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7312221 |
Inhibitors of macrophage migration inhibitory factor and methods for identifying the same
Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF...
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7307089 |
Aryloxy quinolines and uses thereof
Compounds of Formula 1
and pharmaceutically acceptable salts thereof, wherein m, Ar, R 1 , R 2 , and R 3 are as defined herein. The invention also provides methods for preparing, coompositions...
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7301024 |
Crystalline forms of gatifloxacin and processes for preparation
Provided are novel crystalline forms of gatifloxacin, some of which are DMSO solvates, and methods for making them.
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7300939 |
Substituted 1-propiolylpiperazine compounds, their preparation and use
Substituted 1-propiolylpiperazine compounds corresponding to formula I
in which X denotes N or C—R 2 , and n is an integer from 0 to 8, a method for producing such substituted...
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7291619 |
Melanocortin receptor agonists
The present invention relates to melanocortin receptor agonists of formula (I), which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction
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7282585 |
Salt and crystalline forms of (2R)-anti-5-{3-[4-(10,11-difluoromethanodibenzosuber-5-yl)piperazin-1-yl]-2-hydroxypropoxy}quinoline
The present invention provides novel salt and hydrate crystal forms of (2R)-anti-5-{3-[4-(10,11-difluoromethano-dibenzosuber-5-yl)p
iperazin-1-yl]-2-hydroxypropoxy}quinoline 2.5 hydrochloride.
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7279481 |
Quinoline and quinazoline derivatives having affinity for 5HT1-type receptors
Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided:
wherein R 1 , m, X, R 2 , n, W, p, Y, Z, R 3 , R 4 , R 5 and q have the meanings as defined in the...
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7276603 |
Benzofuranyl-and benzothienyl-piperazinyl quinolines and methods of their use
Benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such compounds are disclosed. Methods of using benzofuranyl- and benzothienyl-piperzinyl quinoline...
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7276508 |
Indole derivatives useful for the treatment of CNS disorders
The present invention relates to dopamine D 4 ligands having the general formula I
wherein R 1 -R 10 , W, X, Y 1 -Y 4 , and n are as described herein.
The compounds of the invention are...
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7265116 |
Aryl and heteroaryl substituted tetrahydroisoquinolines and use thereof
Provided herein are compounds of the formula (I):
wherein R 1 -R 8 are as described herein, R 4 being phthalazinyl, pyrazinyl, pyridazinyl, or quinoxalinyl. Such compounds are particularly...
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7232826 |
Tyrosine kinase inhibitors
The present invention provides compounds of Formula I or II that are useful as anti-cancer agents and other diseases that can be treated by inhibiting tyrosine kinase enzymes
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7230106 |
Process for the preparation of inhibitors of macrophage migration inhibitory factor
Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF...
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7229997 |
Compounds and their use
Compounds of the general formula (I):
wherein R 1 , R 2 , R 3 and R 4 are as described in the specification.
Further included are pharmaceutical compositions comprising the...
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7214679 |
Piperidine/piperazine-type inhibitors of p38 kinase
Compounds of the formula:
wherein the substituents are as defined herein are useful for treating conditions mediated by p38 kinase.
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7214674 |
Heterocyclymethylpiperidines and -piperazines possessing affinity at 5ht-1 type receptors
Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed:
wherein: A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl,...
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7202249 |
Antagonists of chemokine receptors
Compounds are provided which are antagonists of chemokine receptor activity. The compounds thereof have the structure
including enantiomers, diastereomers, tautomers, pharmaceutically...
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7196080 |
Phenylpyridinecarbonylpiperazinederivative
The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. ...
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7196088 |
Substituted tetrahydroisoquinolines and uses thereof
The invention provides compounds of the formula:
and pharmaceutically acceptable salts or prodrugs thereof, wherein, n, X, Y, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. The subject...
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7186715 |
Piperazine- and piperidine-derivatives as melanocortin receptor agonists
The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction
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7176313 |
Anti acid-fast bacterial agent containing pyridonecarboxylic acids as active ingredient
An anti acid-fast bacterial agent containing, as an active ingredient, a pyridonecarboxylic acid derivative represented by the following general formula (1), a salt thereof, or a hydrate thereof,...
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7176206 |
Antibiotics
The invention provides compounds of the general formula:
wherein
X is selected from the group consisting of oxygen, sulfur and nitrogen-containing groups selected from azine, oxime,...
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7173035 |
Arylsulfonamide compounds
The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the...
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7169788 |
Tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to...
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7163949 |
4-phenyl substituted tetrahydroisoquinolines and use thereof
Provided herein are compounds of the formulae IA–IF. These compounds are tetrahydroisoquinolines of the following structure:
wherein R 1 –R 8 for compounds of each of the formulae IA, IB,...
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7160886 |
Acylated piperazine derivatives as melanocortin-4 receptor agonists
Certain novel N-acylated piperazine 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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7160888 |
[1,8]naphthyridin-2-ones and related compounds for the treatment of schizophrenia
This invention relates to compounds of the formula 1
wherein G, D, A, Z, Q, X, Y, R 1 , and R 4 through R 7 are defined as in the specification, processes for preparing the same and...
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7157577 |
5-sulfonamido-substituted indolinone compounds as protein kinase inhibitors
The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating...
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7157463 |
Substituted piperidines/piperazines as melanocortin receptor agonists
The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction
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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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7135466 |
Quinoline and quinazoline derivatives and drugs containing the same
There are provided compounds which can be used in the treatment of diseases mediated by the autophosphorylation of a PDGF receptor, specifically, compounds which can inhibit neointima formation...
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7135473 |
Cyclic diamine compound with condensed-ring groups
A cyclic diamine compound of formula (1):
wherein R 1 and R 2 are individually a hydrogen atom or a methoxy group, provided R 1 is a methoxy group when R 2 is a hydrogen atom, or a hydrogen...
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7132539 |
Melanocortin receptor ligands
The present invention relates to compounds which comprise a nitrogen-containing ring scaffold substituted by an R 1 alkyl units selected from the group consisting of C 1 –C 12 linear or...
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7129261 |
Cytotoxic agents
The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming...
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7125870 |
Isoxazoline derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme
The present application describes novel isoxazoline of formula I or II:
or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, R 1 , R 2 , R 3 , R 4 , Z, U, X, Y, Z a , and n...
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7125876 |
Substituted heterocyclic compounds
Disclosed are novel heterocyclic compounds having the structure
which are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and...
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7115607 |
Substituted piperazinyl amides and methods of use
Selected substituted piperazine compounds of Formula I
are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds,...
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7109338 |
1,2-disubstituted 1,4-dihydro-4-oxoquinoline compounds
The present invention relates to substituted 1,4-dihydro-4-oxoquinolines having antiviral activity. The substituents are present at positions 1, 2 and at least one of 5-8 positions of the quinoline...
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7105519 |
Inhibitors of macrophage migration inhibitory factor and methods for identifying the same
Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF...
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7101886 |
Phenylalkyl and pyridylalkyl piperazine derivatives
This invention relates to compounds of the formula 1
wherein R 1 , R 3 , R 4 , X 1 , and X 2 are defined as in the specification, pharmaceutical compositions containing them and their use in...
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7101881 |
Tetrahydroquinolines
The present invention relates to compounds of formula I
wherein X and Y are as defined in the specification, and to pharmaceutical compositions comprising the compound of formula I and a...
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7094895 |
Tyrosyl derivatives and their use as P2X7 receptor modulators
The present invention relates to compounds of the formula
wherein R 1 and R 2 are independently hydrogen, C1–C4 alkyl, C1–C4 substituted alkyl, C1–C4 alkoxy, C1–C4 substituted...
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7087609 |
3-(pyridinyl-piperazin-1-yl)-phenylethyl amides as potassium channel openers
The present invention provides piperazinyl phenylethyl amides and related derivatives having the general Formula I
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A and B are as defined in the...
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7087610 |
Benzothiazole antiviral agents
The invention encompasses a series of benzothiazole compounds which inhibit HIV entry and are useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions...
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7074796 |
4-phenyl-1-piperazinyl, -piperidinyl and -tetrahydropyridyl derivatives
The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I
wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C...
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7067513 |
Phenylpiperazines
The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D 2 receptor and/or the serotonin reuptake site,...
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7049309 |
3-Thia-4-arylquinolin-2-one potassium channel modulators
This invention describes compounds of Formula (I) which are modulators of potassium channels and are useful for treating conditions affected by abnormal potassium channel activity including...
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7041664 |
2-aminoquinolinecarboxamides: neurokinin receptor ligands
Disclosed are compounds of the formula:
or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof,
wherein R 1 , R 2 , R 3 , X, Q 1 and Q 2 are defined herein,
...
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7037913 |
Bicyclo 4.4.0 antiviral derivatives
This invention provides compounds of Formula I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido...
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7030241 |
Mesylates of piperazine derivatives and process for their preparation
The invention relates to the mesylates of a group of piperazine derivatives and to a process for the preparation of these mesylates in an economic way in the high yield and of high purity....
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7026314 |
Therapeutic chromone compounds
Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating,...
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