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8183248 Substituted pyrrolo[2,3-d]pyrimidines and compositions as protein kinase inhibitors  
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated...
8183238 Bicyclic and tricyclic compounds as KAT II inhibitors  
Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits...
8178543 Bi- and tricyclic fused pyrimidines as tyrosine kinase inhibitors  
The present invention relates to a compound represented by the formula: wherein W is C(R1) or N, each A is an optionally substituted aryl group or a heteroaryl group, X1 is —NR3—Y1—, —O—, —S—, —SO—...
8173707 Ophthalmologic irrigation solutions and method  
Solutions for perioperative intraocular application by continuous irrigation during ophthalmologic procedures are provided. These solutions include multiple agents that act to inhibit inflammation,...
8173662 Fused pyrimidines as inhibitors of nucleoside phosphorylases and nucleosidases  
The present invention relates to compounds of the general formula (I) which are inhibitors of purine muclioside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT),...
8163750 Fluorene derivatives, compositions containing the same and use thereof as inhibitors of the protein chaperone HSP 90  
The present invention relates to compounds of formula (I): wherein R1, R2, R2′, L, Het, p and p′ are as defined herein, compositions containing them, and their use as medicinal products.
8158636 Compounds and methods for kinase modulation, and indications therefor  
Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds...
8153641 Compounds and methods for kinase modulation, and indications therefor  
Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds...
8138167 Methods for treating lung cancers  
The present invention provided methods for treating lung cancers using therapeutic agents for lung cancers comprising erbB receptor inhibitors as active ingredients. Methods for examining the...
8133899 Pyrrolo[2,3-d]pyrimidine compounds  
Described herein is pyrrolo{2,3-d}pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing this compounds, and methods for the preparation of these...
8129372 Compounds having NPY Y5 receptor antagonistic activity  
This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or...
8119649 Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia  
The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b)...
8105608 Method of treatment using ligand-immunogen conjugates  
A method and pharmaceutical composition are provided for enhancing the endogenous immune response-mediated elimination of a population of pathogenic cells in a host animal wherein the pathogenic...
8101623 Substituted pyrrolo[2,3-d]pyrimidine as a protein kinase B inhibitor  
The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment...
8093229 Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs as HSP90-inhibitors  
Alkynyl pyrrolo [2,3-d] pyrimidines of Formula I are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of various...
8080556 2-amino pyrimidine compounds as potent HSP-90 inhibitors  
The present invention is directed to compounds of formula (I), or pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors.
8071583 Pyrrolo[3,2-D] pyrimidines as DPP-IV inhibitors for the treatment of diabetes mellitus  
The present invention relates to substituted pyrrolo[3,2-d]pyrimidines of formula (I), wherein R1 and R2 are defined as in claim 1, including the tautomers, stereoisomers, mixtures and salts...
8053434 Kinase inhibitors and their uses  
The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein...
8034821 Selective serine/threonine kinase inhibitors  
Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective...
8030319 Methods for treating cancer and other pathological proliferating disorders by inhibiting mitosis using pyrrolo[2 3-d]pyrimidines  
The present invention provides methods for treating cancer and other pathological proliferating conditions by inhibiting mitosis using at least one pyrrolo[2,3-d]pyrimidine having the general...
8017618 Antifolate agent combinations in the treatment of cancer  
Compositions and methods useful in the treatment of certain cancers. The methods include administering, to a patient receiving an antifolate anticancer agent, methoxyamine administered in an amount...
8012966 Pyrrolo [3,2-c] pyridine-4-one 2-indolinone protein kinase inhibitors  
The present invention relates to pyrrolo[3,2-c]pyridine-4-one 2-indolinone compounds of Formula (I) and their pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8X, Y...
8008307 Heteroaryl compounds useful as inhibitors of E1 activating enzymes  
This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for...
7998966 Axl kinase inhibitors  
Axl kinase inhibitory compounds are disclosed, as well as compositions and methods of using the same in the treatment of cancer and other conditions mediated by and/or associated with Axl kinase.
7994180 Processes for preparing intermediates of pemetrexed  
The invention provides intermediates of pemetrexed of formula VI and processes for the preparation thereof.
7981902 Substituted pyrrolo[2,3-d]pyrimidines for selectively targeting tumor cells with FR type receptors  
A compound for treating cancer tumors, particularly ovarian cancer tumors, is described, where a fused cyclic pyrimidine having a cancer treating ability is effective to allow selective delivery to...
7981903 2-[2-{phenylamino}-1H-pyrrolo[2,3-D]pyrimidin-4-yl)amino] benzamide derivatives as IGF-1R inhibitors for the treatment of cancer  
Novel pyrrolopyrimidines as shown in formula (I): and pharmaceutically acceptable derivatives thereof. The compounds are useful in the inhibition of IGF-1R.
7981881 Fused heterocyclic compounds and use thereof  
Fused heterocylic compounds of the following Formula wherein R1, R2, R5, Z, J1 and J2 are described herein, and analogs thereof are provided which are useful in treating leukocyte...
7977331 Tetracyclic fused heterocyclic compound and use thereof as HCV polymerase inhibitor  
The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically...
7977345 c-MET modulators and method of use  
A compound for modulating kinase activity according to Formula I, or a pharmaceutically acceptable salt thereof, Wherein J1, J2, J3, R2, J4, Z, Ar and R3 are as defined in the specification,...
7968536 Heterocyclic compounds useful as RAF kinase inhibitors  
The present invention provides compounds useful as inhibitors of protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
7968557 Substituted pyrrolo[2,3-2]pyrimidines as protein kinase inhibitors  
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated...
7960394 Quinazoline derivative  
This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R1 represents a lower alkyl group et al; R2 and R3 are same and different and represents hydrogen...
7960396 Inhibitors of Bruton's tyrosine kinase  
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are...
7951810 Substituted pyrrolo[2,3-d]pyrimidines as inhibitors of E1 activating enzymes  
This invention relates to compounds of formula (I-A) wherein Ring A and the variables X, Y, R3a, R3b, R3c, R3d, R4, R5, R5′, and m are defined herein. The compounds of formula (I-A) inhibit E1 a...
7951811 Pyrrolo[2,3-D]pyrimidine derivatives substituted with a cyclic amino group  
[PROBLEM TO BE SOLVED] An object of the present invention is to provide an antagonist against CRF receptors and/or an agonist for δ receptors which is effective as a therapeutic or prophylactic ...
7951812 Substituted pyrrolo[2,3-d]pyrimidines as antifolates  
The present invention is directed to antifolate compounds having the structure wherein: X is CHR9 or NR9;Y1, Y2, and Y3 independently are O or S;V1 and V2 independently are O, S, or NZ;Z is H,...
7947695 5-membered annelated heterocyclic pyrimidines as kinase inhibitors  
This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, Q1, Q2, X1, X2, Y and Z have defined meanings, having cell cycle kinase inhibiting enzymatic activity,...
7947690 Pyrimidine derivative condensed with a non-aromatic ring  
The present invention provides a condensed pyrimidine compound represented by formula (I) or pharmaceutically acceptable salt thereof: where A represents a ring where at least one carbon atom...
7932259 Pyrrolo[2,3-d]pyrimidine derivatives substituted with a cyclic amino group  
An object of the present invention is to provide an antagonist against CRF receptors which is effective as a therapeutic or prophylactic agent for diseases in which CRF is considered to be...
7919498 Substituted pyrazolo[3,4-d]pyrimidines as PI3K inhibitors  
Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders,...
7910596 Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes  
The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment...
7906520 Methods for treating pain  
The present invention features methods and compositions for preventing, reducing, or treating a traumatic, metabolic or toxic peripheral nerve lesion or pain including, for example, neuropathic...
7902204 Diazaindole-dicarbonyl-piperazinyl antiviral agents  
The invention comprises substituted diazaindole-dicarbonyl-piperazinyl derivatives of general Formula I wherein: Q is selected from the group consisting of -- may represent a bond;T is —C(O)— or ...
7897607 Cyclic compounds  
There is provided a CRF receptor antagonist comprising a compound of the formula (I): A-W—Ar (I) wherein, A is a group represented by the formula (A1) or (A2): (wherein, ring Aa is a 5- or 6...
7884110 Fused heteroaryl pyridyl and phenyl benzenesuflonamides as CCR2 modulators for the treatment of inflammation  
Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the...
7868000 Aspartyl protease inhibitors  
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein j, k, U, W, R, R1, R2, R3, R4, R6, R7 and R7a are as described...
7855216 Aza-indolyl compounds and methods of use  
The invention relates to azaindolyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azaindolyl compounds which inhibit MEK kinase activity. The...
7842699 Pyrrolo[2,3-D]pyrimidine compounds  
A compound of the formula wherein R1, R2 and R3 are as defined above, which are inhibitors of the enzyme protein kinases such as Janus Kinase 3 and as such are useful therapy as immunosuppressive...
7834016 Inhibitors of the interaction between MDM2 and p53  
The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein...
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