JP5546761B2 - 非イミダゾールアルキルアミンヒスタミンｈ３−受容体リガンドによるパーキンソン病、閉塞性睡眠時無呼吸、レビー小体型認知症、血管性認知症の治療 - Google Patents
非イミダゾールアルキルアミンヒスタミンｈ３−受容体リガンドによるパーキンソン病、閉塞性睡眠時無呼吸、レビー小体型認知症、血管性認知症の治療 Download PDFInfo
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- JP5546761B2 JP5546761B2 JP2008503613A JP2008503613A JP5546761B2 JP 5546761 B2 JP5546761 B2 JP 5546761B2 JP 2008503613 A JP2008503613 A JP 2008503613A JP 2008503613 A JP2008503613 A JP 2008503613A JP 5546761 B2 JP5546761 B2 JP 5546761B2
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- -1 imidazole alkylamine Chemical class 0.000 title claims description 155
- 238000011282 treatment Methods 0.000 title claims description 28
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- 208000018737 Parkinson disease Diseases 0.000 title description 37
- 201000002832 Lewy body dementia Diseases 0.000 title description 16
- 201000004810 Vascular dementia Diseases 0.000 title description 14
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 title description 11
- 102000004384 Histamine H3 receptors Human genes 0.000 title description 8
- 108090000981 Histamine H3 receptors Proteins 0.000 title description 8
- 206010067889 Dementia with Lewy bodies Diseases 0.000 title description 7
- 239000003446 ligand Substances 0.000 title description 3
- 150000001875 compounds Chemical class 0.000 claims description 191
- 125000000217 alkyl group Chemical group 0.000 claims description 148
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 97
- 125000004432 carbon atom Chemical group C* 0.000 claims description 74
- 239000003814 drug Substances 0.000 claims description 23
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- 125000005843 halogen group Chemical group 0.000 claims description 22
- 229910052757 nitrogen Inorganic materials 0.000 claims description 19
- NNACHAUCXXVJSP-UHFFFAOYSA-N pitolisant Chemical compound C1=CC(Cl)=CC=C1CCCOCCCN1CCCCC1 NNACHAUCXXVJSP-UHFFFAOYSA-N 0.000 claims description 14
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 12
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- 206010041349 Somnolence Diseases 0.000 claims description 10
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- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 5
- 239000013078 crystal Substances 0.000 claims description 5
- 150000004677 hydrates Chemical class 0.000 claims description 5
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 5
- ZBYDMLXPLCXXGZ-UHFFFAOYSA-N 1-[3-(3-phenylpropoxy)propyl]pyrrolidine Chemical compound C1CCCN1CCCOCCCC1=CC=CC=C1 ZBYDMLXPLCXXGZ-UHFFFAOYSA-N 0.000 claims description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 4
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims description 4
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims description 4
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- ARXUNWQEEIWRFV-UHFFFAOYSA-N 1-[6-phenyl-1-(6-phenyl-3-piperidin-1-ylhexoxy)hexan-3-yl]piperidine Chemical compound C=1C=CC=CC=1CCCC(N1CCCCC1)CCOCCC(N1CCCCC1)CCCC1=CC=CC=C1 ARXUNWQEEIWRFV-UHFFFAOYSA-N 0.000 claims description 3
- FWWOWPGPERBCNJ-UHFFFAOYSA-N 2-hydroxy-4-(2-hydroxyethoxy)-4-oxobutanoic acid Chemical compound OCCOC(=O)CC(O)C(O)=O FWWOWPGPERBCNJ-UHFFFAOYSA-N 0.000 claims description 3
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims description 3
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- OZVBMTJYIDMWIL-AYFBDAFISA-N bromocriptine Chemical compound C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@]2(C(=O)N3[C@H](C(N4CCC[C@H]4[C@]3(O)O2)=O)CC(C)C)C(C)C)C2)=C3C2=C(Br)NC3=C1 OZVBMTJYIDMWIL-AYFBDAFISA-N 0.000 claims description 3
- 229960002802 bromocriptine Drugs 0.000 claims description 3
- 229960003587 lisuride Drugs 0.000 claims description 3
- MUBZPKHOEPUJKR-UHFFFAOYSA-M oxalate(1-) Chemical compound OC(=O)C([O-])=O MUBZPKHOEPUJKR-UHFFFAOYSA-M 0.000 claims description 3
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- 125000003118 aryl group Chemical group 0.000 description 69
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- 125000000753 cycloalkyl group Chemical group 0.000 description 43
- 125000001424 substituent group Chemical group 0.000 description 39
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 29
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- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 26
- 239000001257 hydrogen Substances 0.000 description 25
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 24
- 125000000623 heterocyclic group Chemical group 0.000 description 24
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- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 22
- 229910052717 sulfur Chemical group 0.000 description 22
- 229910052736 halogen Inorganic materials 0.000 description 21
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 15
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- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 15
- 125000004093 cyano group Chemical group *C#N 0.000 description 14
- 125000000468 ketone group Chemical group 0.000 description 14
- RGSFGYAAUTVSQA-UHFFFAOYSA-N Cyclopentane Chemical compound C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 description 13
- 125000001624 naphthyl group Chemical group 0.000 description 13
- 125000000304 alkynyl group Chemical group 0.000 description 12
- 125000003342 alkenyl group Chemical group 0.000 description 11
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- 239000000460 chlorine Substances 0.000 description 11
- 150000002460 imidazoles Chemical class 0.000 description 11
- 125000004434 sulfur atom Chemical group 0.000 description 11
- ORILYTVJVMAKLC-UHFFFAOYSA-N adamantane Chemical compound C1C(C2)CC3CC1CC2C3 ORILYTVJVMAKLC-UHFFFAOYSA-N 0.000 description 10
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 10
- NNBZCPXTIHJBJL-UHFFFAOYSA-N decalin Chemical compound C1CCCC2CCCCC21 NNBZCPXTIHJBJL-UHFFFAOYSA-N 0.000 description 10
- 201000010099 disease Diseases 0.000 description 10
- 208000035475 disorder Diseases 0.000 description 10
- DMEGYFMYUHOHGS-UHFFFAOYSA-N heptamethylene Natural products C1CCCCCC1 DMEGYFMYUHOHGS-UHFFFAOYSA-N 0.000 description 10
- 239000003395 histamine H3 receptor antagonist Substances 0.000 description 10
- 208000009829 Lewy Body Disease Diseases 0.000 description 9
- URLKBWYHVLBVBO-UHFFFAOYSA-N Para-Xylene Chemical compound CC1=CC=C(C)C=C1 URLKBWYHVLBVBO-UHFFFAOYSA-N 0.000 description 9
- 125000002252 acyl group Chemical group 0.000 description 9
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- 230000000694 effects Effects 0.000 description 9
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- 150000002576 ketones Chemical class 0.000 description 9
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 8
- 125000002947 alkylene group Chemical group 0.000 description 8
- 150000001602 bicycloalkyls Chemical group 0.000 description 8
- 150000001721 carbon Chemical group 0.000 description 8
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- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 7
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- 229910052794 bromium Inorganic materials 0.000 description 6
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 6
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- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 description 5
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- BNRNAKTVFSZAFA-UHFFFAOYSA-N hydrindane Chemical compound C1CCCC2CCCC21 BNRNAKTVFSZAFA-UHFFFAOYSA-N 0.000 description 5
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- LSTBLKAYDSCWNI-UHFFFAOYSA-N 1-[4-[[4-[(4-methylpiperidin-1-yl)methyl]phenyl]methoxy]phenyl]ethanone Chemical compound C1CC(C)CCN1CC(C=C1)=CC=C1COC1=CC=C(C(C)=O)C=C1 LSTBLKAYDSCWNI-UHFFFAOYSA-N 0.000 description 2
- RPZVPCNZFPBCRU-UHFFFAOYSA-N 1-[5-(4-phenoxyphenoxy)pentyl]pyrrolidine;n-[4-(5-pyrrolidin-1-ylpentoxy)phenyl]acetamide Chemical compound C1=CC(NC(=O)C)=CC=C1OCCCCCN1CCCC1.C1CCCN1CCCCCOC(C=C1)=CC=C1OC1=CC=CC=C1 RPZVPCNZFPBCRU-UHFFFAOYSA-N 0.000 description 2
- PLRACCBDVIHHLZ-UHFFFAOYSA-N 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine Chemical compound C1N(C)CCC(C=2C=CC=CC=2)=C1 PLRACCBDVIHHLZ-UHFFFAOYSA-N 0.000 description 2
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 description 2
- GCINBWWQZPLPMO-UHFFFAOYSA-N 2-(cyclohexylmethyl)-1-(3-piperidin-1-ylpropyl)guanidine;1-[3-(diethylamino)propyl]-3-phenylurea Chemical compound CCN(CC)CCCNC(=O)NC1=CC=CC=C1.C1CCCCC1CN=C(N)NCCCN1CCCCC1 GCINBWWQZPLPMO-UHFFFAOYSA-N 0.000 description 2
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- 239000000902 placebo Substances 0.000 description 1
- 229940068196 placebo Drugs 0.000 description 1
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- 125000001844 prenyl group Chemical group [H]C([*])([H])C([H])=C(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 description 1
- 229940001470 psychoactive drug Drugs 0.000 description 1
- 239000004089 psychotropic agent Substances 0.000 description 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 description 1
- 125000002206 pyridazin-3-yl group Chemical group [H]C1=C([H])C([H])=C(*)N=N1 0.000 description 1
- 125000004940 pyridazin-4-yl group Chemical group N1=NC=C(C=C1)* 0.000 description 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 description 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 description 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
- 239000002469 receptor inverse agonist Substances 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 235000018770 reduced food intake Nutrition 0.000 description 1
- 230000003252 repetitive effect Effects 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- 230000000284 resting effect Effects 0.000 description 1
- UHSKFQJFRQCDBE-UHFFFAOYSA-N ropinirole Chemical compound CCCN(CCC)CCC1=CC=CC2=C1CC(=O)N2 UHSKFQJFRQCDBE-UHFFFAOYSA-N 0.000 description 1
- 229960001879 ropinirole Drugs 0.000 description 1
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- 238000000926 separation method Methods 0.000 description 1
- 230000004622 sleep time Effects 0.000 description 1
- 230000008454 sleep-wake cycle Effects 0.000 description 1
- 208000020685 sleep-wake disease Diseases 0.000 description 1
- 230000037321 sleepiness Effects 0.000 description 1
- 210000002460 smooth muscle Anatomy 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 210000003523 substantia nigra Anatomy 0.000 description 1
- 125000000547 substituted alkyl group Chemical group 0.000 description 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 description 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 150000003512 tertiary amines Chemical class 0.000 description 1
- 230000004797 therapeutic response Effects 0.000 description 1
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- 125000005425 toluyl group Chemical group 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Hospice & Palliative Care (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP05290727.6 | 2005-04-01 | ||
| EP05290727A EP1707203A1 (en) | 2005-04-01 | 2005-04-01 | Treatment of parkinson's disease obstructive sleep apnea, dementia with lewy bodies, vascular dementia with non-imidazole alkylamines histamine H3- receptor ligands |
| US66861805P | 2005-04-06 | 2005-04-06 | |
| US60/668,618 | 2005-04-06 | ||
| PCT/IB2006/000739 WO2006103546A2 (en) | 2005-04-01 | 2006-03-30 | Treatment of parkinson's disease, obstructive sleep apnea, dementia with lewy bodies, vascular dementia with non-imidazole alkylamines histamine h3-receptor ligands |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014000383A Division JP5955872B2 (ja) | 2005-04-01 | 2014-01-06 | 非イミダゾールアルキルアミンヒスタミンｈ３−受容体リガンドによるパーキンソン病、閉塞性睡眠時無呼吸、レビー小体型認知症、血管性認知症の治療 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008534572A JP2008534572A (ja) | 2008-08-28 |
| JP2008534572A5 JP2008534572A5 (OSRAM) | 2010-11-25 |
| JP5546761B2 true JP5546761B2 (ja) | 2014-07-09 |
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Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008503613A Active JP5546761B2 (ja) | 2005-04-01 | 2006-03-30 | 非イミダゾールアルキルアミンヒスタミンｈ３−受容体リガンドによるパーキンソン病、閉塞性睡眠時無呼吸、レビー小体型認知症、血管性認知症の治療 |
| JP2014000383A Active JP5955872B2 (ja) | 2005-04-01 | 2014-01-06 | 非イミダゾールアルキルアミンヒスタミンｈ３−受容体リガンドによるパーキンソン病、閉塞性睡眠時無呼吸、レビー小体型認知症、血管性認知症の治療 |
| JP2016045424A Pending JP2016106142A (ja) | 2005-04-01 | 2016-03-09 | 非イミダゾールアルキルアミンヒスタミンｈ３−受容体リガンドによるパーキンソン病、閉塞性睡眠時無呼吸、レビー小体型認知症、血管性認知症の治療 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014000383A Active JP5955872B2 (ja) | 2005-04-01 | 2014-01-06 | 非イミダゾールアルキルアミンヒスタミンｈ３−受容体リガンドによるパーキンソン病、閉塞性睡眠時無呼吸、レビー小体型認知症、血管性認知症の治療 |
| JP2016045424A Pending JP2016106142A (ja) | 2005-04-01 | 2016-03-09 | 非イミダゾールアルキルアミンヒスタミンｈ３−受容体リガンドによるパーキンソン病、閉塞性睡眠時無呼吸、レビー小体型認知症、血管性認知症の治療 |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US8486947B2 (OSRAM) |
| EP (2) | EP1707203A1 (OSRAM) |
| JP (3) | JP5546761B2 (OSRAM) |
| KR (1) | KR101308527B1 (OSRAM) |
| CN (1) | CN101171009B (OSRAM) |
| AU (1) | AU2006228413C1 (OSRAM) |
| BR (1) | BRPI0612216B1 (OSRAM) |
| CA (1) | CA2603656C (OSRAM) |
| CY (1) | CY1114636T1 (OSRAM) |
| DK (1) | DK1863487T4 (OSRAM) |
| EA (1) | EA016007B1 (OSRAM) |
| ES (1) | ES2426008T5 (OSRAM) |
| HR (1) | HRP20130748T4 (OSRAM) |
| MA (1) | MA29353B1 (OSRAM) |
| ME (1) | ME01713B (OSRAM) |
| MX (1) | MX2007012162A (OSRAM) |
| NO (1) | NO343603B1 (OSRAM) |
| NZ (1) | NZ561940A (OSRAM) |
| PL (1) | PL1863487T5 (OSRAM) |
| PT (1) | PT1863487E (OSRAM) |
| RS (1) | RS52911B2 (OSRAM) |
| SG (1) | SG147415A1 (OSRAM) |
| SI (1) | SI1863487T2 (OSRAM) |
| TN (1) | TNSN07365A1 (OSRAM) |
| UA (1) | UA94902C2 (OSRAM) |
| WO (1) | WO2006103546A2 (OSRAM) |
| ZA (1) | ZA200708086B (OSRAM) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
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| MX2008016343A (es) | 2006-06-23 | 2009-01-19 | Abbott Lab | Derivados ciclopropil amina como moduladores del receptro de histamina h3. |
| US9108948B2 (en) | 2006-06-23 | 2015-08-18 | Abbvie Inc. | Cyclopropyl amine derivatives |
| FR2903904A1 (fr) * | 2006-07-21 | 2008-01-25 | Bioprojet Soc Civ Ile | Association de modafinil et d'un antagoniste ou agoniste inverse du recepteur h3 |
| JP5335675B2 (ja) | 2006-07-25 | 2013-11-06 | セファロン、インク． | ピリジジノン誘導体 |
| US8153813B2 (en) | 2007-12-20 | 2012-04-10 | Abbott Laboratories | Benzothiazole and benzooxazole derivatives and methods of use |
| MX2010008375A (es) | 2008-01-30 | 2011-03-04 | Cephalon Inc Star | Derivados de piperidina espirocíclicos substituidos como ligandos de receptores de histamina-3 (h3). |
| FR2932479A1 (fr) * | 2008-06-13 | 2009-12-18 | Servier Lab | Nouveaux derives azabicycliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent. |
| US9186353B2 (en) | 2009-04-27 | 2015-11-17 | Abbvie Inc. | Treatment of osteoarthritis pain |
| US8853390B2 (en) | 2010-09-16 | 2014-10-07 | Abbvie Inc. | Processes for preparing 1,2-substituted cyclopropyl derivatives |
| US9181275B2 (en) | 2011-08-11 | 2015-11-10 | Abbvie Inc. | Mercaptoamidine derivatives and methods of use |
| WO2013151982A1 (en) | 2012-04-03 | 2013-10-10 | Arena Pharmaceuticals, Inc. | Methods and compounds useful in treating pruritus, and methods for identifying such compounds |
| CN104703592A (zh) * | 2012-10-05 | 2015-06-10 | 转化技术制药有限责任公司 | 治疗轻度和中度阿尔茨海默病的方法 |
| EP3391886A1 (en) | 2017-04-19 | 2018-10-24 | Novartis AG | The use of a h3r inverse agonist for the treatment of shift work disorder |
| US20200282215A1 (en) | 2019-03-06 | 2020-09-10 | Medtronic Xomed, LLC | Evaluating stimulation eficacy for treating sleep apnea and lingual muscle tone sensing system for improved osa therapy |
| EP4248969A1 (en) | 2022-03-23 | 2023-09-27 | Bioprojet | Use of pitolisant for treating severe fatigue |
| WO2024201139A1 (en) | 2023-03-31 | 2024-10-03 | Bioprojet Pharma | Polymorph form of pitolisant hydrochloride |
| WO2025082974A1 (en) | 2023-10-16 | 2025-04-24 | Bioprojet Pharma | New formulations of pitolisant and methods of use |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JPS5815945A (ja) * | 1981-07-21 | 1983-01-29 | Teikoku Hormone Mfg Co Ltd | 新規なフエノキシアルキルアミン誘導体 |
| FR2579596B1 (fr) | 1985-03-26 | 1987-11-20 | Inst Nat Sante Rech Med | (imidazolyl-4) piperidines, leur preparation et leur application en therapeutique |
| FR2671083B1 (fr) | 1990-12-31 | 1994-12-23 | Inst Nat Sante Rech Med | Nouvelles 4-(4-imidazolyl) piperidines substituees en 1, leur preparation ainsi que leurs applications therapeutiques. |
| ATE159248T1 (de) | 1991-02-27 | 1997-11-15 | Seed Capital Investments | Imidazol-derivate mit antagonistischer aktivität auf den histamin-h3-receptor |
| ZA929788B (en) | 1991-12-18 | 1993-06-22 | Schering Corp | Imidazolyl or imidazoylalkyl substituted with a four or five membered nitrogen containing heterocyclic ring. |
| WO1993012107A1 (en) | 1991-12-18 | 1993-06-24 | Schering Corporation | Imidazoylalkyl substituted with a six membered nitrogen containing heterocyclic ring |
| FR2686084B1 (fr) | 1992-01-10 | 1995-12-22 | Bioprojet Soc Civ | Nouveaux derives de l'imidazole, leur preparation et leurs applications therapeutiques. |
| US5639775A (en) | 1992-04-01 | 1997-06-17 | The University Of Toledo | 4-[4'-piperodinyl or 3'-pirrolidinyl] substituted imidazoles as H3 -receptor antagonists and therapeutic uses thereof |
| US5380858A (en) | 1992-04-01 | 1995-01-10 | The University Of Toledo | Process for the preparation of intermediates useful for the synthesis of histamine receptor antagonists |
| US5486526A (en) * | 1992-04-01 | 1996-01-23 | The University Of Toledo | Histamine H3 -receptor antagonists and therapeutic uses thereof |
| WO1994017058A1 (fr) | 1993-01-25 | 1994-08-04 | The Green Cross Corporation | Compose d'imidazole |
| JP3522790B2 (ja) | 1993-06-08 | 2004-04-26 | 花王株式会社 | Ｈ３−レセプター刺激薬 |
| AU7823894A (en) | 1993-08-27 | 1995-03-21 | Vrije Universiteit | New imidazole derivatives having agonistic or antagonistic activity on the histamine h3 receptor |
| GB9319534D0 (en) * | 1993-09-22 | 1993-11-10 | Boots Co Plc | Therapeutic agents |
| HUT74386A (en) | 1993-11-15 | 1996-12-30 | Schering Corp | Phenyl-alkyl imidazoles as h3-receptor antagonists and pharmaceutical compositions containing them |
| GB9411045D0 (en) * | 1994-06-02 | 1994-07-20 | Smithkline Beecham Plc | Compounds and use |
| FR2732017B1 (fr) | 1995-03-21 | 2000-09-22 | Inst Nat Sante Rech Med | Nouveaux derives de l'imidazole antagonistes et/ou agonistes du recepteur h3 de l'histamine, leur preparation et leurs applications therapeutiques |
| US5652258A (en) | 1995-05-30 | 1997-07-29 | Gliatech, Inc. | 2-(4-imidazoyl) cyclopropyl derivatives |
| JPH11506106A (ja) | 1995-05-30 | 1999-06-02 | グリアテツク・インコーポレイテツド | １ｈ−４（５）−置換イミダゾール誘導体 |
| AU713166B2 (en) | 1995-06-07 | 1999-11-25 | Gliatech Inc. | 1H-4(5)-substituted imidazole derivatives |
| NZ331272A (en) | 1996-02-09 | 2000-01-28 | Black James Foundation | Histamine H3 receptor ligands |
| JP3925579B2 (ja) * | 1998-02-03 | 2007-06-06 | 日本精工株式会社 | 潤滑剤供給体、並びに前記潤滑剤供給体を備える転がり軸受、リニアガイド装置及びボールねじ装置 |
| EP0982300A3 (en) * | 1998-07-29 | 2000-03-08 | Societe Civile Bioprojet | Non-imidazole alkylamines as histamine H3 - receptor ligands and their therapeutic applications |
| US6136559A (en) * | 1998-10-07 | 2000-10-24 | Ortho Pharmaceutical Corporation | DNA encoding as human histamine receptor of the H3 subtype |
| ATE438614T1 (de) | 1999-06-11 | 2009-08-15 | Toyama Chemical Co Ltd | N-alkoxyalkyl-n,n-dialkylamin-derivate oder ihre salze und heilmittel zur behandlung degenerativer erkrankungen der nerven die diese enthalten |
| GB9924941D0 (en) | 1999-10-22 | 1999-12-22 | Univ Manchester | Treatment of dyskinesia |
| US6620839B2 (en) * | 2000-07-13 | 2003-09-16 | Abbott Laboratories | 1,3-disubstituted and 1,3,3-trisubstituted pyrrolidines as histamine-3 receptor ligands and their therapeutic applications |
| US7186732B2 (en) * | 2000-08-08 | 2007-03-06 | Ortho-Mcneil Pharmaceutical, Inc. | Non-imidazole aryloxyalkylamines |
| US20020042400A1 (en) | 2000-08-17 | 2002-04-11 | Yajing Rong | Novel alicyclic imidazoles as H3 agents |
| WO2002015905A1 (en) * | 2000-08-21 | 2002-02-28 | Gliatech, Inc. | The use of histamine h3 receptor inverse agonists for the control of appetite and treatment of obesity |
| ES2299596T3 (es) | 2001-03-29 | 2008-06-01 | Ortho Mcneil Pharmaceutical, Inc. | Derivados de imidazol utiles como ligandos del receptor h3 de la histamina. |
| WO2003044059A1 (en) * | 2001-11-15 | 2003-05-30 | Ortho-Mcneil Pharmaceutical, Inc. | Agonists of recombinant human histamine h3 receptor |
| AU2002357775A1 (en) * | 2001-12-10 | 2003-06-23 | Ortho-Mcneil Pharmaceutical, Inc. | Phenylalkynes |
| CA2504272A1 (en) | 2002-10-23 | 2004-05-06 | Janssen Pharmaceutica, N.V. | Phenylpiperidines and phenylpyrrolidines as histamine h3 receptor modulators |
| FR2856596B1 (fr) | 2003-06-27 | 2007-04-27 | Bioprojet Soc Civ | Nouvelle association medicamenteuse psychiatrique et utilisation d'une antagoniste ou agoniste inverse du recepteur h3 de l'histamine pour preparer un medicament prevenant des effets indesirables de psychotropes. |
| CN1812981A (zh) * | 2003-06-27 | 2006-08-02 | 万有制药株式会社 | 杂芳氧基含氮饱和杂环衍生物 |
| SE0302116D0 (sv) * | 2003-07-21 | 2003-07-21 | Astrazeneca Ab | Novel compounds |
| JP4765627B2 (ja) | 2003-09-22 | 2011-09-07 | Ｍｓｄ株式会社 | 新規ピペリジン誘導体 |
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2005
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2006
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- 2006-03-30 CN CN2006800157656A patent/CN101171009B/zh active Active
- 2006-03-30 MX MX2007012162A patent/MX2007012162A/es active IP Right Grant
- 2006-03-30 ME MEP-2013-98A patent/ME01713B/me unknown
- 2006-03-30 SI SI200631636T patent/SI1863487T2/sl unknown
- 2006-03-30 BR BRPI0612216-7A patent/BRPI0612216B1/pt active IP Right Grant
- 2006-03-30 DK DK06744466.1T patent/DK1863487T4/da active
- 2006-03-30 UA UAA200710712A patent/UA94902C2/ru unknown
- 2006-03-30 EA EA200702135A patent/EA016007B1/ru not_active IP Right Cessation
- 2006-03-30 EP EP06744466.1A patent/EP1863487B2/en active Active
- 2006-03-30 PT PT67444661T patent/PT1863487E/pt unknown
- 2006-03-30 WO PCT/IB2006/000739 patent/WO2006103546A2/en not_active Ceased
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