JO3805B1 - مثبطات كراس جي12سي - Google Patents

مثبطات كراس جي12سي

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Publication number
JO3805B1
JO3805B1 JOP/2014/0289A JOP20140289A JO3805B1 JO 3805 B1 JO3805 B1 JO 3805B1 JO P20140289 A JOP20140289 A JO P20140289A JO 3805 B1 JO3805 B1 JO 3805B1
Authority
JO
Jordan
Prior art keywords
compounds
inhibitors
activity
kras
mutant kras
Prior art date
Application number
JOP/2014/0289A
Other languages
English (en)
Inventor
Yi Liu
Yuan Liu
Tao Wu
Yun Oliver Long
Liansheng Li
Pingda Ren
Jun Feng
Original Assignee
Araxes Pharma Llc
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 Araxes Pharma Llc filed Critical Araxes Pharma Llc
Priority to KR1020167011577A priority Critical patent/KR20160076519A/ko
Priority to EP14799915.5A priority patent/EP3055290B1/en
Priority to EP19195037.7A priority patent/EP3636639A1/en
Priority to JP2016521333A priority patent/JP6559123B2/ja
Priority to CA2926328A priority patent/CA2926328C/en
Priority to CN201480055783.1A priority patent/CN106488910B/zh
Priority to BR112016008016A priority patent/BR112016008016B8/pt
Priority to UAA201605067A priority patent/UA119971C2/uk
Priority to MX2016004360A priority patent/MX2016004360A/es
Priority to AU2014331794A priority patent/AU2014331794C1/en
Priority to PCT/US2014/060036 priority patent/WO2015054572A1/en
Priority to NZ719076A priority patent/NZ719076B2/en
Priority to SG11201602662YA priority patent/SG11201602662YA/en
Priority to MYPI2016701035A priority patent/MY188058A/en
Priority to EA201690752A priority patent/EA033689B9/ru
Priority to PH12016500538A priority patent/PH12016500538A1/en
Priority to IL244699A priority patent/IL244699B/en
Priority to ZA2016/02245A priority patent/ZA201602245B/en
Priority to NI201600049A priority patent/NI201600049A/es
Priority to NO20160646A priority patent/NO20160646A1/en
Publication of JO3805B1 publication Critical patent/JO3805B1/ar
Application granted granted Critical

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    • C07ORGANIC CHEMISTRY
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    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
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    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
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    • C07D241/40Benzopyrazines
    • C07D241/44Benzopyrazines 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 carbon atoms of the hetero ring
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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

يتم تقديم المركبات التي لها نشاط كمثبطات لبروتين <span dir="LTR">KRAS</span> المطفر <span dir="LTR">G12C</span>. المركبات التي لها التركيبة التالية (<span dir="LTR">I</span>): <span dir="RTL">أو ملح، صنو، دواء مساعد أو مصاوغ مرآتي مقبول صيدلانيا منه حيث</span> R1,R2a, R3a, R3b,R4a,R4b,G1,L1,L2,m1,m2,A,B,W,X,Y,Z و E <span dir="RTL">كما هو محدد في هذا الاختراع. يتم تقديم الطرق المرتبطة بتحضير واستخدام هذه المركبات، التركيبات الصيدلانية تتضمن هذه المركبات وطرق لتعديل نشاط بروتين </span>KRAS<span dir="RTL"> المطفر </span>G12C<span dir="RTL"> لعلاج الاضطرابات، مثل السرطان، أيضا. </span>
JOP/2014/0289A 2013-10-10 2014-10-09 مثبطات كراس جي12سي JO3805B1 (ar)

Priority Applications (20)

Application Number Priority Date Filing Date Title
NZ719076A NZ719076B2 (en) 2013-10-10 2014-10-10 Inhibitors of kras g12c
EP14799915.5A EP3055290B1 (en) 2013-10-10 2014-10-10 Inhibitors of kras g12c
JP2016521333A JP6559123B2 (ja) 2013-10-10 2014-10-10 Krasg12cの阻害剤
CA2926328A CA2926328C (en) 2013-10-10 2014-10-10 Substituted quinazolinyl and quinolinyl derivatives and pharmaceutical compositions thereof useful as inhibitors of kras g12c
CN201480055783.1A CN106488910B (zh) 2013-10-10 2014-10-10 Kras g12c的抑制剂
BR112016008016A BR112016008016B8 (pt) 2013-10-10 2014-10-10 Compostos inibidores de kras g12c, composição farmacêutica compreendendo ditos compostos, métodos para regular a atividade e para preparar uma proteína mutante kras, hras ou nras g12c, método para inibir a proliferação de uma população de células e usos terapêuticos dos ditos compostos
UAA201605067A UA119971C2 (uk) 2013-10-10 2014-10-10 Інгібітори g12c kras
SG11201602662YA SG11201602662YA (en) 2013-10-10 2014-10-10 Inhibitors of kras g12c
KR1020167011577A KR20160076519A (ko) 2013-10-10 2014-10-10 Kras g12c 억제제
AU2014331794A AU2014331794C1 (en) 2013-10-10 2014-10-10 Inhibitors of KRAS G12C
EP19195037.7A EP3636639A1 (en) 2013-10-10 2014-10-10 Inhibitors of kras g12c
MX2016004360A MX2016004360A (es) 2013-10-10 2014-10-10 Inhibidores de kras g12c.
MYPI2016701035A MY188058A (en) 2013-10-10 2014-10-10 Inhibitors of kras g12c
EA201690752A EA033689B9 (ru) 2013-10-10 2014-10-10 Ингибиторы g12c kras
PCT/US2014/060036 WO2015054572A1 (en) 2013-10-10 2014-10-10 Inhibitors of kras g12c
PH12016500538A PH12016500538A1 (en) 2013-10-10 2016-03-21 Inhibitors of kras g12c
IL244699A IL244699B (en) 2013-10-10 2016-03-21 kras g12c inhibitors
ZA2016/02245A ZA201602245B (en) 2013-10-10 2016-04-05 Inhibitors of kras g12c
NI201600049A NI201600049A (es) 2013-10-10 2016-04-08 Inhibidores de kras g12c
NO20160646A NO20160646A1 (en) 2013-10-10 2016-04-19 Inhibitors of kras g12c

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361889460P 2013-10-10 2013-10-10
US201462034619P 2014-08-07 2014-08-07
US201462052366P 2014-09-18 2014-09-18

Publications (1)

Publication Number Publication Date
JO3805B1 true JO3805B1 (ar) 2021-01-31

Family

ID=53491698

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2014/0289A JO3805B1 (ar) 2013-10-10 2014-10-09 مثبطات كراس جي12سي

Country Status (6)

Country Link
US (7) US9840516B2 (ar)
CR (1) CR20160205A (ar)
EA (1) EA201991884A3 (ar)
JO (1) JO3805B1 (ar)
TW (1) TWI659021B (ar)
UY (1) UY35781A (ar)

Families Citing this family (83)

* Cited by examiner, † Cited by third party
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WO2014143659A1 (en) 2013-03-15 2014-09-18 Araxes Pharma Llc Irreversible covalent inhibitors of the gtpase k-ras g12c
US9227978B2 (en) 2013-03-15 2016-01-05 Araxes Pharma Llc Covalent inhibitors of Kras G12C
TWI659021B (zh) 2013-10-10 2019-05-11 亞瑞克西斯製藥公司 Kras g12c之抑制劑
JO3556B1 (ar) 2014-09-18 2020-07-05 Araxes Pharma Llc علاجات مدمجة لمعالجة السرطان
US10011600B2 (en) 2014-09-25 2018-07-03 Araxes Pharma Llc Methods and compositions for inhibition of Ras
EP3197870B1 (en) 2014-09-25 2020-08-19 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
WO2016164675A1 (en) 2015-04-10 2016-10-13 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
US10428064B2 (en) 2015-04-15 2019-10-01 Araxes Pharma Llc Fused-tricyclic inhibitors of KRAS and methods of use thereof
CN106366093B (zh) * 2015-07-21 2020-08-18 广州再极医药科技有限公司 稠环嘧啶类化合物、中间体、其制备方法、组合物和应用
US10144724B2 (en) * 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
HUE060733T2 (hu) 2015-07-31 2023-04-28 Taiho Pharmaceutical Co Ltd Pirrolo[2,3-d]pirimidin vegyület vagy annak sója
WO2017058805A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10647703B2 (en) 2015-09-28 2020-05-12 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058728A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
US10875842B2 (en) 2015-09-28 2020-12-29 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
US10975071B2 (en) 2015-09-28 2021-04-13 Araxes Pharma Llc Inhibitors of KRAS G12C mutant proteins
WO2017058902A1 (en) 2015-09-28 2017-04-06 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
EP3356359B1 (en) 2015-09-28 2021-10-20 Araxes Pharma LLC Inhibitors of kras g12c mutant proteins
EP3364977A4 (en) 2015-10-19 2019-09-04 Araxes Pharma LLC PROCESS FOR SCREENING INHIBITORS OF RAS
JP7015059B2 (ja) * 2015-11-16 2022-02-15 アラクセス ファーマ エルエルシー 置換複素環式基を含む2-置換キナゾリン化合物およびその使用方法
US9988357B2 (en) 2015-12-09 2018-06-05 Araxes Pharma Llc Methods for preparation of quinazoline derivatives
BR112018012914B1 (pt) 2015-12-22 2023-04-18 SHY Therapeutics LLC Composto, uso de um composto e composição farmacêutica
US10822312B2 (en) 2016-03-30 2020-11-03 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
JP7039489B2 (ja) 2016-05-18 2022-03-22 ミラティ セラピューティクス, インコーポレイテッド Kras g12c阻害剤
US10646488B2 (en) 2016-07-13 2020-05-12 Araxes Pharma Llc Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof
CN109715612B (zh) 2016-07-14 2022-09-16 克林提克斯医药股份有限公司 促生长素抑制素调节剂及其用途
CN106278918B (zh) * 2016-08-12 2018-05-11 合肥久诺医药科技有限公司 一种溴芬酸钠杂质标准品2-氨基-3-(4-溴苯甲酰基)苯甲酸的合成方法
WO2018064510A1 (en) 2016-09-29 2018-04-05 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
CN110312711A (zh) * 2016-10-07 2019-10-08 亚瑞克西斯制药公司 作为ras抑制剂的杂环化合物及其使用方法
HUE056777T2 (hu) * 2016-12-22 2022-03-28 Amgen Inc Benzizotiazol-, izotiazolo[3,4-b]piridin-, kinazolin-, ftálazin-, pirido[2,3-d]piridazin- és pirido[2,3-d]pirimidin-származékok mint KRAS G12C inhibitorok tüdõ-, hasnyálmirigy- vagy vastagbélrák kezelésére
US11358959B2 (en) 2017-01-26 2022-06-14 Araxes Pharma Llc Benzothiophene and benzothiazole compounds and methods of use thereof
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