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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.
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2.发明授权RecA inhibitors with antibiotic activity, compositions and methods of use 有权具有抗生素活性的RecA抑制剂，组合物和使用方法公开(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
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。
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3.发明授权Use of isoQC inhibitors in the treatment and prevention of inflammatory diseases or conditions 有权使用isoQC抑制剂治疗和预防炎性疾病或病症公开(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。
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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。
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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
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Patent Agency Ranking
公开(公告)号：US09499535B2
公开(公告)日：2016-11-22
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: A61K31/55 , A61K31/54 , A61K31/535 , C07D471/04
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.
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公开(公告)号：US20100125086A1
公开(公告)日：2010-05-20
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 Tremel
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 Tremel
IPC: A61K31/4178 , C12Q1/25 , A61K31/437 , A61K31/433 , A61K31/4184 , A61P29/00
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 demyelinising 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 神经性疼痛，移植物排斥/移植物衰竭/移植物血管病变，HIV感染/艾滋病，睾丸炎，结节性硬化症，吉兰巴利综合征，慢性炎症性脱髓鞘性多发性神经病和多发性硬化症; （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。
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8.发明申请公开(公告)号：US20090264342A1
公开(公告)日：2009-10-22
申请号：US12279237
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: A61K38/00 , C12Q1/68 , C12N5/02 , A61K31/70 , A61K31/435 , A61K31/352
CPC classification number: A61K45/06 , A61K38/12 , C12Q1/18 , G01N33/5023 , A61K2300/00
Abstract: The present invention provides methods for identifying target genes whose partial or complete functional inactivation potentiates the activity of an antibiotic agent, e.g., a quinolone antibiotic. The invention further provides methods for identifying agents that modulate expression of target genes or that modulate activity of expression products of target genes. Agents identified according to various methods of the invention potentiate the activity of antibiotics such as quinolones, aminoglycosides, peptide antibiotics and β-lactams. Also provided are agents that suppress and/or retard resistance to antibiotics. The inventive methods provide potentiating agents and compositions comprising potentiating agents and antibiotics. Such agents and compositions can be used for inhibiting growth or survival of a microbial cell or of treating a subject suffering from or susceptible to a microbial infection.
Abstract translation: 本发明提供用于鉴定其部分或完全功能失活增强抗生素试剂例如喹诺酮抗生素活性的靶基因的方法。 本发明还提供用于鉴定调节靶基因表达或调节靶基因表达产物的活性的试剂的方法。 根据本发明各种方法鉴定的药剂增强了抗生素如喹诺酮类，氨基糖苷类，肽类抗生素和β-内酰胺类的活性。 还提供了抑制和/或延缓抗生素抗性的药剂。 本发明的方法提供增效剂和包含增效剂和抗生素的组合物。 这些药剂和组合物可用于抑制微生物细胞的生长或存活或治疗患有或易受微生物感染的受试者。
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公开(公告)号：US07504436B2
公开(公告)日：2009-03-17
申请号：US10556175
申请日：2004-05-07
Applicant: Michael Thormann , Michael Almstetter
Inventor： Michael Thormann , Michael Almstetter
IPC: A61K31/185 , C07C259/06
CPC classification number: 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
Abstract: 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.
Abstract translation: 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。
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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。
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