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7625902 |
Imidazolidinone derivatives
The invention is concerned with novel imidazolidinone derivatives of formula (I):
wherein R 1 to R 11 and X are as defined in the description and in the claims, as well as physiologically...
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7625889 |
Substituted bis aryl and heteroaryl compounds as selective 5HT2A antagonists
The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I):
Wherein X, Y, Z, A, B, D, Ar, R 1 and R 2 are as defined herein. The compounds of...
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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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7622056 |
High dielectric anisotropy liquid crystal compound and composition containing the same
The invention relates to a high dielectric anisotropy liquid crystal compound which is a pyridyl derivative with substituents of electrons push-pull effect. Furthermore, the high dielectric...
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7615550 |
Substituted piperazines,(1,4) diazepines, and 2,5-diazabicyclo (2.2.1)iieptanes as histamine H1 and/or H3 antagonists or histamine H3 reverse antagonists
The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the...
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7598250 |
Cyclic amine BACE-1 inhibitors having a heterocyclic substituent
Disclosed are novel compounds of the formula
or a pharmaceutically acceptable salt or solvate thereof, wherein
R 1 is
X is —O—, —C(R 14 ) 2 — or —N(R)—; Z is...
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7595319 |
Compounds having selective inhibiting effect at GSK3
Selective phenyl substituted aminopyrazine inhibitors of GSK3 useful for the prevention and/or treatment of cognitive disorders.
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7595314 |
Benzoyl-piperazine derivatives
A compound of formula
wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia,...
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7572786 |
Substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives and their use as neurokinin antagonists
This invention concerns substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity, a combined NK 1 /NK...
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7550469 |
Heterocyclic amide derivatives and their use as dopamine D3 receptor ligands
The invention relates to heterocyclic substituted amide derivatives that display selective binding to dopamine D 3 receptors. In another aspect, the invention relates to a method for treating...
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7544683 |
Cyclohexyl derivatives
The present invention relates to compounds of formula I
wherein R 1 and R 2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are...
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7491821 |
Inhibitors of P2X3
Compounds of formula 1 are modulators of P2X3 useful for the treatment of pain and genitourinary, gastrointestinal, and respiratory disorders:
wherein
R 1 is —C(═S)CH 3 , pyridyl,...
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7462617 |
Substituted acylpiperazine derivatives
The invention relates to compounds of formula
wherein the substituents are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof.
The invention further...
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7456180 |
Piperazine derivatives and their use as therapeutic agents
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula...
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7452891 |
MCH antagonists and their use in the treatment of obesity
The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention...
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7449576 |
Substituted piperazines
Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1....
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7449468 |
Thiazole and oxazole derivatives as activators of human peroxisome proliferator activated receptors
The present invention provides a compound of formula (I):
wherein R 1 -R 5 , R 25 , R 26 , Y, y, and X 2 are as defined herein. The compounds activate human peroxisome proliferater...
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7449460 |
3-Quinolinecarbonitrile protein kinase inhibitors
This invention provides a compound of Formula 1
where Ar, X, R 1 , R 2 , R 3 , and R 4 are defined herein, or a pharmaceutically acceptable salt thereof useful in the prevention or inhibition...
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7435736 |
Substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine derivatives and their use as neurokinin antagonists
The invention concerns substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine having neurokinin antagonistic activity, in particular NK 1 and NK 1 /NK 3 -antagonistic activity, their preparation,...
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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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7432264 |
Antimicrobial biaryl compounds
Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain.
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7427612 |
Benzoyl-piperazine derivatives
A compound of formula
wherein the substituents are as described in the specification for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia,...
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7423058 |
Inhibitors of hepatitis C virus NS3 protease
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses...
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7423039 |
(4-phenylpiperazin-1-yl)acylpiperidine derivatives, preparation thereof and application of same in therapeutics
The invention relates to substituted (4-phenylpiperazin-1-yl)acylpiperidine derivatives of formula (I)
in the form of a base or an addition salt with an acid, and also in the form of a hydrate...
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7414047 |
Piperazinyl and diazapanyl benzamides and benzthioamides
Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
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7405217 |
N-aroyl piperazine derivatives as orexin receptor antagonists
This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals.
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7396830 |
Piperazine amidines as antiviral agents
This disclosure provides compounds of Formula I
as described herein having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure...
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7381719 |
Diaryl ethers as opioid receptor antagonist
A compound of the formula (I) wherein the variables X 1 to X 10 , R 1 to R 7 including R 3′ , E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer,...
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7378422 |
Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life...
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7365073 |
3-(heteroaryl) alanine derivatives-inhibitors of leukocyte adhesion mediated by VLA-4
Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a...
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7354924 |
Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
This invention provides Compounds I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl...
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7351822 |
Serine protease inhibitors
Compounds of formula (I)
in which R 2 , X, Y, Cy, L and Lp(D) n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment...
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7342041 |
3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis C virus NS3 serine protease
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses...
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7319099 |
Benzoyl-piperazine derivatives
The invention relates to compounds of formula
wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such...
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7317013 |
Cyclic pyrazinoylguanidine sodium channel blockers
The present invention provides sodium channel blockers represented by formula (I):
where the structural variables are defined herein. The compounds of the present invention may be used for...
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7307081 |
Piperidine derivatives useful as CCR5 antagonists
The present invention provides a compound of the formula
or a pharmaceutically acceptable salt or solvate thereof, wherein the various moieties are as defined in the specification. The present...
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7262197 |
Phospholipase C inhibitors for use in treating inflammatory disorders
This invention is directed to heterocyclyl-substituted anilino phospholipase C inhibitor compounds useful in treating or ameliorating an inflammatory disorders and/or restenosis of the general...
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7253168 |
Substituted 1-benzyl-4-substituted piperazine analogues
Compounds of Formula I are provided, in which variables are as described herein:
Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly...
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7244722 |
Amino-substituted 1H-pyrazin-2-ones and 1H-quinoxalin-2-ones
Compounds of the general formula (I):
wherein m, n, 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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7241758 |
Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological...
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7238693 |
Aryl carbamate derivatives, preparation and use thereof
The present invention relates to novel compounds, the preparation and use, particularly therapeutic, thereof. More specifically, it relates to compounds derived from aryl carbamates, the...
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7238688 |
Piperidine compounds
Disclosed are novel compounds of the formula
Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or...
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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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7229998 |
Thiazole and oxazole derivatives as activators of human peroxisome proliferator activated receptors
The present invention provides a compound of formula (I):
wherein R 1 –R 5 , R 25 , R 26 , Y and X 2 are as defined herein. The compounds activate human peroxisome proliferator...
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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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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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7176311 |
Process for preparing pharmaceutically active compounds
A process for the preparation of Compounds of the formula (1):
wherein R 1 , R 2 , R 4 and R 13 are as defined or a pharmaceutically or veterinarily acceptable salt or polymorph thereof, or a...
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7163948 |
Heterocyclic substituted 1,4-dihydri-4ox9-1,8-naphthyridine analogs
The present invention relates to 1,4-dihydro-4-oxo-1,8-napthpyridine analogs of the formula
and pharmaceutically acceptable salts, esters, and prodrugs thereof, wherein A, X, W and Y are...
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7153858 |
Arylpiperazinyl compounds
The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formulae I: and II, and synthesis and uses of those compounds for treating...
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7153856 |
Cyclic protein tyrosine kinase inhibitors
Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders...
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