ES2237188T3 - Composiciones de desmetilolanzapina y metodos. - Google Patents
Composiciones de desmetilolanzapina y metodos.Info
- Publication number
- ES2237188T3 ES2237188T3 ES99960547T ES99960547T ES2237188T3 ES 2237188 T3 ES2237188 T3 ES 2237188T3 ES 99960547 T ES99960547 T ES 99960547T ES 99960547 T ES99960547 T ES 99960547T ES 2237188 T3 ES2237188 T3 ES 2237188T3
- Authority
- ES
- Spain
- Prior art keywords
- desmethylolanzapine
- salt
- treatment
- disorder
- pharmaceutically acceptable
- 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.)
- Expired - Lifetime
Links
- 239000000203 mixture Substances 0.000 title description 19
- 238000000034 method Methods 0.000 title description 8
- 239000003814 drug Substances 0.000 claims abstract description 36
- FHPIXVHJEIZKJW-UHFFFAOYSA-N 4'-N-desmethylolanzapine Chemical compound S1C(C)=CC2=C1NC1=CC=CC=C1N=C2N1CCNCC1 FHPIXVHJEIZKJW-UHFFFAOYSA-N 0.000 claims abstract description 35
- 238000011282 treatment Methods 0.000 claims abstract description 28
- 150000003839 salts Chemical class 0.000 claims abstract description 27
- 208000028017 Psychotic disease Diseases 0.000 claims abstract description 15
- 238000004519 manufacturing process Methods 0.000 claims abstract description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 26
- 229940079593 drug Drugs 0.000 claims description 26
- 208000035475 disorder Diseases 0.000 claims description 22
- 208000019901 Anxiety disease Diseases 0.000 claims description 14
- 150000001875 compounds Chemical class 0.000 claims description 10
- 239000002775 capsule Substances 0.000 claims description 9
- 208000024891 symptom Diseases 0.000 claims description 9
- 208000020925 Bipolar disease Diseases 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 230000016571 aggressive behavior Effects 0.000 claims description 7
- 230000001079 digestive effect Effects 0.000 claims description 7
- 206010026749 Mania Diseases 0.000 claims description 6
- 230000036506 anxiety Effects 0.000 claims description 6
- 201000000980 schizophrenia Diseases 0.000 claims description 6
- 201000009032 substance abuse Diseases 0.000 claims description 6
- 231100000736 substance abuse Toxicity 0.000 claims description 6
- 208000011117 substance-related disease Diseases 0.000 claims description 6
- 208000020706 Autistic disease Diseases 0.000 claims description 5
- 206010017543 Fungal skin infection Diseases 0.000 claims description 5
- 239000000126 substance Substances 0.000 claims description 5
- AHOUBRCZNHFOSL-YOEHRIQHSA-N (+)-Casbol Chemical compound C1=CC(F)=CC=C1[C@H]1[C@H](COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-YOEHRIQHSA-N 0.000 claims description 4
- 229960004038 fluvoxamine Drugs 0.000 claims description 4
- CJOFXWAVKWHTFT-XSFVSMFZSA-N fluvoxamine Chemical compound COCCCC\C(=N/OCCN)C1=CC=C(C(F)(F)F)C=C1 CJOFXWAVKWHTFT-XSFVSMFZSA-N 0.000 claims description 4
- 229960002296 paroxetine Drugs 0.000 claims description 4
- -1 sertaline Chemical compound 0.000 claims description 4
- PNVNVHUZROJLTJ-UHFFFAOYSA-N venlafaxine Chemical compound C1=CC(OC)=CC=C1C(CN(C)C)C1(O)CCCCC1 PNVNVHUZROJLTJ-UHFFFAOYSA-N 0.000 claims description 4
- RTHCYVBBDHJXIQ-MRXNPFEDSA-N (R)-fluoxetine Chemical compound O([C@H](CCNC)C=1C=CC=CC=1)C1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-MRXNPFEDSA-N 0.000 claims description 3
- AHOUBRCZNHFOSL-UHFFFAOYSA-N Paroxetine hydrochloride Natural products C1=CC(F)=CC=C1C1C(COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-UHFFFAOYSA-N 0.000 claims description 3
- 229960002464 fluoxetine Drugs 0.000 claims description 3
- 239000003112 inhibitor Substances 0.000 claims description 3
- 229960001800 nefazodone Drugs 0.000 claims description 3
- VRBKIVRKKCLPHA-UHFFFAOYSA-N nefazodone Chemical compound O=C1N(CCOC=2C=CC=CC=2)C(CC)=NN1CCCN(CC1)CCN1C1=CC=CC(Cl)=C1 VRBKIVRKKCLPHA-UHFFFAOYSA-N 0.000 claims description 3
- 229940124834 selective serotonin reuptake inhibitor Drugs 0.000 claims description 3
- 239000012896 selective serotonin reuptake inhibitor Substances 0.000 claims description 3
- 238000002560 therapeutic procedure Methods 0.000 claims description 3
- 229960004688 venlafaxine Drugs 0.000 claims description 3
- 206010002859 Anxiety disorder due to a general medical condition Diseases 0.000 claims description 2
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims description 2
- 208000013403 hyperactivity Diseases 0.000 claims description 2
- 208000011688 Generalised anxiety disease Diseases 0.000 claims 1
- 241001276587 Tonina Species 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 208000029364 generalized anxiety disease Diseases 0.000 claims 1
- 208000028173 post-traumatic stress disease Diseases 0.000 claims 1
- KVWDHTXUZHCGIO-UHFFFAOYSA-N olanzapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 KVWDHTXUZHCGIO-UHFFFAOYSA-N 0.000 description 20
- 229960005017 olanzapine Drugs 0.000 description 18
- 239000003826 tablet Substances 0.000 description 12
- 230000014509 gene expression Effects 0.000 description 11
- 230000000694 effects Effects 0.000 description 10
- 239000004480 active ingredient Substances 0.000 description 7
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 description 6
- 239000004615 ingredient Substances 0.000 description 6
- 239000007788 liquid Substances 0.000 description 6
- 208000008234 Tics Diseases 0.000 description 5
- 239000003795 chemical substances by application Substances 0.000 description 5
- 239000008187 granular material Substances 0.000 description 5
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 description 4
- 102000008144 Cytochrome P-450 CYP1A2 Human genes 0.000 description 4
- 108010074922 Cytochrome P-450 CYP1A2 Proteins 0.000 description 4
- 108010010803 Gelatin Proteins 0.000 description 4
- 230000002411 adverse Effects 0.000 description 4
- 229920000159 gelatin Polymers 0.000 description 4
- 239000008273 gelatin Substances 0.000 description 4
- 235000019322 gelatine Nutrition 0.000 description 4
- 235000011852 gelatine desserts Nutrition 0.000 description 4
- 239000002207 metabolite Substances 0.000 description 4
- 230000004044 response Effects 0.000 description 4
- 208000013716 Motor tics 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
- 230000001684 chronic effect Effects 0.000 description 3
- 230000003993 interaction Effects 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 239000007905 soft elastic gelatin capsule Substances 0.000 description 3
- 208000004998 Abdominal Pain Diseases 0.000 description 2
- 206010010774 Constipation Diseases 0.000 description 2
- 206010011224 Cough Diseases 0.000 description 2
- 208000005038 Cytochrome P-450 CYP1A2 Inducers Diseases 0.000 description 2
- 206010013710 Drug interaction Diseases 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 208000013717 Phonic tics Diseases 0.000 description 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 description 2
- 150000007513 acids Chemical class 0.000 description 2
- 230000000561 anti-psychotic effect Effects 0.000 description 2
- 238000003556 assay Methods 0.000 description 2
- 239000011230 binding agent Substances 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 230000000747 cardiac effect Effects 0.000 description 2
- MYSWGUAQZAJSOK-UHFFFAOYSA-N ciprofloxacin Chemical compound C12=CC(N3CCNCC3)=C(F)C=C2C(=O)C(C(=O)O)=CN1C1CC1 MYSWGUAQZAJSOK-UHFFFAOYSA-N 0.000 description 2
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 description 2
- 230000013872 defecation Effects 0.000 description 2
- 230000017858 demethylation Effects 0.000 description 2
- 238000010520 demethylation reaction Methods 0.000 description 2
- 230000003001 depressive effect Effects 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 239000006185 dispersion Substances 0.000 description 2
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 230000035873 hypermotility Effects 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 208000002551 irritable bowel syndrome Diseases 0.000 description 2
- 210000004185 liver Anatomy 0.000 description 2
- 239000000314 lubricant Substances 0.000 description 2
- 230000002503 metabolic effect Effects 0.000 description 2
- 230000004060 metabolic process Effects 0.000 description 2
- 238000000465 moulding Methods 0.000 description 2
- 230000001575 pathological effect Effects 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- JTJMJGYZQZDUJJ-UHFFFAOYSA-N phencyclidine Chemical compound C1CCCCN1C1(C=2C=CC=CC=2)CCCCC1 JTJMJGYZQZDUJJ-UHFFFAOYSA-N 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000004094 surface-active agent Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 231100001274 therapeutic index Toxicity 0.000 description 2
- 208000016686 tic disease Diseases 0.000 description 2
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 description 1
- LDCYZAJDBXYCGN-VIFPVBQESA-N 5-hydroxy-L-tryptophan Chemical compound C1=C(O)C=C2C(C[C@H](N)C(O)=O)=CNC2=C1 LDCYZAJDBXYCGN-VIFPVBQESA-N 0.000 description 1
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 description 1
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 description 1
- 229940000681 5-hydroxytryptophan Drugs 0.000 description 1
- 206010000060 Abdominal distension Diseases 0.000 description 1
- 108060003345 Adrenergic Receptor Proteins 0.000 description 1
- 102000017910 Adrenergic receptor Human genes 0.000 description 1
- 206010001497 Agitation Diseases 0.000 description 1
- 201000009487 Amblyopia Diseases 0.000 description 1
- COVZYZSDYWQREU-UHFFFAOYSA-N Busulfan Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 description 1
- 244000025254 Cannabis sativa Species 0.000 description 1
- 235000012766 Cannabis sativa ssp. sativa var. sativa Nutrition 0.000 description 1
- 235000012765 Cannabis sativa ssp. sativa var. spontanea Nutrition 0.000 description 1
- 206010010144 Completed suicide Diseases 0.000 description 1
- 206010010964 Coprolalia Diseases 0.000 description 1
- 229920002785 Croscarmellose sodium Polymers 0.000 description 1
- 208000006104 Cytochrome P-450 CYP1A2 Inhibitors Diseases 0.000 description 1
- 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 1
- 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 1
- 101150049660 DRD2 gene Proteins 0.000 description 1
- 108050004812 Dopamine receptor Proteins 0.000 description 1
- 102000015554 Dopamine receptor Human genes 0.000 description 1
- 208000000059 Dyspnea Diseases 0.000 description 1
- 206010013975 Dyspnoeas Diseases 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 229920003136 Eudragit® L polymer Polymers 0.000 description 1
- 229920003137 Eudragit® S polymer Polymers 0.000 description 1
- LFMYNZPAVPMEGP-PIDGMYBPSA-N Fluvoxamine maleate Chemical compound OC(=O)\C=C/C(O)=O.COCCCC\C(=N/OCCN)C1=CC=C(C(F)(F)F)C=C1 LFMYNZPAVPMEGP-PIDGMYBPSA-N 0.000 description 1
- 208000014540 Functional gastrointestinal disease Diseases 0.000 description 1
- 208000018522 Gastrointestinal disease Diseases 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- 208000000857 Hepatic Insufficiency Diseases 0.000 description 1
- 206010019663 Hepatic failure Diseases 0.000 description 1
- 208000008454 Hyperhidrosis Diseases 0.000 description 1
- 108010044467 Isoenzymes Proteins 0.000 description 1
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
- 206010027514 Metrorrhagia Diseases 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 206010028629 Myoglobinuria Diseases 0.000 description 1
- RTHCYVBBDHJXIQ-UHFFFAOYSA-N N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine Chemical compound C=1C=CC=CC=1C(CCNC)OC1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-UHFFFAOYSA-N 0.000 description 1
- 206010028813 Nausea Diseases 0.000 description 1
- 206010029216 Nervousness Diseases 0.000 description 1
- 206010031127 Orthostatic hypotension Diseases 0.000 description 1
- 208000027089 Parkinsonian disease Diseases 0.000 description 1
- 206010034010 Parkinsonism Diseases 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 206010036618 Premenstrual syndrome Diseases 0.000 description 1
- 208000001647 Renal Insufficiency Diseases 0.000 description 1
- 206010038583 Repetitive speech Diseases 0.000 description 1
- 206010039020 Rhabdomyolysis Diseases 0.000 description 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 1
- 206010041349 Somnolence Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 208000013200 Stress disease Diseases 0.000 description 1
- 208000001871 Tachycardia Diseases 0.000 description 1
- 208000000323 Tourette Syndrome Diseases 0.000 description 1
- 208000016620 Tourette disease Diseases 0.000 description 1
- 206010044565 Tremor Diseases 0.000 description 1
- 206010046543 Urinary incontinence Diseases 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- 230000001133 acceleration Effects 0.000 description 1
- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 238000013019 agitation Methods 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 230000008485 antagonism Effects 0.000 description 1
- 239000003242 anti bacterial agent Substances 0.000 description 1
- 229940088710 antibiotic agent Drugs 0.000 description 1
- 239000000164 antipsychotic agent Substances 0.000 description 1
- VMWNQDUVQKEIOC-CYBMUJFWSA-N apomorphine Chemical compound C([C@H]1N(C)CC2)C3=CC=C(O)C(O)=C3C3=C1C2=CC=C3 VMWNQDUVQKEIOC-CYBMUJFWSA-N 0.000 description 1
- 229960004046 apomorphine Drugs 0.000 description 1
- 206010003119 arrhythmia Diseases 0.000 description 1
- 230000002763 arrhythmic effect Effects 0.000 description 1
- 206010003549 asthenia Diseases 0.000 description 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 description 1
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 description 1
- 229940049706 benzodiazepine Drugs 0.000 description 1
- 150000001557 benzodiazepines Chemical class 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
- 208000028683 bipolar I disease Diseases 0.000 description 1
- 208000024330 bloating Diseases 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000036765 blood level Effects 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 229960003405 ciprofloxacin Drugs 0.000 description 1
- 229960003920 cocaine Drugs 0.000 description 1
- 230000006957 competitive inhibition Effects 0.000 description 1
- 239000007891 compressed tablet Substances 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 230000001143 conditioned effect Effects 0.000 description 1
- 230000008602 contraction Effects 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 229960005168 croscarmellose Drugs 0.000 description 1
- 239000001767 crosslinked sodium carboxy methyl cellulose Substances 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
- 230000007423 decrease Effects 0.000 description 1
- 208000013219 diaphoresis Diseases 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 229960003638 dopamine Drugs 0.000 description 1
- 206010013781 dry mouth Diseases 0.000 description 1
- 229940098766 effexor Drugs 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 239000002702 enteric coating Substances 0.000 description 1
- 238000009505 enteric coating Methods 0.000 description 1
- 206010015037 epilepsy Diseases 0.000 description 1
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
- 230000001815 facial effect Effects 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000002538 fungal effect Effects 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- 150000002334 glycols Chemical class 0.000 description 1
- 230000021061 grooming behavior Effects 0.000 description 1
- 239000000380 hallucinogen Substances 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 208000006750 hematuria Diseases 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 239000003701 inert diluent Substances 0.000 description 1
- 206010022000 influenza Diseases 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 206010022437 insomnia Diseases 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 230000001788 irregular Effects 0.000 description 1
- 201000006370 kidney failure Diseases 0.000 description 1
- 230000003908 liver function Effects 0.000 description 1
- 229940009622 luvox Drugs 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 239000007932 molded tablet Substances 0.000 description 1
- 210000003097 mucus Anatomy 0.000 description 1
- 230000003551 muscarinic effect Effects 0.000 description 1
- 230000008693 nausea Effects 0.000 description 1
- DYCKFEBIOUQECE-UHFFFAOYSA-N nefazodone hydrochloride Chemical compound [H+].[Cl-].O=C1N(CCOC=2C=CC=CC=2)C(CC)=NN1CCCN(CC1)CCN1C1=CC=CC(Cl)=C1 DYCKFEBIOUQECE-UHFFFAOYSA-N 0.000 description 1
- 229960002715 nicotine Drugs 0.000 description 1
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- LDCYZAJDBXYCGN-UHFFFAOYSA-N oxitriptan Natural products C1=C(O)C=C2C(CC(N)C(O)=O)=CNC2=C1 LDCYZAJDBXYCGN-UHFFFAOYSA-N 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 238000001050 pharmacotherapy Methods 0.000 description 1
- 229950010883 phencyclidine Drugs 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 229920000058 polyacrylate Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920005862 polyol Polymers 0.000 description 1
- 150000003077 polyols Chemical class 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 229940068965 polysorbates Drugs 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 229940035613 prozac Drugs 0.000 description 1
- 230000001337 psychedelic effect Effects 0.000 description 1
- 208000020016 psychiatric disease Diseases 0.000 description 1
- 230000003236 psychic effect Effects 0.000 description 1
- 239000003196 psychodysleptic agent Substances 0.000 description 1
- 230000033764 rhythmic process Effects 0.000 description 1
- 230000000697 serotonin reuptake Effects 0.000 description 1
- VGKDLMBJGBXTGI-SJCJKPOMSA-N sertraline Chemical compound C1([C@@H]2CC[C@@H](C3=CC=CC=C32)NC)=CC=C(Cl)C(Cl)=C1 VGKDLMBJGBXTGI-SJCJKPOMSA-N 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 229940099190 serzone Drugs 0.000 description 1
- 238000007493 shaping process Methods 0.000 description 1
- 229910052710 silicon Inorganic materials 0.000 description 1
- 239000010703 silicon Substances 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 210000005070 sphincter Anatomy 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 230000006794 tachycardia Effects 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
- 235000012431 wafers Nutrition 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 229940020965 zoloft Drugs 0.000 description 1
- 229940039925 zyprexa 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Communicable Diseases (AREA)
- Pain & Pain Management (AREA)
- Addiction (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10958498P | 1998-11-23 | 1998-11-23 | |
| US109584P | 1998-11-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2237188T3 true ES2237188T3 (es) | 2005-07-16 |
Family
ID=22328453
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES99960547T Expired - Lifetime ES2237188T3 (es) | 1998-11-23 | 1999-11-22 | Composiciones de desmetilolanzapina y metodos. |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US6348455B1 (enExample) |
| EP (1) | EP1133300B1 (enExample) |
| JP (1) | JP2002530341A (enExample) |
| AT (1) | ATE286398T1 (enExample) |
| AU (1) | AU757973B2 (enExample) |
| CA (1) | CA2351718A1 (enExample) |
| DE (1) | DE69923081T2 (enExample) |
| ES (1) | ES2237188T3 (enExample) |
| PT (1) | PT1133300E (enExample) |
| WO (1) | WO2000030650A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200402289A (en) * | 2002-05-17 | 2004-02-16 | Wyeth Corp | Methods of treating gastrointestinary and genitourinary pain disorders |
| PL199016B1 (pl) | 2002-06-20 | 2008-08-29 | Adamed Sp Z Oo | Sposób wytwarzania olanzapiny |
| US6831077B2 (en) * | 2002-07-25 | 2004-12-14 | Comprehensive Neuroscience, Inc. | Augmentation of atypical antipsychotic agent pharmacotherapy with chromium supplementation |
| MXPA05000294A (es) * | 2002-07-30 | 2005-08-19 | Peter Migaly | Terapia combinada para la depresion, prevencion de suicidios y varias condiciones medicas y psiquiatricas. |
| AR042806A1 (es) * | 2002-12-27 | 2005-07-06 | Otsuka Pharma Co Ltd | Combinacion de derivados de carboestirilo e inhibidores de la reabsorcion de serotonina para el tratamiento de trastornos del animo |
| AU2003295235B2 (en) | 2002-12-27 | 2008-06-19 | Otsuka Pharmaceutical Co., Ltd. | Carbostyril derivatives and serotonin reuptake inhibitors for treatment of mood disorders |
| WO2004071417A2 (en) * | 2003-02-05 | 2004-08-26 | University Of Vermont And State Agricultural College | Inhibitors of candida albicans |
| PL198589B1 (pl) | 2004-11-22 | 2008-06-30 | Adamed Sp Z Oo | Sposób wytwarzania N-demetyloolanzapiny |
| US20060194769A1 (en) * | 2005-01-25 | 2006-08-31 | University Of Vermont And State Agricultural College | Small molecules that reduce fungal growth |
| US20080081067A1 (en) * | 2006-10-03 | 2008-04-03 | Gupta Manishkumar | Sustained release pharmaceutical compositions of venlafaxine and process for preparation thereof |
| EP2114150A4 (en) * | 2007-02-01 | 2010-03-10 | Alan I Green | COMBINATIONS OF BLOCKING OF DOPAMINERGIC D2 RECEPTORS WITH INHIBITION OF NOREPINEPHRINE RECAPTATION AND BLOCKING OF NOREPINEPHRINE ALPHA RECEPTORS |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4115568A (en) | 1974-11-26 | 1978-09-19 | Lilly Industries Limited | Thieno[3,2-b]-[1,5]benzodiazepines |
| US4590213A (en) * | 1983-04-08 | 1986-05-20 | Eli Lilly And Company | Anti-anxiety method |
| US5229382A (en) | 1990-04-25 | 1993-07-20 | Lilly Industries Limited | 2-methyl-thieno-benzodiazepine |
| US5627178A (en) | 1991-04-23 | 1997-05-06 | Lilly Industries Limited | 2-methyl-thieno-benzodiazepine |
| US5605897A (en) | 1991-04-23 | 1997-02-25 | Eli Lilly And Company | 2-methyl-thieno-benzodiazepine |
| US5457101A (en) | 1994-06-03 | 1995-10-10 | Eli Lilly And Company | Thieno[1,5]benzoidiazepine use |
| US6274636B1 (en) | 1995-09-29 | 2001-08-14 | Eli Lilly And Company | Method for treating a tic disorder |
| AU1335397A (en) * | 1995-12-21 | 1997-07-17 | Eli Lilly And Company | Method for treating dermatitis |
| HUP9903684A3 (en) | 1995-12-22 | 2001-12-28 | Lilly Co Eli | Use of olanzapine for the preparation of pharmaceutical compositions treating depression |
| UA57727C2 (uk) | 1996-03-11 | 2003-07-15 | Елі Ліллі Енд Компані | Спосіб лікування надмірної агресивності |
| JP2000506859A (ja) * | 1996-03-11 | 2000-06-06 | イーライ・リリー・アンド・カンパニー | 双極性障害の処置方法 |
| NZ331845A (en) | 1996-03-11 | 2000-09-29 | Lilly Co Eli | Use of olanzapine for treating substance abuse, alcohol and nicotine dependency |
| EP0946179B1 (en) | 1996-03-11 | 2003-09-17 | Eli Lilly And Company | Use of olanzapine or a pharmaceutically acceptable salt for the manufacture of a medicament for the treatment of autism and mental retardation |
| GB9615767D0 (en) | 1996-07-26 | 1996-09-04 | Smithkline Beecham Plc | Novel treatment |
-
1999
- 1999-11-22 DE DE69923081T patent/DE69923081T2/de not_active Expired - Fee Related
- 1999-11-22 EP EP99960547A patent/EP1133300B1/en not_active Expired - Lifetime
- 1999-11-22 AT AT99960547T patent/ATE286398T1/de not_active IP Right Cessation
- 1999-11-22 AU AU17416/00A patent/AU757973B2/en not_active Ceased
- 1999-11-22 JP JP2000583533A patent/JP2002530341A/ja not_active Withdrawn
- 1999-11-22 CA CA002351718A patent/CA2351718A1/en not_active Abandoned
- 1999-11-22 US US09/444,590 patent/US6348455B1/en not_active Expired - Fee Related
- 1999-11-22 PT PT99960547T patent/PT1133300E/pt unknown
- 1999-11-22 ES ES99960547T patent/ES2237188T3/es not_active Expired - Lifetime
- 1999-11-22 WO PCT/US1999/027647 patent/WO2000030650A1/en not_active Ceased
-
2001
- 2001-12-19 US US10/026,303 patent/US6468997B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| WO2000030650A1 (en) | 2000-06-02 |
| PT1133300E (pt) | 2005-04-29 |
| ATE286398T1 (de) | 2005-01-15 |
| DE69923081T2 (de) | 2005-12-08 |
| US6348455B1 (en) | 2002-02-19 |
| DE69923081D1 (de) | 2005-02-10 |
| AU1741600A (en) | 2000-06-13 |
| EP1133300B1 (en) | 2005-01-05 |
| EP1133300A1 (en) | 2001-09-19 |
| JP2002530341A (ja) | 2002-09-17 |
| US20020082251A1 (en) | 2002-06-27 |
| AU757973B2 (en) | 2003-03-13 |
| US6468997B2 (en) | 2002-10-22 |
| CA2351718A1 (en) | 2000-06-02 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2226435T3 (es) | Metodos de uso y composiciones que comprenden inhibidores de la recaptacion de dopamina. | |
| ES2256032T3 (es) | Utilizacion de dapoxetina, un inhibidor selectivo de la recaptacion de serotonina, para el tratamiento de una disfuncion sexual. | |
| ES2237188T3 (es) | Composiciones de desmetilolanzapina y metodos. | |
| ES2260195T3 (es) | Metodos de producir (r)-y (s)-didesmetil-sibutramina opticamente pura. | |
| ES2211205T3 (es) | Composiciones farmaceuticas que contienen olanzapina-n-oxido. | |
| WO2015089111A1 (en) | Novel methods | |
| US6174882B1 (en) | 2-hydroxymethylolanzapine compositions and methods | |
| CA2386547C (en) | Orally disintegrating composition comprising mirtazapine | |
| US20150258097A1 (en) | Compositions and methods for the treatment of catatonia | |
| US20140148465A1 (en) | Compositions and Methods to Improve Treatment of Medical Conditions Using D-Cycloserine | |
| US20250275924A1 (en) | Anticholinergic Agents and Muscarinic Agonists for the Treatment of Demodex Related Conditions | |
| Standard | PrACT FLUVOXAMINE | |
| Antidepressant et al. | M8Z 2S6 | |
| Dom-FLUVOXAMINE et al. | DOMINION PHARMACAL | |
| WO2005097138A2 (en) | Combinations comprising oxcarbazepine to treat affective disorders | |
| INC | PrNU-MIRTAZAPINE | |
| INC | NU-FLUVOXAMINE |