|| List of recent Antagonist-related patents
| Nicotinic receptor non-competitive modulators|
The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for use, and their pharmaceutical compositions.. .
| Nicotinic receptor non-competitive antagonists|
The present invention relates to compounds that modulate nicotinic receptors as non-competitive antagonists, methods for their synthesis, methods for their use, and their pharmaceutical compositions.. .
| Mir-142 and antagonists thereof for treating disease|
Methods of treating various conditions using mir-142, mir-142 mimics, and antagonists of mir-142 are provided.. .
| Molecular genetic approach to treatment and diagnosis of alcohol and drug dependence|
Compositions and methods are provided that are useful for diagnosing, treating, and monitoring alcohol dependence and disorders, susceptibility to alcohol dependence disorders, as well as drug related dependence and disorders. The methods include treating patients with an antagonist of the serotonin receptor 5-ht3 for such disorders, wherein the patient's serotonin transporter gene slc6a4 is known to have particular genotypes..
| Angiotensin ii receptor antagonist for the prevention or treatment of systemic diseases in cats|
A method is described for the treatment of systemic diseases in cats. A composition is administered to a cat, where the composition includes a therapeutically effective amount of angiotensin ii receptor 1 (at-1) antagonist (sartan)..
| 8-azabicyclo[3.2.1]octane compounds as mu opioid receptor antagonists|
Wherein r1, r2, r3, a, and g are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds..
| Cycloalkane carboxylic acid derivatives as cxcr3 receptor antagonists|
That are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of cxcr3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds..
| P13 kinase antagonists|
The present invention provides novel pi3-kinase antagonists and methods of use thereof.. .
| Method and composition for treating alzheimer-type dementia|
There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetylcholinesterase inhibitor (achei) in a patient suffering from an alzheimer type dementia by decreasing concomitant adverse effects by administration of said achei in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetylcholinesterase inhibition in the cns of said patient is achieved and alleviation of the symptoms of alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of alzheimer type dementia in combination with an acetylcholinesterase inhibitor (achei) and pharmaceutical compositions comprising (a) a 5ht3 receptor antagonist, a dopamine antagonist, a h1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholinesterase inhibitor are also described..
| Novel c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity|
Described are steroidal c-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3β-ol or analogs thereof with tributylstannyl diazines.
| Ddr1 antagonist or an inhibitor of ddr1 gene expression for use in the prevention or treatment of crescentic glomerulonephritis|
The present invention relates to uses, methods and compositions for treating crescentic glomerulonephritis. More specifically, the present invention relates to a ddr1 antagonist or an inhibitor of ddr1 gene expression for the prevention or the treatment of said disease..
| Hepcidin, hepcidin antagonists and methods of use|
The invention relates to purified, correctly folded hepcidin, antibodies that bind hepcidin, and methods of making and using such materials. Also provide are methods of treated hepcidin-related disorders..
| Anti-human cxcr4 antibodies|
The present invention provides novel antibodies to human cxcr4 with high affinity to the target and the ability to act potently as antagonists. The antibodies disclosed herein bind to a diverse range of epitopes..
|Methods for making cytokine compositions from tissues using non-centrifugal methods|
Apparatus and methods for generating a solution rich in interleukin-1 receptor antagonist from a tissue comprising cytokine-producing cells. The apparatus can include a filter used with a separation system.
|Small molecule antagonists of bacterial quorum-sensing receptors|
A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized.
|Combinations of opioid/tlr4 antagonist and a cyclooxygenase (cox) inhibitor for use in the treatment of pain|
Disclosed are compositions for treatment of pain comprising a first compound and a second compound, the first compound is an opioid antagonist that treats pain by blocking toll-like receptor 4 (tlr4) and the second compound is a cyclooxygenase (cox) inhibitor that enhances the pain treatment effect of the first compound. Examples of opioid antagonist include naltrexone and naloxone.
|Combinations of opioid/tlr4 antagonists and acetyl-para-aminophenol (apap) for use in the treatment of pain|
Disclosed are compositions for the treatment of pain comprising a first compound and a second compound, the first compound is an opioid antagonist that treats pain by blocking toll-like receptor 4 (tlr4) and the second compound is acetyl-para-aminophenol (apap) that enhances the pain treatment effect of the first compound. Examples of opioid antagonist include naltrexone and naloxone, synergistic pharmaceutical compositions thereof, and their use in the treatment, prevention, and reversal of neuropathic and nociceptive pain..
|Mineralocorticoid receptor antagonists|
The present invention is directed to compounds of the formula (i) as well as pharmaceutically acceptable salts thereof that are possible useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the formula (i), to their possible use for the treatment of the above mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the formula (i)..
|Product and method for treating diarrhea|
A method of treating diarrhea in a patient includes administering an h1 receptor antagonist and an h2 receptor antagonist to the patient.. .
|Crystal of androgen receptor antagonistic compound|
[solution] a01-type crystal of monohydrate, a01-type crystal of hydrochloride, a01-type crystal of hydrobromide, and a01-type crystal of methanesulfonate of (2r,5s)-4-(3-chloro-4-cyanophenyl)-n-(2-cyclopropylpyrimidin-5-yl)-2,5-dimethylpiperazine-1-carboxamide, which have certain crystal forms, are provided.. .
|Solid state forms of 6-[4-[3-((r)-2-methylpyrrolidine-1-yl)-propoxy]phenyl] 2h-pyridazine-3-one hydrochloride|
Solid state forms of the compound 6-[4-[3-((r)-2-methylpyrrolidine-1-yl)-propoxy]phenyl]2h-pyridazine-3-one hydrochloride (compound 1), processes for preparing the solid state forms, and pharmaceutical compositions thereof, are provided. Compound 1 is a histamine h3 receptor antagonist/inverse agonist.
|Novel chiral n-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective nk-3 receptor antagonists, pharmaceutical composition, methods for use in nk-3 receptor mediated disorders and chiral synthesis thereof|
The present invention relates to novel compounds of formula i and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using n-sp3 protective groups.
|Heterocyclic derivative having pgd2 receptor antagonist activity|
Wherein x1, x2, x3, x4, x5, r5, r6, r7, r8, n, p, q, ring a and ring b are as described in the specification, or a pharmaceutically acceptable salt thereof.. .
|2,5-disubstituted thiomorpholine orexin receptor antagonists|
The present invention is directed to 2,5-disubstituted thiomorpholine amide compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2,5-disubstituted thiomorpholine amide compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.
|Substituted pyrazole analogs as rar antagonists|
The present invention provides compounds of formula i or a pharmaceutical salt thereof; methods of treating osteoarthritis and the pain associated with osteoarthritis using the compounds; and processes for preparing the compounds.. .
|Cgrp receptor antagonists|
(wherein variables a1, a2, a3, ring-b, m, n, j, e1, e2, e3, r5, rpg and y are as described herein), which are useful as antagonists of cgrp receptors, and useful in the treatment or prevention of diseases in which cgrp receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (i) and the use of these compounds and compositions in the prevention or treatment of diseases in which cgrp receptors are involved..
Specifically, the invention provides azole derivatives represented by general formula (i), or pharmaceutically acceptable salts thereof that have an antagonistic action against the arginine-vasopressin (avp) v1b receptor:. .
|Novel prodrugs of c-17-heteroaryl steroidal cyp17 inhibitors/antiandrogens: synthesis, in vitro biological activities, pharmacokinetics and antitumor activity|
Prodrugs of steroidal c-17 benzoazoles, pyrimidinoazoles (az-abenzoazoles) and diazines. Methods of synthesis are also described, whereby a prodrug group is substituted for a functional group at a ring portion of the abc ring structure of the steroid.
|Use of antagonists of growth hormone or growth hormone receptor to prevent or treat stress-sensitive psychiatric illness|
The invention relates to methods for treating stress sensitive condition. For instance a subject having or at risk of having a stress-sensitive condition may be treated with a growth hormone (gh) antagonist in an effective amount to treat the stress sensitive condition.
|Methods and non-immunogenic compositions for treating inflammatory disorders|
Methods for making non-immunogenic anti-inflammatory cytokine compositions, comprising (a) obtaining a liquid comprising cytokine producing cells from a mammalian donor; (b) contacting the liquid with a solid extraction material to generate a composition rich in interleukin-1 receptor antagonist; and performing one or both of (i) removing cells from the composition and (ii) freezing the composition. The compositions comprise two or more of il1-ra, stnf-r1, stnf-rii, igf-i, egf, hgf, pdgf-ab, pdgf-bb, vegf, tgf-β1, and sil-1rii, compositions may also contain white blood cells and platelets..
|Methods for making cytokine compositions from tissues using non-centrifugal methods|
Non-centrifugal methods for generating a solution rich in interleukin-1 receptor antagonist from a tissue comprising cytokine-producing cells. The solution rich in il-1ra can also include at least one of stnf-ri, stnf-rii, igf-i, egf, hgf, pdgf-ab, pdgf-bb, vegf, tgf-β1, and sil-1 rii..
|Newcastle disease viruses and uses thereof|
Described herein are chimeric newcastle disease viruses engineered to express an agonist of a co-stimulatory signal of an immune cell and compositions comprising such viruses. Also described herein are chimeric newcastle disease viruses engineered to express an antagonist of an inhibitory signal of an immune cell and compositions comprising such viruses.
|Use of lxr antagonists for treatment of side effects of elevated glucocorticoid levels|
The present application is directed to uses of an agent that antagonizes the lxrβ receptor for the treatment of side effects associated with elevated glucocorticoid levels as well as uses of a glucocorticoid in combination with the agent that antagonizes the lxrβ receptor for treatment of a disease wherein glucocorticoid treatment is indicated.. .
|Interferon alpha and omega antibody antagonists|
Broadly neutralizing interferon-α and interferon-ω antibody antagonists, polynucleotides encoding the antibodies or fragments, and methods of making and using the foregoing are useful in the treatment of diseases associated with increased production of ifnα and ifnω.. .
|Method for treating inflammation|
A method for treating il-20 induced inflammation. An antagonist to il-20 is administered to treat inflammation and associated diseases.
|Il-33 antagonists and uses thereof|
The present invention provides interleukin-33 (il-33) antagonists comprising one or more il-33-binding domains and one or more multimerizing domains and methods of using the same. According to certain embodiments of the invention, the il-33-binding domains can comprise an il-33-binding portion of an st2 protein and/or an extracellular portion of an il-1 racp protein.
|Methods of using adenosine receptor antagonists for treating bleeding disorders|
Methods of treating bleeding disorders, such as bleeding diseases such as hemophilia, by administering adenosine 2a receptor and/or adenosine 2b receptor antagonists to subjects in need thereof are disclosed. In some embodiments, the methods further include administration of the antagonist with one or more of factor viii, factor ix and factor xi to treat the bleeding disorder..
|Pyrazole derivatives as modulators of hepatocyte growth factor (scatter factor) activity|
And pharmaceutically acceptable derivatives thereof, wherein r1, r2 and b are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases in which hgf/sf or the activities thereof, or agonists or antagonists thereof have a therapeutically useful role.. .
|Tamper resistant dosage form comprising an adsorbent and an adverse agent|
Pharmaceutical compositions and dosage forms comprising an adsorbent, and an adverse agent, such as an opioid antagonist. In one embodiment, at least a portion of the adverse agent is on the surface or within the micropore structure of an adsorbent material.
|Polycyclic compounds as lysophosphatidic acid receptor antagonists|
Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating lpa-dependent or lpa-mediated conditions or diseases..
|Methods and compositions of small molecule modulators of hepatocyte growth factor (scatter factor) activity|
The present invention provides compositions and formulations of compounds having formula (i) and pharmaceutically acceptable derivatives thereof, wherein p, r1, r2 and b are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of injuries, conditions or diseases in which hgf/sf or the activities thereof, or agonists or antagonists thereof have a therapeutically useful role. In addition, methods are provided for treating such diseases or diseases starting at a time after the onset of the injury, condition or disease..
|Fsh receptor antagonists|
The invention relates to fsh receptor antagonist according to general formula i or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders..
|Mineralocorticoid receptor antagonists|
The present invention is directed to compounds of the formula (i) as well as pharmaceutically acceptable salts thereof that are aldosterone receptor antagonists which might be useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the formula (i), to their possible use for the treatment of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the formula (i)..
|Cancer treatment using bmp inhibitor|
Methods for regulating cancer cell growth and survival, inhibiting cancer cell growth, promoting cancer cell death, and/or treating a cancer make use of antagonists of a type i bmp receptor. In some embodiments the cancer is a lung cancer and the cancer cell is a lung cancer cell..
|Polypeptides involved in immune response|
Novel polypeptides which comprise a receptor-ligand pair involved in t-cell activation are disclosed. Nucleic acid molecules encoding said polypeptides, and vectors and host cells for expressing same are also disclosed.
|Process for the preparation of an endothelin receptor antagonist|
The present invention relates to a novel process for the preparation of a compound of formula (i) wherein r is a methyl or methoxy group; to certain novel intermediates prepared in such a process and their use.. .
|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.. .
|Methods of treating autoimmune diseases with dll4 antagonists|
The present invention provides methods of treating a disease or disorder, in which increasing the number of regulatory t cell (treg) is beneficial, by administering to a subject suffering from such a disease or disorder a therapeutically effective amount of dll4 antagonists that block dll4-notch signal pathways, thereby increasing the number of treg. Diseases or disorders treatable by the methods of the invention include autoimmune diseases or disorders, such as multiple sclerosis (ms), diabetes, and the like.
|Combination therapy for neoplasia treatment|
The present invention relates to an insulin-like growth factor (igf) receptor antagonist for use in the treatment of prostate neoplasia, including benign prostatic hyperplasia (bph), prostate cancer, and particularly crpc, wherein the antagonist is used in combination with an androgen receptor antagonist. An embodiment of the invention is where the androgen receptor antagonist is enzalutamide..
|Oral composition comprising a tnf antagonist and use thereof|
This application further describes a method of treating, preventing or reducing the severity of obesity, the method comprising, administering to the subject a therapeutically effective amount of a tnf antagonist molecule.. .
|Kv1.3 antagonists and methods of use|
The present invention relates to kv1.3 antagonists, and polynucleotides encoding them, and methods of making and using the foregoing.. .
|Methods and compositions for modulation of blood-neural barrier|
Methods and compositions for modulating blood-neural barrier (bnb) for the treatment of cns conditions such as edema, and for increased drug delivery efficacy across the bnb. The present invention further relates to improved tpa treatment of ischemic cerebrovascular and related diseases in combination with antagonism of the pdgf signaling pathway.
|Method of treating rheumatoid arthritis with an anti-il-6r antibody|
The present invention provides methods of preventing or treating rheumatoid arthritis using a fully human antibody or antigen-binding fragment thereof that specifically binds human interleukin-6 receptor (hil-6r). The methods of the present invention may include administration of a second therapeutic agent, such as one or more of a non-steroidal anti-inflammatory drug (nsaid), a glucocorticoid, a disease-modifying anti-rheumatic drug (dmard), or a tnf-alpha antagonist, t-cell blocker, anti-cd20 antibody, an il-1, jak or il-17 antagonist, or any combination thereof..
|Toll like receptor 3 antagonists, methods and uses|
Toll like receptor 3 (tlr3) antagonists, polynucleotides encoding tlr3 antagonists or fragments, and methods of making and using the foregoing are disclosed.. .
|Microrna modulators and method for identifying and using the same|
The present invention is a method for identifying agents which modulate microrna activity. The invention involves contacting a cell harboring a microrna and a microrna binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microrna modulator.