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Class 514/217.04 - The additional hetero ring is six-membered and contains nitrogen


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein nitrogen is a ring member of the
No. of patents: 310
Last issue date: 04/24/2012


1                
NumberTitleIssue Date
8163733Sulfonylamino-derivatives as novel inhibitors of histone deacetylase
This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y, Z and have defi...
04/24/2012
8097610Derivative having PPAR agonistic activity
A compound of the formula (I): or a pharmaceutically acceptable salt thereof. ...
01/17/2012
7872002Therapeutic pyrazoloquinoline derivatives
The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABA
01/18/2011
7863266Therapeutic pyrazoloquinoline urea derivatives
The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABA
01/04/2011
7858614Therapeutic pyrazolonaphthyridine derivatives
The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the α5 subtype of GABAA, and use of the compound of formula I...
12/28/2010
7727981Benzamides and related inhibitors of factor Xa
Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and c...
06/01/2010
7595312Selected CGRP antagonists, processes for preparing them and their use as pharmaceutical compositions
The present invention relates to CGRP antagonists of general formula wherein A, U, V, W, X and R1 to R3 are defined as in claim 1, the tautomers, diastereomers, enantiomers, hydrates,...
09/29/2009
7589085Tetrahydropyran heterocyclic cyclopentyl heteroaryl modulators of chemokine receptor activity
The present invention is further directed to compounds of the formulas: (I) (II) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16
09/15/2009
7494989Pyridine compounds useful as N-type calcium channel antagonists
Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when they were taken orally. They are useful as therapeutic agents for pains ...
02/24/2009
7405209Protease inhibitors
The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such co...
07/29/2008
7368471Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, ...
05/06/2008
7365068Substituted aryl acylthioureas and related compounds; inhibitors of viral replication
The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds o...
04/29/2008
7365077Piperazine bis-amide derivatives and their use as antagonists of the orexin receptor
Disclosed are piperazine bis-amide derivatives useful as antagonists of the orexin receptor and pharmaceutical compositions containing the same. ...
04/29/2008
7361682Indole derivatives as H3 inverse agonists
The present invention relates to compounds of formula I: wherein X, R1, R2, R3, R4 and R5 are as defined in the description and claims, and pharmaceutically acceptable ...
04/22/2008
7351730Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8,...
04/01/2008
7351726Substituted oxadiazolidinediones
The present invention relates generally to substituted oxadiazolidinediones and methods of using them. ...
04/01/2008
7348351Substituted 3-alkyl and 3-arylalkyl -indol-1yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
The invention formula substituted 3-alkyl and 3-arylalkyl 1H indol-1yl acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure ...
03/25/2008
7348335Compositions useful as inhibitors of JAK and other protein kinases
The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and metho...
03/25/2008
7342039Substituted indole oximes
The present invention relates to substituted indole oximes and methods of using them. ...
03/11/2008
7332521Substituted indoles
The present invention relates generally to substituted indoles such as substituted 1H-indole-2-carboxylic acid derivatives, and methods of using them. ...
02/19/2008
7319097Compounds
The present invention relates to substituted bis-arylsulfonamide and arylsulfonamide compounds of the general formula (I) or the formula (II), which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II...
01/15/2008
7307074Diazepan derivatives or salts thereof
To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such a...
12/11/2007
7304071Protein kinase inhibitors and uses thereof
Described herein are compounds that are useful as protein kinase inhibitors having the formulae I and V: or a pharmaceutically acceptable salt thereof, wherein Ring B, Z1, Z2, U, T, m, n, p,...
12/04/2007
7300917Remedy for chronic disease
A remedy and/or a preventive for a chronic disease which contains an EDG-2 antagonist. Because of binding to a subtype EDG-2 of LPA receptor, an EDG-2 antagonist is useful in treating and/or preventing chronic diseases (for example, diseases caused by the progress o...
11/27/2007
7291613Inhibitors of p38 kinase
The invention is directed to methods to inhibit p38-α kinase using compounds comprising saturated heterocycles coupled to a fused ring system. ...
11/06/2007
7268159Substituted indoles
The present invention relates generally to substituted indoles and methods of using them. ...
09/11/2007
7265148Substituted pyrrole-indoles
The present invention relates generally to substituted pyrrole-indoles such as substituted pyrrole-indoles, and methods of using them. ...
09/04/2007
7259182Aryl, aryloxy, and aklyloxy substituted 1-indol-3-yl glyoxylic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
Compounds of formula I are provided: wherein: R1, R2, and R3, are as defined herein, as well as pharmaceutical composition and methods using the compounds as inhibitors of plasminogen activator inhibitor ...
08/21/2007
7241745Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their m...
07/10/2007
7223750Derivatives of 5-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, the preparation thereof and the application of same in therapeutics
Compounds complying with the general formula (I) in which R either represents a halogen atom or a phenyl group substituted by one or more groups chosen from halogen atoms and (C1–C6)alkyl,...
05/29/2007
7202237Pyridylether derivatives, their preparation and use
The present invention relates to novel pyridylether derivatives which are cholinergic ligands at nicotinic Ach receptors. The compounds of the invention are useful for the treatment of conditions, disorders, or diseases involving the cholinergic system of the centra...
04/10/2007
7186749Pyrrolo-naphthyl acids and methods for using them
The present invention relates to pyrrolo-naphthyl compounds of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders. ...
03/06/2007
7173034Respiratory syncytial virus replication inhibitors
This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of for CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH—, —CH═CH—CH═N— wherein each ...
02/06/2007
7163954Substituted naphthyl benzothiophene acids
The present invention relates generally to substituted naphthyl benzothiophene acids and methods of using them. ...
01/16/2007
7160918Substituted indole oxo-acetyl amino acetic acid derivatives as inhibitors of plasminogen activator inhibitor (PAI-1)
This invention provides indole oxo-acetyl amino acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure:
01/09/2007
7141592Substituted oxadiazolidinediones
The present invention relates generally to substituted oxadiazolidinediones and methods of using them. ...
11/28/2006
7115596Thiazole compounds as integrin receptor antagonists derivatives
The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of ...
10/03/2006
7115635Benzylpiperidine compound
The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following ben...
10/03/2006
7105556Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2
09/12/2006
7078429Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives of formula I are provided: wherein: R1, R2, R3, R4 and R5 are as defined herein which are useful a...
07/18/2006
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