JP2007517900A5 - - Google Patents
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- Publication number
- JP2007517900A5 JP2007517900A5 JP2006549524A JP2006549524A JP2007517900A5 JP 2007517900 A5 JP2007517900 A5 JP 2007517900A5 JP 2006549524 A JP2006549524 A JP 2006549524A JP 2006549524 A JP2006549524 A JP 2006549524A JP 2007517900 A5 JP2007517900 A5 JP 2007517900A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- compound
- aryl
- compound according
- 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
- 150000001875 compounds Chemical class 0.000 claims 46
- 238000010276 construction Methods 0.000 claims 12
- -1 alkyl sulfone Chemical class 0.000 claims 9
- 150000002085 enols Chemical class 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 125000000547 substituted alkyl group Chemical group 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 239000000651 prodrug Substances 0.000 claims 8
- 229940002612 prodrug Drugs 0.000 claims 8
- 125000003107 substituted aryl group Chemical group 0.000 claims 8
- ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical group OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical compound [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 claims 6
- 125000006239 protecting group Chemical group 0.000 claims 6
- 229910019142 PO4 Inorganic materials 0.000 claims 5
- 150000001408 amides Chemical class 0.000 claims 5
- 150000002148 esters Chemical class 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 5
- 239000010452 phosphate Substances 0.000 claims 5
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 5
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 5
- IIACRCGMVDHOTQ-UHFFFAOYSA-M sulfamate Chemical compound NS([O-])(=O)=O IIACRCGMVDHOTQ-UHFFFAOYSA-M 0.000 claims 5
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 125000005360 alkyl sulfoxide group Chemical group 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 125000005362 aryl sulfone group Chemical group 0.000 claims 4
- 125000005361 aryl sulfoxide group Chemical group 0.000 claims 4
- 125000005110 aryl thio group Chemical group 0.000 claims 4
- 150000003951 lactams Chemical class 0.000 claims 4
- 150000002596 lactones Chemical class 0.000 claims 4
- 150000002825 nitriles Chemical class 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 229940124530 sulfonamide Drugs 0.000 claims 4
- 150000003456 sulfonamides Chemical class 0.000 claims 4
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims 4
- 208000030507 AIDS Diseases 0.000 claims 3
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000004663 dialkyl amino group Chemical group 0.000 claims 3
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000005208 trialkylammonium group Chemical group 0.000 claims 3
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 125000004419 alkynylene group Chemical group 0.000 claims 2
- 239000003443 antiviral agent Substances 0.000 claims 2
- 125000000732 arylene group Chemical group 0.000 claims 2
- 150000001540 azides Chemical class 0.000 claims 2
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000006835 (C6-C20) arylene group Chemical group 0.000 claims 1
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims 1
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
- BWGNESOTFCXPMA-UHFFFAOYSA-N Dihydrogen disulfide Chemical compound SS BWGNESOTFCXPMA-UHFFFAOYSA-N 0.000 claims 1
- 108010002459 HIV Integrase Proteins 0.000 claims 1
- 229940122440 HIV protease inhibitor Drugs 0.000 claims 1
- UCKMPCXJQFINFW-UHFFFAOYSA-N Sulphide Chemical compound [S-2] UCKMPCXJQFINFW-UHFFFAOYSA-N 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 150000001350 alkyl halides Chemical class 0.000 claims 1
- 150000008052 alkyl sulfonates Chemical class 0.000 claims 1
- 150000001356 alkyl thiols Chemical class 0.000 claims 1
- 229960005475 antiinfective agent Drugs 0.000 claims 1
- 239000004599 antimicrobial Substances 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 150000007942 carboxylates Chemical class 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000004030 hiv protease inhibitor Substances 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 229940121354 immunomodulator Drugs 0.000 claims 1
- 230000002584 immunomodulator Effects 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 150000003457 sulfones Chemical class 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 150000003573 thiols Chemical class 0.000 claims 1
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 1
- 0 CCCC(*)(C(C)(CC)C(C)(*)CC)C(C)(C#CC)N*C(C)(*)* Chemical compound CCCC(*)(C(C)(CC)C(C)(*)CC)C(C)(C#CC)N*C(C)(*)* 0.000 description 4
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US53601004P | 2004-01-12 | 2004-01-12 | |
| PCT/US2005/000815 WO2005070901A2 (en) | 2004-01-12 | 2005-01-11 | Pyrimidyl phosphonate antiviral compounds and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007517900A JP2007517900A (ja) | 2007-07-05 |
| JP2007517900A5 true JP2007517900A5 (https=) | 2008-02-07 |
Family
ID=34806976
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006549524A Pending JP2007517900A (ja) | 2004-01-12 | 2005-01-11 | ピリミジンホスホネート抗ウイルス化合物および使用方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20050282839A1 (https=) |
| EP (1) | EP1711476A2 (https=) |
| JP (1) | JP2007517900A (https=) |
| KR (1) | KR20060124701A (https=) |
| CN (1) | CN1934093A (https=) |
| AU (1) | AU2005206511A1 (https=) |
| BR (1) | BRPI0506786A (https=) |
| CA (1) | CA2552584A1 (https=) |
| MX (1) | MXPA06007906A (https=) |
| WO (1) | WO2005070901A2 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004062613A2 (en) | 2003-01-13 | 2004-07-29 | Bristol-Myers Squibb Company | Hiv integrase inhibitors |
| 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 |
| CA2616314A1 (en) * | 2005-07-27 | 2007-02-01 | Gilead Sciences, Inc. | Antiviral phosphonate conjugates for inhibition of hiv |
| US20070129379A1 (en) * | 2005-12-01 | 2007-06-07 | Bristol-Myers Squibb Company | Hiv integrase inhibitors |
| US7763630B2 (en) | 2007-06-06 | 2010-07-27 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US8143244B2 (en) | 2009-02-26 | 2012-03-27 | Bristol-Myers Squibb Company | Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors |
| EP2669290A1 (en) | 2009-03-02 | 2013-12-04 | Alnylam Pharmaceuticals Inc. | Nucleic Acid Chemical Modifications |
| US8383639B2 (en) | 2009-10-15 | 2013-02-26 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| WO2011123621A2 (en) | 2010-04-01 | 2011-10-06 | Alnylam Pharmaceuticals Inc. | 2' and 5' modified monomers and oligonucleotides |
| EP4556010A3 (en) | 2011-11-30 | 2025-07-23 | Emory University | Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae |
| KR20150039832A (ko) | 2012-08-06 | 2015-04-13 | 사피라 파르마슈티칼즈 게엠베하 | 디하이드록시피리미딘 탄산 유도체 및 바이러스성 질환의 치료, 개선 또는 예방에서의 이의 용도 |
| JO3470B1 (ar) | 2012-10-08 | 2020-07-05 | Merck Sharp & Dohme | مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv |
| WO2015153304A1 (en) | 2014-04-01 | 2015-10-08 | Merck Sharp & Dohme Corp. | Prodrugs of hiv reverse transcriptase inhibitors |
| DK3236972T3 (en) | 2014-12-26 | 2021-10-04 | Univ Emory | Antivirale N4-hydroxycytidin-derivativer |
| JP6804790B1 (ja) | 2017-12-07 | 2020-12-23 | エモリー ユニバーシティー | Ｎ４−ヒドロキシシチジンおよび誘導体ならびにそれらに関連する抗ウイルス用途 |
Family Cites Families (14)
| 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 |
| 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 |
| US5798340A (en) * | 1993-09-17 | 1998-08-25 | Gilead Sciences, Inc. | Nucleotide analogs |
| US6312662B1 (en) * | 1998-03-06 | 2001-11-06 | Metabasis Therapeutics, Inc. | Prodrugs phosphorus-containing compounds |
| AU3118200A (en) * | 1998-12-14 | 2000-07-03 | Merck & Co., Inc. | Hiv integrase inhibitors |
| US6245806B1 (en) * | 1999-08-03 | 2001-06-12 | Merck & Co., Inc. | HIV integrase inhibitors |
| WO2001027309A1 (en) * | 1999-10-13 | 2001-04-19 | Merck & Co., Inc. | Hiv integrase inhibitors |
| 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 |
| NZ533057A (en) * | 2001-10-26 | 2005-11-25 | Angeletti P Ist Richerche Bio | N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase |
| AU2003231765B9 (en) * | 2002-04-26 | 2010-01-28 | Gilead Sciences, Inc. | Cellular accumulation of phosphonate analogs of HIV protease inhibitor compounds and the compounds as such |
| 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 |
| TW200526635A (en) * | 2003-12-22 | 2005-08-16 | Shionogi & Co | Hydroxypyrimidinone derivative having HIV integrase inhibitory activity |
-
2005
- 2005-01-11 MX MXPA06007906A patent/MXPA06007906A/es unknown
- 2005-01-11 JP JP2006549524A patent/JP2007517900A/ja active Pending
- 2005-01-11 BR BRPI0506786-3A patent/BRPI0506786A/pt not_active IP Right Cessation
- 2005-01-11 US US11/033,422 patent/US20050282839A1/en not_active Abandoned
- 2005-01-11 EP EP05705460A patent/EP1711476A2/en not_active Withdrawn
- 2005-01-11 WO PCT/US2005/000815 patent/WO2005070901A2/en not_active Ceased
- 2005-01-11 CN CNA2005800022601A patent/CN1934093A/zh active Pending
- 2005-01-11 KR KR1020067016388A patent/KR20060124701A/ko not_active Ceased
- 2005-01-11 AU AU2005206511A patent/AU2005206511A1/en not_active Abandoned
- 2005-01-11 CA CA002552584A patent/CA2552584A1/en not_active Abandoned
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