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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: 515
Last issue date: 05/15/2012


1                      
NumberTitleIssue Date
8178555Apoptosis signal-regulating kinase 1 inhibitors
The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, ...
05/15/2012
8163770Benzoxathiin derivative
Disclosed is a compound represented by the formula (I) below and a pharmaceutically acceptable salt thereof. This compound is useful for treatment of obesity, diabetes and the like. [In the formula (I), Ar represents a benzen...
04/24/2012
8124616Bicyclic PPAT inhibitors as antibacterial agents
Disclosed are compounds of Formula I, pharmaceutical compositions comprising Formula I and methods of treating bacterial infections. The disclosed compounds are inhibitors of PPAT (phosphopantetheine adenyl transferase), and are useful in the treatment and preventio...
02/28/2012
8093264Fused heterocycles as inhibitors of VEGF receptor and HGF receptor signaling
The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds of general formula (A) wherein A1 is sulfur, A3 is CH, A2 is C...
01/10/2012
8088791Antibacterial agents
Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ═C(R1)— or ═N—; R1 is hydrogen or an optional substituent and R...
01/03/2012
80763552-heteroarylcarboxylic acid amides
The invention relates to novel 2-heteroarylcarboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory. ...
12/13/2011
8003662Heterobicyclic thiophene compounds and methods of use
Compounds of Formula I and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula I and pharmaceutically acceptable salts thereof, for in vitro...
08/23/2011
7973051Aminothiazoles as FBPase inhibitors for diabetes
Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in claim 1 and which can be used in the form of pharmaceuti...
07/05/2011
7973050Enantiomeric compounds with antibacterial activity
Novel compounds in enantiomeric excess that are inhibitors of bacterial methionyl synthetase (MetRS) are disclosed. Also disclosed are methods for their preparation and their use in therapy as antibacterial agents, and in particular their use in therapy for Clost...
07/05/2011
7964612Therapeutic pyrazolyl thienopyridines
The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 h...
06/21/2011
7956068Inhibitors of human immunodeficiency virus replication
The present invention relates to compounds of formula (I) wherein c, X, Y, R2, R3, R4 and R6 are as defined herein, compositions and uses thereof for treating human immunodeficien...
06/07/2011
7943637Thienopyridine derivatives and the use thereof as HSP90 modulators
Novel thienopyridine derivatives of the formula (I), in which R1, R2, R3 and Y have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in w...
05/17/2011
7897613Crystalline polymorphs of clopidogrel
The present invention relates to novel crystalline forms of the platelet aggregation inhibitor (+)-(S)-methyl-2-(2-chlorophenyl)-(6,7-dihydro-4H-thieno[3,2-c]pyrid-5-yl)acetate, clopidogrel (1), in the form of hydrogen bromide salts, identified as polymorph forms 1,...
03/01/2011
7897615Cyanoamide compounds useful as malonyl-CoA decarboxylase inhibitors
The present invention provides previous methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibi...
03/01/2011
7897614Preventive agent/remedial agent for constipation predominant IBS
A novel preventive and/or therapeutic medicament for a constipation predominant IBS which contains as the active ingredient a thieno[3,2-b]pyridinecarboxamide derivative represented by the formula (I): wherein R1
03/01/2011
7893085Aza-benzothiophenyl compounds and methods of use
The invention relates to azabenzothiophenyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azabenzothiophenyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for ...
02/22/2011
7893086Sirtuin modulating compounds
Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, dis...
02/22/2011
7875627Thienopyridyl compounds that inhibit vanilloid receptor subtype 1 (VR1) and uses thereof
The present invention discloses fused thienopyridyl compounds of general formula (I) wherein X1-X6, R5-R7, Z1 and L are as defined in the description. The resent invent...
01/25/2011
7872019Polymorphs and amorphous form of (S)-(+)-clopidogrel bisulfate
The present invention relates to new polymorphs of S-(+)-Clopidogrel bisulfate and a process for preparing the same. ...
01/18/2011
7795275Method of treatment or prophylaxis
The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2...
09/14/2010
7781451Thiazolopyridine derivatives, pharmaceut ical conditions containing them and methods of treating glucokinase mediated conditions
The present invention provides compounds of the formula which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the co...
08/24/2010
7772247Substituted thieno[3,2-d]pyridines as inhibitors of the VEGF receptor and HGF receptor
The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for tr...
08/10/2010
7759360Methods and materials for the treatment of testosterone deficiency in men
The present invention relates to the use of compositions comprising trans-clomiphene for treating men with hypogonadism. The invention is also directed to methods for treating males with hypogonadism. ...
07/20/2010
7750021Immunosuppressant compounds and compositions
The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by...
07/06/2010
7750020Sulfonamide-thiazolpyridine derivatives as glucokinase activators useful the treatment of Type 2 diabetes
The present invention provides compounds of the formula (I), which are activators of glucokinase activity and, thus, may be employed as therapeutic agents for the treatment of glucokinase mediated conditions. Accordingly, the compounds of formula (I) may be employed...
07/06/2010
7737160Thienopyridine and furopyridine kinase inhibitors
Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using th...
06/15/2010
7737159Antibacterial compounds
Bacterial protein synthesis-inhibiting compounds having formula (I) and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates in the processes, compositions containing the compou...
06/15/2010
7696223Pyrrolo- and Thiazolo-pyridine compounds, and methods of use thereof
The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF). ...
04/13/2010
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
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
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
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
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
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
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
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
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
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