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US20090318441 |
Pyrrolopyrimidine Compounds and Their Uses
The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrrolopyrimidine compounds and derivatives are...
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US20090318368 |
ANGIOTENSIN-CONVERTING ENZYME INHIBITORY PEPTIDES
It is intended to provide ACE inhibitory tripeptides which are not easily digested by digestive enzymes after being orally taken and thus have fewer tendencies to lose their ACE inhibitory activity...
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US20090312318 |
THERAPEUTIC COMPOUNDS AND METHODS
The present invention provides compounds of Formula (I): wherein A, X, Q, R 2 -R 6, m, and W have the values described herein, as well as compositions comprising such compounds. The compounds are...
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US20090311183 |
METALLOPROTEINASE 12 BINDING PROTEINS
Proteins that bind to matrix metalloproteinase 12 and methods of using such proteins are described.
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US20090311245 |
METALLOPROTEINASE 9 BINDING PROTEINS
Proteins that bind to matrix metalloproteinase 9 and methods of using such proteins are described.
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US20090312319 |
CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS
Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions...
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US20090312341 |
CYCLIC AMINE BACE-1 INHIBITORS HAVING A HETEROCYCLIC SUBSTITUENT
Disclosed are novel compounds of the formula
or a pharmaceutically acceptable salt or solvate thereof, wherein
R 1 is
X is —O—, —C(R 14 ) 2 — or —N(R)—; Z is...
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US20090311688 |
Novel Labeled oligonucleotide
The present invention relates to a labeled oligonucleotide comprising a first nucleotide segment and a second nucleotide segment, complementary to a target sequence, characterized in that it...
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US20090312363 |
BIFUNCTIONAL HISTONE DEACETYLASE INHIBITORS
In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional...
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US20090306090 |
HETEROCYCLIC DERIVATIVES AND THEIR USE AS STEAROYL-COA DESATURASE INHIBITORS
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula...
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US20090304693 |
Dual Variable Domain Immunoglobulins and Uses Thereof
The present invention relates to engineered multivalent and multispecific binding proteins, methods of making, and specifically to their uses in the prevention, diagnosis, and/or treatment of disease.
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US20090305382 |
ALKOXY INDOLINONE BASED PROTEIN KINASE INHIBITORS
Alkoxy indolinone based acid and amide derivatives have enhanced and unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein...
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US20090297449 |
METALLOPROTEINASE 9 AND METALLOPROTEINASE 2 BINDING PROTEINS
Proteins that bind to matrix metalloproteinase 9 and to matrix metalloproteinase 2 and methods of using such proteins are described.
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US20090297476 |
NOVEL PEPTIDE INHIBITORS OF HEPATITIS C VIRUS REPLICATION
The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments provide compounds of the...
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US20090297641 |
HERBAL COMPOSITIONS FOR THE TREATMENT OF MUCOSAL LESIONS
The present invention provides therapeutic compositions comprising extracts of the plant species Echinacea purpurea and Sambucus nigra and the extract(s) of at least one further plant selected...
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US20090298844 |
ABL KINASE INHIBITION
The present invention relates to inhibition of AbI kinase.
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US20090298924 |
HYDROXAMIC ACID DERIVATIVES AS INHIBITORS OF HDAC ENZYMATIC ACTIVITY
Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers:
wherein Y 1 is a bond, —(C═O)—, —S(O 2 )—,...
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US20090291957 |
HETEROCYCLIC DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise, for example, administering to a mammal in need thereof a...
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US20090291956 |
SALTS OF 2-FLUORO-N-METHYL-4-[7-(QUINOLIN-6-YL-METHYL)-IMIDAZO[1,2-b][1,2,4]TRIAZIN-2-YL]BENZAMIDE AND PROCESSES RELATED TO PREPARING THE SAME
The present invention is directed to dihydrochloric acid and dibenzenesulfonic acid salts of the c-Met kinase inhibitor...
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US20090291984 |
SUBSTITUTED PYRAZOLES, COMPOSITIONS CONTAINING THESE, METHOD OF PRODUCTION AND USE
The disclosure relates to a compound of formula (1):
and salts thereof; wherein Ar, L, A, X, R 1 , R 2 , R 3 , R 4 a, R 4 b, and R 5 are as defined in the disclosure; compositions comprising...
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US20090281082 |
COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS
The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of...
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US20090281115 |
INHIBITORS OF C-KIT AND USES THEREOF
Compounds and methods useful as inhibitors of c-Kit are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of c-Kit and processes for...
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US20090275533 |
FUSED BICYCLIC PYRIMIDINE COMPOUNDS AS AURORA KINASE INHIBITORS
Fused bicyclic pyrimidine compounds of formula (I):
wherein R 1 , R 3 , R 4 , X 1 , X 2 , Y, Z, A, B, C, D, n, and the two bonds are defined herein. Also disclosed are a method for inhibiting...
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US20090275099 |
Methods and compositions for treating diseases and conditions associated with mitochondrial function
The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides compounds as therapeutic agents to treat a...
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US20090275639 |
USP47 INHIBTORS AND METHODS TO INDUCE APOPTOSIS
The present invention relates to USP47 (ubiquitin specific protease 47) inhibitors and methods for inducing apoptosis or cell death in a target cell. In certain embodiments, the invention relates...
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US20090275063 |
Distinguishing cells in a sample by inactivating extracellular enzyme before releasing intracellular enzyme
A method for detecting the absence or presence of cells of interest in a liquid sample, wherein: (a) the sample: (i) comprises an extracellular medium containing an enzyme with a measurable...
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US20090275637 |
PROTEIN TYROSINE PHOSPHATASE INHIBITORS
The present invention provides compositions and methods for binding and/or modulating enzymatic activity of human protein tyrosine phosphatases such as PTP1B. Additionally, the invention provides...
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US20090275100 |
COMPOSITIONS AND METHODS FOR ENHANCED SENSITIVITY AND SPECIFICITY OF NUCLEIC ACID SYNTHESIS
The present invention relates to nucleic acid inhibitors, compositions and method for enhancing synthesis of nucleic acid molecules. In a preferred aspect, the invention relates to inhibition or...
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US20090270427 |
PURINE DERIVATIVES
The present invention relates to compounds of formula 1
or pharmaceutically acceptable salts thereof, wherein
one of R 1 and R 2 is methyl, ethyl or isopropyl, and the other is H;
R 3 and...
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US20090269360 |
THERAPY
The invention relates to a method of inhibiting chemotherapy induced upregulation of Cathepsin S on the surface of tumour cells, the method comprising the administration of a Cathepsin S inhibitor...
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US20090270462 |
2-SULFANYL-SUBSTITUTED IMIDAZOLE DERIVATIVES AND THEIR USE AS CYTOKINE INHIBITORS
The invention relates to 2-thio-substituted imidazole derivatives of the Formula I, and to methods of use thereof.
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US20090271879 |
ANALOGUES OF (-)-PICROPODOPHYLLIN, SYNTHESIS AND USES THEREOF
Compounds, compositions, methods of making, and methods of using analogues of (−)-picropodophyllin, as well as a transgenic animal model and its use for identifying anticancer agents.
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US20090270418 |
PYRAZOLE PYRAZINE AMINE COMPOUNDS AS KINASE INHIBITORS, COMPOSITIONS THEREOF AND METHODS OF TREATMENT THEREWITH
Provided herein are Pyrazole Pyrazine Amine Compounds having the following structure:
Wherein Q and R 1 -R 3 are as defined herein, compositions comprising an effective amount of a...
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US20090270382 |
Soluble epoxide hydrolase inhibitors
Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for...
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US20090269305 |
NOVEL MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS REPLICATION
The embodiments provide compounds of the general Formulae I, II, III, IV, V, VI, VII, and X, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The...
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US20090264514 |
SPHINGOMYELIN SYNTHASE 2 (SMS2) DEFICIENCY ATTENUATES NFkB ACTIVATION, A POTENTIAL ANTI-ATHEROGENIC PROPERTY
The present invention is directed to a method of screening for NFκB inhibiting agents, the method including the steps of administering a biologically effective amount of a candidate SMS2 inhibitor...
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US20090264494 |
USE OF NEUROPROTECTIVE 3-SUBSTITUTED INDOLONE COMPOSITIONS
The present invention include providing a therapeutically effective amount of a 3-substituted indolin-2-one compositions to protect against neurodegeneration including diseases such as Alzheimer's...
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US20090264440 |
INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY
This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth...
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US20090258855 |
BICYCLIC TRIAZOLES AS PROTEIN KINASE MODULATORS
The present disclosure provides bicyclic triazole protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.
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US20090258915 |
RIBONUCLEOTIDE REDUCTASE INHIBITORS AND METHODS OF USE
Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme. These inhibitors may be used to...
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US20090257979 |
Novel Inhibitors of Hepatitis C Virus Replication
The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment...
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US20090253679 |
NEW IMIDAZOLONE DERIVATIVES, PREPARATION THEREOF AS DRUGS, PHARMACEUTICAL COMPOSITIONS, AND USE THEREOF AS PROTEIN KINASE INHIBITORS, IN PARTICULAR CDC7
The present invention relates to imidazolone derivatives of formula (I)
to methods of preparing such derivatives, intermediates thereto, pharmaceutical compositions comprising such derivatives,...
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US20090247554 |
KINASE INHIBITORS
Compounds are provided for use with kinases that comprise (I), (II), (III), (IV): wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of...
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US20090247507 |
Enzyme Inhibitors
Compounds of formula (I), are aurora kinase inhibitors: wherein X is —N—, —CH2—N—, —CH2—CH—, or —CH—; R1 is a radical of formula (IA) wherein Z is —CH2—, —NH—, -0-,...
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US20090247538 |
Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors
The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR 5...
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US20090239219 |
TELOMERASE EXPRESSION REPRESSOR PROTEINS AND METHODS OF USING THE SAME
Telomerase repressor proteins and nucleic acid compositions encoding the same are provided. The subject repressor proteins bind to a repressor site in the TERT minimal promoter, e.g., a Site C...
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US20090233945 |
NEW COMPOUNDS 834
This invention relates to novel compounds having the structural formula I below:
and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a...
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US20090233969 |
BIARYL SUBSTITUTED NITROGEN CONTAINING HETEROCYCLE INHIBITORS OF LTA4H FOR TREATING INFLAMMATION
The present invention relates to a chemical genus of biaryl substituted nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general...
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US20090233930 |
Novel 2-Amino-Imidazole-4-One Compounds and Their Use in the Manufacture of a Medicament to Be Used in the Treatment of Cognitive Impairment, Alzheimer's Disease, Neurodegeneration and Dementia
This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a...
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US20090227607 |
DEAZAPURINES USEFUL AS INHIBITORS OF JANUS KINASES
The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions...
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