Abstract: The present application describes modulators of CCR3 of formula (I):
or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
Type:
Grant
Filed:
June 20, 2001
Date of Patent:
October 28, 2003
Assignee:
Bristol-Myers Squibb Pharma Company
Inventors:
John V. Duncia, Joseph B. Santella, Dean A. Wacker, Wenqing Yao, Changsheng Zheng
Abstract: An aromatic sulfonyl alpha-cycloamino hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-cycloamino hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
Type:
Grant
Filed:
December 23, 1999
Date of Patent:
October 28, 2003
Assignee:
Pharmacia Corporation
Inventors:
Hui Li, Daniel P. Becker, Clara I. Villamil, Terri L. Boehm, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo
Abstract: Method of using anabaseine, DMAB-anabaseine, and anabaseine for stimulating brain cholinergic transmission and a method of making anabaseine.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
October 7, 2003
Assignee:
University of Florida
Inventors:
John A Zoltewicz, William R. Kem, Edwin M. Meyer
Abstract: Polymorphic crystalline forms of the antihistaminic drug norasternizole are disclosed. Processes for the production of the preferred polymorph are also disclosed.
Type:
Grant
Filed:
July 17, 2001
Date of Patent:
September 30, 2003
Assignee:
Sepracor Inc.
Inventors:
Roger P. Bakale, Chris Senanayake, Yaping Hong, Kostas Saranteas, Martin P. Redmon, Stephen A. Wald
Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4, or both m1 and m4, receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.
Type:
Grant
Filed:
April 27, 2001
Date of Patent:
September 30, 2003
Assignee:
Acadia Pharmaceuticals, Inc.
Inventors:
Carl-Magnus A. Andersson, Bo Lennart M. Friberg, Niels Skjaerbaek, Tracy A. Spalding, Allan K. Uldam
Abstract: The present invention relates to the production of a product compound having a structure according to Formulae IA and/or IB:
wherein
n is 0 or 1;
R1 is hydrogen or hydroxy;
R2 is hydrogen;
or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen;
R3 is —COOH or —COOR4;
R4 is an alkyl or aryl moiety;
A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, and alkoxy.
This process involves incubating a starting compound having a structure according to Formulae IIA and/or IIB:
wherein R3 is —CH3 and R1, R2, A, B, and D are defined above In the presence of a microorganism under conditions effective to produce the product compound.
Abstract: A disease treatment is provided by controlling the expression of a protein induced by a heat shock factor.
The novel compound benzo-1,3-dioxole provides an inhibitor of HSF activity or an inhibitor of inducing the production of a protein regulated by HSF, which inhibits the activity of a heat shock factor, a transcriptional regulatory factor, thereby in turn inhibiting transcription of a structural gene having a heat shock element sequence in the gene region for transcriptional regulation into RNA, and thus inhibiting translation of the gene into a protein, and resulting in inhibition of inducing production of RNA or protein encoded by the gene. It also provides a drug for treating or preventing cancer through thermotherapy and a drug for treating or preventing stress diseases such as depression.
Abstract: Novel compounds having general formula (I), and pharmaceutically and veterinarily acceptable salts thereof wherein R1, R2, R3, W, Y1, Y2, X, n and y are as defined above and processes for their preparation and intermediate compounds prepared therein. The novel compounds are useful for having utility in the treatment of pruritic dermatoses including allergic dermatitis and atopy in animals and humans.
Type:
Grant
Filed:
May 11, 2000
Date of Patent:
August 26, 2003
Assignee:
Pfizer Inc.
Inventors:
Richard Edward Armer, Christopher James Dutton, David Morris Gethin, Stephen Paul Gibson, Julian Duncan Smith, Ivan Tommasini
Abstract: Compounds of the formula:
wherein R1, Y, W, A and R2 are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases and nerve damage.
Type:
Grant
Filed:
September 1, 1999
Date of Patent:
August 26, 2003
Assignee:
Pfizer Inc.
Inventors:
David John Bull, Robert John Maguire, Michael John Palmer, Martin James Wythes
Abstract: The invention relates to novel diaryl naphthyl methane compounds having general formula I as shown herein below, and said compounds useful in the treatment of esterogen related disease or syndrome,
Pharmaceutical compositions comprising said novel methane derivatives, process for the preparation of the novel methane derivatives and methods for the treatment of esterogen related diseases or syndrome.
Type:
Grant
Filed:
March 31, 2000
Date of Patent:
August 26, 2003
Assignee:
Council of Scientific and Industrial Research
Abstract: A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I):
wherein R1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or —CO2R7 group in which R7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R1 is hydrogen atom and Z is ca
Abstract: This invention relates to (2R,3S,4R,5R)-2-amino-5-methylpiperidine-3,4-diol or a (2S,3S,4R,5R)-2-N-substituted-2-amino-5-methylpiperidine-3,4-diol represented by the general formula (I):
wherein R1 and R2 each are a hydrogen atom, or R1 is a hydrogen atom and R2 is a lower alkanoyl group or a lower &ohgr;-trihaloalkanoyl group, or R1 and R2 together denote phthaloyl group, and a pharmaceutically acceptable salt thereof. Said compound can be prepared from a (2S,3S,4R)-5-N-protected-2,3,4-O-tri-protected-5-aminopentane-1,2,3,4-tetraol by multi-steps of reactions.
Abstract: The present invention is directed to a novel crystalline hydrate of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]-phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene hydrochloride and uses for same, including inhibition of disease states associated with estrogen deprivation including cardiovascular disease, hyperlipidemia, and osteoporosis; and inhibition of other pathological conditions such as endometriosis, uterine fibrosis, estrogen-dependent cancer (including breast and uterine cancer), prostate cancer, benign prostatic hyperplasia, CNS disorders including Alzheimer's disease, prevention of breast cancer, and up-regulating ChAT.
Type:
Grant
Filed:
January 10, 2002
Date of Patent:
August 26, 2003
Assignee:
Eli Lilly and Company
Inventors:
Julie Kay Bush, Preston Charles Conrad, Merlyn Gerard Flom
Abstract: A composition, a process for producing the composition, and a process for producing a nitrile are disclosed. The composition is substantially anhydrous or free of water and comprises ammonia and an anti-foaming agent. The composition can be produced by contacting substantially anhydrous ammonia with an anti-foaming amount of an anti-foaming agent. The process for producing a nitrile comprises contacting a hydrocarbon with the composition disclosed herein.
Type:
Grant
Filed:
May 15, 2001
Date of Patent:
August 12, 2003
Assignee:
E. I. du Pont de Nemours and Company
Inventors:
Timothy P. Stauffer, Gregory P. Shankwitz
Abstract: The invention relates to an improved process for the preparation of N-carboxyanhydrides by reaction of the corresponding amino acid or one of its salts with phosgene, diphosgene and/or triphosgene in a solvent medium, characterized in that at least a portion of the reaction is carried out under a pressure of less than 1000 mbar. The N-carboxyanhydrides are thus obtained with better yields and an improved purity.
Abstract: A novel process for preparing the compounds of the formula I
where:
n is 0, 1 or 2;
R1, R2 are C1-C6-alkyl;
R3, R4, R5 are hydrogen or C1-C6-alkyl, or R4 and R5 together form a bond;
R6 is Cl, Br,
which comprises a synthesis sequence starting from 1,2-dialkylbenzenes of the formula II
with subsequent halogenation to give 3,6-dihalo-1,2-dialkylbenzenes, haloalkylation to give benzyl bromides, oxidation to give benzaldehydes, oximation, reaction with alkenes to give isoxazoles, conversion into thioethers and, if appropriate, oxidation to give sulfenyl or sulfonyl derivatives of the formula I.
Type:
Grant
Filed:
May 9, 2002
Date of Patent:
August 5, 2003
Assignee:
BASF Aktiengesellschaft
Inventors:
Michael Rack, Norbert Götz, Helmut Hagen, Wolfgang von Deyn, Ernst Baumann, Rene Lochtman, Joachim Gebhardt
Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides naphthalene compounds, intermediates, formulations, and methods.
Type:
Grant
Filed:
August 26, 1997
Date of Patent:
July 29, 2003
Assignee:
Eli Lilly and Company
Inventors:
Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones
Abstract: The present invention relates to novel herbicidal phenoxypropionic acid N-alkyl-N-2-fluorophenyl amide compounds represented in the following formula (1), a method for preparing thereof, their use to control barnyard grass produced from rice and composition as suitable herbicides.
wherein,
R is methyl or ethyl group;
X is hydrogen, halogen, cyano, C1˜C6 alkyl, C1˜C6 alkoxy, C1˜C3 haloalkyl substituted with 1 to 3 of halogen atom(s), C1˜C3 haloalkoxy substituted with 1 to 3 of halogen atom(s), C2˜C4 alkoxyalkoxy, phenox,benzyloxy, C2˜C6 alkenyl, C2˜C6 alkinyl, C2˜C6 alkenyloxy, C2˜C6 alkinyloxy, or phenyl group;
Y is hydrogen or fluoro;
n is an integer of 1 or 2 and when n is 2, X can be in a combination of other substituents.
Type:
Grant
Filed:
July 30, 2002
Date of Patent:
July 29, 2003
Assignee:
Dongbu Hannong Chemical Co., Ltd.
Inventors:
Dae Whang Kim, Hae Sung Chang, Young Kwan Ko, Jae Wook Ryu, Jae Chun Woo, Dong Wan Koo, Jin Seog Kim