JP2021522254A - Ｈｉｖインテグラーゼ阻害剤として有用な三環式複素環化合物 - Google Patents
Ｈｉｖインテグラーゼ阻害剤として有用な三環式複素環化合物 Download PDFInfo
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- JP2021522254A JP2021522254A JP2020559525A JP2020559525A JP2021522254A JP 2021522254 A JP2021522254 A JP 2021522254A JP 2020559525 A JP2020559525 A JP 2020559525A JP 2020559525 A JP2020559525 A JP 2020559525A JP 2021522254 A JP2021522254 A JP 2021522254A
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- 235000019345 sodium thiosulphate Nutrition 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 125000004079 stearyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000000707 stereoselective effect Effects 0.000 description 1
- 239000012258 stirred mixture Substances 0.000 description 1
- 229960005322 streptomycin Drugs 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 150000003900 succinic acid esters Chemical class 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 150000003459 sulfonic acid esters Chemical class 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000011885 synergistic combination Substances 0.000 description 1
- 229920003051 synthetic elastomer Polymers 0.000 description 1
- 239000005061 synthetic rubber Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 150000003899 tartaric acid esters Chemical class 0.000 description 1
- YBRBMKDOPFTVDT-UHFFFAOYSA-N tert-butylamine Chemical compound CC(C)(C)N YBRBMKDOPFTVDT-UHFFFAOYSA-N 0.000 description 1
- BCNZYOJHNLTNEZ-UHFFFAOYSA-N tert-butyldimethylsilyl chloride Chemical compound CC(C)(C)[Si](C)(C)Cl BCNZYOJHNLTNEZ-UHFFFAOYSA-N 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 229940126585 therapeutic drug Drugs 0.000 description 1
- 150000003567 thiocyanates Chemical class 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- LBLYYCQCTBFVLH-UHFFFAOYSA-M toluenesulfonate group Chemical class C=1(C(=CC=CC1)S(=O)(=O)[O-])C LBLYYCQCTBFVLH-UHFFFAOYSA-M 0.000 description 1
- 125000005490 tosylate group Chemical group 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- PBIMIGNDTBRRPI-UHFFFAOYSA-N trifluoro borate Chemical compound FOB(OF)OF PBIMIGNDTBRRPI-UHFFFAOYSA-N 0.000 description 1
- ONDSBJMLAHVLMI-UHFFFAOYSA-N trimethylsilyldiazomethane Chemical compound C[Si](C)(C)[CH-][N+]#N ONDSBJMLAHVLMI-UHFFFAOYSA-N 0.000 description 1
- 229960005486 vaccine Drugs 0.000 description 1
- 239000000273 veterinary drug Substances 0.000 description 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- HBOMLICNUCNMMY-XLPZGREQSA-N zidovudine Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](N=[N+]=[N-])C1 HBOMLICNUCNMMY-XLPZGREQSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/16—Peri-condensed systems
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Quinoline Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862663377P | 2018-04-27 | 2018-04-27 | |
| US62/663,377 | 2018-04-27 | ||
| US201862664527P | 2018-04-30 | 2018-04-30 | |
| US62/664,527 | 2018-04-30 | ||
| PCT/US2019/028432 WO2019209667A1 (en) | 2018-04-27 | 2019-04-22 | Tricyclic heterocycle compounds useful as hiv integrase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JP2021522254A true JP2021522254A (ja) | 2021-08-30 |
Family
ID=68294232
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020559525A Pending JP2021522254A (ja) | 2018-04-27 | 2019-04-22 | Ｈｉｖインテグラーゼ阻害剤として有用な三環式複素環化合物 |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP3784241A4 (zh) |
| JP (1) | JP2021522254A (zh) |
| KR (1) | KR20210005139A (zh) |
| CN (1) | CN112088005A (zh) |
| AU (1) | AU2019260608A1 (zh) |
| BR (1) | BR112020021768A2 (zh) |
| CA (1) | CA3101180A1 (zh) |
| MA (1) | MA52367A (zh) |
| MX (1) | MX2020011317A (zh) |
| WO (1) | WO2019209667A1 (zh) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT3805220T (lt) | 2018-05-31 | 2024-08-26 | Shionogi & Co., Ltd | Policikliniai karbamoilpiridono dariniai, skirti živ gydymui |
| US11453669B2 (en) | 2018-05-31 | 2022-09-27 | Shionogi & Co., Ltd. | Polycyclic pyridone derivative |
| US11884683B2 (en) | 2018-06-05 | 2024-01-30 | Merck Sharp & Dohme Llc | Tricyclic heterocycle compounds useful as HIV integrase inhibitors |
| EP4122537A1 (en) | 2019-03-22 | 2023-01-25 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use |
| JP7441947B2 (ja) * | 2019-11-26 | 2024-03-01 | ギリアード サイエンシーズ， インコーポレイテッド | Ｍｃｌ１阻害剤を調製するためのプロセス及び中間体 |
| AU2021225809B2 (en) * | 2020-02-24 | 2023-08-24 | Gilead Sciences, Inc. | Tetracyclic compounds for treating HIV infection |
| CR20230315A (es) | 2021-01-19 | 2023-09-01 | Gilead Sciences Inc | Compuestos de piridotriazina sustituidos y usos de estos |
| TWI843506B (zh) | 2022-04-06 | 2024-05-21 | 美商基利科學股份有限公司 | 橋聯三環胺甲醯基吡啶酮化合物及其用途 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2002334205B2 (en) * | 2001-10-26 | 2007-07-05 | Istituto Di Ricerche Di Biologia Molecolara P. Angeletti Spa | Dihydroxypyrimidine carboxamide inhibitors of HIV integrase |
| TW200510425A (en) * | 2003-08-13 | 2005-03-16 | Japan Tobacco Inc | Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor |
| US7902182B2 (en) * | 2005-11-16 | 2011-03-08 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| LT2997033T (lt) * | 2013-05-17 | 2018-02-12 | Merck Sharp & Dohme Corp. | Kondensuoti tricikliniai heterocikliniai junginiai, kaip živ integrazės inhibitoriai |
| WO2017113288A1 (en) * | 2015-12-31 | 2017-07-06 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
-
2019
- 2019-04-22 MX MX2020011317A patent/MX2020011317A/es unknown
- 2019-04-22 BR BR112020021768-9A patent/BR112020021768A2/pt not_active Application Discontinuation
- 2019-04-22 JP JP2020559525A patent/JP2021522254A/ja active Pending
- 2019-04-22 CN CN201980028504.5A patent/CN112088005A/zh active Pending
- 2019-04-22 MA MA052367A patent/MA52367A/fr unknown
- 2019-04-22 EP EP19793407.8A patent/EP3784241A4/en not_active Withdrawn
- 2019-04-22 KR KR1020207033726A patent/KR20210005139A/ko unknown
- 2019-04-22 CA CA3101180A patent/CA3101180A1/en active Pending
- 2019-04-22 AU AU2019260608A patent/AU2019260608A1/en not_active Abandoned
- 2019-04-22 WO PCT/US2019/028432 patent/WO2019209667A1/en active Application Filing
Also Published As
| Publication number | Publication date |
|---|---|
| EP3784241A1 (en) | 2021-03-03 |
| MA52367A (fr) | 2021-03-03 |
| KR20210005139A (ko) | 2021-01-13 |
| BR112020021768A2 (pt) | 2021-01-26 |
| WO2019209667A1 (en) | 2019-10-31 |
| MX2020011317A (es) | 2020-11-18 |
| AU2019260608A1 (en) | 2020-10-29 |
| CN112088005A (zh) | 2020-12-15 |
| EP3784241A4 (en) | 2022-01-19 |
| CA3101180A1 (en) | 2019-10-31 |
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