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Class 546/214 - The additional hetero ring consists of one oxygen and four carbons


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which the additional hetero ring consists of
No. of patents: 301
Last issue date: 09/30/2008


1                
NumberTitleIssue Date
7429603C-fms kinase inhibitors
The invention is directed to compounds of Formulae I, II and III: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomer...
09/30/2008
7390803Tetrahydropyranyl cyclopentyl benzylamide modulators of chemokine receptor activity
The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28...
06/24/2008
7381721Substituted piperidine compounds
3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as anta...
06/03/2008
7361666Heterocyclic analgesic compounds and methods of use thereof
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-couple...
04/22/2008
7358251N-sulfonylurea apoptosis promoters
Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds. ...
04/15/2008
73420271-phenylpiperidin-3-one derivatives and processes for the preparation thereof
Provided are 1-phenylpiperidin-3-one derivatives and pharmaceutically acceptable salts thereof, having cysteine protease inhibitory activity, pharmaceutical compositions containing the same as an active ingredient, and processes for the preparation thereof. ...
03/11/2008
7335670Derivatives of N-[heteroaryl(piperidine-2-yl) methyl]benzamide, preparation method thereof and application of same in therapeutics
Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyrami...
02/26/2008
7326716Treatment of inflammatory bowel disease
The present invention provides a method of treating inflammatory bowel disease which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a piperidinyl prostaglandin E analog. ...
02/05/2008
7288657Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 ar...
10/30/2007
72054104-(aminomethyl)-piperidine benzamides for treating gastrointestinal disorders
The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, —R1—R2— is a ...
04/17/2007
7186719Antibacterial agents
Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(═O) or the formula: —C(═O)NH(OH); R1 represents hydrogen, C1–C6 alkyl or C1–C6 alkyl substit...
03/06/2007
7125895Cyclic amine derivatives and their uses
This invention relates to novel arylalkyl cyclic amine derivatives. This invention also relates to chemokine receptor antagonists that are be effective as therapeutic agents and/or preventive agents for diseases such as atherosclerosis, rheumatoid arthritis, transpl...
10/24/2006
7119203Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors
This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metallop...
10/10/2006
7115610Substituted heterocyclic compounds
Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atri...
10/03/2006
7084144Sulfonyl group containing compounds and their use for the treatment of erectile dysfunction
A compound having the general formula (I): wherein: X is N or C; R0 is H, a lower alkyl group, a lower O-alkyl group, lower alkyl group, a benzyl ...
08/01/2006
7041682NKantagonists
Disclosed are NK1 antagonists having the formula: Also disclosed are methods for treating a number of physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough, usi...
05/09/2006
7034110Method of identifying chemical compounds having selected properties for a particular application
A method for obtaining compounds having selected properties for a particular application by forming base modules having at least two structural diversity elements from the reaction of a first compound having at least one structural diversity element and a first reac...
04/25/2006
7019007CCR-3 receptor antagonists (I)
The invention provides compounds of Formula (I): wherein: R1–R4, A, D, and L have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions c...
03/28/2006
6995268N- and O-substituted 4-[2-(diphenylmethoxy)-ethyl]-1- (phenyl) methyl) piperidine analogs and methods of treating CNS disorders therewith
N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SE...
02/07/2006
6977260Piperidinyl prostaglandin E analogs
The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I;
12/20/2005
6977263Chemical compounds
Provided herein are novel and useful compounds having a tryptase inhibition activity, pharmaceutical compositions comprising such compounds, and methods treating subjects suffering from a condition, disease, or disorder that can be ameliorated by the administration ...
12/20/2005
6903120Modulators of dopamine neurotransmission
New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, O...
06/07/2005
6887871Use of phenylheteroakylamine derivatives
There is disclosed the use of a compound of formula (I) wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the t...
05/03/2005
6887870Heterocyclic sodium/proton exchange inhibitors and method
Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, a...
05/03/2005
6878723LTA4 hydrolase inhibitors
The invention concerns compounds inhibiting LTA4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications. ...
04/12/2005
6872735LFA-1 antagonist compounds
The invention relates to novel compounds having formula (I) wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-...
03/29/2005
6861530Piperidine derivatives
This invention relates to substituted piperidine derivatives having at least one six-membered ring substituent. The piperidine derivatives exhibit antitumor activity and are useful as pharmaceuticals such as an antitumor agent. ...
03/01/2005
6846825Antibacterial agents
Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(═O) or the formula: —C(═O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted...
01/25/2005
6800628N-substituted 4-((-4′-aminobenzoyl)-oxymethyl)-piperidines having gastric prokinetic properties
This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R1 is C1-6alkyloxy, C...
10/05/2004
6787650Urea compounds, process for producing the same and use thereof
A compound of the formula: [wherein R1 is a hydrocarbon group which may be substituted; R2 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substitu...
09/07/2004
6756387Hydroxyphenyl-piperidin-4-ylidene-methyl-benzamide derivatives for the treatment of pain
Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, triazolyl and thiazolyl; where each R1 phenyl ring and R1 heteroaroma...
06/29/2004
6747037Piperidinyl prostaglandin E analogs
The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I;
06/08/2004
67203364,4-biarylpiperidine derivatives
The present invention relates to compounds of the formula I, wherein Z1, Z2, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containin...
04/13/2004
6696443Piperidine/piperazine-type inhibitors of p38 kinase
Certain compounds which contain a piperidine moiety flanked by aryl groups are inhibitors of p38-଱ kinase and thus useful in the treatment of a variety of conditions characterized by inappropriate p38-଱ kinase activity....
02/24/2004
6680329N-(heterocyclyl)benzene or pyridinesulphonamides as antithrombotic agents and anticoagulants
Compounds of formula [I] ##STR1## in which: W may represent a --(CH2)2 --, --(CH2)3 --, --CH2 --C.ident.C-- or --CH2 --CH.dbd.CH-- group, R2 may in particular represent a pipe...
01/20/2004
6670379Piperidine compounds for use as ccr-3 inhibitors
##STR1## Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more halogen atoms, Ar2 is phenyl or naphthyl which is unsubstituted or substituted by one or more substituents selected from halogen, ...
12/30/2003
6667318LFA-1 antagonist compounds
The invention relates to novel compounds having formula (I) ##STR1## wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore ...
12/23/2003
6664273Piperidine based MCH antagonists for treatment of obesity and CNS disorders
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...
12/16/2003
6645980Heterocyclic analgesic compounds and methods of use thereof
One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-pro...
11/11/2003
6638950Piperidine amides as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): ##STR1## or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases....
10/28/2003
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