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7608724 |
Antibacterial and/or antiprotozoal nitromidazole derivative compounds with urease inhibitor activity, process for preparing these compounds and use in pharmaceutical compositions and medicines
The present application describes nitroimidazolic derivative compounds with antibacterial and/or antiprotozoal activity, which are potent urease inhibitors. It also describes the process for...
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7601720 |
Nicotinic receptor agonists for the treatment of inflammatory diseases
This invention relates to the use of nicotine receptor agonists for treating inflammatory diseases, including a variety of pulmonary diseases. Such agonists have fewer side effects than other...
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7585460 |
Method for inhibiting the biological acidification of water in contact with materials containing sulfur
The invention relates to a method for inhibiting the biological acidification of water which is in contact with materials containing sulfur in reduced form or with elemental sulfur, susceptible to...
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7579481 |
Method of making imidazole-2-ones and 2-thiones
A method of 4-substituted imidazole-2-ones and thiones which comprises reacting a methylene urea or methylene thiourea wherein said methylene is substituted with the 4-subsituent and a cyano or...
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7569596 |
Imidazolamino compounds
The invention relates to novel imidazolamino compounds. Also disclosed are methods of treating cancer by using one of these compounds and pharmaceutical compositions containing one of these compounds.
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7550466 |
Alpha and/or β-adrenergic antagonists and agonists to treat pain
The present disclosure provides for improved methods for treating pain, including pain associated with chronic inflammatory diseases, neuropathic pain and cancer by using α-adrenergic antagonists...
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7511068 |
Mercaptoimidazoles as CCR2 receptor antagonists
The present invention relates to a compound of formula (I) having CCR2 receptor antagonistic properties, particularly anti-inflammatory properties.
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7504517 |
Kv1.5 potassium channel inhibitors
The present invention relates to 1-N-amino-2-imidazolidinones and derivatives thereof which are effective as Kv1.5 potassium channel inhibitors providing atrial-selective antiarrhythmic agents. The...
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7423158 |
Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of β-secretase
The present invention provides a 2-amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compound of formula I
The present invention also provides methods for the use thereof to inhibit...
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7396828 |
PI-3 kinase inhibitor prodrugs
The invention provides prodrugs of inhibitors of PI-3 kinase. The compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.
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7390829 |
Alpha-2 adrenergic agonists
A compound is disclosed herein comprising
or a pharmaceutically acceptable salt or a prodrug thereof;
wherein R is OH or NH 2 .
Methods, compositions, and medicaments related thereto are...
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7361654 |
Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity...
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7358239 |
Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z...
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7332517 |
Derivatives of hydantoins, thiohydantoins, pyrimidinediones and thioxopyrimidinones, their preparation processes and their use as medicaments
A method of treating a disorder selected from the group consisting of acromegaly, hypophyseal adenomas, endocrine gastroenteropancreatic tumors including carcinoid syndrome and gastrointestinal...
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7312238 |
Nonsedating α-2 agonists
The present invention provides an α-2A/α-1A selective agonist that includes a compound represented by Structure 1 or a pharmaceutically acceptable salt, ester, amide, sterioisomer or racemic...
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7304083 |
2-iminoimidazole derivatives (2)
A 2-iminoimidazole derivative represented by the formula:
{wherein R 1 , R 2 and R 3 represent hydrogen, optionally substituted C 1-6 alkyl, etc.; R 6 represents hydrogen, C 1-6 alkyl, C...
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7282515 |
Derivatives of azaspiro compounds for the treatment of pain
This invention relates to azaspiro compounds and their use as medications especially for the treatment of chronic, chronic-phlogistic and/or neuropathic pain. Compounds that lend themselves...
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7271172 |
Pyrrolidine and azetidine compounds as CCR5 antagonists
The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in...
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7262223 |
Amidine derivatives for treating amyloidosis
The present invention relates to the use of amidine compounds in the treatment of amyloid-related diseases. In particular, the invention relates to a method of treating or preventing an...
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7241787 |
Substituted N-cycloexylimidazolinones, process for their preparation and their use as medicaments
The invention relates to substituted N-cyclohexylheterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to processes for their preparation and...
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7202251 |
Bicyclic anilide spirohydantoin CGRP receptor antagonists
The present invention is directed to compounds of the formula:
that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is...
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7199146 |
Imidazolidinedione analogs useful as anticoagulants and antithrombotics
A compound is disclosed, which is useful in treating a mammal having a disease-state characterized by thrombotic activity. The compound is of the following formula:
wherein A, B, R 1 , R 2 , R 3...
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7183277 |
Carboxylic acid amides
Novel compounds of the formula I
in which
D, W, X, Y, T and R 1 are as defined in Patent Claim 1,
are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or...
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7179829 |
Substituted imidazolidines, process for their preparation, and their use as a medicament or diagnostic, and medicament comprising them
The invention relates to novel compounds of the type of the imidazolidines of the formula I
in which R1 to R7 are as defined in the claims.
They are used for preparing a medicament for the...
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7091232 |
4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones and 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
Compounds of Formula 1
where X is S and the variables have the meaning defined in the specification are specific or selective to alpha 2B and/or alpha 2C adrenergic receptors in...
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7071223 |
Benzamide inhibitors of the P2X7 receptor
The present invention provides benzamide inhibitors of the P2X 7 receptor of the formula:
wherein R 1 –R 3 are as defined herein. The compounds of the invention are useful in the treatment...
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7045532 |
ACE-2 modulating compounds and methods of use thereof
ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include...
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7019021 |
Compounds and methods for treating urinary incontinence
Compounds of the formula (II)
wherein R 1 , R 2 , R 3 , R 4 , and R 5 are as set forth herein, pharmaceutical compositions containing them, and their use in treating urinary incontinence.
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6989384 |
Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
Compounds of the formula:
where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds,...
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6900213 |
Bisaryl derivatives having FSH modulatory activity
The invention relates to bisaryl derivatives of the formula I,
wherein (R,R) is selected from (H,H), O, (H,CH 3 ), (H,OH) and (H,CN); Ar is substituted phenyl
and A is a group of formula II,...
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6890928 |
Aromatic sulfone hydroxamic acids and their use as protease inhibitors
This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix...
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6867198 |
Agents and methods for the treatment of proliferative diseases
The present invention provides selective kinase inhibitors of formula (I)
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6858636 |
1-phenyl imidazol-2-one biphenylmethyl compounds for treatment of circulatory disorders
A class of 1-phenyl imidazol-2-one biphenylmethyl compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the...
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6747051 |
m-Amino-phenylimino-imidazolidine derivatives for treating urinary incontinence
A compound of Formula I or of Formula II wherein: R 1 is F, Cl, Br, CH 2 F, CF 2 H, or CF 3 ; R 2 is NR 6 R 7 , where R 6 is Me, Et, Pr, or iPr, and R 7 is Me, Et or Pr; and R 3 , R 4 , and...
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6730691 |
Uses of alpha adrenergic blocking agents
Disclosed are methods and compositions for inhibiting undesirable visual anomalies commonly experienced by individuals who have undergone refractive eye surgery, including photophobia, glare,...
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6706739 |
Imidazolidinone compounds
A compound having the formula: in which R 1 , R 2 , R 3 , T, W, m, x, and y are defined as in the specification. Also disclosed is a method of treating enterovirus infection by using a compound...
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6706290 |
Methods for eradication of nanobacteria
Nanobacteria contribute to pathological calcification in the human and animal body, including diseases such as kidney stones, salivary gland stones, dental pulp stones and atherosclerosis. The...
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6703409 |
2′-Halo-3′,5′-dialkoxyphen-1′-yl-imino-2-imidazolidine and the use thereof as a drug
The present invention relates to 2′-halo-3′,5′-dialkoxyphen-1′-yl-imino-2-imidazolidi
ne, the tautomeric 2′-halo-3′,5′-dialkoxyanilino-2-imidazoline and/or the pharmacologically...
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6689794 |
Aromatic sulfone hydroxamates and their use as protease inhibitors
This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known...
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6664286 |
Serotonergic 5ht2 agonists for treating glaucoma
Compounds with 5HT 2 receptor agonist activity useful for treating glaucoma, including lowering intraocular pressure. Compositions and methods for their use are also disclosed.
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6586452 |
C1 to C4 side chain modified nodulisporic acid analogs
The present invention relates to novel nodulosporic acid derivatives, which are acaricidal, antiparasitic, insecticidal and anthelmintic agents.
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6576632 |
Biaryl compounds useful as anticancer agents
The present invention relates to compounds of formula I and to pharmaceutically acceptable salts, hydrates and prodrugs thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 10 , R 11 , b, m, n, p...
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6534048 |
Topical clonidine preparation
An aqueous gel in unit dose form and suitable for topical delivery of clonidine and comprising clonidine, a water-gelling amount of a pharmaceutically acceptable gelling agent and having a pH value...
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6518293 |
Anti-HIV imidazolone derivatives
The invention is concerned with novel imidazolone derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds...
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6492409 |
Kinase inhibitors
The present invention relates to compounds of formula (I) wherein: Ar 1 or Ar 2 is an optionally substituted indole, and the other group is an optionally substituted aromatic or heteroaromatic...
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6448286 |
Imino pyrrolidine derivatives useful as nitric oxide synthase inhibitors
The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.
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6417184 |
Triple drug therapy for the treatment and prevention of acute or chronic pain
A triple drug therapy, pharmaceutical kit, composition, and method of treatment regimen utilized as a combination of effective amounts of an anxiolytic agent, centrally acting alpha antiadrenergic...
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6395764 |
2-imidazolinylaminoindole compounds useful as alpha-2 adrenoceptor agnonists
This invention involves compounds having the following structure: wherein: a) R 1 is hydrogen; or alkyl; bond (a) is a single or a double bond; b) R 2 and R 3 are each independently selected...
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6391904 |
Iminoguanidine derivatives, preparation method, use as medicines
A compound of the formula where the substituents are defined in the specification and its pharmaceutically acceptable salts and prodrugs thereof useful as antagonists of vitronectin receptors.
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6340679 |
Guanidine derivatives as inhibitors of cell adhesion
The present invention relates to acylguanidine derivatives of the formula I in which R 1 , R 2 , R 4 , Ar, X and n have the meanings indicated in the claims, their physiologically tolerable...
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