公开(公告)号：US20200079724A1

公开(公告)日：2020-03-12

申请号：US16685751

申请日：2019-11-15

申请人： Insmed Incorporated

发明人： Vladimir MALININ ,  Walter PERKINS ,  Franziska LEIFER ,  Donna KONICEK ,  Zhili LI ,  Adam PLAUNT

IPC分类号： C07C69/734 ,  A61M16/14 ,  A61M15/00 ,  A61K47/34 ,  A61K47/28 ,  A61K47/24 ,  A61K47/14 ,  A61K9/51 ,  A61K9/14 ,  A61K9/10 ,  A61K9/00 ,  A61P11/00 ,  A61P9/12 ,  A61K47/06 ,  A61K31/225 ,  A61K31/216 ,  A61K31/165 ,  C07C235/20 ,  C07C235/22 ,  C07C69/753 ,  C07C69/736 ,  A61K47/54 ,  A61K47/60 ,  C07C69/712

摘要： Prostacyclin compounds and compositions comprising the same are provided herein. Specifically, prostacyclin compounds comprising treprostinil covalently linked to a linear C5-C18 alkyl, branched C5-C18 alkyl, linear C2-C18 alkenyl, branched C3-C18 alkenyl, aryl, aryl-C1-C18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide) are described. The linkage, in one embodiment, is via a carbamate, amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. Methods for treating pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension are also provided.

公开(公告)号：US20180200186A1

公开(公告)日：2018-07-19

申请号：US15742812

申请日：2016-07-11

申请人： INSMED INCORPORATED

发明人： Kuan-Ju CHEN ,  Franziska LEIFER ,  Vladimir MALININ ,  Walter PERKINS ,  Jimin ZHANG ,  Keith DIPETRILLO

IPC分类号： A61K9/127 ,  A61K9/00 ,  A61P11/00 ,  A61K31/713

CPC分类号： A61K9/1272 ,  A61K9/0075 ,  A61K9/0078 ,  A61K9/008 ,  A61K31/713 ,  A61K47/24 ,  A61P11/00 ,  C12N15/88

摘要： Compositions comprising an RNA interference (RNAi) compound complexed to or encapsulated by lipid particles are provided. The lipid particle is a lipid nanoparticle, a liposome or a combination thereof. The lipid particle comprises a cationic lipid, a phospholipid, a sterol or a tocopherol or a derivative thereof, and a conjugated lipid. The invention also provides methods for treating pulmonary diseases or disorders such as pulmonary fibrosis and sarcoidosis using the compositions comprising the RNAi-lipid particles of the invention. The methods comprise administering one or more of the RNAi compositions to the lungs of the patient in need thereof via an inhalation delivery device, for example, a nebulizer, dry powder inhaler, or a metered dose inhaler.

公开(公告)号：US20220135513A1

公开(公告)日：2022-05-05

申请号：US17470723

申请日：2021-09-09

申请人： Insmed Incorporated

发明人： Vladimir MALININ ,  Walter PERKINS ,  Franziska LEIFER ,  Donna M. KONICEK ,  Zhili LI ,  Adam PLAUNT

IPC分类号： C07C231/02 ,  C07C67/08

摘要： Methods for making prodrugs of treprostinil and treprostinil derivatives are provided. Specifically, methods are provided herein for producing prostacyclin compounds comprising treprostinil covalently linked to a linear C5-C18 alkyl, branched C5-C18 alkyl, linear C2-C18 alkenyl, branched C3-C18 alkenyl, aryl, aryl-C1-C18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide). The linkage, in one embodiment, is via an amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. The compounds provided herein can be used to treat pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension.

公开(公告)号：US20240109834A1

公开(公告)日：2024-04-04

申请号：US18368410

申请日：2023-09-14

申请人： Insmed Incorporated

发明人： Vladimir MALININ ,  Walter PERKINS ,  Franziska LEIFER ,  Donna M. KONICEK ,  Zhili LI ,  Adam PLAUNT

IPC分类号： C07C69/734 ,  A61K9/00 ,  A61K9/10 ,  A61K9/14 ,  A61K9/51 ,  A61K31/165 ,  A61K31/216 ,  A61K31/225 ,  A61K47/06 ,  A61K47/14 ,  A61K47/24 ,  A61K47/28 ,  A61K47/34 ,  A61K47/54 ,  A61K47/60 ,  A61M15/00 ,  A61M16/14 ,  A61P9/12 ,  A61P11/00 ,  C07C69/712 ,  C07C69/736 ,  C07C69/753 ,  C07C235/20 ,  C07C235/22

CPC分类号： C07C69/734 ,  A61K9/0019 ,  A61K9/0043 ,  A61K9/0053 ,  A61K9/0073 ,  A61K9/0075 ,  A61K9/0078 ,  A61K9/10 ,  A61K9/14 ,  A61K9/51 ,  A61K31/165 ,  A61K31/216 ,  A61K31/225 ,  A61K47/06 ,  A61K47/14 ,  A61K47/24 ,  A61K47/28 ,  A61K47/34 ,  A61K47/543 ,  A61K47/544 ,  A61K47/60 ,  A61M15/0085 ,  A61M15/009 ,  A61M16/14 ,  A61P9/12 ,  A61P11/00 ,  C07C69/712 ,  C07C69/736 ,  C07C69/753 ,  C07C235/20 ,  C07C235/22 ,  A61M2202/064 ,  C07C2601/18 ,  C07C2603/14

摘要： Prostacyclin compounds and compositions comprising the same are provided herein. Specifically, prostacyclin compounds comprising treprostinil covalently linked to a linear C5-C18 alkyl, branched C5-C18 alkyl, linear C2-C18 alkenyl, branched C3-C18 alkenyl, aryl, aryl-C1-C18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide) are described. The linkage, in one embodiment, is via a carbamate, amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. Methods for treating pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension are also provided.

公开(公告)号：US20210276940A1

公开(公告)日：2021-09-09

申请号：US17186658

申请日：2021-02-26

申请人： Insmed Incorporated

发明人： Vladimir MALININ ,  Walter PERKINS ,  Franziska LEIFER ,  Donna KONICEK ,  Zhili LI ,  Adam PLAUNT

IPC分类号： C07C69/734 ,  C07C69/712 ,  A61K47/60 ,  A61K47/54 ,  C07C69/736 ,  C07C69/753 ,  C07C235/22 ,  C07C235/20 ,  A61K31/165 ,  A61K31/216 ,  A61K31/225 ,  A61K47/06 ,  A61K9/00 ,  A61P9/12 ,  A61P11/00 ,  A61K9/10 ,  A61K9/14 ,  A61K9/51 ,  A61K47/14 ,  A61K47/24 ,  A61K47/28 ,  A61K47/34 ,  A61M15/00 ,  A61M16/14

摘要： Prostacyclin compounds and compositions comprising the same are provided herein. Specifically, prostacyclin compounds comprising treprostinil covalently linked to a linear C5-C18 alkyl, branched C5-C18 alkyl, linear C2-C18 alkenyl, branched C3-C18 alkenyl, aryl, aryl-C1-C18 alkyl or an amino acid or a peptide (e.g., dipeptide, tripeptide, tetrapeptide) are described. The linkage, in one embodiment, is via a carbamate, amide or ester bond. Prostacyclin compounds provided herein can also include at least one hydrogen atom substituted with at least one deuterium atom. Methods for treating pulmonary hypertension (e.g., pulmonary arterial hypertension) and portopulmonary hypertension are also provided.