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Class 544/364 - At least three hetero rings containing


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain a hetero ring in addition to the
No. of patents: 831
Last issue date: 04/17/2012


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NumberTitleIssue Date
8158789Arginine derivatives with NP-I antagonistic activity
The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists. ...
04/17/2012
8153792Process for the synthesis of 2-aminothiazole compounds as kinase inhibitors
The present invention relates to an industrial process of preparing pharmaceutical compounds having the formula (1) which are useful as certain tyrosine kinase inhibitors and more particularly as c-kit and bcr-abl inhibitors. The groups R1 and R2, identical or diffe...
04/10/2012
8124766Inhibitors of diacylglycerol acyltransferase
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...
02/28/2012
7928231Thienopyrazoles
Thienopyrazoles of formula I, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical uses in the treatment of disease states capable of being modulated by the inhibition of the protein kinases, in particular interleukin-2...
04/19/2011
RE41425Piperazine and piperidine compounds
A group of new piperazine and piperidine compounds having interesting advantageous pharmacological properties and have the formula (a) wherein A represents a heterocyclic group having 5-7 ring a...
07/06/2010
7576203Method for producing cyclic diamine derivative
The present invention provides an industrially useful method for synthesizing a cyclic diamine derivative (4) or a salt thereof which serves as an ACAT inhibitor. A 2-hydroxyacetylaminopyridine compound represented by formula (1), and a method for producing a...
08/18/2009
7439371Indol kinase inhibitors
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. ...
10/21/2008
7439360Vanilloid receptor ligands and their use in treatments
Therapeutic benzimidazoles and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, ...
10/21/2008
7435736Substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine derivatives and their use as neurokinin antagonists
The invention concerns substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine having neurokinin antagonistic activity, in particular NK1 and NK1/NK3-antagonistic activity, their preparation, compositions comprising them and their us...
10/14/2008
74322551H-indol-5-yl-piperazin-1-yl-methanone derivatives
The present invention relates to compounds of formula I and their pharmaceutically acceptable salts wherein in formula I is: wherein R1 to R4 are as defined in the description and claims. The compounds...
10/07/2008
7432264Antimicrobial biaryl compounds
Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain. ...
10/07/2008
7425557Inhibitors of glycogen synthase kinase 3
New pyridine-based compounds of Formula I, compositions, and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3-mediated disorders in vivo are provided. The methods, compounds, and compositions of the invention ma...
09/16/2008
7425558Serotonergic agents for treating sexual dysfunction
Methods and compositions are provided for treating sexual dysfunction, e.g., sexual dysfunction associated with drug treatment, using 5-HT1A receptor antagonists. ...
09/16/2008
74230552-(3-Aminoaryl)amino-4-aryl-thiazoles for the treatment of diseases
The present invention relates to novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human an...
09/09/2008
7423039(4-phenylpiperazin-1-yl)acylpiperidine derivatives, preparation thereof and application of same in therapeutics
The invention relates to substituted (4-phenylpiperazin-1-yl)acylpiperidine derivatives of formula (I) in the form of a base or an addition salt with an acid, and also in the form of a hydrate or solvate, and their preparat...
09/09/2008
7410970Substituted 1,4,-di-piperidin-4-yl-piperazine derivatives and their use as neurokinin antagonists
The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular fo...
08/12/2008
7405217N-aroyl piperazine derivatives as orexin receptor antagonists
This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals. ...
07/29/2008
7393845Heteroaryl derivates, their preparation and use
A heteroaryl derivative having the formula (I). The compounds of the invention are considered useful for the treatment of affective disorders such as general anxiety disorder, panic disorder, obsessive compulsive disorder, depression, social phobia and eating disord...
07/01/2008
7365196Sulphonamido-substituted bridged bicycloalkyl derivatives
A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease. ...
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
7351822Serine protease inhibitors
Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovasc...
04/01/2008
7351828Benzimidazoles that are useful in treating sexual dysfunction
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction. ...
04/01/2008
7348327Compounds
The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms. ...
03/25/2008
7345042MCH antagonists for the treatment of obesity
The present invention discloses methods of using antagonists for melanin-concentrating hormone (MCH), to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes, as well as novel compounds which are antagonists for melanin-concentratin...
03/18/2008
7332495Aralkyl-ketone piperazine derivatives and their uses as new antalgic or ataractic agent
Arylalkyl ketone piperazine derivatives of the formula: and pharmaceutical compositions comprising the same. Also disclosed are methods for using the compounds as analgesic and sedative agents. The compounds of t...
02/19/2008
7314879Melanocortin receptor agonists
The present invention relates to melanocortin receptor agonist of the formula (I): which is useful in the treatment for obesity, diabetes, and male and/or female sexual dysfunction ...
01/01/2008
7307081Piperidine derivatives useful as CCR5 antagonists
The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein the various moieties are as defined in the specification. The present invention also provides pharma...
12/11/2007
7300939Substituted 1-propiolylpiperazine compounds, their preparation and use
Substituted 1-propiolylpiperazine compounds corresponding to formula I in which X denotes N or C—R2, and n is an integer from 0 to 8, a method for producing such substituted 1-propiolylpiperazine com...
11/27/2007
7291738Therapeutic compounds
The present invention provides compounds, for example, of formula (I): wherein R1, R2, and R3 have any of the values defined in the specification, as well as pharmaceutical compos...
11/06/2007
7288545Piperazinedione compounds
This invention relates to a method for treating an angiogenesis-related disease. The method includes administering to a subject in need thereof an effective amount of a piperazinedione compound having the formula:
10/30/2007
7285545Cytokine inhibitors
Disclosed are compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as...
10/23/2007
7271168Piperazine derivatives having SST1 antagonistic activity
The invention provides compounds of formula (1) wherein X, R1 and R2 are as defined in the specification, their, preparation and to their use in treating, e.g., depression, anxiety an...
09/18/2007
7271261Substituted benzimidazoles and imidazo-[4,5]-pyridines
2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer. ...
09/18/2007
7241761Phenyl-piperazine methanone derivatives, substituted by heterocyclic groups
The present invention relates to compounds of the general formula I wherein R1 is the group and R2, R′, R″, R3...
07/10/2007
7241787Substituted N-cycloexylimidazolinones, process for their preparation and their use as medicaments
The invention relates to substituted N-cyclohexylheterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to processes for their preparation and to their use as medicaments. Compounds of the formula I,
07/10/2007
7238688Piperidine compounds
Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such ...
07/03/2007
7235661Fused bicyclic aromatic compounds that are useful in treating sexual dysfunction
The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherei...
06/26/2007
7229997Compounds and their use
Compounds of the general formula (I): wherein R1, R2, R3 and R4 are as described in the specification. F...
06/12/2007
7226928Methods for the treatment of periodontal disease
The disclosure provides methods for the treatment and prevention of periodontal disease. In preferred embodiments, the invention provides for local treatment of periodontal tissues with a pharmaceutical composition including an immune response modifier (IRM) selecte...
06/05/2007
7223760Substituted triazole compounds
Novel substituted triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ...
05/29/2007
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