UA73619C2 - Stable pharmaceutical compositions of nmda receptor agonist (variants) and method of treatment - Google Patents
Stable pharmaceutical compositions of nmda receptor agonist (variants) and method of treatment Download PDFInfo
- Publication number
- UA73619C2 UA73619C2 UA2003065485A UA2003065485A UA73619C2 UA 73619 C2 UA73619 C2 UA 73619C2 UA 2003065485 A UA2003065485 A UA 2003065485A UA 2003065485 A UA2003065485 A UA 2003065485A UA 73619 C2 UA73619 C2 UA 73619C2
- Authority
- UA
- Ukraine
- Prior art keywords
- pharmaceutical composition
- free
- pharmaceutically acceptable
- composition according
- disease
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 34
- 238000000034 method Methods 0.000 title claims abstract description 23
- 239000003706 n methyl dextro aspartic acid receptor stimulating agent Substances 0.000 title abstract 2
- 210000003169 central nervous system Anatomy 0.000 claims abstract description 12
- 208000024827 Alzheimer disease Diseases 0.000 claims abstract description 10
- 208000006011 Stroke Diseases 0.000 claims abstract description 8
- 208000015122 neurodegenerative disease Diseases 0.000 claims abstract description 8
- 206010046543 Urinary incontinence Diseases 0.000 claims abstract description 7
- 206010015037 epilepsy Diseases 0.000 claims abstract description 7
- 208000023105 Huntington disease Diseases 0.000 claims abstract description 6
- 208000013016 Hypoglycemia Diseases 0.000 claims abstract description 6
- 208000019695 Migraine disease Diseases 0.000 claims abstract description 6
- 208000002193 Pain Diseases 0.000 claims abstract description 6
- 208000028017 Psychotic disease Diseases 0.000 claims abstract description 6
- 201000004810 Vascular dementia Diseases 0.000 claims abstract description 6
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims abstract description 6
- 206010013663 drug dependence Diseases 0.000 claims abstract description 6
- 230000002218 hypoglycaemic effect Effects 0.000 claims abstract description 6
- 230000000302 ischemic effect Effects 0.000 claims abstract description 6
- 206010027599 migraine Diseases 0.000 claims abstract description 6
- 208000011117 substance-related disease Diseases 0.000 claims abstract description 6
- 208000018737 Parkinson disease Diseases 0.000 claims abstract description 5
- 206010039966 Senile dementia Diseases 0.000 claims abstract description 5
- 208000030886 Traumatic Brain injury Diseases 0.000 claims abstract description 5
- 230000009529 traumatic brain injury Effects 0.000 claims abstract description 5
- 206010012289 Dementia Diseases 0.000 claims abstract description 3
- 239000000203 mixture Substances 0.000 claims description 52
- 239000000872 buffer Substances 0.000 claims description 20
- 229910021645 metal ion Inorganic materials 0.000 claims description 20
- 150000003839 salts Chemical class 0.000 claims description 20
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 12
- 239000001301 oxygen Substances 0.000 claims description 12
- 229910052760 oxygen Inorganic materials 0.000 claims description 12
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 11
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 10
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims description 9
- 239000007864 aqueous solution Substances 0.000 claims description 9
- 239000002738 chelating agent Substances 0.000 claims description 9
- XEEYBQQBJWHFJM-UHFFFAOYSA-N iron Substances [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 9
- -1 iron ion Chemical class 0.000 claims description 9
- 229940095064 tartrate Drugs 0.000 claims description 9
- JPVYNHNXODAKFH-UHFFFAOYSA-N Cu2+ Chemical compound [Cu+2] JPVYNHNXODAKFH-UHFFFAOYSA-N 0.000 claims description 8
- 229910001431 copper ion Inorganic materials 0.000 claims description 8
- 239000007857 degradation product Substances 0.000 claims description 8
- 229910052742 iron Inorganic materials 0.000 claims description 8
- 208000019901 Anxiety disease Diseases 0.000 claims description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 6
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical group OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 6
- 241000124008 Mammalia Species 0.000 claims description 6
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 6
- RGHHSNMVTDWUBI-UHFFFAOYSA-N 4-hydroxybenzaldehyde Chemical compound OC1=CC=C(C=O)C=C1 RGHHSNMVTDWUBI-UHFFFAOYSA-N 0.000 claims description 5
- 208000020431 spinal cord injury Diseases 0.000 claims description 5
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical group CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims description 4
- 150000001450 anions Chemical class 0.000 claims description 4
- KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims description 4
- BDAGIHXWWSANSR-UHFFFAOYSA-M Formate Chemical compound [O-]C=O BDAGIHXWWSANSR-UHFFFAOYSA-M 0.000 claims description 3
- 238000003860 storage Methods 0.000 claims description 3
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims description 2
- 230000009920 chelation Effects 0.000 claims description 2
- 239000001384 succinic acid Substances 0.000 claims description 2
- 239000011975 tartaric acid Substances 0.000 claims description 2
- 235000002906 tartaric acid Nutrition 0.000 claims description 2
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 150000003893 lactate salts Chemical group 0.000 claims 1
- 238000012876 topography Methods 0.000 claims 1
- 210000000748 cardiovascular system Anatomy 0.000 abstract description 4
- 238000001356 surgical procedure Methods 0.000 abstract description 4
- 208000030507 AIDS Diseases 0.000 abstract description 2
- 208000014674 injury Diseases 0.000 abstract description 2
- 210000000278 spinal cord Anatomy 0.000 abstract description 2
- 230000008733 trauma Effects 0.000 abstract description 2
- QEMSVZNTSXPFJA-HNAYVOBHSA-N 1-[(1s,2s)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl]-4-phenylpiperidin-4-ol Chemical compound C1([C@H](O)[C@H](C)N2CCC(O)(CC2)C=2C=CC=CC=2)=CC=C(O)C=C1 QEMSVZNTSXPFJA-HNAYVOBHSA-N 0.000 abstract 1
- 208000005314 Multi-Infarct Dementia Diseases 0.000 abstract 1
- 239000002249 anxiolytic agent Substances 0.000 abstract 1
- 230000000949 anxiolytic effect Effects 0.000 abstract 1
- 230000001010 compromised effect Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 description 50
- 239000000243 solution Substances 0.000 description 22
- 230000015556 catabolic process Effects 0.000 description 10
- 239000008380 degradant Substances 0.000 description 10
- 238000006731 degradation reaction Methods 0.000 description 10
- 230000000694 effects Effects 0.000 description 8
- 229920000642 polymer Polymers 0.000 description 7
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 6
- 239000000306 component Substances 0.000 description 6
- 239000012895 dilution Substances 0.000 description 6
- 238000010790 dilution Methods 0.000 description 6
- 230000001954 sterilising effect Effects 0.000 description 6
- 238000004659 sterilization and disinfection Methods 0.000 description 6
- 229910021655 trace metal ion Inorganic materials 0.000 description 6
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 5
- 239000005557 antagonist Substances 0.000 description 5
- 239000012458 free base Substances 0.000 description 5
- 102000005962 receptors Human genes 0.000 description 5
- 108020003175 receptors Proteins 0.000 description 5
- 239000012086 standard solution Substances 0.000 description 5
- KQKFQBTWXOGINC-UHFFFAOYSA-N 4-phenylpiperidin-4-ol Chemical compound C=1C=CC=CC=1C1(O)CCNCC1 KQKFQBTWXOGINC-UHFFFAOYSA-N 0.000 description 4
- XKRFYHLGVUSROY-UHFFFAOYSA-N Argon Chemical compound [Ar] XKRFYHLGVUSROY-UHFFFAOYSA-N 0.000 description 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 4
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 4
- 238000005481 NMR spectroscopy Methods 0.000 description 4
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 4
- 238000002474 experimental method Methods 0.000 description 4
- 238000002560 therapeutic procedure Methods 0.000 description 4
- 206010065040 AIDS dementia complex Diseases 0.000 description 3
- 208000012902 Nervous system disease Diseases 0.000 description 3
- 208000025966 Neurological disease Diseases 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- 239000004480 active ingredient Substances 0.000 description 3
- 239000007853 buffer solution Substances 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 230000002860 competitive effect Effects 0.000 description 3
- 230000007423 decrease Effects 0.000 description 3
- 239000007789 gas Substances 0.000 description 3
- 238000004128 high performance liquid chromatography Methods 0.000 description 3
- 239000011261 inert gas Substances 0.000 description 3
- LKGCPYOBWLSCTK-UHFFFAOYSA-N methanesulfonic acid;trihydrate Chemical compound O.O.O.CS(O)(=O)=O LKGCPYOBWLSCTK-UHFFFAOYSA-N 0.000 description 3
- 239000011780 sodium chloride Substances 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
- IAZDPXIOMUYVGZ-WFGJKAKNSA-N Dimethyl sulfoxide Chemical compound [2H]C([2H])([2H])S(=O)C([2H])([2H])[2H] IAZDPXIOMUYVGZ-WFGJKAKNSA-N 0.000 description 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 229910052786 argon Inorganic materials 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- 239000007979 citrate buffer Substances 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 238000001802 infusion Methods 0.000 description 2
- 238000001990 intravenous administration Methods 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 229910052757 nitrogen Inorganic materials 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 239000002464 receptor antagonist Substances 0.000 description 2
- 229940044551 receptor antagonist Drugs 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- BDERNNFJNOPAEC-UHFFFAOYSA-N 1-propanol Substances CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 1
- 229940006190 2,3-dimercapto-1-propanesulfonic acid Drugs 0.000 description 1
- JLVSRWOIZZXQAD-UHFFFAOYSA-N 2,3-disulfanylpropane-1-sulfonic acid Chemical compound OS(=O)(=O)CC(S)CS JLVSRWOIZZXQAD-UHFFFAOYSA-N 0.000 description 1
- 201000006474 Brain Ischemia Diseases 0.000 description 1
- 206010008120 Cerebral ischaemia Diseases 0.000 description 1
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 description 1
- QXNVGIXVLWOKEQ-UHFFFAOYSA-N Disodium Chemical compound [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 description 1
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical compound NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 description 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 1
- 239000004471 Glycine Substances 0.000 description 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 description 1
- 208000007101 Muscle Cramp Diseases 0.000 description 1
- 102100039506 Organic solute transporter subunit alpha Human genes 0.000 description 1
- 208000005392 Spasm Diseases 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 235000001014 amino acid Nutrition 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
- 230000015572 biosynthetic process Effects 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
- 230000037396 body weight Effects 0.000 description 1
- 208000029028 brain injury Diseases 0.000 description 1
- 230000005587 bubbling Effects 0.000 description 1
- 239000008366 buffered solution Substances 0.000 description 1
- 238000004364 calculation method Methods 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 206010008118 cerebral infarction Diseases 0.000 description 1
- 239000013522 chelant Substances 0.000 description 1
- 238000002144 chemical decomposition reaction Methods 0.000 description 1
- 239000012141 concentrate Substances 0.000 description 1
- 238000011109 contamination Methods 0.000 description 1
- 229910052802 copper Inorganic materials 0.000 description 1
- 239000010949 copper Substances 0.000 description 1
- 230000002939 deleterious effect Effects 0.000 description 1
- 230000000368 destabilizing effect Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 230000002461 excitatory amino acid Effects 0.000 description 1
- 239000003257 excitatory amino acid Substances 0.000 description 1
- 230000009540 excitatory neurotransmission Effects 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 239000005308 flint glass Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 235000013922 glutamic acid Nutrition 0.000 description 1
- 239000004220 glutamic acid Substances 0.000 description 1
- 230000003400 hallucinatory effect Effects 0.000 description 1
- 239000001307 helium Substances 0.000 description 1
- 229910052734 helium Inorganic materials 0.000 description 1
- SWQJXJOGLNCZEY-UHFFFAOYSA-N helium atom Chemical compound [He] SWQJXJOGLNCZEY-UHFFFAOYSA-N 0.000 description 1
- VKWVKRZCWUQLHV-UHFFFAOYSA-N hex-3-ene-1,6-diamine Chemical group NCCC=CCCN VKWVKRZCWUQLHV-UHFFFAOYSA-N 0.000 description 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 239000012535 impurity Substances 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 150000002500 ions Chemical group 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 150000002739 metals Chemical class 0.000 description 1
- 230000000926 neurological effect Effects 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 238000010525 oxidative degradation reaction Methods 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 230000000737 periodic effect Effects 0.000 description 1
- 239000005426 pharmaceutical component Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- LVTJOONKWUXEFR-FZRMHRINSA-N protoneodioscin Natural products O(C[C@@H](CC[C@]1(O)[C@H](C)[C@@H]2[C@]3(C)[C@H]([C@H]4[C@@H]([C@]5(C)C(=CC4)C[C@@H](O[C@@H]4[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@@H](O)[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@H](CO)O4)CC5)CC3)C[C@@H]2O1)C)[C@H]1[C@H](O)[C@H](O)[C@H](O)[C@@H](CO)O1 LVTJOONKWUXEFR-FZRMHRINSA-N 0.000 description 1
- 238000004007 reversed phase HPLC Methods 0.000 description 1
- 101150101156 slc51a gene Proteins 0.000 description 1
- ACTRVOBWPAIOHC-XIXRPRMCSA-N succimer Chemical compound OC(=O)[C@@H](S)[C@@H](S)C(O)=O ACTRVOBWPAIOHC-XIXRPRMCSA-N 0.000 description 1
- 229960005346 succimer Drugs 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 238000011477 surgical intervention Methods 0.000 description 1
- 230000005062 synaptic transmission Effects 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 229910001428 transition metal ion Inorganic materials 0.000 description 1
- QXJQHYBHAIHNGG-UHFFFAOYSA-N trimethylolethane Chemical compound OCC(C)(CO)CO QXJQHYBHAIHNGG-UHFFFAOYSA-N 0.000 description 1
- MBYLVOKEDDQJDY-UHFFFAOYSA-N tris(2-aminoethyl)amine Chemical compound NCCN(CCN)CCN MBYLVOKEDDQJDY-UHFFFAOYSA-N 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
Classifications
-
- 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
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
- A61K47/02—Inorganic compounds
-
- 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
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/14—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
- A61P25/22—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
- A61P25/28—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
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- 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
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- 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)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Inorganic Chemistry (AREA)
- Diabetes (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Psychology (AREA)
- Emergency Medicine (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25537200P | 2000-12-13 | 2000-12-13 | |
| PCT/IB2001/002359 WO2002047685A2 (en) | 2000-12-13 | 2001-12-05 | Nmda receptor agonist pharmaceutical compositions |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UA73619C2 true UA73619C2 (en) | 2005-08-15 |
Family
ID=22968017
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UA2003065485A UA73619C2 (en) | 2000-12-13 | 2001-05-12 | Stable pharmaceutical compositions of nmda receptor agonist (variants) and method of treatment |
Country Status (42)
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104383542B (zh) | 2003-04-08 | 2017-09-26 | 普罗热尼奇制药公司 | 包含甲基纳曲酮的药物配方 |
| TW200800959A (en) * | 2005-06-10 | 2008-01-01 | Wyeth Corp | Piperazine-piperidine antagonists and agonists of the 5-HT1a receptor |
| TW200808740A (en) * | 2006-06-09 | 2008-02-16 | Wyeth Corp | Succinate salts of 6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline and crystalline forms thereof |
| TW200811144A (en) * | 2006-06-09 | 2008-03-01 | Wyeth Corp | Crystalline forms of 6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline |
| TW200808741A (en) * | 2006-06-09 | 2008-02-16 | Wyeth Corp | 6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline hydrochloric acid salts |
| US20080262228A1 (en) * | 2006-11-28 | 2008-10-23 | Wyeth | Metabolites of 5-fluoro-8- quinoline and methods of preparation and uses thereof |
| TW200901974A (en) * | 2007-01-16 | 2009-01-16 | Wyeth Corp | Compounds, compositions, and methods of making and using them |
| CN101317844B (zh) * | 2007-06-08 | 2010-11-17 | 章劲夫 | 化合物(+)-5-甲基-10，11-二氢-5H-二苯并〔a，d〕环庚烯-5，10-亚胺在制备避孕药物中的应用 |
| AU2009293164B2 (en) | 2008-09-18 | 2015-07-09 | Northwestern University | NMDA receptor modulators and uses thereof |
| US8951968B2 (en) | 2009-10-05 | 2015-02-10 | Northwestern University | Methods of treating depression and other related diseases |
| BR112012020142A2 (pt) | 2010-02-11 | 2020-08-18 | Northwestern University | moduladores do receptor de nmda com estrutura secundária estabilizada e usos dos mesmos. |
| KR101692275B1 (ko) | 2010-02-11 | 2017-01-04 | 노오쓰웨스턴 유니버시티 | ２차 구조 안정화된 ｎｍｄａ 수용체 조절제 및 그의 용도 |
| CN102586243A (zh) * | 2012-03-08 | 2012-07-18 | 中国人民解放军军事医学科学院放射与辐射医学研究所 | 一种预防电磁辐射致脑损伤的标志物 |
| WO2014078568A1 (en) | 2012-11-14 | 2014-05-22 | The Johns Hopkins University | Methods and compositions for treating schizophrenia |
| US9758525B2 (en) | 2013-01-29 | 2017-09-12 | Aptinyx Inc. | Spiro-lactam NMDA receptor modulators and uses thereof |
| TR201908596T4 (tr) | 2013-01-29 | 2019-07-22 | Aptinyx Inc | Spiro-laktam NMDA reseptörü modülatörleri ve bunların kullanımları. |
| EP2951185B1 (en) | 2013-01-29 | 2016-12-21 | Aptinyx Inc. | Spiro-lactam nmda receptor modulators and uses thereof |
| AU2014212485C1 (en) | 2013-01-29 | 2018-10-25 | Aptinyx, Inc. | Spiro-lactam NMDA receptor modulators and uses thereof |
| MX2015009778A (es) | 2013-01-29 | 2016-02-09 | Aptinyx Inc | Moduladores de receptores nmda de espiro-lactama y sus usos. |
| CN105934247A (zh) | 2013-12-23 | 2016-09-07 | 株式会社三养生物制药 | 包含帕洛诺司琼的药物组合物 |
| WO2017201285A1 (en) | 2016-05-19 | 2017-11-23 | Aptinyx Inc. | Spiro-lactam nmda receptor modulators and uses thereof |
| AU2017267708B2 (en) | 2016-05-19 | 2020-02-20 | Aptinyx Inc. | Spiro-lactam NMDA receptor modulators and uses thereof |
| EA201990428A1 (ru) | 2016-08-01 | 2019-08-30 | Аптиникс Инк. | Спиролактамовые модуляторы nmda-рецептора и их применение |
| AU2017306152A1 (en) | 2016-08-01 | 2019-01-31 | Aptinyx Inc. | Spiro-lactam NMDA receptor modulators and uses thereof |
| JP7036792B2 (ja) | 2016-08-01 | 2022-03-15 | アプティニックス インコーポレイテッド | スピロ－ラクタムｎｍｄａ受容体修飾因子およびその使用 |
| AU2017306158B2 (en) | 2016-08-01 | 2021-10-14 | Aptinyx Inc. | Spiro-lactam and bis-spiro-lactam NMDA receptor modulators and uses thereof |
| US11370790B2 (en) | 2016-08-01 | 2022-06-28 | Aptinyx Inc. | Spiro-lactam NMDA modulators and methods of using same |
| SG11202007256PA (en) | 2018-01-31 | 2020-08-28 | Aptinyx Inc | Spiro-lactam nmda receptor modulators and uses thereof |
| US12012413B2 (en) | 2019-11-11 | 2024-06-18 | Tenacia Biotechnology (Hong Kong) Co., Limited | Methods of treating painful diabetic peripheral neuropathy |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5272160A (en) * | 1989-05-17 | 1993-12-21 | Pfizer Inc | 2-piperidino-1-alkanol derivatives as antiischemic agents |
| US5710168A (en) * | 1991-10-23 | 1998-01-20 | Pfizer Inc. | 2-piperidino-1-alkanol derivatives as neuroprotective agents |
| AU710984B2 (en) * | 1995-08-11 | 1999-10-07 | Pfizer Inc. | (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin -1-yl)-1-propanolmethanesulfonate trihydrate |
| TW450807B (en) * | 1995-09-15 | 2001-08-21 | Pfizer | Pharmaceutical compositions for treating tinnitus comprising neuroprotective agents |
-
2001
- 2001-05-12 UA UA2003065485A patent/UA73619C2/uk unknown
- 2001-12-05 AU AU2002218454A patent/AU2002218454B2/en not_active Ceased
- 2001-12-05 GE GE5171A patent/GEP20053568B/en unknown
- 2001-12-05 DZ DZ013484A patent/DZ3484A1/fr active
- 2001-12-05 PT PT01270205T patent/PT1347760E/pt unknown
- 2001-12-05 SK SK698-2003A patent/SK6982003A3/sk unknown
- 2001-12-05 AU AU1845402A patent/AU1845402A/xx active Pending
- 2001-12-05 HU HU0400645A patent/HUP0400645A2/hu unknown
- 2001-12-05 WO PCT/IB2001/002359 patent/WO2002047685A2/en not_active Application Discontinuation
- 2001-12-05 BR BR0116085-0A patent/BR0116085A/pt not_active IP Right Cessation
- 2001-12-05 CZ CZ20031543A patent/CZ20031543A3/cs unknown
- 2001-12-05 PL PL01362080A patent/PL362080A1/xx not_active Application Discontinuation
- 2001-12-05 KR KR10-2003-7007874A patent/KR100533407B1/ko not_active IP Right Cessation
- 2001-12-05 CA CA002431172A patent/CA2431172A1/en not_active Abandoned
- 2001-12-05 MX MXPA03005257A patent/MXPA03005257A/es active IP Right Grant
- 2001-12-05 EE EEP200300284A patent/EE200300284A/et unknown
- 2001-12-05 DE DE60111265T patent/DE60111265T2/de not_active Expired - Fee Related
- 2001-12-05 CN CNB018203922A patent/CN1273135C/zh not_active Expired - Fee Related
- 2001-12-05 YU YU41103A patent/YU41103A/sh unknown
- 2001-12-05 US US10/010,827 patent/US6635270B2/en not_active Expired - Fee Related
- 2001-12-05 ES ES01270205T patent/ES2239648T3/es not_active Expired - Lifetime
- 2001-12-05 EA EA200300514A patent/EA006489B1/ru not_active IP Right Cessation
- 2001-12-05 JP JP2002549256A patent/JP2004515529A/ja active Pending
- 2001-12-05 IL IL15581001A patent/IL155810A0/xx unknown
- 2001-12-05 OA OA1200300145A patent/OA12414A/en unknown
- 2001-12-05 NZ NZ525742A patent/NZ525742A/en unknown
- 2001-12-05 AT AT01270205T patent/ATE296629T1/de not_active IP Right Cessation
- 2001-12-05 EP EP01270205A patent/EP1347760B1/en not_active Expired - Lifetime
- 2001-12-10 DO DO2001000300A patent/DOP2001000300A/es unknown
- 2001-12-11 AR ARP010105748A patent/AR035607A1/es unknown
- 2001-12-11 PE PE2001001235A patent/PE20020710A1/es not_active Application Discontinuation
- 2001-12-12 TN TNTNSN01173A patent/TNSN01173A1/fr unknown
- 2001-12-12 UY UY27068A patent/UY27068A1/es not_active Application Discontinuation
- 2001-12-13 AP APAP/P/2001/002376A patent/AP1235A/en active
- 2001-12-13 PA PA20018534901A patent/PA8534901A1/es unknown
-
2003
- 2003-05-08 IS IS6811A patent/IS6811A/is unknown
- 2003-05-09 BG BG107788A patent/BG107788A/bg unknown
- 2003-05-20 ZA ZA200303892A patent/ZA200303892B/en unknown
- 2003-06-03 MA MA27191A patent/MA26970A1/fr unknown
- 2003-06-11 HR HR20030473A patent/HRP20030473A2/hr not_active Application Discontinuation
- 2003-06-12 NO NO20032678A patent/NO20032678L/no not_active Application Discontinuation
- 2003-06-13 EC EC2003004655A patent/ECSP034655A/es unknown
- 2003-08-19 US US10/643,441 patent/US20040039022A1/en not_active Abandoned
-
2004
- 2004-04-07 HK HK04102474A patent/HK1059575A1/xx not_active IP Right Cessation
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| UA73619C2 (en) | Stable pharmaceutical compositions of nmda receptor agonist (variants) and method of treatment | |
| AU2002218454A1 (en) | NMDA receptor agonist pharmaceutical compositions | |
| RU2362560C2 (ru) | Фармацевтическая препаративная форма | |
| US10251848B2 (en) | Process for producing a stable low concentration, injectable solution of noradrenaline | |
| KR20090040248A (ko) | 화합물의 비경구 전달을 위한 제형 및 이의 용도 | |
| TWI454286B (zh) | 安定氧化性不安定組合物之方法 | |
| AU2019215801B2 (en) | Parenteral formulations and uses thereof | |
| WO2013108180A1 (en) | Aqueous paracetamol composition for injection | |
| UA122285C2 (uk) | Фізіологічно збалансовані склади для ін'єкцій, які включають фоснетупітант | |
| AU2005296875B2 (en) | Complex containing mequitazine, a cyclodextrin and an interaction agent | |
| JP3668225B2 (ja) | Ｏｃｔ製剤 | |
| JP2002528230A (ja) | 安定化処理した薬物製剤を含むプラスチック容器 | |
| JP2008297277A (ja) | 注射剤の安定化法 |