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7348326 |
Heteroaryl fused aminoalkyl imidazole derivatives: selective modulators of GABAa receptors
Disclosed are compounds of the formula:
or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 , are variables defined...
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7345045 |
Pyrido-pyrimidine compounds as medicaments
The invention is directed to methods to inhibit TGF-β and/or p38-α kinase using compounds of the formula
or the pharmaceutically acceptable salts thereof
wherein R 3 is a...
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7338955 |
Medicament for treatment of neuropathies
Compounds of formula (I) in which R 1 =C 1-6 alkyl, optionally halosubstituted; R 2 =H, C 1-4 alkyl, optionally halosubstituted or replaced by halogen; R 3 =C 2-4 alkyl, optionally...
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7297700 |
Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
Bicycloheteroaryl compounds are disclosed that have a formula represented by the following:
The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and...
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7253155 |
Combinations for the treatment of immunoinflammatory disorders
The invention features a method for treating a patient having an immunoinflammatory disorder, by administering to the patient (i) a tetra-substituted pyrimidopyrimidine, and (ii) a corticosteroid...
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7232828 |
PPAR Ligands that do not cause fluid retention, edema or congestive heart failure
Methods are provided for treating or prophylactically preventing metabolic disorders in humans without causing, promoting, or aggravating fluid retention, peripheral edema, pulmonary edema, or...
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7223767 |
Tetrahydroquinazolines and dihydrocyclopentapyrimidines as CRF antagonists
Compounds of the formula (I):
and pharmaceutically acceptable salts or prodrugs thereof, wherein m, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined herein. The invention also provides...
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7223766 |
Bi-cyclic pyrimidine inhibitors of TGFβ
Compounds in which a pyrimidine nucleus is bridged at the 5 and 6 position and are further substituted at positions 2 and 4 with substituents comprising aromatic moieties are useful in treating...
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7211587 |
Quinoline derivatives and quinazoline derivatives having azolyl group
An object of the present invention is to provide compounds having potent antitumor activity. The compounds according to the present invention are compounds represented by formula (I) or...
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7208498 |
Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in...
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7205289 |
Combinations of active ingredients with insecticidal and acaricidal properties
The invention relates to novel active compound combinations of certain cyclic ketoenols and certain insecticidally active compounds that together have very good insecticidal and acaricidal properties.
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7192949 |
Substituted bicyclic pyrimidinones as a mitotic kinesin KSP inhibitors
The present invention relates to cycloalkylpyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for...
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7166595 |
Compounds, methods and compositions
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
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7160890 |
Compounds specific to adenosine A3 receptor and uses thereof
This invention pertains to compounds which specifically inhibit the adenosine A 3 receptor and the use of these compounds to treat a disease associated with A 3 adenosine receptor in a subject,...
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7153861 |
5,6 -Trimethylenepyrimidin-4-one compounds
Pyrimidone compounds of formula (I):
are inhibitors of the enzyme Lp-PLA 2 and are of use is treating atheroscelerosis.
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7138398 |
Substituted 4-amino-2-arylcyclopenta[d]pyrimidines, their preparation, their use and pharmaceutical preparations comprising them
The present invention relates to compounds of formula (I) wherein R 1 , R 2 and R 3 have the meanings given in the claims. Said compounds are valuable active agents in medicaments for the...
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7125880 |
Corticotropin releasing factor antagonists
Corticotropin-releasing factor (CRF) antagonists having the formulae
wherein the dashed lines, A, B, Y, Z, G, R 3 , R 4 , R 5 , R 6 , R 16 and R 17 are as defined in the application, and...
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7115658 |
Inhibitors of hepatitis C virus RNA-dependent RNA polymerase
Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus
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7112590 |
Thrombin inhibitors
The invention relates to compounds that are heterocyclic derivatives of dipeptides and dipeptides mimetics and pharmaceutically acceptable salts thereof. The compounds are used as thrombin inhibitors
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7105525 |
6-alkoxy-pyrido-pyrimidines
The present invention provides compounds of the Formula I:
wherein R 1 is alkyl, cycloalkyl, cycloalkylalkyl, or —CH 2 -alkenyl, X 1 is O, NH, N(alkyl), S or —C(═O), Z is N or CH; and R...
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RE39265 |
Heteroarylpiperidines, and their use as antipsychotics and analgetics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a...
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7091207 |
Method of treating myocardial infarction with PDE-5 inhibitors
A method is provided for the prevention of ischemia/reperfusion injury, for example, in patients undergoing heart surgery, and involves the administration of a phosphodiesterase-5 (PDE-5) inhibitor...
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7071190 |
Inhibitors to tubulin polymerization
The invention relates to the inhibition of tubulin polymerization. The invention provides compounds and methods for inhibiting tubulin polymerization. The invention also provides compositions and...
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7064130 |
Use of radical-scavenging compounds for treatment and prevention of NO-dependent microcirculation disorders
A method of treatment of the human or non-human animal body for treating NO-dependent microcirculation disorders is disclosed, for example microcirculation disorders caused by metabolic diseases,...
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7019003 |
Peptide deformylase inhibitors
Novel PDF inhibitors and novel methods for their use are provided.
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7001887 |
Peptide derivatives
A compound of Formula (1):
wherein
R 1 represents an amidinophenyl group, etc.; R 2 represents a hydrogen atom, etc.; R 3 represents a carbamoylalkyl group, etc.; R 4 represents a...
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6964968 |
Method for the treatment or prevention of viral infection using nucleoside analogues
Viral infections selected from the group consisting of herpes simplex virus, varicella zoster virus, respiratory syncytial virus and cytomegalovirus can be treated by administering to the host a...
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6962919 |
Nitrogen-containing heterocyclic compounds, their production and use
A compound of the formula:
wherein one of A and D is N and the other is C, or both are N; B is N or C; m is 0-3; R 1 , R 2 and R 3 each is (i) H or (ii) a group bound via C, N, O or S; R 4 ...
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6943172 |
Rho-kinase inhibitors
Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and...
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6911449 |
Inhibition of matrix metalloproteases by substituted biaryl oxobutyric acids
Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the...
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6881753 |
Potassium channel inhibitors and method
Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure:
where A, B, D, Q, X 1 , R, R 1 , X 2 and R 2 are as defined herein....
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6872727 |
Polycyclic pyrimidine -2,4(1H,3H)-diones with functionalized alkyl residues at the 1- and/or 3-position(s); methods for their synthesis and pharmaceutical preparation
Polycyclic pyrimidine-2,4(1H,3H)-diones with functionalized alkyl residues at the 1-, the 3-, or both position(s); methods for their synthesis, production, and pharmaceutical preparation. The...
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6867201 |
Heteroaromatic bicyclic derivatives useful as anticancer agents
The invention relates to compounds of the formula 1
and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R 1 , R 3 and R 4 are as defined herein. The invention also...
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6858611 |
Potassium channel inhibitors
Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described.
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6852722 |
Compositions and methods for stimulating gastrointestinal mobility
The present invention is directed to methods for stimulating the motility of the gastrointestinal system in a patient which comprises administering a growth hormone secretagogue, a prodrug thereof...
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6849634 |
Potassium channel inhibitors
Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.
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6787553 |
Methods for remodeling neuronal and cardiovascular pathways
The present invention provides a method of administration of an agent which acts to remodel neuronal or vascular pathways for the long term management of sexual dysfunction in both males and...
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6787541 |
Thieno-and furopyrimidine derivatives as A2A-receptor antagonists
Compounds of formula (I): wherein X is S. Compounds can be used for treating a disorder in which the blocking of purine receptors is beneficial.
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6743799 |
Use of PDE V inhibitors for improved fecundity in mammals
The invention relates to the use of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase type five (cGMP PDE V) inhibitor for increasing fecundity in a mammal by one or more of (a)...
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6740654 |
Squaric acid derivatives
Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L 2 is a covalent bond or an atom or group —O—,...
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6686382 |
Sulfonamides and derivatives thereof that modulate the activity of endothelin
Thienyl-, furyl-, pyrrolyl- and phenylsulfonamides, formulations of pharmaceutically-acceptable derivatives thereof and methods for modulating or altering the activity of the endothelin family of...
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6660746 |
Substituted 4-amino-2-aryl-tetrahydoquinazolines, their preparation, their use and pharmaceutical preparations comprising them
The present invention relates to compounds of formula I: wherein R 1 , R 2 , and R 3 have the meanings indicated in the specification, which are valuable pharmaceutical active compounds for the...
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6653309 |
Inhibitors of IMPDH enzyme technical field of the invention
The present invention relates to compounds which inhibit IMPDH. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions...
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6653295 |
Inhibitors of hepatitis C virus NS3 protease
The present invention relates generally to a novel class of pyrimidinones of Formula (I): that are useful as serine protease inhibitors, and more particularly as Hepatitis C virus NS3 protease...
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6649619 |
Compounds
Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA 2 and are of use in treating atheroscelerosis.
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6649618 |
Substituted amidoalkyl-uracils and their use
Novel amidoalkyl-uracil derivatives of the formula (I) in which A represents 1-3 ring atoms and X represents optionally substituted (C 2 -C 10 )alkylene or (C 3 -C 8 )cycloalkylene as defined in...
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6645971 |
Quinazolinone derivatives
A compound given by general formula (1): [wherein T represents oxygen or sulfur atom, Y represents alkyl, cycloalkyl group, etc., ring W represents benzene ring, etc., R 1 and R 2 represent...
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6627628 |
Substituted 4-amino-2-aryl-cyclopenta&lsqb d&rsqb pyrimidines, their production and use and pharmaceutical preparations containing same
The present invention relates to compounds of formula (I) wherein R 1 , R 2 and R 3 have the meanings given in the claims. Said compounds are valuable active agents in medicaments for the...
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6617330 |
Pyrimidin-4-enamine as fungicide
Novel pyrimidine derivatives of formula I as well as possible isomers and mixtures of isomers thereof. The novel compounds have plant-protective properties and are suitable for protecting plants...
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6617325 |
Biphenyl derivatives, production thereof and uses as medicines
The present invention relates to biphenyl derivatives of general formula wherein R a to R g and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically...
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