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Class 514/252.03 - The additional hetero ring is six-membered consisting of one nitrogen and five carbon atoms


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the additional hetero ring consists
No. of patents: 366
Last issue date: 03/20/2012


1                    
NumberTitleIssue Date
8138188Melanocortin type 4 receptor agonist piperidinoylpyrrolidines
The present invention relates to a class of melanocortin MCR4 agonists of general formula (I) wherein the variables and substituents are as defined herein and especially to selective MCR4 agonist compounds, to their use in ...
03/20/2012
8044052Biaryl ether urea compounds
The present invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions c...
10/25/2011
8034814Phthalazine derivatives with angiogenesis inhibiting activity
The invention relates to new phthalazine derivatives of formula I, and to processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof alone or i...
10/11/2011
8026240Octahydro-pyrrolo[3,4-b]pyrrole N-oxides
The invention relates to octahydro-pyrrolo[3,4-b]pyrrole N-oxides as prodrugs of CNS-active compounds, compositions comprising such compounds, methods for making the compounds, salts, and polymorphs, and methods of treating conditions and disorders using such compou...
09/27/2011
7968546Pyridazinone kinase inhibitors
Disclosed are compounds of Formula I wherein X is and R2, R1, A, B, D, E, R9 are as defined herein useful for treating cancers. ...
06/28/2011
7960383Pyridazin-3(2)-one derivatives and their use as PDE4 inhibitors
The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives of Formula (I) and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatm...
06/14/2011
7872010Substituted diazabicycloalkane derivatives having affinity for nicotinic acetylcholine receptors
Provided herein are compositions of a class of substituted diazabicycloalkane derivative compounds, which are useful as modulators of nicotinic acetylcholine receptors. The compounds are useful in treating conditions and disorders prevented by, or ameliorated by, ni...
01/18/2011
7846932Methods for the use of pyrimidine derivatives which are antagonists of 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...
12/07/2010
7825119Pyrimidine derivatives which are antagonists of 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...
11/02/2010
7803801Aminopyridine compounds having Syk inhibitory activity
The present invention relates to an aminopyridine compound represented by the following general formula (I) or a salt thereof and an Syk inhibitor containing the compound or a salt thereof as an active ingredient. Here, X1, X2, X3, Z...
09/28/2010
7799787Heteroaromatic compounds as inhibitors of stearoyl-coenzyme a delta-9 desaturase
Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment o...
09/21/2010
7790723Thiazole derivatives as phosphodiesterase IV inhibitors
Thiazole derivatives of the formula I in which R1, R2, R3, V, W, X and B are as defined in claim 1, act as phosphodiesterase IV inhibitors and can be employed for the treatment of ost...
09/07/2010
7786119Drug conjugates of ion channel modulating compounds
This invention is directed to drug conjugates of certain ion channel modulating compounds having the following formula: wherein A, X, R1, R2, R3, R4, R5, LB, L and DM a...
08/31/2010
7732448Pyrimidine compounds and pests controlling composition containing the same
The present invention relates to a pyrimidine compound of the formula (I): wherein R1 represents a hydrogen atom, halogen atom or C1-C4 alkyl; R2 represents C3-C7 alkynyloxy; R3 represents a...
06/08/2010
77279894-benzimidazol-2-yl-pyridazine-3-one-derivatives, production and use thereof in medicaments
The present invention relates to kinase inhibitor compounds and derivatives thereof as well as compositions comprising them consisting of the structure of formula I: Wherein R1, R2, A, B, D and E are defined herein. These 4...
06/01/2010
7547700Aryl-[4-halo-4(heteroarylmethylamino)-methyl]-piperidin-1-1yl]-methanone derivatives, methods for production and use thereof as medicaments
The invention relates to compounds of general formula (1) in which X and Y=a carbon with a bonded hydrogen atom (CH) or a nitrogen atom, A=a methyl, fluoromethyl, cyano, hydroxyl, methoxy group, or a chlorine or fluorine atom on condition that when A=methyl (CH3) an...
06/16/2009
7465731HDAC inhibitor
A compound having the formula (I): wherein R1 is hydrogen, lower alkyl, lower alkenyl, lower or higher alkynyl, cyclo(lower)alkyl, cyclo(higher)alkyl, cyclo(lower)alkyl(lower)alkyl, cyclo(higher)alky...
12/16/2008
7399761Phthalazine derivatives with angiogenesis inhibiting activity
The invention relates to new phthalazine derivatives of formula (I), wherein R1 and R2: a) are independently in each case a lower alkyl; b) together form a bridge of subformula (I*), wherein the bond is achieved via the two terminal C atoms and...
07/15/2008
7396831Vanilloid receptor ligands and their use in treatments
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascu...
07/08/2008
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
7381725Pyridazine derivatives as ligands for GABA receptors
A class of pyridazine derivatives, substituted in the 4-position by an optionally substituted heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of b...
06/03/2008
7365074Pyridazine, pyrimidine and pyrazine ethyne compounds
In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring that includes at least one nitrogen atom and at least one...
04/29/2008
7361657Respiratory syncytial virus replication inhibitors
This invention concerns the use of compounds of formula (I) wherein −a1=a2−a3=a4—is a radical of formula —CH═CH—CH═CH—, —N═CH—CH═CH—, —CH═N—CH═CH—, —CH═CH—N═CH—, —CH═CH—C...
04/22/2008
7348327Compounds
The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms. ...
03/25/2008
7338968Thiadiazoles AS CXC- and CC- chemokine receptor ligands
Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl...
03/04/2008
7338955Medicament for treatment of neuropathies
Compounds of formula (I) in which R1=C1-6 alkyl, optionally halosubstituted; R2=H, C1-4 alkyl, optionally halosubstituted or replaced by halogen; R3=C2-4 alkyl, optionally halosubstituted; R4
03/04/2008
7329660Phthalazine derivatives for treating inflammatory diseases
The invention relates to the treatment of leukemias with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specificatio...
02/12/2008
7320977Substituted 2-phenyl-3(2h)-pyridazinones
The invention relates to substituted 2-Phenyl-3(2H)-Pyridazinones, to a method for the production thereof, and to their use as medicaments for the prophylaxis and/or treatment of diseases in humans and/or animals. ...
01/22/2008
7309701Pyridazinone derivatives as pharmaceuticals and pharmaceutical compositions containing them
The present invention relates to novel pyridazinone derivatives of the general formula (I) wherein A is A1 or A2; ...
12/18/2007
7294627Chemical compounds
Compounds of formula (I) in which R1, R2, R3 and R4, have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorde...
11/13/2007
7294625Pyrazole compounds
The present invention relates to pyrazole compounds represented by the formula (I): wherein R1 represents phenyl which may be substituted, R2 represents H, halogen, ...
11/13/2007
7288542Non-nucleoside reverse transcriptase inhibitors
The present invention relates to a compounds according to formula I, methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula I and pharmaceutical compositions for treating diseases mediated by human ...
10/30/2007
72681502-cyano-4-fluoropyrrolidine derivative or its salt
Provided is a compound having excellent dipeptidyl peptidase IV-inhibiting activity, and a remedy based on the activity for insulin-dependent diabetes (type 1 diabetes), especially for non insulin-dependent diabetes (type 2 diabetes), insulin-resistant disorders, an...
09/11/2007
7259157N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain. ...
08/21/2007
7256192Aromatic diamide derivatives, chemicals for agricultural or horticultural use and usage thereof
The present invention relates to an aromatic diamide derivative represented by the general formula (I): [A1 is optionally substituted (C1-C8)alkylene grou...
08/14/2007
7241758Compounds useful as anti-inflammatory agents
Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory disease...
07/10/2007
72301059-aminoacridine derivatives and process for the preparation thereof
The present invention relates to a new 9-aminoacridine derivative which exhibits prominent antitumor activity and low toxicity. ...
06/12/2007
7214678Arylsulfanyl and heteroarylsulfanyl derivatives for treating pain
According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.
05/08/2007
7211577Water-soluble phenylpyridazine derivative and medicine containing the same
A phenylpyridazine derivative represented by the formula (1): Wherein, R1, R2, R3, X, Y, Z and n have the same meaning as defined in the specification; or a salt thereof, or a medicine containing the compound. Th...
05/01/2007
7208515Diphenylmethyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, e, m, R1, R2, R3, R4a, R4b, R5, R6, R7, and R8 a...
04/24/2007
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