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1. 发明公开

US20230373985A1 KINASE MODULATORS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：US20230373985A1
公开(公告)日：2023-11-23
申请号：US18030723
申请日：2021-07-12
申请人： Origenis Gmbh , Neuron23, Inc.
发明人： Roland KOESTLER , Nasser Yehia , Jean Tassel , Marcus Wegmann , Federico Medda , Patricia Perez-Gallan , Christiane Gilch , Michael Thormann , Andreas Treml , Michael Almstetter , Zhonghua Pei , Scott Savage
IPC分类号： C07D417/12 , C07D401/14 , C07D491/052 , C07D487/04 , C07D413/12 , C07D249/06 , C07D401/12 , C07D413/14 , C07D417/14 , C07D405/12 , C07D231/38 , C07D498/04
CPC分类号： C07D417/12 , C07D401/14 , C07D491/052 , C07D487/04 , C07D413/12 , C07D249/06 , C07D401/12 , C07D413/14 , C07D417/14 , C07D405/12 , C07D231/38 , C07D498/04
摘要： The present invention relates to novel compounds that modulate the activity of one or more kinases, such as TYK2 or mutants thereof. The compounds, which may be kinase inhibitors or activators, are useful for treating autoimmune diseases, such as, such as psoriasis, lupus, multiple sclerosis, and inflammatory bowel disease.

2. 发明申请

US20220380373A1 1,4-DIHYDROBENZO[D]PYRAZOLO[3,4-F][1,3]DIAZEPINE DERIVATIVES AND RELATED COMPOUNDS AS LRRK2, NUAK1 AND/OR TYK2 KINASE MODULATORS FOR THE TREATMENT OF E.G. AUTOIMMUNE DISEASE 有权
公开(公告)号：US20220380373A1
公开(公告)日：2022-12-01
申请号：US17642136
申请日：2020-09-11
申请人： Origenis GMBH
发明人： Roland Koestler , Jean Tassel , Michael Thormann , Nasser Yehia , Andreas Treml , Michael Almstetter
IPC分类号： C07D487/04 , C07D487/14
摘要： The present invention relates to compounds of formula (I) that are capable of modulating, e.g., inhibiting or activating, one or more kinases, especially LRRK2 and/or NUAK1 and/or TYK2 or mutants thereof. The compounds are useful for treating diseases, such as 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. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 40 to 146; examples 1 to 63; compounds 1 to 248; tables 1 to 3). Preferred compounds are e.g. 1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine derivatives and related compounds. An exemplary compound is e.g. 5-(2,6-difluorophenyl)-8-methoxy-1,4-dihydrobenzo[d]pyrazolo[3,4-f][1,3]diazepine (example 49). (Formula (II):

3. 发明申请

US20220380374A1 1,4-DIHYDROBENZO[D]PYRAZOLO[3,4-F][1,3]DIAZEPINE DERIVATIVES AND RELATED COMPOUNDS AS LRRK2, NUAK1 AND/OR TYK2 KINASE MODULATORS FOR THE TREATMENT OF E.G. AUTOIMMUNE DISEASE 有权
公开(公告)号：US20220380374A1
公开(公告)日：2022-12-01
申请号：US17642142
申请日：2020-09-11
申请人： Origenis GMBH
发明人： Roland Koestler , Michael Thormann , Jean Tassel , Nasser Yehia , Andreas Treml , Michael Almstetter
IPC分类号： C07D487/04 , C07D471/14
摘要： The present invention relates to compounds of formula (I) that are capable of modulating, e.g., inhibiting or activating, one or more kinases, especially LRRK2 and/or NUAK1 and/or TYK2 or mutants thereof. The compounds are useful for treating diseases, such as 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. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 40 to 146; examples 1 to 63; compounds 1 to 248; tables 1 to 3). Preferred compounds are e.g. 1,4-dihydrobenzo[d]pyrazolo[3,4-f] [1,3]diazepine derivatives and related compounds. An exemplary compound is e.g. 5-(2,6-difluorophenyl)-8-methoxy-1,4-dihydrobenzo[d]pyrazolo[3,4-f] [1,3]diazepine (example 49). (Formula (II)).

4. 发明申请

US20180305356A1 NOVEL KINASE INHIBITORS 审中-公开
公开(公告)号：US20180305356A1
公开(公告)日：2018-10-25
申请号：US15983423
申请日：2018-05-18
申请人： Origenis GmbH
发明人： Michael Almstetter , Michael Thormann , Andreas Treml , Roland Koestler , Nasser Yehia
IPC分类号： C07D471/04 , A61K31/444
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. 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.

5. 发明授权

US10752624B2 Kinase inhibitors 有权
公开(公告)号：US10752624B2
公开(公告)日：2020-08-25
申请号：US15983423
申请日：2018-05-18
申请人： Origenis GmbH
发明人： Michael Almstetter , Michael Thormann , Andreas Treml , Roland Koestler , Nasser Yehia
IPC分类号： C07D471/04 , A61K31/444
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. 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.

6. 发明授权

US10000482B2 Kinase inhibitors 有权
公开(公告)号：US10000482B2
公开(公告)日：2018-06-19
申请号：US14436152
申请日：2013-10-18
申请人： Origenis GmbH
发明人： Michael Almstetter , Michael Thormann , Andreas Treml , Roland Koestler , Nasser Yehia
IPC分类号： C07D471/04 , A61K31/444
CPC分类号： C07D471/04 , A61K31/444
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. 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.

7. 发明申请

US20150259340A1 NOVEL KINASE INHIBITORS 有权
标题翻译：新鲜激素抑制剂
公开(公告)号：US20150259340A1
公开(公告)日：2015-09-17
申请号：US14436152
申请日：2013-10-18
申请人： ORIGENIS GMBH
发明人： Michael Almstetter , Michael Thormann , Andreas Treml , Roland Koestler , Nasser Yehia
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K31/444
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. 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.
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。这些疾病包括自身免疫性疾病，炎性疾病，骨病，代谢疾病，神经和神经退行性疾病，癌症，心血管疾病，过敏症，哮喘，阿尔茨海默病，帕金森病，皮肤病，眼病，感染性疾病和激素相关疾病。

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