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8119635 Diazabicyclic central nervous system active agents  
Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
8106064 Pyrimidine-2,4-dione HIV reverse transcriptase inhibitors  
The invention is related to pyrimidine-2,4-dione HIV reverse transcriptase inhibitors of Formula (I), (II), or (III): or a pharmaceutically acceptable salt, thereof, compositions containing such...
8101625 Pyrimidinones as Casein Kinase II (CK2) modulators  
A compound having Formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1 and R2 are defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.
8101615 1,4-diaryl-dihydropyrimidin-2-ones and their use as human neutrophil elastase inhibitors  
The invention relates to novel heterocyclic derivatives of the general formula (I), processes for their preparation, and their use in medicaments, especially for the treatment of chronic...
8101626 GPR119 receptor agonists in methods of increasing bone mass and of treating osteoporosis and other conditions characterized by low bone mass, and combination therapy relating thereto  
The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an...
8093246 O-linked pyrimidin-4-amine-based compounds, compositions comprising them, and methods of their use to treat cancer  
O-linked pyrimidin-4-amine-based compounds, pharmaceutical compositions comprising them, and methods of their use are described. Particular compounds of the invention are of formula I:
8093245 4-amino-1H-pyrimidin-2-one based compounds, compositions comprising them and methods of their use  
4-Amino-1H-pyrimidin-2-one-based compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of various diseases and disorders are disclosed....
8088783 MAPK/ERK kinase inhibitors  
Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(pyrimidinylamino)-1,2,3,4-tetrahydr opyrimidine-5-hydroxamic acids, show below: wherein the variables are as defined herein, and pharmaceutical...
8084458 Synthesis of locked nucleic acid derivatives  
Methods are described for the synthesis of Locked Nucleic Acid (LNA) derivatives using certain nitrogen-containing nucleophiles.
8076324 Di(hetero)arylcyclohexane derivatives, their preparation, their use and pharmaceutical compositions comprising them  
The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are...
RE43029 Process for preparing a creatine heterocyclic acid salt and method of use  
This invention relates to a process for the synthesis and method of use of an effective amount of a creatine heterocyclic acid salt for the regulation athletic function in humans.
8076302 Pyrimidine nucleoside derivatives and salts thereof  
A novel pyrimidine nucleoside derivative represented by the following formula (1) and a salt thereof, as well as a pharmaceutical composition comprising the same as an active ingredient have...
8076347 Compounds and methods for the treatment of cancer  
(−)-(2S,4S)-1-(2-Hydroxymethyl-1,3-dioxolan-4-yl)cytosine (also referred to as (−)-OddC) or its derivative and its use to treat cancer in animals, including humans.
8048888 Anti-proliferative combination therapy using certain platinum-based chemotherapeutic agents and EGFR inhibitors or pyrimidine analogues  
The present invention describes a method or uses of prevention and/or treatment of a cancer or a tumor, and in particular to a combination therapy, methods, compositions and pharmaceutical packages...
8044040 N-heterocyclic inhibitors of TNF-alpha expression  
N-heterocyclic compounds that block cytokine production via inhibition of p38 kinase are disclosed. In one embodiment, compounds of the present invention are represented by Formula (I): Methods of...
8034823 Method of increasing drug oral bioavailability and compositions of less toxic orotate salts  
The present invention relates generally to the method of increasing the oral bioavailability, reducing chemotherapy induced toxicity and side effects, and improving the effectiveness of...
8034824 Iontophoretic preparation for treatment of breast cancer and/or mastitis  
The present invention is to provide means to treat breast cancer and/or mastitis by topically administering a non-steroidal antiinflammatory analgetic agent and/or an anticancer agent and allowing...
8030322 Spirocompounds useful as modulators for dopamine D3 receptors  
The present invention relates to compounds of formula (I) or salts thereof wherein A, X, R2, R4 and n are defined herein, processes for their preparation, intermediates used in these processes,...
8025899 Solid pharmaceutical dosage form  
A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one...
7994170 1,3-dihydro-imidazo[4,5-C]quinolin-2-ones as lipid kinase inhibitors  
The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use...
7994183 Solid preparation comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-4-fluorobenzonitrile  
The present invention provides a solid preparation containing 2[[6-[(3R)-3-amino-1 -piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidin yl]methyl]-4-fluorobenzonitrile (compound (A)) or a...
7989446 4-amino 5-cyanopyrimidine derivatives  
The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof, having a safe and potent...
7973038 Modulators of ATP-binding cassette transporters  
Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cys...
7973035 Inhibitors of C-FMS kinase  
The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts...
7968124 Compositions for the reversal and detoxification of anesthetics and other compounds and methods of their use  
Methods of attenuating the toxic or medically undesirable effects of drugs and toxins in a human by administering to a human an injectable formulation comprised of a dispersion of particles...
7964624 Inhibitors of serine proteases  
The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof. These compounds inhibit serine protease, particularly the hepatitis C virus NS3-NS4A protease.
7956052 Modulators of ATP-binding cassette transporters  
Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cys...
7943626 Substituted 1,3-dialkyl-2,4-dioxo-6-(pyridylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acid inhibitors of MAPK/ERK kinase  
Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(arylamino)-1,2,3,4-tetrahydropyrimi dine-5-hydroxamic acids, show below: wherein the variables are as defined herein, and pharmaceutical...
7939109 Method of treating neoplastic disease in a human or animal patient  
A method of treating neoplastic disease in a human or animal patient is provided comprising administering to the patient an anti-neoplastic effective amount of a composition comprising as the sole...
7939527 Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase  
Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical...
7935710 Microbicidal pyrimidine or triazine for preventing sexual HIV transmission  
The present invention concerns the microbicidal activity of certain pyrimidine or triazine containing non-nucleoside reverse transcriptase inhibitors. The compounds of the present invention inhibit...
7915270 Oxazole ketones as modulators of fatty acid amide hydrolase  
Certain oxazole ketone compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions...
7915271 1,3-oxazolidin-2-one derivatives useful as CETP inhibitors  
Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol,...
7910580 Enhancement of effectiveness of 5-Fluorouracil in treatment of tumor metastases and cancer  
Tumor growth and metastases in cancer patients are inhibited by administration of a combination therapy including effective amounts of 5-Fluorouracil and a methylol transfer agent such as...
7906523 Dipeptidyl peptidase inhibitors  
Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently...
7906554 Combination chemotherapy compositions and methods  
This invention relates to combination therapies involving anticancer chemotherapeutic agents and isoflavones or analogues thereof. The invention further relates to compounds, methods and...
7902192 Inhibitors of P38 and methods of using the same  
In general, the present invention relates to compounds capable of inhibiting p38, methods for inhibiting p38 in vivo or in vitro, and methods for treating conditions associated with p38 activity or...
7893073 Heterocyclic derivatives  
The invention relates to novel 3,4-dihydropyrimidin-2(1H)-one derivatives having the formula processes for their preparation, and their use in compositions, and in the treatment of chronic...
7888367 1-[2′,3′ -dideoxy-3′ C-(hydroxymethyl)—beta-D-erythro-pentofuranosyl] cytosine derivatives as HIV  
Compounds of the formula (I) wherein: R1 is independently H1—OR3, —NHR4; C1-C4 alkyl; or, when n is 2, adjacent R1 together define an olefinic bond; R2 is H; or when the gem R1 is C1-C4 alkyl, tha...
7872010 Substituted diazabicycloalkane derivatives having affinity for nicotinic acetylcholine receptors  
Provided herein are compositions of a class of substituted diazabicycloalkane derivative compounds, which are useful as modulators of nicotinic acetylcholine receptors. The compounds are useful in...
7872012 Pyrimidinone compounds and preparation and use thereof  
Disclosed are pyrimidinone compounds having formula (I), a preparation and use thereof. The compounds are inhibitors of HMG-CoA reductase, and therefore have antivirus activities and are useful for...
7851479 Use of pyrimidinedione derivative for preventing or treating hepatitis C  
A pyrimidinedione derivative of formula (I) or a pharmaceutically acceptable salt thereof exhibits excellent inhibitory activity against hepatitis C virus.
7846469 Reversible inhibition of sperm receptor synthesis for contraception  
Methods and pharmaceutical compositions are disclosed for reversibly inhibiting sperm receptor activity in animals. Nicarbazin, its derivatives and modifications which retain pharmacological...
7834002 4-amino-5-cyanopyrimidine derivatives  
The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof, having a safe and potent...
7829575 Methods for treating androgen receptor related disorders  
One embodiment is directed toward a method for treating an individual with a disorder affected by androgen receptor activity. This method includes administering a therapeutic amount of DL3...
7820686 Therapeutic agent for inflammatory bowel disease  
The invention is directed to a method of treating an inflammatory bowel disease such as ulcerative colitis or Crohn's disease, which comprises administering an effective amount of the therapeutic...
7820685 Aminopyrimidines useful as kinase inhibitors  
The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and...
7816354 Oxazolidinone compounds and their use as metabotropic glutamate receptor potentiators  
The present invention is directed to compounds of Formula I: Wherein R1, R2, Y, m and n are further defined in the description. The invention also relates to processes for the preparation of the...
7816366 Compositions and methods for treating and preventing dermatoses  
The invention encompasses protectant agents including uracil or a metabolite thereof that effectively prevent and/or treat the cutaneous toxicities and dermatological side-effects associated with...
7812030 Methods, compositions, and kits for organ protection during systemic anticancer therapy  
Methods, compositions, and kits are presented for local tissue protection during systemic administration of anticancer therapeutic agents.