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7612094 |
Tri-substituted heteroaryls and methods of making and using the same
Compounds of formula (I) possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic...
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7612073 |
Methods of administering tetrahydrobiopterin, associated compositions, and methods of measuring
The present invention is directed to treatment methods of administering tetrahydrobiopterin, including in oral dosage forms, in intravenous formulations, and with food. Also disclosed herein are...
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7612072 |
Amorphous form of a phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor
The present invention relates to a novel amorphous form of the dihydrogenphosphate salt of...
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7612071 |
Compositions and methods employing aminopterin
The present invention relates to pharmaceutical compositions containing the antifolate aminopterin, processes for making the compositions, and methods of using them to treat disorders in adult and...
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7612070 |
Indole derivative having heterocycle and mono- or diazaindole derivative
There is provided a compound represented by the general formula (1):
wherein Het represents an optional substituted heterocylic group A 1 and A 2 each independently represent —CH═, etc.;...
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7608622 |
Imidazo[4,5-b]pyrazinone inhibitors of protein kinases
The invention is directed to compounds of Formula I:
wherein Q, Y, A are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof,...
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7608618 |
Urea or thiourea substituted 1,4-pyrazine compounds useful as anti-cancer agents and for inhibiting Chk1
Compounds of the formula
wherein: Y′ is O or S, W′ is
optionally substituted,
Z′ is selected from the group consisting of
wherein Q′ is OR 7 and R 7 is C 1-3 alkyleneC 3-8...
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7601726 |
Substituted pyrazolo[3,4-d]pyrimidines as p38 MAP kinase inhibitors
Compounds of formula Ia or Ib:
wherein A, W, X, Y, R 1 , R 2 , R 3 and R 4 are as defined herein. Also disclosed are methods of making the compounds and methods of using the compounds for...
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7601717 |
Pterin analogs
Disclosed herein are analogs of tetrahydrobiopterin, compositions containing the same, and methods of treating an individual suffering from a condition responsive to tetrahydrobiopterin by...
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7601716 |
Pyridopyrazines and derivatives thereof as ALK and c-Met inhibitors
The present invention provides a compound of Formula I
or a pharmaceutically acceptable salt form thereof, wherein A, L 1 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and X are as defined herein. The...
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7598253 |
Reverse-turn mimetics and methods relating thereto
Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have...
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7592342 |
Quinoxaline derivatives as PI3 kinase inhibitors
Invented is a method of inhibiting the activity/function of PI3 kinases using quinoxaline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune...
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7592341 |
Peptide-enhanced corneal drug delivery
Improved methods and preparations are provided for ocular administration of therapeutic drugs. The preparations include respective quantities of a drug and a peptide which enhances transport of the...
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7592340 |
Quinoxalines useful as inhibitors of protein kinases
The present invention relates to compounds of formula I useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and...
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7589093 |
Alkyl substituted indoloquinoxalines
Novel substituted indoloquinoxalines of formula
wherein
R 1 is hydrogen or represents one or more similar or different substituents in the positions 7 to 10 selected from the group...
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7589068 |
Inhibitors of Akt activity
The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for...
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7585873 |
1-(aminoalkyl)-3-sulfonylazaindoles as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
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7585863 |
Therapeutic amides
The invention provides compounds of the formula:
wherein A, X, Y, and Z are as defined in the specification. The compounds are effective anti-tumor agents. The invention also provides...
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7585862 |
Reverse-turn mimetics and method relating thereto
Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures...
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7576085 |
Imidazopyrazines as cyclin dependent kinase inhibitors
In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds,...
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7572787 |
Substituted naphthalene sulfonamides
The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful...
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7566715 |
Substituted sulfonamide compounds useful for the prophylaxis and treatment of conditions relating to obesity, type II diabetes and/or disorders of the central nervous system
The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the...
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7566714 |
Methods and compositions for the treatment of metabolic disorders
The present invention is directed to a novel methods and compositions for the therapeutic intervention in hyperphenylalaninemia. More specifically, the specification describes methods and...
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7563895 |
Quinoxaline compounds
Certain amidophenyl-sulfonylamino-quinoxaline compounds are CCK2 modulators useful in the treatment of CCK2 mediated diseases.
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7563790 |
Pyridazine derivatives
Pyridazine derivatives of the formula (I) act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumors, cachexia, atherosclerosis, rheumatoid arthritis,...
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7563773 |
Anthelmintic oral homogeneous veterinary pastes
This invention provides for, inter alia, oral homogeneous veterinary pastes for the treating, controlling and preventing of endo- and ectoparasite infections in warm-blooded animals or birds, such...
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7560483 |
Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require...
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7560450 |
Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted xanthines of general formula
the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable...
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7557104 |
Imidazopyrazines as protein kinase inhibitors
In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds,...
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7553836 |
Melanin concentrating hormone receptor-1 antagonists
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I
wherein R 1a , R 1b , R 1c...
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7550597 |
Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases
This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or Lck tyrosine kinase, to pharmaceutical compositions comprising...
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7544694 |
Substituted diaza-spiro-[5.5]-undecane derivatives and their use as neurokinin antagonists
This invention concerns substituted diaza-spiro-[5.5]-undecane derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity, a combined NK 1 /NK 2 antagonistic...
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7544684 |
Hydrazono-malonitriles
Hydrazono-malonitrile derivatives of the formula (I) in which R 1 , R 2 , R 3 , R 3′ and R 4 have the meanings given in Claim 1 act as phosphodiesterase IV inhibitors and can be employed for...
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7541360 |
4-amino-7,8-dihydropteridines, pharmaceutical compositions containing them and their use for the treatment of diseases which are caused by an increased nitric oxide level
The present invention relates to the area of NO synthase inhibition and, more particularly, relates to novel 4-amino-7,8-dihydropteridines, pharmaceutical compositions containing said compounds,...
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7541031 |
Methods for treating rheumatoid arthritis using human antibodies that bind human TNFα
Human antibodies, preferably recombinant human antibodies, that specifically bind to human tumor necrosis factor α (hTNFα) are disclosed. These antibodies have high affinity for hTNFα (e.g., K d...
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7538110 |
Opioid antagonists
Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.
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7538109 |
Quinoxalin-3-one derivatives as orexin receptor antagonists
The invention relates to quinoxalinone derivatives of general Formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related...
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7534795 |
Compounds and their use related to compositions for treating disease
Novel compounds and their uses are disclosed herein.
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7534794 |
Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases
The invention relates to compounds of the general formula (I):
wherein
Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO 2 —, —NH—, (ii) a C 1-4...
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7524845 |
Azaindazole compounds and methods of use
Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in...
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7524839 |
Compounds, their use and preparation
The invention-provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I):
in which Ar, R 2 , R 3 , R 4 and R 5 are as defined in...
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7517988 |
Hydroxamates as therapeutic agents
The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore...
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7517874 |
Substituted imidazo[1,5-a][1,4]diazepines and imidazo[1,5-a]pyrazines as cannabinoid receptor agonists for the treatment of pain
The present invention provides substituted imidazoheterocyclic compounds having the structure of formula I
Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates...
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7511040 |
Imidazopyrazines as protein kinase inhibitors
In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or Aurora kinases, methods of preparing such compounds,...
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7501416 |
Quinoxaline compounds and methods of using them
The present invention generally relates to quinoxaline compounds having Formula 1 or Formula 2 wherein the variables are as defined herein, and methods of using them.
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7501411 |
Triazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following:
The compounds may be prepared as pharmaceutical compositions, and may be used for...
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7498334 |
Pyrrolopyrimidines as phosphodiesterase VII inhibitors
Pyrrolopyrimidine derivatives of the formula I
in which R 3 , R 4 , R 5 , R 6 and X are as defined in claim 1 , act as phosphodiesterase VII inhibitors and can be employed for the treatment...
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7498323 |
Spiro-piperidine compounds and medicinal use thereof
The present invention relates to a spiro-piperidine compound represented by formula (I):
wherein R 1 represents hydrogen, an aliphatic hydrocarbon group which may have a substituent(s) or a...
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7491383 |
Compositions having enhanced pharmacokinetic characteristics
Compositions comprising a therapeutic component and an efficacy enhancing component, that enhances the pharmacokinetic disposition of the therapeutic component, are disclosed. The therapeutic...
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7482336 |
Aminocyclohexanes as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment...
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