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Class 514/266.1 - Quinazoline (including hydrogenated)(i.e., the second cyclo in the bicyclo ring system is an ortho-fused six-membered carbocycle)


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the bicyclo ring system is the
No. of patents: 143
Last issue date: 05/01/2012


1        
NumberTitleIssue Date
8168644Quinazolinone derivatives as tubulin polymerization inhibitors
The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2...
05/01/2012
8158637Quinazolines useful as modulators of voltage gated ion channels
The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of...
04/17/2012
8067427Pharmaceutical compositions comprising ZD6474
A pharmaceutical composition comprising ZD6474 or a pharmaceutically acceptable salt thereof, a brittle diluent and a second diluent which is practically insoluble and has ductile compression properties. ...
11/29/2011
8053440Compounds for the prevention and treatment of cardiovascular diseases
The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disor...
11/08/2011
8034822Glucokinase activators
Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compoun...
10/11/2011
8003658Quinazoline derivatives for inhibiting cancer cell growth and method for the preparation thereof
The present invention relates to a novel quinazoline derivative and a pharmaceutically acceptable salt thereof for inhibiting the growth of cancer cells, a method for the preparation thereof and a pharmaceutical composition comprising same as an active ingredient.
08/23/2011
7989460Quinazoline derivatives as angiogenesis inhibitors
The present invention relates to compounds of the formula I: wherein: ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which moiety may be saturated or unsaturated, which may be aromatic or non-aromatic...
08/02/2011
7977346Spiro compounds and methods of use
The present invention relates to spiro compounds of formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states such as cancers associated with protein tyrosine kinases, es...
07/12/2011
7968558Amidine derivatives of 2-heteroaryl-quinazolines and quinolines; potent analgesics and anti-inflammatory agents
The present invention concerns novel amidines derivatives of 2-heteroaryl-quinazoline and quinolines of general formula (I), to a process for their preparation, to their pharmaceutical compositions and to the use of these compounds, salts and solvates thereof, along...
06/28/2011
7960399Quinazolinone derivatives useful as vanilloid antagonists
The present invention relates to the use of a quinazolinone compound of the formula (I) wherein R1, R2, R3, R4, R5 and m are as defined in the specification and in the claims, in free form or in salt form, and, ...
06/14/2011
7960398Regulation of TNF-alpha
The present invention relates to methods for identifying compounds useful for regulating TNF-alpha levels and/or activity. The invention also relates to methods for decreasing TNF-alpha levels and/or activity. Compounds and compositions according to this invention a...
06/14/2011
7932260Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta
The invention provides a class of substituted quinazolinone compounds and methods of treating diseases mediated by PI3Kδ activity. The disclosed compounds are useful in treating diseases such as bone-resorption disorders; and cancer, especially hematopoietic cancer...
04/26/2011
7928113Integrin-binding small molecules
The present invention relates to compositions containing integrin-binding small molecules. Also disclosed are methods of binding integrins to these small molecules and methods of identifying small molecules binding to integrins. ...
04/19/2011
7713983Quinazolines useful as modulators of ion channels
The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the composition...
05/11/2010
7709491Substituted quinazolines as antiviral agents, especially against cytomegaloviruses
The invention relates to substituted quinazolines and to methods for the production thereof, in addition to the use thereof in the production of medicaments for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, especially against ...
05/04/2010
7696214Quinazoline derivatives for the treatment of tumours
The invention concerns 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; processes for their preparation, pharmaceutical comp...
04/13/2010
RE41065Alkynl and azido-substituted 4-anilinoquinazolines
The invention relates to compounds of the formula and to pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, n and m are as defined herein. The compounds of formula I are...
12/29/2009
7632840Quinazoline compounds for the treatment of hyperproliferative disorders
A quinazoline derivative of the formula I: wherein: R1, R2, R3, R3a, R4, R5, R5a R6, R7, a, m and p are as defined in the de...
12/15/2009
7618977Method of treating dermatitis comprising administering a chymase inhibitor
Medicaments for the treatment of dermatitis exhibiting a biphasic inflammation reaction or dermatitis induced by repeated exposure to an antigen, having quinazolidone derivatives of formula I or II that are herein defined, are disclosed. ...
11/17/2009
7544690MCH receptor antagonists
The present invention relates to novel compounds of the formula (I) which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of obesity, obesity related disorders, anxiety, or dep...
06/09/2009
7501427Quinazoline analogs as receptor tyrosine kinase inhibitors
This invention concerns quinazoline analogs of Formula I: where an A group is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to three independent R...
03/10/2009
RE40558Therapeutic uses of di-aryl acid derivatives
The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as P...
10/28/2008
7439248Pharmaceutical composition and the process for its preparation
The present invention provides a new stable pharmaceutical composition containing 5-[[4-[3-Methyl-4-oxo-3,4-dihydro-2-quinazolinyl]methoxy]phenyl-methyl]thiadiazolidine-2,4-dione as active ingredient. ...
10/21/2008
7427624Purine nucleoside phosphorylase inhibitory phosphonate compounds
The invention is related to phosphorus substituted purine nucleoside phosphorylase inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates usef...
09/23/2008
7417062Substituted arylamides
Substituted benzamide compounds are provided along with methods for the use of those compounds for treating cancer. ...
08/26/2008
73880193-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV en...
06/17/2008
7378409Substituted cycloalkylamine 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 arthritis.
05/27/2008
7365096Methods for selectively inhibiting Janus tyrosine kinase 3 (Jak3)
Methods are disclosed for inhibiting or disrupting Janus tyrosine kinase 3 (Jak3) dependent function in cells of lymphoid or myeloid origin, especially for blocking proliferation and function of lymphocytes (e.g., T-cells, B-cells). A Mannich base compound, or a der...
04/29/2008
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
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
7256197Methods for synthesis of diarylmethanes
The present invention relates to dihydrofolate reductase inhibitors having an aromatic group and a heteroaromatic group linked by a methylene group; methods of preparation of dihydrofolate reductase inhibitors that include metal mediated cross coupling of an aromati...
08/14/2007
7235559Therapeutic quinazoline derivatives
A compound of formula (I) or a salt, ester, amide or prodrug thereof; where X is O, or S, S(O), S(O)2 or NR6 where R6 is hydrogen of C1-6alkyl; R5 is an optionally substituted 6-membered aromatic ring containing...
06/26/2007
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
72328334-substituted quinoline derivatives, method and intermediates for their preparation and pharmaceutical compositions containing them
The invention relates to 4-substituted quinoline compounds of general formula: which are active as antimicrobials, in which: X1, X2, X3, X4 and X5
06/19/2007
7223760Substituted triazole compounds
Novel substituted triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...
05/29/2007
7220751Quinazoline derivatives and drugs
The invention provides an excellent novel analgesic which acts on a nociceptin receptor to exhibit a wide range of the analgesic effect for example on a chronic pain as well as an allodynia accompanied with a herpes zoster. The invention relates to a nocicept...
05/22/2007
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
7166595Compounds, methods and compositions
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed. ...
01/23/2007
7132418Peptidyl heterocyclic ketones useful as tryptase inhibitors
The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particul...
11/07/2006
7081460Quinazoline and quinazoline-like compounds for the treatment of integrin-mediated disorders
The invention is directed to novel quinazoline and quinazoline-like derivatives of Formula (I): useful as integrin antagonists and methods for the treatment of integrin-mediated disorders. ...
07/25/2006
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