AR119728A1 - Derivados de 1,1-dioxido de 3-amino-4h-benzo[e][1,2,4]tiadiazina como inhibidores de mrgx2 - Google Patents
Derivados de 1,1-dioxido de 3-amino-4h-benzo[e][1,2,4]tiadiazina como inhibidores de mrgx2Info
- Publication number
- AR119728A1 AR119728A1 ARP200101202A ARP200101202A AR119728A1 AR 119728 A1 AR119728 A1 AR 119728A1 AR P200101202 A ARP200101202 A AR P200101202A AR P200101202 A ARP200101202 A AR P200101202A AR 119728 A1 AR119728 A1 AR 119728A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituents
- alkyl
- independently selected
- optional
- amino
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/15—Six-membered rings
- C07D285/16—Thiadiazines; Hydrogenated thiadiazines
- C07D285/18—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines
- C07D285/20—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems
- C07D285/22—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
- C07D285/24—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with oxygen atoms directly attached to the ring sulfur atom
- C07D285/26—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with oxygen atoms directly attached to the ring sulfur atom substituted in position 6 or 7 by sulfamoyl or substituted sulfamoyl radicals
- C07D285/32—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with oxygen atoms directly attached to the ring sulfur atom substituted in position 6 or 7 by sulfamoyl or substituted sulfamoyl radicals with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/15—Six-membered rings
- C07D285/16—Thiadiazines; Hydrogenated thiadiazines
- C07D285/18—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines
- C07D285/20—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems
- C07D285/22—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
- C07D285/24—1,2,4-Thiadiazines; Hydrogenated 1,2,4-thiadiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with oxygen atoms directly attached to the ring sulfur atom
-
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/549—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Physical Education & Sports Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Se describen compuestos de fórmula (1), tautómeros de estos y sales farmacéuticamente aceptables de los compuestos o tautómeros, donde L, R¹, R², R³, R⁴ y R⁵ se definen en la memoria descriptiva. Esta descripción también hace referencia a materiales y métodos para la preparación de compuestos de fórmula (1), a composiciones farmacéuticas que los contienen y a su uso para el tratamiento de enfermedades, trastornos o afecciones asociados con MRGX2. Reivindicación 1: Un compuesto de fórmula (1), o un tautómero de este, o una sal farmacéuticamente aceptable del compuesto de fórmula (1) o tautómero de este, donde: L se selecciona de un enlace y alcanodiilo C₁₋₄; R¹ se selecciona de (a) alquilo C₁₋₄ que se sustituye con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo, hidroxi, ciano, alcoxi C₁₋₄, amino y aminocarbonilo, donde cada uno de los sustituyentes opcionales de alcoxi C₁₋₄ se sustituye independientemente con 0 a 3 sustituyentes que se seleccionan independientemente de halo, y donde cada uno de los sustituyentes opcionales amino y aminocarbonilo se sustituye independientemente con 0 a 2 sustituyentes que se seleccionan independientemente de alquilo C₁₋₄; y (b) un grupo cíclico que se selecciona de cicloalquilo C₃₋₈, heterociclilo C₂₋₉, arilo C₆₋₁₄ y heteroarilo C₁₋₉, donde el grupo cíclico se sustituye con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo, hidroxi, ciano, alquilo C₁₋₄, alcoxi C₁₋₄, amino y aminocarbonilo, donde cada uno de los sustituyentes opcionales de alquilo C₁₋₄ y alcoxi C₁₋₄ se sustituye independientemente con 0 a 3 sustituyentes que se seleccionan independientemente de halo, y donde cada uno de los sustituyentes opcionales amino y aminocarbonilo se sustituye independientemente con 0 a 2 sustituyentes que se seleccionan independientemente de alquilo C₁₋₄; R² se selecciona de (a) alquilo C₁₋₄, que se sustituye con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo, hidroxi, ciano, alcoxi C₁₋₄ y amino; y (b) un grupo cíclico que se selecciona de cicloalquilo C₃₋₈, heterociclilo C₂₋₉, arilo C₆₋₁₄ y heteroarilo C₁₋₉, donde el grupo cíclico se sustituye con 0 a 3 sustituyentes opcionales que se seleccionan independientemente de halo, hidroxi, ciano, alquilo C₁₋₄, alcoxi C₁₋₄, amino, cicloalquilo C₃₋₈ y heterociclilo C₃₋₅, siempre y cuando el grupo cíclico no tenga más de un sustituyente opcional que se selecciona de cicloalquilo C₃₋₈ y heterociclilo C₃₋₅, y donde cada uno de los sustituyentes opcionales de alquilo C₁₋₄, alcoxi C₁₋₄, cicloalquilo C₃₋₈ y heterociclilo C₃₋₅ se sustituye independientemente con 0 a 3 sustituyentes que se seleccionan independientemente de halo, y donde el sustituyente opcional amino se sustituye independientemente con 0 a 2 sustituyentes que se seleccionan independientemente de alquilo C₁₋₄; cada uno de R³, R⁴ y R⁵ se selecciona independientemente de hidrógeno, halo, ciano y alquilo C₁₋₃; donde cada uno de los restos heterociclilo y heteroarilo antemencionados tiene independientemente de 1 a 4 heteroátomos como miembros anulares, donde cada uno se selecciona independientemente de N, O y S.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962840344P | 2019-04-29 | 2019-04-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR119728A1 true AR119728A1 (es) | 2022-01-05 |
Family
ID=70779887
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP200101202A AR119728A1 (es) | 2019-04-29 | 2020-04-29 | Derivados de 1,1-dioxido de 3-amino-4h-benzo[e][1,2,4]tiadiazina como inhibidores de mrgx2 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US20220119361A1 (es) |
| EP (1) | EP3962901A1 (es) |
| JP (1) | JP2022535672A (es) |
| KR (1) | KR20220012244A (es) |
| CN (1) | CN114072393A (es) |
| AR (1) | AR119728A1 (es) |
| AU (1) | AU2020266529A1 (es) |
| BR (1) | BR112021021508A2 (es) |
| CA (1) | CA3137584A1 (es) |
| CL (1) | CL2021002805A1 (es) |
| CO (1) | CO2021014155A2 (es) |
| CR (1) | CR20210544A (es) |
| DO (1) | DOP2021000223A (es) |
| EC (1) | ECSP21080966A (es) |
| IL (1) | IL287521A (es) |
| JO (1) | JOP20210275A1 (es) |
| MA (1) | MA55804A (es) |
| MX (1) | MX2021013135A (es) |
| PE (1) | PE20220425A1 (es) |
| SG (1) | SG11202111717XA (es) |
| WO (1) | WO2020223255A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2022152852A1 (en) * | 2021-01-15 | 2022-07-21 | Glaxosmithkline Intellectual Property Development Limited | Antagonists of mrgx2 |
| WO2022152853A1 (en) * | 2021-01-15 | 2022-07-21 | Glaxosmithkline Intellectual Property Development Limited | Antagonists of mrgx2 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| GB9518953D0 (en) | 1995-09-15 | 1995-11-15 | Pfizer Ltd | Pharmaceutical formulations |
| GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
| WO2006089286A2 (en) * | 2005-02-18 | 2006-08-24 | Acadia Pharmaceuticals Inc. | Triazadibenzoazulene compounds useful for the treatment and prevention of pain and screening methods therefor compounds useful for the treatment and prevention of pain and screening methods therefor |
| US20080249081A1 (en) * | 2006-10-24 | 2008-10-09 | Roger Olsson | Compounds for the treatment of pain and screening methods therefor |
-
2020
- 2020-04-28 JO JOP/2021/0275A patent/JOP20210275A1/ar unknown
- 2020-04-28 MX MX2021013135A patent/MX2021013135A/es unknown
- 2020-04-28 BR BR112021021508A patent/BR112021021508A2/pt unknown
- 2020-04-28 PE PE2021001772A patent/PE20220425A1/es unknown
- 2020-04-28 SG SG11202111717XA patent/SG11202111717XA/en unknown
- 2020-04-28 KR KR1020217037664A patent/KR20220012244A/ko unknown
- 2020-04-28 CN CN202080047972.XA patent/CN114072393A/zh active Pending
- 2020-04-28 WO PCT/US2020/030305 patent/WO2020223255A1/en active Application Filing
- 2020-04-28 AU AU2020266529A patent/AU2020266529A1/en active Pending
- 2020-04-28 CR CR20210544A patent/CR20210544A/es unknown
- 2020-04-28 EP EP20727455.6A patent/EP3962901A1/en active Pending
- 2020-04-28 US US17/605,962 patent/US20220119361A1/en active Pending
- 2020-04-28 JP JP2021564138A patent/JP2022535672A/ja active Pending
- 2020-04-28 MA MA055804A patent/MA55804A/fr unknown
- 2020-04-28 CA CA3137584A patent/CA3137584A1/en active Pending
- 2020-04-29 AR ARP200101202A patent/AR119728A1/es unknown
-
2021
- 2021-10-22 CO CONC2021/0014155A patent/CO2021014155A2/es unknown
- 2021-10-24 IL IL287521A patent/IL287521A/en unknown
- 2021-10-26 CL CL2021002805A patent/CL2021002805A1/es unknown
- 2021-10-29 DO DO2021000223A patent/DOP2021000223A/es unknown
- 2021-11-15 EC ECSENADI202180966A patent/ECSP21080966A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CL2021002805A1 (es) | 2022-07-22 |
| CR20210544A (es) | 2022-03-30 |
| BR112021021508A2 (pt) | 2022-03-22 |
| JP2022535672A (ja) | 2022-08-10 |
| DOP2021000223A (es) | 2022-01-16 |
| IL287521A (en) | 2021-12-01 |
| US20220119361A1 (en) | 2022-04-21 |
| SG11202111717XA (en) | 2021-11-29 |
| CA3137584A1 (en) | 2020-11-05 |
| PE20220425A1 (es) | 2022-03-29 |
| MX2021013135A (es) | 2021-11-25 |
| CO2021014155A2 (es) | 2021-10-29 |
| MA55804A (fr) | 2022-04-06 |
| AU2020266529A1 (en) | 2021-12-16 |
| EP3962901A1 (en) | 2022-03-09 |
| ECSP21080966A (es) | 2022-01-31 |
| WO2020223255A1 (en) | 2020-11-05 |
| TW202106669A (zh) | 2021-02-16 |
| CN114072393A (zh) | 2022-02-18 |
| JOP20210275A1 (ar) | 2023-01-30 |
| KR20220012244A (ko) | 2022-02-03 |
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