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Class 514/254.01 - The additional hetero ring is five-membered having ring nitrogen


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the additional hetero ring has exactly
No. of patents: 341
Last issue date: 05/22/2012


1                  
NumberTitleIssue Date
8183243Melanocortin receptor agonists
The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient. ...
05/22/2012
8088776Biphenyl amide lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
The present invention discloses novel compounds of Formula I: possessing 11 β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula...
01/03/2012
7994176Inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
The present invention discloses novel compounds of Formula I: having 11 Beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I...
08/09/2011
7939534Certain chemical entities, compositions, and methods
Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, and chemical entities, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described. ...
05/10/2011
7906516Carbonyl compounds
Novel compounds of the formula (I), in which D, E, G, W, X, Y, T, R1 and R2 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and f...
03/15/2011
7820673Urea derivative, process for producing the same, and use
The present invention provides a urea derivative or a salt thereof, which is useful as a therapeutic agent for thrombosis. The derivative is represented by Formula (I): wherein Cy is an aromatic hydrocarbon group which may ...
10/26/2010
7790725Thiazolidine derivatives and medicinal use thereof
A thiazolidine derivative represented by the formula (I) wherein each symbol is as defined in the specification, and a pharmaceutically acceptable salt thereof exhibit a potent DPP-IV inhibitory activity, and can be provide...
09/07/2010
7595320Hydrazinocarbonyl-thieno[2,3-C]pyrazoles, process for preparing them, compositions containing them and use thereof
The present invention concerns hydrazinocarbonyl-thieno[2,3-c]pyrazoles of formula (I): wherein R1, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and thei...
09/29/2009
7528136Prolinamide derivatives as NK3 antagonists
The present invention relates to a compound of formula I wherein R1, R2, R3, R4, R5, X, n, and o are as defined here...
05/05/2009
7432264Antimicrobial biaryl compounds
Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain. ...
10/07/2008
7419980Fused-aryl and heteroaryl derivatives and methods of their use
The present invention is directed to fused-aryl and heteroaryl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms...
09/02/2008
7414047Piperazinyl and diazapanyl benzamides and benzthioamides
Substituted piperazinyl and diazepanyl benzamides and benzthioamides of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. ...
08/19/2008
73968344(Phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain or gastrointestinal disorders
Compounds of general formula: wherein R1 and R2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the ma...
07/08/2008
7390799Apoptosis promoters
Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed. ...
06/24/2008
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
7371764Quinolin-isoquinolin-and quinazolin-oxyalkylamides and their use as fungicides
The present invention discloses fungicidal compounds and compositions of the formula (1): wherein the substituents R1, R2, R3, R4, R5, X, Y and Z are as defined in the ...
05/13/2008
7358253Indolylmaleimide derivatives
Provided are compounds of formula (I) which are useful in the treatment and/or prevention of diseases or disorders mediated by T lymphocytes and/or PKC, e.g. acute or chronic rejection of organ or tissue allo- or xenografts...
04/15/2008
7358239Pyrrolidinyl, piperidinyl or homopiperidinyl substituted (benzodioxan, benzofuran or benzopyran) derivatives
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 -Z1-Z2- is...
04/15/2008
7351702Caspase inhibitors and uses thereof
This invention provides compounds of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; next to R3 represents a...
04/01/2008
7345041Chemical compounds
The invention relates to methods for the treatment of a sleep disorder comprising administering a compound of formula (I): wherein all variables are as defined herein. ...
03/18/2008
7338947Cyclic derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma, pro...
03/04/2008
7335660Isochroman compounds for treatment of CNS disorders
This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals for the tre...
02/26/2008
7300934Benzamide nitriles
Compounds of the formula (I) wherein m, n, A, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds an...
11/27/2007
7276518Substituted cyclohexane-1,4-diamine compounds
Substituted cyclohexane-1,4-diamine compounds, methods for production thereof, pharmaceutical compositions comprising these compounds and methods of treatment using these compounds. ...
10/02/2007
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
7250414Diphenylmethyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, e, m, n, Ar1, R1, R2, R3, R4a, R4b, R5 and R6 are as defined ...
07/31/2007
7223751Sulfonamide derivatives, intermediate thereof, its preparation methods, and pharmaceutical composition comprising the same
The present invention relates to a novel sulfonamide derivatives and novel intermediates thereof, preparation thereof, and a pharmaceutical composition comprising the same, and more particularly, to novel sulfonamide derivatives and intermediates thereof that are us...
05/29/2007
7223760Substituted triazole compounds
Novel substituted triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...
05/29/2007
721471420-hydroxyeicosatetraenoic acid production inhibitors
A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a...
05/08/2007
7208497Substituted piperazines and diazepanes
A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of dis...
04/24/2007
7186725Anti-inflammatory compositions and methods
The present invention provides compositions and their use in the treatment of inflammatory diseases caused by T-cell proliferation such as sepsis, inflammatory bowel diseases, autoimmune encephalomyelitis, or lupus. The compositions comprise disubstituted ureas of F...
03/06/2007
7183270Cyclic derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of rheumatoid arthritis, multiple sclerosis, atherosclerosis and ...
02/27/2007
7173024Compounds having prolyl oligopeptidase inhibitory activity, methods for their preparation and their use
Compounds of the formula (I), wherein the symbol aa means a residue of an α-amino acid. The invention is also directed to a method for the preparation of the compounds of formula (I), as well as their use as pro...
02/06/2007
7169798Inhibitors of c-Jun N terminal kinases (JNK) and other protein kinases
The present invention provides compounds of formula I: where R1 is H, CONH2, T(n)-R, or T(n)-Ar2, n may be zero or one, and G, XYZ, and Q are as described be...
01/30/2007
7166607Substituted indoles
The present invention relates to substituted indoles of formula (I) useful as pharmaceutical compounds for treating respiratory disorders ...
01/23/2007
7163944Cyclic diamine compound and pharmaceutical containing the same
The present invention relates to 2-[4-[2-(7-trifluoromethylbenzoxazol-2-ylthio)ethyl]piperazin-1-yl]-N-[4-hydroxy-2,6-bis(trifluoromethyl)phenyl]acetamide or salt thereof, and an intermediate for the preparation thereof. The above-described compound has both ...
01/16/2007
7163937Cyclic derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the treatment of rheumatoid arthritis, multiple sclerosis, atherosclerosis and a...
01/16/2007
7160886Acylated piperazine derivatives as melanocortin-4 receptor agonists
Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of disease...
01/09/2007
7157464Substituted piperazines
Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful ...
01/02/2007
7157487Vla-4 inhibitors
The present invention relates to a compound represented by the following formula (I): (wherein, W represents WA-A1-WB- (in which, WA is substituted or unsubstituted ary...
01/02/2007
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