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7276521 |
Muscarinic acetylcholine receptor antagonists
Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.
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RE39820 |
Esters of thienyl carboxylic acids and amino alcohols and their quaternization products
Compounds of the formula
of which, in exemplary compounds, the thienyl group is attached via the 2-position and;
(a) A is 3α-(6β, 7β-epoxy)-tropanyl methobromide and R 1 is...
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7244415 |
HFA suspension formulations of an anhydrate
The invention relates to propellant gas formulations containing suspensions of the crystalline anhydrate of...
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7241745 |
Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I)
as well as methods for their production, medicaments containing these compounds...
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7217716 |
N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists
Compounds represented by Formula (I): (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain
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7217721 |
Tropane derivatives useful in therapy
The present invention provides compounds of formula (I)
wherein X, Y, R 1 , R 2 and R 3 are as defined hereinabove.
The compounds of the present invention are modulators, especially...
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7199132 |
Tropane analogs and methods for inhibition of monoamine transport
New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-hydroxyl or ketone substituents. The compounds of the present...
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7186731 |
2-cyanopyrrolidinecarboxamide compound
A compound of the formula (I) or a pharmaceutically acceptable salt thereof:
[wherein
X 1 and X 2 each is independently lower alkylene; X 3 is ═CH 2 , ═CHF or ═CF 2 ; R 1 is...
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7183290 |
Fluoropyrrolidines as dipeptidyl peptidase inhibitors
The present invention relates to novel compounds, their use for inhibiting post prolin/analine-cleaving proteases, such as serine proteases, such as dipeptidyl peptidases, such as dipeptidyl...
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7176217 |
Azabicyclo compound matrix metalloprotease inhibitor and skin preparation
An azabicyclo compound (I) or a salt thereof in accordance with the present invention has an excellent inhibiting action on matrix metalloproteases (MMPs) activity, and is useful for...
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7160898 |
Pharmacological treatment for sleep apnea
The present invention relates to pharmacological methods for the amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess...
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7148236 |
Modulators of acetylcholine receptors
The present invention relates to compounds that modulate neurotransmission by promoting the release of neurotransmitters such as acetylcholine, dopamine and norepinephrine. More particularly, the...
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7138405 |
Pharmaceutical combinations
Pharmaceutical combinations suitable for treating the lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH) in men are described herein. The combinations contain an...
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7115628 |
Bridged piperidine derivatives as melanocortin receptor agonists
Certain novel bridged piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are...
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RE39300 |
Inhibiting the development of tolerance to and/or dependence on an addictive substance
Nontoxic substances that block the N-methyl-D-aspartate (NMDA) receptor, e.g., a morphinan such as dextromethorphan or dextrorphan, or that block a major intracellular consequence of NMDA-receptor...
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7094784 |
High affinity ligands for nociceptin receptor ORL-1
Novel compounds of the formula
or a pharmaceutically acceptable salt or solvate thereof, wherein:
the dotted line represents an optional double bond; X 1 is optionally substituted...
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7094788 |
Esters of hydroxyl-substituted nitrogen heterocycles, processes for the preparation thereof as well as the use thereof as pharmaceutical compositions
The present invention relates to new compounds of general formula 1
wherein X − and the groups A, B, R, R 1 , R 2 , R 3 , R 3′ , R 4 , R 4′ , R x and R x′ may have the meanings given...
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7084153 |
Medicaments comprising steroids and a novel anticholinergic
A pharmaceutical composition comprising:
(a) a salt of formula 1
wherein: X − is an anion with a single negative charge; and (b) a steroid 2,
processes for preparing...
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7081466 |
2-aroylimidazole compounds for treating cancer
Disclosed is a compound represented by Structural Formula (I):
R 1 is a substituted or unsubstituted 2-imidazolyl group which is optionally fused to a substituted or unsubstituted aryl...
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7071209 |
Process for preparing a pharmaceutically active compound (granisetron)
The invention relates to a process for preparing granisetron, or a pharmaceutically acceptable salt thereof, which comprises: a) cyclisation of a compound of formula (I) in an inert solvent and at...
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RE39128 |
Pleuromutilin derivatives as antimicrobials
The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly...
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7045522 |
8-Azabicyclo[3.2.1]oct-2-ene and -octane derivatives technical field
The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene and -octane derivatives which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their...
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7041674 |
Carbamic acid esters with anticholinergic activity
A compound of formula 1
wherein X − , A, R 1 , R 2 , R 3 , and R 4 may have the meanings given in the claims and in the specification, processes for preparing them, their use in...
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7041667 |
CCR5 modulators
Compounds of Formula 1
[R egion α]—[R egion β]—[R egion γ]—[R egion δ] (1)
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7001900 |
Azabicyclic compounds for the treatment of disease
The invention provides compounds of Formula I:
wherein Azabicyclo is
W is a six-membered heterocyclic ring system having 1–2 nitrogen atoms or a 10-membered bicyclic-six-six-fused-ring...
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6982271 |
Tropane analogs
The present invention provides compounds, specifically novel tropane analogs, capable of acting as inhibitors of reuptake of monoamines. In preferred embodiments, these compositions are selective...
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6964972 |
8-Azabicyclo(3,2,1)oct-2 ene and octane derivatives as cholinergic ligands at nicotinic ACh receptors
The invention disclosed herein relates to novel a 8-azabicyclo[3.2.1]oct-2-ene compound of Formula II,
wherein
R is hydrogen, methyl, ethyl or benzyl; and R 1 is 3-thienyl, 2-thienyl,...
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6921541 |
Formulations and methods for providing prolonged local anesthesia
A formulation and methods for inducing sustained regional local anesthesia in a patient comprising a substrate comprising a local anesthetic and an effective amount of a biocompatible,...
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6908928 |
Crystalline tiotropium bromide monohydrate, processes for the preparation thereof, and pharmaceutical compositions
Crystalline monohydrate of (1α,2β,4β,5α,7β)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9
-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.0 2,4 ]nonane bromide (tiotropium bromide monohydrate), processes for...
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6858623 |
Compounds useful as reversible inhibitors of cysteine proteases
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , Het and X are defined herein. The...
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6852728 |
Anticholinergics, processes for preparing them, and pharmaceutical compositions containing them
A compound of formula 1
wherein:
A is a group selected from
X − is an anion with a single negative charge; R 1 and R 2 are each independently a C 1 -C 4 -alkyl optionally substituted...
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6835733 |
Tropane linked benzofuran derivatives
The present invention provides compounds of formula (I) which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of...
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6821985 |
Pharmaceutical combinations for the treatment of stroke and traumatic brain injury
This invention relates to methods of treating traumatic brain injury (TBI) or hypoxic or ischemic stroke, comprising administering to a patient in need of such treatment an NR2B subtype selective...
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6790857 |
Benzoylecgonine compositions and methods for producing them
This invention provides a method for preparing a benzoylecgonine composition comprising the steps of: (a) contacting benzoylmethylecgonine and propylene glycol in the presence or absence of water...
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6780860 |
Azabicyclylmethyl derivatives of 7,8-dihydro-1,6,9-trioxa-3-aza-cyclopenta&lsqb a&rsqb naphthalene as 5-ht1a antagonists
Compounds of the formula are useful for treating the cognitive deficits due to aging, stroke, head trauma, Alzheimer's disease or other neurodegenerative diseases, or schizophrenia and are also...
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6750195 |
Use of 5-HT4 modulators for the manufacture of a medicament for the treatment of the bladder diseases
A compound which acts as an antagonist at 5-HT 4 receptors is of potential use in the treatment of conditions associated with bladder hypersensitivity, such as urinary incontinence, which is often...
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6740672 |
Use of 5HT3-receptor antagonists for the treatment of chronic fatigue syndrome
5HT 3 -receptor-antagonists for the treatment of CFS (Chronic Fatigue Syndrome) are disclosed.
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6727254 |
Heteroaryl tropane derivatives as superior ligands for nociceptin receptor ORL-1
Novel compounds of the formula wherein R is optionally substituted heteroaryl or R 1 is H or C 1 -C 6 alkyl; and R 2 and R 3 are —CH 3 , —OCH 3 or halo; or a pharmaceutically...
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6680328 |
8-azabicyclo&lsqb 3.2.1&rsqb oct-2-ene and -octane derivatives
The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene and -octane derivatives which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their...
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6664271 |
Immunopotentiator agents
Novel compounds and methods for preparing same, immunopotentiating compositions, and a method for potentiating the immune system of a host animal. The method comprises administering to the animal...
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6656951 |
8-aza-bicyclo&lsqb 3.2.1&rsqb octan-3-ol derivatives of 2,3-dihydro-1,4-benzodioxan as 5-HT1A antagonists
Compounds of the formula: are useful for treating the cognitive deficits due to aging, stroke, head trauma, Alzheimer's disease or other neurodegenerative diseases, or schizophrenia and also...
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6645977 |
8-azabicyclo(3,2,1)oct-2-ene and octane derivatives as cholinergic ligands at nicotinic ACh receptors
The present invention discloses compounds of formula (1) any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein - - - - is a single or a double...
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6642246 |
Quinuclidine acrylamides
Compounds of formula I wherein A represents: and R, R 1 , R 2 , R 3 and R 4 are as defined in the specification, pharmaceutically-cceptable salts thereof, processes for preparing them,...
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6635237 |
Pharmaceutical composition based on cocaethylene and use thereof for treating psychoactive substance dependence
The present invention relates to a pharmaceutical composition comprising cocaethylene as active ingredient and to its use in treating dependence on psychoactive substances, in particular on cocaine.
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6632823 |
Substituted pyridine compounds useful as modulators of acetylcholine receptors
In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of...
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6632842 |
Albuterol and ipratropium inhalation solution, system, kit and method for relieving symptoms of chronic obstructive pulmonary disease
The present invention relates to a dual bronchodilator inhalation solution, system, kit and method for relieving bronchospasm in patients suffering from chronic obstructive pulmonary disease...
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6632824 |
Aryl-8-azabicyclo&lsqb 3.2.1&rsqb octanes for the treatment of depression
The present invention includes compounds of formula I wherein A, X, n, Ar 1 , and Ar 2 are defined as set forth herein. These compounds may be used to treat depression. The invention also...
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6617339 |
Oxazolidinone derivatives, process for their preparation and pharmaceutical compositions containing them
Compounds of formula (I) as defined herein, or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, are useful as antibacterial agents. Processes for their manufacture and...
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6593336 |
Methods for treating irritable bowel syndrome
This invention relates to the use of 5-HT3 receptor antagonists in the treatment of nonconstipated female IBS patients.
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6573275 |
Bicyclic amines
A compound of formula (I): wherein R 1 represents a group of formula (A) where each of W, X, Y and Z and Z represents either a group CR or the nitrogen atom, provided that not more than two of...
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