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Class 548/364.1 - Additional hetero ring attached directly or indirectly to the diazole ring by nonionic bonding


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds containing an additional hetero ring which is
No. of patents: 380
Last issue date: 05/22/2012


1                    
NumberTitleIssue Date
8183387Phenylpyrazole derivatives
The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, cir...
05/22/2012
8067615Sulphonylpyrroles
Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors. ...
11/29/2011
8058452Pyrazolyl-substituted heterocycles and their use as phytosanitary products
The present invention relates to novel pyrazolyl-substituted heterocycles of the formula (I) in which X, Y, Z and Het are as defined in the disclosure, to processes for their preparation, and to the...
11/15/2011
77456383,4-disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinase and glycogen synthase kinase-3 modulators
The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3....
06/29/2010
7491829RAF inhibitor compounds and methods
Pyrazolyl compounds of Formulas Ia and Ib are useful for inhibiting Raf kinase and for treating disorders mediated thereby. Methods of using pyrazolyl compounds for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cell...
02/17/2009
7435829Pyrazolyl-substituted heterocycles and their use as phytosanitary products
The present invention relates to novel pyrazolyl-substituted heterocycles of the formula (I) in which X, Y, Z and Het are as defined in the disclosure, to processes for their preparation, and to the...
10/14/2008
7432271Pyrazolyl inhibitors of 15-lipoxygenase
The present invention provides pyrazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions. ...
10/07/2008
7429581Pyrazole-derivatives as factor Xa inhibitors
The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is...
09/30/2008
7414056Pyrazole-amide compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where G, X, R1, R2, R3, R4, R5, R6
08/19/2008
7407977Substituted N-acyl-2-aminothiazoles
There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea. ...
08/05/2008
7407974Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade
The present invention provides compounds of Formula (I): wherein A, B, C, G, and W1 have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful to treat thro...
08/05/2008
7402683Cinnamic acid amides
The present invention relates to compounds, to processes for preparing them, to pharmaceutical compositions comprising them, and to their use in the therapy and/or prophylaxis in illnesses in people or animals, especially diseases of bacterial infection. ...
07/22/2008
7393842Pyrazole analogs acting on cannabinoid receptors
One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the i...
07/01/2008
7390810Pyrazole-amine compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I) useful for treating p38 kinase-associated conditions, where G, X, R1, R2, R3, R4, R5, R6
06/24/2008
7361672Heteroarylacetamide inhibitors of factor Xa
The invention is concerned with novel heteroarylacetamides of formula (I) Rd—C(O)—N(Re)—Rc—CH2—C(O)—N(Ra)(Rb)  (I) wherein Ra to Re are as def...
04/22/2008
7354944Thiadiazole compounds and methods of use
The invention relates to thiadiazole compounds useful for treating diseases mediated by protein kinase B (PKB). The invention also relates to the therapeutic use of such thiadiazole compounds and compositions thereof in treating disease states associated with abnorm...
04/08/2008
7348440Mitotic kinesin inhibitors
The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comp...
03/25/2008
7332518Carboxamides as fungicides in agriculture
The invention concerns novel carboxamides of formula (I) wherein A is (A1), (A2), (A3), (A4), (A5); Q is (Q1), (Q2), (Q3), (Q4), (Q5), (Q6); R1 is CH2 R2, CH2CH═CHR2, CH═C═CHR2 or COR3
02/19/2008
7317014Bio-active pyrimidine molecules
The present invention relates to novel derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutical...
01/08/2008
7300950Pyrazole derivatives, their preparation and their use in pharmaceuticals
The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: in which X, R1, R1a, R2, R3, R4 a...
11/27/2007
72825164-cyanopyrazole-3-carboxamide derivatives, preparation, and application thereof
The invention relates to 4-cyanopyrazole-3-carboxamide derivatives of formula (I): in which R1, R2, R3, R4, R5, R6, R7, R8 a...
10/16/2007
7279476Pyrazole-derived kinase inhibitors and uses thereof
Described herein are compounds that are useful as protein kinase inhibitors having the formula: where B, R1, n, R3, Q, and R4 are described in the specification. The compounds are...
10/09/2007
7253290Pyrazole derivatives as GnRH inhibitors
The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R5, R6, R6a, R7, R8, A, B and M are...
08/07/2007
7247635Pyrazole derivative
Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors conta...
07/24/2007
72477343,4-diarylpyrazoles and their use in the therapy of cancer
The present invention pertains to the use of certain 3,4-diarylpyazoles of formula (I), both in vitro and in vivo, to inhibit heat shock protein 90 (HSP90), and in the treatment of conditions mediated by HSP90, including, for example, cancer; wherein: Ar3
07/24/2007
7244739Compounds and uses thereof in modulating amyloid beta
Novel compounds, compositions, and kits are provided. Methods of modulating Aβ levels, and methods of treating a disease associated with aberrant Aβ levels are also provided. ...
07/17/2007
7241792Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof
The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor.
07/10/2007
7238722Pyrazolylalkines
The present invention relates to pyrazolyalkines and to their use, to a process for preparing them and also to intermediates. ...
07/03/2007
7232912Indazole compounds, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modulate and/or i...
06/19/2007
7230025Pyrazole derivatives
This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R4 are defined in the description, and to pr...
06/12/2007
7230116Pyrazolyl-substituted heterocycles and their use as phytosanitary products
The present invention relates to novel pyrazolyl-substituted heterocycles of the formula (I) in which X, Y, Z and Het are as defined in the disclosure, to processes for t...
06/12/2007
7208169Biphenyl carboxamides
The invention relates to novel biphenylcarboxamides of the formula (I) in which R1, R2, m, n, R3, Y and A are as defined in the disclosure, to a plurality...
04/24/2007
7205323Dipeptidyl peptidase IV inhibitors pharmaceutical compositions containing them, and process for their preparation
The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: wherein X, Y, a, R1, and R2 are as defined herein. ...
04/17/2007
7189755Pyrrolidine melanocortin-specific compounds
Melanocortin receptor-specific pyrrolidine compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where R1, R2, and R3 are as described in...
03/13/2007
7186741Neurotensin active 2,3,diaryl-pyrazolidine derivatives
The invention relates to a group of novel 2,3 diaryl-pyparazolidine derivatives having formula (1). The symbols used in formula (1) have the meanings given in the specification. The compounds have inhibiting activity on enzymes which degrade the neuropeptide neurote...
03/06/2007
7186843Aminomethylpyrrolidine derivatives having aromatic substituents
This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of th...
03/06/2007
7186738Antibacterial oxalidinones
Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl, substituted with: T is for example selected from (TAa1 to TAa12) such...
03/06/2007
7183307Pyrazole-derived kinase inhibitors and uses thereof
Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein B, R1, n, R3, Q and R4 are described in the specification. The compounds ar...
02/27/2007
71798352-(3-sulfonylamino-2-oxopyrrolidin-1-yl)propanamides as factor xa inhibitors
The invention relates to compounds of formula (I) pharmaceutical compositions containing the same as well as methods of treating patients suffering from a condition susceptible to amelioration by a Factor Xa inhibitor using the same.
02/20/2007
7157482Antibacterial 1,3-oxazolidin-2-one derivatives
Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereof, wherein: N—HET is for example triazolyl substituted with R1; R1 is for example optionally substituted (1-4C)alkyl; Q is for example ...
01/02/2007
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