JP2005538184A - Hivインテグラーゼ阻害剤として有用な8−ヒドロキシ−1−オキソ−テトラヒドロピロロピラジン化合物 - Google Patents
Hivインテグラーゼ阻害剤として有用な8−ヒドロキシ−1−オキソ−テトラヒドロピロロピラジン化合物 Download PDFInfo
- Publication number
- JP2005538184A JP2005538184A JP2004555293A JP2004555293A JP2005538184A JP 2005538184 A JP2005538184 A JP 2005538184A JP 2004555293 A JP2004555293 A JP 2004555293A JP 2004555293 A JP2004555293 A JP 2004555293A JP 2005538184 A JP2005538184 A JP 2005538184A
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- haloalkyl
- independently
- compound
- substituents
- 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- Withdrawn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 *C(C(*)(*)[n](c(*)c1C(*)=O)c2c1O)N(*)C2=O Chemical compound *C(C(*)(*)[n](c(*)c1C(*)=O)c2c1O)N(*)C2=O 0.000 description 1
- AJZGFFKDLABHDD-UHFFFAOYSA-N C1CNSCC1 Chemical compound C1CNSCC1 AJZGFFKDLABHDD-UHFFFAOYSA-N 0.000 description 1
- UETBHOKUPRJQBQ-UHFFFAOYSA-N C1CNSNC1 Chemical compound C1CNSNC1 UETBHOKUPRJQBQ-UHFFFAOYSA-N 0.000 description 1
- BNBQRQQYDMDJAH-UHFFFAOYSA-N C1Oc2ccccc2OC1 Chemical compound C1Oc2ccccc2OC1 BNBQRQQYDMDJAH-UHFFFAOYSA-N 0.000 description 1
- KJCIMSSFGUGTGA-UHFFFAOYSA-N CN(CCNC1)C1=O Chemical compound CN(CCNC1)C1=O KJCIMSSFGUGTGA-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
-
- 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
-
- 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)
- Public Health (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)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (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 |
|---|---|---|---|
| US40974502P | 2002-09-11 | 2002-09-11 | |
| PCT/US2003/028363 WO2004047725A2 (en) | 2002-09-11 | 2003-09-10 | 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as hiv integrase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005538184A true JP2005538184A (ja) | 2005-12-15 |
| JP2005538184A5 JP2005538184A5 (https=) | 2006-10-19 |
Family
ID=32393259
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004555293A Withdrawn JP2005538184A (ja) | 2002-09-11 | 2003-09-10 | Hivインテグラーゼ阻害剤として有用な8−ヒドロキシ−1−オキソ−テトラヒドロピロロピラジン化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US7399763B2 (https=) |
| EP (1) | EP1539714B1 (https=) |
| JP (1) | JP2005538184A (https=) |
| AT (1) | ATE404563T1 (https=) |
| CA (1) | CA2498566A1 (https=) |
| DE (1) | DE60322919D1 (https=) |
| WO (1) | WO2004047725A2 (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4824673B2 (ja) * | 2004-05-07 | 2011-11-30 | メルク・シャープ・エンド・ドーム・コーポレイション | Hivインテグラーゼ阻害剤 |
| JP2019520380A (ja) * | 2016-07-01 | 2019-07-18 | ジー1 セラピューティクス, インコーポレイテッド | N−(ヘテロアリール)−ピロロ[3,2−d]ピリミジン−2−アミンの合成 |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2498111A1 (en) * | 2002-09-11 | 2004-03-25 | Merck & Co., Inc. | Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors |
| CA2542047A1 (en) * | 2003-10-20 | 2005-05-12 | Merck & Co., Inc. | Hydroxy pyridopyrrolopyrazine dione compounds useful as hiv integrase inhibitors |
| US7476666B2 (en) | 2004-06-09 | 2009-01-13 | Merck & Co., Inc. | HIV integrase inhibitors |
| US20080280849A1 (en) * | 2005-06-01 | 2008-11-13 | Herve Leh | Synergic Combinations Comprising a Quinoline Compound and Other Hiv Infection Therapeutic Agents |
| JP2009513640A (ja) * | 2005-10-27 | 2009-04-02 | メルク エンド カムパニー インコーポレーテッド | Hivインテグラーゼインヒビター |
| WO2010031816A1 (en) | 2008-09-19 | 2010-03-25 | Nerviano Medical Sciences S.R.L. | 3,4 DIHYDRO-2H-PYRROLO[1,2-a]PYRAZIN-1-ONE DERIVATIVES |
| PE20130010A1 (es) | 2010-02-26 | 2013-02-05 | Japan Tobacco Inc | Derivado de 1,3,4,8-tetrahidro-2h-pirido[1,2-a]pirazina como inhibidor de la integrasa del vih |
| EP2841417A1 (en) | 2012-04-26 | 2015-03-04 | Francis Xavier Tavares | Synthesis of lactams |
| RS67557B1 (sr) | 2018-08-24 | 2026-01-30 | Pharmacosmos Holding As | Unapređena sinteza 1,4-diazaspiro[5.5]undekan-3-ona |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL101860A0 (en) * | 1991-05-31 | 1992-12-30 | Ici Plc | Heterocyclic derivatives |
| US5821241A (en) * | 1994-02-22 | 1998-10-13 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| WO2000000478A1 (en) * | 1998-06-26 | 2000-01-06 | Bristol-Myers Squibb Pharma Company | Substituted quinoxalin-2(1h)-ones useful as hiv reverse transcriptase inhibitors |
| CA2425440C (en) | 2000-10-12 | 2010-04-13 | Merck & Co., Inc. | Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors |
| JP2004517860A (ja) | 2000-10-12 | 2004-06-17 | メルク エンド カムパニー インコーポレーテッド | Hivインテグラーゼ阻害薬として有用なアザ−およびポリアザ−ナフタレニルカルボキサミド類 |
| JP2004513134A (ja) * | 2000-10-12 | 2004-04-30 | メルク エンド カムパニー インコーポレーテッド | Hivインテグラーゼ阻害薬として有用なアザ−およびポリアザ−ナフタレニルケトン類 |
| US6919351B2 (en) * | 2000-10-12 | 2005-07-19 | Merck & Co., Inc. | Aza-and polyaza-naphthalenyl-carboxamides useful as HIV integrase inhibitors |
| NZ533057A (en) | 2001-10-26 | 2005-11-25 | Angeletti P Ist Richerche Bio | N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase |
| EP1441734B1 (en) | 2001-10-26 | 2007-02-28 | Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A. | Dihydroxypyrimidine carboxamide inhibitors of hiv integrase |
| CA2498111A1 (en) * | 2002-09-11 | 2004-03-25 | Merck & Co., Inc. | Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors |
-
2003
- 2003-09-10 JP JP2004555293A patent/JP2005538184A/ja not_active Withdrawn
- 2003-09-10 EP EP03812013A patent/EP1539714B1/en not_active Expired - Lifetime
- 2003-09-10 US US10/526,280 patent/US7399763B2/en not_active Expired - Fee Related
- 2003-09-10 AT AT03812013T patent/ATE404563T1/de not_active IP Right Cessation
- 2003-09-10 WO PCT/US2003/028363 patent/WO2004047725A2/en not_active Ceased
- 2003-09-10 DE DE60322919T patent/DE60322919D1/de not_active Expired - Lifetime
- 2003-09-10 CA CA002498566A patent/CA2498566A1/en not_active Abandoned
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4824673B2 (ja) * | 2004-05-07 | 2011-11-30 | メルク・シャープ・エンド・ドーム・コーポレイション | Hivインテグラーゼ阻害剤 |
| JP2019520380A (ja) * | 2016-07-01 | 2019-07-18 | ジー1 セラピューティクス, インコーポレイテッド | N−(ヘテロアリール)−ピロロ[3,2−d]ピリミジン−2−アミンの合成 |
| JP7106462B2 (ja) | 2016-07-01 | 2022-07-26 | ジー1 セラピューティクス, インコーポレイテッド | N-(ヘテロアリール)-ピロロ[3,2-d]ピリミジン-2-アミンの合成 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1539714A4 (en) | 2007-04-25 |
| US20050288293A1 (en) | 2005-12-29 |
| EP1539714A2 (en) | 2005-06-15 |
| CA2498566A1 (en) | 2004-06-10 |
| EP1539714B1 (en) | 2008-08-13 |
| ATE404563T1 (de) | 2008-08-15 |
| US7399763B2 (en) | 2008-07-15 |
| WO2004047725A3 (en) | 2004-09-30 |
| AU2003302382A1 (en) | 2004-06-18 |
| WO2004047725A2 (en) | 2004-06-10 |
| DE60322919D1 (de) | 2008-09-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A524 | Written submission of copy of amendment under article 19 pct |
Free format text: JAPANESE INTERMEDIATE CODE: A524 Effective date: 20060831 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20060831 |
|
| A761 | Written withdrawal of application |
Free format text: JAPANESE INTERMEDIATE CODE: A761 Effective date: 20091207 |