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1. 发明申请

US20080176892A1 Novel Azaheterocyclic Compounds as Kinase Inhibitors 有权
标题翻译：新型氮杂环化合物作为激酶抑制剂
公开(公告)号：US20080176892A1
公开(公告)日：2008-07-24
申请号：US11912462
申请日：2006-03-30
申请人： Timo Heinrich , Andree Blaukat , Wolfgang Staehle , Hartmut Greiner , Maria Kordowicz
发明人： Timo Heinrich , Andree Blaukat , Wolfgang Staehle , Hartmut Greiner , Maria Kordowicz
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to compounds of the formula (I), to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases in the development or course of which kinases are involved.
摘要翻译：本发明涉及式（I）化合物的制备和用途，其用于制备用于治疗疾病，特别是涉及激酶发展过程中的肿瘤和/或疾病的药物。

2. 发明授权

US08114882B2 (1H-indol-7-yl)-(pyrimidin-2-ylamino)methanone derivatives and related compounds as IGF-R1 inhibitors for the treatment of cancer 失效
标题翻译：（1H-吲哚-7-基） - （嘧啶-2-基氨基）甲酮衍生物和相关化合物作为治疗癌症的IGF-R1抑制剂
公开(公告)号：US08114882B2
公开(公告)日：2012-02-14
申请号：US11911268
申请日：2006-03-17
申请人： Timo Heinrich , Andree Blaukat , Maria Kordowicz
发明人： Timo Heinrich , Andree Blaukat , Maria Kordowicz
IPC分类号： C07D401/14 , C07D403/14 , A61K31/506
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14
摘要： The invention relates to compounds of the formula (I), in which Ar denotes a mono- or bicyclic aromatic homo- or heterocycle having 1 to 4 N, O and/or S atoms and 5 to 10 skeleton atoms, which may be unsubstituted or mono-, di- or trisubstituted by carbonyl oxygen, Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 and/or S(O)9A, A denotes unbranched, branched or cyclic alkyl having 1-14 C atoms, in which one or two CH2 groups may be replaced by O or S atoms and/or by —CH═CH— groups and/or in addition 1-7 H atoms may be replaced by F and/or Cl, Hal: F, Cl, Br or I, D: NH, NH2, NA2, NHA, CH2, CH3, OH, OA, O or S, E: CH2, CH, NH or N, Y: E or a saturated or unsaturated bond, X: CH2, O or NH, Q: Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 or X-M, to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumors and/or diseases in the development or course of which kinases are involved.
摘要翻译：本发明涉及式（I）化合物，其中Ar表示具有1至4个N，O和/或S原子和5至10个骨架原子的单环或双环芳族均聚或杂环，其可以是未取代的或羰基氧，Hal，A，OH，OA，NH2，NHA，NA2，NO2，CN，OCN，SCN，COOH，COOA，CONH2，CONHA，CONA2，NHCOA，NHCONH2，NHSO2A，CHO的单，二或三取代，COA，SO 2 NH 2和/或S（O）9A，A表示具有1-14个C原子的无支链，支链或环状烷基，其中一个或两个CH 2基团可被O或S原子替代和/或由-CH = CH-基和/或另外1-7个H原子可以被F和/或Cl，Hal，F，Cl，Br或I，D：NH，NH2，NA2，NHA，CH2，CH3，OH，OA ，O或S，E：CH 2，CH，NH或N，Y：E或饱和或不饱和键，X：CH 2，O或NH，Q：Hal，A，OH，OA，NH 2，NHA，，CN，OCN，SCN，COOH，COOA，CONH 2，CONHA，CONA2，NHCOA，NHCONH 2，NHSO 2 A，CHO，COA，SO 2 NH 2或XM，用于制备和用于制备治疗药物疾病，特别是涉及激酶的发展或过程中的肿瘤和/或疾病。

3. 发明申请

US20080194605A1 (1H-Ind0l-7-Yl)-(Pyrimidin-2-Ylamino)Methanone Derivatives and Related Compounds as Igf-R1 Inhibitors for the Treatment of Cancer 失效
标题翻译：（1H-吲哚-7-基） - （嘧啶-2-基氨基）甲酮衍生物和相关化合物作为Igf-R1抑制剂治疗癌症
公开(公告)号：US20080194605A1
公开(公告)日：2008-08-14
申请号：US11911268
申请日：2006-03-17
申请人： Timo Heinrich , Andree Blaukat , Maria Kordowicz
发明人： Timo Heinrich , Andree Blaukat , Maria Kordowicz
IPC分类号： A61K31/497 , C07D401/14 , A61P35/04 , C07D401/12
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14
摘要： The invention relates to compounds of the formula (I), in which Ar denotes a mono- or bicyclic aromatic homo- or heterocycle having 1 to 4 N, O and/or S atoms and 5 to 10 skeleton atoms, which may be unsubstituted or mono-, di- or trisubstituted by carbonyl oxygen, Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 and/or S(O)9A, A denotes unbranched, branched or cyclic alkyl having 1-14 C atoms, in which one or two CH2 groups may be replaced by O or S atoms and/or by —CR═CH— groups and/or in addition 1-7 H atoms may be replaced by F and/or Cl, Hal: F, Cl, Br or I, D: NH, NH2, NA2, NHA, CH2, CH3, OH, OA, O or S, E: CH2, CH, NH or N, Y: E or a saturated or unsaturated bond, X: CH2, O or NH, Q: Hal, A, OH, OA, NH2, NHA, NA2, NO2, CN, OCN, SCN, COOH, COOA, CONH2, CONHA, CONA2, NHCOA, NHCONH2, NHSO2A, CHO, COA, SO2NH2 or X-M, to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases in the development or course of which kinases are involved.
摘要翻译：本发明涉及式（I）化合物，其中Ar表示具有1至4个N，O和/或S原子和5至10个骨架原子的单环或双环芳族均聚或杂环，其可以是未取代的或羰基氧，Hal，A，OH，OA，NH 2，NHA，NA 2，NO 2，，CN，OCN，SCN，COOH，COOA，CONH 2，CONHA，CONA 2，NHCOA，NHCONH 2，NHSO 2 A，CHO，COA，SO 2 NH 2和/或S（O）9 A，A表示无支链，支链或具有1-14个C原子的环状烷基，其中一个或两个CH 2基团可以被O或S原子和/或被-CR-CH-基团和/或另外的1- 7 H原子可以被F和/或Cl，Hal：F，Cl，Br或I，D：NH，NH 2，NH 2，NH 2，CH CH 2，CH 3，OH，OA，O或S，E：CH 2，CH，NH或N，Y：E或饱和或不饱和键，X：CH 2，O或NH，Q：Hal，A，OH，OA，NH 2，NHA，N CN 2，NO 2，CN，OCN，SCN，COOH，COOA，CONH 2，CONHA，CONA 2 ，NHCOA，NHCONH 2，NHSO 2 A，CHO，COA，SO 2 NH 2或XM，涉及其制备和用途，用于制备用于治疗疾病，特别是涉及激酶的发展或过程中的肿瘤和/或疾病的药物。

4. 发明授权

US08859581B2 Azaheterocyclic compounds as kinase inhibitors 有权
标题翻译：氮杂环化合物作为激酶抑制剂
公开(公告)号：US08859581B2
公开(公告)日：2014-10-14
申请号：US11912462
申请日：2006-03-30
申请人： Timo Heinrich , Andree Blaukat , Wolfgang Staehle , Hartmut Greiner , Maria Kordowicz
发明人： Timo Heinrich , Andree Blaukat , Wolfgang Staehle , Hartmut Greiner , Maria Kordowicz
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to compounds of the formula (I), to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumors and/or diseases in the development or course of which kinases are involved.
摘要翻译：本发明涉及式（I）化合物的制备和用途，其用于制备用于治疗疾病，特别是涉及激酶发展过程中的肿瘤和/或疾病的药物。

5. 发明申请

US20090306122A1 SUBSTITUTED TETRAHYDROPYRROLOQUINOLINE DERIVATIVES AS KINASE MODULATORS, ESPECIALLY OF TYROSINE AND RAF KINASES 审中-公开
标题翻译：作为激酶调节剂的替代四氢呋喃醇衍生物，特别是酪氨酸激酶和RAF激酶
公开(公告)号：US20090306122A1
公开(公告)日：2009-12-10
申请号：US11908215
申请日：2006-02-13
申请人： Wolfgang Staehle , Timo Heinrich , Maria Kordowicz , Andree Blaukat , Lars Thore Burgdorf
发明人： Wolfgang Staehle , Timo Heinrich , Maria Kordowicz , Andree Blaukat , Lars Thore Burgdorf
IPC分类号： A61K31/437 , C07D471/06 , A61P35/00 , A61P27/00 , A61P29/00
CPC分类号： C07D471/06
摘要： Compound of the formula (I), in which X, R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.
摘要翻译：式（I）化合物，其中X，R 1，R 2和R 3具有权利要求1所示的含义，是酪氨酸激酶，特别是TIE-2和Raf激酶的抑制剂，特别可用于治疗肿瘤。

6. 发明申请

US20100160356A1 NOVEL CYCLOBUTYL COMPOUNDS AS KINASE INHIBITORS 审中-公开
标题翻译：新型环烷基化合物作为激酶抑制剂
公开(公告)号：US20100160356A1
公开(公告)日：2010-06-24
申请号：US12296138
申请日：2007-03-08
申请人： Timo Heinrich , Wolfgang Staehle , Hartmut Greiner , Andree Blaukat
发明人： Timo Heinrich , Wolfgang Staehle , Hartmut Greiner , Andree Blaukat
IPC分类号： A61K31/519 , C07D487/04 , A61P35/00 , A61P9/00 , A61P29/00
CPC分类号： C07D487/04
摘要： The invention relates to compounds of the formula I, to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases in the formation or course of which protein kinases are involved.
摘要翻译：本发明涉及式I化合物的制备和用途，用于制备用于治疗疾病，特别是涉及蛋白激酶的形成或过程中的肿瘤和/或疾病的药物。

7. 发明授权

US08877751B2 Benzothiazolone derivatives 有权
标题翻译：苯并噻唑酮衍生物
公开(公告)号：US08877751B2
公开(公告)日：2014-11-04
申请号：US13143467
申请日：2009-12-08
申请人： Frank Stieber , Oliver Schadt , Dieter Dorsch , Andree Blaukat
发明人： Frank Stieber , Oliver Schadt , Dieter Dorsch , Andree Blaukat
IPC分类号： A61K31/5377 , A61K31/505 , A61K31/41 , A61K31/425 , C07D413/14 , C07D417/14 , C07D417/10 , C07D277/68
CPC分类号： C07D417/10 , C07D277/68 , C07D417/14
摘要： Compounds of the formula I, in which R1, R2, R3, R3′, R4, R4′, E, E′, E″ and E′″ have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
摘要翻译：其中R1，R2，R3，R3'，R4，R4'，E，E'，E“和E”“具有权利要求1所示含义的式I化合物是酪氨酸激酶抑制剂，特别是Met 激酶，并且可以特别用于治疗肿瘤。

8. 发明申请

US20110269771A1 PYRIDAZINONE DERIVATIVES 有权
标题翻译：吡咯烷酮衍生物
公开(公告)号：US20110269771A1
公开(公告)日：2011-11-03
申请号：US13143646
申请日：2009-12-10
申请人： Dieter Dorsch , Oliver Schadt , Frank Stieber , Andree Blaukat
发明人： Dieter Dorsch , Oliver Schadt , Frank Stieber , Andree Blaukat
IPC分类号： C07D417/14 , A61P35/04 , A61P35/02 , A61K31/501
CPC分类号： C07D417/14 , C07D413/10 , C07D413/14 , C07D417/10
摘要： Compounds of the formula (I), in which D, R1, R2, R3, R4 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.
摘要翻译：式（I）化合物，其中D，R 1，R 2，R 3，R 4具有权利要求1所示的含义，是酪氨酸激酶，特别是Met激酶的抑制剂，并且可以特别用于治疗的肿瘤。

9. 发明申请

US20110136819A1 6-THIOXOPYRIDAZINE DERIVATIVES 审中-公开
标题翻译： 6-硫代吡啶衍生物
公开(公告)号：US20110136819A1
公开(公告)日：2011-06-09
申请号：US12673704
申请日：2008-07-18
申请人： Dieter Dorsch , Oliver Schadt , Andree Blaukat , Frank Stieber
发明人： Dieter Dorsch , Oliver Schadt , Andree Blaukat , Frank Stieber
IPC分类号： A61K31/501 , C07D403/12 , C07D417/10 , C07D417/14 , A61K31/506 , A61P35/00
CPC分类号： C07D237/18 , C07D403/10 , C07D417/10 , C07D417/14
摘要： Compounds of the formula I, in which R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
摘要翻译： R1，R2和R3具有权利要求1所述含义的式I化合物是酪氨酸激酶，特别是Met激酶的抑制剂，尤其可用于治疗肿瘤。

10. 发明申请

US20100280030A1 2-OXO-3-BENZYLBENZOXAZOL-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS MET KINASE INHIBITORS FOR THE TREATMENT OF TUMOURS 有权
标题翻译： 2-OXO-3-BENZYLBENZOXAZOL-2-ONE衍生物和相关化合物作为MET激动剂抑制剂治疗肿瘤
公开(公告)号：US20100280030A1
公开(公告)日：2010-11-04
申请号：US12663206
申请日：2008-05-08
申请人： Oliver Schadt , Dieter Dorsch , Frank Stieber , Andree Blaukat
发明人： Oliver Schadt , Dieter Dorsch , Frank Stieber , Andree Blaukat
IPC分类号： A61K31/5377 , C07D413/12 , A61K31/496 , C07D401/14 , A61K31/501 , C07D413/14 , A61P35/02 , A61P35/00
CPC分类号： C07D413/10 , C07D498/06
摘要： Compounds of the formula (I), in which R1, R2, R3, R3′, R4, R4′, E, E′, E″ and E′″ have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
摘要翻译：其中R 1，R 2，R 3，R 3'，R 4，R 4'，E'，E'，E“和E”具有权利要求1所示含义的式（I）化合物是酪氨酸激酶抑制剂，特别的Met激酶，并且可以特别用于治疗肿瘤。

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