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Class 548/190 - Nitrogen attached directly to the thiazole ring by nonionic bonding


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which nitrogen is attached directly to the
No. of patents: 241
Last issue date: 11/20/2012


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NumberTitleIssue Date
8314249Process for the preparation of [4-(2-chloro-4-methoxy-5-methylphenyl)-5-methyl-thiazolo-2-yl]-[2-cyclopropyl-1-(3-fluoro-4-methylphenyl
The present invention is a process for the preparation of [4-(2-chloro-4-methoxy-5-methylphenyl)-5-methyl-thiazolo-2-yl]-[2-cyclopropyl-1-(3-fluoro-4-methylphenyl)-ethyl]-amine as set forth in formula (I) and new intermedia...
11/20/2012
8178688Benzamidine derivatives, process for the preparation thereof and pharmaceutical composition comprising the same
The present invention relates to novel benzamidine derivatives, process for the preparation thereof and pharmaceutical composition comprising the same. The novel benzamidine derivatives of the present invention are useful for the prevention and treatment of osteopor...
05/15/2012
8153814Sulfonamide derivatives
The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions...
04/10/2012
7741491Diphenylamine-substituted salicylthiazole derivatives and related compounds as phosphotyrosine phosphatase 1B (PTB1B) inhibitors for using as blood-sugar decreasing active ingredients for treating diabetes
The invention therefore relates to compounds of the formula I in which the variables are as defined in the specification, to pharmaceutical compositions containing them and to their use for therapeutically lowering blood gl...
06/22/2010
7524969Malonyl-CoA decarboxylase inhibitors useful as metabolic modulators
The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of...
04/28/2009
7427635Substituted hydantoins
The present invention relates to compounds of the formula which are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as, ...
09/23/2008
7425555Heteroaryl substituted biphenyl derivatives as p38 kinase inhibitors
Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38. ...
09/16/2008
7417150Azoles having an insecticidal action
The present application relates to novel heterocyclic compounds, to processes for their preparation, and to their use as crop protection agents, particularly for controlling animal pests. ...
08/26/2008
7414067Ophthalmic compositions for treating ocular hypertension
This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such co...
08/19/2008
7408069Preparation of 2-amino-thiazole-5-carboxylic-acid derivatives
A method for preparing a compound of the structure I, ...
08/05/2008
7396929Synthesis of 3-amino-4-substituted pyrazole derivatives
This application discloses a novel process to synthesize 3-amino-4-substituted pyrazole derivatives, which may be used, for example, as intermediates to prepare compounds having, for example, pharmaceutical utility. ...
07/08/2008
7384968Thiazole-amine compounds for the treatment of neurodegenerative disorders
The present invention relates to compounds of the Formula I wherein R1, R3, R4, R5, R6 and R7 are as defined. Compounds of the Formula I have activity inhibi...
06/10/2008
7371770Acylaminothiazole derivatives and use thereof as β-amyloid inhibitors
Compounds of formula (I) as defined herein: inhibit the formation of the β-amyloid peptide (β-A4) and are, therefore, useful in the treatment of pathologies in which a β-amyloid peptide (β-A4) formation inhibitor provid...
05/13/2008
7371751Thiazole derivatives
The present invention relates to compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, fo...
05/13/2008
7361654Substituted heteroaryl amide modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory- and immune-associated disea...
04/22/2008
7358264Statine derivatives for the treatment of Alzheimer's disease
The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment ...
04/15/2008
7354943Statine derivatives for the treatment of Alzheimer's disease
The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment ...
04/08/2008
7345043Inhibitors of histone deacetylase
Disclosed are compounds which inhibit histone deacetylase (HDAC) enzymatic activity. Also disclosed are pharmaceutical compositions comprising such compounds as well as methods to treat conditions, particularly proliferative conditions, mediated at least in part by ...
03/18/2008
7317024Heterocyclic modulators of the glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
The invention relates to a class of novel non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including obesity, diabetes, inflammatory and immune diseases, and have th...
01/08/2008
7304081Amido compounds and their use as pharmaceuticals
The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases...
12/04/2007
72946421,3-Diamino-2-hydroxypropane pro-drug derivatives
The present invention relates to compounds of formula (AA) (I) and (X): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are ...
11/13/2007
7285567Halogenated benzamide derivatives
A halogenated benzamide derivative characterized by greater specificity for viral pathogens and less disruptive to beneficial gut microflora, according to formula (III): in which ...
10/23/2007
7271186Nanomolar β-lactamase inhibitors
New carboxyphenyl-glycylboronic acid transition-state analog inhibitors, representative of a class of compounds effective against class C β-lactamase AmpC. The new compounds improve inhibition by over two-orders of magnitude compared to analogous glycylboronic acid...
09/18/2007
7268095Transition metal catalysts for (co) polymerizing of olefinic monomers
A compound of the formula Ia or Ib; where, in the formula Ia, E1 is O, S, Se, Te, NR, CR2, or PR; E2, E...
09/11/2007
7265134Tyrosine kinase inhibitors
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogen...
09/04/2007
7211576Diaminothiazoles
Novel diaminothiazoles of formula (I): are discussed. These compounds selectively inhibit the activity of Cdk4 and are thus useful in the treatment or control of cancer, in particular, the treatment or control of...
05/01/2007
7148219Biaryl heterocyclic compounds and methods of making and using the same
The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety th...
12/12/2006
7145017Preparation of Aztreonam
The invention relates to a process for the synthesis of Aztreonam. Specifically, the process entails hydrolyzing [3S-[3α(Z),4β]]-3-[[(2-amino-4-thiazolyl)[(1-t-butoxycarbonyl-1-methylethoxy)imino]acetyl]amino]-4-methyl-2-oxo-1-azetidinesulfonic acid (t-Bu Aztreona...
12/05/2006
71191112-oxo-1,3,4-trihydroquinazolinyl derivatives and methods of use
Selected compounds are effective for treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and m...
10/10/2006
7115640Heterocyclic modulators of nuclear receptors
Compounds, compositions and methods for modulating the activity of nuclear receptors are provided. In particular, heterocyclic compounds are provided for modulating the activity of farnesoid X receptor (FXR), liver X receptor (LXR) and/or orphan nuclear receptors. I...
10/03/2006
7109224Acyl guanidine compounds and use thereof
Acyl guanidine compounds of the following Formula wherein R1, R2, R3, R4 and L are described herein, and pharmaceutical compositions thereof, are useful in treating leu...
09/19/2006
7084120Prodrugs of DP IV-inhibitors
Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds can be used in the treatment of impaired glucose tolerance, glucosuria,...
08/01/2006
7074794Proline derivatives and the use thereof as drugs
The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position...
07/11/2006
7067542Diaminediols for the treatment of Alzheimer's disease
The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the...
06/27/2006
70569394-(4Methoxybenzyl)-n′-(5-nitro1,3-thiazol-2-yl)urea and its use in the treatment of conditions associated with glycogen-synthase kinase-3 (gsk3)
The present invention relates to a new compound of formula I as a free base or a pharmaceutically acceptable salt thereof, a process for the preparation, pharmaceutical formulations containing said therapeutically active compound and to the use of said compound in t...
06/06/2006
7053109Aminediols for the treatment of Alzheimer's disease
The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the...
05/30/2006
7049271Phenyl-substituted 2-enamino-ketonitriles
The present invention relates to novel phenyl-substituted 2-enamino-ketonitriles of the formula (I): in which Ar, X, Z, Y and K are each as defined in the description, to a plurality of pro...
05/23/2006
6974830NR1H4 nuclear receptor binding compounds
The present invention relates to compounds according to the general formula (I) which bind to the NR1H4 receptor and act as agonists of the NR1H4 receptor. The invention further relates to the treatment of diseases and/or conditions through binding of the nuclear re...
12/13/2005
6960664Aza hydroxylated ethyl amine compounds
Disclosed are compounds of formula: and pharmaceutically acceptable salts and esters thereof, useful in treating and/or preventing Alzheimer's disease and other similar diseases, wherein RN, RC, R...
11/01/2005
69583483-glyoxylamideindoles for treating cancer
Disclosed is an anti-cancer compound represented by Structural Formula (I): The variables in Structural Formula (I) are described hereinbelow. Also disclosed is a pharmaceutical composition comprising a pharmaceuticall...
10/25/2005
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