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1. 发明授权

US4406889A Derivatives of aldohexoses, intermediates, processes for their manufacture, preparations containing such compounds, and their use 失效
标题翻译：己二酸衍生物，中间体，其制备方法，含有此类化合物的制剂及其用途
公开(公告)号：US4406889A
公开(公告)日：1983-09-27
申请号：US233223
申请日：1981-02-10
申请人： Albert Hartmann , Gerhard Baschang , Oskar Wacker , Jaroslav Stanek
发明人： Albert Hartmann , Gerhard Baschang , Oskar Wacker , Jaroslav Stanek
IPC分类号： C07H1/00 , A23K1/16 , A61K31/70 , A61P37/04 , C07H15/00 , C07K1/113 , C07K5/00 , C07K9/00 , C07K14/52 , C07K14/53 , C07K14/535 , A61K37/02 , A61K31/71 , C07C103/52
CPC分类号： C07K9/005 , A23K20/147 , Y02P20/55
摘要： Described are derivatives of pyranoses of the formula I, manufacturing processes and intermediates, and their use as medicaments. ##STR1## The pyranose moiety in the compounds of the formula I is derived especially from D-glucose, but alternatively from D-galactose or D-mannose.Characteristic of the compounds of the formula I is the lower alkyl or phenyl-lower alkyl radical R.sub.8, which carries an oxycarbonyl, mercaptocarbonyl or aminocarbonyl group, which is bonded to an aliphatic, cycloaliphaticaliphatic, cycloaliphatic or aromatic hydrocarbon radical R.sub.0, each of which is optionally substituted and which may be interrupted by oxycarbonyl, mercaptocarbonyl and/or iminocarbonyl and which, like the remaining radicals of the formula I, is defined in patent claim 1.
摘要翻译：描述了式I的吡喃糖衍生物，制造方法和中间体以及它们作为药物的用途。（I）式I化合物中的吡喃糖部分特别是衍生自D-葡萄糖，或者来自D-半乳糖或D-甘露糖。式I化合物的特征是低级烷基或苯基 - 低级烷基基团R8，其携带氧羰基，巯基羰基或氨基羰基，其与脂族，脂环族脂环族或芳族烃基R 0结合，任选地被取代并且可以被氧羰基，巯基羰基和/或亚氨基羰基中断，并且其与式I的剩余基团一起在专利权利要求1中定义。

2. 发明授权

US4439425A Peptide derivatives 失效
标题翻译：肽衍生物
公开(公告)号：US4439425A
公开(公告)日：1984-03-27
申请号：US385594
申请日：1982-06-07
申请人： Lajos Tarcsay , Bruno Kamber , Jaroslav Stanek , Gerhard Baschang , Albert Hartmann
发明人： Lajos Tarcsay , Bruno Kamber , Jaroslav Stanek , Gerhard Baschang , Albert Hartmann
IPC分类号： C07K1/113 , A61K38/00 , A61P37/04 , C07J41/00 , C07K5/083 , C07K5/103 , C07K7/06 , C07K14/245 , A61K37/00
CPC分类号： C07K7/06 , C07K14/245 , C07K5/081 , C07K5/1013 , A61K38/00
摘要： The present invention relates to new lipopeptides and in particular to compounds of either of the formulae ##STR1## wherein R.sub.1 and R.sub.2 each represent a saturated or unsaturated aliphatic or mixed aliphatic-cycloaliphatic hydrocarbon radical which has 11-21 C atoms and which is also optionally substituted by oxygen functions, R.sub.3 represents hydrogen or the radical R.sub.1 --CO--O--CH.sub.2 --, where R.sub.1 has the same meaning, R.sub.1 ' is a saturated or unsaturated aliphatic hydrocarbon radical of at least 9 C atoms, which is optionally substituted at one of the C atoms non adjacent to the sulfur atom by a free hydroxyl group or a hydroxyl group esterified with a monobasic carboxylic acid and which is optionally interrupted in the C atoms chain by one or more oxygen atoms, and which hydrocarbon is optionally substituted by a maximum of 2 cycloaliphatic hydrocarbon radicals having 5-8 ring C atoms, or R.sub.1 ' is the radical --CO--R.sub.1 ", wherein R.sub.1 " represents a saturated or unsaturated aliphatic or mixed aliphatic-cycloaliphatic hydrocarbon radical of 11-21 C-atoms and which is optionally interrupted in the C atoms chain by oxygen atoms, and X represents an amino acid with free esterified or amidated carboxyl group, or an amino acid sequence of 2-10 aliphatic amino acids, the terminal carboxyl group of which is free or in the ester or amide form, the amino acids being naturals ones in the case of compounds of formula (1).
摘要翻译：本发明涉及新的脂肽，特别是涉及式（I）* = R ** = R或S或R / S中的任一个的化合物（I'）n = 1,2 * = R / S或R或S，其中R 1和R 2各自表示饱和或不饱和的具有11-21个C原子的脂族或混合的脂族 - 脂环族烃基，并且也可任选被氧官能团取代，R 3表示氢或基团R 1 - CO-O-CH 2 - ，其中R 1具有相同的含义，R 1'是至少9个C原子的饱和或不饱和脂族烃基，其任选地在不与硫原子相邻的C原子之一被自由基羟基或用一元羧酸酯化的羟基，其任选地在C原子链中被一个或多个氧原子中断，并且该烃任选被具有5-8个环C原子的最多2个脂环族烃基取代，或者R1'是-CO-R1“基团，其中R1”表示是11-21个C原子的饱和或不饱和脂族或混合脂族 - 脂环族烃基，其任选在C原子链中被氧原子中断，X表示具有游离酯化或酰胺化羧基的氨基酸，或 2-10脂肪族氨基酸的氨基酸序列，其末端羧基是游离的或呈酯或酰胺形式，氨基酸在式（1）化合物的情况下是天然的。

3. 发明授权

US4446128A Antigen derivatives and processes for their preparation 失效
标题翻译：抗原衍生物及其制备方法
公开(公告)号：US4446128A
公开(公告)日：1984-05-01
申请号：US379404
申请日：1982-05-18
申请人： Gerhard Baschang , Felix M. Dietrich , Roland Gisler , Albert Hartmann , Jaroslav Stanek , Lajos Tarcsay
发明人： Gerhard Baschang , Felix M. Dietrich , Roland Gisler , Albert Hartmann , Jaroslav Stanek , Lajos Tarcsay
IPC分类号： A61K39/00 , A61K39/385 , C07H9/04 , C07H23/00 , C07K9/00 , A61K37/00 , C07C103/52 , C07G7/00
CPC分类号： C07H9/04 , A61K39/00 , A61K39/385 , C07H23/00 , C07K9/005 , A61K2039/55583 , A61K2039/6062 , Y10S530/806 , Y10S530/807
摘要： The invention relates to novel antigen derivatives comprising an antigen and at least one muramyl-peptide covalently bonded thereto, if appropriate via a spacer, to pharmaceutical preparations which contain such compounds and to their use as a vaccine.The novel antigen derivatives produce a pronounced increase in the immuno-response to the antigen, and in particular also a cell-medicated immunity under clinically acceptable conditions of administration.
摘要翻译：本发明涉及包含抗原的新型抗原衍生物和至少一种通过间隔基共价键合到其上的胞壁酰肽与含有这些化合物的药物制剂及其作为疫苗的用途。新抗原衍生物对抗原的免疫应答产生明显的增加，特别是在临床可接受的施用条件下也是细胞免疫。

4. 发明授权

US4574058A Antigen derivatives and processes for their preparation 失效
标题翻译：抗原衍生物及其制备方法
公开(公告)号：US4574058A
公开(公告)日：1986-03-04
申请号：US477281
申请日：1983-03-21
申请人： Gerhard Baschang , Felix M. Dietrich , Roland Gisler , Albert Hartmann , Jaroslav Stanek , Lajos Tarcsay
发明人： Gerhard Baschang , Felix M. Dietrich , Roland Gisler , Albert Hartmann , Jaroslav Stanek , Lajos Tarcsay
IPC分类号： A61K39/00 , A61K39/385 , C07H9/04 , C07H23/00 , C07K9/00 , A61K37/00
CPC分类号： C07H9/04 , A61K39/00 , A61K39/385 , C07H23/00 , C07K9/005 , A61K2039/55583 , A61K2039/6062 , Y10S530/807
摘要： The invention relates to novel antigen derivatives comprising an antigen and at least one muramylpeptide covalently bonded thereto, if appropriate via a spacer, to pharmaceutical preparations which contain such compounds and to their use as a vaccine.The novel antigen derivatives produce a pronounced increase in the immuno-response to the antigen, and in particular also a cell-medicated immunity under clinically acceptable conditions of administration.
摘要翻译：本发明涉及包含抗原和至少一种通过间隔基共价连接到其上的胞壁酰肽与包含这些化合物的药物制剂和它们作为疫苗的用途的新型抗原衍生物。新抗原衍生物对抗原的免疫应答产生明显的增加，特别是在临床可接受的施用条件下也是细胞免疫。

5. 发明授权

US4414204A Antibiotic preparations having increased effectiveness, processes for their manufacture and method for increasing the antibiotic action of antibiotics 失效
标题翻译：具有增加效力的抗生素制剂，其制备方法和增加抗生素抗生素作用的方法
公开(公告)号：US4414204A
公开(公告)日：1983-11-08
申请号：US226966
申请日：1981-01-21
申请人： Lajos Tarcsay , Gerhard Baschang , Albert Hartmann , Jaroslav Stanek
发明人： Lajos Tarcsay , Gerhard Baschang , Albert Hartmann , Jaroslav Stanek
IPC分类号： C07H13/00 , A61K38/00 , A61K38/14 , A61K39/39 , A61P37/04 , C07K1/06 , C07K1/113 , C07K9/00 , C07K14/52 , C07K14/53 , C07K14/535 , A61K37/02 , A61K31/71 , C07C103/52
CPC分类号： C07K9/005
摘要： The invention relates to pharmaceutical preparations that contain an antibiotic and a muramylpeptide of the formula I or a salt thereof, to processes for their manufacture and to a method for increasing the antibiotic effectiveness of antibiotics. ##STR1## In the formula I, X represents carbonyl or carbonyloxy, R.sub.1 represents optionally substituted alkyl or aryl, R.sub.2, R.sub.3, R.sub.4 and R.sub.6 represent hydrogen or lower alkyl, R.sub.5 represents hydrogen, optionally substituted lower alkyl, cycloalkyl, aryl or nitrogen-containing heterocyclyl, or R.sub.4 and R.sub.5 together represent also C.sub.3 -C.sub.4 alkylene, R.sub.7 represents hydrogen or free, esterified or amidated carboxyl, one of the radicals A.sub.1 and A.sub.2 represents a radical of the formula II and the other of the radicals A.sub.1 and A.sub.2 represents optionally substituted or functionally modified hydroxy or amino. ##STR2## In the formula II, T represents NH or O, Y represents an optionally substituted alkylene group that can also be interrupted by oxycarbonyl or iminocarbonyl, W represents hydrogen and Z represents an optionally esterified or etherified 1,2-dihydroxyethyl or 2-hydroxyethyl group, or W and Z represent an optionally esterified or etherified hydroxymethyl group.
摘要翻译：本发明涉及含有抗生素和式I的胞壁酰胺或其盐的药物制剂及其制备方法以及提高抗生素抗生素效力的方法。（I）在式I中，X表示羰基或羰氧基，R 1表示任选取代的烷基或芳基，R 2，R 3，R 4和R 6表示氢或低级烷基，R 5表示氢，任选取代的低级烷基，环烷基，芳基或含氮杂环基，或者R4和R5一起也代表C3-C4亚烷基，R7代表氢或游离的酯化或酰胺化的羧基，基团A1和A2之一代表式II的基团和基团A1中的另一个且A2表示任选取代的或官能改性的羟基或氨基。（II）在式II中，T表示NH或O，Y表示也可被氧羰基或亚氨基羰基间隔的任选取代的亚烷基，W表示氢，Z表示任选酯化或醚化的1,2-二羟乙基或2-羟乙基，或W和Z表示任选酯化或醚化的羟甲基。

6. 发明授权

US4406890A Novel lipophilic muramyl peptides and processes for their manufacture 失效
标题翻译：新型亲脂胞壁酰多肽及其制备方法
公开(公告)号：US4406890A
公开(公告)日：1983-09-27
申请号：US283759
申请日：1981-07-16
申请人： Lajos Tarcsay , Gerhard Baschang , Albert Hartmann , Jaroslav Stanek
发明人： Lajos Tarcsay , Gerhard Baschang , Albert Hartmann , Jaroslav Stanek
IPC分类号： C07H13/00 , A61K38/00 , A61K38/14 , A61K39/39 , A61P37/04 , C07K1/06 , C07K1/113 , C07K9/00 , C07K14/52 , C07K14/53 , C07K14/535 , A61K37/02 , C07C103/52 , C07G7/00
CPC分类号： C07K9/005
摘要： The invention relates to muramyl peptide compounds, especially of the formula ##STR1## in which R.sub.1 represents, for example, alkyl or phenyl,R.sub.3 represents, for example, hydrogen or methyl andR.sub.5 represents, for example, hydrogen or lower alkyl optionally substituted, for example, by hydroxy, mercapto, or methylthio,and in which one of the radicalsA.sub.1 and A.sub.2 represents a group of the formula ##STR2## in which T represents the group of the formula -NH or -O, andY represents an alkylene radical optionally interrupted by a radical of the formula -CO-O- or -CO-NH-,and in whichW represents hydrogen andZ represents a hydroxy-substituted ethyl group, wherein at least one hydroxy group is esterified by a long-chained acyl radical orW and Z represent hydroxymethyl, wherein hydroxy is esterified by a long-chained acyl radical,and the other of the radicals A.sub.1 and A.sub.2 represents optionally etherified hydroxy or optionally substituted amino.The novel compounds have immunopotentiating properties.
摘要翻译：本发明涉及胞壁酰胺肽化合物，特别是式（I）的化合物，其中R 1表示例如烷基或苯基，R 3表示例如氢或甲基，R 5表示例如氢或低级烷基任选地被羟基，巯基或甲硫基取代，其中基团A1和A2中的一个表示式为“IMAGE”的基团，其中T表示式-NH或-O的基团，Y 表示任选地被式-CO-O-或-CO-NH-的基团中断的亚烷基，其中W表示氢，Z表示羟基取代的乙基，其中至少一个羟基被长链酰基或W和Z表示羟甲基，其中羟基被长链酰基酯化，基团A1和A2中的另一个表示任选醚化的羟基或任选取代的氨基。该新化合物具有免疫增强特性。

7. 发明授权

US4409209A Novel phosphorylmuramyl peptides and processes for the manufacture thereof 失效
公开(公告)号：US4409209A
公开(公告)日：1983-10-11
申请号：US327381
申请日：1981-12-04
申请人： Gerhard Baschang , Lajos Tarcsay , Albert Hartmann , Jaroslav Stanek
发明人： Gerhard Baschang , Lajos Tarcsay , Albert Hartmann , Jaroslav Stanek
IPC分类号： C07K9/00 , A61K37/00
CPC分类号： C07K9/005
摘要： Phosphorylmuramyl peptides of the formula ##STR1## are immuno-potentiating. In the formula, R.sub.1 represents optionally substituted alkyl or aryl, R.sub.2, R.sub.4, R.sub.6 and R.sub.7 represent, for example, hydrogen, R.sub.3 represents hydrogen or lower alkyl, R.sub.5 represents, for example, hydrogen, lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl or aralkyl, or nitrogen-containing heterocyclyl or heterocyclyl-lower alkyl, and one of the radicals A.sub.1 and A.sub.2 represents a radical of the formula (II) ##STR2## In the formula (II), T represents NH or O, Y represents an optionally substituted alkylene group, which may also be interrupted by one or two oxycarbonyl and/or iminocarbonyl groups, and W represents an aliphatic radical or a cycloalkyl or cycloalkenyl radical having more than 6 carbon atoms. The other of the radicals A.sub.1 and A.sub.2 represents free or etherified hydroxy, amino, lower alkylamino or aminocarbonyl-lower alkylamino.

8. 发明授权

US4397844A Antigen derivatives and processes for their preparation 失效
公开(公告)号：US4397844A
公开(公告)日：1983-08-09
申请号：US303244
申请日：1981-09-17
申请人： Gerhard Baschang , Felix M. Dietrich , Roland Gisler , Albert Hartmann , Jaroslav Stanek , Lajos Tarcsay
发明人： Gerhard Baschang , Felix M. Dietrich , Roland Gisler , Albert Hartmann , Jaroslav Stanek , Lajos Tarcsay
IPC分类号： A61K39/00 , A61K39/385 , C07H9/04 , C07H23/00 , C07K9/00 , A61K37/00 , C07C103/52
CPC分类号： C07H9/04 , A61K39/00 , A61K39/385 , C07H23/00 , C07K9/005 , A61K2039/55583 , A61K2039/6062 , Y10S530/806 , Y10S530/807
摘要： The invention relates to novel antigen derivatives comprising an antigen and at least one muramylpeptide covalently bonded thereto, if appropriate via a spacer, to pharmaceutical preparations which contain such compounds and to their use as a vaccine.The novel antigen derivatives produce a pronounced increase in the immuno-response to the antigen, and in particular also a cell-medicated immunity under clinically acceptable conditions of administration.

9. 发明授权

US4323560A Novel phosphorylmuramyl peptides and processes for the manufacture thereof 失效
标题翻译：新型磷酰木瓜霉糖肽及其制备方法
公开(公告)号：US4323560A
公开(公告)日：1982-04-06
申请号：US194104
申请日：1980-10-06
申请人： Gerhard Baschang , Lajos Tarcsay , Albert Hartmann , Jaroslav Stanek
发明人： Gerhard Baschang , Lajos Tarcsay , Albert Hartmann , Jaroslav Stanek
IPC分类号： A61K31/70 , A61P37/04 , C07J17/00 , C07K1/113 , C07K9/00 , C07K14/52 , C07K14/53 , C07K14/535 , A61K37/00 , A61K37/02 , C07C103/52
CPC分类号： C07K9/005
摘要： Phosphorylmuramyl peptides of the formula ##STR1## are immuno-potentiating. In the formula, R.sub.1 represents optionally substituted alkyl or aryl, R.sub.2, R.sub.4, R.sub.6 and R.sub.7 represent, for example, hydrogen, R.sub.3 represents hydrogen or lower alkyl, R.sub.5 represents, for example, hydrogen, lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl or aralkyl, or nitrogen-containing heterocyclyl or heterocyclyl-lower alkyl, and one of the radicals A.sub.1 and A.sub.2 represents a radical of the formula (II) ##STR2## In the formula (II), T represents NH or O, Y represents an optionally substituted alkylene group, which may also be interrupted by one or two oxycarbonyl and/or iminocarbonyl groups, and W represents an aliphatic radical or a cycloalkyl or cycloalkenyl radical having more than 6 carbon atoms. The other of the radicals A.sub.1 and A.sub.2 represents free or etherified hydroxy, amino, lower alkylamino or aminocarbonyl-lower alkylamino.
摘要翻译：式“IMAGE”的磷酰木瓜霉素肽是免疫增强的。在该式中，R 1表示任选取代的烷基或芳基，R 2，R 4，R 6和R 7表示例如氢，R 3表示氢或低级烷基，R 5表示例如氢，低级烷基，羟基 - 低级烷基，氨基 - 低级烷基，环烷基，环烷基 - 低级烷基，芳基或芳烷基或含氮杂环基或杂环基 - 低级烷基，基团A1和A2之一表示式（II）的基团。式（II）中，T表示NH或O，Y表示任选取代的亚烷基，其也可被一个或两个氧羰基和/或亚氨基羰基间隔，W表示具有更多的脂族基团或环烷基或环烯基超过6个碳原子。基团A1和A2中的另一个表示游离的或醚化的羟基，氨基，低级烷基氨基或氨基羰基 - 低级烷基氨基。

10. 发明授权

US4640911A Acylated sugar derivatives, processes for their manufacture, and their use 失效
标题翻译：酰化糖衍生物，其制备方法及其用途
公开(公告)号：US4640911A
公开(公告)日：1987-02-03
申请号：US739269
申请日：1985-05-29
申请人： Gerhard Baschang , Albert Hartmann , Oskar Wacker
发明人： Gerhard Baschang , Albert Hartmann , Oskar Wacker
IPC分类号： C07K9/00 , A61K31/70 , C08G18/08
CPC分类号： C07K9/005
摘要： There are described sugar derivatives of the formula I ##STR1## that have immuno-stimulating action and that contain as inventive element at least one radical A.sup.1 or A.sup.2. These radicals A.sup.1 and A.sup.2, which may be constituents of the radicals R.sup.1, R.sup.2, R.sup.4, R.sup.6, R.sup.9, R.sup.10 or R.sup.12 according to formula I, are defined as follows:A.sup.1 represents lower alkanoyl that is substituted by aryl, heteroaryl or heteroarylthio and that may be additionally substituted by an ethylene radical which, with the above-mentioned aryl or heteroaryl substituent, forms a five-membered ring or represents ortho- or ortho/meta-substituted aroyl. A.sup.2 represents lower alkoxy substituted by aryl heteroaryl or heteroarylthio.Also described are processes for the manufacture of the compounds of the formula I and novel intermediates.
摘要翻译：描述具有免疫刺激作用的式I（I）的糖衍生物，并且含有至少一个基团A1或A2的本发明元素。这些基团A1和A2可以是根据式I的基团R 1，R 2，R 4，R 6，R 9，R 10或R 12的组分，其定义如下：A1代表被芳基，杂芳基或杂芳硫基取代的低级烷酰基，其可以另外被乙烯基团取代，其中上述芳基或杂芳基取代基形成五元环或代表邻位或邻位/间位取代的芳酰基。 A2代表被芳基杂芳基或杂芳硫基取代的低级烷氧基。还描述了制备式I化合物和新型中间体的方法。

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