公开(公告)号：US20240317682A1

公开(公告)日：2024-09-26

申请号：US18680563

申请日：2024-05-31

申请人： Omeros Corporation

发明人： Neil S. Cutshall ,  Jennifer Lynn Gage ,  Sara Rebecca Goldstein ,  Do Yeon Kwon ,  Thomas L. Little ,  Markus Metz ,  Peter Kurt Nollert von Specht ,  Jennifer Tsoung

IPC分类号： C07D207/16 ,  C07D403/04 ,  C07D413/04 ,  C07D471/04

CPC分类号： C07D207/16 ,  C07D403/04 ,  C07D413/04 ,  C07D471/04

摘要： The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.

公开(公告)号：US20240307537A1

公开(公告)日：2024-09-19

申请号：US18451632

申请日：2023-08-17

申请人： Omeros Corporation

发明人： Michael Cicirelli ,  Neil S. Cutshall ,  Gregory A. Demopulos ,  George A. Gaitanaris ,  Marc A. Gavin ,  Alexander Gragerov ,  Thomas L. Little ,  Rene Onrust

IPC分类号： A61K39/00 ,  A61K31/17 ,  A61K31/341 ,  A61K31/381 ,  A61K31/4409 ,  A61K31/473 ,  A61K31/495 ,  A61K31/496 ,  A61K31/502 ,  A61K31/506 ,  A61K31/519 ,  A61K31/522 ,  A61K31/53 ,  A61K31/55 ,  A61K39/395 ,  A61K45/06 ,  A61P35/00 ,  C07K16/28 ,  G01N33/574

CPC分类号： A61K39/4643 ,  A61K31/17 ,  A61K31/341 ,  A61K31/381 ,  A61K31/4409 ,  A61K31/473 ,  A61K31/495 ,  A61K31/496 ,  A61K31/502 ,  A61K31/506 ,  A61K31/519 ,  A61K31/522 ,  A61K31/53 ,  A61K31/55 ,  A61K39/39558 ,  A61K45/06 ,  A61P35/00 ,  C07K16/28 ,  G01N33/57488 ,  A61K2039/505 ,  A61K2039/545 ,  C07K2317/76

摘要： This disclosure is directed to compounds, compositions, and methods for the treatment of various diseases and/or conditions related to G protein-coupled receptor 174 (e.g., cancers).

公开(公告)号：US20170096420A1

公开(公告)日：2017-04-06

申请号：US15291948

申请日：2016-10-12

申请人： Omeros Corporation

发明人： Neil S. Cutshall ,  Kenneth M. Ferguson ,  Charles Prince Zuta

IPC分类号： C07D417/10

CPC分类号： C07D417/10

摘要： The present invention is directed to a pure enantiomer of 1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, in particular, (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone. The present invention is also directed a crystal structure of (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, a pharmaceutical composition of (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, a method of inhibiting PDE10 with (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, and a process and particular individual intermediates used in the production of (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone.

公开(公告)号：US20130196994A1

公开(公告)日：2013-08-01

申请号：US13679818

申请日：2012-11-16

申请人： Omeros Corporation

发明人： Neil S. Cutshall ,  Jennifer Lynn Gage ,  Thomas Neil Wheeler ,  Thomas L. Little

IPC分类号： A61K31/5377 ,  A61K31/422 ,  A61K31/454 ,  A61K31/421 ,  A61K31/4709 ,  A61K31/4245 ,  A61K31/497 ,  A61K31/433 ,  A61K31/4155 ,  A61K31/341 ,  A61K31/4545 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/415 ,  A61K31/427

CPC分类号： C07D307/46 ,  A61K31/341 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/5377 ,  C07D231/12 ,  C07D285/08 ,  C07D285/12 ,  C07D307/34 ,  C07D307/40 ,  C07D401/04 ,  C07D405/10 ,  C07D407/10 ,  C07D413/10 ,  C07D417/10 ,  Y02A50/465

摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.

公开(公告)号：US20240228499A1

公开(公告)日：2024-07-11

申请号：US18523642

申请日：2023-11-29

申请人： Omeros Corporation

发明人： Neil S. Cutshall ,  Jennifer Lynn Gage ,  Do Yeon Kwon ,  Thomas L. Little ,  Markus Metz ,  Peter Kurt Nollert von Specht ,  Jennifer Tsoung ,  Sudheer Babu Vaddela ,  Connor Weidle

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  C07D519/00

CPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  C07D519/00

摘要： The disclosure provides synthetic compositions useful as inhibitors of mannan-binding lectin-associated serine protease-2 (MASP-2), including compositions that selectively inhibit MASP-2 over thrombin, as well as methods for the manufacture and use thereof.

公开(公告)号：US20180118711A1

公开(公告)日：2018-05-03

申请号：US15694342

申请日：2017-09-01

申请人： Omeros Corporation

发明人： Neil S. Cutshall ,  Jennifer Lynn Gage ,  Thomas Neil Wheeler

IPC分类号： C07D401/04 ,  C07C251/80 ,  C07D295/135 ,  C07C243/32 ,  C07D333/60 ,  C07D319/18 ,  C07D317/62 ,  C07D295/155 ,  C07D275/02 ,  C07D265/36 ,  C07D257/06 ,  C07D249/08 ,  C07D249/04 ,  C07D235/16 ,  C07D231/12 ,  C07D215/14 ,  C07D213/74 ,  C07D213/56 ,  C07C255/66 ,  C07C251/88 ,  C07C251/86 ,  A61K31/54 ,  A61K31/5375 ,  A61K31/47 ,  A61K31/425 ,  A61K31/4196 ,  A61K31/4184 ,  A61K31/415 ,  A61K31/41 ,  A61K31/40 ,  A61K31/36 ,  A61K31/357 ,  A61K31/15

CPC分类号： C07D401/04 ,  A61K31/15 ,  A61K31/357 ,  A61K31/36 ,  A61K31/40 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/4196 ,  A61K31/425 ,  A61K31/47 ,  A61K31/5375 ,  A61K31/54 ,  C07C243/32 ,  C07C251/80 ,  C07C251/86 ,  C07C251/88 ,  C07C255/66 ,  C07C2601/08 ,  C07D213/56 ,  C07D213/74 ,  C07D215/14 ,  C07D231/12 ,  C07D235/16 ,  C07D249/04 ,  C07D249/08 ,  C07D257/06 ,  C07D265/36 ,  C07D275/02 ,  C07D295/135 ,  C07D295/155 ,  C07D317/62 ,  C07D319/18 ,  C07D333/60

摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.

公开(公告)号：US09920045B2

公开(公告)日：2018-03-20

申请号：US15344372

申请日：2016-11-04

申请人： Omeros Corporation

发明人： Ekaterina Albert ,  Jennifer Leigh Nelson ,  Christopher Scott Seadeek ,  Karl Reineke ,  Marco Jonas ,  Suba Iyer ,  Xufeng Sun ,  Neil S. Cutshall ,  Jennifer Lynn Gage ,  Thomas L. Little ,  Wayne Douglas Luke ,  Elisabeth C. A. Brot ,  Michael James McDermott

IPC分类号： C07D417/10

CPC分类号： C07D417/10 ,  C07B2200/13

摘要： The invention relates to a novel variable hydrate crystalline form of 1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, methods for the preparation thereof, pharmaceutical compositions thereof and their use in the inhibition of PDE10.

公开(公告)号：US20170152238A1

公开(公告)日：2017-06-01

申请号：US15229020

申请日：2016-08-04

申请人： Omeros Corporation

发明人： Neil S. Cutshall ,  Jennifer Lynn Gage ,  Thomas Neil Wheeler ,  Thomas L. Little

IPC分类号： C07D307/46 ,  C07D417/10 ,  C07D407/10 ,  C07D413/10 ,  C07D405/10

CPC分类号： C07D307/46 ,  A61K31/341 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/5377 ,  C07D231/12 ,  C07D285/08 ,  C07D285/12 ,  C07D307/34 ,  C07D307/40 ,  C07D401/04 ,  C07D405/10 ,  C07D407/10 ,  C07D413/10 ,  C07D417/10 ,  Y02A50/465

摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.

公开(公告)号：US20160015715A1

公开(公告)日：2016-01-21

申请号：US14806007

申请日：2015-07-22

申请人： Omeros Corporation

发明人： John E. Bergmann ,  Neil S. Cutshall ,  Gregory A. Demopulos ,  Vincent A. Florio ,  George A. Gaitanaris ,  Patrick Gray ,  John Hohmann ,  Rene Onrust ,  Hongkui Zeng

IPC分类号： A61K31/551 ,  A61K31/4162 ,  A61K31/506 ,  A61K31/505 ,  A61K31/4025 ,  A61K31/381 ,  A61K31/4985 ,  A61K31/122 ,  A61K31/085 ,  A61K31/192 ,  A61K31/527 ,  A61K31/542 ,  A61K45/06 ,  A61K31/198 ,  A61K31/4439

CPC分类号： A61K31/551 ,  A61K31/00 ,  A61K31/085 ,  A61K31/122 ,  A61K31/137 ,  A61K31/192 ,  A61K31/195 ,  A61K31/198 ,  A61K31/381 ,  A61K31/4025 ,  A61K31/4162 ,  A61K31/425 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/527 ,  A61K31/542 ,  A61K45/06 ,  C07D471/04 ,  A61K2300/00

摘要： A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act.

摘要翻译： 通过施用治疗有效量的PDE7抑制剂来治疗与神经运动障碍的病理学相关的运动异常的方法，例如帕金森病或不宁腿综合症。 本发明的一个方面提供了与多巴胺激动剂或前体如左旋多巴结合施用PDE和抑制剂。 在本发明的另一方面，PDE7抑制剂可以相对于已知与帕金森病病理学有关的其它分子靶标（i）可能对PDE7具有选择性，或（ii）其他治疗有效的药物 治疗帕金森病。

公开(公告)号：US09102643B2

公开(公告)日：2015-08-11

申请号：US14177952

申请日：2014-02-11

申请人： Omeros Corporation

发明人： Neil S. Cutshall ,  Jennifer Lynn Gage ,  Thomas Neil Wheeler ,  Thomas L. Little

IPC分类号： C07D307/34 ,  C07D307/40 ,  C07D231/12 ,  C07D401/04 ,  C07D405/10 ,  C07D413/10 ,  C07D417/10 ,  A61K31/341 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/5377 ,  C07D285/12

CPC分类号： C07D307/46 ,  A61K31/341 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/5377 ,  C07D231/12 ,  C07D285/08 ,  C07D285/12 ,  C07D307/34 ,  C07D307/40 ,  C07D401/04 ,  C07D405/10 ,  C07D407/10 ,  C07D413/10 ,  C07D417/10 ,  Y02A50/465

摘要： Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.

摘要翻译： 公开了抑制PDE10的化合物，其可用于治疗各种病症，包括（但不限于）精神病性，焦虑症，运动障碍和/或神经障碍，例如帕金森病，亨廷顿氏病，阿尔茨海默病，脑炎，恐惧症 ，癫痫，失语症，贝尔麻痹，脑性麻痹，睡眠障碍，疼痛，图雷特综合征，精神分裂症，妄想症，药物诱发的精神病，恐慌和强迫症。 还提供了化合物的药学上可接受的盐，立体异构体，溶剂合物和前药。 还公开了含有与药学上可接受的载体组合的化合物的组合物，以及涉及其在需要其的温血动物中用于抑制PDE10的方法。