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SA519401541B1 - [1، 5-a] مركبات بيرازولو كيناز ret بيريدين بها استبدال كمثبطات - Google Patents

[1، 5-a] مركبات بيرازولو كيناز ret بيريدين بها استبدال كمثبطات

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Publication number
SA519401541B1
SA519401541B1 SA519401541A SA519401541A SA519401541B1 SA 519401541 B1 SA519401541 B1 SA 519401541B1 SA 519401541 A SA519401541 A SA 519401541A SA 519401541 A SA519401541 A SA 519401541A SA 519401541 B1 SA519401541 B1 SA 519401541B1
Authority
SA
Saudi Arabia
Prior art keywords
ret kinase
kinase inhibitors
pyridine compounds
substituted pyrazolo
ret
Prior art date
Application number
SA519401541A
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English (en)
Inventor
سين ارونو
ستيفين دبليو اندريوس
باربارا جا براندبير
جيمس اف بلاك
تونى بى تانج
يوتونج جينج
لى رين
ادم كوك
جابريل ار كولاكوسكى
اليزابيث ايه مكفادين
اورين تى مكنولتى
ميجين ال مكينى
ديفيد ايه مورينو
اندريو تى ميتكالف
جوليا هاس
Original Assignee
اراى بيوفارما انك
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Publication date
Application filed by اراى بيوفارما انك filed Critical اراى بيوفارما انك
Publication of SA519401541B1 publication Critical patent/SA519401541B1/ar

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/4995Pyrazines or piperazines forming part of bridged ring 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Pyridine Compounds (AREA)

Abstract

يوفر الاختراع الحالي مركبات لها الصيغة I: I وأيزومرات تجاسمية stereoisomers وأملاح مقبولة صيدليًا أو ذوابات solvates مما سبق، حيث يكون لـ A، B، X1، X2، X3، X4، الحلقة D، وE المعاني المحددة في المواصفات، والتي تكون عبارة عن مثبطات لكيناز kinase معاد ترتيبه أثناء نقل العدوى Rearranged during Transfection (RET) وتكون مفيدة في علاج والوقاية من الأمراض التي يمكن علاجها بمثبط كيناز معاد ترتيبه أثناء نقل العدوى، والتي تتضمن الأمراض والاضطرابات المصاحبة لكيناز معاد ترتيبه أثناء نقل العدوى.
SA519401541A 2016-10-10 2019-04-10 [1، 5-a] مركبات بيرازولو كيناز ret بيريدين بها استبدال كمثبطات SA519401541B1 (ar)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201662406252P 2016-10-10 2016-10-10
US201762447850P 2017-01-18 2017-01-18
US201762491164P 2017-04-27 2017-04-27
US201762554817P 2017-09-06 2017-09-06
US201762566093P 2017-09-29 2017-09-29
PCT/US2017/055983 WO2018071447A1 (en) 2016-10-10 2017-10-10 Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors

Publications (1)

Publication Number Publication Date
SA519401541B1 true SA519401541B1 (ar) 2022-08-04

Family

ID=60153575

Family Applications (1)

Application Number Title Priority Date Filing Date
SA519401541A SA519401541B1 (ar) 2016-10-10 2019-04-10 [1، 5-a] مركبات بيرازولو كيناز ret بيريدين بها استبدال كمثبطات

Country Status (39)

Country Link
US (8) US10112942B2 (ar)
EP (2) EP3523301B1 (ar)
JP (5) JP6776446B2 (ar)
KR (1) KR102143899B1 (ar)
CN (2) CN110382494B (ar)
AU (1) AU2017342022B2 (ar)
BR (1) BR112019007144B8 (ar)
CA (1) CA3039760C (ar)
CL (1) CL2019000941A1 (ar)
CO (1) CO2019004650A2 (ar)
CR (1) CR20190218A (ar)
CY (1) CY1123201T1 (ar)
DK (1) DK3523301T3 (ar)
DO (1) DOP2019000090A (ar)
EC (1) ECSP19032676A (ar)
ES (1) ES2805087T3 (ar)
HR (1) HRP20201008T1 (ar)
HU (1) HUE051424T2 (ar)
IL (2) IL265916B (ar)
JO (1) JOP20190076B1 (ar)
LT (1) LT3523301T (ar)
MA (1) MA53675A (ar)
MD (1) MD3523301T2 (ar)
MX (2) MX2020011250A (ar)
MY (1) MY195573A (ar)
NZ (1) NZ752793A (ar)
PE (1) PE20190918A1 (ar)
PH (1) PH12019500775A1 (ar)
PL (1) PL3523301T3 (ar)
PT (1) PT3523301T (ar)
RS (1) RS60536B1 (ar)
SA (1) SA519401541B1 (ar)
SG (1) SG11201903144PA (ar)
SI (1) SI3523301T1 (ar)
TN (1) TN2019000110A1 (ar)
TW (1) TWI704148B (ar)
UA (1) UA125030C2 (ar)
WO (1) WO2018071447A1 (ar)
ZA (1) ZA202004040B (ar)

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