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7612060 |
Triazoles and methods of use
Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically...
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7601837 |
Quinoline derivatives and their use as 5-HT6 ligands
The present invention relates to novel quinoline compounds having pharmacological activity, to processes for their preparation, to compositions containing them and to their use in the treatment of...
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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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7598242 |
Compounds for the treatment of inflammatory disorders
This invention relates to compounds of the Formula (I):
or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions...
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7582762 |
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 methods of treating leukemia comprising administration of a resistance modulating amount of a compound having the formula...
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7582761 |
Vanilloid receptor ligands and their use in treatments
Therapeutic benzimidazoles having the general structure:
and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache,...
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7582638 |
Pyrazole-isoquinoline urea derivatives as p38 kinase inhibitors
The present invention provides kinase inhibitors of Formula (I) wherein R1, R2, and X are as described herein, or a pharmaceutically acceptable salt thereof.
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7576086 |
Aralkyl-alcohol peiperazine derivatives and their uses as antidepressant
Aryl alkanol piperazine derivatives of the formula
and pharmaceutical compositions comprising the same. Also disclosed are methods for treating depression using the pharmaceutical composition....
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7569563 |
Substituted quinolones II
The invention relates to substituted quinolones of formula (I) and to methods for their preparation as well as their use for the production of medicaments for the treatment and/or prophylaxis of...
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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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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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7541357 |
Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
The compounds of the present invention are represented by the chemical structure found in Formula (I):
wherein:
the carbon atom designated * is in the R or S configuration; and X is a fused...
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7531656 |
Synthesis of gatifloxacin
Provided are a method for making (±)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methy
l-1-piperazinyl)-4-oxo-3-quinolenecarboxylic acid, commonly known as gatifloxacin, in high purity, in a...
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7531535 |
Lactam-containing compounds and derivatives thereof as factor Xa inhibitors
The present application describes lactam-containing compounds and derivatives thereof of Formula I:
or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7...
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7528135 |
Pyridine derivatives as H3 antagonists
The present invention relates to compounds of formula I
wherein R 1 , R 2 and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to...
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7507732 |
Cyclopentapyridine and tetrahydroquinoline derivatives
6,7-Dihydro-5H-cyclopenta[b]pyridine and 5,6,7,8-tetrahydroquinoline compounds of Formula (I), including salts, hydrates and solvates thereof, that act as 5-HT 2 receptor ligands and their uses in...
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7504504 |
Methods of preparing aripiprazole crystalline forms
The invention encompasses aripiprazole crystalline forms, methods of preparing the same, and pharmaceutical compositions having aripiprazole crystalline forms.
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7504400 |
MTP inhibiting aryl piperydines or piperazines substituted with 5-membered heterocycles
The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant...
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7501412 |
Isoquinoline compounds and medicinal use thereof
The present invention relates to an isoquinoline compound represented by the following formula (I) or (II), an optically active form thereof, a pharmaceutically acceptable salt thereof, a water...
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7491726 |
Crystalline forms of aripiprazole
The present invention provides novel crystalline forms of aripiprazole and aripiprazole hydrochloride, processes for their preparation and pharmaceutical compositions containing them.
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7482347 |
Piperazine derivatives with CCR-3 inhibiting activity
Compounds of formula I
in free or salt form, wherein Ar, R 1 , R 2 , R 3 , X and T have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3,...
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7476675 |
Quinolinone derivatives and uses thereof
The invention provides compounds of the formula:
and pharmaceutically acceptable salts or prodrugs thereof, wherein m, p, q, r, A, E, X, Y, R 1 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and are as...
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7473692 |
Sulfonamide derivatives as D3-receptor ligands
The present invention relates to new D 3 dopamine receptor subtype selectice ligands of formula (I) to pharmacological compositions containing the same and to their use in therapy and/or...
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7468369 |
Sulfonyl pyrrolidines, method for producing the same and their use as drugs
The invention relates to substituted sulfonylpyrrolidines of the formula I
and to the physiologically tolerated salts thereof, as well as to their use as medicaments.
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7465733 |
Piperazine compounds
A compound selected from those of formula (I):
wherein:
R 1 , R 2 , R 3 and R 4 , which may be the same or different, each represent an atom or group selected from hydrogen, halogen,...
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7459456 |
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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7456196 |
Bicyclic-substituted amines as histamine-3 receptor ligands
Compounds of formula (I)
are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising...
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7456181 |
Aripiprazole crystalline forms
The present invention provides novel crystalline forms of aripiprazole and processes for their preparation.
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7456175 |
Piperazinyl-pyridine derivatives
The present invention relates to compounds of formula I
wherein R 1 , R 2 , X, Y, Z and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as...
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7452888 |
Quinoline derivatives and their use as 5-ht6 ligands
Disclosed are novel quinoline compounds of formula (I), processes for their preparation, compositions containing them and their use in the treatment of CNS disorders.
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7452887 |
Quinoline- and isoquinoline-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof
Quinoline- and isoquinoline-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions...
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7449477 |
7-phenyl-isoquinoline-5-sulfonylamino derivatives as inhibitors of akt (protein kinase B)
The present invention relates to compounds Formula (I) as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.
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7442710 |
Substituted phenyl methanones
The present invention relates to compounds of general formula IA or IB
wherein
X 1 and X 2 are each independently N or C—R″ and R 1 , R 2 ,R 3 , R 4 , R 5 , and R 6 are as defined in...
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7439244 |
Quinoline compounds and pharmeceutical compositions containing them
Disclosed are quinoline compounds of formula (I) having pharmacological activity, processes for their preparation, compositions containing them, and methods for the treatment of CNS and other...
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7439243 |
Piperazinyl-quinoline derivatives useful for the treatment of CNS disorders
Disclosed are quinoline compounds of formula (I) having pharmacological activity, processes for their preparation, compositions containing them, and methods for the treatment of CNS and other...
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7432269 |
Arylpiperaszine derivatives, to the process for the production thereof and to the use thereof as therapeutic agents
The invention relates to compounds of the general formula (I):
to the process for preparing them, and to the use thereof as a therapeutic agent having the property of being selective ligands...
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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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7429585 |
Phenyl-piperazine methanone derivatives, substituted by heterocyclic groups
The present invention relates to compounds of the general formula IC
wherein
R 2 , R′, R″, R 3 , R 6 , X 1 and X 1 ′ are as defined herein and pharmaceutically active acid...
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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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7402583 |
Substituted quinolines as antitumor agents
The invention provides a compound of Formula (Ia),
or a pharmaceutically acceptable salt thereof, a process for t he preparation of a compound of Formula (1 a ) and pharmaceutical compositions...
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7396834 |
4(Phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders
Compounds of general formula: wherein R 1 and R 2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared....
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7388012 |
(Hydrazido)(amino)thiophene compounds
Compounds represented by Formula (I):
or a pharmaceutically acceptable salt or N-oxide thereof, wherein A and J are defined herein, are useful in the treatment of tumors and cancers such as...
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7365077 |
Piperazine bis-amide derivatives and their use as antagonists of the orexin receptor
Disclosed are piperazine bis-amide derivatives useful as antagonists of the orexin receptor and pharmaceutical compositions containing the same.
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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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7332495 |
Aralkyl-ketone piperazine derivatives and their uses as new antalgic or ataractic agent
Arylalkyl ketone piperazine derivatives of the formula:
and pharmaceutical compositions comprising the same. Also disclosed are methods for using the compounds as analgesic and sedative agents....
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7329749 |
Piperazinylcarbonylquinolines and -isoquinolines
Compound of the formula (I) in which R 1 , R 2 and alk are as defined in Claim 1, are potent 5-HT 2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression,...
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7326710 |
Aralkyl formyl-alkyl piperazine derivatives and their uses as a cerebral nerve protective agent
Aralkyl formyl alkyl piperazine derivatives
Pharmaceutical compositions comprising the same, and methods of using them as a neuroprotective agent. Pharmaceutical results indicate that these...
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7314879 |
Melanocortin receptor agonists
The present invention relates to melanocortin receptor agonist of the formula (I): which is useful in the treatment for obesity, diabetes, and male and/or female sexual dysfunction
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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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