MX370639B - Nueva forma policristalina de profármaco tenofovir, y método de preparación y aplicación del mismo. - Google Patents
Nueva forma policristalina de profármaco tenofovir, y método de preparación y aplicación del mismo.Info
- Publication number
- MX370639B MX370639B MX2017000516A MX2017000516A MX370639B MX 370639 B MX370639 B MX 370639B MX 2017000516 A MX2017000516 A MX 2017000516A MX 2017000516 A MX2017000516 A MX 2017000516A MX 370639 B MX370639 B MX 370639B
- Authority
- MX
- Mexico
- Prior art keywords
- crystalline form
- preparation
- present
- application therefor
- henoxyphosphinyl
- Prior art date
Links
- 238000002360 preparation method Methods 0.000 title abstract 2
- 229940002612 prodrug Drugs 0.000 title 1
- 239000000651 prodrug Substances 0.000 title 1
- 229960004556 tenofovir Drugs 0.000 title 1
- VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical compound OC(=O)\C=C\C(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VCMJCVGFSROFHV-WZGZYPNHSA-N 0.000 title 1
- GFFGJBXGBJISGV-UHFFFAOYSA-N Adenine Chemical compound NC1=NC=NC2=C1N=CN2 GFFGJBXGBJISGV-UHFFFAOYSA-N 0.000 abstract 2
- 229930024421 Adenine Natural products 0.000 abstract 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 abstract 2
- 229960000643 adenine Drugs 0.000 abstract 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 238000001647 drug administration Methods 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
- C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
-
- 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
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
- C07C57/13—Dicarboxylic acids
- C07C57/15—Fumaric acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Oncology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Communicable Diseases (AREA)
- AIDS & HIV (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente invención se refiere a una nueva forma cristalina de 9-[(R)-2-[[(S)[[[1-(isopropoxicarbonil)-1-metil]etil]amino]fenoxi fosfinil]metoxil]propil]adeninafuram ato, y un método de preparación y aplicación para los mismos. Específicamente, la presente invención se refiere a una nueva forma cristalina de 9-[(R)-2-[[(S)-[[[1-(isopropoxicarbonil)-1-metil]etil]amino]fenox ifosfinil]metoxil]propil]adeninafuram ato representado por la fórmula (I), caracterizado porque el patrón de XRPD de la forma cristalina incluye al menos 2? ± 0.20° siendo 5.08, 12.44, 13.18, 22.37, 23.37 y 28.56 los picos de difracción. La forma cristalina de la presente invención tiene características tales como alta biodisponibilidad, eficacia significativa, buena estabilidad, alto rendimiento y alta pureza, y contribuye a la selección y diseño de una ruta de administración de fármaco y la determinación de parámetros de proceso de una preparación farmacéutica, mejorando así la calidad de la producción de fármacos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201410349141.4A CN105399771B (zh) | 2014-07-21 | 2014-07-21 | 替诺福韦前药晶型及其制备方法和用途 |
PCT/CN2015/084671 WO2016011932A1 (zh) | 2014-07-21 | 2015-07-21 | 替诺福韦前药新多晶型及其制备方法和用途 |
Publications (2)
Publication Number | Publication Date |
---|---|
MX2017000516A MX2017000516A (es) | 2017-09-01 |
MX370639B true MX370639B (es) | 2019-12-17 |
Family
ID=55162513
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2017000516A MX370639B (es) | 2014-07-21 | 2015-07-21 | Nueva forma policristalina de profármaco tenofovir, y método de preparación y aplicación del mismo. |
Country Status (12)
Country | Link |
---|---|
US (1) | US9840525B2 (es) |
EP (1) | EP3173417A4 (es) |
JP (1) | JP6872179B2 (es) |
KR (1) | KR102476361B1 (es) |
CN (2) | CN105399771B (es) |
AU (1) | AU2015292050B2 (es) |
BR (1) | BR112017000605B1 (es) |
CA (1) | CA2954395C (es) |
MX (1) | MX370639B (es) |
RU (1) | RU2701728C2 (es) |
TW (1) | TWI718990B (es) |
WO (1) | WO2016011932A1 (es) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN108794530A (zh) * | 2017-04-26 | 2018-11-13 | 上海医药工业研究院 | 一种替诺福韦丙酚酰胺盐晶型及其制备方法和用途 |
CN111096954B (zh) * | 2018-10-29 | 2022-09-16 | 江苏豪森药业集团有限公司 | 一种用于抗病毒感染的药物组合物及制备方法 |
EP4081217A1 (en) | 2019-12-24 | 2022-11-02 | F. Hoffmann-La Roche AG | Pharmaceutical combination of antiviral agents targeting hbv and/or an immune modulator for treatment of hbv |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1248869A2 (en) * | 2000-01-07 | 2002-10-16 | Transform Pharmaceuticals, Inc. | High-throughput formation, identification, and analysis of diverse solid-forms |
AU2004206827A1 (en) * | 2003-01-14 | 2004-08-05 | Gilead Sciences, Inc. | Compositions and methods for combination antiviral therapy |
CN102240295B (zh) * | 2005-06-13 | 2013-04-03 | 博瑞生物医药技术(苏州)有限公司 | 泰诺福韦衍生物及用途 |
CN100396689C (zh) | 2006-03-07 | 2008-06-25 | 中国医学科学院医药生物技术研究所 | 一组具有抑制hiv-1/hbv病毒复制活性的替诺福韦单酯化合物 |
US9187508B2 (en) * | 2010-08-01 | 2015-11-17 | Jiangsu Chiatai Tianqing Pharmaceutical Co., Ltd. | Crystalline forms of tenofovir dipivoxil fumarate |
ES2661705T3 (es) * | 2011-10-07 | 2018-04-03 | Gilead Sciences, Inc. | Métodos para la preparación de análogos de nucleótidos antivirales |
CN103665043B (zh) * | 2012-08-30 | 2017-11-10 | 江苏豪森药业集团有限公司 | 一种替诺福韦前药及其在医药上的应用 |
KR101703258B1 (ko) | 2014-12-30 | 2017-02-06 | 한미정밀화학주식회사 | 고순도의 (r)-9-[2-(포스포노메톡시)프로필]아데닌의 제조방법 |
-
2014
- 2014-07-21 CN CN201410349141.4A patent/CN105399771B/zh active Active
-
2015
- 2015-07-21 BR BR112017000605-7A patent/BR112017000605B1/pt active IP Right Grant
- 2015-07-21 KR KR1020177002578A patent/KR102476361B1/ko active IP Right Grant
- 2015-07-21 CN CN201580035392.8A patent/CN106536532B/zh active Active
- 2015-07-21 EP EP15825169.4A patent/EP3173417A4/en not_active Withdrawn
- 2015-07-21 JP JP2017500324A patent/JP6872179B2/ja active Active
- 2015-07-21 AU AU2015292050A patent/AU2015292050B2/en active Active
- 2015-07-21 TW TW104123520A patent/TWI718990B/zh active
- 2015-07-21 WO PCT/CN2015/084671 patent/WO2016011932A1/zh active Application Filing
- 2015-07-21 CA CA2954395A patent/CA2954395C/en active Active
- 2015-07-21 US US15/326,126 patent/US9840525B2/en active Active
- 2015-07-21 RU RU2017102321A patent/RU2701728C2/ru active
- 2015-07-21 MX MX2017000516A patent/MX370639B/es active IP Right Grant
Also Published As
Publication number | Publication date |
---|---|
RU2017102321A3 (es) | 2018-12-06 |
TWI718990B (zh) | 2021-02-21 |
CA2954395C (en) | 2022-08-16 |
TW201623323A (zh) | 2016-07-01 |
CN106536532B (zh) | 2019-09-03 |
CN105399771A (zh) | 2016-03-16 |
KR20170033862A (ko) | 2017-03-27 |
CN106536532A (zh) | 2017-03-22 |
WO2016011932A1 (zh) | 2016-01-28 |
EP3173417A1 (en) | 2017-05-31 |
CN105399771B (zh) | 2020-11-24 |
JP2017522301A (ja) | 2017-08-10 |
AU2015292050A1 (en) | 2017-02-02 |
RU2701728C2 (ru) | 2019-10-01 |
MX2017000516A (es) | 2017-09-01 |
AU2015292050B2 (en) | 2019-01-31 |
JP6872179B2 (ja) | 2021-05-19 |
US9840525B2 (en) | 2017-12-12 |
US20170204125A1 (en) | 2017-07-20 |
RU2017102321A (ru) | 2018-08-21 |
KR102476361B1 (ko) | 2022-12-09 |
BR112017000605B1 (pt) | 2023-04-18 |
BR112017000605A2 (pt) | 2017-11-07 |
CA2954395A1 (en) | 2016-01-28 |
EP3173417A4 (en) | 2018-01-03 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
MX2024001890A (es) | Preparacion de psilocibina, diferentes formas polimorficas, intermediarios, formulaciones, y su uso. | |
WO2012122340A8 (en) | Soluble guanylate cyclase activators | |
MD4664C9 (ro) | Lactame aril şi heteroaril condensate | |
MX2015005286A (es) | Procedimiento para la preparación de derivados del ácido biliar. | |
SG10201902206QA (en) | Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof | |
MX2017014645A (es) | Profarmacos de alvocidib que tienen una biodisponibilidad aumentada. | |
IN2014CN00989A (es) | ||
MY198066A (en) | Method for the preparation of (4s)- 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carbox-amide and the purification thereof for use as an active pharmaceutical ingredient | |
PH12015500211B1 (en) | 4-methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes | |
EA032972B1 (ru) | Гетероциклические карбоновые кислоты в качестве активаторов растворимой гуанилатциклазы | |
MX2019011844A (es) | Proceso para la preparación de derivados de ácidos biliares de sulfonil carbamato. | |
MX2019006165A (es) | Proceso para la preparacion de derivados del acido biliar de las sulfonilureas. | |
ZA201805240B (en) | Tlr7 agonist trifluoroacetate salt and crystalline form b thereof, preparation methods and uses | |
MX2016008665A (es) | Derivado basado en 1,2-naftoquinona y metodo de preparacion del mismo. | |
IN2013MN02170A (es) | ||
WO2013121235A3 (en) | Process for preparation of dronedarone by removal of hydroxyl group | |
MX2013014577A (es) | Compuestos de heteroarilo como ligandos del receptor 5-ht4. | |
MX370639B (es) | Nueva forma policristalina de profármaco tenofovir, y método de preparación y aplicación del mismo. | |
MX339858B (es) | Compuestos novedosos como ligandos del receptor h3 de la histamina. | |
MY191352A (en) | Aldosterone synthase inhibitors | |
WO2012176218A8 (en) | Process for preparing rosuvastatin calcium through novel amine salt | |
MX2018008799A (es) | Derivado de azaciclo amida, metodo de preparacion del mismo y aplicacion farmaceutica. | |
MX2019012257A (es) | Procesos para la preparacion de furazanobencimidazoles y formas cristalinas de estos. | |
IN2015DN02616A (es) | ||
NZ740119A (en) | Cyclic ether derivatives of pyrazolo[1,5-a]pyrimidine-3-carboxyamide |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG | Grant or registration |