SG11201901658PA - Beta-lactamase inhibitor compounds - Google Patents
Beta-lactamase inhibitor compoundsInfo
- Publication number
- SG11201901658PA SG11201901658PA SG11201901658PA SG11201901658PA SG11201901658PA SG 11201901658P A SG11201901658P A SG 11201901658PA SG 11201901658P A SG11201901658P A SG 11201901658PA SG 11201901658P A SG11201901658P A SG 11201901658PA SG 11201901658P A SG11201901658P A SG 11201901658PA
- Authority
- SG
- Singapore
- Prior art keywords
- international
- street
- drive
- beta
- english
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 239000003781 beta lactamase inhibitor Substances 0.000 title abstract 2
- 229940126813 beta-lactamase inhibitor Drugs 0.000 title abstract 2
- 229940126085 β‑Lactamase Inhibitor Drugs 0.000 title abstract 2
- 239000003814 drug Substances 0.000 abstract 5
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 229940079593 drug Drugs 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 208000035143 Bacterial infection Diseases 0.000 abstract 1
- 235000018185 Betula X alpestris Nutrition 0.000 abstract 1
- 235000018212 Betula X uliginosa Nutrition 0.000 abstract 1
- 241000269333 Caudata Species 0.000 abstract 1
- 241000183024 Populus tremula Species 0.000 abstract 1
- 208000022362 bacterial infectious disease Diseases 0.000 abstract 1
- 239000003782 beta lactam antibiotic agent Substances 0.000 abstract 1
- 208000015181 infectious disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 102220240796 rs553605556 Human genes 0.000 abstract 1
- 239000002132 β-lactam antibiotic Substances 0.000 abstract 1
- 229940124586 β-lactam antibiotics Drugs 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
-
- 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
- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
- A61K31/546—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
-
- 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
- A61P31/04—Antibacterial agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B43/00—Formation or introduction of functional groups containing nitrogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D211/78—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0834—Compounds having one or more O-Si linkage
- C07F7/0892—Compounds with a Si-O-N linkage
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 22 March 2018 (22.03.2018) WIP0 I PCT omit VIII °nolo III 011110110111 °num oimIE (10) International Publication Number WO 2018/053215 Al (51) International Patent Classification: C07D 471/08 (2006.01) A61K 31/439 (2006.01) CO7D 211/78 (2006.01) A61P 31/04 (2006.01) (21) International Application Number: PCT/US2017/051692 (22) International Filing Date: 15 September 2017 (15.09.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/395,464 16 September 2016 (16.09.2016) US 62/456,423 08 February 2017 (08.02.2017) US (71) Applicant: ENTASIS THERAPEUTICS LIMITED [GB/GB]; Two Kingdom Street, London W2 6BD (GB). (72) Inventors; and (71) Applicants: BASARAB, Gregory, S. [US/US]; Enta- sis Therapeutics Limited, 35 Gatehouse Drive, Waltham, MA 02451 (US). MOSS, Bill [GB/GB]; Woodlands Wil- lowmead Drive, Prestbury, Cheshire SK10 4BU (GB). (72) Inventors: COMITA-PREVOIR, Janelle; 11 Prospect Street, Northborough, MA 01532 (US). DU- RAND-REVILLE, Thomas, Francois; 34 Birch Hill Road, Belmont, MA 02478 (US). GAUTHIER, Lise; En- tasis Therapeutics Limited, 35 Gateshouse Drive, Waltham, MA 02451 (US). O'DONNELL, John; 7 Beacon Street, Mattapoisett, MA 02739 (US). ROMERO, Jan; 8 Lang- ley Road, Arlington, MA 02474 (US). TOMMASI, Ruben; 16 Salamander Lane, Stow, MA 01775 (US). VERHEI- JEN, Jeroen, Cunera; 5 Stratton Drive, Westborough, MA 01581 (US). WU, Frank; 5 Aspen Way, Shrewsbury, MA 01545 (US). WU, Xiaoyun; 3 Hundreds Road, Westbor- ough, MA 01581 (US). ZHANG, Jing; 11 Run Brook Cir- cle, Subdruy, MA 01776 (US). (74) Agent: DAVIS, Steven, G. et al.; Mccarter & English, LLP, 265 Franklin Street, Boston, MA 02110 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: with international search report (Art. 21(3)) before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h)) (54) Title: BETA-LACTAMASE INHIBITOR COMPOUNDS (57) : The present invention is directed to compounds which are be- ta-lactamase inhibitors. The compounds and their pharmaceutically acceptable salts are useful in combination with beta- lactam antibiotics, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes com- pounds according to Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of R 1 , R , R 2 3 , R 4 , R s and R 6 are described herein. R 2 R 3
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662395464P | 2016-09-16 | 2016-09-16 | |
| US201762456423P | 2017-02-08 | 2017-02-08 | |
| PCT/US2017/051692 WO2018053215A1 (en) | 2016-09-16 | 2017-09-15 | Beta-lactamase inhibitor compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201901658PA true SG11201901658PA (en) | 2019-04-29 |
Family
ID=60083416
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201901658PA SG11201901658PA (en) | 2016-09-16 | 2017-09-15 | Beta-lactamase inhibitor compounds |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US10800778B2 (en) |
| EP (1) | EP3512851B1 (en) |
| JP (2) | JP6997178B2 (en) |
| KR (2) | KR102537340B1 (en) |
| CN (2) | CN109715630B (en) |
| AU (1) | AU2017325863B2 (en) |
| CA (1) | CA3036557A1 (en) |
| DK (1) | DK3512851T3 (en) |
| ES (1) | ES2927986T3 (en) |
| HR (1) | HRP20221217T1 (en) |
| HU (1) | HUE060282T2 (en) |
| IL (2) | IL289686B2 (en) |
| LT (1) | LT3512851T (en) |
| MA (1) | MA46242A (en) |
| MX (2) | MX385507B (en) |
| PH (1) | PH12019500558B1 (en) |
| PL (1) | PL3512851T3 (en) |
| PT (1) | PT3512851T (en) |
| SG (1) | SG11201901658PA (en) |
| SI (1) | SI3512851T1 (en) |
| SM (1) | SMT202200397T1 (en) |
| TW (1) | TWI773687B (en) |
| WO (1) | WO2018053215A1 (en) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102403296B1 (en) | 2016-06-30 | 2022-05-27 | 큐펙스 바이오파마 인코포레이티드 | Boronic acid derivatives and therapeutic uses thereof |
| SMT202200397T1 (en) * | 2016-09-16 | 2022-11-18 | Entasis Therapeutics Ltd | Beta-lactamase inhibitor compounds |
| HUE057592T2 (en) | 2017-05-08 | 2022-05-28 | Entasis Therapeutics Inc | Compounds and methods for treating bacterial infections |
| CN112424209A (en) | 2018-04-20 | 2021-02-26 | Qpex生物制药有限公司 | Boronic acid derivatives and their therapeutic use |
| US11905286B2 (en) | 2018-08-09 | 2024-02-20 | Antabio Sas | Diazabicyclooctanones as inhibitors of serine beta-lactamases |
| DK3833665T3 (en) | 2018-08-09 | 2023-10-09 | Antabio Sas | Diazabicyclooctanones as inhibitors of serine beta-lactamases |
| CN112209928B (en) * | 2019-07-10 | 2023-02-17 | 华东理工大学 | Covalent bond labeled serine beta-lactamase reagent and preparation and application thereof |
| CN110898999A (en) * | 2019-11-26 | 2020-03-24 | 中国矿业大学 | A kind of coal tar-based slime flotation agent and preparation method thereof |
| CN111790439B (en) * | 2020-07-29 | 2022-12-27 | 成都能特科技发展有限公司 | Chiral secondary amine diphenylphosphine arylformamide bifunctional catalyst and preparation method and application thereof |
| CN115151544B (en) | 2020-09-01 | 2024-08-16 | 宁夏农林科学院 | β-lactamase inhibitor and its preparation |
| AU2022254114A1 (en) * | 2021-04-05 | 2023-09-21 | Qpex Biopharma, Inc. | Ceftibuten dosing regimens |
| WO2022233181A1 (en) | 2021-05-07 | 2022-11-10 | Ningxia Academy Of Agriculture And Forestry Sciences | Sulfonylamidine substituted compounds and their use as beta-lactamase inhibitors |
| US11814385B2 (en) | 2021-06-25 | 2023-11-14 | University Of South Florida | Small molecule inhibitors targeting Clostridioides difficile sporulation |
| WO2023206580A1 (en) | 2022-04-29 | 2023-11-02 | Entasis Therapeutics Limited | Durlobactam crystalline forms |
| US20230398101A1 (en) * | 2022-06-09 | 2023-12-14 | Fleurir Abx Llc | Co-agents as Therapy Against Anaerobic Pathogens |
| CN118271319B (en) * | 2022-12-30 | 2025-02-28 | 成都四面体药物研究有限公司 | A β-lactamase inhibitor containing urea bicyclic compound, preparation method and use thereof |
| CN118772145B (en) * | 2023-04-04 | 2025-10-10 | 上海医药工业研究院有限公司 | A preparation method of diazabicyclooctene compound |
| CN116693531A (en) * | 2023-06-09 | 2023-09-05 | 河南师范大学 | A kind of synthetic method of bridged polycyclic lactam compound |
| WO2025106662A1 (en) * | 2023-11-15 | 2025-05-22 | Entasis Therapeutics, Inc. | Preparation of boronic acid intermediates useful for the preparation of compounds for treating bacterial infections |
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| WO2014141132A1 (en) * | 2013-03-14 | 2014-09-18 | Naeja Pharmaceutical Inc. | NEW HETEROCYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND β-LACTAMASE INHIBITORS |
| EA033829B1 (en) * | 2014-11-17 | 2019-11-29 | Entasis Therapeutics Ltd | Combination therapy for treatment of resistant bacterial infections |
| EP3277686B1 (en) | 2015-03-31 | 2020-07-22 | Mutabilis | Novel heterocyclic compounds and their use in preventing or treating bacterial infections |
| SMT202200397T1 (en) * | 2016-09-16 | 2022-11-18 | Entasis Therapeutics Ltd | Beta-lactamase inhibitor compounds |
| KR20230007830A (en) * | 2021-07-06 | 2023-01-13 | 현대자동차주식회사 | Thermoplastic resin composition and molded article comprising the same |
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