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DK2716633T3 - Quinazolin-derivat som tyrosin-kinaseinhibitor, fremgangsmåde til fremstilling deraf og anvendelse deraf - Google Patents

Quinazolin-derivat som tyrosin-kinaseinhibitor, fremgangsmåde til fremstilling deraf og anvendelse deraf Download PDF

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Publication number
DK2716633T3
DK2716633T3 DK12788871.7T DK12788871T DK2716633T3 DK 2716633 T3 DK2716633 T3 DK 2716633T3 DK 12788871 T DK12788871 T DK 12788871T DK 2716633 T3 DK2716633 T3 DK 2716633T3
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cancer
methyl
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DK12788871.7T
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Frank Wu
Aichen Wang
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Xuanzhu Pharma Co Ltd
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    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
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    • 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
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    • 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
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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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    • 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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
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    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/06—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing isoquinuclidine ring systems
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    • 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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
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    • C—CHEMISTRY; METALLURGY
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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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    • 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
    • C07D491/10—Spiro-condensed systems
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    • 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
    • C07D498/08—Bridged systems

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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (9)

1. Forbindelse repræsenteret af den generelle formel (1-2), eller en stereoisomer deraf, eller et farmaceutisk acceptabelt salt deraf:
hvor R1 er valgt fra gruppen bestående af de følgende grupper, der er usubstitueret eller substitueret af halogen, hydroxy, amino, carboxyl, cyano, methyl, ethyl, methoxy, ethoxy, methylamino, ethylamino, dimethylamino, eller diethylamino: methyl, ethyl,
R2 er valgt fra gruppen bestående af de følgende grupper, der er usubstitueret eller substitueret af halogen, hydroxy, amino, methyl, ethyl, methoxy, ethoxy, methylamino, ethylamino, dimethylamino, diethylamino, acetoxy, acetylamino, methylsulfonyl, eller methylsulfonylamino:
og Ler 0.
2. Forbindelsen ifølge krav 1 eller en stereoisomer deraf, eller et farmaceutisk acceptabelt salt deraf, hvor forbindelsen er valgt fra gruppen bestående af:
3. Forbindelse, eller en stereoisomer deraf, eller et farmaceutisk acceptabelt salt deraf, hvor forbindelsen er valgt fra gruppen bestående af:
4. Farmaceutisk sammensætning, der indeholder forbindelsen ifølge et hvilket som helst af kravene 1-3, eller en stereoisomer deraf, eller et farmaceutisk acceptabelt salt deraf.
5. Den farmaceutiske sammensætning ifølge krav 4, hvilken yderligere indeholder et andet terapeutisk middel valgt fra gruppen bestående af et antineoplastisk middel og et immunosuppressivt middel, hvilket andet terapeutiske middel er valgt fra gruppen bestående af en antimetabolit, der inkluderer capecitabin og gemcitabin; en vækstfaktorinhibitor, der inkluderer pazopanib og imatinib; et antistof, der inkluderer herceptin og bevacizumab; en mitoseinhibitor, der inkluderer paclitaxel, vinorelbin, docetaxel, og doxorubicin; et antineoplastisk hormon, der inkluderer letrozol, tamoxifen og fulvestrant; et alkylerende middel, der inkluderer cyklophosphamid og carmustin; et platinmetal, der inkluderer carboplatin, cisplatin, og oxaliplatin; en topoisomeraseinhibitor, der inkluderer topotecan; og et immunosuppressivt middel, der inkluderer everolimus.
6. Farmaceutisk formulering, der indeholder en forbindelse ifølge et hvilket som helst af kravene 1-3, eller en stereoisomer deraf, eller et farmaceutisk acceptabelt salt deraf og en eller flere farmaceutisk acceptable bærere.
7. Forbindelsen ifølge et hvilket som helst af kravene 1-3, eller en stereoisomer deraf, eller et farmaceutisk acceptabelt salt deraf til anvendelse i behandling af en excessiv proliferativ sygdom eller en kronisk obstruktiv lungesygdom.
8. Forbindelsen til anvendelse ifølge krav 7, eller en stereoisomer deraf, eller et farmaceutisk acceptabelt salt deraf, hvor den excessive proliferative sygdom inkluderer en kræftsygdom og en ikke-kræftsygdom, hvilken kræftsygdom er valgt fra gruppen bestående af cerebroma, lungekræft, ikke-småcellet lungekræft, pladeepitelcelle, blærekarcinom, mavekræft, kræft i æggestokkene, peritonealkræft, kræft i bugspytkirtlen, brystkræft, kræft i hoved og hals, livmoderhalskræft, endometriekræft, kolorektalkræft, leverkræft, nyrekarcinom, adenokarcinom i spiserøret, pladeepitelcellekræft i spiserøret, fast tumor, non-Hodgkin lymfom, tumor i det centrale nervesystem (gliom, gliobaston multiform, gliom sarcomatose), prostatakarcinom eller karcinom i skjoldbruskkirtel; og ikke-kræftsygdom men er godartede proliferative sygdomme af hud eller prostata.
9. Fremgangsmåde til fremstilling af en forbindelse ifølge krav 1, omfattende trinnene: Reaktionsfremgangsmåde:
hvor R1, R2, R3, R3', R4, R5, R6, X, L, T, Z og q er som defineret i krav 1, Hal1 vælges fra gruppen bestående af Cl, Br og I, Hal2 vælges fra gruppen bestående af Cl og Br, og Hal1 og Hal2 kan være identiske eller forskellige; 1) at opløse en forbindelse af udgangsmaterialet (a) i et organisk solvent, og at reagere det med en forbindelse af formlen (V) under tilstedeværelsen af en uorganisk base for at fremstille en forbindelse af formlen (IV); 2) at reagere forbindelsen af formlen (IV) og et reduktionsmiddel for at fremstille en forbindelse af formlen (III); 3) at opløse forbindelsen af formlen (III) i et organisk solvent, og at reagere den med en forbindelse af formlen (b) for at fremstille en forbindelse af formlen (II); og 4) at reagere forbindelsen af formlen (II) og en forbindelse af formlen (c) under tilstedeværelsen af en base for at fremstille en forbindelse af formlen (i); hvor hvis nødvendigt, en funktionel gruppe, der har brug for at blive beskyttet kan beskyttes, og derefter afbeskyttes ifølge en konventionel fremgangsmåde.
DK12788871.7T 2011-05-26 2012-05-28 Quinazolin-derivat som tyrosin-kinaseinhibitor, fremgangsmåde til fremstilling deraf og anvendelse deraf DK2716633T3 (da)

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CN201110138115 2011-05-26
PCT/CN2012/000737 WO2012159457A1 (zh) 2011-05-26 2012-05-28 喹唑啉衍生物类酪氨酸激酶抑制剂及其制备方法与应用

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US (2) US9586939B2 (da)
EP (1) EP2716633B1 (da)
JP (1) JP5859118B2 (da)
CN (1) CN103748080B (da)
DK (1) DK2716633T3 (da)
HU (1) HUE033575T2 (da)
WO (1) WO2012159457A1 (da)

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DK2716633T3 (da) 2011-05-26 2017-07-17 Xuanzhu Pharma Co Ltd Quinazolin-derivat som tyrosin-kinaseinhibitor, fremgangsmåde til fremstilling deraf og anvendelse deraf
CN103987700B (zh) * 2012-03-09 2016-08-31 江苏豪森药业集团有限公司 4-喹唑啉胺类衍生物及其用途
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WO2017107985A1 (zh) * 2015-12-25 2017-06-29 山东轩竹医药科技有限公司 喹唑啉衍生物的晶体及其制备方法
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CN107721985A (zh) * 2016-08-12 2018-02-23 山东轩竹医药科技有限公司 喹唑啉类酪氨酸激酶抑制剂的晶型
CN107721986A (zh) * 2016-08-12 2018-02-23 山东轩竹医药科技有限公司 喹唑啉类酪氨酸激酶抑制剂的晶型
CN107721987A (zh) * 2016-08-12 2018-02-23 山东轩竹医药科技有限公司 喹唑啉类酪氨酸激酶抑制剂的晶型
US11111234B2 (en) 2016-08-12 2021-09-07 Xuanzhu Pharma Co., Ltd. Salt of a quinazoline derivative-like tyrosine kinase inhibitor and crystal form thereof
CN108078990B (zh) * 2016-11-23 2023-06-02 山东轩竹医药科技有限公司 喹唑啉衍生物类酪氨酸激酶抑制剂的新用途
CN109071498B (zh) * 2017-02-16 2021-03-30 四川科伦博泰生物医药股份有限公司 激酶抑制剂及其制备方法和用途
CN110963972A (zh) * 2019-11-21 2020-04-07 苏州明锐医药科技有限公司 一种喹唑啉衍生物及其制备方法与药物用途
CN113292574B (zh) * 2020-02-21 2022-05-03 四川大学 一类手性多环的托品烷化合物及其制备方法和用途
WO2021209039A1 (zh) * 2020-04-17 2021-10-21 北京赛特明强医药科技有限公司 一种喹唑啉类化合物、制备方法及其应用
CN112920103A (zh) * 2021-03-02 2021-06-08 康化（上海）新药研发有限公司 一种温和制备2-氮杂螺[3.3]庚烷盐酸盐的方法
CN113264888A (zh) * 2021-03-04 2021-08-17 江苏康可得生物技术股份有限公司 酪氨酸激酶抑制剂及其药物应用

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JP5859118B2 (ja) 2016-02-10
EP2716633B1 (en) 2017-05-17
US9956222B2 (en) 2018-05-01
WO2012159457A1 (zh) 2012-11-29
EP2716633A4 (en) 2014-10-29
CN103748080A (zh) 2014-04-23
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US20140161801A1 (en) 2014-06-12

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