TWI683807B - 作為轉染重排（ｒｅｔ）抑制劑之新穎化合物 - Google Patents

作為轉染重排（ｒｅｔ）抑制劑之新穎化合物 Download PDF

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TWI683807B
TWI683807B TW104129876A TW104129876A TWI683807B TW I683807 B TWI683807 B TW I683807B TW 104129876 A TW104129876 A TW 104129876A TW 104129876 A TW104129876 A TW 104129876A TW I683807 B TWI683807 B TW I683807B
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Taiwan
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compound
formula
weight
cancer
ethoxy
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TW104129876A
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Chinese (zh)
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TW201625534A (en
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麥可 迪麥提諾
關慧萍
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英商葛蘭素史克智慧財產發展有限公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/69—Two or more oxygen 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • 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
    • 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
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
TW104129876A 2014-09-10 2015-09-10 作為轉染重排（ｒｅｔ）抑制劑之新穎化合物 TWI683807B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
WOPCT/CN2014/086197 2014-09-10
CN2014086197 2014-09-10
WOPCT/CN2015/086995 2015-08-14
CN2015086995 2015-08-14

Publications (2)

Publication Number Publication Date
TW201625534A TW201625534A (en) 2016-07-16
TWI683807B true TWI683807B (zh) 2020-02-01

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TW104129876A TWI683807B (zh) 2014-09-10 2015-09-10 作為轉染重排（ｒｅｔ）抑制劑之新穎化合物

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Country Link
US (4) US9918974B2 (https=)
EP (2) EP3517526B1 (https=)
JP (2) JP6538154B2 (https=)
KR (1) KR20170045350A (https=)
CN (1) CN107074768B (https=)
AU (1) AU2015313841B2 (https=)
BR (1) BR112017004900A2 (https=)
CA (1) CA2960768A1 (https=)
CL (1) CL2017000588A1 (https=)
CO (1) CO2017002273A2 (https=)
CR (1) CR20170093A (https=)
CY (1) CY1121661T1 (https=)
DK (1) DK3191450T3 (https=)
DO (1) DOP2017000059A (https=)
EA (1) EA033544B1 (https=)
ES (2) ES2725704T3 (https=)
HR (1) HRP20190815T1 (https=)
HU (1) HUE044604T2 (https=)
IL (1) IL250908B (https=)
LT (1) LT3191450T (https=)
MA (1) MA40581A (https=)
ME (1) ME03432B (https=)
MX (1) MX373863B (https=)
MY (1) MY181913A (https=)
PE (1) PE20170705A1 (https=)
PH (1) PH12017500425A1 (https=)
PL (1) PL3191450T3 (https=)
PT (1) PT3191450T (https=)
RS (1) RS58813B1 (https=)
SG (1) SG11201701694QA (https=)
SI (1) SI3191450T1 (https=)
SM (1) SMT201900304T1 (https=)
TW (1) TWI683807B (https=)
UA (1) UA122213C2 (https=)
UY (1) UY36293A (https=)
WO (1) WO2016038552A1 (https=)

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TWI752098B (zh) 2016-10-10 2022-01-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
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JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
JP2020519672A (ja) 2017-05-15 2020-07-02 ブループリント メディシンズ コーポレイション ＲＥＴ阻害剤とｍＴＯＲＣ１阻害剤との組合せ及び異常なＲＥＴ活性によって媒介されるがんを処置するためのその使用
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
TWI876442B (zh) 2017-10-10 2025-03-11 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
US11472802B2 (en) 2018-01-18 2022-10-18 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors
JP7060694B2 (ja) 2018-01-18 2022-04-26 アレイ バイオファーマ インコーポレイテッド Ｒｅｔキナーゼ阻害剤としての置換ピロロ［２，３－ｄ］ピリミジン化合物
EP3740490A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
PE20210096A1 (es) 2018-04-03 2021-01-12 Blueprint Medicines Corp Inhibidor de ret para uso en tratar cancer que tiene una alteracion de ret
CN112996794A (zh) 2018-09-10 2021-06-18 阿雷生物药品公司 作为ret激酶抑制剂的稠合杂环化合物
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WO2016038552A1 (en) 2016-03-17
AU2015313841B2 (en) 2018-03-08
PH12017500425B1 (en) 2017-07-31
DK3191450T3 (da) 2019-05-20
SG11201701694QA (en) 2017-04-27
MY181913A (en) 2021-01-14
US20180147194A1 (en) 2018-05-31
DOP2017000059A (es) 2017-03-31
EP3517526A1 (en) 2019-07-31
US9918974B2 (en) 2018-03-20
US20190022078A1 (en) 2019-01-24
HRP20190815T1 (hr) 2019-07-12
US20190247382A1 (en) 2019-08-15
JP2017527578A (ja) 2017-09-21
TW201625534A (en) 2016-07-16
CL2017000588A1 (es) 2017-10-06
CN107074768A (zh) 2017-08-18
LT3191450T (lt) 2019-06-10
EA201790546A1 (ru) 2017-07-31
ME03432B (me) 2020-01-20
CO2017002273A2 (es) 2017-06-20
JP6538154B2 (ja) 2019-07-03
MX2017003114A (es) 2017-11-15
SMT201900304T1 (it) 2019-07-11
ES2725704T3 (es) 2019-09-26
IL250908B (en) 2020-11-30
US20170340617A1 (en) 2017-11-30
CN107074768B (zh) 2019-12-10
BR112017004900A2 (pt) 2017-12-12
US10709695B2 (en) 2020-07-14
JP2019163316A (ja) 2019-09-26
JP6728447B2 (ja) 2020-07-22
HUE044604T2 (hu) 2019-11-28
UA122213C2 (uk) 2020-10-12
PL3191450T3 (pl) 2019-08-30
ES2816453T3 (es) 2021-04-05
PT3191450T (pt) 2019-05-29
SI3191450T1 (sl) 2019-07-31
PH12017500425A1 (en) 2017-07-31
US10292975B2 (en) 2019-05-21
PE20170705A1 (es) 2017-05-21
AU2015313841A1 (en) 2017-03-23
US10111866B2 (en) 2018-10-30
EP3517526B1 (en) 2020-08-19
KR20170045350A (ko) 2017-04-26
MX373863B (es) 2020-03-26
EP3191450B1 (en) 2019-04-10
IL250908A0 (en) 2017-04-30
RS58813B1 (sr) 2019-07-31
CR20170093A (es) 2017-07-17
EA033544B1 (ru) 2019-10-31
MA40581A (fr) 2019-04-10
CA2960768A1 (en) 2016-03-17
CY1121661T1 (el) 2020-07-31
EP3191450A1 (en) 2017-07-19
UY36293A (es) 2016-04-01

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