HRP20090491T1 - Inhibitori giraze i njihova upotreba - Google Patents
Inhibitori giraze i njihova upotreba Download PDFInfo
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- HRP20090491T1 HRP20090491T1 HR20090491T HRP20090491T HRP20090491T1 HR P20090491 T1 HRP20090491 T1 HR P20090491T1 HR 20090491 T HR20090491 T HR 20090491T HR P20090491 T HRP20090491 T HR P20090491T HR P20090491 T1 HRP20090491 T1 HR P20090491T1
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- 239000002271 gyrase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 27
- 239000000203 mixture Substances 0.000 claims abstract 13
- 208000035143 Bacterial infection Diseases 0.000 claims abstract 6
- 208000022362 bacterial infectious disease Diseases 0.000 claims abstract 6
- 230000001580 bacterial effect Effects 0.000 claims abstract 3
- 238000000034 method Methods 0.000 claims abstract 2
- 125000001931 aliphatic group Chemical group 0.000 claims 15
- 230000000694 effects Effects 0.000 claims 8
- 230000002401 inhibitory effect Effects 0.000 claims 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000003242 anti bacterial agent Substances 0.000 claims 3
- 229940088710 antibiotic agent Drugs 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 241000193738 Bacillus anthracis Species 0.000 claims 2
- 241001647372 Chlamydia pneumoniae Species 0.000 claims 2
- 102000004127 Cytokines Human genes 0.000 claims 2
- 108090000695 Cytokines Proteins 0.000 claims 2
- 241000588914 Enterobacter Species 0.000 claims 2
- 241000194032 Enterococcus faecalis Species 0.000 claims 2
- 241000194031 Enterococcus faecium Species 0.000 claims 2
- 241000588724 Escherichia coli Species 0.000 claims 2
- 208000002633 Febrile Neutropenia Diseases 0.000 claims 2
- 241000606768 Haemophilus influenzae Species 0.000 claims 2
- 208000036209 Intraabdominal Infections Diseases 0.000 claims 2
- 241000588747 Klebsiella pneumoniae Species 0.000 claims 2
- 241000589242 Legionella pneumophila Species 0.000 claims 2
- 241000588655 Moraxella catarrhalis Species 0.000 claims 2
- 241000187479 Mycobacterium tuberculosis Species 0.000 claims 2
- 241000202934 Mycoplasma pneumoniae Species 0.000 claims 2
- 206010035664 Pneumonia Diseases 0.000 claims 2
- 241000588769 Proteus <enterobacteria> Species 0.000 claims 2
- 241000589517 Pseudomonas aeruginosa Species 0.000 claims 2
- 206010057190 Respiratory tract infections Diseases 0.000 claims 2
- 206010040047 Sepsis Diseases 0.000 claims 2
- 241000607720 Serratia Species 0.000 claims 2
- 206010062255 Soft tissue infection Diseases 0.000 claims 2
- 241000191967 Staphylococcus aureus Species 0.000 claims 2
- 241000191963 Staphylococcus epidermidis Species 0.000 claims 2
- 241001147691 Staphylococcus saprophyticus Species 0.000 claims 2
- 241000193998 Streptococcus pneumoniae Species 0.000 claims 2
- 241000193996 Streptococcus pyogenes Species 0.000 claims 2
- 229940065181 bacillus anthracis Drugs 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 208000037815 bloodstream infection Diseases 0.000 claims 2
- 229940032049 enterococcus faecalis Drugs 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 229940047650 haemophilus influenzae Drugs 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 208000015181 infectious disease Diseases 0.000 claims 2
- 229940115932 legionella pneumophila Drugs 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229940013390 mycoplasma pneumoniae Drugs 0.000 claims 2
- 201000007094 prostatitis Diseases 0.000 claims 2
- 230000035945 sensitivity Effects 0.000 claims 2
- 206010040872 skin infection Diseases 0.000 claims 2
- 229940031000 streptococcus pneumoniae Drugs 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 208000019206 urinary tract infection Diseases 0.000 claims 2
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 241000894006 Bacteria Species 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 239000000867 Lipoxygenase Inhibitor Substances 0.000 claims 1
- 101710183280 Topoisomerase Proteins 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- -1 gem-dimethyl Chemical group 0.000 claims 1
- 239000003102 growth factor Substances 0.000 claims 1
- 150000002431 hydrogen Chemical group 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 229940121354 immunomodulator Drugs 0.000 claims 1
- 229960003444 immunosuppressant agent Drugs 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 239000011159 matrix material Substances 0.000 claims 1
- 239000003475 metalloproteinase inhibitor Substances 0.000 claims 1
- 229940094443 oxytocics prostaglandins Drugs 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 150000003180 prostaglandins Chemical class 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 241000124008 Mammalia Species 0.000 abstract 1
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/00—Medicinal preparations containing organic active ingredients
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- 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
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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- 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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- 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
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- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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Abstract
Spoj formule VII:ili njegova farmaceutski prihvatljiva sol, gdje: V je odabran od dušika, CH, ili CF; R3 je vodik ili alifatski C1-4, gdje: kada je R3 alifatski C1-4, R3 je supstituiran s 0-3 skupine neovisno odabrane od OH, R5, ili OR5;gdje: R5 je alifatski C1-3, gdje: dvije R5 alifatske skupine mogu biti opcionalno uzete zajedno s ugljikom na koji su vezane kako bi činile C3-4 cikloalkilni prsten; s tim da ukoliko je R3 vodik, tada V nije dušik ili CH; R4 je C1-3 alifatska skupina; iprsten C je 6-člani heteroarilni prsten koji ima 1-2 dušika, gdje: je prsten C supstituiran s 1-3 skupine odabrane od R6;gdje: svaki R6 je neovisno odabran od OR7 ili halogena; iR7 je alifatski C1-4; ili prsten C je nesupstituirani 2-pirimidinski prsten. Patent sadrži još 20 patentnih zahtjeva.
Claims (21)
1. Spoj formule VII:
[image]
ili njegova farmaceutski prihvatljiva sol, gdje:
V je odabran od dušika, CH, ili CF;
R3 je vodik ili alifatski C1-4, gdje:
kada je R3 alifatski C1-4, R3 je supstituiran s 0-3 skupine neovisno odabrane od OH, R5, ili OR5;
gdje:
R5 je alifatski C1-3, gdje:
dvije R5 alifatske skupine mogu biti opcionalno uzete zajedno s ugljikom na koji su vezane kako bi činile C3-4 cikloalkilni prsten;
s tim da ukoliko je R3 vodik, tada V nije dušik ili CH;
R4 je C1-3 alifatska skupina; i
prsten C je 6-člani heteroarilni prsten koji ima 1-2 dušika, gdje:
je prsten C supstituiran s 1-3 skupine odabrane od R6;
gdje:
svaki R6 je neovisno odabran od OR7 ili halogena; i
R7 je alifatski C1-4; ili
prsten C je nesupstituirani 2-pirimidinski prsten.
2. Spoj prema zahtjevu 1, naznačen time da je prsten C je 2-piridilni prsten supstituiran s jednim od oblika u kojim se može pojaviti R6.
3. Spoj prema zahtjevu 2, naznačen time da je prsten C:
[image]
4. Spoj prema zahtjevu 3, naznačen time da je R6 odabran od halogena, na primjer gdje R6je fluoro; ili OR7, na primjer gdje R7 je metil.
5. Spoj prema bilo kojem zahtjevu od 1 do 4, naznačen time da
[image]
radikal je:
[image]
6. Spoj prema bilo kojem zahtjevu od 1 do 5, naznačen time da R3 je opcionalno supstituirana C1-3 alkilna skupina;
na primjer gdje R3 je C1-3 alkilna skupina opcionalno supstituirana s OH skupinom;
primjerice gdje R3 je C1-3 alkilna skupina supstituirana s OH skupinom;
na primjer gdje R3 je C1-3 alkilna skupina supstituirana s metil, gem-dimetil, etil, propil, izopropil, ciklopropil, ili ciklobutil, i OH skupinom.
7. Spoj prema bilo kojem zahtjevu od 1 do 6, naznačen time da:
(a) V je dušik i R3 je supstituiran s dvije skupine neovisno odabrane od R5 i OH; ili
(b) V je CH i R3 je supstituiran s dvije skupine neovisno odabrane od R5 i OH;
na primjer gdje R3 je supstituiran s jednom R5 skupinom i jednom OH skupinom.
8. Spoj prema bilo kojem zahtjevu od 1 do 7, naznačen time da je navedeni spoj formule VIIA, VIIB ili VIIC:
[image]
ili njihova farmaceutski prihvatljiva sol, gdje:
R4 je C1-3 alifatska skupina; i
prsten C je 6-člani heteroarilni prsten koji ima 1-2 dušika, gdje:
prsten C je supstituiran s 1-3 skupine odabrane od R6;
gdje:
svaki R6 je neovisno odabran od OR7 ili halogena;
R7 je alifatski C1-4; ili
prsten C je nesupstituirani 2-pirimidinski prsten; ili
gdje navedeni spoj je formule VIID, VIIE, VIIF ili VIIG:
[image]
ili njihova farmaceutski prihvatljiva sol, gdje:
R3 je alifatski C1-4, gdje:
R3 je supstituiran s 0-3 skupine neovisno odabrane od OH, R5, ili OR5;
gdje:
R5 je alifatski C1-3; i
R4 je C1-3 alifatska skupina; ili
gdje navedeni spoj je formule VIIH, ili VIIJ:
[image]
ili njihova farmaceutski prihvatljiva sol, gdje:
R3 je vodik ili alifatski C1-4, gdje:
kada je R3 alifatski C1-4, R3 je supstituiran s 0-3 skupine neovisno odabrane od OH, R5, ili OR5;
gdje:
R5 je alifatski C1-3; i
R4 je C1-3 alifatska skupina.
9. Spoj prema bilo kojem zahtjevu od 1 do 8, naznačen time da R4 je etil.
10. Spoj odabran od skupine koja se sastoji od:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
11. Sastav koji sadrži spoj prema bilo kojem zahtjevu od 1 do 10, i farmaceutski prihvatljiv nosač, adjuvans, ili sredstvo.
12. Sastav prema zahtjevu 11, naznačen time da nadalje sadrži dodatno terapeutsko sredstvo odabrano od antibiotika, protuupalnog sredstva, inhibitora matriksa metaloproteaze, inhibitora lipoksigenaze, antagonista citokina, imunosupresanta, protutumorskog sredstva, sredstva protiv virusa, citokina, faktora rasta, imunomodulatora, prostaglandina, spoja protiv vaskularne hiperproliferacije, ili sredstva koje povećava osjetljivost bakterijskih organizama na antibiotike.
13. Metoda inhibicije aktivnosti giraze, inhibicije aktivnosti Topo (topoizomeraze) IV ili inhibicije i aktivnosti giraze i aktivnosti Topo IV u biološkom uzorku, naznačena time da sadržava korak dolaženja u doticaj biološkog uzorka sa:
a) sastavom prema zahtjevu 11; ili
b) spojem prema bilo kojem zahtjevu od 1 do 10.
14. Sastav prema zahtjevu 11; ili spoj prema bilo kojem zahtjevu od 1 do 10, naznačeni time da su za upotrebu u inhibiranju aktivnosti giraze, inhibiranju aktivnosti Topo IV ili inhibiranju i aktivnosti giraze i aktivnosti Topo IV kod pacijenta.
15. Sastav prema zahtjevu 11; ili spoj prema bilo kojem zahtjevu od 1 do 10, naznačeni time da su za upotrebu u smanjenju količine bakterija u pacijenta.
16. Sastav prema zahtjevu 11; ili spoj prema bilo kojem zahtjevu od 1 do 10, naznačeni time da su za upotrebu u liječenju, prevenciji, ili ublažavanju ozbiljnosti bakterijske infekcije kod pacijenta.
17. Spoj prema bilo kojem od zahtjeva 1 do 10, ili sastav prema zahtjevu 11, za upotrebu prema zahtjevu 16, naznačeni time da je bakterijska infekcija koju treba liječiti karakterizirana prisutnošću jedne ili više os sljedećih:
Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecalis, Enterococcus faecium, Klebsiella pneumoniae, Enterobacter sps., Proteus sps., Pseudomonas aeruginosa, E. coli, Serratia marcesens, Staphylococcus aureus, Staphylococcus saprophyticus, Coag. Neg. Staph, Haemophilus influenzae, Bacillus anthracis, Mycoplasma pneumoniae, Moraxella catarralis, Chlamydia pneumoniae, Legionella pneumophila, Staphylococcus epidermidis, Mycobacterium tuberculosis, ili Heliobacter pylori.
18. Spoj prema bilo kojem zahtjevu od 1 do 10, ili sastav prema zahtjevu 11, za upotrebu prema zahtjevu 17, naznačeni time da je bakterijska infekcija koju treba liječiti odabrana od jedne ili više od sljedećih: infekcija urinarnog trakta, respiratorna infekcija, upala pluća, prostatitis, infekcija kože ili mekog tkiva, intraabdominalna infekcija, infekcija krvotoka, ili infekcija pacijenata oboljelih od febrilne neutropenije.
19. Spoj prema bilo kojem zahtjevu od 1 do 10, ili sastav prema zahtjevu 11, za upotrebu prema zahtjevu 18, naznačeni time da su za upotrebu uzastopno ili istovremeno sa, i zajedno sa ili odvojeno od, dodatnog terapeutskog sredstva.
20. Spoj prema bilo kojem zahtjevu od 1 do 10, ili sastav prema zahtjevu 11, za upotrebu prema zahtjevu 17, naznačeni time da su za uzastopnu upotrebu, ili istovremenu sa sredstvom koji povećava osjetljivost bakterijskih organizama na antibiotike.
21. Upotreba spoja prema bilo kojem zahtjevu od 1 do 10, ili sastava prema zahtjevu 11, naznačeni time da su za proizvodnju lijeka za liječenje bakterijske infekcije karakterizirane prisutnošću jedne ili više od sljedećih: Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus faecalis, Enterococcus faecium, Klebsiella pneumoniae, Enterobacter sps., Proteus sps., Pseudomonas aeruginosa, E. coli, Serratia marcesens, Staphylococcus aureus, Staphylococcus saprophyticus,
Coag. Neg. Staph, Haemophilus influenzae, Bacillus anthracis, Mycoplasma pneumoniae, Moraxella catarralis, Chlamydia pneumoniae, Legionella pneumophila, Staphylococcus epidermidis, Mycobacterium tuberculosis, ili Heliobacter pylori; ili odabrane od jedne ili više od sljedećih: infekcija urinarnog trakta, respiratorna infekcija, upala pluća, prostatitis, infekcija kože ili mekog tkiva, intraabdominalna infekcija, infekcija krvotoka, ili infekcija pacijenata oboljelih od febrinle neutropenije.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/901,928 US7569591B2 (en) | 2003-01-31 | 2004-07-29 | Gyrase inhibitors and uses thereof |
| PCT/US2004/034919 WO2006022773A1 (en) | 2004-07-29 | 2004-10-21 | Gyrase inhibitors and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20090491T1 true HRP20090491T1 (hr) | 2009-11-30 |
Family
ID=34959926
Family Applications (1)
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|---|---|---|---|
| HR20090491T HRP20090491T1 (hr) | 2004-07-29 | 2009-09-15 | Inhibitori giraze i njihova upotreba |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US7569591B2 (hr) |
| EP (1) | EP1789419B1 (hr) |
| KR (1) | KR20070048762A (hr) |
| AT (1) | ATE433980T1 (hr) |
| AU (1) | AU2004322641B2 (hr) |
| CA (1) | CA2577758C (hr) |
| CY (1) | CY1110230T1 (hr) |
| DE (1) | DE602004021644D1 (hr) |
| DK (1) | DK1789419T3 (hr) |
| ES (1) | ES2325026T3 (hr) |
| HR (1) | HRP20090491T1 (hr) |
| PL (1) | PL1789419T3 (hr) |
| PT (1) | PT1789419E (hr) |
| SI (1) | SI1789419T1 (hr) |
| WO (1) | WO2006022773A1 (hr) |
| ZA (1) | ZA200701629B (hr) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
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| ATE345132T1 (de) * | 2002-06-13 | 2006-12-15 | Vertex Pharma | 2-ureido-6-heteroaryl-3h-benzoimidazol-4- carbonsäurederivate und verwandte verbindungen als gyrase und/oder topoisomerase iv inhibitoren zur behandlung von bakteriellen infektionen |
| US8193352B2 (en) * | 2003-01-31 | 2012-06-05 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| US7618974B2 (en) * | 2003-01-31 | 2009-11-17 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| US8404852B2 (en) | 2003-01-31 | 2013-03-26 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| US7569591B2 (en) * | 2003-01-31 | 2009-08-04 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| US7582641B2 (en) * | 2003-01-31 | 2009-09-01 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| AR042956A1 (es) * | 2003-01-31 | 2005-07-13 | Vertex Pharma | Inhibidores de girasa y usos de los mismos |
| DK1928454T3 (da) | 2005-05-10 | 2014-11-03 | Intermune Inc | Pyridonderivater til modulering af stress-aktiveret proteinkinasesystem |
| DE102005028862A1 (de) * | 2005-06-22 | 2007-01-11 | Sanofi-Aventis Deutschland Gmbh | Substituierte Heterocyclen, ihre Verwendung als Medikament sowie sie enthaltende pharmazeutische Zubereitungen |
| WO2007003961A2 (en) * | 2005-06-30 | 2007-01-11 | Prosidion Limited | Gpcr agonists |
| US8394803B2 (en) * | 2005-11-07 | 2013-03-12 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| WO2009027733A1 (en) * | 2007-08-24 | 2009-03-05 | Astrazeneca Ab | (2-pyridin-3-ylimidazo[1,2-b]pyridazin-6-yl) urea derivatives as antibacterial agents |
| CA2708241A1 (en) | 2007-12-07 | 2009-06-18 | Vertex Pharmaceuticals Incorporated | Solid forms of 1-ethyl-3-(5-(5-fluoropyridin-3-yl)-7-(pyrimidin-2-yl)-1h-benzo[d]imidazol-2-yl)urea |
| TW200940537A (en) * | 2008-02-26 | 2009-10-01 | Astrazeneca Ab | Heterocyclic urea derivatives and methods of use thereof |
| JP5627574B2 (ja) | 2008-06-03 | 2014-11-19 | インターミューン， インコーポレイテッド | 炎症性および線維性疾患を治療するための化合物および方法 |
| PE20120403A1 (es) * | 2009-05-15 | 2012-05-03 | Novartis Ag | Aril-piridinas como inhibidoras de sintasa de aldosterona |
| AU2011313820A1 (en) * | 2010-10-08 | 2013-04-11 | Biota Europe Ltd | Antibacterial compounds |
| JP6006235B2 (ja) | 2011-01-14 | 2016-10-12 | 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | ジャイレースおよびトポイソメラーゼｉｖ阻害剤を作製するプロセス |
| TWI535714B (zh) * | 2011-01-14 | 2016-06-01 | 維泰克斯製藥公司 | 旋轉酶抑制劑（ｒ）－１－乙基－３－［６－氟－５－［２－（１－羥基－１－甲基－乙基）嘧啶－５－基］－７－（四氫呋喃－２－基）－１ｈ－苯并咪唑－２－基］脲之固體形式 |
| CN103443096B (zh) * | 2011-01-14 | 2016-06-29 | 沃泰克斯药物股份有限公司 | 促旋酶和拓扑异构酶iv抑制剂 |
| SG191924A1 (en) | 2011-01-14 | 2013-08-30 | Vertex Pharma | Solid forms of gyrase inhibitor (r)-1-ethyl-3-[5-[2-{1-hydroxy-1-methyl-ethyl}pyrimidin-5-yl]-7-(tetrahydrofuran-2-yl}-1h-benzimidazol-2-yl]urea |
| EP2721026B1 (en) | 2011-06-20 | 2016-03-02 | Vertex Pharmaceuticals Incorporated | Phosphate esters of gyrase and topoisomerase inhibitors |
| TWI595002B (zh) * | 2012-07-18 | 2017-08-11 | 思沛羅三南公司 | （Ｒ）－２－（５－（２－（３－乙基脲基）－６－氟－７－（四氫呋喃－２－基）－１Ｈ－苯并［ｄ］咪唑－５－基）嘧啶－２－基）丙烷－２－基磷酸二氫鹽之固體形式及其鹽 |
| US9572809B2 (en) | 2012-07-18 | 2017-02-21 | Spero Trinem, Inc. | Combination therapy to treat Mycobacterium diseases |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| CA2938459A1 (en) | 2014-02-03 | 2015-08-06 | Spero Gyrase, Inc. | Antibacterial compounds |
| RU2692485C2 (ru) | 2014-04-02 | 2019-06-25 | Интермьюн, Инк. | Противофиброзные пиридиноны |
| MY195016A (en) | 2014-08-04 | 2023-01-03 | Nuevolution As | Optionally Fused Heterocyclyl-Substituted Derivatives of Pyrimidine Useful for The Treatment of Inflammatory, Metabolic, Oncologic and Autoimmune Diseases |
| CN105884752B (zh) * | 2015-02-13 | 2018-08-31 | 山东轩竹医药科技有限公司 | 并环类回旋酶和拓扑异构酶iv抑制剂 |
| JPWO2018174288A1 (ja) | 2017-03-24 | 2020-01-23 | 大正製薬株式会社 | ２（１ｈ）−キノリノン誘導体 |
| JP2021098692A (ja) | 2019-12-20 | 2021-07-01 | ヌエヴォリューション・アクティーゼルスカブＮｕｅｖｏｌｕｔｉｏｎ Ａ／Ｓ | 核内受容体に対して活性の化合物 |
| AU2021245397A1 (en) | 2020-03-31 | 2022-10-20 | Nuevolution A/S | Compounds active towards nuclear receptors |
| AU2021249530A1 (en) | 2020-03-31 | 2022-12-01 | Nuevolution A/S | Compounds active towards nuclear receptors |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2015676A1 (de) | 1970-04-02 | 1971-10-21 | Farbenfabriken Bayer Ag, 5090 Leverkusen | Neue Imine der 2-Formyl-chinoxalindi-N-oxidcarbon-säure-(3) und deren Salze, Verfahren zu ihrer Herstellung und ihre Verwendung als antimikrobielle Mittel |
| US4174400A (en) | 1978-09-13 | 1979-11-13 | Merck & Co., Inc. | Anthelmintic benzimidazoles |
| US4512998A (en) | 1980-10-20 | 1985-04-23 | Schering Corporation | Anthelmintic benzimidazole carbamates |
| DE19514313A1 (de) | 1994-08-03 | 1996-02-08 | Bayer Ag | Benzoxazolyl- und Benzothiazolyloxazolidinone |
| HRP960159A2 (en) | 1995-04-21 | 1997-08-31 | Bayer Ag | Benzocyclopentane oxazolidinones containing heteroatoms |
| US5643935A (en) | 1995-06-07 | 1997-07-01 | The University Of North Carolina At Chapel Hill | Method of combatting infectious diseases using dicationic bis-benzimidazoles |
| TW538046B (en) | 1998-01-08 | 2003-06-21 | Hoechst Marion Roussel Inc | Aromatic amides having antiobiotic activities and the preparation processes, intermediates and pharmaceutical composition thereof |
| AUPP873799A0 (en) | 1999-02-17 | 1999-03-11 | Fujisawa Pharmaceutical Co., Ltd. | Pyridine compounds |
| GB9911594D0 (en) | 1999-05-19 | 1999-07-21 | Smithkline Beecham Plc | Novel compounds |
| GB9912413D0 (en) | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| ES2331250T3 (es) | 2000-12-15 | 2009-12-28 | Vertex Pharmaceuticals Incorporated | Inhibidores de la girasa bacteriana y usos de los mismos. |
| ATE345132T1 (de) | 2002-06-13 | 2006-12-15 | Vertex Pharma | 2-ureido-6-heteroaryl-3h-benzoimidazol-4- carbonsäurederivate und verwandte verbindungen als gyrase und/oder topoisomerase iv inhibitoren zur behandlung von bakteriellen infektionen |
| US7582641B2 (en) | 2003-01-31 | 2009-09-01 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| AR042956A1 (es) * | 2003-01-31 | 2005-07-13 | Vertex Pharma | Inhibidores de girasa y usos de los mismos |
| US7569591B2 (en) | 2003-01-31 | 2009-08-04 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| US7618974B2 (en) * | 2003-01-31 | 2009-11-17 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
| US8394803B2 (en) | 2005-11-07 | 2013-03-12 | Vertex Pharmaceuticals Incorporated | Gyrase inhibitors and uses thereof |
-
2004
- 2004-07-29 US US10/901,928 patent/US7569591B2/en not_active Expired - Fee Related
- 2004-10-21 DK DK04810009T patent/DK1789419T3/da active
- 2004-10-21 AU AU2004322641A patent/AU2004322641B2/en not_active Ceased
- 2004-10-21 ZA ZA200701629A patent/ZA200701629B/xx unknown
- 2004-10-21 WO PCT/US2004/034919 patent/WO2006022773A1/en active Application Filing
- 2004-10-21 PT PT04810009T patent/PT1789419E/pt unknown
- 2004-10-21 CA CA2577758A patent/CA2577758C/en not_active Expired - Fee Related
- 2004-10-21 KR KR1020077005024A patent/KR20070048762A/ko not_active Application Discontinuation
- 2004-10-21 EP EP04810009A patent/EP1789419B1/en not_active Expired - Lifetime
- 2004-10-21 AT AT04810009T patent/ATE433980T1/de active
- 2004-10-21 PL PL04810009T patent/PL1789419T3/pl unknown
- 2004-10-21 SI SI200431220T patent/SI1789419T1/sl unknown
- 2004-10-21 ES ES04810009T patent/ES2325026T3/es not_active Expired - Lifetime
- 2004-10-21 DE DE602004021644T patent/DE602004021644D1/de not_active Expired - Lifetime
-
2009
- 2009-06-04 US US12/478,372 patent/US8034832B2/en not_active Expired - Fee Related
- 2009-09-07 CY CY20091100932T patent/CY1110230T1/el unknown
- 2009-09-15 HR HR20090491T patent/HRP20090491T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| DE602004021644D1 (de) | 2009-07-30 |
| ZA200701629B (en) | 2008-09-25 |
| US20090325935A1 (en) | 2009-12-31 |
| AU2004322641B2 (en) | 2012-05-31 |
| WO2006022773A1 (en) | 2006-03-02 |
| PL1789419T3 (pl) | 2009-11-30 |
| KR20070048762A (ko) | 2007-05-09 |
| SI1789419T1 (sl) | 2009-12-31 |
| EP1789419A1 (en) | 2007-05-30 |
| CY1110230T1 (el) | 2015-01-14 |
| CA2577758A1 (en) | 2006-03-02 |
| EP1789419B1 (en) | 2009-06-17 |
| PT1789419E (pt) | 2009-09-17 |
| ATE433980T1 (de) | 2009-07-15 |
| ES2325026T3 (es) | 2009-08-24 |
| AU2004322641A1 (en) | 2006-03-02 |
| US7569591B2 (en) | 2009-08-04 |
| DK1789419T3 (da) | 2009-08-10 |
| CA2577758C (en) | 2012-12-18 |
| US20050038247A1 (en) | 2005-02-17 |
| US8034832B2 (en) | 2011-10-11 |
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