公开(公告)号：US20180110864A1

公开(公告)日：2018-04-26

申请号：US15842684

申请日：2017-12-14

申请人： Graybug Vision, Inc.

发明人： Jeffrey R. Cleland ,  Ming Yang ,  John G. Bauman ,  Nu Hoang ,  Emmett Cunningham

IPC分类号： C07D513/04 ,  C07D495/04 ,  C07D403/06 ,  C07C69/73

CPC分类号： A61K47/59 ,  A61K47/54 ,  A61K47/542 ,  A61K47/543 ,  A61K47/55 ,  A61K47/593 ,  A61K47/60 ,  C07C69/73 ,  C07C2601/08 ,  C07D403/06 ,  C07D495/04 ,  C07D513/04 ,  H05K999/99

摘要： The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.

公开(公告)号：US20180064823A1

公开(公告)日：2018-03-08

申请号：US15782749

申请日：2017-10-12

申请人： Graybug Vision, Inc.

发明人： Jeffrey L. Cleland ,  Ming Yang ,  John G. Bauman ,  Nu Hoang ,  Emmett Cunningham

IPC分类号： C07D513/04 ,  C07D495/04 ,  C07D403/06 ,  C07C69/73

CPC分类号： A61K47/54 ,  A61K47/542 ,  A61K47/543 ,  A61K47/55 ,  A61K47/59 ,  A61K47/593 ,  A61K47/60 ,  C07C69/73 ,  C07C2601/08 ,  C07D403/06 ,  C07D495/04 ,  C07D513/04 ,  H05K999/99

摘要： The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.

公开(公告)号：US11548861B2

公开(公告)日：2023-01-10

申请号：US16578003

申请日：2019-09-20

申请人： Graybug Vision, Inc.

发明人： Ming Yang ,  John G. Bauman ,  Jeffrey L. Cleland ,  Nu Hoang ,  Emmett Cunningham

IPC分类号： C07D271/04 ,  C07D231/12 ,  C07D403/06 ,  C07D403/12 ,  C07D417/04 ,  C07D417/14 ,  C07D487/04 ,  C07D495/04 ,  C07D513/04

摘要： The present invention provides new prodrugs of therapeutically active compounds, including oligomeric prodrugs, and compositions to treat medical disorders, for example glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.

公开(公告)号：US10111964B2

公开(公告)日：2018-10-30

申请号：US15842712

申请日：2017-12-14

申请人： Graybug Vision, Inc.

发明人： Jeffrey L. Cleland ,  Ming Yang ,  John G. Bauman ,  Nu Hoang ,  Emmett Cunningham

IPC分类号： A61K47/60 ,  A61K47/54 ,  A61K47/48 ,  C07D495/04 ,  C07D513/04 ,  C07C69/73 ,  C07D403/06 ,  A61K47/55 ,  A61K47/59

摘要： The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.

公开(公告)号：US09956302B2

公开(公告)日：2018-05-01

申请号：US15782755

申请日：2017-10-12

申请人： Graybug Vision, Inc.

发明人： Jeffrey L. Cleland ,  Ming Yang ,  John G. Bauman ,  Nu Hoang ,  Emmett Cunningham

IPC分类号： C07D403/06 ,  A61K47/54 ,  A61K47/59 ,  A61K47/55 ,  A61K47/60 ,  C07D513/04 ,  C07D495/04 ,  C07C69/73

CPC分类号： A61K47/54 ,  A61K47/542 ,  A61K47/543 ,  A61K47/55 ,  A61K47/59 ,  A61K47/593 ,  A61K47/60 ,  C07C69/73 ,  C07C2601/08 ,  C07D403/06 ,  C07D495/04 ,  C07D513/04

摘要： The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.

公开(公告)号：US20190060474A1

公开(公告)日：2019-02-28

申请号：US16162158

申请日：2018-10-16

申请人： Graybug Vision, Inc.

发明人： Jeffrey L. Cleland ,  Ming Yang ,  John G. Bauman ,  Nu Hoang ,  Emmett Cunningham

IPC分类号： A61K47/59 ,  C07D513/04 ,  C07D495/04 ,  C07D403/06 ,  C07C69/73 ,  A61K47/60 ,  A61K47/54 ,  A61K47/55

摘要： The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.

公开(公告)号：US10159747B2

公开(公告)日：2018-12-25

申请号：US15842684

申请日：2017-12-14

申请人： Graybug Vision, Inc.

发明人： Jeffrey L. Cleland ,  Ming Yang ,  John G. Bauman ,  Nu Hoang ,  Emmett Cunningham

IPC分类号： C07D513/04 ,  A61K47/54 ,  C07D495/04 ,  C07C69/73 ,  C07D403/06 ,  A61K47/60 ,  A61K47/55 ,  A61K47/59

摘要： The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.

公开(公告)号：US10098965B2

公开(公告)日：2018-10-16

申请号：US15782744

申请日：2017-10-12

申请人： Graybug Vision,Inc.

发明人： Jeffrey L. Cleland ,  Ming Yang ,  John G. Bauman ,  Nu Hoang ,  Emmett Cunningham

IPC分类号： C07D403/06 ,  A61K47/54 ,  A61K47/59 ,  A61K47/55 ,  C07D513/04 ,  C07D495/04 ,  C07C69/73 ,  A61K47/60

摘要： The disclosure describes prodrugs and derivatives of prostaglandins, carbonic anhydrase inhibitors, kinase inhibitors, beta-adrenergic receptor antagonists and other drugs, as well as controlled delivery formulations containing such prodrugs and derivatives, for the treatment of ocular disorders.

公开(公告)号：US20210040111A1

公开(公告)日：2021-02-11

申请号：US17077853

申请日：2020-10-22

申请人： Graybug Vision, Inc.

发明人： Ming Yang ,  John G. Bauman ,  Jinzhong Zhang ,  Nu Hoang ,  Jeffrey L. Cleland

IPC分类号： C07D495/04 ,  A61K9/00 ,  C07D307/52 ,  C07C311/16 ,  C07D207/06 ,  C07D417/04 ,  C07D417/14

摘要： The present invention provides new prodrugs of therapeutically active loop diuretics, including oligomeric prodrugs, and compositions to treat medical disorders, for example, ocular disorders such as glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.

公开(公告)号：US20200308162A1

公开(公告)日：2020-10-01

申请号：US16899422

申请日：2020-06-11

申请人： Graybug Vision, Inc.

发明人： Jeffrey L. Cleland ,  Ming Yang ,  John G. Bauman ,  Nu Hoang ,  Jane Chisholm

IPC分类号： C07D417/04

摘要： New prodrugs of therapeutically active compounds, including oligomeric prodrugs of ethacrynic acid, and compositions to treat medical disorders, for example glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy. Also a method for the controlled administration of timolol to a patient in need thereof, such as a human, comprising administering a prodrug of timolol in a microparticle in vivo, wherein the timolol prodrug containing microparticle exhibits in vitro drug release kinetics in an aqueous solution at a pH between 6-8 at body temperature of a substantially consistent release of at least 60% timolol itself by molar ratio to the prodrug of timolol or an intermediate metabolite thereof over at least 100 days.