PE20220425A1 - Derivado de 1,1-dioxido de 3-amino-4h-benzo[e][1,2,4]tiadiazina como inhibidores de mrgx2 - Google Patents

Derivado de 1,1-dioxido de 3-amino-4h-benzo[e][1,2,4]tiadiazina como inhibidores de mrgx2

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Publication number
PE20220425A1
PE20220425A1 PE2021001772A PE2021001772A PE20220425A1 PE 20220425 A1 PE20220425 A1 PE 20220425A1 PE 2021001772 A PE2021001772 A PE 2021001772A PE 2021001772 A PE2021001772 A PE 2021001772A PE 20220425 A1 PE20220425 A1 PE 20220425A1
Authority
PE
Peru
Prior art keywords
thiadiazine
benzo
amino
mrgx2
inhibitors
Prior art date
Application number
PE2021001772A
Other languages
English (en)
Inventor
Simone Bigi
Allison L Chambers
Tony Gibson
Jason Pickens
Steve Swann
Angie Vassar
Feng Zhou
Mitsunori Kono
Masaki Seto
Zenyu Shiokawa
Original Assignee
Solent Therapeutics Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Solent Therapeutics Llc filed Critical Solent Therapeutics Llc
Publication of PE20220425A1 publication Critical patent/PE20220425A1/es

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    • 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

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  • 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

Esta referido a compuestos derivados de 1,1-dioxido de 3-amino-5-metil-4H-benzo[e][1,2,4] tiadiazina de Formula I, en donde: L es un enlace o alcanodiilo de C1-4; R1 es alquilo, grupo ciclico, cualquiera de ellos opcionalmente sustituido; R2 es alquilo, grupo ciclico, cualquiera de ellos opcionalmente sustituido; R3, R4 y R5 son H, halo, CN, alquilo. Entre los compuestos preferidos tenemos los siguientes: 1,1-dioxido de 5-(2-cloro-3-fluorofenil)-3-(metilamino)-4H-benzo[e][1,2,4] tiadiazina; 1,1-dioxido de 5-(2-cloro-3-fluorofenil)-3-((2-metoxietil)amino)-4H-benzo[e][1,2,4] tiadiazina; entre otros. Estos compuestos son inhibidores de gen X2 relacionado con Mas (MRGX2) y se emplean en el tratamiento de enfermedades, trastornos o afecciones asociadas con MRGX, incluyendo dermatitis atopica, urticaria cronica y asma, entre otras
PE2021001772A 2019-04-29 2020-04-28 Derivado de 1,1-dioxido de 3-amino-4h-benzo[e][1,2,4]tiadiazina como inhibidores de mrgx2 PE20220425A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962840344P 2019-04-29 2019-04-29
PCT/US2020/030305 WO2020223255A1 (en) 2019-04-29 2020-04-28 3-amino-4h-benzo[e][1,2,4]thiadiazine 1,1-dioxide derivatives as inhibitors of mrgx2

Publications (1)

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PE20220425A1 true PE20220425A1 (es) 2022-03-29

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PE2021001772A PE20220425A1 (es) 2019-04-29 2020-04-28 Derivado de 1,1-dioxido de 3-amino-4h-benzo[e][1,2,4]tiadiazina como inhibidores de mrgx2

Country Status (22)

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)
TW (1) TW202106669A (es)
WO (1) WO2020223255A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI782504B (zh) * 2020-05-08 2022-11-01 美商美國禮來大藥廠 (三氟甲基)嘧啶-2-胺化合物
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

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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
EP1865963A2 (en) * 2005-02-18 2007-12-19 Acadia Pharmaceuticals Inc. Triazadibenzoazulene compounds useful for the treatment and prevention of pain and screening methods therefor
WO2008052072A2 (en) * 2006-10-24 2008-05-02 Acadia Pharmaceuticals Inc. Compounds for the treatment of pain and screening methods therefor

Also Published As

Publication number Publication date
CA3137584A1 (en) 2020-11-05
EP3962901A1 (en) 2022-03-09
MA55804A (fr) 2022-04-06
TW202106669A (zh) 2021-02-16
AR119728A1 (es) 2022-01-05
BR112021021508A2 (pt) 2022-03-22
KR20220012244A (ko) 2022-02-03
CL2021002805A1 (es) 2022-07-22
WO2020223255A1 (en) 2020-11-05
CO2021014155A2 (es) 2021-10-29
ECSP21080966A (es) 2022-01-31
CR20210544A (es) 2022-03-30
CN114072393A (zh) 2022-02-18
JOP20210275A1 (ar) 2023-01-30
IL287521A (en) 2021-12-01
US20220119361A1 (en) 2022-04-21
JP2022535672A (ja) 2022-08-10
SG11202111717XA (en) 2021-11-29
MX2021013135A (es) 2021-11-25
DOP2021000223A (es) 2022-01-16
AU2020266529A1 (en) 2021-12-16

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