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7612096 |
Methods for treatment, modification and management of radiculopathy using 1-oxo-2-(2,6-dioxopiperidin-3yl)-4-aminoisoindoline
Methods of treating, preventing, modifying and managing various types of pain are disclosed. Specific methods comprise the administration of an immunomodulatory compound, or a pharmaceutically...
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7612065 |
Inhibitors of c-JUN N-terminal kinases (JNK)
The present invention relates to inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods...
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7595329 |
Benzimidazolone carboxylic acid derivatives
This invention relates to compounds of the formula (I):
wherein R 1 , R 2 , R 3 , A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions...
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7585857 |
Cytotoxic agents comprising taxanes and their therapeutic use
A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more...
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7582767 |
Substituted sulphonamide compound and uses thereof
The present invention relates to compounds of the formula (I),
wherein R 1 and R 2 are as defined in the description; to pharmaceutical formulations comprising these compounds, and to the use...
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7579333 |
Therapy using a combination of raloxifene and alendronate
Provided are methods of treating bone disease including, but not limited to, osteoporosis, metastatic bone disease, or Paget's disease, by administering a combination of raloxifene and alendronate...
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7569604 |
Heterocyclic derivatives for modulation of calcium channels
Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.
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7569586 |
Compounds having β2 adrenergic receptor agonist and muscarinic receptor antagonist activity
This invention provides compounds of formula I:
wherein R 1 , R 2 , R 3 , R 4 ,R 5 , R 6 , R 7 , R 8a , R 8b , W, a, b, c and m are as defined in the specification, or a pharmaceutically...
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RE40793 |
Bicyclic benzamides of 3-or 4-substituted 4-(aminomethyl)-piperidine derivatives
The present invention of compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R 1 and R 2 ...
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7534801 |
Piperidinylchromen-6-ylsulfonamide compounds as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of a CNS disorder relating to or affected by the 5-HT6 receptor.
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7524864 |
Methods of treating sleep disorders
The invention relates to novel antihistamines and methods of modulating sleep by administering a doxepin analog or a pharmaceutically effective salt thereof.
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7498347 |
Hydroxycarbonylphenyl substituted 4-(aminomethyl)-piperidine benzamides as 5HT4 antagonists
The present invention is concerned with novel compounds of formula (I) having 5HT 4 -antagonistic properties. The invention further relates to methods for preparing such novel compounds,...
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7495111 |
Compounds useful as serotonin inhibitors and 5-HT1A agonists and antagonists
3-Amino chroman and 2-amino tetralin derivatives and compositions containing such compounds are disclosed. Such compounds are useful for modulating activity of a 5-HT 1A receptor (agonizing or...
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7470710 |
N-aroyl cyclic amine derivatives as orexin receptor antagonists
This invention relates to N-aroyl cyclic amine derivatives of formula (I), wherein X represents a bond, oxygen, NR 3 or a group (CH 2 ), wherein n represents 1, 2 or 3; Y represents CH 2 , CO,...
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7425565 |
Use of benzothiopenes to treat and prevent prostate cancer
Disclosed herein is a method for treating and preventing prostate cancer, and particularly androgen-independent prostate cancer, the method including administering to a mammal a benzothiopene...
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7423052 |
Piperidine compounds for use as orexin receptor antagoinst
A invention relates to N aroyl cyclic amine derivatives and their use as pharmaceuticals, specifically as orexin receptor antagonists.
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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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7393862 |
Method using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for treatment of certain leukemias
Methods of treating, preventing or managing leukemias are disclosed. The methods encompass the administration of an immunomodulatory compound of the invention known as Revlimid® or lenalidomide....
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7393861 |
Derivatives of 4-aminopiperidine and their use as a medicament
A subject of the present application is new derivatives of 4-aminopiperidines of formula
in which R 1 , R 2 and R 3 represent various radical, and their preparation processes by synthetic...
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7390798 |
Carboxamide spirolactam CGRP receptor antagonists
The present invention is directed to compounds of Formula I: I (where variables A 1 , A 2 , B, J, K, m, n, R 4 , R 5a , R 5b and R 5c are as defined herein) useful as antagonists of CGRP...
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7378421 |
Chromenone derivatives
Novel compounds of the formula I
in which
R 1 , R 2 , R 3 and Het are as defined herein, which
are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for the treatment of...
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7378399 |
Avermectins substituted in the 4″ and 4′-positions having pesticidal properties
What is described are a compound of the formula (I) Wherein A-B is —CH═CH— or —CH 2 —CH 2 —; n is 0 or 1; R 1 , is C 1 -C 12 alkyl, C 3 -C 8 cycloalkyl or C 2 -C 12 alkenyl; R 2 and R...
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7368476 |
Hydroxamates as therapeutic agents
The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone...
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7342027 |
1-phenylpiperidin-3-one derivatives and processes for the preparation thereof
Provided are 1-phenylpiperidin-3-one derivatives and pharmaceutically acceptable salts thereof, having cysteine protease inhibitory activity, pharmaceutical compositions containing the same as an...
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7326721 |
Doxepin analogs and methods of use thereof
The invention relates to novel doxepin analog compounds and methods of modulating sleep by administering such compounds, or a pharmaceutically effective salt thereof.
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7326720 |
Phenyl- and pyridylpiperidines with TNF activity
The present invention relates to compounds of formula (I):
in which X represents N or CH; R 1 represents a hydrogen or halogen atom or a CF 3 group; R 2 and R 3 independently represent a...
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7317026 |
CNS target modulators
The invention is directed to compositions used for treating Central Nervous System (CNS) disorders. More specifically, the invention is directed to derivatized, e.g., ester or carboxylic acid...
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7317025 |
Non-peptidic NPY Y2 receptor inhibitors
The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to...
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7314883 |
Anti-migraine treatments
The present invention relates to methods of treating neurogenic vasodilation, neurogenic inflammaton, migraine and other headaches, thermal injury, circulatory shock, flushing associated with...
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7312222 |
Heterocyclic piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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7265102 |
Substituted pyrazoles
Substituted pyrazoles of general formula
methods of manufacturing them, compositions containing them, and methods of using them to, for example, treat autoimmune diseases mediated by cathepsin...
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7247646 |
Benzopyranone compounds, compositions thereof, and methods of treatment therewith
Benzopyranone Compounds having the following structure:
wherein R 1 , R 2 , X, Y and n are as defined herein, are disclosed. The Benzopyranone Compounds are useful for treating or...
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7238709 |
Therapeutic carbamates
This invention relates to hindered carbamate derivatives that are muscarinic receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.
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7235584 |
Non-psychotropic cannabinoids
Novel non-psychotropic cannabinoids are disclosed and pharmaceutical compositions comprising these novel compounds are described for preventing neurotoxicity, neuroinflammation, immune or...
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7208495 |
Benzo-fused 5-membered hetrocycle compounds, process for preparation of the same, and use thereof
A compound represented by the formula:
(wherein, R 1 and R 2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R 1 and R 2 may form,...
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7208491 |
N-monoacylated o-phenylenediamines
Mono-acylated o-phenylendiamines derivatives of formula I
wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone...
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7205294 |
Selected CGRP-antagonists process for preparing them and their use as pharmaceutical compositions
The present invention relates to substituted piperidines of general formula
wherein A, B, D, E, X, R 1 and R 2 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers,...
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7189757 |
Treatment of sleep disorders using CNS target modulators
The invention is directed to compositions used for treating Central Nervous System (CNS) disorders. In addition, the invention provides convenient methods of treatment of a CNS disorder....
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7189726 |
Benzofuran derivatives as inhibitors of p38-α kinase
The invention is directed to methods to inhibit p38-α kinase using compounds which contain an aromatic residue coupled to an benzofuran moiety through a piperidine.
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7186719 |
Antibacterial agents
Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(═O) or the formula: —C(═O)NH(OH); R 1 represents hydrogen, C 1 –C 6 alkyl or C...
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7153868 |
N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises...
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7148240 |
Aminoalkoxybenzoyl-benzofuran or benzothiophene derivatives, method for preparing same and compositions containing same
The invention relates to benzofuran or benzothiophene derivatives of general formula:
These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes...
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7144883 |
Bicyclic sulfonamide compounds
The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful...
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7125887 |
Pyrrolidine modulators of CCR5 chemokine receptor activity
Pyrrolidine compounds of Formula (I), (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6a , R 6b , R 7 and R 8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor...
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7115634 |
4-aminopiperidine and their use as a medicine
A subject of the present application is new derivatives of 4-aminopiperidines of formula
in which R 1 , R 2 and R 3 represent various radical, and their preparation processes by synthetic...
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7115632 |
Sulfonyl aryl or heteroaryl hydroxamic acid compounds
A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a...
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7105542 |
2-Heterosubstituted 3-aryl-4H-1-benzopyran-4-ones as novel therapeutics in breast cancer
The present invention provides 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of cancers, namely breast cancer. This invention further provides a method of synthesis of...
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7090853 |
Noscapine derivatives as adjuvant compositions and methods of use thereof
An adjuvant composition comprising noscapine and its derivatives, for use in the treatment of tumors, cancer, as an adjuvant for vaccines.
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7071201 |
Quinoline derivatives
A novel compound of the formula:
wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R 1, R 2 , R 3 , R 4 , and R 5 represent each a substituent; n represents 0 or an integer...
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7041673 |
Ultrashort acting hypnotic barbiturates
The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are...
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