PE20210177A1 - Inhibidores de cd73 - Google Patents

Inhibidores de cd73

Info

Publication number
PE20210177A1
PE20210177A1 PE2020001302A PE2020001302A PE20210177A1 PE 20210177 A1 PE20210177 A1 PE 20210177A1 PE 2020001302 A PE2020001302 A PE 2020001302A PE 2020001302 A PE2020001302 A PE 2020001302A PE 20210177 A1 PE20210177 A1 PE 20210177A1
Authority
PE
Peru
Prior art keywords
compound
nucleotidase
pyridazin
gem
dione
Prior art date
Application number
PE2020001302A
Other languages
English (en)
Inventor
Robert Dean Dally
Paredes Maria Cristina Garcia
Ii Lawrence Joseph Heinz
Jennifer Marie Howell
Frank George Njoroge
Yan Wang
Genshi Zhao
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 PE20210177A1 publication Critical patent/PE20210177A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invencion se refiere a un compuesto de formula (I); en donde, n es 0-3; R1 es -H, -F, -gem-difluoro, -gem-dimetilo, -C1-4 alquilo, -CHF2, -CHF2CH3 o -CH2CH2F; y R2 se selecciona de -H, -CH3, -F, -Cl, -CN, o -OCH3 o sales aceptables desde el punto de vista farmaceutico. Un compuesto seleccionado es 5-[5]-[2-cicloalquil]-6-piridazin-3-il]-1Hpirimidin-2,4-diona; 5-[5-[(1S,2R)-2-isopropilciclopropil]-6-metil-piridazin-3-il]-1H-pirimidin-2,4-diona. Dicho compuesto inhibe la actividad de CD73 (enzima 5'-nucleotidasa o ecto-5'nucleotidasa) y son utiles en el tratamiento contra el cancer.
PE2020001302A 2018-03-01 2019-02-22 Inhibidores de cd73 PE20210177A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862636978P 2018-03-01 2018-03-01
US201862775553P 2018-12-05 2018-12-05
PCT/US2019/019074 WO2019168744A1 (en) 2018-03-01 2019-02-22 Cd73 inhibitors

Publications (1)

Publication Number Publication Date
PE20210177A1 true PE20210177A1 (es) 2021-01-29

Family

ID=65686120

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2020001302A PE20210177A1 (es) 2018-03-01 2019-02-22 Inhibidores de cd73

Country Status (33)

Country Link
US (1) US11028074B2 (es)
EP (1) EP3759096B1 (es)
JP (1) JP6794560B2 (es)
KR (1) KR20200116965A (es)
CN (1) CN111819173B (es)
AU (1) AU2019228473B2 (es)
BR (1) BR112020016066A2 (es)
CA (1) CA3092661C (es)
CL (1) CL2020002158A1 (es)
CO (1) CO2020010191A2 (es)
CR (1) CR20200376A (es)
CY (1) CY1125145T1 (es)
DK (1) DK3759096T3 (es)
DO (1) DOP2020000148A (es)
EC (1) ECSP20052897A (es)
ES (1) ES2909701T3 (es)
HR (1) HRP20220459T1 (es)
IL (1) IL277006B2 (es)
JO (1) JOP20200209A1 (es)
LT (1) LT3759096T (es)
MA (1) MA52413A (es)
MX (1) MX2020009115A (es)
PE (1) PE20210177A1 (es)
PH (1) PH12020551464A1 (es)
PL (1) PL3759096T3 (es)
PT (1) PT3759096T (es)
RS (1) RS63073B1 (es)
SG (1) SG11202008366RA (es)
SI (1) SI3759096T1 (es)
TW (1) TWI702954B (es)
UA (1) UA123890C2 (es)
WO (1) WO2019168744A1 (es)
ZA (1) ZA202004805B (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220038453A (ko) * 2019-08-29 2022-03-28 일라이 릴리 앤드 캄파니 Cd73 억제제의 결정질 형태
US20210198239A1 (en) * 2019-12-06 2021-07-01 Plexxikon Inc. Compounds and methods for cd73 modulation and indications therefor
JP2023522949A (ja) * 2020-04-23 2023-06-01 オプナ バイオ ソシエテ アノニム Ｃｄ７３調節のための化合物及び方法並びにそれらの表示
BR112022020769A2 (pt) 2020-05-01 2022-12-20 Gilead Sciences Inc Compostos de 2,4-dioxopirimidina de inibição de cd73
WO2022007677A1 (zh) * 2020-07-07 2022-01-13 贝达药业股份有限公司 Cd73抑制剂及其在医药上的应用
CN116348118A (zh) 2020-09-08 2023-06-27 贝达药业股份有限公司 Cd73抑制剂及其在医药上的应用
CN114315839A (zh) * 2020-09-30 2022-04-12 武汉人福创新药物研发中心有限公司 嘧啶二酮类化合物及其用途
WO2022090711A1 (en) 2020-10-26 2022-05-05 AdoRx Therapeutics Limited Compounds as cd73 inhibitors
CN114437038A (zh) * 2020-11-05 2022-05-06 武汉人福创新药物研发中心有限公司 哒嗪炔烃类化合物及其用途
CN114437039A (zh) 2020-11-05 2022-05-06 武汉人福创新药物研发中心有限公司 Cd73抑制剂及其应用
WO2022121914A1 (zh) * 2020-12-10 2022-06-16 上海翰森生物医药科技有限公司 氧代氮环类衍生物调节剂、其制备方法和应用
WO2022195499A1 (en) * 2021-03-19 2022-09-22 Aurigene Discovery Technologies Limited Substituted pyridazine compounds as cd73 inhibitors
CA3235986A1 (en) 2021-10-29 2023-05-04 Gilead Science, Inc. Cd73 compounds
CN118829639A (zh) * 2022-03-07 2024-10-22 贝达药业股份有限公司 一种哒嗪类衍生物的晶型、制备方法及其应用
WO2023201267A1 (en) 2022-04-13 2023-10-19 Gilead Sciences, Inc. Combination therapy for treating trop-2 expressing cancers
US20240116928A1 (en) * 2022-07-01 2024-04-11 Gilead Sciences, Inc. Cd73 compounds
WO2024013206A1 (en) * 2022-07-14 2024-01-18 F. Hoffmann-La Roche Ag Heterocycle compounds for the treatment of cancer

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2434337T3 (es) 2006-04-03 2013-12-16 Glaxo Group Limited Derivados de azabiciclo[3.1.0]hexilo como moduladores de los receptores D3 de la dopamina
EP1860113A1 (en) 2006-05-24 2007-11-28 Rheinische Friedrich-Wilhelms-Universität Bonn Ectonucleotidase inhibitors
AR105654A1 (es) 2015-08-24 2017-10-25 Lilly Co Eli Anticuerpos pd-l1 (ligando 1 de muerte celular programada)
BR112018013827B1 (pt) * 2016-01-08 2024-02-20 Arcus Biosciences, Inc Moduladores de 5-nucleotidase, ecto, composição farmacêutica, combinação, kit e uso dos mesmos
WO2017153952A1 (en) * 2016-03-10 2017-09-14 Glaxosmithkline Intellectual Property Development Limited 5-sulfamoyl-2-hydroxybenzamide derivatives

Also Published As

Publication number Publication date
IL277006B (en) 2022-11-01
IL277006A (en) 2020-10-29
JP6794560B2 (ja) 2020-12-02
LT3759096T (lt) 2022-04-11
HRP20220459T1 (hr) 2022-05-27
US11028074B2 (en) 2021-06-08
CA3092661C (en) 2022-07-12
EP3759096B1 (en) 2022-02-16
WO2019168744A1 (en) 2019-09-06
TWI702954B (zh) 2020-09-01
PT3759096T (pt) 2022-03-30
JOP20200209A1 (ar) 2020-08-30
PL3759096T3 (pl) 2022-05-09
EP3759096A1 (en) 2021-01-06
UA123890C2 (uk) 2021-06-16
PH12020551464A1 (en) 2021-09-01
JP2020517655A (ja) 2020-06-18
RS63073B1 (sr) 2022-04-29
ECSP20052897A (es) 2020-09-30
CL2020002158A1 (es) 2020-11-13
TW201945002A (zh) 2019-12-01
AU2019228473B2 (en) 2021-02-25
CN111819173A (zh) 2020-10-23
BR112020016066A2 (pt) 2020-12-08
ZA202004805B (en) 2022-01-26
DOP2020000148A (es) 2020-09-15
SI3759096T1 (sl) 2022-07-29
US20210002257A1 (en) 2021-01-07
CY1125145T1 (el) 2024-02-16
CO2020010191A2 (es) 2020-08-31
IL277006B2 (en) 2023-03-01
KR20200116965A (ko) 2020-10-13
MX2020009115A (es) 2022-11-15
CN111819173B (zh) 2023-06-06
DK3759096T3 (en) 2022-03-07
AU2019228473A1 (en) 2020-08-20
CA3092661A1 (en) 2019-09-06
CR20200376A (es) 2020-10-23
SG11202008366RA (en) 2020-09-29
ES2909701T3 (es) 2022-05-10
MA52413A (fr) 2021-01-06

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