JP2010519261A - 新規方法 - Google Patents
新規方法 Download PDFInfo
- Publication number
- JP2010519261A JP2010519261A JP2009550665A JP2009550665A JP2010519261A JP 2010519261 A JP2010519261 A JP 2010519261A JP 2009550665 A JP2009550665 A JP 2009550665A JP 2009550665 A JP2009550665 A JP 2009550665A JP 2010519261 A JP2010519261 A JP 2010519261A
- Authority
- JP
- Japan
- Prior art keywords
- patient
- acridinium
- use according
- disease
- treatment
- 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.)
- Granted
Links
- 238000000034 method Methods 0.000 title claims abstract description 15
- DZBUGLKDJFMEHC-UHFFFAOYSA-O acridine;hydron Chemical compound C1=CC=CC2=CC3=CC=CC=C3[NH+]=C21 DZBUGLKDJFMEHC-UHFFFAOYSA-O 0.000 claims abstract description 54
- 238000011282 treatment Methods 0.000 claims abstract description 27
- 208000023504 respiratory system disease Diseases 0.000 claims abstract description 25
- 230000001022 anti-muscarinic effect Effects 0.000 claims abstract description 22
- 230000009885 systemic effect Effects 0.000 claims abstract description 19
- 239000003814 drug Substances 0.000 claims description 27
- 229940079593 drug Drugs 0.000 claims description 14
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 11
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 claims description 11
- 229960004373 acetylcholine Drugs 0.000 claims description 11
- 239000000812 cholinergic antagonist Substances 0.000 claims description 9
- 239000000843 powder Substances 0.000 claims description 9
- 206010010774 Constipation Diseases 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 208000024827 Alzheimer disease Diseases 0.000 claims description 7
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims description 7
- 229940125715 antihistaminic agent Drugs 0.000 claims description 7
- 239000000739 antihistaminic agent Substances 0.000 claims description 7
- 208000006673 asthma Diseases 0.000 claims description 7
- 230000002829 reductive effect Effects 0.000 claims description 7
- 206010012218 Delirium Diseases 0.000 claims description 6
- 208000018737 Parkinson disease Diseases 0.000 claims description 6
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 6
- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 6
- 230000002265 prevention Effects 0.000 claims description 6
- 210000002307 prostate Anatomy 0.000 claims description 6
- 210000001747 pupil Anatomy 0.000 claims description 6
- 208000004756 Respiratory Insufficiency Diseases 0.000 claims description 5
- 206010038678 Respiratory depression Diseases 0.000 claims description 5
- 239000000808 adrenergic beta-agonist Substances 0.000 claims description 5
- 238000013019 agitation Methods 0.000 claims description 5
- 239000003246 corticosteroid Substances 0.000 claims description 5
- 229960001334 corticosteroids Drugs 0.000 claims description 5
- 230000006735 deficit Effects 0.000 claims description 5
- 206010013781 dry mouth Diseases 0.000 claims description 5
- 230000004410 intraocular pressure Effects 0.000 claims description 5
- 206010027175 memory impairment Diseases 0.000 claims description 5
- 239000003149 muscarinic antagonist Substances 0.000 claims description 5
- 230000004393 visual impairment Effects 0.000 claims description 5
- 206010013496 Disturbance in attention Diseases 0.000 claims description 4
- 201000007100 Pharyngitis Diseases 0.000 claims description 4
- 208000001871 Tachycardia Diseases 0.000 claims description 4
- 229940123445 Tricyclic antidepressant Drugs 0.000 claims description 4
- 206010006451 bronchitis Diseases 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 230000030135 gastric motility Effects 0.000 claims description 4
- 239000003112 inhibitor Substances 0.000 claims description 4
- 239000008101 lactose Substances 0.000 claims description 4
- 230000001629 suppression Effects 0.000 claims description 4
- 230000006794 tachycardia Effects 0.000 claims description 4
- 239000003029 tricyclic antidepressant agent Substances 0.000 claims description 4
- 206010007559 Cardiac failure congestive Diseases 0.000 claims description 3
- 206010008479 Chest Pain Diseases 0.000 claims description 3
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims description 3
- 206010013774 Dry eye Diseases 0.000 claims description 3
- 208000010412 Glaucoma Diseases 0.000 claims description 3
- 206010019280 Heart failures Diseases 0.000 claims description 3
- 208000008454 Hyperhidrosis Diseases 0.000 claims description 3
- 208000031481 Pathologic Constriction Diseases 0.000 claims description 3
- WOVFJBGKJQEQQD-UHFFFAOYSA-N acridine;hydrobromide Chemical compound [Br-].C1=CC=CC2=CC3=CC=CC=C3[NH+]=C21 WOVFJBGKJQEQQD-UHFFFAOYSA-N 0.000 claims description 3
- 206010003119 arrhythmia Diseases 0.000 claims description 3
- 230000006793 arrhythmia Effects 0.000 claims description 3
- 230000001684 chronic effect Effects 0.000 claims description 3
- 210000001072 colon Anatomy 0.000 claims description 3
- 210000003238 esophagus Anatomy 0.000 claims description 3
- YEESKJGWJFYOOK-IJHYULJSSA-N leukotriene D4 Chemical compound CCCCC\C=C/C\C=C/C=C/C=C/[C@H]([C@@H](O)CCCC(O)=O)SC[C@H](N)C(=O)NCC(O)=O YEESKJGWJFYOOK-IJHYULJSSA-N 0.000 claims description 3
- 239000000203 mixture Substances 0.000 claims description 3
- 206010028417 myasthenia gravis Diseases 0.000 claims description 3
- 208000010125 myocardial infarction Diseases 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims description 3
- 208000037803 restenosis Diseases 0.000 claims description 3
- 201000000980 schizophrenia Diseases 0.000 claims description 3
- 210000000813 small intestine Anatomy 0.000 claims description 3
- 210000004243 sweat Anatomy 0.000 claims description 3
- 230000035900 sweating Effects 0.000 claims description 3
- 206010003210 Arteriosclerosis Diseases 0.000 claims description 2
- 206010006458 Bronchitis chronic Diseases 0.000 claims description 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- 206010014561 Emphysema Diseases 0.000 claims description 2
- 108010040718 Neurokinin-1 Receptors Proteins 0.000 claims description 2
- 208000006011 Stroke Diseases 0.000 claims description 2
- 102100037346 Substance-P receptor Human genes 0.000 claims description 2
- 230000001154 acute effect Effects 0.000 claims description 2
- 230000001668 ameliorated effect Effects 0.000 claims description 2
- 208000011775 arteriosclerosis disease Diseases 0.000 claims description 2
- 239000003693 atypical antipsychotic agent Substances 0.000 claims description 2
- 229940127236 atypical antipsychotics Drugs 0.000 claims description 2
- 208000007451 chronic bronchitis Diseases 0.000 claims description 2
- 230000003247 decreasing effect Effects 0.000 claims description 2
- 150000002016 disaccharides Chemical class 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 206010013990 dysuria Diseases 0.000 claims description 2
- 239000003862 glucocorticoid Substances 0.000 claims description 2
- 150000004676 glycans Chemical class 0.000 claims description 2
- 229940043355 kinase inhibitor Drugs 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 150000002772 monosaccharides Chemical class 0.000 claims description 2
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 claims description 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims description 2
- 229920001282 polysaccharide Polymers 0.000 claims description 2
- 239000005017 polysaccharide Substances 0.000 claims description 2
- 229940044551 receptor antagonist Drugs 0.000 claims description 2
- 239000002464 receptor antagonist Substances 0.000 claims description 2
- 230000036262 stenosis Effects 0.000 claims description 2
- 208000037804 stenosis Diseases 0.000 claims description 2
- 150000005846 sugar alcohols Chemical class 0.000 claims description 2
- 229940037128 systemic glucocorticoids Drugs 0.000 claims description 2
- 239000004480 active ingredient Substances 0.000 claims 1
- 230000004899 motility Effects 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 230000001078 anti-cholinergic effect Effects 0.000 description 16
- 230000000694 effects Effects 0.000 description 16
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 15
- LERNTVKEWCAPOY-DZZGSBJMSA-N tiotropium Chemical compound O([C@H]1C[C@@H]2[N+]([C@H](C1)[C@@H]1[C@H]2O1)(C)C)C(=O)C(O)(C=1SC=CC=1)C1=CC=CS1 LERNTVKEWCAPOY-DZZGSBJMSA-N 0.000 description 14
- 229940110309 tiotropium Drugs 0.000 description 14
- -1 2-hydroxy-2,2-dithien-2-ylacetoxy Chemical group 0.000 description 13
- OEXHQOGQTVQTAT-JRNQLAHRSA-N ipratropium Chemical compound O([C@H]1C[C@H]2CC[C@@H](C1)[N@@+]2(C)C(C)C)C(=O)C(CO)C1=CC=CC=C1 OEXHQOGQTVQTAT-JRNQLAHRSA-N 0.000 description 11
- 229960001888 ipratropium Drugs 0.000 description 11
- 150000001875 compounds Chemical class 0.000 description 10
- 239000000902 placebo Substances 0.000 description 10
- 229940068196 placebo Drugs 0.000 description 10
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 6
- 230000015556 catabolic process Effects 0.000 description 6
- 238000006731 degradation reaction Methods 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- VPNYRYCIDCJBOM-UHFFFAOYSA-M Glycopyrronium bromide Chemical compound [Br-].C1[N+](C)(C)CCC1OC(=O)C(O)(C=1C=CC=CC=1)C1CCCC1 VPNYRYCIDCJBOM-UHFFFAOYSA-M 0.000 description 5
- 108050003473 Muscarinic acetylcholine receptor Proteins 0.000 description 5
- 102000014415 Muscarinic acetylcholine receptor Human genes 0.000 description 5
- 239000002253 acid Substances 0.000 description 5
- 229940065524 anticholinergics inhalants for obstructive airway diseases Drugs 0.000 description 5
- 239000000544 cholinesterase inhibitor Substances 0.000 description 5
- 229940015042 glycopyrrolate Drugs 0.000 description 5
- NZWOPGCLSHLLPA-UHFFFAOYSA-N methacholine Chemical compound C[N+](C)(C)CC(C)OC(C)=O NZWOPGCLSHLLPA-UHFFFAOYSA-N 0.000 description 5
- 229960002329 methacholine Drugs 0.000 description 5
- 239000003643 water by type Substances 0.000 description 5
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 4
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 4
- 239000012071 phase Substances 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 3
- RKUNBYITZUJHSG-UHFFFAOYSA-N Hyosciamin-hydrochlorid Natural products CN1C(C2)CCC1CC2OC(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-UHFFFAOYSA-N 0.000 description 3
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 3
- 239000000048 adrenergic agonist Substances 0.000 description 3
- 150000001450 anions Chemical class 0.000 description 3
- 238000006243 chemical reaction Methods 0.000 description 3
- 239000000064 cholinergic agonist Substances 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
- 229960002848 formoterol Drugs 0.000 description 3
- BPZSYCZIITTYBL-UHFFFAOYSA-N formoterol Chemical compound C1=CC(OC)=CC=C1CC(C)NCC(O)C1=CC=C(O)C(NC=O)=C1 BPZSYCZIITTYBL-UHFFFAOYSA-N 0.000 description 3
- ZQDWXGKKHFNSQK-UHFFFAOYSA-N hydroxyzine Chemical compound C1CN(CCOCCO)CCN1C(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 ZQDWXGKKHFNSQK-UHFFFAOYSA-N 0.000 description 3
- 230000014759 maintenance of location Effects 0.000 description 3
- 239000002207 metabolite Substances 0.000 description 3
- 230000036470 plasma concentration Effects 0.000 description 3
- 102000005962 receptors Human genes 0.000 description 3
- 108020003175 receptors Proteins 0.000 description 3
- 238000011084 recovery Methods 0.000 description 3
- MNDBXUUTURYVHR-UHFFFAOYSA-N roflumilast Chemical compound FC(F)OC1=CC=C(C(=O)NC=2C(=CN=CC=2Cl)Cl)C=C1OCC1CC1 MNDBXUUTURYVHR-UHFFFAOYSA-N 0.000 description 3
- 229960002586 roflumilast Drugs 0.000 description 3
- 150000003839 salts Chemical class 0.000 description 3
- 238000002560 therapeutic procedure Methods 0.000 description 3
- VHRSUDSXCMQTMA-PJHHCJLFSA-N 6alpha-methylprednisolone Chemical compound C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)CO)CC[C@H]21 VHRSUDSXCMQTMA-PJHHCJLFSA-N 0.000 description 2
- 229930003347 Atropine Natural products 0.000 description 2
- VOVIALXJUBGFJZ-KWVAZRHASA-N Budesonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O VOVIALXJUBGFJZ-KWVAZRHASA-N 0.000 description 2
- 108010009685 Cholinergic Receptors Proteins 0.000 description 2
- GDLIGKIOYRNHDA-UHFFFAOYSA-N Clomipramine Chemical compound C1CC2=CC=C(Cl)C=C2N(CCCN(C)C)C2=CC=CC=C21 GDLIGKIOYRNHDA-UHFFFAOYSA-N 0.000 description 2
- HCYAFALTSJYZDH-UHFFFAOYSA-N Desimpramine Chemical compound C1CC2=CC=CC=C2N(CCCNC)C2=CC=CC=C21 HCYAFALTSJYZDH-UHFFFAOYSA-N 0.000 description 2
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 2
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
- PWWVAXIEGOYWEE-UHFFFAOYSA-N Isophenergan Chemical compound C1=CC=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 PWWVAXIEGOYWEE-UHFFFAOYSA-N 0.000 description 2
- OCJYIGYOJCODJL-UHFFFAOYSA-N Meclizine Chemical compound CC1=CC=CC(CN2CCN(CC2)C(C=2C=CC=CC=2)C=2C=CC(Cl)=CC=2)=C1 OCJYIGYOJCODJL-UHFFFAOYSA-N 0.000 description 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 2
- PHVGLTMQBUFIQQ-UHFFFAOYSA-N Nortryptiline Chemical compound C1CC2=CC=CC=C2C(=CCCNC)C2=CC=CC=C21 PHVGLTMQBUFIQQ-UHFFFAOYSA-N 0.000 description 2
- GIIZNNXWQWCKIB-UHFFFAOYSA-N Serevent Chemical compound C1=C(O)C(CO)=CC(C(O)CNCCCCCCOCCCCC=2C=CC=CC=2)=C1 GIIZNNXWQWCKIB-UHFFFAOYSA-N 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 2
- KLBQZWRITKRQQV-UHFFFAOYSA-N Thioridazine Chemical compound C12=CC(SC)=CC=C2SC2=CC=CC=C2N1CCC1CCCCN1C KLBQZWRITKRQQV-UHFFFAOYSA-N 0.000 description 2
- GFBKORZTTCHDGY-UWVJOHFNSA-N Thiothixene Chemical compound C12=CC(S(=O)(=O)N(C)C)=CC=C2SC2=CC=CC=C2\C1=C\CCN1CCN(C)CC1 GFBKORZTTCHDGY-UWVJOHFNSA-N 0.000 description 2
- WKHOPHIMYDJVSA-UHFFFAOYSA-N [3-[2-(tert-butylamino)-1-hydroxyethyl]-5-(2-methylpropanoyloxy)phenyl] 2-methylpropanoate Chemical compound CC(C)C(=O)OC1=CC(OC(=O)C(C)C)=CC(C(O)CNC(C)(C)C)=C1 WKHOPHIMYDJVSA-UHFFFAOYSA-N 0.000 description 2
- 102000034337 acetylcholine receptors Human genes 0.000 description 2
- 150000001298 alcohols Chemical class 0.000 description 2
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 2
- KRMDCWKBEZIMAB-UHFFFAOYSA-N amitriptyline Chemical compound C1CC2=CC=CC=C2C(=CCCN(C)C)C2=CC=CC=C21 KRMDCWKBEZIMAB-UHFFFAOYSA-N 0.000 description 2
- QWGDMFLQWFTERH-UHFFFAOYSA-N amoxapine Chemical compound C12=CC(Cl)=CC=C2OC2=CC=CC=C2N=C1N1CCNCC1 QWGDMFLQWFTERH-UHFFFAOYSA-N 0.000 description 2
- 239000000164 antipsychotic agent Substances 0.000 description 2
- 229940005529 antipsychotics Drugs 0.000 description 2
- 229960000396 atropine Drugs 0.000 description 2
- RKUNBYITZUJHSG-SPUOUPEWSA-N atropine Chemical compound O([C@H]1C[C@H]2CC[C@@H](C1)N2C)C(=O)C(CO)C1=CC=CC=C1 RKUNBYITZUJHSG-SPUOUPEWSA-N 0.000 description 2
- 229940092732 belladonna alkaloid Drugs 0.000 description 2
- GERIGMSHTUAXSI-UHFFFAOYSA-N bis(8-methyl-8-azabicyclo[3.2.1]octan-3-yl) 4-phenyl-2,3-dihydro-1h-naphthalene-1,4-dicarboxylate Chemical compound CN1C(C2)CCC1CC2OC(=O)C(C1=CC=CC=C11)CCC1(C(=O)OC1CC2CCC(N2C)C1)C1=CC=CC=C1 GERIGMSHTUAXSI-UHFFFAOYSA-N 0.000 description 2
- 210000004556 brain Anatomy 0.000 description 2
- 230000007883 bronchodilation Effects 0.000 description 2
- JBRBWHCVRGURBA-UHFFFAOYSA-N broxaterol Chemical compound CC(C)(C)NCC(O)C1=CC(Br)=NO1 JBRBWHCVRGURBA-UHFFFAOYSA-N 0.000 description 2
- 229950008847 broxaterol Drugs 0.000 description 2
- 229960004436 budesonide Drugs 0.000 description 2
- 229960001386 carbuterol Drugs 0.000 description 2
- KEMXXQOFIRIICG-UHFFFAOYSA-N carbuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(NC(N)=O)=C1 KEMXXQOFIRIICG-UHFFFAOYSA-N 0.000 description 2
- 229960001076 chlorpromazine Drugs 0.000 description 2
- ZPEIMTDSQAKGNT-UHFFFAOYSA-N chlorpromazine Chemical compound C1=C(Cl)C=C2N(CCCN(C)C)C3=CC=CC=C3SC2=C1 ZPEIMTDSQAKGNT-UHFFFAOYSA-N 0.000 description 2
- 230000001713 cholinergic effect Effects 0.000 description 2
- 238000004587 chromatography analysis Methods 0.000 description 2
- JURKNVYFZMSNLP-UHFFFAOYSA-N cyclobenzaprine Chemical compound C1=CC2=CC=CC=C2C(=CCCN(C)C)C2=CC=CC=C21 JURKNVYFZMSNLP-UHFFFAOYSA-N 0.000 description 2
- JJCFRYNCJDLXIK-UHFFFAOYSA-N cyproheptadine Chemical compound C1CN(C)CCC1=C1C2=CC=CC=C2C=CC2=CC=CC=C21 JJCFRYNCJDLXIK-UHFFFAOYSA-N 0.000 description 2
- 229960001140 cyproheptadine Drugs 0.000 description 2
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 description 2
- CURUTKGFNZGFSE-UHFFFAOYSA-N dicyclomine Chemical compound C1CCCCC1C1(C(=O)OCCN(CC)CC)CCCCC1 CURUTKGFNZGFSE-UHFFFAOYSA-N 0.000 description 2
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 description 2
- 229960000520 diphenhydramine Drugs 0.000 description 2
- HYPPXZBJBPSRLK-UHFFFAOYSA-N diphenoxylate Chemical compound C1CC(C(=O)OCC)(C=2C=CC=CC=2)CCN1CCC(C#N)(C=1C=CC=CC=1)C1=CC=CC=C1 HYPPXZBJBPSRLK-UHFFFAOYSA-N 0.000 description 2
- UVTNFZQICZKOEM-UHFFFAOYSA-N disopyramide Chemical compound C=1C=CC=NC=1C(C(N)=O)(CCN(C(C)C)C(C)C)C1=CC=CC=C1 UVTNFZQICZKOEM-UHFFFAOYSA-N 0.000 description 2
- 208000002173 dizziness Diseases 0.000 description 2
- ADEBPBSSDYVVLD-UHFFFAOYSA-N donepezil Chemical compound O=C1C=2C=C(OC)C(OC)=CC=2CC1CC(CC1)CCN1CC1=CC=CC=C1 ADEBPBSSDYVVLD-UHFFFAOYSA-N 0.000 description 2
- 229960003638 dopamine Drugs 0.000 description 2
- ODQWQRRAPPTVAG-GZTJUZNOSA-N doxepin Chemical compound C1OC2=CC=CC=C2C(=C/CCN(C)C)/C2=CC=CC=C21 ODQWQRRAPPTVAG-GZTJUZNOSA-N 0.000 description 2
- 230000008030 elimination Effects 0.000 description 2
- 238000003379 elimination reaction Methods 0.000 description 2
- 238000000605 extraction Methods 0.000 description 2
- 229960000855 flavoxate Drugs 0.000 description 2
- SPIUTQOUKAMGCX-UHFFFAOYSA-N flavoxate Chemical compound C1=CC=C2C(=O)C(C)=C(C=3C=CC=CC=3)OC2=C1C(=O)OCCN1CCCCC1 SPIUTQOUKAMGCX-UHFFFAOYSA-N 0.000 description 2
- ASUTZQLVASHGKV-JDFRZJQESA-N galanthamine Chemical compound O1C(=C23)C(OC)=CC=C2CN(C)CC[C@]23[C@@H]1C[C@@H](O)C=C2 ASUTZQLVASHGKV-JDFRZJQESA-N 0.000 description 2
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 2
- 229950002451 ibuterol Drugs 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 210000004072 lung Anatomy 0.000 description 2
- 238000005259 measurement Methods 0.000 description 2
- 238000002483 medication Methods 0.000 description 2
- 229960004584 methylprednisolone Drugs 0.000 description 2
- 208000024449 overflow incontinence Diseases 0.000 description 2
- SIOXPEMLGUPBBT-UHFFFAOYSA-N picolinic acid Chemical compound OC(=O)C1=CC=CC=N1 SIOXPEMLGUPBBT-UHFFFAOYSA-N 0.000 description 2
- REQCZEXYDRLIBE-UHFFFAOYSA-N procainamide Chemical compound CCN(CC)CCNC(=O)C1=CC=C(N)C=C1 REQCZEXYDRLIBE-UHFFFAOYSA-N 0.000 description 2
- 238000011002 quantification Methods 0.000 description 2
- LOUPRKONTZGTKE-LHHVKLHASA-N quinidine Chemical compound C([C@H]([C@H](C1)C=C)C2)C[N@@]1[C@H]2[C@@H](O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-LHHVKLHASA-N 0.000 description 2
- 229960004017 salmeterol Drugs 0.000 description 2
- 229910052708 sodium Inorganic materials 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- 239000007974 sodium acetate buffer Substances 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
- 230000002485 urinary effect Effects 0.000 description 2
- QCHFTSOMWOSFHM-WPRPVWTQSA-N (+)-Pilocarpine Chemical compound C1OC(=O)[C@@H](CC)[C@H]1CC1=CN=CN1C QCHFTSOMWOSFHM-WPRPVWTQSA-N 0.000 description 1
- JWZZKOKVBUJMES-UHFFFAOYSA-N (+-)-Isoprenaline Chemical compound CC(C)NCC(O)C1=CC=C(O)C(O)=C1 JWZZKOKVBUJMES-UHFFFAOYSA-N 0.000 description 1
- XWTYSIMOBUGWOL-UHFFFAOYSA-N (+-)-Terbutaline Chemical compound CC(C)(C)NCC(O)C1=CC(O)=CC(O)=C1 XWTYSIMOBUGWOL-UHFFFAOYSA-N 0.000 description 1
- WYDUSKDSKCASEF-LJQANCHMSA-N (1s)-1-cyclohexyl-1-phenyl-3-pyrrolidin-1-ylpropan-1-ol Chemical compound C([C@](O)(C1CCCCC1)C=1C=CC=CC=1)CN1CCCC1 WYDUSKDSKCASEF-LJQANCHMSA-N 0.000 description 1
- RKUNBYITZUJHSG-FXUDXRNXSA-N (S)-atropine Chemical compound C1([C@@H](CO)C(=O)O[C@H]2C[C@H]3CC[C@@H](C2)N3C)=CC=CC=C1 RKUNBYITZUJHSG-FXUDXRNXSA-N 0.000 description 1
- GOHUJGMYCZDYDF-UHFFFAOYSA-N 1,1,1-trifluoro-n-[3-(quinolin-2-ylmethoxy)phenyl]methanesulfonamide Chemical compound FC(F)(F)S(=O)(=O)NC1=CC=CC(OCC=2N=C3C=CC=CC3=CC=2)=C1 GOHUJGMYCZDYDF-UHFFFAOYSA-N 0.000 description 1
- JOROEVAWQLGPFQ-UHFFFAOYSA-N 1-benzhydryl-4-methylpiperazine;2-hydroxypropanoic acid Chemical compound CC(O)C(O)=O.C1CN(C)CCN1C(C=1C=CC=CC=1)C1=CC=CC=C1 JOROEVAWQLGPFQ-UHFFFAOYSA-N 0.000 description 1
- ASIFEXZWAKYMRM-UHFFFAOYSA-N 118314-35-5 Chemical compound N=1N2C(=O)C3=NNN=C3N=C2SC=1CCC1CCCCC1 ASIFEXZWAKYMRM-UHFFFAOYSA-N 0.000 description 1
- YREYLAVBNPACJM-UHFFFAOYSA-N 2-(tert-butylamino)-1-(2-chlorophenyl)ethanol Chemical compound CC(C)(C)NCC(O)C1=CC=CC=C1Cl YREYLAVBNPACJM-UHFFFAOYSA-N 0.000 description 1
- VXYDHPDQMSVQCU-UHFFFAOYSA-N 2-[4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)piperidin-1-yl]-n-hydroxyacetamide Chemical compound COC1=CC=C(C2(CCN(CC(=O)NO)CC2)C#N)C=C1OC1CCCC1 VXYDHPDQMSVQCU-UHFFFAOYSA-N 0.000 description 1
- RRUNJEUMTFLLDY-UHFFFAOYSA-N 2-[[5-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propylsulfanyl]-1,3,4-thiadiazol-2-yl]sulfanyl]acetic acid Chemical compound C1=CC(C(C)=O)=C(O)C(CCC)=C1OCCCSC1=NN=C(SCC(O)=O)S1 RRUNJEUMTFLLDY-UHFFFAOYSA-N 0.000 description 1
- WFLUEQCOAQCQLP-UHFFFAOYSA-N 2-cyclopentyl-2-hydroxy-2-phenylacetic acid Chemical compound C=1C=CC=CC=1C(O)(C(=O)O)C1CCCC1 WFLUEQCOAQCQLP-UHFFFAOYSA-N 0.000 description 1
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- DBCKRBGYGMVSTI-UHFFFAOYSA-N 2-oxo-7-[2-[2-[3-(2-phenylethoxy)propylsulfonyl]ethylazaniumyl]ethyl]-3h-1,3-benzothiazol-4-olate Chemical compound C1=2SC(=O)NC=2C(O)=CC=C1CCNCCS(=O)(=O)CCCOCCC1=CC=CC=C1 DBCKRBGYGMVSTI-UHFFFAOYSA-N 0.000 description 1
- AXUZQJFHDNNPFG-LHAVAQOQSA-N 3-[(r)-[3-[(e)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-[3-(dimethylamino)-3-oxopropyl]sulfanylmethyl]sulfanylpropanoic acid Chemical compound CN(C)C(=O)CCS[C@H](SCCC(O)=O)C1=CC=CC(\C=C\C=2N=C3C=C(Cl)C=CC3=CC=2)=C1 AXUZQJFHDNNPFG-LHAVAQOQSA-N 0.000 description 1
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
- OEXHQOGQTVQTAT-UHFFFAOYSA-N 3-hydroxy-2-phenylpropanoic acid (8-methyl-8-propan-2-yl-8-azoniabicyclo[3.2.1]octan-3-yl) ester Chemical compound CC(C)[N+]1(C)C(C2)CCC1CC2OC(=O)C(CO)C1=CC=CC=C1 OEXHQOGQTVQTAT-UHFFFAOYSA-N 0.000 description 1
- UTUUPXBCDMQYRR-HSZRJFAPSA-N 4-[(2r)-2-(3-cyclopentyloxy-4-methoxyphenyl)-2-phenylethyl]pyridine Chemical compound COC1=CC=C([C@H](CC=2C=CN=CC=2)C=2C=CC=CC=2)C=C1OC1CCCC1 UTUUPXBCDMQYRR-HSZRJFAPSA-N 0.000 description 1
- RTLJQOLVPIGICL-UHFFFAOYSA-N 4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(methylsulfonylmethyl)phenol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CS(C)(=O)=O)=C1 RTLJQOLVPIGICL-UHFFFAOYSA-N 0.000 description 1
- LZOUGWUAFCXMTJ-UHFFFAOYSA-N 4-[3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl]-1-hydroxycyclohexane-1-carbonitrile Chemical compound OC1(CCC(CC1)c1ccc(OC(F)F)c(OCC2CC2)c1)C#N LZOUGWUAFCXMTJ-UHFFFAOYSA-N 0.000 description 1
- ZAKKEARLDPTRLX-UHFFFAOYSA-N 4-[4-[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propylsulfonyl]phenyl]-4-oxobutanoic acid Chemical compound CCCC1=C(O)C(C(C)=O)=CC=C1OCCCS(=O)(=O)C1=CC=C(C(=O)CCC(O)=O)C=C1 ZAKKEARLDPTRLX-UHFFFAOYSA-N 0.000 description 1
- QMYRXIWINUJUNY-UHFFFAOYSA-N 4-[6,7-diethoxy-2,3-bis(hydroxymethyl)naphthalen-1-yl]-1-(2-methoxyethyl)pyridin-2-one Chemical compound C=12C=C(OCC)C(OCC)=CC2=CC(CO)=C(CO)C=1C=1C=CN(CCOC)C(=O)C=1 QMYRXIWINUJUNY-UHFFFAOYSA-N 0.000 description 1
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 description 1
- QTQGHKVYLQBJLO-UHFFFAOYSA-N 4-methylbenzenesulfonate;(4-methyl-1-oxo-1-phenylmethoxypentan-2-yl)azanium Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1.CC(C)CC(N)C(=O)OCC1=CC=CC=C1 QTQGHKVYLQBJLO-UHFFFAOYSA-N 0.000 description 1
- XBGQGAPUUJJOTA-KWLUMGGGSA-N 4b52439y33 Chemical compound O.C([C@@H]1C2)C3=CC=CC=C3C[C@@]1(C(=O)CO)[C@]1(C)[C@@H]2[C@H](CCC=2[C@@]3(C=CC(=O)C=2)C)[C@]3(F)[C@@H](O)C1 XBGQGAPUUJJOTA-KWLUMGGGSA-N 0.000 description 1
- LSLYOANBFKQKPT-DIFFPNOSSA-N 5-[(1r)-1-hydroxy-2-[[(2r)-1-(4-hydroxyphenyl)propan-2-yl]amino]ethyl]benzene-1,3-diol Chemical compound C([C@@H](C)NC[C@H](O)C=1C=C(O)C=C(O)C=1)C1=CC=C(O)C=C1 LSLYOANBFKQKPT-DIFFPNOSSA-N 0.000 description 1
- RVRGDCZGEKSIRW-UHFFFAOYSA-N 9-[(4-acetyl-3-hydroxy-2-propylphenoxy)methyl]-3-(2h-tetrazol-5-yl)pyrido[1,2-a]pyrimidin-4-one Chemical compound C1=CC(C(C)=O)=C(O)C(CCC)=C1OCC1=CC=CN2C(=O)C(C3=NNN=N3)=CN=C12 RVRGDCZGEKSIRW-UHFFFAOYSA-N 0.000 description 1
- 229930000680 A04AD01 - Scopolamine Natural products 0.000 description 1
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 1
- 229930024421 Adenine Natural products 0.000 description 1
- GFFGJBXGBJISGV-UHFFFAOYSA-N Adenine Chemical compound NC1=NC=NC2=C1N=CN2 GFFGJBXGBJISGV-UHFFFAOYSA-N 0.000 description 1
- 206010001497 Agitation Diseases 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- KUVIULQEHSCUHY-XYWKZLDCSA-N Beclometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)COC(=O)CC)(OC(=O)CC)[C@@]1(C)C[C@@H]2O KUVIULQEHSCUHY-XYWKZLDCSA-N 0.000 description 1
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 description 1
- 206010066091 Bronchial Hyperreactivity Diseases 0.000 description 1
- 206010006482 Bronchospasm Diseases 0.000 description 1
- GJUPJBUKBPKRFE-UHFFFAOYSA-N CN(C)C(CCSC[S+](CCC([O-])=O)C1=CC(C=CC2=NC3=CC(Cl)=CC=C3C=C2)=CC=C1)=O.[Na+] Chemical compound CN(C)C(CCSC[S+](CCC([O-])=O)C1=CC(C=CC2=NC3=CC(Cl)=CC=C3C=C2)=CC=C1)=O.[Na+] GJUPJBUKBPKRFE-UHFFFAOYSA-N 0.000 description 1
- DBAKFASWICGISY-BTJKTKAUSA-N Chlorpheniramine maleate Chemical compound OC(=O)\C=C/C(O)=O.C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 DBAKFASWICGISY-BTJKTKAUSA-N 0.000 description 1
- 229940122041 Cholinesterase inhibitor Drugs 0.000 description 1
- LUKZNWIVRBCLON-GXOBDPJESA-N Ciclesonide Chemical compound C1([C@H]2O[C@@]3([C@H](O2)C[C@@H]2[C@@]3(C[C@H](O)[C@@H]3[C@@]4(C)C=CC(=O)C=C4CC[C@H]32)C)C(=O)COC(=O)C(C)C)CCCCC1 LUKZNWIVRBCLON-GXOBDPJESA-N 0.000 description 1
- 206010012289 Dementia Diseases 0.000 description 1
- XIQVNETUBQGFHX-UHFFFAOYSA-N Ditropan Chemical compound C=1C=CC=CC=1C(O)(C(=O)OCC#CCN(CC)CC)C1CCCCC1 XIQVNETUBQGFHX-UHFFFAOYSA-N 0.000 description 1
- 102100025027 E3 ubiquitin-protein ligase TRIM69 Human genes 0.000 description 1
- 108060006698 EGF receptor Proteins 0.000 description 1
- VWLHWLSRQJQWRG-UHFFFAOYSA-O Edrophonum Chemical compound CC[N+](C)(C)C1=CC=CC(O)=C1 VWLHWLSRQJQWRG-UHFFFAOYSA-O 0.000 description 1
- 108090000371 Esterases Proteins 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical class CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- WJOHZNCJWYWUJD-IUGZLZTKSA-N Fluocinonide Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)COC(=O)C)[C@@]2(C)C[C@@H]1O WJOHZNCJWYWUJD-IUGZLZTKSA-N 0.000 description 1
- PLDUPXSUYLZYBN-UHFFFAOYSA-N Fluphenazine Chemical compound C1CN(CCO)CCN1CCCN1C2=CC(C(F)(F)F)=CC=C2SC2=CC=CC=C21 PLDUPXSUYLZYBN-UHFFFAOYSA-N 0.000 description 1
- YCISZOVUHXIOFY-HKXOFBAYSA-N Halopredone acetate Chemical compound C1([C@H](F)C2)=CC(=O)C(Br)=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2CC[C@](OC(C)=O)(C(=O)COC(=O)C)[C@@]2(C)C[C@@H]1O YCISZOVUHXIOFY-HKXOFBAYSA-N 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 description 1
- 101000830203 Homo sapiens E3 ubiquitin-protein ligase TRIM69 Proteins 0.000 description 1
- FOGXJPFPZOHSQS-AYVLZSQQSA-N Hydrocortisone butyrate propionate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)CC)(OC(=O)CCC)[C@@]1(C)C[C@@H]2O FOGXJPFPZOHSQS-AYVLZSQQSA-N 0.000 description 1
- STECJAGHUSJQJN-GAUPFVANSA-N Hyoscine Natural products C1([C@H](CO)C(=O)OC2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-GAUPFVANSA-N 0.000 description 1
- ZJVFLBOZORBYFE-UHFFFAOYSA-N Ibudilast Chemical compound C1=CC=CC2=C(C(=O)C(C)C)C(C(C)C)=NN21 ZJVFLBOZORBYFE-UHFFFAOYSA-N 0.000 description 1
- 238000012404 In vitro experiment Methods 0.000 description 1
- 206010061218 Inflammation Diseases 0.000 description 1
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 description 1
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 description 1
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 description 1
- NZDMFGKECODQRY-UHFFFAOYSA-N Maprotiline hydrochloride Chemical compound Cl.C12=CC=CC=C2C2(CCCNC)C3=CC=CC=C3C1CC2 NZDMFGKECODQRY-UHFFFAOYSA-N 0.000 description 1
- IMWZZHHPURKASS-UHFFFAOYSA-N Metaxalone Chemical compound CC1=CC(C)=CC(OCC2OC(=O)NC2)=C1 IMWZZHHPURKASS-UHFFFAOYSA-N 0.000 description 1
- 206010028111 Mucosal dryness Diseases 0.000 description 1
- 108010008409 Muscarinic M5 Receptor Proteins 0.000 description 1
- STECJAGHUSJQJN-UHFFFAOYSA-N N-Methyl-scopolamin Natural products C1C(C2C3O2)N(C)C3CC1OC(=O)C(CO)C1=CC=CC=C1 STECJAGHUSJQJN-UHFFFAOYSA-N 0.000 description 1
- 206010028813 Nausea Diseases 0.000 description 1
- XCIHEXIWRNTQHV-QTQXQZBYSA-N OC(C(O[C@@H]1C(CC2)CC[N+]2(CCCOC2=CC=CC=C2)C1)=O)(C1=CC=CS1)C1=CC=CS1.C1=CC=C2N=C(C=CC=C3)C3=CC2=C1 Chemical compound OC(C(O[C@@H]1C(CC2)CC[N+]2(CCCOC2=CC=CC=C2)C1)=O)(C1=CC=CS1)C1=CC=CS1.C1=CC=C2N=C(C=CC=C3)C3=CC2=C1 XCIHEXIWRNTQHV-QTQXQZBYSA-N 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 description 1
- PIJVFDBKTWXHHD-UHFFFAOYSA-N Physostigmine Natural products C12=CC(OC(=O)NC)=CC=C2N(C)C2C1(C)CCN2C PIJVFDBKTWXHHD-UHFFFAOYSA-N 0.000 description 1
- SBQAKZYUNWNIRL-WIPKXTQKSA-N Prednisolone farnesylate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)/C=C(C)/CC/C=C(C)/CCC=C(C)C)(O)[C@@]1(C)C[C@@H]2O SBQAKZYUNWNIRL-WIPKXTQKSA-N 0.000 description 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 1
- RVOLLAQWKVFTGE-UHFFFAOYSA-N Pyridostigmine Chemical compound CN(C)C(=O)OC1=CC=C[N+](C)=C1 RVOLLAQWKVFTGE-UHFFFAOYSA-N 0.000 description 1
- LCTONWCANYUPML-UHFFFAOYSA-M Pyruvate Chemical compound CC(=O)C([O-])=O LCTONWCANYUPML-UHFFFAOYSA-M 0.000 description 1
- XSVMFMHYUFZWBK-NSHDSACASA-N Rivastigmine Chemical compound CCN(C)C(=O)OC1=CC=CC([C@H](C)N(C)C)=C1 XSVMFMHYUFZWBK-NSHDSACASA-N 0.000 description 1
- QCHFTSOMWOSFHM-UHFFFAOYSA-N SJ000285536 Natural products C1OC(=O)C(CC)C1CC1=CN=CN1C QCHFTSOMWOSFHM-UHFFFAOYSA-N 0.000 description 1
- 208000032140 Sleepiness Diseases 0.000 description 1
- 206010041349 Somnolence Diseases 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 1
- KPWYNAGOBXLMSE-UHFFFAOYSA-N Tipelukast Chemical compound CCCC1=C(O)C(C(C)=O)=CC=C1SCCCOC1=CC=C(C(C)=O)C(OCCCC(O)=O)=C1CCC KPWYNAGOBXLMSE-UHFFFAOYSA-N 0.000 description 1
- DXEXNWDGDYUITL-FXSSSKFRSA-N Tipredane Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1CC[C@@](SC)(SCC)[C@@]1(C)C[C@@H]2O DXEXNWDGDYUITL-FXSSSKFRSA-N 0.000 description 1
- HWHLPVGTWGOCJO-UHFFFAOYSA-N Trihexyphenidyl Chemical group C1CCCCC1C(C=1C=CC=CC=1)(O)CCN1CCCCC1 HWHLPVGTWGOCJO-UHFFFAOYSA-N 0.000 description 1
- 101100107916 Xenopus laevis chrm4 gene Proteins 0.000 description 1
- YEEZWCHGZNKEEK-UHFFFAOYSA-N Zafirlukast Chemical compound COC1=CC(C(=O)NS(=O)(=O)C=2C(=CC=CC=2)C)=CC=C1CC(C1=C2)=CN(C)C1=CC=C2NC(=O)OC1CCCC1 YEEZWCHGZNKEEK-UHFFFAOYSA-N 0.000 description 1
- 238000002835 absorbance Methods 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- DZBUGLKDJFMEHC-UHFFFAOYSA-N acridine Chemical class C1=CC=CC2=CC3=CC=CC=C3N=C21 DZBUGLKDJFMEHC-UHFFFAOYSA-N 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 229960000643 adenine Drugs 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- NDAUXUAQIAJITI-UHFFFAOYSA-N albuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1 NDAUXUAQIAJITI-UHFFFAOYSA-N 0.000 description 1
- 229960000552 alclometasone Drugs 0.000 description 1
- FJXOGVLKCZQRDN-PHCHRAKRSA-N alclometasone Chemical compound C([C@H]1Cl)C2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O FJXOGVLKCZQRDN-PHCHRAKRSA-N 0.000 description 1
- 229960004229 alclometasone dipropionate Drugs 0.000 description 1
- DJHCCTTVDRAMEH-DUUJBDRPSA-N alclometasone dipropionate Chemical compound C([C@H]1Cl)C2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)COC(=O)CC)(OC(=O)CC)[C@@]1(C)C[C@@H]2O DJHCCTTVDRAMEH-DUUJBDRPSA-N 0.000 description 1
- 229960000836 amitriptyline Drugs 0.000 description 1
- 229960002519 amoxapine Drugs 0.000 description 1
- 229940025141 anafranil Drugs 0.000 description 1
- 239000012491 analyte Substances 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 239000003416 antiarrhythmic agent Substances 0.000 description 1
- 239000003146 anticoagulant agent Substances 0.000 description 1
- 229940127219 anticoagulant drug Drugs 0.000 description 1
- 239000000935 antidepressant agent Substances 0.000 description 1
- 229940005513 antidepressants Drugs 0.000 description 1
- 229940125714 antidiarrheal agent Drugs 0.000 description 1
- 239000003793 antidiarrheal agent Substances 0.000 description 1
- 229940125684 antimigraine agent Drugs 0.000 description 1
- 239000002282 antimigraine agent Substances 0.000 description 1
- 229940071731 antivert Drugs 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 229940065779 atarax Drugs 0.000 description 1
- 229960003060 bambuterol Drugs 0.000 description 1
- ANZXOIAKUNOVQU-UHFFFAOYSA-N bambuterol Chemical compound CN(C)C(=O)OC1=CC(OC(=O)N(C)C)=CC(C(O)CNC(C)(C)C)=C1 ANZXOIAKUNOVQU-UHFFFAOYSA-N 0.000 description 1
- 229950000210 beclometasone dipropionate Drugs 0.000 description 1
- 229940088007 benadryl Drugs 0.000 description 1
- 229940090012 bentyl Drugs 0.000 description 1
- 229960001081 benzatropine Drugs 0.000 description 1
- GIJXKZJWITVLHI-PMOLBWCYSA-N benzatropine Chemical compound O([C@H]1C[C@H]2CC[C@@H](C1)N2C)C(C=1C=CC=CC=1)C1=CC=CC=C1 GIJXKZJWITVLHI-PMOLBWCYSA-N 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 229960002537 betamethasone Drugs 0.000 description 1
- UREBDLICKHMUKA-DVTGEIKXSA-N betamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-DVTGEIKXSA-N 0.000 description 1
- 229960001102 betamethasone dipropionate Drugs 0.000 description 1
- NZUPCNDJBJXXRF-UHFFFAOYSA-O bethanechol Chemical compound C[N+](C)(C)CC(C)OC(N)=O NZUPCNDJBJXXRF-UHFFFAOYSA-O 0.000 description 1
- 229960000910 bethanechol Drugs 0.000 description 1
- 230000005540 biological transmission Effects 0.000 description 1
- 229960003003 biperiden Drugs 0.000 description 1
- YSXKPIUOCJLQIE-UHFFFAOYSA-N biperiden Chemical compound C1C(C=C2)CC2C1C(C=1C=CC=CC=1)(O)CCN1CCCCC1 YSXKPIUOCJLQIE-UHFFFAOYSA-N 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
- 210000004204 blood vessel Anatomy 0.000 description 1
- 230000007885 bronchoconstriction Effects 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000007853 buffer solution Substances 0.000 description 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 229940072350 chlor-trimeton Drugs 0.000 description 1
- SOYKEARSMXGVTM-UHFFFAOYSA-N chlorphenamine Chemical compound C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 SOYKEARSMXGVTM-UHFFFAOYSA-N 0.000 description 1
- 229960003291 chlorphenamine Drugs 0.000 description 1
- 229960001231 choline Drugs 0.000 description 1
- OEYIOHPDSNJKLS-UHFFFAOYSA-N choline Chemical compound C[N+](C)(C)CCO OEYIOHPDSNJKLS-UHFFFAOYSA-N 0.000 description 1
- 229960003728 ciclesonide Drugs 0.000 description 1
- LOUPRKONTZGTKE-UHFFFAOYSA-N cinchonine Natural products C1C(C(C2)C=C)CCN2C1C(O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-UHFFFAOYSA-N 0.000 description 1
- KSPYMJJKQMWWNB-UHFFFAOYSA-N cipamfylline Chemical compound O=C1N(CC2CC2)C(=O)C=2NC(N)=NC=2N1CC1CC1 KSPYMJJKQMWWNB-UHFFFAOYSA-N 0.000 description 1
- 229950002405 cipamfylline Drugs 0.000 description 1
- YURNCBVQZBJDAJ-WAYWQWQTSA-N cis-2-heptenoic acid Chemical compound CCCC\C=C/C(O)=O YURNCBVQZBJDAJ-WAYWQWQTSA-N 0.000 description 1
- 229960001117 clenbuterol Drugs 0.000 description 1
- STJMRWALKKWQGH-UHFFFAOYSA-N clenbuterol Chemical compound CC(C)(C)NCC(O)C1=CC(Cl)=C(N)C(Cl)=C1 STJMRWALKKWQGH-UHFFFAOYSA-N 0.000 description 1
- 229960004606 clomipramine Drugs 0.000 description 1
- QZUDBNBUXVUHMW-UHFFFAOYSA-N clozapine Chemical compound C1CN(C)CCN1C1=NC2=CC(Cl)=CC=C2NC2=CC=CC=C12 QZUDBNBUXVUHMW-UHFFFAOYSA-N 0.000 description 1
- 229940088505 compazine Drugs 0.000 description 1
- 230000001143 conditioned effect Effects 0.000 description 1
- 210000004351 coronary vessel Anatomy 0.000 description 1
- ALEXXDVDDISNDU-JZYPGELDSA-N cortisol 21-acetate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)C)(O)[C@@]1(C)C[C@@H]2O ALEXXDVDDISNDU-JZYPGELDSA-N 0.000 description 1
- 229960003572 cyclobenzaprine Drugs 0.000 description 1
- 125000001887 cyclopentyloxy group Chemical group C1(CCCC1)O* 0.000 description 1
- 230000006378 damage Effects 0.000 description 1
- 229960003914 desipramine Drugs 0.000 description 1
- 229960003957 dexamethasone Drugs 0.000 description 1
- 229950000812 dexamethasone palmitate Drugs 0.000 description 1
- 229960002344 dexamethasone sodium phosphate Drugs 0.000 description 1
- PLCQGRYPOISRTQ-FCJDYXGNSA-L dexamethasone sodium phosphate Chemical compound [Na+].[Na+].C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)COP([O-])([O-])=O)(O)[C@@]1(C)C[C@@H]2O PLCQGRYPOISRTQ-FCJDYXGNSA-L 0.000 description 1
- 229960002777 dicycloverine Drugs 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- PCHPORCSPXIHLZ-UHFFFAOYSA-N diphenhydramine hydrochloride Chemical compound [Cl-].C=1C=CC=CC=1C(OCC[NH+](C)C)C1=CC=CC=C1 PCHPORCSPXIHLZ-UHFFFAOYSA-N 0.000 description 1
- 229960004192 diphenoxylate Drugs 0.000 description 1
- 229960001066 disopyramide Drugs 0.000 description 1
- 229960003530 donepezil Drugs 0.000 description 1
- 229960001857 dopexamine Drugs 0.000 description 1
- RYBJORHCUPVNMB-UHFFFAOYSA-N dopexamine Chemical compound C1=C(O)C(O)=CC=C1CCNCCCCCCNCCC1=CC=CC=C1 RYBJORHCUPVNMB-UHFFFAOYSA-N 0.000 description 1
- 229960005426 doxepin Drugs 0.000 description 1
- 229940000406 drug candidate Drugs 0.000 description 1
- 229940112141 dry powder inhaler Drugs 0.000 description 1
- KYFWUBJMTHVBIF-QFIPXVFZSA-N dsstox_cid_27248 Chemical compound N([C@@H]1N=C(C=2C=3N(C1=O)CCC=3C=C(C=2)C)C=1C=CC=CC=1)C(=O)C1=CC=NC=C1 KYFWUBJMTHVBIF-QFIPXVFZSA-N 0.000 description 1
- 229960003748 edrophonium Drugs 0.000 description 1
- 229940011681 elavil Drugs 0.000 description 1
- 125000004185 ester group Chemical group 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 239000003777 experimental drug Substances 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 229960001022 fenoterol Drugs 0.000 description 1
- STTRYQAGHGJXJJ-LICLKQGHSA-N filaminast Chemical compound COC1=CC=C(C(\C)=N\OC(N)=O)C=C1OC1CCCC1 STTRYQAGHGJXJJ-LICLKQGHSA-N 0.000 description 1
- 229950006884 filaminast Drugs 0.000 description 1
- 229940099283 flexeril Drugs 0.000 description 1
- 229960000676 flunisolide Drugs 0.000 description 1
- 229960001347 fluocinolone acetonide Drugs 0.000 description 1
- FEBLZLNTKCEFIT-VSXGLTOVSA-N fluocinolone acetonide Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O FEBLZLNTKCEFIT-VSXGLTOVSA-N 0.000 description 1
- 229960000785 fluocinonide Drugs 0.000 description 1
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 description 1
- 229960002690 fluphenazine Drugs 0.000 description 1
- 229960000289 fluticasone propionate Drugs 0.000 description 1
- WMWTYOKRWGGJOA-CENSZEJFSA-N fluticasone propionate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(OC(=O)CC)[C@@]2(C)C[C@@H]1O WMWTYOKRWGGJOA-CENSZEJFSA-N 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 239000003517 fume Substances 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 229960003980 galantamine Drugs 0.000 description 1
- ASUTZQLVASHGKV-UHFFFAOYSA-N galanthamine hydrochloride Natural products O1C(=C23)C(OC)=CC=C2CN(C)CCC23C1CC(O)C=C2 ASUTZQLVASHGKV-UHFFFAOYSA-N 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 229960002475 halometasone Drugs 0.000 description 1
- GGXMRPUKBWXVHE-MIHLVHIWSA-N halometasone Chemical compound C1([C@@H](F)C2)=CC(=O)C(Cl)=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]2(C)C[C@@H]1O GGXMRPUKBWXVHE-MIHLVHIWSA-N 0.000 description 1
- 229950004611 halopredone acetate Drugs 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 208000019622 heart disease Diseases 0.000 description 1
- 229920000669 heparin Polymers 0.000 description 1
- 229960002897 heparin Drugs 0.000 description 1
- OXLZNBCNGJWPRV-UHFFFAOYSA-N hexoprenaline Chemical compound C=1C=C(O)C(O)=CC=1C(O)CNCCCCCCNCC(O)C1=CC=C(O)C(O)=C1 OXLZNBCNGJWPRV-UHFFFAOYSA-N 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 229960001340 histamine Drugs 0.000 description 1
- 239000000938 histamine H1 antagonist Substances 0.000 description 1
- 229960000890 hydrocortisone Drugs 0.000 description 1
- 229960001067 hydrocortisone acetate Drugs 0.000 description 1
- 229960001401 hydrocortisone sodium succinate Drugs 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 229960000930 hydroxyzine Drugs 0.000 description 1
- 229930005342 hyoscyamine Natural products 0.000 description 1
- 229960003210 hyoscyamine Drugs 0.000 description 1
- 229960002491 ibudilast Drugs 0.000 description 1
- 229960004801 imipramine Drugs 0.000 description 1
- BCGWQEUPMDMJNV-UHFFFAOYSA-N imipramine Chemical compound C1CC2=CC=CC=C2N(CCCN(C)C)C2=CC=CC=C21 BCGWQEUPMDMJNV-UHFFFAOYSA-N 0.000 description 1
- XZZXIYZZBJDEEP-UHFFFAOYSA-N imipramine hydrochloride Chemical compound [Cl-].C1CC2=CC=CC=C2N(CCC[NH+](C)C)C2=CC=CC=C21 XZZXIYZZBJDEEP-UHFFFAOYSA-N 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 229960004078 indacaterol Drugs 0.000 description 1
- QZZUEBNBZAPZLX-QFIPXVFZSA-N indacaterol Chemical compound N1C(=O)C=CC2=C1C(O)=CC=C2[C@@H](O)CNC1CC(C=C(C(=C2)CC)CC)=C2C1 QZZUEBNBZAPZLX-QFIPXVFZSA-N 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 230000030214 innervation Effects 0.000 description 1
- 229960001317 isoprenaline Drugs 0.000 description 1
- 210000003734 kidney Anatomy 0.000 description 1
- 230000003907 kidney function Effects 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 229960004502 levodopa Drugs 0.000 description 1
- 208000013433 lightheadedness Diseases 0.000 description 1
- 229910052744 lithium Inorganic materials 0.000 description 1
- 230000003908 liver function Effects 0.000 description 1
- 229940087973 lomotil Drugs 0.000 description 1
- 229940125386 long-acting bronchodilator Drugs 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 229960001798 loteprednol Drugs 0.000 description 1
- YPZVAYHNBBHPTO-MXRBDKCISA-N loteprednol Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)OCCl)[C@@H]4[C@@H]3CCC2=C1 YPZVAYHNBBHPTO-MXRBDKCISA-N 0.000 description 1
- 230000004199 lung function Effects 0.000 description 1
- JSJCTEKTBOKRST-UHFFFAOYSA-N mabuterol Chemical compound CC(C)(C)NCC(O)C1=CC(Cl)=C(N)C(C(F)(F)F)=C1 JSJCTEKTBOKRST-UHFFFAOYSA-N 0.000 description 1
- 229950004407 mabuterol Drugs 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 229960004090 maprotiline Drugs 0.000 description 1
- QSLMDECMDJKHMQ-GSXCWMCISA-N maprotiline Chemical compound C12=CC=CC=C2[C@@]2(CCCNC)C3=CC=CC=C3[C@@H]1CC2 QSLMDECMDJKHMQ-GSXCWMCISA-N 0.000 description 1
- 229940063647 marezine Drugs 0.000 description 1
- 229960001474 meclozine Drugs 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- FXXQDYPNDZFBMV-UHFFFAOYSA-N methyl 5-cyano-5-[3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl]-2-oxocyclohexane-1-carboxylate Chemical compound C1CC(=O)C(C(=O)OC)CC1(C#N)C1=CC=C(OC(F)F)C(OCC2CC2)=C1 FXXQDYPNDZFBMV-UHFFFAOYSA-N 0.000 description 1
- 229960002037 methylprednisolone aceponate Drugs 0.000 description 1
- DALKLAYLIPSCQL-YPYQNWSCSA-N methylprednisolone aceponate Chemical compound C1([C@@H](C)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@@](C(=O)COC(C)=O)(OC(=O)CC)[C@@]2(C)C[C@@H]1O DALKLAYLIPSCQL-YPYQNWSCSA-N 0.000 description 1
- 230000027939 micturition Effects 0.000 description 1
- 150000007522 mineralic acids Chemical group 0.000 description 1
- 229960001664 mometasone Drugs 0.000 description 1
- QLIIKPVHVRXHRI-CXSFZGCWSA-N mometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CCl)(O)[C@@]1(C)C[C@@H]2O QLIIKPVHVRXHRI-CXSFZGCWSA-N 0.000 description 1
- LBFBRXGCXUHRJY-HKHDRNBDSA-M montelukast sodium Chemical compound [Na+].CC(C)(O)C1=CC=CC=C1CC[C@H](C=1C=C(\C=C\C=2N=C3C=C(Cl)C=CC3=CC=2)C=CC=1)SCC1(CC([O-])=O)CC1 LBFBRXGCXUHRJY-HKHDRNBDSA-M 0.000 description 1
- 229960001951 montelukast sodium Drugs 0.000 description 1
- 210000003097 mucus Anatomy 0.000 description 1
- 229940035363 muscle relaxants Drugs 0.000 description 1
- 239000003158 myorelaxant agent Substances 0.000 description 1
- UBYNBZKQYLBKFN-UHFFFAOYSA-N n-(3,5-dichloropyridin-4-yl)-8-methoxyquinoline-5-carboxamide Chemical compound C12=CC=CN=C2C(OC)=CC=C1C(=O)NC1=C(Cl)C=NC=C1Cl UBYNBZKQYLBKFN-UHFFFAOYSA-N 0.000 description 1
- BMKINZUHKYLSKI-DQEYMECFSA-N n-[2-hydroxy-5-[(1r)-1-hydroxy-2-[2-[4-[[(2r)-2-hydroxy-2-phenylethyl]amino]phenyl]ethylamino]ethyl]phenyl]formamide Chemical compound C1([C@@H](O)CNC2=CC=C(C=C2)CCNC[C@H](O)C=2C=C(NC=O)C(O)=CC=2)=CC=CC=C1 BMKINZUHKYLSKI-DQEYMECFSA-N 0.000 description 1
- ZHUGICMGWXPYIV-UHFFFAOYSA-N n-ethyl-8-propan-2-yl-7h-purin-2-amine Chemical compound N1C(NCC)=NC=C2N=C(C(C)C)N=C21 ZHUGICMGWXPYIV-UHFFFAOYSA-N 0.000 description 1
- 229950005486 naflocort Drugs 0.000 description 1
- 230000008693 nausea Effects 0.000 description 1
- 229960002362 neostigmine Drugs 0.000 description 1
- LULNWZDBKTWDGK-UHFFFAOYSA-M neostigmine bromide Chemical compound [Br-].CN(C)C(=O)OC1=CC=CC([N+](C)(C)C)=C1 LULNWZDBKTWDGK-UHFFFAOYSA-M 0.000 description 1
- 239000002858 neurotransmitter agent Substances 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 231100000957 no side effect Toxicity 0.000 description 1
- 229940079063 norflex Drugs 0.000 description 1
- 229940088938 norpace Drugs 0.000 description 1
- 229940087480 norpramin Drugs 0.000 description 1
- 229960001158 nortriptyline Drugs 0.000 description 1
- 210000004798 organs belonging to the digestive system Anatomy 0.000 description 1
- MMMNTDFSPSQXJP-UHFFFAOYSA-N orphenadrine citrate Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=C(C)C=1C(OCCN(C)C)C1=CC=CC=C1 MMMNTDFSPSQXJP-UHFFFAOYSA-N 0.000 description 1
- 229940055692 pamelor Drugs 0.000 description 1
- 230000001734 parasympathetic effect Effects 0.000 description 1
- 230000036961 partial effect Effects 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 238000009520 phase I clinical trial Methods 0.000 description 1
- 238000009521 phase II clinical trial Methods 0.000 description 1
- 229940107333 phenergan Drugs 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 229960001697 physostigmine Drugs 0.000 description 1
- PIJVFDBKTWXHHD-HIFRSBDPSA-N physostigmine Chemical compound C12=CC(OC(=O)NC)=CC=C2N(C)[C@@H]2[C@@]1(C)CCN2C PIJVFDBKTWXHHD-HIFRSBDPSA-N 0.000 description 1
- 229960001416 pilocarpine Drugs 0.000 description 1
- 230000007505 plaque formation Effects 0.000 description 1
- 229960004583 pranlukast Drugs 0.000 description 1
- UAJUXJSXCLUTNU-UHFFFAOYSA-N pranlukast Chemical compound C=1C=C(OCCCCC=2C=CC=CC=2)C=CC=1C(=O)NC(C=1)=CC=C(C(C=2)=O)C=1OC=2C=1N=NNN=1 UAJUXJSXCLUTNU-UHFFFAOYSA-N 0.000 description 1
- 238000011533 pre-incubation Methods 0.000 description 1
- 229960005205 prednisolone Drugs 0.000 description 1
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 description 1
- 229950011084 prednisolone farnesylate Drugs 0.000 description 1
- JDOZJEUDSLGTLU-VWUMJDOOSA-N prednisolone phosphate Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)COP(O)(O)=O)[C@@H]4[C@@H]3CCC2=C1 JDOZJEUDSLGTLU-VWUMJDOOSA-N 0.000 description 1
- 229960002943 prednisolone sodium phosphate Drugs 0.000 description 1
- XOFYZVNMUHMLCC-ZPOLXVRWSA-N prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 description 1
- 229960004618 prednisone Drugs 0.000 description 1
- 229960000244 procainamide Drugs 0.000 description 1
- 229960003111 prochlorperazine Drugs 0.000 description 1
- WIKYUJGCLQQFNW-UHFFFAOYSA-N prochlorperazine Chemical compound C1CN(C)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 WIKYUJGCLQQFNW-UHFFFAOYSA-N 0.000 description 1
- DSKIOWHQLUWFLG-SPIKMXEPSA-N prochlorperazine maleate Chemical compound [H+].[H+].[H+].[H+].[O-]C(=O)\C=C/C([O-])=O.[O-]C(=O)\C=C/C([O-])=O.C1CN(C)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 DSKIOWHQLUWFLG-SPIKMXEPSA-N 0.000 description 1
- 229960005253 procyclidine Drugs 0.000 description 1
- 229960003910 promethazine Drugs 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 229960002601 protriptyline Drugs 0.000 description 1
- BWPIARFWQZKAIA-UHFFFAOYSA-N protriptyline Chemical compound C1=CC2=CC=CC=C2C(CCCNC)C2=CC=CC=C21 BWPIARFWQZKAIA-UHFFFAOYSA-N 0.000 description 1
- OGQDIIKRQRZXJH-UHFFFAOYSA-N protriptyline hydrochloride Chemical compound [Cl-].C1=CC2=CC=CC=C2C(CCC[NH2+]C)C2=CC=CC=C21 OGQDIIKRQRZXJH-UHFFFAOYSA-N 0.000 description 1
- 229960002290 pyridostigmine Drugs 0.000 description 1
- 229940076788 pyruvate Drugs 0.000 description 1
- MIXMJCQRHVAJIO-TZHJZOAOSA-N qk4dys664x Chemical compound O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O.C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O MIXMJCQRHVAJIO-TZHJZOAOSA-N 0.000 description 1
- 229960001404 quinidine Drugs 0.000 description 1
- 229960002720 reproterol Drugs 0.000 description 1
- WVLAAKXASPCBGT-UHFFFAOYSA-N reproterol Chemical compound C1=2C(=O)N(C)C(=O)N(C)C=2N=CN1CCCNCC(O)C1=CC(O)=CC(O)=C1 WVLAAKXASPCBGT-UHFFFAOYSA-N 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 229960001487 rimexolone Drugs 0.000 description 1
- QTTRZHGPGKRAFB-OOKHYKNYSA-N rimexolone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CC)(C)[C@@]1(C)C[C@@H]2O QTTRZHGPGKRAFB-OOKHYKNYSA-N 0.000 description 1
- 229960001457 rimiterol Drugs 0.000 description 1
- IYMMESGOJVNCKV-SKDRFNHKSA-N rimiterol Chemical compound C([C@@H]1[C@@H](O)C=2C=C(O)C(O)=CC=2)CCCN1 IYMMESGOJVNCKV-SKDRFNHKSA-N 0.000 description 1
- 229960001634 ritodrine Drugs 0.000 description 1
- IOVGROKTTNBUGK-SJCJKPOMSA-N ritodrine Chemical compound N([C@@H](C)[C@H](O)C=1C=CC(O)=CC=1)CCC1=CC=C(O)C=C1 IOVGROKTTNBUGK-SJCJKPOMSA-N 0.000 description 1
- 229950008133 ritolukast Drugs 0.000 description 1
- 229960004136 rivastigmine Drugs 0.000 description 1
- HJORMJIFDVBMOB-UHFFFAOYSA-N rolipram Chemical compound COC1=CC=C(C2CC(=O)NC2)C=C1OC1CCCC1 HJORMJIFDVBMOB-UHFFFAOYSA-N 0.000 description 1
- 229950005741 rolipram Drugs 0.000 description 1
- 229960002052 salbutamol Drugs 0.000 description 1
- 238000005070 sampling Methods 0.000 description 1
- STECJAGHUSJQJN-FWXGHANASA-N scopolamine Chemical compound C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-FWXGHANASA-N 0.000 description 1
- 229960002646 scopolamine Drugs 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 229950005229 sibenadet Drugs 0.000 description 1
- 229940105580 skelaxin Drugs 0.000 description 1
- 230000036620 skin dryness Effects 0.000 description 1
- 230000037321 sleepiness Effects 0.000 description 1
- 230000016160 smooth muscle contraction Effects 0.000 description 1
- 239000012064 sodium phosphate buffer Substances 0.000 description 1
- XNAYQOBPAXEYLI-UHFFFAOYSA-M sodium;3-[[3-[2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-[3-(dimethylamino)-3-oxopropyl]sulfanylmethyl]sulfanylpropanoate Chemical compound [Na+].CN(C)C(=O)CCSC(SCCC([O-])=O)C1=CC=CC(C=CC=2N=C3C=C(Cl)C=CC3=CC=2)=C1 XNAYQOBPAXEYLI-UHFFFAOYSA-M 0.000 description 1
- 239000007790 solid phase Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 229950007862 sulfonterol Drugs 0.000 description 1
- 229950009709 sulukast Drugs 0.000 description 1
- YPHOSUPSOWQQCB-AFOLHBCXSA-N sulukast Chemical compound CCCCCCCCC\C=C/C=C/[C@@H](SCCC(O)=O)[C@@H](O)C1=CC=CC(C2=NNN=N2)=C1 YPHOSUPSOWQQCB-AFOLHBCXSA-N 0.000 description 1
- 229940118176 surmontil Drugs 0.000 description 1
- 229960001685 tacrine Drugs 0.000 description 1
- YLJREFDVOIBQDA-UHFFFAOYSA-N tacrine Chemical compound C1=CC=C2C(N)=C(CCCC3)C3=NC2=C1 YLJREFDVOIBQDA-UHFFFAOYSA-N 0.000 description 1
- 229960000195 terbutaline Drugs 0.000 description 1
- 125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 description 1
- 229960002784 thioridazine Drugs 0.000 description 1
- 229940028300 tigan Drugs 0.000 description 1
- 229960005013 tiotixene Drugs 0.000 description 1
- 229950001669 tipredane Drugs 0.000 description 1
- 229940041597 tofranil Drugs 0.000 description 1
- MWYHLEQJTQJHSS-UHFFFAOYSA-N tomelukast Chemical compound C1=CC(C(C)=O)=C(O)C(CCC)=C1OCCCCC1=NNN=N1 MWYHLEQJTQJHSS-UHFFFAOYSA-N 0.000 description 1
- 229950010953 tomelukast Drugs 0.000 description 1
- 229960002117 triamcinolone acetonide Drugs 0.000 description 1
- YNDXUCZADRHECN-JNQJZLCISA-N triamcinolone acetonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O YNDXUCZADRHECN-JNQJZLCISA-N 0.000 description 1
- ZEWQUBUPAILYHI-UHFFFAOYSA-N trifluoperazine Chemical compound C1CN(C)CCN1CCCN1C2=CC(C(F)(F)F)=CC=C2SC2=CC=CC=C21 ZEWQUBUPAILYHI-UHFFFAOYSA-N 0.000 description 1
- 229960001032 trihexyphenidyl Drugs 0.000 description 1
- 229960002431 trimipramine Drugs 0.000 description 1
- ZSCDBOWYZJWBIY-UHFFFAOYSA-N trimipramine Chemical compound C1CC2=CC=CC=C2N(CC(CN(C)C)C)C2=CC=CC=C21 ZSCDBOWYZJWBIY-UHFFFAOYSA-N 0.000 description 1
- YDGHCKHAXOUQOS-BTJKTKAUSA-N trimipramine maleate Chemical compound [O-]C(=O)\C=C/C([O-])=O.C1CC2=CC=CC=C2[NH+](CC(C[NH+](C)C)C)C2=CC=CC=C21 YDGHCKHAXOUQOS-BTJKTKAUSA-N 0.000 description 1
- 229960000859 tulobuterol Drugs 0.000 description 1
- 229950008396 ulobetasol propionate Drugs 0.000 description 1
- BDSYKGHYMJNPAB-LICBFIPMSA-N ulobetasol propionate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H](C)[C@@](C(=O)CCl)(OC(=O)CC)[C@@]2(C)C[C@@H]1O BDSYKGHYMJNPAB-LICBFIPMSA-N 0.000 description 1
- 210000001635 urinary tract Anatomy 0.000 description 1
- 229950003905 verlukast Drugs 0.000 description 1
- 229940079707 vistaril Drugs 0.000 description 1
- 229940045977 vivactil Drugs 0.000 description 1
- 229960004764 zafirlukast 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- 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
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/04—Drugs for disorders of the respiratory system for throat disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pulmonology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Otolaryngology (AREA)
- Hospice & Palliative Care (AREA)
- Nutrition Science (AREA)
- Vascular Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
本発明は、特に、喘息および慢性閉塞性肺疾患(COPD)のような呼吸器疾患のための、抗ムスカリン化合物のクラス関連副作用(class−related adverse effect)を引き起こすことのない、抗コリン作動薬療法の新規方法に関する。
アクリジニウム(3(R)−(2−ヒドロキシ−2,2−ジチエン−2−イル アセトキシ)−1−(3−フェノキシプロピル)−1−アゾニアビシクロ[2.2.2]オクタン)は、例えばWO01/04118、WO05/115467、WO05/115466、およびWO05/115462(その内容は、参照により本明細書中に包含される。)に記載の、可能性のあるムスカリン受容体アンタゴニストである。アクリジニウムは、現在臨床試験中の、呼吸器疾患、とりわけ喘息およびCOPDの処置のための吸入による投与を目的とする長期作用性気管支拡張剤である。
今回、アクリジニウムが、患者を全身的に活性な抗ムスカリン化合物のクラス関連副作用の危険にさらすことなく、呼吸器疾患の処置において用いられ得ることを発見した。アクリジニウムは、例えばチオトロピウム(2−ヒドロキシ−2,2−ジチエン−2−イルアセトキシ)と同様にエステル基を有するが、吸入により投与されるアクリジニウムは、驚くべきことに、血漿中でその不活性な酸およびアルコール代謝物により分解されやすい。結果として、該化合物への全身暴露は、ほとんど影響がない。アクリジニウムの迅速な代謝のため、望ましくない全身性の抗コリン作用をもたらすという結果の可能性は低い。しかしながら、アクリジニウムは、受容体での長時間作用性を有し、そして肺および気道への抗ムスカリン療法の長期的効果を与え得る。
a.統合失調症、集中力低下、錯乱状態、動揺、せん妄、注意欠陥、記憶障害、呼吸抑制、
b.緑内障、ドライアイ、瞳孔の拡大、視覚低下、眼内圧上昇、
c.肥大または閉塞した前立腺、排尿困難、溢流性失禁、
d.小腸の狭窄または閉塞、肥大した結腸、慢性便秘、肥大した下部食道、低下した胃運動性、便秘、
e.口渇、のどの炎症、発汗障害
f.心血管疾患(再狭窄、動脈硬化症、過去の卒中または心臓発作、鬱血性心不全のいずれかを含む)、不整脈、頻脈、
g.パーキンソン病、アルツハイマー病、認知症、および/または
h.重症筋無力症
から選択される1種以上の状態を有するか、またはその状態になりやすい。
典型的に、該医薬は、単糖類、二糖類もしくは多糖類および糖アルコールから選択される薬学的に許容される担体を含む。好ましくは、担体はラクトースである。
抗コリン作用を有し得るか、または患者を抗コリン作用により感受性にし得る医薬には、例えば、
a.悪心または目眩のための薬剤、とりわけ抗コリン作動薬、例えばプロメタジン(Phenergan)、プロクロルペラジン(Compazine)、トリメトベンズアミド(Tigan)、メクリジン(Antivert)、シクリジン(Marezine)、スコポラアミン
b.パーキンソン病のための薬剤、とりわけ抗コリン作動薬、例えばベンズトロピン;ビペリデン;プロシクリジン;トリヘキシフェニジル;エトプロパジン(ethoproprazine)
c.抗鬱剤、とりわけ三環式抗鬱剤、例えばアミトリプチリン(Elavil)、ドキセピン(Sinequan)、イミプラミン(Tofranil)、トリミプラミン(Surmontil)、ノルトリプチリン(Pamelor)、プロトリプチリン(Vivactil)、アモキサピン(Asendin)、マプロチリン(Ludiomil)、クロミプラミン(Anafranil);デシプラミン(Norpramin)
d.抗ヒスタミン剤、とりわけ第一世代鎮静性抗ヒスタミン剤、例えばジフェンヒドラミン(Benadryl)、クロルフェニラミン(Chlor−Trimeton)、ヒドロキシジン(Atarax/Vistaril)、シプロヘプタジン(Periactin)
e.筋弛緩剤、例えば、メタキサロン(Skelaxin)、シクロベンザプリン(flexeril)、オルフェナドリン(Norflex)
f.ある種の抗偏頭痛薬、例えばベラドンナアルカロイド
g.ある種の抗下痢剤、例えば、ジフェノキシレート/アトロピン(Lomotil)
h.尿路およびGIの鎮痙薬、例えばオキシブチニン(Ditropan)、フラボキサート(Urispas)、ジシクロミン(Bentyl)、ヒヨスチアミン;ベラドンナアルカロイド類;トルテロジン(Detrol)、トロスピウム、クリンジニウム(clindinium);プロパンテリン、ピレンゼピン、テレンゼピン、
i.抗不整脈薬、例えばジソピラミド(Norpace)、プロカインアミド(Pronestyl)、キニジン、アトロピン
j.抗精神病薬、例えばクロルプロマジン(Thorazine)、チオリダジン(Mellaril)、クロザピン(クロザリル)、フルフェナジン(Stelazine)、チオチキセン(Navane)
が含まれる。
a.可逆性コリンエステラーゼ阻害剤、例えば、エドロホニウム、タクリン、ドネペジル、フィゾスチグミン、ピリドスチグミン、リバスチグミン、ガランタミン、ネオスチグミン、
b.コリン作動性アゴニスト、例えば、メタコリン、ベタネコール、ピロカルピン
が含まれる。
ヒト血漿中での、チオトロピウムおよびイプラトロピウムおよびグリコピロレートの安定性と比較した、アクリジニウムのインビトロ安定性
インビトロ実験を、36℃にて、5μg/mlの濃度で行う(各物質の6μlの1mg/mlジメチルスルホキシド溶液を、1.2mlの最終容量まで添加する)。3分間のプレインキュベーション後、反応を、試験物質の添加により開始する。0、5、15、30および60分の所定の時間で、血漿の100μlのアリコートを単離し、反応を、1mlの20mM、pH4.0酢酸ナトリウム緩衝溶液の添加により停止させる。試験物質を、対照反応用に緩衝液で置換する。ヒト血漿を、書面によるインフォームド・コンセントによりボランティアから入手する。血液を抗凝固剤としてヘパリンリチウムを含むチューブ中に集め、直ちに4℃で遠心し、得られる血漿を、使用しないときは−20℃で貯蔵する。
第I相臨床試験:臭化アクリジニウムを、アクリジニウムの活性、薬物動態および耐容性評価するための、フェーズI、二重盲検、部分的クロスオーバー、プラセボ対照試験で試験する。
第II相臨床試験:二重盲検、無作為化、プラセボ−対照、クロスオーバー試験は、アクリジニウムの薬理学、薬物動態学および耐容性、ならびにCOPD患者におけるその効果を評価する。
Claims (23)
- 患者に全身性の抗ムスカリン作用を生じることなく、吸入により該患者における呼吸器疾患または状態の処置または予防に使用するための医薬の製造における、アクリジニウムの使用。
- 該呼吸器疾患が、ムスカリン受容体アンタゴニストにより処置、改善または阻止され得る疾患である、請求項1記載の使用。
- 該呼吸器疾患または状態が、急性もしくは慢性気管支炎、気腫、喘息および慢性閉塞性肺疾患、とりわけ喘息および慢性閉塞性肺疾患から選択される、請求項1および2の何れか一項記載の使用。
- 該患者が、全身性の抗ムスカリン活性により悪化され得る状態を有するか、またはその状態になりやすい、請求項1ないし3の何れか一項記載の使用。
- 該患者が、
i.統合失調症、集中力低下、錯乱、動揺、せん妄、注意欠陥、記憶障害、呼吸抑制、
ii.緑内障、ドライアイ、瞳孔の拡大、視覚低下、眼内圧上昇、
iii.肥大または閉塞した前立腺、排尿困難、
iv.小腸の狭窄または閉塞、肥大した結腸、慢性便秘、肥大した下部食道、低下した胃運動性、便秘、
v.口渇、のどの炎症、発汗障害、
vi.心血管疾患(再狭窄、動脈硬化症、過去の卒中もしくは心臓発作、鬱血性心不全のいずれかを含む)、不整脈、頻脈、
vii.パーキンソン病、アルツハイマー病、認知症、ならびに
viii.重症筋無力症
から選択される1個以上の状態を有するか、またはその状態になりやすい、請求項4記載の使用。 - 該患者が男性である、請求項1ないし5の何れか一項記載の使用。
- 該患者が年齢60歳以上である、請求項1ないし6のいずれか一項記載の使用。
- 該患者が、処置過程中に機械を運転または操作することを予定する、請求項1ないし7のいずれか一項記載の使用。
- 該患者が、全身的に活性な抗コリン作動薬である第二剤、または請求項5に記載のいずれかの状態を引き起こすか、もしくは悪化させ得る薬物を受容している、請求項1ないし8のいずれか一項記載の使用。
- 該第二剤が、非定型抗精神病薬、三環式抗鬱剤、および抗ヒスタミン剤から選択される、請求項9記載の使用。
- 該患者が、アセチルコリン作用を増大することを目的とする薬剤を受容している、請求項1ないし10のいずれか一項記載の使用。
- 該アクリジニウムが、臭化アクリジニウムの形態である、請求項1ないし11のいずれか一項記載の使用。
- 該アクリジニウムが、吸入に適する乾燥粉末の形態である、請求項1ないし12のいずれか一項記載の使用。
- 該医薬が、単糖類、二糖類もしくは多糖類および糖アルコールから選択される薬学的に許容される担体を含む、請求項1ないし13のいずれか一項記載の使用。
- 該担体がラクトースである、請求項14記載の使用。
- 避けられるべき全身性の抗ムスカリン作用が、口渇、のどの炎症、発汗抑制、瞳孔の拡大、視覚低下、眼内圧上昇、心拍数増加、胸痛、排尿困難、肥大または閉塞した前立腺、低下した胃運動性、便秘、集中力低下、錯乱状態、動揺、せん妄、注意欠陥、記憶障害、および呼吸抑制から選択される、請求項1ないし15のいずれか一項記載の使用。
- 該患者が、呼吸器疾患または状態の処置のための1個以上の付加的医薬を受容する、請求項1ないし16のいずれか一項記載の使用。
- 呼吸器疾患または状態の処置のための付加的医薬が、ベータ−アドレナリンアゴニスト、コルチコステロイドもしくはグルココルチコイド、PDE IV阻害剤、抗ヒスタミン剤、抗IgE抗体、ロイコトリエンD4阻害剤、egfr−キナーゼの阻害剤、p38キナーゼ阻害剤および/またはNK1−受容体アンタゴニストから選択される、請求項17記載の使用。
- 該付加的医薬が、コルチコステロイドおよび/またはベータ−アドレナリンアゴニストから選択される、請求項18記載の使用。
- 請求項1および16のいずれか一項記載の該患者における全身性の抗ムスカリン作用を生じることなく、請求項1、4ないし11および17ないし19のいずれか一項記載の該患者において、請求項1ないし3のいずれか一項記載の呼吸器疾患または状態の吸入による処置または予防に使用するための、請求項1、12および13のいずれか一項記載のアクリジニウム、または請求項1、14および15のいずれか一項記載の医薬。
- かかる処置の必要な患者(患者は、請求項1、4ないし11および17ないし19のいずれか一項に定義の通りである。)における、請求項1および16のいずれか一項記載の全身性の抗ムスカリン作用を該患者に生じることなく、請求項1ないし3のいずれか一項記載の呼吸器疾患または状態を吸入により処置または予防する方法であって、有効量の、請求項1、12および13のいずれか一項記載のアクリジニウムまたは請求項14もしくは15に記載の医薬を該患者に投与することを含む、方法。
- 請求項1、4ないし11および17ないし19のいずれか一項に定義の患者における、請求項1または16に記載の該患者における全身性の抗ムスカリン作用を生じることのない、請求項1ないし3のいずれか一項記載の呼吸器疾患または状態の吸入による処置または予防における使用のための医薬組成物であって、薬学的に許容される担体、および有効成分として、請求項1、12および13のいずれか一項記載のアクリジニウムを含む、医薬組成物。
- 該薬学的に許容される担体が、請求項14または15に記載のものである、請求項22記載の組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US90284307P | 2007-02-21 | 2007-02-21 | |
US60/902,843 | 2007-02-21 | ||
PCT/EP2008/000782 WO2008101591A1 (en) | 2007-02-21 | 2008-01-31 | Novel methods |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2013252283A Division JP2014062114A (ja) | 2007-02-21 | 2013-12-05 | 新規方法 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2010519261A true JP2010519261A (ja) | 2010-06-03 |
JP2010519261A5 JP2010519261A5 (ja) | 2011-02-10 |
JP5739616B2 JP5739616B2 (ja) | 2015-06-24 |
Family
ID=39247776
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009550665A Active JP5739616B2 (ja) | 2007-02-21 | 2008-01-31 | 新規方法 |
JP2013252283A Pending JP2014062114A (ja) | 2007-02-21 | 2013-12-05 | 新規方法 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2013252283A Pending JP2014062114A (ja) | 2007-02-21 | 2013-12-05 | 新規方法 |
Country Status (32)
Country | Link |
---|---|
US (2) | US20110243924A1 (ja) |
EP (1) | EP2120936B1 (ja) |
JP (2) | JP5739616B2 (ja) |
KR (2) | KR20090114401A (ja) |
CN (2) | CN101616670A (ja) |
AR (1) | AR065392A1 (ja) |
AT (1) | ATE513547T1 (ja) |
AU (1) | AU2008217301B2 (ja) |
BR (1) | BRPI0806392A8 (ja) |
CA (1) | CA2678975C (ja) |
CL (1) | CL2008000461A1 (ja) |
CO (1) | CO6210814A2 (ja) |
CY (1) | CY1111799T1 (ja) |
DK (1) | DK2120936T3 (ja) |
EC (1) | ECSP099556A (ja) |
ES (1) | ES2367722T3 (ja) |
HK (1) | HK1132673A1 (ja) |
HR (1) | HRP20110556T1 (ja) |
IL (1) | IL200278A (ja) |
MX (1) | MX2009008825A (ja) |
MY (1) | MY153408A (ja) |
NZ (1) | NZ578473A (ja) |
PE (1) | PE20081789A1 (ja) |
PL (1) | PL2120936T3 (ja) |
PT (1) | PT2120936E (ja) |
RU (1) | RU2484821C2 (ja) |
SI (1) | SI2120936T1 (ja) |
TW (1) | TWI475994B (ja) |
UA (1) | UA98136C2 (ja) |
UY (1) | UY30901A (ja) |
WO (1) | WO2008101591A1 (ja) |
ZA (1) | ZA200904941B (ja) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2022528813A (ja) * | 2020-05-20 | 2022-06-16 | シンテカバイオ インコーポレイティッド | 二類重症急性呼吸器症候群コロナウイルス感染症の予防または治療用組成物 |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2165768B1 (es) | 1999-07-14 | 2003-04-01 | Almirall Prodesfarma Sa | Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen. |
EP2100598A1 (en) | 2008-03-13 | 2009-09-16 | Laboratorios Almirall, S.A. | Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease |
EP2100599A1 (en) | 2008-03-13 | 2009-09-16 | Laboratorios Almirall, S.A. | Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease |
NZ597920A (en) | 2009-08-07 | 2014-05-30 | Generics Uk Ltd | Anhydrate of tiotropium bromide |
WO2011095800A2 (en) * | 2010-02-02 | 2011-08-11 | Generics [Uk] Limited | Analytical methods |
EP2510928A1 (en) | 2011-04-15 | 2012-10-17 | Almirall, S.A. | Aclidinium for use in improving the quality of sleep in respiratory patients |
WO2014007772A2 (en) | 2012-07-05 | 2014-01-09 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Inhalation compositions comprising glucose anhydrous |
WO2014007771A2 (en) | 2012-07-05 | 2014-01-09 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Inhalation compositions comprising muscarinic receptor antagonist |
WO2014007767A1 (en) * | 2012-07-05 | 2014-01-09 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Dry powder inhalers comprising a carrier other than lactose and a ternary component |
WO2018129434A1 (en) | 2017-01-09 | 2018-07-12 | Gt Biopharma, Inc. | Use and composition for treating myasthenia gravis and other myasthenic syndromes |
WO2019023175A1 (en) * | 2017-07-25 | 2019-01-31 | Gt Biopharma, Inc. | PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE AND NEOSTIGMINE AND AN ANTAGONIST NK-1 FOR THE TREATMENT OF SEVERE MYASTHENIA |
WO2019023318A1 (en) * | 2017-07-25 | 2019-01-31 | Gt Biopharma, Inc. | PHARMACEUTICAL COMPOSITIONS AND METHODS USING PYRIDOSTIGMINE AND AN ANTAGONIST OF NK-1 FOR TREATING SEVERE MYASTHENIA |
WO2020014072A1 (en) * | 2018-07-09 | 2020-01-16 | Gt Biopharma, Inc. | Neostigmine pharmaceutical combination for treating myasthenia gravis |
KR102169476B1 (ko) * | 2020-05-20 | 2020-10-23 | (주)신테카바이오 | 제2형 중증급성호흡기증후군 코로나바이러스 감염 질환의 예방 또는 치료용 조성물 |
CN115267024B (zh) * | 2022-07-31 | 2023-06-30 | 浙江知一药业有限责任公司 | 治疗呼吸系统疾病的药物组合物及其检测方法 |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2003504368A (ja) * | 1999-07-14 | 2003-02-04 | アルミラル・プロデスフアルマ・エス・エイ | キヌクリジン誘導体およびそれらのムスカリンm3レセプターリガンドとしての使用 |
WO2005115466A1 (en) * | 2004-05-31 | 2005-12-08 | Almirall Prodesfarma S.A. | Combinations comprising antimuscarinic agents and corticosteroids |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20050026948A1 (en) * | 2003-07-29 | 2005-02-03 | Boehringer Ingelheim International Gmbh | Medicaments for inhalation comprising an anticholinergic and a betamimetic |
DE102004016179A1 (de) * | 2004-03-30 | 2005-10-20 | Boehringer Ingelheim Pharma | Verbindungen zur Behandlung von proliferativen Prozessen |
-
2008
- 2008-01-31 CN CN200880005871A patent/CN101616670A/zh active Pending
- 2008-01-31 SI SI200830381T patent/SI2120936T1/sl unknown
- 2008-01-31 CA CA2678975A patent/CA2678975C/en active Active
- 2008-01-31 RU RU2009135078/15A patent/RU2484821C2/ru active
- 2008-01-31 AT AT08707469T patent/ATE513547T1/de active
- 2008-01-31 DK DK08707469.6T patent/DK2120936T3/da active
- 2008-01-31 KR KR1020097017243A patent/KR20090114401A/ko not_active Application Discontinuation
- 2008-01-31 MX MX2009008825A patent/MX2009008825A/es active IP Right Grant
- 2008-01-31 KR KR20157007787A patent/KR20150038750A/ko not_active Application Discontinuation
- 2008-01-31 ES ES08707469T patent/ES2367722T3/es active Active
- 2008-01-31 MY MYPI20093444A patent/MY153408A/en unknown
- 2008-01-31 WO PCT/EP2008/000782 patent/WO2008101591A1/en active Application Filing
- 2008-01-31 BR BRPI0806392A patent/BRPI0806392A8/pt not_active Application Discontinuation
- 2008-01-31 US US12/528,267 patent/US20110243924A1/en not_active Abandoned
- 2008-01-31 JP JP2009550665A patent/JP5739616B2/ja active Active
- 2008-01-31 UA UAA200909464A patent/UA98136C2/ru unknown
- 2008-01-31 CN CN201510633145.XA patent/CN105395548A/zh active Pending
- 2008-01-31 PL PL08707469T patent/PL2120936T3/pl unknown
- 2008-01-31 EP EP08707469A patent/EP2120936B1/en active Active
- 2008-01-31 PT PT08707469T patent/PT2120936E/pt unknown
- 2008-01-31 AU AU2008217301A patent/AU2008217301B2/en active Active
- 2008-01-31 NZ NZ578473A patent/NZ578473A/en unknown
- 2008-02-07 UY UY0001030901A patent/UY30901A/es unknown
- 2008-02-13 CL CL200800461A patent/CL2008000461A1/es unknown
- 2008-02-20 TW TW097105887A patent/TWI475994B/zh not_active IP Right Cessation
- 2008-02-20 PE PE2008000361A patent/PE20081789A1/es not_active Application Discontinuation
- 2008-02-20 AR ARP080100680A patent/AR065392A1/es unknown
-
2009
- 2009-07-15 ZA ZA2009/04941A patent/ZA200904941B/en unknown
- 2009-08-04 EC EC2009009556A patent/ECSP099556A/es unknown
- 2009-08-06 IL IL200278A patent/IL200278A/en active IP Right Grant
- 2009-08-21 CO CO09088171A patent/CO6210814A2/es not_active Application Discontinuation
-
2010
- 2010-01-05 HK HK10100031.9A patent/HK1132673A1/xx unknown
-
2011
- 2011-07-26 HR HR20110556T patent/HRP20110556T1/hr unknown
- 2011-08-31 CY CY20111100836T patent/CY1111799T1/el unknown
-
2013
- 2013-12-05 JP JP2013252283A patent/JP2014062114A/ja active Pending
-
2014
- 2014-12-05 US US14/561,857 patent/US20150093374A1/en not_active Abandoned
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2003504368A (ja) * | 1999-07-14 | 2003-02-04 | アルミラル・プロデスフアルマ・エス・エイ | キヌクリジン誘導体およびそれらのムスカリンm3レセプターリガンドとしての使用 |
WO2005115466A1 (en) * | 2004-05-31 | 2005-12-08 | Almirall Prodesfarma S.A. | Combinations comprising antimuscarinic agents and corticosteroids |
WO2005115462A1 (en) * | 2004-05-31 | 2005-12-08 | Almirall Prodesfarma S.A. | Combinations comprising antimuscarinic agents and pde4 inhibitors |
JP2006527183A (ja) * | 2004-05-31 | 2006-11-30 | アルミラル プロデスファルマ ソシエダッド アノニマ | 抗ムスカリン剤およびベータ−アドレナリンアゴニストを含む組み合わせ |
JP2008500986A (ja) * | 2004-05-31 | 2008-01-17 | ラボラトリオス・アルミラル・ソシエダッド・アノニマ | 抗ムスカリン剤およびpde4阻害剤を含む組合せ剤 |
JP2008500990A (ja) * | 2004-05-31 | 2008-01-17 | ラボラトリオス・アルミラル・ソシエダッド・アノニマ | 抗ムスカリン剤およびコルチコステロイドを含む組合せ剤 |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2022528813A (ja) * | 2020-05-20 | 2022-06-16 | シンテカバイオ インコーポレイティッド | 二類重症急性呼吸器症候群コロナウイルス感染症の予防または治療用組成物 |
JP7104449B2 (ja) | 2020-05-20 | 2022-07-21 | シンテカバイオ インコーポレイティッド | 二類重症急性呼吸器症候群コロナウイルス感染症の予防または治療用組成物 |
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP5739616B2 (ja) | 新規方法 | |
ES2257152B1 (es) | Combinaciones que comprenden agentes antimuscarinicos y agonistas beta-adrenergicos. | |
US20050175548A1 (en) | Combination of anticholinergics and glucocorticoids for the long-term treatment of asthma and COPD | |
JP2010519261A5 (ja) | ||
US20110224177A1 (en) | Combinations comprising antimuscarinic agents and corticosteroids | |
JP6322570B2 (ja) | 呼吸器疾患患者において睡眠の質を改善するために用いるアクリジニウム | |
US20080254022A1 (en) | Method of Treating Airway Diseases With Beta-Adrenergic Inverse Agonists | |
US11571412B2 (en) | Thromboxane receptor antagonists in AERD/asthma | |
TW201427660A (zh) | 阿地銨之新用途 | |
TW201302195A (zh) | 阿地銨(aclidinium)之新用途 | |
NZ707754A (en) | Combination of glycopyrrolate and a beta2 -agonist |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20101216 |
|
A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20101216 |
|
A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20130108 |
|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20130328 |
|
A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20130806 |
|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20131205 |
|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A821 Effective date: 20140115 |
|
A911 | Transfer to examiner for re-examination before appeal (zenchi) |
Free format text: JAPANESE INTERMEDIATE CODE: A911 Effective date: 20140210 |
|
A912 | Re-examination (zenchi) completed and case transferred to appeal board |
Free format text: JAPANESE INTERMEDIATE CODE: A912 Effective date: 20140328 |
|
A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20141118 |
|
A602 | Written permission of extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A602 Effective date: 20141125 |
|
A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20141218 |
|
A602 | Written permission of extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A602 Effective date: 20141224 |
|
A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20150116 |
|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20150319 |
|
A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20150424 |
|
R150 | Certificate of patent or registration of utility model |
Ref document number: 5739616 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |