ZA200208226B - Aminopyridines and their use as anticonvulsants and sodium channel blockers. - Google Patents
Aminopyridines and their use as anticonvulsants and sodium channel blockers. Download PDFInfo
- Publication number
- ZA200208226B ZA200208226B ZA200208226A ZA200208226A ZA200208226B ZA 200208226 B ZA200208226 B ZA 200208226B ZA 200208226 A ZA200208226 A ZA 200208226A ZA 200208226 A ZA200208226 A ZA 200208226A ZA 200208226 B ZA200208226 B ZA 200208226B
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- South Africa
- Prior art keywords
- compound
- alkyl
- hydrogen
- treating
- amino
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- 150000003927 aminopyridines Chemical class 0.000 title description 8
- 229940125681 anticonvulsant agent Drugs 0.000 title description 7
- 239000001961 anticonvulsive agent Substances 0.000 title description 7
- 239000003195 sodium channel blocking agent Substances 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims description 36
- 125000000217 alkyl group Chemical group 0.000 claims description 26
- 229910052739 hydrogen Inorganic materials 0.000 claims description 25
- 239000001257 hydrogen Substances 0.000 claims description 25
- 208000002193 Pain Diseases 0.000 claims description 18
- 229910052799 carbon Inorganic materials 0.000 claims description 16
- 150000002431 hydrogen Chemical class 0.000 claims description 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 14
- 125000003118 aryl group Chemical group 0.000 claims description 13
- 125000003545 alkoxy group Chemical group 0.000 claims description 11
- 125000003342 alkenyl group Chemical group 0.000 claims description 10
- 125000004414 alkyl thio group Chemical group 0.000 claims description 10
- 125000000304 alkynyl group Chemical group 0.000 claims description 10
- 230000036407 pain Effects 0.000 claims description 10
- -1 ~~ - - cyano Chemical group 0.000 claims description 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 8
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims description 8
- 208000009205 Tinnitus Diseases 0.000 claims description 7
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 7
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 7
- 238000000034 method Methods 0.000 claims description 7
- 229940002612 prodrug Drugs 0.000 claims description 7
- 239000000651 prodrug Substances 0.000 claims description 7
- 150000003839 salts Chemical class 0.000 claims description 7
- 239000012453 solvate Substances 0.000 claims description 7
- 231100000886 tinnitus Toxicity 0.000 claims description 7
- 208000000094 Chronic Pain Diseases 0.000 claims description 6
- 241000124008 Mammalia Species 0.000 claims description 6
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims description 6
- 206010010904 Convulsion Diseases 0.000 claims description 5
- 108010052164 Sodium Channels Proteins 0.000 claims description 5
- 102000018674 Sodium Channels Human genes 0.000 claims description 5
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 claims description 5
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims description 5
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims description 5
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 5
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 5
- 125000001188 haloalkyl group Chemical group 0.000 claims description 5
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 5
- 208000028867 ischemia Diseases 0.000 claims description 5
- 125000005100 aryl amino carbonyl group Chemical group 0.000 claims description 4
- 125000004658 aryl carbonyl amino group Chemical group 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 208000004296 neuralgia Diseases 0.000 claims description 4
- 208000021722 neuropathic pain Diseases 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 208000020925 Bipolar disease Diseases 0.000 claims description 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 3
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 3
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims description 3
- 208000028683 bipolar I disease Diseases 0.000 claims description 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 3
- 125000004181 carboxyalkyl group Chemical group 0.000 claims description 3
- 230000036461 convulsion Effects 0.000 claims description 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 3
- 125000001153 fluoro group Chemical group F* 0.000 claims description 3
- 229910052736 halogen Inorganic materials 0.000 claims description 3
- 125000005843 halogen group Chemical group 0.000 claims description 3
- 150000002367 halogens Chemical class 0.000 claims description 3
- 230000000626 neurodegenerative effect Effects 0.000 claims description 3
- 125000003396 thiol group Chemical class [H]S* 0.000 claims description 3
- 125000004423 acyloxy group Chemical group 0.000 claims description 2
- 125000003282 alkyl amino group Chemical group 0.000 claims description 2
- 125000005125 aryl alkyl amino carbonyl group Chemical group 0.000 claims description 2
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 239000002287 radioligand Substances 0.000 claims description 2
- 241001465754 Metazoa Species 0.000 claims 5
- 238000004519 manufacturing process Methods 0.000 claims 3
- 206010003119 arrhythmia Diseases 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 238000002690 local anesthesia Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 101100478314 Caenorhabditis elegans sre-1 gene Proteins 0.000 claims 1
- 206010026749 Mania Diseases 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 108091006146 Channels Proteins 0.000 description 14
- 239000011734 sodium Substances 0.000 description 14
- 229960000623 carbamazepine Drugs 0.000 description 4
- FFGPTBGBLSHEPO-UHFFFAOYSA-N carbamazepine Chemical compound C1=CC2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 FFGPTBGBLSHEPO-UHFFFAOYSA-N 0.000 description 4
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 description 3
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 description 3
- 229960004194 lidocaine Drugs 0.000 description 3
- 208000032131 Diabetic Neuropathies Diseases 0.000 description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
- CXOFVDLJLONNDW-UHFFFAOYSA-N Phenytoin Chemical compound N1C(=O)NC(=O)C1(C=1C=CC=CC=1)C1=CC=CC=C1 CXOFVDLJLONNDW-UHFFFAOYSA-N 0.000 description 2
- FKNQFGJONOIPTF-UHFFFAOYSA-N Sodium cation Chemical compound [Na+] FKNQFGJONOIPTF-UHFFFAOYSA-N 0.000 description 2
- 230000009471 action Effects 0.000 description 2
- 230000001154 acute effect Effects 0.000 description 2
- 208000005298 acute pain Diseases 0.000 description 2
- 230000003288 anthiarrhythmic effect Effects 0.000 description 2
- 239000003416 antiarrhythmic agent Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 125000000623 heterocyclic group Chemical group 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- PYZRQGJRPPTADH-UHFFFAOYSA-N lamotrigine Chemical compound NC1=NC(N)=NN=C1C1=CC=CC(Cl)=C1Cl PYZRQGJRPPTADH-UHFFFAOYSA-N 0.000 description 2
- 229960001848 lamotrigine Drugs 0.000 description 2
- 239000003589 local anesthetic agent Substances 0.000 description 2
- 229960005015 local anesthetics Drugs 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 230000000324 neuroprotective effect Effects 0.000 description 2
- 239000002581 neurotoxin Substances 0.000 description 2
- 231100000618 neurotoxin Toxicity 0.000 description 2
- 229960002036 phenytoin Drugs 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- 229910052708 sodium Inorganic materials 0.000 description 2
- 229910001415 sodium ion Inorganic materials 0.000 description 2
- 210000004885 white matter Anatomy 0.000 description 2
- LEBVLXFERQHONN-UHFFFAOYSA-N 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide Chemical compound CCCCN1CCCCC1C(=O)NC1=C(C)C=CC=C1C LEBVLXFERQHONN-UHFFFAOYSA-N 0.000 description 1
- XZMCDFZZKTWFGF-UHFFFAOYSA-N Cyanamide Chemical compound NC#N XZMCDFZZKTWFGF-UHFFFAOYSA-N 0.000 description 1
- 206010021143 Hypoxia Diseases 0.000 description 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 1
- 208000019695 Migraine disease Diseases 0.000 description 1
- 208000028389 Nerve injury Diseases 0.000 description 1
- 101710138657 Neurotoxin Proteins 0.000 description 1
- FTALBRSUTCGOEG-UHFFFAOYSA-N Riluzole Chemical group C1=C(OC(F)(F)F)C=C2SC(N)=NC2=C1 FTALBRSUTCGOEG-UHFFFAOYSA-N 0.000 description 1
- 208000034189 Sclerosis Diseases 0.000 description 1
- PDOCBJADCWMDGL-UHFFFAOYSA-N Sipatrigine Chemical compound C1CN(C)CCN1C1=NC=C(C=2C(=C(Cl)C=C(Cl)C=2)Cl)C(N)=N1 PDOCBJADCWMDGL-UHFFFAOYSA-N 0.000 description 1
- 125000004442 acylamino group Chemical group 0.000 description 1
- 239000003282 amino acid receptor affecting agent Substances 0.000 description 1
- 229940035674 anesthetics Drugs 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 230000003561 anti-manic effect Effects 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 229960003150 bupivacaine Drugs 0.000 description 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 125000001309 chloro group Chemical group Cl* 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 231100000318 excitotoxic Toxicity 0.000 description 1
- 230000003492 excitotoxic effect Effects 0.000 description 1
- 239000003193 general anesthetic agent Substances 0.000 description 1
- 229930195712 glutamate Natural products 0.000 description 1
- 239000003825 glutamate receptor antagonist Substances 0.000 description 1
- 230000001146 hypoxic effect Effects 0.000 description 1
- 230000004941 influx Effects 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 230000002452 interceptive effect Effects 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- HTDFEXRUDGWNHA-UHFFFAOYSA-N lifarizine Chemical compound CC=1NC(C=2C=CC(C)=CC=2)=NC=1CN(CC1)CCN1C(C=1C=CC=CC=1)C1=CC=CC=C1 HTDFEXRUDGWNHA-UHFFFAOYSA-N 0.000 description 1
- 229950003413 lifarizine Drugs 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 206010027599 migraine Diseases 0.000 description 1
- 230000008764 nerve damage Effects 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 230000003961 neuronal insult Effects 0.000 description 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 1
- 230000008058 pain sensation Effects 0.000 description 1
- JWHAUXFOSRPERK-UHFFFAOYSA-N propafenone Chemical compound CCCNCC(O)COC1=CC=CC=C1C(=O)CCC1=CC=CC=C1 JWHAUXFOSRPERK-UHFFFAOYSA-N 0.000 description 1
- 229960000203 propafenone Drugs 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 229960004181 riluzole Drugs 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 230000008733 trauma Effects 0.000 description 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
- C07D213/60—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 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
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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- 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
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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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
- C07D213/26—Radicals substituted by halogen atoms or nitro radicals
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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
- C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
- C07D213/30—Oxygen atoms
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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
- C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/55—Acids; Esters
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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
- C07D213/60—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 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
- C07D213/61—Halogen atoms or nitro radicals
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- C—CHEMISTRY; METALLURGY
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- 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
- C07D213/60—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 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
- C07D213/62—Oxygen or sulfur atoms
- C07D213/70—Sulfur atoms
- C07D213/71—Sulfur atoms to which a second hetero atom is attached
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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
- C07D213/60—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 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
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Anesthesiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19344100P | 2000-03-31 | 2000-03-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200208226B true ZA200208226B (en) | 2003-10-13 |
Family
ID=22713650
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200208226A ZA200208226B (en) | 2000-03-31 | 2002-10-11 | Aminopyridines and their use as anticonvulsants and sodium channel blockers. |
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| US (1) | US6335354B2 (xx) |
| EP (1) | EP1268427A1 (xx) |
| JP (1) | JP2003529589A (xx) |
| KR (1) | KR20020084278A (xx) |
| CN (1) | CN1426397A (xx) |
| AU (2) | AU2001249610B2 (xx) |
| BR (1) | BR0109706A (xx) |
| CA (1) | CA2403991A1 (xx) |
| IL (1) | IL151952A0 (xx) |
| MX (1) | MXPA02009619A (xx) |
| NZ (1) | NZ521870A (xx) |
| WO (1) | WO2001074779A1 (xx) |
| ZA (1) | ZA200208226B (xx) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
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| JP2004538285A (ja) * | 2001-07-16 | 2004-12-24 | ユーロ−セルティック エス． ア． | アリール置換チアゾリジノンおよびその使用 |
| AR036873A1 (es) * | 2001-09-07 | 2004-10-13 | Euro Celtique Sa | Piridinas aril sustituidas a, composiciones farmaceuticas y el uso de las mismas para la preparacion de un medicamento |
| AR037233A1 (es) * | 2001-09-07 | 2004-11-03 | Euro Celtique Sa | Piridinas aril sustituidas, composiciones farmaceuticas y el uso de dichos compuestos para la elaboracion de un medicamento |
| DK1483247T3 (da) * | 2002-03-13 | 2009-08-17 | Euro Celtique Sa | Arylsubstituerede pyrimidiner og anvendelsen deraf |
| EP1532119A2 (en) * | 2002-07-31 | 2005-05-25 | Euro-Celtique S.A. | Aryl substituted benzimidazoles and their use as sodium channel blockers |
| US20050227974A9 (en) * | 2002-08-01 | 2005-10-13 | Euro-Celtique S.A. | Aminoalkyl-substituted aryl compounds and their use as sodium channel blockers |
| US20040152696A1 (en) * | 2002-08-01 | 2004-08-05 | Euro-Celtique S.A. | 2-substituted bicyclic benzoheterocyclic compounds and their use as sodium channel blockers |
| US7589110B2 (en) * | 2002-09-06 | 2009-09-15 | Durect Corporation | Delivery of modulators of glutamate-mediated neurotransmission to the inner ear |
| US20050192321A1 (en) * | 2003-09-15 | 2005-09-01 | Meythaler Jay M. | Treatment of neuropathy with rapid release aminopyridine |
| US20080287399A1 (en) * | 2004-12-14 | 2008-11-20 | Astrazeneca Ab | Substituted Aminopyridines and Uses Thereof |
| TWI385169B (zh) | 2005-10-31 | 2013-02-11 | Eisai R&D Man Co Ltd | 經雜環取代之吡啶衍生物及含有彼之抗真菌劑 |
| PT1963280E (pt) | 2005-12-22 | 2016-02-02 | Newron Pharm Spa | Derivados de 2-feniletilamino como cálcio e/ou moduladores do canal de sódio |
| LT2474521T (lt) | 2006-06-19 | 2016-11-25 | Newron Pharmaceuticals S.P.A. | Aukšto grynumo laipsnio 2-[4-(3- ir 2-fluorbenziloksi)benzilamino]propanamidai, skirti naudoti kaip medikamentai, ir juos apimančios farmacinės kompozicijos |
| NZ581288A (en) | 2007-06-15 | 2011-08-26 | Newron Pharm Spa | Substituted 2- [2- (phenyl) ethylamino] alkaneamide derivatives and their use as sodium and/or calcium channel modulators |
| LT2229351T (lt) * | 2007-12-11 | 2018-01-25 | Newron Pharmaceuticals S.P.A. | Didelio grynumo laipsnio 2-[4-(3- arba 2-fluorbenziloksi)benzilamino]propanamidų gamybos būdas |
| US8513287B2 (en) | 2007-12-27 | 2013-08-20 | Eisai R&D Management Co., Ltd. | Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same |
| WO2010093787A2 (en) * | 2009-02-11 | 2010-08-19 | Northwestern University | Aminopyridine dimer compounds, compositions and related methods for neuronal nitric oxide synthase inhibition |
| US8932842B2 (en) | 2009-02-11 | 2015-01-13 | Northwestern University | Aminopyridine dimer compounds, compositions and related methods for neuronal nitric oxide synthase inhibition |
| US9120752B2 (en) | 2010-07-16 | 2015-09-01 | Purdue Pharma, L.P. | Pyridine compounds as sodium channel blockers |
| AU2011303597A1 (en) | 2010-09-17 | 2013-04-11 | Purdue Pharma L.P. | Pyridine compounds and the uses thereof |
| CN103168033A (zh) | 2010-10-05 | 2013-06-19 | 普渡制药公司 | 作为钠通道阻断剂的喹唑啉化合物 |
| KR20130119964A (ko) | 2010-12-22 | 2013-11-01 | 퍼듀 퍼머 엘피 | 나트륨 채널 차단제로서의 치환된 피리딘 |
| RS55240B1 (sr) | 2011-06-27 | 2017-02-28 | Newron Pharm Spa | Fluorisani derivati arilalkilaminokarboksamida |
| ME02873B (me) | 2011-09-02 | 2018-04-20 | Purdue Pharma Lp | Pirimidini kao blokatori natrijumskog kanala |
| WO2013064883A1 (en) | 2011-10-31 | 2013-05-10 | Purdue Pharma L.P. | Heteroaryl compounds as sodium channel blockers |
| AU2012321111A1 (en) | 2011-10-31 | 2013-05-16 | Purdue Pharma L.P. | Quaternized amines as sodium channel blockers |
| WO2013072758A1 (en) | 2011-11-15 | 2013-05-23 | Purdue Pharma L.P. | Pyrimidine diol amides as sodium channel blockers |
| WO2013136170A1 (en) | 2012-03-16 | 2013-09-19 | Purdue Pharma L.P. | Substituted pyridines as sodium channel blockers |
| US9714252B2 (en) | 2012-12-20 | 2017-07-25 | Purdue Pharma L.P. | Cyclic sulfonamides as sodium channel blockers |
| US9637458B2 (en) | 2013-03-04 | 2017-05-02 | Jeffrey Lockman | Pyrimidine carboxamides as sodium channel blockers |
| US9120786B2 (en) | 2013-03-04 | 2015-09-01 | Purdue Pharma, L.P. | Triazine carboxamides as sodium channel blockers |
| JP6186494B2 (ja) | 2013-03-15 | 2017-08-23 | パーデュー、ファーマ、リミテッド、パートナーシップ | カルボキサミド誘導体及びその使用 |
| EP3039019B1 (en) | 2013-08-26 | 2020-04-22 | Purdue Pharma L.P. | Azaspiro[4.5]decane derivatives and use thereof |
| US9359330B2 (en) | 2013-08-26 | 2016-06-07 | Purdue Pharma L.P. | Substituted piperidines as sodium channel blockers |
| CN105745597B (zh) | 2013-09-20 | 2019-07-16 | 惠普发展公司，有限责任合伙企业 | 数据承载介质 |
| US9828348B2 (en) | 2013-11-08 | 2017-11-28 | Purdue Pharma L.P. | Benzimidazole derivatives and use thereof |
| US9340504B2 (en) | 2013-11-21 | 2016-05-17 | Purdue Pharma L.P. | Pyridine and piperidine derivatives as novel sodium channel blockers |
| WO2015094443A1 (en) | 2013-12-20 | 2015-06-25 | Purdue Pharma L.P. | Pyrimidines and use thereof |
| US9695144B2 (en) | 2013-12-23 | 2017-07-04 | Purdue Pharma L.P. | Dibenzazepine derivatives and use thereof |
| CN106103415B (zh) | 2013-12-23 | 2023-02-24 | 普渡制药公司 | 吲唑和其用途 |
| US9902726B2 (en) | 2013-12-30 | 2018-02-27 | Purdue Pharma L.P. | Pyridone-sulfone morphinan analogs as opioid receptor ligands |
| EP3097078B1 (en) | 2014-01-24 | 2022-05-25 | Purdue Pharma LP | Pyridines and pyrimidines and use thereof |
| WO2015123398A1 (en) | 2014-02-12 | 2015-08-20 | Purdue Pharma L.P. | Isoquinoline derivatives and use thereof |
| US10730866B2 (en) | 2014-04-07 | 2020-08-04 | Purdue Pharma L.P. | Indole derivatives and use thereof |
| EP3139921A4 (en) | 2014-05-06 | 2018-02-14 | Purdue Pharma L.P. | Benzomorphan analogs and use thereof |
| EP3154972A4 (en) | 2014-06-13 | 2017-11-22 | Purdue Pharma L.P. | Azamophinan derivatives and use thereof |
| WO2015192039A1 (en) | 2014-06-13 | 2015-12-17 | Purdue Pharma L.P. | Heterocyclic morphinan derivatives and use thereof |
| CA2977367A1 (en) | 2015-02-19 | 2016-08-25 | Purdue Pharma L.P. | Methods and compositions for decreasing gastric emptying |
| CN106365966A (zh) * | 2015-07-24 | 2017-02-01 | 上海医药集团股份有限公司 | 一种苄基芳基醚的制备方法 |
| US11111208B2 (en) | 2019-06-17 | 2021-09-07 | RK Pharma Solutions LLC | Process for the preparation of safinamide mesylate intermediate |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9515412D0 (en) | 1995-07-27 | 1995-09-27 | Pharmacia Spa | 2-(4-substituted)-benzylamino-2-methyl-propanamide derivatives |
| DE60003893T2 (de) | 1999-02-25 | 2004-02-05 | Pfizer Products Inc., Groton | 2-aminopyridine mit kondensierten ringsubstituenten |
| US6414011B1 (en) | 1999-03-26 | 2002-07-02 | Euro-Celtique S.A. | Aryl substituted pyrazoles, and pyrroles, and the use thereof |
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2001
- 2001-03-29 KR KR1020027013015A patent/KR20020084278A/ko not_active Application Discontinuation
- 2001-03-29 MX MXPA02009619A patent/MXPA02009619A/es unknown
- 2001-03-29 CA CA002403991A patent/CA2403991A1/en not_active Abandoned
- 2001-03-29 WO PCT/US2001/010125 patent/WO2001074779A1/en not_active Application Discontinuation
- 2001-03-29 AU AU2001249610A patent/AU2001249610B2/en not_active Ceased
- 2001-03-29 CN CN01808453A patent/CN1426397A/zh active Pending
- 2001-03-29 BR BR0109706-7A patent/BR0109706A/pt not_active IP Right Cessation
- 2001-03-29 JP JP2001572474A patent/JP2003529589A/ja active Pending
- 2001-03-29 US US09/819,693 patent/US6335354B2/en not_active Expired - Lifetime
- 2001-03-29 NZ NZ521870A patent/NZ521870A/en unknown
- 2001-03-29 AU AU4961001A patent/AU4961001A/xx active Pending
- 2001-03-29 IL IL15195201A patent/IL151952A0/xx unknown
- 2001-03-29 EP EP01922853A patent/EP1268427A1/en not_active Withdrawn
-
2002
- 2002-10-11 ZA ZA200208226A patent/ZA200208226B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20020084278A (ko) | 2002-11-04 |
| NZ521870A (en) | 2004-08-27 |
| BR0109706A (pt) | 2003-02-04 |
| JP2003529589A (ja) | 2003-10-07 |
| AU4961001A (en) | 2001-10-15 |
| EP1268427A1 (en) | 2003-01-02 |
| CA2403991A1 (en) | 2001-10-11 |
| US20010044428A1 (en) | 2001-11-22 |
| MXPA02009619A (es) | 2004-07-30 |
| AU2001249610B2 (en) | 2005-03-24 |
| US6335354B2 (en) | 2002-01-01 |
| IL151952A0 (en) | 2003-04-10 |
| WO2001074779A1 (en) | 2001-10-11 |
| CN1426397A (zh) | 2003-06-25 |
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