AR125363A1 - Nuevos derivados de pirazolo[1,5-a]pirimidina como ligandos sigma - Google Patents
Nuevos derivados de pirazolo[1,5-a]pirimidina como ligandos sigmaInfo
- Publication number
- AR125363A1 AR125363A1 ARP220100976A ARP220100976A AR125363A1 AR 125363 A1 AR125363 A1 AR 125363A1 AR P220100976 A ARP220100976 A AR P220100976A AR P220100976 A ARP220100976 A AR P220100976A AR 125363 A1 AR125363 A1 AR 125363A1
- Authority
- AR
- Argentina
- Prior art keywords
- atom
- radical
- group
- alkyl radical
- haloalkyl
- Prior art date
Links
- 239000003446 ligand Substances 0.000 title abstract 2
- LDIJKUBTLZTFRG-UHFFFAOYSA-N pyrazolo[1,5-a]pyrimidine Chemical class N1=CC=CN2N=CC=C21 LDIJKUBTLZTFRG-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 108010085082 sigma receptors Proteins 0.000 abstract 2
- 102100028656 Sigma non-opioid intracellular receptor 1 Human genes 0.000 abstract 1
- 101710104750 Sigma non-opioid intracellular receptor 1 Proteins 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
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
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente invención se refiere a nuevos compuestos de fórmula (1) como ligandos sigma que tienen una gran afinidad por sigma receptores, receptor sigma-1 (s1) y/o receptor (s2). La presente invención también se refiere al proceso para su preparación, a las composiciones que los contienen, y a su uso como medicamentos. Reivindicación 1: Un compuesto de fórmula general (1) en donde W¹, W², W³, W⁴ y W⁵ representan de modo independiente entre sí un átomo de N, un átomo de C o -CH- con la condición de que, independientemente de su significado, los anillos sean siempre aromáticos, tal como se representa con las líneas de puntos. R¹ y R² son de modo independiente entre sí hidrógeno o un radical alquilo C₁-C₆ lineal o ramificado o, alternativamente, R¹ y R² junto con el átomo de N al que están unidos, forman un heterociclo saturado que opcionalmente contiene un heteroátomo adicional seleccionado de N u O y opcionalmente sustituido con al menos uno de un radical alquilo C₁-C₆, un átomo de halógeno, un radical haloalquilo C₁-C₆, un grupo -(CH₂)ₙOR, un grupo arilo, un heterociclo saturado de 3 a 6 miembros que contiene al menos un heteroátomo seleccionado de N u O, o alternativamente R¹ y R² junto con el átomo de N al que están unidos, forman un espiro-heterociclo saturado que contiene opcionalmente un heteroátomo adicional seleccionado de O, N o S y está opcionalmente sustituido con al menos uno de un radical alquilo C₁-C₆, un átomo de halógeno, un radical haloalquilo C₁-C₆, un grupo -(CH₂)ₙOR; R es un átomo de H o un radical alquilo C₁-C₆; n es 0 o 1 R³ es un radical piridinilo opcionalmente sustituido con un radical alquilo C₁-C₆, un átomo de halógeno, un radical haloalquilo C₁-C₆, un grupo OH, un grupo alcoxi C₁₋₆ o un grupo ciano; R⁴, R⁴ son de modo independiente entre sí hidrógeno o un radical alquilo C₁-C₆ lineal o ramificado; R⁵ y R⁵ son de modo independiente entre sí hidrógeno, halógeno, alquilo C₁-₆, haloalquilo C₁₋₆, alcoxi C₁-₆, -CN; R⁶ es hidrógeno, halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₆, -CN; en donde el compuesto de fórmula (1) está opcionalmente en forma de uno de los estereoisómeros, con preferencia enantiómeros o diastereómeros, un racemato o en forma de una mezcla de al menos dos de los estereoisómeros, con preferencia enantiómeros y/o diastereómeros, en cualquier relación de mezcla, o una correspondiente sal, cocristal o profármaco del mismo. Reivindicación 5: Un compuesto de acuerdo con la reivindicación 1 que tiene una de las fórmulas generales (1), (1a), (1b) o (1c) en donde R¹, R², R³, R⁴, R⁴, R⁵, R⁵ y R⁶ son como se definen en cualquiera de las reivindicaciones previas. Reivindicación 11: Un compuesto de acuerdo con la reivindicación 10 para uso en el tratamiento y/o profilaxis de enfermedades y/o trastornos mediados por un receptor sigma.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP21382324 | 2021-04-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR125363A1 true AR125363A1 (es) | 2023-07-12 |
Family
ID=75581480
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP220100976A AR125363A1 (es) | 2021-04-16 | 2022-04-18 | Nuevos derivados de pirazolo[1,5-a]pirimidina como ligandos sigma |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20240246966A1 (es) |
| EP (1) | EP4323363A1 (es) |
| JP (1) | JP2024514200A (es) |
| KR (1) | KR20240021758A (es) |
| CN (1) | CN117561261A (es) |
| AR (1) | AR125363A1 (es) |
| AU (1) | AU2022256725A1 (es) |
| BR (1) | BR112023021381A2 (es) |
| CA (1) | CA3215521A1 (es) |
| IL (1) | IL307766A (es) |
| MX (1) | MX2023012246A (es) |
| TW (1) | TW202304453A (es) |
| WO (1) | WO2022218856A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2024105225A1 (en) | 2022-11-18 | 2024-05-23 | Universitat De Barcelona | Synergistic combinations of a sigma receptor 1 (s1r) antagonist and a soluble epoxide hydrolase inhibitor (sehi) and their use in the treatment of pain |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010055126A1 (en) * | 2008-11-14 | 2010-05-20 | Neurosearch A/S | Benzimidazole derivatives and their use for modulating the gabaa receptor complex |
| EP2733143A1 (en) * | 2012-11-14 | 2014-05-21 | Laboratorios Del Dr. Esteve, S.A. | Substituted pyrazolo[3,4-d]pyrimidine compounds, their preparation and use as sigma receptors ligands |
-
2022
- 2022-04-08 CA CA3215521A patent/CA3215521A1/en active Pending
- 2022-04-08 WO PCT/EP2022/059439 patent/WO2022218856A1/en active Application Filing
- 2022-04-08 CN CN202280042742.3A patent/CN117561261A/zh active Pending
- 2022-04-08 EP EP22721381.6A patent/EP4323363A1/en active Pending
- 2022-04-08 MX MX2023012246A patent/MX2023012246A/es unknown
- 2022-04-08 US US18/555,720 patent/US20240246966A1/en active Pending
- 2022-04-08 BR BR112023021381A patent/BR112023021381A2/pt unknown
- 2022-04-08 KR KR1020237038467A patent/KR20240021758A/ko unknown
- 2022-04-08 JP JP2023563207A patent/JP2024514200A/ja active Pending
- 2022-04-08 IL IL307766A patent/IL307766A/en unknown
- 2022-04-08 AU AU2022256725A patent/AU2022256725A1/en active Pending
- 2022-04-14 TW TW111114198A patent/TW202304453A/zh unknown
- 2022-04-18 AR ARP220100976A patent/AR125363A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20240246966A1 (en) | 2024-07-25 |
| JP2024514200A (ja) | 2024-03-28 |
| EP4323363A1 (en) | 2024-02-21 |
| IL307766A (en) | 2023-12-01 |
| MX2023012246A (es) | 2023-10-30 |
| WO2022218856A1 (en) | 2022-10-20 |
| CA3215521A1 (en) | 2022-10-20 |
| TW202304453A (zh) | 2023-02-01 |
| AU2022256725A1 (en) | 2023-11-02 |
| BR112023021381A2 (pt) | 2023-12-19 |
| KR20240021758A (ko) | 2024-02-19 |
| CN117561261A (zh) | 2024-02-13 |
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