Настройки

Укажите год
-

Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

Подробнее
-

Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

Подробнее

Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Укажите год
Укажите год

Применить Всего найдено 28. Отображено 28.
26-06-2013 дата публикации

Solid form of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydr o-4-oxoquinoline-3-carboxamide

Номер: CN103180298A
Принадлежит:

The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

Подробнее
17-01-2013 дата публикации

Solid Forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide

Номер: US20130018071A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

Подробнее
28-03-2013 дата публикации

SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE-3-CARBOXAMIDE

Номер: US20130079367A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith. 126-. (canceled)27. A method of treating or lessening the severity of a disease in a patient , wherein said disease is selected from cystic fibrosis , asthma , smoke induced COPD , chronic bronchitis , rhinosinusitis , constipation , pancreatitis , pancreatic insufficiency , male infertility caused by congenital bilateral absence of the vas deferens (CBAVD) , mild pulmonary disease , idiopathic pancreatitis , allergic bronchopulmonary aspergillosis (ABPA) , liver disease , hereditary emphysema , hereditary hemochromatosis , coagulation-fibrinolysis deficiencies , such as protein C deficiency , Type 1 hereditary angioedema , lipid processing deficiencies , such as familial hypercholesterolemia , Type 1 chylomicronemia , abetalipoproteinemia , lysosomal storage diseases , such as I-cell disease/pseudo-Hurler , mucopolysaccharidoses , Sandhof/Tay-Sachs , Crigler-Najjar type II , polyendocrinopathy/hyperinsulemia , Diabetes mellitus , Laron dwarfism , myleoperoxidase deficiency , primary hypoparathyroidism , melanoma , glycanosis CDG type 1 , congenital hyperthyroidism , osteogenesis imperfecta , hereditary hypofibrinogenemia , ACT deficiency , Diabetes insipidus (DI) , neurophyseal DI , neprogenic DI , Charcot-Marie Tooth syndrome , Perlizaeus-Merzbacher disease , neurodegenerative diseases such as Alzheimer's disease , Parkinson's disease , amyotrophic lateral sclerosis , progressive supranuclear plasy , Pick's disease , several polyglutamine neurological disorders such as Huntington's , spinocerebullar ataxia type I , spinal and bulbar muscular atrophy , dentatorubal pallidoluysian , and myotonic dystrophy , as well as spongiform encephalopathies , such as hereditary Creutzfeldt-Jakob disease (due to prion protein processing defect) , Fabry disease , ...

Подробнее
23-05-2013 дата публикации

PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF

Номер: US20130131107A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to pharmaceutical compositions comprising a compound of Formulas I and II, optionally in combination with a Compound of Formula III and/or a Compound of Formula IV. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. 9. The pharmaceutical composition of claim 8 , wherein the Column A component is Compound 1 claim 8 , the Column B Component is Compound 2 claim 8 , and the third Component is any of the embodiments listed in Column C of Table I.10. The pharmaceutical composition of claim 8 , wherein the Column A component is Compound 1 claim 8 , the Column B Component is Compound 2 claim 8 , and the third Component is any of the embodiments listed in Column D of Table I.1128-. (canceled)29. A pharmaceutical composition comprising:a solid dispersion of Compound 1 or a pharmaceutically acceptable salt thereof; andCompound 3 or a pharmaceutically acceptable salt thereof.30. The pharmaceutical composition of claim 29 , wherein the solid dispersion of Compound 1 comprises about 80 wt % of substantially amorphous Compound 1 by weight of the dispersion claim 29 , about 19.5 wt % of HPMCAS by weight of the dispersion claim 29 , and about 0.5 wt % SLS by weight of the dispersion.31. The pharmaceutical composition of claim 30 , wherein the composition comprises about 34.1 wt % of the solid dispersion by weight of the composition; about 30.5 wt % of microcrystalline cellulose by weight of the composition; about 30.4 wt % of lactose by weight of the composition; about 3 wt % of sodium croscarmellose by weight of the composition; about 0.5 wt % of SLS by weight of the composition; about 0.5 wt % of colloidal silicon dioxide by weight of the composition; and about 1 wt % of magnesium stearate by weight of the composition.32. The pharmaceutical composition according to claim 31 , wherein the composition ...

Подробнее
06-06-2013 дата публикации

PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF

Номер: US20130143919A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. 2. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I and a Compound of Formula II.3. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I and a Compound of Formula III.4. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I claim 1 , a Compound of Formula H and a Compound of Formula III.98. A method of treating a CFTR mediated disease in a human comprising administering to the human an effective amount of a pharmaceutical composition according to any one of -.10. The method of claim 9 , wherein the CFTR mediated disease is selected from cystic fibrosis claim 9 , asthma claim 9 , smoke induced COPD claim 9 , chronic bronchitis claim 9 , rhinosinusitis claim 9 , constipation claim 9 , pancreatitis claim 9 , pancreatic insufficiency claim 9 , male infertility caused by congenital bilateral absence of the vas deferens (CBAVD) claim 9 , mild pulmonary disease claim 9 , idiopathic pancreatitis claim 9 , allergic bronchopulmonary aspergillosis (ABPA) claim 9 , liver disease claim 9 , hereditary emphysema claim 9 , hereditary hemochromatosis claim 9 , coagulation-fibrinolysis deficiencies claim 9 , such as protein C deficiency claim 9 , Type 1 hereditary angioedema claim 9 , lipid processing deficiencies claim 9 , such as familial hypercholesterolemia claim 9 , Type 1 chylomicronemia claim 9 , abetalipoproteinemia claim 9 , lysosomal storage diseases claim 9 , such as I-cell disease/pseudo-Hurler claim 9 , mucopolysaccharidoses claim 9 , Sandhof/Tay-Sachs claim 9 , Crigler-Najjar type II claim 9 , ...

Подробнее
24-10-2013 дата публикации

Solid Forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide

Номер: US20130281487A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith. 1. A crystalline solvate of Compound 1 , wherein the crystalline solvate is designated as a solid form selected from the group consisting of Form D , Form E , Form F , Form G , Form H , Form I , Form J , Form K , Form L , Form M , Form N , Form O , Form P , Form Q , Form R , Form S , Form T , Form W , and Hydrate B.2. The crystalline solvate Form D of claim 1 , characterized by one or more peaks selected from the group consisting of 5.6±0.2 degrees claim 1 , 6.0±0.2 degrees claim 1 , 7.8±0.2 degrees claim 1 , 13.5±0.2 degrees claim 1 , 14.1±0.2 degrees claim 1 , 14.7±0.2 degrees claim 1 , and 16.2±0.2 degrees on a 2θ scale in an X-ray powder diffraction pattern.3. The crystalline solvate Form E of claim 1 , characterized by one or more peaks selected from the group consisting of 8.0±0.2 degrees claim 1 , 8.6±0.2 degrees claim 1 , 10.1±0.2 degrees claim 1 , 11.0±0.2 degrees claim 1 , 11.9±0.2 degrees claim 1 , 16.5±0.2 degrees claim 1 , 17.1±0.2 degrees claim 1 , and 18.1±0.2 degrees on a 2θ scale in an X-ray powder diffraction pattern.4. The crystalline solvate Form F of claim 1 , characterized by one or more peaks selected from the group consisting of 7.2±0.2 degrees claim 1 , 7.8±0.2 degrees claim 1 , 9.4±0.2 degrees claim 1 , 10.7±0.2 degrees claim 1 , 12.1±0.2 degrees claim 1 , 12.8±0.2 degrees claim 1 , 14.1±0.2 degrees claim 1 , and 14.7±0.2 degrees on a 2θ scale in an X-ray powder diffraction pattern.5. The crystalline solvate Form G of claim 1 , characterized by one or more peaks selected from the group consisting of 6.3±0.2 degrees claim 1 , 7.3±0.2 degrees claim 1 , and 12.4±0.2 degrees on a 2θ scale in an X- ...

Подробнее
19-12-2013 дата публикации

PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF

Номер: US20130338188A9
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. 2. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I and a Compound of Formula II.3. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I and a Compound of Formula III.4. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I claim 1 , a Compound of Formula II and a Compound of Formula III.98. A method of treating a CFTR mediated disease in a human comprising administering to the human an effective amount of a pharmaceutical composition according to any one of -.10. The method of claim 9 , wherein the CFTR mediated disease is selected from cystic fibrosis claim 9 , asthma claim 9 , smoke induced COPD claim 9 , chronic bronchitis claim 9 , rhinosinusitis claim 9 , constipation claim 9 , pancreatitis claim 9 , pancreatic insufficiency claim 9 , male infertility caused by congenital bilateral absence of the vas deferens (CBAVD) claim 9 , mild pulmonary disease claim 9 , idiopathic pancreatitis claim 9 , allergic bronchopulmonary aspergillosis (ABPA) claim 9 , liver disease claim 9 , hereditary emphysema claim 9 , hereditary hemochromatosis claim 9 , coagulation-fibrinolysis deficiencies claim 9 , such as protein C deficiency claim 9 , Type 1 hereditary angioedema claim 9 , lipid processing deficiencies claim 9 , such as familial hypercholesterolemia claim 9 , Type 1 chylomicronemia claim 9 , abetalipoproteinemia claim 9 , lysosomal storage diseases claim 9 , such as I-cell disease/pseudo-Hurler claim 9 , mucopolysaccharidoses claim 9 , Sandhof/Tay-Sachs claim 9 , Crigler-Najjar type II claim 9 , ...

Подробнее
28-01-2016 дата публикации

Pharmaceutical Compositions and Administrations Thereof

Номер: US20160022665A2
Принадлежит:

The present invention relates to pharmaceutical compositions comprising a compound of Formulas I and II, optionally in combination with a Compound of Formula III and/or a Compound of Formula IV. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. 2. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I and Compound of Formula II.5. The pharmaceutical composition of claim 4 , comprising Compound 1 claim 4 , Compound 2 claim 4 , and Compound 3.6. The pharmaceutical composition of claim 1 , comprising Compound 1 claim 1 , Compound 2 claim 1 , and Compound 4.7. The pharmaceutical composition of claim 4 , comprising Compound 1 claim 4 , Compound 2 claim 4 , Compound 3 and Compound 4.9. The pharmaceutical composition of claim 8 , wherein the Column A component is Compound 1 claim 8 , the Column B Component is Compound 2 claim 8 , and the third Component is any of the embodiments listed in Column C of Table I.10. The pharmaceutical composition of claim 8 , wherein the Column A component is Compound 1 claim 8 , the Column B Component is Compound 2 claim 8 , and the third Component is any of the embodiments listed in Column D of Table I.11. The pharmaceutical composition of claim 8 , wherein the Column A component is Compound 1 claim 8 , the Column B Component is Compound 2 claim 8 , the third component is any of the embodiments listed in Column C of Table I claim 8 , and the fourth Component is any of the embodiments listed in Column D of Table I.12. The pharmaceutical composition of claim 8 , wherein the Column A component is Compound 1 claim 8 , the Column B Component is Compound 2 claim 8 , and the third Component is Compound 3.13. The pharmaceutical composition of claim 8 , wherein the Column A component is Compound 1 claim 8 , the Column B Component is Compound 2 claim 8 , and the third Component ...

Подробнее
07-02-2019 дата публикации

PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF

Номер: US20190038615A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. 17-. (canceled)8. A pharmaceutical composition comprising substantially amorphous N-(5-hydroxy-2 ,4-di-tert-butyl-phenyl)-4-oxo-1H-quinoline-3-carboxamide (Compound 1) and substantially amorphous (R)-1-(2 ,2-difluorobenzo[d][1 ,3]dioxol-5-yl)-N-(1-(2 ,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cycloropanecarboxamide (Compound 3) ,wherein the substantially amorphous Compound 1 comprises less than 15% crystalline Compound 1,wherein the substantially amorphous Compound 3 comprises less than 15% crystalline Compound 3, andwherein the pharmaceutical composition is a tablet which comprises 50 mg of substantially amorphous Compound 3.9. A method of treating a CFTR mediated disease in a human claim 8 , wherein the method comprises administering to the human an effective amount of the pharmaceutical composition of .1011-. (canceled)12. The method of claim 9 , wherein the CFTR mediated disease is cystic fibrosis.1322-. (canceled) This application is a continuation of U.S. application Ser. No. 15/643,182, filed Jul. 6, 2017, which is a divisional of U.S. application Ser. No. 14/603,779, filed Jan. 23, 2015, which is a continuation of U.S. application Ser. No. 13/657,321, filed Oct. 22, 2012, which is a continuation of PCT Application No. PCT/US2011/033687, filed Apr. 22, 2011, which claims priority to U.S. provisional application 61/327,078, filed on Apr. 22, 2010, U.S. provisional application 61/327,091, filed on Apr. 22, 2010, and U.S. provisional application 61/329,510, filed on Apr. 29, 2010, all of which are incorporated herein by reference.The present ...

Подробнее
22-05-2014 дата публикации

SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE-3-CARBOXAMIDE

Номер: US20140142312A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith. 127-. (canceled)28. A process for making a crystalline solvate form of Compound 1 , selected from Form D or Form E comprising:a) dissolving Form XX of Compound 1 in at least one solvent to form a mixture;b) heating the mixture until the solid has dissolved;c) precipitating the solid form by cooling the mixtures; andd) isolating the solid form.29. The process of claim 28 , wherein at least one of the solvents is acetonitrile.30. The process of claim 28 , wherein the solvent is a mixture of MEK and water claim 28 , wherein the mixture is 99% MEK and 1% water claim 28 , 90% MEK and 10% water claim 28 , or 80% MEK and 20% water.31. A process for making a crystalline solvate form of Compound 1 claim 28 , selected from Form F or Form E comprising:a) slurrying Form XX of Compound 1 in a solvent comprising acetonitrile and, optionally, water to form a mixture;b) removing residual solid from the mixture by filtration;c) removing the solvent by rapid evaporation; andd) isolating the solid form.32. The process of clause 31 claim 28 , wherein the solvent is acetonitrile.33. A process for making a crystalline solvate Form G of Compound 1 comprising:a) slurrying Form XX of Compound 1 in a solvent comprising isopropyl acetate to form a mixture;b) removing the residual solid from the mixture by filtration;c) removing the solvent by rapid evaporation; andd) isolating the Form G.34. A process for making a crystalline solvate Form H of Compound 1 comprising:a) slurrying Form XX of Compound 1 in a solvent comprising isopropyl acetate and water to form a mixture;b) removing the residual solid from the mixture by filtration;c) removing the ...

Подробнее
10-03-2016 дата публикации

PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF

Номер: US20160067239A9
Принадлежит:

The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. 2. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I and a Compound of Formula II.3. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I and a Compound of Formula III.4. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I claim 1 , a Compound of Formula II and a Compound of Formula III.98. A method of treating a CFTR mediated disease in a human comprising administering to the human an effective amount of a pharmaceutical composition according to any one of -.10. The method of claim 9 , wherein the CFTR mediated disease is selected from cystic fibrosis claim 9 , asthma claim 9 , smoke induced COPD claim 9 , chronic bronchitis claim 9 , rhinosinusitis claim 9 , constipation claim 9 , pancreatitis claim 9 , pancreatic insufficiency claim 9 , male infertility caused by congenital bilateral absence of the vas deferens (CBAVD) claim 9 , mild pulmonary disease claim 9 , idiopathic pancreatitis claim 9 , allergic bronchopulmonary aspergillosis (ABPA) claim 9 , liver disease claim 9 , hereditary emphysema claim 9 , hereditary hemochromatosis claim 9 , coagulation-fibrinolysis deficiencies claim 9 , such as protein C deficiency claim 9 , Type 1 hereditary angioedema claim 9 , lipid processing deficiencies claim 9 , such as familial hypercholesterolemia claim 9 , Type 1 chylomicronemia claim 9 , abetalipoproteinemia claim 9 , lysosomal storage diseases claim 9 , such as I-cell disease/pseudo-Hurler claim 9 , mucopolysaccharidoses claim 9 , Sandhof/Tay-Sachs claim 9 , Crigler-Najjar type II claim 9 , ...

Подробнее
21-05-2015 дата публикации

PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF

Номер: US20150141459A1
Принадлежит:

The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. 2. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I and a Compound of Formula II.3. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I and a Compound of Formula III.4. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I claim 1 , a Compound of Formula II and a Compound of Formula III.98. A method of treating a CFTR mediated disease in a human comprising administering to the human an effective amount of a pharmaceutical composition according to any one of -.10. The method of claim 9 , wherein the CFTR mediated disease is selected from cystic fibrosis claim 9 , asthma claim 9 , smoke induced COPD claim 9 , chronic bronchitis claim 9 , rhinosinusitis claim 9 , constipation claim 9 , pancreatitis claim 9 , pancreatic insufficiency claim 9 , male infertility caused by congenital bilateral absence of the vas deferens (CBAVD) claim 9 , mild pulmonary disease claim 9 , idiopathic pancreatitis claim 9 , allergic bronchopulmonary aspergillosis (ABPA) claim 9 , liver disease claim 9 , hereditary emphysema claim 9 , hereditary hemochromatosis claim 9 , coagulation-fibrinolysis deficiencies claim 9 , such as protein C deficiency claim 9 , Type 1 hereditary angioedema claim 9 , lipid processing deficiencies claim 9 , such as familial hypercholesterolemia claim 9 , Type 1 chylomicronemia claim 9 , abetalipoproteinemia claim 9 , lysosomal storage diseases claim 9 , such as I-cell disease/pseudo-Hurler claim 9 , mucopolysaccharidoses claim 9 , Sandhof/Tay-Sachs claim 9 , Crigler-Najjar type II claim 9 , ...

Подробнее
08-09-2022 дата публикации

SALT AND CRYSTAL FORMS OF AN ACTIVIN RECEPTOR-LIKE KINASE INHIBITOR

Номер: US20220281879A1
Принадлежит:

Various salt forms of Compound (I) represented by the following structural formula, and their corresponding pharmaceutical compositions, are disclosed. Particular single crystalline forms of 1:1.5 Compound (I) succinate, 1:1 Compound (I) hydrochloride salt, and 1:1 Compound (I) fumarate salt are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms are also disclosed. The present disclosure also provides methods of treating or ameliorating fibrodysplasia ossificans progressive in a subject. 2. The succinate salt of claim 1 , wherein the succinate salt is crystalline.3. The succinate salt of claim 1 , wherein the succinate salt is in a single crystalline form.4. The succinate salt of claim 1 , wherein the succinate salt is unsolvated.5. The succinate salt of claim 1 , wherein the succinate salt is in a single crystalline form claim 1 , Form A claim 1 , characterized by an X-ray powder diffraction pattern which comprises peaks at 8.5° claim 1 , 15.4° claim 1 , and 21.3°±0.2 in 2θ.6. The succinate salt of claim 1 , wherein the succinate salt is in a single crystalline form claim 1 , Form A claim 1 , characterized by an X-ray powder diffraction pattern which comprises at least three peaks chosen from 4.3° claim 1 , 8.5° claim 1 , 14.0° claim 1 , 15.4° claim 1 , and 21.3°±0.2 in 2θ.7. The succinate salt of claim 1 , wherein the succinate salt is in a single crystalline form claim 1 , Form A claim 1 , characterized by an X-ray powder diffraction pattern which comprises peaks at 4.3° claim 1 , 8.5° claim 1 , 14.0° claim 1 , 15.4° claim 1 , and 21.3°±0.2 in 2θ.8. The succinate salt of claim 1 , wherein the succinate salt is in a single crystalline form claim 1 , Form A claim 1 , characterized by an X-ray powder diffraction pattern which comprises peaks at 4.3° claim 1 , 6.7° claim 1 , 8.5° claim 1 , 12.8° claim 1 , 14.0° claim 1 , 15.4° claim 1 , 17.0° claim 1 , and 21.3°±0.2 in 2θ.9. The succinate salt of claim ...

Подробнее
07-06-2018 дата публикации

PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF

Номер: US20180153874A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. 18-. (canceled)10. The method of claim 9 , wherein the CFTR mediated disease is selected from cystic fibrosis claim 9 , asthma claim 9 , smoke induced COPD claim 9 , chronic bronchitis claim 9 , rhinosinusitis claim 9 , constipation claim 9 , pancreatitis claim 9 , pancreatic insufficiency claim 9 , male infertility caused by congenital bilateral absence of the vas deferens (CBAVD) claim 9 , mild pulmonary disease claim 9 , idiopathic pancreatitis claim 9 , allergic bronchopulmonary aspergillosis (ABPA) claim 9 , liver disease claim 9 , hereditary emphysema claim 9 , hereditary hemochromatosis claim 9 , coagulation-fibrinolysis deficiencies claim 9 , such as protein C deficiency claim 9 , Type 1 hereditary angioedema claim 9 , lipid processing deficiencies claim 9 , such as familial hypercholesterolemia claim 9 , Type 1 chylomicronemia claim 9 , abetalipoproteinemia claim 9 , lysosomal storage diseases claim 9 , such as I-cell disease/pseudo-Hurler claim 9 , mucopolysaccharidoses claim 9 , Sandhof/Tay-Sachs claim 9 , Crigler-Najjar type II claim 9 , polyendocrinopathy/hyperinsulemia claim 9 , Diabetes mellitus claim 9 , Laron dwarfism claim 9 , myleoperoxidase deficiency claim 9 , primary hypoparathyroidism claim 9 , melanoma claim 9 , glycanosis CDG type 1 claim 9 , congenital hyperthyroidism claim 9 , osteogenesis imperfecta claim 9 , hereditary hypofibrinogenemia claim 9 , ACT deficiency claim 9 , Diabetes insipidus (DI) claim 9 , neurophyseal DI claim 9 , neprogenic DI claim 9 , Charcot-Marie Tooth syndrome claim 9 , Perlizaeus-Merzbacher disease claim 9 , neurodegenerative ...

Подробнее
18-06-2015 дата публикации

PHARMACEUTICAL COMPOSITIONS AND ADMINISTRATIONS THEREOF

Номер: US20150164883A1
Принадлежит:

The present invention relates to pharmaceutical compositions comprising a compound of Formulas I and II, optionally in combination with a Compound of Formula III and/or a Compound of Formula IV. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis. 2. The pharmaceutical composition of claim 1 , comprising a Compound of Formula I and Compound of Formula II.5. The pharmaceutical composition of claim 4 , comprising Compound 1 claim 4 , Compound 2 claim 4 , and Compound 3.6. The pharmaceutical composition of claim 1 , comprising Compound 1 claim 1 , Compound 2 claim 1 , and Compound 4.7. The pharmaceutical composition of claim 4 , comprising Compound 1 claim 4 , Compound 2 claim 4 , Compound 3 and Compound 4.9. The pharmaceutical composition of claim 8 , wherein the Column A component is Compound 1 claim 8 , the Column B Component is Compound 2 claim 8 , and the third Component is any of the embodiments listed in Column C of Table I.10. The pharmaceutical composition of claim 8 , wherein the Column A component is Compound 1 claim 8 , the Column B Component is Compound 2 claim 8 , and the third Component is any of the embodiments listed in Column D of Table I.11. The pharmaceutical composition of claim 8 , wherein the Column A component is Compound 1 claim 8 , the Column B Component is Compound 2 claim 8 , the third component is any of the embodiments listed in Column C of Table I claim 8 , and the fourth Component is any of the embodiments listed in Column D of Table I.12. The pharmaceutical composition of claim 8 , wherein the Column A component is Compound 1 claim 8 , the Column B Component is Compound 2 claim 8 , and the third Component is Compound 3.13. The pharmaceutical composition of claim 8 , wherein the Column A component is Compound 1 claim 8 , the Column B Component is Compound 2 claim 8 , and the third Component ...

Подробнее
06-11-2014 дата публикации

SOLID FORMS OF N-[2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL]-1,4-DIHYDRO-4-OXOQUINOLINE-3-CARBOXAMIDE

Номер: US20140329855A1
Принадлежит:

The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith. 138-. (canceled)39. Crystalline N-[2 ,4-bis(1 ,1-dimethylethyl)-5-hydroxyphenyl]-1 ,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) characterized as Form C , wherein the Form C is characterized by all of the following peaks in an XRPD pattern: about 6.2 , about 7.5 , about 8.3 , about 12.4 , about 14.6 , about 17.9 , about 20.5 and about 20.9 degrees as measured on a 2-Theta scale , and wherein the Form C is isolated and purified.40. A pharmaceutical composition comprising Form C according to claim 39 , and a pharmaceutically acceptable adjuvant or carrier.41. Crystalline N-[2 claim 39 ,4-bis(1 claim 39 ,1-dimethylethyl)-5-hydroxyphenyl]-1 claim 39 ,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) characterized as Form C claim 39 , wherein the Form C is characterized by a peak having a 2-Theta value from about 6.0 to about 6.4 degrees in an XRPD pattern claim 39 , a peak having a 2-Theta value from about 7.3 to about 7.7 degrees in an XRPD pattern claim 39 , a peak having a 2-Theta value from about 8.1 to about 8.5 degrees in an XRPD pattern claim 39 , a peak having a 2-Theta value from about 12.2 to about 12.6 degrees in an XRPD pattern claim 39 , a peak having a 2-Theta value from about 14.4 to about 14.8 degrees in an XRPD pattern claim 39 , a peak having a 2-Theta value from about 17.7 to about 18.1 degrees in an XRPD pattern claim 39 , a peak having a 2-Theta value from about 20.3 to about 20.7 degrees in an XRPD pattern claim 39 , and a peak having a 2-Theta value from about 20.7 to about 21.1 degrees in an XRPD pattern; and wherein the Form C is isolated and purified. This application claims priority under 35 U.S.C. 119(e) to provisional application Ser. No. 61/315,885, filed on Mar. 19, 2010. The entire contents of which is incorporated by ...

Подробнее
19-08-2010 дата публикации

Solid forms of 2-(2, 4-difluorophenyl)-6-(1-(2,6-difluorophenyl)ureido)nicotinamide

Номер: CA2752544A1
Принадлежит: Vertex Pharmaceuticals Inc

This invention relates to solid forms of 2-(2, 4-difluorophenyl)-6-(1- (2,6-difluorophenyl)ureido)nicotinamide and pharmaceutical compositions thereof, and methods and uses therewith.

Подробнее
22-09-2011 дата публикации

Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide

Номер: CA2792207A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

Подробнее
06-09-2011 дата публикации

Solid forms of 2-(2, 4-difluorophenyl)-6-(1-(2,6-difluorophenyl)u reido)nicotinamide.

Номер: MX2011008499A
Принадлежит: Vertex Pharma

Esta invención se refiere a formas sólidas de 2-(2,4-difluorofenil)-6-(1-(2,6-difluorofenil)ureido)nicotinamida y composiciones farmacéuticas de la misma, y métodos y usos con las mismas.

Подробнее
08-03-2017 дата публикации

Pharmaceutical compositions and administrations thereof

Номер: EP3138563A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.

Подробнее
21-12-2011 дата публикации

Solid forms of 2-(2, 4-difluorophenyl)-6-(1-(2,6-difluorophenyl)ureido)nicotinamide

Номер: EP2396303A2
Принадлежит: Vertex Pharmaceuticals Inc

This invention relates to solid forms of 2-(2, 4-difluorophenyl)-6-(l- (2,6-difluorophenyl)ureido)nicotinamide and pharmaceutical compositions thereof, and methods and uses therewith.

Подробнее
18-03-2014 дата публикации

Solid forms of N-[2,4-bis(1,1-dimethylethy)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide

Номер: US8674108B2
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith.

Подробнее
27-10-2011 дата публикации

Pharmaceutical compositions and administrations thereof

Номер: WO2011133951A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to pharmaceutical compositions comprising a compound of Formula I in combination with one or both of a Compound of Formula II and/or a Compound of Formula III. The invention also relates to solid forms and to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis.

Подробнее
05-07-2022 дата публикации

SALT AND CRYSTALLINE FORMS OF A KINASE INHIBITOR SIMILAR TO ACTIVIN RECEPTOR

Номер: BR112022002597A2
Принадлежит: Blueprint Medicines Corp

SAL E FORMAS CRISTALINAS DE UM INIBIDOR DE CINASE SIMILAR AO RECEPTOR DE ACTIVINA. A presente invenção refere-se a várias formas de sal do Composto (I) representadas pela seguinte fórmula estrutural e suas composições farmacêuticas correspondentes. Formas cristalinas únicas particulares de succinato do Composto (I) 1:1,5, sal cloridrato do Composto (I) 1:1 e sal fumarato do Composto (I) 1:1 são caracterizadas por uma variedade de propriedades e medições físicas. Métodos de preparação de formas cristalinas específicas também são divulgados. A presente divulgação também fornece métodos para tratar ou melhorar a fibrodisplasia ossificante progressiva em um indivíduo. SALT AND CRYSTALLINE FORMS OF A KINASE INHIBITOR SIMILAR TO THE ACTIVIN RECEPTOR. The present invention relates to various salt forms of Compound (I) represented by the following structural formula and their corresponding pharmaceutical compositions. Particular single crystalline forms of Compound (I) 1:1.5 succinate, 1:1 Compound (I) hydrochloride salt, and 1:1 Compound (I) fumarate salt are characterized by a variety of physical properties and measurements. Methods of preparing specific crystalline forms are also disclosed. The present disclosure also provides methods for treating or ameliorating fibrodysplasia ossificans progressives in an individual.

Подробнее
18-02-2021 дата публикации

Salt and crystal forms of an activin receptor-like kinase inhibitor

Номер: WO2021030386A1
Принадлежит: BLUEPRINT MEDICINES CORPORATION

Various salt forms of Compound (I) represented by the following structural formula, and their corresponding pharmaceutical compositions, are disclosed. Particular single crystalline forms of 1:1.5 Compound (I) succinate, 1:1 Compound (I) hydrochloride salt, and 1 : 1 Compound (I) fumarate salt are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms are also disclosed. The present disclosure also provides methods of treating or ameliorating fibrodysplasia ossificans progressive in a subject.

Подробнее
23-10-2014 дата публикации

Solid forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide

Номер: AU2012377446A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to crystalline solvate forms of N-[2,4-bis(1,1- dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods for their preparation. The present invention further relates to pharmaceutical compositions comprising the crystalline solvate forms, as well as methods of treatment therewith.

Подробнее
13-06-2024 дата публикации

Treatment or prevention of depressive disorders through combination therapy

Номер: WO2024123935A2
Принадлежит: Freedom Biosciences, Inc.

Provided here are compositions and methods for treating diseases or disorders using a therapeutically effective amount of a N-methyl-D-aspartate (NMDA) receptor modulator and a therapeutically effective amount of a mechanistic target of rapamycin (mTOR) inhibitor.

Подробнее
11-07-2024 дата публикации

Treatment or prevention of depressive disorders through combination therapy

Номер: WO2024123935A3
Принадлежит: Freedom Biosciences, Inc.

Provided here are compositions and methods for treating diseases or disorders using a therapeutically effective amount of a N-methyl-D-aspartate (NMDA) receptor modulator and a therapeutically effective amount of a mechanistic target of rapamycin (mTOR) inhibitor.

Подробнее