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Class 544/127 - 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 in which the polycyclo ring system consists of
No. of patents: 342
Last issue date: 09/20/2011


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NumberTitleIssue Date
8022206Furo[3,2-C]pyridines
Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT ...
09/20/2011
7750151Inhibitors of Akt activity
The present invention is directed to compounds which contain substituted napthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention...
07/06/2010
7547779Preparation of 1,6-disubstituted azabenzimidazoles as kinase inhibitors
Novel inhibitors of Rho-kinases are disclosed. ...
06/16/2009
7429584Furo[2.3-b]pyridine derivatives for the treatment of hyper-proliferative disorders
This invention relates to a compound of Formula (I) wherein Y is CH or N; Ar1 is phenyl or pyridyl each optionally substituted with 1 or 2 substituents each selected independently from (C1-C3)alkoxy halo, OH, CF3, CN, NO
09/30/2008
7371766Curcumin analogs with anti-tumor and anti-angiogenic properties
The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds. ...
05/13/2008
7358244Azabicycloalkane compounds
This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acc...
04/15/2008
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
7348339Imidazopyridine derivatives as kinase inhibitors
A compound of the formula and physiologically acceptable salts and or N-oxides thereof wherein, X1 is N or CR3; X2 is N or CR4; X3 is N or CR5; ...
03/25/2008
7326784Intermediates for the preparation of tricyclic dihydropyrano-imidazo-pyridines derivatives
The invention relates to compounds of the formula 1, in which R1, R2, R3, Arom and PG have the meanings as indicated in the description. These compounds are valuable intermediates for the preparation of pharmaceu...
02/05/2008
7323460N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides useful as HIV integrase inhibitors
N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I): wherein R1′, R
01/29/2008
7273865Thiazolopyridine
The present invention relates to compounds of formula I wherein R1 and R2 are described hereinbelow. These compounds have high affinity to A2A receptors and good selectivity to A
09/25/2007
7268232Androgen receptor modulators and method of treating disease using the same
Disclosed herein are bicycloaryl compounds of Formula (I) that selectively modulate nuclear receptors, preferably the androgen receptor, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, and methods of treating disease comprising administering...
09/11/2007
7256293Imidazopyridine intermediates
The invention relates to compounds of the formula 1, in which the substituents and symbols have the meanings indicated in the description. The compounds are valuable intermediates for the preparation of pharmaceu...
08/14/2007
7230009Pyridoxal analogues and methods of treatment
Pyridoxal analogues can be useful for treating B6 deficiency and related diseases; cardiovascular and related diseases; melanoma and related diseases; and symptoms thereof. One such analogue is a compound of the formula:
06/12/2007
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
7227020Azaindoles
Chemical compositions containing physiologically active compounds of general formula (I): wherein R1 is aryl or heteroaryl; R2 represents hydrogen, acyl, cyano, halo, lower alkenyl or lower ...
06/05/2007
7220758Ether substituted imidazopyridines
Imidazopyridine compounds that contain an ether or thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of ...
05/22/2007
7199119Antiinflammation agents
Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic, infectious and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the expres...
04/03/2007
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
7189716Tyrosine kinase inhibitors
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase enzymes thereby making them useful as anti-cancer agents. ...
03/13/2007
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
71762167-phenylpyrazolopyridine compounds
A compound represented by the formula: [wherein R1 is methoxy, methylthio, ethyl, etc.; R5 and R6 are each independently cyclopropylmethyl, (4-tetrahydropyranyl)methyl, etc.; and ...
02/13/2007
71697877-azaindoles, use thereof as phosphodiesterase 4 inhibitors and method for producing the same
The invention relates to new 7-azaindoles, their use as inhibitors of phosphodiesterase 4 and to methods for their synthesis. ...
01/30/2007
7166596Heterocyclic aromatic compounds useful as growth hormone secretagogues
Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I wherein R1...
01/23/2007
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
7153960Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones
A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibi...
12/26/2006
7138410Aza-bicyclic N-biarylamides with affinity for the α7 nicotinic acetylcholine receptor
The invention relates to novel 1-aza-bicyclic N-biarylamides, methods for production and use thereof for the production of medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning ability and memory. ...
11/21/2006
7125890Ether substituted imidazopyridines
Imidazopyridine compounds that contain an ether or thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention can induce the biosynthesis of various cytokines and are useful in the treatment of ...
10/24/2006
7122545Imidazo-benzothiazoles
The invention relates to 2-imidazo-benzothiazoles of general formula wherein R1, R2, R3, R4, R5, R6, R7, R′, R″, X, R′″ and n a...
10/17/2006
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
7087601Metabotropic glutamate receptor-5 modulators
Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered hetaryl, and further optionally substituted at the 3,4 positions, are ...
08/08/2006
7078522Pyridopyrimidine or naphthyridine derivative
A pyridopyrimidine or a naphthyridine derivative of the formula (I): wherein R1 is an optionally substituted nitrogen-containing heterocyclic group, etc.; R2 is H or a lower alkyl group; R
07/18/2006
7067515Quinuclidines-substituted-multi-cyclic-heteroaryls for the treatment of disease
The invention provides compounds of Formula I: where in W is These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or...
06/27/2006
7064123Compounds and compositions as cathepsin inhibitors
The present invention relates to novel selective cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making. ...
06/20/2006
7045528Benzofused heterozryl amide derivatives of thienopyridines useful as therapeutic agents, pharmaceutical compositions including the same, and methods for their use
The invention relates to compounds represented by the formula I and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, whe...
05/16/2006
7041675Heterocyclic compounds and their use as PARP inhibitors
The invention relates to compounds of the formula I and the tautomeric forms, possible enantiomeric and diasteromeric forms thereof, and prodrugs thereof, and use thereof as PARP inhibitors. ...
05/09/2006
7041667CCR5 modulators
Compounds of Formula 1 [Region α]—[Region β]—[Region γ]—[Region δ]  (1) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and m...
05/09/2006
7038053Process for imidazo[4,5-]pyridin-4-amines
A process and intermediates for preparing 1H-imidazo[4,5-c]pyridin-4-amines are disclosed. The process includes providing a 7H-imidazo[4,5-c]tetrazolo[1,5-a]pyridine and converting a 7H-imidazo[4,5-c]tetrazolo[1,5-a]pyridine to a 1H-imidazo[4,5-c]pyridin-4-amine.
05/02/2006
7030129Method of reducing and treating UVB-induced immunosuppression
Methods of preventing and/or treating UV-induced immunosuppression by administration of immune response modifier compounds are disclosed herein. Suitable immune response modifier compounds include agonists of one or more TLRs. ...
04/18/2006
7030116Compounds and compositions as cathepsin inhibitors
The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making. ...
04/18/2006
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