HRP20170441T1 - Tio-supstituirani derivati biaril-metansulfinila - Google Patents
Tio-supstituirani derivati biaril-metansulfinila Download PDFInfo
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- HRP20170441T1 HRP20170441T1 HRP20170441TT HRP20170441T HRP20170441T1 HR P20170441 T1 HRP20170441 T1 HR P20170441T1 HR P20170441T T HRP20170441T T HR P20170441TT HR P20170441 T HRP20170441 T HR P20170441T HR P20170441 T1 HRP20170441 T1 HR P20170441T1
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- Croatia
- Prior art keywords
- substituted
- alkyl
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- occurrence
- phenyl
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- -1 methylenedioxy group Chemical group 0.000 claims 76
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 61
- 229910052739 hydrogen Inorganic materials 0.000 claims 52
- 150000001875 compounds Chemical class 0.000 claims 50
- 229910052799 carbon Inorganic materials 0.000 claims 41
- 229910052731 fluorine Inorganic materials 0.000 claims 34
- 229910052801 chlorine Inorganic materials 0.000 claims 32
- 229910052794 bromium Inorganic materials 0.000 claims 30
- 125000003118 aryl group Chemical group 0.000 claims 28
- 229910052757 nitrogen Inorganic materials 0.000 claims 25
- 125000001072 heteroaryl group Chemical group 0.000 claims 21
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 18
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 17
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 17
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 16
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 16
- 150000003839 salts Chemical group 0.000 claims 16
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 16
- 229910052760 oxygen Inorganic materials 0.000 claims 15
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 14
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 14
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 12
- 125000001041 indolyl group Chemical group 0.000 claims 11
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 10
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 10
- 125000005842 heteroatom Chemical group 0.000 claims 10
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 10
- 239000000203 mixture Substances 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 10
- 125000003710 aryl alkyl group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 125000000168 pyrrolyl group Chemical group 0.000 claims 9
- 125000004432 carbon atom Chemical group C* 0.000 claims 8
- 125000002950 monocyclic group Chemical group 0.000 claims 8
- 125000004076 pyridyl group Chemical group 0.000 claims 8
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 7
- 125000004618 benzofuryl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 7
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 7
- 125000002541 furyl group Chemical group 0.000 claims 7
- 125000000842 isoxazolyl group Chemical group 0.000 claims 7
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 7
- ZIJTYIRGFVHPHZ-UHFFFAOYSA-N selenium oxide(seo) Chemical group [Se]=O ZIJTYIRGFVHPHZ-UHFFFAOYSA-N 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- 125000001544 thienyl group Chemical group 0.000 claims 7
- 208000032140 Sleepiness Diseases 0.000 claims 6
- 206010041349 Somnolence Diseases 0.000 claims 6
- 201000003631 narcolepsy Diseases 0.000 claims 6
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 6
- 230000037321 sleepiness Effects 0.000 claims 6
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 6
- KVGZZAHHUNAVKZ-UHFFFAOYSA-N 1,4-Dioxin Chemical compound O1C=COC=C1 KVGZZAHHUNAVKZ-UHFFFAOYSA-N 0.000 claims 5
- 125000001162 cycloheptenyl group Chemical group C1(=CCCCCC1)* 0.000 claims 5
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims 5
- 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 0.000 claims 5
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 5
- 125000001624 naphthyl group Chemical group 0.000 claims 5
- 125000004043 oxo group Chemical group O=* 0.000 claims 5
- 229910052711 selenium Inorganic materials 0.000 claims 5
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 4
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 4
- 239000004215 Carbon black (E152) Substances 0.000 claims 4
- 208000012902 Nervous system disease Diseases 0.000 claims 4
- 208000018737 Parkinson disease Diseases 0.000 claims 4
- 101100054666 Streptomyces halstedii sch3 gene Proteins 0.000 claims 4
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 4
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 4
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 4
- 125000002837 carbocyclic group Chemical group 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 229930195733 hydrocarbon Natural products 0.000 claims 4
- 208000013403 hyperactivity Diseases 0.000 claims 4
- 125000002883 imidazolyl group Chemical group 0.000 claims 4
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 208000001797 obstructive sleep apnea Diseases 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 125000001425 triazolyl group Chemical group 0.000 claims 4
- XXJGBENTLXFVFI-UHFFFAOYSA-N 1-amino-methylene Chemical compound N[CH2] XXJGBENTLXFVFI-UHFFFAOYSA-N 0.000 claims 3
- 125000001462 1-pyrrolyl group Chemical group [*]N1C([H])=C([H])C([H])=C1[H] 0.000 claims 3
- 125000000539 amino acid group Chemical group 0.000 claims 3
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000002757 morpholinyl group Chemical group 0.000 claims 3
- 208000025966 Neurological disease Diseases 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 208000033914 shift work type circadian rhythm sleep disease Diseases 0.000 claims 2
- 208000019116 sleep disease Diseases 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- UUFQTNFCRMXOAE-UHFFFAOYSA-N 1-methylmethylene Chemical compound C[CH] UUFQTNFCRMXOAE-UHFFFAOYSA-N 0.000 claims 1
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 1
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 1
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 claims 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- SYGWYBOJXOGMRU-UHFFFAOYSA-N chembl233051 Chemical compound C1=CC=C2C3=CC(C(N(CCN(C)C)C4=O)=O)=C5C4=CC=CC5=C3SC2=C1 SYGWYBOJXOGMRU-UHFFFAOYSA-N 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 235000019256 formaldehyde Nutrition 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000005954 phenoxathiinyl group Chemical group 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000004055 thiomethyl group Chemical group [H]SC([H])([H])* 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/02—Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to acyclic carbon atoms
- C07C317/10—Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/64—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton
- C07C323/65—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfone or sulfoxide groups bound to the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
- C07D207/325—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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 with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
- C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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 with substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/333—Radicals substituted by oxygen or sulfur atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
- C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
-
- 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
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/40—Acylated substituent nitrogen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
- C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/04—Systems containing only non-condensed rings with a four-membered ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/10—Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated
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- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/16—Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated
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- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/18—Systems containing only non-condensed rings with a ring being at least seven-membered
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Furan Compounds (AREA)
- Pyridine Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pyrrole Compounds (AREA)
- Indole Compounds (AREA)
- Quinoline Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (45)
1. Spoj formule (Ii):
[image]
njegovi stereoizomerni oblici, smjese stereoizomernih oblika ili njihovi farmaceutski prihvatljivi oblici soli,
pri čemu:
Ar je C6-C10 aril grupa supstituirana sa 0-5 R3;
C5-C10 cikloalkenil supstituiran sa 0-5 R3; ili
5 do 14-točlana heteroaril grupa supstituirana sa 0-5 R3, pri čemu spomenuta heteroaril grupa sadrži jedan, dva ili tri heteroatoma odabrana od N, O, S ili Se;
Y je -CH2-, -CH(OCH3) -, ili -CH2CH2-;
R1 je C(=O)NR12R13;
R2 je odabran od H, F, Cl, Br, J, OR16, OR25, NR17R18, NHOH, NO2, CN, CF3, C1-C6alkil, C2- C6 alkenil, C2-C6 alkinil, C(=O)R16, C(=O)OR16, OC(=O)R16, C(=O)NR17R18, NR15C(=O)R16, NR15CO2R16, OC(=O)NR17R18, NR15C(=S)R16, SR16; S(=O)R16; i S(=O)2R16;
alternativno, dvije R2 grupe se mogu kombinirati da formiraju metilendioksi grupu, etilendioksi grupu, ili propilendioksi grupu;
R3 je odabran od H, F, Cl, Br, J, OR16, OCF3, OR25, NR17R18, NHOH, NO2, CN, CF3, CH2OR16, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C7 cikloalkil, 3-7 člani heterocikloalkil, fenil, 5 ili 6 člani heteroaril, C7-C10arilalkil, C(=O)R16, C(=O)OR16, OC(=O)R16, C(=O)NR17R18, NR15C(=O)R16, NR15CO2R16, OC(=O)NR17R18, NR15C(=S)R16, SR16; S(=O)R16; S(=O)2 R16, i NR15S(=O)2R16;
alternativno, dvije R3 grupe se mogu kombinirati da formiraju metilendioksi grupu, etilendioksi grupu ili propilendioksi grupu;
R4 i R5 su H;
R12 i R13 u svakom pojavljivanju su svaki nezavisno odabrani od: H, C1-C6 alkil supstituiran sa 0-3 R20 i C6-C10 aril, supstituiran sa 0-3 R20;
alternativno, R12 i R13, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten supstituiran sa 0-3 R20;
R15 je u svakom pojavljivanju nezavisno odabran od H i C1-C6 alkil;
R16 je u svakom pojavljivanju nezavisno odabran od H, C1-C6 alkil, i C6-C10 aril;
R17 i R18 u svakom pojavljivanju su svaki nezavisno odabrani od H, C1-C6 alkil, i C6-C10 aril, ili alternativno, R17 i R18, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten, pri čemu je spomenuti 3-7 člani heterociklični prsten supstituiran sa 0-2 okso grupe;
R20 je u svakom pojavljivanju nezavisno odabran od: F, Cl, Br, J, OH, OR22, OR21, NR23R24, NHOH, NO2, CN, CF3, C1-C6alkil, C1-C6alkil-OH, C2-C6alkenil, C2-C6alkinil, C3-C7cikloalkil, 3-7 člani heterocikloalkil, fenil supstituiran sa 0-1 R26; 5 ili 6 člani heteroaril, C7-C10 arilalkil, =O, C(=O)R22, C(=O)OR22, OC(=O)R22, C(=O)NR23R24, NR21C(=O)R22 , NR21CO2R22, OC(=O) NR23R24, NR21C(=S)R22, SR22; S(=O)R22; i S(=O)2R22;
R21 je u svakom pojavljivanju nezavisno odabran od H i C1-C6 alkil;
R22 je u svakom pojavljivanju nezavisno odabran od H, C1-C6alkil, C1-C6alkil-OH, i C6-C10aril;
R23 i R24 su u svakom pojavljivanju svaki nezavisno odabrani od H, C1-C6 alkil, i C6-C10 aril, ili alternativno, R23 i R24, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten;
R25 je u svakom pojavljivanju nezavisno aminokiselinski ostatak nakon uklanjanja hidroksilne grupe iz karboksilne grupe sa formulom -C(=O)CH(NH2)-(bočni lanac), pri čemu je bočni lanac izabran između:
H CH3CH(CH3)2
CH2CH(CH3)2CH(CH3)CH2CH3 ̧CH2OH
CH2SH CH(OH)CH3 CH2CH2SCH3
CH2C6H5(CH2)4NH2, (CH2)3NHC(=NH)NH2
CH2COOH CH2CH2COOH CH2CONH2
CH2CH2CONH2CH2CH3CH2CH2CH3
CH2CH2CH2CH3 CH2CH2SH CH2CH2OH
CH2CH2SCH3(CH2)3NH2(CH2)2CH(OH)CH2NH2
(CH2)3NHC(=O)NH2 (CH2)2ONHC(=NH)NH2 CH2C(=O)NHCH2COOH
[image]
[image]
i
[image]
R26 je u svakom pojavljivanju nezavisno odabran od H, F, Cl, Br, C1-C6 alkil, i C1-C6 alkoksi; i
x je 0, 1, 2, 3 ili 4;
pod uvjetom da
(i) kada Y je -CH2-; Ar je fenil supstituiran sa 0-2 R3, i R3 je H, F, Cl, Br, J, CH3, OCH3, SCH3, CN, NO2 ili metilendioksifenil; onda je Ar u orto ili meta položaju u odnosu na supstituent -C(R4)(R5)- na jezgru fenil prstena;
(ii) kada Ar predstavlja imidazopiridin supstituiran sa 0-5 R3, Ar je u orto ili meta položaju u odnosu na -C(R4)(R5)- supstituent na jezgru fenil prstena; i
(iii) kada je Ar u meta položaju u odnosu na -C(R4)(R5)- supstituent na jezgru fenil prstena, a Ar je heteroaril grupa vezana za fenil prsten preko atoma dušika, onda je Ar pirolil, indolil, imidazolil, benzimidazolil, benzotriazolil, triazolil, ili 1,3-dihidroizoindolil;
pri čemu se "aril" odnosi na supstituirane ili nesupstituirane, mono- ili biciklične ugljikovodične aromatične prstenske sisteme koji imaju 6 do 10 atoma ugljika; "heterociklični" se odnosi na supstituiranu ili nesupstituiranu karbocikličnu grupu u kojoj prstenski dio obuhvaća najmanje jedan do četiri heteroatoma, kao što su O, N ili S; a "cikloalkil" se odnosi na zasićeni ili djelomično zasićeni mono- ili biciklični alkil prstenski sistem koji sadrži 3 do 10 atoma ugljika.
2. Spoj prema patentnom zahtjevu 1 Formule (Ii) u kojoj Y predstavlja -CH2-.
3. Spoj prema patentnom zahtjevu 1 Formule (Ii) u kojoj je Ar fenil supstituiran sa 0-5 R3.
4. Spoj prema patentnom zahtjevu 1 Formule (Ii) u kojoj je Ar u orto položaju u odnosu na supstituent -C(R4)(R5)- na jezgru fenil prstena.
5. Spoj prema patentnom zahtjevu 1 Formule (Ib):
[image]
njegovi stereoizomerni oblici, smjese stereoizomernih oblika ili farmaceutski prihvatljivi oblici soli.
6. Spoj prema patentnom zahtjevu 1 formule (le):
[image]
njegovi stereoizomerni oblici, smjese stereoizomernih oblika ili farmaceutski prihvatljivi oblici soli,
pri čemu:
Ar je C6-C10 aril grupa supstituirana sa 0-5 R3;
C5-C10 cikloalkenil supstituiran 0-5 R3; ili
5 do 14 člana heteroaril grupa supstituirana sa 0-5R3, gdje spomenuta heteroaril grupa sadrži jedan, dva ili tri heteroatoma odabrana od N, O, S ili Se;
R2 je odabran od H, F, Cl, Br, J, OR16, NR17R18, NHOH, NO2, CN, CF3, C1-C6 alkil, C2-C6 alkenil, C2-C6alkinil, C(=O)R16, C(=O)OR16, OC(=O)R16, C(=O)NR17R18, NHC(=O)R16, NHCO2R16, OC(=O)NR17R18, NHC(=S)R16, SR16; S(=O)R16; i S(=O)2R16;
alternativno, dvije R2 grupe se mogu kombinirati da formiraju metilendioksi grupu, etilendioksi grupu ili propilendioksi grupu;
R3 je odabran od H, F, Cl, Br, J, O R16, OCF3, NR17R18, NHOH, NO2, CN, CF3, CH2OR16, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C7 cikloalkil, 3-7 člani heterocikloalkil, fenil, 5 ili 6 člani heteroaril, C7-C10 arilalkil, C(=O)R16, C(=O)OR16, OC(=O)R16, C(=O) NR17R18, NHC(=O)R16, NHCO2R16, OC(=O)NR17R18, NHC(= S)R16, SR16; S(=O)R16; S(=O)2R16, i NHS(=O)2R16;
alternativno, dvije R3 grupe se mogu kombinirati da formiraju metilendioksi grupu, etilendioksi grupu ili propilendioksi grupu;
R12 i R13 u svakom pojavljivanju su svaki nezavisno odabrani od H, C1-C6alkila supstituiranog sa 0-3 R20 i C6-C10arila, supstituiranog sa 0-3 R20;
alternativno, R12 i R13, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten supstituiran sa 0-3 R20;
R16 je u svakom pojavljivanju nezavisno odabran od H, C1-C6 alkil, i C6-C10 aril;
R17 i R18 su u svakom pojavljivanju svaki nezavisno odabrani od H, C1-C6 alkil, i C6-C10 aril, ili alternativno, R17 i R18, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten, pri čemu je spomenuti 3-7 člani heterociklični prsten supstituiran sa 0-2 okso grupe;
R20 je u svakom pojavljivanju nezavisno odabran od F, Cl, Br, J, OH, OR22, NR23R24, NHOH, NO2, CN, CF3, C1-C6 alkil, C1-C6alkil-OH, C2-C6alkenil, C2-C6alkinil, C3-C7cikloalkil, 3-7 člani heterocikloalkil, fenil supstituiran sa 0-1 R26; 5 ili 6 člani heteroaril, C7-C10 arilalkil, =O, C(=O)R22, C(=O)OR22, OC(=O)R22, C(=O)NR23R24, NHC(=O)R22, NHCO2R22, OC(=O)NR23R24, NHC(=S)R22, SR22; S(=O)R22; i S(=O)2R22;
R22 je u svakom pojavljivanju nezavisno odabran od H, C1-C4 alkil, C1-C4 alkil-OH, i C6-C10 aril;
R23 i R24 u svakom pojavljivanju su svaki nezavisno odabrani od H, C1-C4 alkil, i C6-C10 aril, ili alternativno, R23 i R24, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten;
R26 je u svakom pojavljivanju nezavisno odabran od H, F, Cl, Br, C1-C4 alkil i C1-C4 alkoksi; i
x je 0, 1, 2, 3, ili 4;
pod uvjetom da
(i) kada je Ar fenil supstituiran sa 0-2 R3, i R3 je H, F, Cl, Br, J, CH3, OCH3, SCH3, CN, NO2 ili metilendioksifenil; onda je Ar u orto ili meta položaju u odnosu na supstituent -CH2S(=O)-CH2C(=O)NR12R13 na jezgru fenil prstena;
(ii) kada je Ar imidazopiridin supstituiran sa 0-5R3, Ar je u orto ili meta položaju u odnosu na -CH2S(=O)-CH2C(=O)NR12R13 supstituent na jezgru fenil prstena; i
(iii) kada je Ar u meta položaju u odnosu na -CH2S(=O)-CH2C(=O)NR12R13 supstituent na jezgru fenil prstena i Ar je heteroaril grupa vezana za fenil prsten preko atoma dušika onda je Ar pirolil, indolil, imidazolil, benzimidazolil, benzotriazolil, triazolil, ili 1,3-dihidroizoindolil.
7. Spoj prema patentnom zahtjevu 6 gdje je Ar fenil supstituiran sa 0-5 R3, pri čemu je navedena Ar grupa u orto ili meta položaju u odnosu na -CH2S(=O)-CH2C(=O)NR12R13 supstituent na jezgru fenil prstena.
8. Spoj prema Zahtjevu 6 gdje Ar predstavlja C5-C10 cikloalkenil supstituiran 0-5 R3; pri čemu je navedena Ar grupa u orto ili meta položaju u odnosu na -CH2S(=O)-CH2C(=O)NR12R13 supstituent na jezgru fenil prstena.
9. Spoj prema patentnom zahtjevu 6, naznačeno time što Ar je 5 do 14 člana heteroaril grupa supstituirana sa 0-5 R3, pri čemu spomenuta heteroaril grupa sadrži jedan, dva ili tri heteroatoma izabrana od N, O, S ili Se; pri čemu je spomenuta 5 do 14 člana heteroaril grupa odabrana od fenoksatiinil, kinolinil, izoksazolil, tienil, benzotienil, (1,1-diokso)-benzotienil, indolil, furil, benzofuril, piridil, seleninil, 1,3-dihidroizoindolil, pirolil, i 2-benzo[1,4]dioksin; pri čemu je navedena Ar grupa u orto ili meta položaju u odnosu na -CH2S(=O)-CH2C(=O)NR12R13 supstituent na jezgru fenil prstena.
10. Spoj prema patentnom zahtjevu 6 Formule (If):
[image]
njegovi stereoizomerni oblici, smjese stereoizomernih oblika ili farmaceutski prihvatljivi oblici soli.
11. Spoj prema patentnom zahtjevu 6 Formule (Ig):
[image]
njegovi stereoizomerni oblici, smjese stereoizomernih oblika ili farmaceutski prihvatljivi oblici soli.
12. Spoj prema patentnom zahtjevu 6 Formule (Ih):
[image]
njegovi stereoizomerni oblici, smjese stereoizomernih oblika ili farmaceutski prihvatljivi oblici soli.
13. Spoj prema patentnom zahtjevu 6 Formule (le) gdje je Ar fenil supstituiran sa 0-5 R3, pri čemu je navedena Ar grupa u orto položaju u odnosu na supstituent -CH2S(=O)-CH2C(=O)NR12R13 na jezgru fenil prstena.
14. Spoj prema patentnom zahtjevu 1 Formule (Iii):
[image]
njegovi stereoizomerni oblici, smjese stereoizomernih oblika ili farmaceutski prihvatljivi oblici soli,
pri čemu:
Ar je C6- C10 aril supstituiran sa 0-5 R3;
C5-C10 cikloalkenil supstituiran 0-5 R3; ili
5 do 10 člana heteroaril grupa supstituirana sa 0-5 R3, pri čemu spomenuta heteroaril grupa sadrži jedan, dva ili tri heteroatoma izabrana od N, O ili S;
pri čemu je spomenuta 5 do 10 člana heteroaril grupa odabrana od sljedećeg kinolinil, izoksazolil, tienil, benzotienil, (1,1-diokso)-benzotienil, indolil, furil, benzofuril, piridil, seleninil, 1,3-dihidro-izoindolil, pirolil i 2-benzo[1,4]dioksin;
Y je -CH2-, -CH(OCH3)-, ili -CH2CH2-;
R1 je C(=O)NR12R13;
R2 je odabran od sljedećeg H, F, Cl, Br, C1-C4 alkoksi, CN, CF3, C1-C4 alkil;
alternativno, dvije R2 grupe se mogu kombinirati da formiraju metilendioksi grupu, etilendioksi grupu, ili propilendioksi grupu;
R3 je odabran od sljedećeg H, F, Cl, Br, OR16, OCF3, NR17R18, NHOH, NO2, CN, CF3, CH2OR16, C1-C6 alkil, C2-C6alkenil, C2-C6alkinil, C3-C7cikloalkil, 3-7 člani hetero-cikloalkil, fenil, 5 ili 6 člani heteroaril, C7-C10 arilalkil, C(=O)R16, C(=O)OR16, OC(=O) R16, C(=O)NR17R18, NHC(=O)R16, NHCO2R16, OC(=O)NR17R18, NHC(=S)R16, SR16; S(=O)R16; S(=O)2R16, i NHS(=O)2R16;
alternativno, dvije R3 grupe se mogu kombinirati da formiraju metilendioksi grupu, etilendioksi grupu ili propilendioksi grupu;
R4 i R5 su H;
R12 i R13 u svakom pojavljivanju su svaki nezavisno odabrani od H, C1-C6 alkila supstituiranog sa 0-3 R20 i C6-C10 arila, supstituiranog sa 0-3 R20;
alternativno, R12 i R13, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten supstituiran sa 0-3 R20;
R16 je u svakom pojavljivanju nezavisno odabran od: H, C1-C6 alkil, i C6-C10 aril;
R17 i R18 u svakom pojavljivanju su svaki nezavisno odabrani od H, C1-C6 alkil, i C6-C10 aril, ili alternativno, R17 i R18, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten, pri čemu je spomenuti 3-7 člani heterociklični prsten supstituiran sa 0-2 okso grupe;
R20 je u svakom pojavljivanju nezavisno odabran od F, Cl, Br, OH, OR22, NR23R24, NHOH, NO2, CN, CF3, C1-C6 alkil, C1-C6 alkil-OH, C2-C6 alkenil, C2-C6 alkinil, C3-C7 cikloalkil, 3-7 člani heterocikloalkil, fenil supstituiran sa 0-1 R26; 5 ili 6 člani heteroaril, C7-C10 arilalkil, =O, C(=O)R22, C(=O)OR22, OC(=O)R22, C(=O)NR23R24, NHC(=O)R22, NHCO2R22 , OC(=O)NR23R24, NHC(=S)R22, SR22; S(=O)R22; i S(=O)2R22;
R22 je u svakom pojavljivanju nezavisno odabran od H, C1-C6 alkil, C1-C6 alkil-OH, i C6-C10 aril;
R23 i R24 u svakom pojavljivanju su svaki nezavisno odabrani od H, C1-C6 alkil, i C6-C10 aril, ili alternativno, R23 i R24, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten;
R26 je u svakom pojavljivanju nezavisno odabran od H, F, C1-C6 alkil i C1-C6 alkoksi; i x je 0, 1, 2, 3 ili 4;
pod uvjetom da
(i) kada Y predstavlja -CH2-; Ar je fenil supstituiran sa 0-2 R3, i R3 je H, F, Cl, Br, J, CH3, OCH3, SCH3, CN, NO2 ili metilendioksifenil; onda je Ar u orto ili meta položaju u odnosu na -C(R4)(R5)- supstituent na jezgru fenil prstena; i
(iii) kada je Ar u meta položaju u odnosu na -C(R4)(R5)- supstituent na jezgru fenil prstena i Ar je heteroaril grupa vezana za fenil prsten preko atoma dušika, onda Ar predstavlja pirolil, indolil, imidazolil, benzimidazolil, benzotriazolil, triazolil, ili 1,3-dihidroizoindolil.
15. Spoj prema patentnom zahtjevu 14 Formule (Iii) u kojoj R1 je C(=O)NH2.
16. Spoj prema patentnom zahtjevu 14, pri čemu:
Ar grupa je u orto položaju u odnosu na -C(R4)(R5)- supstituent na jezgru fenil prstena;
Ar je C6-C10 aril grupa supstituirana sa 0-5 R3;
C5-C10 cikloalkenil supstituiran sa 0-5 R3; ili
5 do 10 člana heteroaril grupa supstituirana sa 0-5 R3, pri čemu je navedena aril, cikloalkenil, ili heteroaril grupa izabrana od sljedećeg: fenil, ciklopentenil, cikloheksenil, cikloheptenil, naftil, kinolinil, izoksazolil, tienil, benzotienil, (1,1-diokso)-benzotienil, indolil, furil, benzofuril, piridil, seleninil, 1,3-dihidro-izoindolil ili 2-benzo [1,4] dioksin; ili
njihovi farmaceutski prihvatljivi oblici soli.
17. Spoj prema patentnom zahtjevu 16 Formule (Iii) u kojoj Ar je fenil supstituiran sa 0-5 R3.
18. Spoj prema patentnom zahtjevu 16 Formule (Iii) u kojoj Ar je fenil supstituiran sa 0-3 R3; i R3 je odabran od F, Cl, i Br.
19. Spoj prema patentnom zahtjevu 16 formule (Iii) pri čemu; Ar je fenil supstituiran sa 0-3 R3; R3 je odabran od F, Cl, i Br; a R1 je C(=O)NH2.
20. Spoj prema patentnom zahtjevu 14, pri čemu:
Ar grupa je u meta položaju u odnosu na -C(R4)(R5)- supstituent na jezgru fenil prstena;
Ar je C6-C10 aril grupa supstituirana sa 0-5 R3;
C5-C10 cikloalkenil supstituiran 0-5 R3; ili
5 do 10 člani heteroaril grupa supstituirana sa 0-5 R3, pri čemu je navedena aril, cikloalkenil, i heteroaril grupa izabrana od sljedećeg: fenil, ciklopentenil, cikloheksenil, cikloheptenil, naftil, kinolinil, izoksazolil, tienil, benzotienil, (1,1-diokso)-benzotienil, indolil, furil, benzofuril, piridil, seleninil, 1,3-dihidro- izoindolil, pirolil ili 2-benzo[1,4] dioksin; ili
njihovi farmaceutski prihvatljivi oblici soli.
21. Spoj prema patentnom zahtjevu 20 formule (Iii) gdje je Ar fenil supstituiran sa 0-5 R3.
22. Spoj prema patentnom zahtjevu 20 formule (Iii) gdje je Ar fenil supstituiran sa 0-3 R3; a R3 je odabran od F, Cl, i Br.
23. Spoj prema patentnom zahtjevu 20 formule (Iii) gdje je Ar fenil supstituiran sa 0-3 R3; a R3 je odabran od F, Cl, i Br; i R1 je C (= O) NH2.
24. Spoj Formule (Iiii):
[image]
njegovi stereoizomerni oblici, smjese stereoizomernih oblika ili farmaceutski prihvatljivi oblici soli, gdje:
Ar je C6-C10 aril grupa supstituirana sa 0-3 R3;
C5-C10 cikloalkenil supstituiran 0-3 R3; ili
5 do 10 člana heteroaril grupa supstituirana sa 0-1 R3; pri čemu su spomenuti aril, cikloalkenil, ili heteroaril grupe odabrane od fenil, ciklopentenil, cikloheksenil, cikloheptenil, naftil, kinolinil, izoksazolil, tienil, benzotienil, (1,1-diokso)-benzotienil, indolil, furil, benzofuril, piridil, seleninil, 1,3-dihidro-izo indolil, pirolil i 2-benzo[1,4] dioksin grupe;
Y je -CH2-, -CH(OCH3)-, ili -CH2CH2-;
R1 je C(=O)NR12R13;
R2 je odabran od H, Cl, F, metoksi, etoksi, metil, etil, i-propil grupe;
alternativno, dvije R2 grupe se mogu kombinirati da formiraju metilendioksi grupu;
R3 je odabran od H, F, Cl, Br, CF3, cijano, OCF3, NO2, OH, fenil, ciklopropil, ciklobutil, ciklopentil, cikloheksil, metil, etil, propil, i-propil, n-butil, i-butil, s-butil, t-butil, CH2= CH2, morfolinil, OR16, NR17R18, CH200 R16, C(=O)R16, C(=O)OR16, C(=O)NR17R18, SR16; S(=O)R16; S(=O)2R16, i NHS(=O)2R16;
alternativno, dvije R3 grupe se mogu kombinirati da formiraju metilendioksi grupu, etilendioksi grupu ili propilendioksi grupu;
R4 je H;
R5 je H;
R12 i R13 u svakom pojavljivanju su svaki nezavisno odabrani od H i C1-C3 alkil supstituiranog sa 0-1 R20; pri čemu navedeni alkil je metil, etil, n-propil ili i-propil;
alternativno, R12 i R13, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten supstituiran sa 0-3 R20; pri čemu je spomenuti 3-7 člani heterociklični prsten odabran od sljedećeg: morfolinil, piperazinil, azetidinil, piperidinil, i pirolidinil;
R16 je u svakom pojavljivanju nezavisno izabran od H, metil, etil, propil, butil, i fenil;
R17 i R18 u svakom pojavljivanju su svaki nezavisno odabrani od H, metil, i etil; ili
alternativno, R17 i R18, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten odabran od sljedećeg: piperidinil, (4-okso)-piperidinil i morfolinil;
R20 je u svakom pojavljivanju nezavisno odabran od F, Cl, OH, CN, CF3, metil, etil, propil, i-propil, nbutil, i-butil, s-butil, t-butil, CH2CH2OH, ciklopropil, ciklobutil, ciklopentil, cikloheksil, piridil, i pirolidinil, OR22, NR23R24, C(=O)R22, C(=O)OR22, C(=O)NR23R24 i fenila supstituiranog sa 0-1 R26;
R22 je u svakom pojavljivanju nezavisno izabran od H, metil, etil, propil, butil, i CH2CH2OH;
R23 i R24 u svakom pojavljivanju su svaki nezavisno odabrani od H, metil, etil, propil, butil, i fenil;
R26je u svakom pojavljivanju nezavisno odabran od H, F, metil, etil, propil, metoksi, i etoksi; i
x je 0, 1 ili 2;
q je 1 ili 2;
pod uvjetom da
(i) kada Y predstavlja -CH2-, Ar je fenil supstituiran sa 0-2 R3, i R3 je H, F, Cl, Br, J, CH3, OCH3, SCH3, CN, NO2 ili metilendioksifenil; onda je Ar u orto ili meta položaju u odnosu na supstituent -C(R4)(R5)- na jezgru fenil prstena;
(ii) kada je Ar u meta položaju u odnosu na -C(R4)(R5)- supstituent na jezgru fenil prstena i Ar je heteroaril grupa vezana za fenil prsten preko atoma dušika, onda Ar je pirolil, indolil, imidazolil, benzimidazolil, benzotriazolil, triazolil, ili 1,3-dihidroizoindolil;
(iii) kada q je 2, onda je Ar u orto ili meta položaju u odnosu na supstituent -C(R4)(R5)- na jezgru fenil prstena; i
(iv) kada q je 2, Y je -CH2-, i Ar je 1, 2- (metilendioksi) fenil, onda je Ar u orto položaju u odnosu na -C(R4)(R5)- supstituent na jezgru fenil prstena; pri čemu se "aril" odnosi na supstituirane ili nesupstituirane, mono- ili biciklične ugljikovodične aromatične prstenske sisteme koji imaju 6 do 10 atoma ugljika; "heterociklični" se odnosi na supstituiranu ili nesupstituiranu karbocikličnu grupu u kojoj prstenski dio obuhvaća najmanje jedan do četiri heteroatoma, kao što su O, N ili S; i "cikloalkil" se odnosi na zasićeni ili djelomično zasićeni mono- ili biciklični alkil prstenski sistem koji sadrži 3 do 10 atoma ugljika.
25. Spoj prema patentnom zahtjevu 24 formule (Iiii) u kojoj q je 1.
26. Spoj prema patentnom zahtjevu 24, u kojem:
Ar grupa je u orto položaju u odnosu na -C(R4)(R5)- supstituent na jezgru fenil prstena;
Ar je C6-C10 aril grupa supstituirana sa 0-3 R3;
C5-C10 cikloalkenil supstituiran 0-3 R3; ili
5 do 10 člana heteroaril grupa ja supstituirana sa 0-1 R3; pri čemu je spomenuta aril, cikloalkenil, ili heteroaril grupa odabrana od fenil, ciklopentenil, cikloheksenil, cikloheptenil, naftil, kinolinil, izoksazolil, tienil, benzotienil, (1,1-diokso)-benzotienil, indolil, furil, benzofuril, piridil, seleninil, 1,3-dihidro-izoindolil, i 2-benzo [1,4] dioksin; ili
njihovi farmaceutski prihvatljivi oblici soli.
27. Spoj prema patentnom zahtjevu 26 Formule (Iiii) u kojoj q je 1.
28. Spoj prema patentnom zahtjevu 26 Formule (Iiii) u kojoj q je 1; i Ar je fenil supstituiran sa 0-3 R3.
29. Spoj prema patentnom zahtjevu 26 formule (Iiii) u kojoj q je 1; Y je -CH2-; Ar je fenil supstituiran sa 0-3 R3; i R3 je odabran od F, Cl, i Br.
30. Spoj prema patentnom zahtjevu 24, naznačeno time:
Ar grupa je u meta položaju u odnosu na -C(R4)(R5)- supstituent na jezgru fenil prstena;
Ar je C6-C10 aril grupa supstituirana sa 0-3 R3;
C5-C10 cikloalkenil supstituiran sa 0-3 R3; ili
5 do 10 člana heteroaril grupa supstituirana sa 0-1 R3; pri čemu je spomenuta aril, cikloalkenil, ili heteroaril grupa odabrana od fenil, ciklopentenil, cikloheksenil, cikloheptenil, naftil, kinolinil, izoksazolil, tienil, benzotienil, (1,1-diokso)-benzotienil, indolil, furil, benzofuril, piridil, seleninil, 1,3-dihidro-izoindolil, pirolil i 2-benzo [1,4] dioksin; ili
njihovi farmaceutski prihvatljivi oblici soli.
31. Spoj prema patentnom zahtjevu 30 Formule (Iiii) u kojoj q je 1.
32. Spoj prema patentnom zahtjevu 30 Formule (Iiii) u kojoj q je 1; i Ar je fenil supstituiran sa 0-3 R3.
33. Spoj prema patentnom zahtjevu 30 Formule (Iiii) u kojoj q je 1; Y je -CH2-; Ar je fenil supstituiran sa 0-3 R3; a R3 je odabran od F, Cl, i Br.
34. Spoj odabran od:
TABELA 1
[image]
[image]
[image]
TABELA 2
____________________________________________________________________
[image]
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[image]
TABELA 3
[image]
TABELA 4
[image]
TABELA 5
[image]
TABELA 6
[image]
TABELA 7
[image]
Ar Ar Položaj q R
177 Pirol-1-il orto 1 CH2CO-N-pirolidinil
178 Pirol-1-il orto 1 CH2CONMe2
179 Pirol-1-il orto 1 CH2CONHCHMe2
180 Pirol-1-il orto 1 CH2CO-1-(4-acetil)-piperazinil
181 Pirol-1-il meta 1 CH2CONHCH2CN
182 Pirol-1-il meta 1 CH2CONHCHMe2
183 Pirol-1-il meta 1 CH2CONMe2
TABELA 8
[image]
Ar Ar Položaj q R
184 2-Benzofuril orto 1 CH2CON(CH3)2
185 2-Benzofuril orto 1 CH2ONHCH(CH3)2
TABELA 9
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TABELA 10
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TABELA 11
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TABELA 12
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TABELA 13
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TABELA 14
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TABELA 14A
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TABELA 15
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TABELA 15A
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TABELA 16
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q Supstitucija
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TABELA 16A
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TABELA 17
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ili njihove farmaceutski prihvatljive soli.
35. Spoj odabran od:
TABELA 2-nastavak
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TABELA 18
[image]
ili njihove farmaceutski prihvatljive soli.
36. Farmaceutski sastav koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1-35 i jedan ili više farmaceutski prihvatljivih ekscipijenata.
37. Spoj prema bilo kojem od patentnih zahtjeva 1 do 35, za upotrebu u terapiji.
38. Upotreba spoja Formule (Iiv), stereoizomernog oblika spoja formule (Iiv), smjese stereoizomernih oblika spoja formule (Iiv) ili farmaceutski prihvatljive soli spoja Formule (Iiv) za proizvodnju lijeka za liječenje pospanosti povezane sa narkolepsijom, opstruktivne apneje u snu, ili poremećaja uslijed smjenskog rada; Parkinsonove bolesti; Alzhheimerove bolesti; poremećaja nedostatka pažnje; poremećaja pažnje sa hiperaktivnošću; depresije; ili zamora:
[image]
gdje:
Ar predstavlja C6-C10 aril supstituiran sa 0-5 R3;
C5-C10 cikloalkenil supstituiran 0-5 R3; ili
5 do 14 članu heteroaril grupu supstituiranu sa 0-5 R3, pri čemu spomenuta heteroaril grupa sadrži jedan, dva ili tri heteroatoma odabrana od N, O, S ili Se;
Y je -CH2-, -CH(OCH3)-, ili -CH2CH2-;
R1 je odabran od H, C(=O)NR12R13, i C(=O)OR11;
R2 je odabran od H, F, Cl, Br, J, OR16, OR25, NR17R18, NHOH, NO2, CN, CF3, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C(=O)R16, C(=O)OR16, OC(=O)R16, C(=O)NR17R18, NR15C(=O)R16, NR15CO2R16, OC(=O)NR17R18, NR15C(=S)R16, SR16; S(=O)R16; i S(=O)2R16;
alternativno, dvije R2 grupe se mogu kombinirati da formiraju metilendioksi grupu, etilendioksi grupu ili propilendioksi grupu;
R3 je odabran od H, F, Cl, Br, J, OR16, OCF3, OR25, NR17R18, NHOH, NO2, CN, CF3, CH2OR16, C1-C6alkil, C2-C6alkenil, C2-C6alkinil, C3-C7cikloalkil, 3-7 člani heterocikloalkil, fenil, 5 ili 6 člani heteroaril, C7-C10 arilalkil, C(=O)R16, C(=O)OR16, OC (=O)R16, C(=O)NR17R18, NR15C(=O)R16, NR15CO2R16, OC(=O)NR17R18, NR15, C(=S)R16, SR16; S(=O)R16; S(=O)2R16, i NR15S(=O)2R16;
alternativno, dvije R3 grupe se mogu kombinirati da formiraju metilendioksi grupu, etilendioksi grupu ili propilendioksi grupu;
R4 i R5 su H;
R11 je H;
R12 i R13 su u svakom pojavljivanju svaki nezavisno odabrani od H, C1-C6 alkila supstituiranog sa 0-3 R20; i C6-C10 arila, supstituiranog sa 0-3 R20;
alternativno, R12 i R13, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten supstituiran sa 0-3 R20;
R15 je u svakom pojavljivanju nezavisno odabran od H i C1-C6alkil;
R16 je u svakom pojavljivanju nezavisno odabran od H, C1-C6 alkil, i C6-C10 aril;
R17 i R18 u svakom pojavljivanju su svaki nezavisno odabrani od H, C1-C6 alkil, i C6-C10 aril, ili
alternativno, R17 i R18, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten, pri čemu je spomenuti 3-7 člani heterociklični prsten supstituiran sa 0-2 okso grupe;
R20 je u svakom pojavljivanju nezavisno odabran od F, Cl, Br, J, OH, OR22, OR25, NR23R24, NHOH, NO2, CN, CF3, C1-C6 alkil, C1-C6 alkil-OH, C2-C6alkenil, C2C6 alkinil, C3-C7 cikloalkil, 3-7 člani heterocikloalkil, fenil supstituiran sa 0-1 R26; 5 ili 6 člani heteroaril, C7-C10 arilalkil, =O, C(=O)R22, C(=O)OR22, OC(=O)R22, C(=O)NR23R24, NR21C(=O)R22, NR21CO2R22, OC(=O)NR23R24, NR21C(=S)R22, SR22; S(=O)R22; i S(=O)2R22;
R21 je u svakom pojavljivanju nezavisno odabran od H i C1-C6 alkil;
R22 je u svakom pojavljivanju nezavisno odabran od H, C1-C6 alkil, C1-C6 alkil-OH, i C6-C10 aril;
R23 i R24 su u svakom pojavljivanju svaki nezavisno odabrani od H, C1-C6 alkil, i C6-C10 aril, ili
alternativno, R23 i R24, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten;
R25 je u svakom pojavljivanju nezavisno aminokiselinski ostatak nakon uklanjanja hidroksilne grupe iz karboksilne grupe, sa formulom -C(=O)CH(NH2)-(bočni lanac), pri čemu je bočni lanac izabran od:
H CH3 CH(CH3)2
CH2CH(CH3)2 CH(CH3)CH2CH3 CH2OH
CH2SH CH(OH)CH3 CH2CH2SCH3
CH2C6H5 (CH2)4NH2 (CH2)3NHC(=NH)NH2
CH2COOH CH2CH2COOH CH2CONH2
CH2CH2CONH2 CH2CH3 CH2CH2CH3
CH2CH2CH2CH3 CH2CH2SH CH2CH2OH
CH2CH2SCH3 (CH2)3NH2 (CH2)2CH(OH)CH2NH2
(CH2)3NHC(=O)NH2 (CH2)2ONHC(=NH)NH2 CH2C(=O)NHCH2COOH
[image]
[image]
[image]
i
R26 je u svakom pojavljivanju nezavisno izabran od H, F, Cl, Br, C1-C6 alkil i C1-C6 alkoksi;
m je 0 ili 1;
n je 0 ili 1;
x je 0, 1,2, 3 ili 4; i
q je 0, 1 ili 2,
pri čemu se "aril" odnosi na supstituirani ili nesupstituirani, mono- ili biciklični ugljikovodični aromatični prstenski sistem koji ima 6 do 10 atoma ugljika u prstenu; "heterociklični" se odnosi na supstituiranu ili nesupstituiranu karbocikličnu grupu u kojoj prsten uključuje najmanje jedan do četiri heteroatoma poput O, N ili S; i "cikloalkil" se odnosi na zasićeni ili djelomično zasićeni mono- ili biciklični alkil prstenski sistem koji sadrži 3 do 10 atoma ugljika.
39. Upotreba prema zahtjevu 38, za liječenje pospanosti povezane sa narkolepsijom.
40. Upotreba spoja prema jednom od patentnih zahtjeva 1-35 za proizvodnju lijeka za liječenje pospanosti povezane sa narkolepsijom, opstruktivnom apnejom u snu, ili poremećajem uslijed rada u smjenama.
41. Upotreba spoja prema jednom od patentnih zahtjeva 1-35 za proizvodnju lijeka za liječenje Parkinsonove bolesti; Alzheimerove bolesti; poremećaja nedostatka pažnje; poremećaja pažnje sa hiperaktivnošću; depresije; ili zamora povezanog sa neurološkom bolešću ili poremećajem.
42. Spoj Formule (Iiv), stereoizomerni oblik spoja Formule (Iiv), smjesa stereoizomernih oblika spoja Formule (Iiv) ili farmaceutski prihvatljiva sol spoja Formule (Iiv) za upotrebu u liječenju pospanosti povezane sa narkolepsijom, opstruktivnom apnejom u snu, ili poremećaja uslijed smjenskog rada; Parkinsonove bolesti; Alzheimerove bolesti; poremećaja nedostatka pažnje; poremećaja pažnje sa hiperaktivnošću; depresije; ili zamora:
[image]
gdje:
Ar predstavlja C6-C10 aril grupu supstituiranu sa 0-5 R3;
C5-C10 cikloalkenil supstituiran 0-5 R3; ili
5 do 14 članu heteroaril grupu supstituiranu sa 0-5 R3, gdje spomenuta heteroaril grupa sadrži jedan, dva ili tri heteroatoma odabrana od N, O, S ili Se;
Y je -CH2-, -CH(OCH3)-, ili -CH2CH2-;
R1 je odabran od H, C(=O)NR12R13, i C(=O)OR11;
R2 je odabran od H, F, Cl, Br, J, OR16, OR25, NR17R18, NHOH, NO2, CN, CF3, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C(=O)R16, C(=O)OR16, OC(=O)R16, C(=O)NR17R18, NR15C(=O)R16, NR15CO2 R16, OC(=O)NR17R18, NR15C(=S)R16, SR16 ; S(=O)R16; i S(=O)2R16;
alternativno, dvije R2 grupe se mogu kombinirati da formiraju metilendioksi grupu, etilendioksi grupu ili propilendioksi grupu;
R3 je odabran od H, F, Cl, Br, J, O R16, OCF3, OR25, NR17R18, NHOH, NO2, CN, CF3, CH2O R16, C1-C6 alkil, C2-C6 alkenil, C2-C6 alkinil, C3-C7 cikloalkil, 3-7 člani heterocikloalkil, fenil, 5 ili 6 člani heteroaril, C7-C10 arilalkil, C(=O)R16, C(=O)OR16, OC(=O)R16, C(=O)NR17R18, NR15C(=O)R16, NR15CO2R16, OC(=O)NR17R18, NR15C(=S)R16, SR16; S(=O)R16; S(=O)2R16, i NR15S (O)2R16; alternativno, dvije R3 grupe se mogu kombinirati da formiraju metilendioksi grupu, etilendioksi grupu ili grupu propilendioksi;
R4 i R5 su H;
R11 je H;
R12 i R13 su u svakom pojavljivanju svaki nezavisno odabrani od H, C1-C6 alkila supstituiranog sa 0-3 R20; i C6-C10 arila, supstituiranog sa 0-3 R20;
alternativno, R12 i R13, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten supstituiran sa 0-3 R20;
R15 je u svakom pojavljivanju nezavisno odabran od H i C1-C6 alkil;
R16 je u svakom pojavljivanju nezavisno odabran od H, C1-C6 alkil, i C6-C10 aril;
R17 i R18u svakom pojavljivanju su svaki nezavisno odabrani od H, C1-C6 alkil, i C6-C10 aril, ili
alternativno, R17 i R18, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten, pri čemu je spomenuti 3-7 člani heterociklični prsten supstituiran sa 0-2 okso grupe;
R20 je u svakom pojavljivanju nezavisno odabran od F, Cl, Br, J, OH, OR22, OR25, NR23R24, NHOH, NO2, CN, CF3, C1-C6alkil, C1-C6alkil-OH, C2-C6alkenil, C2-C6alkinil, C3-C7cikloalkil, 3-7 člani heterocikloalkil, fenil supstituiran sa 0-1 R26; 5 ili 6 člani heteroaril, C7-C10 arilalkil, = O, C(=O)R22, C(=O)OR22, OC(=O)R22, C=O)NR23R24, NR21C(=O)R22, NR21CO2R22, OC(=O) NR23R24, NR21C(=S)R22, SR22; S(=O)R22; i S(=O)2R22;
R21 je u svakom pojavljivanju nezavisno odabran od H i C1-C6 alkil;
R22 je u svakom pojavljivanju nezavisno odabran od H, C1-C6 alkil, C1-C6 alkil-OH, i C6-C10 aril;
R23 i R24 u svakom pojavljivanju su svaki nezavisno odabrani od H, C1-C6 alkil, i C6-C10 aril, ili alternativno, R23 i R24, zajedno sa dušikom za koji su vezani, formiraju 3-7 člani heterociklični prsten;
R25 je u svakom pojavljivanju nezavisno aminokiselinski ostatak, nakon uklanjanja hidroksilne grupe iz karboksilne grupe, sa formulom -C(=O)CH(NH2)-(bočni lanac), pri čemu je bočni lanac odabran od:
H CH3 CH(CH3)2
CH2CH(CH3)2 CH(CH3)CH2CH3 CH2OH
CH2SH CH(OH)CH3 CH2CH2SCH3
CH2C6H5 (CH2)4NH2 (CH2)3NHC(=NH)NH2
CH2COOH CH2CH2COOH CH2CONH2
CH2CH2CONH2 CH2cH3 CH2CH2CH3
CH2CH2CH2CH3 CH2CH2SH CH2CH2OH
CH2CH2SCH3 (CH2)3NH2 (CH2)2CH(OH)CH2NH2
(CH2)3NHC(=O)NH2 (CH2)2ONHC(=NH)NH2 CH2C(=O)NHCH2COOH
[image]
[image]
[image]
R26 je u svakom pojavljivanju nezavisno odabran od H, F, Cl, Br, C1-C6 alkil i C1-C6 alkoksi;
m je 0 ili 1;
n je 0 ili 1;
x je 0, 1, 2, 3, ili 4; i
q je 0, 1 ili 2,
pri čemu se "aril" odnosi na supstituirani ili nesupstituirani, mono- ili biciklični ugljikovodični aromatični prstenski sistem koji ima 6 do 10 atoma ugljika; "Heterociklični" se odnosi na supstituiranu ili nesupstituiranu karbocikličnu grupu u kojoj prstenski dio obuhvaća najmanje jedan do četiri heteroatoma, kao što su O, N ili S; a "cikloalkil" se odnosi na zasićeni ili djelomično zasićeni mono- ili biciklični alkil prstenski sistem koji sadrži 3 do 10 atoma ugljika.
43. Spoj za upotrebu prema patentnom zahtjevu 42, za liječenje pospanosti povezane sa narkolepsijom.
44. Spoj prema jednom od patentnih zahtjeva 1-35 za upotrebu u liječenju pospanosti povezane sa narkolepsijom, opstruktivnom apnejom u snu, ili poremećajem uslijed smjenskog rada.
45. Spoj prema jednom od patentnih zahtjeva 1-35 za upotrebu u liječenju Parkinsonove bolesti; Alzheimerove bolesti; poremećaja nedostatka pažnje; poremećaja pažnje sa hiperaktivnošću; depresije; ili zamora udruženog sa neurološkim oboljenjem ili poremećajem.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04290982A EP1586559A1 (en) | 2004-04-13 | 2004-04-13 | Biaryl-methanethio-, -sulphinyl- and sulphonyl derivatives |
| US56915304P | 2004-05-07 | 2004-05-07 | |
| US11/104,091 US7449481B2 (en) | 2004-04-13 | 2005-04-12 | Thio-substituted biaryl-methanesulfinyl derivatives |
| PCT/US2005/012836 WO2005100308A1 (en) | 2004-04-13 | 2005-04-13 | Thio-substituted biaryl-methanesulfinyl derivatives |
| EP05735327.8A EP1737815B1 (en) | 2004-04-13 | 2005-04-13 | Thio-substituted biaryl-methanesulfinyl derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20170441T1 true HRP20170441T1 (hr) | 2017-05-19 |
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ID=34965682
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20170441TT HRP20170441T1 (hr) | 2004-04-13 | 2017-03-20 | Tio-supstituirani derivati biaril-metansulfinila |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US7449481B2 (hr) |
| EP (1) | EP1737815B1 (hr) |
| JP (1) | JP4859828B2 (hr) |
| AU (1) | AU2005233195B2 (hr) |
| CA (1) | CA2561897C (hr) |
| CY (1) | CY1118870T1 (hr) |
| DK (1) | DK1737815T3 (hr) |
| ES (1) | ES2619844T3 (hr) |
| HK (1) | HK1095808A1 (hr) |
| HR (1) | HRP20170441T1 (hr) |
| HU (1) | HUE031853T2 (hr) |
| LT (1) | LT1737815T (hr) |
| MX (1) | MXPA06011836A (hr) |
| NZ (1) | NZ550555A (hr) |
| PL (1) | PL1737815T3 (hr) |
| PT (1) | PT1737815T (hr) |
| RS (1) | RS55795B1 (hr) |
| WO (1) | WO2005100308A1 (hr) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7314875B2 (en) * | 2004-04-13 | 2008-01-01 | Cephalon, Inc. | Tricyclic aromatic and bis-phenyl sulfinyl derivatives |
| US7449481B2 (en) * | 2004-04-13 | 2008-11-11 | Cephalon, Inc. | Thio-substituted biaryl-methanesulfinyl derivatives |
| US7297817B2 (en) | 2004-04-13 | 2007-11-20 | Cephalon France | Thio-substituted arylmethanesulfinyl derivatives |
| EP1586560A1 (en) * | 2004-04-13 | 2005-10-19 | Cephalon, Inc. | Thio-substituted arylmethanesulfinyl derivatives |
| EP1702915A1 (en) * | 2005-03-14 | 2006-09-20 | Cephalon France | Process for enantioselective synthesis of single enantiomers of thio-substituted arylmethanesulfinyl derivatives by asymmetric oxidation |
| FR2936798B1 (fr) * | 2008-10-03 | 2012-09-28 | Novexel | Nouveaux composes heterocycliques azotes, leur preparation et leur utilisation comme medicaments antibacteriens. |
| FR2936951B1 (fr) * | 2008-10-10 | 2010-12-03 | Novexel | Nouvelles combinaisons de composes heterocycliques azotes antibacteriens avec d'autres composes antibacteriens et leur utilisation comme medicaments |
| FR2937034B1 (fr) * | 2008-10-10 | 2012-11-23 | Novexel | Nouveaux composes heterocycliques azotes, leur preparation et leur utilisation comme medicaments antibacteriens |
| WO2012040511A2 (en) * | 2010-09-22 | 2012-03-29 | Calcimedica, Inc. | Compounds that modulate intracellular calcium |
| EP2985279B1 (en) | 2014-08-13 | 2017-08-02 | Red Bull GmbH | Heterocyclic compounds with working memory enhancing activity |
| WO2016023997A1 (en) | 2014-08-13 | 2016-02-18 | Red Bull Gmbh | Heterocyclic compounds with working memory enhancing activity |
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-
2005
- 2005-04-12 US US11/104,091 patent/US7449481B2/en not_active Expired - Fee Related
- 2005-04-13 NZ NZ550555A patent/NZ550555A/en unknown
- 2005-04-13 PT PT57353278T patent/PT1737815T/pt unknown
- 2005-04-13 AU AU2005233195A patent/AU2005233195B2/en not_active Ceased
- 2005-04-13 HU HUE05735327A patent/HUE031853T2/en unknown
- 2005-04-13 RS RS20170296A patent/RS55795B1/sr unknown
- 2005-04-13 JP JP2007508562A patent/JP4859828B2/ja not_active Expired - Fee Related
- 2005-04-13 CA CA2561897A patent/CA2561897C/en not_active Expired - Fee Related
- 2005-04-13 WO PCT/US2005/012836 patent/WO2005100308A1/en active Application Filing
- 2005-04-13 ES ES05735327.8T patent/ES2619844T3/es active Active
- 2005-04-13 MX MXPA06011836A patent/MXPA06011836A/es active IP Right Grant
- 2005-04-13 LT LTEP05735327.8T patent/LT1737815T/lt unknown
- 2005-04-13 EP EP05735327.8A patent/EP1737815B1/en active Active
- 2005-04-13 PL PL05735327T patent/PL1737815T3/pl unknown
- 2005-04-13 DK DK05735327.8T patent/DK1737815T3/en active
-
2007
- 2007-03-22 HK HK07103066.6A patent/HK1095808A1/zh not_active IP Right Cessation
-
2008
- 2008-08-27 US US12/199,167 patent/US7981907B2/en not_active Expired - Fee Related
-
2017
- 2017-03-16 CY CY20171100334T patent/CY1118870T1/el unknown
- 2017-03-20 HR HRP20170441TT patent/HRP20170441T1/hr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2008505058A (ja) | 2008-02-21 |
| AU2005233195B2 (en) | 2012-04-19 |
| HUE031853T2 (en) | 2017-08-28 |
| EP1737815A1 (en) | 2007-01-03 |
| RS55795B1 (sr) | 2017-08-31 |
| US20050245747A1 (en) | 2005-11-03 |
| LT1737815T (lt) | 2017-04-25 |
| AU2005233195A1 (en) | 2005-10-27 |
| CA2561897C (en) | 2013-05-28 |
| WO2005100308A1 (en) | 2005-10-27 |
| US7981907B2 (en) | 2011-07-19 |
| MXPA06011836A (es) | 2007-05-04 |
| US7449481B2 (en) | 2008-11-11 |
| CA2561897A1 (en) | 2005-10-27 |
| EP1737815B1 (en) | 2016-12-21 |
| US20090062284A1 (en) | 2009-03-05 |
| NZ550555A (en) | 2010-10-29 |
| PL1737815T3 (pl) | 2017-06-30 |
| DK1737815T3 (en) | 2017-02-06 |
| PT1737815T (pt) | 2017-04-03 |
| ES2619844T3 (es) | 2017-06-27 |
| CY1118870T1 (el) | 2018-01-10 |
| HK1095808A1 (zh) | 2007-05-18 |
| JP4859828B2 (ja) | 2012-01-25 |
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