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7414046 |
Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I:
or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity....
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7407974 |
Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I):
wherein A, B, C, G, and W 1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are...
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7402606 |
Derivatives of 1-(oxoaminoacetyl) pentylcarbamate as cathepsin K inhibitors for the treatment of bone loss
Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The...
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7396840 |
Chemokine receptor binding heterocyclic compounds
Tertiary amine compounds that bind chemokine receptors such as CXCR4 and CCR5 are disclosed.
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7396838 |
Use of 1H-indol-3-yl-2-oxoacetamide compounds
A method of treating cancer including administering to a subject in need thereof an effective amount of a compound of the formula 1:
wherein R 1 , R 2 , R 3 , R 4 , and n are as defined herein.
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RE40418 |
Treatment of neoplasms with CCI-779/EKB-569 combination
This invention provides the use of a combination of CCI-779 and EKB-569 in the treatment of neoplasms.
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7388012 |
(Hydrazido)(amino)thiophene compounds
Compounds represented by Formula (I):
or a pharmaceutically acceptable salt or N-oxide thereof, wherein A and J are defined herein, are useful in the treatment of tumors and cancers such as...
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7381738 |
Substituted bicycloalkylamine derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I):
or stereoisomers or pharmaceutically acceptable salts thereof, wherein X, Z, a, b, c, d, n, R 1 , R 2 , R 3 , R 4 , R 5 , R...
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7371765 |
Quinoline derivatives having VEGF inhibiting activity
The invention relates to compounds of formula (I) wherein: either any one of G 1 , G 2 , G 3 , G 4 and G 5 is nitrogen and the other four are —CH—, or G 1 , G 2 , G 3 , G 4 and G 5 are all...
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7365081 |
Indole derivatives and their use as medicaments
The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors
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RE40245 |
Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I:
or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase...
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7358261 |
Heteroaryl alkylamide derivatives useful as bradykinin receptor modulators
This invention is directed towards novel alkylamide derivatives as bradykinin receptor antagonists useful for the treatment of bradykinin modulated disorders such as pain, inflammation, asthma and...
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7354934 |
Chemokine receptor binding heterocyclic compounds with enhanced efficacy
The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl...
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7354933 |
Cyclic urea derivatives, preparation thereof and pharmaceutical use thereof as kinase inhibitors
The present invention relates to a cyclic urea compound of formula I:
as defined herein. The invention is also directed to the process for its preparation, pharmaceutical composition comprising...
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7351729 |
JNK inhibitors for use in combination therapy for treating or managing proliferative disorders and cancers
The present invention relates to methods and compositions designed for the treatment, management or prevention of cancer. The methods of the invention comprise the administration of an effective...
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7345058 |
Pyrazoles
Provided herein are compounds of the formula (I):
as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds,...
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7342027 |
1-phenylpiperidin-3-one derivatives and processes for the preparation thereof
Provided are 1-phenylpiperidin-3-one derivatives and pharmaceutically acceptable salts thereof, having cysteine protease inhibitory activity, pharmaceutical compositions containing the same as an...
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7342026 |
Substituted quinolines for the treatment of protozoa and retrovirus co-infections
The invention relates to the use of quinolines having general formula (I), wherein R 1 denotes H; alkyl C 1 -C 15 ; alkenyl or alkynyl C 2 -C 15 ; —CHO; heteroaryl; alkyl C 1 -C 15 or alkenyl...
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7335753 |
Bifunctional heterocyclic compounds and methods of making and using same
The invention provides a family of bifunctional heterocyclic compounds useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The invention also provides methods of...
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7335677 |
Inhibitors of dipeptidyl peptidase IV
Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R 1 is H or CN, X 1 is O, S, CH 2 , CHF, CF 2 ,...
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7332504 |
Heterocyclic substituted aminoazacycles useful as central nervous system agents
Heterocyclic substituted aminoazacyclic compounds of formula I
Z-R 3 I,
...
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7323477 |
7-((1H-imidazol-4-yl)methyl)-5,6,7,8-tetrahydroquinoline
A compound having a structure
or a pharmaceutically acceptable salt, or a prodrug thereof is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also...
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7320992 |
Substituted 2,3-dihydro-1h-isoindol-1-one derivatives and methods of use
Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically...
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7312234 |
Chemokine receptor binding heterocyclic compounds
Tertiary amines containing a multiplicity of heteroaromatic substituents are useful as chemokine receptor modulators.
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7312222 |
Heterocyclic piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
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7312218 |
Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If:
or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic...
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7304066 |
Pyridyl cyanoguanidine compounds
Compounds according to formula (I)
wherein R1 represents hydrogen, halogen or one or more straight or branched, saturated or unsaturated C 1-6 hydrocarbon radical, optionally substituted with...
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7304062 |
Peroxisome proliferator activated receptor alpha agonists
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or...
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7291631 |
CXCR4 chemokine receptor binding compounds
The present invention relates to compounds that bind to chemokine receptors, and having the formula
wherein each A, X, Y, R 1 , R 2 and R 3 are substituents. The present invention also...
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7288559 |
Carboxamide spirohydantoin CGRP receptor antagonists
The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache,...
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7276522 |
4-(substituted cycloalkylmethyl) imidazole-2-thiones, 4-(substituted cycloalkenylmethyl) imidazole-2-thiones, 4-(substituted cycloalkylmethyl) imidazol-2-ones, 4-(substituted cycloalkenylmethyl) imidazol-2-ones and related compounds
The compound of the formula
wherein the * indicates an asymmetric carbon, is specific to alpha 2B adrenergic receptors in preference over alpha 2A and alpha 2C adrenergic receptors, and as...
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7276491 |
Anticoagulant and fibrinolytic therapy using p38 MAP kinase inhibitors
Disclosed are methods for a treating a disease or condition relating to blood coagulation and fibrinolysis using p38 MAP kinase inhibitors.
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7268148 |
Compositions and methods for use against acne-induced inflammation and dermal matrix-degrading enzymes
Acne-affected skin has been found to be accompanied by the presence of matrix-degrading enzymes such as MMPs and neutrophil elastase, induction of neutrophils, and a reduction in procollagen...
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7265115 |
Diazabicyclic CNS active agents
Compounds of formula I:
or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.
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7259157 |
N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
Compounds represented by Formula (I):
or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
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7253170 |
Pyrazole-amine compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I)
useful for treating p38 kinase-associated conditions, where W, X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and m are as...
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7253168 |
Substituted 1-benzyl-4-substituted piperazine analogues
Compounds of Formula I are provided, in which variables are as described herein:
Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly...
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7241745 |
Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I)
as well as methods for their production, medicaments containing these compounds...
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7235566 |
Pyridinone derivatives for treatment of atherosclerosis
Compounds of formula (I):
are inhibitors of the enzyme Lp-PLA 2 and are of use in therapy, in particular for treating atherosclerosis.
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7232833 |
4-substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them
The invention relates to 4-substituted quinoline compounds of general formula:
which are active as antimicrobials, in which:
X 1 , X 2 , X 3 , X 4 and X 5 is C—R′ 1 , to C—R′ 5 ...
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7232832 |
Antibacterial agents
Quinoline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.
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7232817 |
α- and β-amino acid hydroxyethlamino sulfonyl urea derivatives useful as retroviral protease inhibitors
α- and β-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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7226942 |
2-amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor...
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7226940 |
Substituted heterocycles for the treatment of diabetes and other diseases
The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes,...
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7226929 |
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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7223759 |
Antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds
The invention relates to antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds and pharmaceutical compositions thereof. This invention also relates to a method of...
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7223738 |
Inhibitors of Akt activity
The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to...
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7220760 |
Quinoline derivatives as CRTH2 antagonists
The invetion 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 defined in the description, their use as medicament, pharmaceutical...
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7220756 |
N-sulfonylheterocyclopyrrolyl-alkylamine compounds as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of a CNS disorder relating to or affected by the 5-HT6 receptor
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7214690 |
Tricyclic quinolinone and tricyclic quinoline androgen receptor modulator compounds and methods
Novel non-steroidal tricyclic quinolinone and tricyclic quinoline compounds and compositions that are agonists, partial agonists and/or antagonists for androgen receptors (AR), their preparation...
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