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US20090286831 |
VR1 Receptor Ligands and u-Opioid Receptor Ligands for the Treatment of Pain
A pharmaceutical composition comprising i) at least one composition that has affinity to the μ-opioid receptor, and at least one compound that has affinity to the VR1 receptor, or ii) at least one...
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US20090286766 |
AZOLECARBOXAMIDE DERIVATIVE
Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as...
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US20090286758 |
SUBSTITUTED N-PHENYL-5-PHENYL-PYRAZOLIN-3-YL AMIDES AS CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING OBESITY
The present invention provides novel pyrazolines that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for...
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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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US20090281084 |
PHENYL-1,2,4-OXADIAZOLONE DERIVATIVES WITH PHENYL GROUP, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS
The invention relates to phenyl-1,2,4-oxadiazolone derivatives with phenyl group and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta agonist...
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US20090281060 |
HETEROCYCLIC DERIVATIVES AS GPCR RECEPTOR AGONISTS
Compounds of Formula (I), R 1 -A-V—B—R 2 ; or pharmaceutically acceptable salts thereof, are agonists of GPR116 and are useful as regulators of satiety, e.g. for the treatment of obesity, and...
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US20090275563 |
Combination of 5-HT7 Receptor Antagonist and Serotonin Reuptake Inhibitor Therapy
Patients suffering from serotonin-mediated diseases or conditions, such as depression, may be treated by administering an effective combined amount of a 5-HT7 receptor antagonist and a serotonin...
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US20090275538 |
ARYLMETHYLIDENE HETEROCYCLES AS NOVEL ANALGESICS
The present invention relates to Arylmethylidene heterocycles, compositions comprising an Arylmethylidene heterocycle, and methods useful for treating or preventing pain comprising administering an...
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US20090270455 |
Therapeutic agent for intestinal diseases and visceral pain
The present invention relates to a therapeutic agent for irritable bowel syndrome of diarrhea type, ulcerative colitis, visceral pain or abdominal pain, which contains a compound of the following...
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US20090270454 |
Sulfonamide containing compounds for treatment of inflammatory disorders
Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of an inflammatory condition, in particular asthma. The compounds are of the general Formula I, or a...
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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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US20090264471 |
Compounds, Compositions and Methods Comprising Triazole Derivatives
The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance...
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US20090264470 |
CB1 Antagonists and Inverse Agonists
The present invention relates to methods of treating obesity, anorexia nervosa, or bulimia nervosa comprising administering a compound of the invention. The present invention further relates to the...
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US20090264469 |
NOVEL DICARBOXYLIC ACID DERIVATIVES
The present patent application concerns new compounds of formula (I): displaying agonistic activity at sphingosine-1-phosphate (S1P) receptors, their process of preparation and their use as...
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US20090264466 |
Certain Chemical Entities, Compositions and Methods
Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin...
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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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US20090263398 |
PHARMACEUTICAL COMBINATIONS
The invention provides a combination comprising an ancillary compound and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is a group R 1 -A-NR 4...
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US20090258902 |
BIPHENYL-PYRAZOLECARBOXAMIDE COMPOUNDS
The present invention relates to biphenyl-pyrazole compounds and in particular biphenyl-pyrazolecarboxamides. The invention further provides compositions comprising a compound of this invention and...
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US20090258868 |
HETEROCYCLIC ASPARTYL PROTEASE INHIBITORS
Disclosed are compounds of the formula I
or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein
W is a bond, —C(═S)—, —S(O)—, —S(O) 2...
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US20090253744 |
Acylated piperidine derivatives as melanocortin-4 receptor modulators
Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They...
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US20090253684 |
LEUKOTRIENE B4 INHIBITORS
Provided herein are compounds of the formula (I):
as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and...
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US20090253673 |
Substituted Pyrazoles as Ghrelin Receptor Antagonists
Certain novel N-acylated spiropiperidine derivatives are ligands of the human ghrelin receptor(s) and, in particular, are antagonists/inverse agonists of the human ghrelin receptor. They are...
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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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US20090247525 |
SIGMA RECEPTOR INHIBITORS
The invention relates to compounds of formula I
having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions...
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US20090247521 |
SOLUBLE EPOXIDE HYDROLASE INHIBITORS FOR THE TREATMENT OF ENDOTHELIAL DYSFUNCTION
The present invention generally relates to methods useful for a therapy using a class of urea or amide compounds and related compositions, wherein the compound is a soluble epoxide hydrolase...
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US20090247503 |
5-DEMETHOXYFUMAGILLOL AND DERIVATIVES THEREOF
Provided herein are 5-demethoxyfumagillol and its derivatives. Also provided herein are methods of making the 5-demethoxyfumagillol and derivatives. Also provided herein are biological activities...
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US20090247500 |
NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS
Disclosed herein are compounds of formula (I)
wherein R 1 , R 2 , R 3 , R 25a , R 26a , X, and n are as defined in the specification. Pharmaceutical compositions comprising such compounds, and...
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US20090239909 |
TREATMENT OF METABOLIC SYNDROME WITH LACTAMS
The present invention relates to the treatment of metabolic syndrome or disorders associated with metabolic syndrome comprising administering a compound of the invention.
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US20090239905 |
PIPERIDINES AND RELATED COMPOUNDS FOR THE TREATMENT OF DEMENTIA
Compounds of formula I: modulate the action of gamma secretase, and hence find use in treatment of Alzheimer's disease and related conditions.
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US20090239866 |
PEPTIDE DEFORMYLASE INHIBITORS
Novel PDF inhibitors and novel methods for their use are provided.
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US20090239862 |
Substituted Imidazole 4-Carboxamides as Cholecystokinin-1 Receptor Modulators
Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They...
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US20090233967 |
Crystalline forms of mc4r agonist and process for synthesis
The present invention relates to a process for producing N-{(1S)-1-[2-(1-{[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl
)pyrrolidin-3-yl]carbonyl}piperidin-4-yl)-5-chlorophenyl]eth
yl}acetamide, and...
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US20090233966 |
Analogues of the Azinomycins as Anti-Tumour Agents and as Prodrugs
Compounds of general formula (I) or a salt thereof in which R 1 is preferably an aromatic DNA binding subunit are oxidation-activated prodrugs. The compounds are expected to be converted into an...
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US20090233965 |
Alkyl Esters Of Cyclic Amino Alcohols With Muscarinic M3 Receptor Antagonist Activity, Useful For Treating E.G. Chronic Bronchial Obstruction, Asthma And Overactive Bladder
The invention provides compounds of formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 and X are as defined in the specification, a process for their preparation, pharmaceutical compositions...
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US20090221639 |
Heterocyclic GPCR Agonists
Compounds of formula (I) or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful as regulators of satiety, e.g. for the treatment of obesity, and for the treatment of...
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US20090215825 |
SUBSTITUTED PYRAZOLES, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF USE
The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for...
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US20090215822 |
Substituted Oxadiazole Derivatives as Positive Allosteric Modulators of Metabotropic Glutamate Receptors
The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q, W, R 1 and R 2 are defined in the description. Invention compounds are useful in...
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US20090215795 |
CYCLIC AMIDINE DERIVATIVES
A cyclic amidine derivative represented by the formula:
[wherein R 1 , R 2 and R 3 represent hydrogen, C 1-6 alkyl, aryl-C 1-6 alkyl, etc.; R 4 , R 5 and R 7 represent hydrogen, C 1-6 ...
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US20090215755 |
USE OF A PYRAZOLE DERIVATIVE FOR PREPARING MEDICINAL PRODUCTS THAT ARE USEFUL IN THE PREVENTION AND TREATMENT OF DYSLIPIDAEMIAS AND OF DISEASES RELATED TO DYSLIPIDAEMIAS AND/OR TO OBESITY
Use of a pyrazole-derived compound that is an antagonist for cannabinoid CB 1 receptors, alone or combined with another active principal, for preparing medicinal products that are useful in the...
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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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US20090209538 |
THERAPEUTIC SUBSTITUTED LACTAMS
Herein are described compounds having a structure
or a pharmaceutically acceptable salt thereof, wherein Y, A, and B are as described. Methods, compositions, and medicaments related thereto are...
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US20090203737 |
Pyrrole Derivatives as Positive Allosteric Modulators of Metabotropic Receptors
The present invention relates to new compounds which are Pyrrole derivatives of formula (I) wherein A, B, P, Q 5 W, R 1 and R 2 are defined in the description. Invention compounds are useful in...
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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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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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US20090203694 |
INHIBITORS OF UNDECAPRENYL PYROPHOSPHATE SYNTHASE
The present invention relates to compounds that are selective and/or potent inhibitors of UPPS. In addition to compounds which inhibit UPPS, the invention also provides pharmaceutical compositions...
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US20090203669 |
COMPOSITIONS AND METHODS FOR THE TREATMENT OF ADDICTION AND OTHER NEUROPSYCHIATRIC DISORDERS
The present invention is based, in part, on our discovery that certain types of therapeutic agents can be used in combination to treat a variety of neuropsychiatric and related disorders, including...
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US20090203523 |
Fungicidal Mixtures Made From 1-Methylpyrazol-4-Ylcarboxanilides
Fungicidal mixtures, comprising as active components
1) at least one 1-methylpyrazol-4-ylcarboxanilide I
in which X═O or S, R 1 ═C 1 -C 4 -alkyl or C 1 -C 4 -haloalkyl and R 2 ═H...
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US20090197917 |
USE OF RIMONABANT FOR THE PREPARATION OF MEDICAMENTS USEFUL IN THE PREVENTION AND TREATMENT OF TYPE 2 DIABETES
The invention relates to the use of rimonabant, either alone or combined with another active ingredient, for the preparation of medicaments useful in the prevention and treatment of type 2 diabetes...
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US20090197884 |
Compounds Useful as Antagonists of CCR2
The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the...
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US20090186895 |
ETHERS, SECONDARY AMINES AND DERIVATIVES THEREOF AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical...
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