JP2011515412A - Hivインテグラーゼ阻害剤としての架橋ヘテロ環 - Google Patents
Hivインテグラーゼ阻害剤としての架橋ヘテロ環 Download PDFInfo
- Publication number
- JP2011515412A JP2011515412A JP2011500942A JP2011500942A JP2011515412A JP 2011515412 A JP2011515412 A JP 2011515412A JP 2011500942 A JP2011500942 A JP 2011500942A JP 2011500942 A JP2011500942 A JP 2011500942A JP 2011515412 A JP2011515412 A JP 2011515412A
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- JP
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- Prior art keywords
- alkyl
- mmol
- hydroxy
- methyl
- alkoxy
- 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.)
- Pending
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- 0 *OCC(CC1)OCC1=O Chemical compound *OCC(CC1)OCC1=O 0.000 description 7
- WSDQKZFAVSJGHU-UHFFFAOYSA-N CC(C)(C)OC(N(C)CCF)=O Chemical compound CC(C)(C)OC(N(C)CCF)=O WSDQKZFAVSJGHU-UHFFFAOYSA-N 0.000 description 1
- IAVATLFZOHRTLU-UHFFFAOYSA-N CC(C)(C)[S+](C)OCC(CC1)CCC1(C#N)OCCO Chemical compound CC(C)(C)[S+](C)OCC(CC1)CCC1(C#N)OCCO IAVATLFZOHRTLU-UHFFFAOYSA-N 0.000 description 1
- LTKJSDFLXHVZEJ-UHFFFAOYSA-N CC(C)(C)[Si+](C)(C)OCC(CC1)CCC1(C(NO)=N)OCCO Chemical compound CC(C)(C)[Si+](C)(C)OCC(CC1)CCC1(C(NO)=N)OCCO LTKJSDFLXHVZEJ-UHFFFAOYSA-N 0.000 description 1
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- PSSMFMZCZXVWGA-UHFFFAOYSA-N CS(N(CCC1)C1C(NC(CC1)(CCC1CN1C2=O)C1=NC(C(NCc(cc1)ccc1F)=O)=C2O)=O)(=O)=O Chemical compound CS(N(CCC1)C1C(NC(CC1)(CCC1CN1C2=O)C1=NC(C(NCc(cc1)ccc1F)=O)=C2O)=O)(=O)=O PSSMFMZCZXVWGA-UHFFFAOYSA-N 0.000 description 1
- RUUXVDAELZGGJB-UHFFFAOYSA-N Cc(cc(CNC(C(N=C(C(CC1)(CC1CC1)NC(C(N(C)C)=O)=O)N1C1=O)=C1OCc1ccccc1)=O)cc1)c1F Chemical compound Cc(cc(CNC(C(N=C(C(CC1)(CC1CC1)NC(C(N(C)C)=O)=O)N1C1=O)=C1OCc1ccccc1)=O)cc1)c1F RUUXVDAELZGGJB-UHFFFAOYSA-N 0.000 description 1
- KLBONGSBWPFKRL-UHFFFAOYSA-N Cc(cc(CNC(C(N=C(C(CC1)(CCC1C1)N(C)C(C(N(C)CCOC)=O)=O)N1C1=O)=C1O)=O)cc1)c1F Chemical compound Cc(cc(CNC(C(N=C(C(CC1)(CCC1C1)N(C)C(C(N(C)CCOC)=O)=O)N1C1=O)=C1O)=O)cc1)c1F KLBONGSBWPFKRL-UHFFFAOYSA-N 0.000 description 1
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- XRVCGKHNNQWAIL-UHFFFAOYSA-N Cc(cc(CNC(C(N=C(C(CC1)(CCC1C1)NC(C(N(C)CCOC)=O)=O)N1C1=O)=C1O)=O)cc1)c1F Chemical compound Cc(cc(CNC(C(N=C(C(CC1)(CCC1C1)NC(C(N(C)CCOC)=O)=O)N1C1=O)=C1O)=O)cc1)c1F XRVCGKHNNQWAIL-UHFFFAOYSA-N 0.000 description 1
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- UASQDNHYROZFQS-UHFFFAOYSA-N NC(C(N=C(C(CC1)(COC1C1)NC(OCc2ccccc2)=O)N1C1=O)=C1O)=O Chemical compound NC(C(N=C(C(CC1)(COC1C1)NC(OCc2ccccc2)=O)N1C1=O)=C1O)=O UASQDNHYROZFQS-UHFFFAOYSA-N 0.000 description 1
- XUYHFYZAEAUBDY-UHFFFAOYSA-N NC(COC(C1)CN2C3=O)C1CC2=NC(C(N)=O)=C3O Chemical compound NC(COC(C1)CN2C3=O)C1CC2=NC(C(N)=O)=C3O XUYHFYZAEAUBDY-UHFFFAOYSA-N 0.000 description 1
- VRSKZZIXPDVEFN-UHFFFAOYSA-N NCc(cc1)cc(C#N)c1F Chemical compound NCc(cc1)cc(C#N)c1F VRSKZZIXPDVEFN-UHFFFAOYSA-N 0.000 description 1
- DBCIDXBUENCDAD-UHFFFAOYSA-N OC(C1)CN1C(C(NC(CC1)(CCC1CN1C2=O)C1=NC(C(NCc(cc1)ccc1F)=O)=C2O)=O)=O Chemical compound OC(C1)CN1C(C(NC(CC1)(CCC1CN1C2=O)C1=NC(C(NCc(cc1)ccc1F)=O)=C2O)=O)=O DBCIDXBUENCDAD-UHFFFAOYSA-N 0.000 description 1
- RFXLAUDCFBPSME-UHFFFAOYSA-N OC1=C(C(NCc(cc2)ccc2F)=O)N=C(C(CC2)(CC2CC2)NC(OCc3ccccc3)=O)N2C1=O Chemical compound OC1=C(C(NCc(cc2)ccc2F)=O)N=C(C(CC2)(CC2CC2)NC(OCc3ccccc3)=O)N2C1=O RFXLAUDCFBPSME-UHFFFAOYSA-N 0.000 description 1
- AIUQRLQMVWINDY-UHFFFAOYSA-N OC1=C(C(NCc(cc2)ccc2F)=O)N=C(C(CC2)(CCC2C2)NC(C(N(CC3)CCC3F)=O)=O)N2C1=O Chemical compound OC1=C(C(NCc(cc2)ccc2F)=O)N=C(C(CC2)(CCC2C2)NC(C(N(CC3)CCC3F)=O)=O)N2C1=O AIUQRLQMVWINDY-UHFFFAOYSA-N 0.000 description 1
- ORQKXFPPKGYWKR-UHFFFAOYSA-N OC1=C(C(NCc(cc2)ccc2F)=O)N=C(C(CC2)(CCC2C2)NC(C(N3CCNCC3)=O)=O)N2C1=O Chemical compound OC1=C(C(NCc(cc2)ccc2F)=O)N=C(C(CC2)(CCC2C2)NC(C(N3CCNCC3)=O)=O)N2C1=O ORQKXFPPKGYWKR-UHFFFAOYSA-N 0.000 description 1
- DBJBJJATLGKWQF-UHFFFAOYSA-N OC1=C(C(NCc(cc2)ccc2F)=O)N=C(C(CC2)(CCC2C2)NC(NC(c3ccccc3)=O)=S)N2C1=O Chemical compound OC1=C(C(NCc(cc2)ccc2F)=O)N=C(C(CC2)(CCC2C2)NC(NC(c3ccccc3)=O)=S)N2C1=O DBJBJJATLGKWQF-UHFFFAOYSA-N 0.000 description 1
- KQULNRLGKUTZFQ-UHFFFAOYSA-N OC1=C(C(NCc(cc2)ccc2F)=O)N=C(C(CC2)(CCC2C2)NC(c3cc(OCC(F)(F)F)ncc3)=O)N2C1=O Chemical compound OC1=C(C(NCc(cc2)ccc2F)=O)N=C(C(CC2)(CCC2C2)NC(c3cc(OCC(F)(F)F)ncc3)=O)N2C1=O KQULNRLGKUTZFQ-UHFFFAOYSA-N 0.000 description 1
- RPOCHGCJTZOZDK-UHFFFAOYSA-N OC1=C(C(NCc(cc2)ccc2F)=O)N=C(C(CC2)(CCC2C2)NC(c3ccncc3)=O)N2C1=O Chemical compound OC1=C(C(NCc(cc2)ccc2F)=O)N=C(C(CC2)(CCC2C2)NC(c3ccncc3)=O)N2C1=O RPOCHGCJTZOZDK-UHFFFAOYSA-N 0.000 description 1
- CEKRLLCESSAGOL-UHFFFAOYSA-N OCCC(C1)OCC1OCc1ccccc1 Chemical compound OCCC(C1)OCC1OCc1ccccc1 CEKRLLCESSAGOL-UHFFFAOYSA-N 0.000 description 1
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
- C07D498/18—Bridged 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
- 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
- C07D471/02—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 two hetero rings
- C07D471/08—Bridged 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
- C07D471/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/12—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings
- C07D493/18—Bridged systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Tropical Medicine & Parasitology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US3772908P | 2008-03-19 | 2008-03-19 | |
| US61/037,729 | 2008-03-19 | ||
| US12/406,268 | 2009-03-18 | ||
| US12/406,268 US8129398B2 (en) | 2008-03-19 | 2009-03-18 | HIV integrase inhibitors |
| PCT/US2009/037596 WO2009117540A1 (en) | 2008-03-19 | 2009-03-19 | Bridged heterocycles as hiv integrase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011515412A true JP2011515412A (ja) | 2011-05-19 |
| JP2011515412A5 JP2011515412A5 (enExample) | 2012-05-10 |
Family
ID=40863725
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011500942A Pending JP2011515412A (ja) | 2008-03-19 | 2009-03-19 | Hivインテグラーゼ阻害剤としての架橋ヘテロ環 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8129398B2 (enExample) |
| EP (1) | EP2280981B8 (enExample) |
| JP (1) | JP2011515412A (enExample) |
| KR (1) | KR20100137522A (enExample) |
| CN (1) | CN102036996A (enExample) |
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| JP2018529714A (ja) * | 2015-09-30 | 2018-10-11 | ギリアード サイエンシーズ, インコーポレイテッド | Hivの処置のための化合物および組合せ物 |
| JP2022526895A (ja) * | 2019-03-22 | 2022-05-27 | ギリアード サイエンシーズ, インコーポレイテッド | 有橋三環式カルバモイルピリドン化合物およびその薬学的使用 |
| JP2023033640A (ja) * | 2019-03-22 | 2023-03-10 | ギリアード サイエンシーズ, インコーポレイテッド | 有橋三環式カルバモイルピリドン化合物およびその薬学的使用 |
| JP7265647B2 (ja) | 2019-03-22 | 2023-04-26 | ギリアード サイエンシーズ, インコーポレイテッド | 有橋三環式カルバモイルピリドン化合物およびその薬学的使用 |
| US12227520B2 (en) | 2019-03-22 | 2025-02-18 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use |
| JP7710476B2 (ja) | 2019-03-22 | 2025-07-18 | ギリアード サイエンシーズ, インコーポレイテッド | 有橋三環式カルバモイルピリドン化合物およびその薬学的使用 |
| US11697652B2 (en) | 2020-02-24 | 2023-07-11 | Gilead Sciences, Inc. | Tetracyclic compounds and uses thereof |
| US12421235B2 (en) | 2020-09-30 | 2025-09-23 | Gilead Sciences, Inc. | Bridged tricyclic carbamoylpyridone compounds and uses thereof |
| US11613546B2 (en) | 2021-01-19 | 2023-03-28 | Gilead Sciences, Inc. | Substituted pyridotriazine compounds and uses thereof |
| US11897892B2 (en) | 2021-01-19 | 2024-02-13 | Gilead Sciences, Inc. | Substituted pyridotriazine compounds and uses thereof |
| US12187734B2 (en) | 2021-01-19 | 2025-01-07 | Gilead Sciences, Inc. | Substituted pyridotriazine compounds and uses thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| IL208068A0 (en) | 2010-12-30 |
| US20090253677A1 (en) | 2009-10-08 |
| NZ588031A (en) | 2011-12-22 |
| CN102036996A (zh) | 2011-04-27 |
| KR20100137522A (ko) | 2010-12-30 |
| AU2009225577A1 (en) | 2009-09-24 |
| CO6331439A2 (es) | 2011-10-20 |
| EP2280981B1 (en) | 2014-04-23 |
| CA2718950A1 (en) | 2009-09-24 |
| EP2280981B8 (en) | 2014-09-17 |
| MX2010009995A (es) | 2010-09-30 |
| BRPI0910307A2 (pt) | 2019-09-24 |
| US8129398B2 (en) | 2012-03-06 |
| WO2009117540A1 (en) | 2009-09-24 |
| EP2280981A1 (en) | 2011-02-09 |
| EA201001508A1 (ru) | 2011-04-29 |
| ZA201006589B (en) | 2012-02-29 |
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