HRP20160495T1 - Morfolinilbenzotriazini za uporabu u terapiji raka - Google Patents

Morfolinilbenzotriazini za uporabu u terapiji raka Download PDF

Info

Publication number
HRP20160495T1
HRP20160495T1 HRP20160495TT HRP20160495T HRP20160495T1 HR P20160495 T1 HRP20160495 T1 HR P20160495T1 HR P20160495T T HRP20160495T T HR P20160495TT HR P20160495 T HRP20160495 T HR P20160495T HR P20160495 T1 HRP20160495 T1 HR P20160495T1
Authority
HR
Croatia
Prior art keywords
atoms
hal
image
denotes
tautomers
Prior art date
Application number
HRP20160495TT
Other languages
English (en)
Inventor
Werner Mederski
Thomas Fuchss
Ulrich Emde
Hans-Peter Buchstaller
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of HRP20160495T1 publication Critical patent/HRP20160495T1/hr

Links

Classifications

    • 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/08—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 condensed with carbocyclic rings or ring systems
    • 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
    • C07D401/04—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
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/10—Compounds having one or more C—Si linkages containing nitrogen having a Si-N linkage
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Radiology & Medical Imaging (AREA)
  • Pathology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (14)

1. Spojevi s formulom (I) [image] naznačeni time da R1 označava Het1 ili Ar; R2, R3, međusobno neovisno, označavaju Y ili OY, ili zajedno također označavaju -O-(CH2)n-; R4 označava A ili (CH2)nOA; L označava -CR2R3-, jednostruku vezu, -(CH2)n-, -CH(Hal)-, -C(Hal)2-, -(CH2)nCH(OY)-, -(CH2)nCO-, -(CH2)nNH-, -(CH2)nCONY2-, -NYCO-, -NHCO-NH-, -NR4CO-, -NYSO2-, -C(=NR4)-, -C(=NCN)-, -CY(NY2)-, -CY(CN)-, -CY(O-(CH2)nCN)-, -CY(Het2)- ili -CY(O-(CH2)nHet2)-; Y označava H ili A; A označava nerazgranati ili razgranati alkil koji ima 1-10 C atoma, u kojem, međusobno neovisno, 1-7 H atoma mogu biti zamijenjeni s Hal; Cyc označava ciklički alkil koji ima 3-7 C atoma, u kojem, međusobno neovisno, 1-4 H atoma mogu biti zamijenjeni s Hal; Ar označava fenil koji je nesupstituiran ili jednostruko- ili dvostruko supstituiran s Hal, (CH2)pOY, R4, (CH2)pOR4, COOY, NY2, NYCOY i/ili CN; Het1 označava mono- ili biciklički heteroaril koji ima 2-9 C atoma i 1-4 N, O i/ili S atoma, koji mogu biti nesupstituirani ili jednostruko- ili dvostruko supstituirani s Hal, (CH2)pOY, R4, (CH2)pOR4, =O, COOY, NY2, NYCOY, CONY2, Cyc, Het2 i/ili CN; Het2 označava monociklički zasićeni heterocikal koji ima 2-7 C atoma i 1-4 N, O i/ili S atoma, koji mogu biti nesupstituirani ili jednostruko supstituirani s A; Hal označava F, Cl, Br ili I; m označava 0, 1 ili 2; i n, p, međusobno neovisno, označavaju 0, 1, 2, 3, 4 ili 5, i/ili njihove fiziološki prihvatljive soli, tautomeri i/ili stereoizomeri, uključujući njihove smjese u svim omjerima.
2. Spojevi prema zahtjevu 1 naznačeni time da R1 označava Het1.
3. Spojevi prema zahtjevu 1 ili 2 naznačeni time da R2, R3, međusobno neovisno, označavaju Y ili OY.
4. Spojevi prema jednom od zahtjeva 1 do 3 naznačeni time da L označava -CR2R3-.
5. Spojevi prema jednom od zahtjeva 1 do 4 naznačeni time da Het1 označava mono- ili biciklički heteroaril koji ima 2-8 C atoma i 1-3 N, O i/ili S atoma, koji mogu biti nesupstituirani ili jednostruko- ili dvostruko supstituirani s Hal, (CH2)pOY, A i/ili =O.
6. Spojevi prema zahtjevu 1 koji imaju pod-formulu (IA) [image] naznačeni time da R1 označava Het1 ili Ar; R2 označava Y ili OY; R3 označava OY ili A; R2, R3 zajedno također označavaju -O-(CH2)n-; L označava -CR2R3-; Y označava H ili A; A označava nerazgranati ili razgranati alkil koji ima 1-6 C atoma, u kojem, međusobno neovisno, 1-5 H atoma mogu biti zamijenjeni s Hal; Ar označava fenil koji je nesupstituiran ili jednostruko- ili dvostruko supstituiran s Hal i/ili (CH2)pOY; Het1 označava mono- ili biciklički heteroaril koji ima 2-8 C atoma i 1-3 N, O i/ili S atoma, koji mogu biti nesupstituirani ili jednostruko- ili dvostruko supstituirani s Hal, (CH2)pOY, A i/ili =O; Hal označava F, Cl, Br ili I; i n, p, međusobno neovisno, označavaju 0, 1, 2, 3 ili 4, i/ili njihove fiziološki prihvatljive soli, tautomeri i/ili stereoizomeri, uključujući njihove smjese u svim omjerima.
7. Spojevi prema zahtjevu 1 koji imaju pod-formulu (IB) [image] naznačeni time da Y označava H ili A; A označava nerazgranati ili razgranati alkil koji ima 1-6 C atoma, u kojem, međusobno neovisno, 1-3 H atoma mogu biti zamijenjeni s Hal; Het1 označava heteroaril koji je nesupstituiran ili jednostruko- ili dvostruko supstituiran s Hal, (CH2)pOY, A i/ili =O, odabran iz skupine koju čine: [image] [image] [image] [image] [image] Hal označava F, Cl, Br ili I; i p označava 0, 1 ili 2, i/ili njihove fiziološki prihvatljive soli, tautomeri i/ili stereoizomeri, uključujući njihove smjese u svim omjerima.
8. Spojevi prema jednom od zahtjeva 1 do 7, naznačeni time da su odabrani iz skupine: [image] [image] [image] i/ili njihove fiziološki prihvatljive soli, tautomeri i/ili stereoizomeri, uključujući njihove smjese u svim omjerima.
9. Postupak za pripravu spojeva formule (I) u skladu s patentnim zahtjevom 1 i/ili njihovih fiziološki prihvatljivih soli, tautomera i/ili stereoizomera naznačen time da sadrži slijedeće korake: (a) reakciju spoja formule (II) [image] sa spojem formule (III) ili (V) [image] u kojoj R1, L i m imaju značenje navedeno u zahtjevu 1, uz dobivanje spojeva formule (I) [image] u kojoj R1, L i m imaju značenje navedeno u zahtjevu 1, i proizvoljno (b) pretvorbu baze ili kiseline spojeva formule (I) u njihovu sol.
10. Uporaba spojeva prema jednom od zahtjeva 1 do 8 i/ili njihovih fiziološki prihvatljivih soli, tautomera i/ili stereoizomera, uključujući njihove smjese u svim omjerima, naznačena time da je za inhibiciju serin/treonin protein kinaza in vitro, poželjno PIKK, naročito poželjno DNA-PK.
11. Spojevi prema jednom od zahtjeva 1 do 8 i/ili njihove fiziološki prihvatljive soli, tautomeri i/ili stereoizomeri, uključujući njihove smjese u svim omjerima, naznačeni time da su za uporabu za senzitizaciju stanica raka na sredstvo protiv raka i/ili na ionizirajuće zračenje.
12. Lijekovi naznačeni time da sadrže barem jedan spoj prema jednom od zahtjeva 1 do 8 i/ili njihove fiziološki prihvatljive soli, tautomere i/ili stereoizomere, uključujući njihove smjese u svim omjerima.
13. Farmaceutski pripravak naznačen time da sadrži, kao aktivni spoj, učinkovitu količinu barem jednog spoja prema jednom od zahtjeva 1 do 8 i/ili njihove fiziološki prihvatljive soli, tautomere i/ili stereoizomere, uključujući njihove smjese u svim omjerima, zajedno s farmaceutski podnošljivim pomoćnim sredstvima, u kombinaciji s barem jednim antikancerogenim sredstvom.
14. Spojevi prema jednom od zahtjeva 1 do 8 i/ili njihove fiziološki prihvatljive soli, tautomeri i/ili stereoizomeri, uključujući njihove smjese u svim omjerima, naznačeni time da su za uporabu za profilaksu, terapiju i/ili kontrolu napredovanja raka, tumora, metastaza i/ili poremećaja angiogeneze, u kombinaciji s radioterapijom i/ili s barem jednim antikancerogenim sredstvom.
HRP20160495TT 2011-11-18 2016-05-09 Morfolinilbenzotriazini za uporabu u terapiji raka HRP20160495T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE102011118830A DE102011118830A1 (de) 2011-11-18 2011-11-18 Morpholinylbenzotriazine
PCT/EP2012/004542 WO2013072015A1 (de) 2011-11-18 2012-10-30 Morpholinylbenzotriazine zur anwendung in der krebstherapie
EP12783121.2A EP2780332B1 (de) 2011-11-18 2012-10-30 Morpholinylbenzotriazine zur anwendung in der krebstherapie

Publications (1)

Publication Number Publication Date
HRP20160495T1 true HRP20160495T1 (hr) 2016-06-03

Family

ID=47143824

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20160495TT HRP20160495T1 (hr) 2011-11-18 2016-05-09 Morfolinilbenzotriazini za uporabu u terapiji raka

Country Status (24)

Country Link
US (1) US9187469B2 (hr)
EP (1) EP2780332B1 (hr)
JP (1) JP6096792B2 (hr)
KR (1) KR20140097391A (hr)
CN (1) CN103930408B (hr)
AU (1) AU2012339196B2 (hr)
BR (1) BR112014011805A2 (hr)
CA (1) CA2856103C (hr)
DE (1) DE102011118830A1 (hr)
DK (1) DK2780332T3 (hr)
EA (1) EA201400595A1 (hr)
ES (1) ES2572605T3 (hr)
HK (1) HK1199875A1 (hr)
HR (1) HRP20160495T1 (hr)
HU (1) HUE027577T2 (hr)
IL (1) IL232577A (hr)
IN (1) IN2014KN01287A (hr)
MX (1) MX2014005838A (hr)
PL (1) PL2780332T3 (hr)
RS (1) RS54768B1 (hr)
SG (1) SG11201402206YA (hr)
SI (1) SI2780332T1 (hr)
WO (1) WO2013072015A1 (hr)
ZA (1) ZA201404438B (hr)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102089239B1 (ko) 2012-04-24 2020-03-16 버텍스 파마슈티칼스 인코포레이티드 Dna-pk 억제제
ES2900061T3 (es) 2013-03-12 2022-03-15 Vertex Pharma Inhibidores de DNA-PK
DE102013008118A1 (de) 2013-05-11 2014-11-13 Merck Patent Gmbh Arylchinazoline
JP6408569B2 (ja) 2013-10-17 2018-10-17 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ｄｎａ−ｐｋ阻害剤としての（ｓ）−ｎ−メチル−８−（１−（（２’−メチル−［４，５’−ビピリミジン］−６−イル）アミノ）プロパン−２−イル）キノリン−４−カルボキサミドおよびその重水素化誘導体の共結晶
TW201815418A (zh) 2016-09-27 2018-05-01 Vertex Pharma 使用dna破壞劑及dna-pk抑制劑之組合治療癌症的方法
CN107793373B (zh) * 2017-10-31 2019-09-17 广西师范大学 2-取代苯并三嗪酮衍生物及其制备方法
EA202091708A1 (ru) * 2018-01-17 2020-11-10 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы днк-пк
CN114630825A (zh) 2019-11-01 2022-06-14 先正达农作物保护股份公司 杀有害生物活性的稠合二环杂芳香族化合物
CA3221180A1 (en) 2021-06-24 2022-12-29 Syngenta Crop Protection Ag 2-[3-[1 [(quinazolin-4-yl)amino]ethyl]pyrazin-2-yl]thiazole-5-carbonitrile derivatives and similar compounds as pesticides
WO2023247360A1 (en) 2022-06-21 2023-12-28 Syngenta Crop Protection Ag Pesticidally active fused bicyclic heteroaromatic compounds

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2095213A1 (en) 1990-11-06 1992-05-07 Jotham W. Coe Quinazoline derivatives for enhancing antitumor activity
WO2000061186A1 (en) 1999-04-08 2000-10-19 Arch Development Corporation Use of anti-vegf antibody to enhance radiation in cancer therapy
WO2002020500A2 (en) * 2000-09-01 2002-03-14 Icos Corporation Materials and methods to potentiate cancer treatment
US7291733B2 (en) * 2003-10-10 2007-11-06 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted tricyclic heterocycles and their uses
CN101230045B (zh) * 2008-02-14 2013-04-10 沈阳药科大学 芳环并三嗪类衍生物及其应用
CN102803227B (zh) * 2010-03-16 2016-01-20 默克专利有限公司 吗啉基喹唑啉

Also Published As

Publication number Publication date
EA201400595A1 (ru) 2014-11-28
IL232577A0 (en) 2014-06-30
AU2012339196B2 (en) 2017-04-27
PL2780332T3 (pl) 2016-07-29
BR112014011805A2 (pt) 2017-05-16
IN2014KN01287A (hr) 2015-10-16
WO2013072015A1 (de) 2013-05-23
HK1199875A1 (en) 2015-07-24
DE102011118830A1 (de) 2013-05-23
AU2012339196A1 (en) 2014-07-03
JP6096792B2 (ja) 2017-03-15
IL232577A (en) 2017-05-29
CN103930408B (zh) 2016-09-07
HUE027577T2 (en) 2016-10-28
ZA201404438B (en) 2015-12-23
SI2780332T1 (sl) 2016-06-30
RS54768B1 (sr) 2016-10-31
ES2572605T3 (es) 2016-06-01
CA2856103A1 (en) 2013-05-23
CA2856103C (en) 2020-08-25
CN103930408A (zh) 2014-07-16
MX2014005838A (es) 2014-07-30
US20140275072A1 (en) 2014-09-18
US9187469B2 (en) 2015-11-17
DK2780332T3 (en) 2016-05-30
JP2015502926A (ja) 2015-01-29
EP2780332A1 (de) 2014-09-24
KR20140097391A (ko) 2014-08-06
EP2780332B1 (de) 2016-02-24
SG11201402206YA (en) 2014-11-27

Similar Documents

Publication Publication Date Title
HRP20160495T1 (hr) Morfolinilbenzotriazini za uporabu u terapiji raka
HRP20150489T1 (hr) Imidazo[4,5-c]kinolini kao inhibitori dna-pk
JP6789239B2 (ja) Ｋｒａｓの縮合三環系インヒビターおよびその使用の方法
JP6862495B2 (ja) Ｊａｋ及びｐｉ３ｋ阻害剤併用によるｂ細胞悪性腫瘍の処置
HRP20150030T1 (hr) Derivati pirazolokinolina kao inhibitori dna-pk
JP2021098721A (ja) 置換キナゾリン化合物およびその使用方法
MX2009008953A (es) Compuestos como inhibidores de angiogenesis.
MX2009009843A (es) Compuestos espiro sustituidos como inhibidores de la angiogenesis.
EA201201289A1 (ru) Морфолинилхиназолины
NZ630457A (en) Compounds useful as inhibitors of atr kinase
JP2021107465A (ja) Ｎ−（シアノメチル）−４−（２−（４−モルホリノフェニルアミノ）ピリミジン−４−イル）ベンズアミド塩酸塩
HRP20140814T1 (hr) Inhibitori jak2 i njihova uporaba za lijeäśenje mijeloproliferativnih bolesti i karcinoma
HRP20220886T1 (hr) Pripravci i postupci za proizvodnju pirimidina i spojeva piridina s btk inhibicijskom aktivnošću
AR073551A1 (es) Pirimidinas macrociclicas como inhibidores de proteina cinasa
JP2014503567A5 (hr)
JP2013529196A5 (hr)
WO2010021918A8 (en) Compounds as kinase inhibitors
RU2758669C2 (ru) Способ лечения рака с применением сочетания днк-поражающих агентов и ингибиторов днк-пк
HRP20211801T1 (hr) Derivati kinolin-2-ona
PE20230372A1 (es) Triazolopirimidinas como inhibidores de a2a/a2b
JP2015503627A (ja) ジヒドロピロロ［１，２−ｃ］イミダゾリルアルドステロンシンターゼまたはアロマターゼ阻害薬の新たな形態および塩
EP2906564A1 (en) Treating brain cancer using agelastatin a (aa) and analogues thereof
US20220315563A1 (en) Alk-5 inhibitors and uses thereof
HRP20231276T1 (hr) Inhibitor egfr-a za liječenje raka
SI2864328T1 (en) Pharmaceutically active compounds