公开(公告)号：US20230338405A1

公开(公告)日：2023-10-26

申请号：US18142532

申请日：2023-05-02

申请人： Insmed Incorporated

发明人： Walter PERKINS ,  Vladimir MALININ ,  Xingong LI ,  Brian MILLER ,  Dominique SEIDEL ,  Philipp HOLZMANN ,  Harald SCHULZ ,  Michael HAHN

IPC分类号： A61K9/00 ,  A61K31/7036 ,  A61M11/00 ,  A61M11/02 ,  A61K9/127

CPC分类号： A61K31/7036 ,  A61K9/0078 ,  A61K9/127 ,  A61K9/1271 ,  A61M11/005 ,  A61M11/02

摘要： Provided herein are systems for treating a subject with a pulmonary infection, for example, a nontuberculous mycobacterial pulmonary infection, a Burkholderia pulmonary infection, a pulmonary infection associated with bronchiectasis, or a Pseudomonas pulmonary infection. The system includes a pharmaceutical formulation comprising a liposomal aminoglycoside dispersion, and the lipid component of the liposomes consist essentially of electrically neutral lipids. The system also includes a nebulizer which generates an aerosol of the pharmaceutical formulation at a rate greater than about 0.53 gram per minute. The aerosol is delivered to the subject via inhalation for the treatment of the pulmonary infection.

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：US20220133843A1

公开(公告)日：2022-05-05

申请号：US17344322

申请日：2021-06-10

申请人： Insmed Incorporated

发明人： Ryan HECKLER ,  Donna KONICEK ,  Adam PLAUNT ,  Vladimir MALININ ,  Walter PERKINS

IPC分类号： A61K38/14 ,  A61P31/04 ,  A61K9/00

摘要： The present invention provides certain lipo-glycopeptide cleavable derivatives and methods for using the same for the treatment of bacterial infections, for example, pulmonary bacterial infections. The LGPC derivatives include a cleavable moiety that in certain embodiments, is designed to allow for cellular uptake and/or a more rapid clearance of the glycopeptide metabolite (i.e., the cleaved glycopeptide) from the site of administration (e.g., the lung) as compared to the uncleaved LGPC.

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：US20230250051A1

公开(公告)日：2023-08-10

申请号：US18302682

申请日：2023-04-18

申请人： Insmed Incorporated

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

IPC分类号： C07C231/02 ,  C07C67/08

CPC分类号： C07C231/02 ,  C07C67/08 ,  C07C2602/24 ,  C07C2601/18

摘要： Methods for making prodrugs of trepreostinil 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-C18alkenyl, branched C3-C18alkenyl, 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：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.

公开(公告)号：US20200368312A1

公开(公告)日：2020-11-26

申请号：US16615232

申请日：2018-05-22

申请人： Insmed Incorporated

发明人： Ryan HECKLER ,  Donna KONICEK ,  Adam PLAUNT ,  Vladimir MALININ ,  Walter PERKINS

IPC分类号： A61K38/14 ,  A61K9/00 ,  A61P31/04

摘要： Provided herein are methods and compositions for the treatment of Gram positive bacterial infections. The infection in some embodiments, is a pulmonary infection. The method for treating the bacterial infection, comprises in one embodiment, administering to a patient in need thereof, a composition comprising an effective amount of a compound a glycopeptide derivative of Formula (I) or (II), or a pharmaceutically acceptable salt of Formula (I) or (II).

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：US20210369752A1

公开(公告)日：2021-12-02

申请号：US17175317

申请日：2021-02-12

申请人： INSMED INCORPORATED

发明人： Walter PERKINS ,  Vladimir MALININ ,  Xingong LI ,  Brian MILLER ,  Dominique SEIDEL ,  Philipp HOLZMANN ,  Harald SCHULZ ,  Michael HAHN

IPC分类号： A61K31/7036 ,  A61K9/127 ,  A61K9/00 ,  A61M11/00 ,  A61M11/02

摘要： Provided herein are systems for treating a subject with a pulmonary infection, for example, a nontuberculous mycobacterial pulmonary infection, a Burkholderia pulmonary infection, a pulmonary infection associated with bronchiectasis, or a Pseudomonas pulmonary infection. The system includes a pharmaceutical formulation comprising a liposomal aminoglycoside dispersion, and the lipid component of the liposomes consist essentially of electrically neutral lipids. The system also includes a nebulizer which generates an aerosol of the pharmaceutical formulation at a rate greater than about 0.53 gram per minute. The aerosol is delivered to the subject via inhalation for the treatment of the pulmonary infection.