公开(公告)号：US20240197685A1

公开(公告)日：2024-06-20

申请号：US18283484

申请日：2022-03-23

申请人： Vicore Pharma AB

发明人： Tomas Fex ,  Bengt Ohlsson ,  Anders Hallberg ,  Mats Larhed

IPC分类号： A61K31/4178 ,  A61K31/4439 ,  C07D409/10 ,  C07D409/14

CPC分类号： A61K31/4178 ,  A61K31/4439 ,  C07D409/10 ,  C07D409/14

摘要： There is provided pharmaceutical compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, Y1, Y2, Y3 and Y4 have meanings given in the description, which compounds are useful in the treatment of autoimmune and/or fibrotic diseases, including interstitial lung diseases, such as idiopathic pulmonary fibrosis and sarcoidosis.

公开(公告)号：US11844868B2

公开(公告)日：2023-12-19

申请号：US17696984

申请日：2022-03-17

申请人： VICORE PHARMA AB

发明人： Ola Camber ,  Arnout Everaert ,  Stefan Grudén

IPC分类号： A61K9/48 ,  A61K9/00 ,  C07D403/08

CPC分类号： A61K9/4808 ,  A61K9/0053 ,  A61K9/485 ,  A61K9/4816 ,  A61K9/4858 ,  A61K9/4866 ,  C07D403/08

摘要： There is provided a pharmaceutical dosage form that is suitable for peroral administration to the gastrointestinal tract, which dosage form comprises a pharmaceutical composition in the form of a particulate mixture comprising solid particles of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide (C21), or a pharmaceutically-acceptable salt thereof, admixed with a blend of carrier particles with weight- and/or a volume-based mean diameter, and/or a structural/particle density, that is/are similar to the weight- and/or volume-based mean diameter, and/or the structural/particle density, of the solid particles of C21, and a glidant, which composition is contained within a capsule that is suitable for such peroral administration. Preferred carrier particles have a weight- and/or a volume-based mean diameter that is less than about 100 μm. Preferred carrier particle materials include mannitol. Preferred glidants comprise colloidal silica. Such dosage forms find utility in the treatment of lung diseases, such as idiopathic pulmonary fibrosis, sarcoidosis and respiratory virus-induced tissue damage.

公开(公告)号：US20230149362A1

公开(公告)日：2023-05-18

申请号：US17920558

申请日：2021-04-23

申请人： Vicore Pharma AB

发明人： Ola Camber ,  Stefan Gruden

IPC分类号： A61K31/4178 ,  A61K9/48

CPC分类号： A61K31/4178 ,  A61K9/4858 ,  A61K9/4825 ,  A61K9/4833 ,  A61K9/0053

摘要： According to the invention there is provided a pharmaceutical dosage form that is suitable for peroral administration to the gastrointestinal tract, which dosage form comprises a pharmaceutical composition in the form of a heterogeneous mixture comprising solid particles of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide (C21), or a pharmaceutically-acceptable salt thereof, suspended in a pharmaceutically-acceptable, hydrophobic, lipid-based carrier in which C21 or salt thereof is essentially insoluble, which composition is contained within a capsule that is suitable for such peroral administration. Preferred carriers include triglycerides. Such dosage forms find utility in the treatment of lung diseases, such as idiopathic pulmonary fibrosis, sarcoidosis and respiratory virus-induced tissue damage.

公开(公告)号：US20220233480A1

公开(公告)日：2022-07-28

申请号：US17580440

申请日：2022-01-20

申请人： VICORE PHARMA AB

发明人： Carl-Johan DALSGAARD ,  Johan RAUD ,  Rohit BATTA

IPC分类号： A61K31/18 ,  A61P31/14

摘要： There is provided N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-isobutylthiophene-2-sulfonamide, or a pharmaceutically-acceptable salt thereof, for use in a method of treatment of respiratory virus-induced tissue damage. Such damage may be caused by coronaviruses, including severe acute respiratory syndrome coronavirus and severe acute respiratory syndrome coronavirus. N-Butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide alleviates symptoms of diseases caused by those viruses (including coronavirus disease 2019 or COVID-19), such as cough, dyspnea, pneumonia, respiratory distress, respiratory failure and/or fibrosis of organs such as the lungs, the heart or the kidneys, and may thus prevent respiratory virus-induced morbidity and/or mortality. In particular, it has been found in a clinical study that the proportion of patients with COVID-19 needing oxygen treatment was significantly lower for patients that were administered N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide compared to placebo.

公开(公告)号：US20220202729A1

公开(公告)日：2022-06-30

申请号：US17696997

申请日：2022-03-17

申请人： VICORE PHARMA AB

发明人： Ola CAMBER ,  Christina JOHANSSON

IPC分类号： A61K9/48 ,  A61K31/4178 ,  A61K9/00

摘要： According to the invention there is provided a pharmaceutical composition comprising N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide (C21), or a pharmaceutically-acceptable salt thereof, in which composition the C21 or salt thereof is protected by the presence of a coating comprising an enteric substance. Preferred dosage forms comprise capsules in which C21 or salt thereof is presented in the form of a dry powder mixture or a suspension of particles of C21 in a solvent in which it is insoluble. Such dosage forms find utility in the treatment of lung diseases, such as idiopathic pulmonary fibrosis, sarcoidosis and respiratory virus-induced tissue damage.

公开(公告)号：US12121614B2

公开(公告)日：2024-10-22

申请号：US18300739

申请日：2023-04-14

申请人： VICORE PHARMA AB

发明人： Ola Camber ,  Christina Johansson

IPC分类号： A61K9/28 ,  A61K9/00 ,  A61K9/48 ,  A61K31/4178

CPC分类号： A61K9/4866 ,  A61K9/0056 ,  A61K9/4808 ,  A61K9/4825 ,  A61K31/4178

摘要： According to the invention there is provided a pharmaceutical composition comprising N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide (C21), or a pharmaceutically-acceptable salt thereof, in which composition the C21 or salt thereof is protected by the presence of a coating comprising an enteric substance. Preferred dosage forms comprise capsules in which C21 or salt thereof is presented in the form of a dry powder mixture or a suspension of particles of C21 in a solvent in which it is insoluble. Such dosage forms find utility in the treatment of lung diseases, such as idiopathic pulmonary fibrosis, sarcoidosis and respiratory virus-induced tissue damage.

公开(公告)号：US20240122902A1

公开(公告)日：2024-04-18

申请号：US18391451

申请日：2023-12-20

申请人： VICORE PHARMA AB

发明人： Carl-Johan DALSGAARD ,  Rohit BATTA

IPC分类号： A61K31/4178 ,  A61K9/48 ,  A61P1/00 ,  A61P11/00

CPC分类号： A61K31/4178 ,  A61K9/485 ,  A61K9/4858 ,  A61P1/00 ,  A61P11/00

摘要： According to the invention there is provided a method of improving (e.g. restoring) function in a patient having idiopathic pulmonary fibrosis, which method comprises perorally administering a therapeutically-effective amount of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide (C21), or a pharmaceutically acceptable salt thereof, to said patient. Said treatment is capable of treating said IPF in a therapeutic, including a curative, fashion.

公开(公告)号：US11819494B2

公开(公告)日：2023-11-21

申请号：US17680654

申请日：2022-02-25

申请人： VICORE PHARMA AB

发明人： Carl-Johan Dalsgaard ,  Rohit Batta

IPC分类号： A61K31/4178 ,  A61K9/48 ,  A61P11/00 ,  A61P1/00

CPC分类号： A61K31/4178 ,  A61K9/485 ,  A61K9/4858 ,  A61P1/00

摘要： According to the invention there is provided a method of improving (e.g. restoring) function in a patient having idiopathic pulmonary fibrosis, which method comprises perorally administering a therapeutically-effective amount of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide (C21), or a pharmaceutically acceptable salt thereof, to said patient. Said treatment is capable of treating said IPF in a therapeutic, including a curative, fashion.

公开(公告)号：US20230114153A1

公开(公告)日：2023-04-13

申请号：US17912645

申请日：2021-03-18

申请人： Vicore Pharma AB

发明人： Tomas Fex ,  Bengt Ohlsson ,  Johan Raud

IPC分类号： A61K31/4178 ,  A61K31/192 ,  A61K31/138 ,  A61K31/428 ,  A61K31/635 ,  A61K31/675 ,  A61K31/405 ,  A61K38/13 ,  A61K31/167 ,  A61K31/58 ,  A61K31/4965 ,  A61K31/4418 ,  C07D409/10

摘要： There is provided herein a compound of formula (I), wherein R1, R2, R3, R4, R5 and Z are as defined herein, for use in the treatment of a disease or condition in which activation of AT2 receptors is desired or required but in which inhibition of CYPs is not desired. Such compounds are particularly useful in the treatment of autoimmune and/or fibrotic diseases, including interstitial lung diseases, such as idiopathic pulmonary fibrosis and sarcoidosis.

公开(公告)号：US20220388994A1

公开(公告)日：2022-12-08

申请号：US17761670

申请日：2020-09-18

申请人： Vicore Pharma AB

发明人： Tomas Fex ,  Bengt Ohlsson

IPC分类号： C07D409/10 ,  C07D409/14

摘要： There is provided herein a compound of formula I, wherein R1, R2, R3 Y1, Y2, Y3, Y4, R4, R5 and R6 are as defined herein, which compounds are useful in the treatment of autoimmune and/or fibrotic diseases, including interstitial lung diseases, such as idiopathic pulmonary fibrosis and sarcoidosis.