CN103724339B - 二氢嘧啶衍生物的晶型 - Google Patents
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- CN103724339B CN103724339B CN201310446506.0A CN201310446506A CN103724339B CN 103724339 B CN103724339 B CN 103724339B CN 201310446506 A CN201310446506 A CN 201310446506A CN 103724339 B CN103724339 B CN 103724339B
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- 235000013681 dietary sucrose Nutrition 0.000 description 1
- 238000001938 differential scanning calorimetry curve Methods 0.000 description 1
- GXGAKHNRMVGRPK-UHFFFAOYSA-N dimagnesium;dioxido-bis[[oxido(oxo)silyl]oxy]silane Chemical compound [Mg+2].[Mg+2].[O-][Si](=O)O[Si]([O-])([O-])O[Si]([O-])=O GXGAKHNRMVGRPK-UHFFFAOYSA-N 0.000 description 1
- ZPWVASYFFYYZEW-UHFFFAOYSA-L dipotassium hydrogen phosphate Chemical compound [K+].[K+].OP([O-])([O-])=O ZPWVASYFFYYZEW-UHFFFAOYSA-L 0.000 description 1
- 235000019797 dipotassium phosphate Nutrition 0.000 description 1
- 229910000396 dipotassium phosphate Inorganic materials 0.000 description 1
- 229910000397 disodium phosphate Inorganic materials 0.000 description 1
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- 239000003221 ear drop Substances 0.000 description 1
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 description 1
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- 238000010438 heat treatment Methods 0.000 description 1
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 1
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- 238000006317 isomerization reaction Methods 0.000 description 1
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 1
- 239000007951 isotonicity adjuster Substances 0.000 description 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
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- 210000004185 liver Anatomy 0.000 description 1
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- VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 description 1
- 239000000347 magnesium hydroxide Substances 0.000 description 1
- 229910001862 magnesium hydroxide Inorganic materials 0.000 description 1
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- 239000001788 mono and diglycerides of fatty acids Substances 0.000 description 1
- CQDGTJPVBWZJAZ-UHFFFAOYSA-N monoethyl carbonate Chemical compound CCOC(O)=O CQDGTJPVBWZJAZ-UHFFFAOYSA-N 0.000 description 1
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- 239000006186 oral dosage form Substances 0.000 description 1
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- 239000002304 perfume Substances 0.000 description 1
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- 239000008055 phosphate buffer solution Substances 0.000 description 1
- 150000003016 phosphoric acids Chemical class 0.000 description 1
- 229920000058 polyacrylate Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000010241 potassium sorbate Nutrition 0.000 description 1
- 239000004302 potassium sorbate Substances 0.000 description 1
- 229940069338 potassium sorbate Drugs 0.000 description 1
- 229940069328 povidone Drugs 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
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- 150000003856 quaternary ammonium compounds Chemical class 0.000 description 1
- 239000003340 retarding agent Substances 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 238000010583 slow cooling Methods 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 235000013599 spices Nutrition 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
- 239000007929 subcutaneous injection Substances 0.000 description 1
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- 239000000829 suppository Substances 0.000 description 1
- 210000001258 synovial membrane Anatomy 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- BSYVTEYKTMYBMK-UHFFFAOYSA-N tetrahydrofurfuryl alcohol Chemical compound OCC1CCCO1 BSYVTEYKTMYBMK-UHFFFAOYSA-N 0.000 description 1
- 230000008719 thickening Effects 0.000 description 1
- 239000010496 thistle oil Substances 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 229940125725 tranquilizer Drugs 0.000 description 1
- 239000003204 tranquilizing agent Substances 0.000 description 1
- 230000002936 tranquilizing effect Effects 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
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 description 1
- 229940038773 trisodium citrate Drugs 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Molecular Biology (AREA)
- Gastroenterology & Hepatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
晶型 | 300mg/mL制样的溶解情况 |
B | 完全溶解,1小时有少量析出 |
C | 完全溶解,4小时无析出 |
0天 | 10天 | 20天 | 30天 | |
高温 | 0.06% | 0.13% | 0.20% | 0.24% |
加速 | 0.06% | 0.09% | 0.08% | 0.10% |
中间 | 0.06% | 0.10% | 0.13% | 0.12% |
高湿 | 0.06% | 0.06% | N/A | N/A |
光照 | 0.06% | 0.12% | N/A | N/A |
0天 | 10天 | 20天 | 30天 | |
高温 | 0.03% | 0.06% | 0.03% | 0.03% |
加速 | 0.03% | 0.04% | 0.04% | 0.04% |
中间 | 0.03% | 0.03% | 0.03% | 0.03% |
高湿 | 0.03% | 0.04% | N/A | N/A |
光照 | 0.03% | 0.03% | N/A | N/A |
Claims (10)
Priority Applications (2)
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CN201310446506.0A CN103724339B (zh) | 2012-09-27 | 2013-09-26 | 二氢嘧啶衍生物的晶型 |
CN201510364423.6A CN104945394B (zh) | 2012-09-27 | 2013-09-26 | 二氢嘧啶衍生物的晶型 |
Applications Claiming Priority (7)
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CN2012103690194 | 2012-09-27 | ||
CN201210369019 | 2012-09-27 | ||
CN201210369019.4 | 2012-09-27 | ||
CN2013101170768 | 2013-04-04 | ||
CN201310117076.8 | 2013-04-04 | ||
CN201310117076 | 2013-04-04 | ||
CN201310446506.0A CN103724339B (zh) | 2012-09-27 | 2013-09-26 | 二氢嘧啶衍生物的晶型 |
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CN201510364423.6A Division CN104945394B (zh) | 2012-09-27 | 2013-09-26 | 二氢嘧啶衍生物的晶型 |
Publications (2)
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CN103724339A CN103724339A (zh) | 2014-04-16 |
CN103724339B true CN103724339B (zh) | 2015-10-14 |
Family
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CN201510364423.6A Active CN104945394B (zh) | 2012-09-27 | 2013-09-26 | 二氢嘧啶衍生物的晶型 |
CN201310446506.0A Active CN103724339B (zh) | 2012-09-27 | 2013-09-26 | 二氢嘧啶衍生物的晶型 |
CN201310445326.0A Pending CN103694234A (zh) | 2012-09-27 | 2013-09-26 | 二氢嘧啶衍生物的晶型 |
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CN201510364423.6A Active CN104945394B (zh) | 2012-09-27 | 2013-09-26 | 二氢嘧啶衍生物的晶型 |
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Country | Link |
---|---|
US (1) | US9403814B2 (zh) |
EP (1) | EP2900664B1 (zh) |
JP (1) | JP6310923B2 (zh) |
KR (1) | KR20150060610A (zh) |
CN (3) | CN104945394B (zh) |
AU (1) | AU2013324779B2 (zh) |
BR (1) | BR112015002979B8 (zh) |
CA (1) | CA2881260C (zh) |
DK (1) | DK2900664T3 (zh) |
ES (1) | ES2660642T3 (zh) |
HK (1) | HK1207081A1 (zh) |
HU (1) | HUE037285T2 (zh) |
MX (1) | MX362829B (zh) |
MY (1) | MY171497A (zh) |
PL (1) | PL2900664T3 (zh) |
PT (1) | PT2900664T (zh) |
RU (1) | RU2646599C2 (zh) |
SG (1) | SG11201500145TA (zh) |
TW (1) | TWI561520B (zh) |
WO (1) | WO2014048355A1 (zh) |
ZA (1) | ZA201500290B (zh) |
Families Citing this family (5)
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MA37942B1 (fr) | 2012-09-10 | 2020-01-31 | Hoffmann La Roche | Hétéroaryldihydropyrimidines d'acide 6-aminé pour le traitement et la prophylaxie d'une infection par le virus de l'hépatite b |
JP6523566B2 (ja) * | 2015-11-04 | 2019-06-05 | チールー ファーマシューティカル カンパニー、リミテッド | ジヒドロピリド環化合物の結晶形、製造方法および中間体 |
WO2017198201A1 (en) * | 2016-05-19 | 2017-11-23 | Sunshine Lake Pharma Co., Ltd. | Crystalline form, salt and complex of dihydropyrimidine derivative, and uses thereof in medicine |
CN107722109B (zh) * | 2016-08-11 | 2020-12-18 | 广东东阳光药业有限公司 | 作为丙型肝炎病毒抑制剂的晶型 |
US9856232B1 (en) * | 2017-06-20 | 2018-01-02 | King Saud University | Dihydropyrimidinone derivatives |
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CN101328170B (zh) | 2007-06-18 | 2011-09-14 | 张中能 | 一种氟苯基-取代噻唑二氢嘧啶 |
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-
2013
- 2013-09-26 CN CN201510364423.6A patent/CN104945394B/zh active Active
- 2013-09-26 TW TW102134813A patent/TWI561520B/zh active
- 2013-09-26 CN CN201310446506.0A patent/CN103724339B/zh active Active
- 2013-09-26 CN CN201310445326.0A patent/CN103694234A/zh active Pending
- 2013-09-27 MY MYPI2015700253A patent/MY171497A/en unknown
- 2013-09-27 MX MX2015004115A patent/MX362829B/es active IP Right Grant
- 2013-09-27 SG SG11201500145TA patent/SG11201500145TA/en unknown
- 2013-09-27 ES ES13841041.0T patent/ES2660642T3/es active Active
- 2013-09-27 PL PL13841041T patent/PL2900664T3/pl unknown
- 2013-09-27 RU RU2015114085A patent/RU2646599C2/ru active
- 2013-09-27 WO PCT/CN2013/084383 patent/WO2014048355A1/en active Application Filing
- 2013-09-27 JP JP2015533438A patent/JP6310923B2/ja active Active
- 2013-09-27 AU AU2013324779A patent/AU2013324779B2/en active Active
- 2013-09-27 PT PT138410410T patent/PT2900664T/pt unknown
- 2013-09-27 DK DK13841041.0T patent/DK2900664T3/en active
- 2013-09-27 US US14/420,666 patent/US9403814B2/en active Active
- 2013-09-27 BR BR112015002979A patent/BR112015002979B8/pt active IP Right Grant
- 2013-09-27 CA CA2881260A patent/CA2881260C/en active Active
- 2013-09-27 HU HUE13841041A patent/HUE037285T2/hu unknown
- 2013-09-27 EP EP13841041.0A patent/EP2900664B1/en active Active
- 2013-09-27 KR KR1020147037155A patent/KR20150060610A/ko not_active IP Right Cessation
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- 2015-08-13 HK HK15107822.2A patent/HK1207081A1/zh unknown
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