PE20160869A1 - Derivados novedosos de amino pirimidina - Google Patents

Derivados novedosos de amino pirimidina

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Publication number
PE20160869A1
PE20160869A1 PE2016000683A PE2016000683A PE20160869A1 PE 20160869 A1 PE20160869 A1 PE 20160869A1 PE 2016000683 A PE2016000683 A PE 2016000683A PE 2016000683 A PE2016000683 A PE 2016000683A PE 20160869 A1 PE20160869 A1 PE 20160869A1
Authority
PE
Peru
Prior art keywords
fluorobenzamide
methylphenyl
cyclopropyl
oxy
fluoro
Prior art date
Application number
PE2016000683A
Other languages
English (en)
Inventor
Daniela Angst
Anna Vulpetti
François Gessier
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.)
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Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20160869A1 publication Critical patent/PE20160869A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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 carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

La presente invencion se refiere a derivados de pirimidina de formula (I), que interactuan con la tirosina quinasa de Bruton (Btk) utiles para tratar trastornos autoinmunes, enfermedades inflamatorias, alergicas, de las vias aereas como asma, enfermedad pulmonar obstructiva cronica, rechazo de trasplantes, cancer, etc. Donde R1, R2, R3, R4, R5, R6 y R7 son entre otros H; R12 es H o alquilo C1-C6, etc.; o R12 y cualquiera de R8, R9, R, R´, R10 o R11 junto con los atomos a los que estan unidos pueden formar un anillo azaciclico de 4, 5, 6 o 7 miembros, tal anillo puede opcionalmente estar sustituido por halogeno, etc.; n es 0 o 1; R13 es alquenilo C2-C6 opcionalmente sustituido por alquilo C1-C6, etc. Son compuestos preferidos: N-(3-(5-((1-Acriloilazetidin-3-il)oxi)-6-aminopirimidin-4-il)-5-fluoro-2-metilfenil)-4-ciclopropil-2-fluorobenzamida; (E)-N-(3-(6-Amino-5-((1 -(but-2-enoil)azetidin-3-il)oxi)pirimidin-4-il)-5-fluoro-2-metilfenil)-4-ciclopropil-2-fluorobenzamida, entre otros.
PE2016000683A 2013-11-29 2014-11-28 Derivados novedosos de amino pirimidina PE20160869A1 (es)

Applications Claiming Priority (1)

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EP13195081 2013-11-29

Publications (1)

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PE20160869A1 true PE20160869A1 (es) 2016-09-08

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US (6) US9512084B2 (es)
EP (4) EP3299368B1 (es)
JP (2) JP6342495B2 (es)
KR (2) KR102421388B1 (es)
CN (2) CN110172056B (es)
AP (1) AP2016009158A0 (es)
AR (1) AR098549A1 (es)
AU (1) AU2014356069B2 (es)
BR (1) BR112016010397B1 (es)
CA (1) CA2926908C (es)
CL (1) CL2016001055A1 (es)
CR (1) CR20160244A (es)
CU (1) CU24384B1 (es)
CY (3) CY1119705T1 (es)
DK (3) DK3074386T3 (es)
EA (1) EA031218B1 (es)
EC (1) ECSP16054826A (es)
ES (3) ES2791525T3 (es)
FI (1) FI3689865T3 (es)
HK (2) HK1223368A1 (es)
HR (3) HRP20230585T1 (es)
HU (3) HUE037588T2 (es)
IL (1) IL244943B (es)
JO (1) JO3314B1 (es)
LT (3) LT3074386T (es)
MA (1) MA39055B1 (es)
MX (1) MX367911B (es)
MY (2) MY191381A (es)
NO (1) NO3074386T3 (es)
NZ (1) NZ718835A (es)
PE (1) PE20160869A1 (es)
PH (1) PH12016500791B1 (es)
PL (3) PL3299368T3 (es)
PT (3) PT3074386T (es)
RS (3) RS64275B1 (es)
SI (3) SI3299368T1 (es)
SV (1) SV2016005206A (es)
TN (1) TN2016000128A1 (es)
TW (1) TWI652261B (es)
UA (1) UA117256C2 (es)
UY (1) UY35858A (es)
WO (1) WO2015079417A1 (es)
ZA (1) ZA201602275B (es)

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