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66 results about "Melanin-concentrating hormone receptor" patented technology
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Two Melanin-concentrating hormone receptors (MCHR) have recently been characterized: MCH-R1 and MCH-R2. These two receptors share approximately 38% homology.
4-Aminoquinoline compounds
The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.
Owner:DEVITA ROBERT J +5
2-Aminoquinoline compounds
The present invention is concerned with compounds of the general Formula I: and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.
Owner:MERCK SHARP & DOHME CORP
2-Aminoquinoline compounds
The present invention is concerned with compounds of the general Formula I:and pharmaceutically acceptable salts thereof, which are useful as melanin concentrating hormone receptor antagonists, particularly MCH-1R antagonists. As such, compounds of the present invention are useful for the treatment or prevention of obesity or eating disorders associated with excessive food intake and complications thereof, osteoarthritis, certain cancers, AIDS wasting, cachexia, frailty (particularly in elderly), mental disorders stress, cognitive disorders, sexual function, reproductive function, kidney function, locomotor disorders, attention deficit disorder (ADD), substance abuse disorders and dyskinesias, Huntington's disease, epilepsy, memory function, and spinal muscular atrophy. Compounds of formula I may therefore be used in the treatment of these conditions, and in the manufacture of a medicament useful in treating these conditions. Pharmaceutical formulations comprising one of the compounds of formula (I) as an active ingredient are disclosed, as are processes for preparing these compounds.
Owner:MERCK SHARP & DOHME CORP
Non-basic melanin concentrating hormone receptor-1 antagonists and methods
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula IwhereinR1, R2, R3, R8, and R9 are defined herein.Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
Owner:BRISTOL MYERS SQUIBB CO
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water / electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.
Owner:ABBOTT LAB INC
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
The present invention is directed to compounds of formula (I), which antagonize of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water / electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.
Owner:ABBOTT LAB INC
Non-basic melanin concentrating hormone receptor-1 antagonists
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula Iwhere R1, R1a, R1b, A, R3, R4, R5, R5b and R6 are as defined herein.
Owner:BRISTOL MYERS SQUIBB CO
Melanin concentrating hormone receptor antagonists
Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I wherein W, X, Y, Z, R3-R6, and R11 are as defined in the specification, are provided. Also provided are methods of treating or preventing a melanin concentrating hormone-mediated disorder in a subject, comprising administering to a subject in need of such treatment or prevention a compound of Formula I.
Owner:AMGEN INC
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water / electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.
Owner:ABBVIE INC
Non-basic melanin concentrating hormone receptor-1 antagonists and methods
Owner:BRISTOL MYERS SQUIBB CO
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water / electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.
Owner:ABBOTT LAB INC
Piperazinone-substituted tetrahydro-carboline MCH-1 antagonists, methods of making, and uses thereof
InactiveUS8697700B2High affinityHigh indexNervous disorderOrganic chemistryMelanin-concentrating hormoneCombinatorial chemistry
The present invention relates to piperazinone-substituted tetrahydrocarboline derivatives of formula (I):having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.
Owner:ALBANY MOLECULAR RESEARCH INC
Pyrimidinones as melanin concentrating hormone receptor 1
Owner:SMITHKLINE BECKMAN CORP
Azolotriazinone melanin concentrating hormone receptor-1 antagonists
The present application provides compounds that are useful as MCHR1 antagonists, especially for the treatment of obesity, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula Iwherein the variables are defined herein.
Owner:BRISTOL MYERS SQUIBB CO
2-Aminoquinoline derivatives
InactiveUS20060287340A1Potent MCH-1R antagonistic activityExcel in oral absorptionBiocideOrganic active ingredientsAlkoxy groupAntagonist
This invention provides 2-aminoquinoline derivatives represented by a general formula [I][in which R1 and R2 either stand for lower alkyl, lower cycloalkyl, etc., or R1 and R2 together form an aliphatic nitrogen-containing heterocycle with the nitrogen atom to which they bind; R3, R4, R5, R6 and R7 stand for hydrogen, lower alkyl, etc.; R8 stands for lower alkyl, lower alkyloxy, etc.; and n stands for an integer of 0-4]. The compounds act as melanin concentrating hormone receptor antagonist, and are useful as medicines for central nervous system disorders, cardiovascular disorders and metabolic disorders.
Owner:MSD KK
Melanin concentrating hormone receptor-1 antagonists
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula Iwherein R1a, R1b, R1c, Q, A, R3, W, D and R2 are defined herein.Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
Owner:BRISTOL MYERS SQUIBB CO
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water / electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.
Owner:ABBVIE INC
Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient
The invention provides melanin-concentrating hormone receptor antagonists containing as the active ingredient piperidine derivatives represented by the general formula [I]: [wherein R1 is hydrogen, hydroxyl, lower alkyl, or the like; R2, R3a, R3b, R4a, R4b, R5a, R5b and R6 each stands for hydrogen, halogen, or the like; W1 and W2 each independently stands for —O—, —CH2—, or the like; Y1, Y2, Y3 and Y4 stand for —CH—, —CF—, —N—, or the like; Z stands for lower alkyl, an aliphatic heterocyclic group, or the like; Ar is a mono- or bi-cyclic aliphatic heterocycle or an aromatic heterocycle; and n is an integer of 1 to 8]. The compounds act as antagonist against melanin-concentrating hormone receptor and are useful as drugs for central diseases, circulatory diseases, or metabolic diseases.
Owner:MSD KK
Melanin concentrating hormone receptor-1 antagonists
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1a, R1b, R1c, Q, A, R3, W, D and R2 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.
Owner:BRISTOL MYERS SQUIBB CO
Antagonists of melanin concentrating hormone receptor
This invention provides compounds that are antagonists of melanin concentrating hormone receptor-1 (MCH-R1). The compounds are represented by formula I: where m is zero or one, n is zero to two, Y is oxygen or —N(R9)—, R1, R2, R3, R4, R5, R9 and Ring A are defined in the specification. Coumarin and quinolone compounds where R1 and R2 together form a fused benzo ring are preferred. The invention also provides compounds of formula VI where the coumarin moiety is replaced by a quinazolinone ring. The compounds are useful for treating MCH-R1-related disorders, particularly overweight conditions including obesity.
Owner:ABBVIE INC
Non-basic melanin concentrating hormone receptor-1 antagonists
Owner:BRISTOL MYERS SQUIBB CO
Methods of identifying melanin concentrating hormone receptor antagonists
InactiveUS7393655B2High activityReduce exceptionOrganic active ingredientsFungiNucleic Acid ProbesDna encoding
This invention provides an isolated nucleic acid encoding a human MCH1 receptor, a purified human MCH1 receptor, vectors comprising isolated nucleic acid encoding a human MCH1 receptor, cells comprising such vectors, antibodies directed to a human MCH1 receptor, nucleic acid probes useful for detecting nucleic acid encoding human MCH1 receptors, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding human MCH1 receptors, transgenic, nonhuman animals which express DNA encoding a normal or mutant human MCH1 receptor, methods of isolating a human MCH1 receptor, methods of treating an abnormality that is linked to the activity of a human MCH1 receptor, as well as methods of determining binding of compounds to mammalian MCH1 receptors.
Owner:H LUNDBECK AS
Hydroxy substituted thieno pyrimidinones as melanin concentrating hormone receptor-1 antagonists
Owner:BRISTOL MYERS SQUIBB CO
Spirodiamine-diaryl ketoxime derivative
[Problem] To provide a melanin concentrating hormone receptor antagonist useful as medicines for central system disorders, cardiovascular disorders, metabolic disorders.[Means for Resolution] Provided are compound of a formula (I):[wherein R1 a and R1 b each are a hydrogen atom, etc.; R2 is a hydrogen atom, a C1-6 alkyl, etc.; Ar1 is a 6-membered aromatic carbocyclic group or a 6-membered aromatic nitrogen-containing heterocyclic group; Ar2 is a group to be formed by removing two hydrogen atoms from a 6-membered aromatic carbon ring, a 6-membered aromatic nitrogen-containing hetero ring, etc.; Ar3 is a mono- or bi-cyclic aromatic carbon ring or aromatic hetero ring; m1, m2, m3 and m4 each are independently 0, 1, 2, 3 or 4, provided that the total of m1 and m2 is from 2 to 6, the total of m3 and m4 is from 2 to 6]. The compounds are useful as medicines for central system disorders, cardiovascular disorders, metabolic disorders.
Owner:MSD KK
Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water / electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders.
Owner:ABBVIE INC
Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient
The invention provides melanin-concentrating hormone receptor antagonists containing as the active ingredient piperidine derivatives represented by the general formula [I]:[wherein R1 is hydrogen, hydroxyl, lower alkyl, or the like; R2, R3a, R3b, R4a, R4b, R5a, R5b and R6 each stands for hydrogen, halogen, or the like; W1 and W2 each independently stands for —O—, —CH2—, or the like; Y1, Y2, Y3 and Y4 stand for —CH—, —CF—, —N—, or the like; Z stands for lower alkyl, an aliphatic heterocyclic group, or the like; Ar is a mono- or bi-cyclic aliphatic heterocycle or an aromatic heterocycle; and n is an integer of 1 to 8]. The compounds act as antagonist against melanin-concentrating hormone receptor and are useful as drugs for central diseases, circulatory diseases, or metabolic diseases.
Owner:MSD KK
Pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists
Owner:BRISTOL MYERS SQUIBB CO
Heterocyclic mchr1 antagoists
InactiveUS20060194871A1BiocideNervous disorderCombinatorial chemistryMelanin-concentrating hormone receptor
This invention relates to novel heterocycles which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), also referred to as 11 CBy, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in medicines. Compounds of the invention have the formula:
Owner:SMITHKLINE BECKMAN CORP
Human MCHR1 epitope domain gene expression-associated protein MCHR1-C and encoding gene thereof
ActiveCN101955528ACell receptors/surface-antigens/surface-determinantsMicrobiological testing/measurementEpitopeAutoantibody production
The invention provides a human melanin concentrating hormone receptor-1 (MCHR1) epitope domain gene expression-associated protein MCHR1-C, an encoding gene and a recombinant vector thereof and an application of the polypeptide in identifying antoantibody in serum of a vitiligo patient. The human MCHR1 epitope domain gene expression-associated protein MCHR1-C of the invention has an amino acid sequence shown in SEQ ID No:1. The human MCHR1 epitope domain gene expression-associated protein MCHR1-C of the invention has the beneficial effects that an polypeptide capable of effectively identifying the antoantibody in the serum of the vitiligo patient is provided; and the application of the human MCHR1 epitope domain gene expression-associated protein and the polypeptide in detecting MCHR1 antibody of pigmentary dermatosis, in particular the autoantibody in the serum of the vitiligo patient, thereby laying foundation for further new drug screening.
Owner:许爱娥 +1
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