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7595331 |
N-and O-substituted 4-[2-(diphenylmethoxy)-ethyl]-1-[(phenyl)methyl]piperidine analogs and methods of treating CNS disorders therewith
N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred...
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7585858 |
N-sulfonylcarboximidamide apoptosis promoters
Compounds having the formula
are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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7582656 |
Guanidine derivatives and therapeutic uses thereof
Compounds of the formula (I):
in which the radicals R and R 1 to R 10 are as defined in the description, processes for the preparation of them, use thereof for the treatment of cardiovascular...
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7569588 |
Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I:
wherein a, b, c, m, p, r, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , W and X 1 are as defined in the specification. The compounds of formula I are...
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7550485 |
Substituted N-heterocycle derivatives and methods of their use
The present invention is directed to substituted N-heterocycle derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions...
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7550486 |
N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
The present application describes modulators of chemokine receptor activity of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other...
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7544716 |
Tetrahydro-naphthalene derivatives as vanilloid receptor antagonists
This invention relates to tetrahydro-naphthalene derivatives of formula (I)
in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms...
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7517892 |
Ligands for monoamine receptors and transporters, and methods of use thereof
One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian...
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7504512 |
N-acylsulfonamide apoptosis promoters
N-Benzoyl arylsulfonamides having the formula
are BCL-X1 inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-X1 inhibiting compositions and methods of promoting apoptosis...
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7495105 |
Non-racemic mixtures of (S) and (R) enantiomers of N-(2,6-dimethylphenyl)-1-propyl-2-piperidinocarboxamide; related processes and pharmaceutical compositions
The present invention describes a method of separation of the enantiomers of N-(2,6-dimethylphenyl)-1-propyl-2-piperidinocarboxamide. Another object of the present invention refers to the...
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7488738 |
Aminophenoxyacetic acid derivatives and pharmaceutical composition containing thereof
There is provided an aminophenoxyacetic acid derivative of the following formula (I):
wherein, R 1 , R 2 , R 3 and R 4 are, independent from each other, alkoxy group, alkyl group or aryl...
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7479491 |
Azanthranylalkyl and -cycloalkyl amides and their use as VEGF receptor inhibitors
The invention relates to substituted anthranylalkyl and -cycloalkyl amides of general formula (I) and to their use as medicaments for treating diseases caused by persistent angiogenesis.
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7473698 |
Secondary amino anilinic piperidines as MCH1 antagonists and uses thereof
This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a...
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7470711 |
Piperidinyl substituted cyclohexane-1,4-diamines
The present invention relates to piperidine substituted cyclohexane-1,4-diamine compounds of Formula (I)
and pharmaceutically acceptable forms thereof, as α 1a /α 1d adrenoreceptor...
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7459467 |
Manufacturing process for methyl phenidate and intermediates thereof
The present invention discloses selective and complete reduction of pyridine ring in a biaryl system comprising ∝-substituted or non-substituted benzene ring and relates more specifically, not...
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7452908 |
Amide derivatives
This invention relates to compounds which are represented by the general formula [I]
[in which A stands for a group of the following formula [a o ] or [b 0 ]
Ar 1 , Ar 2 and Ar 3 ...
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7452891 |
MCH antagonists and their use in the treatment of obesity
The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention...
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7435747 |
Guanidine and amidine derivatives as factor Xa inhibitors
The present invention relates to compounds of the formula I,
in which R 0 ; Q; X; Q′, D, R 10 and V have the meanings indicated in the claims. The compounds of the formula I are valuable...
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7427632 |
Factor Xa inhibitors
Compounds of formula (I)
in which R 1 , n, Z, R 3 and R 4 have any of the meanings given in the specification, are inhibitors of the serine protease Factor Xa and are useful in the treatment...
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7425567 |
Piperidine derivative compounds and drugs containing the compounds as the active ingredient
A piperidine derivative of formula (I)
(wherein all symbols are as described in the specification.) and an intermediate for the preparation thereof. The compound of formula (I) has...
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7393873 |
Arylsulfonamide derivatives
N-aryl arylsulfonamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin...
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7381734 |
Serine protease inhibitors
Compounds of formula (I)
where R 5 , R 6a , each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
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7368443 |
2,6-disubstituted piperidines and piperazine compounds
The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula:
which are used to treat diseases of the central nervous system,...
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7365082 |
N-(substituted arylmethyl)-4-(disubstituted methyl)piperidines and piperazines
It has now been found that certain novel N-(substituted aryl)-4-(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are...
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7365070 |
Modulators of melanocortin receptor
This invention provides compounds and methods for treating melanocortin receptor associated disorders, such as weight loss disorders including cachexia resulting from cancer and other chronic...
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7365081 |
Indole derivatives and their use as medicaments
The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors
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7351719 |
Amide compounds having MCH-antagonistic activity and medicaments comprising these compounds
The present invention relates to amide compounds of general formula I
wherein the groups and residues A, B, b, W, X, Y, Z, R 1 , R 2 and R 3 have the meanings given in claim 1 . Moreover the...
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7348341 |
Chemical compounds
The invention concerns compounds of formula (I), and their use in therapy, particularly in the modulation of CCR3 activity.
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7326722 |
N-[Phenyl(piperidin-2-yl)methyl]benzamide derivatives, their preparation and their application in therapy
The present invention discloses and claims a compound of general formula (I)
wherein A, X and R 2 are as described herein. Also disclosed and claimed is application of this compound in a...
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7323478 |
Melanin concentrating hormone receptor ligands
Disclosed are compounds of the formula:
and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R 1 R 9 , and R 12 -R 19 are defined herein.
These compounds are selective...
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7319104 |
hPPARs activators
Compounds of formula (1) or a pharmaceutically acceptable salt, solvate, acid isostere, or hydrolyzable ester thereof, are disclosed. Methods of making and using the compounds are also disclosed....
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7294637 |
Method of treating addiction or dependence using a ligand for a monamine receptor or transporter
One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a...
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7259173 |
Derivatives of 3-phenyl-n-(2-(4-benzyl)-piperidin-1-yl)-ethyl)-acrylamid with ccr-3-receptor antagonistic activity for use in the treatment of inflammations and allergic conditions
This invention relates to organic compounds of formula I,
in which Ar 1 is unsubstituted phenyl substituted by one or more halogen atoms; Ar 2 is unsubstituted phenyl or phenyl substituted by...
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7256191 |
Materials and methods for the treatment of depression
The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters...
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7250412 |
PH sensitive prodrugs of 2,6-Diisopropylphenol
The present invention is directed to water-soluble derivatives of 2,6-diisopropylphenol (Propofol). The compounds act as prodrugs of 2,6-diisopropylphenol and metabolize rapidly to Propofol thereby...
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7214714 |
20-hydroxyeicosatetraenoic acid production inhibitors
A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof
[wherein R 1 represents a substituted morpholino group, a substituted...
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7208153 |
Method for the improvement of neuronal regeneration
A method for the improvement of neuronal regeneration by prevention or inhibition of basal membrane formation induced by a lesion of neuronal tissue.
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7205317 |
4[piperidin-4-yliden-(3-carbamoylpheny)methyl]benzamide derivatives and their use for the treatment of pain spinal injuries or gastrointestinal disorders
Compounds of general formula (I) wherein R 1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl and triazolyl; where each R 1 phenyl ring and R 1 ...
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RE39558 |
5-Substituted-6-cyclic-5,6,7,8-tetrahydronaphthalen 2-ol compounds which are useful for treating osteoporosis
Compounds of this formula
are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.
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7199158 |
Succinoylamino hydroxyethylamino sulfonyl urea derivatives useful as retroviral protease inhibitors
Succinoylamino hydroxyethylamino sulfonyl urea derivatives of the formula:
wherein R 1 –R 6 , R 7 , R 7′ , R 8 , R 30 –R 34 , X′, Y, Y′, t, x, and n are as defined herein, are...
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7169797 |
Protein-tyrosine phosphatase inhibitors and uses thereof
The present invention is directed to compounds of formula (I),
or a pharmaceutically suitable salt or prodrug thereof, which are useful for the selective inhibition of protein tyrosine...
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7157078 |
Devices and methods for eliminating termite colonies
This invention relates to devices, kits, and methods for eliminating termite colonies. The kits, devices, and methods employ a termiticidal bait matrix containing
a) a termiticide selected...
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7151115 |
Diphenylmethyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I:
wherein a, b, c, e, m, R 1 , R 2 , R 3 , R 4a , R 4b , R 5 , R 6 , R 7 and R 8 are as defined in the specification. The compounds of formula I...
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7148239 |
Method of enhancing cellular production of molecular chaperon, hydroxylamine derivatives useful for enhancing the chaperon production and the preparation thereof
A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed...
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7148208 |
Pharmaceutical compositions for headache, migraine, nausea and emesis
S-alkylsiothiouronium derivatives such as S-ethylisothiouronium diethylphosphate are used for the treatment of headaches, in particular, migraines, as well as for the prevention or treatment of...
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7135483 |
Substituted heterocyclic compounds for treating multidrug resistance
Substituted heterocyclinc compounds are disclosed. The compounds are useful for treating multidrug resistance. The compounds can be formulated in compositions with a carrier and, optionally, a...
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7129228 |
Heterocyclic analgesic compounds and methods of use thereof
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various...
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7129251 |
Nitrosated and nitrosylated H2 receptor antagonist compounds, compositions and methods of use
The invention describes novel nitrosated and/or nitrosylated H 2 receptor antagonist compounds, and novel compositions comprising at least one H 2 receptor antagonist compound that is optionally...
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7105544 |
Substituted alkyl amido piperidines
This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a...
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7105507 |
Cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and...
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