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Class 548/266.6 - The additional unsaturated hetero ring and the triazole ring are attached to the same acyclic atom or to the same acyclic chain


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the triazole ring and the additional unsaturated
No. of patents: 161
Last issue date: 03/25/2008


1          
NumberTitleIssue Date
7348440Mitotic kinesin inhibitors
The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comp...
03/25/2008
7223780Triazole-derivatives as blood clotting enzyme factor Xa inhibitors
The present invention is directed to the compound of formula I which is useful for inhibiting the activity of blood clotting enzyme Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their us...
05/29/2007
7102012Process for preparing N,N'-carbonyldiazoles
A process is provided for preparing N,N′-carbonyldiazoles by reacting azoles with phosgene in halogenated aliphatic hydrocarbon solvents, the entirety of the azole for reaction being introduced in the solvent, followed by the addition of phosgene. ...
09/05/2006
7094904Process for preparing monohydrate and crystal modifications of fluconazole
A new process is disclosed for the synthesis of fluconazole monohydrate and for crystal modifications of fluconazole which comprises the step of hydrolyzing a silyl ether of the formula (II)
08/22/2006
6969727Heterocyclic aromatic compounds useful as growth hormone secretagogues
Heterocyclic aromatic compounds are provided which are useful in stimulating endogenous production or release of growth hormone and in treating obesity, osteoporosis (improving bone density) and in improving muscle mass and muscle strength. The heterocyclic a...
11/29/2005
6831177Processes for the preparation of substituted propenone derivatives
Industrial and commercial processes for the preparation of 2-acyl-5-benzylfuran derivatives, 1,2,4-triazole-3-carboxylic acid ester derivatives or propenone derivatives having an anti-HIV activity; and useful crystals of the derivatives. A deblocking: (III-2), (IV-1...
12/14/2004
6759387Compositions and methods for enhancing drug delivery across and into epithelial tissues
This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, and the like. The compositions and methods are also useful for delivery acr...
07/06/2004
6630468Disubstituted pyrazolines and triazolines as factor Xa inhibitors
The present application describes disubstituted pyrazolines and triazolines of formulae I and II: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of M1 and M2 maybe N and D may be a variety of N-containing gro...
10/07/2003
6486159Water soluble prodrugs of azole compounds
Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula ##STR1## wherein A is the no...
11/26/2002
6451833N-substituted (଱-imidazolyl-toluyl)pyrrole compounds for treatment of circulatory disorders
A class of N-substituted (଱-imidazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein m is one; wherein each of R...
09/17/2002
6410582Thienylazolylalcoxyethanamines, their preparation and their application as medicaments
The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromati...
06/25/2002
6376526Triazole antifungal agents
An antifungal compound of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of either entity, wherein X is CH or N; R1 is phenyl subsituted with 1 to 3 substituents each independently ...
04/23/2002
6362206Azole compounds, their production and use
The present invention provides an azole compound represented by the formula (I): ##STR1## wherein Ar is an optionally substituted phenyl group; R1 and R2, the same or different, are a hydrogen atom or a lower alkyl group, or R
03/26/2002
6359141Water soluble prodrugs of azole compounds
Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula ##STR1## wherein A is the no...
03/19/2002
63589842,4-dioxopyrrolidine and 2,4-dioxotetrahydrofuran derivatives and medicines containing the same as the active ingredient
Compounds including 1-(biphenyl-4-yl)methyl-1H-1,2,4-triazoles and 1-(biphenyl-4-yl)methyl-4H-1,2,4-triazoles each having a (2,4-dioxopyrrolidine-5-ylidene) methyl or (2,4-dioxo-tetrahydrofuran-5-ylidene)methyl group as the substituent at the 2'-posi...
03/19/2002
6333323Indole derivatives with antiviral activity
A compound of the formula: ##STR1## wherein R1 is hydrogen, lower alkyl, or optionally substituted arylsulfonyl, or the like, R2 is hydrogen, lower alkyl, or optionally substituted aralklyl, or the like, R3, R4,...
12/25/2001
6316505Pharmaceutical compositions comprising fluorinated co-polymers
Block copolymers containing a fluorinated hydrocarbon unit, a hydrocarbon unit, and a poly(oxyethylene) unit are useful in fluid formulations of pharmaceutical agents. A typical embodiment is: C11 H23 --CONHC2 H4 NHC...
11/13/2001
6300357Triazole antifungal agent
A triazole compound having the formula: ##STR1## wherein Ar1 represents a phenyl group which may be substituted, Ar2 represents a heterocyclic group which may be substituted, R0 represents a hydrogen atom or a lower alkyl;...
10/09/2001
6265352Substituted carbamoyl triazoles and their use as herbicides
Substituted carbamoyltriazoles of the formula I as defined in the specification and the agriculturally useful salts thereof, processes for their preparation and their use as herbicides....
07/24/2001
6265584Water soluble prodrugs of azole compounds
Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided having the general formula ##STR1## wherein A is the no...
07/24/2001
6245804Nonsteroidal gestagens
This invention describes the new, nonsteroidal gestagens of general formula I ##STR1## in which A, B, Ar, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very ...
06/12/2001
6159995Substituted diaminocarboxylic acids
Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved....
12/12/2000
6127355High molecular weight polymer-based prodrugs
The present invention is directed compositions of the formula: ##STR1## wherein: D is a residue of a biologically active moiety; X is an electron withdrawing group; Y and Y' are independently O or S; (n) is zero (0) or a positive integer, preferably from 1 to ...
10/03/2000
6107321Diazabicyclooctane derivatives having selective 5-HT1Dalpha agonist activity
A class of 3-substituted 3,7-diazabicyclo[3.3.0]octane derivatives, further substituted at the 7-position by an optionally substituted alkenyl, alkynyl, arylcarbonyl, aryl-alkyl or heteroaryl-alkyl moiety, are selective agonists of 5-HT1 -like ...
08/22/2000
6080772Thiazole compounds and methods of modulating signal transduction
The present invention relates to thiazole containing compounds capable of inhibiting protein tyrosine phosphatase activity. The invention further relates to the use of such compounds to modulate or regulate signal transduction by inhibiting protein tyrosi...
06/27/2000
6063933Process for the manufacture of bis-triazole compounds and intermediates useful in the manufacture thereof having antifungal activity
The present invention relates to a process to prepare a compound of formula (I) wherein Y and Z can be identical or different and represent a halogene. The bis-triazole compounds of formula (I) and intermediates have antifungal activity....
05/16/2000
6057353Triazolyl-mercaptides and their use as microbicides
Triazoyl mercaptides of the formula (I) ##STR1## in which M is an alkaline metal cation, an equivalent of an alkaline earth cation, an equivalent of a copper zinc, iron or nickel cation or an ammonium cation and R1 is various radicals, a p...
05/02/2000
6051572Azetidine, pyrrolidine and piperidine derivatives
A class of azetidine, pyrrolidine and piperidine derivatives, substituted by inter alia a phenylmorpholinyl, phenylpiperidinyl or benzimidazolone moiety, are selective agonists of 5-HT1 -like receptors, being potent agonists of the human 5-HT
04/18/2000
6015825Triazole antifungal agents
The invention relates to compounds of the formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein Ar, Z and Het are as defined herein. The compounds of formula (I) possess activity as antifungal agents. The invention also relates ...
01/18/2000
6008368Pharmaceutical compositions for treatment of circulatory disorders using N-substituted (଱-imidazolyl-toluyl) pyrrole aniotensin II antagonists
Pharmaceutical compositions comprising a compound selected from a class of N-substituted (଱-imidazolyl-toluyl)pyrrole compounds are described for use in treatment of circulatory disorders. Compositions of particular interest comprise angiotensin II ...
12/28/1999
5981560Triazole antifungal agents
An antifungal compound of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of either entity, wherein X is CH or N; R1 is phenyl substituted with 1 to 3 substituents each independ...
11/09/1999
5872258Commercial process for the manufacture of fluconazole and intermediates useful in the manufacture thereof
A process for making Fluconazole is provided comprising carrying out the following scheme of reaction: ##STR1##...
02/16/1999
5861516Process for preparing an antifungal azole with hydrazino and amidrazone intermediates
A process for preparing an antifungal azole compound of formula (I) by reacting an epoxide with hydrazine to from a hydrazino compound which is subsequently reacted with an iminoether. The amidrazone product is subsequently reacted with an orthoformate to...
01/19/1999
5792780Azole compounds, their production and use
The present invention provides an azole compound represented by the formula (I): ##STR1## , wherein Ar is an optionally-substituted phenyl group; R1 and R2 are, the same or different, a hydrogen atom or a lower alkyl group,...
08/11/1998
5750719Commercial process for the manufacture of fluconazole and intermediates useful in the manufacture thereof
A process for making Fluconazole is provided comprising carrying out the following scheme of reaction: ##STR1##...
05/12/1998
5731434Endothelin antagonists
A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin....
03/24/1998
5710280Preparation of fluconazole and pharmaceutically acceptable salts thereof
A process for preparing fluconazole, including the steps of (1) acylating 1,3-difluorobenzene (DFB) to obtain 2-chloro-2',4'-difluoroacetophenone (CAP); (2) alkylating 4-amino-4H-1,2,4-triazole (4-AT) with CAP to obtain 2-(1H-1,2,4-triazol-1-yl)-2',4'-dif...
01/20/1998
5691363Fungicidal azole derivatives
Compounds having the formula ##STR1## wherein Q is ##STR2## R1 is C1 -C8 alkyl; R2 is C4 -C17 heterocyclic aryl, unsubstituted or substituted with one or more C1 -...
11/25/1997
5648372Antifungal agents, and compositions
A compound represented by the general formula: ##STR1## wherein R1 and R2 denote a halogen atom or hydrogen atom; R3 means a hydrogen atom or lower alkyl group; l, r and m stand for 0 or 1; A is N or CH; W denotes an ...
07/15/1997
5633386Commercial process for the manufacture of fluconazole and intermediates useful in the manufacture thereof
A process for making Fluconazole is provided comprising carrying out the following scheme of reaction: ##STR1##...
05/27/1997
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