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Class 548/538 - The -C(=X)- is bonded directly to the ring nitrogen of the five-membered hetero ring (e.g., 1-pyrrolidine carboxanilides, etc.)


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the group is bonded directly to the ring
No. of patents: 195
Last issue date: 09/22/2009


1          
NumberTitleIssue Date
7592466Ureas having antiangiogenic activity
Compounds having the formula are angiogenesis inhibitors. Also disclosed are compositions containing the compounds, methods of making the compounds, and methods of treatment using the compounds. ...
09/22/2009
75572221-[(4-Ethynylphenyl)]-2-[(phenyl)]-pyrrolidine-1,2-dicarboxamide derivatives as inhibitors of coagulation factors Xa and VIIa for the treatment of thrombosis
Novel compounds of the formula (I), in which R, R1, R2 and R3 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for ...
07/07/2009
7407974Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thro...
08/05/2008
7365196Sulphonamido-substituted bridged bicycloalkyl derivatives
A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease. ...
04/29/2008
RE401837-Substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines
The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula wherein R, X, R5 and R6 are defined in the specification. The compounds of the invention ...
03/25/2008
7348440Mitotic kinesin inhibitors
The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comp...
03/25/2008
7329670Inhibition of RAF kinase using aryl and heteroaryl substituted heterocyclic ureas
The compounds are aryl and heteroaryl substituted heterocyclic ureas of the formula A—NH—C(O)—NH—B where A is the aryl or hetaryl substituted heterocyclic group and B is an aryl or heteroaryl moiety. The compounds inhibit raf kinase and are useful in the tre...
02/12/2008
7304165Oligomers and polymers of di-substituted cyclic imino carboxylic acids
Disclosed are cyclic imino oligomers and polymers comprised of subunits of the formula: Also disclosed are combinatorial libraries and arrays of the cyclic imino compounds. ...
12/04/2007
7291620N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also direct...
11/06/2007
7265146Integrin receptor inhibitors
Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to α4 integrin receptors and thereby inhi...
09/04/2007
7262207Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and v...
08/28/2007
7235580Mitotic kinesin inhibitors
The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which c...
06/26/2007
7211666Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors
Methods of preparing kinase inhibiting pharmaceutical compounds having the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1 through R6 and Z are as described...
05/01/2007
7160877Aliphatic nitrogen-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 A represents —CH2— or —S—, ...
01/09/2007
7157585Serine protease inhibitors
Compounds of formula (I) where R5, R6a, each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents. ...
01/02/2007
7094909HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
The present invention concerns processes for preparing compounds of formula (I-H), or a prodrug, pharmaceutically active metabolite, or pharmaceutically active salt or solvate thereof, which are useful as inhibit...
08/22/2006
7084139Pyrrolidin-2-one derivatives as inhibitors of factor Xa
The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical con...
08/01/2006
7030141Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat...
04/18/2006
7005439Compounds
The invention provides compounds of general formula (I) wherein m, n, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, process...
02/28/2006
6992102Bicyclic modulators of androgen receptor function
The invention provides compounds of the formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated con...
01/31/2006
6951874Compounds
The invention provides compounds of general formula (I) wherein Q, R, R2, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions contai...
10/04/2005
6906046Pharmaceutical uses and synthesis of benzobicyclooctanes
Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual ...
06/14/2005
6903116Methods of treating cancer using a heat shock factor activity inhibitor
A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, whi...
06/07/2005
6903085Substituted piperidine compounds useful as modulators of chemokine receptor activity
The invention provides compounds of formula (I) wherein R1, R2, R3, R6, Z, Q, m, n, X1, X2, X3, X4 and T are as defined in the specification, processes for their preparation, pha...
06/07/2005
6900238HIV protease inhibitors
Combinatorial libraries of HIV and FIV protease inhibitors are characterized by α-keto amide or hydroxyethylamine core structures flanked by on one side by substituted pyrrolidines, piperidines, or azasugars and on the other side by phenylalanine, tyrosine, or subs...
05/31/2005
6852752Urea compounds, compositions and methods of use and preparation
Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptide deformylase (PDF), an enzyme present in prokaryotes and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed....
02/08/2005
6838565Substituted benzoic acid amides, their preparation and their use as pharmaceutical compositions
Carboxylic acid amides of general formula having an antithrombotic activity and a factor Xa-inhibiting activity. Exemplary are: (a) N-[1-(3-amidino-phenyl)-2-(1H-tetrazol-5-yl)-ethyl]...
01/04/2005
6762178Acetylenic aryl sulfonamide and phosphinic acid amide hydroxamic acid TACE inhibitors
Hydroxamic acids having the formula are useful in treating disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and de...
07/13/2004
6727368Oligomers and polymers of cyclic imino carboxylic acids
Disclosed are cyclic imino oligomers and polymers comprised of subunits of the formula: Also disclosed are combinatorial libraries and arrays of the cyclic imino compounds. ...
04/27/2004
6710186Oligomers and polymers of di-substituted cyclic imino carboxylic acids
Disclosed are cyclic imino oligomers and polymers comprised of subunits of the formula: Also disclosed are combinatorial libraries and arrays of the cyclic imino compounds. ...
03/23/2004
6706753Integrin receptor inhibitors
Provided are compounds of formula (I) wherein A, Q, W, X, Y, Z, R1 to R4, m and n are as defined herein. Compounds of the invention bind to α4 integrin receptors and thereby inhibit bind...
03/16/2004
6664400N-arylsulfonamide and pyrrolidinecarboxylic acid intermediates, and their use for the preparation of herbicidal 1,3-dioxo-1h-pyrrolo[1,2-c]imidazole derivatives
The present invention relates to a compound of Formula 3 ##STR1## wherein X is H, F or Cl; Y is F or Cl; R1 is C1 -C3 haloalkyl, C2 -C4 alkoxyalkyl; C2 -C6 haloalkoxyalkyl...
12/16/2003
6613780Heat shock factor activity inhibitor
A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor. The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, ...
09/02/2003
6607868Photoresist monomers, polymers thereof, and photoresist compositions containing the same
Dipropargyl acetamide derivatives of following Formula 1 which are photoresist monomers, polymers thereof, and photoresist compositions containing the same. The photoresist polymer has high etching resistance, adhesiveness and post-exposure delay stabilit...
08/19/2003
6534536Alkylsulfonamido heterocyclic thrombin inhibitors
Alkylsulfonamido heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; R is hydrogen, hydroxyalkyl, aminoalkyl, alkyl, cycloalkyl, amidoalkyl, ...
03/18/2003
6531612Nitrile derivatives that inhibit cathepsin K
Compounds of the formula: ##STR1## wherein R1 to R7 and Y are as defined in the specification, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof, are useful for treating diseases associated with ...
03/11/2003
6515011Thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## or a pharmaceutically acceptable salt thereof, e.g. where R3 is --CH2 NH2, --CH
02/04/2003
6512120Methods for the synthesis of densely functionalized pyrrolidine intermediates
This invention is directed to methods of synthesizing densely functionalized pyrrolidine compounds through the use of intramolecular Diels Alder reactions....
01/28/2003
6423689Peptidyl calcium channel blockers
The present invention provides compounds that block calcium channels having the Formula I shown below. ##STR1## The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy an...
07/23/2002
6403612Thrombin receptor antagonists
A thrombin receptor antagonist having the formula ##STR1## or a pharmaceutically acceptable salt thereof, useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises ad...
06/11/2002
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