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11. 发明授权

US07741354B2 Inhibitors of glutaminyl cyclase 有权
公开(公告)号：US07741354B2
公开(公告)日：2010-06-22
申请号：US11937159
申请日：2007-11-08
申请人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz
发明人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz
IPC分类号： A61K31/41 , C07D257/00
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein: R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, -alkoxy, -thioalkyl, —C(O)O-alkyl and —C(O)OH; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, haloalkyl, amino, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)O-alkyl and —C(O)OH; alkenyl; alkynyl; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -heteroaryl-heteroaryl; -aryl-aryl; -aryl (monocyclic or bicyclic); heteroaryl (monocyclic or bicyclic); heterocyclyl; or R2 together with R4 may form a carbocyclyl group optionally substituted by one or more alkyl groups; R3 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, amino, halogen, haloalkyl, hydroxyl, -alkoxy, -thioalkyl, —C(O)OH and —C(O)O-alkyl; alkenyl; -alkyl-aryl; -alkyl(aryl)2, -alkyl(heteroaryl)2, -alkyl(aryl)(heteroaryl), -alkyl-heteroaryl; -alkyl-heterocyclyl which heterocyclyl group may optionally be substituted by one or more groups selected from alkyl, hydroxy and oxo ; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-aryl; -aryl-O-aryl, -heteroaryl-heteroaryl; -aryl; heteroaryl; heterocyclyl; -aryl-alkyl-aryl; -aryl-O-alkyl-aryl; -alkyl-C(O)—NH-alkyl-aryl; -alkyl-C(O)—NH-alkyl-heteroaryl; -alkyl-C(O)—NH-alkyl-heterocyclyl; -alkyl-C(O)—(N-piperidinyl) or -alkyl-C(O)—(N-pyrrolidinyl) in which piperidinyl or pyrrolidinyl may optionally be fused to optionally substituted phenyl. R4 represents H or alkyl.

12. 发明授权

US07728146B2 Enzyme inhibitors 失效
标题翻译：酶抑制剂
公开(公告)号：US07728146B2
公开(公告)日：2010-06-01
申请号：US11734369
申请日：2007-04-12
申请人： Michael Thormann , Michael Almstetter , Andreas Treml
发明人： Michael Thormann , Michael Almstetter , Andreas Treml
IPC分类号： A61K31/4178 , C07D409/06
CPC分类号： C07D409/06 , C07D233/64 , C07D401/06 , C07D403/06 , C07D405/06
摘要： There is disclosed herein compounds of formula (I), wherein: R1, R2, R3, R4 and R5 are defined throughout the description and the claims. The compounds of formula (I) are useful for the treatment of neurological diseases and neurodegenerative diseases, e.g. anxiety, depression, Alzheimer's disease etc.
摘要翻译：本文公开了式（I）的化合物，其中：在整个说明书和权利要求书中限定了R1，R2，R3，R4和R5。式（I）化合物可用于治疗神经疾病和神经变性疾病，例如，焦虑，抑郁，阿尔茨海默病等

13. 发明申请

US20080207715A1 Novel Inhibitors of Glutaminyl Cyclase 有权
公开(公告)号：US20080207715A1
公开(公告)日：2008-08-28
申请号：US11937159
申请日：2007-11-08
申请人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz
发明人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz
IPC分类号： A61K31/41 , C07D403/02 , A61K35/04 , A61P25/00 , A61P19/00
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, wherein: R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, -alkoxy, -thioalkyl, —C(O)O-alkyl and —C(O)OH; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, haloalkyl, amino, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)O-alkyl and —C(O)OH; alkenyl; alkynyl; -alkyl-aryl; -alkyl-heteroaryl; -alkyl-heterocyclyl; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -heteroaryl-heteroaryl; -aryl-aryl; -aryl (monocyclic or bicyclic); heteroaryl (monocyclic or bicyclic); heterocyclyl; or R2 together with R4 may form a carbocyclyl group optionally substituted by one or more alkyl groups; R3 represents alkyl, which may optionally be substituted by one or more groups selected from amino, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, amino, halogen, haloalkyl, hydroxyl, -alkoxy, -thioalkyl, —C(O)OH and —C(O)O-alkyl; alkenyl; -alkyl-aryl; -alkyl(aryl)2, -alkyl(heteroaryl)2, -alkyl(aryl)(heteroaryl), -alkyl-heteroaryl; -alkyl-heterocyclyl which heterocyclyl group may optionally be substituted by one or more groups selected from alkyl, hydroxy and oxo ; -alkyl-carbocyclyl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-aryl; -aryl-O-aryl, -heteroaryl-heteroaryl; -aryl; heteroaryl; heterocyclyl; -aryl-alkyl-aryl; -aryl-O-alkyl-aryl; -alkyl-C(O)—NH-alkyl-aryl; -alkyl-C(O)—NH-alkyl-heteroaryl; -alkyl-C(O)—NH-alkyl-heterocyclyl; -alkyl-C(O)—(N-piperidinyl) or -alkyl-C(O)—(N-pyrrolidinyl) in which piperidinyl or pyrrolidinyl may optionally be fused to optionally substituted phenyl. R4 represents H or alkyl.

14. 发明申请

US20080207630A1 2-Aminocarbonyl Substituted Piperazine or Diaza-Cyclic Compounds as Apoptosis Protein Inhibitors (Iap) Modulators 失效
标题翻译： 2-氨基羰基取代的哌嗪或二氮杂环化合物作为凋亡蛋白抑制剂（Iap）调节剂
公开(公告)号：US20080207630A1
公开(公告)日：2008-08-28
申请号：US11911418
申请日：2006-04-13
申请人： Robert Eckl , Roswitha Taube , Michael Almstetter , Michael Thormann , Andreas Treml , Christopher Straub , Zhuoliang Chen
发明人： Robert Eckl , Roswitha Taube , Michael Almstetter , Michael Thormann , Andreas Treml , Christopher Straub , Zhuoliang Chen
IPC分类号： A61K31/496 , C07D241/04 , A61P35/04
CPC分类号： C07D241/04 , C07D295/185 , C07D401/04 , C07D403/06 , C07K5/06052 , C07K5/0806 , C07K7/06
摘要： The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates or pharmaceutically acceptable formulations thereof. These compounds may be used to modulate cellular proliferation and to prevent and/or treat proliferative diseases.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物，水合物或其药学上可接受的制剂。这些化合物可用于调节细胞增殖并预防和/或治疗增殖性疾病。

15. 发明申请

US20070060624A1 Novel bioisosteres of actinonin 失效
标题翻译：肌动蛋白的新型生物电子学
公开(公告)号：US20070060624A1
公开(公告)日：2007-03-15
申请号：US10556175
申请日：2004-05-07
申请人： Michael Thormann , Michael Almstetter
发明人： Michael Thormann , Michael Almstetter
IPC分类号： C07D213/56 , C07D207/30 , A61K31/44 , A61K31/40 , C07C259/04 , A61K31/19
CPC分类号： C07D213/40 , C07C259/06 , C07C259/08 , C07C2601/14 , C07C2602/10 , C07D209/14 , C07D209/20 , C07D209/94 , C07D213/56 , C07D215/12 , C07D215/18 , C07D243/08 , C07D295/13 , C07D307/14 , C07D405/12 , C07D491/08
摘要： The present invention relates to novel bioisosteres of the antibiotic actinonin of the general formula (I). The novel compounds are of particular interest as inhibitors of metalloproteinases.
摘要翻译：本发明涉及通式（I）的抗生素放线菌素的新型生物电子等排体。新化合物作为金属蛋白酶抑制剂是特别有意义的。

16. 发明授权

US08962860B2 Inhibitors of glutaminyl cyclase 有权
标题翻译：谷氨酰胺环化酶抑制剂
公开(公告)号：US08962860B2
公开(公告)日：2015-02-24
申请号：US12554611
申请日：2009-09-04
申请人： Ulrich Heiser , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Almstetter , Michael Thormann , Andreas Treml , Hans-Ulrich Demuth , Torsten Hoffman
发明人： Ulrich Heiser , Robert Sommer , Ulf-Torsten Gaertner , Antje Hamann , Michael Almstetter , Michael Thormann , Andreas Treml , Hans-Ulrich Demuth , Torsten Hoffman
IPC分类号： C07D403/04 , C07D403/06 , C07D417/04 , C07D471/04 , C07D405/14 , C07D417/14
CPC分类号： C07D403/04 , C07D403/06 , C07D405/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Compounds of general formula (I): wherein R1, R2, R3, R4, X and Y are as defined herein are inhibitors of glutaminyl cyclase and are therefore useful in treating conditions that can be treated by modulation of glutaminyl cyclase activity.
摘要翻译：通式（I）的化合物：其中R1，R2，R3，R4，X和Y如本文所定义，是谷氨酰胺酰环化酶的抑制剂，因此可用于治疗可通过调节谷氨酰胺酰环化酶活性治疗的病症。

17. 发明授权

US08420684B2 Inhibitors of glutaminyl cyclase 有权
标题翻译：谷氨酰胺环化酶抑制剂
公开(公告)号：US08420684B2
公开(公告)日：2013-04-16
申请号：US11937146
申请日：2007-11-08
申请人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
发明人： Michael Thormann , Michael Altmstetter , Andreas Treml , Ulrich Heiser , Mirko Buchholz , Andre J. Niestroj
IPC分类号： A61K31/4166 , A61K31/4178 , C07D233/70 , C07D233/88
CPC分类号： C07D405/14 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/14 , C07D417/14
摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents heteroaryl; -carbocyclyl-heteroaryl; -alkenylheteroaryl or -alkylheteroaryl; R2 represents alkyl which may optionally be substituted by hydroxy; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl and hydroxy; aryl; -aryl-heteroaryl; -heteroaryl-aryl; -aryl-heterocyclyl; H; heteroaryl; or heterocyclyl, which may optionally be substituted by one or more groups selected from alkyl oxo and hydroxy; R3 represents alkyl which may optionally be substituted by one of more groups selected from alkoxy, amine, hydroxy and —C(O)Oalkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl haloalkyl, alkoxy, amine, hydroxy and —C(O)Oalkyl; -alkyl-aryl; -alkyl(aryl)2; -alkyl-heteroaryl; -alkyl(heteroaryl)2; -alkyl(heteroaryl)(aryl); -aryl-O-aryl; aryl; heterocyclyl, -alkyl-C(O)-heterocyclyl, -alkyl-heterocyclyl, -alkyl-C(O)—NR5-heterocyclyl or -alkyl(heterocyclyl)2 in any of which groups heterocyclyl may be optionally substituted by one or more groups selected from alkyl hydroxy and oxo; -heteroaryl; or -hydroxyalkylaryl; R4 represents H or C1-3 alkyl; R5 represents H or C1-3 alkyl; and X represents O or S.
摘要翻译：本发明涉及式（I）化合物，其用于疾病治疗的组合和用途，或其药学上可接受的盐，溶剂化物或多晶型物，包括其所有互变异构体和立体异构体，其中R 1表示杂芳基; 羧基 - 杂芳基; - 烯基杂芳基或 - 烷基杂芳基; R 2表示可任意被羟基取代的烷基; 碳环基，其可任选被一个或多个选自烷基和羟基的基团取代; 芳基; 芳基 - 杂芳基; - 杂芳基 - 芳基; 芳基 - 杂环基 H; 杂芳基; 或杂环基，其可任选被一个或多个选自烷基氧基和羟基的基团取代; R3表示可以任选被选自烷氧基，胺，羟基和-C（O）O烷基的更多个基团之一取代的烷基; 碳环基，其可任选被一个或多个选自烷基卤代烷基，烷氧基，胺，羟基和-C（O）O烷基的基团取代; - 烷基 - 芳基; - 烷基（芳基）2; - 烷基 - 杂芳基 - 烷基（杂芳基）2; - 烷基（杂芳基）（芳基）; 芳基-O-芳基; 芳基; 杂环基， - 烷基-C（O） - 杂环基， - 烷基 - 杂环基， - 烷基-C（O）-NR5 - 杂环基或 - 烷基（杂环基）2，其中任意一个组杂环基可以任选被一个或多个基团取代选自烷基羟基和氧代; 杂芳基或 - 羟基烷基芳基; R 4表示H或C 1-3烷基; R5表示H或C1-3烷基; X表示O或S.

18. 发明申请

US20120329785A1 Novel kinase inhibitors 有权
标题翻译：新型激酶抑制剂
公开(公告)号：US20120329785A1
公开(公告)日：2012-12-27
申请号：US13506509
申请日：2012-04-23
申请人： Michael Thormann , Andreas Treml , Michael Almstetter , Roland Koestler , Nasser Yehia
发明人： Michael Thormann , Andreas Treml , Michael Almstetter , Roland Koestler , Nasser Yehia
IPC分类号： C07D471/04 , C07D401/14 , A61K31/496 , A61K31/5513 , A61P27/02 , A61K31/5377 , A61P29/00 , A61P37/06 , A61P37/08 , A61K31/437 , C07D413/14
CPC分类号： C07D471/04
摘要： The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases.
摘要翻译：本发明涉及能够抑制一种或多种激酶，特别是SYK（脾脏酪氨酸激酶），LRRK2（富含亮氨酸重复激酶2）和/或MYLK（肌球蛋白轻链激酶）的新型的式（I）化合物或其突变体。该化合物可用于治疗各种疾病。

19. 发明申请

US20100234397A1 ENZYME INHIBITORS 审中-公开
标题翻译：酶抑制剂
公开(公告)号：US20100234397A1
公开(公告)日：2010-09-16
申请号：US12750930
申请日：2010-03-31
申请人： Michael Thormann , Michael Almstetter , Andreas Treml
发明人： Michael Thormann , Michael Almstetter , Andreas Treml
IPC分类号： A61K31/497 , A61K31/4164 , A61K31/4439 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/08 , A61P25/18 , A61P29/00 , A61P37/00 , A61P35/00 , A61P37/06
CPC分类号： C07D409/06 , C07D233/64 , C07D401/06 , C07D403/06 , C07D405/06
摘要： There is disclosed herein methods for using compounds of formula (I), wherein: R1, R2, R3, R4 and R5 are defined throughout the description and the claims. The compounds of formula (I) are useful for the treatment of neurological diseases and neurodegenerative diseases, e.g. anxiety, depression, Alzheimer's disease etc.
摘要翻译：本文公开了使用式（I）化合物的方法，其中：在整个说明书和权利要求书中限定了R1，R2，R3，R4和R5。式（I）化合物可用于治疗神经疾病和神经变性疾病，例如，焦虑，抑郁，阿尔茨海默病等

20. 发明申请

US20100029597A1 RECA INHIBITORS WITH ANTIBIOTIC ACTIVITY, COMPOSITIONS AND METHODS OF USE 有权
标题翻译：具有抗生物活性的RECA抑制剂，组合物和使用方法
公开(公告)号：US20100029597A1
公开(公告)日：2010-02-04
申请号：US12279243
申请日：2007-02-13
申请人： Guillaume Cottarel , Jamey Wierzbowski , Kollol Pal , Michael Kohanski , Daniel Dwyer , James Collins , Michael Almstetter , Michael Thormann , Andreas Treml
发明人： Guillaume Cottarel , Jamey Wierzbowski , Kollol Pal , Michael Kohanski , Daniel Dwyer , James Collins , Michael Almstetter , Michael Thormann , Andreas Treml
IPC分类号： A61K31/65 , A61K31/352 , A61K31/382 , A61K31/47 , A61P31/04
CPC分类号： A61K45/06 , A61K38/12 , C12Q1/18 , G01N33/5023 , A61K2300/00
摘要： The present invention is directed to the use of RecA inhibitors as antibiotic agents, and provides RecA inhibitors useful in treating infections. Also provided are various compositions and methods associated with RecA inhibition.
摘要翻译：本发明涉及使用RecA抑制剂作为抗生素，并提供可用于治疗感染的RecA抑制剂。还提供了与RecA抑制相关的各种组合物和方法。

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