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Class 546/229 - Nitrogen attached indirectly to the piperidine ring by nonionic bonding


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which nitrogen is attached indirectly to the
No. of patents: 263
Last issue date: 11/16/2010


1              
NumberTitleIssue Date
7834185Quaternary ammonium diphenylmethyl compounds useful as muscarinic receptor antagonists
The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarin...
11/16/2010
7786307Amino alcohol derivatives and their activity as renin inhibitors
The application relates to novel amino alcohols of general formula (I) where R, R1, R2, R3, R4, R5, X1 and X2 each have the definitions illustrated in detail in the description, to a proces...
08/31/2010
7728145Industrial method for separation and purification of fentanyl by reverse phase preparative chromatography
There is described a process for the purification of an impure preparation containing fentanyl by means of a reverse phase preparative chromatography process. A chromatographic column is loaded with a stationary phase, typically a silica particle having an organic l...
06/01/2010
7482462Acylsulfonamides as inhibitors of steroid sulfatase
A compound of formula wherein R1 is haloalkyl, alkenyl, phenyl, thienyl, pyridine, benzthiazolyl, chromanyl (1,2-dihydrobenzopyranyl) or (C6-18)aryl, and R1 or R2 independently of...
01/27/2009
7435747Guanidine and amidine derivatives as factor Xa inhibitors
The present invention relates to compounds of the formula I, in which R0; Q; X; Q′, D, R10 and V have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacological...
10/14/2008
7405298Process for making risperidone and intermediates therefor
The formation of risperidone is enhanced by the use of enriched Z-isomer oxime intermediate(s) of formula (3) or (7). The oxime(s) can be isomerically enriched by a variety of techniques including the use of the novel aceti...
07/29/2008
7393849Substituted sulfonamides and ureas useful for inhibiting kinase activity
Sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formul...
07/01/2008
73684432,6-disubstituted piperidines and piperazine compounds
The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula: which are used to treat diseases of the central nervous system, drug abuse, and withdrawal there...
05/06/2008
7365082N-(substituted arylmethyl)-4-(disubstituted methyl)piperidines and piperazines
It has now been found that certain novel N-(substituted aryl)-4-(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): wherein m, n, q, r, and s are independently sele...
04/29/2008
7348341Chemical compounds
The invention concerns compounds of formula (I), and their use in therapy, particularly in the modulation of CCR3 activity. ...
03/25/2008
7300946N-(substituted arylmethyl)-4-(disubstituted methyl) piperidines and pyridines
It has now been found that certain novel N-(substituted aryl)-4(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): wherein m, n, q, r, and s are independently selec...
11/27/2007
7294637Method of treating addiction or dependence using a ligand for a monamine receptor or transporter
One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substitute...
11/13/2007
7276612Hydroxamates as therapeutic agents
The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase...
10/02/2007
7276511Benzylamine derivative
The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor. The compound is a benzylamine derivative represented by formula (1) or a salt thereof
10/02/2007
7265133Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 are as d...
09/04/2007
72652261-alkyl-4-(3-substitutedphenyl)piperidines
8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful ...
09/04/2007
7259157N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain. ...
08/21/2007
7223763Substituted sulfonamides and ureas useful for inhibiting kinase activity
Sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formul...
05/29/2007
7214831Histone deacetylase inhibitors based on alpha-chalcogenmethylcarbonyl compounds
Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-chalcogenmethylcarbonyl group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can re...
05/08/2007
7214824Substituted -sulfonylaminobenzyl-2-phenoxyacetamide compounds as VR1 receptor agonists
This invention provides a compound of the formula (I): wherein R1 represents a (C1–C6)alkyl group; R2 represents a hydrogen atom, a halogen atom, a hydroxy group, a (...
05/08/2007
RE395585-Substituted-6-cyclic-5,6,7,8-tetrahydronaphthalen 2-ol compounds which are useful for treating osteoporosis
Compounds of this formula are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease. ...
04/10/2007
7183279Histogranin-like peptides and non-peptides, processes for their preparation and uses thereof
The invention relates to new basic amino acid derivatives of general formulae I, II and III, and the preparation and use thereof in treatment of pain. The compounds have histogranin-like antinociceptive, morphine potentiating and COX-2 induction modulating activitie...
02/27/2007
7135483Substituted heterocyclic compounds for treating multidrug resistance
Substituted heterocyclinc compounds are disclosed. The compounds are useful for treating multidrug resistance. The compounds can be formulated in compositions with a carrier and, optionally, a therapeutic agent. One suitable substituted heterocyclic compound has the...
11/14/2006
7122677NK1 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 and R5...
10/17/2006
7115632Sulfonyl aryl or heteroaryl hydroxamic acid compounds
A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid ...
10/03/2006
7109342Piperidine derivatives and agent comprising the derivative as active ingredient
Piperidine derivatives represented by formula (I) or nontoxic salts thereof (wherein symbols are defined in the description): Since the compound represented by formula (I) has a PDE4 inhibitory activity, it is usef...
09/19/2006
7078537Phenylalkyl diamine and amide analogs
The present invention relates to novel 1,2- or 1,3-diamine and amide compounds and pharmaceutically useful salts thereof and methods for treating central nervous system diseases. The present 1,2- or 1,3-diamine and amide compounds have high binding affinity to the s...
07/18/2006
7074786Histogranin-like peptides, processes for their preparation and uses thereof
The invention relates to new basic amino acid derivatives of general formulae I, II and III, and the preparation and use thereof in treatment of pain. The compounds have histogranin-like antinociceptive, morphine potentiating and COX-2 induction modulating activitie...
07/11/2006
7074820Amidino derivatives and their use as thrombin inhibitors
There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like protease...
07/11/2006
7070630Primary intermediates for oxidative coloration of hair
Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein R1 and R2 are each independently selected from hydrogen atoms, a C1...
07/04/2006
70675355-Phenylbenzylamine compounds, process for their production and intermediates for their synthesis
The present invention relates to a 5-phenylbenzylamine compound represented by the formula [1]: wherein Ring A represents a phenyl group having a substituent(s), Ra
06/27/2006
7053078Serine 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 cardi...
05/30/2006
7049327Substituted dimethyl-[1-(1-phenyl-cyclohexyl)-piperidin-3-ylmethyl]-amines and the use of the same as analgesics
A variety of dimethyl-[1-(1-phenyl-cyclohexyl)-piperidin-3-ylmethyl]-amines are disclosed, along with processes for their preparation, medicaments containing those compounds, and methods for the use of those substances in the preparation of medicaments. ...
05/23/2006
7049330Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents
This invention relates to compounds which have activity as 5-HT1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer, having the formula
05/23/2006
7041830Process for preparing (RS) 3-methyl-1-(2-piperidinyl phenyl) butyl amine
The Present invention relates to a process for the preparation of (RS) 3-methyl-1-(2-piperidinyl phenyl) butyl amine of formula 1. (RS) 3-Methyl-1-(2-piperidinyl phenyl butyl amine having formula 1 is an important ...
05/09/2006
70190332-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives
Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrog...
03/28/2006
7005439Compounds
The invention provides compounds of general formula (I) wherein m, n, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, process...
02/28/2006
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
6979691Compounds useful as modulators of melanocortin receptors and pharmaceutical compositions comprising same
Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates and prodrugs thereof, in which E is X is N or CH, W is —NR16R17, —NR16C(═O)R22
12/27/2005
6979690Oxo or oxy-pyridine compounds as 5-HT4 receptor modulators
This invention provides compounds of the formula (I) and (II): or the pharmaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein R1 is hydrogen or halo; R2
12/27/2005
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