ME02532B - Jedinjenja beta-laktama supstituisana amidinom, njihovo dobijanje i upotreba kao antibakterijskih sredstava - Google Patents
Jedinjenja beta-laktama supstituisana amidinom, njihovo dobijanje i upotreba kao antibakterijskih sredstavaInfo
- Publication number
- ME02532B ME02532B MEP-2016-191A MEP2016191A ME02532B ME 02532 B ME02532 B ME 02532B ME P2016191 A MEP2016191 A ME P2016191A ME 02532 B ME02532 B ME 02532B
- Authority
- ME
- Montenegro
- Prior art keywords
- amino
- thiazol
- imino
- ethoxy
- kiselina
- Prior art date
Links
- -1 BETA-LACTAM COMPOUNDS Chemical class 0.000 title claims 44
- 239000003242 anti bacterial agent Substances 0.000 title 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 69
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 45
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 38
- 125000001424 substituent group Chemical group 0.000 claims 31
- 150000001875 compounds Chemical class 0.000 claims 24
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 21
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 239000001257 hydrogen Substances 0.000 claims 20
- 125000004567 azetidin-3-yl group Chemical group N1CC(C1)* 0.000 claims 18
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 16
- 239000012453 solvate Substances 0.000 claims 16
- 229910052736 halogen Chemical group 0.000 claims 15
- 150000002367 halogens Chemical group 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 15
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 14
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 13
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 12
- 125000000623 heterocyclic group Chemical group 0.000 claims 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 12
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 11
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 10
- 125000004432 carbon atom Chemical group C* 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims 7
- 229940079593 drug Drugs 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 7
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 6
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 6
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical group C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 6
- 239000002253 acid Substances 0.000 claims 6
- 208000035143 Bacterial infection Diseases 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 5
- 208000022362 bacterial infectious disease Diseases 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical group C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 3
- 125000006239 protecting group Chemical group 0.000 claims 3
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000004103 aminoalkyl group Chemical group 0.000 claims 2
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical group C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 238000011321 prophylaxis Methods 0.000 claims 2
- 238000011282 treatment Methods 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- YOTRRQGYOHCXKO-YKVGDQEKSA-N 2-[[amino-[4-[2-[(z)-[1-(2-amino-1,3-thiazol-4-yl)-2-[[(3s)-2,2-dimethyl-4-oxo-1-sulfooxyazetidin-3-yl]amino]-2-oxoethylidene]amino]oxyethoxy]phenyl]methylidene]amino]acetic acid Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCOC1=CC=C(C(N)=NCC(O)=O)C=C1 YOTRRQGYOHCXKO-YKVGDQEKSA-N 0.000 claims 1
- 241000894006 Bacteria Species 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
- 229940123930 Lactamase inhibitor Drugs 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- NYNWPBAFYJGUTB-CWEJAESISA-N NC=1SC=C(N1)/C(/C(=O)N[C@H]1C(N(C1=O)O)(C)C)=N/OCCOC1=CC=C(C=C1)C(NCCNC=N)=N Chemical compound NC=1SC=C(N1)/C(/C(=O)N[C@H]1C(N(C1=O)O)(C)C)=N/OCCOC1=CC=C(C=C1)C(NCCNC=N)=N NYNWPBAFYJGUTB-CWEJAESISA-N 0.000 claims 1
- OQTYUNDCTQEHCJ-DBPQUTDOSA-N O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\c1csc(N)n1)=N/OC(CC(O)=O)COc1ccc(C(N)=N)cc1 Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\c1csc(N)n1)=N/OC(CC(O)=O)COc1ccc(C(N)=N)cc1 OQTYUNDCTQEHCJ-DBPQUTDOSA-N 0.000 claims 1
- SYZVWJMXJFBLIC-QMRYPOTESA-N [(2r,3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-(4-carbamimidoylphenoxy)ethoxyimino]acetyl]amino]-2-methyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)[C@H](C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCOC1=CC=C(C(N)=N)C=C1 SYZVWJMXJFBLIC-QMRYPOTESA-N 0.000 claims 1
- SYZVWJMXJFBLIC-AAGJFWKWSA-N [(2s,3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-(4-carbamimidoylphenoxy)ethoxyimino]acetyl]amino]-2-methyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)[C@@H](C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCOC1=CC=C(C(N)=N)C=C1 SYZVWJMXJFBLIC-AAGJFWKWSA-N 0.000 claims 1
- LRVCSPNHHKZZMG-VLKICEKPSA-N [(3S)-3-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-(4-carbamimidoyl-3-hydroxyphenoxy)ethoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\c1csc(N)n1)=N/OCCOc1ccc(C(N)=N)c(O)c1 LRVCSPNHHKZZMG-VLKICEKPSA-N 0.000 claims 1
- FRXMKZSHABUSIH-YZVKNKPJSA-N [(3S)-3-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-(6-carbamimidoyl-5-hydroxypyridin-3-yl)oxyethoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\c1csc(N)n1)=N/OCCOc1cnc(C(N)=N)c(O)c1 FRXMKZSHABUSIH-YZVKNKPJSA-N 0.000 claims 1
- FFCNEMJFZGPFRF-IFUVNARDSA-N [(3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[(4-carbamimidoylphenyl)methoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCC1=CC=C(C(N)=N)C=C1 FFCNEMJFZGPFRF-IFUVNARDSA-N 0.000 claims 1
- ILSDAURZRGBRFR-UWLYNBDASA-N [(3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-(2-carbamimidoylpyridin-4-yl)oxyethoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCOC1=CC=NC(C(N)=N)=C1 ILSDAURZRGBRFR-UWLYNBDASA-N 0.000 claims 1
- LZNPBCGXCLQRKF-VLKICEKPSA-N [(3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-(4-carbamimidoylphenoxy)ethoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCOC1=CC=C(C(N)=N)C=C1 LZNPBCGXCLQRKF-VLKICEKPSA-N 0.000 claims 1
- PPRLWQYPXRWUQS-VLKICEKPSA-N [(3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-(4-carbamimidoylphenyl)sulfanylethoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCSC1=CC=C(C(N)=N)C=C1 PPRLWQYPXRWUQS-VLKICEKPSA-N 0.000 claims 1
- JRAWFUCLJDJOOJ-UWLYNBDASA-N [(3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-(4-carbamimidoylpyridin-2-yl)oxyethoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCOC1=CC(C(N)=N)=CC=N1 JRAWFUCLJDJOOJ-UWLYNBDASA-N 0.000 claims 1
- SDXKOGVXUZWXHC-UWLYNBDASA-N [(3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-(6-carbamimidoylpyridin-3-yl)oxyethoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCOC1=CC=C(C(N)=N)N=C1 SDXKOGVXUZWXHC-UWLYNBDASA-N 0.000 claims 1
- HHSIGOWCXLQBNP-LRAQNNFBSA-N [(3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-[(2-carbamimidoyl-5-methyl-1,3-thiazol-4-yl)oxy]ethoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound S1C(C(N)=N)=NC(OCCO\N=C(/C(=O)N[C@H]2C(N(OS(O)(=O)=O)C2=O)(C)C)C=2N=C(N)SC=2)=C1C HHSIGOWCXLQBNP-LRAQNNFBSA-N 0.000 claims 1
- JYXRWNBDPAGPRM-CWEJAESISA-N [(3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-[4-[n'-(1,3-diaminopropan-2-yl)carbamimidoyl]phenoxy]ethoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCOC1=CC=C(C(N)=NC(CN)CN)C=C1 JYXRWNBDPAGPRM-CWEJAESISA-N 0.000 claims 1
- ACENDXHPNOEURW-ROAJQUDYSA-N [(3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-[4-[n'-(pyridin-2-ylmethyl)carbamimidoyl]phenoxy]ethoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCOC1=CC=C(C(N)=NCC=2N=CC=CC=2)C=C1 ACENDXHPNOEURW-ROAJQUDYSA-N 0.000 claims 1
- IXUCHBUKQYYVCQ-JUMRHNHYSA-N [(3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-[4-[n'-[(3s)-pyrrolidin-3-yl]carbamimidoyl]phenoxy]ethoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCOC1=CC=C(C(N)=N[C@@H]2CNCC2)C=C1 IXUCHBUKQYYVCQ-JUMRHNHYSA-N 0.000 claims 1
- QQELDOOYSFPGBG-LMITWDTESA-N [(3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-[4-[n'-[2-(dimethylamino)ethyl]carbamimidoyl]phenoxy]ethoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound C1=CC(C(N)=NCCN(C)C)=CC=C1OCCO\N=C(C=1N=C(N)SC=1)/C(=O)N[C@H]1C(C)(C)N(OS(O)(=O)=O)C1=O QQELDOOYSFPGBG-LMITWDTESA-N 0.000 claims 1
- HPZWNWQNCPATTB-ZASWBZMTSA-N [(3s)-3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[3-(4-carbamimidoylphenoxy)propoxyimino]acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCCOC1=CC=C(C(N)=N)C=C1 HPZWNWQNCPATTB-ZASWBZMTSA-N 0.000 claims 1
- XCAVYCWFYSZJEL-DXKFBMHFSA-N [(3s)-3-[[(2z)-2-[1-amino-3-(4-carbamimidoylphenoxy)-1-oxopropan-2-yl]oxyimino-2-(2-amino-1,3-thiazol-4-yl)acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OC(C(N)=O)COC1=CC=C(C(N)=N)C=C1 XCAVYCWFYSZJEL-DXKFBMHFSA-N 0.000 claims 1
- DKOMWZLYEIWRDV-BGYQVPDLSA-N [(3s)-3-[[(2z)-2-[2-[4-(5-amino-1,4,5,6-tetrahydropyrimidin-2-yl)phenoxy]ethoxyimino]-2-(2-amino-1,3-thiazol-4-yl)acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCOC1=CC=C(C=2NCC(N)CN=2)C=C1 DKOMWZLYEIWRDV-BGYQVPDLSA-N 0.000 claims 1
- FQNDEKJXIFRHHH-BGYQVPDLSA-N [(3s)-3-[[(2z)-2-[2-[4-[n'-(3-aminopropyl)carbamimidoyl]phenoxy]ethoxyimino]-2-(2-amino-1,3-thiazol-4-yl)acetyl]amino]-2,2-dimethyl-4-oxoazetidin-1-yl] hydrogen sulfate Chemical compound O=C1N(OS(O)(=O)=O)C(C)(C)[C@@H]1NC(=O)C(\C=1N=C(N)SC=1)=N/OCCOC1=CC=C(C(N)=NCCCN)C=C1 FQNDEKJXIFRHHH-BGYQVPDLSA-N 0.000 claims 1
- TVKLJLGMUIRXLS-DICXZTSXSA-N [3-[[(2z)-2-(2-amino-1,3-thiazol-4-yl)-2-[2-(4-carbamimidoylphenoxy)ethoxyimino]acetyl]amino]-2-oxo-1-azaspiro[3.4]octan-1-yl] hydrogen sulfate Chemical compound C1=CC(C(=N)N)=CC=C1OCCO\N=C(C=1N=C(N)SC=1)/C(=O)NC1C2(CCCC2)N(OS(O)(=O)=O)C1=O TVKLJLGMUIRXLS-DICXZTSXSA-N 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 231100000252 nontoxic Toxicity 0.000 claims 1
- 230000003000 nontoxic effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 1
Classifications
-
- 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
- A61K31/41—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
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
- A61K31/433—Thidiazoles
-
- 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
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
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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
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| EP12152279 | 2012-01-24 | ||
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| EP13701246.4A EP2806873B1 (en) | 2012-01-24 | 2013-01-23 | Amidine substituted beta-lactam compounds, their preparation and use as antibacterial agents |
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| CN105175335B (zh) * | 2015-08-13 | 2017-11-03 | 南阳师范学院 | 一种3‑(3,3‑二氯烯丙氧基)‑1‑甲基吡唑‑5‑甲酰胺衍生物及其制备方法 |
| SMT202000480T1 (it) | 2015-09-23 | 2020-11-10 | Novartis Ag | Sali e forme solide di un antibiotico monobactamico |
| CN108368040B (zh) | 2015-12-15 | 2024-08-23 | 默沙东有限责任公司 | 二芳基单环β-内酰胺化合物及其用于治疗细菌感染的方法 |
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| 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 |
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| JP2019535724A (ja) | 2016-11-18 | 2019-12-12 | アイキュリス アンチ−インフェクティブ キュアズ ゲゼルシャフト ミット ベシュレンクテル ハフツング | 細菌感染症の治療に使用するためのアミジン置換β−ラクタム化合物のリポソーム製剤 |
| US20190365720A1 (en) | 2016-11-18 | 2019-12-05 | Aicuris Anti-Infective Cures Gmbh | Novel formulations of amidine substituted beta-lactam compounds on the basis of modified cyclodextrins and acidifying agents, their preparation and use as antimicrobial pharmaceutical compositions |
| CN110312715A (zh) | 2016-12-21 | 2019-10-08 | 艾库里斯有限及两合公司 | 用于抗生素耐药性细菌菌株感染的使用脒取代的β-内酰胺化合物和β-内酰胺酶抑制剂的组合疗法 |
| AU2018304841A1 (en) | 2017-07-18 | 2020-02-06 | Bayer Aktiengesellschaft | Substituted 3-heteroaryloxy-1H-pyrazoles and salts thereof and their use as herbicidal active substances |
| TW201920163A (zh) | 2017-07-28 | 2019-06-01 | 德商艾庫里斯抗感染治療有限公司 | (2s)‐2‐[[(z)‐[1‐(2‐胺基‐4‐噻唑基)‐2‐[[(3s)‐2,2‐二甲基‐4‐側氧基‐1‐(磺氧)‐3‐吖丁啶基]胺基]‐2‐氧亞乙基]胺基]氧基]‐3‐[4‐[亞胺基[(3r)‐3-哌啶基胺基]甲基]苯氧基]-丙酸之晶型 |
| EP3661933B1 (en) | 2017-08-02 | 2022-03-23 | Novartis AG | Process for preparing 1-(((z)-(1-(2-aminothiazol-4-yl)-2-oxo-2-(((3s,4r)-2-oxo-4-((2-oxooxazolidin-3-yl)methyl)-1-sulfoazetidin-3- yl)amino)ethylidene)amino)oxy)cyclopropane carboxylic acid |
| PE20201256A1 (es) * | 2017-10-02 | 2020-11-16 | Merck Sharp & Dohme | Compuestos monobactamicos cromanos para el tratamiento de infecciones bacterianas |
| EP3676247B8 (en) * | 2017-10-02 | 2023-04-12 | Arixa Pharmaceuticals, Inc. | Aztreonam derivatives and uses thereof |
| 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 |
| CA3119394A1 (en) * | 2018-11-13 | 2020-05-22 | Nanjing Sanhome Pharmaceutical Co., Ltd. | Monobactam compounds and use therefor |
| US12310948B2 (en) | 2018-12-18 | 2025-05-27 | Shenzhen Optimum Biological Technology Co., Ltd | Application of monocyclic β-lactam compound in pharmacy |
| 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 |
| CN114828850B (zh) | 2019-12-19 | 2024-08-13 | 深圳嘉科生物科技有限公司 | 化合物在制药中的应用 |
| CN111253405B (zh) * | 2020-03-20 | 2022-12-16 | 南京安伦化工科技有限公司 | 一种比阿培南中间体的制备方法 |
| CN113754651B (zh) * | 2020-06-02 | 2023-04-18 | 中国医学科学院医药生物技术研究所 | 一种β-内酰胺化合物、其用途及其制备方法 |
| CN111675641B (zh) * | 2020-06-04 | 2023-09-08 | 宁夏农林科学院农业资源与环境研究所（宁夏土壤与植物营养重点实验室） | 单环β-内酰胺类化合物、单环内酰胺类化合物盐及其制备方法 |
| CN111592536B (zh) * | 2020-06-04 | 2023-11-03 | 宁夏农林科学院农业资源与环境研究所（宁夏土壤与植物营养重点实验室） | 单环β-内酰胺化合物及其制备方法和应用 |
| CN115210231B (zh) * | 2020-07-16 | 2024-10-08 | 宁夏农林科学院 | 单环内酰胺类化合物、其制备方法及其作为抗菌药的用途 |
| EP4007759A4 (en) * | 2020-08-06 | 2024-04-10 | Ningxia Academy of Agriculture and Forestry Sciences | BETA-LACTAM COMPOUNDS, THEIR PREPARATION AND THEIR USE AS ANTIBACTERIAL AGENTS |
| CN112079791A (zh) * | 2020-08-21 | 2020-12-15 | 宁夏农林科学院农业资源与环境研究所（宁夏土壤与植物营养重点实验室） | 单环β-内酰胺类抗生素侧链酸及其酯、其制备方法和应用 |
| CN111909067B (zh) * | 2020-08-28 | 2022-03-15 | 浙江凯普化工有限公司 | 一种d-青霉胺的有机全合成方法 |
| AU2021473165B2 (en) * | 2021-11-09 | 2025-05-22 | Guangzhou HC New Drug Research Co., Ltd. | PHARMACEUTICAL COMPOSITION CONTAINING β-LACTAM COMPOUND AND USE THEREOF |
| 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 |
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| CN118255695B (zh) * | 2024-02-26 | 2025-03-14 | 广州艾奇西医药科技有限公司 | 一种β-内酰胺类化合物的中间体的纯化方法和制备方法 |
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