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Class 548/465 - Additional hetero ring, attached directly or indirectly to the bicyclo ring system by nonionic bonding


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein an additional hetero ring is attached
No. of patents: 397
Last issue date: 02/22/2011


1                    
NumberTitleIssue Date
7893279Cyclohexanecarboxylic acid compound
The present invention provides a VLA-4 inhibitor having high water-solubility and excellent long-term stability; i.e., sodium trans-4-[1-[2,5-dichloro-4-[(1-methyl-1H-3-indolylcarbonyl)amino]phenylacetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate ...
02/22/2011
7847106Process for the preparation of macrocyclic compounds
The present invention relates to a new process for the preparation of tripeptides of formula I wherein R1 is an amino protecting group and X is a halogen atom and wherein the tipeptide contains two olefinic moiet...
12/07/2010
7842819Derivatives for modulation of ion channels
Sulfonamide derivatives act as ion channel antagonists. The compositions are useful for treating or relieving pain-related conditions. ...
11/30/2010
7619094Ketoamides with cyclic P4's as inhibitors of NS3 serine protease of hepatitis C virus
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of us...
11/17/2009
7579483Process for preparing 7-(acryloyl)indoles
The present invention involves a process for preparing substituted indoles, such as DTSI involving two sequential cross-coupling reactions. ...
08/25/2009
7566790Intermediates and the synthesis of modified carbocyanine dyes and their conjugates
Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that a...
07/28/2009
7528262Indole derivatives as histamine 3 receptor inhibitors for the treatment of cognitive and sleep disorders, obesity and other CNS disorders
This invention relates to compounds having pharmacological activity, to compositions containing these compounds, and to a method of treatment employing the compounds and compositions. More particularly, this invention concerns certain indole derivatives and their sa...
05/05/2009
7442805Substituted sulfonamide-indoles
The present invention relates generally to substituted sulfonamide indoles such as substituted sulfonamide indoles, and methods of using them. ...
10/28/2008
7439371Indol 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. ...
10/21/2008
7435832Crystals including a malic acid salt of a 3-pyrrole substituted 2-indolinone, and compositions thereof
The present invention provides crystals, and compositions thereof, wherein the crystals include a malic acid salt of N-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide. Methods of preparing such ...
10/14/2008
7429611Indole inhibitors of 15-lipoxygenase
The present invention provides indole inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions. ...
09/30/2008
7429661Intermediates for linezolid and related compounds
The present invention provides a novel process for preparation of 5 aminomethyl substituted oxazolidinones, key intermediates for oxazolidinone antibacterials including linezolid. Thus, the key intermediate of linezolid is prepared by a) reacting N-[3-Chloro-2-(R)-h...
09/30/2008
74053063-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-b]indole-1-acetamide derivatives, their preparation and their application in therapeutics
The invention discloses and claims therapeutic uses of compounds of general formula (I) Wherein X, R1, R2 and R3 are as described herein. The invention further discloses processes for prepar...
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
7375118Phenyl-indole compounds for modulating IgE and Inhibiting cellular proliferation
The present invention is directed to small molecule inhibitors of the IgE response to allergens, which are useful in the treatment of allergy and/or asthma or any diseases where IgE is pathogenic. This invention also relates to phenyl-indole molecules that are cellu...
05/20/2008
7358364Substituted carboxylic acids
The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance or hyperglycemia. These compounds inclu...
04/15/2008
7358014Electrophotographic organophotoreceptors with novel charge transport compounds
A novel charge transport compound, a novel process using that novel compound and an organophotoreceptor includes: (a) a novel charge transport compound having the formula
04/15/2008
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
7345081Azabicyclo-octane inhibitors of IAP
The invention provides novel inhibitors of IAP that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: X1 and X2 are independently O or S; L is...
03/18/2008
7342005Antibiotic compounds
The present invention relates to carbapenems and provides a compound of the formula (I): or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein: R1 ...
03/11/2008
7332487Nitrogen-containing 5-membered ring compound
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein symbols in the formula have the following meanings; ...
02/19/2008
7332515Indole-amid derivatives which possess glycogen phosphorylase inhibitory activity
Heterocyclic amides of formula (1) and pharmaceutically acceptable salts or pro-drugs thereof wherein variable groups are as described herein; which possess glycogen phosphorylase inhibitory activity and accordin...
02/19/2008
7323488Chromogenic enzyme substrates
This invention provides novel chromogenic enzyme substrates which are indoxyl β-D-ribofuranosides. A process for their production is provided. Methods for detecting β-D-ribofuranosidase activity are given. The advantages of these novel compounds includes: detectin...
01/29/2008
7317025Non-peptidic NPY Y2 receptor inhibitors
The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurologica...
01/08/2008
7300928Benzimidazolidinone derivatives as muscarinic agents
Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the s...
11/27/2007
7291644Indole derivatives
Compounds represented by formula (I) wherein all symbols represent the same meanings as described in specification and salts thereof. Since the compound represented by the formula (I) binds and antagonize...
11/06/2007
7288662Process for the preparation of eletriptan
The present invention provides an improved process for the preparation of the anti-migraine drug, (R)-5-(2-benzenesulphonylethyl)-3-N-methylpyrrolidin-2-ylmethyl)-1H-indole (eletriptan), available commercially as the hydrobromide salt, and an intermediate and dimer-...
10/30/2007
7288563Substituted bicycloalkylamine derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein X, Z, a, b, c, d, bond g, n, s, R1, R2, R4
10/30/2007
7282510Small molecule inhibitors of rotamase enzyme activity
This invention relates to neurotrophic N-glyoxyl-prolyl ester compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prol...
10/16/2007
7273885Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents....
09/25/2007
7271265Cyanine compounds and their application as quenching compounds
The present invention provides methods and non-fluorescent carbocyanine quencher compounds having the general formula: Wherein the A moiety is a substituted pyridinium, unsubstituted pyridinium, substituted quino...
09/18/2007
7271192Substituted 2-pyrrolidine-2-yl-1H-indole compounds
Novel 2-pyrrolidin-2-yl-1H-indole compounds corresponding to formula (I) wherein R1, R2, R3 and R4 have the meanings given in the description, and pharmaceutical compos...
09/18/2007
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
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
7232906Substituted pyrrolines as kinase inhibitors
The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder. ...
06/19/2007
7223783Indolinone derivatives
Compounds of formula (I) in which R1, R2, R3 and R4 have the meanings given in the specification, are receptor tyrosine kinase inhibitors useful in the treatment of pro...
05/29/2007
7214700(2-Oxindol-3-ylidenyl) acetic acid derivatives and their use as protein kinase inhibitors
The present invention relates to (2-oxindol-3-ylidenyl)acetic acid derivatives which modulate the activity of protein kinases and are therefore useful in the prevention and treatment of protein kinase related cellular disorders such as cancer. ...
05/08/2007
7208566Imide-linked maleimide and polymaleimide compounds
The invention is based on the discovery that a remarkable improvement in the performance of maleimide thermosets can be achieved through the incorporation of imide-extended mono-, bis-, or polymaleimide compounds. These imide-extended maleimide compounds are readily...
04/24/2007
7192957Compounds as inhibitors of hepatitis C virus NS3 serine protease
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of us...
03/20/2007
7186739Stabilized activated derivatives of carbamic acid, their process of preparation and their use for the preparation of ureas
A carbamate compound is disclosed. ...
03/06/2007
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