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Class 548/331.5 - The nitrogen is bonded directly at the 2-position of the diazole ring


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the nitrogen is bonded directly to the
No. of patents: 146
Last issue date: 11/22/2011


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NumberTitleIssue Date
8063231Methods of treating alpha adrenergic mediated conditions
Described herein are novel N-(2 and/or 3-substituted benzyl)-4,5-dihydro-1H-imidazol-2-amine derivatives processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals modulators of subtype α2B and/or α2C... 		11/22/2011
7442717Substituted 2-aminoimidazoles, process for their preparation, their use as medicament or diagnostic aid
Novel substituted 2-aminoimidazoles of formula I, process for their preparation, their use as medicament or diagnostic aid, and medicament containing them. The compounds of this type are useful in the prevention or treatment of various disorders and can be employed ... 		10/28/2008
7439395Process for the preparation of guanidinium salts
The present invention relates to a two-step process for the preparation of guanidinium salts of the formula (1), where the substituents R have a meaning indicated in Claim, and A− is a sulfonate, alkyl- or arylsulfate, hydrogensulfate, imide, methanide,... 		10/21/2008
7427618Ethynyl derivatives as factor Xa inhibitors
Novel compounds of the formula (I), in which R1, R2, R3, X and Y have the meaning indicated in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic di... 		09/23/2008
7326792Heterocyclic compounds as P2X7 ion channel blockers
The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R1, R2, R3, R4, R5, X... 		02/05/2008
73040832-iminoimidazole derivatives (2)
A 2-iminoimidazole derivative represented by the formula: {wherein R1, R2 and R3 represent hydrogen, optionally substituted C1-6 alkyl, etc.; R6 represents h... 		12/04/2007
7279582Retroviral protease inhibiting compounds
A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed. ... 		10/09/2007
72651352-oxy, 2-amino, and 2-thio-imidazole compounds
The invention relates to novel 2-Oxy, 2-Amino, and 2-Thio-imidazole compounds of formula (I): wherein all variables are as herein defined, pharmaceutical compositions containing the compo... 		09/04/2007
7247733Process for preparing nuclear-fluorinated aromatics
The present invention relates to the preparation of nuclear-fluorinated aromatics by reacting, with a fluoride at 40 to 260° C., an aromatic compound substituted at the nucleus with halogen that is exchangeable for fluorine in the presence of at least one compound ... 		07/24/2007
7141680Aromatic compounds possessing antifungal or antibacterial activity
The present invention provides novel compounds possessing antibacterial, and/or antifungal activities. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided. ... 		11/28/2006
7091362Process for preparing nuclear-fluorinated aromatics
The present invention relates to the preparation of nuclear-fluorinated aromatics by reacting, with a fluoride at 40 to 260° C., an aromatic compound substituted at the nucleus with halogen that is exchangeable for fluorine in the presence of at least one compound ... 		08/15/2006
6956050Imidazole compounds as anti-inflammatory and analgesic agents
This invention provides a compound of the formula (I): wherein: R1 represents a hydrogen atom, an alkyl group, etc.; R2 represents a hydrogen atom, a halogen atom, etc.; R3 		10/18/2005
6949578Cycloalkyl alkanoic acids as integrin receptor antagonists
The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of select... 		09/27/2005
6911595Charge transfer material, and photoelectric conversion device and photoelectric cell using same, and pyridine compound
A charge transfer material comprising a basic compound having negative charge and represented by the following general formula (I): (A1-L)n1-A2·M  (I), wherein A1 represents a group having negativ... 		06/28/2005
6891068Water as promoter in the nucleophilic substitution of chloride
Disclosed is a one step method for preparing a β-substituted sulfide by treating a β-halosulfide with a nucleophile in water. ... 		05/10/2005
6849646Chromenone and chromanone derivatives as integrin inhibitors
The invention relates to compounds having formula (I), wherein R1, R2, R3, R4, R5, R7, R8, R11, Z, m and n have the meaning cited in... 		02/01/2005
6747051m-Amino-phenylimino-imidazolidine derivatives for treating urinary incontinence
A compound of Formula I or of Formula II wherein: R1 is F, Cl, Br, CH2F, CF2H, or CF3; R2 is NR6R7, where R6 is Me, Et... 		06/08/2004
66932002-(substituted-phenyl)amino-imidazoline derivatives
This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: ##STR1## where: R1 is a group represented by formula (A), (B) or (C); ##STR2## and other substituents as defined in the specifi... 		02/17/2004
6660732Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such c... 		12/09/2003
6656933Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such c... 		12/02/2003
6602897m-Amino-phenylimino-imidazolidine derivatives for treating urinary incontinence
A compound of formula I or of formula II ##STR1## wherein: R1 is F, Cl, Br, CH2 F, CF2 H, or CF3 ; R2 is NR6 R7, where R6 is Me, Et, Pr, or iPr, and R7 is Me, Et... 		08/05/2003
6596739N-(1-phenylethyl)-5-phenyl-imidazole-2-amine compounds, their compositions and uses
The subject invention involves compounds having structure (I): wherein each R1 is independently alkyl, aryl, or heterocycle; each R2, R4, R7, and R8 is independently hydrogen or other substituent; A is aryl or heterocycle; and pharmaceutically acceptable ... 		07/22/2003
65968762-(substituted-phenyl)amino-imidazoline derivatives
This invention relates to IP receptor antagonists selected from the group of compounds represented by Formula I: ##STR1## where: R1 is a group represented by formula (A), (B) or (C); ##STR2## and other substituents as defined in the specificat... 		07/22/2003
6569884Conformationally rigid bicyclic and adamantane derivatives useful as 댒-adrenergic blocking agents
A compound of formula I ##STR1## in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or ... 		05/27/2003
6492356Acylguanidine derivatives as inhibitors of bone resorption and as vitronectin receptor antagonists
The present invention relates to acylguanidine derivatives of formula (I) in which R1, R2, R4, R5, R6, A, m and n have the meanings indicated in the patent claims, their physiologically tolerable salt... 		12/10/2002
6472529Retroviral protease inhibiting compounds
A compound of the formula: ##STR1## is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.... 		10/29/2002
6448286Imino pyrrolidine derivatives useful as nitric oxide synthase inhibitors
The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.... 		09/10/2002
63957642-imidazolinylaminoindole compounds useful as alpha-2 adrenoceptor agnonists
This invention involves compounds having the following structure: ##STR1## wherein: a) R1 is hydrogen; or alkyl; bond (a) is a single or a double bond; b) R2 and R3 are each independently selected from hydrogen; unsubstituted C... 		05/28/2002
6391904Iminoguanidine derivatives, preparation method, use as medicines
A compound of the formula ##STR1## where the substituents are defined in the specification and its pharmaceutically acceptable salts and prodrugs thereof useful as antagonists of vitronectin receptors.... 		05/21/2002
6358945Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such c... 		03/19/2002
6348482Catechols as antimicrobial agents
Compounds, pharmaceutically acceptable salts, and compositions thereof of the general formula: ##STR1## wherein Ar is aryl and heteroaryl; R1, R2, R3, and R4 are hydrido, alkyl, cyano, heteroaryl, hydroxy, amino... 		02/19/2002
6319935Conformationally rigid bicyclic and adamantane derivatives useful as 댒-adrenergic blocking agents
A compound of formula I ##STR1## in which: ring A is one of the five alternative multi-cyclic rings as shown wherein a dotted line adjacent to a bond indicates that a single bond or a double bond may be present at that position; X is nitrogen, oxygen or ... 		11/20/2001
6268389Treatment of urinary incontinence by administration of 댑L-adrenoceptor agonists
The present invention relates to the use of ଱lL -agonists for treating urinary incontinence.... 		07/31/2001
6121303Pharmacologically active catechol derivatives
A compound of formula I ##STR1## wherein R1 is nitro, halogeno or cyano group and R2 is a group selected from ##STR2## wherein Y and Z are independently oxygen, sulfur or NR, wherein R is hydrogen, straight or branched... 		09/19/2000
6103749Aryl imidazole compounds having phosphodiesterase IV inhibitory activity
Novel compounds which are effective PDE IV inhibitors are disclosed. These compounds have the general structure of: ##STR1## where R1, R2, R3, R4, X1, X2 and Z are described herein. Th... 		08/15/2000
6093727Imidazole and imidazoline derivatives and uses thereof
This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human a, adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation... 		07/25/2000
6051718PDE IV inhibiting 2-cyanoiminoimidazole derivatives
The present invention concerns 2-cyanoiminoimidazole derivatives having the formula ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 and R2 ea... 		04/18/2000
6011045Vitronectin receptor antagonists, their preparation and their use
The present invention relates to compounds of the formula I A--B--D--E--F--G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds... 		01/04/2000
6007865Reversing the formation of advanced glycosylation endproducts
The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylatio... 		12/28/1999
5932606Pyrazinone, pyridinone, piperidine and pyrrolidine thrombin inhibitors
A compound which inhibits human thrombin and where has the structure and pharmaceutically acceptable salts thereof, wherein such as ##STR1## which are useful for inhibiting formation of blood platelet aggregates in blood in a mammal.... 		08/03/1999
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