KR101272613B1 - 1-(4-(4-(3,4-디클로로-2-플루오로페닐아미노)-7-메톡시퀴나졸린-6-일옥시)피페리딘-1-일)프로프-2-엔-1-온 염산염의 제조 방법 및 이에 사용되는 중간체 - Google Patents

1-(4-(4-(3,4-디클로로-2-플루오로페닐아미노)-7-메톡시퀴나졸린-6-일옥시)피페리딘-1-일)프로프-2-엔-1-온 염산염의 제조 방법 및 이에 사용되는 중간체 Download PDF

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Publication number
KR101272613B1
KR101272613B1 KR1020110101422A KR20110101422A KR101272613B1 KR 101272613 B1 KR101272613 B1 KR 101272613B1 KR 1020110101422 A KR1020110101422 A KR 1020110101422A KR 20110101422 A KR20110101422 A KR 20110101422A KR 101272613 B1 KR101272613 B1 KR 101272613B1
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KR
South Korea
Prior art keywords
formula
compound
dichloro
fluorophenylamino
methoxyquinazolin
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Expired - Fee Related
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KR1020110101422A
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English (en)
Korean (ko)
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KR20130037079A (ko
Inventor
방극찬
문영호
장영길
Original Assignee
한미사이언스 주식회사
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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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48044309&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR101272613(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 한미사이언스 주식회사 filed Critical 한미사이언스 주식회사
Priority to KR1020110101422A priority Critical patent/KR101272613B1/ko
Priority to AU2012319291A priority patent/AU2012319291B2/en
Priority to CN201280049302.7A priority patent/CN103857672B/zh
Priority to SI201231742T priority patent/SI2763981T1/sl
Priority to EP12838558.0A priority patent/EP2763981B1/en
Priority to RS20200295A priority patent/RS60118B1/sr
Priority to HRP20200426TT priority patent/HRP20200426T1/hr
Priority to EP19201644.2A priority patent/EP3611172A1/en
Priority to US14/349,887 priority patent/US8859767B2/en
Priority to DK12838558.0T priority patent/DK2763981T3/da
Priority to PL12838558T priority patent/PL2763981T3/pl
Priority to HUE12838558A priority patent/HUE048798T2/hu
Priority to ES12838558T priority patent/ES2775197T3/es
Priority to PCT/KR2012/008077 priority patent/WO2013051883A2/en
Priority to JP2014534478A priority patent/JP5805880B2/ja
Priority to RU2014117648/04A priority patent/RU2563630C1/ru
Priority to IN3447DEN2014 priority patent/IN2014DN03447A/en
Priority to CA2850055A priority patent/CA2850055C/en
Priority to PT128385580T priority patent/PT2763981T/pt
Priority to BR112014007718-5A priority patent/BR112014007718B1/pt
Priority to MX2014003959A priority patent/MX348815B/es
Priority to CN201811593540.XA priority patent/CN110003174A/zh
Priority to LTEP12838558.0T priority patent/LT2763981T/lt
Publication of KR20130037079A publication Critical patent/KR20130037079A/ko
Publication of KR101272613B1 publication Critical patent/KR101272613B1/ko
Application granted granted Critical
Priority to IL231911A priority patent/IL231911B/en
Priority to IL259694A priority patent/IL259694B/en
Priority to CY20201100214T priority patent/CY1122758T1/el
Priority to IL291738A priority patent/IL291738A/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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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
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020110101422A 2011-10-05 2011-10-05 1-(4-(4-(3,4-디클로로-2-플루오로페닐아미노)-7-메톡시퀴나졸린-6-일옥시)피페리딘-1-일)프로프-2-엔-1-온 염산염의 제조 방법 및 이에 사용되는 중간체 Expired - Fee Related KR101272613B1 (ko)

Priority Applications (27)

Application Number Priority Date Filing Date Title
KR1020110101422A KR101272613B1 (ko) 2011-10-05 2011-10-05 1-(4-(4-(3,4-디클로로-2-플루오로페닐아미노)-7-메톡시퀴나졸린-6-일옥시)피페리딘-1-일)프로프-2-엔-1-온 염산염의 제조 방법 및 이에 사용되는 중간체
JP2014534478A JP5805880B2 (ja) 2011-10-05 2012-10-05 １−（４−（４−（３，４−ジクロロ−２−フルオロフェニルアミノ）−７−メトキシキナゾリン−６−イルオキシ）ピペリジン−１−イル）−プロパ−２−エン−１−オン塩酸塩の製造方法および該方法で用いられる中間体
RU2014117648/04A RU2563630C1 (ru) 2011-10-05 2012-10-05 Способ получения гидрохлорида 1-(3,4-дихлор-2-фторфениламино)-7-метоксихиназолин-6-илокси)пиперидин-1-ил)проп-2-ен-1-она и используемых в нем промежуточных соединений
SI201231742T SI2763981T1 (sl) 2011-10-05 2012-10-05 Metoda za pripravo 1-(4-(4-(3,4-dikloro-2-fluorofenilamino)-7-metoksikinazolin-6-iloksi) piperidin-1-IL)-PROP-2-EN-1-ON hidroklorida in intermediati uporabljeni pri tem
EP12838558.0A EP2763981B1 (en) 2011-10-05 2012-10-05 Method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one hydrochloride and intermediates used therein
RS20200295A RS60118B1 (sr) 2011-10-05 2012-10-05 Postupak za pripremu 1-(4-(4-(3,4-dihloro-2-fluorofenilamino)-7-metoksikvinazolin-6-iloksi)piperidin-1-il)-prop-2-en-1-on hidrohlorida i intermedijeri koji se u njemu koriste
HRP20200426TT HRP20200426T1 (hr) 2011-10-05 2012-10-05 Postupak za pripremu 1-(4-(4-(3,4-dikloro-2-fluorofenilamino)-7-metoksikinazolin-6-iloksi)piperi din-1-il)-prop-2-en-1-on hidroklorida i posrednici koji se koriste
EP19201644.2A EP3611172A1 (en) 2011-10-05 2012-10-05 Method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one
US14/349,887 US8859767B2 (en) 2011-10-05 2012-10-05 Method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one hydrochloride and intermediates used therein
DK12838558.0T DK2763981T3 (da) 2011-10-05 2012-10-05 Fremgangsmåde til fremstilling af 1-(4-(4-(3,4-dichlor-2-fluorphenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-on-hydrochlorid og mellemprodukter anvendt deri
PL12838558T PL2763981T3 (pl) 2011-10-05 2012-10-05 Sposób wytwarzania chlorowodorku 1-(4-(4-(3,4-dichloro-2-fluorofenyloamino)-7-meto-ksychinazolin-6-yloksy)piperydyn-1-ylo)prop-2-en-1-onu i stosowane w nim związki pośrednie
HUE12838558A HUE048798T2 (hu) 2011-10-05 2012-10-05 Eljárás l-(4-(4-(3,4-diklór-2-fluorfenilamino)-7-metoxikinazolin-6-iloxi)piperidin-1-il)-prop-2-én-1-on hidroklorid elõállítására és az abban alkalmazott intermedierek
ES12838558T ES2775197T3 (es) 2011-10-05 2012-10-05 Procedimiento de preparación de clorhidrato de 1-(4-(4-(3,4-dicloro-2-fluorofenilamin)-7-metoxiquinazolin-6- iloxi)piperidin-1-il)-prop-2-en-1-ona y productos intermedios usados en el mismo
PCT/KR2012/008077 WO2013051883A2 (en) 2011-10-05 2012-10-05 Method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one hydrochloride and intermediates used therein
AU2012319291A AU2012319291B2 (en) 2011-10-05 2012-10-05 Method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one hydrochloride and intermediates used therein
IN3447DEN2014 IN2014DN03447A (enExample) 2011-10-05 2012-10-05
BR112014007718-5A BR112014007718B1 (pt) 2011-10-05 2012-10-05 Método para preparar hidrocloreto de 1-(4-(4-(3,4-dicloro-2-fluorofenilamino)-7- metoxiquinazolin-6-iloxi)piperidin-1-il)-prop-2-en-1-ona e intermediários usados no mesmo
CN201280049302.7A CN103857672B (zh) 2011-10-05 2012-10-05 用于制备1-(4-(4-(3,4-二氯-2-氟苯氨基)-7-甲氧基喹唑啉-6-基氧基)哌啶-1-基)-丙-2-烯-1-酮盐酸盐的方法及其中使用的中间产物
PT128385580T PT2763981T (pt) 2011-10-05 2012-10-05 Método de preparação de cloridrato de 1-(4-(4-(3,4-dicloro-2-fluorofenilamino)-7-metoxiquinazolin-6-iloxi)piperidin-1-il)-prop-2-en-1-ona e intermediários utilizados no mesmo
CA2850055A CA2850055C (en) 2011-10-05 2012-10-05 Method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one hydrochloride and intermediates used therein
MX2014003959A MX348815B (es) 2011-10-05 2012-10-05 Metodo para preparar clorhidrato de 1-(4-(4-(3,4-dicloro-2-fluorof enilamino)-7-metoxiquinazolin-6-iloxi)piperidin-1-il)-prop-2-en-1 -ona e intermediarios usados en el mismo.
CN201811593540.XA CN110003174A (zh) 2011-10-05 2012-10-05 一种盐酸盐化合物的制备方法
LTEP12838558.0T LT2763981T (lt) 2011-10-05 2012-10-05 1-(4-(4-(3,4-dichlor-2-fluorfenilamino)-7-metoksichinazolin-6-iloksi)piperidin-1-il)-prop-2-en-1-ono hidrochlorido gamybos būdas ir jame naudojami tarpiniai junginiai
IL231911A IL231911B (en) 2011-10-05 2014-04-03 Production method for 1-(4-(4-(4,3-dichloro-2-fluorophenylamino)-7-methoxyquinazoline-6-yloxy-piperidin-1-yl)-prop-2-en-1-one hydrochloride and intermediates used for this
IL259694A IL259694B (en) 2011-10-05 2018-05-29 Production method for 1-(4-(4-(4,3-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yl-oxy)piperidine-1-yl)-prop-2-en-1-one hydrochloride and intermediates used for this
CY20201100214T CY1122758T1 (el) 2011-10-05 2020-03-11 Μεθοδος για παρασκευη υδροχλωρικης 1-(4-(4-(3,4-διχλωρο-2-φθοροφαινυλαμινο)-7-μεθοξυκιναζολιν-6-υλοξυ)πιπεριδιν-1-υλο)-προπ-2-εν-1-ονης και ενδιαμεσων που χρησιμοποιουνται σε αυτη
IL291738A IL291738A (en) 2011-10-05 2022-03-27 Production method for 1-(4-(4-(4,3-dichloro-2-fluorophenylamino)-7-methoxyquinazoline-6-yloxy-piperidin-1-yl)-prop-2-en-1-one hydrochloride and intermediates used for this

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR1020110101422A KR101272613B1 (ko) 2011-10-05 2011-10-05 1-(4-(4-(3,4-디클로로-2-플루오로페닐아미노)-7-메톡시퀴나졸린-6-일옥시)피페리딘-1-일)프로프-2-엔-1-온 염산염의 제조 방법 및 이에 사용되는 중간체

Publications (2)

Publication Number Publication Date
KR20130037079A KR20130037079A (ko) 2013-04-15
KR101272613B1 true KR101272613B1 (ko) 2013-06-10

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ID=48044309

Family Applications (1)

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KR1020110101422A Expired - Fee Related KR101272613B1 (ko) 2011-10-05 2011-10-05 1-(4-(4-(3,4-디클로로-2-플루오로페닐아미노)-7-메톡시퀴나졸린-6-일옥시)피페리딘-1-일)프로프-2-엔-1-온 염산염의 제조 방법 및 이에 사용되는 중간체

Country Status (23)

Country Link
US (1) US8859767B2 (enExample)
EP (2) EP3611172A1 (enExample)
JP (1) JP5805880B2 (enExample)
KR (1) KR101272613B1 (enExample)
CN (2) CN110003174A (enExample)
AU (1) AU2012319291B2 (enExample)
BR (1) BR112014007718B1 (enExample)
CA (1) CA2850055C (enExample)
CY (1) CY1122758T1 (enExample)
DK (1) DK2763981T3 (enExample)
ES (1) ES2775197T3 (enExample)
HR (1) HRP20200426T1 (enExample)
HU (1) HUE048798T2 (enExample)
IL (3) IL231911B (enExample)
IN (1) IN2014DN03447A (enExample)
LT (1) LT2763981T (enExample)
MX (1) MX348815B (enExample)
PL (1) PL2763981T3 (enExample)
PT (1) PT2763981T (enExample)
RS (1) RS60118B1 (enExample)
RU (1) RU2563630C1 (enExample)
SI (1) SI2763981T1 (enExample)
WO (1) WO2013051883A2 (enExample)

Cited By (1)

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Publication number Priority date Publication date Assignee Title
KR20190012245A (ko) * 2019-01-28 2019-02-08 한미약품 주식회사 1-(4-(4-(3,4-디클로로-2-플루오로페닐아미노)-7-메톡시퀴나졸린-6-일옥시)피페리딘-1-일)프로프-2-엔-1-온의 제조방법

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KR101317809B1 (ko) 2011-06-07 2013-10-16 한미약품 주식회사 암세포의 성장을 억제하는 아마이드 유도체 및 비금속염 활택제를 포함하는 약학 조성물
KR20140096571A (ko) * 2013-01-28 2014-08-06 한미약품 주식회사 1-(4-(4-(3,4-디클로로-2-플루오로페닐아미노)-7-메톡시퀴나졸린-6-일옥시)피페리딘-1-일)프로프-2-엔-1-온의 제조방법
CN104513229A (zh) * 2013-09-28 2015-04-15 正大天晴药业集团股份有限公司 喹唑啉衍生物及其制备方法
JP6704422B2 (ja) 2015-03-20 2020-06-03 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッドChia Tai Tianqing Pharmaceutical Group Co., Ltd. キナゾリン誘導体の塩およびその製造方法
KR102802129B1 (ko) * 2018-09-14 2025-05-02 한미약품 주식회사 퀴나졸린 화합물 및 이의 염산염의 결정 형태
US20210221792A1 (en) * 2020-01-16 2021-07-22 Hanmi Pharm Co., Ltd. Convergent synthesis of poziotinib derivative
WO2022043923A1 (en) * 2020-08-28 2022-03-03 Hanmi Science Co., Ltd. Synthesis of poziotinib derivative

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KR101013319B1 (ko) * 2007-06-05 2011-02-09 한미홀딩스 주식회사 암세포 성장 억제 효과를 갖는 신규 아마이드 유도체

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WO2003082831A1 (en) * 2002-03-28 2003-10-09 Astrazeneca Ab 4-anilino quinazoline derivatives as antiproliferative agents
KR101013319B1 (ko) * 2007-06-05 2011-02-09 한미홀딩스 주식회사 암세포 성장 억제 효과를 갖는 신규 아마이드 유도체

Cited By (2)

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Publication number Priority date Publication date Assignee Title
KR20190012245A (ko) * 2019-01-28 2019-02-08 한미약품 주식회사 1-(4-(4-(3,4-디클로로-2-플루오로페닐아미노)-7-메톡시퀴나졸린-6-일옥시)피페리딘-1-일)프로프-2-엔-1-온의 제조방법
KR101950942B1 (ko) 2019-01-28 2019-02-22 한미약품 주식회사 1-(4-(4-(3,4-디클로로-2-플루오로페닐아미노)-7-메톡시퀴나졸린-6-일옥시)피페리딘-1-일)프로프-2-엔-1-온의 제조방법

Also Published As

Publication number Publication date
HUE048798T2 (hu) 2020-08-28
EP2763981A2 (en) 2014-08-13
LT2763981T (lt) 2020-05-25
ES2775197T3 (es) 2020-07-24
DK2763981T3 (da) 2020-03-16
JP2014528444A (ja) 2014-10-27
EP2763981B1 (en) 2020-01-08
CN103857672B (zh) 2018-11-30
JP5805880B2 (ja) 2015-11-10
WO2013051883A2 (en) 2013-04-11
CA2850055E (en) 2013-04-11
EP2763981A4 (en) 2015-02-25
CA2850055C (en) 2016-05-17
US20140275534A1 (en) 2014-09-18
CA2850055A1 (en) 2013-04-11
IL231911A0 (en) 2014-05-28
US8859767B2 (en) 2014-10-14
IN2014DN03447A (enExample) 2015-06-26
CN110003174A (zh) 2019-07-12
BR112014007718A2 (pt) 2017-04-25
RS60118B1 (sr) 2020-05-29
PT2763981T (pt) 2020-03-25
PL2763981T3 (pl) 2020-08-10
RU2563630C1 (ru) 2015-09-20
EP3611172A1 (en) 2020-02-19
IL259694A (en) 2018-07-31
BR112014007718B1 (pt) 2022-02-22
CY1122758T1 (el) 2021-03-12
MX2014003959A (es) 2014-05-14
CN103857672A (zh) 2014-06-11
IL291738A (en) 2022-05-01
WO2013051883A3 (en) 2013-06-06
IL231911B (en) 2018-06-28
HRP20200426T1 (hr) 2020-09-04
SI2763981T1 (sl) 2020-07-31
KR20130037079A (ko) 2013-04-15
AU2012319291A1 (en) 2014-05-22
IL259694B (en) 2022-04-01
MX348815B (es) 2017-06-30
AU2012319291B2 (en) 2016-03-31

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