CA2760527A1 - Method of treatment of depression - Google Patents
Method of treatment of depression Download PDFInfo
- Publication number
- CA2760527A1 CA2760527A1 CA2760527A CA2760527A CA2760527A1 CA 2760527 A1 CA2760527 A1 CA 2760527A1 CA 2760527 A CA2760527 A CA 2760527A CA 2760527 A CA2760527 A CA 2760527A CA 2760527 A1 CA2760527 A1 CA 2760527A1
- Authority
- CA
- Canada
- Prior art keywords
- depression
- viloxazine
- activity
- pharmaceutical agent
- day
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- 238000000034 method Methods 0.000 title claims abstract description 21
- 208000020401 Depressive disease Diseases 0.000 title claims abstract description 12
- 230000000694 effects Effects 0.000 claims abstract description 40
- 102000005962 receptors Human genes 0.000 claims abstract description 18
- 108020003175 receptors Proteins 0.000 claims abstract description 18
- 230000002474 noradrenergic effect Effects 0.000 claims abstract description 12
- 239000008177 pharmaceutical agent Substances 0.000 claims abstract description 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 9
- 230000001747 exhibiting effect Effects 0.000 claims abstract description 4
- 230000000862 serotonergic effect Effects 0.000 claims abstract description 3
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims description 47
- 229960001255 viloxazine Drugs 0.000 claims description 35
- YWPHCCPCQOJSGZ-LLVKDONJSA-N (2r)-2-[(2-ethoxyphenoxy)methyl]morpholine Chemical compound CCOC1=CC=CC=C1OC[C@@H]1OCCNC1 YWPHCCPCQOJSGZ-LLVKDONJSA-N 0.000 claims description 33
- 229940076279 serotonin Drugs 0.000 claims description 18
- 101710150237 5-hydroxytryptamine receptor 7 Proteins 0.000 claims description 8
- 230000005764 inhibitory process Effects 0.000 claims description 8
- 230000002295 serotoninergic effect Effects 0.000 claims description 7
- 239000013543 active substance Substances 0.000 claims description 6
- 230000002411 adverse Effects 0.000 claims description 5
- 230000003042 antagnostic effect Effects 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- 230000001270 agonistic effect Effects 0.000 claims description 2
- 230000003466 anti-cipated effect Effects 0.000 claims description 2
- 230000003291 dopaminomimetic effect Effects 0.000 claims description 2
- 230000003371 gabaergic effect Effects 0.000 claims description 2
- 238000007423 screening assay Methods 0.000 claims description 2
- 108010078791 Carrier Proteins Proteins 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 102000040811 transporter activity Human genes 0.000 claims 1
- 108091092194 transporter activity Proteins 0.000 claims 1
- 238000003556 assay Methods 0.000 description 12
- 239000000556 agonist Substances 0.000 description 10
- 239000003446 ligand Substances 0.000 description 10
- 238000003345 scintillation counting Methods 0.000 description 10
- 239000005557 antagonist Substances 0.000 description 9
- 150000001875 compounds Chemical class 0.000 description 8
- 108091005436 5-HT7 receptors Proteins 0.000 description 7
- 230000027455 binding Effects 0.000 description 7
- 208000035475 disorder Diseases 0.000 description 5
- 230000004044 response Effects 0.000 description 5
- 230000009870 specific binding Effects 0.000 description 5
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 description 4
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 description 4
- HJOCKFVCMLCPTP-UHFFFAOYSA-N 2-[(2-ethoxyphenoxy)methyl]morpholine;hydron;chloride Chemical compound Cl.CCOC1=CC=CC=C1OCC1OCCNC1 HJOCKFVCMLCPTP-UHFFFAOYSA-N 0.000 description 3
- 102100024959 5-hydroxytryptamine receptor 2C Human genes 0.000 description 3
- 101710138093 5-hydroxytryptamine receptor 2C Proteins 0.000 description 3
- ASXGJMSKWNBENU-UHFFFAOYSA-N 8-OH-DPAT Chemical compound C1=CC(O)=C2CC(N(CCC)CCC)CCC2=C1 ASXGJMSKWNBENU-UHFFFAOYSA-N 0.000 description 3
- 239000000935 antidepressant agent Substances 0.000 description 3
- 229940005513 antidepressants Drugs 0.000 description 3
- FPCCSQOGAWCVBH-UHFFFAOYSA-N ketanserin Chemical compound C1=CC(F)=CC=C1C(=O)C1CCN(CCN2C(C3=CC=CC=C3NC2=O)=O)CC1 FPCCSQOGAWCVBH-UHFFFAOYSA-N 0.000 description 3
- 102100022738 5-hydroxytryptamine receptor 1A Human genes 0.000 description 2
- 101710138638 5-hydroxytryptamine receptor 1A Proteins 0.000 description 2
- 206010000087 Abdominal pain upper Diseases 0.000 description 2
- 208000020925 Bipolar disease Diseases 0.000 description 2
- 206010010305 Confusional state Diseases 0.000 description 2
- 206010010774 Constipation Diseases 0.000 description 2
- 206010012735 Diarrhoea Diseases 0.000 description 2
- 206010013887 Dysarthria Diseases 0.000 description 2
- 206010024421 Libido increased Diseases 0.000 description 2
- 208000001089 Multiple system atrophy Diseases 0.000 description 2
- 206010028813 Nausea Diseases 0.000 description 2
- 206010030113 Oedema Diseases 0.000 description 2
- 206010031127 Orthostatic hypotension Diseases 0.000 description 2
- 208000001431 Psychomotor Agitation Diseases 0.000 description 2
- 206010037211 Psychomotor hyperactivity Diseases 0.000 description 2
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 2
- 102000003929 Transaminases Human genes 0.000 description 2
- 108090000340 Transaminases Proteins 0.000 description 2
- 206010044565 Tremor Diseases 0.000 description 2
- 102000002852 Vasopressins Human genes 0.000 description 2
- 108010004977 Vasopressins Proteins 0.000 description 2
- 208000012886 Vertigo Diseases 0.000 description 2
- 206010047700 Vomiting Diseases 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 230000001430 anti-depressive effect Effects 0.000 description 2
- 230000004596 appetite loss Effects 0.000 description 2
- KBZOIRJILGZLEJ-LGYYRGKSSA-N argipressin Chemical compound C([C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CSSC[C@@H](C(N[C@@H](CC=2C=CC(O)=CC=2)C(=O)N1)=O)N)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C1=CC=CC=C1 KBZOIRJILGZLEJ-LGYYRGKSSA-N 0.000 description 2
- 238000001514 detection method Methods 0.000 description 2
- 238000006073 displacement reaction Methods 0.000 description 2
- 210000003743 erythrocyte Anatomy 0.000 description 2
- 238000002825 functional assay Methods 0.000 description 2
- 238000002868 homogeneous time resolved fluorescence Methods 0.000 description 2
- 238000011534 incubation Methods 0.000 description 2
- 206010022437 insomnia Diseases 0.000 description 2
- 238000012417 linear regression Methods 0.000 description 2
- 208000019017 loss of appetite Diseases 0.000 description 2
- 235000021266 loss of appetite Nutrition 0.000 description 2
- 210000003141 lower extremity Anatomy 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 230000008693 nausea Effects 0.000 description 2
- 230000002285 radioactive effect Effects 0.000 description 2
- 230000028327 secretion Effects 0.000 description 2
- 238000004062 sedimentation Methods 0.000 description 2
- 230000000638 stimulation Effects 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 229960003726 vasopressin Drugs 0.000 description 2
- 231100000889 vertigo Toxicity 0.000 description 2
- 230000008673 vomiting Effects 0.000 description 2
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 description 1
- AQHHHDLHHXJYJD-AWEZNQCLSA-N (2s)-1-naphthalen-1-yloxy-3-(propan-2-ylamino)propan-2-ol Chemical compound C1=CC=C2C(OC[C@@H](O)CNC(C)C)=CC=CC2=C1 AQHHHDLHHXJYJD-AWEZNQCLSA-N 0.000 description 1
- VAYOSLLFUXYJDT-QZGBZKRISA-N (6ar,9r)-n,n-diethyl-7-(tritritiomethyl)-6,6a,8,9-tetrahydro-4h-indolo[4,3-fg]quinoline-9-carboxamide Chemical compound C1=CC(C2=C[C@H](CN([C@@H]2C2)C([3H])([3H])[3H])C(=O)N(CC)CC)=C3C2=CNC3=C1 VAYOSLLFUXYJDT-QZGBZKRISA-N 0.000 description 1
- WYCMFCPHWDZHMR-UHFFFAOYSA-N 1-(4,7-dimethyl-6,6a,8,9,10,10a-hexahydroindolo[4,3-fg]quinoline-9-yl)-n,n-dimethylmethanesulfonamide Chemical compound C1=CC(C2CC(CN(C)C2C2)CS(=O)(=O)N(C)C)=C3C2=CN(C)C3=C1 WYCMFCPHWDZHMR-UHFFFAOYSA-N 0.000 description 1
- MFWNKCLOYSRHCJ-UHFFFAOYSA-N 1-Methyl-N-{9-methyl-9-azabicyclo[3.3.1]nonan-3-yl}-1H-indazole-3-carboxamide Chemical compound C1=CC=C2C(C(=O)NC3CC4CCCC(C3)N4C)=NN(C)C2=C1 MFWNKCLOYSRHCJ-UHFFFAOYSA-N 0.000 description 1
- YWPHCCPCQOJSGZ-UHFFFAOYSA-N 2-[(2-ethoxyphenoxy)methyl]morpholine Chemical compound CCOC1=CC=CC=C1OCC1OCCNC1 YWPHCCPCQOJSGZ-UHFFFAOYSA-N 0.000 description 1
- OFCNTYBPPAQCRE-UHFFFAOYSA-N 3-(2-aminoethyl)-3h-indol-5-ol Chemical compound C1=C(O)C=C2C(CCN)C=NC2=C1 OFCNTYBPPAQCRE-UHFFFAOYSA-N 0.000 description 1
- 102100027499 5-hydroxytryptamine receptor 1B Human genes 0.000 description 1
- 101710138639 5-hydroxytryptamine receptor 1B Proteins 0.000 description 1
- 102100036321 5-hydroxytryptamine receptor 2A Human genes 0.000 description 1
- 101710138091 5-hydroxytryptamine receptor 2A Proteins 0.000 description 1
- 102100040370 5-hydroxytryptamine receptor 5A Human genes 0.000 description 1
- 101710138069 5-hydroxytryptamine receptor 5A Proteins 0.000 description 1
- 101100455526 Drosophila melanogaster Lsd-2 gene Proteins 0.000 description 1
- 208000001640 Fibromyalgia Diseases 0.000 description 1
- 101000744211 Homo sapiens 5-hydroxytryptamine receptor 7 Proteins 0.000 description 1
- 208000019022 Mood disease Diseases 0.000 description 1
- 229940123445 Tricyclic antidepressant Drugs 0.000 description 1
- -1 Vivarint Chemical compound 0.000 description 1
- MOZPSIXKYJUTKI-RLXJOQACSA-N [1-[2-(methanesulfonamido)ethyl]piperidin-4-yl]methyl 1-(tritritiomethyl)indole-3-carboxylate Chemical compound C12=CC=CC=C2N(C([3H])([3H])[3H])C=C1C(=O)OCC1CCN(CCNS(C)(=O)=O)CC1 MOZPSIXKYJUTKI-RLXJOQACSA-N 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 230000008484 agonism Effects 0.000 description 1
- 230000001022 anti-muscarinic effect Effects 0.000 description 1
- 230000006399 behavior Effects 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 125000002619 bicyclic group Chemical group 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 231100000457 cardiotoxic Toxicity 0.000 description 1
- 230000001451 cardiotoxic effect Effects 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 210000004978 chinese hamster ovary cell Anatomy 0.000 description 1
- 230000003292 diminished effect Effects 0.000 description 1
- 230000003467 diminishing effect Effects 0.000 description 1
- 238000010494 dissociation reaction Methods 0.000 description 1
- 230000005593 dissociations Effects 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000002779 inactivation Effects 0.000 description 1
- 229960005417 ketanserin Drugs 0.000 description 1
- 150000002780 morpholines Chemical class 0.000 description 1
- 230000010004 neural pathway Effects 0.000 description 1
- 210000000118 neural pathway Anatomy 0.000 description 1
- 229960002748 norepinephrine Drugs 0.000 description 1
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 239000000902 placebo Substances 0.000 description 1
- 229940068196 placebo Drugs 0.000 description 1
- 239000002287 radioligand Substances 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 238000009738 saturating Methods 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 229940126570 serotonin reuptake inhibitor Drugs 0.000 description 1
- 239000003772 serotonin uptake inhibitor Substances 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 239000003029 tricyclic antidepressant agent Substances 0.000 description 1
- HDDNYFLPWFSBLN-ZSHCYNCHSA-N tropanyl 3,5-dimethylbenzoate Chemical compound O([C@H]1C[C@H]2CC[C@@H](C1)N2C)C(=O)C1=CC(C)=CC(C)=C1 HDDNYFLPWFSBLN-ZSHCYNCHSA-N 0.000 description 1
- 229960005014 viloxazine hydrochloride Drugs 0.000 description 1
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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17408409P | 2009-04-30 | 2009-04-30 | |
| US61/174,084 | 2009-04-30 | ||
| PCT/US2010/032974 WO2010127120A1 (en) | 2009-04-30 | 2010-04-29 | Method of treatment of depression |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2760527A1 true CA2760527A1 (en) | 2010-11-04 |
Family
ID=43032555
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2760527A Abandoned CA2760527A1 (en) | 2009-04-30 | 2010-04-29 | Method of treatment of depression |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20120115871A1 (https=) |
| EP (1) | EP2424539A4 (https=) |
| JP (2) | JP2012525426A (https=) |
| AU (1) | AU2010242971A1 (https=) |
| CA (1) | CA2760527A1 (https=) |
| CO (1) | CO6470848A2 (https=) |
| MX (1) | MX2011011579A (https=) |
| WO (1) | WO2010127120A1 (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2341912B1 (en) | 2008-09-05 | 2014-01-22 | Supernus Pharmaceuticals, Inc. | Method of treatment of attention deficit/hyperactivity disorder (adhd) |
| AU2013217013B2 (en) | 2012-02-08 | 2017-04-20 | Supernus Pharmaceuticals, Inc. | Modified release formulations of viloxazine |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4260606A (en) * | 1979-07-19 | 1981-04-07 | A. H. Robins Company, Inc. | 3-Methyleneazetidine derivatives |
| DE19830201A1 (de) * | 1998-07-07 | 2000-01-13 | Boehringer Ingelheim Pharma | Mittel mit antidepressiver Wirkung |
| WO2000006162A1 (de) * | 1998-07-27 | 2000-02-10 | Boehringer Ingelheim Pharma Kg | Mittel mit antidepressiver wirkung, mit pramipexol und einem weiteren antidepressivum |
| JP2004517112A (ja) * | 2001-01-02 | 2004-06-10 | ファルマシア・アンド・アップジョン・カンパニー | 新規薬物コンビネーション |
| AU2007260356B2 (en) * | 2006-06-16 | 2013-01-24 | H. Lundbeck A/S | Crystalline forms of 4- [2- (4-methylphenylsulfanyl) -phenyl] piperidine with combined serotonin and norepinephrine reuptake inhibition for the treatment of neuropathic pain |
| EP2341912B1 (en) * | 2008-09-05 | 2014-01-22 | Supernus Pharmaceuticals, Inc. | Method of treatment of attention deficit/hyperactivity disorder (adhd) |
-
2010
- 2010-04-29 JP JP2012508732A patent/JP2012525426A/ja active Pending
- 2010-04-29 WO PCT/US2010/032974 patent/WO2010127120A1/en not_active Ceased
- 2010-04-29 CA CA2760527A patent/CA2760527A1/en not_active Abandoned
- 2010-04-29 US US13/318,007 patent/US20120115871A1/en not_active Abandoned
- 2010-04-29 EP EP10770332A patent/EP2424539A4/en not_active Withdrawn
- 2010-04-29 MX MX2011011579A patent/MX2011011579A/es not_active Application Discontinuation
- 2010-04-29 AU AU2010242971A patent/AU2010242971A1/en not_active Abandoned
-
2011
- 2011-11-30 CO CO11165136A patent/CO6470848A2/es not_active Application Discontinuation
-
2014
- 2014-08-25 JP JP2014170572A patent/JP2014240417A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| MX2011011579A (es) | 2012-01-27 |
| WO2010127120A1 (en) | 2010-11-04 |
| AU2010242971A1 (en) | 2011-11-24 |
| JP2012525426A (ja) | 2012-10-22 |
| US20120115871A1 (en) | 2012-05-10 |
| EP2424539A4 (en) | 2012-09-19 |
| JP2014240417A (ja) | 2014-12-25 |
| EP2424539A1 (en) | 2012-03-07 |
| CO6470848A2 (es) | 2012-06-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20160429 |