Abstract: New intermediates of the formula (II)B described below for the synthesis of amidine derivatives of (−)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid, such as for example (S)-N-{4-[4-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)-carbonyl]-1-piperazinyl]phenyl}-2-thiophenecarboximidamide
wherein A′ is
X is —Z1—CO;
&rgr; is a bond or a heterocycle selected from the group consisting of piperidine, piperazine, homopiperazine, 2-methylpiperazine, 2,5-dimethyl-piperazine and 4-aminopiperidine;
Y is —Z2— or —NR3—Z2,
R3 is hydrogen, alkyl of 1 to 6 carbon atoms or —COR4,
R4 is alkyl of 1 to 6 carbon atoms;
Z1 and Z2 independently are a single bond or alkylene of 1 to 6 carbon atoms;
and R6 is hydrogen or OH.
Type:
Grant
Filed:
April 26, 2002
Date of Patent:
November 25, 2003
Assignee:
Societe de Conseils de Recherches et d'Applications
Scientifiques (S.C.R.A.S.)
Inventors:
Christine Le Breton, Eric Manginot, Jean-Bernard Cazaux
Abstract: In various embodiments, chromophores are described that include novel electron acceptors, novel electron donors, and/or novel conjugated bridges that are useful in nonlinear optical applications. In some embodiments, the present invention provides chromophore architectures wherein a chromophore contains more than one electron acceptor in electronic communication with a single electron donor, and/or more than one electron donor in electronic communication with a single electron acceptor. Also described is processes for providing materials comprising the novel chromophores and polymer matrices containing the novel chromophores. Electro-optic devices described herein contain one or more of the described electron acceptors, electron donors, conjugated bridges, or chromophores.
Type:
Application
Filed:
May 16, 2003
Publication date:
November 6, 2003
Inventors:
Diyun Huang, Tim Londergan, Galina K. Todorova, Jingsong Zhu
Abstract: The synthesis of novel, high &mgr;&bgr; electro-optical chromophores is described. These chromophores are polymerizable with a host polymer or copolymer. The chromophore polymerizable groups comprise epoxy, thioepoxy, oxetane and thiooxetane material which undergo a ring opening polymerization reaction in the presence of a cationic photoinitiator and actinic radiation. The high &mgr;&bgr; chromophores, mixed with a selected host polymer, copolymer, oligomer, or one or a plurality of polymerizable monomers, can be used to prepare optical waveguides and other optical elements and/or devices. The electro-optical chromophores of the invention can be used as a replacement for LiNbO3 in the formation of electro-optical devices, particularly electro-optical modulators.
Type:
Application
Filed:
April 30, 2002
Publication date:
October 30, 2003
Inventors:
Mingqian He, Paul J. Shustack, Jianguo Wang
Abstract: The present invention provides methods of making substituted phenylketoenols of the general formula I,
wherein V, W, X, Y, Z and Het are as defined herein. The compounds have pesticidal and herbicidal activity.
Type:
Grant
Filed:
January 28, 2002
Date of Patent:
October 7, 2003
Assignee:
Bayer Aktiengesellschaft
Inventors:
Hermann Hagemann, Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Peter Dahmen, Markus Dollinger, Alan Graff, Wolfram Andersch
Abstract: Process of treatment of mammals, including humans to treat diseases or conditions of the type which are normally treated with retinoid-like compounds is disclosed, with pharmaceutical compositions containing an active compound which is a selective agonist of the RXR retinoid receptor sites in preference to the RAR retinoid receptor sites. A compound is defined to be a selective agonist of the RXR receptor site if the compound is at least approximately ten times more effective as an agonist in the RXR receptor sites than in the RAR receptor sites.
Abstract: The present invention is concerned with a novel process for the preparation of compounds of formula I
comprising bromomethylation or chloromethylation of a compound of formula II
and subsequent reaction with a compound of formula IV
The compounds of formula I and the corresponding salts, e.g. the sodium salts, are pharmaceutically active substances.
Abstract: Novel selenophene compounds useful as anti-tumor agents are described. Preferred compounds include compounds of formula I:
wherein R1 and R2 are independently selected from the group consisting of;
H, CHO, CH2OH and CH2NH2; and
X and Y are independently selected from the group consisting of Se, S, O, NCH3 and NH. Pharmaceutical compositions and a method for treating patients having tumors utilizing the disclosed selenophene compounds are also described.
Type:
Grant
Filed:
February 1, 2002
Date of Patent:
September 16, 2003
Assignee:
Purdue Research Foundation
Inventors:
Ching-jer Chang, Curtis L. Ashendel, Darrick Kim
Abstract: Compounds of Formula (I),
wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are described.
Type:
Grant
Filed:
December 11, 2001
Date of Patent:
August 26, 2003
Assignees:
Wyeth, ArQule Inc.
Inventors:
Anthony F. Kreft, Derek C. Cole, Kevin R. Woller, Joseph R. Stock, George Diamantidis, Dennis M. Kubrak, Kristina M. Kutterer, William J. Moore, David S. Casebier, Lynn Resnick
Abstract: Novel non-psychotropic cannabinoids are disclosed and pharmaceutical compositions comprising these novel compounds are described for preventing neurotoxicity, neuroinflammation, immune or inflammatory disorders comprising as active ingredient the stereospecific (+) enantiomer, having (3S,4S) configuration of &Dgr;6 tetrahydrocannabinol type compounds. The compositions are particularly effective in alleviating and even preventing neurotoxicity due to acute injuries to the central nervous system, including mechanical trauma, compromised or reduced blood supply as may occur in cardiac arrest or stroke, or poisonings. They are also effective in the treatment of certain inflammatory disorders and chronic degenerative diseases characterized by neuronal loss and chronic pain including neuropathic pain.
Abstract: Taxanes having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
Abstract: Compounds of formula I
are useful for treating type II diabetes, obesity, hyperglycemia, inadequate glucose clearance, hyperinsulinemia, hypertriglyceridemia, and high-circulating glucocorticoid levels, preparations of the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Type:
Grant
Filed:
February 28, 2001
Date of Patent:
July 15, 2003
Assignee:
Abbott Laboratories
Inventors:
Philip R. Kym, Benjamin C. Lane, John K. Pratt, Tom Von Geldern, Martin Winn, Jehrod Brenneman, Jyoti R. Patel, David L. Arendsen, Irini Akritopoulou-Zanze, Kimba L. Ashworth, Kresna Hartandi
Abstract: Taxanes having a carbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
Abstract: Described are polymeric matrix compatibilized naphthopyran compounds, examples of which are certain 2H-naphtho[1,2-b]pyrans, 3H-naphtho[2,1-b]pyrans and indeno[2,1-f]naphtho[1,2-b]pyrans each having at least one substituent containing terminal and/or pendant groups selected from hydroxyl, carboxyl, sulfo, sulfono, (meth)acryloxy, 2-(methacryloxy)ethylcarbamyl, epoxy or a mixture thereof. Specific substituents are also present on the naphtho, indeno and/or pyrano portions of the compounds. These compounds may be represented by the following graphic formulae:
Also described are various substrates that contain or that are coated with such compounds. Optically clear articles such as contact lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, are also described.
Abstract: The invention provides photochromic bis-naphthopyran compounds as well as methods for their manufacture and their use. The bis-naphthopyran compounds of the invention exhibit a wide range of color, i.e., from pink to purple to blue gray, upon activation by a source of UV light. Additionally, the bis-naphthopyran compounds of the present invention exhibit broad coloration ability, fast response as to both color change on activation and return to original color, and good fatigue-resistance.
Abstract: Taxanes having a carbamoyloxy substituent at C(7), a hydroxy substituent at C(10, and a range of C(2), C(9), C(14), and side chain substituents.
Type:
Application
Filed:
February 6, 2002
Publication date:
March 27, 2003
Applicant:
Florida State University Research Foundation Inc.
Abstract: The invention relates to p-thienylbenzylamides of formula (I)
in which R(1), R(2), R(3), R(4), R(5), R(6) and X have the meanings given in the description. The compounds of formula (I) are potent agonists of angiotensin-(1-7) receptors and are useful as pharmaceutically active compounds to treat and/or prevent hypertension; cardiac hypertrophy; cardiac insufficiency; coronary heart diseases, such as angina pectoris; and endothelial dysfunction or endothelial damage as a consequence, for example, of atherosclerotic processes or in association with diabetes mellitus.
Abstract: The present invention provides substituted benzofuran, indene, thianaphthene and oxidized thianaphthene compounds and methods of treatment and pharmaceutical compositions that comprise such compounds. Preferred compounds of the invention contain benzofuran, indene or thianaphthene group substituted with a tetrahydrofuran or other alicyclic group.
Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.
Abstract: Heterocyclic aromatic amides having a hydroxy group adjacent to the amide functionality are useful as antifungal agents, particularly for plants.
Type:
Grant
Filed:
July 20, 2000
Date of Patent:
February 18, 2003
Assignee:
Dow AgroSciences LLC
Inventors:
Michael J. Ricks, William H. Dent, III, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesel, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Robert P. Gajewski
Abstract: A class of 3,4-diaryl substituted thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders.
Type:
Application
Filed:
July 1, 2002
Publication date:
January 16, 2003
Applicant:
G.D. Searle & Co.
Inventors:
John J. Talley, Stephen R. Bertenshaw, Paul W. Collins, Thomas D. Penning, David B. Reitz, Roland S. Rogers
Abstract: The invention relates to novel thienylsulphonylamino(thio)carbonyl compounds of the formula (I), 1
Type:
Application
Filed:
November 9, 2001
Publication date:
January 2, 2003
Inventors:
Klaus-Helmut Muller, Ernst Rudolf F. Gesing, Mark Wilhelm Drewes, Johannes Rudolf Jansen, Rolf Kirsten, Joachim kluth, Klaus Konig, Ulrich Philipp, Markus Dollinger
Abstract: The present invention provides a novel class of 4,5-diaryl-3(2H)-furanone derivatives, which inhibit strongly and selectively COX-2 over COX-1. They are useful to treat inflammation, inflammation-associated disorders, and COX-2 mediated diseases.
Type:
Grant
Filed:
November 27, 2001
Date of Patent:
December 10, 2002
Assignee:
Pacific Corporation
Inventors:
Song Seok Shin, Min-Soo Noh, Young Joo Byun, Jin Kyu Choi, Jin Kwan Kim, Kyung Min Lim, Ji Young Kim, Young Hoon Choi, Jun-Yong Ha, Ki-Wha Lee, Joo Hyun Moh, Yeon Su Jeong, Shin Chung, Yung Hyup Joo, Chang Hoon Lee, Seon Hwa Kang, Young-Ho Park, Jung Bum Yi
Abstract: Described are photochromic 2H-naphtho[1,2-] pyrans characterized by having an aromatic substituent in the 5 position. The aromatic group at 5-position of the naphthopyran is a substituted or unsubstituted aryl group or other substituted or unsubstituted aromatic group.
Abstract: Photochromic pyran compounds and their use in synthetic resin objects of all types, especially for ophthalmic applications, particularly spiro compounds having a fluorene structure derived from naphthopyrans, which are known as spirofluorenopyrans. By introducing respectively only one strongly electron donating or withdrawing group at specific positions in the periphery of the pyran dye, photochromic compounds obtained which in the excited state are distinguished by an expanded color spectrum, while simulataneously offering comparably good bleaching rates and good durability.
Abstract: Described are photochromic 2H-naphtho[1,2-b]pyrans characterized by having an aromatic substituent in the 5 position. The aromatic group at 5-position of the naphthopyran is a substituted or unsubstituted aryl group or other substituted or unsubstituted aromatic group. These compounds may be represented by the following graphic formula:
Also described are polymeric organic host materials that contain or that are coated with such compounds.
Abstract: A photochromic compound which by itself develops a color tone of a neutral tint, exhibits a large fading rate and offers a good photochromic light resistance.
Abstract: Compounds of the formula
where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.
Type:
Grant
Filed:
July 6, 2001
Date of Patent:
October 15, 2002
Assignee:
Allergan, Inc.
Inventors:
Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
Abstract: The present invention relates to novel substituted (&agr;,&bgr;-fused butyrolactones, to processes for their preparation and to their use for the prevention and/or treatment of disorders caused by hyper- or hypofunction of the glutamatergic system, in particular of cerebral ischaemias, craniocerebral trauma, states of pain or CNS-mediated spasms.
Type:
Grant
Filed:
July 14, 2000
Date of Patent:
October 8, 2002
Assignee:
Bayer Aktiengesellschaft
Inventors:
Andreas Stolle, Horst-Peter Antonicek, Stephen Lensky, Arnd Voerste, Thomas Müller, Jörg Baumgarten, Karsten von dem Bruch, Gerhard Müller, Udo Stropp, Ervin Horváth, Jean-Marie-Viktor de Vry, Rudy Schreiber
Abstract: A novel compound which inhibits certain integrins, particularly &agr;v integrins. Additionally, the novel compound may be used in a method of treating tumors or cancer which comprises administering a pharmaceutically effective amount of the compound to a patient. Additionally, the novel compound may be used in a method of inhibiting angiogensis. Finally, a method of producing the novel compound is disclosed.
Type:
Application
Filed:
January 16, 2002
Publication date:
September 26, 2002
Applicant:
BioChem Pharma Inc.
Inventors:
Denis Labrecque, Serge Lamothe, Marc Courchesne, Laval Chan, Giorgio Attardo, Karen Meerovitch
Abstract: Novel 3-phenyl-pyrones of the formula
in which
A, D, X and Y are each as defined in the description,
a process for preparing these substances and their use as pesticides, fungicides and herbicides.
Type:
Grant
Filed:
April 6, 2001
Date of Patent:
August 27, 2002
Assignee:
Bayer Aktiengesellschaft
Inventors:
Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Michael Ruther, Christoph Erdelen, Wolfram Andersch, Ulrike Wachendorff-Neumann, Gerd Hänssler, Astrid Mauler-Machnik, Klaus Stenzel
Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1
Type:
Application
Filed:
January 8, 2002
Publication date:
August 1, 2002
Inventors:
Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, Richard Cordova, Kevin Pan, Joseph Meschino
Abstract: The invention relates to cyclopentabenzofuran derivatives, processes for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-&kgr;B-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.
Type:
Grant
Filed:
March 26, 2001
Date of Patent:
July 16, 2002
Assignee:
Bayer Aktiengesellschaft
Inventors:
Walter Guarnieri, Thomas Jaetsch, Andreas Schoop, Jörg Baumgarten, Axel Kretschmer, Horst-Peter Antonicek
Abstract: Process for the preparation of compounds of formula (I), wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula (V), wherein the general symbols are as defined in claim 1, with carbon monoxide in the presence of a catalyst.
Type:
Grant
Filed:
December 22, 2000
Date of Patent:
July 9, 2002
Assignee:
Ciba Specialty Chemicals Corporation
Inventors:
Michael Tinkl, Samuel Evans, Peter Nesvadba
Abstract: This invention is to provide a compound of the formula:
wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of the formula:
wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an, optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof, which is useful for antagonizing MCP-1 receptor.