Abstract: A tetralylmethylene-2-oxindole derivative having the following formula (I) ##STR1## wherein one or two of R, R.sub.1, R.sub.2 and R.sub.3 the said two being the same or different, are selected from:a) --X--(CH.sub.2).sub.m --NH.sub.2, --X--(CH.sub.2).sub.m --NR.sub.4 R.sub.5 or --X--(CH.sub.2).sub.m --NHR.sub.6, in which X is --O--, --S-- or --NH--, m is an integer of 2 to 4, one of R.sub.4 and R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl and the other is C.sub.1 -C.sub.6 alkyl or R.sub.4 and R.sub.5 taken together with the N atom to which they are linked form a 5 to 7 membered saturated heteromonocycle, and R.sub.6 is C.sub.2 -C.sub.6 alkanoyl or a C-terminally linked peptidyl residue containing from 1 to 3 aminoacids wherein the terminal amino group is either free or protected or in an alkylated form to provide a --NR.sub.4 R.sub.5 group in which R.sub.4 and R.sub.5 are as defined above.
Abstract: The invention provides a pharmaceutical composition comprising a particular physical form of N-[4-[5-(cyclopentyloxy-carbonyl)amino-1-methylindol-3-yl-methyl]-3-methox ybenzoyl]-2-methyl-benzenesulphonamide and polyvinylpyrrolidone. It also provides methods for preparing this physical form, and another physical form of N-[4-[5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-yl-methyl]-3-methoxy benzoyl]-2-methylbenzenesulphonamide useful in the preparation of the first mentioned physical form. The compositions are useful in the treatment of diseases in which leukotrienes are implicated, for example asthma.
Type:
Grant
Filed:
November 23, 1999
Date of Patent:
November 7, 2000
Assignee:
Zeneca Limited
Inventors:
James Joseph Holohan, Ieuan John Edwards
Abstract: The present invention provides novel iodopropargyl derivatives represented by the following formula (1): ##STR1## wherein R.sup.1 is a methoxy group or a cyano group, which have a reduced unpleasant smell and also have a wide antimicrobial spectrum and a high antimicrobial activity. Also, the present invention provides antimicrobial, antifungal and preservative or antimold agents comprising the above derivatives as an active ingredient.
Abstract: Organometallic compounds useful for forming aluminum films by chemical vapor deposition are disclosed. Also disclosed are methods of preparing the organimetallic compounds and methods of forming aluminum films.
Abstract: The invention relates to derivatives of general formula I ##STR1## as defined in the description. The invention also relates to a process for their preparation and to their therapeutic use, in particular for the treatment of complaints associated with melatonin disorders, and pharmaceutical and cosmetic compositions comprising them.
Type:
Grant
Filed:
April 16, 1999
Date of Patent:
October 31, 2000
Assignee:
Cemaf and Laboratories Besins Isovesco S.A.
Inventors:
Jean-Bernard Fourtillan, Marianne Fourtillan, Jean-Claude Jacquesy, Marie-Paule Jouannetaud, Bruno Violeau, Omar Karam
Abstract: .beta.-Aminotetralin derivatives of the formula: ##STR1## which are ligands for the neuropeptide Y Y5 (NPY5) receptor, methods of preparation and pharmaceutical compositions containing a .beta.-aminotetralin derivative as the active ingredient are described. The .beta.-aminotetralins are useful in the treatment of disorders and diseases associated with NPY receptor subtype Y5.
Type:
Grant
Filed:
April 12, 1999
Date of Patent:
October 31, 2000
Assignee:
Ortho-McNeil Pharmaceutical, Inc.
Inventors:
Scott L. Dax, Timothy W. Lovenberg, James McNally, Allen B. Reitz, Mark A. Youngman
Abstract: The present invention provides novel compounds such as certain aryloxy indanamines which are useful as anti-depressants and as inhibitors of synaptic norepinephrine and serotonin uptake. The present invention also provides an improvement in the treatment of depression which comprises inhibiting synaptic serotonin and epinepherine uptake.
Abstract: Biologically-active, water soluble, 3-substituted trioxanes of the formula ##STR1## wherein R represents a COOH-- substituted aryl group, a substituted or unsubstituted heteroaryl group or an alkyl group, and C.sub.12 -(p-carboxy)benzyloxy trioxanes of formula ##STR2## wherein R represents a substituted or unsubstituted alkyl, alkenyl, aryl or heteroaryl group and methods for their use as antiparasitic agents, particularly for the treatment of malaria.
Type:
Grant
Filed:
April 7, 1999
Date of Patent:
October 24, 2000
Assignee:
Johns Hopkins University
Inventors:
Gary H. Posner, Michael H. Parker, Mikhail Krasavin, Theresa A. Shapiro
Abstract: A tetrazole derivative of formula (I) ##STR1## wherein R is H, alkyl, alkoxy, carbocyclic ring, alkyl or alkoxy substituted by carbocyclic ring;AA.sup.1 and AA.sup.2 is a bond or ##STR2## and ##STR3## respectively, or AA.sup.1 and AA.sup.2, together, may have the formula (a); ##STR4## and Y is formula (b) ##STR5## wherein the Tet ring is tetrazole; Z is alkylene, alkenylene, O, S, SO, SO.sub.2, NR.sup.26, methylene in alkylene replaced by O, S, --SO--, --SO.sub.2 -- or --NR.sup.26 --; and E is H, alkyl, or COOR.sup.27.
Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-.beta.-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-.beta.-lactones, and analogs thereof and their use as proteosome inhibitors.
Type:
Grant
Filed:
August 14, 1998
Date of Patent:
October 17, 2000
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Fran.cedilla.ois Soucy, Louis Plamondon, Mark Behnke, William Roush
Abstract: This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors.
Type:
Grant
Filed:
October 28, 1999
Date of Patent:
October 17, 2000
Assignee:
Eli Lilly and Company
Inventors:
Jefferson Ray McCowan, John Eldon Toth, Daniel Jon Sall
Abstract: A process for preparing a compound of the formula ##STR1## wherein R is C.sub.1 -C.sub.18 alkyl by reacting a compound of the formulaRO.sub.2 C--CH.sub.2 CN (II)with a cyanide salt and formaldehyde or source thereof. Compounds of formula (I) are useful intermediates to pesticidally active compounds.
Type:
Grant
Filed:
December 1, 1998
Date of Patent:
October 17, 2000
Assignee:
Rhone-Poulenc Agro
Inventors:
David William Hawkins, David Alan Roberts, John Harry Wilkinson, Jean-Louis Clavel
Abstract: There is provided a process for the preparation of 2-aryl-5-(perfluoroalkyl)pyrrole compounds from N-(arylmethylene)-1-chloro-1-(perfluoroalkyl)methylamine compounds. The 2-aryl-5-(perfluoroalkyl)pyrrole compounds are useful for the control of insect and acarid pests, and may also be used to prepare other pesticidal arylpyrrole compounds.In addition, the present invention provides N-(arylmethylene)-1-chloro-1-(perfluoroalkyl)methylamine compounds which are useful as intermediates in the preparation of arylpyrrole compounds.
Abstract: A method for producing pyrrolidine derivatives such as 3,4-epoxypyrrolodines, 3-pyrrolidols and the like, by oxidizing 3-pyrrolines with at least one peroxide in the presence of at least one acid is disclosed. The 3-pyrrolines are produced by deriving cis-2-butene compounds from cis-2-butene-1,4-diols and performing a cyclization between the cis-2-butene derivatives and at least one primary amine. The method may be performed as a one-pot synthesis and may be performed as a continuous reaction.
Abstract: The present invention relates to a process for stereoselective cycloaddition reactions which generally comprises a cycloaddition reaction between a pair of chiral or prochiral substrates that contain reactive .pi.-systems, in the present of a non-racemic chiral catalyst, to produce a stereoisomerically enriched product.
Type:
Grant
Filed:
January 13, 1998
Date of Patent:
October 10, 2000
Assignee:
President and Fellows of Harvard College
Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.
Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.
Type:
Grant
Filed:
August 9, 1999
Date of Patent:
October 3, 2000
Assignees:
Scriptgen Pharmaceuticals, Inc., Trustees of Boston University
Inventors:
Mark A. Wuonola, Gary R. Gustafson, James S. Panek, Tao Hu, Jennifer V. Schaus