EA201790396A1 - Активный метаболит димезилатмоногидрата 1-[(2-бромфенил)сульфонил]-5-метокси-3-[(4-метил-1-пиперазинил)метил]-1h-индола и димезилатдигидратная соль активного метаболита - Google Patents
Активный метаболит димезилатмоногидрата 1-[(2-бромфенил)сульфонил]-5-метокси-3-[(4-метил-1-пиперазинил)метил]-1h-индола и димезилатдигидратная соль активного метаболитаInfo
- Publication number
- EA201790396A1 EA201790396A1 EA201790396A EA201790396A EA201790396A1 EA 201790396 A1 EA201790396 A1 EA 201790396A1 EA 201790396 A EA201790396 A EA 201790396A EA 201790396 A EA201790396 A EA 201790396A EA 201790396 A1 EA201790396 A1 EA 201790396A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- methyl
- retrattrahretretritretratretr
- piperasininyl
- dimezyletdihdrett
- dimezilatmonhydrat
- Prior art date
Links
- -1 2-BROMPHENYL Chemical class 0.000 title abstract 2
- RAHZWNYVWXNFOC-UHFFFAOYSA-N Sulphur dioxide Chemical compound O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 title 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 title 1
- 229940127239 5 Hydroxytryptamine receptor antagonist Drugs 0.000 abstract 1
- MPBVSCLRCJRANQ-UHFFFAOYSA-N O.COc1ccc2n(cc(CN3CCN(C)CC3)c2c1)S(=O)(=O)c1ccccc1Br Chemical compound O.COc1ccc2n(cc(CN3CCN(C)CC3)c2c1)S(=O)(=O)c1ccccc1Br MPBVSCLRCJRANQ-UHFFFAOYSA-N 0.000 abstract 1
- 239000003420 antiserotonin agent Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—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
- A61K31/4035—Isoindoles, e.g. phthalimide
-
- 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
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
- C07C309/01—Sulfonic acids
- C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/14—Sulfones; Sulfoxides having sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Настоящее изобретение относится к активному метаболиту димезилатмоногидрата 1-[(2-бромфенил)сульфонил]-5-метокси-3-[(4-метил-1-пиперазинил)метил]-1Н-индола, имеющему следующую структуру:Настоящее изобретение также относится к димезилатдигидратной соли формулы (I), имеющей следующую структуру:Соединения формулы (I) и формулы (II) полезны при лечении различных заболеваний, которые связаны с антагонистом рецептора 5-НТ.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN4011CH2014 | 2014-08-16 | ||
| PCT/IN2014/000667 WO2016027276A1 (en) | 2014-08-16 | 2014-10-20 | Active metabolite of 1-[(2-bromophenyl) sulfonyl]-5-methoxy-3- [(4-methyl-1-piperazinyl) methyl]-1h-indole dimesylate monohydrate and dimesylate dihydrate salt of active metabolite |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201790396A1 true EA201790396A1 (ru) | 2017-06-30 |
| EA031319B1 EA031319B1 (ru) | 2018-12-28 |
Family
ID=52345478
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201790396A EA031319B1 (ru) | 2014-08-16 | 2014-10-20 | Активный метаболит димезилатмоногидрата 1-[(2-бромфенил)сульфонил]-5-метокси-3-[(4-метил-1-пиперазинил)метил]-1h-индола и димезилатдигидратная соль активного метаболита |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US10010527B2 (ru) |
| EP (1) | EP3180001B1 (ru) |
| JP (1) | JP6629322B2 (ru) |
| KR (1) | KR101938408B1 (ru) |
| CN (1) | CN106794170A (ru) |
| AP (1) | AP2017009752A0 (ru) |
| AU (1) | AU2014404000B2 (ru) |
| BR (1) | BR112017002921B1 (ru) |
| CA (1) | CA2957497C (ru) |
| CY (1) | CY1121393T1 (ru) |
| DK (1) | DK3180001T3 (ru) |
| EA (1) | EA031319B1 (ru) |
| ES (1) | ES2715113T3 (ru) |
| HR (1) | HRP20190446T1 (ru) |
| HU (1) | HUE044011T2 (ru) |
| IL (1) | IL250411B (ru) |
| LT (1) | LT3180001T (ru) |
| MX (1) | MX2017002045A (ru) |
| NZ (1) | NZ728907A (ru) |
| PL (1) | PL3180001T3 (ru) |
| PT (1) | PT3180001T (ru) |
| RS (1) | RS58575B1 (ru) |
| SG (1) | SG11201701106RA (ru) |
| SI (1) | SI3180001T1 (ru) |
| TR (1) | TR201903344T4 (ru) |
| WO (1) | WO2016027276A1 (ru) |
| ZA (1) | ZA201700915B (ru) |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL361887A1 (en) * | 2000-10-20 | 2004-10-04 | Biovitrum Ab | 2-, 3-, 4-, or 5-substituted-n1-(benzensulfonyl)indoles and their use in therapy |
| ATE401072T1 (de) * | 2002-02-12 | 2008-08-15 | Organon Nv | 1-arylsulfonyl-3-substituierte indol und indolinederivate verwendbar zur behandlung von erkrankungen des zentralnervensystem |
| NZ572186A (en) * | 2002-11-28 | 2010-02-26 | Suven Life Sciences Ltd | N-arylsulfonyl-3-substituted indoles having serotonin receptor affinity, process for their preparation and pharmaceutical composition containing them |
| PT1581538E (pt) * | 2002-12-18 | 2007-05-31 | Suven Life Sciences Ltd | Indolos tetracíclicos substituidos na posição 3 que possuem afinidade pelo receptor de serotonina. |
| AU2008216032A1 (en) * | 2007-02-16 | 2008-08-21 | Memory Pharmaceuticals Corporation | 6 ' substituted indole and indazole derivatives having 5-HT6 receptor affinity |
| ES2370680T3 (es) * | 2007-10-26 | 2011-12-21 | Suven Life Sciences Limited | Compuestos de aminoarilsulfonamida y su empleo como ligandos de 5-ht6. |
-
2014
- 2014-10-20 CN CN201480081234.1A patent/CN106794170A/zh active Pending
- 2014-10-20 JP JP2017527993A patent/JP6629322B2/ja active Active
- 2014-10-20 KR KR1020177004616A patent/KR101938408B1/ko active IP Right Grant
- 2014-10-20 EP EP14825443.6A patent/EP3180001B1/en active Active
- 2014-10-20 US US15/504,014 patent/US10010527B2/en active Active
- 2014-10-20 LT LTEP14825443.6T patent/LT3180001T/lt unknown
- 2014-10-20 ES ES14825443T patent/ES2715113T3/es active Active
- 2014-10-20 TR TR2019/03344T patent/TR201903344T4/tr unknown
- 2014-10-20 AP AP2017009752A patent/AP2017009752A0/en unknown
- 2014-10-20 WO PCT/IN2014/000667 patent/WO2016027276A1/en active Application Filing
- 2014-10-20 NZ NZ728907A patent/NZ728907A/en unknown
- 2014-10-20 CA CA2957497A patent/CA2957497C/en active Active
- 2014-10-20 MX MX2017002045A patent/MX2017002045A/es active IP Right Grant
- 2014-10-20 AU AU2014404000A patent/AU2014404000B2/en active Active
- 2014-10-20 PL PL14825443T patent/PL3180001T3/pl unknown
- 2014-10-20 BR BR112017002921-9A patent/BR112017002921B1/pt active IP Right Grant
- 2014-10-20 RS RS20190286A patent/RS58575B1/sr unknown
- 2014-10-20 SI SI201431124T patent/SI3180001T1/sl unknown
- 2014-10-20 DK DK14825443.6T patent/DK3180001T3/en active
- 2014-10-20 HU HUE14825443A patent/HUE044011T2/hu unknown
- 2014-10-20 PT PT14825443T patent/PT3180001T/pt unknown
- 2014-10-20 EA EA201790396A patent/EA031319B1/ru unknown
- 2014-10-20 SG SG11201701106RA patent/SG11201701106RA/en unknown
-
2017
- 2017-02-02 IL IL250411A patent/IL250411B/en active IP Right Grant
- 2017-02-06 ZA ZA2017/00915A patent/ZA201700915B/en unknown
-
2019
- 2019-03-06 HR HRP20190446TT patent/HRP20190446T1/hr unknown
- 2019-03-08 CY CY20191100280T patent/CY1121393T1/el unknown
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