JO3067B1 - بيرميدينات بيرازولو امينو كمثبطات ل fak - Google Patents

بيرميدينات بيرازولو امينو كمثبطات ل fak

Info

Publication number
JO3067B1
JO3067B1 JOP/2009/0395A JOP20090395A JO3067B1 JO 3067 B1 JO3067 B1 JO 3067B1 JO P20090395 A JOP20090395 A JO P20090395A JO 3067 B1 JO3067 B1 JO 3067B1
Authority
JO
Jordan
Prior art keywords
fak
inhibitors
amino pyrimidines
pyrimidine amino
pyrimidine
Prior art date
Application number
JOP/2009/0395A
Other languages
English (en)
Inventor
H Faitg Thomas
Leroy Adams Jerry
W Johnson Neil
Lin Hong
Original Assignee
Glaxosmithkline 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42132177&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=JO3067(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Glaxosmithkline Llc filed Critical Glaxosmithkline Llc
Application granted granted Critical
Publication of JO3067B1 publication Critical patent/JO3067B1/ar

Links

Classifications

    • 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
    • A61K31/435—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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • 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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/435—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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D401/14—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 three or more hetero rings
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/575—Immunoassay; Biospecific binding assay; Materials therefor for cancer
    • G01N33/5752—Immunoassay; Biospecific binding assay; Materials therefor for cancer of the lungs

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Cell Biology (AREA)
  • Microbiology (AREA)
  • Pathology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

يتعلق الاختراع الحالي لمركب الصياغة(I): (I) أو ملح مقبول صيدلانيا لهم, حيث R1, R2, R3, R11, R12, R13, Q, Z وp هم كما وصف هنا. مركبات الاختراع الحالي تكون مفيدة لعلاج السرطانات.
JOP/2009/0395A 2008-10-27 2009-10-25 بيرميدينات بيرازولو امينو كمثبطات ل fak JO3067B1 (ar)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US10856808P 2008-10-27 2008-10-27
US17851709P 2009-05-15 2009-05-15
US24243209P 2009-09-15 2009-09-15

Publications (1)

Publication Number Publication Date
JO3067B1 true JO3067B1 (ar) 2017-03-15

Family

ID=42132177

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2009/0395A JO3067B1 (ar) 2008-10-27 2009-10-25 بيرميدينات بيرازولو امينو كمثبطات ل fak

Country Status (35)

Country Link
US (6) US20100113475A1 (ar)
EP (1) EP2421537B1 (ar)
JP (1) JP5642689B2 (ar)
KR (1) KR101512217B1 (ar)
CN (1) CN102264371B (ar)
AR (1) AR073993A1 (ar)
AU (1) AU2009320144B2 (ar)
BR (1) BRPI0920053B8 (ar)
CA (1) CA2741760C (ar)
CL (1) CL2011000933A1 (ar)
CO (1) CO6361929A2 (ar)
CR (1) CR20110264A (ar)
CY (1) CY1116399T1 (ar)
DK (1) DK2421537T3 (ar)
DO (1) DOP2011000113A (ar)
EA (1) EA021927B1 (ar)
ES (1) ES2539835T3 (ar)
HR (1) HRP20150531T1 (ar)
IL (1) IL212444A (ar)
JO (1) JO3067B1 (ar)
MA (1) MA32727B1 (ar)
MX (1) MX2011004369A (ar)
MY (1) MY161890A (ar)
NZ (1) NZ592477A (ar)
PE (1) PE20110941A1 (ar)
PL (1) PL2421537T3 (ar)
PT (1) PT2421537E (ar)
RS (1) RS54045B1 (ar)
SG (1) SG195608A1 (ar)
SI (1) SI2421537T1 (ar)
SM (1) SMT201500157B (ar)
TW (1) TWI454467B (ar)
UY (1) UY32200A (ar)
WO (1) WO2010062578A1 (ar)
ZA (1) ZA201102892B (ar)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8338441B2 (en) 2009-05-15 2012-12-25 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication
US20120244141A1 (en) 2010-09-28 2012-09-27 Boehringer Ingelheim International Gmbh Stratification of cancer patients for susceptibility to therapy with PTK2 inhibitors
EA201391076A1 (ru) * 2011-01-26 2014-07-30 Глэксосмитклайн Интеллекчуал Проперти Лимитед Комбинации
DK2675793T3 (en) 2011-02-17 2018-11-12 Cancer Therapeutics Crc Pty Ltd FAK INHIBITORS
EP2675794B1 (en) 2011-02-17 2019-02-13 Cancer Therapeutics Crc Pty Limited Selective fak inhibitors
WO2013003575A1 (en) * 2011-06-28 2013-01-03 Glaxosmithkline Llc Method of administration and treatment
WO2015054477A1 (en) 2013-10-09 2015-04-16 The General Hospital Corporation Methods of diagnosing and treating b cell acute lymphoblastic leukemia
CN108289892B (zh) 2015-06-29 2021-11-23 维瑞斯特姆股份有限公司 治疗组合物、组合和使用方法
CN108948019B (zh) * 2017-05-18 2022-07-08 广东东阳光药业有限公司 黏着斑激酶抑制剂及其用途
WO2019117813A1 (en) * 2017-12-15 2019-06-20 National University Of Singapore Focal adhesion kinase targeted therapeutics for the treatment of glaucoma and fibrosis
EP3765085A1 (en) 2018-03-12 2021-01-20 Université de Paris Use of caloric restriction mimetics for potentiating chemo-immunotherapy for the treatment of cancers
CN108912095B (zh) * 2018-08-09 2019-08-20 广州安岩仁医药科技有限公司 苯并咪唑类化合物及其制备方法和应用
WO2020069117A1 (en) * 2018-09-27 2020-04-02 Dana-Farber Cancer Institute, Inc. Degradation of fak or fak and alk by conjugation of fak and alk inhibitors with e3 ligase ligands and methods of use
CN111377871B (zh) * 2018-12-27 2021-03-19 海创药业股份有限公司 一种fak抑制剂及其联合用药物
US12187722B2 (en) * 2019-03-15 2025-01-07 The General Hospital Corporation Small molecule inhibitors of TEAD transcription factors
CN113387947B (zh) * 2021-07-12 2022-07-01 中国科学院成都生物研究所 调节雌激素受体合成活性的吡唑并吡啶衍生物
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ｒａｓ抑制劑
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
CN119499253A (zh) * 2024-11-15 2025-02-25 贵州医科大学 一种化合物在抑制Aurora和JAK激酶家族活性及在几种肿瘤治疗方面的应用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US166139A (en) * 1875-07-27 Improvement in dental pluggers
EP1109823B1 (en) * 1998-09-08 2005-11-16 Agouron Pharmaceuticals, Inc. Modifications of the vegf receptor-2 protein and methods of use
US7102009B2 (en) * 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
BR122019017579B8 (pt) * 2003-08-15 2021-07-27 Novartis Ag 2,4-pirimidinadiaminas, seus usos, combinação e composição farmacêutica
GB0419161D0 (en) * 2004-08-27 2004-09-29 Novartis Ag Organic compounds
GB0419160D0 (en) * 2004-08-27 2004-09-29 Novartis Ag Organic compounds
EP1746096A1 (en) * 2005-07-15 2007-01-24 4Sc Ag 2-Arylbenzothiazole analogues and uses thereof in the treatment of cancer
JP5569956B2 (ja) * 2007-03-16 2014-08-13 ザ スクリプス リサーチ インスティテュート 接着斑キナーゼのインヒビター
US20100317663A1 (en) * 2008-02-19 2010-12-16 Jerry Leroy Adams Anilinopyridines as inhibitors of fak
CN102124000B (zh) * 2008-06-17 2014-09-17 阿斯利康(瑞典)有限公司 吡啶化合物

Also Published As

Publication number Publication date
CA2741760C (en) 2016-02-23
IL212444A0 (en) 2011-06-30
EP2421537A4 (en) 2012-06-13
CY1116399T1 (el) 2017-02-08
US20100113475A1 (en) 2010-05-06
EA201170617A1 (ru) 2011-12-30
HK1161680A1 (en) 2012-08-03
PT2421537E (pt) 2015-07-03
US20110269774A1 (en) 2011-11-03
SG195608A1 (en) 2013-12-30
HRP20150531T1 (hr) 2015-06-19
MA32727B1 (ar) 2011-10-02
US20150265589A1 (en) 2015-09-24
CN102264371A (zh) 2011-11-30
CN102264371B (zh) 2013-10-02
EP2421537B1 (en) 2015-04-08
CR20110264A (es) 2011-10-04
AU2009320144B2 (en) 2013-11-21
RS54045B1 (sr) 2015-10-30
KR20110080172A (ko) 2011-07-12
BRPI0920053B1 (pt) 2019-11-26
CO6361929A2 (es) 2012-01-20
AR073993A1 (es) 2010-12-15
BRPI0920053B8 (pt) 2021-05-25
US20160095841A1 (en) 2016-04-07
UY32200A (es) 2010-05-31
PL2421537T3 (pl) 2015-08-31
CA2741760A1 (en) 2010-06-03
SMT201500157B (it) 2015-09-07
US9446034B2 (en) 2016-09-20
JP2012506876A (ja) 2012-03-22
EA021927B1 (ru) 2015-09-30
NZ592477A (en) 2013-01-25
PE20110941A1 (es) 2012-02-08
MX2011004369A (es) 2011-05-25
US20140107131A1 (en) 2014-04-17
IL212444A (en) 2015-11-30
WO2010062578A1 (en) 2010-06-03
SI2421537T1 (sl) 2015-06-30
EP2421537A1 (en) 2012-02-29
AU2009320144A1 (en) 2010-06-03
TW201028394A (en) 2010-08-01
MY161890A (en) 2017-05-15
BRPI0920053A2 (pt) 2015-12-15
CL2011000933A1 (es) 2011-10-21
ZA201102892B (en) 2012-02-29
KR101512217B1 (ko) 2015-04-15
DOP2011000113A (es) 2011-07-15
DK2421537T3 (da) 2015-06-22
US20110207743A1 (en) 2011-08-25
TWI454467B (zh) 2014-10-01
US9012479B2 (en) 2015-04-21
ES2539835T3 (es) 2015-07-06
JP5642689B2 (ja) 2014-12-17

Similar Documents

Publication Publication Date Title
JO3067B1 (ar) بيرميدينات بيرازولو امينو كمثبطات ل fak
EA201100580A1 (ru) Имидазопиридазинкарбонитрилы, используемые в качестве ингибиторов киназы
TN2011000404A1 (en) Fused pyrimidines
PH12015501585A1 (en) Manufacturing process for pyrimidine derivatives
EA201000113A1 (ru) Пиразольные соединения
TN2011000293A1 (en) Protein kinase inhibitors
JO3007B1 (ar) مركبات و تركيبات كمثبطات كيناز بروتين
EA200970207A1 (ru) Соединения пиридо[2,3-d]пиримидинона и их применение в качестве pi3 ингибиторов
MY160454A (en) Oxazole substituted indazoles as pi3-kinase inhibitors
TN2010000070A1 (en) Fused bicyclic pyrimidines
TW200626610A (en) Analogs of 17-hydroxywortmannin as PI3K inhibitors
MD20140047A2 (ro) Inhibitori ai protein kinazei
EA201001359A1 (ru) Гетероциклические соединения в качестве ингибиторов cxcr2
EA201290632A1 (ru) Производные бетулина
GEP20135957B (en) Heterocyclic compound and usage thereof
PH12014500373A1 (en) Amino quinazolines as kinase inhibitors
EA201170154A1 (ru) Производные пиридинопиридинонов, способ их получения и применение в терапии
MX2012006805A (es) Indolil-piperidinil bencilaminas como inhibidores de beta-triptasa.
MA32142B1 (ar) شكل بلوري لمشتقات الفينيل امينو بيريميدين
EA201190293A1 (ru) Пролекарства триптолида
EA201001348A1 (ru) Пирролопиримидинкарбоксамиды
EA201200322A1 (ru) Метилпирролопиримидинкарбоксамиды
TNSN06260A1 (en) Process for the preparation of tryptase inhibitors
MX2009004625A (es) Derivados de 3-amino-pirazol-4-carboxamida utiles como inhibidores de proteina cinasas.
EA201170461A1 (ru) Арилсульфонамидные аминосоединения и их применение в качестве лигандов 5-ht