RU2016148183A - (s)-пирлиндол и его фармацевтические приемлемые соли для применения в медицине - Google Patents
(s)-пирлиндол и его фармацевтические приемлемые соли для применения в медицине Download PDFInfo
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- RU2016148183A RU2016148183A RU2016148183A RU2016148183A RU2016148183A RU 2016148183 A RU2016148183 A RU 2016148183A RU 2016148183 A RU2016148183 A RU 2016148183A RU 2016148183 A RU2016148183 A RU 2016148183A RU 2016148183 A RU2016148183 A RU 2016148183A
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- RU
- Russia
- Prior art keywords
- pharmaceutically acceptable
- enantiomer
- acceptable salt
- pirlindol
- use according
- Prior art date
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- 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
- 239000005557 antagonist Substances 0.000 claims 3
- -1 clonixfinalis Chemical compound 0.000 claims 3
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- 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
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- 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
- XILVEPYQJIOVNB-UHFFFAOYSA-N 2-[3-(trifluoromethyl)anilino]benzoic acid 2-(2-hydroxyethoxy)ethyl ester Chemical compound OCCOCCOC(=O)C1=CC=CC=C1NC1=CC=CC(C(F)(F)F)=C1 XILVEPYQJIOVNB-UHFFFAOYSA-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
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- 229960003692 gamma aminobutyric acid Drugs 0.000 claims 1
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- 230000001057 ionotropic effect Effects 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
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- 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
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- 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
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- PTXGHCGBYMQQIG-UHFFFAOYSA-N proglumetacin Chemical compound C=1C=CC=CC=1C(=O)NC(C(=O)N(CCC)CCC)CCC(=O)OCCCN(CC1)CCN1CCOC(=O)CC(C1=CC(OC)=CC=C11)=C(C)N1C(=O)C1=CC=C(Cl)C=C1 PTXGHCGBYMQQIG-UHFFFAOYSA-N 0.000 claims 1
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- 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
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- TUGDLVFMIQZYPA-UHFFFAOYSA-N tetracopper;tetrazinc Chemical compound [Cu+2].[Cu+2].[Cu+2].[Cu+2].[Zn+2].[Zn+2].[Zn+2].[Zn+2] TUGDLVFMIQZYPA-UHFFFAOYSA-N 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
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Classifications
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- 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
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- 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
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Claims (12)
1. (S)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения для терапевтического лечения или предупреждения боли.
2. (S)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по п. 1, отличающийся тем, что (S)-пирлиндол является энантиомерно чистым.
3. (S)-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. (S)-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. (S)-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. (S)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по любому из пп. 1-5 в форме (R)-манделата (S)-пирлиндола.
7. (S)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по любому из пп. 1-5 в форме мезилата (S)-пирлиндола.
8. (S)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по любому из пп. 1-5 в форме цитрата (S)-пирлиндола.
9. (S)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по пп. 3-8, отличающегося 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. (S)-Энантиомер пирлиндола или его фармацевтически приемлемая соль для применения по пп. 3-8, отличающегося 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. (S)-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 (S)-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/PT2014/000029 WO2015171005A1 (en) | 2014-05-09 | 2014-05-09 | (s)-pirlindole or its pharmaceutically acceptable salts for use in medicine |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2016148183A3 RU2016148183A3 (ru) | 2018-06-13 |
| RU2016148183A true RU2016148183A (ru) | 2018-06-13 |
| RU2695647C2 RU2695647C2 (ru) | 2019-07-25 |
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Country Status (30)
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| JP (1) | JP6768520B2 (ru) |
| KR (1) | KR102298676B1 (ru) |
| CN (1) | CN106456637B (ru) |
| AU (1) | AU2014393490B2 (ru) |
| CA (1) | CA2948598C (ru) |
| CY (1) | CY1119532T1 (ru) |
| DK (1) | DK3057589T3 (ru) |
| EC (1) | ECSP16086247A (ru) |
| ES (1) | ES2649492T3 (ru) |
| HR (1) | HRP20171651T1 (ru) |
| HU (1) | HUE035071T2 (ru) |
| IL (1) | IL248855B (ru) |
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| MA (1) | MA39447B1 (ru) |
| MX (1) | MX368734B (ru) |
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| NZ (1) | NZ726132A (ru) |
| PH (1) | PH12016502233A1 (ru) |
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| PT (1) | PT3057589T (ru) |
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| RU (1) | RU2695647C2 (ru) |
| SA (1) | SA516380264B1 (ru) |
| SI (1) | SI3057589T1 (ru) |
| SM (1) | SMT201700519T1 (ru) |
| TN (1) | TN2016000498A1 (ru) |
| UA (1) | UA118474C2 (ru) |
| WO (1) | WO2015171005A1 (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 |
| EP3392251A1 (en) | 2017-04-21 | 2018-10-24 | Tecnimede-Sociedade Tecnico-Medicinal, S.A. | Process for the preparation of pirlindole enantiomers and its salts |
| EP3392250A1 (en) | 2017-04-21 | 2018-10-24 | Tecnimede-Sociedade Tecnico-Medicinal, S.A. | Process for the preparation of piperazine ring for the synthesis of pyrazinocarbazole derivatives |
| MX2018011142A (es) | 2018-09-13 | 2019-10-10 | Federico Amezcua Amezcua | Combinacion farmaceutica sinergica de un inhibidor selectivo de la ciclooxigenasa 2 y un derivado de antraquinona. |
| EP3900716A1 (en) * | 2020-04-21 | 2021-10-27 | Dompe' Farmaceutici S.P.A. | Co-crystal of gabapentin, ketoprofen and lysine, pharmaceutical compositions and their medical use |
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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 |
| EP3831385B1 (en) * | 2014-05-09 | 2024-07-10 | Tecnimede Sociedade Tecnico-Medicinal S.A. | Mandelate salts of pirlindole enantiomers for use in medicine |
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2014
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- 2014-05-09 JP JP2016567545A patent/JP6768520B2/ja active Active
- 2014-05-09 HU HUE14726444A patent/HUE035071T2/en unknown
- 2014-05-09 RS RS20171094A patent/RS56591B1/sr unknown
- 2014-05-09 SM SM20170519T patent/SMT201700519T1/it unknown
- 2014-05-09 TN TN2016000498A patent/TN2016000498A1/en unknown
- 2014-05-09 SI SI201430462T patent/SI3057589T1/sl unknown
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2017
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