JO3805B1 - مثبطات كراس جي12سي - Google Patents

مثبطات كراس جي12سي

Info

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 EP14799915.5A priority Critical patent/EP3055290B1/en
Priority to CA2926328A priority patent/CA2926328C/en
Priority to PCT/US2014/060036 priority patent/WO2015054572A1/en
Priority to AU2014331794A priority patent/AU2014331794C1/en
Priority to MX2016004360A priority patent/MX380928B/es
Priority to BR112016008016A priority patent/BR112016008016B8/pt
Priority to SG11201602662YA priority patent/SG11201602662YA/en
Priority to JP2016521333A priority patent/JP6559123B2/ja
Priority to KR1020167011577A priority patent/KR20160076519A/ko
Priority to EA201690752A priority patent/EA033689B9/ru
Priority to MYPI2016701035A priority patent/MY188058A/en
Priority to CN201480055783.1A priority patent/CN106488910B/zh
Priority to EP19195037.7A priority patent/EP3636639A1/en
Priority to UAA201605067A priority patent/UA119971C2/uk
Priority to NZ719076A priority patent/NZ719076B2/en
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
Application granted granted Critical
Publication of JO3805B1 publication Critical patent/JO3805B1/ar

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • C07D215/46—Nitrogen atoms attached in position 4 with hydrocarbon radicals, substituted by nitrogen atoms, attached to said nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic 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
    • C07D215/16—Heterocyclic 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/28—Cinnolines
    • 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
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
    • 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
    • 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
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines 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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    • 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
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    • 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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • C07D403/10—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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • 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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    • 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
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D417/02—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 two hetero rings
    • C07D417/10—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 two hetero rings linked by a carbon chain containing aromatic rings
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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
MYPI2016701035A MY188058A (en) 2013-10-10 2014-10-10 Inhibitors of kras g12c
PCT/US2014/060036 WO2015054572A1 (en) 2013-10-10 2014-10-10 Inhibitors of kras g12c
AU2014331794A AU2014331794C1 (en) 2013-10-10 2014-10-10 Inhibitors of KRAS G12C
MX2016004360A MX380928B (es) 2013-10-10 2014-10-10 Inhibidores de kras g12c.
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
SG11201602662YA SG11201602662YA (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
KR1020167011577A KR20160076519A (ko) 2013-10-10 2014-10-10 Kras g12c 억제제
EP14799915.5A EP3055290B1 (en) 2013-10-10 2014-10-10 Inhibitors of kras g12c
CN201480055783.1A CN106488910B (zh) 2013-10-10 2014-10-10 Kras g12c的抑制剂
CA2926328A CA2926328C (en) 2013-10-10 2014-10-10 Substituted quinazolinyl and quinolinyl derivatives and pharmaceutical compositions thereof useful as inhibitors of kras g12c
EA201690752A EA033689B9 (ru) 2013-10-10 2014-10-10 Ингибиторы g12c kras
UAA201605067A UA119971C2 (uk) 2013-10-10 2014-10-10 Інгібітори g12c kras
NZ719076A NZ719076B2 (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
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 (8) US9840516B2 (ar)
CR (1) CR20160205A (ar)
EA (1) EA201991884A3 (ar)
JO (1) JO3805B1 (ar)
TW (1) TWI659021B (ar)
UY (1) UY35781A (ar)

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JO3805B1 (ar) 2013-10-10 2021-01-31 Araxes Pharma Llc مثبطات كراس جي12سي
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NZ754994A (en) * 2016-12-22 2022-12-23 Amgen Inc Benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer
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