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1. WO2016142855 - PYRAZOLO[1,5-A][1,3,5]TRIAZINE AND PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AS CDK INHIBITORS

Publication Number WO/2016/142855
Publication Date 15.09.2016
International Application No. PCT/IB2016/051302
International Filing Date 08.03.2016
IPC
A61K 31/437 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
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
CPC
A61K 31/53
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
53having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 31/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 35/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
02specific for leukemia
Applicants
  • AURIGENE DISCOVERY TECHNOLOGIES LIMITED [IN]/[IN]
Inventors
  • SAMAJDAR, Susanta
  • PODDUTOORI, Ramulu
  • MUKHERJEE, Subhendu
  • GOSWAMI, Rajeev
Priority Data
1128/CHE/201509.03.2015IN
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PYRAZOLO[1,5-A][1,3,5]TRIAZINE AND PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AS CDK INHIBITORS
(FR) DÉRIVÉS DE PYRAZOLO[1,5-A][1,3,5]TRIAZINE ET DE PYRAZOLO[1,5-A]PYRIMIDINE UTILISÉS EN TANT QU'INHIBITEURS DE CDK
Abstract
(EN)
The present invention provides substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I), which are therapeutically useful, particularly as selective transcriptional CDK inhibitors including CDK7, CDK9, CDK12, CDK13 and CDK18, more particularly transcriptional CDK7 inhibitors wherein X, ring A, ring B, L1, L2, R1,R2, R3, R4, R6, m, n and p have the meanings given in the specification and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention of diseases or disorder associated with selective transcriptional CDKs in a mammal. The present invention also provides preparation of the compounds and pharmaceutical formulations comprising at least one of the substituted pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof.
(FR)
La présente invention concerne des dérivés substitués de pyrazolo[1,5-a][1,3,5]triazine et de pyrazolo[1,5-a]pyrimidine de formule (I), qui sont thérapeutiquement utiles, en particulier en tant qu'inhibiteurs de CDK transcriptionnelles sélectives notamment de la CDK7, la CDK9, la CDK12, la CDK13 et la CDK18, plus particulièrement en tant qu'inhibiteurs de la CDK7 transcriptionnelle, dans laquelle formule, X, le cycle A, le cycle B, L1, L2, R1, R2, R3, R4, R6, m, n et p ont la signification donnée dans la description, et des sels pharmaceutiquement acceptables de ces derniers qui sont utiles dans le traitement et la prévention de maladies ou troubles associés à des CDK transcriptionnelles sélectives chez un mammifère. La présente invention concerne également la préparation des composés et des formulations pharmaceutiques comprenant au moins l'un des dérivés substitués de pyrazolo[1,5-a][1,3,5]triazine et de pyrazolo[1,5-a]pyrimidine de formule (I) ou un sel pharmaceutiquement acceptable de ce dernier ou un stéréoisomère de ce dernier.
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