AR075894A1 - Derivados oxidados de triazolilpurinas utiles como ligandos de receptor de adenosina a2a y su uso como medicamentos. - Google Patents

Derivados oxidados de triazolilpurinas utiles como ligandos de receptor de adenosina a2a y su uso como medicamentos.

Info

Publication number
AR075894A1
AR075894A1 ARP100100883A ARP100100883A AR075894A1 AR 075894 A1 AR075894 A1 AR 075894A1 AR P100100883 A ARP100100883 A AR P100100883A AR P100100883 A ARP100100883 A AR P100100883A AR 075894 A1 AR075894 A1 AR 075894A1
Authority
AR
Argentina
Prior art keywords
alkyl
branched
linear
group
independently
Prior art date
Application number
ARP100100883A
Other languages
English (en)
Inventor
Walter Cabri
Giovanni Piersanti
Patrizia Minetti
Giorgio Tarzia
Original Assignee
Sigma Tau Ind Farmaceuti
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 Sigma Tau Ind Farmaceuti filed Critical Sigma Tau Ind Farmaceuti
Publication of AR075894A1 publication Critical patent/AR075894A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
    • A61K31/198Alpha-aminoacids, e.g. alanine, edetic acids [EDTA]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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

Abstract

También se refiere a procesos para su preparacion y a composiciones farmacéuticas que los contienen, para el tratamiento de trastornos neurologicos o isquemia cerebral, para los cuales la inhibicion de receptor de adenosina A2A dará como resultado la mejoría del estado de salud de un paciente. Reivindicacion 1: Un compuesto que tiene la formula general 1: R1 = es alquilo C1-6 lineal o ramificado; R2 es un grupo de la formula R9-(CHR8)p-(CR6R7)m-(CR4R5)n-; R4, R6 y R8 son, independientemente H, hidroxilo o =O, con el significado de carbonilo; R5, R7 y R9 son, independientemente, H o están ausentes; m, n y p son, independientemente un numero entero comprendido entre 0 y 2; m + n + p >=4; R3 es NH2, NHR10; R10 es alquilo C1-6 o hidroxialquilo C1-6, alcoxialquilo C1-3, amino(C1-6)alquilo, donde el grupo amino está sustituido, opcionalmente por uno o dos grupos alquilo C1-3, siendo los citados grupos alquilo lineales o ramificados; arilo C6-14 o arilo C6-14-alquilo C1-6, con el grupo arilo sustituido opcionalmente por uno o más sustituyentes, ya sea iguales o diferentes, seleccionados por el grupo constituido por halogeno, hidroxi, alcoxi C1-6 lineal o ramificado, saturado o insaturado, amino, mono- o di-sustituidos con alquilo C1-6 lineal o ramificado; sus formas opticamente activas, tales como enantiomeros, diastereomeros y sus formas de racemato y sales farmacéuticamente aceptables de los mismos; con la condicion de que R4, R6 y R8 no sean todos H al mismo tiempo.
ARP100100883A 2009-03-20 2010-03-19 Derivados oxidados de triazolilpurinas utiles como ligandos de receptor de adenosina a2a y su uso como medicamentos. AR075894A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09155690 2009-03-20

Publications (1)

Publication Number Publication Date
AR075894A1 true AR075894A1 (es) 2011-05-04

Family

ID=40941572

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100100883A AR075894A1 (es) 2009-03-20 2010-03-19 Derivados oxidados de triazolilpurinas utiles como ligandos de receptor de adenosina a2a y su uso como medicamentos.

Country Status (14)

Country Link
US (2) US9133197B2 (es)
EP (1) EP2408775B1 (es)
JP (1) JP5648044B2 (es)
AR (1) AR075894A1 (es)
DK (1) DK2408775T3 (es)
ES (1) ES2542555T3 (es)
HR (1) HRP20150766T1 (es)
HU (1) HUE025704T2 (es)
PL (1) PL2408775T3 (es)
PT (1) PT2408775E (es)
SI (1) SI2408775T1 (es)
SM (1) SMT201500174B (es)
TW (1) TWI473809B (es)
WO (1) WO2010106145A1 (es)

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WO2018237173A1 (en) 2017-06-22 2018-12-27 Novartis Ag ANTIBODY MOLECULES DIRECTED AGAINST CD73 AND CORRESPONDING USES
CN110785187B (zh) 2017-06-22 2024-04-05 诺华股份有限公司 针对cd73的抗体分子及其用途
MX2020003732A (es) * 2017-09-28 2021-06-29 Cstone Pharmaceuticals Suzhou Co Ltd Derivado de anillo fusionado como inhibidor del receptor a2a.
CN111655288A (zh) 2017-11-16 2020-09-11 诺华股份有限公司 组合疗法
US20200371091A1 (en) 2017-11-30 2020-11-26 Novartis Ag Bcma-targeting chimeric antigen receptor, and uses thereof
NZ767596A (en) 2018-03-14 2022-01-28 Surface Oncology Inc Antibodies that bind cd39 and uses thereof
AR126019A1 (es) 2018-05-30 2023-09-06 Novartis Ag Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación
WO2019232244A2 (en) 2018-05-31 2019-12-05 Novartis Ag Antibody molecules to cd73 and uses thereof
BR112020024351A2 (pt) 2018-06-01 2021-02-23 Novartis Ag moléculas de ligação contra bcma e usos das mesmas
AR116109A1 (es) 2018-07-10 2021-03-31 Novartis Ag Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos
CA3123511A1 (en) 2018-12-20 2020-06-25 Novartis Ag Dosing regimen and pharmaceutical combination comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
WO2020165834A1 (en) 2019-02-15 2020-08-20 Novartis Ag Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
CN113490528A (zh) 2019-02-15 2021-10-08 诺华股份有限公司 3-(1-氧代-5-(哌啶-4-基)异吲哚啉-2-基)哌啶-2,6-二酮衍生物及其用途
TW202124444A (zh) 2019-09-16 2021-07-01 美商表面腫瘤學公司 抗cd39抗體組合物及方法
TW202124446A (zh) 2019-09-18 2021-07-01 瑞士商諾華公司 與entpd2抗體之組合療法
CN114502590A (zh) 2019-09-18 2022-05-13 诺华股份有限公司 Entpd2抗体、组合疗法、以及使用这些抗体和组合疗法的方法
US20210115127A1 (en) 2019-09-25 2021-04-22 Surface Oncology, Inc. Anti-il-27 antibodies and uses thereof
AU2020406350A1 (en) 2019-12-20 2022-08-11 Novartis Ag Uses of anti-TGF-beta antibodies and checkpoint inhibitors for the treatment of proliferative diseases
WO2021260528A1 (en) 2020-06-23 2021-12-30 Novartis Ag Dosing regimen comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
JP2023536164A (ja) 2020-08-03 2023-08-23 ノバルティス アーゲー ヘテロアリール置換3-(1-オキソイソインドリン-2-イル)ピペリジン-2,6-ジオン誘導体及びその使用
US20240025993A1 (en) 2020-11-06 2024-01-25 Novartis Ag Cd19 binding molecules and uses thereof
JP2024505049A (ja) 2021-01-29 2024-02-02 ノバルティス アーゲー 抗cd73及び抗entpd2抗体のための投与方式並びにその使用
TW202304979A (zh) 2021-04-07 2023-02-01 瑞士商諾華公司 抗TGFβ抗體及其他治療劑用於治療增殖性疾病之用途
AR125874A1 (es) 2021-05-18 2023-08-23 Novartis Ag Terapias de combinación

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Publication number Priority date Publication date Assignee Title
AU1688599A (en) * 1998-01-05 1999-07-26 Eisai Co. Ltd. Purine derivatives and adenosine a2 receptor antagonists serving as preventives/remedies for diabetes
JP3990061B2 (ja) * 1998-01-05 2007-10-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 プリン誘導体および糖尿病の予防・治療剤としてのアデノシンa2受容体拮抗剤
DK1221444T3 (da) * 1999-07-02 2005-11-14 Eisai Co Ltd Kondenserede imidazolforbindelser og lægemidler mod diabetes mellitus
DK1272897T3 (da) * 2000-02-10 2008-09-15 Univ New York Adenosin-A2A-receptorantagonister til behandling og forebyggelse af leverfibrose, cirrose og fedtlever
ES2247356T3 (es) * 2001-06-29 2006-03-01 Cv Therapeutics, Inc. Derivados de purina com antagonistas del receptor a2b de adenosina.
ITRM20010465A1 (it) 2001-07-31 2003-01-31 Sigma Tau Ind Farmaceuti Derivati della triazolil-imidazopiridina e delle triazolilpurine utili come ligandi del recettore a2a dell'adenosina e loro uso come medicam
WO2003020723A1 (fr) * 2001-08-30 2003-03-13 Kyowa Hakko Kogyo Co., Ltd. Derive de [1,2,4]triazolo[1,5-a]pyrimidine
GB0500785D0 (en) * 2005-01-14 2005-02-23 Novartis Ag Organic compounds
JPWO2006129626A1 (ja) * 2005-05-30 2009-01-08 協和醗酵工業株式会社 [1,2,4]トリアゾロ[1,5−c]ピリミジン誘導体の製造法

Also Published As

Publication number Publication date
DK2408775T3 (en) 2015-07-27
US9133197B2 (en) 2015-09-15
EP2408775A1 (en) 2012-01-25
US20160002244A1 (en) 2016-01-07
PL2408775T3 (pl) 2015-10-30
PT2408775E (pt) 2015-08-05
EP2408775B1 (en) 2015-06-17
US20120053191A1 (en) 2012-03-01
SMT201500174B (it) 2015-10-30
JP2012520854A (ja) 2012-09-10
TWI473809B (zh) 2015-02-21
HRP20150766T1 (hr) 2015-08-14
HUE025704T2 (en) 2016-04-28
ES2542555T3 (es) 2015-08-06
SI2408775T1 (sl) 2015-08-31
JP5648044B2 (ja) 2015-01-07
TW201100425A (en) 2011-01-01
WO2010106145A1 (en) 2010-09-23

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