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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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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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7626040 |
Substituted imidazole compounds as KSP inhibitors
The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with...
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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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7612201 |
Pyrazole compounds
Compounds of formula (IA) or (IB) or a salt, N-oxide, hydrate or solvate thereof are inhibitors of HSP90, and are of value in the treatment of diseases responsive to HSP90 inhibition such as...
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7605162 |
Phenylpiperazine
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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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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7595322 |
Heterocyclic sulfonamides as modulators of cardiac sarcomeres
Certain substituted sulfonamide derivatives of Formula I selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart...
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7595330 |
Benzimidazole thiophene compounds
The present invention provides benzimidazole thiophene compounds pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
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7582635 |
Therapeutic agents useful for treating pain
A compound of formula:
wherein Ar 1 , A, R 3 , x, and m are as disclosed herein and Ar 2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt...
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7572921 |
Substituted benzylimidazoles useful for the treatment of inflammatory diseases
The invention comprises a class of derivatives of substituted benzylimidazoles of the formula (I) and methods for making the same. These compounds are useful for the treatment of inflammatory...
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7557108 |
(Indol-4-yl) or (indol-5-yl)-piperazinylmethanones
The present invention relates to compounds of formula I
wherein one of R 1 and R 2 is hydrogen and the other one is
and wherein A and R 1 to R 4 are as defined in the description and...
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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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7547698 |
Bicyclic heterocyclic derivatives and their use as inhibitors of stearoyl-coadesaturase (SCD)
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise, for example, administering to a mammal in need thereof a...
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7514436 |
Pyridazine 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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7479502 |
2-(2-hydroxybiphenyl-3-yl)-1H-benzoimidazole-5-carboxamidine derivatives as factor VIIA inhibitors
The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these...
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7439360 |
Vanilloid receptor ligands and their use in treatments
Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular...
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7420057 |
Stable polymorph of flibanserin
The invention relates to the polymorph A of flibanserin, to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments.
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7414058 |
Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders
There is disclosed a method for the treatment of Extra Pyramidal syndrome (EPS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents...
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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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7381726 |
Polymorphic forms of 1-′4-(5-cyanoindol-3-yl)butyl-4-(2-carbamoylbenzofuran-5-yl)piperazine hydrochloride
The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-y
l)-piperazine, crystalline modification of the...
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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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7351828 |
Benzimidazoles that are useful in treating sexual dysfunction
The present invention relates to the use of compounds of formula (I)
for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual...
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7335660 |
Isochroman compounds for treatment of CNS disorders
This invention relates to compounds of formula (I)
where R 1 to R 12 , —W—V—, —X—Y—, p and n have the values defined in claim 1 , their preparation and use as pharmaceuticals for...
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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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7291642 |
Bradykinin-B1 antagonists, process for their preparation and their use as medicaments
The present invention provides bradykinin-B1 antagonists of the formula
in which A, Ar, G, Q, R 1 and R 4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and...
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7241787 |
Substituted N-cycloexylimidazolinones, process for their preparation and their use as medicaments
The invention relates to substituted N-cyclohexylheterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to processes for their preparation and...
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7223764 |
2,4-bis (trifluoroethoxy)pyridine compound and drug containing the compound
The present invention is directed to a 2,4-bis(trifluoroethoxy)pyridine compound represented by formula (1):
(wherein X 1 represents a fluorine atom or a hydrogen atom) or a salt thereof, and...
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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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7214796 |
Process for production of 1-[2-(benzimidazol-2-yl-thio)ethyl]piperazine or salts thereof
This invention relates to a method for producing 1-[2-(benzimidazol-2-ylthio)ethyl]piperazine (5) or its salt by the following reaction scheme:
This invention enables efficient production 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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7202233 |
Alprazolam inclusion complexes and pharmaceutical compositions thereof
A pharmaceutical composition an inclusion complex and methods for treating patients and preparing said complex disclosed for transmucosal delivery comprising an inclusion complex of (a) alprazolam...
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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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7186724 |
Heterocyclic substituted carbonyl derivatives and their use as dopamine D3 receptor ligands
The invention relates to heterocyclic substituted carbonyl 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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7169775 |
Amino methyl imidazoles as C5a receptor modulators
Amino methyl imidazoles of Formula I are provided:
wherein R, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are defined herein.
Such compounds are ligands of C5a receptors. Preferred compounds of...
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7160912 |
Heterocyclic compounds having antibacterial activity: process for their preparation and pharmaceutical compositions containing them
The present invention relates to novel oxazolidinone compounds of formula (I), their stereoisomers, their salts and pharmaceutical compositions containing them.
The present invention also...
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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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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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7138420 |
Substituted benzimidazole compounds
Disclosed are substituted benzimidazole compounds of formula (I):
wherein R 1 , R 2 , R 3 , R 4 and X a are defined herein. The compounds of the invention inhibit Itk kinase and are therefore...
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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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7132421 |
CIS-imidazoles
The present invention provides compounds according to formula I and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction...
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7125877 |
Benzimidazole derivatives
This invention provides compounds which are represented by a general formula [I]
[in which X stands for hydrogen or halogen; B stands for halogen, cyano or optionally fluorine-substituted lower...
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7119086 |
Phenylsulfonyl-1,3-dihydro-2h-indole-2-one derivatives, their preparation and their therapeutic use
The invention relates to compounds of formula:
and also to the salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, with affinity for and selectivity towards...
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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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7091219 |
Bis-sulfonamide hydroxyethyl-amino retroviral protease inhibitors
Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease...
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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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7056918 |
Benzimidazole anti-inflammatory compounds
The present invention relates to novel triazolo-pyridines of the formula I
wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from...
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7030113 |
Aminobenzimidazoles as selective melanin concentrating hormone receptor antagonists for the treatment of obesity and related disorders
The present invention discloses compounds of formula I
wherein Ar, Z, m, n, p, R 1 and R 8 are herein defined, said compounds being novel antagonists for melanin-concentrating hormone (MCH),...
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7030150 |
Benzimidazole compounds and antiviral uses thereof
The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion...
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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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