BR112021004661A2 - composto, composição farmacêutica, método para tratamento de dor neuropática e/ou prurido, e, uso do composto - Google Patents
composto, composição farmacêutica, método para tratamento de dor neuropática e/ou prurido, e, uso do composto Download PDFInfo
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- BR112021004661A2 BR112021004661A2 BR112021004661-5A BR112021004661A BR112021004661A2 BR 112021004661 A2 BR112021004661 A2 BR 112021004661A2 BR 112021004661 A BR112021004661 A BR 112021004661A BR 112021004661 A2 BR112021004661 A2 BR 112021004661A2
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- Prior art keywords
- compound
- pruritus
- neuropathic pain
- treatment
- rats
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- XNGIFLGASWRNHJ-UHFFFAOYSA-L phthalate(2-) Chemical compound [O-]C(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-L 0.000 description 1
- 238000000053 physical method Methods 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 229920002401 polyacrylamide Polymers 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- 238000002600 positron emission tomography Methods 0.000 description 1
- 238000010149 post-hoc-test Methods 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- GNSKLFRGEWLPPA-UHFFFAOYSA-M potassium dihydrogen phosphate Chemical compound [K+].OP(O)([O-])=O GNSKLFRGEWLPPA-UHFFFAOYSA-M 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 230000000069 prophylactic effect Effects 0.000 description 1
- 150000003180 prostaglandins Chemical class 0.000 description 1
- 238000000159 protein binding assay Methods 0.000 description 1
- 208000020016 psychiatric disease Diseases 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 229940075993 receptor modulator Drugs 0.000 description 1
- 230000011514 reflex Effects 0.000 description 1
- 230000000284 resting effect Effects 0.000 description 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 1
- 229960001860 salicylate Drugs 0.000 description 1
- 208000005687 scabies Diseases 0.000 description 1
- 210000003497 sciatic nerve Anatomy 0.000 description 1
- 238000007790 scraping Methods 0.000 description 1
- 238000007789 sealing Methods 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 238000013207 serial dilution Methods 0.000 description 1
- 229940076279 serotonin Drugs 0.000 description 1
- 238000002603 single-photon emission computed tomography Methods 0.000 description 1
- 239000000344 soap Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 235000017550 sodium carbonate Nutrition 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 235000010344 sodium nitrate Nutrition 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- 230000000392 somatic effect Effects 0.000 description 1
- 229940075554 sorbate Drugs 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000004611 spectroscopical analysis Methods 0.000 description 1
- 230000002269 spontaneous effect Effects 0.000 description 1
- 230000010473 stable expression Effects 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 229940114926 stearate Drugs 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000011550 stock solution Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 229940086735 succinate 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
- 239000000375 suspending agent Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- BWMISRWJRUSYEX-SZKNIZGXSA-N terbinafine hydrochloride Chemical compound Cl.C1=CC=C2C(CN(C\C=C\C#CC(C)(C)C)C)=CC=CC2=C1 BWMISRWJRUSYEX-SZKNIZGXSA-N 0.000 description 1
- 229960003604 testosterone Drugs 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 231100001274 therapeutic index Toxicity 0.000 description 1
- 210000001685 thyroid gland Anatomy 0.000 description 1
- 201000004647 tinea pedis Diseases 0.000 description 1
- 230000009092 tissue dysfunction Effects 0.000 description 1
- 238000004448 titration Methods 0.000 description 1
- 229960005371 tolbutamide Drugs 0.000 description 1
- 238000003325 tomography Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- WBYWAXJHAXSJNI-VOTSOKGWSA-M trans-cinnamate Chemical compound [O-]C(=O)\C=C\C1=CC=CC=C1 WBYWAXJHAXSJNI-VOTSOKGWSA-M 0.000 description 1
- 229910052722 tritium Inorganic materials 0.000 description 1
- 210000000689 upper leg Anatomy 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
- 210000004885 white matter Anatomy 0.000 description 1
- 239000002023 wood Substances 0.000 description 1
- 210000002268 wool Anatomy 0.000 description 1
- 229910052725 zinc Inorganic materials 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Dermatology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18194297.0 | 2018-09-13 | ||
| EP18194297 | 2018-09-13 | ||
| PCT/EP2019/074465 WO2020053377A1 (en) | 2018-09-13 | 2019-09-13 | A gabaa receptor ligand |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112021004661A2 true BR112021004661A2 (pt) | 2021-06-01 |
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| US (1) | US11396510B2 (https=) |
| EP (1) | EP3849976B1 (https=) |
| JP (1) | JP7353663B2 (https=) |
| KR (1) | KR102712565B1 (https=) |
| CN (1) | CN112714765B (https=) |
| AU (1) | AU2019338236B2 (https=) |
| BR (1) | BR112021004661A2 (https=) |
| CA (1) | CA3110283A1 (https=) |
| DK (1) | DK3849976T3 (https=) |
| EA (1) | EA202190717A1 (https=) |
| ES (1) | ES2935705T3 (https=) |
| FI (1) | FI3849976T3 (https=) |
| HR (1) | HRP20230067T1 (https=) |
| HU (1) | HUE060943T2 (https=) |
| IL (1) | IL281335B2 (https=) |
| LT (1) | LT3849976T (https=) |
| MX (1) | MX2021003010A (https=) |
| PH (1) | PH12021550299A1 (https=) |
| PL (1) | PL3849976T3 (https=) |
| PT (1) | PT3849976T (https=) |
| SG (1) | SG11202101360VA (https=) |
| SI (1) | SI3849976T1 (https=) |
| WO (1) | WO2020053377A1 (https=) |
| ZA (1) | ZA202100976B (https=) |
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| EP4322955A1 (en) | 2021-04-16 | 2024-02-21 | Saniona A/S | A gaba receptor modulator for use in the treatment of pain |
| WO2025056751A1 (en) * | 2023-09-15 | 2025-03-20 | Saniona A/S | A gaba receptor modulator for use in the treatment of absence seizures |
| CN121793969A (zh) * | 2023-09-15 | 2026-04-03 | 萨尼奥纳有限责任公司 | 一种用于治疗与睡眠纺锤波缺陷相关的疾病的gaba受体调节剂 |
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| AU675484B2 (en) | 1993-03-24 | 1997-02-06 | Neurosearch A/S | Benzimidazole compounds, their use and preparation |
| GB9702524D0 (en) | 1997-02-07 | 1997-03-26 | Merck Sharp & Dohme | Therapeutic agents |
| GB9813576D0 (en) | 1998-06-24 | 1998-08-19 | Merck Sharp & Dohme | Therapeutic agents |
| JP2002535407A (ja) | 1999-01-27 | 2002-10-22 | メルク シャープ エンド ドーム リミテッド | Ｇａｂａ受容体のリガンドとしてのトリアゾロピリダジン誘導体 |
| GB9921150D0 (en) | 1999-09-07 | 1999-11-10 | Merck Sharp & Dohme | Therapeutic agents |
| GB0208394D0 (en) | 2002-04-11 | 2002-05-22 | Merck Sharp & Dohme | Therapeutic agents |
| GB0208392D0 (en) | 2002-04-11 | 2002-05-22 | Merck Sharp & Dohme | Therapeutic compounds |
| GB0212048D0 (en) | 2002-05-24 | 2002-07-03 | Merck Sharp & Dohme | Therapeutic agents |
| WO2004087690A2 (en) | 2003-04-03 | 2004-10-14 | Neurosearch A/S | Benzimidazole derivatives and their use for modulating the gaba-a receptor complex |
| TWI391381B (zh) | 2006-03-24 | 2013-04-01 | Neurosearch As | 新穎的苯并咪唑衍生物、含有其之醫藥組成物、及其於製造藥物之用途 |
| TW201029986A (en) | 2008-11-14 | 2010-08-16 | Neurosearch As | Novel compounds |
| SG11201806393QA (en) | 2016-01-27 | 2018-08-30 | Univ Zuerich | Use of gabaa receptor modulators for treatment of itch |
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2019
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- 2019-09-13 JP JP2021514324A patent/JP7353663B2/ja active Active
- 2019-09-13 PT PT197657471T patent/PT3849976T/pt unknown
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- 2019-09-13 CA CA3110283A patent/CA3110283A1/en active Pending
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- 2019-09-13 CN CN201980059446.2A patent/CN112714765B/zh active Active
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- 2019-09-13 HU HUE19765747A patent/HUE060943T2/hu unknown
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2021
- 2021-02-10 PH PH12021550299A patent/PH12021550299A1/en unknown
- 2021-02-12 ZA ZA2021/00976A patent/ZA202100976B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2022500445A (ja) | 2022-01-04 |
| AU2019338236A1 (en) | 2021-05-20 |
| EP3849976B1 (en) | 2022-10-26 |
| US11396510B2 (en) | 2022-07-26 |
| JP7353663B2 (ja) | 2023-10-02 |
| DK3849976T3 (da) | 2023-01-23 |
| IL281335B1 (en) | 2024-03-01 |
| IL281335A (en) | 2021-04-29 |
| EA202190717A1 (ru) | 2021-09-22 |
| LT3849976T (lt) | 2023-02-10 |
| CN112714765A (zh) | 2021-04-27 |
| PH12021550299A1 (en) | 2021-10-25 |
| HUE060943T2 (hu) | 2023-04-28 |
| PT3849976T (pt) | 2023-01-13 |
| KR102712565B1 (ko) | 2024-10-02 |
| FI3849976T3 (fi) | 2023-02-19 |
| WO2020053377A1 (en) | 2020-03-19 |
| SG11202101360VA (en) | 2021-03-30 |
| PL3849976T3 (pl) | 2023-02-27 |
| CN112714765B (zh) | 2023-06-30 |
| IL281335B2 (en) | 2024-07-01 |
| CA3110283A1 (en) | 2020-03-19 |
| US20210332042A1 (en) | 2021-10-28 |
| EP3849976A1 (en) | 2021-07-21 |
| MX2021003010A (es) | 2021-05-27 |
| ES2935705T3 (es) | 2023-03-09 |
| SI3849976T1 (sl) | 2023-03-31 |
| ZA202100976B (en) | 2022-08-31 |
| HRP20230067T1 (hr) | 2023-03-17 |
| KR20210061338A (ko) | 2021-05-27 |
| AU2019338236B2 (en) | 2025-01-09 |
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| B06W | Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette] |