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Class 544/293 - Nitrogen bonded directly at 4-position


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein nitrogen is bonded directly at the 4-position
No. of patents: 228
Last issue date: 05/29/2012


1            
NumberTitleIssue Date
8188274Process for preparing aminocrotonylamino-substituted quinazoline derivatives
The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups Ra, Rb, Rc and Rd have ...
05/29/2012
8067593Process for preparing aminocrotonylamino-substituted quinazoline derivatives
The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups Ra, Rb, Rc and Rd have ...
11/29/2011
7960545Process for the prepartion of erlotinib
The present invention discloses an improved and novel process for the preparation of erlotinib (N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine) of formula (1), which comprises: (i) demethylation of commercially available 6,7-dimethoxy-4(3H)-quinazoli...
06/14/2011
7960546Process for preparing aminocrotonylamino-substituted quinazoline derivatives
The invention relates to an improved process for preparing aminocrotonylamino-substituted quinazoline derivatives of general formula (I) wherein the groups Ra, Rb, Rc and Rd have the meanings given in the claims, as well a...
06/14/2011
7547781Quinazoline based EGFR inhibitors containing a zinc binding moiety
The present invention relates to quinazoline containing zinc-binding moiety based derivatives that have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related d...
06/16/2009
7432275Carboxylic acid, phosphate or phosphonate substituted quinazolin-4-ylamine analogues as capsaicin receptor modulators
Acid-substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor act...
10/07/2008
7429597Substituted nitrogen-containing heterobicycles, the preparation thereof and their use as pharmaceutical compositions
The present invention relates to new substituted nitrogen-containing heterobicyclic compounds of general formula wherein B, X1 to X3 and R1 to R5 are defined as in claim 1,...
09/30/2008
7417055Kinase inhibitory phosphonate analogs
The invention is related to phosphorus substituted kinase inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such com...
08/26/2008
7410975Small molecule toll-like receptor (TLR) antagonists
The invention provides methods and compositions useful for modulating signaling through Toll-like receptors. The methods involve contacting a TLR-expressing cell with a small molecule having a core structure including at least two rings. Certain of the compounds are...
08/12/2008
7410974Halogenated Quinazolinyl nitrofurans as antibacterial agents
The present invention includes novel compounds of the formula (I) wherein X is absent or trans or cis CHCH, R1 is (C1-C10) alkyl unsubstituted or substituted by one to three hydroxy, (C1-C10) alkenyl unsubstitut...
08/12/2008
7388014Quinazoline derivatives and therapeutic use thereof
Quinazoline derivatives represented by the general formula pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for using the compounds for treatment of hyperprolifer...
06/17/2008
7368454(3,4-dihydro-quinazolin-2-yl)-aryl-amines
The present invention relates to methods for treating 5-HT5A receptor related diseases which comprises administering compounds of formula I wherein R1, R2,...
05/06/2008
7361663N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa
This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions cont...
04/22/2008
7358256ATP competitive kinase inhibitors
The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 th...
04/15/2008
7348332(3,4-dihydro-quinazolin-2-yl)-indan-1-yl-amines
The present invention relates to compounds of formula wherein R1, R2, and n are as defined herein and to pharmaceutically acceptable acid addition salts thereof.
03/25/2008
7326712Substituted tricyclic compounds as protein kinase inhibitors
Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including ...
02/05/2008
7317019N-alkylated diaminopropane derivatives as modulators of chemokine receptor activity
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid a...
01/08/2008
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
7262201Quinazoline derivatives
The invention relates to the use of compounds of the formula I: wherein: ring C is a 5-6 membered heterocyclic moiety; Z is —O—, —S—, or —CH2—; R1 is hydrogen, C1-4alk...
08/28/2007
7232824Quinazoline derivatives as medicaments
Quinazoline derivatives have the formula: or the pharmaceutically acceptable salts thereof; wherein each of Z5, Z6, Z7 and Z8 ...
06/19/2007
7223767Tetrahydroquinazolines and dihydrocyclopentapyrimidines as CRF antagonists
Compounds of the formula (I): and pharmaceutically acceptable salts or prodrugs thereof, wherein m, R1, R2, R3, R4, R5 and R6 are as defined herei...
05/29/2007
7220750Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rc, A to E and X are defined as in claim 1, the tautomers, stereoisomers and salts thereof, pa...
05/22/2007
7202253Cycloalkyl inhibitors of potassium channel function
Novel cycloalkyl compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating...
04/10/2007
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
7173038Quinazoline derivatives as VEGF inhibitors
The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C
02/06/2007
7160891Quinazoline derivatives for the treatment of T cell mediated diseases
The invention concerns the use of the quinazoline derivatives of Formula (I) wherein each of Q1, Z, m, R1, R2, R3 and Q2 have any of the meanings defined in the description in the manufacture of a medicament for...
01/09/2007
7157466Quinazoline ditosylate salt compounds
Ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorde4rs characterized by aberrant erbB family PTK activity. ...
01/02/2007
7157467Therapeutic use
The invention concerns the use of the quinazoline derivatives of Formula (I) Wherein each of m, R1, n, R2 and R3 have any of the meanings defined in the description in the manufacture of a medicament for use in the prevention or trea...
01/02/2007
7148231[6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride polymorph
The invention is concerned with a novel polymorph of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride. This polymorph exhibits superior properties compared to the previously known forms of [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-...
12/12/2006
7148230Quinazoline derivatives
The invention concerns quinazoline derivatives of Formula I wherein R1 and R2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical composition...
12/12/2006
7141564Nitrogen-containing bicyclic heterocycles for use as antibacterials
Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man. ...
11/28/2006
7132427Quinazolines and uses thereof
This invention relates to compounds of the general formula: in which RA, RB, RC and RD are as defined herein, and to their preparation and use. ...
11/07/2006
7115615Quinazoline derivatives
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 preparat...
10/03/2006
7109333Heterocyclic compounds
A process for the preparation of a compound of formula (I) comprising the steps: (a) reacting a compound of formula (II) ...
09/19/2006
7105669Quinazoline derivatives
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 NR10 where R10 is hydrogen or C1-6 alkyl, and R1, R2, R3, R4, R5, R
09/12/2006
7084147Anilinoquinazaolines as protein tyrosine kinase inhibitors
Heteroaromatic compounds are described, methods for their preparation, pharmaceutical compositions containing them, methods of use, and their use in medicines. In particular, the invention relates to quinazoline and pyridopyrimidine derivatives which exhibit protein...
08/01/2006
7081461Quinazoline compounds and pharmaceutical compositions containing them
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, NH or NR8 where R8 is hydrogen or C1-6alkyl;
07/25/2006
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
7045526Substituted 4-amino-2-aryl-tetrahydroquinazolines, their preparation, their use and pharmaceutical preparations comprising them
The present invention relates to compounds of formula I: wherein R1, R2, and R3 have the meanings indicated in the specification, which are valuable pharmaceutical active compound...
05/16/2006
7038049Haloanilino quinazolines and therapeutic use thereof
The present disclosure includes compounds, for example a compound according to formula I or a pharmaceutically acceptable salt thereof. The compounds of the present disclosure are useful in methods of treating cancerous...
05/02/2006
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