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US20100004228 |
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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US20100004241 |
NON-IMIDAZOLE ARYLOXYALKYLAMINES
Substituted aryloxyalkylamines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
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US20090325980 |
PIPERIDINE OR PIPERAZINE SUBSTITUTED TETRAHYDRO-NAPHTHALENE-1-CARBOXYLIC ACID MTP INHIBITING COMPOUNDS
The present invention is concerned with novel piperidine or piperazine substituted tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant...
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US20090318467 |
NOVEL HETEROARYL CARBOXAMIDE DERIVATIVES
The invention is concerned with novel heteroaryl carboxamide derivatives of formula (I),
wherein
m, X, Y, R 1 , R 2 , R 3 and R 4 are as defined in the description and in the claims, as well...
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US20090318498 |
PIPERIDYL ACRYLAMIDE ANTAGONISTS OF CCR2
The present invention comprises compounds of Formula I.
wherein: R 1 , R 2 , R 3 , R 4 , R 5 and X are as defined in the specification. The invention also comprises a method of treating or...
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US20090306136 |
Benzenesulfonamide Compounds and the Use Thereof
The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R 1 -R...
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US20090306134 |
Muscarinic receptor antagonists
Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more...
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US20090306059 |
CYCLIC AMINE DERIVATIVE HAVING SUBSTITUTED ALKYL GROUP
A compound having the general formula (I), pharmacologically acceptable salts thereof or prodrugs thereof:
[wherein R 1 represents a hydrogen atom, a C1-C6 alkyl group which may be substituted,...
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US20090306070 |
TETRA-O-SUBSTITUTED BUTANE-BRIDGE MODIFIED NDGA DERIVATIVES, THEIR SYNTHESIS AND PHARMACEUTICAL USE
The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified...
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US20090286830 |
HETEROATOM-LINKED SUBSTITUTED PIPERIDINES AND DERIVATIVES THEREOF USEFUL AS HISTAMINE H3 ANTAGONISTS
Disclosed are novel compounds of the formula
or a pharmaceutically acceptable salt thereof, wherein:
M 1 and M 3 are CH or N; M 2 is CH, CF or N; Y is —C(═O)—, —C(═S)—,...
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US20090281097 |
NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
The object of the present invention is to provide a compound having an ACC inhibitory action, which is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia,...
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US20090281116 |
PYRROLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
The invention relates to compounds having the formula (I):
Wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 9 and A-R 9 are as defined herein. Also disclosed are the preparative methods...
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US20090275581 |
RENIN INHIBITORS
Disclosed are compounds according to Formula I:
wherein the variables are defined herein. Such compounds are can bind aspartic proteases to inhibit their activity. They are useful in the...
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US20090275556 |
Aryl sulfonamides useful as inhibitors of chemokine receptor activity
The present invention provides compounds of general formula I:
or a pharmaceutically acceptable salt thereof, wherein R 1 , X, Z, R 2 , X 1 , Ar, n, R 3 and R 4 are defined generally and in...
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US20090275609 |
Carboxamide Compounds and Methods for Using The Same
Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure
in which R 1 , R 2 , R 3 , R 4 , D, J, Z, T, p,...
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US20090275613 |
INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
The present invention discloses novel compounds of Formula I: (I) possessing 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the...
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US20090270451 |
Piperdine Glycine Transporter Inhibitors
The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with...
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US20090270367 |
SUBSTITUTED HYDROXYETHYLAMINE ASPARTYL PROTEASE INHIBITORS
The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a...
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US20090270372 |
NOVEL DERIVATIVES OF BENZIMIDAZOLE AND IMIDAZO-PYRIDINE AND THEIR USE AS MEDICAMENTS
A subject of the present Application is novel derivatives of benzimidazole and imidazopyridine which have a good affinity for certain sub-types of melanocortin receptors, in particular the MC4...
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US20090264418 |
5-AMIDO-INDOLE-2-CARBOXAMIDE DERIVATIVES
The present invention relates to compounds of formula I
wherein G and R 1 to R 5 and R 12 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The...
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US20090264407 |
Substituted Sulfonamide Compounds
Substituted sulfonamide compounds corresponding to formula I:
a process for their preparation, pharmaceutical compositions comprising such compounds, and the use of such substituted sulfonamide...
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US20090264400 |
Substituted Sulfonamide Compounds
Substituted sulfonamide compounds corresponding to formula I:
processes for the preparation thereof, pharmaceutical compositions containing these compounds, and the use of such substituted...
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US20090253656 |
BCRP/ABCG2 INHIBITOR
The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative represented by...
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US20090253709 |
SYNTHESIS, TELOMERASE INHIBITION AND CYTOTOXIC STUDIES ON 2,7-DISUBSTITUTED ANTHRAQUINONE DERIVATIVES
An series of 2,7-disubstituted anthraquinone derivatives including a formula I are provided.
R is a first substituted group selected from a group consisting of a hydrogen, an amino group, a...
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US20090247509 |
Novel Heterocyclic Substituted Carbonyl Derivatives and Their Use as Dopamine D3 Receptor Ligands
The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D 3 receptors. In another aspect, the invention relates to a method for treating...
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US20090226379 |
BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
This invention provides compounds of formula I:
wherein a, b, c, d, m, n, p, s, t, W, Ar 1 , R 1 , R 2 , R 3 , R 4 , R 6 , R 7 , and R 8 are as defined in the specification. The compounds of...
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US20090209582 |
Benzimidazole-carboxamide compounds as 5-ht4 receptor agonists
The invention relates to benzimidazole-carboxamide 5-HT 4 receptor agonist compounds of formula (I)
wherein R 1 and X are as defined in the specification, or a pharmaceutically acceptable salt...
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US20090209578 |
CHEMICAL COMPOUNDS
The present invention provides compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 , Het and m are as defined in the description. The compounds of the present invention are modulators,...
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US20090203710 |
Novel piperidine derivative
Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty...
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US20090203696 |
Aryl- and Heteroaryl-Ethyl-Acylguanidine Derivatives, Their Preparation and Their Application in Therapeutics
Disclosed are compounds according to formula (I):
wherein A, Q, X, Y, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined herein. The disclosure also relates to pharmaceutical...
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US20090203736 |
PIPERIDINE SULPHONAMIDE DERIVATIVES
The present invention relates to piperidine sulphonamide derivatives of formula
wherein Ar 1 , Ar 2 , R 1 , R 2 , m and n are as defined in the description and claims, or pharmaceutically...
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US20090192139 |
CGRP RECEPTOR ANTAGONISTS
The present invention is directed to compounds of Formula I:
and Formula II:
(where variables R 1 , R 2 , R 3 , R 4 , A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as...
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US20090186894 |
N-Substituted-Heterocycloalkyloxybenzamide Compounds and Methods of Use
The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having...
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US20090186874 |
Carboxamide derivative and use thereof
The present invention relates to a compound represented by the formula
wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B and ring C are each an...
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US20090170829 |
Carboxamide, Sulfonamide and Amine Compounds and Methods for Using The Same
Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure
in which R 1 , R 2 , R 4...
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US20090163544 |
Use of NK-3 Receptor Antagonists for the Treatment of Nausea and Vomiting
This invention relates to the treatment or prevention of nausea and/or vomiting by the administration of a NK-3 receptor antagonist.
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US20090156572 |
Nitrogen-containing heterocyclic compound and use thereof
The present invention relates to a compound represented by the formula
wherein ring A is a nitrogen-containing heterocycle optionally further having substituent(s), ring B is an aromatic ring...
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US20090156638 |
Uses of nordihydroguaiaretic acid (NDGA) and derivatives thereof in preventing transmission of sexually transmitted diseases
Provided herein are methods for inhibiting proliferation of a microbe associated with a sexually transmitted disease (STD) or infection and for preventing transmission of one or more sexually...
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US20090143372 |
CHEMICAL COMPOUNDS
The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I:
where R1, R2, R3, U and V are defined below and to...
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US20090137576 |
Novel Piperidine Derivative
Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly...
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US20090118267 |
INDANES
Compounds of the formula (I), in which R 1 , R 2 , R 3 , R 4 , and q have the meanings indicated in claim 1 , can be employed, inter alia, for the treatment of tumours.
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US20090111808 |
NOVEL HISTAMINE H3-RECEPTOR LIGANDS AND THEIR THERAPEUTIC APPLICATIONS
The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated...
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US20090111809 |
INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
The present invention discloses novel compounds of Formula I: (I) having 11-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention...
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US20090099182 |
INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
The present invention discloses novel compounds of Formula I:
having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention...
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US20090088430 |
PIERIDINYL SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
The present invention discloses novel compounds of Formula I:
having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention...
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US20090076078 |
New compounds 966
Compounds of Formula I, or pharmaceutically acceptable salts thereof:
wherein R 2 , R 3 , X, m and n are as defined in the specification as well as salts and pharmaceutical compositions...
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US20090076026 |
BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
The invention provides compounds of formula I:
wherein a, b, c, d, f, W, Q, Y, R 1 , R 2 , and R 3 are as defined in the specification. The compounds of formula I are muscarinic receptor...
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US20090062260 |
COMPOUNDS AND COMPOSITIONS AS LXR MODULATORS
The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of...
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US20090054451 |
Use of Piperidine Derivatives as Agonists of Chemokine Receptor Activity
The present invention is directed to novel piperidine derivatives and to the use of piperidine derivatives of formula I
as agonists of chemokine receptor activity.
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US20090048228 |
Heterocycle Derivatives As Histone Deacetylase (Hdac) Inhibitors
The present invention relates to compounds of formula I:
or pharmaceutically acceptable salts or tautomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the...
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