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Class 514/266.23 - The additional hetero ring is five-membered consisting of carbon and plural nitrogens as the only ring members


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the additional hetero ring has
No. of patents: 178
Last issue date: 04/10/2012


1          
NumberTitleIssue Date
8153643Quinazoline derivatives
The invention concerns quinazoline derivatives of Formula (I) or a pharmaceutically-acceptable salt, solvate or pro-drug thereof, wherein each of X1, p, R1, q, R2, R3, R4, R5, Ring A, r and R6
04/10/2012
80805584-(tetrazol-5-yl)-quinazoline derivatives as anti-cancer agent
The invention relates to substituted 4-(tetrazol-5-yl)-quinazoline derivatives of the formula-I, or pharmaceutically-acceptable salts thereof, which possess anti-proliferative activity such as anti-cancer activity and are a...
12/20/2011
8053441Pyrazolylquinazolinones as potassium channel openers
The present invention is directed to novel pyrazolylquinazolinone derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel. ...
11/08/2011
7879867Crystalline antifungal compounds
Novel crystalline forms of (1R,2R)-7-chloro-3-[2-(2,4-difluorophenyl)-2 -hydroxy-1-methyl-3-(1H-1,2,4-triazol-1-yl)propyl]quinazolin-4(3H)-one, pharmaceutical compositions containing these crystalline forms, methods of using these crystalline forms for treating and/...
02/01/2011
7863282Compositions useful as inhibitors of protein kinases
A compound of formula Ia: or a pharmaceutically acceptable salt thereof. ...
01/04/2011
7718663Quinazoline derivatives and medicaments
An object of the present invention is to provide an antipruritic agent having a novel action mechanism. The present invention provides an antipruritic agent comprising a compound represented by the following general formula (1):
05/18/2010
7625910Co-crystal
The present invention relates to a novel co-crystal of 2-{ethyl[3-({4-[(5-{2-[(3-fluorophenyl)amino]-2-oxoethyl}-1H-pyrazol-3-yl)amino]quinazolin-7-yl}oxy)propyl]amino}ethyl dihydrogen phosphate (AZD1152) which is an aurora kinase inhibitor that is useful in the tre...
12/01/2009
7427681Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula II: wherein Z1 is nitrogen or CR8; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, whe...
09/23/2008
7402585Substituted quinazoline derivatives as inhibitors of aurora kinases
The invention provides quinazoline derivatives of formula (I): in the preparation of a medicament for use in the inhibition of Aurora kinase and also novel quinazoline derivatives, processes for their preparation, pharamceutical compositions containing them and thei...
07/22/2008
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
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
7294634Methods 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 ...
11/13/2007
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
7241767Quinazoline(di)ones for invertebrate pest control
Compounds of Formula I including all geometric and stereoisomers, N-oxides, and agriculturally suitable salts thereof, are disclosed which are useful as invertebrate pest control agents, (I) wherein A, B, J, K, L and R3 are as defined in the disclosure. A...
07/10/2007
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
7223756Quinazoline compounds with therapeutic use
The invention concerns the use of the quinazoline derivatives of Formula (I) wherein each of m, R1, Z, n and R3 have any of the meanings defined in the description in the manufacture of a medicament for use in the prevention or treatment of T c...
05/29/2007
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
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
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
7160874Phenylalanine derivatives
Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin. ...
01/09/2007
7160882Long acting β-2-agonists and their use as medicaments
The present invention relates to compounds of formula 1 wherein the groups X, Ra, Rb, R1, R1′, R2, R2′, R2″, R2′″,...
01/09/2007
7132432Hydantoin derivatives as inhibitors of tumor necrosis factor-alpha converting enzyme (TACE)
The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables L, Z0, R1, R4, R5, an...
11/07/2006
7115739Triazole compounds useful as protein kinase inhibitors
This invention describes novel triazole compounds of formula IX: wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2
10/03/2006
7112590Thrombin inhibitors
The invention relates to compounds that are heterocyclic derivatives of dipeptides and dipeptides mimetics and pharmaceutically acceptable salts thereof. The compounds are used as thrombin inhibitors ...
09/26/2006
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
7098330Pyrazolylamine substituted quinazoline compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula III: wherein Ring D is a 5–7 membered monocyclic ring or 8–10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; R...
08/29/2006
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
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
7053215Substituted Quinazolin-4(3H)-one compounds, compositions, and methods for their use
Compounds are provided that have the formula: where X, A4, Ra, R1, R2, R3, R4, R14, L and Q are as described herein. These compounds ar...
05/30/2006
6989385Pyrazole compounds useful as protein kinase inhibitors
This invention describes novel pyrazole compounds of formula IIc: wherein R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heteroc...
01/24/2006
6962922Alkynylated quinazoline compounds
A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represe...
11/08/2005
6949535Inhibitors of human phosphatidyl-inositol 3-kinase delta
Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ ac...
09/27/2005
6949550Substituted amino methyl factor Xa inhibitors
The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa. ...
09/27/2005
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
6919331Substituted 2-methyl-benzimidazole respiratory syncytial virus antiviral agents
The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides heterocyclic substituted 2-methylbenzimidazole derivatives for the treatm...
07/19/2005
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
6906070Guanidine mimics as factor Xa inhibitors
The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are use...
06/14/2005
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
6890924Substituted 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 and p a...
05/10/2005
6869945Pyrrolyl-and imidazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula:
03/22/2005
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