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7390812 |
N, N'-disubstituted piperazine compounds and their use as analgesics
N,N′-disubstituted piperazine compounds, processes for the production thereof, and pharmaceutical preparations containing these compounds. The use of N,N′-disubstituted piperazine compounds for...
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7384944 |
Piperazine derivatives useful as CCR5 antagonists
The use of CCR5 antagonists of the formula
or a pharmaceutically acceptable salt thereof, wherein
R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R 1 is hydrogen or...
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7384943 |
Substituted chroman derivatives
The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives having the formula (I)
wherein
X is N; Y is NR 2 CH 2 , CH 2 NR 2 , NR 2 CO, CONR...
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7384939 |
Process for preparation of pyridine derivatives of NK-1 receptor antagonist
The present invention provides a process for preparing a pyridine compound of the formula:
wherein R 1 , R 2 , R 3 and a are those defined herein.
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7381727 |
Pyrrole derivatives, their preparation and their therapeutic use
The invention concerns compounds of formula (I):
Wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are as defined herein. The invention also concerns the method for preparing said...
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7371747 |
Cyanoalkylamino derivatives as protease inhibitors
The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical...
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7361658 |
2-acylaminothiazole derivative or salt thereof
2-Acylaminothiazole derivatives or salts thereof which have a platelet increasing activity based on an excellent human c-mpl-Ba/F3 cell growth function and a function of accelerating formation of...
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7361654 |
Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity...
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7358253 |
Indolylmaleimide derivatives
Provided are compounds of formula (I)
which are useful in the treatment and/or prevention of diseases or disorders mediated by T lymphocytes and/or PKC, e.g. acute or chronic rejection of organ...
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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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7348347 |
Substituted 4,5,6,7-tetrahydrobenzthiazol-2-ylamine compounds
Substituted 4,5,6,7-tetrahydrobenzothiazol-2-ylamine compounds, a method for their production; pharmaceutical compositions comprising them, and methods of use for modulating biological functions...
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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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7332494 |
Method for treating allergies using substituted pyrazoles
A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.
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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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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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7312211 |
Pryanone compounds useful as reversible inhibitors of cysteine proteases
Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R 2 , R 3 , R 4 , R 6 , R 8 and Y are defined herein. The compounds are useful for...
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7294628 |
Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I)
in which:
n is 1 or 2; R 1 represents a halogen atom; a trifluoromethyl radical; a (C...
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7279475 |
Fluorinated di-aryl urea compounds
Disclosed are compounds of formula(I):
wherein R 1 , R 2 , W and X of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are...
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7279472 |
Compounds useful as reversible inhibitors of cysteine proteases
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune...
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7268139 |
Methods of promoting osteogenesis
The invention is directed to methods of bone healing by administering a p38 MAP kinase inhibitor. The invention is directed to methods of treating bone fractures, bone diseases, bone grafting,...
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7265121 |
Chemical compounds
Compounds of formula (I)
in which R 1 , R 2 and X 4 have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders.
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7253205 |
Gem-disubstituted cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of the formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 represent a variety of substituents, ring A is a phenyl or pyridyl...
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7253172 |
Dipeptidyl peptidase inhibitors for the treatment of diabetes
Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (I) are inhibitors of the dipeptidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of...
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7253171 |
Urea derivatives as integrin α4 antagonists
Novel antagonists of ∝4β1 integrin and/or ∝4β7 integrin of the general Formula I: wherein R1, R2, R5, L1, L2, Rb, W and Z are as defined in any one of claims 1 to 13, A represents...
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7205294 |
Selected CGRP-antagonists process for preparing them and their use as pharmaceutical compositions
The present invention relates to substituted piperidines of general formula
wherein A, B, D, E, X, R 1 and R 2 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers,...
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7196106 |
Cyanothiophene derivatives, compositions containing such compounds and methods of use
The present invention addresses substituted cyanothiophene derivatives of the formula I:
as well as compositions containing such compounds and methods of treatment. The compounds in the present...
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7189725 |
Enantiomerically pure opioid diarylmethylpiperazine as a cardioprotection agent
(−)3-((S)-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)(3-t
hienyl)methyl)phenol and pharmaceutically acceptable esters or salts thereof, in essentially enantiomerically pure form have utility as...
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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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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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7157454 |
Derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and the pharmaceutical compositions containing same
The invention relates to compounds of formula:
These compounds show affinity for the bradykinin receptors with selectivity towards the B 1 receptors; they may be used for the preparation of...
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7153857 |
Arylpiperazines and arylpiperidines and their use as metalloproteinase inhibiting agents
Compounds of the formula I
useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.
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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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7141561 |
Substituted diaryl heterocycles, process for their preparation and their use as medicaments
This invention discloses and claims diary heterocycles of formula (I)
and their pharmaceutically acceptable salts, pharmaceutical compositions thereof, and methods of using said compounds of...
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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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7125887 |
Pyrrolidine modulators of CCR5 chemokine receptor activity
Pyrrolidine compounds of Formula (I), (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6a , R 6b , R 7 and R 8 are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor...
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7115637 |
Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods...
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7115608 |
Pyridinone and pyridinethione derivatives having HIV inhibiting properties
The present invention is concerned among others with compounds of formula (1), the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric...
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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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7094779 |
Piperazine oxime dervatives having NK-1 receptor antagonistic activity
The present invention relates to a group of novel piperazine oxime derivatives having interesting NK-1 antagonistic activity. The invention relates to compounds of the general formula (1) wherein:...
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7094431 |
Method of healing skin wounds in mammals and a composition therefor
This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or...
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7094397 |
Methods and reagents for the treatment of multiple sclerosis
The invention features methods and reagents for the diagnosis, monitoring, and treatment of multiple sclerosis. The invention is based in part on the discovery that Chlamydia is present in...
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7078407 |
4-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them
The present invention relates to 4-hydroxycinnamamide derivatives as antioxidants and pharmaceutical compositions containing them. More particularly, it relates to 4-hydroxycinnamamide derivatives...
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7067517 |
Use of compounds for decreasing activity of hormone-sensitive lipase
Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The...
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7049323 |
Amidoheterocycles as modulators of the melanocortin-4 receptor
Novel azetidinyl and pyrrolidinyl compounds are ligands of melanocortin-4 receptors and are useful for treating conditions responsive to the modulation of melanocortin-4 receptors such as obesity,...
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7045530 |
Spirocyclic quinuclidinic ether derivatives
Compounds of formula (I)
wherein n1 is 0, 1, or 2; n2 is 0, 1, or 2; X is a bond, O, S, or NR 1 ; and Ar 1 is a 5-membered aromatic ring, 6-membered aromatic ring, or a fused...
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7030122 |
1,4-disubstituted piperazine ligands for neurotransmitter receptors
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various...
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7026308 |
Topical anti-microbial compositions
Disclosed are topical compositions for the treatment of microbial infections on the skin or scalp which include a polyvalent metal salt of pyrithione and include a metal ion source. Also disclosed...
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7019007 |
CCR-3 receptor antagonists (I)
The invention provides compounds of Formula (I):
wherein: R 1 –R 4 , A, D, and L have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical...
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7012075 |
Cathepsin cysteine protease inhibitors
This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for...
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7008903 |
Pesticide
The present invention provides a composition comprising synergistic amounts of a compound of the formula (I)
wherein X, E, R, A and Z are as defined herein, and at least one fungicidal active...
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