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7618650 |
Combination of a hypnotic agent and substituted bis aryl and heteroaryl compound and therapeutic application thereof
The invention concerns the combination of a short-acting hypnotic agent and a compound of formula (I):
Wherein X, Y, Z, A, B, D, Ar, R 1 and R 2 are as defined herein. The combination of this...
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7608616 |
Methods for reducing the risk of an adverse drug interaction in a patient suffering from insomnia
Disclosed herein is a method for treating a patient with Quazepam that reduces the risk of an adverse interaction between the Quazepam and drug that is a substrate of the cytochrome P450 enzyme...
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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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7598237 |
7-aryl 1,5-dihydro-4,1-benzoxazepin-2(3H)-one derivatives and their use as progesterone receptor modulators
This invention provides progesterone receptor modulators having the structure:
wherein R 1 to R 7 , X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.
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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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7582625 |
Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP-antagonists of general formula I
wherein R 1 , R 2 , R 3 and R 4 are defined as in claim 1, the tautomers, the isomers, the diastereomers, the...
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7582624 |
Benzodiazepine derivatives and pharmaceutical compositions containing them
Benzodiazepine derivative of formula (I), and pharmaceutically acceptable salts thereof, are found to be active against RSV. Formula (I) Wherein: —R 1 represents C 1-6 alkyl, aryl or...
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7579341 |
Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP antagonists of general formula I
wherein R 1 , R 2 , R 3 and R 4 are as defined in claim 1 , the tautomers, the isomers, the diastereomers, the...
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7576077 |
Fused heterocyclic compounds and their use as metabotropic glutamate receptor antagonists
The present invention is directed to compounds of formula I:
wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 , X 9 , X 10 , R 1 , R 2 , R 3 , R 4 , and n are as defined for formula I in...
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7572783 |
Substituted benzofused heterocycles
The present invention relates to the compounds of Formula I, their preparation and pharmaceutical compositions comprising them. The compounds and pharmaceutical compositions are useful, for...
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7569561 |
2,4-diaminopyrimidines useful for treating cell proliferation diseases
The present invention encompasses compounds of general formula (1)
wherein
R 1 to R 6 , X and Y are defined as in claim 1 , which are suitable for the treatment of diseases...
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7566707 |
Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula
wherein Y and R 1 to R 4 are defined as in claim 1 , the tautomers, enantiomers,...
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7560455 |
3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The pre-sent invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the...
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7541355 |
Conversion process for 2,3-benzodiazepine enantiomers
Methods for the racemization of an enantiomer of a 2,3-benzodiazepine molecule into the corresponding racemic mixture under either basic or acidic conditions are described. Furthermore, the...
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7534859 |
Protein kinase C epsilon as modulator of anxiety, alcohol consumption and self-administration of drugs of abuse
The present invention is directed to the production of PKC isozyme ε (PKCε)-deficient cells and non-human animals. The present invention is further directed to the identification of PKCε as a...
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7528129 |
CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP-antagonists of general formula I
wherein R 1 , R 2 , R 3 , R 4 and X are defined as in claim 1 , the tautomers, the isomers, the diastereomers, the...
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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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7517873 |
Substituted pyrimidodiazepines
The present invention provides PLK1 inhibitor compounds of formula I:
Useful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and...
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7514442 |
Trisubstituted 4-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds,...
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7511039 |
β-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins
There are disclosed β-sheet mimetics and methods relating to the same for imparting or stabilizing the β-sheet structure of a peptide, protein or molecule. In one aspect, β-sheet mimetics are...
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7511033 |
Dihydro-benzo[B][1,4]diazepin-2-one sulfonamide derivatives
The present invention relates to compounds of formula (I), a process for the manufacture thereof, their use for the preparation of medicaments for treating CNS disorders and pharmaceutical...
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7498324 |
Substituted lactams as inhibitors of Aβ protein production
This invention relates to novel lactams of Formula (I):
having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the...
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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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7494984 |
Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors
The invention encompasses a series of bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the...
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7482338 |
Non-amide nonanes
Compounds of Formula I:
and pharmaceutically-acceptable salts thereof, wherein Q, E and D are as defined in the specification, enantiomers, in vivo-hydrolysable precursors, pharmaceutical...
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7482337 |
Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
Disclosed are substituted xanthines of general formula
wherein R 1 to R 4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts...
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7476665 |
Benzodiazepine CGRP receptor antagonists
The present invention is directed to compounds of Formula I: I (where variables R 1?, R 2?, R 3?, R 6?, R 7?, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP...
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7470695 |
N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds,...
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7462621 |
Use of substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo[1,2-a] pyrimidin-5(1H)one derivatives as therapeutic agents
The invention relates to an use of pyrimidone derivative represented by formula (I) or a salt thereof:
wherein m, n, p, X, Y, R1, R2, R3, R4 and R5 are as defined herein for treating a variety...
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7456223 |
Treatment of bruxism
A composition and its use for local percutaneous delivery of a drug, in particular a muscle relaxant, more particularly cyclobenzaprine present in an amount of about 1 to about 10% by weight of the...
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7456172 |
Succinoylamino benzodiazepines as inhibitors of Aβ protein production
This invention relates to novel lactams having the formula (I):
to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid...
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7456171 |
1,4-Diazabicyclo[3.2.2]nonanecarboxamide derivatives, preparation and therapeutic use thereof
The present invention discloses and claims compounds of general formula
in which X represents a nitrogen atom or a group of formula C—R 2 , P represents a group of formula C—R 3 , Q...
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7442694 |
Diazabicyclic compounds useful in the treatment of CNS and other disorders
The present invention relates to a compounds of formula I:
wherein A, B, D, E and F are defined herein; that are useful in treating central nervous system (CNS) diseases, disorders and...
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7439237 |
Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP antagonists of general formula
wherein A, X and R 1 to R 3 are defined as in claim 1 , the tautomers, the diastereomers, the enantiomers, the...
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7439236 |
Pharmaceutical composition for the treatment of CNS and other disorders
The present invention relates to compounds of formula I
The substituent designations are as disclosed. At least one of B, Q, D and E is nitrogen. The present invention also provides a method of...
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7427613 |
7-aryl-3,9-diazabicyclo(3.3.1)non-6-ene derivatives and their use as renin inhibitors in the treatment of hypertension, cardiovascular or renal diseases
The invention relates to novel 3,9-diazabicyclo[3.3.1]nonene derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions....
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7423033 |
Hydroxyalkanoylaminolactams and related structures as inhibitors of aβ protein production
This invention relates to novel lactams having the formula (I):
to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid...
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7414049 |
4-oxo-2,3,4,5-tetrahydro-benzo[b][1,4]diazepine derivatives
The invention relates to 4-oxo-2,3,4,5-tetrahydro-benzo [b][1,4]diazepines of formula I
wherein R 1 , R 2 , R 3 and R 4 are as defined in the description and claims, which are γ-secretase...
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7410963 |
Benzo-1,4-diazepin-2-one derivatives as phosphodiesterase PDE2 inhibitors, preparation and therapeutic use thereof
The invention relates to compounds having PDE2 inhibitory activities, as well as therapeutic methods by administering said compounds, in particular for treating various diseases of the central or...
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7407952 |
Reverse-turn mimetics and compositions and methods related thereto
Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed:
...
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7390801 |
Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions...
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7388005 |
Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo [1,2-a]pyrimidin-5(1H)one derivatives for neurodegenerative disorders
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C 1-2 alkyl group and a...
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7375101 |
Benzodiazepine derivatives, preparation thereof and use thereof
Compounds of Formula (I) wherein R 1 , R 3 , R 4 , R 5 and X are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are...
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7375099 |
Malonamide derivatives
The invention relates to malonamide derivatives of formula
wherein each of the variables are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The...
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7358243 |
Diazabicyclonane and-decane derivatives and their use as opioid receptor ligands
This invention relates to novel diazabicyclononane and -decane derivatives useful as opioid receptor ligands. More specifically, the invention provides compounds useful as μ opioid receptor ligands.
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7358239 |
Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z...
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7314871 |
2-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors, for treatment of hypertension
The application claims a method for treating hypertension by administering an effective amount of a compound of the formula (I)
wherein the variable groups are as defined in the specification...
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7304056 |
Succinoylamino lactams as inhibitors of Aβ protein production
This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid...
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7282496 |
Allenic aryl sulfonamide hydroxamic acids as matrix metalloproteinase and TACE inhibitors
Compounds of the formula
are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis,...
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7265106 |
Method for isolating (R)-tofisopam
(R)-tofisopam, substantially free of the (S)-enantiomer of tofisopam, is obtained by separating the enantiomers of tofisopam by chromatography employing a chiral separation medium comprising (i)...
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