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Class 546/201 - Bicyclo ring system which is indole (including hydrogenated)


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the polycyclo ring system is bicyclo and
No. of patents: 788
Last issue date: 04/10/2012


1                      
NumberTitleIssue Date
8153806Synthesis of 4-amino-thalidomide enantiomers
The invention provides new and useful analogs of 4-amino-thalidomide. These analogs include S(−)-4-amino-thalidomide and R(+)-4-amino-thalidomide. The invention also provides processes for making these analogs. Further, the invention provides methods for inhibitin...
04/10/2012
8110688Method for producing indole derivative having piperidine ring
It is possible to commercially advantageously prepare 1-{1-[2-(7-methoxy-2,2-dimethyl-4-oxochroman-8-y)ethyl]piperidin-4-yl}-N-methyl-1H-indole-6-carboxamide by coupling (7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)acetaldehyde, which is obtained by oxidizing 8-(2-hydr...
02/07/2012
7994327Processes for the preparation of 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds
The present invention provides new processes for the preparation of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds which are useful, for example, for preventing or treating diseases or conditions related to an abnorm...
08/09/2011
7863451Processes for the preparation of substituted 2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolines
The present invention concerns new processes for the preparation of substituted 2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolines which are useful for preventing or treating diseases or conditions related to an abnormally high level or activity of TNFα. The invention p...
01/04/2011
7858796Chemical compounds
The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable ...
12/28/2010
7812169Method of synthesis of 4-amino-thalidomide enantiomers
The invention provides new and useful analogs of 4-amino-thalidomide. These analogs include S(−)-4-amino-thalidomide and R(+)-4-amino-thalidomide. The invention also provides processes for making these analogs. Further, the invention provides methods for inhibitin...
10/12/2010
7763732Indole derivatives
Disclosed herein are indole derivatives of the formula (I) wherein each of the substitutents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing th...
07/27/2010
7544806Piperidine-substituted indoles-or heteroderivatives thereof
Accordingly, one object of the present invention are novel piperidine-substituted indoles- or heteroderivatives thereof of the formula 1: wherein R1, R5, R6, A, B, D-E, X-W-V, Y, i, j, n and...
06/09/2009
7531665Kinase inhibitors for the treatment of disease
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. ...
05/12/2009
7435744Piperidine derivatives as NMDA receptor antagonists
The present invention relates to a compound of formula (I): wherein: V and U are hydrogen, halogen, C1-C4 alkylamino, or together form a group that contains one or more heteroatoms, and that taken toge...
10/14/2008
7427632Factor Xa inhibitors
Compounds of formula (I) in which R1, n, Z, R3 and R4 have any of the meanings given in the specification, are inhibitors of the serine protease Factor Xa and are useful in the treatment of ...
09/23/2008
74255661,3-dihydro-2H-indol-2-one derivatives, process for preparing them and pharmaceutical compositions containing them
The invention relates to compounds of formula: and to solvates and/or hydrates thereof, with affinity for and selectivity towards the V1b receptors or both the V1b and V1a receptors of argin...
09/16/2008
7417058Pharmaceutically active benzsulfonamide derivatives as inhibitors of protein junkinases
The present invention is related to benzsulfonamide derivatives of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzsulfonamide derivatives. Said benzsulfonamide derivatives are ef-ficient ...
08/26/2008
7408067Aza-cyclic compounds as modulators of acetylcholine receptors
Compounds comprising an aza-cyclic portion and an aromatic portion linked via a sulphur atom are disclosed. The compounds disclosed are selective modulators of beta 4 subtype nicotinic acetylcholine receptors and are useful for the treatment of dysfunctions of the c...
08/05/2008
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
7396940Combinatorial library of 3-aryl-1H-indole-2-carboxylic acid
Combinatorial libraries that contains various different 4, 5 fused 3-substituted-2-pyrrolocarboxylic acids for screening pharmacological activity and methods of synthesizing said libraries. ...
07/08/2008
73880955-substituted indole-2-carboxamide derivatives
The present invention relates to compounds of formula I wherein R1 to R4 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for t...
06/17/2008
7384945Indole or benzimidazole derivatives as CB1 inverse agonists
Provided are compounds of the formula I: and pharmaceutically acceptable salts thereof, processes for making said compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compound...
06/10/2008
7381726Polymorphic forms of 1-′4-(5-cyanoindol-3-yl)butyl-4-(2-carbamoylbenzofuran-5-yl)piperazine hydrochloride
The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl...
06/03/2008
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
73650612-Amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia...
04/29/2008
7361666Heterocyclic analgesic compounds and methods of use thereof
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-couple...
04/22/2008
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
7361670Amide derivatives as NMDA receptor antagonists
Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3
04/22/2008
7354935Radiolabeled neurokinin-1 receptor antagonists
The present invention is directed to radiolabeled neurokinin-1 receptor antagonists which are useful for the labeling and diagnostic imaging of neurokinin-1 receptors in mammals. ...
04/08/2008
7351720N-ureidoalkyl-piperidines as modulators of chemokine receptor activity
The present application describes modulators of chemokine receptor activity of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases, as well as auto...
04/01/2008
7348337Indole, azaindole and related heterocyclic 4-alkenyl piperidine amides
This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with new piperidine 4-alkenyl derivatives that possess unique antiviral activity. More particul...
03/25/2008
7345060Compounds having βadrenergic receptor agonist and muscarinic receptor antagonist activity
The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1
03/18/2008
7314883Anti-migraine treatments
The present invention relates to methods of treating neurogenic vasodilation, neurogenic inflammaton, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstru...
01/01/2008
7294637Method of treating addiction or dependence using a ligand for a monamine receptor or transporter
One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substitute...
11/13/2007
72916336H-oxazolo[4,5-e]indole derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands
Compounds of the formula I in which R1, R2, R3 and R4 are as defined in claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychose...
11/06/2007
7259157N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain. ...
08/21/2007
7244846Substituted benzofuran-2-carboxamides derivatives
Compounds of the formula (I), in which D, R1, R2 and n are defined in Claim 1, are potent 5-HT1A agonists and 5-HT reuptake inhibitors and are suitable for the treatment of depression, anxiety states, panic attacks, obsessive-...
07/17/2007
7241789Substituted indoles and their use as integrin antagonists
The present invention relates to novel substituted indole compounds that are antagonists of alpha V (αv) integrins, for example αvβ3 and αvβ5 integrins, their pharmaceutically acceptable salts, and pharmaceutical comp...
07/10/2007
7238712Indole-type derivatives as inhibitors of p38 kinase
The invention is directed to methods to inhibit p38-α kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wh...
07/03/2007
7238709Therapeutic carbamates
This invention relates to hindered carbamate derivatives that are muscarinic receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds. ...
07/03/2007
7235569Piperidinyl indole and tetrohydropyridinyl indole derivatives and method of their use
3-Piperidin-4-yl-1H-indole and 3-(1,2,3,6-tetrahydro-pyridin-4-yl)-1H-indole derivatives are disclosed. Methods of using the derivatives and compositions containing the derivatives in the prevention and/or treatment of serotonin disorders, such as depression and anx...
06/26/2007
7230011Benzenesulfonic acid indol-5-yl esters as antagonists of the 5ht receptor
The present invention relates to compounds of formula I: which are antagonists of 5-HT6 receptor. ...
06/12/2007
7220862Calcitonin gene related peptide receptor antagonists
The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying th...
05/22/2007
7208491N-monoacylated o-phenylenediamines
Mono-acylated o-phenylendiamines derivatives of formula I wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone deacetylase, such as c...
04/24/2007
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