HRP20191026T1 - Novi derivati hidroksamične kiseline ili njihove soli - Google Patents
Novi derivati hidroksamične kiseline ili njihove soli Download PDFInfo
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- HRP20191026T1 HRP20191026T1 HRP20191026TT HRP20191026T HRP20191026T1 HR P20191026 T1 HRP20191026 T1 HR P20191026T1 HR P20191026T T HRP20191026T T HR P20191026TT HR P20191026 T HRP20191026 T HR P20191026T HR P20191026 T1 HRP20191026 T1 HR P20191026T1
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- 150000003839 salts Chemical class 0.000 title claims 21
- NEAQRZUHTPSBBM-UHFFFAOYSA-N 2-hydroxy-3,3-dimethyl-7-nitro-4h-isoquinolin-1-one Chemical compound C1=C([N+]([O-])=O)C=C2C(=O)N(O)C(C)(C)CC2=C1 NEAQRZUHTPSBBM-UHFFFAOYSA-N 0.000 title 1
- 239000002253 acid Substances 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 claims 29
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 27
- 150000001875 compounds Chemical class 0.000 claims 22
- 125000002029 aromatic hydrocarbon group Chemical group 0.000 claims 13
- 125000000623 heterocyclic group Chemical group 0.000 claims 13
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 11
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 11
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 6
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 5
- 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 5
- 125000002252 acyl group Chemical group 0.000 claims 5
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 5
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 5
- 125000006591 (C2-C6) alkynylene group Chemical group 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 4
- 125000005110 aryl thio group Chemical group 0.000 claims 4
- 125000004104 aryloxy group Chemical group 0.000 claims 4
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 4
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 4
- -1 isovaleryl group Chemical group 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000001820 oxy group Chemical group [*:1]O[*:2] 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 125000003808 silyl group Chemical group [H][Si]([H])([H])[*] 0.000 claims 4
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 3
- 125000003277 amino group Chemical group 0.000 claims 3
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 238000006467 substitution reaction Methods 0.000 claims 3
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 125000006590 (C2-C6) alkenylene group Chemical group 0.000 claims 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- DWUWQSPGGAUCFL-VNJOCVIMSA-N (2S)-2-[[4-[2-[4-[(1S,2S)-1,2-dihydroxypropyl]phenyl]ethynyl]benzoyl]-methylamino]-N-hydroxy-N',2-dimethylpropanediamide Chemical compound O[C@H]([C@H](C)O)C1=CC=C(C=C1)C#CC1=CC=C(C(=O)N([C@](C(=O)NO)(C(=O)NC)C)C)C=C1 DWUWQSPGGAUCFL-VNJOCVIMSA-N 0.000 claims 1
- OAJLLWZPLIDAFL-BWKNWUBXSA-N (2S)-N-hydroxy-2-[[4-[2-[4-[(1S)-1-hydroxy-2-(2-hydroxyethoxy)ethyl]phenyl]ethynyl]benzoyl]-methylamino]-N',2-dimethylpropanediamide Chemical compound ONC([C@@](C(=O)NC)(C)N(C)C(C1=CC=C(C=C1)C#CC1=CC=C(C=C1)[C@@H](COCCO)O)=O)=O OAJLLWZPLIDAFL-BWKNWUBXSA-N 0.000 claims 1
- ZGLQMYZBECECRC-VWLOTQADSA-N (2S)-N-hydroxy-2-[[4-[2-[4-[3-hydroxy-2-(hydroxymethyl)propyl]phenyl]ethynyl]benzoyl]-methylamino]-N',2-dimethylpropanediamide Chemical compound ONC([C@@](C(=O)NC)(C)N(C)C(C1=CC=C(C=C1)C#CC1=CC=C(C=C1)CC(CO)CO)=O)=O ZGLQMYZBECECRC-VWLOTQADSA-N 0.000 claims 1
- XYGACYZKHBVOLP-BVHINDKJSA-N (2s)-2-[[4-[2-[4-(1,2-dihydroxyethyl)phenyl]ethynyl]benzoyl]-methylamino]-n-hydroxy-n',2-dimethylpropanediamide Chemical compound C1=CC(C(=O)N(C)[C@@](C)(C(=O)NC)C(=O)NO)=CC=C1C#CC1=CC=C(C(O)CO)C=C1 XYGACYZKHBVOLP-BVHINDKJSA-N 0.000 claims 1
- QZUMVPABESDUKR-YKSBVNFPSA-N (2s)-2-[[4-[2-[4-[(1r)-1,3-dihydroxypropyl]phenyl]ethynyl]benzoyl]-methylamino]-n-hydroxy-n',2-dimethylpropanediamide Chemical compound C1=CC(C(=O)N(C)[C@@](C)(C(=O)NC)C(=O)NO)=CC=C1C#CC1=CC=C([C@H](O)CCO)C=C1 QZUMVPABESDUKR-YKSBVNFPSA-N 0.000 claims 1
- PNLQFYNPWAEUJY-YKSBVNFPSA-N (2s)-n-hydroxy-2-[[4-[2-[4-[(1s)-1-hydroxy-2-methoxyethyl]phenyl]ethynyl]benzoyl]-methylamino]-n',2-dimethylpropanediamide Chemical compound C1=CC(C(=O)N(C)[C@@](C)(C(=O)NC)C(=O)NO)=CC=C1C#CC1=CC=C([C@H](O)COC)C=C1 PNLQFYNPWAEUJY-YKSBVNFPSA-N 0.000 claims 1
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 claims 1
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 1
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims 1
- 229940123346 LpxC inhibitor Drugs 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 150000004945 aromatic hydrocarbons Chemical class 0.000 claims 1
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 150000002926 oxygen Chemical class 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
- C07C259/04—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
- C07C259/06—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D305/00—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
- C07D305/02—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D305/04—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D305/08—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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 atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
- C07D309/10—Oxygen atoms
- C07D309/12—Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
-
- 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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- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Epoxy Compounds (AREA)
Claims (15)
1. Spoj predstavljen općom formulom [1]:
naznačen time, da
R1 predstavlja atom vodika, po izboru supstituiranu C1-6 alkil skupinu, po izboru supstituiranu C3-8 cikloalkil skupinu ili po izboru supstituiranu C1-6 alkoksi skupinu;
R2 predstavlja atom vodika, po izboru supstituiranu C1-6 alkil skupinu, po izboru supstituiranu C3-8 cikloalkil skupinu ili po izboru supstituiranu C1-6 alkoksi skupinu;
R3 predstavlja atom vodika ili po izboru supstituiranu C1-6 alkilnu skupinu;
R4 predstavlja atom vodika, po izboru supstituiranu C1-6 alkil skupinu, po izboru supstituiranu C3-8 cikloalkil skupinu, po izboru supstituiranu C1-6-alkoksi skupinu, po izboru supstituiranu aromatsku ugljikovodičnu skupinu ili po izboru supstituiranu heterocikličku skupinu;
X1 predstavlja po izboru supstituiranu C1-6 alkilensku skupinu, prema potrebi supstituiranu C2-6 alkenilen skupinu ili po izboru supstituiranu C2-6 alkinilensku skupinu;
A predstavlja po izboru supstituiranu C3-8 cikloalkilensku skupinu ili po izboru supstituiranu dvovalentnu aromatsku ugljikovodičnu skupinu;
X2 predstavlja skupinu opće formule [3]:
pri čemu X2a predstavlja po izboru supstituiranu C1-5 alkilensku skupinu, pod uvjetom da je X2a vezan na Y1;
Y1 predstavlja atom kisika ili atom sumpora; i
R5 predstavlja atom vodika, po izboru supstituiranu C1-6 alkil skupinu, po izboru supstituiranu C2-6 alkenilskupinu, po izboru supstituiranu C2-6 alkinil, po izboru supstituiranu aromatski ugljikovodik, po izboru supstituiranu kisik koji sadržavaju heterocikličku skupinu, hidroksil-zaštitnu skupinu ili tiol-zaštitnu skupinu,
ili njezinu sol;
pri čemu su supstituenti za C1-6 alkil skupinu i C1-6 alkoksi skupinu od R1 su jedna ili više skupina odabranih iz skupine supstituenata A;
supstituenti za C3-8 cikloalkil skupinu od R1 su jedna ili više skupina odabranih iz skupine supstituenata B;
supstituenti za C1-6 alkil skupinu i C1-6 alkoksi skupinu od R2 su jedna ili više skupina odabranih iz skupine supstituenata A;
supstituenti za C3-8 cikloalkil skupinu od R2 su jedna ili više skupina odabranih iz skupine supstituenata B;
supstituenti za C1-6 alkil skupinu od R3 su jedna ili više skupina odabranih iz skupine supstituenata A;
supstituenti za C1-6 alkil skupinu i C1-6 alkoksi skupinu od R4 su jedna ili više skupina odabranih iz skupine supstituenata A;
supstituenti za C3-8 cikloalkil skupinu, aromatske ugljikovodične skupine i heterocikličke skupine od R4 su jedna ili više skupina odabranih iz skupine supstituenata B;
supstituenti za C1-6 alkilensku skupinu, C2-6 alkenilen skupinu i C2-6 alkinilen skupinu od X1 su jedna ili više skupina odabranih iz skupine supstituenata B;
supstituenti za C3-8 cikloalkilensku skupinu i dvovalentnu aromatsku ugljikovodičnu skupinu od A su jedna ili više skupina odabranih od skupine supstituenata B;
supstituenti za C1-5 alkilensku skupinu od X2a su jedna ili više skupina odabranih od skupine supstituenata B;
supstituenti za C1-6 alkil skupinu, C2-6 alkenilna grupa i C2-6 alkinil skupinu od R5 su jedna ili više skupina odabranih iz skupine supstituenata A;
supstituenti za aromatske ugljikovodične skupine i heterocikličke skupine koji sadržava kisik od R5 su jedna ili više skupina odabranih iz skupine supstituenata B;
supstitucijsku skupinu A čine: halogeni atom; cijano skupina; nitro skupina; okso skupina; po izboru supstituirana karbamoilna skupina; po izboru supstituirana C3-8 cikloalkilna skupina; po izboru supstituirana C1-6alkoksi skupina; po izboru supstituirana C1-6 alkilamino skupina; opcijski supstituirana di(C1-6 alkil) amino skupina; po izboru supstituirana aromatska ugljikovodična skupina; po izboru supstituirana ariloksi skupina; po izboru supstituirana ariltio skupina; po izboru supstituirana heterociklička skupina; po izboru supstituirana heterociklička oksi skupina; po izboru zaštićena amino skupina; po izboru zaštićena imino skupina; po izboru zaštićena hidroksilna skupina; i po izboru zaštićenu karboksilnu skupinu;
supstitucijsku skupinu B čine: halogeni atom; cijano skupina; nitro skupina; okso skupina; po izboru supstituirana karbamoilna skupina; opcionalno supstituirana C1-6 alkilna skupina; po izboru supstituirana C2-6 alkenilna skupina; po izboru supstituirana C2-6 alkinilna skupina; po izboru supstituirana C3-8 cikloalkilna skupina; po izboru supstituirana C1-6 alkoksi skupina; po izboru supstituirana C1-6 alkilamino skupina; opcijski supstituirana di(C1-6 alkil) amino skupina; po izboru supstituirana aromatska ugljikovodična skupina; po izboru supstituirana ariloksi skupina; po izboru supstituirana ariltio skupina; po izboru supstituirana heterociklička skupina; po izboru supstituirana heterociklička oksi skupina; po izboru zaštićena amino skupina; po izboru zaštićena imino skupina; po izboru zaštićena hidroksilna skupina; i po izboru zaštićena karboksilna skupina;
karbamoilna skupina, C3-8 cikloalkilna skupina, C1-6 alkoksi skupina, C1-6alkilamino skupina, di(C1-6 alkil) amino skupina, aromatska ugljikovodična skupina, ariloksi skupina, ariltio skupina, heterociklička skupina i heterociklička oksi skupina supstitucijske skupine A, i karbamoilna skupina, C1-6 alkilna skupina, C1-6 alkenilna skupina, C1-6 alkinilna grupa, C3-8 cikloalkilna skupina, C1-6 alkoksi skupina, C1-6 alkilamino skupina, di(C1-6 alkil) amino skupina, aromatska ugljikovodična skupina, ariloksi skupina, ariltio skupina, heterociklička skupina i heterociklička oksi skupina u supstituentskoj skupini Bje svaka po izboru supstituirana s jednom ili više skupina odabranih između atoma halogena, cijano skupine, nitro grupe, C1-6 alkilne skupine, C2-6 alkenilne skupine, C2-6 alkinilna . skupina, C1-6 alkoksi skupine, acilna skupine, C1-6 alkilamino skupine, di(C1-6 alkil)amino skupine, C1-6 alkiltio skupine, C1-6 alkilsulfonilne skupine, arilsulfonil skupine, C3-8 cikloalkilne skupine, aromatske ugljikovodične skupine, heterocikličke skupine, karbamoilne skupine, amino skupine, karboksilne skupine i hidroksilne skupine;
hidroksilna zaštitna skupina predstavlja C1-6 alkil skupinu, C2-6-alkenilnu skupinu, arC1-6 alkil skupinu, C1-6-alkoksi-C1-5-alkil skupinu, ar-C1-6 alkoksi-C1-6 alkil skupinu, acil skupinu, C1-6 alkoksikarbonil skupinu, ar-C1-6alkoksikarbonilnu skupinu, C1-6 alkilsulfonilnu skupinu, arilsulfonilnu skupinu, sililnu skupinu, tetrahidrofuranil skupinu i tetrahidropiranilnu skupinu;
tiol-zaštitna skupinu označava C1-6- alkilnu skupinu, C2-6-alkenilnu skupinu, ar-C1-6- alkilnu skupinu, C1-5-alkoksi- C1-6- alkilnu skupinu, acilnu skupinu i silil skupinu;
amino-zaštitna skupina označava Ar-C1-6-alkil skupinu, C1-6-alkoksi-C1-6-alkil skupinu, acilnu skupinu, C1-6 alkoksikarbonilnu skupinu, Ar-C1-6alkoksikarbonil skupinu, ariloksikarbonilnu skupinu, C1-6 alkilsulfonilnu
skupinu, arilsulfonilnu skupinu i sililnu skupinu;
imino-zaštitna skupina označava C2-12 alkanoilnu skupinu s ravnim ili razgrananim lancem kao stoje acetilna skupina, propionilna skupina i izovalerilna skupina;
karboksil-zaštitna skupina predstavlja C1-6 alkil skupinu, C2-5-alkenilnu skupinu, aromatsku ugljikovodičnu skupinu, ar-C1-6 alkil skupinu, C1-6-alkoksi-C1-6 alkil skupinu ar- C1-6 alkoksi-C1-6 alkilnu skupinu, acil-C1-6akilnu skupinu, aciloksi-C1-6 alkilnu skupinu i sililnu skupinu.
2. Spoj ili njegova sol u skladu s patentnim zahtjevom 1, naznačen time, da je navedeni spoj predstavljen općom formulom [2]:
pri čemu su R1, R2, R3, R4, R5, X1, X2, Y1, i A su kao što je definirano u patentnom zahtjevu 1.
3. Spoj ili njegova sol u skladu s bilo kojim od patentnih zahtjeva 1 ili 2, naznačen time, da je X1 po izboru supstituirani C2-6 alkinilen; pri čemu su supstituenti za C2-6 alkinilensku skupinu od X1 kao što je definirano u patentnom zahtjevu 1.
4. Spoj ili njegova sol u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time, da je A po izboru supstituirana dvovalentna aromatska ugljikovodična skupina;
pri čemu su supstituenti za dvovalentnu aromatsku ugljikovodičnu skupinu A kao što je definirano u patentnom zahtjevu 1.
5. Spoj ili njegova sol u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time, da Y1 predstavlja atom kisika.
6. Spoj ili njegova sol u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time, da je R5 vodikov atom, po izboru supstituirana C1-6 alkil skupina, po izboru supstituirana C2-6 alkenil skupina, po izboru supstituirana C2-6 alkinil skupina, hidroksilna zaštitna skupina ili tiol zaštitna skupina,
pri čemu su supstituenti za C1-6 alkil skupinu, C2-6 alkenilnu skupinu i C2-6 alkinil skupinu od R5, hidroksil-zaštitna skupina i tiol-zaštitna skupina kao stoje definirano u patentnom zahtjevu 1.
7. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1 do 6, naznačen time, da je X2 skupina predstavljena općom formulom [4]:
pri čemu X2a predstavlja po izboru supstituiranu C1-5 alkilensku skupinu, pod uvjetom da je X2a vezan na Y1; pri čemu su supstituenti za C1-5 alkilensku skupinu od X2a definiranu kao što je definirano u patentnom zahtjevu 1.
8. Spoj ili njegova sol u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time, da se spoj bira između (2S)-2-((4-((4-(l,2-dihidroksietil)fenil)etinil)benzoil)(metil)amino)-N-hidroksi-N',2-dimetilmalonamid, (2S)-N-hidroksi-2-((4-((4-(3-hidroksi-2-(hidroksimetil)propil)fenil)etinil)benzoil)(metil)amino)-N',2-dimetilmalonamid, (2S)-2-((4-((4-((1R)-l,2-dihidroksietil)fenil)etinil)benzoil)(metil)amino)-N;-hidroksi-N',2-dimetilmalonamid, (2S)-2-((4-((4-((1S)-l,2-dihidroksietil)fenil)etinil)benzoil)(metil)amino)-N-hidroksi;-N',2-dimetilmalonamid, (2S)-N-hidroksi-2-((4-((4-((1S)-l-hidroksi-2-metoksietil)fenil)etinil)benzoil)(metil)amino)-N',2-dimetilmalonamid, (2S)-N-hidroksi-2-((4-((4-((1S)-l-hidroksi-2-(2-hidroksietoksi)etil)fenil)etinil)benzoil)(metil)amino)-N',2-dimetilmalonamid, (2S)-2-((4-((4-((1R)-l,3-dihidroksipropil)fenil)etinil)benzoil)(metil)amino)-N-hidroksi-N',2-dimetilmalonamid, (2S)-2-((4-((4-((1S,2S)-l,2-dihidroksipropil)fenil)etinil)benzoil)(metil)amino)-N-hidroksi-N',2-dimetilmalonamid, (2S)-2-((4-((4-(l,4-dihidroksibutil)fenil)etinil)benzoil)(metil)amino)-N-hidroksi-N2-dimetilmalonamidi(2S)-N-hidroksi-2-((4-((4-((1R)-l-hidroksi-3-metoksipropil)fenil)etinil)benzoil)(metil)amino)-N;",2-dimetilmalonamid.
9. Spoj ili njegova sol u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time, da je spoj (2S)-2-((4-((4-(l,2-dihidroksietil)fenil)etinil)benzoil)(metil)amino)-N-hidroksi-N',2-dimetilfnalonamid ili njegova sol.
10. Spoj ili njegova sol u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time, da je spoj (2S)-2-((4-((4-((1R)-l,2-Dihidroksietil)fenil)etinil.)benzoil)(metil)amino)-N-hidroksi-N',2-dimetilmalonamid ili njegova sol.
11. Spoj ili njegova sol u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time, da je spoj (2S)-2-((4-((4-((1S)-l,2-dihidroksietil)fenil)etinil)benzoil)(metil)amino)-N-hidroksi-N',2-dimetilmalonamid ili njegova sol.
12. Spoj ili njegova sol u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time, da je spoj (2R)-2-((4-((4-((1R)-l,2-Dihidroksietil)fenil)etinil)benzoil)(metil)amino)-N-hidroksi-N',2-dimetilmalonamid ili njegova sol.
13. Spoj ili njegova sol u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time, da je spoj (2S)-N-hidrokši-2-((4-((4-((1S)-l-hidroksi-2);metoksietil)fenil)etinil)benzoil)(meti|)amino)-N',2-dimetilmalonamid ili njegove soli.
14. Inhibitor LpxC, naznačen time, da sadržava spoj ili njegovu sol u skladu s bilo kojim od patentnih zahtjeva 1 do 13.
15. Antibakterijsko sredstvo, naznačeno time, da sadržava spoj ili njegovu sol u skladu s bilo kojim od patentnih zahtjeva 1 do 13.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2013052798 | 2013-03-15 | ||
| EP14763168.3A EP2975022B1 (en) | 2013-03-15 | 2014-03-14 | Novel hydroxamic acid derivative or salt thereof |
| PCT/JP2014/056864 WO2014142298A1 (ja) | 2013-03-15 | 2014-03-14 | 新規なヒドロキサム酸誘導体またはその塩 |
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| Publication Number | Publication Date |
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| HRP20191026T1 true HRP20191026T1 (hr) | 2019-10-18 |
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| HRP20191026TT HRP20191026T1 (hr) | 2013-03-15 | 2019-06-07 | Novi derivati hidroksamične kiseline ili njihove soli |
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| Country | Link |
|---|---|
| US (1) | US9862676B2 (hr) |
| EP (1) | EP2975022B1 (hr) |
| JP (1) | JP6259814B2 (hr) |
| CN (1) | CN105073710B (hr) |
| CA (1) | CA2905248A1 (hr) |
| CY (1) | CY1121626T1 (hr) |
| DK (1) | DK2975022T3 (hr) |
| ES (1) | ES2728336T3 (hr) |
| HR (1) | HRP20191026T1 (hr) |
| HU (1) | HUE043922T2 (hr) |
| LT (1) | LT2975022T (hr) |
| PL (1) | PL2975022T3 (hr) |
| PT (1) | PT2975022T (hr) |
| RS (1) | RS58930B1 (hr) |
| SI (1) | SI2975022T1 (hr) |
| TR (1) | TR201911245T4 (hr) |
| WO (1) | WO2014142298A1 (hr) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JP6458270B2 (ja) * | 2013-08-16 | 2019-01-30 | デューク ユニバーシティ | 置換されたヒドロキサム酸化合物 |
| CA2960949A1 (en) * | 2014-09-12 | 2016-03-17 | Tatsuya Honda | Novel pharmaceutical composition containing hydroxamic acid derivative or salt thereof |
| EP3192505A4 (en) * | 2014-09-12 | 2018-04-25 | Toyama Chemical Co., Ltd. | Method for using novel hydroxamic acid derivative and antibacterial substance in combination |
| WO2017170884A1 (ja) * | 2016-03-31 | 2017-10-05 | 富山化学工業株式会社 | 新規なヒドロキサム酸誘導体の製造方法およびその中間体 |
| CN109415302A (zh) * | 2016-03-31 | 2019-03-01 | 富士胶片富山化学株式会社 | 新的异羟肟酸衍生物的晶体、其制造方法及医药用组合物 |
| US20200062789A1 (en) | 2017-01-31 | 2020-02-27 | Fujifilm Toyama Chemical Co., Ltd. | Hydroxamic acid prodrug compound or salt thereof, lyophilized formulation, lpxc inhibitor, and antibacterial agent |
| CN110963907B (zh) * | 2019-12-05 | 2023-12-19 | 中国农业科学院植物保护研究所 | 一种2,2-二烷氧基苯乙酮衍生物的绿色合成 |
| CN117769548A (zh) | 2021-08-05 | 2024-03-26 | 浙江海正药业股份有限公司 | 芳香乙炔类衍生物及其制备方法和用途 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US20040229955A1 (en) | 2003-01-08 | 2004-11-18 | Andersen Niels H. | Antibacterial agents |
| CA2634005C (en) | 2005-12-15 | 2012-01-03 | Vicuron Pharmaceuticals Inc. | N-hydroxyamide derivatives possessing antibacterial activity |
| ES2602615T3 (es) | 2007-06-12 | 2017-02-21 | Achaogen, Inc. | Agentes antibacterianos |
| AU2009279949A1 (en) | 2008-08-04 | 2010-02-11 | Merck Sharp & Dohme Corp. | Urea derivatives as antibacterial agents |
| US8372885B2 (en) | 2008-09-17 | 2013-02-12 | Novartis Ag | Organic compounds and their uses |
| CA2735929C (en) | 2008-09-19 | 2013-12-17 | Pfizer Inc. | Hydroxamic acid derivatives useful as antibacterial agents |
| DK2562155T3 (da) | 2010-04-20 | 2019-06-24 | Fujifilm Toyama Chemical Co Ltd | Hydroxaminsyrederivat |
| WO2012031298A2 (en) * | 2010-09-03 | 2012-03-08 | Duke University | Ethynylbenzene derivatives |
| WO2013170165A1 (en) * | 2012-05-10 | 2013-11-14 | Achaogen, Inc. | Antibacterial agents |
| JP2016210683A (ja) | 2013-10-18 | 2016-12-15 | 大正製薬株式会社 | ヒドロキサム酸誘導体 |
| JP2016210682A (ja) | 2013-10-18 | 2016-12-15 | 大正製薬株式会社 | ヒドロキサム酸誘導体 |
-
2014
- 2014-03-14 RS RS20190827A patent/RS58930B1/sr unknown
- 2014-03-14 CA CA2905248A patent/CA2905248A1/en not_active Abandoned
- 2014-03-14 DK DK14763168.3T patent/DK2975022T3/da active
- 2014-03-14 PL PL14763168T patent/PL2975022T3/pl unknown
- 2014-03-14 WO PCT/JP2014/056864 patent/WO2014142298A1/ja active Application Filing
- 2014-03-14 PT PT14763168T patent/PT2975022T/pt unknown
- 2014-03-14 US US14/777,156 patent/US9862676B2/en active Active
- 2014-03-14 HU HUE14763168A patent/HUE043922T2/hu unknown
- 2014-03-14 TR TR2019/11245T patent/TR201911245T4/tr unknown
- 2014-03-14 LT LTEP14763168.3T patent/LT2975022T/lt unknown
- 2014-03-14 CN CN201480015562.1A patent/CN105073710B/zh active Active
- 2014-03-14 ES ES14763168T patent/ES2728336T3/es active Active
- 2014-03-14 JP JP2015505594A patent/JP6259814B2/ja active Active
- 2014-03-14 EP EP14763168.3A patent/EP2975022B1/en active Active
- 2014-03-14 SI SI201431227T patent/SI2975022T1/sl unknown
-
2019
- 2019-05-10 CY CY20191100509T patent/CY1121626T1/el unknown
- 2019-06-07 HR HRP20191026TT patent/HRP20191026T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ES2728336T3 (es) | 2019-10-23 |
| WO2014142298A1 (ja) | 2014-09-18 |
| HUE043922T2 (hu) | 2019-09-30 |
| EP2975022B1 (en) | 2019-05-08 |
| TR201911245T4 (tr) | 2019-08-21 |
| CN105073710B (zh) | 2018-02-16 |
| PT2975022T (pt) | 2019-06-11 |
| SI2975022T1 (sl) | 2019-08-30 |
| EP2975022A4 (en) | 2016-10-12 |
| JPWO2014142298A1 (ja) | 2017-02-16 |
| JP6259814B2 (ja) | 2018-01-10 |
| LT2975022T (lt) | 2019-07-25 |
| US9862676B2 (en) | 2018-01-09 |
| EP2975022A1 (en) | 2016-01-20 |
| CA2905248A1 (en) | 2014-09-18 |
| US20160039751A1 (en) | 2016-02-11 |
| RS58930B1 (sr) | 2019-08-30 |
| DK2975022T3 (da) | 2019-07-15 |
| PL2975022T3 (pl) | 2019-11-29 |
| CN105073710A (zh) | 2015-11-18 |
| CY1121626T1 (el) | 2020-07-31 |
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