公开(公告)号：US20170320813A1

公开(公告)日：2017-11-09

申请号：US15527811

申请日：2015-11-18

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 ,  C07C2601/18 ,  C07C2602/24

CPC分类号： C07C231/02 ,  C07C67/08 ,  C07C2601/18 ,  C07C2602/24 ,  C07C235/06 ,  C07C235/12 ,  C07C235/14 ,  C07C69/712

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-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：US20180155359A9

公开(公告)日：2018-06-07

申请号：US15676726

申请日：2017-08-14

申请人： Aquinox Pharmaceuticals (Canada) Inc.

发明人： Lloyd F. Mackenzie ,  Thomas B. MacRury ,  Curtis Harwig ,  David Bogucki ,  Jeffery R. Raymond ,  Jeremy D. Pettigrew

IPC分类号： C07D493/10 ,  C07D333/20 ,  C07D307/52 ,  C07C35/21 ,  C07D307/42 ,  C07D277/64 ,  C07D277/28 ,  C07D261/20 ,  C07D231/56 ,  C07D231/54 ,  C07D221/16 ,  C07D215/227 ,  C07D213/82 ,  C07D213/75 ,  C07D213/38 ,  C07D211/58 ,  C07C335/10 ,  C07C275/22 ,  C07C255/30 ,  C07C233/23 ,  C07C215/38 ,  C07C35/23 ,  C07C2602/24 ,  C07C2601/14

CPC分类号： C07D493/10 ,  A61K31/416 ,  C07C35/21 ,  C07C35/23 ,  C07C215/26 ,  C07C215/38 ,  C07C233/23 ,  C07C255/30 ,  C07C275/22 ,  C07C335/10 ,  C07C2601/14 ,  C07C2602/24 ,  C07D211/58 ,  C07D213/30 ,  C07D213/38 ,  C07D213/75 ,  C07D213/82 ,  C07D215/227 ,  C07D221/16 ,  C07D221/18 ,  C07D231/54 ,  C07D231/56 ,  C07D261/20 ,  C07D277/24 ,  C07D277/28 ,  C07D277/64 ,  C07D307/42 ,  C07D307/52 ,  C07D333/16 ,  C07D333/20

摘要： Compounds of formula (II): wherein R1, R2, R5 and R13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

公开(公告)号：US20170369436A1

公开(公告)日：2017-12-28

申请号：US15537391

申请日：2015-12-18

申请人： NUCELIS LLC

发明人： Laszlo TREIBER

IPC分类号： C07C401/00 ,  A23L33/155 ,  C07J9/00 ,  C07C2602/24 ,  C07C2601/14

CPC分类号： C07C401/00 ,  A23L33/155 ,  A23V2250/7104 ,  A23V2250/7106 ,  C07C2601/14 ,  C07C2602/24 ,  C07J9/00

摘要： It is an object of the present invention to provide methods for producing vitamin D that gives improved yields and reduced side product contamination. In various aspects, these methods provide for production of vitamin-D2 using ergosterol as provitamin D2 or a dihydroxy derivative thereof as a starting material, or production of vitamin-D3 using 7-dehydrocholesterol as provitamin D3 or a dihydroxy derivative thereof as the starting material. The methods described herein comprise irradiating the starting material in a solution including an organic or inorganic base with light in the wavelength range 245-360 nanometers (nm) to obtain a product containing pre-vitamin-D2 or pre-vitamin-D3, and heating the product to convert the resulting pre-vitamin-D2 or pre-vitamin-D3 to vitamin D2 or vitamin D3. In various embodiments, these methods further comprise recovering vitamin D2 or vitamin D3 from this reaction as a purified product.

公开(公告)号：US20170362250A1

公开(公告)日：2017-12-21

申请号：US15676726

申请日：2017-08-14

申请人： Aquinox Pharmaceuticals (Canada) Inc.

发明人： Lloyd F. Mackenzie ,  Thomas B. MacRury ,  Curtis Harwig ,  David Bogucki ,  Jeffery R. Raymond ,  Jeremy D. Pettigrew

IPC分类号： C07D493/10 ,  C07D307/52 ,  C07C35/21 ,  C07D307/42 ,  C07D277/64 ,  C07D277/28 ,  C07D261/20 ,  C07D231/56 ,  C07D231/54 ,  C07D221/16 ,  C07D215/227 ,  C07D213/82 ,  C07D213/75 ,  C07D213/38 ,  C07D211/58 ,  C07C335/10 ,  C07C275/22 ,  C07C255/30 ,  C07C233/23 ,  C07C215/38 ,  C07C35/23 ,  C07D333/20 ,  C07C2602/24 ,  C07C2601/14

CPC分类号： C07D493/10 ,  A61K31/416 ,  C07C35/21 ,  C07C35/23 ,  C07C215/26 ,  C07C215/38 ,  C07C233/23 ,  C07C255/30 ,  C07C275/22 ,  C07C335/10 ,  C07C2601/14 ,  C07C2602/24 ,  C07D211/58 ,  C07D213/30 ,  C07D213/38 ,  C07D213/75 ,  C07D213/82 ,  C07D215/227 ,  C07D221/16 ,  C07D221/18 ,  C07D231/54 ,  C07D231/56 ,  C07D261/20 ,  C07D277/24 ,  C07D277/28 ,  C07D277/64 ,  C07D307/42 ,  C07D307/52 ,  C07D333/16 ,  C07D333/20

摘要： Compounds of formula (II): wherein R1, R2, R5 and R13 are described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.