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7622497 |
Derivatives of gambogic acid and analogs as activators of caspases and inducers of apoptosis
The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are...
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7615555 |
Piperidine derivatives as modulators of chemokine receptor CCR5
Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).
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7608617 |
Naphthaline derivatives as H3 inverse agonists
The present invention relates to compounds of formula I:
and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The...
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7585879 |
Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I:
wherein a, b, c, d, m, n, p, s, t, W, Ar 1 , R 1 , R 2 , R 3 , R 4 , R 6 , R 7 , and R 8 are as defined in the specification. The compounds of...
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7585866 |
Protein tyrosine kinase inhibitors
The present invention relates to compounds of the Formula I, the pharmaceutically acceptable salts and stereoisomers thereof, which inhibit, regulate and/or modulate tyrosine kinase signal...
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7582655 |
Antineoplastic compounds
The present invention relates to 4-piperidone derivatives represented by the following formula (I) and the acid addition salts thereof.
The method of preparation and antineoplastic activity of...
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7576101 |
Composition for and treatment of demyelinating diseases and paralysis by administration of remyelinating agents
The application provides for methods and compositions for inhibiting demyelination, promoting remyelination and/or treating paralysis in a subject in need thereof. Preferably, such compositions...
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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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7569585 |
1, 5-diaminopentan-3-ol compounds and related treatment methods
Substituted 1,5-diaminopentan-3-ol compounds and methods of making the same. Pharmaceutical compositions containing these compounds and methods of treatment using these pharmaceutical compositions.
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7560483 |
Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require...
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7550485 |
Substituted N-heterocycle derivatives and methods of their use
The present invention is directed to substituted N-heterocycle derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions...
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7547693 |
Piperidine derivative
Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty...
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7541369 |
Amino-derivatives as novel inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I)
wherein n, m, t, R 1 , R 2 , L, Q, X, Y, Z and
have defined meanings, having histone deacetylase inhibiting enzymatic activity;...
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7534788 |
Benzofuran and benzothiophene-2-carboxylic acid amide derivatives
The present invention relates to compounds of formula I
wherein X, A and R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds...
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7514431 |
Piperidinyl cyclopentyl aryl benzylamide modulators of chemokine receptor activity
The present invention is directed to compounds of the formula I: I (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X, Z and n are defined herein) which are useful as modulators of chemokine receptor...
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7495013 |
Chemical compounds
The present invention relates to compounds of formula (I):
The variables recited in formula (I) are defined in the specification. The present invention also relates to processes of preparing...
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7482364 |
Phenylalkynes
Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
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7482363 |
Piperidine derivatives useful as modulators of chemokine receptor activity
The present invention provides a compound of formula (I), wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of...
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7476681 |
17β-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
In its many embodiments, the present invention provides a novel class of compounds as illustrated below, wherein the various moieties are described herein, as inhibitors of type 3...
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7449480 |
Small molecule inhibitors of HER2 expression
Peptide mimetic small molecule inhibitors of Sur-2 are provided having the general formula:
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7432268 |
17β-hydroxysteroid dehydrogenase type 3 inhibitors for the treatment of androgen dependent diseases
There are disclosed compounds of the formula (I):
prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3...
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7419990 |
Piperidine derivatives as melanocortin-4 receptor agonists
Certain novel 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 therefore...
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7399771 |
Piperidine derivatives as CCR5 inhibitors
Disclosed are compounds of formula I:
wherein R 1 , R 2 , R 3 and X are as defined herein, in free or salt form, which are useful as CCR5 inhibitors, e.g. in the prevention or treatment of...
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7368461 |
Compounds and method for the treatment of overactive bladder
NK2R binding compounds in accord with structural diagram I useful for the treatment or prevention of OAB or UI in mammals, particularly humans are disclosed:
wherein in said compounds D, A, R 1...
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7361682 |
Indole derivatives as H3 inverse agonists
The present invention relates to compounds of formula I:
wherein X, R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof,...
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7354919 |
Isoxazole compositions useful as inhibitors of ERK
Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula:
where A, B, R 1 , R 2 , T and Ht are described in the...
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7348324 |
Cyclic amine compounds as CCR5 antagonists
A compound of formula (I) (wherein R 1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R 2 is a hydrocarbon group...
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7317066 |
Liquid crystal polymers
Liquid crystal polyester derived from phenylene-naphthalene monomers and one or more comonomers display an improved balance of properties, including low melt viscosity, fast cycle time in molding,...
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7307090 |
Piperidine derivatives useful as modulators of chemokine receptor activity
The invention provides a compound of formula (I), wherein: T is C(O) or S(O) 2 ; W is C(O) or S(O) 2 ; X is CH 2 , O or NH; Y is CR 5 or N; R 1 is optionally substituted aryl or optionally...
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7304076 |
Neuropeptide Y Y5 receptor antagonists
The present invention discloses compounds which, are novel receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses...
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7297706 |
Certain glycine derivatives as factor Xa inhibitors for use in the treatment of thrombotic disorders
Compounds of formula (I)
in which R, R 1 , R 2 , n and X 1 have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.
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7297693 |
Nitrogen-containing heterocyclic compounds and their use as Raf inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac...
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7279491 |
Phenylpiperidines and phenylpyrrolidines
Substituted phenylpiperidines and phenylpyrrolidines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
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7279490 |
Ophthalmic compositions for treating ocular hypertension
This invention relates to selective m1 muscarinic agonist, their use or a formulation thereof in the treatment of glaucoma and/or other conditions which are related to elevated intraocular pressure...
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7253186 |
N-substituted piperidine derivatives as serotonin receptor agents
Disclosed herein are compounds of Formula I,
or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine...
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7241778 |
Non-imidazole aryloxypiperidines
Substituted non-imidazole aryloxypiperidine compounds, compositions containing them, and methods of making and using them to treat or prevent histamine-mediated conditions.
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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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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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7223759 |
Antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds
The invention relates to antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds and pharmaceutical compositions thereof. This invention also relates to a method of...
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RE39608 |
Substituted benzimidazoles and their use as PARP inhibitors
Compounds of the formula Ia or IB
where
A is a saturated or monounsaturated heterocyclic, 4 - to 8-membered ring which contains one or two nitrogen atoms,
and their tautomeric forms,...
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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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7192973 |
Piperidine derivatives and their use as modulators of chemokine receptor activity (especially CCR5)
Compounds of formula (I): wherein L is CH or N; M is CH or N; provided that L and M are not both CH; compositions comprising them, processes for preparing them and their use in medical therapy (for...
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7183274 |
Piperidine-2,6-diones heterocyclically substituted in the 3-position
Piperidine-2,6-diones heterocyclically substituted in the 3-position corresponding to formula I
Also the production and use of such compounds in pharmaceutical formulations and related methods...
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7176236 |
Water-soluble etoposide analogs and methods of use thereof
Etoposide analogs with improved water-solubility such as 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-n
itroanilino)-4-desoxy-podophyllotoxin (8) and...
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7169795 |
Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia–If:
or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic...
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7141560 |
Alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics
The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I
The invention also relates to pharmaceutical compositions comprising said derivatives,...
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7122551 |
Metalloproteinase inhibitor compounds
Compounds of the formula I
useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.
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7115644 |
Heterocyclic compounds
Disclosed are benzimidazolone compounds of formulas (I) & (II): wherein R 1 , R 2 , R 3 , R 4 , R 5 , X, L, m, n and t are defined herein. The compounds inhibit production of cytokines...
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7115635 |
Benzylpiperidine compound
The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral...
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