JP2013504592A5 - - Google Patents
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- Publication number
- JP2013504592A5 JP2013504592A5 JP2012528919A JP2012528919A JP2013504592A5 JP 2013504592 A5 JP2013504592 A5 JP 2013504592A5 JP 2012528919 A JP2012528919 A JP 2012528919A JP 2012528919 A JP2012528919 A JP 2012528919A JP 2013504592 A5 JP2013504592 A5 JP 2013504592A5
- Authority
- JP
- Japan
- Prior art keywords
- oxopurine
- dichlorobenzylamino
- morpholinyl
- unsubstituted
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 25
- -1 4-methoxybutyl Chemical group 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000005843 halogen group Chemical group 0.000 claims 10
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 9
- QADPKINXOWMXKE-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-(5-morpholin-4-ylpentyl)-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCCCCN1CCOCC1)C=N2 QADPKINXOWMXKE-UHFFFAOYSA-N 0.000 claims 6
- FZCPHYJBAMREKV-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-[[2-(morpholin-4-ylmethyl)cyclobutyl]methyl]-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CC1C(CC1)CN1CCOCC1)C=N2 FZCPHYJBAMREKV-UHFFFAOYSA-N 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 238000000034 method Methods 0.000 claims 5
- HVUNHTWEGZXFIG-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-(4-morpholin-4-ylbutyl)-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCCCN1CCOCC1)C=N2 HVUNHTWEGZXFIG-UHFFFAOYSA-N 0.000 claims 4
- 241000193163 Clostridioides difficile Species 0.000 claims 4
- 125000001309 chloro group Chemical group Cl* 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 3
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 3
- OJNXQNDIPQEMCP-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-(4-piperidin-1-ylbutyl)-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCCCN1CCCCC1)C=N2 OJNXQNDIPQEMCP-UHFFFAOYSA-N 0.000 claims 3
- HYKBTGWGCOJDME-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-(4-pyrrolidin-1-ylbutyl)-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCCCN1CCCC1)C=N2 HYKBTGWGCOJDME-UHFFFAOYSA-N 0.000 claims 3
- NPELVJUIDRQJNO-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-(5-morpholin-4-ylpentyl)-3h-purin-6-one;hydrochloride Chemical compound Cl.C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCCCCN1CCOCC1)C=N2 NPELVJUIDRQJNO-UHFFFAOYSA-N 0.000 claims 3
- PCSPBXBHMVCJSG-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-(5-piperidin-1-ylpentyl)-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCCCCN1CCCCC1)C=N2 PCSPBXBHMVCJSG-UHFFFAOYSA-N 0.000 claims 3
- GMWZMTWWGPFKTC-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-(5-pyrrolidin-1-ylpentyl)-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCCCCN1CCCC1)C=N2 GMWZMTWWGPFKTC-UHFFFAOYSA-N 0.000 claims 3
- NFYRSHBCDBFCNQ-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-[2-(2-morpholin-4-ylethoxy)ethyl]-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCOCCN1CCOCC1)C=N2 NFYRSHBCDBFCNQ-UHFFFAOYSA-N 0.000 claims 3
- WWEPCYBWHAIGDM-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-[2-(2-piperidin-1-ylethoxy)ethyl]-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCOCCN1CCCCC1)C=N2 WWEPCYBWHAIGDM-UHFFFAOYSA-N 0.000 claims 3
- BEJKZYNWGGPKHL-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-[2-(2-pyrrolidin-1-ylethoxy)ethyl]-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCOCCN1CCCC1)C=N2 BEJKZYNWGGPKHL-UHFFFAOYSA-N 0.000 claims 3
- NVVPCMBWBUAKHQ-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-[[2-(morpholin-4-ylmethyl)cyclobutyl]methyl]-3h-purin-6-one;hydrochloride Chemical compound Cl.C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CC1C(CC1)CN1CCOCC1)C=N2 NVVPCMBWBUAKHQ-UHFFFAOYSA-N 0.000 claims 3
- BYQZUEQWQRKGGY-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-[[2-(morpholin-4-ylmethyl)cyclopentyl]methyl]-3h-purin-6-one;hydrochloride Chemical compound Cl.C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CC1C(CCC1)CN1CCOCC1)C=N2 BYQZUEQWQRKGGY-UHFFFAOYSA-N 0.000 claims 3
- FJXKXCGUXBKOCS-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-[[2-(piperidin-1-ylmethyl)cyclobutyl]methyl]-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CC1C(CC1)CN1CCCCC1)C=N2 FJXKXCGUXBKOCS-UHFFFAOYSA-N 0.000 claims 3
- HQPMHDJADXPDCH-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-[[2-(piperidin-1-ylmethyl)cyclopentyl]methyl]-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CC1C(CCC1)CN1CCCCC1)C=N2 HQPMHDJADXPDCH-UHFFFAOYSA-N 0.000 claims 3
- DUVLHCQQNVUWDR-UHFFFAOYSA-N 7-[2-[2-(azetidin-1-yl)ethoxy]ethyl]-2-[(3,4-dichlorophenyl)methylamino]-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCOCCN1CCC1)C=N2 DUVLHCQQNVUWDR-UHFFFAOYSA-N 0.000 claims 3
- VEPACANBVJRRFH-UHFFFAOYSA-N 7-[4-(azetidin-1-yl)butyl]-2-[(3,4-dichlorophenyl)methylamino]-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCCCN1CCC1)C=N2 VEPACANBVJRRFH-UHFFFAOYSA-N 0.000 claims 3
- WFLFFQCMGDXUBJ-UHFFFAOYSA-N 7-[5-(azetidin-1-yl)pentyl]-2-[(3,4-dichlorophenyl)methylamino]-3h-purin-6-one Chemical compound C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCCCCN1CCC1)C=N2 WFLFFQCMGDXUBJ-UHFFFAOYSA-N 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 3
- 125000002877 alkyl aryl group Chemical group 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 229910002091 carbon monoxide Inorganic materials 0.000 claims 3
- 230000003287 optical effect Effects 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- DWGZFWJMYDGRAP-UHFFFAOYSA-N 2-[(3,4-dichlorophenyl)methylamino]-7-(4-morpholin-4-ylbutyl)-3h-purin-6-one;hydrochloride Chemical compound Cl.C1=C(Cl)C(Cl)=CC=C1CNC(NC1=O)=NC2=C1N(CCCCN1CCOCC1)C=N2 DWGZFWJMYDGRAP-UHFFFAOYSA-N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- SXIFAEWFOJETOA-UHFFFAOYSA-N 4-hydroxy-butyl Chemical group [CH2]CCCO SXIFAEWFOJETOA-UHFFFAOYSA-N 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 206010009887 colitis Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000001963 growth medium Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004205 trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- 125000004951 trihalomethoxy group Chemical group 0.000 claims 1
- 125000004953 trihalomethyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27643609P | 2009-09-11 | 2009-09-11 | |
| US61/276,436 | 2009-09-11 | ||
| PCT/US2010/048379 WO2011031935A1 (en) | 2009-09-11 | 2010-09-10 | Selective antibacterials for clostridium difficile infections |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013504592A JP2013504592A (ja) | 2013-02-07 |
| JP2013504592A5 true JP2013504592A5 (enExample) | 2013-10-31 |
| JP5934647B2 JP5934647B2 (ja) | 2016-06-15 |
Family
ID=43732808
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012528919A Active JP5934647B2 (ja) | 2009-09-11 | 2010-09-10 | クロストリジウム・ディフィシル感染症のための選択的抗菌薬 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8796292B2 (enExample) |
| EP (1) | EP2475252B1 (enExample) |
| JP (1) | JP5934647B2 (enExample) |
| CA (1) | CA2772907C (enExample) |
| WO (1) | WO2011031935A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201509326D0 (en) | 2015-05-29 | 2015-07-15 | Antibio Tx Aps | Novel use |
| US10723741B1 (en) * | 2018-12-21 | 2020-07-28 | Acurx Pharmaceuticals, Llc | DNA polymerase IIIC inhibitors and use thereof |
| WO2022266318A2 (en) * | 2021-06-16 | 2022-12-22 | Acurx Pharmaceuticals Llc | Use of ibezapolstat to promote microbiome health |
| CN117813085A (zh) * | 2021-06-16 | 2024-04-02 | 阿科利斯制药股份有限公司 | 伊贝扎波尔司他用于促进微生物组健康的用途 |
| US20260144796A1 (en) * | 2022-10-17 | 2026-05-28 | Acurx Pharmaceuticals, Inc. | Compounds and Methods for Improving Health |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5516905A (en) | 1994-08-30 | 1996-05-14 | University Of Massachusetts Medical Center | Antibiotic compounds and methods to treat gram-positive bacterial and mycoplasmal infections |
| DE19845153A1 (de) | 1998-10-01 | 2000-04-06 | Merck Patent Gmbh | Imidazo[4,5]-pyridin-4-on-derivate |
| WO2001029010A1 (en) | 1999-10-21 | 2001-04-26 | Merck & Co., Inc. | Gram-positive selective antibacterial compounds, compositions containing such compounds and methods of treatment |
| WO2001028561A1 (en) | 1999-10-21 | 2001-04-26 | Merck & Co., Inc. | Gram-positive selective antibacterial compounds, compositions containing such compounds and methods of treatment |
| WO2001029045A1 (en) | 1999-10-21 | 2001-04-26 | Merck & Co., Inc. | Gram-positive selective antibacterial compounds, compositions containing such compounds and methods of treatment |
| AU2002327182B2 (en) * | 2001-06-15 | 2005-09-15 | Microbiotix, Inc. | Novel heterocyclic antibacterial compounds |
| US6777420B2 (en) | 2001-06-15 | 2004-08-17 | Microbiotix, Inc. | Heterocyclic antibacterial compounds |
| WO2003066586A2 (en) * | 2002-02-08 | 2003-08-14 | Glsynthesis Inc. | Purine and isosteric antibacterial compounds |
| AU2003240545A1 (en) * | 2002-06-06 | 2003-12-22 | Therapeutics Corporation Genome | Use of ramoplanin to treat diseases associated with the use of antibiotics |
| AU2003303953B2 (en) * | 2002-09-10 | 2007-10-04 | Microbiotix, Inc. | Antibacterial pyrazole carboxylic acid hydrazides |
| FR2906244B1 (fr) * | 2006-09-22 | 2010-09-10 | Centre Nat Rech Scient | Nouvelle classe de composes derives de terpene a activite antibiotique, compositions les contenant et utilisations. |
-
2010
- 2010-09-10 WO PCT/US2010/048379 patent/WO2011031935A1/en not_active Ceased
- 2010-09-10 CA CA2772907A patent/CA2772907C/en active Active
- 2010-09-10 US US13/395,296 patent/US8796292B2/en active Active
- 2010-09-10 JP JP2012528919A patent/JP5934647B2/ja active Active
- 2010-09-10 EP EP10816135.7A patent/EP2475252B1/en active Active
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