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Class 514/233.5 - Bicyclo ring system having the additional hetero ring as one of the cyclos


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the additional hetero ring is one
No. of patents: 388
Last issue date: 01/24/2012


1                    
NumberTitleIssue Date
8101606Neurofibromin pathway modulators
The present invention encompasses methods for treating neurofibromatosis. ...
01/24/2012
8067412Macrocyclic compounds useful as inhibitors of kinases and HSP90
Disclosed are macrocyclic compounds of formulae I-V, which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also ...
11/29/2011
7915255Metabolism-modulating agents and uses therefor
The present invention is directed to methods and agents for modulating adipogenesis. More particularly, the present invention relates to molecules that modulate the level or functional activity of inosine-5′ monophosphate dehydrogenase (IMPDH) and to their use in ...
03/29/2011
7855200Method for treatment of gastric ulcers and ulcers induced by aspirin
The present invention relates to methods of using Oroxylum indicum as a rich source for flavanoid compounds having mucoprotective and antigastric ulcer properties, and containing Oroxylin A, Chrysin and Baicalein. ...
12/21/2010
78295572-heterosubstituted 3-aryl-4H-1-benzopyran-4-ones as novel therapeutics in breast cancer
The present invention provides 2-heterosubstituted 3-aryl-4H-benzopyran-4-one compounds for the treatment of cancers, namely breast cancer. This invention further provides a method of synthesis of 2-(alkylthio)isoflavones that can be carried out at ambient condition...
11/09/2010
7812019Chromanylurea compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor and uses thereof
Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R...
10/12/2010
7772230Chroman compound, processes for its preparation, and its pharmaceutical use
The present invention provides a chroman compound of formula (I) and its pharmaceutical salt, methods of its preparation and its pharmaceutical applications. Wherein: X is O or S; n is for 2, 3 or 4; R1 is 6-substituted or 7-substituted halogen, C1-4...
08/10/2010
77676713-Quinolinecarbonitrile protein kinase inhibitors
This invention provides a compound of Formula 1 where Ar, X, R1, R2, R3, and R4 are defined herein, or a pharmaceutically acceptable salt thereof useful in the prevention or inhib...
08/03/2010
7622465Costunolide derivatives
Disclosed are methods for inhibiting TNFα expression, IL-1β expression, iNOS expression, and NF-κB activity and methods for treating autoimmune disease, cancer, or atherosclerosis with a compound of the following formula: ...
11/24/2009
7605158Carbamoyl-type benzofuran derivatives
The present invention provides a carbamoyl-type benzofuran derivative of the formula [1]: wherein Ring Z is a group of the formula: etc.; A is a single bond, and the like; Y is a ...
10/20/2009
7572791Therapeutic morpholino-substituted compounds
Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as othe...
08/11/2009
74494603-Quinolinecarbonitrile protein kinase inhibitors
This invention provides a compound of Formula 1 where Ar, X, R1, R2, R3, and R4 are defined herein, or a pharmaceutically acceptable salt thereof useful in the prevention or inhib...
11/11/2008
7371749Benzothiazole derivatives
The present invention relates to compounds of formulae IA and IB wherein R1 and R2 are each independently lower alkyl or —(CH2)m—O-lower alkyl, or together with t...
05/13/2008
7358244Azabicycloalkane compounds
This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acc...
04/15/2008
7338949Mycobacterial inhibitors
The present invention relates to novel substituted quinoline derivatives according to the general formula (Ia) or the general formula (Ib) salts, quaternary amines, stereochemically isomeric forms, tautomeric forms and N-ox...
03/04/2008
7304058Carbamic acid esters of benzothiazoles
The present invention relates to a compound of formula I wherein R, X and n are defined hereinabove, and to a pharmaceutically acceptable salt thereof. The compound may be used for the treatment of diseases relat...
12/04/2007
72976921,3-dihydro-2-indol-2-one derivatives, process for preparing them and pharmaceutical compositions containing them
The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b
11/20/2007
7291619Melanocortin receptor agonists
The present invention relates to melanocortin receptor agonists of formula (I), which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction ...
11/06/2007
7285548Urea substituted benzothiazoles
The present invention relates to compounds of formula I wherein R1 and R2 are described herein, and their pharmaceutically acceptable salts thereof for the...
10/23/2007
7282497Pyrrolidin-2-one derivatives as inhibitors of factor xa
The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical con...
10/16/2007
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
7247627Salts and polymorphs of a pyrrole-substituted indolinone compound
The invention relates to non-hygroscopic salts of 5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-N-[(2S)-2-hydroxy-3-morpholin-4-ylpropyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, such as maleate salts, and to crystalline polymorphs of these salts. The ...
07/24/2007
7235675Conjugates of mycophenolic acid
The present invention provides a method for the measurement of an analyte in biological samples whereby an uncompetitive inhibitor is coupled to a ligand and utilized in a homogeneous assay. The analyte can be a drug or drug derivative, hormone, polypeptide, or olig...
06/26/2007
7214701Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ...
05/08/2007
7196082Ophthalmic compositions for treating ocular hypertension
This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for 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 us...
03/27/2007
7189715Compositions comprising zopiclone derivatives and methods of making and using the same
The invention is directed to racemic and stereomerically pure compounds of Formula 3: and to pharmaceutical compositions comprising them, methods of their use, and methods of their preparation. ...
03/13/2007
7189714N-type calcium channel antagonists for the treatment of pain
Compounds useful for the treatment of pain in accord with the following structural diagram, wherein R1, R2 and R3 are any of a number of groups as defined in the specification and...
03/13/2007
7186715Piperazine- and piperidine-derivatives as melanocortin receptor agonists
The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction ...
03/06/2007
71731363-Cyano-quinoline derivatives
The invention concerns quinoline derivatives of Formula (I) wherein each of Z1, m, R1, n, R3, Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmac...
02/06/2007
7169777Melanocortin receptor agonists
The present invention relates to melanocortin receptor agonist of the formula I useful in the treatment of obesity, diabetes, and male and/or female sexual dysfunction ...
01/30/2007
7157466Quinazoline ditosylate salt compounds
Ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorde4rs characterized by aberrant erbB family PTK activity. ...
01/02/2007
71575775-sulfonamido-substituted indolinone compounds as protein kinase inhibitors
The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions ...
01/02/2007
7157463Substituted piperidines/piperazines as melanocortin receptor agonists
The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction ...
01/02/2007
7148230Quinazoline derivatives
The invention concerns quinazoline derivatives of Formula I wherein R1 and R2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical composition...
12/12/2006
7148252Use of benzopyranones for treating or preventing a primary brain cancer or a brain metastasis
This invention relates to methods for using benzopyranones, or their pharmaceutically acceptable salts, for treating or preventing a primary brain cancer or a brain metastasis. The benzopyranones have the formula:
12/12/2006
71292401,3-dihydro-2H-indol-2one derivatives, process for preparing them and pharmaceutical compositions containing them
The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V
10/31/2006
7128900Light-protection agents
The invention relates to a preparation having light-protection properties comprising at least one compound of the formula I where R1 and R2 are selected from H and OR11, where eac...
10/31/2006
7122687Process for the production of an immunosuppressant
In one aspect, the present invention provides a process for producing a sodium salt of an immunosupressant of Formula I ...
10/17/2006
7109333Heterocyclic compounds
A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) ...
09/19/2006
7105513Acylated, heteroaryl-condensed cycloalkenylamines and their use as pharmaceuticals
The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administeri...
09/12/2006
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