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Class 540/527 - Nitrogen bonded directly to the hetero ring


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds in which nitrogen is bonded directly to the hetero
No. of patents: 94
Last issue date: 08/30/2011


1      
NumberTitleIssue Date
8008479Organic compounds
A process for preparing compounds of formula (I) or a solvate or hydrate thereof, where R, R1, R2, R3 and R5 have the meanings as indicated in the specification. Such compounds are useful in the treatment of a number of co...
08/30/2011
7718796Process for the preparation of caprolactam CGRP antagonist
An efficient syntheses for the preparation of (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one. ...
05/18/2010
7378410Substituted lactams and their use as anti-cancer agents
This invention relates to certain substituted lactam compounds of the formula (I), particularly caprolactam compounds, which are useful for the treatment of cancer ...
05/27/2008
7348318α-Amino-N-(diaminophosphinyl)lactam derivatives
There are disclosed a novel α-amino-N-(diaminophosphinyl)lactam derivative represented by general formula (1): wherein, for example, A is a hydrogen atom or a substituent such as a lower alkyl group or the like; W, X, Y an...
03/25/2008
7342007Lactams and uses thereof
This invention relates to novel compounds having formula (I) to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit secretase and thereby inhibit the production of amyloid β protein, thereby acting to prevent the formation o...
03/11/2008
7294622Lactams and uses thereof
Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid β protein production and neurological disorders such as Alzheimer's disease. These compounds inhibit...
11/13/2007
7253158Sulfonamides
The invention relates to compounds of the general formula in which R1, R2, R3, R4, R2′, R3′, R4′, R5, and X is —CHR— are as defined in t...
08/07/2007
7208488N-substituted benzene sulfonamides
Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. In Formula (I), R1, R2, R3, R4, R
04/24/2007
7153846Bengamide derivatives, process for preparing them, and their use
The present invention relates to bengamide derivatives which are formed, during fermentation, by the microorganism Myxococcus virescens ST200611 (DSM 15898), to their use for treating cancer diseases, to pharmaceuticals which comprise bengamide derivatives, t...
12/26/2006
7118873Polynucleotides encoding cellular transporters and methods of use thereof
This disclosure encompasses the Indy gene, polypeptides encoded by the Indy gene and fragments thereof. This disclosure also encompasses homologs of the Indy gene both from Drosophila and other organisms. In addition, this disclosure encompasses the use of In...
10/10/2006
7001899Interleukin converting enzyme inhibitors
The present invention relates to novel compounds, compositions comprising said compounds, and uses thereof, said compounds having the formula: wherein each X is independently selected from: i) —C(W)2...
02/21/2006
6960576Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production
This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more spec...
11/01/2005
6958329Lactams substituted by cyclic succinates as inhibitors of A-β protein production
This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more spec...
10/25/2005
6953789Thiol compounds, their production and use
The present invention provides a compound represented by Formula: wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and the like, each R1
10/11/2005
69537883-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase
The present invention relates to certain novel 3-mercaptoacetylamino-1,5-substituted-2-oxo-azepan derivatives useful as inhibitors of matrix metalloproteinase. Pharmaceutical compositions containing said compounds as well as methods of treating various disease state...
10/11/2005
6906056Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release an...
06/14/2005
6900213Bisaryl derivatives having FSH modulatory activity
The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV ...
05/31/2005
6794381Succinoylamino lactams as inhibitors of aβ protein
This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-pe...
09/21/2004
6777550N-formyl hydroxylamine containing compounds useful as ACE inhibitors and/or NEP inhibitors
N-formyl hydroxylamines are provided which have the structure wherein R is H, alkyl, alkenyl, aryl-(CH2)p—, heteroaryl-(CH2)p— or cycloheteroalkyl-(CH2)p
08/17/2004
67706401-Carboxylmethyl-2-oxo-azepan derivatives useful as selective inhibitors of MMP-12
The present invention relates to certain novel 1-carboxymethyl-2-oxo-azepan derivatives of the formula useful as inhibitors of matrix metalloproteinases (MMPs). The compounds of formula (1) are especially useful as selec...
08/03/2004
6759404Cyclic malonamides as inhibitors of aβ protein production
Novel cyclic malonamides having the formula (I): and their pharmaceutical compositions. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-pept...
07/06/2004
6627629N-ureidoheterocycloalkyl-piperidines 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....
09/30/2003
6559141Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ଲ-amyloid peptide release and/or its synthesis by use of such compounds
Disclosed are compounds which inhibit ଲ-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ଲ-amyloid...
05/06/2003
6552041Cyclized amide derivatives
The present invention relates to cyclized amide derivatives of formula (I) ##STR1## These cyclized amide derivatives are useful for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comp...
04/22/2003
6544978Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ଲ-amyloid peptide release and/or its synthesis by use of such compounds
Disclosed are compounds which inhibit ଲ-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ଲ-amyloid...
04/08/2003
6544981Lactam inhibitors of factor Xa and method
Lactam inhibitors are provided which have the structure ##STR1## including pharmaceutically acceptable salts thereof and all stereoisomers thereof, and prodrug esters thereof, wherein n is 1 to 5; and and R1, R2, R3, R4
04/08/2003
6541466Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting ଲ-amyloid peptide release and/or its synthesis by use of such compounds
Disclosed are compounds which inhibit ଲ-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ଲ-amyloid...
04/01/2003
6534495Serine protease inhibitors
##STR1## The invention relates to a compound having the formula (I): R1 SO2 --B--X--Z--C(O)--Y, B is a bond, an amino acid of the formula --NR--CH[(CH2)p C(O)OH]--C(O)-- or an ester derivative thereof wherein p ...
03/18/2003
6511973Lactam inhibitors of FXa and method
Compound of the formula ##STR1## are inhibitors of the enzyme Factor Xa. These compounds are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses....
01/28/2003
6509330Hydroxamic acid containing compounds useful as ACE inhibitors and/or NEP inhibotors
Hydroxamic acids are provided which are ACE and/or NEP inhibitors and have the structure ##STR1## wherein R*, R and R1 are as defined herein and A is a dipeptide preferably derived from an amino acid, or is a conformationally restricted di...
01/21/2003
6503897Antibacterial agents
Compounds of formula (I) are antibacterial agents wherein: R3 and R4, taken together with the carbon atoms to which they are respectively attached, form an optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 ...
01/07/2003
6495540Lactams as inhibitors of A-ଲ protein production
This invention relates to novel lactams having the Formula (I): ##STR1## to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the produc...
12/17/2002
6486315Recrystallization processes
Mercaptoalkanoylamino lactam acids are recrystallized by treatment with an agent that minimizes the formation of disulfides. Suitable agents are bismercaptans, phosphine or phosphite reducing agents, zinc metal powder, and sodium hydrosulfite....
11/26/2002
6455521Condensed thiophene compounds and pharmaceutical use thereof
A condensed thiophene compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof and hydrates thereof. The compound of the formula (I) of the present invention is useful as a nov...
09/24/2002
6452001Diazapane derivatives useful as antagonists of neurokinin 1 receptor and methods for their formation
The invention relates to compounds of the formula ##STR1## wherein R1, R2 are independently from each other aryl or heteroaryl, wherein the heteroaryl group contains one or two heteroatoms, selected from N, O, or S, and wherein the a...
09/17/2002
6444810Deprotection processes
Acylmercaptoalkanoylamino lactam esters or acids are converted to the corresponding mercaptoalkanoylamino lactam ester or acid under basic conditions by including an agent which minimizes the amount of disulfides. Suitable agents are bismercaptans, phosph...
09/03/2002
6413954Certain substituted caprolactam carbonates and ethers, pharmaceutical compositions containing them and their use in treating tumors
The present invention relates to certain substituted caprolactam carbonate and ether compounds, pharmaceutical compositions containing said compounds, the use of said compounds in treating tumors and to a process for making said compounds....
07/02/2002
6344450Lactam compounds and their use as inhibitors of serine proteases and method
Lactam inhibitors are provided which have the structure ##STR1## X is ##STR2## wherein Y is O or S and R4 is ##STR3## R7 O-- or R8 and R1, R2, R3, R5, R6, R7
02/05/2002
6331640Diaminopropionic acid derivatives
A compound of formula 1a ##STR1## which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds....
12/18/2001
6326379Fused pyridine inhibitors of cGMP phosphodiesterase
Compounds of the formulas ##STR1## are useful as inhibitors of cGMP PDE, especially type V....
12/04/2001
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