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Class 548/535 - The five-membered hetero ring is further unsubstituted or alkyl substituted only (e.g., proline, etc.)


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the five-membered hetero ring is further
No. of patents: 178
Last issue date: 09/22/2009


1          
NumberTitleIssue Date
7592465Fertilizer/plant vitalizer
Contamination by microorganism of an aqueous proline solution is prevented by adjusting a proline concentration of the solution to 20% (W/W/) or more. Such solutions are useful as fertilizers and/or plan vitalizers. Preservation of the novel solutions are possible o...
09/22/2009
7371871Inhibitors of glutaminyl cyclase
The present invention relates to compounds that act as inhibitors of QC including those represented by the general formulae 1 to 9: and combinations thereof for the treatment of neuronal disorders, especially Alzheimer's di...
05/13/2008
7368421Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis
The present invention provides a new use of DP IV-inhibitors. The compounds of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, are useful in treating conditions mediated by DP IV or DP IV-like enzymes, such as imm...
05/06/2008
7368576Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for treating conditions mediated by DPIV or DPIV-like enzymes, such as cancer and tumors. In a more pre...
05/06/2008
7335645Effectors of dipeptidyl peptidase IV for topical use
The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least one f...
02/26/2008
7230119Process for the preparation of substituted pyrrolidine derivatives and intermediates
Two syntheses are provided; one for the preparation of (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol, and other for the preparation of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol. (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is prepared using the achiral ylide prepared from ben...
06/12/2007
7230074Inhibitors of dipeptidyl-aminopeptidase type IV
Peptide inhibitors of dipeptidyl-aminopeptidase type IV (DP-IV) are provided. The peptide inhibitors have an isomeric purity of about 96–99 percent. The peptide inhibitors include one or more amino acids covalently coupled to boroproline moiety. The compounds are ...
06/12/2007
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
7166579Prodrugs 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,...
01/23/2007
7166580Compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, su...
01/23/2007
7144856Inhibitors of dipeptidyl peptidase I
The present invention relates to specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I)which can be used in the treatment of malignant cell degeneration, immune diseases impaired wound healing and metabolic diseases of humans and are represented ...
12/05/2006
7132104Modulation of central nervous system (CNS) dipeptidyl peptidase IV (DPIV) -like activity for the treatment of neurological and neuropsychological disorders
The present invention discloses a method for therapeutically treating an animal, including a human, for psychosomatic, depressive and neuropsychiatric diseases, such as anxiety, depression, insomnia, schizophrenia, epilepsy, spasm and chronic pain. Administration of...
11/07/2006
7109347Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents
The present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for treating conditions mediated by DPIV or DPIV-like enzymes, such as cancer and tumors. In a more pre...
09/19/2006
7070941Methods and compositions for tagging via azido substrates
The invention provides methods and compositions for azide tagging of biomolecules. In one embodiment of the invention, proteins are tagged by metabolic incorporation of prenylated azido-analog substrates. Examples of such analogs are azido farnesyl diphosphate and a...
07/04/2006
7053055Compounds of unstable DP IV-inhibitors
Novel compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The compounds can be used in the treatment of impaired glucose tolerance, glucosuria, hyperlipi...
05/30/2006
6992067Diphenylazetidinones, process for their preparation, medicaments comprising these compounds and their use
Compounds of the formula I, in which R1, R2, R3, R4, R5, and R6 have the meanings given in the description, and their physiologically acceptable salts. The compounds are suitable for use, for example, as hypolipidemics....
01/31/2006
6949658Process for producing optically active α-amino acid and optically active α-amino acid amide
The present invention provides a process for efficiently producing an optically active α-amino acid and an optically active α-amino acid amide. After contacting with cells or processed cells thereof having an ability to asymmetrically hydrolyse, a water solvent is...
09/27/2005
6949515Effectors of dipeptidyl peptidase IV for topical use
The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least ...
09/27/2005
6946480Glutaminyl based DPIV inhibitors
The present invention provides compounds of the formula: wherein X═CH2 or S or pharmaceutical acceptable salts thereof useful for treating conditions mediated by DPIV or DPIV-like enzymes, such as arthriti...
09/20/2005
6939855Anti-inflammatory compositions and method
The disclosed invention includes pharmaceutical compositions and methods for treating inflammatory conditions, particularly those that are characterized by increased binding of alpha-9 integrin to one or more of its ligands. Also disclosed are methods for selecting ...
09/06/2005
6911467Antidiabetic agents
Compounds which are 1-(2′-aminoacyl)-2-cyanopyrrolidine derivatives according to general formula (1) are DP-IV inhibitors for treatment of impaired glucose tolerance or type 2 diabetes; wherein A is selected from groups (2, 3 and 4); X is selected from aminoacyl g...
06/28/2005
6903075Heterocyclic amide compounds as cell adhesion inhibitors
Compounds of Formula I are antagonists of VLA-4 and/or α4β7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions an...
06/07/2005
6884782STAT modulators
The present invention provides compounds, compositions and methods for the inhibition or treatment of conditions or disorders modulated by the STAT transcription factors, particularly STAT4 and STAT6. Additionally, the compounds are useful for the diagnosis of condi...
04/26/2005
6875737Multivalent compounds for crosslinking receptors and uses thereof
Synthetic crosslinking homobivalent and heterobivalent compounds have been designed and developed. These compounds are low in molecular weight, have antagonistic or agonistic activity, and induce the association between two identical or similar natural receptors (ho...
04/05/2005
6872805Hepatitis C virus inhibitors
The present invention relates to tripeptide compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. In particular, the present invention provides novel tripeptide analogs, pharmaceutical compositions containing such analogs and me...
03/29/2005
6673772Dipeptide compounds and their use as antiviral agents
A novel dipeptide compound inhibiting the enzymatic activity of HIV protease and an anti-AIDS medicine comprising this dipeptide compound as an effective component represented by formula (I) ##STR1## wherein R1, R2, and R3...
01/06/2004
6645939Substituted ଲ-alanine derivatives as cell adhesion inhibitors
ଲ-Alanine derivatives of Formula I are antagonists of VLA-4 and/or 댔ଲ.sub.7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated in...
11/11/2003
6632950Process for the preparation of derivatives of 4-amino-3-hydroxypyrrole-2-carboxylic acid
Novel processes and intermediates are provided for the synthesis of derivatives of 4-amino-3-hydroxypyrrole-2-carboxylic acids that are useful as monomers for polyamides capable of binding dsDNA. According to one preferred reaction scheme, an alkyl alkoxy...
10/14/2003
6632825Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
Compounds of the formula: ##STR1## where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containi...
10/14/2003
6627760Amorphous compound
The present invention relates to a novel form of (S)-1-[N2 -(1-carboxy-3-phenylpropyl]-L-lysyl]-L-proline known under the generic name lisinopril. Further, the present invention also relates to the use of the novel amorphous form of lisinopril ...
09/30/2003
6613879FAP-activated anti-tumour compounds
The invention relates to a prodrug that is capable of being converted into a drug by the catalytic action of human fibroblast activation protein (FAP଱), said prodrug having a cleavage site which is recognised by FAP଱, and said drug being cytot...
09/02/2003
6559127Compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g....
05/06/2003
6552038Anticoagulant agents
This invention relates to a compound of the Formula I X--C(O)--Y--G--R I (wherein X, Y, G and R have the values defined in the description), or a pharmaceutically acceptable salt thereof, processes and intermediates for the preparation of such a compound or ...
04/22/2003
6515179Process for the removal of nitrobenzenesulfonyl
A 2- or 4-nitrobenzenesulfonamide is allowed to react with an alkali metal alkoxide to remove a nitrobenzenesulfonyl group to thereby obtain an amine corresponding to the amide. Furthermore, a method for producing an amine derivative by allowing the resul...
02/04/2003
6509477Small molecule inhibitors of rotamase enzyme activity
This invention relates to neurotrophic compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase...
01/21/2003
6489300Carbamyloxy compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g....
12/03/2002
6462173Inhibitors of phosphoserine and phosphothreonine-proline-specific isomerases
Inhibitors of phosphoserine- or posphothreonine-specific peptidyl prolyl isomerases are described. Such inhibitors include molecules that mimic the structure and conformation of the pSer/pThr-Pro peptide moiety of the isomerase substrate when the substrat...
10/08/2002
6458769Amorphous compound
The present invention relates to a novel form of (S)-1-[N2 -(1-carboxy-3-phenylpropyl]-L-lysyl]-L-proline known under the generic name lisinopril. Further, the present invention also relates to the use of the novel amorphous form of lisinopril ...
10/01/2002
6440937Dipeptide benzamidine as a kininogenase inhibitor
Compounds of the formula I ##STR1## where R, R1, R2, R3, R4, R5 and R6, and l, m and n have the meanings stated in the description, and their preparation are described. The novel compounds ...
08/27/2002
6432923VLA-4 antagonists
Compounds of the formula I ##STR1## as defined, and their pharmaceutically acceptable salts are VLA-4 antagonists which are useful in inhibiting cell adhesion and in the therapeutic or prophylactic treatment of inflammatory and autoimmune diseases, p...
08/13/2002
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