KR20190086017A - Hiv 인테그라제 억제제로서 유용한 트리시클릭 헤테로사이클 화합물 - Google Patents
Hiv 인테그라제 억제제로서 유용한 트리시클릭 헤테로사이클 화합물 Download PDFInfo
- Publication number
- KR20190086017A KR20190086017A KR1020197018596A KR20197018596A KR20190086017A KR 20190086017 A KR20190086017 A KR 20190086017A KR 1020197018596 A KR1020197018596 A KR 1020197018596A KR 20197018596 A KR20197018596 A KR 20197018596A KR 20190086017 A KR20190086017 A KR 20190086017A
- Authority
- KR
- South Korea
- Prior art keywords
- int
- mmol
- compound
- group
- alkyl
- 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.)
- Withdrawn
Links
- 0 *CC(OC(C(O)=O)=C1OCc2ccccc2)=CC1=O Chemical compound *CC(OC(C(O)=O)=C1OCc2ccccc2)=CC1=O 0.000 description 6
- NYNZJYAZGCTJMX-UHFFFAOYSA-N CC(C)N(CCC(CN(C(CN1C)=C(C2=O)Br)C3=C2OCc2ccccc2)C1=O)C3=O Chemical compound CC(C)N(CCC(CN(C(CN1C)=C(C2=O)Br)C3=C2OCc2ccccc2)C1=O)C3=O NYNZJYAZGCTJMX-UHFFFAOYSA-N 0.000 description 1
- KUYDAIIXAIDERM-UHFFFAOYSA-N CC(C)N(CN(C(C)=O)N(C(CNC)=CC1=O)C2=C1OCc1ccccc1)C2=O Chemical compound CC(C)N(CN(C(C)=O)N(C(CNC)=CC1=O)C2=C1OCc1ccccc1)C2=O KUYDAIIXAIDERM-UHFFFAOYSA-N 0.000 description 1
- NLHLDFWAJGMMOJ-UHFFFAOYSA-N CC(C)N(CN(C(N(C)CC1=C(C(NCc(ccc(F)c2)c2F)=O)C2=O)=O)N1C1=C2O)C1=O Chemical compound CC(C)N(CN(C(N(C)CC1=C(C(NCc(ccc(F)c2)c2F)=O)C2=O)=O)N1C1=C2O)C1=O NLHLDFWAJGMMOJ-UHFFFAOYSA-N 0.000 description 1
- KUZGOWDBSPLFGG-UHFFFAOYSA-O CC(C)N(CN)C(C([NH2+]C(CNC)=CC1=O)=C1OCc1ccccc1)=O Chemical compound CC(C)N(CN)C(C([NH2+]C(CNC)=CC1=O)=C1OCc1ccccc1)=O KUZGOWDBSPLFGG-UHFFFAOYSA-O 0.000 description 1
- ANIBAUDTDVYXBN-UHFFFAOYSA-N CC(C)N(CNC(N(C)CC(N(C)C1=C2OCc3ccccc3)=C(C(NCc(ccc(F)c3)c3F)=O)C2=O)=O)C1=O Chemical compound CC(C)N(CNC(N(C)CC(N(C)C1=C2OCc3ccccc3)=C(C(NCc(ccc(F)c3)c3F)=O)C2=O)=O)C1=O ANIBAUDTDVYXBN-UHFFFAOYSA-N 0.000 description 1
- OCJOWRZCAXBPQS-UHFFFAOYSA-N CCC(N(C(C(C)=O)=C1OCc2ccccc2)N)=CC1=O Chemical compound CCC(N(C(C(C)=O)=C1OCc2ccccc2)N)=CC1=O OCJOWRZCAXBPQS-UHFFFAOYSA-N 0.000 description 1
- QDZZDVQGBKTLHV-UHFFFAOYSA-N NCc(ccc(F)c1)c1F Chemical compound NCc(ccc(F)c1)c1F QDZZDVQGBKTLHV-UHFFFAOYSA-N 0.000 description 1
- YLACRFYIUQZNIV-UHFFFAOYSA-N NOc(c([N+]([O-])=O)c1)ccc1[N+]([O-])=O Chemical compound NOc(c([N+]([O-])=O)c1)ccc1[N+]([O-])=O YLACRFYIUQZNIV-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- 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
- 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
-
- 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
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 (1)
| Publication Number | Publication Date |
|---|---|
| KR20190086017A true KR20190086017A (ko) | 2019-07-19 |
Family
ID=62242756
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197018596A Withdrawn KR20190086017A (ko) | 2016-12-02 | 2017-12-01 | Hiv 인테그라제 억제제로서 유용한 트리시클릭 헤테로사이클 화합물 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10934312B2 (https=) |
| EP (1) | EP3548031B1 (https=) |
| JP (1) | JP2020500866A (https=) |
| KR (1) | KR20190086017A (https=) |
| CN (1) | CN110062627A (https=) |
| AU (1) | AU2017367714B2 (https=) |
| BR (1) | BR112019011074B1 (https=) |
| CA (1) | CA3042314A1 (https=) |
| MX (1) | MX384729B (https=) |
| RU (1) | RU2749043C2 (https=) |
| WO (1) | WO2018102634A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4257137A3 (en) | 2018-05-31 | 2023-11-01 | Shionogi & Co., Ltd | Polycyclic carbamoylpyridone derivatives for the treatment of hiv |
| MA52802A (fr) | 2018-05-31 | 2021-04-14 | Shionogi & Co | Dérivé de pyridone polycyclique |
| EP3801543B1 (en) | 2018-06-05 | 2024-09-11 | Merck Sharp & Dohme LLC | Tricyclic heterocycle compounds useful as hiv integrase inhibitors |
| 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 |
| CN112047945B (zh) * | 2020-09-10 | 2021-11-12 | 浙江大学 | 螺环吡啶酮衍生物及应用 |
| 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 |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2572030T3 (es) | 2001-08-10 | 2017-07-19 | Shionogi & Co., Ltd. | Agente antiviral |
| ATE355064T1 (de) | 2001-10-26 | 2006-03-15 | Angeletti P Ist Richerche Bio | Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase |
| IL161337A0 (en) | 2001-10-26 | 2004-09-27 | Angeletti P Ist Richerche Bio | N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase |
| EP1467970B1 (en) | 2002-01-17 | 2007-08-22 | Merck & Co., Inc. | Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors |
| WO2003091264A2 (en) | 2002-04-26 | 2003-11-06 | Gilead Sciences, Inc. | Non nucleoside reverse transcriptase inhibitors |
| NZ540729A (en) | 2002-12-27 | 2008-03-28 | Angeletti P Ist Richerche Bio | 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 |
| 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 |
| US7176196B2 (en) | 2004-05-28 | 2007-02-13 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| CA2600832C (en) | 2005-03-31 | 2011-12-13 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Hiv integrase inhibitors |
| KR101363875B1 (ko) | 2005-04-28 | 2014-02-21 | 시오노기세야쿠 가부시키가이샤 | Ｈｉｖ 통합효소 억제 활성을 가지는 다환식카르바모일피리돈 유도체 |
| MX2008005137A (es) * | 2005-10-27 | 2008-09-29 | Shionogi & Co | Derivado de carbamoilpiridona policiclica que tiene actividad inhibidora en vih integrasa. |
| 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 |
| ES2446720T3 (es) | 2009-10-13 | 2014-03-10 | Elanco Animal Health Ireland Limited | Inhibidores de la integrasa macrocíclica |
| WO2011121105A1 (en) | 2010-04-02 | 2011-10-06 | Tibotec Pharmaceuticals | Macrocyclic integrase inhibitors |
| EP2931730B1 (en) * | 2012-12-17 | 2019-08-07 | Merck Sharp & Dohme Corp. | 4-pyridinonetriazine derivatives as hiv integrase inhibitors |
| US9493479B2 (en) * | 2013-04-16 | 2016-11-15 | Merck Sharp & Dohme Corp. | Substituted pyrido[1,2-a]pyrazines as HIV integrase inhibitors |
| 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 |
| WO2015089847A1 (en) * | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Spirocyclic heterocycle compounds useful as hiv integrase inhibitors |
| US9975906B2 (en) * | 2014-05-16 | 2018-05-22 | Shionogi & Co., Ltd. | Tricyclic heterocycle derivatives having HIV replication inhibitory effect |
| 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 CA CA3042314A patent/CA3042314A1/en not_active Abandoned
- 2017-12-01 US US16/465,614 patent/US10934312B2/en active Active
- 2017-12-01 KR KR1020197018596A patent/KR20190086017A/ko not_active Withdrawn
- 2017-12-01 JP JP2019529156A patent/JP2020500866A/ja not_active Ceased
- 2017-12-01 AU AU2017367714A patent/AU2017367714B2/en not_active Ceased
- 2017-12-01 WO PCT/US2017/064116 patent/WO2018102634A1/en not_active Ceased
- 2017-12-01 BR BR112019011074-7A patent/BR112019011074B1/pt not_active IP Right Cessation
- 2017-12-01 MX MX2019006449A patent/MX384729B/es unknown
- 2017-12-01 RU RU2019116590A patent/RU2749043C2/ru active
- 2017-12-01 EP EP17876015.3A patent/EP3548031B1/en active Active
- 2017-12-01 CN CN201780074646.6A patent/CN110062627A/zh active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US20200017524A1 (en) | 2020-01-16 |
| MX384729B (es) | 2025-03-14 |
| RU2749043C2 (ru) | 2021-06-03 |
| EP3548031B1 (en) | 2023-07-19 |
| EP3548031A4 (en) | 2020-06-03 |
| AU2017367714A1 (en) | 2019-05-16 |
| MX2019006449A (es) | 2019-09-10 |
| BR112019011074A2 (pt) | 2019-08-20 |
| AU2017367714B2 (en) | 2020-11-12 |
| RU2019116590A (ru) | 2021-01-11 |
| BR112019011074B1 (pt) | 2021-01-19 |
| JP2020500866A (ja) | 2020-01-16 |
| US10934312B2 (en) | 2021-03-02 |
| EP3548031A1 (en) | 2019-10-09 |
| CA3042314A1 (en) | 2018-06-07 |
| CN110062627A (zh) | 2019-07-26 |
| WO2018102634A1 (en) | 2018-06-07 |
| RU2019116590A3 (https=) | 2021-01-26 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20190627 Patent event code: PA01051R01D Comment text: International Patent Application |
|
| PG1501 | Laying open of application | ||
| A201 | Request for examination | ||
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 20201112 Comment text: Request for Examination of Application |
|
| PC1202 | Submission of document of withdrawal before decision of registration |
Comment text: [Withdrawal of Procedure relating to Patent, etc.] Withdrawal (Abandonment) Patent event code: PC12021R01D Patent event date: 20220513 |
|
| WITB | Written withdrawal of application |