AU2009256905A1 - 1-amino-alkylcyclohexane derivatives for the treatment of sleep disorders - Google Patents
1-amino-alkylcyclohexane derivatives for the treatment of sleep disorders Download PDFInfo
- Publication number
- AU2009256905A1 AU2009256905A1 AU2009256905A AU2009256905A AU2009256905A1 AU 2009256905 A1 AU2009256905 A1 AU 2009256905A1 AU 2009256905 A AU2009256905 A AU 2009256905A AU 2009256905 A AU2009256905 A AU 2009256905A AU 2009256905 A1 AU2009256905 A1 AU 2009256905A1
- Authority
- AU
- Australia
- Prior art keywords
- neramexane
- amino
- derivative
- administered
- tinnitus
- 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
- 208000019116 sleep disease Diseases 0.000 title claims description 42
- OGZQTTHDGQBLBT-UHFFFAOYSA-N neramexane Chemical group CC1(C)CC(C)(C)CC(C)(N)C1 OGZQTTHDGQBLBT-UHFFFAOYSA-N 0.000 claims description 104
- 229950004543 neramexane Drugs 0.000 claims description 98
- 208000009205 Tinnitus Diseases 0.000 claims description 85
- 231100000886 tinnitus Toxicity 0.000 claims description 78
- 239000003814 drug Substances 0.000 claims description 62
- CLUKHUGGXSIGRX-UHFFFAOYSA-N methanesulfonic acid;1,3,3,5,5-pentamethylcyclohexan-1-amine Chemical group CS(O)(=O)=O.CC1(C)CC(C)(C)CC(C)(N)C1 CLUKHUGGXSIGRX-UHFFFAOYSA-N 0.000 claims description 45
- 150000003839 salts Chemical class 0.000 claims description 40
- 239000000203 mixture Substances 0.000 claims description 35
- 238000009472 formulation Methods 0.000 claims description 17
- 208000012902 Nervous system disease Diseases 0.000 claims description 16
- 208000025966 Neurological disease Diseases 0.000 claims description 16
- 239000008194 pharmaceutical composition Substances 0.000 claims description 14
- 238000004448 titration Methods 0.000 claims description 14
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 11
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 10
- 239000008177 pharmaceutical agent Substances 0.000 claims description 8
- 239000003937 drug carrier Substances 0.000 claims description 7
- 230000002265 prevention Effects 0.000 claims description 7
- YJPIGAIKUZMOQA-UHFFFAOYSA-N Melatonin Natural products COC1=CC=C2N(C(C)=O)C=C(CCN)C2=C1 YJPIGAIKUZMOQA-UHFFFAOYSA-N 0.000 claims description 3
- 229940053999 hypnotics and sedatives melatonin receptor agonists Drugs 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 229960003987 melatonin Drugs 0.000 claims description 3
- DRLFMBDRBRZALE-UHFFFAOYSA-N melatonin Chemical compound COC1=CC=C2NC=C(CCNC(C)=O)C2=C1 DRLFMBDRBRZALE-UHFFFAOYSA-N 0.000 claims description 3
- 229940079593 drug Drugs 0.000 description 57
- 239000003826 tablet Substances 0.000 description 37
- 230000007958 sleep Effects 0.000 description 28
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 26
- 239000000902 placebo Substances 0.000 description 25
- 229940068196 placebo Drugs 0.000 description 25
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 21
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 21
- 230000008859 change Effects 0.000 description 17
- 230000002411 adverse Effects 0.000 description 16
- 201000010099 disease Diseases 0.000 description 15
- 238000000034 method Methods 0.000 description 12
- 230000000694 effects Effects 0.000 description 11
- 229940124301 concurrent medication Drugs 0.000 description 10
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 10
- 239000000243 solution Substances 0.000 description 10
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 9
- 238000004458 analytical method Methods 0.000 description 9
- 239000011248 coating agent Substances 0.000 description 9
- 150000001875 compounds Chemical class 0.000 description 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 8
- 239000004480 active ingredient Substances 0.000 description 8
- 238000000576 coating method Methods 0.000 description 8
- 230000006872 improvement Effects 0.000 description 8
- 238000012360 testing method Methods 0.000 description 8
- 239000013543 active substance Substances 0.000 description 7
- 230000037396 body weight Effects 0.000 description 7
- 239000002552 dosage form Substances 0.000 description 7
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 6
- 239000002775 capsule Substances 0.000 description 6
- 208000035475 disorder Diseases 0.000 description 6
- 230000007717 exclusion Effects 0.000 description 6
- 229920000159 gelatin Polymers 0.000 description 6
- 235000019322 gelatine Nutrition 0.000 description 6
- 239000004615 ingredient Substances 0.000 description 6
- 238000002347 injection Methods 0.000 description 6
- 239000007924 injection Substances 0.000 description 6
- 239000007788 liquid Substances 0.000 description 6
- 239000012669 liquid formulation Substances 0.000 description 6
- 238000002483 medication Methods 0.000 description 6
- 238000012552 review Methods 0.000 description 6
- 239000000454 talc Substances 0.000 description 6
- 235000012222 talc Nutrition 0.000 description 6
- 229910052623 talc Inorganic materials 0.000 description 6
- 239000011230 binding agent Substances 0.000 description 5
- 239000007884 disintegrant Substances 0.000 description 5
- 239000007941 film coated tablet Substances 0.000 description 5
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 5
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 5
- 239000000314 lubricant Substances 0.000 description 5
- 235000019359 magnesium stearate Nutrition 0.000 description 5
- 230000001225 therapeutic effect Effects 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- OVDULOGIHPNNKW-UHFFFAOYSA-N 1-(1,3,3,5,5-pentamethylcyclohexyl)pyrrolidine Chemical compound C1C(C)(C)CC(C)(C)CC1(C)N1CCCC1 OVDULOGIHPNNKW-UHFFFAOYSA-N 0.000 description 4
- GUBGYTABKSRVRQ-UHFFFAOYSA-N 2-(hydroxymethyl)-6-[4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol Chemical compound OCC1OC(OC2C(O)C(O)C(O)OC2CO)C(O)C(O)C1O GUBGYTABKSRVRQ-UHFFFAOYSA-N 0.000 description 4
- 229920002785 Croscarmellose sodium Polymers 0.000 description 4
- 241000124008 Mammalia Species 0.000 description 4
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 4
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 4
- 239000003795 chemical substances by application Substances 0.000 description 4
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 4
- 229960001681 croscarmellose sodium Drugs 0.000 description 4
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 4
- 238000011156 evaluation Methods 0.000 description 4
- 230000006870 function Effects 0.000 description 4
- 230000000670 limiting effect Effects 0.000 description 4
- 231100000252 nontoxic Toxicity 0.000 description 4
- 230000003000 nontoxic effect Effects 0.000 description 4
- 230000009467 reduction Effects 0.000 description 4
- 238000012216 screening Methods 0.000 description 4
- 208000022925 sleep disturbance Diseases 0.000 description 4
- 239000007787 solid Substances 0.000 description 4
- 238000000528 statistical test Methods 0.000 description 4
- 238000002560 therapeutic procedure Methods 0.000 description 4
- NBZGMQHFDNUNRQ-UHFFFAOYSA-N 3,3-diethyl-1,5,5-trimethylcyclohexan-1-amine Chemical compound CCC1(CC)CC(C)(C)CC(C)(N)C1 NBZGMQHFDNUNRQ-UHFFFAOYSA-N 0.000 description 3
- 108010010803 Gelatin Proteins 0.000 description 3
- 239000001828 Gelatine Substances 0.000 description 3
- 206010020559 Hyperacusis Diseases 0.000 description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 3
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 description 3
- 208000002193 Pain Diseases 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 239000002253 acid Substances 0.000 description 3
- 238000013459 approach Methods 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 230000004064 dysfunction Effects 0.000 description 3
- 235000019441 ethanol Nutrition 0.000 description 3
- 239000008273 gelatin Substances 0.000 description 3
- 235000011852 gelatine desserts Nutrition 0.000 description 3
- 239000008101 lactose Substances 0.000 description 3
- JVUYSNBGWFWRLJ-UHFFFAOYSA-N n-ethyl-1,3,3,5,5-pentamethylcyclohexan-1-amine Chemical compound CCNC1(C)CC(C)(C)CC(C)(C)C1 JVUYSNBGWFWRLJ-UHFFFAOYSA-N 0.000 description 3
- 208000004296 neuralgia Diseases 0.000 description 3
- 208000021722 neuropathic pain Diseases 0.000 description 3
- 229940100688 oral solution Drugs 0.000 description 3
- 229920000642 polymer Polymers 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 239000003755 preservative agent Substances 0.000 description 3
- 239000000651 prodrug Substances 0.000 description 3
- 229940002612 prodrug Drugs 0.000 description 3
- -1 semisolid Substances 0.000 description 3
- 239000012453 solvate Substances 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- 235000010356 sorbitol Nutrition 0.000 description 3
- 239000000600 sorbitol Substances 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 235000000346 sugar Nutrition 0.000 description 3
- 230000002459 sustained effect Effects 0.000 description 3
- 235000015112 vegetable and seed oil Nutrition 0.000 description 3
- 239000008158 vegetable oil Substances 0.000 description 3
- 239000003981 vehicle Substances 0.000 description 3
- PMNUOTQOFZGNNQ-UHFFFAOYSA-N 1,3,5-trimethylcyclohexan-1-amine Chemical compound CC1CC(C)CC(C)(N)C1 PMNUOTQOFZGNNQ-UHFFFAOYSA-N 0.000 description 2
- YKLPCZMZROZLJA-UHFFFAOYSA-N 1-ethyl-3,3,5,5-tetramethylcyclohexan-1-amine Chemical compound CCC1(N)CC(C)(C)CC(C)(C)C1 YKLPCZMZROZLJA-UHFFFAOYSA-N 0.000 description 2
- OMYKWZGACJRFAJ-UHFFFAOYSA-N 3,3,5,5-tetramethyl-1-propylcyclohexan-1-amine Chemical compound CCCC1(N)CC(C)(C)CC(C)(C)C1 OMYKWZGACJRFAJ-UHFFFAOYSA-N 0.000 description 2
- JINZKAFNDLFUEW-UHFFFAOYSA-N 3-ethyl-1,3,5,5-tetramethylcyclohexan-1-amine Chemical compound CCC1(C)CC(C)(C)CC(C)(N)C1 JINZKAFNDLFUEW-UHFFFAOYSA-N 0.000 description 2
- 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 description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
- 208000019901 Anxiety disease Diseases 0.000 description 2
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 2
- 206010008874 Chronic Fatigue Syndrome Diseases 0.000 description 2
- 229920002261 Corn starch Polymers 0.000 description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 2
- 208000007590 Disorders of Excessive Somnolence Diseases 0.000 description 2
- 208000001640 Fibromyalgia Diseases 0.000 description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 235000010643 Leucaena leucocephala Nutrition 0.000 description 2
- 240000007472 Leucaena leucocephala Species 0.000 description 2
- 229930195725 Mannitol Natural products 0.000 description 2
- 229940121723 Melatonin receptor agonist Drugs 0.000 description 2
- 229940127523 NMDA Receptor Antagonists Drugs 0.000 description 2
- 208000006199 Parasomnias Diseases 0.000 description 2
- 239000002202 Polyethylene glycol Substances 0.000 description 2
- 229920000954 Polyglycolide Polymers 0.000 description 2
- ZTHYODDOHIVTJV-UHFFFAOYSA-N Propyl gallate Chemical compound CCCOC(=O)C1=CC(O)=C(O)C(O)=C1 ZTHYODDOHIVTJV-UHFFFAOYSA-N 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- 229930006000 Sucrose Natural products 0.000 description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- 230000001154 acute effect Effects 0.000 description 2
- 239000000443 aerosol Substances 0.000 description 2
- 230000036506 anxiety Effects 0.000 description 2
- 230000037007 arousal Effects 0.000 description 2
- 210000003984 auditory pathway Anatomy 0.000 description 2
- 238000010241 blood sampling Methods 0.000 description 2
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 description 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 2
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 2
- 229940105329 carboxymethylcellulose Drugs 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- 235000010980 cellulose Nutrition 0.000 description 2
- 229920002678 cellulose Polymers 0.000 description 2
- 239000001913 cellulose Substances 0.000 description 2
- 239000011247 coating layer Substances 0.000 description 2
- 210000003477 cochlea Anatomy 0.000 description 2
- 239000003086 colorant Substances 0.000 description 2
- 238000007405 data analysis Methods 0.000 description 2
- 238000013461 design Methods 0.000 description 2
- 238000009792 diffusion process Methods 0.000 description 2
- 239000000796 flavoring agent Substances 0.000 description 2
- 235000013355 food flavoring agent Nutrition 0.000 description 2
- 235000003599 food sweetener Nutrition 0.000 description 2
- 239000007903 gelatin capsule Substances 0.000 description 2
- 150000004677 hydrates Chemical class 0.000 description 2
- 239000001257 hydrogen Substances 0.000 description 2
- 229910052739 hydrogen Inorganic materials 0.000 description 2
- 238000001802 infusion Methods 0.000 description 2
- 230000000977 initiatory effect Effects 0.000 description 2
- 206010022437 insomnia Diseases 0.000 description 2
- 238000007912 intraperitoneal administration Methods 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 238000012423 maintenance Methods 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 208000029766 myalgic encephalomeyelitis/chronic fatigue syndrome Diseases 0.000 description 2
- 210000000653 nervous system Anatomy 0.000 description 2
- 230000002981 neuropathic effect Effects 0.000 description 2
- 230000003287 optical effect Effects 0.000 description 2
- 239000003960 organic solvent Substances 0.000 description 2
- 230000036961 partial effect Effects 0.000 description 2
- 230000008447 perception Effects 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 230000036470 plasma concentration Effects 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 239000004633 polyglycolic acid Substances 0.000 description 2
- 229920001592 potato starch Polymers 0.000 description 2
- 230000002335 preservative effect Effects 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 230000002829 reductive effect Effects 0.000 description 2
- 230000013707 sensory perception of sound Effects 0.000 description 2
- 230000008667 sleep stage Effects 0.000 description 2
- 230000008454 sleep-wake cycle Effects 0.000 description 2
- 239000003381 stabilizer Substances 0.000 description 2
- 235000019698 starch Nutrition 0.000 description 2
- 238000007920 subcutaneous administration Methods 0.000 description 2
- 125000001424 substituent group Chemical group 0.000 description 2
- 229960004793 sucrose Drugs 0.000 description 2
- 239000000829 suppository Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 239000003765 sweetening agent Substances 0.000 description 2
- NEVCGYUBKUPZRL-UHFFFAOYSA-N (3,3,5,5-tetramethylcyclohexyl)methanamine Chemical compound CC1(C)CC(CN)CC(C)(C)C1 NEVCGYUBKUPZRL-UHFFFAOYSA-N 0.000 description 1
- DDMOUSALMHHKOS-UHFFFAOYSA-N 1,2-dichloro-1,1,2,2-tetrafluoroethane Chemical compound FC(F)(Cl)C(F)(F)Cl DDMOUSALMHHKOS-UHFFFAOYSA-N 0.000 description 1
- RTRXNNYIVXZLDQ-UHFFFAOYSA-N 1,3,3,5-tetramethyl-5-propylcyclohexan-1-amine Chemical compound CCCC1(C)CC(C)(C)CC(C)(N)C1 RTRXNNYIVXZLDQ-UHFFFAOYSA-N 0.000 description 1
- WCYNWVWYGZJUFX-UHFFFAOYSA-N 1,3,3,5-tetramethylcyclohexan-1-amine Chemical compound CC1CC(C)(C)CC(C)(N)C1 WCYNWVWYGZJUFX-UHFFFAOYSA-N 0.000 description 1
- WCBGLHDVUJFUDO-UHFFFAOYSA-N 1,3,3-trimethyl-5,5-dipropylcyclohexan-1-amine Chemical compound CCCC1(CCC)CC(C)(C)CC(C)(N)C1 WCBGLHDVUJFUDO-UHFFFAOYSA-N 0.000 description 1
- QTXWDXKTMLBHIW-UHFFFAOYSA-N 1,3,3-trimethylcyclohexan-1-amine Chemical compound CC1(C)CCCC(C)(N)C1 QTXWDXKTMLBHIW-UHFFFAOYSA-N 0.000 description 1
- BADMBUCXLGEWNJ-UHFFFAOYSA-N 1,3-dimethyl-3-propylcyclohexan-1-amine Chemical compound CCCC1(C)CCCC(C)(N)C1 BADMBUCXLGEWNJ-UHFFFAOYSA-N 0.000 description 1
- AEWYCWAJLDLBGX-UHFFFAOYSA-N 1-(1,3,3,5-tetramethylcyclohexyl)pyrrolidine Chemical compound C1C(C)CC(C)(C)CC1(C)N1CCCC1 AEWYCWAJLDLBGX-UHFFFAOYSA-N 0.000 description 1
- QVEQDLBYFRYKKW-UHFFFAOYSA-N 1-(1,3,5-trimethylcyclohexyl)pyrrolidine Chemical compound C1C(C)CC(C)CC1(C)N1CCCC1 QVEQDLBYFRYKKW-UHFFFAOYSA-N 0.000 description 1
- LODZBBPOQRJCTJ-UHFFFAOYSA-N 1-(3,3,5,5-tetramethyl-1-propylcyclohexyl)pyrrolidine Chemical compound C1CCCN1C1(CCC)CC(C)(C)CC(C)(C)C1 LODZBBPOQRJCTJ-UHFFFAOYSA-N 0.000 description 1
- JURFVVKQIRIWBJ-UHFFFAOYSA-N 1-(3,3-diethyl-1,5,5-trimethylcyclohexyl)pyrrolidine Chemical compound C1C(CC)(CC)CC(C)(C)CC1(C)N1CCCC1 JURFVVKQIRIWBJ-UHFFFAOYSA-N 0.000 description 1
- VZMMNFHWJMVOSI-UHFFFAOYSA-N 1-(3-ethyl-1,3,5,5-tetramethylcyclohexyl)pyrrolidine Chemical compound C1C(CC)(C)CC(C)(C)CC1(C)N1CCCC1 VZMMNFHWJMVOSI-UHFFFAOYSA-N 0.000 description 1
- OKMWKBLSFKFYGZ-UHFFFAOYSA-N 1-behenoylglycerol Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(O)CO OKMWKBLSFKFYGZ-UHFFFAOYSA-N 0.000 description 1
- YDBHSDRXUCPTQQ-UHFFFAOYSA-N 1-methylcyclohexan-1-amine Chemical compound CC1(N)CCCCC1 YDBHSDRXUCPTQQ-UHFFFAOYSA-N 0.000 description 1
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 1
- VCYIMJZEIXYSRU-UHFFFAOYSA-N 2-(1,3,3,5,5-pentamethylcyclohexyl)ethanamine Chemical compound CC1(C)CC(C)(C)CC(C)(CCN)C1 VCYIMJZEIXYSRU-UHFFFAOYSA-N 0.000 description 1
- OIHULWBOFIEYPQ-UHFFFAOYSA-N 2-(3,3,5,5-tetramethylcyclohexyl)ethanamine Chemical compound CC1(C)CC(CCN)CC(C)(C)C1 OIHULWBOFIEYPQ-UHFFFAOYSA-N 0.000 description 1
- KBPLVGBTXYNDFW-UHFFFAOYSA-N 3-ethyl-1,3-dimethylcyclohexan-1-amine Chemical compound CCC1(C)CCCC(C)(N)C1 KBPLVGBTXYNDFW-UHFFFAOYSA-N 0.000 description 1
- 244000215068 Acacia senegal Species 0.000 description 1
- 235000019489 Almond oil Nutrition 0.000 description 1
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 229920000945 Amylopectin Polymers 0.000 description 1
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 1
- 241000416162 Astragalus gummifer Species 0.000 description 1
- COVZYZSDYWQREU-UHFFFAOYSA-N Busulfan Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 description 1
- 239000004255 Butylated hydroxyanisole Substances 0.000 description 1
- 239000004322 Butylated hydroxytoluene Substances 0.000 description 1
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 description 1
- 208000000094 Chronic Pain Diseases 0.000 description 1
- 206010011903 Deafness traumatic Diseases 0.000 description 1
- 239000004338 Dichlorodifluoromethane Substances 0.000 description 1
- 208000030453 Drug-Related Side Effects and Adverse reaction Diseases 0.000 description 1
- 241000792859 Enema Species 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- RRHGJUQNOFWUDK-UHFFFAOYSA-N Isoprene Chemical compound CC(=C)C=C RRHGJUQNOFWUDK-UHFFFAOYSA-N 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
- 235000019759 Maize starch Nutrition 0.000 description 1
- 102000001419 Melatonin receptor Human genes 0.000 description 1
- 108050009605 Melatonin receptor Proteins 0.000 description 1
- 244000246386 Mentha pulegium Species 0.000 description 1
- 235000016257 Mentha pulegium Nutrition 0.000 description 1
- 235000004357 Mentha x piperita Nutrition 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- YLXDSYKOBKBWJQ-LBPRGKRZSA-N N-[2-[(8S)-2,6,7,8-tetrahydro-1H-cyclopenta[e]benzofuran-8-yl]ethyl]propanamide Chemical compound C1=C2OCCC2=C2[C@H](CCNC(=O)CC)CCC2=C1 YLXDSYKOBKBWJQ-LBPRGKRZSA-N 0.000 description 1
- 229940123859 Nicotinic receptor antagonist Drugs 0.000 description 1
- 208000002946 Noise-Induced Hearing Loss Diseases 0.000 description 1
- 239000005662 Paraffin oil Substances 0.000 description 1
- 235000019483 Peanut oil Nutrition 0.000 description 1
- 229920001710 Polyorthoester Polymers 0.000 description 1
- 206010062519 Poor quality sleep Diseases 0.000 description 1
- 208000005793 Restless legs syndrome Diseases 0.000 description 1
- 206010038743 Restlessness Diseases 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
- 239000004141 Sodium laurylsulphate Substances 0.000 description 1
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 description 1
- 229920001615 Tragacanth Polymers 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- YJYPHIXNFHFHND-UHFFFAOYSA-N agomelatine Chemical compound C1=CC=C(CCNC(C)=O)C2=CC(OC)=CC=C21 YJYPHIXNFHFHND-UHFFFAOYSA-N 0.000 description 1
- 229960002629 agomelatine Drugs 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 239000008168 almond oil Substances 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 239000003420 antiserotonin agent Substances 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 238000012076 audiometry Methods 0.000 description 1
- 210000003926 auditory cortex Anatomy 0.000 description 1
- 239000012752 auxiliary agent Substances 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid group Chemical group C(C1=CC=CC=C1)(=O)O WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 230000002146 bilateral effect Effects 0.000 description 1
- 238000012742 biochemical analysis Methods 0.000 description 1
- 229920000249 biocompatible polymer Polymers 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 229920001400 block copolymer Polymers 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000008499 blood brain barrier function Effects 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 210000001218 blood-brain barrier Anatomy 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000000337 buffer salt Substances 0.000 description 1
- 239000006172 buffering agent Substances 0.000 description 1
- 235000019282 butylated hydroxyanisole Nutrition 0.000 description 1
- 235000010354 butylated hydroxytoluene Nutrition 0.000 description 1
- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 description 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
- 235000013539 calcium stearate Nutrition 0.000 description 1
- 239000008116 calcium stearate Substances 0.000 description 1
- 229940078456 calcium stearate Drugs 0.000 description 1
- 235000011132 calcium sulphate Nutrition 0.000 description 1
- 239000001569 carbon dioxide Substances 0.000 description 1
- 229910002092 carbon dioxide Inorganic materials 0.000 description 1
- 229960004424 carbon dioxide Drugs 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 208000022371 chronic pain syndrome Diseases 0.000 description 1
- 229960004106 citric acid Drugs 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 238000011970 concomitant therapy Methods 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 230000001054 cortical effect Effects 0.000 description 1
- WZHCOOQXZCIUNC-UHFFFAOYSA-N cyclandelate Chemical compound C1C(C)(C)CC(C)CC1OC(=O)C(O)C1=CC=CC=C1 WZHCOOQXZCIUNC-UHFFFAOYSA-N 0.000 description 1
- PAFZNILMFXTMIY-UHFFFAOYSA-N cyclohexylamine Chemical class NC1CCCCC1 PAFZNILMFXTMIY-UHFFFAOYSA-N 0.000 description 1
- HCAJEUSONLESMK-UHFFFAOYSA-N cyclohexylsulfamic acid Chemical compound OS(=O)(=O)NC1CCCCC1 HCAJEUSONLESMK-UHFFFAOYSA-N 0.000 description 1
- 230000006735 deficit Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 235000019700 dicalcium phosphate Nutrition 0.000 description 1
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 description 1
- 235000019404 dichlorodifluoromethane Nutrition 0.000 description 1
- 229940042935 dichlorodifluoromethane Drugs 0.000 description 1
- 229940087091 dichlorotetrafluoroethane Drugs 0.000 description 1
- 235000013681 dietary sucrose Nutrition 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 238000009510 drug design Methods 0.000 description 1
- 210000005069 ears Anatomy 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 239000007920 enema Substances 0.000 description 1
- 229940079360 enema for constipation Drugs 0.000 description 1
- 230000007613 environmental effect Effects 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 description 1
- 230000005713 exacerbation Effects 0.000 description 1
- 230000009540 excitatory neurotransmission Effects 0.000 description 1
- 239000003925 fat Substances 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 239000007789 gas Substances 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 235000001727 glucose Nutrition 0.000 description 1
- 229930195712 glutamate Natural products 0.000 description 1
- 229940049654 glyceryl behenate Drugs 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 210000003128 head Anatomy 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 235000001050 hortel pimenta Nutrition 0.000 description 1
- 239000000017 hydrogel Substances 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 230000009539 inhibitory neurotransmission Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000000185 intracerebroventricular administration Methods 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 239000010410 layer Substances 0.000 description 1
- 239000000787 lecithin Substances 0.000 description 1
- 235000010445 lecithin Nutrition 0.000 description 1
- 229940067606 lecithin Drugs 0.000 description 1
- 231100000518 lethal Toxicity 0.000 description 1
- 230000001665 lethal effect Effects 0.000 description 1
- 210000003715 limbic system Anatomy 0.000 description 1
- 239000008297 liquid dosage form Substances 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 230000007257 malfunction Effects 0.000 description 1
- 230000000873 masking effect Effects 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000003094 microcapsule Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 239000004005 microsphere Substances 0.000 description 1
- 239000002480 mineral oil Substances 0.000 description 1
- 235000010446 mineral oil Nutrition 0.000 description 1
- 239000007912 modified release tablet Substances 0.000 description 1
- RUUUZPJNWLBOMQ-UHFFFAOYSA-N n,1,3,3,5,5-hexamethylcyclohexan-1-amine Chemical compound CNC1(C)CC(C)(C)CC(C)(C)C1 RUUUZPJNWLBOMQ-UHFFFAOYSA-N 0.000 description 1
- GOLVFRNKGGSJRP-UHFFFAOYSA-N n,n,1,3,3,5,5-heptamethylcyclohexan-1-amine Chemical compound CN(C)C1(C)CC(C)(C)CC(C)(C)C1 GOLVFRNKGGSJRP-UHFFFAOYSA-N 0.000 description 1
- 239000006199 nebulizer Substances 0.000 description 1
- 230000000926 neurological effect Effects 0.000 description 1
- 210000002569 neuron Anatomy 0.000 description 1
- 230000006764 neuronal dysfunction Effects 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 239000003367 nicotinic antagonist Substances 0.000 description 1
- 239000002687 nonaqueous vehicle Substances 0.000 description 1
- 239000000820 nonprescription drug Substances 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 230000008506 pathogenesis Effects 0.000 description 1
- 230000007310 pathophysiology Effects 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 239000007967 peppermint flavor Substances 0.000 description 1
- 230000000737 periodic effect Effects 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 239000003208 petroleum Substances 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 229920000747 poly(lactic acid) Polymers 0.000 description 1
- 229920001610 polycaprolactone Polymers 0.000 description 1
- 229920002721 polycyanoacrylate Polymers 0.000 description 1
- 239000004626 polylactic acid Substances 0.000 description 1
- 229920006324 polyoxymethylene Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 210000002442 prefrontal cortex Anatomy 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 239000003380 propellant Substances 0.000 description 1
- 239000000473 propyl gallate Substances 0.000 description 1
- 235000010388 propyl gallate Nutrition 0.000 description 1
- 229940075579 propyl gallate Drugs 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 229960001150 ramelteon Drugs 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 229940121356 serotonin receptor antagonist Drugs 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 238000009097 single-agent therapy Methods 0.000 description 1
- 208000019830 sleep disorder, initiating and maintaining sleep Diseases 0.000 description 1
- 235000010378 sodium ascorbate Nutrition 0.000 description 1
- PPASLZSBLFJQEF-RKJRWTFHSA-M sodium ascorbate Substances [Na+].OC[C@@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RKJRWTFHSA-M 0.000 description 1
- 229960005055 sodium ascorbate Drugs 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 description 1
- 239000008109 sodium starch glycolate Substances 0.000 description 1
- 229940079832 sodium starch glycolate Drugs 0.000 description 1
- 229920003109 sodium starch glycolate Polymers 0.000 description 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 description 1
- PPASLZSBLFJQEF-RXSVEWSESA-M sodium-L-ascorbate Chemical compound [Na+].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RXSVEWSESA-M 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
- 235000012424 soybean oil Nutrition 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 229940032147 starch Drugs 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 238000012916 structural analysis Methods 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 231100001274 therapeutic index Toxicity 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- 235000010215 titanium dioxide Nutrition 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 235000010487 tragacanth Nutrition 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 1
- 229940029284 trichlorofluoromethane Drugs 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- 239000000080 wetting agent Substances 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
- A61K31/13—Amines
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- 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)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Anesthesiology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13178908P | 2008-06-12 | 2008-06-12 | |
| EP08010749 | 2008-06-12 | ||
| US61/131,789 | 2008-06-12 | ||
| EP08010749.3 | 2008-06-12 | ||
| PCT/EP2009/004184 WO2009149920A1 (en) | 2008-06-12 | 2009-06-10 | 1-amino-alkylcyclohexane derivatives for the treatment of sleep disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU2009256905A1 true AU2009256905A1 (en) | 2009-12-17 |
Family
ID=39721946
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2009256905A Abandoned AU2009256905A1 (en) | 2008-06-12 | 2009-06-10 | 1-amino-alkylcyclohexane derivatives for the treatment of sleep disorders |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20110207793A1 (enExample) |
| EP (1) | EP2315586A1 (enExample) |
| JP (1) | JP5923305B2 (enExample) |
| KR (1) | KR20110005909A (enExample) |
| CN (1) | CN102026633A (enExample) |
| AR (1) | AR074246A1 (enExample) |
| AU (1) | AU2009256905A1 (enExample) |
| BR (1) | BRPI0911920A2 (enExample) |
| CA (1) | CA2722763A1 (enExample) |
| IL (1) | IL209417A0 (enExample) |
| MX (1) | MX2010013450A (enExample) |
| RU (1) | RU2010154623A (enExample) |
| TW (1) | TW201010691A (enExample) |
| WO (1) | WO2009149920A1 (enExample) |
| ZA (1) | ZA201007763B (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20100052558A (ko) * | 2007-09-12 | 2010-05-19 | 메르츠 파마 게엠베하 운트 코. 카가아 | 네라멕산을 위한 적정 패키지 및 내이 질환의 치료에서의 그의 용도 |
| US20110294890A1 (en) * | 2010-05-28 | 2011-12-01 | Merz Pharma Gmbh & Co. Kgaa | Neramexane for the treatment or prevention of inner ear disorders |
| WO2015166918A1 (ja) * | 2014-04-28 | 2015-11-05 | 杏林製薬株式会社 | 耳鳴患者の治療用の薬剤 |
| CN113274365B (zh) * | 2021-07-22 | 2021-10-22 | 广东科泰鼎润药业科技有限公司 | 雷美替胺速释缓释双释放制剂及其制备方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19528388A1 (de) * | 1995-08-02 | 1997-02-06 | Hans Peter Prof Dr Med Zenner | Verwendung von Adamantan-Derivaten zur Behandlung von Erkrankungen des Innenohrs |
| US6071966A (en) * | 1997-06-30 | 2000-06-06 | Merz + Co. Gmbh & Co. | 1-amino-alkylcyclohexane NMDA receptor antagonists |
| ES2200358T3 (es) * | 1997-06-30 | 2004-03-01 | MERZ PHARMA GMBH & CO. KGAA | 1-amino-alquilciclohexanos antagonistas del receptor de nmda. |
| AU2003274353B2 (en) * | 2002-10-24 | 2007-04-05 | Merz Pharma Gmbh & Co. Kgaa | Combination therapy using 1-aminocyclohexane derivatives and acetylcholinesterase inhibitors |
| US20070141148A1 (en) * | 2005-11-30 | 2007-06-21 | Merz Pharma Gmbh & Co. Kgaa | Neramexane MR matrix tablet |
| JP2007246507A (ja) * | 2006-02-15 | 2007-09-27 | Kracie Seiyaku Kk | 疲労の予防・治療組成物及び予防・治療方法 |
| DE102006011922A1 (de) * | 2006-03-15 | 2007-09-20 | Uwe Stoldt | Mittel zur Behandlung von Tinnitus |
-
2009
- 2009-06-09 TW TW098119212A patent/TW201010691A/zh unknown
- 2009-06-10 CA CA2722763A patent/CA2722763A1/en not_active Abandoned
- 2009-06-10 RU RU2010154623/15A patent/RU2010154623A/ru not_active Application Discontinuation
- 2009-06-10 EP EP09761483A patent/EP2315586A1/en not_active Withdrawn
- 2009-06-10 KR KR1020107027774A patent/KR20110005909A/ko not_active Ceased
- 2009-06-10 US US12/737,092 patent/US20110207793A1/en not_active Abandoned
- 2009-06-10 CN CN2009801170115A patent/CN102026633A/zh active Pending
- 2009-06-10 MX MX2010013450A patent/MX2010013450A/es unknown
- 2009-06-10 WO PCT/EP2009/004184 patent/WO2009149920A1/en not_active Ceased
- 2009-06-10 JP JP2011512891A patent/JP5923305B2/ja not_active Expired - Fee Related
- 2009-06-10 AU AU2009256905A patent/AU2009256905A1/en not_active Abandoned
- 2009-06-10 BR BRPI0911920A patent/BRPI0911920A2/pt not_active IP Right Cessation
- 2009-06-12 AR ARP090102149A patent/AR074246A1/es not_active Application Discontinuation
-
2010
- 2010-10-29 ZA ZA2010/07763A patent/ZA201007763B/en unknown
- 2010-11-18 IL IL209417A patent/IL209417A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RU2010154623A (ru) | 2012-08-10 |
| MX2010013450A (es) | 2011-02-23 |
| CN102026633A (zh) | 2011-04-20 |
| ZA201007763B (en) | 2011-07-27 |
| IL209417A0 (en) | 2011-01-31 |
| AR074246A1 (es) | 2011-01-05 |
| TW201010691A (en) | 2010-03-16 |
| JP2011522850A (ja) | 2011-08-04 |
| JP5923305B2 (ja) | 2016-05-24 |
| KR20110005909A (ko) | 2011-01-19 |
| WO2009149920A1 (en) | 2009-12-17 |
| CA2722763A1 (en) | 2009-12-17 |
| BRPI0911920A2 (pt) | 2015-10-06 |
| EP2315586A1 (en) | 2011-05-04 |
| US20110207793A1 (en) | 2011-08-25 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2008298015B2 (en) | Interval therapy for the treatment of tinnitus | |
| AU2009256905A1 (en) | 1-amino-alkylcyclohexane derivatives for the treatment of sleep disorders | |
| US20110178179A1 (en) | 1-amino-alkylcyclohexane derivatives for the treatment of cognitive impairment in tinnitus | |
| WO2011147589A1 (en) | Neramexane for the treatment or prevention of inner ear disorders | |
| RU2446794C2 (ru) | Терапия с интервалами для лечения тиннитуса | |
| HK1154791A (en) | 1-amino-alkylcyclohexane derivatives for the treatment of sleep disorders |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MK4 | Application lapsed section 142(2)(d) - no continuation fee paid for the application |