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Class 544/387 - Plural -C(=X)- groups bonded directly to the piperazine ring


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein at least two groups are bonded directly
No. of patents: 105
Last issue date: 08/30/2011


1      
NumberTitleIssue Date
8008492Compounds that act as a vehicle for delivery through the blood-brain barrier and charge delivery vehicle constructions
Compounds of formula (I), where R1 and R3 are H or (C1-C4)-alkyl; R2 is H or a C-radical derived from one of the known ring systems with 1-4 rings; X1 is a (C1-C6)-alkyl biradica...
08/30/2011
7714131Process for the stereoselective preparation of (−)-halofenate and derivatives thereof
The present invention provides a compounds the formula (IV): and methods for producing an α-(phenoxy)phenylacetic acid compound of the formula: wherein R1 is a member ...
05/11/2010
7384943Substituted chroman derivatives
The present invention relates to new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives having the formula (I) wherein X is N; Y is NR2CH2, CH2
06/10/2008
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
7176207Platelet adenosine diphosphate receptor antagonists
Compounds of the following formula (I): where A, a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate...
02/13/2007
7094895Tyrosyl derivatives and their use as P2X7 receptor modulators
The present invention relates to compounds of the formula wherein R1 and R2 are independently hydrogen, C1–C4 alkyl, C1–C4 substituted alkyl, C1–C4 alkoxy, C1â...
08/22/2006
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
6872825Peptide β-turn mimetic compounds and processes for making them
The subject invention involves compounds having structure (I), wherein: (a) R1 is hydrogen or alkyl; and R2 is selected from hydrogen, alkyl, aryl, heterocyclyl, carboxy and its esters and amides; or R1 and R2 are attached and are together alkylene or heteroalkylene...
03/29/2005
6858599Tricyclic compound having spiro union
This invention relates to tricyclic compounds having spiro union represented by the following formula (I) or its salt which is useful as a drug, and in particular, as an inhibitor for activated blood coagulation factor X, which can be administered orally and which e...
02/22/2005
6818637Polyhydroxypyrazine derivatives, their preparation and the pharmaceutical compositions which comprise them
The invention concerns novel derivatives of formula (I) wherein: R1 represents the stereoisomeric forms of the chain —(CHOH)3—CH2—O—COR (II) and either R2 represents ...
11/16/2004
6809202Diketodiazacyclic compounds, diazacyclic compounds and combinatorial libraries thereof
The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl gorup and 6-8 atoms in...
10/26/2004
6635786Symmetrically disubstituted aromatic compounds and pharmaceutical compositions for inhibiting poly (ADP-ribose) glycohydrolase, and methods for their use
Symmetrically disubstituted aromatic compounds and pharmaceutical compositions containing such compounds that inhibit and/or modulate the activity of poly(ADP-ribose) glycohydrolase, also known as PARG, are described. The invention is also directed to the...
10/21/2003
6608061Bisaryl compound and medicament for cancer treatment comprising the same
A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1 --S--R1 --S--Ar2 wherein R1 represents a nonmetal bridging...
08/19/2003
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
6531476Piperazine derivatives inhibiting human immunodeficiency virus replication
The invention concerns the use of a piperazine derivative of formula (I) ##STR1## wherein: A and B=C.dbd.O, C.dbd.S or CR7 R8 with R7 =H, methyl, cyano, cyanomethyl, CO2 CH3 or (C.dbd.O)CH3 and ...
03/11/2003
6521619Aryl phenylcyclopropyl sulfide derivatives and their use as cell adhesion inhibiting anti-inflammatory and immune suppressive agents
The present invention relates to novel cyclopropane-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or ...
02/18/2003
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
6441172Diketodiazacyclic compounds, diazacyclic compounds and combinatorial libraries thereof
The synthesis of individual di- and tri-substituted-1,4-diazacyclic compounds having 6- to 8-atoms in the cyclic ring, their corresponding 1,6-diketo-2,5-diazacyclic compounds and similar 1,4-diazacyclic ring compounds having one ring carbonyl group and 6...
08/27/2002
6399613Pyrazine derivatives, their preparation and medicaments containing them
The invention concerns pyrazine derivatives of formula (1) in which a pharmaceutical composition comprising at least one compound of formula: ##STR1## in which R represents a nitrogen atom, R1 and R3 each represent the same radical s...
06/04/2002
6344466Benzamide and sulfonamide substitued aminoguanidines and alkoxyguanidines as protease inhibitors
The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: ##STR1## wherein X is O or NH, L is --O-- or --SO2 --, and R1 -R4, R9 -R19, Ra...
02/05/2002
6340682Diamide compound and drugs containing the same
The present invention provides diamide derivatives represented by the following general formula (1): ##STR1## wherein A is a phenyl group or the like, which may be substituted, B is --CH.dbd.CH--, --C.dbd.C--, --(CH.dbd.CH)2 --, --C.ident....
01/22/2002
6303611Kappa agonist compounds and pharmaceutical formulations thereof
Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formula having the structure: ##STR1## wherein R1, R2, and X Y, Z, Ar and n are as describe...
10/16/2001
61438931,4-bis{ଲ-[N-methyl-N-(2-hydroxyethyl)amino]propionyl}piperazine and process for its preparation
The compound of formula is useful as chain extender in the preparation of polymers, in particular of linear and cross-linkable, heparinizable, biocompatible polymers....
11/07/2000
6057323Kappa agonist compounds pharmaceutical formulations and method of prevention and treatment of pruritus therewith
Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compound of formula I, having the structure: ##STR1## wherein R1, R2 ...
05/02/2000
6022873Metalloproteinase inhibitors
Compounds of formula (I) ##STR1## wherein n, V, R1, R2, R3 and R4 are as defined in the specification are matrix metalloproteinase inhibitors....
02/08/2000
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
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
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
5892039Piperazino derivatives as neurokinin antagonists
The invention relates to compounds of the formula ##STR1## These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma....
04/06/1999
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
5869554Polycarbonate compositions comprising hindered amine light stabilizers and ultraviolet light absorbers
Weatherable polycarbonate compositions (formulations or blends) comprise at least one of a piperazinone and piperazine dione based HALS, and at least one of a benzotriazole, benzophenone, triazine, oxanilide, and cyanoacrylate based UVA. The combination o...
02/09/1999
5756504Tocolytic oxytocin receptor antagonists
Compounds of the formula X--Y--R, or the pharmaceutically acceptable salts and esters thereof, wherein X is ##STR1## Y is --SO2 --, --(CH2)p -- or --CO--(CH2)p --; R is unsubstituted or substitut...
05/26/1998
5756742Polymerizable compounds
Polymerizable compounds based on N-acylamido-piperazines are provided. Such compounds have the formula: ##STR1## wherein: a, b, c and d are independently 0 or 1 and the sum of a, b, c and d is at least 3. R1, R2, and R3
05/26/1998
5756505N-acylpiperazine derivative, antibacterial drug and anti-ulcer drug
An N-acylpiperazine derivative or a salt thereof in accordance with the present invention is represented by the following formula 1: ##STR1## wherein R1 represents a lower alkyl, hydroxy lower alkyl, lower acyl, or arylcarbonyloxy lower al...
05/26/1998
5736539Inhibitors 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...
04/07/1998
5670505Piperazine derivatives
A piperazine compound of the formula: ##STR1## wherein: X is carbonyl or sulfonyl; Y is a direct bond or lower alkylene; and R1, R2, R3, R4 are as defined herein. The compounds are advantageously used as Tachyki...
09/23/1997
5654465Process for the production of cyanocinnamamides
This invention provides a process for producing cyanocinnamamides. More particularly, the invention provides a process for condensing an cyanoacetamide with a carbonyl-containing compound to produce cyanocinnamamides in good yield....
08/05/1997
5650412HIV protease inhibitors useful for the treatment of AIDS
Compounds of formula ##STR1## are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ...
07/22/1997
5646151Kappa agonist compounds and pharmaceutical formulations thereof
Compounds, compositions and method of treating hyperalgesia comprising a compound of formula I, II, III and IV as defined in the specification....
07/08/1997
5612479Polyphenols containing mesogenic moieties as lateral substituents
Novel polycyanate compositions containing one or more mesogenic moieties as lateral substituents are disclosed which provide improved processability relative to polycyanates containing one or more mesogenic moieties in the main chain of the molecule. Mole...
03/18/1997
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