JP2020500866A - 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
- Publication number
- JP2020500866A JP2020500866A JP2019529156A JP2019529156A JP2020500866A JP 2020500866 A JP2020500866 A JP 2020500866A JP 2019529156 A JP2019529156 A JP 2019529156A JP 2019529156 A JP2019529156 A JP 2019529156A JP 2020500866 A JP2020500866 A JP 2020500866A
- Authority
- JP
- Japan
- Prior art keywords
- int
- mmol
- alkyl
- compound
- group
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
Links
- 0 CCCC(C1)C1[C@@]1C[C@@](*CCCC=C[C@]2CC=C[C@](CCC[C@](C)CC)C2)CCC1 Chemical compound CCCC(C1)C1[C@@]1C[C@@](*CCCC=C[C@]2CC=C[C@](CCC[C@](C)CC)C2)CCC1 0.000 description 4
Classifications
-
- 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
- C07D498/16—Peri-condensed systems
-
- 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
-
- 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
- A61K31/5365—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
-
- 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
- A61K31/5395—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 having two or more nitrogen atoms in the same ring, e.g. oxadiazines
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (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)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662429376P | 2016-12-02 | 2016-12-02 | |
| US62/429,376 | 2016-12-02 | ||
| PCT/US2017/064116 WO2018102634A1 (en) | 2016-12-02 | 2017-12-01 | Tricyclic heterocycle compounds useful as hiv integrase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020500866A true JP2020500866A (ja) | 2020-01-16 |
| JP2020500866A5 JP2020500866A5 (enExample) | 2021-01-14 |
Family
ID=62242756
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019529156A Ceased JP2020500866A (ja) | 2016-12-02 | 2017-12-01 | 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 (11)
| Country | Link |
|---|---|
| US (1) | US10934312B2 (enExample) |
| EP (1) | EP3548031B1 (enExample) |
| JP (1) | JP2020500866A (enExample) |
| KR (1) | KR20190086017A (enExample) |
| CN (1) | CN110062627A (enExample) |
| AU (1) | AU2017367714B2 (enExample) |
| BR (1) | BR112019011074B1 (enExample) |
| CA (1) | CA3042314A1 (enExample) |
| MX (1) | MX384729B (enExample) |
| RU (1) | RU2749043C2 (enExample) |
| WO (1) | WO2018102634A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20230571A (es) | 2018-05-31 | 2024-01-22 | Shionogi & Co | DERIVADO POLICÍCLICO DE CARBAMOILPIRIDONA (divisional 2020-0644) |
| EP3805221A4 (en) | 2018-05-31 | 2022-01-05 | 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 |
| KR20240151256A (ko) | 2019-03-22 | 2024-10-17 | 길리애드 사이언시즈, 인코포레이티드 | 가교된 트리시클릭 카르바모일피리돈 화합물 및 그의 제약 용도 |
| 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 |
| EP4110783A1 (en) | 2020-02-24 | 2023-01-04 | Gilead Sciences, Inc. | Tetracyclic compounds for treating hiv infection |
| CN112047945B (zh) * | 2020-09-10 | 2021-11-12 | 浙江大学 | 螺环吡啶酮衍生物及应用 |
| CN116390924B (zh) | 2020-09-30 | 2025-11-07 | 吉利德科学公司 | 桥连三环氨基甲酰基吡啶酮化合物及其用途 |
| CR20260070A (es) | 2021-01-19 | 2026-04-24 | Gilead Sciences Inc | COMPUESTOS DE PIRIDOTRIAZINA SUSTITUIDOS Y USOS DE ESTOS (Divisional 2023-0315) |
| TWI856796B (zh) | 2022-04-06 | 2024-09-21 | 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 |
Citations (4)
| 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 |
| WO2014183532A1 (en) * | 2013-05-17 | 2014-11-20 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
| WO2015089847A1 (en) * | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Spirocyclic heterocycle compounds useful as hiv integrase inhibitors |
| US20150329539A1 (en) * | 2012-12-17 | 2015-11-19 | Merck Sharp & Dohme Corp. | 4-pyridinonetriazine derivatives as hiv integrase inhibitors |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE530520T1 (de) | 2001-08-10 | 2011-11-15 | Shionogi & Co | Antivirales mittel |
| CA2463975A1 (en) | 2001-10-26 | 2003-05-01 | Maria Emilia Di Francesco | Dihydroxypyrimidine carboxamide inhibitors of hiv integrase |
| DE122009000048I1 (de) | 2001-10-26 | 2010-04-08 | Angeletti P Ist Richerche Bio | N-substituierte hydroxypyrimidinoncarboxamid-hemmer der hiv-integrase |
| EP1467970B1 (en) | 2002-01-17 | 2007-08-22 | Merck & Co., Inc. | Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors |
| TW200408645A (en) | 2002-04-26 | 2004-06-01 | Gilead Sciences Inc | Non nucleoside reverse transcriptase inhibitors |
| WO2004058756A1 (en) | 2002-12-27 | 2004-07-15 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa | Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors |
| WO2004062613A2 (en) | 2003-01-13 | 2004-07-29 | Bristol-Myers Squibb Company | Hiv integrase inhibitors |
| US7037908B2 (en) | 2003-04-24 | 2006-05-02 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| TW200510425A (en) | 2003-08-13 | 2005-03-16 | Japan Tobacco Inc | Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor |
| AR046938A1 (es) | 2003-12-12 | 2006-01-04 | Merck & Co Inc | Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares |
| TW200526635A (en) | 2003-12-22 | 2005-08-16 | Shionogi & Co | Hydroxypyrimidinone derivative having HIV integrase inhibitory activity |
| US7273859B2 (en) | 2004-05-12 | 2007-09-25 | Bristol-Myers Squibb Company | HIV integrase inhibitors: cyclic pyrimidinone compounds |
| US7115601B2 (en) | 2004-05-18 | 2006-10-03 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US7176196B2 (en) | 2004-05-28 | 2007-02-13 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7173022B2 (en) | 2004-05-28 | 2007-02-06 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7157447B2 (en) | 2004-05-28 | 2007-01-02 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7192948B2 (en) | 2004-05-28 | 2007-03-20 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| WO2006103399A1 (en) | 2005-03-31 | 2006-10-05 | Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa | Hiv integrase inhibitors |
| DK3187225T3 (da) | 2005-04-28 | 2022-02-28 | Viiv Healthcare Co | Polycyklisk carbamoylpyridonderivat med hiv-integrasehæmmende aktivitet |
| US8039458B2 (en) | 2005-11-17 | 2011-10-18 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| WO2007143446A1 (en) | 2006-05-30 | 2007-12-13 | Bristol-Myers Squibb Company | Spiro-condensed heterotricyclic compounds as hiv integrase inhibitors |
| US7893055B2 (en) | 2006-06-28 | 2011-02-22 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| WO2011045330A1 (en) | 2009-10-13 | 2011-04-21 | Tibotec Pharmaceuticals | Macrocyclic integrase inhibitors |
| WO2011121105A1 (en) | 2010-04-02 | 2011-10-06 | Tibotec Pharmaceuticals | Macrocyclic integrase inhibitors |
| US9493479B2 (en) * | 2013-04-16 | 2016-11-15 | Merck Sharp & Dohme Corp. | Substituted pyrido[1,2-a]pyrazines as HIV integrase inhibitors |
| US9951079B2 (en) | 2013-06-13 | 2018-04-24 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as HIV integrase inhibitors |
| JP6579549B2 (ja) | 2014-05-16 | 2019-09-25 | 塩野義製薬株式会社 | Hiv複製阻害作用を有する3環性複素環誘導体 |
| WO2016187788A1 (en) * | 2015-05-25 | 2016-12-01 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds useful for treating hiv infection |
| WO2017113288A1 (en) | 2015-12-31 | 2017-07-06 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
-
2017
- 2017-12-01 WO PCT/US2017/064116 patent/WO2018102634A1/en not_active Ceased
- 2017-12-01 MX MX2019006449A patent/MX384729B/es unknown
- 2017-12-01 EP EP17876015.3A patent/EP3548031B1/en active Active
- 2017-12-01 JP JP2019529156A patent/JP2020500866A/ja not_active Ceased
- 2017-12-01 BR BR112019011074-7A patent/BR112019011074B1/pt not_active IP Right Cessation
- 2017-12-01 US US16/465,614 patent/US10934312B2/en active Active
- 2017-12-01 RU RU2019116590A patent/RU2749043C2/ru active
- 2017-12-01 KR KR1020197018596A patent/KR20190086017A/ko not_active Withdrawn
- 2017-12-01 CA CA3042314A patent/CA3042314A1/en not_active Abandoned
- 2017-12-01 CN CN201780074646.6A patent/CN110062627A/zh active Pending
- 2017-12-01 AU AU2017367714A patent/AU2017367714B2/en not_active Ceased
Patent Citations (4)
| 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 |
| US20150329539A1 (en) * | 2012-12-17 | 2015-11-19 | Merck Sharp & Dohme Corp. | 4-pyridinonetriazine derivatives as hiv integrase inhibitors |
| WO2014183532A1 (en) * | 2013-05-17 | 2014-11-20 | Merck Sharp & Dohme Corp. | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
| WO2015089847A1 (en) * | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Spirocyclic heterocycle compounds useful as hiv integrase inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2017367714B2 (en) | 2020-11-12 |
| EP3548031A1 (en) | 2019-10-09 |
| BR112019011074B1 (pt) | 2021-01-19 |
| RU2749043C2 (ru) | 2021-06-03 |
| CN110062627A (zh) | 2019-07-26 |
| BR112019011074A2 (pt) | 2019-08-20 |
| KR20190086017A (ko) | 2019-07-19 |
| US10934312B2 (en) | 2021-03-02 |
| EP3548031A4 (en) | 2020-06-03 |
| MX384729B (es) | 2025-03-14 |
| WO2018102634A1 (en) | 2018-06-07 |
| RU2019116590A (ru) | 2021-01-11 |
| RU2019116590A3 (enExample) | 2021-01-26 |
| EP3548031B1 (en) | 2023-07-19 |
| AU2017367714A1 (en) | 2019-05-16 |
| MX2019006449A (es) | 2019-09-10 |
| CA3042314A1 (en) | 2018-06-07 |
| US20200017524A1 (en) | 2020-01-16 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6550083B2 (ja) | Hivインテグラーゼ阻害薬として有用な置換されたキノリジン誘導体 | |
| EP3083641B1 (en) | Spirocyclic heterocycle compounds useful as hiv integrase inhibitors | |
| RU2749043C2 (ru) | Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич | |
| KR102345924B1 (ko) | Hiv 인테그라제 억제제로서 유용한 테트라시클릭 헤테로사이클 화합물 | |
| EP3008044B1 (en) | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors | |
| EP3397639B1 (en) | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors | |
| EP3377065B1 (en) | Spirocyclic pyridotriazine derivatives useful as hiv integrase inhibitors | |
| EP3303341B1 (en) | Fused tricyclic heterocyclic compounds useful for treating hiv infection | |
| EP3801543B1 (en) | Tricyclic heterocycle compounds useful as hiv integrase inhibitors | |
| WO2016090545A1 (en) | Spirocyclic heterocycle compounds useful as hiv integrate inhibitors | |
| KR20210005139A (ko) | Hiv 인테그라제 억제제로서 유용한 트리시클릭 헤테로사이클 화합물 | |
| EP3285582A1 (en) | Phosphate-substituted quinolizine derivatives useful as hiv integrase inhibitors |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20201124 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20201124 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20211014 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20211109 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20220119 |
|
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20220524 |
|
| A045 | Written measure of dismissal of application [lapsed due to lack of payment] |
Free format text: JAPANESE INTERMEDIATE CODE: A045 Effective date: 20220927 |