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1. WO2020139943 - EZH2 AND ANDROGEN RECEPTOR SIGNALING INHIBITORS AS TOOLS FOR TARGETING PROSTATE CANCER

Publication Number WO/2020/139943
Publication Date 02.07.2020
International Application No. PCT/US2019/068575
International Filing Date 26.12.2019
IPC
A61K 31/4166 2006.1
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
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41641,3-Diazoles
4166having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
A61K 31/4545 2006.1
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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
4545containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/58 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
58containing heterocyclic rings, e.g. aldosterone, danazol, stanozolol, pancuronium, digitogenin
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61K 31/573 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
57substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane, progesterone
573substituted in position 21, e.g. cortisone, dexamethasone, prednisone
CPC
A61K 31/4166
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
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41641,3-Diazoles
4166having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
A61K 31/4545
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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
445Non condensed piperidines, e.g. piperocaine
4523containing further heterocyclic ring systems
4545containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/573
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids
57substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane, progesterone
573substituted in position 21, e.g. cortisone, dexamethasone, prednisone ; or aldosterone
A61K 31/58
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids
58containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • CONSTELLATION PHARMACEUTICALS, INC. [US]/[US]
Inventors
  • MCGRATH, John
  • SENDEROWICZ, Adrian
  • TROJER, Patrick
  • BRADLEY, William, D.
Agents
  • DAVIS, Steven, G.
  • BENNETT, Coalton
  • BOWLES, Anita, M.
  • BLAZESKI, George
  • BAI, Mei
Priority Data
PCT/US2018/06764627.12.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) EZH2 AND ANDROGEN RECEPTOR SIGNALING INHIBITORS AS TOOLS FOR TARGETING PROSTATE CANCER
(FR) INHIBITEURS DE LA SIGNALISATION DE L'EZH2 ET D'UN RÉCEPTEUR D'ANDROGÈNES EN TANT QU'OUTILS POUR LE CIBLAGE DU CANCER DE LA PROSTATE
Abstract
(EN)
Provided herein are methods of using (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide, or a pharmaceutically acceptable salt thereof and an androgen receptor signaling inhibitor for treating prostate cancer. Also provided are pharmaceutical compositions comprising (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2- methyl- 1-( 1-( 1-(2, 2, 2-trifluoroethyl)piperidin-4-yl)ethyl)-1H- indole-3-carboxamide, or a pharmaceutically acceptable salt thereof and an androgen receptor signaling inhibitor.
(FR)
L'invention concerne des méthodes d'utilisation du (R)-N-((4-méthoxy-6-méthyl-2-oxo-1,2-dihydropyridin-3-yl)méthyl)-2-méthyl-1-(1-(1-(2,2,2-trifluoroéthyl)pipéridin-4-yl)éthyl)-1H-indole-3-carboxamide, ou un sel pharmaceutiquement acceptable de celui-ci et d'un inhibiteur de signalisation d'un récepteur d'androgènes pour le traitement du cancer de la prostate. L'invention concerne également des compositions pharmaceutiques comprenant du (R)-N-((4-méthoxy-6-méthyl-2-oxo-1,2-dihydropyridin-3-yl)méthyl)-2- méthyl- 1-( 1-( 1-(2, 2, 2-trifluoroéthyl)pipéridin-4-yl)éthyl)-1H- indole-3-carboxamide, ou un sel pharmaceutiquement acceptable de celui-ci et un inhibiteur de signalisation d'un récepteur d'androgènes.
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