JP2007514782A5 - - Google Patents
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- Publication number
- JP2007514782A5 JP2007514782A5 JP2006545691A JP2006545691A JP2007514782A5 JP 2007514782 A5 JP2007514782 A5 JP 2007514782A5 JP 2006545691 A JP2006545691 A JP 2006545691A JP 2006545691 A JP2006545691 A JP 2006545691A JP 2007514782 A5 JP2007514782 A5 JP 2007514782A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- pharmaceutically acceptable
- compound according
- acceptable salt
- 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 58
- 125000000217 alkyl group Chemical group 0.000 claims 37
- 150000003839 salts Chemical class 0.000 claims 29
- 150000002148 esters Chemical class 0.000 claims 19
- 239000000651 prodrug Substances 0.000 claims 19
- 229940002612 prodrug Drugs 0.000 claims 19
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 12
- 229920006395 saturated elastomer Polymers 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000000203 mixture Substances 0.000 claims 9
- 241000124008 Mammalia Species 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 239000001301 oxygen Substances 0.000 claims 6
- 239000011593 sulfur Substances 0.000 claims 6
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 208000015181 infectious disease Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical class Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 238000010276 construction Methods 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical group N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- 206010056519 Abdominal infection Diseases 0.000 claims 1
- 206010060968 Arthritis infective Diseases 0.000 claims 1
- 208000031729 Bacteremia Diseases 0.000 claims 1
- 206010017533 Fungal infection Diseases 0.000 claims 1
- 208000017228 Gastrointestinal motility disease Diseases 0.000 claims 1
- 208000008745 Healthcare-Associated Pneumonia Diseases 0.000 claims 1
- 201000009906 Meningitis Diseases 0.000 claims 1
- 208000037942 Methicillin-resistant Staphylococcus aureus infection Diseases 0.000 claims 1
- 208000031888 Mycoses Diseases 0.000 claims 1
- 206010031252 Osteomyelitis Diseases 0.000 claims 1
- 208000030852 Parasitic disease Diseases 0.000 claims 1
- 206010035664 Pneumonia Diseases 0.000 claims 1
- 206010035737 Pneumonia viral Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 206010058028 Shunt infection Diseases 0.000 claims 1
- 206010041925 Staphylococcal infections Diseases 0.000 claims 1
- 108010059993 Vancomycin Proteins 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 206010014665 endocarditis Diseases 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- TYZROVQLWOKYKF-ZDUSSCGKSA-N linezolid Chemical compound O=C1O[C@@H](CNC(=O)C)CN1C(C=C1F)=CC=C1N1CCOCC1 TYZROVQLWOKYKF-ZDUSSCGKSA-N 0.000 claims 1
- 229960003907 linezolid Drugs 0.000 claims 1
- 230000000813 microbial effect Effects 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 206010034674 peritonitis Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 206010040872 skin infection Diseases 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 201000008827 tuberculosis Diseases 0.000 claims 1
- 208000019206 urinary tract infection Diseases 0.000 claims 1
- 229960003165 vancomycin Drugs 0.000 claims 1
- MYPYJXKWCTUITO-UHFFFAOYSA-N vancomycin Natural products O1C(C(=C2)Cl)=CC=C2C(O)C(C(NC(C2=CC(O)=CC(O)=C2C=2C(O)=CC=C3C=2)C(O)=O)=O)NC(=O)C3NC(=O)C2NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(CC(C)C)NC)C(O)C(C=C3Cl)=CC=C3OC3=CC2=CC1=C3OC1OC(CO)C(O)C(O)C1OC1CC(C)(N)C(O)C(C)O1 MYPYJXKWCTUITO-UHFFFAOYSA-N 0.000 claims 1
- MYPYJXKWCTUITO-LYRMYLQWSA-O vancomycin(1+) Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C2C=C3C=C1OC1=CC=C(C=C1Cl)[C@@H](O)[C@H](C(N[C@@H](CC(N)=O)C(=O)N[C@H]3C(=O)N[C@H]1C(=O)N[C@H](C(N[C@@H](C3=CC(O)=CC(O)=C3C=3C(O)=CC=C1C=3)C([O-])=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)O2)=O)NC(=O)[C@@H](CC(C)C)[NH2+]C)[C@H]1C[C@](C)([NH3+])[C@H](O)[C@H](C)O1 MYPYJXKWCTUITO-LYRMYLQWSA-O 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 230000002861 ventricular Effects 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
- 208000009421 viral pneumonia Diseases 0.000 claims 1
- 0 *C[C@](CN1c2ccc(*(*)*N)cc2)OC1=O Chemical compound *C[C@](CN1c2ccc(*(*)*N)cc2)OC1=O 0.000 description 4
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US53037103P | 2003-12-17 | 2003-12-17 | |
| US57626704P | 2004-06-02 | 2004-06-02 | |
| PCT/US2004/039988 WO2005061468A1 (en) | 2003-12-17 | 2004-12-01 | Halogenated biaryl heterocyclic compounds and methods of making and using the same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007514782A JP2007514782A (ja) | 2007-06-07 |
| JP2007514782A5 true JP2007514782A5 (https=) | 2008-02-07 |
Family
ID=34713773
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006545691A Pending JP2007514782A (ja) | 2003-12-17 | 2004-12-01 | ハロゲン化ビアリール複素環式化合物ならびにその作製方法および使用方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US7129259B2 (https=) |
| EP (1) | EP1713785A1 (https=) |
| JP (1) | JP2007514782A (https=) |
| AR (1) | AR046782A1 (https=) |
| TW (1) | TW200526649A (https=) |
| WO (1) | WO2005061468A1 (https=) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200420573A (en) * | 2002-09-26 | 2004-10-16 | Rib X Pharmaceuticals Inc | Bifunctional heterocyclic compounds and methods of making and using same |
| US8324398B2 (en) | 2003-06-03 | 2012-12-04 | Rib-X Pharmaceuticals, Inc. | Process for the synthesis of biaryl oxazolidinones |
| EP1656370B1 (en) * | 2003-06-03 | 2012-08-15 | Rib-X Pharmaceuticals, Inc. | Biaryl heterocyclic compounds and methods of making and using the same |
| US8428884B1 (en) | 2003-07-14 | 2013-04-23 | Rib-X Pharmaceuticals, Inc. | Protein synthesis modulators |
| EP2725008A1 (en) * | 2003-08-18 | 2014-04-30 | NovaBay Pharmaceuticals, Inc. | N,N-dihalogenated amino acids and derivatives |
| AR046782A1 (es) * | 2003-12-17 | 2005-12-21 | Rib X Pharmaceuticals Inc | Compuestos heterociclicos de biarilo halogenados, composiciones farmaceuticas que los contienen, metodos para su elaboracion y su uso como medicamentos. |
| KR100854211B1 (ko) * | 2003-12-18 | 2008-08-26 | 동아제약주식회사 | 신규한 옥사졸리디논 유도체, 그의 제조방법 및 이를유효성분으로 하는 항생제용 약학 조성물 |
| CA2567929A1 (en) * | 2004-05-25 | 2005-12-08 | Astrazeneca Ab | 3- {4- (pyridin-3-yl) phenyl} -5- (1h-1, 2, 3-triazol-1-ylmethyl) -1, 3-oxazolidin-2-ones as antibacterial agents |
| TWI386201B (zh) * | 2005-01-25 | 2013-02-21 | Novabay Pharmaceuticals Inc | N-鹵化胺基酸、n,n-二鹵化胺基酸與其衍生物;以及使用其之組合物與方法 |
| JP5534497B2 (ja) | 2005-06-08 | 2014-07-02 | メリンタ セラピューティクス,インコーポレイテッド | トリアゾール類の合成方法 |
| TW200740779A (en) | 2005-07-22 | 2007-11-01 | Mitsubishi Pharma Corp | Intermediate compound for synthesizing pharmaceutical agent and production method thereof |
| WO2007133803A2 (en) * | 2006-05-15 | 2007-11-22 | Rib-X Pharmaceuticals, Inc. | Treatment of mycobacterial infections |
| TW200843787A (en) * | 2006-12-29 | 2008-11-16 | Novabay Pharmaceuticals Inc | N-halogenated amino compounds and derivatives; compositions and methods of using them |
| US20090132514A1 (en) * | 2007-11-16 | 2009-05-21 | Iac Search & Media, Inc. | method and system for building text descriptions in a search database |
| JP5613656B2 (ja) * | 2008-03-26 | 2014-10-29 | グローバル、アライアンス、フォア、ティービー、ドラッグ、ディベロップメント | 置換されたフェニルオキサゾリジノンと共有結合した二環式ニトロイミダゾール |
| WO2009127924A1 (en) * | 2008-04-15 | 2009-10-22 | Waldemar Gottardi | Compositions and devices for antisepsis and anticoagulation |
| RU2659792C1 (ru) | 2008-10-10 | 2018-07-04 | Мерк Шарп Энд Домэ Корп. | Оксазолидиноны и способ их очистки |
| MY156354A (en) | 2009-02-03 | 2016-02-15 | Merck Sharp & Dohme | Crystalline form of r)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate |
| EP2230231A1 (de) * | 2009-03-16 | 2010-09-22 | Bayer CropScience AG | Verfahren zur Herstellung von 2,2-Difluorethylamin-Derivaten durch Imin-Hydrierung |
| US8580767B2 (en) * | 2009-05-28 | 2013-11-12 | Trius Therapeutics, Inc. | Oxazolidinone containing dimer compounds, compositions and methods to make and use |
| EA022765B1 (ru) | 2009-10-13 | 2016-02-29 | Мелинта Терапьютикс, Инк. | Фармацевтическая композиция |
| NZ610638A (en) | 2010-11-24 | 2015-05-29 | Melinta Therapeutics Inc | Pharmaceutical compositions comprising radezolid |
| KR102237887B1 (ko) | 2013-03-15 | 2021-04-07 | 멜린타 서브시디어리 코프. | 항생제를 사용하여 과체중 및 비만 환자에서 감염을 치료하는 방법 |
| CN107205989A (zh) | 2014-11-14 | 2017-09-26 | 梅琳塔治疗公司 | 治疗、预防或降低皮肤感染风险的方法 |
| WO2017066964A1 (en) * | 2015-10-22 | 2017-04-27 | Merck Sharp & Dohme Corp. | Oxazolidinone compounds and methods of use thereof as antibacterial agents |
| WO2020147504A1 (en) | 2019-01-18 | 2020-07-23 | Merck Sharp & Dohme Corp. | Oxazolidinone compounds and methods of use thereof as antibacterial agents |
| CN113045477B (zh) * | 2019-12-26 | 2022-11-01 | 中蓝晨光化工研究设计院有限公司 | 一种含氟伯胺中间体的制备方法 |
| CN120794967A (zh) * | 2024-04-10 | 2025-10-17 | 沈阳药科大学 | 联芳基噁唑烷酮类化合物及其应用 |
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| US4948801A (en) | 1988-07-29 | 1990-08-14 | E. I. Du Pont De Nemours And Company | Aminomethyloxooxazolidinyl arylbenzene derivatives useful as antibacterial agents |
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| US5130316A (en) | 1988-07-29 | 1992-07-14 | Du Pont Merck Pharmaceutical Company | Aminomethyloxooxazlidinyl arylbenzene derivatives useful as antibacterial agents |
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| DE4425612A1 (de) | 1994-07-20 | 1996-04-04 | Bayer Ag | 6-gliedrige stickstoffhaltige Heteroaryl-oxazolidinone |
| HRP970049A2 (en) | 1996-02-06 | 1998-04-30 | Bayer Ag | New heteroaryl oxazolidinones |
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| AU1694099A (en) * | 1997-12-26 | 1999-07-19 | Cheil Jedang Corporation | Cephem derivatives and a method for producing the compounds and an antibacterialcomposition containing the compounds |
| BR9907183A (pt) | 1998-01-23 | 2003-06-10 | Versicor Inc | Colet neas combinatórias de oxazolidinona, composições e processos de preparação |
| US6562844B2 (en) | 1998-01-23 | 2003-05-13 | Pharmacia & Upjohn Company | Oxazolidinone combinatorial libraries, compositions and methods of preparation |
| WO1999064417A2 (en) | 1998-06-05 | 1999-12-16 | Astrazeneca Ab | Oxazolidinone derivatives, process for their preparation and pharmaceutical compositions containing them |
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| TW572757B (en) | 1998-08-24 | 2004-01-21 | Bristol Myers Squibb Co | Novel isoxazolinone antibacterial agents |
| GB9821938D0 (en) | 1998-10-09 | 1998-12-02 | Zeneca Ltd | Chemical compounds |
| AU1379900A (en) | 1998-11-17 | 2000-06-05 | Bayer Aktiengesellschaft | Novel substituted phenyloxazolidone derivatives |
| WO2001009107A1 (en) | 1999-07-28 | 2001-02-08 | Pharmacia & Upjohn Company | Oxazolidinones and their use as antiinfectives |
| US6297242B1 (en) | 1999-08-12 | 2001-10-02 | Ortho-Mcneil Pharmaceutical, Inc. | N-substituted amidine and guanidine oxazolidinone antibacterials and methods of use thereof |
| KR20020063888A (ko) | 1999-11-04 | 2002-08-05 | 바실리어 파마슈티카 아게 | 치환된 5-벤질-2,4-디아미노피리미딘 |
| GB9928499D0 (en) | 1999-12-03 | 2000-02-02 | Zeneca Ltd | Chemical processes and intermediates |
| GB0009803D0 (en) | 2000-04-25 | 2000-06-07 | Astrazeneca Ab | Chemical compounds |
| AU5889701A (en) | 2000-06-05 | 2001-12-17 | Dong A Pharm Co Ltd | Novel oxazolidinone derivatives and a process for the preparation thereof |
| DE10034627A1 (de) | 2000-07-17 | 2002-01-31 | Bayer Ag | Aryl-substituierte Oxazolidinone mit Cytokin inhibitorischer Wirkung |
| DE60212959T2 (de) | 2001-04-07 | 2007-02-15 | Astrazeneca Ab | Eine sulfonimid-gruppe enthaltende oxazolidinone als antibiotika |
| GB0108793D0 (en) | 2001-04-07 | 2001-05-30 | Astrazeneca Ab | Chemical compounds |
| GB0108764D0 (en) | 2001-04-07 | 2001-05-30 | Astrazeneca Ab | Chemical compounds |
| GB0108794D0 (en) | 2001-04-07 | 2001-05-30 | Astrazeneca Ab | Chemical compound |
| GB0113299D0 (en) | 2001-06-01 | 2001-07-25 | Astrazeneca Ab | Chemical process & intermediates |
| GB0113297D0 (en) | 2001-06-01 | 2001-07-25 | Astrazeneca Ab | Chemical Process |
| SI1427711T1 (sl) | 2001-09-11 | 2005-12-31 | Astrazeneca Ab | Oksazolidinonski in/ali izoksazolinski derivati kot antibakterijska sredstva |
| GB2396350A (en) | 2001-10-25 | 2004-06-23 | Astrazeneca Ab | Aryl substituted oxazolidinones with antibacterial activity |
| AR038536A1 (es) | 2002-02-25 | 2005-01-19 | Upjohn Co | N-aril-2-oxazolidinona-5- carboxamidas y sus derivados |
| CN1649866A (zh) | 2002-02-28 | 2005-08-03 | 阿斯特拉曾尼卡有限公司 | 3-环状基-5-(含氮5-元环)甲基-噁唑烷酮衍生物及其作为抗菌药物的用途 |
| EP1490059A1 (en) * | 2002-03-29 | 2004-12-29 | Pharmacia & Upjohn Company LLC | Parenteral, intravenous, and oral administration of oxazolidinones for treating diabetic foot infections |
| TW200420573A (en) | 2002-09-26 | 2004-10-16 | Rib X Pharmaceuticals Inc | Bifunctional heterocyclic compounds and methods of making and using same |
| US20040132764A1 (en) | 2002-10-23 | 2004-07-08 | Morphochem Aktiengesellschaft Fuer Kombinatorische Chemie | Antibiotics for the treatment of infections in acidic environments |
| MXPA05005651A (es) | 2002-11-28 | 2005-07-27 | Astrazeneca Ab | Derivados de oxazolidinona y/o isoxazolina como agentes antibacterianos. |
| GB0229521D0 (en) * | 2002-12-19 | 2003-01-22 | Astrazeneca Ab | Chemical compounds |
| GB0229518D0 (en) | 2002-12-19 | 2003-01-22 | Astrazeneca Ab | Chemical compounds |
| GB0229526D0 (en) | 2002-12-19 | 2003-01-22 | Astrazeneca Ab | Chemical compounds |
| TW200500360A (en) | 2003-03-01 | 2005-01-01 | Astrazeneca Ab | Hydroxymethyl compounds |
| JP2006522791A (ja) | 2003-04-09 | 2006-10-05 | ファルマシア・アンド・アップジョン・カンパニー・エルエルシー | 抗微生物性[3.1.0]ビシクロヘキシルフェニルオキサゾリジノン誘導体および類似体 |
| WO2005012271A2 (en) | 2003-07-29 | 2005-02-10 | Rib-X Pharmaceuticals, Inc. | Process for the synthesis of biaryl oxazolidinones |
| SI1656370T1 (sl) | 2003-06-03 | 2012-12-31 | Rib-X Pharmaceuticals, Inc. | Biarilne heterociklične spojine in postopki za njihovo izdelavo in uporabo |
| EP1656370B1 (en) | 2003-06-03 | 2012-08-15 | Rib-X Pharmaceuticals, Inc. | Biaryl heterocyclic compounds and methods of making and using the same |
| WO2005003087A2 (en) | 2003-07-01 | 2005-01-13 | Orchid Chemicals And Pharmaceuticals Ltd. | Oxazole derivatives as antibacterial agents |
| ATE471937T1 (de) | 2003-07-02 | 2010-07-15 | Merck Sharp & Dohme | Cyclopropylgruppensubstituierte oxazolidinonantibiotika und derivate davon |
| JP2007500707A (ja) | 2003-07-29 | 2007-01-18 | リブ−エックス ファーマシューティカルズ,インコーポレイテッド | ビアリールヘテロ環状のアミン、アミドおよび硫黄−含有化合物、並びに該化合物の製造方法および使用方法 |
| AR046782A1 (es) * | 2003-12-17 | 2005-12-21 | Rib X Pharmaceuticals Inc | Compuestos heterociclicos de biarilo halogenados, composiciones farmaceuticas que los contienen, metodos para su elaboracion y su uso como medicamentos. |
| KR100854211B1 (ko) | 2003-12-18 | 2008-08-26 | 동아제약주식회사 | 신규한 옥사졸리디논 유도체, 그의 제조방법 및 이를유효성분으로 하는 항생제용 약학 조성물 |
-
2004
- 2004-12-01 AR ARP040104472A patent/AR046782A1/es unknown
- 2004-12-01 EP EP04812498A patent/EP1713785A1/en not_active Withdrawn
- 2004-12-01 JP JP2006545691A patent/JP2007514782A/ja active Pending
- 2004-12-01 TW TW093136988A patent/TW200526649A/zh unknown
- 2004-12-01 WO PCT/US2004/039988 patent/WO2005061468A1/en not_active Ceased
- 2004-12-01 US US11/001,446 patent/US7129259B2/en not_active Expired - Lifetime
-
2006
- 2006-02-23 US US11/362,133 patent/US20060148869A1/en not_active Abandoned
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