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Class 540/491 - The chalcogen and the nitrogen are in the 1,5-positions of the bicyclo ring system (e.g., 1,5-benzothiazepinone, etc.)


Subclass of Class 540 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the chalcogen and the nitrogen are in
No. of patents: 144
Last issue date: 12/28/2010


1        
NumberTitleIssue Date
7858776Lactams 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 A...
12/28/2010
7425550Lactam glycogen phosphorylase inhibitors and method of use
A compound of formula I is provided having the structure wherein W is as defined herein; X is —CHR5O—; Y is a bond; Z is a...
09/16/2008
7390798Carboxamide spirolactam CGRP receptor antagonists
The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in...
06/24/2008
7361648Heterocyclylakylamines as muscarinic receptor antagonists
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR5, and the other substituents are as defined...
04/22/2008
7354914Lactams substituted by cyclic succinates 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 specifica...
04/08/2008
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
7211573Malonamide derivatives
The invention relates to compounds of the formula I wherein R, R1, R2, R3, X, and n are defined in the specification. Th...
05/01/2007
7169774Cephalotaxane derivatives and their processes of preparation and purification
The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constit...
01/30/2007
7141562Substituted benzoxazinones and uses thereof
Compound of the Formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is —SO2— or —(CRaRb)r—, n is 1 or 2, R...
11/28/2006
7101909Calcium channel drugs and uses
Novel multibinding compounds are disclosed. The compounds of this invention comprise 2–10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Ca++ channel, thereby modulating the biological activities...
09/05/2006
7011960Substituted 2-amino-3-(2-amino-phenylsulfanyl)-propionic acids
The present invention relates to a new process for the preparation compounds of formula I wherein R1, R2, R3 and n are as described in the description which process comprises reacting co...
03/14/2006
7001901Tetrazolylpropionamides as inhibitors of Aβ protein production
This invention relates to novel tetrazolyl-propionamides in which the amide group comprises an aminoazepinone, and related structures, of Formula (I): or pharmaceutically acceptable salt or prod...
02/21/2006
6924277Cyclized benzamide neurokinin antagonists for use in therapy
Compounds having the general formula wherein R1a, R1b, R1c, X1, X2, R2, R3, R4, R5, R6, n, Y and Z are as de...
08/02/2005
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
6897305Calcium channel drugs and uses
Novel multibinding compounds are disclosed. The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Ca++ channel , thereby modulating the biological activities ...
05/24/2005
6881839Process for preparing diltiazem using a heterogeneous trifunctional catalyst
The present invention comprises a simplified synthesis of (+)-diltiazem through IE-PdOsW wherein IE is ion-exchanger, catalyzed three-component coupling reaction and Fe3+-exchanged clay catalyzed ring opening of sulfite with 2-aminothiophenol followed by ...
04/19/2005
6864250N-acylated lipophilic amino acid derivatives
Compounds of structural Formula (I) where A is a lipophilic group including an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group and R is hydrogen, alkyl or cycloalkyl, and pharmaceutically acceptabl...
03/08/2005
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
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
6664249Bicyclic vasopressin agonists
Compounds according to general formula (1), and pharmaceutically acceptable salts thereof, wherein V is a covalent bond or NH, X is selected from CH2, O and N-alkyl, Z is either S or --CH.dbd.CH--, R1 and R2 are independen...
12/16/2003
6602865Pyridazino(4,5-b)(1,5)oxazepinone, -thiazepinone and -diazepinone compounds
Pyridazino(4,5-b)(1,5)oxazepinone, thiazepinone and diazepinone compounds of formula(I) ##STR1## and their tautomers and the acid-addition salts of all these compounds show memory-enhancing and neuroprotective properties....
08/05/2003
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
6455522Cyclic sulfonamide derivatives as metalloproteinase inhibitors
The present application describes novel lactams and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein rings ring B is a 4-8 membered cyclic sulfonamide containing from 0-3 additional heteroatoms sel...
09/24/2002
6258948Inhibitors of Interleukin-1ଲ converting enzyme
The present invention relates to novel classes of compounds which are inhibitors of interleukin-IB converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates t...
07/10/2001
6232308Bezazepine derivatives as ଱v integrin receptor antagonists
The present invention relates to benzazepine derivatives and their use as ଱v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors ଱v댣, ଱v댥, and/o...
05/15/2001
6197953Process for preparing optically active trans-3-substituted glycidic acid ester
Methods for the preparation of (2S,3S)-1,5-benzothiazepine derivatives of the formula (II) and isomers thereof, and for the preparation of (2R,3R)-1,5-benzothiazepine derivatives of the formula (III) and isomers thereof, ##STR1## wherein ring A and r...
03/06/2001
6187936Process for the enzymatic kinetic resolution of 3-phenylglycidates by transesterification with aminoalcohols
A process for the preparation of I: ##STR1## in which R and R1 have the meanings reported in the description, that comprises the enzymatic kinetic resolution by transesterification with aminoalcohols of 3-phenylglycidates of formula I: ##STR2## is de...
02/13/2001
6180785Process for preparing diltiazem
A process for preparing a 2R-hydroxy-3-[(2-amino-phenylthio)]-3-[(p-alkoxyaryl)] propanoic acid alkyl ester of formula (V) ##STR1## wherein R is an alkyl, or benzoyl residue, R1 is hydrogen, an alkyl, alkoxy, aryloxy, phenyl, naphthyl, or ...
01/30/2001
6114523Process for the recycle of a waste product of diltiazem synthesis
A process which allows the re-use of compounds of formula ##STR1## in diltiazem synthesis through a process of conversion to a mixture of enantiomers III-(2R,3R) and III-(2S,3S) is described....
09/05/2000
5998400Hypolipidemic benzothiazepines
The invention is concerned with novel hypolipidemic compounds of formula (I), with processes and novel intermediates for their preparation, pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and tre...
12/07/1999
5968924Benzo-fused lactams promote release of growth hormone
There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat pr...
10/19/1999
5945533Process for preparing optically active benzothiazepine compound and intermediate therefor
Powdery aggregate of 2-phenyl-1,5-benzothiazepin-3,4(2H,5H)-dione compound: ##STR1## wherein Ring A and Ring B are benzene ring having optionally substituent selected from lower alkyl, lower alkoxy and halogen, which is prepared by admixing solution ...
08/31/1999
5874424Inhibitors of interleukin-1ଲ converting enzyme
The present invention relates to novel classes of compounds which are inhibitors of interleukin-1ଲ converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also rel...
02/23/1999
5859239Mercaptoalkanoylamino and acylmercaptoalkanoylamino benzoxazepines and benzothiazepines
Compounds of the formula ##STR1## wherein X1 is ##STR2## are disclosed. These compounds possess inhibitory activity against angiotensin converting enzyme and neutral endopeptidase and thus useful as cardiovascular agents....
01/12/1999
5854233Method of treating liver disease and like indications with vasodilating agents
Liver diseases, such as cirrhosis of the liver, toxic and medicamentary liver damage, a liver-parenchymic disorder or hepatitis, are treated by administering to a human or animal subject in need thereof a therapeutically active or prophylactically effecti...
12/29/1998
5847122Process for preparing 1,5-benzothiazepine derivative
A novel process for preparing 1,5-benzothiazepine derivative ›II!: ##STR1## wherein Ring A and Ring B are substituted or unsubstituted benzene ring, and R3 is H, (di-lower alkylamino)-lower alkyl or substituted or unsubstituted piperaziny...
12/08/1998
5846967Natriuretic and anti-hypertensive compounds
A compound having the formula I ##STR1## in which R1, R2 independently are OH, OOC--R3 or O--R3, and R3 is an unsubstituted or substituted C1 -C6 alkyl, alkenyl, alkynyl or ...
12/08/1998
5817602Herbicidal thiadiazabicyclodecanes
Thiadiazabicyclodecanes of formula (I) wherein, Z is oxygen or sulfur; R is an optional substituent and W is an optionally condensed or substituted phenyl radical and the salts, complexes and stereisomers thereof, have good selective pre- and post-emergen...
10/06/1998
5726307Benzo-fused lactams promote release of growth hormone
There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat pr...
03/10/1998
5723458Hypolipidaemic compounds
The invention provides novel 1,4-benzothiazepine compounds substituted with hydroxy or a group containing hydroxy, compositions comprising such compounds and their use in the treatment or prophylaxis of treating clinical conditions in which inhibition of ...
03/03/1998
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