HRP20140350T1 - Organski spojevi - Google Patents
Organski spojevi Download PDFInfo
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- HRP20140350T1 HRP20140350T1 HRP20140350AT HRP20140350T HRP20140350T1 HR P20140350 T1 HRP20140350 T1 HR P20140350T1 HR P20140350A T HRP20140350A T HR P20140350AT HR P20140350 T HRP20140350 T HR P20140350T HR P20140350 T1 HRP20140350 T1 HR P20140350T1
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- 150000002894 organic compounds Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 20
- 125000000623 heterocyclic group Chemical group 0.000 claims 12
- 125000002837 carbocyclic group Chemical group 0.000 claims 11
- 125000005843 halogen group Chemical group 0.000 claims 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 125000001033 ether group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 3
- 108091008648 NR7C Proteins 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 3
- 239000012907 medicinal substance Substances 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 125000006661 (C4-C6) heterocyclic group Chemical group 0.000 claims 2
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 2
- 101001043818 Mus musculus Interleukin-31 receptor subunit alpha Proteins 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000000081 (C5-C8) cycloalkenyl group Chemical group 0.000 claims 1
- HZMAFSFOEIRHAL-UHFFFAOYSA-N 6-chloro-3-[[3,4-dioxo-2-(pentan-3-ylamino)cyclobuten-1-yl]amino]-2-hydroxy-n-methoxy-n-methylbenzenesulfonamide Chemical compound O=C1C(=O)C(NC(CC)CC)=C1NC1=CC=C(Cl)C(S(=O)(=O)N(C)OC)=C1O HZMAFSFOEIRHAL-UHFFFAOYSA-N 0.000 claims 1
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims 1
- 206010027654 Allergic conditions Diseases 0.000 claims 1
- 101100212791 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) YBL068W-A gene Proteins 0.000 claims 1
- 101000585507 Solanum tuberosum Cytochrome b-c1 complex subunit 7 Proteins 0.000 claims 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 230000000954 anitussive effect Effects 0.000 claims 1
- 230000001387 anti-histamine Effects 0.000 claims 1
- 230000003110 anti-inflammatory effect Effects 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 229940124584 antitussives Drugs 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 239000012752 auxiliary agent Substances 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
- 230000003182 bronchodilatating effect Effects 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- PCHPORCSPXIHLZ-UHFFFAOYSA-N diphenhydramine hydrochloride Chemical compound [Cl-].C=1C=CC=CC=1C(OCC[NH+](C)C)C1=CC=CC=C1 PCHPORCSPXIHLZ-UHFFFAOYSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 238000002955 isolation Methods 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
- C07D213/52—Sulfur atoms
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/18—Sulfonamides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C311/48—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups having nitrogen atoms of sulfonamide groups further bound to another hetero atom
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/04—Heterocyclic compounds containing five-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
- C07D307/10—Heterocyclic compounds containing five-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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D307/14—Radicals substituted by nitrogen atoms not forming part of a nitro radical
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- C07—ORGANIC CHEMISTRY
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- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D307/40—Radicals substituted by oxygen atoms
- C07D307/42—Singly bound oxygen atoms
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D307/52—Radicals substituted by nitrogen atoms not forming part of a nitro radical
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- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
- C07D333/30—Hetero atoms other than halogen
- C07D333/36—Nitrogen atoms
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- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07C2601/14—The ring being saturated
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- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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- Pyridine Compounds (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Furan Compounds (AREA)
Claims (16)
1. Spoj, naznačen time, da ima formulu I
[image]
ili njegovi solvati, hidrati ili njegove farmaceutski prihvatljive soli, gdje
R1 je H, 3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina, 3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina, (C1-C4 alkil)-3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina, (C1-C4 alkil)-3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina, C1-C6 alkil opcijski supstituiran s jednim ili više atoma halogena, CN-skupinama ili OH-skupinama, C1-C6 alkoksi opcijski supstituiran s jednim ili više atoma halogena ili OH-skupinama, ili eter-skupina koja sadrži 2 do 10 atoma ugljika i 1 do 3 atoma kisika, pri čemu je eter-skupina opcijski supstituirana s jednim ili više supstituenata od kojih je svaki neovisno odabran od sljedećih: OH, halogen, 3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina. i 3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina;
R2 je 3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina, 3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina, (C1-C4 alkil)-3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina, (C1-C4 alkil)-3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina, C1-C6 alkil opcijski supstituiran s jednim ili više atoma halogena, CN-skupinama ili OH-skupinama, ili eter-skupina koja sadrži 2 do 10 atoma ugljika i 1 do 3 atoma kisika, pri čemu je eter-skupina opcijski supstituirana s jednim ili više supstituenata od kojih je svaki neovisno odabran od sljedećih: OH, halogen, 3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina, i 3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina, ili
R1 i R2, zajedno s atomom ugljika na kojega su priključeni, tvore 3 do 10-članu karbocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina, ili 3 do 10-članu heterocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina;
R3 je vodik, halogen ili cijano;
R4 je H, C1-C8 alkil, C3-C8 cikloalkil, C6-C8 cikloalkenil ili (C1-C4 alkil)-R6, gdje je svaka alkil-skupina opcijski supstituirana s jednim ili više atoma halogena;
R5 je C1-C8 alkil, C3-C8 cikloalkil, C5-C8 cikloalkenil, (C1-C4 alkil)-C3-C8 cikloalkil ili (C1-C4 alkil)-C5-C8 cikloalkenil, gdje je svaka alkil-skupina opcijski supstituirana s jednim ili više atoma halogena; ili
R1 i R6, zajedno s atomima kisika i dušika na koje su priključeni, tvore 5 do 10-članu heterocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina;
R6 je odabran od sljedećih: 3 do 10-člana karbociklička skupina opcijski supstituirana s jednom ili više Z-skupina, 3 do 10-člana heterociklička skupina opcijski supstituirana s jednom ili više Z-skupina, NR7R9, NR7(SO2)R9, (SO2)NR7R8, (SO2)R9, NR7C(O)R9, C(O)NR7R9, NR7C(O)NR8R9, NR7C(O)OR9, C(O)OR7, OC(O)R9, OC(O)NR7, C(O)R9, SR7, CN i NO2;
R7 i R8 su svaki neovisno odabrani od sljedećih: H, C1-C6 alkil, C3-C10 cikloalkil, C5-C10 cikloalkenil i -(C1-C3 alkilen)-C3-C10 cikloalkil;
R9 je odabran od sljedećih: H, C1-C6 alkil, -(C1-C3 alkilen)-C3-C10 cikloalkil,
3 do 10-člana karbociklička skupina, 3 do 10-člana heterociklička skupina, gdje je svaka od alkil-skupina i alkil-prstenastih sustava opcijski supstituiran(a) s OH, halo, C1-C3 alkil i C1-C3 alkoksi;
X je CR14 ili N;
Z je neovisno odabran od sljedećih: OH;
3 do 10-člana karbociklička skupina;
3 do 10-člana heterociklička skupina; benzil; C1-C6 alkil opcijski supstituiran s jednim ili više atoma halogena, CN-skupinama ili OH-skupinama; C1-C6 alkoksi opcijski supstituiran s jednim ili više atoma halogena, CN-skupinama ili OH-skupinama; -Oaril; -Obenzil; -O(CH2)aC(O)E; NR10(SO2)R12; (SO2)NR10R11; (SO2)R12;NR10C(O)R12; C(O)NR10R12; NR10C(O)NR11R12; NR10C(O)OR12; NR10R12; C(O)OR10; OC(O)R12; OC(O)NR10; C(O)R12; SR12; CN; NO2; i halogen; ili gdje postoje dva ili više Z supstituenta, ta dva Z supstituenta zajedno s atomima na koje su priključeni, opcijski tvore 5- do 7-člani karbociklički ili 4- do 7-člani heterociklički supstituent kondenziran na prstenasti sustav;
a je 0, 1, 2, 3 ili 4, gdje je alkilen-skupina opcijski supstituirana s OH ili NH2, kada
a je 1, 2, 3 ili 4; E je NR10R12 ili OR12;
svaki od R10 i R11 su neovisno odabrani od sljedećih:
H, C1-C6 alkil, C3-C10 cikloalkil, C5-C10 cikloalkenil i -(C1-C3alkilen)-C3-C10 cikloalkil;
svaki R12 je odabran od sljedećih: H, C1-C6 alkil, -(C1-C3 alkilen)-C3-C10 cikloalkil,
3 do 10-člana karbociklička skupina i 3 do 10-člana heterociklička skupina, gdje je svaki od tih prstenastih sustava opcijski supstituiran s OH, halo, C1-C3 alkil i C1-C3 alkoksi; i
R14 je H ili C1-C6 alkil.
2. Spoj prema zahtjevu 1, naznačen time, da R1 je H ili C1-C4 alkil.
3. Spoj prema zahtjevu 1 ili zahtjevu 2, naznačen time, da
R1 je H ili C1-C4 alkil;
R2 je C1-C6 alkil opcijski supstituiran s jednim ili više atoma halogena, CN-skupinama ili OH-skupinama, ili eter-skupina sadrži 2 do 10 atoma ugljika i 1 do 3 atoma kisika, 4 do 6-članu karbocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina, ili 4 do 6-članu heterocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina; ili
R1 i R2, zajedno s atomom ugljika na koji su priključeni, tvore 4 do 6-članu karbocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina ili 4 do 6-članu heterocikličku skupinu opcijski supstituiranu s jednom ili više Z-skupina.
4. Spoj prema bilo kojem prethodnom zahtjevu, naznačen time, da R3 je halogen.
5. Spoj prema bilo kojem prethodnom zahtjevu, naznačen time, da R4 je H, C1-C4 alkil, C3-C6 cikloalkil ili (C1-C3 alkil)-C3-C6 cikloalkil.
6. Spoj prema bilo kojem prethodnom zahtjevu, naznačen time, da R5 je C1-C6 alkil.
7. Spoj prema bilo kojem prethodnom zahtjevu, naznačen time, da X je CH.
8. Spoj prema zahtjevu 1, naznačen time, da je spoj odabran između sljedećih:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema zahtjevu 1, naznačen time, da je taj spoj
6-kloro-3-[2-(1-etil-propilamino)-3,4-diokso-ciklobut-1-enilamino]-2-hidroksi-N-metoksi-N-metil-benzensulfonamid sljedeće strukture:
[image]
ili njegova farmaceutski prihvatljiva sol.
10. Spoj prema bilo kojem od zahtjeva 1 do 9, naznačen time, da se taj spoj u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, upotrebljava kao farmaceutsko sredstvo.
11. Uporaba spoja prema bilo kojem od zahtjeva 1 do 9, naznačena time, da se taj spoj u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, koristi u proizvodnji lijeka za liječenje upalnih ili alergijskih stanja ili bolesti.
12. Uporaba prema zahtjevu 11, naznačena time, da to stanje je COPD.
13. Farmaceutski sastav, naznačen time, da obuhvaća spoj prema bilo kojem od zahtjeva 1 do 9, u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, zajedno s farmaceutski prihvatljivim nosačem ili pomoćnim sredstvom.
14. Postupak proizvodnje spoja prema bilo kojem od zahtjeva 1 do 9, naznačen time, da taj postupak obuhvaća reakciju spoja formule II
[image]
gdje su R3, R4 i R5 određeni u zahtjevu 1, sa spojem formule III
[image]
gdje su X, R1 i R2 određeni u zahtjevu 1; a zatim izolaciju proizvoda.
15. Kombinacija spoja prema bilo kojem od zahtjeva 1 do 9, naznačena time, da se taj spoj u slobodnom obliku ili u obliku farmaceutski prihvatljive soli, miješa s drugom ljekovitom tvari.
16. Kombinacija prema zahtjevu 15, naznačena time, da druga ljekovita tvar je protuupalna, bronhodilatacijska, antihistaminska ili antitusivna ljekovita tvar.
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