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Class 514/210.17 - Having -C(=X)-, wherein X is chalcogen, bonded directly to the four-membered hetero ring


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein a -C(=X)- group, wherein
No. of patents: 130
Last issue date: 05/08/2012


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NumberTitleIssue Date
8173634Polymorphic form of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic
This invention relates to a novel crystalline form (Form A) of 1-(4-{1-[(E)-4-cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl}-2-ethyl-benzyl)-azetidine-3-carboxylic acid (Compound I), to pharmaceutical compositions comprising this crystalline form, to processes ...
05/08/2012
8163727Biphenyloxyacetic acid derivatives for the treatment of respiratory disease
The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their...
04/24/2012
8080542S1P receptor modulating compounds and use thereof
The present invention relates to amides that have activity as SIP receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or pre...
12/20/2011
7939519Immunosuppresant 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...
05/10/2011
7825109Compound capable of binding S1P receptor and pharmaceutical use thereof
A compound having an ability to bind to an S1P receptor (particularly EDG-6, preferably EDG-1 and EDG-6), for example, the compound represented by formula (I) of the present invention, a salt thereof, a solvate thereof or a prodrug thereof is useful for prevention a...
11/02/2010
7820645Crystalline forms
There are provided crystalline forms of the compounds Ph(3-Cl)(5-OCHF2)—(R)CH(OH)C(O)-Aze-Pab(OMe) and Ph(3-Cl)(5-OCHF2)—(R)CH(OH)C(O)-Aze-Pab(OH), pharmaceutical compositions containing them, processes for obtaining them and their use in m...
10/26/2010
7737135Biphenyloxyacetic acid derivatives for the treatment of respiratory disease
The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their...
06/15/2010
7727978Cyclic 11-beta hydroxysteroid dehydrogenase type I inhibitors
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrog...
06/01/2010
7691843N-hydroxyamide derivatives possessing antibacterial activity
Novel N-hydroxyamide derivatives are disclosed. These N-hydroxyamide derivatives inhibit UPD-3-O—(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase, an enzyme present in gram negative bacteria and are therefore useful as antimicrobials and antibiotics. Methods...
04/06/2010
7678785Substituted aniline derivatives
The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections. ...
03/16/2010
7494988Inhibitors of serine proteases, particularly hepatitis C virus NS3 protease
The present invention relates to compounds that are useful as protease inhibitors, particularly as serine protease inhibitors, and more particularly as hepatitis C NS3 protease inhibitors. As such, they act by interfering with the life cycle of the hepatitis C virus...
02/24/2009
7378440Substituted benzoylureido-o-benzoylamides, process for their preparation and their use
The invention relates to substituted benzoylureido-o-benzoylamides and to their physiologically tolerated salts and physiologically functional derivatives. The invention relates to compounds of the formula I in which...
05/27/2008
7309714Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved...
12/18/2007
7288537Azetidine derivatives as CCR-3 receptor antagonists
Compounds of formula I in free or salt form, wherein Ar, X, Y, R1, R2, R3, R5, m, n, p and q have the meanings as indicated in the specification, are useful for treatin...
10/30/2007
7279578Sulfonylamino-acetic acid derivatives
The invention relates to novel sulfonylamino-acetic acid derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of such compounds, pharmac...
10/09/2007
7273858Salts
There is provided pharmaceutically-acceptable acid addition salts of compounds of formula I, wherein R1 represents C1-2 alkyl substituted by one or more fluoro substituents;
09/25/2007
7250516Phenylalanine derivatives
Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning α4 integrin i...
07/31/2007
7244748Pyridines for treating injured mammalian nerve tissue
The invention provides novel pyridines, pharmaceutical compositions comprising such pyridines, and the use of such compositions in treating injured mammalian nerve tissue, including but not limited to an injured spinal cord. In one embodiment, the compounds, composi...
07/17/2007
7241757Amidino derivatives and their use as thrombin inhibitors
There is provided compounds of formula I wherein R1, Rx, Y, Ry, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases...
07/10/2007
7238683Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-RV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is in...
07/03/2007
7232812Substituted azetidine compounds, their preparation and use as medicaments
The present invention relates to substituted Azetidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals. ...
06/19/2007
7230000Methods and compositions utilizing quinazolinones
Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity ...
06/12/2007
72207341-(amino)indanes and (1,2-dihydro-3-amino)-benzofurans, benzothiophenes and indoles as Edg receptor agonists
The present invention encompasses compounds of Formula (I): as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejecti...
05/22/2007
7202236Modified release pharmaceutical formulation
A modified release pharmaceutical composition comprising, as active ingredient, a compound of formula (I), wherein R1 represents C?1-2#191 alkyl substituted by one or more fluoro substituents; R2 represents hydrogen, hydroxy, methoxy or ethoxy;...
04/10/2007
7196201Pyrrolidines as dipeptidyl peptidase inhibitors
The present invention relates to novel compounds, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their production and their therapeutic utility
03/27/2007
7160902Amide derivatives and methods of their use
Amide derivatives of the general formulae Ia and Ib: are disclosed. Pharmaceutical compositions containing these compounds, and methods for their use, inter alia, for treating and/or preventing gastrointestinal d...
01/09/2007
7160874Phenylalanine derivatives
Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin. ...
01/09/2007
7144899Thrombin inhibitors
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure Formula (I): wherein u is CH or N; Q is 1)—N(R25)CH(R30)— wherein the nitrogen atom is attached to R1
12/05/2006
7129233Mandelic acid derivatives and their use as thrombin inhibitors
There is provided a compound of formula I wherein Ra, R1, R2, Y and R3 have meanings given in the description and pharmaceutically-acceptable derivatives (including pro...
10/31/2006
7087594Alkyl ether derivatives or salts thereof
An alkyl ether represented by the general formula: or its salt. This compound has activity to protect neurons, activity to accelerate nerve regeneration and activity to accelerate neurite extension and hence is u...
08/08/2006
7084120Prodrugs of DP IV-inhibitors
Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds can be used in the treatment of impaired glucose tolerance, glucosuria,...
08/01/2006
7060697Immunosuppressant 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...
06/13/2006
7056907Mandelic acid derivatives and their use as thrombin inhibitors
There is provided a compound of formula (1) and pharmaceutically-acceptable derivatives (including prodrugs) thereof. Which compound and derivatives are useful as, or are as useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, a...
06/06/2006
7041314GPE analogs and peptidominetics
This invention relates to analogs and peptidomimetics of glycyl-L-prolyl-L-glutamic acid (GPE). In particular, this invention relates to GPE analogs and peptidomimetics that are anti-apoptotic and anti-necrotic, to methods of making them, to pharmaceutical compositi...
05/09/2006
7030147Combinations comprising an antidiarrheal agent and an epothilone or an epothilone derivative
Epothilone derivatives are co-administered with an antidiarrheal agent, e.g., a DPP-IV inhibitor, in the treatment of a proliferative disease. ...
04/18/2006
6921758Amino acid derivatives
There is provided amino acid derivatives of formula I, wherein p, q, R1, R2, R3, R4, Y, n and B have meanings given in the description which are useful as competitive inhibit...
07/26/2005
6872717Pharmacological uses of azetidine derivatives
A method of treating or preventing obesity, this method comprising administering to a patient in need of such treatment an effective amount of a compound of formula in which R, R3 and R4 are as de...
03/29/2005
6864249Piperidine and azetidine thrombin inhibitors
The present invention relates to a compound having formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I and pharmaceutical compositions containing them are of the class of thrombin inhib...
03/08/2005
6855706Phenylalanine derivatives
Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α 4 integrin. They are used as therapeutic agents for various diseases concerning α 4 integrin. ...
02/15/2005
6831078Azetidinecarboxamide derivatives for treating CNS disorders
A compound of formula (1) wherein R1 is aryl; and R2 is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and their use in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epi...
12/14/2004
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