PE20171449A1 - Derivados de nucleosidos sustituidos utiles como agentes antineoplasicos - Google Patents

Derivados de nucleosidos sustituidos utiles como agentes antineoplasicos

Info

Publication number
PE20171449A1
PE20171449A1 PE2017001447A PE2017001447A PE20171449A1 PE 20171449 A1 PE20171449 A1 PE 20171449A1 PE 2017001447 A PE2017001447 A PE 2017001447A PE 2017001447 A PE2017001447 A PE 2017001447A PE 20171449 A1 PE20171449 A1 PE 20171449A1
Authority
PE
Peru
Prior art keywords
alkyl
nucleosid
substitute
antineoplastic agents
derivatives useful
Prior art date
Application number
PE2017001447A
Other languages
English (en)
Inventor
John Howard Tatlock
Indrawan James Mcalpine
Michelle Bich Tran-Dube
Eugene Yuanjin Rui
Martin James Wythes
Robert Arnold Kumpf
Michele Ann Mctigue
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of PE20171449A1 publication Critical patent/PE20171449A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/14Pyrrolo-pyrimidine radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • 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
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • C07H19/167Purine radicals with ribosyl as the saccharide radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/23Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups C07H19/14 - C07H19/22
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/24Heterocyclic radicals containing oxygen or sulfur as ring hetero atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Se refiere a un derivado de nucleosido sustituido de formula (I) o una sal farmaceuticamente aceptable, donde: R1 es (C3-C8)alquilo, (C1-C8)haloalquilo, entre otros; R2 es H, halogeno, entre otros; R3 es H, hidroxi, entre otros; Q esta ausente o es una porcion divalente de O, S, NH o (C1-C8)alquileno; U es OR6, SR6, entre otros; V, W,X son N o C, en donde si cada uno forma un enlace doble, cada uno es C; Y es CR10, N, entre otros; R10 es H, (C1-C8)alquilo, hidroxi, entre otros; R6 es H, (C1-C8)alquilo, entre otros; Z es CR12, N, NR12, entre otros; R12 es H, (C1-C8)alquilo, entre otros;----- es un enlace opcional, en donde no mas de dos ----- no adyacentes pueden estar presentes; m y n son 0-1. Es un compuesto seleccionado el (3,4-difluorofenil)(2S,3S,4R,5R)-3,4-dihidroxi-5-(4-metil-7H-pirrolo[2,3-d]pirimidin-7-il)tetrahidrofuran-2-il)metanona; entre otros. Tambien se refiere una composicion farmaceutica que lo comprenda. Dicho derivado es util como agente antineoplasico
PE2017001447A 2015-02-24 2016-02-15 Derivados de nucleosidos sustituidos utiles como agentes antineoplasicos PE20171449A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562119932P 2015-02-24 2015-02-24
US201562213801P 2015-09-03 2015-09-03
US201662279209P 2016-01-15 2016-01-15

Publications (1)

Publication Number Publication Date
PE20171449A1 true PE20171449A1 (es) 2017-10-02

Family

ID=55451515

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017001447A PE20171449A1 (es) 2015-02-24 2016-02-15 Derivados de nucleosidos sustituidos utiles como agentes antineoplasicos

Country Status (29)

Country Link
US (1) US10428104B2 (es)
EP (1) EP3262057B1 (es)
JP (1) JP6584521B2 (es)
KR (1) KR20170119705A (es)
CN (1) CN107278205A (es)
AU (2) AU2016225133B2 (es)
BR (1) BR112017017396A2 (es)
CA (1) CA2921314A1 (es)
CL (1) CL2017002155A1 (es)
CO (1) CO2017008403A2 (es)
CR (1) CR20170384A (es)
CU (1) CU20170105A7 (es)
DO (1) DOP2017000195A (es)
EA (1) EA031895B1 (es)
ES (1) ES2792899T3 (es)
GT (1) GT201700189A (es)
IL (1) IL253637A0 (es)
MX (1) MX2017010844A (es)
NI (1) NI201700095A (es)
PE (1) PE20171449A1 (es)
PH (1) PH12017501413A1 (es)
SG (1) SG11201706050WA (es)
SV (1) SV2017005514A (es)
TN (1) TN2017000357A1 (es)
TW (1) TWI622595B (es)
UA (1) UA118315C2 (es)
UY (1) UY36564A (es)
WO (1) WO2016135582A1 (es)
ZA (1) ZA201705092B (es)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR104326A1 (es) * 2015-05-04 2017-07-12 Lilly Co Eli Compuestos nucleósidos 5-sustituidos
TW202321249A (zh) 2015-08-26 2023-06-01 比利時商健生藥品公司 使用作為prmt5抑制劑之新穎經6-6雙環芳香環取代之核苷類似物
WO2017153186A1 (en) 2016-03-10 2017-09-14 Janssen Pharmaceutica Nv Substituted nucleoside analogues for use as prmt5 inhibitors
JP6909799B2 (ja) * 2016-03-10 2021-07-28 ヤンセン ファーマシューティカ エヌ.ベー. Prmt5阻害剤として使用するための置換ヌクレオシドアナログ
US12084462B2 (en) 2016-09-14 2024-09-10 Janssen Pharmaceutica Nv Spiro bicyclic inhibitors of menin-MLL interaction
MX2019002959A (es) 2016-09-14 2019-07-04 Janssen Pharmaceutica Nv Inhibidores biciclicos condensados de la interaccion de menina-mll.
KR102493644B1 (ko) 2016-09-14 2023-01-30 얀센 파마슈티카 엔.브이. 메닌-mll 상호작용의 스피로 바이사이클릭 억제제
EP3519413A1 (en) 2016-10-03 2019-08-07 Janssen Pharmaceutica NV Novel monocyclic and bicyclic ring system substituted carbanucleoside analogues for use as prmt5 inhibitors
CA3044739A1 (en) 2016-12-15 2018-06-21 Janssen Pharmaceutica Nv Azepane inhibitors of menin-mll interaction
WO2018152501A1 (en) * 2017-02-20 2018-08-23 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
WO2018152548A1 (en) * 2017-02-20 2018-08-23 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
EA201990851A1 (ru) 2017-02-24 2019-09-30 Янссен Фармацевтика Нв Новые аналоги карбануклеозида, замещенные моноциклической и бициклической кольцевой системой, для применения в качестве ингибиторов prmt5
US11279970B2 (en) 2017-02-27 2022-03-22 Janssen Pharmaceutica Nv Use of biomarkers in identifying cancer patients that will be responsive to treatment with a PRMT5 inhibitor
WO2018160855A1 (en) 2017-03-01 2018-09-07 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
ES2885180T3 (es) * 2017-08-09 2021-12-13 Prelude Therapeutics Inc Inhibidores selectivos de la proteína arginina metiltransferasa 5 (PRMT5)
CN111542525B (zh) * 2017-10-26 2023-06-27 普莱鲁德疗法有限公司 蛋白质精氨酸甲基转移酶5(prmt5)的选择性抑制剂
EP3720865B1 (en) * 2017-12-08 2024-03-13 Janssen Pharmaceutica NV Novel spirobicyclic analogues
US11459330B2 (en) 2017-12-13 2022-10-04 Lupin Limited Substituted bicyclic heterocyclic compounds as PRMT5 inhibitors
US11396517B1 (en) 2017-12-20 2022-07-26 Janssen Pharmaceutica Nv Exo-aza spiro inhibitors of menin-MLL interaction
US10711007B2 (en) 2018-03-14 2020-07-14 Prelude Therapeutics Incorporated Selective inhibitors of protein arginine methyltransferase 5 (PRMT5)
JP7328241B2 (ja) * 2018-03-14 2023-08-16 プレリュード セラピューティクス,インコーポレイティド タンパク質アルギニンメチルトランスフェラーゼ5(prmt5)の選択的阻害剤
WO2020033285A1 (en) * 2018-08-07 2020-02-13 Merck Sharp & Dohme Corp. Prmt5 inhibitors
CN113811539A (zh) * 2019-02-13 2021-12-17 普莱鲁德疗法有限公司 蛋白质精氨酸甲基转移酶5(prmt5)的选择性抑制剂
SG11202110272SA (en) * 2019-03-25 2021-10-28 California Inst Of Techn Prmt5 inhibitors and uses thereof
TW202112375A (zh) 2019-06-06 2021-04-01 比利時商健生藥品公司 使用prmt5抑制劑治療癌症之方法
JP2022536337A (ja) 2019-06-10 2022-08-15 ルピン・リミテッド Prmt5阻害剤
EP3983393A1 (en) 2019-06-12 2022-04-20 Janssen Pharmaceutica NV Novel spirobicyclic intermediates
CA3156135A1 (en) 2019-10-22 2021-04-29 Lupin Limited PHARMACEUTICAL COMBINATION OF PRMT5 INHIBITORS
JP2023504279A (ja) 2019-12-03 2023-02-02 ルピン・リミテッド Prmt5阻害剤としての置換ヌクレオシドアナログ
PE20231308A1 (es) 2020-08-18 2023-08-24 Incyte Corp Proceso e intermedios para preparar un inhibidor de jak1
IL300555A (en) 2020-08-18 2023-04-01 Incyte Corp Process and intermediates for preparing a JAK inhibitor
WO2022074391A1 (en) * 2020-10-08 2022-04-14 Storm Therapeutics Limited Compounds inhibitors of mettl3
CN112679505B (zh) * 2020-12-25 2022-04-22 杭州澳赛诺生物科技有限公司 一种4-甲基-7H-吡咯并[2,3-d]嘧啶的合成方法
WO2022153161A1 (en) 2021-01-14 2022-07-21 Pfizer Inc. Treatment of cancer using a prmt5 inhibitor
EP4370504A1 (en) 2021-07-12 2024-05-22 Incyte Corporation Process and intermediates for preparing baricitinib
WO2023017152A1 (en) * 2021-08-13 2023-02-16 Albert-Ludwigs-Universität Freiburg Specific small molecule inhibitors that block kmt9 methyltransferase activity and function
WO2024170488A1 (en) 2023-02-13 2024-08-22 Astrazeneca Ab Prmt5 inhibitor for use in cancer therapy

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5795977A (en) * 1989-09-15 1998-08-18 Metabasis Therapeutics, Inc. Water soluble adenosine kinase inhibitors
US5646128A (en) * 1989-09-15 1997-07-08 Gensia, Inc. Methods for treating adenosine kinase related conditions
US5864033A (en) * 1989-09-15 1999-01-26 Metabasis Therapeutics, Inc. Adenosine kinase inhibitors
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
WO2000035296A1 (en) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Improved release of medicament active agents from a chewing gum coating
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
GB9813554D0 (en) * 1998-06-23 1998-08-19 Glaxo Group Ltd Chemical compounds
US6831069B2 (en) * 1999-08-27 2004-12-14 Ribapharm Inc. Pyrrolo[2,3-d]pyrimidine nucleoside analogs
US7022681B2 (en) * 2002-08-15 2006-04-04 Cv Therapeutics, Inc. Partial and full agonists of A1 adenosine receptors
EP2408306A4 (en) * 2009-03-20 2012-11-07 Alios Biopharma Inc SUBSTITUTED NUCLEOSIDE AND NUCLEOTIDE ANALOGUES
US20120077814A1 (en) 2010-09-10 2012-03-29 Zhong Wang Sulfonamide, sulfamate, and sulfamothioate derivatives
WO2013009735A1 (en) * 2011-07-13 2013-01-17 Merck Sharp & Dohme Corp. 5'-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
WO2013044030A1 (en) * 2011-09-23 2013-03-28 Enanta Pharmaceuticals, Inc. 2'-chloroacetylenyl substituted nucleoside derivatives
EP3160477A4 (en) * 2014-06-25 2018-07-04 Epizyme, Inc. Prmt5 inhibitors and uses thereof
AR104326A1 (es) * 2015-05-04 2017-07-12 Lilly Co Eli Compuestos nucleósidos 5-sustituidos
MX2018001073A (es) * 2015-08-06 2018-06-12 Chimerix Inc Nucleosidos de pirrolopirimidina y analogos de los mismos utiles como agentes antivirales.

Also Published As

Publication number Publication date
CR20170384A (es) 2017-11-16
CU20170105A7 (es) 2017-10-05
KR20170119705A (ko) 2017-10-27
SG11201706050WA (en) 2017-09-28
EA201791563A1 (ru) 2018-01-31
EP3262057A1 (en) 2018-01-03
WO2016135582A1 (en) 2016-09-01
EP3262057B1 (en) 2020-04-15
US20160244475A1 (en) 2016-08-25
ES2792899T3 (es) 2020-11-12
TWI622595B (zh) 2018-05-01
TW201643176A (zh) 2016-12-16
UY36564A (es) 2016-09-30
AU2018278842A1 (en) 2019-01-03
BR112017017396A2 (pt) 2018-04-03
PH12017501413A1 (en) 2018-01-29
CO2017008403A2 (es) 2017-10-31
CL2017002155A1 (es) 2018-05-11
DOP2017000195A (es) 2017-10-15
AU2016225133B2 (en) 2018-11-29
TN2017000357A1 (en) 2019-01-16
IL253637A0 (en) 2017-09-28
CN107278205A (zh) 2017-10-20
CA2921314A1 (en) 2016-08-24
JP2018510850A (ja) 2018-04-19
ZA201705092B (en) 2019-06-26
US10428104B2 (en) 2019-10-01
EA031895B1 (ru) 2019-03-29
MX2017010844A (es) 2017-12-07
SV2017005514A (es) 2018-04-11
UA118315C2 (uk) 2018-12-26
NI201700095A (es) 2017-10-31
AU2016225133A1 (en) 2017-08-10
GT201700189A (es) 2019-06-10
JP6584521B2 (ja) 2019-10-02

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