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Class 546/216 - Chalcogen bonded directly to ring carbon of the piperidine ring


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which chalcogen (i.e., oxygen, sulfur, selenium,
No. of applications: 134
Last issue date: 05/24/2012


1        
Application No.Application TitleIssue Date
20120129888LIBRARIES OF N-(2-OXO-1-PHENYLPIPERIDIN-3-YL)SULFONAMIDES FOR DRUG DISCOVERY
Novel compounds are continually sought after to treat and prevent disorders. The invention relates to N-(2-oxo-1-phenylpiperidin-3-yl)sulfonamides useful for contributing to the search and identification of new lead compounds which can modulate the functional activity o...
05/24/2012
20120108814PROCESS 738
Processes for the preparation of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-{[1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy}quinazoline, salts thereof, and the intermediates used in the process are described....
05/03/2012
201200462471,5-DIPHENYL-PENTA-1,4-DIEN-3-ONE COMPOUNDS
This invention relates to compounds of Formula (I), (II), or (III) as shown in the specification, which contain a 1,5-diphenylpenta-1,4-dien-3-one backbone. These compounds can be used to treat cancer, inflammatory disease, or autoimmune disease....
02/23/2012
20120004310NON-PEPTIDE BDNF NEUROTROPHIN MIMETICS
Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule....
01/05/2012
20110319378PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER
The present invention provides MDM2 inhibitor compounds of Formula I,

    • wherein the variab...
12/29/2011
20110301200THYROID RECEPTOR LIGANDS
The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta (TR-Beta). Further, the present invention relates to processes of preparing such compounds, thei...
12/08/2011
20110207709MODULATORS OF SEROTONIN RECEPTOR
Certain biphenyl compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases....
08/25/2011
20110207714SEROTONIN RECEPTOR MODULATORS
The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases.

...

08/25/2011
20110172431PROCESS FOR PRODUCING 1-SUBSTITUTED TRANS-4-(SUBSTITUTED AMINO) PIPERIDIN-3-OL
A process is provided for producing a 1-substituted trans-4-(substituted amino)piperidin-3-ol represented by formula (III-1):

The process includes a step of reacting a 1-substituted-3,4-epoxypiperidine repres...

07/14/2011
20110172297Oxopiperdinyl And Pyranyl Sulfonamides and Pharmaceutical Compositions Thereof
The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of Formula (I): as defined in the specification. The invention is also directed to compositions containing the compounds of Formula ...
07/14/2011
20110105562ALKYNYL DERIVATIVES USEFUL AS DPP-1 INHIBITORS
The present invention is directed to novel alkynyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1....
05/05/2011
20110098468NK1 ANTAGONISTS
A NK1 antagonist having the formula (I),

wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 a...

04/28/2011
20110098320Lactam Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1
This invention relates to novel compounds of the Formula (I), (I*), (Ia), (Ib), (Ic), (Id), (Ie), (If), (If*), (Ig), (Ih), (Ij), (Ik), (ll1-3), (Im1-3), (In1-3), (lo1-2), (Ip1-9), (Iq1-9), (Ir1-9) and (Is1-3) pharmaceutically acceptable salts thereof, and pharmaceutical...
04/28/2011
20110071139Cycloalkyl Lactame Derivatives As Inhibitors Of 11-Beta-Hydroxysteroid Dehydrogenase 1
This invention relates to novel compounds of the Formula (I), any of the formulas I1-I26 Ia1-3-Ij1-3 or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic t...
03/24/2011
20110053984NOVEL 4-BENZHYDRYLOXY-TETRAALKYL-PIPERIDINE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS
This invention relates to novel 4-benzhydryloxy-tetraalkyl-piperidine derivatives of Formula (I), any of its stereoisomers or any mixture of its stereoisomers, or an N-oxide thereof, or a pharmaceutically acceptable salt thereof, wherein Ra represents hydroge...
03/03/2011
20110009622LONG-CHAIN FATTY ACYL ELONGASE INHIBITOR COMPRISING ARYLSULFONYL DERIVATIVE AS ACTIVE INGREDIENT
[Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides.

01/13/2011

20100267945AMINE DERIVATIVE HAVING NPY Y5 RECEPTOR ANTAGONISTIC ACTIVITY
A compound of the formula (I):

a pharmaceutically acceptable salt or solvate thereof, where R1 is optionally substituted lower alkyl, Y is —S(O)2—, R2 is hydrogen or optio...

10/21/2010
20100168167Piperidinones Useful in the Treatment of Inflammation
There is provided compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, m and n have meanings given in the description, and pharmaceutically acceptable derivatives thereof, which compou...
07/01/2010
20100076190METHOD FOR SYNTHESIS OF NITROXYL RADICAL
The problem to be solved by the present invention is to provide a highly-versatile method for producing a nitroxyl radical derivative, in which position-2 and position-6 in a TEMPO-based compound can be easily substituted, and further, a method for producing a nitroxyl ...
03/25/2010
20100048550SELECTIVE TR-BETA 1 AGONIST
The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta(TR-Beta). Further, the present invention relates to processes of preparing such compounds, their...
02/25/2010
20100035865Sulfonamides and Pharmaceutical Compositions Thereof
The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula (I), as defined in the specification. The invention is also directed to compositions containing the compounds of formula ...
02/11/2010
20100035879N-SULFONYLCARBOXIMIDAMIDE 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....

02/11/2010
20100029720Carboxamide Derivatives As Muscarinic Receptor Antagonists
The invention relates to compounds of formula

processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them....

02/04/2010
20090239829THIOARYL SUBSTITUTED INHIBITORS OF ZINC PROTEASES AND THEIR USE
There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibitors of zinc me...
09/24/2009
20090233969BIARYL SUBSTITUTED NITROGEN CONTAINING HETEROCYCLE INHIBITORS OF LTA4H FOR TREATING INFLAMMATION
The present invention relates to a chemical genus of biaryl substituted nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula:

They are...

09/17/2009
20090215821N-Substituted Azacycles
N-substituted azacycle derivative compounds represented by formula (I):

wherein m, q, r, t and u are independently selected from 0 or 1; and p is 0, 1, 2, or 3; and A, B, D, X, Y, R, R1, R2

08/27/2009
20090198052METHOD FOR PREPARING OPTICALLY ACTIVE PIPERIDINE COMPOUNDS
The present invention relates to a method for preparing a syn-form piperidine compound represented by general formula [I]:

wherein,

  • ...
08/06/2009
20090176767BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
This invention provides compounds of formula I:

wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the sp...

07/09/2009
200901565891,2-DI(CYCLIC GROUP)SUBSTITUTED BENZENE DERIVATIVE
A compound represented by the following general formula (1) or (100), a salt thereof or a hydrate of the foregoing has excellent cell adhesion inhibitory action and cell infiltration inhibitory action.

wherei...

06/18/2009
20090137813PROCESS FOR PRODUCTION OF CAREBASTINE
Processes are disclosed for preparing piperidine derivative compounds of the formulae I, II or III:

...

05/28/2009
20090093451IL-8 Receptor Antagonists
This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8)....
04/09/2009
20090076026BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS
The invention provides compounds of formula I:

wherein a, b, c, d, f, W, Q, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic re...

03/19/2009
20090062344THERAPEUTIC SUBSTITUTED PIPERIDONE COMPOUNDS
Compounds comprising

or a pharmaceutically acceptable salt or a prodrug thereof are disclosed herein. Details are provided herein. Compositions, methods, and medicaments related thereto are also disclosed....

03/05/2009
20090012055Organic compounds
Novel substituted piperidines of the general formulae (I) and (II)

with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin i...

01/08/2009
20080318907Nitroxide Free Radical Synergized Antineoplastic Agents
Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives...
12/25/2008
20080269275Novel Mchr1 Antagonists and Their Use for the Treatment of Mchr1 Mediated Conditions and Disorders
Compounds of Formula I

wherein R1, D, R2, A and R3 are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions con...

10/30/2008
20080182991N- AND O-SUBSTITUED 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 SERT ...
07/31/2008
20080166332Methods of Treatment of Amyloidosis Using Subsituted Ethanolcyclicamine Aspartyl Protease Inhibitors
The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein...
07/10/2008
20080161354STABLE S-NITROSOTHIOLS, METHOD OF SYNTHESIS AND USE
The present invention relates to stable S-nitrosothiols derivatives of formula (I)

having vasodilating effect and which inhibit the aggregation of the platelets and which therefore are useful for the preparat...

07/03/2008
20080146588Piperidinyl Piperidine Tachykinin Receptor Antagonists
The present invention is directed to certain piperidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these ...
06/19/2008
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