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1. 发明授权

US07087637B2 Substituted indoles which are PARP inhibitors 有权
标题翻译：取代的吲哚是PARP抑制剂
公开(公告)号：US07087637B2
公开(公告)日：2006-08-08
申请号：US10275574
申请日：2001-05-09
申请人： Roland Grandel , Wilfried Lubisch , Michael Kock , Thomas Hoger , Reinhold Muller , Sabine Schult , Uta Holzenkamp
发明人： Roland Grandel , Wilfried Lubisch , Michael Kock , Thomas Hoger , Reinhold Muller , Sabine Schult , Uta Holzenkamp
IPC分类号： A61K31/40 , C07D204/42 , C07D209/12
CPC分类号： C07D209/08
摘要： The present invention relates to novel indole derivatives, to their preparation and to their use, as inhibitors of the enzyme poly(ADP-ribose)polymerase or PARP (EC 2.4.2.30), for producing drugs.
摘要翻译：本发明涉及用于生产药物的新型吲哚衍生物，其制备及其用途，作为聚（ADP-核糖）聚合酶或PARP（EC 2.4.2.30）酶的抑制剂。

2. 发明授权

US06696437B1 Heterocyclically substituted benzimidazoles, the production and application thereof 有权
标题翻译：杂环取代的苯并咪唑，的生产和应用
公开(公告)号：US06696437B1
公开(公告)日：2004-02-24
申请号：US09959632
申请日：2002-03-25
申请人： Wilfried Lubisch , Michael Kock , Thomas Hoeger , Roland Grandel , Uta Holzenkamp , Sabine Schult , Reinhold Mueller
发明人： Wilfried Lubisch , Michael Kock , Thomas Hoeger , Roland Grandel , Uta Holzenkamp , Sabine Schult , Reinhold Mueller
IPC分类号： C07D40104
CPC分类号： C07D401/04 , C07D235/18 , C07D403/04
摘要： The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.
摘要翻译：本发明涉及新的苯并咪唑，其制备及其作为多聚（ADP-核糖）聚合酶或PARP（EC 2.4.2.30）酶抑制剂用于生产药物的用途。

3. 再颁专利

USRE39608E1 Substituted benzimidazoles and their use as PARP inhibitors 有权
标题翻译：取代的苯并咪唑及其用作PARP抑制剂
公开(公告)号：USRE39608E1
公开(公告)日：2007-05-01
申请号：US10935683
申请日：1999-11-23
申请人： Wilfried Lubisch , Michael Kock , Thomas Höger , Sabine Schult , Roland Grandel , Reinhold Müller
发明人： Wilfried Lubisch , Michael Kock , Thomas Höger , Sabine Schult , Roland Grandel , Reinhold Müller
IPC分类号： A61K31/4184 , A61K31/454 , C07D401/04 , C07D401/14 , C07D403/02
CPC分类号： C07D401/04 , C07D235/30 , C07D401/14 , C07D403/04
摘要： Compounds of the formula Ia or IB where A is a saturated or monounsaturated heterocyclic, 4 - to 8-membered ring which contains one or two nitrogen atoms, and their tautomeric forms, possible enantiomeric and diastereomeric forms, their prodrugs and possible physiologically tolerated salts are useful as inhibitors of the enzyme poly(ADP-ribose)polymerase.
摘要翻译：式Ia或IB的化合物，其中A是饱和或单不饱和的杂环，含有一个或两个氮原子的4至8元环及其互变异构形式，其可能的对映体和非对映体形式，其前药和可能的生理学耐受盐是可用作聚（ADP-核糖）聚合酶的抑制剂。

4. 发明授权

US07041675B2 Heterocyclic compounds and their use as PARP inhibitors 失效
标题翻译：杂环化合物及其作为PARP抑制剂的用途
公开(公告)号：US07041675B2
公开(公告)日：2006-05-09
申请号：US10182532
申请日：2001-01-25
申请人： Wilfried Lubisch , Michael Kock , Thomas Hoeger , Roland Grandel , Reinhold Mueller , Sabine Schult
发明人： Wilfried Lubisch , Michael Kock , Thomas Hoeger , Roland Grandel , Reinhold Mueller , Sabine Schult
IPC分类号： A61K31/437 , A61K31/4709 , A61K31/4725 , A61P9/10 , C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to compounds of the formula I and the tautomeric forms, possible enantiomeric and diasteromeric forms thereof, and prodrugs thereof, and use thereof as PARP inhibitors.
摘要翻译：本发明涉及式I化合物及互变异构形式，其可能的对映异构体和非对映体形式及其前药，及其作为PARP抑制剂的用途。

5. 发明授权

US06448271B1 Substituted benzimidazoles and their use as parp inhibitors 有权
标题翻译：取代的苯并咪唑及其作为抑制剂的用途
公开(公告)号：US06448271B1
公开(公告)日：2002-09-10
申请号：US09856686
申请日：2001-05-24
申请人： Wilfried Lubisch , Michael Kock , Thomas Höger , Sabine Schult , Roland Grandel , Reinhold Müller
发明人： Wilfried Lubisch , Michael Kock , Thomas Höger , Sabine Schult , Roland Grandel , Reinhold Müller
IPC分类号： A61K314184
CPC分类号： C07D401/04 , C07D235/30 , C07D401/14 , C07D403/04
摘要： Compounds of the formula Ia or IB where A is a saturated or monounsaturated heterocyclic, 4- to 8-membered ring which contains one or two nitrogen atoms, and their tautomeric forms, possible enantiomeric and diastereomeric forms, their prodrugs and possible physiologically tolerated salts are useful as inhibitors of the enzyme poly(ADP-ribose)polymerase.
摘要翻译：式Ia或IBaaA的化合物是饱和或单不饱和的杂环，含有一个或两个氮原子的4至8元环，其互变异构形式，可能的对映体和非对映体形式，其前药和可能的生理学耐受盐可用作聚（ADP-核糖）聚合酶的抑制剂。

6. 发明授权

US06737421B1 Cyclo-alkyl substituted benzimidazoles and their use as PARP inhibitors 有权
标题翻译：环烷基取代的苯并咪唑及其作为PARP抑制剂的用途
公开(公告)号：US06737421B1
公开(公告)日：2004-05-18
申请号：US09959161
申请日：2002-04-04
申请人： Wilfried Lubish , Michael Kock , Thomas Hoeger , Roland Grandel , Sabine Schult , Reinhold Mueller
发明人： Wilfried Lubish , Michael Kock , Thomas Hoeger , Roland Grandel , Sabine Schult , Reinhold Mueller
IPC分类号： C07D23506
CPC分类号： C07D235/14
摘要： Compounds of the formula I or II and their tautomeric forms, possible enantiomeric and diastereomeric forms, possible cistrans isomers on the rings in A and prodrugs thereof, pharmaceutical compositions containing these compounds and methods of treating neurodegenerative diseases or neuronal damage with these compounds.
摘要翻译：式I或II化合物及其互变异构形式，可能的对映异构体和非对映异构体形式，A中的环上的可能的顺式异构体及其前药，含有这些化合物的药物组合物和用这些化合物治疗神经变性疾病或神经元损伤的方法。

7. 发明授权

US07781596B1 Substituted 2-phenylbenzimidazoles, the production thereof and their use 有权
标题翻译：取代的2-苯基苯并咪唑，其制备及其用途
公开(公告)号：US07781596B1
公开(公告)日：2010-08-24
申请号：US09830992
申请日：1999-10-28
申请人： Wilfried Lubisch , Michael Kock , Thomas Höger
发明人： Wilfried Lubisch , Michael Kock , Thomas Höger
IPC分类号： A61K31/4184 , A61K31/496 , C07D235/18 , C07D403/10
CPC分类号： C07D231/12 , C07C237/30 , C07D233/56 , C07D235/18 , C07D249/08 , C07D403/10 , C12Q1/48
摘要： The invention relates to novel 2-phenylbenzimidazoles of general formula (I) or (II), wherein the radicals have the meanings cited in the description, and to their tautomeric forms, possible enantiomeric and diastereomeric forms, to their prodrugs, and to possible physiologically compatible salts. The invention also relates to the production of said compounds and to their use.
摘要翻译：本发明涉及通式（I）或（II）的新型2-苯基苯并咪唑，其中基团具有本说明书中引用的含义及其互变异构形式，其可能的对映异构体和非对映异构体形式，其前体药物以及可能的生理学相容的盐。本发明还涉及所述化合物的生产及其用途。

8. 发明授权

US07754459B1 Poly(ADP-ribose) polymerase-gene 失效
标题翻译：聚（ADP-核糖）聚合酶基因
公开(公告)号：US07754459B1
公开(公告)日：2010-07-13
申请号：US09701586
申请日：1999-06-04
申请人： Michael Kock , Thomas Höger , Burkhard Kröger , Bernd Otterbach , Wilfried Lubisch , Hans-Georg Lemaire
发明人： Michael Kock , Thomas Höger , Burkhard Kröger , Bernd Otterbach , Wilfried Lubisch , Hans-Georg Lemaire
IPC分类号： C12N9/12
CPC分类号： C12N9/1077 , A01K2217/05 , A61K38/00 , A61K49/00 , C07K16/40 , C07K2317/76 , C07K2319/00 , C12Q1/48 , C12Y204/0203 , G01N2333/91142
摘要： The invention relates to poly(ADP-ribose)polymerase (PARP) homologs which have an amino acid sequence which has a) a functional NAD+ binding domain and b) no zinc finger sequence motif of the general formula CX2CXmHX2C in which m is an integral value from 28 or 30, and the X radicals are, independently of one another, any amino acid; and the functional equivalents thereof; nucleic acids coding therefor; antibodies with specificity for the novel protein; pharmaceutical and gene therapy compositions which comprise products according to the invention; methods for the analytical determination of the proteins and nucleic acids according to the invention; methods for identifying effectors or binding partners of the proteins according to the invention; novel PARP effectors; and methods for determining the activity of such effectors.
摘要翻译：本发明涉及具有氨基酸序列的聚（ADP-核糖）聚合酶（PARP）同系物，该氨基酸序列具有a）功能性的NAD +结合域，b）没有通式CX2CXmHX2C的锌指序列基序，其中m是整数值 28或30个，X基彼此独立地为任何氨基酸; 及其功能等同物; 为此编码的核酸; 对新蛋白具有特异性的抗体; 包括根据本发明的产品的药物和基因治疗组合物; 根据本发明的用于分析测定蛋白质和核酸的方法; 用于鉴定根据本发明的蛋白质的效应物或结合配偶体的方法; 新型PARP效应器; 以及用于确定这种效应物的活性的方法。

9. 发明授权

US06509365B1 2-phenylbenzimidazoles and 2-phenylindoles, and production and use thereof 有权
标题翻译： 2-苯基苯并咪唑和2-苯基吲哚，以及其生产和使用
公开(公告)号：US06509365B1
公开(公告)日：2003-01-21
申请号：US09856036
申请日：2001-05-17
申请人： Wilfried Lubisch , Michael Kock , Thomas Höger
发明人： Wilfried Lubisch , Michael Kock , Thomas Höger
IPC分类号： C07D23504
CPC分类号： C07D209/14 , A61K31/404 , A61K31/4184 , C07D235/18
摘要： 2-Phenylbenzimidazoles and 2-phenylindoles of formula I wherein A is N or CH, R1 is hydrogen or alkyl which optionally carries an OR11 group, R11 is hydrogen or alkyl, R2 is hydrogen, chlorine, fluorine, bromine, iodine, alkyl, nitro, CF3, CN, NR21R22, NH—CO—R23, OR21, R21 and R22 are each hydrogen or alkyl, R23 is hydrogen, alkyl or phenyl, R3 is —(CH2)q—NR31R32, q is 0, 1, 2 or 3, R31 is hydrogen, alkyl, (CH2)rNR33R34, R32 is (CH2)rNR33R34, r is 2, 3, 4, 5 or 6, R33 and R34 are each hydrogen, alkyl or phenylalkyl wherein the phenyl ring is optionally substituted, or R33 and R34 and the nitrogen atom form a 3- to 8-membered ring, R4 is hydrogen, alkyl, chlorine, bromine, fluorine, nitro, cyano, NR41R42, NH—CO—R43, OR41, R41 and R42 are each hydrogen or alkyl, and R43 is alkyl or phenyl, are useful as inhibitors of poly(ADP-ribose)polymerase and for the production of drugs.
摘要翻译：式I的2-苯基苯并咪唑和2-苯基吲哚，其中A是N或CH，R 1是氢或任选地带有OR 11基团的烷基，R 11是氢或烷基，R 2是氢，氯，氟，溴，碘，烷基，硝基，CF 3 ，CN，NR21R22，NH-CO-R23，OR21，R21和R22各自为氢或烷基，R23为氢，烷基或苯基，R3为 - （CH2）q-NR31R32，q为0,1,2或3， R31是氢，烷基，（CH2）rNR33R34，R32是（CH2）rNR33R34，r是2,3,4,5或6，R33和R34各自是氢，烷基或苯基烷基，其中苯环是任选取代的，或R 33和 R34和氮原子形成3-至8-元环，R4为氢，烷基，氯，溴，氟，硝基，氰基，NR41R42，NH-CO-R43，OR41，R41和R42各自为氢或烷基，和R43是烷基或苯基，可用作聚（ADP-核糖）聚合酶的抑制剂和用于生产药物。

10. 发明授权

US09051553B2 Poly(ADP-ribose) polymerase genes 有权
标题翻译：聚（ADP-核糖）聚合酶基因
公开(公告)号：US09051553B2
公开(公告)日：2015-06-09
申请号：US12778692
申请日：2010-05-12
申请人： Michael Kock , Thomas Höger , Burkhard Kröger , Bernd Otterbach , Wilfried Lubisch , Hans-Georg Lemaire
发明人： Michael Kock , Thomas Höger , Burkhard Kröger , Bernd Otterbach , Wilfried Lubisch , Hans-Georg Lemaire
IPC分类号： C12N1/20 , C12N9/10 , A61K38/00 , A61K49/00
CPC分类号： C12N9/1077 , A01K2217/05 , A61K38/00 , A61K49/00 , C07K16/40 , C07K2317/76 , C07K2319/00 , C12Q1/48 , C12Y204/0203 , G01N2333/91142
摘要： The invention relates to poly(ADP-ribose)polymerase (PARP) homologs which have an amino acid sequence which has a) a functional NAD binding domain and b) no zinc finger sequence motif of the general formula CX2CXmHX2C in which m is an integral value from 28 or 30, and the X radicals are, independently of one another, any amino acid; and the functional equivalents thereof; nucleic acids coding therefor; antibodies with specificity for the novel protein; pharmaceutical and gene therapy compositions which comprise products according to the invention; methods for the analytical determination of the proteins and nucleic acids according to the invention; methods for identifying effectors or binding partners of the proteins according to the invention; novel PARP effectors; and methods for determining the activity of such effectors.
摘要翻译：本发明涉及具有氨基酸序列的聚（ADP-核糖）聚合酶（PARP）同系物，该氨基酸序列具有a）功能性NAD结合域，b）没有通式CX2CXmHX2C的锌指序列基序，其中m是整数值 28或30个，X基彼此独立地为任何氨基酸; 及其功能等同物; 为此编码的核酸; 对新蛋白具有特异性的抗体; 包括根据本发明的产品的药物和基因治疗组合物; 根据本发明的用于分析测定蛋白质和核酸的方法; 用于鉴定根据本发明的蛋白质的效应物或结合配偶体的方法; 新型PARP效应器; 以及用于确定这种效应物的活性的方法。

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