AR092137A2 - Derivados macrociclicos de quinazolina utiles como agentes antiproliferativos - Google Patents

Derivados macrociclicos de quinazolina utiles como agentes antiproliferativos

Info

Publication number
AR092137A2
AR092137A2 ARP130102897A ARP130102897A AR092137A2 AR 092137 A2 AR092137 A2 AR 092137A2 AR P130102897 A ARP130102897 A AR P130102897A AR P130102897 A ARP130102897 A AR P130102897A AR 092137 A2 AR092137 A2 AR 092137A2
Authority
AR
Argentina
Prior art keywords
alkyl
amino
hydroxy
optionally substituted
mono
Prior art date
Application number
ARP130102897A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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=33493782&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR092137(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR092137A2 publication Critical patent/AR092137A2/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/06—Peri-condensed systems
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
    • C07C229/16—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/40—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • 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
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/93—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms

Abstract

Reivindicación 1: Un compuesto que tiene la fórmula (1), las formas N-óxido, las sales de adición farmacéuticamente aceptables y las formas estereoquímicamente isómeras del mismo, caracterizado porque Z representa O, CH₂, NH o S; Y representa -alquilo C₃₋₉-, -alquenilo C₃₋₉-, -alquinilo C₃₋₉-, -alquil C₃₋₇-CO-NH- opcionalmente sustituido con amino, mono- o di(alquil C₁₋₄)amino o alquil C₁₋₄oxicarbonilamino-, -alquenil C₃₋₇-CO-NH- opcionalmente sustituido con amino, mono- o di(alquil C₁₋₄)amino o alquil C₁₋₄oxicarbonilamino-, -alquinil C₃₋₇-CO-NH- opcionalmente sustituido con amino, mono- o di(alquil C₁₋₄)amino o alquil C₁₋₄oxicarbonilamino-, -alquil C₁₋₅-oxi-alquil C₁₋₅-, -alquil C₁₋₅-NR¹³-alquil C₁₋₅-, -alquil C₁₋₅-NR¹⁴-CO-alquil C₁₋₅-, -alquil C₁₋₅-CO-NR¹⁵-alquil C₁₋₅-, -alquil C₁₋₆-CO-NH-, -alquil C₁₋₆-NH-CO-, -alquil C₁₋₃-NH-CS-Het²⁰-, -alquil C₁₋₃-NH-CO-Het²⁰-, alquil C₁₋₂-CO-Het²¹-CO-, -Het²²-CH₂-CO-NH-alquil C₁₋₃-, -CO-NH-alquil C₁₋₆-, -NH-CO-alquil C₁₋₆-, -CO-alquil C₁₋₇-, -alquil C₁₋₇-CO-, -alquil C₁₋₆-CO-alquil C₁₋₆-, -alquil C₁₋₂-NH-CO-CR¹⁶R¹⁷-NH-, -alquil C₁₋₂-CO-NH-CR¹⁸R¹⁹-CO-, -alquil C₁₋₂-CO-NR²⁰-alquil C₁₋₃-CO-, -alquil C₁₋₂-NR²¹-CH₂-CO-NH-alquil C₁₋₃-, o -NR²²-CO-alquil C₁₋₃-NH-; X¹ representa un enlace directo, O, -O-alquil C₁₋₂-, CO, -CO-alquil C₁₋₂-, NR¹¹, -NR¹¹-alquil C₁₋₂-, -CH₂-, -O-N=CH- o -alquil C₁₋₂-; X² representa un enlace directo, O, -O-alquil C₁₋₂-, CO, -CO-alquil C₁₋₂-, NR¹², -NR¹²-alquil C₁₋₂-, -CH₂-, -O-N=CH- o -alquil C₁₋₂-; R¹ representa hidrógeno, ciano, halo, hidroxi, formilo, alcoxi C₁₋₆-, alquil C₁₋₆-, halo-fenil-carbonilamino-, alcoxi C₁₋₆- sustituido con halo, alquilo C₁₋₄ sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados de hidroxi o halo; R² representa hidrógeno, ciano, halo, hidroxi, hidroxicarbonil-, Het¹⁶-carbonil-, alquil C₁₋₄oxicarbonil-, alquil C₁₋₄carbonil-, aminocarbonil-, mono- o di(alquil C₁₋₄)aminocarbonil-, Het¹, formilo, alquil C₁₋₄-, alquinil C₂₋₆-, cicloalquil C₃₋₆-, cicloalquil C₃₋₆oxi-, alcoxi C₁₋₆-, Ar⁵, Ar¹-oxi-, dihidroxiborano, alcoxi C₁₋₆- sustituido con halo, alquilo C₁₋₄ sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de halo, hidroxi o NR⁵R⁶, alquil C₁₋₄carbonil- en donde dicho alquilo C₁₋₄ está opcionalmente sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de hidroxi o alquil C₁₋₄-oxi-; R³ representa hidrógeno, alquilo C₁₋₄, o alquilo C₁₋₄ sustituido con uno o más sustituyentes seleccionados a partir de halo, alquil C₁₋₄oxi-, amino-, mono- o di(alquil C₁₋₄)amino-, alquil C₁₋₄-sulfonil- o fenilo; R⁴ representa hidrógeno, hidroxi, Ar³-oxi, Ar⁴-alquil C₁₋₄oxi-, alquil C₁₋₄oxi-, alquenil C₂₋₄oxi- opcionalmente sustituido con Het¹² o R⁴ representa alquil C₁₋₄oxi sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de alquil C₁₋₄oxi-, hidroxi, halo, Het²-, -NR⁷R⁸, -carbonil-NR⁹R¹⁰ o Het³-carbonil-; R⁵ y R⁶ están cada uno independientemente seleccionados a partir de hidrógeno o alquilo C₁₋₄; R⁷ y R⁸ están cada uno independientemente seleccionados a partir de hidrógeno, alquilo C₁₋₄, Het⁸, aminosulfonil-, mono- o di(alquil C₁₋₄)-aminosulfonil, hidroxi-alquil C₁₋₄-, alquil C₁₋₄-oxi-alquil C₁₋₄-, hidroxicarbonil-alquil C₁₋₄-, cicloalquil C₃₋₆, Het⁹-carbonil-alquil C₁₋₄-, Het¹⁰-carbonil-, polihidroxi-alquil C₁₋₄-, Het¹¹-alquil C₁₋₄- o Ar²-alquil C₁₋₄-; R⁹ y R¹⁰ están cada uno independientemente seleccionados a partir de hidrógeno, alquilo C₁₋₄, cicloalquilo C₃₋₆, Het⁴, hidroxi-alquil C₁₋₄-, alquil C₁₋₄oxialquil C₁₋₄- o polihidroxi-alquil C₁₋₄-; R¹¹ representa hidrógeno, alquilo C₁₋₄, Het⁵, Het⁶-alquil C₁₋₄-, alquenil C₂₋₄carbonil- opcionalmente sustituido con Het⁷-alquil C₁₋₄aminocarbonil-, alquenil C₂₋₄sulfonil-, alquil C₁₋₄oxialquil C₁₋₄- o fenilo opcionalmente sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de hidrógeno, hidroxi, amino o alquil C₁₋₄oxi-; R¹² representa hidrógeno, alquilo C₁₋₄, alquil C₁₋₄-oxi-carbonil-, Het¹⁸-alquil C₁₋₄-, fenil-alquil C₁₋₄-oxi-carbonil-, Het¹⁷, alquenil C₂₋₄carbonil- opcionalmente sustituido con Het¹⁹-alquil C₁₋₄aminocarbonil-, alquenil C₂₋₄sulfonil-, alquil C₁₋₄oxialquil C₁₋₄- o R¹² representa fenilo opcionalmente sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de hidrógeno, hidroxi, amino o alquil C₁₋₄oxi-; R¹³ representa hidrógeno, alquilo C₁₋₄, Het¹³, Het¹⁴-alquil C₁₋₄- o fenilo opcionalmente sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de hidrógeno, hidroxi, amino o alquil C₁₋₄oxi-; R¹⁴ y R¹⁵ están cada uno independientemente seleccionados a partir de hidrógeno, alquilo C₁₋₄, Het¹⁵-alquil C₁₋₄- o alquil C₁₋₄oxialquil C₁₋₄-; R¹⁶ y R¹⁷ cada uno independientemente representa hidrógeno o alquilo C₁₋₄ opcionalmente sustituido con fenilo, indolilo, metilsulfuro, hidroxi, tiol, hidroxifenilo, aminocarbonilo, hidroxicarbonilo, amina, imidazoilo o guanidino; R¹⁸ y R¹⁹ cada uno independientemente representa hidrógeno o alquilo C₁₋₄ opcionalmente sustituido con fenilo, indolilo, metilsulfuro, hidroxi, tiol, hidroxifenilo, aminocarbonilo, hidroxicarbonilo, amina, imidazoilo o guanidino; R²⁰ y R²² cada uno independientemente representa hidrógeno o alquilo C₁₋₄ opcionalmente sustituido con hidroxi o alquil C₁₋₄oxi; R²¹ representa hidrógeno, alquilo C₁₋₄, Het²³-alquil C₁₋₄carbonil- o R²¹ representa mono- o di(alquil C₁₋₄)amino-alquil C₁₋₄-carbonil- opcionalmente sustituido con hidroxi, pirimidinilo, dimetilamina o alquil C₁₋₄oxi; Het¹ representa un heterociclo seleccionado a partir de piperidinilo, morfolinilo, piperazinilo, furanilo, pirazolilo, dioxolanilo, tiazolilo, oxazolilo, imidazolilo, isoxazolilo, oxadiazolilo, piridinilo o pirrolidinilo en donde dicho Het¹ está opcionalmente sustituido con amino, alquilo C₁₋₄, hidroxi-alquil C₁₋₄, fenilo, fenil-alquil C₁₋₄-, alquil C₁₋₄-oxi-alquil C₁₋₄-, mono- o di(alquil C₁₋₄)amino- o amino-carbonil-; Het² representa un heterociclo seleccionado a partir de morfolinilo, piperazinilo, piperidinilo, pirrolidinilo, tiomorfolinilo o ditianilo en donde dicho Het² está opcionalmente sustituido con uno o cuando sea posible dos o más sustituyentes seleccionados a partir de hidroxi, halo, amino, alquil C₁₋₄-, hidroxi-alquil C₁₋₄-, alquil C₁₋₄-oxi-alquil C₁₋₄-, hidroxi-alquil C₁₋₄-oxi-alquil C₁₋₄-, mono- o di(alquil C₁₋₄)amino-, mono- o di(alquil C₁₋₄)amino-alquil C₁₋₄-, aminoalquil C₁₋₄-, mono- o di(alquil C₁₋₄)amino-sulfonil-, aminosulfonil-; Het³, Het⁴ y Het⁸ cada uno independientemente representa un heterociclo seleccionado a parti
ARP130102897A 2003-05-27 2013-08-15 Derivados macrociclicos de quinazolina utiles como agentes antiproliferativos AR092137A2 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP0305723 2003-05-27
EP0310266 2003-09-15
EP0351061 2003-12-18

Publications (1)

Publication Number Publication Date
AR092137A2 true AR092137A2 (es) 2015-03-25

Family

ID=33493782

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP040101806A AR045687A1 (es) 2003-05-27 2004-05-26 Macrociclos derivados de la quinazolina, procesos de preparacion y composiciones farmaceuticas que los contienen
ARP130102897A AR092137A2 (es) 2003-05-27 2013-08-15 Derivados macrociclicos de quinazolina utiles como agentes antiproliferativos

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP040101806A AR045687A1 (es) 2003-05-27 2004-05-26 Macrociclos derivados de la quinazolina, procesos de preparacion y composiciones farmaceuticas que los contienen

Country Status (32)

Country Link
US (4) US7648975B2 (es)
EP (2) EP2305687A1 (es)
JP (1) JP4887151B2 (es)
KR (1) KR101143878B1 (es)
CN (1) CN102718775B (es)
AR (2) AR045687A1 (es)
AT (1) ATE544454T1 (es)
AU (1) AU2004243487B2 (es)
BR (1) BRPI0410714B8 (es)
CA (1) CA2525214C (es)
CL (1) CL2004001267A1 (es)
CO (1) CO5640038A2 (es)
CY (1) CY1113002T1 (es)
DK (1) DK1633365T3 (es)
EA (1) EA009064B1 (es)
ES (1) ES2381976T3 (es)
HK (1) HK1176350A1 (es)
HR (1) HRP20120351T1 (es)
IL (3) IL172154A0 (es)
IS (1) IS3030B (es)
JO (1) JO2785B1 (es)
MX (1) MXPA05012762A (es)
MY (1) MY148633A (es)
NO (1) NO334209B1 (es)
NZ (1) NZ544154A (es)
PA (1) PA8603801A1 (es)
PL (1) PL1633365T3 (es)
PT (1) PT1633365E (es)
SI (1) SI1633365T1 (es)
TW (3) TWI468372B (es)
UA (1) UA84010C2 (es)
WO (1) WO2004105765A1 (es)

Families Citing this family (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PA8603801A1 (es) 2003-05-27 2004-12-16 Janssen Pharmaceutica Nv Derivados de la quinazolina
US7767670B2 (en) * 2003-11-13 2010-08-03 Ambit Biosciences Corporation Substituted 3-carboxamido isoxazoles as kinase modulators
WO2005058318A1 (en) 2003-12-18 2005-06-30 Janssen Pharmaceutica N.V. 3-cyano-quinoline derivatives with antiproliferative activity
MXPA06007017A (es) 2003-12-18 2006-08-31 Janssen Pharmaceutica Nv Derivados de pirido y pirimidopirimidina como agentes antiproliferativos.
JO3088B1 (ar) * 2004-12-08 2017-03-15 Janssen Pharmaceutica Nv مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف
MY169441A (en) 2004-12-08 2019-04-11 Janssen Pharmaceutica Nv 2,4, (4,6) pyrimidine derivatives
NI200700147A (es) * 2004-12-08 2019-05-10 Janssen Pharmaceutica Nv Derivados de quinazolina inhibidores de cinasas dirigidos a multip
EP1854789B1 (en) 2005-02-23 2013-10-09 Shionogi & Co., Ltd. Quinazoline derivative having tyrosine kinase inhibitory activity
GB0509227D0 (en) * 2005-05-05 2005-06-15 Chroma Therapeutics Ltd Intracellular enzyme inhibitors
CN101341138B (zh) * 2005-06-30 2012-11-14 詹森药业有限公司 作为gsk-3抑制剂的环状苯胺基-吡啶并三嗪类
WO2008006884A2 (en) * 2006-07-13 2008-01-17 Janssen Pharmaceutica N.V. Mtki quinazoline derivatives
JP2009242240A (ja) * 2006-08-04 2009-10-22 Mebiopharm Co Ltd 含ホウ素キナゾリン誘導体
US7977347B2 (en) * 2006-09-11 2011-07-12 Curis, Inc. Quinazoline based EGFR inhibitors
WO2008033749A2 (en) 2006-09-11 2008-03-20 Curis, Inc. Quinazoline based egfr inhibitors containing a zinc binding moiety
US7547781B2 (en) 2006-09-11 2009-06-16 Curis, Inc. Quinazoline based EGFR inhibitors containing a zinc binding moiety
AU2007310845A1 (en) * 2006-10-27 2008-05-02 Janssen Pharmaceutica Nv Use of MTKI 1 for treating or preventing bone cancer
JP2010507384A (ja) * 2006-10-27 2010-03-11 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ キナーゼ阻害剤のプロファイリング方法
BRPI0718061A2 (pt) * 2006-10-27 2013-11-05 Janssen Pharmaceutica Nv Inibidores de vegfr3
KR20090091119A (ko) * 2006-10-27 2009-08-26 얀센 파마슈티카 엔.브이. 뇌암을 치료하거나 예방하기 위한 ｍｔ 키나아제 저해제의 용도
EP2123627B1 (en) * 2007-01-19 2013-11-20 Ube Industries, Ltd. Process for producing aromatic amine having aralkyloxy or heteroaralkyloxy group
US8642067B2 (en) 2007-04-02 2014-02-04 Allergen, Inc. Methods and compositions for intraocular administration to treat ocular conditions
DK2185562T3 (en) 2007-07-27 2016-02-22 Janssen Pharmaceutica Nv PYRROLOPYRIMIDINES SUITABLE FOR TREATING PROLIFERATIVE DISEASES
US8119616B2 (en) 2007-09-10 2012-02-21 Curis, Inc. Formulation of quinazoline based EGFR inhibitors containing a zinc binding moiety
CL2008003384A1 (es) * 2007-11-14 2009-12-11 Enanta Pharm Inc Compuestos derivados de quinoxalina macrocíclica, inhibidores de serina proteasa; composicion farmaceutica que los comprende; y su uso en el tratamiento de la hepatitis c.
US8426430B2 (en) 2008-06-30 2013-04-23 Hutchison Medipharma Enterprises Limited Quinazoline derivatives
CA2738026C (en) 2008-09-22 2017-01-24 Array Biopharma Inc. Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors
DK3106463T6 (da) 2008-10-22 2020-02-24 Array Biopharma Inc Pyrazolo[1,5-]pyrimidinforbindelse som trk-kinasehæmmer
US8765727B2 (en) 2009-01-23 2014-07-01 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
TWI406853B (zh) * 2010-04-07 2013-09-01 Dev Center Biotechnology Ｅｇｆｒ與ｖｅｇｆｒ－２雙重抑制劑及其用途與製法
HUE035337T2 (en) 2010-05-20 2018-05-02 Array Biopharma Inc Macrocyclic compounds as TRK kinase inhibitors
WO2013126015A1 (en) 2012-02-23 2013-08-29 N. V. Nutricia Composition comprising non- digestible oligosaccharides
BR112014022106B1 (pt) * 2012-03-06 2022-08-02 Pfizer Inc Derivados macrocíclicos, combinação, composição e usos na fabricação de um medicamento para o tratamento de doenças
CN104513253A (zh) * 2013-10-01 2015-04-15 南京波尔泰药业科技有限公司 用于治疗增殖性疾病的大环化合物
JP6382997B2 (ja) * 2014-02-07 2018-08-29 エクセセーラ ファーマシューティカルズ インコーポレイテッド 治療用化合物および組成物
MA39822A (fr) 2014-04-03 2018-02-06 Janssen Pharmaceutica Nv Dérivés de pyrimidine bicycle
MA39823A (fr) 2014-04-03 2018-01-09 Janssen Pharmaceutica Nv Dérivés de pyridine macrocyclique
DK3699181T3 (da) 2014-11-16 2023-03-20 Array Biopharma Inc Krystallinsk form af (s)-n-(5-((r)-2-(2,5-difluorphenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamidhydrogensulfat
AU2016333987A1 (en) 2015-10-05 2018-05-10 Ny State Psychiatric Institute Activators of autophagic flux and phospholipase D and clearance of protein aggregates including tau and treatment of proteinopathies
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc Point mutations in trk inhibitor-resistant cancer and methods relating to the same
ES2833959T3 (es) 2016-02-29 2021-06-16 Oncodesign Sa Inhibidor del EGFR macrocíclico radiomarcado
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
PE20181888A1 (es) 2016-04-04 2018-12-11 Loxo Oncology Inc Formulaciones liquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
EP3800189B1 (en) 2016-05-18 2023-06-28 Loxo Oncology, Inc. Preparation of (s)-n-(5-((r)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
CA3084298A1 (en) * 2017-12-07 2019-06-13 Amplyx Pharmaceuticals, Inc. Heterocycle substituted pyridine derivative antifungal agents
US11771688B2 (en) 2018-06-25 2023-10-03 Amplyx Pharmaceuticals, Inc. Pyridine derivatives substituted by heterocyclic ring and amino group
WO2021216440A1 (en) * 2020-04-20 2021-10-28 Tenova Pharmaceuticals Inc. Novel protein kinase inhibitors
WO2023114809A1 (en) 2021-12-16 2023-06-22 Kinnate Biopharma Inc. Inhibitors of met kinase
WO2024017258A1 (zh) * 2022-07-19 2024-01-25 百极弘烨(南通)医药科技有限公司 Egfr小分子抑制剂、含其的药物组合物及其用途

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE558251A (es) * 1956-06-11
DE2423536A1 (de) * 1974-05-15 1975-11-27 Bayer Ag 3-amino-phenylessigsaeure-derivate, verfahren zu ihrer herstellung sowie ihre verwendung als herbizide
US4066772A (en) * 1975-07-21 1978-01-03 Janssen Pharmaceutica N.V. 1,3-Dihydro-1-[3-(1-piperidinyl)propyl]-2H-benzimidazol-2-ones and related compounds
NZ181256A (en) * 1975-07-21 1978-04-28 Janssen Pharmaceutica Nv 1-(w-benzazol-11-ylalkyl)-piperidine derivatives and pharmaceutical compositions containing certain of these derivatives
US4126688A (en) 1976-05-17 1978-11-21 Janssen Pharmaceutica N.V. Antiemetic 1-(benzotriazolyl-alkyl)-piperidine derivatives
US5721237A (en) 1991-05-10 1998-02-24 Rhone-Poulenc Rorer Pharmaceuticals Inc. Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties
GB9510757D0 (en) * 1994-09-19 1995-07-19 Wellcome Found Therapeuticaly active compounds
GB9508538D0 (en) * 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
DE69710712T3 (de) 1996-04-12 2010-12-23 Warner-Lambert Co. Llc Umkehrbare inhibitoren von tyrosin kinasen
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
WO2000020402A1 (en) * 1998-10-01 2000-04-13 Astrazeneca Ab Chemical compounds
FR2809400B1 (fr) * 2000-05-25 2004-04-09 Inst Francais Du Petrole Materiaux comportant des groupements organiques contenant du soufre et du phosphore lie par l'intermediaire d'atomes d'oxygenes a un oxyde mineral
PA8603801A1 (es) * 2003-05-27 2004-12-16 Janssen Pharmaceutica Nv Derivados de la quinazolina
JO3088B1 (ar) * 2004-12-08 2017-03-15 Janssen Pharmaceutica Nv مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف
GB2446974B (en) * 2006-04-13 2009-01-14 Siemens Magnet Technology Ltd A solenoidal magnet structure

Also Published As

Publication number Publication date
US8394786B2 (en) 2013-03-12
TWI379835B (en) 2012-12-21
JP4887151B2 (ja) 2012-02-29
US20060247237A1 (en) 2006-11-02
CN102718775A (zh) 2012-10-10
US7648975B2 (en) 2010-01-19
EP1633365B1 (en) 2012-02-08
IL172154A0 (en) 2006-04-10
NO334209B1 (no) 2014-01-13
TWI468397B (zh) 2015-01-11
US20130178624A1 (en) 2013-07-11
DK1633365T3 (da) 2012-05-14
PT1633365E (pt) 2012-05-07
BRPI0410714A (pt) 2006-06-13
US20100105668A1 (en) 2010-04-29
CL2004001267A1 (es) 2005-04-22
IL233045B (en) 2018-07-31
JP2007504276A (ja) 2007-03-01
CY1113002T1 (el) 2016-04-13
KR101143878B1 (ko) 2012-05-24
PA8603801A1 (es) 2004-12-16
SI1633365T1 (sl) 2012-06-29
TW201245111A (en) 2012-11-16
US9273013B2 (en) 2016-03-01
KR20060014415A (ko) 2006-02-15
AU2004243487A1 (en) 2004-12-09
CO5640038A2 (es) 2006-05-31
ES2381976T3 (es) 2012-06-04
JO2785B1 (en) 2014-03-15
MXPA05012762A (es) 2006-02-13
HK1176350A1 (zh) 2013-07-26
EA200501866A1 (ru) 2006-06-30
UA84010C2 (en) 2008-09-10
TW200510431A (en) 2005-03-16
NO20056196L (no) 2005-12-28
AR045687A1 (es) 2005-11-09
TWI468372B (zh) 2015-01-11
BRPI0410714B8 (pt) 2021-05-25
WO2004105765A1 (en) 2004-12-09
CA2525214C (en) 2012-11-27
EP2305687A1 (en) 2011-04-06
CA2525214A1 (en) 2004-12-09
AU2004243487B2 (en) 2009-12-03
HRP20120351T1 (hr) 2012-05-31
NZ544154A (en) 2009-01-31
EA009064B1 (ru) 2007-10-26
IS3030B (is) 2021-06-15
US20160207938A1 (en) 2016-07-21
IS8077A (is) 2005-10-14
PL1633365T3 (pl) 2012-07-31
BRPI0410714B1 (pt) 2019-09-24
IL233046A0 (en) 2014-07-31
MY148633A (en) 2013-05-15
IL233045A0 (en) 2014-07-31
CN102718775B (zh) 2016-02-17
ATE544454T1 (de) 2012-02-15
EP1633365A1 (en) 2006-03-15
TW201245160A (en) 2012-11-16

Similar Documents

Publication Publication Date Title
AR092137A2 (es) Derivados macrociclicos de quinazolina utiles como agentes antiproliferativos
AR109805A1 (es) Derivados de oxadiazol microbiocidas
AR112687A1 (es) Agonistas del receptor tipo toll 7 (tlr7) que tienen una porción tricíclica, conjugados de estos y métodos y usos de estos
AR106301A1 (es) Composiciones de pirrolpirimidina como inhibidores de quinasas
AR120684A1 (es) INHIBIDORES DE HIF-2a
AR112290A1 (es) Dinucleótidos cíclicos como agentes anticáncer
AR075731A1 (es) Derivados heterociclicos de bencimidazoles, composiciones farmaceuticas que los comprenden y uso de los mismos para el tratamiento del virus sincicial respiratorio(vsr).
EA200601177A1 (ru) Пиридо- и пиримидопиримидиновые производные в качестве антипролиферативных агентов
AR088449A1 (es) Benzilindazoles sustituidos
AR087467A1 (es) Compuesto heterociclico fusionado y su uso para el control de plagas
AR038703A1 (es) Derivados de 5-feniltiazol y uso como inhibidor de quinasa p i 3
UA90693C2 (en) 2,4 (4,6)-pyrimidine derivatives
AR059086A1 (es) Derivados de urea ciclica su preparcion y su utilizacion farmaceutica como inhibidores de cinasas
AR091022A1 (es) Inhibidores del nampt
AR114369A1 (es) Dinucleótidos cíclicos como agentes antineoplásicos
AR105929A1 (es) Derivados de 2-difluorometil-nicotin(tio)carboxanilida sustituidos y su uso como fungicidas
AR088596A1 (es) Compuestos de bencilamina sustituidos
AR113842A1 (es) Derivados de tiazol microbiocidas
AR114430A1 (es) Compuestos herbicidas
AR109689A1 (es) Compuesto de oxadiazol y su uso
AR095570A1 (es) Derivados de urea
AR113931A1 (es) Tratamientos de combinación que comprenden la administración de 1h-pirazolo[4,3-b]piridinas
AR100821A1 (es) Pirazolil-triazolil-piridinas como agentes plaguicidas
AR096727A1 (es) Derivados terapéuticamente activos de estratrien-tiazol
AR101206A1 (es) Derivados de piridina triazolil arilo como pesticidas

Legal Events

Date Code Title Description
FB Suspension of granting procedure