AR115020A1 - Compuesto heterocíclico nitrogenado y su uso como antagonista del receptor nmda - Google Patents
Compuesto heterocíclico nitrogenado y su uso como antagonista del receptor nmdaInfo
- Publication number
- AR115020A1 AR115020A1 ARP190100766A ARP190100766A AR115020A1 AR 115020 A1 AR115020 A1 AR 115020A1 AR P190100766 A ARP190100766 A AR P190100766A AR P190100766 A ARP190100766 A AR P190100766A AR 115020 A1 AR115020 A1 AR 115020A1
- Authority
- AR
- Argentina
- Prior art keywords
- atom
- alkyl group
- nitrogen atom
- optionally substituted
- cra
- Prior art date
Links
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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines 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
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4833—Encapsulating processes; Filling of capsules
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente proporciona un compuesto heterocíclico que tiene una acción antagonista sobre un receptor de NMDA que contiene la subunidad NR2B y se espera que sea de utilidad como un agente para la prevención o el tratamiento de depresión mayor, trastorno bipolar, migraña, dolor, comportamiento y síntomas psicológicos de demencia, y similares. La presente se refiere a un compuesto representado por la fórmula (1), en donde cada símbolo es como se describe en la descripción, o una de sus sales. Reivindicación 1: Un compuesto representado por la fórmula [1] caracterizado porque el grupo representado por la fórmula [2] es un grupo representado por los compuestos de fórmula [3] ó [4]; Xᵃ¹ es CH o un átomo de nitrógeno; Xᵃ² es (1) CRᵃ en donde Rᵃ es (a) un átomo de hidrógeno, (b) un átomo de halógeno o (c) un grupo alquilo C₁₋₆ o (2) un átomo de nitrógeno; Xᵃ³ es (1) CRᵃ en donde Rᵃ es (a) un átomo de hidrógeno o (b) un grupo alquilo C₁₋₆ o (2) un átomo de nitrógeno; Xᵃ⁴ es (1) CRᵃ en donde Rᵃ es (a) un átomo de hidrógeno o (b) un grupo alquilo C₁₋₆ o (2) un átomo de nitrógeno; y Xᵃ⁵ es (1) CRᵃ en donde Rᵃ es (a) un átomo de hidrógeno, (b) un grupo alquilo C₁₋₆ opcionalmente sustituido con 1 a 3 sustituyentes seleccionados de un átomo de halógeno y un grupo alcoxi C₁₋₆, (c) un grupo alcoxi C₁₋₆ o (d) un grupo cicloalquilo C₃₋₁₀ o (2) un átomo de nitrógeno; siempre que, cuando Xᵃ⁵ es CRᵃ, entonces al menos uno de Xᵃ¹, Xᵃ² y Xᵃ³ es un átomo de nitrógeno; Xᵇ¹ es CH o un átomo de nitrógeno; Xᵇ² es CRᵇ en donde Rᵇ es (a) un átomo de hidrógeno o (b) un grupo alquilo C₁₋₆; Xᵇ³ es un átomo de nitrógeno opcionalmente sustituido con un grupo alquilo C₁₋₆ opcionalmente sustituido con 1 a 3 átomos de halógeno; y Xᵇ⁴ es CRᵇ en donde Rᵇ es (a) un átomo de hidrógeno o (b) un grupo alquilo C₁₋₆; R¹ y R² son ambos átomos de hidrógeno; y R³ es un grupo representado por los compuestos de fórmula [5] ó [6]; R⁴ es (1) un grupo alquilo C₁₋₆ opcionalmente sustituido con 1 a 3 átomos de halógeno, (2) un grupo alcoxi C₁₋₆ opcionalmente sustituido con 1 a 3 átomos de halógeno, (3) un grupo cicloalquil C₃₋₁₀-oxi o (4) un átomo de halógeno; Y es un átomo de nitrógeno o CR⁶ en donde R⁶ es un átomo de hidrógeno o un átomo de halógeno; y el anillo C¹ es un anillo benceno (es decir, Y es CR⁶) o un anillo piridina (es decir, Y es N), cada uno de los cuales está opcionalmente sustituido con un átomo de halógeno; R⁵ es un grupo alquilo C₁₋₆ opcionalmente sustituido con 1 a 3 átomos de halógeno; y el anillo C² es un anillo tiofeno sustituido con sólo R⁵; o una de sus sales.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2018062939 | 2018-03-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR115020A1 true AR115020A1 (es) | 2020-11-18 |
Family
ID=66397395
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190100766A AR115020A1 (es) | 2018-03-28 | 2019-03-27 | Compuesto heterocíclico nitrogenado y su uso como antagonista del receptor nmda |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US10807987B2 (es) |
| EP (1) | EP3774800A1 (es) |
| JP (1) | JP7279067B2 (es) |
| KR (1) | KR20200136957A (es) |
| CN (1) | CN111936495A (es) |
| AR (1) | AR115020A1 (es) |
| AU (1) | AU2019241765B2 (es) |
| BR (1) | BR112020018238A2 (es) |
| CA (1) | CA3100133A1 (es) |
| EA (1) | EA202092294A1 (es) |
| IL (1) | IL276912A (es) |
| MA (1) | MA52214A (es) |
| MX (1) | MX2020010148A (es) |
| SG (1) | SG11202008519RA (es) |
| TW (1) | TW202003519A (es) |
| WO (1) | WO2019189945A1 (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7114594B2 (ja) | 2017-07-28 | 2022-08-08 | 武田薬品工業株式会社 | 複素環化合物 |
| TW202003519A (zh) * | 2018-03-28 | 2020-01-16 | 日商武田藥品工業股份有限公司 | 雜環化合物及其用途 |
| JP2021050161A (ja) | 2019-09-25 | 2021-04-01 | 武田薬品工業株式会社 | 複素環化合物及びその用途 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2492382A1 (fr) * | 1980-10-22 | 1982-04-23 | Synthelabo | Derives d'imidazo (1,2-a) pyridine, leur preparation et leur application en therapeutique |
| US5252563A (en) * | 1991-12-19 | 1993-10-12 | G. D. Searle & Company | 5,6,7,8-tetrahydro-imidazo[1,2-a]pyrimidine compounds for treatment of neurotoxic injury |
| JP3439551B2 (ja) * | 1994-11-08 | 2003-08-25 | 富士写真フイルム株式会社 | ハロゲン化銀写真感光材料 |
| ES2175083T3 (es) | 1995-03-14 | 2002-11-16 | Praecis Pharm Inc | Moduladores de la agregacion de amiloides. |
| DE69733655T2 (de) | 1996-08-27 | 2006-04-27 | Praecis Pharmaceuticals, Inc., Cambridge | beta-AMYLOID PEPTIDAGGREGATION REGULIERENDE PEPTIDE MIT D-AMINOSÄUREN |
| US6331640B1 (en) | 1998-10-13 | 2001-12-18 | Hoffmann-La Roche Inc. | Diaminopropionic acid derivatives |
| US6545127B1 (en) | 1999-06-28 | 2003-04-08 | Oklahoma Medical Research Foundation | Catalytically active recombinant memapsin and methods of use thereof |
| WO2002080928A1 (en) * | 2001-04-03 | 2002-10-17 | Merck & Co., Inc. | N-substituted nonaryl-heterocyclo amidyl nmda/nr2b antagonists |
| JP2004161716A (ja) * | 2002-11-15 | 2004-06-10 | Takeda Chem Ind Ltd | Ｊｎｋ阻害剤 |
| JP2006522794A (ja) * | 2003-04-10 | 2006-10-05 | ファイザー株式会社 | Ｎｒ２ｂ受容体拮抗物質としての二環系化合物 |
| US20080234318A1 (en) | 2005-08-31 | 2008-09-25 | Kristjan Gudmundsson | Chemical Compounds |
| US8450363B2 (en) * | 2009-02-06 | 2013-05-28 | Elan Pharmaceuticals, Inc. | Inhibitors of Jun N-terminal kinase |
| US8404859B2 (en) | 2011-03-16 | 2013-03-26 | Hoffmann-La Roche Inc. | Thiazole and thiophene compounds |
| CN103534257A (zh) * | 2011-04-05 | 2014-01-22 | 辉瑞有限公司 | 作为原肌球蛋白相关激酶抑制剂的吡咯并[2,3-d]嘧啶衍生物 |
| FR2998892B1 (fr) | 2012-12-04 | 2015-01-02 | Pf Medicament | Derives d'aminocyclobutane, leur procede de preparation et leur utilisation a titre de medicaments |
| CA2903572A1 (en) | 2013-03-15 | 2014-10-23 | Epizyme, Inc. | Substituted benzene compounds |
| US9243001B2 (en) | 2013-03-15 | 2016-01-26 | Epizyme, Inc. | Substituted benzene compounds |
| EP3239150B1 (en) * | 2014-12-24 | 2020-02-05 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| JP6827757B2 (ja) | 2016-10-11 | 2021-02-10 | 鬼怒川ゴム工業株式会社 | ウエザーストリップ取付用クリップ |
| JP7114594B2 (ja) | 2017-07-28 | 2022-08-08 | 武田薬品工業株式会社 | 複素環化合物 |
| TW202003519A (zh) * | 2018-03-28 | 2020-01-16 | 日商武田藥品工業股份有限公司 | 雜環化合物及其用途 |
| JP7541487B2 (ja) | 2019-01-24 | 2024-08-28 | 武田薬品工業株式会社 | 複素環化合物及びその用途 |
| WO2020196828A1 (ja) | 2019-03-28 | 2020-10-01 | 武田薬品工業株式会社 | 含窒素複素環化合物 |
-
2019
- 2019-03-27 TW TW108110758A patent/TW202003519A/zh unknown
- 2019-03-27 MA MA052214A patent/MA52214A/fr unknown
- 2019-03-27 WO PCT/JP2019/014901 patent/WO2019189945A1/en unknown
- 2019-03-27 CN CN201980023246.1A patent/CN111936495A/zh active Pending
- 2019-03-27 AU AU2019241765A patent/AU2019241765B2/en active Active
- 2019-03-27 BR BR112020018238-9A patent/BR112020018238A2/pt not_active IP Right Cessation
- 2019-03-27 KR KR1020207030605A patent/KR20200136957A/ko not_active Application Discontinuation
- 2019-03-27 CA CA3100133A patent/CA3100133A1/en active Pending
- 2019-03-27 EP EP19721865.4A patent/EP3774800A1/en active Pending
- 2019-03-27 SG SG11202008519RA patent/SG11202008519RA/en unknown
- 2019-03-27 JP JP2020551599A patent/JP7279067B2/ja active Active
- 2019-03-27 EA EA202092294A patent/EA202092294A1/ru unknown
- 2019-03-27 AR ARP190100766A patent/AR115020A1/es unknown
- 2019-03-27 MX MX2020010148A patent/MX2020010148A/es unknown
- 2019-03-27 US US16/366,710 patent/US10807987B2/en active Active
-
2020
- 2020-08-25 IL IL276912A patent/IL276912A/en unknown
-
2021
- 2021-03-15 US US17/201,878 patent/US11702419B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| MA52214A (fr) | 2021-04-21 |
| KR20200136957A (ko) | 2020-12-08 |
| JP2021519294A (ja) | 2021-08-10 |
| TW202003519A (zh) | 2020-01-16 |
| US20210332053A1 (en) | 2021-10-28 |
| CN111936495A (zh) | 2020-11-13 |
| EP3774800A1 (en) | 2021-02-17 |
| US20190300536A1 (en) | 2019-10-03 |
| AU2019241765B2 (en) | 2022-07-07 |
| US11702419B2 (en) | 2023-07-18 |
| US10807987B2 (en) | 2020-10-20 |
| AU2019241765A8 (en) | 2021-02-18 |
| WO2019189945A1 (en) | 2019-10-03 |
| IL276912A (en) | 2020-10-29 |
| CA3100133A1 (en) | 2019-10-03 |
| AU2019241765A1 (en) | 2020-11-12 |
| EA202092294A1 (ru) | 2021-01-15 |
| SG11202008519RA (en) | 2020-10-29 |
| MX2020010148A (es) | 2020-12-07 |
| JP7279067B2 (ja) | 2023-05-22 |
| BR112020018238A2 (pt) | 2020-12-29 |
| WO2019189945A8 (en) | 2020-10-15 |
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