JP2005533061A5 - - Google Patents
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- JP2005533061A5 JP2005533061A5 JP2004512749A JP2004512749A JP2005533061A5 JP 2005533061 A5 JP2005533061 A5 JP 2005533061A5 JP 2004512749 A JP2004512749 A JP 2004512749A JP 2004512749 A JP2004512749 A JP 2004512749A JP 2005533061 A5 JP2005533061 A5 JP 2005533061A5
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- JP
- Japan
- Prior art keywords
- heteroatoms
- independently selected
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- groups
- compound
- 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.)
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 40
- 150000001875 compounds Chemical class 0.000 claims 38
- 125000005842 heteroatom Chemical group 0.000 claims 38
- 229910052760 oxygen Inorganic materials 0.000 claims 23
- 239000000203 mixture Substances 0.000 claims 22
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 21
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 21
- 229910052757 nitrogen Inorganic materials 0.000 claims 21
- 239000001301 oxygen Substances 0.000 claims 21
- 229910052717 sulfur Inorganic materials 0.000 claims 21
- 239000011593 sulfur Substances 0.000 claims 21
- 125000001931 aliphatic group Chemical group 0.000 claims 20
- 229910052736 halogen Inorganic materials 0.000 claims 18
- 150000002367 halogens Chemical class 0.000 claims 18
- 125000003118 aryl group Chemical group 0.000 claims 17
- 238000000034 method Methods 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 229920006395 saturated elastomer Polymers 0.000 claims 11
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 208000035143 Bacterial infection Diseases 0.000 claims 5
- 208000022362 bacterial infectious disease Diseases 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 241000187479 Mycobacterium tuberculosis Species 0.000 claims 4
- 239000003242 anti bacterial agent Substances 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 4
- 239000003586 protic polar solvent Substances 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 102000004127 Cytokines Human genes 0.000 claims 3
- 108090000695 Cytokines Proteins 0.000 claims 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 3
- 229940088710 antibiotic agent Drugs 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 241000193738 Bacillus anthracis Species 0.000 claims 2
- 241000894006 Bacteria Species 0.000 claims 2
- 241001647372 Chlamydia pneumoniae Species 0.000 claims 2
- 241000194032 Enterococcus faecalis Species 0.000 claims 2
- 241000194031 Enterococcus faecium Species 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 241000590002 Helicobacter pylori Species 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical group C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 2
- 241000589242 Legionella pneumophila Species 0.000 claims 2
- 239000000867 Lipoxygenase Inhibitor Substances 0.000 claims 2
- 241000588655 Moraxella catarrhalis Species 0.000 claims 2
- 241000202934 Mycoplasma pneumoniae Species 0.000 claims 2
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical group [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims 2
- 241000191967 Staphylococcus aureus Species 0.000 claims 2
- 241000193998 Streptococcus pneumoniae Species 0.000 claims 2
- 241000193996 Streptococcus pyogenes Species 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 2
- 230000002137 anti-vascular effect Effects 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 239000003443 antiviral agent Substances 0.000 claims 2
- 229940065181 bacillus anthracis Drugs 0.000 claims 2
- 125000005605 benzo group Chemical group 0.000 claims 2
- LPIQUOYDBNQMRZ-UHFFFAOYSA-N cyclopentene Chemical compound C1CC=CC1 LPIQUOYDBNQMRZ-UHFFFAOYSA-N 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 229940032049 enterococcus faecalis Drugs 0.000 claims 2
- 239000003102 growth factor Substances 0.000 claims 2
- 229940037467 helicobacter pylori Drugs 0.000 claims 2
- 230000003463 hyperproliferative effect Effects 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 239000002955 immunomodulating agent Substances 0.000 claims 2
- 229940121354 immunomodulator Drugs 0.000 claims 2
- 239000003018 immunosuppressive agent Substances 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- 229910052500 inorganic mineral Inorganic materials 0.000 claims 2
- 229940115932 legionella pneumophila Drugs 0.000 claims 2
- 239000011707 mineral Substances 0.000 claims 2
- 229940013390 mycoplasma pneumoniae Drugs 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 229940094443 oxytocics prostaglandins Drugs 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 229910052700 potassium Inorganic materials 0.000 claims 2
- 239000011591 potassium Chemical group 0.000 claims 2
- 150000003180 prostaglandins Chemical class 0.000 claims 2
- 229910052708 sodium Inorganic materials 0.000 claims 2
- 239000011734 sodium Substances 0.000 claims 2
- 229940031000 streptococcus pneumoniae Drugs 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 208000031729 Bacteremia Diseases 0.000 claims 1
- 241000588914 Enterobacter Species 0.000 claims 1
- 241000588724 Escherichia coli Species 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 241000606790 Haemophilus Species 0.000 claims 1
- 241000606768 Haemophilus influenzae Species 0.000 claims 1
- 241000588747 Klebsiella pneumoniae Species 0.000 claims 1
- 229940122142 Lipoxygenase inhibitor Drugs 0.000 claims 1
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical group [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims 1
- 102000005741 Metalloproteases Human genes 0.000 claims 1
- 108010006035 Metalloproteases Proteins 0.000 claims 1
- 206010035664 Pneumonia Diseases 0.000 claims 1
- 206010036410 Postoperative wound infection Diseases 0.000 claims 1
- 241000588769 Proteus <enterobacteria> Species 0.000 claims 1
- 241000589517 Pseudomonas aeruginosa Species 0.000 claims 1
- 206010057190 Respiratory tract infections Diseases 0.000 claims 1
- 241000607720 Serratia Species 0.000 claims 1
- 206010062255 Soft tissue infection Diseases 0.000 claims 1
- 241000191940 Staphylococcus Species 0.000 claims 1
- 241000191963 Staphylococcus epidermidis Species 0.000 claims 1
- 208000031650 Surgical Wound Infection Diseases 0.000 claims 1
- 210000000683 abdominal cavity Anatomy 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 230000001580 bacterial effect Effects 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 229910052792 caesium Inorganic materials 0.000 claims 1
- TVFDJXOCXUVLDH-UHFFFAOYSA-N caesium atom Chemical group [Cs] TVFDJXOCXUVLDH-UHFFFAOYSA-N 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000000430 cytokine receptor antagonist Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 229940047650 haemophilus influenzae Drugs 0.000 claims 1
- 229960003444 immunosuppressant agent Drugs 0.000 claims 1
- 229940125721 immunosuppressive agent Drugs 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 229910052744 lithium Inorganic materials 0.000 claims 1
- 239000011159 matrix material Substances 0.000 claims 1
- 229940121386 matrix metalloproteinase inhibitor Drugs 0.000 claims 1
- 239000003771 matrix metalloproteinase inhibitor Substances 0.000 claims 1
- 229910017464 nitrogen compound Inorganic materials 0.000 claims 1
- 150000002830 nitrogen compounds Chemical class 0.000 claims 1
- RGSFGYAAUTVSQA-UHFFFAOYSA-N pentamethylene Natural products C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 201000007094 prostatitis Diseases 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical group OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 239000011541 reaction mixture Substances 0.000 claims 1
- 229910052701 rubidium Inorganic materials 0.000 claims 1
- IGLNJRXAVVLDKE-UHFFFAOYSA-N rubidium atom Chemical group [Rb] IGLNJRXAVVLDKE-UHFFFAOYSA-N 0.000 claims 1
- 230000035945 sensitivity Effects 0.000 claims 1
- 201000009890 sinusitis Diseases 0.000 claims 1
- 206010040872 skin infection Diseases 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 208000019206 urinary tract infection Diseases 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38866502P | 2002-06-13 | 2002-06-13 | |
| US42907702P | 2002-11-26 | 2002-11-26 | |
| PCT/US2003/018401 WO2003105846A1 (en) | 2002-06-13 | 2003-06-11 | 2-ureido-6-heteroaryl-3h-benzoimidazole-4-carboxylic acid derivatives and related compounds as gyrase and/or topoisomerase iv inhibitors for the treatment of bacterial infections |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005533061A JP2005533061A (ja) | 2005-11-04 |
| JP2005533061A5 true JP2005533061A5 (https=) | 2006-07-20 |
| JP4489586B2 JP4489586B2 (ja) | 2010-06-23 |
Family
ID=29740049
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004512749A Expired - Fee Related JP4489586B2 (ja) | 2002-06-13 | 2003-06-11 | 細菌感染を治療するジャイレースおよび／またはトポイソメラーゼｉｖ阻害剤としての２−ウレイド−６−ヘテロアリール−３ｈ−ベンゾイミダゾール−４−カルボン酸誘導体および関連化合物 |
Country Status (17)
| Country | Link |
|---|---|
| US (2) | US7727992B2 (https=) |
| EP (1) | EP1511482B1 (https=) |
| JP (1) | JP4489586B2 (https=) |
| KR (1) | KR101052433B1 (https=) |
| CN (1) | CN1674898A (https=) |
| AT (1) | ATE345132T1 (https=) |
| AU (1) | AU2003245442B2 (https=) |
| CA (1) | CA2489128C (https=) |
| DE (1) | DE60309701T2 (https=) |
| ES (1) | ES2277088T3 (https=) |
| IL (1) | IL165715A (https=) |
| MX (1) | MXPA04012628A (https=) |
| NO (1) | NO20050099L (https=) |
| PL (1) | PL374191A1 (https=) |
| RU (1) | RU2333208C2 (https=) |
| TW (1) | TWI282335B (https=) |
| WO (1) | WO2003105846A1 (https=) |
Families Citing this family (56)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100590859B1 (ko) * | 1999-09-14 | 2006-06-19 | 삼성전자주식회사 | 교환기 시스템의 기능 시험방법 |
| DE60309701T2 (de) * | 2002-06-13 | 2007-09-06 | Vertex Pharmaceuticals Inc., Cambridge | 2-ureido-6-heteroaryl-3h-benzoimidazol-4-carbonsäurederivate und verwandte verbindungen als gyrase und/oder topoisomerase iv inhibitoren zur behandlung von bakteriellen infektionen |
| US7569591B2 (en) | 2003-01-31 | 2009-08-04 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| US7618974B2 (en) | 2003-01-31 | 2009-11-17 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| US8404852B2 (en) | 2003-01-31 | 2013-03-26 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| US7582641B2 (en) | 2003-01-31 | 2009-09-01 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| US8193352B2 (en) | 2003-01-31 | 2012-06-05 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| AR042956A1 (es) | 2003-01-31 | 2005-07-13 | Vertex Pharma | Inhibidores de girasa y usos de los mismos |
| ES2400287T3 (es) | 2005-03-14 | 2013-04-08 | High Point Pharmaceuticals, Llc | Derivados de benzazol, composiciones y procedimientos de uso como inhibidores de beta-secretasa |
| AU2006311729A1 (en) | 2005-11-07 | 2007-05-18 | Vertex Pharmaceuticals Incorporated | Benzimidazole derivatives as gyrase inhibitors |
| TWI417095B (zh) | 2006-03-15 | 2013-12-01 | Janssen Pharmaceuticals Inc | １，４-二取代之３-氰基-吡啶酮衍生物及其作為ｍＧｌｕＲ２-受體之正向異位性調節劑之用途 |
| TW200845978A (en) | 2007-03-07 | 2008-12-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives |
| TW200900065A (en) | 2007-03-07 | 2009-01-01 | Janssen Pharmaceutica Nv | 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives |
| TW200906412A (en) * | 2007-06-12 | 2009-02-16 | Astrazeneca Ab | Piperidine compounds and uses thereof |
| PL2203439T3 (pl) | 2007-09-14 | 2011-06-30 | Addex Pharmaceuticals Sa | 1',3'-dipodstawione-4-fenylo-3,4,5,6-tetrahydro-2H, 1'H-[1, 4']bipirydynylo-2'-ketony |
| MX2010006237A (es) * | 2007-12-07 | 2010-12-21 | Vertex Pharma | Formas solidas de 1-etil-3-(5-(5-fluoropiridin-3-il)-7-(pirimidin- 2-il)-1h-benzo[d]imidazol-2-il)urea. |
| GB0724342D0 (en) | 2007-12-13 | 2008-01-30 | Prolysis Ltd | Anitbacterial compositions |
| JP5547194B2 (ja) | 2008-09-02 | 2014-07-09 | ジャンセン ファーマシューティカルズ， インコーポレイテッド． | 代謝型グルタミン酸受容体の調節因子としての３−アザビシクロ［３．１．０］ヘキシル誘導体 |
| WO2010060589A1 (en) | 2008-11-28 | 2010-06-03 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors |
| GB0821913D0 (en) | 2008-12-02 | 2009-01-07 | Price & Co | Antibacterial compounds |
| CN102439008B (zh) | 2009-05-12 | 2015-04-29 | 杨森制药有限公司 | 1,2,4-三唑并[4,3-a]吡啶衍生物及其用于治疗或预防神经和精神病症的用途 |
| MY153912A (en) | 2009-05-12 | 2015-04-15 | Janssen Pharmaceuticals Inc | 1, 2, 4,-triazolo[4,3-a[pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| MY153913A (en) | 2009-05-12 | 2015-04-15 | Janssen Pharmaceuticals Inc | 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| BR112012024705A2 (pt) | 2010-03-31 | 2016-06-07 | Actelion Pharmaceuticals Ltd | derivados antibacterianos de isoquinolin-3-ilureia |
| WO2011151618A2 (en) | 2010-06-01 | 2011-12-08 | Summit Corporation Plc | Compounds for the treatment of clostridium difficile-associated disease |
| ES2568455T3 (es) | 2010-06-01 | 2016-04-29 | Summit Therapeutics Plc | Compuestos para el tratamiento de enfermedad asociada a Clostridium difficile |
| WO2011151619A1 (en) | 2010-06-01 | 2011-12-08 | Summit Corporation Plc | Compounds for the treatment of clostridium difficile associated disease |
| WO2011151617A1 (en) | 2010-06-01 | 2011-12-08 | Summit Corporation Plc | Compounds for the treatment of clostridium difficile associated disease |
| WO2011151620A1 (en) | 2010-06-01 | 2011-12-08 | Summit Corporation Plc | Compounds for the treatment of clostridium difficile associated disease |
| EP2661435B1 (en) | 2010-11-08 | 2015-08-19 | Janssen Pharmaceuticals, Inc. | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS |
| CN103261195B (zh) | 2010-11-08 | 2015-09-02 | 杨森制药公司 | 1,2,4-三唑并[4,3-a]吡啶衍生物及其作为MGLUR2受体的正变构调节剂的用途 |
| PL2649069T3 (pl) | 2010-11-08 | 2016-01-29 | Janssen Pharmaceuticals Inc | Pochodne 1,2,4-triazolo[4,3-a]pirydyny i ich zastosowanie jako dodatnich allosterycznych modulatorów receptorów mGluR2 |
| CN103384665B (zh) | 2011-01-14 | 2018-01-09 | 斯派罗吹耐姆公司 | 制备促旋酶和拓扑异构酶抑制剂的方法 |
| US8476281B2 (en) * | 2011-01-14 | 2013-07-02 | Vertex Pharmaceuticals Incorporated | Solid forms of gyrase inhibitor (R)-1-ethyl-3-[6-fluoro-5-[2-(1-hydroxy-1-methyl-ethyl)pyrimidin-5-yl]-7-(tetrahydrofuran-2-yl)-1H-benzimidazol-2-yl]urea |
| AU2012205415B2 (en) | 2011-01-14 | 2017-02-02 | Spero Therapeutics, Inc. | Pyrimidine gyrase and topoisomerase IV inhibitors |
| WO2012097270A1 (en) * | 2011-01-14 | 2012-07-19 | Vertex Pharmaceuticals Incorporated | Solid forms of gyrase inhibitor (r)-1-ethyl-3-[5-[2-{1-hydroxy-1-methyl-ethyl}pyrimidin-5-yl]-7-(tetrahydrofuran-2-yl}-1h-benzimidazol-2-yl]urea |
| AR088729A1 (es) | 2011-03-29 | 2014-07-02 | Actelion Pharmaceuticals Ltd | Derivados de 3-ureidoisoquinolin-8-ilo y una composicion farmaceutica |
| CN103702994B (zh) | 2011-06-20 | 2016-03-23 | 沃泰克斯药物股份有限公司 | 旋转酶和拓扑异构酶抑制剂的磷酸酯 |
| US9572809B2 (en) | 2012-07-18 | 2017-02-21 | Spero Trinem, Inc. | Combination therapy to treat Mycobacterium diseases |
| WO2014015105A1 (en) | 2012-07-18 | 2014-01-23 | Vertex Pharmaceuticals Incorporated | Solid forms of (r)-2-(5-(2-(3-ethylureido)-6-fluoro-7-(tetrahydrofuran-2-yl)-1h-benzo[d]imidazol-5-yl)pyrimidin-2-yl)propan-2-yl dihydrogen phosphate and salts thereof |
| US9079935B2 (en) | 2012-08-13 | 2015-07-14 | The Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Las Vegas | Reducing risk of contracting Clostridium-difficile associated disease |
| JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
| JO3367B1 (ar) | 2013-09-06 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2 |
| HUE053734T2 (hu) | 2014-01-21 | 2021-07-28 | Janssen Pharmaceutica Nv | 2-es altípusú metabotróp glutamáterg receptor pozitív allosztérikus modulátorait tartalmazó kombinációk és alkalmazásuk |
| KR20220049612A (ko) | 2014-01-21 | 2022-04-21 | 얀센 파마슈티카 엔.브이. | 대사 조절형 글루탐산 작동성 수용체 제2아형의 양성 알로스테릭 조절제 또는 오르토스테릭 작동제를 포함하는 조합 및 그 용도 |
| MX2016010057A (es) | 2014-02-03 | 2017-04-27 | Spero Gyrase Inc | Compuestos antibacterianos. |
| BR112016019469B1 (pt) * | 2014-02-12 | 2022-12-06 | Albert Einstein College Of Medicine, Inc. | Tratamento de infecções por h. pylori utilizando -se inibidores de mtan |
| WO2016127102A2 (en) | 2015-02-06 | 2016-08-11 | Ernesto Abel-Santos | Inhibiting germination of clostridium perfringens spores to reduce necrotic enteritis |
| CA3057431A1 (en) | 2017-03-24 | 2018-09-27 | Taisho Pharmaceutical Co., Ltd. | 2(1h)-quinolinone derivative |
| US20200345637A1 (en) * | 2018-01-19 | 2020-11-05 | Aiviva Biopharma, Inc. | Suspension compositions of multi-target inhibitors |
| KR102737283B1 (ko) | 2019-07-17 | 2024-12-03 | 서밋 (옥스포드) 리미티드 | 리디닐라졸 및 이의 결정 형태의 제조방법 |
| WO2021126118A1 (en) * | 2019-12-20 | 2021-06-24 | Anadolu Üni̇versi̇tesi̇ | Synthesis of 2-(substitutedphenyl)-5-(substitutedheteroaryl)- 1h-benzimidazole derivatives and investigation of their biological effects |
| GB202100470D0 (en) | 2021-01-14 | 2021-03-03 | Summit Oxford Ltd | Solid tablet dosage for of ridinilazole |
| GB202100471D0 (en) | 2021-01-14 | 2021-03-03 | Summit Oxford Ltd | Preparation of antibacterial compounds |
| EP4398890A4 (en) | 2021-09-09 | 2025-07-30 | The Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The Univ Of Nevada Las Ve | C. Difficile Spore Germination Inhibitors |
| NL2033609B1 (en) * | 2022-11-24 | 2024-05-30 | Innes John Centre | DNA Gyrase Inhibitors |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| GB8803429D0 (en) * | 1988-02-15 | 1988-03-16 | Fujisawa Pharmaceutical Co | Imidazole compounds processes for preparation thereof & pharmaceutical composition comprising same |
| CA2028530A1 (en) | 1989-11-21 | 1991-05-22 | Christian Hubschwerlen | Substituted pyrimidobenzimidazole derivatives |
| US5559127A (en) * | 1992-10-14 | 1996-09-24 | Merck & Co., Inc. | Fibrinogen receptor antagonists |
| US5527910A (en) * | 1992-12-30 | 1996-06-18 | Cheil Foods & Chemicals, Inc. | Pyridone carboxylic acid compounds and their uses for treating infectious diseases caused by bacteria |
| DE4344074A1 (de) * | 1993-12-23 | 1995-06-29 | Hoechst Schering Agrevo Gmbh | Bicyclische Heteroarylverbindungen, Verfahren zu deren Herstellung, diese enthaltende Mittel und deren Verwendung als Safener |
| DE19514313A1 (de) | 1994-08-03 | 1996-02-08 | Bayer Ag | Benzoxazolyl- und Benzothiazolyloxazolidinone |
| US5643935A (en) * | 1995-06-07 | 1997-07-01 | The University Of North Carolina At Chapel Hill | Method of combatting infectious diseases using dicationic bis-benzimidazoles |
| ES2124167B1 (es) * | 1996-06-04 | 1999-09-16 | Espanola Prod Quimicos | Nuevos derivados del bencimidazol con actividad antihistaminica. |
| GB9911594D0 (en) | 1999-05-19 | 1999-07-21 | Smithkline Beecham Plc | Novel compounds |
| HUP0303494A3 (en) * | 2000-12-15 | 2009-08-28 | Vertex Pharma | Parmaceutical compositions containing bacterial gyrase inhibitors and uses thereof |
| DE60309701T2 (de) * | 2002-06-13 | 2007-09-06 | Vertex Pharmaceuticals Inc., Cambridge | 2-ureido-6-heteroaryl-3h-benzoimidazol-4-carbonsäurederivate und verwandte verbindungen als gyrase und/oder topoisomerase iv inhibitoren zur behandlung von bakteriellen infektionen |
| US7618974B2 (en) * | 2003-01-31 | 2009-11-17 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| US7569591B2 (en) * | 2003-01-31 | 2009-08-04 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| AR042956A1 (es) * | 2003-01-31 | 2005-07-13 | Vertex Pharma | Inhibidores de girasa y usos de los mismos |
| US7582641B2 (en) * | 2003-01-31 | 2009-09-01 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
-
2003
- 2003-06-11 DE DE60309701T patent/DE60309701T2/de not_active Expired - Lifetime
- 2003-06-11 KR KR1020047020292A patent/KR101052433B1/ko not_active Expired - Fee Related
- 2003-06-11 WO PCT/US2003/018401 patent/WO2003105846A1/en not_active Ceased
- 2003-06-11 CN CNA038185709A patent/CN1674898A/zh active Pending
- 2003-06-11 MX MXPA04012628A patent/MXPA04012628A/es active IP Right Grant
- 2003-06-11 CA CA2489128A patent/CA2489128C/en not_active Expired - Fee Related
- 2003-06-11 AT AT03739082T patent/ATE345132T1/de active
- 2003-06-11 JP JP2004512749A patent/JP4489586B2/ja not_active Expired - Fee Related
- 2003-06-11 ES ES03739082T patent/ES2277088T3/es not_active Expired - Lifetime
- 2003-06-11 EP EP03739082A patent/EP1511482B1/en not_active Expired - Lifetime
- 2003-06-11 PL PL03374191A patent/PL374191A1/xx not_active Application Discontinuation
- 2003-06-11 US US10/459,420 patent/US7727992B2/en not_active Expired - Fee Related
- 2003-06-11 RU RU2005100516/04A patent/RU2333208C2/ru not_active IP Right Cessation
- 2003-06-11 AU AU2003245442A patent/AU2003245442B2/en not_active Ceased
- 2003-06-13 TW TWGYRASEINA patent/TWI282335B/zh active
-
2004
- 2004-12-12 IL IL165715A patent/IL165715A/en not_active IP Right Cessation
-
2005
- 2005-01-07 NO NO20050099A patent/NO20050099L/no not_active Application Discontinuation
-
2010
- 2010-04-16 US US12/761,576 patent/US8426426B2/en not_active Expired - Fee Related
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