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Attorney: Korsen; Elliott


Number of patents: 134
Last date: April 03, 2012

1        
NumberTitleIssue Date
8148523Intermediates useful in preparing certain pyrrolotriazine compounds and a process for making the intermediates
The invention relates to 4-chloro-2-iodopyrrolo[1,2-f][1,2,4]triazine, which is an intermediate useful in preparing 2,4-disubstituted pyrrolotriazine compounds, and a process for preparing said intermediate. ...
04/03/2012
8148522Intermediate useful in preparing certain pyrrolotriazine compounds and a process for making the intermediate
The invention relates to 2,4-dibromoropyrrolo[1,2-f][1,2,4]triazine, which is an intermediate useful in preparing 2,4-disubstituted pyrrolotriazine compounds, and a process for preparing the intermediate. ...
04/03/2012
8148400Thiazolyl compounds useful as kinase inhibitors
The invention provides compounds of formula II: and pharmaceutically acceptable salts thereof. The formula II thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the ...
04/03/2012
7985861Piperidinyl derivatives as modulators of chemokine receptor activity
The present application describes substituted piperidinyl modulators of MIP-1α or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as wel...
07/26/2011
7982033Pyrrolotriazine kinase inhibitors
The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB, TrkC or Flt-3 thereby making...
07/19/2011
7932383Crystalline forms of [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester
Crystalline form, Form N-1, of [(1R),2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester (Compound I) is provided. Also provided are a pharmaceutical composition and an oral dosage for...
04/26/2011
7846931Pyrrolotriazine compounds as kinase inhibitors
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 th...
12/07/2010
7879855Pyrrolotriazine kinase inhibitors
The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treat...
02/01/2011
7855192Macrolactams by engineered biosynthesis
Macrolactams are made by feeding aromatic amino acids as replacement starter units to a mutant strain of the geldanamycin-producing microorganism Streptomyces hygroscopicus var. geldanus NRRL 3602, wherein the gene cluster encoding enzymes for the bios...
12/21/2010
7851500Aminopyrazole kinase inhibitors
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents. ...
12/14/2010
7820814Inhibitors of kinases
The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-...
10/26/2010
7691838Method for treating diseases using HSP90-inhibiting agents in combination with antimitotics
The present invention provides a method for treating cancer. The method involves the administration of an HSP90 inhibitor and an antimitotic, where the combined administration provides a synergistic effect. In one aspect of the invention, a method of treating cancer...
04/06/2010
7691392Method of treating multiple myeloma using 17-AAG or 17-AG or a prodrug of either
A method for treating multiple myeloma in a subject by administering 17-allylamino-17-demethoxy-geldanamycin or 17-amino geldanamycin, or a prodrug of either 17-AAG or 17-AG, to the subject. ...
04/06/2010
7671199Process for the preparation of [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2, 1-F][1,2,4]triazin-6-yloxy]-1-methylethyl ester
The invention relates to an improved process for preparing [(1R), 2S]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester of the formula: Compound ...
03/02/2010
7619083Intermediates useful in preparing certain pyrrolotriazine compounds and process for making such intermediates
The invention relates to 2,4-dichloropyrrolo[1,2-f][1,2,4]triazines, which are intermediates useful in preparing at least one 2,4-disubstituted pyrrolotriazine compound, and at least one method for making such intermediates. ...
11/17/2009
7615556Piperazinyl derivatives as modulators of chemokine receptor activity
The present application describes modulators of MIP-1α of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, T, W, R1, R4, R5, R5a and R5...
11/10/2009
7605160Pyrrolotriazine kinase inhibitors
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB and TrkC thereby maki...
10/20/2009
7601852Macrocyclic kinase inhibitors
A compound having a structure according to formula I wherein R1, R2, R3, R4, and R5 are as defined herein, are useful as kinase inhibitors. ...
10/13/2009
7601844Piperidinyl derivatives as modulators of chemokine receptor activity
The present application describes substituted piperidinyl modulators of MIP-1α or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as wel...
10/13/2009
75953007-quinolyl ketolide antibacterial agents
15-fluoroketolides of the formula having improved activity and safety, compositions comprising them, and methods for their preparation and use in the treatment of bacterial infections. ...
09/29/2009
7557143Thyroid receptor ligands
Thyroid receptor ligands are provided which have the general formula I wherein: R1 is R2...
07/07/2009
7547711Heterocyclic inhibitors of kinases
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, t...
06/16/2009
7534792Pyrrolotriazine kinase inhibitors
The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treat...
05/19/2009
7531539Pyrrolotriazine kinase inhibitors
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of such as TrkA, TrkB, TrkC, Jak2, Jak3 and CK2, thereby ...
05/12/2009
7521450Inhibitors of kinases
The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-...
04/21/2009
7514435Pyrrolotriazine kinase inhibitors
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of Trk receptors such as TrkA, TrkB, TrkC or Flt-3 thereb...
04/07/2009
7470696Tyrosine kinase inhibitors
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents. ...
12/30/2008
7446196Leptomycin compounds
Leptomycin-type compounds according to Formula I wherein R0, R1, R2, R10, R11, R12, R13, R14, and m are as defined herein, exhibit anti...
11/04/2008
7432373Processes and intermediates useful for preparing fused heterocyclic kinase inhibitors
The present invention is directed to intermediates that are useful for preparing pyrrolotriazines, and processes for preparing such intermediates. ...
10/07/2008
7393667Stereoselective reduction process for the preparation of pyrrolotriazine compounds
The invention relates to a process for the enzymatic, stereoselective reduction of ketone compounds to provide chiral alcohols, for example the compound of formula Ib: ...
07/01/2008
7388098Dynamic resolution of isomers and resolved isomers
Provided is a dynamic resolution method of enriching a desired isomer of an alpha-substituted carboxylic acid relative to an undesired isomer, the method comprising: (a) in a solvent, contacting the alpha-substituted carboxylic acid, wherein the alpha substitution i...
06/17/2008
7358256ATP competitive kinase inhibitors
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 th...
04/15/2008
7323587Selective estrogen receptor modulators
The present invention provides, inter alia, triphenylethylene derivatives, such as, 3-{4-[6-(3-Methoxy-phenyl)-8,9-dihydro-7H-benzocyclohepten-5-yl]-phenyl}-acrylic acid, as selective estrogen receptor modulators. Also provided are methods for treating estrogen stim...
01/29/2008
7297695Pyrrolotriazine compounds as kinase inhibitors
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 th...
11/20/2007
7265113Inhibitors of kinases
The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-...
09/04/2007
7250435Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents
The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to t...
07/31/2007
7244733Pyrrolotriazine inhibitors of kinases
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2...
07/17/2007
7232901Intermediates useful in preparing certain pyrrolotriazine compounds and process for making such intermediates
Described herein is at least one pyrrolo[1,2-f][1,2,4]triazine-2,4(1H,3H)-dione, which is an intermediates useful in preparing 2,4-disubstituted pyrrolotriazine compounds, and at least one method for making such intermediate. ...
06/19/2007
7223757Tyrosine kinase inhibitors
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agent...
05/29/2007
7176326β-Lactams, methods for the preparation of taxanes, and sidechain-bearing taxanes
Novel β-lactams finding utility as intermediates in the preparation of sidechain-bearing taxanes such as taxol and taxol derivatives. The present invention also relates to novel methods of coupling β-lactams to form such sidechain-bearing taxanes, and to novel sid...
02/13/2007
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