PE20161362A1 - Derivados macrociclicos de pirimidina - Google Patents

Derivados macrociclicos de pirimidina

Info

Publication number
PE20161362A1
PE20161362A1 PE2016001882A PE2016001882A PE20161362A1 PE 20161362 A1 PE20161362 A1 PE 20161362A1 PE 2016001882 A PE2016001882 A PE 2016001882A PE 2016001882 A PE2016001882 A PE 2016001882A PE 20161362 A1 PE20161362 A1 PE 20161362A1
Authority
PE
Peru
Prior art keywords
hydrogen
alkyl
alkanediyl
macrociclic
pyrimidine
Prior art date
Application number
PE2016001882A
Other languages
English (en)
Inventor
Didier Jean-Claude Berthelot
Gaston Stanislas Marcella Diels
Werner Constant Johan Embrechts
Lieven Meerpoel
Berthold Wroblowski
Matthias Luc Aime Versele
Marcel Viellevoye
Marc Willems
Bruno Schoentjes
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 PE20161362A1 publication Critical patent/PE20161362A1/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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Se refiere a compuestos de formula I, donde: Xa, Xb y Xc son independientemente CH o N; X1 es -(CHR12)s-NR1-Xe-alcanodiil C1-C4- (SO2)p3- o –(CH2)s-O-Xe-alcanodiil C1-C4-(SO2)p3-; Xe es –C(=O)-, entre otros; a es NR4-C(=O)-[C(R5b)2]r, NR4-C(R5b)2-C(=O)- o C(=O)- NR4-C(R5b)2; b es i), donde Xd1 es CH o N, Xd2 es CH2 o NH; el anillo A es fenilo o piridilo; R1 es hidrogeno, alquilo C1-C4, entre otros; R12 es hidrogeno o alquilo C1-C4; o R1 y R12 se unen para formar alcanodiilo C1-C4, entre otros; s es 0, 1 o 2; p3 es es 0 o 1; R3 es hidrogeno, oxo, entre otros; R4 es hidrogeno, alquilo C1-C4 o alquiloxi C1-C4-alquilo C1-C4; R5b es hidrogeno, alquilo C1-C4, entre otros; p2 y r son 0, 1 o 2; R6 es hidrogeno, halo, entre otros; n es 1 o 2. Dichos compuestos son inhibidores de EF2K y opcionalmente tienen actividad inhibidora de Vps34, siendo utiles en el tratamiento de neoplasias malignas hematologicas y de tumores solidos como glioblastoma, meduloblastoma, entre otros
PE2016001882A 2014-04-03 2015-04-02 Derivados macrociclicos de pirimidina PE20161362A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14163443 2014-04-03
EP14183747 2014-09-05

Publications (1)

Publication Number Publication Date
PE20161362A1 true PE20161362A1 (es) 2016-12-17

Family

ID=52781117

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016001882A PE20161362A1 (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) PH12016501963A1 (es)
SG (1) SG11201608240RA (es)
UA (1) UA118219C2 (es)
WO (1) WO2015150555A1 (es)

Families Citing this family (14)

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CA3015005A1 (en) 2016-02-19 2017-08-24 Sprint Bioscience Ab 6-heterocyclyl-4-morpholin-4-ylpyridine-2-one compounds useful for the treatment of cancer and diabetes
PL3416945T3 (pl) 2016-02-19 2020-12-28 Sprint Bioscience Ab Związki 6-arylo-4-(morfolin-4-ylo)-1h-pirydyn-2-onu przydatne w leczeniu nowotworu i cukrzycy
EP3601236A1 (en) 2017-03-28 2020-02-05 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
WO2018177899A1 (en) 2017-03-28 2018-10-04 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
KR20200044025A (ko) 2017-08-23 2020-04-28 스프린트 바이오사이언스 아베 모르폴리닐피리돈 화합물
CA3072974A1 (en) 2017-08-23 2019-02-28 Sprint Bioscience Ab Pyridylpyridone compounds
ES2929424T3 (es) 2017-08-23 2022-11-29 Sprint Bioscience Ab Compuestos de piridinamina-piridona y pirimidinamina-piridona
TW202325708A (zh) 2017-08-23 2023-07-01 瑞典商斯普林特生物科技公司 氮雜吲哚基吡啶酮及二氮雜吲哚基吡啶酮化合物
MX2022010128A (es) * 2020-02-18 2023-01-04 Theseus Pharmaceuticals Inc Compuestos macrocíclicos y usos de estos.
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
CN118139846A (zh) * 2021-09-23 2024-06-04 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
WO2024094171A1 (zh) * 2022-11-04 2024-05-10 江苏恒瑞医药股份有限公司 取代的氨基嘧啶类化合物、其制备方法及其在医药上的应用

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CN1802159B (zh) 2003-03-24 2013-04-24 阿克西金药品公司 治疗哮喘及其它炎症或免疫性疾病的具有ccr3拮抗活性的2-苯氧基-和2-苯基磺酰胺衍生物
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Also Published As

Publication number Publication date
EP3126364A1 (en) 2017-02-08
CA2942636A1 (en) 2015-10-08
CN106164075A (zh) 2016-11-23
WO2015150555A1 (en) 2015-10-08
SG11201608240RA (en) 2016-10-28
AU2015239098A1 (en) 2016-09-29
BR112016021982B1 (pt) 2022-07-26
CA2942636C (en) 2023-03-21
IL248005B (en) 2018-12-31
JP6529513B2 (ja) 2019-06-12
UA118219C2 (uk) 2018-12-10
US10017509B2 (en) 2018-07-10
CN106164075B (zh) 2021-11-26
KR20160142316A (ko) 2016-12-12
PH12016501963B1 (en) 2017-01-09
BR112016021982A2 (es) 2017-08-15
EA031246B1 (ru) 2018-12-28
EA201692003A1 (ru) 2017-06-30
US20170022202A1 (en) 2017-01-26
EP3126364B1 (en) 2018-02-07
MX2016012992A (es) 2016-12-07
NZ725399A (en) 2023-01-27
JP2017509687A (ja) 2017-04-06
MA39822A (fr) 2018-02-06
MX369798B (es) 2019-11-21
ES2667723T3 (es) 2018-05-14
AU2015239098B2 (en) 2019-08-01
CL2016002461A1 (es) 2017-06-23
KR102390276B1 (ko) 2022-04-22
MY185491A (en) 2021-05-19
CN114213415A (zh) 2022-03-22
PH12016501963A1 (en) 2017-01-09

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