BR112016008016B8 - 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 - Google Patents

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

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Publication number
BR112016008016B8
BR112016008016B8 BR112016008016A BR112016008016A BR112016008016B8 BR 112016008016 B8 BR112016008016 B8 BR 112016008016B8 BR 112016008016 A BR112016008016 A BR 112016008016A BR 112016008016 A BR112016008016 A BR 112016008016A BR 112016008016 B8 BR112016008016 B8 BR 112016008016B8
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BR
Brazil
Prior art keywords
compounds
kras
activity
methods
hras
Prior art date
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BR112016008016A
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English (en)
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BR112016008016A2 (pt
BR112016008016B1 (pt
Inventor
Jun Feng
Liansheng Li
Pingda Ren
Tao Wu
Yi Liu
Yuan Liu
Oliver Long Yun
Original Assignee
Araxes Pharma Llc
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Priority claimed from JOP/2014/0289A external-priority patent/JO3805B1/ar
Application filed by Araxes Pharma Llc filed Critical Araxes Pharma Llc
Publication of BR112016008016A2 publication Critical patent/BR112016008016A2/pt
Publication of BR112016008016B1 publication Critical patent/BR112016008016B1/pt
Publication of BR112016008016B8 publication Critical patent/BR112016008016B8/pt

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    • 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
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    • 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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    • 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
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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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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    • A61P35/02—Antineoplastic agents specific for leukemia
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    • 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
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    • 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
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    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
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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
    • C07D401/04—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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    • C07D401/00—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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    • C07D417/12—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 chain containing hetero atoms as chain links
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    • C07D417/14—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 three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
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    • C07D495/04—Ortho-condensed systems

Abstract

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. são proporcionados compostos tendo atividade como inibidores da proteína kras mutante g12c. os compostos têm a seguinte estrutura (i): ou um sal farmaceuticamente aceitável, tautômero, pró-medicamento ou estereoisômero deles, onde r1, r2a, r3a, r3b, r4a, r4b, g1, g2, l1, l2, m1, m2, a, b, w, x, y, z e e são como definidos neste documento. são também proporcionados métodos associados com a preparação e o uso de tais compostos, composições farmacêuticas compreendendo tais compostos e métodos para modular a atividade da proteína kras mutante g12c para o tratamento de distúrbios, tais como o câncer.
BR112016008016A 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 BR112016008016B8 (pt)

Applications Claiming Priority (11)

Application Number Priority Date Filing Date Title
US201361889460P 2013-10-10 2013-10-10
US61/889,460 2013-10-10
US201462034619P 2014-08-07 2014-08-07
US62/034,619 2014-08-07
US201462052366P 2014-09-18 2014-09-18
US62/052.366 2014-09-18
TW103135318 2014-10-09
JOP/2014/0289A JO3805B1 (ar) 2013-10-10 2014-10-09 مثبطات كراس جي12سي
JO289/2014 2014-10-09
TW103135318A TWI659021B (zh) 2013-10-10 2014-10-09 Ｋｒａｓ ｇ１２ｃ之抑制劑
PCT/US2014/060036 WO2015054572A1 (en) 2013-10-10 2014-10-10 Inhibitors of kras g12c

Publications (3)

Publication Number Publication Date
BR112016008016A2 BR112016008016A2 (pt) 2017-09-12
BR112016008016B1 BR112016008016B1 (pt) 2021-01-19
BR112016008016B8 true BR112016008016B8 (pt) 2023-09-26

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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

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EP (2) EP3636639A1 (pt)
JP (1) JP6559123B2 (pt)
KR (1) KR20160076519A (pt)
CN (1) CN106488910B (pt)
AU (1) AU2014331794C1 (pt)
BR (1) BR112016008016B8 (pt)
CA (1) CA2926328C (pt)
EA (1) EA033689B9 (pt)
IL (1) IL244699B (pt)
MX (1) MX2016004360A (pt)
NI (1) NI201600049A (pt)
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UA (1) UA119971C2 (pt)
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AR102094A1 (es) * 2014-09-25 2017-02-01 Araxes Pharma Llc Inhibidores de proteínas kras con una mutación g12c
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