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Class 514/307 - Isoquinolines (including hydrogenated)


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the bicyclo ring system has the following
No. of patents: 1297
Last issue date: 05/29/2012


1                      
NumberTitleIssue Date
8188116Agents for therapy efficacy monitoring and deep tissue imaging
Compounds and methods related to NIR molecular imaging, in-vitro and in-vivo functional imaging, therapy/efficacy monitoring, and cancer and metastatic activity imaging. Compounds and methods demonstrated pertain to the field of peripheral benzodiazepine receptor im...
05/29/2012
81881155-HTreceptor antagonists
The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions compr...
05/29/2012
8173673Biofilm-inhibiting effect and anti-infective activity of -linked aryl isoquinolines and the use thereof
Anti-infective and biofilm-inhibiting activities of aryl isoquinoline-derivatives of the general formulae 1 to 3 are described. ...
05/08/2012
8168655Compositions and methods for treatment of eye disorders
The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides ...
05/01/2012
8153655Compositions useful as inhibitors of voltage-gated sodium channels
The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of...
04/10/2012
81536546-and 7-amino isoquinoline compounds and methods for making and using the same
6- and 7-amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6- and 7-aminoisoquinoline compounds and pharmaceutically acceptable carriers ...
04/10/2012
81483975-HT7 receptor antagonists
The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline propyl sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising...
04/03/2012
8097636Heterocyclic derivatives as modulators of ion channels
The present invention relates to heterocyclic derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of v...
01/17/2012
8084464Tetrahydroisoquinoline derivatives
This invention relates to novel tetrahydroisoquinoline derivatives, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treatin...
12/27/2011
8080562Crystalline pharmaceutical and methods of preparation and use thereof
Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in ...
12/20/2011
8071617Modulators of cellular adhesion
The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in...
12/06/2011
8071616Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases ...
12/06/2011
8071615Carbonylamino-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 and have defined...
12/06/2011
8044067Isoquinolines as IGF-1R inhibitors
Compounds of the formula (I): were synthesized. In at least one embodiment, they were found to down-regulate or inhibit the expression or function of the IGF-1 receptor. ...
10/25/2011
7998977Inhibitors of AKT (protein kinase B)
4-[5-(2-Amino-ethanesulfonyl)-isoquinolin-7-yl]-phenol or a pharmaceutically acceptable salt thereof or a hydrate of the compound or the salt thereof as Akt inhibitors that are antineoplastic and/or antiviral agents as well as compositions comprising these compounds...
08/16/2011
7951820Triazole compounds useful as protein kinase inhibitors
This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitr...
05/31/2011
79281215-HT7 receptor antagonists
The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions compr...
04/19/2011
7928122Modulators of cellular adhesion
The present invention provides compounds having formula (I); and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as d...
04/19/2011
7928120Cyanoisoquinoline compounds and methods of use thereof
The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoietin-associated conditions. The cyanoisoquinoline compounds of the invention have the following structure: ...
04/19/2011
7919504Thiadiazole modulators of PKB
The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The ...
04/05/2011
79152881-aryl-4-substituted isoquinolines
1-aryl-4-substituted isoquinoline or 1-aryl-3,4-disubstituted isoquinoline analogues of Formula I and Formula II, as follows: wherein R1, R2, R3, R8, R9, A and Ar are d...
03/29/2011
7897618N-aroyl cyclic amine derivatives as orexin receptor antagonists
Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists. ...
03/01/2011
7868019Dermatitis treating agent
The present invention is to provide a topical dermatitis treating agent which comprises a pyridine compound represented by the following formula [I]: wherein R1 and R2 each rep...
01/11/2011
7820692Tetrahydro isoquinoline derivatives, preparation methods and medicinal uses thereof
A kind of tetrahydro isoquinoline derivatives (I), their preparation methods, medicine compositions and medicinal uses thereof, especially their uses as κ-opioid receptor excitant in pain relieving, which belongs to the medicine chemistry. The substituents R1
10/26/2010
7807692Antidiabetic oxazolidinediones and thiazolidinediones
Phenoxyphenyl and phenoxybenzyl oxazolidine-2,4-diones and thiazolidine-2,4-diones are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipi...
10/05/2010
77952777-(2-(4-(3-trifuloromethyl-phenyl)-1,2,3,6-tetrahydropyrid-1-yl)ethyl)isoquinoline besylate salt, preparation and therapeutic use thereof
The present invention relates to the besylate salt of 7-(2-(4-(3-(trifluoromethyl)phenyl)-1,2,3,6-tetrahydropyrid-1-yl)ethyl)isoquinoline, to its preparation and to its use in therapeutics. The salt may be represented by the formula (II) below.
09/14/2010
7790742Substituted 4-phenyltetrahydroisoquinolines, pharmaceutical compositions thereof, methods for their preparation and therapeutic use
The present invention relates to substituted 4-phenyltetrahydroisoquinoline compounds of the structure of formula I and pharmaceutical compositions comprising them wherein the R groups are herein defined. These are excellen...
09/07/2010
7790743Modulators of cellular adhesion
The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof; wherein R1-R4, n, p, A, B, D, E, L and AR1 are as d...
09/07/2010
7786137Bicyclic derivatives as modulators of ion channels
Bicyclic derivatives having formula (I) and a composition thereof are useful as ion channel antagonists: ...
08/31/2010
7745460Modulators of cellular adhesion
The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as d...
06/29/2010
7718671Substituted arylthiourea derivatives useful as inhibitors of viral replication
Substituted arylthiourea compounds of Formula I, and the pharmaceutically acceptable salts of such compounds, useful as antiviral agents, are provided herein. Certain substituted arylthioureas disclosed herein are potent an...
05/18/2010
7718672Substituted tetrahydroisoquinoline compounds, methods of making, and their use
Disclosed are novel substituted tetrahydroisoquinoline compounds, pharmaceutical compositions containing the compounds, methods of making the compounds, and methods of using the compounds to destroy a target cell, such as a cancer cell, and to treat or prevent a can...
05/18/2010
7705017Compounds for treatment of neurodegenerative diseases
The present invention relates to a class of small molecule hydroxamic acid compounds capable of inhibiting histone deacetylases (HDACs). The present invention also relates to methods of preparation of hydroxamic acid HDAC inhibitor compounds of the invention, which ...
04/27/2010
7700620C-linked cyclic antagonists of P2Yreceptor useful in the treatment of thrombotic conditions
The present invention provides novel C-linked cyclic compounds and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as ...
04/20/2010
7691879Isoquinoline potassium channel inhibitors
The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like. ...
04/06/2010
7678811Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases ...
03/16/2010
7678812Aminotetralin-derived urea modulators of vanilloid VR1 receptor
This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to β-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain ...
03/16/2010
7635703Imidazole substituted pyrazole kinase inhibitors
The present invention is directed to novel substituted pyrazole compounds of Formula (I) or a form or composition thereof and the use thereof as inhibitors of ATP-protein kinase interactions. ...
12/22/2009
7625926P-glycoprotein inhibitor, method for preparing the same and pharmaceutical composition comprising the same
The bioavailability of an anticancer agent is enhanced when the anticancer agent is administered together with a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof. ...
12/01/2009
7615563Compositions useful as inhibitors of voltage-gated sodium channels
The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of...
11/10/2009
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