JP2005538184A5 - - Google Patents
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- Publication number
- JP2005538184A5 JP2005538184A5 JP2004555293A JP2004555293A JP2005538184A5 JP 2005538184 A5 JP2005538184 A5 JP 2005538184A5 JP 2004555293 A JP2004555293 A JP 2004555293A JP 2004555293 A JP2004555293 A JP 2004555293A JP 2005538184 A5 JP2005538184 A5 JP 2005538184A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- haloalkyl
- independently
- substituents
- optionally 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.)
- Withdrawn
Links
- 125000000217 alkyl group Chemical group 0.000 claims description 90
- 150000001875 compounds Chemical class 0.000 claims description 21
- 150000003839 salts Chemical class 0.000 claims description 11
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 3
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 2
- 125000001424 substituent group Chemical group 0.000 claims 27
- 125000005842 heteroatom Chemical group 0.000 claims 15
- 229910052760 oxygen Inorganic materials 0.000 claims 15
- 229910052717 sulfur Inorganic materials 0.000 claims 15
- 125000003118 aryl group Chemical group 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 125000005843 halogen group Chemical group 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 229920006395 saturated elastomer Polymers 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- -1 —O—C 1-6 haloalkyl Chemical group 0.000 claims 6
- 125000002877 alkyl aryl group Chemical group 0.000 claims 4
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 208000030507 AIDS Diseases 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 108010002459 HIV Integrase Proteins 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 0 *C(c1c[n](CCN(CC2=CC*=CC=C2)C2=O)c2c1O)=O Chemical compound *C(c1c[n](CCN(CC2=CC*=CC=C2)C2=O)c2c1O)=O 0.000 description 1
- 125000001475 halogen functional group Chemical group 0.000 description 1
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 JP2005538184A (ja) | 2005-12-15 |
| JP2005538184A5 true 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=) |
Families Citing this family (11)
| 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 |
| AU2004285449A1 (en) * | 2003-10-20 | 2005-05-12 | Merck & Co., Inc. | Hydroxy pyridopyrrolopyrazine dione compounds useful as HIV integrase inhibitors |
| US7538112B2 (en) * | 2004-05-07 | 2009-05-26 | Merck & Co., Inc. | HIV integrase inhibitors |
| US7476666B2 (en) | 2004-06-09 | 2009-01-13 | Merck & Co., Inc. | HIV integrase inhibitors |
| WO2006129134A1 (en) * | 2005-06-01 | 2006-12-07 | Bioalliance Pharma | Synergic combinations comprising a styrylquinoline compound and other hiv infection therapeutic agents |
| AU2006306355A1 (en) * | 2005-10-27 | 2007-05-03 | Merck & Co., Inc. | HIV integrase inhibitors |
| JP5746032B2 (ja) | 2008-09-19 | 2015-07-08 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | ３，４−ジヒドロ−２Ｈ−ピロロ［１，２−ａ］ピラジン−１−オン誘導体 |
| CA2789457A1 (en) | 2010-02-26 | 2011-09-01 | Susumu Miyazaki | 1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine derivative and use of same as hiv integrase inhibitor |
| CA2870019C (en) | 2012-04-26 | 2020-08-18 | Francis Xavier Tavares | Synthesis of lactams |
| WO2018005865A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Synthesis of n-(heteroaryl)-pyrrolo[3,2-d]pyrimidin-2-amines |
| AU2019325685B2 (en) | 2018-08-24 | 2025-07-24 | Pharmacosmos Holding A/S | Improved synthesis of 1,4-diazaspiro(5.5)undecan-3-one |
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 |
| 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 |
| PL360944A1 (en) | 2000-10-12 | 2004-09-20 | Merck & Co, Inc. | Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors |
| WO2002036734A2 (en) | 2000-10-12 | 2002-05-10 | Merck & Co., Inc. | Aza-and polyaza-naphthalenyl ketones useful as hiv integrase inhibitors |
| 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 |
| 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 AT AT03812013T patent/ATE404563T1/de not_active IP Right Cessation
- 2003-09-10 EP EP03812013A patent/EP1539714B1/en not_active Expired - Lifetime
- 2003-09-10 CA CA002498566A patent/CA2498566A1/en not_active Abandoned
- 2003-09-10 JP JP2004555293A patent/JP2005538184A/ja not_active Withdrawn
- 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 US US10/526,280 patent/US7399763B2/en not_active Expired - Fee Related
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