JP2010511668A5 - - Google Patents
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- Publication number
- JP2010511668A5 JP2010511668A5 JP2009539738A JP2009539738A JP2010511668A5 JP 2010511668 A5 JP2010511668 A5 JP 2010511668A5 JP 2009539738 A JP2009539738 A JP 2009539738A JP 2009539738 A JP2009539738 A JP 2009539738A JP 2010511668 A5 JP2010511668 A5 JP 2010511668A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- amino
- mono
- aryl
- formula
- 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
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- 125000000217 alkyl group Chemical group 0.000 claims 63
- -1 —C═N—OR 11 Chemical group 0.000 claims 45
- 150000001875 compounds Chemical class 0.000 claims 28
- 125000003545 alkoxy group Chemical group 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 20
- 125000001475 halogen functional group Chemical group 0.000 claims 17
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 13
- 239000002904 solvent Substances 0.000 claims 13
- 239000000543 intermediate Substances 0.000 claims 12
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 10
- 125000001424 substituent group Chemical group 0.000 claims 9
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 8
- 125000002757 morpholinyl group Chemical group 0.000 claims 8
- 125000004076 pyridyl group Chemical group 0.000 claims 8
- 239000002585 base Substances 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 125000002632 imidazolidinyl group Chemical group 0.000 claims 6
- 125000002883 imidazolyl group Chemical group 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000003373 pyrazinyl group Chemical group 0.000 claims 6
- 125000003226 pyrazolyl group Chemical group 0.000 claims 6
- 125000002098 pyridazinyl group Chemical group 0.000 claims 6
- 125000000168 pyrrolyl group Chemical group 0.000 claims 6
- 208000035143 Bacterial infection Diseases 0.000 claims 5
- 239000002253 acid Substances 0.000 claims 5
- 208000022362 bacterial infectious disease Diseases 0.000 claims 5
- 239000003054 catalyst Substances 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 4
- 125000004414 alkyl thio group Chemical group 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 125000004663 dialkyl amino group Chemical group 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 4
- 125000001624 naphthyl group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims 4
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims 4
- 125000004306 triazinyl group Chemical group 0.000 claims 4
- 125000001425 triazolyl group Chemical group 0.000 claims 4
- 241000191967 Staphylococcus aureus Species 0.000 claims 3
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 3
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 208000015181 infectious disease Diseases 0.000 claims 3
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 3
- 241000894006 Bacteria Species 0.000 claims 2
- MZRVEZGGRBJDDB-UHFFFAOYSA-N N-Butyllithium Chemical compound [Li]CCCC MZRVEZGGRBJDDB-UHFFFAOYSA-N 0.000 claims 2
- 125000006350 alkyl thio alkyl group Chemical group 0.000 claims 2
- 150000001412 amines Chemical class 0.000 claims 2
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000004103 aminoalkyl group Chemical group 0.000 claims 2
- 239000003242 anti bacterial agent Substances 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- MKRTXPORKIRPDG-UHFFFAOYSA-N diphenylphosphoryl azide Chemical compound C=1C=CC=CC=1P(=O)(N=[N+]=[N-])C1=CC=CC=C1 MKRTXPORKIRPDG-UHFFFAOYSA-N 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000005984 hexahydro-1H-1,4-diazepinyl group Chemical group 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 239000003446 ligand Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 2
- 231100000252 nontoxic Toxicity 0.000 claims 2
- 230000003000 nontoxic effect Effects 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- JRMUNVKIHCOMHV-UHFFFAOYSA-M tetrabutylammonium bromide Chemical compound [Br-].CCCC[N+](CCCC)(CCCC)CCCC JRMUNVKIHCOMHV-UHFFFAOYSA-M 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000005943 1,2,3,6-tetrahydropyridyl group Chemical group 0.000 claims 1
- LMDZBCPBFSXMTL-UHFFFAOYSA-N 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide Chemical compound CCN=C=NCCCN(C)C LMDZBCPBFSXMTL-UHFFFAOYSA-N 0.000 claims 1
- ZLTWIJREHQCJJL-UHFFFAOYSA-N 1-trimethylsilylethanol Chemical compound CC(O)[Si](C)(C)C ZLTWIJREHQCJJL-UHFFFAOYSA-N 0.000 claims 1
- JMTMSDXUXJISAY-UHFFFAOYSA-N 2H-benzotriazol-4-ol Chemical compound OC1=CC=CC2=C1N=NN2 JMTMSDXUXJISAY-UHFFFAOYSA-N 0.000 claims 1
- 125000004364 3-pyrrolinyl group Chemical group [H]C1=C([H])C([H])([H])N(*)C1([H])[H] 0.000 claims 1
- 241000192125 Firmicutes Species 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- WTDHULULXKLSOZ-UHFFFAOYSA-N Hydroxylamine hydrochloride Chemical compound Cl.ON WTDHULULXKLSOZ-UHFFFAOYSA-N 0.000 claims 1
- RJQXTJLFIWVMTO-TYNCELHUSA-N Methicillin Chemical compound COC1=CC=CC(OC)=C1C(=O)N[C@@H]1C(=O)N2[C@@H](C(O)=O)C(C)(C)S[C@@H]21 RJQXTJLFIWVMTO-TYNCELHUSA-N 0.000 claims 1
- 241000187479 Mycobacterium tuberculosis Species 0.000 claims 1
- 125000000815 N-oxide group Chemical group 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 241000193998 Streptococcus pneumoniae Species 0.000 claims 1
- ATJFFYVFTNAWJD-UHFFFAOYSA-N Tin Chemical compound [Sn] ATJFFYVFTNAWJD-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000003513 alkali Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000005094 alkyl carbonyl amino alkyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 239000003638 chemical reducing agent Substances 0.000 claims 1
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- NPZTUJOABDZTLV-UHFFFAOYSA-N hydroxybenzotriazole Substances O=C1C=CC=C2NNN=C12 NPZTUJOABDZTLV-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims 1
- 229960003085 meticillin Drugs 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000007800 oxidant agent Substances 0.000 claims 1
- 230000001590 oxidative effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000376 reactant Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 229940031000 streptococcus pneumoniae Drugs 0.000 claims 1
- 230000009466 transformation Effects 0.000 claims 1
- 238000000844 transformation Methods 0.000 claims 1
- 0 *C(C(*)(C*N(*)*)O)c1c(*)c(c(CC(O)=O)ccc2)c2nc1* Chemical compound *C(C(*)(C*N(*)*)O)c1c(*)c(c(CC(O)=O)ccc2)c2nc1* 0.000 description 4
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06125499 | 2006-12-06 | ||
| EP06125499.1 | 2006-12-06 | ||
| PCT/EP2007/063313 WO2008068267A1 (en) | 2006-12-06 | 2007-12-04 | Antibacterial quinoline derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010511668A JP2010511668A (ja) | 2010-04-15 |
| JP2010511668A5 true JP2010511668A5 (cg-RX-API-DMAC7.html) | 2010-11-18 |
| JP5466011B2 JP5466011B2 (ja) | 2014-04-09 |
Family
ID=38126091
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009539738A Expired - Fee Related JP5466011B2 (ja) | 2006-12-06 | 2007-12-04 | 抗菌性キノリン誘導体 |
Country Status (32)
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX358506B (es) | 2012-04-27 | 2018-08-22 | Janssen Pharmaceutica Nv | Derivados de quinolina antibacterianos. |
| EP2841425B1 (en) | 2012-04-27 | 2016-03-23 | Janssen Pharmaceutica, N.V. | Antibacterial quinoline derivatives |
| BR112015008515A2 (pt) | 2012-10-16 | 2017-07-04 | Janssen Pharmaceutica Nv | moduladores de ror t de quinolinila ligada à heteroarila |
| ES2628365T3 (es) | 2012-10-16 | 2017-08-02 | Janssen Pharmaceutica N.V. | Moduladores de quinolinilo unidos a fenilo de ROR-GAMA-T |
| PE20150778A1 (es) | 2012-10-16 | 2015-05-23 | Janssen Pharmaceutica Nv | Moduladores de quinolinilo unidos a metileno de ror-gamma-t |
| US9284308B2 (en) | 2013-10-15 | 2016-03-15 | Janssen Pharmaceutica Nv | Methylene linked quinolinyl modulators of RORγt |
| CA2926339A1 (en) | 2013-10-15 | 2015-04-23 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of roryt |
| WO2015057626A1 (en) | 2013-10-15 | 2015-04-23 | Janssen Pharmaceutica Nv | QUINOLINYL MODULATORS OF RORyT |
| US9328095B2 (en) | 2013-10-15 | 2016-05-03 | Janssen Pharmaceutica Nv | Heteroaryl linked quinolinyl modulators of RORgammat |
| US10555941B2 (en) | 2013-10-15 | 2020-02-11 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
| US9403816B2 (en) | 2013-10-15 | 2016-08-02 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of RORγt |
| US9221804B2 (en) | 2013-10-15 | 2015-12-29 | Janssen Pharmaceutica Nv | Secondary alcohol quinolinyl modulators of RORγt |
| CN105330595B (zh) * | 2014-07-14 | 2019-12-10 | 上海嘉坦医药科技有限公司 | 吡啶衍生物及其作为抗分支杆菌的应用 |
| EP3170810B1 (en) * | 2014-07-14 | 2018-09-19 | Cisen Pharmaceutical Co., Ltd. | Pyridine derivatives and anti-mycobacterial use thereof |
| UA126891C2 (uk) * | 2015-01-27 | 2023-02-22 | Янссен Фармацевтика Нв | Здатні до диспергування композиції |
| CN108473428B (zh) * | 2016-01-13 | 2021-07-23 | 上海嘉坦医药科技有限公司 | 一种吡啶衍生物类化合物的制备方法及其中间体和晶型 |
| CN105601566A (zh) * | 2016-02-02 | 2016-05-25 | 张敏 | 一种护理烧伤后感染的药物组合物 |
| ES2934785T3 (es) | 2016-03-07 | 2023-02-27 | Global Alliance For Tb Drug Development Inc | Compuestos antibacterianos y usos de los mismos |
| WO2018048882A1 (en) | 2016-09-06 | 2018-03-15 | The Research Foundation For The State University Of New York | Positron imaging tomography imaging agent composition and method for bacterial infection |
| US20210052597A1 (en) * | 2018-01-29 | 2021-02-25 | Cadila Healthcare Limited | Heterocyclic compounds useful as antibacterial agents |
| IL302095A (en) * | 2020-10-22 | 2023-06-01 | Lunella Biotech Inc | Mitochondrial atp inhibitors targeting the gamma subunit prevent metastasis |
| US20250214980A1 (en) | 2022-03-14 | 2025-07-03 | Slap Pharmaceuticals Llc | Multicyclic compounds |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2270123A1 (en) | 1996-10-28 | 1998-05-07 | Department Of The Army, U.S. Government | Compounds, compositions and methods for treating antibiotic-resistant infections |
| JP4484703B2 (ja) * | 2002-07-25 | 2010-06-16 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | キノリン誘導体およびミコバクテリア抑制剤としてのそれらの使用 |
| PL1711181T3 (pl) | 2004-01-23 | 2010-02-26 | Janssen Pharmaceutica Nv | Pochodne chinoliny i ich zastosowanie jako inhibitorów mykobakteryjnych |
| US7338949B2 (en) | 2004-01-23 | 2008-03-04 | Janssen Pharmaceutica N.V. | Mycobacterial inhibitors |
| EA011572B9 (ru) | 2004-01-29 | 2018-01-31 | Янссен Фармацевтика Н.В. | Производные хинолина для применения в качестве микобактериальных ингибиторов |
| AU2005249231B2 (en) * | 2004-05-28 | 2010-11-11 | Janssen Pharmaceutica N.V. | Use of substituted quinoline derivatives for the treatment of drug resistant mycobacterial diseases |
| PT1797115T (pt) | 2004-09-28 | 2017-08-29 | Janssen Pharmaceutica Nv | Domínio de ligação de atp-sintase bacteriana |
| EE05394B1 (et) | 2004-12-24 | 2011-04-15 | Janssen Pharmaceutica N.V. | Kinoliinihendid kasutamiseks latentse tuberkuloosi ravis |
| CA2528849C (en) * | 2005-06-08 | 2014-01-14 | Janssen Pharmaceutica N.V. | Quinoline derivatives as antibacterial agents |
| JO2855B1 (en) * | 2005-08-03 | 2015-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinoline derivatives acting as antibacterial agents |
| JO2837B1 (en) * | 2005-08-03 | 2014-09-15 | جانسن فارمسيتكا ان في | Quinoline derivatives acting as antibacterial agents |
| JO2952B1 (en) * | 2005-08-03 | 2016-03-15 | جانسين فارماسوتيكا ان. في | Quinoline derivatives acting as antibacterial agents |
-
2007
- 2007-11-29 JO JOP/2007/0504A patent/JO3271B1/ar active
- 2007-12-04 CN CNA2007800449358A patent/CN101553470A/zh active Pending
- 2007-12-04 HU HUE07847811A patent/HUE028769T2/en unknown
- 2007-12-04 PT PT07847811T patent/PT2099758E/pt unknown
- 2007-12-04 AP AP2009004874A patent/AP2479A/xx active
- 2007-12-04 KR KR1020097012967A patent/KR101490222B1/ko not_active Expired - Fee Related
- 2007-12-04 EA EA200970535A patent/EA016733B1/ru unknown
- 2007-12-04 NZ NZ576823A patent/NZ576823A/en not_active IP Right Cessation
- 2007-12-04 HR HRP20160585TT patent/HRP20160585T1/hr unknown
- 2007-12-04 JP JP2009539738A patent/JP5466011B2/ja not_active Expired - Fee Related
- 2007-12-04 CA CA2669819A patent/CA2669819C/en active Active
- 2007-12-04 EP EP07847811.2A patent/EP2099758B1/en active Active
- 2007-12-04 MX MX2009005978A patent/MX2009005978A/es active IP Right Grant
- 2007-12-04 CN CN201510088659.1A patent/CN104744361B/zh not_active Expired - Fee Related
- 2007-12-04 RS RS20160374A patent/RS54794B1/sr unknown
- 2007-12-04 BR BRPI0720220A patent/BRPI0720220B8/pt not_active IP Right Cessation
- 2007-12-04 DK DK07847811.2T patent/DK2099758T3/en active
- 2007-12-04 SI SI200731779A patent/SI2099758T1/sl unknown
- 2007-12-04 WO PCT/EP2007/063313 patent/WO2008068267A1/en not_active Ceased
- 2007-12-04 AU AU2007328887A patent/AU2007328887B2/en not_active Ceased
- 2007-12-04 ME MEP-2016-109A patent/ME02498B/me unknown
- 2007-12-04 PL PL07847811T patent/PL2099758T3/pl unknown
- 2007-12-04 MY MYPI20092283A patent/MY181645A/en unknown
- 2007-12-04 US US12/516,065 patent/US8415475B2/en not_active Expired - Fee Related
- 2007-12-04 ES ES07847811.2T patent/ES2573689T3/es active Active
- 2007-12-04 UA UAA200904716A patent/UA100972C2/ru unknown
- 2007-12-05 TW TW096146217A patent/TWI406659B/zh not_active IP Right Cessation
- 2007-12-05 AR ARP070105444A patent/AR064151A1/es unknown
- 2007-12-05 CL CL200703514A patent/CL2007003514A1/es unknown
-
2009
- 2009-06-02 IL IL199083A patent/IL199083A/en active IP Right Grant
- 2009-06-05 ZA ZA200903950A patent/ZA200903950B/xx unknown
- 2009-07-06 NO NO20092542A patent/NO341983B1/no unknown
-
2016
- 2016-06-08 CY CY20161100496T patent/CY1117766T1/el unknown
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