIETMAR , EMIG PETER , SCHMIDT JURGEN , GUNTHER ECKHARD , NICKEL BERND , BRUNE KAY , SZELENYI ISTVAN
IPC分类号： A61K31/4439 , C07D401/06 , A61K31/403 , A61K31/404 , A61K31/4178 , A61K31/4427 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61P35/00 , A61P35/02 , A61P35/04 , C07D209/18 , C07D401/12 , C07D401/14
摘要： The invention relates to the use of N-substituted indol-3-glyoxyamides of general formula (1) as antitumoral agents, as well as to pharmaceutical compositions with an antitumoral activity characterised in that they contain at least one of the compounds of general formula (1), possibly in the form of their physiologically acceptable acid addition salts or N oxides. The invention also relates to antitumoral agents containing as active ingredient one or more N-substituted indol-3-glyoxyamides of general formula (1) and their physiologically acceptable acid addition salts, and as far as possible their N-oxides, as well as a pharmaceutically acceptable carrier and/or diluent or additive, in the form of tablets, dragées, capsules, solutions for infusion or ampoules, suppositories, dressings, powder preparations for inhalation, suspensions, creams and ointments.

4. 发明专利

UA70942C2 ЗАСТОСУВАННЯ N-ЗАМІЩЕНОГО ІНДОЛІЛ-3-ГЛІОКСИЛАМІДУ ЯК ПРОТИПУХЛИННОГО ЗАСОБУ, СПОСІБ ЛІКУВАННЯ ПУХЛИННИХ ЗАХВОРЮВАНЬ ТА ЛІКАРСЬКА КОМПОЗИЦІЯ ДЛЯ ЛІКУВАННЯ ПУХЛИННИХ ЗАХВОРЮВАНЬ 未知
公开(公告)号：UA70942C2
公开(公告)日：2004-11-15
申请号：UA00116192
申请日：1999-03-22
申请人： ASTA MEDICA AG
发明人： SCHMIDT JUERGEN , EMIG PETER , REICHERT DIETMAR , GUENTHER ECKHARD
IPC分类号： C07D401/06 , A61K31/403 , A61K31/404 , A61K31/4178 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61P35/00 , A61P35/02 , A61P35/04 , C07D209/18 , C07D401/12 , C07D401/14
摘要： Предметомвинаходує застосування N-заміщенихіндол-3-гліоксиламідівзагальноїформули (1) якпротипухлиннихзасобів, атакожфармацевтичнийпрепаратпротипухлинноїдії, якийвідрізняєтьсятим, щоміститьпринаймніоднузісполукзагальноїформули (1), можливотакожу форміфізіологічнo переносимихсолей, утворенихшляхомприєднаннякислот, або N-оксидів. Крімтого, винахідстосуєтьсятакожпротипухлиннихзасобів, активноюречовиноюякихє одинабокілька N-заміщенихіндол-3-гліоксиламідівзгідноз загальноюформулою (1), атакож, можливо, їхніфізіологічнопереносимi солі, утворенішляхомприєднаннякислоті, якщоможливо, N-оксидитанаповнювачіта/аборозчинникитадопоміжнікомпоненти (домішки), якізастосовуютьу фармацевтиціі яківиробляютьсяу формітаблеток, драже, капсул, розчинівдлявливань (інфузії) абоампул, супозиторіїв, пластирів, порошківдляінгаляцій, атакожсуспензій, кремівтамазей. (1)

5. 发明专利

NZ507084A Indolyl-3-glyoxylic acid derivatives with antitumoral activity 未知
公开(公告)号：NZ507084A
公开(公告)日：2003-10-31
申请号：NZ50708499
申请日：1999-03-22
申请人： ASTA MEDICA AG
发明人： SZELENYI ISTVAN , SCHMIDT JURGEN , EMIG PETER , EICHERT DIETMAR , GUNTHER ECKHARD , BRUNE KAY , NICKEL BERND
IPC分类号： C07D401/06 , A61K31/403 , A61K31/404 , A61K31/4178 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61P35/00 , A61P35/02 , A61P35/04 , C07D209/18 , C07D401/12 , C07D401/14 , A61K31/40
摘要： Use of N-substituted indole-3-glyoxylamides of formula (I) as antitumor agents and a pharmaceutical composition having antitumor action, characterized in that it contains at least one of the compounds of the general formula (I), if appropriate also in the form of the physiologically tolerable acid addition salts or N-oxides is disclosed, wherein the variables shown therein are as defined in the specification. Furthermore, antitumor agents comprising as active compound one or more N-substituted indole-3- glyoxylamides of formula (I) and, if appropriate, their physiologically tolerable acid addition salts and, if possible, N-oxides and a pharmaceutically utilizable carrier and/or diluent or auxiliary substance in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments are also disclosed.

6. 发明专利

DE10037310A1 未知
公开(公告)号：DE10037310A1
公开(公告)日：2002-02-07
申请号：DE10037310
申请日：2000-07-28
申请人： ASTA MEDICA AG
发明人： EMIG PETER , BACHER GERALD , REICHERT DIETMAR , BAASNER SILKE , AUE BEATE , NICKEL BERND , GUENTHER ECKHARD
IPC分类号： A61K31/4709 , A61P35/00 , C07D401/12 , C07D473/00 , C07D471/04 , C07D409/04 , C07D417/04 , A61K31/404
摘要： The invention relates to novel indole derivatives of general formula (I), to the production of said derivatives and to their use as medicaments, especially for treating tumours.

7. 发明专利

PL343525A1 INDOLYL-3-GLYOXYLIC ACID DERIVATIVES WITH ANTITUMORAL ACTIVITY 未知
公开(公告)号：PL343525A1
公开(公告)日：2001-08-27
申请号：PL34352599
申请日：1999-03-22
申请人： ASTA MEDICA AG
发明人： NICKEL BERND , SZELENYI ISTVAN , SCHMIDT JUERGEN , EMIG PETER , REICHERT DIETMAR , GUENTHER ECKHARD , BRUNE KAY
IPC分类号： C07D401/06 , A61K31/403 , A61K31/404 , A61K31/4178 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61P35/00 , A61P35/02 , A61P35/04 , C07D209/18 , C07D401/12 , C07D401/14 , A61K31/4045
摘要： The invention relates to the use of N-substituted indole-3-glyoxylamides of the general formula I as antitumor agents and to a pharmaceutical composition having antitumor action, characterized in that it contains at least one of the compounds of the general formula 1, if appropriate also in the form of the physiologically tolerable acid addition salts or N-oxides. Furthermore, the invention also includes antitumor agents comprising as active compound one or more N-substituted indole-3-glyoxylamides according to the general formula 1 and, if appropriate, their physiologically tolerable acid addition salts and, if possible, N-oxides and a pharmaceutically utilizable carrier and/or diluent or auxiliary substance in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments.

8. 发明专利

AU2011901A Substituted n-benzyl-indol-3-yl glyoxylic acid derivatives having an anti-tumoral effect 未知
公开(公告)号：AU2011901A
公开(公告)日：2001-07-09
申请号：AU2011901
申请日：2000-12-19
申请人： ASTA MEDICA AG
发明人： GUNTHER ECKHARD , EMIG PETER , REICHERT DIETMAR , BAUT GUILLAUME LE , NICKEL BERND , BACHER GERALD
IPC分类号： C07D209/22 , A61K9/02 , A61K9/06 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/20 , A61K9/48 , A61K31/404 , A61K31/4439 , A61P35/00 , C07D401/06 , C07D401/12
摘要： The invention relates to novel, substituted N-benzyl-indol-3-ylglyoxylic acid derivatives of the following formula and their use for the treatment of oncosesThe invention further relates to their physiologically tolerable acid addition salts and if possible their N-oxides. In addition, the invention relates to pharmaceutical preparations containing at least one of the compounds of the abovementioned formula or their salts or N-oxides with physiologically tolerable inorganic or organic acids and, if appropriate, pharmaceutically utilizable vehicles and/or diluents or excipients and also administration forms of the compounds of the abovementioned formula containing at least one of the compounds of this formula or their salts in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments

9. 发明专利

DE19962300A1 New N-benzylindolyl glyoxylic acid derivatives are useful as antitumor agents 未知
公开(公告)号：DE19962300A1
公开(公告)日：2001-06-28
申请号：DE19962300
申请日：1999-12-23
申请人： ASTA MEDICA AG
发明人： GUENTHER ECKHARD , EMIG PETER , REICHERT DIETMAR , LE BAUT GUILLAUME , NICKEL BERND , BACHER GERALD
IPC分类号： C07D209/22 , A61K9/02 , A61K9/06 , A61K9/08 , A61K9/10 , A61K9/12 , A61K9/20 , A61K9/48 , A61K31/404 , A61K31/4439 , A61P35/00 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , A61K31/40
摘要： N-benzylindol-3-yl glyoxylic acid derivatives (I) or their acid addition salts, are new. N-benzylindol-3-yl glyoxylic acid derivatives of formula (I), or their acid addition salts, are new. R = nitro or amino is optionally substituted by amino is substituted by 1 or 2 1-6C alkyl or cycloalkyl; 1-6C acyl; phenyl(1-6C)alkyl; (hetero)aroyl; 1-6C alkylsulfonyl; arylsulfonyl; Z; Boc; 9-fluorenylmethoxycarbonyl; triphenyl; 2-(4-pyridyl)ethoxycarbonyl; diphenylmethylsilyl; or it is maleimido, succinimido or phthalimido; also, when R1 = hydrogen, Me, benzyl, Z, Boc or acetyl, R may be N-linked Gly, Ala, Leu, Ile, Ser, Phe, His, Arg, Lys, Asn or Glu. In R1, substituents on alkyl are phenyl (optionally substituted by one or more halo, 1-6C alkyl, 3-7C cycloalkyl, carboxy, 1-6C alkoxycarbonyl, trifluoromethyl, hydroxy, MeO, EtO, benzyloxy) or benzyl (optionally ring substituted by one or more 1-6C alkyl, halo or trifluoromethyl); R1 = H, 1-6C alkyl (optionally substituted), benzyloxycarbonyl (Z), tert-butoxycarbonyl (Boc) or acetyl; R2 = phenyl (optionally substituted by one or more 1-6C alkyl or alkoxy, CN, halo, trifluoromethyl, hydroxy, benzyloxy, nitro, amino (optionally substituted by 1-6C alkyl or alkoxycarbonyl), carboxy or 1-6C alkoxycarbonyl; substituents for 2-pyrimidinyl are one or more Me; those for quinolinyl are one or more of 1-6C alkyl, halo, nitro, amino or 1-6C alkylamino, and ring carbons in the pyridylmethyl component of quinolyl and quinolylmethyl may be substituted by 1-6C alkyl, alkoxy or alkoxycarbonylamino, nitro or amino), pyridinyl (optionally substituted by R5 and R6, optionally as N-oxide), or (all optionally substituted) 2- or 4-pyrimidinyl, quinolinyl, 3- or 4-quinolinylmethyl, also allylaminocarbonyl-2-methylprop-1-yl, or a wide variety of other substituents, depending on nature of R1, or R1 and R2 together complete 4-R7-piperazino or homopiperazino. When R1 = H, Me, benzyl, Z, Boc or acetyl, R2 may be N-linked Gly, Ala, Leu, Ile, Ser, Phe, His, Arg, Lys, Asn or Glu, or the residue of any natural or non-natural amino acid (optionally protected), and if R2 = residue of Asp or Glu, the second, non-bound carboxy may be as free acid or 1-6C alkyl ester; R5, R6 = 1-6C alkyl or alkoxy, 3-7C cycloalkyl, nitro, amino, hydroxy, halo, trifluoromethyl, ethoxycarbonylamino or carboxy(1-4C)alkoxy; R7 = alkyl, phenyl (optionally substituted by one or more 1-6C alkyl or alkoxy, halo, nitro, amino or 1-6C alkylamino), benzhydryl or bis-p-fluorobenzhydryl; R3, R4 = H, 1-6C alkyl, alkoxy or alkanoyl, 3-7C cycloalkyl, halo, benzyloxy, nitro, amino (optionally substituted by 1 or 2 1-4C alkyl), 1-6C alkoxycarbonylamino or 1-6C alkoxycarbonylamino(1-6C) alkyl; and Z = O or S. Independent claims are also included for: (a) pharmaceutical composition comprising (I) or its salt, optionally also carriers, diluents and/or auxiliaries; and (b) galenical formulations comprising (I) or its salt as (coated) tablets, solutions for infusion, capsules, ampoules, suppositories, plasters, inhalable powders, suspensions, creams or ointments.

10. 发明专利

BR9909902A 未知
公开(公告)号：BR9909902A
公开(公告)日：2000-12-26
申请号：BR9909902
申请日：1999-03-22
申请人： ASTA MEDICA AG
发明人： NICKEL BERND , SZELENYI ISTVAN , SCHMIDT JUERGEN , EMIG PETER , REICHERT DIETMAR , GUENTHER ECKHARD , BRUNE KAY
IPC分类号： C07D401/06 , A61K31/403 , A61K31/404 , A61K31/4178 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61P35/00 , A61P35/02 , A61P35/04 , C07D209/18 , C07D401/12 , C07D401/14 , A61K31/40
摘要： The invention relates to the use of N-substituted indole-3-glyoxylamides of the general formula I as antitumor agents and to a pharmaceutical composition having antitumor action, characterized in that it contains at least one of the compounds of the general formula 1, if appropriate also in the form of the physiologically tolerable acid addition salts or N-oxides. Furthermore, the invention also includes antitumor agents comprising as active compound one or more N-substituted indole-3-glyoxylamides according to the general formula 1 and, if appropriate, their physiologically tolerable acid addition salts and, if possible, N-oxides and a pharmaceutically utilizable carrier and/or diluent or auxiliary substance in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments.

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