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1. WO2020005807 - TAIRE FAMILY KINASE INHIBITORS AND USES THEREOF

Publication Number WO/2020/005807
Publication Date 02.01.2020
International Application No. PCT/US2019/038677
International Filing Date 24.06.2019
IPC
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
415
1,2-Diazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02
not condensed with other rings
10
having two or three double bonds between ring members or between ring members and non-ring members
14
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38
Nitrogen atoms
A61K 31/415 (2006.01)
C07D 231/38 (2006.01)
CPC
A61K 31/415
A61K 31/4155
A61K 31/454
A61K 45/06
C07D 231/40
C07D 401/12
Applicants
  • DANA-FARBER CANCER INSTITUTE, INC. [US/US]; 450 Brookline Avenue Boston, MA 02215, US
Inventors
  • GRAY, Nathanael, S.; US
  • FERGUSON, Fleur, M.; US
  • DOCTOR, Zainab, M.; US
Agents
  • BAKER, Hunter, C.; US
  • ATTISHA, Michael, J.; US
  • AMUNDSEN, Eric, L.; US
  • ACHLLES, Daryl, L.; US
  • ALAM, Saad; US
Priority Data
62/689,55125.06.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) TAIRE FAMILY KINASE INHIBITORS AND USES THEREOF
(FR) INHIBITEURS DE KINASE DE LA FAMILLE TAIRE ET UTILISATIONS CORRESPONDANTES
Abstract
(EN)
Provided herein are compounds of Formula (I´) or (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers (e.g., carcinoma); lung cancer, breast cancer, liver cancer, pancreatic cancer, gastric cancer, ovarian cancer, colon cancer, colorectal cancer)), metabolic disorders (e.g., diabetes), autoimmune diseases, and neurological diseases (e.g., Alzheimer's disease, gliosis, spinal cord injury)) in a subject, as well as for male contraception (e.g., reducing or inhibiting spermatogenesis, or reducing the rate of male fertility in a healthy fertile male subject). Provided are methods of inhibiting a CDK (e.g., CDK14, CDK15, CDK16, CDK17, CDK18) in a subject.
(FR)
La présente invention concerne des composés de formule (I') ou (I) et des sels, des solvates, des hydrates, des polymorphes, des cocristaux, des tautomères, des stéréo-isomères, des dérivés marqués de façon isotopique, des promédicaments, et des compositions, pharmaceutiquement acceptables correspondant(e)s. L'invention concerne également des procédés et des kits impliquant les composés ou les compositions de l'invention pour le traitement et/ou la prévention de maladies (par exemple des maladies prolifératives (par exemple des cancers (par exemple un carcinome) ; le cancer du poumon, le cancer du sein, le cancer du foie, le cancer du pancréas, le cancer de l'estomac, le cancer de l'ovaire, le cancer du côlon, le cancer colorectal)), des troubles métaboliques (par exemple le diabète), des maladies auto-immunes et des maladies neurologiques (par exemple la maladie d'Alzheimer, la gliose, une lésion de la moelle épinière) chez un sujet, ainsi que pour la contraception masculine (par exemple la réduction ou l'inhibition de la spermatogenèse ou la réduction du taux de fertilité mâle chez un sujet mâle fertile sain). L'invention concerne des procédés d'inhibition d'un CDK (par exemple CDK14, CDK15, CDK16, CDK17, CDK18) chez un sujet.
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