PE20121431A1 - Derivados de pirimidina como inhbidores de la enzima cinasa ptk2 - Google Patents

Derivados de pirimidina como inhbidores de la enzima cinasa ptk2

Info

Publication number
PE20121431A1
PE20121431A1 PE2012000420A PE2012000420A PE20121431A1 PE 20121431 A1 PE20121431 A1 PE 20121431A1 PE 2012000420 A PE2012000420 A PE 2012000420A PE 2012000420 A PE2012000420 A PE 2012000420A PE 20121431 A1 PE20121431 A1 PE 20121431A1
Authority
PE
Peru
Prior art keywords
radical
alkyl
kinase enzyme
inhbidors
compounds
Prior art date
Application number
PE2012000420A
Other languages
English (en)
Inventor
Heinz Stadtmueller
Ioannis Sapountzis
Original Assignee
Boehringer Ingelheim Int
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43048878&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20121431(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of PE20121431A1 publication Critical patent/PE20121431A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D401/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE PIRIMIDINAS DE FORMULA (1a) Y (1b) DONDE: A ES UN RADICAL, OPCIONALMENTE SUSTITUIDO CON UNO O VARIOS R2, IGUALES O DIFERENTES, SELECCIONADO ENTRE CICLOALQUILO C3-10, HETEROCICLOALQUILO C3-8, ARILO C6-15 Y HETEROARILO C5-12; Q ES UN RADICAL, OPCIONALMENTE SUSTITUIDO CON UNO O VARIOS R4, IGUALES O DIFERENTES, SELECCIONADO ENTRE FENILO Y HETEROARILO C5-6; R1 ES ALQUILO C1-3, -CF3, -NO , ENTRE OTROS; R2, R4 Y R5 SON INDEPENDIENTEMENTE H O UN RADICAL SELECCIONADO ENTRE Ra, Rb, ENTRE OTROS; R3 ES -OS(O)Rc, -OS(O)NRcRc, -SC(O)Rc, ENTRE OTROS; Ra ES INDEPENDIENTEMENTE ALQUILO C1-6, ARILO C6-10, ENTRE OTROS; Rb ES UN RADICAL SELECCIONADO ENTRE =O, -ORc, ENTRE OTROS; Rc ES H O UN RADICAL SELECCIONADO ENTRE ALQUILO C1-6, ARILO C6-10, ENTRE OTROS; m, n, p Y q SON UN ENTERO ENTRE 0 Y 3. SON COMPUESTOS PREFERIDOS: 4-[4-((1R,2R)-1-METANSULFONILAMINO-INDAN-2-ILOXI)-5-TRIFLUOROMETIL-PIRIMIDIN-2-ILAMINO]-3-METOXI-N-(1-METIL-PIPERIDIN-4-IL)-BENZAMIDA; N-((1R,2R)-2-{2-[4-(4-TERC-BUTIL-PIPERAZIN-1-IL)-2-METOXI-FENILAMINO]-5-TRIFLUOROMETIL-PIRIMIDIN-4-ILOXI}-INDAN-1-IL)-N-METIL-METANSULFONAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ENZIMA CINASA PTK2, SIENDO UTILES PARA EL TRATAMIENTO DE ENFERMEDADES CARACTERIZADAS POR UNA PROLIFERACION CELULAR EXCESIVA O ANORMAL
PE2012000420A 2009-10-02 2010-10-01 Derivados de pirimidina como inhbidores de la enzima cinasa ptk2 PE20121431A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09172026 2009-10-02
EP10172460 2010-08-11

Publications (1)

Publication Number Publication Date
PE20121431A1 true PE20121431A1 (es) 2012-11-10

Family

ID=43048878

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012000420A PE20121431A1 (es) 2009-10-02 2010-10-01 Derivados de pirimidina como inhbidores de la enzima cinasa ptk2

Country Status (24)

Country Link
US (1) US8466155B2 (es)
EP (1) EP2483249B1 (es)
JP (1) JP5702390B2 (es)
KR (1) KR20120092617A (es)
CN (1) CN102695700A (es)
AP (1) AP2012006166A0 (es)
AR (1) AR078513A1 (es)
AU (1) AU2010302648A1 (es)
BR (1) BR112012007300A2 (es)
CA (1) CA2775418A1 (es)
CL (1) CL2012000825A1 (es)
EA (1) EA201200552A1 (es)
EC (1) ECSP12011830A (es)
IL (1) IL218543A0 (es)
IN (1) IN2012DN02714A (es)
MA (1) MA33606B1 (es)
MX (1) MX2012003101A (es)
NZ (1) NZ598614A (es)
PE (1) PE20121431A1 (es)
TN (1) TN2012000142A1 (es)
TW (1) TW201124386A (es)
UY (1) UY32916A (es)
WO (1) WO2011039344A1 (es)
ZA (1) ZA201201703B (es)

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US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
AU2012216894B2 (en) 2011-02-17 2016-07-14 Cancer Therapeutics Crc Pty Limited Selective FAK inhibitors
AU2012216893B2 (en) 2011-02-17 2016-08-11 Cancer Therapeutics Crc Pty Limited FAK inhibitors
WO2013086260A2 (en) * 2011-12-09 2013-06-13 Oncomed Pharmaceuticals, Inc. Combination therapy for treatment of cancer
US9187453B2 (en) 2012-03-28 2015-11-17 Takeda Pharmaceutical Company Limited Heterocyclic compound
UA117347C2 (uk) 2012-06-13 2018-07-25 Інсайт Холдинґс Корпорейшн Заміщені трициклічні сполуки як інгібітори fgfr
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
CN105263931B (zh) 2013-04-19 2019-01-25 因赛特公司 作为fgfr抑制剂的双环杂环
WO2014190207A1 (en) * 2013-05-22 2014-11-27 The Regents Of The University Of California Aurora kinase inhibitors
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
UA121669C2 (uk) 2015-02-20 2020-07-10 Інсайт Корпорейшн Біциклічні гетероцикли як інгібітори fgfr
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
MA52493A (fr) 2018-05-04 2021-03-10 Incyte Corp Sels d'un inhibiteur de fgfr
SG11202010636VA (en) 2018-05-04 2020-11-27 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
PE20221085A1 (es) 2019-10-14 2022-07-05 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN115151539A (zh) 2019-12-04 2022-10-04 因赛特公司 Fgfr抑制剂的衍生物
WO2021113479A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors

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Also Published As

Publication number Publication date
EP2483249A1 (en) 2012-08-08
AP2012006166A0 (en) 2012-04-30
ECSP12011830A (es) 2012-06-29
AU2010302648A1 (en) 2012-04-05
CL2012000825A1 (es) 2012-08-24
IL218543A0 (en) 2012-05-31
WO2011039344A1 (en) 2011-04-07
UY32916A (es) 2011-04-29
CA2775418A1 (en) 2011-04-07
IN2012DN02714A (es) 2015-09-11
MA33606B1 (fr) 2012-09-01
MX2012003101A (es) 2012-04-11
BR112012007300A2 (pt) 2017-11-07
NZ598614A (en) 2013-08-30
TN2012000142A1 (en) 2013-09-19
JP5702390B2 (ja) 2015-04-15
US8466155B2 (en) 2013-06-18
AR078513A1 (es) 2011-11-16
ZA201201703B (en) 2014-05-28
US20110237598A1 (en) 2011-09-29
EA201200552A1 (ru) 2013-03-29
CN102695700A (zh) 2012-09-26
KR20120092617A (ko) 2012-08-21
JP2013506636A (ja) 2013-02-28
TW201124386A (en) 2011-07-16
EP2483249B1 (en) 2015-12-23

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