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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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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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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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7595320 |
Hydrazinocarbonyl-thieno[2,3-C]pyrazoles, process for preparing them, compositions containing them and use thereof
The present invention concerns hydrazinocarbonyl-thieno[2,3- c ]pyrazoles of formula (I):
wherein R1, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions...
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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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7579352 |
Retinoic acid mimetic anilides
The present invention is concerned with compounds of formula
the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents...
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7569568 |
Cytokine inhibitors
Disclosed are compounds of formula (I)
Where Ar 1 , X, R 3 , R 4 , R 5 and R 6 are defined herein. The compounds of the invention inhibit production of cytokines involved in inflammatory...
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7524848 |
Diaza heterocyclic amide compounds and their uses
Diaza heterocyclic amide derivatives according to Formula (I) have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders:
where R 5 , R 6...
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7514438 |
Melanin concentrating hormone receptor antagonist
Novel compounds, or pharmaceutically-acceptable salts, tautomers or prodrugs thereof, of Formula I
wherein A, W, X, Z, R 1 -R 3 , and R 8 are as defined in the specification, are provided....
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7511046 |
Thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives useful as D4 antagonists
The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D 4 antagonists. Said compounds are useful for the treatment of medical...
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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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7501422 |
Prolinamide-tetrazole derivatives as NK3 receptor antagonists
The present invention relates to a compound of formula I
wherein
R 1 , R 2 , R 3 , and n are as defined herein or to a pharmaceutically acceptable acid addition salt thereof. These...
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7482344 |
Tricyclic steroid hormone nuclear receptor modulators
The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula I in...
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7468371 |
Tricyclic pyrazole kinase inhibitors
Compounds of the present invention are useful for inhibiting protein tyrosine kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of...
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7429659 |
Furan compounds as histamine H3 modulators
Certain furan compounds are histamine H 3 modulators useful in the treatment of histamine H 3 receptor mediated diseases.
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7427620 |
Azole derivative useful as antifungal agents with reduced interaction with metabolic cytochromes
The present invention relates to novel compounds, of the general formula (I), the N-oxide forms thereof, the salts thereof with pharmaceutically acceptable acids and the stereochemical isomers...
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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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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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7384945 |
Indole or benzimidazole derivatives as CB1 inverse agonists
Provided are compounds of the formula I:
and pharmaceutically acceptable salts thereof, processes for making said compounds and pharmaceutically acceptable salts thereof, pharmaceutical...
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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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7354923 |
Piperazine melanocortin-specific compounds
Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure:
and stereoisomer and pharmaceutically acceptable salts thereof, where X is CH 2 or C═O, R 1 , R 2...
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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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7323480 |
Substituted triazoles as modulators of PPAR and methods of their preparation
The present invention is directed to certain novel triazole compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof. The present invention...
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7320978 |
Oxazole derivatives, preparation and therapeutic use thereof
This invention relates to compounds of formula (I):
Wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as described herein. The invention further relates to a method for prevention...
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7279469 |
Diaminotriazoles useful as inhibitors of protein kinases
The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the...
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7259250 |
C-nitroso compounds and use thereof
A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon,...
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7193084 |
Polymorphic form of itraconazole
The present invention provides a polymorphic form of itraconazole.
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7186827 |
Dipeptide synthesis
Disclosed are processes of making dipeptide compounds of formula(I) as further described in the detailed description section:
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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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7148240 |
Aminoalkoxybenzoyl-benzofuran or benzothiophene derivatives, method for preparing same and compositions containing same
The invention relates to benzofuran or benzothiophene derivatives of general formula:
These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes...
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7119203 |
Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors
This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter...
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7105507 |
Cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and...
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RE39265 |
Heteroarylpiperidines, and their use as antipsychotics and analgetics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a...
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7098212 |
Piperazine derivatives
The present invention relates to compounds of the formula I
and the pharmaceutically acceptable forms thereof; wherein X, Y, a, b, c, d, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein....
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7094778 |
Heterocyclylalkylamines as muscarinic receptor antagonists
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I:
wherein X, Y, and Z are O, S or NR 5 , and the other...
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RE39198 |
Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analgesics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a...
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7064201 |
Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
Compounds represented by the following structure (I) are disclosed:
as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first...
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7049308 |
C-nitroso compounds and use thereof
A C-nitroso compound having a molecular weight ranging from 225 to 1,000 (from 225 to 600 for oral administration) on a monomeric basis wherein a nitroso group is attached to a tertiary carbon,...
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7045520 |
Opioid receptor active compounds
The invention provides compounds of formula I:
wherein R 1 to R 4 and n have any of the meanings defined in the specification and their pharmaceutically acceptable salts. The invention also...
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7026322 |
Phenylahistin and the phenylahistin analogs, a new class of anti-tumor compounds
Methods of using a compound, its pharmaceutically acceptable salts, and/or its pro-drug esters, in isolated form, to treat cancer, and methods for isolating, for formulating, and for administering...
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7019033 |
2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives
Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula
where R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are hydrogen or substituent groups such as alkyl, and...
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6958337 |
Crystalline antifungal polymorph
The crystalline polymorph Form I of...
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6951880 |
Aryl and heteroaryl compounds as antibacterial and antifungal agents
This invention provides novel compounds possessing antibacterial and/or antifungal and/or antitumor activity. Pharmaceutical compositions containing these compounds, methods of making and methods...
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6916927 |
Pyrazolopyrimidinones which inhibit type 5 cyclic guanosine 3′,5′-monophosphate phosphodiesterase (cGMP-PDE5) for the treatment of sexual dysfunction
Compounds of formulae (IA) and (IB) or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein R 1 is C 1 to C...
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6906074 |
2-phenylpiperazine derivatives
A 2-phenylpiperazine derivative represented by the formula (I) or a pharmaceutically acceptable salt, hydrate, or complex thereof:
wherein each of X 1 and X 3 is oxygen or two hydrogen...
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6900206 |
Indole, azaindole and related heterocyclic sulfonylureido piperazine derivatives
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with sulfonylureido...
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6852718 |
Phenylsulphonylipiperazinyl derivatives as 5-HT receptor ligands
A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted piperazine ring are selective antagonists of the human 5-HT 2A receptor and are...
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6818637 |
Polyhydroxypyrazine derivatives, their preparation and the pharmaceutical compositions which comprise them
The invention concerns novel derivatives of formula (I) wherein: R 1 represents the stereoisomeric forms of the chain —(CHOH) 3 —CH 2 —O—COR (II) and either R 2 represents a hydrogen...
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6815550 |
Processes for the preparation of benzotriazole UV absorbers
Provided is a process for preparing 2H-benzotriazole UV absorbers containing a perfluoroalkyl moiety at the 5-position of the benzoic ring, for example a trifluoromethyl group, which involves...
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6815214 |
Pharmaceutical uses and synthesis of diketopiperazines
The synthesis of novel diketopiperazines, their use in inhibiting cellular events such as those involving NFK-α, NFK-β and in the treatment of inflammation events, a combinatorial library of...
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