公开(公告)号：WO2017053638A8

公开(公告)日：2017-03-30

申请号：PCT/US2016/053210

申请日：2016-09-22

Applicant: GRAYBUG VISION, INC.

Inventor： CLELAND, Jeffrey, L. ,  YANG, Ming ,  BAUMAN, John ,  HOANG, Nu ,  CUNNINGHAM, Emmett

IPC: A61K31/20 ,  A61K47/34

Abstract: 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：WO2020102758A1

公开(公告)日：2020-05-22

申请号：PCT/US2019/061859

申请日：2019-11-15

Applicant: GRAYBUG VISION, INC.

Inventor： YANG, Ming ,  SALAIN, Daniel, Louis ,  SEMBA, Charles, Pauling ,  YU, Yun ,  YU, Weiling ,  KAYS, Joshua ,  CHISHOLM, Jane ,  LU, Qingyun ,  CLELAND, Jeffrey, L.

IPC: A61K9/16 ,  A61K9/00 ,  A61K47/00

Abstract: Compositions and methods are provided that include aggregating microparticles which include an active agent that exhibit an increased hardness and/or durability of the resulting aggregated microparticles in vivo, which can lead to more stable, long-term ocular therapy.

公开(公告)号：WO2020069353A1

公开(公告)日：2020-04-02

申请号：PCT/US2019/053513

申请日：2019-09-27

Applicant: GRAYBUG VISION, INC.

Inventor： BAUMAN, John, G. ,  YANG, Ming ,  HOANG, Nu ,  CUNNINGGHAM, Emmett ,  CLELAND, Jeffrey, L.

IPC: A61K31/165 ,  C07D209/04 ,  C07D209/08

Abstract: The present invention provides new prodrags of Sunitinib, Brinzolamide, and Dorzolamide and compositions to treat medical disorders, for example glaucoma, a disorder or abnormality related to an increase in intraocular pressure (TOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.

公开(公告)号：WO2019210215A1

公开(公告)日：2019-10-31

申请号：PCT/US2019/029416

申请日：2019-04-26

Applicant: GRAYBUG VISION, INC.

Inventor： YANG, Ming ,  BAUMAN, John, G. ,  ZHANG, Jinzhong ,  HOANG, Nu ,  CLELAND, Jeffrey, L.

IPC: A61K31/196 ,  A61K31/341 ,  C07C311/38 ,  C07C311/39 ,  C07D307/38

Abstract: 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：WO2018175922A1

公开(公告)日：2018-09-27

申请号：PCT/US2018/024080

申请日：2018-03-23

Applicant: GRAYBUG VISION, INC.

Inventor： CLELAND, Jeffrey, L. ,  YANG, Ming ,  BAUMAN, John, G. ,  HOANG, Nu ,  CUNNINGHAM, Emmett

IPC: A61K31/498 ,  C07D241/44 ,  A61P27/02

Abstract: 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：WO2019209883A1

公开(公告)日：2019-10-31

申请号：PCT/US2019/028803

申请日：2019-04-23

Applicant: GRAYBUG VISION, INC.

Inventor： SARAGNESE, Daniel ,  YANG, Ming ,  YU, Yun ,  GUIRIBA, Toni-Rose ,  MCKENZIE, David

IPC: C08F6/14

Abstract: The present invention is in the field of manufacturing drug-loaded microparticles, and specifically provides processes for producing approximately homogenously sized drug loaded microparticles with high drug loading and reproducible drug release profiles, and which may be provided in a significantly reduced time period.

公开(公告)号：WO2017083779A1

公开(公告)日：2017-05-18

申请号：PCT/US2016/061706

申请日：2016-11-11

Applicant: GRAYBUG VISION, INC.

Inventor： YU, Yun ,  KAYS, Joshua ,  YANG, Ming ,  CLELAND, Jeffrey, L.

IPC: A61K47/50 ,  A61K9/14 ,  A61K9/50

CPC classification number: A61K9/5089 ,  A61K9/0019 ,  A61K9/0048 ,  A61K9/1641 ,  A61K9/1647 ,  A61K9/5026 ,  A61K9/5031 ,  A61K31/404 ,  A61K47/10 ,  A61K47/26 ,  A61K47/36

Abstract: The present invention is a surface treated drug-loaded solid (e.g., non-porous) microparticle that aggregates in vivo to form a consolidated larger particle for medical therapy. In one embodiment, the particles are used for ocular therapy. Processes for producing the surface treated microparticle and injectable formulations which include the surface treated microparticle are also provided. When used in the eye, long-term consistent intraocular delivery can be achieved without disrupting vision and minimizing undesirable inflammatory responses.

Abstract translation: 本发明是载体表面处理的载药固体（例如无孔）微粒，其在体内聚集形成用于药物治疗的固结的较大颗粒。 在一个实施例中，颗粒用于眼部治疗。 还提供了生产经表面处理的微粒的方法和包含经表面处理的微粒的可注射制剂。 当用于眼睛时，可以实现长期一致的眼内给药，而不会中断视力并将不希望的炎症反应降至最低。

公开(公告)号：WO2017053638A1

公开(公告)日：2017-03-30

申请号：PCT/US2016/053210

申请日：2016-09-22

Applicant: GRAYBUG VISION, INC.

Inventor： CLELAND, Jeffrey, L. ,  YANG, Ming ,  BAUMAN, John ,  HOANG, Nu ,  CUNNINGHAM, Emmett

IPC: A61K31/20 ,  A61K47/34

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

Abstract: 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.

Abstract translation: 本公开描述了前列腺素的前药和衍生物，碳酸酐酶抑制剂，激酶抑制剂，β-肾上腺素能受体拮抗剂和其它药物，以及含有这些前药和衍生物的受控递送制剂，用于治疗眼部疾病。

公开(公告)号：WO2021237096A1

公开(公告)日：2021-11-25

申请号：PCT/US2021/033662

申请日：2021-05-21

Applicant: GRAYBUG VISION, INC.

Inventor： YANG, Ming ,  YU, Yun ,  HOANG, Nu

IPC: A61K31/5377 ,  A61K9/00

Abstract: A biodegradable implant or microparticles of a timolol prodrug, optionally with timolol or a pharmaceutically acceptable salt thereof, typically for ocular therapy.

公开(公告)号：WO2019118924A1

公开(公告)日：2019-06-20

申请号：PCT/US2018/065843

申请日：2018-12-14

Applicant: GRAYBUG VISION, INC.

Inventor： CLELAND, Jeffrey L. ,  YANG, Ming ,  BAUMAN, John, G. ,  HOANG, Nu ,  CHISHOLM, Jane

IPC: A61K31/225 ,  C07C69/738

Abstract: 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.