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1. WO2020093006 - METHODS OF TREATING CANCER IN BIOMARKER-IDENTIFIED PATIENTS WITH NON-COVALENT INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)

Publication Number WO/2020/093006
Publication Date 07.05.2020
International Application No. PCT/US2019/059535
International Filing Date 01.11.2019
IPC
A61K 31/404 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
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
404Indoles, e.g. pindolol
A61K 31/506 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
A61K 31/66 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
C07D 209/30 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
04Indoles; Hydrogenated indoles
30with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
C07D 247/02 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
247Heterocyclic compounds containing rings having two nitrogen atoms as the only ring hetero atoms, according to more than one of groups C07D229/-C07D245/186
02having the nitrogen atoms in positions 1 and 3
C07D 403/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
CPC
A61K 31/519
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 ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519ortho- or peri-condensed with heterocyclic rings
A61K 31/565
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
565not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
A61K 31/675
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
66Phosphorus compounds
675having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Applicants
  • SYROS PHARMACEUTICALS, INC. [US]/[US]
Inventors
  • HODGSON, John Graeme
  • JOHANNESSEN, Liv Helena
Agents
  • DENHART, Derek
  • BUCHMAN, Joshua, J.
  • ARGENTIERI, Steven, R.
  • MICHAEL, Brodowski
  • SHOVON, Ashraf
Priority Data
62/754,39801.11.2018US
62/877,18922.07.2019US
62/915,98316.10.2019US
62/927,46929.10.2019US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) METHODS OF TREATING CANCER IN BIOMARKER-IDENTIFIED PATIENTS WITH NON-COVALENT INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)
(FR) MÉTHODES DE TRAITEMENT DU CANCER CHEZ DES PATIENTS IDENTIFIÉS PAR BIOMARQUEURS AVEC DES INHIBITEURS NON COVALENTS DE LA KINASE CYCLINE-DÉPENDANTE 7 (CDK7)
Abstract
(EN) The present invention relates to methods of identifying patients suffering from various types of cancer who are more likely to respond to treatment with a CDK7 inhibitor conforming to structural Formula (I), (la), a species thereof, or a specified form thereof (as described herein), either when administered or used alone or in combination with a second therapeutic agent (e.g., another anti-cancer therapy). Patients are identified based on one or more features (e.g., gene copy number or expression level) of certain biomarkers (e.g., RB1 or another member of the E2F pathway). In addition, the present invention relates to methods of treating an identified patient with a compound conforming to structural Formula (I), (la), a species thereof, or a specified form thereof, either alone or in combination with a second therapeutic agent. In another aspect, the present invention features kits including instructions for treating a patient identified as described herein.
(FR) La présente invention concerne des procédés d'identification de patients souffrant de divers types de cancer qui sont plus susceptibles de réagir au traitement avec un inhibiteur de CDK7 conforme à la formule développée (I), (la), une espèce de celle-ci, ou une forme spécifiée de celle-ci (telle que décrite ici), soit lorsqu'elle est administrée ou utilisée seule ou en combinaison avec un second agent thérapeutique (par exemple, une autre thérapie anticancéreuse). Les patients sont identifiés sur la base d'une ou de plusieurs caractéristiques (par exemple, le nombre de copies ou le niveau d'expression de gènes) de certains biomarqueurs (par exemple, RB1 ou un autre élément de la voie biologique E2F). De plus, la présente invention concerne des méthodes de traitement d'un patient identifié avec un composé conforme à la formule développée (I), (la), une espèce de celui-ci, ou une forme spécifiée de celui-ci, soit seul, soit en combinaison avec un second agent thérapeutique. Dans un autre aspect, la présente invention concerne des kits comprenant des instructions pour traiter un patient identifié comme décrit ici.
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