PE20230106A1 - Compuestos de pirimidina fusionados como moduladores de kcc2 - Google Patents

Compuestos de pirimidina fusionados como moduladores de kcc2

Info

Publication number
PE20230106A1
PE20230106A1 PE2022001943A PE2022001943A PE20230106A1 PE 20230106 A1 PE20230106 A1 PE 20230106A1 PE 2022001943 A PE2022001943 A PE 2022001943A PE 2022001943 A PE2022001943 A PE 2022001943A PE 20230106 A1 PE20230106 A1 PE 20230106A1
Authority
PE
Peru
Prior art keywords
kcc2
modulators
propan
pyrimidine
compounds
Prior art date
Application number
PE2022001943A
Other languages
English (en)
Inventor
Rebecca Elizabeth Jarvis
Roland Werner Burli
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of PE20230106A1 publication Critical patent/PE20230106A1/es

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Classifications

    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • 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
    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/541—Non-condensed thiazines containing further 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • 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
    • 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
    • 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
    • C07D491/04—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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems
    • 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)
  • 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

SE REFIERE A COMPUESTOS DE PIRIMIDINA FUSIONADOS DE FORMULA (I) DONDE R1, R2, R7 Y EL ANILLO A SON TAL COMO SE DESCRIBEN EN EL PRESENTE DOCUMENTO. SON COMPUESTOS PREFERIDOS: 2-(DIETILAMINO)-6-(PROPAN-2-IL)-4-{[4-(PROPAN-2-IL)FENIL]AMINO}-5,6-DIHIDRO-7H-PIRROLO[3,4-D]PIRIMIDIN-7-ONA; 4-[(4-CICLOHEXILFENIL)AMINO]-2-(2-CICLOPROPILMORFOLIN-4-IL)-6-(PROPAN-2-IL)-5,6-DIHIDRO-7H-PIRROLO[3,4-D]PIRIMIDIN-7-ONA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DEL TRANSPORTADOR DE MEMBRANA ELECTRONEUTRO KCC2 SIENDO UTILES EN EL TRATAMIENTO DE EPILEPSIA, DOLOR, TRASTORNOS EL ESPECTRO AUTISTA, COGNICION, ANSIEDAD Y ESCLEROSIS LATERAL AMIOTROFICA.
PE2022001943A 2020-03-13 2021-03-12 Compuestos de pirimidina fusionados como moduladores de kcc2 PE20230106A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202062989104P 2020-03-13 2020-03-13
PCT/EP2021/056393 WO2021180952A1 (en) 2020-03-13 2021-03-12 Fused pyrimidine compounds as kcc2

Publications (1)

Publication Number Publication Date
PE20230106A1 true PE20230106A1 (es) 2023-01-25

Family

ID=74874882

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022001943A PE20230106A1 (es) 2020-03-13 2021-03-12 Compuestos de pirimidina fusionados como moduladores de kcc2

Country Status (24)

Country Link
US (1) US20230151013A1 (es)
EP (1) EP4103566B1 (es)
JP (1) JP2023517680A (es)
KR (1) KR20220152319A (es)
CN (1) CN115298182A (es)
AU (1) AU2021234134A1 (es)
BR (1) BR112022018173A2 (es)
CA (1) CA3171192A1 (es)
CL (1) CL2022002386A1 (es)
CO (1) CO2022012884A2 (es)
DK (1) DK4103566T3 (es)
ES (1) ES2962136T3 (es)
FI (1) FI4103566T3 (es)
HR (1) HRP20231314T1 (es)
HU (1) HUE064037T2 (es)
IL (1) IL296265A (es)
LT (1) LT4103566T (es)
MX (1) MX2022011354A (es)
PE (1) PE20230106A1 (es)
PL (1) PL4103566T3 (es)
PT (1) PT4103566T (es)
RS (1) RS64823B1 (es)
SI (1) SI4103566T1 (es)
WO (1) WO2021180952A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3240377A1 (en) * 2021-12-08 2023-06-15 Gnanasambandam Kumaravel Bicyclic heteroarenes and methods of their use
CN117843618A (zh) * 2022-08-29 2024-04-09 北京沐华生物科技有限责任公司 一种ep300/cbp调节剂及其制备方法和用途

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090099195A1 (en) * 2007-05-08 2009-04-16 Astrazeneca Ab Therapeutic Compounds 570
EP3110820B1 (en) * 2014-02-28 2022-04-06 Nimbus Lakshmi, Inc. Tyk2 inhibitors and uses thereof
US11331313B2 (en) * 2017-05-22 2022-05-17 Whitehead Institute For Biomedical Research KCC2 expression enhancing compounds and uses thereof
CN112752573A (zh) * 2018-05-25 2021-05-04 儿童医疗中心有限公司 治疗脊髓损伤的方法

Also Published As

Publication number Publication date
CN115298182A (zh) 2022-11-04
FI4103566T3 (fi) 2023-10-20
PT4103566T (pt) 2023-11-09
US20230151013A1 (en) 2023-05-18
WO2021180952A1 (en) 2021-09-16
JP2023517680A (ja) 2023-04-26
ES2962136T3 (es) 2024-03-15
CA3171192A1 (en) 2021-09-16
HUE064037T2 (hu) 2024-03-28
CO2022012884A2 (es) 2022-10-11
BR112022018173A2 (pt) 2022-10-25
KR20220152319A (ko) 2022-11-15
AU2021234134A1 (en) 2022-11-03
EP4103566A1 (en) 2022-12-21
CL2022002386A1 (es) 2023-04-28
HRP20231314T1 (hr) 2024-02-16
SI4103566T1 (sl) 2024-04-30
WO2021180952A9 (en) 2021-12-16
PL4103566T3 (pl) 2024-02-05
MX2022011354A (es) 2022-11-30
DK4103566T3 (da) 2023-10-30
RS64823B1 (sr) 2023-12-29
EP4103566B1 (en) 2023-10-04
IL296265A (en) 2022-11-01
LT4103566T (lt) 2023-11-10

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