"It is my heart-warmed and world-embracing Christmas hope and aspiration that all of us, the high, the low, the rich, the poor, the admired, the despised, the loved, the hated, the civilized, the savage (every man and brother of us all throughout the whole earth), may eventually be gathered together in a heaven of everlasting rest and peace and bliss, except the inventor of the telephone. "
Mark Twain ; Christmas greetings, 1890
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| Number | Title | Issue Date |
| 7858776 | Lactams 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 |
| 7425550 | Lactam 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 |
| 7390798 | Carboxamide 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 |
| 7361648 | Heterocyclylakylamines 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 |
| 7354914 | Lactams 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 |
| 7294622 | Lactams 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 |
| 7211573 | Malonamide 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 |
| 7169774 | Cephalotaxane 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 |
| 7141562 | Substituted 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 |
| 7101909 | Calcium 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 |
| 7011960 | Substituted 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 |
| 7001901 | Tetrazolylpropionamides 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 |
| 6924277 | Cyclized 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 |
| 6906056 | Cycloalkyl, 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 |
| 6897305 | Calcium 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 |
| 6881839 | Process 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 |
| 6864250 | N-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 |
| 6777550 | N-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 |
| 6759404 | Cyclic 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 |
| 6664249 | Bicyclic 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 |
| 6602865 | Pyridazino(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 |
| 6503897 | Antibacterial 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 |
| 6455522 | Cyclic 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 |
| 6258948 | Inhibitors 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 |
| 6232308 | Bezazepine 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 |
| 6197953 | Process 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 |
| 6187936 | Process 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 |
| 6180785 | Process 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 |
| 6114523 | Process 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 |
| 5998400 | Hypolipidemic 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 |
| 5968924 | Benzo-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 |
| 5945533 | Process 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 |
| 5874424 | Inhibitors 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 |
| 5859239 | Mercaptoalkanoylamino 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 |
| 5854233 | Method 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 |
| 5847122 | Process 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 |
| 5846967 | Natriuretic 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 |
| 5817602 | Herbicidal 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 |
| 5726307 | Benzo-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 |
| 5723458 | Hypolipidaemic 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 |