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1. 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。

2. 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。

3. 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。

4. 发明授权

US4711879A 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：US4711879A
公开(公告)日：1987-12-08
申请号：US928493
申请日：1986-11-07
申请人： Gerhard Baschang , Albert Hartmann , Oskar Wacker
发明人： Gerhard Baschang , Albert Hartmann , Oskar Wacker
IPC分类号： A61K38/00 , A61K39/39 , A61P37/04 , C07K1/113 , 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。

5. 发明授权

US4788182A Phosphatidyl compounds, processes for their manufacture, and their use 失效
标题翻译：磷脂酰基化合物，其制备方法及其用途
公开(公告)号：US4788182A
公开(公告)日：1988-11-29
申请号：US113359
申请日：1987-10-23
申请人： Gerhard Baschang , Bruno Fechtig , Albert Hartmann , Bohumir Lukas , Oskar Wacker
发明人： Gerhard Baschang , Bruno Fechtig , Albert Hartmann , Bohumir Lukas , Oskar Wacker
IPC分类号： A61K31/66 , A61P31/12 , C07F9/09 , C07F9/10
CPC分类号： C07F9/10 , C07F9/091
摘要： Described are phosphatidyl compounds of the formula I ##STR1## in which R.sup.1 represents C.sub.3-14 -alkanoyl, benzoyl, the acyl radical of an .alpha.-aminocarboxylic acid that is other than glycine, L-alanine and derivatives thereof having a substituted amino group, and of which the .alpha.-amino group may be substituted by lower alkanoyl, lower alkoxycarbonyl or by benzyloxycarbonyl, or the acyl radical of a .beta.-aminocarboxylic acid or an .alpha.- or .beta.-hydroxycarboxylic acid,T represents a group NH that is unsubstituted or is substituted by lower alkyl, or oxygen,Y represents dimethylene that is unsubstituted or is substituted by free, etherified or amidated carboxy,W represents hydrogen, andZ represents a 1,2-dihydroxyethyl, 2-hydroxyethyl or hydroxymethyl group, in which at least one of the hydroxy groups is esterified by an aliphatic C.sub.8-30 -carboxylic acid or is etherified by an aliphaticC.sub.8-30 -alcohol, oreach of W and Z represents a hydroxymethyl group that is esterified by an aliphatic C.sub.8-30 -carboxylic acid or is etherified by an aliphatic C.sub.8-30 -alcohol,and their salts, and processes for their manufacture.The mentioned novel compounds, and structurally related compounds that are likewise described and that belong to the state of the art, are used for the propylaxis and treatment of viral infections.
摘要翻译：描述了式I（I）的磷脂酰基化合物，其中R 1表示C 3-14 - 烷酰基，苯甲酰基，除了甘氨酸以外的α-氨基羧酸的酰基，L-丙氨酸及其衍生物具有取代基氨基，其中α-氨基可被低级烷酰基，低级烷氧基羰基或苄氧基羰基取代，或β-氨基羧酸或α-或β-羟基羧酸的酰基，T代表NH基团未取代或被低级烷基或氧取代，Y代表未取代的或被游离的醚化或酰胺化羧基取代的二亚甲基，W代表氢，Z代表1,2-二羟乙基，2-羟乙基或羟甲基，其中至少一个羟基被脂族C8-30-羧酸酯化，或被脂肪族C 8-30醇醚化，或者W和Z各自表示羟基甲基，其被一个脂肪族C8-30-羧酸或其脂肪族C 8-30醇醚化，及其盐及其制备方法。所提及的新颖化合物和同样描述并属于现有技术的结构相关化合物用于丙烯酸和治疗病毒感染。

6. 发明授权

US4666886A Novel peptide derivatives 失效
标题翻译：新型肽衍生物
公开(公告)号：US4666886A
公开(公告)日：1987-05-19
申请号：US756146
申请日：1985-07-17
申请人： Gerhard Baschang , Albert Hartmann , Oskar Wacker
发明人： Gerhard Baschang , Albert Hartmann , Oskar Wacker
IPC分类号： A61K38/00 , A61P31/04 , A61P31/12 , A61P37/04 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/08 , C07K5/083 , C07K5/10 , C07K5/103 , C07K7/02 , C07K7/06 , C07K9/00 , A61K37/02
CPC分类号： C07K7/06 , C07K5/0606 , C07K5/081 , C07K5/1013 , C07K9/005 , A61K38/00
摘要： The invention relates to lipopeptides of the formula I, ##STR1## in which each of R.sub.a.sup.1 and R.sub.b.sup.1, independently of the other, represents an aliphatic or cycloaliphatic-aliphatic hydrocarbon radical having from 7 to 21 carbon atoms that is optionally substituted by oxygen functions, orone of the radicals R.sub.a.sup.1 --CO-- and R.sub.b.sup.1 --CO-- represents hydrogen and the other of the radicals R.sub.a.sup.1 --CO-- and R.sub.b.sup.1 --CO-- represents an acyl radical, wherein R.sub.a.sup.1 and R.sub.b.sup.1 have the meanings given above,R.sup.2 represents an aliphatic or cycloaliphatic-aliphatic hydrocarbon radical having from 1 to 21 carbon atoms that is optionally substituted by oxygen functions,n=0 or 1,As.degree. represents a radical of the formula --O--Kw--CO-- or --NH--Kw--CO-- wherein Kw represents an aliphatic hydrocarbon radical having a maximum of 12 carbon atoms,As.sup.1 represents a D- or L-.alpha.-amino acid,each of Z.sup.1 and Z.sup.2, independently of the other, represents hydroxy or the N-terminal radical of a D- or L-.alpha.-aminocarboxylic acid, of an amino-lower alkanesulphonic acid or of a peptide having a maximum of 6 amino acids from the group consisting of D- or L-.alpha.-aminocarboxylic acids and amino-lower alkanesulphonic acids, andZ.sup.3 represents hydrogen or --CO--Z.sup.4 wherein Z.sup.4 represents hydroxy or the N-terminal radical of a D- or L-.alpha.-amino acid, of an amino-lower alkanesulphonic acid or of a peptide having a maximum of 6 amino acids from the group consisting of D- or L-.alpha.-aminocarboxylic acids and amino-lower alkanesulphonic acids,and the amides and esters of such compounds that contain carboxy groups.The novel lipopeptides have an immunity-stimulating action.
摘要翻译：本发明涉及式I的脂肽，其中R 1和R 2各自独立地表示脂族基团，其中R 1，R 2，R 3，或具有7至21个碳原子的脂环族脂族烃基，其任选被氧官能团取代，或者一个基团Ra1-CO-和Rb1-CO-代表氢，另一个基团Ra1-CO-和Rb1- CO-表示酰基，其中Ra1和Rb1具有上面给出的含义，R2表示任选被氧官能团取代的具有1至21个碳原子的脂族或脂环族脂族烃基，n = 0或1，As 表示式-O-Kw-CO-或-NH-Kw-CO-的基团，其中Kw表示具有最多12个碳原子的脂族烃基，As 1表示D-或L-α-氨基酸，各自的Z1和Z2独立地代表D-或L-α-氨基卡波姆的羟基或N-末端基团氨基 - 低级烷基磺酸或具有最多6个氨基酸的肽的D-木糖酸，由D-或L-α-氨基羧酸和氨基 - 低级链烷磺酸组成，并且Z 3表示氢或-CO- Z4其中Z4表示羟基或D-或L-α-氨基酸的N-末端基团，氨基 - 低级链烷磺酸或具有来自D-或L的最多6个氨基酸的肽 - α-氨基羧酸和氨基 - 低级烷基磺酸，以及含有羧基的这类化合物的酰胺和酯。新型脂肽具有免疫刺激作用。

7. 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。

8. 发明授权

US5827846A Carbazole derivatives as agents against multi-drug resistance 失效
标题翻译：咔唑衍生物作为抗多药耐药的药物
公开(公告)号：US5827846A
公开(公告)日：1998-10-27
申请号：US750155
申请日：1996-11-27
申请人： Urs Regenass , Giorgio Caravatti , Oskar Wacker
发明人： Urs Regenass , Giorgio Caravatti , Oskar Wacker
IPC分类号： A61K31/55 , A61P35/00 , C07D498/22 , C07H9/06 , C07H19/044
CPC分类号： C07D498/22 , C07H19/044 , C07H9/06
摘要： The utility of known and novel staurosporin derivatives of formula I ##STR1## wherein R.sub.1 is formyl, an aliphatic hydrocarbon radical having up to 29 carbon atoms that is unsubstituted or substituted by aryl, or is an aryl radical, R.sub.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, benzoyl, lower alkanoyl or .alpha.-aminoacyl having a free or protected amino group, and R.sub.3 is hydrogen, hydroxy, lower alkoxy or oxo, or wherein R.sub.1 is methoxycarbonylmethyl, R.sub.2 is benzoyl, and R.sub.3 is hydrogen, for avoiding or removing multi-drug resistance to anti-tumour agents, such as vinblastine or adriamycin, is described.
摘要翻译： PCT No.PCT / EP95 / 01909 Sec。 371日期：1996年11月27日 102（e）日期1996年11月27日PCT提交1995年5月19日PCT公布。公开号WO95 / 32974 日期1995年12月7日公知的已知和新型星形孢菌素衍生物（Ⅰ）其中R1是甲酰基，具有至多29个碳原子的脂族烃基，未被取代或被芳基取代，或是芳基 R2为氢，C1-C5烷基，苯甲酰基，低级烷酰基或具有游离或保护氨基的α-氨基酰基，R3为氢，羟基，低级烷氧基或氧代，或其中R1为甲氧基羰基甲基，R2为苯甲酰基，R3为描述了用于避免或去除对抗肿瘤剂如长春花碱或阿霉素的多种药物抗性的氢。

9. 发明授权

US5382675A Polycyclic compounds and processes for the preparation thereof 失效
标题翻译：多环化合物及其制备方法
公开(公告)号：US5382675A
公开(公告)日：1995-01-17
申请号：US234763
申请日：1994-04-28
申请人： Oskar Wacker
发明人： Oskar Wacker
IPC分类号： A61K31/40 , A61K31/55 , A61P9/10 , A61P17/00 , A61P35/00 , A61P43/00 , C07D207/04 , C07D273/06 , C07D309/12 , C07D311/22 , C07D498/22
CPC分类号： C07D498/22
摘要： A tetrahydropyran-4-yloxy-alkanoic acid of formula III ##STR1## wherein R.sub.2 is hydrogen or C.sub.1-4 alkyl and R.sub.3 is hydrogen or C.sub.1-4 alkyl.
摘要翻译：式III的四氢吡喃-4-基氧基 - 链烷酸其中R 2是氢或C 1-4烷基，R 3是氢或C 1-4烷基。

10. 发明授权

US4145344A Bicyclomycin derivatives 失效
标题翻译： BICYCLOMYCIN衍生物
公开(公告)号：US4145344A
公开(公告)日：1979-03-20
申请号：US817314
申请日：1977-07-20
申请人： Beat Muller , Wilhelm Kump , Oskar Wacker
发明人： Beat Muller , Wilhelm Kump , Oskar Wacker
IPC分类号： C07D498/08 , A61K31/495 , A61P31/04 , C07H9/06
CPC分类号： C07H9/06 , Y02P20/55
摘要： Bicyclomycin derivatives (i.e. compounds with the skeleton of the 5-methylene-2-oxa-7,9-diazabicyclo�4,2,2!decane) of the formula ##STR1## wherein R.sup.a to R.sub.d represent hydrogen atoms or hydroxyl protective groups, X represents a free or functionally modified carboxyl group, a substituted or unsubstituted hydrocarbon radical or a halogen atom, and n is 0 or 1, possess valuable antibiotic properties which are of importance in particular for combating infections caused by Enterobacteriaceae and Proteus species.

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