JO3073B1 - مثبطات ثنائية ملتحمة ثلاثية الحلقة ل cdk 4/6 و flt3 - Google Patents

مثبطات ثنائية ملتحمة ثلاثية الحلقة ل cdk 4/6 و flt3

Info

Publication number
JO3073B1
JO3073B1 JOP/2012/0063A JOP20120063A JO3073B1 JO 3073 B1 JO3073 B1 JO 3073B1 JO P20120063 A JOP20120063 A JO P20120063A JO 3073 B1 JO3073 B1 JO 3073B1
Authority
JO
Jordan
Prior art keywords
flt3
cdk
fused tricyclic
formula
dual inhibitors
Prior art date
Application number
JOP/2012/0063A
Other languages
English (en)
Inventor
Wang Xianghong
N Huard Justin
Zhang Jian
Duquette Jason
Chen Xiaoqi
Li Zhihong
Elizabeth Lively Sarah
Keegan Kathleen
Dia Kang
R Mcgee Lawrence
F Weidner Margaret
L Ragains Mark
W Gribble Michael Jr
Original Assignee
Amgen Inc
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 Amgen Inc filed Critical Amgen Inc
Application granted granted Critical
Publication of JO3073B1 publication Critical patent/JO3073B1/ar

Links

Classifications

    • 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
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/14Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

مركبات الصيغة I هي مثبطات مفيدة ل CDK4، CDK6، و FLT3. هذه المركبات مفيدة في علاج السرطان وحالات مرضية أخرى مختلفة. مركبات الصيغة I لها التركيب التالي: I حيث R1 تمثل مجموعة بالصيغة IA، الصيغة IB، الصيغة IC، أو الصيغة ID
JOP/2012/0063A 2011-03-23 2012-03-25 مثبطات ثنائية ملتحمة ثلاثية الحلقة ل cdk 4/6 و flt3 JO3073B1 (ar)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161466841P 2011-03-23 2011-03-23

Publications (1)

Publication Number Publication Date
JO3073B1 true JO3073B1 (ar) 2017-03-15

Family

ID=45926933

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2012/0063A JO3073B1 (ar) 2011-03-23 2012-03-25 مثبطات ثنائية ملتحمة ثلاثية الحلقة ل cdk 4/6 و flt3

Country Status (19)

Country Link
US (3) US8623885B2 (ar)
EP (2) EP2937349B1 (ar)
JP (1) JP5647374B2 (ar)
KR (2) KR101606250B1 (ar)
CN (1) CN103703000B (ar)
AR (1) AR085544A1 (ar)
AU (1) AU2012230896B9 (ar)
CA (1) CA2830516C (ar)
DK (2) DK2937349T3 (ar)
ES (2) ES2543569T3 (ar)
JO (1) JO3073B1 (ar)
MX (1) MX2013010871A (ar)
MY (1) MY161199A (ar)
PH (1) PH12013501940A1 (ar)
PT (2) PT2688887E (ar)
SG (1) SG193580A1 (ar)
TW (1) TWI438204B (ar)
UY (1) UY33969A (ar)
WO (1) WO2012129344A1 (ar)

Families Citing this family (142)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS52711B (sr) 2005-05-10 2013-08-30 Incyte Corporation Modulatori indolamin 2,3-dioksigenaze i postupci upotrebe istih
WO2009085185A1 (en) * 2007-12-19 2009-07-09 Amgen Inc. Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
PL2315756T3 (pl) 2008-07-08 2015-02-27 Incyte Holdings Corp 1,2,5-oksadiazole jako inhibitory 2,3-dioksygenazy indoloaminy
PT2688887E (pt) 2011-03-23 2015-07-06 Amgen Inc Inibidores duais tricíclicos fusionados de cdk 4/6 e flt3
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
US20140199728A1 (en) 2013-01-14 2014-07-17 Amgen Inc. Methods of using cell-cycle inhibitors to modulate one or more properties of a cell culture
US9527857B2 (en) 2013-03-15 2016-12-27 GI Therapeutics, Inc. HSPC-sparing treatments for RB-positive abnormal cellular proliferation
US20140271460A1 (en) * 2013-03-15 2014-09-18 G1 Therapeutics, Inc. Highly Active Anti-Neoplastic and Anti-Proliferative Agents
ES2782003T3 (es) 2013-04-16 2020-09-09 Memorial Sloan Kettering Cancer Center Compañero de diagnóstico para inhibidores de CDK4
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為fgfr抑制劑之雙環雜環
US9732154B2 (en) 2014-02-28 2017-08-15 Janssen Biotech, Inc. Anti-CD38 antibodies for treatment of acute lymphoblastic leukemia
US9603927B2 (en) 2014-02-28 2017-03-28 Janssen Biotech, Inc. Combination therapies with anti-CD38 antibodies
WO2016015598A1 (en) * 2014-07-26 2016-02-04 Sunshine Lake Pharma Co., Ltd. 2-amino-pyrido[2,3-d]pyrimidin-7(8h)-one derivatives as cdk inhibitors and uses thereof
EP3191187B1 (en) 2014-09-09 2021-07-28 Janssen Biotech, Inc. Combination therapies with anti-cd38 antibodies
WO2016040858A1 (en) 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Combinations and dosing regimes to treat rb-positive tumors
JP6802791B2 (ja) * 2014-12-04 2020-12-23 ヤンセン バイオテツク,インコーポレーテツド 急性骨髄性白血病の治療のための抗cd38抗体
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
JP6793401B2 (ja) * 2015-03-11 2020-12-02 国立研究開発法人理化学研究所 難治性白血病治療薬
BR112017019286B1 (pt) 2015-03-11 2023-02-14 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Derivados de 2h-pirazol substituídos ou um sal farmacêuticamente aceitável dos mesmos
WO2016183071A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Hetero-tricyclic compounds and their use for the treatment of cancer
BR112017024877A2 (pt) 2015-05-20 2019-09-17 Janssen Biotech, Inc. anticorpo anti-cd38 e seu uso no tratamento de amiloidose de cadeia leve e outras malignidades hematológicas positivas para cd38
NZ777133A (en) 2015-06-22 2025-05-02 Janssen Biotech Inc Combination therapies for heme malignancies with anti-cd38 antibodies and survivin inhibitors
US20170044265A1 (en) 2015-06-24 2017-02-16 Janssen Biotech, Inc. Immune Modulation and Treatment of Solid Tumors with Antibodies that Specifically Bind CD38
WO2017027717A1 (en) 2015-08-12 2017-02-16 Incyte Corporation Bicyclic fused pyrimidine compounds as tam inhibitors
WO2017035366A1 (en) 2015-08-26 2017-03-02 Incyte Corporation Pyrrolopyrimidine derivatives as tam inhibitors
MD3827845T2 (ro) 2015-11-03 2022-09-30 Janssen Biotech Inc Formulări subcutanate de anticorpi anti-CD38 și utilizări ale acestora
US10781261B2 (en) 2015-11-03 2020-09-22 Janssen Biotech, Inc. Subcutaneous formulations of anti-CD38 antibodies and their uses
WO2017156263A1 (en) 2016-03-09 2017-09-14 Memorial Sloan-Kettering Cancer Center Enigma and cdh18 as companion diagnostics for cdk4 inhibitors
AU2017241524B2 (en) 2016-03-28 2021-07-08 Incyte Corporation Pyrrolotriazine compounds as TAM inhibitors
US20190233533A1 (en) 2016-06-28 2019-08-01 Umc Utrecht Holding B.V. Treatment Of IgE-Mediated Diseases With Antibodies That Specifically Bind CD38
CA3034875C (en) * 2016-08-23 2024-05-28 Eisai R&D Management Co., Ltd. Combination therapies for the treatment of hepatocellular carcinoma
KR102513448B1 (ko) 2016-12-16 2023-03-23 씨스톤 파마슈티컬즈 Cdk4/6 억제제
EP3558971B1 (en) 2016-12-22 2022-02-23 Global Blood Therapeutics, Inc. Histone methyltransferase inhibitors
JP7076741B2 (ja) 2016-12-27 2022-05-30 国立研究開発法人理化学研究所 Bmpシグナル阻害化合物
US11395821B2 (en) 2017-01-30 2022-07-26 G1 Therapeutics, Inc. Treatment of EGFR-driven cancer with fewer side effects
MX2019010981A (es) 2017-03-16 2020-09-07 Eisai R&D Man Co Ltd Terapias de combinacion para el tratamiento de cancer de mama.
CN107021965B (zh) * 2017-05-16 2019-08-13 无锡捷化医药科技有限公司 一种合成5,6,7,8-四氢-1,6-萘啶-2胺的方法
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CN110997671A (zh) * 2017-06-09 2020-04-10 全球血液疗法股份有限公司 作为组蛋白甲基转移酶抑制剂的氮杂吲哚化合物
KR102464677B1 (ko) * 2017-08-11 2022-11-10 셍커 파마슈티컬스 (지앙수) 엘티디. 단백질 인산화효소 억제제로 작용하는 1h-피라졸로[4,3-h]퀴나졸린 화합물
TWI821200B (zh) 2017-09-27 2023-11-11 美商英塞特公司 Tam抑制劑之鹽
MA50514A (fr) 2017-10-31 2020-09-09 Janssen Biotech Inc Méthodes de traitement du myélome multiple à haut risque
WO2019136451A1 (en) 2018-01-08 2019-07-11 G1 Therapeutics, Inc. G1t38 superior dosage regimes
US20190292188A1 (en) 2018-02-27 2019-09-26 Incyte Corporation Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors
ES2991427T3 (es) 2018-05-04 2024-12-03 Incyte Corp Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
MA52940A (fr) 2018-05-18 2021-04-28 Incyte Corp Dérivés de pyrimidine fusionnés utilisés en tant qu'inhibiteurs de a2a/a2b
US11241438B2 (en) 2018-06-29 2022-02-08 Incyte Corporation Formulations of an AXL/MER inhibitor
CN113166153B (zh) 2018-07-05 2024-11-01 因赛特公司 作为a2a/a2b抑制剂的稠合吡嗪衍生物
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
CN111377922B (zh) * 2018-12-29 2021-12-17 武汉光谷通用名药物研究院有限公司 稠合三环类化合物及其用途
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
MA54947A (fr) 2019-02-15 2021-12-22 Incyte Corp Biomarqueurs de kinase 2 dépendant de la cycline et leurs utilisations
CN113727758A (zh) 2019-03-01 2021-11-30 锐新医药公司 双环杂环基化合物及其用途
KR20210146287A (ko) 2019-03-01 2021-12-03 레볼루션 메디슨즈, 인크. 이환식 헤테로아릴 화합물 및 이의 용도
US11472791B2 (en) 2019-03-05 2022-10-18 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021022172A1 (en) 2019-08-01 2021-02-04 Incyte Corporation A dosing regimen for an ido inhibitor
MX2022001940A (es) 2019-08-14 2022-05-10 Incyte Corp Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2.
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN119930610A (zh) 2019-10-11 2025-05-06 因赛特公司 作为cdk2抑制剂的双环胺
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20220109407A (ko) 2019-11-04 2022-08-04 레볼루션 메디슨즈, 인크. Ras 억제제
EP4054719B1 (en) 2019-11-04 2026-02-11 Revolution Medicines, Inc. Ras inhibitors
JP7823816B2 (ja) 2019-11-04 2026-03-04 レヴォリューション・メディスンズ,インコーポレイテッド Ras阻害剤
BR112022008858A2 (pt) 2019-11-08 2022-09-06 Revolution Medicines Inc Composto, composição farmacêutica e métodos para inibir sos1 em um sujeito, para inibir a interação de sos1 e uma proteína, para tratar ou prevenir uma doença e para tratar ou prevenir câncer
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN114929279A (zh) 2020-01-07 2022-08-19 锐新医药公司 Shp2抑制剂给药和治疗癌症的方法
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP4114401A1 (en) 2020-03-06 2023-01-11 Incyte Corporation Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors
TWI901650B (zh) 2020-03-26 2025-10-21 匈牙利商羅特格登公司 啶及吡啶并〔3,4-c〕嗒衍生物
IL297165A (en) 2020-04-16 2022-12-01 Incyte Corp Soysag tricyclic CRS inhibitors
US11739102B2 (en) 2020-05-13 2023-08-29 Incyte Corporation Fused pyrimidine compounds as KRAS inhibitors
US10988479B1 (en) 2020-06-15 2021-04-27 G1 Therapeutics, Inc. Morphic forms of trilaciclib and methods of manufacture thereof
CA3183032A1 (en) 2020-06-18 2021-12-23 Mallika Singh Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
WO2022047093A1 (en) 2020-08-28 2022-03-03 Incyte Corporation Vinyl imidazole compounds as inhibitors of kras
MX2023002248A (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
CR20230165A (es) 2020-09-15 2023-06-02 Revolution Medicines Inc Derivados indólicos como inhibidores de ras en el tratamiento del cáncer
CN112043710A (zh) * 2020-09-28 2020-12-08 广州智睿医药科技有限公司 一种治疗或预防与lrrk2激酶或异常lrrk2突变激酶活性相关疾病的药物
US11767320B2 (en) 2020-10-02 2023-09-26 Incyte Corporation Bicyclic dione compounds as inhibitors of KRAS
CN117396472A (zh) 2020-12-22 2024-01-12 上海齐鲁锐格医药研发有限公司 Sos1抑制剂及其用途
WO2022155941A1 (en) 2021-01-25 2022-07-28 Qilu Regor Therapeutics Inc. Cdk2 inhibitors
WO2022206888A1 (en) 2021-03-31 2022-10-06 Qilu Regor Therapeutics Inc. Cdk2 inhibitors and use thereof
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CR20230558A (es) 2021-05-05 2024-01-24 Revolution Medicines Inc Inhibidores de ras para el tratamiento del cáncer
IL308193A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
CA3224674A1 (en) 2021-07-07 2023-01-12 Pei Gan Tricyclic compounds as inhibitors of kras
EP4370515A1 (en) 2021-07-14 2024-05-22 Incyte Corporation Tricyclic compounds as inhibitors of kras
CA3229855A1 (en) 2021-08-31 2023-03-09 Incyte Corporation Naphthyridine compounds as inhibitors of kras
US12030883B2 (en) 2021-09-21 2024-07-09 Incyte Corporation Hetero-tricyclic compounds as inhibitors of KRAS
WO2023056421A1 (en) 2021-10-01 2023-04-06 Incyte Corporation Pyrazoloquinoline kras inhibitors
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
IL312114A (en) 2021-10-14 2024-06-01 Incyte Corp Quinoline compounds as Kras inhibitors
JP2024542248A (ja) 2021-11-22 2024-11-13 インサイト・コーポレイション Fgfr阻害剤とkras阻害剤を含む併用療法
US20230203010A1 (en) 2021-12-03 2023-06-29 Incyte Corporation Bicyclic amine cdk12 inhibitors
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
JP2025500878A (ja) 2021-12-17 2025-01-15 ジェンザイム・コーポレーション Shp2阻害剤としてのピラゾロピラジン化合物
TW202340215A (zh) 2021-12-22 2023-10-16 美商英塞特公司 Fgfr抑制劑之鹽及固體形式以及其製備方法
WO2023116884A1 (en) 2021-12-24 2023-06-29 Qilu Regor Therapeutics Inc. Cdk2 inhibitors and use thereof
WO2023168686A1 (en) 2022-03-11 2023-09-14 Qilu Regor Therapeutics Inc. Substituted cyclopentanes as cdk2 inhibitors
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
CR20240408A (es) 2022-03-07 2024-11-22 Incyte Corp Formas sólidas, sales y procesos de preparación de un inhibidor de cdk2.
CN119136806A (zh) 2022-03-08 2024-12-13 锐新医药公司 用于治疗免疫难治性肺癌的方法
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2023250430A1 (en) 2022-06-22 2023-12-28 Incyte Corporation Bicyclic amine cdk12 inhibitors
WO2024015731A1 (en) 2022-07-11 2024-01-18 Incyte Corporation Fused tricyclic compounds as inhibitors of kras g12v mutants
AU2023383006A1 (en) * 2022-11-14 2025-05-22 Schrödinger, Inc. Tricyclic compounds
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
PE20260039A1 (es) 2023-04-07 2026-01-09 Revolution Medicines Inc Inhibidores macrociclicos de ras
WO2024211663A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
TW202448897A (zh) 2023-04-14 2024-12-16 美商銳新醫藥公司 Ras抑制劑之結晶形式、含有其之組合物及其使用方法
WO2024220532A1 (en) 2023-04-18 2024-10-24 Incyte Corporation Pyrrolidine kras inhibitors
EP4698542A1 (en) 2023-04-18 2026-02-25 Incyte Corporation 2-azabicyclo[2.2.1]heptane kras inhibitors
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
WO2024254245A1 (en) 2023-06-09 2024-12-12 Incyte Corporation Bicyclic amines as cdk2 inhibitors
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
WO2025096738A1 (en) 2023-11-01 2025-05-08 Incyte Corporation Kras inhibitors
US20250195536A1 (en) 2023-12-13 2025-06-19 Incyte Corporation Bicyclooctane kras inhibitors
TW202542151A (zh) 2023-12-22 2025-11-01 美商銳格醫藥有限公司 Sos1抑制劑及其用途
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
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
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors

Family Cites Families (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1168290A (en) 1964-08-27 1969-10-22 Allen & Hanburys Ltd Novel Heterocyclic Compounds
US4160452A (en) 1977-04-07 1979-07-10 Alza Corporation Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
IT1153216B (it) 1981-10-16 1987-01-14 Schering Ag Procedimento per la preparazione di composti cianoeterociclici
JP2762522B2 (ja) 1989-03-06 1998-06-04 藤沢薬品工業株式会社 血管新生阻害剤
US5112946A (en) 1989-07-06 1992-05-12 Repligen Corporation Modified pf4 compositions and methods of use
US5892112A (en) 1990-11-21 1999-04-06 Glycomed Incorporated Process for preparing synthetic matrix metalloprotease inhibitors
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
EP0669929B1 (en) 1992-11-13 2007-01-03 Immunex Corporation Elk ligand, a cytokine
US5629327A (en) 1993-03-01 1997-05-13 Childrens Hospital Medical Center Corp. Methods and compositions for inhibition of angiogenesis
US5516658A (en) 1993-08-20 1996-05-14 Immunex Corporation DNA encoding cytokines that bind the cell surface receptor hek
US5700823A (en) 1994-01-07 1997-12-23 Sugen, Inc. Treatment of platelet derived growth factor related disorders such as cancers
WO1995028484A1 (en) 1994-04-15 1995-10-26 Amgen Inc. Hek5, hek7, hek8, hek11, new eph-like receptor protein tyrosine kinases
US6303769B1 (en) 1994-07-08 2001-10-16 Immunex Corporation Lerk-5 dna
US5919905A (en) 1994-10-05 1999-07-06 Immunex Corporation Cytokine designated LERK-6
US6057124A (en) 1995-01-27 2000-05-02 Amgen Inc. Nucleic acids encoding ligands for HEK4 receptors
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5880141A (en) 1995-06-07 1999-03-09 Sugen, Inc. Benzylidene-Z-indoline compounds for the treatment of disease
US6846630B2 (en) 1996-10-18 2005-01-25 Takara Shuzo Co., Ltd. Nucleic acid encoding receptor type protein kinase
WO1998028281A1 (en) 1996-12-23 1998-07-02 Celltech Therapeutics Limited Fused polycyclic 2-aminopyrimidine derivatives, their preparation and their use as protein tyrosine kinase inhibitors
US6498163B1 (en) 1997-02-05 2002-12-24 Warner-Lambert Company Pyrido[2,3-D]pyrimidines and 4-aminopyrimidines as inhibitors of cellular proliferation
CO4950519A1 (es) 1997-02-13 2000-09-01 Novartis Ag Ftalazinas, preparaciones farmaceuticas que las comprenden y proceso para su preparacion
GB9800569D0 (en) 1998-01-12 1998-03-11 Glaxo Group Ltd Heterocyclic compounds
JP2002505330A (ja) 1998-03-04 2002-02-19 ブリストル−マイヤーズ スクイブ カンパニー ヘテロシクロ−置換イミダゾピラジン・たんぱくチロシンキナーゼ抑制剤
IL139934A (en) 1998-05-29 2007-10-31 Sugen Inc History 2 - Indulinone converted to pyrrole and pharmaceutical preparations containing them
UA60365C2 (uk) 1998-06-04 2003-10-15 Пфайзер Продактс Інк. Похідні ізотіазолу, спосіб їх одержання, фармацевтична композиція та спосіб лікування гіперпроліферативного захворювання у ссавця
WO2000002871A1 (en) 1998-07-10 2000-01-20 Merck & Co., Inc. Novel angiogenesis inhibitors
CA2341409A1 (en) 1998-08-31 2000-03-09 Merck And Co., Inc. Novel angiogenesis inhibitors
ATE538794T1 (de) 1999-01-13 2012-01-15 Bayer Healthcare Llc Gamma carboxyarylsubstituierte diphenylharnstoffverbindungen als p38 kinasehemmer
PT1165085E (pt) 1999-03-30 2006-10-31 Novartis Ag Derivados de ftalazina para tratar doencas inflamatorias
JP4587626B2 (ja) 1999-06-07 2010-11-24 イミュネックス・コーポレーション Tekアンタゴニスト
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
PL203782B1 (pl) 1999-11-05 2009-11-30 Astrazeneca Ab Pochodne chinazoliny,sposoby ich wytwarzania,ich kompozycje farmaceutyczne oraz ich zastosowania
PT1233943E (pt) 1999-11-24 2011-09-01 Sugen Inc Formulações para agentes farmacêuticos ionizáveis como ácidos livres ou bases livres
US6515004B1 (en) 1999-12-15 2003-02-04 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
US6727225B2 (en) 1999-12-20 2004-04-27 Immunex Corporation TWEAK receptor
AU4721901A (en) 2000-02-25 2001-09-03 Immunex Corp Integrin antagonists
YU66502A (sh) 2000-03-06 2005-09-19 Warner-Lambert Company 5-alkilpirido(2,3-d)pirimidini, inhibitori tirozinkinaza
KR100826817B1 (ko) 2000-03-15 2008-05-02 사노피-아벤티스 도이칠란트 게엠베하 치환된 베타-카볼린
GB0007371D0 (en) 2000-03-28 2000-05-17 Astrazeneca Uk Ltd Chemical compounds
CA2413002A1 (en) 2000-06-30 2002-12-19 Banyu Pharmaceutical Co., Ltd. Novel pyrazinone derivatives
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
ATE430742T1 (de) 2000-12-21 2009-05-15 Smithkline Beecham Corp Pyrimidinamine als angiogenesemodulatoren
US7105682B2 (en) 2001-01-12 2006-09-12 Amgen Inc. Substituted amine derivatives and methods of use
US20020147198A1 (en) 2001-01-12 2002-10-10 Guoqing Chen Substituted arylamine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
WO2003062246A1 (en) 2002-01-22 2003-07-31 Warner-Lambert Company Llc 2-thia-1,6,8-triaza-naphtalene-2,2-dioxides as cdk inhibitors
DE60303009T2 (de) 2002-01-22 2006-07-13 Warner-Lambert Co. Llc 2-(pyridin-2-ylamino)-pyrido[2,3-d]pyrimidin-7-one
US20030199525A1 (en) 2002-03-21 2003-10-23 Hirst Gavin C. Kinase inhibitors
US7307088B2 (en) 2002-07-09 2007-12-11 Amgen Inc. Substituted anthranilic amide derivatives and methods of use
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
US7563798B2 (en) 2002-09-04 2009-07-21 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
JP2006516561A (ja) 2003-01-17 2006-07-06 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー 細胞増殖の阻害剤としての2−アミノピリジン置換ヘテロ環類
US7482354B2 (en) 2003-05-22 2009-01-27 Nerviano Medical Sciences S.R.L. Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
JP4053073B2 (ja) 2003-07-11 2008-02-27 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー 選択的cdk4阻害剤のイセチオン酸塩
WO2005042498A2 (en) 2003-10-31 2005-05-12 Neurogen Corporation 4-amino (aza) quinoline derivatives as capsaicin receptor agonists
GB0329214D0 (en) 2003-12-17 2004-01-21 Glaxo Group Ltd Novel compounds
JP2007523151A (ja) 2004-02-18 2007-08-16 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー 2−(ピリジン−3−イルアミノ)−ピリド[2,3−d]ピリミジン−7−オン
GB0403606D0 (en) 2004-02-18 2004-03-24 Novartis Ag Organic compounds
WO2005094830A1 (en) 2004-03-30 2005-10-13 Pfizer Products Inc. Combinations of signal transduction inhibitors
WO2005110410A2 (en) 2004-05-14 2005-11-24 Abbott Laboratories Kinase inhibitors as therapeutic agents
US7452887B2 (en) 2004-06-04 2008-11-18 Amphora Discovery Corporation Quinoline- and isoquinoline-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof
MXPA06014021A (es) 2004-06-04 2007-02-08 Pfizer Prod Inc Procedimiento para tratar crecimiento celular anormal.
CA2575804A1 (en) 2004-08-26 2006-03-02 Boehringer Ingelheim International Gmbh Pteridinones used as plk (polo like kinase) inhibitors
US7906528B2 (en) 2004-10-05 2011-03-15 Novartis International Pharmaceutical Ltd. Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
JP2008515982A (ja) 2004-10-13 2008-05-15 メルク エンド カムパニー インコーポレーテッド 高眼圧症を治療するための眼科組成物
TW200633990A (en) 2004-11-18 2006-10-01 Takeda Pharmaceuticals Co Amide compound
US20060142312A1 (en) 2004-12-23 2006-06-29 Pfizer Inc C6-aryl and heteroaryl substituted pyrido[2,3-D] pyrimidin-7-ones
ES2411975T3 (es) 2005-01-14 2013-07-09 Janssen Pharmaceutica Nv Pirimidinas heterocíclicas anilladas de 5 miembros como inhibidores de cinasas
EP1845973B1 (en) 2005-01-21 2015-08-12 Astex Therapeutics Limited Pharmaceutical compounds
EP1896472A1 (de) 2005-06-09 2008-03-12 Boehringer Ingelheim International GmbH Alpha-carboline als cdk-1 inhibitoren
EP1931683B1 (en) 2005-08-19 2011-07-13 Schering Corporation Fused tricyclic mglur1 antagonists as therapeutic agents
AU2006283592A1 (en) 2005-08-22 2007-03-01 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
CN101360499B (zh) 2005-10-06 2015-10-07 默沙东公司 吡唑并[1,5-a]嘧啶衍生物在制备抑制蛋白激酶的药物中的用途
EA018128B1 (ru) 2006-01-23 2013-05-30 Амген Инк. Модуляторы аурора киназы, способы их получения и их применение
AR060432A1 (es) 2006-04-12 2008-06-18 Vertex Pharma Tetrahidropteridinas utiles como inhibidores de las proteinas quinasas
CA2651072A1 (en) 2006-05-01 2007-11-08 Pfizer Products Inc. Substituted 2-amino-fused heterocyclic compounds
US20090142337A1 (en) 2006-05-08 2009-06-04 Astex Therapeutics Limited Pharmaceutical Combinations of Diazole Derivatives for Cancer Treatment
US7893058B2 (en) 2006-05-15 2011-02-22 Janssen Pharmaceutica Nv Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
US20070270362A1 (en) 2006-05-18 2007-11-22 The University Of Washington Methods and compositions for prevention or treatment of inflammatory-related diseases and disorders
JO3235B1 (ar) 2006-05-26 2018-03-08 Astex Therapeutics Ltd مركبات بيررولوبيريميدين و استعمالاتها
WO2008001076A1 (en) 2006-06-26 2008-01-03 Ucb Pharma S.A. Fused thiazole derivatives as kinase inhibitors
RU2009108006A (ru) 2006-09-08 2010-10-20 Пфайзер Продактс Инк. (Us) Синтез 2-(пиридин-2-иламино)-пиридо[2, 3-d]пиримидин-7-онов
EP2109450A2 (en) 2006-12-14 2009-10-21 Panacea Pharmaceuticals, Inc. Methods of neuroprotection by cyclin-dependent kinase inhibition
CA2672960A1 (en) 2006-12-20 2008-07-10 Schering Corporation Novel jnk inhibitors
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
WO2009014642A1 (en) 2007-07-19 2009-01-29 Amgen Inc. Combination of a de novo purine biosynthesis inhibitor and a cyclin dependent kinase inhibitor for the treatment of cancer
US7982035B2 (en) 2007-08-27 2011-07-19 Duquesne University Of The Holy Spirit Tricyclic compounds having antimitotic and/or antitumor activity and methods of use thereof
US7960400B2 (en) 2007-08-27 2011-06-14 Duquesne University Of The Holy Ghost Tricyclic compounds having cytostatic and/or cytotoxic activity and methods of use thereof
PE20091195A1 (es) 2007-11-07 2009-08-06 Schering Corp Nuevos moduladores de los puntos de control del ciclo celular y su uso en combinacion con inhibidores de quinasa de punto de control
WO2009061345A2 (en) 2007-11-07 2009-05-14 Cornell Research Foundation, Inc. Targeting cdk4 and cdk6 in cancer therapy
WO2009085185A1 (en) * 2007-12-19 2009-07-09 Amgen Inc. Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
US20110014191A1 (en) 2007-12-28 2011-01-20 Ipsogen Breast cancer expression profiling
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
MX2010010975A (es) 2008-04-07 2010-11-01 Amgen Inc Amino piridinas/pirimidinas gem-disustituidas y espirociclicas como inhibidores de ciclo celular.
JP2011518219A (ja) * 2008-04-22 2011-06-23 ポートラ ファーマシューティカルズ, インコーポレイテッド タンパク質キナーゼの阻害剤
PT2688887E (pt) 2011-03-23 2015-07-06 Amgen Inc Inibidores duais tricíclicos fusionados de cdk 4/6 e flt3

Also Published As

Publication number Publication date
KR101606250B1 (ko) 2016-03-24
KR20130140150A (ko) 2013-12-23
ES2543569T3 (es) 2015-08-20
PT2937349T (pt) 2017-03-24
TW201302750A (zh) 2013-01-16
PT2688887E (pt) 2015-07-06
AU2012230896A1 (en) 2013-10-03
CA2830516A1 (en) 2012-09-27
CA2830516C (en) 2017-01-24
CN103703000A (zh) 2014-04-02
US20140163052A1 (en) 2014-06-12
EP2688887A1 (en) 2014-01-29
EP2688887B1 (en) 2015-05-13
US20160368933A1 (en) 2016-12-22
SG193580A1 (en) 2013-10-30
EP2937349A1 (en) 2015-10-28
US8623885B2 (en) 2014-01-07
PH12013501940A1 (en) 2015-12-04
ES2620521T3 (es) 2017-06-28
HK1191014A1 (en) 2014-07-18
HK1216889A1 (en) 2016-12-09
MX2013010871A (es) 2014-01-31
US9359355B2 (en) 2016-06-07
TWI438204B (zh) 2014-05-21
MY161199A (en) 2017-04-14
US20120244110A1 (en) 2012-09-27
WO2012129344A1 (en) 2012-09-27
UY33969A (es) 2012-10-31
JP5647374B2 (ja) 2014-12-24
AU2012230896B9 (en) 2015-06-18
CN103703000B (zh) 2015-11-25
JP2014508808A (ja) 2014-04-10
AR085544A1 (es) 2013-10-09
EP2937349B1 (en) 2016-12-28
KR20160035613A (ko) 2016-03-31
DK2937349T3 (en) 2017-02-20
AU2012230896B2 (en) 2015-05-28
DK2688887T3 (en) 2015-06-29

Similar Documents

Publication Publication Date Title
JO3073B1 (ar) مثبطات ثنائية ملتحمة ثلاثية الحلقة ل cdk 4/6 و flt3
MX385616B (es) Inhibidores de cdk
EA201270619A1 (ru) Применение бетанехола для лечения ксеростомии
PH12013502059A1 (en) Pyrrolotriazinone derivatives as p13k inhibitors
UA111382C2 (uk) Інгібітори протеїнкінази
PH12013500005A1 (en) Indolizine derivatives, process for the preparation thereof and therapeutic use thereof
MX2013008212A (es) Derivados de 7-azaindol.
CR11757A (es) Compuestos de triazina como inhibidores mtor y quinasa pi3
EA201490912A1 (ru) Производные [1,2,3]триазоло[4,5-d]пиримидина в качестве агонистов каннабиноидного рецептора 2
UA111075C2 (uk) Триазолопіридинові сполуки як інгібітори кінази рім
EA201100580A1 (ru) Имидазопиридазинкарбонитрилы, используемые в качестве ингибиторов киназы
TR201816379T4 (tr) DNA-PK inhibitörleri.
MX341456B (es) Amino-quinolinas como inhibidores de cinasa.
EA201270535A1 (ru) Пуриновые производные, применимые в качестве ингибиторов hsp90
TW201129565A (en) Tricyclic heterocyclic compounds, compositions and methods of use thereof
BR112014005226A2 (pt) derivados de benzonitrila como inibidores de cinase
MX336381B (es) Boronatos como inhibidores de arginasa.
UA112795C2 (uk) Біциклічні піразинонові похідні
PH12014500373A1 (en) Amino quinazolines as kinase inhibitors
MX2014012477A (es) Inhibidores pirrolopirazona de tanquirasa.
MX2014003376A (es) Derivados de acido benzoico como inhibidores eif4e.
PH12014500499A1 (en) Triazolopyridine compounds as pde10a inhibitors
CU24052B1 (es) Derivados de anilina-pirimidina sustituidos con sulfoximina como inhibidores de quinasas dependientes de ciclina (cdk), y método de producción de los mismos
CY1120133T1 (el) Πυριδαζινονες ως αναστολεις ενζυμου daao
MX2015012386A (es) Inhibidores de la cinasa cdk9.