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Class 544/291 - Nitrogen bonded directly at 2- and 4-positions


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogens are bonded directly at the 2-
No. of patents: 140
Last issue date: 01/10/2012


1        
NumberTitleIssue Date
8093384Processes for the preparation of alfuzosin
The invention relates to processes for the preparation of alfuzosin or pharmaceutically acceptable salts thereof in high purity. More particularly, it relates to the preparation of pure crystalline alfuzosin base. The invention also relates to pharmaceutical composi...
01/10/2012
7262200Indazolinone compositions useful as kinase inhibitors
The present invention provides compounds of formula I: These compounds, and pharmaceutically acceptable compositions thereof, are useful generally as kinase inhibitors, particularly as inhibitors of PRAK, GSK3, ERK...
08/28/2007
7238698Substituted quinazoline compounds useful as p38 kinase inhibitors
Compounds having the formula (I), are useful as p38 kinase inhibitors, wherein R4 and R5 are hydrogen, halogen, cyano, haloalkyl, or haloalkoxy, but are not both hydrogen; R6 and ...
07/03/2007
7211697Method for producing specific crystalline modifications of polmorphous substances
The present invention pertains to a process for the production of a specific crystal modification of a polymorphic, organic substance by precipitation of the specific crystal modification from the aqueous solution of the salt of the polymorphic substances using ordi...
05/01/2007
7205309Quinazoline derivatives
Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1, R2, R3 and A have the significance given in the specification are provided. The...
04/17/2007
7176312Kinase inhibitor scaffolds and methods for their preparation
General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, bor...
02/13/2007
7060825Process for synthesizing 6-quinazolinyl-ethyl-benzoyl and related antifolates
The invention claimed herein relates to an improvement in a process for synthesizing a compound of formula Ib: wherein R1 and R2 are each individually amino or N-alkyl substituted amino; hydroxy; alkoxy; keto;...
06/13/2006
6930113Nitrosated and nitrosylated phosphodiesterase inhibitors, compositions and methods of use
The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer...
08/16/2005
6911446Methods of modulating serine/threonine protein kinase function with quinazoline-based compounds
The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with quinazoline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In addition, the inv...
06/28/2005
6806274Quinazoline derivatives
The invention concerns quinazoline derivatives of Formula (I) wherein Q1 includes a quinazoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X
10/19/2004
6800644Nitrogen-containing heterocyclic compounds and medicaments containing the compounds
The present invention provides a novel nitrogen-containing heterocyclic compound useful as a phosphodiesterase-4 inhibitor, and a medicament comprising the same. Further, the present invention provides a nitrogen-containing heterocyclic compound represented by the f...
10/05/2004
6794389Quinazoline derivatives and drugs
There is provided an excellent novel analgesic having an analgesic effect which is effective widely against a pain including a chronic pain or an allodynia accompanied with herpes zoster by acting on a nociceptin receptor. The present invention relates to a c...
09/21/2004
6733982Method for screening compounds for alpha1B adrenergic receptor antagonist and analgesic activity
A method for identifying compounds that can be useful for producing analgesia is disclosed. In particular, the method involves providing preparation of a cell, that expresses an alpha1B adrenergic receptor, combining a test compound with the cell preparat...
05/11/2004
6706705Quinazoline derivatives
The present invention provides a new compound which shows slow and continuous blood pressure reducing action and is useful as an antihypertensive agent. The invention resides in a quinazoline derivative of the following formula (I) and its pharmaceutically ac...
03/16/2004
6677339Phenylalanine derivatives
Phenylalanine derivatives of formula (1) are described: ##STR1## in which: Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; Ar2 is an optionall...
01/13/2004
6649620Quinoline and quinazoline compounds useful in therapy
Compounds of formula I, ##STR1## wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents an aryl group or a heteroaryl group, optionally substituted by C1-4 ...
11/18/2003
6642242Quinoline and quinazoline compounds useful in therapy
The invention provides compounds of formula (I), ##STR1## wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or m...
11/04/2003
6608200Process for the preparation of N-(2,3-Dihydrobenzo[1,4]dioxin-2-carbonyl)piperazine
Described herein is an improved process for the preparation of N-(2,3-Dihydrobenzo[1,4]dioxin-2-carbonyl)piperazine which includes heating a reaction mixture ethyl of 2,3-dihydrobenzo[1,4]dioxin-2-carboxylate and piperazine. The reaction mixture is t...
08/19/2003
6608055Crystalline anticholinergic, processes for preparing it and its use for preparing a pharmaceutical composition
The invention relates to crystalline anhydrous (1଱,2ଲ,4ଲ,5଱,7ଲ)-7-[(hydroxydi-2-thienylacetyl) oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.022,4 ]nonane-bromide, processes for preparing it and its use for prepari...
08/19/2003
6559153Quinazoline derivatives as alpha-1 adrenergic antagonists
This invention relates to compounds which are generally alpha-1B adrenergic receptor antagonists and which are represented by Formula (I): ##STR1## wherein R', R", R1, R2, m, n, and A are as defined in the specification, or acceptabl...
05/06/2003
6545003Fused ring heteroaryl and heterocyclic 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....
04/08/2003
6525195Method for obtaining polymorph a from doxazosine mesylate
The invention discloses a process for the preparation of the polymorh A of doxazosin meylate, consisting essentially of reacting doxazosin base with methanesulfonic acid in a mixture of solvents containing an alcohol and a chlorinated solvent, subsequentl...
02/25/2003
6500830Conversion of modification D to modification A of doxazosin mesylate
A process for preparing doxazosin mesylate in modification A which comprises dissolving doxazosin with methanesulfonic acid in methanol or a mixture of an aprotic, polar organic solvent and methanol, removing any turbidity from the resulting solution, and...
12/31/2002
6476033Medicaments containing doxazosin mesylate of crystalline modification D
Drugs comprising modification D of doxazosin mesylate are described. They are suitable for treating high blood pressure....
11/05/2002
6458798Bicyclic pyrimidine compounds and therapeutic use thereof
A pyrimidine derivative of the formula (1) or a salt thereof; ##STR1## has an inhibitory activity of production of Th2 type cytokines such as IL-4, IL-5, etc., and is useful as an therapeutic agent for allergic diseases, autoimmune diseases such as system...
10/01/2002
6417194Quinolines and quinazolines useful in therapy
Compounds of formula I, ##STR1## wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 and R3 independently represent H or C1-6 alkoxy (which is optionally substit...
07/09/2002
6399775Methods for the preparation of polymorphs of doxazosin mesylate
Form D of doxazosin mesylate and a process for preparing Form D of doxazosin mesylate is described. The process is (a) dissolving doxazosin base and methane sulfonic acid in an alcohol having 1 to 8 carbon atoms; (b) precipitating Form D of doxazosin mesy...
06/04/2002
6352989Nitrogenous heterocyclic derivatives and medicine thereof
The present invention provides a novel nitrogen-containing heterocyclic compound useful as a phosphodiesterase-4 inhibitor, and a medicament comprising the same. Further, the present invention provides a nitrogen-containing heterocyclic compound represent...
03/05/2002
6348463Phenylalanine derivatives
Phenylalanine derivatives of formula (1) are described: ##STR1## in which: Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; Ar2 is an optionally substituted ar...
02/19/2002
6339089Pyrimidine nucleus-containing compound and a medicament containing the same for a blood oxygen partial pressure amelioration, and a method for preparing the same
A pyrimidine nucleus-containing compound represented by the formula (I): ##STR1## wherein ring A represents the ring of the formula (a): ##STR2## in which R1 is a nitro group, an amino group, a substituted amino group or a halogen atom, or the ...
01/15/2002
6313294Process for preparing amides
The present invention provides a process for preparing an amide, which comprises reacting an amine with an ester in a molten form in the absence of a solvent....
11/06/2001
6258952Thermally stable trimetrexates and processes for producing the same
The present invention provides for thermally stable forms of 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline, or trimetrexate. A crystalline 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline monohydrate, or tri...
07/10/2001
6258821Compositions comprising trimetrexate and methods of their synthesis and use
This invention is directed to the novel composition of matter trimetrexate ascorbate, to compositions comprising trimetrexate ascorbate, and to compositions comprising trimetrexate and ascorbic acid. These compositions are useful in the treatment of disea...
07/10/2001
6248888Process for the preparation of terazosin hydrochloride dihydrate
A process for the preparation of 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-tetrahydrofuroyl)piperazine hydrochloride dihydrate, and the product produced thereby, comprising reacting by heating 2-chloro-4-amino-6,7-dimethoxyquinazoline and 1-(2-te...
06/19/2001
6204267Methods of modulating serine/thereonine protein kinase function with quinazoline-based compounds
The present invention is directed in part towards methods of modulating the function of serine/threonine protein kinases with quinazoline-based compounds. The methods incorporate cells that express a serine/threonine protein kinase, such as RAF. In additi...
03/20/2001
6140334Polymorphic form of doxazosin mesylate (form III)
A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of high and medium intensity: 8.49°, 11.72°, 16.03°, 18.29°...
10/31/2000
6133269Polymorphic form of doxazosin mesylate (form II)
A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of high and medium intensity: 10.68°, 14.45°, 17.37°, 23.45Â...
10/17/2000
6130218Polymorphic form of doxazosin mesylate (Form I)
A new crystalline and anhydrous form of doxazosin mesylate is described. The new form is crystalline and anhydrous and is characterized in its X-ray spectrum by the following reflex positions of high and medium intensity: 15.40°, 16.85°, 18.06°, 24.15Â...
10/10/2000
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
6048864Quinolines and quinazolines useful in therapy
Compounds of formula I, ##STR1## wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 and R3 independently represent H or C1-6 alkoxy (which is optionally su...
04/11/2000
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