AR080197A1 - Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk 4/6 - Google Patents

Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk 4/6

Info

Publication number
AR080197A1
AR080197A1 ARP110100477A ARP110100477A AR080197A1 AR 080197 A1 AR080197 A1 AR 080197A1 AR P110100477 A ARP110100477 A AR P110100477A AR P110100477 A ARP110100477 A AR P110100477A AR 080197 A1 AR080197 A1 AR 080197A1
Authority
AR
Argentina
Prior art keywords
compound
inhibitors
cdk4
cancer
pirrolopirimidine
Prior art date
Application number
ARP110100477A
Other languages
English (en)
Inventor
Christopher Thomas Brain
Lawrence Blas Perez
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR080197A1 publication Critical patent/AR080197A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Los compuestos son inhibidores de la CDK4/6 y podrían ser utiles en el tratamiento de enfermedades y trastornos mediados por la CDK4/6, tales como el cáncer, incluyendo linfoma de células de manto, liposarcoma, cáncer pulmonar de células no pequenas, melanoma, cáncer esofágico de células escamosas y cáncer de mama. Además está dirigido a composiciones farmacéuticas que comprenden un compuesto, y a métodos de inhibir la actividad de la CDK4/6 y al tratamiento de trastornos asociados con la misma utilizando un compuesto o una composicion farmacéutica que comprende un compuesto. Reivindicacion 1: Un compuesto segun la formula (1) en donde: R1 es hidrogeno, metilo, CH2D, CHD2, o CD3; y R2 es CH2D, CHD2, o CD3 o una sal de los mismos.
ARP110100477A 2010-02-19 2011-02-17 Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk 4/6 AR080197A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US30624810P 2010-02-19 2010-02-19

Publications (1)

Publication Number Publication Date
AR080197A1 true AR080197A1 (es) 2012-03-21

Family

ID=44168434

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110100477A AR080197A1 (es) 2010-02-19 2011-02-17 Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk 4/6

Country Status (15)

Country Link
US (1) US20130203765A1 (es)
EP (1) EP2536727B1 (es)
JP (1) JP2013519708A (es)
KR (1) KR20130008557A (es)
CN (1) CN103003280A (es)
AR (1) AR080197A1 (es)
AU (1) AU2011217199B2 (es)
BR (1) BR112012020704A2 (es)
CA (1) CA2790641A1 (es)
EA (1) EA201201159A1 (es)
GT (1) GT201200242A (es)
MX (1) MX2012009606A (es)
TW (1) TW201136934A (es)
UY (1) UY33226A (es)
WO (1) WO2011101417A1 (es)

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GEP20135785B (en) 2008-08-22 2013-03-11 Novartis Ag Pyrrolopyrimidine compounds as cdk inhibitors
UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
EA201892726A1 (ru) * 2013-03-15 2019-04-30 Консерт Фармасьютикалс, Инк. Дейтерированный палбоциклиб
LT2968290T (lt) 2013-03-15 2019-12-10 G1 Therapeutics Inc Laikina normalių ląstelių apsauga chemoterapijos metu
JP6435315B2 (ja) * 2013-03-15 2018-12-05 ジー1、セラピューティクス、インコーポレイテッドG1 Therapeutics, Inc. 高活性抗新生物薬及び抗増殖剤
EP3033086B1 (en) 2013-08-14 2021-09-22 Novartis AG Combination therapy for the treatment of cancer
TWI558399B (zh) * 2014-02-26 2016-11-21 美國禮來大藥廠 癌症之組合療法
CN105294737B (zh) * 2014-07-26 2019-02-12 广东东阳光药业有限公司 Cdk类小分子抑制剂的化合物及其用途
WO2016040858A1 (en) 2014-09-12 2016-03-17 G1 Therapeutics, Inc. Combinations and dosing regimes to treat rb-positive tumors
KR102601320B1 (ko) * 2015-05-29 2023-11-10 데이진 화-마 가부시키가이샤 피리도[3,4-d]피리미딘 유도체 및 그 약학적으로 허용되는 염
CN106336412A (zh) * 2015-07-10 2017-01-18 南开大学 作为cdk4/6抑制剂的2-(n-氧化芳环-2基氨基)-吡咯并嘧啶及嘌呤类化合物
CN105130992B (zh) * 2015-07-16 2018-02-09 苏州大学 具有激酶抑制活性的含氮杂环化合物、制备方法和用途
US11077110B2 (en) 2016-03-18 2021-08-03 Tufts Medical Center Compositions and methods for treating and preventing metabolic disorders
CN108290899B (zh) * 2016-06-06 2020-09-18 深圳市塔吉瑞生物医药有限公司 一种取代的吡咯并嘧啶化合物及其应用
KR102466192B1 (ko) 2016-08-23 2022-11-14 에자이 알앤드디 매니지먼트 가부시키가이샤 간세포성 암종의 치료를 위한 조합 요법
CN106478641B (zh) * 2016-10-09 2018-07-24 杭州科巢生物科技有限公司 瑞博西尼中间体的合成方法
WO2018081211A1 (en) * 2016-10-26 2018-05-03 Li George Y Deuterated 7-cyclopentyl-n, n-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7h-pyrrolo[2,3-d]pyrimdine-6-carboxamide
WO2018170447A1 (en) 2017-03-16 2018-09-20 Eisai R&D Management Co., Ltd. Combination therapies for the treatment of breast cancer
AU2018354972B2 (en) * 2017-10-27 2021-07-08 Fresenius Kabi Oncology Ltd. An improved process for the preparation of ribociclib and its salts
AU2019205821B2 (en) 2018-01-08 2024-07-18 G1 Therapeutics, Inc. G1T38 superior dosage regimes
BR112020015431A2 (pt) 2018-02-15 2020-12-08 Nuvation Bio Inc. Compostos heterocíclicos como inibidores de quinase
JP7352981B2 (ja) * 2018-10-10 2023-09-29 深▲チェン▼市塔吉瑞生物医薬有限公司 ジヒドロイミダゾピラジノン化合物、該化合物を含む組成物およびその使用
CN111100128B (zh) * 2018-10-26 2022-09-06 广安凯特制药有限公司 一种瑞博西尼中间产品的合成方法及其中间体化合物
US10988479B1 (en) 2020-06-15 2021-04-27 G1 Therapeutics, Inc. Morphic forms of trilaciclib and methods of manufacture thereof
WO2022113003A1 (en) 2020-11-27 2022-06-02 Rhizen Pharmaceuticals Ag Cdk inhibitors
WO2022149057A1 (en) 2021-01-05 2022-07-14 Rhizen Pharmaceuticals Ag Cdk inhibitors
JP2024520461A (ja) * 2021-05-24 2024-05-24 大鵬薬品工業株式会社 Egfr及び/又はher2に異常を有するがんを有する対象の治療方法

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ATE314388T1 (de) * 1997-10-08 2006-01-15 Isotechnika Inc Deuterierte und undeuterierte cyclosporin-analoga und ihre verwendung als immunmodulierende agentien
CN101309917B (zh) * 2005-10-06 2013-09-11 奥斯拜客斯制药有限公司 具有增强治疗性质的胃h+,k+-atp酶氘代抑制剂
MX2008011868A (es) * 2006-03-16 2008-12-15 Vertex Pharma Inhibidores deuterados de la proteasa de la hepatitis c.
JO3235B1 (ar) 2006-05-26 2018-03-08 Astex Therapeutics Ltd مركبات بيررولوبيريميدين و استعمالاتها
US20080051422A1 (en) * 2006-08-22 2008-02-28 Concert Pharmaceuticals Inc. 4-Aminoquinazoline derivatives and methods of use thereof
CN101981036B (zh) * 2008-02-06 2013-09-04 诺瓦提斯公司 吡咯并[2,3-d]嘧啶及其作为酪氨酸激酶抑制剂的用途
GEP20135785B (en) * 2008-08-22 2013-03-11 Novartis Ag Pyrrolopyrimidine compounds as cdk inhibitors

Also Published As

Publication number Publication date
AU2011217199A1 (en) 2012-08-30
US20130203765A1 (en) 2013-08-08
CN103003280A (zh) 2013-03-27
GT201200242A (es) 2015-06-02
EA201201159A1 (ru) 2013-04-30
JP2013519708A (ja) 2013-05-30
WO2011101417A1 (en) 2011-08-25
BR112012020704A2 (pt) 2016-07-26
AU2011217199B2 (en) 2014-05-15
TW201136934A (en) 2011-11-01
CA2790641A1 (en) 2011-08-25
KR20130008557A (ko) 2013-01-22
UY33226A (es) 2011-09-30
EP2536727B1 (en) 2014-07-02
MX2012009606A (es) 2012-09-12
EP2536727A1 (en) 2012-12-26

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