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7388008 |
Lysine based compounds
The present invention provides lysine based compounds of the formula;
and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R...
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7378448 |
Diphenylether amide derivatives as opioid receptor antagonists
A compound of the formula (I) wherein the variables X 1 , X 2 , B, D, R 1 to R 7 including R 3′ , p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer,...
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7378409 |
Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis,...
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7351703 |
Sulfonylamino carboxylic acid N-arylamides as guanylate cyclase activators
The present invention relates to compounds of the formula I
in which A 1 , A 2 , R 2 and R 3 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds for...
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7307078 |
Polycyclic compounds which modulate PPARγ type receptors and cosmetic/pharmaceutical compositions comprised thereof
Novel polycyclic compounds having the structural formula (I) below:
are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology,...
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7285565 |
Benzamides and related inhibitors of factor Xa
Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or...
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7279477 |
Malonyl-CoA decarboxylase inhibitors useful as metabolic modulators
The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating...
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7214701 |
Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising
(a) compounds of the formula (I)
in which W, X, Y, Z, A, B, D and G...
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7183279 |
Histogranin-like peptides and non-peptides, processes for their preparation and uses thereof
The invention relates to new basic amino acid derivatives of general formulae I, II and III, and the preparation and use thereof in treatment of pain. The compounds have histogranin-like...
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7144911 |
Anti-inflammatory medicaments
Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein...
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7125871 |
Excitatory amino acid receptor modulators
Compounds of the formula (I) in which R 1 , R 2 and X 1 have the meanings given in the specification, modulate metabotropic glutamate receptor function and are useful in treating disorders of the...
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7125869 |
Polycyclic compounds which modulate PPARγ type receptors and cosmetic/pharmaceutical compositions comprised thereof
Novel polycyclic compounds having the structural formula (I) below:
are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology,...
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7109243 |
Inhibitors of cathepsin S
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at...
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7101882 |
Morpholin-acetamide derivatives for the treatment of inflammatory diseases
The present invention relates to novel morpholin-acetamide compounds of formula (I) useful for the treatment of inflammatory diseases. Compounds of formula (I)
wherein R 1 , R 2 , R 3 , R 4 ,...
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7087604 |
Cyclic derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis,...
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7074786 |
Histogranin-like peptides, processes for their preparation and uses thereof
The invention relates to new basic amino acid derivatives of general formulae I, II and III, and the preparation and use thereof in treatment of pain. The compounds have histogranin-like...
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7060718 |
Arylsulfonanilide ureas
The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as...
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7053071 |
Induction of apoptosis in cancer cells
The present invention provides compounds that are inducers or inhibitors of apoptosis or apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical...
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7030111 |
Compounds that abrogate DNA-damage-induced cell cycle G2 checkpoint and/or augment the anti-cancer activity of DNA damaging treatments
The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically,...
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7019003 |
Peptide deformylase inhibitors
Novel PDF inhibitors and novel methods for their use are provided.
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7001905 |
Substituted diarylamines as MEK inhibitors
Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C 1-6 alkoxy, or NR 6 OR 7 ; X is OR 12 , NR 13 R 12 , or NR 14 ; inhibitors of MEK and...
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6992095 |
Stilbene compounds comprising an adamantyl group, compositions and methods thereof
The invention relates to novel stilbene compounds having the general formula (I):
as well as to pharmaceutical compositions for use in human or veterinary medicine, including dermatological,...
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6984652 |
Gyrase inhibitors
Compounds comprising an indazolyl group and a thiazolyl group, preferably 7-substituted 3-(thiazol-2-yl)-1H-indazole compounds in which the indazolyl group and a thiazolyl group are each...
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6982263 |
Nitriles useful as reversible inhibitors of cysteine proteases
Disclosed are novel nitrile compounds of formula (I) further defined herein, which compounds are useful as reversible inhibitors of cysteine proteases such as cathepsin K, S, F, L and B. These...
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6903092 |
Naphthamide neurokinin antagonists for use as medicaments
Compounds having the general formula
wherein R 1 , R 2 , R 3 , R 4 , R 5 , X 1 and X 2 are as defined in the specification, methods of using such compounds for the treatment of diseases and...
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6878706 |
Cyanamides useful as reversible inhibitors of cysteine proteases
Compounds according to the following formula (I):
wherein the variables Q and R 1 to R 6 are as described herein, which reversibly inhibit the cysteine proteases, such as cathepsins K, S, F,...
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6803370 |
Alpha amino acid derivatives—inhibitors of leukocyte adhesion mediated by VLA-4
Disclosed are certain alpha amino acid compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such...
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6723753 |
Substituted n-benzyl-n-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer...
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6696442 |
Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof
This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof,...
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6649616 |
Substituted phenylcyclohexanecarboxamides and their use
The present invention relates to substituted phenylcyclohexanecarboxamides of the formula (I) to processes for their preparation and to their use in medicaments, in particular for the prevention...
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6638930 |
Morpholine and thiomorpholine tachykinin receptor antagonists
Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium...
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6632816 |
Aromatic derivatives as HIV aspartyl protease inhibitors
The present invention provides HIV aspartyl protease inhibitors of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof,...
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6596752 |
Inhibitors of α4β1 mediated cell adhesion
The present invention relates to small molecules according to the formula [I]: which are potent inhibitors of α 4 β 1 mediated adhesion to either VCAM or CS-1 and which can be used for...
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6566308 |
Emulsifiable concentrate containing one or more pesticides and adjuvants
The invention relates to a stable emulsifiable concentrate (EC) for crop protection active compounds which comprises (a) one or more crop protection active compounds, (b) 150 to 500 g/l of one or...
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6531471 |
Morpholinone and morpholine derivatives and uses thereof
This invention is directed to morpholinone and morpholine derivatives which are selective antagonists for human α 1a receptors. This invention is also related to uses of these compounds for...
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6525099 |
N-substituted sulfonamide derivatives
The present invention provides certain N-substituted sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of...
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6509337 |
Arylsulfonyl Hydroxamic Acid derivatives as MMP and TNF inhibitors
A compound of the formula wherein R 1 -R 9 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration,...
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6506750 |
Morpholine derivatives, method for the production thereof and pharmaceutical preparations containing said derivatives
N-(phenylacetyl)morpholine derivatives useful as NK1 receptor antagonists, a process for the preparation thereof, and pharmaceutical compositions containing them as active principle.
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6479518 |
Zwitterionic tachykinin receptor antagonists
The present invention is directed to certain novel compounds represented by structural formula I: or a pharmaceutically acceptable salt thereof, wherein R 3 , R 5 , R 6 , R 7 , R 8 , R 11 , R 12...
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6479491 |
Disubstituted morpholine, oxazepine or thiazepine derivatives, their preparation and their use as dopamine d4 receptor antagonists
The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R 1 , R 2 , R 3 , R 4...
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6444618 |
Crop protection emulsifiable concentrate containing defoaming agents
The novel emulsifiable concentrate (EC) formulation comprising at least one pesticidal crop protection active compound, at least one non-polar organic solvent, optionally, at least one polar...
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6436934 |
Fungicide mixtures based on amide compounds and morpholine or piperidine derivatives
Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR 1 R 2 I in which A, R 1 and R 2 are as defined in the description, and b) dimethomorph or...
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6387901 |
Alkyne containing metalloproteinase inhibitors
The present invention relates to alkyne containing metalloproteinase inhibitors of the formula wherein n, X, and R 1 -R 9 are as defined in the specification, and to pharmaceutical compositions...
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6376531 |
Method of treatment using deuterium compounds
The present invention provides organic deuterium compounds which can be therapeutic compounds to treat manic depression. In particular, the present invention relates to deuterated methionine,...
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6376468 |
Protein:prenyl transferase inhibitors
The invention pertains to novel peptide analogs suitable for inhibiting protein:prenyl transferases. As such they are therapeutically useful in e.g. inhibiting oncogenesis and other unwanted cell...
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6362174 |
Reduced dipeptide analogues as calcium channel antagonitsts
The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke,...
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6326369 |
Bicyclic quinone compounds, their production and use
A compound of the formula: ##STR1## wherein R 1 and R 2 each represents a lower alkyl, or R 1 and R 2 may be bonded together to form a ring; X represents a spacer of which the number of atoms...
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6323202 |
HSV primase inhibitors
The invention provides compounds of the formula 1 that are active against the HSV primase enzyme: ##STR1## wherein R 1 is hydroxy or amino; R 2 is hydrogen, halo, (C 1 -4)alkyl or (C 1...
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6313121 |
Microbicides
Metalaxyl having a high content of R-enantiomer of more than 70% by weight, or pure R-metalaxyl, in admixture with 4-[3-(4-chloropheny)-3-(3,4-dimethoxyphenyl)acryloyl]morphol
ine ("dimethomorpho")...
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6294531 |
Calcilytic compounds
Novel arylalkylamino compounds exhibiting calcilytic properties are provided.
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