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1. WO2020112700 - 9-SUBSTITUTED AMINO TRIAZOLO QUINAZOLINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE

Publication Number WO/2020/112700
Publication Date 04.06.2020
International Application No. PCT/US2019/063136
International Filing Date 26.11.2019
IPC
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 487/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/519 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
CPC
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • MERCK SHARP & DOHME CORP. [US]/[US]
  • LARSEN, Matthew, A. [US]/[US] (US)
  • ALI, Amjad [US]/[US] (US)
  • CUMMING, Jared [US]/[US] (US)
  • DEMONG, Duane [US]/[US] (US)
  • DENG, Qiaolin [US]/[US] (US)
  • GRAHAM, Thomas, H. [US]/[US] (US)
  • HENNESSY, Elisabeth [US]/[US] (US)
  • HOOVER, Andrew, J. [US]/[US] (US)
  • LIU, Ping [US]/[US] (US)
  • LIU, Kun [US]/[US] (US)
  • MANSOOR, Umar Faruk [GB]/[US] (US)
  • PAN, Jianping [US]/[US] (US)
  • PLUMMER, Christopher, W. [US]/[US] (US)
  • SATHER, Aaron [US]/[US] (US)
  • SWAMINATHAN, Uma [IN]/[US] (US)
  • WANG, Huijun [US]/[US] (US)
  • ZHANG, Yonglian [CN]/[US] (US)
Inventors
  • LARSEN, Matthew, A.
  • ALI, Amjad
  • CUMMING, Jared
  • DEMONG, Duane
  • DENG, Qiaolin
  • GRAHAM, Thomas, H.
  • HENNESSY, Elisabeth
  • HOOVER, Andrew, J.
  • LIU, Ping
  • LIU, Kun
  • MANSOOR, Umar Faruk
  • PAN, Jianping
  • PLUMMER, Christopher, W.
  • SATHER, Aaron
  • SWAMINATHAN, Uma
  • WANG, Huijun
  • ZHANG, Yonglian
Common Representative
  • MERCK SHARP & DOHME CORP.
Priority Data
62/774,07730.11.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 9-SUBSTITUTED AMINO TRIAZOLO QUINAZOLINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE
(FR) DÉRIVÉS AMINO TRIAZOLO QUINAZOLINE 9-SUBSTITUÉS UTILES EN TANT QU'ANTAGONISTES DU RÉCEPTEUR DE L'ADÉNOSINE, COMPOSITIONS PHARMACEUTIQUES ET LEUR UTILISATION
Abstract
(EN)
In its many embodiments, the present invention provides certain 9-substituted amino triazolo quinazoline compounds of the structural Formula (I): (I), and pharmaceutically acceptable salts thereof, wherein, ring A, R1 and R2 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
(FR)
Dans ses nombreux modes de réalisation, la présente invention concerne certains composés amino triazolo quinazoline 9-substitués de formule structurale (I): (I), et des sels pharmaceutiquement acceptables de ceux-ci, dans laquelle, le cycle A, R1 et R2 sont tels que définis dans la description, des compositions pharmaceutiques comprenant un ou plusieurs de ces composés (seul(s) et en combinaison avec un ou plusieurs autres agents thérapeutiquement actifs), et des procédés pour leur préparation et leur utilisation, seuls ou en combinaison avec d'autres agents thérapeutiques, en tant qu'antagonistes des récepteurs A2a et/ou A2b, et dans le traitement d'une variété de maladies, d'états ou de troubles qui sont médiés, au moins en partie, par le récepteur A2a de l'adénosine et/ou le récepteur d'adénosine A2b.
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