TWI902729B - 以組合整合酶阻礙劑及抗hiv藥為特徵之hiv感染症的預防及治療用醫藥 - Google Patents
以組合整合酶阻礙劑及抗hiv藥為特徵之hiv感染症的預防及治療用醫藥Info
- Publication number
- TWI902729B TWI902729B TW109141739A TW109141739A TWI902729B TW I902729 B TWI902729 B TW I902729B TW 109141739 A TW109141739 A TW 109141739A TW 109141739 A TW109141739 A TW 109141739A TW I902729 B TWI902729 B TW I902729B
- Authority
- TW
- Taiwan
- Prior art keywords
- compound
- substituted
- group
- groups
- aromatic
- Prior art date
Links
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
- A61K31/535—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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
-
- 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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
-
- 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
- A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
-
- 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
- A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
- A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
-
- 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
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- AIDS & HIV (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2019214882 | 2019-11-28 | ||
| JP2019-214882 | 2019-11-28 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202133858A TW202133858A (zh) | 2021-09-16 |
| TWI902729B true TWI902729B (zh) | 2025-11-01 |
Family
ID=76129584
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW109141739A TWI902729B (zh) | 2019-11-28 | 2020-11-27 | 以組合整合酶阻礙劑及抗hiv藥為特徵之hiv感染症的預防及治療用醫藥 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US12564595B2 (https=) |
| EP (1) | EP4066839A4 (https=) |
| JP (2) | JPWO2021107066A1 (https=) |
| TW (1) | TWI902729B (https=) |
| WO (1) | WO2021107066A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY201239A (en) | 2019-03-22 | 2024-02-13 | Gilead Sciences Inc | Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use |
| WO2021107065A1 (ja) | 2019-11-28 | 2021-06-03 | 塩野義製薬株式会社 | 多環性ピリドピラジン誘導体 |
| PE20221569A1 (es) | 2020-02-24 | 2022-10-06 | Gilead Sciences Inc | Compuestos tetraciclicos para el tratamiento de infecciones por vih |
| ES3064867T3 (en) | 2020-09-30 | 2026-04-29 | Gilead Sciences Inc | Bridged tricyclic carbamoylpyridone compounds for a use in the treatment of hiv |
| US11613546B2 (en) | 2021-01-19 | 2023-03-28 | Gilead Sciences, Inc. | Substituted pyridotriazine compounds and uses thereof |
| TW202446773A (zh) | 2022-04-06 | 2024-12-01 | 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 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007049675A1 (ja) * | 2005-10-27 | 2007-05-03 | Shionogi & Co., Ltd. | Hivインテグラーゼ阻害活性を有する多環性カルバモイルピリドン誘導体 |
| TW201706275A (zh) * | 2015-05-29 | 2017-02-16 | 塩野義製藥股份有限公司 | 具有hiv複製抑制作用之含氮3環性衍生物 |
Family Cites Families (60)
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| GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| TW200510425A (en) | 2003-08-13 | 2005-03-16 | Japan Tobacco Inc | Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor |
| ATE516026T1 (de) | 2005-02-21 | 2011-07-15 | Shionogi & Co | Bicyclisches carbamoylpyridonderivat mit hiv- integrase-hemmender wirkung |
| KR101363875B1 (ko) | 2005-04-28 | 2014-02-21 | 시오노기세야쿠 가부시키가이샤 | Hiv 통합효소 억제 활성을 가지는 다환식카르바모일피리돈 유도체 |
| US20100056516A1 (en) | 2006-07-17 | 2010-03-04 | Williams Peter D | 1-hydroxy naphthyridine compounds as anti-hiv agents |
| WO2011075747A1 (en) | 2009-12-18 | 2011-06-23 | Glaxosmithkline Llc | Therapeutic compounds |
| CA2789457A1 (en) | 2010-02-26 | 2011-09-01 | Susumu Miyazaki | 1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine derivative and use of same as hiv integrase inhibitor |
| US9216995B2 (en) | 2010-04-12 | 2015-12-22 | Shionogi & Co., Ltd. | Pyridone derivative having integrase inhibitory activity |
| CN102464654B (zh) | 2010-11-12 | 2016-01-13 | 上海泓博智源医药技术有限公司 | 抗病毒化合物 |
| AU2012278976B2 (en) | 2011-07-06 | 2017-05-11 | Gilead Sciences, Inc. | Compounds for the treatment of HIV |
| RU2014113230A (ru) | 2011-10-12 | 2015-11-20 | Шионоги Энд Ко., Лтд. | Полициклическое производное пиридона, обладающее ингибирующей активностью в отношении интегразы |
| JO3470B1 (ar) | 2012-10-08 | 2020-07-05 | Merck Sharp & Dohme | مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv |
| EP2931730B1 (en) | 2012-12-17 | 2019-08-07 | Merck Sharp & Dohme Corp. | 4-pyridinonetriazine derivatives as hiv integrase inhibitors |
| EA030003B1 (ru) | 2012-12-21 | 2018-06-29 | Джилид Сайэнс, Инк. | Полициклическое карбамоилпиридоновое соединение и его фармацевтическое применение для лечения вич-инфекции |
| PE20151063A1 (es) | 2012-12-27 | 2015-08-03 | Japan Tobacco Inc | DERIVADO SUSTITUIDO DE ESPIROPIRIDO[1,2-a]PIRAZINA Y USO MEDICO DEL MISMO COMO INHIBIDOR DE LA INTEGRASA DEL VIH |
| ES2642265T3 (es) | 2013-01-09 | 2017-11-16 | Gilead Sciences, Inc. | Compuestos terapéuticos para el tratamiento de infecciones virales |
| TW201443037A (zh) | 2013-01-09 | 2014-11-16 | Gilead Sciences Inc | 治療用化合物 |
| US9220710B2 (en) | 2013-01-09 | 2015-12-29 | Gilead Sciences, Inc. | Therapeutic compounds |
| TWI694071B (zh) | 2013-03-01 | 2020-05-21 | 美商基利科學股份有限公司 | 治療反轉錄病毒科(Retroviridae)病毒感染之治療性化合物 |
| RS56701B1 (sr) | 2013-05-17 | 2018-03-30 | Merck Sharp & Dohme | Fuzionisana triciklična heterociklična jedinjenja kao inhibitori hiv integraze |
| EP3008044B1 (en) | 2013-06-13 | 2018-11-21 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
| NO2865735T3 (https=) | 2013-07-12 | 2018-07-21 | ||
| ES2859102T3 (es) | 2013-07-12 | 2021-10-01 | Gilead Sciences Inc | Compuestos de carbamoilpiridona policíclica y su uso para el tratamiento de infecciones por VIH |
| WO2015039348A1 (en) | 2013-09-23 | 2015-03-26 | Merck Sharp & Dohme Corp. | Tetracyclic heterocycle compounds useful as hiv integrase inhibitors |
| UA117499C2 (uk) | 2013-09-27 | 2018-08-10 | Мерк Шарп Енд Доум Корп. | Заміщені похідні хінолізину, які можна використовувати як інгібітори інтегрази віл |
| WO2015089847A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Spirocyclic heterocycle compounds useful as hiv integrase inhibitors |
| WO2015130966A1 (en) | 2014-02-28 | 2015-09-03 | Gilead Sciences, Inc. | Antiviral agents |
| US9975906B2 (en) * | 2014-05-16 | 2018-05-22 | Shionogi & Co., Ltd. | Tricyclic heterocycle derivatives having HIV replication inhibitory effect |
| WO2015199167A1 (ja) | 2014-06-25 | 2015-12-30 | 日本たばこ産業株式会社 | 置換されたスピロピリド[1,2-a]ピラジン誘導体の製造方法および中間体 |
| JPWO2016027879A1 (ja) * | 2014-08-22 | 2017-06-01 | 塩野義製薬株式会社 | インテグラーゼ阻害活性を有する多環性ピリドン誘導体 |
| EP3186239B1 (en) | 2014-08-29 | 2018-10-10 | Gilead Sciences, Inc. | Antiretroviral agents |
| WO2016090545A1 (en) | 2014-12-09 | 2016-06-16 | Merck Sharp & Dohme Corp. | Spirocyclic heterocycle compounds useful as hiv integrate inhibitors |
| US10150780B2 (en) | 2014-12-09 | 2018-12-11 | Merck Sharp & Dohme Corp. | Spirocyclic heterocycle compounds useful as HIV integrase inhibitors |
| TWI695003B (zh) | 2014-12-23 | 2020-06-01 | 美商基利科學股份有限公司 | 多環胺甲醯基吡啶酮化合物及其醫藥用途 |
| WO2016154527A1 (en) | 2015-03-26 | 2016-09-29 | Merck Sharp & Dohme Corp. | Phosphate-substituted quinolizine derivatives useful as hiv integrase inhibitors |
| KR20190057158A (ko) | 2015-04-02 | 2019-05-27 | 길리애드 사이언시즈, 인코포레이티드 | 폴리시클릭-카르바모일피리돈 화합물 및 그의 제약 용도 |
| WO2016187788A1 (en) | 2015-05-25 | 2016-12-01 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds useful for treating hiv infection |
| US10624912B2 (en) | 2015-11-17 | 2020-04-21 | Merck Sharp & Dohme Corp. | Spirocyclic Pyridotriazine Derivatives useful as HIV integrase inhibitors |
| US10548910B2 (en) | 2015-11-17 | 2020-02-04 | Merck Sharp & Dohme Corp. | Amido-substituted pyridotriazine derivatives useful as HIV integrase inhibitors |
| US10544155B2 (en) | 2015-12-15 | 2020-01-28 | Merck Sharp & Dohme Corp. | Spirocyclic quinolizine derivatives useful as HIV integrase inhibitors |
| WO2017113288A1 (en) | 2015-12-31 | 2017-07-06 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
| CN119462611A (zh) | 2016-08-19 | 2025-02-18 | 吉利德科学公司 | 用于预防性或治疗性治疗hiv病毒感染的治疗性化合物 |
| TW201906834A (zh) | 2017-05-02 | 2019-02-16 | 英商Viiv醫療保健英國(No.5)有限公司 | 人類免疫不全病毒複製之抑制劑 |
| JP7083398B2 (ja) | 2018-02-15 | 2022-06-10 | ギリアード サイエンシーズ, インコーポレイテッド | ピリジン誘導体およびhiv感染を処置するためのその使用 |
| EP3774775B8 (en) | 2018-04-11 | 2023-11-15 | VIIV Healthcare UK (No.5) Limited | 4-oxo-3,4-dihydroquinazoline compounds as inhibitors of human immunodeficiency virus replication |
| MA52802A (fr) * | 2018-05-31 | 2021-04-14 | Shionogi & Co | Dérivé de pyridone polycyclique |
| EP4257137A3 (en) | 2018-05-31 | 2023-11-01 | Shionogi & Co., Ltd | Polycyclic carbamoylpyridone derivatives for the treatment of hiv |
| EP3833436A1 (en) | 2018-08-09 | 2021-06-16 | VIIV Healthcare UK (No.5) Limited | Inhibitors of human immunodeficiency virus replication |
| EP3849982A1 (en) | 2018-09-14 | 2021-07-21 | VIIV Healthcare UK (No.5) Limited | Inhibitors of human immunodeficiency virus replication |
| JP7433303B2 (ja) | 2018-09-20 | 2024-02-19 | ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド | ヒト免疫不全ウイルス複製の阻害剤 |
| ES2971987T3 (es) | 2018-10-24 | 2024-06-10 | Viiv Healthcare Uk No 5 Ltd | Inhibidores de la replicación del virus de inmunodeficiencia humana |
| US11541055B2 (en) | 2018-10-24 | 2023-01-03 | VIIV Healthcare UK (No.5) Limited | Inhibitors of human immunodeficiency virus replication |
| JP7500555B2 (ja) | 2018-10-25 | 2024-06-17 | ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド | ヒト免疫不全ウイルス複製の阻害剤 |
| EP3873607B1 (en) | 2018-10-29 | 2023-11-29 | VIIV Healthcare UK (No.5) Limited | Quinazolinyl-indazole derivatives and their use as inhibitors of human immunodeficiency virus replication |
| US20210395248A1 (en) | 2018-11-05 | 2021-12-23 | VIIV Healthcare UK (No.5) Limited | Inhibitors of human immunodeficiency virus replication |
| JP2022506399A (ja) | 2018-11-05 | 2022-01-17 | ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド | ヒト免疫不全ウイルス複製の阻害剤 |
| UY38559A (es) | 2019-02-01 | 2020-07-31 | Viiv Healthcare Uk No 5 Ltd | Inhibidores de la replicación del virus de la inmunodeficiencia humana |
| JP7361013B2 (ja) * | 2019-11-28 | 2023-10-13 | 塩野義製薬株式会社 | 多環性カルバモイルピリドン誘導体を含有する医薬組成物 |
| JP2021091671A (ja) | 2019-11-28 | 2021-06-17 | 塩野義製薬株式会社 | 多環性ピリドン誘導体を含有する医薬組成物 |
| WO2021107065A1 (ja) | 2019-11-28 | 2021-06-03 | 塩野義製薬株式会社 | 多環性ピリドピラジン誘導体 |
-
2020
- 2020-11-27 EP EP20894693.9A patent/EP4066839A4/en active Pending
- 2020-11-27 JP JP2021561527A patent/JPWO2021107066A1/ja not_active Ceased
- 2020-11-27 US US17/779,763 patent/US12564595B2/en active Active
- 2020-11-27 WO PCT/JP2020/044139 patent/WO2021107066A1/ja not_active Ceased
- 2020-11-27 TW TW109141739A patent/TWI902729B/zh active
-
2025
- 2025-06-19 JP JP2025104041A patent/JP2025134871A/ja active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007049675A1 (ja) * | 2005-10-27 | 2007-05-03 | Shionogi & Co., Ltd. | Hivインテグラーゼ阻害活性を有する多環性カルバモイルピリドン誘導体 |
| TW201706275A (zh) * | 2015-05-29 | 2017-02-16 | 塩野義製藥股份有限公司 | 具有hiv複製抑制作用之含氮3環性衍生物 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP4066839A4 (en) | 2023-12-27 |
| EP4066839A1 (en) | 2022-10-05 |
| WO2021107066A1 (ja) | 2021-06-03 |
| JP2025134871A (ja) | 2025-09-17 |
| TW202133858A (zh) | 2021-09-16 |
| US20230059640A1 (en) | 2023-02-23 |
| US12564595B2 (en) | 2026-03-03 |
| JPWO2021107066A1 (https=) | 2021-06-03 |
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