RU2013112937A - Фармацевтические композиции (r)-1-(2, 2-дифторбензо[d][1, 3]диоксол-5-ил)-n-(2, 3-дигидроксипропил)-6-фтор-2-(1-гидрокси-2-метилпропан-2-ил)-1н-индол-5-ил)циклопропанкарбоксамида и их применение - Google Patents
Фармацевтические композиции (r)-1-(2, 2-дифторбензо[d][1, 3]диоксол-5-ил)-n-(2, 3-дигидроксипропил)-6-фтор-2-(1-гидрокси-2-метилпропан-2-ил)-1н-индол-5-ил)циклопропанкарбоксамида и их применение Download PDFInfo
- Publication number
- RU2013112937A RU2013112937A RU2013112937/15A RU2013112937A RU2013112937A RU 2013112937 A RU2013112937 A RU 2013112937A RU 2013112937/15 A RU2013112937/15 A RU 2013112937/15A RU 2013112937 A RU2013112937 A RU 2013112937A RU 2013112937 A RU2013112937 A RU 2013112937A
- Authority
- RU
- Russia
- Prior art keywords
- tablet
- compound
- specified
- mass
- amount
- Prior art date
Links
- -1 2, 3-DIHYDROXYPROPYL Chemical class 0.000 title claims 3
- 239000008194 pharmaceutical composition Substances 0.000 title claims 2
- 229940125904 compound 1 Drugs 0.000 claims abstract 56
- 239000000314 lubricant Substances 0.000 claims abstract 13
- 239000003085 diluting agent Substances 0.000 claims abstract 11
- 239000007884 disintegrant Substances 0.000 claims abstract 11
- AICOOMRHRUFYCM-ZRRPKQBOSA-N oxazine, 1 Chemical compound C([C@@H]1[C@H](C(C[C@]2(C)[C@@H]([C@H](C)N(C)C)[C@H](O)C[C@]21C)=O)CC1=CC2)C[C@H]1[C@@]1(C)[C@H]2N=C(C(C)C)OC1 AICOOMRHRUFYCM-ZRRPKQBOSA-N 0.000 claims abstract 11
- 239000000945 filler Substances 0.000 claims abstract 10
- 238000000034 method Methods 0.000 claims 21
- 239000000203 mixture Substances 0.000 claims 17
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 14
- 201000010099 disease Diseases 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical group O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 7
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims 7
- 235000019359 magnesium stearate Nutrition 0.000 claims 7
- 238000010922 spray-dried dispersion Methods 0.000 claims 7
- 239000004094 surface-active agent Substances 0.000 claims 7
- 201000003883 Cystic fibrosis Diseases 0.000 claims 6
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 6
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 6
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 6
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 6
- 239000008108 microcrystalline cellulose Substances 0.000 claims 6
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical group O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 5
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 5
- 229960001681 croscarmellose sodium Drugs 0.000 claims 5
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 5
- 229960001021 lactose monohydrate Drugs 0.000 claims 5
- 229920000642 polymer Polymers 0.000 claims 5
- 201000009266 primary ciliary dyskinesia Diseases 0.000 claims 5
- 208000025678 Ciliary Motility disease Diseases 0.000 claims 4
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical group [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 4
- 235000010980 cellulose Nutrition 0.000 claims 4
- 229920002678 cellulose Polymers 0.000 claims 4
- 239000001913 cellulose Substances 0.000 claims 4
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 4
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 3
- 229920002261 Corn starch Polymers 0.000 claims 3
- 102100026383 Vasopressin-neurophysin 2-copeptin Human genes 0.000 claims 3
- 239000008120 corn starch Substances 0.000 claims 3
- 201000010064 diabetes insipidus Diseases 0.000 claims 3
- 230000035772 mutation Effects 0.000 claims 3
- 102000027257 transmembrane receptors Human genes 0.000 claims 3
- 108091008578 transmembrane receptors Proteins 0.000 claims 3
- 206010006474 Bronchopulmonary aspergillosis allergic Diseases 0.000 claims 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 2
- 206010010356 Congenital anomaly Diseases 0.000 claims 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 2
- 208000019693 Lung disease Diseases 0.000 claims 2
- 208000001132 Osteoporosis Diseases 0.000 claims 2
- 206010033645 Pancreatitis Diseases 0.000 claims 2
- 229920002472 Starch Polymers 0.000 claims 2
- 208000006778 allergic bronchopulmonary aspergillosis Diseases 0.000 claims 2
- 229910000323 aluminium silicate Inorganic materials 0.000 claims 2
- SNAAJJQQZSMGQD-UHFFFAOYSA-N aluminum magnesium Chemical compound [Mg].[Al] SNAAJJQQZSMGQD-UHFFFAOYSA-N 0.000 claims 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 230000002950 deficient Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 2
- 206010023332 keratitis Diseases 0.000 claims 2
- 230000011164 ossification Effects 0.000 claims 2
- 235000019698 starch Nutrition 0.000 claims 2
- 239000008107 starch Substances 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 230000017105 transposition Effects 0.000 claims 2
- 210000001835 viscera Anatomy 0.000 claims 2
- OKMWKBLSFKFYGZ-UHFFFAOYSA-N 1-behenoylglycerol Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(O)CO OKMWKBLSFKFYGZ-UHFFFAOYSA-N 0.000 claims 1
- 229920001817 Agar Polymers 0.000 claims 1
- 241000398147 Aleurodiscus amorphus Species 0.000 claims 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- 102100034452 Alternative prion protein Human genes 0.000 claims 1
- 102100032187 Androgen receptor Human genes 0.000 claims 1
- 208000009575 Angelman syndrome Diseases 0.000 claims 1
- 206010002961 Aplasia Diseases 0.000 claims 1
- 102000014461 Ataxins Human genes 0.000 claims 1
- 108010078286 Ataxins Proteins 0.000 claims 1
- 206010003694 Atrophy Diseases 0.000 claims 1
- 208000012904 Bartter disease Diseases 0.000 claims 1
- 208000010062 Bartter syndrome Diseases 0.000 claims 1
- 102100022548 Beta-hexosaminidase subunit alpha Human genes 0.000 claims 1
- 206010006458 Bronchitis chronic Diseases 0.000 claims 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims 1
- 206010008025 Cerebellar ataxia Diseases 0.000 claims 1
- 208000010693 Charcot-Marie-Tooth Disease Diseases 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
- 208000027205 Congenital disease Diseases 0.000 claims 1
- 201000002200 Congenital disorder of glycosylation Diseases 0.000 claims 1
- 206010010456 Congenital emphysema Diseases 0.000 claims 1
- 206010062264 Congenital hyperthyroidism Diseases 0.000 claims 1
- 208000029323 Congenital myotonia Diseases 0.000 claims 1
- 208000029767 Congenital, Hereditary, and Neonatal Diseases and Abnormalities Diseases 0.000 claims 1
- 206010010774 Constipation Diseases 0.000 claims 1
- 206010011831 Cytomegalovirus infection Diseases 0.000 claims 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- 208000024940 Dent disease Diseases 0.000 claims 1
- 206010013883 Dwarfism Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 239000001856 Ethyl cellulose Substances 0.000 claims 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims 1
- 208000024720 Fabry Disease Diseases 0.000 claims 1
- 241000206672 Gelidium Species 0.000 claims 1
- 208000003736 Gerstmann-Straussler-Scheinker Disease Diseases 0.000 claims 1
- 206010072075 Gerstmann-Straussler-Scheinker syndrome Diseases 0.000 claims 1
- 208000018565 Hemochromatosis Diseases 0.000 claims 1
- 206010019860 Hereditary angioedema Diseases 0.000 claims 1
- 101000775732 Homo sapiens Androgen receptor Proteins 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 206010058271 Hyperexplexia Diseases 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 206010020707 Hyperparathyroidism primary Diseases 0.000 claims 1
- 208000003892 Kartagener syndrome Diseases 0.000 claims 1
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 1
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 1
- 208000015439 Lysosomal storage disease Diseases 0.000 claims 1
- 208000007466 Male Infertility Diseases 0.000 claims 1
- 240000003183 Manihot esculenta Species 0.000 claims 1
- 235000016735 Manihot esculenta subsp esculenta Nutrition 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 208000029725 Metabolic bone disease Diseases 0.000 claims 1
- 208000002678 Mucopolysaccharidoses Diseases 0.000 claims 1
- 208000010316 Myotonia congenita Diseases 0.000 claims 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 1
- 201000005118 Nephrogenic diabetes insipidus Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 206010049088 Osteopenia Diseases 0.000 claims 1
- 208000035467 Pancreatic insufficiency Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000025237 Polyendocrinopathy Diseases 0.000 claims 1
- 201000000981 Primary Hyperparathyroidism Diseases 0.000 claims 1
- 108091000054 Prion Proteins 0.000 claims 1
- 201000005660 Protein C Deficiency Diseases 0.000 claims 1
- 244000061456 Solanum tuberosum Species 0.000 claims 1
- 235000002595 Solanum tuberosum Nutrition 0.000 claims 1
- 208000009415 Spinocerebellar Ataxias Diseases 0.000 claims 1
- 235000021355 Stearic acid Nutrition 0.000 claims 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- 208000022292 Tay-Sachs disease Diseases 0.000 claims 1
- 208000006269 X-Linked Bulbo-Spinal Atrophy Diseases 0.000 claims 1
- 208000004622 abetalipoproteinemia Diseases 0.000 claims 1
- 235000010419 agar Nutrition 0.000 claims 1
- 235000010443 alginic acid Nutrition 0.000 claims 1
- 229920000615 alginic acid Polymers 0.000 claims 1
- CEGOLXSVJUTHNZ-UHFFFAOYSA-K aluminium tristearate Chemical compound [Al+3].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CEGOLXSVJUTHNZ-UHFFFAOYSA-K 0.000 claims 1
- 229940063655 aluminum stearate Drugs 0.000 claims 1
- SXQXMCWCWVCFPC-UHFFFAOYSA-N aluminum;potassium;dioxido(oxo)silane Chemical compound [Al+3].[K+].[O-][Si]([O-])=O.[O-][Si]([O-])=O SXQXMCWCWVCFPC-UHFFFAOYSA-N 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 230000002924 anti-infective effect Effects 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 201000004562 autosomal dominant cerebellar ataxia Diseases 0.000 claims 1
- 230000002146 bilateral effect Effects 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 230000023555 blood coagulation Effects 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 229940124630 bronchodilator Drugs 0.000 claims 1
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 1
- 235000010216 calcium carbonate Nutrition 0.000 claims 1
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 claims 1
- 239000001506 calcium phosphate Substances 0.000 claims 1
- 229910000389 calcium phosphate Inorganic materials 0.000 claims 1
- 235000011010 calcium phosphates Nutrition 0.000 claims 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims 1
- 235000013539 calcium stearate Nutrition 0.000 claims 1
- 239000008116 calcium stearate Substances 0.000 claims 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 229920002301 cellulose acetate Polymers 0.000 claims 1
- 208000007451 chronic bronchitis Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 210000004081 cilia Anatomy 0.000 claims 1
- 230000001886 ciliary effect Effects 0.000 claims 1
- 239000004927 clay Substances 0.000 claims 1
- 239000003086 colorant Substances 0.000 claims 1
- 229960000913 crospovidone Drugs 0.000 claims 1
- 230000007547 defect Effects 0.000 claims 1
- 230000007812 deficiency Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 235000019700 dicalcium phosphate Nutrition 0.000 claims 1
- 229940095079 dicalcium phosphate anhydrous Drugs 0.000 claims 1
- 239000006185 dispersion Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 1
- 235000019325 ethyl cellulose Nutrition 0.000 claims 1
- 229920001249 ethyl cellulose Polymers 0.000 claims 1
- 239000003172 expectorant agent Substances 0.000 claims 1
- 230000020764 fibrinolysis Effects 0.000 claims 1
- 229940049654 glyceryl behenate Drugs 0.000 claims 1
- 239000008187 granular material Substances 0.000 claims 1
- 229920000591 gum Polymers 0.000 claims 1
- 208000013746 hereditary thrombophilia due to congenital protein C deficiency Diseases 0.000 claims 1
- 239000008172 hydrogenated vegetable oil Substances 0.000 claims 1
- 229920003063 hydroxymethyl cellulose Polymers 0.000 claims 1
- 229940031574 hydroxymethyl cellulose Drugs 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 229960001375 lactose Drugs 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- NRQNMMBQPIGPTB-UHFFFAOYSA-N methylaluminum Chemical compound [CH3].[Al] NRQNMMBQPIGPTB-UHFFFAOYSA-N 0.000 claims 1
- 229940066491 mucolytics Drugs 0.000 claims 1
- 206010028093 mucopolysaccharidosis Diseases 0.000 claims 1
- 208000000638 myeloperoxidase deficiency Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 235000015097 nutrients Nutrition 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 108010040003 polyglutamine Proteins 0.000 claims 1
- 229920000155 polyglutamine Polymers 0.000 claims 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 1
- 229920001592 potato starch Polymers 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 230000022558 protein metabolic process Effects 0.000 claims 1
- 201000009890 sinusitis Diseases 0.000 claims 1
- 230000000391 smoking effect Effects 0.000 claims 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims 1
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 claims 1
- 159000000000 sodium salts Chemical class 0.000 claims 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 1
- 239000000600 sorbitol Substances 0.000 claims 1
- 235000010356 sorbitol Nutrition 0.000 claims 1
- 238000001694 spray drying Methods 0.000 claims 1
- 229940071117 starch glycolate Drugs 0.000 claims 1
- 239000008117 stearic acid Substances 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- 235000000346 sugar Nutrition 0.000 claims 1
- 239000007916 tablet composition Substances 0.000 claims 1
- 239000000454 talc Substances 0.000 claims 1
- 229910052623 talc Inorganic materials 0.000 claims 1
- 235000012222 talc Nutrition 0.000 claims 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims 1
- 210000001177 vas deferen Anatomy 0.000 claims 1
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Reproductive Health (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Gastroenterology & Hepatology (AREA)
- Cardiology (AREA)
- Psychiatry (AREA)
- Immunology (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Dermatology (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37597610P | 2010-08-23 | 2010-08-23 | |
| US61/375,976 | 2010-08-23 | ||
| US201161506220P | 2011-07-11 | 2011-07-11 | |
| US61/506,220 | 2011-07-11 | ||
| PCT/US2011/048565 WO2012027247A2 (en) | 2010-08-23 | 2011-08-22 | Pharmaceutical composition of (r)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxy propyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide and administration therof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2013112937A true RU2013112937A (ru) | 2014-09-27 |
Family
ID=45594557
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2013112937/15A RU2013112937A (ru) | 2010-08-23 | 2011-08-22 | Фармацевтические композиции (r)-1-(2, 2-дифторбензо[d][1, 3]диоксол-5-ил)-n-(2, 3-дигидроксипропил)-6-фтор-2-(1-гидрокси-2-метилпропан-2-ил)-1н-индол-5-ил)циклопропанкарбоксамида и их применение |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20120046330A1 (enExample) |
| EP (1) | EP2608779A2 (enExample) |
| JP (1) | JP2013536231A (enExample) |
| CN (1) | CN103153287A (enExample) |
| AR (1) | AR084473A1 (enExample) |
| AU (2) | AU2011293658B2 (enExample) |
| BR (1) | BR112013004443A8 (enExample) |
| CA (1) | CA2808501A1 (enExample) |
| MX (1) | MX2013002035A (enExample) |
| NZ (1) | NZ606805A (enExample) |
| RU (1) | RU2013112937A (enExample) |
| TW (2) | TW201238611A (enExample) |
| WO (1) | WO2012027247A2 (enExample) |
Families Citing this family (76)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA06002567A (es) | 2003-09-06 | 2006-09-04 | Vertex Pharma | Moduladores de transportadores con casete de union de atp. |
| US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| MX341797B (es) | 2004-06-24 | 2016-09-02 | Vertex Pharmaceuticals Incorporated * | Moduladores de transportadores con casete de union con atp. |
| MX2008002019A (es) | 2005-08-11 | 2008-04-16 | Vertex Pharma | Moduladores del regulador de conductancia transmembrana de fibrosis quistica. |
| ES2778846T3 (es) | 2005-11-08 | 2020-08-12 | Vertex Pharma | Moduladores heterocíclicos de transportadores de casete de unión a ATP |
| AU2006336504C9 (en) | 2005-12-28 | 2015-05-14 | Vertex Pharmaceuticals Incorporated | 1-(benzo [D] [1,3] dioxol-5-yl) -N- (phenyl) cyclopropane- carboxamide derivatives and related compounds as modulators of ATP-Binding Cassette transporters for the treatment of Cystic Fibrosis |
| LT1993360T (lt) | 2005-12-28 | 2017-06-12 | Vertex Pharmaceuticals Incorporated | N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksochinolin-3-karboksamido kieta forma |
| NZ596889A (en) | 2006-04-07 | 2013-06-28 | Vertex Pharma | Use of amide indole derivatives as modulators of ATP-binding cassette transporters |
| USRE50453E1 (en) | 2006-04-07 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| US10022352B2 (en) | 2006-04-07 | 2018-07-17 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| US7645789B2 (en) | 2006-04-07 | 2010-01-12 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| CN102863432B (zh) | 2007-05-09 | 2016-09-07 | 沃泰克斯药物股份有限公司 | Cftr调节剂 |
| HUE028426T2 (en) | 2007-08-24 | 2016-12-28 | Vertex Pharma | Isothiazolopyridinones for (inter alia) treating cystic fibrosis |
| ES2556080T3 (es) | 2007-11-16 | 2016-01-12 | Vertex Pharmaceuticals Incorporated | Moduladores de isoquinolina de transportadores de casete de unión a ATP |
| US20100036130A1 (en) | 2007-12-07 | 2010-02-11 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxamido-pyridine benzoic acids |
| WO2009076142A2 (en) | 2007-12-07 | 2009-06-18 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxiamido-pyridine benzoic acids |
| KR20150063170A (ko) | 2007-12-07 | 2015-06-08 | 버텍스 파마슈티칼스 인코포레이티드 | 3-(6-(1-(2,2-디플루오로벤조[ｄ][1,3]디옥솔-5-일)사이클로프로판카복스아미도)-3-메틸피리딘-2-일)벤조산의 고체 형태 |
| EA201070699A1 (ru) * | 2007-12-07 | 2011-02-28 | Вертекс Фармасьютикалз Инкорпорейтед | Композиции 3-(6-(1-2,2-дифторбензо[d][1,3]диоксол-5-ил)циклопропанкарбоксамидо)-3-метилпиридин-2-ил)бензойной кислоты |
| CN106432213A (zh) | 2008-02-28 | 2017-02-22 | 沃泰克斯药物股份有限公司 | 作为cftr调节剂的杂芳基衍生物 |
| EP2615085B1 (en) | 2008-03-31 | 2015-08-26 | Vertex Pharmaceuticals Incorporated | Pyridyl derivatives as CFTR modulators |
| US12458635B2 (en) | 2008-08-13 | 2025-11-04 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administrations thereof |
| US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
| AU2009296271A1 (en) * | 2008-09-29 | 2010-04-01 | Vertex Pharmaceuticals Incorporated | Dosage units of 3-(6-(1-(2,2-difluorobenzo [d] [1,3] dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| NZ592685A (en) | 2008-10-23 | 2013-04-26 | Vertex Pharma | Modulators of cystic fibrosis transmembrane conductance regulator |
| MX384179B (es) | 2009-03-20 | 2025-03-14 | Vertex Pharma | Proceso para producir moduladores del regulador de conductancia transmembrana de fibrosis quística. |
| SMT202100051T1 (it) * | 2010-03-25 | 2021-03-15 | Vertex Pharma | Dispersione solida di una forma amorfa di (r)-1-(2,2-difluorobenzo[d][1,3]diossol-5-il)-n-(1-(2,3-diidrossipropil)-6-fluoro-2-(1-idrossi-2-metilpropan-2-il)-1h-indol-5-il)ciclopropan-carbossamide |
| US8802868B2 (en) | 2010-03-25 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide |
| BR112012026255A2 (pt) | 2010-04-07 | 2017-03-14 | Vertex Pharma | composições farmacêuticas de ácido 3-(6-(1-(2-,2-difluorbenzo[d][1,3]dioxol-5-il)ciclopropanocarboxamido)-3-metilpiridin-2-il)benzóico e administração das mesmas |
| CN102933206A (zh) | 2010-04-07 | 2013-02-13 | 弗特克斯药品有限公司 | 3-(6-(1-(2，2-二氟苯并[d][1，3]二氧杂环戊烯-5-基)环丙烷甲酰胺基)-3-甲基吡啶-2-基)苯甲酸的固体形式 |
| RU2745977C2 (ru) * | 2010-04-22 | 2021-04-05 | Вертекс Фармасьютикалз Инкорпорейтед | Способ получения циклоалкилкарбоксамидо-индольных соединений |
| US8563593B2 (en) | 2010-06-08 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Formulations of (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)cyclopropanecarboxamide |
| KR101985044B1 (ko) | 2011-11-08 | 2019-05-31 | 버텍스 파마슈티칼스 인코포레이티드 | Atp-결합 카세트 수송체의 조절제 |
| DK2806859T3 (da) | 2012-01-25 | 2019-08-05 | Vertex Pharma | Formuleringer af 3-(6-(1-(2.2-difluorbenzo[d][1,3]dioxol-5-yl) cyclopropancarboxamido)-3-methylpyridin-2-yl)benzoesyre |
| JP2015511583A (ja) | 2012-02-27 | 2015-04-20 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | 薬学的組成物およびその投与 |
| US8674108B2 (en) | 2012-04-20 | 2014-03-18 | Vertex Pharmaceuticals Incorporated | Solid forms of N-[2,4-bis(1,1-dimethylethy)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
| EP2858645A1 (en) * | 2012-06-08 | 2015-04-15 | Vertex Pharmaceuticals Incorporated | Pharmaceuticl compositions for the treatment of cftr -mediated disorders |
| AU2013290444B2 (en) * | 2012-07-16 | 2018-04-26 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions of (R)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl) cyclopropanecarboxamide and administration thereof |
| EP2895150A1 (en) * | 2012-09-11 | 2015-07-22 | Bend Research, Inc. | Methods for making pharmaceutical solid dosage forms of spray-dried dispersions |
| WO2014141064A1 (en) | 2013-03-13 | 2014-09-18 | Novartis Ag | Notch2 binding molecules for treating respiratory diseases |
| DK3068392T5 (da) | 2013-11-12 | 2021-09-20 | Vertex Pharma | Fremgangsmåde til fremstilling af farmaceutiske sammensætninger til behandlingen af cftr-medierede sygdomme |
| KR102162542B1 (ko) | 2013-12-20 | 2020-10-07 | 주식회사 다이셀 | 지질 대사 개선 작용을 갖는 영양 조성물 |
| MX384259B (es) * | 2014-01-09 | 2025-03-14 | Verastem Inc | Composiciones y metodos para tratamiento de crecimiento celular anormal. |
| SG10201913575VA (en) | 2014-04-15 | 2020-02-27 | Vertex Pharma | Pharmaceutical compositions for the treatment of cystic fibrosis transmembrane conductance regulator mediated diseases |
| EP2932966A1 (en) | 2014-04-16 | 2015-10-21 | Novartis AG | Gamma secretase inhibitors for treating respiratory diseases |
| EP3798214B1 (en) | 2014-10-06 | 2022-09-14 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP3204358B1 (en) | 2014-10-07 | 2018-09-19 | Vertex Pharmaceuticals Incorporated | Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator |
| WO2016081556A1 (en) | 2014-11-18 | 2016-05-26 | Vertex Pharmaceuticals Incorporated | Process of conducting high throughput testing high performance liquid chromatography |
| EP3240539A4 (en) | 2014-12-31 | 2018-07-25 | Auspex Pharmaceuticals, Inc. | Cyclopropanecarboxamide modulators of cystic fibrosis transmembrane conductance regulator |
| WO2016160945A1 (en) | 2015-03-31 | 2016-10-06 | Concert Pharmaceuticals, Inc. | Deuterated vx-661 |
| US10047077B2 (en) | 2016-04-13 | 2018-08-14 | Skyline Antiinfectives, Inc. | Deuterated O-sulfated beta-lactam hydroxamic acids and deuterated N-sulfated beta-lactams |
| EP3509570A1 (en) * | 2016-09-07 | 2019-07-17 | Celgene Corporation | Tablet compositions |
| SG10201913595YA (en) | 2016-09-30 | 2020-02-27 | Vertex Pharma | Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| MA49235B1 (fr) | 2016-12-09 | 2021-02-26 | Vertex Pharma | Modulateur de régulateur de conductance transmembranaire de fibrose kystique, compositions pharmaceutiques, procédés de traitement et procédé de fabrication du modulateur |
| EP3634402B1 (en) | 2017-06-08 | 2026-01-21 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| BR112020000941A2 (pt) | 2017-07-17 | 2020-07-21 | Vertex Pharmaceuticals Incorporated | métodos de tratamento para fibrose cística |
| TWI799435B (zh) | 2017-08-02 | 2023-04-21 | 美商維泰克斯製藥公司 | 製備化合物之製程 |
| IL273831B2 (en) | 2017-10-19 | 2024-10-01 | Vertex Pharma | Crystalline forms and compositions of cftr modulators |
| CN111757874B (zh) | 2017-12-08 | 2024-03-08 | 弗特克斯药品有限公司 | 用于制备囊性纤维化跨膜传导调节因子的调节剂的方法 |
| TWI810243B (zh) | 2018-02-05 | 2023-08-01 | 美商維泰克斯製藥公司 | 用於治療囊腫纖化症之醫藥組合物 |
| EP3752510B1 (en) | 2018-02-15 | 2022-12-07 | Vertex Pharmaceuticals Incorporated | Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cycstic fibrosis, and process for making them |
| US11414439B2 (en) | 2018-04-13 | 2022-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| CA3067611A1 (en) | 2019-01-15 | 2020-07-15 | Apotex Inc. | Processes for the preparation of tezacaftor and intermediates thereof |
| TWI848092B (zh) | 2019-04-03 | 2024-07-11 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白調節劑 |
| SG11202110585SA (en) | 2019-04-11 | 2021-10-28 | Goldfinch Bio Inc | Spray-dried formulation of a pyridazinone trpc5 inhibitor |
| TWI899097B (zh) | 2019-08-14 | 2025-10-01 | 美商維泰克斯製藥公司 | 製備cftr調節劑之方法 |
| KR20220064366A (ko) | 2019-08-14 | 2022-05-18 | 버텍스 파마슈티칼스 인코포레이티드 | Cftr 조절제의 결정질 형태 |
| TWI867024B (zh) | 2019-08-14 | 2024-12-21 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白之調節劑 |
| TWI886158B (zh) | 2019-10-10 | 2025-06-11 | 加拿大商再諾製藥公司 | 選擇性鉀通道調節劑之固態晶型 |
| CN111346062A (zh) * | 2020-03-11 | 2020-06-30 | 左人杰 | 一种以复合钙盐增加主药稳定性的口崩片及其制备方法 |
| UY39204A (es) * | 2020-05-08 | 2021-11-30 | Janssen Pharmaceutica Nv | Formulaciones farmacéuticas de acetato de abiraterona y niraparib |
| WO2022013360A1 (en) * | 2020-07-17 | 2022-01-20 | Synthon B.V. | Pharmaceutical composition comprising ivacaftor |
| CR20230120A (es) | 2020-08-07 | 2023-09-01 | Vertex Pharma | Moduladores del regulador de la conductancia transmembrana de la fibrosis quística |
| CA3188787A1 (en) | 2020-08-13 | 2022-02-17 | Vertex Pharmaceuticals Incorporated | Crystalline forms of cftr modulators |
| US12324802B2 (en) | 2020-11-18 | 2025-06-10 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| CA3204725A1 (en) | 2020-12-10 | 2022-06-16 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020017295A1 (en) | 2000-07-07 | 2002-02-14 | Weers Jeffry G. | Phospholipid-based powders for inhalation |
| US6777400B2 (en) | 2000-08-05 | 2004-08-17 | Smithkline Beecham Corporation | Anti-inflammatory androstane derivative compositions |
| JP4977319B2 (ja) | 2002-09-30 | 2012-07-18 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | 嚢胞性線維症膜コンダクタンス制御因子蛋白質阻害薬およびその使用方法 |
| US20050113423A1 (en) | 2003-03-12 | 2005-05-26 | Vangoor Frederick F. | Modulators of ATP-binding cassette transporters |
| EP3345895B1 (en) | 2003-04-11 | 2019-12-04 | PTC Therapeutics, Inc. | 1,2,4-oxadiazole benzoic acid compound and its use for nonsense suppression and the treatment of disease |
| US7696244B2 (en) | 2003-05-16 | 2010-04-13 | The Regents Of The University Of California | Compounds having activity in increasing ion transport by mutant-CFTR and uses thereof |
| EP1646615B1 (en) | 2003-06-06 | 2009-08-26 | Vertex Pharmaceuticals Incorporated | Pyrimidine derivatives as modulators of atp-binding cassette transporters |
| AU2004279855A1 (en) | 2003-10-08 | 2005-04-21 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters containing cycloalkyl or pyranyl groups |
| EP1682127B1 (en) | 2003-11-14 | 2009-07-29 | Vertex Pharmaceuticals Incorporated | Thiazoles and oxazoles useful as modulators of atp-binding cassette transporters |
| AU2005228685B2 (en) | 2004-03-30 | 2010-08-19 | The Regents Of The University Of California | Hydrazide-containing CFTR inhibitor compounds and uses thereof |
| US20050222271A1 (en) * | 2004-03-31 | 2005-10-06 | Le Huang | Novel amorphous form of memantine hydrochloride |
| AU2005251745A1 (en) | 2004-06-04 | 2005-12-22 | The Regents Of The University Of California | Compounds having activity in increasing ion transport by mutant-CFTR and uses thereof |
| WO2006044456A1 (en) | 2004-10-13 | 2006-04-27 | Ptc Therapeutics, Inc. | Compounds for nonsense suppression, and methods for their use |
| EP1865949B1 (en) | 2005-03-11 | 2012-11-14 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| CA2600869A1 (en) | 2005-03-18 | 2006-09-28 | The Regents Of The University Of California | Compounds having activity in correcting mutant-cftr processing and uses thereof |
| CA2603402C (en) | 2005-04-08 | 2017-10-31 | Ptc Therapeutics, Inc. | Compositions of an orally active 1,2,4-oxadiazole for nonsense mutation suppression therapy |
| JP5426878B2 (ja) | 2005-05-24 | 2014-02-26 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ａｔｐ−結合カセットトランスポーターのモジュレーター |
| CN101312722A (zh) | 2005-10-06 | 2008-11-26 | 沃泰克斯药物股份有限公司 | Atp-结合弹夹转运蛋白的调控剂 |
| LT1993360T (lt) * | 2005-12-28 | 2017-06-12 | Vertex Pharmaceuticals Incorporated | N-[2,4-bis(1,1-dimetiletil)-5-hidroksifenil]-1,4-dihidro-4-oksochinolin-3-karboksamido kieta forma |
| US7645789B2 (en) | 2006-04-07 | 2010-01-12 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
| NZ596889A (en) * | 2006-04-07 | 2013-06-28 | Vertex Pharma | Use of amide indole derivatives as modulators of ATP-binding cassette transporters |
| AU2009296271A1 (en) * | 2008-09-29 | 2010-04-01 | Vertex Pharmaceuticals Incorporated | Dosage units of 3-(6-(1-(2,2-difluorobenzo [d] [1,3] dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| UA104876C2 (uk) | 2008-11-06 | 2014-03-25 | Вертекс Фармасьютікалз Інкорпорейтед | Модулятори atф-зв'язувальних касетних транспортерів |
| HRP20150288T1 (hr) * | 2008-11-06 | 2015-04-24 | Vertex Pharmaceuticals Incorporated | Modulatori atp-vezujuä†ih kasetnih transportera |
| AU2011242452A1 (en) * | 2010-04-22 | 2012-11-08 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions and administrations thereof |
-
2011
- 2011-08-22 JP JP2013526057A patent/JP2013536231A/ja active Pending
- 2011-08-22 CA CA2808501A patent/CA2808501A1/en not_active Abandoned
- 2011-08-22 WO PCT/US2011/048565 patent/WO2012027247A2/en not_active Ceased
- 2011-08-22 AU AU2011293658A patent/AU2011293658B2/en not_active Ceased
- 2011-08-22 EP EP11751753.2A patent/EP2608779A2/en not_active Withdrawn
- 2011-08-22 RU RU2013112937/15A patent/RU2013112937A/ru not_active Application Discontinuation
- 2011-08-22 MX MX2013002035A patent/MX2013002035A/es not_active Application Discontinuation
- 2011-08-22 US US13/214,419 patent/US20120046330A1/en not_active Abandoned
- 2011-08-22 CN CN2011800511228A patent/CN103153287A/zh active Pending
- 2011-08-22 NZ NZ60680511A patent/NZ606805A/en not_active IP Right Cessation
- 2011-08-22 BR BR112013004443A patent/BR112013004443A8/pt not_active Application Discontinuation
- 2011-08-23 TW TW100130218A patent/TW201238611A/zh unknown
- 2011-08-23 TW TW103137082A patent/TWI619515B/zh active
- 2011-08-23 AR ARP110103065 patent/AR084473A1/es not_active Application Discontinuation
-
2015
- 2015-06-03 AU AU2015202975A patent/AU2015202975B2/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| MX2013002035A (es) | 2013-03-25 |
| AU2011293658A1 (en) | 2013-04-04 |
| WO2012027247A3 (en) | 2012-05-24 |
| AU2015202975B2 (en) | 2016-05-12 |
| AU2011293658B2 (en) | 2015-03-05 |
| TW201238611A (en) | 2012-10-01 |
| CA2808501A1 (en) | 2012-03-01 |
| TWI619515B (zh) | 2018-04-01 |
| AU2015202975A1 (en) | 2015-06-18 |
| JP2013536231A (ja) | 2013-09-19 |
| CN103153287A (zh) | 2013-06-12 |
| NZ606805A (en) | 2015-03-27 |
| WO2012027247A2 (en) | 2012-03-01 |
| TW201503911A (zh) | 2015-02-01 |
| BR112013004443A2 (pt) | 2016-06-07 |
| US20120046330A1 (en) | 2012-02-23 |
| AR084473A1 (es) | 2013-05-22 |
| EP2608779A2 (en) | 2013-07-03 |
| BR112013004443A8 (pt) | 2018-01-02 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2013112937A (ru) | Фармацевтические композиции (r)-1-(2, 2-дифторбензо[d][1, 3]диоксол-5-ил)-n-(2, 3-дигидроксипропил)-6-фтор-2-(1-гидрокси-2-метилпропан-2-ил)-1н-индол-5-ил)циклопропанкарбоксамида и их применение | |
| RU2012147272A (ru) | Фармацевтические композиции, включающие 3-(2, 2-дифторбензо[d][1, 3]диоксол-5-ил)циклопропанкарбоксамидо)-3-метилпиридин-2-ил)бензойную кислоту, и их введение | |
| JP2013536231A5 (enExample) | ||
| US6645526B2 (en) | Storage stable thyroxine active drug formulations and methods for their production | |
| US10617668B2 (en) | Pharmaceutical formulations | |
| AU2010221167B2 (en) | Oral dosage forms having a high loading of a gabapentin prodrug | |
| US8414918B2 (en) | Stable imatinib compositions | |
| US7202236B2 (en) | Modified release pharmaceutical formulation | |
| TW201408295A (zh) | （Ｒ）－１－（２，２－二氟苯并［d］［１，３］間二氧雜環戊烯－５－基）－Ｎ－（１－（２，３－二羥基丙基）－６－氟－２－（１－羥基－２－甲基丙－２－基）－１Ｈ－吲哚－５－基）環丙烷甲醯胺之醫藥組合物及其投藥 | |
| RU2015153068A (ru) | ТВЕРДЫЕ ФОРМЫ (R)-1-(2, 2-ДИФТОРБЕНЗО[d][1, 3]ДИОКСОЛ-5-ИЛ)-N-(1-(2, 3-ДИГИДРОКСИПРОПИЛ)-6-ФТОР-2-(1-ГИДРОКСИ-2-МЕТИЛПРОПАН-2-ИЛ)-1H-ИНДОЛ-5-ИЛ)ЦИКЛОПРОПАНКАРБОКСАМИДА | |
| TW201311241A (zh) | 包含蒙特魯卡斯特（ｍｏｎｔｅｌｕｋａｓｔ）及左旋西替利□（ｌｅｖｏｃｅｔｉｒｉｚｉｎｅ）的膠囊調配物 | |
| US20060014734A1 (en) | Immediate release pharmaceutical formulation | |
| JP2009527577A (ja) | フルバスタチンナトリウム医薬組成物 | |
| US9085507B2 (en) | Desfesoterodine in the form of a tartaric acid salt | |
| US7781424B2 (en) | Modified release pharmaceutical formulation | |
| WO2020139237A2 (en) | A bilayer tablet formulation of atorvastatin calcium and ezetimibe | |
| TW202139977A (zh) | 包括阿托伐他汀以及怡妥錠的雙層片劑及其製造方法 | |
| US20130274262A1 (en) | Pharmaceutical compositions of linezolid | |
| US9271951B2 (en) | Levothyroxine formulation with acacia | |
| US20170281640A1 (en) | Pharmaceutical Compositions Containing a Muscle Relaxant and a Nonsteroidal Anti-Inflammatory Drugs (NSAID) | |
| AU2022326513B9 (en) | Pharmaceutical compositions and oral dosage forms of ketamine derivatives | |
| US20200078309A1 (en) | Stable tablet compositions of Sacubitril: Valsartan | |
| US20230050931A1 (en) | Solid pharmaceutical preparation | |
| US20100196469A1 (en) | Pharmaceutical Formulation containing an HMG-COA Reductase Inhibitor and method for the preparation thereof | |
| US12059419B2 (en) | Pharmaceutical composition comprising phthalazinone derivatives |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA94 | Acknowledgement of application withdrawn (non-payment of fees) |
Effective date: 20170505 |