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Class 514/266.21 - The additional hetero ring is six-membered consisting of one nitrogen and five carbons


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the additional hetero ring is
No. of patents: 251
Last issue date: 08/02/2011


1              
NumberTitleIssue Date
79894624-arylamin-or-4-heteroarylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof
Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnor...
08/02/2011
77722434-phenylamino-quinazolin-6-yl-amides
This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH
08/10/2010
7700607Substituted pyridone compounds and methods of use
The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The...
04/20/2010
76918662,6-disubstituted quinazolines, quinoxalines, quinolines and isoquinolines and methods of their use as inhibitors of Raf kinase
New substituted quinazoline, quinoxaline, quinoline and isoquinoline compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at...
04/06/2010
7605165Phenylalanine derivatives
The present invention relates to the following phenylalanine derivatives or analogues thereof having an antagonistic activity to α4 integrin and therapeutic agents for various diseases concerning α4 integrin. ...
10/20/2009
7491728Pyrimidinone compounds as calcilytics
The pyrimidinone compounds are disclosed. Methods of preparing the pyrimidinone compounds are also disclosed. ...
02/17/2009
7462623Quinazoline derivatives as Src tyrosine kinase inhibitors
The invention concerns quinazoline derivatives of Formula (I): (A chemical formula should be inserted here—please see paper copy enclosed herewith) wherein Z is an O, S, SO, SO2, N(R2) or C(R2)2 group wherein each R...
12/09/2008
7456188C-5 substituted quinazolinone derivatives as selective estrogen receptor beta modulators
The present application describes compounds according to Formula I, wherein Q, R1, R2 and X are described herein, that are useful as Estrogen Receptor Beta (ERβ) modulators. Additionally, the present application describes pharmaceutical compos...
11/25/2008
7390815Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula II: wherein Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, and R2, R2′, R...
06/24/2008
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
73817303-arylquinazoline derivatives as selective estrogen receptor beta modulators
Novel quinazoline derivatives possessing activity as estrogen receptor beta (ERβ) modulators are provided which have the general formula I wherein X is O or S; A and B ar...
06/03/2008
7368445Fused pyrazole derivatives as TGF-β signal transduction inhibitors for the treatment of fibrosis and neoplasms
The disclosed invention is directed to compounds of the formula: Formula (I) and methods of using these compounds. ...
05/06/2008
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
7332493Substituted bicyclic derivatives for the treatment of abnormal cell growth
The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R3, R4, R5, R11, m a...
02/19/2008
7329664Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol analogues
Substituted (7-pyridyl-4-phenylamino-quinazolin-2-yl)-methanol 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 ...
02/12/2008
7312209Acridone inhibitors of IMPDH enzyme
Compounds having the formula (I), wherein R3 is selected from H, OH and NH2; R30 is selected from ═O and ═S; W is —C(═O)—, —S(═O)—, or —S(O)2—; or W...
12/25/2007
7304059Substituted quinazolin-4-ylamine analogues
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 activati...
12/04/2007
7268142Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline
The invention pertains to substituted quinazoline and isoquinoline compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE-10. The invention also relates to in...
09/11/2007
7268230Quinazoline compounds
The invention relates to compounds of the formula (I): wherein ring C is as defined herein, for example indolyl, indazolyl or azaindolyl; Z is —O—, —NH— or —S—; n is 0-5; m is 0-3; R1 and R2 are defined herein including groups: (i) ...
09/11/2007
7265125Neuropeptide Y antagonists
Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity. ...
09/04/2007
7232903Process for producing quinazolin-4-one and derivatives thereof
A process for preparing quinazolin-4-one or its derivative by reacting anthranilic acid or its derivative with formic acid or its derivative in the presence of ammonia, or by reacting ammonium anthranilate or its derivative with formic acid or its derivative. ...
06/19/2007
7230000Methods and compositions utilizing quinazolinones
Quinazolinones of formulae 1a, 1b, 1c and 1d are disclosed. They are useful for treating cellular proliferative diseases and disorders associated with KSP kinesin activity ...
06/12/2007
7214518Crystal structure of aurora a kinase and uses thereof
The invention provides crystalline forms of a polypeptide corresponding to the catalytic domain of Aurora kinase. The active site ATP binding pocket is defined by its amino acid residues and their atomic coordinates. This structure may be used to select or design ch...
05/08/2007
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
7196094Farnesyl transferase inhibiting 6-heterocyclylmethyl quinoline and quinazoline derivatives
This invention comprises the novel compounds of formula (I) wherein r, t, Y1—Y2, R1, R2, R3, R4, R5, R6 and R7 ...
03/27/2007
7186720Tetrahydropyridyl-alkyl-heterocycles, method for preparing the same and pharmaceutical compositions containing the same
The present invention relates to compounds of formula (I): in which X represents N or CH; R1 represents a hydrogen or halogen atom or a CF3 group; R2 and R3 independent...
03/06/2007
7173040Farnesyl transferase inhibiting 6-[(substituted phenyl)methyl]-quinoline and quinazoline derinazoline derivatives
This invention comprises the compounds of formula (I): wherein r, s, t, Y1–Y2, R1, R2, R3, R4, R5, R6 and R7 ha...
02/06/2007
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
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
7125995Substituted amidoalkyl uracils and their use as inhibitors of the poly(adp-ribose) synthetase (PARS)
This application relates to compounds of formula (I) below in which the several variable groups are as defined in the specification and claims, to methods of preparing these materials, to pharmaceutical compositi...
10/24/2006
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
7091200Quinazolone derivatives as alpha 1A/B adrenergic receptor antagonists
This invention relates to compounds which are generally alpha-1A/B adrenoceptor antagonists and which are represented by Formula I: wherein Z is —C(O)— or —S(O)2—, X is...
08/15/2006
7074800Quinazoline derivatives as angiogenesis inhibitors
The invention relates to the use of compounds of formula (I), wherein ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which optionally may contain 1–3 heteroatoms selected independently from O, N and S; Z is —O—, —NH—, —S—, —CH
07/11/2006
7074801Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof
The present invention discloses compounds and compositions of formula (I): having inhibitory activity on activation of STAT6, wherein X represents quinoline, isoquinoline, quinazoline or imidazopyridine; Y repres...
07/11/2006
7053216Modulators of Rho C activity
Compounds of formula 1 modulate the activity of Rho C: wherein R1 is H, lower alkyl, aralkyl, aryl-lower alkenyl, or —(CH2)nCH(R7)NR8
05/30/2006
7049438Quinazoline derivatives for 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...
05/23/2006
7022856Carboline derivatives
Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents. ...
04/04/2006
6992084Compounds and methods for modulating CXCR3 function
The invention provides compounds and compositions of the formula: wherein, the subscript n is an integer of from 0 to 4; Ar is a member selected from the group consist...
01/31/2006
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
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