CN103228652B - 单环内酰胺类 - Google Patents
单环内酰胺类 Download PDFInfo
- Publication number
- CN103228652B CN103228652B CN201180057264.5A CN201180057264A CN103228652B CN 103228652 B CN103228652 B CN 103228652B CN 201180057264 A CN201180057264 A CN 201180057264A CN 103228652 B CN103228652 B CN 103228652B
- Authority
- CN
- China
- Prior art keywords
- mmol
- formula
- compound
- preparation
- treated
- 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.)
- Expired - Fee Related
Links
- 0 *N(C=C1O)C(I)=CC1=O Chemical compound *N(C=C1O)C(I)=CC1=O 0.000 description 9
- CVJZGRKFISIOOM-UHFFFAOYSA-N CC(N(C=C1O)O)=CC1=O Chemical compound CC(N(C=C1O)O)=CC1=O CVJZGRKFISIOOM-UHFFFAOYSA-N 0.000 description 2
- LJNZCWXEAIJKJR-ZXSNDDASSA-O CC(C)(C(O)=O)O/N=C(\C(NCC(C(CNC(c1ccc(C(NCC(N(CC2O)O)=CC2O)O)cc1)O)N1S(O)([OH2+])=O)C1=O)=O)/c1c[s]c(N)n1 Chemical compound CC(C)(C(O)=O)O/N=C(\C(NCC(C(CNC(c1ccc(C(NCC(N(CC2O)O)=CC2O)O)cc1)O)N1S(O)([OH2+])=O)C1=O)=O)/c1c[s]c(N)n1 LJNZCWXEAIJKJR-ZXSNDDASSA-O 0.000 description 1
- ANFLTTZTVMOFFU-NHDPSOOVSA-N CC(C)(C)OC(C(C)(C)O/N=C(\C(O)=O)/c1c[s]c(NC(OC(C)(C)C)=O)n1)=O Chemical compound CC(C)(C)OC(C(C)(C)O/N=C(\C(O)=O)/c1c[s]c(NC(OC(C)(C)C)=O)n1)=O ANFLTTZTVMOFFU-NHDPSOOVSA-N 0.000 description 1
- OLWRWHDVDLFNGL-UHFFFAOYSA-N CC(C)(C)OC(C(C)(C)ONC(C(O)=O)c1c[s]c(NC(OC(C)(C)C)=O)n1)=O Chemical compound CC(C)(C)OC(C(C)(C)ONC(C(O)=O)c1c[s]c(NC(OC(C)(C)C)=O)n1)=O OLWRWHDVDLFNGL-UHFFFAOYSA-N 0.000 description 1
- KBVCEVHDOSIFAM-HSOSERFQSA-N CC(C)(C)OC(Nc1nc(C(C(N[C@@H](C(CI)N2)C2=O)=O)=N)c[s]1)=O Chemical compound CC(C)(C)OC(Nc1nc(C(C(N[C@@H](C(CI)N2)C2=O)=O)=N)c[s]1)=O KBVCEVHDOSIFAM-HSOSERFQSA-N 0.000 description 1
- FNJYMQXOXPYJIU-UHFFFAOYSA-N CC(C1)C1C1CC(CCC2=CC(C)=C(C)C=CCC2C)CC1 Chemical compound CC(C1)C1C1CC(CCC2=CC(C)=C(C)C=CCC2C)CC1 FNJYMQXOXPYJIU-UHFFFAOYSA-N 0.000 description 1
- AHSWPKLAQXIXKO-SRBOSORUSA-N CC([C@@H](CO)N1)C1=O Chemical compound CC([C@@H](CO)N1)C1=O AHSWPKLAQXIXKO-SRBOSORUSA-N 0.000 description 1
- FHFSVDXYQFWKPC-UHFFFAOYSA-N CC1(C2)C2CCCC1 Chemical compound CC1(C2)C2CCCC1 FHFSVDXYQFWKPC-UHFFFAOYSA-N 0.000 description 1
- DIQXFDTWUBWBEF-UHFFFAOYSA-N COC(c1cc(-c(nc2)cc(OCc3ccccc3)c2OCc2ccccc2)n[o]1)=O Chemical compound COC(c1cc(-c(nc2)cc(OCc3ccccc3)c2OCc2ccccc2)n[o]1)=O DIQXFDTWUBWBEF-UHFFFAOYSA-N 0.000 description 1
- CVJZGRKFISIOOM-UHFFFAOYSA-O Cc([n+](O)c1)cc(O)c1O Chemical compound Cc([n+](O)c1)cc(O)c1O CVJZGRKFISIOOM-UHFFFAOYSA-O 0.000 description 1
- LMTYNADVCDGSGA-UHFFFAOYSA-O NCC(C(CC=C1)[OH2+])=CC(OCc2ccccc2)=C1OCc1ccccc1 Chemical compound NCC(C(CC=C1)[OH2+])=CC(OCc2ccccc2)=C1OCc1ccccc1 LMTYNADVCDGSGA-UHFFFAOYSA-O 0.000 description 1
- KZNICNPSHKQLFF-UHFFFAOYSA-N O=C(CC1)NC1=O Chemical compound O=C(CC1)NC1=O KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 description 1
- GYZWHOMEDJANIF-UHFFFAOYSA-O O=C(c1ccccc11)N(Cc([nH+]c2)cc(OCc3ccccc3)c2OCc2ccccc2)C1=O Chemical compound O=C(c1ccccc11)N(Cc([nH+]c2)cc(OCc3ccccc3)c2OCc2ccccc2)C1=O GYZWHOMEDJANIF-UHFFFAOYSA-O 0.000 description 1
- GYZWHOMEDJANIF-UHFFFAOYSA-N O=C(c1ccccc11)N(Cc(nc2)cc(OCc3ccccc3)c2OCc2ccccc2)C1=O Chemical compound O=C(c1ccccc11)N(Cc(nc2)cc(OCc3ccccc3)c2OCc2ccccc2)C1=O GYZWHOMEDJANIF-UHFFFAOYSA-N 0.000 description 1
- NNEDRWCGFQMNLA-UHFFFAOYSA-N OCc(nc1)cc(OCc2ccccc2)c1OCc1ccccc1 Chemical compound OCc(nc1)cc(OCc2ccccc2)c1OCc1ccccc1 NNEDRWCGFQMNLA-UHFFFAOYSA-N 0.000 description 1
- YASWZFZIEHDRBD-UHFFFAOYSA-N Oc1cc([IH]I)ncc1O Chemical compound Oc1cc([IH]I)ncc1O YASWZFZIEHDRBD-UHFFFAOYSA-N 0.000 description 1
- XIVUCIKVSMROEI-UHFFFAOYSA-N [O-][n+](c(-c1n[o]c(C(O)=O)c1)c1)cc(OCc2ccccc2)c1OCc1ccccc1 Chemical compound [O-][n+](c(-c1n[o]c(C(O)=O)c1)c1)cc(OCc2ccccc2)c1OCc1ccccc1 XIVUCIKVSMROEI-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles not condensed and containing further heterocyclic 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41757510P | 2010-11-29 | 2010-11-29 | |
| US61/417,575 | 2010-11-29 | ||
| PCT/IB2011/055104 WO2012073138A1 (en) | 2010-11-29 | 2011-11-15 | Monobactams |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103228652A CN103228652A (zh) | 2013-07-31 |
| CN103228652B true CN103228652B (zh) | 2015-02-18 |
Family
ID=45315854
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201180057264.5A Expired - Fee Related CN103228652B (zh) | 2010-11-29 | 2011-11-15 | 单环内酰胺类 |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US20120302542A1 (enExample) |
| EP (1) | EP2646436B1 (enExample) |
| JP (1) | JP5777725B2 (enExample) |
| KR (1) | KR101514587B1 (enExample) |
| CN (1) | CN103228652B (enExample) |
| AR (1) | AR084001A1 (enExample) |
| AU (1) | AU2011336209B2 (enExample) |
| CA (1) | CA2815821C (enExample) |
| DK (1) | DK2646436T3 (enExample) |
| ES (1) | ES2542431T3 (enExample) |
| IL (1) | IL226052A0 (enExample) |
| MX (1) | MX2013005994A (enExample) |
| SG (1) | SG190007A1 (enExample) |
| TW (1) | TW201247661A (enExample) |
| UY (1) | UY33754A (enExample) |
| WO (1) | WO2012073138A1 (enExample) |
| ZA (1) | ZA201304479B (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11230543B2 (en) | 2015-12-15 | 2022-01-25 | Merck Sharp & Dohme Corp. | Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015099107A1 (ja) | 2013-12-26 | 2015-07-02 | 塩野義製薬株式会社 | 含窒素6員環誘導体およびそれらを含有する医薬組成物 |
| SI3122745T1 (sl) | 2014-03-24 | 2019-05-31 | Novartis Ag | Organske spojine monobaktama za zdravljenje bakterijskih infekcij |
| HRP20201423T1 (hr) * | 2015-09-23 | 2020-12-11 | Novartis Ag | Soli i čvrsti oblici antibiotika monobaktam |
| CN105481812B (zh) * | 2015-11-30 | 2020-04-21 | 重庆天奕恒化科技有限公司 | 一种5-苄氧基-4-氧代-4h-吡喃-2-羧酸的制备方法 |
| MA43811A (fr) | 2016-03-07 | 2018-11-28 | Merck Sharp & Dohme | Composés d'arylmonobactame bicycliques et leurs méthodes d'utilisation pour le traitement des infections bactériennes |
| WO2017180794A1 (en) * | 2016-04-13 | 2017-10-19 | Skyline Antiinfectives, Inc. | Deuterated o-sulfated beta-lactam hydroxamic acids and deuterated n-sulfated beta-lactams |
| 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 |
| AU2018311521B2 (en) | 2017-08-02 | 2022-03-03 | Novartis Ag | Process for preparing 1 -(((Z)-(1 -(2-aminothiazol-4-yl)-2-oxo-2-(((3S,4R)-2-oxo-4-((2-oxooxazolidin-3-y l)methyl)-1 -sulfoazetidin-3- yl)amino)ethylidene)amino)oxy)cyclopropane carboxylic acid |
| ES2968467T3 (es) | 2017-10-02 | 2024-05-09 | Merck Sharp & Dohme Llc | Compuestos monobactámicos de cromano para el tratamiento de infecciones bacterianas |
| US10513504B2 (en) | 2018-03-08 | 2019-12-24 | Apotex Inc. | Processes for the preparation of apalutamide and intermediates thereof |
| WO2021098840A1 (zh) * | 2019-11-22 | 2021-05-27 | 南京明德新药研发有限公司 | 磺酰脲环取代的单环β-内酰胺类抗生素 |
| CR20220316A (es) | 2019-12-06 | 2022-10-07 | Vertex Pharma | Tetrahidrofuranos sustituidos como moduladores de canales de sodio |
| CN111303144B (zh) * | 2019-12-13 | 2020-11-27 | 苏州信诺维医药科技有限公司 | 一种治疗细菌感染的化合物 |
| US11780832B2 (en) | 2021-03-31 | 2023-10-10 | Fedora Pharmaceuticals Inc. | Lactivicin compounds, their preparation and use as antibacterial agents |
| WO2022235077A1 (ko) * | 2021-05-07 | 2022-11-10 | 한국생명공학연구원 | 신규 사이드로포어 화합물 및 이를 이용한 금속 나노입자 복합체 |
| JP2024522292A (ja) | 2021-06-04 | 2024-06-13 | バーテックス ファーマシューティカルズ インコーポレイテッド | ナトリウムチャネルのモジュレーターとしてのn-(ヒドロキシアルキル(ヘテロ)アリール)テトラヒドロフランカルボキサミド |
| JP7671398B2 (ja) * | 2021-11-18 | 2025-05-01 | メルク・シャープ・アンド・ドーム・エルエルシー | クロマンアミジンモノバクタム抗生物質 |
| MX2024006075A (es) | 2021-11-18 | 2024-05-30 | Merck Sharp & Dohme Llc | Antibioticos monobactamicos de cromano amidina. |
| CN115304594B (zh) * | 2022-10-12 | 2023-02-14 | 苏州二叶制药有限公司 | 磺酰脲环取代的化合物的盐型及其晶型 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101410111A (zh) * | 2005-12-07 | 2009-04-15 | 巴斯利尔药物股份公司 | 单环-内酰胺类抗生素与β-内酰胺酶抑制剂的有效的联合应用 |
| WO2010070523A1 (en) * | 2008-12-19 | 2010-06-24 | Pfizer Inc. | Monocarbams |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0246786A1 (en) * | 1986-05-23 | 1987-11-25 | The Upjohn Company | N-1 subsituted sulfonylaminocarbonyl, C-4 substituted monobactams |
| CN102964296B (zh) | 2007-03-28 | 2015-03-25 | 阿普泰克斯科技公司 | 去铁酮的氟化衍生物 |
-
2011
- 2011-11-15 CA CA2815821A patent/CA2815821C/en not_active Expired - Fee Related
- 2011-11-15 KR KR1020137016718A patent/KR101514587B1/ko not_active Expired - Fee Related
- 2011-11-15 JP JP2013541445A patent/JP5777725B2/ja not_active Expired - Fee Related
- 2011-11-15 ES ES11794237.5T patent/ES2542431T3/es active Active
- 2011-11-15 CN CN201180057264.5A patent/CN103228652B/zh not_active Expired - Fee Related
- 2011-11-15 EP EP11794237.5A patent/EP2646436B1/en not_active Not-in-force
- 2011-11-15 SG SG2013031752A patent/SG190007A1/en unknown
- 2011-11-15 WO PCT/IB2011/055104 patent/WO2012073138A1/en not_active Ceased
- 2011-11-15 DK DK11794237.5T patent/DK2646436T3/en active
- 2011-11-15 AU AU2011336209A patent/AU2011336209B2/en not_active Ceased
- 2011-11-15 MX MX2013005994A patent/MX2013005994A/es active IP Right Grant
- 2011-11-24 TW TW100143172A patent/TW201247661A/zh unknown
- 2011-11-25 AR ARP110104404A patent/AR084001A1/es not_active Application Discontinuation
- 2011-11-28 UY UY0001033754A patent/UY33754A/es not_active Application Discontinuation
- 2011-11-29 US US13/306,581 patent/US20120302542A1/en not_active Abandoned
-
2013
- 2013-02-27 US US13/778,670 patent/US20130252935A1/en not_active Abandoned
- 2013-04-29 IL IL226052A patent/IL226052A0/en unknown
- 2013-06-18 ZA ZA2013/04479A patent/ZA201304479B/en unknown
-
2015
- 2015-01-29 US US14/608,826 patent/US20150148326A1/en not_active Abandoned
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101410111A (zh) * | 2005-12-07 | 2009-04-15 | 巴斯利尔药物股份公司 | 单环-内酰胺类抗生素与β-内酰胺酶抑制剂的有效的联合应用 |
| WO2010070523A1 (en) * | 2008-12-19 | 2010-06-24 | Pfizer Inc. | Monocarbams |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11230543B2 (en) | 2015-12-15 | 2022-01-25 | Merck Sharp & Dohme Corp. | Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections |
Also Published As
| Publication number | Publication date |
|---|---|
| DK2646436T3 (en) | 2015-06-29 |
| SG190007A1 (en) | 2013-06-28 |
| JP5777725B2 (ja) | 2015-09-09 |
| HK1184462A1 (en) | 2014-01-24 |
| CN103228652A (zh) | 2013-07-31 |
| CA2815821A1 (en) | 2012-06-07 |
| US20150148326A1 (en) | 2015-05-28 |
| AR084001A1 (es) | 2013-04-17 |
| MX2013005994A (es) | 2013-07-15 |
| ZA201304479B (en) | 2014-03-26 |
| IL226052A0 (en) | 2013-06-27 |
| TW201247661A (en) | 2012-12-01 |
| UY33754A (es) | 2012-06-29 |
| ES2542431T3 (es) | 2015-08-05 |
| CA2815821C (en) | 2015-07-07 |
| AU2011336209B2 (en) | 2015-03-19 |
| US20120302542A1 (en) | 2012-11-29 |
| AU2011336209A1 (en) | 2013-05-30 |
| US20130252935A1 (en) | 2013-09-26 |
| EP2646436B1 (en) | 2015-05-27 |
| EP2646436A1 (en) | 2013-10-09 |
| KR101514587B1 (ko) | 2015-04-22 |
| WO2012073138A1 (en) | 2012-06-07 |
| JP2013544276A (ja) | 2013-12-12 |
| KR20130112054A (ko) | 2013-10-11 |
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