JO3707B1 - مركبات كينازولين مستبدلة وطرق استعمالها - Google Patents

مركبات كينازولين مستبدلة وطرق استعمالها

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Publication number
JO3707B1
JO3707B1 JOP/2016/0068A JOP20160068A JO3707B1 JO 3707 B1 JO3707 B1 JO 3707B1 JO P20160068 A JOP20160068 A JO P20160068A JO 3707 B1 JO3707 B1 JO 3707B1
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Jordan
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methods
compounds
quinazoline compounds
substituted quinazoline
iii
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JOP/2016/0068A
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English (en)
Inventor
Pingda Ren
Yuan Liu
Jun Feng
Liansheng Li
Yun Oliver Long
Yi Liu
Tao Wu
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Araxes Pharma Llc
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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
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    • 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
    • C07D239/74—Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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
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    • C07D239/72—Quinazolines; Hydrogenated quinazolines
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    • 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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    • 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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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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    • 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
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom

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  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

يتعلق الاختراع الحالي بالمركبات التي لها نشاط على هيئة مثبطات بروتين <span dir="LTR">KRAS</span> بطفرة <span dir="LTR">G12C</span>. يكون للمركبات إحدى البنيات التالية (<span dir="LTR">I</span>)، (<span dir="LTR">II</span>) أو (<span dir="LTR">III</span>): أو ملح مقبول صيدلانيا، متجاسم أو عقار أولى منها، حيث <span dir="LTR">R1, R2a, R2b,R2c,R3a, R3b, R4a, R4b, R5a, R5b, R6, A, B, G1, G2, L1, L2, m1, m2, n, x, y, X</span> هي كما تم تعريفها هنا. <span dir="RTL">يتم توفير طرق مرتبطة بتحضير و استخدام تلك المركبات، التركيبات الصيدلانية التي تشتمل على تلك المركبات و طرق لتعديل نشاط بروتين </span>KRAS<span dir="RTL"> بطفرة </span>G12C<span dir="RTL"> لمعالجة اضطرابات ، مثل سرطان، أيضا.</span>
JOP/2016/0068A 2015-04-10 2016-04-10 مركبات كينازولين مستبدلة وطرق استعمالها JO3707B1 (ar)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562145818P 2015-04-10 2015-04-10
US201562145705P 2015-04-10 2015-04-10
US201562255891P 2015-11-16 2015-11-16
US201562265320P 2015-12-09 2015-12-09
US201562265316P 2015-12-09 2015-12-09

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JO3707B1 true JO3707B1 (ar) 2021-01-31

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US (2) US10246424B2 (ar)
EP (1) EP3280708B1 (ar)
JP (2) JP2018513853A (ar)
KR (1) KR20180005178A (ar)
CN (1) CN107849022A (ar)
AU (1) AU2016245864C1 (ar)
BR (1) BR112017021869A2 (ar)
CA (1) CA2981530A1 (ar)
EA (1) EA201792214A1 (ar)
ES (1) ES2898765T3 (ar)
HK (1) HK1248231A1 (ar)
JO (1) JO3707B1 (ar)
MX (1) MX2017012979A (ar)
TW (1) TW201702232A (ar)
UY (1) UY36612A (ar)
WO (1) WO2016164675A1 (ar)

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