Abstract: A new process for the preparation of corroles, having the structure of formula I below relies on a solvent-free condensation of an aldehyde with a pyrrole. Further disclosed are several new corroles, salts, optically active isomers and complexes thereof synthesized using the process.
Type:
Grant
Filed:
June 19, 2001
Date of Patent:
April 1, 2003
Assignees:
Technion Research and Development Foundation Ltd.
Abstract: The present invention relates to an uracil compound of the formula [I]:
[wherein, Q—R3 represents a R3-substituted group of a 5-membered or 6-membered heterocyclic ring having one or two nitrogen selected from the group consisting of moieties represented in the specification (wherein, this heterocyclic ring may be substituted with at least one kind of substituent, Y represents oxygen, sulfur, imino or C1 to C3 alkylimino, R1 represents C1 to C3 alkyl or C1 to C3 haloalkyl, R2 represents C1 to C3 alkyl, R3 represents carboxy C1 to C6 alkyl, C1 to C6 alkoxycarbonyl C1 to C6 alkyl, OR7, SR8, N(R9)R10 or the like, X1 represents halogen, cyano, thiocarbamoyl or nitro, X2 represents hydrogen or halogen. {wherein, each of R7, R8 and R10 independently represents carboxy C1 to C6 alkyl, C1 to C6 alkoxycarbonyl C1 to C6 alkyl, C1 to C6 haloalkoxycarbonyl C1 to C6 alkyl, or the like, and R9 represents hydrogen or C1 to C6 alkyl.}.].
Abstract: A method is provided for treating or preventing a disorder or condition selected from hypertension, depression, generalized anxiety disorder, phobias, posttraumatic stress syndrome, avoidant personality disorder, premature ejaculation, eating disorders, obesity, cluster headache, migraine, pain, obsessive-compulsive disorder, panic disorder, endocrine disorders, vasospasm, cerebellar ataxia, gastrointestinal tract disorders, premenstrual syndrome, fibromyalgia syndrome, stress incontinence, chronic paroxysmal hemicrania and headache in a mammal, comprising administering to a mammal in need of such treatment or prevention an amount of a compound of the formula (I)
or the pharmaceutically acceptable salt thereof; wherein X, Y, Z, R2 and R3 are as defined herein.
Abstract: Compounds of formula (I)
are useful in treating diseases prevented by or ameliorated with potassium channel openers. Also disclosed are potassium channel opening compositions and a method of opening potassium channels in a mammal.
Type:
Grant
Filed:
November 10, 2000
Date of Patent:
March 25, 2003
Assignee:
Abbott Laboratories
Inventors:
Mark W. Holladay, William A. Carroll, Irene Drizin, Lin Yi, Henry Q. Zhang
Abstract: The invention relates to a novel, heretofore unknown polymorphous modification of 5-fluoro-1-(tetrahydro-2-furyl)uracil (tegafur) having antineoplastic activity. This form is crystalline, and its characteristics it differs essentially from the modification known earlier. In particular, it has an enhanced specific activity. The new form is physically stable and may find application in medicine for treating oncological patients. New anticancer medicinal substances prepared in the form of stable molecular complexes on the basis of said new modification, in particular, crystalline complexes with 6-methyluracil, and amorphous complexes with the biologically active substances from licorice, are also described.
Abstract: Novel uracil substituted phenyl sulfamoyl carboxamides I
and salts thereof, where
A=oxygen or sulfur;
X1=H, halogen, C1-C4-alkyl;
X2=H, CN, CS—NH2, halogen, C1-C4-alkyl, C1-C4-haloalkyl;
X3=H, CN, C1-C6-alkyl, C1-C6-alkoxyalkyl, C3-C7-cycloalkyl, C3-C6-alkenyl, C3-C6-alkynyl, optionally substituted benzyl;
R1, R2=H, halogen, optionally substituted hydroxy, C1-C10-alkyl, C2-C10-alkenyl, C3-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl or C5-C7-cycloalkenyl,
or R1+R2 together with the atom to which they are attached form 3- to 7-membered heterocyclic ring;
Q is selected from Q1 to Q40 as defined in the description.
Use: As herbicides; for the desiccation/defoliation of plants.
Type:
Grant
Filed:
May 4, 2001
Date of Patent:
March 18, 2003
Assignee:
BASF Aktiengesellschaft
Inventors:
Marianne Carlsen, Michael Anthony Guaciaro, James Jan Takasugi
Abstract: This invention relates to compounds of Formula V
H—Y—G—R V
and Formula VI
(wherein f, X, Y, G and R have the values defined in the description) which are useful as intermediates for the preparation of compounds, or pharmaceutically acceptable salts thereof, which are useful as thrombin inhibitors, coagulation inhibitors and agents for the treatment of thromboembolic disorders.
Type:
Grant
Filed:
March 9, 2001
Date of Patent:
March 18, 2003
Assignee:
Eli Lilly and Company
Inventors:
Valentine J Klimkowski, Aaron L Schacht, Michael R Wiley
Abstract: The invention relates to novel compounds of formula I:
wherein E, A, X1, X2, X3, Z, m, x and y have the meaning given in claim 1, and the agronomically acceptable salts or N-oxides thereof, and to herbicidal compositions containing such compounds as active ingredients.
Type:
Grant
Filed:
November 8, 2000
Date of Patent:
March 18, 2003
Assignee:
BASF Aktiengesellschaft
Inventors:
Stefan Scheiblich, Thomas Maier, Helmut Baltruschat
Abstract: The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula I
wherein
X is N or CH;
Y is NR2CH2, CH2—NR2, NR2—CO, CO—NR2 or NR2SO2 wherein R2 is H or C1-C6 alkyl;
R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl;
R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted
n is 0-4;
R9 is C1-C6 alkyl, C3-C6 cycloalkyl OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above,
as (R)- enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salts
Type:
Grant
Filed:
July 10, 2001
Date of Patent:
March 18, 2003
Assignee:
AstraZeneca AB
Inventors:
Stefan Berg, Svante Ross, Seth-Olov Thorberg
Abstract: The present invention relates to compounds of the general formula (I)
The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).
Type:
Grant
Filed:
June 11, 2001
Date of Patent:
March 18, 2003
Assignee:
Novo Nordisk A/S
Inventors:
Lone Jeppesen, Per Sauerberg, Anthony Murray, Paul Stanley Bury
Abstract: There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.
Abstract: The invention provides a novel class of substituted isoindolinone derivatives, useful for the treatment of inflammation and reperfusion injuries. Pharmaceutical compositions, and methods of making and using the compounds, or pharmaceutically acceptable salts, hydrates, stereoisomers or mixtures thereof are also described. The novel isoindolinone derivatives have the formula:
or a pharmaceutically acceptable base or acid addition salt, hydrate, stereoisomer, or mixtures thereof, wherein R14 is described herein.
Type:
Grant
Filed:
January 19, 2001
Date of Patent:
March 18, 2003
Assignee:
Inotek Pharmaceuticals Corp.
Inventors:
Prakash Jagtap, Garry Southan, Andrew Salzman, Csaba Szabo, Siya Ram
Abstract: A process is described for the manufacture of a pyridinesulfonyl chloride or a benzenesulfonyl chloride in which the benzene ring bears one or more electron-withdrawing groups, the process comprising reacting a diazonium salt of an aminopyridine or aminobenzene in which the benzene ring bears one or more electron withdrawing groups with a mixture of thionyl chloride in water, in the presence of an electron transfer catalyst.
Abstract: Compounds are described comprising purines substituted at the C-8 position and pyrimidines substituted at the C-4 position with a linker and quencher. These compounds, when incorporated into hairpin oligonucleotides quench the fluorescence of fluorophores linked to the 5′-terminus of the oligonucleotide. These nucleotide-quencher compounds are also easily incorporated into oligonucleotides using conventional or automated oligonucleotide synthetic techniques.
Type:
Grant
Filed:
October 26, 2000
Date of Patent:
March 11, 2003
Assignee:
Serologicals, Inc.
Inventors:
Glenn Nardone, Irena Nazarenko, Jila Boal
Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.
Type:
Grant
Filed:
September 29, 2000
Date of Patent:
March 4, 2003
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Michael R. Myers, Wei He, Alfred P. Spada, Martin P. Maguire
Abstract: Compounds and compositions are provided which are useful for the treatment of viral infections, particularly human Cytomegalovirus infection. The compounds include novel pyrimidine-based derivatives.
Type:
Grant
Filed:
December 15, 2000
Date of Patent:
March 4, 2003
Assignee:
Tularik INC
Inventors:
Timothy D. Cushing, Heather L. Mellon, Juan C. Jaen, John A. Flygare, Shi-Chang Miao, Xiaoqi Chen, Jay P. Powers
Abstract: The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.
Type:
Grant
Filed:
September 15, 2000
Date of Patent:
March 4, 2003
Assignee:
Georgetown University
Inventors:
Alan P. Kozikowski, Jarda T. Wroblewski, Fajun Nan
Abstract: Disclosed is a process for selectively producing aliphatic cyclic amines which comprises reacting a dihydric alcohol characterized by four to six carbons, preferably 1,5-pentane diol, with excess ammonia in presence of ZSM-5 catalyst modified with group of elements nickel, copper or cobalt-containing, at a temperature of at least 250° C., wherein said catalyst incorporates at least one metal.
Type:
Grant
Filed:
March 27, 2001
Date of Patent:
March 4, 2003
Assignee:
Council of Scientific and Industrial Research
Abstract: The present invention relates to an IgE antibody production inhibitor and an autoimmune disease suppressant containing a heterocyclic amide compound represented by the following general formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient
wherein R represents a hydrogen atom, alkyl, —CHO, —COOH, etc.; R5, R6 and R7 represent each hydrogen, alkyl, aryl, etc.; M represents a carbon atom or a nitrogen atom; Y represents aryl, etc.; and Z represents hydrogen, alkyl, aryl, etc.
Abstract: A bis(aminostyryl)benzene compound of the following general formula [I] is provided
wherein R2 and R3 independently represent an unsubstituted aryl group, and R1 and R4 independently represent an aryl group, and R5 to R8 independently represent a cyano group or the like. A process for the preparation thereof is described wherein a 4-(N,N-diarylamino)benzaldehyde and a diphosphonic acid ester or diphosphonium salt are, for example, subjected to condensation reaction. Intermediates of the bis(aminostyryl)benzene compound are also described.
Type:
Grant
Filed:
November 2, 2000
Date of Patent:
February 25, 2003
Assignee:
Sony Corporation
Inventors:
Mari Ichimura, Shinichiro Tamura, Tadashi Ishibashi, Ichinori Takada