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Class 514/408 - The five-membered hetero ring consists of one nitrogen and four carbons


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the five-membered hetero ring consists
No. of patents: 604
Last issue date: 05/15/2012


1                      
NumberTitleIssue Date
8178574Tosylate salt of trans-N-isobutyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-yl-methyl)-phenyl] cyclobut anecarboxamide
The present invention is directed to the tosylate salt of trans-N-isobutyl-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)-phenyl]-cyclobutanecarboxamide Formula (I): to solvates (e.g., hydrates) thereof, to polymorphs there...
05/15/2012
8110595Ureas and their use in the treatment of heart failure
Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure. ...
02/07/2012
8080575Gamma-lactam compounds for promoting bone growth
The present invention provides compounds, compositions and methods for promoting bone growth. Compounds useful in the methods of the present invention include compounds of Formula I, wherein each R1 and R2 is H, halogen, C1-6 alkyl, ...
12/20/2011
8030341Dmt-derivative compounds and related compositions and methods of use
The present invention relates to symmetric and asymmetric dimeric Dmt (2′,6′-ditnethyl) compounds and Dmt derivative compounds with dual δ and μ opioid receptor antagonist activity. Also, the present invention provides compositions comprising these compounds a...
10/04/2011
7998997Inhibitors of fibroblast activation protein alpha
Disclosed are peptide-based compounds that include boronic acid or cyano functionality, which efficiently and selectively inhibit fibroblast activation protein alpha. Among other therapeutic utilities, the peptide-based compounds may be useful for the treatment of c...
08/16/2011
79942093-phenoxymethylpyrrolidine compounds
In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepine...
08/09/2011
7834047Arylsulfonamides and uses related thereto
Arylsulfonamide compounds of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: ...
11/16/2010
77998197-Amido-isoindolyl compounds and their pharmaceutical uses
The invention encompasses 7-amido-isoindolyl compounds and methods of using these compounds and compositions in mammals for treatment, prevention or management of various diseases and disorders. Examples include, but are not limited to, cancer, inflammatory bowel di...
09/21/2010
7781474Inhibitors 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 general Formula II, as well as compositions, including pharmaceutical ...
08/24/2010
7781475Oxindoles as kinase inhibitors
The present invention relates to oxindoles of the formula I, their use as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases and their use for the manufacture of a phar...
08/24/2010
7776903Pharmaceutical preparations containing substituted 2,5-diaminomethyl-1H-pyrroles
Pharmaceutical preparations containing substituted 2,5-diaminomethyl-1H-pyrrole compounds corresponding to formula I, and the use of these compounds for the production of pharmaceutical preparations and in related treatment...
08/17/2010
7741357Heterocyclic and carbonate derivatives of NDGA and their use as new anti-HIV and anti-cancer agents
Reaction of nordihydroguaiaretic acid with various alkyl chlorides, 1-piperidinecarbonyl chloride, methyl chloroformate, or 1,1′-carbonyldiimidazole under alkaline conditions produced the corresponding phenol ethers, carbamates and carbonates, respectively, in 67-...
06/22/2010
7732476Leukemia treatment method and composition
A method of inducing high anti-leukemia activity responsive to the combination of hydroxamic acid analogue histone deacetylase inhibitors and PKC412 against human acute leukemia characterized as expressing phosphorylated (p)FLT3 kinase by a novel flow cytometry-base...
06/08/2010
7714015Method and composition for treating sunburned skin
The present invention relates to a method and composition for treating sunburned skin. The present invention provides a method and composition for applying a mixture of indomethacin and moisturizing lotion topically to sunburned skin. The composition includes a mixt...
05/11/2010
7705032Method and composition for treating burned skin
The present invention relates to a method and composition for treating sunburned skin. The present invention provides a method and composition for applying a mixture of indomethacin and moisturizing lotion topically to sunburned skin. The composition includes a mixt...
04/27/2010
7659299Compounds inhibiting the binding of sap for treating osteoarthritis
Use of an agent capable of inhibiting SAP ligand binding activity or depleting SAP from the plasma of a subject for the production of a medicament for treatment or prevention of osteoarthritis in the subject. ...
02/09/2010
7625939Cyclopropyl-fused pyrrolidine derivatives as dipeptidyl peptidase IV inhibitors
The present invention relates to DP IV-inhibitors of formula (1) for the treatment and/or prophylaxis of diseases of mammals including cancer and tumors, metastasis and tumor colonization; and metabolic diseases. ...
12/01/2009
7605176β-ketoamide compounds with MCH antagonistic activity
Compounds of formula I wherein the groups and residues A, B, b, X, Y, Z, R1, R2, R3, R5a and R5b have the meanings given in claim 1. The invention further relate...
10/20/2009
7585885Pyrrolidine derivatives useful as BACE inhibitors
The present invention provides BACE inhibitors of Formula I: methods for their use and preparation, and intermediates for their preparation. ...
09/08/2009
7576117Cyclic amine CCR3 antagonist
A medicine containing, as an active ingredient, a cyclic amine derivative represented by the following formula (I), a pharmaceutically acceptable acid addition salt thereof or a pharmaceutically acceptable C1 to ...
08/18/2009
7553864Compounds for the treatment of inflammatory disorders and microbial diseases
This invention relates to compounds of the Formulae (I)-(IX): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or condition...
06/30/2009
7511070Compounds and therapies for the prevention of vascular and non-vascular pathologies
The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compound...
03/31/2009
7495022α,β-unsaturated hydroxamic acid derivatives and their use as histone deacetylase inhibitors
Disclosed are agents that inhibit histone deacetylase. More specifically, the present invention relates to novel hydroxamic acid derivatives or pharmaceutically acceptable salts thereof for anticancer agents or other therapeutic agents based on their histone deacety...
02/24/2009
7485662Therapeutic agent for diabetes mellitus
An object of the present invention is to provide a therapeutic agent for diabetes mellitus or insulin resistance improving agent, or to provide foods and drinks, food and drink additives, and feeds or feed additives for treating diabetes mellitus or improving insuli...
02/03/2009
74255691H-pyrazoles useful in therapy
Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1 and R3 independently represent H, C1-6alkyl, C3-8cycloalkyl, or halogen; R2 re...
09/16/2008
7423170Anticancer agents based on regulation of protein prenylation
Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g....
09/09/2008
7411091N-acyl-N′-benzyl-alkylendiamino derivatives
This invention is related to compounds and use of N-Acyl-N′-benzyl-alkylendiamino derivatives of the following general formula (I), wherein A is a straight or branched C2-C8 alkyl chain; X is a methylene, oxygen, sulphur or a NR7 g...
08/12/2008
7407982Oligo or polyalkylene glycol-coupled thrombin inhibitors
The present invention relates to novel covalent oligo and polyalkylene glycol conjugates with synthetic inhibitors of trypsin-type serine proteases, in particular inhibitors of the hemocoagulation protease thrombin, synthetic intermediates stages required in their p...
08/05/2008
7408071N-aryl pyrrolidine derivatives as beta-secretase inhibitors
There is provided a series of substituted N-aryl pyrrolidine derivatives of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R...
08/05/2008
7399748Antitumor 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. The above administration allows the treatment of a variety of tumors ...
07/15/2008
7396851Heterocyclic 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 medicament for the therapeutic treatment of β-thalassaemia. ...
07/08/2008
73968435′-carbamoyl-1,1′-biphenyl-4-carboxamide derivatives and their use as p38 kinase inhibitors
Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...
07/08/2008
7390821Methods of reducing angiogenesis
The present invention provides methods of reducing angiogenesis in an individual. The methods generally involve administering to the individual an effective amount of a nicotinic acetyl choline receptor antagonist. The methods are useful to treat conditions associat...
06/24/2008
7388007Gamma-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 R1, R2, R4, R5 and R6
06/17/2008
7381727Pyrrole derivatives, their preparation and their therapeutic use
The invention concerns compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The in...
06/03/2008
73817413-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. ...
06/03/2008
7381731Pharmaceutical composition comprising citrulline
Embodiments of the present invention include compositions and pharmaceutical compositions comprising citrulline and Hmg-CoA reductase inhibitors. Further embodiments relate to the use of such composition treat subjects and stimulating nitric oxide synthase. ...
06/03/2008
7378436Compounds
A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1-6alkyl, —C(X)Y, C3-8cycloalkyl, aryl, het, aryl-C1-4alkyl ...
05/27/2008
7365070Modulators of melanocortin receptor
This invention provides compounds and methods for treating melanocortin receptor associated disorders, such as weight loss disorders including cachexia resulting from cancer and other chronic illnesses. The compounds are represented by formula I: ...
04/29/2008
7365092Inhibitors 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 NS3-NS4A protease. As such, they ac...
04/29/2008
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