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1. 发明授权

US07846928B2 Substituted pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same 有权
标题翻译：取代的吡唑并吡啶及其盐，包含其的药物组合物，其制备方法及其用途
公开(公告)号：US07846928B2
公开(公告)日：2010-12-07
申请号：US11761672
申请日：2007-06-12
申请人： Ingo Hartung , Stuart Ince , Georg Kettschau , Karl-Heinz Thierauch , Hans Briem , Ulf Boemer
发明人： Ingo Hartung , Stuart Ince , Georg Kettschau , Karl-Heinz Thierauch , Hans Briem , Ulf Boemer
IPC分类号： A61K31/44 , A61K31/501 , A61K31/535 , A61P43/00 , C07D401/00 , C07D413/00 , C07D471/02
CPC分类号： C07D213/85 , C07D471/04
摘要： The invention relates to substituted pyrazolopyridines according to the general formula (I): in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted pyrazolopyridine compounds, to methods of preparing said substituted pyrazolopyridines, as well as to uses thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.
摘要翻译：本发明涉及根据通式（I）的取代吡唑并吡啶：其中A，B，D，E，Ra，R1，R2，R3，R4，R5和q如权利要求中所定义，包含所述取代的吡唑并吡啶化合物的药物组合物，制备所述取代的吡唑并吡啶的方法，以及其用于制备用于治疗失调的血管生长的疾病的药物组合物或伴有血管生长失调的疾病的用途，其中所述化合物有效干扰Tie2信号。

2. 发明授权

US07795264B2 Substituted arylpyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same 有权
标题翻译：取代的芳基吡唑并吡啶及其盐，包含其的药物组合物，其制备方法及其用途
公开(公告)号：US07795264B2
公开(公告)日：2010-09-14
申请号：US11761605
申请日：2007-06-12
申请人： Ingo Hartung , Georg Mendelstr Kettschau , Karl-Heinz Thierauch , Hans Briem , Philip Lienau , Antonius Ter Laak
发明人： Ingo Hartung , Georg Mendelstr Kettschau , Karl-Heinz Thierauch , Hans Briem , Philip Lienau , Antonius Ter Laak
IPC分类号： A61K31/437 , A61K31/497 , A61P29/00 , A61P35/00 , A61P9/00 , C07D401/14 , C07D471/04
CPC分类号： C07D471/04 , C07D213/85
摘要： The invention relates to substituted arylpyrazolopyridines according to the general formula (I): in which A, B, D, E, Ra, R1, R2, R3, R4, R5 and q are as defined in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted arylpyrazolopyridines, to methods of preparing said substituted arylpyrazolopyridines as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 signalling.
摘要翻译：本发明涉及根据通式（I）的取代芳基吡唑并吡啶：其中A，B，D，E，R a，R 1，R 2，R 3，R 4，R 5和q如权利要求中所定义，包含所述取代的芳基吡唑并吡啶的药物组合物，制备所述取代的芳基吡唑并吡啶的方法及其制备用于治疗失调血管生长疾病的药物组合物或伴有血管生长异常的疾病的用途，其中所述化合物有效地干扰与Tie2信令。

3. 发明申请

US20060252782A1 Sulfoximine-macrocycle compounds and salts thereof, pharmaceutical compositions comprising said compounds, methods of preparing same and uses of same 审中-公开
标题翻译：磺酰亚胺 - 大环化合物及其盐，包含所述化合物的药物组合物，其制备方法及其用途
公开(公告)号：US20060252782A1
公开(公告)日：2006-11-09
申请号：US11399619
申请日：2006-04-07
申请人： Ulrich Luecking , Georg Kettschau , Hans Briem , Wolfgang Schwede , Martina Schaefer , Karl-Heinz Thierauch , Manfred Husemann
发明人： Ulrich Luecking , Georg Kettschau , Hans Briem , Wolfgang Schwede , Martina Schaefer , Karl-Heinz Thierauch , Manfred Husemann
IPC分类号： A61K31/519 , C07D487/14
CPC分类号： C07D209/48 , C07D239/42 , C07D513/08
摘要： The invention relates to macrocyctic sulfoximines of the general Formula I: wherein A, X, Y, R1, R2 and R3 have the meaning as given in the specification and the claims, and to salts thereof; to pharmaceutical compositions comprising the macrocyclic sulfoximines, and to a method of preparing the macrocyclic sulfoximines, as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with angiopoietin and therefore influence Tie2 signalling.
摘要翻译：本发明涉及通式I的大环氰基亚砜：其中A，X，Y，R 1，R 2和R 3具有在说明书和权利要求书中给出的含义及其盐; 涉及包含大环亚磺酰亚胺的药物组合物，以及制备大环亚砜亚胺的方法及其制备用于治疗失调血管生长疾病的药物组合物或伴有血管生长失调的疾病的用途，其中该化合物有效地干扰血管生成素，因此影响Tie2信号。

4. 发明申请

US20060074112A1 N-aryl (thio) anthranilic acid amide derivatives, their preparation and their use as VEGF receptor tyrosine kinase inhibitors 审中-公开
标题翻译： N-芳基（硫代）邻氨基苯甲酸酰胺衍生物，其制备及其作为VEGF受体酪氨酸激酶抑制剂的用途
公开(公告)号：US20060074112A1
公开(公告)日：2006-04-06
申请号：US11254897
申请日：2005-10-20
申请人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul Manley , Jeanette Wood , Stefano Ferrari , Francesco Hofmann , Jurgen Mestan , Andreas Huth , Martin Kruger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
发明人： Karl-Heinz Altmann , Guido Bold , Pascal Furet , Paul Manley , Jeanette Wood , Stefano Ferrari , Francesco Hofmann , Jurgen Mestan , Andreas Huth , Martin Kruger , Dieter Seidelmann , Andreas Menrad , Martin Haberey , Karl-Heinz Thierauch
IPC分类号： C07D213/56 , A61K31/44 , C07D233/54
CPC分类号： A61K31/415 , A61K31/44 , A61K31/47 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/89 , C07D215/12 , C07D233/54 , C07D405/12
摘要： Described are compunds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R1 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y═SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each, other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.
摘要翻译：描述的是式（I）的化合物，其中W是O或S; X是NR 8; Y是CR 9 R 10其中R 9是（CH 2）n - 和R 10彼此独立地为氢或低级烷基，n为0〜3的整数。或Y为SO 2; R 1是芳基; R 2是包含一个或多个环氮原子的单环或双环杂芳基，除了R 2不能表示2-邻苯二甲酰亚氨基，并且在Y-SO的情况下 2不能表示2,1,3-苯并噻二唑-4-基; R 3，R 4，R 5和R 6中的任何一个独立地是H或除氢以外的取代基; R 7和R 8分别独立地为H或低级烷基; 或N-氧化物或其药学上可接受的盐在制备用于治疗对VEGF受体酪氨酸激酶活性的抑制作出反应的肿瘤疾病的药物产品中的用途。式（I）化合物可用于治疗，例如，的肿瘤疾病，如肿瘤疾病，视网膜病变和年龄相关性黄斑变性。

5. 发明授权

US06818661B2 Anthranylalkyl and cycloalkyl amides and use thereof as VEGF receptor inhibitors 失效
标题翻译：蒽基烷基和环烷基酰胺及其作为VEGF受体抑制剂的用途
公开(公告)号：US06818661B2
公开(公告)日：2004-11-16
申请号：US10275585
申请日：2003-05-09
申请人： Dieter Seidelmann , Martin Krüger , Eckhard Ottow , Andreas Huth , Karl-Heinz Thierauch , Andreas Menrad , Martin Haberey
发明人： Dieter Seidelmann , Martin Krüger , Eckhard Ottow , Andreas Huth , Karl-Heinz Thierauch , Andreas Menrad , Martin Haberey
IPC分类号： C07D21300
CPC分类号： C07D213/38
摘要： The invention relates to substituted anthranylalkyl and cycloalkyl amides of general formula (I) and to their use as medicaments for treating diseases caused by persistent angiogenesis.
摘要翻译：本发明涉及通式（I）的取代的苯甲酰基烷基和环烷基酰胺，以及它们作为用于治疗由持续性血管发生引起的疾病的药物的用途。

6. 发明授权

US06344339B1 Monoclonal antibodies against the extracellular domain of human VEGF-receptor protein (KDR) 失效
标题翻译：针对人VEGF受体蛋白（KDR）细胞外结构域的单克隆抗体
公开(公告)号：US06344339B1
公开(公告)日：2002-02-05
申请号：US09254640
申请日：1999-05-19
申请人： Andreas Menrad , Karl-Heinz Thierauch , Georg Martiny-Baron , Frank Totzke
发明人： Andreas Menrad , Karl-Heinz Thierauch , Georg Martiny-Baron , Frank Totzke
IPC分类号： G01N3353
CPC分类号： C07K16/2863 , A61K38/00 , A61K51/103
摘要： Monoclonal antibodies, secreted by hybridoma cell lines, that are directed against an epitope of the extracellular domain of human VEGF-receptor KDR, methods of determining human VEGF-receptor KDR in cell lysates or tissue analysates and the use of the antibodies in analytical assays, in diagnostics and as carrier molecules for therapeutic substances, are described.
摘要翻译：通过杂交瘤细胞系分泌的针对人类VEGF-受体KDR的细胞外结构域的表位的单克隆抗体，在细胞裂解物或组织分析中测定人VEGF-受体KDR的方法以及在分析测定中使用抗体，描述了诊断和作为治疗物质的载体分子。

7. 发明授权

US06225347B1 9-halogen-(Z)-prostaglandin derivatives, process for their production and their use as pharmaceutical agents 失效
标题翻译： 9-卤素 - （Z） - 前列腺素衍生物，其制备方法及其作为药剂的用途
公开(公告)号：US06225347B1
公开(公告)日：2001-05-01
申请号：US08313667
申请日：1994-09-27
申请人： Bernd Buchmann , Werner Skuballa , Helmut Vorbrueggen , Bernd Raduechel , Olaf Loge , Walter Elger , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
发明人： Bernd Buchmann , Werner Skuballa , Helmut Vorbrueggen , Bernd Raduechel , Olaf Loge , Walter Elger , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
IPC分类号： C07C40500
CPC分类号： C07C405/0016 , C07C405/00 , C07C405/0025
摘要： The invention relates to 9-halogen-(Z) prostane derivatives of formula I in which Z represents the radicals Hal represents a chlorine or fluorine atom in the alpha or beta position, R1 represents the radical with R2 meaning a hydrogen atom, an alkyl, cycloalkyl, aryl or heterocyclic radical or R1 represents the radical with R3 meaning an acid radical or the radical R2 and A represents a —CH2—CH2—, a trans-CH═CH or —C≡C group, W represents a free or a functionally modified group, and the respective OH groups can be in the alpha or beta position, D and E together represent a direct bond or D represents a straight-chain alkylene group with 1-10 C atoms, a branched-chain alkylene group with 2-10 C atoms or an annular alkylene group with 3-10 C atoms, which optionally can be substituted by fluorine atoms, and E represents an oxygen or sulfur atom, a direct bond, a C≡C bond or a —CR6═CR7 group, and R6 and R7 are different and mean a hydrogen atom, a chlorine atom or a C1-C4 alkyl group, R4 resents a free or functionally modified hydroxy group, R5 means a hydrogen atom, an alkyl, a halogen-substituted alkyl, a cycloalkyl or an optionally substituted aryl or a heterocyclic group, and if R2 means a hydrogen atom, its salts with physiologically compatible bases or its cyclodextrin chlathrates, process for their production and their pharmaceutical use.
摘要翻译：本发明涉及式Iin的9-卤素 - （Z）前列腺衍生物，其中Z代表基团.Hal表示α或β位上的氯或氟原子，R 1表示R 2表示氢原子，烷基，环烷基，芳基或杂环基或R 1表示基团，其中R 3表示酸基或基团R 2且A表示-CH 2 -CH 2 - ，反式-CH = CH或-C = C基团，W表示游离或功能修饰基团， OH基可以是α或β位，D和E一起代表直接键或D表示具有1-10个C原子的直链亚烷基，具有2-10个C原子的支链亚烷基或环状亚烷基具有3-10个C原子的基团，其任选地可以被氟原子取代，E表示氧或硫原子，直接键合，C = C键或-CR 6 = CR 7基团，并且R 6和R 7不同，一个氢原子，一个氯原子或一个C 1 -C 4烷基，R 4是一个游离的或官能改性的羟基，R 5表示氢原子，烷基，卤素取代的烷基，环烷基或任选取代的芳基或杂环基，如果R 2表示氢原子，则其与生理上相容的碱或其环糊精的盐 chlathrates，生产过程及其药物用途。

8. 发明授权

US5891910A 9-halogen-(Z) prostaglandin derivatives, process for their production and their use as pharmaceutical agents 失效
标题翻译： 9-卤素 - （Z）前列腺素衍生物，其制备方法及其作为药剂的用途
公开(公告)号：US5891910A
公开(公告)日：1999-04-06
申请号：US467888
申请日：1995-06-06
申请人： Bernd Buchmann , Werner Skuballa , Helmut Vorbrueggen , Bernd Raduechel , Olaf Loge , Walter Elger , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
发明人： Bernd Buchmann , Werner Skuballa , Helmut Vorbrueggen , Bernd Raduechel , Olaf Loge , Walter Elger , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
IPC分类号： C07C405/00 , A61K31/557
CPC分类号： C07C405/00 , C07C405/0016 , C07C405/0025
摘要： The invention relates to 9-halogen-(Z) prostane derivatives of formula I ##STR1## in which ##STR2## Z represents the radicals Hal represents a chlorine or fluorine atom,R.sub.1 represents ##STR3## A represents a --CH.sub.2 --CH.sub.2 --, a trans--CH=CH or --C.ident.C, W represents a free or a functionally modified ##STR4## group, D and E together represent a direct bond orD represents a straight-chain alkylene group with 1-10 C atoms, a branched-chain alkylene group with 2-10 C atoms or an annular alkylene group with 3-10 C atoms, which optionally can be substituted by fluorine atoms, andE represents an oxygen or sulfur atom, a direct bond, a C.ident.C bond or a --CR.sub.6 =CR.sub.7 group, and R.sub.6 and R.sub.7 are different and mean a hydrogen atom, a chlorine atom or a C.sub.1 -C.sub.4 alkyl group,R.sub.4 represents a free or functionally modified hydroxy,R.sub.5 means a hydrogen atom, an alkyl, a halogen-substituted alkyl, a cycloalkyl or an optionally substituted aryl or a heterocyclic group.
摘要翻译：本发明涉及式I的9-卤代 - （Z）前列腺衍生物，其中，Z表示基团，Hal表示氯或氟原子，R1表示A表示 -CH 2 -CH 2 - ，反式-CH = CH或-C = C，W表示游离或官能改性的基团，D和E一起表示直接键或D表示直链亚烷基，其中1 -10个C原子，具有2-10个碳原子的支链亚烷基或具有3-10个C原子的环状亚烷基，其任选可以被氟原子取代，E表示氧或硫原子，直接键，C = C键或-CR6 = CR7基，R6和R7不同，表示氢原子，氯原子或C1-C4烷基，R4表示游离或官能改性的羟基，R5表示氢原子，烷基，卤素取代的烷基，环烷基或任选取代的芳基或杂环基。

9. 发明授权

US4886788A Cyclodextrin clathrates of carbacyclin derivatives and their use as medicinal agents 失效
标题翻译：碳环糊精衍生物的环糊精包合物及其作为药物的用途
公开(公告)号：US4886788A
公开(公告)日：1989-12-12
申请号：US23506
申请日：1987-03-09
申请人： Werner Skuballa , Helmut Vorbrueggen , Helmut Dahl , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
发明人： Werner Skuballa , Helmut Vorbrueggen , Helmut Dahl , Claus-Steffen Stuerzebecher , Karl-Heinz Thierauch
IPC分类号： C07C59/46 , A61K31/557 , A61K47/48 , A61P7/02 , A61P9/12 , A61P11/08 , A61P43/00 , C07C51/00 , C07C51/347 , C07C59/125 , C07C59/62 , C07C67/00 , C07C69/732 , C07C405/00 , C07D521/00 , C08B37/00 , C08B37/16
CPC分类号： B82Y5/00 , A61K47/48969 , C07C405/0083 , C08B37/0015
摘要： Cyclodextrin clathrates of carbacyclin analogs of general Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl or alkenyl of up to 10 carbon atoms,A is a --CH.sub.2 CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C-- group,W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR2## wherein the OH-group can be in the .alpha.- or .beta.-position,D is ##STR3## alkylene, or unsaturated alkylene each of which can optionally be substituted by fluorine atoms,m is 1, 2 or 3,E is a direct bond, a --C.tbd.C-- group, or --CR.sub.4 .dbd.CR.sub.5 -- group, wherein R.sub.4 is hydrogen or an alkyl group of 1-5 carbon atoms, and R.sub.5 is hydrogen or an alkyl group of 1-5 carbon atoms, and R.sub.5 is hydrogen, halogen, or an alkyl group of 1-5 carbon atoms,R.sub.2 is alkyl or alkenyl of up to 10 carbon atoms, cycloalkyl of 3-10 carbon atoms or an optionally substituted aryl group of 6-10 carbon atoms, or a heterocyclic group, andR.sub.3 is a free or functionally modified hydroxy group,n is 1, 2, 3, 4 or 5, andX is --CH.sub.2 -- or oxygenas valuable crystalline pharmaceuticals.
摘要翻译：通式Ⅰ的碳霉酸类似物的环糊精包合物其中R 1是氢，至多10个碳原子的烷基或链烯基，A是-CH 2 CH 2 - ，反式-CH = CH-或-C 3位C- 基团，W是游离或官能改性的羟基亚甲基基团或游离或官能改性的“IMAGE”，其中OH基团可以在α或β-位，D是亚烷基，或不饱和亚烷基，其各自可以任选被氟原子取代，m为1,2或3，E为直接键，-C 3位C基或-CR 4 = CR 5 - 基，其中R 4为氢或1-5碳烷基原子，R5为氢或1-5个碳原子的烷基，R5为氢，卤素或1-5个碳原子的烷基，R2为至多10个碳原子的烷基或烯基，环烷基为3 -10个碳原子或任选取代的6-10个碳原子的芳基或杂环基，R3是游离或官能改性的羟基，n是1,2,3,4或5，X是-CH 2 - 或氧作为有价值的结晶药物。

10. 发明申请

US20100261730A1 ALKYNYLARYL COMPOUNDS AND SALTS THEREOF, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, METHODS OF PREPARING SAME AND USES OF SAME 有权
标题翻译：烷基化合物及其盐，其包含其的药物组合物，其制备方法及其用途
公开(公告)号：US20100261730A1
公开(公告)日：2010-10-14
申请号：US12747880
申请日：2008-12-04
申请人： Ingo Hartung , Hans Briem , Georg Kettschau , Karl-Heinz Thierauch , Ulf Bömer
发明人： Ingo Hartung , Hans Briem , Georg Kettschau , Karl-Heinz Thierauch , Ulf Bömer
IPC分类号： A61K31/437 , C07D471/04 , A61K31/496
CPC分类号： C07D471/04
摘要： The invention relates to alkynylaryl compounds according to the general formula (I) in which A, B, D, E, Ra, R1, R3, R4, R5 and q are as defined in the claims, and salts, N-oxides, solvates and prodrugs thereof, to pharmaceutical compositions comprising said alkynylaryl compounds, to methods of preparing said alkynylaryl compounds, to intermediate compounds useful in said methods, to uses of said intermediate compounds in the preparation of said alkynylaryl compounds, as well as to uses of said alkynylaryl compounds for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth.
摘要翻译：本发明涉及根据通式（I）的炔基芳基化合物，其中A，B，D，E，Ra，R 1，R 3，R 4，R 5和q如权利要求中所定义，和盐，N-氧化物，包括所述炔基芳基化合物的药物组合物，制备所述炔基芳基化合物的方法，可用于所述方法的中间体化合物，所述中间体化合物在制备所述炔基芳基化合物中的用途，以及所述炔基芳基用于制备用于治疗失调的血管生长疾病或伴随血管生长失调的疾病的药物组合物的化合物。

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