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Class 546/268.1 - Additional hetero ring containing


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain an additional hetero ring.
No. of patents: 406
Last issue date: 02/05/2013


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NumberTitleIssue Date
8367836Pyridinone antagonists of alpha-4 integrins
The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: or a tautomer, mixture of tautomers, salt or solvate thereof, wherein Cy, ring A, m, n, p,...
02/05/2013
82690154-azetidinyl-1-heteroaryl-cyclohexane antagonists of CCR2
The present invention comprises compounds of Formula (I). wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, ...
09/18/2012
8236962Metalloenzyme inhibitor compounds
The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. ...
08/07/2012
8207346Methods of synthesizing anatabine
Anatabine is obtained by reacting benzophenoneimine with 3-aminomethyl pyridine to form benzylhydrylidene-pyridin-3-yl-methyl-amine. The benzylhydrylidene-pyridin-3-yl-methyl-amine is treated with a non-nucleophilic base and a dielectrophile, such as cis-1,4-dichlor...
06/26/2012
8143408N-(8-heteroaryltetrahydronaphtalene-2yl) or N-(5-heteroarylchromane-3-yl) carboxamide derivatives for the treatment of pain
The present invention relates to new compounds of formula (I) and to pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new...
03/27/2012
8143407Process for production of heteroaryl-type boron compounds with iridium catalyst
The present invention provides an economically and industrially superior simple process that enables the selective production of an aromatic heterocyclic monoboron compound and aromatic heterocyclic diboron compound at a satisfactory yield and in a desired ratio by ...
03/27/2012
8101770Pyridones useful as inhibitors of kinases
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, ...
01/24/2012
8022221Aurora kinase modulators and method of use
The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6...
09/20/2011
7935825Arylsulfanyl and heteroarylsulfanyl derivatives for treating pain
According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification. ...
05/03/2011
7868177Multi-cyclic compounds and method of use
The present invention relates to chemical compounds having a general formula I wherein A, B, C1, C2, D, L1, L2 and R3-4 are defined herein, and synthetic intermediates,...
01/11/2011
7825255Adenosine receptor selective modulators
The invention relates to the compounds of formula (I), to a method for producing the same and to the use thereof as medicaments. ...
11/02/2010
7569694Coumarin compound, material for light emitting device and organic electroluminescent device
Provided are an organic electroluminescent device having better performances in luminous efficiency, device life and driving voltage, a display unit equipped with the same and a lighting instrument equipped with the same. The organic electroluminescent device compri...
08/04/2009
74427162-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to t...
10/28/2008
7442701Amino-heterocycles as VR-1 antagonists for treating pain
The present invention provides a compound of formula (I): wherein V represents NR5, O, S, SO or S(O)2; W and X each independently represent CH or N; Y represents N, CH or C—Ar2, with the proviso that at least one, but no more than ...
10/28/2008
74427132-thio-substituted imidazole derivatives and their use in pharmaceutics
The invention relates to 2-thio-substituted imidazole derivatives of the formula I in which the radicals R1, R2, R3, R4 and p are as defined in the description. The compounds acco...
10/28/2008
7442799Preparation and use of 2-substituted-5-oxo-3-pyrazolidinecarboxylates
A method is disclosed for preparing a 2-substituted-5-oxo-3-pyrazolidinecarboxylate compound of Formula I. The method comprises contacting a succinic acid derivative of the formula R1OC(O)C(H)(X)C(R2a)(R2b)C(O)Y (i.e. Formula II)wher...
10/28/2008
74392607-(1,3-thiazol-2-YL)thio-coumarin derivatives and their use as leukotriene biosynthesis inhibitors
The instant invention provides compounds of Formula (I) which are leukotriene biosynthesis inhibitors. Compounds of formula (I) are useful as anti-asthmatic, anti-allergic, anti-inflammatory, cytoprotective and anti-artherosclerotic agents.
10/21/2008
7435815Sulfonylamino-acetic acid derivatives
The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmac...
10/14/2008
7432286Pharmaceutically active sulfonyl hydrazide derivatives
The present invention is related to sulfonyl hydrazide derivatives for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl hydrazide derivatives. Said sulfonyl hydrazide derivatives are efficient modulators of...
10/07/2008
74322895-Acylamino-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. ...
10/07/2008
7429604Six-membered heterocycles useful as serine protease inhibitors
The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, X1, X2, X3, X4
09/30/2008
7423061Substitute thiophenes and uses thereof
This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cancer. ...
09/09/2008
74230512,6-diaminopyridine derivatives
Novel 2,6-diaminopyridine derivatives of formula wherein R1 and R2 are as defined below, are disclosed. These compounds inhibit cyclin-dependent kinases. These compounds and their pharmaceutically acce...
09/09/2008
74140644-(3,3-dihalo-allyloxy) phenoxy alkyl derivatives
Compounds of formula wherein A1, A2 and A3 are each independently of the others a bond or a C1-C6alkylene bridge; ...
08/19/2008
74109612,6-disubstituted piperiddines as modulators
The present invention is further directed to compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R16, R17, R
08/12/2008
7410979Synergistically effective combinations of dihaloacetamide compounds and interferon or ribavirin against HCV infections
The present invention relates to anti-HCV dihaloacetamide compounds in synergistic combination with an interferon and/or ribavirin and pharmaceutical compositions thereof for inhibition of the replication of HCV virus. The present invention also relates to the use o...
08/12/2008
7407977Substituted N-acyl-2-aminothiazoles
There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea. ...
08/05/2008
7399775β-amyloid protein production/secretion inhibitor
Provided are novel compounds having an inhibitory activity against production or secretion of β-amyloid protein. They embrace compounds represented by the following formula (1): and capable of being replaced with a variety...
07/15/2008
7396840Chemokine receptor binding heterocyclic compounds
Tertiary amine compounds that bind chemokine receptors such as CXCR4 and CCR5 are disclosed. ...
07/08/2008
7396936Modulators of calcitonin and amylin receptor activity
In various aspects, the present invention relates to non-peptidic compounds, which modulate calcitonin and amylin receptor activity; to processes for the preparation of some such compounds; and to pharmaceutical compositions including such compounds. Compounds of th...
07/08/2008
7393865Sleep inducing compounds and methods relating thereto
Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R1, R2, R3a, R3b, L
07/01/2008
7390907Vanilloid receptor ligands and their use in treatments
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascu...
06/24/2008
7384961Saturated and unsaturated heteroarylcycloalkylmethyl amines as anti-depressants
Saturated and unsaturated heteroarylcycloalkylmethyl-amine compounds corresponding to formula I, processes for their preparation, pharmaceutical formulations comprising these compounds and the use of saturated and unsaturat...
06/10/2008
7375118Phenyl-indole compounds for modulating IgE and Inhibiting cellular proliferation
The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic. This invention also relates to phenyl-indole molecules that are cellu...
05/20/2008
7375122Compounds useful as pesticides
Compounds useful to control pests are provided. ...
05/20/2008
7371767Heteroaryl substituted pyrrole modulators of metabotropic glutamate receptor-5
Pyrrole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, ...
05/13/2008
7371777Cyclic compound and PPAR agonist
The present invention provides a novel compound having an excellent PPAR agonist action. More specifically, it provides a compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. ...
05/13/2008
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
7365085Compounds and methods
Disclosed is a compound having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined...
04/29/2008
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
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