PE20211649A1 - Nuevos derivados amino-pirimidonil-piperidinilo, un proceso para su preparacion y composiciones farmaceuticas que los contienen - Google Patents

Nuevos derivados amino-pirimidonil-piperidinilo, un proceso para su preparacion y composiciones farmaceuticas que los contienen

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Publication number
PE20211649A1
PE20211649A1 PE2021000517A PE2021000517A PE20211649A1 PE 20211649 A1 PE20211649 A1 PE 20211649A1 PE 2021000517 A PE2021000517 A PE 2021000517A PE 2021000517 A PE2021000517 A PE 2021000517A PE 20211649 A1 PE20211649 A1 PE 20211649A1
Authority
PE
Peru
Prior art keywords
methyl
amino
pyrimidonil
carbonyl
preparation
Prior art date
Application number
PE2021000517A
Other languages
English (en)
Inventor
Csaba Weber
Andras Kotschy
Attila Vasas
Arpad Kiss
Balazs Molnar
Andrea Fiumana
Alba Macias
James Brooke Murray
Didier Demarles
Lisa Ivanschitz
Olivier Geneste
Kristof Hegedus
Peter Spranitz
Tibor Soos
Original Assignee
Servier Lab
Vernalis Randd Ltd
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 Servier Lab, Vernalis Randd Ltd filed Critical Servier Lab
Publication of PE20211649A1 publication Critical patent/PE20211649A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero 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
    • A61K31/495—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
    • A61K31/495—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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero 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
    • C07D417/14—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
    • 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
    • C07B2200/07—Optical isomers

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Esta referida a nuevos derivados amino-pirimidonil-piperidinilo de Formula I, en donde: Q es O, S; R1 es cicloalquilo, heterocicloalquilo, arilo, heteroarilo; R2 es arilo, heteroarilo; R3 es H, alquilo, halo alquilo, entre otros; R4 es H, halogeno; R5 es H, alquilo, haloalquilo, arilalquilo; n es 0, 1, 2. Entre los compuestos preferidos tenemos los siguientes: 5-amino-3-{[(4S)-3,3-difluoro-4-hidroxi-1-{(3R,4R)-1-[(2-metilpirimidin-4- il)metil]-3-fenilpiperidina-4-carbonil}piperidin-4-il]metil}-6-(4- fluorofenoxi)pirimidin-4(3H)-ona; 5-amino-6-(4-cloro-3-fluorofenoxi)-3-[(4-hidroxi-1-{(3R,4R)-1-[4-metil-2-(6- 15 metilpiridin-3-il)-1,3-tiazol-5-carbonil]-3-fenilpiperidina-4-carbonil}piperidin-4- il)metil]pirimidin-4(3H)-ona; entre otros. Estos compuestos han mostrado propiedades pro-apoptoticas y/o anti-proliferativas y se emplean en el tratamiento de diversos tipos de cancer y de enfermedades inmunes y auto-inmunes.
PE2021000517A 2018-10-19 2019-10-18 Nuevos derivados amino-pirimidonil-piperidinilo, un proceso para su preparacion y composiciones farmaceuticas que los contienen PE20211649A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18306377 2018-10-19
EP19305936 2019-07-12
PCT/EP2019/078318 WO2020079205A1 (en) 2018-10-19 2019-10-18 New amino-pyrimidonyl-piperidinyl derivatives, a process for their preparation and pharmaceutical compositions containing them

Publications (1)

Publication Number Publication Date
PE20211649A1 true PE20211649A1 (es) 2021-08-24

Family

ID=68234009

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2021000517A PE20211649A1 (es) 2018-10-19 2019-10-18 Nuevos derivados amino-pirimidonil-piperidinilo, un proceso para su preparacion y composiciones farmaceuticas que los contienen

Country Status (24)

Country Link
US (1) US20210355106A1 (es)
EP (1) EP3866930A1 (es)
JP (1) JP2022505122A (es)
KR (1) KR20210081371A (es)
CN (1) CN113038990A (es)
AU (1) AU2019360391A1 (es)
BR (1) BR112021006714A2 (es)
CA (1) CA3116089A1 (es)
CL (1) CL2021000973A1 (es)
CO (1) CO2021004553A2 (es)
CR (1) CR20210173A (es)
DO (1) DOP2021000063A (es)
EC (1) ECSP21024078A (es)
IL (1) IL282218A (es)
JO (1) JOP20210063A1 (es)
MA (1) MA53900A (es)
MX (1) MX2021004379A (es)
NI (1) NI202100024A (es)
PE (1) PE20211649A1 (es)
PH (1) PH12021550788A1 (es)
SG (1) SG11202103279RA (es)
TW (1) TW202028188A (es)
UY (1) UY38423A (es)
WO (1) WO2020079205A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021123051A1 (en) 2019-12-20 2021-06-24 Bayer Aktiengesellschaft Substituted thiophene carboxamides, thiophene carboxylic acids and derivatives thereof
CN114507163A (zh) * 2020-11-16 2022-05-17 尚科生物医药（上海）有限公司 一种制备2-氟-5-甲氧基苯磺酰氯的方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR3052452B1 (fr) * 2016-06-10 2018-06-22 Les Laboratoires Servier Nouveaux derives de piperidinyle, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
RU2742271C2 (ru) * 2016-06-10 2021-02-04 Ле Лаборатуар Сервье Новые (гетеро)арил-замещенные пиперидинильные производные, способ их получения и фармацевтические композиции, содержащие их
GB201617758D0 (en) * 2016-10-20 2016-12-07 Almac Discovery Limited Pharmaceutical compounds

Also Published As

Publication number Publication date
JP2022505122A (ja) 2022-01-14
BR112021006714A2 (pt) 2021-07-27
TW202028188A (zh) 2020-08-01
WO2020079205A1 (en) 2020-04-23
IL282218A (en) 2021-05-31
CR20210173A (es) 2021-05-11
JOP20210063A1 (ar) 2023-01-30
MA53900A (fr) 2022-01-26
DOP2021000063A (es) 2021-08-31
CO2021004553A2 (es) 2021-04-30
CN113038990A (zh) 2021-06-25
EP3866930A1 (en) 2021-08-25
US20210355106A1 (en) 2021-11-18
ECSP21024078A (es) 2021-05-31
KR20210081371A (ko) 2021-07-01
PH12021550788A1 (en) 2021-10-18
UY38423A (es) 2021-02-26
SG11202103279RA (en) 2021-04-29
MX2021004379A (es) 2021-06-04
CA3116089A1 (en) 2020-04-23
AU2019360391A1 (en) 2021-05-13
CL2021000973A1 (es) 2021-11-19
NI202100024A (es) 2021-08-24

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