[go: up one dir, main page]

PE20180231A1 - Compuestos nucleosidos 5'-sustituidos - Google Patents

Compuestos nucleosidos 5'-sustituidos

Info

Publication number
PE20180231A1
PE20180231A1 PE2017002330A PE2017002330A PE20180231A1 PE 20180231 A1 PE20180231 A1 PE 20180231A1 PE 2017002330 A PE2017002330 A PE 2017002330A PE 2017002330 A PE2017002330 A PE 2017002330A PE 20180231 A1 PE20180231 A1 PE 20180231A1
Authority
PE
Peru
Prior art keywords
compounds
cancer
substituted
nucleosid
cyclopropoxy
Prior art date
Application number
PE2017002330A
Other languages
English (en)
Inventor
Guillermo S Cortez
Karl Robert Dahnke
Michael John Grogan
Hergueta Antonio Rodriguez
James Andrew Jamison
Brian Morgan Watson
Timothy Andrew Woods
Zahid Quyoom Bonday
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of PE20180231A1 publication Critical patent/PE20180231A1/es

Links

Classifications

    • 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
    • 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
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • 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
    • 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
    • A61K31/70Carbohydrates; 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
    • 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
    • A61K31/7068Compounds 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 having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • 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
    • A61K31/7076Compounds 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 containing purines, e.g. adenosine, adenylic acid

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Reproductive Health (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Saccharide Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Referido a un compuesto de formula (I), donde: R1a es ciclopropoxi; R1b es cloro; R2 es hidrogeno y R3 es amino. Estos compuestos son nucleosidos 5'-sustituidos, composiciones farmaceuticas que comprenden los compuestos. Tambien se refiere a metodos de utilizacion de los compuestos para tratar el cancer, en particular glioblastomas, melanoma, sarcomas, cancer gastrico, cancer de pancreas, colangiocarcinoma, cancer de vejiga, cancer de mama, cancer de pulmon de celulas no pequenas, leucemias que incluyen leucemia mieloide aguda y linfomas.
PE2017002330A 2015-05-04 2016-04-27 Compuestos nucleosidos 5'-sustituidos PE20180231A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP15382225 2015-05-04

Publications (1)

Publication Number Publication Date
PE20180231A1 true PE20180231A1 (es) 2018-01-31

Family

ID=53177322

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017002330A PE20180231A1 (es) 2015-05-04 2016-04-27 Compuestos nucleosidos 5'-sustituidos

Country Status (25)

Country Link
US (1) US9840532B2 (es)
EP (1) EP3292128A1 (es)
JP (2) JP6181889B1 (es)
KR (1) KR20170132871A (es)
CN (1) CN107580602A (es)
AR (1) AR104326A1 (es)
AU (1) AU2016258485A1 (es)
BR (1) BR112017020336A2 (es)
CA (1) CA2981097A1 (es)
CL (1) CL2017002637A1 (es)
CO (1) CO2017010727A2 (es)
CR (1) CR20170443A (es)
DO (1) DOP2017000255A (es)
EA (1) EA201792169A1 (es)
EC (1) ECSP17072987A (es)
HK (1) HK1244007A1 (es)
IL (1) IL254409A0 (es)
MA (1) MA42036A (es)
MX (1) MX2017014001A (es)
PE (1) PE20180231A1 (es)
PH (1) PH12017502002A1 (es)
SG (1) SG11201708345XA (es)
TN (1) TN2017000459A1 (es)
TW (1) TWI615400B (es)
WO (1) WO2016178870A1 (es)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112017017396A2 (pt) * 2015-02-24 2018-04-03 Pfizer derivados substituídos de nucleosídeos substituídos úteis como agentes anticancerígenos
EP3574917A4 (en) * 2017-01-27 2020-05-06 University of Miyazaki Anti-cancer agent, method for screening for anti-cancer agent, kit for determination of efficacy on cancer, and method for determining efficacy on cancer
WO2018152548A1 (en) 2017-02-20 2018-08-23 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
WO2018152501A1 (en) 2017-02-20 2018-08-23 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
WO2018160855A1 (en) 2017-03-01 2018-09-07 Prelude Therapeutics, Incorporated Selective inhibitors of protein arginine methyltransferase 5 (prmt5)
PL3665179T3 (pl) * 2017-08-09 2021-11-29 Prelude Therapeutics, Incorporated Selektywne inhibitory metylotransferazy argininowej białek 5 (prmt5)
JP7328218B2 (ja) * 2017-10-26 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
CA3085259A1 (en) 2017-12-13 2019-06-20 Lupin Limited Substituted bicyclic heterocyclic compounds as prmt5 inhibitors
US10711007B2 (en) 2018-03-14 2020-07-14 Prelude Therapeutics Incorporated Selective inhibitors of protein arginine methyltransferase 5 (PRMT5)
IL277263B2 (en) * 2018-03-14 2024-07-01 Prelude Therapeutics Inc Selective inhibitors of protein arginine methyltransferase 5 (PRMT5)
JP7337539B2 (ja) * 2018-06-21 2023-09-04 メディヴィル・アクチエボラーグ 白血病療法のための塩基修飾シチジンヌクレオチド
EP3833669A4 (en) * 2018-08-07 2022-05-11 Merck Sharp & Dohme Corp. PRMT5 INHIBITORS
MX2021009796A (es) * 2019-02-13 2021-09-08 Prelude Therapeutics Inc Inhibidores selectivos de la proteina arginina metiltransferasa 5 (prmt5).
SMT202400014T1 (it) 2019-06-10 2024-03-13 Lupin Ltd Inibitori di prmt5
MX2022004917A (es) 2019-10-22 2022-08-04 Lupin Ltd Combinación farmacéutica de inhibidores de prmt5.
MX2022006735A (es) 2019-12-03 2022-07-21 Lupin Ltd Análogos de nucleósidos sustituidos como inhibidores de la prmt5.
GB202117230D0 (en) 2021-11-29 2022-01-12 Argonaut Therapeutics Ltd Peptide vaccine
GB202203588D0 (en) 2022-03-15 2022-04-27 Argonaut Therapeutics Ltd Cancer diagnostic
CN116211869B (zh) * 2022-12-07 2023-08-01 浙江省肿瘤医院 含dna损伤修复抑制剂的药物混合物及混合方法、用途

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2381297A1 (en) * 1999-08-27 2001-04-19 Esmir Gunic Pyrrolo¬2,3-d|pyrimidine nucleoside analogs
NZ544187A (en) * 2005-12-15 2008-07-31 Ind Res Ltd Deazapurine analogs of 1'-aza-l-nucleosides
WO2011079236A1 (en) 2009-12-22 2011-06-30 The Ohio State University Research Foundation Compositions and methods for cancer detection and treatment
US9416154B2 (en) * 2011-07-13 2016-08-16 Merck Sharp & Dohme Corp. 5′-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
US10118918B2 (en) 2012-12-21 2018-11-06 Epizyme, Inc. PRMT5 inhibitors and uses thereof
JP2016505002A (ja) 2012-12-21 2016-02-18 エピザイム,インコーポレイティド ジヒドロイソキノリンまたはテトラヒドロイソキノリンを含有するprmt5阻害剤およびその使用
EP2935242A2 (en) 2012-12-21 2015-10-28 Epizyme, Inc. Methods of inhibiting prmt5
EP3498701B1 (en) 2012-12-21 2023-02-22 Epizyme Inc Prmt5 inhibitors and uses thereof
WO2014100695A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. Prmt5 inhibitors and uses thereof
US9365555B2 (en) 2012-12-21 2016-06-14 Epizyme, Inc. PRMT5 inhibitors and uses thereof
BR112017017396A2 (pt) * 2015-02-24 2018-04-03 Pfizer derivados substituídos de nucleosídeos substituídos úteis como agentes anticancerígenos

Also Published As

Publication number Publication date
SG11201708345XA (en) 2017-11-29
BR112017020336A2 (pt) 2019-05-14
PH12017502002A1 (en) 2018-03-26
US20160326208A1 (en) 2016-11-10
HK1244007A1 (zh) 2018-07-27
CN107580602A (zh) 2018-01-12
WO2016178870A1 (en) 2016-11-10
ECSP17072987A (es) 2018-02-28
KR20170132871A (ko) 2017-12-04
CR20170443A (es) 2017-11-07
CO2017010727A2 (es) 2018-01-31
TN2017000459A1 (en) 2019-04-12
AR104326A1 (es) 2017-07-12
MX2017014001A (es) 2018-03-16
JP6181889B1 (ja) 2017-08-16
CL2017002637A1 (es) 2018-04-20
JP2017125029A (ja) 2017-07-20
IL254409A0 (en) 2017-11-30
US9840532B2 (en) 2017-12-12
TWI615400B (zh) 2018-02-21
TW201712022A (zh) 2017-04-01
MA42036A (fr) 2018-03-14
JP2017525667A (ja) 2017-09-07
CA2981097A1 (en) 2016-11-10
EA201792169A1 (ru) 2018-03-30
EP3292128A1 (en) 2018-03-14
DOP2017000255A (es) 2018-01-15
AU2016258485A1 (en) 2017-10-12

Similar Documents

Publication Publication Date Title
PE20180231A1 (es) Compuestos nucleosidos 5'-sustituidos
AR123996A2 (es) Compuestos tricíclicos novedosos como agentes antineoplásicos
CL2018003323A1 (es) Piridinas sustituidas con heteroarilo y métodos de uso.
DOP2022000172A (es) Compuestos de piperidina urea 4-metilsulfonil-sustituidos para el tratamiento de miocardiopatía dilatada (mcd)
CO2019009373A2 (es) Compuestos heterocíclicos útiles como inhibidores duales de atx/ca.
PH12017502090A1 (en) Heterocyclic amides as kinase inhibitors
PH12015501934B1 (en) New octahydro - pyrrolo [3,4-c] - pyrrole derivatives and analogs thereof as autotaxin inhibitors
CL2012000324A1 (es) Compuestos derivados de benciimidazol sustituido con un grupo pirazol sustituido, inhibidor de quinasa fgfr; composicion farmaceutica que los comprende; y su uso en el tratamiento del cancer.
CL2017000507A1 (es) Derivados de benzodiazepina citotóxicos
PH12018500408A1 (en) Bicyclic compounds as atx inhibitors
MX371034B (es) Derivados de amidas policíclicas como inhibidores de cdk9.
MX2018001890A (es) Compuestos biciclicos como inhibidores de autotaxina (atx).
MX2017015294A (es) Administracion intrapulmonar de agonistas de polinucleotidos del receptor 9 tipo toll para el tratamiento contra el cancer de pulmon.
PH12018500409A1 (en) New bicyclic compounds as dual atx/ca inhibitors
MX388321B (es) Compuestos de aminopurina sustituida, composiciones del mismo, y metodos de tratamiento con los mismos.
ECSP17020172A (es) Inhibidores de histona desmetilasa
CU20090161A7 (es) Pirimidinil-piperazinas útiles como ligandos del receptor d3/d2
MX2020003921A (es) Proceso para producir compuestos de tipo piridazinona herbicidas.
JOP20190163B1 (ar) منشط nrf2
BR112019003130A2 (pt) agonista de ppargama para tratamento de cânceres de sangue
SV2016005310A (es) Derivados de diheterociclo enlazado a cicloalquilo
AR106958A1 (es) Derivados de tetrahidrotriazolopirimidina útiles como inhibidores de hne
MX2020003922A (es) Proceso para producir compuestos de piridazinona herbicida.
PH12018500406A1 (en) Bicyclic compounds as atx inhibitors
PH12018500407A1 (en) New bicyclic compounds as dual atx/ca inhibitors

Legal Events

Date Code Title Description
FD Application declared void or lapsed