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1. 发明申请

US20160137646A1 Novel Compounds and Uses Thereof 有权
标题翻译：新型化合物及其用途
公开(公告)号：US20160137646A1
公开(公告)日：2016-05-19
申请号：US14894214
申请日：2014-05-30
申请人： Ben C. ASKEW , Andrew GOOD , Kala Pharmaceuticals, Inc.
发明人： Winston Zapanta Ong , Pawel Wojciech Nowak , Ben C. Askew , Andrew Good
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention provides novel compounds of any one of Formulae (I)-(IV), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of any one of Formulae (I)-(IV) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor signaling pathway (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
摘要翻译：本发明提供式（I） - （IV）中任一项的新化合物及其药物组合物。还提供了包含粘液穿透的式（I） - （IV）中任一项的化合物及其药物组合物的颗粒（例如纳米颗粒）。本发明还提供了用于使用本发明化合物及其药物组合物用于治疗和/或预防与生长因子信号传导途径的异常或病理性血管生成和/或异常信号传导相关的疾病的方法和试剂盒（例如，血管内皮生长因子 VEGF）），例如增殖性疾病（例如癌症，良性肿瘤，炎症性疾病，自身免疫性疾病）和眼部疾病（例如，黄斑变性，青光眼，糖尿病性视网膜病变，视网膜母细胞瘤，水肿，葡萄膜炎，干眼症，睑炎炎，手术炎症）。

2. 发明授权

US11352343B2 Urea derivatives and uses thereof 有权
公开(公告)号：US11352343B2
公开(公告)日：2022-06-07
申请号：US16900657
申请日：2020-06-12
申请人： Kala Pharmaceuticals, Inc.
发明人： Winston Zapanta Ong , Pawel Wojciech Nowak , John Thomas Feutrill , Jinsoo Kim
IPC分类号： C07D413/14 , A61P35/00 , C07D403/10 , A61K9/00 , A61K9/14 , C07D471/04 , C07D231/56 , C07D401/04 , C07D403/04 , A61K31/416
摘要： The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.

3. 发明申请

US20210355136A1 CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF 有权
公开(公告)号：US20210355136A1
公开(公告)日：2021-11-18
申请号：US17389000
申请日：2021-07-29
申请人： Kala Pharmaceuticals, Inc.
发明人： Minh Ngoc Nguyen , Winston Zapanta Ong
IPC分类号： C07D491/107
摘要： Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.

4. 发明授权

US11104685B2 Crystalline forms of therapeutic compounds and uses thereof 有权
公开(公告)号：US11104685B2
公开(公告)日：2021-08-31
申请号：US16818033
申请日：2020-03-13
申请人： Kala Pharmaceuticals, Inc.
发明人： Minh Ngoc Nguyen , Winston Zapanta Ong
IPC分类号： C07D491/107
摘要： Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.

5. 发明申请

US20210261562A1 CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF 有权
公开(公告)号：US20210261562A1
公开(公告)日：2021-08-26
申请号：US17315080
申请日：2021-05-07
申请人： Kala Pharmaceuticals, Inc.
发明人： Minh Ngoc Nguyen , Winston Zapanta Ong
IPC分类号： C07D491/107 , A61K31/517
摘要： Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.

6. 发明申请

US20200010470A1 MEROPENEM DERIVATIVES AND USES THEREOF 审中-公开
公开(公告)号：US20200010470A1
公开(公告)日：2020-01-09
申请号：US16509388
申请日：2019-07-11
申请人： Kala Pharmaceuticals, Inc.
发明人： Winston Zapanta Ong , Pawel Wojciech Nowak , Jinsoo Kim , Elizabeth M. Enlow , James Bourassa , Yen Cu , Alexey Popov , Hongming Chen
IPC分类号： C07D477/20 , A61K9/50 , A61K9/51 , C07D487/04 , A61K45/06 , A61K31/407
摘要： The present invention provides novel derivative of β-lactam antibiotics, such as meropenem. The inventive compounds include compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are particles (e.g., nanoparticles) and pharmaceutical compositions thereof that are mucus penetrating. The inventive particles and pharmaceutical compositions may be useful in delivering an inventive compound to the respiratory tract of a subject. The invention further provides methods of using and kits including the inventive compounds, particles thereof, and/or pharmaceutical compositions thereof for treating and/or preventing a pulmonary disease (e.g., a respiratory tract infection).

7. 发明申请

US20180327389A1 UREA DERIVATIVES AND USES THEREOF 审中-公开
公开(公告)号：US20180327389A1
公开(公告)日：2018-11-15
申请号：US16043000
申请日：2018-07-23
申请人： Kala Pharmaceuticals, Inc.
发明人： Winston Zapanta Ong , Pawel Wojciech Nowak , John Thomas Feutrill , Jinsoo Kim
IPC分类号： C07D403/10 , C07D403/04 , C07D401/04 , A61K9/14 , C07D471/04 , A61K9/00 , C07D231/56 , A61K31/416
CPC分类号： C07D403/10 , A61K9/0048 , A61K9/146 , A61K31/416 , C07D231/56 , C07D401/04 , C07D403/04 , C07D471/04
摘要： The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.

8. 发明申请

US20180065977A1 CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF 审中-公开
公开(公告)号：US20180065977A1
公开(公告)日：2018-03-08
申请号：US15694252
申请日：2017-09-01
申请人： Kala Pharmaceuticals, Inc.
发明人： Minh Ngoc Nguyen , Winston Zapanta Ong
IPC分类号： C07D491/107
CPC分类号： C07D491/107 , C07B2200/13
摘要： Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.

9. 发明申请

US20150072986A1 UREA DERIVATIVES AND USES THEREOF 有权
标题翻译：尿素衍生物及其用途
公开(公告)号：US20150072986A1
公开(公告)日：2015-03-12
申请号：US14301653
申请日：2014-06-11
申请人： Kala Pharmaceuticals, Inc.
发明人： Winston Zapanta Ong , Pawel Wojciech Nowak , John Thomas Feutrill , Jinsoo Kim , Minh Ngoc Nguyen , Elizabeth Enlow
IPC分类号： C07D231/56 , C07D401/04 , C07D403/04 , C07D471/04
CPC分类号： C07D403/10 , A61K9/0048 , A61K9/146 , A61K31/416 , C07D231/56 , C07D401/04 , C07D403/04 , C07D471/04
摘要： The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.
摘要翻译：本发明提供式（I） - （III）中任一项的新化合物及其药物组合物。还提供包含粘液穿透的式（I） - （III）化合物及其药物组合物的颗粒（例如纳米颗粒）。本发明还提供了用于使用本发明化合物及其药物组合物用于治疗和/或预防与生长因子（例如血管内皮生长因子（VEGF））的异常或病理性血管生成和/或异常信号传导相关的疾病的方法和试剂盒，），例如增殖性疾病（例如癌症，良性肿瘤，炎性疾病，自身免疫性疾病）和眼部疾病（例如黄斑变性，青光眼，糖尿病性视网膜病变，视网膜母细胞瘤，水肿，葡萄膜炎，干眼症，睑炎炎和手术后炎症）在有需要的受试者中。

10. 发明授权

US11091487B2 Meropenem derivatives and uses thereof 有权
公开(公告)号：US11091487B2
公开(公告)日：2021-08-17
申请号：US16509388
申请日：2019-07-11
申请人： Kala Pharmaceuticals, Inc.
发明人： Winston Zapanta Ong , Pawel Wojciech Nowak , Jinsoo Kim , Elizabeth M. Enlow , James Bourassa , Yen Cu , Alexey Popov , Hongming Chen
IPC分类号： C07D477/20 , A61K31/407 , A61K9/50 , A61K9/51 , C07D487/04 , A61K45/06
摘要： The present invention provides novel derivative of β-lactam antibiotics, such as meropenem. The inventive compounds include compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are particles (e.g., nanoparticles) and pharmaceutical compositions thereof that are mucus penetrating. The inventive particles and pharmaceutical compositions may be useful in delivering an inventive compound to the respiratory tract of a subject. The invention further provides methods of using and kits including the inventive compounds, particles thereof, and/or pharmaceutical compositions thereof for treating and/or preventing a pulmonary disease (e.g., a respiratory tract infection).

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