UY36176A - Formas cristalinas de (2r, 5s, 13ar)-8-hidroxi-7,9- dioxo- n-(2,4,6 - trifluorobencil)-2,3,4,5,7,9,13,13a -octahidro -2,5- metanopirido[1?,2?,4,5]pirazino[2,1-b][1,3]oxazapina- 10-carboxamida - Google Patents
Formas cristalinas de (2r, 5s, 13ar)-8-hidroxi-7,9- dioxo- n-(2,4,6 - trifluorobencil)-2,3,4,5,7,9,13,13a -octahidro -2,5- metanopirido[1?,2?,4,5]pirazino[2,1-b][1,3]oxazapina- 10-carboxamidaInfo
- Publication number
- UY36176A UY36176A UY0001036176A UY36176A UY36176A UY 36176 A UY36176 A UY 36176A UY 0001036176 A UY0001036176 A UY 0001036176A UY 36176 A UY36176 A UY 36176A UY 36176 A UY36176 A UY 36176A
- Authority
- UY
- Uruguay
- Prior art keywords
- dioxo
- oxazapine
- carboxamide
- trifluorobencil
- metanopirido
- Prior art date
Links
- 239000013078 crystal Substances 0.000 title abstract 2
- -1 2,4,6-trifluorobenzyl Chemical group 0.000 abstract 2
- SFJGCXYXEFWEBK-UHFFFAOYSA-N oxazepine Chemical compound O1C=CC=CC=N1 SFJGCXYXEFWEBK-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229910052708 sodium Inorganic materials 0.000 abstract 1
- 239000011734 sodium Substances 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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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
-
- 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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- 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
- A61K31/537—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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
Abstract
La presente invención se relaciona con formas cristalinas y co-cristales de (2R,5S, 13aR)-8-hidroxi-7,9- dioxo- N-(2,4,6 - trifluorobencil)-2,3,4,5,7,9,13,13a -octahidro -2,5-metanopirido[1?,2?,4,5]pirazino[2,1-b][1,3]oxazapina- 10-carboxamida, las formulaciones farmacéuticas, y los usos terapéuticos de las mismas. La presente invención también se relaciona con formas cristalinas novedosas de (2R, 5S, 13aR)-7,9- dioxo- 10-((2,4,6 - trifluorobencil)carbamoil)-2,3,4,5,7,9,13,13a -octahidro -2,5-metanopirido[1?,2?,4,5]pirazino[2,1- b][1,3]oxazepin - 8-olato de sodio Forma 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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UY36176A true UY36176A (es) | 2016-01-08 |
Family
ID=53514405
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
UY0001036176A UY36176A (es) | 2014-06-20 | 2015-06-17 | Formas cristalinas de (2r, 5s, 13ar)-8-hidroxi-7,9- dioxo- n-(2,4,6 - trifluorobencil)-2,3,4,5,7,9,13,13a -octahidro -2,5- metanopirido[1?,2?,4,5]pirazino[2,1-b][1,3]oxazapina- 10-carboxamida |
Country Status (12)
Country | Link |
---|---|
US (4) | US9682084B2 (es) |
EP (3) | EP4309736A3 (es) |
JP (4) | JP6386104B2 (es) |
AU (2) | AU2015276881B2 (es) |
CA (1) | CA2950309C (es) |
ES (1) | ES2962291T3 (es) |
MA (1) | MA40236A (es) |
NZ (2) | NZ726732A (es) |
PL (1) | PL3564244T3 (es) |
TW (1) | TW201613936A (es) |
UY (1) | UY36176A (es) |
WO (1) | WO2015196137A1 (es) |
Families Citing this family (21)
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DK3067358T3 (da) | 2012-12-21 | 2019-11-04 | Gilead Sciences Inc | Polycykliske carbamoylpyridon-forbindelser og deres farmaceutiske anvendelse |
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 (es) | 2014-06-20 | 2018-06-23 | ||
TWI744723B (zh) | 2014-06-20 | 2021-11-01 | 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 |
KR20170123308A (ko) | 2014-12-26 | 2017-11-07 | 에모리 유니버시티 | N4-하이드록시시티딘, 이와 관련된 유도체 및 이의 항 바이러스적 용도 |
CN113546052A (zh) | 2015-11-09 | 2021-10-26 | 吉利德科学公司 | 治疗人免疫缺陷病毒的治疗组合物 |
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 |
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 |
EP3518935A1 (en) * | 2016-09-27 | 2019-08-07 | Gilead Sciences, Inc. | Therapeutic compositions for treatment of human immunodeficiency virus |
BR122022008466B1 (pt) | 2017-12-07 | 2023-12-05 | Emory University | Uso de um composto |
ES2916405T3 (es) * | 2018-02-09 | 2022-06-30 | Sandoz Ag | Forma cristalina de bictegravir sódico |
WO2019207602A1 (en) * | 2018-04-26 | 2019-10-31 | Mylan Laboratories Limited | Polymorphic forms of bictegravir and its sodium salt |
WO2020003151A1 (en) * | 2018-06-28 | 2020-01-02 | 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 |
JP7313438B2 (ja) * | 2018-09-19 | 2023-07-24 | ギリアード サイエンシーズ, インコーポレイテッド | Hivの予防のためのインテグラーゼ阻害剤 |
EP3653629A1 (en) | 2018-11-16 | 2020-05-20 | Sandoz AG | Acid addition salts of an integrase strand transfer inhibitor |
US20220144851A1 (en) | 2019-02-07 | 2022-05-12 | Cipla Limited | Novel polymorphs of integrase inhibitor |
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 |
EP4153181A1 (en) | 2020-05-21 | 2023-03-29 | Gilead Sciences, Inc. | Pharmaceutical compositions comprising bictegravir |
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 (en) * | 2021-04-19 | 2022-10-27 | Honour Lab Limited | Polymorphic forms of bictegravir potassium |
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EP3564244C0 (en) | 2023-09-13 |
JP2020023509A (ja) | 2020-02-13 |
JP6606692B2 (ja) | 2019-11-20 |
US20200390775A1 (en) | 2020-12-17 |
AU2015276881A1 (en) | 2016-12-15 |
US20150366872A1 (en) | 2015-12-24 |
NZ736644A (en) | 2023-06-30 |
US11202780B2 (en) | 2021-12-21 |
EP4309736A2 (en) | 2024-01-24 |
US10098886B2 (en) | 2018-10-16 |
EP3564244A1 (en) | 2019-11-06 |
JP2017518357A (ja) | 2017-07-06 |
US20170333438A1 (en) | 2017-11-23 |
US9682084B2 (en) | 2017-06-20 |
NZ726732A (en) | 2018-05-25 |
EP3157931A1 (en) | 2017-04-26 |
US20190015420A1 (en) | 2019-01-17 |
AU2015276881B2 (en) | 2018-06-07 |
TW201613936A (en) | 2016-04-16 |
CA2950309A1 (en) | 2015-12-23 |
MA40236A (fr) | 2017-04-26 |
ES2962291T3 (es) | 2024-03-18 |
JP2018199687A (ja) | 2018-12-20 |
JP2022153400A (ja) | 2022-10-12 |
AU2018203737A1 (en) | 2018-06-21 |
CA2950309C (en) | 2019-04-30 |
EP3564244B1 (en) | 2023-09-13 |
WO2015196137A1 (en) | 2015-12-23 |
PL3564244T3 (pl) | 2024-04-08 |
EP4309736A3 (en) | 2024-05-08 |
JP6386104B2 (ja) | 2018-09-05 |
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