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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...
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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...
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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—...
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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,...
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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),...
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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.
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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...
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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...
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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...
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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...
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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...
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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)...
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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...
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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...
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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...
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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.
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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.
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7994180 |
Processes for preparing intermediates of pemetrexed
The invention provides intermediates of pemetrexed of formula VI and processes for the preparation thereof.
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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...
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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.
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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...
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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...
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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,...
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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.
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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...
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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...
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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...
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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...
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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 ...
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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,...
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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,...
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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...
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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...
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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,...
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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...
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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...
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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 ...
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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...
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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...
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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...
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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...
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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...
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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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