公开(公告)号：EP2427193A4

公开(公告)日：2013-04-03

申请号：EP10772372

申请日：2010-05-03

申请人： OMEROS CORP

发明人： BERGMANN JOHN E ,  CUTSHALL NEIL S ,  DEMOPULOS GREGORY A ,  FLORIO VINCENT A ,  GAITANARIS GEORGE ,  GRAY PATRICK ,  HOHMANN JOHN ,  ONRUST RENE ,  ZENG HONGKUI

IPC分类号： A61K31/50 ,  A61K31/137 ,  A61K31/195 ,  A61K31/38 ,  A61K31/415 ,  A61K31/425 ,  A61K31/433 ,  A61K31/519 ,  A61K31/527 ,  A61K45/06 ,  A61P25/14 ,  C07D471/04

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.

公开(公告)号：EP2544679A4

公开(公告)日：2014-05-14

申请号：EP11754087

申请日：2011-03-10

申请人： OMEROS CORP

发明人： CUTSHALL NEIL S ,  GAGE JENNIFER LYNN ,  WHEELER THOMAS NEIL ,  LITTLE THOMAS L

IPC分类号： A61K31/33

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

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：EP3137462A4

公开(公告)日：2017-12-27

申请号：EP15785376

申请日：2015-04-24

申请人： OMEROS CORP

发明人： CUTSHALL NEIL S ,  GAGE JENNIFER LYNN ,  LITTLE THOMAS L ,  LUKE WAYNE DOUGLAS ,  BROT ELISABETH C A ,  JONAS MARCO ,  MCDERMOTT MICHAEL JAMES ,  REINEKE KARL E

IPC分类号： C07D417/10

CPC分类号： C07D417/10 ,  C07D285/12 ,  C07D413/10 ,  C07F3/02

摘要： The present invention is directed to an improved process for the preparation of compounds of Formula (II) and Formula (III), which are useful in the inhibition of PDE10. In particular, the present invention is directed to an improved process for the preparation 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, which is useful in the inhibition of PDE10.

公开(公告)号：EP2139475A4

公开(公告)日：2012-03-07

申请号：EP08744515

申请日：2008-03-27

申请人： OMEROS CORP

发明人： BERGMANN JOHN E ,  CUTSHALL NEIL S ,  DEMOPULOS GREGORY A ,  FLORIO VINCENT A ,  GAITANARIS GEORGE ,  GRAY PATRICK ,  HOHMANN JOHN ,  ONRUST RENE ,  ZENG HONGKUI

IPC分类号： A61K31/435 ,  A61K31/195 ,  A61K31/433 ,  A61K31/519 ,  A61K31/527

CPC分类号： A61K31/195 ,  A61K31/433 ,  A61K31/519 ,  A61K31/527

公开(公告)号：EP3137461A4

公开(公告)日：2017-09-13

申请号：EP15785340

申请日：2015-04-24

申请人： OMEROS CORP

发明人： CUTSHALL NEIL S ,  FERGUSON KENNETH M ,  ZUTA CHARLES PRINCE

IPC分类号： C07D417/10 ,  A61K31/433 ,  A61P25/00

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.

摘要翻译： 本发明涉及1-（5-（4-氯-3,5-二甲氧基苯基）呋喃-2-基）-2-乙氧基-2-（4-（5-甲基-1,3 （S）-1-（5-（4-氯-3,5-二甲氧基苯基）呋喃-2-基）-2-乙氧基-2-（（4-噻二唑-2-基）苯基）乙酮， 4-（5-甲基-1,3,4-噻二唑-2-基）苯基）乙酮。 本发明还涉及（S）-1-（5-（4-氯-3,5-二甲氧基苯基）呋喃-2-基）-2-乙氧基-2-（4-（5-甲基 -1,3,4-噻二唑-2-基）苯基）乙酮，（S）-1-（5-（4-氯-3,5-二甲氧基苯基）呋喃-2-基）-2- （S）-1-（5-（4-氯-3,5-二甲基苯基）乙氧基）-2-乙氧基-2-（4-（5-甲基-1,3,4-噻二唑-2-基）苯基）乙酮的方法， 呋喃-2-基）-2-乙氧基-2-（4-（5-甲基-1,3,4-噻二唑-2-基）苯基）乙酮，和一种方法和特定的单独的中间体用于 （S）-1-（5-（4-氯-3,5-二甲氧基苯基）呋喃-2-基）-2-乙氧基-2-（4-（5-甲基-1,3,4- 噻二唑-2-基）苯基）乙酮。

公开(公告)号：EP2310016A4

公开(公告)日：2011-09-21

申请号：EP09805466

申请日：2009-08-04

申请人： OMEROS CORP

发明人： CUTSHALL NEIL S ,  GAGE JENNIFER LYNN ,  WHEELER NEIL THOMAS

IPC分类号： A61K31/54 ,  A61P25/00

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.