PE20190624A1 - 3-metil pirazinas 2,5-disustituidas y 3-metil pirazinas 2,5,6-trisustituidas como inhibidores alostericos de shp2 - Google Patents

3-metil pirazinas 2,5-disustituidas y 3-metil pirazinas 2,5,6-trisustituidas como inhibidores alostericos de shp2

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Publication number
PE20190624A1
PE20190624A1 PE2019000035A PE2019000035A PE20190624A1 PE 20190624 A1 PE20190624 A1 PE 20190624A1 PE 2019000035 A PE2019000035 A PE 2019000035A PE 2019000035 A PE2019000035 A PE 2019000035A PE 20190624 A1 PE20190624 A1 PE 20190624A1
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PE
Peru
Prior art keywords
pirazinas
metil
rent
trisustituidas
shp2
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PE2019000035A
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English (en)
Inventor
Ashutosh Jogalekar
Walter Won
Elena S Koltun
Adrian Gill
Kevin Mellem
Naing Aay
Andreas Buckl
Christopher Semko
Gert Kiss
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Revolution Medicines Inc
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Publication of PE20190624A1 publication Critical patent/PE20190624A1/es

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    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
    • C07D241/20—Nitrogen atoms
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
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    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
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    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
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    • 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
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    • 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
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    • C07D477/26—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hetero atoms or carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 4
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    • C07D491/04—Ortho-condensed systems
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    • 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
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Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE 3-METIL-PIRAZINAS 2,5-DISUSTITUIDAS Y 3-METIL-PIRAZINAS 2,5,6-TRISUSTITUIDAS DE FORMULA (I-W) DONDE A ES CICLOALQUILO, HETEROCICLOALQUILO, ARILO O HETEROARILO; Y1 ES -S-, UN ENLACE DIRECTO, -NH-, -S(O)2-, ENTRE OTROS; Y2 ES -C(O)-, -C(O)O-, -OC(O)-, ENTRE OTROS; R1 ES -H, -ALQUILO C1-C6, -ALQUENILO C2-C6, ENTRE OTROS; R2 ES -OH, -CN, -ALQUILO C1-C6, ENTRE OTROS; R3 ES -H, -ALQUILO C1-C6, UN ESPIROHETEROCICLO DE 5 A 12 MIEMBROS, ENTRE OTROS; R4 ES -H, -ALQUILO C1-C6, -HALOALQUILO C1-C6, ENTRE OTROS; n ES DE 0 A 10. SON COMPUESTOS PREFERIDOS: (R)-8-(5-((2,3-DICLOROFENIL)TIO)-6-FENILPIRAZIN-2-IL)-8-AZASPIRO[4,5]DECAN-1-AMINA; (R)-8-(6-CICLOPROPIL-5-((2,3-DICLOROPIRIDIN-4-IL)TIO)PIRAZIN-2-IL)-8-AZASPIRO[4,5]DECAN-1-AMINA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN LA ACTIVIDAD DE LA PROTEINA TIROSINA FOSFATASA-2 (SHP2) SIENDO UTIL EN EL TRATAMIENTO DEL SINDROME DE NOONAN, SINDROME LEOPARD, LEUCEMIAS MIELOMONOCITICAS JUVENILES
PE2019000035A 2016-07-12 2017-07-11 3-metil pirazinas 2,5-disustituidas y 3-metil pirazinas 2,5,6-trisustituidas como inhibidores alostericos de shp2 PE20190624A1 (es)

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US201662361249P 2016-07-12 2016-07-12
US201762449523P 2017-01-23 2017-01-23

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US (3) US10590090B2 (es)
EP (2) EP4302834A2 (es)
JP (3) JP6916279B2 (es)
KR (2) KR102598895B1 (es)
CN (3) CN116478132A (es)
AU (3) AU2017296289A1 (es)
BR (1) BR112019000494A2 (es)
CA (1) CA3030167A1 (es)
CL (1) CL2019000090A1 (es)
CO (1) CO2019000613A2 (es)
CR (1) CR20190063A (es)
DO (1) DOP2019000005A (es)
EC (1) ECSP19010079A (es)
IL (1) IL264186B1 (es)
MA (1) MA45660A (es)
MX (2) MX2019000548A (es)
PE (1) PE20190624A1 (es)
PH (1) PH12019500056A1 (es)
SG (1) SG11201900157RA (es)
TN (1) TN2019000010A1 (es)
TW (1) TWI806832B (es)
WO (1) WO2018013597A1 (es)

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