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1. 发明申请

WO02085841A3 SUBSTITUTED CATECHOL DERIVATIVES DERIVED FROM POLYBASIC SECONDARY AMINO ACIDS, METHOD FOR PRODUCTION AND USE THEREOF 审中-公开
标题翻译：衍生自仲氨基多元，方法取代儿茶酚用于生产和及其应用
公开(公告)号：WO02085841A3
公开(公告)日：2003-03-20
申请号：PCT/EP0202071
申请日：2002-02-27
申请人： GRUENENTHAL GMBH , HEINISCH LOTHAR , WITTMANN STEFFEN , SCHERLITZ-HOFMANN INA , STOIBER THOMAS , BERG ALBRECHT , MOELLMANN UTE
发明人： HEINISCH LOTHAR , WITTMANN STEFFEN , SCHERLITZ-HOFMANN INA , STOIBER THOMAS , BERG ALBRECHT , MOELLMANN UTE
IPC分类号： C07C235/52 , C07D265/26 , A61K31/165 , A61K31/535
CPC分类号： C07D265/26 , C07C235/52
摘要： The invention relates to novel substituted catechol derivatives, derived from polybasic secondary amino acids and analogous structures of general formula (I). Said compounds are effective as siderophores in mycobacteria and gram-negative bacteria strains, in particular, pseudomonas, E.coli and Salmonella-strains. The above can be used as transport vehicles for the introduction of active agents, for example, antibiotics (in the form of siderophore-antibiotic conjugates ), in to bacterial cells and thus greatly improve or extend the antibacterial efficacy thereof over known compounds. Furthermore said compounds are suitable as potential pro-drug forms for iron-chelates for application in diseases relating to a malfunctioning iron metabolism. Formula (I) has R = H, alkyl, aryl, R and R = H or acyl, R and R = H, alkyl, aryl and R or R = H, alkyl or catecholate groups, optionally in acylated form, or together with spacer groups, X and Z = direct bonds or bonds interrupted by particular spacer groups and Y = OH (as free acids, in the form of the salts thereof or as easily cleaved esters).
摘要翻译：本发明涉及由多元仲氨基酸和通式I.本发明的化合物可有效地分枝杆菌，以及革兰氏阴性细菌菌株，特别是假单胞菌属，大肠杆菌和沙门氏菌菌株，如铁载体的类似结构衍生的新的取代的儿茶酚衍生物。可以作为运输车辆的药物走私，例如抗生素如“铁载体Antibiotikakonjugate”至在细菌细胞中服务，从而提高它们的抗菌活性，以更大的程度和延伸比以前已知的化合物。此外，所提及的化合物适合作为潜在前药形式为用于治疗基于铁代谢紊乱性疾病的铁螯合剂。式I其中R'1¿= H，烷基，芳基，R？2和R3¿H或酰基，R？4¿和R5¿= H，烷基，芳基和R6¿或 7¿= H，烷基或儿茶酚，任选= OH作为游离酸，意味着在酰化形式或间隔基团，它们的盐或它们的容易裂解的酯R是形式通过某些间隔物键和Y X和Z直接或中断一起？

2. 发明申请

WO02070016A8 CATECHOLATE BETA-LACTAM CONJUGATES, METHOD FOR PRODUCING THE SAME AND THE USE THEREOF 审中-公开
标题翻译： Cathecolateβ-内酰胺共轭物，工艺FOR THEIR及其应用
公开(公告)号：WO02070016A8
公开(公告)日：2003-02-20
申请号：PCT/EP0202070
申请日：2002-02-27
申请人： GRUENENTHAL GMBH , HEINISCH LOTHAR , WITTMANN STEFFEN , SCHERLITZ-HOFMANN INA , STOIBER THOMAS , BERG ALBRECHT , MOELLMANN UTE
发明人： HEINISCH LOTHAR , WITTMANN STEFFEN , SCHERLITZ-HOFMANN INA , STOIBER THOMAS , BERG ALBRECHT , MOELLMANN UTE
IPC分类号： A61K47/48 , A61P3/00 , A61P31/04 , A61P31/10 , C07D499/68 , C07D501/20 , C07D501/59
CPC分类号： A61K47/54

3. 发明申请

WO02070545A3 SIDEROPHORE ANALOGUES AS TETRA- OR HEXADENTATE IRON CHELATORS ON THE BASIS OF AMINO ACIDS OR PEPTIDES, METHOD FOR PRODUCING THEM AND THE USE THEREOF 审中-公开
标题翻译： SIDEROPHORANALOGA大于4或6齿状铁螯合剂基于氨基酸或肽，生产和使用方法
公开(公告)号：WO02070545A3
公开(公告)日：2003-01-03
申请号：PCT/EP0202073
申请日：2002-02-27
申请人： GRUENENTHAL GMBH , WITTMANN STEFFEN , HEINISCH LOTHAR , SCHERLITZ-HOFMANN INA , MOELLMANN UTE
发明人： WITTMANN STEFFEN , HEINISCH LOTHAR , SCHERLITZ-HOFMANN INA , MOELLMANN UTE
IPC分类号： A61K38/00 , C07C235/60 , C07K5/068 , A61K31/198 , A61K38/05
CPC分类号： C07C235/60 , A61K38/00 , C07K5/06086
摘要： The invention relates to novel siderophore analogues as tetra- or hexadentate iron chelators or the acyl derivatives thereof on the basis of amino acids or peptides of the general formula (I), wherein R = OH or a second amino acid molecule or various catechol- or hydroxamate-containing substituents as further chelate groups, R = H, acyl or CO- in combination with R , R = H or acyl, R = H, halogen or various C or O containing substituents, R = H or CO- in combination with R , and the compounds are present as free acids, in the form of their salts or as easily cleavable esters. The inventive compounds are effective siderophores in mycobacteria and in gram-negative bacteria strains, especially pseudomonades, E. coli and Salmonella strains. They can be used as transport vehicles for introducing active substances, for example antibiotics (as siderophore antibiotic conjugates ) in bacterial cells, thereby improving or enlarging their antibacterial activity and overcoming resistances. The inventive compounds are suitable for use as potential prodrug forms for iron chelators in diseases that are associated with a disturbed iron metabolism.
摘要翻译：本发明涉及新的Siderophoranaloga作为氨基酸和通式I的本发明化合物在分枝杆菌以及革兰氏阴性细菌菌株，特别是假单胞菌属，的 E.有用的肽基础上4-或6-齿状铁螯合剂或它们的酰基衍生物大肠杆菌 - 和沙门氏菌的菌株是有效的铁载体。您可以根据运输车辆走私毒品，例如，抗生素（如“铁载体Antibiotikakonjugate”）在细菌细胞中使用，从而提高它们的抗菌活性，并且扩大和克服阻力。此外，所提及的化合物适合作为潜在前药形式为用于治疗基于铁代谢紊乱性疾病的铁螯合剂。（I）其中，R <1> = OH或第二氨基酸分子或不同的含异羟肟酸 - 邻苯二酚或取代基进一步螯合基团，R <2> = H，酰基或-CO-着R连接<5>，R <3> = H，或酰基，R <4> = H，卤素或各种C-和含O的取代基，R <5> = H或-CO-着R连接<2>和该化合物作为游离酸，其盐或它们的容易裂解的酯的形式。

4. 发明申请

WO9954454A9 MUTANTS OF THE MYCOBACTERIUM SPECIES AND USE OF THE SAME FOR SCREENING FOR ANTIBIOTICS VECTORS 审中-公开
标题翻译：分枝杆菌种突变体和它们用于对抗生素向量筛选
公开(公告)号：WO9954454A9
公开(公告)日：2001-03-15
申请号：PCT/EP9902438
申请日：1999-04-10
申请人： GRUENENTHAL GMBH , SCHUMANN GIESBERT , MOELLMANN UTE , HEINEMANN IRMGARD
发明人： SCHUMANN GIESBERT , MOELLMANN UTE , HEINEMANN IRMGARD
IPC分类号： C12N1/20 , C12N1/21 , C12N15/01 , C12N15/09 , C12R1/34 , G01N33/50
CPC分类号： C12R1/34 , C12N15/01 , G01N33/50
摘要： The invention relates to novel mutants of the Mycobacterium species and to their use for screening for potential antibiotics vectors. The novel inventive mutants are characterised in that genes which code the components of the siderophor iron absorption system are deactivated. These genes are deactivated either a) by mutagenesis using chemical or physical mutagens, b) by gene replacement, i.e. exchanging the whole gene or parts of thereof for a marker gene, c) by deletion- or insertion deactivation or d) by a combination of the aforementioned methods. The resulting mutants form the basis for screening for siderophors which are transported into the mycobacteria cell independently of the exochelin/mycobactin transportation system and which therefore represent potential antibiotics vectors.
摘要翻译：本发明涉及分枝杆菌规范的新颖突变体。他们筛选潜在的抗生素载体。新颖的本发明的突变体的特征在于基因已经失活，其编码的siderophorvermittelten铁摄取系统的部件。这些基因的失活要么a）使用化学或物理诱变剂诱变，b）通过“基因替代”，即完成完整的基因或针对标记基因的基因的部件的更换，c）以通过上述方法的组合的缺失或插入或d）。如此得到的突变体是用于筛选这样的铁载体，其被独立地传送在Mykobakterienzelle的铁外螯合素/分支杆菌生长素运输系统的基础，因此代表潜在抗生素载体。

5. 发明专利

DE10111164A1 New catechol derivatives derived from amino acids have siderophore activity and are useful as growth factors in bacterial cultures and as prodrugs for iron chelators 未知
公开(公告)号：DE10111164A1
公开(公告)日：2002-09-05
申请号：DE10111164
申请日：2001-03-01
申请人： GRUENENTHAL GMBH
发明人： HEINISCH LOTHAR , WITTMANN STEFFEN , SCHERLITZ-HOFMANN INA , STOIBER THOMAS , BERG ALBRECHT , MOELLMANN UTE
IPC分类号： C07C235/52 , C07D265/26 , A61K31/535 , C12N1/20
摘要： Catechol derivatives derived from amino acids are new. Catechol derivatives are of formula (I) as free acids, salts and readily cleavable esters are new. R = H or alkyl or aryl (each optionally substituted); R and R = H, CO-alkyl or COO-alkyl; X = direct bond, (CH2)qNH or CO(CH2)qNH; q = 1-6; or R + X = (a) or (b); R = H; halo; or alkyl, aryl or alkoxy (each optionally substituted); R = H; OH; O-alkyl; O-acyl; O-aryl; or alkyl or aryl (each optionally substituted); R = (c), (d) or (e); R = H; CO-alkyl; or COO-alkyl; R and R = -CO-; o = 1-10; R and/or R = (f) or (g); p = 2-10; R = H; alkyl or aryl (each optionally substituted); or -(CH2)s-N(Ra)(Rb); s = 2-4; Ra = (g); Rb = (c); n = 0-8; m = 0-3 Y = OA; A = H; alkali metal; or optionally substituted ammonium; Z' = direct bond; -(CH2)r-; or optionally substituted arylene; and r = 0-10. Provided that: (i) compounds are excluded when R and R together are CO; (ii) R is H when Z is a direct bond; and (iii) R is group (f) when R is group (c), R is H and X and Z are direct bonds.

6. 发明专利

NO311975B1 未知
公开(公告)号：NO311975B1
公开(公告)日：2002-02-25
申请号：NO985858
申请日：1998-12-14
申请人： GRUENENTHAL GMBH STABSSTELLE P
发明人： HEINISCH LOTHAR , MOELLMANN UTE , SCHNABELRAUCH MATTHIAS , REISSBRODT ROLF
IPC分类号： A61K31/195 , A61K31/401 , A61K31/43 , A61K31/431 , A61K31/545 , A61K47/48 , A61P3/00 , A61P31/04 , C07C233/81 , C07C235/60 , C07C235/64 , C07C237/22 , C07C245/08 , C07C251/16 , C07C251/24 , C07C251/80 , C07C251/86 , C07D207/16 , C07D263/06 , C07D499/00 , C07D499/68 , C07D499/70 , C07D501/00 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/46
摘要： Catechol derivatives of general formula (I)in which R1 denotes O-acyl and R2 represents amino acid residues in the 3- and/or 4-position function as siderophores and/or as biological chelating agents for iron in gram-negative bacteria. Conjugates with antibiotics improve penetration into bacterial cells, thereby increasing antibacterial efficacy of the cells.

7. 发明专利

GR3036667T3 NEW SYNTHETIC CATECHOL DERIVATIVES, METHOD FOR PRODUCTION AND USE THEREOF 未知
公开(公告)号：GR3036667T3
公开(公告)日：2001-12-31
申请号：GR20010401527
申请日：2001-09-18
申请人： GRUENENTHAL GMBH
发明人： HEINISCH LOTHAR , MOELLMANN UTE , SCHNABELRAUCH MATTHIAS , REISSBRODT ROLF
IPC分类号： A61K31/195 , A61K31/401 , A61K31/43 , A61K31/431 , A61K31/545 , A61K47/48 , A61P3/00 , A61P31/04 , C07C233/81 , C07C235/60 , C07C235/64 , C07C237/22 , C07C245/08 , C07C251/16 , C07C251/24 , C07C251/80 , C07C251/86 , C07D207/16 , C07D263/06 , C07D499/00 , C07D499/68 , C07D499/70 , C07D501/00 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/46
摘要： Catechol derivatives of general formula (I)in which R1 denotes O-acyl and R2 represents amino acid residues in the 3- and/or 4-position function as siderophores and/or as biological chelating agents for iron in gram-negative bacteria. Conjugates with antibiotics improve penetration into bacterial cells, thereby increasing antibacterial efficacy of the cells.

8. 发明专利

NO20005129A 未知
公开(公告)号：NO20005129A
公开(公告)日：2000-12-18
申请号：NO20005129
申请日：2000-10-12
申请人： GRUENENTHAL GMBH
发明人： SCHUMANN GIESBERT , MOELLMANN UTE , HEINEMANN IRMGARD
IPC分类号： C12N1/20 , C12N1/21 , C12N15/01 , C12N15/09 , C12R1/34 , G01N33/50 , C12N
CPC分类号： C12R1/34 , C12N15/01 , G01N33/50

9. 发明专利

PL330899A1 NOVEL SYNTHETIC CATECHOL DERIVATIVES, METHOD OF OBTAINING THEM AND THEIR APPLICATION 未知
公开(公告)号：PL330899A1
公开(公告)日：1999-06-07
申请号：PL33089997
申请日：1997-05-14
申请人： GRUENENTHAL GMBH
发明人： HEINISCH LOTHAR , MOELLMANN UTE , SCHNABELRAUCH MATTHIAS , REISSBRODT ROLF
IPC分类号： A61K31/195 , A61K31/401 , A61K31/43 , A61K31/431 , A61K31/545 , A61K47/48 , A61P3/00 , A61P31/04 , C07C233/81 , C07C235/60 , C07C235/64 , C07C237/22 , C07C245/08 , C07C251/16 , C07C251/24 , C07C251/80 , C07C251/86 , C07D207/16 , C07D263/06 , C07D499/00 , C07D499/68 , C07D499/70 , C07D501/00 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/46
摘要： Catechol derivatives of general formula (I)in which R1 denotes O-acyl and R2 represents amino acid residues in the 3- and/or 4-position function as siderophores and/or as biological chelating agents for iron in gram-negative bacteria. Conjugates with antibiotics improve penetration into bacterial cells, thereby increasing antibacterial efficacy of the cells.

10. 发明专利

ZA975638B New synthetic catechol derivatives, methods of producing them and their use. 未知
公开(公告)号：ZA975638B
公开(公告)日：1998-01-23
申请号：ZA975638
申请日：1997-06-25
申请人： GRUENENTHAL GMBH
发明人： HEINISCH LOTHAR , SCHNABELRAUCH MATTHIAS , MOELLMANN UTE , REISSBRODT ROLF
IPC分类号： A61K31/195 , A61K31/401 , A61K31/43 , A61K31/431 , A61K31/545 , A61K47/48 , A61P3/00 , A61P31/04 , C07C233/81 , C07C235/60 , C07C235/64 , C07C237/22 , C07C245/08 , C07C251/16 , C07C251/24 , C07C251/80 , C07C251/86 , C07D207/16 , C07D263/06 , C07D499/00 , C07D499/68 , C07D499/70 , C07D501/00 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/46 , C07D
摘要： Catechol derivatives of general formula (I)in which R1 denotes O-acyl and R2 represents amino acid residues in the 3- and/or 4-position function as siderophores and/or as biological chelating agents for iron in gram-negative bacteria. Conjugates with antibiotics improve penetration into bacterial cells, thereby increasing antibacterial efficacy of the cells.

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