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Class 544/119 - Acyclic nitrogen containing


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which include acyclic nitrogen.
No. of patents: 143
Last issue date: 08/30/2011


1        
NumberTitleIssue Date
8008481Indazole compounds
Novel compounds of Formula (I) or pharmaceutically acceptable salts, prodrugs and biologically active metabolites thereof of Formula (I) wherein the substituents are as defined herein, which are useful as therapeutic agents...
08/30/2011
7910731Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them
The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the gastrointestinal tract, the bile duct and the gall bladder by administration to ...
03/22/2011
7598377Inhibition of phosphoinositide 3-kinase β
The present invention relates to selective inhibitors of phosphoinositide (PI) 3-kinase β, use of the selective inhibitors in anti-thrombotic therapy, and a method for screening compounds useful for the new anti-thrombotic therapy by detecting selective inhibitory ...
10/06/2009
7405295Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
Compounds of Formula I-a and all pharmaceutically-acceptable forms thereof, are described herein. The variables R1, R2, R3, Z1, Q, and A shown in Formula I-a are defined h...
07/29/2008
7304051Quinoxaline compounds
Amidophenyl-sulfonylamino-quinoxaline compounds of formula (I) are CCK2 modulators useful in the treatment of CCK2 mediated diseases. ...
12/04/2007
7294629Quinazoline derivatives
A compound of the formula (I) or a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, an optically active compound thereof, a racemate thereof or a diastereomer mixture thereof has a ...
11/13/2007
72712603,4-dihydroquinazoline derivatives as T-type calcium channel blockers and method of preparing the same
The present invention relates to 3,4-dihydroquinazoline derivatives as T-type calcium channel blockers and a method of preparing the same. The present invention further relates to a composition comprising the same. The composition comprising the 3,4-dihydroquinazoli...
09/18/2007
7186710Phthalazinones
The compounds of formula I in which R1, R2, R3, R4 and R5 have the meanings as given in the description are PDE4/7 inhibitors. ...
03/06/2007
7183281Sulfonylquinoxalone derivatives and related compounds as bradykinin antagonists
Disclosed are sulfonylquinoxalone derivatives of the general formula: These compounds are useful as bradykinin antagonists. ...
02/27/2007
70947803-aminoquinazolin-2,4-dione antibacterial agents
Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: R1 and R3 include alkyl, alkenyl, cycloalkyl, aryl, hetero-cyclic, and heteroaryl; R5, R6, and R8 include H, alkyl, alkoxy, halo, NO2
08/22/2006
7071182Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in repro...
07/04/2006
7049307Antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor
The present invention relates to the antagonism of the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in repro...
05/23/2006
7001904Guanidine derivatives quinazoline and quinoline for use in the treatment of autoimmune diseases
The invention concerns quinazoline and quinoline derivatives of Formula (I) wherein Q1 includes a quinazoline or quinoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X
02/21/2006
6982260Quinazolines and their use for inhibiting cyclin-dependent kinase enzymes
This invention provides quinazolines that are useful for treating cell proliferative diseases and disorders, such as cardiovascular diseases, infections, cancers, autoimmune diseases, gout, kidney disease, and neurodegenerative diseases and disorders such as Alzheim...
01/03/2006
6977141Direct adsorption scintillation assay for measuring enzyme activity and assaying biochemical processes
Methods and materials for scintillation assays are disclosed. The scintillation assays rely on differences in general molecular property-based binding interactions, such as charge or hydrophobicity, to localize a radioactive substance near a scintillating material, ...
12/20/2005
69722884-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transduction mediated by tyrosine kinases
The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rd, A to G and X are defined as in claim 1, the tautomers, the steroisome...
12/06/2005
6924285Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them
The present invention relates to bicyclic heterocyclic groups of general formula wherein Ra, Rb, Rc, Rd and X are defined as in claim 1, the tautomers, the stereois...
08/02/2005
6919338Substituted quinazoline derivatives and their use as inhibitors of aurora-2 kinase
The use of a compound of formula (I) or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6alkyl; R
07/19/2005
6897213Heterocycles as cholecystokinin (CCK) ligands
Novel quinazolinone derivatives with good binding affinity for the CCK-A and CCK-B receptors, pharmaceutical compositions containing them and methods of using them are taught. The compounds are useful agents to suppress appetite, reduce gastric acid secretion, and t...
05/24/2005
6897214Quinazoline derivatives
The invention concerns quinazoline derivatives of the formula I wherein X1 is a direct link or a group such as CO, C(R2)2 and CH(OR2);
05/24/2005
6864259Antibacterial agents
The present invention provides compounds of Formula (I): wherein R1-R6 and K have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful as a...
03/08/2005
6849625Quinazoline derivatives with anti-tumour activity
The invention concerns quinazoline derivatives of Formula I wherein each of m, R1, n, R2 and R3 have any of the meanings defined in the description; processes for their preparation, pha...
02/01/2005
6797823Quinoline derivatives and quinazoline derivatives
An object of the present invention is to provide compounds which have antitumor activity and do not change cytomorphosis. Disclosed are compounds represented by formula (I) and a pharmaceutically acceptable salts and solvates thereof and pharmaceutical compositions ...
09/28/2004
6740651Aminoquinazolines which inhibit signal transduction mediated by tyrosine kinases
Compounds of the formula having an inhibitory effect on signal transduction mediated by tyrosine kinases, and the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tr...
05/25/2004
67306686,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines
The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula:
05/04/2004
6699861Anti-quinazoline compounds
Dihydroquinazoline derivatives of the formula ##STR1## where R3 is --(CH2)p --A where p is from 1 to 4 and A is a 5- or 6-membered N-containing heterocyclic ring attached via the N atom or A is --NA'A" wherein A' and A" ar...
03/02/2004
66773332H-phthalazin-1-one derivatives and drug containing its derivatives as active ingredient
Poly(ADP-ribose)polymerase inhibitors containing as the active ingredient 2H-phthalazin-1-one derivatives represented by general formula (I) (wherein each symbol is as defined in the description) or salts thereof. The compounds of the general formula (I) ...
01/13/2004
6664390METHOD FOR THE SIMPLIFIED PRODUCTION OF (3-CHLORO-4-FLUOROPHENYL)-[7-(3-MORPHOLIN-4-YL-PROPOXY)-6-NITRO-QUINAZOLIN E-4-YL]-AMINE OR (3-CHLORO-4-FLUOROPHENYL)-[7-(3-MORPHOLIN-4-YL-PROPOXY)-6-AMINO-QUINAZOLIN E-4-YL]-AMINE
The invention concerns a one-pot reaction for the preparation of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitroquinazolin- 4-yl]-amine (I) ##STR1## or of (3-chloro-4-fluorophenyl)-[7-(3-morpholino-4-yl-propoxy)-6-aminoquinazolin -...
12/16/2003
66328136-subtituted-7-heteroquinoxalinecarboxylic acid derivatives and addition salts thereof and processes for the preparation of both
The invention provides compounds with antagonism against excitatory amino acid receptors, in particular, AMPA receptor having 6-substituted-7-heteroquinoxalinecarboxylic acid derivatives and addition salts thereof as effective ingredients, and processes f...
10/14/2003
66241604-oxo-1,4-dihydro-3-cinnolinecarboxamides as antiviral agents
This invention provides compounds of formula I; ##STR1## which are useful as antiviral agents....
09/23/2003
6617329Aminoquinazolines and their use as medicaments
Compounds of the formula ##STR1## having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and air-ways, and the preparation thereof...
09/09/2003
6528508Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention relates to compounds having the formula: ##STR1## or pharmaceutically accep...
03/04/2003
6525048Azabicyclic 5HT1 receptor ligands
The present invention relates to compounds of the formula ##STR1## These compounds are useful as psychotherapeutic agents....
02/25/2003
6525052Compounds useful as reversible inhibitors of cysteine proteases
Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The co...
02/25/2003
6514971Cinnoline derivatives and use as medicine
The invention relates to the use of cinnoline derivatives of formula (I) ##STR1## wherein Z represents --O--, --NH--, --S-- or --CH2 --; m is a n integer from 1 to 5; R1 represents hydrogen, hydroxy, halogeno, nitro, cyano, trifluoro...
02/04/2003
6492360Phthalazine derivatives phosphodiesterase 4 inhibitors
Compounds of formula (I), ##STR1## wherein {character pullout} is a single or double bond; Z is NH, methylene, a (C2 -C6)alkylene chain optionally branched and/or unsaturated and/or interrupted by a (C5 -C7)cycl...
12/10/2002
6472389Pyrrolo[1,2-b] pyridazine derivatives having sPLA2 inhibitory effect
The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): ##STR1## wherein R1 is --(L1)--R6 wherein L1 is a divalent linking group of 1 t...
10/29/2002
6403580Quinazolines, pharmaceutical compositions containing these compounds, their use and processes for preparing them
Quinazolines of the formula ##STR1## having an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract, and the preparation ...
06/11/2002
6399603Therapeutic heterocycles
A compound having the general formula ##STR1## and methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds....
06/04/2002
6399602Quinazoline derivatives
The invention concerns quinazoline derivatives of the formula I ##STR1## wherein X1 is a direct link or a group such as CO, C(R2)2 and CH(OR2); wherein Q1 is phenyl, naphthyl or a 5- or 6-membered heteroar...
06/04/2002
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