RU2016148182A - (r)-пирлиндол и его фармацевтически приемлемые соли для применения в медицине - Google Patents
(r)-пирлиндол и его фармацевтически приемлемые соли для применения в медицине Download PDFInfo
- Publication number
- RU2016148182A RU2016148182A RU2016148182A RU2016148182A RU2016148182A RU 2016148182 A RU2016148182 A RU 2016148182A RU 2016148182 A RU2016148182 A RU 2016148182A RU 2016148182 A RU2016148182 A RU 2016148182A RU 2016148182 A RU2016148182 A RU 2016148182A
- Authority
- RU
- Russia
- Prior art keywords
- pharmaceutically acceptable
- enantiomer
- acceptable salt
- azofenone
- pirlindol
- Prior art date
Links
- IWVRVEIKCBFZNF-UHFFFAOYSA-N LSM-1636 Chemical compound C1CNC2CCCC3=C2N1C1=CC=C(C)C=C13 IWVRVEIKCBFZNF-UHFFFAOYSA-N 0.000 claims 12
- 229950002220 pirlindole Drugs 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- 208000002193 Pain Diseases 0.000 claims 4
- 238000002648 combination therapy Methods 0.000 claims 4
- -1 proglumethacin Chemical compound 0.000 claims 4
- 239000005557 antagonist Substances 0.000 claims 3
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims 2
- BLXXJMDCKKHMKV-UHFFFAOYSA-N Nabumetone Chemical compound C1=C(CCC(C)=O)C=CC2=CC(OC)=CC=C21 BLXXJMDCKKHMKV-UHFFFAOYSA-N 0.000 claims 2
- 230000000202 analgesic effect Effects 0.000 claims 2
- 239000000730 antalgic agent Substances 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims 2
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims 2
- 229960004270 nabumetone Drugs 0.000 claims 2
- OGNSCSPNOLGXSM-UHFFFAOYSA-N (+/-)-DABA Natural products NCCC(N)C(O)=O OGNSCSPNOLGXSM-UHFFFAOYSA-N 0.000 claims 1
- RJMIEHBSYVWVIN-LLVKDONJSA-N (2r)-2-[4-(3-oxo-1h-isoindol-2-yl)phenyl]propanoic acid Chemical compound C1=CC([C@H](C(O)=O)C)=CC=C1N1C(=O)C2=CC=CC=C2C1 RJMIEHBSYVWVIN-LLVKDONJSA-N 0.000 claims 1
- BMPDWHIDQYTSHX-AWEZNQCLSA-N (S)-MHD Chemical compound C1[C@H](O)C2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 BMPDWHIDQYTSHX-AWEZNQCLSA-N 0.000 claims 1
- IWYDHOAUDWTVEP-ZETCQYMHSA-M (S)-mandelate Chemical compound [O-]C(=O)[C@@H](O)C1=CC=CC=C1 IWYDHOAUDWTVEP-ZETCQYMHSA-M 0.000 claims 1
- XLVXAUNDHWERBM-IVGWJTKZSA-N 2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]-n-[(2r,3r,4s,5r)-3,4,5,6-tetrahydroxy-1-oxohexan-2-yl]acetamide Chemical compound CC1=C(CC(=O)N[C@@H](C=O)[C@@H](O)[C@H](O)[C@H](O)CO)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 XLVXAUNDHWERBM-IVGWJTKZSA-N 0.000 claims 1
- JIEKMACRVQTPRC-UHFFFAOYSA-N 2-[4-(4-chlorophenyl)-2-phenyl-5-thiazolyl]acetic acid Chemical compound OC(=O)CC=1SC(C=2C=CC=CC=2)=NC=1C1=CC=C(Cl)C=C1 JIEKMACRVQTPRC-UHFFFAOYSA-N 0.000 claims 1
- MSWZFWKMSRAUBD-IVMDWMLBSA-N 2-amino-2-deoxy-D-glucopyranose Chemical compound N[C@H]1C(O)O[C@H](CO)[C@@H](O)[C@@H]1O MSWZFWKMSRAUBD-IVMDWMLBSA-N 0.000 claims 1
- TYNLGDBUJLVSMA-UHFFFAOYSA-N 4,5-diacetyloxy-9,10-dioxo-2-anthracenecarboxylic acid Chemical compound O=C1C2=CC(C(O)=O)=CC(OC(C)=O)=C2C(=O)C2=C1C=CC=C2OC(=O)C TYNLGDBUJLVSMA-UHFFFAOYSA-N 0.000 claims 1
- PJJGZPJJTHBVMX-UHFFFAOYSA-N 5,7-Dihydroxyisoflavone Chemical compound C=1C(O)=CC(O)=C(C2=O)C=1OC=C2C1=CC=CC=C1 PJJGZPJJTHBVMX-UHFFFAOYSA-N 0.000 claims 1
- BSYNRYMUTXBXSQ-FOQJRBATSA-N 59096-14-9 Chemical compound CC(=O)OC1=CC=CC=C1[14C](O)=O BSYNRYMUTXBXSQ-FOQJRBATSA-N 0.000 claims 1
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 claims 1
- 206010001497 Agitation Diseases 0.000 claims 1
- MNIPYSSQXLZQLJ-UHFFFAOYSA-N Biofenac Chemical compound OC(=O)COC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl MNIPYSSQXLZQLJ-UHFFFAOYSA-N 0.000 claims 1
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 1
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims 1
- 102000006541 Ionotropic Glutamate Receptors Human genes 0.000 claims 1
- 108010008812 Ionotropic Glutamate Receptors Proteins 0.000 claims 1
- SBDNJUWAMKYJOX-UHFFFAOYSA-N Meclofenamic Acid Chemical compound CC1=CC=C(Cl)C(NC=2C(=CC=CC=2)C(O)=O)=C1Cl SBDNJUWAMKYJOX-UHFFFAOYSA-N 0.000 claims 1
- ZRVUJXDFFKFLMG-UHFFFAOYSA-N Meloxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=NC=C(C)S1 ZRVUJXDFFKFLMG-UHFFFAOYSA-N 0.000 claims 1
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 claims 1
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 1
- CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 claims 1
- CXOFVDLJLONNDW-UHFFFAOYSA-N Phenytoin Chemical compound N1C(=O)NC(=O)C1(C=1C=CC=CC=1)C1=CC=CC=C1 CXOFVDLJLONNDW-UHFFFAOYSA-N 0.000 claims 1
- 101100244562 Pseudomonas aeruginosa (strain ATCC 15692 / DSM 22644 / CIP 104116 / JCM 14847 / LMG 12228 / 1C / PRS 101 / PAO1) oprD gene Proteins 0.000 claims 1
- 108010052164 Sodium Channels Proteins 0.000 claims 1
- 102000018674 Sodium Channels Human genes 0.000 claims 1
- 229960004420 aceclofenac Drugs 0.000 claims 1
- 229960004892 acemetacin Drugs 0.000 claims 1
- FSQKKOOTNAMONP-UHFFFAOYSA-N acemetacin Chemical compound CC1=C(CC(=O)OCC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 FSQKKOOTNAMONP-UHFFFAOYSA-N 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- MSWZFWKMSRAUBD-UHFFFAOYSA-N beta-D-galactosamine Natural products NC1C(O)OC(CO)C(O)C1O MSWZFWKMSRAUBD-UHFFFAOYSA-N 0.000 claims 1
- 229960000623 carbamazepine Drugs 0.000 claims 1
- FFGPTBGBLSHEPO-UHFFFAOYSA-N carbamazepine Chemical compound C1=CC2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 FFGPTBGBLSHEPO-UHFFFAOYSA-N 0.000 claims 1
- 229960000590 celecoxib Drugs 0.000 claims 1
- RZEKVGVHFLEQIL-UHFFFAOYSA-N celecoxib Chemical compound C1=CC(C)=CC=C1C1=CC(C(F)(F)F)=NN1C1=CC=C(S(N)(=O)=O)C=C1 RZEKVGVHFLEQIL-UHFFFAOYSA-N 0.000 claims 1
- 229960001209 clonixin Drugs 0.000 claims 1
- CLOMYZFHNHFSIQ-UHFFFAOYSA-N clonixin Chemical compound CC1=C(Cl)C=CC=C1NC1=NC=CC=C1C(O)=O CLOMYZFHNHFSIQ-UHFFFAOYSA-N 0.000 claims 1
- 229940000425 combination drug Drugs 0.000 claims 1
- 108700023159 delta Opioid Receptors Proteins 0.000 claims 1
- 102000048124 delta Opioid Receptors Human genes 0.000 claims 1
- 229960003428 dexibuprofen Drugs 0.000 claims 1
- HEFNNWSXXWATRW-JTQLQIEISA-N dexibuprofen Chemical compound CC(C)CC1=CC=C([C@H](C)C(O)=O)C=C1 HEFNNWSXXWATRW-JTQLQIEISA-N 0.000 claims 1
- 229960002783 dexketoprofen Drugs 0.000 claims 1
- DKYWVDODHFEZIM-NSHDSACASA-N dexketoprofen Chemical compound OC(=O)[C@@H](C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-NSHDSACASA-N 0.000 claims 1
- NIJJYAXOARWZEE-UHFFFAOYSA-N di-n-propyl-acetic acid Natural products CCCC(C(O)=O)CCC NIJJYAXOARWZEE-UHFFFAOYSA-N 0.000 claims 1
- 229960004590 diacerein Drugs 0.000 claims 1
- 229960001259 diclofenac Drugs 0.000 claims 1
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000003623 enhancer Substances 0.000 claims 1
- 229960004028 eslicarbazepine Drugs 0.000 claims 1
- 229960005293 etodolac Drugs 0.000 claims 1
- XFBVBWWRPKNWHW-UHFFFAOYSA-N etodolac Chemical compound C1COC(CC)(CC(O)=O)C2=N[C]3C(CC)=CC=CC3=C21 XFBVBWWRPKNWHW-UHFFFAOYSA-N 0.000 claims 1
- 229960004945 etoricoxib Drugs 0.000 claims 1
- MNJVRJDLRVPLFE-UHFFFAOYSA-N etoricoxib Chemical compound C1=NC(C)=CC=C1C1=NC=C(Cl)C=C1C1=CC=C(S(C)(=O)=O)C=C1 MNJVRJDLRVPLFE-UHFFFAOYSA-N 0.000 claims 1
- 229960001395 fenbufen Drugs 0.000 claims 1
- ZPAKPRAICRBAOD-UHFFFAOYSA-N fenbufen Chemical compound C1=CC(C(=O)CCC(=O)O)=CC=C1C1=CC=CC=C1 ZPAKPRAICRBAOD-UHFFFAOYSA-N 0.000 claims 1
- 229960002679 fentiazac Drugs 0.000 claims 1
- LPEPZBJOKDYZAD-UHFFFAOYSA-N flufenamic acid Chemical compound OC(=O)C1=CC=CC=C1NC1=CC=CC(C(F)(F)F)=C1 LPEPZBJOKDYZAD-UHFFFAOYSA-N 0.000 claims 1
- 229960004369 flufenamic acid Drugs 0.000 claims 1
- 229960002390 flurbiprofen Drugs 0.000 claims 1
- SYTBZMRGLBWNTM-UHFFFAOYSA-N flurbiprofen Chemical compound FC1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC=C1 SYTBZMRGLBWNTM-UHFFFAOYSA-N 0.000 claims 1
- 229960002870 gabapentin Drugs 0.000 claims 1
- 229960003692 gamma aminobutyric acid Drugs 0.000 claims 1
- 229960004410 glucametacin Drugs 0.000 claims 1
- 229960002442 glucosamine Drugs 0.000 claims 1
- 229960001680 ibuprofen Drugs 0.000 claims 1
- 229960000905 indomethacin Drugs 0.000 claims 1
- 229960004187 indoprofen Drugs 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000001057 ionotropic effect Effects 0.000 claims 1
- 102000048260 kappa Opioid Receptors Human genes 0.000 claims 1
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 claims 1
- 229960000991 ketoprofen Drugs 0.000 claims 1
- 229960004752 ketorolac Drugs 0.000 claims 1
- OZWKMVRBQXNZKK-UHFFFAOYSA-N ketorolac Chemical compound OC(=O)C1CCN2C1=CC=C2C(=O)C1=CC=CC=C1 OZWKMVRBQXNZKK-UHFFFAOYSA-N 0.000 claims 1
- 229960003803 meclofenamic acid Drugs 0.000 claims 1
- 229960003464 mefenamic acid Drugs 0.000 claims 1
- 229960001929 meloxicam Drugs 0.000 claims 1
- 102000051367 mu Opioid Receptors Human genes 0.000 claims 1
- 229960002009 naproxen Drugs 0.000 claims 1
- CMWTZPSULFXXJA-VIFPVBQESA-N naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims 1
- 230000001537 neural effect Effects 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 229960000965 nimesulide Drugs 0.000 claims 1
- HYWYRSMBCFDLJT-UHFFFAOYSA-N nimesulide Chemical compound CS(=O)(=O)NC1=CC=C([N+]([O-])=O)C=C1OC1=CC=CC=C1 HYWYRSMBCFDLJT-UHFFFAOYSA-N 0.000 claims 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 1
- 229960000273 oxametacin Drugs 0.000 claims 1
- AJRNYCDWNITGHF-UHFFFAOYSA-N oxametacin Chemical compound CC1=C(CC(=O)NO)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 AJRNYCDWNITGHF-UHFFFAOYSA-N 0.000 claims 1
- 229960002739 oxaprozin Drugs 0.000 claims 1
- OFPXSFXSNFPTHF-UHFFFAOYSA-N oxaprozin Chemical compound O1C(CCC(=O)O)=NC(C=2C=CC=CC=2)=C1C1=CC=CC=C1 OFPXSFXSNFPTHF-UHFFFAOYSA-N 0.000 claims 1
- 229960001816 oxcarbazepine Drugs 0.000 claims 1
- CTRLABGOLIVAIY-UHFFFAOYSA-N oxcarbazepine Chemical compound C1C(=O)C2=CC=CC=C2N(C(=O)N)C2=CC=CC=C21 CTRLABGOLIVAIY-UHFFFAOYSA-N 0.000 claims 1
- 229960005489 paracetamol Drugs 0.000 claims 1
- 229960004662 parecoxib Drugs 0.000 claims 1
- TZRHLKRLEZJVIJ-UHFFFAOYSA-N parecoxib Chemical compound C1=CC(S(=O)(=O)NC(=O)CC)=CC=C1C1=C(C)ON=C1C1=CC=CC=C1 TZRHLKRLEZJVIJ-UHFFFAOYSA-N 0.000 claims 1
- 239000004031 partial agonist Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229960002036 phenytoin Drugs 0.000 claims 1
- 229960002702 piroxicam Drugs 0.000 claims 1
- QYSPLQLAKJAUJT-UHFFFAOYSA-N piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 229960000371 rofecoxib Drugs 0.000 claims 1
- RZJQGNCSTQAWON-UHFFFAOYSA-N rofecoxib Chemical compound C1=CC(S(=O)(=O)C)=CC=C1C1=C(C=2C=CC=CC=2)C(=O)OC1 RZJQGNCSTQAWON-UHFFFAOYSA-N 0.000 claims 1
- 229960000894 sulindac Drugs 0.000 claims 1
- MLKXDPUZXIRXEP-MFOYZWKCSA-N sulindac Chemical compound CC1=C(CC(O)=O)C2=CC(F)=CC=C2\C1=C/C1=CC=C(S(C)=O)C=C1 MLKXDPUZXIRXEP-MFOYZWKCSA-N 0.000 claims 1
- 229960002871 tenoxicam Drugs 0.000 claims 1
- WZWYJBNHTWCXIM-UHFFFAOYSA-N tenoxicam Chemical compound O=C1C=2SC=CC=2S(=O)(=O)N(C)C1=C(O)NC1=CC=CC=N1 WZWYJBNHTWCXIM-UHFFFAOYSA-N 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- YEZNLOUZAIOMLT-UHFFFAOYSA-N tolfenamic acid Chemical compound CC1=C(Cl)C=CC=C1NC1=CC=CC=C1C(O)=O YEZNLOUZAIOMLT-UHFFFAOYSA-N 0.000 claims 1
- 229960002905 tolfenamic acid Drugs 0.000 claims 1
- 229960002004 valdecoxib Drugs 0.000 claims 1
- LNPDTQAFDNKSHK-UHFFFAOYSA-N valdecoxib Chemical compound CC=1ON=C(C=2C=CC=CC=2)C=1C1=CC=C(S(N)(=O)=O)C=C1 LNPDTQAFDNKSHK-UHFFFAOYSA-N 0.000 claims 1
- MSRILKIQRXUYCT-UHFFFAOYSA-M valproate semisodium Chemical compound [Na+].CCCC(C(O)=O)CCC.CCCC(C([O-])=O)CCC MSRILKIQRXUYCT-UHFFFAOYSA-M 0.000 claims 1
- 229960000604 valproic acid Drugs 0.000 claims 1
- 229960003414 zomepirac Drugs 0.000 claims 1
- ZXVNMYWKKDOREA-UHFFFAOYSA-N zomepirac Chemical compound C1=C(CC(O)=O)N(C)C(C(=O)C=2C=CC(Cl)=CC=2)=C1C ZXVNMYWKKDOREA-UHFFFAOYSA-N 0.000 claims 1
- 108020001588 κ-opioid receptors Proteins 0.000 claims 1
- 108020001612 μ-opioid receptors Proteins 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
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Claims (12)
1. (R)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения для терапевтического лечения или предупреждения боли.
2. (R)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по п. 1, отличающийся тем, что (R)-пирлиндол является энантиомерно чистым.
3. (R)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по пп. 1 и 2 в комбинированной терапии вместе по меньшей мере с одним дополнительным анальгетическим средством.
4. (R)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по п. 3, в котором комбинированная терапия включает комбинированную терапию с фиксированными дозами или раздельную комбинированную терапию, выбранную из группы, включающей одновременное или последовательное введение активных средств.
5. (R)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по пп. 3 и 4 для усиления воздействия по меньшей мере одного дополнительного анальгетического средства для лечения боли.
6. (R)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по любому из пп. 1-5 в форме (S)-манделата (R)-пирлиндола.
7. (R)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по любому из пп. 1-5 в форме мезилата (R)-пирлиндола.
8. (R)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по любому из пп. 1-5 в форме цитрата (R)-пирлиндола.
9. (R)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по пп. 3-8, отличающийся тем, что по меньшей мере одним дополнительным анальгетическим средством является соединение, которое уменьшает гипервозбудимость нейронов, выбранное из группы, включающей: ингибиторы натриевых каналов (карбамазепин, окскарбазепин, эсликарбазепин, фенитоин, вальпроевая кислота), антагонисты кальциевых каналов (прегабалин), антагонисты ионотропного и метаботропного глутаматного рецептора, усилители активности γ-аминомасляной кислоты (габапентин) или агонисты μ, κ и δ опиоидного рецептора, частичные агонисты/антагонисты или антагонисты.
10. (R)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по пп. 3-8, отличающийся тем, что по меньшей мере одним дополнительным анальгетическим средством является соединение, выбранное из группы, включающей: парацетамол, нестероидные противовоспалительные лекарственные средства ацетилсалициловая кислота, диклофенак, набуметон, нимесулид, набуметон, этодолак, пироксикам, клониксинат лизина, дифлунизал, ацеметацин, глюкаметацин, индометацин, проглуметацин, оксаметацин, сулиндак, ацеклофенак, фентиазак, кеторолак, зомепирак, мелоксикам, теноксикам, лорноксикан, фенопрофен, фенбуфен, флурбипрофен, беноксапрофен, ибупрофен, кетопрофен, декскетопрофен, пирпрофен, индопрофен, напроксен, оксапрозин, тиапрофен, дексибупрофен, меклофенаминовая кислота, мефенаминовая кислота, флуфенамовая кислота, толфенамовая кислота, нифлумовая кислота, этофенамат, азапропазон, орготеин, фепразон, морнифлумат, тенидап, глюкозаминогликан, полисульфат, целекоксиб, рофекоксиб, парекоксиб, валдекоксиб и эторикоксиб, глюкозамин или диацереин.
11. (R)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по любому предыдущему пункту, в котором болью является невропатическая боль.
12. Фармацевтическая композиция для лечения боли, включающая (R)-энантиомер пирлиндола или его фармацевтически приемлемую соль по любому из предыдущих пунктов вместе с фармацевтически приемлемыми носителями, разбавителями или инертными наполнителями.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/PT2014/000028 WO2015171004A1 (en) | 2014-05-09 | 2014-05-09 | (r)-pirlindole and its pharmaceutically acceptable salts for use in medicine |
Publications (3)
| Publication Number | Publication Date |
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| RU2016148182A true RU2016148182A (ru) | 2018-06-13 |
| RU2016148182A3 RU2016148182A3 (ru) | 2018-06-13 |
| RU2695607C2 RU2695607C2 (ru) | 2019-07-24 |
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| JP (1) | JP2017514884A (ru) |
| KR (1) | KR102232198B1 (ru) |
| CN (1) | CN106413714A (ru) |
| AU (1) | AU2014393489B2 (ru) |
| CA (1) | CA2948596C (ru) |
| CY (1) | CY1119522T1 (ru) |
| DK (1) | DK3054950T3 (ru) |
| EC (1) | ECSP16086232A (ru) |
| ES (1) | ES2649491T3 (ru) |
| HR (1) | HRP20171650T1 (ru) |
| HU (1) | HUE035030T2 (ru) |
| IL (1) | IL248854B (ru) |
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| MX (1) | MX368735B (ru) |
| NO (1) | NO3054950T3 (ru) |
| NZ (1) | NZ726131A (ru) |
| PH (1) | PH12016502236A1 (ru) |
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| RS (1) | RS56590B1 (ru) |
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| TN (1) | TN2016000497A1 (ru) |
| UA (1) | UA116499C2 (ru) |
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| HUE035030T2 (en) | 2014-05-09 | 2018-05-02 | Tecnimede Sociedade Tecnico Medicinal S | (R) -pirlindole and its pharmaceutically acceptable salts for use in medicine |
| EP3831385B1 (en) * | 2014-05-09 | 2024-07-10 | Tecnimede Sociedade Tecnico-Medicinal S.A. | Mandelate salts of pirlindole enantiomers for use in medicine |
| KR102421013B1 (ko) | 2016-05-19 | 2022-07-14 | 에스케이바이오팜 주식회사 | 삼차신경통을 예방 또는 치료하기 위한 카바메이트 화합물의 용도 |
| US12201441B2 (en) * | 2018-06-13 | 2025-01-21 | Children's Medical Center Corporation | Biomarkers of neuropathic pain |
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| EP1558231A4 (en) * | 2002-10-03 | 2010-09-08 | Cypress Bioscience Inc | DOSAGE CLIMBING AND FRICTIONAL DAILY DOSE OF ANTIDEPRESSANTS TO TREAT NEUROLOGICAL DISORDERS |
| MXPA05006940A (es) * | 2002-12-24 | 2006-02-22 | Neurochem Int Ltd | Formulaciones terapeuticas para el tratamiento de enfermedades relacionadas con beta - amiloide. |
| US20070043030A1 (en) * | 2003-09-15 | 2007-02-22 | Vectura Limited | Pharmaceutical compositions for treating premature ejaculation by pulmonary inhalation |
| EP1688161A1 (en) * | 2004-11-02 | 2006-08-09 | Switch Biotech Aktiengesellschaft | Use of pirlindole for the treatment of diseases which are characterized by proliferation of t-lymphocytes and/or hyperproliferation of keratinocytes in particular atopic dermatitis and psoriasis |
| HUE035030T2 (en) | 2014-05-09 | 2018-05-02 | Tecnimede Sociedade Tecnico Medicinal S | (R) -pirlindole and its pharmaceutically acceptable salts for use in medicine |
| EP3831385B1 (en) * | 2014-05-09 | 2024-07-10 | Tecnimede Sociedade Tecnico-Medicinal S.A. | Mandelate salts of pirlindole enantiomers for use in medicine |
| CN106456637B (zh) * | 2014-05-09 | 2020-06-09 | 特克尼梅德医疗技术股份公司 | (s)-吡吲哚及其药学上可接受的盐的药学用途 |
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2014
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- 2014-05-09 MA MA39448A patent/MA39448B1/fr unknown
- 2014-05-09 JP JP2016567556A patent/JP2017514884A/ja active Pending
- 2014-05-09 UA UAA201611333A patent/UA116499C2/uk unknown
- 2014-05-09 CA CA2948596A patent/CA2948596C/en active Active
- 2014-05-09 AU AU2014393489A patent/AU2014393489B2/en active Active
- 2014-05-09 RU RU2016148182A patent/RU2695607C2/ru active
- 2014-05-09 US US15/309,916 patent/US20170145015A1/en not_active Abandoned
- 2014-05-09 PT PT147264436T patent/PT3054950T/pt unknown
- 2014-05-09 TN TN2016000497A patent/TN2016000497A1/en unknown
- 2014-05-09 LT LTEP14726443.6T patent/LT3054950T/lt unknown
- 2014-05-09 NO NO14726443A patent/NO3054950T3/no unknown
- 2014-05-09 ES ES14726443.6T patent/ES2649491T3/es active Active
- 2014-05-09 CN CN201480078733.5A patent/CN106413714A/zh active Pending
- 2014-05-09 MX MX2016014701A patent/MX368735B/es active IP Right Grant
- 2014-05-09 WO PCT/PT2014/000028 patent/WO2015171004A1/en not_active Ceased
- 2014-05-09 DK DK14726443.6T patent/DK3054950T3/da active
- 2014-05-09 EP EP14726443.6A patent/EP3054950B1/en active Active
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- 2014-05-09 SI SI201430470T patent/SI3054950T1/sl unknown
- 2014-05-09 KR KR1020167031372A patent/KR102232198B1/ko active Active
- 2014-05-09 SM SM20170520T patent/SMT201700520T1/it unknown
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2016
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