|| List of recent Antagonist-related patents
| Compositions for use in treating or diagnosing bone disorders and/or cardiovascular disorders|
Compositions of an inhibitor of a polynucleotide for use in treating or preventing bone disorders such as osteoporosis, osteopenia, bone fracture, bone cancer, as well as impaired bone homeostasis. Preferred compounds to be used in these medical interventions are antagonistic compounds, like nucleic acid molecules, directed against mir-31 and derivatives thereof.
Universitat Fur Bodenkultur Wien
| Use of ghrelin receptor inverse agonists or antagonists for treating sleep disorders|
The present invention relates to methods of treating sleep disorders in patients comprising administration of a ghrelin receptor inverse agonist or antagonist. The invention also includes methods of treating sleep disorders comprising the administration of a pharmaceutical composition comprising a ghrelin receptor inverse agonist or antagonist and at least one pharmaceutically acceptable carrier, diluent, or excipient..
| Therapy of tumors and infectious agents deficient in methylthioadenosine phosphorylase|
Methods for treating diseases in humans and vertebrate animals are provided using competitive antagonists of cellular metabolites combined with a protective agent for protecting host cells from toxic effects of the drugs. Also provided are kits comprising competitive antagonists and suitable protective agents.
| Modulation of angiotensin ii receptors for the prevention and treatment of malaria cerebral|
The present invention is directed to a composition for the treatment or prevention of cerebral malaria that comprises an angiotensin receptor type-2 agonist and an antimalaria drug. The present invention is further directed to methods for treating and preventing cerebral malaria that involve administering an angiotensin receptor type-2 agonist and/or an angiotensin receptor type-1 antagonist..
New York University
| Drug screening platform for rett syndrome|
The invention provides a method for restoring a neural cell having a deficiency or alteration in glutamatergic pathway affecting neuron and/or glial function comprising contacting the cell with a nmda receptor antagonist(s) and/or modulator(s) of a glutamatergic pathway, thereby restoring the neural cell having a deficiency or alteration in glutamatergic pathways affecting neuron and/or glial function.. .
The Regents Of The University Of California
| Lingo-2 antagonists for treatment of conditions involving motor neurons|
The invention provides methods of treating diseases, disorders or injuries involving motor neuron survival and axonal growth, including amylotrophic lateral sclerosis, by the administration of a lingo-2 antagonist. An exemplary method for promoting survival of a motor neuron, comprising contacting said motor neuron with an effective amount of a composition comprising a lingo-2 antagonist selected from the group consisting of: (i) a soluble lingo-2 polypeptide; (ii) a lingo-2 antibody or antigen-binding fragment thereof; (iii) a lingo-2 antagonist polynucleotide; (iv) a lingo-2 aptamer; and (v) a combination of two or more of said lingo-2 antagonists..
Biogen Idec Ma Inc.
| Therapeutic combination and methods of treatment with a dll4 antagonist and an anti-hypertensive agent|
Methods for treating cancer comprising administering a dll4 antagonist and one or more anti-hypertensive agents are described. Also described are pharmaceutical compositions comprising a dll4 antagonist and one or more anti-hypertensive agents, and kits comprising the same..
Oncomed Pharmaceuticals, Inc.
|Process for making cgrp receptor antagonists|
The disclosure encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, having less steps and improved yields as compared to previous synthetic methods for making these compounds, which are cgrp receptor antagonists, useful for the treatment of migraine. Conditions for an amide bond formation between an acid and amine include for example reacting the compounds of formulae b (after salt break) and c with an amide coupling reagent and optionally an additive and an acid and/or a base in a non-reactive solvent..
Merck Sharp & Dohme
|Selective ep4 receptor antagonistic substance for treatment of cancer|
This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin e2 receptor (ep4 receptor) and is represented by the following general formula (i), (ii), (iii), or (iv), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer.
Raqualia Pharma Inc.
|Spirolactam cgrp receptor antagonists|
The present invention is directed to spirolactam analogues which are antagonists of cgrp receptors and useful in the treatment or prevention of diseases in which cgrp is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which cgrp is involved..
Merck Sharp & Dohme Corp.
Methods of diagnosing, preventing, and treating bone mass diseases
The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are tph1 inhibitors or serotonin receptor antagonists..
Substituted triazolo-pyridazine derivatives
This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an α1-gaba-a receptor antagonist and/or a α2, α3 and α5 gaba-a receptor agonist..
Concert Pharmaceuticals Inc.
Benzo[1,3]dioxine derivatives and their use as lpar5 antagonists
The present invention relates to compounds of the formula (i), wherein the residues a, r1 to r5, z1 and z2 have the meanings indicated in the claims. The compounds of the formula (i) are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses.
Dipeptide mimetics of ngf and bdnf neurotrophins
The invention relates to compounds having either agonist or antagonist activities for the neurotrophins ngf and bdnf and represented by monomeric or dimeric substituted dipeptides that are analogs of the exposed portions of loop 1 or loop 4 regions of these neurotrophins near or at a beta-turn of the respective loop. N-acylated substituents of these dipeptides are biostereoisomers of the amino acid residues preceding these dipeptide sequences in the neurotrophin primary structure.
Uchrezhdenie Rossiiskoi Akademii Meditsynskikh Nauk Nauchno-issledovatelsky Institut Farmakologii
Opioid agonist formulations with releasable and sequestered antagonist
Disclosed are oral dosage forms, comprising (i) a therapeutically effective amount of an opioid agonist; (ii) an opioid antagonist in releasable form; and (iii) a sequestered opioid antagonist which is not released when the dosage form is administered intact, and methods thereof.. .
Purdue Pharma L.p.
Cns stimulant and opioid receptor antagonist combination as a non-addictive, non-aversive and synergistic anti-obesity treatment
Combinations comprise a therapeutically effective amount of one or more stimulants and and/or pharmaceutically acceptable analogs, salts, or hydrates of the one or more stimulants, and one or more non-selective opioid receptor antagonists, and/or pharmaceutically acceptable analogs, salts or hydrates of the one or more non-selective opioid receptor antagonists. These combinations may be used for treating obesity via administration to a subject having a need thereof..
The General Hospital Corporation
E-selectin antagonist compounds, compositions, and methods of use
Methods and compositions using e-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of e-selectin to an e-selectin ligand. Described herein are e-selectin antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation..
Polypeptide specifically binding to vegf-c and use thereof
A polypeptide, antagonist, and antibody that specifically bind to and inhibit vegf-c and uses thereof in a method of inhibiting angiogenesis and a method of preventing, treating, and/or diagnosing a disease associated with activation and/or overexpression of vegf-c, using the antibody, and a method of detecting the presence of vegf-c in a sample.. .
Samsung Electronics Co., Ltd.
Antagonist anti-cd40 antibody pharmaceutical compositions
Stable liquid pharmaceutical compositions comprising an antagonist anti-cd40 antibody as a therapeutically or prophylactically active component and methods useful in their preparation are provided. These compositions comprise the antagonist anti-cd40 antibody, a buffering agent to maintain the ph of the composition between about ph 5.0 and about ph 7.0, and an amount of arginine-hcl sufficient to render the liquid composition near isotonic.
Inhibitor of odor caused by sotolone
It is intended to provide a substance inhibiting an odor caused by sotolone. The present invention provides an inhibitor of an odor caused by sotolone, comprising an antagonist of an olfactory receptor or8d1 as an active ingredient..
Pharmaceutical composition comprising a trpa1 antagonist and an analgesic agent
The present patent application relates to a pharmaceutical composition comprising a trpa1 antagonist and an analgesic agent. Particularly, the present patent application provides a pharmaceutical composition comprising a thienopyrimidinedione compound as a trpa1 antagonist and an analgesic agent; and use of such composition for treating pain in a subject..
Glenmark Pharmaceuticals S.a.
Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents
Wherein: ar, z, r3, r4 and r5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have at1 receptor antagonist activity and neprilysin inhibition activity.
Substituted diketopiperazines and their use as oxytocin antagonists
Wherein r1 is 2-indanyl, r2 is 1-methylpropyl, r3 is 2-methyl-1,3-oxazol-4-yl and r4 and r5 together with the nitrogen atom to which they are attached represents morpholino, process for their preparation, pharmaceutical compositions containing them and their use in medicine.. .
Selectively substituted quinoline compounds
Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (sle) and lupus nephritis.. .
Eisai R&d Management Co., Ltd.
Therapeutic compositions and method
This invention relates the use of cortisol blockers (glucocorticoid receptor [gr] antagonists) for the prevention or addiction induced anxiety and withdrawal side effects as a therapeutic and in concert with a diagnostic. Such addictions could be, but are not limited to, alcohol, drugs, caffeine, sugar, food, nicotine, etc.
Pop Test Cortisol Llc
Heterocyclic aspartyl protease inhibitors
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 antagonist.. .
Uses of antagonists of hyaluronan signaling
Described herein is the finding that hyaluronan antagonists that inhibit hyaluronan signaling are capable of inhibiting airway inflammation and airway hyperresponsiveness (ahr). The present disclosure provides a method of preventing or reducing ahr in a subject suffering from or at risk for ahr by administering a hyaluronan antagonist.
The Universtiy Of North Carolina At Chapel Hill
Anti-angiogenic treatment of ovarian, breast, and prostate cancer with a combination of antagonists
The teachings provided herein generally relate to a combination therapy and are directed to pharmaceutical compositions and methods for administering a combination of an α5β1 antagonist with an α2β1 antagonist to a subject. The methods are for use in inhibiting, preventing, or reversing angiogenesis, as well as in treating cancer.
California Northstate College Of Pharmacy
Provided herein are formulations and methods for treating pain in human beings. Also provided are optimal ratios at which an opioid and an opioid antagonist may be combined for administration to humans such that the opioid activity is inhibited.
Alpharma Pharmaceuticals Llc
Il-19 as a biomarker of tslp treatment
The present invention relates to the use of il-19 as a biomarker of treatment with a tslp antagonist.. .
Merck Sharp & Dohme Corp.
Il-17 antagonist antibodies
The disclosure relates to antibodies against human il-17 which act as antagonist antagonists of il-17, and their use in the diagnosis or treatment of il-17 mediated diseases.. .
Antagonists of il-17 isoforms and their uses
The invention relates to antagonists of il-17 isoforms and their uses in diagnosis and therapy, especially for the treatment or prevention of cancers or autoimmune and chronic inflammatory diseases.. .
Human monoclonal antibodies to ctla-4
In accordance with the present invention, there are provided fully human monoclonal antibodies against human cytotoxic t-lymphocyte antigen 4 (ctla-4). Nucleotide sequences encoding and amino acid sequences comprising heavy and light chain immunoglobulin molecules, particularly contiguous heavy and light chain sequences spanning the complementarity determining regions (cdrs), specifically from within fr1 and/or cdr1 through cdr3 and/or within fr4, are provided.
Process for the preparation of cycloheptapyridine cgrp receptor antagonists
The disclosure generally relates to a process for the preparation of compounds of formula i, including synthetic intermediates which are useful in the process.. .
Bristol-myers Squibb Company
Quinolinyl glucagon receptor modulators
Or a pharmaceutically acceptable salt thereof, wherein r1, r2, r3, a1, a2, a3, b1, b2, b3 and b4 are as defined herein. The compounds of formula i have been found to act as glucagon antagonists or inverse agonists.
Antagonists of prostaglandin ep3 receptor
Provided herein are antagonists of prostaglandin ep3 receptor, processes to make said antagonists, and methods comprising administering said antagonists to a mammal in need thereof.. .
Pyridine cgrp receptor antagonists
The present invention is directed to pyridine derivatives which are antagonists of cgrp receptors and useful in the treatment or prevention of diseases in which cgrp is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which cgrp is involved..
Merck Sharp & Dohme Corp.
Fpr1 antagonist derivatives and use thereof
Each of rk and rt is selected from a group consisting of a hydrogen, a hydroxyl group, a c1-c4 alkyl-substituted hydroxyl group, a c1-c4 alkoxyl group, a carboxylic acid group, a c1-c4 alkyl nitrile-substituted, c1-c4 alkyl-substituted or c1-c4 alkoxyl-substituted amido group, a c1-c4 alkyl-substituted ester group and a benzoyl group having a c1-c4 alkyl-substituted benzene ring; and each of rm and rs is selected from a group consisting of a hydrogen, a hydroxyl group, a phenyl group, a pyridinyl group, a carboxylic acid group, a c1-c4 alkoxyl substituted ester group, and a benzoyl group having a hydroxyl-substituted, a halogen-substituted, a c1-c4 alkoxyl-substituted or a c1-c4 alkyl-substituted benzene ring.. .
Methods of treating a patient having an autoimmune disorder by administering a baff antagonist
Therapeutic regimens for administration of baff antagonists for treatment of immunologic and related disorder are described. Regimens involve a short-term baff antagonist administration course followed by an extended no-treatment period prior the round or administration..
Biogen Idec Ma Inc.
Novel antagonist antibodies and their fab fragments against gpvi and uses thereof
The present invention discloses novel antibodies that specifically bind to the human platelet membrane protein glycoprotein vi (gpvi) and their monovalent fragments or derivatives. The antibodies of the invention are antibodies from hybridoma clone 390 and fragment antibodies thereof able to induce a gpvi depletion phenotype.
Glucagon receptor modulators
Or a pharmaceutically acceptable salt thereof wherein r1, r2, r3, a1, a2, a3, a4, l, b1, b2, b3 and b4 are as defined herein. The compounds of formula i have been found to act as glucagon antagonists or inverse agonists.
Crhr1 antagonists for use in the treatment of patients having crh overactivity
The present invention relates to a corticotropin releasing hormone receptor type 1 (crhr1) antagonist for use in the treatment of depressive symptoms and/or anxiety symptoms in a novel group of patients, i.e. Patients having corticotropin releasing hormone (crh) overactivity..
Holsboermaschmeyer Neurochemie Gmbh
Modulation of line-1 reverse transcriptase
A reverse transcriptase encoded by l-1 (line-1) has been identified as a target molecule for treating or preventing cancers induced or mediated by this molecule. Method of treating or preventing such cancers in patients involves administration of a therapeutically effective amount of a composition having an inhibitor or antagonist of the reverse transcriptase in cells of the patients.
Alt Solutions, Inc.
Method and device for the determination of platelet function under flow conditions
The invention lies in the area of platelet function diagnostics and relates to a method for the determination of platelet function under flow conditions as well as a device for the implementation of this method. The method is particularly suitable for the determination of the effect of clopidogrel and of other p2y(12) antagonists with antithrombotic activity as well as the determination of p2y(1) antagonists with antithrombotic activity..
Siemens Healthcare Diagnostics Products Gmbh
Oncostatin m (osm) antagonists for preventing cancer metastasis and il-6 related disorders
A method of treating cancer or metastasis is provided involving administering at least one oncostatin m (osm) antagonist to a subject, wherein the subject has been diagnosed with cancer. Administration of an osm antagonist such as a small molecule pharmaceutical is provided as well as an anti-osm antibody, an anti-osm aptamer, and an osm mrna antagonist.
Boise State University
Use of immunesuppressant receptor
Bir1 functions as an immunosuppressive receptor, and the antagonist of bir1 has immunopotentive activity, which is able to use for preventing and/or treating a cancer, an immunodeficiency disease or an infectious disease.. .
Methods for inhibiting ocular angiogenesis
The present invention provides methods of using tspan12 and norrin antagonists to inhibit ocular vascular development and to treat related disorders.. .
4-substituent-2-hydroxylmorpholine-3-one and preparation method thereof
A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof.. .
Shanghai Institute Of Pharmaceutical Industry
Chimeric il-1 receptor type i agonists and antagonists
Featured herein are non-naturally occuring cytokine domains that can be used, inter alia, to modulate cellular signalling responsive to interleukin-1 receptor i (il-1ri), to treat disorders, and to detect and/or bind to cellular receptors, as well as other agents. Exemplary cytokine domains can contain amino acid residues from at least two parental cytokines domains, for example, receptor binding features, surface features, β strands, and loops from at least two parental cytokines domains..
Eleven Biotherapeutics, Inc.
G protein-coupled purinergic receptor gpr17 mediates orexigenic effects of foxo1 in agrp neurons
G protein-coupled receptor (gpcr) gpr17 expressed in hypothalamic agouti-related peptide-expressing (agrp) neurons increases appetite and glucose tolerance and insulin sensitivity. By contrast, increasing gpr17 reduced glucose tolerance and increased appetite.
The Trustees Of Columbia University In The City Of New York
Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including type i and ii diabetes, insulin resistance and hyperglycemia.
Metabasis Therapeutics, Inc.
Heterocyclic cgrp receptor antagonists
The present invention is directed to heterocyclic compounds which are antagonists of cgrp receptors and useful in the treatment or prevention of diseases in which cgrp is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which cgrp is involved..
Merck Sharp & Dohme Corp.
Methods for treating gi tract disorders
Provided herein are methods, compositions, and kits for the treatment of an enteric nervous system disorder. Such methods may comprise administering to a subject an effective amount of a phenothiazine compound, a peripherally restricted dopamine decarboxylase inhibitor, and/or a peripherally restricted dopamine d2 receptor antagonist that does not substantially inhibit herg channels..
Cyclic amine derivatives as ep4 receptor antagonists
The present invention therefore relates to novel compounds which are selective antagonists of the ep4 subtype of pge2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of prostaglandin e mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.. .
Methods of altering bone growth by administration of sost or wise antagonist or agonist
The present invention provides a method of promoting local bone growth by administering a therapeutic amount of a sost antagonist to a mammalian patient in need thereof. Preferably, the sost antagonist is an antibody or fab fragment selectively recognizing any one of seq id nos: 1-23.
Alpha-4-beta-7 heterodimer specific antagonist antibody
There are disclosed alpha4beta7 heterodimer-specific antigen binding proteins, nucleic acids encoding them, and methods of making and using them.. .
Polypeptide binding to annexin a1 and use thereof
A polypeptide binding to annexin a1, an antagonist against annexin a1 including the polypeptide, an anti-annexin a1 antibody including the polypeptide or an antigen-binding fragment thereof, and methods of preventing, treating and/or diagnosing a disease, including administering the antagonist and/or the antibody or an antigen-binding fragment thereof to a subject.. .
Samsung Electronics Co., Ltd.
Combination therapy for treating breast cancer
The invention provides compositions and methods for treating breast cancer. Specifically, the invention relates to administering a transforming growth factor beta (tgfβ) antagonist in combination with capecitabine and ixabepilone to treat breast cancer..
Use of survivin antagonists in polyomavirus-related disease
A method of treating a polyomavirus (+) cancer in which survivin is upregulated in a patient is provided, comprising administering to the patient a therapeutically effective amount of a composition that downregulates survivin expression or function in cells of the polyomavirus (+) cancer. A method of reducing growth of polyomavirus (+) cancer cells in which survivin is up-regulated is provided, comprising contacting the cells with an amount of a composition that downregulates survivin expression or function effective to reduce growth of the cells.
University Of Pittsburgh-of The Commonwealth System Higher Education
An element comprising a cup containing a thermally expanding material, a piston capable of translational movement along its axis, a rigid guide for guiding the translational movement of the piston, a seal for sealing in the thermally expanding material having an annular overall shape, centered on the axis and through which the piston passes axially right through, and which includes first and second opposite axial parts against which the guide and the cup press respectively in a substantially antagonistic manner so as to compress the seal around the piston, and an anti-extrusion washer mounted coaxially around the piston and axially interposed between the guide and the first part of the seal. The invention provides for including in this thermostatic element means for supercompressing the first part of the seal around the piston, which means are designed to make the degree of compression of the first part of the seal equal to a value strictly higher than that associated with an operational thermostatic element formed by the cup, the piston, the guide, the seal and the anti-extrusion washer assembled with one another without these supercompression means..
Fused cyclopentyl antagonists of ccr2
Wherein: r0, r1, r2, r3, r4, r5, and a are as defined in the specification.. .
Combination of 4- benzamide and a nmda receptor antagonist and pharmaceutical compositions containing the same
Medicinal products containing the same which are useful in the treatment of cognitive disturbances associated with cerebral ageing and neurodegenerative diseases.. .
Compositions and methods for minimizing or reversing agonist-induced desensitization
Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient.
Pharmorx Therapeutics, Inc.
Triazolone compounds and uses thereof
The invention disclosed herein is directed to compounds of formula (i) and pharmaceutically acceptable salts thereof, which are useful in the treatment of prostate, breast, colon, pancreatic, human chronic lymphocytic leukemia, melanoma and other cancers. The invention also comprises pharmaceutical compositions comprising a therapeutically effective amount of compound of formula (i), or a pharmaceutically acceptable salt thereof.
Inception 2, Inc.
Pyridinyl amides as p2x3 and p2x2/3 inhibitors
Or a pharmaceutically acceptable salt thereof, wherein, r1 is optionally substituted phenyl or optionally substituted pyridinyl, and r2, r3, r4, r5, r6, r7, r8 and r9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with p2x3 and/or a p2x2/3 receptor antagonists and methods of making the compounds..
Combinations comprising antimuscarinic agents and pde4 inhibitors
Combinations comprising (a) a pde4 inhibitor 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 diseases.. .
Compounds are provided that act as potent antagonists of the ccr9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for ccr9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of ccr9-mediated diseases, and as controls in assays for the identification of ccr9 antagonists..
Modulation of bacterial quorum sensing with synthetic ligands
The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect.
Wisconsin Alumni Research Foundation
Application of initial doses of lhrh analogues and maintenance doses of lhrh antagonists for the treatment of hormone-dependent cancers and corresponding pharmaceutical kits
Lhrh analogues and lhrh antagonists for use in the treatment or prophylaxis of hormone-dependent cancers, in particular prostate cancer, prostate carcinoma and/or advanced prostate carcinoma, by administering an initial dose of an lhrh analogue over a first period sufficient to effect hormonal castration, then administering a maintenance dose of an lhrh antagonist over a second period, the dose being insufficient to achieve and/or maintain hormonal castration.. .
Aeterna Zentaris Gmbh