ME01073B - Antibakterijski derivati kvinolina - Google Patents
Antibakterijski derivati kvinolinaInfo
- Publication number
- ME01073B ME01073B MEP-2010-111A MEP11110A ME01073B ME 01073 B ME01073 B ME 01073B ME P11110 A MEP11110 A ME P11110A ME 01073 B ME01073 B ME 01073B
- Authority
- ME
- Montenegro
- Prior art keywords
- alkyl
- aryl
- compound according
- het
- mono
- Prior art date
Links
- 125000002943 quinolinyl group Chemical class N1=C(C=CC2=CC=CC=C12)* 0.000 title claims 2
- 230000000844 anti-bacterial effect Effects 0.000 title 1
- 229940027991 antiseptic and disinfectant quinoline derivative Drugs 0.000 title 1
- -1 cyano, formyl Chemical group 0.000 claims 33
- 150000001875 compounds Chemical class 0.000 claims 29
- 125000000217 alkyl group Chemical group 0.000 claims 21
- 125000003118 aryl group Chemical group 0.000 claims 16
- 125000001424 substituent group Chemical group 0.000 claims 14
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 12
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 12
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 12
- 125000005843 halogen group Chemical group 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 10
- 125000003710 aryl alkyl group Chemical group 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000001188 haloalkyl group Chemical group 0.000 claims 7
- 125000004076 pyridyl group Chemical group 0.000 claims 7
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 7
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 6
- 125000004414 alkyl thio group Chemical group 0.000 claims 6
- 125000004663 dialkyl amino group Chemical group 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 5
- 125000006350 alkyl thio alkyl group Chemical group 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 125000002883 imidazolyl group Chemical group 0.000 claims 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 125000002098 pyridazinyl group Chemical group 0.000 claims 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims 4
- 208000035143 Bacterial infection Diseases 0.000 claims 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 3
- 125000004103 aminoalkyl group Chemical group 0.000 claims 3
- 208000022362 bacterial infectious disease Diseases 0.000 claims 3
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 claims 3
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 125000002632 imidazolidinyl group Chemical group 0.000 claims 3
- 125000002757 morpholinyl group Chemical group 0.000 claims 3
- 125000001624 naphthyl group Chemical group 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims 3
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 3
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims 3
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 claims 3
- 125000004306 triazinyl group Chemical group 0.000 claims 3
- 125000001425 triazolyl group Chemical group 0.000 claims 3
- 125000005943 1,2,3,6-tetrahydropyridyl group Chemical group 0.000 claims 2
- 241000894006 Bacteria Species 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 101001043818 Mus musculus Interleukin-31 receptor subunit alpha Proteins 0.000 claims 2
- 241000191967 Staphylococcus aureus Species 0.000 claims 2
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 2
- 239000003242 anti bacterial agent Substances 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000005984 hexahydro-1H-1,4-diazepinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 241000192125 Firmicutes Species 0.000 claims 1
- RJQXTJLFIWVMTO-TYNCELHUSA-N Methicillin Chemical compound COC1=CC=CC(OC)=C1C(=O)N[C@@H]1C(=O)N2[C@@H](C(O)=O)C(C)(C)S[C@@H]21 RJQXTJLFIWVMTO-TYNCELHUSA-N 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 241000193998 Streptococcus pneumoniae Species 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 125000005094 alkyl carbonyl amino alkyl group Chemical group 0.000 claims 1
- 125000005418 aryl aryl group Chemical group 0.000 claims 1
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 125000005605 benzo group Chemical group 0.000 claims 1
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 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
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000003187 heptyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims 1
- 229960003085 meticillin Drugs 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 229940031000 streptococcus pneumoniae Drugs 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
- C07D215/22—Oxygen atoms attached in position 2 or 4
- C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
- C07D215/22—Oxygen atoms attached in position 2 or 4
-
- 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
- A61K31/465—Nicotine; Derivatives thereof
-
- 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
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A61P31/06—Antibacterial agents for tuberculosis
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Quinoline Compounds (AREA)
Claims (24)
1. Jedinjenje formule (Ia) ili (lb)uključujući sve stereohemijske izomerske oblike, naznačeno time da je p ceo broj koji iznosi 1, 2, 3 ili 4; q ceo broj koji iznosi nula, 1, 2, 3 ili 4;R1 je vodonik, cijano, formil, karboksil, halo, alkil, C2-6alkenil, C2-6alkinil, haloalkil, hidroksi, alkiloksi, alkltio, alkiltioalkil, -C=N-OR11, amino, mono ili di(alkil)amino, aminoalkil, mono ili di(alkil)aminoalkil, alkilkarbonilaminoalkil, aminokarbonil, mono ili di(alkil)aminokarbonil, arilalkil, arilkarbonil, R5aR4aNalkil, di(aril)alkil, aril, R5aR4aN-, R5aR4aN-C(=0)-, ili Het;R2 je vodonik, alkiloksi, aril, ariloksi, hidroksi, merkapto, alkiloksialkiloksi, alkiltio, mono ili di(alkil)amino, pirolidin ili radikal formulegde je Y CH2, O, S, NH ili N-alkil;R3je alkil, arilalkil, aril-O-alkil, aril-alkil-O-alkil, aril, aril-aril, Het, Het-alkil, Het-O-alkil, Het-alkil-O-alkil iliR4 i R5su - svaki nezavisno - vodonik; alkil; alkiloksialkil; arilalkil; Het-alkil.; mono- ili dialkilaminoalkil; biciclo[2.2.1]heptil; Het; aril; ili -C(=Nm-NH2; iliR4 i R5 zajedno sa atomom azota za koji su vezani obrazuju radikal izabran između sledećih: pirolidin, piperidin, piperazin, morfolin, 4-tiomorfolin, 1,1-dioksid-tiomorfolinil, azetidinil, 2,3-dihidroizoindol-l-il, tiazolidin-3-il, 1,2,3,6- tetrahidropiridil, heksahidro- lH-azepinil, heksahidro-1H-1,4- diazepinil, heksahidro-1,4-oksazepinil, l,2,3,4-tetrahidroizokvinolin-2- il, 2,5-diazabiciklo[2.2.1]heptil, pirolinil, pirolil, imidazolidinil, pirazolidinil, 2-imidazolinil, 2-pirazolinil, imidazolil, pirazolil, triazolil, piridinil, piridazinil, pirimidinil, pirazinil i triazinil, gde je svaki radikal opciono supstituisan sa 1, 2, 3 ili 4 supstituenta, svaki supstituent je nezavisno izabran između: alkil, haloalkil, alkilkarbonil, halo, arilalkil, hidroksi, alkiloksi, amino, mono- ili dialkilamino, aminoalkil, mono- ili dialkilaminoalkil, alkiltio, alkiltioalkil, aril, piridil, pirimidinil, piperidinil opciono supstituisani sa alkilom ili pirolidinil opciono supstituisan arilalkilom;R4a i R5a zajedno sa atomom azota za koji su vezani obrazuju radikal između sledećih: pirolidin, piperidin, piperazin, morfolin, 4-tiomorfolin, 2,3-dihidroizoindol-l-il, tiazolidin-3-il, 1,2,3,6-tetrahidropiridil, heksahidro-1H-azepinil, heksahidro- 1H-1,4-di azepinil, heksahidro-1,4-oksazepinil, 1,2,3,4- tetrahidroizokvinolin-2-il, pirolinil, pirolil, imidazolidinil, pirazolidinil, 2-imidazolinil, 2-pirazolinil, imidazolil, pirazolil, triazolil, piridinil, piridazinil, pirimidinil, pirazinil i triazinil, a gde je svaki radikal opciono supstituisan sa 1, 2, 3 ili 4 supstituenta, svaki supstituent je nezavisno izabran između: alkil, haloalkil, halo, arilalkil, hidroksi, alkiloksi, amino, mono- ili dialkilamino, alkiltio, alkiltioalkil, aril, piridil ili pirimidinil;R6 je aril1 ili Het;R7 je vodonik, halo, alkil, aril ili Het;R8 je vodonik ili alkil;R9 je okso; iliR8 i R9 zajedno obrazuju radikal -CH=CH-N=;R10 je vodonik, C1-6alkil ili arilC1-6alkil;R11 je vodonik ili alkil;Z je S ili NR10;aril je homociklično jedinjenje izabrano između: fenil, naftil, acenaftil ili tetrahiđronaftil, gde je svaki opciono supstituisan sa 1, 2 ili 3 supstituenta, svaki supstituent je nezavisno izabran između: hidroksi, halo, cijano, nitro, amino, mono- ili dialkilamino, alkil, C2-6alkenil opciono supstituisan sa: fenil, haloalkil, alkiloksi, haloalkiloksi, karboksil, alkiloksikarbonil, aminokarbonil, morfolinil ili mono- ili dialkilaminokarbonil;aril1 je homociklično jedinjenje izabrano između: fenil, naftil, acenaftil ili tetrahidronaftil, gde je svaki opciono supstituisan sa 1, 2 ili 3 supstituenta, svaki supstituent je nezavisno izabran između: hidroksi, halo, cijano, nitro, amino, mono- ili dialkilamino, alkil, haloalkil, alkiloksi, alkiltio, haloalkiloksi, karboksil, alkiloksikarbonil, aminokarbonil, morfolinil, Het ili mono- ili dialkilaminokarbonil;Het je monociklično heterociklično jedinjenje izabrano između: N-fenoksipiperidinil, piperidinil, pirolil, pirazolil, imidazolil, furanil, tienil, oksazolil, izoksazolil, tiazolil, izotiazolil, piridinil, pirimidinil, pirazinil ili piridazinil; odnosno biciklično heterociklično jedinjenje izabrano između: kvinolinil, kvinoksalinil, indolil, benzimidazolil, benzoksazolil, benzizoksazolil, benzotiazolil, benziotiazolil, benzofuranil, benzotienil, 2,3-dihidrobenzo[l,4]dioksinil ili benzo[l,3]dioksolil; gde je svako monociklično i biciklično heterociklično jedinjenje opciono supstituisano sa 1, 2 ili 3 supstituenta, svaki supstituent je nezavisno selektovan između: halo, hidroksi, alkil ili alkiloksi; a njihovi N-oksidi, farmaceutski prihvatljive soli ili solvati.
2. Jedinjenje u prema zahtevu 1, naznačeno time da je R3 je alkil, arilalkil, aril-O-alkil, aril-alkil-O-alkil, aril, Het, alkil, Het-O-alkil, Het-alkil-O-alkil ili R4 i R5 svaki nezavisno je vodonik; alkil; alkiloksialkil; arilalkil; Het- alkil; mono- ili dialkilaminoalkil; Het; aril; ili -C(=NH)-NH2; ili R4 i R5 zajedno sa atomom azota za koji su vezani obrazuju radikal između sledećih: pirolidin, piperidin, piperazin, morfolin, 4-tiomorfolin, 2,3-dihidroizoindol-l-il, tiazolidin-3-il, 1,2,3,6-tetrahidropiridil, heksahidro-lH-azepinil, heksahidro-1H-1,4-diazepinil, heksahidro-1,4- oksazepinil, 1,2,3,4- tetrahidroizokvinolin-2-il, 2,5-diazabiciklo[2.2.1]heptil, pirolinil, pirolil, imidazolidinil, pirazolidinil, 2-imidazolinil, 2-pirazolinil, imidazolil, pirazolil, triazolil, piridinil, piridazinil, pirimidinil, pirazinil i triazinil, svaki radikal opciono supstituisan sa 1, 2, 3 ili 4 supstituenta, svaki supstituent nezavisno izabran između: alkil, haloalkil, alkilkarbonil, halo, arilalkil, hidroksi, alkiloksi, amino, mono- ili dialkilamino, alkiltio, alkiltioalkil, aril, piridil, pirimidinil, piperidinil ili pirolidinil opciono supstituisan sa arilalkil; aril je homociklično jedinjenje izabrano između: fenil, naftil, acenaftil ili tetrahidronaftil, gde je svaki opciono supstituisan sa 1, 2 ili 3 supstituenta, svaki supstituent je nezavisno izabran između: hidroksi, halo, cijano, nitro, amino, mono- ili dialkilamino, alkil, haloalkil, alkiloksi, haloalkiloksi, karboksil, alkiloksikarbonil, aminokarbonil, morfolinil ili mono- ili dialkilaminokarbonil.
3. Jedinjenje prema zahtevu 1 ili 2 naznačeno time da alkil predstavlja C1-6alkil.
4. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time da je R1 halo.
5. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time da je p jednako 1.
6. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time daje R C1-6alkiloksi.
7. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time da je R3 aril.
8. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time daje q jednako 1 ili 2.
9. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time da R4 i R5 predstavljaju C1-6alkil ili gde su R4 i R5 zajedno sa atomom azota za koji su vezani i obrazuju radikal izabran između piperidin ili piperazin, svaki od navedenih prstenova opciono supstituisan sa C1-6alkil.
10. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time da je R6 aril.
11. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time da je R7 vodonik.
12. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time da je jedinjenje jedinjenje formule (Ia).
13. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time daje Z jednako S.
14. Jedinjenje prema bilo kojem od prethodnih zahteva od 1 do 12 naznačeno time da je Z jednako NR10.
15. Jedinjenje prema zahtevu 1 naznačeno time daje R1 halo; R2 je C1-6alkiloksil; R3 je aril; R4 i R5 su C1-6alkil; ili R4 i R5 zajedno sa atomom azota za koji su vezani i obrazuju radikal izabran između piperidin ili piperazin, svaki od navedenih prstenova opciono supstituisan sa C1-6alkil; R6 je aril; R7 je vodonik; q je 1 ili 2; p je 1; R10 je C1-6alkil ili benzil.
16. Jedinjenje prema zahtevu 15 naznačeno time daje R1 brom; R2 je metiloksi; R3 je fenil; R4 i R5 su metil ili etil; ili R4 i R5 zajedno sa atomom azota za koji su vezani i obrazuju radikal izabran između piperidin ili piperazin, svaki od navedenih prstenova opciono supstituisan sa C1-6alkil; R6 je fenil.
17. Jedinjenje prema bilo kojem od prethodnih zahteva naznačeno time da je za primenu u medicini.
18. Jedinjenje prema bilo kojem od zahteva 1 do 16 naznačeno time da je za primenu u medicini za lečenje bakterijske infekcije.
19. Farmaceutski sastav koji uključuje farmaceutski prihvatljiv nosač i, kao aktivnu supstancu, terapijski delotvomu količinu jedinjenja na način defmisan u bilo kojem od zahteva 1 do 16.
20. Jedinjenje prema zahtevu 18 naznačeno time da je bakterijska infekcija infekcija gram-pozitivnim bakterijama.
21. Jedinjenje prema zahtevu 20 naznačeno time da je gram-pozitivna bakterija Streptococcus pneumoniae ili Staphylococcus aureus.
22. Kombinacija (a) jedinjenja prema bilo kojem od zahteva 1 do 16, i (b) jednog ili više drugih antibakterijskih agenasa.
23. Proizvod naznačen time da sadrži (a) jedinjenje prema bilo kojem od zahteva 1 do 16, i (b) jedan ili više drugih antibakterijskih agenasa, kombinovano pripremom za istovremeno, odvojeno ili sekvencijsko lečenje bakterijske infekcije.
24. Jedinjenje prema zahtevu 21 naznačeno time da je gram-pozitivna bakterija meticilin rezistentna Staphylococcus aureus.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06125521 | 2006-12-06 | ||
| PCT/EP2007/063315 WO2008068269A1 (en) | 2006-12-06 | 2007-12-04 | Antibacterial quinoline derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME01073B true ME01073B (me) | 2012-10-20 |
Family
ID=37944337
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2010-111A ME01073B (me) | 2006-12-06 | 2007-12-04 | Antibakterijski derivati kvinolina |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US7998979B2 (me) |
| EP (1) | EP2086941B1 (me) |
| JP (1) | JP5356245B2 (me) |
| KR (1) | KR101490221B1 (me) |
| CN (1) | CN101541752B (me) |
| AR (1) | AR064150A1 (me) |
| AT (1) | ATE465994T1 (me) |
| AU (1) | AU2007328889B2 (me) |
| BR (1) | BRPI0720251B8 (me) |
| CA (1) | CA2668520C (me) |
| CL (1) | CL2007003516A1 (me) |
| CY (1) | CY1110706T1 (me) |
| DE (1) | DE602007006231D1 (me) |
| DK (1) | DK2086941T3 (me) |
| ES (1) | ES2344535T3 (me) |
| HR (1) | HRP20100384T1 (me) |
| IL (1) | IL199081A (me) |
| JO (1) | JO2685B1 (me) |
| ME (1) | ME01073B (me) |
| MX (1) | MX2009005980A (me) |
| NO (1) | NO341995B1 (me) |
| NZ (1) | NZ576673A (me) |
| PL (1) | PL2086941T3 (me) |
| PT (1) | PT2086941E (me) |
| RS (1) | RS51390B (me) |
| RU (1) | RU2446159C2 (me) |
| SI (1) | SI2086941T1 (me) |
| TW (1) | TWI412364B (me) |
| WO (1) | WO2008068269A1 (me) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9133167B2 (en) | 2012-04-27 | 2015-09-15 | Janssen Pharmaceutica Nv | Antibacterial quinoline derivatives |
| KR102110366B1 (ko) | 2012-04-27 | 2020-05-14 | 얀센 파마슈티카 엔.브이. | 항균성 퀴놀린 유도체 |
| CN104650054B (zh) * | 2013-11-25 | 2019-09-13 | 重庆医药工业研究院有限责任公司 | 一种抗结核菌的喹啉噻吩芳氧乙胺衍生物 |
| US11857352B2 (en) | 2016-09-06 | 2024-01-02 | The Research Foundation For The State University Of New York | Positron imaging tomography imaging agent composition and method for bacterial infection |
| KR20240161147A (ko) | 2022-03-14 | 2024-11-12 | 슬랩 파마슈티컬스 엘엘씨 | 다중 사이클릭 화합물 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6033389B2 (ja) * | 1979-02-22 | 1985-08-02 | 日産化学工業株式会社 | 複素環エ−テル系フェノシキ脂肪酸誘導体、その製造法および該誘導体を含有する除草剤 |
| US5965572A (en) | 1996-10-28 | 1999-10-12 | The United States Of America As Respresented By The Secretary Of The Army | Methods for treating antibiotic-resistant infections |
| EA007205B1 (ru) * | 2001-07-31 | 2006-08-25 | Вейне Стейт Юниверсити | Производные хинолина и их использование в качестве противоопухолевых средств |
| PT1527050E (pt) * | 2002-07-25 | 2010-06-22 | Janssen Pharmaceutica Nv | Derivados de quinolina e sua utilização como inibidores de micobactérias |
| KR101150172B1 (ko) | 2004-01-23 | 2012-05-25 | 얀센 파마슈티카 엔.브이. | 치환된 퀴놀린 및 마이코박테리아 저해제로서의 용도 |
| ATE444068T1 (de) * | 2004-01-23 | 2009-10-15 | Janssen Pharmaceutica Nv | Chinolinderivate und ihre verwendung als mycobakterielle inhibitoren |
| MXPA06008596A (es) * | 2004-01-29 | 2006-08-28 | Janssen Pharmaceutica Nv | Derivados de quinolina para uso como inhibidores micobacterianos. |
| JO2524B1 (en) * | 2004-05-28 | 2010-03-17 | جانسن فارمسيتكا ان في | Use of substituted quinoline derivatives to treat drug-resistant microbial diseases |
| KR101539021B1 (ko) | 2004-09-28 | 2015-07-23 | 얀센 파마슈티카 엔.브이. | 박테리아 ａｔｐ 합성효소 결합 부분 |
-
2007
- 2007-11-29 JO JO2007507A patent/JO2685B1/en active
- 2007-12-04 ME MEP-2010-111A patent/ME01073B/me unknown
- 2007-12-04 SI SI200730286T patent/SI2086941T1/sl unknown
- 2007-12-04 JP JP2009539740A patent/JP5356245B2/ja not_active Expired - Fee Related
- 2007-12-04 NZ NZ576673A patent/NZ576673A/en not_active IP Right Cessation
- 2007-12-04 CA CA2668520A patent/CA2668520C/en active Active
- 2007-12-04 AU AU2007328889A patent/AU2007328889B2/en not_active Ceased
- 2007-12-04 ES ES07847813T patent/ES2344535T3/es active Active
- 2007-12-04 PT PT07847813T patent/PT2086941E/pt unknown
- 2007-12-04 BR BRPI0720251A patent/BRPI0720251B8/pt not_active IP Right Cessation
- 2007-12-04 DK DK07847813.8T patent/DK2086941T3/da active
- 2007-12-04 CN CN2007800437666A patent/CN101541752B/zh not_active Expired - Fee Related
- 2007-12-04 KR KR1020097012572A patent/KR101490221B1/ko not_active Expired - Fee Related
- 2007-12-04 HR HR20100384T patent/HRP20100384T1/hr unknown
- 2007-12-04 EP EP07847813A patent/EP2086941B1/en active Active
- 2007-12-04 PL PL07847813T patent/PL2086941T3/pl unknown
- 2007-12-04 AT AT07847813T patent/ATE465994T1/de active
- 2007-12-04 RS RSP-2010/0340A patent/RS51390B/sr unknown
- 2007-12-04 US US12/516,370 patent/US7998979B2/en active Active
- 2007-12-04 WO PCT/EP2007/063315 patent/WO2008068269A1/en not_active Ceased
- 2007-12-04 MX MX2009005980A patent/MX2009005980A/es active IP Right Grant
- 2007-12-04 RU RU2009125525/04A patent/RU2446159C2/ru active
- 2007-12-04 DE DE602007006231T patent/DE602007006231D1/de active Active
- 2007-12-05 CL CL200703516A patent/CL2007003516A1/es unknown
- 2007-12-05 TW TW096146213A patent/TWI412364B/zh not_active IP Right Cessation
- 2007-12-05 AR ARP070105443A patent/AR064150A1/es unknown
-
2009
- 2009-06-02 IL IL199081A patent/IL199081A/en active IP Right Grant
- 2009-07-06 NO NO20092540A patent/NO341995B1/no unknown
-
2010
- 2010-07-28 CY CY20101100708T patent/CY1110706T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20160585T1 (hr) | Antibakterijski derivati kinolina | |
| AR064153A1 (es) | Derivados de quinolina antibacterianos. procesos de obtencion y composiciones farmaceuticas. | |
| JP2010511667A5 (me) | ||
| ME01245B (me) | Antibakterijski hinolinski derivati | |
| HRP20131116T1 (hr) | Derivati kinolina kao antibakterijska sredstva | |
| HRP20100384T1 (hr) | Antibakterijski derivati kvinolina | |
| TNSN06033A1 (en) | Piperazine derivatives and their use as therapeutic agents | |
| HRP20110392T1 (hr) | Derivati kinolina za liječenje latentne tuberkuloze | |
| WO2006078621A3 (en) | 2-phenoxy-n- (1, 3 , 4-thiadizol-2-yl) pyridin-3-amine derivatives and related compounds as p2y1 receptor inhibitors for the treatment of thromboembolic disorders | |
| AR040673A1 (es) | Inhibidores micobacterianos, composicion farmaceutica y proceso de preparacion del compuesto | |
| HRP20080307T3 (hr) | Uporaba supstituiranih kinolinskih derivata za tretman bolesti uzrokovanih mikobakterijama otpornima na lijekove | |
| CA3081423A1 (en) | Antibacterial compounds | |
| JP2010511671A5 (me) | ||
| JP2009503024A5 (me) | ||
| HRP20160252T1 (hr) | C-4" položaj supstituiranog derivata makrolida | |
| HRP20140206T1 (hr) | Derivati kinolina kao antibakterijska sredstva | |
| AR045791A1 (es) | Derivados de triazol sustituidos como antagonistas de oxitocina | |
| JP2010511670A5 (me) | ||
| MY143605A (en) | Tri-, tetra-substituted-3-aminopyrrolidine derivative | |
| PE20061137A1 (es) | Compuestos derivados de macrolidos amino sustituidas | |
| MX2009003051A (es) | Derivados de quinolinona. | |
| HRP20110024T1 (hr) | Antibakterijski derivati kvinolina | |
| AR064147A1 (es) | Derivados de quinolina antibacterianos | |
| HRP20151308T1 (hr) | Antibakterijski derivati kinolina | |
| JP2009502869A5 (me) |