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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: 600
Last issue date: 05/29/2012


1                      
NumberTitleIssue Date
8188282Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles
The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present inven...
05/29/2012
8097727N,N′-diphenylurea derivatives which are suitable as kinase inhibitors
Compounds of the formula (I), in which R1a-R1e, R2a, R2b, R3 and R5 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be e...
01/17/2012
8034941Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diaste...
10/11/2011
8017780Therapeutic compounds and uses thereof
The invention provides novel therapeutic compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions to treat diseases and disorders such as cancer. ...
09/13/2011
7790891Process for the preparation of pyridine-methylsulfinyl compounds
A process for the preparation of a compound of formula (I), or a salt thereof, wherein Q is ═CR8— or ═N—; and R1-R8 are as herein defined; comprising the rea...
09/07/2010
7655800Crystalline 1H-imidazo[4,5-b]pyridin-5-amine, 7-[5-[(cyclohexylmethylamino)-methyl]-1H-indol-2-yl]-2-methyl, sulfate (1:1), trihydrate and its pharmaceutical uses
The invention relates to crystalline 1H-Imidazo[4,5-b]pyridin-5-amine, 7-[5-[(cyclohexylmethylamino)-methyl]-1H-indol-2-yl]-2-methyl, sulfate (1:1), trihydrate, E6070, its method of preparation, and its therapeutic uses. Pharmaceutical compositions containing crysta...
02/02/2010
7608717Sulfonyldihydroimidazopyridinone compounds as 5-hydroxytryptamine-6 ligands
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor. ...
10/27/2009
7579471Tropane derivatives useful in therapy
The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially anta...
08/25/2009
75316601-[[1-[(2-amino-6-methyl-4-pyridinyl)methyl]-4-fluoro-4-piperidinyl]carbonyl]-4-[2-(2-pyridinyl)-3H-imidazo[4,5-B]pyridin-3-YL]piperidine and methods of use thereof
The present invention discloses the compound of Formula I and pharmaceutically acceptable salts and solvates thereof. The invention also relates to pharmaceutical compositions comprising the Compound of Formula I and its us...
05/12/2009
7528251Method for enantioselective preparation of sulphoxide derivatives
The present invention concerns enantioselective preparation of sulphoxide derivatives or their salts. The method consist in performing an enantioselective oxidation of a sulphur of general formula (I) A —CH2—SB, wherein: A is a diversely substituted p...
05/05/2009
7528252Derivatives of triazoly-imidazopyridine useful as ligands of the adenosine Areceptor and their use as medicaments
Compounds of formula (I) wherein: X is CH or CH—R2; R1 is C1-C6 linear or branched alkyl or C1-C6 linear or branched alkenyl; R
05/05/2009
7498439Synthesis of heteroaryl acetamides from reaction mixtures having reduced water content
An improved process for the preparation of a heteroaryl acetamide from a heteroaryl α-hydroxyacetamide is provided. The process comprises directly hydrogenating the heteroaryl α-hydroxyacetamide in the presence of a strong acid, a halide and a catalyst wherein the...
03/03/2009
7462721Aza-quinolinol phosphonate integrase inhibitor compounds
Aza-quinolinol phosphonate compounds and methods for inhibition of HIV-integrase are disclosed. Ar is aryl or heteroaryl connecting R6 to L. L is a bond or a linker connecting a ring atom of Ar to N. The ring atoms...
12/09/2008
7442709N3-substituted imidazopyridine c-Kit inhibitors
Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of cancer. ...
10/28/2008
7439246Fused heterocyclic kinase inhibitors
In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful...
10/21/2008
7439247Bicyclic pyridine and pyrimidine P38 kinase inhibitors
The present invention discloses compounds corresponding to formula wherein A, R, X, Y, R, R1 and R2 are as defined above, pharmaceutical formulations, methods of making and uses thereof. ...
10/21/2008
7417052Phenylene derivative having tetrazole ring or thiazolidinedione ring
The present invention provides a compound represented by the following formula (I) wherein A is a cyclic group etc., B is a 1H-tetrazol-5-yl group or a 2,4-dioxothiazolidin-5-yl group, and Y is a single bond or a C6-10 aryl...
08/26/2008
7414046Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also re...
08/19/2008
7410966Use of and some novel imidazopyridines
The use of compounds of formula (I) wherein R1, R3, R10, m and Ar are as defined in the Specification and pharmaceutically acceptable salts thereof in the manufacture of a medicament for the treatment or prophylaxis of diseases or co...
08/12/2008
7407969Respiratory syncytial virus replication inhibitors
The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4- represents a radical of form...
08/05/2008
7407968Compounds
Compounds of formula (I) wherein RF1, RF2, Z, R1, R2, Ar, X and Y are as defined in the specification as well as salts and pharmaceutical compositions including the compounds were prepared. These compounds are useful in th...
08/05/2008
7402593Monohydrated sodium salt of S-tenatoprazole and the use thereof in therapy
The present invention relates to S-tenatoprazole monohydrated sodium salt, represented by the following formula and the use thereof in therapy for the treatment of digestive diseases. ...
07/22/2008
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
7368571HIV-Integrase inhibitors, pharmaceutical compositions and methods for their use
Bicycling hydroxamate compounds represented by the Formula I: are described. The bicyclic hydroxamate compounds and compositions containing those compounds may be used to inhibit or modulate an enzyme activity of HIV Integr...
05/06/2008
RE40245Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates ...
04/15/2008
7358235Analogs of nitrobenzylthioinosine
Analogs or derivatives of nitrobenzylthioinosine compounds. The use of these new analogs of nitrobenzylthioinosine and methods for the treatment of pain and various other indications using these analogs of nitrobenzylthioinosine as well as pharmaceutical composition...
04/15/2008
7348326Heteroaryl fused aminoalkyl imidazole derivatives: selective modulators of GABAreceptors
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are...
03/25/2008
7348333Cycloalkyl derivatives as inhibitors of bone resorption and vitronectin receptor antagonists
There are described cycloalkyl derivatives of the formula (I) R1—Y-A-B-D-E-F-G  (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds a...
03/25/2008
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
73389642-substituted-1-deaza purine derivatives with adenosine receptor modulating activity
The present invention relates to 2-substituted-1-deaza purine derivatives as adenosine receptor modulating agents, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said purine derivatives. The compounds ...
03/04/2008
7332505Nitrosated and nitrosylated proton pump inhibitors, compositions and methods of use
The present invention describes novel nitrosated and/or nitrosylated proton pump inhibitor compounds, and novel compositions comprising at least one proton pump inhibitor compound that is optionally substituted with at least one NO and/or NO2 group, and, ...
02/19/2008
73326041-[[1-[(2-Amino-6-methyl-4-pyridinyl)methyl]-4-fluoro-4-piperidinyl]carbonyl]-4-[2-(2-pyridinyl)-3H-imidazo[4,5-b]pyridin-3-yl]piperidine
The present invention discloses the compound of Formula I and pharmaceutically acceptable salts and solvates thereof. The invention also relates to pharmaceutical compositions comprising the Compound of Formula I...
02/19/2008
7329677Imidazo(4,5-b)pyridine-derivatives as inducible no-synthase inhibitors
The compounds of formula (I) in which R1, R2, R3, R4 and R11 have the meanings as given in the description are novel effective iNOS inhibitors. ...
02/12/2008
7326705Heterocyclic sodium/proton exchange inhibitors and method
Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, al...
02/05/2008
7323494Compounds and methods
Disclosed is a compound of having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables ...
01/29/2008
7317021Aminopyridine-derivatives as inductible no-synthase inhibitors
The compounds of Formula (I) in which R1, R2, R3 and R4 have the meanings as given in the description are novel effective iNOS inhibitors. ...
01/08/2008
7314940Jun kinase inhibitors
The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particula...
01/01/2008
7314936Deazapurines and uses thereof
The present invention provides compounds having formula (I), wherein R1, R2, R3 and n are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the...
01/01/2008
7309790Chemical compounds
The present invention provides compounds of formula (I) wherein R1 and R2 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, o...
12/18/2007
7300945Benzimidazole and pyridylimidazole derivatives
This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind...
11/27/2007
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