BRPI0809147A2 - Medicamentos combinados para tratamento de infecções bacterianas - Google Patents
Medicamentos combinados para tratamento de infecções bacterianas Download PDFInfo
- Publication number
- BRPI0809147A2 BRPI0809147A2 BRPI0809147-1A BRPI0809147A BRPI0809147A2 BR PI0809147 A2 BRPI0809147 A2 BR PI0809147A2 BR PI0809147 A BRPI0809147 A BR PI0809147A BR PI0809147 A2 BRPI0809147 A2 BR PI0809147A2
- Authority
- BR
- Brazil
- Prior art keywords
- pharmaceutically acceptable
- formula
- substituted
- acceptable salt
- alkyl
- Prior art date
Links
- 239000003814 drug Substances 0.000 title claims description 20
- 208000035143 Bacterial infection Diseases 0.000 title claims description 15
- 208000022362 bacterial infectious disease Diseases 0.000 title claims description 15
- 229940079593 drug Drugs 0.000 title description 10
- 150000001875 compounds Chemical class 0.000 claims description 88
- 150000003839 salts Chemical class 0.000 claims description 84
- 230000003115 biocidal effect Effects 0.000 claims description 60
- 125000001424 substituent group Chemical group 0.000 claims description 58
- YZBQHRLRFGPBSL-RXMQYKEDSA-N carbapenem Chemical compound C1C=CN2C(=O)C[C@H]21 YZBQHRLRFGPBSL-RXMQYKEDSA-N 0.000 claims description 57
- -1 oxyimino group Chemical group 0.000 claims description 52
- 125000000623 heterocyclic group Chemical group 0.000 claims description 42
- 239000003242 anti bacterial agent Substances 0.000 claims description 30
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 29
- 229910052757 nitrogen Inorganic materials 0.000 claims description 28
- WZPBZJONDBGPKJ-VEHQQRBSSA-N aztreonam Chemical compound O=C1N(S([O-])(=O)=O)[C@@H](C)[C@@H]1NC(=O)C(=N/OC(C)(C)C(O)=O)\C1=CSC([NH3+])=N1 WZPBZJONDBGPKJ-VEHQQRBSSA-N 0.000 claims description 25
- 229960003644 aztreonam Drugs 0.000 claims description 25
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 24
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 23
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims description 21
- 229910052739 hydrogen Inorganic materials 0.000 claims description 21
- 239000001257 hydrogen Substances 0.000 claims description 20
- 241000894006 Bacteria Species 0.000 claims description 17
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 17
- 229910052717 sulfur Inorganic materials 0.000 claims description 17
- 239000011593 sulfur Chemical group 0.000 claims description 17
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 16
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 15
- 125000005842 heteroatom Chemical group 0.000 claims description 15
- 238000000034 method Methods 0.000 claims description 15
- 229910052760 oxygen Chemical group 0.000 claims description 14
- 239000001301 oxygen Chemical group 0.000 claims description 14
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- 229940127557 pharmaceutical product Drugs 0.000 claims description 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 12
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 12
- 208000015181 infectious disease Diseases 0.000 claims description 12
- 229910052736 halogen Inorganic materials 0.000 claims description 10
- 150000002367 halogens Chemical group 0.000 claims description 10
- 206010035664 Pneumonia Diseases 0.000 claims description 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 8
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 7
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- ZSKVGTPCRGIANV-ZXFLCMHBSA-N imipenem Chemical compound C1C(SCC\N=C\N)=C(C(O)=O)N2C(=O)[C@H]([C@H](O)C)[C@H]21 ZSKVGTPCRGIANV-ZXFLCMHBSA-N 0.000 claims description 7
- 229960002182 imipenem Drugs 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 7
- 125000003545 alkoxy group Chemical group 0.000 claims description 6
- DHSUYTOATWAVLW-WFVMDLQDSA-N cilastatin Chemical compound CC1(C)C[C@@H]1C(=O)N\C(=C/CCCCSC[C@H](N)C(O)=O)C(O)=O DHSUYTOATWAVLW-WFVMDLQDSA-N 0.000 claims description 6
- 229960004912 cilastatin Drugs 0.000 claims description 6
- CWXYHOHYCJXYFQ-UHFFFAOYSA-N Betamipron Chemical compound OC(=O)CCNC(=O)C1=CC=CC=C1 CWXYHOHYCJXYFQ-UHFFFAOYSA-N 0.000 claims description 4
- 208000008745 Healthcare-Associated Pneumonia Diseases 0.000 claims description 4
- 208000036209 Intraabdominal Infections Diseases 0.000 claims description 4
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- DMJNNHOOLUXYBV-PQTSNVLCSA-N meropenem Chemical compound C=1([C@H](C)[C@@H]2[C@H](C(N2C=1C(O)=O)=O)[C@H](O)C)S[C@@H]1CN[C@H](C(=O)N(C)C)C1 DMJNNHOOLUXYBV-PQTSNVLCSA-N 0.000 claims description 4
- 208000019206 urinary tract infection Diseases 0.000 claims description 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 3
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- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims description 3
- 206010069748 Burkholderia pseudomallei infection Diseases 0.000 claims description 3
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- 230000005713 exacerbation Effects 0.000 claims description 3
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- 230000002195 synergetic effect Effects 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 2
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- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 1
- JUZNIMUFDBIJCM-ANEDZVCMSA-N Invanz Chemical compound O=C([C@H]1NC[C@H](C1)SC=1[C@H](C)[C@@H]2[C@H](C(N2C=1C(O)=O)=O)[C@H](O)C)NC1=CC=CC(C(O)=O)=C1 JUZNIMUFDBIJCM-ANEDZVCMSA-N 0.000 claims 1
- 208000035389 Ring chromosome 6 syndrome Diseases 0.000 claims 1
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- AVAACINZEOAHHE-VFZPANTDSA-N doripenem Chemical compound C=1([C@H](C)[C@@H]2[C@H](C(N2C=1C(O)=O)=O)[C@H](O)C)S[C@@H]1CN[C@H](CNS(N)(=O)=O)C1 AVAACINZEOAHHE-VFZPANTDSA-N 0.000 claims 1
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- IAZDPXIOMUYVGZ-WFGJKAKNSA-N Dimethyl sulfoxide Chemical compound [2H]C([2H])([2H])S(=O)C([2H])([2H])[2H] IAZDPXIOMUYVGZ-WFGJKAKNSA-N 0.000 description 10
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
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- Animal Behavior & Ethology (AREA)
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- Public Health (AREA)
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- Pharmacology & Pharmacy (AREA)
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- Communicable Diseases (AREA)
- Pulmonology (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| EP07006053 | 2007-03-23 | ||
| EP07006053.8 | 2007-03-23 | ||
| PCT/EP2008/053336 WO2008116813A2 (en) | 2007-03-23 | 2008-03-19 | Combination medicaments for treating bacterial infections |
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| BRPI0809147A2 true BRPI0809147A2 (pt) | 2014-08-26 |
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| BRPI0809147-1A BRPI0809147A2 (pt) | 2007-03-23 | 2008-03-19 | Medicamentos combinados para tratamento de infecções bacterianas |
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| WO (1) | WO2008116813A2 (enExample) |
| ZA (1) | ZA200906349B (enExample) |
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| KR101320718B1 (ko) * | 2007-03-23 | 2013-10-21 | 바실리어 파마슈티카 아게 | 세균 감염 치료용 조합 약제 |
| TR201102640T1 (tr) * | 2008-12-01 | 2011-08-22 | Glade Organics Private Limited | Aztreonamın meropenem ve ertapenem adlı karbapenemlerle oluşturduğu sinerjik kombinasyonlar. |
| CA2744756C (en) | 2008-12-19 | 2013-05-28 | Pfizer Inc. | Monocarbams and their use as antibacterial agent |
| HUE048859T2 (hu) | 2010-08-10 | 2020-08-28 | Rempex Pharmaceuticals Inc | Gyûrûs bórsavészter származékok, eljárás elõállításukra, és terápiás alkalmazásuk |
| KR101315483B1 (ko) * | 2011-06-23 | 2013-10-07 | 주식회사 아리바이오 | 항생제 및 라이소포스파티딜콜린을 포함하는 면역 증강 또는 세균성 감염 질환 치료용 조성물 |
| WO2013033461A1 (en) | 2011-08-31 | 2013-03-07 | Rempex Pharmaceuticals, Inc. | Heterocyclic boronic acid ester derivatives and therapeutic uses thereof |
| UY34585A (es) | 2012-01-24 | 2013-09-02 | Aicuris Gmbh & Co Kg | Compuestos b-lactámicos sustituidos con amidina, su preparación y uso |
| US9156858B2 (en) | 2012-05-23 | 2015-10-13 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US10561675B2 (en) | 2012-06-06 | 2020-02-18 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| US9241947B2 (en) | 2013-01-04 | 2016-01-26 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| CA2894891A1 (en) | 2013-01-04 | 2014-07-10 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US9101638B2 (en) | 2013-01-04 | 2015-08-11 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| BR112015016002A2 (pt) | 2013-01-04 | 2017-07-11 | Rempex Pharmaceuticals Inc | compostos, composições farmacêuticas, complexos químicos e respectivos usos e método para tratar ou prevenir infecção bacteriana |
| ES2750805T3 (es) | 2014-05-05 | 2020-03-27 | Rempex Pharmaceuticals Inc | Síntesis de sales de boronato y usos de las mismas |
| WO2015171398A1 (en) | 2014-05-05 | 2015-11-12 | Rempex Pharmaceuticals, Inc. | Salts and polymorphs of cyclic boronic acid ester derivatives and therapeutic uses thereof |
| EA201691988A1 (ru) | 2014-05-19 | 2017-06-30 | Ремпекс Фармасьютикалз, Инк. | Производные бороновой кислоты и их терапевтическое применение |
| US10206937B2 (en) | 2014-07-01 | 2019-02-19 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| WO2016081297A1 (en) | 2014-11-18 | 2016-05-26 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| WO2016149393A1 (en) | 2015-03-17 | 2016-09-22 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| RU2618433C2 (ru) * | 2015-08-10 | 2017-05-03 | Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Санкт-Петербургский государственный университет" (СПбГУ) | Антимикробная комбинация в отношении устойчивых к карбапенемам грамотрицательных бактерий вида pseudomonas aeruginosa, продуцирующих металло-β-лактамазу |
| AU2017290060B2 (en) | 2016-06-30 | 2021-07-22 | Qpex Biopharma, Inc | Boronic acid derivatives and therapeutic uses thereof |
| CN107641119B (zh) * | 2016-07-21 | 2019-11-08 | 中国科学院上海药物研究所 | 单环β-内酰胺-铁载体轭合物及其制备方法和用途 |
| RU2666619C2 (ru) * | 2016-12-01 | 2018-09-11 | Федеральное государственное бюджетное образовательное учреждение высшего образования "Санкт-Петербургский государственный университет" (СПбГУ) | АНТИМИКРОБНАЯ КОМБИНАЦИЯ В ОТНОШЕНИИ УСТОЙЧИВЫХ К КАРБАПЕНЕМАМ ГРАМОТРИЦАТЕЛЬНЫХ БАКТЕРИЙ ВИДА ACINETOBACTER BAUMANNII, ПРОДУЦИРУЮЩИХ МЕТАЛЛО-β-ЛАКТАМАЗУ |
| EP3558987A1 (en) | 2016-12-21 | 2019-10-30 | AiCuris GmbH & Co. KG | COMBINATION THERAPY WITH AMIDINE SUBSTITUTED ß-LACTAM COMPOUNDS AND ß-LACTAMASE INHIBITORS FOR INFECTIONS WITH ANTIBIOTIC RESISTANT BACTERIAL STRAINS |
| BR112020007138B1 (pt) | 2017-10-11 | 2023-03-21 | Qpex Biopharma, Inc | Derivados de ácido borônico, métodos de síntese, composição farmacêutica e uso dos mesmos |
| WO2019144969A1 (zh) | 2018-01-29 | 2019-08-01 | 南京明德新药研发股份有限公司 | 用于治疗细菌感染的单环β-内酰胺化合物 |
| EP3781576B1 (en) | 2018-04-20 | 2024-06-12 | Qpex Biopharma, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| EP3901150B1 (en) | 2018-12-18 | 2025-12-03 | Shenzhen Optimum Biological Technology Co., Ltd | Monocyclic beta-lactam compound for use in the treatment of pneumonia |
| WO2020168265A1 (en) | 2019-02-14 | 2020-08-20 | Singapore Eye Research Institute | Antibacterial compositions |
| WO2021121387A1 (zh) | 2019-12-19 | 2021-06-24 | 南京明德新药研发有限公司 | 化合物在制药中的应用 |
Family Cites Families (8)
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|---|---|---|---|---|
| GB1575803A (en) | 1976-03-09 | 1980-10-01 | Fujisawa Pharmaceutical Co | 3,7 disubstituted 3 cephem 4 carboxylic acid compounds andprocesses for the preparation thereof |
| US4822786A (en) | 1986-07-01 | 1989-04-18 | Kaken Pharmaceutical Co., Ltd. | Cephalosporin compounds, and antibacterial agents |
| US5888998A (en) | 1997-04-24 | 1999-03-30 | Synphar Laboratories, Inc. | 2-oxo-1-azetidine sulfonic acid derivatives as potent β-lactamase inhibitors |
| US5994340A (en) * | 1997-08-29 | 1999-11-30 | Synphar Laboratories, Inc. | Azetidinone derivatives as β-lactamase inhibitors |
| ATE298750T1 (de) * | 2000-09-14 | 2005-07-15 | Pantherix Ltd | 3-(heteroarylacetamido)-2-oxo-azetidin-1- sulfonsäure derivate als antibakterielle mittel |
| US20050065141A1 (en) * | 2003-07-31 | 2005-03-24 | Odink Debra A. | Carbapenems useful in treating and preventing pulmonary infections, pharmaceutical compositions thereof and modes of administration thereof |
| CA2783572C (en) * | 2005-12-07 | 2016-08-09 | Basilea Pharmaceutica Ag | Useful combinations of monobactam antibiotics with beta-lactamase inhibitors |
| KR101320718B1 (ko) * | 2007-03-23 | 2013-10-21 | 바실리어 파마슈티카 아게 | 세균 감염 치료용 조합 약제 |
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- 2013-08-19 JP JP2013169657A patent/JP5779209B2/ja not_active Expired - Fee Related
Also Published As
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| CA2680018C (en) | 2014-01-07 |
| EP2124942B1 (en) | 2016-04-27 |
| EP2124942A2 (en) | 2009-12-02 |
| JP5779209B2 (ja) | 2015-09-16 |
| MX2009009918A (es) | 2009-10-19 |
| US8486929B2 (en) | 2013-07-16 |
| US20130274238A1 (en) | 2013-10-17 |
| US8809315B2 (en) | 2014-08-19 |
| ZA200906349B (en) | 2010-06-30 |
| CN101641095A (zh) | 2010-02-03 |
| WO2008116813A2 (en) | 2008-10-02 |
| AU2008231854B2 (en) | 2013-03-21 |
| JP2010521517A (ja) | 2010-06-24 |
| KR20090122357A (ko) | 2009-11-27 |
| KR101320718B1 (ko) | 2013-10-21 |
| WO2008116813A3 (en) | 2009-01-22 |
| NZ579375A (en) | 2012-02-24 |
| AU2008231854A1 (en) | 2008-10-02 |
| RU2488394C2 (ru) | 2013-07-27 |
| CN101641095B (zh) | 2012-10-31 |
| CA2680018A1 (en) | 2008-10-02 |
| JP2013253094A (ja) | 2013-12-19 |
| HK1138184A1 (en) | 2010-08-20 |
| RU2009139004A (ru) | 2011-04-27 |
| WO2008116813A9 (en) | 2008-11-27 |
| US20100144699A1 (en) | 2010-06-10 |
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| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |