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Class 544/143 - The five-membered hetero ring is one of the cyclos in a bicyclo ring system


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the polycyclo ring system consists of
No. of patents: 233
Last issue date: 09/09/2008


1            
NumberTitleIssue Date
7423058Inhibitors of hepatitis C virus NS3 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...
09/09/2008
7414067Ophthalmic compositions for treating ocular hypertension
This invention relates to the use of potent potassium channel blockers or a formulation thereof in 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 use of such co...
08/19/2008
7393404Pigment dispersants and their use
A pigment dispersant contains the following component (a) alone or the following components (a) and (b) in combination: Component (a): a composite pigment formed of a diketopyrrolopyrrole pigment having a sulfonic group and another diketopyrrolopyrrole pigmen...
07/01/2008
7381738Substituted 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, n, R1, R2, R3, R4, R...
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
73420413,4-(cyclopentyl)-fused proline compounds 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...
03/11/2008
7304048Indole-type derivatives as inhibitors of p38 kinase
The invention is directed to methods to inhibit p38-α kinase using compounds containing an aromatic system coupled through a 7-membered heterocycle to an indole-type system. ...
12/04/2007
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
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
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
7205330Inhibitors of hepatitis C virus NS3 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...
04/17/2007
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
7189726Benzofuran derivatives as inhibitors of p38-α kinase
The invention is directed to methods to inhibit p38-α kinase using compounds which contain an aromatic residue coupled to an benzofuran moiety through a piperidine. ...
03/13/2007
7176200Derivatives of sulphonamides, their preparation and use as medicaments
The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the ph...
02/13/2007
7173027Receptor selective cannabimimetic aminoalkylindoles
Disclosed are cannabimimetic aminoalkylindole compounds and methos for their manufacture. The disclosed compounds are surprisingly potent and selective cannabinoinds. Also disclosed are methods of using the disclosed compounds, including use of the disclosed compoun...
02/06/2007
7173057Ketoamides with cyclic P4'S as inhibitors of NS3 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...
02/06/2007
7173129Sulfonamide-substituted chalcone derivatives and their use to treat diseases
The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the ...
02/06/2007
7141568Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
Pyrrolo[3,4-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be usefu...
11/28/2006
7105516Compounds for the treatment of premature ejaculation
The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment ...
09/12/2006
7101877Ion channel modulating compounds and uses thereof
Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatme...
09/05/2006
70982335-halo-tryptamine derivatives used as ligands on the 5-HT and/or 5-HTserotonin receptors
Compounds of Formula (I): (I); wherein: R1 and R2 either the same or different, are H or linear or branched C1–C6 alkyl; R3=linear or branched C1–C6 alkyl; R4=halogen, and ph...
08/29/2006
7091220Substituted indole Mannich bases
The present invention relates to substituted indole Mannich bases, processes of preparing substituted indole Mannich base, a medicament containing the same, and a pharmaceutical composition containing the same. ...
08/15/2006
7049314Cyclopentyl indole derivatives
The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment ...
05/23/2006
7041235Fluorescent diketopyrrolopyrrole analogues
The present invention relates to fluorescent diketopyrrolopyrrole analogues of the general formula (I), wherein A1 and A2 are C1–C18alkyl, C2–C18alkenyl, C2–C18alkynyl, C
05/09/2006
6933316Indole compounds
Indole compounds of the formula: wherein L1 is CO; L2 is a bond; R1 is aryl or heteroaryl; R2 is H, aryl, heteroaryl, halogen, nitro, nitroso, cyano, azide, isothionitro, OR,...
08/23/2005
69301183-Oxadiazol-5-yl-1-aminoalkyl-1h-indole derivatives
The invention provides aminoalkylindole compounds of Formula (I), wherein R1-R5, n and p are as described. Also provided are compositions containing compounds of Formula (I) and the use of compounds of Formula (I) in modulating the activity of ...
08/16/2005
6903104Indol-3-YL-2-oxoacetamide compounds and methods of use thereof
The invention is based on the discovery that certain 3-oxoacetamideindolyl compounds have potent anticancer and anti-angiogenic activity. The 3-oxoacetamideindolyl compounds are of the following formula. In this formul...
06/07/2005
6849622Aliphatic nitrogenous five-membered ring compounds
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—,
02/01/2005
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
6797708Inhibitors of cytosolic phospholipase A2
This invention provides substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase ...
09/28/2004
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
6774233Process for synthesis of heteroaryl-substituted urea compounds useful as antiinflammatory agents
Disclosed are novel processes and novel intermediate compounds for preparing aryl- and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic c...
08/10/2004
6759428Indole nitriles
Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the...
07/06/2004
6753327Substituted amides, their preparation and use
An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: ...
06/22/2004
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
6743788Carbamate and oxamide compounds
Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are ...
06/01/2004
6730671Compounds useful as reversible inhibitors of cathespin S
Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes, for making such novel compounds.
05/04/2004
6716837Heterocyclic compounds for the treatment of migraine
Described herein are compounds useful in the treatment of migraine, which have the general formula: wherein: W is a CH group or a N atom; Z is N or C—R4; B and D are selected independently from CH and N, with th...
04/06/2004
6710068Phenylindoles for the treatment of HIV
The invention as disclosed herein is a method and composition for the treatment of HIV in humans and other host animals, that includes the administration of an effective HIV treatment amount of a phenylindole as described herein or a pharmaceutically acceptable salt...
03/23/2004
6706709Indolinone derivatives as protein kinase/phosphatase inhibitors
The present invention relates to certain 2-indolinone compounds which modulate the activity of protein kinases (“PKs”) and phosphatases. The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical co...
03/16/2004
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