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Class 544/362 - The additional six-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 wherein the polycyclo ring system consists of
No. of patents: 486
Last issue date: 04/24/2012


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NumberTitleIssue Date
8163906Dihydroquinone and dihydronaphthridine inhibitors of JNK
Compounds of formula I are effective modulators of JNK: wherein X is CR11 or N; Y is —C(O)R3, 5-membered heteroaryl, or 5-membered heterocyclyl;
04/24/2012
7820820Method of preparation of azaindole derivatives
A method of preparing azaindole compounds for antiviral use having the formula ...
10/26/2010
7777035Azaindazole compounds and methods of use
Methods are provided for the synthesis of 1-[4-(substituted phenyl)-piperazin-1-yl ] -2- [3-(1H-imidazol-2-yl)-pyrazolo [3,4-b]pyridin-1-yl]-ethanone compounds via construction of the imidazole portion onto the corresponding aldehyde or nitrile compounds. ...
08/17/2010
7745625Prodrugs of piperazine and substituted piperidine antiviral agents
This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exis...
06/29/2010
7598380Method of preparation of azaindole derivatives
A method of preparing azaindole compounds for antiviral use having the formula ...
10/06/2009
7459557Substituted isoindole-1,3-diones
The present invention relates to substituted isoindole-1,3-dione compounds of Formula (I) and pharmaceutically acceptable forms thereof, as α1a/α1d adrenoreceptor modulators for the treatment of beni...
12/02/2008
7417046Substituted pyrazoles
Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S. ...
08/26/2008
7405217N-aroyl piperazine derivatives as orexin receptor antagonists
This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals. ...
07/29/2008
7405210Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, ...
07/29/2008
7396830Piperazine amidines as antiviral agents
This disclosure provides compounds of Formula I as described herein having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with indole and a...
07/08/2008
7393850Substituted pyrazoles
Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S. ...
07/01/2008
7393851Azaindole derivatives as inhibitors of p38 kinase
The invention is directed to methods to inhibit p38 kinase, preferably p38-α using compounds which are azaindoles wherein the azaindoles are coupled through a piperidine or piperazine type linker to another cyclic moiety. ...
07/01/2008
7390799Apoptosis promoters
Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed. ...
06/24/2008
7390811Respiratory syncytial virus replication inhibitors
This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of formula —CH═CH—CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH—, —CH═CH—CH═N...
06/24/2008
7371755Antiviral agents
This invention relates to a compound capable of binding to a picornavirus capsid comprising two or more capsid binding moieties. ...
05/13/2008
7365200Thienopyridinone derivatives as macrophage migration inhibitory factor inhibitors
Inhibitors of macrophage migration inhibitory factor having a thienopyridinone backbone are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with macrophage migration inhibitory fac...
04/29/2008
7361760Substituted naphthyridine derivatives as inhibitors of macrophage migration inhibitory factor and their use in the treatment of human diseases
Inhibitors of MIF having a naphthyridine backbone are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures:
04/22/2008
7358249Heterocyclic compounds having inhibitory activity against HIV integrase
A heterocyclic compound of the formula (I): wherein B1 is —C(R2)═ or —N═; R1′ is H, etc.; one of R1 and R2 is -Z1-Z2-Z3-R
04/15/2008
7355042Treatment of CNS disorders using CNS target modulators
The invention is directed to compositions and methods useful for treating Central Nervous System (CNS) disorders. Furthermore, the invention provides compositions and methods of treating sleep disorders. More specifically, the invention is directed to the compositio...
04/08/2008
7354924Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
This invention provides Compounds I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral acti...
04/08/2008
7351704Indazole-carboxamide compounds as 5-HTreceptor agonists
The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 recep...
04/01/2008
7351708Pyrrolo [2,3-b] pyridine derivatives
The present invention relates to compounds of formula I wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the tr...
04/01/2008
7348323Pyrrolo [2,3-c] pyridine derivatives
The present invention relates to compounds of formula I wherein R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the tr...
03/25/2008
7309703Substituted pyrazoles
Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described. ...
12/18/2007
7297792Pyrazolopyridines and pyrazolopyridazines as antidiabetics
The present invention includes compound of formula (I), or a derivative thereof, wherein Y is CH or N; R1 is unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substitut...
11/20/2007
7259165Heterocyclyl-3-sulfonylazaindole or-azaindazole derivatives as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor. ...
08/21/2007
7230099Heterocyclic inhibitors of MEK and methods of use thereof
Disclosed are compounds of the Formula and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8, R9 and R10, W and Y are...
06/12/2007
7220748Use of 4-(2-Flurophenyl)-6-methyl-2-(1-piperazinyl)thieno(2,3-D)-pyrimidine for treating of urinary incontinence
4-(2-Fluorophenyl)-6-Methyl-2-(1-Piperazinyl)-Thieno(2,3-D)pyrimidine or a salt thereof is useful for the treatment of urinary incontinence. ...
05/22/2007
7189727Guanidino compounds
Compounds having the general structure III are provided: where D is N or C; W is selected from Z1, Z2, and Z3 are independen...
03/13/2007
7186724Heterocyclic substituted carbonyl derivatives and their use as dopamine Dreceptor ligands
The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine...
03/06/2007
71867163-Pyrrol-pyridopyrazoles and 3-pyrrolyl-indazoles as novel kinase inhibitors
Compounds of Formula I are useful as mediators of protein kinases and have activity as cell proliferation inhibitors: where X, R1–R7 and R9 are as defined herein. ...
03/06/2007
7183284Aminium salts of 1,2,3-triazoles as prodrugs of drugs including antiviral agents
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with new aminium salts of 1,2,3-triazoles which can be used as prodrugs to improve the solubi...
02/27/2007
7179811Respiratory syncytial virus replication inhibitors
This invention concerns compounds of formula (I) prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors; their preparation, c...
02/20/2007
7176313Anti acid-fast bacterial agent containing pyridonecarboxylic acids as active ingredient
An anti acid-fast bacterial agent containing, as an active ingredient, a pyridonecarboxylic acid derivative represented by the following general formula (1), a salt thereof, or a hydrate thereof, which shows excellent antibacterial activity against Mycobacterium ...
02/13/2007
7163948Heterocyclic substituted 1,4-dihydri-4ox9-1,8-naphthyridine analogs
The present invention relates to 1,4-dihydro-4-oxo-1,8-napthpyridine analogs of the formula and pharmaceutically acceptable salts, esters, and prodrugs thereof, wherein A, X, W and Y are ...
01/16/2007
7160888[1,8]naphthyridin-2-ones and related compounds for the treatment of schizophrenia
This invention relates to compounds of the formula 1 wherein G, D, A, Z, Q, X, Y, R1, and R4 through R7 are defined as in the specification, processes for preparing the same and i...
01/09/2007
7135469Linear chain substituted monocyclic and bicyclic derivatives as factor Xa inhibitors
The present application describes linear chain substituted monocyclic and bicyclic compounds and derivatives thereof of Formula I: P4-P-M-M4I or pharmaceutically acceptable salt forms thereof, P-M are rings substituted by a ...
11/14/2006
7125888Tyrosine kinase inhibitors
The present invention relates to imidazopyridine compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, ...
10/24/2006
71091961,8 Naphthyridine derivatives and their use to treat diabetes and related disorders
The invention relates generally to naphthyridine derivatives of the formula wherein one of U, X, Y and Z is nitrogen and the others are C—R, where R is hydrogen or a substituent. More specifically, the inventio...
09/19/2006
RE39265Heteroarylpiperidines, and their use as antipsychotics and analgetics
Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compound...
09/05/2006
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