MX2016012992A - Derivados macrociclicos de pirimidina. - Google Patents

Derivados macrociclicos de pirimidina.

Info

Publication number
MX2016012992A
MX2016012992A MX2016012992A MX2016012992A MX2016012992A MX 2016012992 A MX2016012992 A MX 2016012992A MX 2016012992 A MX2016012992 A MX 2016012992A MX 2016012992 A MX2016012992 A MX 2016012992A MX 2016012992 A MX2016012992 A MX 2016012992A
Authority
MX
Mexico
Prior art keywords
compounds
pyrimidine derivatives
inhibitory activity
present
macrocylic
Prior art date
Application number
MX2016012992A
Other languages
English (en)
Other versions
MX369798B (es
Inventor
Lieven Meerpoel
Gaston Stanislas Marcella Diels
Marc Willems
Marcel Viellevoye
Bruno Schoentjes
Wroblowski Berthold
Luc Aimé Versele Mathias
Constant Johan Embrechts Werner
Jean- Claude Berthelot Didier
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of MX2016012992A publication Critical patent/MX2016012992A/es
Publication of MX369798B publication Critical patent/MX369798B/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/22—Heterocyclic 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 systems contains four or more hetero rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente invención se refiere a derivados sustituidos de pirimidina macrocíclica de Fórmula (I) (ver Fórmula) en donde las variables tienen el significado definido en las reivindicaciones; los compuestos de acuerdo con la presente invención tienen actividad inhibidora de EF2K y opcionalmente también actividad inhibidora de Vps34; la invención también se refiere a procesos para preparar tales compuestos novedosos, a composiciones farmacéuticas que comprenden dichos compuestos como principio activo, así como al uso de dichos compuestos como medicamento.
MX2016012992A 2014-04-03 2015-04-02 Derivados macrociclicos de pirimidina. MX369798B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14163443 2014-04-03
EP14183747 2014-09-05
PCT/EP2015/057399 WO2015150555A1 (en) 2014-04-03 2015-04-02 Macrocylic pyrimidine derivatives

Publications (2)

Publication Number Publication Date
MX2016012992A true MX2016012992A (es) 2016-12-07
MX369798B MX369798B (es) 2019-11-21

Family

ID=52781117

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016012992A MX369798B (es) 2014-04-03 2015-04-02 Derivados macrociclicos de pirimidina.

Country Status (21)

Country Link
US (1) US10017509B2 (es)
EP (1) EP3126364B1 (es)
JP (1) JP6529513B2 (es)
KR (1) KR102390276B1 (es)
CN (2) CN106164075B (es)
AU (1) AU2015239098B2 (es)
BR (1) BR112016021982B1 (es)
CA (1) CA2942636C (es)
CL (1) CL2016002461A1 (es)
EA (1) EA031246B1 (es)
ES (1) ES2667723T3 (es)
IL (1) IL248005B (es)
MA (1) MA39822A (es)
MX (1) MX369798B (es)
MY (1) MY185491A (es)
NZ (1) NZ725399A (es)
PE (1) PE20161362A1 (es)
PH (1) PH12016501963B1 (es)
SG (1) SG11201608240RA (es)
UA (1) UA118219C2 (es)
WO (1) WO2015150555A1 (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS60900B1 (sr) 2016-02-19 2020-11-30 Sprint Bioscience Ab Jedinjenja 6-heterociklil-4-morfolin-4-ilpiridin-2-ona korisna za lečenje kancera i dijabetesa
HUE050863T2 (hu) 2016-02-19 2021-01-28 Sprint Bioscience Ab Rák és cukorbetegség kezelésére alkalmazható 6-aril-4-(morfolin-4-il)-1H-piridin-2-on vegyületek
PL3601253T3 (pl) 2017-03-28 2022-01-17 Bayer Aktiengesellschaft Nowe hamujące ptefb związki makrocykliczne
US11242356B2 (en) 2017-03-28 2022-02-08 Bayer Aktiengesellschaft PTEFb inhibiting macrocyclic compounds
CA3073142A1 (en) 2017-08-23 2019-02-28 Sprint Bioscience Ab Morpholinylpyridone compounds
US11208423B2 (en) 2017-08-23 2021-12-28 Sprint Bioscience Ab Pyridinamine-pyridone and pyrimidinamine- pyridone compounds
JP7199738B2 (ja) 2017-08-23 2023-01-06 スプリント バイオサイエンス アクティエボラーグ アザインドリルピリドンおよびジアザインドリルピリドン化合物
ES2910839T3 (es) 2017-08-23 2022-05-13 Sprint Bioscience Ab Compuestos de piridilpiridona
CN115551868A (zh) * 2020-02-18 2022-12-30 特修斯制药公司 大环化合物和其用途
CN113735856A (zh) * 2020-05-29 2021-12-03 百极弘烨(南通)医药科技有限公司 大环jak抑制剂及其应用
WO2023046030A1 (zh) * 2021-09-23 2023-03-30 河南晟翔医药科技有限公司 一种egfr小分子抑制剂、含其的药物组合物及其用途
KR102613509B1 (ko) * 2021-12-15 2023-12-13 환인제약 주식회사 마크로사이클릭 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 신경 퇴행성 질환의 예방 또는 치료용 약학적 조성물
WO2024078263A1 (zh) * 2022-10-09 2024-04-18 药雅科技(上海)有限公司 大环杂环类化合物作为egfr抑制剂的制备及其应用

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004078682A2 (en) * 2003-03-05 2004-09-16 Irm Llc Cyclic compounds and compositions as protein kinase inhibitors
BRPI0408682A (pt) 2003-03-24 2006-03-28 Actimis Pharmaceuticals Inc derivado de benzenossulfonamida, medicamento, uso do derivado de benzenossulfonamida, e, processo para controlar uma doença ou distúrbio inflamatórios ou imuno-reguladores em humanos e animais
PA8603801A1 (es) 2003-05-27 2004-12-16 Janssen Pharmaceutica Nv Derivados de la quinazolina
WO2005058318A1 (en) 2003-12-18 2005-06-30 Janssen Pharmaceutica N.V. 3-cyano-quinoline derivatives with antiproliferative activity
MXPA06007017A (es) 2003-12-18 2006-08-31 Janssen Pharmaceutica Nv Derivados de pirido y pirimidopirimidina como agentes antiproliferativos.
JO3088B1 (ar) 2004-12-08 2017-03-15 Janssen Pharmaceutica Nv مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف
MY169441A (en) * 2004-12-08 2019-04-11 Janssen Pharmaceutica Nv 2,4, (4,6) pyrimidine derivatives
CN101341138B (zh) * 2005-06-30 2012-11-14 詹森药业有限公司 作为gsk-3抑制剂的环状苯胺基-吡啶并三嗪类
US8143255B2 (en) * 2005-11-16 2012-03-27 S*Bio Pte Ltd. Heteroalkyl linked pyrimidine derivatives
EP1961149B1 (en) 2005-11-24 2018-08-08 Synchronica plc Method for securely associating data with http and https sessions
DK2170827T3 (da) 2007-06-21 2013-11-18 Janssen Pharmaceutica Nv Indolin-2-oner og aza-indolin-2-oner
DK2185562T3 (en) 2007-07-27 2016-02-22 Janssen Pharmaceutica Nv PYRROLOPYRIMIDINES SUITABLE FOR TREATING PROLIFERATIVE DISEASES
TW200922556A (en) 2007-08-20 2009-06-01 Glaxo Group Ltd Novel cathepsin C inhibitors and their use
US8318929B2 (en) * 2008-03-10 2012-11-27 Janssen Pharmaceutica Nv 4-aryl-2-anilino-pyrimidines
KR20110031318A (ko) 2008-06-13 2011-03-25 노파르티스 아게 Ｉａ 심부전 및 암 치료에 유용한 단백질 키나제 ｄ 억제제로서의 2,4'-비피리디닐 화합물
BRPI1011612A2 (pt) 2009-05-28 2019-09-24 Tetralogic Pharm Corp composto, composição farmacêutica, e, métodos para induzir apoptose em uma célula, para tratar câncer, e para tratar uma doença autoimune.
WO2011008788A1 (en) 2009-07-14 2011-01-20 Dawei Zhang Fluoro-substituted compounds as kinase inhibitors and methods of use thereof
TWI513695B (zh) 2009-10-27 2015-12-21 Merck Sharp & Dohme （１，１，１，３，３，３－六氟－２－羥基丙－２－基）苯基衍生物

Also Published As

Publication number Publication date
PH12016501963A1 (en) 2017-01-09
CN106164075B (zh) 2021-11-26
ES2667723T3 (es) 2018-05-14
AU2015239098B2 (en) 2019-08-01
AU2015239098A1 (en) 2016-09-29
KR20160142316A (ko) 2016-12-12
EA031246B1 (ru) 2018-12-28
KR102390276B1 (ko) 2022-04-22
MA39822A (fr) 2018-02-06
PE20161362A1 (es) 2016-12-17
IL248005B (en) 2018-12-31
CA2942636A1 (en) 2015-10-08
MX369798B (es) 2019-11-21
JP6529513B2 (ja) 2019-06-12
CN106164075A (zh) 2016-11-23
UA118219C2 (uk) 2018-12-10
BR112016021982A2 (es) 2017-08-15
EA201692003A1 (ru) 2017-06-30
EP3126364B1 (en) 2018-02-07
BR112016021982B1 (pt) 2022-07-26
MY185491A (en) 2021-05-19
PH12016501963B1 (en) 2017-01-09
CN114213415A (zh) 2022-03-22
WO2015150555A1 (en) 2015-10-08
US10017509B2 (en) 2018-07-10
US20170022202A1 (en) 2017-01-26
SG11201608240RA (en) 2016-10-28
EP3126364A1 (en) 2017-02-08
CA2942636C (en) 2023-03-21
NZ725399A (en) 2023-01-27
CL2016002461A1 (es) 2017-06-23
JP2017509687A (ja) 2017-04-06

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