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1. WO2012058671 - SUBSTITUTED QUINAZOLINE AND PYRIDO-PYRIMIDINE DERIVATIVES

Publication Number WO/2012/058671
Publication Date 03.05.2012
International Application No. PCT/US2011/058584
International Filing Date 31.10.2011
IPC
C07D 413/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14containing three or more hetero rings
A61K 31/506 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
506not condensed and containing further heterocyclic rings
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 31/535
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
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
A61P 1/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
A61P 11/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
A61P 19/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
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 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • ENDO PHARMACEUTICALS INC. [US]/[US] (AllExceptUS)
  • SMITH, Roger, Astbury [US]/[US] (UsOnly)
  • THOMPSON, Scott, Kevin [US]/[US] (UsOnly)
  • HOSAHALLI, Subramanya [IN]/[IN] (UsOnly)
  • BEJUGAM, Mallesham [IN]/[IN] (UsOnly)
  • NANDURI, Srinivas [IN]/[IN] (UsOnly)
  • PANIGRAHI, Sunil, Kumar [IN]/[IN] (UsOnly)
  • MAHALINGAM, Natarajan [IN]/[IN] (UsOnly)
Inventors
  • SMITH, Roger, Astbury
  • THOMPSON, Scott, Kevin
  • HOSAHALLI, Subramanya
  • BEJUGAM, Mallesham
  • NANDURI, Srinivas
  • PANIGRAHI, Sunil, Kumar
  • MAHALINGAM, Natarajan
Agents
  • PALOVICH, Tracy, U.
Priority Data
61/408,62031.10.2010US
61/501,90128.06.2011US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) SUBSTITUTED QUINAZOLINE AND PYRIDO-PYRIMIDINE DERIVATIVES
(FR) DÉRIVÉS DE QUINAZOLINE ET DE PYRIDO-PYRIMIDINE SUBSTITUÉES
Abstract
(EN)
The present application provides novel substituted quinazoline and pyrido- pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
(FR)
La présente invention concerne des composés de quinazoline et de pyrido-pyrimidine substituées et leurs sels pharmaceutiquement acceptables. L'invention a également pour objet des procédés de préparation desdits composés. Ces composés sont utiles dans la corégulation de l'activité de PI3K et/ou mTOR par l'administration d'une quantité thérapeutiquement efficace d'un ou plusieurs des composés à un patient. Ainsi, ces composés sont efficaces dans le traitement d'affections associées au dérèglement de la voie PI3K/AKT/mTOR. De manière avantageuse, ces composés se comportent comme des inhibiteurs doubles de PI3K/mTOR. Il est ainsi possible de traiter toute une diversité d'affections à l'aide de ces composés, lesdites affections comprenant des maladies qui sont caractérisées par une inflammation ou une prolifération cellulaire anormale. Dans un mode de réalisation, la maladie est un cancer.
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