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1. WO2010138589 - BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE

Publication Number WO/2010/138589
Publication Date 02.12.2010
International Application No. PCT/US2010/036199
International Filing Date 26.05.2010
IPC
C07D 487/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 491/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 513/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
513Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/, C07D477/232
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/519 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
519ortho- or peri-condensed with heterocyclic rings
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 9/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
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
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 1/04
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
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
Applicants
  • GENENTECH, INC. [US]/[US] (AllExceptUS)
  • F. HOFFMANN-LA ROCHE AG [CH]/[CH] (AllExceptUS)
  • CASTANEDO, Georgette [US]/[US] (UsOnly)
  • CHAN, Bryan [CA]/[US] (UsOnly)
  • GOLDSTEIN, David Michael [US]/[US] (UsOnly)
  • KONDRU, Rama K. [IN]/[US] (UsOnly)
  • LUCAS, Matthew C. [GB]/[US] (UsOnly)
  • PALMER, Wylie Solang [US]/[US] (UsOnly)
  • PRICE, Stephen [GB]/[GB] (UsOnly)
  • SAFINA, Brian [US]/[US] (UsOnly)
  • SAVY, Pascal Pierre Alexandre [FR]/[GB] (UsOnly)
  • SEWARD, Eileen Mary [IE]/[GB] (UsOnly)
  • SUTHERLIN, Daniel P. [US]/[US] (UsOnly)
  • SWEENEY, Zachary Kevin [US]/[US] (UsOnly)
Inventors
  • CASTANEDO, Georgette
  • CHAN, Bryan
  • GOLDSTEIN, David Michael
  • KONDRU, Rama K.
  • LUCAS, Matthew C.
  • PALMER, Wylie Solang
  • PRICE, Stephen
  • SAFINA, Brian
  • SAVY, Pascal Pierre Alexandre
  • SEWARD, Eileen Mary
  • SUTHERLIN, Daniel P.
  • SWEENEY, Zachary Kevin
Agents
  • ANDRUS, Alex
Priority Data
61/181,45227.05.2009US
61/287,60717.12.2009US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) BICYCLIC PYRIMIDINE PI3K INHIBITOR COMPOUNDS SELECTIVE FOR P110 DELTA, AND METHODS OF USE
(FR) COMPOSÉS PYRIMIDINES BICYCLIQUES INHIBITEURS DE PI3K SÉLECTIFS POUR P110 DELTA, ET PROCÉDÉS D'UTILISATION
Abstract
(EN) Formula (I) ((Ia) and (Ib)) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
(FR) L'invention porte sur des composés de Formule (I) ((Ia) et(Ib)), où (i) X1 représente N et X2 représente S, (ii) X1 représente CR7 et X2 représente S, (iii) X1 représente N et X2 représente NR2, ou (iv) X1 représente CR7 et X2 représente O, comprenant des stéréo-isomères, des tautomères, des métabolites et des sels pharmaceutiquement acceptables de ceux-ci, lesquels composés sont utiles pour inhiber l'isoforme delta de PI3K, et pour traiter des troubles à médiation par des lipides kinases, tels qu'une inflammation, une maladie immunologique et un cancer. L'invention porte sur des procédés d'utilisation des composés de Formule (I) pour un diagnostic in vitro, in situ et in vivo, une prévention ou un traitement de tels troubles dans des cellules de mammifère, ou des états pathologiques associés.
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