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Class 514/256 - 1,3-diazines (e.g., pyrimidines, etc.)


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter in which the ring nitrogen atoms occupy the
No. of patents: 2271
Last issue date: 05/29/2012


1                      
NumberTitleIssue Date
8188094Inhibitors of glutaminyl cyclase
Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: ...
05/29/2012
8188095Gyrase inhibitors and uses thereof
The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the p...
05/29/2012
8188096Protein kinase targeted therapeutics
The present invention relates to compositions and methods useful in treating diseases and disorders related to protein kinases. In particular, the present invention relates to compositions and methods useful for targeting protein kinases related to mitogen activated...
05/29/2012
8178540Pyrimidylmethyl-sulfonamide compounds
The present invention relates to novel pyrimidylmethyl-sulfonamide compounds and to their N-oxides, their agriculturally acceptable salts and their veterinarily acceptable salts and also to agricultural compositions comprising at least one such compound as active co...
05/15/2012
8168642Dihydropyrimidine compounds and their uses in preparation of medicaments for treating and preventing antiviral diseases
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof, to a process for preparing the compound of formula (I), and to use of the compound of formula (I) or a pharmaceutically acceptable salt or hydrate th...
05/01/2012
8148382Compounds for the treatment of hepatitis C
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. ...
04/03/2012
8148381Potentiator of radiation therapy
A radiation therapy potentiator, which, when employed in combination with cancer radiation therapy, can reduce radiation dose and can mitigate adverse effects, the radiation therapy potentiator containing, as an effective ingredient, a uracil derivative represented ...
04/03/2012
8143260Tricyclic amine compound
A compound represented by the following general formula (I): [wherein R1 represents hydrogen atom or a C1-6 alkyl group, A and B represent —(CH2)2—, —(CH2)3
03/27/2012
8133896Pyrimidine derivatives which are antagonist of the vitronectin receptor
A subject of the invention is the compounds of formula (I); in which R1, R2, R3, R4 and R have the meanings indicated in the description, their preparatio...
03/13/2012
81293962-[1H-benzimidazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides and 2-[benzothiazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides as kinase inhibitors
2-[1H-benzimidazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides and 2-[benzothiazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides and their salts are kinase inhibitors, useful in the treatment of cancer. ...
03/06/2012
81293954,5-disubstituted-2-aryl pyrimidines
4,5-disubstituted-2-arypyrimidines of Formula I and Formula II are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a ...
03/06/2012
8119645Fungicide hydroximoyl-tetrazole derivatives
The present invention relates to hydroximoyl-tetrazole derivatives of formula (I) wherein T represent a tetrazolyl substituent, A represents a carbo- or heterocycle, L1 and L2 represent various linking groups and Q represents a 5-membered heter...
02/21/2012
8119646Fungicide hydroximoyl-tetrazole derivatives
The present invention relates to hydroximoyl-tetrazole derivatives of formula (I) wherein T represent a tetrazolyl substituents, A represents a carbo- or heterocycle, L1 and L2 represent various linking groups and Q represents a carbocycle, the...
02/21/2012
8114882(1H-indol-7-yl)-(pyrimidin-2-ylamino)methanone derivatives and related compounds as IGF-R1 inhibitors for the treatment of cancer
The invention relates to compounds of the formula (I), in which Ar denotes a mono- or bicyclic aromatic homo- or heterocycle having 1 to 4 N, O and/or S atoms and 5 to 10 skeleton atoms, which may be unsubstituted or mono-, di- or trisubstituted by carbonyl oxygen, ...
02/14/2012
8101621Aminopyridine derivatives having aurora a selective inhibitory action
The present invention relates to a compound of general formula I: wherein: n1 and n2 are the same or different, and are 0 or 1; R is aryl, heteroaryl, etc.; Re
01/24/2012
8097630Pinane-substituted pyrimidinediamine derivatives useful as Axl inhibitors
Pinane-substituted pyrimidinediamine derivatives and pharmaceutical compositions containing the derivatives are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the derivatives in treating diseases or...
01/17/2012
8093253Leukotriene Binhibitors
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositi...
01/10/2012
8084457Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
The present invention relates to 4,6-disubstituted aminopyrimidine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, i...
12/27/2011
8080552Pyrimidyl derivatives as protein kinase inhibitors
Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the ...
12/20/2011
8076343Benzimidazoles useful as inhibitors of protein kinases
The present invention relates to compounds useful as inhibitors of Aurora, FLT-3, or PDK1 protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various...
12/13/2011
8067423Polymorphs of dasatinib isopropyl alcohol and process for preparation thereof
The invention provides crystalline forms of isopropyl alcohol solvate of dasatinib, methods for their preparation, and pharmaceutical compositions thereof. ...
11/29/2011
8067421Polymorphic forms of imatinib mesylate and processes for preparation of novel crystalline forms as well as amorphous and form α
Solvates and crystalline forms of imatinib mesylate are described. Further, methods for preparing such solvates and crystalline forms of imatinib mesylate are described. ...
11/29/2011
8067422Crystal form of phenylamino pyrimidine derivatives
The present invention relates to a particular form of the (3,5-bis trifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula I), processes for the preparation thereof, pharmaceutical compositions containing this crystal form, and t...
11/29/2011
8058279Insecticidal pyrimidinyl aryl hyrdrazones
Pyrimidinyl aryl hydrazones are effective at controlling insects. ...
11/15/2011
8053439Benzophenone derivatives useful for inhibiting formation of microtubule
Disclosed herein are novel benzophenone derivatives represented by formula I, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, a pharmacological composition containing the same, and a use of the composition as therapeutic drugs. Th...
11/08/2011
8048887Compounds for the treatment of hepatitis C
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. ...
11/01/2011
8026243[4,5′]Bipyrimidinyl-6,4′-diamine derivatives as protein kinase inhibitors
The invention provides a novel class of compounds of the Formula I: in which the symbols have the meanings given in the description and claims, to pharmaceutical compositions comprising such compounds and methods of using s...
09/27/2011
8012985Compounds with antiparasitic activity and medicines containing same
The invention relates to compounds having an anti-parasitic, in particular antimalarial activity, characterized in that they correspond to general formula (I) Applications in particular as compounds with anti-parasitic acti...
09/06/2011
8012986Pyridine and pyrimidine derivatives as MGLUR2 antagonists
The present invention relates to compounds of formula (I) wherein A, B, Q, X, Y, R1, and R2 are as defined herein; pharmaceutical compositions containing them; a process for their manufacture; and meth...
09/06/2011
8008307Heteroaryl compounds useful as inhibitors of E1 activating enzymes
This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including ca...
08/30/2011
8003655Substituted sulphoximines as TIE2 inhibitors and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
The invention relates to substituted sulphoximines according to the general formula (I): in which A, E, G, X, R1, R2, R3, R4, R5, R6, R7, R8
08/23/2011
7989458Pyrimidine derivatives as alk-5 inhibitors
Compounds of formula (I) in free or salt or solvate form, where T1, T2, Ra and Rb have the meanings as indicated in the specification, are useful for treating inflammatory or obstructive airways, pulmonary hypertension, pu...
08/02/2011
7989457Glucagon receptor antagonists, preparation and therapeutic uses
The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention d...
08/02/2011
79819002-phenyl pyrimidines which are tubulin inhibitors
Compounds of general formula (I), (II) (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also de...
07/19/2011
7981899Use of compatible solutes for inhibiting the release of ceramides
Disclosed are the use of compatible solutes for inhibiting the release of ceramides or for the prophylaxis and protection of human skin against premature skin aging and for the prophylaxis and protection of human skin against wrinkling. ...
07/19/2011
7977341Substituted isoxazoles as fungicides
The present invention provides compounds of formula I: (I) along with methods of making the same, compositions thereof, and methods of use thereof, particularly methods of use as fungicides. ...
07/12/2011
7973045Anhydrous form of dasatinib and process for preparation thereof
The invention provides anhydrous forms of dasatinib, methods for their preparation, and pharmaceutical compositions thereof. ...
07/05/2011
7973044Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4
Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, su...
07/05/2011
7968552Oxadiazolidinedione compound
A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided. It was found that an oxadiazolidinedione compound whi...
06/28/2011
7960393Pyrimidine derivatives useful for the treatment of diseases mediated by CRTH2
The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattra...
06/14/2011
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