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1. 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。

2. 发明授权

US5702920A DNAS encoding human macrophage migration inhibition factor related peptides 失效
标题翻译： DNAS编码人巨噬细胞迁移抑制因子相关肽
公开(公告)号：US5702920A
公开(公告)日：1997-12-30
申请号：US508142
申请日：1995-07-27
申请人： Karel Gerrit Odink , Roger Clerc , Nico Cerletti , Josef Bruggen , Lajos Tarcsay , Clemens Sorg , Walter Wiesendanger
发明人： Karel Gerrit Odink , Roger Clerc , Nico Cerletti , Josef Bruggen , Lajos Tarcsay , Clemens Sorg , Walter Wiesendanger
IPC分类号： G01N33/50 , A61K38/00 , A61P29/00 , C07H21/04 , C07K1/20 , C07K1/22 , C07K14/52 , C07K14/54 , C07K14/545 , C07K16/00 , C07K16/24 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/19 , C12N15/85 , C12P21/02 , C12P21/08 , C12R1/19 , C12R1/865 , C12R1/91 , G01N33/53 , G01N33/577
CPC分类号： C07K16/24 , C07K14/52 , C12N15/85 , A61K38/00 , C12N2830/00 , C12N2830/002 , C12N2830/55 , C12N2830/702
摘要： The invention concerns polypeptides related to human macrophage migration inhibition factor, in particular the polypeptides called MRP-8 and MRP-14, processes for their preparation, mRNAs, DNAs and hybrid vectors coding for those polypeptides, hosts transformed with such a hybrid vector, monoclonal and polyclonal antibodies to those polypeptides, and diagnostic methods for inflammatory conditions and cystic fibrosis.
摘要翻译：本发明涉及与人巨噬细胞迁移抑制因子有关的多肽，特别是称为MRP-8和MRP-14的多肽，其制备方法，mRNA，DNA和编码那些多肽的杂交载体，用这种杂交载体转化的宿主，单克隆和多克隆抗体，以及炎性病症和囊性纤维化的诊断方法。

3. 发明授权

US4548923A Muramyl peptides and processes for their manufacture 失效
标题翻译：胞壁酰多肽及其制造方法
公开(公告)号：US4548923A
公开(公告)日：1985-10-22
申请号：US608911
申请日：1984-05-09
申请人： Albert Hartmann , Oskar Wacker , Gerhard Baschang , Lajos Tarcsay
发明人： Albert Hartmann , Oskar Wacker , Gerhard Baschang , Lajos Tarcsay
IPC分类号： A61K38/00 , A61K38/14 , A61K38/17 , A61P31/12 , A61P35/00 , C07K1/113 , C07K9/00 , C07K14/52 , C07K14/53 , C07K14/535 , A61K37/00 , C07D333/32
CPC分类号： C07K9/005
摘要： The compounds of the formula I ##STR1## in which each of R.sup.1, R.sup.4 and R.sup.6, independently of the others, represents hydrogen or lower alkanoyl, R.sup.2 represents C.sub.1-4 -alkyl, hydroxymethyl or phenyl, R.sup.3 represents hydrogen or methyl, R.sup.5 represents hydrogen or C.sub.1-3 -alkyl, R.sup.7 represents C.sub.1-3 -alkyl that is unsubstituted or substituted by hydroxy, mercapto or methylthio, R.sup.8 represents hydrogen or lower alkyl, X represents oxygen or the group NH, Y represents C.sub.1-4 -alkylidene, and each of R.sup.9 and R.sup.10, independently of the other, represents C.sub.11-17 -alkyl or C.sub.11-17 -alkenyl, and their salts, have an immunostimulating activeity.
摘要翻译： R 1，R 4和R 6各自独立地表示氢或低级烷酰基，R 2表示C 1-4 - 烷基，羟甲基或苯基，R 3表示氢或甲基，R 5表示氢或C 1-3 - 烷基，R 7表示未被取代或被羟基，巯基或甲硫基取代的C 3-烷基，R 8表示氢或低级烷基，X表示氧或NH基，Y表示 C 1-4 - 亚烷基，R 9和R 10各自独立地表示C 11-17 - 烷基或C 11-17-链烯基及其盐具有免疫刺激活性。

4. 发明授权

US5350687A Antibodies which bind to novel lymphokine related peptides 失效
标题翻译：结合新型淋巴因子相关肽的抗体
公开(公告)号：US5350687A
公开(公告)日：1994-09-27
申请号：US617485
申请日：1990-11-21
申请人： Karel G. Odink , Roger Clerc , Nico Cerletti , Josef Bruggen , Lajos Tarcsay , Clemens Sorg , Walter Wiesendanger
发明人： Karel G. Odink , Roger Clerc , Nico Cerletti , Josef Bruggen , Lajos Tarcsay , Clemens Sorg , Walter Wiesendanger
IPC分类号： G01N33/50 , A61K38/00 , A61P29/00 , C07H21/04 , C07K1/20 , C07K1/22 , C07K14/52 , C07K14/54 , C07K14/545 , C07K16/00 , C07K16/24 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/19 , C12N15/85 , C12P21/02 , C12P21/08 , C12R1/19 , C12R1/865 , C12R1/91 , G01N33/53 , G01N33/577 , C07K5/00 , C07K15/28 , C12N5/12
CPC分类号： C07K16/24 , C07K14/52 , C12N15/85 , A61K38/00 , C12N2830/00 , C12N2830/002 , C12N2830/55 , C12N2830/702
摘要： The invention concerns polypeptides related to human macrophage migration inhibition factor, in particular the polypeptides called MRP-8 and MRP-14, processes for their preparation, mRNAs, DNAs and hybrid vectors coding for said polypeptides, hosts transformed with such a hybrid vector, monoclonal and polyclonal antibodies to said polypeptides , and diagnostic methods for inflammatory conditions and cystic fibrosis.
摘要翻译：本发明涉及与人巨噬细胞迁移抑制因子有关的多肽，特别是称为MRP-8和MRP-14的多肽，其制备方法，mRNA，DNA和编码所述多肽的杂交载体，用这种杂交载体转化的宿主，单克隆和针对所述多肽的多克隆抗体，以及炎性病症和囊性纤维化的诊断方法。

5. 发明授权

US4971802A Liposomes of synthetic lipids 失效
标题翻译：合成脂质的脂质体
公开(公告)号：US4971802A
公开(公告)日：1990-11-20
申请号：US395286
申请日：1989-08-16
申请人： Lajos Tarcsay , Hansjorg Eibl , Peter Fankhauser , Anita Peil
发明人： Lajos Tarcsay , Hansjorg Eibl , Peter Fankhauser , Anita Peil
IPC分类号： A61K9/00 , A61K9/127 , A61K9/50 , A61K47/24 , C07F9/10
CPC分类号： A61K9/127 , Y10S436/829 , Y10S514/885 , Y10S514/974 , Y10T428/2982
摘要： The invention relates to pharmaceutical compositions containing synthetic, substantially pure phosphatidyl serine and phosphatidyl choline and a substance or a mixture of substances having biological activity. The invention also relates to mixtures comprising synthetic, substantially pure phosphatidyl serine and phosphatidyl choline, and also to processes for the manufacture of the pharmaecutical compositions, and the use thereof.
摘要翻译：本发明涉及含有合成的，基本上纯的磷脂酰丝氨酸和磷脂酰胆碱以及具有生物活性的物质或物质的混合物的药物组合物。本发明还涉及包含合成的，基本上纯的磷脂酰丝氨酸和磷脂酰胆碱的混合物，以及用于制备药物组合物的方法及其用途。

6. 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。

7. 发明授权

US4423038A Phosphoryl compounds, pharmaceutical preparations containing such compounds, and their use 失效
标题翻译：磷酰化合物，含有这些化合物的药物制剂及其用途
公开(公告)号：US4423038A
公开(公告)日：1983-12-27
申请号：US340680
申请日：1982-01-19
申请人： Gerhard Baschang , Albert Hartmann , Oskar Wacker , Lajos Tarcsay
发明人： Gerhard Baschang , Albert Hartmann , Oskar Wacker , Lajos Tarcsay
IPC分类号： A61K39/39 , A61P31/04 , A61P37/00 , C07K1/113 , C07K9/00 , C07K14/52 , C07K14/53 , C07K14/535 , A61K37/02 , C07C103/52
CPC分类号： C07K9/005
摘要： There are described hexopyranose compounds of the formula I and salts thereof having immunomodulatory action, which can be used, for example, in the form of pharmaceutical preparations, and also together with antibiotics, and processes for their manufacture. ##STR1## The variables are as described in the disclosure. The invention relates to the above-mentioned compounds as immunomodulators, especially as immunostimulants, their use as pharmacologically active substances, especially their use as immunomodulators, particularly as immunostimulants, and their use for the manufacture of pharmaceutical preparations, and to pharmaceutical preparations containing these compounds.
摘要翻译：描述了式I的六价吡喃糖化合物及其具有免疫调节作用的盐，其可以例如以药物制剂的形式使用，并且还与抗生素一起使用，以及其制备方法。（I）变量如本公开所述。本发明涉及作为免疫调节剂的上述化合物，特别是作为免疫刺激剂，其作为药理活性物质的用途，特别是其作为免疫调节剂，特别是作为免疫刺激剂的用途，以及其用于制备药物制剂的用途以及含有这些化合物的药物制剂。

8. 发明授权

US5821336A Cytokine which mediates inflammation 失效
标题翻译：介导炎症的细胞因子
公开(公告)号：US5821336A
公开(公告)日：1998-10-13
申请号：US714927
申请日：1996-09-27
申请人： Karel Gerrit Odink , Lajos Tarcsay , Josef Bruggen , Walter Wiesendanger , Nico Cerletti , Clemens Sorg , Christiane DeWolf-Peeters , Jan Delabie
发明人： Karel Gerrit Odink , Lajos Tarcsay , Josef Bruggen , Walter Wiesendanger , Nico Cerletti , Clemens Sorg , Christiane DeWolf-Peeters , Jan Delabie
IPC分类号： G01N33/53 , A61K38/00 , A61K39/395 , A61P29/00 , C07K14/435 , C07K14/52 , C07K16/00 , C07K16/24 , C07K16/30 , C07K19/00 , C12N1/21 , C12N15/19 , C12P21/00 , C12P21/02 , C12P21/08 , C12R1/19 , C12R1/91 , G01N33/577 , C12N15/63
CPC分类号： C07K14/52 , C07K16/24 , C07K16/3061 , A61K38/00
摘要： The invention concerns polypeptides with an apparent molecular weight of around 160 kD which are mediators or precursors for mediators of inflammation, derivatives thereof such as mutants and fragments, processes for their preparation, DNAs and hybrid vectors coding for the polypeptides and derivatives and host cells transformed with such hybrid vectors, polyclonal and monoclonal antibodies specific for the polypeptides or their derivatives and antibody derivatives as well as diagnostic and therapeutic methods for inflammatory conditions and Hodgkin lymphomas.
摘要翻译：本发明涉及具有大约160kD的表观分子量的多肽，其是炎症介质的介体或前体，其衍生物如突变体和片段，其制备方法，编码多肽和衍生物的DNA和杂交载体以及转化的宿主细胞使用这些杂交载体，对多肽或其衍生物和抗体衍生物具有特异性的多克隆和单克隆抗体以及炎性病症和霍奇金淋巴瘤的诊断和治疗方法。

9. 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.

10. 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.

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