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| Number | Title | Issue Date |
| 8148523 | Intermediates 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 |
| 8148522 | Intermediate 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 |
| 8148400 | Thiazolyl 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 |
| 7985861 | Piperidinyl 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 |
| 7982033 | Pyrrolotriazine 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 |
| 7932383 | Crystalline 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 |
| 7846931 | Pyrrolotriazine 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 |
| 7879855 | Pyrrolotriazine 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 |
| 7855192 | Macrolactams 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 |
| 7851500 | Aminopyrazole 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 |
| 7820814 | 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 and FGFR-... | 10/26/2010 |
| 7691838 | Method 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 |
| 7691392 | Method 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 |
| 7671199 | Process 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 |
| 7619083 | Intermediates 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 |
| 7615556 | Piperazinyl 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 |
| 7605160 | Pyrrolotriazine 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 |
| 7601852 | Macrocyclic 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 |
| 7601844 | Piperidinyl 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 |
| 7595300 | 7-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 |
| 7557143 | Thyroid receptor ligands Thyroid receptor ligands are provided which have the general formula I wherein: R1 is R2... | 07/07/2009 |
| 7547711 | Heterocyclic 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 |
| 7534792 | Pyrrolotriazine 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 |
| 7531539 | Pyrrolotriazine 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 |
| 7521450 | 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 and FGFR-... | 04/21/2009 |
| 7514435 | Pyrrolotriazine 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 |
| 7470696 | Tyrosine 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 |
| 7446196 | Leptomycin 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 |
| 7432373 | Processes 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 |
| 7393667 | Stereoselective 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 |
| 7388098 | Dynamic 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 |
| 7358256 | ATP 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 |
| 7323587 | Selective 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 |
| 7297695 | Pyrrolotriazine 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 |
| 7265113 | 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-... | 09/04/2007 |
| 7250435 | Acylsemicarbazides 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 |
| 7244733 | Pyrrolotriazine 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 |
| 7232901 | Intermediates 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 |
| 7223757 | Tyrosine 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 |
| 7176326 | β-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 |