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259 results about "Muscarinics" patented technology
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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—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
Owner:PHARMACOPEIA DRUG DISCOVERY +1
Aspartyl protease inhibitors
Disclosed are compounds of formula I
or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification.
Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
Owner:MERCK SHARP & DOHME LLC
Biphenyl compounds useful as muscarinic receptor antagonists
ActiveUS7288657B2Long duration of actionImprove performanceNervous disorderOrganic chemistryDiseaseCombinatorial chemistry
This invention provides compounds of formula I:wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Owner:THERAVANCE BIOPHARMA R&D IP LLC
Combinations comprising antimuscarinic agents and beta-adrenergic agonists
Combinations comprising (a) a β2 agonist and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for the treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary disease.
Owner:GRAS ESCARDO JORDI +3
M3 muscarinic acetylchoine receptor antagonists
Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.
Owner:GLAXO GRP LTD
Biphenyl compounds useful as muscarinic receptor antagonists
ActiveUS20050203132A1Improve performanceReduce systemic side effectsBiocideOrganic chemistryBiphenyl compoundCombinatorial chemistry
This invention provides compounds of formula I:
wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, and W are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Owner:THERAVANCE BIOPHARMA R&D IP LLC
Benzimidazolidinone derivatives as muscarinic agents
InactiveUS7087593B2Increase acetylcholine signaling and effectHigh selectivityBiocideSenses disorderReceptor subtypeMuscarinic Agents
Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and / or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.
Owner:ACADIA PHARMA INC
Biphenyl compounds useful as muscarinic receptor antagonists
ActiveUS7569588B2Long duration of actionImprove performanceBiocideOrganic chemistryStereochemistryBiphenyl compound
This invention provides compounds of formula I:wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
Owner:THERAVANCE BIOPHARMA R&D IP LLC
Modulators of muscarinic receptors
The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
Owner:VERTEX PHARMA INC
Muscarinic acetylchoine receptor antagonists
Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.
Owner:GLAXO GROUP LTD
Ester derivatives
This invention relates to compounds which exhibit selective muscarinic M3 receptor antagonism, have little side effects, are suitable for inhalation therapy and are useful as treating agents of respiratory system diseases, of the general formula (I);
- [in which A signifies a group expressed by a formula (a0) or (b0);
Ar signifies optionally substituted aryl or heteroaryl; B1 and B2 signify aliphatic hydrocarbon; R1 signifies fluorine-substituted cycloalkyl; R2, R3 and R4 signify lower alkyl, single bond or alkylene bonded to B1, or R2 and R3 are united to signify alkylene; R5 and R7 signify hydrogen, lower alkyl, or a single bond or alkylene bonded to B2; R6 signifies hydrogen, lower alkyl or a group expressed as —N(R8)R9; and X− signifies an anion].
Owner:MSD KK
M3 muscarinic acetylchoine receptor antagonists
Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.
Owner:GLAXO GROUP LTD
Combinations comprising antimuscarinic agents and beta-adrenergic agonists
Combinations comprising (a) a β2 agonist and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for the treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary disease.
Owner:ALMIRALL
RNA interference mediated inhibition of cholinergic muscarinic receptor (CHRM3) gene expression using short interfering nucleic acid (siNA)
InactiveUS20050176664A1Improve bioavailabilityMinimize the possibilityCompounds screening/testingNervous disorderMuscarinic receptor siteCholinergic receptor muscarinic 3
This invention relates to compounds, compositions, and methods useful for modulating cholinergic muscarinic receptor gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of cholinergic muscarinic receptor gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of cholinergic muscarinic receptor genes, such as M3 muscarinic acetylcholine receptor or cholinergic receptor muscarinic 3 (CHRM3).
Owner:SIRNA THERAPEUTICS INC
Modulators of muscarinic receptors
The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
Owner:VERTEX PHARMA INC
Tetrahydroquinoline analogues as muscarinic agonists
InactiveUS20050209226A1Increased intraocular pressureSenses disorderNervous disorderTreatment useMuscarinics
The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.
Owner:ACADIA PHARMA INC
Muscarinic agonists
Compounds and methods are provided for the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4, or both m1 and m4, receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.
Owner:ACADIA PHARMA INC
Pharmaceutical combinations
Pharmaceutical combinations comprising a beta-3 adrenergic receptor agonist and a muscarinic receptor antagonist, and methods for their use are disclosed. Disclosed combinations include solabegron and oxybutynin. Methods of using the pharmaceutical combinations for the treatment of one or more symptoms associated with overactive bladder, for example, frequency of urgency, nocturia, and urinary incontinence, are also disclosed.
Owner:B3AR THERAPEUTICS INC
Method and system for the treatment of chronic obstructive pulmonary disease with nebulized anticholinergic administrations
Inhalation solutions for administration of muscarinic antagonists for the treatment of breathing disorders, such as COPD, are provided.Owner:SUNOVION RESPIRATORY DEV
Quaternary ammonium salt compounds
InactiveUS20120046467A1High activityLower Level RequirementsBiocideOrganic chemistryAdrenergicAdrenergic receptor agonists
[Problem]The object of the present invention is to provide a novel compound having 132 adrenergic receptor agonist activity and muscarinic receptor antagonist activity.[Means for Solving the Problem]The present invention is a quaternary ammonium salt compounds represented by formula (I), or a pharmaceutically acceptable salt thereof, with superior β32 adrenergic receptor agonist activity and muscarinic receptor antagonist activity.
Owner:TEIJIN PHARMA CO LTD
Thienopyridines as allosteric potentiators of the m4 muscarinic receptor
The present invention relates to selective allosteric potentiators of the Formula (I):
or pharmaceutically acceptable salts thereof, for the treatment of disorders associated with M4 muscarinic receptors.
Owner:ELI LILLY & CO
Pharmaceutical combinations of beta-3 adrenergic receptor agonists and muscarinic receptor antagonists
ActiveUS8642661B2BiocidePeptide/protein ingredientsHyperactivity bladderAdrenergic receptor agonists
Pharmaceutical combinations comprising a beta-3 adrenergic receptor agonist and a muscarinic receptor antagonist, and methods for their use are disclosed. Disclosed combinations include solabegron and oxybutynin. Methods of using the pharmaceutical combinations for the treatment of one or more symptoms associated with overactive bladder, for example, frequency of urgency, nocturia, and urinary incontinence, are also disclosed.
Owner:B3AR THERAPEUTICS INC
Dual Pharmacophores - PDE4-Muscarinic Antagonistics
InactiveUS20090203657A1Efficient deliveryGreat potentialBiocideOrganic chemistryMuscarinic antagonistDrug
The present invention is directed to novel compounds of Formula (I) and pharmaceutically acceptable salts thereof,
- pharmaceutical compositions and their use as dual chromaphores having inhibitory activity against PDE4 and muscarinic acetylcholine receptors (mAChRs), and thus being useful for treating respiratory diseases.
Owner:GLAXO GROUP LTD
Prodrugs of muscarinic agonists and methods of treatment of neuropsychiatric disorders
Compounds are described that are prodrugs to active compounds that modulate a muscarinic receptor. In some cases, the compounds are prodrugs to N-desmethylclozapine. The compounds may be used to treat neuropsychiatric disorders.
Owner:ACADIA PHARMA INC
Preparation method and application of glycopyrronium bromide chiral antipode
The invention belongs to the technical field of medicine, and discloses a preparation method of (3S,2'S), (3S,2'R), (3R,2'R) and (3R,2'S) four type chiral monomers of muscarine receptor antagonist racemic medicine glycopyrronium bromide. The method comprises the following steps: resolving racemic alpha-cyclopentylmandelic acid by a chemical resolution method by using L-Tyrosine methyl ester and (R)-alpha-phenylethylamine as resolution reagents to respectively prepare (S)-alpha-cyclopentylmandelic acid and (R)-alpha-cyclopentylmandelic acid; and carrying out esterification reaction to respectively obtain chiral intermediates (S)/(R)-alpha-cyclopentylmethyl mandelate. L/D-malic acid used as the raw material is subjected to four reaction steps, including condensation, carbonyl reduction, catalytic hydrogenation or transfer hydrogenation reduction debenzylation, and reduction alkylation or alkylogen alkylation, in a chiral synthesis mode to obtain another important chiral intermediate (S)/(R)-N-methyl-3-hydroxypyrrolidine. The chiral intermediate is subjected to ester exchange and quaterisation to respectively obtain the four (3S,2'S), (3S,2'R), (3R,2'R) and (3R,2'S) type glycopyrronium bromide chiral monomers. The result indicates that the (3R,2'S)-glycopyrronium bromide has the strongest cholinergic antagonistic action.
Owner:SHENYANG PHARMA UNIVERSITY +1
Piperidin-1-yl and azepin-1-yl carboxylates as muscarinic M4 receptor agonists
The present invention provides muscarinic M4 receptor agonists of formula (I) and pharmaceutically acceptable salts thereof, wherein m, n, p, q, R, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases such as schizophrenia, Alzheimer's disease and various cognitive disorders as well as in the treatment or alleviation of pain.
Owner:HEPTARES THERAPEUTICS
Modulators of muscarinic receptors
The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
Owner:VERTEX PHARMA INC
Aza-bridged-ring compound
[Problems] Provided is a compound which has an antagonistic action on a muscarinic M3 receptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.
[Means for Solving Problems] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic M3 receptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic M3 receptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic M3 receptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.
Owner:ASTELLAS PHARMA INC
Muscarinic receptor agonists
This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where m, p, q, W, Z, Y, X1, X2, R1, R2 R3 and R4 are as defined herein.
Owner:HEPTARES THERAPEUTICS
Heterocyclic aspartyl protease inhibitors
Disclosed are compounds of the formula Ior a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, whereinW is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—;X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—;U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond;and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
Owner:PHARMACOPEIA INC +1
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