JP2009537546A - インテグラーゼ阻害剤 - Google Patents
インテグラーゼ阻害剤 Download PDFInfo
- Publication number
- JP2009537546A JP2009537546A JP2009511069A JP2009511069A JP2009537546A JP 2009537546 A JP2009537546 A JP 2009537546A JP 2009511069 A JP2009511069 A JP 2009511069A JP 2009511069 A JP2009511069 A JP 2009511069A JP 2009537546 A JP2009537546 A JP 2009537546A
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- mmol
- optionally substituted
- substituted
- 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
Links
- 0 C*C(C(C)=*c1c(**)c(OC)c(C(*(*)[C@]2NC)=O)c2c1*O)=C Chemical compound C*C(C(C)=*c1c(**)c(OC)c(C(*(*)[C@]2NC)=O)c2c1*O)=C 0.000 description 19
- DYMKJALBMHDKNT-UHFFFAOYSA-N CC(C)OC(c1ncc(Cc(cc2)ccc2F)cc1C(O)=O)=O Chemical compound CC(C)OC(c1ncc(Cc(cc2)ccc2F)cc1C(O)=O)=O DYMKJALBMHDKNT-UHFFFAOYSA-N 0.000 description 2
- LUJGLFMPEZIRRP-UHFFFAOYSA-N CCCc(cc1)ccc1F Chemical compound CCCc(cc1)ccc1F LUJGLFMPEZIRRP-UHFFFAOYSA-N 0.000 description 2
- LIEVTEBVBGNLEO-UHFFFAOYSA-N CC(C)OC(c(ncc(Cc(cc1Cl)ccc1F)c1)c1C(OC)=O)=O Chemical compound CC(C)OC(c(ncc(Cc(cc1Cl)ccc1F)c1)c1C(OC)=O)=O LIEVTEBVBGNLEO-UHFFFAOYSA-N 0.000 description 1
- OAPDPORYXWQVJE-UHFFFAOYSA-N CCCc(cc1)ccc1N Chemical compound CCCc(cc1)ccc1N OAPDPORYXWQVJE-UHFFFAOYSA-N 0.000 description 1
- XKFLYUDCMJSTCJ-ASGQQMQCSA-N CC[C@H](C)NC(/C(/O)=C(\C(CN1C)=C)/C1=O)=C Chemical compound CC[C@H](C)NC(/C(/O)=C(\C(CN1C)=C)/C1=O)=C XKFLYUDCMJSTCJ-ASGQQMQCSA-N 0.000 description 1
- OITAADMDRNNCNH-UHFFFAOYSA-N CN(C)C(C(CNCCO)=C)=C Chemical compound CN(C)C(C(CNCCO)=C)=C OITAADMDRNNCNH-UHFFFAOYSA-N 0.000 description 1
- NGGALWTVGOHXCY-UHFFFAOYSA-N COc1cc(OC)c(CN(C(c(c2c(c3c4cc(Cc(cc5)ccc5F)cn3)OC(c3ccccc3)c3ccccc3)c4OCC[Si](C)(C)C)=O)C2=O)cc1 Chemical compound COc1cc(OC)c(CN(C(c(c2c(c3c4cc(Cc(cc5)ccc5F)cn3)OC(c3ccccc3)c3ccccc3)c4OCC[Si](C)(C)C)=O)C2=O)cc1 NGGALWTVGOHXCY-UHFFFAOYSA-N 0.000 description 1
- BPBGNSOQXAGHDT-UHFFFAOYSA-N COc1cc(OC)c(CN(C(c2c3c(O)c4ncc(Cc(cc5Cl)ccc5F)cc4c2O)=O)C3=O)cc1 Chemical compound COc1cc(OC)c(CN(C(c2c3c(O)c4ncc(Cc(cc5Cl)ccc5F)cc4c2O)=O)C3=O)cc1 BPBGNSOQXAGHDT-UHFFFAOYSA-N 0.000 description 1
- WRWPPGUCZBJXKX-UHFFFAOYSA-N Cc(cc1)ccc1F Chemical compound Cc(cc1)ccc1F WRWPPGUCZBJXKX-UHFFFAOYSA-N 0.000 description 1
- UVCKCDNJULSEGQ-UHFFFAOYSA-N Nc(c1c(c(O)c2C(N3Cc(cc4)ccc4F)=O)ncc(Br)c1)c2C3=O Chemical compound Nc(c1c(c(O)c2C(N3Cc(cc4)ccc4F)=O)ncc(Br)c1)c2C3=O UVCKCDNJULSEGQ-UHFFFAOYSA-N 0.000 description 1
- BSJVJEPKOVLENN-UHFFFAOYSA-N O=C(c1cc(Cc(cc2)ccc2[FH+])cnc11)OC1=O Chemical compound O=C(c1cc(Cc(cc2)ccc2[FH+])cnc11)OC1=O BSJVJEPKOVLENN-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- C07D471/04—Ortho-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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Immunology (AREA)
- Virology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Communicable Diseases (AREA)
- Oncology (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 (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US80102006P | 2006-05-16 | 2006-05-16 | |
| PCT/US2007/011851 WO2007136714A2 (en) | 2006-05-16 | 2007-05-16 | Integrase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009537546A true JP2009537546A (ja) | 2009-10-29 |
| JP2009537546A5 JP2009537546A5 (https=) | 2011-06-16 |
Family
ID=38573219
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009511069A Pending JP2009537546A (ja) | 2006-05-16 | 2007-05-16 | インテグラーゼ阻害剤 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US20090306054A1 (https=) |
| EP (1) | EP2066670A2 (https=) |
| JP (1) | JP2009537546A (https=) |
| AU (1) | AU2007254190A1 (https=) |
| CA (1) | CA2651579A1 (https=) |
| NZ (1) | NZ572367A (https=) |
| WO (1) | WO2007136714A2 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090291921A1 (en) * | 2007-11-20 | 2009-11-26 | Gilead Sciences, Inc. | Integrase inhibitors |
| US20100233270A1 (en) | 2009-01-08 | 2010-09-16 | Northwestern University | Delivery of Oligonucleotide-Functionalized Nanoparticles |
| US9018227B2 (en) | 2010-03-19 | 2015-04-28 | Indiana State University | Nicotinic acetylcholine receptor agonists |
| CA2830027C (en) | 2011-03-31 | 2016-04-26 | Pfizer Inc. | Novel bicyclic pyridinones |
| ES3018133T3 (en) | 2011-11-30 | 2025-05-14 | Univ Emory | Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae |
| UA110688C2 (uk) | 2012-09-21 | 2016-01-25 | Пфайзер Інк. | Біциклічні піридинони |
| MX368391B (es) | 2015-02-03 | 2019-09-30 | Pfizer | Ciclopropabenzofuranil-piridopirazindionas novedosas. |
| CN106632397B (zh) * | 2016-12-01 | 2019-03-22 | 齐鲁天和惠世制药有限公司 | 一种6α-溴青霉烷-3α-羧酸二苯甲酯-1β-氧化物的制备方法 |
| LT3483164T (lt) | 2017-03-20 | 2020-05-11 | Forma Therapeutics, Inc. | Pirolpirolo kompozicijos kaip piruvato kinazės (pkr) aktyvatoriai |
| EP3852791B1 (en) | 2018-09-19 | 2024-07-03 | Novo Nordisk Health Care AG | Activating pyruvate kinase r |
| EP3853206B1 (en) | 2018-09-19 | 2024-04-10 | Novo Nordisk Health Care AG | Treating sickle cell disease with a pyruvate kinase r activating compound |
| CN112142713A (zh) * | 2019-06-27 | 2020-12-29 | 山东润博生物科技有限公司 | 一种咪草烟的合成方法 |
| CN112142712A (zh) * | 2019-06-27 | 2020-12-29 | 山东润博生物科技有限公司 | 一种甲基咪草烟的合成方法 |
| CN112142714A (zh) * | 2019-06-27 | 2020-12-29 | 山东润博生物科技有限公司 | 一种灭草烟的合成方法 |
| HRP20251148T1 (hr) | 2019-09-19 | 2025-11-21 | Novo Nordisk Health Care Ag | Pripravci koji aktiviraju piruvat-kinazu r (pkr) |
| US12128035B2 (en) | 2021-03-19 | 2024-10-29 | Novo Nordisk Health Care Ag | Activating pyruvate kinase R |
| CN116675684B (zh) * | 2023-08-02 | 2023-11-07 | 上海翰森生物医药科技有限公司 | 含炔基稠环类衍生物拮抗剂、其制备方法和应用 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004024693A1 (ja) * | 2002-08-13 | 2004-03-25 | Shionogi & Co., Ltd. | Hivインテグラーゼ阻害活性を有するヘテロ環化合物 |
| WO2004096807A2 (en) * | 2003-04-28 | 2004-11-11 | Tibotec Pharmaceuticals Ltd. | Hiv integrase inhibitors |
| WO2005117904A2 (en) * | 2004-04-14 | 2005-12-15 | Gilead Sciences, Inc. | Phosphonate analogs of hiv integrase inhibitor compounds |
| JP2006514099A (ja) * | 2002-10-16 | 2006-04-27 | ギリアード サイエンシーズ, インコーポレイテッド | 組織化前の三環系インテグラーゼインヒビター化合物 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4816570A (en) * | 1982-11-30 | 1989-03-28 | The Board Of Regents Of The University Of Texas System | Biologically reversible phosphate and phosphonate protective groups |
| US4968788A (en) * | 1986-04-04 | 1990-11-06 | Board Of Regents, The University Of Texas System | Biologically reversible phosphate and phosphonate protective gruops |
| EP0533833B1 (en) | 1990-06-13 | 1995-12-20 | GLAZIER, Arnold | Phosphorous produgs |
| EP0481214B1 (en) * | 1990-09-14 | 1998-06-24 | Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic | Prodrugs of phosphonates |
| US5543523A (en) | 1994-11-15 | 1996-08-06 | Regents Of The University Of Minnesota | Method and intermediates for the synthesis of korupensamines |
| US5683999A (en) * | 1995-03-17 | 1997-11-04 | The Dupont Merck Pharmaceutical Company | Cyclic urea HIV protease inhibitors |
| US6312662B1 (en) * | 1998-03-06 | 2001-11-06 | Metabasis Therapeutics, Inc. | Prodrugs phosphorus-containing compounds |
| AU4225499A (en) | 1998-06-03 | 1999-12-20 | Merck & Co., Inc. | Hiv integrase inhibitors |
| CA2329134A1 (en) | 1998-06-03 | 1999-12-09 | David L. Clark | Hiv integrase inhibitors |
| AU3118200A (en) * | 1998-12-14 | 2000-07-03 | Merck & Co., Inc. | Hiv integrase inhibitors |
| PL348596A1 (en) | 1998-12-25 | 2002-06-03 | Shionogi & Co | Aromatic heterocycle compounds having hiv integrase inhibiting activities |
| TR200202129T2 (tr) | 1999-06-02 | 2003-03-21 | Shionogi & Co., Ltd. | Yeni ikameli propenon türevlerinin hazırlanması için prosesler. |
| AU5880600A (en) | 1999-06-25 | 2001-01-31 | Merck & Co., Inc. | 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof |
| US6245806B1 (en) * | 1999-08-03 | 2001-06-12 | Merck & Co., Inc. | HIV integrase inhibitors |
| AU8009900A (en) * | 1999-10-13 | 2001-04-23 | Merck & Co., Inc. | Hiv integrase inhibitors |
| EP1326611B1 (en) | 2000-10-12 | 2007-06-13 | Merck & Co., Inc. | Aza- and polyaza-naphthalenyl-carboxamides useful as hiv integrase inhibitors |
| ATE345129T1 (de) | 2000-10-12 | 2006-12-15 | Merck & Co Inc | Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer |
| WO2002036734A2 (en) | 2000-10-12 | 2002-05-10 | Merck & Co., Inc. | Aza-and polyaza-naphthalenyl ketones useful as hiv integrase inhibitors |
| PL360944A1 (en) * | 2000-10-12 | 2004-09-20 | Merck & Co, Inc. | Aza- and polyaza-naphthalenyl carboxamides useful as 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 |
| JP4789144B2 (ja) | 2004-02-04 | 2011-10-12 | 塩野義製薬株式会社 | Hivインテグラーゼ阻害活性を有するナフチリジン誘導体 |
| AR057023A1 (es) * | 2005-05-16 | 2007-11-14 | Gilead Sciences Inc | Compuestos heterociclicos con propiedades inhibidoras de hiv-integrasa |
| WO2007076005A2 (en) * | 2005-12-21 | 2007-07-05 | Gilead Sciences, Inc. | Processes and intermediates useful for preparing integrase inhibitor compounds |
-
2007
- 2007-05-16 AU AU2007254190A patent/AU2007254190A1/en not_active Abandoned
- 2007-05-16 CA CA002651579A patent/CA2651579A1/en not_active Abandoned
- 2007-05-16 EP EP07794999A patent/EP2066670A2/en not_active Withdrawn
- 2007-05-16 NZ NZ572367A patent/NZ572367A/en not_active IP Right Cessation
- 2007-05-16 US US12/299,885 patent/US20090306054A1/en not_active Abandoned
- 2007-05-16 US US11/804,041 patent/US8008287B2/en not_active Expired - Fee Related
- 2007-05-16 WO PCT/US2007/011851 patent/WO2007136714A2/en not_active Ceased
- 2007-05-16 JP JP2009511069A patent/JP2009537546A/ja active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004024693A1 (ja) * | 2002-08-13 | 2004-03-25 | Shionogi & Co., Ltd. | Hivインテグラーゼ阻害活性を有するヘテロ環化合物 |
| JP2006514099A (ja) * | 2002-10-16 | 2006-04-27 | ギリアード サイエンシーズ, インコーポレイテッド | 組織化前の三環系インテグラーゼインヒビター化合物 |
| WO2004096807A2 (en) * | 2003-04-28 | 2004-11-11 | Tibotec Pharmaceuticals Ltd. | Hiv integrase inhibitors |
| WO2005117904A2 (en) * | 2004-04-14 | 2005-12-15 | Gilead Sciences, Inc. | Phosphonate analogs of hiv integrase inhibitor compounds |
Non-Patent Citations (1)
| Title |
|---|
| JPN5009006589; VERSCHUEREN, WIM G.: JOURNAL OF MEDICINAL CHEMISTRY V48 N6, 2005, P1930-1940 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US8008287B2 (en) | 2011-08-30 |
| AU2007254190A1 (en) | 2007-11-29 |
| WO2007136714A2 (en) | 2007-11-29 |
| WO2007136714A3 (en) | 2008-12-18 |
| US20090306054A1 (en) | 2009-12-10 |
| US20080058315A1 (en) | 2008-03-06 |
| EP2066670A2 (en) | 2009-06-10 |
| CA2651579A1 (en) | 2007-11-29 |
| NZ572367A (en) | 2011-09-30 |
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