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Class 548/467 - Substituent on ring carbon of the bicyclo ring system contains the additional hetero ring


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero ring is in a substituent
No. of patents: 270
Last issue date: 05/17/2011


1              
NumberTitleIssue Date
7943784Process for the preparation of almotriptan
The present invention encompasses a method for the preparation of Almotriptan and its pharmaceutically acceptable salts comprises, i) Methylation of 3-[5-(1-Pyrrolidinyl sulfonyl methyl)1H-indol-yl]ethane amine ii) Treating crude Almotriptan with a hydroxy benzoic a...
05/17/2011
7598397Sulfonamide peri-substituted bicyclics for occlusive artery disease
Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representa...
10/06/2009
7405237Isoindoline compounds and methods of their use
Novel isoindoline compounds are disclosed. Methods of treating, preventing and/or managing cancer, diseases and disorders associated with, or characterized by, undesired angiogenesis, and diseases and disorders mediated by PDE 4, using the compounds are also disclos...
07/29/2008
7405300Substituted indoles as inhibitors of poly (ADP-ribose) polymerase (PARP)
The present invention relates to a series of substituted indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. Th...
07/29/2008
7378438Beta-agonist compounds comprising nitric oxide donor groups and reactive oxygen species scavenger groups and their use in the treatment of respiratory disorders
The present invention relates to multifunctional β-agonist compounds comprising a reactive oxygen species scavenger group and a nitric oxide donor, and their use for the treatment of respiratory diseases involving airway obstruction, such as asthma and chronic bron...
05/27/2008
7375219Substituted indole compounds having NOS inhibitory activity
The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other p...
05/20/2008
7355054Indole derivatives
The invention relates to 1-(R1)-2-(R2)-3-(Y—X—NH-A- or Z-A-)-4,5,6,7-R)0-4-indoles, and their acid addition salts where the compounds are basic, wherein A is C1-4 alkylene, X is >CH2, >C═O or >C═S, and t...
04/08/2008
72504151,1-Disubstitutedcycloalkyl-, glycinamidyl-, sulfonyl-amidino-, and tetrahydropyrimidinyl-containing diaminoalkyl, β-aminoacids, α-aminoacids and derivatives thereof as factor Xa inhibitors
The present application describes 1,1-disubstitutedcycloalkyl-, glycinamidyl-, sulfonyl-amidino-, and tetrahydropyrimidinyl-containing diaminoalkyl, β-aminoacids, α-aminoacids and derivatives thereof of Formula I: P-M-M1I or a stereo...
07/31/2007
7211632Perdeuterated polyiimides, their process of preparation and their use as materials which are transparent within the region from 2500 to 3500cm
The present invention relates to a deuterated polyimide, the backbone of which comprises an alternation between: at least one repeat unit corresponding to the following formula (I):
05/01/2007
7208505β3 adrenergic agonists
The present invention relates to a β3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful, e.g., for treating Type 2 diabetes and/or obesity...
04/24/2007
7138415Indolamid derivatives which possess glycogenphosphorylase inhibitory activity
Heterocyclic amides of formula (1) wherein: is a single or double bond; A is phenylene or heteroarylene; m is 0, 1 or 2; n is 0, 1 or 2; R1
11/21/2006
7122538Sulfonamide derivatives as antipsychotic agents
The invention provides compounds of formula (I): wherein A and B represent the groups —(CH2)m— and —(CH2)n— respectively; R1
10/17/2006
7112603Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to a...
09/26/2006
7094800Cyanopyrrolidides, process for their preparation and their use as medicaments
The invention relates to compounds of the formula I in which the radicals have the meanings stated in the text, their stereoisomeric forms, and their physiologically tolerated salts, physiologically functional de...
08/22/2006
6995262Use of acylsulfonamido-substituted polymethine dyes as fluorescene dyes and/or markers
The invention relates to a novel polymethine dyes containing at least one acylsulfonamido group of the formula (I) in which n, Y, A and R have the meaning given in the claims, and at least one compound of the formulae ...
02/07/2006
6989384Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picomaviral 3C protease. These compounds, as well as pharmaceutical ...
01/24/2006
6962942Azacycloalkanone serine protease inhibitors
The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having F...
11/08/2005
6933295Substituted isoindoles and the use thereof
The invention relates to the field of blood clotting, to novel compounds of formula (I), to a method for their production and to the use of these compounds as active ingredients in medicaments for preventing and/or tre...
08/23/2005
6855710Substituted indolines with an inhibitory effect on various kinases and complexes of CDKs
The present invention relates to new substituted indolinones of general formula wherein X and R1 to R5 are defined as in claim 1, the isomers and the salts thereof which have valuable...
02/15/2005
6831178Process for preparation of sulfonamide derivatives and crystals thereof
A process for the preparation of a compound of the formula (I′): which comprises reacting in a solvent a compound of the formula (III): wherein X is halogen, ...
12/14/2004
6815093Light emitting materials based on indole skeleton
An indole-based compound represented by Formula (1) disclosed herein is useful in forming a light emitting material for an organic electroluminescent device. The organic electroluminescent device has a multi-layered structure comprising a cathode, an anode and at le...
11/09/2004
6812243Indole derivatives and their use for the treatment of malignant and other diseases based on pathological proliferation
The invention relates to tyrosine kinase inhibitors of the bis-indolyl compound type of the general formula I: pharmaceuticals containing them and their use for the treatment of malignant and other diseases based on pa...
11/02/2004
6809098Compounds
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...
10/26/2004
6794406Indole derivatives
The invention relates to new indole derivatives, processes for their preparation, and their use in medicaments. ...
09/21/2004
6787651Substituted indoles, pharmaceutical compounds containing such indoles and their use as PPAR-γ binding agents
Disclosed are substituted indoles, pharmaceutical compositions containing such indoles, and their use in treating or preventing PPAR-γ mediated diseases or conditions, such as osteopenia, osteoporosis, cancer, diabetes and atherosclerosis. ...
09/07/2004
6787550Indole derivatives and their use for the treatment of osteoporosis amongst other applications
A compound of formula (1) or a salt thereof, or a solvate thereof, wherein; R1 and R2 each independently represents C1-6alkoxy or halo; R3 and R4
09/07/2004
67650123-(Arylamino)methylene-1,3-dihydro-2H-indol-2-ones as kinase inhibitors
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. ...
07/20/2004
6762180Substituted indolines which inhibit receptor tyrosine kinases
Indolinones of the formula having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are: (a) 3-Z-[1...
07/13/2004
6750241Protein kinase inhibitors
Disclosed are compounds which inhibit or modulate the activity of protein kinases and pharmaceutical compositions containing such compounds. The disclosed compound contain two or more ligand moieties covalently linked together by one or more linking groups. Such com...
06/15/2004
6743817Substituted fused pyrroleimines and pyrazoleimines
Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists...
06/01/2004
6740647Thrombin inhibitors
Novel five-membered heterocyclic amidines, their preparation and use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and kininogenases such as kallikrein. Pharmaceutical compositions which contain the compounds as active ingredients, ...
05/25/2004
6740649Cyclic hydroxamic acids as inhibitors of matrix metalloproteinases and/or TNF- α converting enzyme (TACE)
The present application describes novel cyclic hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected fro...
05/25/2004
6727266Substituted tryptophan derivatives
A compound of the formula (I): wherein: R1 is represented by the formula: wherein R4, R5, R6, R7 and R8 are ...
04/27/2004
6716870Prodrugs of 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
The present invention is directed to prodrugs of certain 3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to a...
04/06/2004
67067352-substituted-4-nitrogen heterocycles as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases. ...
03/16/2004
6696574Processes and intermediates for preparing glycogen phosphorylase inhibitors
The instant invention provides novel processes and intermediates useful in the preparation of certain N-(indole-2-carbonyl)-ଲ-alaninamide compounds, which compounds are glycogen phosphorylase inhibitors useful in the treatment of diseases such as hy...
02/24/2004
6677367HIV protease inhibitors based on amino acid derivatives
A compound selected from the group consisting of a compound of formula I ##STR1## a compound of formula II ##STR2## and when the compound of formula I and II comprises an amino group pharmaceutically acceptable ammonium salts thereof, wherein R1
01/13/2004
6673790Indolin-2-one derivatives, preparation and their use as ocytocin receptor ligands
The present invention relates to novel indolin-2-one derivatives of formula: ##STR1## to the preparation and to the pharmaceutical compositions comprising them. These compounds have an affinity for oxytocin receptors....
01/06/2004
6653312Amidine derivatives, their preparation and application as medicines and pharmaceutical compositions containing same
Amidine compounds of the formula ##STR1## wherein the substituents are defined as in the application useful as NO-synthase enzyme inhibitors....
11/25/2003
6638964Sulfonamide-containing indole compounds
The present invention creates a novel antiangiogenic agent and provides an antitumor agent which shows high safety as compared with conventional antitumor agents, has a sure effect and is able to be administered for a long period. That is, it provides an ...
10/28/2003
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