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Class 546/276.4 - The additional hetero ring is five-membered consisting of one nitrogen and four carbons


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the additional hetero ring is five-membered
No. of patents: 710
Last issue date: 07/12/2011


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NumberTitleIssue Date
79774881-heterocyclylsulfonyl, 2-aminomethyl, 5-(hetero-) aryl substituted 1-H-pyrrole derivatives as acid secretion inhibitors
The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monoc...
07/12/2011
7888512Synthesis of nicotine derivatives from nicotine
Methods of synthesizing nicotine analogs and derivatives are described. In some embodiments the methods utilize an alkyl or aryl silyl-substituted nicotine analog intermediate. Intermediates useful for the synthesis of nicotine and nicotine analogs are also describe...
02/15/2011
7820826Synthesis and regioselective substitution of 6-halo-and 6-alkoxy nicotine derivatives
The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds. ...
10/26/2010
7553968Synthesis of nicotine derivatives from nicotine
Methods of synthesizing nicotine analogs and derivatives are described. In some embodiments the methods utilize an alkyl or aryl silyl-substituted nicotine analog intermediate. Intermediates useful for the synthesis of nicotine and nicotine analogs are also describe...
06/30/2009
7514562Urea derivatives and their use as vanilloid receptor antagonists in the treatment of pain
Compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein P, P′, W, R1, R2, n, p, q, r, s and t are as defined in the specification, processes for preparing such compo...
04/07/2009
7501520Regioselective halogenation of nicotine and substituted nicotines
A first aspect of the present invention is a method for of making a compound of Formula Ia or Formula Ib: wherein X is halo, by (a) metalating a precursor compound to form an organometallic intermediate, and then reacting t...
03/10/2009
7446205Method for making nicotine hapten
A high yielding and short process for preparing the 3′-aminomethylnicotine hapten of general formula I permits the isolation of the hapten in very pure quantities. The process can be adapted for the synthesis of a single ...
11/04/2008
RE40525Hepatitis C inhibitor tri-peptides
A racemate diastereoisomer and optical isomer of a compound of formula (I): wherein B is H, a C6 or C10 aryl, C7-16 aralkyl; Het or (lower alkyl)-Het, all of which may be optionally substituted wi...
09/30/2008
7399765Substituted diazabicycloalkane derivatives
Compounds of formula (I) Z-Ar1—Ar2  (I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substitute...
07/15/2008
73968435′-carbamoyl-1,1′-biphenyl-4-carboxamide derivatives and their use as p38 kinase inhibitors
Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...
07/08/2008
7390907Vanilloid 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...
06/24/2008
7371768Pyrazol derivatives, pest control agent comprising the same as active ingredient, and process for producing the same
The present invention relates to pest control agent having systemic activity and a high safety along with a wide insecticidal spectrum and excellent insecticidal activity, which are 1-aryl-3-cyano-5-pyridylalkylaminopyrazole derivatives represented by formula (1):
05/13/2008
7368470Substituted 3-pyrrolidine-indole derivatives
Substituted 3-pyrrolidine-indole derivatives and methods for their production. Also pharmaceutical compositions containing these compounds and the use of these substances in methods of treatment, in particular treatment of pain and/or depression. ...
05/06/2008
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
7361768Synthesis of nicotine derivatives from nicotine
Methods of synthesizing nicotine analogs and derivatives are described. In some embodiments the methods utilize an alkyl or aryl silyl-substituted nicotine analog intermediate. Intermediates useful for the synthesis of nicotine and nicotine analogs are also describe...
04/22/2008
7358263Fused bicyclic-substituted amines as histamine-3 receptor ligands
Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands...
04/15/2008
7323462Morpholine dopamine agonists
Compounds of formula (I), (Ia) and (Ib) useful as a medicament. ...
01/29/2008
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
7304159Ligands and catalyst systems thereof for ethylene oligomerisation to linear alpha olefins
Mixed bis-imine pyridine ligands of formula (I), wherein Z1, which is different from Z2, is an optionally substituted aryl group; and Z2 comprises an optionally substituted heterohydrocarbyl moiety, or an optionally substituted aryl ...
12/04/2007
7297694Pyridylfurans and pyrroles as Raf kinase inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. ...
11/20/2007
7294647Kappa agonist compounds and pharmaceutical formulations thereof
Compounds having kappa opioid agonist activity, compositions containing them and 5 method of using them as analgesics and pruritic agents are provided. The compounds of formulae I, II, III and IV have the structure: ...
11/13/2007
7279470Compounds and uses thereof for decreasing activity of hormone-sensitive lipase
Use of compounds to inhibit hormone-sensitive lipase, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and novel compounds. The present compounds are inhibitors of hormone-sensitive lipase and may...
10/09/2007
7276524Pyridyl alkane acid amides as cytostatics and immunosuppressives
The invention relates to new pyridyl alkane acid amides according to general formula (I) as well as methods for their production, medicaments containing these compounds as well as their medical use, especially in the treatment of tumors or for immunosuppression ...
10/02/2007
7276500Substituted amides, their preparation and use
An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings:...
10/02/2007
7262207Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and v...
08/28/2007
7256203Dicationic 2,5-diarylfuran aza-analogs as anti-protozoan agents
A compound of Formula (I): wherein: X is selected from the group consisting of O, S, and NR17, where R17 is hydrogen or lower alkyl; A and...
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
7247735Octupolar molecules used as organic semiconductors
In the case of the materials according to the invention, the charge carrier mobility in the correspondingly prepared films is achieved if the molecules are composed in such a way that side chains—consisting of conjugated aromatic or heteroaromatic systems—are at...
07/24/2007
7247648N-alkyl-4-methyleneamino-3-hydroxy-2-pyridones
Compounds of Formula (I) are effective in the treatment of a microbial infection. ...
07/24/2007
7241745Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their m...
07/10/2007
7235566Pyridinone derivatives for treatment of atherosclerosis
Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis. ...
06/26/2007
7220761Compounds and methods for controlling fungi, bacteria and insects
The present invention includes compounds of pyridinium salts and methods of their use for industrial uses. The present invention also relates to methods of controlling fungi and/or bacteria. The present invention may also be used to control insects. ...
05/22/2007
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
7205305Inhibitors of p38
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceut...
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
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
71867222-heteroaryl-3,4-dihydro-2h-pyrrole derivatives and the use thereof as pesticides
Novel Δ1-pyrrolines of the Formula (I) in which R1, R2, R3 and Het have the meanings given in the description, a plurality of processes for prep...
03/06/2007
7183297Biphenyl-derivatives as p38-kinase inhibitors
Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ...
02/27/2007
7179806Δ1-pyrrolines used as pesticides
The invention relates to novel Δ1-pyrrolines of the formula (I) in which R1, R2, R3, m, and Q have the meanings given in the disclosure, to a plurality of processes fo...
02/20/2007
7173129Sulfonamide-substituted chalcone derivatives and their use to treat diseases
The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the ...
02/06/2007
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