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Class 544/359 - Additional hetero ring containing


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain a hetero ring in addition to the
No. of patents: 321
Last issue date: 09/20/2011


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NumberTitleIssue Date
8022209Substituted nitrogen-containing heteroaryl derivatives useful as modulators of the histamine Hreceptor
The present invention relates to substituted nitrogen-containing heteroaryl derivatives, pharmaceutical compositions containing them, and methods of using any of these derivatives and compositions for H4 receptor activity modulation and the treatment of s...
09/20/2011
8013156Tie-2 modulators and methods of use
The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/...
09/06/2011
7582760Benzimidazolone and dihydroindolone derivatives and uses thereof
Compounds of the formula I: or pharmaceutically acceptable salts thereof wherein m, n, X, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for...
09/01/2009
7425557Inhibitors of glycogen synthase kinase 3
New pyridine-based compounds of Formula I, compositions, and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3-mediated disorders in vivo are provided. The methods, compounds, and compositions of the invention ma...
09/16/2008
7423048Compounds for treating fundic disaccomodation
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 -a1═a2-a...
09/09/2008
7417045Heterocyclic substituted pyridine or phenyl compounds with CXCR3 antagonist activity
The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prod rug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general ...
08/26/2008
7402675Process for the synthesis of amine ethers from secondary amino oxides
An amine ether of formula A wherein a is 1 or 2; and when a is 1, E is E′; when a is 2, E is L; E′ is C1-C36 alkyl; C3-C18 alkenyl; C2
07/22/2008
7402581Azetidine compounds
The present invention relates to a compound of the general formula (I) wherein Het is an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring having at least one nitrogen atom; R1 is hydrogen, hydroxy, C1-C4 alkyl, C3-C
07/22/2008
7384962Heterocyclic compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them
The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, the...
06/10/2008
7384943Substituted chroman derivatives
The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives having the formula (I) wherein X is N; Y is NR2CH2, CH2
06/10/2008
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
7371755Antiviral agents
This invention relates to a compound capable of binding to a picornavirus capsid comprising two or more capsid binding moieties. ...
05/13/2008
7365075Aryl sulfonamide compounds and uses related thereto
The present invention provides Aryl Sulfonamide Compounds having the formula: and prodrugs or pharmaceutically acceptable salts or prodrugs thereof. The Aryl Sulfonamide Compounds are useful for treating diabetes, obesity, ...
04/29/2008
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
73616582-acylaminothiazole derivative or salt thereof
2-Acylaminothiazole derivatives or salts thereof which have a platelet increasing activity based on an excellent human c-mpl-Ba/F3 cell growth function and a function of accelerating formation of megakaryocytic colonies and which are useful for treating thrombocytop...
04/22/2008
7309800Biphenylcarboxylic amide derivatives 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. ...
12/18/2007
7300936α-(N-sulfonamido)acetamide derivatives as β-amyloid inhibitors
There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of β-amyloid peptid...
11/27/2007
7285553Serotonergic 5HTreceptor compounds for treating ocular and CNS disorders
Compounds with 5HT7 receptor affinity (some of which are novel) useful for lowering IOP, improving blood flow to the optic nerve head and the retina, providing neuroprotection, and treating retinal diseases are disclosed. The Compounds are also useful for...
10/23/2007
7279475Fluorinated di-aryl urea compounds
Disclosed are compounds of formula(I): wherein R1, R2, W and X of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus...
10/09/2007
7271181Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceut...
09/18/2007
72561883-aminoalkyl-2-aryl-indole derivatives and their use as GnRH antagonists
The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicam...
08/14/2007
7253165Benzisoxazolyl-, pyridoisoxazolyl-and benzthienyl-phenoxy derivatives useful as Dantagonists
The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These c...
08/07/2007
72207532,7-substituted octahydro-1H-pyrido[1,2-a]pyrazine derivatives as ligands for serotonin receptors
Substituted pyrido[1,2-a]pyrazines of general formula I; wherein Ar and Ar1 represent various carbocyclic and heterocyclic aromatic rings; A represents O, S, SO, SO2, CHOH, C═O, or —(CR3R4); and n is 0–2, as well as ...
05/22/2007
7217714CCR5 modulators
Compounds of Formula 1 [Region α]−[Region β]−[Region γ]−[Region δ]   (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...
05/15/2007
7176236Water-soluble etoposide analogs and methods of use thereof
Etoposide analogs with improved water-solubility such as 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4′-O-Demethyl-4′-(N′,N′-dimethyl-glycyl)-4β-(4″-fluoroanilino)-4-desoxy-podophyllotoxin (9) ...
02/13/2007
7153857Arylpiperazines and arylpiperidines and their use as metalloproteinase inhibiting agents
Compounds of the formula I useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13. ...
12/26/2006
7151118Biphenylcarboxylic amide derivatives 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. ...
12/19/2006
7150967Fluorescent tags for amino acid and nucleic acid analysis
Methods and kits for labeling and detecting thiol containing species and nucleic acids using mercurimethyl-dihydropsoralen compounds and derivatives thereof which intercalate nucleic acids and are highly reactive with thiol containing species are provided. Fluoresce...
12/19/2006
7148240Aminoalkoxybenzoyl-benzofuran or benzothiophene derivatives, method for preparing same and compositions containing same
The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular...
12/12/2006
7115607Substituted piperazinyl amides and methods of use
Selected substituted piperazine compounds of Formula I are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceuti...
10/03/2006
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
7064201Dehydrophenylahistins and analogs thereof and the synthesis of dehydrophenylahistins and analogs thereof
Compounds represented by the following structure (I) are disclosed: as are methods for making such compounds, wherein said methods comprise reacting a diacyldiketopiperazine with a first aldehyde to produce an in...
06/20/2006
7056921Substituted chroman derivatives
The present invention relates to new new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the formula (I) wherein X is N or CH; Y is NR2
06/06/2006
7049323Amidoheterocycles as modulators of the melanocortin-4 receptor
Novel azetidinyl and pyrrolidinyl compounds are ligands of melanocortin-4 receptors and are useful for treating conditions responsive to the modulation of melanocortin-4 receptors such as obesity, diabetes, and sexual dysfunction.
05/23/2006
7041825Additive compound for curing halogenated polymers
The present invention relates to 1,3,4-thiadiazole reaction products useful as accelerators and/or curing agents for halogenated polymers in rubber vulcanization processes, and to halogenated polymer compositions containing the thiadiazole derivatives, as well as a ...
05/09/2006
70301221,4-disubstituted piperazine ligands for neurotransmitter receptors
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including serotonin receptors and dopamine recepto...
04/18/2006
7030241Mesylates of piperazine derivatives and process for their preparation
The invention relates to the mesylates of a group of piperazine derivatives and to a process for the preparation of these mesylates in an economic way in the high yield and of high purity. According to the process of the invention the synthesis of the piperazine rin...
04/18/2006
6998272Macrocyclic compounds and their use
The subject invention pertains to macrocyclic compounds, and their use, the compounds having the formula (I) wherein X is a ring bearing an optionally-protected functional group or solid phase group R1, Y is ...
02/14/2006
6982332Hybrid 2-aminotetralin and aryl-substituted piperazine compounds and their use in altering CNS activity
Compounds exhibiting CNS activity in mammalian species, having the structure wherein A is an optionally heterocyclic 5 or 6 membered aromatic ring system; R2
01/03/2006
6969730Amines as histamine-3 receptor ligands and their therapeutic applications
Compounds of formula (I) or a pharmaceutically acceptable salts or prodrug thereof which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the treatment of disorders amelior...
11/29/2005
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