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7468443 |
Alkyl ether derivatives or salts thereof
An alkyl ether derivative represented by the general formula:
wherein each of R 1 and R 2 represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl...
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7465718 |
Ansamycins having improved pharmacological and biological properties
Ansamycins and methods of preparing and using the same are described. At least some of these ansamycins exhibit one or more of improved aqueous formulation ability, chemical stability, and...
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7465751 |
1-substituted-3-pyrrolidine derivatives as muscarinic receptor antagonists
This invention generally relates to the derivatives of 1-substituted-3-pyrroli dines having the structure of Formula (I): The compounds of this invention can function as muscarinic receptor...
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7456210 |
Benzyloxy derivatives
The present invention relates to compounds of formula I
wherein R 1 and R 2 are as defined in the specification and to pharmaceutically acceptable salts thereof for the treatment of diseases,...
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7456190 |
Compositions useful as protein kinase inhibitors
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
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7456164 |
3- or 4-monosubtituted phenol and thiophenol derivatives useful as H3 ligands
The invention relates to 3- or 4-monosubstituted phenol and thiophenol derivatives of formula (I) and to processes for the preparation of, intermediates used in the preparation of, compositions...
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7456209 |
IAP binding compounds
IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPs (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in...
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7456202 |
Marked maleimide compounds, method for preparing same and use thereof for marking macromolecules
Fluorine-18-labelled maleimide compounds of general formula (I):
in which:
m represents an integer from 0 to 10; n represents an integer from 1 to 10; Y represents a group selected from...
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7449483 |
Heteroaromate OSC inhibitors
The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol...
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7449479 |
Hepatitis C virus inhibitors
Hepatitis C virus inhibitors are disclosed having the general formula:
wherein R 1 , R 2 , R 3 , R′, B, Y and X are described in the description.
Compositions comprising the compounds and...
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7446124 |
Wortmannin analogs and methods of using same in combination with chemotherapeutic agents
Novel wortmannin analogs and their use in inhibiting PI-3-kinase activity in mammals and the treatment or prevention of cancer and tumor formation in a subject are described herein. Preferably, the...
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7435750 |
Method of using substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I:
wherein Ar 1 , Ar 3 , A, B and D are defined herein. The...
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7425575 |
Spirocyclic 3-phenyl-3-substituted 4-ketolactams and 4-ketolactones
The present invention relates to novel phenyl-substituted 4-ketolactams and -lactones of the formula (I)
in which
A, B, Q, G, W, X, Y, Z and R 3 are as defined above, to processes and...
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7419986 |
Antidepressant azaheterocyclylmethyl derivatives of heterocycle-fused benzodioxans
Compounds of the Formula:
are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder,...
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7417062 |
Substituted arylamides
Substituted benzamide compounds are provided along with methods for the use of those compounds for treating cancer.
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7414071 |
Methods of treatment with selective EP4 receptor agonists
The present invention provides a method of treating hypertension, liver failure, loss of patency of ductus arteriosus, glaucoma or ocular hypertension in a patient, comprising administering to the...
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7410999 |
Compounds, methods and compositions useful for the treatment of bovine viral diarrhea virus (BVDV) infection and hepatitis C virus (HCV) infection
The present invention relates to novel compounds and methods that are useful in treating members of the Flaviviridae family of viruses. Compounds of the present invention will have a structure...
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7402579 |
Quinobenzoxazine analogs and compositions
The present invention relates to quinobenzoxazines analogs having the general formula:
and pharmaceutically acceptable salts, esters and prodrugs thereof; wherein A, U, W, X, Z, B, L, R 1...
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7402683 |
Cinnamic acid amides
The present invention relates to compounds, to processes for preparing them, to pharmaceutical compositions comprising them, and to their use in the therapy and/or prophylaxis in illnesses in...
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7399748 |
Antitumor therapy comprising distamycin derivatives
The present invention relates to an administration schedule comprising the intravenous administration of a α-halogen-acryloyl distamycin derivative, or a pharmaceutically acceptable salt thereof....
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7396851 |
Heterocyclic and benzoheterocyclic polyamides structurally related to the natural antibiotic distamycin A for the treatment of β-thalassaemia
The invention relates to the use of structural analogues of distamycin having the general formula (I), (II), (III), (IV) or (V) or their pharmaceutically acceptable salts, for the preparation of a...
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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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7381741 |
3-amino-2-phenylpyrrolidine derivatives
3-amino-2-phenylpyrrolidine compounds useful as NK-1 antagonists, with pharmaceutical compositions and methods of treatment comprising same, are disclosed.
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7378421 |
Chromenone derivatives
Novel compounds of the formula I
in which
R 1 , R 2 , R 3 and Het are as defined herein, which
are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for the treatment of...
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7375129 |
Bis-indole pyrroles useful as antimicrobials agents
Compounds of Formula I, commonly referred to as bis-indole pyrroles, including isolated naturally-occurring compounds, synthetic and semi-synthetic derivatives thereof having antimicrobial...
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7371767 |
Heteroaryl substituted pyrrole modulators of metabotropic glutamate receptor-5
Pyrrole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of...
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7365061 |
2-Amino-3-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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7365092 |
Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to compounds of formula I:
or pharmaceutically acceptable salts thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus...
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7365093 |
Endothelin antagonists
A compound of the formula (I):
or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing...
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7361663 |
N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa
This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing...
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7358239 |
Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z...
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7358273 |
Inhibitors of caspases
The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1β converting enzyme (“ICE”) inhibitors. This invention also relates to...
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7358274 |
Methods for treating or preventing cancer using Benzopyranone Compounds
This invention relates to Benzopyranone Compounds, compositions comprising a Benzopyranone Compound and methods for treating or preventing cancer or inhibiting the growth of a cancer cell or...
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7348346 |
Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
The present invention relates to compounds of formula (I),
which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II...
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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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7338974 |
Macrocyclic diaminopropanes as beta-secretase inhibitors
There is provided a series of novel macrocyclic diaminopropanes of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof,
wherein R 1 , R 2 , R 4 , R 5 , n, L, Z, and as...
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7329654 |
Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators
The present invention is directed to novel heteroatom containing tetracyclic derivatives, pharmaceutical compositions containing them, their use in the treatment and/or prevention of disorders...
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7329685 |
1-Phenyl-2-oxo-3-sulfonylamino-pyrrolidine derivatives and related compounds as factor Xa inhibitors for the treatment of acute vascular diseases
The invention relates to compounds of formula (I):
wherein substituents are as defined.
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7326729 |
CXCR1 and CXCR2 chemokine antagonists
The present invention is directed to a compound having the general structure of formula (1):
useful for the treatment, prevention or amelioration of a CXCR1 or CXCR2 chemokine-mediated disease.
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7314885 |
Pyrrole compounds useful as kinase inhibitors
The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for...
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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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7307043 |
Aqueous neonicotinoid compositions for seed treatment
An aqueous composition suitable for applying insecticides or acaricides to plant propagation materials comprising water, an insecticidally or acaricidally effective amount of at least one...
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7304087 |
1-acyl-pyrrolidine derivatives for the treatment of viral infections
Anti-viral agents of Formula (I)
wherein:
A represents hydroxy; D represents aryl or heteroaryl; E represents hydrogen, C 1-6 alkyl, aryl, heteroaryl or heterocyclyl; G represents hydrogen or...
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7291621 |
Substituted biaryl amides C5a receptor modulators
Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C 5 a receptor activity in vivo or in vitro, and are particularly useful in the...
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7291599 |
Use of inhibitors of enzymes having activities of amino peptidase N and/or dipeptidyl peptidase IV and of pharmaceutical preparations thereof for a therapy and prevention of chronical neurodegenerative diseases
The invention relates to a process for the treatment of neurodegenerative diseases wherein mis-folded proteins accumulate in characteristic lesions and contribute substantially to a pathogenesis...
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7288538 |
Phenylenediamine urotensin-II receptor antagonists and CCR-9 antagonists
The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.
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7276531 |
G-lactam derivatives as prostaglandin agonists
A gamma-lactam diene of Formula I:
which is particularly useful as a medicament for the treatment of various disorders such as asthma, hypertension, osteoporosis, sexual dysfunction and...
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7276492 |
Use of ACE inhibitors for treatment of patients suffering from behavioral disorders
A method for the treatment of a patient suffering from an endogenous behavioral disorder in order to ameliorate at least some behavioral aspects of the disorder, the method comprising administering...
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7271172 |
Pyrrolidine and azetidine compounds as CCR5 antagonists
The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in...
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7271193 |
Inhibitors of cyclin-dependent kinases and their use
The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia),
wherein R 1 , R 2 , R 3 , R 4...
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