[go: up one dir, main page]

AR085544A1 - Inhibidores triciclicos fusionados dobles de las cdk 4/6 y de la flt3 - Google Patents

Inhibidores triciclicos fusionados dobles de las cdk 4/6 y de la flt3

Info

Publication number
AR085544A1
AR085544A1 ARP120100971A ARP120100971A AR085544A1 AR 085544 A1 AR085544 A1 AR 085544A1 AR P120100971 A ARP120100971 A AR P120100971A AR P120100971 A ARP120100971 A AR P120100971A AR 085544 A1 AR085544 A1 AR 085544A1
Authority
AR
Argentina
Prior art keywords
alkyl
substituted
halo
independently selected
unsubstituted
Prior art date
Application number
ARP120100971A
Other languages
English (en)
Inventor
Lawrence R Mgee
Mark L Ragains
Xianghong Wang
Margaret F Weidner
Jian Zhang
Xiaoqi Chen
Kang Dai
Jason A Duquette
Michael W Gribble Jr
Justin N Huard
Kathleen Keegan
Sarah Elizabeth Lively
Zhihong Li
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
Publication of AR085544A1 publication Critical patent/AR085544A1/es

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

Compuestos de fórmula (1), que son inhibidores útiles de la CDK4, de la CDK6 y de la FLT3. Estos compuestos sirven para tratar el cáncer y otros estados de enfermedad diversos.Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable del mismo, un hidrato del mismo, o una mezcla de los mismos, donde: R1 es un grupo de fórmulas (2) a (5) donde la línea ondulada indica el punto de unión del grupo de fórmulas (2), (3), (4), o (5) al resto de la molécula; R2 es un grupo cicloalquilo C5-7, es un grupo heterociclilo de entre 5 y 7 miembros que incluye 1, 2, ó 3 heteroátomos seleccionados entre N, O, y S, o es un grupo bicíclico C7-10; donde el grupo cicloalquilo C5-7, el grupo heterociclilo de entre 5 y 7 miembros, o el grupo bicíclico C7-10 no está sustituido o está sustituido con 1 - 3 sustituyentes seleccionados en forma independiente entre -(alquilo C1-6) no sustituido, -OH, halo, -O-(alquilo C1-6), -CO2H, -C(=O)-O-(alquilo C1-6), -C(=O)-NR’R’’, -NR’R’’, o un -(alquilo C1-4) sustituido, donde el -(alquilo C1-4) sustituido está sustituido con 1 - 3 sustituyentes seleccionados en forma independiente entre halo, -OH, -OCH3, -S(=O)2-CH3, o -C(=O)-CH3; R3a se selecciona entre -H, -F, o -Cl, -(alquilo C1-3), o -O-(alquilo C1-3); R3b es -H, halo, -OH, -O-(alquilo C1-6), -(alquilo C1-6) no sustituido, -NR’R’’, -C(=O)-(alquilo C1-6), -C(=O)-O-(alquilo C1-6), -C(=O)-NR’R’’, o un -(alquilo C1-6) sustituido, donde el -(alquilo C1-6) sustituido está sustituido con 1 - 3 sustituyentes seleccionados en forma independiente entre halo, -OH, -OCH3, -CN, o -NO2; R3c es -H, -(alquilo C1-3), o halo; R4 es -H; R5 es -H; R6 se selecciona entre -H, -(alquilo C1-6), -C(=O)-(alquilo C1-6), -C(=O)-O-(alquilo C1-6), -C(=O)-C(=O)-OH, -C(=O)-NR’R’’, o -S(=O)-NR’R’’, donde el grupo alquilo de los grupos -(alquilo C1-6), -C(=O)-(alquilo C1-6), y -C(=O)-O-(alquilo C1-6) no está sustituido o está sustituido con 1 - 3 sustituyentes seleccionados en forma independiente entre -OH, F, -S(=O)2-(alquilo C1-6), -O-(alquilo C1-6), -NR’R’’, o -CN; R7a es -H, -CH3, o halo; R7b es -H, -(alquilo C1-6), o halo; o R7b se encuentra ausente si R1 es un grupo de fórmula (3) o fórmula (5); R7c es -H, -(alquilo C1-6) no sustituido, halo, -O-(alquilo C1-6), -NO2, -CN, -NR’R’’, -CO2H, -C(=O)-O-(alquilo C1-6), -C(=O)-NR’R’’, o un -(alquilo C1-6) sustituido, donde el -(alquilo C1-6) sustituido está sustituido con 1 - 3 sustituyentes seleccionados en forma independiente entre -OH, halo, -O-(alquilo C1-6), -CN, -NR’R’’, o -S(=O)2-CH3; o R7c se encuentra ausente si R1 es un grupo de fórmula (2) o fórmula (4); R8a es -H, -(alquilo C1-6) no sustituido, o un -(alquilo C1-6) sustituido, donde el -(alquilo C1-6) sustituido está sustituido con 1 - 3 sustituyentes seleccionados en forma independiente entre -OH, halo, o -O-(alquilo C1-6); R8b es -H, -(alquilo C1-6) no sustituido, o un -(alquilo C1-6) sustituido, donde el -(alquilo C1-6) sustituido está sustituido con 1 - 3 sustituyentes seleccionados en forma independiente entre -OH, halo, o -O-(alquilo C1-6); o R8a y R8b, cuando se toman juntos, pueden representar =O; R8c se selecciona entre -H, -OH, -(alquilo C1-6) no sustituido, o un -(alquilo C1-6) sustituido, donde el -(alquilo C1-6) sustituido está sustituido con 1 - 3 sustituyentes seleccionados en forma independiente entre -OH, halo, o -O-(alquilo C1-6); R8d es -H, -(alquilo C1-6) no sustituido, o un -(alquilo C1-6) sustituido, donde el -(alquilo C1-6) sustituido está sustituido con 1 - 3 sustituyentes seleccionados en forma independiente entre -OH, halo, o -O-(alquilo C1-6); R8e es -H, -(alquilo C1-6) no sustituido, o un -(alquilo C1-6) sustituido, donde el -(alquilo C1-6) sustituido está sustituido con 1 - 3 sustituyentes seleccionados en forma independiente entre -OH, halo, o -O-(alquilo C1-6); R8f es -H, -(alquilo C1-6) no sustituido, o un -(alquilo C1-6) sustituido, donde el -(alquilo C1-6) sustituido está sustituido con 1 - 3 sustituyentes seleccionados en forma independiente entre -OH, halo, o -O-(alquilo C1-6); o R8e y R8f, cuando se toman juntos, pueden representar =O; y R’ y R’’ se seleccionan en forma independiente entre -H, -(alquilo C1-4) no sustituido, o -(alquilo C1-4) sustituido con entre 1 y 3 sustituyentes seleccionados en forma independiente entre -OH o -F.
ARP120100971A 2011-03-23 2012-03-23 Inhibidores triciclicos fusionados dobles de las cdk 4/6 y de la flt3 AR085544A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
AR085544A1 true AR085544A1 (es) 2013-10-09

Family

ID=45926933

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120100971A AR085544A1 (es) 2011-03-23 2012-03-23 Inhibidores triciclicos fusionados dobles de las cdk 4/6 y de la flt3

Country Status (19)

Country Link
US (3) US8623885B2 (es)
EP (2) EP2688887B1 (es)
JP (1) JP5647374B2 (es)
KR (2) KR101606250B1 (es)
CN (1) CN103703000B (es)
AR (1) AR085544A1 (es)
AU (1) AU2012230896B9 (es)
CA (1) CA2830516C (es)
DK (2) DK2937349T3 (es)
ES (2) ES2543569T3 (es)
JO (1) JO3073B1 (es)
MX (1) MX2013010871A (es)
MY (1) MY161199A (es)
PH (1) PH12013501940A1 (es)
PT (2) PT2937349T (es)
SG (1) SG193580A1 (es)
TW (1) TWI438204B (es)
UY (1) UY33969A (es)
WO (1) WO2012129344A1 (es)

Families Citing this family (141)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR122020016659B8 (pt) 2005-05-10 2021-07-27 Incyte Holdings Corp moduladores de 2,3-dioxigenase de indolamina e métodos de modulação de atividade de inibição e de imunossupressão
BRPI0821209A2 (pt) * 2007-12-19 2019-09-24 Amgen Inc composto, composição farmacêutica, métodos de tratar câncer, para reduzir o tamanho de tumor, para tratar distúrbios, e para reduzir metástase em um tumor.
BR122019015876B8 (pt) 2008-07-08 2021-07-27 Incyte Holdings Corp compostos derivados de 1,2,5-oxadiazóis, composição, bem como seus usos
MX2013010871A (es) 2011-03-23 2014-01-31 Amgen Inc Inhibidores dobles triciclicos fusionados de cdk 4/6 y flt3.
CN107652289B (zh) 2012-06-13 2020-07-21 因塞特控股公司 作为fgfr抑制剂的取代的三环化合物
US20150353542A1 (en) 2013-01-14 2015-12-10 Amgen Inc. Methods of using cell-cycle inhibitors to modulate one or more properties of a cell culture
WO2014144740A2 (en) * 2013-03-15 2014-09-18 G1 Therapeutics, Inc. Highly active anti-neoplastic and anti-proliferative agents
WO2014144326A1 (en) 2013-03-15 2014-09-18 G1 Therapeutics, Inc. Transient protection of normal cells during chemotherapy
WO2014172479A1 (en) 2013-04-16 2014-10-23 Memorial Sloan-Kettering Cancer Center Companion diagnostic for cdk4 inhibitors
KR102269032B1 (ko) 2013-04-19 2021-06-24 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
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
US9828373B2 (en) * 2014-07-26 2017-11-28 Sunshine Lake Pharma Co., Ltd. 2-amino-pyrido[2,3-D]pyrimidin-7(8H)-one derivatives as CDK inhibitors and uses thereof
MA40608A (fr) 2014-09-09 2016-03-17 Janssen Biotech Inc Polythérapies avec des anticorps anti-cd38
WO2016040858A1 (en) 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Combinations and dosing regimes to treat rb-positive tumors
CA2969717A1 (en) * 2014-12-04 2016-06-09 Janssen Biotech, Inc. Anti-cd38 antibodies for treatment of acute myeloid leukemia
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
PE20171514A1 (es) 2015-02-20 2017-10-20 Incyte Corp Heterociclos biciclicos como inhibidores de fgfr
KR102615733B1 (ko) * 2015-03-11 2023-12-18 치아타이 티안큉 파마수티컬 그룹 주식회사 항암제로서의 치환 2-h-피라졸 유도체
US10278979B2 (en) 2015-03-11 2019-05-07 Riken Therapeutic agent for intractable leukemia
WO2016183071A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Hetero-tricyclic compounds and their use for the treatment of cancer
WO2016187546A1 (en) 2015-05-20 2016-11-24 Janssen Biotech, Inc. Anti-cd38 antibodies for treatment of light chain amyloidosis and other cd38-positive hematological malignancies
US10668149B2 (en) 2015-06-22 2020-06-02 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
US9708333B2 (en) 2015-08-12 2017-07-18 Incyte Corporation Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors
US10053465B2 (en) 2015-08-26 2018-08-21 Incyte Corporation Pyrrolopyrimidine derivatives as TAM inhibitors
US10781261B2 (en) 2015-11-03 2020-09-22 Janssen Biotech, Inc. Subcutaneous formulations of anti-CD38 antibodies and their uses
SMT202100192T1 (it) 2015-11-03 2021-05-07 Janssen Biotech Inc Formulazioni sottocutanee di anticorpi anti-cd38 e loro usi.
WO2017156263A1 (en) 2016-03-09 2017-09-14 Memorial Sloan-Kettering Cancer Center Enigma and cdh18 as companion diagnostics for cdk4 inhibitors
EP4321513A3 (en) 2016-03-28 2024-05-08 Incyte Corporation Pyrrolotriazine compounds as tam inhibitors
JP2019527678A (ja) 2016-06-28 2019-10-03 ユーエムセー・ユトレヒト・ホールディング・ベー・フェー CD38に特異的に結合する抗体によるIgE媒介疾患の治療
JP7190425B2 (ja) 2016-08-23 2022-12-15 エーザイ・アール・アンド・ディー・マネジメント株式会社 肝細胞癌の治療のための併用療法
TWI749126B (zh) 2016-12-16 2021-12-11 大陸商基石藥業(蘇州)有限公司 Cdk4/6抑制劑
ES2981507T3 (es) 2016-12-22 2024-10-09 Global Blood Therapeutics Inc Inhibidores de histonas metiltransferasa
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
KR102517650B1 (ko) 2017-03-16 2023-04-05 에자이 알앤드디 매니지먼트 가부시키가이샤 유방암의 치료를 위한 조합물 요법
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
BR112019025770A2 (pt) * 2017-06-09 2020-06-23 Global Blood Therapeutics, Inc. Compostos de azaindol como inibidores de histona metiltransferase
WO2019029663A1 (zh) * 2017-08-11 2019-02-14 晟科药业(江苏)有限公司 1h-吡唑并[4,3-h]喹唑啉类化合物作为蛋白激酶抑制剂
AU2018342471B2 (en) 2017-09-27 2023-08-24 Incyte Corporation Salts of pyrrolotriazine derivatives useful as TAM inhibitors
EP3703749A1 (en) 2017-10-31 2020-09-09 Janssen Biotech, Inc. Methods of treating high risk multiple myeloma
BR112020013915A2 (pt) 2018-01-08 2020-12-01 G1 Therapeutics, Inc. regime de dosagem para liberação, e, método para tratar um câncer dependente de replicação de cdk4/6 em um humano
MX2020008949A (es) 2018-02-27 2021-01-08 Incyte Corp Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b.
SG11202010636VA (en) 2018-05-04 2020-11-27 Incyte Corp Solid forms of an fgfr inhibitor and processes for preparing the same
BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
JP7391046B2 (ja) 2018-05-18 2023-12-04 インサイト・コーポレイション A2a/a2b阻害剤としての縮合ピリミジン誘導体
DK3813800T3 (da) 2018-06-29 2025-06-02 Incyte Corp Formuleringer af en axl/mer-hæmmer
IL279829B2 (en) 2018-07-05 2025-05-01 Incyte Holdings Corp Fused pyrazine derivatives as A2A/A2B inhibitors
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
PH12021551976A1 (en) 2019-02-15 2022-07-04 Incyte Corp Cyclin-dependent kinase 2 biomarkers and uses thereof
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
WO2020180768A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
EP3930845A1 (en) 2019-03-01 2022-01-05 Revolution Medicines, Inc. Bicyclic heterocyclyl compounds and uses thereof
US11472791B2 (en) 2019-03-05 2022-10-18 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
US11919904B2 (en) 2019-03-29 2024-03-05 Incyte Corporation Sulfonylamide compounds as CDK2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020223558A1 (en) 2019-05-01 2020-11-05 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
CA3150681A1 (en) 2019-08-14 2021-02-18 Incyte Corporation Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021072232A1 (en) 2019-10-11 2021-04-15 Incyte Corporation Bicyclic amines as cdk2 inhibitors
WO2021076602A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
KR20220109408A (ko) 2019-11-04 2022-08-04 레볼루션 메디슨즈, 인크. Ras 억제제
CN114901366A (zh) 2019-11-04 2022-08-12 锐新医药公司 Ras抑制剂
PH12022550988A1 (en) 2019-11-04 2023-10-09 Revolution Medicines Inc Ras inhibitors
WO2021092115A1 (en) 2019-11-08 2021-05-14 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
JP7720840B2 (ja) 2019-12-04 2025-08-08 インサイト・コーポレイション Fgfr阻害剤としての三環式複素環
CN115151539A (zh) 2019-12-04 2022-10-04 因赛特公司 Fgfr抑制剂的衍生物
WO2021142026A1 (en) 2020-01-07 2021-07-15 Revolution Medicines, Inc. Shp2 inhibitor dosing and methods of treating cancer
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
AU2021230385A1 (en) 2020-03-06 2022-09-22 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
CN121270549A (zh) 2020-04-16 2026-01-06 因赛特公司 稠合三环kras抑制剂
WO2021231526A1 (en) 2020-05-13 2021-11-18 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
MX2022016355A (es) 2020-06-18 2023-04-03 Revolution Medicines Inc Metodos para retardar, prevenir, y tratar la resistencia adquirida a inhibidores de ras.
US11999752B2 (en) 2020-08-28 2024-06-04 Incyte Corporation Vinyl imidazole compounds as inhibitors of KRAS
CA3187757A1 (en) 2020-09-03 2022-03-24 Ethan AHLER Use of sos1 inhibitors to treat malignancies with shp2 mutations
IL301298A (en) 2020-09-15 2023-05-01 Revolution Medicines Inc Indole derivatives as RAS inhibitors in cancer therapy
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
AU2021409816A1 (en) 2020-12-22 2023-07-06 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
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
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
AR125787A1 (es) 2021-05-05 2023-08-16 Revolution Medicines Inc Inhibidores de ras
AR125782A1 (es) 2021-05-05 2023-08-16 Revolution Medicines Inc Inhibidores de ras
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220155A1 (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
IL309642A (en) 2021-07-07 2024-02-01 Incyte Corp Tricyclic compounds as inhibitors of Kras
JP2024529347A (ja) 2021-07-14 2024-08-06 インサイト・コーポレイション Krasの阻害剤としての三環式化合物
US12441742B2 (en) 2021-08-31 2025-10-14 Incyte Corporation Naphthyridine compounds as inhibitors of KRAS
WO2023049697A1 (en) 2021-09-21 2023-03-30 Incyte Corporation Hetero-tricyclic compounds as inhibitors of kras
US12030884B2 (en) 2021-10-01 2024-07-09 Incyte Corporation Pyrazoloquinoline KRAS inhibitors
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
CA3235146A1 (en) 2021-10-14 2023-04-20 Incyte Corporation Quinoline compounds as inhibitors of kras
IL312886A (en) 2021-11-22 2024-07-01 Incyte Corp Combined treatment that includes a Pegfer inhibitor and a Kras inhibitor
TW202329937A (zh) 2021-12-03 2023-08-01 美商英塞特公司 雙環胺ck12抑制劑
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
CN119212994A (zh) 2021-12-17 2024-12-27 建新公司 作为shp2抑制剂的吡唑并吡嗪化合物
JP2025500466A (ja) 2021-12-22 2025-01-09 インサイト・コーポレイション Fgfr阻害剤の塩及び固体の形態ならびにその調製方法
WO2023168686A1 (en) 2022-03-11 2023-09-14 Qilu Regor Therapeutics Inc. Substituted cyclopentanes as cdk2 inhibitors
TW202341982A (zh) 2021-12-24 2023-11-01 大陸商上海齊魯銳格醫藥研發有限公司 Cdk2抑制劑及其用途
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
TW202342023A (zh) 2022-03-07 2023-11-01 美商英塞特公司 Cdk2抑制劑之固體形式、鹽及製備方法
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
CN120504682A (zh) 2022-06-10 2025-08-19 锐新医药公司 大环ras抑制剂
AR129675A1 (es) 2022-06-22 2024-09-18 Incyte Corp Inhibidores de cdk12 de aminas biciclicas
WO2024015731A1 (en) 2022-07-11 2024-01-18 Incyte Corporation Fused tricyclic compounds as inhibitors of kras g12v mutants
CR20250216A (es) * 2022-11-14 2025-07-17 Schroedinger Inc Compuestos tricíclicos
KR20250164828A (ko) 2023-03-30 2025-11-25 레볼루션 메디슨즈, 인크. Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도
KR20260005904A (ko) 2023-04-07 2026-01-12 레볼루션 메디슨즈, 인크. 매크로사이클릭 ras 억제제
CN121263418A (zh) 2023-04-07 2026-01-02 锐新医药公司 大环ras抑制剂
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
WO2024220645A1 (en) 2023-04-18 2024-10-24 Incyte Corporation 2-azabicyclo[2.2.1]heptane kras inhibitors
US20240390340A1 (en) 2023-04-18 2024-11-28 Incyte Corporation Pyrrolidine kras inhibitors
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ras相關疾病或病症之組合療法
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
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
US20250163079A1 (en) 2023-11-01 2025-05-22 Incyte Corporation Kras inhibitors
WO2025129002A1 (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
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
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
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder

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
CA2148484A1 (en) 1992-11-13 1994-05-26 Stewart Lyman Novel cytokine designated elk ligand
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
EP0756627A1 (en) 1994-04-15 1997-02-05 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
AU5330698A (en) 1996-12-23 1998-07-17 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
RS49779B (sr) 1998-01-12 2008-06-05 Glaxo Group Limited, Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze
AU756838B2 (en) 1998-03-04 2003-01-23 Bristol-Myers Squibb Company Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors
HUP0103617A2 (hu) 1998-05-29 2002-02-28 Sugen, Inc. Protein kinázt gátló, pirrolilcsoporttal helyettesített 2-indolszármazékok, e vegyületeket tartalmazó gyógyászati készítmények, valamint e vegyületek alkalmazása
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
EP1097147A4 (en) 1998-07-10 2001-11-21 Merck & Co Inc NEW ANGIOGENESIS INHIBITORS
AU760020B2 (en) 1998-08-31 2003-05-08 Merck & Co., Inc. Novel angiogenesis inhibitors
JP2002534468A (ja) 1999-01-13 2002-10-15 バイエル コーポレイション p38キナーゼ阻害剤としてのω−カルボキシアリール置換ジフェニル尿素
DE60028740T2 (de) 1999-03-30 2007-05-24 Novartis Ag Phthalazinderivate zur behandlung von entzündlichen erkrankungen
ATE324444T1 (de) 1999-06-07 2006-05-15 Immunex Corp Tek-antagonisten
US6521424B2 (en) 1999-06-07 2003-02-18 Immunex Corporation Recombinant expression of Tek antagonists
EP1676845B1 (en) 1999-11-05 2008-06-11 AstraZeneca AB New quinazoline derivatives
EP1233943B1 (en) 1999-11-24 2011-06-29 Sugen, Inc. Ionizable indolinone derivatives and their use as ptk ligands
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
US7074408B2 (en) 2000-02-25 2006-07-11 Immunex Corporation Use of integrin antagonists to inhibit angiogenesis
BR0109056A (pt) 2000-03-06 2003-06-03 Warner Lambert Co Inibidores da cinase de tirosina de 5-alquilpirido[2,3-d]pirimidinas
HK1054039B (zh) 2000-03-15 2010-04-16 萨诺费-阿文蒂斯德国有限公司 取代的β-咔啉
GB0007371D0 (en) 2000-03-28 2000-05-17 Astrazeneca Uk Ltd Chemical compounds
ATE276257T1 (de) 2000-06-30 2004-10-15 Banyu Pharma Co Ltd Pyrazinonderivate
US6630500B2 (en) 2000-08-25 2003-10-07 Cephalon, Inc. Selected fused pyrrolocarbazoles
CN1307173C (zh) 2000-12-21 2007-03-28 葛兰素集团有限公司 作为血管生成调节剂的嘧啶胺
US7102009B2 (en) 2001-01-12 2006-09-05 Amgen Inc. Substituted amine derivatives and methods of use
US6878714B2 (en) 2001-01-12 2005-04-12 Amgen Inc. Substituted alkylamine derivatives and methods of use
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
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine 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
ES2251677T3 (es) * 2002-01-22 2006-05-01 Warner-Lambert Company Llc 2-(piridin-2-ilamino)-pirido(2,3-d)pirimidin-7-onas.
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
DE602004021558D1 (de) 2003-01-17 2009-07-30 Warner Lambert Co 2-aminopyridin-substituierteheterocyclen als inhibitoren der zellulären proliferation
AU2004240772B2 (en) 2003-05-22 2011-04-28 Nerviano Medical Sciences S.R.L. Pyrazolo-quinazoline derivatives,process for their preparation and their use as kinase inhibitors
ATE412650T1 (de) 2003-07-11 2008-11-15 Warner Lambert Co Isethionat salz eines selektiven cdk4 inhibitors
AU2004285052A1 (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
BRPI0507852A (pt) 2004-02-18 2007-07-10 Warner Lambert Co 2-(piridin-3-ilamino)-pirido[2,3-d]pirimidin-7-onas
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
EP1761281A1 (en) 2004-06-04 2007-03-14 Pfizer Products Incorporated Method for treating abnormal cell growth
CA2569404A1 (en) 2004-06-04 2005-12-22 Amphora Discovery Corporation Quinoline- and isoquinoline-based compounds exhibiting atp-utilizing enzyme inhibitory activity, and compositions, and uses thereof
EP1786817A1 (de) 2004-08-26 2007-05-23 Boehringer Ingelheim International GmbH Pteridinone als plk (polo like kinase) inhibitoren
US7906528B2 (en) 2004-10-05 2011-03-15 Novartis International Pharmaceutical Ltd. Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
CN101035526A (zh) 2004-10-13 2007-09-12 默克公司 用于治疗高眼压的眼用组合物
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
AU2006205851A1 (en) 2005-01-14 2006-07-20 Janssen Pharmaceutica N.V. 5-membered annelated heterocyclic pyrimidines as kinase inhibitors
AU2006207325B2 (en) 2005-01-21 2012-08-16 Astex Therapeutics Limited Pharmaceutical compounds
EP1896472A1 (de) 2005-06-09 2008-03-12 Boehringer Ingelheim International GmbH Alpha-carboline als cdk-1 inhibitoren
CA2619362A1 (en) 2005-08-19 2007-03-01 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
CA2627623C (en) 2005-10-06 2014-04-22 Schering Corporation Methods for inhibiting protein kinases
HRP20160039T1 (hr) 2006-01-23 2016-02-12 Amgen, Inc Modulatori aurora kinaze i postupak uporabe
MX2008013110A (es) 2006-04-12 2009-03-06 Vertex Pharma 4-5-dihidro-[1,2,4]triazolo[4,3-f]pteridinas como inhibidores de la proteina-cinasa plk1 para el tratamiento de trastornos proliferativos.
JP2009535393A (ja) 2006-05-01 2009-10-01 ファイザー・プロダクツ・インク 置換2−アミノ縮合複素環式化合物
EP2026805A1 (en) 2006-05-08 2009-02-25 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
ES2365258T3 (es) 2006-06-26 2011-09-27 Ucb Pharma S.A. Derivados de tiazol condensados como inhibidores de quinasa.
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
MX2009006863A (es) 2006-12-20 2009-08-28 Schering Corp Inhibidores novedosos de c-jun-n-terminal cinasas.
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
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
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
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
US9259399B2 (en) 2007-11-07 2016-02-16 Cornell University Targeting CDK4 and CDK6 in cancer therapy
BRPI0821209A2 (pt) 2007-12-19 2019-09-24 Amgen Inc composto, composição farmacêutica, métodos de tratar câncer, para reduzir o tamanho de tumor, para tratar distúrbios, e para reduzir metástase em um tumor.
JP2011509078A (ja) 2007-12-28 2011-03-24 イプソゲン 乳癌発現プロファイリング
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
ATE531372T1 (de) 2008-04-07 2011-11-15 Amgen Inc Gem-disubstituierte und spirocyclische aminopyridine/pyrimidine als zellcyclus- inhibitoren
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
MX2013010871A (es) 2011-03-23 2014-01-31 Amgen Inc Inhibidores dobles triciclicos fusionados de cdk 4/6 y flt3.

Also Published As

Publication number Publication date
ES2620521T3 (es) 2017-06-28
US9359355B2 (en) 2016-06-07
AU2012230896B9 (en) 2015-06-18
KR20130140150A (ko) 2013-12-23
PH12013501940A1 (en) 2015-12-04
US20160368933A1 (en) 2016-12-22
DK2937349T3 (en) 2017-02-20
TW201302750A (zh) 2013-01-16
KR20160035613A (ko) 2016-03-31
WO2012129344A1 (en) 2012-09-27
US20120244110A1 (en) 2012-09-27
TWI438204B (zh) 2014-05-21
AU2012230896A1 (en) 2013-10-03
CA2830516A1 (en) 2012-09-27
MX2013010871A (es) 2014-01-31
HK1216889A1 (en) 2016-12-09
UY33969A (es) 2012-10-31
KR101606250B1 (ko) 2016-03-24
JP2014508808A (ja) 2014-04-10
PT2937349T (pt) 2017-03-24
EP2937349A1 (en) 2015-10-28
SG193580A1 (en) 2013-10-30
CN103703000A (zh) 2014-04-02
DK2688887T3 (en) 2015-06-29
ES2543569T3 (es) 2015-08-20
JP5647374B2 (ja) 2014-12-24
PT2688887E (pt) 2015-07-06
US20140163052A1 (en) 2014-06-12
HK1191014A1 (en) 2014-07-18
EP2937349B1 (en) 2016-12-28
US8623885B2 (en) 2014-01-07
MY161199A (en) 2017-04-14
CA2830516C (en) 2017-01-24
CN103703000B (zh) 2015-11-25
EP2688887A1 (en) 2014-01-29
EP2688887B1 (en) 2015-05-13
AU2012230896B2 (en) 2015-05-28
JO3073B1 (ar) 2017-03-15

Similar Documents

Publication Publication Date Title
AR085544A1 (es) Inhibidores triciclicos fusionados dobles de las cdk 4/6 y de la flt3
ES2618630T3 (es) Composiciones terapéuticas y métodos de uso relacionados
CO6150159A2 (es) Compuestos de heteroarilo utiles como inhibidores de enzimas de activacion e1
AR058546A1 (es) Derivados de 2- adamantilurea como inhibidores selectivos de 11 beta - hsd1
ES2685568T3 (es) Inhibidores de la isoquinolinona o quinazolinona fosfatidilinositol 3-quinasa
UY29702A1 (es) Inhibidores macrocíclicos del virus de hepatitis c
PE20060570A1 (es) Compuestos de quinazolina e isoquinolina piperidilo sustituidos como inhibidores de fosfodiesterasa pde-10
AR084312A1 (es) Compuestos triciclicos inhibidores de la pi3k y composiciones farmaceuticas
AR054560A1 (es) Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer
AR063022A1 (es) Derivados de indol antagonistas del receptor de glucagon, composiciones farmaceuticas que los contienen y usos para tratar diabetes mellitus tipo 2 y estados patologicos relacionados.
PE20011314A1 (es) DERIVADOS DE N-(4-CARBAMIMIDOIL-FENIL)-GLICINA COMO INHIBIDORES DE LA FORMACION DE FACTORES DE COAGULACION Xa IXa Y TROMBINA
AR062677A1 (es) Derivados de biaril-sulfonamida, procesos de produccion y composiciones farmaceuticas que los comprenden
AR062224A1 (es) Tetrazolilos macrociclicos como inhibidores de serina proteasa ns3 del virus de hepatitis c y composiciones farmaceuticas que los comprenden.
AR052902A1 (es) Derivados de piridazina, composicion farmaceutica que los contiene y su uso como agentes terapeuticos para enfermedades mediadas por la estearoil-coa desaturasa
AR065499A1 (es) Inhibidores de serino proteasas.composiciones farmaceuticas
AR082696A1 (es) Derivados heterociclicos nitrogenados de 1,2,4-oxadiazol, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades cardiovasculares e inflamatorias, entre otras
PE20091429A1 (es) 4-(4-ciano-2-tioaril)dihidropirimidinonas como inhibidores de la elastasa neutrofila humana (hne)
ECSP088149A (es) 3-acilaminobenzanilidas insecticidas
AR072085A1 (es) Compuestos triciclicos, metodos para su preparacion, composicion farma-ceutica que los comprende y su uso en el tratamiento de enfermedades me-diadas por la actividad de las proteinas quinasas
AR061369A1 (es) Derivados de pirimidina y composiciones farmaceuticas que los comprenden
AR039385A1 (es) Derivados de tioxantina como inhibidores de la mieloperoxidasa
ECSP055910A (es) Nuevos acidos carboxilicos y sus esteres, medicamentos que contienen estos compuestos y procedimientos para su preparacion
PE20170684A1 (es) Derivados de heterociclilo opcionalmente condensados de pirimidina utiles para el tratamiento de enfermedades inflamatorias, metabolicas, oncologicas y autoinmunitarias
AR083017A1 (es) Prodrogas de ester de [3-(1-(1h-imidazol-4-il)etil)-2-metilfenil]metanol
NI200800227A (es) Acidos 1,3-dioxano carboxilicos

Legal Events

Date Code Title Description
FB Suspension of granting procedure