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Substituted prolines / piperidines as orexin receptor antagonists
The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and...

Substituted prolines / piperidines as orexin receptor antagonists
The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and...

5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2h-[1,4]oxazin-3-amine derivatives
The present invention relates to novel 5-(3-aminophenyl)-5-alkyl-5,6-dihydro-2H-[1,4]oxazin-3-amine derivatives as inhibitors of beta-secretase, also known as beta-site amyloid cleaving enzyme, BACE, BACE1, Asp2, or memapsin2. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and...

Estrogen receptor modulators and uses thereof
Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen...

Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
and the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula...

Novel sulfonaminoquinoline hepcidin antagonists
The present invention relates to novel hepcidin antagonists, pharmaceutical compositions comprising them and the use thereof as medicaments for the use in the treatment of iron metabolism disorders, such as, in particular, iron deficiency diseases and anemias, in particular anemias in connection with chronic inflammatory diseases....

Methods for increasing the stabilization of hypoxia inducible factor-1 alpha
Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1α) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1α prolyl hydroxylase inhibitors useful in treating diseases, conditions,...

Pyrazolopyrimidine compounds as kinase inhibitors
The present disclosure provides compounds of Formula (IA) and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical...

Substituted pyrazolo[3',4':4,5]thieno[2,3-c]pyridazin-3-amine analogs as positive allosteric modulators of the muscarinic acetylcholine receptor m4
In one aspect, the invention relates to substituted pyrazolo[3′,4′:4,5]thieno[2,3-c]pyridazine-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with...

Antispasmodic 1,2-diols and 1,2,3-triols
The present invention is directed to pharmaceutical compositions comprising antispasmodic C4-C8aliphatic-1,2-diols and C4-C8aliphatic-1,2,3-triols and their use to relieve the spasms associated with pain. These agents may be administered topically or orally and may be combined with anti-inflammatory agents such as a non-steroidal anti-inflammatory drug or a corticosteroid. Administration of the C4-C8aliphatic-1,2-diols...

Pyranyl aryl methyl benzoquinolinone m1 receptor positive allosteric modulators
which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and...

Substituted piperidinyl-carboxamide derivatives useful as scd 1 inhibitors
The present invention is directed to novel piperidinyl-carboxamide derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders....

Therapeutic agents comprising insulin amino acid sequences
The present invention relates in part to agents which provide slow absorption from an injection site. In some embodiments, the pharmaceutical compositions comprises an insulin amino acid sequence and an amino acid sequence that provide slow absorption from an injection site, such as, for example, an amino acid sequence that has...

Compositions and methods for treating cancer and inflammation-related dieseases and conditions
The invention provides di-peptide conjugated antitumor agents, pharmaceutical compositions and methods for preparation and use thereof for treating various cancer and inflammation-related diseases and conditions. The present invention addresses the shortcomings of the existing anti-tumor and anti-inflammatory drugs, particularly in that the anti-tumor agents of the invention that selectively kill cancer...

Pharmaceutical compositions for the treatment of tumors expressing egfr and gm3 n-glycolyl ganglioside (neugcgm3)
The present invention relates to pharmaceutical compositions for the treatment of malignant tumors. Particularly those tumors that express EGFR and GM3 N-glycolyl ganglioside targets to enhance the therapeutic effect produced by separated therapies against these targets. The pharmaceutical compositions of the invention include antibodies and/or vaccines against each of the targets....

Pharmaceutical formulations and the use thereof for the treatment of peanut allergy
The present invention relates to compositions which can be used in immunotherapy and especially to compositions which can be used in immunotherapy for mammals, such as human mammals, suffering from peanut allergy. The present invention further relates to the use of the present compositions for the therapeutic treatment for desentizing the...

2-thio-1,3,4-oxadiazoles azetidine derivatives as sphingosine-1 phosphate receptors modulators
The present invention relates to 2-thio-1,3,4-oxadiazoles azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors....

Binding agents to intracellular target molecules
The application provides polypeptides comprising or essentially consisting of at least one Alphabody, wherein said Alphabody is capable of internalization into a cell and specifically binds to an intracellular target molecule. The application further provides nucleic acids encoding such polypeptides; methods for preparing such polypeptides; host cells expressing or capable of...

Method of providing monoclonal auto-antibodies with desired specificity
Provided are novel binding molecules of human origin, particularly human antibodies as well as fragments, derivatives and variants thereof that recognize antigens such as native endogenous proteins associated with, e.g., immune response, autoimmune disorders, inflammatory diseases, metabolic disorders, vascular function, neurodegenerative diseases or tumors. More particularly, a human Auto-Immunosome and corresponding...

Series of skin whitening (lightening) compounds
The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction...

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Pharmaceutical Compositions patents



      
           
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