CN105906616A - Lde225单磷酸盐的晶型及其制备方法 - Google Patents
Lde225单磷酸盐的晶型及其制备方法 Download PDFInfo
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- CN105906616A CN105906616A CN201610191617.5A CN201610191617A CN105906616A CN 105906616 A CN105906616 A CN 105906616A CN 201610191617 A CN201610191617 A CN 201610191617A CN 105906616 A CN105906616 A CN 105906616A
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- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
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- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- 239000001253 polyvinylpolypyrrolidone Substances 0.000 description 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
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- 238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
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- 201000009410 rhabdomyosarcoma Diseases 0.000 description 1
- 239000012047 saturated solution Substances 0.000 description 1
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
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- 235000017281 sodium acetate Nutrition 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
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- 239000012453 solvate Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
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- 239000004408 titanium dioxide Substances 0.000 description 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 description 1
- 235000019731 tricalcium phosphate Nutrition 0.000 description 1
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- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
2theta | d间隔 | 强度% |
4.76 | 18.58 | 1.26 |
9.71 | 9.11 | 27.91 |
11.80 | 7.50 | 2.02 |
12.54 | 7.06 | 13.67 |
15.36 | 5.77 | 2.16 |
16.45 | 5.39 | 4.21 |
17.22 | 5.15 | 5.61 |
18.87 | 4.70 | 18.05 |
19.22 | 4.62 | 100.00 |
19.58 | 4.53 | 78.78 |
21.22 | 4.19 | 4.09 |
22.35 | 3.98 | 15.81 |
23.86 | 3.73 | 1.94 |
25.02 | 3.56 | 8.90 |
27.29 | 3.27 | 4.00 |
28.47 | 3.13 | 1.56 |
29.05 | 3.07 | 3.18 |
29.59 | 3.02 | 8.66 |
30.58 | 2.92 | 1.40 |
34.49 | 2.60 | 2.32 |
34.98 | 2.57 | 3.29 |
38.35 | 2.35 | 0.79 |
晶型 | 80%相对湿度的增重 |
式(Ⅰ)化合物单磷酸盐晶型A | 0.59% |
Claims (26)
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CN201510144499 | 2015-03-30 |
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EP (1) | EP3279198B1 (zh) |
CN (1) | CN105906616B (zh) |
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WO2017163258A1 (en) * | 2016-03-22 | 2017-09-28 | Msn Laboratories Private Limited | Process for the preparation of n-[6-(cis-2,6-dimethylmorpholin-4-yl)pyridine-3-yl]-2- methyl-4'-(trifiuoromethoxy) [1,1' -biphenyi]-3-carboxamide and its polymorphs thereof |
WO2019168874A1 (en) | 2018-02-27 | 2019-09-06 | The Research Foundation For The State University Of New York | Difluoromethoxylation and trifluoromethoxylation compositions and methods for synthesizing same |
Citations (2)
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CN102159570A (zh) * | 2008-09-17 | 2011-08-17 | 诺瓦提斯公司 | N-[6-(顺式-2,6-二甲基吗啉-4-基)吡啶-3-基]-2-甲基-4’-(三氟甲氧基)[1,1’-联苯]-3-甲酰胺的盐 |
WO2014128661A1 (en) * | 2013-02-25 | 2014-08-28 | Novartis Ag | Oral formulation and suspension of an oncology drug |
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UA93548C2 (uk) * | 2006-05-05 | 2011-02-25 | Айерем Елелсі | Сполуки та композиції як модулятори хеджхогівського сигнального шляху |
AR077490A1 (es) * | 2009-07-21 | 2011-08-31 | Novartis Ag | Composiciones farmaceuticas topicas para el tratamiento de una condicion hiperproliferativa de la piel |
WO2017163258A1 (en) * | 2016-03-22 | 2017-09-28 | Msn Laboratories Private Limited | Process for the preparation of n-[6-(cis-2,6-dimethylmorpholin-4-yl)pyridine-3-yl]-2- methyl-4'-(trifiuoromethoxy) [1,1' -biphenyi]-3-carboxamide and its polymorphs thereof |
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- 2016-03-30 EP EP16771385.8A patent/EP3279198B1/en active Active
- 2016-03-30 CN CN201610191617.5A patent/CN105906616B/zh active Active
- 2016-03-30 US US15/579,881 patent/US10266523B2/en active Active
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CN102159570A (zh) * | 2008-09-17 | 2011-08-17 | 诺瓦提斯公司 | N-[6-(顺式-2,6-二甲基吗啉-4-基)吡啶-3-基]-2-甲基-4’-(三氟甲氧基)[1,1’-联苯]-3-甲酰胺的盐 |
WO2014128661A1 (en) * | 2013-02-25 | 2014-08-28 | Novartis Ag | Oral formulation and suspension of an oncology drug |
Also Published As
Publication number | Publication date |
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US10266523B2 (en) | 2019-04-23 |
EP3279198A4 (en) | 2018-09-05 |
EP3279198B1 (en) | 2020-01-01 |
EP3279198A1 (en) | 2018-02-07 |
WO2016155630A1 (zh) | 2016-10-06 |
US20180170919A1 (en) | 2018-06-21 |
CN105906616B (zh) | 2018-09-04 |
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