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Class 514/233.2 - Ring nitrogen shared by two of the cyclos


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which two of the cyclos in the polycyclo
No. of applications: 530
Last issue date: 05/23/2013


1                      
Application No.Application TitleIssue Date
20130131057NEW BICYCLIC COMPOUNDS AS PI3-K AND MTOR INHIBITORS
There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings gi... 		05/23/2013
201301310395,7-SUBSTITUTED-IMIDAZO[1,2-C]PYRIMIDINES AS INHIBITORS OF JAK KINASES
Compounds of Formula I: (Formula should be inserted here) and stereoisomers and pharmaceutically acceptable salts and solvates thereof in which R1, R2, R3, R4, R5, R6, R7, X1 and X		05/23/2013
20130123254PHARMACEUTICALLY ACCEPTABLE MGLUR5 POSITIVE ALLOSTERIC MODULATORS AND THEIR METHODS OF IDENTIFICATION
The present invention relates to mGluR5 positive allosteric modulators (PAM) and methods for identifying pharmaceutically acceptable compounds with high tolerability and safety, which method comprises the use of at least one non-competitive mGluR5 allosteric modulator w... 		05/16/2013
20130116235HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS
Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, ... 		05/09/2013
20130116233NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurologi... 		05/09/2013
20130116250IMIDAZOPYRIDINE DERIVATIVES, PROCESS FOR PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
The invention relates to compounds corresponding to formula (I):

    • in which
    		05/09/2013
    20130116249INDOLIZINE DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
    The invention relates to compounds corresponding to formula (I):

      • in which
      		05/09/2013
      20130109661IMIDAZOPYRIDAZINE COMPOUNDS
      The present invention relates to the use of novel compounds of formula I:

      wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-i...

      		05/02/2013
      20130096113HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF
      Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFRβ kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions....       		04/18/2013
      20130096114PHARMACOKINETICALLY IMPROVED COMPOUNDS
      A compound of formula A having improved non-specific binding characteristics and pharmacokinetic properties is provided:

      or a pharmaceutically acceptable salt, stereoisomer, or hydrate thereof....

      		04/18/2013
      20130089512HETEROARYL IMIDAZOLONE DERIVATIVES AS JAK INHIBITORS
      New heteroaryl imidazolone derivatives having the chemical structure of formula (I) are disclosed, as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK)....       		04/11/2013
      20130085142SUBSTITUTED OCTAHYDROPYRROLO[1,2-a]PYRAZINES AS CALCIUM CHANNEL BLOCKERS
      The present application relates to: (a) compounds of Formula (I):

      and salts thereof, wherein Z1, Z2, Z3, Z4, R1, R2, and R3 are as ...

      		04/04/2013
      20130085141SUBSTITUTED OCTAHYDROPYRROLO[1,2-a]PYRAZINE SULFONAMIDES AS CALCIUM CHANNEL BLOCKERS
      The present application relates to: (a) compounds of Formula (I):

      and salts thereof, wherein Z′, Z″, L2, G2, R1, and R2 are as defined in the specification; (b)...

      		04/04/2013
      20130085143AMINOACID DERIVATIVES, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES AS INHIBITORS OF ONCOGENIC SIGNALS BY THE MET FAMILY
      Novel amino acids derivatives, in particular some amino acid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer....       		04/04/2013
      20130085134QUINOXALINE COMPOUND
      Quinoxaline compounds of formula (I) have a PDE9-inhibiting action and are useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like....       		04/04/2013
      20130072470NOVEL TRICYCLIC COMPOUNDS
      The invention provides compounds of Formula (I)

      pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The co...

      		03/21/2013
      201300713525,5-FUSED ARYLENE OR HETEROARYLENE HEPATITIS C VIRUS INHIBITORS
      Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment ...       		03/21/2013
      20130065893IMIDAZOLE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS
      The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, R5, R7 and p are defined herein. The invention also relates to a...       		03/14/2013
      20130059845BICYCLIC AGONISTS OF GPR131 AND USES THEREOF
      The present disclosure relates to compounds that act as agonists of, or otherwise modulate the activity of, GPR131 and to their use in the treatment of various diseases. In particular embodiments, the structure of the compounds is given by Formula I:

      		03/07/2013
      20130059846COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS
      The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In s...       		03/07/2013
      20130059832COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS
      The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In s...       		03/07/2013
      201300598442-PHENYL SUBSTITUTED IMIDAZOTRIAZINONES AS PHOSPHODIESTERASE INHIBITORS
      The 2-phenyl-substituted imidazotriazinones having short, unbranched alkyl radicals in the 9-position are prepared from the corresponding 2-phenyl-imidazotriazinones by chlorosulphonation and subsequent reaction with the amines. The compounds inhibit cGMP-metabolizing p...       		03/07/2013
      201300533794-ARYL-2-ANILINO-PYRIMIDINES
      The present invention relates to compounds of Formula (Ia) or (Ib), the N-oxide forms, pharmaceutically acceptable addition salts, quaternary amines, stereoisomers, tautomers, racemics, metabolites, prodrugs, hydrates, or solvates thereof,

      ...

      		02/28/2013
      20130053363IMIDAZO[1,2-a]PYRIDINE DERIVATIVE
      [Problem]

      To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.

      		02/28/2013
      20130053371INHIBITORS OF PI3 KINASE
      There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings gi...       		02/28/2013
      20130040931Amino Heteroaryl Compounds as Beta-Secretase Modulators and Methods of Use
      The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds ha...       		02/14/2013
      20130040946SUBSTITUTED IMIDAZOPYRIMIDINES AND TRIAZOLOPYRIMIDINES
      The invention relates to substituted imidazo- and triazolopyrimidines and processes for their preparation, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, in particular of haematological disorders, preferably of leucope...       		02/14/2013
      20130035324HETEROCYCLIC COMPOUNDS AND USES THEREOF
      Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein....       		02/07/2013
      20130029967Fused Imidazo [3,2 - D] Pyrazines as P13 Kinase Inhibitors
      There is provided compounds of formula (I), wherein A1, A2, A3, A4, n, the dotted lines, B1, B1a, B2, B2a, B3, B3a, B4, B4a, R2       		01/31/2013
      20130029982HETEROCYCLIC COMPOUNDS AND USES THEREOF
      Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are de...       		01/31/2013
      201300299746,7-DIHYDROIMIDAZO[1,5-A]PYRAZIN-8(5H)-ONE DERIVATIVES AS PROTEIN KINASE MODULATORS
      There are provided 3,5-disubstituted derivatives of 6,7-dihydroimidazo[1,5-a]pyrazin-8(5H)-one compounds of formula (I) or a pharmaceutically acceptable salt thereof as defined in the present specification, which modulate the activity of protein kinases. The compounds a...       		01/31/2013
      20130029981COMPOUNDS, COMPOSITIONS, AND METHODS FOR CONTROLLING BIOFILMS
      The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2-a]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2-a]pyrimidinium salts bearing an azidoalkyl substituent, and to su...       		01/31/2013
      20130023530NOVEL NK-3 RECEPTOR SELECTIVE ANTAGONIST COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS FOR USE IN NK-3 RECEPTORS MEDIATED DISORDERS
      The present invention is directed to novel compounds of formula I

      and their use as therapeutic compounds....

      		01/24/2013
      20130023499CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF
      Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehi...       		01/24/2013
      20130023514SUBSTITUTED PYRROLOTRIAZINES AS PROTEIN KINASE INHIBITORS
      The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) pyrrolotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.

      ...

      		01/24/2013
      20130018041PYRIMIDINE-2-AMINE COMPOUNDS AND THEIR USE AS INHIBITORS OF JAK KINASES
      This invention is directed to compounds of formula (I):

      where

      n, m, Y, R1, R2, R3, R4 and R5

      		01/17/2013
      20130012506ANTI-INFECTIVE PYRIDO (1,2-A) PYRIMIDINES
      The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis....       		01/10/2013
      20130005707AMINOTRIAZOLOPYRIDINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
      Provided herein are Heteroaryl Compounds of formula (I):

        • wherein R1 and R
      		01/03/2013
      20130005721INDOLIZINE INHIBITORS OF 5-LIPOXYGENASE
      Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating re...       		01/03/2013
      20130004458Small Molecule Inhibitors of Retroviral Assembly and Maturation
      Chemical compounds that disrupt retroviral assembly and maturation are presented herein. More particularly, this disclosure provides small molecule compounds that disrupt the formation and maturation of virus particles and methods of using such small molecules to treat ...       		01/03/2013
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