专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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。

3. 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.

4. 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。

5. 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。

6. 发明授权

US5455241A 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：US5455241A
公开(公告)日：1995-10-03
申请号：US309384
申请日：1994-09-20
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 , C07D273/00
CPC分类号： C07D498/22
摘要： N-(tetrahydropyran-4-yloxy-alkanoyl)-staurosporin derivatives of formula I ##STR1## wherein R.sub.1 is hydrogen, hydroxy, lower alkoxy or oxo,R.sub.2 is hydrogen or C.sub.1-4 alkyl andR.sub.3 is hydrogen or C.sub.1-4 alkyl,processes and novel intermediates for the preparation thereof and processes for the preparation of the intermediates are described. The compounds of formula I inhibit the enzyme protein kinase C with a high degree of selectivity and can be used especially as tumour-inhibiting active ingredients.
摘要翻译：式（I）的N-（四氢吡喃-4-基氧基 - 烷酰基） - 星孢菌素衍生物其中R 1是氢，羟基，低级烷氧基或氧代，R 2是氢或C 1-4烷基，R 3是氢或C 1-4烷基，其制备方法和新型中间体以及制备中间体的方法。式I的化合物以高选择性抑制酶蛋白激酶C，可以特别用作抑制肿瘤的活性成分。

7. 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。

8. 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。

9. 发明授权

US5264431A Polycyclic conjugates 失效
标题翻译：多环共轭物
公开(公告)号：US5264431A
公开(公告)日：1993-11-23
申请号：US973133
申请日：1992-11-06
申请人： Oskar Wacker , Peter Traxler
发明人： Oskar Wacker , Peter Traxler
IPC分类号： A61K31/70 , A61P35/00 , A61P43/00 , C07H9/06 , C07H15/26 , C07H19/02 , C12N9/99 , C07D498/22 , A61K31/55
CPC分类号： C07H19/02 , C07H15/26
摘要： Staurosporin derivatives of the formula I are described, ##STR1## in which R.sub.1 is hydrogen, hydroxyl, lower alkoxy or oxo and R.sub.2 is a radical of the formula II ##STR2## in which the configuration of the sugar moiety is derived from D-glucose, D-galactose or D-mannose, and R.sub.3 -R.sub.7 are as defined below.These compounds have a pronounced and selective inhibitory action on the enzyme proteinkinase C and have, inter alia, an antitumor action.
摘要翻译：描述了式I的星孢菌素衍生物，其中R1是氢，羟基，低级烷氧基或氧代，R2是式II的基团，其中糖部分的构型衍生自D-葡萄糖，D-半乳糖或D-甘露糖，R3-R7如下所定义。这些化合物对酶蛋白酶C具有显着和选择性的抑制作用，并且尤其具有抗肿瘤作用。

10. 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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式