c-Met Modulators and Method of Use
Granted: September 26, 2013
Application Number:
20130252940
The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above,…
PFKs as Modifiers of the IGFR Pathway and Methods of Use
Granted: August 15, 2013
Application Number:
20130212716
Human PFK genes are identified as modulators of the IGFR pathway, and thus are therapeutic targets for disorders associated with defective IGFR function. Methods for identifying modulators of IGFR, comprising screening for agents that modulate the activity of PFK are provided.
Methods of Treating Cancer Using Pyridopyrimidinone Inhibitors of PI3K and mTOR in Combination with Autophagy Inhibitors
Granted: July 4, 2013
Application Number:
20130172371
The invention provides compounds of Formula I: that inhibit the PI3Ks and mTOR that are useful in the treatment of cancer in humans when used in combination with autophagy inhibitors.
JAK1 Inhibitors
Granted: June 27, 2013
Application Number:
20130165440
JAK1 inhibitors of structural formula (I), wherein Ar1, Ar2, Q, W, X, Y, and Z are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.
Hydrated Crystalline Forms of N-[3-fluoro-4-(oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Granted: June 6, 2013
Application Number:
20130143881
This invention relates crystalline hydrates of N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, Compound (I). The invention provides methods for treatment of cancer by exploiting the modulation of protein kinase activity. The invention also provides pharmaceutical compositions containing a crystalline hydrate of Compound (I) and a pharmaceutically acceptable excipient.
Methods of Preparing Quinoline Derivatives
Granted: January 31, 2013
Application Number:
20130030172
Methods of preparing compounds of formula i(1): or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 join together with the nitrogen atom to which they are attached to form a 6 membered heterocycloalkyl group; X1 is H, Br, Cl or F; X2 is H, Br, Cl or F; s is 2-6; n1 is 0-2; and n2 is 0-2.
Method of Using PI3K and MEK Modulators
Granted: November 29, 2012
Application Number:
20120302545
The invention provides methods of treating cancer with a combination of compounds which inhibit kinases, more specifically MEK and PI3K.
Methods of Using C-Met Modulators
Granted: November 8, 2012
Application Number:
20120282179
Methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments are described, wherein R1 is halo; R2 is halo; and Q is CH or N.
Crystalline Forms of N-[3-fluoro-4-(oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Granted: October 25, 2012
Application Number:
20120270872
This invention relates to three crystalline forms of N—[3-fluoro-4-((6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl|oxy)phenyl]—N?—(4-fluorophenyl)cyclopropane-1,1-dicarboxamide. Compound (I), designated as Form A, Form B, and Form C. The invention provides methods for treatment of cancer by exploiting the modulation of protein kinase activity. The invention also provides pharmaceutical compositions containing a crystalline form of Compound (I) and a pharmaceutically…
Benzoxazepines as Inhibitors of PI3K/mTOR and Methods of Their Use and Manufacture
Granted: October 11, 2012
Application Number:
20120258953
The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides methods of making the compound methods of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds. For example, cancer…
Method of Treating Cancer
Granted: October 4, 2012
Application Number:
20120252840
This invention is directed to the treatment of cancer, particularly ocular melanoma, with a dual inhibitor of MET and VEGF such as Compound 1.
INHIBITORS OF THE HEDGEHOG PATHWAY
Granted: September 27, 2012
Application Number:
20120245139
The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
INHIBITORS OF THE HEDGEHOG PATHWAY
Granted: September 20, 2012
Application Number:
20120238570
The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
C-Met Modulators and Method of Use
Granted: July 19, 2012
Application Number:
20120184523
The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above,…
PSMCs As Modifiers of the RB Pathway and Methods of Use
Granted: May 3, 2012
Application Number:
20120107827
Human PSMC genes are identified as modulators of the RB pathway, and thus are therapeutic targets for disorders associated with defective RB function. Methods for identifying modulators of RB, comprising screening for agents that modulate the activity of PSMC are provided.
Methods of Using C-Met Modulators
Granted: March 22, 2012
Application Number:
20120070368
Disclosed are methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt thereof, in combination with gemcitabine (GEM), or a pharmaceutically acceptable salt thereof, and optionally one or more additional treatments, wherein: R1 is halo; R2 is halo; R3 is (C1-C6)alkyl; R4 is (C1-C6)alkyl; and Q is CH or N.
Quinazolinone Modulators Of Nuclear Receptors
Granted: March 15, 2012
Application Number:
20120064025
Compounds, pharmaceutical compositions and methods for modulating the activity of nuclear receptors are provided. In particular, quinazolinones are provided for modulating the activity of farnesoid X receptor (FXR) and/or orphan nuclear receptors.
TRIAZOLE AND IMIDAZOLE DERIVATIVES FOR USE AS TGR5 AGONISTS IN THE TREATMENT OF DIABETES AND OBESITY
Granted: February 16, 2012
Application Number:
20120040985
The present invention comprises TGR5 agonists of structural formula I, wherein X, R1, R2, and R5 are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises…
(L)-Malate salt of N-(4-phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Granted: February 9, 2012
Application Number:
20120035212
Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N?-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of…
C-Met Modulators and Method of Use
Granted: January 26, 2012
Application Number:
20120022065
The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above,…
