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Class 544/224 - The six-membered hetero ring consists of two nitrogens and four carbons (e.g., 1,2-diazines, etc.)


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the six-membered hetero ring consists
No. of patents: 651
Last issue date: 11/29/2011


1                      
NumberTitleIssue Date
8067589Heterocyclic compounds useful in treating diseases and conditions
The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of su...
11/29/2011
8008485Process for producing 2,3-dihydropyridazine compound
A process for producing a 2,3-dihydropyridazine compound represented by the formula (2): wherein R1, R2 and R3 are the same or different and each represents a hydrogen atom, a halogen atom, ...
08/30/2011
7884204Phenylalanine derivatives
Phenylalanine derivatives of the following formula, analogues thereof and pharmaceutically acceptable salts thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning α4 integrin i...
02/08/2011
7829704Ionic liquids
The present invention relates to compositions of matter that are ionic liquids, the compositions comprising any of eleven cations combined with any of three fluorinated sulfonated anions. Compositions of the invention should be useful as solvents and, perhaps, as ca...
11/09/2010
7662959Quaternary trifluoromethylcyclohexane derivatives for liquid crystals
A compound having the structure: w-A-x-CY—Z(CF3), where CY is cyclohexane or substituted cyclohexane, exemplified by 4-trifluoromethyl-4-methylcarboxy-4′-propyl-1,1′-(bi)cyclohexane. ...
02/16/2010
RE40558Therapeutic uses of di-aryl acid derivatives
The use of diaryl acid derivatives of formula (I) or pharmaceutically acceptable salts, N-oxides, hydrates or solvates thereof, wherein the variables shown are defined in the disclosure, and their pharmaceutical compositions as P...
10/28/2008
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
7432261Anti-inflammatory phosphonate compounds
The invention is related to phosphorus substituted anti-inflammatory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such com...
10/07/2008
7429278N-alkyleheteroaryl secondary para-phenylenediamine and composition comprising such a para-phenylenediamine
The present disclosure is directed to a family of N-alkylheteroaryl secondary para-phenylenediamines, to their preparation, and to a cosmetic composition for dyeing keratin fibers, for example, human keratin fibers such as the hair, comprising, in a suitable dyeing ...
09/30/2008
7419653Method for preparing radiolabeled thymidine having low chromophoric byproducts
The invention is a method and related precursor for preparing 18F-FLT. The precursor has a butoxycarbonyl protecting group at the 5′-position that results in low amounts of chromophoric byproducts being formed during deprotection. The method for prepari...
09/02/2008
7414067Ophthalmic compositions for treating ocular hypertension
This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such co...
08/19/2008
7408066Carbon-linked substituted piperidines and derivatives thereof useful as histamine Hantagonists
Disclosed are compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N;
08/05/2008
7405297Process for preparing inhibitors of nucleoside metabolism
A process of preparing a compound of the formula (I) wherein B is chosen from OH, NH2, NHR, H or halogen; D is chosen from OH, NH2, NHR, H halogen or SCH3; R is an optionally substituted alk...
07/29/2008
7402557Combined treatment with keratinocyte growth factor and epidermal growth factor inhibitor
The present invention relates to compositions and methods for treating the epithelial toxicity caused by administering to a human cancer patient an epidermal growth factor receptor (EGFR) inhibitor. The pharmaceutical composition preferably comprises an EGFR inhibit...
07/22/2008
7396840Chemokine receptor binding heterocyclic compounds
Tertiary amine compounds that bind chemokine receptors such as CXCR4 and CCR5 are disclosed. ...
07/08/2008
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
7371777Cyclic compound and PPAR agonist
The present invention provides a novel compound having an excellent PPAR agonist action. More specifically, it provides a compound represented by the following formula, a salt thereof, an ester thereof or a hydrate of them. ...
05/13/2008
7365092Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they ac...
04/29/2008
7361755Transition-metal-catalyzed process for the conversion of alkenes to sterically hindered substituted n-alkoxyamines
This invention pertains to a novel process for preparing sterically hindered N-substituted alkyloxyamines from alkenes by the transition-metal-catalyzed reaction of a intermediate alkylborane with a sterically hindered nitroxyl radical. ...
04/22/2008
7351826Aryl acid pyrimidinyl methyl amides, pyridazinyl methyl amides and related compounds
The invention provides compounds of Formula (I) that bind to GABAA receptors. In the above formula, variables are defined herein. Such compounds may be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly...
04/01/2008
7351825Cyclopropane compounds and pharmaceutical use thereof
The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1):
04/01/2008
7348326Heteroaryl fused aminoalkyl imidazole derivatives: selective modulators of GABAreceptors
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are...
03/25/2008
7348328MCH antagonists for the treatment of obesity
The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonist...
03/25/2008
7329757Substituted iminoazines
The invention relates to novel substituted iminoazines of the general formula (I) in which R1, R2, R3, R4, Z1, Z2 and Z3 a...
02/12/2008
7320978Oxazole derivatives, preparation and therapeutic use thereof
This invention relates to compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as described herein. The i...
01/22/2008
7317010Thieno-pyrrole compounds as antagonists of gonadotropin releasing hormone
The invention relates to a group of novel thieno-pyrrole compounds of Formula (I), wherein: R1, R2, R4, R5, R6, R6a, R7, R8, A and ...
01/08/2008
7312328Benzoylpyridazines
This invention relates to compounds of the formula (I) in which R1, R2, R3, X and Q are as defined above and their use as PDE IV inhibitors. ...
12/25/2007
7307168Process for the preparation of 3-{2-′4- (6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyllethyl}-6,7,8,9-tetrahydro-2-methyl-4h-pyrido′1,2-methyl-4h-pyrido′,2-a!pyrimidin-4-one
The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by sub...
12/11/2007
7304067Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide
Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease. ...
12/04/2007
7300921Polyene polyketides and methods of production
Novel polyene polyketides, their pharmaceutically acceptable salts, prodrugs and derivatives have been found to have antibiotic activity. One method for obtaining the compounds is by cultivation of Amycolatopsis orientalis ATCC™ 43491 or a mutant or variant...
11/27/2007
7300930Therapeutic acridone and acridine compounds
The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ═O, L is —H, alpha is a single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a doubl...
11/27/2007
7294624Barbituric acid derivatives as inhibitors of TNF-α converting enzyme (TACE) and/or matrix metalloproteinases
The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R1, R2, R3, R...
11/13/2007
7288650Cyclic substituted fused pyrrolocarbazoles and isoindolones
The present invention is directed to cyclic substituted fused pyrrolocarbazoles and isoindolones. The invention also is directed to methods for making and using the cyclic substituted fused pyrrolocarbazoles and isoindolones. ...
10/30/2007
7279480Hexahydropyridazine-3-carboxylic acid hydrazide and hydrazone derivatives, combinatorial libraries containing same, pharmaceutical compositions containing same and methods of preparation
The present invention discloses and claims hexahydropyridazine-3-carboxylic acid hydrazides and hydrazones of formula (I) as inhibitors of proteases and kinases, and methods of using said compounds of formula (I)...
10/09/2007
7279475Fluorinated di-aryl urea compounds
Disclosed are compounds of formula(I): wherein R1, R2, W and X of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus...
10/09/2007
7276086Composition comprising at least one pyrazine derivative and the use thereof for the direct or oxidation dyeing and/or optical bleaching of keratin fibers
The invention relates to a composition comprising a pyrazine derivative and to methods using said compositions as an optical bleach and/or dye in a direct or oxidation dyeing composition for keratin fibers, such as human keratin fibers, for example, hair. The invent...
10/02/2007
7268135Biaryl sulfonamides and methods for using same
The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors. ...
09/11/2007
7259179Kinase inhibitors
A compound of the general formula: or pharmaceutically acceptable salts, hydrates, solvates, crystal forms or diastereomers thereof is described. A method of treating protein kinase-associated disease states usin...
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
72561883-aminoalkyl-2-aryl-indole derivatives and their use as GnRH antagonists
The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicam...
08/14/2007
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