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Class 514/301 - Ring sulfur in the bicyclo ring system


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the bicyclo ring system contains
No. of patents: 487
Last issue date: 03/16/2010


1                      
NumberTitleIssue Date
7678810Thiazole derivative
A thiazolylimidazole derivative represented by the formula or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredi...
03/16/2010
7659284Thiazolopyridine kinase inhibitors
The present invention is directed to novel thiazolopyridines, pharmaceutical compositions thereof, and the use thereof as inhibitors of ATP-protein kinase interactions. The thiazolopyridine compounds have the following Formula (I):
02/09/2010
76520325-Thioxylopyranose compounds
5-thioxylose compounds, especially 5-thioxylopyranose compounds, a process for their preparation, and their use for treating and/or inhibiting thromboses, especially venous thromboses. The compounds correspond to formula I: ...
01/26/2010
7625923Bicyclic modulators of androgen receptor function
The present invention relates to bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for examp...
12/01/2009
7625924Nicotinic alpha-7 receptor ligands and preparation and uses thereof
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of ...
12/01/2009
7612089Tetrahydroisoquinolines as factor Xa inhibitors
The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such...
11/03/2009
7598265Compositions and methods for treating CNS disorders
The invention generally relates to thienopyridinone 5-HT4 receptor modulators, and in particular the use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated ...
10/06/2009
7592352Substituted thieno and furo-pyridines
This invention relates to newly identified compounds for treating and preventing tumors and cancers, and methods for treating proliferative diseases associated with the imbalance or inappropriate activity of tyrosine kinases implicated in proliferative diseases....
09/22/2009
7592353Substituted 3-amino-thieno[2,3-]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
Disclosed are compounds of formula (I): wherein R1 and R4 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are therefore useful ...
09/22/2009
7553848Vanilloid receptor ligands and their use in treatments
bis-Bicyclic amides and derivatives thereof and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, gener...
06/30/2009
7553849Compounds
A compound of formula (I) wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R′ is hydrogen, C1-C4 alkyl, C1-C3 alkoxy; halogen, trifl...
06/30/2009
7521460Thienopyridone derivatives as kinase inhibitors
A series of thieno[2,3-b]pyridin-6(7H)-one derivatives, substituted in the 2-position by a carbonyl- or sulfonyl-linked pyrrolidin-1-yl or related moiety, being inhibitors of p38 MAP kinase, are accordingly of use in medicine, for example in the treatment and/or pre...
04/21/2009
7491733Bicyclic guanidine derivatives and therapeutic uses thereof
The invention relates to compounds of general formula (I), in which A, X, Y and R1 are defined in Claim 1. These compounds may be used in the treatment of pathologies associated with insulin resistane syndrome. ...
02/17/2009
7488736Thienopyridinone compounds and methods of treatment
The invention relates to 5-HT receptor agonists and partial agonists. Thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include ...
02/10/2009
7470707Crystalline monohydrate clopidogrel naphthalenedisulfonate and process of preparation
A crystalline clopidogrel naphthalenesulfonate or a hydrate thereof, a method for preparing same, and a pharmaceutical composition containing same are provided. ...
12/30/2008
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
74358194,5,6,7-tetrahydro-[1,2]dithiolo[4,3-C] pyridine-3-thione compounds
The present invention relates to new compounds directly increasing kinase activity of p90 ribosomal S6 kinase 1 (RSK1), a pharmaceutical composition comprising them as active ingredient, a use thereof to prevent or treat hepatic fibrosis or cirrhosis, and a method f...
10/14/2008
7425562Inhibitors of cruzipain and other cysteine proteases
Compounds of general formula (I) or general formula (II) wherein R1, P1, P2, Q, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibit...
09/16/2008
7423047Arylamine substituted bicyclic heteroaromatic compounds as p38 kinase inhibitors
Bicyclic heteroaromatic derivatives of formula (1) are described: F (1) where: the dashed line joining A and C(Ra) is present and represents a bond and A is a —N═ atom or a —C(Rb)═ group, or the dashed line is absent and A is a —N(R
09/09/2008
7411066Amino methylated 2-pyridinones
Novel amino methylated 2-pyridinones, precursors, intermediates, and derivatives; the methods for the preparation of the same; uses of the same for inhibiting pili formation in bacteria; and pharmaceutical compositions comprising these compounds are described in thi...
08/12/2008
7407966Thienopyridinone compounds and methods of treatment
The invention relates to 5-HT4 receptor agonists and partial agonists. Thienopyridinone compounds and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT4 receptors, are disclosed. Such conditions include Al...
08/05/2008
7407972Inhibitors 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
7405225Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
Disclosed are compounds of formula (I): wherein R1 and R2 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are therefore useful ...
07/29/2008
7405226Cycloalkyl-hydroxyl compounds and compositions for cholesterol management and related uses
The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, card...
07/29/2008
7399770Thieno-imino acid derivatives for use as matrix metalloproteinase inhibitors
The invention is directed to a compound of the formula I wherein the variables are as defined herein, or a stereoisomeric form thereof, mixture of stereoisomeric forms, in any ratio, or a salt thereof. Ano...
07/15/2008
7381734Serine 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. ...
06/03/2008
7371760Medicinal compositions containing aspirin
A combination of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine or a pharmaceutically acceptable salt thereof, and aspirin, which possess excellent inhibitory activity against platelet aggregation and thrombogenesis, and ...
05/13/2008
7371752Aryl fused substituted 4-oxy-pyridines
Disclosed are compounds of the formula: wherein X, Q, W and are as defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain recepto...
05/13/2008
7368471Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, ...
05/06/2008
7365080Pharmaceutical compositions comprising thieno[2,3-c]pyridine derivatives and use thereof
The present invention provides thieno[2,3-C]pyridine derivatives, pharmaceutical compositions comprising the thieno[2,3-C]pyridine derivatives, and methods of use thereof. The compounds capable of inhibiting glycosaminoglycan (GAG) interactions with effector cell ad...
04/29/2008
7351730Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8,...
04/01/2008
7351726Substituted oxadiazolidinediones
The present invention relates generally to substituted oxadiazolidinediones and methods of using them. ...
04/01/2008
7348351Substituted 3-alkyl and 3-arylalkyl -indol-1yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
The invention formula substituted 3-alkyl and 3-arylalkyl 1H indol-1yl acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure ...
03/25/2008
7342039Substituted indole oximes
The present invention relates to substituted indole oximes and methods of using them. ...
03/11/2008
7342014Diamine derivatives
A compound represented by the general formula (1): Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4  (1) wherein R1 and R2 are hydrogen atoms or the li...
03/11/2008
7332521Substituted indoles
The present invention relates generally to substituted indoles such as substituted 1H-indole-2-carboxylic acid derivatives, and methods of using them. ...
02/19/2008
7332504Heterocyclic substituted aminoazacycles useful as central nervous system agents
Heterocyclic substituted aminoazacyclic compounds of formula I Z-R3I, wherein Z is a defined aminoazacycle and R3 is a defined heterocycle moiety, pharmaceutical compositions of these compounds, and use of said compositions ...
02/19/2008
7332492Amino substituted dibenzothiophene derivatives for the treatment of disorders mediated by NP Y5 receptor
Compounds of formula (I): wherein: X is a group of formula (B): and R1, R2
02/19/2008
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
7312218Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If: or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic carbocycle or hetero...
12/25/2007
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