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Class 546/118 - Three ring nitrogens in the bicyclo ring system


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the bicyclo ring system contains exactly
No. of patents: 604
Last issue date: 04/23/2013


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NumberTitleIssue Date
6677365Antagonists of MCP-1 function and methods of use thereof
Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these com...
01/13/2004
6653296Antiretroviral enantiomeric nucleotide analogs
Resolved enantiomers of the formula (IA) and (IB) ##STR1## wherein B is a purine or pyrimidine base or aza and/or deaza analogs thereof are useful in antiviral pharmaceutical compositions to treat retroviral infections....
11/25/2003
6653320Imidazopyridine derivatives
The present invention relates to novel compounds having a phosphatidylinositol 3 kinase (PI3K) inhibiting activity which are useful as medicaments, more particularly as antitumor agent. Novel 3-(imidazo[1,2-a]pyridin-3-yl) derivatives or salts thereof exh...
11/25/2003
6642230Imidazopyrimidines and imidazopyridines for the treatment of neurological disorders
Corticotropin releasing factor (CRF) antagonists of formula (I): ##STR1## and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as wel...
11/04/2003
6635641Amide compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
Amide compounds represented by the formula: ##STR1## wherein: R1 is a moiety represented by the formula ##STR2## where X is selected from the group consisting of CH2, O, S, and NH; and Y is selected from the group consisting...
10/21/2003
6635273Methods of treating vascular diseases characterized by nitric oxide insufficiency
The present invention provides methods of treating vascular diseases where nitric oxide insufficiency is a contributing factor by administering a therapeutically effective amount of at least one antioxidant, or a pharmaceutically acceptable salt thereof, ...
10/21/2003
6632809Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I: ##STR1## or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for tr...
10/14/2003
6630588Dye labeled imidazoquinoline compounds
Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds are useful, inter alia, for determining the binding and/or receptor sites of the molecules....
10/07/2003
6630487Treatment of insulin resistance with growth hormone secretagogues
This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, ##STR1## where the variables are defined in the specification, or the stereoisomeric mixture...
10/07/2003
6613776Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compositions comprising a pharmaceutically acceptable carrier and a compound of formula V: ##STR1## wherein Z1 is N, CRa, or CH, and Z2 is N or CH, provided one of Z1 and ...
09/02/2003
6610692Thrombin 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, wherein b is NY or O; c is CY2 or N; d is CY3...
08/26/2003
6605611Base analogues
Nucleoside analogues or base analogues having structure (I), where X=O or NH or S, Y=N or CHR6 or CR6, W=N or NR6 or CHR6 or CR6 or S, n=1 or 2; each R6 is independently H or O or alkyl or ...
08/12/2003
6586430CCR5 modulators
Compounds of Formula 1 [Region ଱]-[Region ଲ]-[Region γ]-[Region δ] (I) which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treat...
07/01/2003
6582351Imidazopyridinone derivatives and their use as phosphodiesterase inhibitors
A compound (Ia): ##STR1## wherein the variables are defined in the specification, its prodrug or a pharmaceutically acceptable salt thereof useful in the treatment of angina, hypertension etc....
06/24/2003
6573274Sulfonamide compounds and uses thereof as medicines
The present invention relates to a sulfonamide compound of the formula (I): ##STR1## wherein each symbol is as defined in the specification, a salt thereof, and a pharmaceutical composition containing same. This compound can be an effective agent for the ...
06/03/2003
6559167Prodrugs of proton pump inhibitors
Prodrugs of the pyridyl methyl sulfinyl benzimidazole type proton pump inhibitor drugs have a hydrolyzable arylsulfonyl or heteroarylsulfonyl group attached to the benzimidazole nitrogen. The prodrugs of the invention hydrolyze under physiological conditi...
05/06/2003
6555539Indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modula...
04/29/2003
6552192Substituted nitrogen heterocyclic derivatives and pharmaceutical use thereof
Various substituted nitrogen heterocyclic derivatives and their pharmaceutically acceptable salt derivatives are provided for use as medicaments, and particularly, as antimitotic, anti-viral, anti-cancer, anti-degenerative, immunosuppressive, and anti-mic...
04/22/2003
65520372-Substituted imidazo[1,2-A]pyridine derivatives
Disclosed are compounds of the formula: ##STR1## and the pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X, A, B, C, D and W are defined herein, which compounds bind with high selectivity and high affinity to the benzodiazepine s...
04/22/2003
6545015Catechols as antimicrobial agents
Compounds, pharmaceutically acceptable salts, and compositions thereof of the general formula: ##STR1## wherein Ar is aryl and heteroaryl; R1, R2, R3, and R4 are hydrido, alkyl, cyano, heteroaryl, hydroxy, amino...
04/08/2003
6545016Amide substituted imidazopyridines
Imidazopyridine compounds that contain amide 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 a var...
04/08/2003
6545017Urea substituted imidazopyridines
Imidazopyridine compounds that contain urea or thiourea 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 treatme...
04/08/2003
6541486Bis-benzimidazole compounds and analogs thereof for inhibiting cell death
Compounds, pharmaceutical compositions, and methods of use are described which are effective in inhibiting cell death, particularly apoptotic cell death. The compositions may be used for prevention and treatment of injuries associated with cell death, inc...
04/01/2003
6541482Carbocyclic nucleoside agents useful as selective inhibitors of proinflammatory cytokines
The present invention relates to compounds of the formula ##STR1## wherein X is N3, NH2, NHR, N(R)2, CN, SH, SR, or OR1 ; R is C1 -C4 alkyl or (CH2)n --$c;; n is an inte...
04/01/2003
6537994Heterocyclic 댣 adrenergic receptor agonists
This invention provides compounds of Formula I having the structure ##STR1## wherein, ##STR2## U, V, and W are as defined hereinbefore, or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related t...
03/25/2003
65345212-phenyl benzimidazole derivatives as MCP-1 antagonists
The present invention relates to novel compounds and medical methods of treatment of inflammation, atherosclerosis, restenosis, and immune disorders especially those associated with lymphocyte or monocyte accumulation such as arthritis and transplant reje...
03/18/2003
6525064Sulfonamido substituted imidazopyridines
Imidazopyridine compounds that contain sulfonamide 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...
02/25/2003
6525056Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (CRH) antagonists, useful for treating cns and stress-related disorders
Corticotropin releasing factor (CRF) antagonists of Formula (I): ##STR1## and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as wel...
02/25/2003
6521636Imidazo-pyridines as corticotropin releasing factor antagonists
The present invention describes novel imidazo-pyridines of formula I: ##STR1## wherein D is aryl or heteroaryl or pharmaceutically acceptable salt forms thereof, which are useful as corticotropin releasing factor antagonists....
02/18/2003
6518281Immunotherapeutic agents
Novel amides and imides are inhibitors of tumor necrosis factor଱ and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions....
02/11/2003
6515023Thrombin receptor antagonists
A thrombin receptor antagonist having the formula ##STR1## useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method of acting upon a thrombin receptor which comprises administering a therapeutically effective but non...
02/04/2003
64955612-cyclohexyl imidazopyridine NMDA/NR2B antagonists
4-substituted cyclohexanes substituted in the 1-position with imidazopyridine either directly or through a C1 -C4 alkyl, C1 -C4 alkenyl, C1 -C4 alkynyl, C1 -C4 alkoxy,...
12/17/2002
6492384Imidazo (4,5-C) pyridine-4-one derivatives with factor XA inhibiting effect
##STR1## The invention relates to novel compounds of formula (I), wherein R, R1, R2, R3, n and p have the meaning defined in claim 1. Compounds are inhibitors of clotting factor Xa and can be used for the prophylaxis and/o...
12/10/2002
6489338Imidazopyridine and imidazopyrimidine antiviral agents
The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides imidazopyridine and imidazopyrimidine derivatives (Formula I) ...
12/03/2002
6479508Viral polymerase inhibitors
A compound of the formula I: ##STR1## wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3 ; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle bei...
11/12/2002
6476045Azaindole derivatives and their use as therapeutic agents
The present invention relates to compounds of the formula (I): ##STR1## wherein: Het represents a heterocyclic residue selected from: ##STR2## where the dotted line in (b) represents an optional double bond; A completes a fused pyridine ring; and B completes a...
11/05/2002
64760411,4 substituted piperidinyl NMDA/NR2B antagonists
Novel piperidinyl compounds substituted in the 1- and 4-positions are effective as NMDA NR2B antagonists useful for relieving pain....
11/05/2002
6472403଱V integrin receptor antagonists
The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as ଱v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ...
10/29/2002
6465484Angiogenesis inhibitors
The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tryrosine kinase-dependent diseases/conditions such ...
10/15/2002
6461747Heterocyclic compounds, materials for light emitting devices and light emitting devices using the same
Disclosed is a material for a light emitting device excellent in color purity, good in light emitting characteristics and excellent in stability, which consists of a compound represented by the following general formula (I): L.paren open-st.A)m...
10/08/2002
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