公开(公告)号：US09802937B2

公开(公告)日：2017-10-31

申请号：US13506510

申请日：2012-04-23

Applicant: Michael Thormann ,  Andreas Treml ,  Michael Almstetter ,  Nadine Traube

Inventor： Michael Thormann ,  Andreas Treml ,  Michael Almstetter ,  Nadine Traube

IPC: C07D487/04 ,  A61K31/519 ,  A61P29/00 ,  A61P11/06 ,  A61P37/08 ,  A61P27/02 ,  A61P17/04 ,  A61P37/06 ,  A61P35/02 ,  A61P35/04 ,  A61P35/00 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D519/00

Abstract: 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. These diseases include autoimmune diseases, inflammatory diseases, bone diseases, metabolic diseases, neurological and neurodegenerative diseases, cancer, cardiovascular diseases, allergies, asthma, alzheimer's disease, parkinson's disease, skin disorders, eye diseases, infectious diseases and hormone-related diseases.

公开(公告)号：US09155792B2

公开(公告)日：2015-10-13

申请号：US12279243

申请日：2007-02-13

Applicant: Guillaume Cottarel ,  Jamey Wierzbowski ,  Kollol Pal ,  Michael Kohanski ,  Daniel Dwyer ,  James Collins ,  Michael Almstetter ,  Michael Thormann ,  Andreas Treml

Inventor： Guillaume Cottarel ,  Jamey Wierzbowski ,  Kollol Pal ,  Michael Kohanski ,  Daniel Dwyer ,  James Collins ,  Michael Almstetter ,  Michael Thormann ,  Andreas Treml

IPC: A61K49/00 ,  C07H19/16 ,  A61K38/00 ,  A61K45/06 ,  A61K38/12 ,  C12Q1/18 ,  G01N33/50

CPC classification number: A61K45/06 ,  A61K38/12 ,  C12Q1/18 ,  G01N33/5023 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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抑制有关的各种组合物和方法。

公开(公告)号：US08889709B2

公开(公告)日：2014-11-18

申请号：US12554584

申请日：2009-09-04

Applicant: Hans-Ulrich Demuth ,  Stephan Schilling ,  Michael Wermann ,  Holger Cynis ,  Astrid Kehlen ,  Daniel Friedrich ,  Torsten Hoffmann ,  Kathrin Gans ,  Jens-Ulrich Rahfeld ,  Ulrich Heiser ,  Michael Almstetter ,  Robert Sommer ,  Ulf-Torsten Gaertner ,  Antje Hamann ,  Michael Thormann ,  Andreas Treml

Inventor： Hans-Ulrich Demuth ,  Stephan Schilling ,  Michael Wermann ,  Holger Cynis ,  Astrid Kehlen ,  Daniel Friedrich ,  Torsten Hoffmann ,  Kathrin Gans ,  Jens-Ulrich Rahfeld ,  Ulrich Heiser ,  Michael Almstetter ,  Robert Sommer ,  Ulf-Torsten Gaertner ,  Antje Hamann ,  Michael Thormann ,  Andreas Treml

IPC: A01N43/42 ,  C12N9/00 ,  C12N9/10 ,  C12N1/20 ,  C12N15/00 ,  C07H21/04 ,  C07D417/12 ,  C07D405/12 ,  C07D233/61 ,  C07D409/12 ,  C07D403/12 ,  C07D413/12 ,  C07D403/06 ,  C07D401/12 ,  C07D233/54 ,  C07D235/06

CPC classification number: C07D233/54 ,  C07D233/61 ,  C07D235/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C12N9/104

Abstract: The present invention relates in general to an inhibitor of a glutaminyl peptide cyclotransferase-like protein (QPCTL), and the use thereof for the treatment and/or prevention of an inflammatory disease or disorder selected from the group consisting of (a) chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis; (b) other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis, Guillain-Barré syndrome, chronic inflammatory demyelinizing polyradiculoneuropathy and multiple sclerosis; (c) neuroinflammation; and (d) neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia, which may result from neuroinflammation.

Abstract translation: 本发明一般涉及谷氨酰胺肽环转移酶样蛋白（QPCTL）的抑制剂及其用于治疗和/或预防炎性疾病或病症的用途，所述炎性疾病或病症选自（a）慢性和急性 炎症，例如 类风湿关节炎，动脉粥样硬化，再狭窄，胰腺炎; （b）其他炎性疾病，例如 艾滋病，睾丸炎，结节性硬化症，吉兰巴利综合征，慢性炎性脱髓鞘性多发性神经系统疾病和多发性硬化; （c）神经炎症; 和（d）神经变性疾病，例如 轻度认知障碍（MCI），阿尔茨海默氏症，唐氏综合征神经变性，家族性英国痴呆和家族性丹麦痴呆，可能由神经炎症引起。

公开(公告)号：US20100119475A1

公开(公告)日：2010-05-13

申请号：US12554611

申请日：2009-09-04

Applicant: Ulrich Heiser ,  Robert Sommer ,  Ulf-Torsten Gaertner ,  Antje Hamann ,  Michael Almstetter ,  Michael Thormann ,  Andreas Treml ,  Hans-Ulrich Demuth ,  Torsten Hoffman

Inventor： Ulrich Heiser ,  Robert Sommer ,  Ulf-Torsten Gaertner ,  Antje Hamann ,  Michael Almstetter ,  Michael Thormann ,  Andreas Treml ,  Hans-Ulrich Demuth ,  Torsten Hoffman

IPC: A61K31/4184 ,  C07D417/14 ,  C07D403/10 ,  C07D405/14 ,  C07D471/04 ,  A61K31/433 ,  A61K31/4439 ,  A61K39/395 ,  A61K38/20 ,  A61K38/21 ,  A61P35/00 ,  A61P3/00 ,  A61P25/00

CPC classification number: C07D403/04 ,  C07D403/06 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20070244177A1

公开(公告)日：2007-10-18

申请号：US11734369

申请日：2007-04-12

Applicant: Michael Thormann ,  Michael Almstetter ,  Andreas Treml

Inventor： Michael Thormann ,  Michael Almstetter ,  Andreas Treml

IPC: A61K31/416 ,  A61K31/4152 ,  C07D403/02 ,  C07D231/12

CPC classification number: C07D409/06 ,  C07D233/64 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06

Abstract: There is dislosed 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.

Abstract translation: 在本文中，式（I）的化合物是非离子的，其中：R 1，R 2，R 3，R 4， 在整个说明书和权利要求书中限定了SUP＆gt;和R＆lt; 5＆gt;。 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

公开(公告)号：US08962860B2

公开(公告)日：2015-02-24

申请号：US12554611

申请日：2009-09-04

Applicant: Ulrich Heiser ,  Robert Sommer ,  Ulf-Torsten Gaertner ,  Antje Hamann ,  Michael Almstetter ,  Michael Thormann ,  Andreas Treml ,  Hans-Ulrich Demuth ,  Torsten Hoffman

Inventor： Ulrich Heiser ,  Robert Sommer ,  Ulf-Torsten Gaertner ,  Antje Hamann ,  Michael Almstetter ,  Michael Thormann ,  Andreas Treml ,  Hans-Ulrich Demuth ,  Torsten Hoffman

IPC: C07D403/04 ,  C07D403/06 ,  C07D417/04 ,  C07D471/04 ,  C07D405/14 ,  C07D417/14

CPC classification number: C07D403/04 ,  C07D403/06 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14 ,  C07D471/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20120329785A1

公开(公告)日：2012-12-27

申请号：US13506509

申请日：2012-04-23

Applicant: Michael Thormann ,  Andreas Treml ,  Michael Almstetter ,  Roland Koestler ,  Nasser Yehia

Inventor： Michael Thormann ,  Andreas Treml ,  Michael Almstetter ,  Roland Koestler ,  Nasser Yehia

IPC: C07D471/04 ,  C07D401/14 ,  A61K31/496 ,  A61K31/5513 ,  A61P27/02 ,  A61K31/5377 ,  A61P29/00 ,  A61P37/06 ,  A61P37/08 ,  A61K31/437 ,  C07D413/14

CPC classification number: C07D471/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100234397A1

公开(公告)日：2010-09-16

申请号：US12750930

申请日：2010-03-31

Applicant: Michael Thormann ,  Michael Almstetter ,  Andreas Treml

Inventor： Michael Thormann ,  Michael Almstetter ,  Andreas Treml

IPC: 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 classification number: C07D409/06 ,  C07D233/64 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06

Abstract: 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.

Abstract translation: 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

公开(公告)号：US20100029597A1

公开(公告)日：2010-02-04

申请号：US12279243

申请日：2007-02-13

Applicant: Guillaume Cottarel ,  Jamey Wierzbowski ,  Kollol Pal ,  Michael Kohanski ,  Daniel Dwyer ,  James Collins ,  Michael Almstetter ,  Michael Thormann ,  Andreas Treml

Inventor： Guillaume Cottarel ,  Jamey Wierzbowski ,  Kollol Pal ,  Michael Kohanski ,  Daniel Dwyer ,  James Collins ,  Michael Almstetter ,  Michael Thormann ,  Andreas Treml

IPC: A61K31/65 ,  A61K31/352 ,  A61K31/382 ,  A61K31/47 ,  A61P31/04

CPC classification number: A61K45/06 ,  A61K38/12 ,  C12Q1/18 ,  G01N33/5023 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20050177280A1

公开(公告)日：2005-08-11

申请号：US10508355

申请日：2003-03-24

Applicant: Michael Almstetter ,  Peter Zegar ,  Andreas Tremi ,  Michael Thormann ,  Lutz Weber

Inventor： Michael Almstetter ,  Peter Zegar ,  Andreas Tremi ,  Michael Thormann ,  Lutz Weber

IPC: B01J19/00 ,  G05B21/00 ,  G06F19/00

CPC classification number: B01J19/0046 ,  B01J2219/00689 ,  B01J2219/00695 ,  B01J2219/007 ,  B01J2219/0072 ,  G16C20/10 ,  G16C20/30 ,  G16C20/70

Abstract: A preferred embodiment of the present invention comprises method for planning the synthesis of one or more chemical compounds with specified chemical properties, comprising the steps of: (a) representing a space of synthesis plans, wherein each synthesis plan in the space of synthesis plans represents one or more vitual reaction schemas applied to one or more classes of virtual input reactants; (b) representing a space of virtual compounds, wherein each compound in the space of virtual compounds is a product of one or more of said synthesis plans; (c) constructing a first mapping from the space of virtual compounds to range space representing the desirability of a compound, wherein the first mapping is determined by one or more compound properties being measured; and (d) searching the space of synthesis plans for desirable compounds as represented in the range space.

Abstract translation: 本发明的优选实施方案包括用于规划具有特定化学性质的一种或多种化学化合物的合成的方法，包括以下步骤：（a）表示合成计划的空间，其中合成计划空间中的每个合成计划表示 一个或多个虚拟反应模式应用于一类或多类虚拟输入反应物; （b）表示虚拟化合物的空间，其中虚拟化合物空间中的每种化合物是一种或多种所述合成计划的产物; （c）构建从虚拟化合物的空间到表示化合物的适宜性的范围空间的第一映射，其中第一映射由被测量的一种或多种化合物性质确定; 和（d）在合成计划的空间中搜索在范围空间中表示的所需化合物。