MA40236A - Formes cristallines de (2r,5s,13ar)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-méthanpyrido[1',2':4,5]pyrazino 2,1-b][1,3]oxazépine-10-carboxamide - Google Patents
Formes cristallines de (2r,5s,13ar)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-méthanpyrido[1',2':4,5]pyrazino 2,1-b][1,3]oxazépine-10-carboxamideInfo
- Publication number
- MA40236A MA40236A MA040236A MA40236A MA40236A MA 40236 A MA40236 A MA 40236A MA 040236 A MA040236 A MA 040236A MA 40236 A MA40236 A MA 40236A MA 40236 A MA40236 A MA 40236A
- Authority
- MA
- Morocco
- Prior art keywords
- trifluorobenzyl
- pyrazino
- octahydro
- dioxo
- crystalline forms
- Prior art date
Links
- SOLUWJRYJLAZCX-LYOVBCGYSA-N bictegravir Chemical compound C([C@H]1O[C@@H]2CC[C@@H](C2)N1C(=O)C1=C(C2=O)O)N1C=C2C(=O)NCC1=C(F)C=C(F)C=C1F SOLUWJRYJLAZCX-LYOVBCGYSA-N 0.000 title 1
- WJNFBIVCQMPPJC-FQYDJHLKSA-M bictegravir sodium Chemical group O=C1C=2N(C[C@H]3O[C@@H]4CC[C@H](N31)C4)C=C(C(C=2[O-])=O)C(NCC1=C(C=C(C=C1F)F)F)=O.[Na+] WJNFBIVCQMPPJC-FQYDJHLKSA-M 0.000 abstract 1
- 239000013078 crystal Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
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- 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
- A61K31/5365—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 ortho- or peri-condensed with heterocyclic ring systems
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
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- 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
- A61K31/537—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 spiro-condensed or forming part of bridged ring systems
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- 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
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- AIDS & HIV (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La présente invention concerne des formes cristallines et des co-cristaux de (2r,5s,13ar)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13 a-octahydro-2,5-méthanpyrido[1',2':4,5]pyrazino 2,1-b][1,3]oxazépine-10-carboxamide, leurs formulations pharmaceutiques et leurs utilisations thérapeutiques. La présente invention concerne également de nouvelles formes cristallines (2r,5s,13 ar)-7,9-dioxo-10-((2,4,6-trifluorobenzyl)carbamoyle)-2,3,4,5,7,9,13,13a-octahydro-2,5-méthanopyrido[1',2':4,5]pyrazino[2,1-b] [1,3]oxazépin-8-olate de sodium forme i
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462015238P | 2014-06-20 | 2014-06-20 | |
US201462017183P | 2014-06-25 | 2014-06-25 |
Publications (1)
Publication Number | Publication Date |
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MA40236A true MA40236A (fr) | 2017-04-26 |
Family
ID=53514405
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MA040236A MA40236A (fr) | 2014-06-20 | 2015-06-19 | Formes cristallines de (2r,5s,13ar)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-méthanpyrido[1',2':4,5]pyrazino 2,1-b][1,3]oxazépine-10-carboxamide |
Country Status (12)
Country | Link |
---|---|
US (4) | US9682084B2 (fr) |
EP (3) | EP3157931A1 (fr) |
JP (4) | JP6386104B2 (fr) |
AU (2) | AU2015276881B2 (fr) |
CA (1) | CA2950309C (fr) |
ES (1) | ES2962291T3 (fr) |
MA (1) | MA40236A (fr) |
NZ (2) | NZ726732A (fr) |
PL (1) | PL3564244T3 (fr) |
TW (1) | TW201613936A (fr) |
UY (1) | UY36176A (fr) |
WO (1) | WO2015196137A1 (fr) |
Families Citing this family (21)
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PT3608325T (pt) | 2012-12-21 | 2022-10-17 | Gilead Sciences Inc | Compostos carbamoílpiridona policíclicos e sua utilização farmacêutica |
TWI677489B (zh) | 2014-06-20 | 2019-11-21 | 美商基利科學股份有限公司 | 多環型胺甲醯基吡啶酮化合物之合成 |
TW201613936A (en) * | 2014-06-20 | 2016-04-16 | Gilead Sciences Inc | Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide |
NO2717902T3 (fr) | 2014-06-20 | 2018-06-23 | ||
HRP20211456T1 (hr) | 2014-12-26 | 2021-12-24 | Emory University | Protuvirusni derivati n4-hidroksicitidina |
PL3346995T3 (pl) * | 2015-11-09 | 2020-03-31 | Gilead Sciences, Inc. | Kompozycje terapeutyczne do leczenia ludzkiego wirusa niedoboru odporności |
TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Hdac抑制劑與pd-l1抑制劑之組合治療 |
WO2018064071A1 (fr) * | 2016-09-27 | 2018-04-05 | Gilead Sciences, Inc. | Compositions thérapeutiques pour le traitement du virus de l'immunodéficience humaine |
JP6804790B1 (ja) | 2017-12-07 | 2020-12-23 | エモリー ユニバーシティー | N4−ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
WO2019154634A1 (fr) * | 2018-02-09 | 2019-08-15 | Sandoz Ag | Forme cristalline de bictégravir sodique |
EP3784676A1 (fr) * | 2018-04-26 | 2021-03-03 | Mylan Laboratories Ltd. | Formes polymorphes de bictégravir et son sel de sodium |
US11623933B2 (en) | 2018-06-28 | 2023-04-11 | Honour Lab Limited | Process for the preparation of sodium (2R,5S,13AR)-7,9-dioxo-10-((2,4,6-trifluorobenzyl) carbamoyl)-2,3,4,5,7,9,13,13A-octahydro-2,5-Methanopyrido[1 ′,2′:4,5]pyrazino[2,1 -b] [1,3] oxazepin-8-olate and its polymorphic form |
AU2019344929B2 (en) * | 2018-09-19 | 2023-03-30 | Gilead Sciences, Inc. | Integrase inhibitors for the prevention of HIV |
EP3653629A1 (fr) | 2018-11-16 | 2020-05-20 | Sandoz AG | Sels d'addition d'acide d'un inhibiteur de transfert de brins de l'intégrase |
WO2020161744A1 (fr) | 2019-02-07 | 2020-08-13 | Cipla Limited | Nouveaux polymorphes d'inhibiteur d'intégrase |
CN111978333B (zh) * | 2019-09-30 | 2021-06-18 | 常州制药厂有限公司 | Bictegravir钠盐的晶型A、制备方法及用途 |
WO2021236944A1 (fr) | 2020-05-21 | 2021-11-25 | Gilead Sciences, Inc. | Compositions pharmaceutiques contenant du bictégravir |
CN113698420A (zh) * | 2020-05-22 | 2021-11-26 | 上海迪赛诺生物医药有限公司 | 比克替拉韦钠的新晶型及其制备方法 |
WO2022224120A1 (fr) * | 2021-04-19 | 2022-10-27 | Honour Lab Limited | Formes polymorphes de bictégravir potassique |
WO2023248240A1 (fr) * | 2022-06-21 | 2023-12-28 | Mylan Laboratories Limited | Formes polymorphes de bictégravir sodique |
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- 2015-06-17 UY UY0001036176A patent/UY36176A/es not_active Application Discontinuation
- 2015-06-19 EP EP15734504.2A patent/EP3157931A1/fr not_active Withdrawn
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- 2015-06-19 US US14/745,121 patent/US9682084B2/en active Active
- 2015-06-19 EP EP23195199.7A patent/EP4309736A3/fr active Pending
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- 2015-06-19 ES ES19167626T patent/ES2962291T3/es active Active
- 2015-06-19 CA CA2950309A patent/CA2950309C/fr active Active
- 2015-06-19 WO PCT/US2015/036784 patent/WO2015196137A1/fr active Application Filing
- 2015-06-19 MA MA040236A patent/MA40236A/fr unknown
- 2015-06-19 PL PL19167626.1T patent/PL3564244T3/pl unknown
- 2015-06-19 JP JP2016574182A patent/JP6386104B2/ja active Active
- 2015-06-19 AU AU2015276881A patent/AU2015276881B2/en active Active
- 2015-06-19 EP EP19167626.1A patent/EP3564244B1/fr active Active
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- 2018-05-28 AU AU2018203737A patent/AU2018203737A1/en not_active Abandoned
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US20190015420A1 (en) | 2019-01-17 |
AU2015276881B2 (en) | 2018-06-07 |
US20170333438A1 (en) | 2017-11-23 |
JP6606692B2 (ja) | 2019-11-20 |
AU2015276881A1 (en) | 2016-12-15 |
PL3564244T3 (pl) | 2024-04-08 |
WO2015196137A1 (fr) | 2015-12-23 |
TW201613936A (en) | 2016-04-16 |
US10098886B2 (en) | 2018-10-16 |
EP3157931A1 (fr) | 2017-04-26 |
JP2022153400A (ja) | 2022-10-12 |
JP2018199687A (ja) | 2018-12-20 |
EP4309736A2 (fr) | 2024-01-24 |
ES2962291T3 (es) | 2024-03-18 |
CA2950309C (fr) | 2019-04-30 |
NZ726732A (en) | 2018-05-25 |
EP3564244A1 (fr) | 2019-11-06 |
JP2020023509A (ja) | 2020-02-13 |
JP2017518357A (ja) | 2017-07-06 |
EP4309736A3 (fr) | 2024-05-08 |
US11202780B2 (en) | 2021-12-21 |
US20200390775A1 (en) | 2020-12-17 |
EP3564244B1 (fr) | 2023-09-13 |
NZ736644A (en) | 2023-06-30 |
EP3564244C0 (fr) | 2023-09-13 |
CA2950309A1 (fr) | 2015-12-23 |
US9682084B2 (en) | 2017-06-20 |
AU2018203737A1 (en) | 2018-06-21 |
JP6386104B2 (ja) | 2018-09-05 |
US20150366872A1 (en) | 2015-12-24 |
UY36176A (es) | 2016-01-08 |
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