PE20231079A1 - Metil (r)-2-(fluorometil)-5-oxo-4-fenil-4,5,6,7-tetrahidro-1h-ciclopenta[b]piridin-3-carboxilato y metil (r)-2-(fluorometil)-5-oxo-4-fenil-1,4,5,7-tetrahidrofuro[3,4- b]piridin-3-carboxilato como activadores de cav1.2 - Google Patents

Metil (r)-2-(fluorometil)-5-oxo-4-fenil-4,5,6,7-tetrahidro-1h-ciclopenta[b]piridin-3-carboxilato y metil (r)-2-(fluorometil)-5-oxo-4-fenil-1,4,5,7-tetrahidrofuro[3,4- b]piridin-3-carboxilato como activadores de cav1.2

Info

Publication number
PE20231079A1
PE20231079A1 PE2022002898A PE2022002898A PE20231079A1 PE 20231079 A1 PE20231079 A1 PE 20231079A1 PE 2022002898 A PE2022002898 A PE 2022002898A PE 2022002898 A PE2022002898 A PE 2022002898A PE 20231079 A1 PE20231079 A1 PE 20231079A1
Authority
PE
Peru
Prior art keywords
methyl
carboxylate
oxo
pyridine
phenyl
Prior art date
Application number
PE2022002898A
Other languages
English (en)
Inventor
Sung David C Kim
Zaixing Li
Chui Lu
Danuta Lubicka
James Neef
Hye-Yeon Park
Tejaskumar Pankajbhai Pathak
Amir Masoud Sadaghiani
Xilin Zhou
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of PE20231079A1 publication Critical patent/PE20231079A1/es

Links

Classifications

    • 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
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed 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
    • A61K31/435—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
    • A61K31/4355—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 oxygen as a ring hetero 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
    • A61K31/435—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
    • A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • 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)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Refiere a un compuesto de la formula (I), o una sal farmaceuticamente aceptable del mismo, los cuales son activadores de CaV1.22; en donde A es O o CH2, R1 y R2 son H o F, R3 es OCHF2, CHF2, CF3, metilo, etilo o ciclopropilo opcionalmente sustituidos con 1 a 3 F. Dicho compuesto es metil 2-(difluorometil)-4-(3-fluoro-2-(1-fluoroetil)fenil)-5-oxo-1,4,5,7-tetrahidrofuro[3,4-b]piridin-3-carboxilato, o una sal farmaceuticamente aceptable o solvato de este. Asimismo, refiere a formas cristalinas y a una composicion farmaceutica a base de dicho compuesto junto a un excipiente farmaceuticamente aceptable, para el tratamiento del sindrome de Brugada, sindrome de Phelan-McDermid y enfermedad de Alzheimer.
PE2022002898A 2020-06-15 2021-06-11 Metil (r)-2-(fluorometil)-5-oxo-4-fenil-4,5,6,7-tetrahidro-1h-ciclopenta[b]piridin-3-carboxilato y metil (r)-2-(fluorometil)-5-oxo-4-fenil-1,4,5,7-tetrahidrofuro[3,4- b]piridin-3-carboxilato como activadores de cav1.2 PE20231079A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
PCT/CN2020/096177 WO2021253180A1 (en) 2020-06-15 2020-06-15 Methyl (r) -2- (fluoromethyl) -5-oxo-4-phenyl-4, 5, 6, 7-tetrahydro-1h-cyclopenta [b] pyridine-3-carboxylate and methyl (r) -2- (fluoromethyl) -5-oxo-4-phenyl-1, 4, 5, 7-tetrahydrofuro [3, 4-b] pyridine-3-carboxylate as cav1.2 activators
PCT/IB2021/055183 WO2021255607A1 (en) 2020-06-15 2021-06-11 Methyl 2-(fluoromethyl)-5-oxo-4-phenyl-4,5,6,7-tetrahydro-1h-cyclopenta[b]pyridine-3-carboxylates and methyl 2-(fluoromethyl)-5-oxo-4-phenyl-1,4,5,7-tetrahydrofuro[3,4-b]pyridine-3-carboxylates as cav1.2 activators

Publications (1)

Publication Number Publication Date
PE20231079A1 true PE20231079A1 (es) 2023-07-17

Family

ID=76523252

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022002898A PE20231079A1 (es) 2020-06-15 2021-06-11 Metil (r)-2-(fluorometil)-5-oxo-4-fenil-4,5,6,7-tetrahidro-1h-ciclopenta[b]piridin-3-carboxilato y metil (r)-2-(fluorometil)-5-oxo-4-fenil-1,4,5,7-tetrahidrofuro[3,4- b]piridin-3-carboxilato como activadores de cav1.2

Country Status (20)

Country Link
US (1) US11919911B2 (es)
EP (1) EP4165047A1 (es)
JP (1) JP2023530917A (es)
KR (1) KR20230022982A (es)
CN (1) CN115836076A (es)
AR (1) AR122615A1 (es)
AU (1) AU2021293976B2 (es)
BR (1) BR112022025212A2 (es)
CA (1) CA3182354A1 (es)
CL (1) CL2022003525A1 (es)
CO (1) CO2022017502A2 (es)
CR (1) CR20230008A (es)
DO (1) DOP2022000276A (es)
EC (1) ECSP23001748A (es)
IL (1) IL298448A (es)
MX (1) MX2022015866A (es)
PE (1) PE20231079A1 (es)
TW (1) TW202214651A (es)
UY (1) UY39265A (es)
WO (2) WO2021253180A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10004596B2 (en) 2014-07-31 2018-06-26 Lensgen, Inc. Accommodating intraocular lens device
WO2023111799A1 (en) * 2021-12-13 2023-06-22 Novartis Ag PYRIDINE-3-CARBOXYLATE COMPOUNDS AS CaV1.2 ACTIVATORS

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ201395A (en) 1981-07-30 1987-02-20 Bayer Ag Pharmaceutical compositions containing 1,4-dihydropyridines and certain of these dihydropyridines
EP0111455A3 (de) 1982-12-10 1984-07-25 Ciba-Geigy Ag Ungesättigte Lactone
DE3410645A1 (de) 1984-03-23 1985-09-26 Bayer Ag, 5090 Leverkusen L-alkylsubstituierte 1,4-dihydropyridinlactone, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln
US4567268A (en) 1984-04-03 1986-01-28 Merck & Co., Inc. Process for preparation of certain tetrahydrofuro[3,4-b]pyridines
US6518279B2 (en) * 1999-03-04 2003-02-11 Abbott Laboratories Cyclopentanone dihydropyridine compounds useful as potassium channel openers
EP1631260A2 (en) 2003-02-28 2006-03-08 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
WO2010015037A1 (en) 2008-08-08 2010-02-11 Howard Florey Institute Therapeutic methods and compositions

Also Published As

Publication number Publication date
AU2021293976A1 (en) 2022-11-24
ECSP23001748A (es) 2023-03-31
WO2021253180A1 (en) 2021-12-23
AU2021293976B2 (en) 2023-12-14
KR20230022982A (ko) 2023-02-16
MX2022015866A (es) 2023-01-24
BR112022025212A2 (pt) 2023-01-03
CN115836076A (zh) 2023-03-21
JP2023530917A (ja) 2023-07-20
US11919911B2 (en) 2024-03-05
DOP2022000276A (es) 2023-01-15
CO2022017502A2 (es) 2022-12-20
US20210395261A1 (en) 2021-12-23
IL298448A (en) 2023-01-01
EP4165047A1 (en) 2023-04-19
CA3182354A1 (en) 2021-12-23
WO2021255607A1 (en) 2021-12-23
CL2022003525A1 (es) 2023-08-11
UY39265A (es) 2022-01-31
AR122615A1 (es) 2022-09-21
TW202214651A (zh) 2022-04-16
CR20230008A (es) 2023-01-25

Similar Documents

Publication Publication Date Title
PE20231079A1 (es) Metil (r)-2-(fluorometil)-5-oxo-4-fenil-4,5,6,7-tetrahidro-1h-ciclopenta[b]piridin-3-carboxilato y metil (r)-2-(fluorometil)-5-oxo-4-fenil-1,4,5,7-tetrahidrofuro[3,4- b]piridin-3-carboxilato como activadores de cav1.2
PE20231081A1 (es) Derivados de quinoxalina como farmacos contra el cancer
PE20212304A1 (es) Inhibidores de il-17a imidazo[1,2-b]piridazin-2-il
HRP20180444T1 (hr) 9-aminometil-supstituirani tetraciklinski spojevi
PE20170705A1 (es) Nuevos compuestos como inhibidores de ret (reorganizado durante la transfeccion)
PE20141700A1 (es) Compuestos de 2-(2,4,5-anilino sustituido) pirimidina
PE20191245A1 (es) Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de quinasa pim
PE20181093A1 (es) Compuestos heterociclicos y usos de los mismos
HRP20210847T1 (hr) Supstituirani derivati indola kao inhibitori replikacije denga virusa
PE20161369A1 (es) Inhibidores de monoacilglicerol aciltransferasa 2 (mgat2) de dihidropiridinona sustituidos con tetrazolona
PE20170465A1 (es) Agentes inductores de apoptosis para el tratamiento del cancer y de enfermedades inmunes y autoinmunes
EP2581376A4 (en) MATRIC ACID / MATRIN DERIVATIVES AND MANUFACTURING METHOD AND USES THEREOF
ES2655391T3 (es) Inhibidores isoindolinona de fosfatidilinositol 3-quinasa
PE20141351A1 (es) Triazolopiridinas
AR054560A1 (es) Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer
AR056103A1 (es) Compuestos de(piran-piperidinil)benzimidazol, composiciones farmaceuticas que los comprenden, proceso de preparacion y usos en el tratamiento de afecciones mediadas por agonistas del receptor muscarinico m1
RU2013116924A (ru) N1/n2-лактамные ингибиторы ацетил-коа-карбоксилаз
AR104963A1 (es) Derivados de 2-(pirazolopiridin-3-il)pirimidina como inhibidores de jak
PE20130611A1 (es) Triazolopiridinas sustituidas
CL2019003857A1 (es) Composiciones y métodos de uso de 2-(4-clorofenil)-n-((2-(2,6-dioxopiperidin-3-il)-1-oxoisoindolin-5-il)metil)-2,2-difluoroacetamida solicitudes relacionadas.
PE20231094A1 (es) Composicion que contiene un derivado de arilamida
JP2016503778A5 (es)
AR111494A1 (es) Compuestos de anilinoquinazolina c₅ y su uso en el tratamiento del cáncer
JP2016540803A5 (es)
RU2016131189A (ru) ПРОИЗВОДНЫЕ ПИРРОЛО[3,2-d]ПИРИМИДИНА В КАЧЕСТВЕ ИНДУКТОРОВ ЧЕЛОВЕЧЕСКОГО ИНТЕРФЕРОНА