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7390799 |
Apoptosis promoters
Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than...
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7388007 |
Gamma-lactams as beta-secretase inhibitors
There is provided a series of novel substituted gamma-lactams of Formula (I)
or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 4 , R 5 and R 6 as defined...
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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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7381719 |
Diaryl ethers as opioid receptor antagonist
A compound of the formula (I) wherein the variables X 1 to X 10 , R 1 to R 7 including R 3′ , E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer,...
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7365068 |
Substituted aryl acylthioureas and related compounds; inhibitors of viral replication
The invention provides compounds and pharmaceutically acceptable salts of Formula I
wherein the variables A 1 , A 2 , R 1 , R 2 , V, W, X, Y, and Z are defined herein. Certain compounds 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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7338951 |
Pyridine compounds
This invention features compounds of formula (I):
pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12-related diseases and...
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7338950 |
Amide compounds as ion channel ligands and uses thereof
Compounds are disclosed that have a formula represented by the following:
The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a...
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7332487 |
Nitrogen-containing 5-membered ring compound
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]:
wherein symbols in the formula have the following meanings;
...
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7329652 |
Diaminotriazole compounds useful as protein kinase inhibitors
The present invention relates to inhibitors of protein kinases, particularly to inhibitors of JAK2 and JAK3. The invention also provides pharmaceutical compositions comprising the compounds of the...
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7307090 |
Piperidine derivatives useful as modulators of chemokine receptor activity
The invention provides a compound of formula (I), wherein: T is C(O) or S(O) 2 ; W is C(O) or S(O) 2 ; X is CH 2 , O or NH; Y is CR 5 or N; R 1 is optionally substituted aryl or optionally...
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7300931 |
Compositions for treating cell proliferation disorders
The invention relates to compounds and methods for treating cell proliferation disorders.
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7297693 |
Nitrogen-containing heterocyclic compounds and their use as Raf inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac...
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7291613 |
Inhibitors of p38 kinase
The invention is directed to methods to inhibit p38-α kinase using compounds comprising saturated heterocycles coupled to a fused ring system.
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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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7279470 |
Compounds and uses thereof 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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7276500 |
Substituted amides, their preparation and use
An amide of the formula I
and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the...
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7265112 |
Small molecule modulators of hepatocyte growth factor (scatter factor) activity
The present invention provides compounds having formula (I):
and pharmaceutically acceptable derivatives thereof, wherein R 1 , R 2 and B are as described generally and in classes and...
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7253186 |
N-substituted piperidine derivatives as serotonin receptor agents
Disclosed herein are compounds of Formula I,
or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine...
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7244731 |
6-Methylpyridine derivatives, method for preparing thereof and antiviral pharmaceutical composition comprising the same
The present invention relates to 6-methylpyridine derivatives useful as an antiviral agent. More particularly, the present invention relates to novel 6-methylpyridine derivatives having an...
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7238689 |
Isoxazoline derivative and herbicide comprising the same as active ingredient
An isoxazoline derivative represented by the following general formula [I]:
wherein R 1 and R 2 may be the same or different and are each an alkyl group;
R 3 , R 4 , R 5 and R 6 are...
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7235544 |
3-sulfonylamino-pyrrolidine-2-one derivatives as inhibitors of factor Xa
The invention relates to compounds of formula (I):
wherein substituents are as defined.
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7230017 |
Dihydropyridinone derivatives
The invention relates to novel dihydropyridinone derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases,...
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7229991 |
Substituted 5-aminomethyl-1H-pyrrole-2-carboxamides
5-aminomethyl-1H-pyrrole-2-carboxylic acid amide compounds corresponding to formula I
and processes for the production thereof. Pharmaceutical preparations containing these compounds and the...
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7217707 |
Amide of R-2-(aminoaryl)-propionic acid for use in the prevention of leucocyte activation
N-(2-aminoaryl-propionyl)-amides of formula (1) are described.
The process for their preparation and pharmaceutical preparations thereof are also described. The amides of the invention are...
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7214714 |
20-hydroxyeicosatetraenoic acid production inhibitors
A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof
[wherein R 1 represents a substituted morpholino group, a substituted...
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7186719 |
Antibacterial agents
Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(═O) or the formula: —C(═O)NH(OH); R 1 represents hydrogen, C 1 –C 6 alkyl or C...
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7186718 |
Piperidinyl-morpholinyl derivatives as modulators of chemokine receptor activity
The invention provides compounds of general formula (I), in which m, n, Z 1 , Z 2 , R 1 , R 2 , R 3 , R 4 and R 5 are as defined in the specification; processes for their preparation;...
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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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7179794 |
Multivalent macrolide antibiotics
Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptoramins, tetracycline and/or other compounds which bind to bacterial...
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7169787 |
7-azaindoles, use thereof as phosphodiesterase 4 inhibitors and method for producing the same
The invention relates to new 7-azaindoles, their use as inhibitors of phosphodiesterase 4 and to methods for their synthesis.
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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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7148219 |
Biaryl heterocyclic compounds and methods of making and using the same
The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of...
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7132420 |
Aspartic protease inhibitors
The present invention provides an aspartic proteinase-inhibiting compound of the formula:
wherein a, b, c, d, and e, can be the same or different and each are R 7 , OR 7 , SR 7 , NR 7 R 8 ,...
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7119090 |
Pyrrole substituted 2-indolinone protein kinase inhibitors
The present invention relates to novel pyrrole substituted 2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and...
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7115632 |
Sulfonyl aryl or heteroaryl hydroxamic acid compounds
A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a...
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7109186 |
HIV integrase inhibitors
The present invention describes novel compounds of Formula I which inhibit HIV integrase. The invention also describes compositions and treatments of AIDS or ARC by using these compounds
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7087603 |
Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula IV:
wherein Z 1 or Z 2 is nitrogen, Q is —S—, —O—, —N(R 4 )—, —C(R 6′ ) 2 —, 1,2-cyclopropanediyl,...
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7084139 |
Pyrrolidin-2-one derivatives as inhibitors of factor Xa
The invention relates to compounds of formula (Ic)
processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the...
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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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7074785 |
Δ1-pyrrolines used as pesticides
Novel Δ 1 -pyrrolines of the formula (I)
in which
R 1 , R 2 , R 3 , A, R 4 and m have the meanings given in the description,
a number of processes for preparing these substances, and their...
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7067533 |
Aminophenoxyacetamide derivatives and pharmaceutical composition containing thereof
The present invention relates to an aminophenoxyacetamide derivative of the formula (I):
wherein R 1 to R 4 are, independent from each other, a hydrogen atom or an optionally substituted...
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7060700 |
Amide derivatives useful as inhibitors of the production of cytokines
The invention concerns amide derivatives of formula (I):
wherein R 3 is (1-6C)alkyl or halogeno; Q 1 is heteroaryl which is optionally substituted with 1, 2, 3, or 4 substituents such as...
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7037929 |
2-amino-thiazole derivatives, process for their preparation, and their use as antitumor agents
Compounds which are 2-amino-1,3-thiazole derivatives of formula (I)
wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further...
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7034042 |
N-(4-aryloxypiperidin-1-ylalkyl) cinnamic amides as CCR33 receptor antagonists
Compounds of formula (I) in free or salt form, where Ar 1 is phenyl substituted by one or more substituents selected from halogen, cyano, nitro, and C 1 –C 8 -alkyl optionally substituted by...
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7030114 |
Compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the...
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7019005 |
3 (5)-heteroaryl substituted pyrazoles as p38 kinase inhibitors
A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I
wherein R 1 , R 2 , Ar 1 and HetAr 2 ...
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7008943 |
1-(Pyrrolidin-1-ylmethyl)-3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
The present invention is directed to 1-pyrrolidin-1-ylmethyl-3-(pyrrol-2-ylmethylidene)-2-indolin
one derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical...
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6989381 |
Solution composition of an oxazolidinone antibiotic drug having enhanced drug loading
There is provided a pharmaceutical composition for therapeutic or prophylactic administration to a subject having an infective disease or condition or at risk thereof. The composition comprises an...
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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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