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Class 544/388 - Chalcogen or acyclic nitrogen bonded directly to at least one of the -C(=X) groups


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein chalcogen (i.e., oxygen, sulfur, selenium,
No. of patents: 99
Last issue date: 05/31/2011


1      
NumberTitleIssue Date
7951943Method for preparing and purifying 3-hydroxyamidinophenylalanine compounds
The present invention relates to the preparation of 3-hydroxyamidino-phenylalanine derivatives in highly pure form which can be used for example as urokinase inhibitors. The present invention further relates to the use of high-purity 3-hydroxyamidinophenylalanine de... 		05/31/2011
7659396Method for the production of phenylalanine derivatives
The invention relates to an improved method for the production of 3-amidino- or 3-guanidinophenylalanine derivatives, especially triisopropylphenyl-sulfonyl-substituted 3-amidino- or 3-guanidinophenylalanine derivatives. ... 		02/09/2010
7538216Guanidino phenylalanin compounds used as urokinase inhibitors
The invention relates to the use of derivatives of 3-guanidinophenylalanine as urokinase inhibitors for treating malignant tumors and metastasis. ... 		05/26/2009
7247724Method for the production of phenylalanine derivatives
The invention relates to an improved method for the production of 3-amidinophenylalanine derivatives, especially triisopropylphenyl-sulfonyl-substituted 3-amidinophenylalanine derivatives. ... 		07/24/2007
7208497Substituted piperazines and diazepanes
A novel class of substituted piperazines and diazepanes, pharmaceutical compositions comprising them and use thereof in the treatment of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment of dis... 		04/24/2007
7138526Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives
A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries 		11/21/2006
70983382,3,4,4a-tetrahydro-1H-pyrazino(1,2-a) quinoxalin-5(6H)one derivatives
This invention provides compounds of formula I, wherein R is hydrogen or alkyl of 1–6 carbon atoms; R′ is hydrogen, alkyl of 1–6 carbon atoms, acyl of 2â€... 		08/29/2006
7026323Platelet adenosine diphosphate receptor antagonists
Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmace... 		04/11/2006
6921822Process for stereoselectively reducing 4-aryl-4-oxobutanoic acid derivatives
The present invention relates to a process for preparing stereoisomerically enriched 4-aryl-4-hydroxybutanoic acid derivatives by reducing 4-aryl-4-ketobutanoic acid derivatives in the presence of ruthenium-containing catalysts. ... 		07/26/2005
6903092Naphthamide neurokinin antagonists for use as medicaments
Compounds having the general formula wherein R1, R2, R3, R4, R5, X1 and X2 are as defined in the specification, methods of using such compoun... 		06/07/2005
6878712Amides as inhibitors for pyruvate dehydrogenase
A compound of formula (I): wherein: Ring A is a nitrogen linked mono or bicyclic heterocyclic ring as defined within; R1 and R2 are independentl... 		04/12/2005
6803370Alpha amino acid derivatives—inhibitors of leukocyte adhesion mediated by VLA-4
Disclosed are certain alpha amino acid 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... 		10/12/2004
6680320Urokinase inhibitors
The invention relates to the use of derivatives of 3-amidinophenylalanine as urokinase inhibitors for treating malignant tumors and the formation of metastases.... 		01/20/2004
6624169Urokinase inhibitors
The invention relates to the use of derivatives of 3-amidinophenylalanine as urokinase inhibitors for treating malignant tumors and the formation of metastases.... 		09/23/2003
6534509Piperazine derivatives and their use as anti-inflammatory agents
This invention is directed to acyl piperazine derivatives, for example, of the following formula (1a): ##STR1## wherein R1a, R2, R3, R4, R5, and R6 are descried herein. These derivatives ar... 		03/18/2003
6506733Compounds and compositions as protease inhibitors
Compounds of the formula: ##STR1## are provided, and are useful as cysteine protease inhibitors, particularly in the treatment of diseases such as osteoporosis or autoimmune disorders in which cathepsins K or S contribute to the pathology or symptomatolgy... 		01/14/2003
6492368Benzamidine derivatives as factor XA inhibitors
Novel compounds of the formula I ##STR1## in which X, Y, R1, R2 and R3 are as defined in Patent Claim 1 are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.... 		12/10/2002
6218389Acyclic metalloprotease inhibitors
The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of... 		04/17/2001
6133442Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists
Compounds of formula I ##STR1## wherein R1 signifies phenyl, substituted phenyl or heterocyclyl; R2 signifies phenyl or substituted phenyl; R3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phenyl, su... 		10/17/2000
6127372Sulfonamide inhibitors of aspartyl protease
This invention provides a novel class of sulfonamide compounds of formula I which are aspartyl protease inhibitors: ##STR1## This invention also provides pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical composi... 		10/03/2000
6117870Cyclic amide derivatives
A cyclic amide derivative of formula (I): ##STR1## wherein R1 represents a substituted alkyl group, a substituted alkenyl group, a substituted amino group, a substituted alkoxyl group, a substituted alkylthio group, a substituted carbamoyl... 		09/12/2000
6080860Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor
Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediate... 		06/27/2000
6054457Benzamide derivatives and their use as vasopressin antagonists
This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R1 is aryl optionally substituted with lower alkoxy, etc., R2 is lower... 		04/25/2000
6001835Inhibitors of farnesyl-protein transferase
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invent... 		12/14/1999
5977364Process for preparing 4-tert-butyloxycarbonyl-(S)-piperazine-2-tert-butylcarboxamide
An improved process using chiral hydrogenation is described for the synthesis in high yields of a 4-protected-(S)-piperazine-2-tert-butylcarboxaimide, an intermediate for an HIV protease inhibitor.... 		11/02/1999
5977114Selective thrombin inhibitors
The present invention relates to a novel selective thrombin inhibitor having the following formula (I), which is also effective by oral administration: ##STR1## in which R1 represents acetyl substituted with aryl or aryloxy, or repres... 		11/02/1999
5968938Piperazine oxytocin receptor antagonists
This invention relates to certain novel piperazine compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. T... 		10/19/1999
5962456N-acylpiperazine derivative, anti-ulcer drug, and antibacterial drug
An N-acylpiperazine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein R1 represents a pyridylcarbonyloxy lower alkyl group, a benzoylamino lower alkyl group, benzyl group, carbamoyl group, pyridyl gro... 		10/05/1999
5962682Aryl- and hetaryl-sulfonamide derivatives, their preparation and their use as endothelin antagonists
Compounds of formula (I) ##STR1## wherein R1 signifies phenyl, substituted phenyl or heterocyclyl; R2 signifies phenyl or substituted phenyl; R3 signifies hydrogen, lower-alkyl, cyano, carboxy, esterified carboxy, phe... 		10/05/1999
5962487Antipicornaviral compounds and methods for their use and preparation
Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating p... 		10/05/1999
5945534Process for the preparation of optically active piperazine-2-carboxylic acid derivatives
Optically active piperazine-2-carboxylic acid derivatives of the general formula: ##STR1## in which X is alkoxy or a (substituted) amino group, are prepared by asymmetric hydrogenation of the corresponding pyrazinecarboxylic acid derivatives, ca... 		08/31/1999
5929077Thioproline-containing inhibitors of farnesyl protein transferase
Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected b ##STR1## its enantiomers, diastereomers, and pharmaceutically acceptable salts and solvates thereof.... 		07/27/1999
5922707Oxazolidinone antibacterial agent with tricyclic substituents
This invention provides novel oxazolidinone derivatives represented by chemical Formula (I), or pharmaceutically acceptable salts thereof: ##STR1## wherein X is NR1, CR2 R3, O, S, SO, or SO2 ; and Z is NR 		07/13/1999
5919777Compounds with growth hormone releasing properties
The present invention relates to novel compounds of the general formula I ##STR1## which can be used for treating medical disorders resulting from a deficiency in growth hormone.... 		07/06/1999
59143246-Hydroxy and 6-oxo-androstane derivatives active on the cardiovascular system and pharmaceutical compositions containing same
6-hydroxy and 6-oxo-androstane derivatives of formula (I), active on the cardiovascular system. ##STR1## wherein: the symbol A represents CH--OR, C.dbd.N--OR, CH--CH.dbd.N--OR and C.dbd.CH--N--OR; and R1, R2 and R3 ar... 		06/22/1999
5886181Process for the preparation of optically active piperazine-2-carboxylic acid derivatives
Optically active piperazine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein R1 and R2 are inter alia hydrogen, alkyl or acyl and X is alkoxy or a (substituted) amino group, are prepared by asymmetric ... 		03/23/1999
5859015N-heterocyclic piperazinyl and H-heterocyclic piperazinonyl inhibitors of farnesyl-protein transferase
The present invention is directed to compounds of the formula A which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras: ##STR1## The invention is further directed to chemotherapeutic compositions con... 		01/12/1999
5856485Process for preparing 2-piperazinecarboxylic acid derivatives
A process for preparing 2-piperazinecarboxamides in the form of their enantiomers or their enantiomer mixtures of the general formula: ##STR1## wherein R1 is (a) unsubstituted or substituted alkyl or (b) --OR4, wherein R4 		01/05/1999
5807856Alpha 1a adrenergic receptor antagonist
This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These ... 		09/15/1998
5801178Aniline derivative having polyunsaturated fatty acid residue and use thereof
An aniline derivative of the formula (1) ##STR1## wherein R1 is an eicosapentaenoyl or docosahexaenoyl; R2 and R3 are each independently an alkyl or alkoxy having 1 to 6 carbon atoms, or a halogen atom; R4 ... 		09/01/1998
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