HRP20210693T1 - Inhibitori beta-laktamaze - Google Patents
Inhibitori beta-laktamaze Download PDFInfo
- Publication number
- HRP20210693T1 HRP20210693T1 HRP20210693TT HRP20210693T HRP20210693T1 HR P20210693 T1 HRP20210693 T1 HR P20210693T1 HR P20210693T T HRP20210693T T HR P20210693TT HR P20210693 T HRP20210693 T HR P20210693T HR P20210693 T1 HRP20210693 T1 HR P20210693T1
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- Croatia
- Prior art keywords
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- compound according
- alkyl
- hydrogen
- pharmaceutically acceptable
- Prior art date
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- 239000003781 beta lactamase inhibitor Substances 0.000 title 1
- 229940126813 beta-lactamase inhibitor Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 4
- 150000001204 N-oxides Chemical class 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 239000011737 fluorine Substances 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 3
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 2
- 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 2
- 229960003644 aztreonam Drugs 0.000 claims 2
- 239000003782 beta lactam antibiotic agent Substances 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 239000002132 β-lactam antibiotic Substances 0.000 claims 2
- 229940124586 β-lactam antibiotics Drugs 0.000 claims 2
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- -1 -C(O)-R4 Chemical group 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- 229930186147 Cephalosporin Natural products 0.000 claims 1
- 229930182555 Penicillin Natural products 0.000 claims 1
- JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 208000022362 bacterial infectious disease Diseases 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- YZBQHRLRFGPBSL-RXMQYKEDSA-N carbapenem Chemical compound C1C=CN2C(=O)C[C@H]21 YZBQHRLRFGPBSL-RXMQYKEDSA-N 0.000 claims 1
- 229940124587 cephalosporin Drugs 0.000 claims 1
- 150000001780 cephalosporins Chemical class 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 229940049954 penicillin Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- 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
- A61K31/69—Boron compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
- Pyrrole Compounds (AREA)
Claims (15)
1. Spoj formule (II) ili njegove farmaceutski prihvatljive soli, steroizomeri ili N-oksidi:
[image]
naznačen time što:
M je vodik, -CN, -C(O)-R4, ili alkinil;
svaki R1 i R2 je neovisno vodik, fluor, klor, C1-C6 alkil, ili CF3;
n je neovisno 0, 1, 2, 3, 4, 5, ili 6;
X1 je -OR4 ili F;
Z je >C=O, >C=S, ili >SO2;
R3 je -R30OC(O)R31 ili -R30OC(O)OR31;
R30 je -CH2- ili -CH(CH3)-;
R31 je C1-C12 alkil, aril, C3-C8 cikloalkil, ili C3-C8 heterocikloalkil;
Ra, Rb, i Rc su neovisno vodik, fluor, klor, brom, C1-C6 alkil, C3-C6 cikloalkil, heretocikloalkil, aril, heteroaril, -OR4, -NR4R5, ili -SR4;
R4 i R5 su neovisno vodik ili C1-C6 alkil; i
Rd je vodik ili C1-C4 alkil.
2. Spoj prema patentnom zahtjevu 1, naznačen time što Ra, Rb, i Rc su neovisno vodik, fluor, C1-C6 alkil, -OR4, -NR4R5, ili -SR4.
3. Spoj prema patentnom zahtjevu 1, naznačen time što Ra, Rb, i Rc su neovisno vodik, fluor, klor, -OH, ili -OCH3.
4. Spoj prema bilo kojem od patentnih zahtjeva 1-3, naznačen time što Ra, Rb, i Rc su vodik.
5. Spoj prema bilo kojem od patentnih zahtjeva 1-4, naznačen time što X1 je -OH.
6. Spoj prema bilo kojem od patentnih zahtjeva 1-5, naznačen time što Rd je vodik.
7. Spoj prema bilo kojem od patentnih zahtjeva 1-6, naznačen time što Z je >C=O.
8. Spoj prema bilo kojem od patentnih zahtjeva 1-7, naznačen time što n je 0, 1, 2, ili 3.
9. Spoj prema bilo kojem od patentnih zahtjeva 1-8, naznačen time što svaki R1 i R2 su vodik.
10. Spoj prema bilo kojem od patentnih zahtjeva 1-9, naznačen time što R4 je C1-C6 alkil.
11. Spoj prema patentnom zahtjevu 1, naznačen time što ima strukturu:
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ili njegova farmaceutski prihvatljiva sol, N-oksid ili stereoizomer.
12. Spoj prema patentnom zahtjevu 1, naznačen time što ima strukturu:
[image]
ili njegova farmaceutski prihvatljiva sol, N-oksid ili stereoizomer.
13. Farmaceutski pripravak naznačen time što sadrži najmanje jedan spoj iz bilo kojeg od patentnih zahtjeva 1-12, ili njegovu farmaceutski prihvatljivu sol, N-oksid ili stereoizomer, i farmaceutski prihvatljivu pomoćnu tvar.
14. Farmaceutski pripravak prema patentnom zahtjevu 13, naznačen time što nadalje sadrži beta-laktamski antibiotik odabran od penicilina, cefalosporina, karbapenema, monobaktama, premoštenog monobaktama, i njihove kombinacije.
15. Spoj prema bilo kojem od patentnih zahtjeva 1-12 u kombinaciji s terapijski učinkovitom količinom beta-laktamskog antibiotika za uporabu u postupku liječenja bakterijske infekcije kod subjekta.
Applications Claiming Priority (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462010969P | 2014-06-11 | 2014-06-11 | |
| US201462010940P | 2014-06-11 | 2014-06-11 | |
| US201462010968P | 2014-06-11 | 2014-06-11 | |
| US201562118227P | 2015-02-19 | 2015-02-19 | |
| PCT/US2015/035407 WO2015191907A1 (en) | 2014-06-11 | 2015-06-11 | Beta-lactamase inhibitors |
| EP15806746.2A EP3154989B1 (en) | 2014-06-11 | 2015-06-11 | Beta-lactamase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20210693T1 true HRP20210693T1 (hr) | 2021-06-11 |
Family
ID=54834346
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20210693TT HRP20210693T1 (hr) | 2014-06-11 | 2021-05-04 | Inhibitori beta-laktamaze |
Country Status (16)
| Country | Link |
|---|---|
| US (4) | US9637504B2 (hr) |
| EP (2) | EP3154989B1 (hr) |
| JP (2) | JP6622721B2 (hr) |
| KR (2) | KR20220065084A (hr) |
| CN (2) | CN106687465B (hr) |
| AU (2) | AU2015274530B2 (hr) |
| BR (1) | BR112016027988B1 (hr) |
| CA (1) | CA2950917C (hr) |
| ES (1) | ES2874579T3 (hr) |
| HR (1) | HRP20210693T1 (hr) |
| IL (2) | IL249043B (hr) |
| PL (1) | PL3154989T3 (hr) |
| PT (1) | PT3154989T (hr) |
| RU (1) | RU2686740C2 (hr) |
| WO (1) | WO2015191907A1 (hr) |
| ZA (1) | ZA201608847B (hr) |
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| RS60310B1 (sr) | 2010-08-10 | 2020-07-31 | Rempex Pharmaceuticals Inc | Ciklični derivati estra boronske kiseline, postupak za pripremu injihove terapeutske upotrebe |
| EP2928898B1 (en) | 2012-12-07 | 2021-04-14 | Venatorx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| ES2730013T3 (es) | 2013-01-10 | 2019-11-07 | Venatorx Pharmaceuticals Inc | Inhibidores de betalactamasa |
| EP2970340B1 (en) | 2013-03-14 | 2020-02-12 | Venatorx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| CA2947041A1 (en) * | 2014-05-19 | 2015-11-26 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| US9511142B2 (en) | 2014-06-11 | 2016-12-06 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| EP3154989B1 (en) | 2014-06-11 | 2021-03-24 | Venatorx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| US20150361108A1 (en) * | 2014-06-11 | 2015-12-17 | VenatoRx Pharmaceuticals, Inc. | Orally bioavailable beta-lactamase inhibitors |
| WO2016081297A1 (en) | 2014-11-18 | 2016-05-26 | Rempex Pharmaceuticals, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| CN107207537B (zh) | 2014-12-19 | 2019-05-31 | 莱姆派克斯制药公司 | 用于生产硼酸衍生物的设备和连续流方法 |
| US20180051041A1 (en) | 2015-03-17 | 2018-02-22 | Rempex Pharmaceuticals, Inc. | Boronic acid derivatives and therapeutic uses thereof |
| CN108472284A (zh) | 2015-09-11 | 2018-08-31 | 维纳拓尔斯制药公司 | β-内酰胺酶抑制剂 |
| WO2017100537A1 (en) | 2015-12-10 | 2017-06-15 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| MY196909A (en) | 2016-06-30 | 2023-05-09 | Qpex Biopharma Inc | Boronic acid derivatives and therapeutic uses thereof |
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